- CRYSTALLINE FORMS OF N-(2-CHLORO-6-METHY]PHENVN-2-[F6-[4-(2-HVDROXVETHVL)-L- PIPERAZINVIL-2-METHVL-4-PVRIMIDINVLLAMINOL-5-THIAZOLECARBOXAMIDE AND THEIR PROCESS THEREOF
-
The present invention relates to crystalline 1,2-Propanediol solvate of N-(2-chloro-6- methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-l-piperazinyl]-2-methyl-4-pyrimidinyl]ainino]-5- thiazolecarboxamide compound of formula- lb, its process for the preparation and its use in the preparation of anhydrous crystalline form (N-6) and monohydrate of N-(2-chloro-6- methy lphenyl)-2- [ [6- [4-(2 -hydroxy ethyl)- 1 -piperazinyl] -2-methyl-4-pyrimidinyl]amino] -5 - thiazolecarboxamide. [formula] 1,2-Propanediol solvate Formula- lb
- -
-
Page/Page column 17; 18
(2017/01/26)
-
- Synthesis and biological activities of 2-amino-thiazole-5-carboxylic acid phenylamide derivatives
-
In an attempt to develop potent and selective anti-tumor drugs, a series of novel 2-amino-thiazole-5-carboxylic acid phenylamide derivatives were designed based on the structure of dasatinib. All compounds were synthesized by a systematic combinatorial chemical approach. Biological evaluation revealed that N-(2-chloro-6-methylphenyl)-2-(2-(4-methylpiperazin-1-yl)acetamido) thiazole-5-carboxamide (6d) exhibited high antiproliferative potency on human K563 leukemia cells comparable to dasatinib. Against mammary and colon carcinoma cells 6d was either inactive (MDA-MB 231) or distinctly less active (MCF-7 and HT-29: IC50=20.2 and 21.6μM, respectively). Dasatinib showed at each cell line IC501μM. The results of this structure activity relationship study clearly documented that the pyrimidin-4-ylamino core of dasatinib is responsible for the anti-tumor activity against non-leukemia cell lines.
- Liu, Wukun,Zhou, Jinpei,Qi, Fan,Bensdorf, Kerstin,Li, Zhiyu,Zhang, Huibin,Qian, Hai,Huang, Wenlong,Cai, Xueting,Cao, Peng,Wellner, Anja,Gust, Ronald
-
experimental part
p. 451 - 458
(2012/02/01)
-
- TRIAZINE DERIVATIVES AND THEIR THERAPEUTICAL APPLICATIONS
-
The present invention comprises inter alia compounds as shown in formula (I) or a pharmaceutically acceptable salt thereof.
- -
-
-
- A new and efficient preparation of 2-aminothiazole-5-carbamides: Applications to the synthesis of the anti-cancer drug dasatinib
-
A new and efficient method has been developed for the synthesis of 2-amino-N-(-(2-chloro-6-methylphenyl)-thiazole-5-carboxamide. The new method involves a chemoselective α-bromination of β-ethoxyacrylamide followed by a one-pot treatment with thiourea to give the desired 2-aminothiazole-5-carboxylamide in excellent yield. Application of this new method to the efficient synthesis of the anti-cancer drug dasatinib was demonstrated.
- Chen, Bang-Chi,Zhao, Rulin,Wang, Bei,Droghini, Roberto,Lajeunesse, Jean,Sirard, Pierre,Endo, Masaki,Balasubramanian, Balu,Barrisha, Joel C.
-
experimental part
p. 32 - 38
(2010/09/05)
-
- TRIAZINE DERIVATIVES AND THEIR THERAPEUTICAL APPLICATIONS
-
The invention provides for Triazine derivatives and their use to modulate protein kinase activity in a variety of conditions and diseases.
- -
-
Page/Page column 53
(2008/12/06)
-
- PROCESS FOR PREPARING 2-AMINOTHIAZOLE-5-AROMATIC CARBOXAMIDES AS KINASE INHIBITORS
-
The invention relates to processes for preparing compounds having the formula (I) and crystalline forms thereof, wherein Ar is aryl or heteroaryl, L is an optional alkylene linker, and R2, R3, R4, and R5, are as defined in the specification herein, which compounds are useful as kinase inhibitors, in particular, inhibitors of protein tyrosine kinase and p38 kinase.
- -
-
Page/Page column 50-51
(2008/06/13)
-