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A technology of azole derivatives and alkyl groups, applied in the field of azole derivatives, can solve the problems such as no reports of compounds with azole skeletons
Active Publication Date: 2014-06-25
TAISHO PHARMACEUTICAL CO LTD
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However, there is no report on the compounds with azole skeletons disclosed in the present invention
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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). Reversed-phase column chromatography (mobile phase: 0.1% TFA MeCN / H 2 O=10 / 90~90 / 10; v / v) refined. Wash the fractions wi...
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Abstract
The present invention provides agents for treating or preventing diseases such as mood disorder, anxiety disorder, schizophrenia, Alzheimer's disease, Parkinson's disease, Huntington's chorea, eating disorder, hypertension, gastrointestinal disease, drug addiction, epilepsy, cerebral infarction, cerebral ischemia, cerebral edema, head injury, inflammation, immune-related disease, alopecia, and so forth. Specifically, the invention provides azole derivatives represented by general formula (I), or pharmaceutically acceptable salts thereof that have an antagonistic action against the arginine-vasopressin (AVP) V1b receptor:
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,...
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