{"id":10564,"date":"2022-10-26T02:53:05","date_gmt":"2022-10-25T18:53:05","guid":{"rendered":"https:\/\/www.pyrazoles-derivatives.com\/?p=10564"},"modified":"2022-10-26T02:53:05","modified_gmt":"2022-10-25T18:53:05","slug":"morrison-angus-et-al-published-their-patent-in-2015-cas-215610-30-3","status":"publish","type":"post","link":"https:\/\/www.pyrazoles-derivatives.com\/?p=10564","title":{"rendered":"Morrison, Angus et al. published their patent in 2015 |CAS: 215610-30-3"},"content":{"rendered":"

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<\/a> The title of the patent was Preparation of triazole derivatives as inhibitors of Raf kinases. And the patent contained the following:<\/p>\n

Triazolyl compounds of formula [I; A = a 5-membered heterocyclic moiety; B = C6-14 aryl or C5-14 heteroaryl; L = \u00b7SO 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\u00b714 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\u00b0 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<\/a><\/p>\n

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

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

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<\/a><\/p>\n","protected":false},"author":8,"featured_media":0,"comment_status":"closed","ping_status":"open","sticky":false,"template":"","format":"standard","meta":{"footnotes":""},"categories":[279,131],"tags":[743],"class_list":["post-10564","post","type-post","status-publish","format-standard","hentry","category-215610-30-3","category-pyrazoles-derivatives","tag-0-100"],"yoast_head":"\nMorrison, Angus et al. published their patent in 2015 |CAS: 215610-30-3 | pyrazoles-derivatives<\/title>\n<meta name=\"description\" content=\"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:\" \/>\n<meta name=\"robots\" content=\"index, follow, max-snippet:-1, max-image-preview:large, max-video-preview:-1\" \/>\n<link rel=\"canonical\" href=\"https:\/\/www.pyrazoles-derivatives.com\/?p=10564\" \/>\n<meta property=\"og:locale\" content=\"en_US\" \/>\n<meta property=\"og:type\" content=\"article\" \/>\n<meta property=\"og:title\" content=\"Morrison, Angus et al. published their patent in 2015 |CAS: 215610-30-3 | pyrazoles-derivatives\" \/>\n<meta property=\"og:description\" content=\"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:\" \/>\n<meta property=\"og:url\" content=\"https:\/\/www.pyrazoles-derivatives.com\/?p=10564\" \/>\n<meta property=\"og:site_name\" content=\"pyrazoles-derivatives\" \/>\n<meta property=\"article:published_time\" content=\"2022-10-25T18:53:05+00:00\" \/>\n<meta name=\"author\" content=\"Jessica.F\" \/>\n<meta name=\"twitter:card\" content=\"summary_large_image\" \/>\n<meta name=\"twitter:label1\" content=\"Written by\" \/>\n\t<meta name=\"twitter:data1\" content=\"Jessica.F\" \/>\n\t<meta name=\"twitter:label2\" content=\"Est. reading time\" \/>\n\t<meta name=\"twitter:data2\" content=\"2 minutes\" \/>\n<script type=\"application\/ld+json\" class=\"yoast-schema-graph\">{\"@context\":\"https:\/\/schema.org\",\"@graph\":[{\"@type\":\"WebPage\",\"@id\":\"https:\/\/www.pyrazoles-derivatives.com\/?p=10564\",\"url\":\"https:\/\/www.pyrazoles-derivatives.com\/?p=10564\",\"name\":\"Morrison, Angus et al. published their patent in 2015 |CAS: 215610-30-3 | pyrazoles-derivatives\",\"isPartOf\":{\"@id\":\"https:\/\/www.pyrazoles-derivatives.com\/#website\"},\"datePublished\":\"2022-10-25T18:53:05+00:00\",\"author\":{\"@id\":\"https:\/\/www.pyrazoles-derivatives.com\/#\/schema\/person\/d9a9f27bed675392c6f363a01ffd49f1\"},\"description\":\"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:\",\"breadcrumb\":{\"@id\":\"https:\/\/www.pyrazoles-derivatives.com\/?p=10564#breadcrumb\"},\"inLanguage\":\"en-US\",\"potentialAction\":[{\"@type\":\"ReadAction\",\"target\":[\"https:\/\/www.pyrazoles-derivatives.com\/?p=10564\"]}]},{\"@type\":\"BreadcrumbList\",\"@id\":\"https:\/\/www.pyrazoles-derivatives.com\/?p=10564#breadcrumb\",\"itemListElement\":[{\"@type\":\"ListItem\",\"position\":1,\"name\":\"\u9996\u9875\",\"item\":\"https:\/\/www.pyrazoles-derivatives.com\/\"},{\"@type\":\"ListItem\",\"position\":2,\"name\":\"Morrison, Angus et al. published their patent in 2015 |CAS: 215610-30-3\"}]},{\"@type\":\"WebSite\",\"@id\":\"https:\/\/www.pyrazoles-derivatives.com\/#website\",\"url\":\"https:\/\/www.pyrazoles-derivatives.com\/\",\"name\":\"pyrazoles-derivatives\",\"description\":\"Several pyrazole derivatives possess important pharmacological activities and they have been proved useful materials in drug research. Pyrazole derivatives play an important role in antitumor agents.\",\"potentialAction\":[{\"@type\":\"SearchAction\",\"target\":{\"@type\":\"EntryPoint\",\"urlTemplate\":\"https:\/\/www.pyrazoles-derivatives.com\/?s={search_term_string}\"},\"query-input\":{\"@type\":\"PropertyValueSpecification\",\"valueRequired\":true,\"valueName\":\"search_term_string\"}}],\"inLanguage\":\"en-US\"},{\"@type\":\"Person\",\"@id\":\"https:\/\/www.pyrazoles-derivatives.com\/#\/schema\/person\/d9a9f27bed675392c6f363a01ffd49f1\",\"name\":\"Jessica.F\",\"image\":{\"@type\":\"ImageObject\",\"inLanguage\":\"en-US\",\"@id\":\"https:\/\/www.pyrazoles-derivatives.com\/#\/schema\/person\/image\/\",\"url\":\"https:\/\/en.cravatar.com\/avatar\/2d1cec2a99eeaad5a5b217c9cdbfb610?s=96&d=mm&r=g\",\"contentUrl\":\"https:\/\/en.cravatar.com\/avatar\/2d1cec2a99eeaad5a5b217c9cdbfb610?s=96&d=mm&r=g\",\"caption\":\"Jessica.F\"}}]}<\/script>\n<!-- \/ Yoast SEO plugin. -->","yoast_head_json":{"title":"Morrison, Angus et al. published their patent in 2015 |CAS: 215610-30-3 | pyrazoles-derivatives","description":"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:","robots":{"index":"index","follow":"follow","max-snippet":"max-snippet:-1","max-image-preview":"max-image-preview:large","max-video-preview":"max-video-preview:-1"},"canonical":"https:\/\/www.pyrazoles-derivatives.com\/?p=10564","og_locale":"en_US","og_type":"article","og_title":"Morrison, Angus et al. published their patent in 2015 |CAS: 215610-30-3 | pyrazoles-derivatives","og_description":"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:","og_url":"https:\/\/www.pyrazoles-derivatives.com\/?p=10564","og_site_name":"pyrazoles-derivatives","article_published_time":"2022-10-25T18:53:05+00:00","author":"Jessica.F","twitter_card":"summary_large_image","twitter_misc":{"Written by":"Jessica.F","Est. reading time":"2 minutes"},"schema":{"@context":"https:\/\/schema.org","@graph":[{"@type":"WebPage","@id":"https:\/\/www.pyrazoles-derivatives.com\/?p=10564","url":"https:\/\/www.pyrazoles-derivatives.com\/?p=10564","name":"Morrison, Angus et al. published their patent in 2015 |CAS: 215610-30-3 | pyrazoles-derivatives","isPartOf":{"@id":"https:\/\/www.pyrazoles-derivatives.com\/#website"},"datePublished":"2022-10-25T18:53:05+00:00","author":{"@id":"https:\/\/www.pyrazoles-derivatives.com\/#\/schema\/person\/d9a9f27bed675392c6f363a01ffd49f1"},"description":"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:","breadcrumb":{"@id":"https:\/\/www.pyrazoles-derivatives.com\/?p=10564#breadcrumb"},"inLanguage":"en-US","potentialAction":[{"@type":"ReadAction","target":["https:\/\/www.pyrazoles-derivatives.com\/?p=10564"]}]},{"@type":"BreadcrumbList","@id":"https:\/\/www.pyrazoles-derivatives.com\/?p=10564#breadcrumb","itemListElement":[{"@type":"ListItem","position":1,"name":"\u9996\u9875","item":"https:\/\/www.pyrazoles-derivatives.com\/"},{"@type":"ListItem","position":2,"name":"Morrison, Angus et al. published their patent in 2015 |CAS: 215610-30-3"}]},{"@type":"WebSite","@id":"https:\/\/www.pyrazoles-derivatives.com\/#website","url":"https:\/\/www.pyrazoles-derivatives.com\/","name":"pyrazoles-derivatives","description":"Several pyrazole derivatives possess important pharmacological activities and they have been proved useful materials in drug research. Pyrazole derivatives play an important role in antitumor agents.","potentialAction":[{"@type":"SearchAction","target":{"@type":"EntryPoint","urlTemplate":"https:\/\/www.pyrazoles-derivatives.com\/?s={search_term_string}"},"query-input":{"@type":"PropertyValueSpecification","valueRequired":true,"valueName":"search_term_string"}}],"inLanguage":"en-US"},{"@type":"Person","@id":"https:\/\/www.pyrazoles-derivatives.com\/#\/schema\/person\/d9a9f27bed675392c6f363a01ffd49f1","name":"Jessica.F","image":{"@type":"ImageObject","inLanguage":"en-US","@id":"https:\/\/www.pyrazoles-derivatives.com\/#\/schema\/person\/image\/","url":"https:\/\/en.cravatar.com\/avatar\/2d1cec2a99eeaad5a5b217c9cdbfb610?s=96&d=mm&r=g","contentUrl":"https:\/\/en.cravatar.com\/avatar\/2d1cec2a99eeaad5a5b217c9cdbfb610?s=96&d=mm&r=g","caption":"Jessica.F"}}]}},"_links":{"self":[{"href":"https:\/\/www.pyrazoles-derivatives.com\/index.php?rest_route=\/wp\/v2\/posts\/10564","targetHints":{"allow":["GET"]}}],"collection":[{"href":"https:\/\/www.pyrazoles-derivatives.com\/index.php?rest_route=\/wp\/v2\/posts"}],"about":[{"href":"https:\/\/www.pyrazoles-derivatives.com\/index.php?rest_route=\/wp\/v2\/types\/post"}],"author":[{"embeddable":true,"href":"https:\/\/www.pyrazoles-derivatives.com\/index.php?rest_route=\/wp\/v2\/users\/8"}],"replies":[{"embeddable":true,"href":"https:\/\/www.pyrazoles-derivatives.com\/index.php?rest_route=%2Fwp%2Fv2%2Fcomments&post=10564"}],"version-history":[{"count":0,"href":"https:\/\/www.pyrazoles-derivatives.com\/index.php?rest_route=\/wp\/v2\/posts\/10564\/revisions"}],"wp:attachment":[{"href":"https:\/\/www.pyrazoles-derivatives.com\/index.php?rest_route=%2Fwp%2Fv2%2Fmedia&parent=10564"}],"wp:term":[{"taxonomy":"category","embeddable":true,"href":"https:\/\/www.pyrazoles-derivatives.com\/index.php?rest_route=%2Fwp%2Fv2%2Fcategories&post=10564"},{"taxonomy":"post_tag","embeddable":true,"href":"https:\/\/www.pyrazoles-derivatives.com\/index.php?rest_route=%2Fwp%2Fv2%2Ftags&post=10564"}],"curies":[{"name":"wp","href":"https:\/\/api.w.org\/{rel}","templated":true}]}}