Tetrahydro thienopyridine derivative for treating

A compound and hydrate technology, applied in the field of tetrahydrothienopyridine derivatives, can solve problems such as plaque rupture

Inactive Publication Date: 2011-04-06
HC SYNTHETIC PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although the processes that cause vascular disease are complex and not fully understood, the basic etiology shared by many theories involves plaque rupture due to arteriosclerosis and leading to thrombosis or thromboembolism

Method used

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  • Tetrahydro thienopyridine derivative for treating
  • Tetrahydro thienopyridine derivative for treating

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] Embodiment 1: the preparation of compound A

[0022] Reaction equation:

[0023]

[0024] 2-[2-(hydroxyl)-6,7-dihydrothieno[3,2-c]pyridin-5(4H)-yl]-1-cyclopropyl-2-(2-fluorophenyl) 37.3 g (0.1 mol) of ethyl ketone was dissolved in 2000 ml of ethyl acetate, 26.3 g (0.1 mol) of triphenylphosphine and 17.52 g (0.1 mol) of BOC-glycine were added, and diethyl azodicarboxylate was added dropwise under stirring (DEAD) 17.42g (0.1mol) was reacted at room temperature for 5h, filtered, dry HCl gas was passed into the filtrate to saturation, stirred at room temperature for 5h, a large amount of white solid was precipitated, filtered, the filter cake was washed with a small amount of ethyl acetate, and dried to obtain the compound A hydrochloride 13.8g.

[0025] After dissolving 10 g of compound hydrochloride with 100 ml of pure water, slowly add saturated sodium carbonate solution dropwise until the pH is 10 to 10.5, extract three times with 500 ml each time of ethyl acetate,...

Embodiment 2

[0026] Example 2: Preparation of R, S-type isomers of compound A.

[0027] Prepared according to the method of Example 1 except that R-type 2-[2-(hydroxyl)-6,7-dihydrothieno[3,2-c]pyridin-5(4H)-yl]-1-ring Propyl-2-(2-fluorophenyl)ethanone or S-type 2-[2-(hydroxyl)-6,7-dihydrothieno[3,2-c]pyridin-5(4H)-yl] -1-cyclopropyl-2-(2-fluorophenyl)ethanone instead of 2-[2-(hydroxyl)-6,7-dihydrothieno[3,2-c]pyridine-5(4H)- Base]-1-cyclopropyl-2-(2-fluorophenyl)ethanone.

Embodiment 3

[0028] Example 3: Preparation of Compound B.

[0029] 2-[2-(hydroxyl)-6,7-dihydrothieno[3,2-c]pyridin-5(4H)-yl]-1-cyclopropyl-2-(2-fluorophenyl) 37.3 g (0.1 mol) of ethyl ketone was dissolved in 2000 ml of ethyl acetate, 26.3 g (0.1 mol) of triphenylphosphine and 18.92 g (0.1 mol) of BOC-alanine were added, and diethyl azodicarboxylate was added dropwise under stirring. Ethyl ester (DEAD) 17.42g (0.1mol) was reacted at room temperature for 5h, filtered, dry HCl gas was passed through the filtrate to saturation, stirred at room temperature for 5h, a large amount of white solid was precipitated, filtered, the filter cake was washed with a small amount of ethyl acetate, dried 17.3 g of compound B hydrochloride was obtained.

[0030] After dissolving 10 g of compound B hydrochloride with 80 ml of pure water, slowly add saturated sodium carbonate solution dropwise until the pH is 10 to 11, extract three times with 500 ml of ethyl acetate, combine the extracts, and add anhydrous so...

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PUM

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Abstract

The invention provides a novel tetrahydro thienopyridine derivative. The dosage of one or more active compounds in the novel tetrahydro thienopyridine derivative is 0.1-20mg/kg body weight, and the preferable dosage is 0.1-5mg/kg body weight. The novel tetrahydro thienopyridine derivative can be used for producing medicines for preventing and/or treating diseases induced by thrombosis or thromboembolism.

Description

Technical field: [0001] The invention relates to tetrahydrothienopyridine derivatives for use in therapy (in particular for the prophylaxis and or treatment of thrombosis-induced and / or thromboembolism-induced diseases in humans), methods of their use, formulations containing them and their production method. technical background: [0002] Vascular disease, including myocardial infarction and ischemic stroke, is a leading cause of death and disability. Although the processes leading to vascular disease are complex and not fully understood, the basic etiology shared by many theories involves plaque rupture due to arteriosclerosis and leading to thrombosis or thromboembolism. US Patent No. 5288726 discloses that a class of tetrahydrothienopyridine derivatives can be used for the treatment of this disease, and the present invention provides a new class of tetrahydrothienopyridine derivatives. Invention content: [0003] The object of the present invention is to provide a ne...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D495/04C07F9/6561A61K31/4365A61K31/675A61P7/02A61P9/10A61P9/04A61P9/06
Inventor 杨成强建华
Owner HC SYNTHETIC PHARMA CO LTD
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