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：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：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：US4440784A

公开(公告)日：1984-04-03

申请号：US337130

申请日：1982-01-05

申请人： Ikuo Katsumi ,  Hideo Kondo ,  Katsuji Yamashita ,  Takayoshi Hidaka ,  Kazunori Hosoe ,  Yutaka Ariki ,  Toshiaki Yamashita ,  Kiyoshi Watanabe

发明人： Ikuo Katsumi ,  Hideo Kondo ,  Katsuji Yamashita ,  Takayoshi Hidaka ,  Kazunori Hosoe ,  Yutaka Ariki ,  Toshiaki Yamashita ,  Kiyoshi Watanabe

IPC分类号： A61K31/05 ,  A61K31/22 ,  A61K31/255 ,  A61K31/275 ,  C07C49/248 ,  C07C49/747 ,  C07C49/753 ,  C07C49/835 ,  C07C59/52 ,  C07C59/90 ,  A61K31/19 ,  A61K31/235

CPC分类号： C07C205/17 ,  C07C255/00 ,  C07C49/248 ,  C07C49/747 ,  C07C49/753 ,  C07C49/835 ,  C07C59/52 ,  C07C59/90 ,  Y10S514/916

摘要： A new anti-inflammatory, analgesic, and antipyretic pharmaceutical composition is disclosed which contains a 3,5-di-tert-butyl-4-hydroxystyrene derivative of the formula: ##STR1## wherein R.sup.1 stands for a group represented by COR.sup.3 [R.sup.3 denotes a group of OR.sup.4 (R.sup.4 is a hydrogen atom or an alkyl group with C.sub.1 .about.C.sub.4), an alkyl group with C.sub.1 .about.C.sub.3, a phenyl group, or an amino group], a nitro group, or an alkylsulfonyl group represented by SO.sub.2 R.sup.5 (R.sup.5 is an alkyl group with C.sub.1 .about.C.sub.3); and R.sup.2 stands for a hydrogen atom, an alkyl group with C.sub.1 .about.C.sub.4, a hydroxyalkyl group with C.sub.1 .about.C.sub.4, a cyano group, or an acyl group represented by COR.sup.6 (R.sup.6 is an alkyl group with C.sub.1 .about.C.sub.3),or its pharmaceutically acceptable salt as an active ingredient in association with pharmaceutical excipients. The pharmaceutical composition has excellent anti-inflammatory, analgesic, and antipyretic activities and low toxicity.

摘要翻译： 公开了一种新的抗炎，止痛和解热药物组合物，其含有下式的3,5-二叔丁基-4-羟基苯乙烯衍生物：其中R1代表由COR3表示的基团[R3表示 一组OR4（R4为氢原子或C1-C6烷基，C1-C6烷基，C1〜C6烷基，苯基或氨基），硝基或SO2R5表示的烷基磺酰基（ R5是具有C1差异C3的烷基）; R2代表氢原子，具有C1差异C4的烷基，具有C1差异C4的羟基烷基，氰基或由COR6表示的酰基（R6是具有C1差异C3的烷基）或其药学上 可接受的盐作为与药物赋形剂相关的活性成分。 该药物组合物具有优异的抗炎，止痛和解热活性，毒性低。

公开(公告)号：US4431656A

公开(公告)日：1984-02-14

申请号：US337168

申请日：1982-01-05

申请人： Ikuo Katsumi ,  Hideo Kondo ,  Katsuji Yamashita ,  Takayoshi Hidaka ,  Kazunori Hosoe ,  Yutaka Ariki ,  Toshiaki Yamashita ,  Kiyoshi Watanabe

发明人： Ikuo Katsumi ,  Hideo Kondo ,  Katsuji Yamashita ,  Takayoshi Hidaka ,  Kazunori Hosoe ,  Yutaka Ariki ,  Toshiaki Yamashita ,  Kiyoshi Watanabe

IPC分类号： C07C49/248 ,  C07C49/747 ,  C07C49/753 ,  C07C49/835 ,  C07C59/52 ,  C07C59/90 ,  C07D233/96 ,  C07D307/58 ,  A61K31/415 ,  C07D307/26

CPC分类号： C07C255/00 ,  C07C49/248 ,  C07C49/747 ,  C07C49/753 ,  C07C49/835 ,  C07C59/52 ,  C07C59/90 ,  C07D233/96 ,  C07D307/58 ,  Y10S514/825 ,  Y10S514/916

摘要： Novel compounds, 3,5-di-tert-butylstyrene derivatives and their salts, are disclosed, which derivatives are represented by the general formula: ##STR1## wherein R.sup.1 stands for an acyloxy group represented by R.sup.3 COO (R.sup.3 is a hydrogen atom or an alkyl group with C.sub.1 -C.sub.6), an alkoxyl group of R.sub.4 O (R.sup.4 is an alkyl group with C.sub.1 -C.sub.4), a hydroxyl group, or a hydrogen atom; R.sup.2 stands for ##STR2## (R.sup.5 is a hydrogen atom or an alkyl group with C.sub.1 -C.sub.3 and X.sup.1 is CH.sub.2 or an oxygen atom), ##STR3## (R.sup.5 and X.sup.1 are each the same as defined above), or ##STR4## (X.sup.2 is an oxygen or sulfur atom). There are also disclosed an anti-inflammatory, analgesic, and antipyretic pharmaceutical composition and an anti-platelet aggregation pharmaceutical composition, both pharmaceutical compositions comprising the foregoing 3,5-di-tert-butylstyrene derivative or its pharmaceutically acceptable salt as an active ingredient in association with pharmaceutical excipients.

摘要翻译： 公开了新的化合物，3,5-二叔丁基苯乙烯衍生物及其盐，该衍生物由以下通式表示：其中R1代表由R3COO表示的酰氧基（R3是氢原子或 具有C1-C6的烷基），R4O的烷氧基（R4是具有C1-C4的烷基），羟基或氢原子; R2代表（R5是氢原子或具有C1-C3和X1是CH2的烷基或氧原子），＆lt; IMAGE＆gt;（R5和X1各自与上述相同）或 （X2是氧或硫原子）。 还公开了抗炎，镇痛和解热药物组合物和抗血小板聚集药物组合物，两种药物组合物包含前述3,5-二叔丁基苯乙烯衍生物或其药学上可接受的盐作为活性成分 与药物赋形剂的关联。

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：US5786349A

公开(公告)日：1998-07-28

申请号：US762501

申请日：1996-12-09

申请人： Katsuji Yamashita ,  Kazunori Hosoe ,  Takayoshi Hidaka ,  George Todaro ,  Ribhi M. Shawar

发明人： Katsuji Yamashita ,  Kazunori Hosoe ,  Takayoshi Hidaka ,  George Todaro ,  Ribhi M. Shawar

IPC分类号： C07D498/18 ,  A61K31/495 ,  A61K31/535 ,  A61K31/5383 ,  A61K31/54 ,  A61P31/04 ,  A61K31/33

CPC分类号： A61K31/541 ,  A61K31/5383

摘要： A method for treatment of diseases caused by Chlamydia infection is disclosed comprising administering a rifamycin of the formula (I): ##STR1## wherein R.sup.1 is hydrogen atom or acetyl, and X is oxygen, sulfur or a group NR, in which R is hydrogen, an alkyl group having 1 to 7 carbon atoms or a group of the formula (II): ##STR2## in which n is an integer of 1 to 3; or a physiologically acceptable salt thereof.

摘要翻译： 公开了治疗由衣原体感染引起的疾病的方法，其包括施用式（I）的利福霉素：其中R1是氢原子或乙酰基，X是氧，硫或基团NR，其中 R是氢，具有1至7个碳原子的烷基或式（II）的基团：其中n是1至3的整数; 或其生理上可接受的盐。

公开(公告)号：US06486161B1

公开(公告)日：2002-11-26

申请号：US09463580

申请日：2000-05-23

申请人： Kenji Fujii ,  Katsuji Yamashita ,  Kazunori Hosoe ,  Robert J. Yancey, Jr. ,  Jeffrey L. Watts

发明人： Kenji Fujii ,  Katsuji Yamashita ,  Kazunori Hosoe ,  Robert J. Yancey, Jr. ,  Jeffrey L. Watts

IPC分类号： A61K3150

CPC分类号： A61K31/5383

摘要： A method for treating mastitis in a domestic animal in need of such a treatment, which comprises administering to the animal a pharmaceutical composition comprising a rifamycin derivative of the formula (1): wherein R is an alkyl group having 1 to 7 carbon atoms or a physiologically acceptable salt thereof as an active ingredient, and a physiologically acceptable carrier. The present invention provides a novel therapeutic method effective for treatment of mastitis caused by bacterial infection in a domestic animal.

摘要翻译： 一种在需要这种治疗的家畜中治疗乳腺炎的方法，其包括向动物施用包含式（1）的利福霉素衍生物的药物组合物：其中R是具有1至7个碳原子的烷基或 其生理学上可接受的盐作为活性成分，以及生理上可接受的载体。 本发明提供了一种有效治疗家畜细菌感染引起的乳腺炎的新型治疗方法。

公开(公告)号：US06362169B1

公开(公告)日：2002-03-26

申请号：US09622712

申请日：2000-08-22

申请人： Kenji Fujii ,  Katsuji Yamashita ,  Kazunori Hosoe ,  Takayoshi Hidaka

发明人： Kenji Fujii ,  Katsuji Yamashita ,  Kazunori Hosoe ,  Takayoshi Hidaka

IPC分类号： A61K3170

CPC分类号： A61K45/00 ,  A61K31/395 ,  A61K31/415 ,  A61K31/44 ,  A61K31/60 ,  A61K33/245 ,  A61K2300/00

摘要： Antibacterial compositions comprising (1) a rifamycin derivative represented by the formula (I) or its physiologically acceptable salt, and (2) a proton pump inhibitor (a) or a bismuth preparation (b) wherein the components (1) and (2) are used in such amounts as producing a synergistic effect against Helicobacter pylori, drugs and remedies for digestive organ diseases which contain the antibacterial compositions, process for producing them, and pharmaceutical preparations related to the antibacterial compositions. The compositions can be administered to patients with digestive diseases caused by infection of Helicobacter pylori in a smaller dose and at a lower administration frequency as compared with conventional remedies.

摘要翻译： 抗菌组合物，其包含（1）由式（I）表示的利福霉素衍生物或其生理学上可接受的盐，和（2）质子泵抑制剂（a）或铋制剂（b），其中组分（1）和（2） 用于产生对幽门螺杆菌的协同效应，含有抗菌组合物的消化器官疾病的药物和补救剂，其制备方法和与抗菌组合物相关的药物制剂。 与常规治疗相比，组合物可以以较小的剂量和较低的施用频率施用于由幽门螺杆菌感染引起的消化系统疾病的患者。