A method of treating vitiligo, including prophylaxis, in a subject in need thereof, comprising administering to said subject a pharmaceutically effective amount of a compound of Formula (I): (I) wherein: X is CR1 or N; Y is CH, C or N; R1 is hydrogen, C1-6alkoxy or C1-6alkyl; R2 is hydrogen, C1-6alkoxy, halo, -C(O)C1-6alkyl, CN, halo-C1-6alkyl or -C(O)NR4R5; R3 is hydrogen or C1-6alkoxy; R4 is hydrogen or C1-6alkyl: R5 is hydrogen or C1-6alkyl; and m and n are integers each independently selected from 1 and 2, or a pharmaceutically acceptable salt thereof.
A61K 31/00 - Medicinal preparations containing organic active ingredients
A61K 31/4439 - Non-condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
A61K 31/472 - Non-condensed isoquinolines, e.g. papaverine
A61K 31/4725 - Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
A61K 31/55 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
The present invention relates to a method of producing a recombinant protein in a host cell comprising adding Polyethyleneimine (PEI)during cell culture. Addition of PEI to the cell culture as a fermentation enhancer can result in reducing the viscosity of the cell culture, and/or increasing the extracellular concentration of the recombinant protein, and/or reducing the duration of cell culture to the point of harvest or protein recovery.
The present invention relates to denture adhesive compositions comprising a denture adhesive polymer and a bioactive glass, their use and methods of making such compositions.
The present disclosure relates to antigen binding proteins, such as antibodies, that bind to HER3, polynucleotides encoding such antigen binding proteins, pharmaceutical compositions comprising said antigen binding proteins and methods of manufacture. The present disclosure also concerns the use of such antigen binding proteins in the treatment or prophylaxis of diseases associated with breast cancer, ovarian cancer, prostate cancer, bladder cancer, pancreatic, gastric, melanoma and other cancers that overexpress HER3.
C07K 16/32 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against translation products from oncogenes
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
A package (10, 20, 30, 40, 50) which can be torn open by a user, comprising a polymer film material having a preferential tearing direction and defining a cavity for a product, wherein the polymer film material incorporates a bias (16, 24, 35, 56) facilitating tearing along a tear line oriented in a direction other than its preferential tearing direction and a tear initiation location (18, 26, 37, 41, 58) which facilitates tearing of the polymer film material in its preferential tearing direction to open the package, the tear line being adjacent to a tear initiation location. The polymer film material having a preferential tearing direction provides resistance against a child tearing open the package.
B65D 75/32 - Articles or materials enclosed between two opposed sheets or blanks having their margins united, e.g. by pressure-sensitive adhesive, crimping, heat-sealing, or welding one or both sheets or blanks being recessed to accommodate contents
A dispensing container (10) for extrudable fluid materials having a collapsible tubular body (11) with a dispensing nozzle (15) at one end (11A) and the opposite end (11B) being closed with an end wall member (20) biased to fold about a fold axis transverse to the longitudinal direction of the tubular body, wherein the end wall member either comprises a wall part of which two surfaces (81A, 81B) enclose a concave angle between them and being foldable about a fold axis in the direction of the length of the valley or the end wall member bulges convexly in a generally conical shape.
B65D 35/10 - Body construction made by uniting or interconnecting two or more components
B65D 35/24 - Pliable tubular containers adapted to be permanently deformed to expel contents, e.g. collapsible tubes for toothpaste or other plastic or semi-liquid material; Holders therefor with auxiliary devices
B65D 35/28 - Pliable tubular containers adapted to be permanently deformed to expel contents, e.g. collapsible tubes for toothpaste or other plastic or semi-liquid material; Holders therefor with auxiliary devices for expelling contents
The present invention relates to dentifrice compositions comprising low levels of a spherical fused silica particles as an abrasive agent and an orally acceptable carrier. Such compositions can effectively clean, polish and remove stains from the surface of teeth or dentures without a high degree of abrasion thereby reducing scratching and damage to the tooth or denture surface. Such compositions thereby provide superior cleaning, polishing, gentle stain removal and whitening of tooth surfaces or dentures.
The present invention is directed to improved efficacy for use of Alitretinoin in a patient population with Severe Refractory Chronic Hand Eczema (CHE).
The present invention relates to dentifrice compositions comprising spherical fused aluminium oxide particles as an abrasive agent and an orally acceptable carrier. Such compositions can effectively clean, polish and remove stains from the surface of teeth or dentures without a high degree of abrasion thereby reducing scratching and damage to the tooth or denture surface. Such compositions thereby provide superior cleaning, polishing, gentle stain removal and whitening of tooth surfaces or dentures.
Ready to drink milk beverage compositions are described comprising creatine and an added protein such as whey protein, which have good creatine shelf life at ambient temperatures.
A23C 11/10 - Milk substitutes, e.g. coffee whitener compositions containing at least one non-milk component as source of fats or proteins containing or not lactose but no other milk components as source of fats, carbohydrates or proteins
A dentifrice composition comprising a sintered hydroxyapatite abrasive agent providing good cleaning and whitening of the tooth surface, with minimimal dentine abrasivity.
The present invention relates to a dentifrice composition comprising a stannous salt e.g. stannous fluoride and a water-soluble alkali metal tripolyphosphate e.g. sodium tripolyphosphate and a non-aqueous carrier and wherein the composition is substantially free of any water and does not comprise a source of zinc ions or an aqueous buffer system.
Aqueous single phase oral care compositions are described comprising a fluoride salt and an unfunctionalised calcium phosphate compound, which is not β-tricalcium phosphate, characterised in that the calcium phosphate compound is present in a catalytic and fluoride-stable amount relative to the fluoride salt. Such compositions are of use in combating dental caries, dental erosion and/or tooth wear.
The present invention relates to a method of producing a recombinant protein by harvesting a microbial cell broth and adding an amount of a flocculant to achieve an effective particle size distribution. The present invention also relates to a method of clarifying a microbial harvest by adding an amount of a flocculant to achieve an effective particle size distribution.
The present invention is directed to pharmaceutical combination products comprising a muscarinic acetylcholine receptor antagonist, fluticasone propionate and salmeterol xinafoate, and to their use in the treatment of inflammatory or respiratory tract diseases.
A61K 31/137 - Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine
A61K 31/439 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom the ring forming part of a bridged ring system, e.g. quinuclidine
A61K 31/56 - Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
A61K 31/573 - Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone
A61P 11/00 - Drugs for disorders of the respiratory system
The present invention relates to pharmaceutical formulations comprising an anti-inflammatory glucocorticoid compound of the androstane series and levocabastine, an H1 antagonist/anti-allergic. The present invention also relates to therapeutic uses thereof, particularly for the treatment of inflammatory and allergic conditions, specifically rhinitis.
A61K 31/4418 - Non-condensed pyridines; Hydrogenated derivatives thereof having a carbocyclic ring directly attached to the heterocyclic ring, e.g. cyproheptadine
A61K 31/58 - Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
A guide device for assisting the application of a liquid from a dispenser to the eye of a subject has a mount to hold the liquid dispenser in the guide device, a rest (102) to align the guide device with the subject head, and an indicator (410), selectively visible to indicate when the guide device is tilted at or beyond a minimum guide angle. Preferably, the indicator is selectively visible to indicate when the guide device is tilted at, or between, the minimum guide angle and a maximum guide angle. Said minimum guide angle corresponds with a minimum predetermined tilt of the subject head suitable for delivery of the liquid from the dispenser. The maximum guide angle corresponds with a maximum predetermined tilt of the subject head suitable for delivery of the liquid.
A61F 9/00 - Methods or devices for treatment of the eyes; Devices for putting in contact-lenses; Devices to correct squinting; Apparatus to guide the blind; Protective devices for the eyes, carried on the body or in the hand
B05B 11/00 - Single-unit hand-held apparatus in which flow of contents is produced by the muscular force of the operator at the moment of use
19.
CATHEPSIN C INHIBITORS FOR TREATING CYSTIC FIBROSIS, NON-CYSTIC FIBROSIS BRONCHIECTASIS, AND ANCA-ASSOCIATED VASCULITIS
The present invention relates to methods of treatment of diseases mediated by the cathepsin C enzyme such as cystic fibrosis, non-cystic fibrosis bronchiectasis, and anti-neutrophil cytoplasmic auto antibody - related diseases.
A61P 11/00 - Drugs for disorders of the respiratory system
A61K 31/351 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom not condensed with another ring
A61K 31/4045 - Indole-alkylamines; Amides thereof, e.g. serotonin, melatonin
20.
MODULATORS OF THE RETINOID-RELATED ORPHAN RECEPTOR GAMMA (ROR-GAMMA) FOR USE IN THE TREATMENT OF AUTOIMMUNE AND INFLAMMATORY DISEASES
The present invention relates to novel retinoid-related orphan receptor gamma (RORϒ) modulators and their use in the treatment of diseases mediated by RORϒ.
C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 407/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 241/04 - Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
C07D 413/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 417/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
A61K 31/495 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene
A61K 31/506 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
A61K 31/501 - Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
A61K 31/497 - Non-condensed pyrazines containing further heterocyclic rings
21.
CONTAINER SYSTEM FOR MIXING AND DISPENSING A DRINK
A container system (10) for mixing and dispensing a drink comprising water and one or more additional substance, comprising a lower substance compartment (11) with an upper opening connectable to an upper dispensing compartment (14), and an upper dispensing compartment (14) comprising a vessel with a bottom opening (15) connectable to the opening of the lower compartment (11) to form a drinking vessel, with a mixing means between the bottom opening (15) and upper opening (17) of the upper compartment (14).
B65D 81/32 - Containers, packaging elements, or packages, for contents presenting particular transport or storage problems, or adapted to be used for non-packaging purposes after removal of contents for packaging two or more different materials which must be maintained separate prior to use in admixture
A47J 43/27 - Implements for preparing or holding food, not provided for in other groups of this subclass for mixing drinks; Hand-held shakers
The compounds of formula (I) of the subject invention are related to 2-substituted cephem compounds, which have a wide antimicrobial spectrum, in particular exhibit potent antimicrobial activity against beta-lactamase producing Gram negative bacteria, and pharmaceutical compositions comprising the same.
C07D 505/24 - Nitrogen atoms further acylated by radicals derived from carboxylic acids or by nitrogen or sulfur analogues thereof with the acylating radicals further substituted by hetero atoms or by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen further substituted by doubly-bound nitrogen atoms
A61K 31/546 - Compounds containing 5-thia-1-azabicyclo [4.2.0] octane ring systems, i.e. compounds containing a ring system of the formula , e.g. cephalosporins, cefaclor, cephalexine containing further heterocyclic rings, e.g. cephalothin
C07D 501/50 - Methylene radicals, substituted by hetero rings with the 7-amino radical acylated by an aliphatic carboxylic acid, which is substituted by hetero atoms
23.
INHIBITORS OF BROMODOMAIN-CONTAINING PROTEIN PCAF FOR THE TREATMENT OF AUTOIMMUNE AND INFLAMMATORY DISEASES OR FOR THE TREATMENT OF CANCER
A method of treating autoimmune and inflammatory diseases or conditions or cancer in a mammal, such as a human, which comprises the administration of an inhibitor of the bromodomain-containing protein PCAF.
A61K 31/7105 - Natural ribonucleic acids, i.e. containing only riboses attached to adenine, guanine, cytosine or uracil and having 3'-5' phosphodiester links
G01N 1/00 - Sampling; Preparing specimens for investigation
A dispenser (100) for the delivery of a droplet of a liquid comprises a housing (116) which defines an outlet orifice (220), a tip seal (502), biased against the housing to seal the outlet orifice, and a dosing pump (906) for pumping a liquid to the outlet nozzle. The dispenser further comprises an actuation pump (904) configured to provide a hydraulic opening force to the tip seal for opening of the outlet orifice. Preferably the actuation pump is configured to operate at a higher pressure than the dosing pump.
A61F 9/00 - Methods or devices for treatment of the eyes; Devices for putting in contact-lenses; Devices to correct squinting; Apparatus to guide the blind; Protective devices for the eyes, carried on the body or in the hand
25.
COMPOSITIONS COMPRISING A SINGLE VARIABLE DOMAIN AND CAMOSTAT MESYLATE (CM)
The present disclosure provides a means of stabilising a single variable domain, in particular in protease-rich environments such as the stomach and intestine. A composition, in particular a pharmaceutical composition, comprising a single variable domain and camostat mesylate is provided, together with uses of said composition as a medicament and in methods of treatment. Compositions of the disclosure are particularly useful in the topical treatment of gastrointestinal conditions, such as Crohn's Disease or ulcerative colitis, or for direct activity in the gut mucosal immune system.
The present disclosure provides a means of stabilising an antibody, in particular in protease-rich environments such as the stomach and intestine. A composition, in particular a pharmaceutical composition, comprising an antibody and camostat mesylate is provided, together with uses of said composition as a medicament and in methods of treatment. Compositions of the disclosure are particularly useful in the topical treatment of gastrointestinal conditions, such as Crohn's Disease or ulcerative colitis, or for direct activity in the gut mucosal immune system.
The present disclosure concerns antigen binding polypeptides and fragments thereof which specifically bind Low-density lipoprotein receptor-related protein 6 (LRP6) particularly human LRP6 (hl_RP6) and which inhibit the binding of Wnt ligands to the LRP6 receptor. Further disclosed are pharmaceutical compositions, screening and medical treatment methods.
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
The present invention relates to a process for the preparation of umeclidinium bromide, and to processes for preparing intermediates used in the preparation of umeclidinium bromide.
C07D 453/02 - Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing not further condensed quinuclidine ring systems
29.
2 - (AZAINDOL- 2 -YL) BENZ IMIDAZOLES AS PAD4 INHIBITORS
Compounds of formula (I) wherein; R1 is hydrogen or C1-6alkyl; R2 is hydrogen, C1-6alkyl, perhalomethylC0-5alkyl-O-, or C1-6alkoxy; R3 is hydrogen, C1-6alkyl, or C1-6alkoxyC1-6alkyl; R4 is hydrogen, C1-6alkyl, perhalomethylC1-6alkyl; or unsubstituted C3-6cycloalkylC1-6alkyl; A is C-R5 or N; B is C-R6 or N; D is C-R7 or N; with the proviso that at least one of A, B, and D, is N; R5 is hydrogen or C1-6alkyl; R6 is hydrogen or C1-6alkyl; R7 is hydrogen, C1-6alkyl, C1-6alkoxy, or hydroxy; R8 is hydrogen or C1-6alkyl, with the proviso that one of R4 and R8 is hydrogen; R9 is hydrogen or hydroxy; R10 is hydrogen or C1-6alkyl; and salts thereof are PAD4 inhibitors and may be useful in the treatment of various disorders, for example rheumatoid arthritis, vasculitis, systemic lupus erythematosus, ulcerative colitis, cancer, cystic fibrosis, asthma, cutaneous lupus erythematosis, and psoriasis.
A61K 31/407 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with heterocyclic ring systems, e.g. ketorolac, physostigmine
A61K 31/4184 - 1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
30.
OPTIMUM DOSE REGIME OF AN ANTI-NOGO-A ANTIBODY IN THE TREATMENT OF AMYOTROPHIC LATERAL SCLEROSIS
The invention relates to a method of treatment or prophylaxis of a neurological disorder, in particular but not exclusively amyotrophic lateral sclerosis (ALS), comprising administration of an anti-Nogo-A antibody.
There is provided an inhaler device comprising a housing, a mouthpiece, a seat for receiving a unit dose blister and a punch for piercing a lid of the unit dose blister. The housing comprises a base and a lid pivotally joined by a hinge, such that the lid is pivotable from a first 'closed' position in which it abuts the base to define a cavity, to a second 'open' position in which the cavity can be accessed. The seat and the punch are adapted to lie within the cavity when the lid is in the first 'closed' position and moving the lid from the 'open' position to the 'closed' position causes the punch to pierce a lid of a unit dose blister received in the seat. Only the lid of the unit dose blister is pierced.
The disclosure relates to nanoparticles comprising poly(octylcyanoacrylate) for oral administration of a biologically active polypeptide, in particular a metabolic peptide, such as exendin-4. Also disclosed are methods of producing such nanoparticles, pharmaceutical compositions comprising such nanoparticles and methods of treating metabolic disorders, such as obesity, using such nanoparticles.
The present invention is directed to novel retinoid-related orphan receptor gamma (RORγ) modulators, processes for their preparation, pharmaceutical compositions containing these modulators, and their use in the treatment of inflammatory, metabolic and autoimmune diseases mediated by RORγ.
C07C 311/21 - Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
C07C 311/29 - Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound oxygen atoms having the sulfur atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
C07C 311/44 - Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups having the sulfur atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring having sulfur atoms of sulfonamide groups and amino groups bound to carbon atoms of six-membered aromatic rings of the same carbon skeleton having the nitrogen atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
C07D 309/04 - Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
C07D 309/06 - Radicals substituted by oxygen atoms
C07D 319/12 - 1,4-Dioxanes; Hydrogenated 1,4-dioxanes not condensed with other rings
C07D 239/54 - Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals
C07D 205/04 - Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
C07D 265/30 - 1,4-Oxazines; Hydrogenated 1,4-oxazines not condensed with other rings
C07D 207/08 - Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon radicals, substituted by hetero atoms, attached to ring carbon atoms
C07D 265/32 - 1,4-Oxazines; Hydrogenated 1,4-oxazines not condensed with other rings with oxygen atoms directly attached to ring carbon atoms
The present invention is directed to novel retinoid-related orphan receptor gamma (RORγ) modulators, processes for their preparation, pharmaceutical compositions containing these modulators, and their use in the treatment of inflammatory, metabolic and autoimmune diseases mediated by RORγ.
C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
C07D 213/76 - Nitrogen atoms to which a second hetero atom is attached
C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 413/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
A re-sealable flexible sachet (10, 50) with a nozzle portion (14) which is foldable about a fold line (41, 52, 110) to constrict the outlet conduit (15) when the nozzle portion (14) is in the folded configuration, and the nozzle portion (14) has an ear (20A, 20B, 51) extending in a transverse direction with a corresponding slot opening (23A, 23B, 53) to receive the ear (20A, 20B, 51) to secure the nozzle portion (14) when the nozzle portion (14) is in the folded configuration.
C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 409/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
Oral care compositions comprising one or more active agents and hydroxypropyl cellulose, and that are liquid at or below room temperature and which form a two-phase cloudy system at body temperature. In certain embodiments the active agent is a mineralizing agent, an anti-caries agent, an anti-inflammatory agent, an antibacterial agent, an antifungal agent, an anti-malodour agent or a mixture thereof.
An apparatus and method using the apparatus for measuring target samples, particularly pharmaceutical products using Raman radiation. The sample (212) is located in an optically transparent aperture (210) in an optically non-transparent wall structure (208) with a reflective surface (250) on one or both of the sides of the wall structure (208) facing respectively the excitation radiation transmitter (220) or the Raman radiation detector (222). Preferably two reflective surfaces (250) each in hemispherical shape and facing each other in a spherical arrangement are provided, with the wall structure (208) across the diameter of the sphere.
The present invention provides compositions and methods useful for treating and preventing neovascular AMD by inhibition of CCR3. The compositions and methods are useful for treating and preventing diseases and disorders such as but not limited to, neovascular AMD.
A process for separating a compound from solution in organic solvent by a chromatographic process, in particular liquid-liquid chromatography, in which prior to the chromatographic process the composition of the solution is changed by means of a process of organic solvent nanofiltration for a solvent exchange. Additionally or alternatively subsequent to the chromatographic process the output from the chromatographic process is subjected to a process of organic solvent nanofiltration to remove residual target compound and/or impurities in the output for solvent recovery.
B01D 15/12 - Selective adsorption, e.g. chromatography characterised by constructional or operational features relating to the preparation of the feed
B01D 15/18 - Selective adsorption, e.g. chromatography characterised by constructional or operational features relating to flow patterns
B01D 15/24 - Selective adsorption, e.g. chromatography characterised by constructional or operational features relating to the treatment of the fractions to be distributed
The present Invention relates to cephalosporin antibacterial compounds of Formula (!): corresponding pharmaceutically acceptable salts thereof, corresponding pharmaceutical compositions, compound preparation and treatment methods for bacterial infections, especially those caused by gram-negative bacteria.
The present invention is directed to novel retinoid-related orphan receptor gamma (RORy) modulators of formula (I), processes for their preparation, pharmaceutical compositions containing these modulators, and their use in the treatment of inflammatory, metabolic and autoimmune diseases mediated by RORy wherein R1 to R7 are as defined in claim 1.
C07D 213/38 - Radicals substituted by singly-bound nitrogen atoms having only hydrogen or hydrocarbon radicals attached to the substituent nitrogen atom
C07D 213/65 - One oxygen atom attached in position 3 or 5
C07D 213/68 - One oxygen atom attached in position 4
C07D 213/75 - Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
C07D 233/22 - Radicals substituted by oxygen atoms
C07D 239/28 - Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
C07D 261/08 - Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
C07C 311/21 - Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
C07C 311/29 - Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound oxygen atoms having the sulfur atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
The present invention relates to modified HGF-1K1 polypeptides (such as that shown in Seq ID No:4), and certain mutations for the disruption of an identified glycosylation site, DNA sequences encoding those proteins (such as those sequences in Seq ID Nos: 5, 6 and 7) and various methods for their production. The invention also relates to pharmaceutical compositions containing the modified HGF-1K1 polypeptides and to their use in the treatment of various diseases such as COPD, broncheolitis obliterans, acute lung injury (ALI), idiopathic pulmonary fibrosis (IPF), myocardial infarction, liver fibrosis and kidney fibrosis.
C07C 317/14 - Sulfones; Sulfoxides having sulfone or sulfoxide groups bound to carbon atoms of six-membered aromatic rings
C07D 209/08 - Indoles; Hydrogenated indoles with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring
C07D 211/84 - Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
C07D 231/12 - Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
C07D 235/02 - Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
C07D 237/08 - Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
C07D 237/10 - Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
C07D 249/06 - 1,2,3-Triazoles; Hydrogenated 1,2,3-triazoles with aryl radicals directly attached to ring atoms
A61P 19/02 - Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
A61P 37/00 - Drugs for immunological or allergic disorders
46.
PROCESS FOR SEPARATION OF OLIGONUCLEOTIDE OF INTEREST FROM A MIXTURE
A method for separation of an oligonucleotide from a mixture using a biphasic mobile phase / stationary phase liquid - liquid chromatography system. A first mobile phase contains the oligonucleotide and the stationary phase contains an exchanger substance that removably binds to the target oligonucleotide. The mobile phase is caused to flow in contact with the stationary phase in a liquid - liquid chromatography apparatus such that the oligonucleotide becomes bound to the exchanger substance in the liquid stationary phase. The oligonucleotide is then displaced from the liquid stationary phase into a second liquid mobile phase by means of a displacer substance able to displace the oligonucleotide from the stationary phase into the second mobile phase.
C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
A61K 31/4545 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
48.
BENZOFURAN COMPOUNDS FOR THE TREATMENT OF HEPATITIS C VIRUS INFECTIONS
The present invention features compounds of formula (I) and salts thereof, pharmaceutical compositions comprising said compounds, and uses of such compounds in treating or preventing viral infections, such as HCV infections, and diseases associated with such infections.
A01N 43/30 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one or more oxygen or sulfur atoms as the only ring hetero atom with two or more hetero atoms five-membered rings with two hetero atoms in positions 1,3 with two oxygen atoms in positions 1,3, condensed with a carbocyclic ring
A61K 31/36 - Compounds containing methylenedioxyphenyl groups, e.g. sesamin
49.
MODIFIED SINGLE VARIABLE DOMAIN ANTIBODIES WITH REDUCED BINDING TO ANTI-DRUG-ANTIBODIES
The present invention relates to modified proteins and peptides that have reduced ability to bind to pre-existing antibodies. Such modified protein/peptide molecules can comprise C-terminal additions, extensions or tags and/or certain amino acid substitutions. Such modified molecules (e.g. fusions and conjugates) comprise proteins, peptides, antigen binding molecules, antibodies or antibody fragments such as single variable domains e.g. human immunoglobulin (antibody) single variable domains, and also single variable domains derived from non-human sources such as a llama or camel, e.g. a VHH including a nanobodyTM (described in e.g. WO 94/04678 and WO 95/04079 inter alia). The invention further relates to uses, formulations, compositions comprising such modified C terminally extended and/or amino acid substituted molecules and also to methods of production and expression of these molecules.
C07K 16/00 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies
C07K 16/22 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against growth factors
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
The invention relates to non-aqueous dentrfrice compositions comprising a surfactant system. The surfactant system consists of a combination of surfactants i.e. a betaine and a taurate surfactant; or a betaine and an alkyl sulphate surfactant; or a betaine, a taurate and an alkyl sulphate surfactant.
The present invention is directed to antigen binding constructs comprising one or two epitope binding domains separated by a single chain Fc region of an antibody, wherein each epitope binding domain in capable of binding to VEGF, to dimers comprising two antigen binding constructs of the invention, pharmaceutical compositions comprising said dimers and their use in the treatment of diseases associated with VEGF signalling, such as diabetic macular edema (DME), wet age-related macular degeneration (Wet AMD), diabetic retinopathy, retinal vein occlusion (RVO), and corneal neovascularisation, and polynucleotide sequences encoding said antigen binding constructs.
Disclosed are 2,3-dihydroimidazo[1,2-c]pyrimidin-5(1H)-one compounds that inhibit Lp-PLA2, processes for their preparation, compositions containing them and their use in the treatment of diseases associated with the activity of Lp-PLA2, for example atherosclerosis, Alzheimer's disease.
A61K 31/519 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
The present invention relates to novel bicyclic pyrimidone compounds that inhibit Lp-PLA2 activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases associated with the activity of Lp-PLA2, for example atherosclerosis, Alzheimer's disease.
A61K 31/519 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
54.
TNF -ALPHA ANTIGEN- BINDING PROTEINS WITH INCREASED FCRN BINDING
The present invention provides antigen binding proteins which bind specifically to TNF-alpha. For example novel variants of anti-TNF antibodies such as adalimumab which show increased binding to the FcRn receptor or increased half life compared to adalimumab. Also provided are compositions comprising the antigen binding proteins and uses of such compositions in treatment of disorders and disease.
C07K 16/24 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against cytokines, lymphokines or interferons
In general, the present invention relates to uses of voltage-gated sodium channel blocker compounds,, which include corresponding precursors, intermediates, monomers and dimers, corresponding pharmaceutical compositions, compound preparation and treatment methods for respiratory and respiratory tract diseases. In particular, the present invention also relates to methods and uses for treatment of respiratory or respiratory tract diseases, which comprises administering to a subject in need thereof an effective amount of a compound of the present invention.
A pharmaceutical formulation for intravenous (IV) administration comprising 2-(S)-(4-Fluoro-2- methyl-phenyl)-piperazine-1-carboxylic acid [1-(R)-(3,5-bis-trifluoromethyl-phenyl)-ethyl]-methyl-amide or a pharmaceutically acceptable salt thereof and a process for its preparation and its use in medical therapy.
A61K 47/48 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers, inert additives the non-active ingredient being chemically bound to the active ingredient, e.g. polymer drug conjugates
The invention relates to TNFR1 binding proteins, in particular those which are capable of preventing dimerisation of TNFR1 chains, and to their use in therapy.
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
A61K 39/395 - Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
Dry powder inhalers comprising a muscarinic acetylcholine receptor antagonist and optionally a beta 2 agonist and/or a corticosteroid for use in the treatment of inflammatory or respiratory tract diseases, such as asthma or COPD.
A61K 31/138 - Aryloxyalkylamines, e.g. propranolol, tamoxifen, phenoxybenzamine
A61K 31/439 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom the ring forming part of a bridged ring system, e.g. quinuclidine
A61K 31/58 - Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
The present invention is directed to the combination of a muscarinic receptor antagonist and a corticosteroid, and the use of said combination in treating diseases mediated via the M3 muscarinic acetylcholine receptor and/or the glucocorticoid receptor, such as asthma.
A61K 31/138 - Aryloxyalkylamines, e.g. propranolol, tamoxifen, phenoxybenzamine
A61K 31/439 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom the ring forming part of a bridged ring system, e.g. quinuclidine
A61K 31/58 - Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
The present invention concerns antigen binding proteins and fragments thereof which specifically bind B Cell Maturation Antigen (BCMA), particularly human BCMA (hBCMA) and which inhibit the binding of BAFF and APRIL to the BCMA receptor. Further disclosed are pharmaceutical compositions, screening and medical treatment methods.
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
A61K 47/48 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers, inert additives the non-active ingredient being chemically bound to the active ingredient, e.g. polymer drug conjugates
61.
COMPOUNDS AND METHODS FOR THE IDENTIFICATION OF HISTONE DEMETHYLASE INTERACTING MOLECULES AND FOR THE PURIFICATION OF HISTONE DEMETHYLASE PROTEINS
The present invention relates to immobilization compounds, immobilization products and preparations thereof as well as methods and uses for the identification of histone demethylase interacting compounds or for the purification or identification of histone demethylase proteins.
C07D 295/135 - Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms with the ring nitrogen atoms and the substituent nitrogen atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
A61K 31/198 - Alpha-amino acids, e.g. alanine, edetic acid (EDTA)
A compound of Formula (I) or a pharmaceutically acceptable salt thereof, wherein R1 represents a group selected from: i) phenyl optionally substituted with one or two substituents independently selected from Me, OMe, CF3, F, CI and NMe2; ii) furanyl, thiophenyl, pyrrolyl, pyridyl, cyclohexyl or naphthyl, each of which is optionally substituted with one or two substituents independently selected from Me, OMe, CF3, F, CI and NMe2; and iii) benzo[1,3]dioxo5-yl or 2,3-dihydrobenzo[1,4]dioxin-6-yl; R2 represents CF3, C1-4alkyl, or CHF2; When R1 represents optionally substituted furanyl, thiophenyl, pyrrolyl, pyridyl or naphthyl, R3 represents Et; When R1 represents optionally substituted cyclohexyl, R3 represents Et or Me; Otherwise R3 represents Et, Me, Br or OMe, compositions containing them, their use in therapy, for example in the treatment of tuberculosis, and methods for the preparation of such compounds, are provided, together with certain novel compounds
Disclosed herein are antisense compounds and methods for decreasing HBV mRNA, DNA and protein expression. Such methods, compounds, and compositions are useful to treat, prevent, or ameliorate HBV-related diseases, disorders or conditions.
C07H 21/04 - Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids with deoxyribosyl as saccharide radical
A61K 48/00 - Medicinal preparations containing genetic material which is inserted into cells of the living body to treat genetic diseases; Gene therapy
64.
N- CYCLOBUTYL - IMIDAZOPYRIDINE - METHYLAMINE AS TRPV1 ANTAGONISTS
A compound of formula (I) wherein X represents a H atom, or a CH2OH group, Y represents a H atom, or a CH2OH group, but X and Y are not both CH2OH groups and Ar is selected from formulae (IA) and (IB) or a pharmaceutically acceptable salt thereof, useful as TRPY1(VR-1) antagonists.
A61K 31/437 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
A61P 25/02 - Drugs for disorders of the nervous system for peripheral neuropathies
65.
COMPOSITIONS COMPRISING FUSION PROTEINS OR CONJUGATES WITH AN IMPROVED SERUM HALF-LIFE
The present invention relates to drug fusions and conjugates that have improved serum half lives. These fusions and conjugates comprise immunoglobulin (antibody) single variable domains and insulintropic and/or incretin and/or gut peptide molecules. The invention further relates to uses, formulations, compositions and devices comprising such drug fusions and conjugates. The invention also relates to compositions which comprise more than one insulintropic and/or incretin and/or gut peptide molecules present as part of a fusion or conjugate and to uses and formulations thereof.
A61K 39/395 - Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
A61K 47/48 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers, inert additives the non-active ingredient being chemically bound to the active ingredient, e.g. polymer drug conjugates
C07K 16/18 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans
The present invention relates to drug fusions and conjugates that have improved serum half lives. These fusions and conjugates comprise immunoglobulin (antibody) single variable domains and insulintropic and/or incretin and/or gut peptide molecules. The invention further relates to uses, formulations, compositions and devices comprising such drug fusions and conjugates. The invention also relates to compositions which comprise more than one insulintropic and/or incretin and/or gut peptide molecules present as part of a fusion or conjugate and to uses and formulations thereof.
A61K 47/48 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers, inert additives the non-active ingredient being chemically bound to the active ingredient, e.g. polymer drug conjugates
C12N 15/62 - DNA sequences coding for fusion proteins
An oral care composition which is a liquid at or below room temperature and which forms a two-phase cloudy system at body temperature and wherein the composition comprises a water-soluble non-ionic polymer, such as HPC, having a cloud point in the composition at a temperature no higher than about 38°C, for combating (i.e. helping to prevent, inhibit and/or treat) dentinal hypersensitivity.
An air filter material comprising an air permeable substrate having a composition comprising a poly-(carboxylic acid) polymer; a monomeric carboxylic acid; and an anionic and/or non-ionic surfactant deposited on it wherein the weight ratio monomeric carboxylic acid : poly-(carboxylic acid) polymer is in the range 10 : 1 to 2 : 1, and the loading of the composition on the substrate is 1-20 g/m2. The air filter material is suitable for a face mask to neutralize airborne viral and bacterial pathogens.
A compound of formula (I) or a salt thereof; which is an inhibitor of spleen tyrosine kinase (SYK) and therefore potentially of use in treating diseases resulting from inappropriate activation of mast cells, macrophages, and B-cells and related inflammatory responses and tissue damage, for instance inflammatory diseases and/or allergic conditions, in cancer therapy, specifically heme malignancies, and autoimmune conditions.
C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
A compound of formula (I) or a salt thereof; which is an inhibitor of spleen tyrosine kinase (Syk) and therefore potentially of use in treating diseases resulting from inappropriate activation of mast cells, macrophages, and B-cells and related inflammatory responses and tissue damage, for instance inflammatory disease and/or allergic disorders, and in cancer therapy, specifically heme malignancies, and autoimmune conditions.
C07D 519/00 - Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups or
A61K 31/4985 - Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
Provided herein is a method for identifying a patient as a candidate for treatment with an aggrecanase inhibitor. Also provided is a method of evaluating the effectiveness of an aggrecanase inhibitor. In one aspect the present invention is directed to a method for identifying a patient as a candidate for treatment with an aggrecanase inhibitor comprising: isolating a biological sample from a patient; and detecting in the sample the presence or absence of at least one aggrecan degradation product; wherein the presence of at least one aggrecan degradation product in the biological sample indicates that the patient is a good candidate for treatment.
The present invention provides novel antigen-binding proteins derived from human germline VH domains, having improved expression and improved biophysical characteristics.
Provided are retinoid-related orphan receptor gamma(ROR γ) modulators of formula (I), processes for their preparation, pharmaceutical compositions containing them, and their uses in the treatment of diseases mediated by ROR γ.
C07D 333/26 - Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulfur atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
A61K 31/381 - Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
Disclosed are retinoid-related orphan receptor gamma (RORγ) modulators of Formula (I) and their use in the treatment of diseases mediated by RORγ, wherein the radicals have the meanings as defined in the invention.
This invention relates to a novel chemical process for the synthesis of 2-ethyoxycarbonylamino-5-(4-fluorobenzylamino)-nitrobenzene and its use in the preparation of 2-amino-4-(4-fluorobenzylamino)-1-ethoxycarbonylaminobenzene (retigabine/ezogabine) and its polymorphic forms thereof.
C07C 269/04 - Preparation of derivatives of carbamic acid, i.e. compounds containing any of the groups the nitrogen atom not being part of nitro or nitroso groups from amines with formation of carbamate groups
C07C 269/06 - Preparation of derivatives of carbamic acid, i.e. compounds containing any of the groups the nitrogen atom not being part of nitro or nitroso groups by reactions not involving the formation of carbamate groups
C07C 271/28 - Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atom of at least one of the carbamate groups bound to a carbon atom of a six-membered aromatic ring to a carbon atom of a non-condensed six-membered aromatic ring
The disclosure provides an anti -TGFbetaRII immunoglobulin single variable domain. Suitably, an anti -TGFbetaRII immunoglobulin single variable domain in accordance with the disclosure is one having an amino acid sequence as set forth in any one of SEQ ID NO: 1-38, 204, 206, 208, 214, 234, 236, 238, 240, 263, 265, 267, 269, 271, 273, 275, 277, 279, 281, 283, 285, 287, 289 or 291 having up to 5 amino acid substitutions, deletions or additions. The disclosure further provides a polypeptide and pharmaceutical composition for treating a disease associated with TGFbeta signalling and suitably a disease selected from the group of: tissue fibrosis, such as pulmonary fibrosis, including idiopathic pulmonary fibrosis; liver fibrosis, including cirrhosis and chronic hepatitis; rheumatoid arthritis; ocular disorders; fibrosis of the skin, including keloid of skin; Dupuytren's Contracture; kidney fibrosis such as nephritis and nephrosclerosis; wound healing; scarring reduction; and a vascular condition, such as restenosis.
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
77.
AZABICYCLO [4.1.0] HEPT - 4 - YL DERIVATIVES AS HUMAN OREXIN RECEPTOR ANTAGONISTS
C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
A61K 31/444 - Non-condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
A61K 31/506 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
A61K 31/444 - Non-condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
A61K 31/506 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
A61K 31/53 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
A61P 25/00 - Drugs for disorders of the nervous system
Disclosed herein is novel process for preparation of atovaquone, which process includes reacting1H-2-benzopyran-1,4(3H)-dione with 4-(4-chlorophenyl)cyclohexanecarbaldehyde. The invention further discloses novel intermediates useful in the preparation of atovaquone.
C07C 50/32 - Quinones containing groups having oxygen atoms singly bound to carbon atoms the quinoid structure being part of a condensed ring system having two rings
The present invention provides compositions and methods useful for treating and preventing ocular diseases by inhibition of Lp-PLA2. The compositions and methods are useful for treating and preventing diseases and disorders such as but not limited to, macular edema, uveitis and diabetic retinopathy.
A61K 31/00 - Medicinal preparations containing organic active ingredients
A61K 31/135 - Amines, e.g. amantadine having aromatic rings, e.g. methadone
A61K 31/517 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
A61K 31/7088 - Compounds having three or more nucleosides or nucleotides
Disclosed are compounds that inhibit Lp-PLA2 activity, processes for their preparation, compositions containing them and their use in the treatment of diseases associated with the activity of Lp-PLA2, for example atherosclerosis, Alzheimer's disease, and/or diabetic macular edema.
C07D 213/64 - One oxygen atom attached in position 2 or 6
C07D 239/36 - One oxygen atom as doubly bound oxygen atom or as unsubstituted hydroxy radical
C07D 401/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
A61K 31/4412 - Non-condensed pyridines; Hydrogenated derivatives thereof having oxo groups directly attached to the heterocyclic ring
A61K 31/513 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
82.
PYRIMIDINONE COMPOUNDS FOR USE IN THE TREATMENT OF DISEASES OR CONDITIONS MEDIATED BY LP - PLA2
The present invention relates to novel compounds that inhibit Lp-PLA2 activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases associated with the activity of Lp-PLA2, for example atherosclerosis, Alzheimer's disease, and/or diabetic macular edema (I).
C07D 401/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
C07D 403/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
C07D 413/06 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
C07D 417/06 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
A method of determining cleanliness of a manufacturing area is disclosed. The method of determining cleanliness of a manufacturing area comprising swabbing at least one target area within the manufacturing area, placing the swab in a testing apparatus, analyzing for the presence of the at least one substance with the testing apparatus and determining in real time the cleanliness of the manufacturing area.
A compound of formula (I) wherein X1 represents a hydrogen atom, or a CH2OH group X2 represents a hydrogen atom, a fluorine atom, an OCH3 group or a CH2OH group, and at least one of X1 and X2 is hydrogen Y represents a carbon atom and Z represents a nitrogen atom or Y represents a nitrogen atom and Z represents a carbon atom; R1 represents a halogen atom, a C1-4 alkyl group, a trifluoromethyl group or a trifluoromethoxy group, and R2 are R3 each independently selected from a hydrogen atom, a halogen atom, a C1-4 alkyl group, a trifluoromethyl group or a trifluoromethoxy group; or a pharmaceutically acceptable salt or solvate thereof.
A61K 31/437 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
The invention relates to improved anti-serum albumin immunoglobulin single variable domains, as well as ligands and drug conjugates comprising such variable domains, compositions, nucleic acids, vectors and hosts.
The present invention concerns antigen binding proteins and fragments thereof which specifically bind Oncostatin M (OSM), particularly human OSM (hOSM) and which inhibit the binding of OSM to the gp130 receptor but does not directly interact with site II residues. The invention also concerns a method of humanising antibodies. Further disclosed are pharmaceutical compositions, screening and medical treatment methods.
C07K 16/24 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against cytokines, lymphokines or interferons
The invention relates to combinations of HGF-antagonists with VEGF antagonists, and provides antigen-binding proteins which bind to HGF comprising a protein scaffold which are linked to one or more epitope-binding domains wherein the antigen-binding protein has at least two antigen binding sites at least one of which is from an epitope binding domain and at least one of which is from a paired VH/VL domain, methods of making such constructs and uses thereof.
A method of treating autoimmune and inflammatory diseases or conditions in a mammal, such as a human, which comprises the administration of a inhibitor of bromodomain-containing protein: SP140.
The present invention features compounds of formula (I): and salts thereof, pharmaceutical compositions comprising said compounds, and uses of such compounds in treating or preventing viral infections, such as HCV infections, and diseases associated with such infections.
A01N 43/42 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one nitrogen atom as the only ring hetero atom six-membered rings condensed with carbocyclic rings
The present invention features compounds of formula (I): and salts thereof, pharmaceutical compositions comprising said compounds, and uses of such compounds in treating or preventing viral infections, such as HCV infections, and diseases associated with such infections.
A01N 43/40 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one nitrogen atom as the only ring hetero atom six-membered rings
The present invention is directed to novel pharmaceutical compositions comprising lamivudine and adefovir dipivoxil in a single dosage form, and the use of such compositions in the treatment of hepatitis B virus (HBV) infection.
A61K 9/48 - Preparations in capsules, e.g. of gelatin, of chocolate
A61K 47/26 - Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
A61K 31/7068 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
A61K 31/675 - Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
A61P 1/16 - Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
92.
POLYMORPHS AND SALTS OF 6-(1H-INDOL-4-YL)-4-(5- { [4-(1-METHYLETHYL)-1-PI PERAZINYL] METHYL} -1,3-OXAZOL-2-YL)-1H-INDAZOLE AS PI3K INHIBITORS FOR USE IN THE TREATMENT OF E.G. RESPIRATORY DISORDERS
The present invention is directed to a polymorph of a compound of formula (II) and salts and polymorphs thereof, which is an inhibitor of PI3 kinase activity.
C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
A61K 31/422 - Oxazoles not condensed and containing further heterocyclic rings
A method of treating autoimmune and inflammatory diseases or conditions or cancer in a mammal, such as a human, which comprises the administration of an inhibitor of the bromodomain-containing protein: BAZ1B.
A method of treating autoimmune and inflammatory diseases or conditions in a mammal, such as a human, which comprises the administration of an inhibitor of the bromodomain-containing protein: SP110.
A method of treating autoimmune and inflammatory diseases or conditions in a mammal, such as a human, which comprises the administration of an inhibitor of the bromodomain-containing protein: ATAD2.
Polypeptides containing JMJD3 catalytic activity, amino acid and nucleotide sequences encoding the same, and uses and the crystal structure thereof, are provided.
G06F 19/16 - for molecular structure, e.g. structure alignment, structural or functional relations, protein folding, domain topologies, drug targeting using structure data, involving two-dimensional or three-dimensional structures
97.
N-2-(2-PYRIDINYL)-4-PYRIMIDINYL-BETA-ALANINE DERIVATIVES AS INHIBITORS OF HISTONE DEMETHYLASE JMJD3
A method of treating autoimmune diseases or conditions in a mammal, such as a human, which comprises the administration of a therapeutically effective amount of histone demethylase enzymes of formula (I).
C07D 403/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
C07D 409/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
A61K 31/506 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
A61K 31/4155 - 1,2-Diazoles not condensed and containing further heterocyclic rings
A compound of Formula (I) or a pharmaceutically acceptable salt thereof: (I), Wherein: Het is a 5 to 10-membered heteroaromatic ring; Either X is N and Y is CR5; or X is C and Y is S; Z is selected from N and CH; R1 is selected from H and C1-2alkyl; R2 is selected from H, C1-2alkyl, OH, -CH2OH and C1-2alkoxy; Each R3 is independently selected from OH, C1-3alkyl, F, Cl, Br, NH2, and C1-3alkoxy; R4 is selected from C1-3alkyl and haloC1-3alkyl; R5 is selected from H, C1-3alkyl and haloC1-3alkyl; R6 and R7 are either i) each independently selected from H, C1-3alkyl and C1-3alkoxy; or ii) R6 and R7 together with the ring to which they are attached form a 9-membered bicylic ring; p is 0-3; and RA is selected from H and C1-3alkyl, compositions containing them, their use in therapy, for example in the treatment of tuberculosis, and methods for the preparation of such compounds, are provided.
C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
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