US2010273777A1PendingUtilityA1
Compounds for Modulating TRPV3 Function
Est. expiryMay 9, 2025(expired)· nominal 20-yr term from priority
Inventors:Jayhong A. ChongChristopher FangerGlenn R. LarsenWilliam C. Lumma, Jr.Magdalene M. MoranAmy RipkaDennis John UnderwoodManfred WeigeleXiaoguang Zhen
A61P 43/00A61P 9/14A61P 37/02A61P 3/10A61P 35/00A61P 25/14A61P 3/04A61P 3/00A61P 25/28A61P 25/06A61P 25/00A61P 25/02A61P 3/14A61P 29/02A61P 25/16A61P 29/00A61P 11/00A61P 21/04A61P 17/06A61P 17/02A61K 31/4709A61P 19/02A61P 1/02A61P 17/14A61K 9/0053A61P 11/06A61P 13/10C07D 409/04A61K 31/538A61K 31/506A61P 13/12A61K 9/0014A61P 17/00C07D 495/04A61P 11/14A61K 31/498A61P 17/04A61K 31/427A61P 1/04A61P 1/16C07D 215/54A61K 31/55A61K 31/47
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Claims
Abstract
The present application relates to compounds and methods for treating pain and other conditions related to TRPV3.
Claims
exact text as granted — not AI-modified1 - 70 . (canceled)
71 . A method for treating a condition for which reduced TRPV3 activity can reduce the severity, comprising administering to a subject in need thereof an effective amount of a compound that inhibits TRPV3-mediated current with an IC 50 of 1 micromolar or less.
72 . The method of claim 1 , wherein said compound inhibits at least 95% of TRPV3-mediated current at 5 micromolar or less.
73 . The method of claim 1 , wherein said compound inhibits TRPV3-mediated current with an IC 50 at least one order of magnitude lower than its IC 50 for inhibition of one or more of TRPC6, TRPV1, TRPV5, TRPV6, CaV 1.2, CaV 3.1, NaV 1.2, mitochondrial uniporter, and hERG.
74 . The method of claim 1 , wherein said compound inhibits TRPV3-mediated current with an IC 50 of 500 nanomolar or less.
75 . The method of claim 1 , wherein said compound inhibits TRPV3-mediated current with an IC 50 of 200 nanomolar or less.
76 . The method of claim 1 , wherein said compound inhibits TRPV3-mediated current with an IC 50 of 100 nanomolar or less.
77 . The method of claim 1 , wherein said compound inhibits TRPV3-mediated current with an IC 50 of 50 nanomolar or less.
78 . The method of claim 1 , wherein said compound is an organic molecule having a molecular weight of 2000 amu or less.
79 . The method of claim 1 , wherein said compound is administered topically.
80 . The method of claim 1 , wherein said compound is administered orally.
81 . The method of claim 1 , wherein said condition is acute pain, chronic pain, touch sensitivity, or itching sensitivity.
82 . The method of claim 1 , wherein said condition is post-surgical pain, cancer pain, or neuropathic pain.
83 . A method of modulating TRPV3 function in a cell, comprising administering to the cell an effective amount of a compound that inhibits TRPV3-mediated current with an IC so of 1 micromolar or less.
84 . The method of claim 13 , wherein said compound inhibits at least 95% of TRPV3-mediated current at 5 micromolar or less.
85 . The method of claim 13 , wherein said compound inhibits TRPV3-mediated current with an IC 50 at least one order of magnitude lower than its IC 50 for inhibition of one or more of TRPC6, TRPV1, TRPV5, TRPV6, CaV 1.2, CaV 3.1, NaV 1.2, mitochondrial uniporter, and hERG.
86 . The method of claim 13 , wherein said compound inhibits TRPV3-mediated current with an IC 50 of 500 nanomolar or less.
87 . The method of claim 13 , wherein said compound inhibits TRPV3-mediated current with an IC 50 of 200 nanomolar or less.
88 . The method of claim 13 , wherein said compound inhibits TRPV3-mediated current with an IC 50 of 100 nanomolar or less.
89 . The method of claim 13 , wherein said compound inhibits TRPV3-mediated current with an IC 50 of 50 nanomolar or less.
90 . The method of claim 13 , wherein said compound is an organic molecule having a molecular weight of 2000 amu or less.Join the waitlist — get patent alerts
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