US2016220540A1PendingUtilityA1
Compositions, formulations and methods for treating ocular diseases
Est. expiryMar 15, 2033(~6.6 yrs left)· nominal 20-yr term from priority
A61K 38/179A61K 31/428A61K 39/395C07D 417/04C07D 277/60C07D 277/30A61K 2039/54C07D 277/56C07K 16/22A61K 47/40A61K 47/26A61K 31/433A61K 31/426A61K 2039/505A61K 31/513A61K 31/496C07D 277/64A61K 31/427A61P 27/00A61K 39/3955A61K 47/6951A61K 31/506A61K 31/538A61K 9/0019A61K 31/497A61K 9/0051A61P 27/02C07D 417/12A61K 31/4439C07D 277/28
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Claims
Abstract
Disclosed herein are compounds effective for activation of Tie-2 and inhibition of HPTP-beta. The compounds can provide effective therapy for conditions associated with angiogenesis, for example, ocular conditions. Formulations for increased solubility are disclosed. Combination therapy with antibodies and PK/PD data are also disclosed.
Claims
exact text as granted — not AI-modified1 - 54 . (canceled)
55 . A method of treating a condition, the method comprising administering to a subject in need thereof:
a) a therapeutically-effective amount of a Tie-2 activator or a pharmaceutically-acceptable salt thereof; and b) a therapeutically-effective amount of an anti-VEGF binding agent.
56 . The method of claim 55 , wherein the Tie-2 activator binds a phosphatase.
57 . The method of claim 55 , wherein the Tie-2 activator inhibits a phosphatase.
58 . The method of claim 55 , wherein the Tie-2 activator is:
or a pharmaceutically-acceptable salt thereof.
59 . The method of claim 55 , wherein the Tie-2 activator is:
or a pharmaceutically-acceptable salt thereof.
60 . The method of claim 55 , wherein the Tie-2 activator is:
or a pharmaceutically-acceptable salt thereof.
61 . The method of claim 55 , wherein the Tie-2 activator is:
or a pharmaceutically-acceptable salt thereof.
62 . The method of claim 55 , wherein the Tie-2 activator is:
or a pharmaceutically-acceptable salt thereof.
63 . The method of claim 55 , wherein the Tie-2 activator is:
or a pharmaceutically-acceptable salt thereof.
64 . The method of claim 55 , wherein the Tie-2 activator is:
or a pharmaceutically-acceptable salt thereof.
65 . The method of claim 55 , wherein the Tie-2 activator is:
or a pharmaceutically-acceptable salt thereof.
66 . The method of claim 55 , wherein the Tie-2 activator is:
or a pharmaceutically-acceptable salt thereof.
67 . The method of claim 55 , wherein the Tie-2 activator is:
or a pharmaceutically-acceptable salt thereof.
68 . The method of claim 55 , wherein the Tie-2 activator is:
or a pharmaceutically-acceptable salt thereof.
69 . The method of claim 55 , wherein the Tie-2 activator is:
or a pharmaceutically-acceptable salt thereof.
70 . The method of claim 55 , wherein the Tie-2 activator is:
or a pharmaceutically-acceptable salt thereof.
71 . The method of claim 55 , wherein the Tie-2 activator is:
or a pharmaceutically-acceptable salt thereof.
72 . The method of claim 55 , wherein the Tie-2 activator is:
or a pharmaceutically-acceptable salt thereof.
73 . The method of claim 55 , wherein the Tie-2 activator is:
or a pharmaceutically-acceptable salt thereof.
74 . The method of claim 55 , wherein the Tie-2 activator is:
or a pharmaceutically-acceptable salt thereof.
75 . The method of claim 55 , wherein the Tie-2 activator is:
or a pharmaceutically-acceptable salt thereof.
76 . The method of claim 55 , wherein the Tie-2 activator is:
or a pharmaceutically-acceptable salt thereof.
77 . The method of claim 55 , wherein the Tie-2 activator is:
or a pharmaceutically-acceptable salt thereof.
78 . The method of claim 55 , wherein the Tie-2 activator is:
or a pharmaceutically-acceptable salt thereof.
79 . The method of claim 55 , wherein the Tie-2 activator is:
or a pharmaceutically-acceptable salt thereof.
80 . The method of claim 55 , wherein the Tie-2 activator is:
or a pharmaceutically-acceptable salt thereof.
81 . The method of claim 55 , wherein the therapeutically-effective amount of the Tie-2 activator is about 5 mg to about 60 mg.
82 . The method of claim 55 , wherein the therapeutically-effective amount of the Tie-2 activator is about 15 mg.
83 . The method of claim 55 , wherein the therapeutically-effective amount of the Tie-2 activator is about 30 mg.
84 . The method of claim 55 , wherein the therapeutically-effective amount of the anti-VEGF binding agent is about 0.5 mg to about 50 mg.
85 . The method of claim 55 , wherein the anti-VEGF binding agent is ranibizumab.
86 . The method of claim 85 , wherein the therapeutically-effective amount of ranibizumab is about 0.05 mg to about 1.5 mg.
87 . The method of claim 55 , wherein the anti-VEGF binding agent is bevacizumab.
88 . The method of claim 87 , wherein the therapeutically-effective amount of bevacizumab is about 0.1 mg to about 5 mg.
89 . The method of claim 55 , wherein the anti-VEGF binding agent is aflibercept.
90 . The method of claim 89 , wherein the therapeutically-effective amount of aflibercept is about 0.05 mg to about 5 mg.
91 . The method of claim 55 , wherein the administration is intravitreal.
92 . The method of claim 55 , wherein the administration is subcutaneous.
93 . The method of claim 55 , wherein the subject is human.
94 . The method of claim 55 , wherein the condition is an ocular condition.
95 . The method of claim 55 , wherein the condition is diabetic macular edema.
96 . The method of claim 55 , wherein the condition is diabetic retinopathy.
97 . The method of claim 55 , wherein the condition is macular degeneration.
98 . The method of claim 55 , wherein the condition is vascular leak.
99 . The method of claim 55 , wherein the condition is glaucoma.
100 . The method of claim 55 , wherein the condition is cancer.
101 . A method of treating a condition, the method comprising administering to a subject in need thereof:
a) a therapeutically-effective amount of a HPTP-β binding agent or a pharmaceutically-acceptable salt thereof; and b) a therapeutically-effective amount of an anti-VEGF binding agent.
102 . The method of claim 101 , wherein the HPTP-β binding agent is an inhibitor of HPTP-β.
103 . The method of claim 101 , wherein the HPTP-β binding agent inhibits a phosphatase.
104 . The method of claim 101 , wherein the HPTP-β binding agent is:
or a pharmaceutically-acceptable salt thereof.
105 . The method of claim 101 , wherein the HPTP-β binding agent is:
or a pharmaceutically-acceptable salt thereof.
106 . The method of claim 101 , wherein the HPTP-β binding agent is:
or a pharmaceutically-acceptable salt thereof.
107 . The method of claim 101 , wherein the HPTP-β binding agent is:
or a pharmaceutically-acceptable salt thereof.
108 . The method of claim 101 , wherein the HPTP-β binding agent is:
or a pharmaceutically-acceptable salt thereof.
109 . The method of claim 101 , wherein the HPTP-β binding agent is:
or a pharmaceutically-acceptable salt thereof.
110 . The method of claim 101 , wherein the HPTP-β binding agent is:
or a pharmaceutically-acceptable salt thereof.
111 . The method of claim 101 , wherein the HPTP-β binding agent is:
or a pharmaceutically-acceptable salt thereof.
112 . The method of claim 101 , wherein the HPTP-β binding agent is:
or a pharmaceutically-acceptable salt thereof.
113 . The method of claim 101 , wherein the HPTP-β binding agent is:
or a pharmaceutically-acceptable salt thereof.
114 . The method of claim 101 , wherein the HPTP-β binding agent is:
or a pharmaceutically-acceptable salt thereof.
115 . The method of claim 101 , wherein the HPTP-β binding agent is:
or a pharmaceutically-acceptable salt thereof.
116 . The method of claim 101 , wherein the HPTP-β binding agent is:
or a pharmaceutically-acceptable salt thereof.
117 . The method of claim 101 , wherein the HPTP-β binding agent is:
or a pharmaceutically-acceptable salt thereof.
118 . The method of claim 101 , wherein the HPTP-β binding agent is:
or a pharmaceutically-acceptable salt thereof.
119 . The method of claim 101 , wherein the HPTP-β binding agent is:
or a pharmaceutically-acceptable salt thereof.
120 . The method of claim 101 , wherein the HPTP-β binding agent is:
or a pharmaceutically-acceptable salt thereof.
121 . The method of claim 101 , wherein the HPTP-β binding agent is:
or a pharmaceutically-acceptable salt thereof.
122 . The method of claim 101 , wherein the HPTP-β binding agent is:
or a pharmaceutically-acceptable salt thereof.
123 . The method of claim 101 , wherein the HPTP-β binding agent is:
or a pharmaceutically-acceptable salt thereof.
124 . The method of claim 101 , wherein the HPTP-β binding agent is:
or a pharmaceutically-acceptable salt thereof.
125 . The method of claim 101 , wherein the HPTP-β binding agent is:
or a pharmaceutically-acceptable salt thereof.
126 . The method of claim 101 , wherein the HPTP-β binding agent is:
or a pharmaceutically-acceptable salt thereof.
127 . The method of claim 101 , wherein the therapeutically-effective amount of the HPTP-β binding agent is about 5 mg to about 60 mg.
128 . The method of claim 101 , wherein the therapeutically-effective amount of the HPTP-β binding agent is about 15 mg.
129 . The method of claim 101 , wherein the therapeutically-effective amount of the HPTP-β binding agent is about 30 mg.
130 . The method of claim 101 , wherein the therapeutically-effective amount of the anti-VEGF binding agent is about 0.5 mg to about 50 mg.
131 . The method of claim 101 , wherein the anti-VEGF binding agent is ranibizumab.
132 . The method of claim 131 , wherein the therapeutically-effective amount of ranibizumab is about 0.05 mg to about 1.5 mg.
133 . The method of claim 101 , wherein the anti-VEGF binding agent is bevacizumab.
134 . The method of claim 133 , wherein the therapeutically-effective amount of bevacizumab is about 0.1 mg to about 5 mg.
135 . The method of claim 101 , wherein the anti-VEGF binding agent is aflibercept.
136 . The method of claim 135 , wherein the therapeutically-effective amount of aflibercept is about 0.05 mg to about 5 mg.
137 . The method of claim 101 , wherein the administration is intravitreal.
138 . The method of claim 101 , wherein the administration is subcutaneous.
139 . The method of claim 101 , wherein the subject is human.
140 . The method of claim 101 , wherein the condition is an ocular condition.
141 . The method of claim 101 , wherein the condition is diabetic macular edema.
142 . The method of claim 101 , wherein the condition is diabetic retinopathy.
143 . The method of claim 101 , wherein the condition is macular degeneration.
144 . The method of claim 101 , wherein the condition is vascular leak.
145 . The method of claim 101 , wherein the condition is glaucoma.
146 . The method of claim 101 , wherein the condition is cancer.Join the waitlist — get patent alerts
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