PROCESS FOR PRODUCING BICYCLOOCTANE DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AS ACTIVE AGENTS

摘要

Certain novel bicyclooctanes and their pharmaceutically acceptable salts are useful in the treatment of gastrointestinal ulcers. These compounds can be prepared by various methods and have the formula …… wherein X<1> is a free or esterified carboxyl group, a hydroxymethyl group, a cyano group, a group of the formula: …… (R and R are each independently a hydrogen atom, a C1-C4 alkyl group, a C3-C7 cycloalkyl group, a benzyl group, a phenyl group, a phenyl group substituted with a halogen atom or a C1-C4 alkyl group, or, when taken together with the adjacent nitrogen atom to which they are attached, they represent a 5 to 7-membered saturated heterocyclic group) or a group of the formula: …… (R and R are each as defined above), Y is an ethylene group or a vinylene group, R<1> is a hydrogen atom, a hydroxyl group or a protected hydroxyl group, R<2> is a hydrogen atom or R1 and R2, when taken together, means a single linkage to form a double bond between the carbon atoms which they are linked, R<3> is a hydroxyl group or a protected hydroxyl group, R<4> is a hydrogen atom or a C1-C4 alkyl group, R<5> is a hydrogen atom, a C3-C8 alkenyl group, a C3-C8 alkynyl group, a C1-C8 alkyl group, a C3-C7 cycloalkyl group or a group of the formula: -(CH2)n-B (n is 1 or 2 and B is a C1-C4 alkoxyl group, a C3-C7 cycloalkyl group, or a phenyl or phenoxy group optionally substituted with a halogen atom, a C1-C4 alkyl group, a trifluoromethyl group or a C1-C4 alkoxyl group), A is a group of either one of the formulae:… -CH=CH-, …… (R<6> and R<7> are each independently a hydrogen atom or a C1-C4 alkyl group) and …… m1 is 1 or 2 and m2 is 0, 1 or 2.