公开(公告)号：US4740601A

公开(公告)日：1988-04-26

申请号：US941318

申请日：1986-12-15

申请人： Masaki Ogawa ,  Hideaki Matsuda ,  Takemitsu Asaoka ,  Junji Oono ,  Tatsuhiko Katori

发明人： Masaki Ogawa ,  Hideaki Matsuda ,  Takemitsu Asaoka ,  Junji Oono ,  Tatsuhiko Katori

IPC分类号： A01N43/50 ,  A61K31/415 ,  A61P31/04 ,  C07D233/60 ,  C07D405/06 ,  C07D405/12 ,  C07D521/00 ,  C07D233/04 ,  C07D233/54

CPC分类号： C07D231/12 ,  A01N43/50 ,  C07D233/56 ,  C07D249/08

摘要： An imidazole derivative having antimicrobial activities against bacteria, fungi, yeast, pathogenic plant fungi and the like represented by the following general formula (I): ##STR1## wherein R.sub.1 means a hydrogen or halogen atom or a lower alkyl group, R.sub.2 denotes a hydrogen atom or an alkyl, alkenyl, haloalkyl or substituted or unsubstituted benzyl group, R.sub.3 stands for a hydrogen or halogen atom, and R.sub.4 is a substituted or unsubstituted benzylthio group, a phenylthio, alkylthio, alkenylthio, furfurylthio, alkoxy or phenoxy group or a halogen atom; or an acid addition salt thereof.

摘要翻译： 由下列通式（I）表示的具有抗细菌，真菌，酵母，致病植物真菌等的抗微生物活性的咪唑衍生物：其中R1表示氢或卤原子或低级烷基，R2 表示氢原子或烷基，烯基，卤代烷基或取代或未取代的苄基，R3表示氢或卤素原子，R4表示取代或未取代的苄硫基，苯硫基，烷硫基，烯硫基，糠硫基，烷氧基或苯氧基 或卤素原子; 或其酸加成盐。

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：US4925953A

公开(公告)日：1990-05-15

申请号：US277308

申请日：1988-11-29

申请人： Minoru Tokizawa ,  Takemitsu Asaoka ,  Hideaki Matsuda ,  Tatsuhiko Katori

发明人： Minoru Tokizawa ,  Takemitsu Asaoka ,  Hideaki Matsuda ,  Tatsuhiko Katori

IPC分类号： C07D233/60 ,  C07D521/00

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

摘要： Novel imidazole derivatives and their acid adducts are disclosed. The imidazole derivatives are represented by formula: ##STR1## wherein R.sub.1 represents an alkyl group, R.sub.2 represents a hydrogen atom, an alkyl group which may have a substituent, or an aralkyl group which may have a substituent, provided that R.sub.1 and R.sub.2 are not both methyl groups at the same time. They have strong antimicrobial activity, especially against those fungi belonging to the genera Candida, Trichophyton, Microsporum, and Epidermorphyton, as well as against Gram-positive bacteria, and thus are useful as an antimicrobial agent.

公开(公告)号：US5082948A

公开(公告)日：1992-01-21

申请号：US484368

申请日：1990-02-22

申请人： Minoru Tokizawa ,  Takemitsu Asaoka ,  Hideaki Matsuda ,  Tatsuhiko Katori

发明人： Minoru Tokizawa ,  Takemitsu Asaoka ,  Hideaki Matsuda ,  Tatsuhiko Katori

IPC分类号： C07D233/60 ,  C07D521/00

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

摘要： Novel imidazole derivatives and their acid adducts are disclosed. The imidazole derivatives are represented by formula: ##STR1## wherein R.sub.1 represents an alkyl group, R.sub.2 represents a hydrogen atom, an alkyl group which may have a substituent, or an aralkyl group which may have a substituent, provided that R.sub.1 and R.sub.2 are not both methyl groups at the same time. They have strong antimicrobial activity, especially against those fungi belonging to the genera Candida, Trichophyton, Microsporum, and Epidermorphyton, as well as against Gram-positive bacteria, and thus is useful as an antimicrobial agent.

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：US5164513A

公开(公告)日：1992-11-17

申请号：US747632

申请日：1991-08-20

申请人： Minoru Tokizawa ,  Takemitsu Asaoka ,  Hideaki Matsuda ,  Tatsuhiko Kateri

发明人： Minoru Tokizawa ,  Takemitsu Asaoka ,  Hideaki Matsuda ,  Tatsuhiko Kateri

IPC分类号： C07D521/00

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

摘要： Novel imidazole derivatives and their acid adducts are disclosed. The imidazole derivatives are represented by formula: ##STR1## wherein R.sub.1 represents an alkyl group, R.sub.2 represents a hydrogen atom, an alkyl group which may have a substituent, or an aralkyl group which may have a substituent, provided that R.sub.1 and R.sub.2 are not both methyl groups at the same time. They have strong antimicrobial activity, especially against those fungi belonging to the genera Candida, Trichophyton, Microsporum, and Epidermorphyton, as well as against Gram-positive bacteria, and thus is useful as a antimicrobial agent.

摘要翻译： 公开了新的咪唑衍生物及其酸加成物。 咪唑衍生物由下式表示：其中R1表示烷基，R2表示氢原子，可以具有取代基的烷基或可具有取代基的芳烷基，条件是R1和 R2不同时同时为甲基。 它们具有很强的抗微生物活性，特别是针对属于假丝酵母属，毛癣菌属，微孢子虫属和表皮假单胞菌属的真菌，以及抗革兰氏阳性菌，因此可用作抗微生物剂。

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.

公开(公告)号：US4987144A

公开(公告)日：1991-01-22

申请号：US412152

申请日：1989-09-25

申请人： Yoshihiko Kanamaru ,  Minoru Tokizawa ,  Masaru Matsumoto ,  Takemitsu Asaoka ,  Hideaki Matsuda ,  Tadayuki Kuraishi

发明人： Yoshihiko Kanamaru ,  Minoru Tokizawa ,  Masaru Matsumoto ,  Takemitsu Asaoka ,  Hideaki Matsuda ,  Tadayuki Kuraishi

IPC分类号： A61K31/41 ,  A61P31/04 ,  A61P31/10 ,  C07D249/08 ,  C07D521/00

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

摘要： Disclosed herein is 1,3-bis(1,2,4-triazol-1-yl)-2-(4-trifluoromethylphenyl)propan-2-ol represented by the following formula (I): ##STR1## An antimycotic preparation containing the triazole compound (I) is also disclosed. Also disclosed is a method for the prevention and/treatment of a deep-seated mycosis of a human or mammal, which comprises administering an effective dose of the triazole compound (I) to the human or mammal.