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Generated: January 21, 2018

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Claims for Patent: 4,188,390

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Summary for Patent: 4,188,390
Title: Antihypertensive 4-amino-2-[4-(1,4-benzodioxan-2-carbonyl) piperazin-1-yl or homopiperazin-1-yl]quinazolines
Abstract:Compounds having the formula ##STR1## and pharmaceutically acceptable salts thereof wherein R represents 6,7-di(lower alkoxy) or 6,7,8-tri(lower alkoxy); m is 1 or 2, X is --CHR.sup.1 -- or --CH.sub.2 CH.sub.2 --; each R.sup.1 and R.sup.0 may be the same or different and is hydrogen or lower alkyl; each of R.sup.2 and R.sup.3 is hydrogen, lower alkoxy, lower alkyl, halogen, lower alkanoyl, lower alkoxycarbonyl, --CONR.sup.4 R.sup.5 or --SO.sub.2 NR.sup.4 R.sup.5 wherein each of R.sup.4 and R.sup.5 is hydrogen or lower alkyl; processes for their preparation; and their use as regulators of the cardiovascular system, and particularly in the treatment of hypertension.
Inventor(s): Campbell; Simon F. (Deal, GB2)
Assignee: Pfizer Inc. (New York, NY)
Application Number:05/952,317
Patent Claims: 1. A compound of the formula ##STR38## wherein (R).sub.n is selected from the group consisting of 6,7-di(lower alkoxy) or 6,7,8-tri(lower alkoxy);

m is 1 or 2;

X is selected from the group consisting of --CHR.sup.1 -- or --CH.sub.2 CH.sub.2 --;

each of R.sup.1 and R.sup.0 is selected from the group consisting of hydrogen or lower alkyl;

and R.sup.2 and R.sup.3, which may the same or different, are selected from the group consisting of hydrogen, lower alkyl, lower alkoxy, halogen, lower alkanoyl, lower alkoxycarbonyl or a group of the formula --CONR.sup.4 R.sup.5 or --SO.sub.2 NR.sup.4 R.sup.5 wherein R.sup.4 and R.sup.5, which may the same or different, are selected from the group consisting of hydrogen or lower alkyl; and the pharmaceutically acceptable acid addition salts thereof.

2. A compound according to claim 1 wherein each of R.sup.0 and R.sup.1 is independently H or CH.sub.3 ; and R.sup.2 and R.sup.3 are each independently hydrogen, lower alkyl, lower alkoxy, halogen, lower alkanoyl, lower alkoxycarbonyl, --CONH.sub.2 or --SO.sub.2 N(CH.sub.3).sub.2.

3. A compound according to claim 2 wherein R.sup.1 is H or CH.sub.3 ;

each of R.sup.2 and R.sup.3 is hydrogen, lower alkyl, lower alkoxy, halogen or lower alkanoyl; (R).sub.n is 6,7-dimethoxy and the pharmaceutically acceptable acid addition salts thereof; said compound having the formula ##STR39##

4. 4-Amino-2-[4-(1,4-benzodioxan-2-carbonyl)piperazin-1-yl]-6,7,8-trimethox y quinazoline, the compound according to claim 2 wherein R.sub.n is 6,7,8-trimethoxy and each of R.sup.0, R.sup.1, R.sup.2 and R.sup.3 is hydrogen.

5. 4-Amino -2-[4-(1,4-benzodioxan-2-carbonyl)piperazin-1-yl]-6,7-dimethoxyquinazoline, the compound according to claim 3 wherein each of R.sup.1, R.sup.2 and R.sup.3 is hydrogen.

6. A pharmaceutical composition comprising a cardiovascular regulating amount of a compound according to claim 1 or a pharmaceutically acceptable acid addition salt thereof together with a pharmaceutically acceptable diluent or carrier.

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