Month: September 2022

Pyrazole and its derivatives are considered a pharmacologically important active scaffold that possesses almost all types of pharmacological activities. 761446-44-0, formula is C10H17BN2O2, Name is 1-Methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole. Pyrazole is a weak base, with pKb 11.5 (pKa of the conjugated acid 2.49 at 25 °C).Pyrazole used as a ligand to prepare organometallic compounds. Application In Synthesis of 761446-44-0.

Finlay, M. Raymond V.;Barton, Peter;Bickerton, Sue;Bista, Michal;Colclough, Nicola;Cross, Darren A. E.;Evans, Laura;Floc′h, Nicolas;Gregson, Clare;Guerot, Carine M.;Hargreaves, David;Kang, Xiaoming;Lenz, Eva M.;Li, Xu;Liu, Yi;Lorthioir, Olivier;Martin, Matthew J.;McKerrecher, Darren;McWhirter, Claire;O′Neill, Daniel;Orme, Jonathan P.;Mosallanejad, Arash;Rahi, Amar;Smith, Paul D.;Talbot, Verity;Ward, Richard A.;Wrigley, Gail;Wylot, Marta;Xue, Lin;Yao, Tieguang;Ye, Yang;Zhao, Xiliang research published 《 Potent and Selective Inhibitors of the Epidermal Growth Factor Receptor to Overcome C797S-Mediated Resistance》, the research content is summarized as follows. The epidermal growth factor receptor (EGFR) harboring activating mutations is a clin. validated target in non-small-cell lung cancer, and a number of inhibitors of the EGFR tyrosine kinase domain, including osimertinib, have been approved for clin. use. Resistance to these therapies has emerged due to a variety of mol. events including the C797S mutation which renders third-generation C797-targeting covalent EGFR inhibitors considerably less potent against the target due to the loss of the key covalent-bond-forming residue. We describe the medicinal chem. optimization of a biochem. potent but modestly cell-active, reversible EGFR inhibitor starting point with sub-optimal physicochem. properties. These studies culminated in the identification of compound 12 that showed improved cell potency, oral exposure, and in vivo activity in clin. relevant EGFR-mutant-driven disease models, including an Exon19 deletion/T790M/C797S triple-mutant mouse xenograft model.

761446-44-0, 1-Methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole is a useful research compound. Its molecular formula is C10H17BN2O2 and its molecular weight is 208.07 g/mol. The purity is usually 95%., Application In Synthesis of 761446-44-0

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

Pyrazoles and pyrimidines have diverse biological and pharmacological activities. 269410-08-4, formula is C9H15BN2O2, Name is 4-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole. There are a number of antimicrobial compounds containing pyrazole moiety as the core unit. Electric Literature of 269410-08-4.

Finlay, Heather J.;Johnson, James A.;Lloyd, John L.;Jiang, Ji;Neels, James;Gunaga, Prashantha;Banerjee, Abhisek;Dhondi, Naveen;Chimalakonda, Anjaneya;Mandlekar, Sandhya;Conder, Mary Lee;Sale, Harinath;Xing, Dezhi;Levesque, Paul;Wexler, Ruth R. research published 《 Discovery of 5-Phenyl-N-(pyridin-2-ylmethyl)-2-(pyrimidin-5-yl)quinazolin-4-amine as a Potent I_Kur Inhibitor》, the research content is summarized as follows. A new series of phenylquinazoline inhibitors of K_v 1.5 is disclosed. The series was optimized for K_v 1.5 potency, selectivity vs. hERG, pharmacokinetic exposure, and pharmacodynamic potency. 5-Phenyl-N-(pyridin-2-ylmethyl)-2-(pyrimidin-5-yl)quinazolin-4-amine (13k) was identified as a potent and ion channel selective inhibitor with robust efficacy in the preclin. rat ventricular effective refractory period (VERP) model and the rabbit atrial effective refractory period (AERP) model.

269410-08-4, 4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole, also known as 4-Pyrazoleboronic acid pinacol ester , is a useful research compound. Its molecular formula is C9H15BN2O2 and its molecular weight is 194.04 g/mol. The purity is usually 95%.

4-Pyrazoleboronic acid pinacol ester is a useful reagent for Suzuki-Miyaura cross-couplings as well as Ruthenium-catalyzed asymmetric hydrogenation. 4-Pyrazoleboronic acid pinacol ester is also a useful reagent for preparing VEGF, Aurora, RHO (ROCK), Janus Kinase 2, c-MET, ALK, S-nitrsoflutathione reductase, CDC7, Acetyl-CoA carboxylase inhibitors.

4-Pyrazoleboronic acid pinacol ester is used in the preparation of Rho kinase (ROCK) inhibitors as wella s other biologically active compounds.

4-Pyrazoleboronic acid pinacol ester is an organic compound that is the product of a bifunctional coupling reaction between 4-pyrazolecarboxylic acid and pinacol. It has been shown to inhibit protein S6 kinase, which is involved in the regulation of cell growth and proliferation. This compound has also been shown to be effective against cancer cells, including those that are resistant to conventional chemotherapeutic drugs. 4-Pyrazoleboronic acid pinacol ester may also be used as a precursor for other compounds with pharmaceutical activity., Electric Literature of 269410-08-4

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

Pyrazoles are synthesized by the reaction of α,β-unsaturated aldehydes with hydrazine and subsequent dehydrogenation. 2075-46-9, formula is C3H3N3O2, Name is 4-Nitro-1H-pyrazole. Substituted pyrazoles are prepared by condensation of 1,3-diketones with hydrazine (Knorr-type reactions). For example, acetylacetone and hydrazine gives 3,5-dimethylpyrazole. Computed Properties of 2075-46-9.

Fernandez, Belen;Fernandez, Ignacio;Cepeda, Javier;Medina-ODonnell, Marta;Rufino-Palomares, Eva E.;Raya-Baron, Alvaro;Gomez-Ruiz, Santiago;Perez-Jimenez, Amalia;Lupianez, Jose Antonio;Reyes-Zurita, Fernando J.;Rodriguez-Dieguez, Antonio research published 《 Modulating Anticancer Potential by Modifying the Structural Properties of a Family of Zinc Metal-Organic Chains Based on 4-Nitro-1H-pyrazole》, the research content is summarized as follows. The authors synthesized a novel family of metal-organic chains based on 4-nitro-1H-pyrazole linker and zinc as metal center. The authors report the formation of these coordination polymers using hydrothermal routes with water as solvent. These materials display one-dimensional structures with major structural modifications from minimal synthetic variations. What is more interesting, the authors have carried out antitumor measurements, and the authors have related these properties with the structural networks. To the best of the authors’ knowledge, these materials constitute the first examples of polymeric structures for 4-NO₂-pz ligands. NMR and MS spectrometry were used to verify the characterization of the metal complexes in solution to corroborate that these materials are present in the biol. assays.

Computed Properties of 2075-46-9, 4-Nitro-1H-pyrazole, also known as 4-Nitropyrazole, is a useful research compound. Its molecular formula is C3H3N3O2 and its molecular weight is 113.08 g/mol. The purity is usually 95%.

4-Nitropyrazole, is a building block for the synthesis of various pharmaceutical compounds, including inhibitors, and therapeutic agents. It can be used for the synthesis of highly selective, brain-penetrant aminopyrazole LRRK2 Inhibitor, as a potentially viable treatment for Parkinson’s disease., 2075-46-9.

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

Pyrazole is an organic compound with the formula C3H3N2H. It is a heterocycle characterized by a 5-membered ring of three carbon atoms and two adjacent nitrogen atoms, which are in ortho-substitution. 37622-90-5, formula is C6H8N2O2, Name is Ethyl 4-pyrazolecarboxylate. Pyrazoles are a class of compounds that have the ring C3N2 with adjacent nitrogen atoms.Notable drugs containing a pyrazole ring are celecoxib (celebrex) and the anabolic steroid stanozolol. Electric Literature of 37622-90-5.

Fernandes, Celia;Maria, Leonor;Gano, Lurdes;Santos, Isabel C.;Santos, Isabel;Paulo, Antonio research published 《 Re(I) and ^99mTc(I) tricarbonyl complexes with ether-containing pyrazolyl-based chelators: Chemistry, biodistribution and metabolism》, the research content is summarized as follows. Tris(pyrazolyl)methane chelators, L1-L3, containing one or two ether groups at different positions of the azole rings, were synthesized and fully characterized. These chelators enabled the synthesis of fac-[^99mTc(CO)₃{HC[4-(ROCH₂)pz]₃}]⁺ (R = Me (Tc1), Et (Tc2)) and fac-[^99mTc(CO)₃{HC[3,5-(EtOCH₂)₂pz]₃}]⁺ (Tc3) which were identified by HPLC in comparison with the rhenium counterparts. The evaluation of Tc1-Tc3 in CD-1 mice showed that the number and/or nature of the ether groups greatly influence the biodistribution profile, pharmacokinetics and metabolic stability of these complexes. Tc1 and Tc2, bearing a unique ether substituent at the 4-position of the pyrazolyl ring, undergo metabolic transformation in vivo while Tc3 is not metabolized. The metabolization of Tc1 and Tc2 enhanced their rate of excretion but, most probably, also justify their negligible heart uptake in contrast with the high heart uptake of congener non-metabolizable complexes (^99mTc-DMEOP and ^99mTc-TMEOP), which have recently emerged as potential myocardial imaging agents. The attempts made to identify the metabolites of Tc1 and Tc2 showed that the metabolization of these compounds must involve the ether functions with probable formation of carboxylic acid derivatives A comparative study with the congener fac-[^99mTc(CO)₃{[4-(MeOCH₂)pz](CH₂)₂NH(CH₂)₂NH₂}]⁺ (Tc6) led the authors to confirm the formation of such type of metabolites. In fact, Tc6 is also metabolized in mice with formation of fac-[^99mTc(CO)₃{[4-(HOCH₂)pz](CH₂)₂NH(CH₂)₂NH₂}]⁺ (Tc7) and fac-[^99mTc(CO)₃{[4-(HOOC)pz](CH₂)₂NH(CH₂)₂NH₂}]⁺ (Tc8), which were chem. identified by HPLC in comparison with the Re congeners (Re7 and Re8).

37622-90-5, Ethyl 4-pyrazolecarboxylate, also known as Ethyl pyrazole-4-carboxylate, is a useful research compound. Its molecular formula is C6H8N2O2 and its molecular weight is 140.14 g/mol. The purity is usually 95%.

Ethyl pyrazole-4-carboxylate is a low yield, transition metal salt that is used in the synthesis of pyrazoles. It can be synthesized by the reaction of sodium ethoxide with ethyl chloroformate and a Grignard reagent. Sodium ethoxide is added to a suspension of sodium chloride and dried ethyl chloroformate, followed by addition of magnesium turnings. The mixture is refluxed for one hour, cooled, and filtered to give crystals. Ethyl pyrazole-4-carboxylate is used in the preparation of ethyl esters from aliphatic alcohols by reacting with boron trichloride or phosphorus pentachloride. It participates in certain chemical reactions as a byproduct and can damage equipment during chemical reactions. The yield of this compound can be increased by using an excess amount of Grignard reagent or adding hexamethylenetetramine to the reaction mixture, Electric Literature of 37622-90-5

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

Pyrazole and its derivatives are considered a pharmacologically important active scaffold that possesses almost all types of pharmacological activities. 2075-46-9, formula is C3H3N3O2, Name is 4-Nitro-1H-pyrazole. Pyrazole is a weak base, with pKb 11.5 (pKa of the conjugated acid 2.49 at 25 °C).Pyrazole used as a ligand to prepare organometallic compounds. Computed Properties of 2075-46-9.

Feng, Yangbo;Park, HaJeung;Bauer, Luke;Ryu, Jae Cheon;Yoon, Sung Ok research published 《 Thiophene-Pyrazolourea Derivatives as Potent, Orally Bioavailable, and Isoform-Selective JNK3 Inhibitors》, the research content is summarized as follows. Potent JNK3 isoform selective inhibitors were developed from a thiophenyl-pyrazolourea scaffold. Through structure activity relationship (SAR) studies utilizing enzymic and cell-based assays, and in vitro and in vivo drug metabolism and pharmacokinetic (DMPK) studies, potent and highly selective JNK3 inhibitors with oral bioavailability and brain penetrant capability were developed. Inhibitor 17 was a potent and isoform selective JNK3 inhibitor (IC₅₀ = 35 nM), had significant inhibition to only JNK3 in a panel profiling of 374 wild-type kinases, had high potency in functional cell-based assays, had high stability in human liver microsome (t_1/2 = 66 min) and a clean CYP-450 inhibition profile, and was orally bioavailable and brain penetrant. Moreover, cocrystal structures of compounds 17 and 27 in human JNK3 were solved at 1.84 Å, which showed that these JNK3 isoform selective inhibitors bound to the ATP pocket, had interactions in both hydrophobic pocket-I and hydrophobic pocket-II.

2075-46-9, 4-Nitro-1H-pyrazole, also known as 4-Nitropyrazole, is a useful research compound. Its molecular formula is C3H3N3O2 and its molecular weight is 113.08 g/mol. The purity is usually 95%.

4-Nitropyrazole, is a building block for the synthesis of various pharmaceutical compounds, including inhibitors, and therapeutic agents. It can be used for the synthesis of highly selective, brain-penetrant aminopyrazole LRRK2 Inhibitor, as a potentially viable treatment for Parkinson’s disease., Computed Properties of 2075-46-9

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

Pyrazoles can be selectively lithiated at different carbons and subsequently react with electrophiles depending on the substitution patterns. 2075-46-9, formula is C3H3N3O2, Name is 4-Nitro-1H-pyrazole. 1-Methyl-5-(trifluoromethyl)pyrazole underwent deprotonation and subsequent carboxylation mainly or exclusively at either the 4-position of the heterocycle or at the nitrogen-attached methyl group. COA of Formula: C3H3N3O2.

Feng, Pengju;Ma, Guojian;Chen, Xiaoguang;Wu, Xing;Lin, Ling;Liu, Peng;Chen, Tianfeng research published 《 Electrooxidative and Regioselective C-H Azolation of Phenol and Aniline Derivatives》, the research content is summarized as follows. A general and practical protocol was developed for the regioselective C-H azolation of phenol and aniline derivatives by electrooxidative cross-coupling [e.g., 4-methoxyphenol + pyrazole → 4-methoxy-2-(1H-pyrazol-1-yl)phenol (97%)]. The reaction occurs under metal-, oxidant-, and reagent-free conditions, allowing access to a wide variety of synthetically useful heteroarene derivatives The reaction also tolerates a broad range of functional groups and is amenable to gram-scale synthesis. Finally, a preliminary mechanistic study indicated that a radical-radical-combination pathway might be involved in the coupling reaction.

COA of Formula: C3H3N3O2, 4-Nitro-1H-pyrazole, also known as 4-Nitropyrazole, is a useful research compound. Its molecular formula is C3H3N3O2 and its molecular weight is 113.08 g/mol. The purity is usually 95%.

4-Nitropyrazole, is a building block for the synthesis of various pharmaceutical compounds, including inhibitors, and therapeutic agents. It can be used for the synthesis of highly selective, brain-penetrant aminopyrazole LRRK2 Inhibitor, as a potentially viable treatment for Parkinson’s disease., 2075-46-9.

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

Pyrazoles can be selectively lithiated at different carbons and subsequently react with electrophiles depending on the substitution patterns. 761446-44-0, formula is C10H17BN2O2, Name is 1-Methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole. 1-Methyl-5-(trifluoromethyl)pyrazole underwent deprotonation and subsequent carboxylation mainly or exclusively at either the 4-position of the heterocycle or at the nitrogen-attached methyl group. Application of C10H17BN2O2.

Feng, Li;Yu, Shujia;Wang, Hai;Yang, Shengwei;Li, Xue;Dai, Hongjuan;Zhao, Liwen;Jiang, Cheng;Wang, Yazhou research published 《 Synthesis and biological evaluation of spirocyclic chromane derivatives as a potential treatment of prostate cancer》, the research content is summarized as follows. Herein, new compounds from the lead compound A-485 were designed using mol. dynamic simulations. A series of new spirocyclic chroman derivatives was prepared, characterized and proven to be a potential treatment of prostate cancer. The most potent compound I inhibited the proliferation of enzalutamide-resistant 22Rv1 cells with an IC₅₀ value of 96 nM. Furthermore, one of diastereomers of the compound I displayed favorable overall pharmacokinetic profiles, and better tumor growth inhibition than A-485 in an in vivo xenograft model.

Application of C10H17BN2O2, 1-Methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole is a useful research compound. Its molecular formula is C10H17BN2O2 and its molecular weight is 208.07 g/mol. The purity is usually 95%., 761446-44-0.

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

Pyrazole is an organic compound with the formula C3H3N2H. It is a heterocycle characterized by a 5-membered ring of three carbon atoms and two adjacent nitrogen atoms, which are in ortho-substitution. 37622-90-5, formula is C6H8N2O2, Name is Ethyl 4-pyrazolecarboxylate. Pyrazoles are a class of compounds that have the ring C3N2 with adjacent nitrogen atoms.Notable drugs containing a pyrazole ring are celecoxib (celebrex) and the anabolic steroid stanozolol. Application In Synthesis of 37622-90-5.

Fauber, Benjamin P.;Dragovich, Peter S.;Chen, Jinhua;Corson, Laura B.;Ding, Charles Z.;Eigenbrot, Charles;Giannetti, Anthony M.;Hunsaker, Thomas;Labadie, Sharada;Liu, Yichin;Liu, Yingchun;Malek, Shiva;Peterson, David;Pitts, Keith;Sideris, Steve;Ultsch, Mark;VanderPorten, Erica;Wang, Jing;Wei, BinQing;Yen, Ivana;Yue, Qin research published 《 Identification of 2-amino-5-aryl-pyrazines as inhibitors of human lactate dehydrogenase》, the research content is summarized as follows. A 2-amino-5-aryl-pyrazine, e.g. I [R = 2-O₂CC₆H₄, 3-O₂CC₆H₄, 4-O₂CC₆H₄, etc.] was identified as an inhibitor of human lactate dehydrogenase A (LDHA) via a biochem. screening campaign. Biochem. and biophys. experiments demonstrated that the compound specifically interacted with human LDHA. Structural variation of the screening hit resulted in improvements in LDHA biochem. inhibition and pharmacokinetic properties. A crystal structure of an improved compound bound to human LDHA was also obtained and it explained many of the observed structure-activity relationships.

37622-90-5, Ethyl 4-pyrazolecarboxylate, also known as Ethyl pyrazole-4-carboxylate, is a useful research compound. Its molecular formula is C6H8N2O2 and its molecular weight is 140.14 g/mol. The purity is usually 95%.

Ethyl pyrazole-4-carboxylate is a low yield, transition metal salt that is used in the synthesis of pyrazoles. It can be synthesized by the reaction of sodium ethoxide with ethyl chloroformate and a Grignard reagent. Sodium ethoxide is added to a suspension of sodium chloride and dried ethyl chloroformate, followed by addition of magnesium turnings. The mixture is refluxed for one hour, cooled, and filtered to give crystals. Ethyl pyrazole-4-carboxylate is used in the preparation of ethyl esters from aliphatic alcohols by reacting with boron trichloride or phosphorus pentachloride. It participates in certain chemical reactions as a byproduct and can damage equipment during chemical reactions. The yield of this compound can be increased by using an excess amount of Grignard reagent or adding hexamethylenetetramine to the reaction mixture, Application In Synthesis of 37622-90-5

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

Pyrazole and its derivatives are considered a pharmacologically important active scaffold that possesses almost all types of pharmacological activities. 269410-08-4, formula is C9H15BN2O2, Name is 4-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole. Pyrazole is a weak base, with pKb 11.5 (pKa of the conjugated acid 2.49 at 25 °C).Pyrazole used as a ligand to prepare organometallic compounds. Recommanded Product: 4-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole.

Farley, Alistair J. M.;Ermolovich, Yuri;Calvopina, Karina;Rabe, Patrick;Panduwawala, Tharindi;Brem, Jurgen;Bjorkling, Fredrik;Schofield, Christopher J. research published 《 Structural Basis of Metallo-β-lactamase Inhibition by N-Sulfamoylpyrrole-2-carboxylates》, the research content is summarized as follows. Metallo-β-lactamases (MBLs) can efficiently catalyze the hydrolysis of all classes of β-lactam antibiotics except monobactams. While serine-β-lactamase (SBL) inhibitors (e.g., clavulanic acid, avibactam) are established for clin. use, no such MBL inhibitors are available. A report on the synthesis and mechanism of inhibition of N-sulfamoylpyrrole-2-carboxylates (NSPCs) which are potent inhibitors of clin. relevant B1 subclass MBLs, including NDM-1. Crystallog. reveals that the N-sulfamoyl NH₂ group displaces the dizinc bridging hydroxide/water of the B1 MBLs. Comparison of crystal structures of an NSPC and taniborbactam (VRNX-5133), presently in Phase III clin. trials, shows similar binding modes for the NSPC and the cyclic boronate ring systems. The presence of an NSPC restores meropenem efficacy in clin. derived E. coli and K. pneumoniae blaNDM-1. The results support the potential of NSPCs and related compounds as efficient MBL inhibitors, though further optimization is required for their clin. development.

Recommanded Product: 4-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole, 4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole, also known as 4-Pyrazoleboronic acid pinacol ester , is a useful research compound. Its molecular formula is C9H15BN2O2 and its molecular weight is 194.04 g/mol. The purity is usually 95%.

4-Pyrazoleboronic acid pinacol ester is a useful reagent for Suzuki-Miyaura cross-couplings as well as Ruthenium-catalyzed asymmetric hydrogenation. 4-Pyrazoleboronic acid pinacol ester is also a useful reagent for preparing VEGF, Aurora, RHO (ROCK), Janus Kinase 2, c-MET, ALK, S-nitrsoflutathione reductase, CDC7, Acetyl-CoA carboxylase inhibitors.

4-Pyrazoleboronic acid pinacol ester is used in the preparation of Rho kinase (ROCK) inhibitors as wella s other biologically active compounds.

4-Pyrazoleboronic acid pinacol ester is an organic compound that is the product of a bifunctional coupling reaction between 4-pyrazolecarboxylic acid and pinacol. It has been shown to inhibit protein S6 kinase, which is involved in the regulation of cell growth and proliferation. This compound has also been shown to be effective against cancer cells, including those that are resistant to conventional chemotherapeutic drugs. 4-Pyrazoleboronic acid pinacol ester may also be used as a precursor for other compounds with pharmaceutical activity., 269410-08-4.

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

Pyrazoles can be selectively lithiated at different carbons and subsequently react with electrophiles depending on the substitution patterns. 761446-44-0, formula is C10H17BN2O2, Name is 1-Methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole. 1-Methyl-5-(trifluoromethyl)pyrazole underwent deprotonation and subsequent carboxylation mainly or exclusively at either the 4-position of the heterocycle or at the nitrogen-attached methyl group. Application of C10H17BN2O2.

Erra, Montse;Taltavull, Joan;Bernal, Francisco Javier;Caturla, Juan Francisco;Carrascal, Marta;Pages, Lluis;Mir, Marta;Espinosa, Sonia;Gracia, Jordi;Dominguez, Maria;Sabate, Mar;Paris, Stephane;Maldonado, Monica;Hernandez, Begona;Bravo, Monica;Calama, Elena;Miralpeix, Montserrat;Lehner, Martin D.;Calbet, Marta research published 《 Discovery of a Novel Inhaled PI3Kδ Inhibitor for the Treatment of Respiratory Diseases》, the research content is summarized as follows. Oral PI3Kδ inhibitors such as Idelalisib and Duvelisib have shown efficacy as anticancer agents and Idelalisib has been approved for the treatment of three B-cell cancers. However, Idelalisib has a black box warning on its product label regarding the risks of fatal and serious toxicities including hepatic toxicity, severe diarrhea, colitis, pneumonitis, infections, and intestinal perforation. Some of these side effects are mechanism-related and could hinder the development of Idelalisib for less severe conditions. For respiratory diseases, compounds administered by inhalation are delivered directly to the site of action and may improve the therapeutic index of a drug, minimizing undesired side effects. This work describes the discovery and optimization of inhaled PI3Kδ inhibitors intended for the treatment of severe asthma and COPD. Once the potency was in the desired range, efforts were focused on identifying the particular physicochem. properties that could translate into better lung retention. This medicinal chem. exercise led to the identification of LAS195319 as a candidate for clin. development.

761446-44-0, 1-Methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole is a useful research compound. Its molecular formula is C10H17BN2O2 and its molecular weight is 208.07 g/mol. The purity is usually 95%., Application of C10H17BN2O2

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