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21. 发明专利

PT802909E 未知
公开(公告)号：PT802909E
公开(公告)日：2002-03-28
申请号：PT95943478
申请日：1995-12-15
申请人： AVENTIS PHARMA INC
发明人： PEET NORTON PAUL , MEHDI SHUJAATH , LINNIK MATTHEW D , KIM HWA-OK , ANGELASTRO MICHAEL R
IPC分类号： C07D263/06 , A61K31/42 , A61K31/421 , A61K31/535 , A61K31/5377 , A61K38/00 , A61P9/08 , A61P9/10 , A61P25/00 , A61P25/28 , A61P43/00 , C07D263/04 , C07D263/18 , C07K5/062
摘要： This invention relates to oxazolidine inhibitors of calpain and/or cathepsin B and to compositions containing them. As inhibitors of calpain and/or cathepsin B, the compounds are useful in the treatment of patients afflicted with acute or chronic neurodegenerative disorders.

22. 发明专利

PL342604A1 6,9-DISUBSTITUTED 2-[TRANS(4-AMINOCYCLOHEXYL)AMINO]PURIN 未知
公开(公告)号：PL342604A1
公开(公告)日：2001-06-18
申请号：PL34260499
申请日：1999-02-18
申请人： AVENTIS PHARMA INC
发明人： DUMONT JENNIFER ANN , BITONTI ALAN JOSEPH , BORCHERDING DAVID ROGER , PEET NORTON PAUL , MUNSON HARRY RANDALL , SHUM PATRICK WAI-KWOK
IPC分类号： C07D473/16 , A61K31/52 , A61P25/00 , A61P35/00 , A61P35/02 , A61P43/00 , C07D473/00

23. 发明专利

NO309267B1 未知
公开(公告)号：NO309267B1
公开(公告)日：2001-01-08
申请号：NO973216
申请日：1997-07-10
申请人： AVENTIS PHARMA INC
发明人： PEET NORTON PAUL , MEHDI SHUJAATH , LINNIK MATTHEW D , ANGELASTRO MICHAEL RICHARD , KIM HWA-OK
IPC分类号： C07D263/06 , A61K31/42 , A61K31/421 , A61K31/535 , A61K31/5377 , A61K38/00 , A61P9/08 , A61P9/10 , A61P25/00 , A61P25/28 , A61P43/00 , C07D263/04 , C07D263/18 , C07K5/062
摘要： This invention relates to oxazolidine inhibitors of calpain and/or cathepsin B and to compositions containing them. As inhibitors of calpain and/or cathepsin B, the compounds are useful in the treatment of patients afflicted with acute or chronic neurodegenerative disorders.

24. 发明专利

PT1377579E DERIVADOS ACILO E SULFONILO DE 2-(TRANS-1,4-DIAMINOCICLOHEXIL)- PURINAS 6,9-DISSUBSTITUÍDAS E SUA UTILIZAÇÃO COMO AGENTES ANTIPROLIFERATIVOS 未知
公开(公告)号：PT1377579E
公开(公告)日：2009-06-30
申请号：PT01987144
申请日：2001-10-31
申请人： AVENTIS PHARMA INC
发明人： PEET NORTON PAUL , DUMONT JENNIFER A , BORCHERDING DAVID , WRIGHT PAUL S
IPC分类号： C07D473/00 , C07D20060101

25. 发明专利

EE04315B1 未知
公开(公告)号：EE04315B1
公开(公告)日：2004-06-15
申请号：EEP200000501
申请日：1999-02-18
申请人： AVENTIS PHARMA INC
发明人： DUMONT JENNIFER ANN , BITONTI ALAN JOSEPH , BORCHERDING DAVID ROGER , PEET NORTON PAUL , MUNSON HARRY RANDALL , SHUM PATRICK WAI-KWOK
IPC分类号： A61K31/52 , A61P25/00 , A61P35/00 , A61P35/02 , C07D473/16
摘要： The present invention provides novel compounds of formula (I) wherein R is selected from the group consisting of R2, R2NH-, or H2N-R3- wherein R2 is selected from the group consisting of C1-C8 alkyl and formula (II), wherein Z is selected from the group consisting of phenyl, heterocycle and cycloalkyl, each R4 is independently hydrogen or C1-C4 alkyl, and n is an integer 1-8; wherein each C1-C8 alkyl and Z is optionally substituted with 1 to 3 substituents, which may be the same or different, selected from the group consisting of Hal, OH, and C1-C4 alkyl; R3 is C1-C8 alkylene; and R1 is selected from the group consisting of cyclopentyl and isopropyl, and the pharmaceutically acceptable salts, optical isomers, and hydrates thereof. In addition, the present invention provides a method of inhibiting cell cycle progression. More specifically, the present invention provides a method of inhibiting cyclin dependent kinases, particularly cdk-2. The present invention also provides a method of preventing apoptosis in neuronal cells and a method of inhibiting the development of neoplasms. In addition, the present invention provides a composition comprising an assayable amount of a compound of formula (I) in admixture or otherwise in association with an inert carrier. The present invention also provides a pharmaceutical composition comprising an effective inhibitory amount of a compound of formula (I) in admixture or otherwise in association with one or more pharmaceutically acceptable carriers or excipients.

26. 发明专利

DE69912248D1 未知
公开(公告)号：DE69912248D1
公开(公告)日：2003-11-27
申请号：DE69912248
申请日：1999-02-18
申请人： AVENTIS PHARMA INC
发明人： DUMONT JENNIFER ANN , BITONTI ALAN JOSEPH , BORCHERDING DAVID ROGER , PEET NORTON PAUL , MUNSON HARRY RANDALL , SHUM PATRICK WAI-KWOK
IPC分类号： C07D473/16 , A61K31/52 , A61P35/00 , C07D473/00
摘要： Compounds of Formula (I) wherein R is selected from the group consisting of R2, R2NH-, or R3R4N-R5-, and R1 is selected from the group consisting of cyclopentyl, cyclopentenyl and isopropyl, and the pharmaceutically acceptable salts, optical isomers, and hydrates thereof. The invention provides a method of inhibiting cell cycle progression, a method of inhibiting cyclin dependent kinases, particularly cdk-2, a method of preventing apoptosis in neuronal cells and a method of inhibiting the development of neoplasms, a composition comprising an assayable amount of a compound of Formula (I) in admixture or otherwise in association with an inert carrier, and a pharmaceutical composition comprising an effective inhibitory amount of a compound of Formula (I) in admixture or otherwise in association with one or more pharmaceutically acceptable carriers or excipients. (І)

27. 发明专利

NO315161B1 未知
公开(公告)号：NO315161B1
公开(公告)日：2003-07-21
申请号：NO984349
申请日：1998-09-18
申请人： AVENTIS PHARMA INC
发明人： PEET NORTON PAUL , WEIDNER JOHN JOSEPH
IPC分类号： C07C231/10 , C07C231/12 , C07C235/16 , C07D307/91 , C07J41/00
摘要： The present invention is a process of converting a hydroxy aromatic into a 2-hydroxy-N-arylacetamide, comprising: (1) treating a reaction mixture comprising a salt of a hydroxy aromatic with an alkylating agent; and (2) treating the reaction mixture with a Smiles solvent system and raising the temperature of the reaction mixture.

28. 发明专利

DE69620627T2 未知
公开(公告)号：DE69620627T2
公开(公告)日：2002-10-17
申请号：DE69620627
申请日：1996-09-06
申请人： AVENTIS PHARMA INC
发明人： MALIKAYL JOY ANTONY , BURKHART JOSEPH PAUL , BROERSMA ROBERT JAMES , PEET NORTON PAUL
IPC分类号： A61K38/55 , A61K31/00 , A61K38/00 , A61P7/00 , A61P7/02 , C07K5/06 , C07K5/075 , C07K5/08 , C07K5/087 , C07K5/097 , C07K5/065 , A61K38/06
摘要： This invention relates to polyfluoroalkyl tryptophan tripeptides and to compositions containing them. The compounds are highly selective thrombin inhibitors which provide anticoagulant effects useful in the treatment of thrombin conditions and in preventing the coagulation of stored whole blood and blood products.

29. 发明专利

DK0863916T3 未知
公开(公告)号：DK0863916T3
公开(公告)日：2002-07-29
申请号：DK96931485
申请日：1996-09-06
申请人： AVENTIS PHARMA INC
发明人： MALIKAYL JOY ANTONY , BURKHART JOSEPH PAUL , BROERSMA ROBERT JAMES , PEET NORTON PAUL
IPC分类号： A61K38/55 , A61K31/00 , A61K38/00 , A61P7/00 , A61P7/02 , C07K5/06 , C07K5/075 , C07K5/08 , C07K5/087 , C07K5/097 , C07K5/065 , A61K38/06
摘要： This invention relates to polyfluoroalkyl tryptophan tripeptides and to compositions containing them. The compounds are highly selective thrombin inhibitors which provide anticoagulant effects useful in the treatment of thrombin conditions and in preventing the coagulation of stored whole blood and blood products.

30. 发明专利

EE200000489A 未知
公开(公告)号：EE200000489A
公开(公告)日：2002-04-15
申请号：EEP200000489
申请日：1999-02-18
申请人： AVENTIS PHARMA INC
发明人： DUMONT JENNIFER ANN , BITONTI ALAN JOSEPH , BORCHERDING DAVID ROGER , PEET NORTON PAUL , MUNSON HARRY RANDALL , SHUM PATRICK WAI-KWOK
IPC分类号： C07D473/16 , A61K31/52 , A61P25/00 , A61P35/00 , A61P35/02 , A61P43/00 , C07D473/00

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