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1. 发明申请

WO2018175449A1 PROLINE AMIDE COMPOUNDS AND THEIR AZETIDINE ANALOGUES CARRYING A SPECIFICALLY SUBSTITUTED BENZYL RADICAL 审中-公开
公开(公告)号：WO2018175449A1
公开(公告)日：2018-09-27
申请号：PCT/US2018/023376
申请日：2018-03-20
申请人： ABBVIE DEUTSCHLAND GMBH & CO. KG , ABBVIE INC.
发明人： BACKFISCH, Gisela , BAKKER, Margaretha , BLACK, Lawrence , BRAJE, Wilfried , DRESCHER, Karla , ERHARD, Thomas , HAUPT, Andreas , HOFT, Carolin , KLING, Andreas , LAKIS, Viktor , MACK, Helmut , RELO, Ana Lucia
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
摘要： The present invention relates to proline amide compounds and their azetidine derivatives 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, 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, to a method for preventing or treating conditions and disorders which respond to the modulation of the 5-HT 2C receptor, and processes for preparing such compounds and compositions.

2. 发明申请

WO2017089458A1 HEXAHYDROPYRAZINOBENZ- OR -PYRIDO-OXAZEPINES CARRYING AN OXYGEN-CONTAINING SUBSTITUENT AND USE THEREOF IN THE TREATMENT OF 5-HT2C-DEPENDENT DISORDERS 审中-公开
标题翻译：携带含氧取代基的六氢吡嗪或哌啶氧杂吖嗪类化合物及其在治疗5-HT2C依赖性疾病中的用途
公开(公告)号：WO2017089458A1
公开(公告)日：2017-06-01
申请号：PCT/EP2016/078670
申请日：2016-11-24
申请人： ABBVIE DEUTSCHLAND GMBH & CO. KG
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 , 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-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.
摘要翻译：本发明涉及式（I）（I）的化合物，其中变量如权利要求和描述中所定义。本发明进一步涉及含有这些化合物的药物组合物，它们作为5-HT 2C受体的调节剂，特别是激动剂或部分激动剂的用途，它们用于制备用于预防或治疗对5-HT 2C受体调节作出反应的病症和障碍，以及预防或治疗对5-HT 2C /β调节作出反应的病症和障碍的方法 >受体。

3. 发明申请

WO2015136091A1 HEXAHYDRODIAZEPINOQUINOLINES CARRYING A SUBSTITUTED ALKYL RADICAL 审中-公开
标题翻译：携带取代的阿尔茨海默氏菌的十六烷基胆碱
公开(公告)号：WO2015136091A1
公开(公告)日：2015-09-17
申请号：PCT/EP2015/055336
申请日：2015-03-13
申请人： ABBVIE DEUTSCHLAND GMBH & CO. KG
发明人： BACKFISCH, Gisela , BAKKER, Margaretha Henrica Maria , BLAICH, Günter , BRAJE, Wilfried , DRESCHER, Karla , ERHARD, Thomas , HAUPT, Andreas , LAKICS, Viktor , LINSENMEIER, 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 hexahydrodiazepinoquino lines 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-HT 2C receptor, 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, to a method for preventing or treating conditions and disorders which respond to the modulation of 5-HT 2C 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系，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，涉及用于预防或治疗对5-HT 2C受体的调节作出反应的病症和障碍的方法，以及制备其中的方法化合物和组合物。

4. 发明申请

WO2014064038A1 ACYLAMINOCYCLOALKYL COMPOUNDS SUITABLE FOR TREATING DISORDERS THAT RESPOND TO MODULATION OF DOPAMINE D3 RECEPTOR 审中-公开
标题翻译：适用于治疗多巴胺D3受体调节障碍的ACYLAMINOCOCLOALKYL化合物
公开(公告)号：WO2014064038A1
公开(公告)日：2014-05-01
申请号：PCT/EP2013/071947
申请日：2013-10-21
申请人： ABBVIE DEUTSCHLAND GMBH & CO. KG
发明人： HAUPT, Andreas
IPC分类号： C07D405/14 , C07D403/04 , C07D405/04 , C07D239/42 , A61K31/506 , A61P25/00
CPC分类号： C07D239/26 , C07D239/42 , C07D403/04 , C07D405/04 , C07D405/14
摘要： The present invention relates to novel acylaminocycloalkyl compounds, in particular to the compounds of the formula (I) as described herein and to their salts and N-oxides. The compounds possess valuable therapeutic properties and are suitable, in particular, for treating diseases that respond to modulation of the dopamine D3 receptor. In formula (I), the variables have the following meanings: m is 1 or 2, n is 1 or 2, A is selected from the group consisting of CH 2 , CH 2 CH 2 , CHFCH 2 and CF 2 CH 2 , R 1 is hydrogen or C 1 -C 3 -alkyl, R 2 is selected from the group consisting of hydrogen, and fluorine, R 3a is selected from the group consisting of hydrogen and methyl, R 3b is selected from the group consisting of hydrogen and methyl, R 4 is branched C 4 -C 6 alkyl or branched fluorinated C 4 -C 6 alkyl, and R 5 is an oxygen containing radical such as C 1 -C 2 -alkoxy-C 1 -C 4 -alkyl, fluorinated C 1 -C 2 -alkoxy-C 1 -C 4 -alkyl, hydroxy-C 1 -C 4 -alkyl, fluorinated hydroxy-C 1 -C 4 -alkyl, oxetanyl, fluorinated oxetanyl, oxolanyl, fluorinated oxolanyl, C 3 -C 5 cycloalkyl, fluorinated C 3 -C 5 cycloalkyl, C 3 -C 5 cycloalkoxy-C 1 -C 4 -alkyl and fluorinated C 3 -C 5 cycloalkoxy-C 1 -C 4 -alkyl.
摘要翻译：本发明涉及新的酰氨基环烷基化合物，特别涉及本文所述的式（I）化合物及其盐和N-氧化物。该化合物具有有价值的治疗性质，特别适用于治疗对多巴胺D3受体调节作出反应的疾病。在式（I）中，变量具有以下含义：m为1或2，n为1或2，A选自CH 2，CH 2 CH 2，CHFCH 2和CF 2 CH 2，R 1为氢或C 1 -C 3 - 烷基 R2选自氢和氟，R3a选自氢和甲基，R3b选自氢和甲基，R4是支链C4-C6烷基或支链氟化C4-烷基， C6烷基，R5是含氧基团，例如C1-C2-烷氧基-C1-C4-烷基，氟化C1-C2-烷氧基-C1-C4-烷基，羟基-C1-C4-烷基，氟化羟基C1- 氟化C 3 -C 5环烷基，C 3 -C 5环烷氧基-C 1 -C 4 - 烷基和氟化C 3 -C 5环烷氧基-C 1 -C 4烷基。

5. 发明申请

WO2014041131A1 TRICYCLIC QUINOLINE AND QUINOXALINE DERIVATIVES 审中-公开
标题翻译：三元喹啉和喹啉衍生物
公开(公告)号：WO2014041131A1
公开(公告)日：2014-03-20
申请号：PCT/EP2013/069036
申请日：2013-09-13
申请人： ABBVIE DEUTSCHLAND GMBH & CO. KG , ABBVIE INC.
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-HT 2C receptor, 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 a method for preventing or treating conditions and disorders which respond to the modulation of 5-HT 2C 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，其用于制备用于预防或治疗响应于5-HT 2C受体的调节的病症和病症，以及用于预防或治疗对5-HT 2C受体的调节作出反应的病症和障碍的方法。

6. 发明申请

WO2017157929A1 QUINOLINE COMPOUNDS SUITABLE FOR TREATING DISORDERS THAT RESPOND TO THE MODULATION OF THE SEROTONIN 5-HT6 RECEPTOR 审中-公开
标题翻译：喹啉化合物适用于治疗反应调节血清素5-HT6受体的疾病
公开(公告)号：WO2017157929A1
公开(公告)日：2017-09-21
申请号：PCT/EP2017/055975
申请日：2017-03-14
申请人： ABBVIE DEUTSCHLAND GMBH & CO. KG
发明人： GENESTE, Hervé , HAUPT, Andreas , POHLKI, Frauke , RELO, Ana Lucia , UNGER, Liliane , WICKE, Karsten
IPC分类号： C07D401/14 , C07D401/04 , C07D401/12 , A61K31/4709 , A61P25/30 , A61P25/18 , A61P25/28
摘要： The present invention relates to quinoline compounds of formula (I) wherein the variables are defined as in the claims and the description. The invention further relates to a pharmaceutical composition containing such compounds, to their use as modulators of the 5-HT 6 receptor, their use for preparing a medicament for the prevention or treatment of conditions and disorders which respond to the modulation of the 5-HT 6 receptor, and to methods for preventing or treating conditions and disorders which respond to the modulation of the 5-HT 6 receptor.
摘要翻译：本发明涉及式（I）的喹啉化合物，其中变量如权利要求和描述中所定义。本发明进一步涉及含有这些化合物的药物组合物，它们作为5-HT 6受体的调节剂的用途，它们在制备用于预防或治疗病症和病症的药物中的用途，所述病症和病症对 5-HT 6受体的调节，以及预防或治疗对5-HT 6受体的调节作出反应的病症和病症的方法。

7. 发明申请

WO2017050807A1 PYRIDYL OR PYRAZINYL COMPOUNDS CARRYING A METHYL-BOUND ALPHA-AMINO ACID AMIDE GROUP 审中-公开
标题翻译：携带甲基邻苯二甲酸酰胺基的吡啶基或吡嗪基化合物
公开(公告)号：WO2017050807A1
公开(公告)日：2017-03-30
申请号：PCT/EP2016/072387
申请日：2016-09-21
申请人： ABBVIE DEUTSCHLAND GMBH & CO. KG
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-HT 2C 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-HT 2C receptor.
摘要翻译：本发明涉及带有衍生自式I的α-氨基酸的甲基结合的N-酰胺部分的吡啶基或吡嗪基化合物，其中变量如权利要求和说明书所定义。本发明还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，以及其用于制备用于预防或治疗响应的病症和障碍的药物对5-HT 2C受体的调节。

8. 发明申请

WO2015136090A1 HEXAHYDRODIAZEPINOQUINOLINES CARRYING A CYCLIC RADICAL 审中-公开
标题翻译：携带循环放射性的十六烷基二氢喹啉
公开(公告)号：WO2015136090A1
公开(公告)日：2015-09-17
申请号：PCT/EP2015/055335
申请日：2015-03-13
申请人： ABBVIE DEUTSCHLAND GMBH & CO. KG
发明人： BACKFISCH, Gisela , BAKKER, Margaretha Henrica Maria , BLAICH, Günter , BRAJE, Wilfried , DRESCHER, Karla , ERHARD, Thomas , HAUPT, Andreas , KOOLMAN, Hannes , LAKICS, Viktor , LINSENMEIER, Anna , MACK, Helmut , PETER, Raimund , RELO, Ana Lucia
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 tricyclic hexahydrodiazepinoquino lines carrying a cyclic substituent, 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-HT 2C receptor, 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, to a method for preventing or treating conditions and disorders which respond to the modulation of 5-HT 2C receptor, and processes for preparing such compounds and compositions.
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诺酮系，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，以及制备这种化合物的方法和组合物。

9. 发明申请

WO2014140246A1 ACYLAMINOCYCLOALKYL COMPOUNDS SUITABLE FOR TREATING DISORDERS THAT RESPOND TO MODULATION OF DOPAMINE D3 RECEPTOR 审中-公开
标题翻译：适用于治疗多巴胺D3受体调节障碍的ACYLAMINOCOCLOALKYL化合物
公开(公告)号：WO2014140246A1
公开(公告)日：2014-09-18
申请号：PCT/EP2014/055062
申请日：2014-03-14
申请人： ABBVIE DEUTSCHLAND GMBH & CO. KG , ABBVIE INC.
发明人： HAUPT, Andreas , DINGES, Jürgen , UNGER, Liliane , WICKE, Karsten , VAN WATERSCHOOT, Robert , DRESCHER, Karla , RELO, Ana Lucia
IPC分类号： C07D239/42 , A61K31/506 , A61P25/00
CPC分类号： C07D295/155 , A61K31/496 , C07D239/42 , C07D403/04
摘要： The present invention relates to novel acylaminocycloalkyl compounds, in particular to the compounds of the formula I as described herein and to their salts and N-oxides. The compounds possess valuable therapeutic properties and are suitable, in particular, for treating diseases that respond to modulation of the dopamine D3 receptor. In formula I, the variables have the following meanings: m is 1 or 2, n is 1 or 2, A is selected from the group consisting of CH 2 , CH 2 CH 2 , CHFCH 2 and CF 2 CH 2 , R 1 is an oxygen containing cyclic radical selected such as C 3 -C 6 cycloalkyl, which carries one or two oxygen containing radicals selected from the group consisting of OH, C 1 -C 2 -alkoxy, fluorinated C 1 -C 2 -alkoxy, and a carbonyl oxygen,, R 2 is selected from the group consisting of hydrogen, OH and fluorine, R 3a is selected from the group consisting of hydrogen and methyl, R 3b is selected from the group consisting of hydrogen and methyl, R 4 is branched C 4 -C 6 alkyl or branched fluorinated C 4 -C 6 alkyl, and R 5 is inter alia C 1 -C 6 alkyl, fluorinated C 1 -C 3 alkyl, C 1 -C 2 -alkoxy-C 1 -C 4 -alkyl, fluorinated C 1 -C 2 -alkoxy-C 1 -C 4 -alkyl, hydroxy-C 1 -C 4 -alkyl, fluorinated hydroxy-C 1 -C 4 -alkyl, oxetanyl, fluorinated oxetanyl, oxolanyl, fluorinated oxolanyl, C 3 -C 5 cycloalkyl, fluorinated C 3 -C 5 cycloalkyl, etc.
摘要翻译：本发明涉及新的酰氨基环烷基化合物，特别是涉及本文所述的式I化合物及其盐和N-氧化物。该化合物具有有价值的治疗性质，特别适用于治疗对多巴胺D3受体调节作出反应的疾病。在式I中，变量具有以下含义：m为1或2，n为1或2，A选自CH 2，CH 2 CH 2，CHFCH 2和CF 2 CH 2，R 1为选自氧的环状基团，例如C 3 -C 6环烷基，其携带一个或两个选自OH，C 1 -C 2烷氧基，氟化C 1 -C 2烷氧基和羰基氧的含氧基团，R 2选自氢，OH 和氟，R3a选自氢和甲基，R3b选自氢和甲基，R4是支链C4-C6烷基或支链氟化C4-C6烷基，R5特别是C1-C6 烷基，氟化C 1 -C 3烷基，C 1 -C 2烷氧基-C 1 -C 4烷基，氟化C 1 -C 2烷氧基-C 1 -C 4 - 烷基，羟基-C 1 -C 4 - 烷基，氟化羟基-C 1 -C 4烷基，氧杂环丁烷基，氟化氧杂环丁烷基，氧杂环戊烷基，氟代氧杂环戊烷基，C3-C5环烷基，氟化C3-C5环烷基等

10. 发明公开

EP3116874A1 HEXAHYDRODIAZEPINOQUINOLINES CARRYING A SUBSTITUTED ALKYL RADICAL 有权
标题翻译：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
申请人： AbbVie Deutschland GmbH & Co. KG
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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