Inhibitor of prostate specific membrane antigen and pharmaceutical use thereof
AssigneesTianjin Hengrui Medicine Co., Ltd., Jiangsu Hengrui Pharmaceuticals Co., Ltd.
InventorsMengzhe WANG, Shunguang ZHOU, Liang YU, Lidong WANG, Libo ZHAO, Jiyun SUN, Feihu GUO, Xin LI
Life of this patent
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Abstract
An inhibitor of a prostate specific membrane antigen and a pharmaceutical use thereof. Specifically, the present solution belongs to the field of radiopharmaceuticals and relates to a compound represented by formula (IV) or a pharmaceutically acceptable salt thereof.
Claims23
A compound represented by formula (IV) or a pharmaceutically acceptable salt thereof,
- wherein:
- Q is selected from the group consisting of H and a protecting group, preferably from H;
- R1 and R2 are each independently selected from the group consisting of H and C1-4 alkyl and are preferably both H;
- the C1-4 alkyl is optionally substituted with one or more substituents P or is unsubstituted;
- each occurrence of Q, R1, and R2 may be the same or different;
- Y1 is S or O, preferably O;
- T is selected from the group consisting of —NR4(CO)—, —NR4 (SO2)—, and —NR4 (CH2)—;
- R4 is selected from the group consisting of H, C1-6 alkyl, 6-10 membered aryl, and 5-12 membered heteroaryl;
- the C1-6 alkyl, 6-10 membered aryl, or 5-12 membered heteroaryl is optionally substituted with one or more substituents P or is unsubstituted;
- ring A is selected from 3-12 membered nitrogen-containing heterocyclyl, wherein the 3-12 membered nitrogen-containing heterocyclyl is optionally substituted with one or more substituents P or is unsubstituted;
- W is selected from the group consisting of 6-10 membered aryl and 5-12 membered heteroaryl;
- the −10 membered aryl or 5-12 membered heteroaryl is optionally substituted with one or more substituents P or is unsubstituted;
- the substituents P are selected from the group consisting of C1-C6 alkyl, halogen, deuterium, hydroxy, sulfhydryl, —NRiRj, oxo, thio, —C(O)Rk, —C(O)ORk, —S(O)Rk, —S(O)ORk, —S(O)(O)Rk, —S(O)(O)ORk, —C(S)Rk, nitro, cyano, C1-C6 alkoxy, C1-C6 alkylthioether group, C2-C6 alkenyl, C2-C6 alkynyl, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocyclyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl, 8- to 12-membered fused cycloaryl, and 5- to 12-membered fused heteroaryl;
- Ri and Rj are each independently selected from the group consisting of a hydrogen atom, hydroxy, C1-C6 alkyl, and C1-C6 alkoxy;
- Rk is independently selected from the group consisting of a hydrogen atom, C1-C6 alkyl, C1-C6 haloalkyl, C1-C6 alkoxy, hydroxy, and —NRiRj, wherein the alkyl, alkoxy, or haloalkyl is optionally substituted with one or more substituents selected from the group consisting of C1-C6 alkyl, halogen, hydrogen, sulfhydryl, —NRiRj, oxo, thio, carboxyl, nitro, cyano, C1-C6 alkoxy, C1-C6 alkylthioether group, C2-C6 alkenyl, C2-C6 alkynyl, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocyclyl, 6- to 10-membered aryl, and 5- to 10-membered heteroaryl;
- y, z, g, and h are each independently integers of 0-6;
- R3 is selected from the group consisting of H and a chelating agent.
A compound represented by formula (IV) or a pharmaceutically acceptable salt thereof, being
- wherein the chelating agent comprises a radionuclide, and the radionuclide is 68Ga.
A compound represented by formula (IV) or a pharmaceutically acceptable salt thereof, being
- wherein the chelating agent comprises a radionuclide and the radionuclide is 177Lu.
(canceled)
(canceled)
A preparation method for a compound represented by formula (IV) or a pharmaceutically acceptable salt thereof, wherein the compound represented by formula (IV) is the compound represented by formula v or a pharmaceutically acceptable salt thereof;
- the preparation method comprises the step of removing tert-butyl groups from the compound represented by formula v-5:
(canceled)
Dependencies are inferred from the claim text.