{"id":10577,"date":"2022-10-26T02:53:05","date_gmt":"2022-10-25T18:53:05","guid":{"rendered":"https:\/\/www.pyrazoles-derivatives.com\/?p=10577"},"modified":"2022-10-26T02:53:05","modified_gmt":"2022-10-25T18:53:05","slug":"blake-james-f-et-al-published-their-patent-in-2019-cas-1028092-65-0","status":"publish","type":"post","link":"https:\/\/www.pyrazoles-derivatives.com\/?p=10577","title":{"rendered":"Blake, James F. et al. published their patent in 2019 |CAS: 1028092-65-0"},"content":{"rendered":"

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<\/a> 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:<\/p>\n

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<\/a><\/p>\n

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<\/a><\/p>\n

Referemce:
Pyrazole – Wikipedia<\/a>,
Pyrazoles – an overview | ScienceDirect Topics<\/a><\/p>\n","protected":false},"excerpt":{"rendered":"

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<\/a><\/p>\n","protected":false},"author":8,"featured_media":0,"comment_status":"closed","ping_status":"open","sticky":false,"template":"","format":"standard","meta":{"footnotes":""},"categories":[770,131],"tags":[771],"class_list":["post-10577","post","type-post","status-publish","format-standard","hentry","category-1028092-65-0","category-pyrazoles-derivatives","tag-300-400"],"yoast_head":"\nBlake, James F. et al. published their patent in 2019 |CAS: 1028092-65-0 | pyrazoles-derivatives<\/title>\n<meta name=\"description\" content=\"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. 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