CYCLIC LACTAMS FOR CHOLESTEROL AND ATHEROSCLEROSIS CONTROL

WIPO Patent Application WO1989011856

A3

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.

THOMAS EDWARD W (US)
SPILMAN CHARLES H (US)

PCT/US1989/001949

January 11, 1990

May 11, 1989

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UPJOHN CO (US)

A61K31/395; A61K31/435; A61K31/44; A61K31/445; A61K31/4458; A61K31/451; A61K31/55; A61P3/06; A61P9/10; C07D211/76; C07D211/88; C07D221/20; C07D221/24; (IPC1-7): A61K31/395; A61K31/435; A61K31/44; A61K31/445; A61K31/55; C07D211/76; C07D211/88; C07D221/20; C07D221/24

FR2277585A1	1976-02-06
DE2637477A1	1978-02-23
DE2336770A1	1974-01-31
FR2405944A1	1979-05-11
FR1470305A	1967-02-24
GB1015618A	1966-01-05
GB2162180A	1986-01-29

CHEMICAL ABSTRACTS, Vol. 107, No. 17, 26 October 1987 (Columbus, Ohio, US), page 692* Abstract No. 145239z, & HU, A, 38929 (Richter Gedeon, Vegyeszeti Gyar Rt.) 28 July 1986*

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