会员体验
专利管家(专利管理)
工作空间(专利管理)
风险监控(情报监控)
数据分析(专利分析)
侵权分析(诉讼无效)
联系我们
交流群
官方交流:
QQ群: 891211   
微信请扫码    >>>
现在联系顾问~
热词
    • 5. 发明申请
    • SIDE CHAIN DERIVATIZED 15-OXYGENATED STEROLS, METHODS OF USING THEM AND A PROCESS FOR PREPARING THEM
    • 侧链衍生的15-氧化的甾体,使用它们的方法和制备它们的方法
    • WO1994003177A2
    • 1994-02-17
    • PCT/US1993007230
    • 1993-08-03
    • WILLIAM MARSH RICE UNIVERSITYSCHROEPFER, George, J., Jr.HERZ, Josef, E.SWAMINATHAN, ShankarWILSON, William, K.
    • WILLIAM MARSH RICE UNIVERSITY
    • A61K31/575
    • C07J9/005A61K31/575C07J9/00C07J31/006C07J41/0055
    • 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.
    • 提供了用于降低HMG-CoA还原酶和/或降低血清胆固醇的活性的药物组合物,其包含具有式(I)的侧链衍生的15-氧化固醇:所述碱性环结构是饱和或不饱和的,其中R 1是-OH, = O,-OR7,(a),(b),硫酸根基团,糖部分或硫酸根基团的Mg,Na或K盐; R2是-H,-OH,= O,单 - 或二 - 卤素,或可以是不饱和的或被卤素取代的C1-C6烷基; R3是-H,-OH,卤素或C1-C6烷基,其可以是不饱和的或被卤素取代的; 在8和14碳之间存在双键或(α)H,(β)H或(α)C 1至C 6烷基时,R 4不存在; R5是-OH,= O,= NOH或(a); R6是-CH2CH(CH3)2,其中一个或多个氢原子被OH或卤素取代,-CH = C(CH 3)2,其中一个或多个氢原子可以被OH或卤素取代 或-CH 2 N(CH 3)2,其中一个或多个氢原子可以被OH或卤素代替,条件是没有碳原子与OH也被卤素或另外的OH取代; R7是C1-C6烷基; R8是可以是取代或未取代的C1〜C20脂肪族基团或苯基; n为2〜6的整数。 条件是所述甾醇不是3(β),26-二羟基-5(α) - 胆甾-8(14)-en-15-酮。