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61. 发明申请

US20180030033A1 NOVEL INHIBITOR COMPOUNDS OF PHOSPHODIESTERASE TYPE 10A 审中-公开
公开(公告)号：US20180030033A1
公开(公告)日：2018-02-01
申请号：US15724410
申请日：2017-10-04
申请人： AbbVie Inc. , AbbVie Deutschland GmbH & Co. KG
发明人： Hervé GENESTE , Sean Colm TURNER , Michael OCHSE , Karla DRESCHER , Lawrence A. BLACK , Katja JANTOS
IPC分类号： C07D401/14 , C07D471/04 , C07D401/04 , C07D401/10 , 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 Y1 and Y2 are adjacent atoms in Het1, which are independently selected from the group consisting of carbon and nitrogen; k is 0, 1, 2 or 3; Het1 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—Ra 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—Ra as ring members; Het2 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—R1a 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 Het1 and inter alia—halogen, C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, C1-C6-alkoxy, C1-C6-fluoroalkyl, C1-C6-fluoroalkoxy, C3-C6-cycloalkyl etc.

62. 发明授权

US09822171B2 Amyloid-beta binding proteins 有权
公开(公告)号：US09822171B2
公开(公告)日：2017-11-21
申请号：US14618632
申请日：2015-02-10
申请人： AbbVie Deutschland GmbH & Co. KG , AbbVie Inc.
发明人： Stefan Barghorn , Heinz Hillen , Andreas Striebinger , Simone Giaisi , Ulrich Ebert , Lorenzo Benatuil
IPC分类号： C07K16/00 , A61K39/00 , A61K39/395 , C07K16/18 , C07K14/47 , A61K47/48 , A61K49/00
CPC分类号： C07K16/18 , A61K39/3955 , A61K47/6835 , A61K49/00 , C07K14/4711 , C07K2317/21 , C07K2317/24 , C07K2317/30 , C07K2317/31 , C07K2317/54 , C07K2317/55 , C07K2317/56 , C07K2317/565 , C07K2317/569 , C07K2317/622 , C07K2317/624 , C07K2317/626 , C07K2317/92
摘要： The present invention relates to amyloid-beta (Aβ) binding proteins. Antibodies of the invention have high affinity to Aβ(20-42) globulomer or any Aβ form that comprises the globulomer epitope. Method of making and method of using the antibodies of the invention are also provided.

63. 发明授权

US09701679B2 Modulators of 5-HT receptors and methods of use thereof 有权
公开(公告)号：US09701679B2
公开(公告)日：2017-07-11
申请号：US14503198
申请日：2014-09-30
申请人： AbbVie Deutschland GmbH & Co. KG , AbbVie Inc.
发明人： Ying Wang , Jason T. Brewer , Irini Akritopoulou-Zanze , Stevan W. Djuric , Bhadra Shelat , Frauke Pohlki , Wilfried Braje , Ana-Lucia Relo
IPC分类号： C07D487/04 , C07D471/04 , C07D471/14 , C07D491/04 , C07D498/04 , C07D487/14
CPC分类号： C07D487/04 , C07D471/04 , C07D471/14 , C07D487/14 , C07D491/04 , C07D498/04 , Y02E60/321
摘要： The present application relates to 1,2,3,4,4a,5,6,7-octahydropyrazino[1,2-a][1,4]benzodiazepine, 1,2,3,4,4a,5,6,7-octahydropyrazino[1,2-a][1,5]benzodiazepine, 2,3,4,4a,5,6,7,11b-octahydro-1H-pyrido[3,4-d][2]benzazepine, 1,2,3,4,4a,5,6,7-octahydropyrazino[1,2-a][1]benzazepine, 1,2,3,4,4a,5-hexahydro-7H-pyrazino[1,2-a][4,1]benzoxazepine, and 2,3,4,4a,5,6-hexahydro-1H-pyrazino[2,1-d][1,5]benzoxazepine, and 5,6,7,7a,8,9,10,11-octahydropyrazino[1,2-d]pyrido[3,2-b][1,4]diazepine derivatives of formula (I) wherein R1, R2, R3, R4, R5, R6, X1, X2, X3, X4, Y1, Y2, and Y3 are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating disease conditions using such compounds and compositions, and methods for identifying such compounds.

64. 发明申请

US20170166633A1 ANTIBODIES AGAINST THE RGM A PROTEIN AND USES THEREOF 审中-公开
公开(公告)号：US20170166633A1
公开(公告)日：2017-06-15
申请号：US15389627
申请日：2016-12-23
申请人： AbbVie Deutschland GmbH & Co. KG , AbbVie Inc.
发明人： Bernhard K. Mueller , Martin Schmidt , Eve Barlow , Mary Leddy , Chung-Ming Hsieh , Philip Bardwell
IPC分类号： C07K16/22 , A61K45/06 , A61K39/395
CPC分类号： C07K16/22 , A61K39/3955 , A61K45/06 , A61K2039/505 , C07K16/28 , C07K2317/24 , C07K2317/56 , C07K2317/565 , C07K2317/567 , C07K2317/76 , C07K2317/92 , Y02A50/466
摘要： The subject invention relates to isolated proteins, particularly monoclonal antibodies, which bind and neutralize RGM A protein. Specifically, these antibodies have the ability to inhibit the binding of RGM A to its receptor and/or coreceptors. These antibodies or portions thereof of the invention are useful for detecting RGM A and for inhibiting RGM A activity, for example in a human suffering from a disorder including but nor limited to multiple sclerosis, mammalian brain trauma, spinal cord injury, stroke, neurodegenerative diseases, and schizophrenia.

65. 发明申请

US20170073420A1 METHODS FOR TREATING RELAPSING FORMS OF MULTIPLE SCLEROSIS 审中-公开
标题翻译：治疗多发性硬化症相关形式的方法
公开(公告)号：US20170073420A1
公开(公告)日：2017-03-16
申请号：US15261633
申请日：2016-09-09
申请人： AbbVie Inc. , AbbVie Deutschland GmbH & Co. KG
发明人： Steven J. Greenberg , Bernhard K. Mueller , Andreas Popp , Matthew R. Rosebraugh , George M. Haig , Shao-Lee Lin
IPC分类号： C07K16/28 , A61K45/06 , A61K39/395
CPC分类号： A61K45/06 , A61K2039/505 , A61K2039/545 , A61P25/00 , A61P25/28 , C07K16/22 , C07K2317/21 , C07K2317/24 , C07K2317/31 , C07K2317/76 , C07K2317/94
摘要： Disclosed herein are anti-RGMa antibodies and methods of using these antibodies to treat multiple sclerosis, including relapsing forms of multiple sclerosis such as relapsing-remitting multiple sclerosis or relapsing-secondary progressive multiple sclerosis.
摘要翻译：本文公开了抗RGMa抗体和使用这些抗体治疗多发性硬化的方法，包括复发形式的多发性硬化，例如复发性缓解性多发性硬化或复发性继发性进行性多发性硬化症。

66. 发明申请

US20170057966A1 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：US20170057966A1
公开(公告)日：2017-03-02
申请号：US15248994
申请日：2016-08-26
申请人： AbbVie Inc. , AbbVie Deutschland GmbH & Co. KG
发明人： Udo Lange , Michael Ochse , Elizabeth van der Kam , Jeroen van Bergeijk , Sean Turner , Frank Oellien , Patrick Walleser , Wilhelm Amberg , Wilfried Hornberger , Herve Geneste , Mario Mezler , Charles Hutchins
IPC分类号： C07D487/04 , C07D471/04
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用于治疗，缓解或预防由S1P受体介导的疾病或病症的用途。

67. 发明申请

US20170014348A1 Formulations of Nonopioid and Confined Opioid Analgesics 审中-公开
标题翻译：非阿片类药物和限制性阿片类镇痛药的制剂
公开(公告)号：US20170014348A1
公开(公告)日：2017-01-19
申请号：US15278645
申请日：2016-09-28
申请人： AbbVie Deutschland GmbH & Co. KG , AbbVie Inc.
发明人： Joerg Breitenbach , Salih Durak , Sandeep Dutta , Thomas Y. Kessler , Wei Liu , Friedrich W. Richter , Joerg Rosenberg , Gerd Woehrle
IPC分类号： A61K9/28 , A61K31/167 , A61K9/00 , A61K31/485
CPC分类号： A61K9/28 , A61K9/0053 , A61K9/209 , A61K31/167 , A61K31/192 , A61K31/485 , A61K2300/00
摘要： The preferred exemplary embodiments in the present application provide formulations and methods for the delivery of drugs, particularly drugs of abuse, having an abuse-relevant drug substantially confined in the core and a non-abuse relevant drug in a non-core region. These formulations have reduced potential for abuse. In the formulation, preferably the abuse relevant drug is an opioid and the non-abuse relevant drug is acetaminophen or ibuprofen. More preferably, the opioid is hydrocodone, and the non-abuse relevant analgesic is acetaminophen. In certain preferred embodiments, the dosage forms are characterized by resistance to solvent extraction; tampering, crushing or grinding. Certain embodiments of the inventions provide dosage forms that provide an initial burst of release of drug followed by a prolonged period of controllable drug release.
摘要翻译：本申请中优选的示例性实施方案提供用于递送药物，特别是滥用药物，具有基本上限于核心的滥用相关药物和非核心区域中的非滥用相关药物的制剂和方法。这些制剂减少了滥用的可能性。在制剂中，优选滥用相关药物是阿片样物质，非滥用相关药物是对乙酰氨基酚或布洛芬。更优选地，阿片样物质是氢可酮，非滥用相关镇痛药是对乙酰氨基酚。在某些优选的实施方案中，剂型的特征在于耐溶剂萃取; 篡改，破碎或研磨。本发明的某些实施方案提供剂型，其提供药物释放的初始爆发，随后延长药物释放时间。

68. 发明授权

US09527856B2 Oxindole compounds carrying a CO-bound spiro substituent and use thereof for treating vasopressin-related diseases 有权
标题翻译：携带CO键螺旋取代基的羟吲哚化合物及其用于治疗加压素相关疾病的用途
公开(公告)号：US09527856B2
公开(公告)日：2016-12-27
申请号：US14713824
申请日：2015-05-15
申请人： AbbVie Deutschland GmbH & Co. KG
发明人： Wilfried Braje , Hervé Geneste , Wilfried Hornberger , Katja Jantos , Andreas Kling , Claudia Krack , Marcel Van Gaalen
IPC分类号： C07D471/10 , C07D295/135 , C07D305/08 , C07D401/14 , C07D487/10 , C07D209/40 , C07D213/64
CPC分类号： C07D487/10 , C07D209/40 , C07D213/64 , C07D295/135 , C07D305/08 , C07D401/14 , C07D471/10
摘要： The present invention relates to novel substituted oxindole derivatives of formula I wherein the variables are as defined in the claims and the description. The invention further relates to pharmaceutical compositions comprising compounds I and 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，其中变量如权利要求和说明书所定义。本发明还涉及包含化合物I及其用于治疗加压素相关病症的用途的药物组合物。

69. 发明申请

US20160318871A1 NOVEL INHIBITOR COMPOUNDS OF PHOSPHODIESTERASE TYPE 10A 有权
公开(公告)号：US20160318871A1
公开(公告)日：2016-11-03
申请号：US15207137
申请日：2016-07-11
申请人： AbbVie Deutschland GmbH & Co. KG , AbbVie Inc.
发明人： Hervé Geneste , Michael Ochse , Karla Drescher , Jürgen Dinges , Clarissa Jakob
IPC分类号： C07D217/26 , C07D401/14 , C07D471/04 , C07D401/12 , C07D417/12 , C07D409/12 , C07D401/06 , C07D237/32
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. wherein X1 is CH or N, X2 is C—R5 or N, Y is O or S, R1 is inter alia C2-C8-alkyl, C2-C8-alkenyl, C1-C4-fluoroalkyl, C3-C8-cycloalkyl, C5-C8-cycloalkyl carrying a fused benzene ring, or a moiety Z1—Ar1; R2 is a radical of the formula CR21R22R23 or phenyl or 5- or 6-membered hetaryl having 1, 2 or 3 heteroatoms as ring members which are selected from O, S and N, where phenyl and monocyclic hetaryl are unsubstituted or may carry 1, 2 or 3 identical or different substituents Ra, R3 is inter alia hydrogen, C1-C8-alkyl, C2-C8-alkenyl, C1-C4-fluoroalkyl, C3-C8-cycloalkyl, etc, or R2 and R3 together with the nitrogen atom, to which they are bound form an optionally substituted saturated 5- to 7-membered heterocyclic ring which, in addition to the nitrogen atom, may have 1 or 2 further heteroatoms or heteroatom containing groups selected from the group of O, N, S, SO and SO2; R4 is inter alia C1-C4-alkyl, C1-C4-fluoroalkyl, C3-C6-cycloalkyl, C3-C6-cycloalkyl-C1-C4-alkyl or Z4—Ar4; R5 is inter alia hydrogen, halogen, C1-C4-alkyl, C1-C4-fluoroalkyl, C1-C4-alkoxy, C1-C4-fluoroalkoxy, —Z5—Ar5, —O—Z5—Ar5, etc; where Z1 to Z5, Ar1 to Ar5, Ra, R21, R22, and R23 are as defined in the claims.

70. 发明申请

US20160137668A1 NOVEL INHIBITOR COMPOUNDS OF PHOSPHODIESTERASE TYPE 10A 有权
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：US20160137668A1
公开(公告)日：2016-05-19
申请号：US14997997
申请日：2016-01-18
申请人： AbbVie Deutschland GmbH & Co. KG , AbbVie Inc.
发明人： Hervé GENESTE , Michael OCHSE , Karla DRESCHER , Sean TURNER , Berthold BEHL , Loic LAPLANCHE , Jürgen DINGES , Clarissa JAKOB , Lawrence BLACK
IPC分类号： C07D519/00 , C07D401/14 , C07D491/048 , C07D405/14 , C07D471/04 , C07D495/04 , C07D401/06
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, X1 is N or CH, X2 is N or C—R7; X3 is O, S—X4═C(R8)—, where C(R8) is bound to the carbon atom which carries R2, or —X5═C(R9)—, where X5 is bound to the carbon atom which carries R2; X4 is N or C—R9; X5 is N; Het is selected from optionally substituted phenyl, monocyclic hetaryl and fused bicyclic hetaryl; R1 is selected inter alia from hydrogen, halogen, OH, C1-C4-alkyl, trimethylsilyl, C1-C4-alkylsulfanyl, C1-C4-alkoxy-C1-C4-alkyl, C1-C4-alkoxy, C1-C4-alkoxy-C1-C4-alkoxy, the moiety Y1-Cyc1; R2 is selected inter alia from hydrogen, halogen, OH, C1-C4-alkyl, trimethylsilyl, C1-C4-alkoxy-C1-C4-alkyl, C1-C4-alkoxy, C1-C4-alkoxy-C1-C4-alkoxy, C2-C4-alkenyloxy, etc; A represents one of the following groups A1, A2, A3, A4 or A5: where * indicates the points of attachment to Het and to the nitrogen atom, respectively; and where R3 to R9, R3e, R3f, A′, Y1 and Cyc1 are defined in the claims.
摘要翻译：本发明涉及式I的新型化合物，其是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选自神经障碍和精神疾病的医学病症，用于改善与这些疾病相关的症状并降低这种疾病的风险。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R2的碳原子结合 ; 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。

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