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1. 发明申请

US20130345199A1 1-[M-CARBOXAMIDO(HETERO)ARYL-METHYL]-PIPERIDINE-4-CARBOXAMIDE DERIVATIVES 审中-公开
标题翻译： 1- [M-CARBOXAMIDO（HETERO）ARYL-METHYL] - 哌啶-4-羧酰胺衍生物
公开(公告)号：US20130345199A1
公开(公告)日：2013-12-26
申请号：US13923981
申请日：2013-06-21
申请人： Heinz FRETZ , Markus Gude , Philippe Guerry , Thierry Kimmerlin , Francois Lehembre , Thomas Pfeifer , Anja Valdenaire
发明人： Heinz FRETZ , Markus Gude , Philippe Guerry , Thierry Kimmerlin , Francois Lehembre , Thomas Pfeifer , Anja Valdenaire
IPC分类号： C07D211/66 , C07D401/14 , C07D417/12 , C07D409/12 , C07D401/12 , C07D405/12
摘要： The present invention relates to 1-[m-Carboxamido(hetero)aryl-methyl]-piperidine-4-carboxamide derivatives of formula (I) wherein X, Ar1, R1, R2, R3, R4, R5 and p are as described in the description, to their preparation, to pharmaceutically acceptable salts thereof, and to their use as pharmaceuticals, to pharmaceutical compositions containing one or more compounds of formula (I), and especially to their use as CXCR7 receptor modulators.
摘要翻译：本发明涉及式（I）的1- [间 - 甲酰氨基（杂）芳基 - 甲基] - 哌啶-4-甲酰胺衍生物，其中X，Ar1，R1，R2，R3，R4，R5和p如对其制备的描述，其药学上可接受的盐及其作为药物的用途，含有一种或多种式（I）化合物的药物组合物，特别是其作为CXCR7受体调节剂的用途。

2. 发明申请

US20080108638A1 2-Sulfanyl-Benzoimidazol-1-Yl-Acetic Acid Derivatives as Crth2 Antagonists 失效
标题翻译： 2-硫代 - 苯并咪唑-1-基乙酸衍生物作为Crth2拮抗剂
公开(公告)号：US20080108638A1
公开(公告)日：2008-05-08
申请号：US11660907
申请日：2005-08-23
申请人： Heinz Fretz , Markus Gude , Kurt Hilpert , Julien Pothier , Markus Riederer , Matthias Steger
发明人： Heinz Fretz , Markus Gude , Kurt Hilpert , Julien Pothier , Markus Riederer , Matthias Steger
IPC分类号： A61K31/4184 , A61K31/428 , A61K31/4439 , A61K31/454 , A61K31/517 , A61P37/00 , A61P9/00 , C07D235/28 , C07D401/02 , C07D403/02 , C07D417/02
CPC分类号： A61K31/4184 , A61K31/425 , A61K31/4439 , A61K31/445 , A61K31/4709 , C07D235/28 , C07D401/12 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/12 , C07D417/12
摘要： The invention relates to 2-sulfanyl-benzoimidazol-1-yl-acetic acid derivatives and their use as potent “chemoattractant receptor-homologous molecule expressed on Th2 cells” antagonists in the treatment of prostaglandin mediated diseases, to pharmaceutical compositions containing these derivatives and to processes for their preparation.
摘要翻译：本发明涉及2-硫基 - 苯并咪唑-1-基 - 乙酸衍生物及其作为治疗前列腺素介导的疾病的有效“在Th2细胞上表达的”趋化因子受体同源分子“拮抗剂的用途，含有这些衍生物的药物组合物和其准备过程。

3. 发明授权

US08273740B2 2-sulfanyl-benzoimidazol-1-yi-acetic acid derivatives as CRTH2 antagonists 失效
标题翻译： 2-硫基 - 苯并咪唑-1-基乙酸衍生物作为CRTH2拮抗剂
公开(公告)号：US08273740B2
公开(公告)日：2012-09-25
申请号：US11660907
申请日：2005-08-23
申请人： Heinz Fretz , Markus Gude , Kurt Hilpert , Julien Pothier , Markus Riederer , Matthias Steger
发明人： Heinz Fretz , Markus Gude , Kurt Hilpert , Julien Pothier , Markus Riederer , Matthias Steger
IPC分类号： A61K31/4184 , A61K31/425 , A61K31/4439 , A61K31/445 , A61K31/4709 , A61P1/00 , A61P1/04 , A61P5/00 , A61P9/00 , A61P9/10 , A61P11/00 , A61P11/06 , A61P17/00 , A61P19/02 , A61P27/02
CPC分类号： A61K31/4184 , A61K31/425 , A61K31/4439 , A61K31/445 , A61K31/4709 , C07D235/28 , C07D401/12 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/12 , C07D417/12
摘要： The invention relates to 2-sulfanyl-benzoimidazol-1-yl-acetic acid derivatives and their use as potent “chemoattractant receptor-homologous molecule expressed on Th2 cells” antagonists in the treatment of prostaglandin mediated diseases, to pharmaceutical compositions containing these derivatives and to processes for their preparation.
摘要翻译：本发明涉及2-硫基 - 苯并咪唑-1-基 - 乙酸衍生物及其作为治疗前列腺素介导的疾病的有效“在Th2细胞上表达的”趋化因子受体同源分子“拮抗剂的用途，含有这些衍生物的药物组合物和其准备过程。

4. 发明授权

US08188082B2 5,6,7,8-tetrahydro-imidazo[1,5-α]pyrazine derivatives 失效
标题翻译： 5,6,7,8-四氢 - 咪唑并[1,5-a]吡嗪衍生物
公开(公告)号：US08188082B2
公开(公告)日：2012-05-29
申请号：US12520693
申请日：2007-12-20
申请人： Hamed Aissaoui , Christoph Boss , Markus Gude , Raif Koberstein , Thierry Sifferien
发明人： Hamed Aissaoui , Christoph Boss , Markus Gude , Raif Koberstein , Thierry Sifferien
IPC分类号： A61K31/495
CPC分类号： C07D487/04
摘要： The invention relates to 5,6,7,8-tetrahydro-imidazo[1,5-a]pyrazine derivatives of formula (I), wherein X represents CH2 or O; R1 represents a phenyl group, which group is independently mono-, di-, or tri-substituted wherein the substituents are independently selected from the group consisting of (C1-4)alkyl, (C1-4)alkoxy, halogen, cyano, trifluoromethoxy and trifluoromethyl; R2 represents (C1-4)alkyl, (C1-4)alkoxy, (C2-4)alkenyl, halogen, cyano, hydroxymethyl, trifluoromethyl, C(O)NR5R6 or cyclopropyl; R3 represents (C1-4)alkyl, (C1-4)alkoxy-methyl or halogen; R4 represents (C1-4)alkyl; R5 represents hydrogen or (C1-4)alkyl; and R6 represents hydrogen or (C1-4)alkyl. The invention also relates to pharmaceutically acceptable salts of such compounds; and to the use of such compounds as medicaments; especially as orexin receptor antagonists.
摘要翻译：本发明涉及式（I）的5,6,7,8-四氢 - 咪唑并[1,5-a]吡嗪衍生物，其中X表示CH 2或O; R 1表示苯基，该基团独立地是单 - ，二 - 或三 - 取代，其中取代基独立地选自（C 1-4）烷基，（C 1-4）烷氧基，卤素，氰基，三氟甲氧基和三氟甲基; R 2表示（C 1-4）烷基，（C 1-4）烷氧基，（C 2-4）烯基，卤素，氰基，羟甲基，三氟甲基，C（O）NR 5 R 6或环丙基; R 3表示（C 1-4）烷基，（C 1-4）烷氧基 - 甲基或卤素; R 4表示（C 1-4）烷基; R5代表氢或（C1-4）烷基; 并且R 6表示氢或（C 1-4）烷基。本发明还涉及这些化合物的药学上可接受的盐; 以及使用这些化合物作为药物; 特别是作为食欲素受体拮抗剂。

5. 发明授权

US08114867B2 Oxazolidinone antibiotic derivatives 有权
标题翻译：恶唑烷酮类抗生素衍生物
公开(公告)号：US08114867B2
公开(公告)日：2012-02-14
申请号：US12595711
申请日：2008-04-10
申请人： Markus Gude , Christian Hubschwerlen , Georg Rueedi , Jean-Philippe Surivet , Cornelia Zumbrunn-Acklin
发明人： Markus Gude , Christian Hubschwerlen , Georg Rueedi , Jean-Philippe Surivet , Cornelia Zumbrunn-Acklin
IPC分类号： C07D471/04 , C07D413/14 , C07D417/14 , A61K31/4375
CPC分类号： C07D471/04 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14
摘要： The invention relates to antibacterial compounds of formula I wherein R1 is hydrogen, halogen, hydroxy, alkoxy or cyano; Y1 and Y2 each represent CH, one or two of U, V, W and X represent(s) N and the remaining each represent CH or, in the case of X, may also represent CRa, Ra being halogen, and, in the case of W, may also represent CRb, or each of U, V, W, X, Y1 and Y2 represents CH, or each of U, V, W, X and Y1 represents CH and Y2 represents N, or also one or, provided R1 is hydrogen, two of U, V, W, X, Y1 and Y2 represent(s) CRC and the remaining each represent CH, Rb being alkoxy, alkoxycarbonyl or alkoxyalkoxy and Rc being, each time it occurs, independently represents hydroxy or alkoxy; A-B-D represents a chain of 4 to 6 atoms, which 4 to 6 atoms are selected from carbon, oxygen and nitrogen and may be substituted; E is one of the following groups: in which Z is CH or N and Q is O or S, or E is a phenyl group which is substituted once or twice in the meta and/or para position(s); and to salts of such compounds.
摘要翻译：本发明涉及式I的抗菌化合物，其中R 1是氢，卤素，羟基，烷氧基或氰基; Y1和Y2各自表示CH，U，V，W和X中的一个或两个表示（s）N，其余各自表示CH，或在X的情况下也可以表示CR a，R a为卤素，并且在 W的情况也可以表示CRb，或者U，V，W，X，Y1，Y2各自表示CH，或U，V，W，X，Y1各自表示CH，Y2表示N，如果R1是氢，则U，V，W，X，Y1和Y2中的两个表示（s）CRC，其余各自表示CH，Rb是烷氧基，烷氧基羰基或烷氧基烷氧基，Rc每次发生时，独立地表示羟基或烷氧基 A-B-D表示4至6个原子的链，其中4至6个原子选自碳，氧和氮并且可以被取代; E是以下组之一：其中Z是CH或N，Q是O或S，或E是在间位和/或对位被取代一次或两次的苯基; 和这些化合物的盐。

6. 发明授权

US08003654B2 N-glycinsulfonamide derivatives and uses as orexin receptor antagonists 失效
标题翻译： N-甘氨酰磺酰胺衍生物和用作食欲肽受体拮抗剂
公开(公告)号：US08003654B2
公开(公告)日：2011-08-23
申请号：US12296842
申请日：2007-04-10
申请人： Hamed Aissaoui , Christoph Boss , Markus Gude , Ralf Koberstein , Thierry Sifferlen , Cornelia Zumbrunn Acklin
发明人： Hamed Aissaoui , Christoph Boss , Markus Gude , Ralf Koberstein , Thierry Sifferlen , Cornelia Zumbrunn Acklin
IPC分类号： A61K31/4965
CPC分类号： C07C311/29 , C07C2601/02 , C07D213/40 , C07D213/61 , C07D213/64 , C07D231/12 , C07D231/16 , C07D239/26 , C07D241/12 , C07D261/08 , C07D263/32 , C07D275/02 , C07D275/04 , C07D277/28 , C07D285/12 , C07D417/12
摘要： The invention relates to novel sulfonamide compounds of the formula (I) and their use as orexin receptor antagonists.
摘要翻译：本发明涉及式（I）的新型磺酰胺化合物及其作为食欲素受体拮抗剂的用途。

7. 发明申请

US20100222328A1 2-CYCLOPROPYL-THIAZOLE DERIVATIVES 审中-公开
标题翻译： 2-环丙基噻唑衍生物
公开(公告)号：US20100222328A1
公开(公告)日：2010-09-02
申请号：US12600160
申请日：2008-05-13
申请人： Hamed Aissaoui , Christoph Boss , Markus Gude , Ralf Koberstein , Thierry Sifferlen
发明人： Hamed Aissaoui , Christoph Boss , Markus Gude , Ralf Koberstein , Thierry Sifferlen
IPC分类号： A61K31/55 , A61K31/495 , A61K31/445 , C07D417/14 , C07D495/04
CPC分类号： C07D417/06 , C07D417/14
摘要： The invention relates to selected 2-cyclopropyl-thiazole derivatives of the formula (I) wherein B, Y and R1 are as described in the description; to salts and especially pharmaceutically acceptable salts thereof, and to the use of such compounds use as medicaments, especially as orexin receptor antagonists.
摘要翻译：本发明涉及式（I）的选择的2-环丙基 - 噻唑衍生物，其中B，Y和R 1如描述中所述; 盐，特别是其药学上可接受的盐，以及这些化合物的用途用作药物，特别是作为食欲素受体拮抗剂。

8. 发明申请

US20100204285A1 TRANS-3-AZA-BICYCLO[3.1.0]HEXANE DERIVATIVES 失效
标题翻译：衍生物-3-AZA-BICYCLO [3.1.0] HEXANE DORIVATIVES
公开(公告)号：US20100204285A1
公开(公告)日：2010-08-12
申请号：US12670809
申请日：2008-07-25
申请人： Hamed Aissaoui , Christoph Boss , Markus Gude , Ralf Koberstein , David Lehman , Thierry Sifferlen , Daniel Trachsel
发明人： Hamed Aissaoui , Christoph Boss , Markus Gude , Ralf Koberstein , David Lehman , Thierry Sifferlen , Daniel Trachsel
IPC分类号： A61K31/427 , C07D209/52 , C07D277/04 , A61K31/40 , A61P25/18
CPC分类号： C07D209/52 , C07D405/12 , C07D417/14 , C07D513/04
摘要： The invention relates to novel trans-3-aza-bicyclo[3.1.0]hexane derivatives of formula (I), wherein A, B, n and R1 are as described in the description, and to the use of such compounds, or of pharmaceutically acceptable salts of such compounds, as medicaments, especially as orexin receptor antagonists.
摘要翻译：本发明涉及式（I）的新型反式-3-氮杂 - 双环[3.1.0]己烷衍生物，其中A，B，n和R 1如说明书所述，以及这些化合物的用途，或这些化合物的药学上可接受的盐，作为药物，特别是作为食欲素受体拮抗剂。

9. 发明申请

US20100029617A1 1,4,5,6,7,8-HEXAHYDRO-1,2,5-TRIAZA-AZULENE DERIVATIVES AS OREXIN RECEPTOR ANTAGONISTS 审中-公开
标题翻译：作为OREXIN受体拮抗剂的1,4,5,6,7,8-十六氢-1,2,5-三唑衍生物
公开(公告)号：US20100029617A1
公开(公告)日：2010-02-04
申请号：US12439303
申请日：2007-08-27
申请人： Hamed Aissaoui , Christoph Boss , Markus Gude , Ralf Koberstein , Thierry Sifferlen
发明人： Hamed Aissaoui , Christoph Boss , Markus Gude , Ralf Koberstein , Thierry Sifferlen
IPC分类号： A61K31/55 , C07D487/04 , A61P25/00
CPC分类号： C07D487/04
摘要： The invention relates to 1,4,5,6,7,8-hexahydro-1,2,5-triaza-azulene derivatives and their use as orexin receptor antagonists.
摘要翻译：本发明涉及1,4,5,6,7,8-六氢-1,2,5-三氮杂薁衍生物及其作为食欲素受体拮抗剂的用途。

10. 发明授权

US09303023B2 Pyrazole and imidazole derivatives useful as orexin antagonists 有权
标题翻译：吡唑和咪唑衍生物可用作食欲素拮抗剂
公开(公告)号：US09303023B2
公开(公告)日：2016-04-05
申请号：US14000172
申请日：2012-02-17
申请人： Martin Bolli , Christoph Boss , Christine Brotschi , Markus Gude , Bibia Heidmann , Thierry Sifferlen , Jodi T. Williams
发明人： Martin Bolli , Christoph Boss , Christine Brotschi , Markus Gude , Bibia Heidmann , Thierry Sifferlen , Jodi T. Williams
IPC分类号： C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , A61K31/4155 , A61K31/4178 , A61K31/422 , A61P25/28 , A61P25/22 , A61P25/20
CPC分类号： C07D413/12 , A61K31/4155 , A61K31/4178 , A61K31/422 , C07D413/14 , C07D417/12 , C07D417/14
摘要： The present invention relates to pyrazole and imidazole derivatives of formula (I) wherein U, V, L, X, Y, R1, (R2)n and (R3)m and ring A are as described in the description, to their preparation, to pharmaceutically acceptable salts thereof, and to their use as pharmaceuticals, to pharmaceutical compositions containing one or more compounds of formula (I), and especially to their use as orexin receptor antagonists.
摘要翻译：本发明涉及式（I）的吡唑和咪唑衍生物，其中U，V，L，X，Y，R 1，（R 2）n和（R 3）m和环A如说明书所述，以及它们作为药物的用途，含有一种或多种式（I）化合物的药物组合物，特别是其作为食欲蛋白受体拮抗剂的用途。

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