CAS: 63968-85-4; 2-(Trifluoromethoxy)Benzonitrile

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CAS号456-55-3 三氟甲氧基苯 | CAS号1130-90-1 1-naphthyl cyanate | CAS号307989-55-5 5-Nitro-2-(trif...

N-(2-(Trifluoromethoxy)Phenyl)Formamide置于三乙胺,三氯氧磷体系中,用 四氢呋喃 作为反应溶剂,化学反应 4.0H,以85.23%的收率获得产物邻三氟甲氧基苯腈
参考文献:新型4-(2-氟苯氧基)喹啉衍生物作为选择性c-Met抑制剂的设计,合成和生物学评价
标题:新型4-(2-氟苯氧基)喹啉衍生物作为选择性c-Met抑制剂的设计,合成和生物学评价
摘要:设计,合成了两个带有1 H-咪唑-4-羧酰胺基或(e)-3-氢磺酰基丙烯酰胺基序的新型6,7-二取代-4-(2-氟苯氧基)喹啉衍生物(16-31和32-42).并评估其体外细胞毒性活性.大多数化合物对测试的三种细胞系表现出中等至优异的效力,并且进一步检查了十五种化合物对c-Met激酶的抑制活性.最有前途的化合物16(c-Met激酶[ic 50] = 1.1 Nm)对具有ic的ht-29,Mkn-45和a549细胞表现出高选择性和显着的细胞毒性50个值0.08,0.22和0.07μm,它们的活性是福瑞替尼的3.1倍,1.4倍和2.1倍.初步的结构-活性关系以及分子对接表明,1 H-咪唑-4-羧酰胺基作为连接基对于抗肿瘤活性非常重要.
DOI:10.1016/j.Bmc.2016.12.002

专利信息

专利号:US-2010160351-A1
优先权日:2008-12-19
标题:Pharmaceutical compositions and methods for treating hyperuricemia and related disorders
发明人：JENKINS HELEN; KITT MICHAEL; PEARLMAN RODNEY; SERAFINI TITO; THORSETT EUGENE
权利人:NUON THERAPEUTICS INC
摘要:Disclosed is a pharmaceutical composition comprising (a) a first therapeutic agent, wherein the first therapeutic agent is a compound of formula II: n n n n n n n n n n n n or a pharmaceutically acceptable salt thereof, wherein R 1 , R 2 , R 3 , R 4 , X and n are as defined herein; (b) a second therapeutic agent, wherein the second therapeutic agent is a uric acid synthesis inhibitor or a uricosuric agent; and (c) a pharmaceutically acceptable diluent or carrier.

专利号:PH-12015502708-B1
优先权日:2009-11-13
标题:Selective sphingosine 1 phosphate receptor modulators and methods of chiral synthesis