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:
Application
Filed:
December 17, 2013
Publication date:
December 3, 2015
Applicant:
ACTELION PHARMACEUTICALS LTD
Inventors:
KURT HILPERT, FRANCIS HUBLER, DORTE RENNEBERG, SIMON STAMM
Abstract: The invention relates to a method for preparing linear polymers having an amide end or having a star architecture comprising an amide core, by means of a ring opening using lactide and glycolide monomers or a lactide monomer ring in the presence of a catalyst, wherein the method includes the steps of: (i) reacting the excess monomer(s) with an initiator in a solvent, said initiator being selected from among an amine and an amino alcohol, given that the initiator has at least one primary or secondary amine function; (ii) adding a catalyst, said catalyst being a non-nucleophilic base and including at least one neutral sp2 nitrogen atom; and (iii) neutralizing the reaction mixture. Said novel method is particularly advantageous in that it can be easily monitored and enables better modulation of the polymers, and thus of the properties thereof, than the methods of the prior art. The invention also relates to novel polymers that are obtainable by means of said method.
Abstract: The invention relates to a new process suitable for manufacturing the compounds of formula I (I) wherein W is H, Br, Cl or methyl, which are synthetic intermediates useful in the preparation of antibiotic compounds.
Type:
Grant
Filed:
April 26, 2013
Date of Patent:
November 17, 2015
Assignee:
Actelion Pharmaceuticals Ltd.
Inventors:
Stefan Abele, Hans Meier, Gunther Schmidt, Heinz Steiner
Abstract: The invention relates to indole carboxamide derivatives of formula (I), wherein R1, R2, R3, R4, R5 and R6 are as defined in the description, their preparation and their use as pharmaceutically active compounds.
Type:
Application
Filed:
December 11, 2013
Publication date:
November 12, 2015
Applicant:
ACTELION PHARMACEUTICALS LTD
Inventors:
KURT HILPERT, FRANCIS HUBLER, THIERRY KIMMERLIN, DORTE RENNEBERG, SIMON STAMM
Abstract: The invention relates to a product containing the compound of formula (I) below or a pharmaceutically acceptable salt of this compound, in combination of at least one compound having prostacyclin receptor (IP) agonist properties, or a pharmaceutically acceptable salt thereof.
Abstract: The present invention relates to 1-phenyl-substituted heterocyclyl derivatives of the formula (I), wherein Y, Z, R1, R2, R3 and R4 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:
Grant
Filed:
July 4, 2013
Date of Patent:
October 27, 2015
Assignee:
Actelion Pharmaceuticals Ltd.
Inventors:
Hamed Aissaoui, Christoph Boss, Sylvia Richard-Bildstein, Romain Siegrist
Abstract: The present invention relates to 2-(1,2,3-triazol-2-yl)benzamide and 3-(1,2,3-triazol-2-yl)picolinamide derivatives of formula (I) wherein Ar1, Q, and R1 to R5 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 orexin receptor antagonists.
Type:
Grant
Filed:
November 7, 2012
Date of Patent:
October 6, 2015
Assignee:
ACTELION PHARMACEUTICALS LTD.
Inventors:
Martin Bolli, Christoph Boss, Christine Brotschi, Bibia Heidmann, Thierry Sifferlen, Jodi T. Williams
Abstract: The present invention relates to fluorinated bridged spiro[2.4]heptane derivatives of formula (I), wherein n and R1 are as defined in the description, their preparation and their use as pharmaceutically active compounds.
Abstract: The invention relates to pyridine derivatives of Formula (I) wherein A, R1, R2, R3, and R4 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:
January 18, 2012
Date of Patent:
September 15, 2015
Assignee:
Actelion Pharmaceuticals Ltd.
Inventors:
Martin Bolli, Cyrille Lescop, Boris Mathys, Keith Morrison, Claus Mueller, Oliver Nayler, Beat Steiner
Abstract: The invention relates to a process and synthetic intermediates that can be used for manufacturing the compound of formula (1-6) which is a synthetic intermediate useful in the preparation of antibiotic compounds.
Abstract: The present invention relates to 7-(heteroaryl-amino)-6,7,8,9-tetrahydropyrido[1,2-a]indol acetic acid derivatives of the formula (I), wherein R1, R2, R3 and R4 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.
Abstract: The present invention relates to a new process for the preparation of (2Z,5Z)-5-(3-chloro-4-((R)-2,3-dihydroxypropoxy)benzylidene)-2-(propylimino)-3-(o-tolyl)thiazolidin-4-one and to the new intermediate (R)-3-chloro-4-(2,3-dihydroxypropoxy)-benzaldehyde used in this process. (2Z,5Z)-5-(3-Chloro-4-((R)-2,3-dihydroxypropoxy)benzylidene)-2-(propylimino)-3-(o-tolyl)thiazolidin-4-one is described in WO 2005/054215 to act as an immunosuppressive agent. The present invention further also relates to a new process for the preparation of (R)-3-chloro-4-(2,3-dihydroxypropoxy)-benzaldehyde.
Abstract: The invention relates to antibacterial compounds of formula I wherein R1a represents H or carboxy and R1b represents H, or R1a and R1b represent together either the group *—C(O)—NH—S—# or the group *—C(OH)?N—S—# wherein “*” represents the point of attachment of R1a and “#” represents the point of attachment of R1b; R2 represents H, (C1-C3)alkyl, hydroxy-(C1-C3)alkyl, benzyl or (C3-C5)cycloalkyl; R3 represents H or halogen; U represents N or CR4; wherein R4 is H or (C1-C3)alkoxy; A represents CH, B represents NH and m represents 1 or 2 and n represents 1 or 2; or A represents N, B is absent, m represents 2 and n represents 2; Y represents CH or N; and Q represents O or S; and salts of such compounds.
Type:
Grant
Filed:
November 7, 2012
Date of Patent:
July 14, 2015
Assignee:
Actelion Pharmaceuticals Ltd
Inventors:
Christian Hubschwerlen, Georg Rueedi, Jean-Philippe Surivet, Cornelia Zumbrunn Acklin
Abstract: The invention relates to crystalline forms of (R)-5-[3-chloro-4-(2,3-dihydroxy-propoxy)-benz[Z]ylidene]-2-([Z]-propylimino)-3-o-tolyl-thiazolidin-4-one, processes for the preparation thereof, pharmaceutical compositions containing said crystalline forms, and their use as compounds improving vascular function and as immunomodulating agents, either alone or in combination with other active compounds or therapies.
Type:
Grant
Filed:
October 19, 2009
Date of Patent:
June 23, 2015
Assignee:
ACTELION PHARMACEUTICALS LTD.
Inventors:
Nicholas Bonham, Stephan Buchmann, Alex Eberlin, Christoph Imboden, Markus Von Raumer
Abstract: The present invention relates to compounds of the formula (I) wherein Ar1, R1, R2, R3, R4a, R4b and (R5)n 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 orexin receptor antagonists.
Type:
Application
Filed:
June 3, 2013
Publication date:
June 18, 2015
Applicant:
ACTELION PHARMACEUTICALS LTD
Inventors:
Christoph Boss, Christine Brotschi, Markus Gude, Bibia Heidmann, Thierry Sifferlen, Jodi Williams
Abstract: The invention relates to the identification of Neuropeptide Q as ligand of the GALR2 GPCR (G-protein coupled receptor). The invention encompasses the use of the interaction of GALR2 polypeptides and Neuropeptide Q polypeptides as the basis of screening assays for agents that modulate the activity of the GALR2 receptor. The invention also encompasses diagnostic assays based upon the GALR2/Neuropeptide Q polypeptide interaction, as well as kits for performing diagnostic and screening assays.
Abstract: The present invention relates to 2-(1,2,3-triazol-2-yl)benzamide and 3-(1,2,3-triazol-2-yl)picolinamide derivatives of formula (I) wherein Ar1, Q, and R1 to R5 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 orexin receptor antagonists.
Type:
Application
Filed:
November 7, 2012
Publication date:
June 11, 2015
Applicant:
ACTELION PHARMACEUTICALS LTD.
Inventors:
Martin Bolli, Christoph Boss, Christine Brotschi, Bibia Heidmann, Thierry Sifferlen, Jodi T. Williams
Abstract: The present invention relates to 1-phenyl-substituted heterocyclyl derivatives of the formula (I), wherein Y, Z, R1, R2, R3 and R4 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:
July 4, 2013
Publication date:
June 11, 2015
Applicant:
Actelion Pharmaceutical Ltd.
Inventors:
Hamed Aissaoui, Christoph Boss, Sylvia Richard-Bildstein, Romain Siegrist
Abstract: The present invention relates to new processes for the preparation of 2-cyclopentyl-6-methoxy-isonicotinic acid, which is a useful intermediate for the synthesis of pyridine-4-yl derivatives as immunomodulating agent. Moreover, the present invention also relates to new intermediates used in those processes.
Abstract: The invention relates to antibacterial compounds of formula I wherein G and K are as defined in the description; and salts of such compounds.
Type:
Grant
Filed:
November 29, 2012
Date of Patent:
May 12, 2015
Assignee:
Actelion Pharmaceuticals Ltd.
Inventors:
Christian Hubschwerlen, Georg Rueedi, Jean-Philippe Surivet, Cornelia Zumbrunn Acklin