169512-83-8

Upstream product

• 102878-73-9 γ-(pyridin-4-yl)butyric acid 
• 90950-44-0 4-(piperidin-4-yl)butanoic acid 
• 100-43-6 4-vinylpyridine 
• 1026564-84-0 4-[3-({[(S)-2-Benzyloxycarbonyl-1-((S)-1-benzyloxycarbonyl-2-cyclohexyl-ethylcarbamoyl)-ethylcarbamoyl]-methyl}-ethyl-carbamoyl)-propyl]-piperidine-1-carboxylic acid tert-butyl ester 
• 1026234-27-4 (S)-N-((S)-1-Benzyloxycarbonyl-2-cyclohexyl-ethyl)-3-(2-ethylamino-acetylamino)-succinamic acid benzyl ester 
• 222641-21-6 (S)-N-((S)-1-Benzyloxycarbonyl-2-cyclohexyl-ethyl)-3-tert-butoxycarbonylamino-succinamic acid benzyl ester 
• 777029-24-0 (S)-3-Amino-N-((S)-1-benzyloxycarbonyl-2-cyclohexyl-ethyl)-succinamic acid benzyl ester 
• 142247-38-9 4-[1-(tert-butoxycarbonyl)piperidin-4-yl]butanoic acid 
• 92501-98-9 ethyl 2-ethoxycarbonyl-4-(pyrid-4-yl)-butanoate 
• 24424-99-5 di-tert-butyl dicarbonate 

Relevant academic research and scientific papers

Antithrombotic azacycloalkylalkanoyl peptides and pseudopeptides

The present invention relates to azacycloalkylalkanoyl peptides and pseudopeptides which inhibit platelet aggregation and thrombus formation thereby being useful in the prevention and treatment of thrombosis associated with disease states such as myocardial infarction, stroke, peripheral arterial disease, and disseminated intravascular coagulation, to methods for the prevention or treatment of thrombosis in a mammal in need of such therapy comprising the administration of a therapeutically effective amount of such compounds, and to pharmaceutical compositions comprising such compounds.

Design of a new class of orally active fibrinogen receptor antagonists

The integrin receptor recognition sequence Arg-Gly-Asp was successfully used as a template from which to develop a series of potent, selective, orally active, peptide-based fibrinogen receptor antagonists with a long duration of action. Simple modifications centered on the Arg and Gly residues quickly led to a modified peptide (1) with significantly enhanced ability to inhibit in vitro platelet aggregation. Substitution of the guanidino group in 1 by piperidine provided 3, which showed not only a further increase in potency but also a modest degree of oral efficacy. Finally, exploration of the nature of the C-terminal amino acid, with respect to its side-chain functionality and the carboxy terminus, yielded a group of molecules that showed excellent in vitro potency for inhibiting platelet aggregation, excellent integrin selectivity, a high level of oral efficacy, and an extended duration of action.