Steroid derivative regulators, method for preparing the same, and uses thereof
AssigneesJiangsu Hansoh Pharmaceutical Group Co., Ltd., Shanghai Hansoh Biomedical Co., Ltd.
InventorsYidong SU, Haining DENG, Xiaopo CHEN, Rudi BAO, Fujun ZHANG
Life of this patent
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Abstract
Steroid derivative regulators, a method for preparing the same, and uses thereof are described. Specifically, a compound of formula (I), a preparation method therefor, a pharmaceutical composition containing the compound, and uses thereof as a regulator the of GABAA receptor for treating depression, convulsion, Parkinson's disease, and nervous system diseases are described, wherein the substituents of the formula (I) are as defined in the description.
Claims19
-26. (canceled)
A compound of formula (IV), the stereoisomer thereof, or the pharmaceutically acceptable salt thereof:
- wherein:
- Z is selected from the group consisting of —CR23R24—, —(CH2)n1NR23— and —CH2O—;
- ring A is selected from the group consisting of cycloalkyl, heterocyclyl, aryl and heteroaryl, wherein the cycloalkyl, heterocyclyl, aryl and heteroaryl are each optionally further substituted by one or more substituents selected from the group consisting of deuterium atom, alkyl, haloalkyl, halogen, amino, oxo, nitro, cyano, hydroxy, alkenyl, alkynyl, alkoxy, haloalkoxy, hydroxyalkyl, cycloalkyl, heterocyclyl, aryl, heteroaryl, —(CH2)n1R25, —(CH2)n1OR25, —(CH2)n1SR25, —(CH2)n1C(O)R25, —(CH2)n1C(O)OR25, —(CH2)n1S(O)m1R25, —(CH2)n1NR25R26, —(CH2)n1C(O)NR25R26, —(CH2)n1C(O)NHR25, —(CH2)n1NR25C(O)R26 and —(CH2)n1NR25S(O)m1R26;
- each Ra is identical or different and each is selected from the group consisting of hydrogen atom, deuterium atom, alkyl, deuterated alkyl, haloalkyl, alkoxy, haloalkoxy, halogen, amino, nitro, hydroxy, cyano, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl, heteroaryl, —(CH2)n1R23, —(CH2)n1OR23, —(CH2)n1SR23, —(CH2)n1C(O)R23, —(CH2)n1C(O)OR23, —(CH2)n1S(O)m1R23, —(CH2)n1S(O)(NR23)R24, —(CH2)n1NR23R24, —(CH2)n1C(O)NR23R24, —(CH2)n1NR23C(O)R23 and —(CH2)n1NR23S(O)m1R24, wherein the alkyl, haloalkyl, cycloalkyl, heterocyclyl, aryl and heteroaryl are each optionally further substituted by one or more substituents selected from the group consisting of deuterium atom, alkyl, haloalkyl, halogen, amino, oxo, nitro, cyano, hydroxy, alkenyl, alkynyl, alkoxy, haloalkoxy, hydroxyalkyl, cycloalkyl, heterocyclyl, aryl, heteroaryl, —(CH2)n1R25, —(CH2)n1OR25, —(CH2)n1SR25, —(CH2)n1C(O)R25, —(CH2)n1C(O)OR25, —(CH2)n1S(O)m1R25, —(CH2)n1NR25R26, —(CH2)n1C(O)NR25R26, —(CH2)n1C(O)NHR25, —(CH2)n1NR25C(O)R26 and —(CH2)n1NR25S(O)m1R26;
- R15a is selected from the group consisting of alkyl, haloalkyl, alkoxy, halogen, amino, hydroxy, cycloalkyl, heterocyclyl, aryl, heteroaryl, —(CH2)n1R23, —(CH2)n1OR23, —(CH2)n1SR23, —(CH2)n1S(O)m1R23 and —(CH2)n1NR23R24, wherein the alkyl, haloalkyl, cycloalkyl, heterocyclyl, aryl and heteroaryl are each optionally further substituted by one or more substituents selected from the group consisting of deuterium atom, alkyl, haloalkyl, halogen, amino, oxo, nitro, cyano, hydroxy, alkenyl, alkynyl, alkoxy, haloalkoxy, hydroxyalkyl, cycloalkyl, heterocyclyl, aryl and heteroaryl;
- R16a is selected from the group consisting of hydrogen atom, alkyl, haloalkyl, alkoxy, halogen, amino, hydroxy, cycloalkyl, heterocyclyl, aryl, heteroaryl, —(CH2)n1R23, —(CH2)n1OR23, —(CH2)n1SR23, —(CH2)n1S(O)m1R23 and —(CH2)n1NR23R24;
- or, R15a and R16a form a cycloalkyl or heterocyclyl, wherein the cycloalkyl or heterocyclyl is optionally further substituted by one or more substituents selected from the group consisting of deuterium atom, alkyl, haloalkyl, halogen, amino, oxo, nitro, cyano, hydroxy, alkenyl, alkynyl, alkoxy, haloalkoxy, hydroxyalkyl, cycloalkyl, heterocyclyl, aryl and heteroaryl, and R15a and R16a are not hydrogen at the same time;
- R23 and R24 are each selected from the group consisting of hydrogen atom, deuterium atom, alkyl, deuterated alkyl, haloalkyl, alkoxy, haloalkoxy, halogen, amino, nitro, hydroxy, cyano, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl and heteroaryl, wherein the alkyl, haloalkyl, cycloalkyl, heterocyclyl, aryl and heteroaryl are each optionally further substituted by one or more substituents selected from the group consisting of deuterium atom, alkyl, haloalkyl, halogen, amino, oxo, nitro, cyano, hydroxy, alkenyl, alkynyl, alkoxy, haloalkoxy, hydroxyalkyl, cycloalkyl, heterocyclyl, aryl, heteroaryl, —(CH2)n1R25, —(CH2)n1OR25, —(CH2)n1SR25, —(CH2)n1C(O)R25, —(CH2)n1C(O)OR25, —(CH2)n1S(O)m1R25, —(CH2)n1NR25R26, —(CH2)n1C(O)NR25R26, —(CH2)n1C(O)NHR25, —(CH2)n1NR25C(O)R26 and —(CH2)n1NR25S(O)m1R26;
- R25 and R26 are identical or different and are each independently selected from the group consisting of hydrogen atom, deuterium atom, alkyl, deuterated alkyl, haloalkyl, hydroxy, amino, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl and heteroaryl, wherein the alkyl, cycloalkyl, heterocyclyl, aryl and heteroaryl are each optionally further substituted by one or more substituents selected from the group consisting of deuterium atom, alkyl, halogen, hydroxy, amino, oxo, nitro, cyano, alkenyl, alkynyl, alkoxy, hydroxyalkyl, cycloalkyl, heterocyclyl, aryl and heteroaryl;
- x is an integer of 0, 1, 3, 4 or 5;
- m1 is an integer of 0, 1 or 2;
- and
- n1 is an integer of 0, 1, 2, 3, 4 or 5.
A compound selected from the group consisting of:
- or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof.
Dependencies are inferred from the claim text.