Patent ID: 8703714

Claim:
An antibody-drug conjugate having Formula Ia′: Ab A a -W w -Y y -D) p Ia′ or a pharmaceutically acceptable salt thereof, wherein: Ab is an antibody A is a Stretcher unit, a is 1, each W is independently an Amino Acid unit, w is an integer ranging from 2 to 12, Y is a Spacer unit, and y is 1 or 2, p ranges from 1 to about 20, D is a drug moiety of Formula D F : wherein the wavy line of D F indicates the covalent attachment site to Y: R 2 is selected from the group consisting of H and C 1 -C 8 alkyl; R 3 is selected from the group consisting of H, C 1 -C 8 alkyl, C 3 -C 8 carbocycle, aryl, C 1 -C 8 alkyl-aryl, C 1 -C 8 alkyl-(C 3 -C 8 carbocycle), C 3 -C 8 heterocycle and C 1 -C 8 alkyl-(C 3 -C 8 heterocycle); R 4 is selected from the group consisting of H, C 1 -C 8 alkyl, C 3 -C 8 carbocycle, aryl, C 1 -C 8 alkyl-aryl, C 1 -C 8 alkyl-(C 3 -C 8 carbocycle), C 3 -C 8 heterocycle and C 1 -C 8 alkyl-(C 3 -C 8 heterocycle); R 5 is selected from the group consisting of H and methyl; or R 4 and R 5 jointly form a carbocyclic ring and have the formula —(CR a R b ) n — wherein R a and R b are independently selected from the group consisting of H, C 1 -C 8 alkyl and C 3 -C 8 carbocycle and n is selected from the group consisting of 2, 3, 4, 5 and 6; R 6 is selected from the group consisting of H and C 1 -C 8 alkyl; R 7 is selected from the group consisting of H, C 1 -C 8 alkyl, C 3 -C 8 carbocycle, aryl, C 1 -C 8 alkyl-aryl, C 1 -C 8 alkyl-(C 3 -C 8 carbocycle), C 3 -C 8 heterocycle and C 1 -C 8 alkyl-(C 3 -C 8 heterocycle); each R 8 is independently selected from the group consisting of H, OH, C 1 -C 8 alkyl, C 3 -C 8 carbocycle and O—(C 1 -C 8 alkyl); R 9 is selected from the group consisting of H and C 1 -C 8 alkyl; R 10 is aryl or C 3 -C 8 heterocycle; Z is O, S, NH, or NR 12 , wherein R 12 is C 1 -C 8 alkyl; R 11 is H, C 1 -C 20 alkyl, aryl, C 3 -C 8 heterocycle, —(R 13 O) m —R 14 , or —(R 13 O) m —CH(R 15 ) 2 ; m is an integer ranging from 1-1000; R 13 is C 2 -C 8 alkyl; R 14 is H or C 1 -C 8 alkyl; each occurrence of R 15 is independently H, COOH, —(CH 2 ) n —NR 16 ) 2 , —(CH 2 ) n —SO 3 H, or —(CH 2 ) n —SO 3 —C 1 -C 8 alkyl; each occurrence of R 16 is independently H, C 1 -C 8 alkyl, or —(CH 2 ) n —COOH; and n is an integer ranging from 0 to 6.