Patent ID: 6420379
Filing Date: 2002-07-16
Classification: A61P,C07D

Abstract:
An alkynyl-substituted camptothecin compound of the formula (I): wherein:R1 is: hydrogen; optionally substituted C1-C6 alkyl; C3-C7 cycloalkyl; C3-C7 cycloalkyl C1-C6 alkyl; phenyl C1-C6 alkyl; optionally substituted phenyl; optionally substituted naphthyl; â€”Rxâ€”NR3R4, wherein Rx is C1-C4 alkylene, R3 and R4 are, each independently, hydrogen, C1-C6 alkyl, phenyl, or benzyl; â€”(Ry)mâ€”COOR5, wherein m is 0 or 1, Ry is C1-C4 alkylene, R5 is hydrogen, C1-C6 alkyl, C3-C7 cycloalkyl, or phenyl C1-C6 alkyl; â€”(Rz)nâ€”COR6, wherein n is 0 or 1, Rz is C1-C4 alkylene, R6 is C1-C6 alkyl, C3-C7 cycloalkyl, phenyl C1-C6 alkyl, optionally substituted phenyl, or â€”NR7R8, wherein R7 and R8 are, each independently, hydrogen or C1-C6 alkyl; or SiR9R10R11, wherein R9, R10 and R11 are, each independently, C1-C4 alkyl; R2 is: hydrogen; C1-C6 alkyl; C3-C7 cycloalkyl; or phenyl C1-C6 alkyl; X is: hydrogen, C1-C6 alkyl; C3-C7 cycloalkyl, C1-C6 alkoxy, C3-C7 cycloalkoxy, C1-C6 alkanoyloxy, benzoyloxy, amino, hydroxy, nitro, chlorine or methylene- or ethylene-dioxy linked to positions 10 and 11 of the molecule; or a pharmaceutically acceptable salt thereof.