381683-94-9

Usage

Uses

Treatment of pain and symptomatic management of arthritis.

Upstream product

• 847203-50-3 4-{3-[2-(2-Amino-ethyl)-1-benzhydryl-5-chloro-1H-indol-3-yl]-propyl}-benzoic acid 
• 21149-38-2 2,2,2-trifluoro-N,N-bis(trimethylsilyl)-acetamide 
• 85952-30-3 [(3,4-dichlorophenyl)-methyl]sulfonyl chloride 
• 683813-29-8 methyl 4-{3-[5-chloro-2-(2-{[(3,4-dichlorobenzyl)sulfonyl]amino}ethyl)-1-(diphenylmethyl)-1H-indol-3-yl]propyl}benzoate 

Relevant academic research and scientific papers

Indole cytosolic phospholipase A2 α inhibitors: Discovery and in vitro and in vivo characterization of 4-{3-[5-chloro-2-(2-{[(3,4- dichlorobenzyl)sulfonyl]amino}ethyl)-1-(diphenylmethyl)-1H-indol-3-yl]propyl} benzoic acid, efipladib

The optimization of a class of indole cPLA2α inhibitors is described herein. The importance of the substituent at C3 and the substitution pattern of the phenylmethane sulfonamide region are highlighted. Optimization of these regions led to the

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.

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 /

Advanced route for the synthesis of cPLA2 inhibitors

A process for making a compound of formula (I) in which process the compound HC≡C—(CH2)n—NH2 is reacted with the compound R1—SO2Cl to produce an intermediate compound, which intermediate compound is t

A SYNTHETIC METHODOLOGY FOR THE REDUCTIVE ALKYLATION AT THE C-3 POSITION OF INDOLES

A process for the reductive alkylation at the C-3 position of an indole compound in which the indole is treated with an aldehyde in the presence of a Lewis acid and a silicon hydride reducing agent. The process is useful for alkylating the C-3 position of

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.

Process for the synthesis of cPLA2 inhibitors

A process for making the compound of formula (I) wherein Ac represents acetate; X represents O or CH2; Y represents C1-C6alkyl; and Z is selected from the group consisting of H, halogen, CN, CHO, CF3, OCF3

Process for making an aldehyde

A process for making an aromatic aldehyde in which a sulfoxide is reacted with a dihalogenated aromatic compound in the absence of an effective amount of an activating reagent. The aldehyde may then be used to make other compounds, such as a compound that acts as a cPLA inhibitor.