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：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：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：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.

公开(公告)号：US5190951A

公开(公告)日：1993-03-02

申请号：US773432

申请日：1991-10-09

申请人： Hiroshi Hasegawa ,  Kazuo Isomae ,  Takeshi Kotsugai ,  Noriaki Shioiri ,  Kumiko Sekine ,  Naokata Taido ,  Susumu Sato ,  Tadayuki Kuraishi

发明人： Hiroshi Hasegawa ,  Kazuo Isomae ,  Takeshi Kotsugai ,  Noriaki Shioiri ,  Kumiko Sekine ,  Naokata Taido ,  Susumu Sato ,  Tadayuki Kuraishi

IPC分类号： C07D219/06 ,  C07D221/16 ,  C07D401/06 ,  C07D471/04

CPC分类号： C07D401/06 ,  C07D219/06 ,  C07D221/16 ,  C07D471/04

摘要： Quinoline derivatives of the formula, ##STR1## wherein > A represents a group >N--(CH.sub.2).sub.n --, >C.dbd., >C.dbd.CH(CH.sub.2).sub.n --, or >CH(CH.sub.2).sub.n --, wherein n is an integer of 0-7; Y represents a group >C.dbd.O or >CHOH, R.sup.1 is a hydrogen atom, a halogen atom, an alkyl group, an alkoxy group, or an alkylthio group, R.sup.2 is a hydrogen atom, a halogen atom, an alkyl group, a hydroxy group, an alkoxy group, a phenyl group which may have a substituent, a phenoxy group, an alkanoyloxy group, or an amino group which may have a substituent, R.sup.3 is a hydrogen atom, a halogen atom, an alkyl group, or an alkoxy group, and m is an integer of 1-3. The compounds and their salts exhibit a superior antiacetylcholinesterase activity with no side effects and are effective for the prevention or cure of senile dementia or memory disturbance.

公开(公告)号：US5159091A

公开(公告)日：1992-10-27

申请号：US596323

申请日：1990-10-12

申请人： Tadatoshi Kuriyama ,  Masaki Ogawa ,  Susumu Sato ,  Naokata Taido ,  Tadayuki Kuraishi

发明人： Tadatoshi Kuriyama ,  Masaki Ogawa ,  Susumu Sato ,  Naokata Taido ,  Tadayuki Kuraishi

IPC分类号： C07J5/00 ,  C07J7/00 ,  C07J21/00 ,  C07J31/00 ,  C07J75/00

CPC分类号： C07J7/0045 ,  C07J21/00 ,  C07J31/006 ,  C07J5/0053

摘要： A process for preparing 21-desoxyprednisolone 17-esters of formula (IV) is disclosed. ##STR1## The process comprises reacting a prednisolone 17.alpha.,21-cyclic orthoester with an acid in a 40-60% lower alcohol solution to produce a prednisolone 17-ester, sulfonylating the prednisolone 17-ester into a prednisolone 17-ester 21-sulfonate, and reacting the sulfonate with an alkali metal iodide in methyl ethyl ketone in the presence of a lower fatty acid to produce the compound of formula (IV). The process ensures economical industrial production of high purity 21-desoxyprednisolone 17-esters, an excellent local anti-inflammatory medicine, in a high yield by simple procedures.

公开(公告)号：US5231101A

公开(公告)日：1993-07-27

申请号：US821803

申请日：1992-01-17

申请人： Haruyoshi Honda ,  Hiroyuki Mizuno ,  Kinichi Mogi ,  Yoshikuni Ito ,  Yasushi Kaneko ,  Naokata Taido ,  Susumu Sato ,  Tadayuki Kuraishi

发明人： Haruyoshi Honda ,  Hiroyuki Mizuno ,  Kinichi Mogi ,  Yoshikuni Ito ,  Yasushi Kaneko ,  Naokata Taido ,  Susumu Sato ,  Tadayuki Kuraishi

IPC分类号： A61K31/445 ,  A61K31/4427 ,  A61P37/08 ,  A61P43/00 ,  C07D401/04 ,  C07D401/14

CPC分类号： C07D401/04

摘要： Benzo[5,6]cyclohepta[1,2-b]pyridine derivatives of the following formula: ##STR1## wherein R.sup.1 represents a cyano, carbamoyl, alkylsulfoxy, alkylsulfonyl, tetrazolyl or sulfonic acid group, and R.sup.2 represents a hydrogen atom, a cyano, phenyl, aralkyl, alkoxycarbonylalkyl, aminoalkylcarbamoylalkyl or lower alkyl group, or a group ##STR2## or --X--R.sub.4, X being an oxygen or sulfur atom, R.sup.3 standing for a hydrogen atom or a substituted or unsubstituted lower alkyl, phenyl or aralkyl group, and R.sup.4 being a substituted or unsubstituted lower alkyl, phenyl or aralkyl group or an aminoalkyl group, and salts thereof. Antiallergic and antihistamic agents containing one of the above derivatives or salts as an active ingredient are also described.

公开(公告)号：US5300517A

公开(公告)日：1994-04-05

申请号：US53202

申请日：1993-04-28

申请人： Hiroshi Hasegawa ,  Kazuo Isomae ,  Takeshi Kotsugai ,  Noriaki Shioiri ,  Kumiko Sekine ,  Naokata Taido ,  Susumu Sato ,  Tadayuki Kuraishi

发明人： Hiroshi Hasegawa ,  Kazuo Isomae ,  Takeshi Kotsugai ,  Noriaki Shioiri ,  Kumiko Sekine ,  Naokata Taido ,  Susumu Sato ,  Tadayuki Kuraishi

IPC分类号： C07D219/06 ,  C07D221/16 ,  C07D401/06 ,  C07D471/04 ,  A61K31/445 ,  C07D401/04

CPC分类号： C07D401/06 ,  C07D219/06 ,  C07D221/16 ,  C07D471/04

摘要： Piperidine compounds of formula II: ##STR1## that exhibit anticholinesterase activity and are effective in treating dementia.

摘要翻译： 具有抗胆碱酯酶活性并有效治疗痴呆的式II的哌啶化合物：IMAGE（II）。

公开(公告)号：US5240934A

公开(公告)日：1993-08-31

申请号：US946620

申请日：1992-09-18

申请人： Hiroshi Hasegawa ,  Kazuo Isomae ,  Takeshi Kotsugai ,  Noriaki Shioiri ,  Kumiko Sekine ,  Naokata Taido ,  Susumu Sato ,  Tadayuki Kuraishi

发明人： Hiroshi Hasegawa ,  Kazuo Isomae ,  Takeshi Kotsugai ,  Noriaki Shioiri ,  Kumiko Sekine ,  Naokata Taido ,  Susumu Sato ,  Tadayuki Kuraishi

IPC分类号： C07D219/06 ,  C07D221/16 ,  C07D401/06 ,  C07D471/04

CPC分类号： C07D401/06 ,  C07D219/06 ,  C07D221/16 ,  C07D471/04

摘要： Quinoline derivatives of the formula, ##STR1## wherein >A represents a group >N--(CH.sub.2).sub.n --, >C.dbd., >C.dbd.CH(CH.sub.2).sub.n --, or >CH(CH.sub.2).sub.n --, wherein n is an integer of 0-7; Y represents a group >C.dbd.O or >CHOH, R.sup.1 is a hydrogen atom, a halogen atom, an alkyl group, an alkoxy group, or an alkylthio group, R.sup.2 is a hydrogen atom, a halogen atom, an alkyl group, a hydroxy group, an alkoxy group, a phenyl group which may have a substituent, a phenoxy group, an alkanoyloxy group, or an amino group which may have a substituent, R.sup.3 is a hydrogen atom, a halogen atom, an alkyl group, or an alkoxy group, and m is an integer of 1-3. The compounds and their salts exhibit a superior anti-acetylcholinesterase activity with no side effects and are effective for the prevention or cure of senile dementia or memory disturbance.

摘要翻译： 其中> A表示基团> N-（CH 2）n - ，> C = C = CH（CH 2）n - 或> CH（CH 2）n - ，其中n为 0-7的整数; Y表示C = O或> CHOH基团，R1表示氢原子，卤素原子，烷基，烷氧基或烷硫基，R2表示氢原子，卤原子，烷基， 羟基，烷氧基，可以具有取代基的苯基，苯氧基，烷酰氧基或可以具有取代基的氨基，R3是氢原子，卤素原子，烷基或 烷氧基，m为1-3的整数。 化合物及其盐具有优异的抗乙酰胆碱酯酶活性，无副作用，对预防或治愈老年痴呆或记忆障碍有效。