专利号:US-12351573-B2 优先权日:2019-05-09 标 题:Compounds for use in synthesis of peptidomimetics 发明人:AL-ABED YOUSEF; CHENG KAI FAN 权利人:FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH 摘要:Synthesis of O-benzotriazole and O-imidazole synthons are described. Uses of synthons in synthesis of azapeptides and other peptidomimetics, azapeptides and other peptidomimetics synthesized from the synthons and uses of azapeptides and other peptidomimetics are also described.
专利号:US-2023159450-A1 优先权日:2020-05-08 标 题 :Dimers for use in synthesis of peptidomimetics 发明人:AL-ABED YOUSEF; ALTITI AHMAD 权利人:FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH 摘要:Dimers for use in synthesis of peptidomimetics are described. Uses of dimers as synthons in synthesis of azapeptides and other peptidomimetics, azapeptides and other peptidomimetics synthesized from the dimers and uses of azapeptides and other peptidomimetics are also described.
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-4504415-A 优先权日:1983-04-04 标题:Synthesis of thymosin α1 and desacetyl thymosin α1 发明人:FELIX ARTHUR M; GILLESSEN DIETER; STUDER ROLF; MEIENHOFER JOHANNES A; TRZECIAK ARNOLD 权利人:HOFFMANN LA ROCHE 摘要:An improved solution phase synthesis of thymosin alpha 1 and desacetyl thymosin alpha 1 with t-Boc side chain protection and proceeding through novel intermediates is disclosed.
专利号:US-4517119-A 优先权日:1983-04-04 标题:Synthesis of thymosin α1 发明人:FELIX ARTHUR M; GILLESSEN DIETER; LERGIER WILLIAM; MEIENHOFER JOHANNES A; TRZECIAK ARNOLD 权利人:HOFFMANN LA ROCHE 摘要:An improved solution phase synthesis of thymosin α 1 and proceeding through novel intermediates is disclosed.
参考文献:10.1111/j.1440-1827.1996.tb03636.x 摘要:Watanabe I, Tezuka F, Yamaguchi M, Sagawa J, Kaise N. Thymic carcinoma of the thyroid. Pathol Int. 1996 Jun;46(6):450–6. doi: 10.1111/j.1440-1827.1996.tb03636.x. 参考文献:10.1111/j.1600-0676.1996.tb00729.x 摘要:Andreone P, Cursaro C, Gramenzi A, Buzzi A, Covarelli MG, Di Giammarino L, Miniero R, Arienti V, Bernardi M, Gasbarrini G. A double-blind, placebo-controlled, pilot trial of thymosin alpha 1 for the treatment of chronic hepatitis C. Liver. 1996 Jun;16(3):207–10. doi: 10.1111/j.1600-0676.1996.tb00729.x. 参考文献:10.1097/00004836-199609000-00024 摘要:Zavaglia C, Bottelli R, Smedile A, Iamoni G, Mondazzi L, Airoldi A, Lanzani F, Idéo G. A pilot study of thymosin-alpha 1 therapy for chronic hepatitis D. J Clin Gastroenterol. 1996 Sep;23(2):162–3. doi: 10.1097/00004836-199609000-00024. 参考文献:10.1016/0162-3109(96)00131-2 摘要:Pozo D, Guerrero JM, Segura JJ, Calvo JR. Thymosin alpha 1 interacts with the VIP receptor-effector system in rat and mouse immunocompetent cells. Immunopharmacology. 1996 Sep;34(2-3):113–23. doi: 10.1016/0162-3109(96)00131-2. 参考文献:10.1016/s0192-0561(98)00060-5 摘要:Knutsen AP, Freeman JJ, Mueller KR, Roodman ST, Bouhasin JD. Thymosin- α 1 stimulates maturation of CD34+ stem cells into CD3+4+ cells in an in vitro thymic epithelia organ coculture model. International Journal of Immunopharmacology. 1999 Jan;21(1):15–26. doi: 10.1016/s0192-0561(98)00060-5.