Day: October 26, 2022

On July 25, 2019, Blake, James F.; Dai, Donghua; Haas, Julia; Jiang, Yutong; Kolakowski, Gabrielle R.; Metcalf, Andrew T.; Moreno, David A.; Prigaro, Brett; Ren, Li published a patent.Recommanded Product: 1028092-65-0 The title of the patent was Preparation of substituted pyrazolo[3,4-d]pyrimidine compounds as RET kinase inhibitors. And the patent contained the following:

The invention is related to the preparation of compounds I [R1 = (un)substituted 5-membered heteroaryl ring having 2-3 ring heteroatoms independently selected from N, O and S, provided that when R1 is an isoxazolyl ring, then R1 is substituted with 2 specified substituents; R2 = H, alkyl, cyanoalkyl, etc.], their tautomers, stereoisomers, pharmaceutically acceptable salts and solvates, which are inhibitors of RET kinase and are useful in the treatment and prevention of diseases which can be treated with a RET kinase inhibitor, including diseases or disorders mediated by a RET kinase. Thus, II was prepared in 5 steps from 5-cyclopropylisoxazole-3-carboxylic acid and malononitrile using isopropylhydrazine hydrochloride, formamide, NBS and 1-methyl-3-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole. I were screened for their ability to inhibit several RET kinase forms (wild type, V804M M918T, G810R, and G810S mutants) (data given for representative compounds I in an enzyme assay and/or cell assay). Pharmaceutical compositions comprising compound I, alone or in combination with an addnl. therapy or therapeutic agent, were disclosed. 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).Recommanded Product: 1028092-65-0

The Article related to pyrazolopyrimidine preparation ret kinase inhibitor antitumor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Recommanded Product: 1028092-65-0

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

On April 1, 2021, Xie, Yinong; Babiss, Lee E. published a patent.SDS of cas: 98138-75-1 The title of the patent was Preparation of SHP2 inhibitors for treatment of cancer. And the patent contained the following:

Disclosed are compounds of formula I, useful as inhibitors of protein tyrosine phosphatase SHP2 for the treatment of cancer. Compounds of formula I [wherein X = S; Ring A = (un)substituted aryl having 6-10 carbons, (un)substituted 5- to 6-membered mono-cyclic heteroaryl, or (un)substituted bicyclic ring system having 5-10 ring carbons; RA and RB independently = H or C1-12 hydrocarbyl, or N(RA)(RB) optionally = substituted heterocyclic ring system] or pharmaceutically acceptable salts thereof, are claimed and exemplified. Thus, disubstituted 1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one II was prepared from a multistep synthesis (preparation given). Exemplified I were evaluated for inhibition of SHP2 from which II demonstrated an IC50 = ≤ 50 nM. The pharmaceutical compositions comprising compounds of Formula I, methods of synthesis of these compounds, methods of treatment for diseases associated with the aberrant activity of SHP2 such as cancer using these compounds or compositions containing these compounds are also disclosed. The experimental process involved the reaction of 6-Chloro-4-methoxy-1H-pyrazolo[3,4-d]pyrimidine(cas: 98138-75-1).SDS of cas: 98138-75-1

The Article related to dihydropyrazolopyrimidinone preparation shp2 inhibitor preparation inhibitor cancer, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.SDS of cas: 98138-75-1

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

On April 30, 2009, Barlaam, Bernard Christophe; Bower, Justin Fairfield; Delouvrie, Benedicte; Fairley, Gary; Harris, Craig Steven; Lambert, Christine; Ouvry, Gilles; Winter, Jon James Gordon published a patent.Category: pyrazoles-derivatives The title of the patent was Pyridine and pyrazine derivatives as Axl and/or c-Met receptor enzyme inhibitors and their preparation, pharmaceutical compositions and use in the treatment of tumors. And the patent contained the following:

The invention concerns pyridine a nd pyrazine derivatives of formula I or a pharmaceutically-acceptable salt thereof, processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the treatment of tumors. Compounds of formula I wherein W is CH and N; J is O and S; each G1, G2, G3 and G4 is CH and N, proved that no more than two of G1,G2, G3 and R4 is N; A is (un)substituted Ph, (un)substituted 5- to 6-membered monocyclic heteroaryl; and (un)substituted 8- to 10-membered bicyclic ring; each R3 is independently H, halo, CN, amino, sulfamoyl, CF3, C1-8 alkyl, etc.; n is 0, 1, 2, and 3; and pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by cyclization of 2-aminophenol with 2-amino-5-bromopyridine-3-carboxylic acid; the resulting 3-(benzoxazol-2-yl)-5-bromopyridin-2-amine underwent cross-coupling with 4-(dimethylaminomethyl)phenylboronic acid to give compound II. All the invention compounds were evaluated for their Axl and c-Met receptor tyrosine kinase inhibitory activity. From the Axl tyrosine kinase assay, it was determined that compound II exhibited 99.8 % inhibition at 1 μM concentration The experimental process involved the reaction of 5-Methoxy-1H-pyrazole(cas: 215610-30-3).Category: pyrazoles-derivatives

The Article related to pyridine preparation axl cmet tyrosine kinase inhibitor treatment tumor, pyrazine preparation axl cmet tyrosine kinase inhibitor treatment tumor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Category: pyrazoles-derivatives

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

On July 29, 2022, Perma Tenzin, Puno; Sun, Handong; Zhou, Yuanfei; Yan, Bingchao; Yang, Qian; Du, Xue; Hu, Kun published a patent.Related Products of 1014631-89-0 The title of the patent was Preparation of ent-kauranoid derivatives as antitumor drugs. And the patent contained the following:

The invention discloses a preparation of ent-kauranoid derivatives I [wherein R=(un)substituted C3-C8 alkyl and cycloalkyl, heterocyclic group containing N, O, S, substituted Ph, etc.] as antitumor drugs, which has the advantages of easy availability of raw materials, high yield and good anti-tumor effect. For example, (3aS,5aR,6S,7aR,10S,12aS,12bR,13R)-6-hydroxy-5,5-dimethyl-9-methylene-3,7,8-trioxododecahydro-1H,3H-7a,10-methanocyclohepta[6,7]indeno[1,7a-c]furan-13-yl butyrate was prepared by the following steps: oxidation of oridonin; selective reduction; diazotization; oxidation; rearrangement reaction; cyclization to obtain calyx lactone B; esterification. The title compound is used to prepare anti-tumor drugs, and tumors include cervical cancer, colon cancer, ovarian cancer, lung cancer, prostate cancer, breast cancer and liver cancer. The experimental process involved the reaction of 1-(Pyridin-3-yl)-1H-pyrazole-4-carboxylic acid(cas: 1014631-89-0).Related Products of 1014631-89-0

The Article related to preparation ent kauranoid antitumor oxidation reduction diazotization cyclization esterification, Terpenes and Terpenoids: Diterpenes (C20), Including Gibberellins, Retinoids, Quassinoids, and Tocopherols and other aspects.Related Products of 1014631-89-0

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

Kikalishvili, T. Dzh.; Kereselidze, Dzh. A. published an article in 2002, the title of the article was Quantum-chemical study of some physico-chemical properties of derivatives of pyrazole.COA of Formula: C4H6N2O And the article contains the following content:

By modern semiempirical quantum-chem. method the charges on the atoms, dipole moments, and ionization potentials of derivatives of pyrazole were calculated and the correlation anal. using Taft’s substituent constants was carried out. The possibility of quant. description of reactivity of pyrazoles was shown. The experimental process involved the reaction of 5-Methoxy-1H-pyrazole(cas: 215610-30-3).COA of Formula: C4H6N2O

The Article related to pyrazole derivative structure property reactivity, Physical Organic Chemistry: Theoretical Organic Chemical Concepts, Including Quantum and Molecular Mechanical Studies and other aspects.COA of Formula: C4H6N2O

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

On September 23, 2021, Holson, Edward; Blum, Charles published a patent.Electric Literature of 1014631-89-0 The title of the patent was Preparation of benzenesulfonamide derivatives as TRAP1 modulators and uses thereof. And the patent contained the following:

The disclosure provides compounds of formula I and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled compounds, and prodrugs thereof. The provided compounds may be tumor necrosis factor (“”TNF””) receptor associated protein 1 (“”TRAP1″”) modulators (e.g., TRAP1 activators). The provided compounds of formula I may also rescue the activity in PTEN-induced kinase 1 (“”PINK1″”) loss of function contexts. The provided compounds of formula I may also improve mitochondrial health, function, quality, quantity, and/or activity, and/or reduce the production of reactive oxygen species. The provided compounds of formula I may also refold or solubilize aggregated or misfolded proteins such as α-synuclein. The disclosure also provides pharmaceutical compositions comprising the provided compounds; kits comprising the provided compounds or pharmaceutical compositions; and methods of using the provided compounds and pharmaceutical compositions (e.g., for treating a disease in a subject in need thereof). Compounds of formula I wherein A and E are independently aryl and heteroaryl; dashed bonds are single and double bonds are valency permits; m is 0, 1 and 2; n and p are independently 0 – 13; each R1 is independently halo, (un)substituted alkyl, (un)substituted alkenyl, (un)substituted alkynyl, etc.; R3 and R6 are independently H, (un)substituted alkyl and nitrogen protecting group; R1R3 may be taken together to form (un)substituted heterocyclyl; each R4 is independently halo, (un)substituted alkyl, (un)substituted alkenyl, (un)substituted aryl, etc.; R5 and R9 are independently H, halo, (un)substituted alkyl, (un)substituted alkenyl, (un)substituted alkynyl, etc.; each R7 is independently (un)substituted alkyl, (un)substituted alkenyl, (un)substituted alkynyl, (un)substituted aryl, etc.; and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled compounds, and prodrugs thereof, are claimed. Example compound II was prepared by amidation of oxazole-5-carboxylic acid with 5-amino-N-(4-bromophenyl)-2-methoxybenzenesulfonamide. The invention compounds were evaluated for their TRAP1 modulatory activity. From the assay, it was determined that compound II exhibited an EC50 value in the range of 20μM to 100μM and an Emax value in the range of 160 – 199%. The experimental process involved the reaction of 1-(Pyridin-3-yl)-1H-pyrazole-4-carboxylic acid(cas: 1014631-89-0).Electric Literature of 1014631-89-0

The Article related to benzenesulfonamide preparation trap1 modulator, Benzene, Its Derivatives, and Condensed Benzenoid Compounds: Amides, Amidines, Imidic Esters, Hydrazides, and Hydrazonic Esters and other aspects.Electric Literature of 1014631-89-0

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

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