Method for reducing intraocular pressure in the mammalian...

A - Human Necessities – 61 – K

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A61K 31/55 (2006.01) A61K 31/135 (2006.01) A61K 31/445 (2006.01)

Patent

CA 2132007

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-5H-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]-l-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]-tetrahy-drochloride (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).

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