Abstract: The invention relates to novel bicyclononene derivatives of Formula (I); and the use thereof 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 inhibitors of renin.
Type:
Grant
Filed:
August 22, 2005
Date of Patent:
March 20, 2012
Assignee:
Actelion Pharmaceuticals Ltd.
Inventors:
Olivier Bezencon, Christoph Boss, Daniel Bur, Olivier Corminboeuf, Walter Fiśchli, Corinna Grisostomi, Lubos Remen, Sylvia Richard-Bildstein, Thierry Sifferlen, Thomas Weller
Abstract: 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 ant
Type:
Grant
Filed:
November 29, 2007
Date of Patent:
March 13, 2012
Assignee:
Actelion Pharmaceuticals Ltd.
Inventors:
Hamed Aissaoui, Christoph Boss, Markus Gude, Ralf Koberstein, Thierry Sifferlen
Abstract: The invention relates to novel thiophene derivatives, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunomodulating agents.
Type:
Grant
Filed:
July 10, 2007
Date of Patent:
March 13, 2012
Assignee:
Actelion Pharmaceuticals Ltd.
Inventors:
Martin Bolli, David Lehmann, Boris Mathys, Claus Mueller, Oliver Nayler, Beat Steiner, Jörg Velker
Abstract: The invention provides 3(R)-(2-hydroxy-2,2-dithien-2-ylacetoxy)-1-(3-phenoxypropyl)-1-azoniabicyclo[2.2.2]octane bromide in powder inhalant form, and methods of using it for treatment of respiratory disorders.
Type:
Grant
Filed:
January 21, 2011
Date of Patent:
March 6, 2012
Assignee:
Almirall Prodesfarma S.A.
Inventors:
Maria Dolors Fernandez Forner, Maria Prat Quiñones, María Antonia Buil Albero
Abstract: The invention relates to 3-aza-bicyclo[3.3.0]octane derivatives of the formula (I) wherein R1, R2, R3, and A are as described in the description and their use as orexin receptor antagonists.
Type:
Grant
Filed:
July 2, 2008
Date of Patent:
January 31, 2012
Assignee:
Actelion Pharmaceuticals Ltd.
Inventors:
Hamed Aissaoui, Christoph Boss, Markus Gude, Ralf Koberstein, Thierry Sifferlen
Abstract: The present invention relates to a method of isolating fragments of nucleic acid according to the density of CpG dinucleotides and subsequent procedures for producing a library and/or an array or microarray of these fragments, as well as uses thereof.
Type:
Grant
Filed:
October 31, 2005
Date of Patent:
January 31, 2012
Assignee:
The University Court of the University of Edinburgh
Inventors:
Adrian Peter Bird, Robert Scott Illingworth, Helle Faerk Jorgensen
Abstract: The invention provides a new reproducible transgenic mouse model for the study of iron accumulation in the body. In particular, the invention concerns the study of iron overload in an RGMc knockout mouse model and its use in drug discovery and research.
Type:
Grant
Filed:
July 22, 2005
Date of Patent:
January 24, 2012
Assignee:
Novartis Forschungsstiftung, Zweigniederalassung Friedrich Miescher Institute for Biomedical Research
Abstract: The present invention relates to 2-aminocarbonyl-pyridine derivatives of Formula (I) and their use as P2Y12 receptor antagonists in the treatment and/or prevention of peripheral vascular, of visceral-, hepatic- and renal-vascular, of cardiovascular and of cerebrovascular diseases or conditions associated with platelet aggregation, including thrombosis.
Type:
Grant
Filed:
October 12, 2007
Date of Patent:
January 10, 2012
Assignee:
Actelion Pharmaceuticals Ltd.
Inventors:
Eva Caroff, Kurt Hilpert, Emmanuel Meyers
Abstract: The present invention provides novel piperidine derivatives of formula (I), wherein R represents a substituted benzyl group, which are useful as inhibitors of glucosylceramide synthase (GCS). The compounds of the Invention are useful for treating various glycolipid storage diseases, such as Gaucher's disease, Sandhoff's disease, Tay-Schs disease, Fabry disease, and GM1 gangliosidosis; glycolipid accumulation disorders, such as Niemann-Pick disease, mucopolysaccharidoses, mucolipidosis type IV and ?-mannosidosis; various cancers that involve abnormal glycolipid synthesis; and various infectious diseases that involve cell surface glycolipids as receptors for the infectious organisms or for their toxins; as well as a variety of other disorders involving glycolipid synthesis, including neuronal disorders, inflammatory diseases, obesity, and the like.
Abstract: The invention relates to novel piperazine derivatives and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including pharmaceutical compositions containing one or more of those compounds and their use as medicaments for the treatment or prevention of protozoal infections, especially malaria.
Type:
Grant
Filed:
October 20, 2006
Date of Patent:
November 29, 2011
Assignee:
Actelion Pharmaceuticals Ltd.
Inventors:
Christoph Binkert, Christoph Boss, Olivier Corminboeuf, Corinna Grisostomi, Solange Meyer
Abstract: The invention relates to novel trans-3-aza-bicyclo[3.1.0]hexane derivatives of formula (I), wherein A, B, n and R1 are as described in the description, and to the use of such compounds, or of pharmaceutically acceptable salts of such compounds, as medicaments, especially as orexin receptor antagonists.
Type:
Grant
Filed:
July 25, 2008
Date of Patent:
November 22, 2011
Assignee:
Actelion Pharmaceuticals Ltd.
Inventors:
Hamed Aissaoui, Christoph Boss, Markus Gude, Ralf Koberstein, David Lehman, Thierry Sifferlen, Daniel Trachsel
Abstract: The present invention relates to compounds of formula I wherein R1, R2, R4, R5, Ra, Rb, n, W and Z are as defined in the application, their preparation and their use as P2Y12 receptor antagonists in the treatment and/or prevention of peripheral vascular, of visceral-, hepatic- and renal-vascular, of cardiovascular and of cerebrovascular diseases or conditions associated with platelet aggregation, including thrombosis in humans and other mammals.
Type:
Grant
Filed:
April 9, 2009
Date of Patent:
November 15, 2011
Assignee:
Actelion Pharmaceuticals Ltd
Inventors:
Eva Caroff, Kurt Hilpert, Francis Hubler, Emmanuel Meyer, Dorte Renneberg
Abstract: The invention relates to 4-aminocarbonyl-pyrimidine derivatives and their use as P2Y12 receptor antagonists in the treatment and/or prevention and/or treatment of peripheral vascular, of visceral-, hepatic- and renal-vascular, of cardiovascular and of cerebrovascular diseases or conditions associated with platelet aggregation, including thrombosis in humans and other mammals.
Type:
Grant
Filed:
April 27, 2006
Date of Patent:
November 1, 2011
Assignee:
Actelion Pharmaceuticals Ltd.
Inventors:
Eva Caroff, Heinz Fretz, Kurt Hilpert, Olivier Houille, Francis Hubler, Emmanuel Meyer
Abstract: The invention relates to 2-phenyl-6-aminocarbonyl-pyrimidine derivatives and their use as P2Y12 receptor antagonists in the treatment and/or prevention and/or treatment of peripheral vascular, of visceral-, hepatic- and renal-vascular, of cardiovascular and of cerebrovascular diseases or conditions associated with platelet aggregation, including thrombosis in humans and other mammals. Formula (I).
Type:
Grant
Filed:
October 24, 2007
Date of Patent:
October 25, 2011
Assignee:
Actelion Pharmaceuticals Ltd.
Inventors:
Eva Caroff, Kurt Hilpert, Emmanuel Meyer
Abstract: The invention relates to phenyl derivatives of formula (I), their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunomodulating agents.
Type:
Grant
Filed:
July 10, 2007
Date of Patent:
October 25, 2011
Assignee:
Actelion Pharmaceuticals Ltd.
Inventors:
Martin Bolli, David Lehmann, Boris Mathys, Claus Mueller, Oliver Nayler, Beat Steiner, Jorg Velker
Abstract: The invention relates to novel thiophene derivatives, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunosuppressive agents.
Type:
Grant
Filed:
March 29, 2010
Date of Patent:
October 18, 2011
Assignee:
Actelion Pharmaceuticals Ltd.
Inventors:
Martin Bolli, David Lehmann, Boris Mathys, Claus Mueller, Oliver Nayler, Jorg Velker, Thomas Weller
Abstract: The present invention relates to the compound 3,4,5-piperidinetriol, 2-(hydroxymethyl)-1-[(4-(pentyloxy)phenyl)methyl]-, (2S,3S,4R,5S), or a pharmaceutically acceptable salt or prodrug thereof, which is useful as an inhibitor of glucosylceramide synthase. The compounds of the Invention are useful for treating various glycolipid storage diseases, such as Gaucher's disease, Sandhoff's disease, Tay-Sacs disease, Fabry disease, and GM1 gangliosidosis; glycolipid accumulation disorders, such as Niemann-Pick disease, mucopolysaccharidoses, mucolipidosis type IV and ?-mannosidosis; various cancers that involve abnormal glycolipid synthesis; and various infectious diseases that involve cell surface glycolipids as receptors for the infectious organisms or for their toxins; as well as a variety of other disorders involving glycolipid synthesis, including neuronal disorders, inflammatory diseases, obesity, and the like.
Type:
Grant
Filed:
June 9, 2004
Date of Patent:
September 20, 2011
Assignee:
Actelion Pharmaceuticals Ltd.
Inventors:
Michael Glen Orchard, David Ian Carter Scopes
Abstract: The FNIII13 domain of fibronectin and smaller fragments thereof have a tumour cell proliferation inhibitory effect. Compositions are provided comprising fragments of fibronectin having the FNIII 13 domain and fragments thereof. A system comprising cells exposed to fibronectin and caused to proliferate by the presence of tenascin are used as an in vitro method for screening possible anti-tumour agents. Cell-free systems comprising a fibronectin ligand and tenascin are also employed for screening potential anti-tumour or anti-cancer agents. Test compounds are assayed for the ability to disrupt binding of the fibronectin ligand to tenascin. A further cell-free system additionally includes a syndecan molecule.
Type:
Grant
Filed:
September 18, 2006
Date of Patent:
September 13, 2011
Assignee:
Novartis Forschungesstiftung Zweigniederlassung Friedrich Miescher Institute for Biomedical Research
Abstract: The present invention relates to the phosphorylated form of nuclear serine/threonine protein kinase, designated nuclear, Dbf2-related kinase (Ndr), and provides assays and materials for identifying modulators thereof. The invention relates to the fields of molecular biology, chemistry, pharmacology, and screening technology.
Type:
Grant
Filed:
November 25, 2003
Date of Patent:
August 30, 2011
Assignee:
Novartis Forschungesstiftung, Zweigniederlassung Friedrich Miescher Institute for Biomedical Research
Inventors:
Samuel Joseph Bichsel, Brian Arthur Hemmings, Mario Reinhard Stegert, Rastislav Tamaskovic