CAS: 41094-88-6; Tracazolate

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CAS号109-73-9 正丁胺 | CAS号41095-07-2 4-chloro-1-ethy... | CAS号570-08-1 瑞吡司特中间体 | CAS号41095-06-1 ethyl 1-ethyl-4... | CAS号3528-58-3 5-氨基-1-乙基吡唑

📜乙酰基丙二酸二乙酯置于ppa,三氯氧磷体系中,用 乙醇 作为反应溶剂,化学反应生成 西卡唑酯
参考文献:一系列焦虑选择性吡唑并吡啶酯和酰胺抗焦虑剂的合成及构效关系.
标题:一系列焦虑选择性吡唑并吡啶酯和酰胺抗焦虑剂的合成及构效关系.
摘要:合成了一系列的1-取代的4-氨基-1H-吡唑并[3,4-B]吡啶-5-羧酸酯和酰胺,并筛选了在休克诱导的饮酒抑制(ssd)试验中的抗焦虑活性.还测试了化合物从大脑苯并二氮杂(bz)结合位点置换[3H]氟硝西m(flu)的能力.许多化合物在这些筛选中均具有活性,此外,Hill系数显着小于1,并通过[3H] Flu结合分析表明,对1 Bz(bz1)受体的选择性高于对2 Bz(bz2)受体的选择性.来自不同大脑区域的结果.基于这些化合物的结构活性研究结果,提出了一种假设来解释与脑bz受体进行最佳相互作用所必需的结构特征.对最有效的行为活性化合物之一的详细药理评估(27)表明它具有bz1选择性.此外,与地西epa相比,在治疗有效剂量下,27种药物具有最小的镇静和酒精相互作用特性.
DOI:10.1021/jm00132A011

专利信息

专利号:US-8697888-B2
优先权日:2012-01-06
标题 :Substituted (1-(methylsulfonyl)azetidin-3-yl)(heterocycloalkyl)methanone analogs as antagonists of muscarinic acetylcholine M1 receptors
发明人：LINDSLEY CRAIG W; CONN P JEFFREY; WOOD MICHAEL R; MELANCON BRUCE J; CHEUNG YIU-YIN
权利人:UNIV VANDERBILT
摘要:In one aspect, the invention relates to substituted (1-(methylsulfonyl)azetidin-3-yl)(heterocycloalkyl)methanone analogs, derivatives thereof, and related compounds, which are useful as antagonists of the muscarinic acetylcholine receptor M 1 (mAChR M 1 ); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

专利号:US-9056875-B2
优先权日:2012-08-31
标 题 :Substituted pyrazolo[3′,4′:4,5]thieno[2,3-C]pyridazin-3-amine analogs as positive allosteric modulators of the muscarinic acetylcholine receptor M4
发明人：LINDSLEY CRAIG W; CONN P JEFFREY; WOOD MICHAEL R; SALOVICH JAMES M
权利人:UNIV VANDERBILT
摘要:In one aspect, the invention relates to substituted pyrazolo[3′,4′:4,5]thieno[2,3-c]pyridazine-3-amine analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M 4 (mAChR M 4 ); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

专利号:US-9073935-B2
优先权日:2011-11-11
标 题:Substituted benzylspiroindolin-2-one analogs as positive allosteric modulators of the muscarinic acetylcholine receptor M1
发明人：LINDSLEY CRAIG W; CONN P JEFFREY; WOOD MICHAEL R; HOPKINS COREY R; MELANCON BRUCE J; POSLUSNEY MICHAEL S
权利人:UNIV VANDERBILT
摘要:In one aspect, the invention relates to substituted benzylspiroindolin-2-one analogs compounds, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M 1 (mAChR M 1 ); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

专利号:US-7799829-B2
优先权日:2006-07-28
标 题 :Acyloxyalkyl carbamate prodrugs of α-amino acids, methods of synthesis and use
发明人：DAI XUEDONG; GANGAKHEDKAR ARCHANA; XIANG JIA-NING; GALLOP MARK A
权利人:XENOPORT INC
摘要:Acyloxyalkyl carbamate prodrugs of α-amino acids, pharmaceutical compositions thereof, methods of making acyloxyalkyl carbamate prodrugs of α-amino acids and methods of using acyloxyalkyl carbamate prodrugs of α-amino acids, and pharmaceutical compositions thereof to treat a disease are disclosed. Acyloxyalkyl carbamate prodrugs of α-amino acids suitable for oral administration using sustained release dosage forms are also disclosed.

专利号:US-2018170867-A1
优先权日:2015-05-08
标 题:Stereoselective synthesis of 9-cis.13,14-dihydroretinoic acid and its ethyl esters

专利号:US-2016200733-A1
优先权日:2013-08-23
标 题 :Substituted thieno[2,3-b]pyridine-2-carboxamide analogs as positive allosteric modulators of the muscarinic acetylcholine receptor m4
发明人：LINDSLEY CRAIG W; CONN P JEFFREY; WOOD MICHAEL R; POSLUSNEY MICHAEL S; MELANCON BRUCE J
权利人:UNIV VANDERBILT
摘要:In one aspect, the invention relates to substituted thieno[2,3-b]pyridine-2-carboxamide analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M 4 (mAChR M 4 ); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.