CAS: 380843-75-4; 4-((2,4-Dichloro-5-Methoxyphenyl)Amino)-6-Methoxy-7-(3-(4-Methylpiperazin-1-yl)Propoxy)Quinoline-3-Carbonitrile

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CAS号846023-56-1 2-cyano-N-(2,4-... | CAS号109-01-3 N-甲基哌嗪 | CAS号380844-49-5 7-(3-氯丙氧基)-4-[(... | CAS号5317-33-9 1-(3-羟丙基)-4-甲基哌嗪 | CAS号622369-46-4 4-(2,4-二氯-5-甲氧基... | CAS号98446-49-2 2,4-二氯-5-甲氧基苯胺 | CAS号366-99-4 3-氟-4-甲氧基苯胺 | CAS号622369-40-8 4-氯-6-甲氧基7-氟-喹啉-3-甲腈 | CAS号622369-38-4 7-氟-6-甲氧基-4-氧代-... | CAS号214470-68-5 4-氯-7-(3-氯丙氧基)-... | CAS号918639-08-4 bosutinib hydrate | CAS号918639-10-8 4-(2,4-dichloro...

2,4-二氯-5-甲氧基苯胺置于吡啶盐酸盐,Sodium Iodide体系中,用 乙二醇乙醚 作为反应溶剂,化学反应 22.5H,反应生成 伯舒替尼
参考文献:Optimization Of 4-Phenylamino-3-Quinolinecarbonitriles As Potent Inhibitors Of Src Kinase Activity
标题:Optimization Of 4-Phenylamino-3-Quinolinecarbonitriles As Potent Inhibitors Of Src Kinase Activity
摘要:Subsequent To The Discovery Of 4-[(2,4-Dichlorophenyl)Amino]-6,7-Dimethoxy-3-Quinolinecarbonitrile (1A) As An Inhibitor Of Src Kinase Activity (Ic50 = 30 Nm),Several Additional Analogues Were Prepared. Optimization Of The C-4 Anilino Group Of La Led To Le,Which Contains A 2,4-Dichloro-5-Methoxy-Substituted Aniline. Replacement Of The Methoxy Group At C-7 Of Le With A 3-(Morpholin-4-yl)Propoxy Group Provided 2C,Resulting In Increased Inhibition Of Both Src Kinase Activity And Src-Mediated Cell Proliferation. Analogues Of 2C,With Other Trisubstituted Anilines At C-4 Were Also Potent Src Inhibitors,And The Propoxy Group Of 2C Was Preferred Over Ethoxy,Butoxy,Or Pentoxy. Replacement Of The Morpholine Group Of 2C With A 4-Methylpiperazine Group Provided 31A,Which Had An Ic50 Of 1.2 Nm In The Src Enzymatic Assay,An Ic50 Of 100 Nm For The Inhibition Of Src-Dependent Cell Proliferation And Was Selective For Src Over Non-Src Family Kinases. Compound 31A,Which Had Higher 1 And 4 H Plasma Levels Than 2C,Effectively Inhibited Tumor Growth In Xenograft Models.
DOI:10.1021/jm0102250

专利信息

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-12240835-B2
优先权日:2018-09-18
标题:Substituted benzamides as intermediates in the synthesis of inhibitors of tyrosine kinase enzymatic activity
发明人：ROMERO F ANTHONY; KIRSCHBERG THORSTEN A; HALCOMB RANDALL; XU YINGZI
权利人:TERNS PHARMACEUTICALS INC
摘要:Provided herein are compounds, preferably compounds inhibiting tyrosine kinase enzymatic activity of a protein selected from Abelson protein (ABL1), Abelson-related protein (ABL2), or a chimeric protein BCR-ABL1, compositions thereof, and methods of their preparation, and methods of inhibiting tyrosine kinase enzymatic activity of a protein selected from Abelson protein (ABL1), Abelson-related protein (ABL2), or a chimeric protein BCR-ABL1, and methods for treating diseases wherein modulation of BCR-ABL1 activity prevents, inhibits, or ameliorates the pathology and/or symptomology of the disease. Intermediates such as compounds of Formula (S23), which are useful in the synthesis of compounds inhibiting tyrosine kinase enzymatic activity of a protein selected from Abelson protein (ABL1), Abelson-related protein (ABL2), or a chimeric protein BCR-ABL1, are also provided.

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-8828984-B2
优先权日:2012-11-19
标题:Gold(III) complexes containing N-heterocyclic carbene ligand, synthesis, and their applications in cancer treatment and thiol detection
发明人：CHE CHI MING; ZOU TAOTAO
权利人:UNIV HONG KONG; UNIV HONG KONG
摘要:Provided herein is a method of synthesis of Au(III)-NHC complexes, a pharmaceutical composition comprises thereof. Also provided herein are the methods for the treatment and prevention of cancer/tumor in patients in need thereof by the administration of the Au(III)-NHC complexes. Also provided is method of detecting thiol in a biological system. The Au(III)-NHC complexes possess anticancer activity such as the induction of cell death, inhibition of cellular proliferation, inhibition of thioredoxin reductase activity, and inhibition of tumor growth in vivo.

专利号:US-10577387-B1
优先权日:2018-08-09
标题 :Platinum (II) complexes containing N-heterocyclic carbene ligand and pincer ligands, synthesis, and their applications in cancer treatment
发明人：CHE CHI MING; Fung Sin Ki; Chen tian feng
权利人:UNIV HONG KONG
摘要:Provided herein is a method of synthesis of Pt(II) complexes, a pharmaceutical composition comprises thereof. Also provided herein are the methods for the treatment and prevention of cancer/tumor in patients in need thereof by the administration of the Pt(II) complexes. Also provided is a method of detecting the Pt(II) complex in a biological system. Also provided is a method of making the Pt(II) complex The Pt(II) complexes possess anticancer activity such as the induction of cell death, inhibition of cellular proliferation, and inhibition of tumor growth in vivo.

专利号:US-11286271-B2
优先权日:2018-07-31
标 题 :Iridium (III) complexes containing N-heterocyclic carbene ligand, synthesis, and their use thereof in cancer treatment
发明人：CHE CHI MING; LAM TSZ LUNG; TONG KA CHUNG
权利人:UNIV HONG KONG
摘要:Provided herein are Ir(III) complexes comprising N-heterocyclic carbene ligand, method of synthesis of the Ir(III) complexes, a pharmaceutical composition comprises thereof. Also provided herein are the methods for the treatment and prevention of cancer/tumor in patients in need thereof by the administration of the Ir(III) complexes under both dark and light conditions. Also provided is a method of detecting the Ir(III) complex in a biological system. Also provided is a method of making the Ir(III) complex. The Ir(III) complexes possess anticancer activity such as the induction of cell death, inhibition of cellular proliferation, and inhibition of tumor growth in vivo.