On September 29, 2011, Brooks, Carl A.; Cheung, Mui; Eidam, Hilary S.; Fox, Ryan M.; Hilfker, Mark A.; Manas, Eric S.; Ye, Guosen published a patent.Recommanded Product: 141940-37-6 The title of the patent was 4-Quinolinecarboxamide derivatives as TRPV4 antagonists and their preparation and use for the treatment of diseases. And the patent contained the following:
The invention relates to 4-quinolinecarboxamide derivatives of formula I, which are TRPV4 antagonists and which are useful in the treatment of diseases. Compounds of formula I wherein R1 is C1-6 alkyl and C3-6 cycloalkyl; each R2 is independently OH, C1-4 alkoxy, C1-4 alkyl, etc.; R3 is (un)substituted morpholinyl, (un)substituted piperidinyl, (un)substituted pyrrolidinyl, etc.; each R4 is independently CF3, halo, C1-3 alkyl and C1-3 alkoxy; each R5 is independently (un)substituted 2-oxopyrrolidin-1-yl, halo, CN, etc.; two adjacent R5 taken together to form OCH2O and O(CH2)2O; each R6 is independently halo, Me and methoxy; X is N and CH; each n is independently 0 to 2; each p is independently 0 to 2; and pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by a multistep procedure (procedure given). All the invention compounds were evaluated for their TRPV4 antagonistic activity. From the assay, it was determined that all compounds exhibited IC50 values in the range from 1 nM to 10 μM. The experimental process involved the reaction of tert-Butyl (4-(trifluoromethyl)phenyl)carbamate(cas: 141940-37-6).Recommanded Product: 141940-37-6
The Article related to quinolinecarboxamide preparation trpv4 antagonist treatment disease, Heterocyclic Compounds (One Hetero Atom): Quinolines and Isoquinolines and other aspects.Recommanded Product: 141940-37-6
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