On September 20, 2018, Bandiera, Tiziano; Bertozzi, Fabio; Di Fruscia, Paolo; Sorana, Federico; Berti, Francesco; Rodriguez Gimeno, Alejandra; Caci, Emanuela; Ferrera, Loretta; Pedemonte, Nicoletta; Vicente Galietta, Luis Juan published a patent.Category: pyrazoles-derivatives The title of the patent was Preparation of heterocyclic compounds for the treatment of cystic fibrosis. And the patent contained the following:
The invention relates to compounds of formula I or pharmaceutically acceptable salts or solvates thereof; their preparation an use to modulate CFTR protein or ABC protein activities. Compounds of formula I, wherein R1 is C1-6 alkyl, C3-6 cycloalkyl and hydroxy-C1-6 alkyl; Z is CO and SO2; X1, X2, X3 and X4 are independently CR and N; R is H, C1-6 alkyl, aryl, etc.; R2 is H, C1-6 alkyl, OH, CN, etc.; A1 , A2, A3 and A4 are independently O, CO, SO2, etc.; B is (un)substituted aromatic and heteroaromatic; n and m are independently 0, 1, 2; and pharmaceutically acceptable salts and solvates thereof, are claimed. Example compound II was prepared by cyclocondensation of 3-hydrazinobenzoic acid tert-Bu 4-oxo-3-(2,2,2-trifluoroacetyl)piperidine-1-carboxylate to give 3-[5-tert-butoxycarbonyl-3-(trifluoromethyl)-6,7-dihydro-4H-pyrazolo[4,3-c]pyridin-1-yl]benzoic acid, which underwent amidation with N-methyl-1,3-benzodioxol-5-amine hydrochloride to give II. The invention compounds were evaluated for their CFTR modulatory activity. From the assay, it was determined that compound II exhibited EC50 value of < 1 μM. The experimental process involved the reaction of 3-Methyl-1H-pyrazolo[3,4-b]pyridin-5-amine(cas: 1186608-73-0).Category: pyrazoles-derivatives
The Article related to heterocycle preparation cystic fibrosis cftr abc protein modulator, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazoles and other aspects.Category: pyrazoles-derivatives
Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics