5-氨基-1-甲基-1H-苯并咪唑-2-丁酸乙酯置于ammonium Dihydrogen Phosphate,氯化亚砜,Potassium Iodide体系中,用 二氯甲烷,水 作为反应溶剂,化学反应 17.0H,反应生成 盐酸苯达莫司汀 参考文献:Process For The Preparation Of Bendamustine 标题:Process For The Preparation Of Bendamustine 摘要:该发明涉及一种从2-氟-5-硝基苯胺制备烷基4-[5-[双(2-羟乙基)氨基]-1-甲基-1H-苯并咪唑-2-基]丁酸酯(7)的方法,包括以下步骤:(a)将2-氟-5-硝基苯胺转化为5-(2-氟-5-硝基苯胺基)-5-氧代戊酸(1),使用戊二酸酐,将化合物(1)转化为甲胺基5-[2-(甲基氨基)-5-硝基苯胺基]-5-氧代戊酸酯(2),使用甲胺;将化合物(2)转化为5-[2-(甲基氨基)-5-硝基苯胺基]-5-氧代戊酸(3),并将化合物(3)缩合为4-(1-甲基-5-硝基-1H-苯并咪唑-2-基)丁酸(4);(b)酯化步骤a)的产物(4)为烷基4-(1-甲基-5-硝基1H-苯并咪唑-2-基)丁酸酯(5);(c)还原步骤b)的产物为烷基4-(5-氨基-1-甲基-1H-苯并咪唑-2-基)丁酸酯(6),以及(d)将步骤c)的产物转化为烷基4-[5-[双(2-羟乙基)氨基]-1-甲基-1H-苯并咪唑-2-基]丁酸酯(7).
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-2022118094-A1 优先权日:2019-02-21 标题:Synthesis of biomimetic cell wall structure 发明人:WANG YONG; SHI PENG 权利人:PENN STATE RES FOUND 摘要:The present invention relates generally to methods of generating a biomimetic cell wall (BCW) on a target surface, compositions comprising the BCW, and methods of use of the compositions, including biomedical applications of the BCW coated compositions.
专利号:US-11130764-B2 优先权日:2017-02-17 标题 :Analogs of vincamine and uses thereof 发明人:HUIGENS III ROBERT WILLIAM; NORWOOD IV VERRILL M; LUESCH HENDRIK 权利人:UNIV FLORIDA 摘要:The present disclosure provides compounds of any one of Formulae (I′), (I), (IA), (II′), (II), (IIA), (IIIA), (III″), (III′), (III), (IIIA), (IV), (V′), (V), (VI), (VII), (VIII′), (VIII), (IX′), (IX), and (X). The compounds described herein may be useful in treating and/or preventing a broad range of diseases (e.g., proliferative disease (e.g., cancers (e.g., non-small cell lung cancer, or glioma), inflammatory diseases, autoimmune diseases), CNS disorder (e.g., drug addiction), metabolic disorder (e.g., diabetes), or infectious disease (e.g., bacterial infection or parasitic infection (e.g., malaria))). Also provided in the present disclosure are pharmaceutical compositions, methods of synthesis of a compound described herein, kits, methods, and uses including or using a compound described herein.
专利号:US-9643932-B2 优先权日:2011-09-26 标 题:Process for the preparation of bendamustine hydrochloride 发明人:MISHRA BHUWAN BHASKAR; KACHHADIA NIKUNJ SHAMBHUBHAI; TOMAR VINOD SINGH; LAHIRI SASWATA 权利人:FRESENIUS KABI ONCOLOGY LTD 摘要:The present invention relates to an improved process for the synthesis of bendamustine, in particular, bendamustine hydrochloride of the formula (VI) and its intermediate 1-methyl-5-[bis(2-chloroethyl)amino]-1H-benzimidazol-2-yl]lithium butanoate of formula (V), both having a purity of ≧99%, which is simple, convenient, economical, does not use hazardous chemicals and is industrially viable.
专利号:US-2018140724-A1 优先权日:2015-05-27 标 题:Tumor Deliverable Iron and Protein Synthesis Inhibitors as a New Class of Drugs for the Diagnosis and Treatment of Cancer 发明人:DENG CHANGCHUN; LIPSTEIN MARK; O'CONNOR OWEN A 权利人:DENG CHANGCHUN; LIPSTEIN MARK; OCONNOR OWEN A; UNIV COLUMBIA 摘要:Tumor deliverable iron (TDI) drugs and pharmaceutical compositions and kits comprising them are provided and methods for delivering iron to tumors specifically, either intracellularly or extracellularly. As a result, TDI drugs are useful as a sensitizer for radiation therapy, radio-diagnosis, and chemotherapy, and are of interest. In other embodiments, tumor deliverable protein synthesis inhibitors (TDPSI) are provided and can be delivered to tumors, but not normal cells. These TDPSI drugs and pharmaceutical compositions and kits comprising them are useful for their treatment of cancer, either alone or in combination with other active anti-cancer drugs.
专利号:US-2018371021-A1 优先权日:2017-05-11 标 题 :Peptidomimetic macrocycles and uses thereof 发明人:AIVADO MANUEL; GUERLAVAIS VINCENT; OLSON KAREN 权利人:AILERON THERAPEUTICS INC 摘要:The present disclosure describes the synthesis of peptidomimetic macrocycles and methods of using peptidomimetic macrocycles to treat a condition. The present disclosure also describes methods of using peptidomimetic macrocycles in combination with at least one additional pharmaceutically-active agent for the treatment of a condition, for example, cancer.
1: Alrifai T, Grant Szymanski K, Venugopal P, Mahon B, Okwuosa T, Karmali R. Bendamustine and Rituximab: Complete Response in a 62-Year-Old Female with an Aggressive Lymphoma and an Ejection Fraction of 20. Chemotherapy. 2017;62(2):140-146. doi: 10.1159/000452756. Epub 2016 Dec 14. Review. doi: 10.3109/10428194.2015.1110748. Epub 2015 Dec 23. Review. doi: 10.3109/10428194.2015.1099647. Epub 2015 Nov 23. Review. 4: Gentile M, Vigna E, Recchia AG, Morabito L, Mendicino F, Giagnuolo G, Morabito F. Bendamustine in multiple myeloma. Eur J Haematol. 2015 Nov;95(5):377-88. doi: 10.1111/ejh.12609. Epub 2015 Jul 14. Review. doi: 10.1007/s00280-015-2727-6. Epub 2015 Apr 1. Review. 6: Kuno M, Inoue A, Aimoto M, Nakao T, Kameda K, Yoshida M, Kanashima H, Hirai M, Yamane T. [Alleviated anemia by bendamustine in cold agglutinin disease associated with small lymphocytic lymphoma]. Rinsho Ketsueki. 2015 Feb;56(2):204-9. doi: 10.11406/rinketsu.56.204. Review. Japanese. doi: 10.3109/10428194.2014.915545. Epub 2014 Jun 27. Review. doi: 10.1016/j.hemonc.2014.04.001. Epub 2014 Apr 29. Review. doi: 10.1007/s12032-014-0944-1. Epub 2014 Apr 22. Review.
合成参考文献
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