Ketone In Z Radical Patents (Class 514/545)
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Patent number: 11690832Abstract: The present specification provides methods of treating autoimmune diseases with a combination of a RXR agonist and a thyroid hormone.Type: GrantFiled: January 26, 2022Date of Patent: July 4, 2023Assignee: IO TherapeuticsInventors: Roshantha A. Chandraratna, Martin E. Sanders
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Patent number: 10300000Abstract: The present invention provides a method of treating a subject afflicted with hyperpigmentation or of lightening the skin tone of a subject comprising administering to the subject an amount of a compound having the structure: or a salt or ester thereof, so as to thereby treat the subject or lighten the skin tone of the subject.Type: GrantFiled: September 12, 2017Date of Patent: May 28, 2019Assignee: THE RESEARCH FOUNDATION FOR THE STATE UNIVERSITY OF NEW YORKInventors: Shilpi Goenka, Sanford Simon
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Patent number: 10071945Abstract: Disclosed are compounds which are nuclear receptor modulators that can act as antagonists to the androgen receptor, for example, a compound of Formula I: wherein R1 to R5 and X1 to X5 are as described herein, as well as pharmaceutically acceptable salts, solvates, and stereoisomers thereof. Pharmaceutical compositions comprising such compounds, as well as methods of use, and treatment for cancers, including prostate cancers, other nuclear receptor mediated cancers, and other conditions, are also disclosed.Type: GrantFiled: June 15, 2012Date of Patent: September 11, 2018Assignee: The United States of America, as represented by the Secretary, Department of Health and Human ServicesInventors: Jane B. Neckers, Yeong Sang Kim, Sunmin Lee, Vineet Kumar, Sanjay V. Malhotra
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Patent number: 10023544Abstract: A fused heterocyclic compound having an enteropeptidase inhibitory action and use of the compound as a medicament for treatment or prophylaxis of obesity, diabetes mellitus, etc., are provided. Specifically, a compound represented by the following formula (I): wherein each symbol is as defined herein, or a salt thereof and use of the compound as a medicament for treatment or prophylaxis of obesity, diabetes mellitus, etc., are provided.Type: GrantFiled: February 12, 2015Date of Patent: July 17, 2018Assignee: Takeda Pharmaceutical Company LimitedInventors: Zenichi Ikeda, Minoru Sasaki, Keiko Kakegawa, Fumiaki Kikuchi, Yoichi Nishikawa
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Patent number: 9328330Abstract: The present invention discloses the potential of Calebin A in inhibiting adipogenesis and applications thereof in obesity management. The present invention elucidates the potential of Calebin A to favorably modulate biochemical markers associated with obesity. Notable biomodulatory properties of Calebin A include inhibiting leptin production, increasing adiponectin expression and inhibiting local (adipocyte) and systemic inflammation caused by pro-inflammatory cytokines Tumor Necrosis Factor (TNF-?), Interleukin-6 (IL-6) and Interleukin-1 (IL-1?).Type: GrantFiled: May 9, 2014Date of Patent: May 3, 2016Assignee: SAMI LABS LIMITEDInventors: Muhammed Majeed, Kalyanam Nagabhushanam, Anju Majeed, Bani Sarang, Anjali Pandey
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Publication number: 20150126576Abstract: The present invention relates to compounds that may be used to inhibit activation of protein kinase G (“PKG”). It is based, at least in part, on the discovery of the tertiary structure of PKG and the identification of molecules that either bind to the active site of PKG and/or are analogs of balanol.Type: ApplicationFiled: September 29, 2014Publication date: May 7, 2015Applicant: The Trustees of Columbia University in the City of New YorkInventors: Richard Ambron, Ying-Ju Sung, Jeremy Greenwood, Leah Frye, Shi-Xian Deng, Yuli Xie, Donald W. Landry
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Publication number: 20150118317Abstract: Various fenofibrate dosage forms contain a plurality of beads or particles, where the beads or particles include a pharmaceutical composition comprising fenofibrate; from 0.3% to 10% by weight of the beads or particles of a surfactant; and from about 5% to about 15% by weight of the beads or particles of a water soluble or water dispersible cellulosic binder. The mass ratio of the drug to the binder in the dosage form is between about 3.5:1 and 4.5:1; and the dosage form produces a first Cmax in vivo that is between about 10% and about 50% higher than a comparative Cmax produced by a comparative dosage form. The comparative dosage form comprises the drug and the binder in a ratio of between about 5:1 and 15:1.Type: ApplicationFiled: October 23, 2012Publication date: April 30, 2015Applicant: MYLAN, INC.Inventors: Sarat C. Chattaraj, Glenn Allen Redelman, Andrew Alan Shaw
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Publication number: 20150087705Abstract: Disclosed herein are compounds, compositions and methods for preventing and treating diseases such as intracerebral hemorrhage, cancer, or conditions associated with damaged cells, activated lymphocytes, or microbial products. The disclosed compounds are curcumin analogs. The curcumin analogs possess anti-inflammatory and antioxidant properties, which in part, reduce AP-1 and NF-?B activity.Type: ApplicationFiled: September 22, 2014Publication date: March 26, 2015Inventors: Cargill H. Alleyne, JR., Krishnan M. Dhandapani, Ken Wen, MingLiang Ma, WenJing Hu
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Publication number: 20150073021Abstract: The present invention provides a method of inhibiting the binding of anthrax lethal factor with protective antigen comprising contacting the anthrax lethal factor with a compound having the structure:Type: ApplicationFiled: September 5, 2014Publication date: March 12, 2015Applicants: The Research Foundation for The State University of New York, Chem-Master International, Inc.Inventors: Anthony ANTONELLI, Sanford R. SIMON, Yu ZHANG, Lorne M. GOLUB, Francis JOHNSON
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Patent number: 8956589Abstract: Disclosed are a curcumin derivative or a salt thereof, which contains a fluorine atom, represented by formula (I): (wherein R1a and R1b are each independently a hydrogen atom, alkyl, acetyl, or methoxycarbonyl; R2s are each independently a fluorine atom, CHF2—, CF3—, CHF2O—, or CF3O—; R3s are each independently a hydrogen atom or a fluorine atom; A is alkyl, cyano, carboxyl, alkoxycarbonyl, or R4—(CH2)m—; R4 is hydroxy, carboxy, cyano, acetyloxy, alkoxycarbonyl, alkoxyalkoxy, hydroxyalkoxy, or CONR5R6; R5 and R6 are each independently a hydrogen atom or alkyl; and m is an integer from 1 to 5), and a diagnostic imaging agent for diagnosing a disease in which an amyloid ? peptide aggregate accumulates, the diagnostic imaging agent containing a compound having a 1,3-dicarbonyl structure, wherein the compound exists in a keto form and an enol form, and the keto form and the enol form have different affinities, respectively, to the amyloid ? peptide aggregate.Type: GrantFiled: February 26, 2010Date of Patent: February 17, 2015Assignee: Shiga University of Medical ScienceInventors: Ikuo Tooyama, Hiroyasu Taguchi, Shigehiro Morikawa, Makoto Urushitani, Daijiro Yanagisawa, Tomone Nagae, Nobuaki Shirai, Koichi Hirao, Masanari Kato, Hirohiko Kimura, Takashi Okada
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Patent number: 8835376Abstract: A process for making particles for delivery of drug nanoparticles is disclosed herein. The process comprises the steps of (a) forming a suspension of drug nanoparticles by mixing a precipitant solution with an anti-solvent solution under micro-mixing environment, where the formed nanoparticles have a narrow particle size distribution; (b) providing an excipient to at least one of the precipitant solution, the anti-solvent solution and the suspension of drug nanoparticles, the excipient being selected to maintain said drug nanoparticles in a dispersed state when in liquid form; and (c) drying the suspension of drug nanoparticles containing the excipient therein to remove solvent therefrom, wherein removal of the solvent causes the excipient to solidify and thereby form micro-sized matrix particles, each micro-sized particle being comprised of drug nanoparticles dispersed in a solid matrix of the excipient.Type: GrantFiled: September 24, 2009Date of Patent: September 16, 2014Assignee: Nanomaterials Technology Pte LtdInventors: Zhigang Shen, Jimmy Sung Lai Yun, Jun Hu, Nital Arvind Jugade, Jiyao Zhang, Wenhao Chen, Zhe Wang, Lingyan Gao, William Glover, Jian Feng Chen
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Publication number: 20140255499Abstract: A method of forming fine particles of a drug substance using a piston-gap high pressure homogeniser.Type: ApplicationFiled: October 5, 2012Publication date: September 11, 2014Inventors: Guy Vergnault, Alain Nhamias, Pascal Grenier
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Patent number: 8790703Abstract: The invention relates to a process for producing formulations of sparingly water-soluble substances, said sparingly soluble substances being present in amorphous embedded form in a copolymer, and said copolymer being obtained by free-radically initiated polymerization of a mixture of i) 30 to 80% by weight of N-vinyllactam, ii) 10 to 50% by weight of vinyl acetate, and iii) 10 to 50% by weight of a polyether, with the proviso that the sum of components i), ii) and iii) equals 100% by weight, which comprises embedding the sparingly soluble substance into the copolymer at temperatures above the melting point of the sparingly soluble substances.Type: GrantFiled: March 30, 2010Date of Patent: July 29, 2014Assignee: BASF SEInventors: Kathrin Meyer-Böhm, Rainer Dobrawa, Stefan Fischer, Karl Kolter
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Publication number: 20140171444Abstract: The present invention provides aryl- or heteroaryl-diketo acid compounds effective to inhibit an activity of a Mycobacterial malate synthase enzyme or to inhibit a malate synthase activity in other bacteria having the enzyme. The compounds may be phenyl- naphthyl-, or thienyl-substituted diketo acids and carboxylate derivatives thereof. Also provided are methods of treating tuberculosis or other pathophysiological conditions associated with a malate synthase enzyme with the inhibitory compounds and methods of in silico design of the inhibitory compounds. In addition, the present invention provides the inhibitory compounds designed by this method. Furthermore, three-dimensional X-ray crystal structures of the Mycobacterial malate synthase complexed with the inhibitory compounds are provided. Further still a method for stabilizing an aromatic or heteroaromatic diketo acid or its prodrug or close analog in solution by derivatizing at least the ortho position on the aromatic ring is provided.Type: ApplicationFiled: March 3, 2014Publication date: June 19, 2014Applicant: THE TEXAS A&M UNIVERSITY SYSTEMInventors: Joel S. Freundlich, James C. Sacchettini, Inna V. Kriger, Thomas R. Ioerger, Vijay Gawandi
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Patent number: 8729122Abstract: The invention relates to compositions comprising abscisic acid, and/or salts, derivatives and analogs thereof, and methods of pharmaceutical and/or nutraceutical use.Type: GrantFiled: August 30, 2013Date of Patent: May 20, 2014Assignee: Valent BioSciences CorporationInventors: Maria Pilar Herrero, Warren E. Shafer
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Patent number: 8685433Abstract: The present invention provides an absorbable coating for an implantable device and the methods of making and using the same.Type: GrantFiled: March 31, 2010Date of Patent: April 1, 2014Assignee: Abbott Cardiovascular Systems Inc.Inventors: Lothar W. Kleiner, Syed F. A. Hossainy, Mikael Trollsas, Stephen D. Pacetti
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Patent number: 8664255Abstract: The present invention provides aryl- or heteroaryl-diketo acid compounds effective to inhibit an activity of a Mycobacterial malate synthase enzyme or to inhibit a malate synthase activity in other bacteria having the enzyme. The compounds may be phenyl- naphthyl-, or thienyl-substituted diketo acids and carboxylate derivatives thereof. Also provided are methods of treating tuberculosis or other pathophysiological conditions associated with a malate synthase enzyme with the inhibitory compounds and methods of in silico design of the inhibitory compounds. In addition, the present invention provides the inhibitory compounds designed by this method. Furthermore, three-dimensional X-ray crystal structures of the Mycobacterial malate synthase complexed with the inhibitory compounds are provided. Further still a method for stabilizing an aromatic or heteroaromatic diketo acid or its prodrug or close analog in solution by derivatizing at least the ortho position on the aromatic ring is provided.Type: GrantFiled: October 20, 2009Date of Patent: March 4, 2014Assignee: The Texas A&M University SystemInventors: Joel S. Freundlich, James C. Sacchettini, Inna V. Kriger, Thomas R. Ioerger, Vijay Gawandi
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Patent number: 8642644Abstract: The present invention relates generally to ophthamological drugs. More specifically, the invention relates to a method of modifying (derivatizing) ophthamological drugs so as to increase their penetration through the cornea. The invention also relates to drugs modified (derivatized) in accordance with the instant method and to the use of same in treating conditions associated with elevated intraocular pressure, particularly, glaucoma.Type: GrantFiled: July 29, 2009Date of Patent: February 4, 2014Assignee: Duke UniversityInventors: Eric J. Toone, David L. Epstein, Pratap Challa, Phillip W. Snyder, Xin Chen, Mitchell A. deLong
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Publication number: 20130310397Abstract: The invention relates to a novel free-flowing powder pharmaceutical formulation for the delivery of a poorly-water-soluble drug substance that increases the solubility and bioavailability of the poorly- water soluble drug substance, as well as to a method of making the free-flowing powder pharmaceutical formulation. The invention also relates to dispersed particles that disperse instantaneously from the free-flowing powder formulation when the formulation is added to water, aqueous solvent, or organic solvent, wherein the bulk distribution of the poorly-water soluble drug substance of the free-flowing powder formulation in the dispersed particles is uniform. Such dispersed particles increase the bioavailable surface area of the poorly water-soluble drug substance and facilitate the drug substance's dissolution.Type: ApplicationFiled: October 31, 2011Publication date: November 21, 2013Applicant: WESTERN UNIVERSITY OF HEALTH SCIENCESInventors: Guru V. Betageri, Sunil A. Agnihotri, Kumaresh Soppimath
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Publication number: 20130296422Abstract: Novel compounds below are useful for preventing or treating diseases caused by protozoans. At least one of a compound represented by Formula (I) (wherein, X represents a hydrogen atom or a halogen atom; R1 represents a hydrogen atom; R2 represents a hydrogen atom or a C1-7 alkyl group; R3 represents —CHO, —C(?O)R5, —COOR5 (wherein R5 represents a C1-7 alkyl group), —CH2OH or —COOH; and R4 represents a C1-16 alkyl group having one or more substituents on a terminal carbon atom and/or non-terminal carbon atom(s), a C2-16 alkenyl group having one or more substituents on a terminal carbon atom and/or non-terminal carbon atom(s), or a C2-16 alkynyl group having one or more substituents on a terminal carbon atom and/or non-terminal carbon atom(s)), an optical isomer thereof, and a pharmaceutically acceptable salt is used.Type: ApplicationFiled: November 1, 2011Publication date: November 7, 2013Applicant: ARIGEN PHARMACEUTICALS, INC.Inventors: Hiroyuki Saimoto, Kiyoshi Kita, Yoshisada Yabu, Masaichi Yamamoto
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Patent number: 8563054Abstract: An anti-inflammatory agent which includes an oil-soluble licorice extract, prepared by subjecting at least one of a leguminous plant of the genus Glycyrrhiza and a water extraction residue of a leguminous plant of the genus Glycyrrhiza to an extraction treatment with an organic solvent and which has at least one effect selected from an inhibitory effect on hyaluronidase activity, an inhibitory effect on hexosaminidase release (i.e., inhibitory effect on histamine release), an inhibitory effect on platelet aggregation, and an inhibitory effect on phospholipase A2 activity.Type: GrantFiled: January 15, 2010Date of Patent: October 22, 2013Assignee: Maruzen Pharmaceuticals Co., Ltd.Inventors: Yasuo Miyake, Ito Yoko
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Publication number: 20130259850Abstract: Uric acid in mammalian subjects is reduced and excretion of uric acid is increased by administering a compound of Formula I or a pharmaceutically acceptable salt thereof. In Formula I m is 0, 1, 2, 3 or 4; n is 0 or 1; m+n is not more than 4; t is 0 or 1; q is 0 or 1; and r is 0, 1 or 2. R6 is hydrogen, methyl or ethyl and R12 is hydrogen or methyl, or R6 is hydroxy and R12 is hydrogen, or R6 is O and R12 is absent, or R6 and R12 together are —CH2CH2—. R7 is hydrogen or alkyl having from 1 to 3 carbon atoms. One of R8 and R9 is alkyl having from 1 to 3 carbon atoms, and the other is hydrogen or alkyl having from 1 to 3 carbon atoms. R10 is hydrogen, halo, alkyl having from 1 to 3 carbon atoms or alkoxy having from 1 to 3 carbon atoms. X is C(O) and r is 0 and t is 0; or X is NH(R11) wherein R11 is hydrogen or alkyl having from 1 to 3 carbon atoms.Type: ApplicationFiled: May 9, 2013Publication date: October 3, 2013Applicant: WELLSTAT THERAPEUTICS CORPORATIONInventors: James Dennen O'NEIL, Michael K. BAMAT, Reid W. von BORSTEL, Shalini SHARMA, Ramachandran ARUDCHANDRAN
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Publication number: 20130243707Abstract: Topical compositions are disclosed that are useful for delivering a therapeutic level of an NSAID to a target within a subject having a local inflammatory disorder. A composition of the present invention comprises a Drug and a solvent system, wherein the solvent system comprises at least two solvent alcohols and wherein the solvent system is present in an amount sufficient to solubilize the Drug, the solvent system is a low alkanol system, and the composition is a single phase composition. Exemplary solvent systems are those for which one of the at least two solvent alcohols is polyethylene glycol, glycerin, butylene glycol, diproylene glycol, propylene glycol, ethanol, isopropanol, or a derivative thereof. Optionally the local inflammatory disorder is pseudofolliculitis barbae, dermatitis, psoriasis, wounds, or sunburn.Type: ApplicationFiled: March 28, 2013Publication date: September 19, 2013Inventors: Monique Renata GREEN, Kenton FEDDE
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Publication number: 20130224318Abstract: The present invention describes methods for improving the appearance of skin, particularly, treating, ameliorating, preventing, delaying, and/or improving one or more signs of excess accumulation and/or production of subcutaneous fat, such as cellulite, and conditions related thereto, by topically applying compositions comprising Carnitine Palmitoyl Transferase-1 (CPT-1) modulators, optionally with other anti-lipid agents; and also describes compositions and methods for treating, preventing and improving the appearance of skin, particularly, treating, preventing, ameliorating, reducing and/or eliminating loss of subcutaneous fat in the skin, wherein the compositions include natural plant constituents that stimulate lipid synthesis.Type: ApplicationFiled: February 26, 2013Publication date: August 29, 2013Applicant: Avon Products, Inc.Inventor: Avon Products, Inc.
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Patent number: 8501806Abstract: The present invention is directed in part to methods of preventing or reducing colon carcinogenesis comprising administering to a patient at risk of colorectal cancer, a pharmaceutical preparation comprising a chemopreventive agent disclosed herein.Type: GrantFiled: December 3, 2009Date of Patent: August 6, 2013Assignee: Nogra Pharma LimitedInventors: Sergio Baroni, Salvatore Bellinvia, Francesca Viti, Giovanni Monteleone
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Patent number: 8487000Abstract: Compounds useful for the treatment of various metabolic disorders, such as insulin resistance syndrome, diabetes, hyperlipidemia, fatty liver disease, cachexia, obesity, atherosclerosis and arteriosclerosis, are disclosed.Type: GrantFiled: December 6, 2004Date of Patent: July 16, 2013Assignee: Wellstat Therapertics CorporationInventors: Shalini Sharma, Reid W. von Borstel
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Publication number: 20130108602Abstract: Methods of decreasing, reducing, inhibiting, suppressing, limiting or controlling an undesirable or aberrant immune response, immune disorder, inflammatory response, or inflammation in a subject; decreasing, reducing, inhibiting, suppressing, limiting or controlling an autoimmune response, disorder or disease in a subject; and decreasing, reducing, inhibiting, suppressing, limiting or controlling an adverse cardiovascular event or cardiovascular disease in a subject, are provided. Methods include, for example, administering a Nur77 polypeptide or subsequence thereof, a Nur77 agonist, or CD14+ CD16+ monocytes or CD14dimCD16+ (CD115+CD11b+GR1? (Ly6C?)) monocytes or macrophages to a subject to decrease, reduce, inhibit, suppress, limit or control the underlying condition or an adverse symptom or pathology of the condition.Type: ApplicationFiled: October 5, 2012Publication date: May 2, 2013Applicant: LA JOLLA INSTITUTE FOR ALLERGY AND IMMUNOLOGYInventor: LA JOLLA INSTITUTE FOR ALLERGY AND IMMU
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Publication number: 20130065850Abstract: Alterations of certain metabolite concentrations and fluxes that occur in response to viral infection are described. Host cell enzymes in the involved metabolic pathways are selected as targets for intervention; i.e., to restore metabolic flux to disadvantage viral replication, or to further derange metabolic flux resulting in “suicide” of viral-infected cells (but not uninfected cells) in order to limit viral propagation. While any of the enzymes in the relevant metabolic pathway can be selected, pivotal enzymes at key control points in these metabolic pathways are preferred as candidate antiviral drug targets. Inhibitors of these enzymes are used to reverse, or redirect, the effects of the viral infection. Drug candidates are tested for antiviral activity using screening assays in vitro and host cells, as well as in animal models. Animal models are then used to test efficacy of candidate compounds in preventing and treating viral infections. The antiviral activity of enzyme inhibitors is demonstrated.Type: ApplicationFiled: April 3, 2012Publication date: March 14, 2013Applicant: THE TRUSTEES OF PRINCETON UNIVERSITYInventors: Josh MUNGER, Bryson BENNETT, Thomas SHENK, Joshua RABINOWITZ
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Publication number: 20120129931Abstract: This invention relates to caffeic acid derivatives and improving viability of neuronal cells by contacting neuronal cells by caffeic acid derivatives as shown in the specification.Type: ApplicationFiled: November 15, 2011Publication date: May 24, 2012Applicant: ChemiGenInventors: Junyi Liu, Yangsheng Du
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Publication number: 20120095051Abstract: This invention provides a compound having the structure wherein ?, ?, X, Y, and R1-R11 are defined herein. This invention also provides a pharmaceutical composition comprising the above compounds, a method of inhibiting the activity and/or levels of a matrix metalloproteinase (MMP), a method of inhibiting the production of a cytokine in a population of cells, a method of inhibiting the production of a growth factor in a population of cells, and a method of inhibiting NF?-B activation in a population of cells.Type: ApplicationFiled: May 14, 2010Publication date: April 19, 2012Inventors: Francis Johnson, Lorne Golub
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Publication number: 20120065179Abstract: There is provided a prodrug of a pharmaceutically active agent, such prodrug comprising a beta-keto carboxylic acid, a beta-keto carboxylic acid salt or a beta-keto carboxylic acid ester functional group, a pharmaceutical composition comprising the prodrug, and to the use of the prodrug or composition for treatment of a mammalian subject suffering from a condition which can be cured or alleviated by administration of the pharmaceutically active agent. There is further provided a method of inhibiting decarboxylation of a compound comprising a beta-keto carboxylic acid or a salt thereof with a monovalent cation, characterized in that a dry salt of the beta-keto carboxylic acid with a divalent or polyvalent cation is prepared.Type: ApplicationFiled: April 13, 2010Publication date: March 15, 2012Applicant: YKI, Ytemiska Institutet ABInventor: Martin Andersson
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Publication number: 20120022079Abstract: The invention relates to a process for producing formulations of sparingly water-soluble substances, said sparingly soluble substances being present in amorphous embedded form in a copolymer, and said copolymer being obtained by free-radically initiated polymerization of a mixture of i) 30 to 80% by weight of N-vinyllactam, ii) 10 to 50% by weight of vinyl acetate, and iii) 10 to 50% by weight of a polyether, with the proviso that the sum of components i), ii) and iii) equals 100% by weight, which comprises embedding the sparingly soluble substance into the copolymer at temperatures above the melting point of the sparingly soluble substances.Type: ApplicationFiled: March 30, 2010Publication date: January 26, 2012Applicant: BASF SEInventors: Kathrin Meyer-Böehm, Rainer Dobrawa, Stefan Fischer, Karl Kolter
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Publication number: 20120003282Abstract: Pharmaceutical compositions are provided comprising an active agent and a dextran polymer derivative. The compositions include from 0.01 to 99 wt % of an active agent and from 1 to 99.99 wt % of a dextran polymer derivative. The dextran polymer derivative is selected from dextran acetate, dextran propionate, dextran succinate, dextran acetate propionate, dextran acetate succinate, dextran propionate succinate, dextran acetate propionate succinate, and mixtures thereof.Type: ApplicationFiled: March 3, 2010Publication date: January 5, 2012Inventors: Warren K. Miller, David T. Vodak, Daniel E. Dobry, David K. Lyon, Dwayne T. Friesen, Michael M. Morgen, Corey J. Bloom, Daniel t. Smithey
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Publication number: 20110306539Abstract: A process for making particles for delivery of drug nanoparticles is disclosed herein. The process comprises the steps of (a) forming a suspension of drug nanoparticles by mixing a precipitant solution with an anti-solvent solution under micro-mixing environment, where the formed nanoparticles have a narrow particle size distribution; (b) providing an excipient to at least one of the precipitant solution, the anti-solvent solution and the suspension of drug nanoparticles, the excipient being selected to maintain said drug nanoparticles in a dispersed state when in liquid form; and (c) drying the suspension of drug nanoparticles containing the excipient therein to remove solvent therefrom, wherein removal of the solvent causes the excipient to solidify and thereby form micro-sized matrix particles, each micro-sized particle being comprised of drug nanoparticles dispersed in a solid matrix of the excipient.Type: ApplicationFiled: September 24, 2009Publication date: December 15, 2011Inventors: Zhigang Shen, Jimmy Sung Lai Yun, Jun Hu, Arvind Jugade, Jiyao Zhang, Wenhao Chen, Zhe Wang, Lingyan Gao, Jian Feng Chen
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Publication number: 20110294864Abstract: Aqueous gel-free two-phase coacervate compositions including a coacervate phase and an equilibrium water phase, comprising a mixture of: (a) a poorly water-soluble bio-active agent, (b) a tensio-active system consisting of non-ionic tensio-active agents, (c) one or more water-soluble carriers for said poorly water-soluble bio-active agent, said carriers being selected from the group consisting of maltodextrins and polyols, and (d) water. Such coacervate compositions may be dried into solid dosage forms from which rapid release of the bio-active agent can be obtained.Type: ApplicationFiled: July 12, 2011Publication date: December 1, 2011Applicant: Universiteit GentInventors: Jean Paul REMON, Chris VERVAET, Andre Bruno DA FONSECA ANTUNES
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Publication number: 20110263705Abstract: A topical or transdermal composition including a polar derivative of ketoprofen and a pharmaceutically acceptable topical or transdermal carrier, wherein the polar derivative of ketoprofen comprises a polarity that is greater than that of ketoprofen.Type: ApplicationFiled: July 1, 2011Publication date: October 27, 2011Inventors: Rod Hartwig, David Houze
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Publication number: 20110244017Abstract: The present invention provides an absorbable coating for an implantable device and the methods of making and using the same.Type: ApplicationFiled: March 31, 2010Publication date: October 6, 2011Applicant: ABBOTT CARDIOVASCULAR SYSTEMS INC.Inventors: Lothar W. Kleiner, Syed F.A. Hossainy, Mikael Trollsas, Stephen D. Pacetti
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Publication number: 20110160225Abstract: Disclosed herein are novel compositions and methods for treating or preventing a variety of disorders and conditions associated with lipid metabolism. The methods generally include administering to a patient in need thereof a therapeutically effective amount of a pharmaceutical composition comprising one or more fibric acid or statin derivative compositions alone or in combination with one or more lipid altering agents and/or PDE inhibitors.Type: ApplicationFiled: November 19, 2010Publication date: June 30, 2011Applicant: IRONWOOD PHARMACEUTICALS, INC.Inventors: Mark G. Currie, John Jeffrey Talley, Brian Cali
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Patent number: 7799954Abstract: Derivatives of dicarbonyl compounds having antitumor and antibiotic activity which can be used as anticancer agents.Type: GrantFiled: November 14, 2007Date of Patent: September 21, 2010Assignee: Abraxis BioScience, LLCInventors: Chunlin Tao, Qinwei Wang, Vuong Trieu, Neil Desai, Patrick Soon-Shiong
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Publication number: 20100151037Abstract: The present application relates to a method for preparing nanoparticles containing a poorly water-soluble pharmaceutically acceptable compound and compositions containing such nanoparticulates.Type: ApplicationFiled: August 6, 2009Publication date: June 17, 2010Inventors: Yivan Jiang, Zhiwei Jiang
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Publication number: 20100144874Abstract: The present invention relates to the combined use of a PPAR? agonist and metformin for decreasing serum triglycerides.Type: ApplicationFiled: February 12, 2010Publication date: June 10, 2010Applicant: Fournier Laboratories Ireland LimitedInventors: Jean-Louis Junien, Alan Edgar, Evelyne Chaput
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Patent number: 7728169Abstract: A pharmaceutical composition comprising a compound of formula (1) in polymorphic crystalline Form A: together with a pharmaceutically acceptable carrier or excipient, wherein the compound of formula (1) is present in polymorphic Form A (see, e.g., FIG. 6) substantially free of other polymorphic forms.Type: GrantFiled: April 21, 2008Date of Patent: June 1, 2010Assignee: Medicinova, Inc.Inventors: Kenneth Walter Locke, David Gregory Roe
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Publication number: 20100112049Abstract: Pharmaceutical compositions comprising micronized fenofibrate, a surfactant and a binding cellulose derivative as a solubilization adjuvant, wherein said compositions contain an amount of fenofibrate greater than or equal to 60% by weight and methods of producing fenofibrate compositions.Type: ApplicationFiled: January 13, 2010Publication date: May 6, 2010Applicant: ETHYPHARMInventors: Bruno Criere, Pascal Suplie, Philippe Chenevier, Pascal Oury, Keith S. Rotenberg, George Bobotas
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Publication number: 20100113477Abstract: The present invention provides aryl- or heteroaryl-diketo acid compounds effective to inhibit an activity of a Mycobacterial malate synthase enzyme or to inhibit a malate synthase activity in other bacteria having the enzyme. The compounds may be phenyl-naphthyl-, or thienyl-substituted diketo acids and carboxylate derivatives thereof. Also provided are methods of treating tuberculosis or other pathophysiological conditions associated with a malate synthase enzyme with the inhibitory compounds and methods of in silico design of the inhibitory compounds. In addition, the present invention provides the inhibitory compounds designed by this method. Furthermore, three-dimensional X-ray crystal structures of the Mycobacterial malate synthase complexed with the inhibitory compounds are provided. Further still a method for stabilizing an aromatic or heteroaromatic diketo acid or its prodrug or close analog in solution by derivatizing at least the ortho position on the aromatic ring is provided.Type: ApplicationFiled: October 20, 2009Publication date: May 6, 2010Inventors: Joel S. Freundlich, James C. Sacchettini, Inna V. Kriger, Thomas R. Ioerger, Vijay Gawandi
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Publication number: 20100081715Abstract: A formulation comprising i) fenofibric acid, a physiologically acceptable salt or derivative thereof a other active substances, ii) a binder component comprising at least one enteric binder, and optionally iii) other physiologically ceptable excipients is described. Fenofibric acid, the physiologically acceptable salt or derivative thereof is preferably in the form of a molecular dispersion in these formulations. An advantageous process for their preparation, in particular by melt extrusion, and the use of this formulation for oral administration of fenofibric acid, a physiologically acceptable salt or derivative thereof are likewise described.Type: ApplicationFiled: August 30, 2009Publication date: April 1, 2010Inventors: Joerg Rosenberg, Matthias Degenhardt, Joerg Breitenbach, Tom L. Reiland, Kennan C. Marsh
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Publication number: 20090324703Abstract: Curcuminoid formulations having enhanced bioavailability are provided and comprise a curcuminoid, antioxidant, glucuronidation inhibitor, and water-soluble, pharmaceutically acceptable inhibitor. A method of treating Alzheimer's and other age-related diseases by administering such a composition is also provided.Type: ApplicationFiled: March 6, 2007Publication date: December 31, 2009Inventors: Sally A. Frautschy, Gregory M. Cole
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Publication number: 20090318496Abstract: A preparation (pharmaceutical composition) reducing a concentration of a free fatty acid and/or fibrinogen in the blood is prepared. The preparation contains a statin agent comprising at least a statin compound having a benzopyridine skeleton (e.g., pitavastatin) and a fibrate agent (e.g., fenofibrate). The preparation is useful as a preventive or treating agent for hyper-free fatty acidemia, metabolic syndrome, or type II diabetes.Type: ApplicationFiled: August 4, 2006Publication date: December 24, 2009Inventors: Hashime Kanazawa, Masaya Morimoto, Naoto Tanimori
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Publication number: 20090318542Abstract: The present invention relates generally to ophthamological drugs. More specifically, the invention relates to a method of modifying (derivatizing) ophthamological drugs so as to increase their penetration through the cornea. The invention also relates to drugs modified (derivatized) in accordance with the instant method and to the use of same in treating conditions associated with elevated intraocular pressure, particularly, glaucoma.Type: ApplicationFiled: July 29, 2009Publication date: December 24, 2009Inventors: Eric J. Toone, David L. Epstein, Pratap Challa, Phillip W. Snyder, Xin Chen, Mitchell A. deLong
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Publication number: 20090227674Abstract: The present invention relates to a method of treating cancer in a subject in need thereof, by administering to a subject in need thereof a first amount of SAHA or a pharmaceutically acceptable salt or hydrate thereof, and a second amount of Targretin. The SAHA and Targretin may be administered to comprise therapeutically effective amounts.Type: ApplicationFiled: August 18, 2006Publication date: September 10, 2009Inventors: Victoria M. Richon, Stanley R. Frankel, Steven Averbuch
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Publication number: 20090202649Abstract: The present invention relates to pharmaceutical formulations comprising fenofibrate. The invention also relates to stable and bioavailable pharmaceutical formulations comprising fenofibrate. Further the invention also relates to processes for preparing the compositions and/or formulations of fenofibrate and their methods of use, treatment and administration.Type: ApplicationFiled: February 5, 2009Publication date: August 13, 2009Inventors: Subhash Gore, Anand Sankaranarayanan, Balaji Sathurappan, Raviraj Sukumar Pillai, Pradip Kumar Ghosh, S.H. Seyed Mohamed Buhary, Sainath Kalisetty, Pratit Premchand Agrawal, Manikandan Ramalingam, Venugopal Kumaran, Ajay Kumar Reddy Thupalli