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CAS号118289-16-0 2-溴吡啶-4-甲烷醇 | CAS号383426-36-6 2-bromo-pyridin... | CAS号58530-53-3 2,4-二溴吡啶 | CAS号68-12-2 N,N-二甲基甲酰胺 | CAS号865449-19-0 2-bromo-4-(dibr... | CAS号4926-28-7 2-溴-4-甲基吡啶 | CAS号695-34-1 2-氨基-4-甲基吡啶 | CAS号461-87-0 2-氟-4-甲基吡啶 | CAS号66572-56-3 2-溴吡啶-4-羧酸 | CAS号88046-02-0 2-溴-4-(1-哌啶甲基)吡啶 | CAS号1289386-60-2 2-溴-N-(1-甲基乙基)-... | CAS号118289-16-0 2-溴吡啶-4-甲烷醇 | CAS号83004-14-2 2-溴-4-(溴甲基)吡啶 | CAS号474799-53-6 methyl 2-[(2-br...2-溴-4-甲基吡啶置于potassium Permanganate,Lithium Aluminium Tetrahydride,磷酸,氯甲酸乙酯,二甲基亚砜,三乙胺,N,N'-二环己基碳二亚胺体系中,用 水 用作溶剂,化学反应 3.0H,反应生成2-溴吡啶-4-甲醛
参考文献:新型1,4-二氢吡啶类钙拮抗剂.I.4-(取代的吡啶基)-1,4-二氢吡啶衍生物的合成和降血压活性.
标题:新型1,4-二氢吡啶类钙拮抗剂.I.4-(取代的吡啶基)-1,4-二氢吡啶衍生物的合成和降血压活性.
摘要:合成了一系列4-(取代的吡啶基)-1,4-二氢吡啶衍生物,并研究了它们的降压作用.几种化合物,2-(n-苄基-N-甲基氨基)乙基甲基1,4-二氢-2,6-二甲基-4-(3-硝基-2-吡啶基)-3,5-吡啶二甲酸(2B),4-(4-硝基-2-吡啶基)类似物(2G),4-(3-三氟甲基-2-吡啶基)类似物(2C),4-(2-三氟甲基-3-吡啶基)类似物(3E),4-发现(4-氰基-2-吡啶基)类似物(2E),4-(2-氰基-3-吡啶基)类似物(3D)和4-(6-溴-2-吡啶基)类似物(2I)具有与尼卡地平类似的降压活动;特别是2C和3E的持续时间约为尼卡地平的两倍,而2E具有在所有合成衍生物中最有效的降压活性.
Doi:10.1248/cpb.38.2446
专利信息
专利号:US-2008242866-A1
优先权日:2007-03-30
标 题 :Synthesis of anthranilamides
发明人:SCHMEES NORBERT; PETROV ORLIN
权利人:SCHMEES NORBERT; PETROV ORLIN
摘要:The present invention relates to a novel method of preparing anthranilamides of formula I: n n n n n n n n n n in which R 1 , R 2 , R 3 , A, E, Q, X, and W are defined in the claims, to a novel intermediate compound, and to the use of said novel intermediate compound for the preparation of said anthranilamides of formula I.
专利号:US-2025222120-A1
优先权日:2024-01-09
标题 :Synthesis of novel small molecule carm1 degraders, compounds formed thereby, and pharmaceutical compositions containing them
发明人:TANG WEIPING; XU WEI; XIE HAIBO; BACABAC MEGAN
权利人:WISCONSIN ALUMNI RES FOUND
摘要:Provided herein are CARM1 PROTACs comprising a binding molecule of CARM1 with an optimized linker attached to an E3 ubiquitin ligase ligand that recruits the E3 ubiquitin ligase to CARM1. The PROTACs find use, e.g., for selectively targeted degradation of CARM1 protein in cancer cells. Also provided herein are compositions comprising the PROTACs, as well as methods of using the PROTACs.
专利号:WO-2023091726-A1
优先权日:2021-11-18
标题:Inhibitors of cyclin‑dependent kinase 12 (cdk12)
发明人:BENOIT GUILLAUME; CARULLI JOHN; CHEN FEI; CHUAQUI CLAUDIO; CIBLAT STEPHANE; COOPER ELLIOT; DAGENAIS ROBIN; HU SHANHU; KABRO ANZHELIKA; LAPLACA DEREK; MARINEAU JASON; MOEBIUS DAVID; MOON DIANE; SOLODININ ANDREI; WHITMORE KENNETH
权利人:SYROS PHARMACEUTICALS INC
摘要:The present invention provides chemical compounds that inhibit one or more families of kinases (e.g., serine/threonine kinases, including one or more of the families of CDK proteins, and in particular, CDK12). More specifically, the present invention provides CDK12 inhibitors, of formula (I), pharmaceutically acceptable salts and isotopically labeled derivatives thereof, pharmaceutical compositions containing the compounds/inhibitors, and methods of their synthesis and use in treating proliferative diseases (e.g., a bladder cancer, a breast cancer, Ewing's sarcoma, a gastric cancer, a gastrointestinal cancer, a hematologic cancer, a lung cancer (e.g., small cell lung cancer (SCLC)), an ovarian cancer (e.g., a high grade serous ovarian cancer), a pancreatic cancer (e.g., pancreatic ductal adenocarcinoma (PDAC)), a brain cancer (e.g., glioblastoma), or a prostate cancer), alone or in combination with a second therapeutic agent. The proliferative disease can be a cancer, benign neoplasm, or pathologic angiogenesis, and any of the therapeutic methods or uses described herein can include a step of diagnosing the patient's disease. In other embodiments of the invention, the compositions described herein (e.g., the compounds, pharmaceutical compositions, and kits containing them) are used for the treatment of myotonic dystrophy (type 1 or type 2).
专利号:EP-3070087-B1
优先权日:2011-08-05
标题 :Intermediates for the synthesis of cyclic p1 linkers as factor xia inhibitors
专利号:EP-3070087-A1
优先权日:2011-08-05
标 题 :Intermediates for the synthesis of cyclic p1 linkers as factor xia inhibitors
专利号:ES-2733096-T3
优先权日:2011-08-05
标题:Intermediaries for the synthesis of cyclic P1 linkers as XIA factor inhibitors