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1. 发明授权

US08278327B2 PDE10 inhibitors and related compositions and methods 有权
标题翻译： PDE10抑制剂及相关组合物和方法
公开(公告)号：US08278327B2
公开(公告)日：2012-10-02
申请号：US12848766
申请日：2010-08-02
申请人： John E. Bergmann , Neil S. Cutshall , Rene Onrust , Hongkui Zeng , Jennifer Lynn Gage , Derek Johnston , Sándor Cseh , László Ürögdi , Ákos Papp
发明人： John E. Bergmann , Neil S. Cutshall , Rene Onrust , Hongkui Zeng , Jennifer Lynn Gage , Derek Johnston , Sándor Cseh , László Ürögdi , Ákos Papp
IPC分类号： A01N43/42 , A61K31/47 , C07D215/00
CPC分类号： A61K31/341 , A61K31/404 , A61K31/4184 , A61K31/4409 , A61K31/47 , A61K31/4965 , A61K31/5415 , C07D209/18 , C07D213/81 , C07D215/36 , C07D235/16 , C07D235/28 , C07D249/18 , C07D279/16 , C07D333/24 , C07D405/12
摘要： Compounds that inhibit PDE10 are disclosed that have utility in the treatment of a variety of conditions, including (but not limited to) psychotic, anxiety, movement disorders and/or neurological disorders such as Parkinson's disease, Huntington's disease, Alzheimer's disease, encephalitis, phobias, epilepsy, aphasia, Bell's palsy, cerebral palsy, sleep disorders, pain, Tourette syndrome, schizophrenia, delusional disorders, drug-induced psychosis and panic and obsessive-compulsive disorders. The compounds have the general structure: wherein m, n, p, x, R, R1, R2, R3, R4, R5, A and B, are defined herein, including pharmaceutically acceptable salts, stereoisomers, solvates or prodrugs thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for inhibiting PDE10 in a warm-blooded animal in need of the same.
摘要翻译：公开了抑制PDE10的化合物，其可用于治疗各种病症，包括（但不限于）精神病性，焦虑症，运动障碍和/或神经障碍，例如帕金森病，亨廷顿氏病，阿尔茨海默病，脑炎，恐惧症癫痫，失语症，贝尔麻痹，脑性麻痹，睡眠障碍，疼痛，图雷特综合征，精神分裂症，妄想症，药物诱发的精神病，恐慌和强迫症。该化合物具有以下通式：其中m，n，p，x，R，R 1，R 2，R 3，R 4，R 5，A和B在本文中定义，包括其药学上可接受的盐，立体异构体，溶剂合物或前药。还公开了含有本发明化合物与药学上可接受的载体的组合物的组合物，以及涉及其在需要其的温血动物中用于抑制PDE10的方法。

2. 发明申请

US20110091388A1 USE OF PDE7 INHIBITORS FOR THE TREATMENT OF MOVEMENT DISORDERS 审中-公开
标题翻译：使用PDE7抑制剂治疗运动障碍
公开(公告)号：US20110091388A1
公开(公告)日：2011-04-21
申请号：US12974693
申请日：2010-12-21
申请人： John E. Bergmann , Neil S. Cutshall , Gregory A. Demopulos , Vincent A. Florio , George A. Gaitanaris , Patrick Gray , John Hohmann , Rene Onrust , Hongkui Zeng
发明人： John E. Bergmann , Neil S. Cutshall , Gregory A. Demopulos , Vincent A. Florio , George A. Gaitanaris , Patrick Gray , John Hohmann , Rene Onrust , Hongkui Zeng
IPC分类号： A61K49/00 , A61K31/197 , A61K31/519 , A61K31/517 , A61K31/433 , A61P25/14 , A61P25/16 , A61P25/00
CPC分类号： A61K31/195 , A61K31/433 , A61K31/519 , A61K31/527
摘要： A method of treating a movement abnormality associated with the pathology of a neurological movement disorder, such as Parkinson's disease or Restless Leg(s) Syndrome by administering a therapeutically effective amount of a PDE7 inhibitory agent. An aspect of the invention provides for the administration of a PDE& inhibitory agent in conjunction with a dopamine agonist or precursor, such as levodopa. In another aspect of the invention, the PDE7 inhibitory agent may be selective for PDE7 relative to other molecular targets (i) known to be involved with the pathology of Parkinson's disease or (ii) at which other drug(s) that are therapeutically effective to treat Parkinson's disease act.
摘要翻译：通过施用治疗有效量的PDE7抑制剂来治疗与神经运动障碍的病理学相关的运动异常的方法，例如帕金森病或不宁腿综合症。本发明的一个方面提供了与多巴胺激动剂或前体如左旋多巴结合施用PDE和抑制剂。在本发明的另一方面，PDE7抑制剂可以相对于已知与帕金森病病理学有关的其它分子靶标（i）可能对PDE7具有选择性，或（ii）其他治疗有效的药物治疗帕金森病。

3. 发明授权

US07151112B1 Pharmaceutical uses and synthesis of nicotinamides 失效
标题翻译：制药用途和合成烟酰胺
公开(公告)号：US07151112B1
公开(公告)日：2006-12-19
申请号：US10744380
申请日：2003-12-23
申请人： Neil S Cutshall , Scott C Jeffrey
发明人： Neil S Cutshall , Scott C Jeffrey
IPC分类号： A61K31/4427 , A61K31/4412 , C07D213/62 , C07D213/24
CPC分类号： C07D213/64 , C07D213/75 , C07D213/82
摘要： This invention is directed to methods of using a compound of the formula and pharmaceutically acceptable salts thereof, wherein n, X, R1 and R2 are disclosed herein, for treating inflammatory events in an animal subject.
摘要翻译：本发明涉及使用其中n，X，R 1和R 2的化合物及其药学上可接受的盐的方法，用于治疗炎症动物受试者的事件。

4. 发明授权

US08377930B2 PDE10 inhibitors and related compositions and methods 有权
公开(公告)号：US08377930B2
公开(公告)日：2013-02-19
申请号：US12535598
申请日：2009-08-04
申请人： Neil S. Cutshall , Jennifer Lynn Gage , Thomas Neil Wheeler
发明人： Neil S. Cutshall , Jennifer Lynn Gage , Thomas Neil Wheeler
IPC分类号： A61K31/536 , A61K31/47 , C07D215/12 , C07D265/36
CPC分类号： C07D401/04 , A61K31/15 , A61K31/357 , A61K31/36 , A61K31/40 , A61K31/41 , A61K31/415 , A61K31/4184 , A61K31/4196 , A61K31/425 , A61K31/47 , A61K31/5375 , A61K31/54 , C07C243/32 , C07C251/80 , C07C251/86 , C07C251/88 , C07C255/66 , C07C2601/08 , C07D213/56 , C07D213/74 , C07D215/14 , C07D231/12 , C07D235/16 , C07D249/04 , C07D249/08 , C07D257/06 , C07D265/36 , C07D275/02 , C07D295/135 , C07D295/155 , C07D317/62 , C07D319/18 , C07D333/60
摘要： Compounds that inhibit PDE10 are disclosed that have utility in the treatment of a variety of conditions, including (but not limited to) psychotic, anxiety, movement disorders and/or neurological disorders such as Parkinson's disease, Huntington's disease, Alzheimer's disease, encephalitis, phobias, epilepsy, aphasia, Bell's palsy, cerebral palsy, sleep disorders, pain, Tourette's syndrome, schizophrenia, delusional disorders, drug-induced psychosis and panic and obsessive-compulsive disorders. Pharmaceutically acceptable salts, stereoisomers, solvates and prodrugs of the compounds are also provided. Also disclosed are compositions containing a compound in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for inhibiting PDE10 in a warm-blooded animal in need of the same.

5. 发明申请

US20080300240A1 PDE10 INHIBITORS AND RELATED COMPOSITIONS AND METHODS 有权
标题翻译： PDE10抑制剂及相关组合物和方法
公开(公告)号：US20080300240A1
公开(公告)日：2008-12-04
申请号：US12124051
申请日：2008-05-20
申请人： John E. Bergmann , Neil S. Cutshall , Rene Onrust , Hongkui Zeng , Jennifer Lynn Gage , Derek Johnston , Sandor Cseh , Laszlo Urogdi , Akos Papp
发明人： John E. Bergmann , Neil S. Cutshall , Rene Onrust , Hongkui Zeng , Jennifer Lynn Gage , Derek Johnston , Sandor Cseh , Laszlo Urogdi , Akos Papp
IPC分类号： A61K31/5415 , C07D279/14 , C07D209/18 , A61K31/404 , A61K31/47 , A61K31/341 , C07D215/36 , C07D235/28 , A61P25/00 , A61K31/4965 , A61K31/4184 , A61K31/4409 , C07D213/81
CPC分类号： A61K31/341 , A61K31/404 , A61K31/4184 , A61K31/4409 , A61K31/47 , A61K31/4965 , A61K31/5415 , C07D209/18 , C07D213/81 , C07D215/36 , C07D235/16 , C07D235/28 , C07D249/18 , C07D279/16 , C07D333/24 , C07D405/12
摘要： Compounds that inhibit PDE10 are disclosed that have utility in the treatment of a variety of conditions, including (but not limited to) psychotic, anxiety, movement disorders and/or neurological disorders such as Parkinson's disease, Huntington's disease, Alzheimer's disease, encephalitis, phobias, epilepsy, aphasia, Bell's palsy, cerebral palsy, sleep disorders, pain, Tourette syndrome, schizophrenia, delusional disorders, drug-induced psychosis and panic and obsessive-compulsive disorders. The compounds have the general structure: wherein m, n, p, x, R, R1, R2, R3, R4, R5, A and B, are defined herein, including pharmaceutically acceptable salts, stereoisomers, solvates or prodrugs thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for inhibiting PDE 10 in a warm-blooded animal in need of the same.
摘要翻译：公开了抑制PDE10的化合物，其可用于治疗各种病症，包括（但不限于）精神病性，焦虑症，运动障碍和/或神经障碍，例如帕金森病，亨廷顿氏病，阿尔茨海默病，脑炎，恐惧症癫痫，失语症，贝尔麻痹，脑性麻痹，睡眠障碍，疼痛，图雷特综合征，精神分裂症，妄想症，药物诱发的精神病，恐慌和强迫症。该化合物具有以下通式：其中m，n，p，x，R，R 1，R 2，R 3，R 4，R 5，A和B在本文中定义，包括其药学上可接受的盐，立体异构体，溶剂合物或前药。还公开了含有本发明化合物与药学上可接受的载体组合的组合物，以及涉及其在需要其的温血动物中用于抑制PDE10的方法。

6. 发明申请

US20080260643A1 USE OF PDE7 INHIBITORS FOR THE TREATMENT OF MOVEMENT DISORDERS 审中-公开
标题翻译：使用PDE7抑制剂治疗运动障碍
公开(公告)号：US20080260643A1
公开(公告)日：2008-10-23
申请号：US12057368
申请日：2008-03-27
申请人： John E. Bergmann , Neil S. Cutshall , Gregory A. Demopulos , Vincent A. Florio , George Gaitanaris , Patrick Gray , John Hohmann , Rene Onrust , Hongkui Zeng
发明人： John E. Bergmann , Neil S. Cutshall , Gregory A. Demopulos , Vincent A. Florio , George Gaitanaris , Patrick Gray , John Hohmann , Rene Onrust , Hongkui Zeng
IPC分类号： A61K31/433 , A61K31/195 , A61K31/519 , A61P25/00 , A61P25/28 , A61K51/04 , A61K31/527
CPC分类号： A61K31/195 , A61K31/433 , A61K31/519 , A61K31/527
摘要： A method of treating a movement abnormality associated with the pathology of a neurological movement disorder, such as Parkinson's disease or Restless Leg(s) Syndrome by administering a therapeutically effective amount of a PDE7 inhibitory agent. An aspect of the invention provides for the administration of a PDE& inhibitory agent in conjunction with a dopamine agonist or precursor, such as levodopa. In another aspect of the invention, the PDE7 inhibitory agent may be selective for PDE7 relative to other molecular targets (i) known to be involved with the pathology of Parkinson's disease or (ii) at which other drug(s) that are therapeutically effective to treat Parkinson's disease act.
摘要翻译：通过施用治疗有效量的PDE7抑制剂来治疗与神经运动障碍的病理学相关的运动异常的方法，例如帕金森病或不宁腿综合症。本发明的一个方面提供了与多巴胺激动剂或前体如左旋多巴结合施用PDE和抑制剂。在本发明的另一方面，PDE7抑制剂可以相对于已知与帕金森病病理学有关的其它分子靶标（i）可能对PDE7具有选择性，或（ii）其他治疗有效的药物治疗帕金森病。

7. 发明授权

US07141590B2 Pharmaceutical uses and synthesis of nicotinanilide-N-oxides 失效
公开(公告)号：US07141590B2
公开(公告)日：2006-11-28
申请号：US10015861
申请日：2001-12-12
申请人： Neil S Cutshall , Kraig M Yager
发明人： Neil S Cutshall , Kraig M Yager
IPC分类号： A61K31/4412 , C07D211/94
CPC分类号： C07D213/89 , C07D405/12
摘要： Disclosed are nicotinanilide-N-oxide compounds, methods for their production, pharmaceutical compositions which include these compounds, and methods for their use in various therapies.

8. 发明授权

US06777432B1 Pharmaceutical uses and synthesis of nicotinamides 失效
标题翻译：制药用途和合成烟酰胺
公开(公告)号：US06777432B1
公开(公告)日：2004-08-17
申请号：US10237258
申请日：2002-09-04
申请人： Neil S. Cutshall , Scott C. Jeffrey
发明人： Neil S. Cutshall , Scott C. Jeffrey
IPC分类号： A61K3144
CPC分类号： C07D213/64 , C07D213/75 , C07D213/82
摘要： A compound of the formula and pharmaceutically acceptable salts thereof, wherein R1 is selected from (R3)C(═O)—N(R4)— and (R3)(R4)N—C(═O)—; R2 is selected from —OR5 and —N(R5)(R6); n is 0, 1, 2 or 3; X is selected from oxygen and sulfur; and R3, R4, R5 and R6 are independently selected from hydrogen, alkyl, heteroalkyl, aryl, aryl(akylene), heteroaryl, heteroaryl(alkylene), carbocycle, carbocycle(alkylene), heterocycle, and heterocycle(alkylene); as well as pharmaceutical compositions containing said compound. The compounds and compositions are useful in, for example, the treatment of inflammatory events in an animal subject.
摘要翻译：式（I）化合物及其药学上可接受的盐，其中R 1选自（R 3）C（= O）-N（R 4） - 和（R 3）（R 4） = O） - ; R 2选自-OR 5和-N（R 5）（R 6）; n为0,1,2或3; X选自氧和硫; 并且R 3，R 4，R 5和R 6独立地选自氢，烷基，杂烷基，芳基，芳基（亚烷基），杂芳基，杂芳基（亚烷基），碳环，碳环（亚烷基），杂环和杂环（亚烷基）; 以及含有所述化合物的药物组合物。化合物和组合物可用于例如在动物受试者中治疗炎性事件。

9. 发明授权

US08343970B2 PDE10 inhibitors and related compositions and methods 有权
公开(公告)号：US08343970B2
公开(公告)日：2013-01-01
申请号：US13045162
申请日：2011-03-10
申请人： Neil S. Cutshall , Jennifer Lynn Gage , Thomas Neil Wheeler , Thomas L. Little
发明人： Neil S. Cutshall , Jennifer Lynn Gage , Thomas Neil Wheeler , Thomas L. Little
IPC分类号： A61K31/5377 , A61K31/497 , A61K31/4709 , A61K31/4545 , A61K31/454 , A61K31/4535 , A61K31/4525 , A61K31/444 , A61K31/4439 , A61K31/4436 , A61K31/443 , A61K31/426 , A61K31/4245 , A61K31/421 , A61K31/4196 , A61K31/4192 , A61K31/4164 , A61K31/4155 , A61K31/34 , C07D417/10 , C07D413/14 , C07D413/10 , C07D405/06 , C07D407/14 , C07D407/10 , C07D407/06 , C07D307/46 , C07D263/32 , C07D231/12
CPC分类号： C07D307/46 , A61K31/341 , A61K31/415 , A61K31/4155 , A61K31/4192 , A61K31/4196 , A61K31/421 , A61K31/422 , A61K31/4245 , A61K31/427 , A61K31/433 , A61K31/454 , A61K31/4545 , A61K31/4709 , A61K31/497 , A61K31/5377 , C07D231/12 , C07D285/08 , C07D285/12 , C07D307/34 , C07D307/40 , C07D401/04 , C07D405/10 , C07D407/10 , C07D413/10 , C07D417/10 , Y02A50/465
摘要： Compounds that inhibit PDE10 are disclosed that have utility in the treatment of a variety of conditions, including (but not limited to) psychotic, anxiety, movement disorders and/or neurological disorders such as Parkinson's disease, Huntington's disease, Alzheimer's disease, encephalitis, phobias, epilepsy, aphasia, Bell's palsy, cerebral palsy, sleep disorders, pain, Tourette's syndrome, schizophrenia, delusional disorders, drug-induced psychosis and panic and obsessive-compulsive disorders. Pharmaceutically acceptable salts, stereoisomers, solvates and prodrugs of the compounds are also provided. Also disclosed are compositions containing a compound in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for inhibiting PDE10 in a warm-blooded animal in need of the same.

10. 发明申请

US20110224202A1 PDE10 INHIBITORS AND RELATED COMPOSITIONS AND METHODS 有权
标题翻译： PDE10抑制剂及相关组合物和方法
公开(公告)号：US20110224202A1
公开(公告)日：2011-09-15
申请号：US13045162
申请日：2011-03-10
申请人： Neil S. Cutshall , Jennifer Lynn Gage , Thomas Neil Wheeler , Thomas L. Little
发明人： Neil S. Cutshall , Jennifer Lynn Gage , Thomas Neil Wheeler , Thomas L. Little
IPC分类号： A61K31/5377 , C07D413/10 , C07D417/10 , A61K31/433 , A61K31/4245 , A61K31/422 , C07D241/10 , A61K31/4965 , C07D405/06 , A61K31/4433 , C07D405/10 , A61K31/41 , C07D401/10 , A61K31/4709 , A61K31/4155 , A61P25/00
CPC分类号： C07D307/46 , A61K31/341 , A61K31/415 , A61K31/4155 , A61K31/4192 , A61K31/4196 , A61K31/421 , A61K31/422 , A61K31/4245 , A61K31/427 , A61K31/433 , A61K31/454 , A61K31/4545 , A61K31/4709 , A61K31/497 , A61K31/5377 , C07D231/12 , C07D285/08 , C07D285/12 , C07D307/34 , C07D307/40 , C07D401/04 , C07D405/10 , C07D407/10 , C07D413/10 , C07D417/10 , Y02A50/465
摘要： Compounds that inhibit PDE10 are disclosed that have utility in the treatment of a variety of conditions, including (but not limited to) psychotic, anxiety, movement disorders and/or neurological disorders such as Parkinson's disease, Huntington's disease, Alzheimer's disease, encephalitis, phobias, epilepsy, aphasia, Bell's palsy, cerebral palsy, sleep disorders, pain, Tourette's syndrome, schizophrenia, delusional disorders, drug-induced psychosis and panic and obsessive-compulsive disorders. Pharmaceutically acceptable salts, stereoisomers, solvates and prodrugs of the compounds are also provided. Also disclosed are compositions containing a compound in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for inhibiting PDE10 in a warm-blooded animal in need of the same.
摘要翻译：公开了抑制PDE10的化合物，其可用于治疗各种病症，包括（但不限于）精神病性，焦虑症，运动障碍和/或神经障碍，例如帕金森病，亨廷顿氏病，阿尔茨海默病，脑炎，恐惧症，癫痫，失语症，贝尔麻痹，脑性麻痹，睡眠障碍，疼痛，图雷特综合征，精神分裂症，妄想症，药物诱发的精神病，恐慌和强迫症。还提供了化合物的药学上可接受的盐，立体异构体，溶剂合物和前药。还公开了含有与药学上可接受的载体组合的化合物的组合物，以及涉及其在需要其的温血动物中用于抑制PDE10的方法。

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