NZ335189A - Use of taxane hydrophobic derivatives for the treatment of cancer - Google Patents

Abstract

[ Patent 335189 This invention provides a taxane having the above formula wherein: A1 is H or a group having the formula Z-C(O)NHCH(C6H5)CH(OR)C(O)-; Z is C6H5-, C6H5CH2-O-, C(CH3)3-O- or CH(CH3)=C(CH3)-; A2 is H or CH3C(O)-; A3 is H or OH. Each of R and R' is H or a group having the formula Y1Y2, provided that at least one of R and R' is not H. Y is C(O)CHX1(CH2)n1(CH=CH)n2(CH2)n3(CH=CH)n4(CH2)n5(CH=CH)n6(CH2)n7(CH=CH)n8(CH2)n9 The sum of n1 + 2n2 + n3 + 2n4 + n5 +2n6 +n7 +2n8 + n9 is an integer of from 1 to 21, with each of n2, n4, n6 and n8 being independently zero or 1. n1 is equal to zero or an integer of from 1 to 21, n3 is equal to zero or an integer of from 1 to 18, n5 is equal to zero or an integer of from 1 to 15, n7 is equal to zero or an integer of from 1 to 12, n9 is equal to zero or an integer of from 1 to 9, and each of n1 to n9 can be the same or different at each occurrence. Y2 is -CH3, -CO2H or -CH2OH. X' is a hydrolysis promoting group ("HPG"). Also disclosed are compositions comprising this taxane and their use in treating an animal suffering from cancer, e.g., a brain, stomach, lung, colon, prostate, breast or ovarian cancer, or a leukemia, Iymphoma, carcinoma or sarcoma. Cancer treatment with this medicament involves administering an anticancer effective amount of a taxane to the affected animal. Typically, this anticancer effective amount of the taxane is from about 0.1 mg per kg of body weight of the animal to about 1000 mg per kg.