CAS: 80576-83-6; (2S)-2-(4-(1-(2,4-Diaminopteridin-6-yl)Butan-2-yl)Benzamido)Pentanedioic Acid

上下游产品

CAS号151071-45-3 methyl 4-[2-(2,... | CAS号1118-89-4 L-谷氨酸二乙酯盐酸盐 | CAS号80576-81-4 4-[1-(2,4-diami... | CAS号2438-05-3 4-丙基苯甲酸 | CAS号80576-79-0 4-(5-bromo-6-ox...

📜Methyl 4-<2-(2,4-Diamino-6-Pteridinyl)-1-Ethylethenyl>Benzoate置于platinum(Iv) Oxide Sodium Hydroxide,氢气,三乙胺,氯甲酸异丁酯体系中,用 甲醇,溶剂黄146,二甲基亚砜 作为反应溶剂,20.0~25.0 °C,324.24 Kpa 条件下,反应 87.25H,反应生成 依达曲沙
参考文献:10-乙基-5-甲基-5,10-二氮杂氨基蝶呤的合成和抗叶酸评估,以及10-乙基-10-脱氮杂min蝶呤(edatrexate)的替代合成.
标题:10-乙基-5-甲基-5,10-二氮杂氨基蝶呤的合成和抗叶酸评估,以及10-乙基-10-脱氮杂min蝶呤(edatrexate)的替代合成.
摘要:先前的发现表明5,10-二叠氮杂氨基蝶呤的5,10-二烷基取代的衍生物值得研究,因为潜在的抗叶酸药物提示了10-乙基-5-甲基-5,10-二氮杂氨基蝶呤的合成(12A).合成路线12A的关键步骤是将6-(溴甲基)-2,4-二氨基-5-甲基吡啶并[2,3-D]嘧啶(7A)衍生的三丁基膦与4-丙酰基苯甲酸甲酯进行wittig缩合.使用由6-(溴甲基)-2,4-哌啶二胺(7B)制备的三丁基膦烷开发了wittig缩合反应的条件.每个维蒂希产品8A和8B以75-80%的产率获得.8A和8B在它们的9,10-双键处氢化,得到4-氨基-4-脱氧-10-乙基-5-甲基-5,10-二脱氮杂戊酸甲酯(9A)和4-氨基-4-脱氧-10-乙基-10-脱氮杂戊酸甲酯(9B).据报道,这种通向9B的途径与合成方法有关,可导致10-乙基-10-Deazaaminopterin(10-Edam,Edatrexate),该
DOI:10.1021/jm00094A011

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-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: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-11155562-B2
优先权日:2014-06-30
标 题 :Synthesis of halichondrin analogs and uses thereof
发明人：KISHI YOSHITO; UEDA ATSUSHI; YAMAMOTO AKIHIKO; KATO DAISUKE
权利人:HARVARD COLLEGE
摘要:The present invention provides halichondrin analogs, such as compounds of Formula (I). The compounds may bind to microtubule sites, thereby inhibiting microtubule dynamics. Also provided are methods of synthesis, pharmaceutical compositions, kits, methods of treatment, and uses that involve the compounds for treatment of a proliferative disease (e.g., cancer). Compounds of the present invention are particularly useful for the treatment of metastatic breast cancer, non-small cell lung cancer, prostate cancer, and sarcoma. The included methods of synthesis are useful for the preparation of compounds of Formula (I)-(III) along with naturally occurring halicondrins (e.g., halichondrin B & C, norhalichondrin A, B, & C, and homohalichondrin A, B, & C). Also included are methods for interconverting between the halichondrins, norhalichondrins, and homohalichondrins and their unnatural epimers at the C38 ketal stereocenter through the use of an acid-mediated equilibration.