专利号:EP-4186890-A1 优先权日:2021-11-29 标题 :Preparation of n-benzyl-2-(5-bromo-pyridin-2-yl)-acetamide for the synthesis of tirbanibulin 发明人:ARE CELESTE; BALLETTE ROBERTO; DOBARRO RODRÃ?GUEZ ALICIA 权利人:MOEHS IBERICA SL 摘要:The present invention relates to a process for the preparation of N-benzyl-2-(5-bromo-pyridin-2-yl)-acetamide, which is a suitable intermediate for the synthesis of tirbanibulin or a pharmaceutically acceptable salt thereof, as well as to a process for the preparation of tirbanibulin or a pharmaceutically acceptable salt thereof using said N-benzyl-2-(5-bromo-pyridin-2-yl)-acetamide intermediate.
专利号:US-2024343691-A1 优先权日:2006-12-28 标题:Compositions for modulating a kinase cascade and methods of use thereof 发明人:HANGAUER JR DAVID G; PATRA DEBASIS; CODY JEREMY A; PALMER GRANT J; ISBESTER PAUL K; SALSBURY JONATHON 权利人:ATNX SPV LLC 摘要:The invention relates to compositions comprising 2-(5-(4-(2-morpholinoethoxy)phenyl) pyridin-2-yl)-N-benzylacetamide and its mesylate and dihydrochloride salts. The invention provides an efficient process for the synthesis of 2-(5-(4-(2-morpholinoethoxy)phenyl)pyridin-2-yl)-N-benzylacetamide and its mesylate and dihydrochloride salts and methods for modulating one or more components of a kinase cascade using the compositions of the invention. The present invention also provides a novel polymorph of the mesylate salt of 2-(5-(4-(2-morpholinoethoxy)phenyl)pyridin-2-yl)-N-benzylacetamide (Form A), characterized by a unique X-ray diffraction pattern and Differential Scanning Calorimetry profile, as well as a unique crystalline structure.
专利号:US-8293739-B2 优先权日:2006-12-28 标题:Process for the preparation of compositions for modulating a kinase cascade and methods of use thereof 发明人:HANGAUER JR DAVID G; COUGHLIN DANIEL; GALE JONATHAN; CODY JEREMY A; PATRA DEBASIS; PALMER GRANT J; ISBESTER PAUL K; SALSBURY JONATHON 权利人:HANGAUER JR DAVID G; COUGHLIN DANIEL; GALE JONATHAN; CODY JEREMY A; PATRA DEBASIS; PALMER GRANT J; ISBESTER PAUL K; SALSBURY JONATHON; KINEX PHARMACEUTICALS LLC 摘要:The invention relates to compositions comprising 2-(5-(4-(2-morpholinoethoxy)phenyl)pyridin-2-yl)-N-benzylacetamide and its mesylate and dihydrochloride salts. More specifically, the invention provides an efficient process for the synthesis of 2-(5-(4-(2-morpholinoethoxy) phenyl)pyridin-2-yl)-N-benzylacetamide and its mesylate and dihydrochloride salts and methods for modulating one or more components of a kinase cascade using the compositions of the invention.
专利号:US-12441733-B2 优先权日:2018-03-26 标题:Substituted 2,4-dioxotetrahydropyrimidines as intermediates in the synthesis of bruton's tyrosine kinase inhibitors 发明人:ARISTA LUCA; HEBACH CHRISTINA; HOLLINGWORTH GREGORY JOHN; HOLZER PHILIPP; IMBACH-WEESE PATRICIA; LORBER JULIEN; MACHAUER RAINER; SCHMIEDEBERG NIKO; VULPETTI ANNA; ZOLLER THOMAS 权利人:NOVARTIS AG 摘要:The invention relates to compounds of the formulae (I), (III), (IIIa), (XXIa), (XXIII), and/or (XLVI)or a pharmaceutically acceptable salt thereof, wherein the substituents are as defined in the specification; to intermediates in the preparation of the compounds, to pharmaceutical compositions comprising the compounds and to use of the compounds in the treatment of disease.
专利号:US-9556120-B2 优先权日:2006-12-28 标题:Compositions for modulating a kinase cascade and methods of use thereof 发明人:HANGAUER JR DAVID G; PATRA DEBASIS; CODY JEREMY A; PALMER GRANT J; ISBESTER PAUL K; SALSBURY JONATHON 权利人:ATHENEX INC 摘要:The invention relates to compositions comprising 2-(5-(4-(2-morpholinoethoxyl)phenyl)pyridin-2-yl)-N-benzylacetamide and its mesylate and dihydrochloride salts. The invention provides an efficient process for the synthesis of 2-(5-(4-(2-morpholinoethoxyl)phenyl)pyridin-2-yl)-N-benzylacetamide and its mesylate and dihydrochloride salts and methods for modulating one or more components of a kinase cascade using the compositions of the invention. The present invention also provides a novel polymorph of the mesylate salt of 2-(5-(4-(2-morpholinoethoxyl)phenyl)pyridin-2-yl)-N-benzylacetamide (Form A), characterized by a unique X-ray diffraction pattern and Differential Scanning Calorimetry profile, as well as a unique crystalline structure.
专利号:WO-2023061999-A1 优先权日:2021-10-12 标 题 :Process for preparing a phenolic hydrocarbon 发明人:CORNELLA JOSEP; LE VAILLANT FRANCK 权利人:STUDIENGESELLSCHAFT KOHLE GGMBH 摘要:The present invention discloses a distinct mode of action of a nickel catalyst to forge C-0 bonds to unlock the mild utilization of N2O as O-atom transfer reagent in the synthesis of complex phenols from the corresponding aryl halides.