Elongated and multiple spacers in activatible prodrugs

Chemistry: natural resins or derivatives; peptides or proteins; – Peptides of 3 to 100 amino acid residues – Tripeptides – e.g. – tripeptide thyroliberin – etc.

Reexamination Certificate

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Details

C530S330000, C514S018700, C514S019300

Reexamination Certificate

active

10472921

ABSTRACT:
This invention is directed to prodrugs that can be activated at the preferred site of action in order to selectively deliver the corresponding therapeutic parent drugs to target cells or to the target site. This invention will therefore primarily but not exclusively relate to tumor cells as target cells. More specifically the prodrugs are compounds of the formula V—(W)k—(X)l—A—Z, wherein: V is a specifier; (W)k—(X)l—A is an elongated self-elimination spacer system; W and X are each a 1,(4+2n) electronic cascade spacer, being the same or different; A is either a spacer group of formula (Y)mwherein: Y is a 1,(4+2n) electronic cascade spacer, or a group of formula U being a cyclization elimination spacer; Z is a therapeutic drug; k, l and m are integers from 0 (included) to 5 (included); n is an integer of 0 (included) to 10 (included), with the provisos that: —when A is (Y)m: k+l+m≧1, and if k+l+m=1; —when A is U: k+l≧1.

REFERENCES:
patent: 5691371 (1997-11-01), Denny et al.
patent: 6759509 (2004-07-01), King et al.
patent: 2003/0096743 (2003-05-01), Senter et al.
patent: 2003/0130189 (2003-07-01), Senter et al.
patent: 2005/0256030 (2005-11-01), Feng
patent: 0624377 (1994-11-01), None
patent: 1243276 (2002-09-01), None
patent: WO 8101145 (1981-04-01), None
patent: WO 9813059 (1998-04-01), None
Avalos, Martin (Tetrahedron: Asymmetry 6(4), 945-56, 1995).
Goodwin, (Journal of Organic Chemistry 50(26), 5889-92, 1985).
PCT/EP02/03591 International Search Report.
Chakravarty et al. “Plasmin-activated prodrugs” J. Med. Chem (1983), 26(5), 368-44.
Dubowchik et al. Cathepsin B-sensitive dipeptide prodrugs. 1 Bioorganic & Medicinal Chemistry Letters, Oxford, GB vol. 8, No. 23, Dec. 1, 1998, pp. 3341-3346.
De Groot et al. “Synthesis and Biological Evaluation of Novel Prodrugs” J. Med. Chem. (1999) 42(25) 5277-5283.
De Groot et al. “Synthesis and Biological Evaluation of 2′-Carbamate-Linked” Journal of Medicinal Chemistry (2000) 43(16), 3093-3102.
De Groot et al. “Elongated Multiple Electronic Cascade” Journal of Organic Chemistry (2001) 66(26), 8815-8830.
De Groot et al. “In vivo efficacy of spacer-containing antitumor prodrugs” Proceedings of the American Association for Cancer Research Annual, vol. 43, Mar. 2002, p. 415.
De Groot et al. “Design, synthesis and initial evaluation” proceedings of the American Association for Cancer Research Annual, vol. 43, Mar. 2002 p. 414.
EPO communication dated Dec. 19, 2005 regarding European Patent Application No. 02727513.0 (claiming priority of European Patent Application No. 01201095.5).

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