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11.发明授权Substituted n-benzyl-n-phenyl aminoalcohol compounds useful for inhibiting cholesteryl ester transfer protein activity 失效用于抑制胆固醇酯转移蛋白活性的取代的正苄基 - 正 - 苯基氨基醇化合物公开(公告)号：US06723753B2
公开(公告)日：2004-04-20
申请号：US10071518
申请日：2002-02-07
申请人： James A. Sikorski , Richard C. Durley , Deborah A. Mischke , Emily J. Reinhard , Yvette M. Fobian , Michael B. Tollefson , Lijuan Wang , Margaret L. Grapperhaus , Brian S. Hickory , Mark A. Massa , Monica B. Norton , William F. Vernier , Barry L. Parnas , Michele A. Promo , Ashton T. Hamme , Dale P. Spangler , Melvin L. Rueppel
发明人： James A. Sikorski , Richard C. Durley , Deborah A. Mischke , Emily J. Reinhard , Yvette M. Fobian , Michael B. Tollefson , Lijuan Wang , Margaret L. Grapperhaus , Brian S. Hickory , Mark A. Massa , Monica B. Norton , William F. Vernier , Barry L. Parnas , Michele A. Promo , Ashton T. Hamme , Dale P. Spangler , Melvin L. Rueppel
IPC分类号： A61K3137
CPC分类号： C07C323/25 , B01D2201/345 , C07B2200/07 , C07C215/08 , C07C215/16 , C07C217/58 , C07C217/84 , C07C217/88 , C07C217/90 , C07C217/92 , C07C219/06 , C07C219/28 , C07C219/34 , C07C225/22 , C07C229/38 , C07C229/52 , C07C229/60 , C07C233/25 , C07C233/43 , C07C233/69 , C07C233/80 , C07C235/20 , C07C235/24 , C07C235/56 , C07C237/30 , C07C237/38 , C07C255/13 , C07C255/21 , C07C255/24 , C07C255/54 , C07C255/58 , C07C271/28 , C07C275/34 , C07C275/40 , C07C311/21 , C07C311/58 , C07C317/32 , C07C317/36 , C07C323/19 , C07C323/20 , C07C323/31 , C07C323/32 , C07C323/37 , C07C323/44 , C07C323/65 , C07C327/30 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07C2603/18 , C07D207/335 , C07D209/82 , C07D213/38 , C07D213/62 , C07D225/08 , C07D239/26 , C07D239/34 , C07D251/46 , C07D257/04 , C07D263/04 , C07D265/14 , C07D295/088 , C07D295/108 , C07D295/135 , C07D295/192 , C07D307/04 , C07D307/38 , C07D333/20 , C07D333/28 , C07D491/10
摘要： The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N-benzyl-N-phenyl aminoalcohols. A preferred specific N-benzyl-N-phenyl aminoalcohol is the compound:
摘要翻译： 本发明涉及可用作胆固醇酯转移蛋白（CETP;血浆脂质转移蛋白-I）抑制剂的取代多环芳基和杂芳基叔杂烷基胺化合物以及用于治疗动脉粥样硬化和其它冠状动脉疾病的化合物，组合物和方法。 优选的叔杂烷基胺化合物是取代的N-苄基-N-苯基氨基醇。 优选的特定N-苄基-N-苯基氨基醇是化合物：
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12.发明授权Substituted N,N-disubstituted fused-heterocyclo amino compounds useful for inhibiting cholesteryl ester transfer protein activity 失效用于抑制胆固醇酯转移蛋白活性的取代的N，N-二取代的稠合 - 杂环氨基化合物公开(公告)号：US06696435B2
公开(公告)日：2004-02-24
申请号：US10154861
申请日：2002-05-23
申请人： James A. Sikorski , Richard C. Durley , Deborah A. Mischke , Emily J. Reinhard , Yvette M. Fobian , Michael B. Tollefson , Lijuan Wang , Margaret L. Grapperhaus , Brian S. Hickory , Mark A. Massa , Monica B. Norton , William F. Vernier , Barry L. Parnas , Michele A. Promo , Ashton T. Hamme , Dale P. Spangler , Melvin L. Rueppel
发明人： James A. Sikorski , Richard C. Durley , Deborah A. Mischke , Emily J. Reinhard , Yvette M. Fobian , Michael B. Tollefson , Lijuan Wang , Margaret L. Grapperhaus , Brian S. Hickory , Mark A. Massa , Monica B. Norton , William F. Vernier , Barry L. Parnas , Michele A. Promo , Ashton T. Hamme , Dale P. Spangler , Melvin L. Rueppel
IPC分类号： A61K31536
CPC分类号： C07C323/25 , B01D2201/345 , C07B2200/07 , C07C215/08 , C07C215/16 , C07C217/58 , C07C217/84 , C07C217/88 , C07C217/90 , C07C217/92 , C07C219/06 , C07C219/28 , C07C219/34 , C07C225/22 , C07C229/38 , C07C229/52 , C07C229/60 , C07C233/25 , C07C233/43 , C07C233/69 , C07C233/80 , C07C235/20 , C07C235/24 , C07C235/56 , C07C237/30 , C07C237/38 , C07C255/13 , C07C255/21 , C07C255/24 , C07C255/54 , C07C255/58 , C07C271/28 , C07C275/34 , C07C275/40 , C07C311/21 , C07C311/58 , C07C317/32 , C07C317/36 , C07C323/19 , C07C323/20 , C07C323/31 , C07C323/32 , C07C323/37 , C07C323/44 , C07C323/65 , C07C327/30 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07C2603/18 , C07D207/335 , C07D209/82 , C07D213/38 , C07D213/62 , C07D225/08 , C07D239/26 , C07D239/34 , C07D251/46 , C07D257/04 , C07D263/04 , C07D265/14 , C07D295/088 , C07D295/108 , C07D295/135 , C07D295/192 , C07D307/04 , C07D307/38 , C07D333/20 , C07D333/28 , C07D491/10
摘要： The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N,N-disubstituted fused-heterocyclo amines. A preferred specific N,N-disubstituted fused-heterocyclo amine is the compound:
摘要翻译： 本发明涉及可用作胆固醇酯转移蛋白（CETP;血浆脂质转移蛋白-I）抑制剂的取代多环芳基和杂芳基叔杂烷基胺化合物以及用于治疗动脉粥样硬化和其它冠状动脉疾病的化合物，组合物和方法。 优选的叔杂烷基胺化合物是取代的N，N-二取代的稠合 - 杂环胺。 优选的具体的N，N-二取代稠合 - 杂环胺是化合物：
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公开(公告)号：US20030105100A1
公开(公告)日：2003-06-05
申请号：US10155451
申请日：2002-05-23
申请人： G.D. Searle & Co.
发明人： James A. Sikorski , Richard C. Durley , Deborah A. Mischke , Emily J. Reinhard , Yvette M. Fobian , Michael B. Tollefson , Lijuan Wang , Margaret L. Grapperhaus , Brian S. Hickory , Mark A. Massa , Monica B. Norton , William F. Vernier , Barry L. Parnas , Michele A. Promo , Ashton T. Hamme , Dale P. Spangler , Melvin L. Rueppel
IPC分类号： C07D43/02 , C07D41/02 , A61K031/53 , A61K031/506 , A61K031/501 , A61K031/497
CPC分类号： C07C323/25 , B01D2201/345 , C07B2200/07 , C07C215/08 , C07C215/16 , C07C217/58 , C07C217/84 , C07C217/88 , C07C217/90 , C07C217/92 , C07C219/06 , C07C219/28 , C07C219/34 , C07C225/22 , C07C229/38 , C07C229/52 , C07C229/60 , C07C233/25 , C07C233/43 , C07C233/69 , C07C233/80 , C07C235/20 , C07C235/24 , C07C235/56 , C07C237/30 , C07C237/38 , C07C255/13 , C07C255/21 , C07C255/24 , C07C255/54 , C07C255/58 , C07C271/28 , C07C275/34 , C07C275/40 , C07C311/21 , C07C311/58 , C07C317/32 , C07C317/36 , C07C323/19 , C07C323/20 , C07C323/31 , C07C323/32 , C07C323/37 , C07C323/44 , C07C323/65 , C07C327/30 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07C2603/18 , C07D207/335 , C07D209/82 , C07D213/38 , C07D213/62 , C07D225/08 , C07D239/26 , C07D239/34 , C07D251/46 , C07D257/04 , C07D263/04 , C07D265/14 , C07D295/088 , C07D295/108 , C07D295/135 , C07D295/192 , C07D307/04 , C07D307/38 , C07D333/20 , C07D333/28 , C07D491/10
摘要： The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases.
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14.发明授权Use of substituted N, N-bis-benzyl aminoalcohol compounds inhibiting cholesteryl ester transfer protein activity 失效使用取代的N，N-双苄基氨基醇化合物抑制胆固醇酯转移蛋白活性公开(公告)号：US06476075B1
公开(公告)日：2002-11-05
申请号：US09991301
申请日：2001-11-14
申请人： James A. Sikorski , Richard C. Durley , Deborah A. Mischke , Emily J. Reinhard , Yvette M. Fobian , Michael B. Tollefson , Lijuan Wang , Margaret L. Grapperhaus , Brian S. Hickory , Mark A. Massa , Monica B. Norton , William F. Vernier , Barry L. Parnas , Michele A. Promo , Ashton T. Hamme , Dale P. Spangler , Melvin L. Rueppel
发明人： James A. Sikorski , Richard C. Durley , Deborah A. Mischke , Emily J. Reinhard , Yvette M. Fobian , Michael B. Tollefson , Lijuan Wang , Margaret L. Grapperhaus , Brian S. Hickory , Mark A. Massa , Monica B. Norton , William F. Vernier , Barry L. Parnas , Michele A. Promo , Ashton T. Hamme , Dale P. Spangler , Melvin L. Rueppel
IPC分类号： A61K31137
CPC分类号： C07C323/25 , B01D2201/345 , C07B2200/07 , C07C215/08 , C07C215/16 , C07C217/58 , C07C217/84 , C07C217/88 , C07C217/90 , C07C217/92 , C07C219/06 , C07C219/28 , C07C219/34 , C07C225/22 , C07C229/38 , C07C229/52 , C07C229/60 , C07C233/25 , C07C233/43 , C07C233/69 , C07C233/80 , C07C235/20 , C07C235/24 , C07C235/56 , C07C237/30 , C07C237/38 , C07C255/13 , C07C255/21 , C07C255/24 , C07C255/54 , C07C255/58 , C07C271/28 , C07C275/34 , C07C275/40 , C07C311/21 , C07C311/58 , C07C317/32 , C07C317/36 , C07C323/19 , C07C323/20 , C07C323/31 , C07C323/32 , C07C323/37 , C07C323/44 , C07C323/65 , C07C327/30 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07C2603/18 , C07D207/335 , C07D209/82 , C07D213/38 , C07D213/62 , C07D225/08 , C07D239/26 , C07D239/34 , C07D251/46 , C07D257/04 , C07D263/04 , C07D265/14 , C07D295/088 , C07D295/108 , C07D295/135 , C07D295/192 , C07D307/04 , C07D307/38 , C07D333/20 , C07D333/28 , C07D491/10
摘要： The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N,N-bis-benzyl aminoalcohols. A preferred specific N,N-bis-benzyl aminoalcohol is the compound:
摘要翻译： 本发明涉及可用作胆固醇酯转移蛋白（CETP;血浆脂质转移蛋白-I）抑制剂的取代多环芳基和杂芳基叔杂烷基胺化合物以及用于治疗动脉粥样硬化和其它冠状动脉疾病的化合物，组合物和方法。 优选的叔杂烷基胺化合物是取代的N，N-双苄基氨基醇。 优选的具体的N，N-双苄基氨基醇是化合物：
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15.发明授权Use of substituted N, N-disubstituted cycloalkyl aminoalcohol compounds for inhibiting cholesteryl ester transfer protein activity 失效使用取代的N，N-二取代的环烷基氨基醇化合物抑制胆固醇酯转移蛋白活性公开(公告)号：US06476057B1
公开(公告)日：2002-11-05
申请号：US09990833
申请日：2001-11-14
申请人： James A. Sikorski , Richard C. Durley , Deborah A. Mischke , Emily J. Reinhard , Yvette M. Fobian , Michael B. Tollefson , Lijuan Wang , Margaret L. Grapperhaus , Brian S. Hickory , Mark A. Massa , Monica B. Norton , William F. Vernier , Barry L. Parnas , Michele A. Promo , Ashton T. Hamme , Dale P. Spangler , Melvin L. Rueppel
发明人： James A. Sikorski , Richard C. Durley , Deborah A. Mischke , Emily J. Reinhard , Yvette M. Fobian , Michael B. Tollefson , Lijuan Wang , Margaret L. Grapperhaus , Brian S. Hickory , Mark A. Massa , Monica B. Norton , William F. Vernier , Barry L. Parnas , Michele A. Promo , Ashton T. Hamme , Dale P. Spangler , Melvin L. Rueppel
IPC分类号： A61K31133
CPC分类号： C07C323/25 , B01D2201/345 , C07B2200/07 , C07C215/08 , C07C215/16 , C07C217/58 , C07C217/84 , C07C217/88 , C07C217/90 , C07C217/92 , C07C219/06 , C07C219/28 , C07C219/34 , C07C225/22 , C07C229/38 , C07C229/52 , C07C229/60 , C07C233/25 , C07C233/43 , C07C233/69 , C07C233/80 , C07C235/20 , C07C235/24 , C07C235/56 , C07C237/30 , C07C237/38 , C07C255/13 , C07C255/21 , C07C255/24 , C07C255/54 , C07C255/58 , C07C271/28 , C07C275/34 , C07C275/40 , C07C311/21 , C07C311/58 , C07C317/32 , C07C317/36 , C07C323/19 , C07C323/20 , C07C323/31 , C07C323/32 , C07C323/37 , C07C323/44 , C07C323/65 , C07C327/30 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07C2603/18 , C07D207/335 , C07D209/82 , C07D213/38 , C07D213/62 , C07D225/08 , C07D239/26 , C07D239/34 , C07D251/46 , C07D257/04 , C07D263/04 , C07D265/14 , C07D295/088 , C07D295/108 , C07D295/135 , C07D295/192 , C07D307/04 , C07D307/38 , C07D333/20 , C07D333/28 , C07D491/10
摘要： The invention relates to use of substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N,N-disubstituted cycloalkyl aminoalcohols. A preferred specific N,N-disubstituted cycloalkyl aminoalcohol is the compound:
摘要翻译： 本发明涉及可用作胆固醇酯转移蛋白（CETP;血浆脂质转移蛋白-1）的抑制剂的取代多环芳基和杂芳基叔杂烷基胺化合物的用途以及用于治疗动脉粥样硬化和其它冠状动脉疾病的化合物，组合物和方法。 优选的叔杂烷基胺化合物是取代的N，N-二取代的环烷基氨基醇。 优选的具体的N，N-二取代的环烷基氨基醇是化合物：
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16.发明授权Use of substituted N,N-disubstituted non-fused heterocyclo amino compounds for inhibiting cholesteryl ester transfer protein activity 失效取代的N，N-二取代的非稠合杂环氨基化合物用于抑制胆固醇酯转移蛋白活性的用途公开(公告)号：US06451830B1
公开(公告)日：2002-09-17
申请号：US09991085
申请日：2001-11-14
申请人： James A. Sikorski , Richard C. Durley , Deborah A. Mischke , Emily J. Reinhard , Yvette M. Fobian , Michael B. Tollefson , Lijuan Wang , Margaret L. Grapperhaus , Brian S. Hickory , Mark A. Massa , Monica B. Norton , William F. Vernier , Barry L. Parnas , Michele A. Promo , Ashton T. Hamme , Dale P. Spangler , Melvin L. Rueppel
发明人： James A. Sikorski , Richard C. Durley , Deborah A. Mischke , Emily J. Reinhard , Yvette M. Fobian , Michael B. Tollefson , Lijuan Wang , Margaret L. Grapperhaus , Brian S. Hickory , Mark A. Massa , Monica B. Norton , William F. Vernier , Barry L. Parnas , Michele A. Promo , Ashton T. Hamme , Dale P. Spangler , Melvin L. Rueppel
IPC分类号： A61K31421
CPC分类号： C07C323/25 , B01D2201/345 , C07B2200/07 , C07C215/08 , C07C215/16 , C07C217/58 , C07C217/84 , C07C217/88 , C07C217/90 , C07C217/92 , C07C219/06 , C07C219/28 , C07C219/34 , C07C225/22 , C07C229/38 , C07C229/52 , C07C229/60 , C07C233/25 , C07C233/43 , C07C233/69 , C07C233/80 , C07C235/20 , C07C235/24 , C07C235/56 , C07C237/30 , C07C237/38 , C07C255/13 , C07C255/21 , C07C255/24 , C07C255/54 , C07C255/58 , C07C271/28 , C07C275/34 , C07C275/40 , C07C311/21 , C07C311/58 , C07C317/32 , C07C317/36 , C07C323/19 , C07C323/20 , C07C323/31 , C07C323/32 , C07C323/37 , C07C323/44 , C07C323/65 , C07C327/30 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07C2603/18 , C07D207/335 , C07D209/82 , C07D213/38 , C07D213/62 , C07D225/08 , C07D239/26 , C07D239/34 , C07D251/46 , C07D257/04 , C07D263/04 , C07D265/14 , C07D295/088 , C07D295/108 , C07D295/135 , C07D295/192 , C07D307/04 , C07D307/38 , C07D333/20 , C07D333/28 , C07D491/10
摘要： The invention relates to use of substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N,N-disubstituted non-fused heterocyclo amines. A preferred specific N,N-disubstituted non-fused heterocyclo amine is the compound:
摘要翻译： 本发明涉及可用作胆固醇酯转移蛋白（CETP;血浆脂质转移蛋白-1）的抑制剂的取代多环芳基和杂芳基叔杂烷基胺化合物的用途以及用于治疗动脉粥样硬化和其它冠状动脉疾病的化合物，组合物和方法。 优选的叔杂烷基胺化合物是取代的N，N-二取代的非稠合杂环胺。 优选的具体的N，N-二取代的非稠合杂环胺是化合物：
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17.发明授权Use of substituted N-phenoxy-N-phenyl aminoalcohol compounds for inhibiting cholesteryl ester transfer protein activity 失效使用取代的N-苯氧基-N-苯基氨基醇化合物抑制胆固醇酯转移蛋白活性公开(公告)号：US06451823B1
公开(公告)日：2002-09-17
申请号：US09990645
申请日：2001-11-14
申请人： James A. Sikorski , Richard C. Durley , Deborah A. Mischke , Emily J. Reinhard , Yvette M. Fobian , Michael B. Tollefson , Lijuan Wang , Margaret L. Grapperhaus , Brian S. Hickory , Mark A. Massa , Monica B. Norton , William F. Vernier , Barry L. Parnas , Michele A. Promo , Ashton T. Hamme , Dale P. Spangler , Melvin L. Rueppel
发明人： James A. Sikorski , Richard C. Durley , Deborah A. Mischke , Emily J. Reinhard , Yvette M. Fobian , Michael B. Tollefson , Lijuan Wang , Margaret L. Grapperhaus , Brian S. Hickory , Mark A. Massa , Monica B. Norton , William F. Vernier , Barry L. Parnas , Michele A. Promo , Ashton T. Hamme , Dale P. Spangler , Melvin L. Rueppel
IPC分类号： C07C23300
CPC分类号： C07C323/25 , B01D2201/345 , C07B2200/07 , C07C215/08 , C07C215/16 , C07C217/58 , C07C217/84 , C07C217/88 , C07C217/90 , C07C217/92 , C07C219/06 , C07C219/28 , C07C219/34 , C07C225/22 , C07C229/38 , C07C229/52 , C07C229/60 , C07C233/25 , C07C233/43 , C07C233/69 , C07C233/80 , C07C235/20 , C07C235/24 , C07C235/56 , C07C237/30 , C07C237/38 , C07C255/13 , C07C255/21 , C07C255/24 , C07C255/54 , C07C255/58 , C07C271/28 , C07C275/34 , C07C275/40 , C07C311/21 , C07C311/58 , C07C317/32 , C07C317/36 , C07C323/19 , C07C323/20 , C07C323/31 , C07C323/32 , C07C323/37 , C07C323/44 , C07C323/65 , C07C327/30 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07C2603/18 , C07D207/335 , C07D209/82 , C07D213/38 , C07D213/62 , C07D225/08 , C07D239/26 , C07D239/34 , C07D251/46 , C07D257/04 , C07D263/04 , C07D265/14 , C07D295/088 , C07D295/108 , C07D295/135 , C07D295/192 , C07D307/04 , C07D307/38 , C07D333/20 , C07D333/28 , C07D491/10
摘要： The invention relates to use of substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N-phenoxy-N-phenyl aminoalcohols. A preferred specific N-phenoxy-N-phenyl aminoalcohol is the compound:
摘要翻译： 本发明涉及可用作胆固醇酯转移蛋白（CETP;血浆脂质转移蛋白-1）的抑制剂的取代多环芳基和杂芳基叔杂烷基胺化合物的用途以及用于治疗动脉粥样硬化和其它冠状动脉疾病的化合物，组合物和方法。 优选的叔杂烷基胺化合物是取代的N-苯氧基-N-苯基氨基醇。 优选的特定N-苯氧基-N-苯基氨基醇是化合物：
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公开(公告)号：US06194443B1
公开(公告)日：2001-02-27
申请号：US09284225
申请日：1999-04-09
IPC分类号： A61K3154
CPC分类号： C07D213/80 , A01N43/06 , A01N43/32 , A01N43/40 , A01N43/56 , A01N43/78 , A01N43/80 , A01N47/12 , C07C219/34 , C07C271/16 , C07C2601/14 , C07D231/14 , C07D275/03 , C07D295/205 , C07D307/30 , C07D307/56 , C07D307/68 , C07D327/06 , C07D333/24 , C07D333/38 , C07D333/60
摘要： The present invention pertains to new aminophenol derivatives of the following general formula (1), their preparation and their use as fungicides. wherein Y1, Y2, Y3, Y4, R1, and Z are as defined in the description.
摘要翻译： 本发明涉及以下通式（1）的新氨基苯酚衍生物及其制备方法及其作为杀真菌剂的用途，其中Y1，Y2，Y3，Y4，R1和Z如说明书中所定义。
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19.发明授权Bacterial nitroreductase for the reduction of CB1954 and analogues thereof to a cytotoxic form 失效用于将CB1954及其类似物还原成细胞毒性形式的细菌硝基还原酶
公开(公告)号：US5977065A
公开(公告)日：1999-11-02
申请号：US87855
申请日：1998-06-01
申请人： Gillian Anlezark , Roger Melton , Roger Sherwood , Thomas Connors , Frank Friedlos , Michael Jarman , Richard Knox , Anthony Mauger , Caroline Joy Springer
发明人： Gillian Anlezark , Roger Melton , Roger Sherwood , Thomas Connors , Frank Friedlos , Michael Jarman , Richard Knox , Anthony Mauger , Caroline Joy Springer
IPC分类号： C12N9/12 , A61K38/00 , C07C219/34 , C07C271/18 , C07D203/14 , C07D487/14 , C07H15/252 , C07H19/048 , C07K7/06 , C12N9/02 , C12N15/00 , C12N15/09 , C12N15/53 , C12P17/10 , C12P21/08 , C12R1/01 , C12R1/07 , C12R1/19 , G01N33/53 , G01N33/573 , A61K38/12 , C07K5/00 , C07K7/00
CPC分类号： C07D203/14 , C07C219/34 , C07C271/18 , C07D487/14 , C07H15/252 , C07H19/048 , C07K7/06 , C12N9/0036 , C12P17/10 , C12Y101/01284 , A61K38/00 , Y02E50/16
摘要： A prodrug of the formula (I): ##STR1## where R.sup.1 is a group such that the compound R.sup.1 NH.sub.2 represents actinomycin D, doxorubicin, mitomycin C, or a nitrogen mustard of the formula (IV): ##STR2## a prodrug of the formula (II): ##STR3## where R.sup.2 is a group such that the compound R.sup.2 OH is a phenolic nitrogen mustard; and processes whereby the prodrugs shown above are made in which a prodrug precursor compound is reacted with 4-nitrobenzyl chloroformate under anhydrous conditions.
摘要翻译： 式（I）的前药：其中R1是使化合物R1NH2表示放线菌素D，多柔比星，丝裂霉素C或式（IV）的氮芥的基团：式（II）的前药：其中R 2 是化合物R 2 OH是酚氮芥的基团; 以及其中制备前述前药的方法，其中前药前体化合物与无水条件下的氯甲酸4-硝基苄酯反应。
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公开(公告)号：US5585512A
公开(公告)日：1996-12-17
申请号：US394814
申请日：1995-02-27
IPC分类号： C07D405/04 , A61K31/235 , A61K31/505 , A61P35/00 , C07C213/06 , C07C219/34 , C07C233/47 , C07H19/06 , C07C261/00 , C07C69/76 , C07C269/00
CPC分类号： C07H19/06 , C07C219/34 , C07C233/47
摘要： There is disclosed an ester compound that is resistant to decomposition in blood, but is quickly hydrolyzed in cancer cells, and functions as an anticancer agent. The ester compound has a structure represented by formula (I) or formula (II): ##STR1## wherein R.sub.1 represents a methyl group, a methoxy group, or a trifluoroacetamido group; R.sub.2 represents a phenyl group or a phenylmethyl group; and the absolute configuration of the asymmetric center marked with an asterisk is R.
摘要翻译： 公开了一种对血液中的分解有抗性但在癌细胞中迅速水解的酯化合物，作为抗癌剂起作用。 酯化合物具有由式（I）或式（II）表示的结构：其中R 1表示甲基，甲氧基或三氟乙酰胺基;式（I）其中R 1表示甲基， R2表示苯基或苯甲基; 并且标有星号的不对称中心的绝对配置为+ E，uns R + EE。
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