US2012010416A1PendingUtilityA1
Pyrrolidinone benzenesulfonamide derivatives as modulators of ion channels for the treatment of pain
Est. expiryNov 13, 2027(~1.3 yrs left)· nominal 20-yr term from priority
Inventors:Dean StamosEsther MartinboroughNicole ZimmermannTimothy NeubertMehdi Michel Djamel NumaTara WhitneyAarti Sameer Kawatkar
A61P 9/06A61P 9/12A61P 9/10A61P 25/28A61P 25/00A61P 25/04A61P 25/22A61P 25/08A61P 25/24A61P 25/18A61P 29/00A61P 25/06C07D 417/14A61P 19/02A61P 1/04
48
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Claims
Abstract
The present invention relates to heterocyclic derivatives useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.
Claims
exact text as granted — not AI-modified1 . A compound of formula I:
or a pharmaceutically acceptable salt thereof,
wherein, independently for each occurrence:
ring Z is a thiazole or thiadiazole optionally substituted with 0-2 occurrences of R;
V is CH 2 ; and
R, R 1 , R 2 , and R 3 are hydrogen, C1-C6 aliphatic, aryl, C3-C8 cycloaliphatic, halo, CN, NO 2 , CF 3 , OCF 3 , OH, NH 2 , NH(C1-C6 aliphatic), N(C1-C6 aliphatic) 2 , COOH, COO(C1-C6 aliphatic), O(C1-C6 aliphatic), CHF 2 , or CH 2 F.
2 . The compound of claim 1 , wherein Z is
3 . The compound of claim 1 , wherein Z is
4 . The compound of claim 1 , wherein R 1 , R 2 , and R 3 are hydrogen, C1-C6 aliphatic, halo, or CF 3 .
5 . The compound of claim 1 , wherein Z is
and R 1 , R 2 , and R 3 are hydrogen, C1-C6 aliphatic, halo, or CF 3 .
6 - 7 . (canceled)
8 . The compound of claim 1 , wherein at least two of R 1 , R 2 , or R 3 are halo.
9 . The compound of claim 1 , wherein R 1 , R 2 , and R 3 are H or Cl.
10 . The compound of claim 1 , wherein Z is
.
11 . (canceled)
12 . The compound of claim 1 , wherein Z is
and R 1 and R 3 are Cl.
13 . The compound of claim 1 , wherein Z is
and R 1 and R 2 are Cl.
14 . A compound of formula Ia:
or a pharmaceutically acceptable salt thereof,
wherein, independently for each occurrence:
ring Z is a thiazole or thiadiazole optionally substituted with 0-2 occurrences of R;
V is CH 2 ; and
R, R 1 , R 2 , and R 3 are hydrogen, C1-C6 aliphatic, aryl, C3-C8 cycloaliphatic, halo, CN, NO 2 , CF 3 , OCF 3 , OH, NH 2 , NH(C1-C6 aliphatic), N(C1-C6 aliphatic) 2 , COOH, COO(C1-C6 aliphatic), O(C1-C6 aliphatic), CHF 2 , or CH 2 F.
15 . The compound of claim 14 , wherein Z is
16 . The compound of claim 14 , wherein R 1 , R 2 , and R 3 are hydrogen, C1-C6 aliphatic, halo, or CF 3 .
17 - 18 . (canceled)
19 . The compound of claim 14 , wherein at least two of R 1 , R 2 , or R 3 are halo.
20 . The compound of claim 14 , wherein R 1 , R 2 , and R 3 are H or Cl.
21 . The compound of claim 14 wherein the compound is
22 . A compound of formula Ib:
or a pharmaceutically acceptable salt thereof,
wherein, independently for each occurrence:
ring Z is a thiazole or thiadiazole optionally substituted with 0-2 occurrences of R;
V is CH 2 ; and
R, R 1 , R 2 , and R 3 are hydrogen, C1-C6 aliphatic, aryl, C3-C8 cycloaliphatic, halo, CN, NO 2 , CF 3 , OCF 3 , OH, NH 2 , NH(C1-C6 aliphatic), N(C1-C6 aliphatic) 2 , COOH, COO(C1-C6 aliphatic), O(C1-C6 aliphatic), CHF 2 , or CH 2 F.
23 . The compound of claim 22 , wherein Z is
24 . The compound of claim 22 , wherein R 1 , R 2 , and R 3 are hydrogen, C1-C6 aliphatic, halo, or CF 3 .
25 - 26 . (canceled)
27 . The compound of claim 22 , wherein at least two of R 1 , R 2 , or R 3 are halo.
28 . The compound of claim 22 , wherein R 1 , R 2 , and R 3 are H or Cl.
29 . The compound of claim 22 wherein the compound is
30 . A pharmaceutical composition comprising a compound of claim 1 and a pharmaceutically acceptable carrier.
31 - 32 . (canceled)Cited by (0)
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