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11. 发明专利

NO20063255L 未知
公开(公告)号：NO20063255L
公开(公告)日：2006-09-14
申请号：NO20063255
申请日：2006-07-13
申请人： INCYTE CORP
发明人： XUE CHU-BIAO , METCALF BRIAN , ROBINSON DARIUS J , HAN AMY QI , ZHENG CHANGSHENG , WANG ANLAI , ZHANG YINGXIN
IPC分类号： C07D401/12 , A61K31/40 , A61K31/4025 , A61K31/427 , A61K31/44 , A61K31/4439 , A61K31/506 , C07D207/14 , C07D401/14 , C07D413/14 , C07D417/02
摘要： (wherein R1, R2, R3, R4, R5, R6, R7, X, Y and Z are as defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of chemokine receptors and more specifically as modulators of the CCR2 and/or CCR5 receptor. The compounds and compositions of the invention may bind to chemokine receptors, e.g., the CCR2 and/or CCR5 chemokine receptors, and are useful for treating diseases associated with chemokine, e.g., CCR2 and/or CCR5, activity, such as atherosclerosis, restenosis, lupus, organ transplant rejection and rheumatoid arthritis.

12. 发明专利

IS8466A 3-Sýklóalkýlamínópýrrólidín afleiður sem stillar á flakkboða viðtaka 未知
公开(公告)号：IS8466A
公开(公告)日：2006-05-15
申请号：IS8466
申请日：2006-05-15
申请人： INCYTE CORP
发明人： XUE CHU-BIAO , METCALF BRIAN , HAN AMY QI , ROBINSON DARIUS J , ZHENG CHANGSHENG , WANG ANLAI , ZHANG YINGXIN
IPC分类号： A61K31/4025 , A61K31/427 , A61K31/44 , A61K31/4439 , A61K31/506 , C07D401/12 , C07D401/14 , C07D417/02

13. 发明专利

AU2003293129A1 3-AMINOPYRROLIDINE DERIVATIVES AS MODULATORS OF CHEMOKINE RECEPTORS 未知
公开(公告)号：AU2003293129A1
公开(公告)日：2004-06-23
申请号：AU2003293129
申请日：2003-11-26
申请人： INCYTE CORP
发明人： ROBINSON DARIUS J , HAN AMY QI , XUE CHU-BIAO , METCALF BRIAN , FENG HAO , CAO GANFENG , HUANG TAISHING , ZHENG CHANGSHENG
IPC分类号： C07D207/14 , C07D401/08 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/08 , C07D403/10 , C07D405/04 , C07D405/08 , C07D405/10 , C07D405/14 , C07D409/08 , C07D413/10 , C07D413/14 , C07D417/08 , C07D417/10 , C07D417/14 , C07D495/10
摘要： The present invention relates to 3-aminopyrrolidine derivatives of the formula I: (wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , X, Y and X are as defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of chemokine receptors and more specifically as a modulator of the CCR2 and/or CCR5 receptor. The compounds and compositions of the invention may bind to chemokine receptors, e.g., the CCR2 and/or CCR5 chemokine receptors, and are useful for treating diseases associated with chemokine, e.g., CCR2 and/or CCR5, activity, such as atherosclerosis, restenosis, lupus, organ transplant rejection and rheumatoid arthritis.

14. 发明专利

GEP20115290B 3-AMINOPYRROLIDINE DERIVATIVES AS MODULATORS OF CHEMOKINE RECEPTORS 未知
公开(公告)号：GEP20115290B
公开(公告)日：2011-09-26
申请号：GEAP2003008862
申请日：2003-11-26
申请人： INCYTE CORP
发明人： XUE CHU-BIAO , METCALF BRIAN , FENG HAO , CAO GANFENG , HUANG TAISHING , ZHENG CHANGSHENG , ROBINSON DARIUS J , HAN AMY QI
IPC分类号： C07D207/14 , A61K31/40 , A61P13/12 , A61P25/02 , C07D401/08 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/08 , C07D403/10 , C07D405/04 , C07D405/08 , C07D405/10 , C07D405/14 , C07D409/08 , C07D413/10 , C07D413/14 , C07D417/08 , C07D417/10 , C07D417/14 , C07D495/10
摘要： A compound of the formula: III wherein R1, R2, R3, R4, R5, R6, R7, R8, and m are provided in the specification, pharmaceutical compositions on their base and use of their therapeutically effective amount in patients for treatment of the diseases associated with chemokine receptor activity, in particular of multiple sclerosis and nephritis.

15. 发明专利

NZ540290A 3-aminopyrrolidine derivatives as modulators of chemokine receptors 未知
公开(公告)号：NZ540290A
公开(公告)日：2007-09-28
申请号：NZ54029003
申请日：2003-11-26
申请人： INCYTE CORP
发明人： XUE CHU-BIAO , METCALF BRIAN , FENG HAO , CAO GANFENG , HUANG TAISHING , ZHENG CHANGSHENG , ROBINSON DARIUS J , HAN AMY QI
IPC分类号： C07D207/14 , C07D401/08 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/08 , C07D403/10 , C07D405/04 , C07D405/08 , C07D405/10 , C07D405/14 , C07D409/08 , C07D413/10 , C07D413/14 , C07D417/08 , C07D417/10 , C07D417/14 , C07D495/10
摘要： Disclosed are 3-aminopyrrolidine derivatives of the formula (I) that are useful as modulators of chemokine receptor activity, wherein the variables R1, R2, R3, R4, R5, R6, R7, R8, X, Y and Z are as defined in the specification. In particular, these compounds are useful as modulators of chemokine receptors and more specifically as a modulator of the CCR2 and/or CCR5 receptor. The compounds and compositions of the invention may bind to chemokine receptors, e.g., the CCR2 and/or CCR5 chemokine receptors, and are useful for treating diseases associated with chemokine, e.g., CCR2 and/or CCR5, activity, such as atherosclerosis, restenosis, lupus, organ transplant rejection and rheumatoid arthritis.

16. 发明专利

OA13338A 3-cycloalkylaminopyrrolidine derivates as modulators of chemokine receptors. 未知
公开(公告)号：OA13338A
公开(公告)日：2007-04-13
申请号：OA1200600195
申请日：2004-12-16
申请人： INCYTE CORP
发明人： HAN AMY QI , METCALF BRIAN , ROBINSON DARIUS J , WANG ANLAI , XUE CHU-BIAO , ZHANG YINGXIN , ZHENG CHANSHENG
IPC分类号： A61K31/4025 , A61K31/427 , A61K31/44 , A61K31/4439 , A61K31/506 , C07D401/00 , C07D401/12 , C07D401/14 , C07D417/02
摘要： (wherein R1, R2, R3, R4, R5, R6, R7, X, Y and Z are as defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of chemokine receptors and more specifically as modulators of the CCR2 and/or CCR5 receptor. The compounds and compositions of the invention may bind to chemokine receptors, e.g., the CCR2 and/or CCR5 chemokine receptors, and are useful for treating diseases associated with chemokine, e.g., CCR2 and/or CCR5, activity, such as atherosclerosis, restenosis, lupus, organ transplant rejection and rheumatoid arthritis.

17. 发明专利

MA28391B1 Dérivés de 3-cycloalkylaminopyrrolidine utiles comme modulateurs de récepteurs de chimiokines 未知
公开(公告)号：MA28391B1
公开(公告)日：2007-01-02
申请号：MA29111
申请日：2006-06-16
申请人： INCYTE CORP
发明人： XUE CHU-BIAO , METCALF BRIAN , HAN AMY QI , ROBINSON DARIUS J , ZHENG CHANGSHENG , WANG ANLAI , ZHANG YINGXIN
IPC分类号： A61K31/4025 , A61K31/427 , A61K31/44 , A61K31/4439 , A61K31/506 , C07D401/12 , C07D401/14 , C07D417/02

19. 发明专利

ES2439894T3 Derivados de 3-cicloalquilaminopirrolidina como moduladores de receptores de quimioquina 未知
公开(公告)号：ES2439894T3
公开(公告)日：2014-01-27
申请号：ES04814497
申请日：2004-12-16
申请人： INCYTE CORP
发明人： XUE CHU-BIAO , METCALF BRIAN , HAN AMY QI , ROBINSON DARIUS J , ZHENG CHANGSHENG , WANG ANLAI , ZHANG YINGXIN
IPC分类号： C07D207/14 , A61K31/4025 , A61K31/427 , A61K31/44 , A61K31/4439 , A61K31/506 , C07D401/12 , C07D401/14 , C07D403/12 , C07D413/12 , C07D413/14 , C07D417/02 , C07D417/12 , C07D417/14
摘要： Un compuesto seleccionado del grupo consistente en: N-(2-{(3S)-3-[(4-Hidroxi-4-fenilciclohexil)amino]pirrolidin-1-il}-2-oxoetil)-3-(trifluorometil)benzamida, N-(2-{(3S)-3-[(4-Hidroxi-4-piridin-3-ilciclohexil)amino]pirrolidin-1-il}-2-oxoetil)-3-(trifluorometil)benzamida, N-(2-{(3S)-3-[(4-Hidroxi-4-piridin-3-ilciclohexil)(metil)amino]pirrolidin-1-il}-2-oxoetil)-3-(trifluorometil)benzamida, N-(2-{(3S)-3-[(4-Hidroxi-4-[5-(metoximetil)piridin-2-il]ilciclohexil}amino]pirrolidin-1-il]-2-oxoetil}-3-(trifluorometil)benzamida, N-(2-((3S)-3-[(4-{5-[(Dimetilamino)metil]piridin-2-il}4-hidroxiciclohexil)-amino]pirrolidin-1-il}-2-oxoetil}-3-(trifluorometil)benzamida, N-(2-{3S)-3-{[(4-Hidroxi-4-[4-(metilfenil)ciclohexil]amino}pirrolidin-1-il]-2-oxoetil]-3-(trifluorometil)benzamida, N-(2-{3S)-3-[(4-hidroxi-4-piridin-3-ilciclohexil)amino]pirrolidin-1-il}-2-oxoetil]-3-(trifluorometil)benzamida, N-(2-{3S)-3-[(4-hidroxi-4-piridin-4-ilciclohexil)amino]pirrolidin-1-il}-2-oxoetil]-3-(trifluorometil)benzamida, N-[2-((3S)-3-{[(4-Hidroxi-4-[5-metilpiridin-2-il)ciclohexil]amino}pirrolidin-1-il]-2-oxoetil]-3-(trifluorometil)benzamida, N-[(2-((3S)-3-{[(4-Hidroxi-4-[4-metilpiridin-2-il)ciclohexil]amino}pirrolidin-1-il]-2-oxoetil]-3-(trifluorometil)benzamida, N-[2-((3S)-3-{[(4-Hidroxi-4-[6-metilpiridin-2-il)ciclohexil]amino}pirrolidin-1-il]-2-oxoetil]-3-(trifluorometil)benzamida, N-[2-((3S)-3-{[(4-Hidroxi-4-[6-metoxipiridin-2-il)ciclohexil]amino}pirrolidin-1-il]-2-oxoetil]-3-(trifluorometil)benzamida, N-[2-((3S)-3-{[(4-Hidroxi-4-[6-metoxipiridin-3-il)ciclohexil]amino}pirrolidin-1-il]-2-oxoetil]-3-(trifluorometil)benzamida, 3-(Trifluorometil)-N-[2-((3S)-3-{[(4-hidroxi-4-(5-metil-1,3-tiazol-2-il)ciclohexil]amino}pirrolidin-1-il]-2-oxoetil]-benzamida, 3-(Trifluorometil)-N-[2-((3S)-3-{[(4-hidroxi-4-(5-(1-hidroxi-1-mtetiletil)-1,3-tiazol-2-il]ciclohexil}amino)pirrolidin-1-il]-2-oxoetil]-benzamida, 3-(Trifluorometil)-N-[2-((3S)-3-{[(4-hidroxi-4-(5-(metoximetil)-1,3-tiazol-2-il]ciclohexil}amino)pirrolidin-1-il]-2-oxoetil]-benzamida, 2-(1-Hidroxi-4-{[(3S)-1-({[3-(trifluorometil)benzoil]amino}acetil)pirrolidin-3-il]amino}ciclohexil)-N-metil-1,3-tiazol-5-carboxamida, N-Etil-2-(1-hidroxi-4-{[(3S)-1-({[3-(trifluorometil)benzoil]amino}acetil)pirrolidin-3-il]amino}ciclohexil)-1,3-tiazol-5-carboxamida, N-{2-[(3S)-3-[{4-Hidroxi-4-[5-(pirrolidin-1-ilcarbonil)-1,3-tiazol-2-il]ciclohexil}amino)pirrolidin-1-il]-2-oxoetil}-3-(trifluorometil)benzamida, 3-(Trifluorometil)-N-{2-[(3S)-3-({4-hidroxi-4-(2-(metoximetil)-1,3-tiazol-5-il]ciclohexil}amino)pirrolidin-1-il]-2-oxoetil]-benzamida, 3-(Trifluorometil)-N-[2-((3S)-3-{(4-hidroxi-4-(2-metil-1,3-tiazol-5-il)ciclohexil]-amino}pirrolidin-1-il]-2-oxoetil]-benzamida, 3-(Trifluorometil)-N-[2-((3S)-3-{(4-(2-etil-1,3-tiazol-5-il)-4-hidroxiciclohexil]-amino}pirrolidin-1-il]-2-oxoetil]-benzamida, N-[2-((3S)-3-{[4-Hidroxi-4-[(2-isopropil-1,3-tiazol-5-il)ciclohexil]amino}pirrolidin-1-il]-2-oxoetil]-3-(trifluorometil)benzamida, N-[2-(3S)-(3-{[4-Hidroxi-4-(5-piridin-3-il-1,3-tiazol-2-il)ciclohexil]metil}pirrolidin-1-il]-2-oxoetil]-3-(trifluorometil)benzamida, N-[2-({(3S)-1-[4-Hidroxi-4-(5-piridin-2-il-1,3-tiazol-2-il)ciclohexil]pirrolidin-3-il}-2-oxoetil]-3-(trifluorometil)benzamida, N-[2-{(3S)-3-[(4-hidroxi-4-piradazin-3-ilciclohexil)amino]pirrolidin-1-il}-2-oxoetil]-3-(trifluorometil)benzamida,N-[2-{(3S)-3-[(4-hidroxi-4-pirazin-2-ilciclohexil)amino]pirrolidin-1-il}-2-oxoetil]-3-(trifluorometil)benzamida,N-[2-{(3S)-3-[(4-Hidroxi-4-pirimidin-2-ilciclohexil)amino]pirrolidin-1-il}-2-oxoetil]-3-(trifluorometil)benzamida,6-(1-Hidroxi-4-{[(3S)-1-({[3-(trifluorometil)benzoil]amino}acetil)pirrolidin-3-il]amino}ciclohexil)-Nmetilnicotinamida,6-(1-Hidroxi-4-{[(3S)-1-({[3-(trifluorometil)benzoil]amino}acetil)pirrolidin-3-il]amino}ciclohexil)-N,Ndimetilnicotinamida, N-{2-[(3S)-3-({4-Hidroxi-4-[5-(pirrolidin-1-ilcarbonil)piridin-2-il]ciclohexil}amino)pirrolidin-1-il]-2-oxoetil}-3-(trifluorometil)benzamida, N-[2-((3S)-3-[4-(5-bromopiridin-2-il)-4-hidroxiciclohexil]aminopirrolidin-1-il)-2-oxoetil]-3-(trifluorometil)benzamida,N-[2-[(3S)-3-(4-[5-(2-formilfenil)piridin-2-il]-4-hidroxiciclohexil}amino)pirrolidin-1-il]-2-oxoetil}-3-(trifluorometil)benzamida, N-(2-(3S)-3-[(4-hidroxi-4-5-[2-(hidroximetil)fenil]piridin-2-ilciclohexil)-amino]pirrolidin-1-il-2-oxoetil)-3-(trifluorometil)benzamida bis(trifluoroacetato), N-[2-((3S)-3-[4-hidroxi-4-(4-pirimidin-2-ilfenil)ciclohexil]-aminopirrolidin-1-il)-2-oxoetil]-3-(trifluorometil)benzamidabis(trifluoroacetato), N-[2-((3S)-3-{[4-Hidroxi-4-(5-fenilpiridin-2-il)ciclohexil]-amino}pirrolidin-1-il)-2-oxoetil]-3-(trifluorometil)benzamida.

20. 发明专利

AP2439A 3-Cycloalkylaminopyrrolidine derivatives as modulators of chemokine receptors 未知
公开(公告)号：AP2439A
公开(公告)日：2012-08-31
申请号：AP2006003629
申请日：2004-12-16
申请人： INCYTE CORP
发明人： HAN AMY QI , METCALF BRIAN , ROBINSON DARIUS J
IPC分类号： A61K31/4025 , A61K31/427 , A61K31/44 , A61K31/4439 , A61K31/506 , C07D401/12 , C07D401/14 , C07D417/02
摘要： (wherein R1, R2, R3, R4, R5, R6, R7, X, Y and Z are as defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of chemokine receptors and more specifically as modulators of the CCR2 and/or CCR5 receptor. The compounds and compositions of the invention may bind to chemokine receptors, e.g., the CCR2 and/or CCR5 chemokine receptors, and are useful for treating diseases associated with chemokine, e.g., CCR2 and/or CCR5, activity, such as atherosclerosis, restenosis, lupus, organ transplant rejection and rheumatoid arthritis.

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