IP Library Granted Patent US 6,906,097
Granted Patent B2
US 6,906,097 · App. 10/411,036 · Granted Jun 14, 2005

8-azaprostaglandin analogs as agents for lowering intraocular pressure

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Quick Facts
Patent No.
US 6,906,097
App. No.
10/411,036
Granted
Jun 14, 2005
Kind
B2
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.

Claims (13)

1. A compound useful for treating ocular hypertension or glaucoma which comprises a compound represented by the general formula I;

wherein hatched lines represent the α configuration, a triangle represents the β configuration, a wavy line represents either the α configuration or the β configuration and a dotted line represents the presence or absence of a double bond;

D represents a covalent bond or CH 2 , O, S or NH;

X is CONR 2 , CH 2 OR, P(O)(OR) 2 , CONRSO 2 R or SONR 2 ;

Z is CH 2 or a covalent bond;

R is H or R 2 ;

R 1 is H, R 2 , phenyl, or COR 2 ;

R 2 is C 1 -C 5 lower alkyl or alkenyl and R 3 is selected from the group consisting of R 2 , phenyl, thienyl, furanyl, pyridyl, benzothienyl, benzofuranyl, naphthyl, or substituted derivatives thereof, wherein the substituents maybe selected from the group consisting of C 1 -C 5 alkyl, halogen, CF 3 , CN, NO 2 , NR 2 , CO 2 R and OR.

2. A compound selected from the group consisting of

7-[2S-[3-Oxo-4-(phenyl)-butyl]-5-oxo-pyrrolidin-1-yl]-heptanoic acid;

7-[2S-[3-Oxo-4-(phenyl)-butyl]-5-oxo-pyrrolidin-1-yl]-heptanoic acid, ethyl ester;

7-[2S-[3-Oxo-4-(phenyl)-but-1-enyl]-5-oxo-pyrrolidin-1-yl]-heptanoic acid;

7-[2S-[3-Oxo-4-(phenyl)-but-1-enyl]-5-oxo-pyrrolidin-1-yl]-heptanoic acid, ethyl ester.