CAS: 1108743-60-7; N-(5-(3,5-Difluorobenzyl)-1H-Indazol-3-yl)-4-(4-Methylpiperazin-1-yl)-2-((Tetrahydro-2H-Pyran-4-yl)Amino)Benzamide

上下游产品

2-Amino-N-[5-(3,5-Difluorobenzyl)-1H-Indazol-3-Yl]-4-(4-Methylpiperazin-1-yl)Benzamide 1108743-96-9
N-[5-(3,5-Difluorobenzyl)-1H-Indazol-3-Yl]-4-(4-Methylpiperazin-1-yl)-2-[(Tetrahydropyran-4-yl)-(2,2,2-Trifluoroacetyl)Amino]Benzamide 1108745-38-5

5-(3,5-二氟苄基)-2-氟苯腈置于一水合肼,N,N-二异丙基乙胺体系中,用 四氢呋喃,正丁醇 用作溶剂,化学反应 4.0H,反应生成恩曲替尼
参考文献:Entrectinib的发现:一种新型的3-氨基吲唑作为一种强力的间变性淋巴瘤激酶(alk),C-Ros癌基因1激酶(ros1)和pan-Tropomyosin受体激酶(pan-Trks)抑制剂
标题:Entrectinib的发现:一种新型的3-氨基吲唑作为一种强力的间变性淋巴瘤激酶(alk),C-Ros癌基因1激酶(ros1)和pan-Tropomyosin受体激酶(pan-Trks)抑制剂
摘要:间变性淋巴瘤激酶(alk)是负责不同肿瘤类型发展的受体酪氨酸激酶.尽管2011年批准了首个alk抑制剂克唑替尼(xalkori)的卓越临床活性,但耐药性突变和脑转移瘤的出现经常导致患者复发.在我们的alk药物发现计划中,我们鉴定了化合物1,这是一种在生化和细胞分析中对alk具有活性的新型3-氨基吲唑.其优化导致了化合物2(entrectinib)是一种对alk依赖的细胞系具有活性的有效口服alk抑制剂,可有效穿透不同动物物种的血脑屏障(bbb),并且在体内异种移植模型中非常有效.此外,恩替替尼在最近被发现在几种肿瘤类型中组成性激活的紧密相关的酪氨酸激酶ros1和trks上具有严格的作用.Entrectinib目前正在进行i / Ii期临床试验,用于治疗受alk-,Ros1-和trk阳性肿瘤影响的患者.
Doi:10.1021/acs.Jmedchem.6B00064

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-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-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:US-2024208898-A1
优先权日:2021-03-25
标 题 :Enamine n-oxides: synthesis and application to hypoxia-responsive prodrugs and imaging agents
发明人：KIM JUSTIN; KANG DAHYE; CHEUNG SHELDON T
权利人:DANA FARBER CANCER INST INC
摘要:Disclosed are compounds and pharmaceutically acceptable salts and stereoisomers thereof that are suitable for diagnosis and the treatment of diseases and disorders characterized by, associate with or which exhibit tissue hypoxia, such as, for example, solid tumors. Also disclosed are pharmaceutical compositions containing same, and methods of making and using the compounds.

专利号:WO-2025137620-A1
优先权日:2023-12-21
标题:Methods for high quality and high accuracy methylation sequencing
发明人：KENNEDY ANDREW
权利人:GUARDANT HEALTH INC
摘要:Provided herein are methods and compositions for calibrating one or more base calling metrics in a sequencing by synthesis reaction, and for calling at least a portion of nucleobases in a converted region of a DNA molecule using the one or more calibrated base calling metrics. Provided herein are also methods for determining the likelihood that a subject has a disease or condition, such as cancer.

专利号:JP-2024512568-A
优先权日:2021-03-25
标 题:Enamine N-oxide: synthesis and application of hypoxia-responsive prodrugs and contrast agents