916736-25-9

Upstream product

• 130761-99-8 benzyl 3-oxocyclopentanecarboxylate 
• 98-78-2 3-Oxo-cyclopentanecarboxylic acid 
• 1048963-82-1 tert-butyl ((1R)-1-{5-[5-chloro-3-fluoro-2-(2-methyl-2H-tetrazol-5-yl)phenyl]-3-fluoropyridin-2-yl}ethyl)carbamate 
• 916736-73-7 benzyl 3,3-difluoro-1-hydroxycyclopentanecarboxylate 
• 916736-70-4 5-(2-bromo-4-chloro-6-fluorophenyl)-1H-tetrazole 
• 858414-22-9 2-bromo-4-chloro-6-fluorobenzonitrile 
• 916736-69-1 5-(2-bromo-4-chloro-6-fluorophenyl)-2-methyl-2H-tetrazole 

Downstream Products

• 1075221-24-7 C₂₁H₁₉ClF₄N₆O₂ 
• 1075221-23-6 C₂₁H₁₉ClF₄N₆O₂ 

Relevant academic research and scientific papers

Bradykinin B1 receptor antagonists: An α-hydroxy amide with an improved metabolism profile

A series of carbo- and heterocyclic α-hydroxy amide-derived bradykinin B1 antagonists was prepared and evaluated. A 4,4-difluorocyclohexyl α-hydroxy amide was incorporated along with a 2-methyl tetrazole in lieu of an oxadiazole to afford a suitable compound with good pharmacokinetic properties, CNS penetration, and clearance by multiple metabolic pathways.

l-HYDROXYCYCLOALKANECARBOXAMIDE DERIVATIVES AS BRADYKININ ANTAGONISTS

α-Hydroxycycloalkanecarboxamide derivatives of formula (I) or a pharmaceutically acceptable salt thereof, wherein formula (a) is a single or double bond; Rl, R2 and R3 are each independently selected from H, halogen and OH; or Rl and R2 attached to the same carbon atom together represent oxo; R4 is H or methyl; R5 is Cl or F; R6 is selected from -CO2-C1-4alkyl, -O-C1-4alkyl, -O- C1-4haloalkyl, 2-methyltetrazol-5-yl, 5-methyl l,2,4-oxadiazol-3-yl, 3-methyl-1,2,4-oxadiazol-5-yl, 5-halomethyl-l,2,4-oxadiazol-3-yl, 3-halomethyl- l,2,4-oxadiazol-5-yl, tetrazol-5-yl, 5-halomethyl-l,2,3-triazolyl, and 5-methyl-l ,2,3-triazolyl; R7 and R8 are each independently Cl or F; and n is 0 or 1, are bradykinin B1 antagonists or inverse agonists useful in the treatment or prevention of symptoms such as pain and inflammation associated with the bradykinin B1 pathway.