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:WO-2022226312-A1 优先权日:2021-04-22 标 题:Combination nucleotide pool depletion for treatment of viral infections and cancers 发明人:KUMAR VIKRAM; HESSON DAVID; DEMAREST JAMES 权利人:CLEAR CREEK BIO INC 摘要:The invention provides methods of treating cancers and viral infections by providing a combination of agents that inhibit both nucleotide synthesis and nucleotide salvage in the cells of a subject to prevent cancer proliferation and viral replication. The invention provides methods of depleting nucleotide pools by using both inhibitors of dihydroorotate dehydrogenase (DHODH), such as brequinar, which block synthesis of pyrimidine-based nucleotides, in combination of one or more nucleotide salvage inhibitors, for example deoxycytidine kinase (dCK) inhibitors, Equilibrative nucleoside transporter (ENT) inhibitors, and Uridine-cytidine kinase (UCK) inhibitors, which inhibit salvage of purine and/or pyrimidine-based nucleotides or nucleosides
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:US-11850220-B2 优先权日:2020-05-19 标题 :Synthesis of ibuprofen hybrid conjugates as anti-inflammatory and analgesic agents 发明人:PANDA SIVA 权利人:UNIV RES INST INC AUGUSTA 摘要:Disclosed herein as ibuprofen hybrid conjugates and methods of their use to reduce inflammation, pain, and fever. The ibuprofen conjugates have potent anti-inflammatory and analgesic properties with low potential for ulcerogenic activity. An exemplary compound is an ibuprofen-amino acid-4-aminophenol hybrid. Also disclosed are methods of treating or reducing inflammation, pain, and fever in a subject.
专利号:US-6150403-A 优先权日:1997-10-14 标 题 :Topical compositions for regulating the oily/shiny appearance of skin 发明人:BIEDERMANN KIMBERLY A; SCHUBERT HARRY L; PARRAN JR JOHN J 权利人:PROCTER & GAMBLE 摘要:The present invention relates to methods for inhibiting sebaceous gland activity in mammalian skin comprising administration of a topical composition comprising dehydroacetic acid or pharmaceutically acceptable salts thereof, and a dermatologically-acceptable carrier. The present invention also relates to methods and topical compositions further comprising agents which regulate the oily and/or shiny appearance of skin, and agents which treat acne and related skin disorders in mammalian skin and scalp. Methods of reducing sebum synthesis with the use of dehydroacetic acid, methods of regulating the oily and/or shiny appearance of skin, and methods of treating acne and other skin disorders are also encompassed by the present invention.