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Triazolopyridazines as PAR1 inhibitors, production thereof, and use as medicaments

A technology of triazolo and pyridazine, applied in the field of preparing compounds of formula 1

Inactive Publication Date: 2013-08-14
SANOFI AVENTIS SA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This dual activity of thrombin against coagulation factor VIII results in a self-limiting protease complex formation and thus localized blood coagulation

Method used

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  • Triazolopyridazines as PAR1 inhibitors, production thereof, and use as medicaments
  • Triazolopyridazines as PAR1 inhibitors, production thereof, and use as medicaments
  • Triazolopyridazines as PAR1 inhibitors, production thereof, and use as medicaments

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Abstract

The invention relates to novel compounds of formula I where R1, R2, R3, R4, R5, R6, R7, R8, Q1, Q2 and Q3 are each as defined below. The compounds of formula I have antithrombotic activity and inhibit especially protease-activated receptor 1 (PAR1). The invention further relates to a process for preparing the compound of formula I and to the use thereof as a medicament.

Description

Technical field [0001] The invention involves a new type I compound: [0002] [0003] Among them, R1, R2, R3, R4, R5, R6, R7, R8, Q1, Q2 and Q3 are defined as follows.The type I compound has anticoagulant activity (Antithrombotic Activity), and especially inhibitory protease activation receptor 1 (PAR1).The present invention also involves the method of preparation of 1 compound and its use for drugs. Background technique [0004] Proteinase activation receptor 1 (PAR1) is a thrombin receptor that belongs to the G protein coupling body (GPCR).The gene of PAR1 is located on the chromosomal 5Q13, which is composed of two exogenous sons and covers a area of about 27KB. [0005] PAR1 is particularly expressed in endothelial cells, smooth muscle cells, fibroblasts, neurons and human platelets.As far as platelets are concerned, PAR1 is an important receptor of signal transmission, and it is caused by the aggregation of platelets. [0006] The activation of PAR is as follows: Remove t...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D487/04A61K31/5025A61P7/02
CPCC07D487/04A61K31/5025A61P11/00A61P17/00A61P17/02A61P19/02A61P25/00A61P27/02A61P29/00A61P3/00A61P35/00A61P35/04A61P7/00A61P7/02A61P9/00A61P9/06A61P9/10A61P3/10
Inventor 尤维·海内尔特沃尔克马·韦纳马赛厄斯·赫尔曼卡尔·舍纳芬格亨宁·斯坦哈根博多·谢珀
Owner SANOFI AVENTIS SA