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8470818 Compounds and methods for kinase modulation, and indications therefor  
Compounds active on protein kinases are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases.
8470849 7-azaindole derivatives as selective 11-β-hydroxysteroid dehydrogenase type 1 inhibitors  
The present invention relates to 7-azaindole derivatives of formula I as selective inhibitors of the enzyme 11-beta-hydroxysteroid dehydrogenase type 1 (11β-HSD-1) and the use of such compounds ...
8470817 Compounds and methods for treatment of cancer  
Compounds for treating, preventing or managing cancer are disclosed. Also provided are methods for using the compounds in treatment of various cancers. Also provided are methods of treatment using...
8466152 (aza)indole derivative and use thereof for medical purposes  
The present invention provides compounds useful as agents for the prevention or treatment of a disease associated with abnormal serum uric acid level which has a uricosuric activity or the like....
8466169 SF5 derivatives as PAR1 inhibitors, production thereof, and use as medicaments  
The invention relates to novel compounds of formula I where R1, R2, R3, R4, R5, R9, Ar, Q1, Q2 and Q3 are each as defined below. The compounds of the formula I have antithrombotic activity and...
8466170 7-azaindole derivatives  
Novel 7-azaindole derivatives of the formula (I), in which U, L, R, Y, X1, X2 and X3 have the meanings indicated in Claim (1), are kinase inhibitors and can be used for the treatment of diseases...
8461169 Compounds modulating c-fms and/or c-kit activity  
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...
8461176 Enantiomerically enriched aryloazol-2-yl cyanoethylamino compounds, method of making and method of using thereof  
The present invention relates to novel aryloazol-2-yl-cyanoethylamino derivatives substantially enriched in an enantiomer of formula (I): and compounds of formula (IH) wherein R3, R4, R5, R6, R7,...
8461083 Herbicidal compounds  
The present invention relates to novel herbicidal [1,8]-naphthyridines of Formula (Ia) or (Ib), or an agronomically acceptable salt of said compound wherein R2, R3, R4, R5, R6, R7, R8, n, m, X and...
8461179 Dihydronaphthyridines and related compounds useful as kinase inhibitors for the treatment of proliferative diseases  
The invention relates to dihydronaphthyridines and related compounds; compositions comprising an effective amount of a dihydronaphthyridine or a related compound; and methods for treating or...
8461178 Naphthyridine derivatives and the use thereof as kinase inhibitors  
The present invention relates to kinase modulators of the naphthyridine type and to the preparation and use thereof as medicaments for the modulation of misdirected cellular signal transduction...
8461177 Antiviral drugs for treatment of arenavirus infection  
Compounds, methods and pharmaceutical compositions for treating viral infections, by administering certain compounds in therapeutically effective amounts are disclosed. Methods for preparing the...
8455477 Therapeutic compounds  
The present invention relates to pyrazolopyridines and imidazopyridines which are inhibitors of the kinase PDK1 and are thus useful for the treatment of myeloproliferative disorders or cancer. The...
8455511 Pyrrolopyridine derivatives substituted with cyclic amino group  
An object of the present invention is to provide an antagonist against CRF receptors which is effective as a therapeutic or prophylactic agent for diseases in which CRF is considered to be...
8450340 1H-pyrazolo[3,4-b]pyridines and therapeutic uses thereof  
Provided herein are compounds according to Formula I and pharmaceutically acceptable salts thereof, and compositions comprising the same, for use in various methods, including treating cancers such...
8450341 Substituted indolin-2-one derivatives and their use as P38 mitogen-activated kinase inhibitors  
The present disclosure is directed to new inhibitors of the p38 mitogen-activated protein kinase having the general formula (I), processes for preparation thereof, pharmaceutical compositions...
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.
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...
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...
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...
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...
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,...