Abstract: Provided herein are novel compounds that inhibit ribonucleotide reductase (RR) by binding to RRM2 and interfering with the activity of the RRM1/RRM2 holoenzyme. These inhibitors may be used to inhibit RR activity and to treat various conditions associated with RRM2 expression, such as for example certain cancer types, mitochondrial diseases, or degenerative diseases.
Type:
Grant
Filed:
April 25, 2011
Date of Patent:
April 24, 2012
Assignee:
City of Hope
Inventors:
Yun Yen, David Horne, Yate-Ching Yuan, Bing-Sen Zhou, Angela L Perkins Harki, Leila Su
Abstract: The present invention provides novel substituted isoxazole compounds, pharmaceutical compositions, therapeutic uses and processes for preparing the same.
Type:
Grant
Filed:
March 9, 2010
Date of Patent:
April 17, 2012
Assignee:
GlaxoSmithKline LLC
Inventors:
Richard Caldwell, David Norman Deaton, Robert Blount McFadyen, Frank Navas, III, Paul Kenneth Spearing
Abstract: Compounds of formula I: wherein R1, R2, R3, R4, R5, R6, R7, R8, R9 and n are as defined in the description, processes for the preparing the compounds, new intermediates employed in the preparation, pharmaceutical compositions containing the compounds, and uses of the compounds in therapy.
Type:
Grant
Filed:
August 23, 2010
Date of Patent:
April 10, 2012
Assignee:
AstraZeneca AB
Inventors:
Bradford Van Wagenen, Radhakrishnan Ukkiramapandian, Joshua Clayton, Ian Egle, James R. Empfield, Methvin Isaac, Fupeng Ma, Abdelmalik Slassi, Gary Steelman, Rebecca Urbanek, Sally Walsh
Abstract: The invention relates to a process for preparing an amino nitrile mixture comprising aminoacetonitrile (AAN) and from 5 to 70% by weight of iminodiacetonitrile (IDAN), which comprises heating crude AAN which is largely free of formaldehyde cyanohydrin (FACH-free) at a temperature of from 50 to 150° C.
Type:
Grant
Filed:
February 28, 2008
Date of Patent:
April 10, 2012
Assignee:
BASF SE
Inventors:
Alfred Oftring, Kirsten Dahmen, Thilo Hahn, Randolf Hugo, Katrin Baumann, Johann-Peter Melder
Abstract: The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.
Type:
Grant
Filed:
June 23, 2011
Date of Patent:
April 3, 2012
Assignee:
Bristol-Myers Squibb Company
Inventors:
Kap-Sun Yeung, Kyle E. Parcella, John A. Bender, Brett R. Beno, Katharine A. Grant-Young, Ying Han, Piyasena Hewawasam, John F. Kadow, Andrew Nickel
Abstract: Compounds of formula I: (wherein variables A1, A2, B, m, n, J, X, R4, G1, G2, G3 and Y are as described herein) which are antagonists of CGRP receptors and which are useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.
Type:
Grant
Filed:
April 11, 2008
Date of Patent:
March 27, 2012
Assignee:
Merck, Sharp & Dohme Corp
Inventors:
Ian M. Bell, Harold G. Selnick, Craig A. Stump
Abstract: The presently disclosed subject matter provides compositions that selectively bind cyclooxygenase-2 and comprise a therapeutic and/or diagnostic moiety. Also provided are methods for using the disclosed compositions for diagnosing (i.e., by imaging) a target cell and/or treating a disorder associated with a cyclooxygenase-2 biological activity.
Type:
Grant
Filed:
June 11, 2010
Date of Patent:
March 27, 2012
Assignee:
Vanderbilt University
Inventors:
Lawrence J. Marnett, Md. Jashim Uddin, Brenda C. Crews
Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein A, B, L, Q, R1, R2, and R3 are defined herein.
Type:
Grant
Filed:
August 11, 2009
Date of Patent:
March 27, 2012
Assignee:
Janssen Pharmaceutica, NV
Inventors:
Raymond W. Colburn, Scott L. Dax, Christopher M. Flores, Donald W. Ludovici, Jay M. Matthews, Mingde Xia, Xiaoqing Xu, Mark A. Youngman, Bin Zhu
Abstract: N-Thio-anthranilamid compounds of formula (I) wherein A is a group selected from A1 and A2 wherein the variables and the indices are as defined per the description, processes for preparing the compounds I, pesticidal compositions comprising compounds I, use of compounds I for the control of insects, acarids or nematodes, and methods for treating, controlling, preventing or protecting animals against infestation or infection by parasites by use of compounds of formula I.
Type:
Grant
Filed:
June 30, 2006
Date of Patent:
March 27, 2012
Assignee:
BASF SE
Inventors:
Thomas Schmidt, Michael Puhl, Joachim Dickhaut, Henricus Maria Martinus Bastiaans, Michael Rack, Deborah L. Culbertson, Douglas D. Anspaugh, Franz-Josef Braun, Toni Bucci, Henry Van Tuyl Cotter, David G. Kuhn, Hassan Oloumi-Sadeghi
Abstract: The present invention relates to compounds of formula I, The compounds of formula I are valuable pharmacologically active compounds. They exhibit a strong anti-thrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardio-vascular disorders like thromboembolic diseases or restenoses. They are inhibitors of the blood clotting enzymes, especially factor VIIa and can in general be applied in conditions in which an undesired activity of factor VIIa is present or for the cure or prevention of which an inhibition of factor VIIa is intended. The invention furthermore relates to processes for the preparation of compounds of formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.
Type:
Grant
Filed:
January 7, 2010
Date of Patent:
March 27, 2012
Assignee:
Sanofi-Aventis
Inventors:
Henning Steinhagen, Hauke Szillat, Markus Follmann, Reinhard Kirsch, Volkmar Wehner, Hans Matter, Martin Lorenz, Kent W. Neuenschwander, Anthony C. Scotese
Abstract: The invention relates to compounds and their use in the treatment of thrombocytopenia resulting from diseases or conditions such as immune thrombocytopenic purpura, cancer chemotherapy, surgery, bone marrow or stem cell transplantation, radiation injury or treatment, chronic viral infection, and pancytopenia. The invention further relates to pharmaceutical compositions containing the compounds and compositions of the invention as well as methods for treating such diseases or conditions in a mammal, including a human, by administering to such mammal an effective amount of a selected thrombopoietin receptor agonist.
Abstract: A process for the preparation of a compound of formula (Ia): which are useful as intermediates in the preparation of i.a. pharmaceutically active compounds.
Type:
Grant
Filed:
March 31, 2009
Date of Patent:
March 27, 2012
Assignee:
Hoffmann-LA Roche Inc.
Inventors:
Gerard John Harnett, Ursula Hoffmann, Michael Jansen, Reinhard Reents, Tim Sattelkau, Dennis A. Smith, Helmut Stahr
Abstract: An isoxazole derivative is provided. The isoxazole derivative has following formula: wherein R1, R2, R3, R4 and R5, independently, include hydrogen, hydroxy or C1-C12 alkoxy optionally substituted with oxirane, thiirane, aziridine, amino, cycloamino, aminohydroxy or cycloaminohydroxy. The invention also provides a pharmaceutical composition for treatment of osteoporosis and cancer including an isoxazole derivative or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier.
Abstract: The invention relates to novel thiophene derivatives, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunomodulating agents.
Type:
Grant
Filed:
July 10, 2007
Date of Patent:
March 13, 2012
Assignee:
Actelion Pharmaceuticals Ltd.
Inventors:
Martin Bolli, David Lehmann, Boris Mathys, Claus Mueller, Oliver Nayler, Beat Steiner, Jörg Velker
Abstract: The invention relates to 3,5-substituted piperidine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (=disorder) that depends on activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on activity of renin; the use of a compound of that class in the treatment of a disease that depends on activity of renin; pharmaceutical formulations comprising a 3,5-substituted piperidine compound, and/or a method of treatment comprising administering a 3,5-substituted piperidine compound, a method for the manufacture of a 3,5-substituted piperidine compound, and novel intermediates and partial steps for its synthesis. The compounds have the formula I? wherein R1, R2, T, R3 and R4 are as defined in the specification.
Abstract: Provided herein are isoindoline compounds, pharmaceutical compositions comprising one or more of such compounds, and methods of their use for treating, preventing, or managing various diseases.
Type:
Grant
Filed:
October 29, 2009
Date of Patent:
March 6, 2012
Assignee:
Celgene Corporation
Inventors:
George W. Muller, Alexander L. Ruchelman
Abstract: The present application relates to calcium channel inhibitors containing compounds of formula (I) wherein L1, L2, R1, R2, and R3 are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions.
Type:
Grant
Filed:
November 25, 2009
Date of Patent:
March 6, 2012
Assignee:
Abbott Laboratories
Inventors:
Andrew O. Stewart, Xenia B. Searle, Daria Darczak, Ming Clinton Yeung, Stanley DiDomenico
Abstract: Methods of using di, tri, and tetracyclic acylhydrazide derivatives and analogs, as well as pharmaceutical compositions containing the same, for the treatment or prophylaxis of viral infections and diseases associated therewith, particularly those viral infections and associated diseases caused by the orthopoxvirus.
Type:
Grant
Filed:
December 21, 2009
Date of Patent:
February 28, 2012
Assignee:
Siga Technologies, Inc.
Inventors:
Robert Jordan, Thomas R. Bailey, Susan R. Rippin
Abstract: Substituted sulfonamide compounds corresponding to formula I: a process for their preparation, pharmaceutical compositions comprising such compounds, and the use of such substituted sulfonamide compounds in pharmaceutical compositions for the treatment of pain or other disorders or diseases that are mediated at least in part by B1R receptors.
Type:
Grant
Filed:
April 8, 2009
Date of Patent:
February 28, 2012
Assignee:
Gruenenthal GmbH
Inventors:
Stefan Oberboersch, Melanie Reich, Stefan Schunk, Michael Engels, Ruth Jostock, Tieno Germann, Sabine Hees
Abstract: A compound having the following formula (III) wherein R2 is hydrogen, alkyl, cycloalkyl, phenyl or a 5- or 6-membered heterocyclic, and X is oxygen, sulfur or nitrogen, and a method for preparing said compound.