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51. 发明申请

WO2008065626A2 PIPERIDINE COMPOUNDS 审中-公开
标题翻译：哌啶化合物
公开(公告)号：WO2008065626A2
公开(公告)日：2008-06-05
申请号：PCT/IB2007/054851
申请日：2007-11-29
申请人： ACTELION PHARMACEUTICALS LTD , AISSAOUI, Hamed , BOSS, Christoph , GUDE, Markus , KOBERSTEIN, Ralf , SIFFERLEN, Thierry
发明人： AISSAOUI, Hamed , BOSS, Christoph , GUDE, Markus , KOBERSTEIN, Ralf , SIFFERLEN, Thierry
IPC分类号： C07D401/12 , C07D417/14 , C07D513/04 , A61K31/4188 , A61K31/4523 , A61K31/506 , A61P25/00
CPC分类号： C07D401/12 , C07D417/14 , C07D513/04
摘要： The invention relates to piperidine compounds of formula (I) wherein X-R 1 represents -N(H)-pyrimidinyl, wherein said pyrimidinyl is unsubstituted or mono-substituted wherein the substituent is selected from (C 1-4 )alkyl or halogen, or X-R 1 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 (C 1-4 )alkyl; A represents a phenyl- or thiazolyl-group, wherein the phenyl or thiazolyl is unsubstituted or mono-substituted with (C 1-4 )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 (C 1-4 )alkyl, (C 1-4 )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XR 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 -C 6） 1-4）烷基或卤素，或XR 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 - 取代的，其中取代基独立地选自（C 1-4烷基）烷基; A表示苯基或噻唑基，其中苯基或噻唑基是未取代的或被（C 1-4烷基）单取代的烷基; 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）烷基，（C 1 -C 4） 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。

52. 发明申请

WO2008020405A2 AZETIDINE COMPOUNDS 审中-公开
标题翻译： AZETIDINE化合物
公开(公告)号：WO2008020405A2
公开(公告)日：2008-02-21
申请号：PCT/IB2007/053244
申请日：2007-08-15
申请人： ACTELION PHARMACEUTICALS LTD , AISSAOUI, Hamed , BOSS, Christoph , GUDE, Markus , KOBERSTEIN, Ralf , SIFFERLEN, Thierry
发明人： AISSAOUI, Hamed , BOSS, Christoph , GUDE, Markus , KOBERSTEIN, Ralf , SIFFERLEN, Thierry
IPC分类号： B60C1/00 , C08L19/00 , C08L21/00
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 R 1 , R 2 , 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。

53. 发明申请

WO2007122591A3 PYRAZOLO-TETRAHYDRO PYRIDINE DERIVATIVES AS OREXIN RECEPTOR ANTAGONISTS 审中-公开
标题翻译：作为OREXIN受体拮抗剂的吡唑并四氢吡啶衍生物
公开(公告)号：WO2007122591A3
公开(公告)日：2008-01-10
申请号：PCT/IB2007051522
申请日：2007-04-25
申请人： ACTELION PHARMACEUTICALS LTD , AISSAOUI HAMED , BOSS CHRISTOPH , GUDE MARKUS , KOBERSTEIN RALF , SIFFERLEN THIERRY
发明人： AISSAOUI HAMED , BOSS CHRISTOPH , GUDE MARKUS , KOBERSTEIN RALF , SIFFERLEN THIERRY
IPC分类号： C07D471/04 , A61K31/4745 , A61P25/00
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蛋白受体拮抗剂的用途。

54. 发明申请

WO2006129237A3 NOVEL PIPERIDINE CARBOXYLIC ACID AMIDE DERIVATIVES 审中-公开
标题翻译：新型哌啶羧酸酰胺衍生物
公开(公告)号：WO2006129237A3
公开(公告)日：2007-03-22
申请号：PCT/IB2006051641
申请日：2006-05-23
申请人： ACTELION PHARMACEUTICALS LTD , BEZENCON OLIVIER , BOSS CHRISTOPH , BUR DANIEL , CHEN AUSTIN CHIH-YU , CORMINBOEUF OLIVIER , DUBE DANIEL , FISCHLI WALTER , GRISOSTOMI CORINNA , REMEN LUBOS , RICHARD-BILDSTEIN SYLVIA , SIFFERLEN THIERRY , THERIEN MICHEL , WELLER THOMAS
发明人： BEZENCON OLIVIER , BOSS CHRISTOPH , BUR DANIEL , CHEN AUSTIN CHIH-YU , CORMINBOEUF OLIVIER , DUBE DANIEL , FISCHLI WALTER , GRISOSTOMI CORINNA , REMEN LUBOS , RICHARD-BILDSTEIN SYLVIA , SIFFERLEN THIERRY , THERIEN MICHEL , WELLER THOMAS
IPC分类号： C07D211/78 , A61K31/451 , A61P9/00 , C07D401/10 , C07D401/12 , C07D471/08
CPC分类号： C07D471/08 , C07D211/78 , C07D401/10 , C07D401/12
摘要： The invention relates to novel piperidine carboxylic acid amide derivatives and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of these novel compounds, pharmaceutical compositions comprising such compounds and especially the use of such compounds as inhibitors of renin.
摘要翻译：本发明涉及新型的哌啶羧酸酰胺衍生物及其在制备药物组合物中作为活性成分的用途。本发明还涉及包括制备这些新化合物的方法，包含这些化合物的药物组合物，特别是使用这些化合物作为肾素抑制剂的相关方面。

55. 发明申请

WO2006129237A2 NOVEL PIPERIDINE CARBOXYLIC ACID AMIDE DERIVATIVES 审中-公开
标题翻译：新型哌啶羧酸酰胺衍生物
公开(公告)号：WO2006129237A2
公开(公告)日：2006-12-07
申请号：PCT/IB2006/051641
申请日：2006-05-23
申请人： ACTELION PHARMACEUTICALS LTD , BEZENCON, Olivier , BOSS, Christoph , BUR, Daniel , CHEN, Austin, Chih-Yu , CORMINBOEUF, Olivier , DUBE, Daniel , FISCHLI, Walter , GRISOSTOMI, Corinna , REMEN, Lubos , RICHARD-BILDSTEIN, Sylvia , SIFFERLEN, Thierry , THERIEN, Michel , WELLER, Thomas
发明人： BEZENCON, Olivier , BOSS, Christoph , BUR, Daniel , CHEN, Austin, Chih-Yu , CORMINBOEUF, Olivier , DUBE, Daniel , FISCHLI, Walter , GRISOSTOMI, Corinna , REMEN, Lubos , RICHARD-BILDSTEIN, Sylvia , SIFFERLEN, Thierry , THERIEN, Michel , WELLER, Thomas
IPC分类号： H04N5/76
CPC分类号： C07D471/08 , C07D211/78 , C07D401/10 , C07D401/12
摘要： The invention relates to novel piperidine carboxylic acid amide derivatives and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of these novel compounds, pharmaceutical compositions comprising such compounds and especially the use of such compounds as inhibitors of renin.
摘要翻译：本发明涉及新型的哌啶羧酸酰胺衍生物及其在制备药物组合物中作为活性成分的用途。本发明还涉及包括制备这些新化合物的方法，包含这些化合物的药物组合物，特别是使用这些化合物作为肾素抑制剂的相关方面。

56. 发明申请

WO2006021401A3 BICYLONONENE DERIVATIVES 审中-公开
标题翻译：二氯苯衍生物
公开(公告)号：WO2006021401A3
公开(公告)日：2006-04-13
申请号：PCT/EP2005009048
申请日：2005-08-22
申请人： ACTELION PHARMACEUTICALS LTD , BEZENCON OLIVIER , BOSS CHRISTOPH , BUR DANIEL , CORMINBOEUF OLIVIER , FISCHLI WALTER , GRISOSTOMI CORINNA , REMEN LUBOS , RICHARD SYLVIA , SIFFERLEN THIERRY , WELLER THOMAS
发明人： BEZENCON OLIVIER , BOSS CHRISTOPH , BUR DANIEL , CORMINBOEUF OLIVIER , FISCHLI WALTER , GRISOSTOMI CORINNA , REMEN LUBOS , RICHARD SYLVIA , SIFFERLEN THIERRY , WELLER THOMAS
IPC分类号： C07D471/08 , A61K31/4995
CPC分类号： C07D471/08
摘要： The invention relates to bicyclononene derivatives and the use thereof as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and especially their use as inhibitors of renin.
摘要翻译：本发明涉及双环壬烯衍生物及其在制备药物组合物中作为活性成分的用途。本发明还涉及包括制备化合物的方法，含有一种或多种这些化合物的药物组合物，特别是其作为肾素抑制剂的用途的相关方面。

57. 发明申请

WO2005054244A2 DIAZABICYCLONONENE AND TETRAHYDROPYRIDINE DERIVATIVES WITH A NEW SIDE-CHAIN 审中-公开
标题翻译：具有新侧链的二氮杂萘酮和四氢吡啶衍生物
公开(公告)号：WO2005054244A2
公开(公告)日：2005-06-16
申请号：PCT/EP2004/013579
申请日：2004-11-30
申请人： ACTELION PHARMACEUTICALS LTD , BEZENCON, Olivier , SIFFERLEN, Thierry , BUR, Daniel , FISCHLI, Walter , WELLER, Thomas , REMEN, Lubos , RICHARD-BILDSTEIN, Sylvia
发明人： BEZENCON, Olivier , SIFFERLEN, Thierry , BUR, Daniel , FISCHLI, Walter , WELLER, Thomas , REMEN, Lubos , RICHARD-BILDSTEIN, Sylvia
IPC分类号： C07D471/08
CPC分类号： C07D451/02 , C07D451/06
摘要： The invention relates to novel bicyclic derivatives, and related compounds and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and especially their use as inhibitors of renin.
摘要翻译：本发明涉及新型双环衍生物及其相关化合物及其在制备药物组合物中作为活性成分的用途。本发明还涉及包括制备化合物的方法，含有一种或多种这些化合物的药物组合物，特别是其作为肾素抑制剂的用途的相关方面。

58. 发明申请

WO2004096780A1 QUINOXALINONE-3- ONE DERIVATIVES AS OREXIN RECEPTOR ANTAGONISTS 审中-公开
标题翻译：喹喔啉酮-3-一种衍生物作为OREXIN受体拮抗剂
公开(公告)号：WO2004096780A1
公开(公告)日：2004-11-11
申请号：PCT/EP2004/004374
申请日：2004-04-26
申请人： ACTELION PHARMACEUTICALS LTD , FISCHLI, Walter , AISSAOUI, Hamed , CLOZEL, Martine , WELLER, Thomas , KOBERSTEIN, Ralf , SIFFERLEN, Thierry
发明人： AISSAOUI, Hamed , CLOZEL, Martine , WELLER, Thomas , KOBERSTEIN, Ralf , SIFFERLEN, Thierry
IPC分类号： C07D241/44
CPC分类号： C07D401/12 , C07D241/44
摘要： The invention relates to quinoxalinone derivatives of general Formula (I) and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and especially their use as orexin receptor antagonists.General Formula (I) wherein X and R 1 -R 9 are as defined in the description
摘要翻译：本发明涉及通式（I）的喹喔啉酮衍生物及其在制备药物组合物中作为活性成分的用途。本发明还涉及包括制备化合物的方法，含有一种或多种这些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的相关方面。通式（I）其中X和R 1 -R 9 如说明书中所定义

59. 发明申请

WO2013050938A1 3,7-DIAZABICYCLO[3.3.1]NONANE AND 9-OXA-3,7-DIAZABICYCLO[3.3.1]NONANE DERIVATIVES 审中-公开
标题翻译： 3,7-二氮杂环[3.3.1]壬和9-OXA-3,7-二氮杂双环[3.3.1] NONANE衍生物
公开(公告)号：WO2013050938A1
公开(公告)日：2013-04-11
申请号：PCT/IB2012/055292
申请日：2012-10-03
申请人： ACTELION PHARMACEUTICALS LTD , BOSS, Christoph , BROTSCHI, Christine , HEIDMANN, Bibia , SIFFERLEN, Thierry , WILLIAMS, Jodi, T.
发明人： BOSS, Christoph , BROTSCHI, Christine , HEIDMANN, Bibia , SIFFERLEN, Thierry , WILLIAMS, Jodi, T.
IPC分类号： C07D471/08 , C07D498/08 , A61K31/439 , A61K31/5386
CPC分类号： C07D471/08 , C07D498/08
摘要： The present invention relates to 3,7-diazabicyclo[3.3.1]nonane and 9-oxa-3,7- diazabicyclo[3.3.1 ]nonane derivatives of formula (I) wherein Ar 1 and Ar 2 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3,7-二氮杂双环[3.3.1]壬烷和9-氧杂-3,7-二氮杂双环[3.3.1]壬烷衍生物，其中Ar1和Ar2如说明书所述，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的药物组合物，其药学上可接受的盐及其作为药物的用途。

60. 发明申请

WO2012085857A1 3,8-DIAZA-BICYCLO[4.2.0]OCT-3-YL AMIDES 审中-公开
标题翻译： 3,8-DIAZA-BICYCLO [4.2.0] OCT-3-YL AMIDES
公开(公告)号：WO2012085857A1
公开(公告)日：2012-06-28
申请号：PCT/IB2011/055846
申请日：2011-12-21
申请人： ACTELION PHARMACEUTICALS LTD , BOSS, Christoph , BROTSCHI, Christine , HEIDMANN, Bibia , SIFFERLEN, Thierry , WILLIAMS, Jodi T.
发明人： BOSS, Christoph , BROTSCHI, Christine , HEIDMANN, Bibia , SIFFERLEN, Thierry , WILLIAMS, Jodi T.
IPC分类号： C07D471/04 , A61K31/4353 , A61P25/00
CPC分类号： C07D471/04
摘要： The present invention relates to 3,8-diaza-bicyclo[4.2.0]oct-3-yl amide derivatives of formula (I), wherein the relative configuration of the diazabicyclooctane moiety is cis; and wherein Ar 1 , and Ar 2 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3,8-二氮杂双环[4.2.0]辛-3-基酰胺衍生物，其中二氮杂双环辛烷部分的相对构型是顺式的; 并且其中Ar1和Ar2如本说明书所述，其制备方法，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，特别是其作为食欲肽受体拮抗剂。

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