Camptothecins with a modified lactone ring

Details Camptothecins with a modified lactone ring Camptothecins with a modified lactone ring

2007-09-25

2007-09-25

Aulakh, Charanjit S. (Department: 1625)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

C546S048000

Reexamination Certificate

active

10511724

ABSTRACT:
Compounds of formula (I) or (II) are described: where the groups are as defined in the description here below, the racemic mixtures, their individual enantiomers, their individual diastereoisomers, their mixtures, and their pharmaceutically acceptable salts. Said compounds are topoisomerase I inhibitors.

REFERENCES:
patent: 4399276 (1983-08-01), Miyasaka et al.
patent: 6242457 (2001-06-01), Penco et al.
patent: 2001/0008939 (2001-07-01), Lucio et al.
patent: 1 044 977 (2000-10-01), None
patent: WO97/00876 (1997-01-01), None
Bom, D., et al., “ Novel A, B, E-Ring-Modified Comptothecins Displaying High Lipophilicity and Markedly Improved Human Blood Stabilities”,J. Med. Chem., 42:3018-3022 (1999).
Dallavalle, S., et al., “Perspectives in camptothecin development”,Expert Opin. Ther. Patents, 12(6):837-844 (2002).
Hertzberg, R.P., et al., “Modification of the Hydroxy Lactone Ring of Camptothecin: Inhibition of Mammalian Topoisomerase I and Biological Activity”,J. Med. Chem., 32:715-720 (1989).

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