Claims for Patent: 4,188,390

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 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 -CHR1- or -CH2CH2-; each R1 and R0 may be the same or different and is hydrogen or lower alkyl; each of R2 and R3 is hydrogen, lower alkoxy, lower alkyl, halogen, lower alkanoyl, lower alkoxycarbonyl, -CONR4R5 or -SO2NR4R5 wherein each of R4 and R5 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):	Simon F. Campbell
Assignee:	Pfizer Corp SRL
Application Number:	US05/952,317
Patent Claims:	1. A compound of the formula ##STR38## wherein (R)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 --CHR1 -- or --CH2 CH2 --; each of R1 and R0 is selected from the group consisting of hydrogen or lower alkyl; and R2 and R3, 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 --CONR4 R5 or --SO2 NR4 R5 wherein R4 and R5, 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 R0 and R1 is independently H or CH3 ; and R2 and R3 are each independently hydrogen, lower alkyl, lower alkoxy, halogen, lower alkanoyl, lower alkoxycarbonyl, --CONH2 or --SO2 N(CH3)2. 3. A compound according to claim 2 wherein R1 is H or CH3 ;each of R2 and R3 is hydrogen, lower alkyl, lower alkoxy, halogen or lower alkanoyl; (R)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-trimethoxyquinazoline, the compound according to claim 2 wherein Rn is 6,7,8-trimethoxy and each of R0, R1, R2 and R3 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 R1, R2 and R3 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.