Abstract: The present invention provides novel purinones and purines useful for the prevention and treatment of autoimmune diseases, inflammatory disease, mast cell mediated disease and transplant rejection.
Type:
Grant
Filed:
August 22, 2008
Date of Patent:
March 8, 2011
Assignee:
Wyeth LLC
Inventors:
Irina Neagu, David Diller, Celia Kingsbury, Adolph C. Bohnstedt, Michael J. Ohlmeyer, Vidyadhar Paradkar, Nasrin Ansari
Abstract: wherein R3 is Alk14ArR16, and wherein Alk14 is C1-8 straight or branched alkylene or alkenylene. The present invention provides novel adenosine receptor antagonists, more particularly, A1 adenosine receptor antagonists of formula (I). Pharmaceutical compositions comprising an A1 adenosine receptor antagonist of formula (I) and a pharmaceutically acceptable carrier are further provided. Compositions also include diagnostic assay-type probes comprising a novel A1 adenosine receptor antagonist of formula (I) that is labeled or conjugated with radioactive or non-radioactive material. Methods for treating A1 adenosine receptor related disorders comprising administering an A1 adenosine receptor antagonist of formula I are also disclosed. The novel A1 adenosine receptor antagonist compositions of formula (I) find further use in diagnostic and imaging methods.
Abstract: A process for preparing 7-amino-3-[(E/Z)-2-(4-methylthiazol-5-yl)vinyl]-3-cephem-4-carboxylic acid of the formula (1) and an alkali metal salt thereof, said acid and said salt being improved in the content of 7-amino-3-[(Z)-2-(4-methylthiazol-5-yl)vinyl]-3-cephem-4-carboxylic acid of the formula (2) or an alkali metal salt thereof, the process being characterized in that an aqueous solution of an alkali metal salt of 7-amino-3-[(E/Z)-2-(4-methylthiazol-5-yl)vinyl]-3-cephem-4-carboxylic acid of the formula (1) is treated with a high porous polymer and/or active carbon as added thereto.
Type:
Grant
Filed:
June 3, 2005
Date of Patent:
February 22, 2011
Assignees:
Otsuka Chemical Co., Ltd., Meiji Seika Kaisha Ltd.
Abstract: Compounds of formula (I): (wherein variable groups are as defined within) pharmaceutically acceptable salts, solvates, solvates of such salts and prodrugs thereof and their use as cholesterol absorption inhibitors for the treatment of hyperlipidaemia are described. Processes for their manufacture and pharmaceutical compositions containing them are also described.
Abstract: The present invention involves substituted bicyclic 8-pyrrolidinoxanthines and their derivatives of formula I: wherein the various R groups are defined herein. The present invention also comprises pharmaceutical compositions comprising them as well as processes for the preparation of these compounds and methods for the treatment of metabolic disorders such as type-2 diabetes, insulin resistance, hyperglycemia, arteriosclerosis diseases and the like through the administration of said compositions.
Type:
Grant
Filed:
January 18, 2007
Date of Patent:
February 15, 2011
Assignee:
Sanofi-A Ventis Deutschland GmbH
Inventors:
Karl Schoenafinger, Gerhard Jaehne, Elisabeth Defossa, Lothar Schwink, Holger Wagner, Christian Buning, Georg Tschank, Ulrich Werner
Abstract: The present invention provides substituted 8-[6-amino-3-pyridyl]xanthines like the compound shown in the following formula: and pharmaceutical compositions that are selective antagonists of A2B adenosine receptors (ARs). These compounds and compositions are useful as pharmaceutical agents.
Type:
Grant
Filed:
June 12, 2007
Date of Patent:
February 8, 2011
Assignee:
PGxHealth, LLC
Inventors:
Guoquan Wang, Robert D. Thompson, Jayson M. Rieger
Abstract: The present invention relates to Azetidinone Derivatives of structural formula 1: and compositions comprising an Azetidinone Derivative and methods for treating or preventing a disorder of lipid metabolism, pain, diabetes, a vascular condition, demyelination or nonalcoholic fatty liver disease, comprising administering to a patient an effective amount of an Azetidinone Derivative.
Type:
Grant
Filed:
September 13, 2007
Date of Patent:
February 8, 2011
Assignee:
Schering Plough Corporation
Inventors:
Robert G. Aslanian, Chad E. Bennett, Duane A. Burnett, Tin-Yau Chan, Eugenia Y. Kiselgof, Chad E. Knutson, Joel M. Harris, Brian A. McKittrick, Anandan Palani, Elizabeth M. Smith, Henry M. Vaccaro, Dong Xiao, Hyunjin M. Kim
Abstract: The present invention provides novel purine and imidazopyridine derivatives useful for the prevention and treatment of autoimmune diseases, inflammatory disease, mast cell mediated disease and transplant rejection.
Type:
Grant
Filed:
October 11, 2007
Date of Patent:
February 8, 2011
Assignee:
Wyeth LLC
Inventors:
Michael J. Ohlmeyer, Adolph C. Bohnstedt, Celia Kingsbury, Koc-Kan Ho, Jorge Gabriel Quintero, Ming You, Haengsoon Park, Yingchun Lu
Abstract: The present invention relates to 4-alkenyl-2-azetidinone derivatives, a process for preparing 4-alkenyl-2-azetidinone derivatives and multicyclic compounds prepared using 4-alkenyl-2-azetidinone derivatives. More specifically, the present invention relates to a 4-alkenyl-2-azetidinone derivative having a novel structure represented by the following chemical formula 1, in which an alkenyl group such as 1,3-dien-2-yl or 1,2,4,5-hexatetraen-3-yl is substituted at the C-4 position of azetidinone; to a process for preparing the 4-alkenyl-2-azetidinone derivative by reacting 4-acetoxy-2-azetidinone with organic indium, which is prepared by reacting a propargyl halide derivative with indium; and to a novel multicyclic compound prepared using the compound represented by the following chemical formula 1 as an intermediate in the Diels-Alder reaction.
Abstract: Compounds for the treatment of elevated blood glucose levels and the physiological and metabolic disorders arising therefrom are disclosed which are inhibitors of the enzyme dipeptidyl peptidase IV (DDP-IV) and comprise novel substituted bicyclic 8-pyrrolidinoxanthines of formula I and their derivatives: wherein the various R-groups are defined herein. These compounds may be combined with other secondary active compounds which also are effective in the treatment of said disorders and the disease states or physiological manifestations arising therefrom.
Type:
Grant
Filed:
February 13, 2007
Date of Patent:
February 1, 2011
Assignee:
Sanofi-Aventis Deutschland GmbH
Inventors:
Karl Schoenafinger, Gerhard Jaehne, Elisabeth Defossa, Christian Buning, Georg Tschank, Ulrich Werner
Abstract: The present invention provides substituted 8-[6-amino-3-pyridyl]xanthines like the compound shown in the following formula: and pharmaceutical compositions that are selective antagonists of A2B adenosine receptors (ARs). These compounds and compositions are useful as pharmaceutical agents.
Type:
Grant
Filed:
December 17, 2008
Date of Patent:
January 25, 2011
Inventors:
Robert D. Thompson, Guoquan Wang, Anthony Beauglehole, Frank Schmidtmann
Abstract: The invention is related to phosphorus substituted anti-viral inhibitory compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.
Type:
Grant
Filed:
July 26, 2005
Date of Patent:
January 18, 2011
Assignee:
Gilead Sciences, Inc.
Inventors:
Constantine G. Boojamra, Kuei-Ying Lin, Richard Mackman, David Y. Markevitch, Oleg V. Petrakovsky, Adrian S. Ray, Lijun Zhang
Abstract: Compounds of formula (I): (wherein variable groups are as defined within) pharmaceutically acceptable salts, solvates, solvates of such salts and prodrugs thereof and their use as cholesterol absorption inhibitors for the treatment of hyperlipidaemia are described. Processes for their manufacture and pharmaceutical compositions containing them are also described.
Abstract: The present invention provides methods for suppressing autoimmunity in a patient in need of treatment for systemic lupus erythematosus by administering to the patient an effective amount of methyl 4-(Adenin-9-yl)-2-hydroxybutanoate or pharmaceutically acceptable salts thereof. In some embodiments, the claimed methods include co-administering an effective amount of an immunosuppressant.
Abstract: Compounds of formula (I) (wherein variable groups are as defined within) pharmaceutically acceptable salts, solvates, solvates of such salts and prodrugs thereof and their use as cholesterol absorption inhibitors for the treatment of hyperlipidaemia are described. Processes for their manufacture and pharmaceutical compositions containing them are also described.
Abstract: The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, methods of using the same, processes for preparing the same, and intermediates thereof.
Type:
Grant
Filed:
May 4, 2006
Date of Patent:
December 7, 2010
Assignee:
Eli Lilly and Company
Inventors:
David Michael Bender, James Ray McCarthy
Abstract: The invention relates to heterosubstituted N-thiolated beta-lactams, compositions comprising these compounds, methods for their production, and methods of use as antibiotics to inhibit the growth of bacteria. In one embodiment, the compounds have the structure shown in formula (A) or formula (B) or formula (C): wherein the R groups are as defined in the specification. The antibacterial agents of the invention can be administered to a human or animal to treat or inhibit bacterial infection, such as that of Staphylococcus species, including methicillin-resistant Staphylococcus aureus (MRSA).
Abstract: The present invention provides 2-azetidinone derivatives, or pharmaceutically acceptable salts, solvates, solvates of such salts and prodrugs thereof, comprising formula (I): wherein the substituents are as herein defined. The compounds possess cholesterol absorption inhibitory activity and are accordingly of value in the treatment of disease states associated with hyperlipidaemic conditions.
Abstract: Compounds of formula (I) wherein R1 is a phenylcarbonylmethyl group wherein the phenyl moiety is substituted by R10 and R11 and R2 to R4 and R10 and R1l are defined as in the claims, or the prodrugs or salts thereof, particularly the physiologically acceptable salts thereof, pharmaceutical compositions containing these compounds, and methods of treating type II diabetes mellitus and obesity using these compounds.
Type:
Grant
Filed:
January 16, 2009
Date of Patent:
November 23, 2010
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Frank Himmelsbach, Elke Langkopf, Matthias Eckhardt, Michael Mark, Roland Maier, Ralf Lotz