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.
Claims25
A method for treating an ophthalmic disease or disorder resulting at least in part from lipofuscin pigment accumulation in an eye of a subject, comprising administering to the subject a pharmaceutical composition comprising a compound having the structure of Formula (E):
- or a pharmaceutically acceptable salt 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 or carbocyclyl;
- 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.
A method for treating an ophthalmic disease or disorder resulting at least in part from lipofuscin pigment accumulation in an eye of a subject, comprising administering to the subject a pharmaceutical composition comprising a compound having the structure of Formula (F):
- or a pharmaceutically acceptable salt 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;
- 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, alkyl or —C(═O)R9;
- each R14 is the same or different and independently alkyl, halo, fluoroalkyl or —OR6;
- and
- R16, R17 and R18 are each the same or different and independently hydrogen, alkyl, —OR6, carbocyclyl or aryl.
A method for treating an ophthalmic disease or disorder resulting at least in part from lipofuscin pigment accumulation in an eye of a subject, comprising administering to the subject a pharmaceutical composition comprising a compound chosen from:
- 4-((3-(2-aminoethoxy)phenyl)ethynyl)-heptan-4-ol;
- 1-(3-(2-aminoethoxy)phenyl)-3-ethylpent-1-yn-3-ol;
- 1-(3-(2-aminoethoxy)phenyl)-3-isopropyl-4-methylpent-1-yn-3-ol;
- 5-((3-(2-aminoethoxy)phenyl)ethynyl)-nonan-5-ol;
- 4-(3-(2-aminoethoxy)phenyl)-2-methylbut-3-yn-2-ol;
- 2-(3-(4-methylpent-1-ynyl)phenoxy)ethanamine;
- 6-(3-(2-aminoethoxy)phenyl)hex-5-yn-1-ol;
- 2-(3-(3-phenylprop-1-ynyl)phenoxy)ethanamine;
- 4-(3-(2-aminoethoxy)phenyl)but-3-yn-1-ol;
- 2-(3-(hept-1-ynyl)phenoxy)ethanamine;
- 2-(3-(3-cyclopentylprop-1-ynyl)phenoxy)ethanamine;
- 2-(3-(4-phenylbut-1-ynyl)phenoxy)ethanamine;
- 5-(3-(2-aminoethoxy)phenyl)pent-4-yn-1-ol;
- 2-(3-(hex-1-ynyl)phenoxy)ethanamine;
- 2-(3-(3-methoxyprop-1-ynyl)phenoxy)ethanamine;
- 1-(3-(2-aminoethoxy)phenyl)hex-1-yn-3-ol;
- 1-(3-(2-aminoethoxy)phenyl)-3-methylhex-1-yn-3-ol;
- 1-(3-(2-aminoethoxy)phenyl)-4-methylpent-1-yn-3-ol;
- 2-(3-(4-methoxybut-1-ynyl)phenoxy)ethanamine;
- 5-(3-(2-aminoethoxy)-phenyl)-N-methylpent-4-ynamide;
- 5-(3-(2-aminoethoxy)phenyl)-N,N-dimethylpent-4-ynamide;
- 5-(3-(2-aminoethoxy)phenyl)pent-4-ynamide;
- 2-(3-(5-methoxypent-1-ynyl)phenoxy)ethanamine, or a pharmaceutically acceptable salt thereof.
Dependencies are inferred from the claim text.