OCULOSELECTIVE DRUGS AND PRODRUGS
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Accused Products
Abstract
Compounds of the following formula are disclosed:
Methods of preparing the compounds, pharmaceutical compositions comprising the compounds, and methods of treating patients by administration of the pharmaceutical compositions are disclosed.
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Citations
62 Claims
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1-19. -19. (canceled)
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20. A compound of Formula II:
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wherein; R1 and R2 are each independently H, W, or a phenoxyl protecting group; R3 is hydrogen, straight chain or branched C1-C10 alkyl, cycloalkyl, amino, C1-C10 alkoxy, —
NHC(═
O)Ra, or —
C(═
O)N(H)Ra;Ra is alkyl, aryl, or heterocyclyl; R4 is H or W; Z is —
O—
or —
O(C═
O)—
;R5 is H, straight chain or branched C1-C10 alkyl, cycloalkyl, C1-C10 alkoxyalkyl, amino, benzyl, tetrahydrofuranyl, dihydrofuranyl, furanyl, morpholinyl, piperidinyl, tetrahydropyranyl, dioxolanyl, 2,2-dimethyl dioxolanyl, dioxanyl, pyrrolyl, pyrrolidinyl, tetrahydrooxazolyl, dihydrooxazolyl, phenyl, phenyl substituted with C1-C10 alkyl, C1-C10 alkoxy, or halo, or cycloalkyl substituted with at least one straight or branched C1-C10 alkyl; W is; each R6 is independently H, straight chain or branched C1-C10 alkyl, or straight chain or branched C1-C10 alkoxyalkyl; and R7 is straight chain or branched alkyl, cycloalkyl, aryl, or aralkyl; provided that; when Z is —
O(C═
O)—
, then R5 is other than H;or a stereoisomer, hydrate, solvate, acid salt hydrate, or pharmaceutically acceptable salt thereof. - View Dependent Claims (21, 22, 24, 25, 29, 30, 31, 32, 33, 34, 36, 37, 38, 39, 40, 42, 59, 60, 62)
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25. A compound according to claim 20, wherein R4 is W.
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29. A compound according to claim 25 wherein R1 and R2 are each aralkyl.
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30. A compound according to claim 25 wherein R4 is:
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31. A compound according to claim 20, wherein at least one of the R6 substituents is other than H.
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32. A compound according to claim 20, wherein each R6 is independently H, C1-C5 alkyl or lower alkoxyalkyl.
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33. A compound according to claim 20, wherein each R6 is independently H, methyl, or CH2OCH3.
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34. A compound according to claim 20, wherein each W is independently:
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36. A compound according to claim 20 wherein R3 is H or C1-C5 alkyl.
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37. A compound according to claim 20 wherein R3 is methyl.
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38. A compound according to claim 20, wherein R5 is furanyl, dihydrofuranyl, or tetrahydrofuranyl.
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39. A compound according to claim 38, wherein R5 is tetrahydrofuran-3-yl.
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40. A compound according to claim 20, wherein W is:
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42. A compound according to claim 20, wherein R5 is 3-alkyltetrahydrofuran-3-yl.
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59. A method of treating glaucoma, wherein the glaucoma, ocular hypertension, or optic neuropathy associated with the eye of a patient, wherein the method comprises administering to the eye of the patient a composition comprising an opthalmologically acceptable carrier or diluent and a compound according to claim 20, or a stereoisomer, hydrate, solvate, acid salt hydrate, or pharmaceutically acceptable salt thereof, in a therapeutically sufficient amount to ameliorate, delay, or prevent the development of, or reduce the symptoms of glaucoma, wherein the glaucoma, ocular hypertension, or optic neuropathy.
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60. The method according to claim 59, wherein the glaucoma, ocular hypertension, or optic neuropathy is classified as open-angle glaucoma.
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62. The method according to claim 59, wherein the composition is administered from a polymeric disk or wafer placed upon the surface of the eye.
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23. (canceled)
- 26. (canceled)
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28. (canceled)
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35. (canceled)
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41. (canceled)
- 43. (canceled)
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46-58. -58. (canceled)
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61. (canceled)
Specification