Conjugate for targeting therapy
The present disclosure provides a novel conjugate or a pharmaceutically acceptable salt thereof, wherein the conjugate has an active pharmaceutical moiety or a prodrug thereof, a targeting module and a linker therebetween. The conjugate or a pharmaceutically acceptable salt thereof is useful for treating a disease, recurrence or progression in a subject or increasing the likelihood of survival over a relevant period in a subject diagnosed with a disease.
1 . A conjugate represented by Formula III or a pharmaceutically acceptable salt thereof,
wherein:
R is OH or
wherein
A is 5-fluorouracil (5-FU), SN-38, or irinotecan; and
wherein
R 1 is —S—S—(CH 2 ) n —OC(O)—(CH 2 ) m —, —S—S—(CH 2 ) n —C(O)O—(CH 2 ) m — or
n is an integer of 2 to 9, and
m is 0 or 1;
wherein A is connected to (CH 2 ) m — in R 1 .
2 . The conjugate of claim 1 or a pharmaceutically acceptable salt thereof, wherein when R 1 is —S—S—(CH 2 ) n —OC(O)—(CH 2 ) m —, n is 2, and m is 0.
3 . The conjugate of claim 1 or a pharmaceutically acceptable salt thereof, wherein when R 1 is
n is 4, and m is 1.
4 . The conjugate of claim 1 or a pharmaceutically acceptable salt thereof, wherein when R 1 is —S—S—(CH 2 ) n —C(O)O—(CH 2 ) m —, n is 2, and m is 0.
5 . A conjugate or a pharmaceutically acceptable salt thereof, which is selected from the group consisting of:
wherein R is OH or
6 . A pharmaceutical composition comprising the conjugate of claim 1 .
7 . The pharmaceutical composition of claim 6 , which further comprises a therapeutic agent.
8 . The conjugate of claim 1 or a pharmaceutically acceptable salt thereof, which is selected from the group consisting of:
wherein R is OH or
9 . A pharmaceutical composition comprising the conjugate of claim 5 .
10 . The pharmaceutical composition of claim 9 , further comprising a therapeutic agent.