Bicyclooctane derivatives

Details Bicyclooctane derivatives Bicyclooctane derivatives

1981-03-13

1985-01-15

Brust, Joseph Paul

Drug, bio-affecting and body treating compositions

Antigen, epitope, or other immunospecific immunoeffector

Recombinant or stably-transformed bacterium encoding one or...

424305, 424317, 260464, 260465D, 260465F, 560 56, 560119, 562466, 562501, 568633, 568648, 568649, 568665, 564172, 564180, 564188, 549372, 549453, C07C 69608, C07C 69616, C07C 6113, C07C 6128

Patent

active

044938462

ABSTRACT:
A compound of the formula ##STR1## wherein X.sup.1 is a free or esterified carboxyl group, a hydroxymethyl group, a cyano group, a group of the formula: ##STR2## (R.sup.a and R.sup.b are each independently a hydrogen atom, a C.sub.1 -C.sub.4 alkyl group, a C.sub.3 -C.sub.7 cycloalkyl group, a benzyl group, a phenyl group, a phenyl group substituted with a halogen atom or a C.sub.1 -C.sub.4 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: ##STR3## (R.sup.a and R.sup.b are each as defined above), Y is an ethylene group or a vinylene group, R.sup.1 is a hydrogen atom, a hydroxyl group or a protected hydroxyl group, R.sup.2 is a hydrogen atom or R.sub.1 and R.sub.2, when taken together, means a single linkage to form a double bond between the carbon atoms which they are linked, R.sup.3 is a hydroxyl group or a protected hydroxyl group, R.sup.4 is a hydrogen atom or a C.sub.1 -C.sub.4 alkyl group, R.sup.5 is a hydrogen atom, a C.sub.3 -C.sub.8 alkenyl group, a C.sub.3 -C.sub.8 alkynyl group, a C.sub.1 -C.sub.8 alkyl group, a C.sub.3 -C.sub.7 cycloalkyl group or a group of the formula: --(CH.sub.2).sub.n --B (n is 1 or 2 and B is a C.sub.1 -C.sub.4 alkoxyl group, a C.sub.3 -C.sub.7 cycloalkyl group, or a phenyl or phenoxy group optionally substituted with a halogen atom, a C.sub.1 -C.sub.4 alkyl group, a trifluoromethyl group or a C.sub.1 -C.sub.4 alkoxyl group), A is a group of either one of the formulae: ##STR4## (R.sup.6 and R.sup.7 are each independently a hydrogen atom or a C.sub.1 -C.sub.4 alkyl group) and ##STR5## m.sub.1 is 1 or 2 and m.sub.2 is 0, 1 or 2, and the non-toxic pharmaceutically acceptable salts threreof. Said compounds have strong anti-ulcerogenic activity and are useful in treatment of gastraintestinal ulcer.

REFERENCES:
patent: 4096337 (1978-06-01), Marsham
Whittle, et al., Prostaglandins, 19, (4), pp. 605-627, (1980).
Whittle, et al., Communications, J. Pharm. Pharmacol., (1980), 32, pp._ 603-604.
Moncada, et al., Nature, 263, 1976, pp. 663-665.

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