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1. 发明申请

WO2014140186A1 OXINDOLE DERIVATIVES CARRYING AN OXETANE SUBSTITUENT AND USE THEREOF FOR TREATING VASOPRESSINE-RELATED DISEASES 审中-公开
标题翻译：携带OXETANE取代物的OXINDOLE衍生物及其用于治疗类风湿性关节炎的用途
公开(公告)号：WO2014140186A1
公开(公告)日：2014-09-18
申请号：PCT/EP2014/054973
申请日：2014-03-13
申请人： ABBVIE DEUTSCHLAND GMBH & CO. KG
发明人： JANTOS, Katja , BRAJE, Wilfried , GENESTE, Hervé , KLING, Andreas , UNGER, Liliane , BEHL, Berthold , VAN GAALEN, Marcel , HORNBERGER, Wilfried , LAPLANCHE, Loic , WEBER, Silke
IPC分类号： C07D405/14 , A61K31/4545 , A61P3/00 , A61P9/00 , A61P25/00 , A61P7/00
CPC分类号： C07D405/14 , C07D487/08
摘要： The present invention relates to novel substituted oxindole derivatives, pharmaceutical compositions comprising them, and their use for the treatment of vasopressin-related disorders.
摘要翻译：本发明涉及新型取代的羟基吲哚衍生物，包含它们的药物组合物及其用于治疗加压素相关病症的用途。

2. 发明申请

WO2014079995A2 NOVEL INHIBITOR COMPOUNDS OF PHOSPHODIESTERASE TYPE 10A 审中-公开
标题翻译：新型的磷酸二酯酶抑制剂化合物10A
公开(公告)号：WO2014079995A2
公开(公告)日：2014-05-30
申请号：PCT/EP2013/074532
申请日：2013-11-25
申请人： ABBVIE INC. , ABBVIE DEUTSCHLAND GMBH & CO. KG
发明人： GENESTE, Hervé , TURNER, Sean , OCHSE, Michael , DRESCHER, Karla , BLACK, Lawrence A. , JANTOS, Katja
IPC分类号： C07D401/14 , A61K31/4353 , A61K31/4427 , C07D401/04 , C07D401/10 , C07D471/04 , C07D487/04
CPC分类号： C07D401/14 , C07D401/04 , C07D401/10 , C07D471/04 , C07D487/04
摘要： The present invention relates to compounds of the formula I and their salts etc. which are inhibitors of phosphodiesterase type 10A and to their use for the manufacture of a medicament and which thus are suitable for treating or controlling of medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders wherein Y 1 and Y 2 are adjacent atoms in Het 1 , which are independently selected from the group consisting of carbon and nitrogen; k is 0, 1, 2 or 3; Het 1 is a bivalent monocyclic 5- or 6-membered heteroaromatic radical, having 1, 2 or 3 heteroatoms or heteroatom moieties selected from O, S, N and N-R a as ring members, or a bivalent fused bicyclic 8-, 9- or 10-membered heteroaromatic radical, having 1, 2, 3 or 4 heteroatoms or heteroatom moieties selected from O, S, N and N-R a as ring members; Het 2 is inter alia monocyclic 5- or 6-membered hetaryl, having 1, 2 or 3 heteroatoms or heteroatom moieties selected from O, S, N and N-R 1a as ring members, Cyc is inter alia optionally substituted monocyclic 5- or 6-membered hetaryl or optionally substituted fused 8-, 9- or 10-membered bicyclic hetaryl; Ar is optionally substituted phenylene or optionally substituted bivalent 6-membered hetaryl; R is attached to a carbon atom of Het 1 and inter alia - halogen, C 1 -C 6 -alkyl, C 2 -C 6 -alkenyl, C 2 -C 6 -alkynyl, C 1 -C 6 -alkoxy, C 1 -C 6 -fluoroalkyl, C 1 -C 6 -fluoroalkoxy, C 3 -C 6 -cycloalkyl etc.
摘要翻译：本发明涉及作为磷酸二酯酶10A型抑制剂的式I化合物及其盐等，并涉及它们在制备药物中的应用，因此适用于治疗或控制选自神经障碍和精神障碍的医学病症，用于改善与这种病症相关的症状，以及用于降低这种病症的风险，其中Y 1和Y 2是相邻的原子 Het 1，它们独立地选自由碳和氮组成的组; k是0,1,2或3; Het 1是具有1,2或3个选自O，S，N和NR a的杂原子或杂原子部分的二价单环5-或6-元杂芳族基团，其为环成员或具有1,2,3或4个选自O，S，N和NR a的杂原子或杂原子部分的二价稠合双环8,9或10元杂芳族基团作为戒指成员; Het 2尤其是单环5-或6-元杂芳基，其具有1,2或3个选自O，S，N和NR 1a的杂原子或杂原子部分作为环 Cyc特别是任选取代的单环5-或6-元杂芳基或任选取代的稠合的8-，9-或10-元双环杂芳基; Ar是任选取代的亚苯基或任选取代的二价6-元杂芳基; R连接到Het 1 1的碳原子上，尤其是 - 卤素，C 1 -C 6 - 烷基，C≡2 C 6 -C 6 - 烯基，C 2 -C 6 - 炔基，C 1 -C 6 - C 1-6 - 烷氧基，C 1 -C 6 - 氟代烷基，C 1 -C 6 - 烷氧基，C 1 -C 6 - C 1-3 - 烷氧基，C 3-6 - 环烷基等。

3. 发明申请

WO2015091931A1 OXINDOLE DERIVATIVES CARRYING A PIPERIDYL-SUBSTITUTED AZETIDINYL SUBSTITUENT AND USE THEREOF FOR TREATING VASOPRESSINE-RELATED DISEASES 审中-公开
标题翻译：携带哌啶取代的亚胺基取代基的氧化衍生物及其用于治疗类风湿关节疾病的用途
公开(公告)号：WO2015091931A1
公开(公告)日：2015-06-25
申请号：PCT/EP2014/078699
申请日：2014-12-19
申请人： ABBVIE DEUTSCHLAND GMBH & CO. KG , ABBVIE INC.
发明人： GENESTE, Hervé , HORNBERGER, Wilfried , HUTCHINS, Charles W. , JANTOS, Katja , KLING, Andreas , LAPLANCHE, Loic , VAN GAALEN, Marcel
IPC分类号： C07D401/14 , C07D401/04 , A61K31/444 , A61P25/24 , A61P3/10
CPC分类号： C07D401/14 , C07B59/002 , C07B2200/05 , C07D401/04 , C07D405/14 , C07D491/107
摘要： The present invention relates to novel substituted oxindole derivatives of formula (I) wherein the variables are as defined in the claims and description; to pharmaceutical compositions comprising them, and to their use for treatment of vasopressin-related disorders.
摘要翻译：本发明涉及式（I）的新型取代的羟基吲哚衍生物，其中变量如权利要求和说明书所定义; 包含它们的药物组合物及其用于治疗加压素相关病症的用途。

4. 发明申请

WO2014140086A1 NOVEL INHIBITOR COMPOUNDS OF PHOSPHODIESTERASE TYPE 10A 审中-公开
标题翻译：磷酸二酯酶类型10A的新型抑制剂化合物
公开(公告)号：WO2014140086A1
公开(公告)日：2014-09-18
申请号：PCT/EP2014/054810
申请日：2014-03-12
申请人： ABBVIE DEUTSCHLAND GMBH & CO. KG , ABBVIE INC.
发明人： JANTOS, Katja , OCHSE, Michael , GENESTE, Hervé , FROGGETT, Jayne , JAKOB, Clarissa , DRESCHER, Karla , DINGES, Jürgen
IPC分类号： C07D495/04 , A61K31/5025 , A61P25/00
CPC分类号： C07D495/04
摘要： The present invention relates to compounds of the formula I, the N-oxides, tautomers, the prodrugs and the pharmaceutically acceptable salts thereof: (I). In formula I the variables X 1 is CH or N, X 2 is O or S and where R 1 , R 2 , R 3 , R 4 and Q are as defined in the claims. The compounds of the formula I, the N-oxides, tautomers, the prodrugs and the pharmaceutically acceptable salts thereof are inhibitors of phosphodiesterase type 10A. Thus, the invention also relates to the use of the compounds of the formula I, the N-oxides, tautomers, the prodrugs and the pharmaceutically acceptable salts thereof for the manufacture of a medicament and which thus are suitable for treating or controlling of medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders.
摘要翻译：本发明涉及式I化合物，其N-氧化物，互变异构体，其前药及其药学上可接受的盐：（I）。在式I中，变量X1是CH或N，X2是O或S，其中R1，R2，R3，R4和Q如权利要求中所定义。式I化合物，N-氧化物，互变异构体，其前药和药学上可接受的盐是10A型磷酸二酯酶的抑制剂。因此，本发明还涉及式I化合物，N-氧化物，互变异构体，前药和其药学上可接受的盐在制备药物中的用途，因此其适用于治疗或控制医学病症选自神经障碍和精神障碍，用于改善与这种障碍相关的症状并降低这种障碍的风险。

5. 发明申请

WO2016034703A1 FUSED HETEROCYCLIC OR CARBOCYCLIC COMPOUNDS CARRYING A SUBSTITUTED CYCLOALIPHATIC RADICAL AND USE THEREOF FOR TREATING VASOPRESSIN-RELATED DISEASES 审中-公开
标题翻译：携带取代的循环系统的融合的杂环化合物或碳环化合物及其用于治疗与血管相关性疾病
公开(公告)号：WO2016034703A1
公开(公告)日：2016-03-10
申请号：PCT/EP2015/070223
申请日：2015-09-04
申请人： ABBVIE DEUTSCHLAND GMBH & CO. KG
发明人： BRAJE, Wilfried , FROGGETT, Jayne , GENESTE, Hervé , HORNBERGER, Wilfried , JANTOS, Katja , KLING, Andreas , VAN GAALEN, Marcel
IPC分类号： C07D239/91
CPC分类号： C07D239/91 , C07D401/12 , C07D403/12 , C07D455/02 , C07D491/107
摘要： The present invention relates to novel fused heterocyclic or carbocyclic compounds of formula (I) wherein the variables are as defined in the claims and the description. The invention further relates to pharmaceutical compositions comprising these compounds, and to their use for the treatment of vasopressin-related disorders.
摘要翻译：本发明涉及式（I）的新型稠合杂环或碳环化合物，其中变量如权利要求和说明书所定义。本发明还涉及包含这些化合物的药物组合物及其用于治疗加压素相关病症的用途。

6. 发明申请

WO2015091934A1 OXINDOLE DERIVATIVES CARRYING AN AMINE-SUBSTITUTED PIPERIDYL-AZETIDINYL SUBSTITUENT AND USE THEREOF FOR TREATING VASOPRESSINE-RELATED DISEASES 审中-公开
标题翻译：实施胺取代的哌嗪 - 亚胺基替代物的氧化衍生物及其用于治疗与维生素A相关的疾病的用途
公开(公告)号：WO2015091934A1
公开(公告)日：2015-06-25
申请号：PCT/EP2014/078702
申请日：2014-12-19
申请人： ABBVIE DEUTSCHLAND GMBH & CO. KG , ABBVIE INC.
发明人： GENESTE, Hervé , HORNBERGER, Wilfried , HUTCHINS, Charles, W. , JANTOS, Katja , KLING, Andreas , LAPLANCHE, Loic , VAN GAALEN, Marcel
IPC分类号： C07D401/14 , A61K31/4545 , A61P9/00
CPC分类号： C07D401/14
摘要： The present invention relates to novel substituted oxindole derivatives of formula (I) wherein the variables are as defined in the claims and description; to pharmaceutical compositions comprising them, and to their use for the treatment of vasopressin-related disorders.
摘要翻译：本发明涉及式（I）的新型取代的羟基吲哚衍生物，其中变量如权利要求和说明书所定义; 包含它们的药物组合物及其用于治疗加压素相关病症的用途。

7. 发明申请

WO2014140184A1 NOVEL INHIBITOR COMPOUNDS OF PHOSPHODIESTERASE TYPE 10A 审中-公开
标题翻译：磷酸二酯酶类型10A的新型抑制剂化合物
公开(公告)号：WO2014140184A1
公开(公告)日：2014-09-18
申请号：PCT/EP2014/054971
申请日：2014-03-13
申请人： ABBVIE DEUTSCHLAND GMBH & CO. KG , ABBVIE INC.
发明人： GENESTE, Hervé , OCHSE, Michael , DRESCHER, Karla , BEHL, Berthold , LAPLANCHE, Loic , DINGES, Jürgen , JAKOB, Clarissa
IPC分类号： C07D471/04 , C07D519/00 , A61P25/00 , A61K31/437 , A61K31/4709 , A61K31/5377 , A61K31/541 , A61K31/444 , A61K31/506
CPC分类号： C07D471/04 , C07D519/00
摘要： The present invention relates to compounds of the formula (I), the N-oxides, tautomers, the prodrugs and the pharmaceutically acceptable salts thereof. In formula I the variables Het, A, X, Y, Z, R 1 , R 2 , R 3 , R 4 , R 5 and Q are as defined in the claims. The compounds of the formula I, the N-oxides, tautomers, the prodrugs and the pharmaceutically acceptable salts thereof are inhibitors of phosphodiesterase type 10A. Thus, the invention also relates to the use of the compounds of the formula I, the N-oxides, tautomers, the prodrugs and the pharmaceutically acceptable salts thereof for the manufacture of a medicament and which thus are suitable for treating or controlling of medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders.
摘要翻译：本发明涉及式（I）化合物，N-氧化物，互变异构体，其前药及其药学上可接受的盐。在式I中，变量Het，A，X，Y，Z，R1，R2，R3，R4，R5和Q如权利要求中所定义。式I化合物，N-氧化物，互变异构体，其前药和药学上可接受的盐是10A型磷酸二酯酶的抑制剂。因此，本发明还涉及式I化合物，N-氧化物，互变异构体，前药和其药学上可接受的盐在制备药物中的用途，因此其适用于治疗或控制医学病症选自神经障碍和精神障碍，用于改善与这种障碍相关的症状并降低这种障碍的风险。

8. 发明申请

WO2019016112A1 1,2,3,4-SUBSTITUTED QUINOLINE COMPOUNDS AS S1P MODULATORS 审中-公开
公开(公告)号：WO2019016112A1
公开(公告)日：2019-01-24
申请号：PCT/EP2018/069196
申请日：2018-07-16
申请人： ABBVIE DEUTSCHLAND GMBH & CO. KG
发明人： AMBERG, Wilhelm , GENESTE, Hervé , HORNBERGER, Wilfried , LANGE, Udo , MEZLER, Mario , OCHSE, Michael , OELLIEN, Frank , TURNER, Sean C , VAN BERGEIJK, Jeroen , VAN DER KAM, Elizabeth
IPC分类号： C07D217/04 , C07D401/06 , C07D405/06 , C07D409/06 , A61P25/28 , A61K31/4725
摘要： The invention relates to 1,2,3,4-substituted quinoline compounds as S1P modulators, pharmaceutical compositions comprising such compounds, and uses thereof in the treatment, alleviation or prevention of diseases or disorders mediated by an S1P receptor.

9. 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。

10. 发明申请

WO2015173393A1 OXINDOLE COMPOUNDS CARRYING A NITROGEN-BOUND SPIRO SUBSTITUENT AND USE THEREOF FOR TREATING VASOPRESSIN-RELATED DISEASES 审中-公开
标题翻译：携带氮离子螺旋体替代物的氧化合物及其用于治疗相关疾病的用途
公开(公告)号：WO2015173393A1
公开(公告)日：2015-11-19
申请号：PCT/EP2015/060763
申请日：2015-05-15
申请人： ABBVIE DEUTSCHLAND GMBH & CO. KG
发明人： GENESTE, Hervé , HORNBERGER, Wilfried , JANTOS, Katja , KLING, Andreas , VAN GAALEN, Marcel
IPC分类号： C07D471/10 , C07D487/10 , C07D295/135 , C07D305/08
CPC分类号： C07D471/10 , C07D295/135 , C07D305/08 , C07D487/10
摘要： The present invention relates to novel substituted oxindole derivatives of the formula I wherein A is a ring selected from phenyl and 6-membered hetaryl containing 1 or 2 nitrogen atoms as ring members, where ring A carries one substituent R 6 and optionally one substituent R 7 ;B is a ring selected from phenyland a monocyclic or bicyclic het- eroaromatic ring containing 1, 2 or 3 heteroatoms selected from O, N and S as ring members, where ring B may carry 1, 2 or 3 substituents R 8 ;X 1 , X 2 , X 3 and X 4 , independently of each other, are selected from -CH 2 -, -O-, -S(O) c -, -NH-, -C(O)-, -CH 2 CH 2 -,-CH 2 O-, -OCH 2 -, -S(O) c CH 2 -, -CH 2 S(O)c-, CH 2 NH-,-NHCH 2 -, -CH 2 C(O)-andC(O)CH 2 -;X 5 is NH,CH 2 or O,;and wherein c, R 1 , R 2 , (R 3 )a, (R 4 )b, R 5 , R 6 , R 7 , and R 8 are as defined in the claims. The present invention also relates to pharmaceutical compositions comprising the novel substituted oxindole derivatives of the formula I, and to their use for the treatment of vasopressin-related disorders.
摘要翻译：本发明涉及式I的新的取代的羟基吲哚衍生物，其中A是选自苯基和含有1或2个氮原子作为环成员的6元杂芳基的环，其中环A携带一个取代基R6和任选的一个取代基R7; B 是选自苯基和含有1,2或3个选自O，N和S作为环成员的杂原子的单环或双环环芳族环的环，其中环B可以带有1,2或3个取代基R8; X1，X2，X3 和X 4彼此独立地选自-CH 2 - ， - O - ， - S（O）c - ， - NH - ， - C（O） - ， - CH 2 CH 2 - ， - CH 2 O-，-OCH 2 - -S（O）cCH 2 - ， - CH 2 S（O）c - ，CH 2 NH-， - NHCH 2 - ， - CH 2 C（O） - 和C（O）CH 2 - ; X 5是NH，CH 2或O，并且其中c， R2，（R3）a，（R4）b，R5，R6，R7和R8如权利要求中所定义。本发明还涉及包含式I的新型取代的羟吲哚衍生物的药物组合物及其用于治疗加压素相关病症的用途。

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