CAS: 39499-34-8; 5-Methylisoxazole-3-Carbonyl Chloride

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62254-74-4 35166-37-1 24068-54-0

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5-methyl-isoxazole-3-carboxylic acid; sodium salt 5-methylisoxazole 3-carboxylic acid ethyl 5-methylisoxazole-3-carboxylate 5-methyl-isoxazole-3-carboxylic acid dimethylamide 5-methyl-3-(N-phenylcarbamoyl)isoxazole 5-methyl-isoxazole-3-carbothioic acid amide H-pyrazole3,5-dimethyl-1-(5-methyl-isoxazole-3-carbonyl)-1H-pyrazole

5-甲基异恶唑-3-甲酸置于氯化亚砜体系中,用 六甲基磷酰三胺,乙腈 作为反应溶剂,化学反应 0.5H,反应生成 5-甲基异恶唑-3-羰酰氯
参考文献:融合的咪唑并吡啶的合成与构效关系:一系列苯二氮杂ze受体配体
标题:融合的咪唑并吡啶的合成与构效关系:一系列苯二氮杂ze受体配体
摘要:合成了2-Arylimidazo [4,5-C]喹啉和类似的稠合咪唑并吡啶,并评价为苯并二氮杂receptor受体配体.与吡唑并喹啉如cgs-9896相比,与受体的亲和力受2-位芳基庞大性的影响.在2-位具有异恶唑部分的衍生物显示出高结合亲和力和体内活性.在咪唑并[4,5-C]喹啉系列中,在6-位的取代降低或消除了活性.除7-卤代类似物外,大多数具有未取代异恶唑基的衍生物均表现出拮抗或反向激动剂活性.另一方面,5-甲基异恶唑-3-基或3-甲基异恶唑-5-基衍生物通常表现出激动剂活性.在与非芳族环稠合的咪唑并吡啶中观测到对异恶唑部分的类似取代作用.根据详细的药理评估,S-8510,2-(3-异恶唑基)-3,6,7,9-四氢咪唑并[4,5-D]吡喃++ + [4,3-B]吡啶一磷酸具有弱的反向激动剂选择活性作为治疗老年性痴呆某些症状的治疗候选药物.
DOI:10.1021/jm9600609

专利信息

专利号:US-6534530-B1
优先权日:1999-08-04
标题:Antipicornaviral compounds and compositions, their pharmaceutical uses, and materials for their synthesis
发明人：DRAGOVICH PETER SCOTT; ZHOU RU; WEBBER STEPHEN EVAN; PRINS THOMAS J; REICH SIEGFRIED HEINZ; KEPHART SUSAN E; RUI YUANJIN
权利人:AGOURON PHARMA
摘要:Compounds of the formula:where the formula variables are as defined in the disclosure, advantageously inhibit or block the biological activity of the picornaviral 3C protease. These compounds, as well as pharmaceutical compositions containing these compounds, are useful for treating patients or hosts infected with one or more picornaviruses, such as RVP. Intermediates and synthetic methods for preparing such compounds are also described.

专利号:US-6514997-B2
优先权日:1999-12-03
标题:Antipicornaviral compounds and compositions, their pharmaceutical uses, and materials for their synthesis
发明人：DRAGOVICH PETER S; PRINS THOMAS J; ZHOU RU; JOHNNSON JR THEODORE O
权利人:AGOURON PHARMA
摘要:Compounds of the formula: n where the formula variables are as defined herein, are disclosed that advantageously inhibit or block the biological activity of the picornaviral 3C protease. Also disclosed are compounds of the formula: n where the formula variables are as defined herein that advantageously inhibit or block the biological activity of the picornaviral 3C protease. These compounds, as well as pharmaceutical compositions containing these compounds, are useful for treating patients or hosts infected with one or more picornaviruses, such as rhinovirus 3C proteases. Intermediates and synthetic methods for preparing such compounds are also described.

专利号:US-6995142-B2
优先权日:1998-04-30
标题 :Antipicornaviral compounds and compositions, their pharmaceutical uses, and materials for their synthesis
发明人：DRAGOVICH PETER SCOTT; WEBBER STEPHEN EVAN; PRINS THOMAS JAY; ZHOU RU; MARAKOVITS JOSEPH TIMOTHY; JOHNSON JR THEODORE O
权利人:AGOURON PHARMA
摘要:Peptido and peptidomimetic compounds of the formula: n nwherein the formula variables are as defined in the disclosure, advantageously inhibit or block the biological activity of the picornaviral 3C protease. These compounds, as well as pharmaceutical compositions containing these compounds, are useful for treating patients or hosts infected with one or more picornaviruses, such as RVP. Intermediates and synthetic methods for preparing such compounds are also provided.