Abstract: The invention provides novel furoxan compounds, or pharmaceutically acceptable salts thereof, and novel compositions comprising at least one compound, and, optionally, at least one nitric oxide enhancing compound and/or at least one therapeutic agent. The compounds and compositions of the invention can also be bound to a matrix. The invention also provides methods for (a) treating cardiovascular diseases; (b) inhibiting platelet aggregation and platelet adhesion caused by the exposure of blood to a medical device; (c) treating pathological conditions resulting from abnormal cell proliferation; (d) treating transplantation rejections, (e) treating autoimmune, inflammatory, proliferative, hyperproliferative or vascular diseases; (f) reducing scar tissue or for inhibiting wound contraction; (g) treating diseases resulting from oxidative stress; (h) treating endothelial dysfunctions; and (j) treating diseases caused by endothelial dysfunctions.
Abstract: Compounds as modulators of peroxisome proliferator activated receptors, pharmaceutical compositions comprising the same, and methods of treating disease using the same are disclosed.
Type:
Grant
Filed:
September 4, 2008
Date of Patent:
November 16, 2010
Assignee:
Kalypsys, Inc
Inventors:
Stewart A. Noble, Guy Oshiro, James W. Malecha, Cunxiang Zhao, Carmen Robinson, Sergio G. Duron, Michael Sertic, Andrew K. Lindstrom, Andrew K. Shiau, Christopher D Bayne, Mehmet Kahraman, Boliang Lou, Steven P. Govek
Abstract: The present invention relates to isoxazoline derivatives, which can be used as selective inhibitors of phosphodiesterase (PDE) type IV. In particular, compounds disclosed herein can be useful in the treatment of AIDS, asthma, arthritis, bronchitis, chronic obstructive pulmonary disease (COPD), psoriasis, allergic rhinitis, shock, atopic dermatitis, Crohn's disease, adult respiratory distress syndrome (ARDS), eosinophilic granuloma, allergic conjunctivitis, osteoarthritis, ulcerative colitis and other inflammatory diseases in a patient, particularly in humans. The present invention also relates to processes for the preparation of disclosed compounds, as well as pharmaceutical compositions thereof, and their use as phosphodiesterase (PDE) type IV inhibitors.
Type:
Grant
Filed:
August 30, 2004
Date of Patent:
November 2, 2010
Assignee:
Ranbaxy Laboratories Limited
Inventors:
Venkata P. Palle, Sarala Balachandran, Mohammad Salman, Gagan Kukreja, Nidhi Gupta, Abhijit Ray, Sunanda G. Dastidar
Abstract: This invention relates to indazole compounds of formula (I) or (II) shown below. Each variable in formula (I) or (II) is defined in the specification. These compounds can be used to treat cancer.
Abstract: The present invention relates to a method of treatment and/or prophylaxis of a microbial infection, comprising the step of administering an effective amount of a compound of formula (I), in which X and Y are either the same or different and selected from a heteroatom; is a double or single bond depending on the heteroatoms X and Y; R1 to R5 are either the same or different and selected from hydrogen or a non-deleterious substituent; and R6 and R7 are either the same or different and selected from hydrogen and a non-deleterious substituent or one of R6 and R7 are absent when there is a double bond present, pharmaceutically acceptable salts or derivatives, pro-drugs, tautomers and/or isomers thereof. The present invention also relates to a method for protecting a subject from radiation damage, a method of cancer radiotherapy and use as an antimicrobial or radioprotective agent of the compound of formula (I) defined above.
Type:
Grant
Filed:
October 24, 2007
Date of Patent:
November 2, 2010
Assignee:
Biodiem Ltd
Inventors:
Peter Prokofievich Denisenko, Nickolay Sergeevich Sapronov, Alexander Alexandrovich Tarasenko
Abstract: Chemically reactive carbocyanine dyes that are intramolecularly crosslinked between the 1-position and 3?-position, their bioconjugates and their uses are described. 1,3?-crosslinked carbocyanines are superior to those of conjugates of spectrally similar 1,1?-crosslinked or non-crosslinked dyes. The invention includes derivative compounds having one or more benzo nitrogens.
Type:
Grant
Filed:
October 6, 2008
Date of Patent:
October 26, 2010
Assignee:
AnaSpec Incorporated
Inventors:
Zhenjun Diwu, Jianheng Zhang, Yi Tang, Xiang Guobing
Abstract: There are provided crystalline forms of the compounds Ph(3-Cl)(5-OCHF2)—(R)CH(OH)C(O)-Aze-Pab(OMe) and Ph(3-Cl)(5-OCHF2)—(R)CH(OH)C(O)-Aze-Pab(OH), pharmaceutical compositions containing them, processes for obtaining them and their use in medical treatment.
Type:
Grant
Filed:
December 5, 2007
Date of Patent:
October 26, 2010
Assignee:
AstraZeneca AB
Inventors:
Bengt Leonard Åslund, Stefan Bengtsson, Gudrun Anita Bergman, Ursula Renata Maria Hohlneicher, Bo Ingvar Ymén
Abstract: The present invention is directed to compounds of Formula I: Wherein R1, R2, Y, m and n are further defined in the description. The invention also relates to processes for the preparation of the compounds and to new intermediates employed in the preparation, pharmaceutical compositions containing the compounds, and to the use of the compounds in therapy.
Type:
Grant
Filed:
December 6, 2006
Date of Patent:
October 19, 2010
Assignee:
AstraZeneca AB
Inventors:
Abdelmalik Slassi, Methvin Isaac, Ian Egle, Fupeng Ma, Babu Joseph, Joshua Clayton, Krzysztof Swierczek
Abstract: The present invention relates to novel crystalline modifications of pyraclostrobin, to processes for their preparation and to the use of the novel modifications for preparing crop protection compositions.
Type:
Grant
Filed:
June 19, 2006
Date of Patent:
October 19, 2010
Assignee:
BASF Aktiengesellschaft
Inventors:
Hans Ziegler, Winfried Mayer, Thomas Kröhl, Karl-Heinrich Schneider, Gerhard Cox, Peter Erk, Uwe Josef Vogelbacher, Rainer Noack, Roland Götz, Jörg Wuckelt, Matthias Rauls
Abstract: The present invention relates to compounds with the formula (I), (II), (III) or (IV): wherein R1, R2, R3, R4, R5, R6, R7, X and Z are as defined herein, and also to pharmaceutical compositions comprising the compounds, as well as methods of use of the compounds for treatment of disorders associated with human 11-?-hydroxysteroid dehydrogenase type 1 enzyme and for the preparation of a medicament which acts on the human 11-?-hydroxysteroid dehydrogenase type 1 enzyme.
Type:
Grant
Filed:
June 28, 2007
Date of Patent:
October 5, 2010
Assignee:
Amgen Inc.
Inventors:
Martin Henriksson, Evert Homan, Lars Johansson, Jerk Vallgarda, Meredith Williams, Eric Bercot, Christopher H. Fotsch, Aiwen Li, Guolin Cai, Randall W. Hungate, Chester Chenguang Yuan, Christopher Tegley, David J. St. Jean, Jr., Nianhe Han, Qi Huang, Qingyian Liu, Michael D. Bartberger, George A. Moniz, Matthew J. Frizzle
Abstract: Compounds of formula (I) are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Also disclosed are pharmaceutical compositions comprising the histamine-3 receptor ligands and methods for using such compounds and compositions.
Type:
Grant
Filed:
January 29, 2008
Date of Patent:
October 5, 2010
Assignee:
Abbott Laboratories
Inventors:
Marlon D. Cowart, Yi-Yin Ku, Sou-Jen Chang, Dilinie P. Fernando, Timothy A. Grieme, Robert J. Altenbach
Abstract: The present invention relates to new substituted prolinamides of general formula (I) wherein D, L, E, G, J, M, R3, R4, R5 and R13 are defined as in the specification, the tautomers, the enantiomers, the diastereomers, the mixtures, and the salts thereof.
Type:
Grant
Filed:
May 16, 2007
Date of Patent:
October 5, 2010
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Kai Gerlach, Georg Dahmann, Herbert Nar, Roland Pfau, Henning Priepke, Annette Schuler-Metz, Wolfgang Wienen
Abstract: The present invention provides compounds of the formula: or pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein p, Ar, R1, R2, R3, Ra, Rb, Rc, Rd and Re are defined herein. Also provided are pharmaceutical compositions, methods of using, and methods of preparing the compounds.
Type:
Grant
Filed:
October 8, 2008
Date of Patent:
September 28, 2010
Assignee:
Roche Palo Alto LLC
Inventors:
Pravin Iyer, Matthew C. Lucas, Ryan Craig Schoenfeld, Marzia Villa, Robert James Weikert
Abstract: This invention concerns novel substituted tetracyclic tetrahydrofuran, pyrrolidine and tetrahydrothiophene derivatives with binding affinities towards serotonin receptors, in particular 5-HT2A and 5-HT2C receptors, and towards dopamine receptors, in particular dopamine D2 receptors and with norepinephrine reuptake inhibition properties, pharmaceutical compositions comprising the compounds according to the invention, the use thereof as a medicine, in particular for the prevention and/or treatment of a range of psychiatric and neurological disorders, in particular certain psychotic, cardiovascular and gastrokinetic disorders and processes for their production. The compounds according to the invention can be represented by general Formula (I) and comprises also the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the N-oxide form thereof and prodrugs thereof, wherein all substituents are defined as in Claim 1.
Type:
Grant
Filed:
December 6, 2005
Date of Patent:
September 21, 2010
Assignee:
Janssen Pharmaceutica NV
Inventors:
José Maria Cid-Núñez, Antonius Andrianus Hendrikus Petrus Megens, Andrés Avelino Trabanco-Suárez, Mohamed Koukni, Georges Joseph Cornelius Hoornaert, Frans Josef Cornelius Compernolle, Tomasz Kozlecki, Hua Mao, Sushil Chandra Jha, Francisco Javier Fernández-Gadea
Abstract: The present invention relates to compounds that have activity as S1P receptor modulating agents and the use of such compounds to treat diseases associated with inappropriate S1P receptor activity. In certain embodiments, the compounds of the invention relate to aryl oxoimidazolidinyls.
Abstract: Compounds of formula Ia and Ib wherein A, B, C and R1 are described herein.
Type:
Grant
Filed:
November 13, 2006
Date of Patent:
September 7, 2010
Assignee:
Bristol-Myers Squibb Company
Inventors:
Mark E. Salvati, Heather Finlay, Lalgudi S. Harikrishnan, Ji Jiang, James A. Johnson, Muthoni G. Kamau, R. Michael Lawrence, 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 invention concerns novel compounds of the N-acylamino-amide family, compositions, in particular cosmetic or pharmaceutical, containing them, and their use for treating body or face skin ageing, whether chronobiologic or light-induced, and in particular skin ageing caused by decrease of skin elasticity and/or by collagen degradation in the structure for tissues.
Abstract: Combretastatin derivatives of formula (I), preparation and use thereof are disclosed, wherein: Rf is alkyl with 1-8 carbon atoms and 1-17 fluorine atoms, R is amino, substituted amino, hydroxyl, nitro, halo, alkyloxy, phosphate or amino acid side chain. Said derivatives have a capability to inhibit the polymerization of microtubules and are useful in treatment against tumor and neovascularization.
Type:
Grant
Filed:
November 22, 2006
Date of Patent:
August 31, 2010
Assignee:
Zhejiang Dade Pharmaceutical Group Co. Ltd.