| abstract |
1399283 Histamine receptor inhibitors SMITH KLINE & FRENCH LABORATORIES Ltd 19 April 1973 [20 April 1972] 18301/72 Heading A5B A pharmaceutical composition having H-1 and H-2 histamine-receptor-inhibiting activity comprises (I) an antihistamine, (II) an H-*2 receptor inhibitor and (III) a pharmaceutically acceptable diluent or carrier, the H-2 receptor inhibitor being selected from: (a) thioureas of formula: wherein A together with the attached carbon and nitrogen atoms represents a basic heterocycle, X is H, C 1-4 alkyl, halogen or C 1-4 alkylthio, n is 3-6 and R is H, C 1-4 alkyl, aroyl, substituted aroyl, aralkyl or substituted aralkyl but not benzyl, (b) amidines of formula: wherein A together with the attached carbon and nitrogen atoms represents a basic heterocycle of 5 or 6 atoms, X is H, OH, CF 3 , amino, halogen, C 1-4 alkyl or C 1-4 alkylthio, n is 2-5, R 1 is C 1-4 alkyl, phenyl, substituted phenyl, aralkyl, alkylthioalkyl, -NHR 3 or SR 4 , R 2 is H, C 1-4 alkyl, aryl or aralkyl or (when R 1 is -NHR 3 ) CN or NO 2 , R 3 is H, CH 3 , aralkyl or amino or together with R 2 and the -N=C-NH- grouping represents a 5- membered ring, R 4 is C 1-6 alkyl, C 1-6 alkenyl or (CH 2 ) m Z or together with the -NH-C= NR 2 grouping represents a 5-membered ring, m is 1-3 and Z is aryl, substituted aryl, hydroxy, alkylamino, cyano, carboxy or aryloxy, (c) isothioureas of formula: wherein A together with the carbon and nitrogen atoms represents a basic 5- or 6-membered hetero-cycle, X is H, halogen or methyl, n is 2-4, R 1 is H or C 1-4 alkyl, R 2 is H, C 1-4 alkyl, amino or aralkyl or R 1 and R 2 together represent ethylene, (d) amidines of formula: wherein n is 3 or 4 and (e) pharmaceutically acceptable salts thereof. Many compounds are specified.n[GB1399283A] |