CAS: 24279-91-2; [2-[2,5-Bis(Aziridin-1-yl)-4-Methyl-3,6-Dioxocyclohexa-1,4-Dien-1-Yl]-2-Methoxyethyl] Carbamate

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      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-10342858-B2
      优先权日:2015-01-24
      标题 :Glycan conjugates and methods of use thereof
      发明人:WONG CHI-HUEY; WU CHUNG-YI
      权利人:ACADEMIA SINICA
      摘要:The present disclosure is directed to vaccines, antibodies, and/or immunogenic conjugate compositions targeting the SSEA3/SSEA4/GloboH associated epitopes (natural and modified) which elicit antibodies and/or binding fragment production useful for modulating the globo-series glycosphingolipid synthesis. The present disclosure relates to methods and compositions which can modulate the globo-series 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 globo-series glycosphingolipid SSEA3/SSEA4/GloboH in the biosynthetic pathway; particularly, the glycoenzyme inhibitors target the alpha-4GalT; beta-4GalNAcT-I; or beta-3GalT-V enzymes in the globo-series synthetic pathway. 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.

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      主要参考文献


      1: Díaz-Espinosa Y, Crespo-Hernández CE, Alegría AE, García C, Arce R. Quenching enhancement of the singlet excited state of pheophorbide-a by DNA in the presence of the quinone carboquone. Photochem Photobiol. 2011 Mar-Apr;87(2):275-83. doi: 10.1111/j.1751-1097.2010.00869.x. Epub 2011 Jan 4.
      2: Tabata M, Imagawa S, Tarumoto T, Ohmine K, Hatake K, Miura Y, Ozawa K. Essential thrombocythemia transformed to acute myelogenous leukemia with t(3;17)(p24; q12), del(5)(q13q34) after treatment with carboquone and hydroxyurea. Jpn J Clin Oncol. 2000 Jul;30(7):310-2. Japanese. Japanese.

      合成参考文献


      参考文献:10.1016/0024-3205(80)90166-6
      摘要:Uehara N, Shirakawa S, Uchino H, Saeki Y, Nozaki M. Elevated polyamine levels in erythrocytes of SLC:ICR mice inoculated with Ehrlich ascites carcinoma cells. Life Sci. 1980 Feb 11;26(6):461–7. doi: 10.1016/0024-3205(80)90166-6.
      参考文献:10.1007/bf02054057
      摘要:Yamaue H, Tanimura H, Nakamori M, Noguchi K, Iwahashi M, Tani M, Hotta T, Murakami K, Ishimoto K. Clinical evaluation of chemosensitivity testing for patients with colorectal cancer using MTT assay. Dis Colon Rectum. 1996 Apr;39(4):416–22. doi: 10.1007/bf02054057.
      参考文献:10.1159/000227045
      摘要:Sakaguchi Y, Kohnoe S, Emi Y, Maehara Y, Kusumoto T, Sugimachi K. Cytotoxicity of mitomycin C and carboquone combined with hyperthermia against hypoxic tumor cells in vitro. Oncology. 1992;49(3):227–32. doi: 10.1159/000227045.
      摘要:Koike K. [Experimental combination chemotherapy with carboquone and 5-fluorouracil of human germ cell tumors transplanted into nude mice]. Nihon Gan Chiryo Gakkai Shi. 1986 Jul 20;21(6):1302–10.
      参考文献:10.1248/bpb1978.9.651
      摘要:Komiyama T, Kikuchi T, Sugiura Y. Interactions of anticancer quinone drugs, aclacinomycin A, adriamycin, carbazilquinone, and mitomycin C, with NADPH-cytochrome P-450 reductase, xanthine oxidase and oxygen. J Pharmacobiodyn. 1986 Aug;9(8):651–64. doi: 10.1248/bpb1978.9.651.
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