专利号:US-12391691-B2 优先权日:2018-11-16 标题:Synthesis of key intermediate of KRAS G12C inhibitor compound 发明人:PARSONS ANDREW THOMAS; COCHRAN BRIAN MCNEIL; POWAZINIK IV WILLIAM; CAPORINI MARC ANTHONY 权利人:AMGEN INC 摘要:The present invention relates to an improved, efficient, scalable process to prepare intermediate compounds, such as compound 5M, having the structure n nuseful for the synthesis of compounds that target KRAS G12C mutations, such as
专利号:US-2025206736-A1 优先权日:2019-11-14 标题 :Synthesis of kras g12c inhibitor compound 发明人:CORBETT MICHAEL THOMAS; CAILLE SEBASTIEN 权利人:AMGEN INC 摘要:The present disclosure relates to an improved, efficient, scalable process to prepare intermediate compounds, such as 2-isopropyl-4-methylpyridin-3-amine, useful for the synthesis of compounds, such as Compound 9, for the treatment of KRAS G12C mutated cancers.
专利号:US-9315483-B2 优先权日:2007-09-13 标题 :Synthesis of deuterated catechols and benzo[D][1,3]dioxoles and derivatives thereof 发明人:JONES ANDREW D; ZELLE ROBERT E; SILVERMAN I ROBERT 权利人:CONCERT PHARMACEUTICALS INC 摘要:The present invention provides a convenient and efficient process for the synthesis of d 2 -benzo[d][1,3]dioxoles.
专利号:US-8802660-B2 优先权日:2007-03-12 标 题:De novo synthesis of glucocorticoids in the epidermis and its uses and applications 发明人:TOMIC-CANIC MARJANA; BREM HAROLD; SAMUELS HERBERT H 权利人:TOMIC-CANIC MARJANA; BREM HAROLD; SAMUELS HERBERT H; UNIV NEW YORK 摘要:The present invention relates to methods and compositions that control, i.e., antagonize/inhibit or agonize/stimulate, de novo glucocorticoid production in the skin. Such methods and compositions can be used for the prevention and/or treatment of a variety of skin conditions, including inflammation, acute wounds, chronic non-healing wounds, keloid, fibrotic or hypertrophic scars, and epithelial-derived cancer.
专利号:US-2024287041-A1 优先权日:2021-05-20 标题 :Methods of synthesis of heteroaryl derivatives of triazolyl acrylamides and crystalline forms 发明人:BALOGLU ERKAN; AUSTAD BRIAN C; ROE DAVID G; KEDUC ANDREW; GOTTSCHLING STEPHEN EDMUND; HECKER EVAN 权利人:KARYOPHARM THERAPEUTICS INC 摘要:The present invention relates to a method of preparing a compound represented by structural formula (VII), comprising reacting a compound represented by structural formula (II), with a compound represented by structural formula (III), in a solvent, in the presence of a Pd catalyst and one or more inorganic bases under conditions suitable to prepare a compound represented by structural formula (VII): The values and example values of the variables in structural formulas (VII), (II), and (III) are defined herein. The present invention also relates to crystalline Forms I and II of the compound represented by Structural Formula (VII), the use of the crystalline Forms in treating disease or disorders associated with CRM1 and method of preparing the crystalline Forms.
专利号:EP-1422235-B1 优先权日:2001-07-26 标题 :Stereoselective method of producing 6alpha-fluoropregnanes and intermediaries 发明人:MURILLO GARRIDO JOSE VICENTE; SILVA GUISASOLA LUIS OCTAVIO; MARTIN JUAREZ JORGE 权利人:RAGACTIVES SL 摘要:6 alpha -fluorpregnanes (I), where the dotted line between positions 1 and 2 represents a single or double bond; R1 is OH, OCOR2, X, SO3R3, or an (R7)(R8)(R9)SiO- group, where X is halogen, R2 and R3 are C1-6 alkyl or phenyl optionally substituted by C1-4 alkyl, and R7, R8 and R9, equal or different, are C1-6 alkyl or phenyl optionally substituted by C1-4 alkyl, can be obtained by means of a high stereoselectivity process comprising reacting a 3-(trisubstituted)silyloxy-pregna-3,5-diene (IV) with a fluorinating agent selected among N-fluorosulfonimides and N-fluorosulfonamides. The 6 alpha -fluorpregnanes (I) are intermediates for the synthesis of steroids useful as anti-inflammatory and anti-asthmatic agents.
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