Fused azole derivative

A technology of condensed ring azoles and derivatives, applied in the field of condensed ring azole derivatives, can solve problems such as unreported compounds

Inactive Publication Date: 2014-12-03
TAISHO PHARMACEUTICAL CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, there is no report on the compounds with fused

Method used

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Examples

Experimental program
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Embodiment

[0313] Hereinafter, the present invention will be described in more detail with reference examples, examples, and test examples, but the present invention is not limited thereto, and changes can be made without departing from the scope of the present invention.

[0314] In Reference Examples and Examples, "Phase Separator" in the following treatments refers to Biotage's ISOLUTE (registered trademark) Phase Separator. For "SNAP Cartridge KP-NH" purified by column chromatography, use Biotage's SNAP Cartridge KP-NH; for "SNAP Cartridge KP-Sil", use Biotage's SNAP Cartridge KP-Sil; for "SNAP Cartridge HP For "-Sil", SNAP Cartridge HP-Sil from Biotage Co., Ltd. was used; for "Chromatorex NH", Cromatrex (registered trademark) NH manufactured by Fuji Silysia Chemical Co., Ltd. was used; TLC Platinum NH (manufactured by Fuji Silysia Corporation) was used for thin-layer chromatography (TLC); In addition, Silikagel 60 and Siricagel 60N refer to the use of silica gel sold by Kanto Chemic...

reference example P-A1

[0339] · Reference Example P-A1: Synthesis of 2-nitro-4-[3-(piperidin-1-yl)propoxy]aniline

[0340] [chem 36]

[0341]

[0342] 4-Amino-3-nitrophenol (2.15g) was dissolved in THF (40mL), and 1-piperidine propanol (2.00g), triphenylphosphine (5.49g), DEAD (2.2mol / L toluene solution, 9.52 mL), stirred at room temperature for 16 hours. The residue obtained by concentrating the reaction solution under reduced pressure was purified by silica gel column chromatography (Cromatrex NH, mobile phase: n-hexane / EtOAc=80 / 20-65 / 35; v / v) to obtain the title compound (3.41 g, reddish-brown oil). the

[0343] .

[0344] · Reference example P-A2: Synthesis of 3-chloro-N-{2-nitro-4-[3-(piperidin-1-yl)propoxy]phenyl}benzamide

[0345] [chem 37]

[0346]

[0347] CHCl of the compound (3.40 g), pyridine (4.92 mL) obtained in Reference Example P-A1 3 (40 mL) was added 3-chlorobenzoyl chloride (1.87 mL) and stirred at room temperature for 1.5 hours. The reaction solution was washed su...

reference example P-A15

[0412] · Reference example P-A15: 2-[5-bromo-2-(4-fluoro-3-methoxyphenyl)-1H-benzimidazol-1-yl]-N-isopropylacetamide and 2 Synthesis of a mixture of -[6-bromo-2-(4-fluoro-3-methoxyphenyl)-1H-benzimidazol-1-yl]-N-isopropylacetamide

[0413] [chemical 50]

[0414]

[0415] The title compound (0.33 g, colorless solid) was obtained from the compound (0.45 g) obtained in Reference Example P-A14 by the same method as in Reference Example P-A10. the

[0416] .

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Abstract

Provided is a therapeutic or prophylactic agent for mood disorders, anxiety, schizophrenia, Alzheimer's disease, Parkinson's disease, Huntington's chorea, eating disorders, hypertension, digestive diseases, drug dependence, epilepsy, cerebral infarction, cerebral ischemia, cerebral edema, head injury, inflammation, immune related diseases, depilation, and so on. More specifically, provided is a fused azole derivative represented by general formula (I), which has arginine vasopressin 1b receptor antagonism, or a pharmaceutically acceptable salt thereof.

Description

technical field [0001] The present invention relates to arginine-vasopressin (AVP) V1b receptor antagonistic compound of fused ring azole skeleton and the pharmaceutical composition using the compound as an active ingredient, especially related to affective disorders (including depression) disease), anxiety disorder, schizophrenia, Alzheimer's disease, Parkinson's disease, Huntington's disease, eating disorder, high blood pressure, digestive organ disease, drug dependence, epilepsy, cerebral infarction, cerebral ischemia A therapeutic or preventive agent for diseases such as cerebral edema, head trauma, inflammation, immune-related diseases, and alopecia. 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] So far, three subtypes of AVP recept...

Claims

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Application Information

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IPC IPC(8): C07D209/10A61K31/405A61K31/4184A61K31/438A61K31/454A61K31/4545A61K31/5377A61K31/5386A61K31/55A61P1/14A61P7/10A61P9/10A61P9/12A61P17/14A61P25/00A61P25/08A61P25/14A61P25/16A61P25/18A61P25/22A61P25/28A61P29/00A61P37/00A61P43/00C07D231/56C07D235/18C07D401/04C07D401/12C07D403/12C07D471/04C07D491/08C07D491/107
CPCC07D209/10C07D491/08C07D471/04C07D235/18C07D403/12C07D231/56C07D401/12C07D401/04C07D491/107A61P1/14A61P17/14A61P25/00A61P25/08A61P25/14A61P25/16A61P25/18A61P25/22A61P25/28A61P29/00A61P37/00A61P43/00A61P7/10A61P9/10A61P9/12
Inventor 吉永光周石坂知子若杉大介城川伸一服部信隆柏修平桒田刚志岛崎洋一
Owner TAISHO PHARMACEUTICAL CO LTD
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