CAS: 1197953-54-0; (2-((5-Chloro-2-((2-Methoxy-4-(4-(4-Methylpiperazin-1-yl)Piperidin-1-yl)Phenyl)Amino)Pyrimidin-4-yl)Amino)Phenyl)Dimethylphosphine Oxide

上下游产品

(2-((2,5-dichloropyrimidin-4-yl)amino)phenyl)dimethyl phosphine oxide 2-iodophenylamine (2-aminophenyl)dimethyl phosphorus oxide 4-fluoro-2-methoxy-1-nitrobenzene

(2-氨基苯基)二甲基氧化膦置于盐酸,四丁基硫酸氢铵,Potassium Carbonate体系中,用 乙醇,乙二醇甲醚,N,N-二甲基甲酰胺 用作溶剂,化学反应 14.0H,反应生成布格替尼
参考文献:Brigatinib(ap26113)的发现,它是间变性淋巴瘤激酶中一种含磷氧化物的强效口服活性抑制剂
标题:Brigatinib(ap26113)的发现,它是间变性淋巴瘤激酶中一种含磷氧化物的强效口服活性抑制剂
摘要:在棘皮动物微管相关蛋白样4(eml4)-间变性淋巴瘤激酶阳性(alk +)非小细胞肺癌(nsclc)的治疗中,Alk激酶结构域内的继发突变已成为对二者的主要耐药机制第一代和第二代alk抑制剂.该报告描述了一系列基于2,4-二芳基氨基嘧啶的有效和选择性alk抑制剂的设计和合成,这些抑制剂最终可鉴定出临床研究候选药物brigatinib.Brigatinib的独特结构特征是氧化膦,这是一种被忽视但新颖的氢键受体,除了具有非常好的adme性能外,还可以提高效价和选择性.Brigatinib展示了低纳摩尔ic 50在基于酶的生化和基于细胞的活力测定中均针对天然alk和所有经过测试的临床相关alk突变体,并在小鼠的多种alk +异种移植物中证明了功效,包括karpas-299(间变性大细胞淋巴瘤[alcl])和h3122( Nsclc).Brigatinib代表了迄今为止临床上最先进的含氧化膦药物候选
Doi:10.1021/acs.Jmedchem.6B00306

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-2022118094-A1
优先权日:2019-02-21
标题:Synthesis of biomimetic cell wall structure
发明人：WANG YONG; SHI PENG
权利人:PENN STATE RES FOUND
摘要:The present invention relates generally to methods of generating a biomimetic cell wall (BCW) on a target surface, compositions comprising the BCW, and methods of use of the compositions, including biomedical applications of the BCW coated compositions.

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-11406709-B2
优先权日:2014-09-15
标 题 :Therapeutic and research application of PDCL3
发明人：RAHIMI NADER
权利人:UNIV BOSTON
摘要:Described herein are novel compositions comprising, for example, PDCL3 polypeptides having VEGFR-2 inhibitory activity, inhibitory PDCL3 antibodies and PDCL3-binding fragments thereof, or PDCL3 inhibitory nucleic acid molecules, and methods of their use in anti-angiogenesis and anti-tumor proliferation and invasiveness therapies, such as the treatment of cancer, as well as the treatment of those vascular diseases where pathological angiogenesis plays a role, such as in carotid artery disease, macular degeneration, and plaque neovascularization. Also described herein are novel compositions comprising engineered PDCL3 polypeptides having enhanced chaperone activity, recombinant cells comprising such engineered PDCL3 polypeptides having enhanced chaperone activity, and methods thereof for therapeutic protein production and in vitro protein synthesis.

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-113336703-B
优先权日:2021-05-17
标 题:Synthesis of 1,3,4,5-tetrasubstituted 1H-pyrazole derivatives