Abstract: The invention relates to a continuous process for preparing dihydropyrones of general formula I, wherein the groups R1 and R2 have the meanings described herein.
Type:
Grant
Filed:
February 14, 2002
Date of Patent:
November 28, 2006
Assignee:
Boehringer Ingelheim Pharma GmbH & Co. KG
Inventors:
Oliver Meyer, Markus Sauter, Mark Goehlich
Abstract: Cyclohexane and cyclohexene derivatives and pharmaceutically acceptable derivatives thereof useful in methods of treatment of bacterial infections in mammals, particularly man.
Type:
Grant
Filed:
May 24, 2002
Date of Patent:
November 28, 2006
Assignee:
SmithKline Beecham p.l.c.
Inventors:
Gerald Brooks, David Thomas Davies, Graham Elgin Jones, Roger Edward Markwell, Neil David Pearson
Abstract: Compounds of Formula (I) that act as cannabinoid receptor ligands and their uses in the treatment of diseases linked to the mediation of the cannabinoid receptors in animals are described herein
Abstract: Disclosed herein are an acetone-extracted product obtained from gamboge resin and compounds further purified from said acetone-extracted product, including a new compound called formoxanthone A. The acetone-extracted product and the further purified compounds have been demonstrated to have activities in inhibiting the growth of tumor/cancer cells. Also disclosed are the processes for obtaining said further purified compounds, and the uses of the acetone-extracted product and the further purified compounds in the preparation of pharmaceutical composition for inhibiting the growth of tumor/cancer cells.
Type:
Grant
Filed:
October 6, 2004
Date of Patent:
November 21, 2006
Assignee:
Taiwan Sunpan Biotechnology Development Company, Ltd.
Abstract: Bicyclic hydroxamate compounds represented by the Formula I: are described. The bicyclic hydroxamate compounds and compositions containing those compounds may be used to inhibit or modulate an enzyme activity of HIV Integrase and to treat HIV mediated diseases and conditions.
Type:
Grant
Filed:
October 30, 2003
Date of Patent:
November 14, 2006
Assignee:
Agouron Pharmaceuticals, Inc.
Inventors:
Qiyue Hu, Ted William Johnson, Atsuo Kuki, Michael Bruno Plewe, Dawn Marie Nowlin, Hai Wang, Junhu Zhang
Abstract: Certain proanthocyanidins found in various wines, grape juice, and other plant extracts exhibit endothelium-dependent vasorelaxing activity that involves increased nitric oxide production by endothelial cells. The smallest procyanidins (PCs) possessing substantial EDR activity were isolated from grape seeds. A dimer di-gallate (epicatechin-galloyl-epicatechin-gallate) was purified from concord grape seed extracts by Toyopearl TSK-40 gel chromatography, HPLC and electrospray FTMS. Further characterization was achieved using tannase treatment and acid thiolysis. This compound had an EC50 for vasorelaxation of 0.67±0.04 ?g/ml when tested for endothelium-dependent relaxing activity in phenylephrine pre-contracted rat aortic rings.
Abstract: The present invention is comprised of culturing microorganism having ability to produce FKI-1083 substance represented by the formula: in a medium, accumulating FKI-1083 substance in the cultured medium, and isolating FKI-1083 substance from the cultured mass. The thus obtained FKI-1083 substance has growth inhibitory activities against microorganisms, nematodes and arthropods, and is useful as anthelmintic and insecticide.
Abstract: The present invention relates to oripavine derivatives of formula (I), wherein R1 is hydrogen or methyl, R2 is methyl, cyclopropyl methyl, cyclobutyl methyl or allyl, R3 is thiophenyl ethyl or cycloalkyl methyl where the cycloalkyl has 3 to 6 carbon atoms, or non-toxic pharmaceutically acceptable salts thereof. These compounds can be used for the preparation of analgesics or abstinence agents of opium habit-forming drugs.
Type:
Grant
Filed:
September 13, 2002
Date of Patent:
October 10, 2006
Assignees:
Institute of Pharmacology and Toxicology Academy of Military Medical Sciences, P.L.A. China, Zhejiang Xianju Pharmaceuticals Co. Ltd.
Inventors:
Bohua Zhong, Zehui Gong, Yaping Wang, Yongshao Liu
Abstract: The present invention relates to compounds of the following formula (I) or pharmaceutically acceptable salts thereof. The present invention also relates to use for a cognitive-enhancing agent of compounds of the following formula (I) or pharmaceutically acceptable salts thereof and to a process for preparing the same. Further, the present invention relates to use for a congnitive-enhancing agent of decursin of the following formula (II) or pharmaceutically acceptable salts thereof. In addition, the present invention relates to extracts of Angelica gigantis Radix comprising decursin of the following formula (II), having cognitive-enhancing effects.
Type:
Grant
Filed:
April 9, 2002
Date of Patent:
October 3, 2006
Assignee:
Elcom Biotechnology, Co. Ltd.
Inventors:
Jeong-Seon Yoon, Ji-Young Lee, Young-Choong Kim, Ki-Yong Lee, Sang-Hyun Sung, Hak-Joong Kim, So-Young Kang
Abstract: Compounds of general structural formula (I) and use of the compounds and salts and solvates thereof, as therapeutic agents as inhibitors of phosphodiesterase 5 cardiovascular disorders
Type:
Grant
Filed:
April 2, 2002
Date of Patent:
October 3, 2006
Assignee:
Lilly Icos LLC
Inventors:
Jason S. Sawyer, Mark W. Orme, James D. Copp
Abstract: Disclosed are the compounds of formula I wherein R is methyl or ethyl; R1 is chloro or fluoro; R2 is hydrogen or fluoro; R3 is hydrogen, fluoro, chloro, methyl, ethyl, methoxy, ethoxy or hydroxy; R4 is hydrogen or fluoro; and R5 is chloro, fluoro, trifluoromethyl or methyl; and pharmaceutically acceptable salts thereof, as selective COX-2 cyclooxygenase inhibitors; and pharmaceutically acceptable prodrug esters thereof.
Type:
Grant
Filed:
December 4, 2003
Date of Patent:
October 3, 2006
Assignee:
Novartis AG
Inventors:
Roger A Fujimoto, Leslie W McQuire, Benjamin B Mugrage, John H Van Duzer, Daqiang Xu
Abstract: The invention relates to a method of treating at least one symptom of a lower urinary tract disorder in a subject in need of treatment wherein the symptom is selected from the group consisting of urinary frequency, urinary urgency, urinary urge incontinence, nocturia and enuresis. The method comprises administering to a subject in need of treatment a therapeutically effective amount of a compound that has 5-HT3 receptor antagonist activity and NorAdrenaline Reuptake Inhibitor (NARI) activity.
Type:
Grant
Filed:
June 7, 2004
Date of Patent:
October 3, 2006
Assignee:
Dynogen Pharmaceuticals, Inc.
Inventors:
Steven B. Landau, Cheryl L. Miller, Matthew O. Fraser
Abstract: The invention relates to new heterocyclic compounds of general formula (I), and their salts with a base or an acid: The invention also relates to a process for the preparation of these compounds as well as their use as medicaments, in particular as anti-bacterial agents.
Type:
Grant
Filed:
July 24, 2001
Date of Patent:
September 26, 2006
Assignee:
Aventis Pharma S.A.
Inventors:
Maxime Lampilas, Jozsef Aszodi, David Alan Rowlands, Claude Fromentin
Abstract: Disclosed herein is a method for making compounds that are useful as caspase inhibitor prodrugs of formula I: wherein R1 is an optionally substituted group selected from an aliphatic group, aralkyl group, heterocyclylalkyl group or aryl group, and R2 is preferably a P2—P4 moiety of a caspase inhibitor.
Abstract: The present invention relates to sulfone derivatives of formula (I): Ar—SO2—CR2R3-L-N(R1)2I wherein Ar, L, R1, R2 and R3 are as defined herein, and pharmaceutically acceptable salts and N-oxides thereof, useful in the treatment of a condition which is susceptible to treatment by modulation of 5-HT7 receptor activity, such as depression or a sleep disorder.
Type:
Grant
Filed:
May 14, 2004
Date of Patent:
September 5, 2006
Assignee:
Merck Sharp & Dohme Ltd.
Inventors:
Sylvie Bourrain, Peter Alan Hunt, Ian Thomas Huscroft, Janusz Jozef Kulagowski, Clare London, Elizabeth Mary Naylor, Piotr Antoni Raubo, Eileen Mary Seward
Abstract: Methods of utilizing compounds of general formulas I and II as modulators and affinity labels of the MPTP complex are elucidated. Furthermore, methods for modulating the activity of the MPTP complex, methods for determining the presence of a component of the MPTP complex, and methods for identifying an active agent that modulates the activity of the MPTP complex, specifically methods for identifying an active agent that modulates the activity of the MPTP complex by interacting with the VDAC1 component are identified. Moreover, novel compounds of general formulas I and II are disclosed.
Abstract: An ascorbic acid derivative of the formula Ia: where the variables independently of one another have the following meanings: R1 and R2 independently of one another are hydrogen or C1-C20-acyl; R3 is hydrogen or a cation selected from the group consisting of NH4+, alkali metal and alkaline earth metal cations; R4 is C1-C6-alkoxycarbonyl, and a process for its preparation.
Type:
Grant
Filed:
October 1, 2001
Date of Patent:
September 5, 2006
Assignee:
BASF Aktiengesellschaft
Inventors:
Harald Streicher, Bernd Ostersehlt, Horst Westenfelder
Abstract: The present invention describes compounds of the general formula I as well as processes for their manufacture, pharmaceutical compositions containing them and methods for using these compounds and pharmaceutical compositions as pharmaceutical agents. The compounds according to this invention show antiproliferative and differentiation-inducing activity, which results in inhibition of tumor cell proliferation, induction of apoptosis and inhibition of invasion.
Type:
Grant
Filed:
December 10, 2003
Date of Patent:
August 29, 2006
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Georg Fertig, Frank Herting, Matthias Koerner, Manfred Kubbies, Anja Limberg, Ulrike Reiff, Michael Weidner