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公开(公告)号：DE69918062T2
公开(公告)日：2005-06-02
申请号：DE69918062
申请日：1999-02-18
Applicant: AVENTIS PHARMA INC
Inventor： DUMONT A , BITONTI J , BORCHERDING R , PEET P , MUNSON RANDALL , SHUM W
IPC: A61K31/52 , A61P25/00 , A61P35/00 , A61P35/02 , C07D473/16
Abstract: 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.
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公开(公告)号：DE69707844D1
公开(公告)日：2001-12-06
申请号：DE69707844
申请日：1997-02-25
Applicant: AVENTIS PHARMA INC
IPC: C07C231/10 , C07C231/12 , C07C235/16 , C07D307/91 , C07J41/00
Abstract: 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.
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公开(公告)号：DE69531459T2
公开(公告)日：2004-06-24
申请号：DE69531459
申请日：1995-05-05
Applicant: AVENTIS PHARMA INC
Inventor： METZ A , GALLION L , BURKHART P , ANGELASTRO R , PEET P
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公开(公告)号：DE69523072D1
公开(公告)日：2001-11-08
申请号：DE69523072
申请日：1995-12-15
Applicant: AVENTIS PHARMA INC
Inventor： PEET P , MEHDI SHUJAATH , LINNIK D , ANGELASTRO R , KIM HWA-OK
IPC: 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
Abstract: 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.
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公开(公告)号：DE69523072T2
公开(公告)日：2002-06-20
申请号：DE69523072
申请日：1995-12-15
Applicant: AVENTIS PHARMA INC
Inventor： PEET P , MEHDI SHUJAATH , LINNIK D , ANGELASTRO R , KIM HWA-OK
IPC: 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
Abstract: 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.
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Patent Agency Ranking
公开(公告)号：DE69918062D1
公开(公告)日：2004-07-22
申请号：DE69918062
申请日：1999-02-18
Applicant: AVENTIS PHARMA INC
Inventor： DUMONT A , BITONTI J , BORCHERDING R , PEET P , MUNSON RANDALL , SHUM W
IPC: A61K31/52 , A61P25/00 , A61P35/00 , A61P35/02 , C07D473/16
Abstract: 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.
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公开(公告)号：DE69531459D1
公开(公告)日：2003-09-11
申请号：DE69531459
申请日：1995-05-05
Applicant: AVENTIS PHARMA INC
Inventor： METZ A , GALLION L , BURKHART P , ANGELASTRO R , PEET P
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公开(公告)号：DE69710217T2
公开(公告)日：2002-08-08
申请号：DE69710217
申请日：1997-09-12
Applicant: AVENTIS PHARMA INC
IPC: C07D213/68 , C07D213/73 , C07D215/38 , C07D215/40 , C07D215/42 , C07D219/06 , C07D219/08
Abstract: A process of converting a hydroxy heteroaromatic compound to an arylamine, comprising the steps of : 1) treating a salt of a hydroxy heteroaromatic compound with an alkylating agent; and 2) treating the reaction mixture with a Smiles solvent system and raising the temperature of the reaction mixture; and a compound made according to the above process.
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公开(公告)号：DE69707844T2
公开(公告)日：2002-06-27
申请号：DE69707844
申请日：1997-02-25
Applicant: AVENTIS PHARMA INC
IPC: C07C231/10 , C07C231/12 , C07C235/16 , C07D307/91 , C07J41/00
Abstract: 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.
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公开(公告)号：DE69710217D1
公开(公告)日：2002-03-14
申请号：DE69710217
申请日：1997-09-12
Applicant: AVENTIS PHARMA INC
IPC: C07D213/68 , C07D213/73 , C07D215/38 , C07D215/40 , C07D215/42 , C07D219/06 , C07D219/08
Abstract: A process of converting a hydroxy heteroaromatic compound to an arylamine, comprising the steps of : 1) treating a salt of a hydroxy heteroaromatic compound with an alkylating agent; and 2) treating the reaction mixture with a Smiles solvent system and raising the temperature of the reaction mixture; and a compound made according to the above process.
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