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    • 7. 发明授权
    • Method for reducing intraocular pressure in the mammalian eye by
administration of muscarinic antagonists
    • US5716952A
    • 1998-02-10
    • US853374
    • 1992-03-18
    • Elizabeth WoldeMussieGuadalupe Ruiz
    • Elizabeth WoldeMussieGuadalupe Ruiz
    • A61K45/00A61K31/135A61K31/445A61K31/55A61P27/02A61K31/34
    • A61K31/55A61K31/135A61K31/445Y10S514/913
    • 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. 发明授权
    • Method for reducing intraocular pressure in the mammalian eye by
administration of gamma aminobutyric acid (GABA) agonists
    • 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
    • US6077839A
    • 2000-06-20
    • US856012
    • 1992-03-19
    • Elizabeth WoldeMussieGuadalupe Ruiz
    • Elizabeth WoldeMussieGuadalupe Ruiz
    • A61K9/08A61K31/19A61K31/195A61K31/42A61K31/425A61K31/44A61K31/445A61K31/475A61K31/55A61K45/00A61P27/02A61P27/06A61P43/00A61K31/205A61K31/385
    • A61K31/195A61K31/42A61K31/44A61K31/445A61K31/475A61K31/55Y10S514/913
    • 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.
    • 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 。