Abstract: Certain novel benzothiazoles and benzoxazoles, e.g., 2-(piperazin-1-yl)benzothiazoles and 2-(piperazin-1-yl)benzoxazoles, optionally substituted in the 3 and/or 4 positions of the piperazine rings,! of the general formula (1): having histamine H3 antagonistic activity can be used in pharmaceutical compositions.
Type:
Grant
Filed:
March 22, 2007
Date of Patent:
March 12, 2013
Assignee:
High Point Pharmaceuticals, LLC
Inventors:
Florencio Zaragoza Dorwald, Rolf Hohlweg, Inge Thoger Christensen, Jane Marie Lundbeck, Knud Erik Andersen
Abstract: The use of substituted amides for modulating the activity of 11?-hydroxysteroid dehydro-genase type 1 (11?HSD1) and the use of these compounds as pharmaceutical composi-tions, are described. Also a novel class of substituted amides, their use in therapy, phar-maceutical compositions comprising the compounds, as well as their use in the manufac-ture of medicaments are described. The present compounds are modulators and more specifically inhibitors of the activity of 11?HSD1 and may be useful in the treatment of a range of medical disorders where a decreased intracellular concentration of active gluco-corticoid is desirable.
Abstract: The use of substituted amides for modulating the activity of 11?-hydroxysteroid dehydrogenase type 1 (11?HSD1) and the use of these compounds as pharmaceutical compositions, are described. Also a novel class of substituted amides, 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 are modulators and more specifically inhibitors of the activity of 11?HSDI and may be useful in the treatment of a range of medical disorders where a decreased intracellular concentration of active glucocorticoid is desirable.
Abstract: Novel substituted benzamide based 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: 3-(1,3-Benzodioxol-5-yl)-6-(4-cyclopropylpiperazin-1-yl)pyridazine and salts and solvates thereof, having histamine H3 antagonistic activity can be used in pharmaceutical compositions.
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.
Type:
Grant
Filed:
April 4, 2011
Date of Patent:
January 29, 2013
Assignee:
High Point Pharmaceuticals, LLC
Inventors:
Per Sauerberg, Pavel Pihera, Zdenek Polivka, Miroslav Havranek, Ingrid Pettersson, John Patrick Mogensen
Abstract: The present invention is directed to substituted isoquinoline derivatives, pharmaceutically acceptable salts thereof, and tautomers of such compounds or salts, that inhibit ?-site amyloid precursor protein-cleaving enzyme (BACE) and that may be useful in the treatment 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 treatment of such diseases in which BACE is involved.
Type:
Grant
Filed:
August 22, 2011
Date of Patent:
January 8, 2013
Assignee:
High Point Pharmaceuticals, LLC
Inventors:
Adnan M. M. Mjalli, Bapu Gaddam, Devi Reddy Gohimukkula, Dharma Rao Polisetti, Hassan El Abdellaoui, Mohan Rao, Pingzhen Wang, Robert Carl Andrews, Rongyuan Xie, Tan Ren
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: 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-? or by PDE4, including but not limited to rheumatoid arthritis.
Type:
Grant
Filed:
March 2, 2012
Date of Patent:
December 11, 2012
Assignee:
High Point Pharmaceuticals, LLC
Inventors:
Adnan M. M. Mjalli, Bapu Gaddam, Dharma Rao Polisetti, Matthew J. Kostura, Mustafa Guzel
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 describes phenoxy-acetic acids and pharmaceutical compositions containing the same and methods of using the same. The phenoxy-acetic acids are activators of PPAR-? and should be useful for treating conditions mediated by the same.
Abstract: Novel compounds which interact with the histamine H3 receptor are defined. These compounds are particularly useful in the treatment of a variety of diseases or conditions in which histamine H3 interactions are beneficial. Thus, the compounds may find use, e.g., in the treatment of diseases of the central nervous system, the peripheral nervous system, the cardiovascular system, the pulmonary system, the gastrointestinal system and the endocrinological system. The novel compounds have a core consisting of a 6 membered aromatic ring containing at least one nitrogen atom and two carbon atoms in the ring and, at the remaining positions in the ring, there is either a carbon or a nitrogen atom.
Type:
Application
Filed:
May 15, 2012
Publication date:
September 13, 2012
Applicant:
HIGH POINT PHARMACEUTICALS, LLC
Inventors:
Rolf Hohlweg, Knud Erik Andersen, Jan Lindy Sorensen, Jane Marie Lundbeck
Abstract: The present invention describes phenoxy-acetic acids and pharmaceutical compositions containing the same and methods of using the same. The phenoxy-acetic acids are activators of PPAR-? and should be useful for treating conditions mediated by the same.
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-? or by PDE4, including but not limited to rheumatoid arthritis.
Type:
Application
Filed:
March 2, 2012
Publication date:
July 5, 2012
Applicant:
HIGH POINT PHARMACEUTICALS, LLC
Inventors:
Adnan M. M. Mjalli, Bapu Gaddam, Dharma Rao Polisetti, Matthew J. Kostura, Mustafa Guzel
Abstract: The present invention is directed to substituted imidazo[1,2-a]pyridine derivatives, pharmaceutically acceptable salts thereof, and tautomers of such compounds or salts, that inhibit ?-site amyloid precursor protein-cleaving enzyme (BACE) and that may be useful in the treatment 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 treatment of such diseases in which BACE is involved.
Type:
Application
Filed:
August 22, 2011
Publication date:
April 26, 2012
Applicant:
HIGH POINT PHARMACEUTICALS, LLC
Inventors:
Adnan M. M. Mjalli, Anitha Hari, Bapu Gaddam, Devi Reddy Gohimukkula, Dharma Rao Polisetti, Hassan El Abdellaoui, Mohan Rao, Robert Carl Andrews, Rongyuan Xie, Tan Ren
Abstract: The present invention is directed to substituted isoquinoline derivatives, pharmaceutically acceptable salts thereof, and tautomers of such compounds or salts, that inhibit ?-site amyloid precursor protein-cleaving enzyme (BACE) and that may be useful in the treatment 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 treatment of such diseases in which BACE is involved.
Type:
Application
Filed:
August 22, 2011
Publication date:
April 26, 2012
Applicant:
HIGH POINT PHARMACEUTICALS, LLC
Inventors:
Adnan M. M. Mjalli, Bapu Gaddam, Devi Reddy Gohimukkula, Dharma Rao Polisetti, Hassan El Abdellaoui, Mohan Rao, Pingzhen Wang, Robert Carl Andrews, Rongyuan Xie, Tan Ren
Abstract: The use of substituted amides of structure (I) for modulating the activity of 11 ?-hydroxysteroid dehydrogenase type 1 (11 ?HSD1) and the use of these compounds as pharmaceutical compositions, are described. Also a novel class of substituted amides, their use in therapy, pharmaceutical compositions comprising the compounds, as well as their use in the manufacture of medicaments 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.
Type:
Grant
Filed:
March 9, 2007
Date of Patent:
April 10, 2012
Assignee:
High Point Pharmaceuticals, LLC
Inventors:
John Paul Kilburn, Henrik Sune Andersen, Gita Camilla Tejlgaard Kampen
Abstract: Substituted pyridine derivatives, methods of their preparation, pharmaceutical compositions comprising a substituted pyridine derivative, and methods of use in treating inflammation are provided. The substituted pyridine derivatives may control of the activity or the amount or both the activity and the amount of heme-oxygenase.
Type:
Application
Filed:
October 21, 2011
Publication date:
March 22, 2012
Applicant:
HIGH POINT PHARMACEUTICALS, LLC
Inventors:
Bapu Gaddam, Dharma Rao Polisetti, Matthew J. Kostura, Mustafa Guzel, Samuel Victory
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:
January 18, 2010
Publication date:
February 23, 2012
Applicant:
HIGH POINT PHARMACEUTICALS, LLC
Inventors:
Lone Jeppesen, Ingrid Pettersson, Per Sauerberg, Pavel Pihera, Miroslav Havranek