Abstract: Progesterone receptor modulators of formula I, or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R6, and R7 are as defined herein. These compounds are useful for contraception and hormone replacement therapy. Also provided are products containing these compounds.
Type:
Grant
Filed:
July 27, 2006
Date of Patent:
November 20, 2007
Assignee:
Wyeth
Inventors:
Casey Cameron McComas, Andrew Fensome, Edward George Melenski
Abstract: The present invention provides compounds, compositions and methods for the selective inhibition of cathepsin S. In a preferred aspect, cathepsin S is selectively inhibited in the presence of at least one other cathepsin isozyme. The present invention also provides methods for treating a disease state in a subject by selectively inhibiting cathepsin S.
Type:
Grant
Filed:
October 20, 2004
Date of Patent:
November 20, 2007
Assignee:
IRM LLC
Inventors:
Hong Liu, Phillip Alper, Daniel Mutnick, Donald Karanewsky
Abstract: Crystalline forms of the compounds (R)-2-(4-amidinophenylaminomethyl)-1-methyl-5-[1-(carboxymethylamino)-1-(pyrrolidinocarbonyl)-ethyl]-benzimidazole and the monohydrochloride thereof, processes for the preparation thereof and the use thereof as pharmaceutical compositions.
Type:
Grant
Filed:
December 13, 2006
Date of Patent:
November 13, 2007
Assignee:
Boehringer Ingelheim Pharma GmbH & Co. KG
Inventors:
Guenter Linz, Peter Sieger, Gunnar Schreiner, Werner Rall, Rolf Schmid
Abstract: A process for preparing perindopril is provided comprising condensing an N-[(S)-1-carbethoxybutyl]-(S)-alanyl halide of formula II: wherein X is a halide with an (2S,3aS,7aS)-2-carboxyperhydroindole of formula III: wherein R is hydrogen or a protecting group.
Abstract: Progesterone receptor modulators of formula I, or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R6 and R7 are as defined herein, are useful for contraception and hormone replacement therapy are described. Also provided are products containing these compounds.
Type:
Grant
Filed:
July 27, 2006
Date of Patent:
November 6, 2007
Assignee:
Wyeth
Inventors:
Casey Cameron McComas, Andrew Fensome, Edward George Melenski
Abstract: Process for the synthesis of compounds of formula (I): wherein R represents a hydrogen atom or a protecting group for the amino function. Application in the synthesis of perindopril and pharmaceutically acceptable salts thereof.
Abstract: Resistance-repellent and multidrug resistant retroviral protease inhibitors are provided. Pharmaceutical composition comprising such compounds, and methods of using such compounds to treat HIV infections in mammals, are also provided.
Type:
Grant
Filed:
January 7, 2003
Date of Patent:
October 23, 2007
Inventors:
John W. Erickson, Michael Eissenstat, Abelardo Silva, Sergei Gulnik
Abstract: Fluorescent dyes and probes are key components in multiphoton based fluorescence microscopy imaging of biological samples. In order to address the demand for better performing dyes for two-photon based imaging, a new series of reactive fluorophores tailored for multiphoton imaging has been disclosed. These fluorophores are based upon the fluorene ring system, known to exhibit high fluorescence quantum yields, typically >0.7, and possess high photostability. They have been functionalized with moieties to act, e.g., as efficient amine-reactive fluorescent probes for the covalent attachment onto, e.g., proteins and antibodies. The synthesis and the single-photon spectral characteristics, as well as measured two-photon absorption cross sections of the reactive fluorophores in solution are presented. Spectral characterizations of bovine serum albumin (BSA) conjugated with the new reactive probe is presented.
Type:
Grant
Filed:
April 11, 2007
Date of Patent:
October 16, 2007
Assignee:
Research Foundation of The University of Central Florida, Inc.
Inventors:
Kevin D. Belfield, Katherine J. Schafer
Abstract: Compounds, compositions, and methods for labeling membranes are disclosed. Compounds of formula G-L-E are described wherein G is a lipophilic group, L is a cleavable linkage and E is an electrophoretic group. The compounds become associated with membranes, and can be cleaved with a cleavage-inducing moiety thereby releasing the detectable electrophoretic group.
Abstract: There is provided pharmaceutically-acceptable acid addition salts of compounds of formula I, wherein R1 represents C1-2 alkyl substituted by one or more fluoro substituents; R2 represents C1-2 alkyl; and n represents 0, 1 or 2, which salts are useful as prodrugs of competitive inhibitors of trypsin-like proteases, such as thrombin, and thus, in particular, in the treatment of conditions where inhibition of thrombin is required (e.g. thrombosis) or as anticoagulants.
Type:
Grant
Filed:
May 27, 2003
Date of Patent:
September 25, 2007
Assignee:
AstraZeneca AB
Inventors:
Matti Ahlqvist, Martin Bohlin, Tord Inghardt, Anita Lundblad, Carl-Gustaf Sigfridsson
Abstract: The invention relates to a group of 1H-imidazole derivatives which are modulators of cannabinoid receptors, to methods for the preparation of these compounds, to novel intermediates useful for the synthesis of said imidazole derivatives, to methods for the preparation of these intermediates, to pharmaceutical compositions containing one or more of these 1H-imidazole derivatives as active ingredient, as well as to the use of these pharmaceutical compositions for the treatment of psychiatric and neurological disorders in which cannabinoid receptors are involved. The compounds have the general formula (I) wherein R, R1-R4 and X have the meanings given in the specification.
Type:
Grant
Filed:
October 15, 2004
Date of Patent:
September 18, 2007
Assignee:
Solvay Pharmaceuticals, Inc.
Inventors:
Josephus H. M. Lange, Cornelis G. Kruse, Herman H. Van Stuivenberg, Hiskias G. Keizer
Abstract: This invention relates to compounds of the formula I: wherein one of R6, R7 and R8 is and R1 to R15 and n are as defined in the description, and all enantiomers and pharmaceutically acceptable salts and/or esters thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and/or prevention of diseases which are modulated by PPAR ? and/or PPAR? agonists.
Type:
Grant
Filed:
March 8, 2005
Date of Patent:
September 4, 2007
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Jean Ackermann, Johannes Aebi, Alfred Binggeli, Uwe Grether, Georges Hirth, Bernd Kuhn, Hans-Peter Maerki, Markus Meyer, Peter Mohr, Matthew Blake Wright
Abstract: The present invention relates to compounds of formula (I): wherein —X—Y—, R1 to R11 and n are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prevention of diseases which are mediated by CETP inhibitors.
Type:
Grant
Filed:
August 4, 2005
Date of Patent:
August 21, 2007
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Aurelia Conte-Mayweg, Holger Kuehne, Thomas Luebbers, Cyrille Maugeais, Werner Mueller, Philippe Pflieger
Abstract: Fluorescent dyes and probes are key components in multiphoton based fluorescence microscopy imaging of biological samples. In order to address the demand for better performing dyes for two-photon based imaging, a new series of reactive fluorophores tailored for multiphoton imaging has been disclosed. These fluorophores are based upon the fluorene ring system, known to exhibit high fluorescence quantum yields, typically >0.7, and possess high photostability. They have been functionalized with moieties to act, e.g., as efficient amine-reactive fluorescent probes for the covalent attachment onto, e.g., proteins and antibodies. The synthesis and the single-photon spectral characteristics, as well as measured two-photon absorption cross sections of the reactive fluorophores in solution are presented. Spectral characterizations of bovine serum albumin (BSA) conjugated with the new reactive probe is presented.
Type:
Grant
Filed:
May 13, 2005
Date of Patent:
August 7, 2007
Assignee:
Research Foundation of The University of Central Florida, Inc.
Inventors:
Kevin D. Belfield, Katherine J. Schafer
Abstract: Benzodioxepines of the formula (I) and physiologically tolerated salts and solvates thereof, in which R1, R2, R3, R4, A, B, a and b have the meanings indicated in claim 1, are ligands of the 5HT1A receptors and/or the 5HT4 receptors with simultaneously strong serotonin reuptake inhibition.
Type:
Grant
Filed:
November 27, 2003
Date of Patent:
August 7, 2007
Assignee:
Merck Patent GmbH
Inventors:
Timo Heinrich, Henning Böttcher, Kai Schiemann, Günter Hölzemann, Christoph van Amsterdam, Gerd Bartoszyk, Hartmut Greiner, Christoph Seyfried, Michel Brunet, Jean Zeiller, Jean Berthelon
Abstract: The present invention relates to novel hydroxyethylamine compounds having Asp2 (?-secretase, BACE1 or Memapsin) inhibitory activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases characterised by elevated ?-amyloid levels or ?-amyloid deposits, particularly Alzheimer's disease.
Type:
Grant
Filed:
December 3, 2003
Date of Patent:
August 7, 2007
Assignee:
Glaxo Group Limited
Inventors:
Emmanuel H Demont, Andrew Faller, David Timothy MacPherson, Peter Henry Milner, Alan Naylor, Sally Redshaw, Steven James Stanway, David R Vesey, Daryl S Walter
Abstract: The invention is concerned with novel hexafluoroisopropanol substituted cyclohexane derivatives of formula (I) wherein R1 to R4, X, m and n are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds bind to LXR alpha and LXR beta and can be used as medicaments.
Abstract: The present invention is directed to water-soluble derivatives of 2,6-diisopropylphenol (Propofol). The compounds act as prodrugs of 2,6-diisopropylphenol and metabolize rapidly to Propofol thereby providing an alternative to the water-insoluble 2,6-diisopropylphenol. Pharmaceutical compositions comprising these compounds, methods of induction and maintenance of anesthesia or sedation as well as methods of treating neurodegenerative diseases utilizing pharmaceutical compositions comprising these compounds and methods of preparing them are also disclosed.
Abstract: The invention relates to the compounds (2R,4R), (2S,4R)-2-methylthiazolidine-2,4-dicarboxylic acid and (2RS,4R)-2-methylthiazolidine-2,4-dicarboxylic acid and salts of said compounds, the use thereof for the prophylaxis and/or treatment of neurodegenerative diseases, methods for the prophylaxis and/or treatment of neurodegenerative diseases, and pharmaceutical compositions containing said compounds together with physiologically compatible carriers, auxiliary agents, and/or solvents.