📜3-Methoxy-4-[3-(Morpholin-4-yl)Propoxy]-2-Nitrobenzaldehyde置于4-二甲氨基吡啶,C9H19N3*clh,5% Pd-1%fe/c,氢气,Potassium Carbonate,三乙胺体系中,用 乙醇,二氯甲烷,N,N-二甲基甲酰胺 用作溶剂,-5.0~75.0 °C,10.0 Mpa 条件下,反应 47.92H,反应生成库潘尼西 参考文献: Synthesis Of Copanlisib And Its Dihydrochloride Salt[fr] Synthèse De Copanlisib Et De Son Sel Dichlorhydrate 标题: Synthesis Of Copanlisib And Its Dihydrochloride Salt[fr] Synthèse De Copanlisib Et De Son Sel Dichlorhydrate 摘要:本发明涉及一种制备科帕利西布和科帕利西布盐酸二水合物的新方法,涉及新的中间化合物,以及利用这些新的中间化合物制备科帕利西布的用途.
专利信息
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.
专利号:US-10494372-B2 优先权日:2014-11-07 标 题 :Synthesis of copanlisib and its dihydrochloride salt 发明人:PETERS JAN-GEORG; RUBENBAUER PHILIPP; GÖTZ DANIEL; GROSSBACH DANJA; MAIS FRANZ-JOSEF; SCHIRMER HEIKO; STIEHL JUERGEN; LOVIS KAI; LENDER ANDREAS; SEYFRIED MARTIN; ZWEIFEL THEODOR; MARTY MAURUS; WEINGÄRTNER GÜNTER 权利人:Bayer Pharma AG 摘要:The present invention relates to a novel method of preparing copanlisib, copanlisib dihydrochloride, or hydrates of copanlisib dihydrochloride, to novel intermediate compounds, and to the use of said novel intermediate compounds for the preparation of said copanlisib, copanlisib dihydrochloride, or hydrates of copanlisib dihydrochloride. The present invention also relates to copanlisib dihydrochloride hydrates as compounds.
专利号:US-10035803-B2 优先权日:2014-11-07 标 题:Synthesis of copanlisib and its dihydrochloride salt 发明人:PETERS JAN-GEORG; STIEHL JÜRGEN; LOVIS KAI 权利人:Bayer Pharma AG 摘要:The present invention relates to a novel method of preparing copanlisib, and copanlisib dihydrochloride, to novel intermediate compounds, and to the use of said novel intermediate compounds for the preparation of said copanlisib.
专利号:US-2025289827-A1 优先权日:2022-12-02 标 题:Morphic forms of a mutant braf degrader and methods of manufacture thereof 发明人:YU ROBERT T; HE MINSHENG; SCHNADERBECK MATTHEW J; KREGER BRIDGET; POLLOCK ROY MACFARLANE; JIANG SIYI; LI MEIQI; CHEN BOLU; LU JIANNAN 权利人:C4 THERAPEUTICS INC 摘要:Advantageous isolated morphic forms of (3R)-3-[6-[2-cyano-3-[[ethyl(methyl)sulfamoyl]amino]-6-fluorophenoxy]-4-oxoquinazolin-3-yl]-8-[2-[1-[3-(2,4-dioxo-1,3-diazinan-1-yl)-5-fluoro-1-methylindazol-6-yl]-4-hydroxypiperidin-4-yl]acetyl]-1-oxa-8-azaspiro[4.5]decane (Compound 1), which is a mutant BRAF degrader, and methods to prepare Compound 1 morphic forms for therapeutic applications are provided in the invention. The invention also provides improved methods for the synthesis of Compound 1, new pharmaceutical compositions comprising Compound 1, and new uses of Compound 1.
专利号:US-2022118123-A1 优先权日:2019-02-22 标 题 :Combination of ar antagonists and targeted thorium conjugates 发明人:HAMMER STEFANIE; HAGEMANN URS BEAT; HAENDLER BERNARD; LEJEUNE PASCALE; ZITZMANN-KOLBE SABINE; SCHATZ CHRISTOPH; KARLSSON JENNY 权利人:BAYER AG; BAYER AS 摘要:The present invention covers combinations of at least two components, component A and component B, comprising component A being PSMA-TTC, and component B being an antiandrogen selected form AR antagonists such as from cyproterone acetate, bicalutamide, flutamide, nilutamide, enzalutamide, apalutamide, darolutamide or keto-darolutamide, or an AR degrader such as ARV-110, or an ARN-terminal domain binder such as EPI-506, or an antisense oligonucleotide that reduces AR expression such as EZN-4176 or AZD-5312, or an androgen synthesis inhibitor such as abiraterone, particularly abiraterone acetate, seviteronel, galeterone, orteronel or ketoconazole, or a dual AR antagonist and androgen synthesis inhibitor such as ODM-204. Another aspect of the present invention covers the use of such combinations as described herein for the preparation of a medicament for the treatment or prophylaxis of a disease, particularly for the treatment of a hyper-proliferative disease.
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.
1: LiverTox: Clinical and Research Information on Drug-Induced Liver Injury [Internet]. Bethesda (MD): National Institute of Diabetes and Digestive and Kidney Diseases; 2012-. Available from http://www.ncbi.nlm.nih.gov/books/NBK548413/ doi: 10.1038/s41420-019-0165-7. eCollection 2019. 4: Eltantawy A, Vallejos X, Sebea E, Evans K. Copanlisib: An Intravenous Phosphatidylinositol 3-Kinase (PI3K) Inhibitor for the Treatment of Relapsed Follicular Lymphoma. Ann Pharmacother. 2019 Sep;53(9):954-958. doi: 10.1177/1060028019833992. Epub 2019 Feb 27. doi: 10.1016/j.clml.2018.11.021. Epub 2018 Nov 29. 7: Dittakavi S, Mullangi R. LC-ESI-MS/MS determination of copanlisib, a novel PI3K inhibitor, in mouse plasma and its application to a pharmacokinetic study in mice. Biomed Chromatogr. 2019 Apr;33(4):e4460. doi: 10.1002/bmc.4460. Epub 2019 Jan 7. doi: 10.1007/s00277-018-3547-7. Epub 2018 Nov 15. doi: 10.2147/DDDT.S142406. eCollection 2018. Review.
合成参考文献
摘要:Preliminary results of a phase II study of single agent Bay 80-6946, a Novel PI3K inhibitor, in patients with relapsed/refractory, indolent or aggressive lymphoma. Clin Adv Hematol Oncol. 2014 Feb;12(2 Suppl 5):14–6. 参考文献:10.1007/s40487-021-00161-5 摘要:Rodgers TD, Casulo C, Boissard F, Launonen A, Parreira J, Cartron G. Early Relapse in First-Line Follicular Lymphoma: A Review of the Clinical Implications and Available Mitigation and Management Strategies. Oncology and Therapy. 2021 Jul 28;9(2):329–46. doi: 10.1007/s40487-021-00161-5.