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1. 发明申请

WO00066598A1 IMPROVED PREPARATIONS OF THIOPHOSPHITES AND THIOPHOSPHONATES 审中-公开
标题翻译：改善硫代磷酸酯和硫代磷酸酯的制备
公开(公告)号：WO00066598A1
公开(公告)日：2000-11-09
申请号：PCT/US2000/011940
申请日：2000-05-03
IPC分类号： C07F9/201 , C07F9/40 , C07F9/16
CPC分类号： C07F9/4065 , C07F9/201
摘要： Improved methods for converting phosphite or phosphonate esters into corresponding thiophosphites or thiophosphonates and for synthesizing specific thiophosphite and thiophosphonate compounds so produced are disclosed and claimed. The methods start from phosphite diesters using P4S10 as the thionation reagent. The reaction mixture is refluxed until the reaction is complete and may be followed by separation and chloroformate ester phosphonation steps to produce pure thiophosphonocarboxylate triesters. Alternatively, these esters may be prepared directly by action of P4S10 on the corresponding phosphonocarboxylate esters. The former method was used to prepare dimethyl thiophosphite and thence trimethyl thiophosphonoformate, a key intermediate in synthesis of salts of thiophosphonoformic acid, which have anti-viral properties.
摘要翻译：公开和要求保护的方法将亚磷酸酯或膦酸酯转化成相应的硫代亚磷酸酯或硫代膦酸酯并合成特定的硫代亚磷酸酯和硫代膦酸酯化合物。该方法从使用P4S10作为硫化试剂的亚磷酸二酯开始。将反应混合物回流直到反应完成，然后分离和氯甲酸酯膦酸化步骤以产生纯的硫代膦酰基羧酸酯三酯。或者，这些酯可以通过P4S10在相应的膦酰基羧酸酯上的作用直接制备。使用前一种方法制备二硫代亚磷酸二甲酯，然后制备硫代膦酰甲酸三甲酯，这是合成硫代膦酰甲酸盐的关键中间体，具有抗病毒性质。

2. 发明申请

WO2006044825A3 MITOTIC KINESIN INHIBITORS AND METHODS OF USE THEREOF 审中-公开
标题翻译： MITOTIC KINESIN INHIBITORS及其使用方法
公开(公告)号：WO2006044825A3
公开(公告)日：2006-10-05
申请号：PCT/US2005037305
申请日：2005-10-18
申请人： ARRAY BIOPHARMA INC , HANS JEREMY , WALLACE ELI M , ZHAO QIAN , LYSSIKATOS JOSEPH P , AICHER TOM , LAIRD ELLEN , ROBINSON JOHN , ALLEN SHELLEY
发明人： HANS JEREMY , WALLACE ELI M , ZHAO QIAN , LYSSIKATOS JOSEPH P , AICHER TOM , LAIRD ELLEN , ROBINSON JOHN , ALLEN SHELLEY
IPC分类号： A61K31/4245 , C07D413/00 , C07D417/00
CPC分类号： C07D285/12 , C07D271/107 , C07D401/12 , C07D413/04 , C07D413/06 , C07D413/12 , C07D417/04 , C07D417/06 , C07D417/12 , C07F9/201 , C07F9/65392
摘要： This invention relates to inhibitors of mitotic kinesins, particularly KSP, and methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing the inhibitors and pharmaceutical compositions in the treatment and prevention of various disorders.
摘要翻译：本发明涉及有丝分裂驱动蛋白抑制剂，特别是KSP，以及制备这些抑制剂的方法。本发明还提供包含本发明抑制剂的药物组合物和利用抑制剂和药物组合物治疗和预防各种疾病的方法。

3. 发明申请

WO2006044825A2 MITOTIC KINESIN INHIBITORS AND METHODS OF USE THEREOF 审中-公开
公开(公告)号：WO2006044825A2
公开(公告)日：2006-04-27
申请号：PCT/US2005/037305
申请日：2005-10-18
申请人： ARRAY BIOPHARMA INC. , HANS, Jeremy , WALLACE, Eli, M. , WALLACE, Eli, M. , ZHAO, Qian , LYSSIKATOS, Joseph, P. , AICHER, Tom , LAIRD, Ellen , ROBINSON, John , ALLEN, Shelley
发明人： HANS, Jeremy , WALLACE, Eli, M. , WALLACE, Eli, M. , ZHAO, Qian , LYSSIKATOS, Joseph, P. , AICHER, Tom , LAIRD, Ellen , ROBINSON, John , ALLEN, Shelley
IPC分类号： A61K38/04 , A61K31/675 , A61K31/496 , A61K31/4439 , A61K31/433 , A61K31/4245 , C07D417/04 , C07D413/04
CPC分类号： C07D285/12 , C07D271/107 , C07D401/12 , C07D413/04 , C07D413/06 , C07D413/12 , C07D417/04 , C07D417/06 , C07D417/12 , C07F9/201 , C07F9/65392
摘要： This invention relates to inhibitors of mitotic kinesins, particularly KSP, and methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing the inhibitors and pharmaceutical compositions in the treatment and prevention of various disorders.

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