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US 2022/0087992 A1Published application
Compounds and methods of treating retinal degeneration
AssigneeCase Western Reserve University
InventorsKrzysztof Palczewski, Yuanyuan Chen
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Abstract
A method of treating retinal degeneration in a subject includes administering to the subject a therapeutically effective amount of a compound of formula (I).
Claims35
A method of treating retinal degeneration in a subject, comprising:
- administering to the subject a therapeutically effective amount of a compound of formula (I):
- wherein X1 is CH2, C═O, N—R3;
- wherein X2 is O or N—R4;
- wherein R1 and R2 are each independently selected from the group consisting of hydrogen a substituted or unsubstituted cycloalkyl, heterocyclyl, aryl, and heteroaryl, wherein at least one of R1 or R2 is not H;
- wherein R3 and R4 are each independently selected from the group consisting of hydrogen, a substituted or unsubstituted C1-C24 alkyl, C2-C24 alkenyl, C2-C24 alkynyl, C3-C20 aryl, heteroaryl, heterocycloalkenyl containing from 5-6 ring atoms (wherein from 1-3 of the ring atoms is independently selected from N, NH, N(C1-C6 alkyl), NC(O)(C1-C6 alkyl), o, and S), C6-C24 alkaryl, C6-C24 aralkyl, halo, —Si(C1-C3 alkyl)3, hydroxyl, sulfhydryl, C1-C24 alkoxy, C2-C24 alkenyloxy, C2-C24 alkynyloxy, C5-C20 aryloxy, acyl, acyloxy, C2-C24 alkoxycarbonyl, C6-C20 aryloxycarbonyl, C2-C24 alkylcarbonato, C6-C20 arylcarbonato, carboxy, carboxylato, carbamoyl, C1-C24 alkyl-carbamoyl, arylcarbamoyl, thiocarbamoyl, carbamido, cyano, isocyano, cyanato, isocyanato, isothiocyanato, azido, formyl, thioformyl, amino, C1-C24 alkyl amino, C5-C20 aryl amino, C2-C24 alkylamido, C6-C20 arylamido, imino, alkylimino, arylimino, nitro, nitroso, sulfo, sulfonato, C1-C24 alkylsulfanyl, arylsulfanyl, C1-C24 alkylsulfinyl, C5-C20 arylsulfinyl, C1-C24 alkylsulfonyl, C5-C20 arylsulfonyl, phosphono, phosphonato, phosphinato, phospho, or phosphino or combinations thereof;
- and pharmaceutically acceptable salts thereof.
3 more elements
A method of treating retinitis pigmentosa in a subject, comprising:
- administering to the subject a therapeutically effective amount of a compound of formula (I);
- wherein X1 is CH2, C═O, N—R3;
- wherein X2 is O or N—R4;
- wherein R1 and R2 are each independently selected from the group consisting of a substituted or unsubstituted cycloalkyl, heterocyclyl, aryl, and heteroaryl, wherein at least one of R1 or R2 is not H;
- wherein R3 and R4 are each independently selected from the group consisting of hydrogen, a substituted or unsubstituted C1-C24 alkyl, C2-C24 alkenyl, C2-C24 alkynyl, C3-C20 aryl, heteroaryl, heterocycloalkenyl containing from 5-6 ring atoms (wherein from 1-3 of the ring atoms is independently selected from N, NH, N(C1-C6 alkyl), NC(O)(C1-C6 alkyl), O, and S), C6-C24 alkaryl, C6-C24 aralkyl, halo, -Si(C1-C3 alkyl)3, hydroxyl, sulfhydryl, C1-C24 alkoxy, C2-C24 alkenyloxy, C2-C24 alkynyloxy, C5-C20 aryloxy, acyl, acyloxy, C2-C24 alkoxycarbonyl, C6-C20 aryloxycarbonyl, C2-C24 alkylcarbonato, C6-C20 arylcarbonato, carboxy, carboxylato, carbamoyl, C1-C24 alkyl-carbamoyl, arylcarbamoyl, thiocarbamoyl, carbamido, cyano, isocyano, cyanato, isocyanato, isothiocyanato, azido, formyl, thioformyl, amino, C1-C24 alkyl amino, C5-C20 aryl amino, C2-C24 alkylamido, C6-C20 arylamido, imino, alkylimino, arylimino, nitro, nitroso, sulfo, sulfonato, C1-C24 alkylsulfanyl, arylsulfanyl, C1-C24 alkylsulfinyl, C5-C20 arylsulfinyl, C1-C24 alkylsulfonyl, C5-C20 arylsulfonyl, phosphono, phosphonato, phosphinato, phospho, or phosphino or combinations thereof;
- and pharmaceutically acceptable salts thereof.
3 more elements
Dependencies are inferred from the claim text.