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Keto-substituted heterocyclic compounds and their anesthetic effects

A compound, unsubstituted technology, used in anesthetics, drug combinations, organic chemistry, etc.

Active Publication Date: 2022-06-03
CHENGDU MFS PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] However, with the clinical use, the disadvantages of etomidate gradually emerged, and thus limited its application.

Method used

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  • Keto-substituted heterocyclic compounds and their anesthetic effects
  • Keto-substituted heterocyclic compounds and their anesthetic effects
  • Keto-substituted heterocyclic compounds and their anesthetic effects

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0111]

[0113]

[0115]

[0117]

[0119]

[0121]

[0122] At room temperature, compound A-2 (3.5 g, 16.2 mmol), N,O-dimethylhydroxylamine

[0124]

[0127]

[0130]

[0132] At room temperature, the PTSA.H

[0133]

[0135]

[0137] Compound C2: 91 mg, ESI [M+H]

[0138]

[0139] Compound C3: 39 mg, ESI [M+H]

[0140]

[0142]

[0144]

[0146]

[0147] Compound C7: 46 mg, ESI [M+H]

[0148]

Embodiment 2

[0150]

[0152]

Embodiment 3

[0154]

[0156]

[0159]

[0161]

[0163]

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PUM

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Abstract

The invention discloses a ketone-substituted heterocyclic compound and its anesthetic effect. Specifically provided are compounds represented by formula I, or pharmaceutically acceptable salts thereof, or stereoisomers thereof, or deuterated derivatives thereof. The ketone-substituted heterocyclic compound provided by the present invention has a good inhibitory effect on the central nervous system, can produce sedative, hypnotic and / or general anesthesia, and can control status epilepticus; the ketone-substituted heterocyclic compound maintains excellent anesthetic activity At the same time, it also has the characteristics of rapid onset and rapid recovery; at the same time, the ketone-substituted heterocyclic compound has almost no inhibitory effect on the function of the adrenal cortex, and has little side effects, which solves the technical problems in this field. Or the preparation of drugs for sedation, hypnosis and / or general anesthesia and drugs for controlling status epilepticus provides a new option.

Description

Ketone Substituted Heterocyclic Compounds and Their Anesthetic Effects technical field The invention belongs to the field of medicinal chemistry, be specifically related to a class of ketone-substituted heterocyclic compounds, and this class of compounds in Use in the preparation of drugs for sedation, hypnosis and / or general anesthesia and for the preparation of drugs capable of controlling status epilepticus. Background technique [0002] Heterocyclic compounds refer to the atoms constituting the ring containing atoms other than carbon (including but not limited to N, O, S atoms) a class of cyclic organic compounds. Heterocyclic compounds exist widely in nature, and most of the important compounds related to biology For heterocyclic compounds, such as nucleic acids, antibiotics, hormones, pigments and alkaloids. Heterocyclic compounds are structurally diverse, common Cyclic compounds include furan and its derivatives, thiophene and its derivatives, pyridine and its...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D231/12A61K31/415A61P23/00A61P25/20
CPCC07D231/12A61P23/00A61P25/20Y02P20/55
Inventor 刘进张文胜马海军王昌华解振彪
Owner CHENGDU MFS PHARMA CO LTD
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