Tag: 200-300

On March 1, 2007, Arora, Nidhi; Billedeau, Roland Joseph; Dewdney, Nolan James; Gabriel, Tobias; Goldstein, David Michael; O’Yang, Counde; Soth, Michael; Trejo-Martin, Teresa Alejandra published a patent.Recommanded Product: 4-Chloro-6-(methylthio)-1H-pyrazolo[3,4-d]pyrimidine The title of the patent was Preparation of fused pyrazole derivatives as P38 MAP kinase inhibitors. And the patent contained the following:

The title fused pyrazole derivatives are prepared as p38 MAP kinase inhibitors for the treatment of p38-mediated diseases. For example, the compound I was prepared in a multi-step synthesis. I inhibited p38 MAP kinase with IC50 of 0.001 μM in vitro. Formulations containing the title compound as an active ingredient were also described. The experimental process involved the reaction of 4-Chloro-6-(methylthio)-1H-pyrazolo[3,4-d]pyrimidine(cas: 85426-79-5).Recommanded Product: 4-Chloro-6-(methylthio)-1H-pyrazolo[3,4-d]pyrimidine

The Article related to preparation pyrazolo pyrimidine pyridine p38 map kinase inhibitor, formulation treatment arthritis human, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazoles and other aspects.Recommanded Product: 4-Chloro-6-(methylthio)-1H-pyrazolo[3,4-d]pyrimidine

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

On September 30, 2012, Siddhartha, Tarun; Mithilesh; Sharma, Raju; Chawla, Pooja; Saraf, S. K. published an article.Quality Control of 3-(Naphthalen-2-yl)-1-phenyl-1H-pyrazole-4-carbaldehyde The title of the article was Syntheses and antioxidant screening of pyrazole-4-carboxaldehyde derivatives. And the article contained the following:

Pyrazole-4-carboxaldehydes were synthesized by AcOH-mediated condensation of aryl Me ketones with phenylhydrazines in EtOH to afford the corresponding phenylhydrazones. Subsequent reaction with 2 equiv DMF-POCl3 adduct (Vilsmeier Haack reagent) in DMF at 60-70° for 6 h afforded immonium perchlorates. Further, alk. hydrolysis (NaOH) afforded pyrazole-4-carboxaldehydes. All the synthesized compounds were screened for antioxidant activity. In a ferric reducing power assay, increased absorbance of the compounds with concentration indicates increased reducing power. Compounds with higher concentrations showed a higher reducing power. The reducing power showed good linear relation (R2) in both standard as well as in the newly prepared compounds Thus, the compounds have antioxidant activity. The experimental process involved the reaction of 3-(Naphthalen-2-yl)-1-phenyl-1H-pyrazole-4-carbaldehyde(cas: 36640-53-6).Quality Control of 3-(Naphthalen-2-yl)-1-phenyl-1H-pyrazole-4-carbaldehyde

The Article related to phenylhydrazone vilsmeier haack cyclization formylation, pyrazolecarboxaldehyde preparation antioxidant, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazoles and other aspects.Quality Control 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

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

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 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 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