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公开(公告)号:US4876359A
公开(公告)日:1989-10-24
申请号:US103415
申请日:1987-10-01
IPC分类号: C07K5/02
CPC分类号: C07K5/0222
摘要: Novel .gamma.-butyrolactone derivatives having strong ACE inhibitory activity are provided. They are represented by the following general formula (I): ##STR1## wherein R.sup.1 and R.sup.2 may be the same or different and mean individually a hydrogen atom or a straight-chain or branched alkyl or cycloalkyl group, or R.sup.1 and R.sup.2 are bonded together to mean an alkylene group having 2-6 carbon atoms, R.sup.3 denotes a hydrogen atom or a lower alkyl, aralkyl, amino lower alkyl or lower alkoxycarbonylamino lower alkyl group, R.sup.4 means a lower alkyl, cycloalkyl or aralkyl group, R.sup.5 means a hydrogen atom or a lower alkyl group, or R.sub.4 and R.sub.5 are bonded together to denote an alkylene group having 2-4 carbon atoms, and R.sup.6 stands for a hydrogen atom or a lower alkyl or aralkyl group; or a pharmacologically acceptable salt thereof.
摘要翻译: 提供了具有强ACE抑制活性的新型γ-丁内酯衍生物。 它们由以下通式(I)表示:其中R 1和R 2可以相同或不同,并且分别表示氢原子或直链或支链烷基或环烷基,或者R1和R2 键合在一起表示具有2-6个碳原子的亚烷基,R3表示氢原子或低级烷基,芳烷基,氨基低级烷基或低级烷氧基羰基氨基低级烷基,R4表示低级烷基,环烷基或芳烷基,R5表示 氢原子或低级烷基,或者R4和R5键合在一起,表示具有2-4个碳原子的亚烷基,R6代表氢原子或低级烷基或芳烷基; 或其药理学上可接受的盐。
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公开(公告)号:US4977275A
公开(公告)日:1990-12-11
申请号:US333239
申请日:1989-04-05
IPC分类号: A61K31/40 , A01N43/36 , A61K31/4025 , A61K31/44 , A61K31/4427 , A61K31/4433 , A61P17/00 , C07D207/34 , C07D401/12 , C07D409/12
CPC分类号: C07D207/34
摘要: A pyrrole derivative having excellent anti-microbial activities is disclosed. This compound is represented by the following formula (I): ##STR1## wherein X.sub.1 and X.sub.2 are the same or different and mean individually a halogen atom, R.sub.1 denotes an alkyl, cycloalkyl, haloalkyl, alkenyl, substituted or unsubstituted phenyl, substituted or unsubstituted aralkyl group or a group --COR.sub.3 in which R.sub.3 is an alkyl group having at least five carbon atoms or a cycloalkyl, haloalkyl, alkenyl, substituted or unsubstituted phenyl, substituted or unsubstituted aralkyl, or heterocyclic group, and R.sub.2 stands for a hydrogen or halogen atom or an alkyl group, with a proviso that R.sub.1 is other than a hydrogen atom or methyl group when X.sub.1, X.sub.2 and R.sub.2 are each a bromine atom.
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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:US4942172A
公开(公告)日:1990-07-17
申请号:US196431
申请日:1988-05-20
IPC分类号: C07D339/06 , A61K31/385 , A61P1/16
CPC分类号: A61K31/385 , Y10S514/894
摘要: A method of curing or alleviating hepatic disease comprising administrating to the patient 1,3-dithiole-2-thione or 1,3-dithiolane-2-thione is disclosed. Adminstration of the compound can be made in various dosing forms, including tablets, granules, powders, capsules, suspensions, injections, and suppositories. Normal dosing amount can be determined from the range of 0.01 to 50 mg/kg/day for oral administration, and 0.002 to 10 mg/kg/day for injection or other forms of administration.
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公开(公告)号:US4564615A
公开(公告)日:1986-01-14
申请号:US441177
申请日:1982-11-12
IPC分类号: C07D513/04 , A61K31/535
CPC分类号: C07D513/04 , Y10S514/825 , Y10S514/885 , Y10S514/892
摘要: An immunoactivator comprising an effective amount of a thiazolobenzoxazine derivative of the formula, or its salt ##STR1## wherein R.sup.1 represents a hydrogen atom, carboxyl group or lower alkoxycarbonyl group, R.sup.2 represents a substituted or unsubstituted phenyl group, lower alkyl group or furyl group, and R.sup.3 represents a hydrogen atom or lower alkoxy group.
摘要翻译: 包含有效量的下式的噻唑并恶嗪衍生物或其盐,其中R1表示氢原子,羧基或低级烷氧基羰基,R2表示取代或未取代的苯基,低级烷基或呋喃基, 并且R 3表示氢原子或低级烷氧基。
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公开(公告)号:US5082948A
公开(公告)日:1992-01-21
申请号:US484368
申请日:1990-02-22
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.
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公开(公告)号:US5047428A
公开(公告)日:1991-09-10
申请号:US365368
申请日:1989-06-13
IPC分类号: A61K31/195 , A61K31/198 , A61P11/10 , C07C323/58
CPC分类号: A61K31/195 , Y10S514/855
摘要: An expectorant comprising a hydroxyalkylcysteine derivative of the following formula (I) is disclosed. ##STR1## wherein n represents an integer of 1 to 4. The expectorant is stabile, has little side effects and toxicity, and exhibits an excellent expectorant effect.
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公开(公告)号:US4968825A
公开(公告)日:1990-11-06
申请号:US418169
申请日:1989-10-06
申请人: Koichi Yokoi , Kinichi Mogi , Kazuhiko Irinoda , Hidehiko Kohya , Susumu Sato , Tatsuhiko Katori
发明人: Koichi Yokoi , Kinichi Mogi , Kazuhiko Irinoda , Hidehiko Kohya , Susumu Sato , Tatsuhiko Katori
IPC分类号: C07F15/00
CPC分类号: C07F15/0093
摘要: A platinum complex having a superior antitumor activity is disclosed. The platinum complex has a structure represented by the formula: ##STR1## wherein A and B independently represent a lower alkanoyloxy group which may have a halogen atom substituent, or in combination represent a group: ##STR2## wherein R.sub.1 and R.sub.2 independently represent a hydrogen atom, a hydroxyl group, or a lower alkyl group, or in combination with each other and with the adjacent carbon atom a cyclobutane ring, and R.sub.3 represents a hydrogen atom, a lower alkyl group, a lower alkoxy group, a halogen atom, a sulfo group, or nitro group.
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公开(公告)号:US4740601A
公开(公告)日:1988-04-26
申请号:US941318
申请日:1986-12-15
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。
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公开(公告)号:US5008419A
公开(公告)日:1991-04-16
申请号:US451637
申请日:1989-12-18
IPC分类号: C07F15/00
CPC分类号: C07F15/0093
摘要: A platinum complex having the following formula (I) is disclosed, ##STR1## wherein R.sup.1 and R.sup.2 may be the same or different and each independently represents a methyl group or an ethyl group, and the configuration of 1,2-diaminocyclohexane is either cis-, trans-l-, trans-d-, or trans-dl-.The compound possess excellent antitumor activity with a high therapeutic index and abundant water solubility, and thus are effective as an antitumor agent.
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