公开(公告)号：US5519122A

公开(公告)日：1996-05-21

申请号：US359825

申请日：1994-12-20

申请人： Keiichi Ajito ,  Ken-ichi Kurihara ,  Akira Shimizu ,  Shuichi Gomi ,  Nobue Kikuchi ,  Minako Araake ,  Tsuneo Ishizuka ,  Aiko Miyata ,  Osamu Hara ,  Seiji Shibahara

发明人： Keiichi Ajito ,  Ken-ichi Kurihara ,  Akira Shimizu ,  Shuichi Gomi ,  Nobue Kikuchi ,  Minako Araake ,  Tsuneo Ishizuka ,  Aiko Miyata ,  Osamu Hara ,  Seiji Shibahara

IPC分类号： C07H17/08 ,  B01D53/047

CPC分类号： C07H17/08

摘要： 16-membered macrolide derivatives represented by the formula (I): ##STR1## wherein R.sup.1 represents a hydrogen atom or a COR.sup.6 group, wherein R.sup.6 represents a straight-chain alkyl group having 1 to 3 carbon atoms; R.sup.2 represents a hydrogen atom or a COR.sup.6 group, wherein R.sup.6 is as defined above; R.sup.3 represents a hydrogen atom or a COR.sup.6 group, wherein R.sup.6 is as defined above; R.sup.4 represents a straight-chain alkyl group having 1 to 4 carbon atoms or a substituted or unsubstituted allyl group; and R.sup.5 represents a substituted or unsubstituted, straight-chain or branched alkyl, alkenyl or aralkyl group having 1 to 10 carbon atoms;and pharmaceutically acceptable salts thereof are disclosed. These compounds show excellent and long-acting antimicrobial activities. A novel process for producing these 16-membered macrolide derivatives is further disclosed.

公开(公告)号：US5407918A

公开(公告)日：1995-04-18

申请号：US143125

申请日：1993-10-29

申请人： Keiichi Ajito ,  Ken-ichi Kurihara ,  Akira Shimizu ,  Shuichi Gomi ,  Nobue Kikuchi ,  Minako Araake ,  Tsuneo Ishizuka ,  Aiko Miyata ,  Osamu Hara ,  Seiji Shibahara

发明人： Keiichi Ajito ,  Ken-ichi Kurihara ,  Akira Shimizu ,  Shuichi Gomi ,  Nobue Kikuchi ,  Minako Araake ,  Tsuneo Ishizuka ,  Aiko Miyata ,  Osamu Hara ,  Seiji Shibahara

IPC分类号： C07H17/08 ,  C12P19/62 ,  A61K31/70 ,  C12P19/60

CPC分类号： C07H17/08

摘要： 16-membered macrolide derivatives represented by the formula (I): ##STR1## wherein R.sup.1 represents a hydrogen atom or a COR.sup.6 group, wherein R.sup.6 represents a straight-chain alkyl group having 1 to 3 carbon atoms; R.sup.2 represents a hydrogen atom or a COR.sup.6 group, wherein R.sup.6 is as defined above; R.sup.3 represents a hydrogen atom or a COR.sup.6 group, wherein R.sup.6 is as defined above; R.sup.4 represents a straight-chain alkyl group having 1 to 4 carbon atoms or a substituted or unsubstituted allyl group; and R.sup.5 represents a substituted or unsubstituted, straight-chain or branched alkyl, alkenyl or aralkyl group having 1 to 10 carbon atoms; and pharmaceutically acceptable salts thereof are disclosed. These compounds show excellent and long-acting antimicrobial activities. A novel process for producing these 16-membered macrolide derivatives is further disclosed.

摘要翻译： 由式（I）表示的16元大环内酯衍生物：其中R 1表示氢原子或COR 6基团，其中R 6表示具有1至3个碳原子的直链烷基; R2表示氢原子或COR6基团，其中R6如上所定义; R3表示氢原子或COR6基团，其中R6如上所定义; R4表示碳原子数1〜4的直链烷基或取代或未取代的烯丙基; R 5表示具有1〜10个碳原子的取代或未取代的直链或支链烷基，烯基或芳烷基; 及其药学上可接受的盐。 这些化合物显示出优异的长效抗菌活性。 进一步公开了一种制备这些16元大环内酯衍生物的新方法。

公开(公告)号：US5444174A

公开(公告)日：1995-08-22

申请号：US22165

申请日：1993-02-25

申请人： Keiichi Ajito ,  Kenichi Kurihara ,  Tsuneo Ishizuka ,  Tetsuro Hara ,  Takayuki Usui ,  Seiji Shibahara

发明人： Keiichi Ajito ,  Kenichi Kurihara ,  Tsuneo Ishizuka ,  Tetsuro Hara ,  Takayuki Usui ,  Seiji Shibahara

IPC分类号： A61K31/70 ,  A61K31/7042 ,  A61K31/7048 ,  A61P31/04 ,  C07H17/08 ,  C07D313/06

CPC分类号： C07H17/08

摘要： 16-membered macrolide compounds wherein both of hydroxyl groups at the 3"- and 4"-positions form ether bonds together with two alkyl groups which are either the same or different from each other is useful as an antibacterial agent. The macrolide compounds represented by formula (I) are prepared by chemically modifying midecamycin A.sub.3 to obtain a synthesis intermediate of the formula (II), which is further chemically modified. ##STR1##

摘要翻译： 3“和4”位上的两个羟基与其彼此相同或不同的两个烷基形成醚键的16元大环内酯化合物可用作抗菌剂。 由式（I）表示的大环内酯化合物通过化学修饰麦地卡霉素A3制备得到式（II）的合成中间体，其进一步化学修饰。 （一）