Category: 215610-30-3

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

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 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 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 April 1, 2021, Richards, Nicole; Lewis, Richard; Hamilton, Matthew; Ray, William; Alvarez, Fernando; Pfaffinger, Dana; Reyna, Naphtali; Cross, Jason; Ramaswamy, Suyambu Kesava Vijayan; Bardenhagen, Jennifer; Lightfoot, Yaima Luzardo; Acton, Paul; Goodwani, Sunil published a patent.Reference of 5-Methoxy-1H-pyrazole The title of the patent was Preparation of 1-[(4,5-dihydro-1H-pyrazol-1-yl)carbonyl]bicyclo[1.1.1]pentane derivatives as inhibitors of receptor interacting protein kinase for the treatment of disease. And the patent contained the following:

The is invention is related to the preparation of compounds I [X = a bond, carbamoyl, carbonyl, (un)substituted alkylene; R1a, R1b = independently H, (un)substituted alkyl; or R1aNR1b= (un)substituted heterocycloalkyl or heteroaryl; R2 = H, OH, CN, halo, NH2, etc.] or salts thereof which inhibit RIPK1, pharmaceutical compositions, and methods of treatment of RIPK1-mediated diseases, such as neurodegenerative disorders, inflammatory disorders, and cancer. Thus, Wittig reaction between 3,5-difluorobenzaldehyde and 2-(triphenylphosphoranylidene)acetaldehyde, cyclization of (E)-3-(3,5-difluorophenyl)-2-propenal with NH2NH2 and reaction of 5-(3,5-difluorophenyl)-4,5-dihydro-1H-pyrazole with 3-(methoxycarbonyl)bicyclo[1.1.1]pentane-1-carboxylic acid gave II. Exemplified compounds I were tested for their RIPK1 activity (data given for representative compounds I). The experimental process involved the reaction of 5-Methoxy-1H-pyrazole(cas: 215610-30-3).Reference of 5-Methoxy-1H-pyrazole

The Article related to dihydropyrazolylcarbonylbicyclopentane derivative preparation receptor interacting protein kinase 1 inhibitor, ripk1 inhibitor dihydropyrazolylcarbonylbicyclopentane derivative preparation antiinflammatory anticancer neurodegenerative disorder and other aspects.Reference of 5-Methoxy-1H-pyrazole

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