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：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：US5986144A

公开(公告)日：1999-11-16

申请号：US311057

申请日：1999-05-14

申请人： Minoru Tokizawa ,  Sunao Takeda ,  Yasushi Kaneko ,  Hiromichi Eto ,  Kazuya Ishida ,  Kazunori Maebashi ,  Masaru Matsumoto ,  Takemitsu Asaoka ,  Susumu Sato ,  Hideaki Matsuda

发明人： Minoru Tokizawa ,  Sunao Takeda ,  Yasushi Kaneko ,  Hiromichi Eto ,  Kazuya Ishida ,  Kazunori Maebashi ,  Masaru Matsumoto ,  Takemitsu Asaoka ,  Susumu Sato ,  Hideaki Matsuda

IPC分类号： C07D249/08 ,  C07D303/34 ,  C07D521/00 ,  C07C323/07

CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D303/34

摘要： Described is a triazole derivative represented by the formula (1) or salt thereof, preparation process thereof, preparation intermediates represented by the formulas (2) and (3), and a pharmaceutical comprising the compound represented by the formula (1) or salt thereof. wherein n stands for 0, 1 or 2, X.sup.1 represents H or F and Y.sup.1 and Y.sup.2 each independently represents H, halogen or CF.sub.3.

摘要翻译： 描述由式（1）表示的三唑衍生物或其盐，其制备方法，由式（2）和（3）表示的制备中间体，以及包含式（1）表示的化合物或其盐的药物 。 其中n表示0,1或2，X 1表示H或F，Y 1和Y 2各自独立地表示H，卤素或CF 3。

公开(公告)号：US6002028A

公开(公告)日：1999-12-14

申请号：US311058

申请日：1999-05-14

申请人： Minoru Tokizawa ,  Sunao Takeda ,  Yasushi Kaneko ,  Hiromichi Eto ,  Kazuya Ishida ,  Kazunori Maebashi ,  Masaru Matsumoto ,  Takemitsu Asaoka ,  Susumu Sato ,  Hideaki Matsuda

发明人： Minoru Tokizawa ,  Sunao Takeda ,  Yasushi Kaneko ,  Hiromichi Eto ,  Kazuya Ishida ,  Kazunori Maebashi ,  Masaru Matsumoto ,  Takemitsu Asaoka ,  Susumu Sato ,  Hideaki Matsuda

IPC分类号： C07D303/34 ,  C07D521/00

CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D303/34

摘要： Described is a triazole derivative represented by the formula (1) or salt thereof, preparation process thereof, preparation intermediates represented by the formulas (2) and (3), and a pharmaceutical comprising the compound represented by the formula (1) or salt thereof. ##STR1## wherein n stands for 0, 1 or 2, X.sup.1 represents H or F and Y.sup.1 and Y.sup.2 each independently represents H, halogen or CF.sub.3.

公开(公告)号：US5939448A

公开(公告)日：1999-08-17

申请号：US872159

申请日：1997-06-10

申请人： Minoru Tokizawa ,  Sunao Takeda ,  Yasushi Kaneko ,  Hiromichi Eto ,  Kazuya Ishida ,  Kazunori Maebashi ,  Masaru Matsumoto ,  Takemitsu Asaoka ,  Susumu Sato ,  Hideaki Matsuda

发明人： Minoru Tokizawa ,  Sunao Takeda ,  Yasushi Kaneko ,  Hiromichi Eto ,  Kazuya Ishida ,  Kazunori Maebashi ,  Masaru Matsumoto ,  Takemitsu Asaoka ,  Susumu Sato ,  Hideaki Matsuda

IPC分类号： C07D249/08 ,  C07D303/34 ,  C07D521/00 ,  A61K31/41

CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D303/34

摘要： Described is a triazole derivative represented by the formula (1): wherein R represents a hydrogen atom, an alkyl group, an aralkyl group or an acyl group, n stands for 0 to 2 and m stands for 1 to 5 or salt thereof, and a pharmaceutical containing the derivative or salt as an effective ingredient.

摘要翻译： 描述了由式（1）表示的三唑衍生物：其中R表示氢原子，烷基，芳烷基或酰基，n表示0至2，m表示1至5或其盐， 含有衍生物或盐作为有效成分的药物。

公开(公告)号：US6063945A

公开(公告)日：2000-05-16

申请号：US327516

申请日：1999-06-08

申请人： Minoru Tokizawa ,  Sunao Takeda ,  Yasushi Kaneko ,  Hiromichi Eto ,  Kazuya Ishida ,  Kazunori Maebashi ,  Masaru Matsumoto ,  Takemitsu Asaoka ,  Susumu Sato ,  Hideaki Matsuda

发明人： Minoru Tokizawa ,  Sunao Takeda ,  Yasushi Kaneko ,  Hiromichi Eto ,  Kazuya Ishida ,  Kazunori Maebashi ,  Masaru Matsumoto ,  Takemitsu Asaoka ,  Susumu Sato ,  Hideaki Matsuda

IPC分类号： C07D249/08 ,  C07D303/34 ,  C07D521/00

CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D303/34

摘要： A compound having formula (2): ##STR1## wherein R represents hydrogen, a straight or branched C.sub.1-10 alkyl group, a C.sub.7-11 aralkyl group or a C.sub.2-10 carboacyl group and m stands for 1 to 5.

摘要翻译： 具有式（2）的化合物：其中R表示氢，直链或支链C 1-10烷基，C 7-11芳烷基或C 2-10烷酰基，m代表1至5。

公开(公告)号：US5945438A

公开(公告)日：1999-08-31

申请号：US767694

申请日：1996-12-17

申请人： Minoru Tokizawa ,  Sunao Takeda ,  Yasushi Kaneko ,  Hiromichi Eto ,  Kazuya Ishida ,  Kazunori Maebashi ,  Masaru Matsumoto ,  Takemitsu Asaoka ,  Susumu Sato ,  Hideaki Matsuda

发明人： Minoru Tokizawa ,  Sunao Takeda ,  Yasushi Kaneko ,  Hiromichi Eto ,  Kazuya Ishida ,  Kazunori Maebashi ,  Masaru Matsumoto ,  Takemitsu Asaoka ,  Susumu Sato ,  Hideaki Matsuda

IPC分类号： C07D249/08 ,  C07D303/34 ,  C07D521/00 ,  A61K31/41

CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D303/34

摘要： Described is a triazole derivative represented by the formula (1) or salt thereof, preparation process thereof, preparation intermediates represented by the formulas (2) and (3), and a pharmaceutical comprising the compound represented by the formula (1) or salt thereof. ##STR1## wherein n stands for 0, 1 or 2, X.sup.1 represents H or F and Y.sup.1 and Y.sup.2 each independently represents H, halogen or CF.sub.3.

摘要翻译： 描述由式（1）表示的三唑衍生物或其盐，其制备方法，由式（2）和（3）表示的制备中间体，以及包含式（1）表示的化合物或其盐的药物 。 其中n表示0,1或2，X 1表示H或F，Y 1和Y 2各自独立地表示H，卤素或CF 3。

公开(公告)号：US6008239A

公开(公告)日：1999-12-28

申请号：US135163

申请日：1998-08-17

申请人： Yasushi Kaneko ,  Sunao Takeda ,  Minoru Tokizawa ,  Hiromichi Eto ,  Kazuya Ishida ,  Kazunori Maebashi ,  Masaru Matsumoto ,  Takemitsu Asaoka ,  Susumu Sato

发明人： Yasushi Kaneko ,  Sunao Takeda ,  Minoru Tokizawa ,  Hiromichi Eto ,  Kazuya Ishida ,  Kazunori Maebashi ,  Masaru Matsumoto ,  Takemitsu Asaoka ,  Susumu Sato

IPC分类号： A01N43/653 ,  C07D249/08 ,  C07D521/00 ,  A61K31/505

CPC分类号： C07D231/12 ,  A01N43/653 ,  C07D233/56 ,  C07D249/08

摘要： Described is a triazole derivative represented by the formula (1): ##STR1## wherein R.sup.1 represents a lower alkyl group or an aralkyl group, R.sup.2 represents a hydrogen atom, a lower alkyl group, an aralkyl group or an acyl group, X.sup.1 and X.sup.2 are the same or different and each independently represents a hydrogen atom, a halogen atom or a trifluoromethyl group, n stands for an integer of 0 to 2 and m stands for an integer of 1 to 5, or salt thereof; and also a pharmaceutical comprising the derivative or salt thereof as an effective ingredient. The compound as described above has a high antimycotic activity and is useful for the prevention and treatment of mammalian mycotic infections.

摘要翻译： 描述了由式（1）表示的三唑衍生物：其中R1表示低级烷基或芳烷基，R2表示氢原子，低级烷基，芳烷基或酰基，X1和X2相同 或不同，各自独立地表示氢原子，卤素原子或三氟甲基，n表示0〜2的整数，m表示1〜5的整数，或其盐。 以及包含其衍生物或其盐作为有效成分的药物。 如上所述的化合物具有高的抗真菌活性，并且可用于预防和治疗哺乳动物真菌感染。

公开(公告)号：US06194592B1

公开(公告)日：2001-02-27

申请号：US09551569

申请日：2000-04-18

申请人： Sunao Takeda ,  Yasushi Kaneko ,  Minoru Tokizawa ,  Hiromichi Eto ,  Kazuya Ishida ,  Kazunori Maebashi ,  Masaru Matsumoto ,  Takemitsu Asaoka ,  Susumu Sato

发明人： Sunao Takeda ,  Yasushi Kaneko ,  Minoru Tokizawa ,  Hiromichi Eto ,  Kazuya Ishida ,  Kazunori Maebashi ,  Masaru Matsumoto ,  Takemitsu Asaoka ,  Susumu Sato

IPC分类号： C07D30334

CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D303/48

摘要： Described is a triazole derivative represented by the formula (1): wherein R1 represents a hydrogen atom, a lower alkyl group or an aralkyl group, X1 and X2 are the same or different and each independently represents a hydrogen atom, a halogen atom or a halogenoalkyl and n stands for an integer of 0 to 2, or salt thereof; a preparation process of said compound and a pharmaceutical comprising said compound as an effective ingredient. The compound as described above has high antimycotic activity and is useful for the prevention and treatment of mammalian mycotic infections.