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11. 发明申请

US20150111875A1 Aminotetraline and aminoindane derivatives, pharmaceutical compositions containing them, and their use in therapy 有权
标题翻译：氨基四氢化萘和氨基茚满衍生物，含有它们的药物组合物及其在治疗中的应用
公开(公告)号：US20150111875A1
公开(公告)日：2015-04-23
申请号：US14517205
申请日：2014-10-17
申请人： AbbVie Deutschland GmbH & Co. KG , AbbVie Inc.
发明人： Wilhelm Amberg , Frauke Pohlki , Udo Lange , Ying Wang , Jason Brewer , Anil Vasudevan , Yanbin Lao , Charles Hutchins , Hongyu Zhao , Huan-Qiu Li
IPC分类号： C07D403/14 , C07D405/14 , C07D403/10
CPC分类号： A61K31/454 , A61K31/397 , A61K31/4025 , A61K31/4178 , A61K31/4192 , C07D205/04 , C07D207/273 , C07D233/42 , C07D401/12 , C07D403/10 , C07D403/12 , C07D403/14 , C07D405/14
摘要： The present invention relates to aminotetraline and aminoindane derivatives of the formula (I) or a physiologically tolerated salt thereof.The invention relates to pharmaceutical compositions comprising such aminotetraline and aminoindane derivatives, and the use of such aminotetraline and aminoindane derivatives for therapeutic purposes. The aminotetraline and aminoindane derivatives are GlyT1 inhibitors.
摘要翻译：本发明涉及式（I）的氨基四氢化萘和氨基茚满衍生物或其生理上耐受的盐。本发明涉及包含这种氨基四氢化萘和氨基茚满衍生物的药物组合物，以及这种氨基四氢化萘和氨基茚满衍生物用于治疗目的的用途。氨基四氢化萘和氨基茚满衍生物是GlyT1抑制剂。

12. 发明申请

US20150065477A1 CARBOXAMIDE COMPOUNDS AND THEIR USE AS CALPAIN INHIBITORS V 有权
标题翻译：羧酰胺化合物及其作为钙抑制剂V
公开(公告)号：US20150065477A1
公开(公告)日：2015-03-05
申请号：US14390381
申请日：2013-03-14
申请人： ABBVIE DEUTSCHLAND GMBH &CO. KG , ABBVIE INC.
发明人： Andreas Kling , Katja Jantos , Helmut Mack , Achim Möller , Wilfried Hornberger , Gisela Backfisch , Yanbin Lao , Marjoleen Nijsen
IPC分类号： C07D401/14 , C07D491/107 , C07D413/14 , C07D491/048 , C07D401/04 , C07D471/04
CPC分类号： C07D401/14 , C07D401/04 , C07D405/14 , C07D413/14 , C07D471/04 , C07D487/04 , C07D491/048 , C07D491/107
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 and n have the meanings mentioned in the claims and the description, Y is a radical of the formulae (Y1) or (Y2) where # indicates the point of attachment of Y to the pyridine ring, R3, R4, R5, Ry and m have the meanings mentioned in the claims and the description, A is (CH2)p with p being 1, 2, 3 or 4, where one or two hydrogen atoms may be replaced by a radical R6, where A is attached to the 3- or 4-position of the pyrazole radical and R6 has the meaning mentioned in the claims and the description; A1 is (CH2)q with q being 0, 1, 2 or 3, where one or two hydrogen atoms may be replaced by halogen or C1-C4-alkyl; and A2 is (CH2)r with r being 0, 1, 2 or 3, where one or two hydrogen atoms may be replaced by halogen or C1-C4-alkyl, provided that that r+q is 2, 3, 4, 5 or 6; their tautomers, the hydrates thereof, the pharmaceutically suitable salts of the carbox-amide compounds (I), the prodrugs of (I) and the pharmaceutically suitable salts of the prodrugs, tautomers or hydrates of (I).
摘要翻译：本发明涉及新的羧酰胺化合物及其用于制备药物的用途。羧酰胺化合物是钙蛋白酶（钙依赖性半胱氨酸蛋白酶）的抑制剂。因此，本发明还涉及这些羧酰胺化合物用于治疗与升高的钙蛋白酶活性相关的病症的用途。羧酰胺化合物是通式（I）的化合物，其中R 1，R 2和n具有权利要求书和描述中所述的含义，Y是式（Y1）或（Y2）的基团，其中＃表示 Y连接到吡啶环，R3，R4，R5，Ry和m具有权利要求书和说明书中所述的含义，A是（CH 2）p，其中p是1,2,3或4，其中一个或两个氢原子可以被基团R6代替，其中A连接到吡唑基团的3-或4-位，R6具有权利要求书和说明书中提及的含义; A 1是（CH 2）q，其中q是0,1,2或3，其中一个或两个氢原子可以被卤素或C 1 -C 4 - 烷基取代; 并且A 2为（CH 2）r，其中r为0,1,2或3，其中一个或两个氢原子可被卤素或C 1 -C 4 - 烷基取代，条件是该r + q为2,3,4,5 或6; 其互变异构体，其水合物，羧酰胺化合物（I）的药学上合适的盐，（I）的前药和（I）的前药，互变异构体或水合物的药学上合适的盐。

13. 发明申请

US20140275086A1 PYRROLIDINE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM, AND THEIR USE IN THERAPY 有权
公开(公告)号：US20140275086A1
公开(公告)日：2014-09-18
申请号：US14215533
申请日：2014-03-17
申请人： AbbVie Inc. , AbbVie Deutschland GmbH & Co. KG
发明人： Wilhelm Amberg , Frauke Pohlki , Udo Lange , Ying X. Wang , Hongyu H. Zhao , Huan-Qiu Li , Jason T. Brewer , Irini Zanze , Justin Dietrich , Anil Vasudevan , Stevan W. Djuric , Yanbin Lao , Charles W. Hutchins
IPC分类号： C07D207/09 , C07D401/12 , C07D207/48 , C07D401/14 , C07D403/14 , C07D487/04 , C07D487/10 , C07D417/14 , C07D409/14 , C07D495/04 , C07D471/04 , C07D403/12 , C07D405/14
CPC分类号： C07D207/09 , A61K31/4025 , A61K31/44 , C07D207/48 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/14 , C07D409/14 , C07D417/14 , C07D471/04 , C07D487/04 , C07D487/10 , C07D495/04
摘要： The present invention relates to pyrrolidine derivatives of the formula (I), or a physiologically tolerated salt thereof.The invention relates to pharmaceutical compositions comprising such pyrrolidine derivatives, and the use of such pyrrolidine derivatives for therapeutic purposes. The pyrrolidine derivatives are GlyT1 inhibitors.

14. 发明申请

US20190290632A1 Aminotetraline and aminoindane derivatives, pharmaceutical compositions containing them, and their use in therapy 审中-公开
公开(公告)号：US20190290632A1
公开(公告)日：2019-09-26
申请号：US16276144
申请日：2019-02-14
申请人： AbbVie Deutschland GmbH & Co. KG , AbbVie Inc.
发明人： Wilhelm Amberg , Frauke Pohlki , Udo Lange , Ying Wang , Jason Brewer , Anil Vasudevan , Yanbin Lao , Charles Hutchins , Hongyu Zhao , Huan-Qiu Li
IPC分类号： A61K31/454 , C07D405/14 , C07D403/10 , A61K31/4192 , A61K31/4178 , A61K31/4025 , C07D403/12 , C07D403/14 , C07D207/273 , C07D205/04 , C07D401/12 , C07D233/42 , A61K31/397
摘要： The present invention relates to aminotetraline and aminoindane derivatives of the formula (I) or a physiologically tolerated salt thereof.The invention relates to pharmaceutical compositions comprising such aminotetraline and aminoindane derivatives, and the use of such aminotetraline and aminoindane derivatives for therapeutic purposes. The aminotetraline and aminoindane derivatives are GlyT1 inhibitors.

15. 发明申请

US20170173009A1 Aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives, pharmaceutical compositions containing them, and their use in therapy 审中-公开
公开(公告)号：US20170173009A1
公开(公告)日：2017-06-22
申请号：US15449565
申请日：2017-03-03
申请人： AbbVie Deutschland GmbH & Co. KG , AbbVie Inc.
发明人： Wilhelm Amberg , Frauke Pohlki , Udo Lange , Ying Wang , Jason Brewer , Anil Vasudevan , Yanbin Lao , Charles Hutchins , Hongyu Zhao , Huan-Qiu Li
IPC分类号： A61K31/501 , A61K31/4433 , A61K31/4155 , A61K31/4192 , A61K31/4178 , A61K31/397
摘要： The present invention relates to aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives of the formula (I) or a physiologically tolerated salt thereof.The invention relates to pharmaceutical compositions comprising such aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives, and the use of such aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquin oline derivatives for therapeutic purposes. The aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives are GlyT1 inhibitors.

16. 发明授权

US09550754B2 4,5-dihydropyrazole derivatives, pharmaceutical compositions containing them, and their use in therapy 有权
标题翻译： 4,5-二氢吡唑衍生物，含有它们的药物组合物及其在治疗中的用途
公开(公告)号：US09550754B2
公开(公告)日：2017-01-24
申请号：US14849470
申请日：2015-09-09
申请人： ABBVIE DEUTSCHLAND GMBH & CO. KG , ABBVIE INC.
发明人： Wilhelm Amberg , Jason Brewer , Charles Hutchins , Udo Lange , Yanbin Lao , Huan-Qiu Li , Frauke Pohlki , Anil Vasudevan , Ying Wang , Hongyu Zhao
IPC分类号： C07D403/12 , C07D401/14
CPC分类号： C07D403/12 , C07D401/14
摘要： The present invention relates to 4,5-dihydropyrazole derivatives of the formula (I) and physiologically tolerated salts thereof which are GlyT1 inhibitors. The invention further relates to pharmaceutical compositions comprising such 4,5-dihydropyrazole derivatives, and the use of such 4,5-dihydropyrazole derivatives for therapeutic purposes.
摘要翻译：本发明涉及式（I）的4,5-二氢吡唑衍生物及其生理学上耐受的盐，它们是GlyT1抑制剂。本发明还涉及包含这种4,5-二氢吡唑衍生物的药物组合物，以及这些用于治疗目的的这种4,5-二氢吡唑衍生物的用途。

17. 发明授权

US09150545B2 Carboxamide compounds and their use as calpain inhibitors V 有权
标题翻译：羧酰胺化合物及其作为钙蛋白酶抑制剂的用途
公开(公告)号：US09150545B2
公开(公告)日：2015-10-06
申请号：US14390381
申请日：2013-03-14
申请人： ABBVIE DEUTSCHLAND GMBH & CO. KG , ABBVIE INC.
发明人： Andreas Kling , Katja Jantos , Helmut Mack , Achim Möller , Wilfried Hornberger , Gisela Backfisch , Yanbin Lao , Marjoleen Nijsen
IPC分类号： A61K31/44 , C07D221/18 , C07D401/00 , C07D401/14 , C07D405/14 , C07D401/04 , C07D471/04 , C07D487/04 , C07D413/14 , C07D491/048 , C07D491/107
CPC分类号： C07D401/14 , C07D401/04 , C07D405/14 , C07D413/14 , C07D471/04 , C07D487/04 , C07D491/048 , C07D491/107
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 and n have the meanings mentioned in the claims and the description, Y is a radical of the formulae (Y1) or (Y2) where # indicates the point of attachment of Y to the pyridine ring, R3, R4, R5, Ry and m have the meanings mentioned in the claims and the description, A is (CH2)p with p being 1, 2, 3 or 4, where one or two hydrogen atoms may be replaced by a radical R6, where A is attached to the 3- or 4-position of the pyrazole radical and R6 has the meaning mentioned in the claims and the description; A1 is (CH2)q with q being 0, 1, 2 or 3, where one or two hydrogen atoms may be replaced by halogen or C1-C4-alkyl; and A2 is (CH2)r with r being 0, 1, 2 or 3, where one or two hydrogen atoms may be replaced by halogen or C1-C4-alkyl, provided that that r+q is 2, 3, 4, 5 or 6; their tautomers, the hydrates thereof, the pharmaceutically suitable salts of the carbox-amide compounds (I), the prodrugs of (I) and the pharmaceutically suitable salts of the prodrugs, tautomers or hydrates of (I).
摘要翻译：本发明涉及新的羧酰胺化合物及其用于制备药物的用途。羧酰胺化合物是钙蛋白酶（钙依赖性半胱氨酸蛋白酶）的抑制剂。因此，本发明还涉及这些羧酰胺化合物用于治疗与升高的钙蛋白酶活性相关的病症的用途。羧酰胺化合物是通式（I）的化合物，其中R 1，R 2和n具有权利要求书和描述中所述的含义，Y是式（Y1）或（Y2）的基团，其中＃表示 Y连接到吡啶环，R3，R4，R5，Ry和m具有权利要求书和说明书中所述的含义，A是（CH 2）p，其中p是1,2,3或4，其中一个或两个氢原子可以被基团R6代替，其中A连接到吡唑基团的3-或4-位，R6具有权利要求书和说明书中提及的含义; A 1是（CH 2）q，其中q是0,1,2或3，其中一个或两个氢原子可以被卤素或C 1 -C 4 - 烷基取代; 并且A 2为（CH 2）r，其中r为0,1,2或3，其中一个或两个氢原子可被卤素或C 1 -C 4 - 烷基取代，条件是该r + q为2,3,4,5 或6; 其互变异构体，其水合物，羧酰胺化合物（I）的药学上合适的盐，（I）的前药和（I）的前药，互变异构体或水合物的药学上合适的盐。

18. 发明申请

US20150111867A1 Aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives, pharmaceutical compositions containing them, and their use in therapy 有权
标题翻译：氨基荧光素，氨基硫辛烷和氨基-1,2,3,4-四氢喹啉衍生物，含有它们的药物组合物及其在治疗中的用途
公开(公告)号：US20150111867A1
公开(公告)日：2015-04-23
申请号：US14517034
申请日：2014-10-17
申请人： AbbVie Deutschland GmbH & Co. KG , AbbVie Inc.
发明人： Wilhelm Amberg , Frauke Pohlki , Udo Lange , Ying Wang , Jason Brewer , Anil Vasudevan , Yanbin Lao , Charles Hutchins , Hongyu Zhao , Huan-Qiu Li
IPC分类号： C07D405/14 , C07D405/04
CPC分类号： A61K31/501 , A61K31/397 , A61K31/4155 , A61K31/4178 , A61K31/4192 , A61K31/4433 , C07D311/58 , C07D405/04 , C07D405/14
摘要： The present invention relates to aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives of the formula (I) or a physiologically tolerated salt thereofThe invention relates to pharmaceutical compositions comprising such aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives, and the use of such aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquin oline derivatives for therapeutic purposes. The aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives are GlyT1 inhibitors.
摘要翻译：本发明涉及式（I）的氨基苯并二氢吡喃，氨基硫色烷和氨基-1,2,3,4-四氢喹啉衍生物或其生理上可耐受的盐。本发明涉及包含这种氨基苯并二氢吡喃，氨基硫色烷和氨基-1,2 ，3,4-四氢喹啉衍生物，以及用于治疗目的的这种氨基苯并二氢吡喃，氨基硫辛烷和氨基-1,2,3,4-四氢喹啉衍生物的用途。氨基苯并二氢吡喃，氨基硫色烷和氨基-1,2,3,4-四氢喹啉衍生物是GlyT1抑制剂。

19. 发明授权

US10174061B2 Carbidopa and L-dopa prodrugs and methods of use 有权
公开(公告)号：US10174061B2
公开(公告)日：2019-01-08
申请号：US15715245
申请日：2017-09-26
申请人： AbbVie Inc.
发明人： Benoit Cardinal-David , Vincent S. Chan , Brian P. Enright , Ye Huang , Alexander D. Huters , Russell C. Klix , Scott W. Krabbe , Philip R. Kym , Yanbin Lao , Xiaochun Lou , Sean E. Mackey , Mark A. Matulenko , Peter T. Mayer , Christopher P. Miller , James Stambuli , Eric A. Voight , Zhi Wang , Geoff G. Zhang , Valentino J. Stella
IPC分类号： C07F9/09 , A61K31/661 , C07F9/06 , A61K31/6615 , C07C281/02 , C07C309/24 , C07C47/277 , A61K45/06
摘要： The present disclosure relates to (a) carbidopa prodrugs, (b) pharmaceutical combinations and compositions comprising a carbidopa prodrug and/or an L-dopa prodrug, and (c) methods of treating Parkinson's disease and associated conditions comprising administering a carbidopa prodrug and an L-dopa prodrug to a subject with Parkinson's disease.

20. 发明申请

US20180079762A1 Carbidopa and L-Dopa Prodrugs and Methods of use 审中-公开
公开(公告)号：US20180079762A1
公开(公告)日：2018-03-22
申请号：US15715245
申请日：2017-09-26
申请人： AbbVie Inc.
发明人： Benoit Cardinal-David , Vincent S. Chan , Kassibla Dempah , Brian P. Enright , Rodger F. Henry , Raimundo Ho , Ye Huang , Alexander D. Huters , Russell C. Klix , Scott W. Krabbe , Philip R. Kym , Yanbin Lao , Xiaochun Lou , Sean E. Mackey , Mark A. Matulenko , Peter T. Mayer , Christopher P. Miller , James Stambuli , Eric A. Voight , Zhi Wang , Geoff G. Zhang , Valentino J. Stella
IPC分类号： C07F9/09 , A61K31/661 , C07F9/06 , A61K45/06 , C07C47/277 , C07C309/24 , C07C281/02 , A61K31/6615
CPC分类号： C07F9/094 , A61K31/661 , A61K31/6615 , A61K45/06 , C07B2200/13 , C07C47/277 , C07C281/02 , C07C309/24 , C07F9/06 , A61K2300/00
摘要： The present disclosure relates to (a) carbidopa prodrugs, (b) pharmaceutical combinations and compositions comprising a carbidopa prodrug and/or an L-dopa prodrug, and (c) methods of treating Parkinson's disease and associated conditions comprising administering a carbidopa prodrug and an L-dopa prodrug to a subject with Parkinson's disease.

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