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公开(公告)号：US5541208A
公开(公告)日：1996-07-30
申请号：US186197
申请日：1994-01-24
申请人： Maria L. Garcia , Robert A. Giacobbe , Otto D. Hensens , Seok H. Lee , Owen B. McManus , Deborah L. Zink
发明人： Maria L. Garcia , Robert A. Giacobbe , Otto D. Hensens , Seok H. Lee , Owen B. McManus , Deborah L. Zink
IPC分类号： A61K31/40 , A61K45/06 , A61P25/28 , A61P43/00 , C07D491/04 , C07D491/052 , C07D491/14 , C07D491/20 , C07D491/22 , C07D498/14 , C12P17/10 , C12P17/18 , C12R1/645 , A61K31/41 , A61K31/395 , C07D498/22
CPC分类号： C07D491/04 , C07D491/14 , C12P17/10 , C12P17/18
摘要： The present invention relates to compounds of the formula: ##STR1## and the pharmaceutically acceptable salts thereof which are useful as potassium channel antagonists, particularly Maxi-K channel antagonists, and thus useful in treating Alzheimer's Disease and other cognitive disorders. This invention is also related to a method of making the compound of formula (I).
摘要翻译： 本发明涉及下式的化合物及其药学上可接受的盐，其可用作钾通道拮抗剂，特别是Maxi-K通道拮抗剂，因此可用于治疗阿尔茨海默病和其他认知障碍。 本发明还涉及制备式（I）化合物的方法。
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公开(公告)号：US5399587A
公开(公告)日：1995-03-21
申请号：US166499
申请日：1993-12-13
申请人： Maria L. Garcia , Robert A. Giacobbe , Otto D. Hensens , Gregory J. Kaczorowski , Seok H. Lee , Owen B. McManus , Deborah L. Zink
发明人： Maria L. Garcia , Robert A. Giacobbe , Otto D. Hensens , Gregory J. Kaczorowski , Seok H. Lee , Owen B. McManus , Deborah L. Zink
IPC分类号： C12N1/14 , A61K31/045 , A61K31/23 , A61P1/00 , A61P9/08 , A61P9/12 , A61P11/00 , A61P13/02 , A61P15/00 , A61P43/00 , C07C35/34 , C07C43/18 , C07C43/188 , C07C43/196 , C07C69/007 , C07C69/013 , C07C69/30 , C07C69/52 , C07F7/08 , C12P7/02 , C12P7/62 , A01K31/35
CPC分类号： C07C69/013 , C07C69/007 , C12P7/02 , C12P7/62
摘要： The present invention relates to novel potassium channel agonists which are useful in activating the calcium activated Maxi-K potassium channel in mammalian neuronal and smooth muscle tissue. The claimed compounds are of the general formula: ##STR1## In addition, a novel microbiological process for producing the claimed compounds is described.
摘要翻译： 本发明涉及可用于激活哺乳动物神经元和平滑肌组织中钙激活的Maxi-K钾通道的新型钾通道激动剂。 要求保护的化合物具有以下通式：此外，描述了用于生产所要求保护的化合物的新型微生物方法。
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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：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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9.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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公开(公告)号：US20100184094A1
公开(公告)日：2010-07-22
申请号：US12665110
申请日：2008-06-25
CPC分类号： G01N33/5044 , G01N33/56966 , G01N33/92
摘要： A novel use for MDCK cells in the evaluation of cholesterol modulators is provided. In particular, methods for detecting substances which bind to NPC1L1 and block intestinal cholesterol absorption are provided. Such substances are of use in the treatment of individuals with hypercholesterolemia. The various assays may additionally be employed for studying NPC1L1 function.
摘要翻译： 提供了一种MDCK细胞在胆固醇调节剂评估中的新用途。 特别地，提供了检测结合NPC1L1的物质并阻断肠胆固醇吸收的方法。 这些物质可用于治疗高胆固醇血症个体。 可以另外使用各种测定来研究NPC1L1功能。
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