📜4-[(2-Bromoacryloyl)Amino]-1-Methyl-1H-Pyrrole-2-Carboxylic Acid Chloride,4-Amino-N-[5-[[5-[2-(Diaminomethylideneamino)Ethylcarbamoyl]-1-Methylpyrrol-3-Yl]Carbamoyl]-1-Methylpyrrol-3-Yl]-1-Methylpyrrole-2-Carboxamide 反应生成 N-(5-{[(5-{[(5-{[(2-{[Amino(Imino)Methyl]Amino}Ethyl) Amino]Carbonyl}-1-Methyl-1H-Pyrrol-3-yl)Amino]Carbonyl}-1-Methyl-1H-Pyrrol-3-yl)Amino]Carbonyl}-1-Methyl-1H-Pyrrol-3-yl)-4-[(2-Bromoacryloyl)Amino]-1-Methyl-1H-Pyrrole-2-Carboxamide 参考文献:Cytotoxic α-Bromoacrylic Derivatives Of Distamycin Analogues Modified At The Amidino Moiety 标题:Cytotoxic α-Bromoacrylic Derivatives Of Distamycin Analogues Modified At The Amidino Moiety 摘要:The Design,Synthesis,In Vitro And In Vivo Activities Of Novel Alpha-Bromoacrylic Derivatives Of Distamycin A,Modified At The Amidino Moiety By The Replacement With Basic Or Non-Basic Groups Are Reported. In Spite Of The Relevance Of These Modifications Of Distamycin Frame,The New Derivatives Are Potent Cytotoxics. The Presence Of The Amidino Moiety,Is,Therefore,Not An Absolute Requirement For The Activity. In Particular Due To A Favorable Myclotoxicity/Cytotoxicity Ratio,Guanidino Derivative Pnu 166196 Was Selected For Clinical Development. (C) 2000 Elsevier Science Ltd. All Rights Reserved. Doi:10.1016/S0960-894X(00)00205-5
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-2017283878-A1 优先权日:2015-12-11 标题:Modulation of globoseries glycosphingolipid synthesis and cancer biomarkers 发明人:WONG CHI-HUEY; WU CHUNG-YI; CHEUNG SARAH K C; CHUANG PO-KAI; HSU TSUI-LING 权利人:ACADEMIA SINICA 摘要:The present disclosure relates to methods and compositions which can modulate the globoseries glycosphingolipid synthesis. Particularly, the present disclosure is directed to glycoenzyme inhibitor compound and compositions and methods of use thereof that can modulate the synthesis of globoseries glycosphingolipid SSEA-3/SSEA-4/GloboH in the biosynthetic pathway; particularly, the glycoenzyme inhibitors target the alpha-4GalT; beta-4GalNAcT-I; or beta-3GalT-V enzymes in the globoseries synthetic pathway. Additionally, the present disclosure is also directed to vaccines, antibodies, and/or immunogenic conjugate compositions targeting the SSEA-3/SSEA-4/GLOBO H associated epitopes (natural and modified) which elicit antibodies and/or binding fragment production useful for modulating the globoseries glycosphingolipid synthesis. Moreover, the present disclosure is also directed to the method of using the compositions described herein for the treatment or detection of hyperproliferative diseases and/or conditions. Furthermore, the instant disclosure also relates to cancer stem cell biomarkers for diagnostic and therapeutic uses.
专利号:US-10272065-B2 优先权日:2013-01-14 标题 :Gem-difluorinated C-glycoside compounds as anti-cancer agents 发明人:SLILATY STEVE N 权利人:ADVANOMICS CORP; BENOIT & COTE 摘要:The present document describes a synthesis of a class of gem-difluorinated C-glycoside compounds derived from podophyllotoxin, which may be used, but not exclusively, in oncology for the treatment of cancer. More particularly, the podophyllotoxin gem-difluorinated C-glycoconjugated derivatives display improved conformational and chemical stability, and improved cytotoxicity exhibited against drug-resistant cancer cell lines.
专利号:US-11299491-B2 优先权日:2018-11-16 标 题:Synthesis of key intermediate of KRAS G12C inhibitor compound
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合成参考文献
摘要:Geroni C, Marchini S, Cozzi P, Galliera E, Ragg E, Colombo T, Battaglia R, Howard M, D'Incalci M, Broggini M. Brostallicin, a novel anticancer agent whose activity is enhanced upon binding to glutathione. Cancer Res. 2002 Apr 15;62(8):2332–6.