The invention relates to use of surfactants of the formula 1 M+ formula 1 wherein R corresponds to an aliphatic radical selected from the group consisting of a mixture of n-dodecyl and n-tetradecyl; n-dodecyl; isotridecyl; a mixture of n- tetradecyl and n- hexadecyl; and n-hexadecyl; A denotes a polyalkoxylene group which is built up from only ethoxylene or propoxylene radicals, wherein the monomers may be different and the oligo- or polyalkoxylene unit are built up from the monomers blockwise or as a statistical mixture; M denotes the cation of potassium; and x denotes a number between 1 and 10, as an adjuvant for agrochemical products.
A01N 25/30 - Biocides, pest repellants or attractants, or plant growth regulators, characterised by their forms, or by their non-active ingredients or by their methods of application; Substances for reducing the noxious effect of the active ingredients to organisms other than pests characterised by the surfactants
A01N 57/20 - Biocides, pest repellants or attractants, or plant growth regulators containing organic phosphorus compounds having phosphorus-to-carbon bonds containing acyclic or cycloaliphatic radicals
This invention relates to novel substituted 5-(1-benzothiophen-2-yl)pyrrolo[2,1-f][1,2,4]triazin-4-amine derivatives having protein tyrosine kinase inhibitory activities, to processes for the preparation of such compounds, to pharmaceutical compositions containing such compounds, and to the use of such compounds or compositions for treating proliferative disorders, in particular cancer and tumor diseases.
This invention relates to novel substituted 5-(1-benzothiophen-2-yl) pyrrolo[2,1-f][1,2,4]triazin-4-amine derivatives of formula (I) wherein R1 is hydrogen, chloro, methyl or methoxy, R2 is hydrogen or methoxy, with the proviso that at least one of R1 and R2 is other than hydrogen, G1 represents chloro, (C1-C4)-alkyl, (C1-C4)-alkoxycarbonyl, 5-membered aza-heteroaryl, or the group -CH2-OR3, -CH2-NR4R5 or -C(=0)- NR4R6, and G2 represents chloro, cyano, (C1-C4)-alkyl, or the group - CR8AR8B-OH, -CH2-NR9R10, -C(=0)-NR11R12 or -CH2-OR15, having protein tyrosine kinase inhibitory activities, to processes for the preparation of such compounds, to pharmaceutical compositions containing such compounds, and to the use of such compounds or compositions for treating proliferative disorders, in particular cancer and tumor diseases.
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
This invention relates to novel substituted 5-(1-benzothiophen-2-yl)pyrrolo[2,1-fJ[1,2,4] triazin-4-amine derivatives having protein tyrosine kinase inhibitory activities, to processes for the preparation of such compounds, to pharmaceutical compositions containing such compounds, and to the use of such compounds or compositions for treating proliferative disorders, in particular cancer and tumor diseases.
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
The invention relates to novel tyrosine based linkers that allow the releasable connection of peptides or proteins with other molecular entities, e.g. polyethylene glycol, to processes for their preparation and their use for preparing medicaments for the treatment and/or prophylaxis of diseases.
The invention relates to novel polyethylene glycol (PEG) based prodrug of Adrenomedullin, to processes for preparation thereof, to the use thereof for treatment and/or prevention of diseases, and to the use thereof for producing medicaments for treatment and/or prevention of diseases, especially of cardiovascular, edematous and/or inflammatory disorders.
A61K 47/60 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
The present invention relates to disubstituted 5-fluoro pyrimidine derivatives containing a sulfoximine group of general formula (I) as described and defined herein, and methods for their preparation, their use for the treatment and/or prophylaxis of disorders, in particular of hyper-proliferative disorders and/or virally induced infectious diseases and/or of cardiovascular diseases. The invention further relates to intermediate compounds useful in the preparation of said compounds of general formula (I).
C07D 405/04 - 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 directly linked by a ring-member-to-ring- member bond
8.
NEUTRALIZING PROLACTIN RECEPTOR ANTIBODY MAT3 AND ITS THERAPEUTIC USE
The neutralizing prolactin receptor antibody Mat3. and antigen binding fragments, pharmaceutical compositions containing them and their use in the treatment or prevention of benign disorders and indications mediated by the prolactin receptor such as endometriosis, adenomyosis, non-hormonal female contraception, benign breast disease and mastalgia, lactation inhibition, benign prostate hyperplasia, fibroids, hyper- and normoprolactinemic hair loss, and cotreatment in combined hormone therapy to inhibit mammary epithelial cell proliferation and for the treatment and prevention of antiestrogen - resistant breast cancer. The antibody blocks prolactin receptor-mediated signalling.
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
A61P 5/00 - Drugs for disorders of the endocrine system
9.
4-ARYL-N-PHENYL-1,3,5-TRIAZIN-2-AMINES CONTAINING A SULFOXIMINE GROUP
The present invention relates to 4-aryl-N-phenyl-1,3,5,-triazin-2-amines containing a sulfoximine group of general formula (I) or (Ia): , and methods for their preparation, and their use for the treatment and/or prophylaxis of disorders, in particular of hyper-proliferative disorders and/or virally induced infectious diseases and/or of cardiovascular diseases. The invention further relates to intermediate compounds useful in the preparation of said compounds of general formula (I) or (Ia).
C07C 311/13 - Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an unsaturated carbon skeleton containing rings the carbon skeleton containing six-membered aromatic 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 9/00 - Drugs for disorders of the cardiovascular system
A61P 31/00 - Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
C07D 251/16 - Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hydrogen or carbon atoms directly attached to at least one ring carbon atom to only one ring carbon atom
C07D 251/22 - Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hydrogen or carbon atoms directly attached to at least one ring carbon atom to two ring 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 405/04 - 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 directly linked by a ring-member-to-ring- member bond
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
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
What is described is a process for producing high-purity gadobutrol in a purity (according to HPLC) of more than 99.7or 99.8 or 99.9% and the use for preparing a pharmaceutical formulation for parenteral administration. The process is carried out using specifically controlled crystallization conditions. The more recent developments in the field of the gadolinium-containing MR contrast agents (EP 0448191 B1, CA Patent 1341176, EP 0643705 B1, EP 0986548 B1, EP 0596586 B1) include the MRT contrast agent gadobutrol (Gadovist® 1.0) which has been approved for a relatively long time in Europe and more recently also in the USA under the name Gadavist®.
The present application relates to compounds of the formula (I): (see formula I) to processes for their preparation, to their use for the treatment and/or prevention of diseases and to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of cardiovascular diseases.
C07C 233/55 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a six-membered aromatic ring having the carbon atom of the carboxamide group bound to a carbon atom of an unsaturated carbon skeleton
A61K 31/195 - Carboxylic acids, e.g. valproic acid having an amino group
A61P 9/00 - Drugs for disorders of the cardiovascular system
12.
VISUAL INFORMATION SYSTEM AND COMPUTER MOBILITY APPLICATION FOR FIELD PERSONNEL
A system for providing visual crop data to a mobile device includes at least one server computer in communication with a mobile device. The at least one server computer is configured to receive location data relating to a geographical position of the mobile device; retrieve topographical data associated with at least a portion of the location data; generate shape data based at least partially on the topographical data; and transmit at least a portion of the shape data to the mobile device, such that at least one shape is visually displayed on at least a portion of a map image displayed on the mobile device. Also disclosed is a computer-implemented method and computer program product for providing and/or interacting with visual crop data, including appropriately communicatively connected hardware components.
G01V 9/00 - Prospecting or detecting by methods not provided for in groups
13.
USE OF 2-AMINO-N-[7-METHOXY-8-(3-MORPHOLIN-4-YLPROPOXY)-2,3-DIHYDROIMIDAZO[1,2-C]QUINAZOLIN-5-YL]PYRIMIDINE-5-CARBOXAMIDE IN THE TREATMENT OR PREVENTION OF BREAST CANCER
The present invention relates to use of 2-amino-N-[7-methoxy-8-(3-morpholin-4-ylpropoxy)-2,3-dihydroimidazo[1,2- c]quinazolin-5-yl]pyrimidine-5-carboxamide as the sole therapeutic or prophylactic agent in the treatment or prophylaxis of inflammatory breast cancer, triple negative breast cancer, Her2 receptor positive breast cancer, or hormone receptor positive breast cancer, or to a combination of 2-amino-N-[7- methoxy-8-(3-morpholin-4-ylpropoxy)-2,3-dihydroimidazo[1,2-c]quinazolin-5- yl]pyrimidine-5-carboxamide with ABT-737 or rapamycin, or both.
A61K 31/517 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
The present invention relates : - to 2-amino-N-[7-methoxy-8-(3-morpholin-4- ylpropoxy)-2,3-dihydroimidazo- [1,2-c] quinazolin-5-yl]pyrimidine-5-carboxamide dihydrochloride salt of formula (II) : or a tautomer, solvate or hydrate thereof; - to methods of preparing said dihydrochloride salt; - to said dihydrochloride salt for the treatment and/or prophylaxis of a disease; - to the use of said dihydrochloride salt for the preparation of a medicament for the treatment and/or prophylaxis of a disease, in particular of a hyper- proliferative and/or angiogenesis disorder, more particularly for the treatment or prophylaxis of a cancer, particularly lung cancer, in particular non-small cell lung carcinoma, colorectal cancer, melanoma, pancreatic cancer, hepatocyte carcinoma, pancreatic cancer, hepatocyte carcinoma or breast cancer; - to a pharmaceutical composition comprising said dihydrochloride salt; and - to a pharmaceutical combination comprising said dihydrochloride salt in combination with one or more further pharmaceutical agents.
The present invention relates to disubstituted triazine derivatives and/or pharmaceutically acceptable salts thereof, the use of these derivatives as pharmaceutically active agents, especially for the prophylaxis and/or treatment of infectious diseases, including opportunistic diseases, immunological diseases, autoimmune diseases, cardiovascular diseases, cell proliferative diseases, inflammation, erectile dysfunction and stroke, and pharmaceutical compositions containing at least one of said disubstituted triazine derivatives and/or pharmaceutically acceptable salts thereof. Furthermore, the present invention relates to the use of said disubstituted triazine derivatives as inhibitors for a protein kinase.
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
A61K 31/5355 - Non-condensed oxazines containing further heterocyclic rings
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
The invention relates to novel 2-acyloxypyrrolin-4-ones of the formula (I) in which A, B, G, W, X, Y and Z have the meaning given above, to a plurality of processes and intermediates for their preparation, and to their use as pesticides and/or herbicides. The invention also relates to selective herbicidal compositions comprising, firstly, the 2-acyloxypyrrolin-4-ones and, secondly, a crop plant compatibility-improving compound. The present invention furthermore relates to the boosting of the action of crop protection compositions comprising, in particular, 2-acyloxypyrrolin-4-ones, through the addition of ammonium salts or phosphonium salts and optionally penetrants, to the corresponding compositions, to processes for producing them and to their application in crop protection as insecticides and/or nematicides and/or acaricides and/or for preventing unwanted plant growth. (see above formula)
A01N 43/36 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one nitrogen atom as the only ring hetero atom five-membered rings
A01N 43/38 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one nitrogen atom as the only ring hetero atom five-membered rings condensed with carbocyclic rings
A01N 43/90 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having two or more relevant hetero rings, condensed among themselves or with a common carbocyclic ring system
The present invention relates to disubstituted pyridine derivatives of formula (l) and/or pharmaceutically acceptable salts thereof, the use of these derivatives as pharmaceutically active agents, especially for the prophylaxis and/or treatment of infectious diseases, including opportunistic diseases, immunological diseases, autoimmune diseases, cardiovascular diseases, cell proliferative diseases, inflammation, erectile dysfunction and stroke, and pharmaceutical compositions containing at least one of said disubstituted pyridine derivatives and/or pharmaceutically acceptable salts thereof. Furthermore, the present invention relates to the use of said disubstituted pyridine derivatives as inhibitors for a protein kinase. (see formula I)
The present invention relates to a process for the production of sized and/or wet- strength papers, paperboards or cardboards, wherein an aqueous radiation-curable dispersion containing water and at least one polymer, characterized in that the polymer contains cationic groups, is mixed with suspended wood pulp and/or chemical pulp and this mixture is sieved, pressed, thermally dried and then radiation-cured, characterized in that the dispersion is employed in amounts, based on its non-aqueous content in relation to the solid content of the wood pulp and/or chemical pulp, of from 0.001 to 10 wt.%, the papers, paperboards and cardboards produced by this process, and compositions comprising suspended wood pulp and/or chemical pulp and an aqueous radiation-curable dispersion containing at least one polymer, characterized in that the polymer contains cationic groups.
The present application relates to sodium 1-[6-(morpholin-4-yl)pyrimidin-4-yl]-4-(1H-1,2,3-triazol-1-yl)-1H-pyrazol-5- olate, to processes for its preparation, to its use for the treatment and/or prophylaxis of diseases and to its use for the preparation of medicaments for the treatment and/or prophylaxis of diseases, in particular cardiovascular and haematological diseases and kidney diseases, and for promoting wound healing.
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
A61K 31/506 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
A61P 9/00 - Drugs for disorders of the cardiovascular system
20.
AMINOALCOHOL SUBSTITUTED 2,3-DIHYDROIMIDAZO[1,2-C]QUINAZOLINE DERIVATIVES USEFUL FOR TREATING HYPER-PROLIFERATIVE DISORDERS AND DISEASES ASSOCIATED WITH ANGIOGENESIS
This invention relates to novel 2,3-dihydroimidazo[1,2 -c]quinazoline compounds, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for phosphotidylinositol-3-kinase ( PI3K) inhibition and treating diseases associated with phosphotidylinositol-3-kinase ( PI3K) activity, in particular treating hyper-proliferative and/or angiogenesis disorders, as a sole agent or in combination with other active ingredients.
The present invention relates to an ALS inhibitor herbicide tolerant Beta vulgaris plant and parts thereof comprising a mutation of an endogenous acetolactate synthase (ALS) gene, wherein the ALS gene encodes an ALS polypeptide containing an amino acid different from tryptophan at a position 569 of the ALS polypeptide.
The present invention relates to novel low-monomer low-viscosity high-activity formulations composed of isocyanurate containing isocyanate groups, exclusively based on 2,4-diisocyanatotoluene and phthalate-free plasticizers, to the use thereof as adhesion promoters with improved adhesion for coating compositions based on plasticized polyvinyl chloride, and to coatings and coated substrates.
The present invention relates to a very low-dosed dosage form for hormone replacement therapy (HRT). More particularly, the present invention concerns a solid oral dosage form comprising about 0.5 mg estradiol and about 0.25 mg drospirenone, and at least one pharmaceutically acceptable excipient. Despite the very low E2 and DRSP doses it has surprisingly been found that a high proportion of the women suffering from moderate to severe hot flushes actually respond to this treatment. Accordingly, the dosage form of the invention may be used as maintenance HRT or may be used already when HRT is initiated.
A61K 31/565 - Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. oestrane, oestradiol
A61K 31/57 - 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
A61P 15/12 - Drugs for genital or sexual disorders; Contraceptives for climacteric disorders
24.
PHARMACEUTICALLY ACTIVE DISUBSTITUTED TRIAZINE DERIVATIVES
The present invention relates to disubstituted triazine derivatives and/or pharmaceutically acceptable salts thereof, the use of these derivatives as pharmaceutically active agents, especially for the prophylaxis and/or treatment of infectious diseases, including opportunistic diseases, immunological diseases, autoimmune diseases, cardiovascular diseases, cell proliferative diseases, inflammation, erectile dysfunction and stroke, and pharmaceutical compositions containing at least one of said disubstituted triazine derivatives and/or pharmaceutically acceptable salts thereof. Furthermore, the present invention relates to the use of said disubstituted triazine derivatives as inhibitors for a protein kinase. formula (I) wherein R1 is formula (II), formula (III) or formula (IV).
C07D 251/22 - Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hydrogen or carbon atoms directly attached to at least one ring carbon atom to two ring carbon atoms
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 37/00 - Drugs for immunological or allergic disorders
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 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 407/04 - 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 directly linked by a ring-member-to-ring- member bond
25.
SILICON-CONTAINING BIODEGRADABLE MATERIAL FOR ANTI-INFLAMMATORY THERAPY
The present invention relates to the field of silicon-containing materials for treating certain inflammatory diseases. In particular, the invention provides a silicon- containing, biodegradable material for preventing and/or treating diseases that are associated with increased interleukin-1.beta. and/or interleukin-6 and/or interleukin-8 activity and/or that can be treated by lowering said cytokine activity, wherein the silicon-containing, biodegradable material is a polyhydroxysilicic acid ethyl ester compound of the general formula H[OSigO12(OH)x(OC2H5)6-x]n OH, in which x stands for 2 to 5 and n > 1, and wherein the diseases are as defined herein.
The present invention relates to novel low-monomer-content, low-viscosity, high-activity preparations made of isocyanurates containing isocyanate groups and of phthalate-free plasticizers, to use of the same as adhesion promoters with improved adhesion for coating compositions based on plasticized polyvinyl chloride, and also to coatings and coated substrates.
C08G 18/02 - Polymeric products of isocyanates or isothiocyanates of isocyanates or isothiocyanates only
C08G 18/18 - Catalysts containing secondary or tertiary amines or salts thereof
C08G 18/70 - Polymeric products of isocyanates or isothiocyanates with compounds having active hydrogen characterised by the isocyanates or isothiocyanates used
C08G 18/79 - Nitrogen characterised by the polyisocyanates used, these having groups formed by oligomerisation of isocyanates or isothiocyanates
C08L 27/06 - Homopolymers or copolymers of vinyl chloride
C09D 127/06 - Homopolymers or copolymers of vinyl chloride
27.
NEUTRALIZING PROLACTIN RECEPTOR ANTIBODIES AND THEIR THERAPEUTIC USE
The present invention is directed to the neutralizing prolactin receptor antibody 006- H08, as well as maturated forms thereof, and antigen-binding fragments, pharmaceutical compositions containing them and their use in the treatment or prevention of benign disorders and indications mediated by the prolactin receptor such as endometriosis, adenomyosis, non-hormonal female contraception, benign breast disease and mastalgia, lactation inhibition, benign prostate hyperplasia, fibroids, hyper- and normoprolactinemic hair loss, and cotreatment in combined hormone therapy to inhibit mammary epithelial cell proliferation. The antibodies of the invention block prolactin receptor-mediated signaling.
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
A61P 5/08 - Drugs for disorders of the endocrine system of the anterior pituitary hormones, e.g. TSH, ACTH, FSH, LH, PRL, GH for decreasing, blocking or antagonising the activity of the anterior pituitary hormones
The present invention relates to antibodies or antigen-binding fragments thereof that antagonize prolactin receptor (PRLR)-mediated signaling and that bind to the extracellular domain of PRLR or a human polymorphic variant thereof. The antibody or antigen-binding fragment comprises 3 heavy chain complementarity- determining regions (HCDRs) and 3 light chain complementarity-determining regions (LCDRs), each specifically defined by sequence.
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
A61P 5/08 - Drugs for disorders of the endocrine system of the anterior pituitary hormones, e.g. TSH, ACTH, FSH, LH, PRL, GH for decreasing, blocking or antagonising the activity of the anterior pituitary hormones
The invention relates to an injector containing a processor, a pump or a motor with advance for a piston, which is suitable for driving liquid out of a cartridge, a data storage device, a device for data transfer, wherein the processor is electronically connected to the data storage device, to a control unit for the pump or the motor, and to the device for data transfer; wherein the injector is suitable for being connected to a container or a cartridge for fluid transfer, which container or cartridge contains a multiplicity of doses of a parenteral solution; wherein a data storage device is fixedly connected to the container or the cartridge; wherein the device for data transfer is suitable for reading out information from the data storage device on the container or the cartridge; and wherein at least one specification in respect of the identity of the product stored in the container or in the cartridge is stored in the data storage device on the container or the cartridge. The invention furthermore relates to a container or a cartridge, which contains a multiplicity of doses of a parenteral solution, wherein a data storage device is fixedly connected to the container or the cartridge. The invention furthermore relates to
A61M 5/168 - Means for controlling media flow to the body or for metering media to the body, e.g. drip meters, counters
G16H 20/17 - ICT specially adapted for therapies or health-improving plans, e.g. for handling prescriptions, for steering therapy or for monitoring patient compliance relating to drugs or medications, e.g. for ensuring correct administration to patients delivered via infusion or injection
The invention concerns a process for the preparation of the calcium complex of 10-(2,3-Dihydroxy-1 -(hydroxymethyl)propyl)-1,4,7,10-tetraazacyclododecane- 1,4,7-triacetic acid, also known as Calcobutrol, starting from the pure gadolinium complex (Gadobutrol). The invention furthermore concerns Calcobutrol with a hitherto unknown level of purity.
The invention relates to 17-hydroxy-17-pentafluorethyl-estra-4,9(10)-dien-11-aryl derivatives of formula (I) exhibiting progesterone-antagonistic effects and to methods for the production thereof, to the use thereof for the treatment and/or prophylaxis of diseases and to the use thereof for producing medicaments for the treatment and/or prophylaxis of diseases, in particular uterine fibroids (myomas, uterine leiomyomas), endometriosis, menorrhagia, meningiomas, hormone-dependent mammary carcinomas and menopause-associated troubles, or for fertility control and emergency contraception.
C07J 31/00 - Normal steroids containing one or more sulfur atoms not belonging to a hetero ring
A61K 31/567 - Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. oestrane, oestradiol substituted in position 17 alpha, e.g. mestranol, norethandrolone
The present invention provides immunoconjugates composed of antibodies, e.g., monoclonal antibodies, or antibody fragments that bind to mesothelin, that are conjugated to cytotoxic agents, e.g., maytansine, or derivatives thereof, and/or co-administered or formulated with one or more additional anti-cancer agents. The immunoconjugates of the invention can be used in the methods of the invention to treat and/or diagnose and/or monitor cancers, e.g. solid tumors. The immunoconjugates comprise antibodies and functional fragments containing such antigen-binding regions that are specific for the membrane-anchored, 40 kDa mesothelin polypeptide, which which is overexpressed in several tumors, such as pancreatic and ovarian tumors, mesothelioma and lung cancer cells.
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
The crystalline Polymorph B of N-(2-aminophenyl)-4-[N-(pyridine-3-yl)methoxy- carbonyaminomethyl] benza-mide (MS-275) of formula (I) is described, as well as the process for the production of said compound, and its use as a medica-ment for the treatment of selected diseases.
The present invention provides recombinant antigen-binding regions and antibodies and functional fragments containing such antigen-binding regions that are specific for the membrane- anchored, 40.kDa mesothelin polypeptide, which is overexpressed in several tumors, such as pancreatic and ovarian tumors, mesothelioma and lung cancer cells. These antibodies, accordingly, can be used to treat these and other disorders and conditions. Antibodies of the invention also can be used in the diagnostics field, as well as for further investigating the role of mesothelin in the progression of disorders associated with cancer. The invention also provides nucleic acid sequences encoding the foregoing antibodies, vectors containing the same, pharmaceutical compositions and kits with instructions for use.
C07K 16/30 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants from tumour cells
A61K 39/395 - Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
The present application relates to substituted 4-ary1-1,4-dihydro-1,6- naphthyridine-3- carboxamides of the formula (I): (see formula I) wherein D, Ar, R1, R2 and R3 are described herein, a process for their preparation, and their use as mineralocorticoid receptor 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 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
37.
SUBSTITUTED DIHYDROPYRAZOLONES FOR TREATING CARDIOVASCULAR AND HAEMATOLOGICAL DISEASES
The present application relates to novel substituted dihydropyrazolone derivatives of formula (I): (see formula I) wherein R1, R2 and R3 are as described in the specification, processes for their preparation, their use for treatment and/or prophylaxis of diseases and their use for the preparation of medicaments for treatment and/or prophylaxis of diseases, in particular cardiovascular and hematological diseases and kidney diseases, and for promoting wound healing.
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
A61K 31/41 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
A61K 31/435 - 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
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
A61P 7/00 - Drugs for disorders of the blood or the extracellular fluid
A61P 9/00 - Drugs for disorders of the cardiovascular system
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
38.
SUBSTITUTED 2,3-DIHYDROIMIDAZO[1,2-C]QUINAZOLINE DERIVATIVES USEFUL FOR TREATING HYPER-PROLIFERATIVE DISORDERS AND DISEASES ASSOCIATED WITH ANGIOGENESIS
This invention relates to novel 2,3-dihydroimidazo[1,2-c]quinazoline compounds, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for phosphotidylinositol-3-kinase (PI3K) inhibition and treating diseases associated with phosphotidylinositol-3-kinase (PI3K) activity, in particular treating hyper-proliferative and/or angiogenesis disorders, as a sole agent or in combination with other active ingredients.
The present invention relates to combinations of A) oxazolidinones of the formula (I) with B) acetylsalicylic acid (aspirin) and C) an ADP receptor antagonist, in particular P2Y12 purino receptor blocker, a process for producing these combinations and the use thereof as medicaments, in particular for the prophylaxis and/or treatment of thromboembolic disorders.
A61K 31/4365 - 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 having sulfur as a ring hetero atom, e.g. ticlopidine
A61P 9/04 - Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
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 43/00 - Drugs for specific purposes, not provided for in groups
40.
METHOD OF SELECTIVELY CONTROLLING MORNING GLORY SPP
A method of selectively controlling morning glory spp., by treating a lower portion of a hill of morning glory spp. with one compound or a combination of two or more compounds selected from glufosinate, L-glufosinate, bialaphos, paraquat, diquat and agriculturally acceptable salts of the compounds.
A01N 57/20 - Biocides, pest repellants or attractants, or plant growth regulators containing organic phosphorus compounds having phosphorus-to-carbon bonds containing acyclic or cycloaliphatic radicals
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
A01N 43/90 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having two or more relevant hetero rings, condensed among themselves or with a common carbocyclic ring system
Compounds of the formula (I) in which A, B, G, W, X, Y and Z can have the meanings given in the description are highly suitable for controlling animal pests such as insects and/or spider mites and/or nematodes by treating the soil/growth substrate by drenching or drip application or dipping or soil injection.
A01N 47/06 - Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a carbon atom not being member of a ring and having no bond to a carbon or hydrogen atom, e.g. derivatives of carbonic acid the carbon atom having no bond to a nitrogen atom containing —O—CO—O— groups; Thio-analogues thereof
A01N 43/38 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one nitrogen atom as the only ring hetero atom five-membered rings condensed with carbocyclic rings
Compounds of the formula (I) (see formula I) in which A, B, G, W, X, Y and Z can have the meanings given in the description are highly suitable for controlling animal pests such as insects and/or spider mites and/or nematodes by treating the soil/growth substrate by drenching or drip application or dipping or soil injection.
A01N 47/06 - Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a carbon atom not being member of a ring and having no bond to a carbon or hydrogen atom, e.g. derivatives of carbonic acid the carbon atom having no bond to a nitrogen atom containing —O—CO—O— groups; Thio-analogues thereof
A01N 43/38 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one nitrogen atom as the only ring hetero atom five-membered rings condensed with carbocyclic rings
The present invention relates to a method for the reliable and reproducible preparation of 4-[17.beta.-methoxy-17.alpha.-methoxymethyl-3-oxoestra-4,9-dien-ll.beta.- yl]benzaldehyde (E)-oxime (asoprisnil) on the pilot and manufacturing scale. Asoprisnil, which is prepared by this method, is distinguished by a very good physical stability and is therefore particularly suitable for the manufacture of solid pharmaceutical forms (tablets, coated tablets, etc.).
A61K 31/567 - Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. oestrane, oestradiol substituted in position 17 alpha, e.g. mestranol, norethandrolone
C07J 1/00 - Normal steroids containing carbon, hydrogen, halogen, or oxygen, not substituted in position 17 beta by a carbon atom, e.g. oestrane, androstane
C07J 75/00 - Processes for the preparation of steroids, in general
44.
USE OF ESTRADIOL VALERATE OR ESTRADIOL COMBINED WITH DIENOGEST FOR THE ORAL THERAPY OF DYSFUNCTIONAL UTERINE BLEEDING IN THE FORM OF ORAL CONTRACEPTIVES
The invention relates to the use of estradiol valerate or estradiol combined with 17a- cyanomethyl-17-~-hydroxyestra-4,9-diene-3on (dienogest) for producing a multi-phase combination preparation for the oral therapy of the dysfunctional uterine bleeding in the form of oral contraceptives. Said combination of estradiol valerate or estradiol with dienogest comprises a first phase consisting of 2 daily dose units of estradiol valerate at 3 mg or estradiol of less than 3mg, a second phase consisting of 2 groups of daily dose units, whereby the first group contains 5 daily dose units of a combination of 2 mg estradiol valerate or estradiol of less than 2mg and 2 mg of dienogest and the second group contains 17 daily dose units consisting of a combination of 2 mg of estradiol valerate or estradiol of less than 2mg and 3 mg dienogest, a third phase consisting of 2 daily dose units having 1 mg estradiol valerate or estradiol of less than 2mg and an additional phase consisting of 2 daily dose units on a pharmaceutically harmless placebo. All of the daily dose units of the multi-phase combination and the pharmaceutically harmless placebo correspond to 28 days. The duration of application comprises at least one menstruation cycle and is dependent on individual wishes of the woman with respect to contraception.
A61K 31/565 - Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. oestrane, oestradiol
A61K 31/57 - 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
A61P 15/00 - Drugs for genital or sexual disorders; Contraceptives
The present invention relates to solid pharmaceutical dosage forms which can be administered orally and comprise 5-chloro-N-({5S)-2-oxo-3-[4-(3-oxo-4-morpholinyl)phenyl]- 1,3-oxazolidin-5-yl}methyl)-2-thiophenecarboxamide in amorphous form and/or thermodynamically metastable crystal modification and have rapid release of active ingredient, and to process for the production thereof, the use thereof as medicament, the use thereof for the prophylaxis, secondary prophylaxis and/or treatment of disorders, and to the use thereof for producing a medicament for the prophylaxis, secondary prophylaxis and/or treatment of disorders.
The present invention relates to a novel polymorphic form of 5-chloro-N-({(5S)-2-oxo-3-[4-(3-oxo-4-morpholinyl)-phenyl]-1,3-oxazolidin-5-yl- methyl)-2-thiophenecarboxamide, processes for their preparation and medicaments comprising these forms.
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 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
The present invention relates to a novel amorphous form of 5-chloro-N-({(5S)-2- oxo-3-[4-(3- oxo-4-morpholinyl)-phenyl]-1,3-oxazolidin-5-yl}-methyl)-2- thiophenecarboxamide, processes for its preparation and medicaments comprising the form.
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 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
48.
2-AMINOETHOXYACETIC ACID DERIVATIVES AND THEIR USE
The present application relates to novel 2-aminoethoxyacetic acid derivatives, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and also to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular thromboembolic disorders.
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
The present application relates to novel drug formulations of vardenafil which dissolve rapidly in the mouth and lead to increased bioavailability and to a plateau-like plasma concentration profile, and to processes for their preparation.
A61K 9/22 - Sustained or differential release type
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
50.
USE OF TETRAMIC ACID DERIVATIVES FOR CONTROLLING INSECTS FROM THE GENUS OF THE PLANT LICE (STERNORRHYNCHA)
The present invention relates to the use of a compound of the formula (I): (see formula I) wherein: G is CO2C2H5, in the form of an isomer mixture or pure isomer for controlling insects from the suborder of Sternorrhyncha, except for the use against Myzus persicae on brassica vegetable, Aphis gossypii on cotton and Bemisia tabaci on cotton.
A01N 43/38 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one nitrogen atom as the only ring hetero atom five-membered rings condensed with carbocyclic rings
A01N 47/06 - Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a carbon atom not being member of a ring and having no bond to a carbon or hydrogen atom, e.g. derivatives of carbonic acid the carbon atom having no bond to a nitrogen atom containing —O—CO—O— groups; Thio-analogues thereof
A01N 25/00 - Biocides, pest repellants or attractants, or plant growth regulators, characterised by their forms, or by their non-active ingredients or by their methods of application; Substances for reducing the noxious effect of the active ingredients to organisms other than pests
51.
LOW-FOAMING AQUEOUS FORMULATIONS USED FOR CROP PROTECTION
A liquid aqueous crop protectant composition, comprising: (a) 1% to 40% by weight of a water-soluble active crop protectant ingredient of the formula (1) or a salt thereof: (see formula 1) wherein Z1 represents a radical of the formula -OM, -NHCH(CH3)CONHCH(CH3)CO2M or -NHCH(CH3)CONHCH[CH2CH(CH3)2]CO2M and wherein M represents H or a salt-forming cation; (c) 0% to 40% by weight of a polar organic solvent; (d) 3% to 80% by weight of an anionic surfactant; (e) 0 to 20% by weight of a nonionic, cationic and/or zwitterionic surfactant; (f) 0.02% to 10% by weight of silicone-based defoamer which is a linear polydimethylsiloxane having an average dynamic viscosity, measured at 25°C, in the range from 1000 to 8000 mPas, and containing silica; (g) 0 to 30% by weight of a customary formulation assistant; and (h) 0.1% to 90% by weight of water is suitable as a low-foam formulation for application in crop protection. Also provided is the use of the corresponding active-ingredient-free adjuvant formulations in a tank mix with or in split application with active-ingredient formulations.
A01N 25/30 - Biocides, pest repellants or attractants, or plant growth regulators, characterised by their forms, or by their non-active ingredients or by their methods of application; Substances for reducing the noxious effect of the active ingredients to organisms other than pests characterised by the surfactants
A01N 25/02 - Biocides, pest repellants or attractants, or plant growth regulators, characterised by their forms, or by their non-active ingredients or by their methods of application; Substances for reducing the noxious effect of the active ingredients to organisms other than pests containing liquids as carriers, diluents or solvents
A01N 25/20 - Combustible or heat-generating compositions
A01N 55/00 - Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing elements other than carbon, hydrogen, halogen, oxygen, nitrogen and sulfur
A01N 57/20 - Biocides, pest repellants or attractants, or plant growth regulators containing organic phosphorus compounds having phosphorus-to-carbon bonds containing acyclic or cycloaliphatic radicals
52.
CONCENTRATED AQUEOUS FORMULATIONS FOR CROP PROTECTION
Liquid aqueous formulations of water-soluble active crop protectant ingredients, comprising (a) one or more water-soluble active crop protectant ingredients (type (a) active ingredients), (b) if desired, one or more water-insoluble active crop protectant ingredients (type (b) active ingredients), (c) if desired, organic solvents, (d) nonionic, cationic, anionic and/or zwitterionic surfactants, (e) nonionic surfactants from the group of the alkylpolyglycosides, (f) inorganic salts from the group of ammonium salts, (g) if desired, other nonionic, anionic, cationic and/or zwitterionic surfactants, (h) if desired, other customary formulation assistants, and (i) water, are suitable as concentrated formulations for use in crop protection.
A01N 25/30 - Biocides, pest repellants or attractants, or plant growth regulators, characterised by their forms, or by their non-active ingredients or by their methods of application; Substances for reducing the noxious effect of the active ingredients to organisms other than pests characterised by the surfactants
A01N 25/02 - Biocides, pest repellants or attractants, or plant growth regulators, characterised by their forms, or by their non-active ingredients or by their methods of application; Substances for reducing the noxious effect of the active ingredients to organisms other than pests containing liquids as carriers, diluents or solvents
A01N 57/20 - Biocides, pest repellants or attractants, or plant growth regulators containing organic phosphorus compounds having phosphorus-to-carbon bonds containing acyclic or cycloaliphatic radicals
A01N 59/00 - Biocides, pest repellants or attractants, or plant growth regulators containing elements or inorganic compounds
The invention relates to a multi-phase contraceptive preparation that is based on a natural estrogen combined with a synthetic gestagen. Conventional anovulant preparations known in the prior art have proven to be reliable and safe in large-scale application. The aim of the invention is to provide a preparation that offers a higher contraceptive safety over the entire duration of the cycle, improves the cyclic bleeding behavior, and reduces or excludes side-effects, such as tender breasts, headaches, depressive moods, and libido disorders and the like.
A61K 31/57 - 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
A61K 31/56 - Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
A61K 31/565 - Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. oestrane, oestradiol
A61K 31/585 - Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin containing lactone rings, e.g. oxandrolone, bufalin
The present invention- relates to a process for preparing 5-chloro-N-{{(5S) 2- oxo-3-[4-(3-oxo-4- morpholinyl)phenyl]-1,3-oxazolidin-5 yl}methyl)-2-thiophenecarboxamide starting from 2-[(2S)- 2-oxiranylmethyl]-1H-isoindole-1,3(2H)-dione, 4-(4-aminophenyl)-3-morpholinone and 5- chlorothiophene-2-carbonyl chloride.
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
55.
METHOD FOR THE PRODUCTION OF A SOLID, ORALLY APPLICABLE PHARMACEUTICAL COMPOSITION
The present invention relates to a process for the preparation of a solid, orally administrable pharmaceutical composition, comprising 5-chloro-N-({(5S)-2-oxo-3-[4-(3-oxo-4-morpholinyl)-phenyl]-1,3-oxazolidin-5- yl}-methyl)-2-thiophenecarboxamide in hydrophilized form, and its use for the prophylaxis and/or treatment of diseases.
The invention relates to flavouring-containing pharmaceutical formulations with improved pharmaceutical properties, and to process for the production thereof.
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
57.
PROCESS FOR PREPARING 4-(4-AMINOPHENYL)-3-MORPHOLINONE
The present invention relates to a process for preparing 4-(4-aminophenyl)-3-morpholinone by reacting 4-(4-nitrophenyl)-3-morpholinone with hydrogen in the presence of a hydrogenation catalyst, characterized in that the reaction is effected in an aliphatic alcohol. In a specific embodiment, the 4-(4-aminophenyl)-3-morpholinone has the structure: (see formula I)
The present invention relates to the use of certain quinolone antibiotics for controlling bacterial disorders of the oral cavity, in particular in veterinary medicine.
A61K 31/4709 - Non-condensed quinolines containing further heterocyclic rings
A61K 31/4745 - Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenanthrolines
The present application relates to injection formulations of avermectins and milbemycins based on a solvent mixture comprising sesame oil, medium-chain triglycerides, glycol esters or fatty acid esters and a further solvent from the group consisting of mono- or polyhydric aliphatic or aromatic alcohols and their derivatives (e.g. cyclic carbonates; acetates; acetals; ketals) or castor oil.