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7619095 |
Process for the preparation of indolone derivative
A process for the preparation of 4-[2-(Di-n-propylamino)ethyl]-2,3-dihydro-1H-indol-2-one of formula (I) and its pharmaceutically acceptable salts, solvates Formula I involving new intermediates of...
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7618967 |
Indane compounds
The invention provides novel indane compounds which are useful in the treatment of affective disorders, pain disorders, attention deficit hyperactivity disorder (ADHD), cognitive disorders,...
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7612099 |
Vinylogous acid derivatives
The invention is concerned with vinylogous acids derivatives of formula (I)
wherein A and R 1 to R 6 are as defined in the description and in the claims, as well as physiologically acceptable...
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7612065 |
Inhibitors of c-JUN N-terminal kinases (JNK)
The present invention relates to inhibitors of JNK, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods...
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7608723 |
Indole and benzimidazole derivatives
The present invention relates to new indole and benzimidazole compounds and pharmaceutically acceptable salts, esters or prodrugs thereof, compositions of the new compounds together with...
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7608634 |
Substituted pyrrolines as kinase inhibitors
The present invention is directed to novel substituted pyrroline compounds useful as kinase or dual-kinase inhibitors, methods for producing such compounds and methods for treating or ameliorating...
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7605168 |
PDE4B inhibitors
Compounds are described that are active on PDE4. Also described are crystal structures of PDE4B determined using X-ray crystallography, the use of PDE4B crystals and structural information for...
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7601751 |
Indole acetic acid acyl guanidines as β-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 , R 5 , R 6 , R 7 , and...
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7601750 |
Small molecule inhibition of a PDZ-domain interaction
Novel compounds that have been found effective in inhibiting PDZ domain interactions, and particularly interactions of PDZ domains in MAGIs with the oncogenic (tumor suppressor) protein PTEN and...
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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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7592373 |
Amide compounds with MCH antagonistic activity and medicaments comprising these compounds
Compounds of formula (I)
wherein A, B, b, W, X, Y, Z, R 1 , R 2 , and R 3 have the meanings given in claim 1 , pharmaceutical compositions these compounds, and methods of preventing or...
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7582773 |
Substituted phenyl indoles
The present invention relates generally to substituted phenyl indoles and methods of using them, for example as PAI-1 inhibitors.
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7582770 |
Viral polymerase inhibitors
An enantiomer, diastereoisomer or tautomer of a compound, represented by formula I:
wherein A, B, R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , R 9 , and R 10 are as defined herein, or a...
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7582672 |
Compounds for the treatment of CRTH2-mediated diseases and conditions
The present invention provides indole derivatives that antagonize prostaglandin D 2 , and that can be used to treat inflammatory diseases mediated by prostaglandin D 2 .
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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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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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7572782 |
Use of targeted oxidative therapeutic formulation in bone regeneration
A pharmaceutical formulation and its use. The pharmaceutical formulation contains peroxidic species or reaction products resulting from oxidation of an alkene, such as geraniol, by an...
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7566736 |
Substituted indoles, compositions containing them, method for the production thereof and their use
Compounds of formula (I):
wherein R1, R5, R6, R7, Ar, L, A, and Q are as defined in the description, and to salts thereof, to compositions containing them, to the process for preparing them,...
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7563817 |
Purified 2-aryl-3,3-bis(hydroxyaryl)phthalimidines
A method for purifying a 2-aryl-3,3-bis(hydroxyaryl)phthalimidine comprises contacting a crude 2-aryl-3,3-bis(hydroxyaryl)phthalimidine with a purification agent, removing a...
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7560483 |
Methods for synthesis of prodrugs from 1-acyl-alkyl derivatives and compositions thereof
The present invention provides a method for synthesizing 1-(acyloxy)-alkyl derivatives from 1-acyl-alkyl derivatives, which typically proceeds stereospecifically, in high yield, does not require...
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7560473 |
Amine derivative with potassium channel regulatory function, its preparation and use
The present invention provides amine derivatives represented by formula I, its isomers, racemes or optical isomers, pharmaceutical salts thereof, its amides or esters, pharmaceutical compositions...
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7557135 |
Inhibitors of cytosolic phospholipase A2
This invention provides chemical inhibitors of the activity of various phospholipase enzymes, particularly cytosolic phospholipase A 2 enzymes (cPLA 2 ), more particularly including inhibitors of...
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7550499 |
Urea antagonists of P2Y1 receptor useful in the treatment of thrombotic conditions
The present invention provides novel ureas containing N-aryl or N-heteroaryl substituted heterocycles and analogues thereof, which are selective inhibitors of the human P2Y 1 receptor. The...
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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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7534897 |
Indole arylsulfonaimide compounds exhibiting PGD 2 receptor antagonism
A compound having CRTH2 receptor antagonism, represented by the following formula (I). The compound is useful for the treatment of allergic diseases having a relation to eosinophils and the like. ...
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7534809 |
Phospho-indoles as HIV inhibitors
3-phosphoindole compounds for the treatment of retroviral infections, and particularly for HIV, are described. Also included are compositions comprising the 3-phosphoindole derivatives alone or in...
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7531670 |
Methods for treating cognitive/attention deficit disorders using tetrahydroindolone analogues and derivatives
Methods for treating cognitive/attention deficit disorders in general using tetrahydroindolone derivatives and analogues, particularly tetrahydroindolone derivatives or analogues in which the...
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7524863 |
Sulfonylaminovalerolactams and derivatives thereof as factor Xa inhibitors
The present application describes sulfonylaminovalerolactams and derivatives thereof of Formula I:
or pharmaceutically acceptable salt forms thereof, wherein ring G is a mono- or bicyclic...
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7524839 |
Compounds, their use and preparation
The invention-provides 2, 3-, 4- or 5-substituted-N1-(arylsulfonyl)indole and (heteroaryl)indole compounds of the general formula (I):
in which Ar, R 2 , R 3 , R 4 and R 5 are as defined in...
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7524516 |
Corrosion inhibiting mildew remover kit
The corrosion inhibiting mildew remover kit includes a premeasured amount of sodium perborate, a premeasured amount of a liquid inhibitor and a premeasured amount of a liquid blend. The premeasured...
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7521472 |
Crystal of two-ring heterocyclic sulfonamide compound
Novel β-type crystal of N-(3-chloro-1H-indol-7-yl)-4-sulfamoylbenzenesulfonamide of the formula: characterized in, for example, that in powder X-ray diffractometry, it has a diffraction peak at a...
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7517906 |
Dimeric IAP inhibitors
Molecular mimics of Smac are capable of modulating apoptosis through their interaction with cellular IAPs (inhibitor of apoptosis proteins). The mimetics are based on a monomer or dimer of the...
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7511072 |
7-amido-isoindolyl compounds and methods of its use
The invention encompasses 7-amido-isoindolyl compounds and methods of using these compounds and compositions in mammals for treatment, prevention or management of various diseases and disorders....
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7507758 |
4-alkyl-/4-alkenyl-/4-alkynyl methyl/-1-aryl-cyclohexylamine compounds
4-alkyl/4-alkenyl/4-alkynyl methyl/-1-arylcyclohexylamine compounds corresponding to the formula I
a method for producing them, pharmaceutical compositions containing them, and methods of using...
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7504431 |
Sulfonyl amide inhibitors of calcium channel function
Compounds of formula I
its stereoisomers, solvates, and salts, thereof, wherein: a, b, c, d, f, n, m and Ra are defined herein are are inhibitors of calcium channel function, and are useful in...
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7504427 |
Fluoroalkoxy-substituted 1,3-dihydro-isoindolyl compounds and their pharmaceutical uses
The invention encompasses novel compounds, pharmaceutically acceptable salts, hydrates, solvates, clathrates, enantiomers, diastereomers, racemates, or mixtures of stereoisomers thereof,...
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7504401 |
Anti-cancer agents and uses thereof
The present invention is in the area of novel compounds and salts thereof, their syntheses, and their use as anti-cancer agents. The compounds include compounds of Formula I:
and solvates,...
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7494670 |
Composition and process for removing and preventing mildew and fungal growth
This invention comprises a composition and the process of using the composition for removing and preventing mold, mildew, and fungal growth. The composition comprises at least one alkali metal...
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7491831 |
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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7488749 |
Therapy of diseases of the eye, the inner ear and the central nervous system
The present invention relates to 5,6-dihydroxyindole (DHI), 5,6-dihydroxyindole-2-carboxylic acid (DHICA) and/or 5-S-cysteinyldopa (CD) as medicaments, as well as their use, and the use of...
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7488468 |
Near infrared fluorescent contrast agent and fluorescence imaging
A near infrared fluorescent contrast agent comprising a compound having three or more sulfonic acid groups in a molecule, and a method of fluorescence imaging comprising introducing the near...
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7485651 |
Compounds with activity on muscarinic receptors
Compounds and methods are provided for the alleviation or treatment of diseases or conditions in which modification of muscarinic m1 receptor activity has a beneficial effect. In the method, a...
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7485641 |
Substituted 3-amino-pyrrolidino-4-lactams
The invention provides compounds of formula (1),
and the pharmaceutically acceptable salt thereof, wherein R 1 , n and R 2 are as described herein; compositions thereof; and uses thereof.
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7482472 |
Substituted isoindoles and their use
The invention relates to coagulation of the blood. Disclosed are novel compounds of formula (I),
a method for the production of these compounds, pharmaceutical compositions containing them, and...
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7476690 |
Thio-substituted tricyclic and bicyclic aromatic methanesulfinyl derivatives
The present invention is related to chemical compositions, processes for the preparation thereof and uses of the composition. Particularly, the present invention relates to compositions of...
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7476676 |
Methods for increasing bone formation using inhibitors of glycogen synthase kinase-3β
This invention relates to the use of inhibitors of glycogen synthase kinase-3β to increase bone formation.
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7462640 |
Indol-6yl sulfonamide derivatives, their preparation and their use as 5-HT-6 as modulators
The present invention refers to new sulfonamide derivatives, of general formula (Ia, Ib, Ic) optionally in form of one of their stereoisomers, preferably enantiomers or diastereomers, their...
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7459585 |
Benzene derivatives and pharmaceutical use thereof
The present invention provides an AP-1 activation inhibitor, NF-kappa B activation inhibitor, inflammatory cytokine production inhibitor, matrix metalloprotease production inhibitor, inflammatory...
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7459478 |
Substituted dihydropyrano indole-3,4-dione derivatives as inhibitors of plasminogen activator inhibitor-1 (PAI-1)
Compounds of formula (I) and II) are provided
wherein: X is an alkali metal or a basic amine moiety; R 1 is alkyl, cycloalkyl, —CH 2 -cycloalkyl, pyridinyl, —CH 2 -pyridinyl, phenyl or...
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7456209 |
IAP binding compounds
IAP binding molecules and compositions including these are disclosed. The IAP binding molecules interact with IAPs (inhibitor of apoptosis proteins) in cells and may be used to modify apoptosis in...
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