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1. 发明授权

US5663162A Cephem derivatives 失效
标题翻译： Cephem衍生物
公开(公告)号：US5663162A
公开(公告)日：1997-09-02
申请号：US436280
申请日：1995-07-25
申请人： Kunio Atsumi , Eijiro Umemura , Yuko Kano , Sohjiro Shiokawa , Toshiaki Kudo , Masaki Tsushima , Katsuyoshi Iwamatsu , Atsushi Tamura , Seiji Shibahara
发明人： Kunio Atsumi , Eijiro Umemura , Yuko Kano , Sohjiro Shiokawa , Toshiaki Kudo , Masaki Tsushima , Katsuyoshi Iwamatsu , Atsushi Tamura , Seiji Shibahara
IPC分类号： C07D501/00 , C07D501/46 , C07D519/06 , A61K31/545
CPC分类号： C07D501/00
摘要： Compounds represented by the following formula (I), that is, cephem derivatives having substituted or unsubstituted imidazo[5,1-b]thiazolium-6-yl as a substituent at the 3-position of the cephem ring: ##STR1## wherein X represents CH or N, R.sup.1 represents H, alkyl, alkenyl or the like, and R.sup.2, R.sup.3, R.sup.4 and R.sup.5 represent H, alkyl, carbamoyl, amino or the like. The above compounds have excellent antibacterial activity, and useful as medicines for the treatment of various infectious diseases caused by bacteria.
摘要翻译： PCT No.PCT / JP94 / 01529 Sec。 371日期：1995年7月25日 102（e）日期1995年7月25日PCT 1994年9月16日PCT PCT。出版物WO95 / 07912 日期：1993年3月23日由下式（I）表示的化合物，即具有取代或未取代的咪唑并[5,1-b]噻唑鎓-6-基作为头孢烯环3位的取代基的头孢烯衍生物：其中X表示CH或N，R 1表示H，烷基，烯基等，R 2，R 3，R 4和R 5表示H，烷基，氨基甲酰基，氨基等。上述化合物具有优异的抗菌活性，可用作治疗由细菌引起的各种感染性疾病的药物。

2. 发明授权

US5827845A Cephalosporin derivative 失效
标题翻译：头孢菌素衍生物
公开(公告)号：US5827845A
公开(公告)日：1998-10-27
申请号：US617870
申请日：1996-07-31
申请人： Sohjiro Shiokawa , Kunio Atsumi , Katsuyoshi Iwamatsu , Atsushi Tamura , Seiji Shibahara
发明人： Sohjiro Shiokawa , Kunio Atsumi , Katsuyoshi Iwamatsu , Atsushi Tamura , Seiji Shibahara
IPC分类号： C07D501/00 , C07D501/24 , C07D501/56 , A61K31/545
CPC分类号： C07D501/00 , Y02P20/55
摘要： A cephalosporin derivative which has a substituted or unsubstituted 2-(5-thiazolyl)vinyl group at the 3-position and is represented by the following formula (I) ##STR1## wherein X is CH or N, R.sup.1 is an amino group or a protected amino group, R.sup.2 is a hydrogen atom or a hydroxyimino-protecting group, R.sup.3 is a hydrogen atom, a salt-forming cation or a carboxyl-protecting group, R.sup.4 is a hydrogen atom, and R.sup.5 is a hydrogen atom, a lower alkyl group, a halo-(lower)alkyl group or a halogen atom, is now synthetised as a cephem compound which exhibits excellent antibacterial activities and is useful as a therapeutic agent for various bacterial infections.
摘要翻译： PCT No.PCT / JP94 / 01618 Sec。 371日期：1996年7月31日 102（e）日期1996年7月31日PCT 1994年9月29日PCT PCT。公开号WO95 / 09171 日期：1995年4月6日，头孢菌素衍生物，其3-位具有取代或未取代的2-（5-噻唑基）乙烯基，由下式（I）表示：其中X为CH或N R1为氨基或被保护的氨基，R2为氢原子或羟基亚氨基保护基，R3为氢原子，成盐阳离子或羧基保护基，R4为氢原子，R5为作为氢原子，低级烷基，卤代（低级）烷基或卤素原子，现在被合成为具有优异抗菌活性的头孢烯化合物，可用作各种细菌感染的治疗剂。

3. 发明授权

US5464829A Cephalosporin derivatives 失效
标题翻译：头孢菌素衍生物
公开(公告)号：US5464829A
公开(公告)日：1995-11-07
申请号：US167204
申请日：1993-12-16
申请人： Masaki Tsushima , Yuko Kano , Katsuyoshi Iwamatsu , Atsushi Tamura , Seiji Shibahara
发明人： Masaki Tsushima , Yuko Kano , Katsuyoshi Iwamatsu , Atsushi Tamura , Seiji Shibahara
IPC分类号： A61K31/545 , A61K31/546 , A61P31/04 , C07D501/00 , C07D519/06 , C07D501/36
CPC分类号： C07D501/00 , Y02P20/55
摘要： A cephalosporin derivative having a quaternary salt type substituent group at the 3-position, represented by formula (I): ##STR1## wherein X is a carbon atom or a nitrogen atom; Y is a sulfur atom, an oxygen atom or a nitrogen atom substituted with a substituted or unsubstituted lower alkyl group; R.sup.1 is a hydrogen atom, a lower alkyl group or a substituted lower alkyl group; R.sup.2 is a lower alkyl group, a substituted lower alkyl group, a lower alkylene group or a substituted lower alkylene group; and A is an unsaturated six-membered heterocyclic ring containing at least one nitrogen atom, or a pharmaceutically acceptable salt thereof is disclosed. The derivatives have excellent antibacterial activities and can be used as a drug for the treatment of various bacterial infections.
摘要翻译：由式（I）表示的3-位具有季盐型取代基的头孢菌素衍生物：其中X为碳原子或氮原子; Y是硫原子，氧原子或被取代或未取代的低级烷基取代的氮原子; R1是氢原子，低级烷基或取代的低级烷基; R2是低级烷基，取代的低级烷基，低级亚烷基或取代的低级亚烷基; 并且A是含有至少一个氮原子的不饱和六元杂环，或其药学上可接受的盐。该衍生物具有优异的抗菌活性，可用作治疗各种细菌感染的药物。

4. 发明授权

US5607927A Cephalosporin derivative 失效
标题翻译：头孢菌素衍生物
公开(公告)号：US5607927A
公开(公告)日：1997-03-04
申请号：US385363
申请日：1995-02-07
申请人： Masaki Tsushima , Katsuyoshi Iwamatsu , Atsushi Tamura , Seiji Shibahara
发明人： Masaki Tsushima , Katsuyoshi Iwamatsu , Atsushi Tamura , Seiji Shibahara
IPC分类号： A61K31/545 , A61K31/546 , A61P31/04 , C07D501/00 , C07D501/59 , C07D519/00 , C07D519/06 , C07D501/36
CPC分类号： C07D501/00 , Y02P20/55
摘要： An aminothiazolyl- or aminothiadiazolyl-cephalosporin derivative represented by the following general formula (I) which has a condensed-ring thio group as a 3-positioned substituent group that contains a thiazolylthio group, an oxazolylthio group or a heterocyclic ring thereof as one of the ring components. The compound according to the present invention has excellent activities to inhibit growth of various bacteria, especially Gram-positive bacteria including methicillin-resistant Staphylococcus aureus (MRSA), and therefore, the antibacterial agent comprising, as an active ingredient, the inventive compound can be used as a therapeutic drug for the treatment of various bacterial infections. ##STR1##
摘要翻译：作为下述通式（I）表示的氨基噻唑基 - 或氨基噻二唑基 - 头孢菌素衍生物，其具有稠环硫基作为含有噻唑基硫基，恶唑基硫基或其杂环的3位取代基环组件。根据本发明的化合物具有优异的抑制各种细菌，特别是耐甲氧西林金黄色葡萄球菌（MRSA）的革兰氏阳性菌生长的活性，因此作为本发明化合物作为活性成分的抗菌剂可以是用作治疗各种细菌感染的治疗药物。

5. 发明授权

US5461044A Cephalosporin derivatives 失效
标题翻译：头孢菌素衍生物
公开(公告)号：US5461044A
公开(公告)日：1995-10-24
申请号：US369274
申请日：1995-01-05
申请人： Masaki Tsushima , Katsuyoshi Iwamatsu , Atsushi Tamura , Seiji Shibahara
发明人： Masaki Tsushima , Katsuyoshi Iwamatsu , Atsushi Tamura , Seiji Shibahara
IPC分类号： A61K31/545 , A61K31/546 , A61P31/04 , C07D501/00 , C07D501/59
CPC分类号： C07D501/00 , Y02P20/55
摘要： As new antibacterial agent are provided cephalosporin derivatives having a general formula (I): ##STR1## wherein R.sup.1 is a hydrogen atom, a lower alkyl group or a substituted lower alkyl group, R.sup.2 is a hydrogen atom or an ester-forming group easily cleavable by an esterase present in the digestive tracts, R.sup.3 and R.sup.4 may be the same and each is independently a hydrogen atom, a halogen atom, a lower alkyl group, a lower alkenyl group, hydroxyl group, amino group or a lower alkoxy group, and a pharmaceutically acceptable salt thereof.The cephalosporin derivative of formula (I) is useful as an orally or injectably administrable cephalosporin derivative which exhibits in combination a high antibacterial activity and a favorable characteristic capable of giving a high concentration of this compound in blood when administered.
摘要翻译：作为新的抗菌剂，提供具有通式（I）的头孢菌素衍生物：其中R 1为氢原子，低级烷基或取代的低级烷基，R 2为氢原子或酯形成可以通过存在于消化道中的酯酶容易地切割，R3和R4可以相同，各自独立地为氢原子，卤素原子，低级烷基，低级烯基，羟基，氨基或低级烷氧基基团及其药学上可接受的盐。式（I）的头孢菌素衍生物可用作口服或可注射给药的头孢菌素衍生物，其组合具有高的抗菌活性和在给药时能够在血液中给予高浓度该化合物的有利特征。

6. 发明授权

US5061702A Cephem compound as an antimicrobial agent 失效
标题翻译： CEPHEM化合物作为抗微生物剂
公开(公告)号：US5061702A
公开(公告)日：1991-10-29
申请号：US402814
申请日：1989-09-05
申请人： Kunio Atsumi , Katsuyoshi Iwamatsu , Kenji Sakagami , Takashi Yoshida , Haruo Yamamoto , Seiji Shibahara , Shigeharu Inouye
发明人： Kunio Atsumi , Katsuyoshi Iwamatsu , Kenji Sakagami , Takashi Yoshida , Haruo Yamamoto , Seiji Shibahara , Shigeharu Inouye
IPC分类号： C07D501/22 , A61K31/545 , A61K31/546 , A61P31/04 , C07D501/04 , C07D501/06 , C07D501/24
CPC分类号： C07D501/24 , Y02P20/55
摘要： A novel cephem compound which has antimicrobial activity is disclosed. The cephem compound is represented by the formula: ##STR1## wherein R.sup.1 represents a hydrogen atom or a carboxyl group; R.sup.2 and R.sup.3, which may be the same or different, each represent a hydrogen atom or a lower alkyl group of 1-3 carbon atoms; and R.sup.4 and R.sup.5, which may be the same or different, each represent a hydrogen atom or an acyl group; and pharmaceutically acceptable salts thereof.

7. 发明授权

US5075299A Cephalosporin compounds and antibacterial agents 失效
标题翻译： CEPHALOSPORIN化合物和抗菌剂
公开(公告)号：US5075299A
公开(公告)日：1991-12-24
申请号：US390580
申请日：1989-08-07
申请人： Kenji Sakagami , Katsuyoshi Iwamatsu , Kunio Atsumi , Seiji Shibahara
发明人： Kenji Sakagami , Katsuyoshi Iwamatsu , Kunio Atsumi , Seiji Shibahara
IPC分类号： C07D501/22 , A61K31/545 , A61K31/546 , A61P31/04 , C07D501/20 , C07D501/36
CPC分类号： C07D501/36 , C07D501/20 , Y02P20/55
摘要： Novel cephalosporin compounds represented by formula (I): ##STR1## wherein R.sup.1 represents a lower alkyl group which may optionally have a substituent; each of R.sup.2 and R.sup.3 independently represents a hydrogen atom or hydroxy group; and A represents a hydrogen atom or a residue of nucleophilic compound, and pharmacologically acceptable salts or esters thereof exhibit a potent antibacterial activity against gram positive and gram negative bacteria.

8. 发明授权

US5618795A Dibekacin derivatives and arbekacin derivatives active against resistant bacteria, and the production thereof 失效
标题翻译：对抗性细菌有活性的二比卡星衍生物和阿贝卡星衍生物及其生产
公开(公告)号：US5618795A
公开(公告)日：1997-04-08
申请号：US524644
申请日：1995-09-08
申请人： Shinichi Kondo , Seiji Shibahara , Takayuki Usui , Toshiaki Kudo , Shuichi Gomi , Atsushi Tamura , Yoko Ikeda , Daishiro Ikeda , Tomio Takeuchi
发明人： Shinichi Kondo , Seiji Shibahara , Takayuki Usui , Toshiaki Kudo , Shuichi Gomi , Atsushi Tamura , Yoko Ikeda , Daishiro Ikeda , Tomio Takeuchi
IPC分类号： C07H15/236 , A61K31/70
CPC分类号： C07H15/234
摘要： As new dibekacin derivatives and new arbekacin derivatives are now provided 2"-amino-2"-deoxydibekacin, 2"-amino-5,2"-dideoxydibekacin, 2"-amino-2"-deoxyarbekacin, 2"-amino-5,2"-dideoxyarbekacin, 2"-amino-5,2"-dideoxy-5-epi-fluoroarbekacin and 2"-amino-5,2"-dideoxy-5-epi-aminoarbekacin which all exhibit high antibacterial activity against a wide variety of gram-positive and gram-negative bacteria, including resistant bacteria such as methicillin-resistant Staphylococcus aureus and which are of low toxicity to mammals and are useful as antibacterial agent for treatment of bacterial infections.
摘要翻译：现在提供新的二卡辛衍生物和新的阿贝卡星衍生物2' - 氨基-2' - 脱氧胆碱，2“ - 氨基-5,2” - 脱氧胆酸，2“ - 氨基-2'-脱氧阿糖胞苷，2 “ - 氨基-5,2” - 双脱氧肉豆蔻素，2“ - 氨基-5,2” - 双脱氧-5-表 - 氟代贝卡星和2“ - 氨基-5,2” - 双脱氧-5-表所有这些都表现出对各种革兰氏阳性和革兰氏阴性细菌的高抗菌活性，包括耐甲氧西林金黄色葡萄球菌等抗性细菌，对哺乳动物毒性低，可用作细菌治疗的抗菌剂感染。

9. 发明授权

US5488038A Dibekacin derivatives and arbekacin derivatives active against resistant bacteria 失效
标题翻译：敌百虫素衍生物和对抗性细菌有活性的阿贝卡星衍生物
公开(公告)号：US5488038A
公开(公告)日：1996-01-30
申请号：US154002
申请日：1993-11-18
申请人： Shinichi Kondo , Seiji Shibahara , Takayuki Usui , Toshiaki Kudo , Shuichi Gomi , Atsushi Tamura , Yoko Ikeda , Daishiro Ikeda , Tomio Takeuchi
发明人： Shinichi Kondo , Seiji Shibahara , Takayuki Usui , Toshiaki Kudo , Shuichi Gomi , Atsushi Tamura , Yoko Ikeda , Daishiro Ikeda , Tomio Takeuchi
IPC分类号： C07H15/236 , A61K31/70 , C07H15/22
CPC分类号： C07H15/234
摘要： As new dibekacin derivatives and new arbekacin derivatives are now provided 2"-amino-2"-deoxydibekacin, 2"-amino-5,2"-dideoxydibekacin, 2"-amino-2"-deoxyarbekacin, 2"-amino-5,2"-dideoxyarbekacin, 2"-amino-5,2"-dideoxy-5-epi-fluoroarbekacin and 2"-amino-5,2"-dideoxy-5-epi-aminoarbekacin which all exhibit high antibacterial activity against a wide variety of gram-positive and gram-negative bacteria, including resistant bacteria such as methicillin-resistant Staphylococcus aureus and which are of low toxicity to mammals and are useful as antibacterial agent for treatment of bacterial infections.
摘要翻译：现在提供新的二卡辛衍生物和新的阿贝卡星衍生物2' - 氨基-2' - 脱氧胆碱，2“ - 氨基-5,2” - 脱氧胆酸，2“ - 氨基-2'-脱氧阿糖胞苷，2 “ - 氨基-5,2” - 双脱氧肉豆蔻素，2“ - 氨基-5,2” - 双脱氧-5-表 - 氟代贝卡星和2“ - 氨基-5,2” - 双脱氧-5-表所有这些都表现出对各种革兰氏阳性和革兰氏阴性细菌的高抗菌活性，包括耐甲氧西林金黄色葡萄球菌等抗性细菌，对哺乳动物毒性低，可用作细菌治疗的抗菌剂感染。

10. 发明授权

US5631257A Benzoxazole derivatives 失效
标题翻译：苯并恶唑衍生物
公开(公告)号：US5631257A
公开(公告)日：1997-05-20
申请号：US487697
申请日：1995-06-07
申请人： Katsuyoshi Iwamatsu , Yasuo Sato , Masaaki Izumi , Fukio Konno , Seiji Shibahara , Shigeharu Inoye , Koichi Shudo , Kazuko Amano
发明人： Katsuyoshi Iwamatsu , Yasuo Sato , Masaaki Izumi , Fukio Konno , Seiji Shibahara , Shigeharu Inoye , Koichi Shudo , Kazuko Amano
IPC分类号： A61K31/42 , A61K31/423 , A61K31/495 , A61K31/496 , A61K31/55 , A61P1/00 , A61P1/08 , A61P1/14 , A61P25/04 , A61P25/18 , A61P25/20 , A61P25/22 , A61P43/00 , C07D263/58 , C07D263/60 , C07D487/10 , C07D401/00 , C07D419/00
CPC分类号： C07D263/58 , C07D263/60 , C07D487/10
摘要： A benzoxazole derivative of the formula (1) or (2) which has an alicyclic diamine group at the 2-position: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, X.sup.-, m and n are defined herein. The compound shows excellent 5-HT.sub.3 receptor antagonism and is useful as an antiemetic agent, a peristalsis controlling agent, an analgesic agent, an antianxiety agent and a schizophrenia treating agent.
摘要翻译：（2）中具有脂环族二胺基团的式（1）或（2）的苯并恶唑衍生物：其中R1，R2，R3，R4，R5，R6， X，m和n在本文中定义。该化合物显示优异的5-HT 3受体拮抗作用，可用作止吐剂，蠕动控制剂，止痛剂，抗焦虑剂和精神分裂症治疗剂。

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