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8178531 |
Antiviral agents
The present invention relates to antiviral compounds of formula (I), compositions containing these compounds, processes for their preparation, intermediates in their synthesis, and their use as...
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8148367 |
Renin inhibitors
Disclosed are compounds, pharmaceutical compositions, kits, articles of manufacture, methods of using, and methods of preparing compounds having the formula: wherein the variables are as defined...
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8129389 |
Substituted oxindole derivatives, medicaments containing the latter and use thereof
The invention relates to novel oxindole derivatives of general formula (I), in which the substituents A, B, R1, R2 and R3 are defined as cited in claim 1, to medicaments containing said derivatives...
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8114871 |
3-amido-pyrrolo[3,4-C]pyrazole-5(1H,4H,6H) carbaldehyde derivatives
The present invention relates to compounds and pharmaceutically acceptable salts of Formula (I): wherein X, R1, R2, R3, R4, R5, R6, R7, and R8 are as defined above. The invention further relates to...
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8101618 |
1,4-substituted piperazine derivatives
A compound represented by the formula (I): or a pharmaceutically acceptable salt thereof, wherein: R1 represents a branched lower alkyl group having from 3 to 9 carbon atoms or the like;R2...
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8093250 |
2-aminocarbonyl-pyridine derivatives
The present invention relates to 2-aminocarbonyl-pyridine derivatives of Formula (I) and their use as P2Y12 receptor antagonists in the treatment and/or prevention of peripheral vascular, of...
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8063052 |
Wound healing
The present invention relates to the use of p38 MAP kinase inhibitors and p38 MAP kinase inhibition to promote wound healing.
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8058269 |
Oxindole derivatives
There is provided compounds of the formula wherein R6, V, W, X, Y, Q and n are as described. The compounds exhibit activity as anticancer agents.
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8053436 |
9-(piperazinylalkyl) carbazoles as bax-modulators
The present invention is related to piperazine derivatives of carbazole of formula (I) notably for use as pharmaceutically active compounds, as well as to pharmaceutical formulations containing...
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8044079 |
Substituted oxindole derivatives, medicaments containing said derivatives and use thereof
The invention relates to novel oxindole derivative of general formula (I), wherein the substituents R1, R2, A, B, and Y are defined as in Claim 1. The invention further relates to medicaments...
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8017616 |
Heterocyclic substituted pyridine compounds with CXCR3 antagonist activity
The present application discloses a compound, or enantiomers, stereoisomers, rotamers, tautomers, racemates or prodrug of said compound, or pharmaceutically acceptable salts, solvates or esters of...
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8012969 |
11C-labeled benzyl-lactam compounds and their use as imaging agents
The invention relates to “C-labeled compounds, their preparation, compositions comprising an effective amount of a “C-labeled compound, and the use of a “C-labeled compound as a radio...
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8008299 |
Urotensin II receptor antagonists
This invention is directed to a compound of Formula (I): and forms thereof, wherein A, B, E, G, X and L2 are as defined herein and their use as urotensin II receptor antagonists.
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7998963 |
Arylpiperazine derivatives and uses thereof
Compounds of formula I: or pharmaceutically acceptable salts thereof, wherein Ar is indolyl, indazolyl or dihydroindolyl, and R1, R2, R3 and R4 are as defined herein. Also provided are...
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7994202 |
Bicyclic nitrogen-containing heterocyclic compounds
A nitrogen-containing bicyclic heterocyclic compound represented by the following formula (1) is provided. When the compound or a salt thereof is administered to a human being or an animal, the...
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7964602 |
Biaryl compounds useful as agonists of the Gpr38 receptor
The present invention relates to novel biaryl derivatives such as compounds of formula (I), which have activity as agonists of the GPR38 receptor and the use of such compounds or pharmaceutical...
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7956058 |
Dehydrophenylahistins and analogs thereof and the synthesis of dehydrophenylahistins and analogs thereof
Compounds represented by the following structure (I) are disclosed: as are methods for making such compounds, wherein said methods comprise reacting a diacyldiketopiperazine with a first aldehyde...
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7951807 |
Substituted oxindol derivatives and medicaments containing the same
The present invention relates to novel oxindole derivatives of the general formula (I), wherein the substituents A, B, R1, R2 and R3 are as defined in Claim 1, and medicaments containing the same...
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7943605 |
Compounds comprising a lactam or a lactam derivative moiety, processes for making them, and their uses
The present invention relates to compounds of formula (I) comprising a lactam or a lactam derivative moiety, processes for preparing them, pharmaceutical compositions comprising said compounds and...
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7935704 |
Dehydrophenylahistins and analogs thereof and the synthesis of dehydrophenylahistins and analogs thereof
Compounds represented by the following structure (I) are disclosed: as are methods for making such compounds, wherein said methods comprise reacting a diacyldiketopiperazine with a first aldehyde...
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7932250 |
Thienopyrazole derivative having PDE7 inhibitory activity
To provide thienopyrazole derivatives inhibiting PDE 7 selectively, and therefore, enhance cellular cAMP level. Consequently, the compound is useful for treating various kinds of disease such as...
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7919489 |
Heterocyclyamide-substituted imidazoles
The invention relates to heterocyclylamide-substituted imidazoles and methods for their preparation, their use for the treatment and/or prophylaxis of diseases as well as their use for the...
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7915260 |
Urotensin II receptor antagonists
The invention is directed to Urotensin II antagonists. More specifically, the present invention relates to certain novel compounds, methods for preparing compounds, compositions, intermediates and...
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7910591 |
Piperazine derivatives of alkyl oxindoles
The present invention is concerned with new indol-2-one derivatives of Formula (I), which have favorable activity profile for the prophylaxis and treatment of disorders in the central nervous or in...
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7910588 |
5-HT7 receptor antagonists
The present invention provides selective 5-HT7 receptor antagonist compounds of Formula I and their use in the treatment of migraine: where A is —C(H)═ or —N═ and R1-7 are as defined herein.
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7897603 |
Selected CGRP-antagonists, processes for preparing them and their use as pharmaceutical compositions
The present invention relates to the CGRP-antagonists of general formula I wherein R1, R2, R3 and R4 are defined as in claim 1, the tautomers, the isomers, the diastereomers, the enantiomers, the...
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7893049 |
Thiazolyl-dihydro-indazole
The present invention encompasses compounds of general formula (1) wherein R1 to R6 are defined as in claim 1, which are suitable for the treatment of diseases characterized by excessive or...
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7884106 |
Method of stabilizing lipid-rich plaque and method of preventing rupture thereof
A method of stabilizing lipid-rich plaques and method of preventing the rupture thereof, characterized in that an effective amount of...
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7846933 |
4-imidazolin-2-one compounds
The present invention relates to a compound of the formula [I]: wherein G1 is an alkyl which is substituted by a halogen atom or an alkoxy, or a group of the formula: wherein ring B is benzene ring...
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7842693 |
Substituted piperazines
Compounds are provided that act as potent antagonists of the CCR1 receptor, and which have been further confirmed in animal testing for inflammation, one of the hallmark disease states for CCR1....
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7834016 |
Inhibitors of the interaction between MDM2 and p53
The present invention provides compounds of formula (I), their use as an inhibitor of a p53-MDM2 interaction as well as pharmaceutical compositions comprising said compounds of formula (I) wherein...
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7820672 |
Indolylmaleimide derivatives
The compounds are indolylmaleimide derivatives comprising either a substituted pyridyl or indolyl residue. The compounds have interesting pharmaceutical properties, e.g. in the treatment and/or...
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7816360 |
MTP inhibiting aryl piperidines or piperazines substituted with 5-membered heterocycles
The present invention is concerned with novel aryl piperidine or piperazine compounds substituted with certain 5-membered heterocycles having apoB secretion/MTP inhibiting activity and concomitant...
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7816361 |
Immuno inhibitory pyrazolone compounds
Compounds of formula (IA) or (IB) are inhibitors of CD80 and useful in immunomodulation therapy: wherein Ar represents an optionally substituted monocyclic or bicyclic aromatic or heteroaromatic...
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7812021 |
Pyrrolidine aryl-ether as NK3 receptor antagonists
The invention relates to a compound of general formula wherein Ar, R1, R2, R3, R4, n, o, p, s, X and are as defined herein or to a pharmaceutically active salt thereof, including all stereoisomeric...
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7807672 |
Compounds that are ERK inhibitors
Disclosed are the ERK inhibitors of formula 1.0: and the pharmaceutically acceptable salts and solvates thereof. Q is a piperidine or piperazine ring that can have a bridge or a fused ring. The...
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7795261 |
Substituted 1-piperidin-4-yl-4-pyrrolidin-3-yl-piperazine derivatives and their use as neurokinin antagonists
This invention concerns substituted I-piperidin-4-yl-4-pyrrolidin-3-yl-piperazine derivatives having neurokinin antagonistic activity, in particular NK1 antagonistic activity, a combined NK1/NK3...
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7786129 |
Piperazine derivatives of dialkyl oxindoles
The present invention is concerned with new 3,3-disubstituted indol-2-one derivatives of the general Formula (I), wherein R1 stands for hydrogen, halogen, alkyl having 1-7 carbon atom(s) or...
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7786124 |
Heterocyclic substituted pyridine compounds with CXCR3 antagonist activity
The present application discloses a compound, or enantiomers, stereoisomers, rotamers, tautomers, racemates or prodrug of said compound, or pharmaceutically acceptable salts, solvates or esters of...
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7776862 |
Pyridyl and phenyl substituted piperazine-piperidines with CXCR3 antagonist activity
The present application discloses a compound, or enantiomers, stereoisomers, rotamers, tautomers, racemates or prodrug of said compound, or pharmaceutically acceptable salts, solvates or esters of...
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7767674 |
Kinase inhibitors
The present invention provides kinase inhibitors of Formula I:
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7763616 |
Piperazine-piperidines with CXCR3 antagonist activity
The present application discloses a compound, or enantiomers, stereoisomers, rotamers, tautomers, racemates or prodrug of said compound, or pharmaceutically acceptable salts, solvates or esters of...
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7754750 |
Metalloproteinase inhibitors
Compounds of the formula (I) wherein z is SO2 or SO, useful as metalloproteinase inhibitors, especially as inhibitors of MMP12.
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7754723 |
Therapeutic agents useful for treating pain
Compounds of formulae: where Ar1, Ar2, R3, R4, and m are disclosed herein, or a pharmaceutically acceptable salt thereof (a “Nitro(cyano)vinylpiperazine Compound”); compositions comprising an eff...
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7754721 |
Arylpiperazine derivatives and uses thereof
Compounds of the formula: or pharmaceutically acceptable salts thereof, wherein m, n, X, Y, Z, Ar, R1, R2, R3, R4, R5, R6 and R7 are defined herein. Also provided are pharmaceutical compositions,...
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7704997 |
Amino-tetrazole analogues and methods of use
A compound having Formula (I) or Formula (II) is disclosed as an P2X7 antagonist, wherein A, B, C, Y, Y, Z, m, v, R1, R2, R3, R4, and R5, are as defined in the description. Methods and compositions...
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7700598 |
Selected CGRP-antagonists, process for preparing them and their use as pharmaceutical compositions
The present invention relates to the CGRP antagonists of general formula wherein A, X, D, E, G, M, Q and R1 to R3 are defined as in claim 1, the tautomers, the isomers, the diastereomers, the...
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7696209 |
CGRP-antagonists, process for preparing them and their use as pharmaceutical compositions
The present invention relates to the CGRP-antagonists of general formula I wherein R1, R2, R3, R4 and X are defined as in claim 1, the tautomers, the isomers, the diastereomers, the enantiomers,...
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7683067 |
3-heterocyclyl-indole derivatives as inhibitors of glycogen synthase kinase-3 (GSK-3)
Compounds of formula Ia or Ib wherein P; R1; R2; m; and n are as defined in the application, salts thereof, processed for their preparation, new intermediates used therein, pharmaceutical...
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7671056 |
Piperazine-piperidine antagonists and agonists of the 5-HT1A receptor
The present invention relates to novel piperazine-piperidine compounds. The compounds are useful as 5-HT1A binding agents, particularly as 5-HT1A receptor antagonists and agonists. These compounds...
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