4-(叠氮甲基)苯甲腈置于palladium On Activated Charcoal Sodium Tetrahydroborate,氢气体系中,用 四氢呋喃 用作溶剂,20.0~35.0 °C,310.26 Kpa 条件下,反应 28.0H,反应生成1-(N-Boc-氨基甲基)-4-(氨基甲基)苯 参考文献:Unexpected Enhancement Of Thrombin Inhibitor Potency With O-Aminoalkylbenzylamides In The P1 Position 标题:Unexpected Enhancement Of Thrombin Inhibitor Potency With O-Aminoalkylbenzylamides In The P1 Position 摘要:Thrombin Inhibitors Incorporating O-Aminoalkylbenzylamides In The P1 Position Were Designed,Synthesized And Found To Have Enhanced Potency And Selectivity In Several Different Structural Classes. X-Ray Crystallographic Analysis Of Compound 24 Bound In The Alpha-Thrombin-Hirugen Complex Provides An Explanation For These Unanticipated Results. (C) 2003 Elsevier Ltd. All Rights Reserved. Doi:10.1016/s0960-894X(03)00732-7
专利信息
专利号:US-2025129021-A1 优先权日:2023-09-19 标 题:Small molecule protein synthesis modulators 发明人:GYGI DAVID; BAHMANYAR SOGOLE SAMI; HAMANN LAWRENCE 权利人:INTERDICT BIO INC 摘要:The present disclosure provides compounds of the formulae herein (e.g., Formula (I), Formula (V)), and pharmaceutically acceptable salts thereof, which are useful for modulating protein synthesis (e.g., modulating synthesis of BCL-2, MYC, CCND1, MCL-1, ALK, KRAS-G12D). The present disclosure also provides pharmaceutical compositions and kits comprising the compounds, or pharmaceutically acceptable salts thereof, and methods of treating or preventing diseases or disorders (e.g., diseases or disorders associated with BCL-2, MYC, CCND1, MCL-1, ALK, KRAS-G12D) by administering to a subject in need thereof the compounds, or pharmaceutically acceptable salts thereof, or pharmaceutical compositions thereof.
专利号:WO-2024255798-A1 优先权日:2023-06-14 标题:Fluorescent probe compound for tumor targeting imaging, and synthesis method therefor and use thereof 发明人:WANG LEI; ZHANG YINING; LUO ZIJUN; GUO LIXIAO; LIU YI; GUO HUICAI 权利人:UNIV HEBEI MEDICAL 摘要:The present invention relates to a fluorescent probe compound for tumor targeting imaging, and a synthesis method therefor and the use thereof. For the compound, an anti-tumor drug having a pyrrolo[2,3-d]pyrimidine core structure is used as a targeting ligand for the first time, and a fluorescent dye is linked after modification is performed by a linker molecule. The compound has a structure as represented by formula I. The compound has a high affinity and selectivity for targeting tumor cells expressing a target receptor, can be used in the positioning, qualitative and quantitative analysis of related experiments such as in-vivo and in-vitro tracing, receptor affinity and action mechanism of the tumor cells expressing the target receptor, and is highly specific, sensitive and intuitive. The fluorescent probe of the present invention can be rapidly cleared from normal tissue and can remain at a tumor site for a long time, so as to achieve the effect of in vivo diagnosis. The fluorescent probe has certain clinical application prospects and can be used in clinical intraoperative navigation.
专利号:WO-2025068371-A1 优先权日:2023-09-28 标 题:Inhibitors of the proprotein convertase furin, methods of production thereof and use 发明人:STEINMETZER TORSTEN; LANGE ROMAN WERNER; BOLLER CHARLOTTE; FRIEBERTSHÄUSER EVA; BLOCH KONSTANTIN 权利人:PHILIPPS UNIV MARBURG 摘要:The invention relates to novel inhibitors of the serine protease furin and to related furin-like proprotein convertases according to claim 1, and to methods of synthesis thereof and to use for production of medicaments for treatment of furin-dependent viral and bacterial infection diseases, and other disorders involving furin, such as cystic fibrosis, cancer, osteoarthritis, hypertension, and neurodegenerative disorders.
参考标题:Synthesis Of Short Cationic Antimicrobial Peptidomimetics Containing Arginine Analogues 作者:Leonardo Baldassarre,Francesco Pinnen,Catia Cornacchia,Erika Fornasari,Luigina Cellini,Marina Baffoni,Ivana Cacciatore |发布日期:2012.9 摘要:Worldwide Efforts Are Underway To Develop New Antimicrobial Agents Against Bacterial Resistance. To Identify New Compounds With A Good Antimicrobial Profile, We Designed And Synthesized Two Series Of Small Cationic Antimicrobial Peptidomimetics (1-8) Containing Unusual Arginine Mimetics (To Introduce Cationic Charges) And Several Aromatic Amino Acids (Bulky Moieties To Improve Lipophilicity). Both
合成参考文献
摘要:Sato, S.; Furukawa, N., Science of Synthesis, (2005) 18, 898.