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| Number | Title | Issue Date |
| 8410267 | Regioselective reduction of fused pyrrolocarbazoles-5,7-diones The present invention relates to a method for regioselectively reducing the maleimide compounds of formula (I). The invention also relates to C7 hydroxy lactam regioisomers of formula (II) obtainable by this method and their use for the preparation of lac... | 04/02/2013 |
| 8399668 | Process for the preparation of 5-(2-amino-pyrimidin-4-yl)-2-aryl-1H-pyrrole-3-carboxamides The present invention relates to a process for the preparation of 5-(2-amino-pyrimidin-4-yl)-2-aryl-1H-pyrrole-3-carboxamides and to the useful intermediate compounds of such process. 5-(2-Amino-pyrimidin-4-yl)-2-aryl-1H-pyrrole-3-carboxamides are described and clai... | 03/19/2013 |
| 8383813 | Fused pyrrolocarbazoles The present invention relates generally to selected fused pyrrolocarbazoles, including pharmaceutical compositions thereof and methods of treating diseases therewith. The present invention is also directed to intermediates and processes for making these fused pyrrol... | 02/26/2013 |
| 8309721 | HSP90 inhibitory carbazole derivatives, compositions containing same and use thereof The invention relates to the novel substances in Formula (I): wherein Het is a heterocycle optionally substituted by one or a plurality of radicals R1 or R′1; R is selected from the group comprising Formula (A′), (B), (C), (D), or (E), with R1 and/or R′1 selec... | 11/13/2012 |
| 8288540 | 2-heteroarylamino-pyrimidine derivatives as kinase inhibitors The invention provides compounds of Formula (I) and pharmaceutical compositions thereof, which are useful as protein kinase inhibitors, as well as methods for using such compounds to treat, ameliorate or prevent a condition associated with abnormal or deregulated ki... | 10/16/2012 |
| 8242273 | Synthesis of 4/5-pyrimidinylimidazoles via sequential functionalization of 2,4-dichloropyrimidine This invention relates to methods of making pyrimidinyl-substituted imidazole compounds by sequential substitution of the 4- and 2-chloro groups of 2,4-dichloropyrimidine, nucleophilic substitution to form pyrimidinylalkyne derivatives, oxidation to the correspondin... | 08/14/2012 |
| 8232395 | Method for producing 2-(2-aminopyrimidin-4-yl)-1H-indole-5-carboxylic acid derivatives This invention relates to a novel process for obtaining a compound of formula I: wherein the values of R1, R2, and R3 and P are as described in the specification. ... | 07/31/2012 |
| 8173808 | Substituted naphthalenyl-pyrimidine compounds The present invention relates to substituted naphthalenyl-pyrimidine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted naphthalenyl-pyrimidine compounds and methods of trea... | 05/08/2012 |
| 8168787 | Process for the preparation of imatinib and intermediates thereof A process for the preparation of 4-methyl-N3-[4-(3-pyridinyl)-2-pyrimidinyl]-1,3-benzenediamine and analogues thereof, intermediates useful for the synthesis of Imatinib, or 4-[(4-methyl-1-piperazinyl)methyl]-N-[4-methyl-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]pheny... | 05/01/2012 |
| 8163904 | Salts of 4-methyl-N-[3-(4-methyl-imidazol-1-yl)-5-trifluoromethyl-phenyl]-3-(4-pyridin-3-yl-pyrimidin-2-ylamino)-Benzamide Salts of 4-methyl-N-[3-(4-methyl-imidazol-1-yl)-5-trifluoromethyl-phenyl]-3-(4-pyridin-3-yl-pyrimidin-2-ylamino)-benzamide are prepared by various processes. ... | 04/24/2012 |
| 8134000 | Imidazolyl pyrimidine inhibitor compounds A compound of general Formula (I) having histone deacetylase (HDAC) and/or Cyclin-dependent kinase (CDK) inhibitory activity, a pharmaceutical composition comprising the compound, and a method useful to treat diseases using the compound. | 03/13/2012 |
| 8124765 | Synthesis of 4/5-pyrimidinylimidazoles via sequential functionalization of 2,4-dichloropyrimidine This invention relates to methods of making pyrimidinyl-substituted imidazole compounds by sequential substitution of the 4- and 2-chloro groups of 2,4-dichloropyrimidine, nucleophilic substitution to form pyrimidinylalkyne derivatives, oxidation to the correspondin... | 02/28/2012 |
| 8124764 | Fused heterocyclyc inhibitor compounds The present invention provides a compound of general Formula (I) having histone deacetylase (HDAC) and/or Cyclin-dependent kinase (CDK) inhibitory activity, a pharmaceutical composition comprising the compound, and a method useful to treat diseases using the compoun... | 02/28/2012 |
| 8063212 | Imidazolidinonyl aminopyrimidine compounds for the treatment of cancer The present invention provides novel imidazolidinonyl aminopyrimidine compounds believed to have clinical use for treatment of cancer through inhibiting Plk1. Formula I wherein: R1 is aminomethyl, (C1-C3 alkyl)aminomethyl, di(C1... | 11/22/2011 |
| 7977481 | Pyrimidinyl-thiophene kinase modulators The present invention provides novel pyrimidinyl-thiophene kinase modulators and methods of using the novel pyrimidinyl-thiophene kinase modulators to treat diseases mediated by kinase activity. ... | 07/12/2011 |
| 7902361 | Pyrimidin-4-yl-3, 4-thione compounds and their use in therapy The present invention relates to compounds of formula I, or pharmaceutically acceptable salts thereof, wherein R1 and R5 are each independently H, C(ORj′) or a hydrocarbyl group optionally... | 03/08/2011 |
| 7767812 | Crystals of pyrimidine compound and process for producing the same Crystals of 5-[2-amino-4-(2-furyl)pyrimidin-5-yl]-1-methylpyridin-2(1H)-one having a diffraction peak at a diffraction angle (2θ±0.2°) of 9.7° and/or 21.9° in a powder X-ray diffraction are suitable for an active ingredient of a preventing and therapeutic agent... | 08/03/2010 |
| 7674901 | Process for preparation of imatinib base An improved process for the preparation of imatinib base and its pharmaceutically acceptable acid addition salts by (a) reacting 2-methyl-5-nitroaniline with cyanamide in the presence of hydrochloric acid to obtain 1-(2-methyl-5-nitrophenyl)guanidine hydrochloride; ... | 03/09/2010 |
| 7638627 | Process of preparing imatinib and imatinib prepared thereby A process of preparing imatinib, either as the free base or as an acid addition salt, which process comprises reacting N-(2-methyl-5-aminophenyl-4-(3-pyridyl)-2-pyrimidine amine of formula (II) with a 4-(4-methyl-piperazino methyl)benzoyl halide of formula (III) in ... | 12/29/2009 |
| 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 |
| 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 |
| 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 |
| 7429593 | Utilities of amide compounds Compounds having an activity to enhance the expression of apoAI are provided, which are used as medicaments. Compounds of formula (I): in which ring A and Ar1 are independently a monocyclic or bicyclic aro... | 09/30/2008 |
| 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 |
| 7427627 | N-(4-(4-methylthiazol-5-yl) pyrimidin-2-yl)-N-phenylamines as antiproliferative compounds The present invention relates to 2-substituted 4-heteroaryl-pyrimidines, 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 suc... | 09/23/2008 |
| 7423148 | Small molecule PI 3-kinase inhibitors and methods of their use Compounds having formula I are provided where the variables have the values described herein. Pharmaceutical formulations include the compounds or pharmaceutically acceptable salts thereof and a pharmaceutically acceptable ca... | 09/09/2008 |
| 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 |
| 7396836 | Pyrimidine compound and medicinal composition thereof A compound having excellent adenosine receptor (A1, A2A, A2B receptor) antagonistic action, of the following formula, a salt thereof or a solvate of them: wherein, R1 and R2 | 07/08/2008 |
| 7396928 | Crystals of 5-[2-amino-4-(2-furyl) pyrimidin-5-yl]-1-methylpyridin-2(1H)-one and processes for preparing the same Crystals of 5-[2-amino-4-(2-furyl)pyrimidin-5-yl]-1-methylpyridin-2(1H)-one having a diffraction peak at a diffraction angle (2θ±0.2°) of 12.8°, 18.1° and/or 23.5° in a powder X-ray diffraction are excellent in stability against light, therefore are suitable f... | 07/08/2008 |
| 7388015 | N-(4-(4-methylthiazol-5-yl)pyrimidin-2-yl)-N-phenylamines as antiproliferative compounds The present invention relates to 2-substituted 4-heteroaryl-pyrimidines, 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 suc... | 06/17/2008 |
| 7371759 | HMG-CoA reductase inhibitors and method Compounds are provided having the following structure which are HMG CoA reductase inhibitors and thus are active in inhibiting cholesterol biosynthesis, modulating blood serum lipids, for example, lowering LDL cholesterol and/or increasing HDL cholesterol, and treat... | 05/13/2008 |
| 7368569 | Process for making spirolactone compounds This invention relates to a process for making spirolactone compounds analogous to formula I ... | 05/06/2008 |
| 7368455 | 6,7-Dihydro-5H-pyrazolo[1,2-a]pyrazol-1-ones which control inflammatory cytokines The present invention relates to 2-(4-fluorophenyl)-3-(2-phenoxy-pyrimidin-4-yl)-6,7-dihydro-5H-pyrazolo-[1,2-a]pyrazol-1-one, including all enantiomeric and diasteriomeric forms and pharmaceutically acceptable salts thereof, having the formula: ... | 05/06/2008 |
| 7361665 | Inhibitors of c-Jun N-terminal kinases (JNK) and other protein kinases The present invention provides compounds of formula I: or a pharmaceutically acceptable derivative thereof, wherein R1, R2, A, G, and W are as described in the specification. These compounds are inhibi... | 04/22/2008 |
| 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 |
| 7358258 | Prodrugs of an ERK protein kinase inhibitor 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, ... | 04/15/2008 |
| 7351733 | Tetrahydrocarbazole derivatives and their pharmaceutical use The present invention relates to novel compounds that are useful in the treatment of human papillomaviruses, and also to the methods for the making and use of such compounds. ... | 04/01/2008 |
| 7351711 | Tricyclic indanyls as integrin inhibitors The present invention is directed to substituted indanyl compounds of Formula (I): Useful for treating integrin-mediated disorders such as, but not limited to unstable angina, thromboemboic disorders, osteoporosis, growth a... | 04/01/2008 |
| 7348335 | Compositions useful as inhibitors of JAK and other protein kinases The present invention provides a compound of formula I: or a pharmaceutically acceptable salt thereof. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and metho... | 03/25/2008 |
| 7348333 | Cycloalkyl derivatives as inhibitors of bone resorption and vitronectin receptor antagonists There are described cycloalkyl derivatives of the formula (I) R1—Y-A-B-D-E-F-G (I) in which R1, Y, A, B, D, E, F and G have the meaning indicated herein, their preparation and their use as medicaments. The compounds a... | 03/25/2008 |
