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8173679 |
Indazoles, benzisoxazoles and benzisothiazoles and their use as estrogenic agents
The present invention relates to compounds of formula (I): in which R1, R2, R3, X, Y and A are as defined in the specification. The compounds are modulators of the estrogen receptors.
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8163774 |
Amide-substituted 8-N-benzimidazoles, method for the production thereof, and use of the same as medicaments
The present invention comprises the use of amino-substituted 8-N-benzimidazoles compounds of formula I wherein R3, R4-R5, R11 and R20-R21 are hereinafter defined which display a therapeutically...
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8153658 |
Piperidine derivative or salt thereof
To provide a compound which can be used for treating diseases in which a calcium sensing receptor (CaSR) participates, particularly hyperparathyroidism. It was found that a novel piperidine...
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8148363 |
Heterocyclic compounds as factor IXA inhibitors
The present invention relates to novel heterocyclic compounds of Formulae I-III; as disclosed herein or a pharmaceutically acceptable salt, solvate, ester, prodrug or stereoisomer thereof. Also...
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8143282 |
Heterocyclic compounds
The present invention relates to compounds which are inhibitors of histone deacetylase. More particularly, the present invention relates to heterocyclic compounds and methods for their preparation....
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8138207 |
Aminocarbonyl-substituted 8-N-benzimidazoles, methods for their preparation and their use in pharmaceutical compositions
The present invention comprises the use of amino-carbonyl-substituted 8-N-benzimidazoles compounds of formula I wherein R3, R4-R5, R11 and R20-R21 are hereinafter defined which display a...
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8138168 |
Renin inhibitors
The invention relates to compounds having the formulae: wherein the variables are as defined herein. The invention further relates to methods of making and using these compounds, and pharmaceutical...
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8138177 |
Benzimidazolone derivatives as CB2 receptor ligands
This invention relates to compounds of the formula (I): or pharmaceutically acceptable salts thereof, wherein: A, B, R1, R2 and R3 are each as described herein, and compositions containing such...
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8119661 |
Piperidine derivatives and their use as muscarinic receptor modulators
Compounds of Formula I, or pharmaceutically acceptable salts thereof: wherein R2, R3, X, m and n are as defined in the specification as well as salts and pharmaceutical compositions including the...
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8114899 |
2H- or 3H-benzo[e]indazol-1-yl carbamate derivatives, the preparation and therapeutic use thereof
Compounds corresponding to the formula (I) as defined in the disclosure, as well as methods for making such compounds, intermediates employed in such methods, pharmaceutical compositions containing...
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8114865 |
Indazole derivatives as kinase inhibitors for the treatment of cancer
Substituted indazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, process for their preparation and pharmaceutical compositions...
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8110578 |
Pyrazino[2,3-b]pyrazine mTOR kinase inhibitors for oncology indications and diseases associated with the mTOR/PI3K/Akt pathway
Provided herein are Heteroaryl Compounds having the following structure: wherein R1-R4 are as defined herein, compositions comprising an effective amount of a Heteroaryl Compound and methods for...
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8106191 |
Synthetic multimerizing agents
New compounds are disclosed for multimerizing immunophilins and proteins containing immunophilin or immunophilin-related domains. The compounds are of the formula M-L-Q where M is a synthetic...
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8071622 |
Indoles
The present invention is concerned with novel indol-2-yl-carbonyl-piperidin-benzoimidazolon and indol-2-yl-carbonyl-piperidin-benzoxazolon derivatives as V1a receptor antagonists, their...
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8071623 |
Amide substituted indazoles as poly(ADP-ribose)polymerase(PARP) inhibitors
The present invention relates to compounds of formula I: and pharmaceutically acceptable salts, stereoisomers or tautomers thereof which are inhibitors of poly (ADP-ribose) polymerase (PARP) and...
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8071779 |
Cytoskeletal active rho kinase inhibitor compounds, composition and use
The present invention is directed to synthetic cytoskeletal active compounds that are inhibitors of rho-associated protein kinase. The present invention is also directed to pharmaceutical...
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8067603 |
Benzimidazolone and quinazolinone derivatives as agonists on human ORL1 receptors
The invention relates to a group of novel benzimidazolone and quinazolinone derivatives which are agonists on human ORL1 (nociceptin) receptors. The invention also relates to the preparation of...
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8067613 |
Benzimidazole poly(ADP ribose)polymerase inhibitors
Compounds which inhibit the activity of poly(ADP-ribose)polymerase (PARP), compositions containing the compounds and methods of treating diseases using them are disclosed.
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8053431 |
Pharmaceutical use of substituted amides
The use of substituted amides for modulating the activity of 11-hydroxysteroid dehydrogenase type 1 (11HSD1) and the use of these compounds as pharmaceutical compositions, are described. Also a...
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8044213 |
Thiazolyl-benzimidazoles
The invention is directed to compounds of formula (1) and pharmaceutically acceptable salts thereof, methods for the preparation thereof, and methods of use thereof.
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8030314 |
Use of 2h-benzimidazol-2-one, 1,3-dihydro-1-(2{4-[3-(trifluoromethyl)phenyl]-1-piperazinyl}ethyl)-and its physiologically acceptable acid addition salts
Use of 2H-benzimidazol-2-one, 1,3-dihydro-1-(2{4-[-(trifluoromethyl)phenyl]-1-piperazinyl}
ethyl)- or a physiologically acceptable acid addition salt thereof, for the manufacture of a medicament...
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8026257 |
Substituted heterocyclic ethers and their use in CNS disorders
The invention encompasses compounds of Formula I, including pharmaceutically acceptable salts, their pharmaceutical compositions, and their use in treating CNS disorders.
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8026233 |
P38 inhibitors and methods of use thereof
Compounds of formula (I): in which A, B, X, Ar1, R8 and R4 have any of the meanings given in the specification, are inhibitors of p38 useful in the treatment and prevention of various disorders...
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8022059 |
Indazole acrylic acid amide compound
A compound of the formula: wherein ring X is benzene or pyridine; R1 is substituted alkyl; R2 is optionally substituted aryl or optionally substituted heterocyclic group; R3 is hydrogen or alkyl;...
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8012997 |
Isoindole-imide compounds, compositions, and uses thereof
The invention relates to isoindole-imide compounds and pharmaceutically acceptable salts, hydrates, solvates, clathrates, enantiomers, diastereomers, racemates, or mixtures of stereoisomers...
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8012995 |
Pharmaceutically active sulfonamide derivatives
The present invention is related to sulfonamide derivatives of formula (I0 notably for use as pharmaceutically active compounds, as well as to pharmaceutical formulations containing such...
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8012974 |
Pyrrolopyrazinyl urea kinase inhibitors
The present invention relates to the use of novel pyrrolopyrazinyl urea derivatives of Formula I, wherein the variables R1, R2, R3, R4, and R5 are defined as described herein, which inhibit JAK and...
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8008326 |
4-benzyledene-piperidin derivatives
The present invention relates to new 4-benzylidene-piperidin derivatives of formula (I), useful as NMDA, in a particular NR2B subunit containing receptor antagonists and analgesica.
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8008481 |
Indazole compounds
Novel compounds of Formula (I) or pharmaceutically acceptable salts, prodrugs and biologically active metabolites thereof of Formula (I) wherein the substituents are as defined herein, which are...
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8003668 |
Amino-substituted 8-N-benzimidazoles and methods for their use in blood sugar disorders
The present invention comprises the use of amino-substituted 8-N-benzimidazoles compounds of formula I wherein R3, R4-R5, R11 and R20-R21 are hereinafter defined which display a therapeutically...
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8003669 |
Remedy for sleep disturbance
The present invention has been made based on the finding that a compound acting on the ORL-1 receptor as an agonist acts as a non-photic entrainment factor, and advances the circadian rhythm phase,...
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8003806 |
Integrin antagonists useful as anticancer agents
The invention relates to compounds of the Formula 1 and to pharmaceutically acceptable salts and solvates thereof, wherein A, X2, X4, X5 and X1 are as defined herein. The invention also relates to...
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7994196 |
Indazole compound and pharmaceutical use thereof
The present invention can provide a cancer treatment drug containing, as an active ingredient, a substance selected from the group consisting of an indazole compound of the following formula (I), a...
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7994325 |
CGRP receptor antagonists
Compounds of Formula I: (where variables R1, A, B, W, X, Y and Z are as defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the...
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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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7985755 |
2,4-diaminoquinazolines for spinal muscular atrophy
2,4-Diaminoquinazolines of formula (I) are provided herein and are useful for treating spinal muscular atrophy (SMA).
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7956069 |
Compounds
Compounds of Formulae I, or pharmaceutically acceptable salts thereof: wherein A1, A2, G1, G2 G3, R1, R2, X, Y, Z, m, n and p are as defined in the specification as well as salts and pharmaceutical...
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7943774 |
Heterocyclyl-substituted thiazoles as crop protection agents
Heterocyclyl-substituted thiazoles of the formula (I), in which the symbols have the meanings given in the description, and also to the agrochemically active salts thereof, and their use for...
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7939520 |
Aminoazacyclyl-3-sulfonylindazoles as 5-hydroxytryptamine-6 ligands
The present invention provides a compound of formula I and the use thereof in the therapeutic treatment of disorders related to or affected by the 5-HT6 receptor.
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7935709 |
2-quinazolinone compounds and methods of use
The present invention comprises a new class of compounds useful for the prophylaxis and treatment of pro-inflammatory cytokine mediated diseases, including inflammation and related conditions. The...
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7935719 |
N-substituted-azacyclylamines as histamine-3 antagonists
The present invention provides a compound of formula I and the use thereof for the treatment of a central nervous system disorder related to or affected by the histamine-3 receptor: wherein the...
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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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7928129 |
Nanomolar β-lactamase inhibitors
New carboxyphenyl-glycylboronic acid transition-state analog inhibitors, representative of a class of compounds effective against class C β-lactamase AmpC. The new compounds improve inhibition by ...
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7928105 |
Substituted 6a,7,8,9-tetrahydropyrido[3,2-e]pyrrolo[1,2-a]pyrazin-6(5H)-ones
Disclosed are compounds of the following formula: in which R1, R2, R5, R6, R7, R31, u, and X are defined in the specification. Also disclosed are pharmaceutical compositions, kits, and articles of...
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7919510 |
Substituted benzimidazole compounds with dual NOS inhibitory activity and mu opioid agonist activity
The present invention relates to benzimidazole compounds having dual nitric oxide synthase (NOS) inhibitory activity and agonist activity at the mu-opioid receptor, to pharmaceutical and diagnostic...
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7906655 |
Hepatitis C virus inhibitors
The present disclosure relates to compounds, compositions and methods for the treatment of Hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such...
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7906532 |
Indazole derivatives
This invention relates to compounds of the formula (I): or pharmaceutically acceptable salts thereof, wherein: R1, R2, R3, A and m are each as described herein and compositions containing such...
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7897634 |
Pyrazoles for the treatment of obesity and other CNS disorders
This invention relates to compounds of the formulas (1), (2) and (3) having pharmacological activity, to compositions containing these compounds, and to methods of treatment employing the compounds...
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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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7879850 |
Organic compounds
The present invention provides compounds of the following structure; A-Q-B—C-D that are useful for treating conditions or disorders associated with DGAT1 activity in animals, particularly humans.
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