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Last Updated: January 24, 2020

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Details for Patent: 4,604,463

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Summary for Patent: 4,604,463
Title: Camptothecin derivatives and process for preparing same
Abstract:New camptothecin derivatives possessing high anti-tumor activity with slight toxicity, represented by the general formula: ##STR1## wherein R.sup.1 is a hydrogen atom, a halogen atom or an alkyl group with 1-4 carbon atoms and X is a chlorine atom or --NR.sup.2 R.sup.3 where R.sup.2 and R.sup.3 are the same or different and each represents a hydrogen atom, a substituted or unsubstituted alkyl group with 1-4 carbon atoms or a substituted or unsubstituted carbocyclic or heterocyclic group, with the proviso that when both R.sup.2 and R.sup.3 are the substituted or unsubstituted alkyl groups, they may be combined together with the nitrogen atom, to which they are bonded, to form a heterocyclic ring which may be interrupted with --O--, --S-- and/or >N--R.sup.4 in which R.sup.4 is a hydrogen atom, a substituted or unsubstituted alkyl group with 1-4 carbon atoms or a substituted or unsubstituted phenyl group and wherein the grouping --O--CO--X is bonded to a carbon atom located in any of the 9-, 10- and 11-positions in the ring A of camptothecin, as well as an ammonium salt or an alkali metal salt thereof. These new camptothecin derivatives are prepared by reacting a 7-R.sup.1 -camptothecin derivative having a hydroxyl group in any of the 9-, 10- and 11-positions on the ring A thereof with phosgen and then reacting, if necessary, the resultant 7-R.sup.1 -camptothecin derivative having a chlorocarbonyloxy group in the same position on the ring A thereof with an amine HNR.sup.2 R.sup.3 or by reacting a 7-R.sup.1 -camptothecin derivative having a hydroxyl group in any of the 9-, 10- and 11-positions on the ring A thereof with a carbamoyl chloride Cl-CONR.sup.2 R.sup.3.
Inventor(s): Miyasaka; Tadashi (Kanagawa, JP), Sawada; Seigo (Tokyo, JP), Nokata; Kenichiro (Tokyo, JP), Sugino; Eiichi (Tokyo, JP), Mutai; Masahiko (Tokyo, JP)
Assignee: Kabushiki Kaisha Yakult Honsha (Tokyo, JP)
Application Number:06/627,980
Patent Claim Types:
see list of patent claims
Compound;

Drugs Protected by US Patent 4,604,463

Applicant Tradename Generic Name Dosage NDA Approval Date TE Type RLD RS Patent No. Patent Expiration Product Substance Delist Req. Patented / Exclusive Use Submissiondate
>Applicant >Tradename >Generic Name >Dosage >NDA >Approval Date >TE >Type >RLD >RS >Patent No. >Patent Expiration >Product >Substance >Delist Req. >Patented / Exclusive Use >Submissiondate

Foreign Priority and PCT Information for Patent: 4,604,463

Foriegn Application Priority Data
Foreign Country Foreign Patent Number Foreign Patent Date
Japan58-126946Jul 14, 1983

International Family Members for US Patent 4,604,463

Country Patent Number Estimated Expiration Supplementary Protection Certificate SPC Country SPC Expiration
Austria 33839   Start Trial
Canada 1235415   Start Trial
Germany 137145   Start Trial
Germany 3470744   Start Trial
European Patent Office 0137145   Start Trial SPC/GB97/010 United Kingdom   Start Trial
Japan H034077   Start Trial
>Country >Patent Number >Estimated Expiration >Supplementary Protection Certificate >SPC Country >SPC Expiration

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