Claims
- 1. A compound of formula (I): ##STR26## wherein: n is 1 or 2;
- R.sub.1 is chloro, bromo, C.sub.1-6 alkylcarbonyl or cyano;
- one of R.sub.3 and R.sub.4 is hydrogen or C.sub.1-4 alkyl and the other is C.sub.1-4 alkyl or R.sub.3 and R.sub.4 together are C.sub.2-5 polymethylene;
- and either;
- R.sub.5 is hydroxy, C.sub.1-3 alkoxy or C.sub.1-8 acyloxy; and
- R.sub.2 is hydrogen and the cyclic amide moiety and R.sub.5 are trans; or R.sub.5 and R.sub.2 together form a bond.
- 2. A compound according to claim 1, wherein R.sub.3 and R.sub.4 are both methyl.
- 3. A compound according to claim 1 of formula (III): ##STR27## wherein R.sub.1 and n are as defined in formula (I).
- 4. A compound according to claim 1, wherein n is 1.
- 5. A compound according to claim 1, wherein R.sub.1 is chloro, bromo, acetyl or cyano.
- 6. 6-Bromo-2,2-dimethyl-4-(2-oxo-1-pyrrolidinyl)-1,2-dihydroquinoline,
- 6-cyano-2,2-dimethyl-4-(2-oxo-1-pyrrolidinyl)-1,2-dihydroquinoline,
- trans-2,2-dimethyl-6-cyano-4-(2-oxo-1-pyrrolidinyl)-1,2,3,4-tetrahydroquinolin-3-ol,
- trans-2,2-dimethyl-6-chloro-4-(2-oxo-1-pyrrolidinyl)-1,2,3,4-tetrahydroquinolin-3-ol,
- 6-chloro-2,2-dimethyl-4-(2-oxo-1-pyrrolidinyl)-1,2-dihydroquinoline or
- trans-2,2-dimethyl-6-bromo-4-(2-oxo-1-pyrrolidinyl)-1,2,3,4-tetrahydroquinolin-3-ol.
- 7. Trans-2,2-Dimethyl-6-bromo-4-(2-oxo-1-pyrrolidinyl)-1,2,3,4-tetrahydroquinolin-3-ol.
- 8. An anti-hypertensive pharmaceutical composition comprising an anti-hypertensive effective amount of a compound according to claim 1 and a pharmaceutically acceptable carrier.
- 9. A method of treating hypertension in mammals including man, which comprises administering to the suffering mammal an anti-hypertensive effective amount of a compound according to claim 1.
- 10. A pharmaceutical composition for the treatment and/or prophylaxis of cerebrovascular disorders and/or disorders associated with cerebral senility in mammals, such as humans, comprising an effective and/or prophylactic amount of a compound according to claim 1 and a pharmaceutically acceptable carrier.
- 11. A method for the treatment and/or prophylaxis of cerebrovascular disorders and/or disorders associated with cerebral senility in mammals, such as humans, which comprises administering to the mammal in need of such treatment and/or prophylaxis an effective and/or prophylactic amount of a compound according to claim 1.
- 12. A method according to claim 11, wherein n is 1.
- 13. A method according to claim 11, wherein R.sub.1 is chloro, bromo or cyano.
- 14. A method according to claim 11, wherein R.sub.3 and R.sub.4 are both methyl.
- 15. A method according to claim 11, wherein R.sub.2 and R.sub.5 together form a bond.
- 16. A method according to claim 11, wherein R.sub.2 is hydrogen and R.sub.5 is hydroxy.
- 17. A method according to claim 11, wherein the compound of formula (I) is 6-bromo-2,2-dimethyl-4-(2-oxo-1-pyrrolidinyl)-1,2-dihydroquinoline,
- 6-cyano-2,2-dimethyl-4-(2-oxo-1-pyrolidinyl)-1,2-dihydroquinoline,
- trans-2,2-dimethyl-6-cyano-4-(2-oxo-1-pyrrolidinyl)-1,2,3,4-tetrahydroquinolin-3-ol,
- trans-2,2-dimethyl-6-chloro-4-(2-oxo-1-pyrrolidinyl)-1,2,3,4-tetrahudroquinolin-3-ol,
- 6-chloro-2,2-dimethyl-4-(2-oxo-1-pyrrolidinyl)-1,2-dihydroquinoline or
- trans-2,2-dimethyl-6-bromo-4-(2-oxo-1-pyrrolidinyl)-1,2,3,4-tetrahydroquinolin-3-ol.
- 18. A method according to claim 11, wherein the compound of formula (I) is 6-bromo-2,2-dimethyl-4-(2-oxo-1-pyrrolidinyl)-1,2-dihydroquinoline or 6-cyano-2,2-dimethyl-4-(2-oxo-1-pyrrolidinyl)-1,2-dihydroquinoline.
Priority Claims (5)
Number |
Date |
Country |
Kind |
8320184 |
Jul 1983 |
GBX |
|
8334415 |
Dec 1983 |
GBX |
|
PCT/GB84/00252 |
Jul 1984 |
WOX |
|
8519306 |
Jul 1985 |
GBX |
|
8527994 |
Nov 1985 |
GBX |
|
Parent Case Info
The present invention is a continuation-in-part of U.S. patent application Ser. No. 717,177, filed Mar. 25, 1985 now abandoned, which is incorporated herein by reference thereto.
US Referenced Citations (4)
Non-Patent Literature Citations (1)
Entry |
Bentue-Ferrer et al., Experimental Aging Research, 11, 137-141 (1985). |
Continuation in Parts (1)
|
Number |
Date |
Country |
Parent |
717177 |
Mar 1985 |
|