Abstract: Methods for the treatment of a patient suffering from a disease or disorder ameliorated by inhibition of casein kinase I? activity comprising the administration of a compounds of formula (I) and formula (II) as inhibitors of human casein kinase I?, and methods of using the compounds of formula (I) and formula (II) for treating central nervous system diseases and disorders including mood disorders and sleep disorders. The R-group substituents are defined herein and pharmaceutical compositions comprising compounds of formula (I) or formula (II) useful in the claimed methods of treatment are also disclosed.
Type:
Grant
Filed:
November 12, 2008
Date of Patent:
April 12, 2011
Assignee:
Aventis Pharmaceuticals Inc.
Inventors:
William Arthur Metz, Jr., Fa-Xiang Ding
Abstract: The present invention is a DNA intercalating agent represented by the structure Y—Z—Y, wherein Y is an anti-tumor bis-carbazole and Z is a linear arrangement of multiple aromatic rings, containing at least two aromatic rings, or at least two alicyclic rings, wherein the rings are linked in a 1,4 or 1,3 manner. Methods of inhibiting cancer cells and treating subjects having cancer with these agents are also provided.
Abstract: The invention relates to novel compounds and methods of treating diseases, disorders, and conditions associated with amyloidosis. Amyloidosis refers to a collection of diseases, disorders, and conditions associated with abnormal deposition of A-beta protein.
Type:
Grant
Filed:
October 12, 2006
Date of Patent:
March 15, 2011
Assignee:
Elan Pharmaceuticals, Inc.
Inventors:
R. Jeffrey Neitz, Eric Tisdale, Barbara Jagodzinska, Anh Truong, Jay Tung
Abstract: Compounds of formula (I): wherein: ALK represents an alkylene chain, W represents a group selected from wherein R and R? are as defined in the description. Medicinal products containing the same which are useful in the treatment of cognitive and psycho-behavioural disorders associated with cerebral ageing, with neurodegenerative diseases or with cranial traumas and also in the treatment of mood disorders, of schizophrenia and of cognitive disorders associated therewith, of sleep disorders, of sleep-waking rhythm disorders, of attention-deficit hyperactivity syndrome or of obesity.
Type:
Grant
Filed:
June 12, 2009
Date of Patent:
March 15, 2011
Assignee:
Les Laboratoires Servier
Inventors:
Patrick Casara, Anne-Marie Chollet, Alain Dhainaut, Pierre Lestage, Fany Panayi, Anita Roger
Abstract: The present invention relates to novel inhibitors of glutaminyl cyclase and combinations thereof for the treatment of neuronal disorders, especially Alzheimer's disease, Down Syndrome, Parkinson disease, Chorea Huntington, pathogenic psychotic conditions, schizophrenia, impaired food intake, sleep-wakefulness, impaired homeostatic regulation of energy metabolism, impaired autonomic function, impaired hormonal balance, impaired regulation, body fluids, hypertension, fever, sleep dysregulation, anorexia, anxiety related disorders including depression, seizures including epilepsy, drug withdrawal and alcoholism, neurodegenerative disorders including cognitive dysfunction and dementia.
Type:
Grant
Filed:
October 24, 2007
Date of Patent:
March 1, 2011
Assignee:
Probiodrug AG
Inventors:
Stephan Schilling, Mirko Buchholz, Andre Niestroj, Ulrich Heiser, Hans-Ulrich Demuth
Abstract: Heterocyclic derivatives act as Ca channel antagonists. The compositions are useful for treating or relieving Ca channel mediated conditions.
Type:
Grant
Filed:
April 16, 2009
Date of Patent:
February 15, 2011
Assignee:
Vertex Pharmaceuticals Incorporated
Inventors:
Andreas Termin, Esther Martinborough, Nicole Zimmerman, Charles Cohen, Corey Gutierrez
Abstract: Compounds having the formula wherein the symbols have the meaning described in the specification are hydroxamic acid derivatives of phenoxy-acetic acids and analogs capable of inhibiting the lethal effects of infection by anthrax bacteria and are useful in the treatment of poisoning by anthrax.
Type:
Grant
Filed:
January 30, 2008
Date of Patent:
February 1, 2011
Inventors:
Alan T. Johnson, Guan-Sheng Jiao, Seongjin Kim
Abstract: Compounds, compositions and methods are provided for stabilizing transthyretin and for treating, preventing, or ameliorating one or more symptoms of transthyretin mediated diseases. In one embodiment, the compounds are benzoxazoles and related compounds.
Abstract: An efficient process is disclosed for producing a compound that is an inhibitor of CETP. The last step of the process is the coupling of an oxazolidinone derivative with a biphenyl moiety to provide a compound of formula (I). In a specific embodiment of this synthesis, a crystalline product is produced which is characterized as a non-solvated crystalline polymorph.
Abstract: A compound comprising or a pharmaceutically acceptable salt or a prodrug thereof, having the groups described in detail herein is disclosed. Also disclosed herein are compounds comprising or derivatives thereof, or pharmaceutically acceptable salts, tetrazoles, or prodrugs of compounds of the structure or derivatives thereof, said derivatives being described in detail herein. Also disclosed herein are methods of treating diseases or conditions, including glaucoma and elevated intraocular pressure. Compositions and methods of manufacturing medicaments related thereto are also disclosed.
Type:
Grant
Filed:
January 16, 2007
Date of Patent:
January 4, 2011
Assignee:
Allergan, Inc.
Inventors:
Yariv Donde, Robert M. Burk, Michael E. Garst
Abstract: This invention relates to novel macrocyclic lactams intermediates useful for the preparation of diazonamide analogs. This invention also relates to a novel electrochemical oxidative cyclization for the preparation of such macrocyclic lactams, and their further elucidation to provide diazonamide analogs.
Type:
Grant
Filed:
June 6, 2008
Date of Patent:
December 14, 2010
Assignees:
Board of Regents, The University of Texas System, Joyant Pharmaceuticals, Inc.
Inventors:
Gunnar Hanson, Charles Caldwell, Patrick G. Harran, Susan Harran, Qi Wei, Ming Zhou
Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.
Type:
Grant
Filed:
July 31, 2008
Date of Patent:
December 7, 2010
Assignee:
Vertex Pharmaceuticals Incorporated
Inventors:
Mark T. Miller, Sarah S. Hadida Ruah, Peter D. J. Grootenhuis, Matthew Hamilton
Abstract: The present invention provides synthetic processes for the preparation of sulfonyl halides of Formula Ar—(R)z—SO2—X and sulfonamides of Formula Ar—(R)z—SO2—NR4R5, where the constituent variables are as defined herein, that are useful as intermediates in the preparation of pharmaceuticals.
Type:
Grant
Filed:
July 20, 2006
Date of Patent:
November 30, 2010
Assignee:
Wyeth LLC
Inventors:
Ronald S. Michalak, Jean L. Helom, Joseph Zeldis
Abstract: A composition comprising a high molecular weight, water soluble polymer having a cloud point from about 20 to about 90° C. and at least one carrageenan is provided. The composition may be used as a component of a pharmaceutical dosage form, such as the shell of a dosage form, to provide burst release of active ingredient contained therein.
Type:
Grant
Filed:
October 28, 2003
Date of Patent:
November 23, 2010
Assignee:
McNeil-PPC, Inc.
Inventors:
Shun-Por Li, Der-Yang Lee, Frank J. Bunick, Jen Chi Chen, Harry S. Sowden
Abstract: The present invention relates to compounds and methods useful in the prevention or treatment of diseases or conditions associated with Toll-like receptor 2 activation.
Type:
Grant
Filed:
April 1, 2009
Date of Patent:
November 23, 2010
Assignee:
Eisai R&D Management Co., Ltd.
Inventors:
Jesse Chow, Fabian Gusovksy, Lynn Hawkins, Mark Spyvee
Abstract: The present invention relates to a compound of the formula (I) wherein R1 is H, C1-C6-alkyl which may be substituted by C3-C6-cycloalkyl, fluorinated C1-C6-alkyl, C3-C6-cycloalkyl, fluorinated C3-C6-cycloalkyl, C3-C6-alkenyl, fluorinated C3-C6-alkenyl, formyl, acetyl or propionyl; A is phenylene, pyridylene, pyrimidylene, pyrazinylene, pyridazinylene or thiophenylene, which can be substituted by one or more substituents selected from halogen, methyl, methoxy and CF3; E is NR5 or CH2, wherein R5 is H or C1-C3-alkyl; Ar is a cyclic radical selected from the group consisting of phenyl, a 5- or 6-membered heteroaromatic radical comprising as ring members 1, 2 or 3 heteroatoms selected from N, O and S and a phenyl ring fused to a saturated or unsaturated 5- or 6-membered carbocyclic or heterocyclic ring, where the heterocyclic ring comprises as ring members 1, 2 or 3 heteroatoms selected from N, O and S and/or 1, 2 or 3 heteroatom-containing groups each independently selected from NR8, where R8 is H, C1-C4-alk
Type:
Grant
Filed:
October 14, 2005
Date of Patent:
November 16, 2010
Assignee:
Abbott GmbH & Co. KG
Inventors:
Karla Drescher, Andreas Haupt, Liliane Unger, Sean C. Turner, Wilfried Braje, Roland Grandel
Abstract: The present invention relates to compounds useful as inhibitors of protein kinase, represented by structural formula I: or pharmaceutically acceptable salts thereof, wherein values of the variables of structural formula are as described in the specification and claims. The invention also provides pharmaceutically acceptable compositions comprising the compounds or salts, and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.
Type:
Grant
Filed:
April 12, 2007
Date of Patent:
November 9, 2010
Inventors:
Guy Brenchley, Steven Durrant, Jean-Damien Charrier, Ronald Knegtel, Sharn Ramaya, Shazia Sadiq
Abstract: Methods and formulations for treating inflammatory bowel disease are disclosed. The methods and formulations include, but are not limited to, methods and formulations for delivering effective concentrations of 4-aminosalicylic acid and/or 5-aminosalicylic acid, and pharmaceutically acceptable salts and pro-drugs thereof, to affected areas of the intestine, i.e., distal gut. The methods and formulations comprise modified-release elements, providing for drug delivery to the affected or desired area. Diseases and conditions treatable with the present invention include Crohn's disease and ulcerative colitis.
Abstract: A compound of general formula (I): A process for preparing this compound. A fungicide composition comprising a compound of general formula (I). A method for treating plants by applying a compound of general formula (I) or a composition comprising it.
Type:
Grant
Filed:
April 6, 2006
Date of Patent:
November 2, 2010
Assignee:
Bayer Cropscience AG
Inventors:
Darren Mansfield, Heiko Rieck, Pierre-Yves Coqueron, Philippe Desbordes, Alain Villier, Marie-Claire Grosjean-Cournoyer, Pierre Genix
Abstract: Compounds, compositions and methods are provided for modulating the activity of receptor kinases and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder mediated by receptor kinases.
Type:
Grant
Filed:
March 16, 2007
Date of Patent:
October 26, 2010
Assignee:
Ambit Biosciences Corporation
Inventors:
Shripad Bhagwat, Qi Chao, Robert M. Grotzfeld, Hitesh K. Patel, Kelly G. Sprankle