The invention relates to compounds of formula (I) and salts thereof wherein the substituents are as defined in the specification; a compound of formula (I) for use in the treatment of the human or animal body, in particular with regard to c-Met tyrosine kinase mediated diseases or conditions; the use of a compound of formula (I) for manufacturing a medicament for the treatment of such diseases; pharmaceutical compositions comprising a compound of the formula (I), optionally in the presence of a combination partner, and processes for the preparation of a compound of formula (I).
The invention relates to compounds of formula (I) and salts thereof:
wherein the substituents are as defined in the specification; a compound of formula (I) for use in the treatment of the human or animal body, in particular with regard to c-Met tyrosine kinase mediated diseases or conditions; the use of a compound of formula (I) for manufacturing a medicament for the treatment of such diseases; pharmaceutical compositions comprising a compound of the formula (I), optionally in the presence of a combination partner, and processes for the preparation of a compound of formula (I).
The invention relates to compounds of formula (I) and salts thereof:
wherein the substituents are as defined in the specification; a compound of formula (I) for use in the treatment of the human or animal body, in particular with regard to c-Met tyrosine kinase mediated diseases or conditions; the use of a compound of formula (I) for manufacturing a medicament for the treatment of such diseases; pharmaceutical compositions comprising a compound of the formula (I), optionally in the presence of a combination partner, and processes for the preparation of a compound of formula (I).
Identification of isothiazole-4-carboxamidines derivatives as a novel class of allosteric MEK1 inhibitors
作者:Hassan El Abdellaoui、Chamakura V.N.S. Varaprasad、Dinesh Barawkar、Subrata Chakravarty、Andreas Maderna、Robert Tam、Huanming Chen、Matt Allan、Jim Z. Wu、Todd Appleby、Shunqi Yan、Weijian Zhang、Stanley Lang、Nanhua Yao、Robert Hamatake、Zhi Hong
DOI:10.1016/j.bmcl.2006.08.048
日期:2006.11
The development of potent, orally bioavailable, and selective series of 5-amino-3-hydroxy-N(1-hydroxypropane-2-yl)isothiazole-4-carboxamidine inhibitors of MEK1 and MEK-2 kinase is described. Optimization of the carboxamidine and the phenoxyanifine group led to the identification of 55 which gave good potency as in vitro MEK1 inhibitors, and good oral exposure in rat. (c) 2006 Elsevier Ltd. All rights reserved.