CAS: 926037-48-1; 4-Methyl-N-(3-(4-Methyl-1H-Imidazol-1-yl)-5-(Trifluoromethyl)Phenyl)-3-((4-(Pyrazin-2-yl)Pyrimidin-2-yl)Amino)Benzamide

📜3-乙酰胺基-4甲基苯甲酸置于氯化亚砜,硝酸,Sodium Hydroxide体系中,用 乙醇,二氯甲烷,水 作为反应溶剂,化学反应 64.0H,反应生成 拉多替尼
参考文献:一种拉多替尼的高收率合成方法
标题:一种拉多替尼的高收率合成方法
摘要:本发明公开了一种拉多替尼的高收率合成方法,涉及药物有机合成技术领域,以3‑乙酰胺基‑4‑甲基苯甲酸作为起始原料,与3‑(4‑甲基‑1H‑咪唑‑1‑基)‑5‑三氟甲基苯胺经酰胺缩合反应得到中间体i,中间体i与单氰胺经加成反应得到中间体ii,中间体ii与二甲氨基‑1‑(3‑吡嗪基)‑2‑丙烯‑1‑酮经闭环反应得到拉多替尼;本发明在简化反应操作的同时降低成本投入,减少三废产生量,提高起始原料和中间体的转化率,所制拉多替尼的总收率能够达到79%以上.

专利信息

专利号:US-2022233673-A1
优先权日:2019-06-04
标 题:METHODS OF PRODUCING SHIGA TOXIN B-SUBUNIT (STxB) MONOMERS AND OLIGOMERS, AND USES THEREOF
发明人：BILLET ANNE; SCHMIDT FRÉDÉRIC; JOHANNES LUDGER; SERVENT DENIS; MOURIER GILLES; TARTOUR ÉRIC; KAY MICHAEL; FULCHER JAMES M
权利人:INST CURIE; CENTRE NAT RECH SCIENT; INST NAT SANTE RECH MED; COMMISSARIAT A LENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES CEA; APHP ASSIST PUBLIQUE HOPITAUX DE PARIS; UNIV PARIS; UNIV OF UTAH RESEARCH FOUDATION; UNIV UTAH RES FOUND
摘要:A method of producing a monomer of a Shiga toxin B-subunit (STxB) protein or of a variant thereof by peptide chemical synthesis, as well as to a method of producing a pentamer of the STxB protein or of the variant thereof. The methods are particularly advantageous as they overcome major issues typically observed in peptide chemical synthesis, including solubility and purity issues.

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.

专利号:CN-115838697-A
优先权日:2022-10-13
标 题:Imine reductase mutants and their application in the synthesis of chiral intermediates of larotrectinib

专利号:WO-2024115549-A1
优先权日:2022-11-30
标题:Aryl- and heteroaryl-sulfonamide derivatives as ccr8 modulators
发明人：AISSAOUI HAMED; CORMINBOEUF OLIVIER; DIETHELM STEFAN; REMEN LUBOS; RICHARD-BILDSTEIN SYLVIA
权利人:IDORSIA PHARMACEUTICALS LTD
摘要:The present invention relates to compounds of Formula (I), their synthesis and use as CCR8 receptor modulators in medicine.