Amino hexatomic ring derivative and application thereof to medicine

An alkyl and pharmaceutical technology, applied in the field of amino six-membered ring derivatives and its application in medicine, can solve problems such as the burden of diabetes

Active Publication Date: 2016-02-03
SICHUAN HAISCO PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Diabetes treatment places a heavy burden on families and society

Method used

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  • Amino hexatomic ring derivative and application thereof to medicine
  • Amino hexatomic ring derivative and application thereof to medicine
  • Amino hexatomic ring derivative and application thereof to medicine

Examples

Experimental program
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Effect test

Embodiment 1

[0267] (2R,3R,4R,5S)-2-(2,5-difluorophenyl)-4-fluoro-5-(2-(methylsulfonyl)pyrrolo[3,4-c]pyrazole- 5(2H,4H,6H)-yl)tetrahydro-2H-pyran-3-amine (compound 1)

[0268] (2R,3R,4R,5S)-2-(2,5-difluorophenyl)-4-fluoro-5-(2-(methylsulfonyl)pyrrolo[3,4-c]pyrazol-5(2H,4H,6H) -yl)tetrahydro-2H-pyran-3-amine

[0269]

[0270] The first step: tert-butyl ((2R,3R,4R)-2-(2,5-difluorophenyl)-4-fluoro-5-carbonyltetrahydro-2H-pyran-3-yl)aminomethyl Ester (1b)

[0271] tert-butyl((2R,3R,4R)-2-(2,5-difluorophenyl)-4-fluoro-5-oxotetrahydro-2H-pyran-3-yl)carbamate

[0272] Under nitrogen protection, intermediate 1 (1.5g, 4.58mmol), trans-4-hydroxy-D-proline hydrochloride (77mg, 0.46mmol) and anhydrous sodium carbonate (728mg, 6.78mmol) were added to tetrahydrofuran (20 mL), stirred at room temperature for 10 minutes, added N-fluorobisbenzenesulfonamide (1.44 g, 4.58 mmol) at this temperature, and continued the reaction for 48 hours. Ethyl acetate (40mL) was added to the reaction solution, stir...

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PUM

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Abstract

The invention relates to an amino hexatomic ring derivative and application thereof to medicine, in particular to the amino hexatomic ring derivative shown in the general formula (I) (in the description), a stereoisomer thereof, a pharmaceutically acceptable salt thereof or a prodrug thereof, a drug composition comprising the derivative, and medical application to preparation of a dipeptidyl peptidase IV (DPP-IV) inhibitor. In the general formula (I), the definitions of the substituent groups are the same as those in the description.

Description

technical field [0001] The present invention relates to an amino six-membered ring derivative and its application in medicine, in particular to an amino six-membered ring derivative represented by general formula (I) or its pharmaceutically acceptable salt or its stereoisomer , and a pharmaceutical composition containing the derivative or its pharmaceutically acceptable salt or its stereoisomer, and its use as a therapeutic agent, especially as a dipeptidyl peptidase IV (DPP-IV) inhibitor. Background technique [0002] Diabetes is a major medical problem worldwide. According to the statistics of the International Diabetes Federation (IDF), the number of diabetic patients in the world reached 382 million in 2013, and the global medical expenditure reached 548 billion US dollars, accounting for 11% of the global medical expenditure. Global healthcare costs related to diabetes are projected to reach $627.3 billion by 2035. Insulin is a hormone needed to convert sucrose, starch...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D487/04A61K31/4162A61P3/10A61P27/02A61P25/00A61P13/12A61P5/50A61P3/06A61P3/04A61P3/00A61P9/10A61P9/12
CPCC07D487/04
Inventor 张晨范江雷鸣魏用刚
Owner SICHUAN HAISCO PHARMA CO LTD
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