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公开(公告)号：EP1951696A2
公开(公告)日：2008-08-06
申请号：EP06844335.7
申请日：2006-11-13
申请人： Amgen Inc. , BIOVITRUM AB
发明人： HENRIKSSON, Martin , HOMAN, Evert , JOHANSSON, Lars , VALLGARDA, Jerk , WILLIAMS, Meredith , BERCOT, Eric, A. , FOTSCH, Christopher, H. , LI, Aiwen , CAI, Guolin , HUNGATE, Randall, W. , YUAN, Chester, Chenguang , TEGLEY, Christopher , ST. JEAN, David, J., Jr. , HAN, Nianhe , HUANG, Qi , LIU, Qingyian , BARTBEGER, Michael, D. , MONIZ, George, A. , FRIZZLE, Matthew, J. , MARSHALL, Teresa, L.
IPC分类号： C07D277/54 , C07D277/60 , C07D417/04 , C07D417/06 , C07D417/12 , C07D417/14 , A61K31/426 , A61K31/427
CPC分类号： C07D277/54 , C07D277/60 , C07D417/04 , C07D417/06 , C07D417/12 , C07D417/14
摘要： The present invention relates to thiazolinones and also to pharmaceutical compositions comprising the compounds, as well as methods of use of the compounds for treatment of disorders associated with human 11-β-hydroxysteroid dehydrogenase type 1 enzyme and for the preparation of a medicament which acts on the human 11- β-hydroxysteroid dehydrogenase type 1 enzyme.
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公开(公告)号：EP1753736A2
公开(公告)日：2007-02-21
申请号：EP05756354.6
申请日：2005-05-24
申请人： Amgen Inc. , BIOVITRUM AB
发明人： HENRIKSSON, Martin , HOMAN, Evert , JOHANSSON, Lars , VALLGARDA, Jerk , WILLIAMS, Meredith , BERCOT, Eric , FOTSCH, Christopher, H. , LI, Aiwen , CAI, Guolin , HUNGATE, Randall, W. , YUAN, Chester, Chenguang , TEGLEY, Chirstopher , ST. JEAN, David , HAN, Nianhe , HUANG, Qi , LIU, Qingyian , BARTBERGER, Michael D. , MONIZ, George, A. , FRIZZLE, Matthew, J.
IPC分类号： C07D277/54 , C07D263/48 , A61K31/42 , A61K31/426 , A61P3/04 , A61P3/00 , A61P3/06 , A61P3/10 , A61P19/10 , A61P31/12 , A61P29/00 , A61P25/28 , A61P25/24
CPC分类号： C07D417/06 , C07D263/34 , C07D263/48 , C07D275/03 , C07D277/42 , C07D277/54 , C07D277/60 , C07D413/14 , C07D417/04 , C07D417/12 , C07D417/14 , C07D513/10 , C07F7/1856
摘要： The present invention relates to compounds with the formula (I), (II), (III) or (IV): (I) (II), (III), or (IV), wherein R1, R2, R3, R4, R5, R6, R7, X and Z are as defined herein, and also to pharmaceutical compositions comprising the compounds, as well as methods of use of the compounds for treatment of disorders associated with human 11-β-hydroxysteroid dehydrogenase type 1 enzyme and for the preparation of a medicament which acts on the human 11-β-hydroxysteroid dehydrogenase type 1 enzyme.
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公开(公告)号：EP1753736B1
公开(公告)日：2008-12-17
申请号：EP05756354.6
申请日：2005-05-24
申请人： Amgen Inc. , BIOVITRUM AB
发明人： HENRIKSSON, Martin , HOMAN, Evert , JOHANSSON, Lars , VALLGARDA, Jerk , WILLIAMS, Meredith , BERCOT, Eric , FOTSCH, Christopher, H. , LI, Aiwen , CAI, Guolin , HUNGATE, Randall, W. , YUAN, Chester, Chenguang , TEGLEY, Chirstopher , ST. JEAN, David , HAN, Nianhe , HUANG, Qi , LIU, Qingyian , BARTBERGER, Michael D. , MONIZ, George, A. , FRIZZLE, Matthew, J.
IPC分类号： C07D277/54 , C07D263/48 , A61K31/42 , A61K31/426 , A61P3/04 , A61P3/00 , A61P3/06 , A61P3/10 , A61P19/10 , A61P31/12 , A61P29/00 , A61P25/28 , A61P25/24
CPC分类号： C07D417/06 , C07D263/34 , C07D263/48 , C07D275/03 , C07D277/42 , C07D277/54 , C07D277/60 , C07D413/14 , C07D417/04 , C07D417/12 , C07D417/14 , C07D513/10 , C07F7/1856
摘要： The present invention relates to compounds with the formula (I), (II), (III) or (IV): (I) (II), (III), or (IV), wherein R1, R2, R3, R4, R5, R6, R7, X and Z are as defined herein, and also to pharmaceutical compositions comprising the compounds, as well as methods of use of the compounds for treatment of disorders associated with human 11-β-hydroxysteroid dehydrogenase type 1 enzyme and for the preparation of a medicament which acts on the human 11-β-hydroxysteroid dehydrogenase type 1 enzyme.
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4.发明公开
公开(公告)号：EP2051977A2
公开(公告)日：2009-04-29
申请号：EP07813049.9
申请日：2007-07-18
申请人： Amgen Inc. , Biovitrum AB
发明人： FOTSCH, Christopher, H. , BARTBERGER, Michael, D. , HARALDSSON, Martin , ST. JEAN, David , JOHANSSON, Lars , NILSSON, Marianne , SUTIN, Lori
IPC分类号： C07D403/06
CPC分类号： C07D403/06 , C07D413/06 , C07D413/12
摘要： Compounds of formula I and IV are described and have therapeutic utility, particularly in the treatment of diabetes, obesity and related conditions and disorders:formula I and IV wherein the variables A-B, R, 1, r R> 2, m, and Q are described herein.
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5.发明公开ISOXAZOLE DERIVATIVES AS MODULATORS OF 11-BETA-HYDROXYSTEROID DEHYDROGENASE TYPE 1 审中-公开异恶唑的11-β-羟基TYPE 1调节剂
公开(公告)号：EP2231650A1
公开(公告)日：2010-09-29
申请号：EP09702264.4
申请日：2009-01-16
申请人： Biovitrum AB (publ)
IPC分类号： C07D413/06 , A61K31/454 , A61P27/00
CPC分类号： C07D413/06
摘要： The present invention relates to novel isoxazole compounds of formula (I), and pharmaceutically acceptable salts, solvates, hydrates, geometrical isomers, tautomers, optical isomers or N-oxides thereof, which are modulators of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1). The invention also relates to pharmaceutical compositions comprising these compounds and to the use of these compounds in the preparation of a medicament for the treatment of glaucoma.
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6.发明公开
公开(公告)号：EP2059517A1
公开(公告)日：2009-05-20
申请号：EP07819987.4
申请日：2007-08-29
申请人： Biovitrum AB (publ)
发明人： BRANDT, Peter , JOHANSSON, Gary , JOHANSSON, Lars , KOOLMEISTER, Tobias , NILSSON, Björn M , SANDVALL, Teresa , WEBER, Michael
IPC分类号： C07D401/12 , A61K31/506 , A61P3/00 , C07D401/14
CPC分类号： A61K31/4545 , A61K31/496 , A61K45/06 , C07D401/12 , C07D401/14 , C07D405/14 , C07D413/14 , A61K2300/00
摘要： The present invention relates to compounds of Formula (1a) and pharmaceutically acceptable salts, hydrates, geometrical isomers, racemates, tautomers, optical isomers and N-oxides thereof, wherein W1 and W3 are N and W and W4 are CR12, or W1 and W3 are CR12 and W2 and W4 are N. The invention also relates to pharmaceutical compositions comprising these compounds, and to the use of these compounds for the prophylaxis and treatment of medical conditions relating to disorders of the G-protein-coupled receptor GPR119, such as diabetes and obesity.
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公开(公告)号：EP2044051B1
公开(公告)日：2010-01-27
申请号：EP07786791.9
申请日：2007-06-21
申请人： BIOVITRUM AB (publ)
发明人： JENMALM JENSEN, Annika , RINGOM, Rune , MEDINA, Carmen , SHILVOCK, John , WIIK, Marie , KOOLMEISTER, Tobias , ANGBRANT, Johan , SUTIN, Lori , HENRIKSSON, Martin , SANDVALL, Teresa , JOHANSSON, Lars , NILSSON, Björn
IPC分类号： C07D401/04 , C07D401/12 , C07D403/12 , C07D403/14 , C07D405/12 , C07D471/04
CPC分类号： C07D401/12 , C07D401/04 , C07D403/12 , C07D403/14 , C07D405/12 , C07D471/04
摘要： The present invention relates to compounds of the general formula (I) wherein X, Y, Z, A, Ar, R1, R2, R3, and R4 are as defined herein, which compounds are inhibitors of MNK2 and MNK1. The invention also relates to the use of the compounds in therapy, pharmaceutical compositions comprising the compounds, and the use of the compounds for the preparation of a medicament for the prophylaxis and treatment of disorders related to undesired activity of MNK1 and/or MNK2 kinases.
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8.发明公开
公开(公告)号：EP2059516A1
公开(公告)日：2009-05-20
申请号：EP07803008.7
申请日：2007-08-29
申请人： BIOVITRUM AB (publ)
发明人： BRANDT, Peter , EMOND, Rikard , JOHANSSON, Gary , JOHANSSON, Lars , KOOLMEISTER, Tobias , NILSSON, Björn, M. , SANDVALL, Teresa , WEBER, Michael
IPC分类号： C07D401/12 , C07D401/14 , C07D405/14 , C07D413/14 , A61K31/4545 , A61K31/496 , A61P3/00
CPC分类号： A61K31/4545 , A61K31/496 , A61K45/06 , C07D401/12 , C07D401/14 , C07D405/14 , C07D413/14 , A61K2300/00
摘要： The present invention relates to compounds of Formula (Ia) and pharmaceutically acceptable salts, hydrates, geometrical isomers, racemates, tautomers, optical isomers and N-oxides thereof, wherein one of W1 and W2 is N and the other is CR12. The invention also relates to pharmaceutical compositions comprising these compounds, and to the use of these compounds for the prophylaxis and treatment of medical conditions relating to disorders of the G-protein-coupled receptor GPRl 19, such as diabetes and obesity.
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公开(公告)号：EP2044051A1
公开(公告)日：2009-04-08
申请号：EP07786791.9
申请日：2007-06-21
申请人： BIOVITRUM AB (publ)
发明人： JENMALM JENSEN, Annika , RINGOM, Rune , MEDINA, Carmen , SHILVOCK, John , WIIK, Marie , KOOLMEISTER, Tobias , ANGBRANT, Johan , SUTIN, Lori , HENRIKSSON, Martin , SANDVALL, Teresa , JOHANSSON, Lars , NILSSON, Björn
IPC分类号： C07D401/04 , C07D401/12 , C07D403/12 , C07D403/14 , C07D405/12 , C07D471/04
CPC分类号： C07D401/12 , C07D401/04 , C07D403/12 , C07D403/14 , C07D405/12 , C07D471/04
摘要： The present invention relates to compounds of the general formula (I) wherein X, Y, Z, A, Ar, R1, R2, R3, and R4 are as defined herein, which compounds are inhibitors of MNK2 and MNK1. The invention also relates to the use of the compounds in therapy, pharmaceutical compositions comprising the compounds, and the use of the compounds for the preparation of a medicament for the prophylaxis and treatment of disorders related to undesired activity of MNK1 and/or MNK2 kinases.
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