IP Library Granted Patent US 10,016,441
Granted Patent B2
US 10,016,441 · App. 15/448,805 · Granted Jul 10, 2018

Prostaglandin conjugates and derivatives for treating glaucoma and ocular hypertension

Inventors: David Archer Ellis (Forth Worth, TX); Lukas Scheibler (Telluride, CO); Najam A. Sharif (Arlington, TX)
Assignee: NOVARTIS AG
A61K31/5575A61K47/48061
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Quick Facts
Patent No.
US 10,016,441
App. No.
15/448,805
Granted
Jul 10, 2018
Kind
B2
Abstract

Prostaglandin conjugates and derivatives and methods for their use to treat glaucoma and/or lower intraocular pressure are disclosed. Additionally, ophthalmic pharmaceutical compositions useful in the treatment of eye diseases such as glaucoma and elevated intraocular pressure are disclosed. Such compositions comprise an effective amount of prostaglandin conjugates or derivatives of the present invention.

Claims (10)

1. A compound represented by Formula (I):

in which A is selected from the group consisting of:

where:

n is 1-6;

R 1 , R 2 , R 3 independently=OH or O—NO 2 ;

R 4 , R 5 independently=H, alkyl, or heteroalkyl; or R 4 and R 5 can combine to form cyclic alkyl or cyclic heteroalkyl; and

R 6 independently=H, NO 2 , organic nitrate, organic nitrite, metal—NO complex, sodium nitroprusside (SNP), dinitrosyl iron thiol complex (DNICs), N-nitrosamine, N-hydroxy-N-nitrosamine, N-nitrosimine, nitrosimine, C-nitroso, diazetine dioxide, furoxan, benzofuroxan, oxatriazole-5-imine, sydnonimine, oxime, hydroxylamine, N-hydroxyguanidine, or hydroxyurea.

2. The compound of claim 1 wherein the compound is a pharmaceutically acceptable salt of a compound according to Formula (I).

3. A compound selected from the group consisting of: Isopropyl (Z)-7-((1R,2R,3R,5S)-3,5-bis(nitrooxy)-2-((R,E)-3-(nitrooxy)-4-(3-(trifluoromethyl)phenoxy)but-1-en-1-yl)cyclopentyl)hept-5-enoate and (Z)-2-((((Z)-7-((1R,2R,3R,5S)-3,5-dihydroxy-2-((R,E)-3-hydroxy-4-(3-(trifluoromethyl)phenoxy)but-1-en-1-yl)cyclopentyl)hept-5-enoyl)oxy)methoxy)-1-(pyrrolidin-1-yl)diazene 1-oxide.

4. The compound of claim 3 , wherein the compound is a pharmaceutically acceptable salt.

Assignments (1)
CONFIRMATORY DEED OF ASSIGNMENT EFFECTIVE APRIL 8, 2019 Recorded Dec 10, 2019
From: NOVARTIS AG
To: ALCON INC.
Reel/Frame 051454/0788 →
Continuity (3)
Division 14884074 · Oct 15, 2015
Provisional Application 62064193 · Oct 15, 2014
Related Publication 20170239268A1 · Aug 24, 2017