Day: October 26, 2022

On July 8, 2010, Chuaqui, Claudio; Cossrow, Jennifer; Dowling, James; Guan, Bing; Hoemann, Michael; Ishchenko, Alexey; Jones, John Howard; Kabigting, Lori; Kumaravel, Gnanasambandam; Peng, Hairuo; Powell, Noel; Raimundo, Brian; Tanaka, Hiroko; Van Vloten, Kurt; Vessels, Jeffrey; Xin, Zhili published a patent.Product Details of 1014631-89-0 The title of the patent was Preparation of heteroaryl compounds useful as Raf kinase inhibitors. And the patent contained the following:

The present invention provides compounds I [Cy1 = (un)substituted phenylene, 5-6 membered saturated or partially unsaturated carbocyclylene, 7-10 membered saturated or partially unsaturated bicyclic carbocyclylene, etc.; Cy2 = (un)substituted Ph, 5-8 membered saturated or partially unsaturated carbocyclic ring, 7-10 membered saturated or partially unsaturated bicyclic carbocyclic ring, etc.; L1 = (un)substituted alkylene; L2 = NR1 or C(O)NR1; R, R1 = H, (un)substituted alkyl; ring A = (un)substituted imidazopyridinyl, imidazopyrazinyl; pyrazolopyridinyl, imidazolyl, thiazolyl, etc.] which are useful as inhibitors of Raf protein kinase. Over three-hundred-fifty compounds I were prepared E.g., a multi-step synthesis of the amide II, starting from III, was given. Exemplified compounds were assayed for Raf kinase activity and were found to be inhibitors of Raf kinase (data given). The present invention also provides compositions comprising I, and methods of treating Raf-mediated diseases. The experimental process involved the reaction of 1-(Pyridin-3-yl)-1H-pyrazole-4-carboxylic acid(cas: 1014631-89-0).Product Details of 1014631-89-0

The Article related to heteroaryl imidazopyridine imidazopyrazine pyrazolopyridine imidazole preparation raf kinase inhibitor, amide carboxamide thiazole pyridine preparation raf kinase inhibitor and other aspects.Product Details of 1014631-89-0

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

Ali, Sahar A.; Awad, Samir Mohamed; Said, Ahmed Mohammed; Mahgoub, Shahenda; Taha, Heba; Ahmed, Naglaa Mohamed published an article in 2020, the title of the article was Design, synthesis, molecular modelling and biological evaluation of novel 3-(2-naphthyl)-1-phenyl-1H-pyrazole derivatives as potent antioxidants and 15-Lipoxygenase inhibitors.Safety of 3-(Naphthalen-2-yl)-1-phenyl-1H-pyrazole-4-carbaldehyde And the article contains the following content:

Oxidative stress is one of the main causes of significant severe diseases. The discovery of new potent antioxidants with high efficiency and low toxicity is a great demand in the field of medicinal chem. Herein, we report the design, synthesis mol. modeling and biol. evaluation of novel hybrids containing pyrazole, naphthalene and pyrazoline/isoxazoline moiety. Chalcones were synthesized efficiently and were used as starting materials for synthesis of a variety of heterocycles. A novel series of pyrazoline , phenylpyrazoline , isoxazoline and pyrazoline carbothioamide derivatives were synthesized and screened for in vitro antioxidant activity using 2,2-diphenyl-1-picrylhydrazyl (DPPH), nitric oxide (NO) and superoxide radical scavenging assay as well as 15-lipoxygenase (15-LOX) inhibition activity. Compounds and showed excellent radical scavenging activity in all three methods in comparison with ascorbic acid and 15-LOX inhibition potency using quercetin as standard then were subjected to in vivo study. Catalase (CAT) activity, glutathione (GSH) and malondialdehyde (MDA) levels were assayed in liver of treated rats. Compounds and showed significant in vivo antioxidant potentials compared to control group at dose of 100 mg/kg B. W. Mol. docking of compound endorsed its proper binding at the active site pocket of the human 15-LOX which explains its potent antioxidant activity in comparison with standard ascorbic acid. The experimental process involved the reaction of 3-(Naphthalen-2-yl)-1-phenyl-1H-pyrazole-4-carbaldehyde(cas: 36640-53-6).Safety of 3-(Naphthalen-2-yl)-1-phenyl-1H-pyrazole-4-carbaldehyde

The Article related to naphthyl phenyl pyrazole derivative preparation antioxidants lipoxygenase inhibitor, 15-lipoxygenase inhibitors, pyrazole, antioxidant activity, hybrids, scavenging activity and other aspects.Safety of 3-(Naphthalen-2-yl)-1-phenyl-1H-pyrazole-4-carbaldehyde

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

On September 8, 2005, Arora, Nidhi; Billedeau, Roland Joseph; Dewdney, Nolan James; Gabriel, Tobias; Goldstein, David Michael; O’Yang, Counde; Soth, Michael published a patent.Electric Literature of 85426-79-5 The title of the patent was Preparation of fused pyrazolo pyrimidine and pyrazolo pyrimidinone derivatives as p38 kinase inhibitors. And the patent contained the following:

The title compounds I-III [R1 = (hetero)aryl, aralkyl, cycloalkyl; R2 = (hetero)aryl, cycloalkyl, alkyl, heterocyclyl; R3 = H, alkyl; R4 = H, alkyl, OH, etc.; R5 = H, alkyl, heteroalkyl, etc.; X, Y = N, or one of X and Y = N and the other = CR6 (R6 = H, alkyl, OH, etc.); Z = N, CR6; W = O, SOm, CH2, (un)substituted NH; m = 0-2; A = O, CH2, SOm, C(O), etc.; B = O, SOm, C(O), etc.; k = 0-1], useful in treating p38 mediated disorders, were prepared and formulated. E.g., a multi-step synthesis of (S)-IV, starting from 4,6-dichloro-2-(methylthio)pyrimidine and 2-chlorobenzaldehyde, was given. The compounds I were found to be inhibitors of p38 MAP kinase. IV showed a p38 IC50 of 0.004 μM. The experimental process involved the reaction of 4-Chloro-6-(methylthio)-1H-pyrazolo[3,4-d]pyrimidine(cas: 85426-79-5).Electric Literature of 85426-79-5

The Article related to fused pyrazolo pyrimidine pyrimidinone preparation p38 kinase inhibitor, pyrazolopyrimidine preparation p38 kinase inhibitor, pyrazolopyrimidinone preparation p38 kinase inhibitor and other aspects.Electric Literature of 85426-79-5

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

On March 11, 2015, Morrison, Angus; Carswell, Emma; Armer, Richard; Pesnot, Thomas; Bingham, Matilda; Bhamra, Inder; Kirkham, James; Colbon, Paul; Avery, Craig; McCarroll, Andrew; Testar, Richard published a patent.Category: pyrazoles-derivatives The title of the patent was Preparation of triazole derivatives as inhibitors of Raf kinases. And the patent contained the following:

Triazolyl compounds of formula [I; A = a 5-membered heterocyclic moiety; B = C6-14 aryl or C5-14 heteroaryl; L = ·SO 2 NRa , where Ra = H, C1-4 alkyl or C1-4 haloalkyl; R1 = C1-6 alkyl, C1-6 alkenyl, C1-6 alkynyl, C3-14 carbocyclyl or C3-14 heterocyclyl, each optionally substituted with 1-5 substituents selected from halo, ORb , SRb , NRbRc, NO, oxo, cyano, C1-4 acyl, C1-6 alkyl, C1-6 haloalkyl, C3-8 cycloalkyl, C(O)Rb and C(O)ORb ; R2 = H, halo, C1-4 alkyl or C1-4 haloalkyl; R3 = H, C1-6 alkyl, C1-6 haloalkyl, C3-8 cycloalkyl, or C3-8 heterocycloalkyl; R4 = H, halo, OR5 , SR5 , NR5R6, NO, oxo, cyano, acyl, C(O)ORb , C(O)NRbRc , C1-6 alkyl, C3-14 carbocyclyl or C3·14 heterocyclyl; R5 and R6 are H, C(O)Rb, C1-4 alkyl, C1-4 haloalkyl, C3-8 carbocyclyl or C3-8 heterocyclyl; Rb, Rc = H, C1-4 alkyl, C1-4 haloalkyl, C1-4 acyl, C3-7 cycloalkyl or C3-7 halocycloalkyl; m = 0-3; n = 0-2] are prepared These compounds may be useful as inhibitors of Raf kinases, e.g. B-Raf and C-Raf. The invention also contemplates the use of the compounds for treating conditions treatable by the inhibition of Raf kinases, for example cancer, including lymphoma, leukemia and melanoma. Thus, N-[3-(5-bromo-2-tert-butyltriazol-4-yl)-2-fluorophenyl]-2,5-difluorobenzenesulfonamide was coupled with a mixture of 3-methoxy-1-tetrahydropyran-2-yl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)pyrazole and 5-methoxy-1-tetrahydropyran-2-yl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)pyrazole in the presence of tripotassium phosphate, tricyclohexylphosphine, and tris(dibenzylideneacetone)dipalladium(0) in DMF and water under heating in a microwave at 130° for 3 h to give N-[3-[2-tert-butyl-5-(3-methoxy-1-tetrahydropyran-2-ylpyrazol-4-yl)triazol-4-yl]-2-fluorophenyl]-2,5-difluorobenzenesulfonamide and N-[3-[2-tert-butyl-5-(5-methoxy-1-tetrahydropyran-2-ylpyrazol-4-yl)triazol-4-yl]-2-fluorophenyl]-2,5-difluorobenzenesulfonamide as an inseparable mixture which was stirred p-toluenesulfonic acid monohydrate in methanol for a total of 72 h to give N-[3-[2-tert-butyl-5-(3-methoxy-1H-pyrazol-4-yl)triazol-4-yl]-2-fluorophenyl]-2,5-difluorobenzenesulfonamide (II). II showed IC50 of <15 nM against B-Raf and C-Raf kinase, resp. The experimental process involved the reaction of 5-Methoxy-1H-pyrazole(cas: 215610-30-3).Category: pyrazoles-derivatives

The Article related to triazole preparation inhibitor raf kinase, pyrazolyltriazolylphenylbenzenesulfonamide preparation inhibitor raf kinase, cancer lymphoma leukemia melanoma treatment triazole preparation and other aspects.Category: pyrazoles-derivatives

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

On January 7, 2016, Chen, Wei; Wang, Longcheng; Yan, Shunqi; Loury, David J.; Jia, Zhaozhong J.; Frye, Leah Lynn; Greenwood, Jeremy Robert; Shelley, Mee Yoo; Atallah, Gordana Babic; Zanaletti, Riccardo; Catalani, Maria Pia; Raveglia, Luca Francesco published a patent.Recommanded Product: 924909-16-0 The title of the patent was Preparation of substituted pyrazolopyridines as inhibitors of Bruton’s tyrosine kinase. And the patent contained the following:

The title compounds I [one of W1 and W2 = C(R9), or N; and the other C(R9); Z = C(R9) or N; L1 = N(R5), O, S or alkyl; T1 = O, N(R5), S, alkylene, or a single bond; Cy1 = substituted aryl or heteroaryl; Cy2 = (un)substituted heterocycloalkyl, aryl, cycloalkyl, or heteroaryl; R1 = H, halo, alkyl, etc; R5 = H, alkyl, heteroalkyl; or when each of L1 and T1 = (independently) N(R5), then the two R5 may join together to form (un)substituted heterocycle; each R9 = (independently) H, halo, CN, etc.] that inhibit Bruton’s tyrosine kinase (Btk), were prepared and formulated. E.g., a multi-step synthesis of 3-hydrazinylpropanenitrile, was described. The Btk IC50 of compounds I was determined in both a cellular kinase assay and in a cellular functional assay of BCR-induced calcium flux (data given). Also described are irreversible inhibitors of Btk. In addition, reversible inhibitors of Btk are also described. Also disclosed are pharmaceutical compositions that include the compounds I. Methods of using the Btk inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions. The experimental process involved the reaction of 1-(4-Methoxybenzyl)-1H-pyrazolo[3,4-b]pyridin-4-ol(cas: 924909-16-0).Recommanded Product: 924909-16-0

The Article related to pyrazolopyridine preparation bruton’s tyrosine kinase btk inhibitor antitumor antiinflammatory, lymphoma autoimmune heteroimmune disease treatment pyrazolopyridine preparation btk inhibitor and other aspects.Recommanded Product: 924909-16-0

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

On December 31, 2007, Shelke, S. N.; Dalvi, N. R.; Gill, C. H.; Karale, B. K. published an article.Synthetic Route of 36640-53-6 The title of the article was Synthesis of various heterocycles from 3-(2-naphthalenyl)-1-phenyl-1H-pyrazole-4-carboxaldehyde. And the article contained the following:

Condensation of the title compound (I) with 2′-hydroxyacetophenones gave propenones II (R1 = H, Cl, Me; R2, R4 = H, Me; R3 = H, Cl, Me, Et, Br, F), which reacted with hydrazine to give pyrazolines III and with iodine in DMSO to give chromones IV. Reaction of IV with hydrazine gave bipyrazoles V. The experimental process involved the reaction of 3-(Naphthalen-2-yl)-1-phenyl-1H-pyrazole-4-carbaldehyde(cas: 36640-53-6).Synthetic Route of 36640-53-6

The Article related to pyrazolecarboxaldehyde condensation hydroxyacetophenone, pyrazolylpyrazoline aryl derivative preparation, pyrazolylchromone aryl derivative preparation, bipyrazole aryl derivative preparation and other aspects.Synthetic Route of 36640-53-6

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

On May 31, 2011, Wenglowsky, Steve; Ren, Li; Ahrendt, Kateri A.; Laird, Ellen R.; Aliagas, Ignacio; Alicke, Bruno; Buckmelter, Alex J.; Choo, Edna F.; Dinkel, Victoria; Feng, Bainian; Gloor, Susan L.; Gould, Stephen E.; Gross, Stefan; Gunzner-Toste, Janet; Hansen, Joshua D.; Hatzivassiliou, Georgia; Liu, Bonnie; Malesky, Kim; Mathieu, Simon; Newhouse, Brad; Raddatz, Nicholas J.; Ran, Yingqing; Rana, Sumeet; Randolph, Nikole; Risom, Tyler; Rudolph, Joachim; Savage, Scott; Selby, LeAnn T.; Shrag, Michael; Song, Kyung; Sturgis, Hillary L.; Voegtli, Walter C.; Wen, Zhaoyang; Willis, Brandon S.; Woessner, Richard D.; Wu, Wen-I.; Young, Wendy B.; Grina, Jonas published an article.Computed Properties of 1186608-73-0 The title of the article was Pyrazolopyridine Inhibitors of B-RafV600E. Part 1: The Development of Selective, Orally Bioavailable, and Efficacious Inhibitors. And the article contained the following:

The V600E mutation of B-Raf kinase results in constitutive activation of the MAPK signaling pathway and is present in approx. 7% of all cancers. Using structure-based design, a novel series of pyrazolopyridine inhibitors of B-RafV600E was developed. Optimization led to the identification of 3-methoxy pyrazolopyridines 17 and 19, potent, selective, and orally bioavailable agents that inhibited tumor growth in a mouse xenograft model driven by B-RafV600E with no effect on body weight On the basis of their in vivo efficacy and preliminary safety profiles, 17 and 19 were selected for further preclin. evaluation. The experimental process involved the reaction of 3-Methyl-1H-pyrazolo[3,4-b]pyridin-5-amine(cas: 1186608-73-0).Computed Properties of 1186608-73-0

The Article related to pyrazolopyridine derivative braf kinase inhibitor preparation antitumor pharmacokinetics toxicity, b-rafv600e, mapk pathway, amorphous spray-dried dispersion, pyrazolopyridine, targeted therapy and other aspects.Computed Properties of 1186608-73-0

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

On December 31, 2012, Ablajan, Keyume; Wang, Liju published an article.Synthetic Route of 36640-53-6 The title of the article was Convenient synthesis and characterization of hydrazone derivatives of 3-(2-naphthyl)-1-phenyl-pyrazole-4-carbaldehyde. And the article contained the following:

In order to obtain novel hydrazone derivatives containing pyrazole and thiazole rings which possess certain biol. activity, a series of 1-(3-β-naphthyl-1-phenylpyrazole-4-methylene)-2-(4-arylthiazol-2-yl)hydrazones I(R = Ph, 4-Me-C6H4, 4-MeO-C6H4, 4-Cl-C6H4, 4-NO2-C6H4, 4-Br-C6H4, 2-naphthyl) were synthesized via two different methods including multi step reactions and one-pot synthetic route using 3-β-naphthyl-1-phenyl-pyrazole-4-carbaldehyde as a starting intermediate. The products were obtained in good yield under ultrasonic irradiation condition rather than heating. The structures of products were characterized by 1H NMR, MS and elemental anal. The preliminary bioassay showed that compounds I(R = 4-Me-C6H4, 4-Cl-C6H4) possess obvious protective effects on the PC12 cells injury induced by H2O2. The experimental process involved the reaction of 3-(Naphthalen-2-yl)-1-phenyl-1H-pyrazole-4-carbaldehyde(cas: 36640-53-6).Synthetic Route of 36640-53-6

The Article related to naphthylphenylpyrazolemethyleneaiylthiazolylhydrazone preparation pc12 cell protection, naphthylphenylpyrazole carbaldehyde preparation hydrazinecarbothioamide arylcarbonylmethyl bromide cyclocondensation and other aspects.Synthetic Route of 36640-53-6

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

On May 31, 2003, Kim, Dong Chan; Lee, Yeo Ran; Yang, Beom-Seok; Shin, Kye Jung; Kim, Dong Jin; Chung, Bong Young; Yoo, Kyung Ho published an article.Quality Control of 4-Chloro-6-(methylthio)-1H-pyrazolo[3,4-d]pyrimidine The title of the article was Synthesis and biological evaluations of pyrazolo[3,4-d]pyrimidines as cyclin-dependent kinase 2 inhibitors. And the article contained the following:

A series of 1,4,6-trisubstituted pyrazolo[3,4-d]pyrimidines capable of selectively inhibiting CDK2 activity were synthesized by derivatization at C-4, C-6 and N-1 with various amines and lower alkyl groups. For above synthetic compounds, biol. evaluation was carried out and structure-activity relationship was examined In the series, 4-anilino compounds exhibited better CDK2 inhibitory activity and antitumor activity compared to 4-benzyl compounds Two compounds having a 3-fluoroaniline group at C-4 showed comparable or superior CDK2 inhibitory activity to those of olomoucine and roscovitine as reference compounds In general, the unsubstituted compounds at N-1 possessed higher potency than the substituted compounds for the CDK2 inhibitory activity. As for EGFR inhibitory activity, most compounds did not have a significant activity. Two compounds exhibited potent cell growth inhibitory activity against human cancer cell lines, but their CDK2 inhibitory activities were slightly poorer than olomoucine. The experimental process involved the reaction of 4-Chloro-6-(methylthio)-1H-pyrazolo[3,4-d]pyrimidine(cas: 85426-79-5).Quality Control of 4-Chloro-6-(methylthio)-1H-pyrazolo[3,4-d]pyrimidine

The Article related to pyrazolopyrimidine preparation cyclin dependent kinase 2 inhibitor, cdk2 inhibitor pyrazolopyrimidine preparation, egfr inhibitor pyrazolopyrimidine preparation, antitumor agent pyrazolopyrimidine preparation and other aspects.Quality Control of 4-Chloro-6-(methylthio)-1H-pyrazolo[3,4-d]pyrimidine

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

On June 2, 2011, Demeese, Jason; Gaudino, John; Neitzel, Alicia Tarin; Lunghofer, Paul; Seo, Jeongbeob; Tian, Hongqi; Young, Wendy B.; Sutherlin, Daniel P. published a patent.Formula: C14H13N3O2 The title of the patent was Preparation of pyrazolopyridines as tyrosine kinase inhibitors. And the patent contained the following:

Compounds of Formulas Ia and Ib, and stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting receptor tyrosine kinases and for treating disorders mediated thereby. Methods of using compounds of Formula Ia and Ib, and stereoisomers, geometric isomers, tautomers, solvates and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathol. conditions are disclosed. Title compounds[I, II; X = O, S, NR10; W = O, S, SO, SO2; R1 = H, alkyl, alkenyl, alkynyl, CONR10R11, (substituted) carbocyclyl, heterocyclyl, aryl, heteroaryl, etc.; R2 = H, CF3, cyano, NR10R11, (substituted) alkyl, alkenyl, alkynyl, carbocyclyl, heterocyclyl, aryl, heteroaryl, etc.; R3 = (substituted) carbocyclyl, heterocyclyl, aryl, heteroaryl; R4 = H, F, Cl, Br, CF3, cyano, NR10R11, OR10, etc.; R10, R11 = H, (substituted) alkyl, alkenyl, alkynyl, carbocyclyl, heteroaryl, etc.], were prepared as c-MET kinase inhibitors (no data). Thus, title compound (III) was prepared in 13 steps from 2,2-dimethyl-1,3-dioxane-4,6-dione, 1-(4-methoxybenzyl)-1H-pyrazol-5-amine, 1,2-difluoro-4-nitrobenzene, 1-(4-fluorophenyl)hydrazine hydrochloride, 1,3-dioxane-4,6-dione, and tert-Bu 4-hydroxypiperidine-1-carboxylate. The experimental process involved the reaction of 1-(4-Methoxybenzyl)-1H-pyrazolo[3,4-b]pyridin-4-ol(cas: 924909-16-0).Formula: C14H13N3O2

The Article related to pyrazolopyridine preparation tyrosine kinase inhibitor, cmet kinase inhibitor piperidinyloxypyrazolopyridine preparation, cancer stroke diabetes hepatomegaly alzheimers treatment phenoxypyrazolopyridine preparation and other aspects.Formula: C14H13N3O2

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