540522-76-7

Upstream product

• 58479-61-1 tert-butylchlorodiphenylsilane 
• 540522-62-1 2-(2-{[tert-butyl(diphenyl)silyl]oxy}ethyl)-5-chloro-1H-indole 
• 540522-61-0 2-(5-chloro-1H-indol-2-yl)ethanol 
• 540522-60-9 N-(2-bromo-4-chlorophenyl)-2,2,2-trifluoroacetamide 
• 873-38-1 4-chloro-2-bromoaniline 
• 540524-33-2 ethyl [1-benzhydryl-2-({[tert-butyl(diphenyl)silyl]oxy}ethyl)-5-chloro-1H-indol-3-yl](oxo)acetate 
• 776-74-9 Bromodiphenylmethane 
• 63069-48-7 p-chloro-o-iodoaniline 
• 934285-48-0 2-(2-{[tert-butyl(diphenyl)silyl]oxy}ethyl)-5-chloro-1-(diphenylmethyl)-1H-indole 
• 540522-75-6 2-[5-chloro-1-(diphenylmethyl)-1H-indol-2-yl]ethanol 
• 540522-74-5 4-{5-chloro-2-[(diphenylmethyl)amino]phenyl}but-3-yn-1-ol 
• 540522-73-4 4-chloro-N-(diphenylmethyl)-2-iodoaniline 
• 1002987-27-0 C₄₂H₄₀ClNO₄Si 

Downstream Products

• 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 
• 540526-79-2 methyl 2-{2-[2-(2-aminoethyl)-5-chloro-1-(diphenylmethyl)-1H-indol-3-yl]ethoxy}benzoate 
• 934285-60-6 methyl 3-{2-[2-{2-[(benzylsulfonyl)amino]ethyl}-5-chloro-1-(diphenylmethyl)-1H-indol-3-yl]ethoxy}benzoate 
• 934285-61-7 methyl 2-{2-[2-{2-[(benzylsulfonyl)amino]ethyl}-5-chloro-1-(diphenylmethyl)-1H-indol-3-yl]ethoxy}benzoate 
• 540524-35-4 methyl 3-[4-({2-[2-(2-{[tert-butyl(diphenyl)silyl]oxy}ethyl)-5-chloro-1-(diphenylmethyl)-1H-indol-3-yl]ethyl}thio)phenyl]propanoate 
• 916136-76-0 methyl 3-[4-({2-[2-(2-{[tert-butyl(diphenyl)silyl]oxy}ethyl)-5-chloro-1-(diphenylmethyl)-1H-indol-3-yl]ethyl}sulfonyl)phenyl]propanoate 

Relevant academic research and scientific papers

PHARMACEUTICAL COMPOSITION FOR TOPICAL ADMINISTRATION

The present invention relates to a pharmaceutical composition for topical administration comprising a compound of formula I, 3-{4-[2-{5-chloro-1-(diphenylmethyl)-2-[2-({[2-(trifluoromethyl)benzyl]sulfonyl}amino)ethyl]-1H-indol-3-yl}ethyl]sulfonyl}phenyl}p

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.

INHIBITORS OF CYTOSOLIC PHOSPHOLIPASE A2

This invention provides chemical inhibitors of the activity of various phospholipase enzymes, particularly cytosolic phospholipase A2 enzymes (cPLA2), more particularly including inhibitors of cytosolic phospholipase A2 alpha enzymes (cPLAα). In some embodiments, the inhibitors have the Formula I: wherein the constituent variables are as defined herein.