104436-76-2

Upstream product

• 3556-60-3 3-methoxy-4-methylcyano-benzene 
• 7151-68-0 3-methoxy-p-toluic acid 
• 104436-77-3 sodium 6-nitroindazolide 
• 104436-60-4 4-bromomethyl-3-methoxybenzonitrile 

Downstream Products

• 104436-79-5 {1-[2-Methoxy-4-(1H-tetrazol-5-yl)-benzyl]-1H-indazol-6-yl}-carbamic acid cyclopentyl ester 
• 104436-75-1 6-(butyloxycarbonyl)amino-1-(2-methoxy-4-[1(H)-tetrazol-5-yl]benzyl)indazole 
• 104436-74-0 6-amino-1-<2-methoxy-4-(1H-tetrazol-5-yl)benzyl>indazole 
• 104436-78-4 1-<2-methoxy-4-(1H-tetrazol-5-yl)benzyl>-6-nitroindazole 

Relevant academic research and scientific papers

Indazole compounds, pharmaceutical compositions and use

The invention provides a series of novel heterocyclic amides of the formula I in which the group A CRa can be --CRb=CRa--, --CHRb--CHRa-- or --N=CRa--, the amidic group Re.L can be Re.X.CO.NH, Re.X.CS.NH or Re.NH.CO attached at position 4, 5 or 6 of the benzenoid moiety, Z is an acid group selected from the group consisting of carboxy, an acylsulphonamide residue of the formula CO.NH.SOn Rg and a tetrazolyl residue of the formula II, and the radicals Ra, Rb, Rc, Rd, Re, Rf, Rg, Rh, n, X, G1, Q and G2 have the meanings defined in the following specification. The compounds of formula I are leukotriene antagonists. The invention also provides pharmaceutically acceptable salts of the formula I compounds; pharmaceutical compositions containing the formula I compounds, or their salts, for use in the treatment of, for example, allergic or inflammatory diseases, or endotoxic or traumatic shock conditions; and processes for the manufacture of the formula I compounds, as well as intermediates for use in such manufacture.

A novel series of selective leukotriene antagonists: Exploration and optimization of the acidic region in 1,6-disubstituted indoles and indazoles

A systematic structure-activity exploration of the carboxylic acid region in a series of indole- or indazole-derived leukotriene antagonists 1 led to several discoveries. Use of the 3-methoxy-p-tolyl fragment (illustrated in acid 1) for connecting the indole and the acidic site provides the most potent carboxylic acids 1, tetrazoles 20, and aryl sulfonimides 21. The aryl sulfonimides are 5-500 times more potent (in vitro and/or in vivo) than the corresponding carboxylic acids 1. The o-tolyl sulfonimides such as 114 show greater oral potency than the phenyl sulfonimides at a given level of in vitro activity. Acidic keto sulfone derivatives 10 (Nu = CH(CO2CH3)SO2Ph) mimic the activity of the sulfonimides.