CAS: 7584-05-6; 3-Methylisonicotinonitrile

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上下游产品

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3-甲基-4-甲酸嘧啶置于ammonium Hydroxide,氯化亚砜,三氯氧磷体系中,用 水 作为反应溶剂,化学反应 27.0H,反应生成 3-甲基-4-氰基吡啶
参考文献:通过支架跳跃策略发现和合成6,7,8,9-四氢-5 H-吡啶并[4,3-C] Azepin-5-One新型化学型ccr2拮抗剂
标题:通过支架跳跃策略发现和合成6,7,8,9-四氢-5 H-吡啶并[4,3-C] Azepin-5-One新型化学型ccr2拮抗剂
摘要:趋化因子cc受体亚型2(ccr2)在包括慢性炎症,糖尿病,神经性疼痛,动脉粥样硬化和癌症在内的多种治疗领域中引起了人们对药物开发的浓厚兴趣.通过采用切开-缝制的支架跳跃策略,我们确定了一个3,4-二氢-2,6-萘吡啶-1(2 H)-One的活性支架作为中心药效基团,以衍生出新颖的ccr2拮抗剂.关于环大小和萘啶酮环上取代的系统结构-活性关系研究产生了1-芳基氨基-6-烷基杂环-6,7,8,9-四氢-5 H-吡啶基[4,3-C] Azepin-5-Ones是具有纳摩尔抑制活性的新型ccr2拮抗剂的化学型.该化合物中最佳的拮抗活性以化合物13A为例,该化合物结合了c-1处的3,4-二氯苯氨基和n-6处的3-(4-(n-甲基甲基磺酰胺基)哌啶-1-基)丙基的最佳取代基位置,Ic 50值为61 Nm,Ccr2的选择性是ccr5的10倍.建立了有效而通用的合成方法,以构建创新的核心结构并推导化合物集合.这是关于我们设计的6
DOI:10.1016/j.Bmc.2018.05.027

专利信息

专利号:US-9394264-B2
优先权日:2009-11-13
标 题:Sphingosine 1 phosphate receptor modulators and methods of chiral synthesis
发明人：MARTINBOROUGH ESTHER; BOEHM MARCUS F; YEAGER ADAM RICHARD; TAMIYA JUNKO; HUANG LIMING; BRAHMACHARY ENUGURTHI; MOORJANI MANISHA
权利人:RECEPTOS INC
摘要:Compounds that selectively modulate the sphingosine 1 phosphate receptor are provided including compounds which modulate subtype 1 of the S1P receptor. Methods of chiral synthesis of such compounds are provided. Uses, methods of treatment or prevention and methods of preparing inventive compositions including inventive compounds are provided in connection with the treatment or prevention of diseases, malconditions, and disorders for which modulation of the sphingosine 1 phosphate receptor is medically indicated.

专利号:US-6960601-B2
优先权日:2001-09-24
标题 :Preparation and use of imidazole derivatives for treatment of obesity
发明人：SMITH ROGER A; O'CONNOR STEPHEN J; WIRTZ STEPHAN-NICHOLAS; WONG WAI C; CHOI SOONGYU; KLUENDER HAROLD C E; SU NING; WANG GAN; ACHEBE FURAHI; YING SHIHONG
权利人:BAYER PHARMACEUTICALS CORP
摘要:This invention relates to substituted imidazole derivatives which have been found to suppress appetite and induce weight loss. The invention also provides methods for synthesis of the compounds, pharmaceutical compositions comprising the compounds, and methods of using such compositions for inducing weight loss and treating obesity and obesity-related disorders.

专利号:CN-113582915-B
优先权日:2021-07-25
标题 :A kind of synthesis method of 4-substituted pyridine compounds

专利号:CA-2780433-C
优先权日:2009-11-13
标 题 :Sphingosine 1 phosphate receptor modulators and methods of chiral synthesis

专利号:US-2015299150-A1
优先权日:2009-11-13
标题:Sphingosine 1 phosphate receptor modulators and methods of chiral synthesis

专利号:WO-2011060389-A1
优先权日:2009-11-13
标题 :Sphingosine 1 phosphate receptor modulators and methods of chiral synthesis