公开(公告)号：EP2102217A2

公开(公告)日：2009-09-23

申请号：EP07849231.1

申请日：2007-11-23

申请人： Actelion Pharmaceuticals Ltd.

发明人： HUBSCHWERLEN, Christian ,  PANCHAUD, Philippe ,  SPECKLIN, Jean-Luc

IPC分类号： C07D498/14 ,  A61K31/5383 ,  A61P31/04

CPC分类号： C07D498/14 ,  C07D209/52 ,  C07D405/14 ,  C07D409/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D495/04 ,  C07D513/04

摘要： The invention relates to novel chimeric antibiotics of formula (I) wherein R1 represents OH, OPO3H2 or OCOR5; R2 represents H, OH or OPO3H2; R3 represents H or halogen; R4 is H, (C1-C3) alkyl, or cycloalkyl; R5 represents piperidin-4-yl or R5 is the residue of a naturally occurring amino acid, of the enantiomer of a naturally occurring amino acid or of dimethylaminoglycine; n is O or 1; and to salts (in particular pharmaceutically acceptable salts) of compounds of formula (I). These chimeric compounds are useful in the manufacture of medicaments for the treatment of infections (e.g. bacterial infections).

公开(公告)号：EP2094685A2

公开(公告)日：2009-09-02

申请号：EP07849292.3

申请日：2007-11-29

申请人： Actelion Pharmaceuticals Ltd.

发明人： AISSAOUI, Hamed ,  BOSS, Christoph ,  GUDE, Markus ,  KOBERSTEIN, Ralf ,  SIFFERLEN, Thierry

IPC分类号： C07D401/12 ,  C07D417/14 ,  C07D513/04 ,  A61K31/4188 ,  A61K31/4523 ,  A61K31/506 ,  A61P25/00

CPC分类号： C07D401/12 ,  C07D417/14 ,  C07D513/04

摘要： The invention relates to piperidine compounds of formula (I) wherein X-R1 represents -N(H)-pyrimidinyl, wherein said pyrimidinyl is unsubstituted or mono-substituted wherein the substituent is selected from (C1-4)alkyl or halogen, or X-R1 represents -NH-C(O)-heterocyclyl, wherein the heterocyclyl is selected from benzofuranyl and imidazo[2,1-b]-thiazolyl, wherein said heterocyclyl is unsubstituted or independently mono-, di-, or tri-substituted wherein the substituents are independently selected from (C1-4)alkyl; A represents a phenyl- or thiazolyl-group, wherein the phenyl or thiazolyl is unsubstituted or mono-substituted with (C1-4)alkyl; B represents a phenyl-group, wherein the phenyl is unsubstituted or mono-, or di- substituted, wherein the substituents are independently selected from the group consisting of (C1-4)alkyl, (C1-4)alkoxy, trifluoromethyl, cyano and halogen; to pharmaceutically acceptable salts thereof, and to the use of such compounds use as medicaments, especially as orexin receptor antagonists.

公开(公告)号：EP1996579A2

公开(公告)日：2008-12-03

申请号：EP07713226.4

申请日：2007-03-09

申请人： Actelion Pharmaceuticals Ltd.

发明人： GAUVIN, Jean-Christophe ,  HUBSCHWERLEN, Christian ,  SURIVET, Jean-Philippe ,  ZUMBRUNN ACKLIN, Cornelia

IPC分类号： C07D405/06 ,  C07D409/14 ,  C07D471/04 ,  C07D495/04 ,  C07D519/00 ,  A61K31/519 ,  A61P31/04

CPC分类号： C07D405/06 ,  C07D409/14 ,  C07D471/04 ,  C07D495/04

摘要： The invention relates to selected antibiotics of formula (Al) wherein R1 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 CRa and, in the case of X, may also represent CRb, Ra representing halogen and Rb representing halogen or alkoxy; A3 represents NHCO, CH2CH2, CH=CH, COCH2, CH(OH)CH2, CH2CH(OH), CH(OH)CH(OH) or OCH2; A4 represents CH2, CO, CH2CH=CH, COCH=CH or CH2CONH; R2 represents hydrogen, alkyl, hydroxyalkyl, alkylcarbonyloxyalkyl, carbamoyloxyalkyl, carboxyalkyl or carbamoylalkyl; R3 and R4 each independently represent hydrogen, hydroxy or alkylcarbonyloxy; or R3 and R4 together represent a bridged dimethylmethylenedioxy chain attached to the carbons bearing R3 and R4; R5 represents hydrogen, alkyl or hydroxyalkyl; and the dotted line represents a single bond or, when R3 and R4 represent hydrogen, also a double bond; and D represents alkyl, aryl or heteroaryl. An example of such an antibiotic is (E)-2-{(2R,3R,6R)-3-[3-(2,5-difluoro-phenyl)- allylamino]-6-[2-(6-methoxy-[l,5]naphthyridin-4-yl)-ethyl]-tetrahydro-pyran-2-yl}-ethanol.

公开(公告)号：EP1981881A1

公开(公告)日：2008-10-22

申请号：EP07705700.8

申请日：2007-01-25

申请人： Actelion Pharmaceuticals Ltd.

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).

公开(公告)号：EP1663993B1

公开(公告)日：2008-03-12

申请号：EP04761896.2

申请日：2004-09-03

申请人： Actelion Pharmaceuticals Ltd.

发明人： FECHER, Anja ,  FRETZ, Heinz ,  HILPERT, Kurt ,  BREU, Volker ,  GILLER, Thomas ,  VALDENAIRE, Olivier

IPC分类号： C07D239/84 ,  A61K31/517 ,  A61P29/00

CPC分类号： C07D239/84 ,  A61K31/517 ,  C07D239/70

摘要： The invention relates to the guanine derivatives of general formula (I), and to hydrates or solvents thereof, for use as neuropeptide FF receptor antagonists in the treatment of pains and hyperalgesia, of withdrawal symptoms of addiction to alcohol, psychotropic drugs or nicotine and in the prevention of or recovery from these addictions, for the regulation of insulin release, food intake, memory functions, blood pressure, electrolyte and energy metabolism, and in the treatment of urinary incontinence.

公开(公告)号：EP1569914A1

公开(公告)日：2005-09-07

申请号：EP03778307.3

申请日：2003-11-10

申请人： Actelion Pharmaceuticals Ltd.

发明人： BOLLI, Martin ,  BOSS, Christoph ,  CLOZEL, Martine ,  FISCHLI, Walter ,  WELLER, Thomas

IPC分类号： C07D239/52 ,  C07D239/46 ,  C07D239/56 ,  A61K31/505

CPC分类号： C07D239/47 ,  C07D239/52 ,  C07D239/56

摘要： The invention relates to novel sulfamic acid amides of General Formula (I) 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 endothelin receptor antagonists. [ADD FORMULA]

公开(公告)号：EP1379523B1

公开(公告)日：2005-07-27

申请号：EP02730036.7

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 ,  WELLER, Thomas ,  VELKER, Jörg

IPC分类号： C07D403/12 ,  A61K31/47 ,  C07D401/12 ,  C07D407/14 ,  C07D471/04 ,  C07D491/04 ,  A61P9/00

CPC分类号： C07D401/12 ,  C07D405/14 ,  C07D471/04 ,  C07D491/04

摘要： The invention relates to novel 1,2,3,4-tetrahydroisoquinoline 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 neurohormonal antagonists especially urotensin II antagonists.

公开(公告)号：EP3897646A1

公开(公告)日：2021-10-27

申请号：EP19832954.2

申请日：2019-12-20

申请人： Actelion Pharmaceuticals Ltd

发明人： CSONKA, Dénes ,  FARES, Wassim ,  HOOGKAMER, Hans ,  TORFS, Koen

IPC分类号： A61K31/506 ,  A61P9/12 ,  A61P11/00

公开(公告)号：EP2943492A1

公开(公告)日：2015-11-18

申请号：EP14701232.2

申请日：2014-01-08

申请人： Actelion Pharmaceuticals Ltd.

发明人： HUBSCHWERLEN, Christian ,  RUEEDI, Georg ,  ZUMBRUNN, Cornelia

IPC分类号： C07D471/06 ,  C07D471/16 ,  C07D487/06 ,  C07D519/00 ,  A61K31/437 ,  A61K31/4375 ,  A61K31/4985 ,  A61K31/536 ,  A61P31/04

CPC分类号： C07D471/06 ,  A61K31/4245 ,  A61K31/4375 ,  C07D471/16 ,  C07D487/06 ,  C07D519/00 ,  Y02A50/401

摘要： The invention relates to antibacterial compounds of formula I wherein U represents CH or N; V represents CH or N, provided that at least one of U and V does not represent N; R represents H, halogen, methyl, methoxy, cyano or ethynyl; either W represents a phenyl group substituted in para position with (C1-C3)alkyl, (C1-C3)alkoxy or (C1-C3)thioalkoxy and optionally in meta position with halogen, or W is a group having one of the formulae W1 and W2 below wherein Q is O or S and X is CH or N; and salts of such compounds.

摘要翻译： 本发明涉及式（I）的抗菌化合物，其中U代表CH或N; V代表CH或N，条件是U和V中的至少一个不代表N; R代表H，卤素，甲基，甲氧基，氰基或乙炔基; 或者W表示在对位被（C 1 -C 3）烷基，（C 1 -C 3）烷氧基或（C 1 -C 3）硫代烷氧基并且任选地在间位被卤素取代的苯基，或者W为基团 具有以下式W 1和W 2中的一个，其中Q是O或S且X是CH或N; 和这些化合物的盐。

公开(公告)号：EP2841434A1

公开(公告)日：2015-03-04

申请号：EP13730322.8

申请日：2013-04-26

申请人： Actelion Pharmaceuticals Ltd.

发明人： ABELE, Stefan ,  MEIER, Hans ,  SCHMIDT, Gunther ,  STEINER, Heinz

IPC分类号： C07D471/04 ,  A61K31/4375

CPC分类号： C07D471/04

摘要： The invention relates to a new process suitable for manufacturing the compounds of formula I (I) wherein W is H, Br, CI or methyl, which are synthetic intermediates useful preparation of antibiotic compounds.