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-12054512-B2 优先权日:2017-11-10 标 题 :Sting modulator compounds, and methods of making and using 发明人:VYSKOCIL STEPAN; CIAVARRI JEFFREY; CULLIS COURTNEY; ENGLAND DYLAN BRADLEY; GOULD ALEXANDRA E; GREENSPAN PAUL; HU YONGBO; LANGSTON STEVEN; LI GANG; MIZUTANI HIROTAKE; OKANIWA MASANORI 权利人:TAKEDA PHARMACEUTICALS CO 摘要:The present disclosure provides STING modulators/agonists, and methods of synthesis and methods for using for the prophylaxis or treatment of cancer and other STING-related diseases.The present disclosure relates to a compound represented by the Formula (I):wherein each symbol is as defined in the description, or a pharmaceutically acceptable salt thereof.
专利号:US-12180188-B2 优先权日:2020-05-19 标题:Antifibrotic compounds and related methods 发明人:STEFANOVIC BRANKO; NEFZI ADEL 权利人:UNIV FLORIDA STATE RES FOUND; THE FLORIDA INTERNATIONAL UNIV BOARD OF TRUSTEES 摘要:This discloses that compounds of Formula 1 have antifibrotic properties. In particular, this discloses a pharmaceutical composition including one or more compounds of Formula 1 and methods of using compounds of Formula 1 in fibrosis treatment and inhibiting type 1 collagen synthesis.
专利号:US-7732436-B2 优先权日:2003-05-19 标 题 :Preparation of hymenialdisine derivatives and use thereof 发明人:TEPE JETZE J 权利人:UNIV MICHIGAN STATE 摘要:The synthesis and biological activity of indoloazepines and acid amine salts thereof which are structurally related to naturally-occurring hymenialdisine is disclosed. Naturally-occurring hymenialdisine obtained from the sponge is a potent inhibitor of production of cytokines interleukin-2 (IL-2) and tumor necrosis factor-α (TNF-α). The chemically-synthesized indoloazepines of the invention also inhibit production of IL-2 and TNF-α. The indoloazepines are useful for treating inflammatory diseases, particularly diseases associated with kinases NF-κB or GSK-3β activation or NF-κB activated gene expression products. The indoloazepines are useful for the treatment of cancer by the inhibition of kinases CHK1 and CHK2.
专利号:US-2023021879-A1 优先权日:2019-11-27 标 题:Synthesis of 3 -rna oligonucleotides
专利号:KR-20000067196-A 优先权日:1999-04-24 标 题:The synthesis of benzimidazole type antifungals and dantib acterial agents
摘要:Irudayanathan, F. M.; Lee, S., Science of Synthesis Knowledge Updates, (2019) 2, 23. 参考文献:10.1016/j.bmcl.2009.11.090 摘要:Potter AJ, Ray S, Gueritz L, Nunns CL, Bryant CJ, Scrace SF, Matassova N, Baker L, Dokurno P, Robinson DA, Surgenor AE, Davis B, Murray JB, Richardson CM, Moore JD. Structure-guided design of alpha-amino acid-derived Pin1 inhibitors. Bioorg Med Chem Lett. 2010 Jan 15;20(2):586–90. doi: 10.1016/j.bmcl.2009.11.090.