CAS: 341031-54-7; (Z)-N-(2-(Diethylamino)Ethyl)-5-((5-Fluoro-2-Oxoindolin-3-Ylidene)Methyl)-2,4-Dimethyl-1H-Pyrrole-3-Carboxamide (S)-2-Hydroxysuccinate

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CAS号97-67-6 L-苹果酸 | CAS号1374685-40-1 5-fluoro-1-(tri... | CAS号356068-86-5 N-(2-(二乙基氨基)乙基)... | CAS号56341-41-4 5-氟吲哚酮 | CAS号1200435-83-1 L-(-)-malic aci... | CAS号557795-19-4 舒尼替尼 | CAS号2689-91-0 L-malic acid , ... | CAS号1332307-07-9 N1,N1-diethylet... | CAS号1032268-12-4 5-fluoro-2-oxindole | CAS号1338703-87-9 sodium (4-((2-(...

2,4-二甲基-5-醛基-1H-吡咯-3-羧酸置于1-羟基苯并三唑,盐酸-N-乙基-Nˊ-(3-二甲氨基丙基)碳二亚胺,三乙胺体系中,用 甲醇,乙腈 作为反应溶剂,化学反应 7.0H,反应生成 苹果酸舒尼替尼
参考文献:一种高纯度苹果酸舒尼替尼的制备方法
标题:一种高纯度苹果酸舒尼替尼的制备方法
摘要:本发明涉及一种高纯度苹果酸舒尼替尼的制备方法,所述方法包括以下步骤:(1)式ⅱ化合物为起始物料,使用1‑乙基‑(3‑二甲基氨基丙基)碳酰二亚胺盐酸盐与1‑羟基苯并三唑为缩合剂,在一定温度下与n,N二乙基乙二胺反应得到化合物ⅲ;(2)在步骤(1)的反应液中,使步骤(1)所得反应物与5‑氟吲哚‑2‑酮在一定温度下反应,得到化合物ⅳ;(3)在步骤(2)的反应液中,使步骤(1)所得反应物与l‑苹果酸在一定温度下反应,得到化合物ⅰ;提供至少在一定程度上解决上述技术问题之一或至少提供一种有用的商业选择.反应路线操作时间短,反应操作简单,反应体系稳定,产物收率较高,产物纯度较高,适于工业化生产.

专利信息

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-2024209029-A1
优先权日:2021-04-21
标题:Adiponectin glycopeptides and compositions and methods of use thereof
发明人：WANG YU; LI XUECHEN; XU AIMIN; WU HONGXIANG; ZHANG YIWEI; LI YUANXIN
权利人:UNIV HONG KONG
摘要:An improved method for the chemical synthesis of glycosylated peptides has been developed. The method uses stereoselective glycan synthesis and chemical peptide ligation to produce glycopeptides at lower-cost and with higher efficiency/yield compared to conventional methods. In particular, a method for the large-scale, chemical synthesis of hydroxylated amino acid building blocks and glycosylated amino acids suitable for solid phase peptide synthesis (SPPS) are disclosed. SPPS-based methods using the glycosylated amino acids to chemically synthesize adiponectin-like peptides are also described. In vivo studies show that the adiponectin mimicking glycopeptides exhibit significant anticancer, anti-obesity and insulin sensitizing effects. Pharmaceutical compositions of the synthetic glycopeptides and methods of use thereof in treating diseases associated with deficient adiponectin are also described.

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-9567430-B2
优先权日:2011-12-02
标 题 :Enzymatic synthesis of poly(amine-co-esters) and methods of use thereof for gene delivery
发明人：SALTZMAN W MARK; JIANG ZHAOZHONG; ZHOU JIANGBING; LIU JIE
权利人:UNIV YALE
摘要:Poly(amine-co-ester) polymers, methods of forming active agent-load nanoparticles therefrom, and methods of using the nanoparticles for drug delivery are disclosed. The nanoparticles can be coated with an agent that reduces surface charge, an agent that increases cell-specific targeting, or a combination thereof. Typically, the loaded nanoparticles are less toxic, more efficient at drug delivery, or a combination thereof compared to a control other transfection reagents. In some embodiments, the nanoparticles are suitable for in vivo delivery, and can be administered systemically to a subject to treat a disease or condition.

专利号:WO-2013082529-A1
优先权日:2011-12-02
标题 :Enzymatic synthesis of poly(amine-co-esters) and methods of use thereof for gene delivery
发明人：SALTZMAN W MARK; JIANG ZHAOZHONG; ZHOU JIANGBING
权利人:UNIV YALE
摘要:Poly(amine-co-ester) polymers, methods of forming active agent-load nanoparticies therefrom, and methods of using the nanoparticies for drug delivery are disclosed. The nanoparticies can be coated with an agent that reduces surface charge, an agent that increases cell-specific targeting, or a combination thereof. Typically, the loaded nanoparticies are less toxic, more efficient at drug delivery, or a combination thereof compared to a control other transfection reagents. In some embodiments, the nanoparticies are suitable for in vivo delivery, and can be administered systemically to a subject to treat a disease or condition.

专利号:US-10772971-B2
优先权日:2017-06-22
标 题:Methods of producing drug-carrying polymer scaffolds and protein-polymer-drug conjugates
发明人：GURIJALA VENU REDDY; BOLLU SATYANARAYAN REDDY; LEBLANC JACQUES; LOWINGER TIMOTHY B; MCGILLICUDDY DENNIS; YIN MAO; YURKOVETSKIY ALEKSANDR V
权利人:MERSANA THERAPEUTICS INC; MERSANA THERPEUTICS INC
摘要:The disclosure provides methods of synthesis of polymeric scaffolds, e.g., those useful for conjugating with a protein based recognition-molecule (PBRM) to form PBRM-polymer-drug conjugates, and PBRM-polymer-drug conjugates thereof. The methods according to the disclosure allow for large-scale preparation of polymeric scaffolds having a high purity. In some embodiments, the methods according to the disclosure also allow for the preparation of scaffolds and conjugates thereof in better yield than previously used methods for preparing same. Also disclosed are methods of purifying polymeric scaffolds.