2-(aryl-2-yl) morpholine and deuterated derivative thereof, preparation method therefor and application thereof
AssigneesShanghai Hansoh Biomedical Co., Ltd., Jiangsu Hansoh Pharmaceutical Group Co., Ltd.
InventorsYidong Su, Kailong Li, Zhiqiang Huang, Haining Deng, Xiaohan Zhou, Wensheng Yu
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Abstract
Provided are a 2-(aryl-2-yl) morpholine and a deuterated derivative thereof, a preparation method therefor and an application thereof. In particular, involved are the use of a compound shown by general formula (V) in the treatment of central nervous system diseases, a deuterated compound thereof, a preparation method of deuterated compound, a pharmaceutical composition containing the deuterated compound, and the use thereof as a TAAR1 agonist in the treatment of central nervous system diseases.
Claims21
A compound of formula (I), a stereoisomer thereof or a pharmaceutically acceptable salt thereof,
- wherein,
- R1, R2, R3, R4, R5, and R9 are each independently selected from the group consisting of hydrogen, deuterium, halogen, amino, hydroxyl, cyano, C1-6 alkyl, C1-6 alkoxy, C1-6 deuterated alkyl, C1-6 deuterated alkoxy, C1-6 haloalkyl and C3-12 cycloalkyl, which can be each optionally further substituted;
- R6a, R6b, R7a, R7b, R8a and R8b are each independently selected from the group consisting of hydrogen and deuterium;
- n is 0, 1, 2, or 3;
- with the proviso that, at least one of R1, R2, R3, R4, R5, R9, R6a, R6b, R7a, R7b,
- R8a and R8b contains D.
A compound of formula (I′), a stereoisomer thereof or a pharmaceutically acceptable salt thereof,
- wherein,
- R1, R2, R3 and R4 are each independently selected from the group consisting of hydrogen, deuterium, halogen, amino, hydroxyl, cyano, C1-6 alkyl, C1-6 deuterated alkyl, C1-6 haloalkyl and C3-12 cycloalkyl;
- R5, R6a, R6b, R7a, R7b, R8a and R8b are each independently selected from the group consisting of hydrogen and deuterium;
- with the proviso that,
- R1, R2, R3, R4, R5, R6a, R6b, R7a, R7b, R8a and R8b are not hydrogen at the same time, and when R1, R2, R3 and R4 are each independently selected from the group consisting of halogen, cyano, hydroxyl, amino, C1-6 alkyl and C1-6 haloalkyl, at least one of R5, R6a, R6b, R7a, R7b, R8a and R8b is D.
A compound of formula (V), a stereoisomer thereof or a pharmaceutically acceptable salt thereof,
- wherein,
- M is selected from the group consisting of N and CRa,
- Ra, R1, R2, R3 and R4 are each independently selected from the group consisting of hydrogen, deuterium, halogen, amino, hydroxyl, cyano, C1-6 alkyl, C1-6 deuterated alkyl, C1-6 haloalkyl and C3-12 cycloalkyl;
- R5, R7a and R7b are each independently selected from the group consisting of hydrogen and deuterium, and at least one of them is deuterium.
A compound, the stereoisomer thereof or the pharmaceutically acceptable salt thereof, which is
(canceled)
Dependencies are inferred from the claim text.