CAS: 2639957-39-2; (S)-N-(3-(2-(((R)-1-Hydroxypropan-2-yl)Amino)-6-Morpholinopyridin-4-yl)-4-Methylphenyl)-3-(2,2,2-Trifluoroethyl)Pyrrolidine-1-Carboxamide

该化合物是一种选择性的小型分子抑制剂,针对与诱导诱导信号有牵连的特定动脉路径,其主要机制包括有选择地有效抑制关键动脉,阻止细胞异常扩散,在目标恶性肿瘤中生存.Exarafenib显示了高度的紧密结合性和特殊性,尽量减少目标外效应,并提高了治疗精确度.临床初步研究表明了强健的抗脉冲活动,特别是在具有相关基因改变的模型中.复合物展示了有利的药用动因特性,包括口服生物利用率和可控代谢稳定性.其优化分子结构增强了目标接触,同时降低了潜在毒性.Exarafenib是精确肿瘤应用的很有希望的调查剂,目前正在开展研究以进一步阐明其临床潜力.

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    专利信息


    专利号:WO-9517903-A1
    优先权日:1993-12-28
    标 题:Modular design and synthesis of oxazolone-derived molecules
    发明人:HOGAN JOSEPH C JR; CASEBIER DAVID; FURTH PAUL; TU CHENG
    权利人:ARQULE PARTNERS L P; HOGAN JOSEPH C JR; CASEBIER DAVID; FURTH PAUL; TU CHENG
    摘要:The design and synthesis of novel oxazolone-derived molecular modules and the use of the modules in the construction of new molecules and fabricated materials is disclosed. The new molecules and fabricated materials are molecular recognition agents useful in the design and synthesis of drugs, and have applications in separations and materials science.

    专利号:US-8168828-B2
    优先权日:2007-06-25
    标题 :Process for the preparation of pregabalin
    发明人:SATYANARAYANA REDDY MANNE; THIRUMALAI RAJAN SRINIVASAN; ESWARAIAH SAJJA; SATYANARAYANA REVU
    权利人:SATYANARAYANA REDDY MANNE; THIRUMALAI RAJAN SRINIVASAN; ESWARAIAH SAJJA; SATYANARAYANA REVU; MSN LAB LTD
    摘要:The present invention encompasses novel intermediates of pregabalin, namely 3-cyano-5-methyl hexanamide (28) and 3-(amino methyl)-5 methyl hexanamide (29), and processes for their preparation. The invention also encompasses a process for converting the novel pregabalin intermediates into pregabalin, Formula (I): The present invention further provides a cost effective method for the synthesis of (S)-pregabalin, which involves the recovery of mandelic acid and tartaric acid used in the resolution process and recycling them, increasing the yields of the final product formed, which substantially reduced the cost of the production.

    专利号:WO-2011161690-A1
    优先权日:2010-06-23
    标题:Processes for the preparation of (+)-n,n-dimethyl-2-[1-(naphthalenyloxy) ethyl] benzene methanamine and intermediates thereof
    发明人:MOHAN RAO DODDA; KRISHNA REDDY PINGILI; JITHENDER AADEPU; VENUGOPAL BINGI
    权利人:SYMED LABS LTD; MOHAN RAO DODDA; KRISHNA REDDY PINGILI; JITHENDER AADEPU; VENUGOPAL BINGI
    摘要:The present invention relates to processes for the preparation of S(+)-N,N-dimethyl-2-[1-(naphthalenyloxy)ethyl]benzene methanamine and intermediates thereof. More particularly the present invention relates to preparation of the compound 3(S)-(+)-N,N-dimethylamino-3-phenyl propanol useful as intermediate in the synthesis of pharmaceutically active compounds.

    专利号:US-5411927-A
    优先权日:1992-08-14
    标 题 :Process of preparing composite catalysts for production of synthesis gas by oxidative conversion of methane or natural gas
    发明人:CHOUDHARY VASANT R; RANE VILAS H; RAJPUT AMARJEET M R
    权利人:COUNCIL SCIENT IND RES
    摘要:An improved process for the production of synthesis gas (or carbon monoxide and hydrogen) by oxidative conversion of natural gas or methane, which comprises passing continuously a gaseous reactant mixture comprising methane (or natural gas) and oxygen (or air) with or without water vapors over reduced or unreduced composite catalyst, containing non-transition and/or transition metal oxides, represented by the formula Tm.Nn.R.Op, wherein T is selected from Ni, CO, Ir or the like or a mixture thereof, m is T/R mole ratio, N is a transition or non-transition element selected from Ti, Zr, Hf, Zn, Mg, Ca or the like or a mixture thereof, n represents the N/R mole ratio, R is a rare earth element selected from La, Ce, Pr, Ho, Yb or the like, or a mixture thereof, O is oxygen and p is the number of oxygen atoms required to fulfill the valence requirement of the elements in the composite catalyst. Synthesis gas can be produced in high yields and with very high production rate by oxidative conversion of methane or natural gas to CO and H2 or synthesis gas, using the composite catalyst containing non-transition and/or transition metal oxides.

    专利号:EP-4217339-A1
    优先权日:2020-09-26
    标题:A process for the synthesis of anthranilic acid/amide compounds and intermediates thereof

    专利号:TW-202222162-A
    优先权日:2020-09-26
    标 题 :A process for the synthesis of anthranilic acid/amide compounds and intermediates thereof

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    ✅ COA系统入驻 | 共享模式

    合成参考文献


    参考文献:10.1021/acs.jmedchem.3c01830
    摘要:Chen YK, Kanouni T, Arnold LD, Cox JM, Gardiner E, Grandinetti K, Jiang P, Kaldor SW, Lee C, Li C, Martin ES, Miller N, Murphy EA, Timple N, Tyhonas JS, Vassar A, Wang TS, Williams R, Yuan D, Kania RS. The Discovery of Exarafenib (KIN-2787): Overcoming the Challenges of Pan-RAF Kinase Inhibition. J Med Chem. 2024 Feb 08;67(3):1747–57. doi: 10.1021/acs.jmedchem.3c01830.
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