公开(公告)号：EP3071567A1

公开(公告)日：2016-09-28

申请号：EP14799475.0

申请日：2014-11-18

Applicant: Actelion Pharmaceuticals Ltd

Inventor： BUR, Daniel ,  GRISOSTOMI, Corinna ,  NAYLER, Oliver ,  REMEN, Lubos ,  VERCAUTEREN, Magali ,  WELFORD, Richard

IPC: C07D471/04 ,  C07D471/14 ,  C07D498/12 ,  C07D513/14 ,  A61K31/453 ,  A61K31/4535 ,  A61K31/454 ,  A61K31/4545 ,  A61P11/00 ,  A61P19/10 ,  A61P35/00 ,  A61P1/00 ,  A61P3/10 ,  A61P9/12 ,  A61P25/00

CPC classification number: C07D471/14 ,  C07D471/04 ,  C07D498/12 ,  C07D513/14

Abstract: The present invention relates to compounds of the formula (I), wherein R
1a , R
1b , R
2 , R
3 , and X 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), to methods for the preparation of such compounds of formula (I), and especially to their use as TPH modulators.

Abstract translation: 其中R1a，R1b，R2，R3和X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， 制备式（I）化合物的方法，特别是其作为TPH调节剂的用途。

公开(公告)号：EP2648724A1

公开(公告)日：2013-10-16

申请号：EP11805211.7

申请日：2011-12-06

Applicant: Actelion Pharmaceuticals Ltd.

Inventor： BUR, Daniel ,  CORMINBOEUF, Olivier ,  CREN, Sylvaine ,  GRISOSTOMI, Corinna ,  LEROY, Xavier ,  RICHARD-BILDSTEIN, Sylvia

IPC: A61K31/4192 ,  C07D413/14 ,  A61P29/00 ,  A61P25/00 ,  A61P9/00

CPC classification number: C07D413/14 ,  C07D417/14

Abstract: The invention relates to hydroxylated aminotriazole derivatives of formula (I), wherein Q, R1, R2, R3 and R4 are as defined in the description, their preparation and their use as pharmaceutically active compounds.

公开(公告)号：EP2432760B1

公开(公告)日：2013-07-17

申请号：EP10723342.1

申请日：2010-05-17

Applicant: Actelion Pharmaceuticals Ltd.

Inventor： BUR, Daniel ,  CORMINBOEUF, Olivier ,  CREN, Sylvaine ,  GRISOSTOMI, Corinna ,  LEROY, Xavier ,  RICHARD-BILDSTEIN, Sylvia

IPC: C07C233/58 ,  C07C233/60 ,  C07C233/63 ,  C07D207/09 ,  C07D211/26 ,  C07D213/40 ,  C07D231/12 ,  C07D233/64 ,  C07D235/14 ,  C07D239/30 ,  C07D249/08 ,  C07D277/28 ,  C07D277/62 ,  C07D307/52 ,  C07D319/12

CPC classification number: C07D295/13 ,  C07C233/58 ,  C07C233/59 ,  C07C233/60 ,  C07C233/61 ,  C07C233/63 ,  C07C255/29 ,  C07C2603/94 ,  C07D205/04 ,  C07D207/14 ,  C07D211/26 ,  C07D211/56 ,  C07D211/58 ,  C07D213/40 ,  C07D213/75 ,  C07D231/12 ,  C07D233/36 ,  C07D233/64 ,  C07D235/14 ,  C07D239/30 ,  C07D249/08 ,  C07D261/08 ,  C07D271/08 ,  C07D275/04 ,  C07D277/46 ,  C07D277/58 ,  C07D277/62 ,  C07D285/08 ,  C07D295/125 ,  C07D295/185 ,  C07D307/14 ,  C07D307/52 ,  C07D333/28 ,  C07D417/12

公开(公告)号：EP2358673A1

公开(公告)日：2011-08-24

申请号：EP09764075.9

申请日：2009-11-18

Applicant: Actelion Pharmaceuticals Ltd.

Inventor： AISSAOUI, Hamed ,  BOSS, Christoph ,  CORMINBOEUF, Olivier ,  FRANTZ, Marie-Celine ,  GRISOSTOMI, Corinna

IPC: C07D211/16 ,  C07D401/12 ,  C07D403/12 ,  C07D413/12 ,  C07C237/06 ,  A61K31/165 ,  A61K31/435

CPC classification number: C07C237/22 ,  C07D211/16 ,  C07D401/12 ,  C07D403/12 ,  C07D413/12

Abstract: The invention relates to novel bis-amide derivatives and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including pharmaceutical compositions containing one or more of those compounds and their use as medicaments for the treatment or prevention of protozoal infections, such as especially malaria.

公开(公告)号：EP3071567B1

公开(公告)日：2017-09-06

申请号：EP14799475.0

申请日：2014-11-18

Applicant: Actelion Pharmaceuticals Ltd

Inventor： BUR, Daniel ,  GRISOSTOMI, Corinna ,  NAYLER, Oliver ,  REMEN, Lubos ,  VERCAUTEREN, Magali ,  WELFORD, Richard

IPC: C07D471/04 ,  C07D471/14 ,  C07D498/12 ,  C07D513/14 ,  A61K31/453 ,  A61K31/4535 ,  A61K31/454 ,  A61K31/4545 ,  A61P11/00 ,  A61P19/10 ,  A61P35/00 ,  A61P1/00 ,  A61P3/10 ,  A61P9/12 ,  A61P25/00

CPC classification number: C07D471/14 ,  C07D471/04 ,  C07D498/12 ,  C07D513/14

公开(公告)号：EP3071578A1

公开(公告)日：2016-09-28

申请号：EP14799473.5

申请日：2014-11-18

Applicant: Actelion Pharmaceuticals Ltd

Inventor： BUR, Daniel ,  GRISOSTOMI, Corinna ,  NAYLER, Oliver ,  REMEN, Lubos ,  VERCAUTEREN, Magali ,  WELFORD, Richard

IPC: C07D513/14 ,  A61K31/437 ,  A61P11/06

CPC classification number: C07D513/14

Abstract: wherein R, R1a, R1b, R2, R3, and X 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), to methods for the preparation of such compounds of formula (I), and especially to their use as TPH modulators.

Abstract translation: 其中R，R 1a，R 1b，R 2，R 3和X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， ，用于制备式（I）化合物的方法，特别是其用作TPH调节剂。

公开(公告)号：EP2649068B1

公开(公告)日：2014-10-29

申请号：EP11804810.7

申请日：2011-12-06

Applicant: Actelion Pharmaceuticals Ltd.

Inventor： BUR, Daniel ,  CORMINBOEUF, Olivier ,  CREN, Sylvaine ,  GRISOSTOMI, Corinna ,  LEROY, Xavier ,  RICHARD-BILDSTEIN, Sylvia

IPC: C07D413/14 ,  A61K31/422 ,  A61P29/00

CPC classification number: C07D413/14

公开(公告)号：EP2440555A1

公开(公告)日：2012-04-18

申请号：EP10725500.2

申请日：2010-06-07

Applicant: Actelion Pharmaceuticals Ltd.

Inventor： BUR, Daniel ,  CORMINBOEUF, Olivier ,  CREN, Sylvaine ,  GRISOSTOMI, Corinna ,  LEROY, Xavier ,  RICHARD-BILDSTEIN, Sylvia

IPC: C07D413/14 ,  C07D417/14 ,  A61K31/4192 ,  A61P9/00

CPC classification number: C07D413/14 ,  C07D417/14

Abstract: The invention relates to fluorinated aminotriazole derivatives of formula (I), wherein A, R
1 and R
2 are as defined in the description, their preparation and their use as pharmaceutically active compounds.

公开(公告)号：EP2242743A1

公开(公告)日：2010-10-27

申请号：EP08862120.6

申请日：2008-12-12

Applicant: Actelion Pharmaceuticals Ltd.

Inventor： BUR, Daniel ,  CORMINBOEUF, Olivier ,  CREN, Sylvaine ,  FRETZ, Heinz ,  GRISOSTOMI, Corinna ,  LEROY, Xavier ,  POTHIER, Julien ,  RICHARD-BILDSTEIN, Sylvia

IPC: C07D231/40 ,  C07D411/12 ,  C07D413/12 ,  A61K31/4155 ,  A61P31/18

CPC classification number: C07D231/40 ,  C07D411/12 ,  C07D413/12

Abstract: The invention relates to aminopyrazole derivatives of formula (I), (I) wherein A, E, R1 and R2 are as defined in the description, their preparation and their use as pharmaceutically active compounds.

公开(公告)号：EP1981847A1

公开(公告)日：2008-10-22

申请号：EP07705752.9

申请日：2007-01-31

Applicant: Actelion Pharmaceuticals Ltd.

Inventor： BEZENCON, Olivier ,  BUR, Daniel ,  CORMINBOEUF, Olivier ,  DUBE, Daniel ,  GRISOSTOMI, Corinna ,  MACDONALD, Dwight ,  MCKAY, Dan ,  POWELL, David ,  REMEN, Lubos ,  RICHARD-BILDSTEIN, Sylvia ,  SCHEIGETZ, John ,  THERIEN, Michel ,  WELLER, Thomas

IPC: C07D211/70 ,  C07D451/02 ,  C07D471/08 ,  A61K31/439 ,  A61K31/4418 ,  A61P9/00 ,  C07D401/14 ,  C07D413/10 ,  C07D413/14 ,  C07D211/34

CPC classification number: C07D211/78 ,  C07D211/34 ,  C07D211/70 ,  C07D401/14 ,  C07D413/10 ,  C07D413/12 ,  C07D413/14 ,  C07D451/02 ,  C07D471/08

Abstract: The invention relates to novel secondary amine derivatives of formula (I) 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.