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8178548 |
Anti-infective agents and uses thereof
This invention relates to: (a) compounds and salts thereof that, inter alia, inhibit HCV; (b) intermediates useful for the preparation of such compounds and salts; (c) compositions comprising such...
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8173639 |
Isoquinolinone derivatives as NK3 antagonists
Isoquinolone derivatives of the general formula are provided. The compounds are NK3 antagonists and useful for the treatment of e.g. psychosis and schizophrenia.
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8173674 |
Sulfonyl-phenyl-2H-[1,2,4]oxadiazol-5-one derivatives, processes for their preparation and their use as pharmaceuticals
The invention relates to sulfonyl-phenyl-oxadiazolones and to their physiologically acceptable salts and physiologically functional derivatives showing PPARdelta or PPARdelta and PPARgamma agonist...
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8163756 |
Enzyme modulators and treatments
Novel compounds and methods of using those compounds for the treatment of inflammatory conditions, hyperproliferative diseases, cancer, and diseases characterized by hyper-vascularization are...
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8163744 |
Tetrahydro-isoquinolin-1-ones for the treatment of cancer
The present invention provides a compound selected from compounds of formula I as ligand binding to the HDM2 protein, inducing apoptosis and inhibiting proliferation, and having therapeutic utility...
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8143274 |
1-(2H)-isoquinolone derivative
The present invention provides: a compound represented by the following formula (I): [wherein Y1 and Y4 represent a hydrogen atom or a halogen atom; either one of Y2 and Y3 represents —NR1R2, and t...
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8143257 |
Substituted phenols as active agents inhibiting VEGF production
The present invention relates to methods, compounds, and compositions for inhibiting angiogenesis. More particularly, the present invention relates to methods, compounds, and compositions for...
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8124582 |
Treatment of diabetes
The present invention relates to methods and compounds for regulating glucose metabolism, achieving glucose homeostasis, and decreasing blood glucose levels. Methods and compounds for treating or...
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8097627 |
Multiply-substituted tetrahydronaphthalene derivatives, process for their production and their use as anti-inflammatory agents
The invention relates to multiply-substituted tetrahydronaphthalene derivatives of formula (I) process for their production and their use as anti-inflammatory agents.
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8093258 |
Use of urokinase inhibitors for the treatment and/or prevention of neuropathological diseases
The present invention relates to methods and compositions for the treatment and/or prevention of neuropathological and/or neurodegenerative diseases. In particular, the invention delivers novel...
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8093288 |
Genipin derivatives and uses thereof
Genipin derivatives and pharmaceutical compositions thereof that inhibit the activity of uncoupling protein-2 (UCP2) and are useful in treating deficient first-phase insulin secretion, non-insulin...
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8093273 |
Flavanoids and isoflavanoids for the prevention and treatment of cardiovascular diseases
The present disclosure provides non-naturally occurring polyphenol compounds that upregulate the expression of Apolipoprotein A-I (ApoA-I). The disclosed compositions and methods can be used for...
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8093265 |
Bicycloheteroaryl compounds as P2X7 modulators and uses thereof
Compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety...
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8084047 |
Compositions and methods for treatment of eye disorders
The present invention provides compounds and methods for the treatment of LFA-1 mediated diseases. In particular, LFA-1 antagonists are described herein and these antagonists are used in the...
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8071618 |
Caspase inhibitors and uses thereof
The present invention provides a compound of formula I: wherein: X is —OR1 or —N(R5)2,Y is halo, trifluorophenoxy, or tetrafluorophenoxy;R1 is: C1-6 straight chained or branched alkyl, alkenyl, or ...
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8067457 |
Compounds useful as antagonists of CCR2
The present invention provides compounds of general formula I: or a pharmaceutically acceptable salt thereof, wherein X, n, Y, and R1 are defined generally and in subsets herein. Compounds of the...
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8048862 |
Macrocyclic inhibitors of hepatitis C virus replication
The embodiments provide compounds of the general Formulae I, II, III, IV, V, VI, VII, and X, as well as compositions, including pharmaceutical compositions, comprising a subject compound. The...
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8044067 |
Isoquinolines as IGF-1R inhibitors
Compounds of the formula (I): were synthesized. In at least one embodiment, they were found to down-regulate or inhibit the expression or function of the IGF-1 receptor.
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8039484 |
Antidiabetic bicyclic compounds
Diaryl ethers in which one of the aryl groups is a phenyl fused to a cycloalkyl or heterocyclic ring, to which is attached an acetic acid group, are agonists of G-protein coupled receptor 40...
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8034806 |
Bicyclic mGluR5 positive allosteric modulators and methods of making and using same
In one aspect, the invention relates to bicyclic MGluR5 positive allosteric modulators, for example 6-(phenylethynyl)-3,4-dihydroisoquinolin-1(2H)-one, derivatives thereof, and related compounds,...
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8017625 |
Nitrogen-containing heteroaryl compounds and methods of use thereof
The present invention relates to compounds suitable for use in mediating hypoxia inducible factor and for treating erythropoietin-associated conditions by increasing endogenous erythropoietin in...
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8012979 |
Compounds and their uses 707
The present invention relates to isoquinolinone derivatives of formula (I): wherein R1, R2, R3, R4, R5, R6 and R7 are as herein defined; processes for their preparation, pharmaceutical compositions...
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7989471 |
Macrocyclic inhibitors of hepatitis C virus
Inhibitors of HCV of formula (I) and the N-oxides, salts, and stereochemically isomeric forms thereof, wherein the terms R1, L, R2, R3, R4, and n have specific definitions; pharmaceutical...
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7968511 |
Combination therapy with glatiramer acetate and mitoxantrone for the treatment of multiple sclerosis
The subject invention provides a method of treating a subject afflicted with a form of multiple sclerosis comprising periodically administering to the subject an amount of glatiramer acetate and an...
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7964613 |
Sulfonamide compound
A compound represented by the formula (1) [A represents a nitrogen-containing saturated ring; m represents an integer of 0 to 2; n represents an integer of 1 to 4; G1 represents hydrogen atom,...
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7932266 |
Isoquinoline derivatives as calpain inhibitors
The invention relates to derivative compounds of partially-reduced isoquinoline with substitution of a sec-butyl group at position 3 with calpain inhibitor activity. The inventive compound...
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7919508 |
3-piperidinylisochroman-5-ols as dopamine agonists
The present invention provides compounds of formula I: a stereoisomer or a pharmaceutically acceptable salt thereof, wherein the variables R1, R2, R3, R4, X and n are defined as defined herein....
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7906504 |
2-(1-oxo-1H-isoquinolin-2-yl)acetamide derivatives
Disclosed herein are 2-(1-oxo-1H-isoquinolin-2-yl)acetamide derivative of formula I, or pharmaceutically acceptable salts or solvates thereof wherein each of the substituents is given the...
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7902223 |
Phenyl derivatives as factor XA inhibitors
Novel compounds of the formula (I), in which D, W, X, Y, T and R1 are as defined in Patent Claim 1, are inhibitors of coagulation factor Xa and can be employed for the prophylaxis and/or therapy of...
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7897618 |
N-aroyl cyclic amine derivatives as orexin receptor antagonists
Disclosed are N-aroyl cyclic amine derivatives having the formula: where the variables are as define herein, and their use as pharmaceuticals, specifically as orexin receptor antagonists.
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7893088 |
6-substituted isoquinoline derivatives
The present invention relates to 6-substituted isoquinoline derivatives having the general Formula I wherein X is O, S or NH; Y is OH or NH2; m is 0, 1 or 2; n is 0 or 1; o is 0 or 1; R1 is H, when...
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7879891 |
Caspase inhibitor prodrugs
This invention relates to prodrugs of caspase inhibitors comprising of a furo[3,2-d]oxazolin-5-one moiety which, under specific conditions, can convert into biologically active compounds,...
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7879876 |
Sulfonamide derivatives and use thereof for the modulation of metalloproteinases
The present invention is related to sulfonamide derivatives of Formula (Ia) where the groups are as defined in the description, and use thereof in particular for the treatment and/or prophylaxis of...
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7858619 |
Substituted tetrahydroisochinolines as MMP inhibitors, related production method and use as medicine
The present invention is directed to a compound of formula (I), wherein R1, R2, R3, R4, A, L and n are as defined herein, its pharmaceutical composition, preparation and uses as a MMP inhibitor.
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7851485 |
Therapeutic agent for neuropathic pain
Disclosed is a therapeutic agent for neuropathic pain having an excellent therapeutic effect on neuropathic pain which is a intractable disease. More specifically, disclosed are a therapeutic agent...
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7842703 |
Substituted benzofused derivatives and their use as vanilloid receptor ligands
The present invention relates to substituted benzofused derivatives, which can be used as vanilloid receptor ligands, method of treating diseases, conditions and/or disorders modulated by vanilloid...
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7820693 |
1-(2H)-isoquinolone derivative
The present invention provides a compound having high antitumor activity, which is useful for therapeutic and preventive agents effective for proliferative diseases such as cancer; a production...
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7816371 |
Bicycloheteroaryl compounds as P2X7 modulators and uses thereof
Bicycloheteroaryl compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and...
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7795278 |
Substituted tetrahydro-2H-isoquinolin-1-one derivatives, and methods for the production and use thereof
This invention relates to compounds according to the general formula (I), where the definitions of the substituents R1, R2, Ar and X are as specified in the description, and to their...
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7786115 |
Amide derivatives
The invention concerns a compound of the Formula I wherein m is 0-2 and each R1 is a group such as hydroxy, halogeno, trifluoromethyl heterocyclyl and heterocyclyloxy; R2 is halogeno,...
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7781457 |
Isoquinolinone potassium channel inhibitors
The present invention relates to compounds having the structure formula (I) useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like.
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7763614 |
Isoquinoline potassium channel inhibitors
The present invention relates to compounds of structural formula I: I useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like.
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7745461 |
Method of treating dry eye disorders
The topical use of EgLN-3 inhibitors is disclosed for the treatment of dry eye.
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7741322 |
Isoquinolinone potassium channel inhibitors
The present invention relates to compounds having the structure (I) useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like.
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7737147 |
Methods and compositions to enhance the efficacy of phosphodiesterase inhibitors
Methods for treatment of sexual dysfunction in men and women using combinations of phosphodiesterase (PDE) type 5 inhibitors and l-deprenyl or propargylamine compounds are described. Methods of...
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7713994 |
Substituted isoquinoline-1,3(2H,4H)-diones, 1-thioxo,1,4-dihydro-2H-isoquinoline-3-ones and 1,4-dihyro-3 (2H)-isoquinolones and methods of use thereof
This invention provides compounds of Formula (I), having the structure where G1, G2, G3, G4, A1, A2, Y1, Y2, L1, Z, e and f are defined herein, or a pharmaceutically acceptable salt thereof, which...
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7709476 |
Isoquinolinone potassium channel inhibitors
The present invention relates to compounds having the structure (I) useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like.
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7705017 |
Compounds for treatment of neurodegenerative diseases
The present invention relates to a class of small molecule hydroxamic acid compounds capable of inhibiting histone deacetylases (HDACs). The present invention also relates to methods of preparation...
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7700604 |
Hydantoin derivatives as metalloproteinase inhibitors
The invention provides compounds of formula (I): wherein R1, R2, A, A1 and B are as defined in the specification; processes for their preparation; pharmaceutical compositions containing them; a...
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7691879 |
Isoquinoline potassium channel inhibitors
The present invention relates to compounds having the structure (I) useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like.
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