4-quinazolinylamino and 4-cinnolinylamino benzenesulphonic acids

Details 4-quinazolinylamino and 4-cinnolinylamino benzenesulphonic acids 4-quinazolinylamino and 4-cinnolinylamino benzenesulphonic acids

1988-01-06

1989-02-28

Daus, Donald G.

Organic compounds -- part of the class 532-570 series

Organic compounds

Four or more ring nitrogens in the bicyclo ring system

544293, C07D23728, C07D23994

Patent

active

048087157

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.sub.1 is halogen or CF.sub.3 and X.sub.3 is one of the groups II, III, IV or V ##STR2## where Q is lower alkylene; R.sub.1 is hydrogen or lower alkyl; R.sub.2 and R.sub.3 are independently lower alkyl or R.sub.2 and R.sub.3 are a divalent radical such that HNR.sub.2 R.sub.3 is a secondary cyclic amine with 5 to 7 ring atoms; R.sub.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.sub.1 are defined above and X.sub.3 is OH).

REFERENCES:
patent: 3933829 (1976-01-01), Archibald et al.
patent: 4684657 (1987-08-01), Boyle

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