Abstract: Novel compounds of the general formula (I), the use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds and methods of treatment employing these compounds and compositions. The present compounds are activators of PPAR? and should be useful for treating conditions mediated by the same.
Abstract: The present invention relates to novel compounds of formula [I], wherein R1 represents heteroaryl, at least one substituent among R5, R6 and R7 represent —SR12, —S(O)R12 or —S(O)2R12 and the remaining substituents are as defined in the claims, that act as chemical uncouplers. Compounds of the invention are useful inter alia, in the treatment, including prevention, of obesity, diabetes and a number of diseases associated therewith.
Type:
Grant
Filed:
November 15, 2007
Date of Patent:
May 10, 2011
Assignee:
High Point Pharmaceuticals, LLC
Inventors:
Anders Klarskov Petersen, Preben Houlberg Olesen, Lise Brown Christiansen, Flemming Elmelund Nielsen
Abstract: The present invention relates to novel compounds that act as chemical uncouplers. Compounds of the invention are useful, inter alia, in the treatment, including prevention, of obesity, diabetes and a number of diseases or conditions associated therewith.
Type:
Grant
Filed:
November 15, 2007
Date of Patent:
March 29, 2011
Assignee:
High Point Pharmaceuticals, LLC
Inventors:
Anders Klarskov Petersen, Preben Houlberg Olesen, Lise Brown Christiansen, Holger Claus Hansen, Flemming Elmelund Nielsen
Abstract: 6- (4-Cyclopropylpiperazin-1-yl) -2?-methyl- [3, 4?]bipyridinyl and salts and hydrates thereof interact with the histamine H3 receptor are defined.
Abstract: The present invention is directed to benzazole compounds that inhibit ?-site amyloid precursor protein-cleaving enzyme (BACE) and that may be useful in the treatment or prevention of diseases in which BACE is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which BACE is involved.
Type:
Application
Filed:
November 19, 2010
Publication date:
March 17, 2011
Applicant:
High Point Pharmaceuticals, LLC
Inventors:
Adnan M.M. Mjalli, David Jones, Devi Reddy Gohimmukkula, Guoxiang Huang, Jeff Zhu, Mohan Rao, Robert C. Andrews, Tan Ren
Abstract: The present invention is directed to benzazole compounds that inhibit ?-site amyloid precursor protein-cleaving enzyme (BACE) and that may be useful in the treatment or prevention of diseases in which BACE is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which BACE is involved.
Type:
Grant
Filed:
March 14, 2006
Date of Patent:
February 22, 2011
Assignee:
High Point Pharmaceuticals, LLC
Inventors:
Adnan M. M. Mjalli, David Jones, Devi Reddy Gohimmukkula, Guoxiang Huang, Jeff Zhu, Mohan Rao, Robert C. Andrews, Tan Ren
Abstract: The present invention provides compounds of the formula wherein R1, R2 and B are as herein described, pharmaceutical compositions comprising these compounds, use of these compounds for the preparation of pharmaceutical compositions and methods of use thereof for the treatment and/or prevention of disorders and diseases wherein modulation of the H3 receptor is beneficial.
Abstract: Novel substituted amide inhibitors, their use in therapy, pharmaceutical compositions comprising the compounds, the use of said compounds in the manufacture of medicaments, and therapeutic methods comprising the administration of said compounds are described. The present compounds modulate the activity of 11?-hydroxysteroid dehydrogenase type 1 (11?HSD1) and are accordingly useful in the treatment of diseases in which such a modulation is beneficial, such as the metabolic syndrome.
Abstract: A novel class of compounds of the general formula (I), their use in therapy, pharmaceutical compositions comprising the compounds, as well as their use in the manufacture of medicaments are described. The present compounds modulate the activity of 11?-hydroxy-steroid dehydrogenase type 1 (11?HSD1) and are accordingly useful in the treatment of diseases in which such a modulation is beneficial, e.g. the metabolic syndrome.
Abstract: A novel class of dicarboxylic acid derivatives, the use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds and methods of treatment employing these compounds and compositions. The present compounds may be useful in the treatment and/or prevention of conditions mediated by Peroxisome Proliferator -Activated Receptors (PPAR).
Type:
Grant
Filed:
December 12, 2003
Date of Patent:
October 19, 2010
Assignee:
High Point Pharmaceuticals, LLC
Inventors:
Per Sauerberg, Lone Jeppesen, Zdenek Polivka, Karel Sindelar
Abstract: A novel class of substituted homopiperidine, piperidine and pyrrolidine derivatives, methods for their preparation, pharmaceutical compositions comprising them and use thereof in the treatment of disorders related to the histamine H3 receptor. More particularly, the compounds possess histamine H3 receptor antagonistic activity and are thus useful in the treatment of disorders in which a histamine H3 receptor blockade is beneficial.
Type:
Grant
Filed:
December 21, 2007
Date of Patent:
September 21, 2010
Assignee:
High Point Pharmaceuticals, LLC
Inventors:
Jan Lindy Sorensen, Knud Erik Andersen, Ingrid Pettersson
Abstract: Novel compounds of the general formula (I), the use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds and methods of treatment employing these compounds and compositions. The present compounds may be useful in the treatment and/or prevention of conditions mediated by Peroxisome proliferator-activated receptors (PPAR), in particular the PPAR? suptype.
Type:
Application
Filed:
April 30, 2010
Publication date:
August 19, 2010
Applicant:
HIGH POINT PHARMACEUTICALS, LLC
Inventors:
Miroslav Havranek, Per Sauerberg, Ingrid Pettersson
Abstract: Methods of using fused 1,2,4-triazoles for modulating the activity of 11?-hydroxysteroid dehydrogenase type 1 (11?HSD1) are described. The present compounds are modulators and more specifically inhibitors of the activity of 11?HSD1 and may be useful in the treatment, prevention and/or prophylaxis of a range of medical disorders where a decreased intracellular concentration of active glucocorticoid is desirable, including type 2 diabetes and metabolic syndrome.
Type:
Application
Filed:
April 14, 2010
Publication date:
August 5, 2010
Applicant:
HIGH POINT PHARMACEUTICALS, LLC
Inventors:
Henrik Sune Andersen, Gita Camilla Tejlgaard Kampen, Inge Thoger Christensen, John Patrick Mogensen, Annette Rosendal Larsen
Abstract: A novel class of substituted piperidines, pharmaceutical compositions comprising them and use thereof in the treatment and/or prevention of diseases and disorders related to the histamine H3 receptor. More particularly, the compounds are useful for the treatment and/or prevention of diseases and disorders in which an interaction with the histamine H3 receptor is beneficial.
Abstract: The present invention relates to chemical compounds of Formula (I) are as herein defined, pharmaceutical compositions, and methods of use in the treatment of conditions or disorders mediated by TNF-alpha or by PDE4, including but not limited to rheumatoid arthritis.
Type:
Application
Filed:
January 23, 2009
Publication date:
July 29, 2010
Applicant:
HIGH POINT PHARMACEUTICALS, LLC.
Inventors:
Adnan M. M. Mjalli, Bapu Gaddam, Dharmo Rao, Matthew Kostura, Mustafa Guzel
Abstract: The use of fused 1,2,4-triazoles for modulating the activity of 11?-hydroxysteroid dehydrogenase type 1 (11?HSD1) and the use of these compounds as pharmaceutical compositions has been described. Also a novel class of fused 1,2,4-triazoles, their use in therapy, pharmaceutical compositions comprising the compounds, as well as their use in the manufacture of medicaments has been described. The present compounds are modulators and more specifically inhibitors of the activity of 11?HSD1 and may be useful in the treatment, prevention and/or prophylaxis of a range of medical disorders where a decreased intracellular concentration of active glucocorticoid is desirable.
Type:
Grant
Filed:
February 27, 2008
Date of Patent:
May 25, 2010
Assignee:
High Point Pharmaceuticals, LLC
Inventors:
Henrik Sune Andersen, Gita Camilla Tejlgaard Kampen, Inge Thoger Christensen, John Patrick Mogensen, Annette Rosendal Larsen
Abstract: A novel class of compounds of the general formula (I), their use in therapy, pharmaceutical compositions comprising the compounds, as well as their use in the manufacture of medicaments are described. The present compounds modulate the activity of 11?-hydroxysteroid dehydrogenase type 1 (11?HSD1) and are accordingly useful in the treatment of diseases in which such a modulation is beneficial, e.g. the metabolic syndrome.
Type:
Application
Filed:
December 17, 2009
Publication date:
May 13, 2010
Applicant:
High Point Pharmaceuticals, LLC
Inventors:
Anette Gundertofte, Anker Steen Jorgensen, Gita Camilla Tejlgaard Kampen, Henrik Sune Andersen, Inge Thoger Christensen, John Paul Kilburn
Abstract: Novel compounds of the general formula (I), the use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds and methods of treatment employing these compounds and compositions. The present compounds may be useful in the treatment and/or prevention of conditions mediated by Peroxisome Proliferator-Activated Receptors (PPAR), in particular the PPAR? suptype.
Type:
Grant
Filed:
May 23, 2006
Date of Patent:
May 4, 2010
Assignee:
High Point Pharmaceuticals, LLC
Inventors:
Lone Jeppesen, Ingrid Pettersson, Per Sauerberg, Pavel Pihera, Miroslav Havranek
Abstract: A novel class of compounds of the general formula (I), their use in therapy, pharmaceutical compositions comprising the compounds, as well as their use in the manufacture of medicaments are described. The present compounds modulate the activity of 11?-hydroxy-steroid dehydrogenase type 1 (11?HSD1) and are accordingly useful in the treatment of diseases in which such a modulation is beneficial, e.g. the metabolic syndrome.
Type:
Grant
Filed:
October 6, 2005
Date of Patent:
April 20, 2010
Assignee:
High Point Pharmaceuticals, LLC
Inventors:
Anette Gundertofte, Anker Steen Jorgensen, Gita Camilla Tejlgaard Kampen, Henrik Sune Andersen, Inge Thoger Christensen, Kilburn Paul John