CAS: 1029712-80-8; 2-Fluoro-N-Methyl-4-(7-(Quinolin-6-Ylmethyl)Imidazo[1,2-B][1,2,4]Triazin-2-yl)Benzamide

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CAS号74-89-5 氨基甲烷

2-Fluoro-4-(7-(Quinolin-6-Ylmethyl)Imidazo[1,2-B][1,2,4]Triazin-2-yl)Benzonitrile置于盐酸,Benzotriazol-1-Yloxyl-Tris-(Pyrrolidino)-Phosphonium Hexafluorophosphate,水,三乙胺体系中,用 四氢呋喃,N,N-二甲基甲酰胺 用作溶剂,化学反应 19.0H,反应生成卡马替尼
参考文献:Absorption,Distribution,Metabolism,And Excretion Of Capmatinib (Inc280) In Healthy Male Volunteers And In Vitro Aldehyde Oxidase Phenotyping Of The Major Metabolite
标题:Absorption,Distribution,Metabolism,And Excretion Of Capmatinib (Inc280) In Healthy Male Volunteers And In Vitro Aldehyde Oxidase Phenotyping Of The Major Metabolite
摘要:卡马替尼 (Inc280) 是一种高度选择性和有效的 Met 受体酪氨酸激酶抑制剂,已在携带 Met 外显子 14 跳跃突变的晚期非小细胞肺癌患者中表现出具有临床意义的疗效和可控的安全性.我们研究了六名健康男性志愿者单次口服剂量 600 Mg 14C 标记的卡马替尼后卡马替尼的吸收,分布,代谢和排泄.测定质量平衡,血液和血浆放射性,血浆卡马替尼浓度以及血浆,尿液和粪便中的代谢物谱.使用质谱法阐明代谢物结构并与参考化合物进行比较.母体化合物占血浆中大部分放射性(42.9%+/-2.9%).口服吸收程度估计为49.6%;血浆中卡马替尼的 Cmax置于2 小时达到(达到 Cmax 的中位时间).卡马替尼在血浆中的表观平均消除半衰期为 7.84 小时.卡马替尼在终末期的表观分布体积为中等到高(几何平均值 473 L).代谢反应涉及内酰胺形成,羟基化,N-脱烷基化,羧酸形成,氢化,N-氧化,葡萄糖醛酸化及其组合. M16 是血浆,尿液和粪便中最丰富的代谢物,是通过内酰胺形成而形成的.吸收的卡马替尼主要通过代谢以及随后的胆汁/粪便和肾脏排泄消除. 7天后放射性物质排出完毕. Cyp表型分析表明cyp3A是参与肝微粒体代谢的主要细胞色素p450酶亚家族,肝细胞质的体外研究表明m16的形成主要由醛氧化酶催化. 意义声明 卡马替尼的吸收,分布,代谢和排泄表明,口服给药后卡马替尼具有显着的全身利用度.它还被广泛代谢并大部分分布到外周组织.平均消除半衰期为 7.84 小时.最丰富的代谢物 M16 是由胞质醛氧化酶催化的咪唑三嗪酮形成而形成的.相关分析,特异性抑制和重组酶表型分析表明,Cyp3A 是参与 [14C]Capmatinib 肝微粒体代谢的主要酶亚家族.
Doi:10.1124/dmd.119.090324

专利信息

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:NO-327896-B1
优先权日:1999-01-19
标 题 :Tricyclic benzodiazepines, pharmaceutical composition, use of the compounds and intermediates useful in the synthesis of the compounds

专利号:US-2024066133-A1
优先权日:2020-03-06
标 题 :Therapeutic agents and conjugates thereof
发明人：SONG YUNTAO; LI ANRONG; LI HUI; LI XIANFENG; YANG JUNBAO
权利人:BEIJING XUANYI PHARMASCIENCES CO LTD
摘要:The present disclosure provides a class of conjugates of general formula (X), a class of TLR9 agonist derivatives, such as formula (I), (XX), and (XXI), certain diastereomers of STING agonists, a class of STING agonist derivatives, such as formula (XXVIV), a class of heterocyclic compounds of general formula (II), a class of heterocyclic compounds of general formula (III), as defined herein. A 1 , A 2 , T, Z 1 , Z 2 , Z 3 , b 1 , and b 2 , in formula (X) are defined herein. The conjugate provides unique properties that are based upon the properties of the therapeutic agents that are part of the conjugate. Also provided are methods of synthesis and use of compounds.

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

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.