Abstract: The invention relates to compounds of the formula or a pharmaceutically acceptable salt thereof, wherein R?, R1 through R7 and Ar are as defined herein. These compounds are useful as inhibitors of phosphodiesterase 10 (PDE10A) which are useful in treating central nervous system diseases such as psychosis and also in treating, for example, obesity, type II diabetes, metabolic syndrome, glucose intolerance, pain and ophthalmic diseases.
Type:
Grant
Filed:
October 16, 2015
Date of Patent:
February 27, 2018
Assignees:
EXONHIT THERAPEUTICS, SA, ALLERGAN, INC.
Inventors:
Bertrand Leblond, Thierry Taverne, Cedric Chauvignac, Eric Beausoleil, Anne-Sophie Casagrande, Laurent Desire, Matthew P. Pando, John E. Donello, Rong Yang
Abstract: Compounds of the formula where the variables have the meaning defined in the specification have analgesic and/or immunostimulant effect in mammals.
Type:
Grant
Filed:
November 30, 2015
Date of Patent:
November 28, 2017
Assignees:
EXONHIT THERAPEUTICS SA, ALLERGAN, INC.
Inventors:
Bertrand Leblond, Eric Beusoleil, Thierry Taverne, John E. Donello
Abstract: The invention relates to compounds of the formula wherein R?, R1 through R7 and Ar are as defined herein. These compounds are useful as inhibitors of phosphodiesterase 10 (PDE10A) which are useful in treating central nervous system diseases such as psychosis and also in treating, for example, obesity, type II diabetes, metabolic syndrome, glucose intolerance, pain and ophthalmic diseases.
Type:
Grant
Filed:
June 25, 2014
Date of Patent:
June 6, 2017
Assignees:
ALLERGAN, INC., EXONHIT THERAPEUTICS SA
Inventors:
Bertrand Leblond, Cedric Chauvignac, Thierry Taverne, Eric Beausoleil, Anne-Sophie Casagrande, Laurent Desire, Matthew P. Pando, John E. Donello, Rong Yang
Abstract: The invention relates to compounds of the formula or a pharmaceutically acceptable salt thereof, wherein R?, R1 through R7 and Ar are as defined herein. These compounds are useful as inhibitors of phosphodiesterase 10 (PDE10A) which are useful in treating central nervous system diseases such as psychosis and also in treating, for example, obesity, type II diabetes, metabolic syndrome, glucose intolerance, pain and ophthalmic diseases.
Type:
Application
Filed:
October 16, 2015
Publication date:
September 15, 2016
Applicant:
EXONHIT THERAPEUTICS, SA
Inventors:
Bertrand Leblond, Thierry Taverne, Cedric Chauvignac, Eric Beausoleil, Anne-Sophie Casagrande, Laurent Desire, Matthew P. Pando, John E. Donello, Rong Yang
Abstract: The compounds shown by the structural formulas below have analgesic effect and are used in compositions and methods for treating mammal in need of such treatment.
Type:
Grant
Filed:
April 19, 2012
Date of Patent:
March 8, 2016
Assignees:
Exonhit Therapeutics SA, Allergan, Inc.
Inventors:
Bertrand Leblond, Eric Beausoleil, Thierry Taverne, John E. Donello, Fabien (Jacques) Schweighoffer
Abstract: The invention relates to compounds of the formula or a pharmaceutically acceptable salt thereof, wherein R?, R1 through R7 and Ar are as defined herein. These compounds are useful as inhibitors of phosphodiesterase 10 (PDE10A) which are useful in treating central nervous system diseases such as psychosis and also in treating, for example, obesity, type II diabetes, metabolic syndrome, glucose intolerance, pain and ophthalmic diseases.
Type:
Grant
Filed:
December 5, 2013
Date of Patent:
December 1, 2015
Assignees:
Allergan, Inc., Exonhit Therapeutics, SA
Inventors:
Bertrand Leblond, Thierry Taverne, Cedric Chauvignac, Eric Beausoleil, Anne-Sophie Casagrande, Laurent Desire, Matthew P. Pando, John E. Donello, Rong Yang
Abstract: The invention relates to compounds of the formula wherein R?, R1, through R7 and Ar are as defined herein. These compounds are useful as inhibitors of phosphodiesterase 10 (PDE10A) which are useful in treating central nervous system diseases such as psychosis and also in treating, for example, obesity, type II diabetes, metabolic syndrome, glucose intolerance, pain and ophthalmic diseases.
Type:
Grant
Filed:
February 17, 2012
Date of Patent:
July 8, 2014
Assignees:
Allergan, Inc., Exonhit Therapeutics SA
Inventors:
Bertrand Leblond, John E. Donello, Cédric Chauvignac, Thierry Taverne, Eric Beausoleil, Anne-Sophie Casagrande, Laurent Désiré, Matthew P. Pando, Rong Yang
Abstract: Compounds of the formula where the variables have the meaning defined in the specification have analgesic and/or immunostimulant effect in mammals.
Type:
Grant
Filed:
August 2, 2011
Date of Patent:
August 20, 2013
Assignees:
Allergan, Inc., ExonHit Therapeutics SA
Inventors:
Bertrand Leblond, Eric Beusoleil, Thierry Taverne, John E. Donello
Abstract: The present invention concerns methods and compositions usable for diagnosing Alzheimer's disease in mammals, in particular humans. It particularly describes serum markers for Alzheimer's disease and their use in diagnostic methods. It also concerns tools and/or kits usable for implementing these methods (reagents, probes, primers, antibodies, chips, cells, etc.), their preparation and their use. The invention is usable to detect the presence or progression of Alzheimer's disease in mammals, including in the early phase, as well as for predicting the efficacy of an Alzheimer's disease treatment.
Abstract: Compounds of Formulas 1 and 2 where the variables have the meaning disclosed in the specification, have analgesic and in some cases immunostimulant activity.
Type:
Grant
Filed:
September 12, 2012
Date of Patent:
April 30, 2013
Assignees:
Allergan, Inc., ExonHit Therapeutics SA
Inventors:
Bertrand Leblond, Eric Beausoleil, Thierry Taverne, John E. Donello
Abstract: Compounds of Formulas 1 and 2 where the variables have the meaning disclosed in the specification, have analgesic and in some cases immunostimulant activity.
Type:
Application
Filed:
September 12, 2012
Publication date:
January 3, 2013
Applicants:
ExonHit Therapeutics SA, Allergan, Inc.
Inventors:
Bertrand Leblond, Eric Beausoleil, Thierry Taverne, John E. Donello
Abstract: Compounds of Formulas 1 and 2 where the variables have the meaning disclosed in the specification, have analgesic and in some cases immunostimulant activity.
Type:
Grant
Filed:
January 25, 2006
Date of Patent:
October 16, 2012
Assignees:
Allergan, Inc., Exonhit Therapeutics SA
Inventors:
Bertrand Leblond, Eric Beausoleil, Thierry Taverne, John E. Donello
Abstract: Disclosed herein is a method of treating disorders of the retina comprising administering to a patient in need of such treatment a therapeutically effective amount of a compound of Formula I as defined herein. These compounds are useful as PDE10 inhibitors.
Type:
Application
Filed:
February 16, 2012
Publication date:
August 23, 2012
Applicants:
ExonHit Therapeutics SA, ALLERGAN, INC.
Inventors:
John E. Donello, Rong Yang, Bertrand Leblond, Eric Beausoleil, Matthew P. Pando, Laurent Désiré, Anne-Sophie Casagrande, Veena Viswanath
Abstract: The invention relates to compounds of the formula wherein R?, R1, through R7 and Ar are as defined herein. These compounds are useful as inhibitors of phosphodiesterase 10 (PDE10A) which are useful in treating central nervous system diseases such as psychosis and also in treating, for example, obesity, type II diabetes, metabolic syndrome, glucose intolerance, pain and ophthalmic diseases.
Type:
Application
Filed:
February 17, 2012
Publication date:
August 23, 2012
Applicants:
ExonHit Therapeutics SA, ALLERGAN, INC.
Inventors:
Bertrand Leblond, Cédric Chauvignac, Thierry Taverne, Eric Beausoleil, Anne-Sophie Casagrande, Laurent Désiré, Matthew P. Pando, John E. Donello, Rong Yang
Abstract: The present invention relates to the fields of biology, genetics and medicine. In particular it concerns new methods for the detection, characterisation and/or treatment (or management) of neurodegenerative diseases, particularly amyotrophic lateral sclerosis. The invention equally concerns methods for identifying or screening compounds active in these diseases. The invention further concerns the compounds, genes, cells, plasmids or compositions useful for implementing the hereinabove methods. In particular, the invention describes the role of PDE4B in these diseases and its use as a therapeutic, diagnostic or experimental target.
Type:
Application
Filed:
March 28, 2012
Publication date:
August 9, 2012
Applicant:
Exonhit Therapeutics SA
Inventors:
Ali AIT IKHLEF, Annelies Resink, Fabien Schweighoffer
Abstract: The invention relates to the field of biology, genetics and medicine. In particular, the invention relates to novel methods for the detection, characterization and/or treatment (or management) of neurodegenerative pathologies. The invention also relates to methods for the identification or screening of compounds active in the aforementioned pathologies. The invention further relates to the compounds, genes, cells, plasmids or compositions which are used to carry out said methods. In particular, the invention is based on the identification of the role of phosphodiesterase 4B, the peripheral benzodiazepine receptor (PBR) and GABA receptors of the type GABA(A) in neurodegenerative pathologies and describes the use of same as therapeutic, diagnostic or experimental markers or targets for said disorders.
Abstract: The present invention relates generally to the fields of genetics, biochemistry, medicinal chemistry and medicine. The present invention more particularly discloses the identification of a human gene variant involved in neuropathological conditions, and methods for the diagnosis, prevention and treatment of such diseases and related disorders, as well as for the screening of therapeutically active drugs. The present invention relates to catalytically active beta-secretase (Memapsin2, BACE) variants, and nucleic acids encoding them. The invention is useful in the identification of agents that inhibit the activity of a particular BACE isoform and thus agents and therapies affecting the genesis, development or progression of neuropathological conditions, including Alzheimer's disease and dementia.