Claims
- 1. A compound having the structural formula: ##STR42## or a pharmaceutically acceptable salt thereof, wherein: Y is ##STR43## n is 1-8; R.sup.1 is
- (1) hydrogen,
- (2) hydroxy, or
- (3) hydroxymethyl;
- R.sup.2 and R.sup.3 are independently:
- (1) hydrogen,
- (2) halo,
- (3) hydroxy,
- (4) amino,
- (5) di(C.sub.1-5 alkyl)amino,
- (6) mono(C.sub.1-5 alkyl)amino,
- (7) nitro,
- (8) cyano,
- (9) C.sub.1-6 alkyl,
- (10) C.sub.3-8 cycloalkyl,
- (11) C.sub.2-5 alkenyl,
- (12) C.sub.1-4 alkoxy,
- (13) C.sub.1-4 alkylthio,
- (14) C.sub.2-5 alkenyloxy, or
- (15) C.sub.1-5 alkanoyl;
- R.sup.4 and R.sup.5 are independently:
- (1) hydrogen,
- (2) C.sub.1-6 alkyl, either unsubstituted or substituted with:
- (a) hydroxy,
- (b) C.sub.1-4 alkoxy, or ##STR44## wherein X is 0, 1 or 2; R.sup.4 and R.sup.5 are joined together to form a 5 or 6 membered ring with the nitrogen to which they are attached, from the group; morpholino, N-methylpiperazino, pyrrolidino and piperidine;
- R.sup.6 is
- (1) --CN, ##STR45## and R.sup.7 is
- (1) C.sub.1-6 alkyl,
- (2) C.sub.1-4 alkoxy, or
- (3) halo.
- 2. The compound of claim 1 or a pharmaceutically acceptable salt thereof wherein R.sup.1 is hydrogen; R.sup.2 and R.sup.3 are halo, nitro, C.sub.1-5 alkanoyl, hydrogen or cyano; n is 2, and Y is: ##STR46##
- 3. The compound of claim 2, or a pharmaceutically acceptable salt thereof wherein R.sup.1 and R.sup.2 are hydrogen; and R.sup.3 is cyano.
- 4. A pharmaceutical .beta.-blocking composition comprising a pharmaceutically acceptable carrier and an effective .beta.-blocking amount of a compound of formula: ##STR47## or a pharmaceutically acceptable salt thereof, wherein:
- Y is ##STR48## n is 1-8; R.sup.1 is
- (1) hydrogen,
- (2) hydroxy, or
- (3) hydroxymethyl;
- R.sup.2 and R.sup.3 are independently:
- (1) hydrogen,
- (2) halo,
- (3) hydroxy,
- (4) amino,
- (5) di(C.sub.1-5 alkyl)amino,
- (6) mono(C.sub.1-5 alkyl)amino,
- (7) nitro,
- (8) cyano,
- (9) C.sub.1-6 alkyl,
- (10) C.sub.3-8 cycloalkyl,
- (11) C.sub.2-5 alkenyl,
- (12) C.sub.1-4 alkoxy,
- (13) C.sub.1-4 alkylthio,
- (14) C.sub.2-5 alkenyloxy, or
- (15) C.sub.1-5 alkanoyl;
- R.sup.4 and R.sup.5 are independently:
- (1) hydrogen,
- (2) C.sub.1-6 alkyl, either unsubstituted or substituted with:
- (a) hydroxy,
- (b) C.sub.1-4 alkoxy, or
- (c) phenyl;
- R.sup.4 and R.sup.5 are joined together to form a 5 or 6 membered ring with the nitrogen to which they are attached, from the group: morpholino, N-methylpiperazino, pyrrolidino and piperidine;
- R.sup.6 is
- (1) --CN, ##STR49## and R.sup.7 is
- (1) C.sub.1-6 alkyl,
- (2) C.sub.1-4 alkoxy, or
- (3) halo.
- 5. The composition of claim 4 wherein R.sup.1 is hydrogen, R.sup.2 and R.sup.3 are halo, nitro, C.sub.1-5 alkanoyl, hydrogen or cyano, n is 2, and Y is: ##STR50##
- 6. The composition of claim 5, wherein R.sup.1 and R.sup.2 are hydrogen, and R.sup.3 is cyano.
- 7. A method of treating hypertension, angina, arrhythmia, post myocardial infarction and/or elevated intraocular pressure in a patient in need of such treatment which comprises administration of an effective antihypertensive amount of a compound of structural formula: ##STR51## or a pharmaceutically acceptable salt thereof, wherein: Y is ##STR52## n is 1-8; R.sup.1 is
- (1) hydrogen,
- (2) hydroxy, or
- (3) hydroxymethyl;
- R.sup.2 and R.sup.3 are independently:
- (1) hydrogen,
- (2) halo,
- (3) hydroxy,
- (4) amino,
- (5) di(C.sub.1-5 alkyl)amino,
- (6) mono(C.sub.1-5 alkyl)amino,
- (7) nitro,
- (8) cyano,
- (9) C.sub.1-6 alkyl,
- (10) C.sub.3-8 cycloalkyl,
- (11) C.sub.2-5 alkenyl,
- (12) C.sub.1-4 alkoxy,
- (13) C.sub.1-4 alkylthio,
- (14) C.sub.2-5 alkenyloxy, or
- (15) C.sub.1-5 alkanoyl;
- R.sup.4 and R.sup.5 are independently:
- (1) hydrogen,
- (2) C.sub.1-6 alkyl, either unsubstituted or substituted with:
- (a) hydroxy,
- (b) C.sub.1-4 alkoxy, or
- (c) phenyl; ##STR53## wherein X is 0, 1 or 2; R.sup.4 and R.sup.5 are joined together to form a 5 or 6 membered ring with the nitrogen to which they are attached, from the group: morpholino, N-methylpiperazino, pyrrolidino and piperidine;
- R.sup.6 is
- (1) --CN, ##STR54## and R.sup.7 is
- (1) C.sub.1-6 alkyl,
- (2) C.sub.1-4 alkoxy, or
- (3) halo.
- 8. The method of claim 7 wherein R.sup.1 is hydrogen R.sup.2 and R.sup.3 are hydrogen, halo, nitro, C.sub.1-5 alkanoyl, or cyano; n is 2, and Y is: ##STR55##
- 9. The method of claim 8 wherein R.sup.1 and R.sup.2 are hydrogen, and R.sup.3 is cyano.
Parent Case Info
This is a division of application Ser. No. 838,851 filed Mar. 12, 1986 which is a division of application Ser. No. 596,200 filed Apr. 2, 1984 now U.S. Pat. No. 4,593,039.
US Referenced Citations (1)
Number |
Name |
Date |
Kind |
4131685 |
Smith |
Dec 1978 |
|
Non-Patent Literature Citations (1)
Entry |
Wolff, Burger's Medicinal Chemistry, 4th Ed., Part III, pp. 310 and 311. |
Divisions (2)
|
Number |
Date |
Country |
Parent |
838851 |
Mar 1986 |
|
Parent |
596200 |
Apr 1984 |
|