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1. 发明专利

PL194174B1 6,9-DISUBSTITUTED 2-[TRANS(4-AMINOCYCLOHEXYL)AMINO]PURIN 未知
公开(公告)号：PL194174B1
公开(公告)日：2007-05-31
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

2. 发明专利

EE04815B1 未知
公开(公告)号：EE04815B1
公开(公告)日：2007-04-16
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： A61K31/52 , C07D473/16 , A61P25/00 , A61P35/00 , A61P35/02 , A61P43/00 , C07D473/00

3. 发明专利

PT1056744E 未知
公开(公告)号：PT1056744E
公开(公告)日：2004-03-31
申请号：PT99908220
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)

4. 发明专利

NZ506234A 6,9-Disubstituted 2-[trans-(4-aminocyclohexyl)amino]purines, pharmaceuticals thereof and their use for inhibiting cdk-2 未知
公开(公告)号：NZ506234A
公开(公告)日：2003-05-30
申请号：NZ50623499
申请日：1999-02-18
申请人： AVENTIS PHARMA INC
发明人： PEET NORTON PAUL , MUNSON HARRY RANDALL , SHUM PATRICK WAI-KWOK , DUMONT JENNIFER ANN , BORCHERDING DAVID ROGER , BITONTI ALAN JOSEPH
IPC分类号： A61K31/52 , A61P25/00 , A61P35/00 , A61P35/02 , C07D473/16 , A61P43/00
摘要： A compound of formula (I); where: R is R2, R2NH-, or H2N-R3-; R2 is C1-C8 alkyl or a group of formula (II); Z is phenyl, heterocycle or cycloalkyl; R4 is H or C1-C4 alkyl; n is an integer of 1-8; Each C1-C8 alkyl and Z is optionally substituted with 1 to 3 substituents, independently selected from Hal, OH, and C1-C4alkyl; R3 is C1-C8 alkylene; R1 is cyclopentyl or isopropyl. Also described is a composition comprising an assayable amount of the compound described above in admixture or otherwise in association with an inert carrier. Also described is a pharmaceutical composition comprising an effective cdk-2 inhibiting amount of the compound described above in admixture or otherwise in association with one or more pharmaceutically acceptable carriers or excipients. The compounds of formula (I) are useful for treating hyperproliferative disorders. The compounds of formula (I) are also useful for preventing apoptosis in neuronal cells.

5. 发明专利

PT863916E 未知
公开(公告)号：PT863916E
公开(公告)日：2002-07-31
申请号：PT96931485
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.

6. 发明专利

EE200000501A 未知
公开(公告)号：EE200000501A
公开(公告)日：2002-02-15
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.

7. 发明专利

HK1030949A1 6,9-DISUBSTITUTED 2-[TRANS-(4-AMINOCYCLOHEXYL)AMINO]PURINES 未知
公开(公告)号：HK1030949A1
公开(公告)日：2001-05-25
申请号：HK01101932
申请日：2001-03-16
申请人： AVENTIS PHARMA INC
发明人： DUMONT JENNIFER ANN , BORCHERDING DAVID ROGER , MUNSON HARRY RANDALL , BITONTI ALAN JOSEPH , PEET NORTON PAUL , SHUM PATRICK WAI-KWOK
IPC分类号： C07D473/16 , A61K31/52 , A61P35/00 , C07D473/00 , C07D , A61K
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)

8. 发明专利

ES2207182T3 未知
公开(公告)号：ES2207182T3
公开(公告)日：2004-05-16
申请号：ES99908220
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
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)

9. 发明专利

PL344021A1 6,9-DISUBSTITUTED 2-[TRANS-(4- AMINOCYCLOHEXYL) AMINO]PURINES 未知
公开(公告)号：PL344021A1
公开(公告)日：2001-09-24
申请号：PL34402199
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.

10. 发明专利

NO20004280L 未知
公开(公告)号：NO20004280L
公开(公告)日：2000-10-25
申请号：NO20004280
申请日：2000-08-25
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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