Abstract: The present invention embraces compounds selected for interacting with the Fingers-Palm pocket of telomerase and use thereof for modulating the activity of telomerase and preventing or treating diseases or conditions associated with telomerase.
Abstract: The present invention relates to a method for preparing 1-(2-aminoethyl)imidazolidin-2-one or the thiocarbonyl thereof, and also to the product that can be obtained according to this method, and which has a purity of at least 98%, and to the uses thereof.
Abstract: There is provided a halogen-containing organosulfur compound having a controlling effect on arthropod pests represented by the formula (I): wherein m represents 0, 1 or 2; n represents 0, 1 or 2; A represents an optionally substituted 3- to 8-membered saturated heterocyclic group; Q represents a fluorine atom or a C1-C5 haloalkyl group having at least one fluorine atom; R1, R1a and R3 independently represent an optionally halogenated C1-C4 chain hydrocarbon group, etc.; R2, R2a and R4 independently represent an optionally halogenated C1-C4 chain hydrocarbon group, etc.
Abstract: This invention relates to use of inhibitors of the transforming growth factor-? (TGF-?) type I receptor (ALK5) and/or the activin type I receptor (ALK4) in treating, preventing, or reducing fibrosis, cancer, and vascular injuries.
Type:
Grant
Filed:
June 24, 2011
Date of Patent:
August 20, 2013
Assignee:
EWHA University—Industry Collaboration Foundation
Inventors:
Dae-Kee Kim, Yhun Yhong Sheen, Chenghua Jin, Chul-Yong Park, Domalapally Sreenu, Kota Sudhakar Rao, Maddeboina Krishnaiah, Vura Bala Subrahmanyam
Abstract: The present invention relates to pyrrolidine-2,5-dione compounds, and methods of preparation of these compounds. The present invention also relates to pharmaceutical compositions comprising pyrrolidine-2,5-dione compounds. The present invention provides methods of treating a cell proliferative disorder, such as a cancer, by administering to a subject in need thereof a therapeutically effective amount of a compound or pyrrolidine-2,5-dione compound of the present invention.
Type:
Grant
Filed:
June 19, 2008
Date of Patent:
August 20, 2013
Assignee:
ArQule, Inc.
Inventors:
Neil Westlund, Jason Hill, Mark A. Ashwell, Nivedita Namdev, Jianqiang Wang, Syed Ali
Abstract: The invention provides novel compounds having the general formula (I) wherein R1, R2, A, E, G and n are as described herein, compositions including the compounds and methods of using the compounds. The compounds are useful as inhibitors of hormone sensitive lipase (HSL) and may be used for the treatment of diabetes, metabolic syndrome, dyslipidemia, atherosclerosis, obesity, cardiovascular diseases, myocardial dysfunction, inflammation, non-alcoholic fatty liver disease or non-alcoholic steatohepatitis.
Type:
Grant
Filed:
May 4, 2012
Date of Patent:
August 6, 2013
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Aurelia Conte, Daniel Hunziker, Werner Neidhart, Matthias Nettekoven, Tanja Schulz-Gasch
Abstract: An inexpensive and industrially advantageous method for producing optically active syn-3-(N-substituted-aminomethyl)-4-fluoropyrrolidine which may be an intermediate for producing pharmaceuticals is provided. The present invention relates a method for producing a syn-1-protected-4-fluoro-3-(N-substituted-N-nitrobenzenesulfonyl)pyrrolidine derivative or it's enantiomer, or their salts comprising the process of fluorinating a compound represented by the general formula (6) (in the formula, PG1 represents a protecting group for an amino group, R1 represents a C1 to C6 alkyl group which may be substituted or a C3 to C8 cycloalkyl group which may be substituted, and Ns represents a 2-nitrobenzenesulfonyl group or a 4-nitrobenzenesulfonyl group) or it's enantiomer using a nucleophilic fluorinating agent and an organic base having an amidine or guanidine structure.
Abstract: The invention is directed to a compound of Formula (I), wherein R is selected from the group consisting of hydrogen atom and unsubstituted or substituted phenyl group; R1 is selected from the group consisting of hydrogen atom and unsubstituted or substituted phenyl group; X is selected from the group consisting of hydrogen atom or halogen atom; and Y is selected from the group consisting of hydrogen atom, halogen atom, C1-C4 alkyl group, nitro group, and —OCF3 group, as well as for its use in therapy, preferably for the treatment of cancer, and to a related pharmaceutical composition, the use of the compound for the manufacture of a medicament for the respective medical indication, and a method of synthesis of the compounds of the invention.
Abstract: Substituted indole compounds corresponding to the formula I: In which R8, R9a, R9b, R10, R11, R200, R210, A, D, T, q, s and t have defined meanings, processes for the preparation thereof, pharmaceutical compositions containing such compounds and the use of substituted indole compounds for the treatment or inhibition of pain and other conditions which are at least partly mediated by Bradykinin 1 receptors (B1R).
Type:
Grant
Filed:
February 3, 2010
Date of Patent:
July 23, 2013
Assignee:
Gruenenthal GmbH
Inventors:
Stefan Schunk, Melanie Reich, Michael Engels, Tieno Germann, Ruth Jostock, Sabine Hees
Abstract: The present invention relates to compounds of formula I: methods of their use, processes for their preparation and isolated actinomycetes strains capable of preparing pyrrolo[4,3,2-de]quinolin-8-amine compounds.
Type:
Grant
Filed:
August 12, 2009
Date of Patent:
July 16, 2013
Assignee:
Wyeth LLC
Inventors:
Min He, Jeffrey Edwin Janso, Ker Yu, Leonard Alexander McDonald, Laurel Rita Barbieri, Ariamala Gopalsamy
Abstract: The present invention relates to the field of drugs associated with treating diabetes. Particularly, the present invention relates to a dipeptidyl peptidase-IV inhibitor having the structure shown by formula (I), which contains amide thiazole structure and has an effect on treating diabetes, and a preparation method and a pharmaceutical composition containing it, as well as use thereof in manufacture of the drugs for treating the diabetes, wherein, R1 is methyl; R2 is phenyl; phenyl, 2-thienyl substituted in a mono-substituted, bi-substituted manner by fluorine and methyl.
Type:
Grant
Filed:
June 16, 2011
Date of Patent:
July 9, 2013
Assignee:
Tianjin Institute of Pharmaceutical Research
Abstract: In its many embodiments, the present invention provides a novel class of chroman compounds of formula I as ?2C adrenergic receptor agonists, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of prepaxing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the ?2C adrenergic receptors using such compounds or pharmaceutical compositions. wherein J is: Z is —[C(Rc)(Rc)]x—, where x is 1, 2, or 3.
Type:
Grant
Filed:
February 11, 2008
Date of Patent:
June 25, 2013
Assignee:
Merck Sharp & Dohme, Corp.
Inventors:
Junying Zheng, Kevin D. McCormick, Jianhua Chao, Christopher W. Boyce, Robert G. Aslanian, Younong Yu
Abstract: Compounds of the general formulae (1) and (2) A-B-D-B?-A???(1) and A-B-D-E??(2) in which A and A? may be identical or different and are the residue in which X is S, O, CH2, CH2CH2, CH2O or CH2NH, and Y is H or CN, and * designates a chiral carbon atom preferably in S- or L-configuration; B and B? may be identical or different and are an O, N or S containing or non-containing, unsubstituted or substituted, unbranched or branched alkylene residue, cycloalkylene residue, aralkylene residue, heterocycloalkylene residue, heteroarylalkylene residue, arylamidoalkylene residue, heteroarylamidoalkylene residue, unsubstituted or mono- or poly-substituted arylene residue or heteroarylene residue having one or more five-, six- or seven-membered ring(s); D is —S—S— or —Se—Se—; and E is the group —CH2—CH(NH2)—R9 or —CH2—*CH(NH2)—R9 respectively in which R9 is an O, N or S containing or non-containing, unsubstituted or substituted, unbranched or branched alkyl residue, cycloalkyl residue, aralkyl residu
Type:
Grant
Filed:
November 10, 2006
Date of Patent:
June 25, 2013
Assignee:
IMTM GmbH
Inventors:
Siegfried Ansorge, Klaus Neubert, Ute Bank, Irene Reichstein, Jürgen Faust, Michael Täger, Petra Fuchs, Bianca Senns
Abstract: The present invention relates to imidazole derivatives having vinyl group represented by general formula (I) which possess electron transporting character, have a high glass transition temperature (Tg), and high decomposition temperature (Td): wherein all symbols are defined as recited in the specification. The present invention also relates to a use of the imidazole derivatives having vinyl group as a guest emitter or electron transporter in luminescent elements.
Type:
Grant
Filed:
February 3, 2012
Date of Patent:
June 25, 2013
Assignee:
Industrial Technology Research Institute
Abstract: The present invention provides processes for the stereoselective synthesis of 6-alpha-amino morphinans. In particular, the invention provides processes for the reductive amination of 6-keto normorphinans by catalytic transfer hydrogenation.
Type:
Grant
Filed:
June 10, 2010
Date of Patent:
June 25, 2013
Assignee:
Mallinckrodt LLC
Inventors:
Christopher W. Grote, Gary L. Cantrell, Joseph P. McClurg, Catherine E. Thomasson, Frank W. Moser
Abstract: Processes and intermediates are provided for the preparation of substituted aminomethyl 2,3,8,9-tetrahydiO-7H-1,4-dioxino[2.3-e]indo]-8-ones of the Formula (A) wherein the variables n, R and R3 are as described herein. Such compounds are useful, for example, as dopamine receptor agonists.
Type:
Grant
Filed:
March 26, 2008
Date of Patent:
June 18, 2013
Assignee:
Ligand Pharmaceuticals
Inventors:
Zhe-qing Wang, Andrew Staab, Christopher Seekamp, George P. Luke
Abstract: Compounds that are useful in treating or preventing viral infections, such as influenza, are described herein. Further described are compositions made from these compounds and methods for using the compounds and their compositions in treating or preventing viral infections.
Abstract: 1-aza-3,7-dioxabicyclo[3.3.0]octane compounds, process for their preparation, their use as pro-fragrances, and washing and cleaning compositions, fabric softeners and cosmetics comprising them, and a process for prolonging the odor perception of such compositions.
Type:
Grant
Filed:
July 17, 2008
Date of Patent:
June 18, 2013
Assignee:
Henkel AG & Co. KGaA
Inventors:
Ursula Huchel, Silvia Sauf, Thomas Gerke
Abstract: The present invention relates to a novel cocrystal compound of 5-chloro-N-({(5S)-2-oxo-3-[4-(3-oxo-4-morpholinyl)phenyl]-1,3-oxazolidin-5-yl}methyl)-2-thiophenecarboxamide (rivaroxaban) and malonic acid, to processes for its preparation, to medicaments comprising this compound and to their use for controlling diseases.
Type:
Grant
Filed:
June 3, 2009
Date of Patent:
June 18, 2013
Assignee:
Bayer Intellectual Property GmbH
Inventors:
Alfons Grunenberg, Karsten Fähnrich, Olaf Queckenberg, Christiane Reute, Birgit Keil, Karen Sue Gushurst, Ezra John Still
Abstract: The invention provides novel, multiply-substituted 1-aryl-3-azabicyclo[3.1.0]hexanes, and related processes and intermediates for preparing these compounds, as well as compositions and methods employing these compounds for the treatment and/or prevention of central nervous system (CNS) disorders, including depression and anxiety.
Type:
Grant
Filed:
February 3, 2012
Date of Patent:
June 11, 2013
Inventors:
Phil Skolnick, Anthony Basile, Zhengming Chen, Joseph W. Epstein