pyrazoles-derivatives

On January 6, 2022, Reynolds, Dominic; Seiler, Michael W.; Agrawal, Anant A.; Vaillancourt, Frederic; Smith, Peter; Hopper, Allen T.; Prajapati, Sudeep; Vyskocil, Stepan published a patent.HPLC of Formula: 2089292-88-4 The title of the patent was Preparation of 2-(indazol-5-yl)-6-(piperidin-4-yl)-1,7-naphthyridine derivatives and related compounds as modulators for splicing nucleic acids for the treatment of proliferative diseases. And the patent contained the following:

The disclosure relates to the title compounds I, wherein A and B are independently (un)substituted heterocyclyl and heteroaryl; L1 and L2 are independently absent, O, CO, etc.; X and Y are independently N and CR6; R2 and R3 are independently C1-6 alkyl, halo, CN, etc.; R6 is H, halo, CN, etc.; m = 0-1; N = 0-2; and pharmaceutically acceptable salts thereof, solvates, hydrates, tautomers, and stereoisomers thereof, that modulate nucleic acid splicing, e.g., splicing of a pre-mRNA, as well as methods of use thereof. Example compound II was prepared by a multistep procedure (procedure given). Compounds described herein were used to modulate RNA transcript abundance in cells (data given for representative compounds I). The experimental process involved the reaction of 5-Bromo-2-methyl-2H-pyrazolo[3,4-c]pyridine(cas: 2089292-88-4).HPLC of Formula: 2089292-88-4

The Article related to indazolyl piperidinylnaphthyridine preparation nucleic acid mrna splicing modulator antiproliferative, Heterocyclic Compounds (More Than One Hetero Atom): Fused-Ring Systems With Two Or More Hetero Atoms, No More Than One Hetero Atom Per Ring and other aspects.HPLC of Formula: 2089292-88-4

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

On August 5, 2021, Wilson, Kevin J.; Schiller, Shawn E.R.; Negretti, Solymar published a patent.Related Products of 215610-30-3 The title of the patent was Carboxamide compounds for the treatment of BAF complex-related diseases and their preparation. And the patent contained the following:

The disclosure features compounds of formula I useful for the treatment of BAF complex-related disorders. Compounds of formula I wherein A is substituted oxetan-3-ylphenyl, (un)substituted bicyclic heterocyclic ring system; B is (un)substituted 6-membered heteroarylene and (un)substituted 9- to 10-membered bicyclic heteroarylene; L is a covalent bond, (un)substituted C1-3 alkylene, C2 alkynylene, (un)substituted C2 alkenylene, etc.; E is (un)substituted 3- to 10-membered cycloalkylene, (un)substituted 6- to 10-membered aryl, (un)substituted 5- to 10-membered heteroaryl, etc.; M is absent, (CR2R3)1-3; R1 is H and (un)substituted C1-6 alkyl; R2 and R3 are independently H, (un)substituted C1-6 alkyl and (un)substituted C1-6 heteroalkyl; and pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by cross-coupling of tert-Bu N-[(4-bromo-2-pyridyl)methyl]carbamate with Me 3-ethynylbenzoate; the resulting Me 3-[2-[2-[(tert-butoxycarbonylamino)methyl]-4-pyridyl]ethynyl]benzoate underwent hydrolysis to give Me 3-[2-[2-(aminomethyl)-4-pyridyl]ethynyl]benzoate, which underwent N-acylation with (4R)-4-cyano-4-methyl-chromane-6-carboxylic acid to give compound II. The invention compounds were evaluated for BRM and BRG1 inhibitory activity (some data given). The experimental process involved the reaction of 5-Methoxy-1H-pyrazole(cas: 215610-30-3).Related Products of 215610-30-3

The Article related to carboxamide preparation treatment baf complex disease, Heterocyclic Compounds (One Hetero Atom): Benzopyrans (Including Coumarins, Isocoumarins, Chromones, Benzopyrones, Dibenzopyrans, and Other Arenopyrans) and other aspects.Related Products of 215610-30-3

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

On November 30, 2016, Ashok, Dongamanti; Rangu, Kavitha; Gundu, Srinivas; Rao, Velagapuri Hanumantha published an article.Application In Synthesis of 3-(Naphthalen-2-yl)-1-phenyl-1H-pyrazole-4-carbaldehyde The title of the article was Synthesis of pyrazolylfuro[2,3-f]chromenes and evaluation of their antimicrobial activity. And the article contained the following:

A new series of furochromene-based pyrazole derivatives were synthesized from their chalcone precursors upon reaction with 2-bromo-1-(4-bromophenyl)ethanone in the presence of anhydrous K2CO3 under conventional, ultrasound and microwave irradiation The shorter reaction times and high yields render the microwave irradiation approach as an advanced method to synthesize the title compounds All obtained compounds were evaluated for their antimicrobial activity against various bacterial and fungal strains. Most of the compounds exhibited variable range of antimicrobial activity and few compounds emerged as prospective antimicrobial agents by displaying promising microbial inhibitory potency. 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 bromobenzoyl aryl phenylpyrazolylvinyl furochromene diastereoselective preparation antibacterial antifungal sar, Heterocyclic Compounds (One Hetero Atom): Benzopyrans (Including Coumarins, Isocoumarins, Chromones, Benzopyrones, Dibenzopyrans, and Other Arenopyrans) 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 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 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