Abstract Novel quinazoline and cinnoline derivatives having the formula ##STR1## (wherein one of A and B is CH and the other one of A and B is N; X 1 is halogen or CF 3 and X 3 is one of the groups II, III, IV or V ##STR2## where Q is lower alkylene; R 1 is hydrogen or lower alkyl; R 2 and R 3 are independently lower alkyl or R 2 and R 3 are a divalent radical such that HNR 2 R 3 is a secondary cyclic amine with 5 to 7 ring atoms; R 4 is lower alkyl; n is 0 or 1; the rings shown in formulae III and IV are piperidine or pyrrolidine optionally substituted by lower alkyl; and the ring shown in formula V is piperazine optionally substituted by lower alkyl) and their pharmaceutically acceptable salts are useful as pharmaceuticals particularly as anti-hypertensives. Novel intermediates are also described including the corresponding sulphonic acids of formula I ( (where A, B and X 1 are defined above and X 3 is OH).
A compound having the formula: ##STR24## and the pharmaceutically acceptable salts thereof, wherein X 1 is selected from halogen and trifluoromethyl; X 4 is selected from --OH and --NR 1 R 5 ; R 1 is selected from hydrogen and lower alkyl; R 5 is selected from hydrogen and a group having the formula --Q--Z; Q represents lower alkylene; one of A and B is CH whilst the other one of A and B is N; and Z is a halogen atom or C 1 -C 6 alkanesulphonyloxy, or substituted or unsubstituted benzenesulphonyloxy.
Claim 2
Dependent Claim
93 words
A compound having the formula: ##STR24## and the pharmaceutically acceptable salts thereof, wherein X 1 is selected from halogen and trifluoromethyl; X 4 is selected from --OH and --NR 1 R 5 ; R 1 is selected from hydrogen and lower alkyl; R 5 is selected from hydrogen and a group having the formula --Q--Z; Q represents lower alkylene; one of A and B is CH whilst the other one of A and B is N; and Z is a halogen atom or C 1 -C 6 alkanesulphonyloxy, or substituted or unsubstituted benzenesulphonyloxy.