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11. 发明申请

US20120088759A1 THIAZOLIDIN-4-ONE AND [1,3]-THIAZINAN-4-ONE COMPOUNDS AS OREXIN RECEPTOR ANTAGONISTS 审中-公开
标题翻译：噻吗啉-4-酮和[1,3] - 噻嗪-4-酮化合物作为OREXIN受体拮抗剂
公开(公告)号：US20120088759A1
公开(公告)日：2012-04-12
申请号：US13319774
申请日：2010-05-11
申请人： Hamed Aissaoui , Christoph Boss , Christine Brotschi , Markus Gude , John Gatfield , Romain Siegrist , Thierry Sifferlen , Jodi T. Williams
发明人： Hamed Aissaoui , Christoph Boss , Christine Brotschi , Markus Gude , John Gatfield , Romain Siegrist , Thierry Sifferlen , Jodi T. Williams
IPC分类号： A61K31/54 , C07D277/34 , C07D417/12 , A61K31/506 , A61K31/4439 , A61K31/426 , A61K31/498 , A61P25/22 , A61P25/00 , C07D417/10 , C07D417/04 , C07D279/06 , A61K31/501 , A61K31/427 , A61K31/4709 , A61K31/541 , A61P25/20 , A61P25/18 , C07D277/14
CPC分类号： C07D277/14 , C07D417/04
摘要： The present invention relates to thiazolidin-4-one and [1,3]-thiazinan-4-one compounds of formula (I) wherein X, Y, R3 and R4 are as described in the description, or pharmaceutically acceptable salts thereof, for the prevention or treatment of diseases related to the orexin system. The present invention also relates to novel thiazolidin-4-one compounds of formula (II) and their use as pharmaceuticals, pharmaceutical compositions containing one or more compounds of formula (II), and especially their use as orexin receptor antagonists.
摘要翻译：本发明涉及式（I）的噻唑烷-4-酮和[1,3]噻嗪-4-酮化合物，其中X，Y，R 3和R 4如说明书中所述或其药学上可接受的盐，用于预防或治疗与食欲素系统有关的疾病。本发明还涉及式（II）的新型噻唑烷-4-酮化合物及其作为药物的用途，含有一种或多种式（II）化合物的药物组合物，特别是其作为食欲素受体拮抗剂的用途。

12. 发明授权

US08133901B2 3-heteroaryl (amino or amido)-1-(biphenyl or phenylthiazolyl) carbonylpiperidine derivatives as orexin receptor inhibitors 失效
标题翻译：（氨基或酰氨基）-1-（联苯基或苯基噻唑基）羰基哌啶衍生物作为食欲素受体抑制剂
公开(公告)号：US08133901B2
公开(公告)日：2012-03-13
申请号：US12517010
申请日：2007-11-29
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： C07D401/12 , C07D417/14 , C07D513/04 , A61K31/506
CPC分类号： C07D401/12 , C07D417/14 , C07D513/04
摘要： The invention relates to piperidine compounds of formula (I): wherein X—R1 represents —N(H)-pyrimidinyl, wherein said pyrimidinyl is unsubstituted or mono-substituted wherein the substituent is selected from (C1-4)alkyl or halogen, or X—R1 represents —NH—C(O)-heterocyclyl, wherein the heterocyclyl is selected from benzofuranyl and imidazo[2,1-b]-thiazolyl, wherein said heterocyclyl is unsubstituted or independently mono-, di- or tri-substituted wherein the substituents are independently selected from (C1-4)alkyl; A represents a phenyl- or thiazolyl-group, wherein the phenyl or thiazolyl is unsubstituted or mono-substituted with (C1-4)alkyl; B represents a phenyl-group, wherein the phenyl is unsubstituted or mono-, or di- substituted, wherein the substituents are independently selected from the group consisting of (C1-4)alkyl, (C1-4)alkoxy, trifluoromethyl, cyano and halogen; to 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）的哌啶化合物：其中X-R 1表示-N（H） - 嘧啶基，其中所述嘧啶基是未取代的或单取代的，其中取代基选自（C 1-4）烷基或卤素，或 X-R1表示-NH-C（O） - 杂环基，其中杂环基选自苯并呋喃基和咪唑并[2,1-b] - 噻唑基，其中所述杂环基是未取代的或独立的单 - ，二 - 或三 - 取代，其中取代基独立地选自（C 1-4）烷基; A表示苯基或噻唑基，其中苯基或噻唑基未被取代或被（C 1-4）烷基单取代; B表示苯基，其中苯基是未取代的或单取代或二取代的，其中取代基独立地选自（C 1-4）烷基，（C 1-4）烷氧基，三氟甲基，氰基和卤素; 和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。

13. 发明申请

US20110263662A1 1,2-DIAMIDO-ETHYLENE DERIVATIVES AS OREXIN ANTAGONISTS 审中-公开
标题翻译： 1,2-二氨基乙烯衍生物作为OREXIN ANTAGONISTS
公开(公告)号：US20110263662A1
公开(公告)日：2011-10-27
申请号：US12673382
申请日：2008-08-14
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： A61K31/427 , A61K31/416 , A61K31/357 , A61K31/343 , C07D513/04 , C07D417/12 , C07D231/56 , C07D319/20 , C07D307/84 , A61P25/20 , A61P25/00 , A61P25/30 , A61P25/18 , A61P25/28 , A61P3/00 , A61K31/429
CPC分类号： C07D209/48 , C07D231/56 , C07D307/79 , C07D319/18 , C07D417/12 , C07D513/04
摘要： The invention relates to 1,2-diamido-ethylene derivatives of the formula (I) wherein R1, R2, R3, and A are as described in the description and their use as medicaments, especially as orexin receptor antagonists.
摘要翻译：本发明涉及式（I）的1,2-二氨基乙烯衍生物，其中R 1，R 2，R 3和A如描述中所述及其作为药物，特别是作为食欲素受体拮抗剂的用途。

14. 发明申请

US20110124636A1 2-AZA-BICYCLO[3.1.0]HEXANE DERIVATIVES AS OREXIN RECEPTOR ANTAGONISTS 失效
标题翻译： 2-AZA-BICYCLO [3.1.0] HEXANE衍生物作为OREXIN受体拮抗剂
公开(公告)号：US20110124636A1
公开(公告)日：2011-05-26
申请号：US12521453
申请日：2007-12-28
申请人： Hamed Aissaoui , Christoph Boss , Markus Gude , Ralf Koberstein , Thierry Sifferlen , Daniel Trachsel
发明人： Hamed Aissaoui , Christoph Boss , Markus Gude , Ralf Koberstein , Thierry Sifferlen , Daniel Trachsel
IPC分类号： A61K31/427 , C07D417/14 , C07D405/12 , C07D405/14 , C07D513/04 , C07D417/06 , C07D495/04 , C07D471/04 , A61K31/403 , A61K31/506 , A61K31/429 , A61K31/4725 , A61K31/4709 , A61K31/433 , A61K31/538 , A61K31/428 , A61K31/437 , A61P25/24 , A61P25/00 , A61P25/18 , A61P25/30 , A61P15/00 , A61P5/00 , A61P25/20 , A61P25/28 , A61P21/00 , A61P25/14 , A61P25/16 , A61P27/16 , A61P25/08 , A61P25/04 , A61P1/00 , A61P3/00 , A61P3/10 , A61P3/08 , A61P35/00 , A61P17/00 , A61P13/00 , A61P37/08 , A61P11/06 , A61P9/00 , A61P11/00 , A61P9/12 , A61P9/04 , A61P3/06 , A61P9/10 , A61P13/12
CPC分类号： C07D513/04 , C07D405/12 , C07D405/14 , C07D417/14
摘要： The invention relates to novel 2-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）的新的2-氮杂 - 双环[3.1.0]己烷衍生物，其中A，B，n和R 1如描述中所述，以及这些化合物或其药学上可接受的盐的用途的这些化合物，作为药物，特别是作为食欲素受体拮抗剂。

15. 发明申请

US20100069418A1 3-HETEROARYL (AMINO OR AMIDO)-1-(BIPHENYL OR PHENYLTHIAZOLYL) CARBONYLPIPERIDINE DERIVATIVES AS OREXIN RECEPTOR INHIBITORS 失效
标题翻译：作为OREXIN受体抑制剂的3-异丙基（氨基或氨基）-1-（联苯胺或苯基乙酰基）碳二苯胺衍生物
公开(公告)号：US20100069418A1
公开(公告)日：2010-03-18
申请号：US12517010
申请日：2007-11-29
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： A61K31/506 , C07D239/28 , C07D417/04 , A61K31/445 , A61P25/30 , A61P25/32
CPC分类号： C07D401/12 , C07D417/14 , C07D513/04
摘要： The invention relates to piperidine compounds of formula (I) wherein X-R1 represents —N(H)-pyrimidinyl, wherein said pyrimidinyl is unsubstituted or mono-substituted wherein the substituent is selected from (C1-4)alkyl or halogen, or X-R1 represents —NH—C(O)-heterocyclyl, wherein the heterocyclyl is selected from benzofuranyl and imidazo[2,1-b]-thiazolyl, wherein said heterocyclyl is unsubstituted or independently mono-, di-, or tri-substituted wherein the substituents are independently selected from (C1-4)alkyl; A represents a phenyl- or thiazolyl-group, wherein the phenyl or thiazolyl is unsubstituted or mono-substituted with (C1-4)alkyl; B represents a phenyl-group, wherein the phenyl is unsubstituted or mono-, or di-substituted, wherein the substituents are independently selected from the group consisting of (C1-4)alkyl, (C1-4)alkoxy, trifluoromethyl, cyano and halogen; to 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）的哌啶化合物，其中X-R 1表示-N（H） - 嘧啶基，其中所述嘧啶基是未取代的或单取代的，其中取代基选自（C 1-4）烷基或卤素，或X -R 1表示-NH-C（O） - 杂环基，其中杂环基选自苯并呋喃基和咪唑并[2,1-b] - 噻唑基，其中所述杂环基是未取代的或独立的单 - ，二 - 或三 - 取代，其中取代基独立地选自（C 1-4）烷基; A表示苯基或噻唑基，其中苯基或噻唑基未被取代或被（C 1-4）烷基单取代; B表示苯基，其中苯基是未取代的或单取代或二取代的，其中取代基独立地选自（C 1-4）烷基，（C 1-4）烷氧基，三氟甲基，氰基和卤素; 和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。

16. 发明授权

US07994336B2 Azetidine compounds as orexin receptor antagonists 失效
标题翻译：氮杂环丁烷化合物作为食欲素受体拮抗剂
公开(公告)号：US07994336B2
公开(公告)日：2011-08-09
申请号：US12377349
申请日：2007-08-15
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： C07D513/04 , C07D277/00 , C07D205/00 , A61K31/427 , A61K31/431 , A61K31/337
CPC分类号： C07D405/12 , C07D417/06 , C07D417/14 , C07D513/04 , C08L19/006 , C08L21/00 , C08L83/10 , C08L2666/08 , C08L2666/04
摘要： The invention relates to novel azetidine compounds of formula (I), wherein R1, R2, and X are as described in the description and their use as orexin receptor antagonists.
摘要翻译：本发明涉及式（I）的新型氮杂环丁烷化合物，其中R 1，R 2和X如说明书中所述及其作为食欲素受体拮抗剂的用途。

17. 发明申请

US20110039857A1 PIPERIDINE AND PYROOLIDINE COMPOUNDS 审中-公开
标题翻译：哌啶和吡咯烷酮化合物
公开(公告)号：US20110039857A1
公开(公告)日：2011-02-17
申请号：US12990020
申请日：2009-04-29
申请人： Hamed Aissaoui , Christoph Boss , Ralf Koberstein , Thierry Sifferlen , Daniel Trachsel
发明人： Hamed Aissaoui , Christoph Boss , Ralf Koberstein , Thierry Sifferlen , Daniel Trachsel
IPC分类号： A61K31/506 , C07D401/12 , A61K31/498 , C07D417/12 , A61K31/454 , C07D417/14 , C07D495/04 , A61K31/4535 , C07D471/04 , A61K31/437 , A61K31/4725 , A61K31/4709 , A61P25/00 , A61P25/30
CPC分类号： C07D211/56 , C07D401/12 , C07D417/06 , C07D417/14 , C07D471/04 , C07D493/04
摘要： The invention relates to piperidine and pyrrolidine compounds of formula (I) wherein A, B, n and X are as described in the description; to 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）的哌啶和吡咯烷化合物，其中A，B，n和X如说明书所述; 和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。

18. 发明授权

US07834028B2 Pyrazolo-tetrahydro pyridine derivatives as orexin receptor antagonists 失效
标题翻译：吡唑并 - 四氢吡啶衍生物作为食欲素受体拮抗剂
公开(公告)号：US07834028B2
公开(公告)日：2010-11-16
申请号：US12298369
申请日：2007-04-25
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： A61K31/44 , C07D471/02
CPC分类号： C07D471/04
摘要： The invention relates to novel pyrazolo-tetrahydropyridines compounds and their use as orexin receptor antagonists.
摘要翻译：本发明涉及新型吡唑并四氢吡啶类化合物及其作为食欲素受体拮抗剂的用途。

19. 发明申请

US20100197733A1 PYRROLIDINES AND PIPERIDINES AS OREXIN RECEPTOR ANTAGONISTS 失效
标题翻译：吡咯啉和哌啶作为OREXIN受体拮抗剂
公开(公告)号：US20100197733A1
公开(公告)日：2010-08-05
申请号：US12679535
申请日：2008-09-23
申请人： Hamed Aissaoui , Christoph Boss , Ralf Koberstein , Thierry Sifferlen
发明人： Hamed Aissaoui , Christoph Boss , Ralf Koberstein , Thierry Sifferlen
IPC分类号： A61K31/454 , C07D401/14 , C07D417/14 , A61K31/4439 , A61P25/30 , A61P25/24
CPC分类号： C07D513/04 , C07D417/14
摘要： The invention relates to compounds of formula (I) wherein Y, A, N and R1 are as described in the description, to salts, especially 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）化合物，其中Y，A，N和R 1如说明书中所述，这些化合物的盐，特别是药学上可接受的盐，以及这些化合物作为药物，特别是食欲素受体拮抗剂

20. 发明申请

US20100093740A1 5,6,7,8-TETRAHYDRO-IMIDAZO[1,5-A]PYRAZINE DERIVATIVES 失效
标题翻译： 5,6,7,8-四氢-1H-咪唑并〔1,5-A〕吡嗪衍生物
公开(公告)号：US20100093740A1
公开(公告)日：2010-04-15
申请号：US12520693
申请日：2007-12-20
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： A61K31/4985 , C07D487/02 , A61P25/18 , A61P25/24 , A61P25/22 , A61P25/00 , A61P25/30 , A61P25/20 , A61P29/00 , A61P11/06 , A61P9/00 , A61P13/12
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。

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