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Azole derivatives

A technology of azole derivatives and medicinal salts, which is applied in the field of azole derivatives and can solve the problems of no reports of compounds with azole skeletons

Active Publication Date: 2016-12-14
TAISHO PHARMACEUTICAL CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there is no report on the compounds with azole skeletons disclosed in the present invention

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment A－01

[1400] ·Example A-01: 2-[2-(3-chlorophenyl)-4-{4-[2-(piperidin-1-yl)ethyl]phenyl}-1H-imidazol-1-yl Synthesis of ]-N-(propane-2-yl)acetamide

[1401] 【Chemical 226】

[1402]

[1403] CHCl of the compound (533 mg) obtained in Reference Example P-A04 3 (11mL) solution, add Et 3 N (0.28 mL), MsCl (0.12 mL) was added under ice-cold conditions, and stirred at room temperature for 2.5 hours. Under ice-cold conditions, after adding water, use CHCl 3 Extract and concentrate the filtrate under reduced pressure. The obtained residue was subjected to OH silica gel column chromatography (mobile phase: CHCl 3 / EtOAc=70 / 30; v / v) to obtain methanesulfonyl compound (414mg, colorless solid).

[1404] The obtained methanesulfonyl compound (102mg), piperidine (0.042mL), iPr 2 A mixture of NEt (0.073 mL) and MeCN (2.0 mL) was reacted by microwave (100°C, 1.5 hours). By reversed-phase column chromatography (mobile phase: 0.1% TFA MeCN / H 2 O=10 / 90~90 / 10; v / v) refined. Wash the fractions...

Embodiment A－02

[1408] ·Example A-02: 2-[2-(3-chlorophenyl)-4-{4-[2-(morpholin-4-yl)ethyl]phenyl}-1H-imidazol-1-yl ]-N-(propan-2-yl)acetamide

[1409] 【Chemical 227】

[1410]

[1411]

[1412]

[1413] .

Embodiment A－03

[1414] ·Example A-03: 2-[2-(3-Chlorophenyl)-4-{4-[2-(2-Oxa-6-azaspiro[3.3]heptane-6-yl)B Base]phenyl}-1H-imidazol-1-yl]-N-(propan-2-yl)acetamide

[1415] 【Chemical 228】

[1416]

[1417]

[1418] .

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PUM

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Abstract

The invention of the present application provides mood disorder, anxiety disorder, schizophrenia, Alzheimer's disease, Parkinson's disease, Huntington's disease, eating disorder, hypertension, digestive organ disease, drug dependence, epilepsy, cerebral infarction, Therapeutic or preventive agents for diseases such as cerebral ischemia, cerebral edema, head trauma, inflammation, immune-related diseases, and alopecia. Specifically, an azole derivative represented by the general formula (I) having an arginine vasopressin 1b receptor antagonistic activity, or a pharmaceutically acceptable salt thereof is provided. 【Chemical 1】

Description

technical field [0001] The present invention relates to an azole skeleton compound with antagonistic effect on the V1b receptor of arginine vasopressin (AVP) and a pharmaceutical composition using the compound as an active ingredient, in particular to emotional disorders (including depression), Anxiety disorder, schizophrenia, Alzheimer's disease, Parkinson's disease, Huntington's disease, eating disorder, hypertension, digestive organ disease, drug dependence, epilepsy, cerebral infarction, cerebral ischemia, cerebral edema, headache Therapeutic or preventive agents for external trauma, inflammation, immune-related diseases, alopecia and other diseases. Background technique [0002] Arginine vasopressin (AVP) is a peptide composed of 9 amino acids, which is mainly biosynthesized in the hypothalamus. As a pituitary hormone, it is closely related to the regulation of plasma osmotic pressure, blood pressure and body fluid volume. [0003] Three subtypes of AVP receptors, V1a,...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D207/444A61K31/4164A61K31/4178A61K31/4196A61K31/4439A61K31/444A61K31/454A61K31/4545A61K31/46A61K31/4725A61K31/496A61K31/537A61K31/5377A61K31/5386A61K31/541A61K31/553A61P1/04A61P9/10A61P9/12A61P17/14A61P25/00A61P25/08A61P25/14A61P25/16A61P25/18A61P25/22A61P25/28A61P25/30A61P29/00A61P37/02A61P43/00C07D231/12C07D233/64C07D233/70C07D249/08C07D249/10C07D263/32C07D277/20C07D277/30C07D401/04C07D401/10C07D403/04C07D403/06C07D403/10C07D413/10C07D451/06C07D491/107C07D498/08
CPCC07D207/444C07D231/12C07D233/64C07D233/70C07D233/90C07D249/08C07D249/12C07D263/32C07D277/30C07D401/04C07D401/10C07D403/04C07D403/06C07D403/10C07D413/10C07D451/06C07D491/107C07D498/08C07D249/10C07D277/20C07D471/08A61P1/00A61P1/04A61P17/00A61P17/14A61P25/00A61P25/08A61P25/14A61P25/16A61P25/18A61P25/22A61P25/24A61P25/28A61P25/30A61P29/00A61P37/02A61P43/00A61P9/00A61P9/10A61P9/12A61K31/4164A61K31/4178A61K31/4196A61K31/4439A61K31/444A61K31/454A61K31/4545A61K31/46A61K31/4725A61K31/496A61K31/537A61K31/5377A61K31/5386A61K31/541A61K31/553
Inventor 吉永光周桑田刚志宫腰直树石坂知子若杉大介城川伸一服部信隆岛崎洋一
Owner TAISHO PHARMACEUTICAL CO LTD
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