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filingDate 2003-11-12-04:00^^<http://www.w3.org/2001/XMLSchema#date>
grantDate 2005-01-25-04:00^^<http://www.w3.org/2001/XMLSchema#date>
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publicationDate 2005-01-25-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber US-6846925-B2
titleOfInvention Colchinol derivatives as angiogenesis inhibitors
abstract The invention related to colchinol derivatives of the formula (I): Wherein: R 1 ; R 2 and R 3 are each independently hydroxy, phosphoryloxy (—OP 3 H 2 ), C 1-4 alkoxy or an in vivo hydrolysable ester of hydroxy, with the proviso that at least 2 of R 1 , R 2 and R 3 are C 1-4 alkoxy; A is —CO—, —C(O)O—, —CON(R 8 )— (wherein R 8 is hydrogen, C 1-4 alkyl, C 1-3 alkoxyC 1-3 alkyl, aminoC 1-3 alkyl or hydroxyC 1-3 alkly); a is an integer from 1 to 4 inclusive; R a and R b are independently selected from hydrogen, hydroxy and amino; B is —O—, —CO—, N(R 9 )CO—, —CON(R 9 )—, —N(R 9 )C(O)O—, —N(R 9 )CON(R 10 )—, —N(R 9 )SO 2 —, —SO 2 N(R 9 )— or a direct single blond (wherein R 9 and R 10 are independently selected from hydrogen, C 1-4 alkyl, C 1-3 alkoxyC 1-3 alkyl, aminoC 1-3 alkyl and hydroxyC 1-3 alkyl); 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-(C 1-4 alkyl)amino, N,N-di(C 1-3 alkyl)amino, or of the formula —Y 1 (CH 2 ) 0 R 11 or —NHCH(R 12 )COOH; [wherein Y 1 is a direct single bond, —O—, —C(O)—, —N(R 13 )C(O)— or —C(O)N(R 13 )— (wherein R 13 is hydrogen, C 1-4 alkyl, C 1-3 alkoxyC 2-3 alkyl, aminoC 2-3 alkyl or hydroxyC 2-3 alkyl); e is O or an integer from 1 to 4 inclusive.
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Total number of triples: 782.