697284-64-3

Upstream product

• 16937-99-8 N-Boc-D-Leu 
• 438056-69-0 4-(4-aminophenyl)morpholin-3-one 
• 811450-82-5 4-(2-(2-chloroethoxy)acetamido)1-nitrobenzene 
• 446292-04-2 4-(4-nitrophenyl)-3-morpholinone 
• 100-01-6 4-nitro-aniline 

Downstream Products

• 697284-65-4 (R)-2-amino-4-methyl-pentanoic acid [4-(3-oxo-morpholin-4-yl)-phenyl]-amide hydrochloride 
• 769119-47-3 (R)-2-Amino-4-methyl-pentanoic acid [4-(3-oxo-morpholin-4-yl)-phenyl]-amide 

Relevant academic research and scientific papers

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.

CARBOXAMIDES

The invention relates to novel compounds of formula (I) wherein D, W, X, Y, T, m and R1 have the designations cited in patent claim 1. Said novel compounds are inhibitors of the coagulation factor Xa and can be used for the prophylaxis and/or treatment of thromboembolic diseases and for the treatment of tumours.