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Pyrazole derivative, or pharmaceutically acceptable salt thereof

A pharmacology and compound technology, applied in the field of pyrazole derivatives or their pharmacologically acceptable salts, can solve the problems of different compound structures, no record or suggestion of TRPM8 inhibitors, different structures, etc.

Active Publication Date: 2018-02-16
KISSEI PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0013] However, the compound described in Non-Patent Document 16 is structurally different from the compound of the present invention, and there is no description or suggestion of a TRPM8 inhibitor
In addition, the compounds described in Patent Documents 1 to 9 are also structurally different from the compounds of the present invention, and TRPM8 inhibitors are not described or suggested

Method used

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  • Pyrazole derivative, or pharmaceutically acceptable salt thereof
  • Pyrazole derivative, or pharmaceutically acceptable salt thereof
  • Pyrazole derivative, or pharmaceutically acceptable salt thereof

Examples

Experimental program
Comparison scheme
Effect test

reference example 1-1-1

[0352] 2-[5-(3-Fluorophenyl)-1H-pyrazol-3-yl]benzoic acid

[0353] According to the method described in Journal of Organic Chemistry, 77(8), 3887-3906; 2012 or a method based thereon, the title compound was obtained. The structural formula, spectral data and purification conditions are shown in Table 3.

reference example 1-1-2～1-1-16

[0355] Using the corresponding raw materials, Reference Examples 1-1-2 to 1-1-16 were synthesized by the same method as Reference Example 1-1-1. In addition, the structural formula, spectrum data, and purification conditions are shown in Table 3-Table 4.

reference example 1-2-1

[0357] 4-Ethynyl-1-fluoro-3-methoxybenzene

[0358] To 4-bromo-1-fluoro-3-methoxybenzene (0.513g), trimethylsilylacetylene (0.737g) in tetrahydrofuran (5mL) was added triethylamine (3.795g), bistri Phenylphosphine palladium(II) chloride (0.175g), copper(I) iodide (0.048g), were stirred at 110°C for 1 hour under microwave irradiation. The mixture was passed through a pad of celite. A saturated aqueous ammonium chloride solution was added to the filtrate, and the crude product was extracted with ethyl acetate. The organic layer was washed with saturated brine, and dried over anhydrous magnesium sulfate. The solvent was distilled off under reduced pressure, and the obtained residue was dissolved in tetrahydrofuran (5 mL), and tetra-n-butylammonium fluoride tetrahydrofuran solution (1 mol / L, 5 mL) was added under ice-cooling, followed by stirring for 30 minutes. After adding saturated aqueous ammonium chloride solution to the reaction mixture, the crude product was extracted wi...

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PUM

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Abstract

The purpose of the present invention is to provide a novel pyrazole derivative, or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition containing same and a pharmaceutical usethereof. The present invention provides a composition having a TRPM8 inhibitory activity and represented by formula (I) (in the formula, ring A is C6-10 aryl or the like, X is CR4a or the like, R1 and R2 are a hydrogen atom or the like, R3 is a hydrogen atom or the like, R4 is a hydrogen atom or the like, ring B is C6-10 aryl or the like, R5 is a hydrogen atom or the like, R6a is a hydrogen atomor the like, R7a is a hydrogen atom or the like, R7b is a hydrogen atom or the like, R6b is a hydrogen atom or the like, R8 is a hydrogen atom or the like, and n is 0, 1, or 2), or a pharmaceuticallyacceptable salt thereof. Furthermore, the composition of the present invention represented by formula (I) or the pharmaceutically acceptable salt thereof can be used as a therapeutic agent or prophylactic agent for diseases or conditions caused by hyperexcitability or disorders of afferent nerves.

Description

technical field [0001] The present invention relates to a pyrazole derivative useful as a medicine or a pharmacologically acceptable salt thereof, a pharmaceutical composition containing the same, and its medical use. Background technique [0002] Transient Receptor Potential (TRP) channels are non-selective cation channels activated by various stimuli such as temperature and chemicals, and are divided into TRPM, TRPA, TRPV, TRPC, TRPP, TRPML, TRPN families . In addition, TRPM1, TRPM2, TRPM3, TRPM4a, TRPM4b, TRPM5, TRPM6, TRPM7, and TRPM8 are known as TRPM families (for example, refer to Non-Patent Document 1). [0003] TRPM8 is the eighth channel of the TRPM family cloned in 2002 (for example, refer to Non-Patent Document 2), and is also known as CMR1 (cold and menthol sensitive receptor-1, cold and menthol sensitive receptor 1), Activated by cold stimulation at 8°C to 28°C or chemical substances (menthol, icilin) ​​that induce low temperature sensation (for example, refe...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D231/12A61K31/415A61K31/4155A61K31/4178A61K31/4192A61K31/4196A61K31/427A61K31/436A61K31/437A61K31/4375A61K31/4439A61K31/444A61K31/454A61K31/4709A61K31/4725A61K31/497A61K31/501A61K31/506A61K31/5377A61P11/02A61P13/10A61P17/04A61P25/04A61P25/06A61P25/22A61P25/24C07D401/04C07D401/12C07D401/14C07D403/12C07D405/14C07D409/14C07D417/12C07D471/04C07D491/052
CPCC07D403/12C07D401/14C07D405/14A61K31/436A61K31/415A61K31/4155A61K31/4178A61K31/4192A61K31/4196A61K31/427A61K31/437A61K31/4375A61K31/4439A61K31/444A61K31/454A61K31/4709A61K31/4725A61K31/497A61K31/501A61K31/506A61K31/5377C07D401/04C07D401/12C07D409/14C07D417/12C07D471/04C07D491/052C07D231/12A61P11/02A61P13/08A61P13/10A61P17/04A61P25/00A61P25/04A61P25/06A61P25/20A61P25/22A61P25/24A61P29/00C07D417/04
Inventor 平泽秀明棚田文也务台阳辅伏见信彦小林淳一木岛喜朗
Owner KISSEI PHARMA
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