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US 12,709,620 B2Granted
Compound for adjusting activity of NMDA receptor, and pharmaceutical composition and use thereof
AssigneeBeijing Greatway Pharmaceutical Technology Co., Ltd.
InventorsWei Gu, Zhaoji Dong, Ruiluan Wang
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Abstract
Provided are a compound for adjusting the activity of an NMDA receptor, and a pharmaceutical composition and the use thereof. In particular, provided are a compound as represented by formula I, a pharmaceutically acceptable salt or ester, a stereoisomer, or a solvate thereof. The compound has the effect of enhancing the activity of the NMDA receptor, and can be used to prepare drugs for preventing/treating depression, anxiety disorder, tension, learning and cognitive defects, neuropathic pain and other diseases,
Claims18
A compound represented by formula I:
- or a pharmaceutically acceptable salt, ester, or stereoisomer thereof wherein,
- Ring A is selected from
- R1 is selected from H, C1-C6 alkyl, aryl-C1-C4 alkyl, C2-C6 acyl, —CONRR′, and natural amino acid fragments;
- when Ring A is
- R2 is selected from H, C1-C6 alkyl, C1-C6 alkoxycarbonyl, C2-C6 acyl, —CONRR′, and natural amino acid fragments;
- when Ring A is
- R2 is selected from C1-C6 alkoxycarbonyl, C2-C6 acyl, —CONRR′, and natural amino acid fragments;
- R3 is selected from H, cyano, 3- to 8-membered nitrogen-containing aliphatic heterocycle-C1-C4 acyl, C1-C6 alkoxycarbonyl, and —CONHR4;
- R and R′ are each independently selected from H and C1-C6 alkyl;
- R4 is selected from H, natural amino acid fragments and carboxylic acid derivatives of the said natural amino acid fragments;
- optionally, the C1-C6 alkyl, aryl-C1-C4 alkyl, C2-C6 acyl, C1-C6 alkoxycarbonyl, —CONRR′, —CONHR4, and natural amino acid fragments are each independently substituted by one or more substituents selected from:
- halogen, amino, hydroxyl, cyano, carboxyl, nitro, C1-C6 alkyl, and C1-C6 alkoxy;
- 3- to 8-membered nitrogen-containing aliphatic heterocycle-C1-C4 acyl is substituted by one or more substituents selected from:
- halogen, amino, hydroxyl, carboxyl, nitro, C1-C6 alkyl, and C1-C6 alkoxy;
- wherein the natural amino acid fragments are selected from the carboxyl or amino residues of the following amino acids:
- Thr, Ser, Val, Gly, Ala, Ile, Leu, Phe, Tyr, Asp, and Gln;
- and, R1, R2 and R3 satisfy:
- (1) R1, R2 and R3 are not H at the same time;
- (2) when R1 and R3 are H, R2 is not Boc;
- (3) when formula I is
- R1 is
- and R3 is H, R2 is not
- (4) when formula I is
- R1 is
- and R3 is H, R2 is not C2-C6 acyl or —CONRR′;
- (5) when formula I is
- R1 and R3 are H, R2 is not acetyl,
- (6) the compound of formula I is not
25 more elements
Dependencies are inferred from the claim text.