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    • 8. 发明申请
    • MACROCYCLIC LACTONE COMPOUNDS AND METHODS FOR THEIR USE
    • MACROCYCLIC LACTONE化合物及其使用方法
    • US20150352089A1
    • 2015-12-10
    • US14831747
    • 2015-08-20
    • Elixir Medical Corporation
    • John YanXiaoxia ZhengVinayak D. Bhat
    • A61K31/439A61K45/06A61K9/00
    • A61K31/436A61K9/0004A61K31/439A61K31/4525A61K45/06
    • The present invention provides a pharmaceutical composition comprising a pharmaceutically acceptable excipient and a compound of the formula: wherein R1, R2, R3, R5, R6, R8, M1, M2, M3, M4, M5, M6 and M7 are each independently a member selected from the group consisting of H, C1-6 alkyl, OH and C1-6 hydroxyalkyl; R4, R7 and R9 are each independently selected from the group consisting of C1-6 alkoxy and OH; R10 is a member selected from the group consisting of H, —OH, —OP(O)Me2, —O—(CH2)n—OH and —O—(CH2)m—O—(CH2)o—CH3, wherein subscripts n and m are each independently from 2 to 8 and subscript o is from 1 to 6; each of L1 and L4 are independently selected from the group consisting of: wherein each M8 is independently a member selected from the group consisting of C1-6 alkyl, OH and C1-6 hydroxyalkyl; each of L2 and L3 are independently selected from the group consisting of: and salts, hydrates, isomers, metabolites N-oxides and prodrugs thereof.
    • 本发明提供包含药学上可接受的赋形剂和下式化合物的药物组合物:其中R1,R2,R3,R5,R6,R8,M1,M2,M3,M4,M5,M6和M7各自独立地为成员 选自H,C 1-6烷基,OH和C 1-6羟基烷基; R 4,R 7和R 9各自独立地选自C 1-6烷氧基和OH; R 10是选自H,-OH,-OP(O)Me 2,-O-(CH 2)n -OH和-O-(CH 2)m -O-(CH 2)o -CH 3的成员,其中 下标n和m各自独立地为2至8,下标o为1至6; L1和L4各自独立地选自:其中每个M8独立地是选自C 1-6烷基,OH和C 1-6羟基烷基的成员; L2和L3中的每一个独立地选自:盐,水合物,异构体,代谢物N-氧化物和前药。