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1. 发明授权

US08871767B2 2-arylimidazo[1,2-B]pyridazine, 2-phenylimidazo[1,2-A]pyridine, and 2-phenylimidazo[1,2-A]pyrazine derivatives 有权
标题翻译： 2-芳基咪唑并[1,2-B]哒嗪，2-苯基咪唑并[1,2-A]吡啶和2-苯基咪唑并[1,2-A]吡嗪衍生物
公开(公告)号：US08871767B2
公开(公告)日：2014-10-28
申请号：US13335072
申请日：2011-12-22
申请人： Robert N. Atkinson , Andy J. Ommen , James M. Veal , Kenneth H. Huang , Emilie D. Smith
发明人： Robert N. Atkinson , Andy J. Ommen , James M. Veal , Kenneth H. Huang , Emilie D. Smith
IPC分类号： A61K31/50 , C07D487/00
CPC分类号： C07D471/04 , C07D487/04
摘要： Disclosed are compounds of formula (I): where X, Y, X, A, R1, R2, and R3 are defined herein. Also disclosed are pharmaceutically acceptable salts of the compounds, compositions containing the compounds, and methods of using the compounds to treat, e.g., cancer.
摘要翻译：公开了式（I）的化合物：其中X，Y，X，A，R 1，R 2和R 3在本文中定义。还公开了化合物的药学上可接受的盐，含有该化合物的组合物，以及使用该化合物治疗例如癌症的方法。

2. 发明申请

US20120178751A1 2-ARYLIMIDAZO[1,2-B]PYRIDAZINE, 2-PHENYLIMIDAZO[1,2-A]PYRIDINE, AND 2-PHENYLIMIDAZO[1,2-A]PYRAZINE DERIVATIVES 有权
标题翻译： 2-氨基咪唑并[1,2-B]吡啶，2-苯基咪唑并[1,2-A]吡啶和2-苯基咪唑并[1,2-A]吡嗪衍生物
公开(公告)号：US20120178751A1
公开(公告)日：2012-07-12
申请号：US13335072
申请日：2011-12-22
申请人： Robert N. Atkinson , Andy J. Ommen , James M. Veal , Kenneth H. Huang , Emilie D. Smith
发明人： Robert N. Atkinson , Andy J. Ommen , James M. Veal , Kenneth H. Huang , Emilie D. Smith
IPC分类号： A61K31/5025 , A61K31/5377 , C07D471/04 , C12N5/02 , A61K31/519 , A61K31/4985 , A61P35/00 , C07D487/04 , A61K31/437
CPC分类号： C07D471/04 , C07D487/04
摘要： Disclosed are compounds of formula (I): where X, Y, X, A, R1, R2, and R3 are defined herein. Also disclosed are pharmaceutically acceptable salts of the compounds, compositions containing the compounds, and methods of using the compounds to treat, e.g., cancer.
摘要翻译：公开了式（I）的化合物：其中X，Y，X，A，R 1，R 2和R 3在本文中定义。还公开了化合物的药学上可接受的盐，含有该化合物的组合物，以及使用该化合物治疗例如癌症的方法。

3. 发明申请

US20130085157A1 ARYLSUBSTITUTED THIAZOLOTRIAZOLES AND THIAZOLOIMIDAZOLES 审中-公开
标题翻译：三唑并吡唑并噻唑烷酮
公开(公告)号：US20130085157A1
公开(公告)日：2013-04-04
申请号：US13630946
申请日：2012-09-28
申请人： Emilie D. Smith , Mark E. Fitzgerald , Rong Jiang , Robert N. Atkinson , James M. Veal , Kenneth H. Huang
发明人： Emilie D. Smith , Mark E. Fitzgerald , Rong Jiang , Robert N. Atkinson , James M. Veal , Kenneth H. Huang
IPC分类号： A61K31/429 , A61K31/4725 , A61P9/10 , C07D513/04
CPC分类号： C07D513/04
摘要： This disclosure relates to compounds, compositions and methods for the treatment of various disorders. In particular, the disclosure relates to thiazolotriazole and thiazoloimidazole compounds which agonize the activity of the protein TGR5.
摘要翻译：本公开涉及用于治疗各种疾病的化合物，组合物和方法。特别地，本公开涉及激活蛋白TGR5的活性的噻唑三唑和噻唑并咪唑化合物。

4. 发明申请

US20120077814A1 SULFONAMIDE, SULFAMATE, AND SULFAMOTHIOATE DERIVATIVES 审中-公开
标题翻译：磺酰胺，磺酰胺和硫代烟酸衍生物
公开(公告)号：US20120077814A1
公开(公告)日：2012-03-29
申请号：US13230443
申请日：2011-09-12
申请人： Zhong Wang , Emilie D. Smith , James M. Veal , Kenneth H. Huang , Robert N. Atkinson , Rong Jiang
发明人： Zhong Wang , Emilie D. Smith , James M. Veal , Kenneth H. Huang , Robert N. Atkinson , Rong Jiang
IPC分类号： A61K31/53 , A61K31/519 , A61P25/28 , A61P35/00 , A61P29/00 , C07D487/04 , C07D495/04
CPC分类号： C07D487/04 , A61K31/519 , A61K31/53 , C07D491/048 , C07D495/04
摘要： The disclosure provides biologically active compounds of formula (I): and pharmaceutically acceptable salts thereof, compositions containing these compounds, and methods of using these compounds in a variety applications, such as treatment of diseases or disorders associated with E1 type activating enzymes, and with Nedd8 activating enzyme (NAE) in particular.
摘要翻译：本公开提供了式（I）的生物活性化合物及其药学上可接受的盐，含有这些化合物的组合物，以及在各种应用中使用这些化合物的方法，例如治疗与E1型活化酶相关的疾病或病症，以及与特别是Nedd8活化酶（NAE）。

5. 发明授权

US07098335B2 Pyrazolopyrimidine compositions 失效
标题翻译：吡唑并嘧啶组合物
公开(公告)号：US07098335B2
公开(公告)日：2006-08-29
申请号：US10987089
申请日：2004-11-12
申请人： Robert N. Atkinson , Michael F. Gross , Albert M. van Rhee
发明人： Robert N. Atkinson , Michael F. Gross , Albert M. van Rhee
IPC分类号： C07D487/00 , A61K31/519
CPC分类号： C07D487/04 , A61K31/519
摘要： Compounds, compositions and methods are provided which are useful in the treatment of diseases through the inhibition of sodium ion flux through voltage-dependent sodium channels. More particularly, the invention provides pyrazolopyrimidines, compositions and methods that are useful in the treatment of central or peripheral nervous system disorders, particularly pain and chronic pain by blocking sodium channels associated with the onset or recurrance of the indicated conditions. The compounds, compositions and methods of the present invention are of particular use for treating neuropathic or inflammatory pain by the inhibition of ion flux through a channel that includes a PN3 subunit.
摘要翻译：提供的化合物，组合物和方法可用于通过电压依赖性钠通道抑制钠离子通量来治疗疾病。更具体地，本发明提供了可用于治疗中枢或周围神经系统疾病，特别是疼痛和慢性疼痛的吡唑并嘧啶类，组合物和方法，其通过阻断与所述病症的发作或复发有关的钠通道。本发明的化合物，组合物和方法特别用于通过包含PN3亚基的通道抑制离子通量来治疗神经性或炎性疼痛。

6. 发明授权

US07119112B2 Sulfonamides as potassium channel blockers 失效
公开(公告)号：US07119112B2
公开(公告)日：2006-10-10
申请号：US10641686
申请日：2003-08-14
申请人： Grant A. McNaughton-Smith , Aimee D. Reed , Robert N. Atkinson
发明人： Grant A. McNaughton-Smith , Aimee D. Reed , Robert N. Atkinson
IPC分类号： A61K31/425 , C07D275/02
CPC分类号： C07D271/06 , A61K9/0048 , A61K31/165 , A61K45/06 , C07C311/20 , C07C317/44 , C07C323/56 , C07C2601/16 , C07D263/32 , C07D307/52 , C07D333/70
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 sulfonamides, and compositions and methods utilizing sulfonamides that are useful in the treatment of diseases by blocking potassium channels associated with the onset or recurrence of the indicated conditions. Exemplary diseases treatable with the compounds, compositions and methods of the invention include sickle cell disease and glaucoma.

7. 发明申请

US20090062290A1 HETEROCYCLES AS POTASSIUM CHANNEL MODULATORS 有权
标题翻译：杂质作为钾通道调节剂
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。

8. 发明授权

US06833371B2 Pyrazolopyrimidines 失效
标题翻译：吡唑并嘧啶
公开(公告)号：US06833371B2
公开(公告)日：2004-12-21
申请号：US10286687
申请日：2002-11-01
申请人： Robert N. Atkinson , Michael F. Gross , Albert M. van Rhee
发明人： Robert N. Atkinson , Michael F. Gross , Albert M. van Rhee
IPC分类号： A61K31519
CPC分类号： C07D487/04 , A61K31/519
摘要： Compounds, compositions and methods are provided which are useful in the treatment of diseases through the inhibition of sodium ion flux through voltage-dependent sodium channels. More particularly, the invention provides pyrazolopyrimidines, compositions and methods that are useful in the treatment of central or peripheral nervous system disorders, particularly pain and chronic pain by blocking sodium channels associated with the onset or recurrance of the indicated conditions. The compounds, compositions and methods of the present invention are of particular use for treating neuropathic or inflammatory pain by the inhibition of ion flux through a channel that includes a PN3 subunit.
摘要翻译：提供的化合物，组合物和方法可用于通过电压依赖性钠通道抑制钠离子通量来治疗疾病。更具体地，本发明提供了可用于治疗中枢或周围神经系统疾病，特别是疼痛和慢性疼痛的吡唑并嘧啶类，组合物和方法，其通过阻断与所述病症的发作或复发有关的钠通道。本发明的化合物，组合物和方法特别用于通过包含PN3亚基的通道抑制离子通量来治疗神经性或炎性疼痛。

9. 发明授权

US08058274B2 Heterocycles as potassium channel modulators 有权
标题翻译：杂环作为钾通道调节剂
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。

10. 发明授权

US08431608B2 Heterocycles as potassium channel modulators 失效
标题翻译：杂环作为钾通道调节剂
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。

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