The invention relates to imidazo[1,5-a]quinoxaline derivatives which are inhibitors of phosphodiesterase 10 (PDE10) useful in treating central nervous system diseases such as psychosis and also in treating, for example, obesity, type 2 diabetes, metabolic syndrome, glucose intolerance, and pain.
The invention relates to triazine derivatives of formula (I): which are inhibitors of phosphodiesterase 2 or 10, useful in treating central nervous system diseases such as psychosis and also in treating, for example, obesity, type 2 diabetes, metabolic syndrome, glucose intolerance, and pain.
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 31/53 - 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
The invention relates to imidazo[5,1-c][1,2,4]benzotriazine derivatives of formula (I): which are inhibitors of phosphodiesterase 2 or 10 useful in treating central nervous system diseases such as psychosis and also in treating, for example, obesity, type 2 diabetes, metabolic syndrome, glucose intolerance, and pain.
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
A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
A method of delivering a hair care active to the hair including the use of a hair care active and a portable moist heat delivery system comprising: a water vapor generating portion comprising a water vapor source and a heat source; and a water vapor-air regulating portion located at a hair-facing side of the water vapor generating portion, the water vapor-air regulating portion comprising a water vapor-air mixing layer, a water vapor-air distribution layer, a latent heat delivery surface, and optionally a hair contact layer, where the water vapor generating portion and the water vapor-air regulating portion are in fluid communication is disclosed.
A61K 8/96 - Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof, of undetermined constitution
Compounds of formula (I) wherein R1, R2, R3, R4, R5, and R6 are as defined herein, including all crystalline forms and pharmaceutically acceptable salts thereof, which are useful in pharmaceutical formulations for the treatment or prevention of hepatitis C virus infections and diseases associated with such infections.
A61K 31/343 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide condensed with a carbocyclic ring, e.g. coumaran, bufuralol, befunolol, clobenfurol, amiodarone
C07D 307/80 - Radicals substituted by oxygen atoms
A61P 31/00 - Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
7.
6-SUBSTITUTED BENZOFURAN COMPOUNDS TO TREAT INFECTION WITH HEPATITIS C VIRUS
Compounds of following formula (I); wherein R1, R2, R3, R4, R5, and R6 are as defined herein, including all crystalline forms and pharmaceutically acceptable salts thereof, which are useful in pharmaceutical formulations for the treatment or prevention of hepatitis C virus infections and diseases associated with such infections.
C07D 307/84 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
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
A61K 31/343 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide condensed with a carbocyclic ring, e.g. coumaran, bufuralol, befunolol, clobenfurol, amiodarone
The present invention discloses fused heterobicyclic 2-aryl- and 2-heteroarylthiazolyl compounds and their pharmaceutically acceptable salts and esters thereof, which are useful for inhibiting the growth of cancerous cells, inhibiting human breast carcinoma tumor growth in particular and to treat diseases or disorders associated with securin (Formula I) and pharmaceutically acceptable salts thereof, wherein A is H, C1-C3 alkyi, or acetyl; Z is NR3 or O; Q is -NR1R2, - NR3N(R3)2. - NR3OR3, or -OH.
The present invention discloses fused bicyclic 2-aryl- or 2-heteroarylthiazolyl compounds and their pharmaceutically acceptable salts and esters thereof, which are useful for inhibiting the growth of cancerous cells, inhibiting human breast carcinoma tumor growth in particular and to treat diseases or disorders associated with securin, including elevated securin levels.
C07D 277/60 - Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings condensed with carbocyclic rings or ring systems
C07D 417/04 - 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 directly linked by a ring-member-to-ring- member bond
C07D 417/10 - 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 aromatic rings
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
A61K 31/428 - Thiazoles condensed with carbocyclic rings
Specific binding fragments, antibodies, and antigen-binding fragments thereof that bind IL-10-like cytokines, including human interleukin-22 (IL-22) are provided. Methods of making and using such binding fragments, antibodies, and antigen-binding fragments are also provided. Kits containing such binding fragments, antibodies, and antigen-binding fragments are also provided.
C07K 16/24 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against cytokines, lymphokines or interferons
A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
Methods of screening for agents for treating inflammatory diseases are provided. The methods involve screening for agents that modulate the activity or expression of GPR64, which has been discovered herein to play a role in inflammatory diseases. Methods for treating an inflammatory disease, as well as methods of modulating the activity or expression of GPR64, methods of screening for an inflammatory disease in a subject, pharmaceutical compositions, a nucleic acid variant, and antibodies are also provided.
A61K 31/20 - Carboxylic acids, e.g. valproic acid having a carboxyl group bound to an acyclic chain of seven or more carbon atoms, e.g. stearic, palmitic or arachidic acid
A61K 31/202 - Carboxylic acids, e.g. valproic acid having a carboxyl group bound to an acyclic chain of seven or more carbon atoms, e.g. stearic, palmitic or arachidic acid having three or more double bonds, e.g. linolenic acid
A61K 31/192 - Carboxylic acids, e.g. valproic acid having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid
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
A61P 19/02 - Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
G01N 33/00 - Investigating or analysing materials by specific methods not covered by groups
13.
INTERLEUKIN-21 (IL-21) AND IL-21 RECEPTOR (IL-21R) MODULATION OF REGULATORY T CELLS AND FORKHEAD BOX P3 (FOXP3)
CATHOLIC HEALTHCARE WEST D/B/A ST. JOSEPH'S HOSPITAL & MEDICAL CENTER& BARROW NEUROLOGICAL INSTITUTE (USA)
Inventor
Shi, Fu-Dong
Young, Deborah, A.
Collins, Mary
Vollmer, Timothy
Liu, Ruolan
Piao, Wenhua
Abstract
Methods of modulating the level and activity of Tregs and Foxp3 using modulators of IL-21/IL-21 R, i.e., IL-21/IL-21 R agonists (i.e., IL-21 agonists and IL-21R agonists) and IL-21/IL-2 I R antagonists (i.e., IL-21 antagonists and IL-21 R antagonists), are disclosed. IL-21 /IL-21 R agonists and antagonists can be used to enhance immunity or induce immune suppression in vivo, ex vivo and/or in vitro, e.g., for treating, ameliorating or preventing autoimmune or inflammatory disorders, cancers, and infectious disorders.
C07K 14/715 - ReceptorsCell surface antigensCell surface determinants for cytokinesReceptorsCell surface antigensCell surface determinants for lymphokinesReceptorsCell surface antigensCell surface determinants for interferons
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 38/17 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans
14.
COMPOSITIONS CONTAINING O-SULFATE AND O-PHOSPHATE CONTAINING ARYL SULFONAMIDE DERIVATIVES USEFUL AS BETA-AMYLOID INHIBITORS
A synthetic compound characterized by having the structure of formula I or II or a pharmaceutically acceptable salt and/or hydrate thereof is provided. Formula I and formula II are defined as follows. wherein R1 is substituted aryl or substituted heteroaryl; R2 and R3 are independently selected from the group consisting of CF3, substituted phenyl, C1-C4 alkyl, substituted C1-C4 alkyl, (CF3)nC1-C4 alkyl, (CF3)n(substituted C1-C4 alkyl), provided that when R2 or R3 is CF3, the other is not an unsubstituted alkyl; R4 and R4,are independently selected from the group consisting of M, C1-C4 alkyl, phenyl, and benzyl, wherein M is a metal ion is selected from the group consisting of sodium, lithium, calcium, magnesium and potassium, or R4 and R4, are taken together to form a cyclic structure. Methods of making such compounds and uses thereof are also provided.
A61K 31/661 - Phosphorus acids or esters thereof not having P—C bonds, e.g. fosfosal, dichlorvos, malathion
C07C 305/04 - Esters of sulfuric acids having oxygen atoms of sulfate groups bound to acyclic carbon atoms of a carbon skeleton being acyclic and saturated
High resolution structures of acidic mammalian chitinase (AMCase) are disclosed. The structures disclosed herein enable selection of, and structure-based rational drug design of, agents that modulate, e.g., antagonize, AMCase activity. Thus, crystal compositions, methods of selecting and/or designing agents, e.g., antagonists, of AMCase, and computer and software programs are disclosed.
G01N 33/573 - ImmunoassayBiospecific binding assayMaterials therefor for enzymes or isoenzymes
C12N 15/56 - Hydrolases (3) acting on glycosyl compounds (3.2), e.g. amylase, galactosidase, lysozyme
G06F 19/00 - Digital computing or data processing equipment or methods, specially adapted for specific applications (specially adapted for specific functions G06F 17/00;data processing systems or methods specially adapted for administrative, commercial, financial, managerial, supervisory or forecasting purposes G06Q;healthcare informatics G16H)
16.
PYRIDO[3,2-E]PYRAZINES, PROCESS FOR PREPARING THE SAME, AND THEIR USE AS INHIBITORS OF PHOSPHODIESTERASE 10
The invention relates to pyrido[3,2-e]pyrazines, to processes for preparing them, to pharmaceutical compositions which comprise these compounds and to the pharmaceutical use of these compounds, which are inhibitors of phosphodiesterase 10, as active compounds for treating central nervous system disorders, obesity, and metabolic disorders.
The invention relates to imidazo[1,5-a]pyrazine derivatives, to processes for preparing them, to pharmaceutical preparations which comprise these compounds and to the pharmaceutical use of these compounds, which are inhibitors of phosphodiesterase 10 (PDE10), as active compounds for treating central nervous system diseases of mammals, including humans.
Assays, e.g., homogenous assays, and methods for identifying, quantifying and/or monitoring the formation and/or stability of a multimeric complex, e.g., a ternary complex are disclosed. The methods and assays of the invention can be used to identify and/or evaluate agents (e.g., proteins, peptides, antibody molecules, and small and large molecules) that interfere with and/or inhibit the formation of a multimeric complex (e.g., a ternary complex) or that disrupt a previously formed complex.
The present invention relates to processes for the preparation of of heteroaryl ethers. In some embodiments, the processes relate to cross coupling reactions between triazol-1-yloxy and triazol-1-yl heterocycles with aryl boronic acids. In a further aspect, this invention also relates to compounds that are useful for the treatment of oncological diseases or disorders, and for the treatment of inflammation.
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 407/12 - 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 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
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 495/12 - Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
A61K 31/505 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
A61K 31/513 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
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
C07K 16/32 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against translation products from oncogenes
Provided are metaflumizone compositions and methods for treating protozoal infections in animals, particularly domesticated animals such as dogs and cats; birds such as chickens and turkeys; and other food animals such as cattle, sheep, pigs, and rabbits. Compositions and methods disclosed herein are effective in protecting against, mitigating, preventing, and/or ameliorating coccidia infections in animals.
A61K 31/175 - Amides, e.g. hydroxamic acids having the group N—C(O)—N or N—C(S)—N, e.g. urea, thiourea, carmustine having the group , N—C(O)—N=N— or , e.g. carbonohydrazides, carbazones, semicarbazides, semicarbazonesThioanalogues thereof
IDENTIFICATION AND CHARACTERIZATION OF HCV REPLICON VARIANTS WITH REDUCED SUSCEPTIBILITY TO A COMBINATION OF POLYMERASE AND PROTEASE INHIBITORS, AND METHODS RELATED THERETO
The present invention provides methods of decreasing the frequency of emergence, decreasing the level of resistance, and delaying the emergence of a treatment-resistant hepatitis C viral infection, by administering to a subject, either in combination or in series, an inhibitor of the hepatitis C RNA-dependent RNA polymerase NS5B, e.g., a benzofuran, such as 5-cyclopropyl-2-(4-fluorophenyl)- 6-[(2-hydroxyethyl)(methylsulfonyl)amino]-N-methyl-l-benzofuran- 3-carboxamide (HCV-796), and an inhibitor of the serine protease NS3, e.g., boceprevir. Additionally, the invention relates to methods of monitoring the course of treatment of a hepatitis C viral infection, methods of monitoring and prognosing a hepatitis C viral infection, and methods of identifying an individual with a decreased likelihood of responding to an anti-hepatitis C viral therapy. These methods use the sequence(s) of HCV nonstructural gene(s) to identify the emergence of a treatment-resistant hepatitis C viral infection, particularly a benzofuran (e.g., HCV-796) and NS3 inhibitor (e.g., boceprevir) treatment- resistant hepatitis C viral infection.
A61K 31/343 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide condensed with a carbocyclic ring, e.g. coumaran, bufuralol, befunolol, clobenfurol, amiodarone
C07D 239/74 - QuinazolinesHydrogenated quinazolines with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, attached to ring carbon atoms of the hetero ring
The invention provides preferred dosage ranges, maximum concentrations, average concentrations and monitoring regimes for use in treatment of Alzheimer's disease using antibodies to A-beta. The invention also provides monitoring regimes that can assess changes in symptoms or signs of the patient following treatment.
One aspect of the invention relates to a method of identifying cell adjacency in a coculture of cells. The method includes generating a first set of image data of the coculture of cells, the first set of image data comprising nuclear position data for each imaged cell; generating a second set of image data of at least a subset of the coculture of cells, the second set of image data comprising cell identifier data associated with a first cell type; generating a third set of image data of at least a subset of the coculture of cells, the third set of image data comprising cell identifier data associated with a second cell type; and identifying a group of cells in response to the nuclear position data, wherein each cell having the first cell type in the group is adjacent another cell in the group having the second cell type.
Novel sulfonamide compounds useful in the treatment of conditions related to the production of beta-amyloid are described, as are routes to their preparation. The sulfonamide compounds are of the following structure, wherein R4-R3 are defined herein. Also provided are pharmaceutical compositions containing these compounds and/or prodrugs of these compounds and a physiologically compatible carrier. These compounds are specifically useful for inhibiting beta amyloid production, and treating Alzheimer's Disease, amyloid angiopathy, cerebral amyloid angiopathy, systemic amyloidosis, hereditary cerebral hemorrhage with amyloidosis of the Dutch type, inclusion body myositis, mild cognitive impairment (MCI) and Down's syndrome.
C07C 311/17 - 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 hydrogen atoms or to an acyclic carbon atom to an acyclic carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms
A61K 31/381 - Heterocyclic compounds having sulfur as a ring hetero atom having five-membered 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
27.
PROCESS FOR THE PREPARATION OF TRIFLUOROALKYL-PHENYL AND HETEROCYCLIC SULFONAMIDES
A novel trifluoroacetylating agent, i.e., N-trifluoroacetylmorpholine, is described. This reagent is useful in the preparation of phenyl and heterocyclic sulfonamide compounds. Methods are therefore described for preparing sulfonamide compounds of the following structure, wherein R1 and R2 are defined herein, using N- trifluoroacetylmorpholine. The sulfonamide compounds that may be prepared as described herein include 5-chloro-thiophene-2-sulfonic acid [(1S,2R)-2-(3,5-difluoro- phenyl)-3,3,3-trifluoro-1-hydroxymethyl-propyl]-amide using N- trifluoroacetylmorpholine. Formula (I).
C07D 295/108 - 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 doubly bound oxygen or sulfur atoms with the ring nitrogen atoms and the doubly bound oxygen or sulfur atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings to an acyclic saturated chain
28.
PROCESSES AND INTERMEDIATES FOR THE PREPARATION OF HETEROCYCLIC SULFONAMIDE COMPOUNDS
Methods for preparing compound of Formula (I) are described, wherein R1-R3 are defined herein, as are methods for preparing the intermediates formed therein. Formula (I) Also described are methods for enantioselectively preparing a chiral compound of the following structure, wherein R2 and R3 are defined herein. Formula (II).
C07C 57/58 - Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms containing halogen containing six-membered aromatic rings
C07C 215/28 - Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being unsaturated and containing six-membered aromatic rings
C07C 311/00 - Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
C07D 263/22 - Oxygen atoms attached in position 2 with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to other ring carbon atoms
C07D 409/00 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
29.
PHARMACEUTICAL COMPOSITIONS AND METHODS OF PREVENTING, TREATING, OR INHIBITING INFLAMMATORY DISEASES, DISORDERS, OR CONDITIONS OF THE SKIN, AND DISEASES, DISORDERS, OR CONDITIONS ASSOCIATED WITH COLLAGEN DEPLETION
The present invention provides compositions and methods for preventing, treating, or inhibiting inflammatory diseases, disorders, or conditions of the skin, and diseases, disorders, or conditions associated with collagen depletion using one or more estrogenic agents.
A61K 31/055 - Phenols the aromatic ring being substituted by halogen
A61K 31/06 - Phenols the aromatic ring being substituted by nitro groups
A61K 31/122 - Ketones having the oxygen atom directly attached to a ring, e.g. quinones, vitamin K1, anthralin
A61K 31/277 - NitrilesIsonitriles having a ring, e.g. verapamil
A61K 31/343 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide condensed with a carbocyclic ring, e.g. coumaran, bufuralol, befunolol, clobenfurol, amiodarone
A61K 31/35 - 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
A61K 31/352 - 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 condensed with carbocyclic rings, e.g. cannabinols, methantheline
A61K 31/381 - Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
A61K 31/395 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
A61K 31/423 - Oxazoles condensed with carbocyclic rings
A61K 31/4741 - QuinolinesIsoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having oxygen as a ring hetero atom, e.g. tubocuraran derivatives, noscapine, bicuculline
A61K 31/7042 - Compounds having saccharide radicals and heterocyclic rings
The invention relates to processes for the preparation of the bicyclic oxazine carboxaldehyde Compound 1: (I) The invention also relates to the use of Compound 1 in the preparation of β-lactamase inhibitors.
C07C 43/10 - Saturated ethers of polyhydroxy compounds
C07C 45/71 - Preparation of compounds having C=O groups bound only to carbon or hydrogen atomsPreparation of chelates of such compounds by reactions not involving the formation of C=O groups by isomerisationPreparation of compounds having C=O groups bound only to carbon or hydrogen atomsPreparation of chelates of such compounds by reactions not involving the formation of C=O groups by change of size of the carbon skeleton by increase in the number of carbon atoms by reaction with functional groups containing oxygen only in singly bound form being hydroxy groups
C07C 47/273 - Unsaturated compounds having —CHO groups bound to acyclic carbon atoms containing hydroxy groups containing halogen
C07C 47/277 - Unsaturated compounds having —CHO groups bound to acyclic carbon atoms containing ether groups, groups, groups, or groups
C07C 257/14 - Compounds containing carboxyl groups, the doubly-bound oxygen atom of a carboxyl group being replaced by a doubly-bound nitrogen atom, this nitrogen atom not being further bound to an oxygen atom, e.g. imino-ethers, amidines with replacement of the other oxygen atom of the carboxyl group by nitrogen atoms, e.g. amidines having carbon atoms of amidino groups bound to acyclic carbon atoms
C07D 265/30 - 1,4-OxazinesHydrogenated 1,4-oxazines not condensed with other rings
31.
N'-(2-HALOBENZYLIDENE)SULFONYLHYDRAZIDES AS INTERMEDIATES IN THE MANUFACTURE OF ARYLSULFONYLINDAZOLES
The present invention provides N'-(2-halobenzylidene)sulfonylhydrazides of formula (I). Compounds of formula (I) are useful for the manufacture of 1-arylsulfonylindazole 5-HT6 ligands.
C07C 303/40 - Preparation of esters or amides of sulfuric acidsPreparation of sulfonic acids or of their esters, halides, anhydrides or amides of amides of sulfonic acids by reactions not involving the formation of sulfonamide groups
C07C 311/49 - Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups having nitrogen atoms of sulfonamide groups further bound to another hetero atom to nitrogen atoms
C07D 295/12 - 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
C07D 295/20 - 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 acylated on ring nitrogen atoms by radicals derived from carbonic acid, or sulfur or nitrogen analogues thereof
32.
METHODS OF PROTECTING ANIMALS FROM AVIAN INFLUENZA INFECTION
The present invention provides methods of vaccinating non-avian, non-human animals against avian influenza. The methods of the invention comprise administering to the animal at least one dose of a vaccine composition comprising an immunologically-effective amount of an inactivated influenza virus. The influenza virus may contain any combination of hemagglutinin and neuraminidase subtypes. An exemplary inactivated influenza virus for use in a vaccine composition of the invention is a reverse genetics H5N3 virus. The animals to which the vaccine composition is administered may be any non-avian, non-human animal such as a dog, a cat or a pig.
The present invention provides a process for the manufacture of an arylmethyl-sulfonylarene, R1CH2SO2R2, wherein R1 and R2 are each independently an optionally substituted phenyl or naphthyl group which process comprises reacting an arylmethylhalide, R1CH2-Hal wherein R1 is as defined hereinabove and Hal is Cl, Br or I with a sodium arylsulfinate R2SO2Na wherein R2 is as defined hereinabove in the presence of a base optionally in the presence of a solvent. Also provided is the use of the inventive process in the manufacture of a 3-arylsulfonylindazole 5-HT6 ligand.
The present invention is directed to methods / systems for measuring the pH of a cell culture medium in a small-scale system utilizing a pH-sensitive dye. The present invention is also directed to methods for predicting the performance of cells in a large-scale culture system.
The present invention provides materials and methods for treatment of diseases involving aberrant B-cell activity, using a CD20-specific binding molecule, in particular, antibodies or antigen binding fragment thereof. The compositions disclosed herein is useful for the treatment and diagnosis of B-cell disorders, such as B-cell malignancies and autoimmune diseases.
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 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
The present invention provides, among other things, systems and methods for identifying genes and proteins that regulate and/or are indicative of cell phenotypes based on expression profiling analysis. The present invention further provides methods of manipulating identified genes and proteins to engineer improved cell lines.
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
C07K 16/32 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against translation products from oncogenes
A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
The invention provides compounds of the Formula: (I) that are useful for the treatment of depression (including but not limited to major depressive disorder, childhood depression and dysthymia), anxiety, panic disorder, post-traumatic stress disorder, premenstrual dysphoric disorder (also known as pre- menstrual syndrome), attention deficit disorder (with and without hyperactivity), obsessive compulsive disorder, social anxiety disorder, generalized anxiety disorder, obesity, eating disorders such as anorexia nervosa, bulimia nervosa, vasomotor flushing, cocaine and alcohol addiction, sexual dysfunction and related illnesses. The compounds are able to block the recptake of serotonin and are modulators at brain 5HT1A serotonin receptors.
Methods and compositions for modulating cardiac, renal and vascular cell function and homeostasis using agonists and antagonists of BMP-IO are disclosed. In particular, methods for treating, preventing and/or diagnosing BMP-10-associated vascular, renal, fibrotic and cardiac conditions and/or disorders are disclosed. Screening methods for evaluating BMP-IO modulators, e.g., agonists and antagonists, are also disclosed.
The present invention provides a method of detecting the presence of the calicheamicin component of a calicheamicin-carrier conjugate in a fluid sample, wherein the calicheamicin is covalently bound to the carrier. A bond between the calicheamicin and carrier is disrupted, the calicheamicin portion is released from the calicheamicin-carrier conjugate and detected.
G01N 33/94 - Chemical analysis of biological material, e.g. blood, urineTesting involving biospecific ligand binding methodsImmunological testing involving narcotics
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
A method is disclosed for preparing hydrazides from hydrazine and an acyl chloride which comprises the steps of (a) preparing a stirred substantially uniform slurry comprising hydrazine and an inert solvent at low temperature; and (b) adding an acyl chloride continuously to said slurry. The method avoids or limits production of undesired bis-hydrazide by-products. The method is used to prepare 3-methyl-3-mercaptobutanoic acid hydrazide, a molecule used to link calicheamicin to a monoclonal antibody.
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
C07C 243/28 - Hydrazines having nitrogen atoms of hydrazine groups acylated by carboxylic acids with acylating carboxyl groups bound to hydrogen atoms or to acyclic carbon atoms to hydrogen atoms or to carbon atoms of a saturated carbon skeleton
C07C 323/48 - Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton having at least one of the nitrogen atoms, not being part of nitro or nitroso groups, further bound to other hetero atoms to nitrogen atoms
Novel primate chitinases (pNC) and nucleic acids encoding these chitinases are disclosed. The pNCs of the invention are homologous to human acidic mammalian chitinases (hAMCase) and human chitotriosidase, in terms of their exon/intron genomic structure and conserved catalytic sites. The polypeptides and nucleic acids of the invention can be used to develop, and/or screen for, modulators of chitinase-activities, e.g., antisense, antibodies, RNAi. The modulators identified using methods and reagents disclosed herein can be used to reduce chitinase-associated inflammatory conditions.
An immunogenic composition having 13 distinct polysaccharide-protein conjugates and optionally, an aluminum-based adjuvant, is described. Each conjugate contains a capsular polysaccharide prepared from a different serotype of Streptococcus pneumoniae (1, 3, 4, 5, 6A, 6B, 7F, 9V, 14, 18C, 19A, 19F and 23F) conjugated to a carrier protein. The immunogenic composition, formulated as a vaccine, increases coverage against pneumococcal disease in infants and young children globally, and provides coverage for serotypes 6A and 19A that is not dependent on the limitations of serogroup cross-protection. Also described is a method for making an immunogenic conjugate comprising Streptococcus pneumoniae serotype 3 polysaccharide covalently linked to a carrier protein, the method including periodic acid oxidation of the polysaccharide in the presence of bivalent cations.
C07K 14/34 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from bacteria from Corynebacterium (G)
C07K 14/315 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from bacteria from Streptococcus (G), e.g. Enterococci
44.
5- (AMINOAZACYCLYL) -3-SULFONYL-LH- INDAZOLES AS 5-HYDROXYTRYPTAMINE- 6 LIGANDS FOR THE TREATMENT OF CNS DISORDERS
The present invention provides a compound of formula I and the use thereof in the therapeutic treatment of central nervous system disorders related to or affected by the 5-HT6 receptor.
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 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
A61K 31/416 - 1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
A61P 25/00 - Drugs for disorders of the nervous system
45.
ELIMINATION OF INTERFERENCE IN IMMUNOASSAYS CAUSED BY ANTI-CARBOHYDRATE ANTIBODIES
The present invention is directed to assays for the detection of an anti-drug antibody in general and in particular to the detection of an anti-drug antibody wherein the drug has a carbohydrate moiety. The invention is also directed to assays for the detection of a drug in general and in particular to the detection of a drug wherein the drug has a carbohydrate moiety. The invention is further directed to methods for identifying appropriate subjects for treatment with a drug containing a carbohydrate moiety.
The present teachings relate to compounds of formula I: and pharmaceutically acceptable salts and esters thereof, wherein R1, R2, R3, R4, X, and Y are as defined herein. The present teachings also provide methods of making the compounds of formula I and methods of inhibiting matrix metalloproteinases, in particular, MMP-12, that may be involved in pathological disorders found in mammals, including a human.
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 405/06 - 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 carbon chain containing only aliphatic carbon atoms
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
C07D 409/04 - 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 directly linked by a ring-member-to-ring- member bond
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 413/04 - 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 directly linked by a ring-member-to-ring- member bond
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 417/04 - 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 directly linked by a ring-member-to-ring- member bond
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 31/343 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide condensed with a carbocyclic ring, e.g. coumaran, bufuralol, befunolol, clobenfurol, amiodarone
A61K 31/381 - Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
Compounds and compositions containing poly-γ-D,L-glutamic acid (PGA) moieties and their use in preventing or treating nosocomial infections caused by Staphylococcus and Bacillus are disclosed.
The invention provides a nutritional supplement and/or pharmaceutical composition for tableting comprising an embedded lubrication matrix. The embedded lubrication matrix comprises an oily liquid finely dispersed in an oil insoluble material. A method of lubricating a nutritional supplement or pharmaceutical composition for tableting using a matrix with embedded lubrication is also provided.
The present invention provides a novel method of reducing protein misfolding and aggregation in the cell culture by growing the cell culture at a reduced temperature and/or reduced pH. As a result, the quality of the protein produced in the cell culture is greatly improved. Thus, the present invention facilitates improvements in the efficacy of therapeutic proteins produced in cell culture.
Methods and compositions for reducing or inhibiting, or preventing or delaying the onset of, one or more symptoms associated with an early and/or a late phase of an IL- 13-associated disorder or condition using IL- 13 binding agents are disclosed. Methods for evaluating the kinetics and/or efficacy of an IL- 13 binding agent in treating or preventing an IL- 13 -associated disorder or condition in a subject, e.g., a human subject, are also disclosed.
C07K 16/24 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against cytokines, lymphokines or interferons
A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
The invention provides improved agents and methods for treatment of cerebral amyloid angiopathy (CAA) and methods to effect prophylaxis of CAA. The methods can treat CAA concurrently with Alzheimer's disease or separately. The methods can effect prophylaxis of CAA concurrently with Alzheimer's disease or separately. The methods involve administering antibody that is specific for the N-terminus of Aß or an agent that can induce such an antibody.
Methods of producing a protein in cell culture comprising an anti-senescence compound, such as the antioxidant carnosine, are provided. According to teachings of the present invention, cells grown in a cell culture medium comprising an anti-senescence compound exhibit increased viability and productivity. Furthermore, cell cultures grown in the presence of an anti-senescence compound exhibit decreased levels of high molecular weight aggregates in the cell culture medium.
A flow assessment apparatus (10) is provided for quantitatively assessing the flow properties of particulate material, such as pharmaceutical formulations and constituent powders. The apparatus (10) includes a vibratory feed device (12) having an inclined dispensing member (16). Particulate material is induced to flow along the inclined member (16) onto a watch glass (18) positioned on a top pan balance (20). The mass of material dispensed onto the watch glass (18) is recorded over a given time period, for example a set time period of 1 minute, or a visually assessed time period where it is deemed that sufficient material has been dispensed. The mass and time data is used to calculate a value representative of a relative flow property of the material, which can be used in the development of pharmaceutical formulations.
G01G 13/08 - Means for automatically loading weigh-pans or other receptacles, e.g. disposable containers, under control of the weighing mechanism involving dribble-feed means controlled by the weighing mechanism to top up the receptacle to the target weight wherein the main feed is effected by mechanical conveying means, e.g. by belt conveyors or by vibratory conveyors
54.
ANTI-TUMOR ACTIVITY OF TEMSIROLIMUS IN PAPILLARY RENAL CELL CANCER
A61K 31/436 - 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 six-membered ring having oxygen as a ring hetero atom, e.g. rapamycin
An anti-neoplastic wortmannin conjugate is described formed by a linking a rapalog and wortmannin. Such a linkage is removable following administration to a subject. Use of such a conjugate in an antineoplastic regimen is described.
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 31/395 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
A rapamycin - wortmannin conjugate is described, in which the conjugate is formed by linking the rapamycin and wortmannin together in such a manner that the rapamycin and the wortmannin are separated following administration to a subject. Use of such a conjugate in an antineoplastic regimen is described.
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 31/395 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
The present invention provides a compound of formula I wherein X-, R1, and R2 are as defined herein, and compositions thereof, useful as a peripheral mu opioid receptor antagonist.
The invention provides a novel mouse IL-17F/IL-17A, and further provides uses of such mouse IL-17F/IL-17A in the characterization of the IL-17F/IL-17A heterodimer. The present invention is also related to polynucleotides and polypeptides of the IL-17F/IL-17A signaling pathway, and targeting of the IL-17F/IL-17A signaling pathway in methods of treating IL-17F/IL-17A- associated disorders. The invention thus provides methods of using isolated IL-17F/IL-17A heterodimer, e.g., in a mouse model of airway inflammation, and specific or selective IL-17F/IL-17A modulators (e.g., signaling agonists or signaling antagonists (e.g., specific or selective antagonistic antibodies, specific or selective antagonistic small molecules, etc.)). The invention also provides methods of screening for compounds capable of modulating IL-17F/IL-17A biological activity, e.g., IL-17F/IL-17A signaling antagonists (e.g., using the mouse model of airway inflammation), as well as methods of identifying whether the IL-17F/IL-17A modulator is a specific IL-17F/IL-17A modulator. The invention is also directed to novel methods for diagnosing, prognosing, monitoring, preventing, and/or treating IL-17F/IL-17A-associated disorders, including, but not limited to, inflammatory disorders (e.g., arthritis (including rheumatoid arthritis), psoriasis, systemic lupus erythematosus, and multiple sclerosis), respiratory diseases (e.g., airway inflammation, chronic obstructive pulmonary disease, cystic fibrosis, asthma, allergy), transplant rejection (including solid organ transplant rejection), and inflammatory bowel diseases or disorders (e.g., ulcerative colitis, Crohn's disease). The present invention is further directed to novel therapeutics and therapeutic targets identified by methods of screening of the invention, and uses of such identified therapeutics in methods of treatment and prevention of IL- 17F/IL- 17A-associated disorders.
Methods are disclosed for separating and detecting bazedoxifene acetate from pharmaceutical compositions containing a mixture of bazedoxifene acetate and one or more other components that produce X-Ray diffraction patterns having interfering peaks at or near the characteristic peaks for bazedoxifene acetate.
C07D 209/00 - Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
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
B01D 53/94 - Chemical or biological purification of waste gases of engine exhaust gases by catalytic processes
The present teachings relate to compounds of formula I: wherein the constituent variables are defined herein. Compounds of the present teachings can act as antagonists of the mammalian adhesion proteins known as selectins. Methods for treating selectin mediated disorders are provided, which include administration of these compounds in a therapeutically effective amount.
The present teachings relate to novel compounds of formula I: wherein the constituent variables are as defined herein. Compounds of the present teachings can act as antagonists of the mammalian adhesion proteins known as selectins. Methods for treating or preventing selectin-mediated disorders are provided, which include administration of these compounds in a therapeutically effective amount.
C07D 215/50 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 4
C07D 409/04 - 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 directly linked by a ring-member-to-ring- member bond
The present invention provides compounds and methods for the use thereof to inhibit ß-secretase (BACE) and treat ß-amyloid deposits and neurofibrillary tangles.
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 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
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
64.
SHORTENED PURIFICATION PROCESS FOR THE PRODUCTION OF CAPSULAR STREPTOCOCCUS PNEUMONIAE POLYSACCHARIDES
A shortened process for producing a solution containing substantially purified capsular polysaccharides from a cellular Streptococcus pneumoniae lysate broth is described. Ultrafiltering and diafiltering a clarified S. pneumoniae lysate followed by pH adjustment to less than 4.5, preferably about 3.5, precipitated at least 98% of the protein in the solution without seriously affecting polysaccharide yield. Furthermore, following ultrafiltration and diafiltration and acidification to a pH of less than 4.5, filtration using activated carbon precipitated at least 90% of remaining protein without seriously affecting polysaccharide yield. Exemplary, non-limiting S. pneumoniae serotypes that can be purified using the shortened process of the invention are 1, 4, 5, 6A, 6B, 7F, 9V, 14, 18C, 19A, 19F, and 23F. In one embodiment, the Streptococcus pneumoniae cells are lysed using deoxycholate sodium (DOC), while in another embodiment the lytic agent is a non-animal derived lytic agent such as N-lauryl sarcosine sodium (NLS).
C08B 37/00 - Preparation of polysaccharides not provided for in groups Derivatives 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
The present invention provides methods for inducing cross-protective immunity against virulent strains of P. multocida in animals such as cattle and poultry. The methods of the invention include administering to an animal a mutant P. multocida strain, whereby the mutant P. multocida strain induces cross-protective immunity against one or more virulent P. multocida strains having serotypes that are different from the serotype of the mutant P. multocida strain. The mutant P. multocida strain will preferably contain one or more mutations that cause the cells to be acapsular and/or attenuated. Exemplary mutations include, e.g., mutations that impair the expression of one or more genes in the P. multocida capsule biosynthetic operon (e.g., phyB, phyA, hyaE, hyaD, hyaC, hyaB, hexD, hexC, hexB, and/or hexA).
The present invention provides a 2-amino-5-[substituted-4-(difluoromethoxy)phenyl]-5-phenylimidazolone compound of formula (I) The present invention also provides methods for the use thereof to inhibit ß-secretase (BACE) and treat ß-amyloid deposits and neurofibrillary tangles.
The present invention provides vaccine compositions comprising at least two strains of avian influenza virus, wherein one of the strains has an H5 hemagglutinin subtype and the other strain has an H7 hemagglutinin subtype, and wherein at least one of the strains has an N4 neuraminidase subtype and neither strain has an N1 subtype. Also provided are vaccination methods that utilize the novel vaccine compositions of the invention. The compositions and methods of the present invention provide protection against infection with H5 and H7 influenza strains (e.g., H5N1 and H7N1) while at the same time facilitating the distinction between infected and vaccinated animals.
The present invention relates to Imidazolopyrimidine Analogs, of Formula Ib methods of making Imidazolopyrimidine Analogs, compositions comprising an Imidazolopyrimidine Analog, and methods foτ treating oτ preventing a PI3K-related disorder comprising administering to a subject in need thereof an effective amount of an Imidazolopyrimidine Analog. The invention also relates to methods for treating or preventing mTOR -related disorders comprising administering to a subject in need thereof an effective amount of an Imidazolopyrimidine Analog.
The present invention relates to Pyrazolopyrimidine Analogs, methods of making Pyrazolopyrimidine Analogs, compositions comprising a Pyrazolopyrimidine Analog, and methods for treating mTOR -related disorders comprising administering to a subject in need thereof an effective amount of a Pyrazolopyrimidine Analog. The invention also relates to treating PI3K -related disorders comprising administering to a subject in need thereof an effective amount of a Pyrazolopyrimidine Analog.
Devices and methods that provide consistent skin side temperature comprising a primary insulative material disposed on a skin side of a thermal source; wherein the device provides a rate of change in temperature of less than about 0.8 are disclosed. Also included are methods of providing improved skin health, and methods of providing passive skin side temperature control.
This disclosure provides isolation and characterization of nucleotides encoding rat and cynomolgus monkey IL-21 and rat, rabbit and cynomolgus monkey IL-22, and the IL-21 and IL-22 polypeptides encoded thereby. This disclosure features rat and cynomolgus monkey IL-21 and rat, rabbit and cynomolgus monkey IL-22 nucleotide and amino acid sequences and variants thereof.
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
72.
SYNTHESIS AND CHARACTERIZATION OF POLYMORPH FORM III OF 4-(2,(4,4-DIMETHYL-2-OXOOXAZOLIDIN-3-YL)THIAZOL-4-YL)BENZONITRILE
A polymorph Form III of 4-(2-(4,4-dimethyl-2-oxooxazolidin-3-yl)thiazol-4-yl)benzonitrile and methods of preparing Form III are described. Also provided are methods of contraception, treating or preventing fibroids, uterine leiomyomata, endometriosis, dysfunctional bleeding, polycystic ovary syndrome, and hormone-dependent carcinomas, providing hormone replacement therapy, stimulating food intake, and synchronizing estrus including using polymorph Form III of 4-(2-(4,4-dimethyl-2-oxooxazolidin-3-yl)thiazol-4-yl)benzonitrile. Also provided are methods for preparing polymorph Form I of 4-(2-(4,4-dimethyl-2-oxooxazolidin-3-yl)thiazol-4-yl)benzonitrile from polymorph Form III of 4-(2-(4,4-dimethyl-2-oxooxazolidin-3-yl)thiazol-4-yl)benzonitrile.
C07D 417/04 - 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 directly linked by a ring-member-to-ring- member bond
A61K 31/422 - Oxazoles not condensed and containing further heterocyclic rings
A polymorph Form II of 4-(2-(4,4-dimethyl-2-oxooxazolidin-3-yl)thiazol-4-yl)benzonitrile and methods of preparing Form II are described. Also provided are methods of contraception, treating or preventing fibroids, uterine leiomyomata, endometriosis, dysfunctional bleeding, polycystic ovary syndrome, and hormone-dependent carcinomas, providing hormone replacement therapy, stimulating food intake, and synchronizing estrus including using polymorph Form II of 4-(2-(4,4-dimethyl-2-oxooxazolidin-3-yl)thiazol-4-yl)benzonitrile. Further provided are methods for preparing polymorph Form I of 4-(2-(4,4-dimethyl-2-oxooxazolidin-3-yl)thiazol-4-yl)benzonitrile from polymorph Form II of 4-(2-(4,4-dimethyl-2-oxooxazolidin-3-yl)thiazol-4-yl)benzonitrile.
C07D 417/04 - 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 directly linked by a ring-member-to-ring- member bond
A61K 31/427 - Thiazoles not condensed and containing further heterocyclic rings
A61P 15/00 - Drugs for genital or sexual disordersContraceptives
A method of automated determination of saccharide concentration is provided herein. The method includes preparing one or more saccharide standards and one or more diluted polysaccharide test samples, transferring a portion of the one or more saccharide standards and the one or more diluted polysaccharide test samples along with a diluent to a series of wells in a multiwell plate, transferring a portion of an acid reagent to the series of wells in the multiwell plate, mixing the contents of the series of wells in the multiwell plate, heating and cooling the contents of the series of wells in the multiwell plate, shaking the multiwell plate, and measuring the radiant energy absorbance of the contents of the series of wells in the multiwell plate, where all steps are performed in the absence of human intervention.
G01N 35/02 - Automatic analysis not limited to methods or materials provided for in any single one of groups Handling materials therefor using a plurality of sample containers moved by a conveyor system past one or more treatment or analysis stations
G01N 33/52 - Use of compounds or compositions for colorimetric, spectrophotometric or fluorometric investigation, e.g. use of reagent paper
75.
SULFONYLATED HETEROCYCLES USEFUL FOR MODULATION OF THE PROGESTERONE RECEPTOR
Compounds of the following structure are provided, wherein R1-R4 and R6-R9 are defined below, as are methods of preparing and using these compounds for contraception; treating or preventing fibroids, uterine leiomyomata, endometriosis, dysfunctional bleeding, polycystic ovary syndrome, and hormone-dependent carcinomas; providing hormone replacement therapy; stimulating food intake; synchronizing estrus; and treating cycle-related symptoms.
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 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 present invention relates to Pyrimxdo [5,4-c]quinoline-2, 4 -diamine Derivatives, compositions comprising an effective amount of a Pyrimido [5, 4 -c] quinoline-2, 4 -diamine Derivative of formula (I), methods for treating or preventing a proliferative disorder, comprising administering to a subject in need thereof an effective amount of an Pyrimido [ 5, 4 - c] quinoline-2, 4 -diamine Derivative. Disclosed are also methods for modulating PDK-I activity, comprising administering to a subject in need thereof an effective amount of a Pyrimido [5,4- c] quinoline- 2,4-diamine Derivative. The invention also relates to a process for preparing a Pyrimido [5,4- c] quinoline-2, 4 -diamine Derivative or a pharmaceutically acceptable salt thereof,
The present invention relates to Benzo[c] [2,7] naph thy ri dine Derivatives of formula (I), compositions comprising an effective amount of a Benzo[c] [2,7]naphthyridine Derivative, methods for treating or preventing a proliferative disorder or an autoimmune disease, comprising administering to a subject in need thereof an effective amount of a Benzo[c] [2,7]naphthyridine Derivative, methods for modulating PDK-I activity, PKA activity, Akt activity, S6K activity, or PKC activity, comprising administering to a subject in need thereof an effective amount of a Benzo[c] [2,7] naphthyridine Derivative. The invention also relates to processes for preparing a Benzo[c] [2,7] naphthyridine Derivative.
A61K 31/4375 - 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 six-membered ring having nitrogen as a ring hetero atom, e.g. quinolizines, naphthyridines, berberine, vincamine
In one embodiment, compounds of the following structure are described, wherein R1 to R7 are described herein. Formula (I). Also provided are methods for preparing these compounds and methods of contraception; treating or preventing fibroids; treating or preventing uterine leiomyomata; treating or preventing endometriosis, dysfunctional bleeding, and polycystic ovary syndrome; treating or preventing hormone-dependent carcinomas; providing hormone replacement therapy; stimulating food intake; synchronizing estrus; and treating cycle-related symptoms using the compounds described herein.
C07D 207/34 - 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 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, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
C07D 417/10 - 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 aromatic rings
A61K 31/40 - 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
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
An improved system for large scale production of polypeptides in cell culture is provided. In accordance with the present invention, cells expressing a polypeptide of interest are grown in media that contain copper, glutamate or both. The use of such a system allows production of polypeptides in which misfolding and/or aggregation are reduced, and in which total glycosylation is increased. Polypeptides expressed in accordance with the present invention may be advantageously used in the preparation of pharmaceutical, agricultural or other commercial compositions.
C12N 5/00 - Undifferentiated human, animal or plant cells, e.g. cell linesTissuesCultivation or maintenance thereofCulture media therefor
C07K 14/435 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans
C12P 21/02 - Preparation of peptides or proteins having a known sequence of two or more amino acids, e.g. glutathione
The present disclosure relates to multivalent immunogen compositions for treating or preventing diseases or disorders in canines caused by or associated with one or more of canine distemper virus, canine adenovirus (type 1 or type 2), canine parainfluenza virus, canine parvovirus, Leptospira canicola, Leptospira icterohaemorrhagiae, Leptospira grippotyphosa, Leptospira pomona, Leptospira bratislava, Leptospira hardjo, Leptospira autumnalis, Leptospira australis, Leptospira hebdomadis, and Bordetella bronchiseptica. The Leptospira compositions can also be used for treating or preventing leptospirosis diseases or disorders in canine, swine, and bovine.
C07K 14/20 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from bacteria from Spirochaetales (O), e.g. Treponema, Leptospira
Compounds of formula (Il) wherein each R1 and R2 is independently selected from H and -P(O)(R3) (R4), provided that at least one of R1 and R2 is -P(O)(R3)(R4); each R3 and R4 is independently selected from the group consisting of H -OH, C1-C6 alkyl, and C1-C6 alkoxy; or a pharmaceutically acceptable salt thereof. Pharmaceutical compositions comprising a compound of formula II, and methods of administering such compounds and compositions.
The present invention relates to processes for selective sulfation of an aromatic hydroxyl group over an aliphatic hydroxyl group where both are present in the same molecule. This invention also relates to processes for selective sulfation of the aromatic hydroxyl group of equilin, equilenin, estradiol, estra(1,3,5-triene)- 3,16,17-triol, dihydroequilenin or dihydroequilin. This invention further relates to alkali metal salts of dihydroequilenin sulfates, dihydroequilin sulfates, estradiol sulfates, and estriol sulfates, processes for making thereof, stable compositions comprising thereof, and the use thereof.
C07J 31/00 - Normal steroids containing one or more sulfur atoms not belonging to a hetero ring
A61K 31/565 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. oestrane, oestradiol
The present invention relates to sustained-release tablet formulations of piperazine- piperidine compounds, which can be useful in treating central nervous system disorders; to processes for their preparation; and to methods of using them.
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
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 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
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
The present invention provides a method for suppressing protein aggregation in a liquid formulation during freeze-thaw by including sorbitol in the liquid formulation. The present invention also provides methods for storing and preparing a liquid formulation containing a protein and sorbitol such that the presence of sorbitol suppresses protein aggregation during freezing and/or thawing.
Disclosed herein are methods of modulating adipogenesis. The methods include contacting a cell expressing the Ccdc80 gene with an agent that modulates the expression or activity of the Ccdc80 gene or Ccdc80 protein. Further disclosed herein are methods of treating conditions such as obesity, insulin resistance, and/or type 2 diabetes with Ccdc80 modulators. Also disclosed herein are methods of identifying Ccdc80 modulators.
A61K 38/17 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans
A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
C12Q 1/00 - Measuring or testing processes involving enzymes, nucleic acids or microorganismsCompositions thereforProcesses of preparing such compositions
G01N 33/50 - Chemical analysis of biological material, e.g. blood, urineTesting involving biospecific ligand binding methodsImmunological testing
A61K 31/7088 - Compounds having three or more nucleosides or nucleotides
88.
IMPROVED STABILITY IN VITAMIN AND MINERAL SUPPLEMENTS
The invention provides a multivitamin and mineral nutritional supplement composition comprising at least one polyvalent metal and at least one oxidizable vitamin with substantially improved resistance to reactions that lead to darkening and /or spotting and reactions that may reduce the potency of oxidizable vitamins. The composition is a multivitamin and mineral composition comprising at least one polyvalent metal and at least one oxidizable vitamin wherein the composition is substantially free of mobile bound water. The invention also includes methods for making such a composition and methods of preventing or reducing oxidation, improving the stability of oxidizable vitamins, and stabilizing the disintegration time of a multi-vitamin and mineral nutritional supplement composition.
The present invention provides a method for suppressing mannitol-induced protein aggregation by providing sucrose to a liquid formulation containing a protein. The present invention also provides methods for storing and preparing a liquid formulation containing a protein and a combination of mannitol and sucrose such that the presence of sucrose suppresses mannitol-induced protein aggregation.
Polymorphs, pharmaceutical compositions containing polymorphs, methods of using polymorphs and methods of preparing polymorphs of [1- (4-tert-Butylbenzyl) -5- (3-methylphenyl) -lH-indol-3-yl] (oxo) acetic acid are described herein.
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
A61K 31/405 - Indole-alkanecarboxylic acidsDerivatives thereof, e.g. tryptophan, indomethacin
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
C07C 209/48 - Preparation of compounds containing amino groups bound to a carbon skeleton by reduction of carboxylic acids or esters thereof in presence of ammonia or amines, or by reduction of nitriles, carboxylic acid amides, imines or imino-ethers by reduction of nitriles
92.
PHARMACEUTICAL COMPOSITIONS CONTAINING SUBSTITUTED INDOLE ACID DERIVATIVES AS INHIBITORS OF PLASMINOGEN ACTIVATOR INHIBITOR-1(PAI-1)
Pharmaceutical compositions containing compounds of formula (I) are provided: wherein the constituent variables are as defined herein. The compounds are inhibitors of plasminogen activator inhibitor-1 (PAI-1 ) and the compositions are useful for treating conditions resulting from fibrinolytic disorders, such as deep vein thrombosis and coronary heart disease, Alzheimer's disease and pulmonary fibrosis.
A61K 31/405 - Indole-alkanecarboxylic acidsDerivatives thereof, e.g. tryptophan, indomethacin
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 43/00 - Drugs for specific purposes, not provided for in groups
Pharmaceutical compositions containing compounds of formula (I) are provided wherein the constituent variables are as defined herein. The compositions are useful as inhibitors of plasminogen activator inhibitor-1 (PAI-1) for treating conditions resulting from fibrinolytic disorders, such as deep vein thrombosis and coronary heart disease, Alzheimer's disease and pulmonary fibrosis.
The present invention provides a topical, high-dose, long-acting ectoparasiticide composition, kit and method for protecting against ectoparasite infestations in a warm-blooded animal for a period of greater than about 6 weeks.
A01N 47/34 - Ureas or thioureas containing the groups N—CO—N or N—CS—N containing the groups , e.g. biuretThio-analogues thereofUrea-aldehyde condensation products
A01N 47/02 - 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
A01N 51/00 - Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds having the sequences of atoms O—N—S, X—O—S, N—N—S, O—N—N or O-halogen, regardless of the number of bonds each atom has and with no atom of these sequences forming part of a heterocyclic ring
A01N 53/00 - Biocides, pest repellants or attractants, or plant growth regulators containing cyclopropane carboxylic acids or derivatives thereof
A01N 37/18 - Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a carbon atom having three bonds to hetero atoms with at the most two bonds to halogen, e.g. carboxylic acids containing the group —CO—N, e.g. carboxylic acid amides or imidesThio-analogues thereof
A01N 37/52 - Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a carbon atom having three bonds to hetero atoms with at the most two bonds to halogen, e.g. carboxylic acids containing groups, e.g. carboxylic acid amidines
A01N 49/00 - Biocides, pest repellants or attractants, or plant growth regulators containing compounds containing the group wherein m+n≥1, both X together may also mean —Y— or a direct carbon-to-carbon bond, and the carbon atoms marked with an asterisk are not part of any ring system other than that which may be formed by the atoms X, the carbon atoms in square brackets being part of any acyclic or cyclic structure, or the group wherein A means a carbon atom or Y, n ≥ 0, and not more than one of these carbon atoms being a member of the same ring system, e.g. juvenile insect hormones or mimics thereof
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 applicationSubstances for reducing the noxious effect of the active ingredients to organisms other than pests containing liquids as carriers, diluents or solvents
A61K 31/175 - Amides, e.g. hydroxamic acids having the group N—C(O)—N or N—C(S)—N, e.g. urea, thiourea, carmustine having the group , N—C(O)—N=N— or , e.g. carbonohydrazides, carbazones, semicarbazides, semicarbazonesThioanalogues thereof
A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
A61K 31/341 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide not condensed with another ring, e.g. ranitidine, furosemide, bufetolol, muscarine
95.
IMMUNOPHILIN LIGANDS AND METHODS FOR MODULATING IMMUNOPHILIN AND CALCIUM CHANNEL ACTIVITY
Immunophilin ligands and their uses as modulators of calcium channel activity are disclosed. Screening, therapeutic and prophylactic methods for conditions associated with calcium channel dysfunction, e.g., neurodegenerative and cardiovascular disorders, are also disclosed.
A61K 38/17 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans
96.
USE OF ESTROGEN RECEPTOR BETA SELECTIVE LIGANDS FOR TREATING ACUTE LUNG INJURIES
The present invention provides a method of treating acute lung injuries, such as acute lung injury induced by peritonitis during sepsis, acute lung injury induced by intravenous bacteremia during sepsis, acute lung injury caused by smoke inhalation, acute lung injury occurring in a premature infant with deficiency of surfactant, acute lung injury caused by oxygen toxicity or acute lung injury caused by barotraumas from mechanical ventilation, using an ERβ selective ligand such as 2-(3-fluoro-4-hydroxyphenyl)-7-vinyl-1,3-benzoxazol-5-ol or 3-(3-fluoro-4-hydroxy-phenyl)-7-hydroxy-naphthalene-1-carbonitrile. The present invention further relates to use of ERβ selective ligands or compositions thereof for the prevention of acute lung injuries in those being at risk thereof.
A61K 31/055 - Phenols the aromatic ring being substituted by halogen
A61K 31/34 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
A61K 31/343 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide condensed with a carbocyclic ring, e.g. coumaran, bufuralol, befunolol, clobenfurol, amiodarone
A61K 31/4184 - 1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
A61K 31/423 - Oxazoles condensed with carbocyclic rings
A61K 31/428 - Thiazoles condensed with carbocyclic rings
A61P 43/00 - Drugs for specific purposes, not provided for in groups
A61P 11/00 - Drugs for disorders of the respiratory system
97.
ASSESSMENT OF ASTHMA AND ALLERGEN-DEPENDENT GENE EXPRESSION
The present invention provides methods for the assessment, diagnosis, or prognosis of asthma including methods for providing an assessment, diagnosis, or prognosis comprising the step of exposing a sample derived from a patient to an allergen in vitro. The present invention also provides methods for selecting, as well as evaluating the effectiveness of, asthma treatments. The markers of the present invention can be used in methods to identify or evaluate agents capable of modulating marker expression levels in subjects with asthma.
The present invention provides methods of treating inflammatory diseases/disorders in a subject by inhibiting/antagonizing TREM-1 expression/activity/signal transduction and/or DAP12/TyroBP expression and/or activity. Methods of detecting the presence of inflammatory disease in a subject by detecting TREM-1 and/or DAP12/TyroBP expression and/or activity in the subject or a sample obtained therefrom, wherein increased expression or activity is indicative of the inflammatory disease are also included. The present invention further provides methods for assessing the efficacy of a TREM-1-modulating agent administered to a patient by detecting levels of secreted phosphoprotein 1 (SPP1) and/or one or more other biomarkers in the patient or in a sample from the patient.
The invention relates to methods of identifying modulators of a cationic amino acid transporter protein, or modulators of CAT-regulated nitric oxide production, which can be used to alleviate pain or to treat pain insensitivity.
The present invention is directed to tablet-in-tablet compositions comprising one or more estrogens in a first layer and a therapeutic agent in a second layer, and processes for their preparation
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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
A61K 31/57 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
A61K 31/565 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. oestrane, oestradiol
patents