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公开(公告)号：US5624953A
公开(公告)日：1997-04-29
申请号：US594613
申请日：1996-02-02
申请人： Samantha J. Ambler , William F. Heath, Jr. , Jai Pal Singh , Colin W. Smith , Lawrence E. Stramm
发明人： Samantha J. Ambler , William F. Heath, Jr. , Jai Pal Singh , Colin W. Smith , Lawrence E. Stramm
IPC分类号： A61K31/35 , A61K31/352 , A61P3/08 , A61P3/10 , A61P9/00 , C07D311/92 , C07D405/04 , A61K31/40 , C07D311/78
CPC分类号： C07D405/04 , C07D311/92
摘要： This invention provides novel compounds and pharmaceutical methods comprising the administration of a compound of the Formula I: ##STR1## wherein n, m, R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are variables.
摘要翻译： 本发明提供新的化合物和药物方法，其包括施用式I化合物：其中n，m，R 1，R 2，R 3和R 4是变量。
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公开(公告)号：US5514706A
公开(公告)日：1996-05-07
申请号：US342993
申请日：1994-11-21
申请人： Samantha J. Ambler , William F. Heath, Jr. , Jai P. Singh , Colin W. Smith , Lawrence E. Stramm
发明人： Samantha J. Ambler , William F. Heath, Jr. , Jai P. Singh , Colin W. Smith , Lawrence E. Stramm
IPC分类号： A61K31/35 , A61K31/352 , A61P3/08 , A61P3/10 , A61P9/00 , C07D311/92 , C07D405/04 , A61K31/40 , A61K31/435
CPC分类号： C07D405/04 , C07D311/92
摘要： This invention provides novel compounds and pharmaceutical methods comprising the administration of a compound of the Formula I: ##STR1## wherein n, m, R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are variables.
摘要翻译： 本发明提供新的化合物和药物方法，其包括施用式I化合物：其中n，m，R 1，R 2，R 3和R 4是变量。
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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。
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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。
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公开(公告)号：US5574133A
公开(公告)日：1996-11-12
申请号：US381049
申请日：1995-01-31
申请人： Richard D. DiMarchi , David B. Flora , William F. Heath, Jr. , James A. Hoffmann , James E. Shields , David L. Smiley
发明人： Richard D. DiMarchi , David B. Flora , William F. Heath, Jr. , James A. Hoffmann , James E. Shields , David L. Smiley
IPC分类号： A61K38/00 , C07K14/575 , C07K7/00 , C07K7/10
CPC分类号： C07K14/5759 , A61K38/00
摘要： The present invention provides anti-obesity proteins, which when administered to a patient regulate fat tissue. Accordingly, such agents allow patients to overcome their obesity handicap and live normal lives with much reduced risk for type II diabetes, cardiovascular disease and cancer.
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公开(公告)号：US5563245A
公开(公告)日：1996-10-08
申请号：US381163
申请日：1995-01-31
申请人： Richard D. DiMarchi , David B. Flora , William F. Heath, Jr. , James A. Hoffmann , James E. Shields , David L. Smiley
发明人： Richard D. DiMarchi , David B. Flora , William F. Heath, Jr. , James A. Hoffmann , James E. Shields , David L. Smiley
IPC分类号： A61K38/00 , C07K14/575 , C07K7/10
CPC分类号： C07K14/5759 , A61K38/00
摘要： The present invention provides anti-obesity proteins, which when administered to a patient regulate fat tissue. Accordingly, such agents allow patients to overcome their obesity handicap and live normal lives with much reduced risk for type II diabetes, cardiovascular disease and cancer.
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公开(公告)号：US5559208A
公开(公告)日：1996-09-24
申请号：US383639
申请日：1995-02-06
IPC分类号： A61K38/00 , C07K14/575 , A61K35/00 , C07K7/10
CPC分类号： C07K14/5759 , A61K38/00
摘要： The present invention provides anti-obesity proteins, which when administered to a patient regulate fat tissue. Accordingly, such agents allow patients to overcome their obesity handicap and live normal lives with much reduced risk for type II diabetes, cardiovascular disease and cancer.
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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。
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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。
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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。
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