1448440-48-9

Usage

Uses

Used in Pharmaceutical Industry:
(S)-tert-butyl 2-(2-carbamoyl-4,4-difluoropyrrolidin-1-yl)-2-oxoethylcarbamate is used as a synthetic intermediate for the development of novel antibiotics and antifungals. Its application is based on its ability to inhibit the growth of dangerous bacteria and fungi, which is crucial in the ongoing battle against antimicrobial resistance.
Used in Antimicrobial Resistance Research:
T990 is used as a research compound to study its potential in combating antimicrobial resistance. The application is due to its demonstrated ability to inhibit bacterial and fungal growth, which could lead to the development of new treatments for drug-resistant infections.

Upstream product

• 4530-20-5 BOC-glycine 
• 1315053-41-8 (S)-4,4-difluoropyrrolidine-2-carboxamide hydrochloride 
• 74844-91-0 1-tert-butyl 2-methyl (2S,4R)-4-hydroxy-1,2-pyrrolidinedicarboxylate 
• 24424-99-5 di-tert-butyl dicarbonate 
• 1448440-46-7 (S)-4,4-difluoropyrrolidine-2-carboxamide trifluoroacetic acid 
• 426844-50-0 (S)-2-carbamoyl-4,4-difluoropyrrolidine-1-carboxylic acid tert-butyl ester 
• 203866-15-3 1-(tert-butoxycarbonyl)-4,4-difluoro-L-proline 
• 203866-17-5 1-tert-butyl 2-methyl (2S)-4,4-difluoropyrrolidine-1,2-dicarboxylate 
• 74844-91-0 (2S,4S)-N-tert-butoxycarbonyl-4-hydroxyproline methyl ester 
• 102195-80-2 (S)-1-tert-butyl 2-methyl 4-oxopyrrolidine-1,2-dicarboxylate 

Downstream Products

• 1448440-50-3 tert-butyl (S)-(2-(2-cyano-4,4-difluoropyrrolidin-1-yl)-2-oxoethyl)carbamate 
• 1448440-51-4 (S)-1-(2-aminoacetyl)-4,4-difluoropyrrolidine-2-carbonitrile hydrochloride 
• 1584652-36-7 (S)-1-(2-aminoacetyl)-4,4-difluoropyrrolidine-2-carbonitrile 4-methylbenzenesulfonic acid 

Relevant academic research and scientific papers

NOVEL FAP INHIBITORS

The present invention relates to novel inhibitors having high selectivity and specificity for FAP (fibroblast activation protein). Said inhibitors are useful as a human and/or veterinary medicine, in particular for the treatment and/or prevention of FAP-related disorders such as but not limited to proliferative disorders.

Extended structure-activity relationship and pharmacokinetic investigation of (4-quinolinoyl)glycyl-2-cyanopyrrolidine inhibitors of fibroblast activation protein (FAP)

Fibroblast activation protein (FAP) is a serine protease related to dipeptidyl peptidase IV (DPPIV). It has been convincingly linked to multiple disease states involving remodeling of the extracellular matrix. FAP inhibition is investigated as a therapeutic option for several of these diseases, with most attention so far devoted to oncology applications. We previously discovered the N-4-quinolinoyl-Gly-(2S)-cyanoPro scaffold as a possible entry to highly potent and selective FAP inhibitors. In the present study, we explore in detail the structure-activity relationship around this core scaffold. We report extensively optimized compounds that display low nanomolar inhibitory potency and high selectivity against the related dipeptidyl peptidases (DPPs) DPPIV, DPP9, DPPII, and prolyl oligopeptidase (PREP) the log D values, plasma stabilities, and microsomal stabilities of selected compounds were found to be highly satisfactory. Pharmacokinetic evaluation in mice of selected inhibitors demonstrated high oral bioavailability, plasma half-life, and the potential to selectively and completely inhibit FAP in vivo.

NOVEL FAP INHIBITORS

The present invention relates to novel inhibitors having high selectivity and specificity for FAP (fibroblast activation protein). Said inhibitors are useful as a human and/or veterinary medicine, in particular for the treatment and/or prevention of FAP-related disorders such as but not limited to proliferative disorders.