1334782-54-5

Basic information

• Product Name: 2-(4-methoxyphenyl)-1-{2-[(1R)-5-(pyrimidin-2-yl)-2,3-dihydro-1H-inden-1-yl]-2,7-diazaspiro[3.5]non-7-yl}ethanone
• Synonyms: 2-(4-methoxyphenyl)-1-{2-[(1R)-5-(pyrimidin-2-yl)-2,3-dihydro-1H-inden-1-yl]-2,7-diazaspiro[3.5]non-7-yl}ethanone
• CAS NO: 1334782-54-5
• Molecular Weight: 468.599
• Mol File: 1334782-54-5.mol
• Article Data: 3

Chemical Properties

• CAS DataBase Reference: 2-(4-methoxyphenyl)-1-{2-[(1R)-5-(pyrimidin-2-yl)-2,3-dihydro-1H-inden-1-yl]-2,7-diazaspiro[3.5]non-7-yl}ethanone(CAS DataBase Reference)
• NIST Chemistry Reference: 2-(4-methoxyphenyl)-1-{2-[(1R)-5-(pyrimidin-2-yl)-2,3-dihydro-1H-inden-1-yl]-2,7-diazaspiro[3.5]non-7-yl}ethanone(1334782-54-5)
• EPA Substance Registry System: 2-(4-methoxyphenyl)-1-{2-[(1R)-5-(pyrimidin-2-yl)-2,3-dihydro-1H-inden-1-yl]-2,7-diazaspiro[3.5]non-7-yl}ethanone(1334782-54-5)

Safety Data

• Hazardous Substances Data: 1334782-54-5(Hazardous Substances Data)

Upstream product

• 1334785-14-6 tert-butyl 2-(5-pyrimidin-2-yl-2,3-dihydro-1H-inden-1-yl)-2,7-diazaspiro[3.5]nonane-7-carboxylate 
• 1414782-20-9 tert-butyl 2-[(R)-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-2,3-dihydro-1H-inden-1-yl]-2,7-diazaspiro[3.5]nonane-7-carboxylate 
• 1312131-45-5 tert-butyl 4-(chloromethyl)-4-(hydroxymethyl)piperidine-1-carboxylate 
• 104-01-8 4-Methoxyphenylacetic acid 
• 1334785-04-4 tert-butyl 2-[(R)-5-(pyrimidin-2-yl)-2,3-dihydro-1H-inden-1-yl]-2,7-diazaspiro[3.5]nonane-7-carboxylate 
• 1312131-48-8 tert-butyl 4-(chloromethyl)-4-formylpiperidine-1-carboxylate 
• 1314319-01-1 1-tert-butyl 4-methyl 4-(chloromethyl)piperidine-1,4-dicarboxylate 
• 124443-68-1 1-tert-Butyl 4-methyl piperidine-1,4-dicarboxylate 
• 1334784-74-5 5-(pyrimidin-2-yl)-2,3-dihydro-1H-inden-1-one 
• 1023301-84-9 tert-butyl 2,7-diazaspiro[3.5]nonane-7-carboxylate hydrochloride 
• 214360-81-3 5-( 4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-2,3-dihydro-1H-inden-1-one 
• 1314319-10-2 tert-butyl 2-[(1R)-5-bromo-2,3-dihydro-1H-inden-1-yl]-2,7-diazaspiro[3.5]nonane-7-carboxylate 
• 1334784-73-4 (1R)-1-azido-5-bromo-2,3-dihydro-1H-indene 
• 1270284-15-5 (1S)-5-bromo-2,3-dihydro-1H-inden-1-ol 

Relevant articles and documents

Discovery of PF-5190457, a potent, selective, and orally bioavailable ghrelin receptor inverse agonist clinical candidate

The identification of potent, highly selective orally bioavailable ghrelin receptor inverse agonists from a spiro-azetidino-piperidine series is described. Examples from this series have promising in vivo pharmacokinetics and increase glucose-stimulated insulin secretion in human whole and dispersed islets. A physicochemistry-based strategy to increase lipophilic efficiency for ghrelin receptor potency and retain low clearance and satisfactory permeability while reducing off-target pharmacology led to the discovery of 16h. Compound 16h has a superior balance of ghrelin receptor pharmacology and off-target selectivity. On the basis of its promising pharmacological and safety profile, 16h was advanced to human clinical trials.

2,3-DIHYDRO-1H-INDEN-1-YL-2,7-DIAZASPIRO[3.5] NONANE DERIVATIVES

The present invention provides a compound of Formula (I) or a pharmaceutically salt thereof wherein R1, R2, Ra, L, Z, Z1 and Z2 are as defined herein, that act as Ghrelin antagonists or inverse agonists; pharmaceutical compositions thereof; and methods of treating diseases, disorders, or conditions mediated by the antagonism of the Ghrelin receptor.