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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

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

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。

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

WO2014027078A1 INHIBITOR COMPOUNDS OF PHOSPHODIESTERASE TYPE 10A 审中-公开
标题翻译：磷酸二酯酶类型10A的抑制剂化合物
公开(公告)号：WO2014027078A1
公开(公告)日：2014-02-20
申请号：PCT/EP2013/067122
申请日：2013-08-16
申请人： ABBVIE DEUTSCHLAND GMBH & CO. KG , ABBVIE INC.
发明人： GENESTE, Hervé , OCHSE, Michael , DRESCHER, Karla , JAKOB, Clarissa
IPC分类号： C07D471/04 , A61K31/4745 , A61P35/00
CPC分类号： C07D471/14 , C07D471/04 , C07D487/04
摘要： The present invention relates to compounds of the formula I, the N-oxides, tautomers, the prodrugs and the pharmaceutically acceptable salts thereof, where in formula I the variables R 1 , R 2 , R 3 , R 4 and R 5 are as defined in the claims and where X is C-R 6 or N,Y is C-R 7 or N, where R 6 and R 7 are, inter alia, hydrogen, halogen, alkoxy, haloalkoxy and the like. The compounds of the formula I, the N-oxides, tautomers,the prodrugs and the pharmaceutically acceptable salts thereof 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.
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，其中在式I中，变量R1，R2，R3，R4和R5如权利要求中所定义，其中 X是C-R6或N，Y是C-R7或N，其中R6和R7尤其是氢，卤素，烷氧基，卤代烷氧基等。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及其用于制备药物的用途，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。

6. 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

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. 发明授权

EP2780324B1 HETEROCYCLIC CARBOXAMIDES USEFUL AS INHIBITORS OF PHOSPHODIESTERASE TYPE 10A 有权
标题翻译：杂环化合物羧酰胺抑制剂抑制剂磷酸二酯酶类型10A
公开(公告)号：EP2780324B1
公开(公告)日：2017-05-17
申请号：EP12781349.1
申请日：2012-11-08
申请人： Abbvie Deutschland GmbH & Co. KG , AbbVie Inc.
发明人： GENESTE, Hervé , OCHSE, Michael , DRESCHER, Karla , DINGES, Jürgen , JAKOB, Clarissa
IPC分类号： C07D217/26 , C07D237/32 , C07D401/06 , C07D401/12 , C07D401/14 , C07D417/12 , C07D471/04 , A61K31/472 , A61K31/502 , A61K31/4375 , A61P25/00
CPC分类号： C07D217/26 , A61K31/47 , C07D217/24 , C07D237/32 , C07D401/06 , C07D401/12 , C07D401/14 , C07D409/08 , C07D409/12 , C07D413/06 , C07D417/06 , C07D417/12 , C07D471/04
摘要： The present invention relates to compounds 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.
摘要翻译：本发明涉及作为10A型磷酸二酯酶抑制剂的化合物及其用于制备药物的用途，因此其适用于治疗或控制选自神经障碍和精神疾病的医学病症，以改善与此类症状相关的症状疾病和降低这种疾病的风险。

9. 发明公开

EP2970328A1 NOVEL INHIBITOR COMPOUNDS OF PHOSPHODIESTERASE TYPE 10A 失效
标题翻译： NEUARTIGE INHIBITORVERBINDUNGEN DER PHOSPHODIESTERASE TYP 10A
公开(公告)号：EP2970328A1
公开(公告)日：2016-01-20
申请号：EP14709320.7
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，N-氧化物，互变异构体，前药及其药学上可接受的盐：在式I中，变量X1是CH或N，X2是O或S，并且其中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。

10. 发明公开

EP2922842A2 NOVEL INHIBITOR COMPOUNDS OF PHOSPHODIESTERASE TYPE 10A 无效
标题翻译：化合物作为磷酸二酯酶10A型抑制剂
公开(公告)号：EP2922842A2
公开(公告)日：2015-09-30
申请号：EP13798625.3
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 , JAKOB, Clarissa
IPC分类号： C07D401/14 , A61K31/4353 , A61K31/4427 , C07D401/04 , C07D401/10 , C07D471/04 , C07D487/04 , A61P25/00
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.

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