1-[(4-hydroxypiperidine-4-yl) methyl] pyridine-2(1H)-one derivatives, preparation method and use thereof

A hydroxypiperidine and methyl technology, which is applied to 1-[(4-hydroxypiperidin-4yl)methyl]pyridin-2(1H)-one derivatives and the fields of their preparation and use, can solve clinical treatment problems The effect is not ideal, etc.

Active Publication Date: 2013-10-23
INST OF PHARMACOLOGY & TOXICOLOGY ACAD OF MILITARY MEDICAL SCI P L A
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  • Abstract
  • Description
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Problems solved by technology

[0008] Vilazodone (Vilazodone, EMD68843), an early discovered arylpiperazine compound, exhibits the effects of SSRIs and 5-HT 1A R partial agonism, showing good antidepressant effect, is currently in Phase III clinical research, but its clinical treatment effect is still not ideal (ME Page, et al.JPharmacol Exp Ther,

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  • 1-[(4-hydroxypiperidine-4-yl) methyl] pyridine-2(1H)-one derivatives, preparation method and use thereof
  • 1-[(4-hydroxypiperidine-4-yl) methyl] pyridine-2(1H)-one derivatives, preparation method and use thereof
  • 1-[(4-hydroxypiperidine-4-yl) methyl] pyridine-2(1H)-one derivatives, preparation method and use thereof

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Embodiment Construction

[0079] All the documents cited in the present invention are incorporated herein by reference in their entirety, and if the meanings expressed in these documents are inconsistent with the present invention, the expression of the present invention shall prevail. In addition, various terms and phrases used in the present invention have common meanings known to those skilled in the art. Even so, the present invention still hopes to make a more detailed description and explanation of these terms and phrases here. The terms and phrases mentioned are as follows: If there is any inconsistency with the known meaning, the meaning expressed in the present invention shall prevail.

[0080] As used herein, the terms "halo", "halogen", "Hal" or "halo" refer to fluorine, chlorine, bromine, and iodine.

[0081]The terms "alkyl", "alkenyl" and "alkynyl" used in the present invention have the common meanings known in the art, which are straight-chain or branched hydrocarbon groups, such as but ...

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Abstract

The present invention relates to N-[(4-hydroxypiperidine-4- Base) methyl] pyridin-2 (1H)-one derivatives, their stereoisomers, their pharmaceutically acceptable salts and their solvates, and their preparation methods, and their use in the prevention or treatment of 5-HT system dysfunction Related central nervous system diseases such as depression, anxiety, cognitive deficits, mania, schizophrenia, pain, etc., or used as a tool drug to study 5-HT function and its 5-HT dysfunction related diseases, and pharmaceutical compositions containing these compounds. Each substituent in formula I is as described in the specification.

Description

technical field [0001] The present invention relates to having 5-hydroxytryptamine 1A (5-HT) as shown in general formula I 1A ) receptor ligands and serotonin reuptake inhibitors (SSRI) dual active N-[(4-hydroxypiperidin-4-yl)methyl]pyridin-2(1H)-one derivatives, their stereoiso Constructs, their pharmaceutically acceptable salts and their solvates, and their preparation methods, and their use in the prevention or treatment of central nervous system diseases such as depression, anxiety, cognitive deficits, and mania associated with 5-HT system dysfunction schizophrenia, pain, etc., or as a tool drug for studying 5-HT function and diseases related to 5-HT dysfunction, and pharmaceutical compositions containing these compounds. Background technique [0002] 5-hydroxytryptamine (5-HT), also known as serotonin, is not only an important monoamine neurotransmitter, but also a vasoactive substance. 5-HT is widely distributed in the central nervous system (CNS) , participate in th...

Claims

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Application Information

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IPC IPC(8): C07D401/06A61K31/4545A61P25/24A61P25/18A61P25/28A61P25/04A61P25/00
CPCC07D401/06A61P1/12A61P1/14A61P11/00A61P13/12A61P15/00A61P25/00A61P25/04A61P25/16A61P25/18A61P25/20A61P25/22A61P25/24A61P25/28A61P25/36A61P29/00A61P37/02A61P43/00A61P5/00
Inventor 李云峰杨日芳张有志李永臻金增亮李鹏袁莉恽榴红赵楠张城徐晓丹赵如胜陈红霞薛瑞秦娟娟王真真姚佳志
Owner INST OF PHARMACOLOGY & TOXICOLOGY ACAD OF MILITARY MEDICAL SCI P L A
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