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公开(公告)号：US06632836B1
公开(公告)日：2003-10-14
申请号：US09422143
申请日：1999-10-21
申请人： Robert K. Baker , Jianming Bao , Jennifer Chee , Maria L. Garcia , Gregory J. Kaczorowski , Frank Kayser , Andrew Kotliar , Chou Juitsai Liu , Shouwu Miao , William H. Parsons , Kathleen M. Rupprecht , William A. Schmalhofer , Christopher F. Claiborne , David A. Claremon , Nigel Liverton , Wayne J. Thompson
发明人： Robert K. Baker , Jianming Bao , Jennifer Chee , Maria L. Garcia , Gregory J. Kaczorowski , Frank Kayser , Andrew Kotliar , Chou Juitsai Liu , Shouwu Miao , William H. Parsons , Kathleen M. Rupprecht , William A. Schmalhofer , Christopher F. Claiborne , David A. Claremon , Nigel Liverton , Wayne J. Thompson
IPC分类号： A61K3116
CPC分类号： C07D207/08 , C07B2200/07 , C07C235/60 , C07C237/22 , C07C255/46 , C07C271/12 , C07C271/34 , C07C271/38 , C07C271/56 , C07C275/26 , C07C309/66 , C07C309/67 , C07C309/73 , C07C311/05 , C07C311/07 , C07C311/20 , C07C333/06 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07C2601/16 , C07D209/14 , C07D213/643 , C07D233/64 , C07D263/28 , C07D307/14 , C07D307/79
摘要： The present invention relates to a class of carbocyclic compounds of Formula I that are useful as potassium channel inhibitors to treat autoimmune disorders, cardiac arrhythmias, and the like.
摘要翻译： 本发明涉及可用作治疗自身免疫性疾病，心律失常等的钾通道抑制剂的一类式I的碳环化合物。
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公开(公告)号：US07414067B2
公开(公告)日：2008-08-19
申请号：US10542169
申请日：2004-03-24
申请人： Edward Andrew Boyd , Michael H. Fisher , Maria L. Garcia , Gregory J. Kaczorowski , Peter T. Meinke , William H. Parsons , Stephen Price , John Stibbard
发明人： Edward Andrew Boyd , Michael H. Fisher , Maria L. Garcia , Gregory J. Kaczorowski , Peter T. Meinke , William H. Parsons , Stephen Price , John Stibbard
IPC分类号： A61K31/427 , A61K31/5377 , C07D277/20 , C07D403/02 , C07D413/02
CPC分类号： C07D405/12 , C07D209/28 , C07D401/12 , C07D413/12 , C07D417/12 , C07D417/14
摘要： This invention relates to the use of potent potassium channel blockers or a formulation thereof in the treatment of glaucoma and other conditions which leads to elevated intraoccular pressure in the eye of a patient. This invention also relates to the use of such compounds to provide a neuroprotective effect to the eye of mammalian species, particularly humans.
摘要翻译： 本发明涉及有效的钾通道阻滞剂或其制剂在治疗青光眼和导致患者眼睛中眼内压升高的其它病症中的用途。 本发明还涉及这些化合物对哺乳动物物种尤其是人的眼睛的神经保护作用的用途。
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公开(公告)号：US06914070B2
公开(公告)日：2005-07-05
申请号：US10361666
申请日：2003-02-10
IPC分类号： A61K9/08 , A61K9/10 , A61K31/404 , A61K31/4045 , A61K31/695 , A61K31/715 , A61K45/00 , A61K45/06 , A61K47/36 , A61P3/10 , A61P9/06 , A61P25/24 , A61P25/28 , A61P27/02 , A61P27/06 , C07D209/26 , A61K31/405
CPC分类号： A61K31/695 , A61K31/404 , A61K31/715 , A61K45/06 , Y10S514/912 , Y10S514/913 , A61K2300/00
摘要： This invention relates to the use of potent potassium channel blockers or a formulation thereof in the treatment of glaucoma and other conditions which leads to elevated intraoccular pressure in the eye of a patient. This invention also relates to the use of such compounds to provide a neuroprotective effect to the eye of mammalian species, particularly humans.
摘要翻译： 本发明涉及有效的钾通道阻滞剂或其制剂在治疗青光眼和导致患者眼睛中眼内压升高的其它病症中的用途。 本发明还涉及这些化合物对哺乳动物物种尤其是人的眼睛的神经保护作用的用途。
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4.发明授权公开(公告)号：US07294646B2
公开(公告)日：2007-11-13
申请号：US10511731
申请日：2003-06-13
申请人： Maria L. Garcia , Michael A. Goetz , Gregory J. Kaczorowski , Owen B. McManus , Richard L. Monaghan , William R. Strohl , Jan S. Tkacz
发明人： Maria L. Garcia , Michael A. Goetz , Gregory J. Kaczorowski , Owen B. McManus , Richard L. Monaghan , William R. Strohl , Jan S. Tkacz
IPC分类号： A61K31/40 , C07D487/00
CPC分类号： C07D491/20 , C12P17/18
摘要： This invention relates to the use of potent potassium channel blockers or a formulation thereof in the treatment of glaucoma and other conditions related to elevated intraocular pressure in the eye of a patient. This invention also relates to the use of such compounds to provide a neuroprotective effect to the eye of a mammalian species, particularly humans.
摘要翻译： 本发明涉及有效的钾通道阻滞剂或其制剂在治疗青光眼和与患者眼睛中升高的眼内压有关的其它病症中的用途。 本发明还涉及这些化合物对哺乳动物物种特别是人的眼睛的神经保护作用的用途。
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5.发明授权
公开(公告)号：US5776734A
公开(公告)日：1998-07-07
申请号：US732506
申请日：1996-11-12
申请人： Gregory J. Kaczorowski , Maria L. Garcia , Reid J. Leonard , Owen B. McManus , Richard J. Swanson , Kimberly L. Folander
发明人： Gregory J. Kaczorowski , Maria L. Garcia , Reid J. Leonard , Owen B. McManus , Richard J. Swanson , Kimberly L. Folander
IPC分类号： C12N15/09 , A61K38/00 , A61P9/00 , A61P9/08 , A61P9/10 , A61P13/02 , A61P15/00 , A61P21/02 , A61P25/04 , A61P29/00 , C07H21/04 , C07K14/47 , C07K14/705 , C07K16/18 , C12N1/19 , C12N5/10 , C12N15/12 , C12P21/02 , C12R1/865 , C12R1/91
CPC分类号： C07K14/705 , A61K38/00 , C12N2799/026
摘要： This invention relates to a heteromultimer and its use in screening pharmaceutically active compounds for modulators of maxi-K channel activity. Such modulators are useful in treating asthma, pregnant human myometrium, hypertension and angina, cerebral ischemia and in conditions where stimulation of neurotransmitter release is desired such as Alzheimer's disease and stimulation of damaged nerves.
摘要翻译： PCT No.PCT / US95 / 05768 Sec。 371日期：1996年11月12日 102（e）日期1996年11月12日PCT提交1995年5月9日PCT公布。 公开号WO95 / 31543 日期1995年11月23日本发明涉及异源多聚体及其用于筛选药物活性化合物用于maxi-K通道活性调节剂的用途。 这种调节剂可用于治疗哮喘，怀孕的人肌层，高血压和心绞痛，脑缺血以及需要刺激神经递质释放的疾病如阿尔茨海默病和刺激受损的神经。
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公开(公告)号：US06924306B2
公开(公告)日：2005-08-02
申请号：US10361346
申请日：2003-02-10
IPC分类号： A61K31/40 , A61K31/407 , A61K31/42 , A61K31/335 , A61K31/35
CPC分类号： A61K31/42 , A61K31/40 , A61K31/407 , Y10S514/912 , Y10S514/913 , A61K2300/00
摘要： This invention relates to the use of potent potassium channel blockers or a formulation thereof in the treatment of glaucoma and other conditions related to elevated intraoccular pressure in the eye of a patient. This invention also relates to the use of such compounds to provide a neuroprotective effect to the eye of a mammalian species, particularly humans.
摘要翻译： 本发明涉及有效的钾通道阻滞剂或其制剂用于治疗青光眼和与患者眼睛中升高的眼内压有关的其它病症的用途。 本发明还涉及这些化合物对哺乳动物物种特别是人的眼睛的神经保护作用的用途。
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公开(公告)号：US06548535B2
公开(公告)日：2003-04-15
申请号：US09765716
申请日：2001-01-17
IPC分类号： A61K31335
CPC分类号： A61K31/42 , A61K31/40 , A61K31/407 , Y10S514/912 , Y10S514/913 , A61K2300/00
摘要： This invention relates to the use of potent potassium channel blockers or a formulation thereof in the treatment of glaucoma and other conditions related to elevated intraoccular pressure in the eye of a patient. This invention also relates to the use of such compounds to provide a neuroprotective effect to the eye of a mammalian species, particularly humans.
摘要翻译： 本发明涉及有效的钾通道阻滞剂或其制剂用于治疗青光眼和与患者眼睛中升高的眼内压有关的其它病症的用途。 本发明还涉及这些化合物对哺乳动物物种特别是人的眼睛的神经保护作用的用途。
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公开(公告)号：US06864383B2
公开(公告)日：2005-03-08
申请号：US10466878
申请日：2002-01-25
IPC分类号： A61K47/36 , A61K31/21 , A61K31/265 , A61K31/4178 , A61K31/5377 , A61K45/00 , A61P3/10 , A61P9/06 , A61P25/24 , A61P25/28 , A61P27/06 , A61P43/00 , C07C327/08 , C07C327/32 , C07C329/06
CPC分类号： C07C327/32
摘要： This invention relates to the use of potent potassium channel blockers or a formulation thereof in the treatment of glaucoma and other conditions which leads to elevated intraoccular pressure in the eye of a patient. This invention also relates to the use of such compounds to provide a neuroprotective effect to the eye of mammalian species, particularly humans.
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公开(公告)号：US06545036B2
公开(公告)日：2003-04-08
申请号：US09764738
申请日：2001-01-17
IPC分类号： A61K31405
CPC分类号： A61K31/695 , A61K31/404 , A61K31/715 , A61K45/06 , Y10S514/912 , Y10S514/913 , A61K2300/00
摘要： This invention relates to the use of potent potassium channel blockers or a formulation thereof in the treatment of glaucoma and other conditions which leads to elevated intraoccular pressure in the eye of a patient. This invention also relates to the use of such compounds to provide a neuroprotective effect to the eye of mammalian species, particularly humans.
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10.发明授权Screening array using cells expressing recombinant .alpha. and .beta. subunits of the mammalian large-conductance (maxi-K) potassium channel 失效筛选阵列使用表达哺乳动物大电导（maxi-K）钾通道的重组α和β亚基的细胞
公开(公告)号：US5637470A
公开(公告)日：1997-06-10
申请号：US389668
申请日：1995-02-16
申请人： Gregory J. Kaczorowski , Maria L. Garcia , Reid J. Leonard , Owen B. McManus , Richard J. Swanson , Kimberly L. Folander
发明人： Gregory J. Kaczorowski , Maria L. Garcia , Reid J. Leonard , Owen B. McManus , Richard J. Swanson , Kimberly L. Folander
IPC分类号： C12N15/09 , A61K38/00 , A61P9/00 , A61P9/08 , A61P9/10 , A61P13/02 , A61P15/00 , A61P21/02 , A61P25/04 , A61P29/00 , C07H21/04 , C07K14/47 , C07K14/705 , C07K16/18 , C12N1/19 , C12N5/10 , C12N15/12 , C12P21/02 , C12R1/865 , C12R1/91 , G01N33/50
CPC分类号： C07K14/705 , A61K38/00 , C12N2799/026
摘要： Disclosed are nucleic acids encoding the .beta. subunit of the mammalian large-conductance ("maxi-K") potassium channel, cells transformed with such nucleic acids, and .beta. subunit proteins produced by the transformed cells. Within the invention are recombinant host cells expressing .alpha..beta. heteromultimers. Such cells or preparations made from them may be used to screen for pharmacologically active modulators of maxi-K channel activity. Such modulators are potentially useful in treating asthma, pregnant human myometrium, hypertension and angina, cerebral ischemia, and conditions where stimulation of neurotransmitter release is desired, such as in Alzheimer's disease and stimulation of damaged nerves.
摘要翻译： 公开了编码哺乳动物大电导（“maxi-K”）钾通道的β亚单位，用这种核酸转化的细胞和由转化细胞产生的β亚基蛋白的核酸。 在本发明内是表达αβ异复合体的重组宿主细胞。 这些由其制备的细胞或制剂可用于筛选具有maxi-K通道活性的药理活性调节剂。 这种调节剂可能用于治疗哮喘，怀孕的人类子宫肌层，高血压和心绞痛，脑缺血以及需要刺激神经递质释放的疾病，例如阿尔茨海默病和刺激受损神经。
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