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1.发明授权公开(公告)号：US08563279B2
公开(公告)日：2013-10-22
申请号：US12810220
申请日：2008-12-19
申请人： Ben De Lange , Anna Maria Cornelia Francisca Castelijns , Johannes Gerardus De Vries , Andreas Hendrikus Maria De Vries , Jeroen Antonius Franciscus Boogers , Quirinus Bernardus Broxterman
发明人： Ben De Lange , Anna Maria Cornelia Francisca Castelijns , Johannes Gerardus De Vries , Andreas Hendrikus Maria De Vries , Jeroen Antonius Franciscus Boogers , Quirinus Bernardus Broxterman
IPC分类号： C07C231/18 , C07C253/16 , C07C255/20 , C07F1/02 , C07F7/18 , C07D307/32 , C07D307/33 , C12P13/00
CPC分类号： C07D307/33 , C07C231/02 , C07C231/18 , C07D307/32 , C07F1/02 , C07F7/1804 , C07C237/22
摘要： Described is a method for the preparation of renin inhibitors such as aliskiren, and intermediates useful therein. The method introduces a nitrogen-containing intermediate such as a lactone of formula (8). with R4 being a branched C3—6 alkyl. In the preparation of the lactone, or related intermediates, a desired stereochemical configuration can be controlled by starting from a chiral aldehyde satisfying formula (10).
摘要翻译： 描述了制备肾素抑制剂如阿利吉仑的方法和其中有用的中间体。 该方法引入含氮中间体如式（8）的内酯。 其中R4是支链C 3-6烷基。 在内酯或相关中间体的制备中，可以通过从满足式（10）的手性醛开始来控制所需的立体化学构型。
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公开(公告)号：US08088954B2
公开(公告)日：2012-01-03
申请号：US12668232
申请日：2008-07-11
申请人： Gerardus Karel Maria Verzijl , Henricus Martinus Maria Gerardus Straatman , Andreas Hendrikus Maria De Vries , Lizette Schmieder , Jeroen Antonius Franciscus Boogers
发明人： Gerardus Karel Maria Verzijl , Henricus Martinus Maria Gerardus Straatman , Andreas Hendrikus Maria De Vries , Lizette Schmieder , Jeroen Antonius Franciscus Boogers
IPC分类号： C07C47/105 , C07C45/67 , C07C41/18
CPC分类号： C07C47/277 , C07C37/002 , C07C37/62 , C07C41/22 , C07C41/26 , C07C45/562 , C07C45/62 , C07C47/27 , C07C69/78 , C07C309/73 , C12P7/04 , C12P7/24 , C07C43/23 , C07C43/225 , C07C39/373 , C07C39/24 , C07C39/11
摘要： The invention relates to a compound according to Formula (IX) and salts thereof, wherein R1, R2 and R5 are each independently selected from H and hydrocarbon moieties, which hydrocarbon moieties optionally comprise one or more heteroatoms, and which hydrocarbons optionally comprise substituents, or when the compound according to formula (IX) is a salt, R1 and/or R2 may be a cation, R3, and R4 each independently selected from hydrocarbon moieties, which hydrocarbon moieties optionally comprise one or more heteroatoms, and which hydrocarbons optionally comprise substituents, and wherein any two of R1, R2, R3, R4 and R5 are optionally linked together to form a ring structure. The invention further relates to the preparation of such a compound and to the use of such a compound for preparing a pharmaceutical compound, an agrochemical compound, an intermediate for a pharmaceutical compound or an intermediate for an agrochemical compound.
摘要翻译： 本发明涉及式（IX）化合物及其盐，其中R 1，R 2和R 5各自独立地选自H和烃部分，该烃部分任选地包含一个或多个杂原子，并且该烃任选地包含取代基，或 当式（IX）化合物为盐时，R 1和/或R 2可以是阳离子，R 3和R 4各自独立地选自烃部分，该烃部分任选地包含一个或多个杂原子，并且该烃任选地包含取代基 并且其中R 1，R 2，R 3，R 4和R 5中的任何两个任选地连接在一起以形成环结构。 本发明还涉及这种化合物的制备以及这种化合物用于制备药物化合物，农药化合物，药物化合物的中间体或农药化合物的中间体的用途。
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公开(公告)号：US20110294171A1
公开(公告)日：2011-12-01
申请号：US13205442
申请日：2011-08-08
申请人： Gerardus Karel Maria Verzijl , Henricus Martinus Maria Gerardus Straatman , Andreas Hendrikus Maria De Vries , Lizette Schmieder , Jeroen Antonius Franciscus Boogers
发明人： Gerardus Karel Maria Verzijl , Henricus Martinus Maria Gerardus Straatman , Andreas Hendrikus Maria De Vries , Lizette Schmieder , Jeroen Antonius Franciscus Boogers
CPC分类号： C07C47/277 , C07C37/002 , C07C37/62 , C07C41/22 , C07C41/26 , C07C45/562 , C07C45/62 , C07C47/27 , C07C69/78 , C07C309/73 , C12P7/04 , C12P7/24 , C07C43/23 , C07C43/225 , C07C39/373 , C07C39/24 , C07C39/11
摘要： The invention relates to a compound according to Formula (IX) and salts thereof, wherein R1, R2 and R5 are each independently selected from H and hydrocarbon moieties, which hydrocarbon moieties optionally comprise one or more heteroatoms, and which hydrocarbons optionally comprise substituents, or when the compound according to formula (IX) is a salt, R1 and/or R2 may be a cation, R3, and R4 each independently selected from hydrocarbon moieties, which hydrocarbon moieties optionally comprise one or more heteroatoms, and which hydrocarbons optionally comprise substituents, and wherein any two of R1, R2, R3, R4 and R5 are optionally linked together to form a ring structure. The invention further relates to the preparation of such a compound and to the use of such a compound for preparing a pharmaceutical compound, an agrochemical compound, an intermediate for a pharmaceutical compound or an intermediate for an agrochemical compound.
摘要翻译： 本发明涉及式（IX）化合物及其盐，其中R 1，R 2和R 5各自独立地选自H和烃部分，该烃部分任选地包含一个或多个杂原子，并且该烃任选地包含取代基，或 当式（IX）化合物为盐时，R 1和/或R 2可以是阳离子，R 3和R 4各自独立地选自烃部分，该烃部分任选地包含一个或多个杂原子，并且该烃任选地包含取代基 并且其中R 1，R 2，R 3，R 4和R 5中的任何两个任选地连接在一起以形成环结构。 本发明还涉及这种化合物的制备以及这种化合物用于制备药物化合物，农药化合物，药物化合物的中间体或农药化合物的中间体的用途。
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公开(公告)号：US20100197972A1
公开(公告)日：2010-08-05
申请号：US12668232
申请日：2008-07-11
申请人： Gerardus Karel Maria Verzijl , Henricus Martinus Maria Gerardus Straatman , Andreas Hendrikus Maria De Vries , Lizette Schmieder , Jeroen Antonius Franciscus Boogers
发明人： Gerardus Karel Maria Verzijl , Henricus Martinus Maria Gerardus Straatman , Andreas Hendrikus Maria De Vries , Lizette Schmieder , Jeroen Antonius Franciscus Boogers
IPC分类号： C07C47/105 , C07C45/67 , C12P7/24 , C07C41/18 , C07C41/22
CPC分类号： C07C47/277 , C07C37/002 , C07C37/62 , C07C41/22 , C07C41/26 , C07C45/562 , C07C45/62 , C07C47/27 , C07C69/78 , C07C309/73 , C12P7/04 , C12P7/24 , C07C43/23 , C07C43/225 , C07C39/373 , C07C39/24 , C07C39/11
摘要： The invention relates to a compound according to Formula (IX) and salts thereof, wherein R1, R2 and R5 are each independently selected from H and hydrocarbon moieties, which hydrocarbon moieties optionally comprise one or more heteroatoms, and which hydrocarbons optionally comprise substituents, or when the compound according to formula (IX) is a salt, R1 and/or R2 may be a cation, R3, and R4 each independently selected from hydrocarbon moieties, which hydrocarbon moieties optionally comprise one or more heteroatoms, and which hydrocarbons optionally comprise substituents, and wherein any two of R1, R2, R3, R4 and R5 are optionally linked together to form a ring structure. The invention further relates to the preparation of such a compound and to the use of such a compound for preparing a pharmaceutical compound, an agrochemical compound, an intermediate for a pharmaceutical compound or an intermediate for an agrochemical compound.
摘要翻译： 本发明涉及式（IX）化合物及其盐，其中R 1，R 2和R 5各自独立地选自H和烃部分，该烃部分任选地包含一个或多个杂原子，并且该烃任选地包含取代基，或 当式（IX）化合物为盐时，R 1和/或R 2可以是阳离子，R 3和R 4各自独立地选自烃部分，该烃部分任选地包含一个或多个杂原子，并且该烃任选地包含取代基 并且其中R 1，R 2，R 3，R 4和R 5中的任何两个任选地连接在一起以形成环结构。 本发明还涉及这种化合物的制备以及这种化合物用于制备药物化合物，农药化合物，药物化合物的中间体或农药化合物的中间体的用途。
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