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1. 发明授权

EP0544906B1 ANTIBACTERIAL PENEM ESTERS DERIVATIVES 失效转让
标题翻译：抗菌青霉烯酯衍生物
公开(公告)号：EP0544906B1
公开(公告)日：1999-11-10
申请号：EP91914603.5
申请日：1991-08-16
申请人： SUNTORY LIMITED
发明人： IWATA, Hiromitsu , NAKATSUKA, Takashi , TANAKA, Rie , ISHIGURO, Masaji
IPC分类号： C07D499/88 , A61K31/43 , C07D499/883
CPC分类号： C07D499/88

2. 发明授权

EP0801057B1 PROCESS FOR PRODUCING OPTICALLY ACTIVE TRANS-VINYL SULFIDE ALCOHOLS 失效
标题翻译：工艺生产光学活性反式乙烯基硫醇类
公开(公告)号：EP0801057B1
公开(公告)日：2002-01-16
申请号：EP96935505.6
申请日：1996-10-30
申请人： SUNTORY LIMITED
发明人： SEKIUCHI, Kazuto , IMOTO, Masahiro , ISHIGURO, Masaji , NAKATSUKA, Takashi , TANAKA, Rie 202, Tatebayashigadenhiruzu , INOUE, Hidekazu
IPC分类号： C07C323/14 , C07C319/20 , C07B53/00
CPC分类号： C07B53/00 , C07C319/20 , C07C323/14
摘要： A process for producing optically active trans-vinyl sulfide alcohols represented by general formula (III), wherein R1 represents alkyl or aryl; which comprises reducing trans-vinyl sulfide ketones with a borane reducing agent in the presence of an optically active oxazaborolidine and an additive.

3. 发明公开

EP0757051A1 PENEM DERIVATIVES AND ANTIMICROBIAL AGENT CONTAINING THE SAME 失效
标题翻译：印度尼西亚反犹太人解放阵线
公开(公告)号：EP0757051A1
公开(公告)日：1997-02-05
申请号：EP96902477.7
申请日：1996-02-19
申请人： SUNTORY LIMITED
发明人： ISHIGURO, Masaji , NAKATSUKA, Takashi , TANAKA, Rie , NAMIKAWA, Koshi , MATSUKI, Shinsuke
IPC分类号： C07D499/88 , A61K31/43
CPC分类号： C07D499/88 , Y02P20/55
摘要： A penem derivative represented by the following formula (I):
wherein R 1 represents a substituted or unsubstituted alkyl group, a substituted or unsubstituted alkenyl group, a substituted or unsubstituted aralkyl group, a substituted or unsubstituted aryl group, a substituted or unsubstituted alkylthio group, a substituted or unsubstituted alkenylthio group, a substituted or unsubstituted aralkylthio group, a substituted or unsubstituted arylthio group, a substituted or unsubstituted heterocyclic group, a substituted or unsubstituted heterocyclic thio group, a substituted or unsubstituted acylthio group, a mercapto group or a hydrogen atom, and R 2 represents a hydrogen atom or a carboxyl-protecting group; or a pharmacologically acceptable salt thereof.
The compound (I) exhibits strong antibacterial activities, and especially, shows strong activities against MRSA. It is therefore useful not only as a general antibacterial agent but also as an antibacterial agent for MRSA against which no general antibacterial agents are recognized to be effective.
摘要翻译：由下式（I）表示的pen嗪衍生物：其中R 1表示取代或未取代的烷基，取代或未取代的烯基，取代或未取代的芳烷基，取代或未取代的芳基，取代或未取代的芳基取代或未取代的芳硫基，取代或未取代的芳硫基，取代或未取代的杂环基，取代或未取代的杂环硫基，取代或未取代的酰硫基，巯基或巯基氢原子，R 2表示氢原子或羧基保护基; 或其药理学上可接受的盐。化合物（I）表现出强烈的抗菌活性，特别是对MRSA具有强烈的活性。因此，不仅可以作为普通抗菌剂，而且作为MRSA的抗菌剂也是有用的，因为没有一般的抗菌剂被认为是有效的。

4. 发明公开

EP0544905A1 ANTIBACTERIAL PENEM COMPOUNDS 失效转让
标题翻译：抗菌青霉烯化合物。
公开(公告)号：EP0544905A1
公开(公告)日：1993-06-09
申请号：EP91914600.0
申请日：1991-08-16
申请人： SUNTORY LIMITED
发明人： IWATA, Hiromitsu , NATAKSUKA, Takashi , TANAKA, Rie , ISHIGURO, Masaji
IPC分类号： A61K31 , A61P31 , C07D499
CPC分类号： C07D499/88
摘要： Composés antibiotiques de penem répondant à la formule (I), dans laquelle R représente un groupe hydrolysable par voie physiologique, à formation d'esters et utile dans le composé de penem. Ce groupe est un groupe facile à enlever par hydrolyse in vivo, par exemple un groupe acétyloxyméthyle, 1-(acétyloxy)éthyle, pivaloyloxyméthyle, 1-(éthoxycarbonyloxy)éthyle, 1-(isopropyloxycarbonyloxy)éthyle, 1-(cyclohexy oxycarbonyloxy)éthyle ou 3-phtalidyle. On décrit également des compositions antibiotiques buvables.

5. 发明公开

EP0801057A1 PROCESS FOR PRODUCING OPTICALLY ACTIVE TRANS-VINYL SULFIDE ALCOHOLS 失效
标题翻译： VERFAHREN ZUR HERSTELLUNG VON OPTISCH AKTIVEN TRANS-VINYL-SULFIDALKOHOLEN
公开(公告)号：EP0801057A1
公开(公告)日：1997-10-15
申请号：EP96935505.6
申请日：1996-10-30
申请人： SUNTORY LIMITED
发明人： SEKIUCHI, Kazuto , IMOTO, Masahiro , ISHIGURO, Masaji , NAKATSUKA, Takashi , TANAKA, Rie 202, Tatebayashigadenhiruzu , INOUE, Hidekazu
IPC分类号： C07C323/14 , C07C319/20 , C07B53/00
CPC分类号： C07B53/00 , C07C319/20 , C07C323/14
摘要： A method for producing an optically active trans-vinylsulfide alcohol having the formula:
wherein R 1 represents an alkyl group or an aryl group, comprising the step of reducing a trans-vinylsulfide ketone with a borane reducing agent in the presence of an optically active oxazaborolidine and an additive.
摘要翻译：一种制备具有下式的光学活性的反式乙烯基硫醚醇的方法：其中R 1表示烷基或芳基，其中R 1表示烷基或芳基，该方法包括在存在下用硼烷还原剂还原反式乙烯基硫醚酮的步骤的光学活性的恶唑硼烷和添加剂。

6. 发明公开

EP0638552A1 PROCESS FOR SYNTHESIZING 4-SUBSTITUTED AZETIDINONE DERIVATIVE 失效
标题翻译：合成4-取代的二氮杂萘酮衍生物的方法
公开(公告)号：EP0638552A1
公开(公告)日：1995-02-15
申请号：EP94906364.8
申请日：1994-02-10
申请人： SUNTORY LIMITED
发明人： ISHIGURO, Masaji , NAKATSUKA, Takashi , TANAKA, Rie , SHIMAMOTO, Tetsuo , YOSHIDA, Takuro
IPC分类号： C07D205/08
CPC分类号： C07D205/08
摘要： The invention relates to a process for synthesizing a 4-substituted azetidinone derivative represented by the general formula (3) (wherein OR₁ represents a protected hydroxyl group; CO₂R₃ represents an esterified carboxyl group; and X and Y represent each independently alkyl, alkenyl, aralkyl, aryl, alkylthio, alkoxy, heterocycle, acyl, amino, hydrogen or halogen, or alternatively X and Y are combined together to represent cycloalkan-2-on-2-yl) by the reaction of an azetidinone derivative represented by general formula (1) (wherein OR₁ is as defined above; and R₂ represents alkyl, alkenyl or aryl) with an ester compound represented by general formula (2): (wherein CO₂R₃, X and Y are each as defined above) in the presence of zinc and copper compounds. The invention relates also to a compound represented by general formula (3) and further to a compound prepared by decarboxylating the compound (3), both being useful as an intermediate for synthesizing antibacterial carbapenem compounds.
摘要翻译：本发明涉及由通式（3）表示的4-取代氮杂环丁酮衍生物的合成方法（式中OR 1代表被保护的羟基; CO 2 R 3代表酯化的羧基; X和Y分别独立地代表烷基，链烯基，芳烷基（1）所示的氮杂环丁酮衍生物与式（1）所示的氮杂环丁酮衍生物反应，从而得到式（1）所示的环烷基-2-酮基）（其中OR 1定义如上; R 2代表烷基，链烯基或芳基）与通式（2）代表的酯化合物反应：（其中CO 2 R 3，X和Y的定义同上）在锌和铜化合物。本发明还涉及由通式（3）表示的化合物，还涉及通过使化合物（3）脱羧而制备的化合物，两者都可用作用于合成抗菌碳杂青霉烯化合物的中间体。

7. 发明公开

EP1376132A1 G PROTEIN-COUPLED RECEPTOR STRUCTURAL MODEL AND A METHOD OF DESIGNING LIGAND BINDING TO G PROTEIN-COUPLED RECEPTOR BY USING THE STRUCTURAL MODEL 审中-公开
标题翻译：结构模型配体的设计结合G蛋白偶联受体使用结构模型A G蛋白偶联受体和方法
公开(公告)号：EP1376132A1
公开(公告)日：2004-01-02
申请号：EP02708749.3
申请日：2002-04-01
申请人： SUNTORY LIMITED
发明人： ISHIGURO, Masaji
IPC分类号： G01N33/566 , G01N33/48 , G06F17/50 , G06F17/30 , C07K1/00
CPC分类号： G06F19/12 , C07K14/723 , C07K2299/00 , G01N33/566 , G01N33/6803 , G06F19/16
摘要： The present invention provides a method for constructing a structural model of a complex that a G protein-coupled protein receptor forms with a ligand capable of binding the G protein-coupled receptor and a three-dimensional structural model of an activated intermediate in the structural model of the complex. The present invention also provides a method for identifying, screening for, searching for, evaluating, or designing a ligand capable of binding a GPCR by using the three-dimensional model. In one specific method provided by the present invention, a three-dimensional structural model of a photoactivated intermediate of rhodopsin is constructed by using a molecule modeling software and by using the three-dimensional structural coordinate of the crystal structure of rhodopsin in such a manner that amino acid residues highly conserved among GPCRs are taken into consideration. The three-dimensional stractural model of the photoactivated intermediate of rhodopsin is subsequently used to construct structural models of activated intermediates of other GPCRs. The present invention further provides a method for identifying, screening for, searching for, evaluating, or designing a ligand that binds a GPCR to act as an agonist or an antagonist. This method employs the three-dimensional structural model constructed by the above-described method.
摘要翻译：本发明提供的方法用于构造复杂的结构模型做了G蛋白偶联蛋白受体与配体能够结合G蛋白偶联受体，并在结构模型活化的中间体的三维结构模型复杂。因此，本发明提供了用于鉴定，筛选，寻找，评价，或设计能够通过使用三维模型结合GPCR的配体的方法。在由本发明提供的一种具体方法，光活化的中间视紫红质的三维结构模型是通过使用分子建模软件并通过使用视紫质的晶体结构的三维结构坐标在寻求的方式做了构筑的GPCR之间高度保守的氨基酸残基被考虑在内。所述光活化stractural中间视紫质的三维模型随后用于构建其它GPCR的活化中间体的结构模型。本发明进一步提供了用于鉴定，筛选，寻找，评价，或设计配体做的方法结合GPCR的充当到激动剂或拮抗剂。该方法采用由上述方法构成的三维结构模型。

8. 发明授权

EP0544905B1 ANTIBACTERIAL PENEM COMPOUNDS 失效转让
标题翻译：抗菌青霉烯
公开(公告)号：EP0544905B1
公开(公告)日：1998-10-14
申请号：EP91914600.1
申请日：1991-08-16
申请人： SUNTORY LIMITED
发明人： IWATA, Hiromitsu , NATAKSUKA, Takashi , TANAKA, Rie , ISHIGURO, Masaji
IPC分类号： C07D499/88 , A61K31/43
CPC分类号： C07D499/88
摘要： Antibiotic penem coumpounds are represented by formula (I), wherein R represents a physiologically-hydrolyzable, ester-forming group. The physiologically hydrolyzable, ester-forming group useful in the penem compound of the present invention means a group which can be removed easily by in vivo hydrolysis, such as an acetyloxymethyl, 1-(acetyloxy)ethyl, pivaloyloxymethyl, 1-(ethoxycarbonyloxy)ethyl, 1-(isopropyloxycarbonyloxy)-ethyl, 1-(cyclohexyloxycarbonyloxy)ethyl or 3-phthalidyl group. Antibiotic compositions for oral administration are also described.

9. 发明公开

EP0544906A1 PENEM COMPOUNDS 失效转让
标题翻译： PENEMVERBINDUNGEN。
公开(公告)号：EP0544906A1
公开(公告)日：1993-06-09
申请号：EP91914603.0
申请日：1991-08-16
申请人： SUNTORY LIMITED
发明人： IWATA, Hiromitsu , NAKATSUKA, Takashi , TANAKA, Rie , ISHIGURO, Masaji
IPC分类号： A61K31 , A61P31 , C07D499
CPC分类号： C07D499/88
摘要： Composés antibiotiques de penem répondant à la formule (I), dans laquelle R représente un groupe répondant à la formule (II) ou (III), dans laquelle R1 représente un groupe alkyle linéaire ou ramifié en C1-6; R2 représente un groupe alkyle, aryle ou aralkyle spécifique et substitué ou non; n vaut 1 ou 2; et R3 représente un groupe alkyle, aryle ou aralkyle spécifique et substitué ou non. On décrit également des compositions antibiotiques buvables.

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