Pharmaceutical compositions of indazoles and methods of use ther

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

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5483601, A61K 31415

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active

054591589

ABSTRACT:
Indazoles of Formula (I) ##STR1## in which R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are each separately selected from hydrogen, halogeno, halogenoalkyl, formyl, carboxy, sulpho, cyano, nitro, COR and .sup.+ NRR'R" groups, wherein R, R' and R" are each separately alkyl, aralkyl or aryl groups, and R.sub.5 is selected from hydrogen, halogeno, halogenoalky, formyl, carboxy, sulpho, cyano, nitro, hydroxy, alkoxy, alkyl, COR, NHCOR and .sup.+ NRR'R" groups, wherein R, R' and R" are each separately alkyl, aralkyl or aryl groups, which may optionally be in the form of a physiologically acceptable ester or salt, are of value for use as an analgesic or in the treatment of any condition where the inhibition of brain/spinal cord nitric oxide synthase is advantageous, for example in neurodegenerative disease.

REFERENCES:
patent: 3843678 (1974-10-01), DiBella
patent: 3988347 (1976-10-01), DiBella
patent: 4051145 (1977-09-01), Dupre et al.
J. of Heterocyclic Chemistry vol. 22, No. 4 Jul.-Aug. 1985, pp. 985-991 Streef et al "Reactivity of some 3-substituted derivatives of 1,6-dihalogenopyridines . . . ".
Chemical Abstracts, vol. 91, No. 7, 1979 No. 56787h, "Rearrangements N-mono--and N,N-disubstituted . . . " Wladyslaw et al.
Biochemical Pharmacology vol. 31, No. 18, 1982, 1982, pp. 3002-3005 Murray "Inhibition . . . heterocycles".
Chemical Abstracts, vol. 102, No. 13, 1985 No. 113361m "Antiallergic activitiy . . . derivatives" Beyer.
Chemical Abstracts, vol. 118, No. 15, Apr. 1993 No. 139709m "7-Nitro indazole . . . blood pressure" Moore.
Chemical Abstracts, vol. 85, No. 7, 1976, 46664c; Floru, "Manufacture of 6-nitroindazole".

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