EP0088642A2
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New camptothecin derivatives and process for their preparation
Assignee: Yakult Honsha Co Ltd
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Filing: 1983-03-10
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Granted: —
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Expires: 2003-03-10
Abstract
Abstract New camptothecin derivatives of the general formula: wherein R 1 and R 2 each stands for a hydrogen atom, a substituted or unsubstituted alkyl group, a substituted or unsubstituted aralkyl group or a substituted or unsubstituted aryl group and R and R 2 , taken together with the nitrogen atom to which they are attached, may form a cyclic group. These new derivatives are useful intermediates for preparing pharmaceuticals or other classes of new camptothecin derivatives. These present new derivatives are prepared by treating camptothecin-7--carboxylic acid first with a carboxyl group-activating reagent and then with ammonia or the corresponding amine.
Inventors
- 👤 Tadashi Miyasaka
- 👤 Seigo Sawada
- 👤 Kenichiro Nokata
- 👤 Masahiko Mutai
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-10-27 07:40
CPC Classifications
C; C07; C07D; C07D491/00; C07D491/22
Claims Analysis
Total Claims: 28
Claim 1
Independent Claim
69 words
A camptothecin derivative of the general formula: wherein R 1 and R: each independently represent a hydrogen atom, a substituted or unsubstituted alkyl group, a substituted or unsubstituted aralkyl group or a substituted or unsubstituted aryl group or R 1 and R 2 when taken together with the nitrogen atom to which they are attached, may form a heterocyclic group containing one or two nitrogen, oxygen and/or sulfur atoms.
Claim 2
Dependent Claim
69 words
A camptothecin derivative of the general formula: wherein R 1 and R: each independently represent a hydrogen atom, a substituted or unsubstituted alkyl group, a substituted or unsubstituted aralkyl group or a substituted or unsubstituted aryl group or R 1 and R 2 when taken together with the nitrogen atom to which they are attached, may form a heterocyclic group containing one or two nitrogen, oxygen and/or sulfur atoms.
Claim 3
Dependent Claim
1 words
Camptothecin-7-carboxamide.
Claim 4
Dependent Claim
1 words
Camptothecin-7-carboxamide.
Claim 5
Dependent Claim
1 words
Camptothecin-7-N-ethylcarboxamide.
Claim 6
Dependent Claim
1 words
Camptothecin-7-N-ethylcarboxamide.
Claim 7
Dependent Claim
1 words
Camptothecin-7-N-cyclohexylcarboxamide.
Claim 8
Dependent Claim
1 words
Camptothecin-7-N-cyclohexylcarboxamide.
Claim 9
Dependent Claim
1 words
Camptothecin-7-N-benxylcarboxamide.
Claim 10
Dependent Claim
1 words
Camptothecin-7-N-benxylcarboxamide.
Claim 11
Dependent Claim
2 words
Ethyl 2-(camptothecin-7-carboxamido)acetate.
Claim 12
Dependent Claim
2 words
Ethyl 2-(camptothecin-7-carboxamido)acetate.
Claim 13
Dependent Claim
1 words
Camptothecin-7-N-phenylcarboxamide.
Claim 14
Dependent Claim
1 words
Camptothecin-7-N-phenylcarboxamide.
Claim 15
Dependent Claim
1 words
N,N-dimethyl-camptothecin-7-carboxamide.
Claim 16
Dependent Claim
1 words
N,N-dimethyl-camptothecin-7-carboxamide.
Claim 17
Dependent Claim
1 words
N,N-diethyl-camptothecin-7-carboxamide.
Claim 18
Dependent Claim
1 words
N,N-diethyl-camptothecin-7-carboxamide.
Claim 19
Dependent Claim
1 words
4-(camptothecin-7-carbonyl)morpholine.
Claim 20
Dependent Claim
1 words
4-(camptothecin-7-carbonyl)morpholine.
Claim 21
Dependent Claim
29 words
A camptothecin derivative as claimed in claim 1 wherein R 1 is a hydrogen atom and R 2 is an alkyl or aralkyl group substituted with a carboxyl group.
Claim 22
Dependent Claim
13 words
A mono sodium salt of a camptothecin derivative as claimed in claim 11.
Claim 23
Dependent Claim
29 words
A camptothecin derivative as claimed i claim 1 wherein R 1 is a hydrogen atom and R 2 is an alkyl or aralkyl group substituted with an alkoxycarbonyl group.
Claim 24
Dependent Claim
29 words
A camptothecin derivative as claimed in claim 1 wherein R 1 is a hydrogen atom and R 2 is an alkyl or aralkyl group substituted with a dialkylamino group.
Claim 25
Dependent Claim
11 words
A hydrochloride of a camptothecin derivative as claimed in claim 14.
Claim 26
Dependent Claim
59 words
A process for the preparation of camptothecin derivatives of the general formula: wherein R 1 and R 2 are each as defined in claim 1 which process comprises treating camptothecin with a carboxyl group-activating reagent and then with ammonia or a primary or secondary amine of the general formula: wherein R 1 and R 2 are as defined above.
Claim 27
Dependent Claim
40 words
A process as claimed in claim 16 wherein the carboxyly group-activating reagent is N,N'-dicyclohexylcarbodiimide (DCC), N,N'-carbonyldiimidazole, N,N'-diisopropylcarbodiimide, diphenyl chlorophosphate, 2,2'- dipyridyl disulfide, N,N'-di-p-tolycarbodiimide, 1-hydroxybenztriazole, N-hydroxysuccinimide, imidazole, triazole, pyrazol, a chloroformic acid ester, phosphorus oxychloride, pivaloyl chloride or a Vilsmeier reagent.
Claim 28
Dependent Claim
17 words
A process according to claim 11, wherein the treatment is carried out in the presence of eriethylamine.
References Cited (Backward Citations)
No citation records indexed.
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