Chalcogens Bonded Directly To At Least Two Ring Carbons Of The Six-membered Hetero Ring Patents (Class 514/348)
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Publication number: 20120058945Abstract: 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, e.g., a neurodegenerative or cerebrovascular disease or disorder, a neoplastic disease, hemochromatosis, thalassemia, a cardiovascular disease, diabetes, an inflammatory disorder, anthracycline cardiotoxicity, a viral infection, a protozoal infection, a yeast infection, retarding aging, and prevention and/or treatment of skin aging 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. A combined antiapoptotic and neuroprotective function is provided by a propargyl group.Type: ApplicationFiled: November 14, 2011Publication date: March 8, 2012Applicants: Yeda Research and Development Co., Ltd., Technion Research and Development Foundation Ltd.Inventors: MOUSSA YOUDIM, Matitiyahu Fridkin, Hailin Zheng, Abraham Warshawsky, Rivka Warshawsky
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Publication number: 20120053212Abstract: A human undergoing an injection of a contrast agent is treated by the administration of an iron chelator. Administration of the iron chelator can essentially prevent the onset of acute renal failure in a human. Administration of the iron chelator can reduce the severity of the acute renal failure and/or reduce the severity of kidney disease consequent to the acute renal failure.Type: ApplicationFiled: March 29, 2011Publication date: March 1, 2012Applicant: Shiva Biomedical, LLCInventor: Sudhir V. Shah
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Publication number: 20120046226Abstract: The invention concerns a novel treatment multiple sclerosis, based on induced anaemia, followed by administration of an erythropoiesis-stimulating agent (ESA). In a preferred embodiment, the ESA is darbopoietin alpha, CERA or Hematide. The anaemia is induced by successive bloodlettings or by administration of an iron chelator, such as deferiprone, deferoxamine, polyanionic amines, substituted polyaza compounds, desferrithiocon, hydroxybenzyl-ethylenediamine-diacetic acid and pyridoxal isonicotinoyl hydra z one.Type: ApplicationFiled: February 12, 2010Publication date: February 23, 2012Applicant: Assis-tance Publique - Hopitaux de ParisInventors: Alain Creange, Frédéric Galacteros, Jean-Pascal Lefaucheur
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Publication number: 20120045496Abstract: A composition for treating fabric includes about 0.1 to about 10.0% cross linking agent, about 0.1 to about 5.0% of a material selected from a group consisting of oxidized polyolefin, polyolefin and mixtures thereof, about 0.1 to about 0.5% wetting agent, about 1.0 to about 14.0% of a material selected from a group consisting of aminofunctional silicone, ionizing agent and mixtures thereof, about 0.0 to about 2.0% catalyst, about 1.0 to about 3.0% antimicrobial/antibacterial/antifungal agent and any remainder as a carrier. The composition has a pH of between about 2.0 to about 4.0. A performance fabric treated with the composition and a method of treating a performance fabric are also provided.Type: ApplicationFiled: February 12, 2009Publication date: February 23, 2012Inventors: Dan C. Short, Bryan S. Short, Albert B. Quimet
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Publication number: 20120041032Abstract: The present invention relates to metalloprotein inhibitors comprising: a. an organic substituent and at least one zinc binding group (ZBG) covalently attached thereto; or b. a ZBG substituted by a side chain wherein the ZBG is of formula (I): wherein X is O or S and each R1, R2, R3, and R4 is individually hydrogen or an organic radical. The metalloprotein inhibitors are useful for preventing or treating a pathological disease, condition, or symptom that is associated with pathological metalloprotein activity and/or that is alleviated by inhibition of said activity.Type: ApplicationFiled: August 15, 2011Publication date: February 16, 2012Applicant: The Regents of the University of California, San DiegoInventors: David T. Puerta, Seth M. Cohen, Jana A. Lewis
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Publication number: 20120027723Abstract: The present invention relates to taurine or taurine-like substances for the prevention and treatment of a disease associated with retinal ganglion cell degeneration. More particularly the invention relates to a substance selected from the group consisting of taurine, a taurine precursor, a taurine metabolite, a taurine derivative, a taurine analog and a substance required for the taurine biosynthesis for the prevention and treatment of a disease associated with retinal ganglion cell degeneration.Type: ApplicationFiled: July 26, 2011Publication date: February 2, 2012Inventor: Serge Picaud
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Patent number: 8097624Abstract: The present invention provides an cycloalkyl derivative of 3-hydroxy-4-pyridinone which is useful for the chelation of metal ions such as iron. Its preparation and use is described. In particular, the invention concerns the removal of iron in chemical and biological systems including chelating agents having the formula I wherein R1 is X with the proviso that R2 is Y; or R1 is T with the proviso that R2 is W; or R1 is X with the proviso that R2R5N when taken together form a heterocyclic ring selected from piperidinyl, morpholinyl, pyrrolidinyl or piperazinyl, wherein the group piperidinyl, morpholinyl, pyrrolidinyl or piperazinyl is either unsubstituted or substituted with one to three C1 to C6 alkyl groups.Type: GrantFiled: May 9, 2008Date of Patent: January 17, 2012Assignee: Apotex Inc.Inventors: Tim Fat Tam, Michael Spino, Wanren Li, Yingsheng Wang, Yanqing Zhao, Birenkumar Hasmukhbhai Shah
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Publication number: 20120010185Abstract: The present invention relates to compounds of general formula I wherein the groups and radicals B, k, L, U, V, W, X, Y, Z, R1, R2, have the meanings given in claim 1. Moreover the invention relates to pharmaceutical compositions containing at least one compound according to the invention. By virtue of their MCH-receptor antagonistic activity the pharmaceutical compositions according to the invention are suitable for the treatment of metabolic disorders and/or eating disorders, particularly obesity, bulimia, anorexia, hyperphagia and diabetes.Type: ApplicationFiled: September 22, 2011Publication date: January 12, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Dirk STENKAMP, Stephan Georg MUELLER, Gerald Juergen ROTH, Joerg KLEY, Klaus RUDOLF, Armin HECKEL, Marcus SCHINDLER, Ralf LOTZ, Thorsten LEHMANN-LINTZ
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Publication number: 20120004166Abstract: The invention relates to aryloxyalkylene-substituted hydroxyphenylhexynoic acid derivatives, and to physiologically compatible salts thereof. The invention relates to compounds of the formula I in which R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14 and A are each defined as specified, and physiologically compatible salts thereof. The compounds are suitable, for example, for treatment of diabetes.Type: ApplicationFiled: July 5, 2011Publication date: January 5, 2012Applicant: SANOFIInventors: Stefanie KEIL, Elisabeth DEFOSSA, Viktoria DIETRICH, Siegfried STENGELIN, Andreas HERLING, Guido HASCHKE, Thomas KLABUNDE
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Publication number: 20120004167Abstract: The invention relates to substituted (2-aryloxyacetylamino)phenylpropionic acid derivatives, and to the physiologically acceptable salts thereof. The invention relates to compounds of the formula I in which R1, R2, R3, R4, R5, R6, R7, R8, R9 and A are each defined as specified, and the physiologically compatible salts thereof. The compounds are suitable, for example, for treatment of diabetes.Type: ApplicationFiled: July 5, 2011Publication date: January 5, 2012Applicant: SANOFIInventors: Elisabeth DEFOSSA, Stefanie KEIL, Viktoria DIETRICH, Siegfried STENGELIN, Andreas HERLING, Guido HASCHKE, Thomas KLABUNDE
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Publication number: 20110312911Abstract: Glucagon receptor antagonist compounds are disclosed. The compounds are useful for treating type 2 diabetes and related conditions. Pharmaceutical compositions and methods of treatment are also included.Type: ApplicationFiled: February 3, 2010Publication date: December 22, 2011Inventors: Roman Kats-Kagan, Christian P. Stevenson, Xibin Liao, Qinghong Fu, Emma R. Parmee, Songnian Lin
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Publication number: 20110294783Abstract: The present invention concerns boosting the activity of crop protection materials comprising inhibitors of fatty acid biosynthesis (for example phenyl-substituted cyclic ketoenols) through the addition of ammonium salts and/or phosphonium salts or through the addition of ammonium salts and/or phosphonium salts and penetrants, the corresponding materials, processes for preparing them, and their use in crop protection.Type: ApplicationFiled: August 10, 2011Publication date: December 1, 2011Applicant: BAYER CROPSCIENCE AGInventors: Reiner FISCHER, Stefan LEHR, Peter MARCZOK, Udo Reckmann, Christian Arnold, Waltraud Hempel, Erich SANWALD, Rolf Pontzen
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Publication number: 20110294800Abstract: The present invention provides, inter alia, a compound of formula I: wherein the substituent designations are indicated in the Specification. The present invention also provides pharmaceutical compositions comprising a compound of formula I, and methods of treatment or prevention of diabetes or hyperglycemia in a patient, and of normalizing blood glucose levels in a subject, by administering an effective amount of a compound of formula I.Type: ApplicationFiled: August 7, 2009Publication date: December 1, 2011Applicant: The Trustees Of Columbia University in the City of New YorkInventors: Yuli Xie, Shixian Deng, Donald W. Landry, Paul Harris, Antonella Maffei
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Publication number: 20110290693Abstract: Therapeutic compositions, devices and protocols for the treatment of keloids and other abnormal scars with improved appearance and a much lower recurrence rate. A therapeutic drug delivery device comprises an injectable mixture of a fibroblast inhibitor such as corticosteroid and a slow release carrier such as milled gel sponge dispersed in a fluid medium such as biological saline. The composition can be injected perilesionally in the dermis following excision of the keloid or other scar tissue, to circumscribe the wound. The infiltration of the mixture around the wound can provide a slow release of the fibroblast inhibitor for an extended period of time until normal wound closure can dominate and keloid or abnormal scar recurrence is inhibited.Type: ApplicationFiled: May 30, 2011Publication date: December 1, 2011Inventor: Canaan Vernon Lavelle Harris
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Patent number: 8067444Abstract: The present invention provides pharmaceutical compositions comprising dosage units of pyridoxamine, or a pharmaceutically acceptable salt thereof; and a pharmaceutically acceptable carrier, and methods for their use in limiting the progression of renal disease and/or diabetic complications in human diabetic patient.Type: GrantFiled: January 25, 2008Date of Patent: November 29, 2011Assignee: NephroGenex, Inc.Inventors: Degenhardt Thorsten, Schotzinger Robert, Fox J. Wesley
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Publication number: 20110281916Abstract: The present invention provides compounds having formula (I): and additionally provides methods for the synthesis thereof, compositions thereof, and methods for the use thereof in the treatment of various disorders including cancer, metastasis and disorders involving increased angiogenesis, wherein R1-R6, Ra-Rc, Q, Y1, Y2 and n are as defined herein.Type: ApplicationFiled: May 12, 2011Publication date: November 17, 2011Applicant: SLOAN-KETTERING INSTITUTE FOR CANCER RESEARCHInventors: Samuel J. Danishefsky, Christoph Gaul, Jon T. Njardarson
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Publication number: 20110256237Abstract: Methods and compositions are described for treating acne vulgaris and acne rosacea by administering compositions suitable for oral administration. Suitable compositions contain high dosages of the vitamin nicotinamide combined with much lower dosages of azelaic acid.Type: ApplicationFiled: April 16, 2010Publication date: October 20, 2011Applicant: ELORAC, INC.Inventor: Joel E. Bernstein
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Publication number: 20110245227Abstract: Novel compounds are provided which are GPR119 G protein-coupled receptor modulators. GPR119 G protein-coupled receptor modulators are useful in treating, preventing, or slowing the progression of diseases requiring GPR119 G protein-coupled receptor modulator therapy. These novel compounds have the structure Formula I or Formula IA.Type: ApplicationFiled: June 14, 2011Publication date: October 6, 2011Inventors: Dean A. Wacker, Karen A. Rossi, Ying Wang
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Publication number: 20110237535Abstract: The invention provides methods for screening test compounds or toxins for effects on cells. The invention also provides methods for determining frequency, amplitude and kinetic profiles of cells.Type: ApplicationFiled: March 28, 2011Publication date: September 29, 2011Inventors: Alexander Yuzhakov, Eric Sandberg, Steven Shamah, Rick Wagner
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Patent number: 8026261Abstract: The present invention relates to novel derivatives of deferiprone. In particular, the present invention relates to fluorinated derivatives of deferiprone or pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising same, processes for the manufacture thereof and their use in the treatment of neurodegenerative diseases caused by the presence of free iron or iron accumulation in neural tissues and in diseases wherein excess iron must be removed or redistributed.Type: GrantFiled: March 27, 2008Date of Patent: September 27, 2011Assignee: Apotex Technologies Inc.Inventors: Tim Fat Tam, Regis Leung-Toung, Yingsheng Wang, Yanqing Zhao
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Publication number: 20110230522Abstract: The present invention relates to combinations of a thiol group modulating enzyme inhibitor and a pyrion compound which provide an improved protecting effect against fouling organisms, fungi or bacteria. More particularly, the present invention relates to compositions comprising a combination of a thiol group modulating enzyme inhibitor selected from dichlofluanid, tolylfluanid, dithane, thiram, ziram, or zineb, together with a pyrion compound selected from 1-hydroxy-2-pyridinone, ciclopirox, ciclopirox olamine, piroctone, piroctone olamine, rilopirox, pyrion disulfide, sodium pyrithione and zinc pyrithione; in respective proportions to provide a synergistic effect against fouling organisms, fungi or bacteria and the use of these compositions for protecting materials against fouling organisms, fungi or bacteria.Type: ApplicationFiled: November 26, 2009Publication date: September 22, 2011Inventors: Jan Pieter Hendrik Bosselaers, Dany Leopold Jozefien Bylemans, Tony Mathilde Jozef Kempen
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Patent number: 8022221Abstract: The present invention relates to chemical compounds having a general formula I wherein A1, A2, C1, C2, D, L1, L2, Z and R3, R4, R6, R7 and R8 are defined herein, which are capable of modulating Aurora kinase protein activity, thereby influencing various disease states and conditions related to the activities of Aurora kinase proteins. For example, the compounds are capable of influencing the process of cell cycle and cell proliferation to treat cancer and cancer-related diseases. The invention also includes pharmaceutical compositions, processes of preparing compounds of the invention, synthetic intermediates and methods of treatment of conditions related to the activity of Aurora kinase.Type: GrantFiled: February 12, 2009Date of Patent: September 20, 2011Assignee: Amgen Inc.Inventors: Victor J. Cee, Holly L. Deak, Bingfan Du, Stephanie D. Geuns-Meyer, Brian L. Hodous, Hanh Nho Nguyen, Philip R. Olivieri, Vinod F. Patel, Karina Romero, Laurie Schenkel
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Publication number: 20110213001Abstract: The object of the present invention is to provide a pharmaceutical composition that inhibits expression of iNOS and COX-2 without inhibiting NF-?B. The pharmaceutical composition that inhibits expression of iNOS and COX-2 without inhibiting NF-?B contains DTCM glutarimide of the Formula (I) as an effective ingredient, thereby being able to inhibit nitric oxide (NO) production and prostaglandin production.Type: ApplicationFiled: June 25, 2009Publication date: September 1, 2011Applicant: KEIO UNIVERSITYInventors: Kazuo Umezawa, Yuichi Ishikawa, Shigeru Nishiyama, Miyuki Tachibana, Ayumi Kaneda
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Publication number: 20110206638Abstract: The disclosure provides compositions and methods for reducing the mutation rate of a virus, such as an RNA virus or a DNA virus, in a cell infected with the virus by, in one aspect, contacting the cell with an effective amount of an iron chelator or an antioxidant. Also provided are compositions and methods for enhancing the efficacy of an agent or a therapy directed at a virus.Type: ApplicationFiled: January 19, 2011Publication date: August 25, 2011Inventor: Jinah Choi
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Publication number: 20110195993Abstract: The present invention relates to novel PPAR agonist compounds as well as pharmaceutical compositions containing them. The compounds according to the invention are of quite particular therapeutic interest, notably for treating diabetes and/or dyslipidemias, as well as for preventing cardiovascular pathologies.Type: ApplicationFiled: May 26, 2009Publication date: August 11, 2011Inventors: Christophe Masson, Karine Caumont-Bertrand
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Patent number: 7989478Abstract: The present invention relates to a cinnamoyl compound represented by the formula (I):Type: GrantFiled: September 16, 2004Date of Patent: August 2, 2011Assignee: Sumitomo Chemical Company, LimitedInventors: Yoshitaka Tomigahara, Kiyoshi Higashi, Junya Takahashi, Chizuko Takahashi
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Publication number: 20110184029Abstract: The present invention relates to 2-pyridone derivatives of Formula I or IV as herein described, compositions containing such compounds, synthetic processes for making such compounds, and therapeutic methods that include the administration of such compounds.Type: ApplicationFiled: July 13, 2009Publication date: July 28, 2011Applicant: KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGYInventors: Choung U. Kim, Michael L. Mitchell, Jong Chan Son
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Publication number: 20110183998Abstract: Heterocyclic derivatives, processes for their preparation, medicaments comprising these compounds, and the use thereof. The invention relates to compounds of the formula I in which the radicals R1, R2, R3, R4, W, A, B, D, E, G, L, M, R, T and Y have the stated meanings, and to the physiologically tolerated salts thereof. The compounds are suitable for example for the treatment of the metabolic syndrome, insulin resistance, obesity and diabetes.Type: ApplicationFiled: July 7, 2009Publication date: July 28, 2011Applicant: SANOFI-AVENTISInventors: Gerhard Zoller, Dieter Schmoll, Marco Mueller, Guido Haschke, Ingo Focken
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Publication number: 20110178045Abstract: The present invention discloses a method to induce fatty liver in an animal. The steps of the method comprise: feeding an animal with a high calorie diet, and injecting a mitochondrial inhibitor into the animal to inhibit the mitochondrial activity of the animal, then resulting in fat accumulation and inflammation in the liver of the animal.Type: ApplicationFiled: July 8, 2010Publication date: July 21, 2011Applicant: TAIPEI MEDICAL UNIVERSITYInventors: Rong-Hong Hsieh, Sheng-Mei Lin
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Patent number: 7973060Abstract: A compound which is effective for inhibiting Fab I, and a method for treating a bacterial infection.Type: GrantFiled: October 11, 2006Date of Patent: July 5, 2011Assignee: CrystalGenomics, Inc.Inventors: Cheol Min Kim, Dong Gyu Shin, Seonggu Ro, Joong Myung Cho, Young Lan Hyun
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Publication number: 20110144167Abstract: The invention described herein relates to certain pyrimidinedione N-substituted glycine derivatives of formula (I) which are antagonists of HIF prolyl hydroxylases and are useful for treating diseases benefiting from the inhibition of this enzyme, anemia being one example.Type: ApplicationFiled: August 21, 2009Publication date: June 16, 2011Applicant: SMITHKLINE BEECHAM CORPORATIONInventor: Rosanna Tedesco
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Patent number: 7951822Abstract: The object is to provide a novel LXR? agonist that is useful as a preventative and/or therapeutic agent for atherosclerosis; arteriosclerosis such as those resulting from diabetes; dyslipidemia; hypercholesterolemia; lipid-related diseases; inflammatory diseases that are caused by inflammatory cytokines; skin diseases such as allergic skin diseases; diabetes; or Alzheimer's disease. The solving means is a 1,3-dihydroisobenzofuran derivative represented by the following general formula (1) or salt thereof, or their solvate.Type: GrantFiled: March 30, 2009Date of Patent: May 31, 2011Assignee: Kowa Company, Ltd.Inventors: Ayumu Okuda, Takayuki Matsuda, Toru Miura, Koichi Yamazaki, Yuki Yamaguchi, Minoru Koura, Sayaka Kurobuchi, Yuichiro Watanabe, Kimiyuki Shibuya
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Publication number: 20110124648Abstract: The present invention discloses novel compounds of Formula I, or pharmaceutically acceptable salts thereof, which have glucagon receptor antagonist or inverse agonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I as well as methods of using them to treat diabetic and other glucagon related metabolic disorders, and the like.Type: ApplicationFiled: January 25, 2011Publication date: May 26, 2011Applicant: ELI LILLY AND COMPANYInventors: Scott Eugene CONNER, Guoxin ZHU, Jianke LI
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Publication number: 20110118300Abstract: The present invention provides, inter alia, dihydropyridone compounds and compositions, including analogs of a vesicular monoamine transporter type 2 (VMAT2) antagonist. The present invention also provides methods of using such compounds/analogs for modulating glucose levels, and/or preventing, treating, or ameliorating the effects of diabetes and hyper-glycemia.Type: ApplicationFiled: April 10, 2009Publication date: May 19, 2011Inventors: Paul Harris, Antonella Maffei, Yuli Xie, Donald Landry
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Publication number: 20110118217Abstract: Short chain fatty acids (SCFAs) and glycerol esters of SCFAs not previously used for that purpose are provided for use as a medicament for treating, preventing or counteracting microbial infections in animals, including humans, by stimulating the innate antimicrobial peptide defense system. Preferred compounds include phenyl substituted short chain fatty acids (SCFAs) derivatives and. Also provided are methods and compositions for treating, preventing or counteracting microbial infections, including bacterial, viral, fungal, and parasitic infections, by administration of medicaments comprising a secretagogue-effective amount of the compounds of the invention.Type: ApplicationFiled: December 11, 2008Publication date: May 19, 2011Applicant: Akthelia PharmaceuticalsInventors: Gudmundur Hrafn Gudmundsson, Birgitta Agerberth, Eirikur Steingrimsson, Roger Stromberg, Raqib Rubhana
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Publication number: 20110111058Abstract: Disclosed herein are methods for controlling the activity of hypoxia-inducible transcription factor 1-alpha (HIF-1?) and diseases, conditions, or syndromes related thereto, inter alia, Peripheral Vascular Disease (PVD), Coronary Artery Disease (CAD), heart failure, ischemia, and anemia. Further disclosed are pharmaceutical compositions comprising HIF-1? prolyl hydroxylase inhibitors useful in treating diseases, conditions, and/or syndromes related thereto the activity of HIF-1?.Type: ApplicationFiled: November 5, 2010Publication date: May 12, 2011Inventors: Robert Shalwitz, Joseph H. Gardner
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Publication number: 20110112113Abstract: The invention provides methods for treatment of acute coronary syndrome and prediction of adverse cardiac events on the basis of elevations of catalytic iron in biological fluid of a human subject. An embodiment of the invention provides a method for early detection of acute coronary syndrome (ACS) in a human subject at the time of presentation of the chest pain. The method includes analyzing a test sample of the biological fluid for amount of catalytic iron and detecting acute coronary syndrome in the human subject.Type: ApplicationFiled: September 15, 2010Publication date: May 12, 2011Inventors: Mohan Rajapurkar, Suhas Lele, Sudhir Shah
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Publication number: 20110092550Abstract: The present invention relates to combinations of imazalil, or a salt thereof, and hydroxypyridones which provide an improved biocidal effect. More particularly, the present invention relates to compositions comprising a combination of imazalil, or a salt thereof, together with one or more hydroxypyridones selected from 1-hydroxy-2-pyridinone, ciclopirox, ciclopirox olamine, piroctone, piroctone olamine and rilopirox in respective proportions to provide a synergistic biocidal effect. Compositions comprising these combinations are useful for the protection of any living or non-living material, such as crops, plants, fruits, seeds, objects made of wood, thatch or the like, engineering material, biodegradable material and textiles against deterioration due to the action of microorganisms such as bacteria, fungi, yeasts, algae, viruses, and the like.Type: ApplicationFiled: August 28, 2008Publication date: April 21, 2011Inventors: Jan Pieter Hendrik Bosselaers, Dany Leopold Jozefien Bylemans, Tony Mathilde Jozef Kempen, Hans Bernhard Leithoff, Amber Paula Marcella Thys, Mark Arthur Josepha Van Der Flaas
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Patent number: 7919509Abstract: To provide a novel LXR? agonist that is useful as a preventative and/or therapeutic agent for atherosclerosis; arteriosclerosis such as those resulting from diabetes; dyslipidemia; hypercholesterolemia; lipid-related diseases; inflammatory diseases that are caused by inflammatory cytokines; skin diseases such as allergic skin diseases; diabetes; or Alzheimer's disease. [Solving Means] A 2-oxochromene derivative represented by the following general formula (1) or salt thereof, or their solvate.Type: GrantFiled: February 27, 2009Date of Patent: April 5, 2011Assignee: Kowa Company, Ltd.Inventors: Ayumu Okuda, Takayuki Matsuda, Toru Miura, Hidefumi Ozawa, Ayako Tosaka, Koichi Yamazaki, Yuki Yamaguchi, Sayaka Kurobuchi, Yuichiro Watanabe, Kimiyuki Shibuya
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Publication number: 20110071164Abstract: This invention relates to the use of ERG channel openers for the treatment of cardiac arrhythmias, and to the use of specific compounds for such treatment. In a separate aspect the invention provides novel compounds useful as ERG channel openers.Type: ApplicationFiled: November 9, 2010Publication date: March 24, 2011Inventors: Søren Peter OLESEN, Morten Grunnet, Palle Christophersen, Dorte STRØBÆK, Joachim Demnitz, Rie S. Hansen
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Publication number: 20110065758Abstract: Methods of diagnosing Helicobacter pylori infection or associated conditions are based in part on the correlation of the presence of a ?-L-fucosidase 2 marker with the infection. Methods and compositions for treating or preventing Helicobacter pylori infection or associated conditions are based in part on administering an ?-L-fucosidase 2 inhibitor to an infected subject or a subject at risk of developing the infection.Type: ApplicationFiled: August 2, 2010Publication date: March 17, 2011Inventor: Chun-Hung Lin
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Patent number: 7906536Abstract: This invention is directed generally to processes for the preparation of compounds of Formula I: wherein R2, R3, R4, R5, X1, X2, X3, X4, X5, X6 are as defined in the specification.Type: GrantFiled: December 12, 2007Date of Patent: March 15, 2011Assignee: Pfizer IncInventors: Daniel Dukesherer, Michael Mao, Richard Vonder Embse, Gopi Yalamanchili, Rajappa Vaidyanathan, Brian Chekal, George Klemm, Ronald VanderRoest, Randy Geurink
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Publication number: 20110052613Abstract: Provided is a method of increasing the stability of wild-type ?-glucocerebrosidase. Also provided are methods of treating and/or preventing an individual having a neurological disease in which increased expression or activity of ?-glucocerebrosidase in the central nervous system would be beneficial. This method comprises administering an effective amount of a pharmacologic chaperone for ?-glucocerebrosidase, with the proviso that the individual does not have a mutation in the gene encoding ?-glucocerebrosidase. Further provided are ?-glucocerebrosidase inhibitors which have been identified as specific pharmacologic chaperones and which have been shown to increase activity of ?-glucocerebrosidase in vivo in the central nervous system.Type: ApplicationFiled: November 8, 2010Publication date: March 3, 2011Applicant: AMICUS THERAPEUTICS, INC.Inventor: Brandon Alan Wustman
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Patent number: 7897624Abstract: This invention concerns N-(ortho phenylamino dihydropyridyl)sulfonamides and N-(ortho phenylamino dihydropyridyl), N?-alkyl sulfamides which are inhibitors of MEK and are useful in the treatment of cancer and other hyperproliferative diseases.Type: GrantFiled: April 18, 2007Date of Patent: March 1, 2011Assignee: Ardea BiosciencesInventors: Shunqi Yan, Jean-Michel Vernier, Zhi Hong, Suetying Chow, Yung-hyo Koh
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Publication number: 20110039897Abstract: An oral pharmaceutical liquid formulation comprising deferiprone and a taste masking composition, said taste masking composition comprising an effective amount of a sweetener (such as sucralose) per litre of liquid composition, an effective amount of a thickening and suspension aid, (for example hydroxyethylcellulose), per litre of liquid composition, an effective amount of a humectant (such as glycerin) per litre of liquid composition, and an effective amount of at least one flavoring agent, wherein a final form of said taste-masked pharmaceutical has a substantially non-bitter and palatable taste.Type: ApplicationFiled: April 25, 2008Publication date: February 17, 2011Applicant: APOTEX TECHNOLOGIES INC.Inventors: Michael Spino, Anita Hui, Cihua Yang, Mohammed N. Kabir
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Patent number: 7868026Abstract: The present invention provides compounds of formula (I), or pharmaceutically acceptable salts or solvates thereof, methods for their preparation, methods for their use, and pharmaceutical formulations comprising them.Type: GrantFiled: January 9, 2007Date of Patent: January 11, 2011Assignee: Pfizer Inc.Inventors: Mitchell David Nambu, Leena Bharat Kumar Patel, Brian Douglas Patterson, Sylvie Kim Sakata, John Howard Tatlock
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Publication number: 20110003013Abstract: The present invention provides a method for increasing metabolism and/or energy expenditure in a subject, e.g., to treat or prevent obesity and/or a related condition and/or to reduce adiposity, the method comprising increasing the level and/or activity of Hypoxia Induced Factor 1? (HIF-1?) in a cell, tissue or organ of the subject, thereby increasing metabolism in the subject. The present invention also provides a method for increasing metabolism in a subject, the method comprising administering an iron chelating agent to the subject, thereby increasing metabolism in the subject.Type: ApplicationFiled: January 5, 2009Publication date: January 6, 2011Inventor: Jenny Gunton
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Publication number: 20100324001Abstract: Methods of inhibiting the cytokine or biological activity of Macrophage Migration Inhibitory Factor (MIF) comprising contacting MIF with a compound of formula (I) are provided. The invention also relates to methods of treating diseases or conditions where MIF cytokine or biological activity is implicated comprising administration of compounds of formula (I), either alone or as a part of combination therapy. Novel compounds of formula (I) are also provided for.Type: ApplicationFiled: June 30, 2010Publication date: December 23, 2010Applicant: Cortical Pty LTDInventors: Eric Francis Morand, Magdy Naguib Iskander, Colin Edward Skene
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Patent number: 7850955Abstract: Gelling agents which contain a specific N-acylamino acid monoamide monoalkyl ester have a melting temperature of about 100° C., are capable of solidifying a wide variety of oily base materials including silicones, and do not cause “sweating” while retaining a practical level of gel strength. When applied to skin, the resulting gels have a good feeling, good spreadability, and good fittability to skin.Type: GrantFiled: July 3, 2008Date of Patent: December 14, 2010Assignee: Ajinomoto Co., Inc.Inventors: Keitaro Saito, Takanori Sugimoto, Tatsuya Hattori
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Publication number: 20100310493Abstract: Acetamide derivatives, their stereoisomers, tautomers, prodrugs, pharmaceutically acceptable salts, polymorphs, solvates and formulations thereof for the prophylaxis, management, treatment, control of progression, or adjunct treatment of diseases and/or medical conditions where the activation of glucokinase would be beneficial, are disclosed. The disclosure also provides process of preparation of these acetamide derivatives.Type: ApplicationFiled: October 7, 2008Publication date: December 9, 2010Applicant: ADVINUS THERAPEUTICS PRIVATE LIMITEDInventors: Debnath Bhuniya, Sandeep Bhausaheb Bhosale, Gobind Sing Kapkoti, Venkata Poornapragnacharyulu Palle, Siddhartha De, Kasim A. Mookhtiar, Bhavesh Dave, Anil Deshpande, Santosh Kurhade, Balasaheb Kobal, Keshav Naik, Sachin Kandalkar