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1. 发明授权

US5677327A Method for identifying muscarinic agents lacking miotic side effects 失效
标题翻译：识别缺乏瞳孔副作用的毒蕈碱药的方法
公开(公告)号：US5677327A
公开(公告)日：1997-10-14
申请号：US493509
申请日：1995-06-22
申请人： Daniel W. Gil , Elizabeth Woldemussie
发明人： Daniel W. Gil , Elizabeth Woldemussie
IPC分类号： G01N33/50 , G01N33/94 , A61K31/415
CPC分类号： G01N33/5044 , G01N33/5008 , G01N33/502 , G01N33/5088 , G01N33/944 , G01N2500/10 , Y10S514/913
摘要： The present invention provides a method for identifying a compound having muscarinic agonist activity that will lower intraocular pressure without causing miosis which comprises measuring the activity of the compound at the m.sub.3 and m.sub.5 muscarinic receptors and determining from the activity measurement a compound having at least twice the agonist activity at the m.sub.5 receptor as compared to the m.sub.3 receptor. Preferably, the method of measuring said muscarinic agonist activity comprises eliciting phosphoinositide hydrolysis in CHO-K1 cells stably expressing the m.sub.3 and m.sub.5 muscarinic receptor subtypes. The present invention also provides a method of lowering the intraocular pressure in a mammal which comprises administering to said mammal a compound that has been determined to have at least twice the agonist activity at the m.sub.5 receptor as compared to the m.sub.3 receptor.
摘要翻译：本发明提供了一种用于鉴定具有毒蕈碱激动剂活性的化合物的方法，其将降低眼内压而不引起瞳孔缩小，其包括测量化合物在m3和m5毒蕈碱受体的活性，并从活性测定确定具有至少两倍与m3受体相比，m5受体的激动剂活性。优选地，测量所述毒蕈碱激动剂活性的方法包括在稳定表达m3和m5毒蕈碱受体亚型的CHO-K1细胞中引发磷酸肌醇水解。本发明还提供一种降低哺乳动物眼内压的方法，其包括向所述哺乳动物施用与m 3受体相比被确定具有m5受体的激动剂活性至少两倍的化合物。

2. 发明授权

US5559151A Method for reducing intraocular pressure in the mammalian eye by administration of chloride channel blockers 失效
标题翻译：通过施用氯化物通道阻断剂降低哺乳动物眼睛眼内压的方法
公开(公告)号：US5559151A
公开(公告)日：1996-09-24
申请号：US346660
申请日：1994-11-30
申请人： Joseph S. Adorante , Elizabeth WoldeMussie , Guadalupe Ruiz
发明人： Joseph S. Adorante , Elizabeth WoldeMussie , Guadalupe Ruiz
IPC分类号： A61K45/00 , A61K31/00 , A61K31/137 , A61K31/192 , A61K31/195 , A61K31/196 , A61K31/24 , A61K31/245 , A61K31/26 , A61P27/02 , A61P27/06
CPC分类号： A61K31/00 , A61K31/137 , A61K31/192 , A61K31/196 , A61K31/26 , Y10S514/912 , Y10S514/913
摘要： Pharmaceutical compositions and a method are disclosed for treating glaucoma and/or ocular hypertension in the mammalian eye by administering to the mammalian eye the pharmaceutical composition of the invention which contains, as the active ingredient, one or more compounds having chloride channel blocking activity. Examples of chloride channel blockers utilized in the pharmaceutical composition and method of treatment are: ##STR1## wherein R is hydrogen or a pharmaceutically-acceptable cation, e.g. an alkali or alkaline earth metal, or a quaternary amine; or R represents a ester-forming moiety, e.g. a lower alkyl radical, having up to six carbon atoms, that may be derived from a lower alkanol.
摘要翻译：公开了用于治疗哺乳动物眼中的青光眼和/或高眼压症的药物组合物和方法，其通过向哺乳动物眼睛施用本发明的药物组合物，其含有一种或多种具有氯通道阻断活性的化合物作为活性成分。在药物组合物和治疗方法中使用的氯化物通道阻断剂的实例是：其中R是氢或药学上可接受的阳离子，例如，碱金属或碱土金属或季胺; 或R表示酯形成部分，例如。具有至多6个碳原子的低级烷基，其可以衍生自低级链烷醇。

3. 发明授权

US08541426B2 Pharmaceutical compositions and methods of treating dry eye disorders 有权
标题翻译：治疗干眼症的药物组合物和方法
公开(公告)号：US08541426B2
公开(公告)日：2013-09-24
申请号：US12668604
申请日：2008-07-04
申请人： Channing R. Beals , Elizabeth WoldeMussie , Hovhannes John Gukasyan , Jingwen Ma
发明人： Channing R. Beals , Elizabeth WoldeMussie , Hovhannes John Gukasyan , Jingwen Ma
IPC分类号： A61K31/519
CPC分类号： A61K31/519 , A61K9/0048
摘要： Inhibitors of Janus kinase-3 (“Jak3”) are useful for treating dry eye disorders and other disorders requiring the wetting of the eye. Jak3 inhibitors useful for treating eye disorders include the compound 3-{(3R,4R)-4-Methyl-3-[methyl-(7H-pyrrolo [2,3-d]pyrimidin-4-yl)-amino]-piperidin-1-yl}-3-oxo-propionitrile.
摘要翻译： Janus激酶-3（“Jak3”）的抑制剂可用于治疗干眼病和其它需要润湿眼睛的疾病。用于治疗眼睛疾病的Jak3抑制剂包括化合物3 - {（3R，4R）-4-甲基-3- [甲基 - （7H-吡咯并[2,3-d]嘧啶-4-基） - 氨基] - 哌啶 -1-基} -3-氧代 - 丙腈。

4. 发明申请

US20100267751A1 PHARMACEUTICAL COMPOSITIONS AND METHODS OF TREATING DRY EYE DISORDERS 有权
标题翻译：药物组合物和治疗干眼症的方法
公开(公告)号：US20100267751A1
公开(公告)日：2010-10-21
申请号：US12668604
申请日：2008-07-04
申请人： Channing R. Beals , Elizabeth Woldemussie
发明人： Channing R. Beals , Elizabeth Woldemussie
IPC分类号： A61K31/519 , A61P27/02
CPC分类号： A61K31/519 , A61K9/0048
摘要： Inhibitors of Janus kinase-3 (“Jak3”) are useful for treating dry eye disorders and other disorders requiring the wetting of the eye. Jak3 inhibitors useful for treating eye disorders include the compound 3-{(3R,4R)-4-Methyl-3-[methyl-(7H-pyrrolo [2,3-d]pyrimidin-4-yl)-amino]-piperidin-1-yl}-3-oxo-propionitrile.
摘要翻译： Janus激酶-3（“Jak3”）的抑制剂可用于治疗干眼病和其它需要润湿眼睛的疾病。用于治疗眼睛疾病的Jak3抑制剂包括化合物3 - {（3R，4R）-4-甲基-3- [甲基 - （7H-吡咯并[2,3-d]嘧啶-4-基） - 氨基] - 哌啶 -1-基} -3-氧代 - 丙腈。

5. 发明授权

US5521210A Ophthalmic use of muscarinic agonists having increased duration of activity 失效
标题翻译：具有增加活动持续时间的毒蕈碱激动剂的眼科用途
公开(公告)号：US5521210A
公开(公告)日：1996-05-28
申请号：US48829
申请日：1993-04-13
申请人： Elizabeth WoldeMussie , Roger F. Steinert , Guadalupe Ruiz
发明人： Elizabeth WoldeMussie , Roger F. Steinert , Guadalupe Ruiz
IPC分类号： A61K31/40
CPC分类号： A61K31/40 , Y10S514/912 , Y10S514/913
摘要： A method for inducing prolonged pseudoaccommodation includes the instillation of an ophthalmic formulation into an eye for contracting the iris sphincter muscle, but not the ciliary muscle, in order to cause sphincter muscle contraction for a period of greater than about one hour per installation. The method further provides for the stabilization of an implanted intraocular lens immediately after surgery and for reducing glare following radial keratotomy.
摘要翻译：用于诱导长时间假性调节的方法包括将眼用制剂滴入眼睛以将虹膜括约肌肌肉而不是睫状肌收缩，以便每次安装大于约1小时引起括约肌收缩。该方法进一步提供了在手术后立即稳定植入的眼内晶状体，并且用于减小径向角膜切开术后的眩光。

6. 发明申请

US20070212395A1 Ocular therapy using sirtuin-activating agents 审中-公开
标题翻译：使用sirtuin激活剂的眼部治疗
公开(公告)号：US20070212395A1
公开(公告)日：2007-09-13
申请号：US11371117
申请日：2006-03-08
申请人： John Donello , Rong Yang , Elizabeth WoldeMussie , Fabien Schweighoffer
发明人： John Donello , Rong Yang , Elizabeth WoldeMussie , Fabien Schweighoffer
IPC分类号： A61K31/7048 , A61K31/353 , A61F2/02 , A61K31/05
CPC分类号： A61K9/0051 , A61K9/1647 , A61K31/05
摘要： Ophthalmically therapeutic compositions, such as polymeric drug delivery systems, include a therapeutic component that includes a sirtuin-activating agent, such as resveratrol, which, upon delivery to the posterior segment of a mammalian eye, treats ocular conditions. Methods of making and using the present compositions are also described.
摘要翻译：眼科治疗组合物，例如聚合物药物递送系统，包括治疗组分，其包括沉默调节蛋白激活剂，例如白藜芦醇，其在递送至哺乳动物眼睛的后部段时治疗眼部病症。还描述了制备和使用本发明组合物的方法。

7. 发明授权

US06465464B2 Method of using (2-imidazolin-2-ylamino) quinoxalines in treating ocular neural injury 有权
标题翻译：使用（2-咪唑啉-2-基氨基）喹喔啉处理眼神经损伤的方法
公开(公告)号：US06465464B2
公开(公告)日：2002-10-15
申请号：US10080451
申请日：2002-02-22
申请人： Larry A. Wheeler , Elizabeth Woldemussie , Ronald K. Lai
发明人： Larry A. Wheeler , Elizabeth Woldemussie , Ronald K. Lai
IPC分类号： A61K31495
CPC分类号： A61K31/498 , A61K31/495 , Y10S514/912 , Y10S514/913
摘要： The present invention provides a method of providing neuroprotection to a mammal comprising administering to said mammal suffering from or at risk of suffering a noxious action on its nerve cells an effective amount of a compound of formula I to inhibit or prevent nerve cell injury or death wherein the 2-imidazolin-2-ylamino group is in either the 5- or 6-position of the quinoxaline nucleus; x, y and z are in any of the remaining 5-, 6-, 7- or 8-positions and are selected from hydrogen, halogen, lower alkyl, lower alkoxy or trifluoromethyl; and R is an optional substituent in either the 2- or 3-position of the quinoxaline nucleus and may be hydrogen, lower alkyl or lower alkoxy, or pharmaceutically acceptable salts thereof and mixtures thereof. Such noxious action may result from ischemia, e.g. spinal ischemia.
摘要翻译：本发明提供了向哺乳动物提供神经保护作用的方法，包括对所述哺乳动物患有或有风险对其神经细胞发生有害作用的有效量的式I化合物以抑制或预防神经细胞损伤或死亡，其中 2-咪唑啉-2-基氨基在喹喔啉核的5-或6-位; x，y和z在剩余的5-，6-，7-或8-位中的任一个中，并且选自氢，卤素，低级烷基，低级烷氧基或三氟甲基; 并且R是喹喔啉核的2-或3-位任选的取代基，并且可以是氢，低级烷基或低级烷氧基，或其药学上可接受的盐及其混合物。这种有害作用可能是由局部缺血引起的。脊髓缺血。

8. 发明授权

US06410544B1 Cholinergic agents in the treatment of presbyopia 有权
标题翻译：胆碱能药物治疗老花眼
公开(公告)号：US06410544B1
公开(公告)日：2002-06-25
申请号：US09842299
申请日：2001-04-25
申请人： Arlene Gwon , Elizabeth WoldeMussie
发明人： Arlene Gwon , Elizabeth WoldeMussie
IPC分类号： A61K31505
CPC分类号： A61K31/695 , A61K31/00 , A61K31/221 , A61K31/27 , A61K31/341 , A61K31/4178 , A61K31/4453 , A61K31/452 , A61K31/551 , A61K31/5513 , Y10S514/912
摘要： A method for increasing or decreasing parasympathetic/cholinergic/ciliary tonic contraction in order to restore the resting portion of the eye and allow normal positive and negative accommodation includes administering to a myopic or hyperopic presbyope.
摘要翻译：用于增加或减少副交感神经/胆碱能/睫状肌紧张收缩以恢复眼睛的静息部分并允许正常的阳性和阴性适应的方法包括给予近视或远视的远视。

9. 发明授权

US06248741B1 Method of using (2-imidazolin-2-ylamino) quinoxalines in treating ocular neural injury 失效
标题翻译：使用（2-咪唑啉-2-基氨基）喹喔啉处理眼神经损伤的方法
公开(公告)号：US06248741B1
公开(公告)日：2001-06-19
申请号：US09655579
申请日：2000-09-06
申请人： Larry A. Wheeler , Elizabeth Woldemussie , Ronald K. Lai
发明人： Larry A. Wheeler , Elizabeth Woldemussie , Ronald K. Lai
IPC分类号： A61K3150
CPC分类号： A61K31/498 , A61K31/495 , Y10S514/912 , Y10S514/913
摘要： The present invention provides a method of providing neuroprotection to a mammal comprising administering to said mammal suffering from or at risk of suffering a noxious action on its nerve cells an effective amount of a compound of formula I to inhibit or prevent nerve cell injury or death wherein the 2-imidazolin-2-ylamino group is in either the 5- or 6-position of the quinoxaline nucleus; x, y and z are in any of the remaining 5-, 6-, 7- or 8-positions and are selected from hydrogen, halogen, lower alkyl, lower alkoxy or trifluoromethyl; and R is an optional substituent in either the 2- or 3-position of the quinoxaline nucleus and may be hydrogen, lower alkyl or lower alkoxy, or pharmaceutically acceptable salts thereof and mixtures thereof. Such noxious action may result from ischemia, e.g. spinal ischemia.
摘要翻译：本发明提供了向哺乳动物提供神经保护作用的方法，包括对所述哺乳动物患有或有风险对其神经细胞发生有害作用的有效量的式I化合物以抑制或预防神经细胞损伤或死亡，其中 2-咪唑啉-2-基氨基在喹喔啉核的5-或6-位; x，y和z在剩余的5-，6-，7-或8-位中的任一个中，并且选自氢，卤素，低级烷基，低级烷氧基或三氟甲基; 并且R是喹喔啉核的2-或3-位任选的取代基，并且可以是氢，低级烷基或低级烷氧基，或其药学上可接受的盐及其混合物。这种有害作用可能是由局部缺血引起的。脊髓缺血。

10. 发明授权

US5891911A Method for reducing intraocular pressure in the mammalian eye by administration of calcium chelators 失效
标题翻译：通过施用钙螯合剂降低哺乳动物眼睛眼内压的方法
公开(公告)号：US5891911A
公开(公告)日：1999-04-06
申请号：US260648
申请日：1995-07-28
申请人： Joseph S. Adorante , Elizabeth WoldeMussie , Guadalupe Ruiz
发明人： Joseph S. Adorante , Elizabeth WoldeMussie , Guadalupe Ruiz
IPC分类号： A61K31/00 , A61K31/198 , A61K31/216 , A61K31/222 , A61K31/23 , A61K47/48
CPC分类号： A61K47/4813 , A61K31/00 , A61K31/198 , A61K31/216 , A61K31/222 , A61K31/23 , Y10S514/912
摘要： Pharmaceutical compositions and a method are disclosed for treating glaucoma and/or ocular hypertension in the mammalian eye by administering to the mammalian eye the pharmaceutical composition of the invention which contains as the active ingredient one or more compounds having calcium chelating activity. Examples of calcium chelating agents utilized in the pharmaceutical composition and method of treatment are: ##STR1## and lower alkyl and alkoxyalkyl esters thereof.
摘要翻译：公开了药物组合物和方法，用于通过向哺乳动物眼睛施用含有作为活性成分的一种或多种具有钙螯合活性的化合物的本发明的药物组合物来治疗哺乳动物眼中的青光眼和/或高眼压症。用于药物组合物和治疗方法的钙螯合剂的实例是：其低级烷基和烷氧基烷基酯。

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