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7635703 |
Imidazole substituted pyrazole kinase inhibitors
The present invention is directed to novel substituted pyrazole compounds of Formula (I) or a form or composition thereof
and the use thereof as inhibitors of ATP-protein kinase interactions.
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7625926 |
P-glycoprotein inhibitor, method for preparing the same and pharmaceutical composition comprising the same
The bioavailability of an anticancer agent is enhanced when the anticancer agent is administered together with a pharmaceutical composition comprising a compound of formula (I) or a...
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7625758 |
Coumarin-based cyanine dyes for non-specific protein binding
Protein dyes whose molecular structure is that of a coumarin moiety coupled to a quaternary ammonium heterocycle through a vinyl or polyvinyl linkage demonstrate the ability to associate with...
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7622585 |
Phenylglycinamide derivatives useful as anticoagulants
The present invention relates generally to phenylglycinamide derivatives that inhibit serine proteases. In particular it0 is directed to novel phenylglycinamide derivatives, and analogues thereof,...
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7615564 |
Isoquinoline derivatives having kinasae inhibitory activity and drugs containing the same
An objective of the present invention is to provide compounds having Rho kinase inhibitory activity and useful for the treatment of diseases mediated by Rho kinase. The compounds according to the...
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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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7538121 |
Vanilloid receptor modulators
Certain compounds of formula (I),
or a pharmaceutically acceptable salt or solvate thereof, wherein R 1 , R 2 , R 3 , P, X, Y, q, r ans s are as defined in the specification, a process for...
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7524861 |
Process for the preparation of a hydrate of an anthranilic acid derivative
A hydrate of an acid addition bis-salt of an anthranilic acid derivative is produced by a process which comprises:
(a) combining, in any order, the anthranalic acid derivative, a...
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7476671 |
2-amino-imidazo[4,5-d]pyridazin-4-ones, their preparation and their use as pharmaceutical compositions
The present invention relates to 2-amino-imidazo[4,5-d]pyridazin-4-ones and 2-amino-imidazo[4,5-c]pyridin-4-ones of general formula
wherein R 1 to R 4 and X are defined as in claims 1 to 6...
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7470787 |
Isoquinoline compounds
Isoquinoline compounds with G are provided that influence, inhibit or reduce the action of a G-protein receptor kinase. Pharmaceutical compositions including therapeutically effective amounts of...
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7465744 |
Triazole compounds and the therapeutic use thereof
The invention relates to triazole compounds of general formula (I), wherein A, B, R 1 , R 2 , R 3 and R 4 have the meaning cited in claim 1. The invention also relates to a pharmaceutical agent...
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7449477 |
7-phenyl-isoquinoline-5-sulfonylamino derivatives as inhibitors of akt (protein kinase B)
The present invention relates to compounds Formula (I) as inhibitors of AKT activity, which are useful for the treatment of susceptible neoplasms and viral infections.
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7439242 |
PPARγ modulators
Modulators of PPARγ activity are provided which are useful in pharmaceutical compositions and methods for the treatment of conditions such as type II diabetes and obesity.
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7417062 |
Substituted arylamides
Substituted benzamide compounds are provided along with methods for the use of those compounds for treating cancer.
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7414063 |
Inhibitors of Akt (protein kinase B)
The present invention relates to compounds Formula (I): as inhibitors of AKT activity, which are useful for the treatment of susceptible neoplasms and viral infections.
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7384957 |
3,4-dihydro-1H-isoquinolin-2-yl-derivatives
The present invention relates to novel compounds of formula I wherein the variable groups are as defined in the claims or a pharmaceutically acceptable acid addition salt thereof. The compounds of...
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7351807 |
Cyanine-sulfenates for dual phototherapy
Dye-sulfenate derivatives and their bioconjugates for dual phototherapy of tumors and other lesions. The compounds comprise sulfenates having the formula, t,0080 where E is selected from the group...
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7345057 |
5-HT7 receptor antagonists
The invention relates to compounds having pharmacological activity towards the 5-HT7 receptor, and more particularly to some some tetrahydroisoquinoline substituted sulfonamide compounds, to...
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7323474 |
Pyridine derivatives inhibiting angiogenesis and/or VEGF receptor tyrosine kinase
The invention relates to pyridine derivatives of formula (I)
wherein the substituents and symbols are defined as indicated in the description, processes for the preparation thereof, their usage...
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7309708 |
Hepatitis C virus inhibitors
Hepatitis C virus inhibitors are disclosed having the general formula:
wherein R 1 , R 2 , R 3 , R′, B, Y and X are described in the description. Compositions comprising the compounds and...
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7256186 |
Gamma secretase inhibitors
This invention discloses novel gamma secretase inhibitors of the formula:
wherein:
R 1 is a substituted aryl or substituted heteroaryl group; R 2 is an R 1 group, alkyl, —XC(O)Y,...
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7250526 |
Transfer hydrogenation process and catalyst
A catalytic transfer hydrogenation process is provided. The catalyst employed in the process is a metal hydrocarbyl complex which is coordinated to defined bidentate ligands substituted with at...
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7208602 |
Gamma secretase inhibitors
This invention discloses novel gamma secretase inhibitors of the formula:
wherein:
R 1 is a substituted aryl or substituted heteroaryl group; R 2 is an R 1 group, alkyl, —X(CO)Y, or...
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7189758 |
Glucocorticoid mimetics, methods of making them, pharmaceutical formulations, and uses thereof
A compound of Formula (I)
wherein R 1 , R 2 , R 3 , R 4 , R 5 , and R 6 are as defined herein, or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such...
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7186720 |
Tetrahydropyridyl-alkyl-heterocycles, method for preparing the same and pharmaceutical compositions containing the same
The present invention relates to compounds of formula (I):
in which X represents N or CH; R 1 represents a hydrogen or halogen atom or a CF 3 group; R 2 and R 3 independently represent a...
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7169927 |
Indole-amide derivatives and their use as glycogen phosphorylase inhibitors
Heterocyclic amides of formula (1)
wherein:
is a single or double bond;
A is phenylene or heteroarylene; m is 0, 1 or 2; n is 0, 1 or 2; R 1 is selected from for example halo, nitro,...
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7166617 |
Cyclic amide derivatives
Novel compounds represented by the following formula (I) that act as a ligand to sigma receptor/binding cite and a medicament comprising the same as an active ingredient:
wherein X represents...
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7166607 |
Substituted indoles
The present invention relates to substituted indoles of formula (I) useful as pharmaceutical compounds for treating respiratory disorders
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RE39265 |
Heteroarylpiperidines, and their use as antipsychotics and analgetics
Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a...
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7041664 |
2-aminoquinolinecarboxamides: neurokinin receptor ligands
Disclosed are compounds of the formula:
or pharmaceutically acceptable salts or pharmaceutically acceptable solvates thereof,
wherein R 1 , R 2 , R 3 , X, Q 1 and Q 2 are defined herein,
...
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7030150 |
Benzimidazole compounds and antiviral uses thereof
The present invention relates to novel benzimidazole compounds that have useful antiviral activity. More specifically, the invention encompasses benzimidazole compounds that inhibit membrane fusion...
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7012078 |
2-aminopyridines containing fused ring substituents
The present invention relates to 2-aminopyridine derivatives of the formula
wherein G, R 1 and R 2 are defined as in the specification, that exhibit activity as nitric oxide synthase (NOS)...
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6982264 |
Substituted alcohols useful in treatment of Alzheimer's disease
The invention relates to substituted alcohol compounds of the formula (I):
wherein X, R 1 , R 2 , R 3 , R N , R 20 and R C are defined herein. The compounds are useful in the treatment or...
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6960599 |
Heterocyclic aminoalkylpyridine derivatives as psychopharmaceuticals
The invention relates to heterocyclic aminoalkylpyridine derivatives of the formula I:
where
R 1 is the radical of a heterocycle having 1 to 3 ring structures, where each ring structure is...
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6949565 |
Protein kinase inhibitors
Novel isoquinoline derivatives which are useful as inhibitors of protein kinases for experimental, medical, and drug design purposes are disclosed. Preferred compounds which are specific inhibitors...
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6849644 |
Isoquinoline derivatives useful in the treatment of CNS disorders
The invention relates to novel tetrahydroquinoline compounds having pharmacological activity, processes for their preparation, to compositions containing them and to their use in the treatment of...
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6846817 |
Nicotine receptor ligands
The invention provides nicotine receptor agonists of formula I:
wherein R 1 , x, y, and n have any of the values given in the specification, or a pharmaceutically acceptable salt thereof, as...
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6841560 |
Substituted isoquinoline derivatives and their use as anticonvulsants
This invention relates to substituted isoquinoline derivatives and their use as anticonvulsants.
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6815451 |
1,2,3,4-Tetrahydroisoquinolines derivatives as urotensin II receptor antagonists
The invention relates to novel 1,2,3,4-tetrahydroisoquinoline derivatives of formula (I) and related compounds and their use as active ingredients in the preparation of pharmaceutical compositions....
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6800642 |
Antipsychotic aminomethyl derivatives of 7,8-dihydro-2,6,9-trioxa-3-aza-cyclopenta&lsqb a&rsqb naphthalene
Compounds of the formula: useful for treatment of disorders such as schizophrenia, schizoaffective disorder, bipolar disorder, Parkinson's disease, L-DOPA induced pychoses and dyskinesias,...
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6720427 |
Thiazole derivatives
The invention provides compounds of formula 1 wherein R 1 , R 3 , and R 4 are as defined, and their pharmaceutically acceptable salts. Compounds of formula 1 are indicated to have activity...
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6703392 |
1,2,3,4-tetrahydroisoquinoline derivatives
The invention relates to novel 1,2,3,4-tetrahydroisochinoline derivatives of formula (I) and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also...
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6642228 |
α1b-adrenergic receptor antagonists
There are provided compounds represented by the general formula (I): [wherein Ar is indole etc., R 1 is hydrogen etc., B is bond, or B—N—R 1 forms a ring structure and is piperidine etc.,...
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6608071 |
Isoquinoline derivatives with angiogenesis inhibiting activity
The invention relates to compounds of formula I wherein r is from 0 to 2; n is from 0 to 2; m is from 0 to 4; A, B, D and E are each independently of the others N or CH, with the proviso that...
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6602867 |
Triazole compounds with dopamine-D3-receptor affinity
Triazole compounds of the following formula where R 1 , R 2 , A and B have the meanings given in the description are described. The compounds according to the invention possess a high affinity...
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6573278 |
Aryl sulfonamides and analogues thereof and their use in the treatment of neurodegenerative diseases
The present invention relates to new aryl ether sulphonamides and analogues, processes for their preparation and their use for the treatment of neurodegenerative disorders, in particular for the...
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6548520 |
Substituted imidazoles having anti-cancer and cytokine inhibitory activity
The present invention is related to novel 2-alkyl substituted imidazoles of formula (I) useful for the treatment of CSBP kinase mediated diseases.
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6534522 |
Subtype-selective NMDA receptor ligands and the use thereof
The invention relates to subtype-selective NMDA receptor ligands and the use thereof for treating or preventing neuronal loss associated with stroke, ischemia, CNS trauma, hypoglycemia and surgery,...
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6509467 |
Transfer hydrogenation process
A catalytic transfer hydrogenation process is provided. The catalyst employed in the process is a metal neutral hydrocarbyl complex which is coordinated to defined bidentate ligands. Preferred...
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6509351 |
Phenyl- and pyridyl-tetrahydro-pyridines having TNF inhibiting activity
The present invention relates to compounds of formula (I): as well as the salts or solvates thereof, to pharmaceutical compositions containing them, to a process for preparing them and to...
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