Category: 924909-16-0

On June 13, 2013, Houze, Jonathan B.; Dransfield, Paul; Pattaropong, Vatee; Du, Xiaohui; Fu, Zice; Lai, Sujen; Park, Jaehyeon; Jiao, Xianyun; Kohn, Todd J.; Aicher, Thomas Daniel; Boyd, Steven Armen; Bencsik, Josef; Condroski, Kevin Ronald; Hinklin, Ronald Jay; Kraser, Christopher F.; Pratt, Scott; Singh, Ajay; Wenglowsky, Steven Mark; Boys, Mark Laurence; Chicarelli, Mark Joseph; Mohr, Peter J.; Cardozo, Mario G. published a patent.Reference of 1-(4-Methoxybenzyl)-1H-pyrazolo[3,4-b]pyridin-4-ol The title of the patent was Urea compounds as GKa activators and their preparation. And the patent contained the following:

The invention relates to urea compounds of formula I, to pharmaceutical compositions comprising the compounds, to a process for making the compounds and to the use of the compounds in the treatment of diseases and disorders that would benefit from activation of glucokinase. Compounds of formula I wherein R1 is H, alkyl, alkenyl, haloalkyl, etc.; R2 is H, alkyl and halo; R3 is H, halo, alkoxycarbonyl, etc.; G is C and N; P is H and LR6; L is O, S, CH2 and CH2O; R6 is aryl aralkyl, heterocyclyl, etc.; and with proviso; 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 glucokinase activation activity (data given). The experimental process involved the reaction of 1-(4-Methoxybenzyl)-1H-pyrazolo[3,4-b]pyridin-4-ol(cas: 924909-16-0).Reference of 1-(4-Methoxybenzyl)-1H-pyrazolo[3,4-b]pyridin-4-ol

The Article related to pyridinyl urea preparation glucokinase activator, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.Reference of 1-(4-Methoxybenzyl)-1H-pyrazolo[3,4-b]pyridin-4-ol

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

On July 16, 2009, Blake, James; Gunawardana, Indrani W.; Le Huerou, Yvan; Mohr, Peter J.; Wallace, Eli M.; Wang, Bin published a patent.Computed Properties of 924909-16-0 The title of the patent was Pyrazolopyridine derivatives and their pharmaceutical compositions as CHK1 and CHK2 kinase inhibitors for the treatment of various diseases and preparation thereof. And the patent contained the following:

Title compounds I and II, their pharmaceutical compositions, and their pharmaceutically acceptable salts, are prepared and disclosed as inhibitors of CHK1 and CHK2 kinases and useful in the treatment of diseases mediated by said kinases. Compounds of formula I [m, n, p independently = 0 or 1; G = (un)substituted Ph when m = 1, or G = absent, alkyl, or (un)substituted Ph when m = 0; R1 = H, alkyl, haloalkyl, etc.; R2 = H, CF3, (un)substituted alkenyl, etc., with the provision that when R1 = H, then R2 = OR14; R14 = alkyl optionally substituted with 1 or more OH; R3, R7, and R8 independently = H or alkyl; R5, R6, and R9 independently = H or Me] and II [Q = CH2 or CH2CH2; R15 and R16 independently = H or alkyl], their pharmaceutical compositions, and their pharmaceutically acceptable salts, are claimed. For example, compound III·2HCl was prepared via amidation of (S)-3-(tert-butoxycarbonyl(isopropyl)amino)-2-(4-chlorophenyl)propanoic acid with 5-phenyl-4-(piperazin-1-yl)-1H-pyrazolo[3,4-b]pyridine dihydrochloride, followed by removal of the BOC protecting group. Select I and II were assayed for CHK1 kinase activity and found to possess IC50 values of <10 μM. The experimental process involved the reaction of 1-(4-Methoxybenzyl)-1H-pyrazolo[3,4-b]pyridin-4-ol(cas: 924909-16-0).Computed Properties of 924909-16-0

The Article related to pyrazolopyridine derivative preparation chk1 chk2 kinase inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazoles and other aspects.Computed Properties of 924909-16-0

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

On March 5, 2020, Hinklin, Ronald Jay; Allen, Shelley; Barbour, Patrick; Cook, Adam; Dahlke, Joshua; Gaudino, John; Laird, Ellen; Mcnulty, Oren T.; Zhao, Qian published a patent.Quality Control of 1-(4-Methoxybenzyl)-1H-pyrazolo[3,4-b]pyridin-4-ol The title of the patent was Pyrazolo[3,4-b]pyridine compounds as inhibitors of TAM and MET kinases and their preparation. And the patent contained the following:

Provided herein are compounds of the formula I and stereoisomers, tautomers and pharmaceutically acceptable salts thereof, which are inhibitors of one or more TAM kinases and/or c-Met kinase, and are useful in the treatment and prevention of diseases which can be treated with a TAM kinase inhibitor and/or a c-Met kinase inhibitor. Compounds of formula I wherein X1 is CH2 and N; R1 is H and C1-6 alkyl; R2 is H, C1-6 alkyl, C1-6 hydroxyalkyl, (un)substituted 3- to 4-membered cycloalkyl, etc.; R9 is H and halo; G is (un)substituted 5- to 6-membered oxoheterocyclyl and (un)substituted oxoquinolinyl; and stereoisomers, tautomers and pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by N-(3-fluoro-4-((3-iodo-1-(4-methoxybenzyl)-lH-pyrazolo[3,4-b]pyridin-4-yl)oxy)phenyl)-2-(4-fluorophenyl)-3-oxo-2,3-dihydropyridazine-4-carboxamide with ethanolamine; the resulting N-(3-fluoro-4-((3-((2-hydroxyethyl)amino)-1-(4-methoxybenzyl)-1H-pyrazolo[3,4-b]pyridin-4-yl)oxy)phenyl)-2-(4-fluorophenyl)-3-oxo-2,3-dihydropyridazine-4-carboxamide underwent hydrolysis to give compound II. The invention compounds were evaluated for their TAM and MET kinase inhibitory activity (data given). The experimental process involved the reaction of 1-(4-Methoxybenzyl)-1H-pyrazolo[3,4-b]pyridin-4-ol(cas: 924909-16-0).Quality Control of 1-(4-Methoxybenzyl)-1H-pyrazolo[3,4-b]pyridin-4-ol

The Article related to pyrazolopyridine preparation tam met kinase inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazoles and other aspects.Quality Control of 1-(4-Methoxybenzyl)-1H-pyrazolo[3,4-b]pyridin-4-ol

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

On May 24, 2018, Gavrilov, Aleksey Sergeevich; Aleshunin, Pavel Aleksandrovich; Gorbunova, Svetlana Leonidovna; Rekharsky, Mikhail Vladimirovich; Kozhemyakina, Natalia Vladimirovna; Kukushkina, Anna Aleksandrovna; Kushakova, Anna Sergeevna; Mikhaylov, Leonid Evgen’evich; Moldavsky, Alexander; Popkova, Aleksandra Vladimirovna; Silonov, Sergey Aleksandrovich; Smirnova, Svetlana Sergeevna; Iakovlev, Pavel Andreevich published a patent.Synthetic Route of 924909-16-0 The title of the patent was Pyrazolopyridine and indazole derivatives as inhibitors of Bruton’s tyrosine kinase and their preparation. And the patent contained the following:

The invention relates to a compound of formula I or pharmaceutically acceptable salt, solvate or stereoisomer thereof, which have properties of inhibitor of Bruton’s tyrosine kinase (Btk), to pharmaceutical compositions containing such compounds, and their use as pharmaceuticals for treatment of diseases and disorder. Compounds of formula I wherein V1 is C and N; V2 is CR2 and N; M is absent and CH2; K is absent and LR3; L is CH2, NH, O and a bond; R1 is (un)substituted 4-(4-oxo-4H-pyridin-1-yl)aryl, (un)substituted 4-(aryloxy)aryl, (un)substituted 4-(arylaminocarbonyl)aryl, etc.; R2 and R11 are independently H, D,halo, CN, C1-6 alkoxy, etc.; R3 is H, halo, CN, OH, C1-6 alkyl, etc.; R6 is N-substituted azetidin-3-yl, N-substituted pyrrolidinyl, and N-substituted piperidin-3-yl; and pharmaceutically acceptable salts, solvates, and stereoisomers thereof, are claimed. Example compound II was prepared by a general procedure (procedure given). The invention compounds were evaluated for their BTK inhibitory activity (data given). The experimental process involved the reaction of 1-(4-Methoxybenzyl)-1H-pyrazolo[3,4-b]pyridin-4-ol(cas: 924909-16-0).Synthetic Route of 924909-16-0

The Article related to pyrazolopyridine indazole preparation bth inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazoles and other aspects.Synthetic Route of 924909-16-0

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

On June 19, 2014, Vankayalapati, Hariprasad; Yerramreddy, Venkatakrishnareddy; Ganipisetty, Venu Babu; Talluri, Sureshkumar; Appalaneni, Rajendra P. published a patent.Quality Control of 1-(4-Methoxybenzyl)-1H-pyrazolo[3,4-b]pyridin-4-ol The title of the patent was Preparation of substituted 1H-pyrrolo[2,3-b]pyridine and 1H-pyrazolo[3,4-b]pyridine derivatives as salt inducible kinase 2 (SIK2) inhibitors. And the patent contained the following:

The present invention relates to compounds I-III [X = N or CH; L1 = H, F, (un)substituted Ph, etc.; Q = direct bond, thienyl, thiazolyl, Ph, etc.; R1 = H, halo, CN, etc.; Z = direct bond, thienyl, thiazolyl, Ph, etc.; R2 = H, halo, CN, etc.; n = 0-2; m = 0-2; with the provisos], to pharmaceutically acceptable composition, salts thereof, their synthesis and their use as SIK2 inhibitors including such compounds and methods of using said compounds in the treatment of various diseases and or disorders such as cancer, stroke, cardiovascular, obesity and type II diabetes. Over two-hundred compounds I were prepared and/or claimed. E.g., a multi-step synthesis of IV, starting from 2,2-dimethyl-1,3-dioxane-4,6-dione and 1-(4-methoxybenzyl)-1H-pyrazol-5-amine, was described. Exemplified compounds I were tested against SIK2 (data given for representative compounds I). The experimental process involved the reaction of 1-(4-Methoxybenzyl)-1H-pyrazolo[3,4-b]pyridin-4-ol(cas: 924909-16-0).Quality Control of 1-(4-Methoxybenzyl)-1H-pyrazolo[3,4-b]pyridin-4-ol

The Article related to pyrrolopyridine pyrazolopyridine preparation salt inducible kinase 2 sik2 inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazoles and other aspects.Quality Control of 1-(4-Methoxybenzyl)-1H-pyrazolo[3,4-b]pyridin-4-ol

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

On September 11, 2014, Vankayalapati, Hariprasad; Yerramreddy, Venkatakrishnareddy; Ganipisetty, Venu Babu; Talluri, Sureshkumar; Appalaneni, Rajendra P. published a patent.HPLC of Formula: 924909-16-0 The title of the patent was Preparation of substituted 1H-pyrrolo[2,3-b]pyridine and 1H-pyrazolo[3,4-b]pyridine derivatives as salt inducible kinase 2 (SIK2) inhibitors. And the patent contained the following:

The present invention relates to compounds I-III [X = N or CH; L1 = H, F, (un)substituted Ph, etc.; Q = direct bond, thienyl, thiazolyl, Ph, etc.; R1 = H, halo, CN, etc.; Z = direct bond, thienyl, thiazolyl, Ph, etc.; R2 = H, halo, CN, etc.; n = 0-2; m = 0-2; with the provisos], to pharmaceutically acceptable composition, salts thereof, their synthesis and their use as SIK2 inhibitors including such compounds and methods of using said compounds in the treatment of various diseases and or disorders such as cancer, stroke, cardiovascular, obesity and type II diabetes. Over two-hundred compounds I were prepared and/or claimed. E.g., a multi-step synthesis of IV, starting from 2,2-dimethyl-1,3-dioxane-4,6-dione and 1-(4-methoxybenzyl)-1H-pyrazol-5-amine, was described. Exemplified compounds I were tested against SIK2 (data given for representative compounds I). The experimental process involved the reaction of 1-(4-Methoxybenzyl)-1H-pyrazolo[3,4-b]pyridin-4-ol(cas: 924909-16-0).HPLC of Formula: 924909-16-0

The Article related to pyrrolopyridine pyrazolopyridine preparation salt inducible kinase 2 sik2 inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazoles and other aspects.HPLC of Formula: 924909-16-0

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

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

On October 15, 2014, Yao, Qingjia; Wu, Simin; Xu, Yangjun published a patent.Electric Literature of 924909-16-0 The title of the patent was A process for preparing 4-chloro-1H-pyrazolo[3,4-b]pyridin-3-amine. And the patent contained the following:

The invention relates to a process for the preparation of 4-chloro-1H-pyrazolo[3,4-b]pyridin-3-amine via heterocyclization of 2-propenenitrile with 4-methoxybenzaldehyde followed by reaction with tri-Et orthoformate and 2,2-dimethyl-1,3-dioxane-4,6-dion, heterocyclization, chlorination, deprotection, nitration, and reduction The experimental process involved the reaction of 1-(4-Methoxybenzyl)-1H-pyrazolo[3,4-b]pyridin-4-ol(cas: 924909-16-0).Electric Literature of 924909-16-0

The Article related to chloropyrazolopyridinamine preparation mannich heterocyclization nitration, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazoles and other aspects.Electric Literature of 924909-16-0

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

On February 15, 2007, Ozawa, Sawako; Oikawa, Nobuhiro; Mizuguchi, Eisaku; Ebiike, Hirosato; Watanabe, Fumio; Morikami, Kenji; Shimma, Nobuo; Ishii, Nobuya; Tsukaguchi, Toshiyuki; Tamaki, Yasuhiro; Takahashi, Hidenori published a patent.Synthetic Route of 924909-16-0 The title of the patent was Preparation of urea derivatives as multi kinase inhibitors. And the patent contained the following:

The title compounds I [wherein Ar = (un)substituted Ph or naphthyl; T = alkyl, alkoxy, etc.; X = O, CH2, CO, etc.; Y = CH or N; R2-R4 = independently H, (un)substituted alkyl, etc.], or pharmaceutically acceptable salts or prodrugs thereof are prepared as multi kinase inhibitors. For example, the compound II was prepared in a multi-step synthesis. Some of compounds I showed good inhibitory activities against human cancer cell growth. The experimental process involved the reaction of 1-(4-Methoxybenzyl)-1H-pyrazolo[3,4-b]pyridin-4-ol(cas: 924909-16-0).Synthetic Route of 924909-16-0

The Article related to phenyl indole pyrrazolo pyridine urea kinase inhibitor preparation human, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazoles and other aspects.Synthetic Route of 924909-16-0

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

On March 28, 2013, Wilson, Timothy R.; Koeppen, Hartmut; Merchant, Mark; Settleman, Jeffrey published a patent.SDS of cas: 924909-16-0 The title of the patent was Combinations comprising c-Met antagonists and B-raf antagonists for treatment of cancer. And the patent contained the following:

The invention provides combination therapies for treating a pathol. condition, such as cancer, wherein a c-met antagonist (e.g. crizotinib, tivantinib, anti-HGF antibody, onartuzumab) is combined with a B-raf antagonist (e.g. vemurafenib), thereby providing significant antitumor activity. C-met expression was inversely correlated with sensitivity to vemurafenib treatment. In one aspect, provided are methods for treating a cancer patient who has increased likelihood of developing resistance to B-raf antagonist comprising administering an effective amount (in combination) of B-raf antagonist and c-met antagonist. In addition, patients with B-raf mutant melanoma who had higher levels of circulating hepatocyte growth factor (HGF) showed substantially reduced progression free survival and overall survival when treated with B-raf antagonist, relative to patients with lower circulating HGF levels treated with B-raf antagonist. The experimental process involved the reaction of 1-(4-Methoxybenzyl)-1H-pyrazolo[3,4-b]pyridin-4-ol(cas: 924909-16-0).SDS of cas: 924909-16-0

The Article related to combination chemotherapy cmet antagonist braf inhibitor cancer treatment, gdc0712 preparation antitumor combination chemotherapy cmet braf drug target, Pharmacology: Effects Of Neoplasm Inhibitors and Cytotoxic Agents and other aspects.SDS of cas: 924909-16-0

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics