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72. 发明授权

EP2997033B1 FUSED TRICYCLIC HETEROCYCLIC COMPOUNDS AS HIV INTEGRASE INHIBITORS 有权转让
标题翻译：融合三环杂环化合物作为HIV整合酶抑制剂
公开(公告)号：EP2997033B1
公开(公告)日：2017-11-15
申请号：EP14798188.0
申请日：2014-04-18
申请人： Merck Sharp & Dohme Corp.
发明人： COLEMAN, Paul J. , HARTINGH, Timothy J. , RAHEEM, Izzat T. , SCHREIER, John , SISKO, John T. , WAI, John , GRAHAM, Thomas , HU, Lihong , PENG, Xuanjia
IPC分类号： C07D491/16 , C07D471/16 , C07D487/16 , A61K31/5025 , A61K31/5365 , A61P31/18
CPC分类号： C07D498/16 , A61K31/4985 , A61K31/5383 , A61K45/06 , C07D471/16 , C07D487/16 , C07D491/16

73. 发明公开

EP3183249A1 1,4,7,10-TETRAZACYCLODODECANE BASED AGENTS TO TARGET BACTERIA AND ITS USE 有权
标题翻译：基于1,4,7,10-TETRAZACYCLODODECANE的靶向杀菌剂及其应用
公开(公告)号：EP3183249A1
公开(公告)日：2017-06-28
申请号：EP15754150.9
申请日：2015-08-18
申请人： Helmholtz-Zentrum für Infektionsforschung GmbH
发明人： BROENSTRUP, Mark , HU, Haiyu , SERGEEV, Galina , RAIS, Bushra , FETZ, Verena , FERREIRA, Kevin
IPC分类号： C07D403/14 , C07D257/02 , C07D491/16 , C07K9/00 , A61K38/14 , A61K31/4353 , A61P31/00
CPC分类号： C07H17/04 , A61K49/0023 , A61K49/0032 , A61K49/0052 , C07D257/02 , C07D403/14 , C07D491/16 , C12Q1/16 , G01N2800/26
摘要： The present invention relates to new compounds comprising a siderophore moiety as well as a core structure able to chelate a metal ion. Optionally, the compounds may have additionally a moiety with a functional element including a marker molecule, a bioactive agent, an activity based probe suitable to monitor the aberrant expression or activity of proteins involved in the initiation and progression of bacterial infection, or a compound useful for bacterial inhibition. In a further aspect, the present invention provides a pharmaceutical composition containing said compound, for example, said pharmaceutical composition is an antibiotic. Additionally, the present invention relates to the use of said compounds in diagnostic methods, in particular, imaging methods including SPEC, PET or MRI. In an embodiment of the present invention, the compound is part of a theranostic composition having both, therapeutic as well as diagnostic activities.
摘要翻译：本发明涉及包含铁载体部分以及能够螯合金属离子的核心结构的新化合物。任选地，所述化合物可以另外具有含功能元件的部分，所述功能元件包括标记分子，生物活性剂，适用于监测参与细菌感染的启动和进展的蛋白质的异常表达或活性的基于活性的探针，或可用的化合物用于细菌抑制。另一方面，本发明提供含有所述化合物的药物组合物，例如所述药物组合物是抗生素。另外，本发明涉及所述化合物在诊断方法中的用途，特别是涉及包括SPEC，PET或MRI的成像方法。在本发明的一个实施方案中，该化合物是具有治疗和诊断活性的诊断组合物的一部分。

74. 发明公开

EP2379515A4 BENZOXAZOLE-BASED FLUORESCENT METAL ION INDICATORS 有权
标题翻译：荧光金属离子的指标BENZOXAZOLBASIS
公开(公告)号：EP2379515A4
公开(公告)日：2012-07-04
申请号：EP09837113
申请日：2009-12-29
申请人： LIFE TECHNOLOGIES CORP
发明人： GEE KYLE , MARTIN VLADIMIR
IPC分类号： C07D263/56 , C07D263/57 , C07D401/04 , C07D413/04 , C07D417/04 , C07D471/06 , C07D491/16 , C07F3/04 , C09K11/06 , G01N33/52
CPC分类号： G01N21/75 , C07D263/56 , C07D263/57 , C07D401/04 , C07D413/04 , C07D417/04 , C07D471/06 , C07D491/16 , C09B57/00 , C09B57/02 , C09K11/06 , C09K2211/1007 , C09K2211/1014 , C09K2211/1029 , C09K2211/1033 , C09K2211/1037 , C09K2211/1048 , C09K2211/1088 , G01N33/582 , G01N33/84

75. 发明公开

EP2264038A1 OPTICALLY ACTIVE DIBENZAZEPINE DERIVATIVES 有权
标题翻译：光学活性的二氮杂吖庚因衍生物
公开(公告)号：EP2264038A1
公开(公告)日：2010-12-22
申请号：EP09730232.7
申请日：2009-04-08
申请人： Nippon Soda Co., Ltd.
发明人： KUBOTA, Yasushi , INOUE, Tsutomu
IPC分类号： C07D491/16 , C07D317/60
CPC分类号： C07D317/60 , C07D491/06 , C07D491/16 , C07D491/20
摘要： It is to provide a novel optically active dibenzazepine derivative having a high utility value as an asymmetric phase-transfer catalyst. It is an optically active 6,7-dihydro-5H-dibenzo[c,e]azepine derivative represented by the following formula (1'), (wherein R represents a divalent organic group for cross-linking the 1 st position and the 11 th position; R 1 and R 2 are the same or different, and represent a hydrogen atom, halogen atom, or organic group, or R 1 and R 2 together represent a divalent organic group; R 3' and R 4' are the same or different and represent a monovalent organic group, or R 3' and R 4' together form an organic group that forms a cyclic structure comprising an onium nitrogen atom; Ar represents a monovalent organic group; * represents optical activity, i.e., that one axially asymmetric isomer is present in excess of the other axially asymmetric isomer with respect to a bond axis that constitutes the biphenyl structure of the compound; and X - represents a counter anion).
摘要翻译：本发明提供作为非对称相转移催化剂具有高利用价值的新型光学活性二苯并氮杂衍生物。它是由下式（1'）表示的旋光的6,7-二氢-5H-二苯并[c，e]氮杂卓衍生物，（其中R代表用于交联第1位和第11位的二价有机基团 ; R1和R2相同或不同，表示氢原子，卤素原子或有机基团，或者R1和R2一起表示二价有机基团; R3'和R4'相同或不同并且表示一价有机基团，或者R3'和R4'一起形成形成包含氮原子的环状结构的有机基团; Ar表示一价有机基团; *表示光学活性，即一个轴向不对称异构体轴向超过另一个相对于构成化合物的联苯结构的键轴的不对称异构体;并且X-表示抗衡阴离子）。

76. 发明公开

EP2220068A1 4-PYRAZOLYL-N-ARYLPYRIMIDIN-2-AMINES AND 4-PYRAZOLYL-N-HETEROARYLPYRIMIDIN-2-AMINES AS JANUS KINASE INHIBITORS 有权转让
标题翻译： 4-吡唑基-N-芳基嘧啶-2-胺和4-吡唑基-N-HETEROARYLPYRIMIDIN -2-胺作为JANUS激酶抑制剂的
公开(公告)号：EP2220068A1
公开(公告)日：2010-08-25
申请号：EP08848610.5
申请日：2008-11-13
申请人： Incyte Corporation
发明人： LI, Yun-long , YAO, Wenqing , RODGERS, James D.
IPC分类号： C07D401/14 , C07D403/04 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D451/06 , C07D471/10 , C07D491/16 , C07D498/10 , C07D491/107 , A61K31/506 , A61P35/00
CPC分类号： C07D403/14 , C07D401/14 , C07D403/04 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D451/06 , C07D471/10 , C07D491/107 , C07D491/16 , C07D498/10
摘要： The present invention provides substituted bicyclic heteroaryl compounds, 5 including, for example, 4-pyrazoIyI-N-arylpyrirnidin-2-arnines and 4-pyrazolyl-N-heteroarylpyτimidin-2-amines that modulate the activity of kinases and are useful in the treatment of diseases related to activity of kinases including, for example, immune-related diseases, skin disorders, myeloid proliferative disorders, cancer, and other diseases.formule :(1)

77. 发明公开

EP1951842A1 VERWENDUNG VON RYLENDERIVATEN ALS PHOTOSENSIBILISATOREN IN SOLARZELLEN 有权
标题翻译：萘嵌苯衍生物作为在太阳能电池中使用的光敏剂
公开(公告)号：EP1951842A1
公开(公告)日：2008-08-06
申请号：EP06829934.6
申请日：2006-11-06
申请人： BASF SE , Max-Planck-Gesellschaft zur Förderung der Wissenschaften e.V.
发明人： PSCHIRER, Neil Gregory , EICKEMEYER, Felix , SCHÖNEBOOM, Jan , QU, Jianqiang , KÖNEMANN, Martin , MÜLLEN, Klaus , LI, Chen , HERRMANN, Andreas , ERK, Peter , NORDMANN, Gero , KUHN, Alfred , HAGFELDT, Anders , EDVINSSON, Tomas
IPC分类号： C09K11/06 , H01L31/0256 , H01L31/04 , H01L51/30 , H01L51/42 , C07D491/06 , C07D491/16 , C07D311/92 , C07D405/10 , C07D471/06 , C07D417/14 , C07D417/10 , C07D409/14 , C07D413/10 , C07D405/12
CPC分类号： H01G9/2031 , C07D221/18 , C07D311/78 , C07D311/92 , C07D405/04 , C07D405/12 , C07D409/14 , C07D413/04 , C07D417/04 , C07D417/14 , C07D471/06 , C07D491/06 , C09B5/62 , C09K11/06 , C09K2211/1007 , C09K2211/1011 , C09K2211/1014 , C09K2211/1029 , C09K2211/1033 , C09K2211/1037 , C09K2211/1044 , C09K2211/1048 , C09K2211/1059 , C09K2211/1088 , H01G9/2059 , H01L51/0053 , H01L51/006 , H01L51/0067 , H01L51/0068 , H01L51/0069 , H01L51/0071 , H01L51/4226 , Y02E10/542 , Y02E10/549
摘要： Use of rylene derivatives (I) in which the variables are defined as follows: X together Formulae (x1) (x2) (x3) both -COOM; Y a radical -L-NR1R2 (y1) -L- Z-R3 (y2) the other radical hydrogen; together Formulae (y3) (y4) both hydrogen; R optionally substituted (Het)aryloxy, (Het)arylthio; P -NR1R2; B alkylene; optionally substituted phenylene; combinations thereof; A -COOM; -SO3M; -PO3M2; D optionally substituted phenylene, naphthylene, pyridylene; M hydrogen; alkali metal cation; [NR5]4+; L chemical bond; optionally indirectly bonded, optionally substituted (Het)arylene radical; R1, R2 optionally substituted (cyclo)alkyl, (Het)aryl; together the nitrogen atom containing, optionally substituted ring; Z -O-; -S-; R3 optionally substituted alkyl, (Het)aryl; R' hydrogen; optionally substituted (cyclo)alkyl, (Het)aryl; R5 hydrogen; optionally substituted alkyl, (Het)aryl; m 0, 1, 2; n, p m=0: 0, 2, 4 with: n+p = 2, 4, optionally 0; m=1: 0, 2, 4 with: n+p = 0, 2, 4; m=2: 0, 4, 6 with: n+p = 0, 4, 6, or of mixtures thereof as photosensitizers in solar cells.

78. 发明授权

EP0831094B1 FUSED POLYCYCLIC HETEROCYCLE DERIVATIVES 失效
标题翻译：相关环的杂环化合物
公开(公告)号：EP0831094B1
公开(公告)日：2004-12-08
申请号：EP96920027.8
申请日：1996-05-31
申请人： Eisai Co., Ltd.
发明人： SUGUMI, Hiroyuki , NIIJIMA, Jun , KOTAKE, Yoshihiko , OKADA, Toshimi , KAMATA, Jun-ichi , YOSHIMATSU, Kentaro , NAGASU, Takeshi , NAKAMURA, Katsuji , UENAKA, Toshimitsu , YAMAGUCHI, Atsumi , YOSHINO, Hiroshi , KOYANAGI, Nozomu , KITO, Kyosuke
IPC分类号： C07D471/06 , C07D471/16 , C07D487/06 , C07D491/16 , C07D495/16 , C07D498/06 , C07D513/06 , A61K31/495 , A61K31/535 , A61K31/54 , C07D487/16
CPC分类号： C07D471/06 , C07D487/06 , C07D513/06

79. 发明公开

EP1320369A4 A METHOD OF ANALGESIA 有权
标题翻译：一种用于减少疼痛的感觉
公开(公告)号：EP1320369A4
公开(公告)日：2003-07-02
申请号：EP01982091
申请日：2001-09-11
申请人： WEX MEDICAL LTD
发明人： DONG QINGBIN , SHUM FRANK HAYKONG
IPC分类号： C07D491/16 , A61K31/506 , A61K31/517 , A61K31/519 , A61K31/52 , A61K45/00 , A61P23/02 , A61P25/04 , A61P29/00 , A61P43/00
CPC分类号： A61K31/519 , A61K31/506 , A61K31/517

80. 发明公开

EP1287002A1 CRF RECEPTOR ANTAGONISTS 审中-公开
标题翻译： CRF受体拮抗剂
公开(公告)号：EP1287002A1
公开(公告)日：2003-03-05
申请号：EP01937569.0
申请日：2001-05-18
申请人： Neurocrine Biosciences, Inc.
发明人： HADDACH, Mustapha , WILLIAMS, John, P. , MARINKOVIC, Dragan , BU, Jane, H.
IPC分类号： C07D498/16 , A61K31/535 , A61P25/22 , C07D513/16 , C07D491/16
CPC分类号： C07D491/16 , C07D498/16 , C07D513/16
摘要： CRF receptor antagonists are disclosed which have utility in the treatment of a variety of disorders, including the treatment of disorders manifesting hypersecretion of CRF in a warm-blooded animals, such as stroke. The CRF receptor antagonists of this invention have the following structure (I): including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof, wherein m, R, R1, R2, X, Y, A, B and C are as defined herein. Compositions containing a CRF receptor antagonist in combination with a pharmaceutically acceptable carrier are also disclosed, as well as methods for use of the same.

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