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7612201 |
Pyrazole compounds
Compounds of formula (IA) or (IB) or a salt, N-oxide, hydrate or solvate thereof are inhibitors of HSP90, and are of value in the treatment of diseases responsive to HSP90 inhibition such as...
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7612069 |
Acyl guanidines as beta-secretase inhibitors
There is provided a series of substituted acyl guanidines of Formula (I)
or a stereoisomer; or a pharmaceutically acceptable salt thereof, wherein R 1 , R 2 , R 3 , R 4 and R 5 as defined...
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7605272 |
IGF-1R inhibitor
The present invention provides a type I insulin-like growth factor receptor (IGF-1R) inhibitor comprising, as an active ingredient, an indazole derivative represented by Formula (I):
{wherein R...
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7592338 |
Pyrazole-amine compounds useful as kinase inhibitors
The present invention provides pyrazole derived compounds of formula (I)
useful for treating p38 kinase-associated conditions, where W, X, R 1 , R 2 , R 3 , R 4 , R 5 , R 6 and m are as...
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7582628 |
Pyrrolo[3,4-c]pyrazole derivatives active as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them
Pyrrolo[3,4-c]pyrazole 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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7566709 |
1,3,4-Substituted pyrazoles as 5-HT receptor antagonists for the treatment of psychoses and neurological disorders
Compounds of the formula (I) and salts and solvates thereof, in which X, R 1 , R 2 , R 5 and Q have the meanings indicated in Claim 1 , are suitable as ligands of 5 HT receptors; as well as...
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7557102 |
Pyrazolidine-1,2-dicarboxyldiphenylamide derivatives as coagulation factor Xa inhibitors for the treatment of thromboses
Novel compounds of the formula (I), in which R, R 1 , R 2 and R 3 have the meanings indicated in Patent Claim 1 , are inhibitors of coagulation factor Xa and can be employed for the prophylaxis...
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7521447 |
P38 inhibitors and methods of use thereof
This invention relates to inhibitors of p38, and methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and...
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7517902 |
Substituted indazoles, compositions containing the same, and the preparation and use thereof
Disclosed are novel substituted indazole compounds, pharmaceutical compositions comprising such compounds, and methods of treatment comprising such compounds.
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7511136 |
Aminoindazole derivatives active as kinase inhibitors
Compounds which are 3-aminoindazole derivatives or pharmaceutically acceptable salts thereof, together with pharmaceutical compositions comprising them are disclosed; these compounds or...
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7482342 |
Indazolecarboxamide derivatives, preparation and use thereof as CDK1, CDK2 and CDK4 inhibitors
Compound corresponding to general formula (I):
in which, R 1 represents a hydrogen or halogen atom, an NH 2 , NHR 2 , NHCOR 2 , NO 2 , CN, CH 2 NH 2 and CH 2 NHR 2 ; or alternatively R 1 ...
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7452997 |
Tetrahydro-indazole cannabinoid modulators
This invention is directed to a tetrahydro-indazole cannabinoid modulator compound of formula I:
and a method for use in treating, ameliorating or preventing a cannabinoid receptor mediated...
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7452873 |
Inhibitors of GSK-3 and uses thereof
The present invention relates to compounds of formula I that are useful as GSK-3 inhibitors. The invention also relates to methods of using compounds of formula I or pharmaceutical compositions...
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7425572 |
Use of dioxindoindazoles and dioxoloindazoles for treating glaucoma
Novel dioxinoindazole compounds and dioxoloindazole compounds are disclosed. Also disclosed are methods for the lowering and controlling of normal or elevated intraocular pressure as well as a...
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7348427 |
Antipathogenic benzamide compounds
Antipathogenic benzamide compounds having the formula
wherein at least one of the R 1 groups is F, Cl, CN or CF 3 and R 2 , R 3 , Y, Z, m, and n are as defined herein.
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7304060 |
Indazolyl-substituted pyrroline compounds as kinase inhibitors
The present invention is directed to novel indazolyl-substituted pyrroline compounds of Formula (I):
useful as kinase or dual-kinase inhibitors, methods for producing such compounds and methods...
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7282499 |
Sigma receptor inhibitors
The invention relates to compounds having pharmacological activity towards the sigma receptor, and more particularly to some pyrazole derivatives, to processes of preparation of such compounds, to...
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7282498 |
Substituted fused pyrroleoximes and fused pyrazoleoximes
Disclosed are compounds of the formula
and the pharmaceutically acceptable salts thereof wherein R, Ar, A, n, R 1 and R 2 are defined herein. These compounds are highly selective agonists,...
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7279476 |
Pyrazole-derived kinase inhibitors and uses thereof
Described herein are compounds that are useful as protein kinase inhibitors having the formula:
where B, R 1 , n, R 3 , Q, and R 4 are described in the specification. The compounds are useful...
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7247628 |
Cannabinoid receptor ligands and uses thereof
Compounds of Formula (I) that act as cannabinoid receptor ligands and their uses in the treatment diseases, conditions and/or disorders herein.
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7189679 |
Herbicidal 3-amino-2-thiomethylbenzoylpyrazoles
3-Amino-2-thiomethylbenzoylpyrazoles of the formula (I) and their use as herbicides are described.
In this formula (I) R 1 to R 9 are various radicals.
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7179804 |
Tachykinin receptor antagonists
The present invention relates to selective NK-1 receptor antagonists of Formula (I); or a pharmaceutically acceptable salt thereof, for the treatment of disorders associated with an excess of...
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7144911 |
Anti-inflammatory medicaments
Novel compounds and methods of using those compounds for the treatment of inflammatory conditions are provided. In a preferred embodiment, modulation of the activation state of p38 kinase protein...
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7141568 |
Pyrrolo[3,4-c]pyrazole derivatives active as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them
Pyrrolo[3,4-c]pyrazole 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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7091340 |
Polymorphs
Disclosed are polymorphs of 1-(5-tert-butyl-2-p-tolyl-2H-pyrazol-3-yl)-3-[4-(2-morpholin
-4-yl-ethoxy)-naphthalen-1-yl]-urea and processes from making the same.
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7067656 |
Sulfamoyl compounds and agricultural and horticultural fungicides
A sulfamoyl compound of the general formulae (1):
wherein
R 1 and R 2 are each independently C 1-4 alkyl, or R 1 and R 2 together are C 4-6 alkylene or C 4-6 alkyleneoxy, Y is H,...
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7064123 |
Compounds and compositions as cathepsin inhibitors
The present invention relates to novel selective cathepsin S inhibitors, the pharmaceutically acceptable salts and N-oxides thereof, their uses as therapeutic agents and the methods of their making.
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7041669 |
1,4-benzofused urea compounds useful in treating cytokine mediated diseases
Disclosed are 1,4-disubstituted benzo-fused urea compounds of formula (I):
wherein Ar, X, A, L, and Q of formula(I) are defined herein. The compounds inhibit production of cytokines involved in...
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7034049 |
3(5)-amino-pyrazole derivatives, process for their preparation and their use as antitumor agents
Compounds which are 3-amino-pyrazole derivatives represented by formula (I) wherein R is C 3 –C 6 cycloalkyl group optionally substituted by a straight or branched C 1 –C 6 alkyl or arylalkyl...
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6979685 |
Cycloalkyl amine compounds and uses thereof
Aminocycloalkyl compounds are disclosed. The compounds of the present invention may be incorporated in compositions and kits. The present invention also discloses a variety of in vitro and in vivo...
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6974810 |
4,5-Dihydro-1H-pyrazole derivatives having potent CB1-antagonistic activity
The present invention relates to a group of novel 4,5-dihydro-1H-pyrazole derivatives which are potent cannabinoid (CB 1 ) receptor antagonists with utility for the treatment of diseases connected...
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6956036 |
6-hydroxy-indazole derivatives for treating glaucoma
Substituted 1-(α-alkyl-ethylamino)-1H-indazol-6-ols useful for lowering and controlling IOP and treating glaucoma are disclosed
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6949579 |
Aminoindazole derivatives and intermediates, preparation thereof, and pharmaceutical compositions thereof
The present invention relates to the novel indazole derivatives of general formula (I):
in which: R is either O, S or NH; R3 is an alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, aryl,...
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6916924 |
Process for synthesis of heteroaryl-substituted urea compounds useful as antiinflammatory agents
This invention relates to novel processes for preparing heteroaryl-substituted urea compounds of formula (I):
which are useful for treating diseases and pathological conditions involving...
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6894173 |
Intermediates useful for synthesis of heteroaryl-substituted urea compounds, and processes of making same
Disclosed are novel processes and novel intermediate compounds for preparing aryl-and heteroaryl-substituted urea compounds of the formula(I) wherein Ar 1 , Ar 2 , L, Q and X are described herein....
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6852717 |
Compounds useful as anti-inflammatory agents
Disclosed are compounds useful in pharmaceutic compositions for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases. Also disclosed are...
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6753426 |
Polymorph and process for preparing same
Disclosed are processes, polymorph and intermediate compounds for preparing aryl-and heteroaryl-substituted urea compounds of the formula(I) wherein Ar 1 , Ar 2 , L, Q and X are described herein....
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6753329 |
Inhibitors of cyclin-dependent kinases, compositions and uses related thereto
The invention pertains to novel cyclin dependent kinase inhibitors (cdks) and specifically, but not exclusively, as inhibitors of cdk/cyclin complexes. As described herein, the inhibitors of this...
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6730671 |
Compounds useful as reversible inhibitors of cathespin S
Disclosed are cathepsin S reversible inhibitory compounds of the formulas (I),(Ia) and (II),(IIa) as defined herein. The compounds are useful for treating autoimmune diseases. Also disclosed are...
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6727246 |
1-(aminoalkyl)-3-sulfonylindole-and-indazole derivatives as 5-hydroxytryptamine-6 ligands
The present invention provides compounds of formula I and the use thereof for the treatment of central nervous system disorders related to or affected by the 5-HT6 receptor.
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6720317 |
Inhibitors of factor Xa
Novel compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds are useful in vitro or in vivo for preventing or treating...
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6716841 |
Nitrogen containing heterobicycles as factor Xa inhibitors
This invention relates generally to nitrogen containing heterobicycles of formulas A and B: which are inhibitors of trypsin-like serine protease enzymes, especially factor Xa, pharmaceutical...
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6716837 |
Heterocyclic compounds for the treatment of migraine
Described herein are compounds useful in the treatment of migraine, which have the general formula: wherein: W is a CH group or a N atom; Z is N or C—R4; B and D are selected independently...
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6706711 |
Pyrazole derived kinase inhibitor
Described herein are compounds that are useful as protein kinase inhibitors having the formula: wherein R 1 , R 2 , T, n and Q are as described in the specification. The compounds are useful for...
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6673923 |
Pyrazole antimicrobial agents
The present invention provides pyrazole and pyrazolone derivatives. Preferred compounds of the invention are useful as RNA polymerase inhibitors. Further preferred compounds of the invention are...
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6660732 |
Compounds useful as anti-inflammatory agents
Disclosed are novel aromatic compounds which are useful for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases. Also disclosed are...
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6656933 |
Compounds useful as anti-inflammatory agents
Disclosed are novel aromatic compounds which are useful for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases. Also disclosed are...
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RE38330 |
Preventing and reversing advanced glycosylation endproducts
The present invention relates to compositions and methods for inhibiting and reversing nonenzymatic cross-linking (protein aging). Accordingly, a composition is disclosed which comprises a...
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6642234 |
Acrylonitrile compounds
The present invention relates to acrylonitrile compounds of formula (1): [wherein, R is a C 1 -C 6 alkyl, a C 3 -C 7 cycloalkyl optionally substituted by a C 1 -C 4 alkyl, a naphthyl, etc., R...
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6638930 |
Morpholine and thiomorpholine tachykinin receptor antagonists
Substituted heterocycles of the general structural formula: are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, asthma and emesis, and calcium...
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