Colchinol derivatives as angiogenesis inhibitors

Details Colchinol derivatives as angiogenesis inhibitors Colchinol derivatives as angiogenesis inhibitors

2005-01-25

2005-01-25

Powers, Fiona T. (Department: 1626)

Organic compounds -- part of the class 532-570 series

Organic compounds

Four or more ring nitrogens in the bicyclo ring system

C544S380000, C548S338100, C558S170000, C558S172000, C564S157000

Reexamination Certificate

active

06846925

ABSTRACT:
The invention related to colchinol derivatives of the formula (I): Wherein: R1; R2and R3are each independently hydroxy, phosphoryloxy (—OP3H2), C1-4alkoxy or an in vivo hydrolysable ester of hydroxy, with the proviso that at least 2 of R1, R2and R3are C1-4alkoxy; A is —CO—, —C(O)O—, —CON(R8)— (wherein R8is hydrogen, C1-4alkyl, C1-3alkoxyC1-3alkyl, aminoC1-3alkyl or hydroxyC1-3alkly); a is an integer from 1 to 4 inclusive; Raand Rbare independently selected from hydrogen, hydroxy and amino; B is —O—, —CO—, N(R9)CO—, —CON(R9)—, —N(R9)C(O)O—, —N(R9)CON(R10)—, —N(R9)SO2—, —SO2N(R9)— or a direct single blond (wherein R9and R10are independently selected from hydrogen, C1-4alkyl, C1-3alkoxyC1-3alkyl, aminoC1-3alkyl and hydroxyC1-3alkyl); b is O or an integer from 1 to 4 inclusive, (provided that when b is O, B is a single direct bond); D is carboxy, sulpho, tetrazolyl, imidazolyl, phosphoryloxy, hydroxy, amino, N-(C1-4alkyl)amino, N,N-di(C1-3alkyl)amino, or of the formula —Y1(CH2)0R11or —NHCH(R12)COOH; [wherein Y1is a direct single bond, —O—, —C(O)—, —N(R13)C(O)— or —C(O)N(R13)— (wherein R13is hydrogen, C1-4alkyl, C1-3alkoxyC2-3alkyl, aminoC2-3alkyl or hydroxyC2-3alkyl); e is O or an integer from 1 to 4 inclusive.

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