CAS: 159178-03-7; 2,6-Dichloro-4-Isocyanatopyridine

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📜柠嗪酸置于sodium Azide,草酰氯,Lithium Hydroxide Monohydrate,三氟乙酸,三氯氧磷体系中,用 四氢呋喃,二氯甲烷,水,丙酮,苯 用作溶剂,化学反应 49.36H,反应生成2,6-二氯-4-吡啶异氰酸酯
参考文献:优化的三嗪腈作为罗德萨因抑制剂:结构与活性之间的关系,生物等位咪唑并吡啶腈和人组织蛋白酶l的x射线晶体结构分析
标题:优化的三嗪腈作为罗德萨因抑制剂:结构与活性之间的关系,生物等位咪唑并吡啶腈和人组织蛋白酶l的x射线晶体结构分析
摘要:引起非洲昏睡病的布鲁氏锥虫寄生虫的半胱氨酸蛋白酶罗氏蛋白酶已成为开发新候选药物的目标.基于三嗪腈部分作为亲电头基,使用基于结构的设计对酶的s1,S2和s3口袋的取代基进行了优化研究,得到了抑制剂,其抑制常数在个位数纳摩尔范围内.全面的结构-活性关系阐明了活性位点各个口袋的结合偏好.S1口袋可容忍各种取代基,其中优先选择挠性和碱性侧链.S2取代基的变化导致抑制亲和力低至2 N M的高亲和力配体用于带有环己基取代基的化合物.对s3口袋的系统研究表明,它有可能通过芳香族载体实现高活性,这些芳香族载体与形成口袋的一部分的平面肽骨架进行堆叠相互作用.用结构相关酶人组织蛋白酶l的x射线晶体结构分析证实了分子建模所提出的三嗪配体系列的结合模式.通过优化周期确定的最佳取代基修饰的配体可实现亚微摩尔对培养寄生虫增殖的抑制.在基于细胞的测定中,在抑制剂上引入基本侧链导致抗锥虫活性提高了35倍.最后,为了减少三
Doi:10.1002/cmdc.201300112

专利信息

专利号:US-7138526-B1
优先权日:1999-06-15
标 题 :Solid phase synthesis of n,n-disubstituted diazacycloalkylcarboxy derivatives
发明人：HERPIN TIMOTHY F; MORTON GEORGE C; SALVINO JOSEPH M
权利人:AVENTIS PHARMA INC
摘要:A method for the solid phase synthesis of N,N-disubstituted diazacycloalkylcarboxy derivatives of general formula (I) and (II) is claimed. Examples include piperazine-2-carboxamide. The method is applicable to the synthesis or large combinatorial libraries

专利号:US-6054464-A
优先权日:1996-02-23
标题:Azabicyclic esters of carbamic acids useful in therapy
发明人：MACOR JOHN; WU EDWIN
权利人:ASTRA AB
摘要:A compound of formula ##STR1## X is O or S; Y is O or S; G and D are independently nitrogen or carbon with the proviso that no more than one of G, D, or E is nitrogen; E is N or C--R 4 ; R 1 is hydrogen or methyl; R 2 is hydrogen or fluoro; R 3 is hydrogen, halogen, C 1 to C 3 alkyl, --OR 5 , --CN, --CONH 2 , --CO 2 R 5 , --NR 5 R 6 or phenyl optionally substituted with one to three of the following substituents: halogen, C 1 to C 3 alkyl, --NO 2 , --CN, or --OCH 3 ; R 4 is hydrogen, halogen, C 1 to C 3 alkyl, --OR 5 , --CN, --CONH 2 , --CO 2 R 5 , --NR 5 R 6 or phenyl optionally substituted with one to three of the following substituents: halogen, C 1 to C 3 alkyl, --NO 2 , --CN, or --OCH 3 ; n or R 2 and R 3 or R 3 and R 4 may together represent a fused phenyl ring optionally substituted with one or two of the following substituents: halogen, C 1 to C 3 alkyl, --NO 2 , --CN, or --OCH 3 ; R 5 and R 6 are independently hydrogen or C 1 to C 3 alkyl; n or an enantiomer thereof, and pharmaceutically acceptable salts thereof, processes for preparing the, compositions containing them, and their use in therapy, especially in the treatment or prophylaxis of psychotic disorders and intellectual impairment disorders, as well as intermediates and use of intermediates in synthesis.

专利号:EP-1200824-B1
优先权日:1999-06-15
标题:Solid phase synthesis of n,n-disubstituted diazacycloalkylcarboxy derivatives

专利号:WO-2014158302-A1
优先权日:2013-03-25
标 题:Novel sphingosine 1-phosphate receptor antagonists
发明人：SWENSON ROLF ERIC
权利人:SWENSON ROLF ERIC
摘要:The present invention relates to sphingosine-1 -phosphate (S1 P) receptors and compounds of the general formula (1), that are useful in the treatment and prevention of conditions associated with such receptors. More specifically, the present invention relates to the synthesis and use of sphingosine 1 -phosphate receptor 2 (S1 P2) antagonists that are useful in the treatment of cancer, atherosclerosis, diabetic retinopathy, and other inflammatory diseases. Among these inflammatory diseases that could be treated with these S1 P2 antagonist are those characterized by fibrosis including chronic lung disease, chronic kidney and liver disease, chronic heart disease, and skin diseases such as sclerosis/scleroderma. The S1 P2 antagonists can also be used in the treatment of glioblastoma multiforme (brain cancer), pediatric neuroblastoma, and other cancers.

专利号:US-9663511-B2
优先权日:2012-03-26
标题:Sphingosine 1-phosphate receptor antagonists
发明人：SWENSON ROLF E
权利人:ARROYO BIOSCIENCES LLC
摘要:The present invention relates to sphingosine-1-phosphate (S1P) receptors and compounds of the general formula: n nthat are useful in the treatment and prevention of conditions associated with such receptors. More specifically, the present invention relates to the synthesis and use of sphingosine 1-phosphate receptor 2 (S1P 2 ) antagonists that are useful in the treatment of cancer, atherosclerosis, diabetic retinopathy, and other inflammatory diseases. Among these inflammatory diseases that could be treated with these S1P 2 antagonist are those characterized by fibrosis including chronic lung disease, chronic kidney and liver disease, chronic heart disease, and skin diseases such as sclerosis/scleroderma. The S1P 2 antagonists can also be used in the treatment of glioblastoma multiforme (brain cancer), pediatric neuroblastoma, and other cancers.