1312440-98-4

Upstream product

• 1147350-75-1 2-Oxoclopidogrel 
• 5538-51-2 O-acetylsalicyloyl chloride 
• 32345-59-8 methyl (R)-2-chloromandelate 
• 10421-85-9 (R)-2-chloromandelic acid 
• 527687-26-9 S(+)-2-(2-chlorophenyl)-2-(4,5,6,7-tetrahydro-thieno[3,2-c]pyridine-2(4H)-one)-5-acetic acid methyl ester 
• 141-78-6 ethyl acetate 
• 1441-87-8 salicyloyl chloride 
• 1312441-08-9 (RS)-2-(2-chlorophenyl)-2-(4,5,6,7-tetrahydro-thieno[3,2-c]pyridine-2 (4H)-one)-5-acetate 

Downstream Products

• 1402715-88-1 C₂₅H₂₂ClNO₆S*C₆H₆O₃S 
• 1403246-13-8 (S)-methyl 2-(2-chlorophenyl)-2-(2-acetyl-salicylic acyloxy-4,5,6,7-tetrahydro-thieno[3,2-C]pyridine)-5-acetate hydrochloride salt 
• 1403246-14-9 (S)-methyl 2-(2-chlorophenyl)-2-(2-acetyl-salicylic acyloxy-4,5,6,7-tetrahydro-thieno[3,2-C]pyridine)-5-acetate hydrobromide salt 
• 1402715-86-9 C₂₅H₂₂ClNO₆S*CH₄O₃S 
• 1402715-91-6 C₂₅H₂₂ClNO₆S*C₇H₈O₃S 

Relevant academic research and scientific papers

NOVEL ANTI-PLATELET COMPOUND ADDITION SALT

The present invention relates to a use of haloid acid salt and sulfonate of a compound of formula I and a salt of the compound of formula I in preparation of medicament for preventing or treating diseases caused by thrombosis or embolism. The present inve

OPTICALLY ACTIVE 2-HYDROXY TETRAHYDROTHIENOPYRIDINE DERIVATIVES, PREPARATION METHOD AND USE IN MANUFACTURE OF MEDICAMENT THEREOF

Optically active 2-hydroxytetrahydrothienopyridine derivatives represented by Formula I and pharmaceutically acceptable salts, preparation method and use in the manufacture of a medicament thereof are disclosed. The pharmacodynamic experiment results show that the present compounds of Formula I are useful for inhibiting platelet aggregation. The pharmacokinetic experiment results show that the present compound of Formula I can be converted in vivo into pharmacologically active metabolites and are therefore useful for inhibiting platelet aggregation. Therefore, the present compounds are useful for the manufacture of a medicament for preventing or treating thrombosis and embolism related diseases.

OPTICALLY ACTIVE 2-HYDROXY TETRAHYDROTHIENOPYRIDINE DERIVATIVES, PREPARATION METHOD AND USE IN MANUFACTURE OF MEDICAMENT THEREOF

Optically active 2-hydroxytetrahydrothienopyridine derivatives represented by Formula I and pharmaceutically acceptable salts, preparation method and use in the manufacture of a medicament thereof are disclosed. The pharmacodynamic experiment results show that the present compounds of Formula I are useful for inhibiting platelet aggregation. The pharmacokinetic experiment results show that the present compound of Formula I can be converted in vivo into pharmacologically active metabolites and are therefore useful for inhibiting platelet aggregation. Therefore, the present compounds are useful for the manufacture of a medicament for preventing or treating thrombosis and embolism related diseases.

Overcoming clopidogrel resistance: Discovery of vicagrel as a highly potent and orally bioavailable antiplatelet agent

A series of optically active 2-hydroxytetrahydrothienopyridine derivatives were designed and synthesized as prodrugs of clopidogrel thiolactone in order to overcome clopidogrel resistance. The final compounds were evaluated for their inhibitory effect on ADP-induced platelet aggregation in rats. Compound 9a was selected for further in vitro and in vivo metabolism studies, since its potency was comparable to that of prasugrel and was much higher than that of clopidogrel. Preliminary pharmacokinetic study results showed that the bioavailability of clopidogrel thiolactone generated from 9a was 6-fold higher than that generated from clopidogrel, implying a much lower clinically effective dose for 9a in comparison with clopidogrel. In summary, 9a (vicagrel) holds great promise as a more potent and a safer antiplatelet agent that might have the following advantages over clopidogrel: (1) no drug resistance for CYP2C19 poor metabolizers; (2) lower dose-related toxicity due to a much lower effective dose; (3) faster onset of action.