540522-73-4

Upstream product

• 63069-48-7 p-chloro-o-iodoaniline 
• 776-74-9 Bromodiphenylmethane 
• 91-01-0 1,1-Diphenylmethanol 

Downstream Products

• 540522-74-5 4-{5-chloro-2-[(diphenylmethyl)amino]phenyl}but-3-yn-1-ol 
• 540522-75-6 2-[5-chloro-1-(diphenylmethyl)-1H-indol-2-yl]ethanol 
• 934285-48-0 2-(2-{[tert-butyl(diphenyl)silyl]oxy}ethyl)-5-chloro-1-(diphenylmethyl)-1H-indole 
• 1002987-27-0 C₄₂H₄₀ClNO₄Si 
• 540522-76-7 2-[2-(2-{[tert-butyl(diphenyl)silyl]oxy}ethyl)-5-chloro-1-(diphenylmethyl)-1H-indol-3-yl]ethanol 
• 540526-73-6 methyl 3-{2-[2-(2-{[tert-butyl(diphenyl)silyl]oxy}ethyl)-5-chloro-1-(diphenylmethyl)-1H-indol-3-yl]ethoxy}benzoate 
• 540526-77-0 methyl 2-{2-[2-(2-{[tert-butyl(diphenyl)silyl]oxy}ethyl)-5-chloro-1-(diphenylmethyl)-1H-indol-3-yl]ethoxy}benzoate 
• 540526-74-7 methyl 3-{2-[5-chloro-1-(diphenylmethyl)-2-(2-hydroxyethyl)-1H-indol-3-yl]ethoxy}benzoate 
• 540526-78-1 methyl 2-{2-[5-chloro-1-(diphenylmethyl)-2-(2-hydroxyethyl)-1H-indol-3-yl]ethoxy}benzoate 
• 1026054-63-6 C₃₄H₃₂ClNO₆S 
• 934285-55-9 C₃₄H₃₂ClNO₆S 
• 1026675-29-5 methyl 3-{2-[2-(2-azidoethyl)-5-chloro-1-(diphenylmethyl)-1H-indol-3-yl]ethoxy}benzoate 
• 934285-57-1 methyl 2-{2-[2-(2-azidoethyl)-5-chloro-1-(diphenylmethyl)-1H-indol-3-yl]ethoxy}benzoate 
• 540523-34-0 methyl 3-{2-[2-(2-aminoethyl)-5-chloro-1-(diphenylmethyl)-1H-indol-3-yl]ethoxy}benzoate 

Relevant academic research and scientific papers

Methods for the use of inhibitors of cytosolic phospholipase A2 in the treatment of thrombosis

This invention provides methods for the use of substituted indole compounds of the general formula: and pharmaceutically acceptable salt forms thereof. The invention provides methods for the use of the compounds in the treating or preventing thrombosis in a mammal, or preventing progression of symptoms of thrombosis.

Discovery of ecopladib, an indole inhibitor of cytosolic phospholipase A2α

The synthesis and structure-activity relationship of a series of indole inhibitors of cytosolic phospholipase A2α (cPLA 2α, type IVA phospholipase) are described. Inhibitors of cPLA2α are predicted to be efficacious in treating asthma as well as the signs and symptoms of osteoarthritis, rheumatoid arthritis, and pain. The introduction of a benzyl sulfonamide substituent at C2 was found to impart improved potency of these inhibitors, and the SAR of these sulfonamide analogues is disclosed. Compound 123 (Ecopladib) is a submicromolar inhibitor of cPLA2α in the GLU micelle and rat whole blood assays. Compound 123 displayed oral efficacy in the rat carrageenan air pouch and rat carrageenan-induced paw edema models.

Process for the synthesis C-2, C-3 substituted N-alkylated indoles useful as CPLA2 inhibitors

The present invention provides method for making a compound of formula 1: comprising the steps of reacting compounds of formulas 2 and 3: to produce a compound of formula 4: wherein R1, R2, R3, R4 and R5 /

Process for the synthesis of a CPLA2 inhibitor

A process for making a substituted indole compound, including the steps of: reacting the compounds in a non-protic polar solvent in the presence of a catalyst to form the intermediate compound wherein Ph and X are as defined herein; and then, heating this intermediate compound in the solvent in the presence of the catalyst to form the substituted indole compound The invention also includes compounds formed by this process.

Inhibitors of cytosolic phospholipase A2

This invention provides substituted indole compounds of the general formula: and pharmaceutically acceptable salt forms thereof, and methods for using the compounds as inhibitors of the activity of various phospholipase enzymes, particularly phospholipase A2 enzymes, and for the medical treatment, prevention and inhibition of pain and inflammation.