328232-95-7

Usage

Uses

Used in Pharmaceutical Industry:
Spiro[cyclohexane-1,3'(1'H)-furo[3,4-c]pyridine]-4-carboxamide, N-[1-(2-fluorophenyl)-1H-pyrazol-3-yl]-1'-oxo-, transis used as a potential pharmaceutical agent for its diverse structural motifs that are commonly found in biologically active compounds. Spiro[cyclohexane-1,3'(1'H)-furo[3,4-c]pyridine]-4-carboxamide, N-[1-(2-fluorophenyl)-1H-pyrazol-3-yl]-1'-oxo-, trans-'s unique molecular structure may offer novel therapeutic opportunities, although further research and testing are required to explore its properties and efficacy.

Upstream product

• 685094-07-9 3-amino-1-(2-fluorophenyl)-1H-pyrazole 
• 328233-23-4 trans-1'-oxospiro[1,3'-cyclohexane(1'H)-furo[3,4-c]pyridine]-4-carboxylic acid 
• 569351-62-8 1'-oxospiro[1,3'-cyclohexane(1'H)-furo[3,4-c]pyridine]-4-carboxylic acid 
• 870466-68-5 C₁₇H₂₁NO₄ 
• 923984-29-6 trans-N-[1-(2-fluorophenyl)-3-pyrazolyl]-3-oxospiro[6-azaisobenzofuran-1(3H),1'-cyclohexane]-4'-carboxamide mesylate 
• 17159-79-4 ethyl 4-oxocyclohexane-1-carboxylate 
• 3034-31-9 N-phenylisonicotinamide 

Downstream Products

• 923984-28-5 trans-N-[1-(2-fluorophenyl)-3-pyrazolyl]-3-oxospiro[6-azaisobenzofuran-1(3H),1'-cyclohexane]-4'-carboxamide fumarate 
• 923984-29-6 trans-N-[1-(2-fluorophenyl)-3-pyrazolyl]-3-oxospiro[6-azaisobenzofuran-1(3H),1'-cyclohexane]-4'-carboxamide mesylate 

Relevant academic research and scientific papers

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.

SYNTHESIS AND CRYSTALLINE FORMS OF NPY5 ANTAGONIST

The present invention relates to a process for producing crystalline trans-N-[l-(2-fluorophenyl)- S-pyrazoly]-3-oxospiro[6-azaisobenzofuran-1(3H),1'-cyclohexane]-4'-carboxamide and novel salts, hydrates and polymorphs thereof.

Practical synthesis of a neuropeptide Y antagonist via stereoselective addition to a ketene

The synthesis of neuropeptide Y antagonist 1, currently under clinical investigation for the treatment of obesity, is described. The convergent synthesis from trans-spirolactone carboxylic acid intermediate 2a and aminopyrazole 3 is predicated on a stereo

Spiro compounds

Compounds of the general formula (I): wherein Ar1represents 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.

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.