Abstract: Compounds of Formula (I): or pharmaceutically acceptable salts or N-oxides thereof, are useful in the prophylactic and therapeutic treatment of hyperglycemia and diabetes.
Type:
Grant
Filed:
February 10, 2004
Date of Patent:
August 28, 2007
Assignee:
Prosidion Limited
Inventors:
Matthew Colin Thor Fyfe, Lisa Sarah Gardner, Maseo Nawano, Martin James Procter, Chrystelle Marie Rasamison, Geoffrey Martyn Williams, David Witter, Arlindo Castelhano, Kosuke Yasuda
Abstract: Prodrug compounds of unstable inhibitors of the serine peptidase dipeptidyl peptidase IV, are used in the treatment of various disorders, especially of metabolic disorders. The Prodrug compounds can be used in the treatment of impaired glucose tolerance, glucosuria, hyperlipidaemia, metabolic acidoses, diabetes mellitus, diabetic neuropathy and nephropathy.
Abstract: This invention pertains to compounds which specifically inhibit the adenosine A3 receptor and the use of these compounds to treat a disease associated with A3 adenosine receptor in a subject, comprising administering to the subject a therapeutically effective amount of the compounds.
Type:
Grant
Filed:
December 1, 2000
Date of Patent:
January 9, 2007
Assignee:
OSI Pharmaceuticals, Inc.
Inventors:
Arlindo L. Castelhano, Bryan McKibben, David J. Witter
Abstract: A screening assay in yeast is disclosed wherein G-protein coupled-receptor independent activators and inhibitors of the pheromone pathway can be identified using a mammalian cDNA library. Novel Activator of G protein Signaling (“AGS”) proteins, which are Ras-related proteins that stimulate G protein activity in a receptor-independent manner, are disclosed, as well as nucleic acid molecules encoding AGS proteins. In addition to isolated AGS proteins, the invention further provides isolated AGS fusion proteins, antigenic peptides and anti-AGS antibodies. The invention also provides isolated AGS nucleic acid molecules, recombinant expression vectors containing a nucleic acid molecule of the invention, host cells into which the expression vectors have been introduced and non-human transgenic animals in which an AGS gene has been introduced or disrupted. Diagnostic, screening and therapeutic methods utilizing compositions of the invention are also provided.
Abstract: A method of treatment of hyperproliferative disorders comprises administering an effective amount of a compound represented by Formula II: or a pharmaceutically acceptable salt thereof.
Abstract: A method of monotherapy for a subject suffering from abnormal cell growth expressing the epidermal growth factor receptor (EGFR) which comprises orally administering to the subject a therapeutically effective amount of a crystalline polymorph of the hydrochloride salt of N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine so as to treat the subject.
Type:
Grant
Filed:
November 18, 2004
Date of Patent:
August 8, 2006
Assignee:
OSI Pharmaceuticals, Inc.
Inventors:
Timothy Norris, Jeffrey W. Raggon, Richard D. Connell, James D. Moyer, Michael J. Morin, Shama M. Kajiji, Barbara A. Foster, Karen J. Ferrante, Sandra L. Silberman
Abstract: The present invention provides compounds of the formula: wherein X=CH2 or S or pharmaceutical acceptable salts thereof useful for treating conditions mediated by DPIV or DPIV-like enzymes, such as arthritis, obesity, immune and autoimmune disorders, allograft transplantation, cancer, neuronal disorders and dermal diseases.
Abstract: Novel compounds of unstable inhibitors of the serine peptidase dipeptidyl peptidase IV, are used in the treatment of various disorders, especially of metabolic disorders. The compounds can be used in the treatment of impaired glucose tolerance, glucosuria, hyperlipidaemia, metabolic acidoses, diabetes mellitus, diabetic neuropathy and nephropathy.
Type:
Grant
Filed:
December 21, 2000
Date of Patent:
May 30, 2006
Assignee:
Prosidion Ltd.
Inventors:
Hans-Ulrich Demuth, Jorn Schmidt, Torsten Hoffmann, Konrad Glund
Abstract: Substituted condensation products of N-benzyl-3-indenylacetamides with heterocyclic aldehydes and other such inhibitors are useful for the treatment of inflammatory bowel disease.
Abstract: There is disclosed 3-(5-methylisoxazol-3-yl)-6-(1-methyl-1,2,3-triazol-4-yl)methyloxy-1,2,4-triazolo[3,4-a]phthalazine in the form of a dihydrate, a dehydrate of the dihydrate and a pentahydrate, pharmaceutical compositions comprising the forms, the use of the forms for enhancing cognition, processes for producing the forms, their incorporation in pharmaceutical compositions comprising pamoate ions and the use of such ions for solubilizing neutral molecules.
Abstract: 4-substituted cyclohexanes substituted in the 1-position with imidazopyridine either directly or through a C1-C4alkyl, C1-C4alkenyl, C1-C4alkynyl, C1-C4alkoxy, amino, aminoC1-C4alkyl, hydroxyC1-C4alkyl, carbonyl, cycloC3-C6alkyl or aminocarbonyl chain are effective as NMDA NR2B antagonists useful for relieving pain.
Type:
Grant
Filed:
May 21, 2001
Date of Patent:
December 17, 2002
Assignee:
Merck & Co., Inc.
Inventors:
Wayne J. Thompson, David A. Claremon, Peter M. Munson, John A. McCauley
Abstract: There are disclosed compounds of formula (I)
and pharmaceutically acceptable salts thereof which exhibit utility for the treatment of cytokine mediated diseases such as arthritis.
Type:
Grant
Filed:
May 4, 2000
Date of Patent:
December 10, 2002
Assignee:
Merck & Co., Inc.
Inventors:
Nigel J. Liverton, David A. Claremon, Cory R. Theberge
Abstract: Compounds according to Formula (I) or a salt thereof are selective antagonists of the human 5-HT2A receptor useful for treatment of adverse conditions of the central nervous system:
Type:
Grant
Filed:
January 12, 2001
Date of Patent:
November 12, 2002
Assignee:
Merck Sharp & Dohme Ltd.
Inventors:
Christopher Richard Moyes, Michael Rowley
Abstract: Novel 3-substituted 8-aza-bicyclo[3.2.1]octanes (commonly known as “tropanes”) substituted in the 8-position are effective as NMDA NR2B antagonists useful for relieving pain.
Type:
Grant
Filed:
October 25, 2000
Date of Patent:
August 13, 2002
Assignee:
Merck & Co., Inc.
Inventors:
Wayne Thompson, David A. Claremon, Peter M. Munson, Brian Phillips
Abstract: A device for supplying air or medical gases in a conditioned, particularly a moistened and/or heated state to a patient, through an air pipe. The device includes at least one component to be connected to said air pipe, the component being formed by a cylinder-shaped element with an inner tube through which the moistened air flows, which cylinder-shaped element is fitted with self-regulating heating resistors which heat the air flowing through the tube, while the cylinder-shaped tube from one element at least is filled with a material which adsorbs or absorbs the water supplied by a water-supply line from a container, and has a good air-permeability.