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1. 发明授权

US08969415B2 Intraocular drug delivery systems 有权
标题翻译：眼内药物输送系统
公开(公告)号：US08969415B2
公开(公告)日：2015-03-03
申请号：US11565917
申请日：2006-12-01
申请人： Michael R. Robinson , Wendy M. Blanda , Patrick M. Hughes , Guadalupe Ruiz , Werhner C. Orilla , Scott M. Whitcup , Devin F. Welty , Joan-En Lin , Lon T. Spada
发明人： Michael R. Robinson , Wendy M. Blanda , Patrick M. Hughes , Guadalupe Ruiz , Werhner C. Orilla , Scott M. Whitcup , Devin F. Welty , Joan-En Lin , Lon T. Spada
IPC分类号： A61K31/165 , A61F2/00 , A61K31/565 , A61F9/00 , A61K9/00 , A61K9/16 , A61K9/50 , A61K31/498 , A61K31/557 , A61K9/10
CPC分类号： A61K31/565 , A61F9/0017 , A61K9/0048 , A61K9/0051 , A61K9/10 , A61K9/1635 , A61K9/1694 , A61K9/5031 , A61K31/498 , A61K31/557 , A61K47/34 , Y10S514/913
摘要： Biodegradable implants sized and suitable for implantation in an ocular region or site and methods for treating ocular conditions. The implants provide an extended release of an active agent at a therapeutically effective amount for a period of time between 10 days and one year or longer.
摘要翻译：尺寸适于植入眼部或部位的可生物降解植入物以及用于治疗眼部病症的方法。植入物以治疗有效量提供活性剂在10天至1年或更长时间内的延长释放。

2. 发明申请

US20080131484A1 INTRAOCULAR DRUG DELIVERY SYSTEMS 有权
标题翻译：内分泌药物输送系统
公开(公告)号：US20080131484A1
公开(公告)日：2008-06-05
申请号：US11565917
申请日：2006-12-01
申请人： Michael R. Robinson , Wendy M. Blanda , Patrick M. Hughes , Guadalupe Ruiz , Werhner C. Orilla , Scott M. Whitcup
发明人： Michael R. Robinson , Wendy M. Blanda , Patrick M. Hughes , Guadalupe Ruiz , Werhner C. Orilla , Scott M. Whitcup
IPC分类号： A61K9/00 , A61K31/56 , A61F9/00 , A61K31/498 , A61P27/02 , A61K31/565 , A61K31/495
CPC分类号： A61K31/565 , A61F9/0017 , A61K9/0048 , A61K9/0051 , A61K9/10 , A61K9/1635 , A61K9/1694 , A61K9/5031 , A61K31/498 , A61K31/557 , A61K47/34 , Y10S514/913
摘要： Biodegradable implants sized and suitable for implantation in an ocular region or site and methods for treating ocular conditions. The implants provide an extended release of an active agent at a therapeutically effective amount for a period of time between 10 days and one year or longer.
摘要翻译：尺寸适于植入眼部或部位的可生物降解植入物以及用于治疗眼部病症的方法。植入物以治疗有效量提供活性剂在10天至1年或更长时间内的延长释放。

3. 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。

4. 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。

5. 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。

6. 发明授权

US5573758A Method for reducing intraocular pressure in the mammalian eye by administration of potassium channel blockers 失效
公开(公告)号：US5573758A
公开(公告)日：1996-11-12
申请号：US431170
申请日：1995-04-28
申请人： Joseph S. Adorante , Elizabeth WoldeMussie , Guadalupe Ruiz
发明人： Joseph S. Adorante , Elizabeth WoldeMussie , Guadalupe Ruiz
IPC分类号： A61K45/00 , A61K31/00 , A61K31/407 , A61K31/475 , A61K31/49 , A61K35/64 , A61K38/17 , A61P27/02 , A61K31/74
CPC分类号： A61K9/0048 , A61K31/00 , A61K31/407 , A61K31/49 , A61K38/1767 , Y10S514/912 , Y10S514/913 , Y10S514/914
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 potassium channel blocking activity. Examples of potassium channel blockers utilized in the pharmaceutical composition and method of treatment are quinine, tremogenic indole alkaloids, such as Penitrem A and paspalicine, and insect toxins such as charybdotoxin and iberiotoxin.

7. 发明授权

US5866605A Method for providing a neuroprotective effect to 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向哺乳动物眼睛提供神经保护作用的方法
公开(公告)号：US5866605A
公开(公告)日：1999-02-02
申请号：US998912
申请日：1997-12-29
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 providing neuroprotective effect to 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 20 atoms, that may be derived from a lower alkanol.
摘要翻译：公开了药物组合物和方法，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氯化物通道阻断活性的化合物的本发明的药物组合物，向哺乳动物眼睛提供神经保护作用。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。

8. 发明授权

US5716952A Method for reducing intraocular pressure in the mammalian eye by administration of muscarinic antagonists 失效
公开(公告)号：US5716952A
公开(公告)日：1998-02-10
申请号：US853374
申请日：1992-03-18
申请人： Elizabeth WoldeMussie , Guadalupe Ruiz
发明人： Elizabeth WoldeMussie , Guadalupe Ruiz
IPC分类号： A61K45/00 , A61K31/135 , A61K31/445 , A61K31/55 , A61P27/02 , A61K31/34
CPC分类号： A61K31/55 , A61K31/135 , A61K31/445 , 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 muscarinic antagonist compounds. Examples of muscarinic antagonists utilized in the pharmaceutical composition and method of treatment are: 10H-thieno(3,4-b)(1,5)benzodiazepin-10-one 4,9-dihydro-3-methyl-4-((4-methyl-1-piperazinyl)acetyl) (telenzepine); 5,11-dihydro-11�4'-methyl-1'-piperazinyl)-acetyl!-6H-pyrido�2,3-b!�1,4!benzodiazepin-6-one (pirenzepine); racemic 11-��2-(Diethylamino)methyl!-1-piperidinyl!-acetyl!-5,11-dihydro-6H-pyrido�2,3-b!�1,4!benzodiazepin-6-one (AF-DX 116); dextrorotatory 11-��2-(Diethylamino)methyl!-1-piperidinyl!-acetyl!-5,11-dihydro-6H-pyrido�2,3-b!�1,4! benzodiazepin-6-one (AF-DX 250); an ophthalmically acceptable salt of 4-diphenylacetoxy-1,1-dimethyl piperidine (4-DAMP); .alpha.-cyclohexyl, -.alpha.-phenyl-1-piperidinepropanol (trihexyphenidyl); cyclohexanemethanol, .alpha.-phenyl, .alpha.-�3-(1-piperidinyl)-1-propynyl (hexbutinol); 6H-pyrido�2,3-b!�1,4!benzodiazepin-6-one, 11-��4-�4-(diethylamino)butyl!-1-piperidinyl!acetyl!-5,11-dihydro (AQ-RA 741); 11-H-pyrido�2,3-b!�1,4!benzodiazepine-11-carboxamide, N-�2-�2-�(dipropylamino)methyl!-1-piperidinyl!ethyl!-5-, 6-dihydro-6-oxo, monomethanesulfonate (AF-DX 384); 1,8-octanediamine, N,N'-bis�6-��2-methoxyphenyl)methyl!amino!hexyl!-tetrahydrochloride (methoctramine) and naphto�2,3-c!furan-1(3H)-one, 4-2-(1,6-dimethyl-2-piperidinyl)ethenyl!decahydro-3-methyl-, �3S-�3 .alpha., 3a .alpha., 4 .beta.�1E,2(2R*,6S*)!,4a .beta., 8a .alpha., 9a .alpha.!!(himbacine).

9. 发明申请

US20060264442A1 Methods for the treatment of ocular and neurodegenerative conditions in a mammal 审中-公开
标题翻译：用于治疗哺乳动物眼部和神经退行性疾病的方法
公开(公告)号：US20060264442A1
公开(公告)日：2006-11-23
申请号：US11133922
申请日：2005-05-18
申请人： Guadalupe Ruiz , Edwin Padillo , Elizabeth WoldeMussie
发明人： Guadalupe Ruiz , Edwin Padillo , Elizabeth WoldeMussie
IPC分类号： A61K31/517
CPC分类号： A61K31/513 , A61K31/517
摘要： Method for the treatment of conditions including ocular and neurodegenerative conditions in a mammal using a composition which comprises an effective amount of an alpha 1 adrenoreceptor antagonist.
摘要翻译：使用包含有效量的α1肾上腺素受体拮抗剂的组合物治疗哺乳动物使用的眼部和神经变性病症的病症的方法。

10. 发明授权

US6077839A Method for reducing intraocular pressure in the mammalian eye by administration of gamma aminobutyric acid (GABA) agonists 失效
标题翻译：通过给予γ-氨基丁酸（GABA）激动剂降低哺乳动物眼睛眼内压的方法
公开(公告)号：US6077839A
公开(公告)日：2000-06-20
申请号：US856012
申请日：1992-03-19
申请人： Elizabeth WoldeMussie , Guadalupe Ruiz
发明人： Elizabeth WoldeMussie , Guadalupe Ruiz
IPC分类号： A61K9/08 , A61K31/19 , A61K31/195 , A61K31/42 , A61K31/425 , A61K31/44 , A61K31/445 , A61K31/475 , A61K31/55 , A61K45/00 , A61P27/02 , A61P27/06 , A61P43/00 , A61K31/205 , A61K31/385
CPC分类号： A61K31/195 , A61K31/42 , A61K31/44 , A61K31/445 , A61K31/475 , A61K31/55 , Y10S514/913
摘要： Ophthalmic compositions and a method are disclosed for treating glaucoma and/or ocular hypertension in the mammalian eye by topically administering to the mammalian eye the ophthalmic composition of the invention which contains as the active ingredient one or more gamma aminobutyric acid agonist compounds. Examples of gamma aminobutyric acid agonists utilized in the ophthalmic composition and method of treatment are: gamma aminobutyric acid (GABA), 5-(aminomethyl)-3(2H)-isoxazolone (muscimol), 4,5,6,7-tetrahydroisoxazolo[5,4-c]pyridin-3-ol (THIP) and a pharmaceutically acceptable salt of 4,5,6,7-tetrahydroisoxazolo[5,4-c]pyridin-3-ol, piperidine-4-sulfonic acid and a pharmaceutically acceptable salt of piperidine-4-sulfonic acid, 3-(2H)-isothiazolone, 5-(aminomethyl) (thiomuscimol), 7-chloro-1,3-dihydro-1-methyl-5-phenyl-2H-1,4-benzodiazepin-2-one (diazepam), 7-chloro-1-[2-(diethylamino)ethyl]-5-(2-fluorophenyl)-1,3-dihydro-2H-1,4-benzodiazaepin-2-one (flurazepam) and a pharmaceutically acceptable salt of 7-chloro-1-[2-(diethylamino)ethyl]-5-(2-fluorophenyl)-1,3-dihydro and 7-chloro-N-methyl-5-phenyl-3H-1,4-benzodiazepin-2-amine 4-oxide (chlordiazepoxide) and a pharmaceutically acceptable salt of 7-chloro-N-methyl-5-phenyl-3H-1,4-benzodiazepin-2-amine 4-oxide.
摘要翻译：公开了用于治疗哺乳动物眼中的青光眼和/或高眼压症的眼科组合物和方法，其通过向哺乳动物眼睛局部施用含有作为活性成分的一种或多种γ-氨基丁酸激动剂化合物的本发明的眼用组合物。用于眼科组合物和治疗方法的γ-氨基丁酸激动剂的实例是：γ-氨基丁酸（GABA），5-（氨基甲基）-3（2H） - 异恶唑酮（麝香草酚），4,5,6,7-四氢异恶唑并[ 5,4-c]吡啶-3-醇（THIP）和4,5,6,7-四氢异恶唑并[5,4-c]吡啶-3-醇的药学上可接受的盐，哌啶-4-磺酸和哌啶-4-磺酸的药学上可接受的盐，3-（2H） - 异噻唑酮，5-（氨基甲基）（硫代假毛醇），7-氯-1,3-二氢-1-甲基-5-苯基-2H- 4-苯并二氮杂-2-酮（地西泮），7-氯-1- [2-（二乙基氨基）乙基] -5-（2-氟苯基）-1,3-二氢-2H-1,4-苯并二氮杂_ 一种（氟西泮）和7-氯-1- [2-（二乙基氨基）乙基] -5-（2-氟苯基）-1,3-二氢和7-氯-N-甲基-5-苯基的药学上可接受的盐 -3H-1,4-苯并二氮杂-2-胺4-氧化物（氯氮烷）和7-氯-N-甲基-5-苯基-3H-1,4-苯并二氮杂-2-胺4-氧化物的药学上可接受的盐。

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