191870-37-8

Upstream product

• 42287-94-5 (4-cyanophenyl)propionic acid 
• 57180-71-9 3-(4cyano-phenyl)propionic acid chloride 

Downstream Products

• 191870-38-9 4-[2-(aminocarbonyl)ethyl]phenylmethanamine 
• 191870-39-0 (R)-N-[[4-[2-(aminocarbonyl)ethyl]phenyl]methyl]-N₅-[amino(nitroimino)methyl]-N₂-(diphenylacetyl)-ornithinamide 

Relevant academic research and scientific papers

Identification of BR102910 as a selective fibroblast activation protein (FAP) inhibitor

Fibroblast activation protein (FAP) belongs to the family of prolyl-specific serine proteases and displays both exopeptidase and endopeptidase activities. FAP expression is undetectable in most normal adult tissues, but is greatly upregulated in sites of tissue remodeling, which include fibrosis, inflammation and cancer. Due to its restricted expression pattern and dual enzymatic activities, FAP inhibition is investigated as a therapeutic option for several diseases. In the present study, we described the structure–activity relationship of several synthesized compounds against DPPIV and prolyl oligopeptidase (PREP). In particular, BR102910 (compound 24) showed nanomolar potency and high selectivity. Moreover, the in vivo FAP inhibition study of BR102910 (compound 24) using C57BL/6J mice demonstrated exceptional profiles and satisfactory FAP inhibition efficacy. Based on excellent in vitro and in vivo profiles, the potential of BR102910 (compound 24) as a lead candidate for the treatment of type 2 diabetes is considered.

Amino acid derivatives, pharmaceutical compositions containing these compounds and processes for preparing them

NPY-antagonistic compounds of the formula STR1 Exemplary are: (A) (R)-N-[[4-(Aminocarbonylaminomethyl)phenyl]methyl]-N 2-bis(4-hydroxyphenyl)acetyl]-argininamide-trifluoracetate;(B) (R)-N-[[4-(Aminocarbonylaminomethyl)phenyl]methyl]-N 2-[bis(4-chlorphenyl)acetyl]-argininamide-trifluoracetate;(C) (R)-N-[[4-Aminocarbonylaminomethyl)phenyl]methyl]-N 2-(diphenylacetyl)-argininamide-trifluoracetate;(D) (R)-N 2-(Diphenylacetyl)-N-[[4-(ethoxycarbonylmethylamino-carbonylaminomethyl) phenyl]methyl]-argininamide-trifluoroacetate;(E) (R,S)-N 5-(Aminoiminomethyl)-N 2-(diphenylacetyl)-N-[(4-hy-droxyphenyl)methyl]-N 5-methyl-ornithinamide-hydrochloride; (F) (R)-N-[[4-(Aminocarbonylmethyl)phenyl]methyl]-N 2-(diphenyl-acetyl)-argininamide-diacetate;(G) (R)-N. sup. 2-(Diphenylacetyl)-N-[[4-(ethylaminocarbonylamino-methyl)-phenyl]methyl]-argininamide-bis-(trifluoroacetate); and,(H) (R)-N. sup.2-(Diphenylacetyl)-N-[[4-(ethoxycarbonylamino-carbonylaminomethyl) phenyl]methyl]-argininamide-trifluoroacetate.