发明名称 Lipids and Lipid Compositions for the Delivery of Active Agents
摘要 This invention provides for a compound of formula (I): or a pharmaceutically acceptable salt thereof, wherein R1-R4, n and p are defined herein. The compounds of formula (I) and pharmaceutically acceptable salts thereof are cationic lipids useful in the delivery of biologically active agents to cells and tissues.;
申请公布号 US2016311759(A1) 申请公布日期 2016.10.27
申请号 US201415104736 申请日期 2014.12.17
申请人 Brito Luis;Chen Delai;Gamber Gabriel Grant;Geall Andrew;Love Kevin;Zabawa Thomas;Zecri Frederic 发明人 Brito Luis;Chen Delai;Gamber Gabriel Grant;Geall Andrew;Love Kevin;Zabawa Thomas;Zecri Frederic
分类号 C07C229/12;C07D295/15;C07D211/06;C07D211/62;C07C271/22;C07D211/34;C07D265/30;C07C229/38;C07D211/44;C07D205/04;A61K9/51;A61K9/127;A61K31/713;A61K39/39;C07D207/16 主分类号 C07C229/12
代理机构 代理人
主权项 1. A compound, or salt thereof, of formula (X): wherein n and p are each, independently, 0, 1 or 2; L1 is —OC(O)—, —C(O)O— or a bond; R1 is heterocyclyl, heterocyclyl-C1-8-alkyl or heterocyclyl-C1-8-alkoxyl, each of which may be optionally substituted with 1, 2, 3, 4 or 5 groups, independently selected from halogen, formidamidine, C1-8-alkyl, C3-7-cycloalkyl, heterocyclyl, —[(C1-C4)alkylene]v-N(R′)R″, —O—[(C1-C4)alkylene]v-N(R′)R″ or —N(H)—[(C1-C4)alkylene]v-N(R′)R″, where said (C1-C4)alkylene is optionally substituted with one or more R groups; v is 0, 1, 2, 3 or 4; R is hydrogen or —C1-8-alkyl or when v is 0 R is absent; R′ and R″, are each, independently, hydrogen, —C1-8-alkyl; or R′ and R″ combine with the nitrogen to which they are bound, and optionally including another heteroatom selected from N, O and S, to form a 5-8 membered heterocycle or heteroaryl, optionally substituted with an —C1-8-alkyl, hydroxy or cycloalkyl-C1-8—; R2 and R3 are each, independently, C7-22 alkyl, C12-22 alkenyl, C3-8 cycloalkyl optionally substituted with 1, 2, or 3 C1-8 alkyl groups, R4 is selected from hydrogen, C1-14 alkyl,
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