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7618965 |
(Arylamidoanilino)nitroethylene compounds
Compounds represented by Formula (I):
or a pharmaceutically acceptable salt or N-oxide thereof, wherein A, Q, Y, R 1 , R 2 , and R 5 are defined herein, are useful in the treatment of tumors...
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7618961 |
Inhibitors of 11-beta-hydroxy steroid dehydrogenase type 1
The present invention relates to compounds with the formula (II) and also to pharmaceutical compositions comprising the compounds, to processes for their preparation, as well as to the use of the...
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7615563 |
Compositions useful as inhibitors of voltage-gated sodium channels
The present invention relates to compounds useful as inhibitors of voltage-gated sodium channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of...
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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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7608614 |
Process for preparing macrocyclic compounds
Intermediates of the formula QUIN:
and methods for their preparation are described. The intermediate compounds are useful for preparing active agents for the treatment of hepatitis C virus...
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7598236 |
Diazabicyclic central nervous system active agents
Compounds of formula I
pharmaceutical compositions of these compounds, and use of said compositions to control synaptic transmission in mammals.
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7592358 |
Alkyne compounds with MCH antagonistic activity and medicaments comprising these compounds
Alkyne compounds having MCH-receptor antagonistic activity, which are useful for preparing pharmaceutical compositions for the treatment of metabolic disorders and/or eating disorders, particularly...
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7592357 |
Compounds
Novel Inhibitors of Rho-kinases are disclosed.
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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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7589106 |
Alcohol free formulation of argatroban
An aqueous formulation of argatroban and of related compounds is disclosed along with a reconstitutable formulation, each of which is substantially, if not totally alcohol free. The formulations...
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7589068 |
Inhibitors of Akt activity
The instant invention provides for compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for...
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7585878 |
Benzamide derivative or salt thereof
There is provided a compound having a capsaicin receptor VR1 inhibitory activity and useful as a therapeutic agent for various pains including inflammatory pain and neurogenic pain, migraine,...
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7576100 |
Muscarinic agonists
The present invention relates to tetrahydroquinoline compounds as muscarinic receptor agonists; compositions comprising the same; methods of inhibiting an activity of a muscarinic receptor with...
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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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7572810 |
Alkene piperidine derivatives as antiviral agents
This disclosure provides compounds having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the disclosure is concerned with alkene piperidine...
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7572794 |
Anthranilamide pyridinureas as vascular endothelial growth factor (VEGF) receptor kinase inhibitors
The invention relates to novel anthranilamide pyridinureas as VEGF receptor kinase inhibitors, their production and use as pharmaceutical agents for preventing or treating diseases that are...
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7569688 |
Propane-1, 3-dione derivative
Provided is a pharmaceutical composition containing a propane-1,3-dione derivative as the active ingredient, particularly a GnRH receptor antagonist. Also, provided is a propane-1,3-dione...
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7569604 |
Heterocyclic derivatives for modulation of calcium channels
Heterocyclic derivatives act as Ca channel antagonists. The compositions are useful for treating or relieving Ca channel mediated conditions.
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7569584 |
4-(2-methyl-5,6,7,8-tetrahydro-quinolin-7-ylmethyl)-1,3-dihydro-imidazole-2-thione as specific alpha2b agonist and methods of using the same
The compound of the formula
wherein the * indicates an asymmetric carbon, is specific to alpha 2B adrenergic receptors in preference over alpha 2A and alpha 2C adrenergic receptors, and...
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7566710 |
Dual molecules containing a peroxide derivative, synthesis and therapeutic applications thereof
The invention relates to dual molecules formed from coupling products complying with the formula
wherein A represents a residue of molecule with anti-malarial activity, Y 1 and Y 2 ,...
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7563807 |
Removal of aldehyde impurity by reactive polystyrene resini
A purification method in the preparation of a substituted 8-arylquinoline, wherein the aryl group at the 8-position contains a substituent substituted-alkenyl group, utilizes a polystyrene-based...
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7563804 |
FMF treatment
The method of improving FMF control, in humans, which includes administering, on an average daily basis, between 5 and 15 milligrams of LTRA to a patient suffering from FMF.
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7550598 |
Kinase inhibitors
Compounds, pharmaceutical compositions, kits and methods are provided for use with kinases that comprise a compound of the formula:
wherein R 1 , R 2 , R 3 , Q, U, V, W, X, and Y are as defined...
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7550597 |
Quinoline and quinoxaline compounds which inhibit platelet-derived growth factor and/or p56lck tyrosine kinases
This invention is directed to quinoline/quinoxaline compounds which inhibit platelet-derived growth factor tyrosine kinase and/or Lck tyrosine kinase, to pharmaceutical compositions comprising...
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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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7534891 |
Quinoline derivatives as H3R inverse agonists
The present invention relates to compounds of formula I:
and pharmaceutically acceptable salts thereof as well as to pharmaceutical compositions comprising these compounds and to methods for...
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7534802 |
Compounds having 4-pyridylalkylthio group as substituent
A subject of the present invention is to provide a novel aromatic five- or six-memberd heterocyclic derivative having 4-pyridylalkylthio as a substituent or a salt thereof which is useful as a...
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7531662 |
Cinchona-alkaloid-based catalysts, and asymmetric alcoholysis of cyclic anhydrides using them
One aspect of the present invention relates to cinchona-alkaloid-based catalysts. A second aspect of the invention relates to a method of preparing a derivatized cinchona alkaloid catalyst by...
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7531554 |
4-oxoquinoline compound and use thereof as HIV integrase inhibitor
Provision of a compound having an anti-HIV activity, particularly an integrase inhibitory activity. A 4-oxoquinoline compound represented by the following formula [I] or a pharmaceutically...
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7531535 |
Lactam-containing compounds and derivatives thereof as factor Xa inhibitors
The present application describes lactam-containing compounds and derivatives thereof of Formula I:
or pharmaceutically acceptable salt forms thereof, wherein ring P, if present is a 5-7...
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7524959 |
Biphenyl derivatives
This invention provides biphenyl derivatives of formula I:
wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , W, a, b and c are as defined in the specification, or a pharmaceutically...
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7524883 |
Eponemycin and epoxomicin analogs and uses thereof
The present invention provides compounds having formula (1): wherein R 1 -R 6 , A, J, D, E, G, Q, w, x, y, and z are as described generally and in classes and subclasses herein, and additionally...
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7524862 |
Alkyne compounds with MCH antagonistic activity and medicaments comprising these compounds
Alkyne compounds of formula I
wherein A, B, W, X, Y, Z, R 1 , and R 2 have the meanings given herein, which have MCH-receptor antagonistic activity and are useful for preparing pharmaceutical...
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7524859 |
(2-carboxamido)(3-amino)thiophene compounds
A method of treatment of hyperproliferative disorders comprises a step of administering an effective amount of a compound represented by
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7514452 |
2-furancarboxylic acid hydrazides and pharmaceutical compositions containing the same
The present invention provides 2-furancarboxylic acid hydrazide compounds represented by General Formula (I) below, and prodrugs, physiologically acceptable salts, hydrates, solvates thereof:
...
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7511145 |
Bicyclic heteroaryl derivatives
Disclosed are compounds, compositions and methods for treating Flaviviridae family virus infections.
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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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7511063 |
High affinity quinoline-based kinase ligands
Quinoline-based inhibitors of cyclin dependent kinase 2, compositions including the inhibitors, and methods of using the inhibitors and inhibitor compositions are described. The inhibitors and...
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7511062 |
Substituted 2-quinolyl-oxazoles useful as PDE4 inhibitors
The invention claims compounds of the formula
wherein
is a 5-membered heteroaryl; X is S or O; R 1 is H, alkyl, cycloalkyl, cylcoalkylalkyl-, —CH 2 F, —CHF 2 , —CF 3 ,...
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7507749 |
Antitumor agents
The invention provides compounds of formula I:
wherein Y is F, Cl, Br, methyl or methoxy; and pharmaceutically acceptable salts thereof. The compounds are effective antitumor agent. The...
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7498343 |
Mycobacterial inhibitors
The present invention relates to novel substituted quinoline derivatives according to the general Formula (Ia) or the general Formula (Ib)
the pharmaceutically acceptable acid or base addition...
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7491825 |
Basic non-peptide bradykinin antagonists and pharmaceutical compositions therefrom
Non-peptide compounds of formula (I) having activity as specific antagonists of bradykinin (BK) B2 receptor. The compounds are chemically characterized by the presence of an alpha,...
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7491714 |
Quinolines and nitrogenated derivatives thereof and their use as antibacterial agents
Quinoline and naphthridine derivatives useful in the treatment of bacterial infections in mammals, particularly humans.
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7488740 |
Substituted quinolin-4-ylamine analogues
Substituted quinolin-4-ylamine analogues are provided. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the...
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7488738 |
Aminophenoxyacetic acid derivatives and pharmaceutical composition containing thereof
There is provided an aminophenoxyacetic acid derivative of the following formula (I):
wherein, R 1 , R 2 , R 3 and R 4 are, independent from each other, alkoxy group, alkyl group or aryl...
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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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7476680 |
Substituted heterocyclic compounds for treating multidrug resistance
Compounds suitable for treating multidrug resistance and methods for their preparation and use are disclosed. The compounds are represented by the following formula:
or an optical isomer,...
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7470709 |
Benzimidazole quinolinones and uses thereof
Methods of inhibiting various enzymes and treating various conditions are provided that include administering to a subject a compound of Structure I or IB, a pharmaceutically acceptable salt...
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7456196 |
Bicyclic-substituted amines as histamine-3 receptor ligands
Compounds of formula (I)
are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Also disclosed are pharmaceutical compositions comprising...
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