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公开(公告)号：US06909002B2
公开(公告)日：2005-06-21
申请号：US10690118
申请日：2003-10-21
IPC分类号： A61K31/4745 , C07D471/02 , C07D471/04
CPC分类号： C07D471/04
摘要： In one aspect, the present invention is directed to a one pot method of preparing intermediates of Formula V, which are useful in making inhibitors of phosphodiesterase-4: The present invention is also directed to a method of preparing phosphodiesterase inhibitors comprising the Formula
摘要翻译： 一方面，本发明涉及制备式V中间体的一锅法，其可用于制备磷酸二酯酶-4的抑制剂：本发明还涉及制备磷酸二酯酶抑制剂的方法，其包含式
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公开(公告)号：US07312334B2
公开(公告)日：2007-12-25
申请号：US10530465
申请日：2003-11-18
IPC分类号： C07D471/02
CPC分类号： C07D471/04
摘要： In one aspect, the present invention is directed to a one pot method of preparing intermediates of Formula (V), which are useful in making inhibitors of phosphodiesterase-4: The present invention is also directed to a method of preparing phosphodiesterase inhibitors comprising the Formula (IX, IXa).
摘要翻译： 一方面，本发明涉及一种制备式（V）中间体的一锅法，其可用于制备磷酸二酯酶-4的抑制剂：本发明还涉及一种制备磷酸二酯酶抑制剂的方法，其包含式 （IX，IXa）。
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公开(公告)号：US20060019981A1
公开(公告)日：2006-01-26
申请号：US10530465
申请日：2003-11-18
IPC分类号： C07D471/02 , A61K31/4745
CPC分类号： C07D471/04
摘要： In one aspect, the present invention is directed to a one pot method of preparing intermediates of Formula (V), which are useful in making inhibitors of phosphodiesterase-4: The present invention is also directed to a method of preparing phosphodiesterase inhibitors comprising the Formula (IX, IXa)
摘要翻译： 一方面，本发明涉及一种制备式（V）中间体的一锅法，其可用于制备磷酸二酯酶-4的抑制剂：本发明还涉及一种制备磷酸二酯酶抑制剂的方法，其包含式 （IX，IXa）
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公开(公告)号：US20090012061A1
公开(公告)日：2009-01-08
申请号：US11662396
申请日：2005-09-09
申请人： Timothy A. Blizzard , Carolyn A. Buser-Doepner , Douglas E. Frantz , Kelly Hamilton , Myle Hoang , Ling Lee , Christopher R. Moyes , Jerry A. Murry , Arash Soheili
发明人： Timothy A. Blizzard , Carolyn A. Buser-Doepner , Douglas E. Frantz , Kelly Hamilton , Myle Hoang , Ling Lee , Christopher R. Moyes , Jerry A. Murry , Arash Soheili
IPC分类号： G01N33/574 , C12N9/99 , A61K31/403 , A61K31/428 , C07C271/06 , A61K31/27 , A61K31/47 , C07D215/38 , C07C39/12 , A61K31/05 , C07C275/28 , A61K31/17 , A61K31/165 , A61K31/415 , A61K31/44 , A61K31/5415 , A61K31/551 , A61P35/00
CPC分类号： C12Q1/42 , G01N33/6893 , G01N2500/00
摘要： The present invention relates to a method of treating cellular proliferative diseases, in particular cancer, which comprises administering a modulator of the activity of the mitotic kinesin KSP, wherein the activity of the KSP modulator is dependent on the presence of microtubules. It is believed that the KSP modulators utilized in the instant method bind to the KSP protein in a previously unreported manner, since the compounds do not bind competitively with respect to either microtubules or ATP, the substrates of KSP. The modulators useful in the instant methods are furthermore not active against the non-microtubule stimulated activity of KSP. Cellular proliferative diseases that may be treated using the method disclosed herein are, for example cancer, hyperplasias, restenosis, cardiac hypertrophy, immune disorders and inflammation.
摘要翻译： 本发明涉及一种治疗细胞增殖性疾病，特别是癌症的方法，其包括施用有丝分裂驱动蛋白KSP活性的调节剂，其中KSP调节剂的活性取决于微管的存在。 相信本方法中使用的KSP调节剂以先前未报道的方式结合KSP蛋白质，因为化合物相对于微管或ATP（KSP的底物）竞争性结合。 在本方法中有用的调节剂还不能抵抗KSP的非微管刺激活性。 可以使用本文公开的方法治疗的细胞增殖性疾病是例如癌症，增生，再狭窄，心脏肥大，免疫疾病和炎症。
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