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1.发明公开
公开(公告)号：EP2895485A1
公开(公告)日：2015-07-22
申请号：EP13762483.9
申请日：2013-09-13
发明人： KOOLMAN, Hannes , BRAJE, Wilfried , MACK, Helmut , HAUPT, Andreas , RELO, Ana Lucia , DRESCHER, Karla , BAKKER, Margaretha Henrica Maria , LAKICS, Viktor , HOFT, Carolin , XU, Ruxu , ZHAO, Xiaona
IPC分类号： C07D471/06 , C07D487/06
CPC分类号： C07D471/06 , C07D487/06 , C07D487/16
摘要： The present invention relates to tricyclic quinoline and quinoxaline derivatives, to a pharmaceutical composition containing such compounds, to their use as modulators, especially agonists or partial agonists, of the 5-HT2C receptor, their use for preparing a medicament for the prevention or treatment of conditions and disorders which respond to the modulation of 5-HT2C receptor, and to a method for preventing or treating conditions and disorders which respond to the modulation of 5-HT2C receptor.
摘要翻译： 本发明涉及三环喹啉和喹喔啉衍生物，涉及含有这些化合物的药物组合物，其用作5-HT 2C受体的调节剂，特别是激动剂或部分激动剂，其用于制备预防或治疗 对5-HT 2C受体的调节作出反应的病症和障碍，以及用于预防或治疗对5-HT 2C受体调节作用的病症和障碍的方法。
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2.发明授权HETEROCYCLIC COMPOUNDS AS POSITIVE MODULATORS OF METABOTROPIC GLUTAMATE RECEPTOR 2 (MGLU2 RECEPTOR) 有权杂环化合物代谢型谷氨酸受体2（的mGlu2 PRS）作为正调节剂
公开(公告)号：EP2167464B1
公开(公告)日：2014-12-03
申请号：EP08759978.3
申请日：2008-05-23
发明人： GENESTE, Hervé , SAUER, Daryl , BRAJE, Wilfried , AMBERG, Wilhelm , MEZLER, Mario , BAKKER, Margaretha Henrica Maria
IPC分类号： C07D209/26 , C07D231/12 , C07D333/58 , C07D239/26 , C07D277/28 , C07D233/58 , C07D409/04 , C07D409/06 , C07D333/20 , C07D307/14 , C07D213/36 , C07D213/38
CPC分类号： C07D209/14 , C07D207/335 , C07D209/26 , C07D213/36 , C07D213/38 , C07D215/12 , C07D231/12 , C07D233/58 , C07D239/26 , C07D261/08 , C07D277/28 , C07D307/14 , C07D307/54 , C07D333/20 , C07D333/58 , C07D407/04 , C07D409/04 , C07D409/06
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3.发明授权HETEROCYCLIC COMPOUNDS AND THEIR USE AS GLYCOGEN SYNTHASE KINASE 3 INHIBITORS 有权杂环化合物和它们作为糖原合酶激酶3抑制剂
公开(公告)号：EP2091943B1
公开(公告)日：2013-11-20
申请号：EP07821595.1
申请日：2007-10-19
IPC分类号： C07D401/12 , C07D413/14 , C07D471/04 , A61K31/4709 , A61K31/497 , A61P25/00
CPC分类号： C07D401/12 , C07D241/20 , C07D413/14 , C07D471/04
摘要： The present invention relates to a heterocyclic compound of the general formula (I) and their use and preparation, methods of making the compounds, compositions containing at least one of said compounds, and methods of treatment using at least one compound. In particular, compounds of the general formula (I) are useful for inhibiting glycogen synthase kinase 3 (GSK-3),
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公开(公告)号：EP3636651A1
公开(公告)日：2020-04-15
申请号：EP19212082.2
申请日：2016-11-24
发明人： BACKFISCH, Gisela , BAKKER, Margaretha Henrica Maria , BLAICH, Günter , BRAJE, Wilfried , DRESCHER, Karla , ERHARD, Thomas , HAUPT, Andreas , HOFT, Carolin , LAKICS, Viktor , MACK, Helmut , OELLIEN, Frank , PETER, Raimund , RELO, Ana Lucia
IPC分类号： C07D498/04 , C07D498/14 , A61K31/553 , A61P25/24
摘要： The present invention relates to compound of formula (I)
wherein the variables are as defined in the claims and the description. The invention further relates to a pharmaceutical composition containing such compounds, to their use as modulators, especially agonists or partial agonists, of the 5-HT 2C receptor, to their use for preparing a medicament for the prevention or treatment of conditions and disorders which respond to the modulation of 5-HT 2C receptor, and to methods for preventing or treating conditions and disorders which respond to the modulation of 5-HT 2C receptor.-
公开(公告)号：EP3116874B1
公开(公告)日：2018-02-28
申请号：EP15711464.6
申请日：2015-03-13
发明人： BACKFISCH, Gisela , BAKKER, Margaretha Henrica Maria , BLAICH, Günter , BRAJE, Wilfried , DRESCHER, Karla , ERHARD, Thomas , HAUPT, Andreas , LAKICS, Viktor , REINGRUBER, Anna , MACK, Helmut , PETER, Raimund , RELO, Ana Lucia , SMYTH, Lynette
IPC分类号： C07D471/04 , A61K31/5513 , A61P25/00
CPC分类号： A61K31/5513 , C07D471/04 , C07D471/18
摘要： The present invention relates to tricyclic hexahydrodiazepinoquinolines carrying a substituted alkyl radical, to a method for producing them, to a pharmaceutical composition containing such compounds, to their use as modulators, especially agonists or partial agonists, of the 5-HT2C receptor, their use for preparing a medicament for the prevention or treatment of conditions and disorders which respond to the modulation of 5-HT2C receptor, to a method for preventing or treating conditions and disorders which respond to the modulation of 5-HT2C receptor, and processes for preparing such compounds and compositions.
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公开(公告)号：EP3116873B1
公开(公告)日：2018-02-28
申请号：EP15711463.8
申请日：2015-03-13
发明人： BACKFISCH, Gisela , BAKKER, Margaretha Henrica Maria , BLAICH, Günter , BRAJE, Wilfried , DRESCHER, Karla , ERHARD, Thomas , HAUPT, Andreas , KOOLMAN, Hannes , LAKICS, Viktor , REINGRUBER, Anna , MACK, Helmut , PETER, Raimund , RELO, Ana Lucia , WANG, Jincheng , ZHAO, Xiaona
IPC分类号： C07D471/04 , A61K31/5513 , A61P25/00
CPC分类号： C07D471/06 , C07D471/04
摘要： The present invention relates to compound of formula (I) as tricyclic hexahydrodiazepinoquinolines carrying a cyclic substituent, useful for modulating the 5-HT2C receptor and preventing and/or treating conditions and disorders that respond to the modulation of the 5-HT2C receptor. The present invention also relates to methods for producing compounds of formula (I), pharmaceutical compositions containing such compounds, and methods for preventing or treating conditions and disorders that respond to the modulation of the 5-HT2C receptor by administering compounds of formula (1) or pharmaceutical compositions thereof.
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公开(公告)号：EP3380483A1
公开(公告)日：2018-10-03
申请号：EP16804731.4
申请日：2016-11-24
发明人： BACKFISCH, Gisela , BAKKER, Margaretha Henrica Maria , BLAICH, Günter , BRAJE, Wilfried , DRESCHER, Karla , ERHARD, Thomas , HAUPT, Andreas , HOFT, Carolin , LAKICS, Viktor , MACK, Helmut , OELLIEN, Frank , PETER, Raimund , RELO, Ana Lucia
IPC分类号： C07D498/04 , C07D498/14 , A61K31/553 , A61P25/24
CPC分类号： C07D498/04 , A61P25/18 , A61P25/22 , A61P25/24 , C07D498/14
摘要： The present invention relates to compound of formula (I) (I) wherein the variables are as defined in the claims and the description. The invention further relates to a pharmaceutical composition containing such compounds, to their use as modulators, especially agonists or partial agonists, of the 5-HT2C receptor, to their use for preparing a medicament for the prevention or treatment of conditions and disorders which respond to the modulation of 5-HT2C receptor, and to methods for preventing or treating conditions and disorders which respond to the modulation of 5-HT2C receptor.
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8.发明公开HEXAHYDRODIAZEPINOQUINOLINES CARRYING A CYCLIC RADICAL 有权HEXAHYDRODIAZEPINOCHINOLINE MIT EINEM CYCLISCHEN RADIKAL
公开(公告)号：EP3116873A1
公开(公告)日：2017-01-18
申请号：EP15711463.8
申请日：2015-03-13
发明人： BACKFISCH, Gisela , BAKKER, Margaretha Henrica Maria , BLAICH, Günter , BRAJE, Wilfried , DRESCHER, Karla , ERHARD, Thomas , HAUPT, Andreas , KOOLMAN, Hannes , LAKICS, Viktor , REINGRUBER, Anna , MACK, Helmut , PETER, Raimund , RELO, Ana Lucia , WANG, Jincheng , ZHAO, Xiaona
IPC分类号： C07D471/04 , A61K31/5513 , A61P25/00
CPC分类号： C07D471/06 , C07D471/04
摘要： The present invention relates to compound of formula (I) as tricyclic hexahydrodiazepinoquinolines carrying a cyclic substituent, useful for modulating the 5-HT2C receptor and preventing and/or treating conditions and disorders that respond to the modulation of the 5-HT2C receptor. The present invention also relates to methods for producing compounds of formula (I), pharmaceutical compositions containing such compounds, and methods for preventing or treating conditions and disorders that respond to the modulation of the 5-HT2C receptor by administering compounds of formula (1) or pharmaceutical compositions thereof.
摘要翻译： 本发明涉及携带环状取代基的三环六氢二氮杂喹啉，其制备方法，含有这些化合物的药物组合物，其用作5-HT 2C受体的调节剂，特别是激动剂或部分激动剂，其用于制备 用于预防或治疗对5-HT 2C受体的调节作出反应的病症和障碍的药物，用于预防或治疗对5-HT 2C受体的调节作出反应的病症和障碍的方法，以及制备这些化合物的方法和 成分。
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公开(公告)号：EP3351543A1
公开(公告)日：2018-07-25
申请号：EP17206645.8
申请日：2011-12-30
发明人： TURNER, Sean Colm , MACK, Helmut , BAKKER, Margaretha Henrica Maria , VAN GAALEN, Marcel , HOFT, Carolin , HORNBERGER, Wilfried
IPC分类号： C07D401/12 , C07D401/14 , C07D405/14 , A61K31/4709 , A61P25/28 , A61P25/16
CPC分类号： C07D471/04 , A61P25/16 , A61P25/28 , C07D215/46 , C07D401/12 , C07D401/14 , C07D405/14
摘要： The present invention relates to 1-(quinolin-4-yl)-3-(6-(trifluoromethyl)-pyridin-2-y)urea and 1-(quinolin-4-yl)-3-(6-(trifluoromethyl)-pyrazine-2-yl) urea derivates of formula (I-2):
as glycogen synthase kinase 3 (GSK-3) for treating e.g. schizophrenia, Alzheimer's disease, behavioural and psychiatric symptoms of dementia, Parkinson's disease, tauopathies, vascular dementia, acute stroke and other traumatic injuries, cerebrovascular accidents, brain and spinal cord trauma, peripheral neuropathies, bipolar disorders, retinopathies, glaucoma, pain, rheumatoid arthritis and osteoarthritis. A preferred example is e.g. 1-(quinolin-4-yl)-3-(6-(trifluoromethyl)-pyridin-2-yl)urea.-
10.发明公开HEXAHYDRODIAZEPINOQUINOLINES CARRYING A SUBSTITUTED ALKYL RADICAL 有权麻黄碱HITAHYDRODIAZEPINCHINOLINE MIT EINEM SUBSTITUIERTEN ALKYLRADIKAL
公开(公告)号：EP3116874A1
公开(公告)日：2017-01-18
申请号：EP15711464.6
申请日：2015-03-13
发明人： BACKFISCH, Gisela , BAKKER, Margaretha Henrica Maria , BLAICH, Günter , BRAJE, Wilfried , DRESCHER, Karla , ERHARD, Thomas , HAUPT, Andreas , LAKICS, Viktor , REINGRUBER, Anna , MACK, Helmut , PETER, Raimund , RELO, Ana Lucia , SMYTH, Lynette
IPC分类号： C07D471/04 , A61K31/5513 , A61P25/00
CPC分类号： A61K31/5513 , C07D471/04 , C07D471/18
摘要： The present invention relates to tricyclic hexahydrodiazepinoquinolines carrying a substituted alkyl radical, to a method for producing them, to a pharmaceutical composition containing such compounds, to their use as modulators, especially agonists or partial agonists, of the 5-HT2C receptor, their use for preparing a medicament for the prevention or treatment of conditions and disorders which respond to the modulation of 5-HT2C receptor, to a method for preventing or treating conditions and disorders which respond to the modulation of 5-HT2C receptor, and processes for preparing such compounds and compositions.
摘要翻译： 本发明涉及携带取代的烷基的三环六氢二氮杂喹啉，其制备方法，含有这些化合物的药物组合物，其用作5-HT 2C受体的调节剂，特别是激动剂或部分激动剂，其用途 制备用于预防或治疗对5-HT 2C受体的调节作出反应的病症和障碍的药物，用于预防或治疗对5-HT 2C受体调节作用的病症和障碍的方法，以及制备这种化合物的方法 和组合物。
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