Abstract: The invention relates to thiophene derivatives of formula (I)/their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunosuppressive agents wherein: A represents *—CO—CH?CH—, *—CO—CH2CH2—, *—CO—CH2—NH—, wherein the asterisks indicate the bond that is linked to the thiophene group of Formula (I), and R1-R3 are as defined in the claims.
Type:
Grant
Filed:
January 10, 2007
Date of Patent:
August 23, 2011
Assignee:
Actelion Pharmaceuticals Ltd.
Inventors:
Martin Bolli, David Lehmann, Boris Mathys, Claus Mueller, Oliver Nayler, Beat Steiner, Jörg Velker
Abstract: The present invention relates to modified GTP cyclohydrolase II enzymes that display increased specific activity, and to polynucleotides encoding them. The invention further pertains to vectors comprising these polynucleotides and host cells containing such vectors. The invention provides a method for producing the modified enzyme and a method for producing riboflavin, a riboflavin precursor, FMN, FAD, or a derivative thereof.
Type:
Grant
Filed:
July 7, 2005
Date of Patent:
August 2, 2011
Assignee:
DSM IP Assets B.V.
Inventors:
Sybille Ebert, Hans-Peter Hohnmann, Martin Lehmann, Nigel John Mouncey, Markus Wyss
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:
November 22, 2006
Date of Patent:
July 19, 2011
Assignee:
Actelion Pharmaceuticals Ltd.
Inventors:
Martin Bolli, David Lehmann, Boris Mathys, Claus Mueller, Oliver Nayler, Beat Steiner, Jörg Velker
Abstract: The invention relates to novel secondary amine 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:
January 31, 2007
Date of Patent:
June 28, 2011
Assignee:
Actelion Pharmaceuticals Ltd.
Inventors:
Olivier Bezencon, Daniel Bur, Olivier Corminboeuf, Daniel Dube, Corinna Grisostomi, Dwight MacDonald, Dan McKay, David Powell, Lubos Remen, Sylvia Richard-Bildstein, John Scheigetz, Michel Therien, Thomas Weller
Abstract: The invention relates to dispersible tablets comprising the compound 4-tert-butyl-N-[6-(2-hydroxy-ethoxy)-5-(2-methoxy-phenoxy)-2-(pyrimidin-2-yl)-pyrimidin-4-yl]-benzenesulfonamide.
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:
June 20, 2006
Date of Patent:
May 31, 2011
Assignee:
Actelion Pharmaceuticals Ltd.
Inventors:
Martin Bolli, David Lehmann, Boris Mathys, Claus Mueller, Jörg Velker
Abstract: A compound of formula (I) wherein R1, R2, R3, R4 and R5 are as defined in the specification, processes for their production, their uses, in particular in transplantation, and pharmaceutical compositions containing them.
Type:
Grant
Filed:
May 25, 2005
Date of Patent:
April 19, 2011
Assignee:
Novartis AG
Inventors:
Klaus Hinterding, Klemens Högenauer, Peter Nussbaumer
Abstract: The invention relates to a novel 3,9-diazabicyclo[3.3.1]nonene derivative of formula (I), enantiomers thereof, and their 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 at least one compound of formula (I): or (I?): and especially their use as inhibitors of renin.
Type:
Grant
Filed:
January 26, 2006
Date of Patent:
March 29, 2011
Assignee:
Actelion Pharmaceuticals Ltd.
Inventors:
Olivier Bezencon, Daniel Bur, Walter Fischli, Lubos Remen, Sylvia Richard-Bildstein, Thierry Sifferlen, Thomas Weller
Abstract: The present invention provides methods and compositions for modulating levels of amyloid-? peptide (A?) exhibited by cells or tissues. The invention also provides pharmaceutical compositions and methods of screening for compounds that modulate A? levels. The invention also provides modulation of A? levels via selective modulation (e.g., inhibition) of ATP-dependent ?-secretase activity. The invention also provides methods of preventing, treating or ameliorating the symptoms of a disorder, including but not limited to an A?-related disorder, by administering a modulator of ?-secretase, including, but not limited to, a selective inhibitor of ATP-dependent ?-secretase activity or an agent that decreases the formation of active (or optimally active) ?-secretase. The invention also provides the use of inhibitors of ATP-dependent ?-secretase activity to prevent, treat or ameliorate the symptoms of Alzheimer's disease.
Type:
Grant
Filed:
January 6, 2003
Date of Patent:
March 22, 2011
Assignee:
The Rockefeller University
Inventors:
William Netzer, Paul Greengard, Huaxi Xu
Abstract: The invention provides 3-(2-hydroxy-2,2-dithien-2-ylacetoxy)-1-(3-phenoxypropyl)-1-azoniabicyclo[2.2.2] octane in salt form, pharmaceutical compositions comprising it, and methods of using it for treatment of respiratory disorders, in association with steroids.
Type:
Grant
Filed:
May 26, 2010
Date of Patent:
March 1, 2011
Assignee:
Almirall Prodesfarma S.A.
Inventors:
Maria Dolors Fernandez Forner, Maria Prat Quiñones, Maria Antonia Buil Albero
Abstract: The invention relates to pharmaceutical compositions containing at least one thiazolidin-4-one derivative to prevent or treat disorders associated with an activated immune system. Furthermore, the invention relates to novel thiazolidin-4-one derivatives notably for use as pharmaceutically active compounds. Said compounds particularly act also as immunosuppressive agents.
Type:
Grant
Filed:
June 3, 2008
Date of Patent:
January 25, 2011
Assignee:
Actelion Pharmaceuticals Ltd.
Inventors:
Christoph Binkert, Martin Bolli, Boris Mathys, Claus Mueller, Michael Scherz, Oliver Nayler
Abstract: The invention relates to novel sulfamic acid amides 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 especially their use as endothelin receptor antagonists.
Type:
Grant
Filed:
November 11, 2005
Date of Patent:
January 11, 2011
Assignee:
Actelion Pharmaceuticals, Ltd.
Inventors:
Martin Bolli, Christoph Boss, Martine Clozel, Walter Fischli, Thomas Weller
Abstract: The present invention relates to extended release pharmaceutical compositions of Levetiracetam and processes for preparing the same. The extended release tablet of Levetiracetam is with a core comprising of Levetiracetam and water dispersible rate controlling polymer, and the tablet core is optionally functional coated comprising a combination of water non-dispersible and/or water dispersible polymer. It provides extended therapeutically effective plasma levels over a twenty four hour period with diminished incidences of neuropsychiatric adverse events by eliminating the troughs and peaks of drug concentration in a patient's blood plasma. The composition also exhibits no food effect.
Abstract: An extended release pharmaceutical composition of Levetiracetam with once a day dosage regime and the process of preparing it. The extended release tablet of Levetiracetam is with the core comprising of Levetiracetam and water dispersible rate controlling polymer, and the tablet core is optionally functional coated comprising a combination of water non-dispersible and/or water dispersible polymer. It provides extended therapeutically effective plasma levels over a twenty four hour period with diminished incidences of neuropsychiatric adverse events by eliminating the troughs and peaks of drug concentration in a patients blood plasma, which comprises administering orally to a patient in need thereof, an extended release tablet that provides a peak blood plasma level of Levetiracetam in from about eight to about Sixteen hours. The core is prepared by Wet granulation, Dry granulation or Direct compression and optionally the tablet core is coated either in an coating pan or in and Fluidized bed system.
Abstract: A compound of formula (I): wherein the substituents are as defined in the specification as inhibitor of C-Jun N terminal Kinases (JNK) and P-38 Kinases.
Abstract: A compound of formula I wherein R, Ra and Rb are as defined in the specification, processes for their production, their uses, in particular in transplantation, and pharmaceutical compositions containing them.
Type:
Grant
Filed:
May 12, 2005
Date of Patent:
December 14, 2010
Assignee:
Novartis AG
Inventors:
Maurice Van Eis, Jürgen Wagner, Peter Von Matt
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 20, 2006
Date of Patent:
December 7, 2010
Assignee:
Actelion Pharmaceuticals Ltd.
Inventors:
Martin Bolli, David Lehmann, Boris Mathys, Claus Mueller, Oliver Nayler, J{umlaut over ())}{umlaut over (})}org Velker, Thomas Weller
Abstract: The present invention is directed to a novel cytochrome c oxidase complex, genetic materials useful for the preparation of the said complex, such as recombinant polypeptides involved in cytochrome c oxidase complex, recombinant DNA fragments, expression vectors, recombinant organisms and the like. Those novel cytochrome c oxidase complex and genetic materials may be originated from a microorganism having the identifying characteristics of Gluconobacter oxydans DSM 4025. The present invention also provides a method for the preparation of the said novel recombinant cytochrome c oxidase complex and a process for the production of 2-keto-L-gulonic acid (2KGA).