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7612089 |
Tetrahydroisoquinolines as factor Xa inhibitors
The present invention is directed to compounds represented by Formula I and pharmaceutically acceptable salts, solvates, hydrates, and prodrugs thereof which are inhibitors of Factor Xa. The...
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7601740 |
Selective serotonin 2A/2C receptor inverse agonists as therapeutics for neurodegenerative diseases
Behavioral pharmacological data with the compound of formula (I), a novel and selective 5HT2A/2C receptor inverse agonist, demonstrate in vivo efficacy in models of psychosis and dyskinesias. This...
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7589105 |
Preventives or remedies for alzheimer's disease, or amyloid protein fibril-formation inhibitors, which include a nitrogen-containing heteroaryl compound
Pharmaceutical compositions and methods of treatment are provided for treating amyloidosis, containing, as an active ingredient, at least one nitrogen-containing heteroaryl compound represented by...
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7582638 |
Pyrazole-isoquinoline urea derivatives as p38 kinase inhibitors
The present invention provides kinase inhibitors of Formula (I) wherein R1, R2, and X are as described herein, or a pharmaceutically acceptable salt thereof.
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7572806 |
PPAR active compounds
Compounds are described that are active on PPARs, including pan-active compounds. Also described are methods for developing or identifying compounds having a desired selectivity profile.
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7550481 |
Phenylamide and pyridylamide beta-secretase inhibitors for the treatment of Alzheimer's disease
The present invention is directed to phenylamide and pyridylamide derivative compounds of which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which...
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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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7528151 |
Heterocyclic urea derivatives for the treatment of pain
Compounds of formula (I):
or a pharmaceutically acceptable salt thereof, or a solvate thereof, wherein: P, P′, R 1 , R 2 , n, p, q, r, and s are as defined in the specification, processes for...
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7528150 |
Urea derivatives having vanilloid receptor antagonist activity
According to the invention there are provided compounds of formula (I)
wherein R 1 , p, P, n, s, r, W, P′, t, R 2 and q are as defined in the specification, processes for preparing them and...
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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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7507748 |
Substituted aryl-amine derivatives and methods of use
Selected amines are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. The invention encompasses novel compounds of Formula I and II
wherein R, R 1 ...
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7504228 |
Integrin linked kinase modulation of monocyte activation
Methods are provided to specifically modulate the activation of monocytes and/or macrophages. Administration of integrin linked kinase (ILK) blocking agents; compounds that otherwise prevent the...
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7495011 |
Anti-coronavirus drug
The present invention provides an anti-coronavirus agent including as an active ingredient as exemplified by nelfinavir and salts thereof, an anti-SARS agent including the anti-coronavirus agent,...
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7482361 |
Crystalline form for quinapril hydrochloride and process for preparing the same
A novel crystalline form of quinapril hydrochloride of formula (I)
An amorphous form of quinapril hydrochloride substantially free of impurities, specially diketopiperazine compound, and...
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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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7476763 |
Oxo-substituted cyclohexyl-1,4-diamine compounds
Novel cyclohexyl-1,4-diamine compounds corresponding to formula I:
methods for their production, pharmaceutical formulations containing these compounds, methods of producing such pharmaceutical...
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7456195 |
Phenylglycinamide and pyridylglycinamide derivatives useful as anticoagulants
The present invention provides novel phenylglycinamide derivatives of Formula (I) or (IV):
or a stereoisomer, tautomer, pharmaceutically acceptable salt, solvate, or prodrug thereof, wherein...
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7452887 |
Quinoline- and isoquinoline-based compounds exhibiting ATP-utilizing enzyme inhibitory activity, and compositions, and uses thereof
Quinoline- and isoquinoline-based compounds exhibiting ATP-utilizing enzyme inhibitory activity, methods of using compounds exhibiting ATP-utilizing enzyme inhibitory activity, and compositions...
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7442710 |
Substituted phenyl methanones
The present invention relates to compounds of general formula IA or IB
wherein
X 1 and X 2 are each independently N or C—R″ and R 1 , R 2 ,R 3 , R 4 , R 5 , and R 6 are as defined in...
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7425563 |
4-(Substituted aryl)-5-hydroxyisoquinolinone derivative
The invention provides 4-substituted aryl-5-hydroxyisoquinolinone derivatives and their pharmacologically acceptable addition salts with excellent inhibitory effect on poly (ADP-ribose) synthetase....
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7423049 |
Inhibitors of p38
The present invention relates to inhibitors of p38, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods...
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7417056 |
5-substituted quinoline and isoquinoline derivatives, a process for their production and their use as anti-inflammatory agents
Compounds of general formula (IIa) or (IIb)
and their use as pharmaceutical agents.
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7396838 |
Use of 1H-indol-3-yl-2-oxoacetamide compounds
A method of treating cancer including administering to a subject in need thereof an effective amount of a compound of the formula 1:
wherein R 1 , R 2 , R 3 , R 4 , and n are as defined herein.
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7371763 |
Inhibition of raf kinase using quinolyl, isoquinolyl or pyridyl ureas
The invention relates to a group of quinolyl, isoquinolyl and pyridyl ureas, their the use in treating raf mediated diseases, and pharmaceutical compositions which contain these ureas for use in...
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7371762 |
3-substituted 6,7-dihydroxytetrahydroisoquinoline derivatives for use as antibacterial agents
The invention relates to novel tetrahydroisoquinoline derivatives of general formula I and theirs use as active ingredients in the preparation of pharmaceutical compositions. The invention also...
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7361687 |
Arylsulphonamide derivatives and methods of preparing
The present invention relates to novel arylsulphonamide compounds, defined by formula I and the description, as well as their method of preparation and their therapeutic use
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7361663 |
N-acylpyrrolidin-2-ylalkylbenzamidine derivatives as inhibitors of factor Xa
This invention is directed to N-acylpyrrolidin-2-ylalkylbenzamidine derivatives which useful for inhibiting the activity of Factor Xa, by contacting said derivatives with a composition containing...
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7351716 |
Dermatological preparations
The present invention relates to a dermatologic preparation containing a diamide derivative represented by the following formula (1):
(wherein, R 1 represents a linear or branched hydrocarbon...
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7351715 |
Unit dosage forms for the treatment of herpes simplex
The components of this invention are chosen because of their complementarity for the prevention or treatment of diseases caused by the herpes simplex virus. L-Lysine favorably increases the...
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7323475 |
Nitrogen-containing heteroaryl compounds and methods of use thereof
The present invention relates to compounds suitable for use in mediating hypoxia inducible factor and for treating erythropoietin-associated conditions by increasing endogenous erythropoietin in...
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7307088 |
Substituted anthranilic amide derivatives and methods of use
Selected compounds are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically...
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7307086 |
3-(4-heteroarylcyclohexylamino)cyclopentanecarboxamides as modulators of chemokine receptors
The present invention is directed to compounds of Formula I:
which are modulators of chemokine receptors. The compounds of the invention, and compositions thereof, are useful in the treatment...
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7285563 |
Heteroaromatic urea derivatives as VR-1 receptor modulators for treating pain
The present invention provides compounds of formula (I); pharmaceutically acceptable salts and N-oxides thereof in which A, B, D and E are C or N with the proviso that one or more are N, R 1 , R 2...
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7268135 |
Biaryl sulfonamides and methods for using same
The present invention relates to biaryl sulfonamides and their use as, for example, metalloproteinase inhibitors.
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7241775 |
Composition, process of making, and medical use of substituted 4-phenyltetrahydroisoquinolines
Substituted 4-phenyltetrahydroisoquinolines of formula I, process for their preparation, their use as a medicament and medicaments containing them.
The compounds of formula I can be used, among...
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7238707 |
Substituted pentanols, a process for their production and their use as anti-inflammatory agents
The invention relates to substituted pentanols, a process for their production and their use as anti-inflammatory agents.
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7211586 |
Substituted tetrahydroisoquinolines
The invention is directed to physiologically active compounds of formula (I):
wherein:
R 1 represents optionally substituted aryl, optionally substituted heteroaryl, R 3 NH—Ar 1 —L 2 —...
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7202253 |
Cycloalkyl inhibitors of potassium channel function
Novel cycloalkyl compounds useful as inhibitors of potassium channel function (especially inhibitors of the K v 1 subfamily of voltage gated K + channels, especially inhibitors K v 1.5 which has...
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7199133 |
Derivatives of phenoxy-n-′4-(isothiazolindin-1, 1-dioxid-2yl)phenyll-valerian-acid amide and other compounds as inhibitors of the coagulation factor xa in the treatment of thromboembolic diseases and tumors
Novel compounds of formula (I), wherein D, W, X, Y, T and R 1 have the meanings cited in claim 1 , are inhibitors of coagulation factor Xa and can be used for the prophylaxis and/or therapy of...
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7169768 |
Method of decreasing atherosclerosis and its complications
A method of decreasing atherosclerosis and its complications including but not limited to myocardial infarction, stroke and peripheral vascular disease wherein the method involves administering to...
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7169767 |
Ophthalmic compositions containing galactomannan polymers and borate
The present invention is directed to ophthalmic compositions containing a gelling amount of a combination of galactomannan polysaccharides and borates. The compositions gel or partially gel upon...
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7163949 |
4-phenyl substituted tetrahydroisoquinolines and use thereof
Provided herein are compounds of the formulae IA–IF. These compounds are tetrahydroisoquinolines of the following structure:
wherein R 1 –R 8 for compounds of each of the formulae IA, IB,...
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7144895 |
Benzene acetamide compounds useful as serine protease inhibitors
Compounds having the formula (I),
and pharmaceutically-acceptable salts, hydrates, or prodrugs thereof, are useful as serine protease inhibitors, wherein X is —OH, —O(alkyl), —O(aryl),...
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7125891 |
Tripeptidyl peptidase inhibitors
The present invention is concerned with novel compounds of formula (I) which are inhibitors of a membrane tripeptidyl peptidase responsible for the inactivation of endogenous neuropeptides such as...
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7122559 |
Phenylglycine derivatives useful as serine protease inhibitors
Compounds having the formula (I),
or a stereoisomer or pharmaceutically-acceptable salt, or hydrate thereof, are useful as factor VIIa inhibitors, wherein X is —NR 6 S(O) p R 16 ; W is...
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7115646 |
Cyclic diamines and derivatives as factor Xa inhibitors
The present application describes cyclic diamino compounds, derivatives thereof, and pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of factor Xa.
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7109212 |
Quinoline and isoquinoline derivatives, a process for their production and their use as inflammation inhibitors
The invention relates to quinoline and isoquinoline derivatives of general formula I
and a process for their production, and their use as inflammation inhibitors.
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7105536 |
Compounds
The invention relates to novel isoquinolines and their use as anticonvulsants and in the treatment of a variety of disorders.
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7094789 |
5-substituted isoquinoline derivatives
A compound represented by the following formula (1) or a salt thereof:
wherein R 1 represents hydrogen atom, a halogen atom and the like; R 2 represents hydrogen atom, a halogen atom, a C 1-6...
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7091249 |
Drugs for spinal anesthesia
Spinal anesthetics for intrathecal administration to produce spinal anesthesia are provided with use of 6-[2-(1(2)H-tetrazole-5-yl)ethyl]decahydroisoquinolone-3-car
boxylic acid or a...
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