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Homocysteine synthase inhibitor

A solvate and amide derivative technology, applied in the field of amide derivatives, can solve the problems of unreported SAHH inhibition, undisclosed, etc.

Inactive Publication Date: 2011-05-11
MITSUBISHI TANABE PHARMA CORP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] In addition, amide compounds are reported in Patent Documents 3 to 7, but the present invention is not disclosed in these reports, and SAHH inhibitory action is not reported (Patent Documents 3 to 7)

Method used

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Examples

Experimental program
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preparation example Construction

[0343] The production method of the compound of the present invention is explained below.

[0344]The compound represented by the general formula (I) or a salt thereof can be synthesized by various known synthesis methods by utilizing the characteristics based on its basic skeleton or type of substituent. Typical production methods are illustrated below, but are not limited to the methods described below. It should be noted that, depending on the type of functional group, sometimes at the stage of raw materials or intermediates, the functional group is first changed into an appropriate protecting group, that is, a group that is easily converted into the functional group is effective in preparation technology, and can be removed as needed. protecting group to give the desired compound. Examples of these functional groups include hydroxyl groups, carboxyl groups, and amino groups, and examples of these protective groups include those described in "Protective Groups in Organic S...

Embodiment

[0904] Hereinafter, although the Example of this invention demonstrates more concretely, the scope of this invention is not limited to the following Example.

[0905] "Room temperature" in the following reference examples and examples means 0 to 30°C. In addition, when a mixed solvent is used, the solvent ratio represents a volume ratio.

[0906] Mass spectra were measured by any of the following methods.

[0907]

[0908] Device: LC-2010

[0909] Column: Chromolith SpeedROD RP-18e (manufactured by Merck)

[0910] Mobile phase: A solution (0.05% trifluoroacetic acid / water), B solution (0.05% trifluoroacetic acid / acetonitrile), gradient elution from A solution: B solution = 95:5 to A solution: B solution = 0:100 4 minutes

[0911] Flow rate: 4.0ml / min

[0912] Column temperature: room temperature

[0913] MS measurement mode: ESI (Electrospray ionization) method Positive

[0914]

[0915] Device: Acquity UPLC / ZQ

[0916] Column: Acquity BEH C18 (manufactured by ...

reference example 1

[0930] (2-Aminoethyl)methylcarbamate tert-butyl hydrochloride

[0931] According to the method described in Synthetic Communications, 23(17), 2443-2449(1993), tert-butyl (2-aminoethyl)methylcarbamate was obtained from 10 g of N-methylaminoethanol. Use 4 equivalents of hydrochloric acid-di The hydrochloride salt was obtained from an alkane solution to obtain 9 g of the title compound as a colorless solid.

[0932] 1 H-NMR (300MHz, DMSO-d 6 ); δ(ppm) 1.41(s, 9H), 2.81(s, 3H), 2.89(q, J=6.1, 2H), 3.39(t, J=6.5, 2H), 8.05(brs, 3H).

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PUM

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Abstract

Disclosed is a homocysteine synthase inhibitor which is useful for the prevention or treatment of a disease associated with homocysteine synthase. Specifically disclosed is a compound represented by general formula (I) [wherein each symbol is as defined in the description], a pharmacologically acceptable salt of the compound, or a solvate of the compound or the pharmacologically acceptable salt, which can be used as the homocysteine synthase inhibitor.

Description

technical field [0001] The present invention relates to novel amide derivatives. More specifically, it relates to a homocysteine ​​synthase inhibitor comprising an amide derivative, a pharmacologically acceptable salt thereof, or a solvate thereof as an active ingredient. Background technique [0002] Homocysteine ​​is a sulfur-containing amino acid and an important intermediate in the metabolism of the essential amino acid methionine. Homocysteine ​​is maintained at an extremely low concentration in cells, and excess homocysteine ​​is released outside the cells, that is, into the blood. Dr. McCully reported 30 years ago that this homocysteine ​​is the cause of vascular diseases such as arteriosclerosis and myocardial infarction (Non-Patent Document 1). Afterwards, according to clinical tests, it was proved that patients with arteriosclerosis in peripheral blood vessels and cerebral blood vessels had high homocysteine ​​levels. (Non-Patent Document 2). Furthermore, in mo...

Claims

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Application Information

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IPC IPC(8): C07C237/10A61K31/277A61K31/404A61K31/4155A61K31/4196A61K31/422A61K31/423A61K31/4245A61K31/427A61K31/433A61K31/4439A61K31/454A61K31/4709A61K31/506A61K31/5375A61P9/00A61P9/10A61P25/28A61P43/00C07C255/58C07D209/44C07D271/06C07D295/22C07D401/12C07D403/12C07D405/12C07D409/12C07D413/12C07D417/12
CPCC07C237/10C07C255/60C07D209/44C07D271/06C07D295/22C07D401/12C07D403/12C07D405/12C07D409/12C07D413/12C07D417/12C07C2602/08A61P25/28A61P43/00A61P9/00A61P9/10
Inventor 中尾朗铃木裕子辰己亮关真纪田中实说田智文岩崎博司
Owner MITSUBISHI TANABE PHARMA CORP
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