CAS: 778270-11-4; 3-(6-((4-(Trifluoromethoxy)Phenyl)Amino)Pyrimidin-4-yl)Benzamide

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CAS号461-82-5 对三氟甲氧基苯胺

📜对三氟甲氧基苯胺置于四(三苯基膦)钯,Sodium Carbonate,N,N-二异丙基乙胺体系中,用 乙醇,水,乙腈 作为反应溶剂,化学反应 11.0H,反应生成 3-[6-[[4-(三氟甲氧基)苯基]氨基]-4-嘧啶基]苯甲酰胺
参考文献:Direct Binding Assay For The Detection Of Type Iv Allosteric Inhibitors Of Abl
标题:Direct Binding Assay For The Detection Of Type Iv Allosteric Inhibitors Of Abl
摘要:Abelson (Abl) Tyrosine Kinase Is An Important Cellular Enzyme That Is Rendered Constitutively Active In The Breakpoint Cluster Region (Bcr)-Abl Fusion Protein,Contributing To Several Forms Of Leukemia. Although Inhibiting Bcr-Abl Activity With Imatinib Shows Great Clinical Success,Many Patients Acquire Secondary Mutations That Result In Resistance To Imatinib. Second-Generation Inhibitors Such As Dasatinib And Nilotinib Can Overcome The Majority Of These Mutations But Fail To Treat Patients With An Especially Prevalent T315I Mutation At The Gatekeeper Position Of The Kinase Domain. However,A Combination Of Nilotinib With An Allosteric Type Iv Inhibitor Was Recently Shown To Overcome This Clinically Relevant Point Mutation. In This Study,We Present The Development Of A Direct Binding Assay That Enables The Straightforward Detection Of Allosteric Inhibitors Which Bind Within The Myristate Pocket Of Abl. The Assay Is Amenable To High-Throughput Screening And Exclusively Detects The Binding Of Ligands To This Unique Allosteric Site.
DOI:10.1021/ja303858W

专利信息

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-7906490-B2
优先权日:1993-04-15
标 题 :Circular DNA vectors for synthesis of RNA and DNA
发明人：KOOL ERIC T
权利人:UNIV ROCHESTER
摘要:The present invention provides methods for synthesis and therapeutic use of DNA and RNA oligonucleotides and analogs. RNA oligonucleotides are synthesized using a small, circular DNA template which lacks an RNA polymerase promoter sequence. The RNA synthesis is performed by combining a circular single-stranded oligonucleotide template with an effective RNA polymerase and at least two types of ribonucleotide triphosphate to form an RNA oligonucleotide multimer comprising multiple copies of the desired RNA oligonucleotide sequence. Preferably, the RNA oligonucleotide multimer is cleaved to produce RNA oligonucleotides having well-defined ends. Preferred RNA oligonucleotide multimers contain ribozymes capable of both cis (autolytic) and trans cleavage.

专利号:US-6368802-B1
优先权日:1993-04-15
标 题 :Circular DNA vectors for synthesis of RNA and DNA
发明人：KOOL ERIC T
权利人:UNIV ROCHESTER
摘要:The present invention provides methods for synthesis and therapeutic use of DNA and RNA oligonucleotides and analogs. RNA oligonucleotides are synthesized using a small, circular DNA template which lacks an RNA polymerase promoter sequence. The RNA synthesis is performed by combining a circular single-stranded oligonucleotide template with an effective RNA polymerase and at least two types of ribonucleotide triphosphate to form an RNA oligonucleotide multimer comprising multiple copies of the desired RNA oligonucleotide sequence. Preferably, the RNA oligonucleotide multimer is cleaved to produce RNA oligonucleotides having well-defined ends. Preferred RNA oligonucleotide multimers contain ribozymes capable of both cis (autolytic) and trans cleavage.

专利号:US-2008031812-A1
优先权日:1999-06-02
标 题:Redox-stable, non-phosphorylated cyclic peptide inhibitors of sh2 domain binding to target protein, conjugates, thereof, compositions and methods of synthesis and use
发明人：ROLLER PETER P; LONG YA-QIU; LUNG FENG-DI T; KING C RICHTER; YANG DAJUN; VOIGT JOHANNES H
权利人:GOVERNMENT OF THE USA REPRESEN; UNIV GEORGETOWN
摘要:A compound of formula: n n nin which (i) aa 1 is Adi and aa 4 is Glu or (ii) each of aa 1 and aa 4 is Adi, L is sulfur, sulfoxide, oxygen or methylene, which compound (and its conjugates) bind to an SH2 domain in a protein comprising an SH2 domain, is non-phosphorylated, is redox-stable in vivo, is characterized by an IC 50 in vivo of less than about 4.0 μM with respect to the SH2 domain in Grb2, and, upon binding to the SH2 domain of Grb2, has a turn conformation. A conjugate comprising a compound as described above and a carrier agent, a composition comprising (i) a compound or a conjugate as described above and (ii) a carrier, a method of inhibiting binding of an SH2 domain in a protein comprising an SH2 domain to a target protein in an animal, wherein the SH2 domain is contacted with a target protein-binding inhibiting effective amount of a compound or a conjugate as described above, and a method of synthesizing such conjugates.

专利号:US-11612610-B2
优先权日:2018-12-14
标题:Mito-magnolol compounds and methods of synthesis and use thereof
发明人：KALYANARAMAN BALARAMAN; ZIELONKA JACEK MICHAL; CHENG GANG; HARDY MICAEL JOËL; OUARI OLIVIER
权利人:MEDICAL COLLEGE WISCONSIN INC; AIX MARSEILLE UNIV; MEDICAL COLLEGE OF WISCONSIN INC
摘要:The present invention provides mito-magnolol compounds, pharmaceutical compositions thereof, and methods of using the mito-magnolol compounds in the treatment of cancer, especially anti-cancer therapy or kinase resistant cancers.

专利号:US-7709657-B2
优先权日:2005-06-09
标 题:Process for the synthesis of organic compounds
发明人：ACEMOGLU MURAT; SCHENKEL BERTHOLD; SHIEH WEN-CHUNG; XUE SONG; WIDMER ERICH; GARCIA FUENTES PEDRO; MARTIN MEDINA JOSE; VICENTE BANOS FRANCISCO
权利人:NOVARTIS AG
摘要:The present invention provides an efficient, safe and cost effective way to prepare 5-(4-methyl-1H-imidazol-1-yl)-3-(trifluoromethyl)-benzenamine which is an intermediate for the preparation of substituted pyrimidinylaminobenzamides of formula (II):