164414-71-5

Basic information

• Product Name: CILOMILAST
• Synonyms: CFBUZOUXXHZCFB-UHFFFAOYSA-N
• CAS NO: 164414-71-5
• Molecular Formula: C20H25NO4
• Molecular Weight: 343.4168
• Mol File: 164414-71-5.mol
• Article Data: 12

Chemical Properties

• Appearance: /
• CAS DataBase Reference: CILOMILAST(CAS DataBase Reference)
• NIST Chemistry Reference: CILOMILAST(164414-71-5)
• EPA Substance Registry System: CILOMILAST(164414-71-5)

Safety Data

• Hazardous Substances Data: 164414-71-5(Hazardous Substances Data)

Upstream product

• 153259-61-1 methyl trans-[4-cyano-4-(3-cyclopentyloxy-4-methoxyphenyl)cyclohexane-1-carboxylate] 
• 152630-47-2 4-cyano-4-[3-(cyclopentyloxy)-4-methoxyphenyl]cyclohexan-1-one 
• 153260-05-0 2-[4-cyano-4-(3-cyclopentyloxy-4-methoxyphenyl)cyclohexylidene]-1,3-dithiane 
• 153259-59-7 methyl 4-cyano-4-(3-cyclopentyloxy-4-methoxyphenyl)cyclohex-1-ene-1-carboxylate 
• 153259-62-2 methyl cis-[4-cyano-4-(3-cyclopentyloxy-4-methoxyphenyl)cyclohexane-1-carboxylate] 
• 326008-99-5 methyl 2-chloro-6-cyano-6-(3-cyclopentyloxy-4-methoxyphenyl)-1-oxospiro[2.5]octane-2-carboxylate 
• 67-56-1 methanol 
• 350044-42-7 4-(3-cyclopentyloxy-4-methoxyphenyl)-1,4-dicyanocyclohexan-1-ol 

Relevant articles and documents

Repurposing human PDE4 inhibitors for neglected tropical diseases: Design, synthesis and evaluation of cilomilast analogues as Trypanosoma brucei PDEB1 inhibitors

A medicinal chemistry exploration of the human phosphodiesterase 4 (hPDE4) inhibitor cilomilast (1) was undertaken in order to identify inhibitors of phosphodiesterase B1 of Trypanosoma brucei (TbrPDEB1). T. brucei is the parasite which causes African sleeping sickness, a neglected tropical disease that affects thousands each year, and TbrPDEB1 has been shown to be an essential target of therapeutic relevance. Noting that 1 is a weak inhibitor of TbrPDEB1, we report the design and synthesis of analogs of this compound, culminating in 12b, a sub-micromolar inhibitor of TbrPDEB1 that shows modest inhibition of T. brucei proliferation.

Process for preparing acids via alpha-chloroepoxy esters

This invention relates to a method for preparing certain acids of formula (I) via a chloroepoxy ester, which are useful as phosphodiesterase 4 inhibitors.

Process and intermediates for making 4-cyanosubstituted cyclohexanoic acids

Herein is provided a process for preparing substituted cyclohexanoic acids of formula (I), where Rais a carbon-containing group optionally linked by oxygen, sulfur or nitrogen to the phenyl ring and j is 1-5; and one of R and R* is hydrogen and the other is C(O)OH.