154731-80-3

Upstream product

• 143060-31-5 N-(tert-butoxycarbonyl)-3,3-diphenyl-D-alanine 

Downstream Products

• 183853-44-3 (S)-1-((R)-2-tert-Butoxycarbonylamino-3,3-dicyclohexyl-propionyl)-pyrrolidine-2-carboxylic acid methyl ester 
• 1300198-05-3 {(R)-2,2-dicyclohexyl-1-[(1H-pyrrolo[2,3-b]pyridin-5-ylmethyl)-carbamoyl]-ethyl}-carbamic acid tert-butyl ester 
• 1194096-67-7 ((S)-1-[(R)-1-[(6-amino-pyridin-3-ylmethyl)-carbamoyl]-2,2-dicyclohexyl-ethylcarbamoyl]-2-methylbutyl)carbamic acid tert-butyl ester 
• 1300006-88-5 N-{(R)-1-[(6-amino-pyridin-3-ylmethyl)-carbamoyl]-2,2-dicyclohexyl-ethyl}-2-hydroxy-2-methyl-propionamide trifluoroacetate 
• 1194096-64-4 {(R)-1-[(6-amino-pyridin-3-ylmethyl)-carbamoyl]-2,2-dicyclohexyl-ethyl}-carbamic acid tert-butyl ester 
• 197893-48-4 ((R)-1-{(S)-2-[(2-Amino-thiazol-4-ylmethyl)-carbamoyl]-pyrrolidine-1-carbonyl}-2,2-dicyclohexyl-ethyl)-carbamic acid tert-butyl ester 
• 183853-45-4 ((R)-1-{(S)-2-[(6-Amino-pyridin-3-ylmethyl)-carbamoyl]-pyrrolidine-1-carbonyl}-2,2-dicyclohexyl-ethyl)-carbamic acid tert-butyl ester 
• 177583-50-5 (S)-1-((R)-2-tert-Butoxycarbonylamino-3,3-dicyclohexyl-propionyl)-pyrrolidine-2-carboxylic acid 

Relevant academic research and scientific papers

Discovery of a novel, selective, and orally bioavailable class of thrombin inhibitors incorporating aminopyridyl moieties at the P1 position

A novel class of thrombin inhibitors incorporating aminopyridyl moieties at the P1 position has been discovered. Four of these thrombin inhibitors (13b,c,e and 14d) showed nanomolar potency (K(i) 0.8-12 nM), 300-1500-fold selectivity for thrombin compared with trypsin, and good oral bioavailability (F = 40-76%) in rats or dogs. The neutral P1 was expected to increase metabolic stability and oral absorption. Identification of this novel aminopyridyl group at P1 was a key step in our search for a clinical candidate.

AZAINDOLE DERIVATIVES

The present invention provides compounds of formula (I): compositions comprising such compounds; the use of such compounds in therapy (such as asthma or COPD); and methods of treating patients with such compounds; wherein R1 to R20 and A1 are as defined herein.

AMINOPYRIDINE DERIVATIVES AS KALLIKREIN INHIBITORS

The present invention provides compounds of formula (I): compositions comprising such compounds; the use of such compounds in therapy (such as asthma or COPD); and methods of treating patients with such compounds; wherein R1 - R10 and A1 are as defined herein.

AMINOTHIAZOLE DERIVATIVES USEFUL AS KLK1 INHIBITORS

The present invention provides compounds of formula (I): compositions comprising such compounds; the use of such compounds in therapy (such as asthma or COPD); and methods of treating patients which such compounds; wherein R1 to R17 and A1 are as defined herein.

AMINOPYRIDINE DERIVATIVES

The present invention provides compounds of formula (I): compositions comprising such compounds; the use of such compounds in therapy (such as asthma or COPD); and methods of treating patients with such compounds; wherein R1 - R11 ar

2,3-methano-amino acid compounds

Compound of formula (I): wherein: n represents 2 or 3, R1represents optionally substituted alkyl, cycloalkyl or optionally substituted phenyl, R2represents amino, optionally substituted amidino, optionally substituted guanidino or optionally substituted isothioureido, Ar represents aryl or heteroaryl, X1represents hydroxy or optionally substituted amino, isomers thereof, and also salts thereof with a pharmaceutically acceptable acid or base, and which medicinal products containing the same/are useful as trypsin-related serine protease inhibitors.