CAS: 1032754-93-0; (S)-1-(4-((2-(2-Aminopyrimidin-5-yl)-7-Methyl-4-Morpholinothieno[3,2-D]Pyrimidin-6-yl)Methyl)Piperazin-1-yl)-2-Hydroxypropan-1-One

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CAS号79-33-4 L-(+)-乳酸 | CAS号955979-02-9 Thieno[3,2-d]py... | CAS号35265-88-4 4-(2-氯-7-甲基噻吩并[...

📜Tert-Butyl 4-((2-Chloro-7-Methyl-4-Morpholinothieno[3,2-D]Pyrimidin-6-yl)Methyl)Piperazine-1-Carboxylate置于盐酸,Bis-Triphenylphosphine-Palladium(II) Chloride,Sodium Carbonate,N,N-二异丙基乙胺,Methanaminium,N-[(Dimethylamino)(3H-1,2,3-Triazolo[4,5-B]Pyridin-3-Yloxy)Methylene]-N-Methyl-,Hexafluorophosphate(1-)体系中,用 1,4-二氧六环,水,N,N-二甲基甲酰胺,乙腈 用作溶剂,化学反应 3.2H,反应生成(S)-1-[4-[[2-(2-氨基嘧啶-5-基)-7-甲基-4-(吗啉-4-基)噻吩并[3,2-D]嘧啶-6-基]甲基]哌嗪-1-基]-2-羟基丙-1-酮
参考文献:发现有效,选择性和口服的i类磷脂酰肌醇3-激酶(pi3K)/雷帕霉素(mtor)激酶抑制剂(gdc-0980)的哺乳动物靶标
标题:发现有效,选择性和口服的i类磷脂酰肌醇3-激酶(pi3K)/雷帕霉素(mtor)激酶抑制剂(gdc-0980)的哺乳动物靶标
摘要:描述了发现2(gdc-0980),I类pi3K和mtor激酶抑制剂的肿瘤学适应症.Mtor抑制作用主要是通过将1中的吲唑替换为2-氨基嘧啶而添加到i类pi3K抑制剂1(gdc-0941)支架上.这种取代也增加了化合物的微粒体稳定性和游离分数,这通过对另外相同的分子进行成对比较来证明.详细强调的是先进化合物4的类似物,旨在改善溶解度,导致2.该化合物对具有ic 50的pi3K I类同工型均有效pi3Kα,β,δ和γ分别为5,27,7和14 Nm的s抑制mtor,K I为17 Nm,但与包括pikk家族中的其他激酶在内的大量激酶相比具有很高的选择性.基于细胞效力,小鼠中的低清除率和高游离分数,当口服剂量低至1 Mg / Kg时,2在小鼠异种移植物中显示出显着的功效,目前正处于癌症的i期临床试验中.
Doi:10.1021/jm2009327

专利信息

专利号:US-12391691-B2
优先权日:2018-11-16
标题:Synthesis of key intermediate of KRAS G12C inhibitor compound
发明人：PARSONS ANDREW THOMAS; COCHRAN BRIAN MCNEIL; POWAZINIK IV WILLIAM; CAPORINI MARC ANTHONY
权利人:AMGEN INC
摘要:The present invention relates to an improved, efficient, scalable process to prepare intermediate compounds, such as compound 5M, having the structure n nuseful for the synthesis of compounds that target KRAS G12C mutations, such as

专利号:US-2025206736-A1
优先权日:2019-11-14
标题 :Synthesis of kras g12c inhibitor compound
发明人：CORBETT MICHAEL THOMAS; CAILLE SEBASTIEN
权利人:AMGEN INC
摘要:The present disclosure relates to an improved, efficient, scalable process to prepare intermediate compounds, such as 2-isopropyl-4-methylpyridin-3-amine, useful for the synthesis of compounds, such as Compound 9, for the treatment of KRAS G12C mutated cancers.

专利号:WO-2025128098-A1
优先权日:2023-12-13
标 题 :Solid oral dosage forms, kits, and methods of using the same
发明人：LI YING; LANGER ROBERT; TRAVERSO CARLO
权利人:MASSACHUSETTS INST TECHNOLOGY; BRIGHAM & WOMENS HOSPITAL INC
摘要:Provided herein are solid oral dosage forms, methods, and kits useful, e.g, for the extension of the residence time of active pharmaceutical agents in vivo by the synthesis of a polymer in situ in a subject. In particular, the solid oral dosage forms, methods, and kits disclosed herein are particularly useful for drugs that require more than once daily administration (e.g, drugs that have short half-lives).

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-2023192682-A1
优先权日:2019-11-14
标题:Improved synthesis of kras g12c inhibitor compound

专利号:US-2023192681-A1
优先权日:2019-11-14
标 题 :Improved synthesis of kras g12c inhibitor compound