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US 12,637,425 B2Granted
Compounds and formulations for treating ophthalmic diseases
AssigneeVisus Therapeutics, Inc.
InventorsMichael S. Lopez, Bryan M. Dunyak
Life of this patent
Estimating the term…
Abstract
The present disclosure is directed to compounds, compositions, formulations and methods of use thereof in the treatment and prevention of ocular conditions including cataract and presbyopia.
Claims20
A compound represented by the structure of Formula (IVa):
- or a pharmaceutically acceptable salt thereof, wherein:
- Y1, Y2, Y3, Y4, Y5, and Y6 are independently selected from CR15 and N, wherein 0, 1, 2,
- or 3 of Y1, Y2, Y3, Y4, Y5, and Y6 are N;
- and wherein one of Y1, Y2, Y3, Y4, Y5, and Y6 is the attachment point to the rest of the molecule;
- R14 is selected from:
- hydrogen;
- C1-C6 alkyl which is optionally substituted with one or more substituents independently selected from R9;
- and
- C3-C6 cycloalkyl and 3- to 6-membered heterocycloalkyl, each of which is optionally substituted with one or more substituents independently selected from R9;
- each R15 is independently selected from:
- hydrogen, halogen, —CN, —OH, —OR13, —N(R12)2, —C(═O)R12, —C(═O)OR12, —C(═O)N(R12)2, —NR12C(═O)R12, —NR12C(═O)N(R12)2, —SR12, —S(═O)R13, —SO2R13, —SO2N(R12)2, and —NO2;
- C1-C6 alkyl, C2-C6 alkenyl, and C2-C6 alkynyl, each of which is optionally substituted with one or more substituents independently selected from R9;
- and
- C3-C6 cycloalkyl and 4-6-membered heterocycloalkyl, each of which is optionally substituted with one or more substituents independently selected from R9;
- R1 is selected from hydrogen;
- and C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, each of which is optionally substituted with one or more substituents independently selected from R9;
- R2 and R3 are independently selected from hydrogen;
- and C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C3-C6 carbocycle, and 3- to 6-membered heterocycle, each of which is optionally substituted with one or more substituents independently selected from R9;
- or R1 and R2 are taken together with the intervening atoms to which they are attached to form a 5- to 8-membered heterocycle, which is optionally substituted with one or more substituents independently selected from R9;
- or R2 and R3 are taken together with the intervening atoms to which they are attached to form a 4- to 10-membered heterocycle, which is optionally substituted with one or more substituents independently selected from R9;
- R7 is selected from:
- hydrogen;
- C1-C6 alkyl, C2-C6 alkenyl, and C2-C6 alkynyl, each of which is optionally substituted with one or more substituents independently selected from R9;
- and
- C3-C6 cycloalkyl and 4-6-membered heterocycloalkyl, each of which is optionally substituted with one or more substituents independently selected from R9;
- and
- each R8 is independently selected from:
- hydrogen, halogen, —CN, —OH, —OR13, —N(R12)2, —C(═O)R12, —C(═O)OR12, —C(═O)N(R12)2, —NR12C(═O)R12, —NR12C(═O)N(R12)2, —SR12, —S(═O)R13, —SO2R13, —SO2N(R12)2, and —NO2;
- C1-C6 alkyl, C2-C6 alkenyl, and C2-C6 alkynyl, each of which is optionally substituted with one or more substituents independently selected from R9;
- C3-C6 cycloalkyl and 4-6-membered heterocycloalkyl, each of which is optionally substituted with one or more substituents independently selected from R9;
- each R9 is independently selected from halogen, ═O, ═S, —CN, —OH, —OR13, —N(R12)2, —C(═O)R12, —C(═O)OR12, —OC(═O)R12, —C(═O)N(R12)2, —NR12C(═O)R12, —NR12C(═O)N(R12)2, —OC(═O)N(R12)2, —NR12C(═O)OR12, —OC(═O)OR12, —SR12, —S(═O)R13, —SO2R13, —SO2N(R12)2, —NO2, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C1-C6 haloalkyl, C1-C6 hydroxyalkyl, C1-C6 aminoalkyl, C3-C6 carbocycle, and 3- to 6-membered heterocycle;
- each R12 is independently selected from hydrogen, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C1-C6 haloalkyl, C3-C6 carbocycle, and 3- to 6-membered heterocycle;
- and
- each R13 is independently selected from C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C1-C6 haloalkyl, C3-C6 carbocycle, and 3- to 6-membered heterocycle.
31 more elements
A compound selected from:
- or a pharmaceutically acceptable salt thereof.
Dependencies are inferred from the claim text.