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7618969 |
Compounds which potentiate glutamate receptor and uses thereof in medicine
Compounds of formula (I) or a pharmaceutically acceptable salt, solvate or prodrug thereof, are disclosed:
wherein R 1 is C 1-6 alkyl, haloC 1-6 alkyl, C 2-6 alkenyl, amino, monoC 1-4...
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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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7608635 |
Pyrazole compounds that modulate HSP90 activity
Compounds of formula (I), pharmaceutical compositions comprising compounds of formula (I) and methods of inhibiting Hsp90 in a cell, treating or preventing a proliferation disorder in a mammal and...
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7608633 |
Heteroaryl-substituted acetone derivatives as inhibitors of phospholipase A2
The invention relates to novel heteroaryl substituted acetone derivatives which inhibit the enzyme phospholipase A 2 , pharmaceutical preparations containing these compounds and a method of...
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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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7605175 |
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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7605156 |
Methods for the use of inhibitors of cytosolic phospholipase A2
This invention provides methods for the use of substituted indole compounds of the general formula:
and pharmaceutically acceptable salt forms thereof. The invention provides methods for the...
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7604813 |
Wood adhesive comprising an insecticide
A wood glue containing 1-(hetero)arylpyrazole-type active insecticide material and wooden materials bonded with a glue containing said active insecticide material are disclosed.
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7598286 |
[(1H-indazol-3-yl)methyl]phenols and (hydroxyphenyl)(1H-indazol-3-yl)methanones
This invention provides anti-inflammatory agents of formula I, having the structure
wherein A and R 1 -R 10 are as defined in the specification, or a N-oxide thereof or a pharmaceutically...
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7598285 |
Pyrazole derivatives, compositions containing such compounds and methods of use
Pyrazoles having a naphthyl group attached are disclosed. The compounds are useful for treating type 2 diabetes and related conditions. Pharmaceutical compositions and methods of treatment are also...
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7598242 |
Compounds for the treatment of inflammatory disorders
This invention relates to compounds of the Formula (I):
or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions...
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7595343 |
Inhibitors of histone deacetylase
The invention relates to the inhibition of histone deacetylase. The invention provides compounds and methods for inhibiting histone deacetylase enzymatic activity. The invention also provides...
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7595320 |
Hydrazinocarbonyl-thieno[2,3-C]pyrazoles, process for preparing them, compositions containing them and use thereof
The present invention concerns hydrazinocarbonyl-thieno[2,3- c ]pyrazoles of formula (I):
wherein R1, R3, R4, are R5 are as defined in the disclosure; their preparation method, compositions...
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7592363 |
Indazoles
This invention provides compounds of Formula (I) or (Ia):
that are useful in the treatment or inhibition of LXR mediated diseases.
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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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7592337 |
Di-aryl substituted tetrazole modulators of metabotropic glutamate receptor-5
Tetrazole compounds substituted directly, or by a bridge, with i) a heteroaryl moiety containing N adjacent to the point of connection of the heteroaryl and ii) another heteroaryl or aryl ring,...
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7582670 |
Methods of treating an inflammatory-related disease
The invention relates to pharmaceutical compositions and methods of treating inflammatory-related diseases associated with pro-inflammatory cytokine expression and/or reduced expression of...
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7582121 |
Composition for dyeing keratin fibers, comprising at least one diamino-N,N-dihydropyrazolone derivative, at least one coupler, and at least one heterocyclic direct dye
Disclose herein is a composition for dyeing keratin fibers, for example, human keratin fibers such as the hair, comprising at least one oxidation base chosen from diamino-N,N-dihydropyrazolones and...
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7579346 |
Carboxamides
Novel compounds of the formula (I), in which D, W, X, Y, T, m and R 1 have the meaning indicated in Patent claim 1 , are inhibitors of coagulation factor Xa and can be employed for the...
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7576116 |
PDK-1/Akt signaling inhibitors
A new class of phosphoinositide-dependent kinase-1 (PDK-1) inhibitors of formula I:
wherein X is selected from the group consisting of alkyl and haloalkyl; Ar is an aryl radical selected from...
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7576115 |
Heterocyclic compounds and thrombopoietin receptor activators
A compound represented by the formula (1):
wherein A is a nitrogen atom or CR 4 , B is an oxygen atom, a sulfur atom or NR 9 (provided that when A is a nitrogen atom, B is not NH), R 1 is a C...
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7576112 |
Therapeutic N-aryl or N-heteroaryl pyrazolidine and pyrazolidinone derivatives
A compound having a structure
and therapeutic methods, compositions, and medicaments related thereto are disclosed herein.
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7576098 |
Heterocyclic compounds as inhibitors of factor VIIa
The present invention relates generally to compounds that inhibit serine proteases. In particular it is directed to novel heterocyclic compounds, or a stereoisomer or pharmaceutically acceptable...
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7576082 |
Oxindole derivatives
The invention describes compounds of the general formula I
or the pharmaceutically acceptable salts thereof,
wherein R 1 , R 2 , R 3 and X are herein described,
a process for their...
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7572922 |
Substituted pyrazoles, compositions containing such compounds and methods of use
The present invention relates to substituted pyrazoles, compositions containing such compounds and methods of treatment The compounds are glucagon receptor antagonists and thus are useful for...
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7572823 |
Heteroaryl carboxamide compounds
Compounds of formula I
their manufacture, pharmaceutical compositions containing them and their use as medicaments.
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7569592 |
Heteroaryl substituted pyrazole modulators of metabotropic glutamate receptor-5
Pyrazole compounds substituted directly, or by a bridge, with a heteroaryl moiety containing N adjacent to the point of connection of the heteroaryl, are mGluR5 modulators useful in the treatment...
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7566735 |
Compounds which potentiate AMPA receptor and uses thereof in medicine
Compounds of formula (I) and salts are provided:
along with pharmaceutical compositions, uses in medicine, e.g., treating disease or condition mediated by a reduction or imbalance in glutamate...
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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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7557138 |
5-phenoxyalkoxypsoralens and methods for selective inhibition of the voltage gated Kv1.3 potassium channel
Compositions of matter comprising 5-phenoxyalkoxypsoralen compounds and their method of synthesis and use. The compounds are useable to treat diseases or disorders in human or animal subjects,...
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7557114 |
Heterocyclic-substituted phenyl methanones
The present invention relates to compounds of formula I
wherein R 1 and R 2 are defined in the specification and to pharmaceutically acceptable acid addition salts thereof. Compounds of the...
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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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7550498 |
1,2-Diaza-dibenzoazulenes as inhibitors of tumour necrosis factor production and intermediates for the preparation thereof
The present invention relates to derivatives of 1,2-diaza-dibenzoazulene, to their pharmacologically acceptable salts and solvates, to processes and intermediates for the preparation thereof as...
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7547720 |
Ophthalmic compositions for treating ocular hypertension
This invention relates to potent potassium channel blocker compounds of Formula I or a formulation thereof for the treatment of glaucoma and other conditions which leads to elevated intraocular...
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7544707 |
Bicyclic derivatives as PPAR modulators
The present invention is directed to compounds represented by the following structural formula, Formula (I), and stereoisomers, pharmaceutically acceptable salts, solvates and hydrates thereof,...
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7541358 |
1-aryl-or 1-alkylsulfonylbenzazole derivatives as 5-hydroxytryptamine-6 ligands
The present invention provides a compound of formula I and the use thereof for the therapeutic treatment of disorders relating to or affected by the 5-HT6 receptor.
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7538135 |
Benzenesulfonylamino compounds and pharmaceutical compositions containing these compounds
Compounds of the formula
provide pharmacological agents which bind to Peroxisome Proliferator-Activated Receptors (PPARs). Accordingly, the compounds of the instant invention are useful for the...
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7538134 |
Substituted arylpyrazoles
This invention relates to a range of 1-aryl-4-cyclopropylpyrazoles in which the cyclopropyl ring is substituted at the angular position, and pharmaceutically acceptable salts and solvates thereof,...
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7538128 |
Dipeptidyl peptidase IV inhibitors, process for their preparation and compositions containing them
The present invention relates to novel compounds useful as dipeptidyl peptidase IV (DPP-IV) inhibitors of the formula:
wherein X, Y, a, R 1 , and R 2 are as defined herein.
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7534806 |
Method for treating neuropathic pain and associated syndromes
The present invention is directed to the use of ibudilast for treating neuropathic pain.
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7524838 |
Pyrazolyl derivatives, preparation process and intermediates of this process as medicinal products and pharmaceutical compositions containing them
The present invention relates to the novel derivatives of formula (I) in which
A is, if it is present, a (C1-C6) alkyl, a (C3-C6) alkenyl, a (C3-C6) alkynyl, a (C3-C7) cycloalkyl or a (C5-C7)...
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7521471 |
4-cyanopyrazole-3-carboxamide derivatives, preparation and application thereof
The invention relates to 4-cyanopyrazole-3-carboxamide derivatives of formula (I):
in which R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 are as described herein. Also disclosed and claimed...
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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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7514570 |
Derivatives of 3-hydroxy-4-(cyclyl-alkylaminoalkyl)-5-phenyl-1h-pyrazole as antagonists of the gonadotropin releasing hormone (GnRH) for use in the treatment of sex hormone related conditions, such as prostatic of uterine cancer
The invention relates to a group of novel pyrazole compounds of Formula (I): wherein: R 1 , R 2 , R 3 , M and R 5 are as defined in the specification, which are useful as gonadotrophin releasing...
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7514465 |
Synthesis of N2-(substituted arylmethyl)-3-(substituted phenyl)indazoles as novel anti-angiogenic agents
Novel compounds of 2-(substituted arylmethyl)-3-(substituted phenyl)-2H-indazoles and 1-(substituted arylmethyl)-3-(substituted phenyl)-1H-indazoles are synthesized, and useful as anti-angiogenic...
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7514457 |
Substituted aryloxymethyl bicyclicmethyl acetamide compounds
Compounds of the general formula (I):
pharmaceutical compositions comprising a compound of general formula (I); and methods of treating disease conditions caused by overactivation of the VR1...
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7514428 |
Pesticidal 1-aryl-3-amidoxime-pyrazole derivatives
1-Arylpyrazole-3-substituted-amidoxime derivatives of formula (Ia) or (Ib):
or salts thereof, wherein the various symbols are as defined in the description, and pesticidal compositions thereof,...
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7511065 |
Mixed lineage kinase modulators
The present invention provides a compound of the formula: (Formula I); or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising an effective amount of a compound of...
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7511046 |
Thienoisoxazolyl- and thienylpyrrazolyl-phenoxy substituted propyl derivatives useful as D4 antagonists
The compounds are of the class thienoisoxazolyl- and thienylpyrrazolyl-phenoxy substituted propyl derivatives, useful as D 4 antagonists. Said compounds are useful for the treatment of medical...
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7511034 |
Dialkylhydroxybenzoic acid derivatives containing metal chelating groups and their therapeutic uses
Novel dialkylhydroxybenzoic acid derivatives containing metal chelating groups are disclosed. The novel compounds are used as therapeutics for treating and/or preventing various medical...
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