GB1194548A - Improvements in Compositions Comprising beta-Adrenolytics - Google Patents

Abstract

1,194,548. #-adrenolytic compositions. BOEHRINGER INGELHEIM G.m.b.H. 24 Nov., 1967 [25 Nov., 1966, 5 Sept., 1967], No. 53550/ 67. Heading A5B. Compositions for treating angina pectoris comprise a #-andrenolytic and a coronary dilator of the general formula: in which R 1 is an amino group substituted by two mono- or dihydroxylower (C 1-6 ) alkyl groups or by two lower acyloxylower alkyl groups; a morpholino, pyrrolidin-l-yl, piperazin-1-yl; 1, 2, 5, 6-tetrahydropyrid-1-yl or piperidino group, optionally substituted by one or two lower alkyl or hydroxy groups; or a lower alkyl or alkylamino group, an amino group substituted by lower alkyl or hydroxy lower alkyl group or an amino group substituted by an aryl lower alkyl group and a hydroxy lower alkyl group; R 2 is piperidino, 1, 2, 5, 6-tetrahydropyrid-1-yl, morpholino, piperazin-1-yl or pyrrolidin-1-yl group optionally substituted by one or two lower alkyl or hydroxy groups, a lower alkoxy or alkylthio group, an amino group substituted by two mono- or dihydroxy lower alkyl groups or by two lower acyloxy lower alkyl groups; or an amino group substituted by a lower alkyl group and a hydroxy lower alkyl group or by an aryl lower alkyl group and a hydroxy lower alkyl group; and A is -N=C(R 3 )-N=CR 4 )- or -N =C(R 3 )-C(R 4 )=N- or -S(CH 2 ) n - or -S(CH 2 ) n - where R 3 is an amino group substi- # O tuted by two mono or dihydroxy lower alkyl groups or by two lower acyloxyl lower alkyl groups; or a phenyl, thienyl or furyl group carrying one or more halogen atoms or lower alkyl groups, R 4 has the same meanings as R 1 and R 2 and n is 2 or 3. Preferred #-adrenolytics are those of the formula ArO-CH 2 -CHOHCH 2 NHR in which Ar is phenyl, naphthyl, tetrahydronaphthyl or indaryl, optionally substituted with one or more lower alkyl groups, -OF 3 , -NH 2 , -CN, halogen atoms, lower alkoxy, alkenyloxy, alkynyloxy, acyloxy, acyl, alkoxyalkyl, alkenyl, alkynyl, alkylthio or mono or dialkylamino groups or -NO 2 , -OH or -O-CH 2 -O- groups; and R is a C 1-6 alkyl group or a C 7-10 aralkyl group, and the compounds 1-(4-methanesulphonamidophenyl)-1- hydroxy-2-isopropylaminoethane and 1-(4-nitrophenyl)-1-hydroxy-2-isopropylaminoethane The compositions may be in conventional (forms for oral, parenteral and rectal administration comprising the active constituents (preferably as acid addition salts) and conventional excipients.