C - Chemistry – Metallurgy – 07 – J
Patent
C - Chemistry, Metallurgy
07
J
C07J 9/00 (2006.01) A61K 31/575 (2006.01) C07J 17/00 (2006.01) C07J 31/00 (2006.01) C07J 41/00 (2006.01) A61K 31/705 (1990.01)
Patent
CA 2120498
2120498 9403177 PCTABS00030 Pharmaceutical compositions are provided for lowering the activity of HMG-CoA reductase and/or lowering serum cholesterol, comprising a side chain derivatized 15-oxygenated sterol having formula (I): the basic ring structure being saturated or unsaturated, wherein R1 is -OH, =O, -OR7, (a), (b), a sulfate group, a sugar moiety, or a Mg, Na, or K salt of a sulfate group; R2 is -H, -OH, =O, mono- or di-halogen, or a C1 to C6 alkyl group, which may be unsaturated or substituted with halogen; R3 is -H, -OH, halogen, or a C1 to C6 alkyl group, which may be unsaturated or substituted with halogen; R4 is nonexistent when there is a double bond between the 8 and 14 carbons or .alpha.H, .beta.H, or an .alpha.C1 to C6 alkyl group; R5 is -OH, =O, =NOH, or (a); R6 is -CH2CH(CH3)2, in which one or more of the hydrogen atoms is replaced by OH or halogen, -CH=C(CH3)2, in which one or more of the hydrogen atoms may be replaced by OH or halogen, or -CH2N(CH3)2, in which one or more of the hydrogen atoms may be replaced by OH or halogen, provided that no carbon atom with an OH is also substituted with halogen or an additional OH; R7 is a C1 to C6 alkyl group; R8 is a C1 to C20 aliphatic group, which may be substituted or unsubstituted, or a phenyl group; and n is an integer of from 2 to 6; with the proviso that said sterol is not 3.beta., 26-dihydroxy-5.alpha.-cholest-8(14)-en-15-one.
Herz Josef E.
Schroepfer George J. Jr.
Swaminathan Shankar
Wilson William K.
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