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    • 9. 发明申请
    • MACROCYCLIC LACTONE COMPOUNDS AND METHODS FOR THEIR USE
    • MACROCYCLIC LACTONE化合物及其使用方法
    • WO2009114010A1
    • 2009-09-17
    • PCT/US2008/056501
    • 2008-03-11
    • ELIXIR MEDICAL CORPORATIONYAN, JohnZHENG, XiaoxiaBHAT, Vinayak D.
    • YAN, JohnZHENG, XiaoxiaBHAT, Vinayak D.
    • A01N43/04A61K31/70
    • A61K31/70A61K31/436
    • The present invention provides a pharmaceutical composition comprising a pharmaceutically acceptable excipient and a compound of the formula (I) wherein R 1 , R 2 , R 3 , R 5 , R 6 , R 8 , M 1 , M 2 , M 3 , M 4 , M 5 , M 6 and M 7 are each independently a member selected from the group consisting of H, C 1-6 alkyl, OH and C 1-6 hydroxyalkyl; R 4 , R 7 and R 9 are each independently selected from the group consisting of C 1-6 alkoxy and OH; R 10 is a member selected from the group consisting of H, -OH, -OP(O)Me 2 , (II), (III), -O-(CH 2 ) n -OH and -O-(CH 2 ) m -O-(CH 2 ) o -CH 3 , wherein subscripts n and m are each independently from 2 to 8 and subscript o is from 1 to 6; each of L 1 and L 4 are independently selected from the group consisting of (IV) and (V) wherein each M 8 is independently a member selected from the group consisting Of C 1-6 alkyl, OH and C1-6 hydroxyalkyl; each of L 2 and L 3 are independently selected from the group consisting of (VI), (VII) and (VIII); 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式(I)化合物的药物组合物,其中R 1,R 2,R 3,R 5,R 6,R 8,M 1,M 2,M 3,M 5,M 6和M 7各自独立 选自H,C 1-6烷基,OH和C 1-6羟基烷基的成员; 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,(II),(III),-O-(CH 2)n -OH和-O-(CH 2)m O-(CH 2) )o-CH3,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(IV)和(V),其中每个M8独立地是选自C1-6烷基,OH和C1-6羟基烷基的成员; L2和L3各自独立地选自由(VI),(VII)和(VIII)组成的组。 及其盐,水合物,异构体,代谢物,N-氧化物和前药。