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1. 发明申请

WO2013068470A1 INHIBITORS OF PHOSPHODIESTERASE TYPE 10A 审中-公开
标题翻译：磷酸二酯酶类型10A的抑制剂
公开(公告)号：WO2013068470A1
公开(公告)日：2013-05-16
申请号：PCT/EP2012/072150
申请日：2012-11-08
申请人： ABBOTT GMBH & CO. KG , ABBVIE INC.
发明人： GENESTE, Hervé , OCHSE, Michael , DRESCHER, Karla , TURNER, Sean , BEHL, Berthold , LAPLANCHE, Loic , DINGES, Jürgen , JAKOB, Clarissa , BLACK, Lawrence A.
IPC分类号： C07D401/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D491/048 , C07D495/04 , C07D519/00 , A61K31/519 , A61P25/00
CPC分类号： C07D519/00 , C07D401/06 , C07D401/14 , C07D405/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D491/048 , C07D495/04
摘要： The present invention relates to novel compounds of the formula (I) 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 Q is O or S, X 1 is N or CH, X 2 is N or C-R 7 ; X 3 is O, S, -X 4 =C(R 8 )-, where C(R 8 ) is bound to the carbon atom which carries R 2 , or -X 5 =C(R 9 )-, where X 5 is bound to the carbon atom which carries R 2 ; X 4 is N or C-R 9 ; X 5 is N; Het is selected from optionally substituted phenyl, monocyclic hetaryl and fused bicyclic hetaryl; R 1 is selected inter alia from hydrogen, halogen, OH, C 1 -C 4 -alkyl, trimethylsilyl, C 1 -C 4 -alkylsulfanyl, C 1 -C 4 -alkoxy-C 1 -C 4 -alkyl, C 1 -C 4 - alkoxy, C 1 -C 4 -alkoxy-C 1 -C 4 -alkoxy, the moiety Y 1 -Cyc 1 ; R 2 is selected inter alia from hydrogen, halogen, OH, C 1 -C 4 -alkyl, trimethylsilyl, C 1 -C 4 -alkoxy-C 1 -C 4 -alkyl, C 1 -C 4 -alkoxy, C 1 -C 4 - alkoxy-C 1 -C 4 -alkoxy, C 2 -C 4 -alkenyloxy, etc; A represents one of the following groups A 1 , A 2 , A 3 , A 4 or A 5 : where * indicates the points of attachment to Het and to the nitrogen atom, respectively; and where R 3 to R 9 , R 3e , R 3f , A', Y 1 and Cyc 1 are defined in the claims.
摘要翻译：本发明涉及作为10A型磷酸二酯酶抑制剂的式（I）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障碍的医学病症，用于改善与这种障碍相关的症状并降低这种障碍的风险。其中Q为O或S，X1为N或CH，X2为N或C-R7; X3是O，S，-X4 = C（R8） - ，其中C（R8）与携带R2的碳原子结合，或-X5 = C（R9） - ，其中X5与携带的碳原子结合 R2; X4是N或C-R9; X5是N; Het选自任选取代的苯基，单环杂芳基和稠合双环杂芳基; R1特别是选自氢，卤素，OH，C 1 -C 4烷基，三甲基甲硅烷基，C 1 -C 4烷基硫烷基，C 1 -C 4 - 烷氧基-C 1 -C 4 - 烷基，C 1 -C 4 - 烷氧基，C 1 -C 4烷氧基 - C1-C4-烷氧基，Y1-Cyc1部分; R2特别是选自氢，卤素，OH，C 1 -C 4 - 烷基，三甲基甲硅烷基，C 1 -C 4 - 烷氧基-C 1 -C 4 - 烷基，C 1 -C 4 - 烷氧基，C 1 -C 4 - 烷氧基-C 1 -C 4烷氧基， C2-C4-烯氧基等; A代表以下组A1，A2，A3，A4或A5：其中*表示分别与Het和氮原子相连的点; 并且在权利要求中定义R3至R9，R3e，R3f，A'，Y1和Cyc1。

2. 发明申请

WO2012020130A1 PHENALKYLAMINE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM, AND THEIR USE IN THERAPY 审中-公开
标题翻译： PHENALKYLAMINE衍生物，含有它们的药物组合物及其在治疗中的使用
公开(公告)号：WO2012020130A1
公开(公告)日：2012-02-16
申请号：PCT/EP2011/063971
申请日：2011-08-12
申请人： ABBOTT GMBH & CO. KG , ABBOTT LABORATORIES , AMBERG, Wilhelm , OCHSE, Michael , LANGE, Udo , BEHL, Berthold , HORNBERGER, Wilfried , MEZLER, Mario , POHLKI, Frauke , TURNER, Sean , HUTCHINS, Charles
发明人： AMBERG, Wilhelm , OCHSE, Michael , LANGE, Udo , BEHL, Berthold , HORNBERGER, Wilfried , MEZLER, Mario , POHLKI, Frauke , TURNER, Sean , HUTCHINS, Charles
IPC分类号： C07C311/04 , C07C311/05 , C07C311/10 , C07D205/04 , C07D207/08 , C07D211/22 , C07D231/18 , C07D233/84 , C07D207/267 , C07D295/03 , A61K31/18 , A61K31/415 , A61K31/4164 , A61P25/28 , A61P25/18
CPC分类号： C07C311/06 , C07C311/04 , C07C311/05 , C07C311/10 , C07C2601/02 , C07C2601/04 , C07D205/04 , C07D207/08 , C07D207/267 , C07D231/18 , C07D233/42 , C07D233/84 , C07D295/135 , C07D401/12 , C07D403/12
摘要： The present invention relates to phenalkylamine derivatives of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such phenalkylamine derivatives, and the use of such phenalkylamine derivatives for therapeutic purposes. The phenalkylamine derivatives are GlyT1 inhibitors.
摘要翻译：本发明涉及式（I）的苯烷基胺衍生物或其生理上耐受的盐。本发明涉及包含这种苯烷基胺衍生物的药物组合物，以及这种苯烷基胺衍生物用于治疗目的的用途。酚烷基胺衍生物是GlyT1抑制剂。

3. 发明申请

WO2017046117A1 SUBSTITUTED ISOXAZOLOPYRIDAZINONES AND ISOTHIAZOLOPYRIDAZINONES AND METHODS OF USE 审中-公开
标题翻译：取代的异丙嗪酰胺和异亮氨酸亚胺碱及其使用方法
公开(公告)号：WO2017046117A1
公开(公告)日：2017-03-23
申请号：PCT/EP2016/071619
申请日：2016-09-14
申请人： ABBVIE INC. , ABBVIE DEUTSCHLAND GMBH & CO. KG
发明人： DINGES, Jürgen , MOELLER, Achim , OCHSE, Michael , SCHMIDT, Martin , SCHULZ, Michael , TURNER, Sean , VAN DER KAM, Elizabeth Louise , VASUDEVAN, Anil
IPC分类号： C07D498/04 , C07D513/04 , A61K31/4985 , A61P1/04 , A61P25/30
CPC分类号： C07D498/04 , C07D513/04
摘要： Compounds of formula (I) (I) and pharmaceutically acceptable salts thereof, wherein R 1 , R 2 and R 3 are as defined in the specification, are useful in treating conditions or disorders prevented by or ameliorated by positive allosteric modulation of the ϒ-aminobutyric acid B (GABA-B) receptor. Methods for making the compounds are described. Also described are pharmaceutical compositions of compounds of formula (I), and methods for using such compounds and compositions.
摘要翻译：式（I）（I）化合物及其药学上可接受的盐，其中R 1，R 2和R 3如说明书中所定义，可用于治疗通过γ-氨基丁酸B的正性变构调节而被预防或改善的病症或病症（GABA-B）受体。描述了制备化合物的方法。还描述了式（I）化合物的药物组合物，以及使用这些化合物和组合物的方法。

4. 发明申请

WO2016169995A1 SUBSTITUTED PYRAZOLOPYRIMIDINES AND METHOD OF USE 审中-公开
标题翻译：取代的吡唑并嘧啶及其使用方法
公开(公告)号：WO2016169995A1
公开(公告)日：2016-10-27
申请号：PCT/EP2016/058779
申请日：2016-04-20
申请人： ABBVIE DEUTSCHLAND GMBH & CO. KG , ABBVIE INC.
发明人： FAGHIH, Ramin , MOELLER, Achim , OCHSE, Michael , POHLKI, Frauke , SCHMIDT, Martin , SCHULZ, Michael , SIPPY, Kevin , TURNER, Sean , VAN DER KAM, Elizabeth Louise
IPC分类号： C07D487/04 , C07D519/00
CPC分类号： C07D487/04 , A61K31/519 , C07D519/00
摘要： Compounds of formula (I) (I) and pharmaceutically acceptable salts thereof, wherein R 1 , R 2 , R 3 , R 4 , L 1 and G 1 are as defined in the specification, are useful in treating conditions or disorders prevented by or ameliorated by positive allosteric modulation of the γ-aminobutyric acid B (GABA-B) receptor. Methods for making the compounds are described. Also described are pharmaceutical compositions of compounds of formula (I), and methods for using such compounds and compositions.
摘要翻译：式（I）（I）化合物及其药学上可接受的盐，其中R 1，R 2，R 3，R 4，L 1和G 1如说明书中所定义，可用于治疗通过正性变构调节而防止或改善的病症或病症 γ-氨基丁酸B（GABA-B）受体。描述了制备化合物的方法。还描述了式（I）化合物的药物组合物，以及使用这些化合物和组合物的方法。

5. 发明申请

WO2017036978A1 FUSED HETEROCYCLIC COMPOUNDS AS S1P MODULATORS 审中-公开
标题翻译：熔融杂环化合物作为S1P调节剂
公开(公告)号：WO2017036978A1
公开(公告)日：2017-03-09
申请号：PCT/EP2016/070225
申请日：2016-08-26
申请人： ABBVIE INC. , ABBVIE DEUTSCHLAND GMBH & CO. KG
发明人： LANGE, Udo , OCHSE, Michael , VAN DER KAM, Elizabeth , VAN BERGEIJK, Jeroen , TURNER, Sean , OELLIEN, Frank , WALLESER, Patrick , AMBERG, Wilhelm , HORNBERGER, Wilfried , GENESTE, Herve , MEZLER, Mario , HUTCHINS, Charles
IPC分类号： C07D471/04 , A61K31/437 , A61K31/4375 , A61P25/00
CPC分类号： C07D487/04 , C07D471/04
摘要： The invention relates to heterocyclic 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.
摘要翻译：本发明涉及作为S1P调节剂的杂环化合物，包含这些化合物的药物组合物及其在治疗，缓解或预防S1P受体介导的疾病或病症中的用途。

6. 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。

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