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21. 发明授权

EP1765812B1 CONTRAST AGENTS ENDOWED WITH HIGH RELAXIVITY FOR USE IN MAGNETIC RESONANCE IMAGING (MRI) WHICH CONTAIN A CHELATING MOIETY WITH POLYHYDROXYLATED SUBSTITUENTS 有权转让
标题翻译： FOR USE IN磁成像（MRI）DYE高弛豫，螯合基团WITH多羟基替代物含
公开(公告)号：EP1765812B1
公开(公告)日：2009-04-29
申请号：EP05755566.6
申请日：2005-06-28
申请人： Bracco Imaging S.p.A
发明人： AIME, Silvio, Bracco Imaging S.p.A. , GALLI, Matteo, Bracco Imaging SpA , LATTUADA, Luciano, Bracco Imaging SpA , MOROSINI, Pierfrancesco, Bracco Imaging SpA , UGGERI, Fulvio, Bracco Imaging SpA , KONDAREDDIAR, Ramalingam, Bracco Research USA
IPC分类号： C07D405/14
CPC分类号： C07H15/26 , A61K49/085 , A61K49/124 , C07C237/08 , C07D243/08 , C07D243/10 , C07F9/3808 , C07F9/4006 , C07F9/5728 , C07H17/02
摘要： The present invention relates to a novel class of paramagnetic ion-based contrast i agents of formula (I), wherein a chelating backbone moiety is highly functionalized by the presence of one or more polyhdroxylated chain, that show a pharmacokinetic i profile analogous to that of the commonly used T1-general extravascular agents (NSA) but are further characterized by a higher relaxivity. Formula (I): A(LR)V wherein: A is a linear or cyclic chelating backbone moiety; R is, independently, H or a C2-C70 aminopolyol moiety comprising a 'straight or branched alkyl chain substituted by from 2 to 30 hydroxyl groups, the said chain being optionally interrupted by one or more groups selected from -0-, -NH-, -N NCO-; and optionally substituted by one or more C4-C10 cyclic units; L is, independently, a direct bond or 'a divalent straight or branched linker moiety between A and R, at most comprising 20 carbon atoms; V is a positive integer from 1 to 7; with the proviso that at least one of the R groups is other than H; or a physiologically acceptable salt of such ligand.

22. 发明公开

EP1770086A1 Ausgewählte CGRP-Antagonisten, Verfahren zu deren Herstellung sowie deren Verwendung als Arzneimittel 审中-公开
标题翻译：选择CGRP拮抗剂，其制备方法及其作为药物使用
公开(公告)号：EP1770086A1
公开(公告)日：2007-04-04
申请号：EP05021236.4
申请日：2005-09-29
申请人： Boehringer Ingelheim Pharma GmbH & Co. KG
发明人： Die Erfindernennung liegt noch nicht vor
IPC分类号： C07D249/12 , C07D243/10 , C07D403/12 , C07D401/12
CPC分类号： C07D243/10 , C07D249/12 , C07D401/12 , C07D403/12
摘要： Gegenstand der vorliegenden Erfindung sind die CGRP-Antagonisten der allgemeinen Formel I

in der R 1 , R 2 , R 3 und R 4 wie in Anspruch 1 definiert sind, deren Tautomere, deren Isomere, deren Diastereomere, deren Enantiomere, deren Hydrate, deren Gemische und deren Salze sowie die Hydrate der Salze, insbesondere deren physiologisch verträgliche Salze mit anorganischen oder organischen Säuren oder Basen, sowie diejenigen Verbindungen der allgemeinen Formel I, in denen ein oder mehrere Wasserstoffatome durch Deuterium ausgetauscht sind, diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Verfahren zu ihrer Herstellung.
摘要翻译：取代的哌啶化合物（I）及其互变异构体和盐是新的。式（I）及其互变异构体和盐的取代哌啶化合物是新的。的R 1>取代的3,4-二氢-1H-喹唑啉-2-酮的式化合物（1a），取代的1,3,4,5-四氢苯并[d] [1,3]二氮杂-2-酮化合物 ;式（2a）或5-苯基-2,4-二氢 - [1,2,4]三唑-3-酮式（3a）的化合物的的R 1> 1> H或H 3 C-O-; R 2>式（4a）的substituiertem甲苯化合物; R 2> 1> HO，H 3 CO，H-C（O）-O或H 3 C-C（O）-O-; R 2> 2> 1-2C烷基或H 3CO-; ，R 3> R4A-2-8C亚烷基-NH-或式杂环化合物（5A-6A）; R4A：H，H 2 N，13 C-烷基-NH，（1-3C烷基）2 N或1-6C烷基-O-C（O）-NH-; ，R 3> 2>，R 3> 4> H或1-3C烷基; ，R 3> 3>自由电子对或氧原子; R 4b为H，1-6C烷基，H 2 N-2-6C亚烷基，1-3C烷基-NH-2-6C亚烷基，（1-3C烷基）2 N-1-6C亚烷基，环烷基3-6C 1-3C亚烷基，NH 2，1-3C烷基，NH或（1-3C烷基）2-N; ，R 4> 7种环状化合物E.G. 式的杂环化合物（7A-10A）; 和R 4> 2>，R 3> 2>。条件是：当X是C，R 4> 1>为H，OH或1-3C烷基; 当X是N，R 4> 1>是自由电子对或氧原子; 如果X是N，则Y 1>是O，S，S（O），S（O）2; 如果X是C，则Y 1>是S，S（O），S（O）2; 并且提供没有R3>和R 4>未在N原子经由彼此结合同时。 [图像] [图像] [图像] [图像] ACTIVITY：止痛; 降糖; 抗关节炎; 骨科; 抗风湿; 抗过敏; 抗炎; 平喘; 胃肠道根。 Vasotropic; 抗菌; 免疫抑制; 皮肤病; 伤药; 止痒; 心血管基因。作用机理：降钙素基因相关肽（CGRP）受体拮抗剂。（I）的拮抗这在SK-N-MC细胞中测试CGRP受体的能力。显示结果做了（I），其> = 10000纳米的IC 5 0值。

23. 发明授权

EP1021190B1 Amid derivatives as growth hormone release promotors 有权
标题翻译： Amide zurFörderungderAusschüttungvon Wachstumshormonen
公开(公告)号：EP1021190B1
公开(公告)日：2006-11-08
申请号：EP98942140.9
申请日：1998-08-20
申请人： KAKEN PHARMACEUTICAL CO., LTD. , Molecular Research Institute
发明人： FUNAMIZU, Hidenori , ISHIYAMA, Nobuo , IKEGAMI, Satoru, Centr. Res. Inst. Kaken Pharm. , OKUNO, Tadashi, Centr. Res. Inst. Kaken Pharm. , INOGUCHI, Kiyoshi, Centr. Res. Inst. Kaken Pharm. , HUANG, Ping, Molecular Research Institute , LOEW, Gilda H., Molecular Research Institute
IPC分类号： A61K31/55 , C07D267/14 , C07D267/16 , C07D281/10 , C07D223/16 , C07K5/02 , C07D403/12 , A61P5/00
CPC分类号： C07D223/16 , C07C237/22 , C07C2602/12 , C07D209/38 , C07D209/52 , C07D211/22 , C07D215/06 , C07D215/227 , C07D215/56 , C07D223/20 , C07D225/06 , C07D225/08 , C07D243/10 , C07D243/12 , C07D243/14 , C07D265/36 , C07D267/14 , C07D267/18 , C07D279/16 , C07D279/26 , C07D281/10 , C07D281/14 , C07D401/04 , C07D403/12 , C07D417/12 , C07D487/04 , C07D498/04
摘要： Disclosed are the novel compounds represented by structural Formula (I), wherein A is a lipophilic group comprising an aliphatic bridging group, B is a lipophilic group, D is a group having at least one amino or substituted amino group and R is hydrogen, alkyl or cycloalkyl, and pharmaceutically acceptable salts and individual isomers thereof, which have growth hormone releasing activity in humans or animals.
摘要翻译：结构式（I）的化合物，其中A是包含脂族桥基的亲脂基团，B是亲脂基团，D是具有至少一个氨基或取代的氨基的基团，R是氢，烷基或环烷基，以及药学上可接受的其盐和单独的异构体，其在人或动物中具有生长激素释放活性

25. 发明授权

EP1021418B1 SUBSTITUTED 2,3-BENZODIAZEPIN-4-ONES AND THE USE THEREOF 失效
标题翻译：取代的2,3-苯并二氮杂4-ONE及其用途
公开(公告)号：EP1021418B1
公开(公告)日：2004-05-19
申请号：EP97916722.8
申请日：1997-03-21
申请人： Euro-Celtique S.A.
发明人： XIA, Haiji , FIELD, George , LAN, Nancy, C. , WANG, Yan , CAI, Sui, Xiong
IPC分类号： C07D243/02 , C07D491/056 , A61K31/55
CPC分类号： C07D491/04 , C07D243/02 , C07D243/10
摘要： The invention relates to substituted 2,3-benzodiazepin-4-ones which are antagonists or positive modulators of AMPA receptors, and the use thereof for treating, preventing or ameliorating neuronal loss associated with stroke, global and focal ischemia, CNS trauma, hypoglycemia and surgery, as well as treating or ameliorating neurodegenerative diseases including Alzheimer's disease, amyotrophic lateral sclerosis, Huntington's disease, Parkinson's disease and Down's syndrome, treating, preventing or ameliorating the adverse consequences of the overstimulation of the excitatory amino acids, treating or ameliorating anxiety, psychosis, convulsions, chronic pain, glaucoma, CMV retinitis, urinary incontinence, muscular spasm and inducing anesthesia, as well as for treating or ameliorating the adverse consequences of excitatory amino acid deficiency such as schizophrenia, Alzheimer's disease and malnutrition and neural maldevelopment, and as cognition enhancers. The invention also is directed to the process for the preparation of the substituted 2,3-benzodiazepin-4-ones.

26. 发明公开

EP1093372A1 CYCLIC AMINO ACID COMPOUNDS, PHARMACEUTICAL COMPOSITIONS COMPRISING SAME, AND METHODS FOR INHIBITING $g(b)-AMYLOID PEPTIDE RELEASE AND/OR ITS SYNTHESIS BY USE OF SUCH COMPOUNDS 审中-公开
标题翻译：氨基化合物，药物组合物时AND METHOD FOR抑制（B）淀粉样肽释放和/或其合成这些化合物的使用
公开(公告)号：EP1093372A1
公开(公告)日：2001-04-25
申请号：EP99930600.4
申请日：1999-06-22
申请人： Elan Pharmaceuticals, Inc. , Eli Lilly & Company
发明人： AUDIA, James, E. , DRESSMAN, Bruce, A. , SHI, Qing
IPC分类号： A61K31/55 , C07D223/14 , C07D243/06 , C07D243/10 , C07D243/12 , C07D243/24 , C07D267/02 , C07D281/02 , C07D487/02 , C07D487/12 , C07D498/02 , C07D513/02
CPC分类号： A61K31/55 , A61K38/00 , C07D223/14 , C07D223/16 , C07D223/18 , C07D243/06 , C07D243/10 , C07D243/12 , C07D243/14 , C07D243/24 , C07D267/02 , C07D267/14 , C07D281/02 , C07D281/10 , C07D401/04 , C07D401/12 , C07D403/12 , C07D409/04 , C07D409/12 , C07D417/04 , C07D471/04 , C07D471/06 , C07D471/08 , C07D487/02 , C07D487/04 , C07D487/12 , C07D498/02 , C07D513/02 , C07K4/00
摘要： Disclosed are compounds which inhibit β-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits β-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.

27. 发明公开

EP0763537A3 Non-peptidyl Ras farnesyl transferase inhibitors 失效
标题翻译：非肽抑制剂Farnesyltransferas
公开(公告)号：EP0763537A3
公开(公告)日：1997-10-22
申请号：EP96118160.9
申请日：1994-05-10
申请人： GENENTECH, INC. , BOARD OF REGENTS THE UNIVERSITY OF TEXAS SYSTEM
发明人： Marsters, James C., Jr. , Brown, Michael S. , Crowley, Craig W. , Goldstein, Joseph L. , James, Guy L. , McDowell, Robert S. , Oare, David , Rawson, Thomas E. , Reynolds, Mark , Somers, Todd C.
IPC分类号： C07D487/04 , A61K31/41 , C07D498/04 , A61K31/42 , C07D513/04 , A61K31/425
CPC分类号： C07D223/16 , A61K38/00 , C07D243/10 , C07D243/24 , C07D401/06 , C07D401/14 , C07D403/06 , C07D403/10 , C07D403/12 , C07D403/14 , C07D405/06 , C07D409/14 , C07D487/04 , C07D513/04 , C07K5/0207 , C07K5/0606 , C07K5/06139 , C07K5/06191 , C07K5/081 , C07K5/0821 , C07K5/0827 , C07K5/1013 , C07K5/1024 , C07K5/1027
摘要： Benzodiazepine derivatives are disclosed that act as potent inhibitors of ras farnesyl:protein transferase. Pharmaceutical compositions containing these benzodiazepines are provided for treatment of diseases for which inhibition of the ras farnesyl:protein transferase is indicated.

28. 发明授权

EP0610334B1 NONPEPTIDYL INTEGRIN INHIBITORS HAVING SPECIFICITY FOR THE GPII B III A RECEPTOR 有权
标题翻译：非肽整合素具有特异性抑制剂用于糖蛋白IIb IIIa受体
公开(公告)号：EP0610334B1
公开(公告)日：1996-01-24
申请号：EP92922468.1
申请日：1992-10-15
申请人： GENENTECH, INC.
发明人： BLACKBURN, Brent , BARKER, Peter , GADEK, Thomas , McDOWELL, Robert , McGEE, Lawrence , SOMERS, Todd , WEBB, Rob , ROBARGE, Kirk
IPC分类号： C07D243/14 , A61K31/55 , C07D223/16 , C07D267/14
CPC分类号： C07D223/16 , C07D243/10 , C07D243/14 , C07D267/14
摘要： A benzodiazepinedione derivative which acts as a nonpeptidyl platelet aggregation inhibitor is provided. This inhibitor potently inhibits fibrinogen binding to the GPIIbIIIa receptor and is provided in therapeutic compositions for the treatment of diseases for which blocking platelet aggregation is indicated. These nonpeptidyl inhibitors are provided in combination with thrombolytics and anticoagulants.

29. 发明授权

EP0496561B1 [[(2-Amino-3,4-dioxo-1-cyclobuten-1-yl)amino]alkyl]-acid derivatives 有权转让
标题翻译： [[（2-氨基-3,4-二氧代-1-环丁烯-1-基）氨基]烷基]säurederivate。
公开(公告)号：EP0496561B1
公开(公告)日：1995-03-15
申请号：EP92300472.5
申请日：1992-01-20
申请人： AMERICAN HOME PRODUCTS CORPORATION
发明人： Kinney, William Alvin , Garrison, Deanna Colette
IPC分类号： C07C229/16 , C07D271/06 , C07D403/06 , C07F9/6509 , C07F9/38 , A61K31/195 , A61K31/66 , A61K31/675 , A61K31/495
CPC分类号： C07D271/07 , C07C229/16 , C07C2601/04 , C07D243/10 , C07D403/06 , C07F9/3808 , C07F9/3826 , C07F9/4006 , C07F9/645 , C07F9/650994

30. 发明公开

EP0001560A3 UV-LIGHT-STABILIZED COMPOSITIONS CONTAINING SUBSTITUTED 1,5-DIAZACYCLOALKANES AND 2-KETO-1,5-DIAZACYCLOALKANES, NOVEL COMPOUNDS AND SYNTHESIS THEREOF 失效
标题翻译：包含取代的1,5-二氮杂环戊烷和2-酮咪-1,5-二氮杂环戊烷的紫外光稳定组合物，新型化合物及其合成
公开(公告)号：EP0001560A3
公开(公告)日：1979-06-13
申请号：EP78100941
申请日：1978-09-20
申请人： THE B.F. GOODRICH COMPANY
发明人： LAI, JOHN TA-YUAN , SON, PYONG NAE
IPC分类号： C07D243/08 , C07D243/10 , C07D243/12 , C07D245/02 , C08K5/3442 , C09K15/30 , C08K5/34
CPC分类号： C07D243/12 , C07D243/08 , C07D243/10 , C08K5/3442
摘要： Novel polysubstituted 1,5-diazacycloalkanes and polysubstituted 2-keto-1,5- diazcycloalkanes are powerful stabilizers for materials subject to ultraviolet (UV) light degradation, particularly for polyolefins. The cyclic compounds of this invention have (a) a fixed three-carbon bridge between the N¹ and N⁵ atoms of the diaza ring, the remaining portion of the ring having a variable length bridge of two or more carbon atoms, (b) an N-adjacent carbon atom of the diaza ring is polysubstituted, that is, has two substituents which may be cyclizable.
Compositions containing (a) the polysubstituted 1,5-diazacycloalkanes and polysubstituted 2-keto-1,5- diazacycloalkanes of this invention, and (b) prior art polysubstituted 1,5-diazacycloalkanes and polysubstituted 2-keto-1,5-diazacycloalkanes, exhibit excellent stability to UV light.
A novel synthesis for preparing polysubstituted 2-keto-1,5- diazacycloalkanes is disclosed.
摘要翻译：新型多取代的1,5-二氮杂环烷烃和多取代的2-酮-1,5-二氮杂环烷烃是经受紫外线（UV）光降解的材料的强大稳定剂，特别是对于聚烯烃。本发明的环状化合物具有（a）在氮杂环的N 1和N 5原子之间的固定的三碳桥，所述环的剩余部分具有两个或多个碳原子的可变长度桥，（b）N 二氮杂环的相邻碳原子是多取代的，即具有可以可环化的两个取代基。包含（a）本发明的多取代的1,5-二氮杂环烷烃和多取代的2-酮-1,5-二氮杂环烷烃的组合物和（b）现有技术的多取代的1,5-二氮杂环烷烃和多取代的2-酮-1,5-二氮杂环烷对紫外光表现出优异的稳定性。公开了一种制备多取代2-酮-1,5-二氮杂环烷烃的新型合成方法。

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