Day: November 2, 2022

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 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 December 31, 2012, Zheng, Chang-Ji; Xu, Li-Li; Sun, Liang-Peng; Miao, Jing; Piao, Hu-Ri published an article.Application In Synthesis of 3-(Naphthalen-2-yl)-1-phenyl-1H-pyrazole-4-carbaldehyde The title of the article was Synthesis and antibacterial activity of novel 1,3-diphenyl-1H-pyrazoles functionalized with phenylalanine-derived rhodanines. And the article contained the following:

In the present study, a series of novel 1,3-diphenyl-1H-pyrazoles functionalized with phenylalanine-derived rhodanine derivatives were synthesized and evaluated for their antibacterial activity. Several of these compounds, e.g. I, exhibited stronger activity than the standard drugs, norfloxacin and oxacillin, with MIC values of 1 μg/mL against methicillin-resistant Staphylococcus aureus and quinolone-resistant S. aureus. None of the compounds showed any activity against Gram-neg. bacteria. The experimental process involved the reaction of 3-(Naphthalen-2-yl)-1-phenyl-1H-pyrazole-4-carbaldehyde(cas: 36640-53-6).Application In Synthesis of 3-(Naphthalen-2-yl)-1-phenyl-1H-pyrazole-4-carbaldehyde

The Article related to pyrazole diphenyl phenylalanine rhodanine preparation antibacterial activity, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazoles and other aspects.Application In Synthesis of 3-(Naphthalen-2-yl)-1-phenyl-1H-pyrazole-4-carbaldehyde

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 November 26, 2020, 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.Synthetic Route of 1186608-73-0 The title of the patent was Preparation of pyrazolopyridines and related heterocycles and compositions containing them for the treatment of cystic fibrosis. And the patent contained the following:

The invention relates to preparation of pyrazolopyridines and related heterocycles of formula (I) or pharmaceutically acceptable salts or solvates thereof: It further discloses a pharmaceutical composition comprising the compounds I and their uses, in particular to modulate CFTR protein or ABC protein activities. Compounds I wherein R1 is H; Z is CO or SO2; X1-X4 each independently is CRVII and N, with the proviso that the number of nitrogen atoms in the ring is comprised from O to 2; R2 is H, OH, NO, etc.; A1-A4 each independently is O, SO2, CO, etc.; B represents an unsubstituted or a substituted aromatic or heteroaromatic ring; n and m are each independently selected from the group consisting of O, 1, 2; etc., are claimed. The example compound II was prepared using 3-hydrazinobenzoic acid as starting material (procedure given). Compounds I were evaluated for their biol. activity (data given). Compounds I and pharmaceutical composition comprising them, are modulators of CFTR protein or ABC protein activities, and can be used in treatment of cystic fibrosis and other diseases. The experimental process involved the reaction of 3-Methyl-1H-pyrazolo[3,4-b]pyridin-5-amine(cas: 1186608-73-0).Synthetic Route of 1186608-73-0

The Article related to pyrazolopyridine preparation cftr modulator abc protein cystic fibrosis treatment, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazoles and other aspects.Synthetic Route of 1186608-73-0

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 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 March 27, 1979, Rainer, Georg published a patent.Reference of 3-(Naphthalen-2-yl)-1-phenyl-1H-pyrazole-4-carbaldehyde The title of the patent was 4-Pyrazoleacetic acid derivatives. And the patent contained the following:

Pyrazoleacetic acid derivatives I (R = CO2H, alkoxycarbonyl, CONH2; R1, R2 = optionally substituted Ph, furyl, thienyl, naphthyl; R3 = H, Ph, furyl) were prepared Thus, CH2Ac2 was treated with BrCH2CO2Et to give Ac2CHCH2CO2Et which was cyclized with PhNHNH2 to give I (R = CO2Et, R1 = Ph, R2 = R3 = Me), which was hydrolyzed to the acid. I had antiinflammatory and analgesic activity. Thus, I (R = CO2H, R1 = Ph, R2 = R3 = 2-furyl) had antiinflammatory ED50 in the UV erythema test of 1.5 mg/kg orally and then analgesic ED40 50 mg/kg orally. The experimental process involved the reaction of 3-(Naphthalen-2-yl)-1-phenyl-1H-pyrazole-4-carbaldehyde(cas: 36640-53-6).Reference of 3-(Naphthalen-2-yl)-1-phenyl-1H-pyrazole-4-carbaldehyde

The Article related to pyrazoleacetic acid, antiinflammatory pyrazoleacetic acid, analgesic pyrazoleacetic acid, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazoles and other aspects.Reference of 3-(Naphthalen-2-yl)-1-phenyl-1H-pyrazole-4-carbaldehyde

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

Verma, Anil; Kumar, Vinod; Kataria, Ramesh; Singh, Joginder published an article in 2019, the title of the article was Novel acetohydrazide pyrazole derivatives, design, synthesis, characterization and antimicrobial activity.Computed Properties of 36640-53-6 And the article contains the following content:

Eleven acetohydrazide linked pyrazole derivatives I [R = Ph, thiophen-2-yl, 1-naphthyl, etc.] were designed and synthesized via condensation of acetohyadrazide with different substituted formyl pyrazole derivatives under mild reaction conditions. Synthesized compounds I were characterized on the basis of IR, NMR (1H & 13C) and mass spectrometry. The antimicrobial activities of all the compounds I were screened against four bacterial and two fungal strains. Among the synthesized compounds, three compounds viz. I [R = 4-fluorophenyl, 4-chlorophenyl, 4-bromophenyl] were found as efficient antimicrobial agents in reference to the standard drugs viz. ciprofloxacin and amphotericin-B. Further, structure-activity relationship (SAR) study revealed that electron-withdrawing group enhances the antimicrobial potential of synthesized derivatives I as compared to other groups present in the ring. Hence, among compounds I [R = 4-fluorophenyl, 4-chlorophenyl, 4-bromophenyl] could be explored further against other microbes to prove its vitality. The experimental process involved the reaction of 3-(Naphthalen-2-yl)-1-phenyl-1H-pyrazole-4-carbaldehyde(cas: 36640-53-6).Computed Properties of 36640-53-6

The Article related to diphenyl pyrazolylmethylene acetohydrazide preparation antibacterial antifungal activity sar, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazoles and other aspects.Computed Properties of 36640-53-6

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

Kendall, Jackie D.; O’Connor, Patrick D.; Marshall, Andrew J.; Frederick, Raphael; Marshall, Elaine S.; Lill, Claire L.; Lee, Woo-Jeong; Kolekar, Sharada; Chao, Mindy; Malik, Alisha; Yu, Shuqiao; Chaussade, Claire; Buchanan, Christina; Rewcastle, Gordon W.; Baguley, Bruce C.; Flanagan, Jack U.; Jamieson, Stephen M. F.; Denny, William A.; Shepherd, Peter R. published an article in 2012, the title of the article was Discovery of pyrazolo[1,5-a]pyridines as p110α-selective PI3 kinase inhibitors.Recommanded Product: 4-Methylpyrazolo[1,5-a]pyridine-3-carboxylic acid And the article contains the following content:

A novel series of pyrazolo[1,5-a]pyridines were prepared as PI3 kinase inhibitors, and their selectivity for the p110α isoform over the other Class Ia PI3 kinases was demonstrated. The SAR around the pyrazolo[1,5-a]pyridine ring system was investigated, and N’-[(5-cyanopyrazolo[1,5-a]pyridin-3-yl)methylene]-N,2-dimethyl-5-nitrobenzenesulfonic acid hydrazide was shown to be a particularly potent example (p110α IC50 0.9 nM). This compound inhibits cell proliferation and phosphorylation of Akt/PKB, a downstream marker of PI3 kinase activity, and showed in vivo activity in an HCT-116 human xenograft model. The experimental process involved the reaction of 4-Methylpyrazolo[1,5-a]pyridine-3-carboxylic acid(cas: 143803-93-4).Recommanded Product: 4-Methylpyrazolo[1,5-a]pyridine-3-carboxylic acid

The Article related to pyrazolopyrazinylmethylene benzenesulfonylhydrazine preparation pi3 kinase inhibitor anticancer, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazoles and other aspects.Recommanded Product: 4-Methylpyrazolo[1,5-a]pyridine-3-carboxylic acid

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