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US 12,565,511 B2Granted
SOS1 inhibitor containing phosphorus
AssigneeChia Tai Tianqing Pharmaceutical Group Co., Ltd.
InventorsYinsheng Zhang, Baomin Liu, Zhengbang Chen, Jinfa Hu, Yuchen Chen, Kewen Sun, Jinan Wang, Lijuan Zhu
Life of this patent
Estimating the term…
Abstract
The present application relates to the field of pharmaceutical chemistry, relates to an SOS1 inhibitor containing phosphorus, i.e., a compound of formula (I) and a preparation method therefor, and a pharmaceutical composition containing the compound, and relates to use thereof in the preparation of a drug for treating a disease and/or disorder related to SOS1 or regulated by SOS1.
Claims19
A compound of formula (I), a stereoisomer thereof or a pharmaceutically acceptable salt thereof:
- wherein,
- X and Y are each independently selected from the group consisting of CRa, C(O), N and NRb;
- “” represents a single bond or a double bond depending on X and Y;
- Ra is selected from the group consisting of hydrogen, hydroxy, halogen, cyano, C1-6 alkyl and C1-6 alkoxy, wherein the C1-6 alkyl or C1-6 alkoxy is optionally substituted with one or more deuterium or halogens;
- Rb is selected from the group consisting of hydrogen, C1-6 alkyl and C1-6 alkoxy;
- R1 and R2 are each independently selected from the group consisting of C1-6 alkyl, NH(Rc)—C1-6 alkyl- and N(Rc)(C1-6 alkyl)-C1-6 alkyl-, or R1, R2 and the phosphorus atom to which they are both connected together form 5-10 membered heterocyclyl, wherein the C1-6 alkyl or 5-10 membered heterocyclyl is optionally substituted with one or more Rc;
- each Rc is independently selected from the group consisting of hydrogen, O═, HN═, C1-6 alkyl-N═, C1-6 alkyl-, C1-6 alkyl-C(O)—, C1-6 alkyl-S(O)2—, 3-6 membered cycloalkyl-S(O)2—, C1-6 alkyl OC(O)—, C1-6 alkyl-O—C1-6 alkyl-, C1-6 alkyl-O—C1-6 alkyl-C(O)—, amino-C(O)—, mono(C1-6 alkyl)amino-C(O)—, di(C1-6 alkyl)amino-C(O)—, amino-C1-6 alkyl-C(O)—, mono(C1-6 alkyl)amino-C1-6 alkyl-C(O)—, di(C1-6 alkyl)amino-C1-6 alkyl-C(O)—, amino-C(O)—C1-6 alkyl-, mono(C1-6 alkyl)amino-C(O)—C1-6 alkyl-, di(C1-6 alkyl)amino-C(O)—C1-6 alkyl-, 3-6 membered cycloalkyl-, 3-6 membered cycloalkyl-C(O)—, 3-6 membered cycloalkyl-C1-6 alkyl-, 3-6 membered heterocycloalkyl-, 3-6 membered heterocycloalkyl-C(O)—, 3-6 membered heterocycloalkyl-C1-6 alkyl-, C6-10 aryl-C1-6 alkyl- and C1-6 alkyl-substituted with one or more hydroxy or cyano, wherein the Rc is optionally substituted with one or more halogens when it is not hydrogen and O═;
- ring A is selected from the group consisting of C6-10 aryl, 5-10 membered heteroaryl, 8-12 membered fused ring and 8-12 membered fused heterocyclic ring;
- n is 0, 1, 2 or 3;
- each R3 is independently selected from the group consisting of amino, nitro, halogen, C1-8 alkyl-, 3-6 membered cycloalkyl- and phenyl, wherein the C1-8 alkyl, 3-6 membered cycloalkyl or phenyl is optionally substituted with one or more Rd;
- Rd is selected from the group consisting of hydroxy, halogen and C1-6 alkyl-NH—C1-6 alkyl-;
- R4 and R5 are each independently selected from the group consisting of hydrogen, deuterium and C1-6 alkyl, wherein the C1-6 alkyl is optionally substituted with one or more halogens;
- and
- R6 is selected from the group consisting of hydrogen, halogen and C1-6 alkyl, wherein the C1-6 alkyl is optionally substituted with one or more halogens.
11 more elements
Dependencies are inferred from the claim text.