328232-91-3

Basic information

• Product Name: trans-3-oxo-N-(1-phenyl-1H-pyrazol-4-yl)-3H-spiro[4-aza-2-benzofuran-1,1'-cyclohexane]-4'-carboxamide
• CAS NO: 328232-91-3
• Molecular Weight: 388.426
• Mol File: 328232-91-3.mol
• Article Data: 3

Chemical Properties

• CAS DataBase Reference: trans-3-oxo-N-(1-phenyl-1H-pyrazol-4-yl)-3H-spiro[4-aza-2-benzofuran-1,1'-cyclohexane]-4'-carboxamide(CAS DataBase Reference)
• NIST Chemistry Reference: trans-3-oxo-N-(1-phenyl-1H-pyrazol-4-yl)-3H-spiro[4-aza-2-benzofuran-1,1'-cyclohexane]-4'-carboxamide(328232-91-3)
• EPA Substance Registry System: trans-3-oxo-N-(1-phenyl-1H-pyrazol-4-yl)-3H-spiro[4-aza-2-benzofuran-1,1'-cyclohexane]-4'-carboxamide(328232-91-3)

Safety Data

• Hazardous Substances Data: 328232-91-3(Hazardous Substances Data)

Upstream product

• 1128-53-6 1-phenyl-1H-pyrazol-4-amine 
• 328233-13-2 trans-3-oxo-3H-spiro[4-aza-2-benzofuran-1,1'-cyclohexane]-4'-carboxylic acid 

Relevant articles and documents

Discovery of trans-N-[1-(2-fluorophenyl)-3-pyrazolyl]-3-oxospiro[6-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide, a potent and orally active neuropeptide Y Y5 receptor antagonist

A series of trans-3-oxospiro[(aza)isobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide derivatives were synthesized to identify potent NPY Y5 receptor antagonists. Of the compounds, 21j showed high Y5 binding affinity, metabolic stability and brain and cerebrospinal fluid (CSF) penetration, and low susceptibility to P-glycoprotein transporters. Oral administration of 21j significantly inhibited the Y5 agonist-induced food intake in rats with a minimum effective dose of 1 mg/kg. This compound was selected for proof-of-concept studies in human clinical trials.

Novel spiro compounds

Compounds of the general formula (I): wherein Ar1 represents optionally substituted aryl or heteroaryl; n represents 0 or 1; T, U, V, and W each independently represent nitrogen atom or optionally substituted methine group, where at least two of them represent the said methine group; X represents methine or hydroxy substituted methine; Y represents an optionally substituted imino or oxygen atom are described and claimed. These novel spiro compounds are useful as neuropeptide Y receptor antagonists and as agents for the treatment of various kinds of cardiovascular disorders, central nervous system disorders, metabolic diseases and the like.