Patents Assigned to Actelion Pharmaceuticals
  • NADPH oxidase 4 inhibitors
    Patent number: 10584118
    Abstract: The invention relates to 2,5-disubstituted benzoxazole and benzothiazole derivatives of Formula (I) wherein L, X, Y, and ring (A) are as described in the description, their preparation and their use as pharmaceutically active compounds. Said compounds may be useful for the prevention or treatment of diseases or disorders associated with impaired reactive oxygen species (ROS) production, and/or for the prevention or treatment of various fibrotic diseases.
    Type: Grant
    Filed: June 21, 2016
    Date of Patent: March 10, 2020
    Assignee: ACTELION PHARMACEUTICALS LTD
    Inventors: Hamed Aissaoui, Martin Bolli, Christoph Boss, Sylvia Richard-Bildstein, Patrick Sieber
  • PHARMACEUTICAL COMBINATION COMPRISING A SELECTIVE S1P1 RECEPTOR AGONIST
    Publication number: 20190175563
    Abstract: The present invention relates to a pharmaceutical combination comprising a first active ingredient which is (R)-5-[3-chloro-4-(2,3-dihydroxy-propoxy)-benz[Z]ylidene]-2-([Z]propylimino)-3-o-tolyl-thiazolidin-4-one or a pharmaceutically acceptable salt thereof and a second active ingredient which is selected from the group consisting of methyl fumarate, dimethyl fumarate, (N,N-diethylcarbamoyl)methyl methyl (2E)but-2-ene-1,4-dioate, and 2-(2,5-dioxopyrrolidin-1-yl)ethyl methyl (2E)but-2-ene-1,4-dioate, or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: February 15, 2019
    Publication date: June 13, 2019
    Applicant: ACTELION PHARMACEUTICALS LTD
    Inventors: Martine CLOZEL, Luca PIALI
  • DOSING REGIMEN FOR A SELECTIVE S1P1 RECEPTOR AGONIST
    Publication number: 20190151292
    Abstract: The present invention relates to a dosing regimen for (R)-5-[3-chloro-4-(2,3-dihydroxy-propoxy)-benz[Z]ylidene]-2-([Z]-propylimino)-3-o-tolyl-thiazolidin-4-one.
    Type: Application
    Filed: January 29, 2019
    Publication date: May 23, 2019
    Applicant: ACTELION PHARMACEUTICALS LTD
    Inventors: Jasper DINGEMANSE, Matthias HOCH, Andres KRAUSE
  • Dosing regimen for a selective S1Preceptor agonist
    Patent number: 10251867
    Abstract: The present invention relates to a dosing regimen for a selective S1P1 receptor agonist, whereby the selective S1P1 receptor agonist is administered to a subject in such a way that during the initial treatment phase the selective S1P1 receptor agonist is administered at a dose which induces desensitization of the heart wherein said dose is below the target dose, and at a dosing frequency that sustains desensitization of the heart, until no further acute heart rate reduction occurs, followed by dose up-titration to the target dose of the selective S1P1 receptor agonist.
    Type: Grant
    Filed: June 5, 2015
    Date of Patent: April 9, 2019
    Assignee: ACTELION PHARMACEUTICALS LTD.
    Inventors: Patrick Brossard, Jasper Dingemanse, Oliver Nayler, Michael Scherz, Beat Steiner
  • Pharmaceutical combination comprising a selective S1P1 receptor agonist
    Patent number: 10245253
    Abstract: The present invention relates to a pharmaceutical combination comprising a first active ingredient which is (R)-5-[3-chloro-4-(2,3-dihydroxy-propoxy)-benz[Z]ylidene]-2-([Z]propylimino)-3-o-tolyl-thiazolidin-4-one or a pharmaceutically acceptable salt thereof and a second active ingredient which is selected from the group consisting of methyl fumarate, dimethyl fumarate, (N,N-diethylcarbamoyl)methyl methyl (2E)but-2-ene-1,4-dioate, and 2-(2,5-dioxopyrrolidin-1-yl)ethyl methyl (2E)but-2-ene-1,4-dioate, or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: December 10, 2015
    Date of Patent: April 2, 2019
    Assignee: ACTELION PHARMACEUTICALS LTD
    Inventors: Martine Clozel, Luca Piali
  • Dosing regimen for a selective S1Preceptor agonist
    Patent number: 10220023
    Abstract: The present invention relates to a dosing regimen for (R)-5-[3-chloro-4-(2,3-dihydroxy-propoxy)-benz[Z]ylidene]-2-([Z]-propylimino)-3-o-tolyl-thiazolidin-4-one.
    Type: Grant
    Filed: December 10, 2015
    Date of Patent: March 5, 2019
    Assignee: ACTELION PHARMACEUTICALS LTD
    Inventors: Jasper Dingemanse, Matthias Hoch, Andreas Krause
  • Tricyclic imidazole compounds as inhibitors of tryptophan hydroxylase
    Patent number: 10189839
    Abstract: The present invention relates to compounds of the formula (I) wherein 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.
    Type: Grant
    Filed: November 18, 2014
    Date of Patent: January 29, 2019
    Assignee: ACTELION PHARMACEUTICALS LTD
    Inventors: Daniel Bur, Corinna Grisostomi, Oliver Nayler, Lubos Remen, Magali Vercauteren, Richard Welford
  • Stable pharmaceutical compositions comprising a pyrimidine-sulfamide
    Patent number: 10117870
    Abstract: The invention relates to stable pharmaceutical compositions comprising the compound of the below formula, or pharmaceutically acceptable salts, solvates, hydrates or morphological forms thereof.
    Type: Grant
    Filed: January 20, 2016
    Date of Patent: November 6, 2018
    Assignee: ACTELION PHARMACEUTICALS LTD.
    Inventors: Charles Tokunbo Adesuyi, Bruce Hamilton Lithgow, Olivier Lambert, Lovelace Holman
  • STABLE PHARMACEUTICAL COMPOSITIONS COMPRISING A PYRIMIDINE-SULFAMIDE
    Publication number: 20180263980
    Abstract: The invention relates to stable pharmaceutical compositions comprising the compound of the below formula, or pharmaceutically acceptable salts, solvates, hydrates or morphological forms thereof
    Type: Application
    Filed: February 20, 2018
    Publication date: September 20, 2018
    Applicant: ACTELION PHARMACEUTICALS LTD.
    Inventors: Charles Tokunbo Adesuyi, Bruce Hamilton Lithgow, Olivier Lambert, Lovelace Holman
  • TRIAZOLE COMPOUNDS AS T-TYPE CALCIUM CHANNEL BLOCKERS
    Publication number: 20180230109
    Abstract: The invention relates to compounds of formula (I) wherein X, Y, R1, R2, (R4)n, and (R5)m are as defined in the description, and to pharmaceutically acceptable salts of such compounds. These compounds are useful as calcium T-channel blockers.
    Type: Application
    Filed: September 14, 2015
    Publication date: August 16, 2018
    Applicant: ACTELION PHARMACEUTICALS LTD
    Inventors: Olivier BEZENCON, John GATFIELD, Bibia HEIDMANN, Romain SIEGRIST, Simon STAMM
  • NADPH OXIDASE 4 INHIBITORS
    Publication number: 20180179194
    Abstract: The invention relates to 2,5-disubstituted benzoxazole and benzothiazole derivatives of Formula (I) wherein L, X, Y, and ring (A) are as described in the description, their preparation and their use as pharmaceutically active compounds. Said compounds may be useful for the prevention or treatment of diseases or disorders associated with impaired reactive oxygen species (ROS) production, and/or for the prevention or treatment of various fibrotic diseases.
    Type: Application
    Filed: June 21, 2016
    Publication date: June 28, 2018
    Applicant: ACTELION PHARMACEUTICALS LTD
    Inventors: Hamed AISSAOUI, Martin BOLLI, Christoph BOSS, Sylvia RICHARD-BILDSTEIN, Patrick SIEBER
  • TRICYCLIC PIPERIDINE COMPOUNDS
    Publication number: 20180155344
    Abstract: The present invention relates to compounds of the formula (I) wherein R1a, R1b, R2, R3, (R4)n and ring (A) 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.
    Type: Application
    Filed: May 3, 2016
    Publication date: June 7, 2018
    Applicant: ACTELION PHARMACEUTICALS LTD
    Inventors: Daniel BUR, Corinna GRISOSTOMI, Thierry KIMMERLIN, Lubos REMEN, Hervé SIENDT, Magali VERCAUTEREN, Richard WELFORD
  • DOSING REGIMEN FOR A SELECTIVE S1P1 RECEPTOR AGONIST
    Publication number: 20180147188
    Abstract: The present invention relates to a dosing regimen for (R)-5-[3-chloro-4-(2,3-dihydroxy-propoxy)-benz[Z]ylidene]-2-([Z]-propylimino)-3-o-tolyl-thiazolidin-4-one.
    Type: Application
    Filed: December 10, 2015
    Publication date: May 31, 2018
    Applicant: ACTELION PHARMACEUTICALS LTD
    Inventors: Jasper DINGEMANSE, Matthias HOCH, Andreas KRAUSE
  • CRYSTALLINE SALT FORM OF (S)-(2-(6-CHLORO-7-METHYL-1H-BENZO[D]IMIDAZOL-2-YL)-2-METHYLPYRROLIDIN-1-YL)(5-METHOXY-2-(2H-1,2,3-TRIAZOL-2-YL)PHENYL)METHANONE AS OREXIN RECEPTOR ANTAGONIST
    Publication number: 20180002317
    Abstract: The invention relates to a crystalline form of (S)-(2-(6-chloro-7-methyl-1H-benzo[d]imidazol-2-yl)-2-methylpyrrolidin-1-yl)(5-methoxy-2-(2H-1,2,3-triazol-2-yl)phenyl)methanone hydrochloride, processes for the preparation thereof, pharmaceutical compositions containing said crystalline form, and its use as medicament, especially as orexin receptor antagonist.
    Type: Application
    Filed: September 12, 2017
    Publication date: January 4, 2018
    Applicant: ACTELION PHARMACEUTICALS LTD
    Inventors: Christoph BOSS, Christine BROTSCHI, Markus GUDE, Bibia HEIDMANN, Thierry SIFFERLEN, Markus VON RAUMER, Jodi T. WILLIAMS
  • PHARMACEUTICAL COMBINATION COMPRISING A SELECTIVE S1P1 RECEPTOR AGONIST
    Publication number: 20170348287
    Abstract: The present invention relates to a pharmaceutical combination comprising a first active ingredient which is (R)-5-[3-chloro-4-(2,3-dihydroxy-propoxy)-benz[Z]ylidene]-2-([Z]propylimino)-3-o-tolyl-thiazolidin-4-one or a pharmaceutically acceptable salt thereof and a second active ingredient which is selected from the group consisting of methyl fumarate, dimethyl fumarate, (N,N-diethylcarbamoyl)methyl methyl (2E)but-2-ene-1,4-dioate, and 2-(2,5-dioxopyrrolidin-1-yl)ethyl methyl (2E)but-2-ene-1,4-dioate, or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: December 10, 2015
    Publication date: December 7, 2017
    Applicant: ACTELION PHARMACEUTICALS LTD
    Inventors: Martine CLOZEL, Luca PIALI
  • DOSING REGIMEN FOR A SELECTIVE S1P1 RECEPTOR AGONIST
    Publication number: 20170319555
    Abstract: The present invention relates to a dosing regimen for (R)-5-[3-chloro-4-(2,3-dihydroxy-propoxy)-benz[Z]ylidene]-2-([Z]-propylimino)-3-o-tolyl-thiazolidin-4-one.
    Type: Application
    Filed: December 10, 2015
    Publication date: November 9, 2017
    Applicant: ACTELION PHARMACEUTICALS LTD
    Inventors: Jasper DINGEMANSE, Matthias HOCH, Andreas KRAUSE
  • Tricyclic piperidine compounds
    Patent number: 9765092
    Abstract: The present invention relates to compounds of the formula (I) 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.
    Type: Grant
    Filed: November 18, 2014
    Date of Patent: September 19, 2017
    Assignee: ACTELION PHARMACEUTICALS LTD
    Inventors: Daniel Bur, Corinna Grisostomi, Oliver Nayler, Lubos Remen, Magali Vercauteren, Richard Welford
  • Preparation of pyrimidine intermediates useful for the manufacture of macitentan
    Patent number: 9676731
    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: July 14, 2016
    Date of Patent: June 13, 2017
    Assignee: ACTELION PHARMACEUTICALS LTD.
    Inventors: Stefan Abele, Jacques-Alexis Funel, Ivan Schindelholz
  • Difluoroethyl-oxazole substituted bridged spiro[2.4]heptane derivatives as ALX receptor agonists
    Patent number: 9676761
    Abstract: The present invention relates to difluoroethyl-oxazole substituted bridged spiro[2.4] heptane derivatives of formula (I), wherein the substituents at the piperidine ring are in trans-arrangement, their preparation and their use as pharmaceutically active compounds.
    Type: Grant
    Filed: June 24, 2014
    Date of Patent: June 13, 2017
    Assignee: ACTELION PHARMACEUTICALS, LTD.
    Inventors: Olivier Corminboeuf, Sylvaine Cren, Davide Pozzi
  • Benzimidazolyl-methyl urea derivatives as ALX receptor agonists
    Patent number: 9663473
    Abstract: The present invention relates to benzimidazolyl-methyl urea derivatives of formula (I), wherein n, D, E, R1, R2, R3, R4, R6, R7, R8 and R9 are as defined in the description, their preparation and their use as pharmaceutically active compounds.
    Type: Grant
    Filed: August 8, 2014
    Date of Patent: May 30, 2017
    Assignee: ACTELION PHARMACEUTICALS LTD.
    Inventors: Olivier Corminboeuf, Sylvaine Cren, Xavier Leroy, Davide Pozzi