Abstract: The invention relates to compositions comprising substituted imidazoline compounds including prodrugs, and salts thereof. In some embodiments, the invention relates to the use of these compositions as therapeutic agents, preferably for the treatment of arthritis or cancer. In further embodiments, The invention relates to the pharmaceutical compositions with effective amounts of substituted imidazoline compounds disclosed herein that function as agonist or antagonists of the genetic expression or interactions with transcription factor NF-?B.
Type:
Grant
Filed:
October 8, 2008
Date of Patent:
August 28, 2012
Assignee:
Board of Trustees of Michigan State University
Abstract: N-tert-butoxycarbonyl-2-pyrrolidinones represented by the following formula (1). In the formula (1), R1, R2, R3, R4, R5 and R6 independently represent a hydrogen atom, a halogen atom, a cyano group, a linear, branched or cyclic alkyl group having 1 to 10 carbon atoms, which may have a substituent, a linear, branched or cyclic alkenyl group having 2 to 10 carbon atoms, which may have a substituent, or the like, R1 and R2 may be linked to form a >C?O group along with the carbon atom to which both are attached, R3 and R4 may be linked to form a >C?O group along with the carbon atom to which both are attached, R5 and R6 may be linked to form a >C?O group along with the carbon atom to which both are attached, or any two among R1, R2, R3, R4, R5 and R6 may be linked to form a polymethylene group having 1 to 4 carbon atoms which may have a substituent.
Abstract: Disclosed herein are novel 1,3-dihydro-5-isobenzofurancarbonitrile derivatives represented by Formula 1, or pharmaceutically acceptable salts thereof. Also disclosed is a pharmaceutical composition for treating or preventing premature ejaculation including the compound. The 1,3-dihydro-5-isobenzofurancarbonitrile derivatives have a short half-life and inhibit the ejaculation process by selectively inhibiting serotonin reuptake via a serotonin reuptake transporter present in a presynaptic neuron. Thus, the compounds are useful in the treatment and prevention of premature ejaculation.
Type:
Grant
Filed:
October 31, 2008
Date of Patent:
August 14, 2012
Assignee:
Dong-A Pharmaceutical. Co., Ltd
Inventors:
Yeong Geon Lee, Soo-Jung Choi, Tae-Kyung Kang, Mi-Jeong Seo, Chang-Yong Shin, Kyung-Seok Lee, Gook-Jun Ahn, Seul-Min Choi, Yong-Duck Kim, Dong-Hwan Kim, Kyung-Koo Kang, Hyun-Joo Shim, Dong-Sung Kim, Byoung-Ok Ahn, Moo-Hi Yoo
Abstract: Anionic acid-labile surfactants may generally comprise compounds represented by the formula: wherein R1 is independently selected from —(CH2)0-9CH3, R2 is selected from the group consisting of —H and —(CH2)0-5CH3, Y is an anion, X is a cation, and n is an integer from 1 to 8. Methods of making and using the anionic acid-labile surfactants are also described. The anionic acid-labile surfactants may be used to facilitate the solubilization of proteins and other molecules in an aqueous environment.
Type:
Grant
Filed:
August 1, 2011
Date of Patent:
July 31, 2012
Assignee:
Protea Biosciences, Inc.
Inventors:
Matthew Jacob Powell, Trust Tariro Razunguzwa, George Augustine O'Doherty, Miaosheng Li
Abstract: A process of preparing a quinolone carboxylic acid or its derivatives having Formula I, Ia, or IV, as shown herein, comprises using a starting quinolone that already has one or more desired substituents at one or more particular positions on the quinolone ring and preserving the orientation of such substituents throughout the synthesis. The present process comprises fewer steps than prior-art processes. The present process also can include a simple separation of a desired enantiomer of the quinolone carboxylic acid or its derivatives from the enantiomeric mixture. Pharmaceutical compositions comprising fluoroquinolones prepared by the present process can be used effectively against a variety of microbial pathogens.
Abstract: 4-(3-Aminobenzoyl)-5-cyclopropylisoxazoles of the formula (I) are described as herbicides. In this formula (I), A, X, Y and Z are radicals such as hydrogen, organic radicals such as alkyl, and other radicals such as halogen.
Type:
Grant
Filed:
March 19, 2009
Date of Patent:
May 29, 2012
Assignee:
Bayer Cropscience AG
Inventors:
Heinz Kehne, Andreas Almsick, Hartmut Ahrens, Dieter Feucht, Ines Heinemann, Jan Dittgen, Martin Jeffrey Hills, Stefan Lehr, Christopher Hugh Rosinger
Abstract: The present application relates to novel substituted enaminocarbonyl compounds, to processes for their preparation and to their use for controlling animal pests, especially arthropods, in particular insects.
Type:
Grant
Filed:
March 19, 2007
Date of Patent:
December 27, 2011
Assignee:
Bayer Cropscience AG
Inventors:
Peter Jeschke, Robert Velten, Thomas Schenke, Otto Schallner, Michael Edmund Beck, Olga Malsam, Ralf Nauen, Thomas Müller, Christian Arnold, Erich Sanwald, Ulrich Görgens
Abstract: There is provided compounds of formula I, wherein A, X1, X2, X3, X4, Y1, Y2, Y3, Y4, Z1, Z2, R4 and R5 have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful as selective agonists of the AT2 receptor, and thus, in particular, in the treatment of inter alia gastrointestinal conditions, such as dyspepsia, IBS and MOF, and cardiovascular disorders.
Type:
Grant
Filed:
April 12, 2006
Date of Patent:
December 20, 2011
Assignee:
Vicore Pharma AB
Inventors:
Mathias Alterman, Anders Hallberg, Xiongyu Wu
Abstract: The present invention relates to diphenylmethyl imidazole mineralocorticoid receptor modulators compounds having the structure and their use in treating cardiovascular events.
Type:
Grant
Filed:
March 19, 2008
Date of Patent:
November 22, 2011
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Philip E. Brandish, James C. Hershey, Mark E. Fraley, Justin T. Steen
Abstract: Disclosed herein is at least one cyclopropyl amide derivative, at least one pharmaceutical composition comprising at least one cyclopropyl amide derivative disclosed herein, and at least one method of using at least one cyclopropyl amide derivative disclosed herein for treating at least one histamine H3 receptor associated condition therewith.
Type:
Grant
Filed:
August 21, 2008
Date of Patent:
November 22, 2011
Assignee:
AstraZeneca AB
Inventors:
James Arnold, Todd Andrew Brugel, Scott Throner, Steven Wesolowski, Phil Edwards, Andrew Griffin, Thierry Groblewski, Denis Labrecque
Abstract: An ester compound represented by the formula (I): (wherein, R1 represents a C1-C3 alkyl group, a 2-propenyl group or a 2-propynyl group.) has excellent pest controlling activity and is useful as an active ingredient for a pest controlling agent.
Abstract: It is an object to provide a method for producing a 2-nitroimidazole derivative having an acyclic sugar chain in a side chain, which is suitable for production of a derivative having a radioisotope. A method for producing 1-(1-benzoyloxymethyl-2-hydroxyethyl)oxymethyl-2-nitroimidazole, characterized by reacting glycerin with a benzoylating agent to obtain 1-O-benzoylglycerin, reacting 1-O-benzoylglycerin with dimethoxymethane in the presence of a dehydrating agent to obtain 4-benzoyloxymethyl-1,3-dioxolane, and then reacting this product with 2-nitroimidazole or 2-nitro-1-trialkylsilylimidazole in the presence of a Lewis acid.
Abstract: Disclosed herein is a method for reducing the rate of degradation of proteins in an animal, comprising contacting cells of the animal with certain boronic ester and acid compounds. Also disclosed herein are novel boronic ester and acid compounds, their synthesis and uses.
Type:
Grant
Filed:
April 1, 2009
Date of Patent:
August 23, 2011
Assignee:
Millennium Pharmaceuticals, Inc.
Inventors:
Julian Adams, Yu-Ting Ma, Ross L. Stein, Matthew Baevsky, Louis Grenier, Louis Plamondon
Abstract: Solid forms of (1R,2S,3R)-1-(2-(isoxazol-3-yl)-1H-imidazol-4-yl)butane-1,2,3,4-tetraol and hydrates thereof are disclosed, as well as compositions comprising them and methods of their use.
Type:
Grant
Filed:
June 16, 2009
Date of Patent:
August 16, 2011
Assignee:
Lexicon Pharmaceuticals, Inc.
Inventors:
Hugh Alfred Burgoon, Suzanne Marie Buttar, Christopher Stephen Frampton
Abstract: Compounds, compositions and methods for modulating the activity of nuclear receptors are provided. In particular, heterocyclic compounds are provided for modulating the activity of nuclear receptors, including liver X receptor (LXR) and orphan nuclear receptors. In certain embodiments, the compounds are N-substituted pyridones.
Type:
Grant
Filed:
December 20, 2002
Date of Patent:
August 16, 2011
Assignee:
Exelixis Patent Company LLC
Inventors:
Christopher D. Bayne, Alan T. Johnson, Shao-Po Lu, Raju Mohan, Ronald C. Griffith
Abstract: The present invention relates to a process for preparing fluoromethyl-substituted heterocyclic compounds of the general formula (I) in which R1 is H or F; R2 is an -[A-O]m—R3 group in which A is C2-C4-alkanediyl, R3 is C1-C4-alkyl and m is 1 or 2; by converting the corresponding chloromethyl-substituted compounds (II) in the presence of fluorinating agents, to processes for preparing the chloromethyl-substituted compounds (II), to processes for preparing amides of the general formula (IV) and to compounds of the general formulae (I) and (II).
Abstract: The present invention provides a compound of the formula: Formula (I) or a pharmaceutically acceptable salt thereof; pharmaceutical compositions comprising a compound of Formula (I) in combination with a suitable carrier, diluent, or excipient; and methods for treating physiological disorders, particularly reduced bones mass, osteoporosis, osteopenia, or reduced muscle mass or strength, comprising administering a compound of Formula (I), or a pharmaceutically acceptable salt thereof. X-17142.
Type:
Grant
Filed:
November 6, 2007
Date of Patent:
June 28, 2011
Assignee:
Eli Lilly and Company
Inventors:
Konstantinos Gavardinas, Jonathan Edward Green, Prabhakar Kondaji Jadhav, Donald Paul Matthews
Abstract: The present invention is directed to novel imidazolidin-2-one derivatives having a structure according to Formula I wherein a, b, R1, R2, R3, and R4 are as defined above, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the androgen receptor.
Abstract: The present invention provides a process for producing N,N?-carbonyldiimidazole, comprising: reacting phosgene, diphosgene, or triphosgene with imidazole in an inert solvent to produce N,N?-carbonyldiimidazole; to imidazole hydrochloride yielded as a by-product in the above step, adding a gaseous or liquid basic compound represented by the below-shown general formula (1) in an inert solvent to conduct neutralization reaction; and circulating the imidazole thus generated to use it as a starting material for N,N?-carbonyldiimidazole production. In the general formula (1), R1, R2, and R3 each independently represents a hydrogen atom, a methyl group, or an ethyl group. The CDI produced by the production process of the invention is a compound useful in the fields of synthesis of pharmaceutical agents, synthesis of agricultural chemicals, peptide synthesis, and the like, e.g.
Abstract: A compound having the formula wherein R1, Z, and the carbonyl can be comprised by a common ring, wherein R1 comprises a chromophore that absorbs light from the visible wavelength range, and wherein n is an integer of at least 12. A solid phase change ink composition is also disclosed containing a colorant comprising a chromophore that absorbs light from the visible wavelength range and has the formula wherein R1, Z, and the carbonyl can be comprised by a common ring, and wherein n is an integer of at least 12. Also disclosed is a method of forming a colorant wherein a first compound having the formula is reacted with a second compound having the formula Z(CH2)nCH3 wherein n is an integer of at least 12 to form a third compound having the formula wherein the third compound comprises a chromophore that absorbs light from the visible wavelength range.
Type:
Grant
Filed:
December 14, 2007
Date of Patent:
May 10, 2011
Assignee:
Xerox Corporation
Inventors:
Jeffrey H Banning, Clifford R King, Donald R Titterington, Michael B Meinhardt