Claims
- 1. A compound of formula (I): ##STR31## wherein: either one of R.sub.1 and R.sub.2 is hydrogen and the other is selected from the class of C.sub.1-6 alkylcarbonyl, C.sub.1-6 alkoxycarbonyl, C.sub.1-6 alkylcarbonyloxy, C.sub.1-6 alkylhydroxymethyl, nitro, cyano, chloro, trifluoromethyl, C.sub.1-6 alkylsulphinyl, C.sub.1-6 alkylsulphonyl, C.sub.1-6 alkoxysulphinyl, C.sub.1-6 alkoxysulphonyl, C.sub.1-6 alkylcarbonylamino, C.sub.1-6 alkoxycarbonylamino, C.sub.1-6 alkyl-thiocarbonyl, C.sub.1-6 alkoxy-thiocarbonyl, C.sub.1-6 alkyl-thiocarbonyloxy, C.sub.1-6 alkyl-thiolmethyl, formyl or aminosulphinyl, aminosulphonyl or aminocarbonyl, the amino moiety being optionally substituted by one or two C.sub.1-6 alkyl groups, or C.sub.1-6 alkylsulphinylamino, C.sub.1-6 alkylsulphonylamino C.sub.1-6 alkoxysulphinylamino or C.sub.1-6 alkoxysulphonylamino or ethylenyl terminally substituted by C.sub.1-6 alkylcarbonyl, nitro or cyano, or --C(C.sub.1-6 alkyl)NOH or --C(C.sub.1-6 alkyl)NNH.sub.2, or one of R.sub.1 and R.sub.2 is nitro, cyano or C.sub.1-3 alkylcarbonyl and the other is methoxy or amino optionlly substituted by one or two C.sub.1-6 alkyl or by C.sub.2-7 alkanoyl;
- one or 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 are C.sub.2-5 polymethylene;
- either R.sub.5 is hydroxy, C.sub.1-6 alkoxy or C.sub.2-7 carboxylic acyloxy and R.sub.6 is hydrogen or R.sub.5 and R.sub.6 together are a bond;
- R.sub.7 is C.sub.1-2 alkyl substituted by hydroxy, C.sub.1-6 alkoxy, C.sub.1-6 alkoxycarbonyl, carboxy, or halogen;
- R.sub.8 is hydrogen or C.sub.1-6 alkyl; and
- X is oxygen or sulphur; the R.sub.8 --N--CX--R.sub.7 group being trans to the R.sub.5 group when R.sub.5 and R.sub.6 together are not a bond; or, when one or the other of R.sub.1 and R.sub.2 is an amino or an amino-containing group, a pharmaceutically acceptable salt thereof.
- 2. A compound according to claim 1, wherein one of R.sub.1 and R.sub.2 is hydrogen, the other is selected from the class of C.sub.1-6 alkylcarbonyl, C.sub.1-6 alkoxycarbonyl, C.sub.1-6 alkylcarbonyloxy, C.sub.1-6 alkylhydroxymethyl, nitro or cyano.
- 3. A compound according to claim 2, wherein R.sub.2 is hydrogen.
- 4. A compound according to claim 1, wherein one of R.sub.1 and R.sub.2 is nitro, cyano or C.sub.1-3 alkylcarbonyl and the other is amino optionally substituted by one or two C.sub.1-6 alkyl or by C.sub.2-7 alkanoyl.
- 5. A compound according to claim 4, wherein one of R.sub.1 and R.sub.2 is nitro or cyano and the other is amino.
- 6. A compound according to claim 4, wherein R.sub.1 is nitro, cyano or C.sub.1-3 alkylcarbonyl.
- 7. A compound according to claim 1, wherein the alkyl groups or alkyl moieties of alkyl-containing groups for R.sub.1 or R.sub.2 are methyl or ethyl.
- 8. A compound according to claim 1, wherein R.sub.3 and R.sub.4 are both C.sub.1-4 alkyl.
- 9. A compound according to claim 8, wherein R.sub.3 and R.sub.4 are both methyl.
- 10. A compound according to claim 1, wherein R.sub.5 is hydroxy or unsubstituted C.sub.2-7 carboxylic acyloxy and R.sub.6 is hydrogen.
- 11. A compound according to claim 1, wherein R.sub.5 and R.sub.6 together are a bond.
- 12. A compound according to claim 1, wherein R.sub.7 is methyl or ethyl terminally substituted by hydroxy, methoxy, ethoxy, methoxycarbonyl, ethoxycarbonyl or carboxy.
- 13. A compound according to claim 1, wherein R.sub.7 is methyl or ethyl terminally substituted by chloro or bromo.
- 14. A compound according to claim 1, wherein R.sub.8 is hydrogen or methyl.
- 15. A compound according to claim 14, wherein R.sub.8 is hydrogen.
- 16. Trans-4-chloroacetylamino-6-cyano-3,4-dihydro-2,2-dimethyl-2H-benzo[b]pyran-3-ol; or trans-4-methoxyacetylamino-6-cyano-3,4-dihydro-2,2-dimethyl-2H-benzo[b]pyran-3-ol.
- 17. A compound according to claim 1, in substantially pure form.
- 18. A pharmaceutical composition for the treatment of hypertension in mammals, including man, which comprises an effective amount of a compound of formula (I), as defined in claim 1, and a pharmaceutically acceptable carrier.
- 19. A method of treating hypertension in mammals including man, which comprises administering to the hypertensive mammal an anti-hypertensive effective amount of a compound of formula (I), as defined in claim 1.
Priority Claims (2)
Number |
Date |
Country |
Kind |
8214821 |
May 1982 |
GBX |
|
8301088 |
Jan 1983 |
GBX |
|
CROSS REFERENCE
This is a division of Ser. No. 496,174 filed May 10, 1983 now U.S. Pat. No. 4,481,214.
US Referenced Citations (11)
Foreign Referenced Citations (1)
Number |
Date |
Country |
46652 |
Mar 1982 |
EPX |
Non-Patent Literature Citations (1)
Entry |
Lap et al., Aust. J. Chem. 1979, 32, pp. 619-636. |
Divisions (1)
|
Number |
Date |
Country |
Parent |
496174 |
May 1983 |
|