Abstract: The subject invention provides novel compositions of biologically active polyketide compounds that can advantageously be used in blocking cellular proliferation and treatment of cancer.
Type:
Grant
Filed:
July 12, 2004
Date of Patent:
August 22, 2006
Assignee:
Harbor Branch Oceanographic Institution, Inc.
Inventors:
K. Brian Killday, Amy E. Wright, Shirley A. Pomponi, Ross E. Longley
Abstract: Compounds of the formula (I) below, or pharmacologically acceptable salts, esters or other derivatives thereof: wherein A is furan, thiophene, pyrazole, imidazole, isoxazole or isothiazole; R1 is a substituted or unsubstituted aryl or a substituted or unsubstituted heteroaryl; R2 is a substituted or unsubstituted heteroaryl; and R3 is a bicyclic amino group; provided that the substituents R1 and R2 are bonded to the two atoms of the cyclic group A which are adjacent to the atom of the cyclic group A to which the substituent R2 is bonded. The compounds inhibit the production of inflammatory cytokines.
Abstract: Aryl substituted imidazoquinoline compounds, pharmaceutical compositions containing the compounds, intermediates, and methods of use of these compounds as immunomodulators, for inducing or inhibiting cytokine biosynthesis in animals and in the treatment of diseases including viral, and neoplastic, are disclosed.
Type:
Grant
Filed:
December 18, 2003
Date of Patent:
August 15, 2006
Assignee:
3M Innovative Properties Co.
Inventors:
David S. Hays, Shri Niwas, Tushar Kshirsagar, Philip D. Heppner, Bryon A. Merrill, Michael E. Danielson, John F. Gerster, Chad A. Haraldson, Maureen A. Kavanagh, Michael J. Rice, Sarah A. Strong, Joshua R. Wurst
Abstract: The invention provides compounds of formula I, wherein X, Y, R1, R2, and R3 are as defined in the description, and the preparation thereof. The compounds of formula I are useful as pharmaceuticals.
Type:
Grant
Filed:
August 14, 2002
Date of Patent:
August 8, 2006
Assignee:
Novartis AG
Inventors:
Samuel Hintermann, Bastian Hengerer, Ulrike Von Krosigk
Abstract: A compound containing an alkylene selenocyanate or an alkylene isoselenocyanate moiety effective to prevent the occurrence or progression of cancer or a precancerous condition. The compound can be provided and administered in the form of a pharmaceutical composition, a cosmetic, a food additive, supplement, or the like. Methods for synthesis and use of the chemopreventive compound of the invention are also provided.
Abstract: The disclosure relates to a fumagillol compound which can be usefully used not only as an angiogenesis inhibiting agent showing a superior angeogenesis inhibitory effect with less toxicity, but also as a cancer metastasis inhibitor and a therapeutic agent against cancer and other various inflammatory diseases such as rheumatic disease, psoriasis, etc., and diabetic retinopathy related to angeogeneois, and also a method for preparing the same.
Type:
Grant
Filed:
June 11, 2002
Date of Patent:
August 8, 2006
Assignee:
Equispharm Co., Ltd.
Inventors:
Cheol-Kyu Han, Jeong-Hyeok Yoon, Seung-Moak Kim, Nam-Doo Kim, Byung-Ha Chang, Jee-Young Lee, Tae-Bo Sim
Abstract: Peripherally administered Brefeldin A and its analogs and derivatives are used to enhance learning and reverse memory dysfunction through induced long term potentiation in hippocampal issues.
Type:
Grant
Filed:
March 22, 2004
Date of Patent:
July 25, 2006
Assignee:
The Regents of the University of California
Inventors:
Katumi Sumikawa, Ken-Ichi Ito, James L. McGaugh
Abstract: Ortho-substituted anthranilic acid amides and use thereof as pharmaceutical agents for treating diseases that are triggered by persistent angiogenesis are described.
Type:
Grant
Filed:
May 8, 2001
Date of Patent:
July 25, 2006
Assignee:
Schering AG
Inventors:
Martin Krueger, Andreas Huth, Orlin Petrov, Dieter Seidelmann, Karl-Heinz Thierauch, Martin Haberey, Andreas Menrad, Alexander Ernst
Abstract: A process for preparing functionalized ?-butyrolactones 3 and various biologically active compounds using mucohalic acid 1 and halide 2 in the presence of indium is disclosed, wherein X, Y, R1, R2, and R3 may have any of the meanings defined herein
Abstract: The present invention provides novel ?-glucosidase inhibitory compound (?)-mesquitol and its analogs isolated in significant yield from traditional medicinal plant Dichrostachys cinerea and further modification of (?)-mesquitol to enhance the ?-glucosidase inhibitory potential; the invention also identifies the usage of (?)-mesquitol and its analogues, based on their ?-glucosidase inhibitory activity, as broad based potential therapeutics as antihyperglycernic, antidiabatic, antiobesity, antiviral, anticancer, immunestimulants and the like.
Type:
Grant
Filed:
April 1, 2003
Date of Patent:
July 4, 2006
Assignee:
Council of Scientific and Industrial Research
Abstract: The invention relates to the inhibition of tubulin polymerization. The invention provides compounds and methods for inhibiting tubulin polymerization. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.
Abstract: Hydrates of N-[1-butyl-4-[3-[3-(hydroxy)propoxy]-phenyl]-1,2-dihydro-2-oxo-1,8-naphthyridin-3-yl]-N?-(2,6-diisopropyl-4-aminophenyl)urea hydrochloride of the formula: are quite excellent in stability than amorphous one and are more preferable for medicaments.
Type:
Grant
Filed:
August 14, 2002
Date of Patent:
June 27, 2006
Assignee:
Sumitomo Pharmaceuticals Co., Ltd.
Inventors:
Masami Muraoka, Satoshi Ohnuma, Hitoshi Ban
Abstract: The invention relates to an imidazo[1,2-a]pyrimidone derivative represented by formula (1) or a salt thereof, wherein: X represents a bond, an ethenylene group, and ethenylene group, a methylene group optionally substituted by one or two groups selected from a C1-6 alkyl group, a hydroxy group and a C1-4 alkoxy group; a carbonyl group, an oxygen atom, a sulfur atom, a sulfonyl group, a sulfoxide group or a nitrogen atom being optionally substituted by a C1-6 alkyl group; R1 represents a 2,3 or 4-pyridyl group optionally substituted by a C1-4 alkyl group, C1-4 alkoxy group or a halogen atom; R2 represents a C1-6 alkyl group, a C1-2 perhalogenated alkyl group, a C1-3 halogenated alkyl group, a benzyl group, a phenyl ring, a naphthyl ring, 5,6,7,8-tetrahydronaphthyl ring, a pyridyl ring, an indole ring, a pyrrole ring, a thiophene ring, a furan ring or an imidazole ring, the benzyl group and the rings being optionally substituted by 1 to 4 substituents selected from a C1-6 alkyl group, a phenyl ring, a halogen a
Abstract: There are disclosed compounds of formulae (I) or (II) in which A is selected from the group consisting of (1), (2), (3) and (4); OH, and one of R1 and R2 is selected from H, OH and OCH3, and the other of R1 and R2 is selected from OH and OCH3; one of R3 and R4 is selected from H, OH and OCH3, and the other of R3 and R4 is selected from OH and OCH3; provided that at least one of the pairs R1, R2 and R3, R4 are both OH; R5 is selected from OH and OCH3; and denotes a single or double bond; and pharmaceutically acceptable salts and prodrugs thereof. The compounds of the invention are useful for the treatment of hormone-dependent conditions and cancers.
Abstract: Taxanes having a carbonate substituent at C(10), a hydroxy substituent at C(7), and a range of C(2), C(9), C(14), and side chain substituents.
Abstract: Disclosed are novel heterocyclic derivatives, useful for the treatment of various disease states, in particular cardiovascular diseases such as atrial and ventricular arrhythmias, intermittent claudication, Prinzmetal's (variant) angina, stable and unstable angina, exercise induced angina, congestive heart disease, and myocardial infarction. The compounds are also useful in the treatment of diabetes, and for increasing HDL plasma levels in mammals.
Type:
Grant
Filed:
January 16, 2004
Date of Patent:
June 6, 2006
Assignee:
CV Therapeutics, Inc.
Inventors:
Prabha Ibrahim, Kevin Shenk, Elfatih Elzein, Venkata Palle, Jeff Zablocki, Kenneth S. Rehder
Abstract: The invention provides aporphine and oxoaporphine compounds that have endothelial nitric oxide synthase (eNOS) maintaining or enhancing activities and may be used to manufacture a medicaments for preventing or treating ischemic diseases in human and mammal, and the ischemic diseases may include ischemic cerebral apoplexy, ischemic cerebral thrombosis, ischemic cerebral embolism, hypoxic ischemic encephlopathy, ischemic cardiac disease or ischemic enteropathy etc.
Abstract: Titanium or vanadium zeolites are pretreated by contacting with an amino polyacid compound, such as ethylenediaminetetraacetic acid or a salt thereof, prior to use in olefin epoxidation with hydrogen peroxide.
Type:
Grant
Filed:
December 17, 2004
Date of Patent:
June 6, 2006
Assignee:
Lyondell Chemical Technology, L.P.
Inventors:
Kun Qin, Roger A. Grey, Peter J. Whitman
Abstract: The present invention discloses the identification of the novel inhibitors of farnesyl protein transferase and ras protein farnesylation. The compounds and pharmaceutical compositions disclosed herein are useful in treating diseases associated with farnesyl protein transferase, such as cancer.
Abstract: The present invention provides serotonergic aminoalkylbenzofurans of Formula (I): where R, R1, R2, R3, R4, R4?, R5, R5?, and R12 are as described in the specification.
Type:
Grant
Filed:
January 19, 2000
Date of Patent:
May 16, 2006
Assignee:
Eli Lilly and Company
Inventors:
Karin Briner, Joseph Paul Burkhart, Timothy Paul Burkholder, Matthew Joseph Fisher, William Harlan Gritton, Daniel Timothy Kohlman, Sidney Xi Liang, Shawn Christopher Miller, Jeffrey Thomas Mullaney, Yao-Chang Xu, Yanping Xu