CAS: 698387-09-6; (E)-N-(4-((3-Chloro-4-(Pyridin-2-Ylmethoxy)Phenyl)Amino)-3-Cyano-7-Ethoxyquinolin-6-yl)-4-(Dimethylamino)But-2-Enamide

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CAS号848139-78-6 6-氨基-4-(3-氯-4-(... | CAS号1055943-40-2 3-N,N-二甲氨基甲基丙烯酰氯盐酸盐 | CAS号524955-09-7 [3-氯-4-(吡啶-2-甲氧... | CAS号848133-88-0 (E)-N-(4-chloro... | CAS号3616-56-6 二甲氨基乙醛缩二乙醇 | CAS号1056149-69-9 3-N,N-二甲氨基甲基丙烯酰氯 | CAS号214476-09-2 4-氯-3-氰基-7-乙氧基-... | CAS号848133-87-9 6-氨基-4-氯-7-乙氧基-... | CAS号619-08-9 2-氯-4-硝基酚

反式-4-二甲基胺基巴豆酸盐酸盐置于草酰氯,吡啶盐酸盐,N,N-二甲基甲酰胺体系中,用 N-甲基吡咯烷酮,异丙醇,乙腈 作为反应溶剂,化学反应 3.0H,反应生成 来那替尼
参考文献:优化6,7-二取代的-4-(芳基氨基)喹啉-3-甲腈作为人类表皮生长因子受体2激酶活性的口服活性,不可逆抑制剂的作用.
标题:优化6,7-二取代的-4-(芳基氨基)喹啉-3-甲腈作为人类表皮生长因子受体2激酶活性的口服活性,不可逆抑制剂的作用.
摘要:一系列新的6,7-二取代的4-(芳基氨基)喹啉-3-甲腈衍生物可作为人类表皮生长因子受体2(her-2)和表皮生长因子受体(egfr)激酶的不可逆抑制剂发挥作用.准备好了.与我们的egfr激酶抑制剂86(ekb-569)相比,这些化合物表现出增强的抑制her-2激酶和her-2阳性细胞生长的活性.使用三种合成途径来制备这些化合物.它们的制备主要是通过6-氨基-4-(芳基氨基)喹啉-3-腈与不饱和酰氯的酰化作用或通过4-氯-6-(巴豆酰胺基)喹啉-3-腈与单环或双环苯胺的胺化而制备的.开发了第三条路线来制备关键中间体,即6-乙酰氨基-4-氯喹啉-3-腈,该中间体涉及更安全的环化步骤.我们显示,在4-(芳基氨基)环的对位上附加一个大的亲脂基团会导致抑制her-2激酶的效力提高.我们还显示了在迈克尔受体末端的碱性二烷基氨基对于活性的重要性,这归因于迈克尔加成的分子内催化作用.这与改善的水溶性一起
DOI:10.1021/jm040159C

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-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-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-2022233673-A1
优先权日:2019-06-04
标 题:METHODS OF PRODUCING SHIGA TOXIN B-SUBUNIT (STxB) MONOMERS AND OLIGOMERS, AND USES THEREOF
发明人：BILLET ANNE; SCHMIDT FRÉDÉRIC; JOHANNES LUDGER; SERVENT DENIS; MOURIER GILLES; TARTOUR ÉRIC; KAY MICHAEL; FULCHER JAMES M
权利人:INST CURIE; CENTRE NAT RECH SCIENT; INST NAT SANTE RECH MED; COMMISSARIAT A LENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES CEA; APHP ASSIST PUBLIQUE HOPITAUX DE PARIS; UNIV PARIS; UNIV OF UTAH RESEARCH FOUDATION; UNIV UTAH RES FOUND
摘要:A method of producing a monomer of a Shiga toxin B-subunit (STxB) protein or of a variant thereof by peptide chemical synthesis, as well as to a method of producing a pentamer of the STxB protein or of the variant thereof. The methods are particularly advantageous as they overcome major issues typically observed in peptide chemical synthesis, including solubility and purity issues.

专利号:US-7126025-B2
优先权日:2003-01-21
标 题 :Synthesis of 4-(amino)-2-butenoyl chlorides and their use in the preparation of 3-cyano quinolines
发明人：CONSIDINE JOHN LEO; DAIGNEAULT SYLVAIN; CHEW WARREN; IERA SILVIO; DUNCAN SCOTT MASON; REN JIANXIN
权利人:WYETH CORP
摘要:This invention provides a compound of Formula (I): n nwhereinn S 1 and S 2 are each independently, hydrogen, alkyl, alkenyl, alkynyl, aralkyl, substituted or unsubstituted aryl, and S 1 and S 2 together with the nitrogen to which they are attached form a nitrogen containing heteroaryl and a pharmaceutically acceptable salt thereof; a method of preparing the compound of Formula (I), and use of the compound of Formula (I) in the preparation of 3-cyano quinolines.

专利号:US-11649285-B2
优先权日:2016-08-03
标题 :Identification of VSIG3/VISTA as a novel immune checkpoint and use thereof for immunotherapy
发明人：KALABOKIS VASSILIOS; WANG JINGHUA; WU GUOPING; BAZAN JOSE FERNANDO; VALLEY CHRISTOPHER CARLIN
权利人:BIO TECHNE CORP
摘要:The ligand for VISTA is identified (VSIG3) as well as the use of this ligand and receptor interaction in the identification or synthesis of a VSIG3 agonist or antagonist compounds, preferably antibodies, polypeptides and fusion proteins which agonize or antagonize the effects of VSIG3 and/or VISTA and/or the VSIG3/VISTA interaction. These antagonists may be used to suppress VSIG3/VISTA's suppressive effects on T cell immunity, and more particularly used in the treatment of cancer, or infectious disease. These agonist compounds may be used to potentiate or enhance VSIG3/VISTA's suppressive effects on T cell immunity and thereby suppress T cell immunity, such as in the treatment of autoimmunity, allergy or inflammatory conditions. Screening assays for identifying these agonists and antagonist compounds are also provided.