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21. 发明授权

US08524710B2 Pyrrolidine derivatives 有权
标题翻译：吡咯烷衍生物
公开(公告)号：US08524710B2
公开(公告)日：2013-09-03
申请号：US13279364
申请日：2011-10-24
申请人： David Banner , Uwe Grether , Wolfgang Haap , Holger Kuehne , Harald Mauser , Jean-Marc Plancher
发明人： David Banner , Uwe Grether , Wolfgang Haap , Holger Kuehne , Harald Mauser , Jean-Marc Plancher
IPC分类号： C07D401/04 , C07D487/04 , A61K31/506
CPC分类号： C07D403/04 , C07D401/04 , C07D413/04 , C07D487/04
摘要： The invention relates to a compound of formula (I) wherein A1 to A4 and R1 to R6 are defined as in the description and in the claims. The compound of formula (I) can be used, for example, as inhibitors of the cysteine protease cathepsin.
摘要翻译：本发明涉及式（I）化合物，其中A1至A4和R1至R6如在说明书和权利要求书中所定义。式（I）化合物可用作例如半胱氨酸蛋白酶组织蛋白酶的抑制剂。

22. 发明申请

US20120115843A1 NOVEL PYRROLIDINE DERIVATIVES 有权
标题翻译：新型吡咯烷衍生物
公开(公告)号：US20120115843A1
公开(公告)日：2012-05-10
申请号：US13279364
申请日：2011-10-24
申请人： David Banner , Uwe Grether , Wolfgang Haap , Holger Kuehne , Harald Mauser , Jean-Marc Plancher
发明人： David Banner , Uwe Grether , Wolfgang Haap , Holger Kuehne , Harald Mauser , Jean-Marc Plancher
IPC分类号： A61K31/5377 , A61K31/506 , C07D403/04 , A61P9/00 , A61P3/10 , A61P9/10 , A61P35/00 , C07D413/14 , A61K31/497
CPC分类号： C07D403/04 , C07D401/04 , C07D413/04 , C07D487/04
摘要： The invention relates to a compound of formula (I) wherein A1 to A4 and R1 to R6 are defined as in the description and in the claims. The compound of formula (I) can be used, for example, as inhibitors of the cysteine protease cathepsin.
摘要翻译：本发明涉及式（I）化合物，其中A1至A4和R1至R6如在说明书和权利要求书中所定义。式（I）化合物可用作例如半胱氨酸蛋白酶组织蛋白酶的抑制剂。

23. 发明授权

US08158655B2 Sulfonamide derivatives 失效
标题翻译：磺酰胺衍生物
公开(公告)号：US08158655B2
公开(公告)日：2012-04-17
申请号：US11970628
申请日：2008-01-08
申请人： David Banner , Harald Mauser , Rudolf E. Minder , Hans P. Wessel
发明人： David Banner , Harald Mauser , Rudolf E. Minder , Hans P. Wessel
IPC分类号： A61K31/4427 , A61K31/38 , C07D333/52 , C07D409/02
CPC分类号： C07D333/62 , C07D213/42 , C07D401/12 , C07D403/12 , C07D409/12
摘要： The invention is concerned with the novel sulfonamide derivatives of formula (I) wherein A, R1 to R2″, X and Y are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit chymase and can be used as medicaments.
摘要翻译：本发明涉及式（I）的新型磺酰胺衍生物，其中A，R 1至R 2“，X和Y如说明书和权利要求书中所定义，以及其生理上可接受的盐。这些化合物抑制胃促胰酶，可用作药物。

24. 发明申请

US20110144098A1 AMINO OXAZINE DERIVATIVES 有权
标题翻译：氨基氧化合物衍生物
公开(公告)号：US20110144098A1
公开(公告)日：2011-06-16
申请号：US12958436
申请日：2010-12-02
申请人： David Banner , Hans Hilpert , Harald Mauser , Alexander V. Mayweg , Mark Rogers-Evans
发明人： David Banner , Hans Hilpert , Harald Mauser , Alexander V. Mayweg , Mark Rogers-Evans
IPC分类号： A61K31/5365 , C07D413/12 , A61K31/5355 , C07D413/14 , A61K31/537 , A61P3/10
CPC分类号： C07D413/12 , C07D265/08 , C07D417/12 , C07D495/04 , C07D498/04
摘要： This invention relates to 5,6-dihydro-4H-[1,3]oxazin-2-ylamine compounds of the formula wherein R1 to R5 are as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds are BACE2 inhibitors and can be used as medicaments for the treatment or prevention of diseases such as diabetes.
摘要翻译：本发明涉及下式的5,6-二氢-4H- [1,3]恶嗪-2-基胺化合物，其中R1至R5如说明书和权利要求书中所定义，以及其药学上可接受的盐。这些化合物是BACE2抑制剂，可用作治疗或预防糖尿病等疾病的药物。

25. 发明授权

US07696240B2 Fused pyrrole derivatives 失效
标题翻译：熔融吡咯衍生物
公开(公告)号：US07696240B2
公开(公告)日：2010-04-13
申请号：US11634584
申请日：2006-12-05
申请人： David Banner , Hans Hilpert , Bernd Kuhn , Harald Mauser
发明人： David Banner , Hans Hilpert , Bernd Kuhn , Harald Mauser
IPC分类号： A61K31/404 , C07D209/10 , C07D209/12
CPC分类号： C07D209/42 , C07D401/06 , C07D403/06 , C07D405/06 , C07D409/06 , C07D471/04 , C07D491/04 , C07D495/04
摘要： The invention is concerned with novel fused pyrrole derivatives of formula (I) wherein A, Ar, R1, R2, R2′ and R2″ and n are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit chymase and can be used as medicaments.
摘要翻译：本发明涉及式（I）的新型稠合吡咯衍生物，其中A，Ar，R 1，R 2，R 2'和R 2“和n如说明书和权利要求书中所定义，以及其生理上可接受的盐。这些化合物抑制胃促胰酶，可用作药物。

26. 发明申请

US20070129421A1 Vinylogous acid derivatives 失效
标题翻译： Vinylogous酸衍生物
公开(公告)号：US20070129421A1
公开(公告)日：2007-06-07
申请号：US11605016
申请日：2006-11-28
申请人： David Banner , Hans Hilpert , Bernd Kuhn , Harald Mauser
发明人： David Banner , Hans Hilpert , Bernd Kuhn , Harald Mauser
IPC分类号： A61K31/404 , C07D403/02
CPC分类号： C07D403/06 , C07D209/12 , C07D209/14 , C07D405/06 , C07D409/14 , C07D487/04
摘要： The invention is concerned with vinylogous acids derivatives of formula (I) wherein A and R1 to R6 are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit chymase and can be used as medicaments.
摘要翻译：本发明涉及式（I）的维酸类衍生物，其中A和R 1至R 6如说明书和权利要求书中所定义，以及生理学上其可接受的盐。这些化合物抑制胃促胰酶，可用作药物。

27. 发明申请

US20140162936A1 NEW CHYMASE BINDING COMPOUNDS AND MEDICAL USES THEREOF 有权
标题翻译：新型化合物结合物及其医疗用途
公开(公告)号：US20140162936A1
公开(公告)日：2014-06-12
申请号：US14119002
申请日：2012-04-24
申请人： Simon Brack , Sarah Batey , Dragan Grabulovski , Julian Bertschinger , Daniel Schlatter , Jörg Benz , David Banner , Michael Hennig
发明人： Simon Brack , Sarah Batey , Dragan Grabulovski , Julian Bertschinger , Daniel Schlatter , Jörg Benz , David Banner , Michael Hennig
IPC分类号： C12N9/12 , G01N33/573
CPC分类号： C12N9/12 , C07K14/4703 , C12N9/1205 , G01N33/573
摘要： The present invention relates to a polypeptide binding to a chymase (EC 3, 4, 21,39), wherein the polypeptide comprises or consists of an amino acid sequence selected from the group consisting of: (a) GVTLFVALYDY(X1)A(X2)(X3)(X4)(X5) (X6)LSFHKGEKFQIL(X7 (X8)(X9)(X10) (X11)(X12)G(X13)(X14)WEARSLTTGETGYIPSNYVAPVDSIQ (SEQ ID NO: 1), wherein (X1) is R, N, Q, E, K, H, S, T, C, or D; (X2) is E, T, D, Q, L, P, A, S, C, M, N, E, G, A, V or I; (X3) is R, T, H, N, K, S, C, N or Q; (X4) is S, W, T, C, N, Q, For Y; (X5) is T, H, L, F, C, S, M, N, Q, R, K, G, A, V, I, P, Y or W; (X6) is D, Q, H, E, S, T, C, N, R or K; (X7) is D, N, R, E, Q, S, T, C, K or D; (X8) is M, W, G, F, A, S, T, C, S, N, Q, Y, V, L, I or P; (X9) is T, H, S, D, C, N, Q, R, K, E or absent; (X10) is V, T, Q, G, A, L, I, P, S, C, M, N or absent; (X11) is P, A, D, G, K, V, L, I, E, R, M, H or absent; (X12) is N, V, P, I, E, T, S, A, G, L, C, M, Q or D; (X13) is D, E, T, P, G, A, V, L, I, S, C, M, N or Q, and (X14) is W, Y, L, G, A, V, I, P, M, or F; (b) an amino acid sequence which is at least 85% identical to the amino acid sequence of (a), wherein the identity determination excludes amino acid positions (X1) to (X14).
摘要翻译：本发明涉及与胃促胰酶（EC3,4,21,39）结合的多肽，其中所述多肽包含选自以下的氨基酸序列或由以下组成：（a）GVTLFVALYDY（X1）A（X2 ）（X4）（X5）（X6）（X6）LSFHKGEKFQIL（X7（X8）（X9）（X10）（X11）（X12）G（X13）（X14）WEARSLTTGETGYIPSNYVAPVDSIQ（SEQ ID NO：1））是R，N，Q，E，K，H，S，T，C或D;（X2）是E，T，D，Q，L，P，A，S，C，M，N，E （X 4）为S，W，T，C，N，Q，Y为Y; （X5）是T，H，L，F，C，S，M，N，Q，R，K，G，A，V，I，P，Y或W;（X6） E，S，T，C，N，R或K;（X7）为D，N，R，E，Q，S，T，C，K或D;（X8）为M，W，G， A，S，T，C，S，N，Q，Y，V，L，I或P;（X9）是T，H，S，D，C，N，Q，R，K，E或不存在; （X10）是V，T，Q，G，A，L，I，P，S，C，M，N或不存在;（X11）是P，A，D，G，K，V，L， E，R，M，H或不存在;（X12）为N，V，P，I，E，T，S，A，G，L，C，M，Q或D;（X13） T，P，G，A，V，L，I，S，C，M，N或Q，（X14）是W，Y，L，G， A，V，I，P，M或F; （b）与（a）的氨基酸序列至少85％相同的氨基酸序列，其中所述身份确定不包括氨基酸位置（X1）至（X14）。

28. 发明授权

US08673894B2 2,5,6,7-tetrahydro-[1,4]oxazepin-3-ylamine or 2,3,6,7-tetrahydro-[1,4]oxazepin-5-ylamine compounds 失效
标题翻译： 2,5,6,7-四氢 - [1,4]氧氮杂-3-基胺或2,3,6,7-四氢 - [1,4]氧氮杂-5-基胺化合物
公开(公告)号：US08673894B2
公开(公告)日：2014-03-18
申请号：US13096059
申请日：2011-04-28
申请人： David Banner , Wolfgang Guba , Hans Hilpert , Roland Humm , Harald Mauser , Alexander V. Mayweg , Robert Narquizian , Eoin Power , Mark Rogers-Evans , Didier Rombach , Thomas Woltering , Wolfgang Wostl
发明人： David Banner , Wolfgang Guba , Hans Hilpert , Roland Humm , Harald Mauser , Alexander V. Mayweg , Robert Narquizian , Eoin Power , Mark Rogers-Evans , Didier Rombach , Thomas Woltering , Wolfgang Wostl
IPC分类号： A61P25/28 , A61K31/553 , C07D267/10 , C07D413/12 , C07D417/12
CPC分类号： C07D267/10 , C07D413/12 , C07D417/12
摘要： This invention relates to compounds of the formula wherein A, B and R1 to R7 are as described below, or to pharmaceutically acceptable salts thereof. These compounds are BACE1 and/or BACE2 inhibitors and can be used as medicaments for the therapeutic and/or prophylactic treatment of diseases such as Alzheimer's disease, diabetes, particularly type 2 diabetes, and other metabolic disorders.
摘要翻译：本发明涉及下式化合物，其中A，B和R 1至R 7如下所述，或其药学上可接受的盐。这些化合物是BACE1和/或BACE2抑制剂，可用作治疗和/或预防性治疗诸如阿尔茨海默病，糖尿病，特别是2型糖尿病和其它代谢紊乱的药物。

29. 发明申请

US20120214806A1 3-AMINO-5-PHENYL-5,6-DIHYDRO-2H-[1,4]OXAZINES 审中-公开
标题翻译： 3-氨基-5-苯基-5,6-二氢-2H- [1,4]氧化物
公开(公告)号：US20120214806A1
公开(公告)日：2012-08-23
申请号：US13460905
申请日：2012-05-01
申请人： Matteo Andreini , David Banner , Emanuele Gabellieri , Wolfgang Guba , Hans Hilpert , Harald Mauser , Alexander V. Mayweg , Robert Narquizian , Eoin Power , Mark Rogers-Evans , Massimiliano Travagli , Michela Valacchi , Thomas Woltering , Wolfgang Wostl
发明人： Matteo Andreini , David Banner , Emanuele Gabellieri , Wolfgang Guba , Hans Hilpert , Harald Mauser , Alexander V. Mayweg , Robert Narquizian , Eoin Power , Mark Rogers-Evans , Massimiliano Travagli , Michela Valacchi , Thomas Woltering , Wolfgang Wostl
IPC分类号： A61K31/5377 , C07D265/30 , A61K31/5375 , C07D471/04 , C07D417/12 , C07D413/14 , A61P3/10 , A61P25/28 , A61P3/00 , A61P7/02 , A61P37/00 , A61P29/00 , A61P35/00 , A61P9/10 , A61P25/00 , A61P17/00 , A61P1/00 , A61P5/16 , A61P19/04 , A61P19/02 , C07D265/32 , C07D413/12
CPC分类号： C07D413/12 , C07D265/30 , C07D413/14 , C07D417/12 , C07D471/04
摘要： The present invention relates to 3-Amino-5-phenyl-5,6-dihydro-2H-[1,4]oxazines of formula I having BACE1 and/or BACE2 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease and type 2 diabetes.
摘要翻译：本发明涉及具有BACE1和/或BACE2抑制活性的式I的3-氨基-5-苯基-5,6-二氢-2H- [1,4]恶嗪，其制备方法，含有它们的药物组合物及其作为治疗活性物质。本发明的活性化合物可用于例如治疗和/或预防性治疗。阿尔茨海默病和2型糖尿病。

30. 发明申请

US20110046122A1 3-AMINO-5-PHENYL-5,6-DIHYDRO-2H-[1,4]OXAZINES 失效
标题翻译： 3-氨基-5-苯基-5,6-二氢-2H- [1,4]氧化物
公开(公告)号：US20110046122A1
公开(公告)日：2011-02-24
申请号：US12852538
申请日：2010-08-09
申请人： Matteo Andreini , David Banner , Wolfgang Guba , Hans Hilpert , Harald Mauser , Alexander V. Mayweg , Robert Narquizian , Eoin Power , Mark Roger-Evans , Massimiliano Travagli , Michela Valacchi , Thomas Woltering , Wolfgang Wostl
发明人： Matteo Andreini , David Banner , Wolfgang Guba , Hans Hilpert , Harald Mauser , Alexander V. Mayweg , Robert Narquizian , Eoin Power , Mark Roger-Evans , Massimiliano Travagli , Michela Valacchi , Thomas Woltering , Wolfgang Wostl
IPC分类号： A61K31/5377 , C07D413/12 , C07D265/30 , C07D409/14 , A61K31/5375 , A61P3/10 , A61P25/28 , A61P29/00 , A61P35/00 , A61P9/00 , A61P19/02
CPC分类号： C07D413/12 , C07D265/30 , C07D413/14 , C07D417/12 , C07D471/04
摘要： The present invention relates to 3-Amino-5-phenyl-5,6-dihydro-2H-[1,4]oxazines of formula I having BACE1 and/or BACE2 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease and type 2 diabetes.
摘要翻译：本发明涉及具有BACE1和/或BACE2抑制活性的式I的3-氨基-5-苯基-5,6-二氢-2H- [1,4]恶嗪，其制备方法，含有它们的药物组合物及其作为治疗活性物质。本发明的活性化合物可用于例如治疗和/或预防性治疗。阿尔茨海默病和2型糖尿病。

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