📜(6-Chloro-4-(Ethylamino)Pyridin-3-yl)Methanol置于manganese(Iv) Oxide,Aluminum Oxide,Potassium Fluoride,三乙胺体系中,用 四氢呋喃,1,4-二氧六环,二氯甲烷,N,N-二甲基乙酰胺,水 用作溶剂,化学反应 102.0H,反应生成瑞普替尼 参考文献:Dihydronaphthyridines And Related Compounds Useful As Kinase Inhibitors For The Treatment Of Proliferative Diseases 标题:Dihydronaphthyridines And Related Compounds Useful As Kinase Inhibitors For The Treatment Of Proliferative Diseases 摘要:这项发明涉及二氢萘啶和相关化合物;包括有效量二氢萘啶或相关化合物的组合物;以及治疗或预防增生性疾病的方法,包括给予有效量二氢萘啶或相关化合物.
专利号:WO-2023122322-A1 优先权日:2021-12-24 标 题:Improved processes for the preparation of ripretinib 发明人:LUTHRA PARVEN KUMAR; SINHA CHANDRASEKHAR; AROTE NITIN DNYANESHWAR; PANDEY ANAND KUMAR; TYAGI BHUPENDRA PRAKASH; SONAR JITENDRA KAMALAKAR; JAISWAL SANJAY; MISTRY MAULIK DIPAKBHAI 权利人:TEVA PHARMACEUTICALS INT GMBH; TEVA PHARMA 摘要:The present invention relates to safe and improved processes for the preparation of substantially pure intermediates of formula Va and their use in the synthesis of Ripretinib and salts thereof.
专利号:US-8188113-B2 优先权日:2006-09-14 标 题 :Dihydropyridopyrimidinyl, dihydronaphthyidinyl and related compounds useful as kinase inhibitors for the treatment of proliferative diseases 发明人:FLYNN DANIEL L; PETILLO PETER A; KAUFMAN MICHAEL D; PATT WILLIAM C 权利人:FLYNN DANIEL L; PETILLO PETER A; KAUFMAN MICHAEL D; PATT WILLIAM C; DECIPHERA PHARMACEUTICALS INC 摘要:The present invention relates to novel dihydropyridopyrimidinyl, dihydronaphthyridinyl, and related compounds which are kinase inhibitors and modulator useful for the treatment of various diseases. More particularly, the invention is concerned with such compounds, kinase/compound adducts, methods of treating diseases, and methods of synthesis of the compounds. Preferably, the compounds are useful for the modulation of kinase activity of Raf kinases and disease polymorphs thereof. Compounds of the present invention find utility in the treatment of mammalian cancers and especially human cancers including but not limited to malignant melanoma, colorectal cancer, ovarian cancer, papillary thyroid carcinoma, non small cell lung cancer, and mesothelioma. Compounds of the present invention also find utility in the treatment of rheumatoid arthritis and retinopathies including diabetic retinal neuropathy and macular degeneration.
专利号:US-12390420-B1 优先权日:2024-10-22 标题 :Compositions for targeted delivery of therapeutic agents and methods for the synthesis and use thereof 发明人:EGUCHI MASAKATSU 权利人:BRYET US INC 摘要:The present disclosure provides compositions and methods for delivering therapeutic agents to particular tissues or cells in a subject. The composition disclosed herein combines unique properties of porous micro- or nano-particles with host-guest chemistry provided by functionalized silicon particle, offering a versatile approach to addressing the challenges associated with delivering therapeutic agents to target tissues or sites within the body. The present disclosure also provides a method for synthesizing a composition capable of delivering therapeutic agents to particular tissues or cells in a subject.
专利号:US-2024208898-A1 优先权日:2021-03-25 标 题 :Enamine n-oxides: synthesis and application to hypoxia-responsive prodrugs and imaging agents 发明人:KIM JUSTIN; KANG DAHYE; CHEUNG SHELDON T 权利人:DANA FARBER CANCER INST INC 摘要:Disclosed are compounds and pharmaceutically acceptable salts and stereoisomers thereof that are suitable for diagnosis and the treatment of diseases and disorders characterized by, associate with or which exhibit tissue hypoxia, such as, for example, solid tumors. Also disclosed are pharmaceutical compositions containing same, and methods of making and using the compounds.
专利号:WO-2025137620-A1 优先权日:2023-12-21 标题:Methods for high quality and high accuracy methylation sequencing 发明人:KENNEDY ANDREW 权利人:GUARDANT HEALTH INC 摘要:Provided herein are methods and compositions for calibrating one or more base calling metrics in a sequencing by synthesis reaction, and for calling at least a portion of nucleobases in a converted region of a DNA molecule using the one or more calibrated base calling metrics. Provided herein are also methods for determining the likelihood that a subject has a disease or condition, such as cancer.
专利号:JP-2024512568-A 优先权日:2021-03-25 标 题:Enamine N-oxide: synthesis and application of hypoxia-responsive prodrugs and contrast agents