10-06-2021 дата публикации
Номер: US20210171454A1
Novel diphenylurea and benzylbenzenesulfonamide compounds are disclosed along with methods of inhibiting the activity of TRPV1 and methods of treating pain associated with transient receptor potential vanilloid type 1 (TRPV1) using such compounds 111.-. (canceled)13. (canceled)14. (canceled)15. The method of claim 12 , wherein Z is N(R′)or NOand a is an integer of 1 to 5; and b is an integer of 0 to 4.16. The method of claim 12 , wherein:{'sub': 1', '6', '1', '6', '1', '6', '1', '6, 'X is independently in each instance halogen, C-Calkyl, C-Cperfluoroalkyl, NHC(O)—C-Calkyl, NHC(O)—C-Cperfluoroalkyl;'}{'sub': 1', '6, 'Y is independently in each instance halogen, C-Calkyl;'}{'sub': 2', '2, 'Z is N(R′)or NO;'}{'sub': 1', '6, 'R is independently in each instance H or C-Calkyl;'}{'sub': 1', '6', '1', '6, 'R′ is independently in each instance H, C-Calkyl, or C-Cperfluoroalkyl;'}a is an integer of 1 to 5; andb is an integer of 0 to 4,wherein the alkyl moieties are optionally substituted by one or more halogen,or a pharmaceutically acceptable salt or solvate thereof.17. The method of claim 12 , wherein a and b are each independently an integer of 1 to 3.18. The method of claim 12 , wherein a and b are one.19. The method of claim 12 , wherein X is fluoro claim 12 , C-Calkyl or C-Cperfluoroalkyl and a is 1.20. The method of claim 12 , wherein Y is a C-Calkyl and b is 1.21. The method of claim 12 , wherein R is H.22. The method of claim 12 , wherein Z is NO.23. The method of claim 12 , wherein the pain associated with TRPV1 is selected from the group consisting of osteoarthritis claim 12 , neuropathic pain claim 12 , migraine claim 12 , inflammatory bowel disease claim 12 , and bone cancer pain.25. The method of claim 24 , wherein Z is N(R′)or NOand a is an integer of 1 to 5; and b is an integer of 0 to 4.27. The method of claim 24 , wherein a and b are each independently an integer of 1 to 3.28. The method of claim 24 , wherein a and b are one.29. The method of claim 24 , ...
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