Patents Assigned to Actelion Pharmaceuticals
  • Publication number: 20170129884
    Abstract: The present invention relates to azaindole acetic acid derivatives of formula (I), wherein R1 and R2 are as described in the description and their use as prostaglandin receptor modulators, most particularly as prostaglandin D2 receptor modulators, in the treatment of various prostaglandin-mediated diseases and disorders, to pharmaceutical compositions containing these compounds and to processes for their preparation.
    Type: Application
    Filed: March 17, 2015
    Publication date: May 11, 2017
    Applicant: Actelion Pharmaceuticals Ltd.
    Inventors: Hamed AISSAOUI, Christoph BOSS, Patrick BOUIS, Julien HAZEMANN, Romain SIEGRIST
  • Patent number: 9637473
    Abstract: The invention relates to novel acrylamide derivatives of the formula I wherein R1, R2, R3, X, and ring A are as defined in the description, and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including pharmaceutical compositions containing those compounds and their use as medicaments for the treatment or prevention of protozoal infections, such as especially malaria.
    Type: Grant
    Filed: March 14, 2014
    Date of Patent: May 2, 2017
    Assignee: ACTELION PHARMACEUTICALS LTD.
    Inventors: Hamed Aissaoui, Christoph Boss, Claire-Lise Ciana, Thierry Kimmerlin, Romain Siegrist
  • Publication number: 20170107214
    Abstract: The invention relates to compounds of Formula (I) wherein R1, R2, R3, R4 and R5 are as described in the description; to pharmaceutically acceptable salts thereof, and to the use of such compounds as medicaments, especially as modulators of the CXCR3 receptor.
    Type: Application
    Filed: March 23, 2015
    Publication date: April 20, 2017
    Applicant: ACTELION PHARMACEUTICALS LTD
    Inventors: Eva CAROFF, Rémy CASTRO, Emmanuel MEYER, Thierry KIMMERLIN
  • Patent number: 9624206
    Abstract: The invention relates to antibacterial compounds of formula I wherein X is N or CH; R1 is H or halogen; R2 is alkynyloxy or the group M; R3 is H or halogen; M is one of the groups MA and MB represented below wherein A is a bond, CH2CH2, CH?CH or C?C; R1A is H or halogen; R2A is H, alkoxy or halogen; R3A is H, alkoxy, hydroxyalkoxy, alkoxyalkoxy, thioalkoxy, trifluoromethoxy, amino, hydroxyalkyl, 2-hydroxyacetamido, 1-aminocyclopropyl, 1-hydroxymethyl-cycloprop-1-yl, 1-((phosphonooxy)methyl)cyclopropyl, 1-(((dimethylglycyl)oxy)methyl)cyclopropyl, trans-2-hydroxymethyl-cycloprop-1-yl, 1,2-dihydroxyethyl, 3-hydroxyoxetan-3-yl, 3-(hydroxyalkyl)oxetan-3-yl, 3-aminooxetan-3-yl, 3-hydroxythietan-3-yl, morpholin-4-ylalkoxy, morpholin-4-yl-alkyl, oxazol-2-yl or [1,2,3]triazol-2-yl; and R1B is hydroxyalkyl, dihydroxyalkyl, aminoalkyl, 1-hydroxymethyl-cycloprop-1-yl, 1-aminomethyl-cycloprop-1-yl, trans-2-hydroxymethyl-cycloprop-1-yl, 3-hydroxyoxetan-3-yl, 3-hydroxythietan-3-yl, 1-(2-hydroxyacetyl)azetidin-3-yl,
    Type: Grant
    Filed: December 18, 2014
    Date of Patent: April 18, 2017
    Assignee: ACTELION PHARMACEUTICALS LTD
    Inventors: Gaelle Chapoux, Jean-Christophe Gauvin, Christian Hubschwerlen, Azely Mirre, Etienne Ochala, Jean-Luc Specklin, Jean-Philippe Surivet
  • Patent number: 9617250
    Abstract: The invention relates to compounds of the Formula (I), Formula (I) wherein R1 and R2 are as described in the description, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunomodulating agents.
    Type: Grant
    Filed: March 14, 2014
    Date of Patent: April 11, 2017
    Assignee: ACTELION PHARMACEUTICALS LTD.
    Inventors: Martin Bolli, Cyrille Lescop, Oliver Nayler, Beat Steiner
  • Patent number: 9597331
    Abstract: The invention relates to a product containing the compound of formula (I) below or a pharmaceutically acceptable salt of this compound, in combination with at least one compound having prostacyclin receptor (IP) agonist properties, or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: October 2, 2015
    Date of Patent: March 21, 2017
    Assignee: ACTELION PHARMACEUTICALS LTD.
    Inventor: Martine Clozel
  • Publication number: 20170029411
    Abstract: The invention relates to antibacterial compounds of formula I wherein X is N or CH; R1 is H or halogen; R2 is alkynyloxy or the group M; R3 is H or halogen; M is one of the groups MA and MB represented below wherein A is a bond, CH2CH2, CH?CH or C?C; R1A is H or halogen; R2A is H, alkoxy or halogen; R3A is H, alkoxy, hydroxyalkoxy, alkoxyalkoxy, thioalkoxy, trifluoromethoxy, amino, hydroxyalkyl, 2-hydroxyacetamido, 1-aminocyclopropyl, 1-hydroxymethyl-cycloprop-1-yl, 1-((phosphonooxy)methyl)cyclopropyl, 1-(((dimethylglycyl)oxy)methyl)cyclopropyl, trans-2-hydroxymethyl-cycloprop-1-yl, 1,2-dihydroxyethyl, 3-hydroxyoxetan-3-yl, 3-(hydroxyalkyl)oxetan-3-yl, 3-aminooxetan-3-yl, 3-hydroxythietan-3-yl, morpholin-4-ylalkoxy, morpholin-4-yl-alkyl, oxazol-2-yl or [1,2,3]triazol-2-yl; and R1B is hydroxyalkyl, dihydroxyalkyl, aminoalkyl, 1-hydroxymethyl-cycloprop-1-yl, 1-aminomethyl-cycloprop-1-yl, trans-2-hydroxymethyl-cycloprop-1-yl, 3-hydroxyoxetan-3-yl, 3-hydroxythietan-3-yl, 1-(2-hydroxyacetyl)azetidin-3-yl,
    Type: Application
    Filed: December 18, 2014
    Publication date: February 2, 2017
    Applicant: ACTELION PHARMACEUTICALS LTD
    Inventors: Gaelle CHAPOUX, Jean-Christophe GAUVIN, Christian HUBSCHWERLEN, Azely MIRRE, Etienne OCHALA, Jean-Luc SPECKLIN, Jean-Philippe SURIVET
  • Patent number: 9556125
    Abstract: The invention relates to a process for preparing a pyrimidine intermediate, namely the compound of formula I-2 or a salt thereof, which involves the use of a liquid-liquid extraction using methyl iso-butyl ketone. Said compound of formula I-2 or its salt can be used to prepare macitentan.
    Type: Grant
    Filed: July 11, 2014
    Date of Patent: January 31, 2017
    Assignee: ACTELION PHARMACEUTICALS LTD.
    Inventors: Stefan Abele, Jacques-Alexis Funel, Ivan Schindelholz
  • Patent number: 9556117
    Abstract: The invention relates to indole carboxamide derivatives of formula (I), wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 and n are as defined in the description, their preparation and their use as pharmaceutically active compounds.
    Type: Grant
    Filed: December 17, 2013
    Date of Patent: January 31, 2017
    Assignee: ACTELION PHARMACEUTICALS LTD.
    Inventors: Kurt Hilpert, Francis Hubler, Dorte Renneberg, Simon Stamm
  • Patent number: 9540399
    Abstract: The invention relates to antibacterial compounds of formula I wherein R1, U, V and A are as defined in the description, to pharmaceutical compositions containing them and uses of these compounds in the manufacture of medicaments for the treatment of bacterial infections.
    Type: Grant
    Filed: April 30, 2014
    Date of Patent: January 10, 2017
    Assignee: Actelion Pharmaceuticals Ltd.
    Inventors: Stephanie Enderlin-Paput, Christian Hubschwerlen, Georg Rueedi, Cornelia Zumbrunn
  • Patent number: 9533964
    Abstract: The present invention relates to a piperazine substituted bridged spiro[2.4]heptane derivative of formula (I), its preparation and its use as pharmaceutically active compound.
    Type: Grant
    Filed: July 17, 2014
    Date of Patent: January 3, 2017
    Assignee: Actelion Pharmaceuticals Ltd.
    Inventors: Olivier Corminboeuf, Sylvaine Cren, Davide Pozzi
  • Patent number: 9532985
    Abstract: The invention relates to methods of treating, reducing the symptoms of, or preventing a post-traumatic stress syndrome by administration of tetrahydroquinoline derivatives of formula I wherein R1 and R2 each independently represent (C1-C4)alkoxy, R3 represents aryl-(C1-C4)alkyl or heteroaryl-(C1-C4)alkyl, and R4 represents hydrogen or (C1-C4)alkyl, or pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: October 9, 2008
    Date of Patent: January 3, 2017
    Assignee: ACTELION PHARMACEUTICALS LTD.
    Inventor: Francois Jenck
  • Patent number: 9527867
    Abstract: The invention relates to antibacterial compounds of formula I and salts thereof and methods of treating bacterial infection using the compounds.
    Type: Grant
    Filed: April 15, 2014
    Date of Patent: December 27, 2016
    Assignee: Actelion Pharmaceuticals Ltd.
    Inventors: Sylvaine Cren, Astrid Friedli, Christian Hubschwerlen, Georg Rueedi, Cornelia Zumbrunn
  • Patent number: 9505750
    Abstract: The invention relates to antibacterial compounds of formula I wherein one or two of U, V, W, and X represent N, the rest represent CH or, in the case of X, may also represent CRa wherein Ra is fluorine; R1 represents alkoxy, halogen or cyano; R2 represents H, CH2OH, CH2N3, CH2NH2, alkylcarbonylaminomethyl or triazol-1-ylmethyl; R3 represents H, or, when n is 1, R3 may also represent OH, NH2, NHCOR6 or triazol-1-yl; A represents CR4; K represents O, NH, OCH2, NHCO, NHCH2, CH2NH, CH2CH2, CH?CH, CHOHCHOH or CHR5; R4 represents H or together with R5 forms a bond, or also R4 can represent OH when K is not O, NH, OCH2 or NHCO; R5 represents OH or together with R4 forms a bond; R6 represents alkyl; m is 0 or 1 and n is 0 or 1; and G is as defined in the description; and to salts of such compounds.
    Type: Grant
    Filed: December 17, 2008
    Date of Patent: November 29, 2016
    Assignee: ACTELION PHARMACEUTICALS LTD.
    Inventors: Christian Hubschwerlen, Georg Rueedi, Jean-Philippe Surivet, Cornelia Zumbrunn Acklin
  • Patent number: 9493446
    Abstract: The present invention relates to [ortho bi-(hetero-)aryl]-[2-(meta bi-(hetero-)aryl)-pyrrolidin-1-yl]-methanone derivatives of formula (I) wherein R, and the rings A1 A2 and A3 are as described in the description, to pharmaceutically acceptable salts thereof, to their preparation, to pharmaceutical compositions containing one or more compounds of formula (I), and to their use as pharmaceuticals, especially to their use as orexin receptor antagonists.
    Type: Grant
    Filed: October 9, 2013
    Date of Patent: November 15, 2016
    Assignee: ACTELION PHARMACEUTICALS LTD.
    Inventors: Martin Bolli, Christoph Boss, Christine Brotschi, Markus Gude, Bibia Heidmann, Thierry Sifferlen, Jodi T. Williams
  • Patent number: 9487516
    Abstract: 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.
    Type: Grant
    Filed: January 8, 2014
    Date of Patent: November 8, 2016
    Assignee: Actelion Pharmaceuticals, Ltd.
    Inventors: Christian Hubschwerlen, Georg Rueedi, Cornelia Zumbrunn
  • Publication number: 20160318879
    Abstract: The present invention relates to a new synthetic 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 the compound of formula I-3 which is an important synthetic intermediate used in the preparation of macitentan.
    Type: Application
    Filed: July 14, 2016
    Publication date: November 3, 2016
    Applicant: ACTELION PHARMACEUTICALS LTD.
    Inventors: Stefan ABELE, Jacques-Alexis FUNEL, Ivan SCHINDELHOLZ
  • Patent number: 9428456
    Abstract: The present invention relates to 1-[m-carboxamido(hetero)aryl-methyl]-heterocycyl-carboxamide compounds of formula (I) wherein X, Ar1, R1, R2, R3, R4, R5a, R5b and p 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), and especially to their use as CXCR7 receptor modulators.
    Type: Grant
    Filed: June 21, 2013
    Date of Patent: August 30, 2016
    Assignee: ACTELION PHARMACEUTICALS LTD
    Inventors: Heinz Fretz, Markus Gude, Philippe Guerry, Thierry Kimmerlin, Francois Lehembre, Thomas Pfeifer, Anja Valdenaire
  • Patent number: 9422249
    Abstract: The present invention relates to a new synthetic 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 the compound of formula I-3 which is an important synthetic intermediate used in the preparation of macitentan.
    Type: Grant
    Filed: March 26, 2014
    Date of Patent: August 23, 2016
    Assignee: ACTELION PHARMACEUTICALS LTD.
    Inventors: Stefan Abele, Jacques-Alexis Funel, Ivan Schindelholz
  • Patent number: 9409917
    Abstract: The invention relates to heterocyclic amide derivatives of formula (I), wherein R1, R2, R3, X and n are as defined in the description, their preparation and their use as pharmaceutically active compounds.
    Type: Grant
    Filed: January 18, 2013
    Date of Patent: August 9, 2016
    Assignee: ACTELION PHARMACEUTICALS LTD.
    Inventors: Kurt Hilpert, Francis Hubler, Thierry Kimmerlin, Dorte Renneberg, Simon Stamm