On May 10, 2013, Crawford, James John; Ortwine, Daniel Fred; Wei, Binqing; Young, Wendy B. published a patent.Application of 87486-34-8 The title of the patent was 8-Fluorophthalazin-1(2H)-one compounds as inhibitors of BTK activity and their preparation. And the patent contained the following:
8-Fluorophthalazin-1(2H)-one compounds of formula I, are provided, including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting BTH kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathol. conditions, are disclosed. Compounds of formula I wherein X1 is CR1 and N; X2 is CR2 and N; X3 is CR3 and N, provided that one or two of X1 – X3 are N; Y1 and Y2 are independently CH and N, provided that not both are N; R1, R2 and R3 are independently H, F, Cl, CN, Me, Et, etc.; R4 is F, F, Cl, CN, CH2OH, etc.; R6 is H, Me, Et, etc.; R8 is C6-20 aryl, C3-12 carbocyclyl, C1-20 heteroaryl, etc.; and stereoisomers, tautomers, or 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 BTK inhibitory activity. From the assay, it was determined that compound II exhibited IC70 value of 0.024 μM. The experimental process involved the reaction of 3,5-Dibromo-1-methylpyrazin-2(1H)-one(cas: 87486-34-8).Application of 87486-34-8
The Article related to fluorophthalazinone preparation btk inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Pyridazines, Cinnolines, and Phthalazines and other aspects.Application of 87486-34-8