- Patent Number:
11884,673
- Appl. No:
17/724601
- Application Filed:
April 20, 2022
- نبذة مختصرة :
Compounds useful in the modulation of ion channel activity in cells are disclosed herein. This disclosure also relates to use of these compounds in the treatment of pain, and pharmaceutical compositions containing these compounds and methods for their preparation.
- Inventors:
BIONOMICS LIMITED (Thebarton, AU)
- Assignees:
BIONOMICS LIMITED (Eastwood, AU)
- Claim:
1. A compound of formula (I) [chemical expression included] or a salt, stereoisomer, solvate or prodrug thereof, wherein R is an optionally substituted aryl, optionally substituted heterocycyl or optionally substituted heteroaryl; R 1 is H or an optionally substituted C 1 -C 4 alkyl; R 2 , R 3 , R 4 and R 5 are independently H or a C 1 -C 4 alkyl or R 2 and R 3 , or R 4 and R 5 together form a cycloalkyl ring; Y is selected from [chemical expression included] X is CH or N; and Z is F or CF 3 .
- Claim:
2. The compound of formula (I) according to claim 1 , [chemical expression included] or a salt, stereoisomer, solvate or prodrug thereof, wherein: R is an optionally substituted heteroaryl; R 1 is H or an optionally substituted C 1 -C 4 alkyl; R 2 , R 3 , R 4 and R 5 are independently H or a C 1 -C 4 alkyl, or R 2 and R 3 , or R 4 and R 5 together form a cycloalkyl ring; Y is selected from [chemical expression included] X is CH or N; and Z is F or CF 3 .
- Claim:
3. The compound of formula (I) according to claim 1 , [chemical expression included] or a salt, stereoisomer, solvate or prodrug thereof, wherein R is an optionally substituted 7-12 membered heteroaryl; R 1 is H or an optionally substituted C 1 -C 4 alkyl; R 2 , R 3 , R 4 and R 5 are independently H or a C 1 -C 4 alkyl, or R 2 and R 3 , or R 4 and R 5 together form a cycloalkyl ring; Y is selected from [chemical expression included] X is CH or N; and Z is F or CF 3 .
- Claim:
4. The compound of formula (I) according to claim 1 , [chemical expression included] or a salt, stereoisomer, solvate or prodrug thereof, wherein: R is an optionally substituted 7-12 membered heteroaryl with 2 or more N atoms; R 1 is H or an optionally substituted C 1 -C 4 alkyl; R 2 , R 3 , R 4 and R 5 are independently H or a C 1 -C 4 alkyl, or R 2 and R 3 , or R 4 and R 5 together form a cycloalkyl ring; Y is selected from [chemical expression included] X is CH or N; and Z is F or CF 3 .
- Claim:
5. The compound of formula (I) according to claim 1 , [chemical expression included] or a salt, stereoisomer, solvate or prodrug thereof, wherein: R is an optionally substituted 7-12 membered heteroaryl with 2 nitrogen atoms; R 1 is H or an optionally substituted C 1 -C 4 alkyl; R 2 , R 3 , R 4 and R 5 are independently H or a C 1 -C 4 alkyl, or R 2 and R 3 , or R 4 and R 5 together form a cycloalkyl ring; Y is selected from [chemical expression included] X is CH or N; and Z is F or CF 3 .
- Claim:
6. The compound according to claim 1 , wherein R 1 is H.
- Claim:
7. The compound according to claim 1 , wherein R 2 , R 3 , R 4 and R 5 are each H.
- Claim:
8. The compound according to any claim 1 , wherein Z is F.
- Claim:
9. The compound according to claim 1 , wherein Y is [chemical expression included]
- Claim:
10. The compound according to claim 1 , wherein Y is [chemical expression included] and X is CH or N.
- Claim:
11. The compound according to claim 10 , wherein X is CH.
- Claim:
12. The compound according to claim 1 , wherein R is selected from one of the following moieties: [chemical expression included] [chemical expression included]
- Claim:
13. The compound according to claim 1 , wherein R is selected from one of the following moieties: [chemical expression included]
- Claim:
14. A pharmaceutical composition comprising the compound according to claim 1 , together with a diluent or carrier adjuvant.
- Claim:
15. A method of manufacturing a medicament for treating pain disorders, said method comprising preparing a compound of formula (I) [chemical expression included] or a salt, stereoisomer, solvate or prodrug thereof, wherein: R is an optionally substituted aryl, optionally substituted heterocycyl or optionally substituted heteroaryl; R 1 is H or an optionally substituted C 1 -C 4 alkyl; R 2 , R 3 , R 4 and R 5 are independently H or a C 1 -C 4 alkyl or R 2 and R 3 , or R 4 and R 5 together form a cycloalkyl ring; Y is selected from [chemical expression included] X is CH or N; and Z is F or CF 3 .
- Claim:
16. The method according to claim 15 , wherein the pain disorder is selected from the group consisting of chronic pain, neuropathic pain, inflammatory pain, and cancer pain.
- Patent References Cited:
20100041694 February 2010 Takaishi
2248423 November 2010
2937335 October 2015
2008126684 October 2008
2013131018 September 2013
2018125968 July 2018
- Other References:
International Search Report and Written Opinion for PCT/AU2019/050472, dated Jul. 19, 2019, 16 pages. cited by applicant
Wei, C. et al., “Development of GLUT4-selective antagnoists for multiple myeloma therapy”, European Journal of Medicinal Chemistry (2017), 139, 573-586. cited by applicant
Database CA [Online], Database accession No. 2017:1384156, XP055845330. cited by applicant
- Primary Examiner:
Seaman, D Margaret M
- Attorney, Agent or Firm:
WARNER NORCROSS + JUDD LLP
- الرقم المعرف:
edspgr.11884673
Processing Request
No Comments.