Abstract

Disclosed herein are disintegrin variants, and methods for suppressing or inhibiting platelet aggregation in a subject in need thereof. The method includes administering to the subject in need thereof an effective amount of the present disintegrin variant to alleviate or ameliorate symptoms associated with diseases, disorders, and/or conditions resulted from platelet aggregation. According to preferred embodiments, the present disintegrain variant is applied as a coating on an implantable device, such as a stent or a catheter.

IPC Classes  ?

• C07K 14/46 - Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from humans from vertebrates
• C07K 7/04 - Linear peptides containing only normal peptide links
• C07K 14/745 - Blood coagulation or fibrinolysis factors
• C12N 9/64 - Proteinases derived from animal tissue, e.g. rennin

Abstract

The present invention is directed to compositions and methods for treating aromatic L-amino acid decarboxylase (AADC) deficiency. This invention includes a method of treating AADC deficiency in a pediatric subject, comprising the steps of: (a) providing a pharmaceutical formulation comprising an rAAV2-hAADC vector, (b) stereotactic ally delivering the pharmaceutical formulation to at least one target site in the brain of the subject in a dose of an amount at least about 1.8 x 1011 vg; wherein delivering the pharmaceutical formulation to the brain is optionally by frameless stereotaxy, and optionally wherein the dose is an amount of at least about 2.4 x 1011 vg and in some embodiments wherein the pharmaceutical formulation comprises a rAAV2-hAADC vector concentration of about 5.7 x 1011 vg/mL. This invention is also directed to methods for treating aromatic L-amino acid decarboxylase (AADC) deficiency, wherein the method optionally further comprises the step of administering a therapeutically effective dose of dopamine-antagonist to the subject such as risperidone. This invention is also directed to methods for treating aromatic L-amino acid decarboxylase (AADC) deficiency, wherein the method optionally comprises providing a pharmaceutical formulation comprising an rAAV2-hAADC vector, and empty capsids.

IPC Classes  ?

• A61K 48/00 - Medicinal preparations containing genetic material which is inserted into cells of the living body to treat genetic diseases; Gene therapy
• A61P 25/00 - Drugs for disorders of the nervous system
• C07K 14/47 - Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from humans from vertebrates from mammals
• C12N 15/86 - Viral vectors

Abstract

A vaccine composition and a method for inducing a systemic immune response and a mucosal immune response, where the vaccine composition comprises an antigen and hepatitis B virus-like particles as an adjuvant. The vaccine composition is applicable on a mucosal surface of a test subject receiving a medicament and is efficacious in initiating a protective immune response against an infection.

IPC Classes  ?

• A61K 39/39 - Medicinal preparations containing antigens or antibodies characterised by the immunostimulating additives, e.g. chemical adjuvants
• C07K 14/02 - Hepadnaviridae, e.g. hepatitis B virus

Abstract

Disclosed is an antigen comprising reconstituted respiratory syncytial virus (RSV) F protein, where the reconstituted RSV F protein comprises an antigenic region connected at either end to an HRN region and to an HRC region, and the antigenic region comprises one or more antigenic sites of groups consisting of site Ø, site II, and site IV. Also disclosed are a nucleic acid molecule for encoding the antigen and a vaccine composition comprising the antigen and used for initiating an immune response against RSV.

IPC Classes  ?

• A61K 39/155 - Paramyxoviridae, e.g. parainfluenza virus
• C07K 14/135 - Respiratory syncytial virus

Abstract

Provided is a method of treating or preventing adenovirus and enterovirus infection by administering an antiviral composition that contains an Echinacea purpurea extract, a Salvia miltiorrhiza extract, or combinations thereof. The antiviral composition blocks adenoviruses and enterovirus infection through virucidal activity against adenovirus and inhibition of adenovirus and enterovirus attachment to and penetration into cells. Also provided is a method of preparing the antiviral composition.

IPC Classes  ?

• A61K 36/537 - Salvia (sage)
• A61K 36/28 - Asteraceae or Compositae (Aster or Sunflower family), e.g. chamomile, feverfew, yarrow or echinacea
• A61P 31/12 - Antivirals

Abstract

The present invention provides novel substituted benzimidazole derivatives used as DAAO inhibitors and for treatment and/or prevention of neurological disorders.

IPC Classes  ?

• 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 31/4184 - 1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
• 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
• C07D 235/04 - Benzimidazoles; Hydrogenated benzimidazoles

Abstract

Herein is described a compound of formula (I), wherein A, Ra Rb, Rc, m, n, and X are ax described herein; or a pharmaceutically acceptable salt thereof.

IPC Classes  ?

• 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 31/4184 - 1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
• 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 31/444 - 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 31/675 - Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
• A61P 25/00 - Drugs for disorders of the nervous system
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
• C07D 235/28 - Sulfur atoms
• 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 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 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
• 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
• C07F 9/6506 - Five-membered rings having the nitrogen atoms in positions 1 and 3

Abstract

The present invention relates to hollow silica nanoparticles as a drug delivery system loading bioactive ingredients. Particularly, the present invention relates to silica nanoparticles comprising multi-layered silica shells with one or more bioactive ingredients encapsulated within and their applications in drug delivery; and processes of preparing the same.

IPC Classes  ?

• A61K 9/48 - Preparations in capsules, e.g. of gelatin, of chocolate
• A61K 9/14 - Particulate form, e.g. powders
• A61K 47/04 - Non-metals; Compounds thereof

Abstract

Silica-based biomolecule carriers, compositions comprising the same and preparation methods and uses thereof for delivering biomolecules into a cell are provided. The silica-based biomolecule carrier comprises a porous core; a first bioactive moiety; a second bioactive moiety functionally associated with the first bioactive moiety; and linkers for respectively conjugating the first bioactive moiety and the second bioactive moiety to the porous core.

IPC Classes  ?

• C08K 5/5415 - Silicon-containing compounds containing oxygen containing at least one Si—O bond
• A61K 39/385 - Haptens or antigens, bound to carriers
• G01N 33/552 - Glass or silica

Abstract

Provided herein are devices and systems that apply full-field optical coherence tomography (OCT) technology to three-dimensional skin tissue imaging. A special designed Mirau type objective and an optical microscope module allowing both OCT mode and orthogonal polarization spectral imaging (OPSI) mode are disclosed.

IPC Classes  ?

• G02B 21/06 - Means for illuminating specimen
• G01B 9/04 - Measuring microscopes
• G01J 3/447 - Polarisation spectrometry
• G02B 21/02 - Objectives
• G02B 21/26 - Stages; Adjusting means therefor
• G02B 21/34 - Microscope slides, e.g. mounting specimens on microscope slides
• G02B 21/36 - Microscopes arranged for photographic purposes or projection purposes

Abstract

An in vitro co-culture system comprising cancer-associated fibroblasts (CAFs) and cancer cells for producing and maintaining cancer stem cells and uses thereof for identifying agents capable of reducing cancer cell stemness. Also disclosed herein are a paracrine network through which CAFs facilitate production and/or maintenance of cancer stem cells and the use of components of such a paracrine network for prognosis purposes and for identifying cancer patients who are likely to respond to certain treatment.

IPC Classes  ?

• C12N 5/095 - Stem cells; Progenitor cells
• C12N 5/071 - Vertebrate cells or tissues, e.g. human cells or tissues
• C12N 5/09 - Tumour cells

Abstract

The invention utilizes virtual screening strategy to seek for current market drugs as anti-schizophrenia therapydrug repurposing. Drug repurposing strategy finds new uses other than the original medical indications of existing drugs. Finding new indications for such drugs will benefit patients who are in needs for a potential new therapy sooner since known drugs are usually with acceptable safety and pharmacokinetic profiles. In this study, repurposing marketed drugs for DAAO inhibitor as new schizophrenia therapy was performed with virtual screening on marketed drugs and its metabolites. The identified and available drugs and compounds were further confirmed with in vitro DAAO enzymatic inhibitory assay.

IPC Classes  ?

• C12Q 1/26 - Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving oxidoreductase
• G16B 35/20 - Screening of libraries
• G16C 20/64 - Screening of libraries
• 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
• A61P 25/00 - Drugs for disorders of the nervous system
• C12N 9/02 - Oxidoreductases (1.), e.g. luciferase
• C40B 30/08 - Methods of screening libraries by measuring catalytic activity

Abstract

Methods for synthesis and preparation of alpha-glycosphingolipids are provided. Methods for synthesis of a-galactosyl ceramides, and pharmaceutically active analogs and variants thereof are provided. Novel alpha-glycosphingolipids are provided, wherein the compounds are immunogenic compounds which serve as ligands for NKT (natural killer T) cells. A process for preparing a chiral compound comprising an R-form or S- form of a glycosphingolipid of formula (1 ) is provided, wherein R1=OH, NH2, NHCOR2, R2 = H or an alkyl, alkenyl, or alkyl terminating in aryl, substituted aryl, heteroaryl, or substituted heteroaryl, X=alkyl group, R3= OH or H, R4=OH or H, R5= aryl, substituted aryl, heteroaryl, or substituted heteroaryl, or a pharmaceutically acceptable salt thereof, wherein the compound of formula 1 is prepared by (a) deprotecting a compound of formula (2): wherein PG is a hydroxyl protecting group, with hydrogen under hydrogenation catalysis.

IPC Classes  ?

• C07H 15/06 - Acyclic radicals, not substituted by cyclic structures attached to an oxygen atom of a saccharide radical being a hydroxyalkyl group esterified by a fatty acid
• A61K 39/39 - Medicinal preparations containing antigens or antibodies characterised by the immunostimulating additives, e.g. chemical adjuvants
• A61P 31/04 - Antibacterial agents
• A61P 31/12 - Antivirals
• A61P 35/00 - Antineoplastic agents
• C07H 15/04 - Acyclic radicals, not substituted by cyclic structures attached to an oxygen atom of a saccharide radical
• C07H 15/18 - Acyclic radicals, substituted by carbocyclic rings

Abstract

The present invention provides substituted phenyl- and heteroaryl- phenyl ether agonists of Src homology-2 containing protein tyrosine phosophase-1 (SHP-1). Also provided are uses of the agonists for the treatment of a disease of condition characterized by decrease SHP-1 expression in a subject. The agonists are represented by Formula I (see formula I)

IPC Classes  ?

• C07D 471/04 - Ortho-condensed systems
• A61K 31/17 - Amides, e.g. hydroxamic acids having the group N—C(O)—N or N—C(S)—N, e.g. urea, thiourea, carmustine
• A61K 31/18 - Sulfonamides
• 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
• A61K 31/44 - Non-condensed pyridines; Hydrogenated derivatives thereof
• A61P 19/10 - Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
• A61P 35/00 - Antineoplastic agents
• C07C 255/54 - Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing cyano groups and etherified hydroxy groups bound to the carbon skeleton
• C07C 275/36 - Derivatives of urea, i.e. compounds containing any of the groups the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton being further substituted by singly-bound oxygen atoms having nitrogen atoms of urea groups and singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring with at least one of the oxygen atoms further bound to a carbon atom of a six-membered aromatic ring, e.g. N-aryloxyphenylureas
• 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
• C07D 213/81 - Amides; Imides
• C07D 215/233 - Oxygen atoms attached in position 2 or 4 only one oxygen atom which is attached in position 4
• C07D 215/40 - Nitrogen atoms attached in position 8

Abstract

Indolyl or indolinyl hydroxamates and pharmaceutical compositions comprising the same, which show histone deacetylase (HDAC) inhibition activity. Method for treating cancer with compounds of Formula (I). (see formula I)

IPC Classes  ?

• C07D 209/20 - Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals substituted additionally by nitrogen atoms, e.g. tryptophane
• A61K 31/404 - Indoles, e.g. pindolol
• A61P 35/00 - Antineoplastic agents
• C07D 209/12 - Radicals substituted by oxygen atoms
• C07D 209/18 - Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
• C07D 209/22 - Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with an aralkyl radical attached to the ring nitrogen atom