[EN] BENZAMIDE CGRP RECEPTOR ANTAGONISTS<br/>[FR] ANTAGONISTES BENZAMIDES DES RÉCEPTEUR CGRP
申请人:MERCK SHARP & DOHME
公开号:WO2015161011A1
公开(公告)日:2015-10-22
The present invention is directed to benzamide compounds which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.
Compounds of the formula (I) below, or pharmacologically acceptable salts, esters or other derivatives thereof:
1
wherein A is furan, thiophene, pyrazole, imidazole, isoxazole or isothiazole;
R
1
is a substituted or unsubstituted aryl or a substituted or unsubstituted heteroaryl; R
2
is a substituted or unsubstituted heteroaryl; and R
3
is a bicyclic amino group; provided that the substituents R
1
and R
2
are bonded to the two atoms of the cyclic group A which are adjacent to the atom of the cyclic group A to which the substituent R
2
is bonded. The compounds inhibit the production of inflammatory cytokines.
This disclosure concerns compounds which are useful as inhibitors of protein kinase C (PKC) and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of PKC. This disclosure also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
This disclosure concerns compounds which are useful as inhibitors of protein kinase C (PKC) and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of PKC. This disclosure also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
本公开涉及的化合物可作为蛋白激酶 C (PKC) 的抑制剂,因此可用于治疗通过 PKC 的活性介导或维持的各种疾病和失调。本公开还涉及包含这些化合物的药物组合物、使用这些化合物治疗各种疾病和失调的方法、制备这些化合物的工艺以及在这些工艺中有用的中间体。