Category: 143803-93-4

Komatsuda, Masaaki; Suto, Ayane; Kondo, Hiroki Jr; Takada, Hiroyuki; Kato, Kenta; Saito, Bunnai; Yamaguchi, Junichiro published an article in 2022, the title of the article was Ring-opening fluorination of bicyclic azaarenes.HPLC of Formula: 143803-93-4 And the article contains the following content:

Authors have discovered a ring-opening fluorination of bicyclic azaarenes. Upon treatment of bicyclic azaarenes such as pyrazolo[1,5-a]pyridines with electrophilic fluorinating agents, fluorination of the aromatic ring is followed by a ring-opening reaction. Although this overall transformation can be classified as an electrophilic fluorination of an aromatic ring, it is a novel type of fluorination that results in construction of tertiary carbon-fluorine bonds. The present protocol can be applied to a range of bicyclic azaarenes, tolerating azines and a variety of functional groups. Addnl., mechanistic studies and enantioselective fluorination have been examined The experimental process involved the reaction of 4-Methylpyrazolo[1,5-a]pyridine-3-carboxylic acid(cas: 143803-93-4).HPLC of Formula: 143803-93-4

The Article related to pyrazolopyridine bicyclic azaarene ring opening fluorination, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.HPLC of Formula: 143803-93-4

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

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

Xu, Juan; Zhao, Xinyu; Kang, Congmin published an article in 2018, the title of the article was Improved synthesis of pyrazolo[1,5-a]pyridine-3-carboxylic acid derivatives.Product Details of 143803-93-4 And the article contains the following content:

Pyrazolo[1,5-a]pyridine-3-carboxylate derivatives were obtained from 1,3-dipolar cycloaddition reaction with Et propynoate and N-aminopyridine sulfate synthesized by the reactions of substituted pyridines and hydroxyamine-O-sulfonic acid. They were further treated with 30% NaOH aqueous solution to give corresponding substituted pyrazolo[1,5-a]pyridine-3-carboxylic acid derivatives In this method, N-aminopyridine sulfate was directly put into the next reaction, which eliminated the step of converting sulfate into iodine salt in the traditional method and solved the problem that the iodine salt was difficult to precipitate N-aminopyridine sulfate and Et propynoate were dissolved in water and N,N-dimethylformamide, resp., and then mixed to increase the solubility of reactants. Six compounds (4a∼4f) were successfully synthesized with yields of 88%∼93%. The method is mild and easy to process and has low cost as a new process for mass production The experimental process involved the reaction of 4-Methylpyrazolo[1,5-a]pyridine-3-carboxylic acid(cas: 143803-93-4).Product Details of 143803-93-4

The Article related to pyrazolopyridine carboxylic acid derivative synthesis, Industrial Organic Chemicals, Leather, Fats, and Waxes: Manufacture Of Industrial Organic Chemicals and other aspects.Product Details of 143803-93-4

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

On May 6, 1992, Higashino, Takeo; Suzuki, Yukio; Sasahara, Takehiko; Saito, Tetsu; Mochizuki, Daisuke published a patent.COA of Formula: C9H8N2O2 The title of the patent was Preparation of pyrazolo[1,5-a]pyridine-3-carboxylic acid as serotonin 3-receptor binding antagonists. And the patent contained the following:

The title compounds (I; R1, R2 = H, alkyl; R3 = azabicyclo groups Q, Q1; Y = O, NH; Z = alkyl; n = 2, 3) or their salts, useful as antianxietics and antiemetics, especially for reducing nausea and vomiting due to side effects of an carcinostatic agent, were prepared, e.g., by amidation of pyrazolo[1,5-a]pyridinecarboxylic acids by azabicycloalkanamines. Thus, 7-methyl-3-pyrazolo[1,5-a]pyridinecarboxylic acid [J. Organic Chem. 33(5), 2062-4 (1968)] was refluxed in SOCl2 for 30 min., distilled, and the residue refluxed for 24 h with endo-8-methyl-8-azabicyclo[3.2.1]oct-3-yl-7-methylpyrazolo[1,5-a]pyridine-3-carboxamide (II). The latter in a 3H-quipazine binding assay in vitro had IC50 = 19.1 nM. II at 0.1 mg/kg i.v. in beagles prevented vomiting following administration of 3 mg/kg i.v. cisplatin. The experimental process involved the reaction of 4-Methylpyrazolo[1,5-a]pyridine-3-carboxylic acid(cas: 143803-93-4).COA of Formula: C9H8N2O2

The Article related to pyrazolopyridine preparation antiemetic antianxietic, nausea cisplatin prevention pyrazolopyridine preparation, vomiting cisplatin prevention pyrazolopyridine preparation and other aspects.COA of Formula: C9H8N2O2

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

On September 30, 2021, Ameriks, Michael K.; Laforteza, Brian Ngo; Ravula, Suchitra; Schiffer, Jamie M.; Stenne, Brice M. published a patent.Electric Literature of 143803-93-4 The title of the patent was Preparation of fused and bridged compounds as monoacylglycerol lipase modulators. And the patent contained the following:

This invention relates to the title compounds I [R1a = alkyl; R1b = H; or R1a and R1b taken together form (CH2)2-3; R2 = (un)substituted Ph, pyridyl, bicyclic heteroaryl; R3 = 1H-alkyl-pyrazolyl, 1H-haloalkyl-pyrazolyl, 1H-pyridyl-pyrazolyl, etc.; with the proviso], and pharmaceutically acceptable salts, isotopes, N-oxides, solvates, and stereoisomers thereof, to pharmaceutical compositions containing them, to methods of making them, and to methods of using them including methods for treating disease states, disorders, and conditions associated with MGL modulation, such as those associated with pain, psychiatric disorders, neurol. disorders (including, but not limited to major depressive disorder, treatment resistant depression, anxious depression, autism spectrum disorders, Asperger syndrome, bipolar disorder), cancers and eye conditions. E.g., a multi-step synthesis of (S)-II, starting from Et L-alaninate hydrochloride and Et 4-bromobutanoate, was described. Exemplified compounds I were tested for their in vitro activity of MGL (data given for representative compounds I). The experimental process involved the reaction of 4-Methylpyrazolo[1,5-a]pyridine-3-carboxylic acid(cas: 143803-93-4).Electric Literature of 143803-93-4

The Article related to analgesics, antidepressants, antitumor agents, anxiety disorders (anxious depression), anxiolytics, asperger syndrome, bipolar disorder, depression (treatment-resistant), eye disease and other aspects.Electric Literature of 143803-93-4

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