Day: November 2, 2022

On December 31, 2014, Goel, Neelima; Drabu, Sushma; Afzal, Obaid; Bawa, Sandhya published an article.Reference of 3-(Naphthalen-2-yl)-1-phenyl-1H-pyrazole-4-carbaldehyde The title of the article was Antimicrobial screening and one-pot synthesis of 4-(substituted-anilinomethyl)-3-(2-naphthyl)-1-phenyl-1H-pyrazole derivatives. And the article contained the following:

A series of 4-(substituted-anilinomethyl)-3-(2-naphthyl)-1-phenyl-1H-pyrazole derivatives (4a-4k) were synthesized through direct reductive amination of 3-(naphthalen-2-yl)-1-phenyl-1H-pyrazole-4-carbaldehyde with various substituted aromatic amines using NaBH4 in the presence of I2 as reducing agent. The reaction was carried out in anhydrous methanol under neutral conditions at room temperature All 4-(substituted-anilinomethyl)-3-(2-naphthyl)-1-phenyl-1H-pyrazole derivatives (4a-4k) were tested in vitro for antifungal and antibacterial activities against different fungal and bacterial strains. Most of the compounds exhibited considerable antifungal activity, but poor antibacterial activity against the test strains. In the series compound 4e, 4g, 4j, and 4k, showed excellent antifungal activity against the fungal strain Aspergillus niger (MTCC) 281 and Aspergillus flavus MTCC 277 (% inhibition in the range of 47.7-58.9). 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 pyrazole naphthyl anilinomethyl preparation antibacterial antifungal, antimicrobial activity, naphthalene, pyrazole, reductive amination, 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 6, 2008, McLaughlin, Mark; Marcantonio, Karen; Chen, Cheng-yi; Davies, Ian W. published an article.Quality Control of 3-Phenyl-1-(tetrahydro-2H-pyran-2-yl)-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole The title of the article was A Simple, Modular Method for the Synthesis of 3,4,5-Trisubstituted Pyrazoles. And the article contained the following:

A modular approach for the regiocontrolled preparation of pyrazoles bearing substituents on all three carbon atoms is described. Central to this method is the use of a switchable metal-directing group to enable sequential direct lithiation of the 3- and 5-positions of the pyrazole ring. Pyrazole boronic esters obtained from these lithiated intermediates can undergo efficient Suzuki cross-coupling under the developed nonaqueous conditions, which minimize undesirable protolytic deboronation. Halogenation of the 4-position provides the means for substitution at the remaining carbon atom. The experimental process involved the reaction of 3-Phenyl-1-(tetrahydro-2H-pyran-2-yl)-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole(cas: 1028092-65-0).Quality Control of 3-Phenyl-1-(tetrahydro-2H-pyran-2-yl)-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole

The Article related to aryl pyrazole regioselective synthesis, pyrazole tetrahydropyranyl regioselective lithiation suzuki coupling aryl halide, tetrahydropyranyl metal directing group, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazoles and other aspects.Quality Control of 3-Phenyl-1-(tetrahydro-2H-pyran-2-yl)-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole

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

Salanouve, Elise; Retailleau, Pascal; Janin, Yves L. published an article in 2012, the title of the article was Few unexpected results from a Suzuki-Miyaura reaction.Recommanded Product: 215610-30-3 And the article contains the following content:

In the course of the synthesis of original anti-infectious compounds, we focused on the palladium-catalyzed Suzuki-Miyaura aryl-aryl coupling reaction between 2-(3-ethoxy-5-iodo-1H-pyrazol-1-yl)pyridine and phenylboronic acid. A study of the reaction products obtained under different conditions (various ligands and solvents) not only provided us with insights to optimize this reaction but also with a few side compounds, resulting from CH activation, along with the unexpected bis(3-ethoxy-1-(pyridin-2-yl)-1H-pyrazol-5-yl)palladium. Stoichiometric experiments with this remarkably stable biscyclopalladated reagent and Ph halides pointed out the occurrence of aryl-aryl coupling, possibly via palladium IV intermediates. The experimental process involved the reaction of 5-Methoxy-1H-pyrazole(cas: 215610-30-3).Recommanded Product: 215610-30-3

The Article related to bispyridinylpyrazolylpalladium preparation reaction aryl halide, palladium bispyridinylpyrazolyl preparation reaction aryl halide, side product suzuki miyaura reaction, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazoles and other aspects.Recommanded Product: 215610-30-3

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

On September 13, 2007, Blake, James F.; Boyd, Steven Armen; Cohen, Frederick; De Meese, Jason; Fong, Kin Chiu; Gaudino, John J.; Kaplan, Tomas; Marlow, Allison L.; Seo, Jeongbeob; Thomas, Allen A.; Tian, Hongqi; Young, Wendy B. published a patent.Related Products of 924909-16-0 The title of the patent was Heterobicyclic pyrazole compounds as Met tyrosine kinase inhibitors and their preparation and use. And the patent contained the following:

The invention is related to the preparation of I and II [X = O, S, NH and derivatives; Z2, Z3 = independently CH and derivatives, N, wherein none or one of Z2, and Z3 = N; R1 = H, (un)substituted alk(en/yn)yl, (hetero)aryl, etc.; R2 = H, CF3, CN, SH and derivatives, SO2NH2 and derivatives, etc.; R3 = (un)substituted carbocyclyl, heterocyclyl, (hetero)/aryl] and their pharmaceutically acceptable salts which are useful for inhibiting receptor tyrosine kinases and for treating disorders mediated thereby. Methods of using compounds I and II and their stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathol. conditions are disclosed. Thus, pyrazolopyridine III was prepared by a multi-step synthesis via 1-(4-methoxybenzyl)-1H-pyrazolo[3,4-b]pyridin-4-ol intermediate which was obtained from 1-(4-methoxybenzyl)-1H-pyrazol-5-amine and Meldrum’s acid. Certain I and II had IC50’s < 1 μM in a c-Met enzyme assay. The experimental process involved the reaction of 1-(4-Methoxybenzyl)-1H-pyrazolo[3,4-b]pyridin-4-ol(cas: 924909-16-0).Related Products of 924909-16-0

The Article related to heterobicyclic pyrazole preparation tyrosine kinase inhibitor antiproliferative, pyrazolopyridine preparation met kinase inhibitor antitumor hyperproliferative disease, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazoles and other aspects.Related Products of 924909-16-0

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

On March 3, 2022, Grall-Ulsemer, Sandra; Guba, Wolfgang; Lerner, Christian; Li, Mingming; Liu, Yongqiang; Rudolph, Markus; Schmitt, Sebastien; Urner, Lorenz; Wang, Yongguang; Wang, Min; Wang, Jianhua; Yang, Song; Zhou, Chengang; Mattei, Patrizio published a patent.Formula: C4H6N2O The title of the patent was Imidazole-pyrazole derivatives as antibacterials and their preparation. And the patent contained the following:

The invention provides imidazole-pyrazole derivatives having formula I, and pharmaceutically acceptable salts thereof. Further provided are pharmaceutical compositions including the compounds, processes of manufacturing the compounds and methods of using the compounds as medicaments, in particular methods of using the compounds as antibiotics for the treatment or prevention of bacterial infections and resulting diseases. Compounds of formula I wherein R1R2 are taken together to form substituted nitrogen-containing heterocyclyl; R1 is (un)substituted 3- to 14-membered heterocyclyl, (un)substituted 3- to 14-membered heterocyclyl-CO and (un)substituted 3- to 14-membered heterocyclyl-C1-6 alkyl; R2 is H and C1-6 alkyl; R3 is H, halo, C1-6 alkyl and C1-6 alkoxy; R4 and R6 are independently H, C1-6 alkyl, C1-6 alkoxy, CN, etc.; R5a, R5b and R5c are independently H, halo, OH, C1-6 alkyl, C1-6 alkoxy, etc.; R7 is H, C1-6 alkyl and C1-6 haloalkyl; A is 5- to 14-membered heteroaryl; and pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by methylation of N-(3-chloro-4-(4-(piperidine-4-carbonyl)piperazine-1-carbonyl)phenyl)-5-(1-(5-methoxypyridin-2-yl)-3-(trifluoromethyl)-pyrazol-4-yl)-1-methyl-imidazole-2-carboxamide with Me iodide. The invention compounds were evaluated for their antibacterial activity. From the assay, it was determined that compound II exhibited IC90 value of 0.095μM. The experimental process involved the reaction of 5-Methoxy-1H-pyrazole(cas: 215610-30-3).Formula: C4H6N2O

The Article related to imidazole pyrazole preparation antibacterial, Heterocyclic Compounds (More Than One Hetero Atom): Imidazoles and other aspects.Formula: C4H6N2O

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

On March 10, 2022, Lerner, Christian; Li, Mingming; Liu, Yongqiang; Schmitt, Sebastien; Wang, Jianhua; Wang, Min; Wang, Yongguang; Yang, Song; Zhou, Chengang published a patent.COA of Formula: C4H6N2O The title of the patent was Preparation of imidazole-pyrazole derivatives with anti-bacterial properties. And the patent contained the following:

The invention provides imidazole pyrazole derivatives having formula I, and pharmaceutically acceptable salts thereof. Further provided are pharmaceutical compositions including the compounds, processes of manufacturing the compounds and methods of using the compounds as medicaments, in particular methods of using the compounds as antibiotics for the treatment or prevention of bacterial infections and resulting diseases. Compounds of formula I wherein R1R2 may be taken together to form substituted nitrogen-containing heterocycle; R1 is C1-6 alkyl, amino-C1-6 alkyl, amino-C1-6 alkoxy-C1-6 alkyl, etc.; R2 is H and C1-6 alkyl; R3 is H, halo, C1-6 alkyl and C1-6 alkoxy; R4 and R6 are independently H, C1-6 alkyl, C1-6 alkoxy, CN, etc.; R5a, R5b and R5c are H, halo, OH, C1-6 alkyl, C1-6 alkoxy, etc.; A is 5- to 14- membered heteroaryl; and pharmaceutically acceptable salts thereof, are claimed. Example compound II•HCO2H was prepared by arylation of tert-Bu 4-(4-(2-chloro-4-(1-methyl-5-(3-(trifluoromethyl)-1H-pyrazol-4-yl)-imidazole-2-carboxamido)benzoyl)piperazine-1-carbonyl)piperidine-1-carboxylate with 2-chloropyrimidine; the resulting tert-Bu 4-(4-(2-chloro-4-(1-methyl-5-(1-(pyrimidin-2-yl)-3-(trifluoromethyl)-pyrazol-4-yl)-imidazole-2-carboxamido)benzoyl)piperazine-1- carbonyl)piperidine-1-carboxylate underwent hydrolysis to give compound II•HCO2H. The invention compounds were evaluated for their antibacterial activity. From the assay, it was determined that compound II exhibited IC90 value of 0.69μM. The experimental process involved the reaction of 5-Methoxy-1H-pyrazole(cas: 215610-30-3).COA of Formula: C4H6N2O

The Article related to imidazole pyrazole preparation antibacterial, Heterocyclic Compounds (More Than One Hetero Atom): Imidazoles and other aspects.COA of Formula: C4H6N2O

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

On January 13, 2022, Barrett, Matthew; Cockerill, George Stuart; Good, James; Avery, Craig Alex; Cochrane, Edward James; Jones, Stefan Paul; Onions, Stuart Thomas; Warner, Andrew Joseph published a patent.Recommanded Product: Ethyl 6,7-dihydro-5H-pyrazolo[5,1-b][1,3]oxazine-2-carboxylate The title of the patent was Synthesis of Benzodiazepines useful in treating a respiratory syncytial virus infection. And the patent contained the following:

The synthesis of benzodiazepines, I, wherein: one of R1 or R2 can be II such that the other group is selected from H, cycloalkyl, halo, amino, benzyl, Ph, 4- to 10-membered heterocyclic or heteroaryl groups; R3 can be H or halo; and the ring A can be a 5- or 6-membered heterocyclic ring system containing a variety of N, O or C atoms are prepared as pharmaceutically acceptable salt RSV inhibitors used to treat or prevent an RSV infection. Of note, II was synthesized and displayed an RSV A2 plaque EC50 of 33 nM and cell cytotoxicity of greater than 25,000 nM CC50 and presented in aqueous formulations. Further, some I derivatives were tested in vitro pharmacokinetics to investigate liver microsomal stability. The experimental process involved the reaction of Ethyl 6,7-dihydro-5H-pyrazolo[5,1-b][1,3]oxazine-2-carboxylate(cas: 153597-59-2).Recommanded Product: Ethyl 6,7-dihydro-5H-pyrazolo[5,1-b][1,3]oxazine-2-carboxylate

The Article related to benzodiazepine preparation antiviral rsv infection, Heterocyclic Compounds (More Than One Hetero Atom): Diazepines and other aspects.Recommanded Product: Ethyl 6,7-dihydro-5H-pyrazolo[5,1-b][1,3]oxazine-2-carboxylate

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

On April 12, 2012, Biggadike, Keith; Birault, Veronique; Champigny, Aurelie Cecile; Coe, Diane Mary; Hughes, Owen Rhys; Needham, Deborah; Tape, Daniel Terence published a patent.Synthetic Route of 143803-93-4 The title of the patent was Imidazo[1,2-a]pyridine and pyrazolo[1,5-a]pyridine derivatives as TRPV1 antagonists and their preparation and use for the treatment of TRPV1-mediated diseases. And the patent contained the following:

The invention relates to imidazopyridine and pyrazolopyridine derivatives of formula I, which are TRPV1 antagonists and which are useful in the treatment of TRPV1-mediated diseases. Compounds of formula I wherein A is single bond, CH2 and CH(CH3); X1 is H, F and Me; X2 is H, F, Me and CH2OH; X3 is H, F and Ch2OH; provided that at least two of X1, X2 and X3 are H; Y is C when Z is N, and Y is N when Z is C; R1 is halo, C1-4 alkyl, CF3 and OCF3; R2 and R3 are independently H, halo, C1-4 alkyl, CF3 and OCF3; and pharmaceutically acceptable salts and solvates, are claimed. Example compound II was prepared by a amidation of imidazo[1,2-a]pyridine-3-carboxylic acid with (2-{[4-(1,1-dimethylethyl)phenyl]oxy}ethyl)amine. All the invention compounds were evaluated for their TRPV1 antagonistic activity. From the assay, it was determined that all compounds exhibited a pIC50 value greater than 5.2. The experimental process involved the reaction of 4-Methylpyrazolo[1,5-a]pyridine-3-carboxylic acid(cas: 143803-93-4).Synthetic Route of 143803-93-4

The Article related to imidazopyridine preparation trpv1 antagonist treatment disease, pyrazolopyridine preparation trpv1 antagonist treatment disease, Heterocyclic Compounds (More Than One Hetero Atom): Imidazoles and other aspects.Synthetic Route of 143803-93-4

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

On August 13, 2009, Hirokawa, Takatsugu; Takemura, Shunji; Shibazaki, Manabu; Ishiwatari, Hiroyuki published a patent.Quality Control of 3-(Naphthalen-2-yl)-1-phenyl-1H-pyrazole-4-carbaldehyde The title of the patent was 3-naphthylpyrazole compounds, histamine H4 receptor antagonists containing them, their use for treatment for inflammatory disorders, and pharmaceutical compositions containing them. And the patent contained the following:

Claimed are title compounds I [ring A = C6-10 aryl; X = (CH2)n (n = 1-6), CH:N; Y = O, S, NR8; Z = direct bond, CHR7; R1-R7 = H, halo, OH, NO2, carboxy, carbamoyl, C1-6 alkyl, C2-6 acyl, C6-10-aryl-C1-6 alkyl, C5-10-heteroaryl-C2-6 alkenyl, etc.; R8 = H, OH, C1-6 alkyloxy], their salts, or their solvates [exclusive of (E)-2-[[3-(2-Naphthyl)-1-phenyl-1H-pyrazol-4-yl]methylene]hydrazinecarboxamide] and histamine H4 receptor antagonists containing I, their salts, or their solvates. Also claimed are prophylactic and/or therapeutic agents and pharmaceutical compositions containing I, their salts, or their solvates. Thus, (S)-2-amino-N-[[3-(2-naphthyl)-1-phenyl-1H-pyrazol-4-yl]methyl]-3-phenylpropanamide at 10 μM (preparation given) showed 86% inhibition against histamine binding to human recombinant H4 receptor expressed on CHO cells. 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 naphthylpyrazole compound preparation histamine h4 receptor antagonist inflammation inhibitor, Pharmacology: Effects Of Inflammation Inhibitors and Immune Agents and other aspects.Quality Control of 3-(Naphthalen-2-yl)-1-phenyl-1H-pyrazole-4-carbaldehyde

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