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US 12,459,931 B2Granted
Benzothiophene derivative regulator, preparation method therefor and use thereof
AssigneesShanghai Hansoh Biomedical Co., Ltd., Jiangsu Hansoh Pharmaceutical Group Co., Ltd.
InventorsYidong Su, Song Li, Xiaopo Chen, Jun Wang
Life of this patent
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Abstract
A nitrogen-containing ring derivative regulator, a preparation method therefor and use thereof. In particular, the present invention relates to a compound as represented by general formula (I), a preparation method therefor, a pharmaceutical composition containing the compound, and use thereof as a G protein-coupled receptor regulator in the treatment or prevention of central nervous system diseases and/or mental diseases.
Claims16
A compound of formula (IV-A), a stereoisomer thereof or a pharmaceutically acceptable salt thereof:
- wherein:
- is selected from the group consisting of single bond and a double bond;
- R2 is selected from the group consisting of hydrogen, cyano, halogen, C1-6 alkyl, C1-6 haloalkyl and C3-6 cycloalkyl;
- or, two R2 on the same or different carbon atoms are bonded to form a C3-8 cycloalkyl or 3 to 8 membered heterocyclyl, wherein the C3-8 cycloalkyl or 3 to 8 membered heterocyclyl is optionally further substituted by one or more substituents selected from the group consisting of deuterium, C1-6 alkyl, halogen, amino, oxo, thioxo, cyano, hydroxy, C3-8 alkoxy, C3-8 haloalkoxy and C3-8 hydroxyalkyl;
- R3 is selected from the group consisting of hydrogen, halogen, C1-6 alkyl, C1-6 haloalkyl, C1-6 alkoxy, C1-6 haloalkoxy, hydroxy, cyano, C2-6 alkenyl and C2-6 alkynyl;
- R4 is selected from the group consisting of hydrogen and C1-6 alkyl;
- R5 is selected from the group consisting of C1-6 alkyl, C3-8 cycloalkyl, 3 to 8 membered heterocyclyl, C6-14 aryl, 5 to 14 membered heteroaryl, —(CH2)n1Raa, —C(O)Raa, —C(O)NRaaRbb, —C(O)(CH2)n1Raa, —C(O)NRaa(CH2)n1Rbb, —S(O)2Raa, —(CH2)n1S(O)(═NRaa)Rbb, —S(O)m1NRaaRbb and —C(O)ORaa, wherein the C1-6 alkyl, C3-8 cycloalkyl, 3 to 8 membered heterocyclyl, C6-14 aryl and 5 to 14 membered heteroaryl are each optionally further substituted by one or more substituents selected from the group consisting of cyano, halogen, C1-6 alkyl and C1-6 alkoxy;
- or, R4 and R5 are bonded to form a 3 to 8 membered heterocyclyl or 5 to 14 membered heteroaryl, which is optionally further substituted by one or more substituents selected from the group consisting of C1-6 alkyl, halogen, amino, oxo, thioxo, cyano, hydroxy, C3-8 alkoxy, C3-8 haloalkoxy, C3-8 hydroxyalkyl, —C(O)Rcc and —C(O)NRccRdd;
- Raa and Rbb are each independently selected from the group consisting of hydrogen, amino, C1-6 alkyl, C1-6 haloalkyl, C1-6 alkoxy, C3-8 cycloalkyl, 3 to 8 membered heterocyclyl, C6-14 aryl and 5 to 14 membered heteroaryl, wherein the amino, C1-6 alkyl, C1-6 haloalkyl, C1-6 alkoxy, C3-8 cycloalkyl, 3 to 8 membered heterocyclyl, C6-14 aryl and 5 to 14 membered heteroaryl are each optionally further substituted by one or more substituents selected from the group consisting of halogen, hydroxy, cyano, oxo, C1-6 alkyl, C1-6 haloalkyl, C1-6 alkoxy, C3-8 cycloalkyl, 3 to 8 membered heterocyclyl, C6-14 aryl and 5 to 14 membered heteroaryl;
- or, Raa and Rbb together with the adjacent nitrogen atom are bonded to form a 4 to 10 membered heterocyclyl, which is optionally further substituted by one or more substituents selected from the group consisting of halogen, hydroxy, cyano, oxo, C1-6 alkyl, C1-6 haloalkyl, C1-6 alkoxy and C1-6 hydroxyalkyl;
- Rcc and Rdd are each independently selected from the group consisting of hydrogen, amino, C1-6 alkyl, C1-6 haloalkyl, C1-6 alkoxy, C3-8 cycloalkyl, 3 to 8 membered heterocyclyl, C6-14 aryl and 5 to 14 membered heteroaryl, wherein the amino, C1-6 alkyl, C1-6 haloalkyl, C1-6 alkoxy, C3-8 cycloalkyl, 3 to 8 membered heterocyclyl, C6-14 aryl and 5 to 14 membered heteroaryl are each optionally further substituted by one or more substituents selected from the group consisting of halogen, hydroxy, cyano, oxo, C1-6 alkyl, C1-6 haloalkyl and C1-6 alkoxy;
- y is 0, 1, 2, 3 or 4;
- z is 0, 1, 2, 3 or 4;
- m is 1 or 2;
- and
- n1 is 0, 1, 2 or 3;
- wherein the compound of formula (IV-A) does not comprise compounds
14 more elements
Dependencies are inferred from the claim text.