EP1176139A1 — Medicinal compositions with 2.2.1] and 3.1.1] bicycloskeleton antagonistic to both of pgd 2?/txa 2? receptors

USPTO Abstract

The present invention provides novel compounds having a dual antagonistic activity against thromboxane A 2 receptor and prostaglandin D 2 receptor and pharmaceutical compositions comprising them. A compound of the formula (I): wherein R 1 is -CH 2 -CH=CH-CH 2 -CH 2 -CH 2 -COOR 2 or -CH=CH-CH 2 -CH 2 -CH 2 -COOR 2 ; R 2 is hydrogen or alkyl; m is 0 or 1; p is 0 or 1; X 1 and X 3 each is independently optionally substituted aryl or optionally substituted heteroaryl; X 2 is a bond, -CH 2 -, -S-, -SO 2 -, -CH 2 -O-, -O-CH 2 -, -CH 2 -S-, -S-CH 2 -, or the like; X 4 is -CH 2 -, -CH 2 -CH 2 -, -C(=O)-, or the like, have a dual antagonistic activity against both a thromboxane A 2 receptor and a prostaglandin D 2 receptor.