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    NEW 2, 1 L -DIAZA-[3.3](2,6)PYRIDINOPHANE COMPOUNDS AND THEIR APPLICATION AS LIGANDS OF ESSENTIAL METAL ION BASED MRI CONTRAST AGENTS AND 52MN BASED PET CONTRAST AGENTS
    21.
    发明公开
    NEW 2, 1 L -DIAZA-[3.3](2,6)PYRIDINOPHANE COMPOUNDS AND THEIR APPLICATION AS LIGANDS OF ESSENTIAL METAL ION BASED MRI CONTRAST AGENTS AND 52MN BASED PET CONTRAST AGENTS 审中-公开

    公开(公告)号：EP3380473A1

    公开(公告)日：2018-10-03

    申请号：EP16819646.7

    申请日：2016-11-25

    申请人： Debreceni Egyetem

    发明人： BOTÁR, Richárd ,  GARDA, Zoltán ,  FODOR, Tamás ,  KÁLMÁN, Ferenc Krisztián ,  NAGY, Victória ,  TIRCSÓ, Gyula ,  TÓTH, Imre

    IPC分类号： C07D471/18 ,  A61K49/12 ,  A61K51/04

    CPC分类号： C07D471/18 ,  A61K51/0472 ,  A61K51/0482 ,  A61K2123/00

    摘要： The one subject of the invention is the compounds of general formula (I), their isomers, their physiologically acceptable salts and/or Mn(II), Fe(II), Fe(III), Co(II) and Ni(II) complexes. The other subject of the invention is the application of the above compounds. The compounds of general formula (I): wherein -NRR1 group may refer to: a) -NRR1 with N atom in the ring means a ring of 4 to 7, that in certain cases may contain another heteroatom, and in specific cases the ring may be replaced with an aryl group (of 5 to 7 carbon atoms) substituted with -COOH, -OH, -OCH3, -NO2, -NH2, -NCS, -NHS- activated ester, aryl (of 5 to 7 carbon atoms), or nitro-, amino- or isothiocyanate group, or b) in the -NRR1 group R means a H atom, alkyl, aryl, nitroaryl, aminoaryl or isothiocyanate-aryl group (of 1 to 6 carbon atoms) and R4 is a H atom, alkyl (of 1 to 6 carbon atoms) or -(CH2)n-COOH group, whereas n=1 to 10 integer, or c) -NRR1 group is one of the following groups: (formula II) whereas R2 is a H atom, carboxyl- or alkyl-carbonyl group (of 1 to 4 carbon atoms);(formula III) and R2 is a H atom or alkyl or aryl group (of 1 to 6 carbon atoms), and X means independently from one another H atom, -CH3, -COOH, -OH, -OCH3, alkoxy- (of 2 to 6 carbon atoms), -NO2, -NH2, -NCS, -NHS -activated ester, alkyl (of 2 to 12 carbon atoms) or aryl (of 5 to 7 carbon atoms) group, in certain cases the latter may be substituted with hydroxyl, hydroxyalkyl (of 1 to 6 carbon atoms), nitro, amino or isothiocyanate group.

    AZAMOPHINAN DERIVATIVES AND USE THEREOF
    25.
    发明公开
    AZAMOPHINAN DERIVATIVES AND USE THEREOF 审中-公开

    公开(公告)号：EP3154972A4

    公开(公告)日：2017-11-22

    申请号：EP15807396

    申请日：2015-06-12

    申请人： PURDUE PHARMA LP

    发明人： PARK JAE HYUN ,  TAFESSE LAYKEA

    IPC分类号： C07D471/08 ,  A61K31/485 ,  A61P1/12 ,  A61P23/00 ,  A61P25/30 ,  C07D471/18

    CPC分类号： C07D471/08 ,  C07D471/18

    摘要： The application is directed to compounds of Formula (I) and pharmaceutically acceptable salts and solvates thereof, wherein R1, R2, R3, R4, Y, and Z are defined as set forth in the specification. The invention is also directed to use of compounds of any one of Formulae I-VIII, and the pharmaceutically acceptable salts and solvates thereof, to treat disorders responsive to the modulation of one or more opioid receptors, or as synthetic intermediates. Certain compounds of the invention are especially useful for treating pain.

    TRICYCLIC COMPOUNDS AS ALPHA-7 NICOTINIC ACETYLCHOLINE RECEPTOR LIGANDS
    28.
    发明公开
    TRICYCLIC COMPOUNDS AS ALPHA-7 NICOTINIC ACETYLCHOLINE RECEPTOR LIGANDS 有权
    TRICYCLISCHE VERBINDUNGEN ALS NIKOTINISCHE ALPHA-7-ACETYLCHOLINREZEPTORLIGANDEN

    公开(公告)号：EP3154973A1

    公开(公告)日：2017-04-19

    申请号：EP15729057.8

    申请日：2015-06-05

    申请人： Bristol-Myers Squibb Company

    发明人： MCDONALD, Ivar M. ,  ZUSI, F. Christopher ,  OLSON, Richard E.

    IPC分类号： C07D471/18 ,  A61K31/4748 ,  A61P25/00

    CPC分类号： C07D471/18

    摘要： The disclosure provides compounds of formula I including their salts, as well as compositions and methods of using the compounds. The compounds are ligands for the nicotinic 7 receptor and may be useful for the treatment of various disorders of the central nervous system, especially affective and neurodegenerative disorders. [INSERT CHEMICAL STRUCTURE HERE] I

    摘要翻译： 本公开提供式I化合物，包括其盐，以及使用该化合物的组合物和方法。 这些化合物是烟碱7受体的配体，可用于治疗中枢神经系统的各种疾病，特别是情感和神经变性疾病。 [INSERT CHEMICAL STRUCTURE HERE] I