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1. 发明公开

EP1137642A1 BIS-SULFONAMIDES 有权
标题翻译： BIS-磺胺
公开(公告)号：EP1137642A1
公开(公告)日：2001-10-04
申请号：EP00956456.8
申请日：2000-08-16
申请人： Actelion Pharmaceuticals Ltd.
发明人： BOLLI, Martin , BOSS, Christoph , CLOZEL, Martine , FISCHLI, Walter
IPC分类号： C07D239/69 , C07D401/12 , A61K31/505 , A61K31/506 , A61P9/12
CPC分类号： C07D239/69 , C07D401/12
摘要： The invention relates to novel bis-sulfonamides and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and especially their use as endothelin antagonists.

2. 发明公开

EP0866075A3 Method to treat microbial infections by uncoupling of phosphotransferase system and appropriate agents therefor 失效
标题翻译：一种用于治疗微生物感染mittles解耦磷酸转移酶系统的方法，以及geeingnete剂
公开(公告)号：EP0866075A3
公开(公告)日：2000-06-07
申请号：EP98101704.9
申请日：1998-02-02
申请人： Arpida
发明人： Erni, Bernhard
IPC分类号： C07K7/06 , C07K7/08 , C07K5/10 , A61K38/00 , C12Q1/02 , C12Q1/48 , C12R1/19
CPC分类号： C07K7/06 , A61K38/00 , C07K5/1024 , C07K7/08
摘要： The bacterial phosphotransferase system (PTS) as a drug target system catalyses the uptake and phosphorylation of carbohydrates. It is further involved in signal transduction, e.g. catabolite repression, chemotaxis, and allosteric regulation of metabolic enzymes and transporters. It is ubiquitous in bacteria but does not occur in eukaryotes. This uniqueness and the pleiotropic function make the PTS a target for the development of new antimicrobials. Assays are described that lead to the discovery of compounds which uncouple the PTS, by acting as protein histidine/cysteine phosphatases. Uncoupling of the PTS leads to inhibition of carbohydrate transport, repression of catabolite controlled genes (e.g. certain virulence genes) and depletion of phosphoenolpyruvate. Compounds from combinatorial libraries with high affinity for phosphoenolpyruvat-protein-phosphatase (Enzyme I) serve as lead structures for the development of inhibitors and uncouplers of the PTS.

3. 发明公开

EP0740938A3 Prolin und 4-hydroxyprolin als therapeutische Wirkstoffe 失效
标题翻译：脯氨酸和4-羟脯氨酸作为治疗剂
公开(公告)号：EP0740938A3
公开(公告)日：1997-03-12
申请号：EP96106804.6
申请日：1996-04-30
申请人： IPR-Institute for Pharmaceutical Research Riehen AG
发明人： Meyer, Hans , Segesser, Bernhard, Dr.
IPC分类号： A61K31/40
CPC分类号： A61K31/401
摘要： Prolin, 4-Hydroxyprolin und ihre pharmazeutisch verträglichen Salze besitzen antiphlogistische, antirheumatische, analgetische und wundheilungsfördernde Wirkung und eignen sich zur Behandlung von Entzündungs- oder Schmerzzuständen oder zur Wundbehandlung, insbesondere zur Behandlung von entzündlich bedingten, rheumatischen oder nicht-rheumatischen Schmerzzuständen oder von postoperativen oder posttraumatischen Schmerzen.

4. 发明公开

EP1465875A1 NOVEL ALKANSULFONAMIDES AS ENDOTHELIN ANTAGONISTS 有权
标题翻译：新的烷基磺酰胺ALS内皮素
公开(公告)号：EP1465875A1
公开(公告)日：2004-10-13
申请号：EP02795133.4
申请日：2002-12-10
申请人： Actelion Pharmaceuticals Ltd.
发明人： BOLLI, Martin , BOSS, Christoph , CLOZEL, Martine , FISCHLI, Walter , WELLER, Thomas
IPC分类号： C07D239/47 , A61K31/506 , A61P9/00 , C07D239/56 , C07D239/52 , C07D239/48 , C07D401/14 , C07D403/14
摘要： The invention relates to novel alkansulfonamides of structure (I), wherein R1 is a lowel alzyl group and the other variables are as defined in the description, and their use as active ingredients in the preparation of pharmaceutical compositions. The invention aslo concerns related aspects inluding processes for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and especially their use as endothelin receptor antagonists in the treatment and prevention of diseases associated to the endothelin system.

5. 发明公开

EP0740938A2 Prolin und 4-hydroxyprolin als therapeutische Wirkstoffe 失效
标题翻译： Prolin和4-羟基拉洛尔治疗Wirkstoffe
公开(公告)号：EP0740938A2
公开(公告)日：1996-11-06
申请号：EP96106804.6
申请日：1996-04-30
申请人： IPR-Institute for Pharmaceutical Research Riehen AG
发明人： Meyer, Hans , Segesser, Bernhard, Dr.
IPC分类号： A61K31/40
CPC分类号： A61K31/401
摘要： Prolin, 4-Hydroxyprolin und ihre pharmazeutisch verträglichen Salze besitzen antiphlogistische, antirheumatische, analgetische und wundheilungsfördernde Wirkung und eignen sich zur Behandlung von Entzündungs- oder Schmerzzuständen oder zur Wundbehandlung, insbesondere zur Behandlung von entzündlich bedingten, rheumatischen oder nicht-rheumatischen Schmerzzuständen oder von postoperativen oder posttraumatischen Schmerzen.
摘要翻译：脯氨酸和4-羟脯氨酸及其盐作为治疗炎症和疼痛并促进伤口愈合的治疗药物。也用于治疗风湿性和非风湿性疼痛，作为止痛剂并治疗手术后或创伤后疼痛。抗坏血酸盐是首选。县。作为片剂，糖衣丸，胶囊剂，颗粒剂，栓剂或凝胶剂，霜剂或软膏剂。液体制剂一个soln 或暂停是首选。

6. 发明公开

EP1499607A1 4-(PIPERIDYL- AND PYRROLIDYL-ALKYL-UREIDO)-QUINOLINES AS UROTENSIN II RECEPTOR ANTAGONISTS 有权
标题翻译： 4-（哌啶基吡咯烷基和烷基 - 脲基）-quinolines AS尾加压素II拮抗剂受体
公开(公告)号：EP1499607A1
公开(公告)日：2005-01-26
申请号：EP02791749.1
申请日：2002-12-02
申请人： Actelion Pharmaceuticals Ltd.
发明人： AISSAOUI, Hamed , BINKERT, Christoph , CLOZEL, Martine , MATHYS, Boris , MUELLER, Claus , NAYLER, Oliver , SCHERZ, Michael , VELKER, Jörg , WELLER, Thomas
IPC分类号： C07D401/12 , C07D401/14 , C07D471/04 , A61K31/4709
CPC分类号： C07D471/04 , C07D401/12 , C07D401/14
摘要： The invention relates to novel 1-pyridin-4-yl urea derivatives and related compounds and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and especially their use as neurohormonal antagonists.

7. 发明授权

EP1274687B1 1,2,3,4- TETRAHYDROISOQUINOLINE DERIVATIVES 有权
标题翻译： 1,2,3,4-四氢衍生物
公开(公告)号：EP1274687B1
公开(公告)日：2005-01-05
申请号：EP01933685.8
申请日：2001-03-12
申请人： Actelion Pharmaceuticals Ltd.
发明人： AISSAOUI, Hamed , CAPPI, Michael , CLOZEL, Martine , FISCHLI, Walter, Actelion Pharmaceuticals Ltd. , KOBERSTEIN, Ralf
IPC分类号： C07D217/20 , C07D217/04 , C07D401/12 , A61K31/435 , A61P3/04 , A61P25/20

8. 发明公开

EP1427417A1 3-SUBSTITUTED 6,7-DIHYDROXYTETRAHYDROISOQUINOLINE DERIVATIVES FOR USE AS ANTIBACTERIAL AGENTS 有权
标题翻译： 3-取代-6,7- DIHYDROXYTETRAHYDROISOCHINOLIN衍生物FOR USE作为一种手段ANTIBKATERIELLE
公开(公告)号：EP1427417A1
公开(公告)日：2004-06-16
申请号：EP02796217.4
申请日：2002-08-09
申请人： Arpida AG,
发明人： BURRI, Kaspar , SCHMITT, Laurent , ISLAM, Khalid
IPC分类号： A61K31/472 , A61P31/04 , C07D217/16 , C07D217/14 , C07D217/02 , C07D405/04 , C07D217/12
CPC分类号： C07D217/02 , C07D217/12 , C07D217/14 , C07D217/16
摘要： The invention relates to novel tetrahydroisoquinoline derivatives of general formula I and theirs use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and their use as anti-infectives, wherein R?1, R2 and R3¿ are as defined in claim 1.

9. 发明公开

EP1307445A1 BENZOFURAN DERIVATIVES AND THEIR USE AS ANTIBACTERIAL AGENTS 有权
标题翻译：苯并呋喃衍生物及其作为抗菌物质
公开(公告)号：EP1307445A1
公开(公告)日：2003-05-07
申请号：EP01969459.5
申请日：2001-07-20
申请人： Arpida AG,
发明人： BURRI, Kaspar , GILLESSEN, Dieter , GREIVELDINGER-POENARU, Sorana , ISLAM, Khalid
IPC分类号： C07D405/06 , C07D405/14 , A61K31/505 , A61P31/04
CPC分类号： C07D401/14 , C07D307/86 , C07D405/06 , C07D405/14 , C07D407/04
摘要： The invention relates to novel benzofuran derivatives and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and especially their use as anti-infectives.

10. 发明公开

EP0866075A2 Method to treat microbial infections by uncoupling of phosphotransferase system and appropriate agents therefor 失效
标题翻译：一种用于治疗微生物感染mittles解耦磷酸转移酶系统的方法，以及geeingnete剂
公开(公告)号：EP0866075A2
公开(公告)日：1998-09-23
申请号：EP98101704.9
申请日：1998-02-02
申请人： Arpida
发明人： Erni, Bernhard
IPC分类号： C07K7/06 , C07K7/08 , C07K5/10 , A61K38/00
CPC分类号： C07K7/06 , A61K38/00 , C07K5/1024 , C07K7/08
摘要： The bacterial phosphotransferase system (PTS) as a drug target system catalyses the uptake and phosphorylation of carbohydrates. It is further involved in signal transduction, e.g. catabolite repression, chemotaxis, and allosteric regulation of metabolic enzymes and transporters. It is ubiquitous in bacteria but does not occur in eukaryotes. This uniqueness and the pleiotropic function make the PTS a target for the development of new antimicrobials. Assays are described that lead to the discovery of compounds which uncouple the PTS, by acting as protein histidine/cysteine phosphatases. Uncoupling of the PTS leads to inhibition of carbohydrate transport, repression of catabolite controlled genes (e.g. certain virulence genes) and depletion of phosphoenolpyruvate. Compounds from combinatorial libraries with high affinity for phosphoenolpyruvat-protein-phosphatase (Enzyme I) serve as lead structures for the development of inhibitors and uncouplers of the PTS.
摘要翻译：细菌磷酸转移酶系统（PTS）作为药物靶标系统催化碳水化合物的摄取和磷酸化。它是在信号转导进一步介入，E.G. 代谢物阻遏，趋化和代谢酶和转运蛋白的变构调节。它是细菌无处不在，但在真核生物中不会发生。这种独特性和多效功能，使PTS对新抗菌药物的发展目标。测定被充当蛋白质组氨酸/半胱氨酸磷酸酶描述确实导致这脱开PTS化合物的发现。的PTS的解偶联导致抑制碳水化合物运输，分解代谢物控制的基因（E. G.某些毒力基因）和磷酸烯醇式丙酮酸的耗尽压制。从与磷酸烯醇丙酮酸蛋白磷酸酶的高亲和力的组合文库的化合物（酶I）作为抑制剂和所述PTS的解偶联剂的发展引线结构。

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