公开(公告)号：US20090062290A1

公开(公告)日：2009-03-05

申请号：US12193639

申请日：2008-08-18

申请人： Thomas Eugene Christos ,  George S. Amato ,  Robert N. Atkinson ,  Maria Graciela Barolli ,  Lilli Wolf-Gouveia ,  Mark J. Suto

发明人： Thomas Eugene Christos ,  George S. Amato ,  Robert N. Atkinson ,  Maria Graciela Barolli ,  Lilli Wolf-Gouveia ,  Mark J. Suto

IPC分类号： A61K31/5025 ,  A61K31/437 ,  C07D471/04 ,  A61K31/519 ,  C12N5/06 ,  A61P25/28 ,  C07D487/04

CPC分类号： C07D471/04 ,  C07D487/04

摘要： Compounds, compositions and methods are provided which are useful in the treatment of diseases through the modulation of potassium ion flux through voltage-dependent potassium channels. More particularly, the invention provides heterocycles, compositions and methods that are useful in the treatment of central or peripheral nervous system disorders (e.g., migraine, ataxia, Parkinson's disease, bipolar disorders, trigeminal neuralgia, spasticity, mood disorders, brain tumors, psychotic disorders, myokymia, seizures, epilepsy, seizure, retinal degeneration, hearing and vision loss, Alzheimer's disease, age-related memory loss, learning deficiencies, anxiety, neuronal degeneration and motor neuron diseases, maintaining bladder control or treating urinary incontinence) and as neuroprotective agents (e.g., to prevent stroke and the like) by modulating potassium channels associated with the onset or recurrence of the indicated conditions.

摘要翻译： 提供了通过电压依赖钾通道调节钾离子通量可用于治疗疾病的化合物，组合物和方法。 更具体地说，本发明提供了可用于治疗中枢性或周围神经系统疾病（例如偏头痛，共济失调，帕金森病，双相情感障碍，三叉神经痛，痉挛状态，情绪障碍，脑肿瘤，精神病症）的杂环，组合物和方法 ，癫痫，癫痫，癫痫，癫痫发作，视网膜变性，听力和视力丧失，阿尔茨海默病，年龄相关记忆丧失，学习缺陷，焦虑，神经元变性和运动神经元疾病，维持膀胱控制或治疗尿失禁）和神经保护剂 （例如，为了预防中风等）通过调节与指示的病症的发作或复发相关的钾通道。

公开(公告)号：US08058274B2

公开(公告)日：2011-11-15

申请号：US12193639

申请日：2008-08-18

申请人： Thomas Eugene Christos ,  George S. Amato ,  Robert N. Atkinson ,  Maria Graciela Barolli ,  Lilli Ann Wolf-Gouveia ,  Mark J. Suto

发明人： Thomas Eugene Christos ,  George S. Amato ,  Robert N. Atkinson ,  Maria Graciela Barolli ,  Lilli Ann Wolf-Gouveia ,  Mark J. Suto

IPC分类号： A01N43/58 ,  A01N43/60 ,  A61K31/50 ,  A61K31/495 ,  C07D487/00

CPC分类号： C07D471/04 ,  C07D487/04

摘要： Compounds, compositions and methods are provided which are useful in the treatment of diseases through the modulation of potassium ion flux through voltage-dependent potassium channels. More particularly, the invention provides heterocycles, compositions and methods that are useful in the treatment of central or peripheral nervous system disorders (e.g., migraine, ataxia, Parkinson's disease, bipolar disorders, trigeminal neuralgia, spasticity, mood disorders, brain tumors, psychotic disorders, myokymia, seizures, epilepsy, seizure, retinal degeneration, hearing and vision loss, Alzheimer's disease, age-related memory loss, learning deficiencies, anxiety, neuronal degeneration and motor neuron diseases, maintaining bladder control or treating urinary incontinence) and as neuroprotective agents (e.g., to prevent stroke and the like) by modulating potassium channels associated with the onset or recurrence of the indicated conditions.

摘要翻译： 提供了通过电压依赖钾通道调节钾离子通量可用于治疗疾病的化合物，组合物和方法。 更具体地说，本发明提供了可用于治疗中枢性或周围神经系统疾病（例如偏头痛，共济失调，帕金森病，双相情感障碍，三叉神经痛，痉挛状态，情绪障碍，脑肿瘤，精神病症）的杂环，组合物和方法 ，癫痫，癫痫，癫痫，癫痫发作，视网膜变性，听力和视力丧失，阿尔茨海默病，年龄相关记忆丧失，学习缺陷，焦虑，神经元变性和运动神经元疾病，维持膀胱控制或治疗尿失禁）和神经保护剂 （例如，为了预防中风等）通过调节与指示的病症的发作或复发相关的钾通道。

公开(公告)号：US08431608B2

公开(公告)日：2013-04-30

申请号：US12706574

申请日：2010-02-16

申请人： Thomas Eugene Christos ,  George S. Amato ,  Robert N. Atkinson ,  Maria Graciela Barolli ,  Lilli Ann Wolf-Gouveia ,  Mark J. Suto

发明人： Thomas Eugene Christos ,  George S. Amato ,  Robert N. Atkinson ,  Maria Graciela Barolli ,  Lilli Ann Wolf-Gouveia ,  Mark J. Suto

IPC分类号： A61K31/4188 ,  C07D235/00

CPC分类号： C07D487/04 ,  A61K31/5025 ,  C07D471/04

摘要： Compounds, compositions and methods are provided which are useful in the treatment of diseases through the modulation of potassium ion flux through voltage-dependent potassium channels. More particularly, the invention provides heterocycles, compositions and methods that are useful in the treatment of central or peripheral nervous system disorders (e.g., migraine, ataxia, Parkinson's disease, bipolar disorders, trigeminal neuralgia, spasticity, mood disorders, brain tumors, psychotic disorders, myokymia, seizures, epilepsy, seizure, retinal degeneration, hearing and vision loss, Alzheimer's disease, age-related memory loss, learning deficiencies, anxiety, neuronal degeneration and motor neuron diseases, maintaining bladder control or treating urinary incontinence) and as neuroprotective agents (e.g., to prevent stroke and the like) by modulating potassium channels associated with the onset or recurrence of the indicated conditions.

摘要翻译： 提供了通过电压依赖钾通道调节钾离子通量可用于治疗疾病的化合物，组合物和方法。 更具体地说，本发明提供了可用于治疗中枢性或周围神经系统疾病（例如偏头痛，共济失调，帕金森病，双相情感障碍，三叉神经痛，痉挛状态，情绪障碍，脑肿瘤，精神病症）的杂环，组合物和方法 ，癫痫，癫痫，癫痫，癫痫发作，视网膜变性，听力和视力丧失，阿尔茨海默病，年龄相关记忆丧失，学习缺陷，焦虑，神经元变性和运动神经元疾病，维持膀胱控制或治疗尿失禁）和神经保护剂 （例如，为了预防中风等）通过调节与指示的病症的发作或复发相关的钾通道。

公开(公告)号：US20100240663A1

公开(公告)日：2010-09-23

申请号：US12706574

申请日：2010-02-16

申请人： Thomas Eugene Christos ,  George S. Amato ,  Robert N. Atkinson ,  Maria Graciela Barolli ,  Lilli Ann Wolf-Gouveia ,  Mark J. Suto

发明人： Thomas Eugene Christos ,  George S. Amato ,  Robert N. Atkinson ,  Maria Graciela Barolli ,  Lilli Ann Wolf-Gouveia ,  Mark J. Suto

IPC分类号： A61K31/5025 ,  C07D471/04 ,  A61K31/437 ,  C07D487/04 ,  A61P25/28 ,  A61P25/16 ,  A61P25/22 ,  A61P25/18 ,  A61P25/08 ,  A61P27/00 ,  C12N5/02

CPC分类号： C07D487/04 ,  A61K31/5025 ,  C07D471/04

摘要： Compounds, compositions and methods are provided which are useful in the treatment of diseases through the modulation of potassium ion flux through voltage-dependent potassium channels. More particularly, the invention provides heterocycles, compositions and methods that are useful in the treatment of central or peripheral nervous system disorders (e.g., migraine, ataxia, Parkinson's disease, bipolar disorders, trigeminal neuralgia, spasticity, mood disorders, brain tumors, psychotic disorders, myokymia, seizures, epilepsy, seizure, retinal degeneration, hearing and vision loss, Alzheimer's disease, age-related memory loss, learning deficiencies, anxiety, neuronal degeneration and motor neuron diseases, maintaining bladder control or treating urinary incontinence) and as neuroprotective agents (e.g., to prevent stroke and the like) by modulating potassium channels associated with the onset or recurrence of the indicated conditions.

摘要翻译： 提供了通过电压依赖钾通道调节钾离子通量可用于治疗疾病的化合物，组合物和方法。 更具体地说，本发明提供了可用于治疗中枢性或周围神经系统疾病（例如偏头痛，共济失调，帕金森病，双相情感障碍，三叉神经痛，痉挛状态，情绪障碍，脑肿瘤，精神病症）的杂环，组合物和方法 ，癫痫，癫痫，癫痫，癫痫发作，视网膜变性，听力和视力丧失，阿尔茨海默病，年龄相关记忆丧失，学习缺陷，焦虑，神经元变性和运动神经元疾病，维持膀胱控制或治疗尿失禁）和神经保护剂 （例如，为了预防中风等）通过调节与指示的病症的发作或复发相关的钾通道。

公开(公告)号：US06342503B1

公开(公告)日：2002-01-29

申请号：US09004150

申请日：1998-01-07

申请人： Paul Edward Aldrich ,  Argyrios Georgios Arvanitis ,  Robert Scott Cheeseman ,  Robert John Chorvat ,  Thomas Eugene Christos ,  Paul Joseph Gilligan ,  Dimitri Emil Grigoriadis ,  Carl Nicholas Hodge ,  Paul John Krenitsky ,  Everett Latham Scholfield ,  Sang William Tam ,  Zelda Rakowitz Wasserman

发明人： Paul Edward Aldrich ,  Argyrios Georgios Arvanitis ,  Robert Scott Cheeseman ,  Robert John Chorvat ,  Thomas Eugene Christos ,  Paul Joseph Gilligan ,  Dimitri Emil Grigoriadis ,  Carl Nicholas Hodge ,  Paul John Krenitsky ,  Everett Latham Scholfield ,  Sang William Tam ,  Zelda Rakowitz Wasserman

IPC分类号： C07D23942

CPC分类号： C07D213/74 ,  A61K31/44 ,  A61K31/505 ,  A61K31/53 ,  A61K31/535 ,  C07D239/42 ,  C07D239/48 ,  C07D251/18 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D403/04 ,  C07D403/06 ,  C07D403/12 ,  C07D405/12 ,  C07D409/04 ,  C07D409/12 ,  C07D417/04 ,  C07D417/12 ,  C07D471/04 ,  C07D473/34 ,  C07D473/40 ,  C07D487/04

摘要： The present invention provides novel compounds, compounds and pharmaceutical compositions thereof, and methods of using same in the treatment of affective disorders, anxiety, depression, post-traumatic stress disorders, eating disorders, supranuclear palsy, irritable bowel syndrome, immune suppression, Alzheimer'disease, gastrointestinal diseases, anorexia nervosa, drug and alcohol withdrawal symptoms, drug addiction, inflammatory disorders, or fertility problems. The novel compounds provided by this invention are those of formula: wherein R1, R3, R4, R5, Z, Y, V, X, X′, J, K, L, and M are as defined herein.

摘要翻译： 本发明提供了新的化合物，其化合物及其药物组合物及其在治疗情感障碍，焦虑，抑郁，创伤后应激障碍，进食障碍，核核后麻痹，肠易激综合征，免疫抑制，阿尔茨海默病 疾病，胃肠道疾病，神经性厌食症，药物和酒精戒断症状，​​药物成瘾，炎性疾病或生殖问题。 本发明提供的新化合物是下式的化合物：其中R1，R3，R4，R5，Z，Y，V，X，X'，J，K，L和M如本文所定义。