-
公开(公告)号：US5545636A
公开(公告)日：1996-08-13
申请号：US324948
申请日：1994-10-18
申请人： William F. Heath, Jr. , John H. McDonald, III , Michael Paal , Gerd R uhter , Theo Schotten , Wolfgang Stenzel
发明人： William F. Heath, Jr. , John H. McDonald, III , Michael Paal , Gerd R uhter , Theo Schotten , Wolfgang Stenzel
IPC分类号： C07D401/14 , C07D403/14 , C07D405/14 , C07D471/04 , C07H15/26 , A61K31/435 , A61K31/445 , C07D463/00
CPC分类号： C07D401/14 , C07D403/14 , C07D405/14 , C07D471/04 , C07H15/26
摘要： The present invention discloses compounds of the general formula: ##STR1## The compounds are highly isozyme selective protein kinase C beta-1 and beta-2 isozyme inhibitors. Accordingly, the present invention provides a method of selectively inhibiting protein kinase C isozymes beta-1, and beta-2. As isozyme selective inhibitors of beta-1 and beta-2, the compounds are therapeutically useful in treating conditions associated with diabetes mellitus and its complications, as well as other disease states associated with an elevation of the beta-1 and beta-2 isozyme.
摘要翻译： 本发明公开了以下通式的化合物：该化合物是高度同功酶选择性蛋白激酶Cβ-1和β-2同功酶抑制剂。 因此，本发明提供了选择性抑制蛋白激酶C同功酶β-1和β-2的方法。 作为β-1和β-2的同工酶选择性抑制剂，该化合物在治疗与糖尿病及其并发症相关的病症以及与β-1和β-2同功酶升高相关的其它疾病状态中是治疗上有用的。
-
公开(公告)号：US5672618A
公开(公告)日：1997-09-30
申请号：US452606
申请日：1995-05-25
申请人： William F. Heath, Jr. , John H. McDonald, III , Michael Paal , Theo Schotten , Wolfgang Stenzel
发明人： William F. Heath, Jr. , John H. McDonald, III , Michael Paal , Theo Schotten , Wolfgang Stenzel
IPC分类号： C07D487/04 , A61K31/40 , A61K31/4025 , A61K31/404 , A61K31/437 , A61K31/454 , A61K31/7056 , A61P3/10 , A61P7/02 , A61P9/00 , A61P9/10 , A61P9/12 , A61P17/00 , A61P17/06 , A61P25/00 , A61P25/28 , A61P29/00 , A61P35/00 , A61P43/00 , C07D401/14 , C07D403/14 , C07D405/14 , C07D471/04 , C07H15/26 , A61K31/70 , C07H17/00
CPC分类号： C07D401/14 , C07D403/14 , C07D405/14 , C07D471/04 , C07H15/26
摘要： The present invention discloses compounds that are highly isozyme selective protein kinase C beta-1 and beta-2 isozyme inhibitors. Accordingly, the present invention provides a method of selectively inhibiting protein kinase C isozymes beta-1, and beta-2. As isozyme selective inhibitors of beta-1 and beta-2, the compounds are therapeutically useful in treating conditions associated with diabetes mellitus and its complications, as well as other disease states associated with an elevation of the beta-1 and beta-2 isozyme.
-
公开(公告)号：US5668152A
公开(公告)日：1997-09-16
申请号：US452617
申请日：1995-05-25
IPC分类号： C07D487/04 , A61K31/40 , A61K31/4025 , A61K31/404 , A61K31/437 , A61K31/454 , A61K31/7056 , A61P3/10 , A61P7/02 , A61P9/00 , A61P9/10 , A61P9/12 , A61P17/00 , A61P17/06 , A61P25/00 , A61P25/28 , A61P29/00 , A61P35/00 , A61P43/00 , C07D401/14 , C07D403/14 , C07D405/14 , C07D471/04 , C07H15/26 , A61K31/445
CPC分类号： C07D401/14 , C07D403/14 , C07D405/14 , C07D471/04 , C07H15/26
摘要： The present invention discloses compounds that are highly isozyme selective protein kinase C beta-1 and beta-2 isozyme inhibitors. Accordingly, the present invention provides a method of selectively inhibiting protein kinase C isozymes beta-1, and beta-2. As isozyme selective inhibitors of beta-1 and beta-2, the compounds are therapeutically useful in treating conditions associated with diabetes mellitus and its complications, as well as other disease states associated with an elevation of the beta-1 and beta-2 isozyme.
摘要翻译： 本发明公开了高度同功酶选择性蛋白激酶Cβ-1和β-2同功酶抑制剂的化合物。 因此，本发明提供了选择性抑制蛋白激酶C同功酶β-1和β-2的方法。 作为β-1和β-2的同工酶选择性抑制剂，该化合物在治疗与糖尿病及其并发症相关的病症以及与β-1和β-2同功酶升高相关的其它疾病状态中是治疗上有用的。
-
公开(公告)号：US5843935A
公开(公告)日：1998-12-01
申请号：US903236
申请日：1997-07-12
IPC分类号： C07D487/14 , A61K31/395 , A61K31/40 , A61K31/407 , A61K31/55 , A61P3/08 , A61P3/10 , A61P9/00 , A61P9/10 , A61P17/00 , A61P25/00 , A61P29/00 , A61P35/00 , A61P43/00 , C07C43/174 , C07C43/178 , C07D487/22 , C07D491/147 , C07D491/22 , C07D498/22 , C07D513/22 , C07F7/18
CPC分类号： C07D487/22 , C07C43/1745 , C07C43/1785 , C07D498/22 , C07D513/22 , C07F7/1852
摘要： This invention provides novel bis-indolemaleimide macrocycle derivatives of the formula: ##STR1## The invention further provides the preparation, pharmaceutical formulations and the methods of use for inhibiting Protein Kinase C in mammals.
摘要翻译： 本发明提供下式的新型双吲哚马来酰亚胺大环衍生物：本发明还提供哺乳动物中抑制蛋白激酶C的制备，药物制剂和用途的方法。
-
公开(公告)号：US5780461A
公开(公告)日：1998-07-14
申请号：US643710
申请日：1996-05-06
IPC分类号： C07D487/14 , A61K31/395 , A61K31/40 , A61K31/407 , A61K31/55 , A61P3/08 , A61P3/10 , A61P9/00 , A61P9/08 , A61P9/10 , A61P17/00 , A61P25/00 , A61P25/28 , A61P29/00 , A61P35/00 , A61P43/00 , C07C43/174 , C07C43/178 , C07D487/04 , C07D487/22 , C07D491/147 , C07D491/22 , C07D498/22 , C07D513/22 , C07F7/18
CPC分类号： C07D487/22 , C07C43/1745 , C07C43/1785 , C07D498/22 , C07D513/22 , C07F7/1852
摘要： This invention provides novel bis-indolemaleimide macrocycle derivatives of the formula: ##STR1## The invention further provides the preparation, pharmaceutical formulations and the methods of use for inhibiting Protein Kinase C in mammals. The compounds of the present invention can be used to treat cancer and inhibiting tumor growth in mammals.
摘要翻译： 本发明提供下式的新型双吲哚马来酰亚胺大环衍生物：本发明还提供哺乳动物中抑制蛋白激酶C的制备，药物制剂和用途的方法。 本发明的化合物可用于治疗哺乳动物的癌症和抑制肿瘤生长。
-
公开(公告)号：US5674862A
公开(公告)日：1997-10-07
申请号：US457060
申请日：1995-06-01
IPC分类号： C07D487/14 , A61K31/395 , A61K31/40 , A61K31/407 , A61K31/55 , A61P3/08 , A61P3/10 , A61P9/00 , A61P9/08 , A61P9/10 , A61P17/00 , A61P25/00 , A61P25/28 , A61P29/00 , A61P35/00 , A61P43/00 , C07C43/174 , C07C43/178 , C07D487/04 , C07D487/22 , C07D491/147 , C07D491/22 , C07D498/22 , C07D513/22 , C07F7/18 , C07D269/00 , C07D413/14
CPC分类号： C07D487/22 , C07C43/1745 , C07C43/1785 , C07D498/22 , C07D513/22 , C07F7/1852
摘要： This invention provides novel bis-indolemaleimide macrocycle derivatives of the formula: ##STR1## The invention further provides the preparation, pharmaceutical formulations and the methods of use for inhibiting Protein Kinase C in mammals.
摘要翻译： 本发明提供下式的新型双吲哚马来酰亚胺大环衍生物：本发明还提供哺乳动物中抑制蛋白激酶C的制备，药物制剂和用途的方法。
-
公开(公告)号：US5621098A
公开(公告)日：1997-04-15
申请号：US457657
申请日：1995-06-01
IPC分类号： C07D487/14 , A61K31/395 , A61K31/40 , A61K31/407 , A61K31/55 , A61P3/08 , A61P3/10 , A61P9/00 , A61P9/08 , A61P9/10 , A61P17/00 , A61P25/00 , A61P25/28 , A61P29/00 , A61P35/00 , A61P43/00 , C07C43/174 , C07C43/178 , C07D487/04 , C07D487/22 , C07D491/147 , C07D491/22 , C07D498/22 , C07D513/22 , C07F7/18 , C07D223/14
CPC分类号： C07D487/22 , C07C43/1745 , C07C43/1785 , C07D498/22 , C07D513/22 , C07F7/1852
摘要： This invention provides novel bis-indolemaleimide macrocycle derivatives of the formula: ##STR1## wherein R.sub.1, R.sub.2, X, W, and Y are as defined in the specification. The invention further provides the preparation, pharmaceutical formulations and the methods of use for inhibiting Protein Kinase C in mammals.
摘要翻译： 本发明提供了新颖的下式的双吲哚马来酰亚胺大环衍生物：其中R 1，R 2，X，W和Y如说明书中所定义。 本发明还提供了用于抑制哺乳动物中的蛋白激酶C的制剂，药物制剂和用途。
-
公开(公告)号：US5739322A
公开(公告)日：1998-04-14
申请号：US822255
申请日：1997-03-20
IPC分类号： C07D487/14 , A61K31/395 , A61K31/40 , A61K31/407 , A61K31/55 , A61P3/08 , A61P3/10 , A61P9/00 , A61P9/08 , A61P9/10 , A61P17/00 , A61P25/00 , A61P25/28 , A61P29/00 , A61P35/00 , A61P43/00 , C07C43/174 , C07C43/178 , C07D487/04 , C07D487/22 , C07D491/147 , C07D491/22 , C07D498/22 , C07D513/22 , C07F7/18 , C07D223/14
CPC分类号： C07D487/22 , C07C43/1745 , C07C43/1785 , C07D498/22 , C07D513/22 , C07F7/1852
摘要： This invention provides novel bis-indolemaleimide macrocycle derivatives of the formula: ##STR1## wherein R1, R2, X, W, and Y are as defined in the specification. The invention further provides the preparation, pharmaceutical formulations and the methods of use for inhibiting Protein Kinase C in mammals.
摘要翻译： 本发明提供了新颖的下式的双吲哚马来酰亚胺大环衍生物：其中R 1，R 2，X，W和Y如说明书中所定义。 本发明还提供了用于抑制哺乳动物中的蛋白激酶C的制剂，药物制剂和用途。
-
公开(公告)号：US5698578A
公开(公告)日：1997-12-16
申请号：US734292
申请日：1996-10-21
IPC分类号： C07D487/14 , A61K31/395 , A61K31/40 , A61K31/407 , A61K31/55 , A61P3/08 , A61P3/10 , A61P9/00 , A61P9/10 , A61P17/00 , A61P25/00 , A61P29/00 , A61P35/00 , A61P43/00 , C07C43/174 , C07C43/178 , C07D487/22 , C07D491/147 , C07D491/22 , C07D498/22 , C07D513/22 , C07F7/18
CPC分类号： C07D487/22 , C07C43/1745 , C07C43/1785 , C07D498/22 , C07D513/22 , C07F7/1852
摘要： This invention provides novel bis-indolemaleimide macrocycle derivatives of the formula: ##STR1## The invention further provides the preparation, pharmaceutical formulations and the methods of use for inhibiting Protein Kinase C in mammals.
-
公开(公告)号：US5696108A
公开(公告)日：1997-12-09
申请号：US646703
申请日：1996-05-06
IPC分类号： C07D487/14 , A61K31/395 , A61K31/40 , A61K31/407 , A61K31/55 , A61P3/08 , A61P3/10 , A61P9/00 , A61P9/08 , A61P9/10 , A61P17/00 , A61P25/00 , A61P25/28 , A61P29/00 , A61P35/00 , A61P43/00 , C07C43/174 , C07C43/178 , C07D487/04 , C07D487/22 , C07D491/147 , C07D491/22 , C07D498/22 , C07D513/22 , C07F7/18 , C07D255/00
CPC分类号： C07D487/22 , C07C43/1745 , C07C43/1785 , C07D498/22 , C07D513/22 , C07F7/1852
摘要： This invention provides novel bis-indolemaleimide macrocycle derivatives of the formula: ##STR1## The invention further provides the preparation, pharmaceutical formulations and the methods of use for inhibiting Protein Kinase C in mammals.
摘要翻译： 本发明提供下式的新型双吲哚马来酰亚胺大环衍生物：本发明还提供哺乳动物中抑制蛋白激酶C的制备，药物制剂和用途的方法。
-
-
-
-
-
-
-
-
-
搜索结果
42 条记录 (耗时 0.036 秒)
