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公开(公告)号:US5385900A
公开(公告)日:1995-01-31
申请号:US149134
申请日:1993-11-08
申请人: Fujiko Konno , Akihiro Shibata , Hideaki Matsuda , Takemitsu Asaoka , Ryuichi Kawahara , Naokata Taido , Tadayuki Kuraishi , Sunao Takeda
发明人: Fujiko Konno , Akihiro Shibata , Hideaki Matsuda , Takemitsu Asaoka , Ryuichi Kawahara , Naokata Taido , Tadayuki Kuraishi , Sunao Takeda
IPC分类号: A61K31/55 , A61P31/04 , C07D215/56 , C07D401/04 , C07D413/04 , C07D417/04 , C07D243/08
CPC分类号: C07D215/56 , C07D401/04 , C07D413/04 , C07D417/04
摘要: A quinolone carboxylic acid derivative having the following formula (1), ##STR1## wherein R.sup.1 is a hydrogen atom, an alkyl group, an aralkyl group, an ester residual group which can be hydrolyzed in living bodies, R.sup.2 is a hydrogen atom or an amino group which may be substituted by one or two lower alkyl groups, X is a hydrogen atom or a halogen atom, Y is CH.sub.2, O, S, SO, SO.sub.2, or N--R.sup.3, wherein R.sup.3 is a hydrogen atom or a lower alkyl group, and Z is an oxygen atom or two hydrogen atoms; or a salt thereof; and an antimicrobial agent comprising the same. The compound exhibits a superior antimicrobial activity, especially against gram positive microorganisms, and is thus useful for the treatments and prevention of various infectious diseases in clinics.
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公开(公告)号:US5447926A
公开(公告)日:1995-09-05
申请号:US305977
申请日:1994-09-16
申请人: Fujiko Konno , Akihiro Shibata , Hideaki Matsuda , Takemitsu Asaoka , Ryuichi Kawahara , Naokata Taido , Tasdayuki Kuraishi , Sunao Takeda
发明人: Fujiko Konno , Akihiro Shibata , Hideaki Matsuda , Takemitsu Asaoka , Ryuichi Kawahara , Naokata Taido , Tasdayuki Kuraishi , Sunao Takeda
IPC分类号: A61K31/55 , A61P31/04 , C07D215/56 , C07D401/04 , C07D413/04 , C07D417/04 , C07D401/10 , C07D417/10
CPC分类号: C07D215/56 , C07D401/04 , C07D413/04 , C07D417/04
摘要: A quinolone carboxylic acid derivative having the following formula (1), ##STR1## wherein R.sup.1 is a hydrogen atom, an alkyl group, an aralkyl group, an ester residual group which can be hydrolyzed in living bodies, R.sup.2 is a hydrogen atom or an amino group which may be substituted by one or two lower alkyl groups, X is a hydrogen atom or a halogen atom, Y is CH.sub.2, O, S, SO, SO.sub.2, or N--R.sup.3, wherein R.sup.3 is a hydrogen atom or a lower alkyl group, and Z is an oxygen atom or two hydrogen atoms; or a salt thereof; and an antimicrobial agent comprising the same. The compound exhibits a superior antimicrobial activity, especially against gram positive microorganisms, and is thus useful for the treatments and prevention of various infectious diseases in clinics.
摘要翻译: 具有下式(1)的喹诺酮羧酸衍生物,其中R1是氢原子,烷基,芳烷基,可在活体中水解的酯残基,R2是氢 原子或可以被一个或两个低级烷基取代的氨基,X是氢原子或卤素原子,Y是CH 2,O,S,SO,SO 2或N-R 3,其中R 3是氢原子 或低级烷基,Z为氧原子或两个氢原子; 或其盐; 和包含该抗微生物剂的抗微生物剂。 该化合物具有优异的抗微生物活性,特别是抗革兰氏阳性微生物,因此可用于临床上各种感染性疾病的治疗和预防。
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公开(公告)号:US5324735A
公开(公告)日:1994-06-28
申请号:US807856
申请日:1992-01-17
申请人: Akihiro Shibata , Hideaki Matsuda , Takemitsu Asaoka , Masaru Matsumoto , Ryuichi Kawahara , Tatsuhiko Katori , Naokata Taido , Tadayuki Kuraishi
发明人: Akihiro Shibata , Hideaki Matsuda , Takemitsu Asaoka , Masaru Matsumoto , Ryuichi Kawahara , Tatsuhiko Katori , Naokata Taido , Tadayuki Kuraishi
IPC分类号: C07D215/56 , C07D401/04 , C07D215/233 , A01K31/47
CPC分类号: C07D215/56 , C07D401/04
摘要: The present invention relates to a quinolone carboxylic acid derivative represented by the following the formula (I), ##STR1## wherein R.sub.1 is a lower alkyl group, R.sub.2 is a hydrogen atom or a lower alkyl group, R.sub.3 is a hydrogen atom or a halogen atom, R.sub.4 and R.sub.5 together form a five- or six-membered ring which may contain hetero atoms or may have substituents, provided that a compound wherein R.sub.1 is a methyl group, R.sub.2 and R.sub.3 are hydrogen atom and ##STR2## is a piperazinyl group is excluded; or a salt thereof; to an antimicrobial agent comprising the same as an effective component; and to an intermediate for producing same.
摘要翻译: PCT No.PCT / JP90 / 00425 Sec。 371日期:1992年1月17日 102(e)日期1992年1月17日PCT 1990年3月29日PCT公布。 出版物WO91 / 01308 1991年2月7日。本发明涉及由下式(I)表示的喹诺酮羧酸衍生物,其中R1是低级烷基,R2是氢原子或低级烷基 基团,R 3是氢原子或卤素原子,R 4和R 5一起形成可含有杂原子或可以具有取代基的五元或六元环,条件是其中R 1是甲基,R 2和R 3是 氢原子和
是不包括的哌嗪基; 或其盐; 涉及包含其作为有效成分的抗微生物剂; 和用于生产它的中间体。 -
公开(公告)号:US5147886A
公开(公告)日:1992-09-15
申请号:US626545
申请日:1990-12-12
申请人: Minoru Tokizawa , Yoshihiko Kanamaru , Masaru Matsumoto , Takemitsu Asaoka , Hideaki Matsuda , Tadayuki Kuraishi , Kazunori Maebashi , Naokata Taido , Ryuichi Kawahara
发明人: Minoru Tokizawa , Yoshihiko Kanamaru , Masaru Matsumoto , Takemitsu Asaoka , Hideaki Matsuda , Tadayuki Kuraishi , Kazunori Maebashi , Naokata Taido , Ryuichi Kawahara
IPC分类号: C07D249/08 , C07D521/00
CPC分类号: C07D231/12 , C07D233/56 , C07D249/08
摘要: A triazole derivative is disclosed. The compound have a general formula, ##STR1## wherein R.sup.1 and R.sup.2 represent a hydrogen atom or a lower alkyl group, or R.sup.1 and R.sup.2 together form a lower alkylene group, R.sup.3 represents a lower alkyl group, and n denotes an integer of 0 to 2, provided that not both R.sup.1 and R.sup.2 are a hydrogen atom at the same time. The triazole derivatives and their salts are effective for curing or preventing deep-seated mycoses, e.g. mycotic meningitis, mycotic infectious diseases of respiratory organs, fungemia, and urinary tract mycosis.
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