Anti-hypertensive compounds of formula (I): ##STR## wherein: one of R 1 and R 2 is nitro, cyano or C 1-3 alkylcarbonyl, and the other is methoxy or amino optionally substituted by one or two C 1-6 alkyl or by C 2-7 alkanoyl; one of R 3 and R 4 is hydrogen or C 1-4 alkyl and the other is C 1-4 alky
Anti-hypertensive compounds of formula (I): ##STR## wherein: one of R 1 and R 2 is nitro, cyano or C 1-3 alkylcarbonyl, and the other is methoxy or amino optionally substituted by one or two C 1-6 alkyl or by C 2-7 alkanoyl; one of R 3 and R 4 is hydrogen or C 1-4 alkyl and the other is C 1-4 alkyl, or R 3 and R 4 together with the carbon atom to which they are attached are C 3-6 spiroalkyl; R 5 is hydrogen, C 1-3 alkyl or C 1-8 acyl; and n is 1 or 2; the lactam group being trans to the OR 5 group; or, when the other of R 1 and R 2 is amino, a pharmaceutically acceptable salt thereof.
대표청구항▼
1. A compound of formula (I): ##STR## wherein: one of R 1 and R 2 is nitro, cyano or C 1-3 alkylcarbonyl, and the other is methoxy or amino optionally substituted by one or two C 1-6 alkyl or by C 2-7 alkanoyl; one of R 3 and R 4 is hydrogen or C 1-4 alkyl and the other is C 1-4 alkyl, or R 3 and
1. A compound of formula (I): ##STR## wherein: one of R 1 and R 2 is nitro, cyano or C 1-3 alkylcarbonyl, and the other is methoxy or amino optionally substituted by one or two C 1-6 alkyl or by C 2-7 alkanoyl; one of R 3 and R 4 is hydrogen or C 1-4 alkyl and the other is C 1-4 alkyl, or R 3 and R 4 together with the carbon atom to which they are attached are C 3-6 spiroalkyl; R 5 is hydrogen, C 1-3 alkyl or C 1-8 carboxylic acyl; and n is 1 or 2; the lactam group being trans to the OR 5 group; or, when the other of R 1 and R 2 is amino, a pharmaceutically acceptable salt thereof. 2. A compound according to claim 1, wherein one of R 1 and R 2 is nitro or cyano. 3. A compound according to claim 2, wherein the other of R 1 and R 2 is amino optionally substituted by one or two C 1-6 alkyl or by C 2-7 alkanoyl. 4. A compound according to claim 3, wherein the other of R 1 and R 2 is amino, methylamino, dimethylamino or acetylamino. 5. A compound according to claim 1, wherein R 3 and R 4 are both C 1-4 alkyl. 6. A compound according to claim 1, wherein R 5 is hydrogen. 7. 6-Acetamido-7-nitro-3,4-dihydro-trans-4-(2-ketopyrrolidinyl)-2,2-dimethyl-2H-benzo[b]pyran-3-ol; or 6-amino-7-nitro-3,4-dihydro-trans-4-(2-ketopyrrolidinyl)-2,2-dimethyl-2H-benzo[b]pyran-3-ol or a pharmaceutically acceptable salt thereof. 8. 6-Nitro-7-acetamido-3,4-dihydro-trans-4-(2-ketopyrrolidinyl)-2,2-dimethyl-2H-benzo[b]pyran-3-ol; or 6-nitro-7-amino-3,4-dihydro-trans-4-(2-ketopyrrolidinyl)-2,2-dimethyl-2H-benzo[b]pyran-3-ol or a pharmaceutically acceptable salt thereof; or 6-cyano-7-amino-3,4-dihydro-trans-4-(2-ketopyrrolidinyl)-2,2-dimethyl-2H-benzo[b]pyran-3-ol or a pharmaceutically acceptable salt thereof. 9. A compound according to claim 1, wherein it is in a substantially pure form. 10. A pharmaceutical composition for the treatment of hypertension, which comprises an anti-hypertensive effective amount of a compound according to claim 1, and a pharmaceutically acceptable carrier. 11. A method of treating hypertension in a mammal including a human, which comprises administering to the suffering mammal an anti-hypertensive effective amount of a compound according to claim 1.
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이 특허에 인용된 특허 (7)
Evans John M. (Roydon GB2) Showell Graham A. (Harlow GB2) Fake Charles S. (Harlow GB2), Anti-hypertensive chromanol derivatives.
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