CAS: 212141-54-3; N-(4-Chlorophenyl)-4-(Pyridin-4-Ylmethyl)Phthalazin-1-Amine

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CAS号106-47-8 对氯苯胺 | CAS号107558-48-5 4-(4-吡啶甲基)-1(2H)-酞嗪酮 | CAS号87-41-2 苯酞 | CAS号101094-85-3 瓦他拉尼中间体 | CAS号67592-40-9 3-羟基-2-(吡啶-4-基)茚-1-酮 | CAS号20265-96-7 对氯苯胺盐酸盐

📜苯酞置于sodium Methylate,Phosphorus Pentoxide,三乙胺盐酸盐,一水合肼体系中,用 甲醇 用作溶剂,化学反应 12.5H,反应生成瓦他拉尼碱
参考文献:新的苯胺酞嗪作为有效的和口服吸收非常好的vegf受体酪氨酸激酶抑制剂,可用作肿瘤驱动的血管生成的拮抗剂.
标题:新的苯胺酞嗪作为有效的和口服吸收非常好的vegf受体酪氨酸激酶抑制剂,可用作肿瘤驱动的血管生成的拮抗剂.
摘要:要使任何实体瘤长到足以引起威胁生命的疾病,新血管的萌发或血管新生都是必不可少的.血管内皮生长因子(vegf)是肿瘤诱导的血管生成的关键启动子之一.Vegf受体,酪氨酸激酶flt-1和kdr在血管内皮细胞上表达,并在被vegf激活后启动血管生成.1-Anilino-(4-吡啶基甲基)-酞嗪,例如cgp 79787D(或ptk787 / Zk222584),可逆地抑制flt-1和kdr,Ic(50)值<0.1 Microm.Cgp 79787D还可以在异位表达kdr受体的cho细胞中阻断vegf诱导的受体自磷酸化(ed(50)= 34 Nm).与相关受体酪氨酸激酶pdgf-R和c-Kit相比,对1-苯胺基部分的修饰提供了对vegf受体酪氨酸激酶flt-1和kdr具有更高选择性的衍生物.由于这些1-苯胺基-(4-吡啶基甲基)酞嗪口服吸收非常好,因此这些化合物可用于进一步的分析,并可作为临床评估的候选药物.
Doi:10.1021/jm9909443

专利信息

专利号:US-12383499-B2
优先权日:2018-01-01
标题:Scale up synthesis of silicasome nanocarriers
发明人：NEL ANDRE E; MENG HUAN; LIU XIANGSHENG
权利人:UNIV CALIFORNIA
摘要:In order to facilitate the approval and commercialization of silicasome drug delivery systems (e.g. irinotecan silicasomes) it is necessary to scale up synthesis of the drug-loaded silicasomes. In this regard, it was discovered that the synthesis protocols used for laboratory synthesis of drug-loaded silicasomes (e.g., 500 mg/batch) do not scale to large scale silicasome production, because the resulting products were too heterogeneous for use as pharmaceuticals. Accordingly, new methods are provided herein that effectively afford the large-scale production of mesoporous silica nanoparticles (MSNPs) and lipid bilayer coated MSNPs (silicasomes).

专利号:US-10973847-B2
优先权日:2017-06-30
标题 :Core-to-surface polymerization for the synthesis of star polymers and uses thereof
发明人：JOHNSON JEREMIAH A; GOLDER MATTHEW R
权利人:MASSACHUSETTS INST TECHNOLOGY
摘要:Disclosed are methods, compositions, reagents, systems, and kits to prepare star polymers, as well as compositions and uses thereof. Various embodiments show that synthesis of these polymers contain low metal concentration to provide polymers for diverse biomedical applications including in vivo applications.

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:US-2017283878-A1
优先权日:2015-12-11
标题:Modulation of globoseries glycosphingolipid synthesis and cancer biomarkers
发明人：WONG CHI-HUEY; WU CHUNG-YI; CHEUNG SARAH K C; CHUANG PO-KAI; HSU TSUI-LING
权利人:ACADEMIA SINICA
摘要:The present disclosure relates to methods and compositions which can modulate the globoseries glycosphingolipid synthesis. Particularly, the present disclosure is directed to glycoenzyme inhibitor compound and compositions and methods of use thereof that can modulate the synthesis of globoseries glycosphingolipid SSEA-3/SSEA-4/GloboH in the biosynthetic pathway; particularly, the glycoenzyme inhibitors target the alpha-4GalT; beta-4GalNAcT-I; or beta-3GalT-V enzymes in the globoseries synthetic pathway. Additionally, the present disclosure is also directed to vaccines, antibodies, and/or immunogenic conjugate compositions targeting the SSEA-3/SSEA-4/GLOBO H associated epitopes (natural and modified) which elicit antibodies and/or binding fragment production useful for modulating the globoseries glycosphingolipid synthesis. Moreover, the present disclosure is also directed to the method of using the compositions described herein for the treatment or detection of hyperproliferative diseases and/or conditions. Furthermore, the instant disclosure also relates to cancer stem cell biomarkers for diagnostic and therapeutic uses.

专利号:US-2025206743-A1
优先权日:2022-03-25
标 题:Tyk2 inhibitor synthesis and intermediates thereof
发明人：MASSE CRAIG E; PHADKE AVINASH S; LAWSON JON P; LEVY STUART; YANG XIAOWEI; WU GUISHENG; FAN SHUFENG
权利人:TAKEDA PHARMACEUTICALS CO
摘要:Described herein are methods of synthesis of a tyrosine-protein kinase 2 (TYK2) inhibitor and to intermediate compounds of the synthesis and methods of making the intermediates. Also provided are pharmaceutically acceptable compositions including compounds prepared by the synthetic method and methods of treating disorders using the same.