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1. 发明申请

WO2011051490A2 HETEROCYCLIC DERIVATIVES 审中-公开
标题翻译：杂环衍生物
公开(公告)号：WO2011051490A2
公开(公告)日：2011-05-05
申请号：PCT/EP2010/066584
申请日：2010-11-02
申请人： N.V. ORGANON , ADAM, Julia , GILLESPIE, Jonathan , LAATS, Steven , MACLEAN, John Kinnaird Ferguson , McARTHUR, Duncan Robert
发明人： ADAM, Julia , GILLESPIE, Jonathan , LAATS, Steven , MACLEAN, John Kinnaird Ferguson , McARTHUR, Duncan Robert
IPC分类号： C07D401/10
CPC分类号： C07D401/10 , C07D401/14 , C07D403/10 , C07D405/14 , C07D413/10
摘要： The present invention relates to a heterocyclic derivative of formula (I) wherein the variables are as defined in the specification, or to a pharmaceutically acceptable salt or solvate thereof. The present invention further relates to pharmaceutical compositions comprising said heterocyclic derivatives and to their use in therapy, for instance in the treatment or prevention of disorders mediated by glutamate dysfunction, such as schizophrenia and generalised anxiety disorder.
摘要翻译：本发明涉及式（I）的杂环衍生物或其药学上可接受的盐或溶剂化物，其中变量如说明书中所定义。本发明进一步涉及包含所述杂环衍生物的药物组合物，并涉及它们在治疗中的应用，例如治疗或预防由谷氨酸功能障碍如精神分裂症和广泛性焦虑症所介导的障碍。

2. 发明申请

WO2011051490A3 HETEROCYCLIC DERIVATIVES 审中-公开
标题翻译：杂环衍生物
公开(公告)号：WO2011051490A3
公开(公告)日：2011-06-23
申请号：PCT/EP2010066584
申请日：2010-11-02
申请人： ORGANON NV , ADAM JULIA , GILLESPIE JONATHAN , LAATS STEVEN , MACLEAN JOHN KINNAIRD FERGUSON , MCARTHUR DUNCAN ROBERT
发明人： ADAM JULIA , GILLESPIE JONATHAN , LAATS STEVEN , MACLEAN JOHN KINNAIRD FERGUSON , MCARTHUR DUNCAN ROBERT
IPC分类号： C07D401/10 , A61K31/4178 , A61K31/422 , A61K31/4439 , A61K31/4725 , A61P25/18 , A61P25/22 , C07D401/14 , C07D403/10 , C07D405/14 , C07D413/10
CPC分类号： C07D401/10 , C07D401/14 , C07D403/10 , C07D405/14 , C07D413/10
摘要： The present invention relates to a heterocyclic derivative of formula (I) wherein the variables are as defined in the specification, or to a pharmaceutically acceptable salt or solvate thereof. The present invention further relates to pharmaceutical compositions comprising said heterocyclic derivatives and to their use in therapy, for instance in the treatment or prevention of disorders mediated by glutamate dysfunction, such as schizophrenia and generalised anxiety disorder.
摘要翻译：本发明涉及式（I）的杂环衍生物，其中变量如说明书中所定义，或其药学上可接受的盐或溶剂合物。本发明还涉及包含所述杂环衍生物的药物组合物及其在治疗中的用途，例如用于治疗或预防由谷氨酸盐功能障碍如精神分裂症和广泛性焦虑症介导的障碍。

3. 发明申请

WO2008020081A1 6-SUBSTITUTED ISOQUINOLINE DERIVATIVES AS ROCK-1 INHIBITORS 审中-公开
标题翻译： 6取代的异喹啉衍生物作为ROCK-1抑制剂
公开(公告)号：WO2008020081A1
公开(公告)日：2008-02-21
申请号：PCT/EP2007/058593
申请日：2007-08-17
申请人： N.V. ORGANON , RAY, Peter, Christopher , LAATS, Steven , MORPHY, John, Richard , SHERBORNE, Brad
发明人： RAY, Peter, Christopher , LAATS, Steven , MORPHY, John, Richard , SHERBORNE, Brad
IPC分类号： C07D217/22 , C07D217/24 , A61K31/472 , A61P9/10 , A61P27/06
CPC分类号： C07D217/22 , C07D217/24
摘要： The present invention relates to 6-substituted isoquinoline derivatives having the general Formula I wherein X is O, S or NH; Y is OH or NH 2 ; m is 0, 1 or 2; n is 0 or 1; o is 0 or 1; R 1 is H, when Y is NH 2 ; or R 1 is H, (C 1-4 )alk yl or halogen, when Y is OH; R 2 and R 3 are independently H, (C 1-4 )alkyl or halogen; R 4 is H or (C 1-6 )alkyl, optionally substituted with halogen, (C 3-7 )cycloalkyl, (C 6-10 )aryl or a saturated 5- or 6-membered heterocyclic ring comprising 1-3 heteroatoms independently selected from O, S and N, the (C 6-10 )aryl and heterocyclic ring being optionally substituted with (C 1-4 )alkyl, (C 1-4 )alkyloxy or halogen; R 5 is H or (C 1-4 )alkyl; or a pharmaceutically acceptable salt thereof, with the proviso that the compounds of Formula I wherein X is O, Y is OH, n is 0 and m+o =2 are excluded, to pharmaceutical compositions comprising the same, as well as to the use of said 6-substituted isoquinoline derivatives for the preparation of a medicament for the treatment of ROCK-I related disorders such as glaucoma, hypertension and atherosclerosis.
摘要翻译：本发明涉及具有通式I的6-取代的异喹啉衍生物，其中X是O，S或NH; Y是OH或NH 2; m为0,1或2; n为0或1; o为0或1; R 1是H，当Y是NH 2时; 或者R 1是H，（C 1-4）烷基或卤素，当Y是OH时; R 2和R 3独立地是H，（C 1-4烷基）烷基或卤素; R 4是H或（C 1-6 - ）烷基，任选被卤素，（C 3-7）环烷基取代，（C 1 -C 6）（C 6-10）芳基或饱和的5-或6-元杂环，其包含1-3个独立地选自O，S和N的杂原子，芳基和杂环任选被（C 1-4烷基）烷基，（C 1-4-4烷基）烷氧基或卤素取代; R 5是H或（C 1-4烷基）烷基; 或其药学上可接受的盐，条件是其中X为O，Y为OH，n为0且m + o = 2的式I化合物排除于包含该化合物的药物组合物中，以及使用的所述6-取代的异喹啉衍生物用于制备用于治疗ROCK-1相关疾病如青光眼，高血压和动脉粥样硬化的药物。

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