4-substituted-N-(piperidinyl or pyrrolidinyl)alkyl benzenesulfon

Details 4-substituted-N-(piperidinyl or pyrrolidinyl)alkyl benzenesulfon 4-substituted-N-(piperidinyl or pyrrolidinyl)alkyl benzenesulfon

1986-10-09

1988-03-29

Daus, Donald G.

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

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

546232, C07D20709, C07D21128

Patent

active

047345101

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: 4396622 (1983-08-01), Jozic
patent: 4640920 (1987-02-01), Boyle et al.

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