CAS: 59-05-2; (S)-2-(4-(((2,4-Diaminopteridin-6-yl)Methyl)(Methyl)Amino)Benzamido)Pentanedioic Acid

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4-[n-(2,4-二氨基-6-蝶啶甲基)-N-甲氨基]苯甲酸半盐酸盐n水置于benzotriazol-1-Yloxyl-Tris-(Pyrrolidino)-Phosphonium Hexafluorophosphate,三乙胺,三氟乙酸体系中,用 二氯甲烷,二甲基亚砜 作为反应溶剂,化学反应 13.0H,反应生成 甲氨蝶呤
参考文献: Methotrexate Analogs And Methods Of Use[fr] Analogues De Méthotrexate Et Procédés D'Utilisation
标题: Methotrexate Analogs And Methods Of Use[fr] Analogues De Méthotrexate Et Procédés D'Utilisation
摘要:本文提供了具有通式(i)或其药用可接受的盐,N-氧化物或水合物的化合物.还提供了制备这些化合物的方法以及它们的使用方法,包括在癌症,自身免疫性疾病和病毒感染的治疗中的应用.

专利信息

专利号:US-7230101-B1
优先权日:2002-08-28
标 题:Synthesis of methotrexate-containing heterodimeric molecules
发明人：MURTHI KRISHNA K; SMITH CHASE C
权利人:GPC BIOTECH INC
摘要:The present invention relates to novel compositions of methotrexate-containing heterodimeric probe molecules, also known as chemical inducers of dimerization (CID), useful in three-hybrid assays. The invention further relates to synthesis of said compositions and their intermediates. Another aspect of the invention is a method for using the heterodimeric probe molecules described herein in drug screens to identify potential protein targets to a given ligand, optimize protein-ligand interactions, or identify potential ligands for a given protein target. In certain embodiments, the invention contemplates the synthesis of the following methotrexate-containing heterodimeric probe:

专利号:US-2012177593-A1
优先权日:2009-07-20
标 题 :Synthesis of dendrimer conjugates
发明人：BAKER JR JAMES R; ZHANG YUEHUA; THOMAS THOMMEY P; DESAI ANKUR MAHESH
权利人:BAKER JR JAMES R; ZHANG YUEHUA; THOMAS THOMMEY P; DESAI ANKUR MAHESH; UNIV MICHIGAN
摘要:The present invention relates to novel methods of synthesis of therapeutic and diagnostic dendrimers. In particular, the present invention is directed to novel dendrimer conjugates, novel methods of synthesizing the same, compositions comprising the conjugates, as well as systems and methods utilizing the conjugates (e.g., in diagnostic and/or therapeutic settings (e.g., for the delivery of therapeutics, imaging, and/or targeting agents (e.g., in disease (e.g., cancer, inflammatory disease) diagnosis and/or therapy, pain therapy, etc.)). Accordingly, dendrimer conjugates of the present invention may further comprise at least two different components for targeting, imaging, sensing, and/or providing a therapeutic or diagnostic material and/or monitoring response to therapy. Furthermore, the novel synthesis methods of certain embodiments of the present invention provide significant advantages with regard to total reaction time and simplicity.

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-2004006137-A1
优先权日:2002-06-28
标题:Asymmetric synthesis of amino-pyrrolidinones and a crystalline, free-base amino-pyrrolidinone
发明人：WALTERMIRE ROBERT E; CAMPAGNA SILVIO; SAVAGE SCOTT A; BORDAWEKAR SHAILENDRA; MADUSKUIE THOMAS P; DESIKAN SRIDHAR; ANDERSON STEPHEN R
摘要:A novel process for the asymmetric synthesis of an amino-pyrrolidinone of the type shown below is described. n n n These compounds are useful as intermediates for MMP and TACE inhibitors. n Crystalline, free-base form of Compound J ((2R)-2-((3R)-3-amino-3-{-[(2-methyl-4-quinolinyl)methoxy]phenyl}-2-oxopyrrolidinyl)-N-hydroxy-4-methylpentanamide): n n n which is useful as a TACE inhibitor, pharmaceutical compositions comprising the same, and methods of using the same for treating inflammatory diseases are also described.

专利号:WO-2024104433-A9
优先权日:2022-11-16
标 题:Use of galectin-1 as immune checkpoint in preparation of tumor immunotherapy medicament and medicament
发明人：ZHANG YU; HONG YU; SI XIAOFANG; LIU WENJING; MAI XUEYING
权利人:NAT INSTITUTE OF BIOLOGICAL SCIENCES BEIJING
摘要:Provided are use of galectin-1 (Gal-1) as an immune checkpoint in the preparation of a tumor immunotherapy medicament and the medicament, and provided is a new tumor immunotherapy strategy targeting the new immune checkpoint. Lactose and a derivative thereof can inhibit the immune checkpoint by competing Gal-1 on the surfaces of a cancer cell and an immune cell, and do not have significant toxic and side effects. Knocking out B4GATL1 to reduce protein galactosylation can significantly reduce the level of Gal-1 transferred from a tumor to a T cell, thereby enhancing the activation and function of the T cell. In addition, a lactose synthetase component LALBA is overexpressed in a mouse tumor, and de novo synthesis of lactose in a tumor microenvironment can be realized, such that an immune response mediated by a CD8+ T cell is enhanced. In combination with the anti-tumor effect and economic cost of lactose, a wide and feasible idea is provided for cancer treatment.

专利号:WO-2025020448-A1
优先权日:2023-07-24
标 题 :Synthesis method for nano drug for treating rheumatoid arthritis
发明人：TAN JIANWEI; CHEN JINGQIN; XUE QIANG; CHEN JIANHAI; LIN RIQIANG; LIU CHENGBO
权利人:SHENZHEN INST OF ADV TECH CAS
摘要:The present invention relates to the technical field of nano drug synthesis. Disclosed is a synthesis method for a nano drug for treating rheumatoid arthritis, comprising the following steps: S10: acquiring or preparing CaO2 nanoparticles having high purity and a small particle size; S20: wrapping the CaO2 nanoparticles in a ZIF67 system to obtain CaO2@ZIF67; and S30: dissolving methotrexate in methanol to obtain an MTX additive solution, dissolving CaO2@ZIF67 in methanol, then dropwise adding the MTX additive solution, fully stirring, and finally purifying, washing and drying the obtained product to obtain CaO2@MTX@ZIF67. For two main pathological features, i.e., inflammation and an anoxic microenvironment, of rheumatoid arthritis, calcium peroxide loaded by ZIF67 is combined with methotrexate to jointly treat the inflammatory part of rheumatoid arthritis, so that a construct can inhibit expression of a tumor necrosis factor -α/interleukin-6 and overcome the anoxic property of rheumatoid arthritis, thereby achieving the technical characteristics of mitigating an inflammatory symptom, changing a disease process, being low in cost, less in side effect and used for long-term treatment, and the like.