Macrocyclic urea and sulfamide derivatives as inhibitors of TAFIA

A technology of heterocycles and compounds, applied in the field of preparation
CN102056922AInactive Publication Date: 2011-05-11SANOFI AVENTIS SA
3 Cites 6 Cited by

Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
SANOFI AVENTIS SA
Publication Date
2011-05-11
Estimated Expiration
Not applicable · inactive patent

Smart Images

  • Figure 1
    Figure 1
  • Figure 2
    Figure 2
  • Figure 3
    Figure 3
Patent Text Reader

Abstract

The invention relates to compounds of the formula (I) which are inhibitors of activated thrombin-activable fibrinolysis inhibitor. The compounds of the formula I are suitable for producing medicaments for prophylaxis, secondary prevention and treatment of one or more disorders associated with thromboses, embolisms, hypercoagulability or fibrotic changes.
Need to check novelty before this filing date? Find Prior Art

Description

technical field

[0001] The present invention relates to novel compounds of formula I which inhibit the enzyme TAFIa (activated thrombin-activatable fibrinolysis inhibitor), their preparation and their use as medicaments. Background technique

[0002] The enzyme TAFIa is generated from the thrombin-activatable fibrinolysis inhibitor zymogen (TAFI) by, for example, thrombin activation. The enzyme TAFI, also known as plasma procarboxypeptidase B, procarboxypeptidase U or procarboxypeptidase R, is a proenzyme similar to carboxypeptidase B (L. Bajzar, Arterioscler. Thromb. Vasc. Biol. 2000, pp. 2511-2518).

[0003] During clot formation, thrombin is produced as the end product of the coagulation cascade, which induces the conversion of soluble plasma fibrinogen into an insoluble fibrin matrix. At the same time, thrombin can activate the endogenous fibrinolysis inhibitor TAFI. Thus, during thrombus formation and lysis, activated TAFI (TAFIa) is generated from the zymogen TAFI b...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More