CAS: 137281-23-3; (S)-2-(4-(2-(2-Amino-4-Oxo-4,7-Dihydro-1H-Pyrrolo[2,3-D]Pyrimidin-5-yl)Ethyl)Benzamido)Pentanedioic Acid

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CAS号165049-28-5 N-(4-[2-(2-氨基-4...

N-[4-[2-(2-氨基-4,7-二氢-4-氧代-1H-吡咯并[2,3-D]嘧啶-5-基)乙基]苯甲酰]-L-谷氨酸二乙酯对甲苯磺酸盐置于sodium Hydroxide体系中,用 水 用作溶剂,化学反应生成培美曲塞
参考文献:抗癌药物培美曲塞二钠杂质的合成及理化表征
标题:抗癌药物培美曲塞二钠杂质的合成及理化表征
摘要:对与培美曲塞二钠合成相关的工艺相关杂质进行了物理化学表征.文献中已经提到形成培美曲塞杂质的可能性,但尚未发表对其结构的研究.本文描述了这些化合物的合成方法的发展,并讨论了基于二维 NMR 实验和 Ms 数据的结构解析.这些杂质的鉴定应有助于培美曲塞二钠盐生产过程中的质量控制.
Doi:10.3390/molecules200610004

专利信息

专利号:US-12383499-B2
优先权日:2018-01-01
标题:Scale up synthesis of silicasome nanocarriers
发明人：NEL ANDRE E; MENG HUAN; LIU XIANGSHENG
权利人:UNIV CALIFORNIA
摘要:In order to facilitate the approval and commercialization of silicasome drug delivery systems (e.g. irinotecan silicasomes) it is necessary to scale up synthesis of the drug-loaded silicasomes. In this regard, it was discovered that the synthesis protocols used for laboratory synthesis of drug-loaded silicasomes (e.g., 500 mg/batch) do not scale to large scale silicasome production, because the resulting products were too heterogeneous for use as pharmaceuticals. Accordingly, new methods are provided herein that effectively afford the large-scale production of mesoporous silica nanoparticles (MSNPs) and lipid bilayer coated MSNPs (silicasomes).

专利号:US-2015182634-A1
优先权日:2012-12-28
标 题:Molecular Design and Chemical Synthesis of Pharmaceutical-Ligands and Pharmaceutical-Pharmaceutical Analogs with Multiple Mechanisms of Action
发明人：COYNE CODY P; BEAR RYAN; JONES TONI
权利人:COYNE CODY P; BEAR RYAN; JONES TONI
摘要:Multi-phase and single-phase chemical reaction schemes have been developed for the synthesis of pharmaceutical-ligand analogs, pharmaceutical-pharmaceutical analogs, and similar molecular-molecular analogs that possess multiple mechanisms of action. The multi-phase organic chemical reaction schemes include relatively mild reaction conditions, high end product yields, and comparatively rapid completion of chemical reactions, which are all of particular utility for the synthesis of preparations including covalent pharmaceutical-receptor ligand or pharmaceutical-immunoglobulin analogs. Examples of pharmaceutical-ligand preparations that can be synthesized utilizing the multi-step chemical reaction schemes include covalent chemotherapeutic-ligand agents that possess selective targeted delivery properties and a capacity to exert additive and synergistic levels of cytotoxic anti-neoplastic potency. Pharmaceutical-pharmaceutical analogs, including chemotherapeutic-chemotherapeutic analogs that are capable of exerting multiple mechanisms of action, can be synthesized using either of the described multi-phase or single-phase organic chemistry reaction schemes. Each of these representative examples has utility against a spectrum of disease states including, for example, neoplastic conditions such as mammary adenocarcinoma/carcinoma, ovarian carcinoma, prostatic carcinoma, intestinal carcinoma, melanoma, leukemia, myeloma, and lymphoma.

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-10973847-B2
优先权日:2017-06-30
标题 :Core-to-surface polymerization for the synthesis of star polymers and uses thereof
发明人：JOHNSON JEREMIAH A; GOLDER MATTHEW R
权利人:MASSACHUSETTS INST TECHNOLOGY
摘要:Disclosed are methods, compositions, reagents, systems, and kits to prepare star polymers, as well as compositions and uses thereof. Various embodiments show that synthesis of these polymers contain low metal concentration to provide polymers for diverse biomedical applications including in vivo applications.

专利号:US-9034624-B2
优先权日:2009-06-16
标 题 :Process for the synthesis of conjugates of glycosaminoglycanes (GAG) with biologically active molecules, polymeric conjugates and relative uses thereof
发明人：D ESTE MATTEO; RENIER DAVIDE; PASUT GIANFRANCO; ROSATO ANTONIO
权利人:D ESTE MATTEO; RENIER DAVIDE; PASUT GIANFRANCO; ROSATO ANTONIO; FIDIA FARMACEUTICI
摘要:The present invention relates to a process for the synthesis of conjugates of glycosaminoglycanes (GAG) with biologically active molecules of varying nature, comprising small molecules and macro-molecules. In particular, the present invention relates to the conjugation of hyaluronic acid (HA) and its derivatives with polypeptides and proteins with a biological action, such as, for example, interferons, erythropoietins, growth factors, insulin, cytokines, antibodies and hormones. n An object of the present invention also relates to isolatable intermediates obtained by the partial or total reaction of GAG with protected amino aldehydes in the conjugation process mentioned above.

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