5 results about "Platelet Aggregation Inhibition" patented technology

The present application relates to a kind of cis 4-(5,6-diphenylpyrazin-2-aminyl) cyclohexyloxy acetic acid compound and its synthesis method and application, belong to the technical field of drug synthesis.The cis 4-(5,6-diphenylpyrazin-2-aminyl) cyclohexyloxy acetic acid compound has simple molecular structure, simple synthesis path and low production cost.Through in vitro platelet aggregation inhibition activity test, it is found that the synthesized compound shows excellent anti-platelet aggregation effect.In addition, in rat pharmacokinetic study, it is found that the compound shows excellent pharmacokinetic characteristics, has high bioavailability and longer half-life, can effectively improve its activity as antithrombotic drug, and shows excellent prevention and treatment effect in antithrombotic, vasodilator and anti-pulmonary arterial hypertension etc..

This invention relates to 2-phenylpyrimidine platelet aggregation inhibitors, their preparation methods, and their application in the preparation of drugs for treating thrombotic diseases, belonging to the field of pharmaceutical technology. The compounds of this invention, their pharmaceutically usable salts, tautomers, and pharmaceutically usable solvates have the structures shown in Formula I, wherein R1-R5 and A are as described in the claims and specification. The compounds of this invention, their pharmaceutically usable salts, tautomers, pharmaceutically usable solvates, and their pharmaceutical compositions have platelet aggregation inhibitory activity and can be used to prepare drugs for the prevention and treatment of thrombotic diseases.

The application discloses a kind of nitroso thiol compounds and synthesis method, purposes thereof, belong to medical field.The application provides a kind of compound shown in formula I or formula II or its pharmaceutically acceptable salt, hydrate, solvate, stereoisomer, tautomer, cis-trans isomer, isotopically labeled compound or prodrug, the compound of the present application is relative to existing product clopidogrel and prasugrel, (1) its platelet aggregation inhibition rate is high;(2) faster onset;(3) to the Asian race due to the loss of P450 enzyme, drug is more easily absorbed, and the efficacy is better;It can be used for treating, improving and preventing cardiovascular diseases, and has good application prospect and important clinical significance.

The present invention discloses a tacrine-pyrazine derivative and its use. The structure of the tacrine-pyrazine derivative is represented by the following general formula (I), general formula (II), and general formula (III): The tacrine-pyrazine derivative of the present invention uses the acetylcholinesterase inhibitor tacrine as a parent nucleus and is combined with a functional group of ligustrazine (tetramethylpyrazine) having an anti-platelet aggregation effect. Other tacrine-pyrazine derivatives have activities such as inhibiting acetylcholinesterase, resisting platelet aggregation, and inhibiting tau protein hyperphosphorylation, thereby being able to better protect neurons from damage and improve impaired learning and memory in rats. The tacrine-pyrazine derivative has high blood-brain barrier permeability and relatively low toxicity, and can be used for the prevention and treatment of vascular dementia.

Disclosed relates to novel Pyrimidine annulated derivatives of Formula (I) and the preparation methods of these compounds,and to their use as P2Y12 receptor antagonists in the treatment and / or prevention of thrombosis or related disorders.