Abstract New camptothecin derivatives, useful as antitumor agents or intermediates therefor, of the general formula (I) ##STR1## wherein X is a lower alkyl group, and R is a hydrogen atom or the grouping -COY where Y is a linear or branched unsubstituted C 1 -C 18 alkyl group; a lower alkyl group substituted by a halogen atom or a lower alkylthio, amino, acylamino, hydroxyl, lower alkoxy, aryloxy or lower alkoxycarbonyl group; a C 3 -C 19 alkenyl, C 3 -C 19 alkynyl or C 3 -C 8 cycloalkyl group; a C 3 -C 8 cycloalkyl group substituted by an acylamino-lower alkyl group; an N-acylpyrrolidyl group; a phenyl group; a phenyl group substituted by a halogen atom or a trifluoromethyl, nitro, amino, lower alkoxycarbonyl, lower alkyl, phenyl or lower alkoxy; a cinnamyl group; a benzyl group; a naphthyl group; a pyridyl group; a furyl group; or a thienyl group, as well as acid addition salts and quaternary ammonium salts thereof, and a process for preparing the new camptothecin derivatives by subjecting 7-ethylcamptothecin to the treatment with an N-di-X-ethylenediamine followed by acylation.
Inventors
👤 Seigo Sawada
👤 Kenichiro Nokata
👤 Satoru Okajima
👤 Hisako Nagai
👤 Takashi Yaegashi
👤 Kenichi Tezuka
👤 Tadashi Miyasaka
Bibliographic Details
Application Number—
JurisdictionUS
Data Sourcegoogle_patents
Last Synchronized2026-11-01 06:04
CPC Classifications
C; C07; C07D; C07D471/00; C07D471/12; C07D471/14
Claims Analysis
Total Claims: 2
Claim 1
Independent Claim
153 words
Camptothecin derivatives of the formula: ##STR8## wherein X is a lower alkyl group, and R is a hydrogen atom or the grouping -COY where Y is a linear or branched unsubstituted C 1 -C 18 alkyl group; a lower alkyl group substituted by a halogen atom or a lower alkylthio, amino, acylamino, hydroxyl, lower alkoxy, aryloxy or lower alkoxycarbonyl group; a C 3 -C 19 alkenyl, C 3 -C 19 alkynyl or C 3 -C 8 cycloalkyl group; a C 3 -C 8 cycloalkyl group substituted by an acylamino-lower alkyl group; an N-acylpyrrolidyl group; a phenyl group; a phenyl group substituted by a halogen atom or a trifluoromethyl, nitro, amino, lower alkoxycarbonyl, lower alkyl, phenyl or lower alkoxy; a cinnamyl group; a benzyl group; a naphthyl group; a pyridyl group; a furyl group; or a thienyl group, and their physiologically acceptable acid addition salts formed at the amino group and quaternary ammonium salts.
Claim 2
Dependent Claim
153 words
Camptothecin derivatives of the formula: ##STR8## wherein X is a lower alkyl group, and R is a hydrogen atom or the grouping -COY where Y is a linear or branched unsubstituted C 1 -C 18 alkyl group; a lower alkyl group substituted by a halogen atom or a lower alkylthio, amino, acylamino, hydroxyl, lower alkoxy, aryloxy or lower alkoxycarbonyl group; a C 3 -C 19 alkenyl, C 3 -C 19 alkynyl or C 3 -C 8 cycloalkyl group; a C 3 -C 8 cycloalkyl group substituted by an acylamino-lower alkyl group; an N-acylpyrrolidyl group; a phenyl group; a phenyl group substituted by a halogen atom or a trifluoromethyl, nitro, amino, lower alkoxycarbonyl, lower alkyl, phenyl or lower alkoxy; a cinnamyl group; a benzyl group; a naphthyl group; a pyridyl group; a furyl group; or a thienyl group, and their physiologically acceptable acid addition salts formed at the amino group and quaternary ammonium salts.