Tetrahydroisoquinolinyl-3-carboxylic acid modified LARGD heptapeptides, and synthesis, antithrombotic activity and application thereof

A tetrahydroisoquinoline and antithrombotic technology, applied in the field of biomedicine, can solve problems such as unsatisfactory clinical efficacy
CN103450344AInactive Publication Date: 2013-12-18CAPITAL UNIVERSITY OF MEDICAL SCIENCES
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
CAPITAL UNIVERSITY OF MEDICAL SCIENCES
Publication Date
2013-12-18
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention provides 3 novel antithrombotic quasi-peptides disclosed as general formula I, a molecular simulation method of the 3 novel antithrombotic quasi-peptides, a preparation method of the 3 novel antithrombotic quasi-peptides, inhibiting action of the 3 novel antithrombotic quasi-peptides on expression of glycoprotein IIb / IIIa and P-lectin, anti-thrombocyte aggregation action of the 3 novel antithrombotic quasi-peptides, and antithrombotic action of the 3 novel antithrombotic quasi-peptides on a rat thrombosis model. Therefore, the invention provides clinical application prospects of the 3 novel antithrombotic quasi-peptides disclosed as general formula I as an antithrombotic agent. In the general formula I, AA represents Ser or Val or Phe residue.
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Description

technical field

[0001] The present invention relates to three novel antithrombotic peptidomimetics, to their molecular imitation methods, to their preparation methods, to their inhibitory effects on the expression of glycoprotein IIb / IIIa and P-selectin, to their anti-platelet aggregation effects, It is further related to their antithrombotic effect on the rat model of thrombosis. Therefore, the present invention relates to the clinical application prospects of three novel antithrombotic peptidomimetics as antithrombotic agents. The invention belongs to the field of biomedicine. Background technique

[0002] Globally, thrombotic disease is the leading cause of morbidity and mortality. There are two types of thrombi in patients with thrombosis, one is a thrombus formed by cross-linking platelets with white blood cells through fibrinogen, and the other is a thrombus formed by cross-linking platelets through fibrinogen and platelets.

[0003] P-selectin exists in two forms: ...

Claims

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