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Oculoselective beta-blockers for treatment of elevated intraocular pressure

Assignee: Merck and Co Inc
•
Filing: 1985-08-29
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Granted: 1987-05-12
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Expires: 2005-08-29
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Abstract

Abstract Hydroxyalkyl-phenoxy-propan-2-olamines and novel esters thereof are oculoselective beta -blockers useful in the treatment of elevated intraocular pressure with little or no effect on the pulmonary or cardiovascular system.

Inventors

  • 👤 John J. Baldwin
  • 👤 Gerald S. Ponticello

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-11-06 15:08
CPC Classifications
C; C07; C07C; C07C217/00; C07C217/02; C07C217/04; A; A61; A61K; A61K31/00; A61K31/21; A61K31/215; A61K31/22; A61K31/13; A61K31/135; A61P; A61P25/00; A61P25/02; A61P27/00; A61P27/02; A61P27/06; C07C217/06; C07C217/14

Claims Analysis

Total Claims: 9
Claim 1
Independent Claim 16 words
The compound (R)- or (S)-2-(4-(3-((1,1-dimethylethyl)amino)-2-hydroxypropoxy) phenyl)-ethyl acetate, [2-(4-(3-((1,1-dimethylethyl)amino) 2-hydroxypropoxy)phenyl)ethyl 2,2-dimethylacetate] or an ophthalmologically acceptable salt thereof.
Claim 2
Dependent Claim 16 words
The compound (R)- or (S)-2-(4-(3-((1,1-dimethylethyl)amino)-2-hydroxypropoxy) phenyl)-ethyl acetate, [2-(4-(3-((1,1-dimethylethyl)amino) 2-hydroxypropoxy)phenyl)ethyl 2,2-dimethylacetate] or an ophthalmologically acceptable salt thereof.
Claim 3
Dependent Claim 11 words
The (S)-enantiomer of claim 1 or an ophthalmologically acceptable salt thereof.
Claim 4
Independent Claim 45 words
A method of treating elevated intraocular pressure in a patient in need of such treatment which comprises the topical ocular administration of an effective intraocular pressure lowering amount of the compound (R)- or (S)-2-(4-(3-((1, 1-dimethylethyl)amino)-2-hydroxypropoxy)phenyl)ethyl acetate, [2-(4-(3-((1,1-dimethylethyl)amino)-2-hydroxypropoxy) phenyl)ethyl 2,2-dimethylacetate] or an ophthalmologically acceptable salt thereof.
Claim 5
Independent Claim 45 words
A method of treating elevated intraocular pressure in a patient in need of such treatment which comprises the topical ocular administration of an effective intraocular pressure lowering amount of the compound (R)- or (S)-2-(4-(3-((1, 1-dimethylethyl)amino)-2-hydroxypropoxy)phenyl)ethyl acetate, [2-(4-(3-((1,1-dimethylethyl)amino)-2-hydroxypropoxy) phenyl)ethyl 2,2-dimethylacetate] or an ophthalmologically acceptable salt thereof.
Claim 6
Dependent Claim 11 words
The method of claim 3, wherein the compound is the (S)-enantiomer.
Claim 7
Dependent Claim 38 words
An ophthalmic formulation for the topical ocular treatment of elevated intraocular pressure comprising an ophthalmologically acceptable carrier and an effective amount of the compound (R)- or (S)-2-(4-(3-((1,1-dimethylethyl)amino)-2-hydroxypropoxy) phenyl)ethyl acetate[; 2-(4-(3-((1,1-dimethylaethyl)amino)2-hydroxy-propoxy) phenyl)ethyl 2,2-dimethylacetate] or an ophthalmologically acceptable salt thereof.
Claim 8
Dependent Claim 38 words
An ophthalmic formulation for the topical ocular treatment of elevated intraocular pressure comprising an ophthalmologically acceptable carrier and an effective amount of the compound (R)- or (S)-2-(4-(3-((1,1-dimethylethyl)amino)-2-hydroxypropoxy) phenyl)ethyl acetate[; 2-(4-(3-((1,1-dimethylaethyl)amino)2-hydroxy-propoxy) phenyl)ethyl 2,2-dimethylacetate] or an ophthalmologically acceptable salt thereof.
Claim 9
Dependent Claim 25 words
The formulationo of claim 2 wherein the compound is the (S)-enantiomer of 2-(4-(3-((1,1-dimethyl-ethyl) amino)-2-hydroxypropoxy)phenyl)ethyl acetate[; [2-(4-(3-((1,1-dimethylethyl)amino)-2-hydroxypropoxy)phenyl) ethyl acetate 2,2-dimethylacetate] or an ophthalmologically acceptable salt thereof.

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1990-05-11 1990-11-10 1991-05-12 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1994-05-11 1994-11-10 1995-05-12 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1998-05-11 1998-11-10 1999-05-12 $7700.00 Window Closed / Lapsed

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