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1.发明授权Tricyclic amide and urea compounds useful for inhibition of G-protein function and for treatment of proliferative diseases 失效可用于抑制G蛋白功能和治疗增殖性疾病的三环酰胺和尿素化合物公开(公告)号：US06242458B1
公开(公告)日：2001-06-05
申请号：US09400714
申请日：1999-09-21
申请人： W. Robert Bishop , Ronald J. Doll , Alan K. Mallams , F. George Njoroge , Joanne M. Petrin , John J. Piwinski , Ronald L. Wolin , Arthur G. Taveras , Stacy W. Remiszewski
发明人： W. Robert Bishop , Ronald J. Doll , Alan K. Mallams , F. George Njoroge , Joanne M. Petrin , John J. Piwinski , Ronald L. Wolin , Arthur G. Taveras , Stacy W. Remiszewski
IPC分类号： A61K314545
CPC分类号： C07D231/12 , A61K31/444 , A61K31/445 , A61K31/47 , A61K31/495 , A61K31/496 , A61K31/50 , A61K31/505 , C07D221/16 , C07D233/56 , C07D249/08 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/14 , C07D409/14 , C07D417/14
摘要： A method of inhibiting Ras function and therefore inhibiting the abnormal growth of cells is disclosed. The method comprises the administration of a compound of Formula 1.0: to a biological system. In particular, the method inhibits the abnormal growth of cells in a mammal such as a human being. Novel compounds of the formulas 5.1 and 5.2 are disclosed.
摘要翻译： 公开了抑制Ras功能并因此抑制细胞异常生长的方法。 该方法包括向生物系统施用式1.0化合物。 特别地，该方法抑制哺乳动物例如人的细胞的异常生长。 公开了式5.1和5.2的新型化合物。
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2.发明授权Tricyclic carbamate compounds useful for inhibition of G-protein function and for treatment of proliferative diseases 失效可用于抑制G蛋白功能和治疗增殖性疾病的三环氨基甲酸酯化合物公开(公告)号：US06492381B1
公开(公告)日：2002-12-10
申请号：US09571922
申请日：2000-05-16
申请人： W. Robert Bishop , Ronald J. Doll , Alan K. Mallams , F. George Njoroge , Joanne M. Petrin , John J. Piwinski , Ronald L. Wolin , Arthur G. Taveras , Stacy W. Remiszewski
发明人： W. Robert Bishop , Ronald J. Doll , Alan K. Mallams , F. George Njoroge , Joanne M. Petrin , John J. Piwinski , Ronald L. Wolin , Arthur G. Taveras , Stacy W. Remiszewski
IPC分类号： A61K31435
CPC分类号： C07D401/12 , A61K31/4545 , A61K31/496
摘要： A method of inhibiting Ras function and therefore inhibiting cellular growth is disclosed. The method comprises the administration of a compound of Formula 1.0 Also disclosed are novel compounds of the formulas: and Also disclosed are processes for making 3-substituted compounds of the Formulas 1.1, 1.2 and 1.3. Further disclosed are novel compounds which are intermediates in the processes for making the 3-substituted compounds of Formulas 1.1, 1.2, and 1.3.
摘要翻译： 公开了抑制Ras功能并因此抑制细胞生长的方法。 该方法包括施用式1.0的化合物。还公开了下式的新化合物：还公开了制备式为1.1,1.2和1.3的3-取代化合物的方法。进一步公开了作为方法中的中间体的新化合物 用于制备式1.1,1.2和1.3的3-取代的化合物。
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3.发明授权Tricyclic carbamate compounds useful for inhibition of G-protein function and for treatment of proliferative diseases 失效可用于抑制G蛋白功能和治疗增殖性疾病的三环氨基甲酸酯化合物
公开(公告)号：US5728703A
公开(公告)日：1998-03-17
申请号：US455018
申请日：1995-05-31
申请人： W. Robert Bishop , Ronald J. Doll , Alan K. Mallams , F. George Njoroge , Joanne M. Petrin , John J. Piwinski , Ronald L. Wolin , Arthur G. Taveras , Stacy W. Remiszewski
发明人： W. Robert Bishop , Ronald J. Doll , Alan K. Mallams , F. George Njoroge , Joanne M. Petrin , John J. Piwinski , Ronald L. Wolin , Arthur G. Taveras , Stacy W. Remiszewski
IPC分类号： A61K31/435 , A61K31/4375 , A61K31/4545 , A61K31/495 , A61K31/496 , A61P35/00 , C07D221/06 , C07D221/16 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04
CPC分类号： C07D401/12 , A61K31/4545 , A61K31/496 , C07D221/16 , C07D401/04 , C07D401/14
摘要： A method of inhibiting Ras function and therefore inhibiting cellular growth is disclosed. The method comprises the administration of a compound of Formula. 1.0 ##STR1## Also disclosed are novel compounds of the formulas: ##STR2## Also disclosed are processes for making 3-substituted compounds of the Formulas 1.1, 1.2 and 1.3. Further disclosed are novel compounds which are intermediates in the processes for making the 3-substituted compounds of Formulas 1.1, 1.2, and 1.3.
摘要翻译： 公开了抑制Ras功能并因此抑制细胞生长的方法。 该方法包括施用式的化合物。 （1.0）还公开了下式的新化合物：
（1.1） -
4.发明授权Tricyclic amide and urea compounds useful for inhibition of g-protein function and for treatment of proliferative diseases 失效用于抑制g-蛋白功能和治疗增殖性疾病的三环酰胺和尿素化合物
公开(公告)号：US5719148A
公开(公告)日：1998-02-17
申请号：US410187
申请日：1995-03-24
申请人： W. Robert Bishop , Ronald J. Doll , Alan K. Mallams , F. George Njoroge , Joanne M. Petrin , John J. Piwinski , Ronald L. Wolin , Arthur G. Taveras , Stacy W. Remiszewski
发明人： W. Robert Bishop , Ronald J. Doll , Alan K. Mallams , F. George Njoroge , Joanne M. Petrin , John J. Piwinski , Ronald L. Wolin , Arthur G. Taveras , Stacy W. Remiszewski
IPC分类号： A61K31/4427 , A61K31/444 , A61K31/445 , A61K31/47 , A61K31/495 , A61K31/496 , A61K31/50 , A61K31/505 , A61K31/54 , A61P35/00 , C07D221/16 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/14 , C07D409/14 , C07D417/14 , C07D521/00 , C07D401/08
CPC分类号： C07D231/12 , A61K31/444 , A61K31/445 , A61K31/47 , A61K31/495 , A61K31/496 , A61K31/50 , A61K31/505 , C07D221/16 , C07D233/56 , C07D249/08 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/14 , C07D409/14 , C07D417/14
摘要： A method of inhibiting Ras function and therefore inhibiting the abnormal growth of cells is disclosed. The method comprises the administration of a compound of Formula 1.0: ##STR1## to a biological system. In particular, the method inhibits the abnormal growth of cells in a mammal such as a human being. Novel compounds of formulas 5.0, 5.1 and 5.2, wherein R is --C(R.sup.20)(R.sup.21)(R.sup.46), and 5.3, 5.3A and 5.3B, wherein R is --N(R.sup.25)(R.sup.48), are disclosed. Also disclosed are processes for making 3-substituted compounds of Formulas 5.0, 5.1, 5.2 and 5.3. Further disclosed are novel compounds which are intermediates in the process for making 3-substituted compounds of Formulas 5.0, 5.1, 5.2 and 5.3.
摘要翻译： 公开了抑制Ras功能并因此抑制细胞异常生长的方法。 该方法包括向生物系统施用式1.0化合物：（IMAGE）（1.0）。 特别地，该方法抑制哺乳动物例如人的细胞的异常生长。 公开了新的式5.0,5.1和5.2的化合物，其中R是-C（R 20）（R 21）（R 46），和5.3,5.3A和5.3B，其中R是-N（R 25）（R 48）。 还公开了制备式5.0,5.1,5.2和5.3的3-取代的化合物的方法。 进一步公开的是在制备式5.0,5.1,5.2和5.3的3-取代化合物的方法中的中间体的新化合物。
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5.发明授权Tricyclic amide and urea compounds useful for inhibition of G-protein function and for treatment of proliferative diseases 失效可用于抑制G蛋白功能和治疗增殖性疾病的三环酰胺和尿素化合物
公开(公告)号：US5696121A
公开(公告)日：1997-12-09
申请号：US450288
申请日：1995-05-25
申请人： W. Robert Bishop , Ronald J. Doll , Alan K. Mallams , F. George Njoroge , Joanne M. Petrin , John J. Piwinski , Ronald L. Wolin , Arthur G. Taveras , Stacy W. Remiszewski
发明人： W. Robert Bishop , Ronald J. Doll , Alan K. Mallams , F. George Njoroge , Joanne M. Petrin , John J. Piwinski , Ronald L. Wolin , Arthur G. Taveras , Stacy W. Remiszewski
IPC分类号： A61K31/4427 , A61K31/444 , A61K31/445 , A61K31/47 , A61K31/495 , A61K31/496 , A61K31/50 , A61K31/505 , A61K31/54 , A61P35/00 , C07D221/16 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/14 , C07D409/14 , C07D417/14 , C07D521/00 , C07D401/08 , A61K31/55
CPC分类号： C07D231/12 , A61K31/444 , A61K31/445 , A61K31/47 , A61K31/495 , A61K31/496 , A61K31/50 , A61K31/505 , C07D221/16 , C07D233/56 , C07D249/08 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/14 , C07D409/14 , C07D417/14
摘要： A method of inhibiting Ras function and therefore inhibiting the abnormal growth of cells is disclosed. The method comprises the administration of a compound of Formula 1.0: ##STR1## to a biological system. In particular, the method inhibits the abnormal growth of cells in a mammal such as a human being. Novel compounds of formulas 5.0, 5.1 and 5.2, wherein R is --C(R.sup.20)(R.sup.21)(R.sup.46), and 5.3, 5.3A and 5.3B, wherein R is --N(R.sub.25)(R.sub.48), are disclosed. Also disclosed are processes for making 3-substituted compounds of Formulas 5.0, 5.1, 5.2 and 5.3. Further disclosed are novel compounds which are intermediates in the process for making 3-substituted compounds of Formulas 5.0, 5.1, 5.2 and 5.3.
摘要翻译： 公开了抑制Ras功能并因此抑制细胞异常生长的方法。 该方法包括向生物系统施用式1.0化合物：（IMAGE）（1.0）。 特别地，该方法抑制哺乳动物例如人的细胞的异常生长。 公开了新的式5.0,5.1和5.2的化合物，其中R是-C（R 20）（R 21）（R 46），和5.3,5.3A和5.3B，其中R是-N（R 25）（R 48）。 还公开了制备式5.0,5.1,5.2和5.3的3-取代的化合物的方法。 进一步公开的是在制备式5.0,5.1,5.2和5.3的3-取代化合物的方法中的中间体的新化合物。
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6.发明授权Tricyclic sulfonamide compounds useful for inhibition of G-protein function and for treatment of proliferative diseases 失效可用于抑制G蛋白功能和治疗增殖性疾病的三环磺酰胺化合物
公开(公告)号：US5661152A
公开(公告)日：1997-08-26
申请号：US444996
申请日：1995-05-19
申请人： W. Robert Bishop , Ronald J. Doll , Alan K. Mallams , F. George Njoroge , Joanne M. Petrin , John J. Piwinski
发明人： W. Robert Bishop , Ronald J. Doll , Alan K. Mallams , F. George Njoroge , Joanne M. Petrin , John J. Piwinski
IPC分类号： C07D221/16 , C07D401/04 , C07D409/14 , C07D417/14 , A61K31/44 , A61K31/495 , C07D401/12
CPC分类号： C07D401/04 , C07D221/16 , C07D409/14 , C07D417/14
摘要： A method of inhibiting Ras function and therefore inhibiting cellular growth is disclosed. The method comprises the administration of a compound containing a tricyclic ring system to a biological system. In particular, the method inhibits cellular growth in a mammal such as a human being.Novel compounds of the formula: ##STR1## are disclosed. Also disclosed are processes for making 3-substituted compounds of Formula 4.0.Further disclosed are novel compounds which are intermediates in the processes for making the 3-substituted compounds of Formula 4.0.
摘要翻译： 公开了抑制Ras功能并因此抑制细胞生长的方法。 该方法包括向生物系统施用含有三环系统的化合物。 特别地，该方法抑制哺乳动物例如人的细胞生长。 公开了下式的新型化合物：
（4.0）。 还公开了制备式4.0的3-取代的化合物的方法。 进一步公开的是在制备式4.0的3-取代化合物的方法中的中间体的新化合物。 -
7.发明授权Tricyclic carbamate compounds useful for inhibition of g-protein function and for treatment of proliferative diseases 失效可用于抑制g-蛋白功能和治疗增殖性疾病的三环氨基甲酸酯化合物公开(公告)号：US06300338B1
公开(公告)日：2001-10-09
申请号：US09348916
申请日：1999-07-07
申请人： W. Robert Bishop , Ronald J. Doll , Alan K. Mallams , F. George Njoroge , Joanne M. Petrin , John J. Piwinski , Ronald L. Wolin , Arthur G. Taveras , Stacy W. Remiszewski
发明人： W. Robert Bishop , Ronald J. Doll , Alan K. Mallams , F. George Njoroge , Joanne M. Petrin , John J. Piwinski , Ronald L. Wolin , Arthur G. Taveras , Stacy W. Remiszewski
IPC分类号： A61K31435
CPC分类号： C07D401/12 , A61K31/4545 , A61K31/496 , C07D221/16 , C07D401/04 , C07D401/14
摘要： A method of inhibiting Ras function and therefore inhibiting cellular growth is disclosed. The method comprises the administration of a compound of Formula 1.0 Also disclosed are novel compounds of the formulas: Also disclosed are processes for making 3-substituted compounds of the Formulas 1.1, 1.2 and 1.3. Further disclosed are novel compounds which are intermediates in the processes for making the 3-substituted compounds of Formulas 1.1, 1.2, and 1.3.
摘要翻译： 公开了抑制Ras功能并因此抑制细胞生长的方法。 该方法包括施用式1.0的化合物。还公开了下式的新化合物：还公开了制备式为1.1,1.2和1.3的3-取代化合物的方法。进一步公开了作为方法中的中间体的新化合物 用于制备式1.1,1.2和1.3的3-取代的化合物。
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8.发明授权Tricyclic carbamate compounds useful for inhibition of G-protein function and for treatment of proliferative diseases 失效可用于抑制G蛋白功能和治疗增殖性疾病的三环氨基甲酸酯化合物
公开(公告)号：US6075025A
公开(公告)日：2000-06-13
申请号：US038416
申请日：1998-03-11
申请人： W. Robert Bishop , Ronald J. Doll , Alan K. Mallams , F. George Njoroge , Joanne M. Petrin , John J. Piwinski , Ronald L. Wolin , Arthur G. Taveras , Stacy W. Remiszewski
发明人： W. Robert Bishop , Ronald J. Doll , Alan K. Mallams , F. George Njoroge , Joanne M. Petrin , John J. Piwinski , Ronald L. Wolin , Arthur G. Taveras , Stacy W. Remiszewski
IPC分类号： A61K31/435 , A61K31/4375 , A61K31/4545 , A61K31/496 , C07D221/06 , C07D401/04 , C07D401/12 , C07D403/04
CPC分类号： C07D401/12 , A61K31/4545 , A61K31/496
摘要： A method of inhibiting Ras function and therefore inhibiting cellular growth is disclosed. The method comprises the administration of a compound of Formula 1.0 ##STR1## Also disclosed are novel compounds of the formulas: ##STR2## Also disclosed are processes for making 3-substituted compounds of the Formulas 1.1, 1.2 and 1.3.Further disclosed are novel compounds which are intermediates in the processes for making the 3-substituted compounds of Formulas 1.1, 1.2, and 1.3.
摘要翻译： 公开了抑制Ras功能并因此抑制细胞生长的方法。 该方法包括施用式1.0的化合物。还公开了下式的新化合物：还公开了制备式1.1,1.2和1.3的3-取代化合物的方法。 进一步公开的是在制备式1.1,1.2和1.3的3-取代化合物的方法中的中间体的新化合物。
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9.发明授权Tricyclic amide and urea compounds, useful inhibition of g-protein function and for treatment of proliferative diseases 失效三环酰胺和尿素化合物，有用的抑制g蛋白功能和治疗增殖性疾病
公开(公告)号：US5807853A
公开(公告)日：1998-09-15
申请号：US450433
申请日：1995-05-25
申请人： W. Robert Bishop , Ronald J. Doll , Alan K. Mallams , F. George Njoroge , Joanne M. Petrin , John J. Piwinski , Ronald L. Wolin , Arthur G. Taveras , Stacy W. Remiszewski
发明人： W. Robert Bishop , Ronald J. Doll , Alan K. Mallams , F. George Njoroge , Joanne M. Petrin , John J. Piwinski , Ronald L. Wolin , Arthur G. Taveras , Stacy W. Remiszewski
IPC分类号： A61K31/4427 , A61K31/444 , A61K31/445 , A61K31/47 , A61K31/495 , A61K31/496 , A61K31/50 , A61K31/505 , A61K31/54 , A61P35/00 , C07D221/16 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/14 , C07D409/14 , C07D417/14 , C07D521/00 , C07D401/02 , C07D401/08 , C07D403/08
CPC分类号： C07D231/12 , A61K31/444 , A61K31/445 , A61K31/47 , A61K31/495 , A61K31/496 , A61K31/50 , A61K31/505 , C07D221/16 , C07D233/56 , C07D249/08 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/14 , C07D409/14 , C07D417/14
摘要： A method of inhibiting Ras function and therefore inhibiting the abnormal growth of cells is disclosed. The method comprises the administration of a compound of Formula 1.0: ##STR1## to a biological system. In particular, the method inhibits the abnormal growth of cells in a mammal such as a human being. Novel compounds of formulas 5.0, 5.1 and 5.2, wherein R is --C(R.sup.20)(R.sup.21)(R.sup.46), and 5.3, 5.3A and 5.3B, wherein R is --N(R.sup.25)(R.sup.48), are disclosed. Also disclosed are processes for making 3-substituted compounds of Formulas 5.0, 5.1, 5.2 and 5.3. Further disclosed are novel compounds which are intermediates in the process for making 3-substituted compounds of Formulas 5.0, 5.1, 5.2 and 5.3.
摘要翻译： 公开了抑制Ras功能并因此抑制细胞异常生长的方法。 该方法包括向生物系统施用式1.0化合物：（IMAGE）（1.0）。 特别地，该方法抑制哺乳动物例如人的细胞的异常生长。 公开了新的式5.0,5.1和5.2的化合物，其中R是-C（R 20）（R 21）（R 46），和5.3,5.3A和5.3B，其中R是-N（R 25）（R 48）。 还公开了制备式5.0,5.1,5.2和5.3的3-取代的化合物的方法。 进一步公开的是在制备式5.0,5.1,5.2和5.3的3-取代化合物的方法中的中间体的新化合物。
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10.发明授权Tricyclic carbamate compounds useful for inhibition of G-protein function and for treatment of proliferative diseases 失效可用于抑制G蛋白功能和治疗增殖性疾病的三环氨基甲酸酯化合物
公开(公告)号：US5721236A
公开(公告)日：1998-02-24
申请号：US410479
申请日：1995-03-24
申请人： W. Robert Bishop , Ronald J. Doll , Alan K. Mallams , F. George Njoroge , Joanne M. Petrin , John J. Piwinski , Ronald L. Wolin , Arthur G. Taveras , Stacy W. Remiszewski
发明人： W. Robert Bishop , Ronald J. Doll , Alan K. Mallams , F. George Njoroge , Joanne M. Petrin , John J. Piwinski , Ronald L. Wolin , Arthur G. Taveras , Stacy W. Remiszewski
IPC分类号： A61K31/435 , A61K31/4375 , A61K31/4545 , A61K31/495 , A61K31/496 , A61P35/00 , C07D221/06 , C07D221/16 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04
CPC分类号： C07D401/12 , A61K31/4545 , A61K31/496 , C07D221/16 , C07D401/04 , C07D401/14
摘要： A method of inhibiting Ras function and therefore inhibiting cellular growth is disclosed. The method comprises the administration of a compound of Formula 1.0 ##STR1## Also disclosed are novel compounds of the formulas: ##STR2## Also disclosed are processes for making 3-substituted compounds of the Formulas 1.1, 1.2 and 1.3. Further disclosed are novel compounds which are intermediates in the processes for making the 3-substituted compounds of Formulas 1.1, 1.2, and 1.3.
摘要翻译： 公开了抑制Ras功能并因此抑制细胞生长的方法。 该方法包括给予式1.0化合物（1.0）还公开了下式的新化合物：（IMAGE）（1.1）
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