📜新戊酰基乙腈置于盐酸,4-二甲氨基吡啶,N,N-二异丙基乙胺体系中,用 乙醇,二氯甲烷,水,二甲基亚砜 用作溶剂,化学反应 9.33H,反应生成N-[3-叔丁基-1-(喹啉-6-基)-1H-吡唑-5-基]-N'-[2-氟-4-[(2-(甲基氨基甲酰基)吡啶-4-基)氧]苯基]脲 参考文献:Methods Of Using Rebastinib In The Treatment Of Disorders 标题:Methods Of Using Rebastinib In The Treatment Of Disorders 摘要:本文描述了治疗患有各种疾病的患者的方法,包括向患者施用化合物i的药物或其药用盐.本文描述的方法可以治疗的示例疾病包括妇科肉瘤,子宫内膜腺癌,间皮瘤,卵巢癌,胰腺导管腺癌和肺癌.
专利信息
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-11753392-B2 优先权日:2018-04-13 标题:Method for synthesis of deuterated amide and deuterated sulfonamide 发明人:DU WU; WEN KUN; HE JINYUN; LI HAIBO; QIN DEKUN; LI XINGHAI; CHEN YUANWEI 权利人:HINOVA PHARMACEUTICALS INC 摘要:A novel method for synthesizing deuterated amides and deuterated sulfonamides includes the following steps: (1) adding a compound M, DMAP, R3—X to a solvent to obtain a compound N after a reaction is complete; and (2) adding the compound N, R4—NH—R5, or a salt and base thereof to a solvent, and purifying after a reaction is complete to obtain a compound I.
专利号:US-12180228-B2 优先权日:2019-06-05 标题:Compounds, conjugates, and compositions of epipolythiodiketopiperazines and polythiodiketopiperazines and uses thereof 发明人:MOVASSAGHI MOHAMMAD; OLSSON CHASE ROBERT; SCOTT TONY Z; CHEAH JAIME; PAYETTE JOSHUA NATHANIEL 权利人:MASSACHUSETTS INST TECHNOLOGY 摘要:The present disclosure provides, e.g., compounds, compositions, kits, methods of synthesis, and methods of use, involving epipolythiodiketopiperazines and polythiodiketopiperazines.
专利号:US-2021115009-A1 优先权日:2018-04-13 标 题 :Method for synthesis of deuterated amide and deuterated sulfonamide
专利号:CA-3096963-A1 优先权日:2018-04-13 标题:A new method for synthesis of deuterated amide and deuterated sulfonamide
1: Zaini A, Jawad HE, Al-Mudhafar DH, Hadi NR. Rebastinib attenuates liver injury following cecal ligation and puncture in male mice. J Med Life. 2023 Nov;16(11):1678-1684. doi: 10.25122/jml-2023-0089. 2: Karagiannis GS, Pastoriza JM, Wang Y, Harney AS, Entenberg D, Pignatelli J, Sharma VP, Xue EA, Cheng E, D'Alfonso TM, Jones JG, Anampa J, Rohan TE, Sparano JA, Condeelis JS, Oktay MH. Neoadjuvant chemotherapy induces breast cancer metastasis through a TMEM-mediated mechanism. Sci Transl Med. 2017 Jul 5;9(397):eaan0026. doi: 10.1126/scitranslmed.aan0026. Erratum in: Sci Transl Med. 2017 Jul 19;9(399):eaao3817. doi: 10.1126/scitranslmed.aao3817. 3: Li X, Li J, Xu L, Wei W, Cheng A, Zhang L, Zhang M, Wu G, Cai C. CDK16 promotes the progression and metastasis of triple-negative breast cancer by phosphorylating PRC1. J Exp Clin Cancer Res. 2022 Apr 21;41(1):149. doi: 10.1186/s13046-022-02362-w.
合成参考文献
参考文献:10.1186/s13287-021-02659-1 摘要:Mojtahedi H, Yazdanpanah N, Rezaei N. Chronic myeloid leukemia stem cells: targeting therapeutic implications. Stem Cell Research & Therapy. 2021 Dec 18;12(1):603. doi: 10.1186/s13287-021-02659-1.