US2013059869A1PendingUtilityA1
Methods and compositions for treating disorders
Est. expiryJun 22, 2027(~0.9 yrs left)· nominal 20-yr term from priority
Inventors:Howard P. NgManfred WeigeleMagdalene M. MoranJayhong A. ChongChristopher FangerGlenn R. LarsenDonato Del CaminoNeil J. HaywardSteven P. AdamsAmy Ripka
A61P 17/06C07D 473/08A61P 29/00A61P 25/06A61K 31/105C07D 473/04A61K 31/11C07D 487/04A61K 31/522
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Claims
Abstract
Compounds and compositions for treating disorders related to TRPA1 are described herein.
Claims
exact text as granted — not AI-modified1 . A method of treating pain, the method comprising administering a compound of formula (VIII), or a pharmaceutically acceptable salt thereof:
wherein,
each of R 1 and R 2 is independently, C 1 -C 6 alkyl;
L is C(O)NR 6 ;
R 3a is an optionally substituted nitrogen-containing heteroaryl,
R 3b is aryl or heteroaryl, each of which is optionally substituted with 1-4 R 7 ;
R 6 is H;
each R 7 is independently heterocyclyl, which is optionally substituted with 1-3 R 8 ;
each R 8 is independently C 1 -C 6 alkyl;
R 9 is H; and
m is 1,
provided that the compound is not a compound depicted in Table 2.
2 . The method of claim 1 , wherein R 3a is pyridyl.
3 . The method of claim 1 , wherein R 3b is phenyl.
4 . The method of claim 1 , wherein R 1 and R 2 are both methyl.
5 . The method of claim 1 , wherein R 3b is substituted with 1-4 R 7 .
6 . The method of claim 1 , wherein R 8 is methyl.
7 . The method of claim 1 , wherein the pain is acute pain.
7 . The method of claim 1 , wherein the pain is chronic pain.
8 . The method of claim 1 , wherein the pain is post-operative pain.
9 . A method of inhibiting a TRPA1 channel in a sample, wherein the sample comprises one or more TRPA1 channels, comprising contacting the sample with a compound of formula (VIII), or a pharmaceutically acceptable salt thereof:
wherein,
each of R 1 and R 2 is independently, C 1 -C 6 alkyl;
L is C(O)NR 6 ;
R 3a is an optionally substituted nitrogen-containing heteroaryl,
R 3b is aryl or heteroaryl, each of which is optionally substituted with 1-4 R 7 ;
R 6 is H;
each R 7 is independently heterocyclyl, which is optionally substituted with 1-3 R 8 ;
each R 8 is independently C 1 -C 6 alkyl;
R 9 is H; and
m is 1,
provided that the compound is not a compound depicted in Table 2.
10 . The method of claim 9 , wherein R 3a is pyridyl.
11 . The method of claim 9 , wherein R 3b is phenyl.
12 . The method of claim 9 , wherein R 1 and R 2 are both methyl.
13 . The method of claim 9 , wherein R 3b is substituted with 1-4 R 7 .
14 . The method of claim 9 , wherein R 8 is methyl.
15 . The method of claim 9 , wherein the TRPA1 channel comprises a TRPA1 protein comprising an amino acid sequence selected from SEQ ID NO: 1, SEQ ID NO: 3, and SEQ ID NO: 5.
16 . The method of claim 9 , wherein the TRPA1 channel comprises a TRPA1 protein comprising at least 80% of an amino acid sequence selected from SEQ ID NO: 1, SEQ ID NO: 3, and SEQ ID NO: 5, and retaining a function of TRPA1.
17 . The method of claim 9 , wherein the sample comprises a cell or a cell culture.
18 . The method of claim 9 , wherein the sample comprises a membrane.
19 . A method of selectively inhibiting a TRPA1 channel in a sample, wherein the sample comprises one or more TRPA1 channels and one or more non-TRPA1 channels, comprising contacting the sample with a compound of formula (VIII), or a pharmaceutically acceptable salt thereof:
wherein,
each of R 1 and R 2 is independently, C 1 -C 6 alkyl;
L is C(O)NR 6 ;
R 3a is an optionally substituted nitrogen-containing heteroaryl,
R 3b is aryl or heteroaryl, each of which is optionally substituted with 1-4 R 7 ;
R 6 is H;
each R 7 is independently heterocyclyl, which is optionally substituted with 1-3 R 8 ;
each R 8 is independently C 1 -C 6 alkyl;
R 9 is H; and
m is 1,
provided that the compound is not a compound depicted in Table 2.
20 . The method of claim 19 , wherein the non-TRPA1 channel is selected from Na V 1.2, Ca V 1.2, Ca V 3.1, HERG, and mitochondrial uniporter.
21 . The method of claim 19 , wherein the non-TRPA1 channel is selected from TRPC6, TRPV5, TRPV6, TRPM8, TRPV1, TRPV2, TRPV4 and TRPV3.Join the waitlist — get patent alerts
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