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US 8,492,589 B2Granted
Alkynyl phenyl derivative compounds for treating ophthalmic diseases and disorders
AssigneeAcucela Inc.
InventorsIan Leslie Scott, Vladimir Aleksandrovich Kuksa, Mark W. Orme, Thomas Little, Anna Gall, Jennifer Gage, Feng Hong
Life of this patent
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Abstract
Provided are alkynyl phenyl derivative compounds, pharmaceutical compositions thereof, and methods of treating ophthalmic diseases and disorders, such as age-related macular degeneration and Stargardt's Disease, using said compounds and compositions.
Claims21
A compound having the structure of Formula (E):
- as a tautomer or a mixture of tautomers, or as a pharmaceutically acceptable salt, N-oxide, stereoisomer, or geometric isomer thereof, wherein:
- m is 0, 1, 2 or 3;
- R21 and R22 are each independently hydrogen, C1-C5 alkyl or fluoroalkyl;
- R3 and R4 are each hydrogen;
- R5 is aryl, carbocyclyl, heteroaryl or heterocyclyl;
- each R6 is the same or different and independently hydrogen or C1-C5 alkyl;
- R9 is alkyl;
- R12 and R13 are the same or different and independently hydrogen, or —C(═O)R9;
- and
- each R14 is the same or different and independently alkyl, halo, fluoroalkyl or —OR6.
7 more elements
A pharmaceutical composition comprising a pharmaceutically acceptable carrier and a compound having the structure of Formula (E):
- as a tautomer or a mixture of tautomers, or as a pharmaceutically acceptable salt, N-oxide, stereoisomer, or geometric isomer thereof, wherein:
- m is 0, 1, 2 or 3;
- R21 and R22 are each independently hydrogen, C1-C5 alkyl or fluoroalkyl;
- R3 and R4 are each hydrogen;
- R5 is aryl, carbocyclyl, heteroaryl or heterocyclyl;
- each R6 is the same or different and independently hydrogen or C1-C5 alkyl;
- R9 is alkyl;
- R12 and R13 are the same or different and independently hydrogen, or —C(═O)R9;
- and
- each R14 is the same or different and independently alkyl, halo, fluoroalkyl or —OR6.
7 more elements
Dependencies are inferred from the claim text.