CAS: 796967-16-3; 1-(4-(3-Amino-1H-Indazol-4-yl)Phenyl)-3-(2-Fluoro-5-Methylphenyl)Urea

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CAS号599191-73-8 3-氨基-4-碘-吲唑 | CAS号796967-18-5 N-(2-氟-5-甲基苯基)-... | CAS号20925-60-4 4-氯-1H-吲唑-3-胺 | CAS号452-84-6 2-氟-5-甲基苯胺 | CAS号79544-29-9 2-氟-6-碘苯甲腈 | CAS号214360-73-3 4-氨基苯硼酸频哪醇酯 | CAS号1145835-80-8 N-[4-(3-amino-1...

4-氨基苯硼酸频哪醇酯置于1,1'-双(二苯膦基)二茂铁二氯化钯(II)二氯甲烷复合物 Sodium Carbonate体系中,用 乙二醇二甲醚,二氯甲烷,水 作为反应溶剂,化学反应 16.0H,反应生成 利尼伐尼
参考文献:Discovery Of N-(4-(3-Amino-1H-Indazol-4-yl)Phenyl)-N'-(2-Fluoro-5-Methylphenyl)Urea (Abt-869),A 3-Aminoindazole-Based Orally Active Multitargeted Receptor Tyrosine Kinase Inhibitor
标题:Discovery Of N-(4-(3-Amino-1H-Indazol-4-yl)Phenyl)-N'-(2-Fluoro-5-Methylphenyl)Urea (Abt-869),A 3-Aminoindazole-Based Orally Active Multitargeted Receptor Tyrosine Kinase Inhibitor
摘要:In Our Continued Efforts To Search For Potent And Novel Receptor Tyrosine Kinase (Rtk) Inhibitors As Potential Anticancer Agents,We Discovered,Through A Structure-Based Design,That 3-Aminoindazole Could Serve As An Efficient Hinge-Binding Template For Kinase Inhibitors. By Incorporating An N,N'-Diaryl Urea Moiety At The C4-Position Of 3-Aminodazole,A Series Of Rtk Inhibitors Were Generated,Which Potently Inhibited The Tyrosine Kinase Activity Of The Vascular Endothelial Growth Factor Receptor And The Platelet-Derived Growth Factor Receptor Families. A Number Of Compounds With Potent Oral Activity Were Identified By Utilizing An Estradiol-Induced Mouse Uterine Edema Model And An Ht1080 Human Fibrosarcoma Xenograft Tumor Model. In Particular,Compound 17P (Abt-869) Was Found To Possess Favorable Pharmacokinetic Profiles Across Different Species And Display Significant Tumor Growth Inhibition In Multiple Preclinical Animal Models.
DOI:10.1021/jm061280H

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-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:WO-2025128098-A1
优先权日:2023-12-13
标 题 :Solid oral dosage forms, kits, and methods of using the same
发明人：LI YING; LANGER ROBERT; TRAVERSO CARLO
权利人:MASSACHUSETTS INST TECHNOLOGY; BRIGHAM & WOMENS HOSPITAL INC
摘要:Provided herein are solid oral dosage forms, methods, and kits useful, e.g, for the extension of the residence time of active pharmaceutical agents in vivo by the synthesis of a polymer in situ in a subject. In particular, the solid oral dosage forms, methods, and kits disclosed herein are particularly useful for drugs that require more than once daily administration (e.g, drugs that have short half-lives).

专利号:US-12441733-B2
优先权日:2018-03-26
标题:Substituted 2,4-dioxotetrahydropyrimidines as intermediates in the synthesis of bruton's tyrosine kinase inhibitors
发明人：ARISTA LUCA; HEBACH CHRISTINA; HOLLINGWORTH GREGORY JOHN; HOLZER PHILIPP; IMBACH-WEESE PATRICIA; LORBER JULIEN; MACHAUER RAINER; SCHMIEDEBERG NIKO; VULPETTI ANNA; ZOLLER THOMAS
权利人:NOVARTIS AG
摘要:The invention relates to compounds of the formulae (I), (III), (IIIa), (XXIa), (XXIII), and/or (XLVI)or a pharmaceutically acceptable salt thereof, wherein the substituents are as defined in the specification; to intermediates in the preparation of the compounds, to pharmaceutical compositions comprising the compounds and to use of the compounds in the treatment of disease.

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.

专利号:US-2024400576-A1
优先权日:2021-09-03
标 题:Nitrogen-containing derivatives of salinomycin, synthesis and uses thereof
发明人：RODRIGUEZ RAPHAËL; CZERWONKA DOMINIKA; ANTOSZCZAK MICHAL; HUCZYNSKI ADAM
权利人:CENTRE NAT RECH SCIENT; INST CURIE; INST NAT SANTE RECH MED; ADAM MICKIEWICZ UNIV
摘要:The present invention relates to nitrogen-containing derivatives of salinomycin having the formula (I), as well as pharmaceutically acceptable salt thereof, and synthesis and uses thereof, in particular for the treatment and/or prevention of cancer including for preventing cancer metastasis and/or for preventing cancer recurrence and/or for decreasing resistance to a chemotherapy in a subject.