Method of treating neurodegenerative disorders of the retina and optic nerve head
AssigneeAlcon Inc.
InventorsDaniel A. Gamache, Gustav Graff, John M. Yanni, Michael A. Kapin
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Abstract
The use of 3-benzolphenylacetic acids and derivatives, including nepafenac, to treat neurodegenerative retinal disorders is disclosed.
Claims12
A method of treating or preventing a neurodegenerative disorder of the retina or optic nerve head in a patient suffering from or predisposed to such a disorder which comprises administering to the patient a therapeutically effective amount of 3-benzoylphenylacetic acid or derivative of the formula:
- wherein
- R=H, C1-4 (un)branched alkyl, CF3, SR4;
- Y=OR′, NR″R′;
- R′=H, C1-10 (un)branched alkyl, aryl, aryl substituted by X, heterocycle, heterocycle substituted by X,
- —(CH2)nZ(CH2)n.A;
- n=2-6;
- n′=1-6;
- Z=nothing, O, C═O, OC(═O), C(═O)O, C(═O)NR3, NR3C(═O), S(O)2, CHOR3, NR3;
- n2=0-2;
- R3=H, C1-6 (un)branched alkyl, aryl, aryl substituted by X, heterocycle, heterocycle substituted by X;
- A=H, OH, aryl, aryl substituted by X, heterocycle, heterocycle substituted by X, —(CH2)nOR3;
- R″=H, OH, OR′;
- X and X′ independently=H, F, Cl, Br, I, OR′, CN, OH, S(O)n2R4, CF3, R4, NO2;
- R4=C1-6 (un)branched alkyl;
- m=0-3;
- m′=0-5;
- and
- W=O, H.
A method of providing neuroprotection to the retina or optic nerve head in a patient suffering from or predisposed to a neurodegenerative disorder of the retina or optic nerve head said method comprising administering to the patient a therapeutically effective amount of 3-benzoylphenylacetic acid or derivative of the formula:
- wherein
- R =H, C1-4 (un)branched alkyl, CF3, SR4
- Y=OR′, NR″R′;
- R′=H, C1-10 (un)branched alkyl, alkyl substituted by X, heterocycle, heterocycle substituted by X,
- —(CH2)nZ(CH2)n′A;
- n=2-6;
- n′=1-6;
- Z=nothing, O, C═O, OC(═O), C(═O)O, C(═O)NR3, NR3C(═O), S(O)n2, CHOR3, NR3;
- n2=0-2;
- R3=H, C1-6 (un)branched alkyl, aryl, aryl substituted by X, heterocycle, heterocycle substituted by X;
- A=H, OH, aryl, aryl substituted by X, heterocycle, heterocycle substituted by X, —(CH2)nOR3,
- R″=H, OH, OR′;
- X and X′ independently=H, F, Cl, Br, I, OR′, CN, OH, S(O)n2R4, CF3, R4, NO2;
- R4=C1-6 (un)branched alkyl;
- m=0-3;
- m′=0-5;
- and
- W=O, H;
- wherein the disorder is selected from the group consisting of atrophic macular degeneration;
- retinitis pigmentosa;
- iatrogenic retinopathy;
- retinal tears and holes;
- diabetic retinopathy;
- sickle cell retinopathy;
- retinal vein and artery occlusion;
- and
- optic neuropathy.
Dependencies are inferred from the claim text.