Imino-bicyclo (3.3.0) octane derivatives
AssigneeSumitomo Chemical Company, Limited
InventorsKeiichi Ono, Akihiko Sugie, Masami Muraoka, Michihiro Yamamoto
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AssigneeSumitomo Chemical Company, Limited
InventorsKeiichi Ono, Akihiko Sugie, Masami Muraoka, Michihiro Yamamoto
Estimating the term…
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.
A compound of the formula ##STR25## wherein R" is a hydrogen atom or a C.sub.1 -C.sub.4 alkyl group, and 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:
2.beta.-(3'. alpha.-hydroxy-trans-1'-octenyl)3.alpha.-hydroxy-7E-(2"-carboxyethoxy)imino -cis-bicyclo[3,3,0]octane, and its stereoisomers.
2.beta.-(3'.alpha.-hydroxy-4',4'-dimethyl-tran s-1'-octenyl)-3.alpha.-hydroxy-7E-(2"-carboxyethoxy)imino-cis-bicyclo[3,3,0 ]octane, and its stereoisomers.
Dependencies are inferred from the claim text.