Imino-bicyclo (3.3.0) octane derivatives

Details Imino-bicyclo (3.3.0) octane derivatives Imino-bicyclo (3.3.0) octane derivatives

1983-04-15

1985-08-27

Trousof, Natalie

Organic compounds -- part of the class 532-570 series

Organic compounds

Carboxylic acids and salts thereof

560 35, 560107, 560108, 560116, 560119, 560251, 560252, 562440, 562498, 564167, 564188, 514822, 514925, 544149, 544152, 544165, 544374, 544391, 546205, 546206, 548517, 548540, 549414, 549415, 549421, 549422, 549473, 549475, C07C13102, A61K 3119, A61K 31195, A61K 31215

Patent

active

045379890

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 is a group of the formula: ##STR3## (R.sup.6 is a hydrogen atom or a C.sub.1 -C.sub.4 alkyl group) or ##STR4## (R.sup.6 is as defined above), 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 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 alkynyl group, a C.sub.3 -C.sub.8 alkenyl group, a C.sub.1 -C.sub.8 alkyl group, a C.sub.3 -C.sub.7 cycloalkyl group, a hydroxy C.sub.1 -C.sub.8 alkyl group or a group of the formula: --(CH.sub.2).sub.m --B (m is 1 or 2 and B is a C.sub.1 14 C.sub.4 alkoxy, a C.sub.3 -C.sub.7 cycloalkyl, 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 alkoxy group), and n is 2 or 3; or a non-toxic pharmaceutically acceptable salt thereof. Said compounds have strong anti-cancer activity and are useful in treatment of a cancer.

REFERENCES:
patent: 4423067 (1983-12-01), Skuballa et al.
patent: 4423068 (1983-12-01), Li et al.

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