CAS: 123148-66-3; (2-Methoxypyridin-4-yl)Methanol

相似化合物

72716-87-1 26156-51-4 156367-50-9

上下游产品

methyl 2-methoxyisonicotinate (2-chloropyridin-4-yl)methanol sodium methylate ethyl 2-methoxy-pyridine-4-carboxylate 2-methoxypyridine-4-carboxaldehyde (2-Methoxy-pyridin-4-yl)-(2-vinyl-phenylamino)-acetic acid methyl ester (2-Methoxy-pyridin-4-yl)-(2-vinyl-phenylamino)-selenoacetic acid Se-methyl ester {5-[(2-Methoxy-pyridin-4-yl)-(2-vinyl-phenylamino)-methyl]-oxazol-4-yl}-methanol

2-甲氧基异烟酸甲酯置于lithium Aluminium Tetrahydride体系中,用 四氢呋喃 用作溶剂,化学反应 3.0H,以33.55 G的收率获得2-甲氧基吡啶-4-甲醇
参考文献:发现和生物学评价新型的4-氨基-2-苯基嘧啶衍生物作为有效和口服活性的gpr119激动剂
标题:发现和生物学评价新型的4-氨基-2-苯基嘧啶衍生物作为有效和口服活性的gpr119激动剂
摘要:合成了新型的4-氨基-2-苯基嘧啶衍生物,并将其评估为gpr119激动剂.优化2-位苯环上的取代基和4-位氨基上的取代基,可以鉴定出显示出强效gpr119激动活性的3,4-二卤代和2,4,5-三卤代苯基衍生物.发现高级类似物(2 R)-3-{[2-(4-氯-2,5-二氟苯基)-6-乙基嘧啶-4-基]氨基}丙烷-1,2-二醇(24G)可以改善在小鼠中口服1 Mg / Kg的葡萄糖耐量,并在小鼠和猴子中表现出出色的药代动力学特征.在单日治疗一周后,化合物24G在糖尿病kk / Ay小鼠中也显示出优异的抗糖尿病作用.这些结果表明,新型gpr119激动剂24G 不仅可以通过增强葡萄糖依赖性胰岛素的分泌来改善葡萄糖耐受性,还可以通过保留胰腺β细胞功能来改善葡萄糖耐受性.
Doi:10.1016/j.Bmc.2012.06.049

专利信息

专利号:US-8178559-B2
优先权日:2004-12-30
标 题:Organic compounds
发明人：BREITENSTEIN WERNER; EHARA TAKERU; EHRHARDT CLAUS; GROSCHE PHILIPP; HITOMI YUKO; IWAKI YUKI; KANAZAWA TAKANORI; KONISHI KAZUHIDE; MAIBAUM JUERGEN KLAUS; MASUYA KEIICHI; IWASAKI ATSUKO; OSTERMANN NILS; SUZUKI MASAKI; TOYAO ATSUSHI; YOKOKAWA FUMIAKI
权利人:BREITENSTEIN WERNER; EHARA TAKERU; EHRHARDT CLAUS; GROSCHE PHILIPP; HITOMI YUKO; IWAKI YUKI; KANAZAWA TAKANORI; KONISHI KAZUHIDE; MAIBAUM JUERGEN KLAUS; MASUYA KEIICHI; IWASAKI ATSUKO; OSTERMANN NILS; SUZUKI MASAKI; TOYAO ATSUSHI; YOKOKAWA FUMIAKI; NOVARTIS AG
摘要:3,4-substituted piperidine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (=disorder) that depends on activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on activity of renin; the use of a compound of that class in the treatment of a disease that depends on activity of renin; pharmaceutical formulations comprising a 3,4-substituted piperidine compound, and/or a method of treatment comprising administering a 3,4substituted piperidine compound, a method for the manufacture of a 3,4-substituted piperidine compound, and novel intermediates and partial steps for their synthesis are disclosed. The 3,4-disubstituted piperidine compounds have the formula (I), wherein the symbols have the meanings defined in the specification.

专利号:RU-2194701-C2
优先权日:1995-12-18
标 题 :Derivatives of quinazoline, methods of their synthesis, pharmaceutical composition comprising thereof and method of achievement of anti-angiogenic effect and/or effect of decrease of vascular penetration with their using