CAS: 58994-96-0; Ranimustine

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CAS号58994-95-9 1-(2-chloroethy... | CAS号5155-43-1 甲基6-脱氧-aD-吡喃葡萄糖苷

甲基 6-脱氧吡喃己糖苷置于盐酸,Sodium Hydroxide,Sodium Nitrite体系中,用 乙醚,乙醇,氯仿,水 作为反应溶剂,化学反应 5.0H,反应生成 1-(2-氯乙基)-1-亚硝基-3-[[(2R,3S,4S,5R,6S)-3,4,5-三羟基-6-甲氧基-氧杂己环-2-基]甲基]脲
参考文献:在寻找新的抗癌药.xxiii:探索含有n-亚硝基氯乙基氨基,N-亚硝基甲基和n-亚硝基氨基甲苯基成分的碳水化合物的抗癌药物的预测设计.
标题:在寻找新的抗癌药.xxiii:探索含有n-亚硝基氯乙基氨基,N-亚硝基甲基和n-亚硝基氨基甲苯基成分的碳水化合物的抗癌药物的预测设计.
摘要:自旋标记的葡萄糖亚硝基脲13-16,链脲佐菌素(18),氯唑菌素(31),半乳糖基24和甘露糖基28的链脲佐菌素类似物及其四-O-乙酰基衍生物25和29,Mcnu(cymerin,34)和葡萄糖胺(21)已合成并在体内评估了其对鼠淋巴细胞性白血病p388的抗癌活性.化合物13-16,18,24,28,31和34的活性增长寿命(%ils)在33%至603%之间,而21,25和29种化合物则无活性(%ils = 9至10).在30天后,所有用活性最高的化合物(13,14和34)以20 Mg / Kg治疗的cd2F1雄性小鼠均存活,而所有经临床链脲佐菌素(18)和经临床测试的氯佐霉素(31)治疗的小鼠均被淘汰.化合物13-16,18,31,进一步评估了34和34的抗淋巴白血病l1210的抗肿瘤活性.与ccnu(1)和自旋标记slcnu(3)相比,化合物13和34在第60天的%ils值分别为557
DOI:10.1002/jps.2600800717

专利信息

专利号:US-10925977-B2
优先权日:2006-10-05
标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications
发明人：YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S
权利人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S; CEIL POINT LLC; UNIV TEXAS
摘要:Novel methods of synthesis of chelator-targeting ligand conjugates, compositions comprising such conjugates, and therapeutic and diagnostic applications of such conjugates are disclosed. The compositions include chelator-targeting ligand conjugates optionally chelated to one or more metal ions. Methods of synthesizing these compositions in high purity are also presented. Also disclosed are methods of imaging, treating and diagnosing disease in a subject using these novel compositions, such as methods of imaging a tumor within a subject and methods of diagnosing myocardial ischemia.

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-2017100796-A1
优先权日:2015-12-11
标 题 :Modulation of globoseries glycosphingolipid synthesis and cancer biomarkers
发明人：WONG CHI-HUEY; HSU TSUI-LING; WU CHUNG-YI; CHEUNG SARAH K C; CHUANG PO-KAI
权利人:SINACA ACAD; WONG CHI-HUEY; HSU TSUI-LING
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 disgnostic and therapeutic uses.

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-8828984-B2
优先权日:2012-11-19
标题:Gold(III) complexes containing N-heterocyclic carbene ligand, synthesis, and their applications in cancer treatment and thiol detection
发明人：CHE CHI MING; ZOU TAOTAO
权利人:UNIV HONG KONG; UNIV HONG KONG
摘要:Provided herein is a method of synthesis of Au(III)-NHC complexes, a pharmaceutical composition comprises thereof. Also provided herein are the methods for the treatment and prevention of cancer/tumor in patients in need thereof by the administration of the Au(III)-NHC complexes. Also provided is method of detecting thiol in a biological system. The Au(III)-NHC complexes possess anticancer activity such as the induction of cell death, inhibition of cellular proliferation, inhibition of thioredoxin reductase activity, and inhibition of tumor growth in vivo.