Abstract: The present invention provides compositions and methods of use for treating, preventing, or ameliorating a disease, disorder, or condition associated with a chemokine receptor such as CXCR4.
Abstract: The present invention provides compounds used in the synthesis of chemiluminescent acridinium compounds and methods of producing these compounds. Specifically, methods are provided for the N-alkylation of acridan compounds using alkylating reagents. Typically, these alkylating reagents comprise a protected sulfonate group protected with an acid-labile protecting group.
Abstract: Disclosed herein are embodiments of a donor compound that releases COS and/or CS2, which can be converted to H2S. The donor compound embodiments described herein can be used to deliver H2S to a subject or a sample and further can be used to administer therapeutic agents. Methods of making and using the donor compound embodiments also are disclosed.
Abstract: Novel iron chelators exhibiting neuroprotective and good transport properties are useful in iron chelation therapy for treatment of a disease, disorder or condition associated with iron overload and oxidative stress, eg. a neurodegenerative or cerebrovascular disease or disorder, a neoplastic disease, hemochromatosis, thalassemia, a cardiovascular disease, diabetes, a inflammatory disorder, anthracycline cardiotoxicity, a viral infection, a protozoal infection, a yeast infection, retarding ageing, and prevention and/or treatment of skin ageing and skin protection against sunlight and/or UV light. The iron chelator function is provided by a 8-hydroxyquinoline, a hydroxypyridinone or a hydroxamate moiety, the neuroprotective function is imparted to the compound e.g. by a neuroprotective peptide, and a combined antiapoptotic and neuroprotective function by a propargyl group.
Type:
Grant
Filed:
November 7, 2003
Date of Patent:
November 15, 2011
Assignees:
Technion Research and Development Foundation Ltd., Yeda Research and Development Co., Ltd.
Abstract: The present invention provides compounds are disclosed herein having the formula: Wherein n is 1 or 2; m is 0 or 1; p is 0, 1 or 2; R1 is aryl, heteroaryl or alkyl; R2 is C1-6 hydrocarbyl, alkylacyl or hydroxyalkyl; R3 is aryl, heteroaryl, or alkyl; R4 is H, OH, —O—(C1-6 alkyl), —NH—(C1-6 alkyl), or oxide; R5 is H, halogen, C1-6 alkyl, O—(C1-6 alkyl), aryl, heteroaryl, —C(?O)(C1-6 alkyl), substituted or un-substituted oxazolin-2-yl; X?O, NH, —C(?O)— or —N?CH—; and Each L is independently alkylene and carbonyl. Therapeutic methods, compositions, and medicaments related thereto are also disclosed.
Abstract: This invention relates to novel compounds that are 4-oxoquinoline derivatives and pharmaceutically acceptable salts thereof. More specifically, this invention relates to novel 4-oxoquinoline derivatives that are derivatives of elvitegravir. This invention also provides pyrogen-free compositions comprising one or more compounds of this invention and a carrier, and the use of the disclosed compounds and compositions in methods of treating diseases and conditions that are beneficially treated by administering an HIV integrase inhibitor, such as elvitegravir.
Abstract: This application discloses a novel process to synthesize 2-(Quinolin-5yo)-4,5-Disubstituted-Azole derivatives, which may be used, for example, as PDE IV inhibitor compounds in pharmaceutical preparations.
Type:
Grant
Filed:
August 10, 2007
Date of Patent:
July 26, 2011
Assignee:
Schering Corporation
Inventors:
Timothy D. Cutarelli, Xiaoyong Fu, Timothy L. McAllister, Michael R. Reeder, Jianguo Yin, Kelvin H. Yong, Shuyi Zhang
Abstract: The invention provides compounds having the formula: wherein R1 is halogen. The invention also provides compositions comprising the compounds, and methods of treating diseases or disorders that comprise administering one or more of the compounds to a subject in need thereof. The disclosed compounds have CCR1 antagonist activity.
Type:
Grant
Filed:
April 22, 2010
Date of Patent:
July 12, 2011
Assignee:
Millennium Pharmaceuticals, Inc.
Inventors:
Kenneth G. Carson, Geraldine C. B. Harriman, Shomir Ghosh
Abstract: The invention concerns quinoline derivatives of Formula I or a pharmaceutically-acceptable salt thereof, wherein each of X1, p, R1, q, R2, R3, R4, R5, Ring A, r and R6 has any of the meanings defined hereinbefore in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the treatment of cell proliferative disorders.
Abstract: Novel compounds of formula (I): or pharmaceutically acceptable salts thereof, wherein R, R1, R2, R3, R4, R5, and R6 have the meanings given in the description, pharmaceutical compositions comprising said compounds and use thereof as protein kinase inhibitors.
Abstract: Imidazo[4,5-c] ring compounds, (e.g. imidazo[4,5-c]pyridines, imidazo[4,5-c]quinolines, 6,7,8,9-tetrahydro imidazo[4,5-c]quinolines, imidazo[4,5-c]naphthyridine, and 6,7,8,9-tetrahydro imidazo[4,5-c]naphthyridine compounds) having an oxime or hydroxylamine substituent at the 2-position, pharmaceutical compositions containing the compounds, intermediates, and methods of making and methods of use of these compounds as immunomodulators, for modulating cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases are disclosed.
Type:
Grant
Filed:
February 10, 2006
Date of Patent:
June 28, 2011
Assignee:
3M Innovative Properties Company
Inventors:
Tushar A. Kshirsagar, Gregory D. Lundquist, Jr., Joseph F. Dellaria, Matthew R. Radmer, Bernhard M. Zimmermann
Abstract: The invention relates to adenozin A3 receptor ligands labeled with iodine isotops of mass number 125, within those favorably to antagonists and their isomers, to the experimental materials containing them, to a process for the preparation of the compounds of the general formula (I) and their isomers, to the new intermediates of the general formula (II) and to the preparation thereof.
Abstract: Compounds of Formula I wherein R1, A, R2, R3, R4, R5, n, m and q are as described in the specification, pharmaceutically-acceptable salts, methods of making, pharmaceutical compositions containing and methods for using the same.
Type:
Grant
Filed:
September 19, 2006
Date of Patent:
June 21, 2011
Assignee:
AstraZeneca AB
Inventors:
Jeffrey S. Albert, Gerard M. Koether, Cristobal Alhambra, James Kang, Thomas R. Simpson, James Woods, Yan Li
Abstract: The invention provides novel ?2 adrenergic receptor agonist compounds. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with ?2 adrenergic receptor activity, and processes and intermediates useful for preparing such compounds.
Type:
Grant
Filed:
April 30, 2008
Date of Patent:
June 21, 2011
Assignee:
Theravance, Inc.
Inventors:
Martin S. Linsell, John R. Jacobsen, Daisuke Roland Saito
Abstract: The invention provides compounds of formula (I), processes for their preparation, pharmaceutical compositions containing them, a process for preparing the pharmaceutical compositions, and their use in therapy, wherein R1, R2, R3 and n are as defined in the specification
Abstract: Compounds, compositions and methods are provided that are useful in the treatment or prevention of a condition or disorder mediated by PPAR?. In particular, the compounds of the invention modulate the function of PPAR?. The subject methods are particularly useful in the treatment and/or prevention of diabetes, obesity, hypercholesterolemia, rheumatoid arthritis and atherosclerosis.
Type:
Grant
Filed:
February 17, 2009
Date of Patent:
June 14, 2011
Assignee:
Amgen Inc.
Inventors:
Lawrence R. McGee, Jonathan B. Houze, Steven M. Rubenstein, Atsushi Hagiwara, Noboru Furukawa, Hisashi Shinkai
Abstract: A succinic acid salt of biphenyl-2-ylcarbamic acid 1-[2-(2-chloro-4-{[(R)-2-hydroxy-2-(8-hydroxy-2-oxo-1,2-dihydroquinolin-5-yl)ethylamino]methyl}-5-methoxyphenylcarbamoyl)ethyl]piperidin-4-yl ester or a solvate thereof, for use in treating pulmonary disorders.
Abstract: Compounds of the general formula (I); wherein the substituents are as defined in claim 1, are useful as fungicides.
Type:
Grant
Filed:
November 29, 2005
Date of Patent:
June 7, 2011
Assignee:
Syngenta Crop Protection, Inc.
Inventors:
Roger Salmon, David Philip Bacon, Ewan James Turner Chrystal, David William Langton, Andrew Jonathan Knee, Gordon Richard Munns, Laura Quaranta, Hans-Georg Brunner, Renaud Beaudegnies, Fredrik Cederbaum, Fiona Murphy Kessabi
Abstract: Disclosed are maleate, tosylate, fumarate, and oxalate salts of the compound 5-(1(S)-Amino-2-Hydroxyethyl)-N-[(2,4-Difluorophenyl)-Methyl]-2-[8-Methoxy-2-(Trifluoromethyl)-5-Quinoline]-4-Oxazolecarboxamide, represented by Formula I, and methods of preparing the same.
Type:
Grant
Filed:
August 10, 2007
Date of Patent:
June 7, 2011
Assignee:
Schering Corporation
Inventors:
Xiaoming Chen, Xiao Chen, Jianguo Yin, Xiaoyong Fu, David J. Blythin, Rongze Kuang, Ho-Jane Shue, Scott Trzaska, Chee-Wah Tang, Vincenzo Liotta, Zaher Shabani