The Carbonyl Is In A -coo- Group Patents (Class 546/318)
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Patent number: 10343997Abstract: An ursolic acid derivative can have the following structural formula: The ursolic acid derivative exhibits potent selective calcium channel blocker activities and may be used to treat a disease or condition for which calcium channel regulation is useful.Type: GrantFiled: December 4, 2018Date of Patent: July 9, 2019Assignee: King Saud UniversityInventors: Abd El-Galil E. Amr, Mohamed A. Al-Omar, Abdulrahman A. Almehizia, Mohammed Mater Alanazi, Nawaf Abdulaziz Alsaif, Ahmad Jomah Obaidullah
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Patent number: 9834570Abstract: A regioselective N-Heterocyclic Carbene (NHC) catalyzed one step process for high yield synthesis of ?-acyloxy carbonyl compounds is disclosed.Type: GrantFiled: June 3, 2014Date of Patent: December 5, 2017Assignee: COUNCIL OF SCIENTIFIC AND INDUSTRIAL RESEARCHInventors: Arumugam Sudalai, Rambabu Reddi, Pushpa Malekar
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Patent number: 9617240Abstract: Provided are a compound expressed by formula (I) or a pharmacologically permissible salt thereof, as well as a drug or drug composition that contains this compound as an active ingredient, having a xanthine oxidase inhibiting effect that is very useful for treating or preventing diseases that are contributed to by xanthine oxidase, such as gout, hyperuricemia, tumor lysis syndrome, urinary tract stones, hypertension, dyslipidemia, diabetes, cardiovascular disease such as heart failure and arterial sclerosis, renal disease such as diabetic near opacity and the like, respiratory disease such as chronic obstructive pulmonary disease and the like, autoimmune diseases such as inflammatory bowel disease, and the like. [In the formula, A, X, Y, Z, R, and R1 have the meaning set forth in claim 1].Type: GrantFiled: March 28, 2014Date of Patent: April 11, 2017Assignee: Teijin Pharma LimitedInventors: Asahi Kawana, Chikashi Kanazawa, Masayuki Tera, Yoshimasa Takahashi, Mariko Imazeki, Hiroyuki Takahashi, Akira Tanokura
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Publication number: 20150126462Abstract: The present invention relates to a new pharmaceutical composition containing nicotinic acid, nicotinamide, tryptophanor related compounds for positively influencing the intestinal microbiota. In certain embodiments, the pharmaceutical composition is partially or entirely released into the small intestine or large intestine.Type: ApplicationFiled: June 14, 2013Publication date: May 7, 2015Applicant: CONARIS RESEARCH INSTITUTE AGInventors: Georg Waetzig, Dirk Seegert
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Publication number: 20140364586Abstract: Reagents and methods for functionalizing polypeptides with moieties (alkylene glycol) molecules and glycan groups are disclosed that are based on a functionalizing reagent which comprises a nitrogen containing heterocyclic aromatic ring having a vinyl substituent that is capable of reacting with one or more thiol groups that are naturally present, or have been introduced into, the polypeptide, for example by employing a thiol group of one or more cysteine residues. The functionalizing reagent is covalently linked to a poly(alkylene glycol) molecule, such as a polyethylene glycol (PEG) molecule, or a glycan group so that the reaction between the vinyl group and the thiol group in the polypeptide covalently links the polypeptide to the poly(alkylene glycol) molecule and/or the glycan group.Type: ApplicationFiled: June 26, 2014Publication date: December 11, 2014Inventors: Andrew Graham WATTS, Terrence Kantner, Amanda Barbara MacKenzie
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Publication number: 20140357680Abstract: The invention relates to the compositions of formula I or its pharmaceutical acceptable polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprises a salt of metformin and the methods for treating or preventing metabolic syndrome, prediabetes and diabetes may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of diabetes mellitus, obesity, lipid disorders, hypertriglyceridemia, hyperglycemia, hyperinsulinemia and insulin resistance.Type: ApplicationFiled: April 4, 2014Publication date: December 4, 2014Inventor: Mahesh Kandula
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Patent number: 8889720Abstract: One aspect of the present invention relates to substituted pyridines and pharmaceutically acceptable salts thereof that are active against a range of mammalian maladies. Another aspect of the invention relates to a pharmaceutical composition, comprising a compound of the present invention or a pharmaceutically acceptable salt thereof; and a pharmaceutically acceptable excipient. The present invention also relates to methods of treating a range of mammalian maladies or conditions, including but not limited to hyperlipidemia, hypercholesterolemia, atherosclerosis, coronary artery disease, congestive heart failure, cardiovascular disease, hypertension, coronary heart disease, angina, pellagra, Hartnup's syndrome, carcinoid syndrome, arterial occlusive disease, obesity, hypothyroidism, vasoconstriction, osteoarthritis, rheumatoid arthritis, diabetes, Alzheimer's disease, lipodystrophy, or dyslipidemia, raising serum high-density lipoprotein (HDL) levels, and lowering serum low-density lipoprotein (LDL) levels.Type: GrantFiled: December 14, 2012Date of Patent: November 18, 2014Assignee: Trustees of Tufts CollegeInventors: William W. Bachovchin, Hung-sen Lai
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Publication number: 20140315950Abstract: The present invention relates to Formula (I), wherein—if X=NH, each of R1, R2, R3, R4 represents a hydrogen atom; if X=N, the core is aromatic, and R2, R3 and R4 represent hydrogen atoms, and R1=H, halogen, aryl, heteroaryl, alkenyl or acetylenyl; or R1, R2, R3, R4 are defined such that R1 or R2 or R3 or R4 represents a methyl group, and the three other radicals represent a hydrogen atom.Type: ApplicationFiled: December 10, 2012Publication date: October 23, 2014Inventors: Daniel Redoules, Sylvie Daunes-Marion, Stephane Poigny, Marie-Florence Galliano
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Publication number: 20140242606Abstract: The present invention relates to a probe for iFRET and use thereof. Specifically, the present invention relates to a novel probe for iFRET, a method for preparing the probe for iFRET, a method for searching a target protein-specific binding site or a molecule having the binding site using the probe for iFRET, and a method for imaging the target protein using the probe for iFRET. The probe for iFRET according to the present invention utilizes an amino acid in a protein as a fluorescent donor, unlike the conventional FRET method. Therefore, only one fluorescent material is used, and its emission wavelength is distinct from the intrinsic fluorescence of the protein. Thus, high specificity and sensitivity are ensured, and the quantity, activity and mechanism of various proteins can be analyzed in an easy and accurate manner.Type: ApplicationFiled: June 25, 2012Publication date: August 28, 2014Applicant: KOREA RESEARCH INSTITUTE OF BIOSCIENCE AND BIOTECHNOLOGYInventors: Sang Jeon Chung, Ju Hwan Kim, Elena Ruchkina, Hyo Jin Kang
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Patent number: 8772230Abstract: This invention relates to the use of niacin and/or trigonelline compounds to increase muscle weight during periods of activity or to inhibit muscle loss during periods of inactivity.Type: GrantFiled: June 10, 2010Date of Patent: July 8, 2014Assignee: DSM IP Assets B.V.Inventors: Angelika Friedel, Karin Kuratli, Christof Wehrli, Karin Wertz, Swen Wolfram, Ying Wang-Schmidt
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Patent number: 8722893Abstract: A process for manufacturing 5-chloromethyl-2,3-pyridine dicarboxylic acid anhydrides (I) wherein Z is hydrogen or halogen; Z1 is hydrogen, halogen, cyano or nitro; comprising the steps of (i) reacting a compound of formula (II), wherein the symbols have the meaning given in formula (I), with a chlorinating agent, optionally in the presence of a radical initiator in a solvent selected from halogenated hydrocarbons, and (ii) crystallizing the compound (I) formed in step (i) from a solvent selected from chlorobenzene, 1,2-dichlorobenzene, 1,3-dichlorobenzene, 1,4-dichlorobenzene, dichloroethane, trichloromethane, dichloromethane, toluene, xylenes, ethyl acetate, methyl tert.-butyl ether, and mixtures thereof. Compounds (I) are useful intermediates in the synthesis of herbicidal imidazolinones.Type: GrantFiled: November 3, 2009Date of Patent: May 13, 2014Assignee: BASF SEInventors: Frederik Menges, Joachim Gebhardt, Michael Rack, Michael Keil, Rodney F. Klima, David Cortes, Robert Leicht, Helmut Zech, Jochen Schroeder
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Patent number: 8653277Abstract: It is to provide a fungicidal composition having stable and high fungicidal effects against cultivated crops infected with plant diseases resulting from plant diseases.Type: GrantFiled: May 29, 2009Date of Patent: February 18, 2014Assignee: Ishihara Sangyo Kaisha, Ltd.Inventors: Hisaya Nishide, Shigeyuki Nishimura, Shigeru Mitani, Koji Minamida, Fumio Kanamori, Munekazu Ogawa, Shigehisa Kanbayashi, Toyoshi Tanimura, Koji Higuchi, Hidemasa Kominami, Tomohiro Okamoto, Akihiro Nishimura
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Publication number: 20130303548Abstract: Niacin prevents and/or reverses the development of experimental hepatic steatosis, deposition of triglycerides in liver and serum of individuals, deposition of total cholesterol in liver and serum in individuals, and inhibit liver lipid peroxidation and oxidative stress in individuals at risk of developing fatty liver disease or NAFLD. In cultured human hepatocytes, niacin inhibits alcohol-induced fat accumulation.Type: ApplicationFiled: November 22, 2011Publication date: November 14, 2013Applicant: The Regents of the University of CaliforniaInventors: Moti L. Kashyap, Shobha V. Kamanna, Vaijinath S. Kamanna
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Patent number: 8563734Abstract: 2-[(1-cyanopropyl)carbamoyl]-5-chloromethyl nicotinic acids of formula (I) where Z is hydrogen or halogen; Z1 is hydrogen, halogen, cyano or nitro; R1 is C1-C4 alkyl; R2 is C1-C4 alkyl, C3-C6 cycloalkyl or R1 and R2, when taken together with the atom to which they are attached, represent a C3-C6 cycloalkyl group optionally substituted with methyl, and R3 is hydrogen or a cation preferably selected from the group consisting of alkali metals, alkaline earth metals, manganese, copper, iron, zinc, cobalt, lead, silver, nickel, ammonium and organic ammonium; are useful intermediates for the synthesis of herbicidal imidazolinones.Type: GrantFiled: November 3, 2009Date of Patent: October 22, 2013Assignee: BASF SEInventors: Frederik Menges, Joachim Gebhardt, Michael Rack, Michael Keil, Rodney F. Klima, David Cortes, Robert Leicht, Helmut Zech, Jochen Schröder
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Patent number: 8552201Abstract: The present invention relates to derivatives of 5,6-bisaryl-2-pyridine-carboxamide, their preparation and their application in therapeutics as antagonists of urotensin II receptors.Type: GrantFiled: December 29, 2011Date of Patent: October 8, 2013Assignee: SanofiInventors: Jean-Michel Altenburger, Valérie Fossey, Philip Janiak, Gilbert Lassalle, Frédéric Petit, Jean Claude Vernieres
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Publication number: 20130059384Abstract: Compositions and methods comprising bioenergetic agents for restoring the quality of aged oocytes, enhancing oogonial stem cells or improving derivatives thereof (e.g., cytoplasm or isolated mitochondria) for use in fertility-enhancing procedures, are described.Type: ApplicationFiled: April 13, 2012Publication date: March 7, 2013Applicants: PRESIDENT AND FELLOWS OF HARVARD COLLEGE, THE GENERAL HOSPITAL CORPORATIONInventors: JONATHAN L. TILLY, DAVID A. SINCLAIR
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Patent number: 8389552Abstract: The present invention provides Formula (1A) compounds that act as glucokinase activators; pharmaceutical compositions thereof; and methods of treating diseases, disorders, or conditions mediated by glucokinase. X, Y, Z, R1, R2, R3, and R4 areas described herein.Type: GrantFiled: April 23, 2012Date of Patent: March 5, 2013Assignee: Pfizer Inc.Inventors: Jeffrey Allen Pfefferkorn, Meihua Mike Tu
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Patent number: 8377971Abstract: One aspect of the present invention relates to substituted pyridines and pharmaceutically acceptable salts thereof that are active against a range of mammalian maladies. Another aspect of the invention relates to a pharmaceutical composition, comprising a compound of the present invention or a pharmaceutically acceptable salt thereof; and a pharmaceutically acceptable excipient. The present invention also relates to methods of treating a range of mammalian maladies or conditions, including but not limited to hyperlipidemia, hypercholesterolemia, atherosclerosis, coronary artery disease, congestive heart failure, cardiovascular disease, hypertension, coronary heart disease, angina, pellagra, Hartnup's syndrome, carcinoid syndrome, arterial occlusive disease, obesity, hypothyroidism, vasoconstriction, osteoarthritis, rheumatoid arthritis, diabetes, Alzheimer's disease, lipodystrophy, or dyslipidemia, raising serum high-density lipoprotein (HDL) levels, and lowering serum low-density lipoprotein (LDL) levels.Type: GrantFiled: August 1, 2007Date of Patent: February 19, 2013Assignee: Trustees of Tufts CollegeInventors: William W. Bachovchin, Hung-Sen Lai
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Patent number: 8318946Abstract: 2-Substituted-5-(1-alkylthio)alkylpyridines are produced efficiently and in high yield.Type: GrantFiled: March 12, 2010Date of Patent: November 27, 2012Assignee: Dow Agrosciences, LLCInventors: Kevin G. Meyer, Kim E. Arndt
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Publication number: 20120291737Abstract: An ashless additive for lubricating oil compositions, lubricating oil compositions and methods for lubricating that are effective to improve the total base number (TBN) of a lubricant composition.Type: ApplicationFiled: March 2, 2012Publication date: November 22, 2012Applicant: AFTON CHEMICAL CORPORATIONInventors: Naresh MATHUR, Jason A. LAGONA, John T. LOPER
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Publication number: 20120289632Abstract: Described herein are novel metal salts capable as nucleating agents for polyolefins. The present invention relates to such salts synthesized by reacting potassium hydroxide with carboxylic acids and further, to the achievement of high crystallization temperatures in polypropylene compositions upon dispersal therein of formulations containing one or more of the said metal salts.Type: ApplicationFiled: January 14, 2011Publication date: November 15, 2012Applicant: RELIANCE INDUSTRIES LIMITEDInventors: Gandham Satya Srinivasa Rao, S. Muthukumaru Pillai, Virendra Kumar Gupta
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Publication number: 20120277180Abstract: Provided herein are methods and systems for identifying one or more cofactors such as vitamins for individuals based on the genetic makeup of the individual by detecting the presence or absence of at least one genetic variant, determining a predisposition to cofactor remediable condition, generating a personalized nutritional advice plan based on the genetic variant. Also provided herein are formulations of cofactors determined by the genetic make-up of the individual and methods of determining and producing these formulations.Type: ApplicationFiled: September 30, 2010Publication date: November 1, 2012Applicants: VITAPATH GENETICS, INC, THE REGENTS OF THE UNIVERSITY OF CALIFORNIAInventors: Nicholas Marini, Jasper Rine, Dennis Austin Gilbert, Bruce Cohen
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Patent number: 8258308Abstract: The present disclosure relates to compounds of formula (I): or a pharmaceutically acceptable salt or N-oxide thereof. The present disclosure also relates to pharmaceutical compositions comprising the compounds of formula (I), and to their methods of use in therapy.Type: GrantFiled: December 21, 2007Date of Patent: September 4, 2012Assignee: Laboratorios Almirall, S.A.Inventors: Julio Cesar Castro Palomino Laria, Montserrat Erra Sola, Maria Estrella Lozoya Toribio, Eloisa Navarro Romero
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Publication number: 20120190617Abstract: This invention relates to the use of niacin and/or trigonelline compounds to increase muscle weight during periods of activity or to inhibit muscle loss during periods of inactivity.Type: ApplicationFiled: June 10, 2010Publication date: July 26, 2012Inventors: Angelika Friedel, Karin Kuratli, Christof Wehrli, Karin Wertz, Swen Wolfram, Ying Wang-Schmidt
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Patent number: 8227636Abstract: The present invention is directed to prodrugs of hydroxamic acid based histone deacetylase (HDAC) inhibitors, e.g., suberoylanilide hydroxamic acid (SAHA). The prodrugs are acylated derivatives having increased aqueous solubility and cellular permeability as compared with the free hydroxamic acid, and are useful for inhibiting HDACs, and for selectively inducing terminal differentiation, cell growth arrest and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the prodrugs of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The prodrugs of the invention are also useful in the prevention and treatment of thioredoxin (TRX)-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.Type: GrantFiled: April 5, 2005Date of Patent: July 24, 2012Assignee: Merck HDAC Research, LLCInventors: Thomas A. Miller, David J. Witter, Sandro Belvedere
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Publication number: 20120157685Abstract: Intermediate release nicotinic acid formulations are described herein exhibiting an in vivo stair-stepped or sigmoidally-shaped absorption curves when the plasma nicotinic acid or nicotinuric acid curves are deconvoluted using the Wagner-Nelson method, which are suitable for oral administration once-a-day preferably during the evening or at night for treating hyperlipidemia without causing drug-induced hepatotoxicity to such a level that requires the therapy to be discontinued.Type: ApplicationFiled: February 15, 2012Publication date: June 21, 2012Inventors: Eugenio A. Cefali, David J. Bova
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Patent number: 8143411Abstract: The present application relates to novel substituted 6-phenylnicotinic acid derivatives, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, preferably for the treatment and/or prophylaxis of cardiovascular disorders, in particular dyslipidaemias, arteriosclerosis and heart failure.Type: GrantFiled: August 26, 2008Date of Patent: March 27, 2012Assignee: Bayer Animal Health GmbHInventors: Lars Bärfacker, Barbara Albrecht-Küpper, Peter Kolkhof, Yolanda Cancho Grande, Adam Nitsche, Heinrich Meier, Carsten Schmeck, Jens Schamberger, Klemens Lustig
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Publication number: 20120022117Abstract: A salt or cocrystal of 3-(3-dimethylamino-1-ethyl-2-methyl-propyl)-phenol (component a) and at least one acid component (b1) or at least one acid component (b2), wherein the salt or cocrystal of component (a) and component (b2) is present in crystalline and/or amorphous form, a pharmaceutical composition comprising said salt or cocrystal, and a method of treating pain in a subject in need thereof by administering an effective amount of said salt or cocrystal.Type: ApplicationFiled: July 22, 2011Publication date: January 26, 2012Applicant: Gruenenthal GmbHInventors: Michael GRUSS, Magda KRASZEWSKI
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Publication number: 20110294858Abstract: In one aspect, the invention relates to substituted 6-methylnicotinamide analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.Type: ApplicationFiled: May 24, 2011Publication date: December 1, 2011Inventors: P. Jeffrey Conn, Craig W. Lindsley, Shaun R. Stauffer, Ya Zhou, Jason Manka, Gregor McDonald, José Manuel Bartolome-Nebreda
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Publication number: 20110269709Abstract: The invention provides the compounds of formula (I) or pharmaceutically acceptable salts thereof. The invention also provides pharmaceutical compositions comprising one or more compounds of formula I or intermediates thereof and one more of pharmaceutically acceptable carriers, vehicles or diluents. The invention further provides methods of preparation and methods of use of prodrugs including NO-releasing prodrugs, double prodrugs and mutual prodrugs comprising the compounds of formula I.Type: ApplicationFiled: December 23, 2010Publication date: November 3, 2011Inventor: Apparao Satyam
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Publication number: 20110263526Abstract: The present invention relates to nitric oxide releasing prodrugs of known drugs or therapeutic agents which are represented herein as compounds of formula (I) wherein the drugs or therapeutic agents contain one or more functional groups independently selected from a carboxylic acid, an amino, a hydroxyl and a sulfhydryl group. The invention also relates to processes for the preparation of the nitric oxide releasing prodrugs (the compounds of formula (I)), to pharmaceutical compositions containing them and to methods of using the prodrugs.Type: ApplicationFiled: April 22, 2011Publication date: October 27, 2011Applicant: PIRAMAL LIFE SCIENCES LIMITEDInventor: Apparao SATYAM
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Publication number: 20110224439Abstract: A process for manufacturing 5-chloromethyl-2,3-pyridine dicarboxylic acid anhydrides (I) wherein Z is hydrogen or halogen; Z1 is hydrogen, halogen, cyano or nitro; comprising the steps of (i) reacting a compound of formula (II), wherein the symbols have the meaning given in formula (I), with a chlorinating agent, optionally in the presence of a radical initiator in a solvent selected from halogenated hydrocarbons, and (ii) crystallizing the compound (I) formed in step (i) from a solvent selected from chlorobenzene, 1,2-dichlorobenzene, 1,3-dichlorobenzene, 1,4-dichlorobenzene, dichloroethane, trichloromethane, dichloromethane, toluene, xylenes, ethyl acetate, methyl tert.-butyl ether, and mixtures thereof. Compounds (I) are useful intermediates in the synthesis of herbicidal imidazolinones.Type: ApplicationFiled: November 13, 2008Publication date: September 15, 2011Inventors: Frederik Menges, Joachim Gebhardt, Michael Rach, Michael Keil, Rodney F. Klima, David Cortes, Robert Leicht, Helmut Zech, Jochen Schroeder
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Patent number: 8017786Abstract: The present invention relates to a compound of the formula (I), wherein R1, R2 and R3 are each independently selected from H, OH, F, Cl, Br, methoxy and ethoxy; or alternatively, R1 and R2 together form —OCH2O—, R3 is selected from H, OH, methoxy, ethoxy and halogens; R4 is OH or acyloxy; R5 is cycloalkoxyl, amino and substituted amino, and when R5 is selected from amino, at least one of R1, R2 and R3 is not H. The present invention further relates to a process for synthesizing a compound of the formula (I), and use of the compound of the formula (I) in the manufacture of a medicament for the prevention or treatment of cardiovascular or cerebrovascular diseases.Type: GrantFiled: May 14, 2007Date of Patent: September 13, 2011Assignee: Northwest UniversityInventors: Xiaohui Zheng, Qunzheng Zhang, Shixiang Wang, Xinfeng Zhao
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Publication number: 20110218340Abstract: 2-[(1-cyanopropyl)carbamoyl]-5-chloromethyl nicotinic acids of formula (I) where Z is hydrogen or halogen; Z1 is hydrogen, halogen, cyano or nitro; R1 is C1-C4 alkyl; R2 is C1-C4 alkyl, C3-C6 cycloalkyl or R1 and R2, when taken together with the atom to which they are attached, represent a C3-C6 cycloalkyl group optionally substituted with methyl, and R3 is hydrogen or a cation preferably selected from the group consisting of alkali metals, alkaline earth metals, manganese, copper, iron, zinc, cobalt, lead, silver, nickel, ammonium and organic ammonium; are useful intermediates for the synthesis of herbicidal imidazolinones.Type: ApplicationFiled: November 3, 2009Publication date: September 8, 2011Applicant: BASF SEInventors: Frederik Menges, Joachim Gebhardt, Michael Rack, Michael Keil, Rodney F. Klima, David Cortes, Robert Leicht, Helmut Zech, Jochen Schröder
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Publication number: 20110178396Abstract: A compound comprising a pyridine carboxamide structure, for use in imaging or treating melanoma, is described. An aromatic ring in the structure is substituted with a radiohalogen atom and the substitution on the amide nitrogen atom is such that the compound binds to melanin.Type: ApplicationFiled: April 22, 2009Publication date: July 21, 2011Applicant: CRC FOR BIOMEDICAL IMAGING DEVELOPMENT LTD.Inventors: Andrew Katsifis, Ivan Greguric
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Publication number: 20110165186Abstract: The present invention relates to novel pyridine alkaloid compounds of formula (I): or a pharmaceutically acceptable derivative thereof as described in the specification, the process for the preparation of the same, and the composition comprising the same. The uses of a pyridine compound for increasing the activity of PPAR?, for the prevention and/or treatment of a disease or disorder related to insulin resistance, and for the prevention and/or treatment of metabolic syndrome or its complication are also provided. The invention also provides extracts of red yeast-fermented products and their uses for prevention and/or treatment of a disease or disorder related to insulin resistance, such as metabolic syndrome.Type: ApplicationFiled: December 30, 2010Publication date: July 7, 2011Inventors: Ming-Der WU, Ming-Jen Cheng, Shie-Jea Lin, Chi-Hua Chen, Yen-Lin Chen, Hui-Ping Chen, Kai-Ping Chen, Ping-Shin Yang, Shiow-Wen Chen, Gwo-Fang Yuan
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Publication number: 20110158947Abstract: We disclose agents useful in the treatment of diseases or conditions that would benefit from improved muscle function and including pharmaceutical compositions and diagnostic tests for determining the predisposition of a subject, in particular a male subject, to cardiovascular disease.Type: ApplicationFiled: July 9, 2009Publication date: June 30, 2011Inventor: Aleksandar Jovanovic
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Publication number: 20110110914Abstract: Methods and formulations for treating oncological disorders in humans using epimetabolic shifters, multidimensional intracellular molecules or environmental influencers are described.Type: ApplicationFiled: May 11, 2010Publication date: May 12, 2011Inventors: Niven Rajin Narain, John Patrick McCook, Rangaprasad Sarangarajan
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Publication number: 20100292482Abstract: The present invention relates to a Compound of the formula (I), wherein X represents CN, COOR, wherein R represents hydrogen or a carboxyl protecting group, CONR?2, wherein R? represents hydrogen or a carboxyl protecting group, or nitro; R1, R2, R3, R4, R5 independently of each other represent hydrogen, C1-C6 alkyl, halogen, trifluoromethyl, cyano, nitro, substituted aryl or substituted heteroaryl group; Y represents hydrogen, C1-C6 alkyl, C3-C7 cycloalkyl, C7-C13 alkaryl, trifluoromethyl, cyano, nitro, substituted aryl or substituted heteroaryl group; and wherein the stereochemically unspecified double bonds in the above formula (I) represent either the E,E; E,Z; Z,E or Z,Z configuration.Type: ApplicationFiled: October 24, 2008Publication date: November 18, 2010Inventors: David Alexander Learmonth, Laszlo Erno Kiss
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Patent number: 7816558Abstract: Provided is a triarylcarboxylic acid derivative, or an isomer, a prodrug, a hydrate, a solvate, a polymorph, or a pharmaceutically acceptable salt thereof, represented by the following general formula (I): wherein A is an optionally substituted aryl or heteroaryl, and B is an optionally substituted monocyclic heteroaryl; and a pharmaceutical composition comprising the same and a pharmaceutically acceptable carrier. The triarylcarboxylic acid derivative (I) exhibits potent xanthine oxidase inhibiting action and is therefore useful as a therapeutic agent for preventing or treating hyperuricemia, gout, inflammatory bowel disease, diabetic nephropathy and diabetic retinopathy.Type: GrantFiled: October 6, 2006Date of Patent: October 19, 2010Assignee: Astellas Pharma Inc.Inventors: Junji Sato, Kazuyuki Hattori, Hirokazu Kubota, Ryosuke Munakata, Toru Asano, Junko Maeda, Masakatsu Kawakami, Akio Kamikawa
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Publication number: 20100240899Abstract: Intermediate release nicotinic acid formulations exhibiting an in vivo stair-stepped or sigmoidally-shaped absorption curves when the plasma nicotinic acid or nicotinuric acid curves are deconvoluted using the Wagner-Nelson method, which are suitable for oral administration once-a-day preferably during the evening or at night for treating hyperlipidemia without causing drug-induced hepatotoxicity to such a level that requires the therapy to be discontinued, are disclosed. The stair-stepped or sigmoidal-shaped absorption profiles for nicotinic acid or nicotinuric acid absorbed from the nicotinic acid formulations of the instant invention are characterized by three phases and by the fact that significant quantities of nicotinic acid are absorbed during the first two phases. The first phase generally ends at about 2.3 hours following ingestion and the second phase generally ends at about 7.3 hours after consumption.Type: ApplicationFiled: October 19, 2009Publication date: September 23, 2010Inventors: Eugenio A. Cefali, David J. Bova
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Publication number: 20100168435Abstract: 2-Substituted-5-(1-alkylthio)alkylpyridines are produced efficiently and in high yield.Type: ApplicationFiled: March 12, 2010Publication date: July 1, 2010Applicant: DOW AGROSCIENCES LLCInventors: Kevin G. Meyer, Kim E. Arndt
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Patent number: 7745495Abstract: The invention relates to compounds of formula (I) wherein A1 is C(R1R2)p; A2 is C(R6R7)q; p is 1 or 2; q is 1 or 2; each of R1, R2, R3, R4, R5, R6, R7 and R8 which may be the same or different, represents hydrogen, methyl or ethyl and R9 is C1-C4alkyl; R10 is hydrogen, halogen, C1-C3alkyl or C1-C3-haloalkyl, and agronomically acceptable salts/isomers/enantiomers/tautomers/N-oxides of those compounds.Type: GrantFiled: December 20, 2005Date of Patent: June 29, 2010Assignee: Syngenta Crop Protection, Inc.Inventors: Sebastian Volker Wendeborn, Renaud Beaudegnies, Andrew Edmunds, Christoph Luthy, Jurgen Schaetzer
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Publication number: 20100069446Abstract: The present invention is directed to a derivative comprised of an L-Threonine bonded to a medicament or drug having a hydroxy, amino, carboxy or acylating derivative thereon. The derivative has the same utility as the drug from which it is made, but it has enhanced therapeutic properties. In fact, the derivatives of the present invention enhance at least one or more therapeutic qualities, as defined herein. The present invention is also directed to pharmaceutical compositions containing same.Type: ApplicationFiled: September 10, 2009Publication date: March 18, 2010Applicant: SIGNATURE R&D HOLDINGSInventor: V. Ravi Chandran
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Patent number: 7678792Abstract: The invention provides compounds and pharmaceutical compositions thereof, which are useful as protein kinase inhibitors, as well as methods for using such compounds to treat, ameliorate or prevent a condition associated with abnormal or deregulated kinase activity. In some embodiments, the invention provides methods for using such compounds to treat, ameliorate or prevent diseases or disorders that involve abnormal activation of c-kit, PDGFR?, PDGFR?, CSF1R, Abl, BCR-Abl, CSK, JNK1, JNK2, p38, p70S6K, TGF?, SRC, EGFR, trkB, FGFR3, FLT3, Fes, Lck, Syk, RAF, MKK4, MKK6, SAPK2?, BRK, KDR, c-raf or b-raf kinase, or mutant forms thereof.Type: GrantFiled: October 16, 2007Date of Patent: March 16, 2010Assignee: IRM LLCInventors: Donatella Chianelli, Christopher Cow, Yun He, Songchun Jiang, Xiaolin Li, Xiaodong Liu, Zuosheng Liu, Jon Loren, Valentina Molteni, Juliet Nabakka, Pingda Ren, Taebo Sim, Xiaodong Wang, Shuli You
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Publication number: 20090318481Abstract: This application relates to a substituted hydroxyphenyl ketone compound of formula I, or a pharmaceutically acceptable salt thereof, a pharmaceutical composition thereof and its use in treating migraine. This application also relates to processes for preparing a compound of formula I, and intermediate compounds useful therein.Type: ApplicationFiled: August 28, 2009Publication date: December 24, 2009Inventors: Thomas Daniel AICHER, Guillermo S. CORTEZ, Todd Michael GROENDYKE, Albert KHILEVICH, James Allen KNOBELSDORF, Fredrik Pehr MARMSATER, Jeffrey Michael SCHKERYANTZ, Tony Pisal TANG
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Patent number: 7615641Abstract: This application pertains to compounds comprising unbranched long chain aliphatic alcohols linked to a heterocyclic carboxylic acid moiety by means of an ester or ether linkage. The aliphatic alcohols may include aliphatic alcohols present in polycosanol, such as octacosanol. The heterocyclic carboxylic acid moieties include a 5-membered ring, a 6-membered ring, or a bicyclic ring. In one embodiment, the compounds of the invention include 1-octacosanyl nicotinate and salts thereof. The invention includes prodrugs, pharmaceutically acceptable salts, and pharmaceutical compositions of the compounds, and methods of making and using the compounds.Type: GrantFiled: July 20, 2004Date of Patent: November 10, 2009Assignee: Sino Pharmaceuticals CorporationInventor: Radka Milanova
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Publication number: 20090269855Abstract: Methods and compounds are provided to improve the desorption and ionization of analyte for mass spectrometry analysis. More specifically, it is for laser desorption/ionization mass spectrometry. The method uses photon energy absorbing molecules that can bind with analyte either temporarily or permanently to improve the desorption and ionization of analyte. The photon energy absorbing molecules can be positively charged or negatively charged.Type: ApplicationFiled: June 23, 2009Publication date: October 29, 2009Inventors: Tiaxin Wang, Qun Liu, Sha Zhou Zou
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Publication number: 20090197767Abstract: The invention relates to compounds of formula (I) wherein A1 is C(R1R2)p; A2 is C(R6R7)q; p is 1 or 2; q is 1 or 2; each of R1, R2, R3, R4, R5, R6, R7 and R8 which may be the same or different, represents hydrogen, methyl or ethyl and R9 is C1-C4alkyl; R10 is hydrogen, halogen, C1-C3alkyl or C1-C3-haloalkyl, and agronomically acceptable salts/isomers/enantiomers/tautomers/N-oxides of those compounds.Type: ApplicationFiled: December 20, 2005Publication date: August 6, 2009Applicant: SYNGENTA CROP PROTECTION, INC.Inventors: Sebastian Volker Wendeborn, Renaud Beaudegnies, Andrew Edmunds, Christoph Luthy, Jürgen Schaetzer
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Patent number: RE41008Abstract: The invention relates to a process for the preparation of 5-arylnicotinaldehydes by reduction of the corresponding 5-arylnicotinic acids by catalytic hydrogenation in the presence of carboxylic anhydrides in which the catalyst used is a palladium/ligand complex, characterized in that the molar ratio between palladium and ligand is from 1:5 to 1:15 in the case of monodentate ligands and from 1:2.5 to 1:7.5 in the case of bidentate ligands.Type: GrantFiled: January 5, 2001Date of Patent: November 24, 2009Assignee: Merck Patent GmbHInventors: Andreas Bathe, Heinz Bokel, Ralf Knieriemen, Christoph Muermann, Thomas Keil