公开(公告)号：US5981522A

公开(公告)日：1999-11-09

申请号：US41821

申请日：1998-03-12

申请人： Katsuji Yamashita ,  Takehiko Yamane ,  Shinichi Sakashita ,  Kazunori Hosoe ,  Kenji Fujii ,  Yasuhiro Saka

发明人： Katsuji Yamashita ,  Takehiko Yamane ,  Shinichi Sakashita ,  Kazunori Hosoe ,  Kenji Fujii ,  Yasuhiro Saka

IPC分类号： A61K31/438 ,  A61K31/5383 ,  A61K31/542 ,  A61K31/54

CPC分类号： A61K31/541 ,  A61K31/438 ,  A61K31/5383 ,  A61K31/542

摘要： A method for treating a digestive organ disease caused by the infection of Helicobacter, comprising administering a rifamycin derivative expressed by the formula (I), or a physiologically acceptable salt thereof ##STR1##

摘要翻译： 一种治疗由幽门螺杆菌感染引起的消化器官疾病的方法，其包括施用式（I）表示的利福霉素衍生物或其生理学上可接受的盐

公开(公告)号：US4983602A

公开(公告)日：1991-01-08

申请号：US407995

申请日：1989-09-14

申请人： Takehiko Yamane ,  Takuji Hashizume ,  Katsuji Yamashita ,  Kazunori Hosoe ,  Fumiyuki Kuze ,  Kiyoshi Watanabe

发明人： Takehiko Yamane ,  Takuji Hashizume ,  Katsuji Yamashita ,  Kazunori Hosoe ,  Fumiyuki Kuze ,  Kiyoshi Watanabe

IPC分类号： C07D498/18

CPC分类号： C07D498/18

摘要： A rifamycin derivative having the formula (I): ##STR1## wherein A is a group having the formula: ##STR2## in which R.sup.1 is an alkyl group having 4 or 5 carbon atoms or an alkenyl group having 3 to 5 carbon atoms, or a group having the formula: in which n is 3 or 4; or a pharmaceutically acceptable salt thereof. The rifamycin derivative (I) exhibits a strong antibacterial activity against Gram-positive bacteria and acid-fast bacteria, and also exhibits a strong antibacterial activity against tubercle bacilli.

公开(公告)号：US4859661A

公开(公告)日：1989-08-22

申请号：US75021

申请日：1987-07-13

申请人： Fumihiko Kano ,  Takehiko Yamane ,  Katsuji Yamashita ,  Kazunori Hosoe ,  Kiyoshi Watanabe

发明人： Fumihiko Kano ,  Takehiko Yamane ,  Katsuji Yamashita ,  Kazunori Hosoe ,  Kiyoshi Watanabe

IPC分类号： C07D498/18 ,  A61K31/365 ,  A61K31/535 ,  A61P31/04 ,  C07D498/14

CPC分类号： C07D498/18 ,  C07D519/00

摘要： A novel rifamycin derivative having the formula (I): ##STR1## wherein X.sup.1 is an alkyl group with 1 to 6 carbon atoms or a cycloalkyl group with 3 to 8 carbon atoms; X.sup.2 is a hydrogen atom or an alkyl group with 1 to 4 carbon atoms; R.sup.1 is hydrogen atom or acetyl group; A is a group represented by the formula: ##STR2## wherein R.sup.2 is an alkyl group with 1 to 4 carbon atoms or an alkoxyalkyl group with 2 to 6 carbon atoms and R.sup.3 is an alkyl group with 1 to 6 carbon atoms or an alkoxyalkyl group with 2 to 6 carbon atoms, or a group represented by the formula ##STR3## wherein ##STR4## is a 3 to 9 membered cyclic amino group with 2 to 8 carbon atoms, R.sup.4 is a hydrogen atom or an alkyl group having 1 to 4 carbon atoms, or salts thereof, a process for preparing the same and antibacterial agents containing the same as an effective ingredient.The rifamycin derivative of the present invention having the formula (I) shows a strong antibacterial activity against the Gram-positive bacteria and the acid-fast bacteria.

公开(公告)号：US4965261A

公开(公告)日：1990-10-23

申请号：US324499

申请日：1989-03-16

申请人： Fumihiko Kanoo ,  Takehiko Yamane ,  Hideo Kondo ,  Takuji Hashizume ,  Katsuji Yamashita ,  Kazunori Hosoe ,  Fumiyuki Kuze ,  Kiyoshi Watanabe

发明人： Fumihiko Kanoo ,  Takehiko Yamane ,  Hideo Kondo ,  Takuji Hashizume ,  Katsuji Yamashita ,  Kazunori Hosoe ,  Fumiyuki Kuze ,  Kiyoshi Watanabe

IPC分类号： C07D498/18

CPC分类号： C07D498/18

摘要： A rifamycin derivative having the formula (I): ##STR1## wherein R.sup.1 is hydrogen atom, methyl group or ethyl group, R.sup.2 is an alkyl group having 1 to 4 carbon atoms, and A is a group having the formula: ##STR2## in which n is an integer of 3 to 5, or group having the formula: ##STR3## in which R.sup.3 is a alkyl group having 1 to 5 carbon atoms; or a salt thereof. The rifamycin derivative (I) exhibits a strong antibacterial activity against Gram-positive bacteria and acid-fast bacteria, and also exhibits a strong antibacterial activity against tubercle bacilli.

公开(公告)号：US4690919A

公开(公告)日：1987-09-01

申请号：US826398

申请日：1986-02-05

申请人： Takehiko Yamane ,  Takuji Hashizume ,  Katsuji Yamashita ,  Kiyoshi Watanabe

发明人： Takehiko Yamane ,  Takuji Hashizume ,  Katsuji Yamashita ,  Kiyoshi Watanabe

IPC分类号： C07D498/18 ,  C07D519/00 ,  A61K31/535

CPC分类号： C07D498/18 ,  C07D519/00

摘要： A novel rifamycin derivative having the general formula (I): ##STR1## or salts thereof, a process for preparing the same and antibacterial agents containing the same as an effective component.The rifamycin derivative of the present invention having the general formula (I) shows a strong antibacterial activity against the Gram-positive bacteria and the acid-fast bacteria.

摘要翻译： 具有通式（I）的新型利福霉素衍生物或其盐，其制备方法和含有该有效成分的抗菌剂。 具有通式（I）的本发明的利福霉素衍生物显示出对革兰氏阳性菌和耐酸细菌的强抗菌活性。

公开(公告)号：US4925969A

公开(公告)日：1990-05-15

申请号：US324497

申请日：1989-03-16

申请人： Satomi Takahashi ,  Yasuyoshi Ueda ,  Kazuhiko Yamada ,  Yukio Yamada ,  Takehiko Yamane ,  Yoshifumi Yanagita ,  Yoshio Shimada ,  Kiyoshi Watanabe ,  Michio Nomura ,  Takehisa Ohashi ,  Kenji Inoue

发明人： Satomi Takahashi ,  Yasuyoshi Ueda ,  Kazuhiko Yamada ,  Yukio Yamada ,  Takehiko Yamane ,  Yoshifumi Yanagita ,  Yoshio Shimada ,  Kiyoshi Watanabe ,  Michio Nomura ,  Takehisa Ohashi ,  Kenji Inoue

IPC分类号： C07C227/08 ,  C07C233/46 ,  C07C271/06

CPC分类号： C07C233/46 ,  C07C227/08 ,  C07C271/06

摘要： Ethyl-.beta.-benzoyacrylate is reacted with an alkali metal salt of (S)-alanine or an alkali metal salt of N.sup.6 -trifluoroacetyl-L-lysine to form the corresponding Michael addition product, and not less than an equivalent amount of acid is added after completion of the Michael addition to prevent conversion of the (S,S) form of the product to the (R,S) form.

摘要翻译： 乙基-β-苯甲酸酯与（S） - 丙氨酸的碱金属盐或N6-三氟乙酰基-L-赖氨酸的碱金属盐反应形成相应的迈克尔加成产物，加入不少于等量的酸 完成迈克尔加成以防止（S，S）形式的产物转化为（R，S）形式。