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US20090286801 |
CARBONYLATED (AZA) CYCLOHEXANES AS DOPAMINE D3 RECEPTOR LIGANDS
The invention relates to compounds of the general formula (I): to the process for preparing them, and to the use thereof as a therapeutic agent.
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US20090281088 |
BICYCLIC NITROIMIDAZOLE-SUBSTITUTED PHENYL OXAZOLIDINONES
The current invention provides a series of bicyclic nitroimidazole-substituted phenyl oxazolidinones in which a bicyclic nitroimidazole pharmacophore is covalently bonded to a phenyl oxazolidinone,...
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US20090275567 |
2-HETEROCYCLOAMINO-4-IMIDAZOLYLPYRIMIDINES AS AGENTS FOR THE INHIBITION OF CELL PROLIFERATION
Compounds of formula (I):
which possess cell-cycle inhibitory activity are described.
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US20090270419 |
COMBINATIONS OF CLASS-I SPECIFIC HISTONE DEACETYLASE INHIBITORS WITH PROTEASOME INHIBITORS
The present invention is concerned with combinations of a proteasome inhibitor and a class-I specific histone deacetylase inhibitor for inhibiting the growth of tumor cells, useful in the treatment...
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US20090270403 |
NOVEL 1,4-DIAZA-BICYCLO[3.2.2]NONYL PYRIMIDINYL DERIVATIVE AND ITS MEDICAL USE
This invention relates to a novel 1,4-diaza-bicyclo[3.2.2]nonyl pyrimidinyl derivative and its use in the manufacture of pharmaceutical compositions. The compound of the invention is found to be a...
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US20090270336 |
Piperazine derivatives
This invention relates to novel compounds that are piperazine derivatives, and pharmaceutically acceptable salts thereof. More specifically, the invention relates to novel piperazine compounds that...
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US20090269420 |
SUBSTITUTED DIHYDROPYRAZOLONES AND THEIR USE
The present application relates to novel substituted dihydropyrazolone derivatives, processes for their preparation, their use for treatment and/or prophylaxis of diseases and their use for the...
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US20090264649 |
DIARYLAMINE-CONTAINING COMPOUNDS AND COMPOSITIONS, AND THEIR USE AS MODULATORS OF C-KIT RECEPTORS
Described herein are compounds that include a diarylamine structural feature. Also described herein are methods for making such compounds, methods for using such compounds to modulate the activity...
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US20090264438 |
Polymorphic forms of imatinib mesylate and processes for preparation of novel crystalline forms as well as amorphous and form alpha
Solvates and crystalline forms of imatinib mesylate are described. Further, methods for preparing such solvates and crystalline forms of imatinib mesylate are described.
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US20090264437 |
4-Piperazinyl-Pyrimidine Compounds Suitable for Treating Disorders that Respond to Modulation of the Dopamine D3 Receptor
The present invention relates to novel 4-piperazinylpyrimidine compounds. The compounds possess valuable therapeutic properties and are suitable, in particular, for treating diseases that respond...
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US20090264425 |
CHEMICAL COMPOUNDS
This invention relates to biaryl ether derivatives of formula (I)
wherein R 1 , R 3 , R 4 , X, W, Y and m are defined in the description, and to compositions containing them and the uses of such...
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US20090264339 |
Heterocyclic Compounds
This invention relates to heterocyclic compounds of the formulas shown in the specification. It also relates to methods for treating inflammatory diseases or immune diseases, developmental or...
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US20090239879 |
N-OXIDES OF N-PHENYL-2-PYRIMIDINE-AMINE DERIVATIVES
The invention relates to N-phenyl-2-pyrimidine-amine derivatives derivatives in which at least one nitrogen atom carries an oxygen atom to form the corresponding N-oxides, to processes for the...
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US20090233944 |
PYRAZINE-2-CARBOXYAMIDE DERIVATIVES
The present invention is concerned with novel pyrazine 2-carboxyamide derivatives of formula (I)
wherein R 1 , R 2 and R 3 are as defined in the specification. These compounds are useful for...
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US20090233896 |
Inhibitors of checkpoint kinases
The instant invention provides for compounds which comprise substituted pyridyl aminothiazoles that inhibit CHK1 activity. The invention also provides for compositions comprising such inhibitory...
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US20090221602 |
PROCESSES FOR PREPARING SUBSTITUTED PYRIMIDINES
The present invention provides a facile process for the preparation of tri- and tetra-substituted pyrimidines. The process is useful for preparing inhibitors of protein kinases, especially Aurora...
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US20090215759 |
MODULATORS FOR AMYLOID BETA
The invention relates to compounds of formula
wherein the substituents are as described in claim 1 . Compounds of formula I are modulators for amyloid beta and thus, they may be useful for the...
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US20090209524 |
Novel Compounds
The present invention provides compounds of formula (1)
wherein R 1 , R 2 , R 3 and R 4 are as defined in the specification, and pharmaceutically acceptable salts thereof, as well as processes...
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US20090203906 |
NOVEL AMINODICARBOXYLIC ACID DERIVATIVES HAVING PHARMACEUTICAL PROPERTIES
The invention relates to compounds of formulae (II), (IV), and (VI) as shown below,
wherein the several variable groups are as defined in the specification and claims. Processes for making these...
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US20090203696 |
Aryl- and Heteroaryl-Ethyl-Acylguanidine Derivatives, Their Preparation and Their Application in Therapeutics
Disclosed are compounds according to formula (I):
wherein A, Q, X, Y, Z, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 and R11 are as defined herein. The disclosure also relates to pharmaceutical...
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US20090203673 |
4-HETEROCYCLOALKYLPYRI(MI)DINES, PROCESS FOR THE PREPARATION THEREOF AND THEIR USE AS MEDICAMENTS
The present invention encompasses compounds of general Formula (I) wherein X and R 1 to R 3 are defined as in claim 1 , which are suitable for the treatment of diseases characterised by...
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US20090197887 |
PIPERAZINYLPIPERIDINE DERIVATIVES AS CHEMOKINE RECEPTOR ANTAGONISTS
The present invention relates to compounds of Formula I:
wherein variable substituents are defined herein, that modulate the activity of or bind to chemokine receptors such as CCR5. In some...
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US20090197877 |
Antibacterial Compositions
Compounds of formula (I) have antibacterial activity: wherein: m is 0 or 1; Q is hydrogen or cyclopropyl; AIk is an optionally substituted, divalent C 1 -C 6 alkylene, alkenylene or alkynylene...
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US20090197864 |
Furo- and Thieno [3,2-c] Pyridines
Furo[3,2-c]Pyridine and Thieno[3,2-c]pyridine compounds of Formula I, and pharmaceutically acceptable salts thereof, preparation, intermediates, pharmaceutical compositions, and use, such as in...
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US20090192146 |
SUBSTITUTED ORGANOSULFUR COMPOUNDS AND METHODS OF USING THEREOF
The present invention provides substituted di-, tri-, tetra- and penta-sulfide compounds and compositions, and methods of using the same for the treatment and/or prevention of a cell proliferative...
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US20090181977 |
Anhydrous Amorphous Imatinib Mesylate
Described is a highly stable amorphous form of imatinib mesylate having a water content of less than 0.5 percent by weight, based on the total weight of the amorphous imatinib mesylate, (anhydrous...
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US20090181943 |
Inhibitors of Histone Deacetylase
This invention relates to compounds for the inhibition of histone deacetylase. More particularly, the invention provides for compounds of formula compounds of the Formula (I)
and N-oxides,...
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US20090176781 |
Acetylenic Heteroaryl Compounds
This invention relates to compounds of the general formula:
in which the variable groups are as defined herein, and to their preparation and use.
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US20090163508 |
AMIDE COMPOUND
An object of the present invention is to provide a novel fused-ring compound which has a FAAH inhibitory effect and is useful as an analgesic. The present invention relates to a compound...
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US20090163469 |
Organic Compounds
The present invention relates to compounds of formula I
and its salts, wherein the substituents are as defined in the description, to compositions and use of the compounds in the treatment of...
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US20090163467 |
New compounds
The present invention encompasses compounds of general formula (1)
wherein
R 1 , R 2 , R 4 , X, m, n and p are defined as in claim 1 , which are suitable for the treatment of diseases...
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US20090149650 |
PROCESS FOR PREPARING 2-AMINOTHIAZOLE-5-AROMATIC CARBOXAMIDES AS KINASE INHIBITORS
The invention relates to processes for preparing compounds having the formula,
and crystalline forms thereof, wherein Ar is aryl or heteroaryl, L is an optional alkylene linker, and R 2 , R 3 ,...
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US20090149466 |
INHIBITORS OF STEAROYL-COA DESATURASE
Provided herein are compounds of the formula (I):
as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and...
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US20090149450 |
SUBSTITUTED IMIDAZOHETEROCYCLES
The present invention provides substituted imidazoheterocyclic compounds having the structure of formula I
Also provided are pharmaceutically acceptable salts, acid salts, hydrates, solvates and...
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US20090149399 |
HETEROCYCLIC KINASE INHIBITORS
This invention relates to novel 2-{6-[4-(2-hydroxy-ethyl)-piperazin-1-yl]-2-methyl-pyrimidin
-4-ylamino}-thiazole-5-carboxylic acid (2-chloro-6-methyl-phenyl)-amide derivatives, and...
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US20090143401 |
Pyridine and Pyrimidine Derivatives as Inhibitors of Histone Deacetylase
This invention comprises the novel compounds of formula (I)
wherein R 1 , R 2 , R 3 and X have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation,...
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US20090143361 |
Pyrido[3,2-E]Pyrazines, Process For Preparing The Same, And Their Use As Inhibitors Of Phosphodiesterase 10
The invention relates to pyrido[3,2-e]pyrazines, to processes for preparing them, to pharmaceutical compositions which comprise these compounds and to the pharmaceutical use of these compounds,...
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US20090137588 |
HETEROARYL COMPOUNDS AND USES THEREOF
The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.
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US20090131436 |
Pyrimidine Derivatives
Novel pyrimidine derivatives of formula (I) to processes for their production, their use as pharmaceuticals and to pharmaceutical compositions comprising them.
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US20090131382 |
TREATMENT OF RHEUMATOID ARTHRITIS USING IMATINIB
4-(4-methylpiperazin-1-ylmethyl)-N—[4-methyl-3-(4-pyridin-
3-yl)pyrimidin-2-ylamino)phenyl]-benzamide of the formula I
or a pharmaceutically acceptable salt thereof can be used in the...
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US20090118501 |
Dicycloalkyl Urea Glucokinase Activators
Dicycloalkyl urea glucokinase activators compounds are glucokinase inhibitors useful for the treatment of diabetes.
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US20090118297 |
POLYMORPHS OF DASATINIB AND PROCESS FOR PREPARATION THEREOF
Provided is dasatinib, solvates thereof and their crystalline forms, methods for their preparation, and pharmaceutical compositions thereof.
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US20090118284 |
Novel compounds that are ERK inhibitors
Disclosed are the ERK inhibitors of formula 1.0:
and the pharmaceutically acceptable salts, esters and solvates thereof. Q is a piperidine or piperazine ring that can have a bridge or a fused...
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US20090111789 |
CHIRAL CIS-IMIDAZOLINES
There are provided compounds of the formula
or the pharmaceutically acceptable salts thereof, wherein X, Y, Z, V 1 , V 2 , R 1 , R 2 , R 3 , R 4 and R 5 are herein described. These compounds...
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US20090087489 |
IMATINIB COMPOSITIONS
The invention relates to a pharmaceutical composition, preferably a tablet, containing about 23-29% w/w imatinib and processes for its preparation.
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US20090082361 |
DEUTERIUM-ENRICHED IMATINIB
The present application describes deuterium-enriched imatinib, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.
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US20090076025 |
DEUTERIUM-ENRICHED DASATINIB
The present application describes deuterium-enriched dasatinib, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.
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US20090076020 |
Cyclopropyl Amide Derivatives 978
Disclosed herein is at least one cyclopropyl amide derivative, at least one pharmaceutical composition comprising at least one cyclopropyl amide derivative disclosed herein, and at least one method...
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US20090076006 |
HSP90 INHIBITORS CONTAINING A ZINC BINDING MOIETY
The present invention relates to HSP90 inhibitors containing a zinc binding moiety and their use in the treatment of cell proliferative diseases such as cancer. The said derivatives may further act...
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US20090069305 |
Substituted nitrogen-containing heteroaryl derivatives useful as modulators of the histamine H4 receptor
The present invention relates to substituted nitrogen-containing heteroaryl derivatives, pharmaceutical compositions containing them, and methods of using any of these derivatives and compositions...
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