811450-79-0

Upstream product

• 811450-77-8 (2R)-2-(tert-butoxycarbonyl-amino)-3-methoxy-N-[3-methyl-4-(3-oxo-morpholin-4-yl)-phenyl]-propionamide 
• 482308-10-1 4-(4-amino-2-methylphenyl)morpholin-3-one 
• 845729-49-9 (2-chloroethoxy)-N-(2-methyl-4-nitrophenyl)acetamide 
• 845729-40-0 4-(2-methyl-4-nitrophenyl)morpholin-3-one 
• 99-52-5 2-methyl-4-nitro-benzenamine 

Downstream Products

• 811811-33-3 EMD 495235 

Relevant academic research and scientific papers

NOVEL SUBSTITUTED THIOPHENECARBOXAMIDES, THEIR PRODUCTION AND THEIR USE AS MEDICAMENTS

The invention relates to novel substituted thiophene-2-carboxamides of general formula (I), in which A, and R1 to R8c are defined as cited in claim 1. The invention also relates to the tautomers, enantiomers, diastereomers, mixtures and salts, in particular the physiologically compatible salts of said compounds containing inorganic or organic acids or bases, which exhibit valuable properties.

Chlorothiophenecarboxamides as P1 surrogates of inhibitors of blood coagulation factor Xa

Neutral chlorothiophenecarboxamides bearing an amino acid and a substituted aniline were synthesized and investigated for their factor Xa inhibitory activity in vitro. From selected 2-methylphenyl morpholinones the solution properties were determined. The most soluble and active compounds were then investigated in different animal species to compare the pharmacokinetic parameters. This led to a potent, water soluble and orally bioavailable candidate for further development: EMD 495235.