Abstract: A novel camphor-derived ?-amino alcohol compound is disclosed. The novel camphor-derived ?-amino alcohol compound can be used in asymmetric addition of organozinc to aromatic and aliphatic aldehydes, including linear aliphatic ones, thus generating corresponding secondary alcohols in high yields and enantiomeric excess.
Abstract: The present invention provides compounds, pharmaceutical compositions and methods for treating, immuno-allergical diseases, autoimmune diseases, and organ or tissue rejection following transplantation.
Abstract: A novel sulfur containing heteroaryl-pyrazole compound of formula (I) or a pharmaceutically acceptable salt thereof is effective as a cannabinoid CB1 receptor inverse agonist or antagonist, which is useful for preventing or treating obesity and obesity-related metabolic disorders. The prevention also provide a method for preparing same, a pharmaceutical composition containing same, and a method for preventing or treating obesity and obesity-related metabolic disorders.
Type:
Grant
Filed:
September 25, 2008
Date of Patent:
November 13, 2012
Assignee:
Green Cross Corporation
Inventors:
Jinhwa Lee, Hee Jeong Seo, Min-Ah Kim, Jeongmin Kim, Sung-Han Lee, Myung Eun Jung, Mi-Soon Kim
Abstract: Compounds of formula Ia and Ib and wherein A, B, C and R1 are described herein.
Type:
Grant
Filed:
June 10, 2010
Date of Patent:
November 6, 2012
Assignee:
Bristol-Myers Squibb Company
Inventors:
Mark E. Salvati, Heather Finlay, Bang-Chi Chen, Lalgudi S. Harikrishnan, Ji Jiang, James A. Johnson, Muthoni G. Kamau, R. Michael Lawrence, Jianqing Li, John Lloyd, Michael M. Miller, Zulan Pi, Jennifer X. Qiao, Richard A. Rampulla, Jacques Y. Roberge, Tammy C. Wang, Yufeng Wang, Wu Yang
Abstract: The present invention relates to pyrrolidin-2-one, pyrrolidin-2,5-dione, pyrrolidine and thiosucciniroide compounds of formulae (I)-(IV), and methods of preparation of these compounds. The present invention also relates to pharmaceutical compositions comprising pyrrolidin-2-one, pyrrolidin-2,5-dione, pyrrolidine and thiosuccinimide 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 of pyrrolidin-2-one, pyrrolidin-2,5-dione, pyrrolidine and thiosuccinimide compound of the present invention.
Type:
Grant
Filed:
June 19, 2008
Date of Patent:
November 6, 2012
Assignee:
ArQule, Inc.
Inventors:
Jianqiang Wang, Syed M. Ali, Eugene Kelleher, Yanbin Liu, Jason Hill, Mark A. Ashwell
Abstract: The invention relates to novel arylpyrroline compounds of formula (I) which having excellent insecticidal activity and which can thus be used as an insecticide is provided.
Abstract: The present application relates to novel 4-cycloalkyl- and 4-heterocycloalkyl-3,5-dicyano-2-thio-pyridine derivatives, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, preferably for the treatment and/or prevention of hypertension and other cardiovascular disorders.
Type:
Grant
Filed:
November 17, 2007
Date of Patent:
November 6, 2012
Assignee:
Bayer Intellectual Property GmbH
Inventors:
Peter Nell, Walter Hübsch, Barbara Albrecht-Küpper, Alexandros Vakalopoulos, Frank Süssmeier, Jörg Keldenich, Joachim Telser
Abstract: A compound represented by the following formula (DII): wherein Y31, Y32 and Y33 each independently represents a methine group or a nitrogen atom; R31, R32 and R33 each independently represents the following formula (DII-R):
Abstract: The present invention relates to novel inhibitors of Factors VIIa, IXa, Xa, XIa, in particular Factor VIIa, pharmaceutical compositions comprising these inhibitors, and methods for using these inhibitors for treating or preventing thromboembolic disorders, cancer or rheumatoid arthritis. Processes for preparing these inhibitors are also disclosed.
Type:
Grant
Filed:
May 3, 2011
Date of Patent:
October 30, 2012
Assignee:
Pharmacyclics, Inc.
Inventors:
Aleksandr Kolesnikov, Roopa Rai, William Dvorak Shrader, Steven M. Torkelson, Kieron E. Wesson, Wendy B. Young
Abstract: A compound represented by the formula (1): wherein Ar represents an aromatic hydrocarbon group having 6 to 20 carbon atoms which may have a substituent, Ar? represents an aromatic hydrocarbon group having 6 to 20 carbon atoms which may have a substituent, and R represents an alkyl group having 1 to 4 carbon atoms.
Abstract: The invention relates to compounds of formula (I) having pharmacological activity towards the sigma receptor, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use for the treatment and or prophylaxis of a disease in which the sigma receptor is involved.
Type:
Grant
Filed:
February 9, 2010
Date of Patent:
October 23, 2012
Assignee:
Laboratories Del Dr. Esteve, S.A.
Inventors:
Christian Laggner, Maria Rosa Cuberes-Altisent, Joerg Holenz, Juana Maria Berrocal-Romero, Maria Montserrat Contijoch-Llobet
Abstract: Neutral antagonists of the CB1 cannabinoid receptor, means for identifying neutral antagonists of the CB1 cannabinoid receptor, and uses thereof. Antagonists of the CB1 cannabinoid receptor can be used to prevent, treat or reduce the severity of various medical conditions and symptoms, including, but not limited to obesity, appetite disorder, another metabolic disorder, drug addiction and/or mental illness. Administering neutral CB1 cannabinoid receptor antagonists in place of or in combination with known CB1 cannabinoid receptor antagonists or inverse CB1 cannabinoid receptor agonists in an individual or animal to treat a medical condition with a reduction of unwanted side effects.
Type:
Grant
Filed:
June 11, 2008
Date of Patent:
October 23, 2012
Assignee:
MAKScientific, LLC
Inventors:
Alexandros Makriyannis, Venkata K Vemuri
Abstract: The invention relates to compounds that have an affinity to the ?-opioid receptor and the ORL 1-receptor, methods for their production, medications containing these compounds and the use of these compounds for the treatment of pain and other conditions.
Type:
Grant
Filed:
March 25, 2009
Date of Patent:
October 23, 2012
Assignee:
Grunenthal GmbH
Inventors:
Saskia Zemolka, Bert Nolte, Sven Frormann, Claudia Hinze, Klaus Linz, Wolfgang Schröder, Werner Englberger, Hans Schick, Helmut Sonnenschein
Abstract: The invention relates to novel substituted 3-phenylamino-5-(3-aminophenyl)pyridines and corresponding pyrazines of formula (I), wherein A is CH or N, R1 represents C(?O)R9, S(?O)2R10, P(?O)(OR11)2, optionally substituted phenyl or optionally substituted heteroaryl, and the other substituents have the meaning described in the specification, processes for the preparation thereof, pharmaceutical compositions containing same, the use thereof optionally in combination with one or more other pharmaceutically active compounds for the therapy of neoplastic diseases and autoimmune diseases, and a method for the treatment of such a diseases.
Type:
Grant
Filed:
September 5, 2005
Date of Patent:
October 16, 2012
Assignee:
Basilea Pharmaceutica AG
Inventors:
Martin Eberle, Felix Bachmann, Alessandro Strebel, Subho Roy, Goutam Saha, Godhuli Nandi
Abstract: There are described N-(1,2,5-oxadiazol-3-yl)benzamides of the general formula (I) as herbicides. In this formula (I), X, Y, Z and R are radicals such as hydrogen, organic radicals such as alkyl, and other radicals such as halogen.
Type:
Grant
Filed:
September 23, 2010
Date of Patent:
October 16, 2012
Assignee:
Bayer Cropscience AG
Inventors:
Arnim Köhn, Jörg Tiebes, Andreas Almsick, Hartmut Ahrens, Ines Heinemann, Ralf Braun, Monika H Schmitt, Lothar Willms, Dieter Feucht, Christopher Hugh Rosinger, Isolde Häuser-Hahn, Mark Drewes, Simon Dörner-Rieping, Jan Dittgen, Martin Adamczewski
Abstract: The invention concerns tricyclic N-heteroaryl-carboxamide derivatives containing a benzimidazole unit of general formula (I): Wherein A, P, Y, R1, R2 and R3 are as defined herein. The invention also concerns a method of preparing the compounds and their therapeutic use.
Type:
Grant
Filed:
January 24, 2012
Date of Patent:
October 16, 2012
Assignee:
Sanofi
Inventors:
Laurent Dubois, Yannick Evanno, Luc Even, Catherine Gille, Andre Malanda, David Machnik, Nathalie Rakotoarisoa
Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, or a pharmaceutically acceptable salt thereof, wherein all of the variables are as defined herein. These compounds are GPR40 G protein-coupled receptor modulators which may be used as medicaments.
Type:
Grant
Filed:
October 5, 2010
Date of Patent:
October 16, 2012
Assignee:
Bristol-Myers Squibb Company
Inventors:
Bruce A. Ellsworth, William R. Ewing, Elizabeth Jurica
Abstract: Potent and selective ligands for the dopamine 3 (D3) receptor are disclosed. The D3 receptor ligands have a structural formula (I) wherein X is C?O or SO2, R1 is C1-6 alkyl, R2 is aryl, heteroaryl, aryl, —(CH2)1-3aryl, or —(CH2)1-3heteroaryl, and n is 0 or 1. Methods of using the D3 receptor ligands in the treatment of diseases and conditions wherein modulation of the D3 receptor provides a benefit also are disclosed.
Type:
Grant
Filed:
August 27, 2009
Date of Patent:
October 9, 2012
Assignee:
The Regents of the University of Michigan
Inventors:
Shaomeng Wang, Jianyong Chen, Gregory Collins, James H. Woods, Beth Levant
Abstract: The present invention relates to compounds of formula (I), combinations and uses thereof for disease therapy, R1 represents heteroaryl, -carbocyclyl-heteroaryl, -alkenylheteroaryl or -alkylheteroaryl; R2 represents hydrogen; halogen; alkenyl; alkynyl; -alkenylaryl; -alkenylheteroaryl; alkyl, which may optionally be substituted by one or more groups selected from halogen, hydroxyl, alkoxy-, -thioalkyl, —C(O)OH and —C(O)O-alkyl; carbocyclyl, which may optionally be substituted by one or more groups selected from alkyl, halogen, hydroxyl, alkoxy-, -thioalkyl, —C(O)OH and —C(O)O-alkyl; -alkylcarbocyclyl; -alkylheterocyclyl; aryl; heteroaryl; heterocyclyl; -alkylaryl; -alkyl(aryl)2, -alkylheteroaryl; -aryl-heteroaryl; -heterocyclyl-aryl; -aryl-aryl; -heteroaryl-aryl; -heteroaryl-heteroaryl, and —C(O)R4; R3 represents halogen; alkyl optionally substituted by one or more groups selected from halogen, hydroxyl, alkoxy, thioalkyl, —C(O)OH and —C(O)O-alkyl; aryl; heteroaryl; —C(O)R5; R4 and R5 independently repre
Type:
Grant
Filed:
November 8, 2007
Date of Patent:
October 2, 2012
Assignee:
Probiodrug AG
Inventors:
Michael Thormann, Michael Altmstetter, Andreas Treml, Ulrich Heiser, Mirko Buchholz, Andre J. Niestroj
Abstract: ?- and ?-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
Type:
Grant
Filed:
September 21, 2011
Date of Patent:
November 13, 2012
Assignee:
G.D. Searle LLC
Inventors:
Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, John N. Freskos, Deborah E. Bertenshaw, Robert M. Heintz