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    CNS active substituted azetidinone compounds
    4.
    发明授权
    CNS active substituted azetidinone compounds 失效
    CNS活性取代的氮杂环丁酮化合物

    公开(公告)号：US4719207A

    公开(公告)日：1988-01-12

    申请号：US747018

    申请日：1985-06-20

    申请人： Toshinari Tamura ,  Makoto Yoshida ,  Shin-ichi Tsukamoto ,  Hidenori Iwamoto ,  Minoru Yamamoto ,  Soichi Kagami

    发明人： Toshinari Tamura ,  Makoto Yoshida ,  Shin-ichi Tsukamoto ,  Hidenori Iwamoto ,  Minoru Yamamoto ,  Soichi Kagami

    IPC分类号： C07D205/08 ,  C07D205/085 ,  C07F7/10 ,  C07K5/097 ,  A61K31/415 ,  C07D403/12 ,  C07D403/14

    CPC分类号： C07K5/0821 ,  C07D205/08 ,  C07D205/085 ,  C07F7/10

    摘要： Substituted azetidinone compounds are provided which have the formula: ##STR1## wherein one of R.sup.1 and R.sup.2 represents a substituted lower alkyl group, an azido group, an amino group, a lower acylamino group, a mercapto group or a lower alkylthio group and the other represents a hydrogen group, or, both represent hydrogen atoms or lower alkyl groups; R.sup.3 represents a hydrogen atom or a group shown by formula: ##STR2## (wherein X represents ##STR3## (wherein R.sup.5 represents a hydrogen atom or a lower alkyl group) and Y represents a hydroxy group, a lower alkoxy group, an amino group, a mono- or di-lower alkylamino group); R.sup.4 represents a hydrogen atom, a substituted or unsubstituted lower alkyl group or a group shown by formula: --CH.sub.2 CO--A (wherein A represents an amino group or a group shown by formula: ##STR4## (wherein X and Y are as defined above), provided that when R.sup.1 and R.sup.2 are both hydrogen atoms, at least R.sup.4 represents a group other than a hydrogen atom and provided that either R.sup.3 or R.sup.4 represents a group other than a hydrogen atom. The compounds have strong CNS action.

    摘要翻译： 提供具有下式的取代的氮杂环丁酮化合物：其中R 1和R 2之一表示取代的低级烷基，叠氮基，氨基，低级酰氨基，巯基或低级烷硫基 另一个表示氢基团，或者都表示氢原子或低级烷基; R3表示氢原子或由下式表示的基团：其中X表示（其中R5表示氢原子或低级烷基），Y表示羟基，低级烷氧基，氨基 ，一或二低级烷基氨基）; R 4表示氢原子，取代或未取代的低级烷基或由式-CH 2 CO-A（其中A表示氨基或由下式表示的基团：其中X和Y如上所定义） ），条件是当R 1和R 2均为氢原子时，至少R 4表示氢原子以外的基团，只要R 3或R 4表示除氢原子以外的基团，则该化合物具有强CNS作用。

    Tylosin derivatives, their preparation and pharmaceutical compositions containing them
    9.
    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。