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Class 514/252.14 - The additional hetero ring is a 1,3 diazine ring


Subclass of Class 514 - Drug, bio-affecting and body treating compositions
Definition: Subject matter wherein the additional hetero ring consists
No. of patents: 385
Last issue date: 02/14/2012


1                    
NumberTitleIssue Date
8114876Pyridine and pyrimidine derivatives as inhibitors of histone deacetylase
This invention comprises the novel compounds of formula (I) wherein R1, R2, R3 and X have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compo...
02/14/2012
8114875Substituted N-heterocyclic compounds and their use as dopamine Dreceptor ligands
The invention relates to substituted N-heterocyclic compounds of general formula (I.A) and to the tautomers of the compounds the physiologically acceptable salts of the compounds and the physiologically acceptable salts of ...
02/14/2012
8101616Pyridine and pyrimidine derivatives as inhibitors of histone deacetylase
This invention comprises the novel compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9 and X have defined me...
01/24/2012
81016151,4-diaryl-dihydropyrimidin-2-ones and their use as human neutrophil elastase inhibitors
The invention relates to novel heterocyclic derivatives of the general formula (I), processes for their preparation, and their use in medicaments, especially for the treatment of chronic obstructive pulmonary diseases, acute coronary syndrome, acute myocardial infar...
01/24/2012
8058276Heterobicyclic carboxamides as inhibitors for kinases
The invention relates to novel organic compounds of formula (I) and their use in the treatment of the animal or human body, to pharmaceutical compositions comprising a compound of formula (I) and to the use of a compound of formula (I) for the preparation of pharmac...
11/15/2011
80440552-phenyl-6-aminocarbonyl-pyrimidine derivatives and their use as P2Y12 receptor
The invention relates to 2-phenyl-6-aminocarbonyl-pyrimidine derivatives and their use as P2Y12 receptor antagonists in the treatment and/or prevention and/or treatment of peripheral vascular, of visceral-, hepatic- and renal-vascular, of cardiovascular a...
10/25/2011
8044054Stereoisomerically enriched 3-aminocarbonyl bicycloheptene pyrimidinediamine compounds and their uses
The present invention provides stereoisomers and stereoisomeric mixtures of 3-aminocarbonyl-bicycloheptene-2,4-pyrimidinediamine compounds having antiproliferative activity, compositions comprising the compounds and methods of using the compounds to inhibit cellular...
10/25/2011
7960386Pyridin-2-one compounds and their use as modulators of the dopamine D3 receptor
The invention relates to pyridin-2-one compounds of general formula (I) in which A represents a 4- to 6-membered hydrocarbon chain that can have 1 or 2 methyl groups as substituents, wherein 1 or 2 carbon atoms...
06/14/2011
7910590Cyclic amine bace-1 inhibitors having a heterocyclic substituent
Disclosed are novel compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R1 is
03/22/2011
7897605Pyrimidine compounds
The present invention relates to substituted pyrimidines of formula I, their preparation, pharmaceutical compositions containing them and their use as inhibitors of cyclin-dependent kinases (CDKs) and hence their use in the treatment of proliferative disorders and/o...
03/01/2011
7888360Pyridine and pyrimidine derivatives as inhibitors of histone deacetylase
This invention comprises the novel compounds of formula (I) wherein R1, R2, R3, X, Y and Z have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation,...
02/15/2011
7884105Squaric acid derivatives as inhibitors of histone deacetylase
This invention comprises the novel compounds of formula (I) wherein R1, R2 and X have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions contain...
02/08/2011
7825121Piperazine derivatives useful as CCR5 antagonists
The use of CCR5 antagonists of the formula or a pharmaceutically acceptable salt thereof, wherein R is optionally substituted phenyl, pyridyl, thiophenyl or naphthyl; R
11/02/2010
7799788Method of treating chronic myelogenous leukemia cells
Here, the inventors disclose the treatment of imatinib mesylate resistant chronic myelogenous leukemia cells with a cotreatment of vorinostat (SAHA, suberoylanilide hydroxamic acid) and dasatinib, a dual Abl/Src kinase (TK) inhibitor. Combined treatment of cultured ...
09/21/2010
7767679Sulfonylamino-derivatives as novel inhibitors of histone deacetylase
This invention comprises the novel compounds of formula (I) wherein n, m, t, R1, R2, R3, R4, R5, L, Q, X, Y, Z and have defi...
08/03/2010
7767680Ion channel modulators and methods of use
In general, the invention relates to novel 4-phenylpyrimidine compounds useful as ion channel modulators. It has now been found that compounds of this invention, and pharmaceutically acceptable compositions thereof, are useful as inhibitors of voltage-gated sodium c...
08/03/2010
7763619Compounds with 5-HTactivity useful for treating disorders of the outer retina
Compositions and methods for treating disorders of the outer retina with compounds with 5-HT1A agonist activity are disclosed. ...
07/27/2010
7759350Pyrimidine carboxamides
The present invention relates to novel compounds of the general formula (I), their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their hydrates, their solvates, their pharmaceutically acceptable salts and compositions, th...
07/20/2010
7723339Combination comprising a signal transduction inhibitor and an epothilone derivative
The present invention relates to a combination comprising N-{5-[4-(4-methyl-piperazino-methyl) -benzoylamido]-2-methylphenyl}-4-(3-pyridyl)-2-pyrimidine-amine and an epothiione derivative; pharmaceutical composition comprising said combination; method of treatment c...
05/25/2010
7709487Sulfonyl-derivatives as novel inhibitors of histone deacetylase
This invention comprises the novel compounds of formula (I) wherein n, m, t, R1, R2, R3, R4, L, Q, X, Y, Z and have defined meanings, h...
05/04/2010
7652013Inhibitors 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 the pharmaceutical compositi...
01/26/2010
7625903Anthranilamide inhibitors of Aurora kinase
The present invention relates to a compound represented by the following formula: or a pharmaceutically acceptable salt thereof; where R1, R2, R3, R4, r and s are as ...
12/01/2009
7615553Inhibitors of histone deacetylase
This invention comprises the novel compounds of formula (I) wherein n, R1, R2, R3, R4, Q, X, Y, Z and have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions contain...
11/10/2009
7598250Cyclic amine BACE-1 inhibitors having a heterocyclic substituent
Disclosed are novel compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R1 is
10/06/2009
75826347-substituted imidazo[4,5-c]pyridine antagonists of gonadotropin releasing hormone receptor
The present invention relates to Gonadotropin Releasing Hormone (GnRH, also known as Luteinizing Hormone Releasing Hormone) receptor antagonists. ...
09/01/2009
7566717Substituted heterocyclic compounds
Disclosed are novel heterocyclic compounds having the structure which are useful for the treatment of various disease states, in particular cardiovascular diseases such as atrial and ventricular arrhythmias, intermittent cl...
07/28/2009
75477024-amino-quinazolines
Quinazolines of the formula (I) in which R, R1, R2, R3, R4 and Y have the meaning indicated in Patent claim 1, and their salts or solvates as glycoprotein 1bIX antagonists. ...
06/16/2009
75381134-substituted imidazo[4,5-c]pyridine antagonists of gonadotropin releasing hormone receptor
The present invention relates to Gonadotropin Releasing Hormone (GnRH, also known as Luteinizing Hormone Releasing Hormone) receptor antagonists. ...
05/26/2009
7534796Imidazo[4,5-b]pyridine antagonists of gonadotropin releasing hormone receptor
The present invention relates to Gonadotropin Releasing Hormone (GnRH, also known as Luteinizing Hormone Releasing Hormone) receptor antagonists. ...
05/19/2009
7511044Vanilloid receptor ligands and their use in treatments
Pyrimidine ethers and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascular syndromes, tension headache, general inflammation, arthritis...
03/31/2009
7501417Aminocarbonyl-derivatives as novel inhibitors of histone deacetylase
This invention comprises the novel compounds of formula (I) wherein n, R1, R2, R3, R4, L, Q, X, Y, Z and have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions cont...
03/10/2009
7485644N-{'4-substituted piperazine-1-sulfonylmethylalkyl}-n-hydroxyfomamide compounds as metalloproteinase inhibitors
The invention provides compounds of formula (I): or a pharmaceutically acceptable salt, prodrug or solvate thereof, wherein ring B represents a monocyclic aryl ring having six ring atoms or a monocyclic heteroaryl ring having up to six ring atoms and containing one ...
02/03/2009
7459455Pyrimidine compounds
Pyrimidine derivatives, which are useful as TIE-2 and/or VEGFR-2 inhibitors are described herein. The described invention also includes methods of making such pyrimidine derivatives as well as methods of using the same in the treatment of hyperproliferative diseases...
12/02/2008
7442698Substituted heterocyclic compounds and methods of use
The present invention relates to pyrimidine or pyridine carbamate compounds having the general Formula I: and pharmaceutically acceptable salts or derivatives thereof. Also included are methods of treatment of various disea...
10/28/2008
7435734N-substituted hydroxypyrimidinone carboxamide inhibitors of HIV integrase
N-substituted 5-hydroxypyrimidin-6-one-4-carboxamides of formula: are described as inhibitors of HIV integrase and inhibitors of HIV replication, wherein R1, R2, R3 and R4 are def...
10/14/2008
7432260Pyrimidine compounds
The present invention relates to substituted pyrimidines of formula I, their preparation, pharmaceutical compositions containing them and their use as inhibitors of cyclin-dependent kinases (CDKs) and hence their use in the treatment of proliferative disorders and/o...
10/07/2008
7419980Fused-aryl and heteroaryl derivatives and methods of their use
The present invention is directed to fused-aryl and heteroaryl derivatives, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions ameliorated by monoamine reuptake including, inter alia, vasomotor symptoms...
09/02/2008
7414046Gyrase inhibitors and uses thereof
The present invention relates to compounds of the formula I: or a pharmaceutically acceptable derivative or prodrug thereof. The compounds are useful as inhibitors of bacterial gyrase activity. The present invention also re...
08/19/2008
7384944Piperazine derivatives useful as CCR5 antagonists
The use of CCR5 antagonists of the formula or a pharmaceutically acceptable salt thereof, wherein R is optionally substituted phenyl, pyridyl, thiophenyl or naphthyl; R
06/10/2008
7381719Diaryl ethers as opioid receptor antagonist
A compound of the formula (I) wherein the variables X1 to X10, R1 to R7 including R3′, E, v, y, z, A and B are as described, or a pharmaceutically acceptable salt, solvate, enantiomer, racemate, diastereomer o...
06/03/2008
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