CAS: 51865-79-3; D-Amethopterin

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methotrexate

专利信息

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-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-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:US-2021220331-A1
优先权日:2016-05-03
标题:Inhibitors of ires-mediated protein synthesis
发明人：GERA JOSEPH F; LICHTENSTEIN ALAN; JUNG MICHAEL E; LEE JIHYE; HOLMES BRENT; BENAVIDES-SERRATO ANGELICA
权利人:UNIV CALIFORNIA; THE UNITED STATE GOVERNMENT REPRESENTED BY THE DEPT OF VETERANS AFFAIRS
摘要:This disclosure relates to inhibitors of IRES-mediated protein synthesis, compositions comprising therapeutically effective amounts of these compounds, and methods of using those compounds and compositions in treating hyperproliferative disorders, e.g., cancers. This disclosure also relates to compositions comprising inhibitors of IRES-mediated protein synthesis and mTOR inhibitors, and to methods of treating cancer by conjoint administration of inhibitors of IRES-mediated protein synthesis and mTOR inhibitors.