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    Enzyme inhibitor compounds
    5.
    发明授权
    Enzyme inhibitor compounds 有权

    公开(公告)号：US09150574B2

    公开(公告)日：2015-10-06

    申请号：US14344417

    申请日：2011-09-14

    申请人： David Evans ,  Allison Carley ,  Alison Stewart ,  Michael Higginbottom ,  Edward Savory ,  Iain Simpson ,  Marianne Nilsson ,  Martin Haraldsson ,  Erik Nordling ,  Tobias Koolmeister

    发明人： David Evans ,  Allison Carley ,  Alison Stewart ,  Michael Higginbottom ,  Edward Savory ,  Iain Simpson ,  Marianne Nilsson ,  Martin Haraldsson ,  Erik Nordling ,  Tobias Koolmeister

    IPC分类号： C07D471/02 ,  A61K31/55 ,  C07D471/04

    CPC分类号： C07D471/04

    摘要： 2-{4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]piperidin-1-yl}ethan-1-amine; 3-aminopropyl 4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]piperidine-1-carboxylate; 1-{4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]piperidin-1-yl}-4-(dimethylamino)butan-1-one; 5-amino-1-{4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]piperidin-1-yl}pentan-1-one; N-(2-aminoethyl)-4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]piperidine-1-carboxamide; N-(3-aminopropyl)-4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]piperidine-1-carboxamide; 4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]-N-[3-(dimethylamino)propyl]piperidine-1-carboxamide; 1-({4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]piperidin-1-yl}carbonyl)piperazine; 4-({4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]piperidin-1-yl}carbonyl)morpholine; 1-({4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]piperidin-1-yl}carbonyl)-1,4-diazepane; ethyl 1-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]piperidine-4-carboxylate; ethyl 1-[1-(4-methylphenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]piperidine-4-carboxylate; 1-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]piperidine-4-carboxylic acid; N-(2-aminoethyl)-1-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]piperidine-4-carboxamide; 4-({1-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]piperidin-4yl}carbonyl)morpholine; 1-({1-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]piperidin-4-yl}carbonyl)piperazine; {4-[1-(4-methylphenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]morpholin-3-yl}methanol; {4-[1-(4-methyl-phenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]morpholin-2-yl}methanol; [(3R)-4-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]morpholin-3-yl]methanol; methyl 4-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]morpholine-3-carboxylate; N-(2-aminoethyl)-4-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]morpholine-3-carboxamide; 2-{4-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]morpholin-3-yl}ethan-1-ol; methyl 1-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]piperidine-2-carboxylate; N-(2-aminoethyl)-1-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]piperidine-2-carboxamide; 1-({1-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]piperidin-2-yl}carbonyl)piperazine; 4-[1-(4-methylphenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]morpholine; 1-(4-chlorophenyl)-3-(piperidin-4-yl)-1H-pyrrolo[2,3-c]pyridin-4-ol; N-butyl-1-(4-chlorophenyl)-N-methyl-1H-pyrazolo[3,4-c]pyridin-3-amine; 1-[4-(fluoromethyl)phenyl]-3-(oxan-4-yl)-1H-pyrazolo[3,4-c]pyridine; and 3-({4-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]piperidin-1-yl}methyl)pyridine are useful for the inhibition of SSAO activity.

    Therapeutic compounds
    9.
    发明申请
    Therapeutic compounds 失效
    治疗化合物

    公开(公告)号：US20080076776A1

    公开(公告)日：2008-03-27

    申请号：US11823377

    申请日：2007-06-26

    申请人： Michael Higginbottom ,  Edward Savory ,  Giles Brown ,  Viet-Anh Horgan ,  Emma Chapman

    发明人： Michael Higginbottom ,  Edward Savory ,  Giles Brown ,  Viet-Anh Horgan ,  Emma Chapman

    IPC分类号： A61K31/497 ,  A61K31/52 ,  A61P43/00 ,  C07D487/00

    CPC分类号： C07H19/16

    摘要： Compounds of formula (I) below are disclosed. Their use as medicaments is described, in particular for the treatment of pain or inflammation: wherein: when X═Y=Z=OH, R1 is OCH2CF2CF3, phenoxy (substituted with 3-(4-trifluoromethylphenyl), 3,4-dichloro, (3-trifluoromethyl,4-fluoro), (3-trifluoromethyl,4-chloro), (3-chloro, 4-cyano), or 3,5-bis(trifluoromethyl)), 1-piperazinyl(4-(3,4-dichlorophenyl)), phenyl (substituted with 3,4-dichloro, 3,5-difluoro, 3,5-bis(trifluoromethyl) or 3,4,5-trifluoro) or 2-benzofuranyl; or when X═Y═OH and Z=OMe, R1 is OCH3, OCH2CHF2, OCH2cyclopentyl, O-(2,5-difluorophenyl) or (S)-sec-butylamino; or when X═H and Y=Z=OH, R1 is n-hexylamino or cyclopentylamino; or when (IV) X=Z=OH and Y═H, R1 is cyclopentylamino; or a pharmaceutically acceptable salt thereof.

    摘要翻译： 公开了下式（I）的化合物。 描述了其作为药物的用途，特别是用于治疗疼痛或炎症：其中：当XY = Z = OH时，R 1是OCH 2 2 CF 2 CF 3，苯氧基（被3-（4-三氟甲基苯基），3,4-二氯，（3-三氟甲基，4-氟），（3-三氟甲基，4-氯） ），（3-氯，4-氰基）或3,5-双（三氟甲基）），1-哌嗪基（4-（3,4-二氯苯基）），苯基（被3,4-二氯， 或三氟甲基或3,4,5-三氟）或2-苯并呋喃基; 或当XY-OH和Z = OMe时，R 1是OCH 3，OCH 2 CHF 2，OCH 环戊基，O-（2,5-二氟苯基）或（S） - 仲丁基氨基; 或当X-H和Y = Z = OH时，R 1是正己基氨基或环戊基氨基; 或当（IV）X = Z = OH和Y-H时，R 1是环戊基氨基; 或其药学上可接受的盐。