On November 26, 2021, Yang, Anyue; Ji, Sen; Wang, Hao; Zhang, Dewei; Wang, Xiao; Wang, Zhi; Shen, Huan; Li, Zhiyong; Qian, Xinying published a patent.Application In Synthesis of 1-(4-Methoxybenzyl)-1H-pyrazolo[3,4-b]pyridin-4-ol The title of the patent was Transforming growth factor receptor antagonist for treating diseases mediated by TGF-β overexpression and preparation method thereof. And the patent contained the following:
The invention relates to the transforming growth factor receptor antagonists with general formula I for treating diseases mediated by TGF-β overexpression and the preparation method thereof [where L1=O, NH; L2=absent or NH; R1=absent or five membered heteroaromatic ring; R2=ethyl, tert Bu, tetrahydropyran-4-yl, tetrahydrofuran-3-yl, cyclopropyl or cyclobutyl; R3=cyclopropyl, Et, iso-Pr, CHF2, CH2CHF2, CH2CF3; R4=F, Cl, H; X1, X2, X3=CH, N; X4=N, -CRa, where Ra=H, alkyl, alkenyl, alkynyl, alkoxy, hydroxyalkyl and hydroxyl substituted alkynyl, hydroxyl substituted alkenyl, C3-C6 cycloalkyl, C3-C6 cycloalkenyl, C3-C6 heterocyclic], which has the use of treating and/or preventing a variety of diseases mediated by ALK5. For example, compound2-(4-((4-((3-cyclopropyl-1-(tetrahydro-2H-pyran-4-yl)-1H-pyrazole-5-yl)oxy)pyridin-2-yl)amino)pyridin-2-yl)propyl-2-ol was prepared by multi-step reaction with tetrahydro-4H-pyran-4-one, tert-Bu carbazate, Et 3-cyclopropyl-3-oxopropionate, 2-chloro-4-fluoropyridine and 2-(4-aminopyridin-2-yl)propan-2-ol. The title compound can be used to prepare drugs for treating diseases mediated by TGF-β overexpression. The experimental process involved the reaction of 1-(4-Methoxybenzyl)-1H-pyrazolo[3,4-b]pyridin-4-ol(cas: 924909-16-0).Application In Synthesis of 1-(4-Methoxybenzyl)-1H-pyrazolo[3,4-b]pyridin-4-ol
The Article related to transforming growth factor beta overexpression receptor antagonist preparation, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazoles and other aspects.Application In Synthesis of 1-(4-Methoxybenzyl)-1H-pyrazolo[3,4-b]pyridin-4-ol
Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics