📜(3-氯苯基)-(4-甲氧基苯基)-甲酮置于platinum On Activated Charcoal 噻吩,盐酸,Sodium Tetrahydroborate,氨,氢气,硝酸体系中,用 甲醇,二氯甲烷,异丙醇 用作溶剂,化学反应 21.75H,反应生成利阿唑 参考文献:Synthesis Of Liazaltm,A Retinoic Acid Metabolism Blocking Agent (Ramba) With Potential Clinical Applications In Oncology And Dermatology 标题:Synthesis Of Liazaltm,A Retinoic Acid Metabolism Blocking Agent (Ramba) With Potential Clinical Applications In Oncology And Dermatology 摘要:The Synthesis Of Liazal(Tm) (Compound 9,R085246) Is Described. Llazal(Tm) Inhibits All-Trans-Retinoic Acid Metabolism And Thereby Exerts Retinoid-Like Effects In Vivo. (C) 1998 Elsevier Science Ltd. All Rights Reserved. Doi:10.1016/s0960-894X(98)00004-3
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-8734846-B2 优先权日:2008-06-16 标 题 :Methods for the preparation of targeting agent functionalized diblock copolymers for use in fabrication of therapeutic targeted nanoparticles 发明人:ALI MIR M; HRKACH JEFF; ZALE STEPHEN E; ALVAREZ DE CIENFUEGOS LUIS 权利人:BIND BIOSCIENCES INC 摘要:This application provides nanoparticles and methods of making nanoparticles using pre-functionalized poly(ethylene glycol)(also referred to as PEG) as a macroinitiator for the synthesis of diblock copolymers. Ring opening polymerization yields the desired poly(ester)-poly (ethylene glycol)-targeting agent polymer that is used to impart targeting capability to therapeutic nanoparticles. This “polymerization fromâ€? approach typically employs precursors of the targeting agent wherein the reactivity of functional groups of the targeting agent is masked using protecting groups. Also described is a “coupling toâ€? that utilized the poly(ethylene glycol)-targeting agent conjugate where the targeting agent remains in its native un-protected form. This method uses “orthogonalâ€? chemistry that exhibit no cross reactivity towards functional groups typically found within targeting agents of interest.
专利号:US-2013035307-A1 优先权日:2010-01-26 标 题:Methods for treating or preventing the spread of cancer using semi-synthetic glycosaminoglycosan ethers 发明人:PRESTWICH GLENN D; KENNEDY THOMAS P 权利人:UNIV UTAH RES FOUND; PRESTWICH GLENN D; KENNEDY THOMAS P 摘要:Described herein are methods for the treatment and prevention of tumor metastasis using alkylated and fluoroalkylated semi-synthetic glycosaminoglycan ethers (“SAGEsâ€?). The synthesis of sulfated alkylated and fluoroalkylated SAGEs is also described.
专利号:US-2008214827-A1 优先权日:2004-02-03 标 题:Synthesis of Cyanoimino-Benzoimidazoles 发明人:GOEHRING R RICHARD; WHITEHEAD JOHN; SHAO BIN 权利人:EURO CELTIQUE SA 摘要:Disclosed in certain embodiments is a process for synthesizing a compound of formula (V) and salts thereof.
专利号:US-9220714-B2 优先权日:2006-03-16 标 题 :Nitrofuran compounds for the treatment of cancer and angiogenesis 发明人:SAULNIER SHOLLER GISELLE L; SWAMY NARASIMHA; KALKUNTE STAYAN; SINGH RAKESH K; BRARD LAURENT; KIM KYU KWANG 权利人:WOMEN AND INFANTS HOSPITAL OF RHODE ISLAND; UNIV BROWN; WOMEN AND INFANTS HOSPITAL RHODE ISLAND 摘要:The invention is directed to the synthesis and use of nitrofuran compounds, especially Nifurtimox, as medicaments to treat cancer, especially neuroblastoma, and to inhibit angiogenesis. The invention also provides compositions, unit dosage forms, and kits comprising the compounds.
1: Gilden M, Malik M, Britten J, Delgado T, Levy G, Catherino WH. Leiomyoma fibrosis inhibited by liarozole, a retinoic acid metabolic blocking agent. Fertil Steril. 2012 Dec;98(6):1557-62. doi: 10.1016/j.fertnstert.2012.07.1132. Epub 2012 Aug 25. doi: 10.2340/00015555-0573. Chinese. 5: Verfaille CJ, Vanhoutte FP, Blanchet-Bardon C, van Steensel MA, Steijlen PM. Oral liarozole vs. acitretin in the treatment of ichthyosis: a phase II/III multicentre, double-blind, randomized, active-controlled study. Br J Dermatol. 2007 May;156(5):965-73. Epub 2007 Jan 30.
合成参考文献
摘要:Van heusden J, Borgers M, Ramaekers F, Xhonneux B, Wouters W, De Coster R, Smets G. Liarozole potentiates the all-trans-retinoic acid-induced structural remodelling in human breast carcinoma MCF-7 cells in vitro. Eur J Cell Biol. 1996 Sep;71(1):89–98. 参考文献:10.1006/excr.1999.4513 摘要:Sonneveld E, van den Brink CE, van der Leede BJ, Maden M, van der Saag PT. Embryonal carcinoma cell lines stably transfected with mRARbeta2-lacZ: sensitive system for measuring levels of active retinoids. Exp Cell Res. 1999 Aug 01;250(2):284–97. doi: 10.1006/excr.1999.4513. 参考文献:10.2165/00128071-200203030-00003 摘要:Cather J, Menter A. Novel Therapies for Psoriasis. American Journal of Clinical Dermatology. 2002 Apr;3(3):159–73. doi: 10.2165/00128071-200203030-00003. 参考文献:10.1186/1471-2407-8-84 摘要:Keith BD. Systematic review of the clinical effect of glucocorticoids on nonhematologic malignancy. BMC Cancer. 2008 Mar 28;8():84. 参考文献:10.1177/030089169408000406 摘要:Boccardo F, Cannata D, Guarneri D, Oneto F, Cortesi E, Bono A. R75251 in prostate cancer patients in progression after first-line hormonal treatment. Tumori. 1994 Aug 31;80(4):276–9. doi: 10.1177/030089169408000406.