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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).