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8445509 Fused heterocyclic derivatives and use thereof  
The present invention provides a fused heterocyclic derivative having a strong kinase inhibitory activity and use thereof. The present invention relates to a compound represented by the formula...
8445488 Pyrrolo[2,3-b]pyridin-4-yl-amines and pyrrolo[2,3-b]pyrimidin-5-yl-amines as Janus kinase inhibitors  
The present invention provides pyrrolo[2,3-b]pyridine-4-yl amines pyrrolo[2,3-b]pyrimidin-4-yl amines that modulate the activity of Janus kinases and are useful in the treatment of diseases related...
8445510 Fused bicyclic kinase inhibitors  
Compounds of Formula I, as shown below and defined herein: pharmaceutically acceptable salts thereof, synthesis, intermediates, formulations, and methods of disease treatment therewith, including...
8440666 Pyridazinone compounds and P2X7 receptor inhibitors  
Novel pyridazinone compounds of formula (I), which inhibit the purinergic P2X7 receptor and are useful for prevention, therapy and improvement of inflammatory and immunological diseases.
8440830 Tetrahydro-fused pyridines as histone deacetylase inhibitors  
The compounds of formula (I), wherein ring D and ring E together form a fused ring system selected from formula (II), (III), (IV), (V), (VI), (VII), and the salts of these compounds are novel,...
8440689 Fused heteroaromatic pyrrolidinones  
Disclosed are compounds of Formula 1, and pharmaceutically acceptable salts thereof, wherein G, L1, L2, R1, R2, R3, and R4 are defined in the specification. This disclosure also relates to...
8436180 Substituted-4-aryl-1,4-dihydro-1,6-naphthyridinamides and use thereof  
The present application relates to novel substituted 4-aryl-1,4-dihydro-1,6-naphthyridine-3-carboxamides, a process for their preparation, their use for the treatment and/or prophylaxis of...
8435980 Pyrrolopyridine inhibitors of kinases  
The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein R1a, R1b, R1c, X, and Y are defined in the description. The present invention relates also to...
8436011 Pyridinopyridinone derivatives, preparation thereof and therapeutic use thereof  
The present invention relates to pyridopyridone derivatives of formula (I): in which the variables are as defined herein, to their preparation and to their therapeutic use as inhibitors of the...
8431703 Pyrrolopyridine compounds and their use in treating disease  
There are provided according to the invention compounds of formula (I) in free ors salt form, wherein R1, R2, R4, R5, R6, A, D, X, W, m and n are as described in the specification, process for...
8431594 Bridged bicyclic heteroaryl substituted triazoles useful as AXL inhibitors  
Bridged bicyclic heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine...
8426441 Inhibitors of bruton's tyrosine kinase  
This application discloses novel imidazo[1,2-a]pyridine and imidazo[1,2-b]pyridazine derivatives according to Formulae I-VI: wherein R, R′, R″, Q, X, and Y are defined as described herein, whi...
8426440 Indolymaleimide derivatives  
A compound of formula (I), wherein R, R1, R2, ring A, which ring contains one or two nitrogen atoms, and ring B are as defined in the Specification, pharmaceutical compositions containing these...
8420666 Pyrazolo (3, 4-B) pyridine derivatives as phosphodiesterase inhibitors  
The present invention relates to phosphodiesterase (PDE) type 4, phosphodiesterase (PDE) type 7 and dual PDE type 4/PDE type 7 inhibitors. Compounds disclosed herein having the structure of Formula...
8415333 Bronchodilating diazaheteroaryls  
The invention relates to novel compounds having the general formula (I), and which compounds are useful to treat a disorder or disease characterized by bronchoconstriction, e.g. COPD and asthma.
8415362 Pyrazolyl substituted pyrrolo[2,3-b]pyrimidines as Janus kinase inhibitors  
The present invention provides heteroaryl substituted pyrrolo[2,3-b]pyridines and heteroaryl substituted pyrrolo[2,3-b]pyrimidines of Formula I: that modulate the activity of Janus kinases and are...
8410109 Pharmaceutical compositions for the prevention and treatment of complex diseases and their delivery by insertable medical devices  
The present invention relates to polyphenol-like compounds that are useful for inhibiting VCAM-1 expression, MCP-1 expression and/or SMC proliferation in a mammal. The disclosed compounds are...
8410132 Modulators of cystic fibrosis transmembrane conductance regulator  
The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions the...
8409606 Drug delivery through hydrogel plugs  
An embodiment is a medical prosthesis for blocking or reducing tear flow through a punctum or canaliculus of a human eye and delivering a drug to the eye that comprises a dehydrated covalently...
8404710 Phosphodiesterase 10A inhibitor  
A phosphodiesterase 10A inhibitor serving as an effective prophylactic or therapeutic agent for Parkinson's disease, Huntington's disease, Alzheimer's disease, and schizophrenia. The PDE10A...
8404845 2,3-substituted azaindole derivatives for treating viral infections  
The present invention relates to 2,3-Substituted Azaindole Derivatives, compositions comprising at least one 2,3-Substituted Azaindole Derivatives, and methods of using the 2,3-Substituted...
8404709 Substituted 4-aryl-1,4-dihydro-1,6-naphthyridines and use thereof  
The present application relates to novel substituted 4-aryl-1,4-dihydro-1,6-naphthyridines, a process for their preparation, their use for the treatment and/or prophylaxis of diseases, and their...
8404700 Compounds modulating c-fms and/or c-kit activity and uses therefor  
Compounds active on the receptor protein tyrosine kinases c-kit and/or c-fms are provided herewith. Also provided herewith are compositions useful for treatment of c-kit mediated diseases or...
8404848 Derivatives of imidazo[1,2-a]pyridine-2-carboxamides, preparation method thereof and use of same in therapeutics  
The present invention is related to a compound of formula (I): wherein R1, R2, R3, R4 and X are as defined herein, or an addition salt with an acid thereof, its pharmaceutical composition or use...
8399449 Fused heterocyclic derivative and use thereof  
The present invention provides a compound having a superior Smo inhibitory activity and lower toxicity, which is sufficiently satisfactory as a pharmaceutical product. The present invention...
8399477 (Aza)indole derivative substituted in position 5, pharmaceutical composition comprising it, intermediate compounds and preparation process therefor  
An (aza)indole derivative substituted in position 5, of formula (I) in which X, Y, Z, G1, G2, G3, R1, W, and R2 have the meanings given in the description, a pharmaceutical composition comprising...
8399476 Imidazo[1,2-a]pyridines and their use as pharmaceuticals  
The present invention relates to derivatives of imidazo[1,2-a]pyridines of formula I, in which R, R1 to R4 and n have the meanings indicated in the claims, which modulate the transcription of...
8399478 Thiophene-carboxamides useful as inhibitors of protein kinases  
The present invention relates to compounds useful as inhibitors of protein kinase represented by formula (I): or a pharmaceutically acceptable salt thereof. The invention also provides...
8394820 N-azabicyclic carboxamide derivatives, preparation thereof and therapeutic use thereof  
This disclosure relates to compounds of formula (I): wherein X1, X2, X3, X4, n, Y, W, and A are as defined in the disclosure, or a salt thereof, or a hydrate or solvate thereof, and to processes...
8389516 Antibacterial compositions  
Compounds of formula (I) have antibacterial activity: wherein: m is 0 or 1; Q is hydrogen or cyclopropyl; Alk is an optionally substituted, divalent C1-C6 alkylene, alkenylene or alkynylene radical...
8383660 Dibenzyl amine compounds and derivatives  
Dibenzyl amine compounds and derivatives of Formula I, pharmaceutical compositions containing such compounds and the use of such compounds to elevate certain plasma lipid levels, including high...
8377942 Isoxazolines derivatives and their use as pesticide  
Novel isoxazoline compounds, compositions containing the compounds and methods for making the compounds are disclosed. The compounds and compositions have pesticidal properties and are suitable for...
8372862 Pharmaceutical composition for preventing or treating osteoporosis or obesity comprising phenyltetrazole derivative  
A phamaceutical composition comprising a phenyltetrazole derivative of formula (I) or a pharmaceutical acceptable salt thereof is effective in preventing or treating osteoporosis, obesity,...
8372863 Tetrahydro-1H-pyrrolo fused pyridones  
The present invention relates to tetrahydro-1H-pyrrolo fused pyridone compounds useful as HIF prolyl hydroxylase inhibitors to treat anemia and like conditions.
8367662 Organic compounds  
Compounds of formula I: in free or salt or solvate form, where R1, R2, R3 and R20 have the meanings as indicated in the specification, are useful for treating diseases mediated by the ALK-5 and/or...
8362020 Hepatitis C virus inhibitors  
The present disclosure is generally directed to antiviral compounds, and more specifically directed to compounds which can inhibit the function of the NS5A protein encoded by Hepatitis C virus...
8362065 Carbazole carboxamide compounds useful as kinase inhibitors  
Compounds having the formula (I), and enantiomers, and diastereomers, pharmaceutically-acceptable salts, thereof, are useful as kinase modulators, including Btk modulation.
8357684 Thyazolopyridin-2-yloxy-phenyl and thiazolopyrazin-2-yloxy-phenyl amines as modulators of leukotriene A4 hydrolase  
Thiazolopyridin-2-yloxy-phenyl and thiazolopyrazin-2-yloxy-phenyl amine compounds are described, which are useful as LTA4 hydrolase (LTA4H) modulators. Such compounds may be used in pharmaceutical...
8354425 Azabicyclic carboxamide derivatives, preparation thereof and therapeutic use thereof  
The disclosure relates to compounds of formula (I): wherein X1, X2, X3, X4, Z1, Z2, Z3, Z4, Ra, Rb, n, Y, and W are as defined in the disclosure, or a salt thereof, or a hydrate or solvate thereof,...
8349830 Aryl aminopyridine PDE10 inhibitors  
The present invention is directed to aryl aminopyridine compounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10...
8343996 Azaquinolinone derivatives and uses thereof  
The present invention provides compounds and methods for treating or preventing the development of a disease, disorder, or condition in a subject or patient.
8338452 Raf inhibitor compounds and methods of use thereof  
Compounds of Formula (I) are useful for inhibition of Raf kinases. Methods of using compounds of Formula (I) and stereoisomers, tautomers, prodrugs and pharmaceutically acceptable salts thereof,...
8338453 Treatment of progressive neurodegenerative disease with ibudilast  
Compositions and methods for treating progressive neurodegenerative diseases, and their associated symptoms by administration of ibudilast (3-isobutyryl-2 -isopropylpyrazolo[1,5-a]pyridine).
8338451 Polysubstituted derivatives of 2-heteroaryl-6-phenylimidazo[1,2-a]pyridines, and preparation and therapeutic use thereof  
Compounds of formula (I): wherein R, R1, R2, R3, R4 and X are as defined in the disclosure, or an acid addition salt thereof, and the therapeutic use and process of synthesis thereof.
8334294 4,8-diphenyl-polyazanaphthalene derivatives  
New inhibitors of the p38 mitogen-activated protein kinase having the general formula (I) are disclosed herein, as well as processes for their preparation, pharmaceutical compositions comprising...
8329724 Process for the manufacture of pharmaceutically active compounds  
According to the present invention there are provided novel processes for the manufacture of the compound of formula 1 as well as novel synthesis routes for key intermediates used in those processes.
8329725 Annelated pyrrolidin sulfonamides with oxadiazolone headgroup, processes for their preparation and their use as pharmaceuticals  
The invention relates to annelated pyrrolidin sulfonamides with oxadiazolone headgroup and to their physiologically acceptable salts and physiologically functional derivatives showing PPARdelta or...
8324214 1,3-dihydro-2H-pyrrolo[3,2-bpyridin-2-one derivatives, preparation thereof and therapeutic uses thereof  
The subject matter of the present invention are compounds corresponding to formula (I): in which: X is an unsubstituted or substituted divalent (C1-C5)alkylene radical; RI is an —NR8R9 group; or a...
8324238 Aspartate of 1-cyclopropyl-6-fluoro-7-(8-methoxyimino-2,6-diaza-spiro[3.4]oct-6-yl)-4-oxo-1,4-dihydro-[1,8]naphthyridine-3-carboxylic acid, method for preparing the same, and antimicrobial pharmaceutical composition comprising the same  
Disclosed are aspartic acid salts of 1-cyclopropyl-6-fluoro-7-(8-methoxyimino-2,6-diaza-spiro[3.4 ]oct-6-yl)-4-oxo-1,4-dihydro-[1,8]naphthyridine-3-carboxylic acid, methods for preparing the same,...
8318703 Methods for improving kidney function  
The invention relates to methods for improving renal (kidney) function. Methods for decreasing blood urea nitrogen (BUN), for increasing glomerular filtration rate (GFR), and for decreasing serum...