Carbacyclin analogs

Details Carbacyclin analogs Carbacyclin analogs

1984-01-26

1987-07-14

Shippen, Michael L.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

548341, 548509, 548540, 548551, 549 79, 549415, 549423, 549464, 549469, 549473, 560 56, 560107, 560116, 560117, 560119, 562466, 562498, 562499, 562501, 564172, 564188, 514234, 514277, 514319, 514415, 514423, 514424, 514438, 514459, 514469, 514473, 514510, 514557, 514569, 514572, 514573, 514622, 514623, 544171, 546206, 546342, C07C 5962, C07C 69734, C07C 6978, C07D31500, A61K 31185, A61K 31215, A61K 31235, A61K 3135

Patent

active

046803076

ABSTRACT:
A compound of the formula: ##STR1## wherein X.sup.1 is a free or an esterified carboxyl group, or 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, Y.sup.1 is a group of the formula: ##STR3## (R.sup.6 is a hydrogen atom or C.sub.1 -C.sub.4 alkyl group), ##STR4## (R.sup.6 is as defined above), ##STR5## R.sup.1 is a hydrogen atom, a hydroxyl group or a protected hydroxyl group, R.sup.2 is a hydrogen atom or R.sup.1 and R.sup.2, when taken together, mean a shingle linkage to from 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.1 -C.sub.12 alkyl group, a C.sub.2 -C.sub.12 alkenyl group, a C.sub.2 -C.sub.12 alkynyl group, a C.sub.3 -C.sub.10 cycloalkyl group, a C.sub.4 -C.sub.10 cycloalkenyl group, a hydroxy C.sub.1 -C.sub.12 alkyl group, a C.sub.3 -C.sub.10 heterocyclic group, a phenyl group optionally substituted with a halogen atom; a hydroxyl group, a C.sub.1 -C.sub.4 alkyl group, a trifluoromethyl group, or a C.sub.1 -C.sub.4 alkyl group or a formula: A-B (A is a C.sub.1 -C.sub.7 alkylene chain and B is a C.sub.3 -C.sub.10 cycloalkyl group, a C.sub.4 -C.sub.10 cycloalkenyl group, a C.sub.1 -C.sub.12 alkoxy group, a C.sub.3 -C.sub.10 cycloalkoxy group, a C.sub.4 -C.sub.10 cycloalkenyloxy group, a C.sub.3 -C.sub.10 heterocyclic group, or a phenyl or phenoxy group optionally substituted with a halogen atom, a hydroxy group, a C.sub.1 -C.sub.4 alkyl group, a trifluoromethyl group or a C.sub.1 -C.sub.4 alkoxy group); or a non-toxic pharmaceutically acceptable salt thereof. Said compound have strong anti-ulcerous action or antithrombotic action, and are useful in treatment of ulcer or thrombosis.

REFERENCES:
patent: 4322435 (1982-03-01), Kojima et al.
patent: 4423067 (1983-12-01), Skuballa et al.
patent: 4479966 (1984-10-01), Hayashi et al.
patent: 4493846 (1985-01-01), Ono et al.
Derwent Abstract, No. 18487 D/11, abstract of Japanese Kokai 56-5456.
Journal of Pharmacology and Experimental Therapeutics, vol. 206, No. 1, 1978, pp. 132-138, Crane et al.

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