Geldanamycin derivatives and antitumor drug
AssigneeKaken Chemical Co., Ltd.
InventorsKazuya Sasaki, Yukio Inoue
Life of this patent
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Abstract
Geldanamycin derivatives the following formula ##STR1## wherein R.sup.1 represents a saturated alkylamino which should have at least two carbon atoms, an unsaturated alkylamino, a substituted lower alkylamino, cycloalkylamino, pyrrolidino or aralkylamino group or methoxy group; R.sup.2 represents hydrogen atom, a halogen atom or a lower mono or dialkylamino; when R.sup.1 is methoxy group, R.sup.2 is a halogen atom or lower alkylamino group, or ##STR2## and Geldanamycin derivative is 8,9-epoxy-Geldanamycin. The compounds are effective as antitumor drugs.
Claims14
A geldanamycin having the following formula:
- ##STR9## wherein R.sup.1 represents (A) ##STR10## wherein R.sup.7 and R.sup.8 respectively represent hydrogen;
- alkyl of 2-12 carbon atoms;
- alkyl of 2-12 carbon atoms substituted with hydroxy, amino, methylamino, pyrrolidino, pyridinyl, methoxy, piperidino, morpholino, glycoxy or halogen;
- cycloalkyl of 3-8 carbon atoms;
- adamanthyl;
- benzyl;
- phenethyl;
- picolyl;
- allyl;
- or diglycol;
- with the proviso that both R.sup.7 and R.sup.8 can be bonded to form one alkylene group of 2-6 carbon atoms;
- or
- (B) methoxy;
- wherein R.sup.2 represents hydrogen, halogen, or an alkylamino group wherein the alkyl group has 2-12 carbon atoms;
- with the proviso that when R.sup.1 is methoxy, R.sup.2 is halogen or an alkylamino group wherein the alkyl group has 2-12 carbon atoms;
- or ##STR11## wherein R.sup.3 represents ##STR12## R.sup.4, R.sup.5 & R.sup.6 respectively represent hydrogen atom or methyl group and at least one of R.sup.4, R.sup.5 and R.sup.6 is a methyl group;
- or ##STR13##
A geldanamycin having the following formula:
- ##STR14## wherein R.sup.1 represents (A) ##STR15## wherein R.sup.7 and R.sup.8 respectively represent hydrogen;
- alkyl of 2-12 carbon atoms;
- alkyl of 2-12 carbon atoms substituted with hydroxy, amino, methylamino, pyrrolidino, pyridinyl, methoxy, piperidino, morpholino, glycoxy or halogen;
- cycloalkyl of 3-8 carbon atoms;
- adamanthyl;
- benzyl;
- phenethyl;
- picolyl;
- allyl;
- or diglycol;
- with the proviso that both R.sup.7 and R.sup.8 can not be hydrogen;
- and R.sup.7 and R.sup.8 can be bonded to form one alkylene group of 2-6 carbon atoms;
- or
- (B) methoxy;
- wherein R.sup.2 represents hydrogen, halogen, or an alkylamino group wherein the alkyl group has 2-12 carbon atoms;
- with the proviso that when R.sup.1 is methoxy, R.sup.2 is halogen or an alkylamino group wherein the alkyl group has 2-12 carbon atoms.
A geldanamycin having the formula ##STR16## wherein R.sup.3 represents ##STR17## R.sup.4, R.sup.5 and R.sup.6 respectively represent hydrogen atom or methyl group and at least one of R.sup.4, R.sup.5 and R.sup.6 is methyl group.
A geldanamycin having the formula ##STR18##
Dependencies are inferred from the claim text.