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Cyclic amine derivative and pharmaceutical use thereof

A technology of cyclic amines and derivatives, which is applied in the field of cyclic amine derivatives and their pharmaceutical applications, can solve the problems of low therapeutic effects of non-steroidal anti-inflammatory drugs and opioid compounds, and achieve the effect of reducing side effects

Active Publication Date: 2016-05-04
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 low (Non-Patent Document 1)

Method used

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  • Cyclic amine derivative and pharmaceutical use thereof
  • Cyclic amine derivative and pharmaceutical use thereof
  • Cyclic amine derivative and pharmaceutical use thereof

Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0439] Preparations of the above-mentioned dosage forms can be carried out according to known production methods generally used in the field of pharmaceuticals. At this time, if necessary, it can be produced containing excipients, binders, lubricants, disintegrants, sweeteners, surfactants, suspending agents, emulsifying agents, etc. generally used in the field of pharmaceutical preparations.

[0440] Tablets can be prepared, for example, with excipients, binders, disintegrants or lubricants, and pills and granules can be prepared, for example, with excipients, binders or disintegrators. In addition, powders and capsules can be prepared with excipients, syrups can be prepared with sweeteners, emulsions or suspensions can be prepared with surfactants, suspending agents or emulsifiers.

[0441] Examples of excipients include lactose, glucose, starch, sucrose, microcrystalline cellulose, licorice powder, mannitol, sodium bicarbonate, calcium phosphate or calcium sulfate.

[0442...

Embodiment

[0453] Hereinafter, although this invention is demonstrated in detail using an Example and a reference example, this invention is not limited to them.

[0454] In the following description, the solvent names shown in the NMR data represent the solvents used in the measurement. In addition, the 400 MHz NMR spectrum was measured using the JNM-AL400 nuclear magnetic resonance apparatus (JEOL Ltd.). The chemical shift is based on tetramethylsilane, expressed in δ (unit: ppm), and the signals are represented by s (single spectrum), d (double spectrum), t (triple spectrum), q (quadruple spectrum) line), quint (quintet), sept (septet), m (multiplet), br (broad), dd (double doublet), dt (double triplet), ddd (double doublet doublet), dq (double quartet), td (triple doublet), tt (triple triplet) said. The ESI-MS spectrum was measured using Agilent Technologies 1200 Series and G6130A (manufactured by Agilent Technologies). As the solvent, all commercially available solvents were used...

reference example 1）

[0456] (Reference Example 1) Synthesis of benzyl 4-((2-((tert-butoxycarbonyl)amino)ethyl)(methyl)amino)piperidine-1-carboxylate:

[0457] [chem 22]

[0458]

[0459]To a solution of benzyl 4-oxopiperidine-1-carboxylate (0.500 g, 2.14 mmol) in dichloromethane (3.0 mL) was added tert-butyl (2-(methylamino)ethyl) at 0°C Carbamate hydrochloride (0.564 g, 2.68 mmol) and sodium triacetoxyborohydride (0.681 g, 3.22 mmol) were stirred at room temperature for 16 hours. The reaction solution was cooled to 0 °C. Saturated aqueous sodium bicarbonate solution was added to the reaction liquid, followed by extraction with chloroform. The organic layer was dried over anhydrous sodium sulfate, filtered, and the filtrate was concentrated under reduced pressure. The residue was purified by flash chromatography (silica gel, hexane / ethyl acetate) to afford 4-((2-((tert-butoxycarbonyl)amino)ethyl)(methyl)amino)piperene as a white solid Benzyl pyridine-1-carboxylate (0.590 g, 1.51 mmol, 70%)....

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Abstract

The purpose of the present invention is to provide a compound that exerts a strong analgesic action against on pain, in particular, against neuropathic pain and / or fibromyalgia syndrome. The present invention provides a cyclic amine derivative represented by chemical formula (AA), a prodrug thereof or a pharmaceutically acceptable salt thereof.

Description

technical field [0001] The present invention relates to cyclic amine derivatives and their medicinal use. Background technique [0002] Pain refers to an experience accompanied by unpleasant sensations and unpleasant emotions that occurs when tissue damage is caused or is possible. Pain is mainly classified into nociceptive pain, neuropathic pain or psychogenic pain according to its cause. In addition, fibromyalgia is known as pain of unknown origin. [0003] Neuropathic pain refers to pathological pain caused by abnormal function of the peripheral or central nervous system. Even if the nociceptors do not receive no noxious stimulation, the pain is caused by direct injury or compression of the nerve tissue. As a therapeutic drug for neuropathic pain, anticonvulsants, antidepressants, anxiolytics, or antiepileptic drugs such as gabapentin or pregabalin can be used. [0004] Fibromyalgia refers to a disease in which general pain is the main symptom, and psychoneurologic...

Claims

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Application Information

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IPC IPC(8): C07D401/06A61K31/454A61P25/04C07D401/14C07D403/06C07D413/14
CPCC07D403/06A61P29/00C07D401/06A61K31/34A61K31/357A61K31/4025A61K31/4178A61K31/454A61K31/4545A61K31/496A61K31/5377C07D401/14C07D403/14C07D405/14C07D413/14
Inventor 盛田康弘泉本直树伊关克彦岩野俊介宇田川秀二三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
Owner TORAY IND INC
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