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8791114 Dihydropyrazoles  
Novel dihydropyrazole derivatives of formula (I) wherein L, R, R3, R4, R5, R6, R7, X1, X2, X3, X4, Y, m and n have the meaning according to the claims, are positive allosteric modulators of the FSH...
8791113 2,4-diaryl-substituted [1,8] naphthyridines as kinase inhibitors for use against cancer  
The present invention relates to novel [1,8]naphthyridine derivatives of formula (I) and to the use of such compounds in which the inhibition, regulation and/or modulation of signal transduction by...
8778964 Hydroxy-substituted imidazo[1,2-a]-pyridinecarboxamides and their use  
The present application relates to novel substituted imidazo[1,2-a]pyridine-3-carboxamides, to processes for their preparation, to their use alone or in combinations for the treatment and/or...
8778977 Pyridinonyl PDK1 inhibitors  
The present invention provides pyridinonyl PDK1 inhibitors and methods of treating cancer using the same.
8772288 Substituted spiro[cycloalkyl-1,3′-indo]-2′(1′H)-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...
8765782 Indole derivatives as selective androgen receptor modulators (SARMS)  
The present invention is directed to novel indole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the androgen...
8765748 Indazolyl, benzimidazolyl, benzotriazolyl substituted indolinone derivatives as kinase inhibitors useful in the treatment of cancer  
The present invention is directed to a compound is represented by Structural Formula (A): or a pharmaceutically acceptable salt thereof. The present invention is also directed to a pharmaceutical...
8765759 Monocyclic CGRP receptor antagonists  
The present invention is directed to compounds of the formula: (wherein variables A1, A2, A3, G1, G2, G3, G4, J, Ea, Eb, Ec, R6, R7, and Y are as described herein) which are antagonists of CGRP...
8765743 Compounds  
The invention is directed to compounds of formula (I) and salts thereof. The compounds of the invention are inhibitors of PI3-kinase activity.
8765954 1,8-naphthyridine compounds for the treatment of cancer  
Compounds and compositions for treating, preventing or managing cancer are disclosed. The compositions provided herein comprise SNS-595 and N-desmethyl-SNS-595. Also provided are pharmaceutical...
8765767 Positive allosteric modulators of mGluR2  
The disclosure generally relates to compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds modulate the mGluR2 receptor and may be...
8759341 Bi- and tricyclic indazole-substituted 1,4-dihydropyridine derivatives and uses thereof  
This invention relates to novel bi- and tricyclic indazole-substituted 1,4-dihydropyridine derivatives having protein tyrosine kinase inhibitory activity, to a process for the manufacture thereof...
8758830 Pyrrolopyridines as kinase inhibitors  
Compounds of Formula I are useful for inhibition of CHK1 and/or CHK2. Methods of using compounds of Formula I and stereoisomers and pharmaceutically acceptable salts thereof, for in vitro, in situ,...
8759539 Substituted bicyclic amines for the treatment of diabetes  
Described herein are substituted bicyclic amines. In particular, described herein are substituted bicyclic amines that are effective as antagonists of SSTR5 and useful for the treatment, control or...
8754101 N-cyclobutyl-imidazopyridine-methylamine as TRPV1 antagonists  
A compound of formula (I) wherein X represents a H atom, or a CH2OH group,Y represents a H atom, or a CH2OH group,but X and Y are not both CH2OH groupsand Ar is selected from or a pharmaceutically...
8754102 Nitrogen containing compounds and their use  
Compounds of Formula (I), their preparation and use in preventing or treating bacterial infections are disclosed.
8754082 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...
8754100 Nitrogen-containing fused heterocyclic compounds and their use as beta amyloid production inhibitors  
A compound represented by the formula [I]: or a pharmacologically acceptable salt or ester thereof, wherein Ring A represents a five-membered aromatic heterocyclic group or the like fused with a...
8754071 Compounds and compositions as c-kit kinase inhibitors  
The invention provides compounds and pharmaceutical compositions thereof, which are useful as protein kinase inhibitors, as well as methods for using such compounds to treat, ameliorate or prevent...
8754103 ***WITHDRAWN PATENT AS PER THE LATEST USPTO WITHDRAWN LIST***
Fused heterocyclic compounds as ion channel modulators
 
The present invention relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In...
8748454 Anti-constipation composition  
An object of the present invention is to provide an anti-constipation composition containing a halogenated-bi-cyclic compound as an active ingredient in ratio of bi-cyclic/mono-cyclic structure of...
8748612 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...
8748455 ***WITHDRAWN PATENT AS PER THE LATEST USPTO WITHDRAWN LIST***
Solid forms of a pharmaceutically active substance
 
The present invention provides solid forms of the compound of formula 1 and pharmaceutical uses thereof.
8741920 Process for the manufacture of pharmaceutically active compounds  
The present invention relates to a composition comprising the compound of formula (1), and the compound of formula (B),
8741921 N-(imidazolidin-2-ylidene)-heterocyclopenta[b]pyridine derivatives as modulators of alpha 2 adrenergic receptors  
The present invention relates to novel N-(imidazolidin-2-ylidene)-heterocyclo penta[b]pyridine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use...
8741895 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...
8741897 Glucocorticoid mimetics, methods of making them, pharmaceutical compositions and uses thereof  
Compounds of Formula (IA), (IB), (IC), and (ID) wherein R1, R2, R3, R4, R5, and R6 are as respectively defined herein for Formula (IA), (IB), (IC), and (ID), or a tautomer, prodrug, solvate, or...
8735398 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...
8735424 Bicyclic kinase inhibitors  
New compounds, compositions and methods of inhibition of Provirus Integration of Maloney Kinase (PIM kinase) activity associated with tumorigenesis in a human or animal subject are provided. In...
8729081 Compositions and methods for treating alcohol use disorders, pain and other diseases  
The present invention provides compounds which antagonize epsilon protein kinase C (PKCε). These compounds have a structural formula (Ia), (Ic) or (II). The present invention also provides ...
8729096 Imidazolidine-2,4-dione derivatives as N-formyl peptide receptor 2 modulators  
The present invention relates to novel imidazolidine-2,4-dione derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators...
8729074 Inhibitors of PI3 kinase  
The present invention relates to compounds of Formula I, II or III or a pharmaceutically acceptable salt thereof; methods of treating diseases or conditions, such as cancer, using the compounds;...
8729095 3-(biaryloxy)propionic acid derivatives for prevention and/or treatment of thromboembolic diseases  
A compound of the general formula (I): [wherein, R1 represents a halogen atom, or the like, R2 represents a hydrogen atom, or the like, R3 and R4, each independently, represent a hydrogen atom, a...
8722677 Viral inhibitors  
Pyrrolo[2,3-c]pyridine or pyrrolo[3,2-c]pyridine compounds having the general formula (A), wherein the dashed lines, X, Y and R1 through R5 are as defined in the specification. The compounds are...
8722708 Substituted isoindolines as aspartyl protease inhibitors  
Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein Q is a bond or —N(R5)—;T is a bond, —O—, —C(O)—; S, —N(R5)—, or...
8722702 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...
8722687 Imidazo [1,2-A]pyridine derivatives as FGFR kinase inhibitors for use in therapy  
The invention relates to new bicyclic heterocyclyl derivatives of formula (I), to pharmaceutical compositions comprising said compounds and to the use of said compounds in the treatment of...
8716273 N-(amino-heteroaryl)-1H-pyrrolopyridine-2-carboxamides derivatives preparation thereof and their use in therapy  
The invention relates to compounds of the general formula (I): Wherein X, Y, Z, Z1, Z2, Z3, Z4 and n are as defined herein. The invention also relates to a method for making the same and to the use...
8716272 N-(amino-heteroaryI)-1H-pyrrolopyridine-2-carboxamides derivatives preparation thereof and their use in therapy  
The invention relates to compounds of the general formula (I): Wherein X, Y, Z, Z1, Z2, Z3, Z4 and n are as defined herein. The invention also relates to a method for making the same and to the use...
8710073 Anti-infective derivatives, method for the production thereof, pharmaceutical compositions containing same and uses of said derivatives in treatment  
The present invention relates to bi-substrate inhibitor molecules combining (i) a pyridine, pyridinium or dihydropyridine-type structure allied to active metabolites of isoniazide, or related...
8710074 Dihydronaphthyridinyl(organo)methanone analogs as positive allosteric mGluR5 modulators  
In one aspect, the invention relates to dihydronaphthyridinyl(organo)methanone analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the...
8709419 Combination therapy  
The present invention relates to a combination therapy of propane-1-sulfonic acid {3-[5-(4-chloro-phenyl)-1H-pyrrolo[2,3-b]pyridine-3-carbonyl ]-2,4-difluoro-phenyl}-amide, or a pharmaceutically...
8710043 TRPM8 antagonists and their use in treatments  
Compounds of Formula I are useful as antagonists of TRPM8. Such compounds are useful in treating a number of TRPM8 mediated disorders and conditions and may be used to prepare medicaments and...
8703794 Indazole inhibitors of the Wnt signal pathway and therapeutic uses thereof  
Indazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of an indazole compound or analogs thereof, in the...
8703165 Spiro fused 1-amino-piperdine pyrrolidine dione derivatives with pesticidal activity  
Compounds of the formula (I) wherein the substituents are as defined in claim 1, are useful as pesticides.
8703797 Condensed ring pyridine compounds as subtype-selective modulators of sphingosine-1-phosphate-2 (S1P2) receptors  
The invention provides compounds represented by the formula I, each of which compounds may have sphingosine-1-phosphate receptor agonist and or antagonist biological activity, wherein these...
8697692 Pyrrolo [3,2-c] pyridine-4-one 2-indolinone protein kinase inhibitors  
The present invention relates to pyrrolo[3,2-c]pyridine-4-one 2-indolinone compounds of Formula (I) and their pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8 X, Y...
8697697 Pyrazole derivatives as ERK inhibitors  
This invention describes substituted pyrazole derivatives of Formula I and methods of making and using the compounds. These compounds have utility in the treatment of conditions or diseases in...
8691813 Indole and benzoxazine derivatives as modulators of metabotropic glutamate receptors  
The present invention relates to novel indole and benzoxazine derivatives which are positive allosteric modulators of the metabotropic glutamate receptor subtype 2 (“mGluR2”) and which are use...
8691838 Heterocycles as protein kinase inhibitors  
Selected compounds are effective for prophylaxis and treatment of diseases, such as HGF mediated diseases. The invention encompasses novel compounds of Formula I, analogs, prodrugs and...