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8-Azaprostaglandin analogs as agents for lowering intraocular pressure

a technology of azaprostaglandin and analogs, applied in the field of ocular hypotensive agents, can solve the problems of pupil blockage, acute attack, and impeded drainage of aqueous humor

Inactive Publication Date: 2004-08-12
OLD DAVID W +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In chronic open-angle glaucoma, the anterior chamber and its anatomic structures appear normal, but drainage of the aqueous humor is impeded.
Dilation of the pupil may push the root of the iris forward against the angle, and may produce pupilary block and thus precipitate an acute attack.
The clinical potentials of prostaglandins in the management of conditions associated with increased ocular pressure, e.g. glaucoma are greatly limited by these side effects.

Method used

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  • 8-Azaprostaglandin analogs as agents for lowering intraocular pressure
  • 8-Azaprostaglandin analogs as agents for lowering intraocular pressure
  • 8-Azaprostaglandin analogs as agents for lowering intraocular pressure

Examples

Experimental program
Comparison scheme
Effect test

example 1a

[0084] 7-[2S-[3R-Hydroxy-4-(chloro-phenyl)-but-1-enyl]-5-oxo-pyrrolidin-1--yl]-heptanoic acid

example 2

[0085] 7-[2S-[3R-Hydroxy-4-(chlorophenyl)-butyl]-5-oxo-pyrrolidin-1-yl]-he-ptanoic acid, ethyl ester

example 2a

[0086] 7-[2S-[3R-Hydroxy-4-(chlorophenyl)-but-1-enyl]-5oxo-pyrrolidin-1-yl-]-heptanoic acid, ethyl ester

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PUM

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Abstract

The present invention provides a method of treating ocular hypertension or glaucoma which comprises administering to an animal having ocular hypertension or glaucoma therapeutically effective amount of a compound represented by the general formula I; wherein X, Y, Z, D and R<3 >are as defined in the specification.

Description

[0001] The present invention relates 8-Azaprostaglandin analogues as potent ocular hypotensives that are particularly suited for the management of glaucoma.DESCRIPTION OF RELATED ART[0002] Ocular hypotensive agents are useful in the treatment of a number of various ocular hypertensive conditions, such as post-surgical and post-laser trabeculectomy ocular hypertensive episodes, glaucoma, and as presurgical adjuncts.[0003] Glaucoma is a disease of the eye characterized by increased intraocular pressure. On the basis of its etiology, glaucoma has been classified as primary or secondary. For example, primary glaucoma in adults (congenital glaucoma) may be either open-angle or acute or chronic angle-closure. Secondary glaucoma results from pre-existing ocular diseases such as uveitis, intraocular tumor or an enlarged cataract.[0004] The underlying causes of primary glaucoma are not yet known. The increased intraocular tension is due to the obstruction of aqueous humor outflow. In chronic...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): C07D207/27A61K31/4015A61K31/559A61P27/06
CPCA61K31/4015A61P9/12A61P27/02A61P27/06A61P43/00A61K31/41C07D207/26
Inventor OLD, DAVID W.DINH, DANNY THANGBURK, ROBERT M.
Owner OLD DAVID W
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