Alkene, alkyne or cycloalkylene derivatives

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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514242, 514258, 514259, 514261, 514274, 514297, 514312, 514347, 514365, 514383, 514385, 514438, 514576, 544265, 544280, 544283, 544315, 544318, 544319, 546103, 546152, 546153, 546157, 546172, 546276, 546280, 548182, 548186, 548263, 548337, 549 78, 549 79, 564162, 564221, 568 18, 568 27, 568 28, 568308, 568715, 568775, 568807, A61K 3153, A61K 31185, C07D47300, C07C25500

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active

050325922

ABSTRACT:
A compound of the formula ##STR1## wherein X has the formula ##STR2## wherein ring a is phenyl, naphthyl or heterocyclic; wherein R.sup.1 is hydrogen, alkyl, alkanoyl or aroyl; wherein R.sup.2, R.sup.3 and R.sup.4, which may be the same or different, each is an electron withdrawing substituent selected from halogeno, nitro, cyano, trifluoromethyl, alkylthio, alkylsulphinyl, and alkylsulphonyl or each is hydrogen, alkyl, alkoxy or dialkylamino provided that when ring A is phenyl or naphthyl at least one of R.sup.2, R.sup.3 and R.sup.4 is an electron-withdrawing substituent; wherein R.sup.5 and R.sup.6, which may be the same or different, each is hydrogen, halogeno or alkyl; wherein R.sup.7 is alkyl or halogenoalkyl; and wherein R.sup.8 is carbamoyl, alkyl, cycloalkyl, alkenyl, alkynyl, halogenoalkyl, halogenoalkenyl, halogenoalkynyl, alkanoyl, alkylcarbamoyl, dialkylcarbamoyl or aroyl; or wherein R.sup.8 is alkyl or alkenyl which bears one or more substituents selected from cyano, carbamoyl, amino, hydroxy, alkanoyl, alkoxy, alkylthio, alkenylthio, alkylsulphinyl, alkenylsulphinyl, alkylsulphonyl, alkenylsulphonyl, alkanoylamino, alkoxycarbonylamino, alkylsulphonamido, alkylamino, dialkylamino, dialkylsulphamoyl, aroyl, aryl, arylthio, arylsulphinyl, arylsulphonyl, heterocyclylthio, heterocyclylsulphinyl and heterocyclylsulphonyl; or wherein R.sup.8 has the formula ##STR3## wherein ring B is phenyl, naphthyl or heterocyclyl and wherein R.sup.2, R.sup.3 and R.sup.4 have any of the meanings stated above, provided that when R.sup.7 is methyl R.sup.8 is not also methyl.

REFERENCES:
patent: 3979471 (1976-09-01), Julia
patent: 4139561 (1979-02-01), Onopchenko et al.
patent: 4191775 (1980-03-01), Glen
patent: 4282218 (1981-08-01), Glen et al.
patent: 4329776 (1980-12-01), Glen et al.
patent: 4386080 (1983-05-01), Crossley et al.
patent: 4507140 (1985-03-01), Sugavanam
patent: 4532341 (1985-07-01), Holmwood et al.
Reddy et al, Synthesis, Oct. 1980, pp. 815-817.

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