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公开(公告)号：WO03068748A9
公开(公告)日：2004-10-07
申请号：PCT/EP0301112
申请日：2003-02-05
Applicant: HOFFMANN LA ROCHE
Inventor： BOEHRINGER MARKUS , LOEFFLER BERND MICHAEL , PETERS JENS-UWE , RIEMER CLAUS , WEISS PETER
IPC: A61K31/435 , A61K31/4355 , A61K31/436 , A61K31/4365 , A61K31/47 , A61K31/4743 , A61P1/00 , A61P1/04 , A61P3/00 , A61P3/04 , A61P3/10 , A61P7/10 , A61P9/12 , A61P43/00 , C07D215/38 , C07D221/10 , C07D221/16 , C07D491/04 , C07D491/048 , C07D491/052 , C07D495/04
CPC classification number: C07D215/38 , C07D221/16 , C07D491/04 , C07D495/04
Abstract: The present invention relates to compounds of formula (I), wherein R , R , R and R are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with DPP IV, such as diabetes, particularly non-insulin dependent diabetes mellitus, and impaired glucose tolerance.
Abstract translation: 本发明涉及式（I）化合物，其中R 1，R 2，R 3和R 4如说明书和权利要求书中所定义，及其药学上可接受的盐。 所述化合物可用于治疗和/或预防与DPP IV相关的疾病，例如糖尿病，特别是非胰岛素依赖性糖尿病和葡萄糖耐量异常。
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公开(公告)号：WO03068757A9
公开(公告)日：2004-10-07
申请号：PCT/EP0301107
申请日：2003-02-05
Applicant: HOFFMANN LA ROCHE
Inventor： BOEHRINGER MARKUS , LOEFFLER BERND MICHAEL , PETERS JENS-UWE , STEGER MATTHIAS , WEISS PETER
IPC: A61K31/4418 , A61K31/443 , A61K31/505 , A61K31/506 , A61K31/5377 , A61P1/04 , A61P3/00 , A61P3/04 , A61P3/10 , A61P7/10 , A61P9/12 , C07D213/73 , C07D239/42 , C07D401/04 , C07D403/04 , C07D405/04 , C07D409/04
CPC classification number: C07D213/73 , C07D239/42 , C07D401/04 , C07D405/04 , C07D409/04
Abstract: The present invention relates to compounds of formula (I), wherein R , R , R , R and X are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with DPP IV, such as diabetes, particularly non-insulin dependent diabetes mellitus, and impaired glucose tolerance.
Abstract translation: 本发明涉及式（I）化合物，其中R 1，R 2，R 3，R 4和X如说明书和权利要求中所定义，及其药学上可接受的盐。 所述化合物可用于治疗和/或预防与DPP IV相关的疾病，例如糖尿病，特别是非胰岛素依赖性糖尿病和葡萄糖耐量异常。
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公开(公告)号：ES2345096T3
公开(公告)日：2010-09-15
申请号：ES03704536
申请日：2003-02-05
Applicant: HOFFMANN LA ROCHE
Inventor： BOEHRINGER MARKUS , LOEFFLER BERND MICHAEL , PETERS JENS-UWE , STEGER MATTHIAS , WEISS PETER
IPC: C07D239/42 , A61K31/4418 , A61K31/443 , A61K31/505 , A61K31/506 , A61K31/5377 , A61P1/04 , A61P3/00 , A61P3/04 , A61P3/10 , A61P7/10 , A61P9/12 , C07D213/73 , C07D401/04 , C07D403/04 , C07D405/04 , C07D409/04
Abstract: Compuestos de fórmula (I) **(Ver fórmula)** en donde X es N o C-R5; R1 y R2 son independientemente hidrógeno o alquilo inferior; R3 es heterociclilo; un heterociclilo mono-, di-, o tri-sustituido, independientemente, por alquilo inferior, alcoxilo inferior, perfluoro-alquilo inferior, amino o halógeno; arilo; o arilo mono-, di-, o tri-sustituido, independientemente, por halógeno, alquilo inferior, alcoxilo inferior, amino o perfluoro-alquilo inferior; R4 es alquilo inferior; alcoxilo inferior; tioalquilo inferior; heterociclilo; heterociclilo mono-, di-, o tri-sustituido, independientemente, por alquilo inferior, alcoxilo inferior, perfluoro-alquilo inferior, amino o halógeno; arilo; arilo mono-, di-, o tri-sustituido, independientemente, por alquilo inferior, alcoxilo inferior, halógeno, amino, o perfluoro-alquilo inferior; ariloxilo alquilo inferior o cicloalquilo; R5 es hidrógeno o alquilo inferior; y sales de los mismos farmacéuticamente aceptables en donde el término "inferior" se utiliza para designar un grupo que comprende de uno a seis átomos de carbono.
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公开(公告)号：DE602004011255D1
公开(公告)日：2008-02-21
申请号：DE602004011255
申请日：2004-11-02
Applicant: HOFFMANN LA ROCHE
Inventor： HILPERT HANS , HUMM ROLAND , KNOPP DIETMAR , WEISS PETER
Abstract: The present invention relates to phosphinic acid derivatives of formula I wherein R 1 , R 2 , R 3 and R 4 are described hereinabove. These compounds can be used in the treatment or prevention of a disease related to the inhibition of beta-secretase, inter alia for the treatment of Alzheimer's disease.
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公开(公告)号：AU2003206834B2
公开(公告)日：2006-10-19
申请号：AU2003206834
申请日：2003-02-05
Applicant: HOFFMANN LA ROCHE
Inventor： RIEMER CLAUS , LOEFFLER BERND MICHAEL , WEISS PETER , PETERS JENS-UWE , BOEHRINGER MARKUS
IPC: C07D215/38 , A61K31/435 , A61K31/4355 , A61K31/436 , A61K31/4365 , A61K31/47 , A61K31/4743 , A61P1/00 , A61P1/04 , A61P3/00 , A61P3/04 , A61P3/10 , A61P7/10 , A61P9/12 , A61P43/00 , C07D221/10 , C07D221/16 , C07D491/04 , C07D491/048 , C07D491/052 , C07D495/04
Abstract: The present invention provides compounds of formula (I)wherein R , R , R and R are as defined in the specification, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with DPP IV, such as diabetes, particularly non-insulin dependent diabetes mellitus, and impaired glucose tolerance.
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Patent Agency Ranking
公开(公告)号：AU2003206833B2
公开(公告)日：2006-07-20
申请号：AU2003206833
申请日：2003-02-05
Applicant: HOFFMANN LA ROCHE
Inventor： STEGER MATTHIAS , PETERS JENS-UWE , WEISS PETER , BOEHRINGER MARKUS , LOEFFLER BERND MICHAEL
IPC: C07D239/42 , A61K31/4418 , A61K31/443 , A61K31/505 , A61K31/506 , A61K31/5377 , A61P1/04 , A61P3/00 , A61P3/04 , A61P3/10 , A61P7/10 , A61P9/12 , C07D213/73 , C07D401/04 , C07D403/04 , C07D405/04 , C07D409/04
Abstract: The present invention provides compounds of formula (I) wherein R 1 , R 2 , R 3 , R 4 and X are as defined in the specification, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with DPP IV, such as diabetes, particularly non-insulin dependent diabetes mellitus, and impaired glucose tolerance.
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公开(公告)号：AT309988T
公开(公告)日：2005-12-15
申请号：AT03704539
申请日：2003-02-05
Applicant: HOFFMANN LA ROCHE
Inventor： BOEHRINGER MARKUS , LOEFFLER BERND MICHAEL , PETERS JENS-UWE , RIEMER CLAUS , WEISS PETER
IPC: A61K31/435 , A61K31/4355 , A61K31/436 , A61K31/4365 , A61K31/47 , A61K31/4743 , A61P1/00 , A61P1/04 , A61P3/00 , A61P3/04 , A61P3/10 , A61P7/10 , A61P9/12 , A61P43/00 , C07D215/38 , C07D221/10 , C07D221/16 , C07D491/04 , C07D491/048 , C07D491/052 , C07D495/04
Abstract: The present invention provides compounds of formula (I)wherein R , R , R and R are as defined in the specification, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with DPP IV, such as diabetes, particularly non-insulin dependent diabetes mellitus, and impaired glucose tolerance.
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8.发明专利
公开(公告)号：AU2004287586A1
公开(公告)日：2005-05-19
申请号：AU2004287586
申请日：2004-11-02
Applicant: HOFFMANN LA ROCHE
Inventor： HILPERT HANS , KNOPP DIETMAR , WEISS PETER , HUMM ROLAND
Abstract: The present invention relates to phosphinic acid derivatives of formula I wherein R 1 , R 2 , R 3 and R 4 are described hereinabove. These compounds can be used in the treatment or prevention of a disease related to the inhibition of beta-secretase, inter alia for the treatment of Alzheimer's disease.
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公开(公告)号：BR0307576A
公开(公告)日：2005-01-11
申请号：BR0307576
申请日：2003-02-05
Applicant: HOFFMANN LA ROCHE
Inventor： BOEHRINGER MARKUS , LOEFFLER BERND MICHAEL , PETERS JENS-UWE , RIEMER CLAUS , WEISS PETER
IPC: A61K31/435 , A61K31/4355 , A61K31/436 , A61K31/4365 , A61K31/47 , A61K31/4743 , A61P1/00 , A61P1/04 , A61P3/00 , A61P3/04 , A61P3/10 , A61P7/10 , A61P9/12 , A61P43/00 , C07D215/38 , C07D221/10 , C07D221/16 , C07D491/04 , C07D491/048 , C07D491/052 , C07D495/04
Abstract: The present invention provides compounds of formula (I)wherein R , R , R and R are as defined in the specification, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with DPP IV, such as diabetes, particularly non-insulin dependent diabetes mellitus, and impaired glucose tolerance.
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公开(公告)号：PA8566101A1
公开(公告)日：2003-12-19
申请号：PA8566101
申请日：2003-02-10
Applicant: HOFFMANN LA ROCHE
Inventor： JENS-UWE PETERS , BOEHRINGER MARKUS , LOEFFLER BERND MICHAEL , STEGER MATTHIAS , WEISS PETER
IPC: A61K31/401 , A61K31/4418 , A61K31/443 , A61K31/505 , A61K31/506 , A61K31/5377 , A61K31/69 , A61P1/04 , A61P3/00 , A61P3/04 , A61P3/10 , A61P7/10 , A61P9/12 , C07D207/16 , C07D213/73 , C07D239/42 , C07D401/04 , C07D403/04 , C07D405/04 , C07D409/04
Abstract: LA PRESENTE INVENCION SE REFIERE A COMPUESTOS DE FORMULA (I) DONDE R1, R2, R3, R4 Y X SON TAL COMO SE DEFINE EN LA DESCRIPCION Y REIVINDICACIONES, Y SALES FARMACEUTICAMENTE ACEPTABLES DE LOS MISMOS. LOS COMPUESTOS SON UTILES PARA EL TRATAMIENTO Y/O PREVENCION DE ENFERMEDADES QUE ESTAN ASOCIADAS CON DPP IV, COMO DIABETES, PARTICULARMENTE DIABETES MELLITUS NO DEPENDIENTE DE INSULINA, Y DISMINUCION DE LA TOLERANCIA A LA GLUCOSA.
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