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21. 发明专利

BR0314353A 未知
公开(公告)号：BR0314353A
公开(公告)日：2005-07-19
申请号：BR0314353
申请日：2003-09-12
申请人： ACTELION PHARMACEUTICALS LTD
发明人： AISSAOUI HAMED , BINKERT CHRISTOPH , MATHYS BORIS , MUELLER CLAUS , NAYLER OLIVER , SCHERZ MICHAEL , WELLER THOMAS , VELKER JOERG , CLOZEL MARTINE
IPC分类号： C07D215/00 , C07D401/12
摘要： The invention relates to novel 1-pyridin-4-yl urea 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 neurohormonal antagonists.

22. 发明专利

HU0402508A2 1,2,3,4-TETRAHYDROISOQUINOLINES DERIVATIVES AS UROTENSIN II RECEPTOR ANTAGONISTS AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM 未知
公开(公告)号：HU0402508A2
公开(公告)日：2005-03-29
申请号：HU0402508
申请日：2002-03-20
申请人： ACTELION PHARMACEUTICALS LTD
发明人： AISSAOUI HAMED , BINKERT CHRISTOPH , CLOZEL MARTINE , MATHYS BORIS , MUELLER CLAUS , NAYLER OLIVER , SCHERZ MICHAEL , VELKER JOERG , WELLER THOMAS
IPC分类号： C07D491/056 , A61K31/47 , A61K31/4709 , A61K31/4725 , A61K31/4741 , A61K31/4745 , A61K31/55 , A61K45/00 , A61P3/10 , A61P5/14 , A61P7/00 , A61P7/06 , A61P9/00 , A61P9/04 , A61P9/06 , A61P9/08 , A61P9/10 , A61P9/12 , A61P11/00 , A61P11/06 , A61P13/08 , A61P13/12 , A61P15/10 , A61P21/00 , A61P25/04 , A61P25/06 , A61P25/08 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P27/02 , A61P27/06 , A61P27/16 , A61P29/02 , A61P31/04 , A61P35/00 , A61P43/00 , C07D401/12 , C07D403/12 , C07D405/14 , C07D407/14 , C07D471/02 , C07D471/04 , C07D491/04
摘要： The invention relates to novel 1,2,3,4-tetrahydroisoquinoline 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 neurohormonal antagonists.

23. 发明专利

CA2523566A1 PIPERAZINE-ALKYL-UREIDO DERIVATIVES 未知
公开(公告)号：CA2523566A1
公开(公告)日：2004-11-18
申请号：CA2523566
申请日：2004-05-04
申请人： ACTELION PHARMACEUTICALS LTD
发明人： SCHERZ MICHAEL , CLOZEL MARTINE , BINKERT CHRISTOPH , MATHYS BORIS , NAYLER OLIVER , AISSAOUI HAMED , MUELLER CLAUS , WELLER THOMAS , VELKER JOERG
IPC分类号： A61P9/10 , A61P9/12 , C07D215/42 , C07D401/12 , A61K31/4709 , A61K31/497
摘要： The invention relates to novel piperazine derivatives and related compounds and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processe s for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and especially their use as neurohormonal antagonists. (I)

24. 发明专利

BRPI0808789A2 未知
公开(公告)号：BRPI0808789A2
公开(公告)日：2014-08-12
申请号：BRPI0808789
申请日：2008-02-29
申请人： ACTELION PHARMACEUTICALS LTD
发明人： BOLLI MARTIN , MATHYS BORIS , MUELLER CLAUS , NAYLER OLIVER , STEINER BEAT , VELKER JOERG
IPC分类号： C07D413/04 , A61K31/4439 , A61P37/00 , C07D417/04
摘要： The invention relates to novel amino-pyridine derivatives, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunomodulating agents.

25. 发明专利

BRPI0716909A2 未知
公开(公告)号：BRPI0716909A2
公开(公告)日：2013-11-05
申请号：BRPI0716909
申请日：2007-09-10
申请人： ACTELION PHARMACEUTICALS LTD
发明人： BOLLI MARTIN , MUELLER CLAUS , MATHYS BORIS , VOSS DAVID LEHMANN , NAYLER OLIVER , VELKER JOERG , STEINER BEAT
IPC分类号： C07D271/06 , A61K31/4245 , A61P35/00 , A61P37/00 , C07D271/107
摘要： The invention relates to phenyl derivatives of formula (I), their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunomodulating agents.

26. 发明专利

BRPI0716482A2 未知
公开(公告)号：BRPI0716482A2
公开(公告)日：2013-03-12
申请号：BRPI0716482
申请日：2007-07-10
申请人： ACTELION PHARMACEUTICALS LTD
发明人： BOLLI MARTIN , MUELLER CLAUS , MATHYS BORIS , LEHMANN DAVID , NAYLER OLIVER , VELKER JOERG , STEINER BEAT
IPC分类号： C07D333/22 , A61K31/381 , A61K31/4245 , A61P17/00 , A61P37/00 , C07D413/04
摘要： The invention relates to novel thiophene derivatives, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunomodulating agents.

27. 发明专利

DK2069336T3 PYRIDIN-4-YL-DERIVATER SOM IMMUNOMODULERENDE MIDLER 未知
公开(公告)号：DK2069336T3
公开(公告)日：2013-02-25
申请号：DK07826287
申请日：2007-09-06
申请人： ACTELION PHARMACEUTICALS LTD
发明人： BOLLI MARTIN , LEHMANN DAVID , MUELLER CLAUS , NAYLER OLIVER , VELKER JOERG , MATHYS BORIS , STEINER BEAT
IPC分类号： C07D413/04 , A61K31/4439 , A61P9/00 , A61P19/00 , A61P35/00 , A61P37/00 , C07D417/04

28. 发明专利

DK2069335T3 PYRIDIN-3-YLDERIVATER SOM IMMUNOMODULERINGSMIDLER 未知
公开(公告)号：DK2069335T3
公开(公告)日：2013-02-18
申请号：DK07826286
申请日：2007-09-06
申请人： ACTELION PHARMACEUTICALS LTD
发明人： BOLLI MARTIN , LEHMANN DAVID , MUELLER CLAUS , NAYLER OLIVER , MATHYS BORIS , STEINER BEAT , VELKER JOERG
IPC分类号： C07D413/04 , A61K31/4439 , A61P9/00 , A61P19/00 , A61P35/00 , A61P37/00 , C07D417/04

29. 发明专利

ES2365747T3 DERIVADOS DE BENZO[C]TIOFENO HIDROGENADOS COMO INMUNOMODULADORES. 未知
公开(公告)号：ES2365747T3
公开(公告)日：2011-10-10
申请号：ES06727679
申请日：2006-03-20
申请人： ACTELION PHARMACEUTICALS LTD
发明人： BOLLI MARTIN , LEHMANN DAVID , MATHYS BORIS , MUELLER CLAUS , NAYLER OLIVER , VELKER JOERG , WELLER THOMAS
IPC分类号： C07D333/72 , A61K31/38 , A61K31/41 , A61P37/00 , C07D333/78 , C07D409/12 , C07D413/04 , C07D413/14
摘要： Un compuesto seleccionado del grupo constituido por tiofenos de la fórmula (I) **Fórmula** en la que A representa -CONH-CH2-, -CO-CH=CH-, -CO-CH2CH2-, -CO-CH2-O-, -CO-CH2-NH-, **Fórmula** R 1 representa hidrógeno, alquilo C1-5, alcoxi C1-5, o halógeno; R 2 representa hidrógeno, alquilo C1-5, alcoxi C1-5, trifluorometilo, trifluorometoxi o halógeno; R 3 representa hidrógeno, hidroxialquilo C1-5, 2,3-dihidroxipropilo, di-(hidroxi-alquilo C1-5)-alquilo-C1-5, -CH2-(CH2)k NR 31 R 32 , (ácido azetidin-3-carboxílico)-1-il-metilo, (éster alquílico C1-5 de ácido azetidin-3-carboxílico)-1-il-metilo, 2 [(ácido azetidin-3-carboxílico)-1-il]-etilo, 2-[(éster alquílico C1-5- de ácido azetidin-3-carboxílico)-1-il]-etilo, 3-[(ácido azetidin-3-carboxílico)-1-il]-propilo, 3-[(éster alquílico C1-5 de ácido azetidin-3-carboxílico)-1-il]-propilo, (ácido pirrolidin-3-carboxílico)-1-il-metilo, (éster alquílico C1-5 de ácido pirrolidin-3-carboxílico)-1-il-metilo, (ácido pirrolidin-2 carboxílico)-1-il-metilo, (éster alquílico C1-5 de ácido pirrolidin-2-carboxílico)-1-il-metilo, 2-[(ácido pirrolidin-3carboxílico)-1-il]-etilo, 2-[(éster alquílico C1-5 de ácido pirrolidin-3-carboxílico)-1-il]-etilo, 2-[(ácido pirrolidin-2carboxílico)-1-il]-etilo, 2-[(éster alquílico C1-5 de ácido pirrolidin-2-carboxílico)-1-il]-etilo, 3-[(ácido pirrolidin-3carboxílico)-1-il]-propilo, 3-[(éster alquílico C1-5 de ácido pirrolidin-3-carboxílico)-1-il]-propilo, 3-[(ácido pirrolidin-2carboxílico)-1-il]-propilo, 3-[(éster alquílico C1-5 de ácido pirrolidin-2-carboxílico)-1-il]-propilo, -CH2-(CH2)n-CONR 31 R 32 , -CO-NHR 31 , 1-(1-(3-carboxi-azetidinil))-2-acetilo, 1-(1-(2-carboxi-pirrolidinil))-2-acetilo, 1-(1-(3-carboxi-pirrolidinil))-2acetilo, 1-(1-(3-carboxi-azetidinil))-3-propionilo, 1-(1-(2-carboxi-pirrolidinil))-3-propionilo, 1-(1-(3-carboxi-pirrolidinil))-3propionilo, -(CH2)nCH(OH)-CH2-NR 31 R 32 , hidroxilo, alcoxi C1-5, fluoroalcoxi C1-5, hidroxialcoxi C2-5, di-(hidroxialquilo C1-5)-alcoxi C1-5, 1-glicerilo, 2-glicerilo, 2-hidroxi-3-metoxi-propoxi, -OCH2-(CH2)m-NR 31 R 32 , 2-pirrolidin-1-il-etoxi, 3pirrolidin-1-il-propoxi, 2-piperazin-1-il-etoxi, 2-[4-(alquilo C1-5)-piperazin-1-il]-etoxi, 2-[4-(2-hidroxi-etil)-piperazin-1-il] etoxi, 3-piperazin-1-il-propoxi, 3-[4-(alquilo C1-5)-piperazin-1-il]-propoxi, 3-[4-(2-hidroxi-etil)-piperazin-1-il]-propoxi, 2morfolin-4-il-etoxi, 3-morfolin-4-il-propoxi, 2-[(ácido azetidin-3-carboxílico)-1-il]-etoxi, 2-[(éster alquílico C1-5 de ácido azetidin-3-carboxílico)-1-il]-etoxi, 2-[(ácido pirrolidin-3-carboxílico)-1-il]-etoxi, 2-[(éster alquílico C1-5 de ácido pirrolidin 3-carboxílico)-1-il]-etoxi, 2-[(ácido pirrolidin-2-carboxílico)-1-il]-etoxi, 2-[(éster alquílico C1-5 de ácido pirrolidin-2carboxílico)-1-il]-etoxi, 2-[(2-hidroxi-pirrolidin)-1-il]-etoxi, 2-[(3-hidroxi-pirrolidin)-1-il]-etoxi, 3-[(ácido azetidin-3 carboxílico)-1-il]-propoxi, 3-[(éster alquílico C1-5 de ácido azetidin-3-carboxílico)-1-il]-propoxi, 3-[(ácido pirrolidin-3carboxílico)-1-il]-propoxi, 3-[(éster alquílico C1-5 de ácido pirrolidin-3-carboxílico)-1-il]-propoxi, 3-[(ácido pirrolidin-2carboxílico)-1-il]-propoxi, 3-[(éster alquílico C1-5 de ácido pirrolidin-2-carboxílico)-1-il]-propoxi, 3-[(2-hidroxi-pirrolidin) 1-il]-propoxi, 3-[(3-hidroxi-pirrolidin)-1-il]-propoxi, 2-amino-3-hidroxi-2-hidroximetil-propoxi, -O-CH2-CONR 31 R 32 , 1-(1 (3-carboxi-azetidinil))-1-oxo-2-etoxi, 1-(1-(ácido pirrolidin-2-carboxílico)-1-il)-1-oxo-2-etoxi, 1-(1-(ácido pirrolidin-3 carboxílico)-1-il)-1-oxo-2-etoxi, 3-carbamoil-propoxi, 3-(alquilcarbamoilo C1-5)propoxi, 3-(2hidroxietilcarbamoil)propoxi, -OCH2-CH(OH)-CH2-NR 31 R 32 , 3-[(ácido azetidin-3-carboxílico)-1-il]-2-hidroxipropoxi, 3 [(éster alquílico C1-5 de ácido azetidin-3-carboxílico)-1-il]-2-hidroxipropoxi, 2-hidroxi-3-[(ácido pirrolidin-3-carboxílico) 1-il]-propoxi, 2-hidroxi-3-[(éster alquílico C1-5 de ácido pirrolidin-3-carboxílico)-1-il]-propoxi, 2-hidroxi-3-[(ácido pirrolidin-2-carboxílico)-1-il]-propoxi, 2-hidroxi-3-[(éster alquílico C1-5 de ácido pirrolidin-2-carboxílico)-1-il]-propoxi, 2hidroxi-3-[(2-hidroxi-pirrolidin)-1-il]-propoxi, 2-hidroxi-3-[(3-hidroxi-pirrolidin)-1-il]-propoxi, 2-hidroxi-3-pirrolidin-1-ilpropoxi, 2-hidroxi-3-piperazin-1-il-propoxi, 2-hidroxi-3-[4-(alquilo C1-5)-piperazin-1-il]-propoxi, 2-hidroxi-3-[4-(2-hidroxietil)-piperazin-1-il]-propoxi, 2-hidroxi-3-morfolin-4-il-propoxi, -NR 31 R 32 , -NHCO-R 31 , -CH2-(CH2)k-NHSO2R 33 , -(CH2)nCH(OH)-CH2-NHSO2R 33 , -OCH2-(CH2)m-NHSO2R 33 , -OCH2-CH(OH)-CH2-NHSO2R 33 , -CH2-(CH2)k-NHCOR 34 , -(CH2)nCH(OH)-CH2-NHCOR 34 , -OCH2-(CH2)m-NHCOR 34 , -OCH2-CH(OH)-CH2-NHCOR , o SO2NHR 31 ; R 31 representa hidrógeno, metilo, etilo, 1-propilo, 2-propilo, 2-hidroxietilo, 2-hidroxi-1-hidroximetil-etilo, 2,3dihidroxipropilo, 2-alcoxietilo C1-5, 3-hidroxipropilo, 3-alcoxipropilo C1-5, 2-aminoetilo, 2-(alquilamino C1-5)etilo, 2-(di (alquilo C1-5)amino)etilo, carboximetilo, alquilcarboximetilo C1-5, 2-carboxietilo, o 2-(alquilcarboxi C1-5)etilo; R 32 representa hidrógeno, metilo, o etilo; R 33 representa metilo, etilo, propilo, isopropilo, butilo, 2-hidroxietilo, 2-metoxietilo, metilamino, etilamino, propilamino, isopropilamino, n-butilamino o dimetilamino; R 34 representa hidroximetilo, hidroxietilo, aminometilo, metilaminometilo, dimetilaminometilo, aminoetilo, 2 metilamino-etilo o 2-dimetilamino-etilo; k representa el número entero 1, 2 ó 3; m representa el número entero 1 ó 2; n representa 0, 1 ó 2; R 4 representa hidrógeno, alquilo C1-5 o halógeno; R 5 representa metilo o etilo; R 6 representa metilo o etilo; o R 5 y R 6 conjuntamente forman un anillo carboxíclico de 3, 4, o 5 miembros; y R 7 representa hidrógeno, metilo, etilo, n-propilo, isopropilo, trifluorometilo, hidroximetilo, metoximetilo, metoxi, metiltio, hidroxicarbonilo, aminocarbonilo, mono- o di-(alquilo C1-5)aminocarbonilo, amino, mono- o di-(alquilo C1 5)amino; y los isómeros de configuración tales como los enantiómeros ópticamente puros, mezclas de enantiómeros tales como racematos, diastereómeros, mezclas de diastereómeros, racematos diastereoméricos, y mezclas de racematos diastereoméricos, así como también sales y complejos solventes de dichos compuestos y formas morfológicas.

30. 发明专利

AT510831T 未知
公开(公告)号：AT510831T
公开(公告)日：2011-06-15
申请号：AT06727679
申请日：2006-03-20
申请人： ACTELION PHARMACEUTICALS LTD
发明人： BOLLI MARTIN , LEHMANN DAVID , MATHYS BORIS , MUELLER CLAUS , NAYLER OLIVER , VELKER JOERG , WELLER THOMAS
IPC分类号： C07D333/72 , A61K31/38 , A61K31/41 , A61P37/00 , C07D333/78 , C07D409/12 , C07D413/04 , C07D413/14
摘要： The invention relates to novel thiophene derivatives, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunosuppressive agents.

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