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US 2014/0275043 A1Published application
Substituted 3-phenylpropylamine derivatives for the treatment of ophthalmic diseases and disorders
AssigneeAcucela Inc.
InventorsVladimir A. Kuksa, Mark W. Orme, Feng Hong, Ryo Kubota
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Abstract
The present invention relates generally to compositions and methods for treating neurodegenerative diseases and disorders, particularly ophthalmic diseases and disorders. Provided herein are substituted 3-phenylpropylamine derivative compounds and pharmaceutical compositions comprising said compounds. The subject compositions are useful for treating and preventing ophthalmic diseases and disorders, including age-related macular degeneration (AMD) and Stargardt's Disease.
Claims16
A compound of Formula (C), or a pharmaceutically acceptable salt thereof:
- wherein,
- A is selected from —O— or —CH2—;
- Y is
- RA is OH, RB is H;
- or optionally, RA and RB together form an oxo;
- R1 and R2 are each independently selected from hydrogen, C1-C4 alkyl, —C(═O)R3;
- and
- R3 is selected from alkyl, alkoxy, or —OCH2OC(O)R4, wherein R4 is an alkyl or alkoxy.
5 more elements
A compound, or a pharmaceutically acceptable salt thereof, selected from the group consisting of:
- (R)-3-Amino-1-(3-((tetrahydro-2H-pyran-4-yl)methoxy)phenyl)propan-1-ol;
- 3-Amino-1-(3-((tetrahydro-2H-pyran-4-yl)methoxy)phenyl)propan-1-ol;
- (1R)-3-Amino-1-(3-((tetrahydro-2H-pyran-3-yl)methoxy)phenyl)propan-1-ol;
- (R)-3-Amino-1-(3-(pyridin-4-ylmethoxy)phenyl)propan-1-ol;
- (R)-3-Amino-1-(3-(pyridin-3-ylmethoxy)phenyl)propan-1-ol;
- (R)-3-Amino-1-(3-(pyridin-2-ylmethoxy)phenyl)propan-1-ol;
- (1R)-3-amino-1-(3-((tetrahydro-2H-thiopyran-3-yl)methoxy)phenyl)propan-1-ol;
- (R)-3-Amino-1-(3-((tetrahydro-2H-thiopyran-4-yl)methoxy)phenyl)propan-1-ol;
- (R)-4-((3-(3-Amino-1-hydroxypropyl)phenoxy)methyl)tetrahydro-2H-thiopyran 1,1-dioxide;
- 3-((3-((R)-3-Amino-1-hydroxypropyl)phenoxy)methyl)tetrahydro-2H-thiopyran 1,1-dioxide;
- (R)-1-(4-((3-(3-amino-1-hydroxypropyl)phenoxy)methyl)piperidin-1-yl)ethanone;
- (R)-3-Amino-1-(3-((6-methylpyridin-2-yl)methoxy)phenyl)propan-1-ol;
- (1R)-3-Amino-1-(3-((2,3-dihydrobenzofuran-2-yl)methoxy)phenyl)propan-1-ol;
- (1R)-3-Amino-1-(3-((tetrahydrofuran-2-yl)methoxy)phenyl)propan-1-ol;
- (R)-3-Amino-1-(3-(piperidin-4-ylmethoxy)phenyl)propan-1-ol;
- (R)-3-Amino-1-(3-((1-methylpiperidin-4-yl)methoxy)phenyl)propan-1-ol;
- (R)-Methyl 4-((3-(3-amino-1-hydroxypropyl)phenoxy)methyl)piperidine-1-carboxylate;
- (R)-3-Amino-1-(3-(pyrimidin-5-ylmethoxy)phenyl)propan-1-ol;
- (1R)-3-Amino-1-(3-(chroman-3-ylmethoxy)phenyl)propan-1-ol;
- (R)-4-((3-(3-Amino-1-hydroxypropyl)phenoxy)methyl)tetrahydro-2H-thiopyran 1-oxide;
- (R)-3-Amino-1-(3-(((S)-1-methylpyrrolidin-2-yl)methoxy)phenyl)propan-1-ol;
- (R)-3-Amino-1-(3-((S)-pyrrolidin-2-ylmethoxy)phenyl)propan-1-ol;
- (R)-3-Amino-1-(3-(((tetrahydro-2H-pyran-4-yl)methyl)amino)phenyl)propan-1-ol;
- 3-Amino-1-(3-(((1,1-dioxidotetrahydro-2H-thiopyran-4-yl)methyl)sulfonyl)phenyl)propan-1-one;
- 3-Amino-1-(3-(((tetrahydro-2H-pyran-3-yl)methyl)sulfonyl)phenyl)propan-1-one;
- 3-Amino-1-(3-(((tetrahydro-2H-pyran-4-yl)methyl) sulfonyl)phenyl)propan-1-one;
- 3-((3-((R)-3-Amino-1-hydroxypropyl)phenoxy)methyl)piperidin-2-one;
- (R)-3-Amino-1-(3-(thiophen-2-ylmethoxy)phenyl)propan-1-ol;
- (R)-3-Amino-1-(3-(thiophen-3-ylmethoxy)phenyl)propan-1-ol;
- (R)-tert-Butyl 4-((3-(3-amino-1-hydroxypropyl)phenoxy)methyl)piperidine-1-carboxylate;
- (E)-3-(3-((Tetrahydro-2H-pyran-4-yl)methoxy)phenyl)prop-2-en-1-amine;
- 3-(3-((Tetrahydro-2H-pyran-4-yl)methoxy)phenyl)propan-1-amine;
- (R)-3-(Methylamino)-1-(3-((tetrahydro-2H-pyran-4-yl)methoxy)phenyl)propan-1-ol;
- 1-((S)-2-((3-((R)-3-Amino-1-hydroxypropyl)phenoxy)methyl)pyrrolidin-1-yl)ethanone;
- 5-((3-((R)-3-Amino-1-hydroxypropyl)phenoxy)methyl)piperidin-2-one;
- 4-((3-((R)-3-Amino-1-hydroxypropyl)phenoxy)methyl)piperidin-2-one;
- 6-((3-((R)-3-Amino-1-hydroxypropyl)phenoxy)methyl)-1-methylpiperidin-2-one;
- 5-((3-((R)-3-Amino-1-hydroxypropyl)phenoxy)methyl)pyrrolidin-2-one;
- 5-((3-((R)-3-Amino-1-hydroxypropyl)phenoxy)methyl)-1-methylpyrrolidin-2-one;
- N-(3-(3-Amino-1-hydroxypropyl)phenyl)-6-oxopiperidine-3-carboxamide;
- 3-((3-((R)-3-Amino-1-hydroxypropyl)phenoxy)methyl)-1,2-thiazinane 1,1-dioxide;
- (R)-1-(3-((1H-Pyrrol-2-yl)methoxy)phenyl)-3-aminopropan-1-ol;
- (R)-3-Amino-1-(3-(furan-2-ylmethoxy)phenyl)propan-1-ol;
- (R)-3-Amino-1-(3-((1-(methylsulfonyl)piperidin-4-yl)methoxy)phenyl)propan-1-ol;
- (R)-1-(3-(((1H-Indol-6-yl)methyl)amino)phenyl)-3-aminopropan-1-ol;
- (R)-1-(3-((1H-Indol-6-yl)methoxy)phenyl)-3-aminopropan-1-ol;
- (R)-3-Amino-1-(3-(benzofuran-2-ylmethoxy)phenyl)propan-1-ol;
- 3-(3-((Tetrahydro-2H-pyran-4-yl)methoxy)phenyl)prop-2-yn-1-amine;
- 3-Amino-1-(3-(((tetrahydro-2H-pyran-4-yl)methyl)thio)phenyl)propan-1-ol;
- 3-Amino-1-(3-(((tetrahydro-2H-pyran-4-yl)methyl)sulfonyl)phenyl)propan-1-ol;
- 3-Amino-1-(3-(2-(tetrahydro-2H-pyran-4-yl)ethyl)phenyl)propan-1-ol;
- 3-Amino-1-(3-(2-(pyridin-3-yl)ethyl)phenyl)propan-1-ol;
- 3-Amino-1-(3-(2-(thiophen-3-yl)ethyl)phenyl)propan-1-ol;
- (E)-1-(3-(3-Amino-1-hydroxypropyl)styryl)pyrrolidin-2-one;
- 1-(3-(3-Amino-1-hydroxypropyl)phenethyl)pyrrolidin-2-one;
- 3-Amino-1-(3-(2-(pyrrolidin-1-yl)ethyl)phenyl)propan-1-ol;
- (E)-1-(3-(2-(1H-Imidazol-1-yl)vinyl)phenyl)-3-aminopropan-1-ol;
- 1-(3-(2-(1H-Imidazol-1-yl)ethyl)phenyl)-3-aminopropan-1-ol;
- (E)-3-Amino-1-(3-(2-(pyridin-2-yl)vinyl)phenyl)propan-1-ol;
- 3-Amino-1-(3-(2-(pyridin-2-yl)ethyl)phenyl)propan-1-ol;
- (E)-3-Amino-1-(3-(2-(tetrahydro-2H-pyran-4-yl)vinyl)phenyl)propan-1-ol;
- and
- 3-Amino-1-(3-(2-(tetrahydro-2H-pyran-4-yl)ethyl)phenyl)propan-1-ol.
60 more elements
Dependencies are inferred from the claim text.