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6589962 |
Alpha-hydroxy-gamma-&lsqb &lsqb (carbocyclic-or heterocyclic-substituted)amino&rsqb carbonyl&rsqb alkanamide derivatives and uses thereof
Certain α-hydroxy-γ-[[(carbocyclic- or heterocyclic-substituted)amino]carbonyl]alkanamide derivatives are described as inhibitors of HIV protease and inhibitors of HIV replication. These...
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6589968 |
Epothilone compounds and methods for making and using the same
This present invention relates to compounds of formula (I) and to pharmaceutically acceptable salts and solvates thereof, wherein R 1 , R 2 , R 3 , R 4 , R 5 , W, X, Y, and Ar are as defined...
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6586453 |
Substituted thiazoles and the use thereof as inhibitors of plasminogen activator inhibitor-1
The present invention relates to the use of aminothiazole derivatives of Formula I of as inhibitors of PAI-1, and to novel classes of aminothiazole derivatives, their synthesis and their use as...
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6586464 |
Artemisinin analogs having antimalarial, antiproliferative, and antitumor activities and chemoselective methods of making the same
Methods for producing novel artemisinin analogs and artemisinin dimers having antimalarial, antiproliferative and antitumor activities are described herein. These novel artemisinin analogs and...
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6586452 |
C1 to C4 side chain modified nodulisporic acid analogs
The present invention relates to novel nodulosporic acid derivatives, which are acaricidal, antiparasitic, insecticidal and anthelmintic agents.
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6583163 |
Agent for inhibition of cytokine production and agent for inhibition of cell adhesion
The present invention provides an agent for inhibiting cytokine production or cell adhesion, comprising at least one compound selected from the group consisting of thiazole derivatives represented...
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6579894 |
Prolines as antimicrobial agents
Transfer ribonucleic acid (tRNA) synthetase inhibitors, salts, and pharmaceutically acceptable compositions thereof of the general formula: wherein Ar is aryl and heteroaryl; L is —C(O)N(Q)CH...
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6579871 |
Methods of using novel compounds as neuro-protective agents
This invention relates to novel phenyl oxazoles, thiazoles, oxazolines, oxadiazoles and benzoxazoles useful as neuro-protective agents.
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6573285 |
Method for preventing or treating pain by administering an endothelin antagonist
Prevention or treatment of pain by administration of an endothelin antagonist.
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6569874 |
Thiazoles as factor Xa inhibitors
The present application describes oxygen and sulfur containing heteroaromatics and derivatives thereof of formula I: or pharmaceutically acceptable salt or prodrug forms thereof, wherein J is O...
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6569875 |
Fungicide mixtures based on pyridin carboxamides and benzimidazoles or the precursors thereof
Fungicidal mixtures comprise as active components a) an amide compound of the formula I A—CO—NR 1 R 2 I in which A is an aryl group or an aromatic or nonaromatic, 5- or 6-membered...
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6566381 |
Hetero-substituted metalloprotease inhibitors
Heterocyclic substituted compounds having the general structure: which are inhibitors of metalloproteases and which are effective in treating conditions characterized by excess activity of these...
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6559142 |
Sulfonamide matrix metalloproteinase inhibitors
Matrix metalloproteinase inhibitors are tricyclic substituted cyclic sulfonamides of the formula or a pharmaceutically acceptable salt thereof wherein R 1 and R 2 include hydrogen, alkyl, and...
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6555540 |
Combinations of aldose reductase inhibitors and selective cyclooxygenase-2 inhibitors
This invention is directed to methods, pharmaceutical compositions and kits comprising an aldose reductase inhibitor (ARI), a prodrug thereof or a pharmaceutically acceptable salt of said ARI or...
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6555535 |
Tricyclic biphenyl sulfonamide matrix metalloproteinase inhibitors
Matrix metalloproteinase inhibitors are tricyclic sulfonamides of the Formula I or a pharmaceutically acceptable salt thereof, wherein R 1 and R 2 include hydrogen, alkyl, and substituted...
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6552031 |
Synergistic analgesic combination of oxycodone and rofecoxib
Disclosed is a pharmaceutical composition, comprising a combination of a dose of rofecoxib or a pharmaceutically acceptable salt thereof and a dose of oxcodone or a pharmaceutically acceptable salt...
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6552054 |
Chromone derivatives, process for the preparation of the same and uses thereof
The invention provides chromone derivatives of the following general formula, a process for preparing such chromone derivatives and a prophylactic and therapeutic agent comprising such chromone...
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6552047 |
H2 receptor antagonist compounds in combination with nitric oxide donors, compositions and methods of use
The present invention describes novel nitrosated and/or nitrosylated H 2 receptor antagonist compounds, and novel compositions comprising at least one H 2 receptor antagonist compound that is...
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6548523 |
Process for the preparation of arylethanolamine derivatives having an anti-obesity and anti-diabetic properties
The present invention is a process for the preparation of a compound of Formula (IA) or a pharmaceutically acceptable salt thereof: that includes preparing a diamide of Formula (II) or a...
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6545009 |
Retinoid-related receptor function regulating agent
1,3-Azole derivatives, pharmaceutical compositions thereof and methods for regulating the function of retinoid-related receptors with 1,3-azole derivatives are disclosed. Such regulation may be...
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6544975 |
Substituted porphyrins
The present invention relates, in general, to a method of modulating physiological and pathological processes and, in particular, to a method of modulating cellular levels of oxidants and thereby...
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6540988 |
Method of reducing or preventing malodour
A method of reducing or preventing body malodour by topically applying to human skin perfume components capable of inhibiting the producation of odoriferous steroids by microorganisms on the skin....
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6541475 |
α, β-unsaturated sulfones for treating proliferative disorders
α, β-Unsaturated sulfones of the following formulae are provided, which are useful as antiproliferative agents, including, for example, anticancer agents:
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6538029 |
Methods for treatment of renal cell carcinoma
A method of treating renal cell carcinoma in a mammal with that disease comprising administering to the mammal a physiologically effective amount of an inhibitor of PDE10.
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6534503 |
Melanocortin receptor-3 ligands to treat sexual dysfunction
Methods for treating sexual dysfunction, such as erectile dysfunction or sexual arousal disorder, with a compound having the generic formula X 1 —X 2 -(D)Phe-Arg-(D)Trp-X 3 . A particularly...
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6528037 |
Method for determining whether a compound is an insulin receptor kinase activator
A method for determining whether a compound is an insulin receptor kinase activator.
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6528535 |
Bicyclic inhibitors of protein farnesyl transferase
The present invention provide compounds of Formula I The present invention also provides a method of treating cancer and treating or preventing restenosis or atherosclerosis. Also provided by...
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6528528 |
Thiourea and benzamide compounds, compositions and methods of treating or preventing inflammatory diseases and atherosclerosis
The present invention provides compounds of Formula I shown below. The present invention also provides methods of treating or preventing 3 inflammation or atherosclerosis, and a pharmaceutical...
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6525099 |
N-substituted sulfonamide derivatives
The present invention provides certain N-substituted sulfonamide derivatives useful for potentiating glutamate receptor function in a mammal and therefore, useful for treating a wide variety of...
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6521651 |
Pharmaceutical composition
A liquid pharmaceutical composition providing improved oral bioavailability is disclosed for compounds which are inhibitors of HIV protease. In particular, the composition comprises a solution in a...
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6521653 |
Microbicidal benzotriazoles
Novel benzotriazoles of the formula in which R, X 1 , X 2 , X 3 , X 4 and Y have the meanings given in the description, and their acid addition salts and metal salt complexes, a process for the...
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6521626 |
Thiocarboxamide derivatives
Compounds of formula (1): wherein R 1 is a hydrogen atom or an optionally substituted cycloaliphatic, polycycloaliphatic, heterocycloaliphatic, polyheterocycloaliphatic, aromatic or...
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6518290 |
Substituted oxazoles and thiazoles derivatives as HPPAr alpha activators
A compound of formula (I) and pharmaceutically acceptable salts, solvates and hydrolysable esters thereof wherein; X 1 represents O or S; R 1 and R 2 independently represent H, halogen, —CH...
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6515002 |
Compounds and compositions for treating C1s-mediated diseases and conditions
Disclosed is a method for treating the symptoms of an acute or chronic disorder mediated by the classical pathway of the complement cascade, comprising administering to a mammal in need of such...
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6515001 |
IL-8 receptor ligands-drugs for inflammatory and autoimmune diseases
The invention provides therapeutic and biological uses of chemokine-receptor-binding compounds (including chemokine receptor ligands such as chemokine receptor agonists or antagonists), such as...
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6514968 |
Aminoalkoxy carbazoles for the treatment of cns diseases
The present invention provides aminoalkoxy carbazole derivatives, and more specifically, provides compounds of formula (I) wherein R 1 , R 2 , R 3 , R 4 , R 8 and R 9 are described herein....
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6511981 |
Compositions and treatment for diabetic complications
This invention is directed to methods, pharmaceutical compositions and kits comprising an aldose reductase inhibitor (ARI), a prodrug thereof or a pharmaceutically acceptable salt of said ARI or...
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6509379 |
Phenylacetic acid derivatives, process and intermediate products for their preparation, and their use as fungicides and pesticides
Phenylacetic acid derivatives of the formula I where the variables are as disclosed herein, their salts, processes and intermediates for their preparation, and their use for controlling harmful...
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6509348 |
Combination of an ADP-receptor blocking antiplatelet drug and a thromboxane A2 receptor antagonist and a method for inhibiting thrombus formation employing such combination
A method is provided for inhibiting platelet aggregation and thrombus formation by administering to a patient an ADP-receptor blocking antiplatelet drug, such as clopidogrel, in combination with a...
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6503935 |
Imidazoles and related compounds as α1A agonists
Compounds having formula I: are useful in treating diseases prevented by or ameliorated with α 1A agonists. Also disclosed are α 1A agonist compositions and a method of activating α 1 ...
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6500804 |
Method for the improvement of islet signaling in diabetes mellitus and for its prevention
The present invention discloses a method for therapeutically treating mammals, including but not limited to humans, to increase the relative insulin producing performance of endogenous pancreatic...
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6500849 |
1-alkyl-, 1-alkenyl-, and 1-alkynylaryl-2-amino 1,3-propanediols and related compounds
Novel 1-alkyl-, 1-alkenyl-, and 1-alkynylaryl-2-amino-1,3-propanediols, intermediates and processes for the preparation thereof, and methods of reducing inflammation and cell proliferation, and...
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6498172 |
Prostaglandin agonists and their use to treat bone disorders
This invention relates to prostaglandin agonists, methods of using such prostaglandin agonists, pharmaceutical compositions containing such prostaglandin agonists and kits containing such...
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6498174 |
Substituted oxazoles and thiazoles derivatives as hPPAR&ggr and hPPARα activators
The present invention discloses compounds of formula (I), and tautomeric forms, pharmaceutically acceptable salts, or solvates thereof. Preferably, the compounds of the invention are dual...
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6495579 |
Method for treating multiple sclerosis
Methods and compositions for treating or preventing inflammatory diseases such as psoriasis or multiple sclerosis are provided, comprising the step of delivering to the site of inflammation an...
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6495580 |
Compounds, compositions and methods for treating or preventing pneumovirus infection and associated diseases
Compounds, compositions and methods are provided for the prophylaxis and treatment of infections caused by viruses of the Pneumovirinae subfamily of Paramyxoviridae and diseases associated with...
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6492404 |
Thiazolylcinnamonitriles and pest controlling agents
Compounds represented by the general formula (1); and pest controlling agents containing one or more of the compounds as the active ingredients, wherein A is substituted phenyl, C 1 -C 6 alkly or...
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6492421 |
Substituted phenylalanine type compounds which inhibit leukocyte adhesion mediated by VLA-4
Disclosed are compounds which bind VLA-4. Certain of these compounds aslo inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the...
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6492402 |
Thrombin inhibitors
The present invention relates to a compound having formula I: and pharmaceutically acceptable salts thereof. The compounds of formula I and pharmaceutical compositions containing them are of the...
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6492403 |
Methods of treating C1s-mediated diseases and conditions and compositions thereof
Disclosed is a method for treating the symptoms of an acute or chronic disorder mediated by the classical pathway of the complement cascade, comprising administering to a mammal in need of such...
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