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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.-
12.发明公开
公开(公告)号：EP3601255A1
公开(公告)日：2020-02-05
申请号：EP18716451.2
申请日：2018-03-20
发明人： BACKFISCH, Gisela , BAKKER, Margaretha , BLACK, Lawrence , BRAJE, Wilfried , DRESCHER, Karla , ERHARD, Thomas , HAUPT, Andreas , HOFT, Carolin , KLING, Andreas , LAKICS, Viktor , MACK, Helmut , RELO, Ana Lucia , OELLIEN, Frank
IPC分类号： C07D401/12 , C07D405/12 , C07D207/16 , A61P25/24 , A61P25/14 , A61P9/00 , A61P25/22 , A61P25/28 , A61P25/18 , A61P25/30 , A61P3/10 , A61K31/40
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公开(公告)号：EP3353155A1
公开(公告)日：2018-08-01
申请号：EP16770000.4
申请日：2016-09-21
发明人： BACKFISCH, Gisela , BAKKER, Margaretha , BLAICH, Günter , BRAJE, Wilfried , DRESCHER, Karla , ERHARD, Thomas , HAUPT, Andreas , HOFT, Carolin , KLING, Andreas , LAKICS, Viktor , MACK, Helmut , OELLIEN, Frank , PETER, Raimund , POHLKI, Frauke , RELO, Ana Lucia
IPC分类号： C07D241/20 , C07D213/56 , A61K31/4439 , A61K31/497 , A61P25/00
CPC分类号： C07D213/56 , C07D241/20
摘要： The present invention relates to pyridyl or pyrazinyl compounds carrying a methyl- bound N-amide moiety derived from an α-amino acid of formula I where 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, and to their use for preparing a medicament for the prevention or treatment of conditions and disorders which respond to the modulation of the 5-HT2C receptor.
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14.发明授权CARBOXAMIDE COMPOUNDS AND THEIR USE AS CALPAIN INHIBITORS 有权CARBOXAMIDVERBINDUNGEN UND IHRE VERWENDUNG ALS CALPAIN-HEMMER
公开(公告)号：EP2427429B1
公开(公告)日：2017-02-15
申请号：EP10715905.5
申请日：2010-05-06
发明人： MACK, Helmut , KLING, Andreas , JANTOS, Katja , MOELLER, Achim , HORNBERGER, Wilfried , HUTCHINS, Charles, W.
IPC分类号： C07D233/32 , C07D401/06 , C07D405/12 , C07D409/12 , C07D417/12 , C07D207/22 , C07D275/03 , C07D211/78 , C07D213/81 , C07D401/12 , C07D207/28 , C07D207/26 , C07D211/76 , C07D233/34 , C07D239/10
CPC分类号： C07D207/22 , C07D207/26 , C07D207/28 , C07D211/76 , C07D211/78 , C07D213/81 , C07D233/32 , C07D233/34 , C07D239/10 , C07D275/03 , C07D401/06 , C07D401/12 , C07D405/12 , C07D409/12 , C07D417/12
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15.发明授权
公开(公告)号：EP2193119B1
公开(公告)日：2014-01-01
申请号：EP08787483.0
申请日：2008-08-26
发明人： MACK, Helmut , TEUSCH, Nicole , MÜLLER, Bernhard K. , HORNBERGER, Wilfried , JARVIS, Michael F. , SAUER, Daryl , SWANN, Steve Jr , HOBSON, Adrian Donald , KEDDY, Ryan , BONAFOUX, Dominique , VASUDEVAN, Anil
IPC分类号： C07D213/56 , C07D401/12 , C07D405/12 , C07D413/12 , C07D417/12 , A61K31/44 , A61K31/4427 , A61P9/00 , A61P25/00 , A61P35/00 , A61P29/00
CPC分类号： C07D401/12 , C07D213/56 , C07D405/12 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/12
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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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17.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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18.发明公开HETEROCYCLIC COMPOUNDS AND THEIR USE AS GLYCOGEN SYNTHASE KINASE-3 INHIBITORS 有权1-（吡啶-2-基）-3-（喹啉-4-基）脲衍生物和相关化合物作为糖原合酶激酶3（GSK-3）抑制剂用于治疗神经变性疾病的治疗
公开(公告)号：EP2658854A2
公开(公告)日：2013-11-06
申请号：EP11811357.0
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 novel heterocyclic compounds of formula I wherein the variables are as defined in the claims or the description, which are useful for inhibiting glycogen synthase kinase 3 (GSK-3), compositions containing the compounds, their use for preparing a medicament for the treatment of a medical disorder susceptible to the treatment with a compound that modulates, preferably inhibits, the activity of glycogen synthase kinase 3&bgr;, and methods of treatment of medical disorders susceptible to treatment with a compound that modulates glycogen synthase kinase 3&bgr; activity using the compounds.
摘要翻译： 本发明涉及新的式杂环化合物我worin各变量如在权利要求或说明书中，哪些是有用的定义为抑制糖原合酶激酶3（GSK-3）的组合物含有所述化合物，它们用于制备药物的用途 用于治疗医学病症的易感的治疗用化合物并调制，优选抑制糖原合成酶激酶3的β的活性;和治疗医学病症的治疗敏感的化合物的方法做了调节糖原合成酶激酶3？ 使用该化合物的活性。
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公开(公告)号：EP2648731A1
公开(公告)日：2013-10-16
申请号：EP11796664.8
申请日：2011-12-08
发明人： KLING, Andreas , JANTOS, Katja , MACK, Helmut , MÖLLER, Achim , HORNBERGER, Wilfried , LAO, Yanbin , BACKFISCH, Gisela , NIJSEN, Marjoleen
IPC分类号： A61K31/4439 , C07D401/04 , A61P25/28
CPC分类号： C07D401/04 , A61K31/4439 , C07D401/14 , Y02A50/411
摘要： The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity. The carboxamide compounds are compounds of the general formula (I) in which R1, R2, R3, R4, X, m and n have the meanings mentioned in the claims and the description, the tautomers thereof, the hydrates thereof and the pharmaceutically suitable salts thereof. Of these compounds those are preferred wherein R1 is optionally substituted benzyl or hetaryl-methyl, X is a single bond or an oxygen atom, R2 is C1-C4-alkyl, C1-C4-haloalkyl, C2-C4-alkenyl, C3-C6-cycloalkyl, C3-C6-cycloalkyl-C1-C2-alkyl, C3-C6-heterocycloalkyl-C1-C2-alkyl, phenyl, phenyl-C1-C3-alkyl, pyridin-2-yl-C1-C3-alkyl or CH2—C(O)OCH3, R3 and R4 independently of one another are halogen, CN, CF3, CHF2, CH2F, C1-C2-alkyl or C1-C2-alkoxy, and m and n independently of one another are 0 or 1.
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