865451-74-7

Upstream product

• 536747-52-1 1-(4-amino-3-fluoro-phenyl)-pyridin-2-one 
• 595556-31-3 (R,R)-pyrrolidine-1,3,4-tricarboxylic acid 1-tert-butyl ester 3-ethyl ester 
• 595547-23-2 (+/-)-trans-pyrrolidine-1,3,4-tricarboxylic acid 1-tert-butyl ester 3,4-diethyl ester 
• 623-91-6 diethyl Fumarate 
• 92486-65-2 diethyl trans-N-benzyl-pyrrolidine-3,4-dicarboxylate 

Downstream Products

• 865451-75-8 (3R,4R)-4-[2-fluoro-4-(2-oxo-2H-pyridin-1-yl)-phenylcarbamoyl]-pyrrolidine-3-carboxylic acid ethyl ester hydrochloride 
• 865528-40-1 C₁₉H₂₀FN₃O₄ 

Relevant academic research and scientific papers

Discovery of a factor Xa inhibitor (3R,4R)-1-(2,2-difluoro-ethyl)- pyrrolidine-3,4-dicarboxylic acid 3-[(5-chloro-pyridin-2-yl)-amide] 4-{[2-fluoro-4-(2-oxo-2H-pyridin-1-yl)-phenyl]-amide} as a clinical candidate

A series of (3R,4R)-pyrrolidine-3,4-dicarboxylic acid amides was investigated with respect to their factor Xa inhibitory activity, selectivity, pharmacokinetic properties, and ex vivo antithrombotic activity. The clinical candidate from this series, R1663

NEW SOLID FORMS OF FXA INHIBITORS

The invention is concerned with crystalline forms or amorphous forms of a pyrrolidine- 3,4-dicarboxamide derivative, which is useful as an active ingredient of medicaments for the diseases which can be treated by the coagulation factor Xa inhibitors.

PROCESSES FOR THE PREPARATION OF (3R, 4R) -N- (4 -CHLOROPHENYL) -1- (2, 2-DIFLUOROETHYL) -N' - [2-FLUORO-4- (2-OXO-1 (2H) -PYRIDINYL) PHENYL] -3, 4-PYRROLIDINEDICARBOXAMIDE

The invention is concerned with processes for the manufacture of pyrrolidine-3,4- dicarboxamide derivative of formula (I), and the intermediates useful for those processes.

NOVEL PYRROLIDINE-3,4-DICARBOXAMIDE DERIVATIVES

The invention is concerned with novel pyrrolidine-3,4-dicarboxamide derivatives of Formula (I) ; wherein Rl to R9 and X are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These c