SENTER, PETER D.,DORONINA, SVETLANA,TOKI, BRIAN E.
申请号：
ES11165204
公开号：
ES2544527T3
申请日:
2003.07.31
申请国别(地区):
ES
年份:
2015
代理人:
摘要：
A compound of formula Ib: ** ** Formula and pharmaceutically acceptable salts and solvates thereof wherein, L- is a Ligand unit -A- is a unit extensor a is 0 or 1 each -W- is independently an amino acid unit -Y- is a spacer unit w is an integer ranging from 2 to 12 y is 0, 1 or 2 p ranges from 1 to about 20 and -D is a Drug unit of the formula wherein, independently at each location: R1 is selected from -H, -C1-C8 alkyl, -C3-C8 carbocycle and R2 is selected from -H and -C1-C8 alkyl or R1 and R2 together, they have the formula - (CRaRb) n- wherein Ra and Rb are independently selected from -H, -C1-C8 alkyl and -C3-C8 carbocycle and n is selected from 2, 3, 4, 5 and 6 and form a ring with the nitrogen atom to which they are attached R3 is selected from -H, -C1-C8 alkyl, -C3-C8 carbocycle, -O- (C1-C8 alkyl), aryl, -C1-C8 alkyl-aryl, -C1-C8 alkyl- (C3-C8 carbocycle ), -C3-C8 heterocycle and -C1-C8 alkyl- (C3-C8 heterocycle) R4 is selected from -H, -C1-C8 alkyl, -C3-C8 carbocycle, -O- (C1-C8 alkyl), aryl, -C1-C8 alkyl-aryl, -C1-C8 alkyl- (C3-C8 carbocycle ), -C3-C8 heterocycle and -C1-C8 alkyl- (C3-C8 heterocycle) wherein R 5 is selected from -H and -methyl or R4 and R5 together have the formula - (CRaRb) n- wherein Ra and Rb are independently selected from -H, -C1-C8 alkyl and -C3-C8 carbocycle and n is selected from 2, 3, 4, 5 and 6 and form a ring with the carbon atom to which they are attached R6 is selected from -H and -C1-C8 alkyl R7 is selected from -H, -C1-C8 alkyl, -C3-C8 carbocycle, -O- (C1-C8 alkyl), -aryl, -C1-C8 alkyl-aryl, -C1-C8 alkyl- (C3-C8 carbocycle), -C3-C8 heterocycle and -C1-C8 alkyl- (C3-C8 heterocycle) each R8 is independently selected from -H, -OH, -C1-C8 alkyl, -C3-C8 carbocycle and -O- (C1-C8 alkyl) R9 is selected from -H and -C1-C8 alkyl R10 is selected from ** ** Formula X is -O-, -S-, -NH- or -N (R14) -, where X is bonded to Y when y is 1 or 2, or X is joined to W when y is 0 Z is -O-, -S-, -NH- or -N (R14) - R11 is selected from -H, -OH, NH2
