Cyclic amine derivative and use thereof for medical purposes

A technology for cyclic amines and derivatives, applied in the field of cyclic amine derivatives and their medicinal uses, can solve the problems of low therapeutic effect of non-steroidal anti-inflammatory drugs, and achieve the effect of strong analgesic effect

Active Publication Date: 2017-09-26
TORAY IND INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the therapeutic effects of NSAIDs and opioids are generally considered to be low (Non-Patent Document 1)

Method used

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  • Cyclic amine derivative and use thereof for medical purposes
  • Cyclic amine derivative and use thereof for medical purposes
  • Cyclic amine derivative and use thereof for medical purposes

Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0186] Preparations of the above-mentioned dosage forms can be carried out in accordance with known production methods commonly used in the field of pharmaceutical preparations. At this time, if necessary, it can be produced containing excipients, binders, lubricants, disintegrants, sweeteners, surfactants, suspending agents, emulsifying agents, etc., which are conventionally used in the field of pharmaceutical preparations.

[0187] Tablets can be prepared, for example, by containing excipients, binders, disintegrants or lubricants. The preparation of pellets and granules can be carried out, for example, with excipients, binders or disintegrants. In addition, powders and capsules can be prepared, for example, with excipients. The preparation of a syrup can contain a sweetener, for example. The preparation of an emulsion or a suspension can be carried out by containing, for example, a surfactant, a suspending agent, or an emulsifying agent.

[0188] Examples of excipients i...

Embodiment

[0200] Hereinafter, although an Example and a reference example demonstrate this invention in detail, this invention is not limited to these.

[0201] In the following description, the solvent names shown in the NMR data indicate the solvents used for the measurement. In addition, the 400 MHz NMR spectrum was measured using the JNM-AL400 nuclear magnetic resonance apparatus (made by JEOL Ltd.). The chemical shift is based on tetramethylsilane, expressed in δ (unit: ppm), and the signals are represented by s (single line), d (double line), t (triple line), q (quadruple line), quint ( Quintuplet), sept (sevenfold), m (multiplet), br (broad peak), dd (double doublet), dt (double triplet), ddd (double doublet doublet) , dq (double quartet), td (triple double line), tt (triple triple line) represent. The ESI-MS spectrum was measured using Agilent Technologies 1200 Series, G6130A (manufactured by Agilent Technology). All solvents used commercially available solvents. For flash c...

reference example 1

[0203] (Reference Example 1) Synthesis of 3-(1H-imidazol-2-yl)acrylic acid (E)-benzyl ester:

[0204] [chemical formula 9]

[0205]

[0206] To a suspension of sodium hydride (55%, 1.12g, 25.6mmol) in tetrahydrofuran (40.0mL), add benzyl dimethylphosphorylacetate (5.12mL, 24.4mmol) at 0°C, and the reaction solution was placed in the same Stir at temperature for 1 hour. To the reaction liquid, 1H-imidazole-2-carbaldehyde (2.46 g, 25.6 mmol) was added at 0° C., and the reaction liquid was stirred at room temperature for 60 hours. To the reaction liquid, saturated aqueous ammonium chloride solution was added, followed by extraction with ethyl acetate. The organic layer was washed with 10% aqueous sodium chloride solution, dried over anhydrous sodium sulfate, filtered, and the filtrate was concentrated under reduced pressure. The residue was purified by flash column chromatography (silica gel, chloroform / methanol) to give (E)-benzyl 3-(1H-imidazol-2-yl)acrylate (0.380 g, 1.6...

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Abstract

The purpose of the present invention is to provide a compound having a potent analgesic effect on pain, particularly neuropathic pain and / or fibromyalgia. The present invention provides a cyclic amine derivative typified by chemical formula (1) or a pharmacologically acceptable salt thereof.

Description

technical field [0001] The present invention relates to cyclic amine derivatives and their medical use. Background technique [0002] Pain refers to the experience accompanied by unpleasant sensations and unpleasant emotions when tissue damage is caused or there is a possibility of it. Pain is mainly classified according to its cause as nociceptive pain, neuropathic pain or psychogenic pain. In addition, fibromyalgia is known as pain of unknown origin. [0003] Neuropathic pain is pathological pain caused by abnormal function of the peripheral or central nervous system itself, and refers to pain caused by direct injury and compression of nerve tissue even if nociceptors are not stimulated by nociception. As a therapeutic agent for neuropathic pain, an anticonvulsant, an antidepressant, an anxiolytic, or an antiepileptic (gabapentin, pregabalin, etc.) can be used. [0004] Fibromyalgia refers to a disease with generalized pain as the main symptom and neuropsychiatric sympt...

Claims

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Application Information

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IPC IPC(8): C07D401/06A61K31/4178A61K31/5377A61P25/04A61P29/02C07D403/06
CPCA61K31/5377C07D401/06C07D403/06A61K31/4178A61P25/04A61P29/02A61K31/4025C07D413/14
Inventor 宇田川秀二盛田康弘泉本直树伊关克彦岩野俊介三好智也长田祐二是枝彻郎村上正德白木元明高桥圭大信田系裕东惠理子
Owner TORAY IND INC
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