| 摘要 |
<p>Cyclic lactams of formula (I), where R is hydrogen or C1 to C6-alkyl; X is oxygen or bivalent sulfur; Y is hydrogen or C1 to C6-alkyl; or -XY taken together represents hydrogen or C1 to C6-alkyl; or -XY is part of a double bond between the 5- and 6-position carbon atoms of the ring when R2 is also part of that double bond; R1 is hydrogen or C1 to C6-alkyl; R2 is part of the double bond between the 5- and 6-position lactam ring carbon atoms when -XY is also part of that same double bond and R3 is hydrogen, C1 to C6-alkyl or phenyl, or R2 and R3 are independently selected from the group consisting of hydrogen, C1 to C6-alkyl or phenyl; R4 and R5 are independently selected from the group consisting of hydrogen, C1 to C6-alkyl or phenyl, and when one of R4 and R5 is phenyl, the other is hydrogen; or R4 and R5 are taken together with the carbon to which they are bonded to complete a spiro-cycloalkyl ring having from 4 to 6 methylene carbon atoms; R6 and R7 are independently hydrogen, C1 to C6-alkyl or phenyl, and when one of R6 and R7 is phenyl, the other is hydrogen, and wherein R3 and R6 can be taken together to form a -(CH2)n-bridge ring forming connections where n is 2 or 3 across the lactam ring; provided that (I) when -XY and R2 form a double bond between the ring carbon atoms in the 5- and 6-positions, R1 is hydrogen and R3 is hydrogen, C1 to C6-alkyl or phenyl, (II) when X is oxygen or bivalent sulfur, Y is hydrogen or C1 to C6-alkyl; and (III) when -XY is taken together they represent hydrogen or C1 to C6-alkyl; are effective as drugs in warm-blooded animal patient to lower total cholesterol to treat atherosclerotic conditions and/or to alter the HDL/LDL ratio toward an increase in HDL cholesterol or toward a lower LDL cholesterol, or both, relative to the HDL/LDL ratio in a sample of the patient's blood before such treatment began.</p> |
