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Beta-amino tetrahydropyrazine, tetrahydropyrimidine and tetrahydropyridine used as dipeptidy peptidase inhibitors for curing or preventing diabetes

An alkyl and phenyl technology, applied in the direction of urinary system diseases, diseases, metabolic diseases, etc., can solve problems that have not yet been studied, and there is no extensive research on DP-IV inhibitors

Active Publication Date: 2010-12-01
CGENETECH (SUZHOU CHINA) CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

To date, DP-IV inhibitors have not been studied extensively, especially for uses other than diabetes

Method used

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  • Beta-amino tetrahydropyrazine, tetrahydropyrimidine and tetrahydropyridine used as dipeptidy peptidase inhibitors for curing or preventing diabetes
  • Beta-amino tetrahydropyrazine, tetrahydropyrimidine and tetrahydropyridine used as dipeptidy peptidase inhibitors for curing or preventing diabetes
  • Beta-amino tetrahydropyrazine, tetrahydropyrimidine and tetrahydropyridine used as dipeptidy peptidase inhibitors for curing or preventing diabetes

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0257]

[0258] (R)-3-Amino-4-(2,5-difluorophenyl)-1-(5,6-dihydroimidazo[1,5-a]pyrazin-7(8H)-yl)butyl Alkan-1-one dihydrochloride

[0259] Step A. (R)-1-(2,5-difluorophenyl)-4-(5,6-dihydroimidazo[1,5-a]pyrazin-7(8H)-yl)-4 -Oxobutan-2-ylcarbamate tert-butyl ester

[0260] At 0°C, 5,6,7,8-tetrahydroimidazo[1,5-a]pyrazine (50.0mg, 0.40mmol) and Boc-(R)-3-amino-4-(2, To a solution of 5-difluorophenyl)butanoic acid (128.0 mg, 0.40 mmol) in dichloromethane (5 mL) was added HOBT (54.5 mg, 0.42 mmol). The reaction was stirred at 0 °C for 10 min, then EDC (96.6 mg, 0.50 mmol) was added. After removing the ice bath, the reaction was stirred at ambient temperature for 14 h. The mixture was concentrated and purified by HPLC (Gilson; YMC-Pack Pro C18 column, 100x20mm I.D.; solvent gradient from 10% acetonitrile, 90% water, and 0.1% trifluoroacetic acid to 90% acetonitrile, 10% water, and 0.1% trifluoroacetic acid) , to obtain 103 mg of the title compound as a foamy solid.

[0261]...

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PUM

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Abstract

The invention relates to beta-amino tetrahydropyrazine, tetrahydropyrimidine and tetrahydropyridine used as dipeptidy peptidase inhibitors for curing or preventing diabetes. Each variable quantity is defined as the application specification. The compounds are the inhibitors of dipeptidy peptidase-IV enzyme ('DP-IV inhibitors') and can be used for curing or preventing diseases relevant to the dipeptidy peptidase-IV enzyme, such as the diabetes, particularly the II-type diabete. The invention also relates to a medicinal composition comprising the compounds and application of the compounds and the composition in preventing or curing the diseases relevant to the dipeptidy peptidase-IV enzyme.

Description

technical field [0001] The present invention relates to compounds which are inhibitors of dipeptidyl peptidase-IV enzymes ("DP-IV inhibitors") and which are useful in the treatment or prophylaxis of diseases associated with dipeptidyl peptidase-IV enzymes such as diabetes, in particular It is type II diabetes. The present invention also relates to pharmaceutical compositions containing these compounds and the use of these compounds and compositions in the prevention or treatment of these dipeptidyl peptidase-IV enzyme-related diseases. Background technique [0002] Diabetes mellitus is a multifactorial disease process characterized by elevated plasma glucose levels or hyperglycemia following administration of glucose in the fasted state or during an oral glucose tolerance test. [0003] Persistent or uncontrolled hyperglycemia is associated with premature morbidity and increased mortality. Frequently abnormal glucose homeostasis is directly and indirectly associated with a...

Claims

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Application Information

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IPC IPC(8): C07D487/04C07D471/04A61K31/4985A61K31/519A61K31/437A61P43/00A61P3/10A61P3/04A61P5/50A61P3/06A61P9/10A61P5/00A61P37/02A61P31/18A61P25/00A61P35/04A61P13/08A61P1/02A61P9/12A61P19/10A61P15/00A61P1/00
Inventor 余强韦凤萍
Owner CGENETECH (SUZHOU CHINA) CO LTD
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