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1. 发明申请

WO2017037039A1 ANTIBACTERIAL HETEROCYCLIC DERIVATIVES 审中-公开
标题翻译：抗真菌杂环衍生物
公开(公告)号：WO2017037039A1
公开(公告)日：2017-03-09
申请号：PCT/EP2016/070362
申请日：2016-08-30
申请人： ACTELION PHARMACEUTICALS LTD
发明人： CHAPOUX, Gaelle , DIETHELM, Stefan , GAUVIN, Jean-Christophe , PANCHAUD, Philippe , SURIVET, Jean-Philippe
IPC分类号： C07D263/54 , A61K31/423 , A61K31/428 , C07D277/62
CPC分类号： C07D277/68 , C07D263/58
摘要： The invention relates to antibacterial compounds of formula (I), wherein R 1 , M, R 2 , R 3 , and V are as described in the description, to their preparation, to 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 antibacterial agents.
摘要翻译：本发明涉及式（I）的抗菌化合物，其中R 1，M，R 2，R 3和V如本说明书所述，其制备方法，其盐类及其作为药物的用途，含有一种或更多的式（I）化合物，特别是其作为抗菌剂的用途。

2. 发明申请

WO2015004265A1 PROCESS FOR PREPARING A PYRIMIDINE INTERMEDIATE 审中-公开
标题翻译：制备吡嗪中间体的方法
公开(公告)号：WO2015004265A1
公开(公告)日：2015-01-15
申请号：PCT/EP2014/064904
申请日：2014-07-11
申请人： ACTELION PHARMACEUTICALS LTD
发明人： ABELE, Stefan , FUNEL, Jacques-Alexis , SCHINDELHOLZ, Ivan
IPC分类号： C07D239/30 , C07D239/47
CPC分类号： C07D239/47 , C07D239/30
摘要： The present invention relates to a process for preparing a pyrimidine intermediate, namely the compound of formula I-2 or a salt thereof. Said compound of formula I-2 or its salt can be used to prepare macitentan. Macitentan (chemical names: N -[5-(4-bromophenyl)-6-[2-[(5-bromo- 2-pyrimidinyl)oxy]ethoxy]-4-pyrimidinyl] - N' -propylsulfamide or N -[5-(4-bromophenyl)- 6- {2- [(5 -bromopyrimidin-2-yl)oxy] ethoxy } pyrimidin-4-yl] - N' -propylsulfuric diamide) is an endothelin receptor antagonist that has notably been approved by the US Food and Drug Administration and the European Commission for the treatment of pulmonary arterial hypertension. It has been first disclosed in WO 02/053557. The last step of one of the potential preparation routes described in WO 02/053557, called "Possibility A" and "Possibility B", can be summarised as shown in Scheme Al hereafter.
摘要翻译：本发明涉及制备嘧啶中间体即式I-2化合物或其盐的方法。所述式I-2的化合物或其盐可用于制备麦替康。（化学名称：N- [5-（4-溴苯基）-6- [2 - [（5-溴-2-嘧啶基）氧]乙氧基] -4-嘧啶基] -N'-丙基磺酰胺或N- [5 - （4-溴苯基）-6- {2 - [（5-溴嘧啶-2-基）氧基]乙氧基}嘧啶-4-基] -N'-丙基硫酸二酰胺）是内皮素受体拮抗剂，其显着地被美国食品和药物管理局和欧洲委员会治疗肺动脉高压。首先在WO 02/053557中披露。在WO 02/053557中描述的称为“可能性A”和“可能性B”的潜在制备途径之一的最后一步可以总结如下方案A1所示。

3. 发明申请

WO2010041219A1 2-BENZOTHIOPHENYL-AND 2-NAPHTHYL-0XAZ0LIDIN0NES AND THEIR AZAISOSTERE ANALOGUES AS ANTIBACTERIAL AGENTS 审中-公开
标题翻译： 2-苯并噻吩和2-萘基-OXAZ0LIDINONES及其作为抗菌剂的AZAISOSTERE类似物
公开(公告)号：WO2010041219A1
公开(公告)日：2010-04-15
申请号：PCT/IB2009/054434
申请日：2009-10-09
申请人： ACTELION PHARMACEUTICALS LTD , EGGER, Verena , GUDE, Markus , HUBSCHWERLEN, Christian , RUEEDI, Georg , SURIVET, Jean-Philippe , ZUMBRUNN ACKLIN, Cornelia
发明人： EGGER, Verena , GUDE, Markus , HUBSCHWERLEN, Christian , RUEEDI, Georg , SURIVET, Jean-Philippe , ZUMBRUNN ACKLIN, Cornelia
IPC分类号： C07D413/04 , C07D417/04 , C07D417/14 , C07D495/04 , A61K31/422 , A61P31/04
CPC分类号： C07D417/14 , C07D413/14 , C07D417/04 , C07D495/04
摘要： The invention relates to antibacterial compounds of Formula (I) wherein U, V, W, X, R 1 , R 2 , m, A, B and G are as defined in the description, to pharmaceutically acceptable salts of such compounds and to the use of these compounds in the manufacture of a medicament.
摘要翻译：本发明涉及其中U，V，W，X，R 1，R 2，m，A，B和G如说明书中所定义的式（I）的抗菌化合物与这些化合物的药学上可接受的盐以及使用这些化合物在制备药物中。

4. 发明申请

WO2010041218A2 OXAZOLIDINYL ANTIBIOTICS 审中-公开
标题翻译：奥昔布林抗生素
公开(公告)号：WO2010041218A2
公开(公告)日：2010-04-15
申请号：PCT/IB2009/054433
申请日：2009-10-09
申请人： ACTELION PHARMACEUTICALS LTD , HUBSCHWERLEN, Christian , RUEEDI, Georg , SURIVET, Jean-Philippe , ZUMBRUNN ACKLIN, Cornelia
发明人： HUBSCHWERLEN, Christian , RUEEDI, Georg , SURIVET, Jean-Philippe , ZUMBRUNN ACKLIN, Cornelia
IPC分类号： C07D413/14 , C07D417/14 , C07D471/04 , A61K31/4709 , A61K31/498 , A61K31/4985
CPC分类号： C07D413/14 , C07D413/12 , C07D417/14 , C07D471/04
摘要： The invention relates to antibacterial compounds of Formula (I) wherein R 1 is alkoxy or halogen; U and V each independently are CH or N; "----" is a bond or is absent; W is CH or N or, when "----" is absent, W is CH 2 or NH, with the proviso that U, V and W are not all N; A is a bond or CH 2 ; R 2 is H or, provided A is CH 2 , may also be OH; m and n each independently are 0 or 1; D is CH 2 or a bond; G represents a phenyl group substituted once or twice in the meta and/or para position (s) by substituents selected from alkyl, (C 1 -C 3 )alkyl and halogen, or G is a group G 1 or G 2 wherein Z 1 , Z 2 and Z 3 may each represent CH or N; X is N or CH and Q is O or S; it being understood that if m and n each are 0, then A is CH 2 ; and salts of such compounds.
摘要翻译：本发明涉及式（I）的抗菌化合物，其中R 1是烷氧基或卤素; U和V各自独立地为CH或N; “----”是债券或不存在; W是CH或N，或当“----”不存在时，W是CH2或NH，条件是U，V和W不全为N; A是键或CH2; R2是H，或者如果A是CH2，也可以是OH; m和n各自独立地为0或1; D是CH 2或键; G表示通过选自烷基，（C1-C3）烷基和卤素的取代基在间位和/或对位取代一次或两次的苯基，或G是基团G1或G2，其中Z1，Z2和Z3可以各自表示CH或N; X为N或CH，Q为O或S; 应理解，如果m和n各自为0，则A为CH 2; 和这些化合物的盐。

5. 发明申请

WO2010038200A1 OXAZOLIDINE COMPOUNDS AS OREXIN RECEPTOR ANTAGONISTS 审中-公开
标题翻译：奥沙芬化合物作为OREXIN受体拮抗剂
公开(公告)号：WO2010038200A1
公开(公告)日：2010-04-08
申请号：PCT/IB2009/054273
申请日：2009-09-30
申请人： ACTELION PHARMACEUTICALS LTD , AISSAOUI, Hamed , BOSS, Christoph , BROTSCHI, Christine , GABILLET, Jerome , SIEGRIST, Romain , SIFFERLEN, Thierry , WILLIAMS, Jodi T.
发明人： AISSAOUI, Hamed , BOSS, Christoph , BROTSCHI, Christine , GABILLET, Jerome , SIEGRIST, Romain , SIFFERLEN, Thierry , WILLIAMS, Jodi T.
IPC分类号： C07D417/12 , C07D417/14 , A61K31/422 , C07D471/04 , A61P25/00 , A61P25/22 , A61P25/28 , A61P25/30
CPC分类号： C07D417/14 , C07D417/12 , C07D471/04
摘要： The invention relates to oxazolidine derivatives of the formula (I) wherein A, B, and R 1 are as described in the description, to salts, especially pharmaceutically acceptable salts, of such compounds and to their use as medicaments, especially as orexin receptor antagonists.
摘要翻译：本发明涉及式（I）的恶唑烷衍生物，其中A，B和R 1如描述中所述，这些化合物的盐，特别是药学上可接受的盐，以及它们作为药物，特别是作为食欲素受体拮抗剂的用途。

6. 发明申请

WO2009034546A3 TRANS-DECAHYDROISOQUINOLINE DERIVATIVES 审中-公开
公开(公告)号：WO2009034546A3
公开(公告)日：2009-03-19
申请号：PCT/IB2008/053688
申请日：2008-09-12
申请人： ACTELION PHARMACEUTICALS LTD , HUBSCHWERLEN, Christian , RUEEDI, Georg , SURIVET, Jean-Philippe , ZUMBRUNN ACKLIN, Cornelia
发明人： HUBSCHWERLEN, Christian , RUEEDI, Georg , SURIVET, Jean-Philippe , ZUMBRUNN ACKLIN, Cornelia
IPC分类号： C07D401/04 , C07D471/04 , C07D519/00 , A61K31/4725 , A61K31/04
摘要： The invention relates to antibacterial compounds of formula (I) wherein R 1 is alkoxy, one or two of U, V, W, X represent(s) N, the remaining represents CH, whereby V may also represent CR a, W may also represent CR b and X may also represent CR C , R a is hydroxyalkyl; R b is alkoxycarbonyl, carboxy or hydroxyalkyl; R c is halogen, R 2 is alkoxycarbonyl, carboxy, hydroxyalkyl or aminoalkyl, A is CH 2 B, C(=O)B or CH 2 CH=CHD, B is the group (II) wherein Z is N or CH and the ring P is selected from the formula (III) in which Q is O or S, and D is aryl (e.g. 1,4-difluoro-2 -phenyl).

7. 发明申请

WO2007086016A1 TETRAHYDROPYRANE ANTIBIOTICS 审中-公开
标题翻译：四氢呋喃抗生素
公开(公告)号：WO2007086016A1
公开(公告)日：2007-08-02
申请号：PCT/IB2007/050252
申请日：2007-01-25
申请人： ACTELION PHARMACEUTICALS LTD , HUBSCHWERLEN, Christian , SURIVET, Jean-Philippe , ZUMBRUNN ACKLIN, Cornelia
发明人： HUBSCHWERLEN, Christian , SURIVET, Jean-Philippe , ZUMBRUNN ACKLIN, Cornelia
IPC分类号： C07D405/06 , C07D405/12 , C07D471/04 , C07D513/04 , A61K31/435 , A61K31/54 , A61P31/00
CPC分类号： C07D405/06 , C07D405/12 , C07D471/04 , C07D513/04
摘要： The invention relates to antibiotic tetrahydro rane derivatives of formula (I).
摘要翻译：本发明涉及式（I）的抗生素四氢兰衍生物。

8. 发明申请

WO2006126171A2 NEW ANTIBIOTIC DERIVATIVES 审中-公开
标题翻译：新型抗生素衍生物
公开(公告)号：WO2006126171A2
公开(公告)日：2006-11-30
申请号：PCT/IB2006/051661
申请日：2006-05-24
申请人： ACTELION PHARMACEUTICALS LTD , BUR, Daniel , HUBSCHWERLEN, Christian , SURIVET, Jean-Philippe , ZUMBRUNN ACKLIN, Cornelia
发明人： BUR, Daniel , HUBSCHWERLEN, Christian , SURIVET, Jean-Philippe , ZUMBRUNN ACKLIN, Cornelia
IPC分类号： C07D417/12 , C07D413/12 , C07D409/12 , A61P31/00 , A61K31/5415
CPC分类号： C07D277/64 , C07D409/12 , C07D413/12 , C07D417/12 , C07D513/04
摘要： 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.
摘要翻译：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。}

9. 发明申请

WO2006032466A2 NEW BICYCLIC ANTIBIOTICS 审中-公开
标题翻译：新的双相抗体
公开(公告)号：WO2006032466A2
公开(公告)日：2006-03-30
申请号：PCT/EP2005/010154
申请日：2005-09-20
申请人： ACTELION PERCUREX AG , HUBSCHWERLEN, Christian , SURIVET, Jean-Philippe , ZUMBRUNN ACKLIN, Cornelia
发明人： HUBSCHWERLEN, Christian , SURIVET, Jean-Philippe , ZUMBRUNN ACKLIN, Cornelia
CPC分类号： C07D471/04 , C07D405/06 , C07D405/12 , C07D405/14 , C07D413/14 , C07D417/12 , C07D417/14 , C07D491/04 , C07D513/04
摘要： The invention relates to novel antibiotics of formula (I) wherein R 1 represents alkyl, alkoxy, haloalkoxy, halogen or cyano; one or two of U, V, W and X represent(s) N, the remaining represent CH, or, in case of U, V and/or W, may also represent CR a and, in the case of X, may also represent CR b ; R a represents halogen; R b represents halogen or alkoxy; M is a linking chain containing a non-aromatic cyclic or heterocyclic group, and D represents alkyl, aryl or heteroaryl.
摘要翻译：本发明涉及式（I）的新抗生素，其中R

10. 发明申请

WO2022162163A1 PROCESS FOR MANUFACTURING A DIPHENYLPYRAZINE DERIVATIVE 审中-公开
公开(公告)号：WO2022162163A1
公开(公告)日：2022-08-04
申请号：PCT/EP2022/052084
申请日：2022-01-28
申请人： ACTELION PHARMACEUTICALS LTD
发明人： VANIERSCHOT, Ronny , COLLAS, Alain , LEYS, Carina , VAN MECHELEN, Kore
IPC分类号： C07D241/20 , A61P11/00 , A61K31/4965
摘要： The present invention relates to a process for the manufacturing of calcium;{4-[(5, 6- diphenylpyrazin-2-yl)(propan-2-yl)amino]butoxy}acetate, or a pharmaceutically acceptable hydrate or solvate thereof. Moreover, it relates to calcium;{4-[(5,6-diphenylpyrazin-2- yl)(propan-2-yl)amino]butoxy}acetate with high purity, as well as to crystalline forms of calcium;{4-[(5,6-diphenylpyrazin-2-yl)(propan-2-yl)amino]butoxy}acetate and hydrates and solvates thereof. Furthermore, the invention relates to the use of calcium;{4-[(5, 6- diphenylpyrazin-2-yl)(propan-2-yl)amino]butoxy}acetate for the treatment or prevention of e.g. pulmonary arterial hypertension (PAH) or chronic thromboembolic pulmonary hypertension (CTEPH).

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