公开(公告)号：US5430028A

公开(公告)日：1995-07-04

申请号：US185898

申请日：1994-01-26

申请人： Terumitsu Kaihoh ,  Sunao Takeda ,  Fujiko Konno ,  Akihiro Shibata ,  Masaru Matsumoto ,  Takemitsu Asaoka ,  Hideaki Matsuda ,  Tadayuki Kuraishi

发明人： Terumitsu Kaihoh ,  Sunao Takeda ,  Fujiko Konno ,  Akihiro Shibata ,  Masaru Matsumoto ,  Takemitsu Asaoka ,  Hideaki Matsuda ,  Tadayuki Kuraishi

IPC分类号： A61K31/47 ,  A61K31/495 ,  C07D215/56 ,  C07D401/04 ,  A61K31/55 ,  A61K31/505 ,  C07D243/00 ,  C07D243/08

CPC分类号： C07D215/56 ,  A61K31/47 ,  A61K31/495 ,  C07D401/04

摘要： A 5-aminoquinolone carboxylic acid derivative represented by the following general formula (1): ##STR1## wherein R.sup.1 means a hydrogen atom, an amino group, a linear or branched alkyl group having 1-5 carbon atoms and an alkylamino group containing a linear or branched alkyl group having 1-5 carbon atoms, R.sup.2 denotes a hydrogen atom or a linear or branched alkyl group having 1-5 carbon atoms, X stands for a halogen atom, Y means CH.sub.2, NH, CHR.sup.3 NR.sup.3, (R.sup.3 denoting a linear or branched alkyl group having 1-5 carbon atoms) or an oxygen atom, and Z stands for an oxygen atom or 2 hydrogen atoms, or a salt thereof, and an antibacterial agent containing such a derivative or salt as an active ingredient.The derivative or salt thereof exhibits strong anti-bacterial activities against Grampositive bacteria including tolerant bacteria, and is satisfactorily absorbed in a living body.

摘要翻译： PCT No.PCT / JP93 / 00694 Sec。 371日期1994年1月26日 102（e）日期1994年1月26日PCT提交1993年5月25日PCT公布。 出版物WO93 / 24460 PCT 日期：1993年12月9日，下列通式（1）表示的5-氨基喹诺酮羧酸衍生物：其中R 1表示氢原子，氨基，直链或支链烷基， 5个碳原子和含有1-5个碳原子的直链或支链烷基的烷基氨基，R2表示氢原子或具有1-5个碳原子的直链或支链烷基，X表示卤素原子，Y表示CH2 ，NH，CHR 3 NR 3，（R3表示具有1-5个碳原子的直链或支链烷基）或氧原子，Z表示氧原子或2个氢原子，或其盐，以及含有这些的抗菌剂 衍生物或盐作为活性成分。 其衍生物或盐对包括耐受性细菌的细菌性细菌表现出强的抗菌活性，并且令人满意地吸收在生物体内。

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.

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。

公开(公告)号：US6124347A

公开(公告)日：2000-09-26

申请号：US162451

申请日：1998-09-29

申请人： Fumio Ishii ,  Haruyoshi Honda ,  Fujiko Konno ,  Tomomi Okada ,  Terumitsu Kaihoh ,  Yoshihiro Nagao ,  Susumu Sato ,  Hideaki Matsuda

发明人： Fumio Ishii ,  Haruyoshi Honda ,  Fujiko Konno ,  Tomomi Okada ,  Terumitsu Kaihoh ,  Yoshihiro Nagao ,  Susumu Sato ,  Hideaki Matsuda

IPC分类号： A61K31/35 ,  A61K31/352 ,  A61P3/08 ,  A61P3/10 ,  A61P43/00 ,  C07D311/58 ,  C07D311/64 ,  A61K31/353 ,  C07D311/60

CPC分类号： C07D311/58

摘要： Disclosed are chromene derivatives represented by the following formula: ##STR1## wherein R.sup.1 s represent alkyl, alkoxy or like groups, R.sup.2 represents a hydrogen atom or an alkyl group, R.sup.3 represents a substituted or unsubstituted phenyl, naphthyl or heterocyclic group, and m stands for an integer of from 0 to 4, and their salts; and pharmaceuticals containing them as effective ingredients. The chromene derivatives and their salts show excellent AGE formation inhibitory action and are useful as preventives and therapeutics for diabetic complications.

摘要翻译： 公开了由下式表示的色烯衍生物：其中R 1表示烷基，烷氧基或类似基团，R 2表示氢原子或烷基，R 3表示取代或未取代的苯基，萘基或杂环基，m表示 0至4，及其盐; 和含有它们作为有效成分的药物。 色烯衍生物及其盐显示优异的AGE形成抑制作用，并且可用作糖尿病并发症的预防剂和治疗剂。

公开(公告)号：US06174900B1

公开(公告)日：2001-01-16

申请号：US09332444

申请日：1999-06-14

申请人： Tomomi Okada ,  Fujiko Konno ,  Terumitsu Kaihoh ,  Masago Ishikawa ,  Yoshinori Takahashi ,  Hiroyuki Mizuno ,  Haruyoshi Honda ,  Susumu Sato ,  Hideaki Matsuda

发明人： Tomomi Okada ,  Fujiko Konno ,  Terumitsu Kaihoh ,  Masago Ishikawa ,  Yoshinori Takahashi ,  Hiroyuki Mizuno ,  Haruyoshi Honda ,  Susumu Sato ,  Hideaki Matsuda

IPC分类号： A61K31445

CPC分类号： C07D401/12 ,  C07D211/58 ,  C07D409/12

摘要： Disclosed herein is a substituted piperidine derivative represented by the following general formula (1): wherein R1 means an aryl or heteroaryl group which may have at least one substituent, R2 denotes an alkyl, alkenyl or aralkyl group, R3 stands for a hydrogen atom or an alkyl group, and R4 is a hydrogen atom, an alkyl group, or an aryl, heteroaryl, aralkyl, aralkenyl or heteroaralkyl group which may have at least one substituent, or a salt thereof. A medicine including this compound is also disclosed. The compound has excellent anticholinergic effect and calcium antagonism and inhibits reflex bladder contraction and is hence useful for prophylaxis of and treatment for a urinary disturbance such as pollakiuria.

摘要翻译： 本文公开了由以下通式（1）表示的取代的哌啶衍生物：其中R 1表示可具有至少一个取代基的芳基或杂芳基，R 2表示烷基，烯基或芳烷基，R 3表示氢原子或 烷基，可以具有至少一个取代基的芳基，杂芳基，芳烷基，芳烯基或杂芳烷基，或其盐。 还公开了包含该化合物的药物。 该化合物具有优异的抗胆碱能作用和钙拮抗作用并抑制反射膀胱收缩，因此可用于预防和治疗尿频紊乱如尿频。

公开(公告)号：US5968956A

公开(公告)日：1999-10-19

申请号：US672058

申请日：1996-06-26

申请人： Tomomi Okada ,  Fujiko Konno ,  Terumitsu Kaihoh ,  Masago Ishikawa ,  Yoshinori Takahashi ,  Hiroyuki Mizuno ,  Haruyoshi Honda ,  Susumu Sato ,  Hideaki Matsuda

发明人： Tomomi Okada ,  Fujiko Konno ,  Terumitsu Kaihoh ,  Masago Ishikawa ,  Yoshinori Takahashi ,  Hiroyuki Mizuno ,  Haruyoshi Honda ,  Susumu Sato ,  Hideaki Matsuda

IPC分类号： C07D211/58 ,  C07D401/12 ,  C07D409/12 ,  A61K31/445 ,  C07D211/56

CPC分类号： C07D401/12 ,  C07D211/58 ,  C07D409/12

摘要： Disclosed herein is a substituted piperidine derivative represented by the following general formula (1): ##STR1## wherein R.sup.1 means an aryl or heteroaryl group which may have at least one substituent, R.sup.2 denotes an alkyl, alkenyl or aralkyl group, R.sup.3 stands for a hydrogen atom or an alkyl group, and R.sup.4 is a hydrogen atom, an alkyl group, or an aryl, heteroaryl, aralkyl, aralkenyl or heteroaralkyl group which may have at least one substituent, or a salt thereof. A medicine including this compound is also disclosed. The compound has excellent anticholinergic effect and calcium antagonism and inhibits reflex bladder contraction and is hence useful for prophylaxis of and treatment for a urinary disturbance such as pollakiuria.

摘要翻译： 本文公开了由以下通式（1）表示的取代的哌啶衍生物：其中R 1表示可具有至少一个取代基的芳基或杂芳基，R 2表示烷基，烯基或芳烷基，R 3表示氢原子或 烷基，可以具有至少一个取代基的芳基，杂芳基，芳烷基，芳烯基或杂芳烷基，或其盐。 还公开了包含该化合物的药物。 该化合物具有优异的抗胆碱能作用和钙拮抗作用并抑制反射膀胱收缩，因此可用于预防和治疗尿频紊乱如尿频。

公开(公告)号：US06958353B2

公开(公告)日：2005-10-25

申请号：US10258610

申请日：2001-06-08

申请人： Fujiko Konno ,  Yoshihiro Nagao ,  Kazuo Isomae ,  Mari Ohtsuka ,  Yoshiyuki Takahashi ,  Fumio Ishii ,  Hiroyuki Hirota ,  Sunao Takeda ,  Noriyuki Kawamoto ,  Haruyoshi Honda ,  Susumu Sato

发明人： Fujiko Konno ,  Yoshihiro Nagao ,  Kazuo Isomae ,  Mari Ohtsuka ,  Yoshiyuki Takahashi ,  Fumio Ishii ,  Hiroyuki Hirota ,  Sunao Takeda ,  Noriyuki Kawamoto ,  Haruyoshi Honda ,  Susumu Sato

IPC分类号： A61P19/02 ,  A61P19/10 ,  A61P29/00 ,  A61P43/00 ,  C07D233/22 ,  C07D233/60 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/14 ,  C07D409/14 ,  C07D521/00 ,  A61K31/4178 ,  A61K31/444

CPC分类号： C07D401/14 ,  C07D231/12 ,  C07D233/22 ,  C07D233/56 ,  C07D249/08 ,  C07D401/12 ,  C07D403/12 ,  C07D405/14 ,  C07D409/14

摘要： The invention is directed to an imidazole derivative represented by formula (1): wherein each of R1 and R2 represents an aryl group, a heteroaryl group, etc.; each of A, X1, and X2 represents N or CH; each of Y and Z represents O, S, etc.; each of R3, R4, and R5 represents a hydrogen atom, an alkyl group, etc.; m is a number of 1 to 4; and n is a number of 0 to 4, or a salt thereof. The invention is also directed to a drug containing the derivative or the salt as an active ingredient. These compounds exert excellent effects of inhibiting production of NO and IL-6 and are useful for preventing or treating diseases induced by overproduction of NO and IL-6.

摘要翻译： 本发明涉及由式（1）表示的咪唑衍生物：其中R 1和R 2各自表示芳基，杂芳基等; A，X 1和X 2各自表示N或CH; Y和Z各自表示O，S等; R 3，R 4和R 5各自表示氢原子，烷基等; m是1到4的数字; n为0〜4的数，或其盐。 本发明还涉及含有衍生物或盐作为活性成分的药物。 这些化合物具有抑制NO和IL-6产生的优异效果，可用于预防或治疗由过量产生NO和IL-6引起的疾病。