Bicyclooctane derivatives

Details Bicyclooctane derivatives Bicyclooctane derivatives

C - Chemistry, Metallurgy

07

D

260/235.01

C07D 295/18 (2006.01) C07C 29/09 (2006.01) C07C 29/128 (2006.01) C07C 35/32 (2006.01) C07C 43/196 (2006.01) C07C 405/00 (2006.01) C07D 211/32 (2006.01)

Patent

CA 1189506

ABSTRACT OF THE DISCLOSURE A compound of the formula Image wherein X1 is a free or esterified carboxyl group, a hydroxymethyl group, a cyano group, a group of the formula: Image (Ra and Rb 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 sub- stituted 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: Image (Ra and Rb are each as defined above), Y is an ethylene group or a vinylene group, R1 is a hydrogen atom, a hydroxyl group or a protected hydroxyl group, R2 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, R3 is a Abstract hydroxyl group or a protected hydroxyl group, R4 is a hydrogen atom or a C1-C4 alkyl group, R5 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=C-, Image (R6 and R7 are each independently a hydrogen atom or a C1-C4 alkyl group) and Image , m1 is 1 or 2 and m2 is 0, 1 or 2, and the non-toxic pharmaceutically acceptable salts thereof. Said compounds have strong anti-ulcerogenic activity and are useful in treatment of gastraintestinal ulcer.

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