Class 544/122 - 1,3-Diazine ring

Subclass of Class 544 - Organic compounds -- part of the class 532-570 series
Definition: Compounds in which the nitrogen atoms of the additional
No. of patents: 447
Last issue date: 02/14/2012

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Number	Title	Issue Date
8114989	Pyrazolylaminopyrimidine derivatives useful as tyrosine kinase inhibitors This invention relates to novel compounds having the formula (I): and to their pharmaceutical compositions and to their methods of use. These novel compounds provide a treatment for cancer. ...	02/14/2012
8030483	Stereoisomerically enriched 3-aminocarbonyl bicycloheptene pyrimidinediamine compounds and their uses The present invention provides stereoisomers and stereoisomeric mixtures of 3-amino carbonyl-bicycloheptene-2,4-pyrimidinediamine compounds having antiproliferative activity, compositions comprising the compounds and methods of using the compounds to inhibit cellula...	10/04/2011
7592450	Piperazinyl-, piperidinyl- and morpholinyl-derivatives as inhibitors of histone deacetylase This invention comprises the novel compounds of formula (I) wherein t, R1, R2, L, Q, X, Y, Z and (a) have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use ...	09/22/2009
7442697	4-imidazolyl substituted pyrimidine derivatives with CDK inhibitory activity Compounds of the formula (I): wherein R1, R2, R3, R4, R5 and p are as defined within and a pharmaceutically acceptable salts and in vivo hydrolysable esters are described. Also described are processes for their ...	10/28/2008
7442699	Anilinopyrimidine derivatives as IKK inhibitors and compositions and methods related thereto Compounds having activity as inhibitors of IKK are disclosed, particularly IKK-2. The compounds of this invention are anilinopyrimidine derivatives having the following structure: wherein R1 and R6 are...	10/28/2008
7442698	Substituted 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
7432260	Pyrimidine 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
7427618	Ethynyl derivatives as factor Xa inhibitors Novel compounds of the formula (I), in which R1, R2, R3, X and Y have the meaning indicated in Patent claim 1, are inhibitors of coagulation factor Xa and can be employed for the prophylaxis and/or therapy of thromboembolic di...	09/23/2008
7427626	2-Anilino-4-(imidazol-5-yl)-pyrimidine derivatives and their use as cdk (cdk2) inhibitors Compounds of the formula (I), and pharmaceutically acceptable salts and in vivo hydrolysable esters thereof are described. Also described are processes for their preparation and their use as medicaments, particularly medicaments for producing a cell cycle inhibitory...	09/23/2008
7414046	Gyrase 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
7390815	Pyrazole compounds useful as protein kinase inhibitors This invention describes novel pyrazole compounds of formula II: wherein Ring C is selected from a phenyl, pyridinyl, pyrimidinyl, pyridazinyl, pyrazinyl, or 1,2,4-triazinyl ring, and R2, R2′, R...	06/24/2008
7365069	Pyrimidone derivatives The present invention relates to novel pyrimidones 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 pharmaceutical...	04/29/2008
RE40245	Gyrase 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 relates ...	04/15/2008
7351700	Aminomethylpyrimidines as allosteric enhancers of the GABA receptors The present invention relates to compounds of formula wherein X is —S— or —NH—; R3/R4 together with the N-atom to which they are attached for...	04/01/2008
7323464	Pyridine and pyrimidine derivatives Compounds of formula (1) are described in which Ra and Rb is each independently a hydrogen atom or a group Rc, or Ra and Rb together form an oxo (═O) or thio (═S) group; X is a N atom or an optionally substi...	01/29/2008
7320989	Pyridine, pyrimidine, quinoline, quinazoline, and naphthalene urotensin-II receptor antagonists The present invention relates to urotensin II receptor antagonists, pharmaceutical compositions containing them and their use. ...	01/22/2008
7320975	2-(2-pyridyl)-5-phenyl-6-aminopyrimidine, method and intermediate products for the production and use thereof for combating noxious fungi The invention relates to 2-(2-pyridyl)-5-phenyl-6-aminopyrimidines of formula I, wherein the substitutes and the index have the following meaning: R1 represents halogen, hydroxy, hyano, hxo, nitro, amino, mercapto, alkyl, halogenalkyl, alkenyl, alkinyl, c...	01/22/2008
7312216	N-phenyl-2-pyrimidine-amine derivatives The invention relates to N-phenyl-2-pyrimidine-amine derivatives of formula I wherein the substituents are defined as indicated in the description, to processes for the preparation thereof, to medicaments compris...	12/25/2007
7312215	Benzimidazole C-2 heterocycles as kinase inhibitors Benzimidazole derivatives having the general formula I are provided. These compounds are useful as tyrosine kinase inhibitors, especially for the treatment of cancer. ...	12/25/2007
7304061	Heterocyclic inhibitors of ERK2 and uses thereof Described herein are compounds that are useful as protein kinase inhibitors having the formula: wherein A1, A2, TmR1, X, R2, R3, R9, R	12/04/2007
7282504	Kinase inhibitors The invention relates to inhibitors of kinases, compositions comprising the inhibitors, and methods of using the inhibitors and inhibitor compositions. The inhibitors and compositions comprising them are useful for treating disease or disease symptoms. The invention...	10/16/2007
7279576	Anti-cancer medicaments Novel compounds and methods of using those compounds for the treatment of oncological conditions are provided. In a preferred embodiment, modulation of the activation states of abl or bcr-abl α-kinase proteins comprises the step of contacting the kinase proteins wi...	10/09/2007
7279475	Fluorinated di-aryl urea compounds Disclosed are compounds of formula(I): wherein R1, R2, W and X of formula(I) are defined herein. The compounds inhibit production of cytokines involved in inflammatory processes and are thus...	10/09/2007
7276502	Thiazoles useful as inhibitors of protein kinases The present invention relates to compounds useful of inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, ...	10/02/2007
7265122	Pyridine, pyrimidine, quinoline, quinazoline, and naphthalene urotensin-II receptor antagonists The present invention relates to urotensin II receptor antagonists, pharmaceutical compositions containing them and their use. ...	09/04/2007
7262200	Indazolinone compositions useful as kinase inhibitors The present invention provides compounds of formula I: These compounds, and pharmaceutically acceptable compositions thereof, are useful generally as kinase inhibitors, particularly as inhibitors of PRAK, GSK3, ERK...	08/28/2007
7259162	Benzazole derivatives and their use as JNK modulators The present invention is related to benzazole derivatives notably for use as pharmaceutically active compounds, as well as to pharmaceutical formulations containing such benzazole derivatives. Said benzazole derivatives are efficient modulators of the JNK pathway, t...	08/21/2007
7235551	1,5-disubstituted-3,4-dihydro-1h-pyrimido[4,5-d]pyrimidin-2-one compounds and their use in treating csbp/p38 kinase mediated diseases Novel substituted pyrimidol[4,5-d]pyrimidin-2-one compounds and compositions for use in therapy as CSBP/p38 kinase inhibitors. ...	06/26/2007
7226919	Compositions useful as inhibitors of protein kinases The present invention provides a compound of formula (I): or a pharmaceutically acceptable salt thereof. These compounds are inhibitors of protein kinases, particularly inhibitors of GSK-...	06/05/2007
7223760	Substituted triazole compounds Novel substituted triazole compounds and compositions for use in therapy as CSBP/p38 kinase inhibitors. ...	05/29/2007
7220736	Pyrimidine compounds A cyclic compound of the formula (I) or a pharmacologically acceptable salt thereof, wherein X is ═CH— or ═N—, Y is —NH—, —NR4—, —S—, —O—, —CH═N—,...	05/22/2007
7217712	4-Substituted-5-cyano-1H-pyrimidin-6-(thi)ones as GSK-3 inhibitors The present invention relates to compounds of formula I that are useful as GSK-3 inhibitors. The invention also relates to methods of using compounds of formula I or pharmaceutical compositions comprising compounds of formula I to inhibit GSK-3 activity. The inventi...	05/15/2007
7217713	N-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	05/15/2007
7205297	Substituted 5-alkynyl pyrimidines having neurotrophic activity The present invention relates to a series of novel substituted 5-alkynyl pyrimidines, pharmaceutical compositions which contain them, methods for their preparation, and their use in therapy, particularly in the treatment of neurodegenerative or other neurological di...	04/17/2007
7199120	Pyrazolo-pyridine derivatives as antiherpes agents The present invention provides compounds of formula (I): wherein all variables are as defined herein, pharmaceutical compositions containing the same, processes for preparing the same and their use as pharmaceuti...	04/03/2007
7189717	Medicinal compositions promoting bowel movement The present invention provides a medicament having a gentle but strong defecation-promoting action without causing diarrhea. That is, it provides a defecation-promoting agent comprising a compound having an adenosine A2 receptor antagonism, preferably an ...	03/13/2007
7186714	Imidazo[1,2-α]pyridine derivatives for the prophylaxis and treatment of herpes viral infections The present invention provides compounds of formula (I) wherein all variables are as defined herein, pharmaceutical compositions containing the same, processes for preparing the same and their use as pharmaceutical agents ...	03/06/2007
7186732	Non-imidazole aryloxyalkylamines Substituted aryloxyalkylamines of formula (I), compositions containing them, and methods of making and using them to treat histamine-mediated conditions. ...	03/06/2007
7179806	Δ1-pyrrolines used as pesticides The invention relates to novel Δ1-pyrrolines of the formula (I) in which R1, R2, R3, m, and Q have the meanings given in the disclosure, to a plurality of processes fo...	02/20/2007
7173029	Fused heteroaryl derivatives The present invention provides a pharmaceutical composition which is useful as a phosphatidylinositol 3 kinase (PI3K) inhibitor and an antitumor agent, and it provides a novel bicyclic or tricyclic fused heteroaryl derivative or a salt thereof which possesses an exc...	02/06/2007

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Class 544/122 - 1,3-Diazine ring