Esters in position 20 of camptothecins

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

Reexamination Certificate

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C546S048000

Reexamination Certificate

active

07452900

ABSTRACT:
Formula (I) compounds are described: (I) 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: 4943579 (1990-07-01), Vishnuvajjala
patent: 6242457 (2001-06-01), Penco et al.
patent: WO 01/49691 (2001-07-01), None
Matsumoto, H. et al; “Controlled Drug Release: New Water-Soluble Prodrugs of an HIV Protease Inhibitor”; BioOrg. Med. Chem. Lett., vol. 11, 2001, pp. 605-609, XP002252920.
Database Crossfire Beilstein ′Online!; Beilstein Institut zur Förderung der Chemischen Wissenschaften, Frankfurt am Main, DE; XP002252923; Database Accession Nos. 9312592, 9312810 (BRN's) & Bhatt, R. et al; “Synthesis and in Vivo Antitumor Activity of Poly(L-glutamic acid) Conjugates of 20(S)-Camptothecin”; J. Med. Chem., vol. 46, 2003, pp. 190-193, XP002252921.
Lerchen H-G et al; “Synthesis of 20-0-Linked 20(S)-Camptothecin Glycoconjugates: Impact of the Side Chain of the Ester-Linked Amino Acid on Epimerization during the Acylation Reaction and on Hydrolytic Stability of the Final Glycoconjugates”; Journal Fuer Praktische Chemie, Wiley Vch, Weinheim, DE, vol. 342, No. 8, 2000, pp. 753-760, XP001000978.
Database Crossfire Beilstein ′Online!; Beilstein Institut zur Förderung der Chemischen Wissenschaften, Frankfurt am Main, DE; XP002252922; Database Accession Nos. 7563919, 7967940 (BRN's) & Greenwald, R.B.; “Camptothecin-20-PEG Ester Transport Forms”; BioOrg. Med. Chem., vol. 6, 1998, pp. 551-562, XP000985272.
Pratesi et al, “Pattern of Antitumor Activity of a Novel Camptothecin, ST1481, in a Large Panel of Human Tumor Xenografts”, Clinical Cancer Research, vol. 8, 3904-3909, Dec. 2002.
Excerpt from an Italian University Handbook of Medicinal Chemistry “ Fondamenti Di Chimica Farmaceutica”, vol. I, Preside della Facolta di Farmacia dell'Universita di Trieste, pp. 166-175.

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