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    • 2. 发明申请
    • MORPHINE AND CODEINE DERIVATIVES FOR USE IN THERAPY
    • 用于治疗的吗啡和代谢衍生物
    • WO1996016063A1
    • 1996-05-30
    • PCT/GB1995002712
    • 1995-11-20
    • BRITISH TECHNOLOGY GROUP LIMITEDMARPLES, Brian, ArthurTRAYNOR, John, Richard
    • BRITISH TECHNOLOGY GROUP LIMITED
    • C07D489/02
    • C07D489/02
    • A compound of formula (I) wherein R1 = H (morphine analogue), CH3 (codeine analogue), R2 = H, alkyl group of 1 to 4 carbon atoms, allyl, cyclopropylmethyl, R3 = a group (A), -O-CH2-R4 (ether), -O-COCH = CHR4 (cinnamate), R4 = (B), wherein X1, X2, X3, X4 and X5 which may be the same or different are separately selected from H, alkyl of 1 to 4 carbon atoms, NH2, NO2, alkoxy group of 1 to 4 carbon atoms, hydroxy, halogen, N-alkyl, group of 1 to 4 carbon atoms, morpholine, or a group COR5 wherein R5 is H, OH, O-alkyl where alkyl is from 1 to 4 carbon atoms, or one of X1 and X2, X2 and X3, X3 and X4 or X4 and X5 together with an alkylene group optionally interrupted by O, S or N of up to 5 atoms in length complete a ring and a pharmaceutically acceptable salt thereof for use in therapy.
    • 式(I)的化合物,其中R1 = H(吗啡类似物),CH3(可待因类似物),R 2 = H,1至4个碳原子的烷基,烯丙基,环丙基甲基,R 3 = A(A) CH2-R4(醚),-O-COCH = CHR4(肉桂酸酯),R4 =(B),其中X1,X2,X3,X4和X5可以相同或不同,分别选自H, 4个碳原子,NH 2,NO 2,1至4个碳原子的烷氧基,羟基,卤素,N-烷基,1至4个碳原子,吗啉或基团COR 5,其中R 5是H,OH,O-烷基 烷基是1至4个碳原子,或者X 1和X 2,X 2和X 3,X 3和X 4或X 4和X 5中的一个与任选被长达5个原子的O,S或N间隔的亚烷基一起形成环 及其药学上可接受的盐用于治疗。