Angiogene Pharmaceuticals Limited

Jean Claude Arnould

The invention related to colchinol derivatives of the formula (I): Wherein: R; Rand Rare each independently hydroxy, phosphoryloxy (&#x2014;OPH), Calkoxy or an in vivo hydrolysable ester of hydroxy, with the proviso that at least 2 of R, Rand Rare Calkoxy; A is &#x2014;CO&#x2014;, &#x2014;C(O)O&#x2014;, &#x2014;CON(R)&#x2014; (wherein Ris hydrogen, Calkyl, CalkoxyCalkyl, aminoCalkyl or hydroxyCalkly); a is an integer from 1 to 4 inclusive; Rand Rare independently selected from hydrogen, hydroxy and amino; B is &#x2014;O&#x2014;, &#x2014;CO&#x2014;, N(R)CO&#x2014;, &#x2014;CON(R)&#x2014;, &#x2014;N(R)C(O)O&#x2014;, &#x2014;N(R)CON(R)&#x2014;, &#x2014;N(R)SO&#x2014;, &#x2014;SON(R)&#x2014; or a direct single blond (wherein Rand Rare independently selected from hydrogen, Calkyl, CalkoxyCalkyl, aminoCalkyl and hydroxyCalkyl); 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-(Calkyl)amino, N,N-di(Calkyl)amino, or of the formula &#x2014;Y(CH)Ror &#x2014;NHCH(R)COOH; [wherein Yis a direct single bond, &#x2014;O&#x2014;, &#x2014;C(O)&#x2014;, &#x2014;N(R)C(O)&#x2014; or &#x2014;C(O)N(R)&#x2014; (wherein Ris hydrogen, Calkyl, CalkoxyCalkyl, aminoCalkyl or hydroxyCalkyl); e is O or an integer from 1 to 4 inclusive.

Colchinol derivatives as angiogenesis inhibitors

The invention related to colchinol derivatives of the formula (I): Wherein: R , R and R are each independently hydroxy, phosphoryloxy (&mdash;OPO H ), C alkoxy or an in vivo hydrolysable ester of hydroxy, with the proviso that at least 2 of R , R and R are C alkoxy; A is &mdash;CO&mdash;, &mdash;C(O)O&mdash;, &mdash;CON(R )&mdash; (wherein R is hydrogen, C alkyl, C alkoxyC alkyl, aminoC alkyl or hydroxyC alkyl); a is an integer from 1 to 4 inclusive; R and R are independently selected from hydrogen, hydroxy and amino; B is &mdash;O&mdash;, &mdash;CO&mdash;, N(R )CO&mdash;, &mdash;CON(R )&mdash;, &mdash;N(R )C(O)O&mdash;, &mdash;N(R )CON(R )&mdash;, &mdash;N(R )SO &mdash;, &mdash;SO N(R )&mdash; or a direct single blond (wherein R and R are independently selected from hydrogen, C alkyl, C alkoxyC alkyl, aminoC alkyl and hydroxyC alkyl); b is 0 or an integer from 1 to 4 inclusive, (provided that when b is 0, B is a single direct bond); D is carboxy, sulpho, tetrazolyl, imidazolyl, phosphoryloxy, hydroxy, amino, N&mdash;(C alkyl)amino, N,N-di(C alkyl)amino, or of the formula &mdash;Y (CH ) R or &mdash;NHCH(R )COOH; &lsqb;wherein Y is a direct single bond, &mdash;O&mdash;, &mdash;C(O)&mdash;, &mdash;N(R )C(O)&mdash; or &mdash;C(O)N(R )&mdash; (wherein R is hydrogen, C alkyl, C alkoxyC alkyl, aminoC alkyl or hydroxyC alkyl); e is 0 or an integer from 1 to 4 inclusive.

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Reims, France

Jean Claude Arnould