公开(公告)号：WO2008126034A3

公开(公告)日：2008-10-23

申请号：PCT/IB2008/051374

申请日：2008-04-11

Applicant: ACTELION PHARMACEUTICALS LTD ,  BUR, Daniel ,  HUBSCHWERLEN, Christian ,  RUEEDI, Georg ,  SURIVET, Jean-Philippe ,  ZUMBRUNN ACKLIN, Cornelia

Inventor： BUR, Daniel ,  HUBSCHWERLEN, Christian ,  RUEEDI, Georg ,  SURIVET, Jean-Philippe ,  ZUMBRUNN ACKLIN, Cornelia

IPC: C07D471/04 ,  A61K31/435 ,  A61P31/00 ,  C07D519/00

Abstract: The invention relates to compounds of formula (I) wherein U, V, W, X, R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , A, B, D, E, G, m and n are as defined in the description, to pharmaceutically acceptable salts of such compounds for use in the manufacture of a medicament for the prevention or treatment of a bacterial infection. Certain compounds of formula (I) are new and are also part of this invention.

公开(公告)号：WO2007099509A2

公开(公告)日：2007-09-07

申请号：PCT/IB2007/050671

申请日：2007-03-01

Applicant: ACTELION PHARMACEUTICALS LTD ,  BEZENCON, Olivier ,  BUR, Daniel ,  CORMINBOEUF, Olivier ,  GRISOSTOMI, Corinna ,  REMEN, Lubos ,  RICHARD-BILDSTEIN, Sylvia ,  WELLER, Thomas

Inventor： BEZENCON, Olivier ,  BUR, Daniel ,  CORMINBOEUF, Olivier ,  GRISOSTOMI, Corinna ,  REMEN, Lubos ,  RICHARD-BILDSTEIN, Sylvia ,  WELLER, Thomas

CPC classification number: C07D277/34 ,  C07D213/64 ,  C07D401/04 ,  C07D417/04

Abstract: The invention relates to novel primary amine 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.

Abstract translation: 本发明涉及新型伯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。

公开(公告)号：WO2006126171A3

公开(公告)日：2007-02-08

申请号：PCT/IB2006051661

申请日：2006-05-24

Applicant: ACTELION PHARMACEUTICALS LTD ,  BUR DANIEL ,  HUBSCHWERLEN CHRISTIAN ,  SURIVET JEAN-PHILIPPE ,  ZUMBRUNN ACKLIN CORNELIA

Inventor： BUR DANIEL ,  HUBSCHWERLEN CHRISTIAN ,  SURIVET JEAN-PHILIPPE ,  ZUMBRUNN ACKLIN CORNELIA

IPC: C07D417/12 ,  A61K31/428 ,  A61K31/538 ,  A61K31/5415 ,  A61P31/00 ,  C07D409/12 ,  C07D413/12

CPC classification number: C07D277/64 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D513/04

Abstract: The invention relates to antibiotic derivatives of formula (I) wherein: A represents -O-, S, -C(=O)-, -C(=NOR 6 )-; Z-B represents NCH 2 CH 2 , NCOCH 2 , NCH 2 CO, NCH 2 CH(OH), CHN(R 8 )CH 2 or CHN(R 8 )C0; D represents binuclear heteroaryl; Y 1 represents -CR 1 - or -N-, Y 2 represents -CR 2 - or -N-, Y 3 represents -CR 3 - or -N- and Y 4 represents -CR 4 - or -N-; U represents -NH-, -O- or -S- and V represents -N- or -CH-; W represents -CH 2 -, -O- or -NR 7 -; R 1 represents H, methyl, ethyl or halogen; R 2 , R 3 and R 4 each represent independently H, C 1 -C 4 alkyl, halogen, or C 1 -C 4 alkoxy; R 5 represents H, C 1 -C 4 alkyl or fluorine; R 6 represents H, C 1 -C 4 alkyl or EiTyI-C 1 -C 4 alkyl; R 7 represents H, C 1 -C 4 alkyl, aryl-Q-Q alkyl or -CH 2 -COOH; R 8 represents H, C 1 -C 4 alkyl or -CH 2 -COOH; with the provisos that if Z-B represents NCH 2 CH 2 , NCOCH 2 , NCH 2 CO or NCH 2 CH(OH), then W represents -CH 2 -; if A represents O or S, then W represents -CH 2 -; and only one or two of Y 1 , Y 2 , Y 3 and Y 4 can represent N at the same time.

Abstract translation: 本发明涉及式（I）的抗生素衍生物，其中：A表示-O-，S，-C（= O） - ， - C（= NOR 6） - 。 ZB表示NCH 2 CH 2，NCOCH 2，NCH 2 CO，NCH 2，/ SUB CH（OH），CHN（R 8）CH 2或CHN（R 8）C 0; D表示双核杂芳基; Y 1表示-CR 1 - 或-N - ，Y 2表示-CR 2 - 或-N - ，Y 3表示-CR 3 - 或-N-，Y 4表示-CR 4 - 或 - -N-; U表示-NH-，-O-或-S-，V表示-N-或-CH-; W表示-CH 2 - ， - O-或-NR 7 - 。 R 1表示H，甲基，乙基或卤素; R 2，R 3和R 4各自独立地表示H，C 1 -C 4， 烷基，卤素或C 1 -C 4烷氧基; R 5表示H，C 1 -C 4烷基或氟; R 6表示H，C 1 -C 4烷基或C 1 -C 1 -C 4烷基或C 1 -C 4 - 烷基; R 7表示H，C 1 -C 4烷基，芳基-QC烷基或-CH 2 -COOH ; R 8表示H，C 1 -C 4烷基或-CH 2 -COOH; 条件是如果ZB表示NCH 2 CH 2，NCOCH 2 N，NCH 2 CO或NCH _{2 CH（OH），则W表示-CH 2 - 。 如果A表示O或S，则W表示-CH 2 - 。 Y 1，Y 2，Y 3和Y 4中只有一个或者两个可以在 同时。}

公开(公告)号：WO2006092268A1

公开(公告)日：2006-09-08

申请号：PCT/EP2006/001827

申请日：2006-02-28

Applicant: ACTELION PHARMACEUTICALS LTD ,  BEZENCON, Olivier ,  BOSS, Christoph ,  BUR, Daniel ,  CORMINBOEUF, Olivier ,  FISCHLI, Walter ,  GRISOSTOMI, Corinna ,  REMEN, Lubos ,  RICHARD, Sylvia ,  SIFFERLEN, Thierry ,  WELLER, Thomas

Inventor： BEZENCON, Olivier ,  BOSS, Christoph ,  BUR, Daniel ,  CORMINBOEUF, Olivier ,  FISCHLI, Walter ,  GRISOSTOMI, Corinna ,  REMEN, Lubos ,  RICHARD, Sylvia ,  SIFFERLEN, Thierry ,  WELLER, Thomas

IPC: C07D451/14 ,  C07D451/02 ,  A61K31/46 ,  A61K31/439

CPC classification number: C07D451/02 ,  C07D451/14

Abstract: The invention relates to novel five-membered heteroaryl 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 comprising one or more of those compounds and especially their use as inhibitors of renin.

Abstract translation: 本发明涉及新型五元杂芳基衍生物及其作为药物组合物制备中的活性成分的用途。 本发明还涉及包括制备化合物的方法，包含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。

公开(公告)号：WO2006010544A3

公开(公告)日：2006-03-30

申请号：PCT/EP2005007892

申请日：2005-07-20

Applicant: ACTELION PHARMACEUTICALS LTD ,  BOLLI MARTIN ,  BUR DANIEL ,  CLOZEL MARTINE ,  FISCHLI WALTER ,  LEHMANN DAVID ,  MATHYS BORIS ,  MUELLER CLAUS ,  NAYLER OLIVER ,  SCHERZ MICHAEL ,  WELLER THOMAS

Inventor： BOLLI MARTIN ,  BUR DANIEL ,  CLOZEL MARTINE ,  FISCHLI WALTER ,  LEHMANN DAVID ,  MATHYS BORIS ,  MUELLER CLAUS ,  NAYLER OLIVER ,  SCHERZ MICHAEL ,  WELLER THOMAS

IPC: C07D333/78 ,  A61K31/4436 ,  A61P37/06 ,  C07D409/12

CPC classification number: C07D333/78 ,  C07D409/12

Abstract: The invention relates to novel thiophene derivatives, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunosuppressive agents.

Abstract translation: 本发明涉及新的噻吩衍生物，其制备及其作为药物活性化合物的用途。 所述化合物特别充当免疫抑制剂。

公开(公告)号：WO2005040165A1

公开(公告)日：2005-05-06

申请号：PCT/EP2004/011186

申请日：2004-10-07

Applicant: ACTELION PHARMACEUTICALS LTD ,  BEZENCON, Olivier ,  SIFFERLEN, Thierry ,  BUR, Daniel ,  FISCHLI, Walter ,  WELLER, Thomas ,  REMEN, Lubos ,  RICHARD-BILDSTEIN, Sylvia

Inventor： BEZENCON, Olivier ,  SIFFERLEN, Thierry ,  BUR, Daniel ,  FISCHLI, Walter ,  WELLER, Thomas ,  REMEN, Lubos ,  RICHARD-BILDSTEIN, Sylvia

IPC: C07D471/08

CPC classification number: C07D471/08

Abstract: The invention relates to novel 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.

Abstract translation: 本发明涉及新型衍生物和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。

公开(公告)号：WO2004096804A1

公开(公告)日：2004-11-11

申请号：PCT/EP2004/004373

申请日：2004-04-26

Applicant: ACTELION PHARMACEUTICALS LTD ,  BEZENCON, Olivier ,  BUR, Daniel ,  FISCHLI, Walter ,  REMEN, Lubos ,  RICHARD-BILDSTEIN, Sylvia ,  WELLER, Thomas

Inventor： BEZENCON, Olivier ,  BUR, Daniel ,  FISCHLI, Walter ,  REMEN, Lubos ,  RICHARD-BILDSTEIN, Sylvia ,  WELLER, Thomas

IPC: C07D471/08

CPC classification number: C07D471/08

Abstract: The invention relates to novel 3,9-diazabicyclo[3.3.1]nonene derivatives, tetrahydropyridine 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.

Abstract translation: 本发明涉及新型的3,9-二氮杂双环[3.3.1]壬烯衍生物，四氢吡啶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。

公开(公告)号：WO2004096366A1

公开(公告)日：2004-11-11

申请号：PCT/EP2004/004371

申请日：2004-04-26

Applicant: ACTELION PHARMACEUTICALS LTD ,  BEZENCON, Oliver ,  BUR, Daniel ,  FISCHLI, Walter ,  REMEN, Lubos ,  RICHARD-BILDSTEIN, Sylvia ,  WELLER, Thomas ,  SIFFERLEN, Thierry

Inventor： BEZENCON, Oliver ,  BUR, Daniel ,  FISCHLI, Walter ,  REMEN, Lubos ,  RICHARD-BILDSTEIN, Sylvia ,  WELLER, Thomas ,  SIFFERLEN, Thierry

IPC: A61P9/00

CPC classification number: C07D513/08

Abstract: The invention relates to novel 9-azabicyclo[3.3.1]nonene 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.

Abstract translation: 本发明涉及新型9-氮杂双环[3.3.1]壬烯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。

公开(公告)号：WO2003093267A1

公开(公告)日：2003-11-13

申请号：PCT/EP2003/003721

申请日：2003-04-08

Applicant: ACTELION PHARMACEUTICALS LTD ,  BEZENCON, Olivier ,  BUR, Daniel ,  FISCHLI, Walter ,  REMEN, Lubos ,  RICHARD-BILDSTEIN, Sylvia ,  WEBER, Hans-Peter ,  WELLER, Thomas

Inventor： BEZENCON, Olivier ,  BUR, Daniel ,  FISCHLI, Walter ,  REMEN, Lubos ,  RICHARD-BILDSTEIN, Sylvia ,  WEBER, Hans-Peter ,  WELLER, Thomas

IPC: C07D471/08

CPC classification number: C07D471/08 ,  A61K31/4995 ,  A61K45/06 ,  Y02A50/411 ,  A61K2300/00

Abstract: The invention relates to novel 3,9-diazabicyclo[3.3.1]nonene derivatives of formula (I) 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 or renin.

Abstract translation: 本发明涉及式（I）的新的3,9-二氮杂双环[3.3.1]壬烯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，特别是其作为抑制剂或肾素的用途的相关方面。

公开(公告)号：WO2012077049A1

公开(公告)日：2012-06-14

申请号：PCT/IB2011/055487

申请日：2011-12-06

Applicant: ACTELION PHARMACEUTICALS LTD ,  BUR, Daniel ,  CORMINBOEUF, Olivier ,  CREN, Sylvaine ,  GRISOSTOMI, Corinna ,  LEROY, Xavier ,  RICHARD-BILDSTEIN, Sylvia

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

Abstract: The invention relates to oxazolyl-methylether derivatives of formula (I), wherein R 1 , R 2 , R 3 , R 4 and R 5 are as defined in the description, their preparation and their use as pharmaceutically active compounds.

Abstract translation: 本发明涉及式（I）的恶唑基 - 甲基醚衍生物，其中R1，R2，R3，R4和R5如说明书中所定义，它们的制备及其作为药物活性化合物的用途。