Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1988-07-13
1990-09-18
Hollrah, Glennon H.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
5482666, C07D24908, A61K 3141
Patent
active
049579347
ABSTRACT:
A 2-propanol derivative of the formula I, wherein R.sup.1 and R.sup.5, which may be the same or different, are each a triazolyl, imidazolyl, pyridyl or pyrimidinyl radical; R.sup.2, R.sup.3 and R.sup.4, which may be the same or different, are each a hydrogen atom, a 1-6C alkyl, halogenoalkyl or alkoxy radical, a 3-8C cycloalkyl radical, or a phenyl, naphthyl, phenoxy, naphthyloxy or phenyl (1-6C alkyl) radical, in each of which the aryl group optionally bears one or more substituents selected from halogen atoms, amino, carboxamido, cyano and nitro radicals, 1-6C alkyl, halogenoalkyl, alkoxy, halogenoalkoxy and alkylamino radicals, 3-8C cycloalkyl radicals, di(1-6C alkyl)amino radicals and 2-6C alkoxycarbonyl radicals; R.sup.6 is a phenyl or naphthyl radical optionally bearing one or more substituents as defined above; X is a direct bond, an alkylene, alkenylene or alkynylene radical, or an oxyalkylene or thioalkylene radical wherein respectively the oxygen or sulphur atom is bonded to R.sup.6 or a phenylalkylene radical in which the phenyl group bears one or more substituents as defined above for R.sup.6 ; and Y is a hydrogen or halogen atom, a hydroxy, cyano or carbamoyl radical, or a phenyl(1-6C alkoxy) radical in which the phenyl group bears one or more substituents as defined above for R.sup.6 ; provided that, when Y is a cyano or carbamoyl radical, neither R.sup.2, R.sup.3 nor R.sup.4 may be an alkoxy or aryloxy radical, and either R.sup.2 is a hydrogen atom, or R.sup.3 and R.sup.4 are both hydrogen atoms; and provided that, when R.sup.1 and R.sup.5 are each a 1,2,4-triazol-1-yl radical, R.sup.2 is hydrogen and Y is a hydroxy radical, R.sup.3 and R.sup.4 may not be hydrogen or methyl when X is a direct bond, and R.sup.3 and R.sup.4 may not be hydrogen when X is a methylene radical; and for those compounds which contain a basic nitrogen atom, the pharmaceutically acceptable acid additon salts thereof.
REFERENCES:
patent: 4602025 (1986-07-01), Hirsch et al.
Taylor et al.: "Aromatase Inhibition by 5-Substituted Pyrimidines and Dihydropyrimidines", Chemical Abstracts, vol. 107, No. 11, Sep. 14, 1987, p. 688, col. 1, Abstract No. 96 674z, Columbus, Ohio.
Hollrah Glennon H.
Imperial Chemical Industries plc
Morris Patricia L.
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