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41. 发明公开

EP2044001A1 PROCESS FOR PREPARATION OF 3-(2-HYDROXY-5-SUBSTITUTED PHENYL)-N-ALKYL-3-PHENYLPROPYLAMINES 有权
标题翻译： PROCESS FOR 3-（2-羟基-5-取代的苯基）的制备-N-烷基-3-苯基丙胺
公开(公告)号：EP2044001A1
公开(公告)日：2009-04-08
申请号：EP07726062.8
申请日：2007-06-18
申请人： Lek Pharmaceuticals D.D.
发明人： FISCHER, Erik
IPC分类号： C07C213/08 , C07C215/54 , C07C253/30 , C07C255/59
CPC分类号： C07C213/08 , C07B2200/07 , C07C253/30 , C07C215/54 , C07C255/59
摘要： A new process for preparation of 3-(2-hydroxy-5-substituted phenyl)-N,alkyl-3- phenylpropylamiηes from cinamoyl chloride via N-alky-3-phenylprop-2-en-1 -amine has been developed.

42. 发明公开

EP1818325A2 3,4-DI-substituted cyclobutene-1,2-diones as CXC-chemokine receptor ligands 有权
标题翻译： 3,4-DI取代物环丁烷-1,2-二酮αCXC-Chemokin-Rezeptorliganden
公开(公告)号：EP1818325A2
公开(公告)日：2007-08-15
申请号：EP07010711.5
申请日：2002-04-15
申请人： SCHERING CORPORATION , Pharmacopeia Drug Discovery, Inc.
发明人： Taveras, Arthur G. , Aki, Cynthia J. , Bond, Richard W. , Chao, Jianping , Dwyer, Michael , Ferreira, Johan A. , Chao, Jianhua , Yu, Younong , Baldwin, John J. , Kaiser, Bernd , Li, Ge , Merritt, Robert J. , Nelson, Kingsley H. , Rokosz, Laura L.
IPC分类号： C07C237/30 , C07C255/59 , C07C225/20 , C07D213/74 , C07D307/52 , C07D333/36
CPC分类号： C07D231/38 , C07C225/20 , C07C237/30 , C07C255/59 , C07C2601/04 , C07D213/74 , C07D307/52 , C07D333/36
摘要： There are disclosed compounds of the formula

or a pharmaceutically acceptable salt or solvate thereof which are useful for the treatment of chemokine-mediated diseases such as acute and chronic inflammatory disorders and cancer.
摘要翻译：公开了可用于治疗趋化因子介导的疾病如急性和慢性炎症性疾病和癌症的具有下式的化合物或其药学上可接受的盐或溶剂合物。

44. 发明公开

EP1787983A1 PROCESS FOR THE PRODUCTION OF ISOINDOLE DERIVATIVES 有权
标题翻译： VERFAHREN ZUR HERSTELLUNG VON ISOINDOLDERIVATEN
公开(公告)号：EP1787983A1
公开(公告)日：2007-05-23
申请号：EP05766977.2
申请日：2005-07-27
申请人： Eisai R&D Management Co., Ltd.
发明人： YOSHIZAWA, Kazuhiro, EISAI CO., LTD. , NAKAMURA, Taiju, EISAI CO., LTD. , NEGI, Shigeto, EISAI CO., LTD.
IPC分类号： C07D209/44 , C07C255/59
CPC分类号： C07C255/59 , C07D209/44
摘要： The present invention relates to a method for producing an isoindole derivative (compound (II)) with the following general formula (II):

(wherein R 1 and R 2 each independently represents a C 1-6 alkyl group) or a salt thereof, comprising the step of cyclizing, in a solvent, compound (I) with the following general formula (I):

(wherein R 1 and R 2 have the same meanings as R 1 and R 2 in formula (II) above) or a salt thereof, or their hydrate or solvate in the presence of a base (Step 1).
摘要翻译：本发明涉及具有下列通式（II）的异吲哚衍生物（化合物（II））的制造方法：（其中R 1和R 2各自独立地表示C 1-6烷基）或其盐，包括在溶剂中使具有以下通式（I）的化合物（I）环化的步骤：（其中R 1和R 2具有与上述式（II）中的R 1和R 2相同的含义）或盐或其水合物或溶剂化物在碱的存在下进行（步骤1）。

45. 发明公开

EP1439164A4 NOVEL PHENYLETHANOLAMINE COMPOUNDS HAVING BETA2-ACCEPTOR EXCITATORY FUNCTION AND THEIR PREPARATION METHOD 有权
标题翻译：随着对效果令人振奋的BETA2受体和方法的新PHENYLETHANOLAMINVERBINDUNGEN及其
公开(公告)号：EP1439164A4
公开(公告)日：2005-12-21
申请号：EP02771983
申请日：2002-09-25
申请人： UNIV SHENYANG PHARMACEUTICAL , JINZHOU JIUTAI PHARMACEUTICAL
发明人： CHENG MAOSHENG , PAN LI , LI LEI , ZHANG LI , SHEN JIANMIN , SONG GUILAN , LI ZHIQING
IPC分类号： A61P11/04 , A61K31/137 , A61K31/275 , A61P11/00 , A61P11/06 , A61P29/00 , A61P43/00 , C07C213/04 , C07C215/28 , C07C215/68 , C07C217/76 , C07C255/59 , A61K31/135
CPC分类号： C07C215/68 , C07C255/59 , C07C2601/02 , C07C2601/04 , C07C2601/14
摘要： The invention provides compounds of formula (I) and their medicinal salts: In which, R1 is H, CI or Br; R2 is selected from electron-withdrawing group of -CF3, -CN, -F, -COSO3H, -CF3SO3 and -NO2; R3 is C1-10 linear or branched alkyl, C2-10 linear or branched alkoxyalkyl, C1-10 aliphatic alkohol or C3-6 cycloalkyl. The invention also relates to the preparation method of said compounds and the compositions containing the same. The inventive compounds have β2- acceptor excitatory function and can be used to treat asthma and bronchitis.
摘要翻译：本发明提供式（I）及其药学上可接受的盐的化合物及其，worin R 1为H，氯，或溴; R 2是选自CF 3，CN，氟，CH 3 SO 3，CF 3 SO 3和NO 2的选择的吸电子基团; R 3是直链或具有1至10个碳原子的直链或支链烷氧基烷基具有含1至10个碳原子，或具有3至6个碳原子的环烷基含2-10个碳原子，脂肪族醇支链烷基。因此，本发明涉及的方法用于制备所述化合物和组合物 - 所述相同。本发明的化合物具有的β2受体激动剂的作用，并且可以用于治疗哮喘和支气管炎的治疗。

46. 发明授权

EP1268396B1 DIPHENYL ETHER COMPOUNDS USEFUL IN THERAPY 有权
标题翻译： THERAPEUTIC SUITABLE二苯基醚
公开(公告)号：EP1268396B1
公开(公告)日：2005-07-20
申请号：EP01917347.5
申请日：2001-03-19
申请人： Pfizer Limited , Pfizer Inc.
发明人： ANDREWS, Mark, David , HEPWORTH, David , MIDDLETON, Donald, Stuart , STOBIE, Alan
IPC分类号： C07C217/58 , C07C229/38 , C07C237/28 , C07C255/43 , C07C255/59 , C07C311/05 , C07C311/08 , C07C311/37 , C07C317/32 , C07C323/20 , C07C323/32 , C07C323/67 , C07D207/12 , C07D231/38 , C07D233/61 , C07D249/06 , C07D249/08 , C07D295/08 , C07D295/18 , A61K31/137
CPC分类号： H04L12/14 , C07C45/71 , C07C47/55 , C07C47/575 , C07C205/44 , C07C217/58 , C07C229/38 , C07C237/28 , C07C255/43 , C07C255/59 , C07C311/05 , C07C311/08 , C07C311/37 , C07C317/32 , C07C323/20 , C07C323/32 , C07C323/67 , C07C2601/02 , C07C2601/08 , C07D231/12 , C07D231/38 , C07D233/56 , C07D249/06 , C07D249/08 , C07D295/096 , C07D295/192 , G06F11/2038 , G06F11/2097 , H04L12/1403
摘要： A compound of general formula (I), or pharmaceutically acceptable salts, solvates or polymorphs thereof; wherein R3 is independ ently CF¿3?, OCF3, C1-C4alkylthio or C1-C4alkoxy; n is 1, 2 or 3; and the other variables are as defined in the claims. These compounds inhibit monoamine re-uptake and in particular exhibit activity as selective serotonin re-uptake inhibitors. They are useful in disorders such as depression, attention deficit hyperactivity disorder, obsessive-compulsive disorder, post-traumatic stress disorder, substance abuse disorders and sexual dysfunction including premature ejaculation.

47. 发明授权

EP1149069B1 PHENYLGLYCINE DERIVATIVES 有权
标题翻译：苯基甘氨酸衍生物
公开(公告)号：EP1149069B1
公开(公告)日：2004-08-25
申请号：EP99962221.0
申请日：1999-12-06
申请人： F. HOFFMANN-LA ROCHE AG
发明人： ACKERMANN, Jean , ALIG, Leo , CHUCHOLOWSKI, Alexander , GROEBKE, Katrin , HILPERT, Kurt , KUEHNE, Holger , OBST, Ulrike , WEBER, Lutz , WESSEL, Hans, Peter
IPC分类号： C07C257/18 , C07C259/18 , C07D295/155 , C07D211/46 , A61K31/155 , A61K31/40 , A61K31/435 , C07D211/96 , C07D309/12 , C07D213/74 , A61K31/34 , A61P7/02 , C07C255/59
CPC分类号： C07D207/27 , C07C257/18 , C07C259/18 , C07C2601/08 , C07C2601/14 , C07D207/12 , C07D209/48 , C07D211/46 , C07D211/58 , C07D211/96 , C07D213/30 , C07D213/55 , C07D213/65 , C07D213/74 , C07D231/12 , C07D233/56 , C07D233/64 , C07D235/18 , C07D249/08 , C07D261/04 , C07D271/06 , C07D277/24 , C07D295/155 , C07D307/12 , C07D307/20 , C07D307/54 , C07D309/12 , C07D309/14 , C07D317/64 , C07D319/18 , C07D321/10 , C07D333/24 , C07D335/04 , C07D403/12
摘要： The invention is concerned with novel N-(4-carbamimidoyl-phenyl)-glycine derivatives of formula (I), wherein R?1, E, X1 to X4 and G1 and G2¿ are as defined in the description and the claims, as well as hydrates or solvates and physiologically usable salts thereof.

48. 发明授权

EP1208077B1 2-HYDROXY-5-AMINO-BIPHENYL-DERIVATE SOWIE DIESE VERBINDUNGEN ENTHALTENDE OXIDATIONSHAARFÄRBEMITTEL 有权
标题翻译： 2-羟基-5-氨基联苯衍生物和含有它们的氧化头发
公开(公告)号：EP1208077B1
公开(公告)日：2004-04-21
申请号：EP01936066.8
申请日：2001-03-10
申请人： Wella Aktiengesellschaft
发明人： CHASSOT, Laurent , BRAUN, Hans-Jürgen
IPC分类号： C07C215/76 , C07C215/78 , C07C215/80 , C07C217/80 , C07C255/59 , C07C225/22 , C07C323/31 , C07D317/58 , C07D209/08 , A61K7/13 , D06P1/32
CPC分类号： C07D317/58 , A61K8/415 , A61Q5/10 , C07C215/76 , C07C215/78 , C07C215/80 , C07C217/80 , C07C225/22 , C07C255/59 , C07C323/31 , C07D209/08
摘要： The invention relates to an oxidative colouring agent for keratin fibres, in particular hair, based on a developing agent-coupling agent combination, which contains as a developing agent, at least one 2-hydroxy-5-amino-biphenyl derivative of general formula (I), in addition to novel 2-hydroxy-5-amino-biphenyl derivatives.

49. 发明公开

EP0957907A4 IL-8 RECEPTOR ANTAGONISTS 失效
标题翻译： IL-8-REZEPTOR-ANTAGONISTEN
公开(公告)号：EP0957907A4
公开(公告)日：2001-08-16
申请号：EP97936438
申请日：1997-08-06
申请人： SMITHKLINE BEECHAM CORP
发明人： WIDDOWSON KATHERINE L , GLEASON JOHN GERALD
IPC分类号： A61P1/00 , A61K31/135 , A61K31/165 , A61K31/18 , A61K31/275 , A61K31/277 , A61P1/04 , A61P7/02 , A61P9/00 , A61P11/00 , A61P11/06 , A61P13/12 , A61P17/00 , A61P17/06 , A61P25/28 , A61P31/00 , A61P37/06 , A61P43/00 , C07C255/59 , C07C211/22 , C07C233/09
CPC分类号： C07C255/59 , A61K31/275 , A61K31/277
摘要： This invention relates to novel compounds, pharmaceutical compositions comprising these compounds and their use in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).
摘要翻译：本发明涉及新化合物，包含这些化合物的药物组合物及其用于治疗由趋化因子介导的疾病状态白细胞介素-8（IL-8）的用途。

50. 发明公开

EP1090911A3 Bis(aminostyryl) anthracene compound, synthesis intermediate thereof, and process for production thereof 有权
标题翻译：双（氨基苯乙烯基）蒽的化合物，其合成中间体和它们的制备的方法
公开(公告)号：EP1090911A3
公开(公告)日：2001-08-08
申请号：EP00121754.6
申请日：2000-10-05
申请人： SONY CORPORATION
发明人： Ichimura, Mari , Ishibashi, Tadashi , Tamura, Shinichiro
IPC分类号： C07C255/58 , C07C255/59 , C07C255/52 , C07F9/40 , C07F9/54
CPC分类号： C07F9/5456 , C07C255/52 , C07C255/58 , C07C255/59 , C07F9/4025
摘要： A bis(aminostyryl)anthracene compound represented by the general formula [I] or the like below. (where R 2 and R 3 each denotes an unsubstituted aryl group; R 1 and R 4 each denotes an aryl group having a specific substituent such as methoxy group; and R 5 and R 6 each denotes a cyano group or the like.) A process for producing a bis(aminostyryl)anthracene compound represented by the general formula [I] by condensation of, for example, 4-(N,N-diarylamino)benzaldehyde with diphosphonic ester or diphosphonium. The bis(aminostyryl)anthracene compound emits intense yellow or red light. The process permits efficient production of the bis(aminostyryl)anthracene compound. The bis(aminostyryl)anthracene compound emits intense yellow or red light. The process permits efficient production of the bis(aminostyryl)anthracene compound.
摘要翻译：由通式AIU或低于等为代表的双（氨基苯乙烯基）蒽化合物。（其中R <2>和R <3>的每个表示在unsubstituiertem芳基; R <1>和R <4>的每个表示具有特定取代基上的芳基：例如甲氧基;和R <5>和 [R <6>各自代表氰基或诸如此类。）一种用于生产由，例如，4-（N，N-二芳基）与二膦苯甲醛缩合用通式表示的AIU（氨基苯乙烯基）蒽化合物酯或二鏻。的双（氨基苯乙烯基）蒽化合物发出强黄色或红色的光。该方法允许有效地生产双（氨基苯乙烯基）蒽化合物。的双（氨基苯乙烯基）蒽化合物发出强黄色或红色的光。该方法允许有效地生产双（氨基苯乙烯基）蒽化合物。

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