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    Tylosin derivatives, their preparation and pharmaceutical compositions containing them
    7.
    发明授权
    Tylosin derivatives, their preparation and pharmaceutical compositions containing them 失效
    泰乐菌素衍生物，它们的制剂和含有它们的药物组合物

    公开(公告)号：US4477443A

    公开(公告)日：1984-10-16

    申请号：US395463

    申请日：1982-07-06

    申请人： Hamao Umezawa ,  Sumio Umezawa ,  Tsutomu Tsuchiya ,  Tomio Takeuchi ,  Akihiro Tanaka ,  Hidenori Iwamoto ,  Shuichi Sakamoto

    发明人： Hamao Umezawa ,  Sumio Umezawa ,  Tsutomu Tsuchiya ,  Tomio Takeuchi ,  Akihiro Tanaka ,  Hidenori Iwamoto ,  Shuichi Sakamoto

    IPC分类号： C07H17/08 ,  A61K31/71

    CPC分类号： C07H17/08

    摘要： Tylosin compounds of the formula ##STR1## wherein R.sub.1 represents a hydroxyl group; a halogen atom; ##STR2## group (wherein R.sub.5 is a hydrogen atom or a lower alkyl group which may be substituted by a hydroxyl group and R.sub.6 is a hydrogen atom, a lower alkyl group which may be substituted by a hydroxyl group, an aryl group, an aralkyl group, a cycloalkyl group having 3-10 carbon atoms, --CO(O).sub.m --R.sub.7 group (wherein m is 0 or 1 and R.sub.7 is a lower alkyl group, an aryl group, an aralkyl group, a furanyl group, or a pyridyl group), or --CH.sub.2 --R.sub.13 group (wherein R.sub.13 is a mono-, di-, or trifluoromethyl group)); --N(CH.sub.2).sub.n group (wherein n is an integer of 2-15) which may be substituted by an oxo group, a hydroxyl group, a lower alkyl group, or a hydroxy lower alkyl group; an imidazolyl group, a morpholino group, or a piperazino group each may be substituted by a lower alkyl group; or --OOCCH.sub.2 --R.sub.8 group (wherein R.sub.8 is ##STR3## group (wherein R.sub.9 and R.sub.10, which may be the same or different, each is a hydrogen atom or a lower alkyl group; said R.sub.9 and R.sub.10 may be combined with each other to form an alkylene group having 3-7 carbon atoms) or --S--R.sub.11 group (wherein R.sub.11 is a furanyl group or a pyridyl group)); R.sub.2 represents a hydrogen atom or a lower alkanoyl group; R.sub.3 represents a methyl group or --CH.sub.2 CHO group; R.sub.4 represents a hydrogen atom or a hydroxyl group; A represents 0.dbd., ##STR4## line represents a single bond or a double bond; and line ---- represents a single bond, a double bond, or ; however, when said R.sub.1 is a hydroxyl group, said R.sub.3 is a methyl group and R.sub.4 is a hydrogen atom, or said line ---- is ; or when said R.sub.1 is a halogen atom, said R.sub.3 is a methyl group of said line ---- is .The foregoing compounds of this invention are useful as antibiotics.

    摘要翻译： 式“IMAGE”的泰乐菌素化合物，其中R 1表示羟基; 卤素原子; 基（其中R5是氢原子或可被羟基取代的低级烷基，R6是氢原子，可被羟基取代的低级烷基，芳基，芳烷基 基团，具有3-10个碳原子的环烷基，-CO（O）m-R7基团（其中m为0或1，R7为低级烷基，芳基，芳烷基，呋喃基或 吡啶基）或-CH 2 -R 13基（其中R 13是单 - ，二 - 或三氟甲基））; -N（CH 2）n基（其中n为2-15的整数），其可被氧代基，羟基，低级烷基或羟基低级烷基取代; 咪唑基，吗啉代基或哌嗪子基各自可以被低级烷基取代; 或-OOCCH 2 -R 8基团（其中R 8为<基团）（其中R 9和R 10可以相同或不同，各自为氢原子或低级烷基;所述R 9和R 10可彼此组合 形成具有3-7个碳原子的亚烷基）或-S-R11基（其中R11是呋喃基或吡啶基））; R2表示氢原子或低级烷酰基; R3表示甲基或-CH2CHO基; R4表示氢原子或羟基; A代表0 =，线代表单键或双键; 线----代表单键，双键，或; 然而，当所述R 1为羟基时，所述R 3为甲基，R 4为氢原子， 或者当所述R 1为卤素原子时，所述R 3为所述线----甲基。 本发明的前述化合物可用作抗生素。