C=o Bonded Directly To The Six-membered Hetero Ring Patents (Class 514/354)
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Patent number: 8481557Abstract: Methods of treating cancer by administering a DNA damaging agent and a CHK1 Inhibitor on a dosing regimen are provided.Type: GrantFiled: April 9, 2010Date of Patent: July 9, 2013Assignee: Array Biopharma Inc.Inventors: Michael J. Humphries, Shannon L. Winski
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Publication number: 20130171268Abstract: The present invention relates to compositions and methods for prophylactic and/or therapeutic treatment of conditions related to mitochondrial function. In various aspects, the present invention comprises administering one or more compounds selected from the group consisting of epicatechin, an epicatechin derivative, catechin, a catechin derivative, nicorandil, and a nicorandil derivative in an amount effective to ameliorate mitochondrial toxicity caused by administration of a chemical, food, or drug.Type: ApplicationFiled: June 5, 2012Publication date: July 4, 2013Inventors: Francisco Villarreal, Alan Maisel, George Schreiner, Guillermo M. Ceballos Reyes, Pam Taub
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Publication number: 20130165443Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is optionally substituted phenyl or optionally substituted pyridinyl, and R2, R3, R4, R5, R6, R7, R8 and R9 are as defined herein. Also disclosed are methods of using the compounds for treating diseases associated with P2X3 and/or a P2X2/3 receptor antagonists and methods of making the compounds.Type: ApplicationFiled: August 23, 2012Publication date: June 27, 2013Inventors: Chris Allen Broka, Ronald Charles Hawley
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Publication number: 20130164221Abstract: Provided herein are methods for detecting, quantifying, differentiating, diagnosing and imaging pathogenic bacteria or condition associated therewith using substrates for bacterial enzymes. Fluorescent, luminescent or colorimetric signals emitted by substrates or enzyme products in the presence of the bacteria are compared to controls to detect and locate the pathogenic bacteria. Provided is a method for screening therapeutic agents to treat the pathophysiological conditions by measuring a signal emitted from the substrates or products in the presence and absence of the potential therapeutic agent and a diagnostic method for detecting a mycobacterial infection in a subject by contacting biological samples with a substrate and imaging for signals emitted from a mycobacterial beta-lactamase product. Also provided are fluorogenic substrates or substrates comprising a colored dye or a chemical reagent effective to induce a color or pH change.Type: ApplicationFiled: December 4, 2012Publication date: June 27, 2013Inventors: Jeffrey D. Cirillo, James C. Sacchettini, Jianghong Rao, Hexin Xie
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Patent number: 8466172Abstract: The present invention relates to methods of stabilizing the alpha subunit of hypoxia inducible factor (HIF). The invention further relates to methods of preventing, pretreating, or treating conditions associated with HIF, including ischemic and hypoxic conditions. Compounds for use in these methods are also provided.Type: GrantFiled: December 2, 2010Date of Patent: June 18, 2013Assignee: FibroGen, Inc.Inventors: Volkmar Guenzler-Pukall, Thomas B. Neff, Qingjian Wang, Michael P. Arend, Lee A. Flippin, Alex Melekhov
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Patent number: 8466179Abstract: Provided herein are ready-to-use premixed pharmaceutical compositions of nicardipine or a pharmaceutically acceptable salt and methods for use in treating cardiovascular and cerebrovascular conditions.Type: GrantFiled: December 23, 2010Date of Patent: June 18, 2013Assignee: EKR Therapeutics, Inc.Inventors: Michelle Renee Duncan, Supriya Gupta, David Hartley Haas, Norma V. Stephens, Camellia Zamiri
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Patent number: 8466178Abstract: Provided herein are ready-to-use premixed pharmaceutical compositions of nicardipine or a pharmaceutically acceptable salt and methods for use in treating cardiovascular and cerebrovascular conditions.Type: GrantFiled: December 22, 2009Date of Patent: June 18, 2013Assignee: EKR Therapeutics, Inc.Inventors: Michelle Renee Duncan, Supriya Gupta, David Hartley Haas, Norma V. Stephens, Camellia Zamiri
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Publication number: 20130150415Abstract: The present invention relates to the use of isotopically labeled derivatives of isoniazid, ethionamide and related compounds as effective therapy for the treatment of mycobacterial diseases, including Mycobacterium tuberculosis.Type: ApplicationFiled: February 6, 2013Publication date: June 13, 2013Applicants: The John Hopkins University, STC.UNMInventors: Graham TIMMINS, Sharon Masters, Vojo P. Deretic, William Bishai
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Publication number: 20130150358Abstract: This invention relates to agents that are inhibitors or activators of variant forms of endogenous proteins and novel methods of identifying such variants. Of particular interest are inhibitors and activators of endogenous protein variants, encoded by genes which have mutated, which variants often arise or are at least first identified as having arisen following exposure to a chemical agent which is known to be an inhibitor or activator of the corresponding unmutated endogenous protein.Type: ApplicationFiled: February 4, 2013Publication date: June 13, 2013Applicant: HMI MEDICAL INNOVATIONS, LLC.Inventor: HMI MEDICAL INNOVATIONS, LLC.
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Publication number: 20130143933Abstract: The present document describes a cancer mutation-selective chemosensitizer that comprise compounds for restoring association between mutated keap1 protein and Nrf2 protein, and inhibition of Nrf2 functions. The present document also describes composition of matter containing the compounds, as well as methods of medical treatment for treating diseases such as cancer with the compounds.Type: ApplicationFiled: November 9, 2012Publication date: June 6, 2013Applicant: TRT Pharma Inc.Inventor: TRT Pharma Inc.
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Patent number: 8455524Abstract: Provided herein are ready-to-use premixed pharmaceutical compositions of nicardipine or a pharmaceutically acceptable salt and methods for use in treating cardiovascular and cerebrovascular conditions.Type: GrantFiled: December 17, 2010Date of Patent: June 4, 2013Assignee: EKR Therapeutics, Inc.Inventors: Michelle Renee Duncan, Supriya Gupta, David Hartley Haas, Norma V. Stephens, Camellia Zamiri
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Publication number: 20130137704Abstract: The present invention relates to novel compounds of Formula (I), wherein X1, X2, X3, X4, Am and Bn are defined as in Formula (I); invention compounds are modulators of metabotropic glutamate receptors—subtype 4 (“mGluR4”) which are useful for the treatment or prevention of central nervous system disorders as well as other disorders modulated by mGluR4 receptors. The invention is also directed to pharmaceutical compositions and the use of such compounds in the manufacture of medicaments, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR4 is involved.Type: ApplicationFiled: January 22, 2013Publication date: May 30, 2013Applicant: Addex Pharma, SAInventor: Addex Pharma, SA
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Publication number: 20130131095Abstract: The invention relates to the use in a composition for caring for human hair or eyelashes of an effective amount of a pyridinedicarboxylic acid derivative of general formula (I) or of one of its salts, in which R1 and R2 represent, independently of one another, OH, OR?, —NH2, —NHR? or —NR?R?, and R? and R? represent, independently of one another, a saturated or unsaturated and linear or branched C1-C18 alkyl radical or an aryl radical, this alkyl or aryl radical optionally being substituted by at least one OH, alkoxy, acyloxy, amino or alkylamino group, or R? and R? together represent a heterocycle, the composition being intended to induce and/or stimulate the growth of human keratinous fibers, such as the hair and eyelashes, and/or slow down their loss; the invention also relates to a cosmetic treatment intended to stimulate the growth of human keratinous fibers, such as the hair and eyelashes, and/or slow down their loss.Type: ApplicationFiled: October 29, 2012Publication date: May 23, 2013Applicant: Societe L'Oreal S.A.Inventor: Societe L'Oreal S.A.
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Publication number: 20130131092Abstract: The present invention relates to novel compounds of Formula (I), wherein X1, X2, X3, X4, Am and Bn are defined as in Formula (I); invention compounds are modulators of metabotropic glutamate receptors—subtype 4 (“mGluR4”) which are useful for the treatment or prevention of central nervous system disorders as well as other disorders modulated by mGluR4 receptors. The invention is also directed to pharmaceutical compositions and the use of such compounds in the manufacture of medicaments, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR4 is involved.Type: ApplicationFiled: January 22, 2013Publication date: May 23, 2013Applicant: Addex Pharma, SAInventor: Addex Pharma, SA
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Publication number: 20130123345Abstract: Described herein is a method of treating a viral infection such as an influenza infection, in a subject comprising administering an effective amount of a pharmaceutical composition to disrupt a adenosine receptor pathway, such as the Aradenosine receptor pathway, in a subject. The adenosine receptor pathway includes the steps of 1) producing the adenosine precursor adenosine triphosphate (ATP), 2) releasing ATP into the extracel lular space, 3) enzymatic conversion of ATP to adenosine, 4) activation of the adenosine receptor and the adenosine receptor cascade, and 5) clearance of adenosine from the extracellular space by degradation or uptake into a cell. The method includes affecting at least one of these steps so as to decrease the activation of the adenosine receptor pathway. This may be accomplished by decreasing the production, release, or conversion of ATP to adenosine, decreasing the expression of the adenosine receptor, antagonizing adenosine receptor activation, and/or increasing adenosine clearance.Type: ApplicationFiled: July 22, 2011Publication date: May 16, 2013Applicant: THE OHIO STATE UNIVERSITYInventor: Ian C. Davis
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Publication number: 20130123254Abstract: The present invention relates to mGluR5 positive allosteric modulators (PAM) and methods for identifying pharmaceutically acceptable compounds with high tolerability and safety, which method comprises the use of at least one non-competitive mGluR5 allosteric modulator which has a shift factor measured at 10 uM glutamate concentration below 3.Type: ApplicationFiled: September 14, 2012Publication date: May 16, 2013Inventors: Barbara Biemans, Georg Jaeschke, Lothar Lindemann, Wolfgang Muster, Heinz Stadler, Eric Vieira
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Publication number: 20130116286Abstract: The present invention is directed to methods of treating neurally mediated hypotension. In particular, the invention provides pharmaceutical compositions comprising droxidopa alone, or in combination with one or more further active ingredients, that can be administered to a patient for the treatment of neurally mediated hypotension.Type: ApplicationFiled: October 4, 2012Publication date: May 9, 2013Applicant: Chelsea Therapeutics, Inc.Inventor: Chelsea Therapeutics, Inc.
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Patent number: 8394839Abstract: The present invention relates to the use of isotopically labeled derivatives of isoniazid, ethionamide and related compounds as effective therapy for the treatment of mycobacterial diseases, including Mycobacterium tuberculosis.Type: GrantFiled: August 20, 2008Date of Patent: March 12, 2013Assignees: STC.UNM, The John Hopkins UniversityInventors: Graham Timmins, Vojo P Deretic
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Publication number: 20130059893Abstract: A novel crystalline form of the sodium salt of 4-tert-butyl-N-[4-chloro-2-(1-oxy-pyridine-4-carbonyl)-phenyl]-benzenesulfonamide and pharmaceutical compositions containing the same are disclosed. Processes for the preparation thereof and methods for use thereof are also disclosed.Type: ApplicationFiled: July 20, 2012Publication date: March 7, 2013Applicant: ChemoCentryx, Inc.Inventor: Andrew M.K. Pennell
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Patent number: 8388939Abstract: The subject matter of the present invention is a cosmetic or dermopharmaceutic composition comprising a combination of homarine and erythritol as well as a non-therapeutic treatment method of the skin to improve cutaneous hydration, to prevent and/or treat cutaneous dryness signs, to restore and/or protect the cutaneous barrier function, to protect cells of the skin and/or of the scalp from osmotic shocks, for example from UV induced osmotic shocks.Type: GrantFiled: February 13, 2009Date of Patent: March 5, 2013Assignee: Sederma, S.A.S.Inventors: Arnaud Fournial, Claire Mas-Chamberlin, Philippe Mondon, Olivier Peschard
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Patent number: 8383653Abstract: Compounds are disclosed which inhibit SIR2 base exchange more than deacetylation, thus enhancing SIR2 deacetylation activity. Methods of using the compounds for enhancing SIR2 deacetylation activity and increasing longevity of an organism are also disclosed. Methods for screening for compounds that enhance SIR2 deacetylation activity and increase longevity of an organism are additionally disclosed.Type: GrantFiled: June 30, 2004Date of Patent: February 26, 2013Assignee: Albert Einstein College of Medicine of Yeshiva UniversityInventors: Vern L. Schramm, Anthony A. Sauve
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Publication number: 20130045941Abstract: Embodiments of the invention relate generally to formulations comprising dimethylsulfoxide (DMSO) alone or in combination with methylsulfonylmethane (MSM), and one or more therapeutic agents, and uses of such formulations to treat infectious diseases. In several embodiments, such formulations are effective in treating drug-resistant infectious diseases, for example, drug-resistant tuberculosis.Type: ApplicationFiled: October 29, 2010Publication date: February 21, 2013Applicant: Abela Pharmaceuticals, Inc.Inventors: Colette Cozean, Rodney Benjamin, Anthony Keller, Jeff Varelman
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Patent number: 8349877Abstract: Ternary fungicidal compositions comprising as active components 1) boscalid, 2) chlorothalonil and 3) at least one active compound III, selected from groups A) to F): A) azoles; B) strobilurins; C) carboxamides; D) heterocyclic compounds; E) carbamates; F) other fungicides; in a synergistically effective amount, methods for controlling phytopathogenic harmful fungi using compositions of boscalid, chlorothalonil and at least one active compound III, the use of boscalid and chlorothalonil with at least one active compound III for preparing such compositions, and also agents and seed comprising such compositions.Type: GrantFiled: September 25, 2008Date of Patent: January 8, 2013Assignee: BASF SEInventors: Horst Dieter Brix, Daniel Ebersold, Martin Semar, Jens Bruns, Michael Vonend
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Publication number: 20120329800Abstract: Administration of a monoamine oxidase inhibitor is useful in the prevention and treatment of muscle dystrophy. Methods and compositions for inhibiting the production of reactive oxygen species in a muscle cell overproducing reactive oxygen species are provided herein.Type: ApplicationFiled: June 22, 2011Publication date: December 27, 2012Inventors: Paolo Bonaldo, Marcella Canton, Fabio DiLisa, Sara Menazza
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Publication number: 20120316147Abstract: The invention relates to a compound of formula (I) wherein R1 to R4 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.Type: ApplicationFiled: June 1, 2012Publication date: December 13, 2012Inventors: Caterina Bissantz, Uwe Grether, Paul Hebeisen, Atsushi Kimbara, Qingping Liu, Matthias Nettekoven, Marco Prunotto, Stephan Roever, Mark Rogers-Evans, Tanja Schulz-Gasch, Christoph Ullmer, Zhiwei Wang, Wulun Yang
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Publication number: 20120309724Abstract: In one aspect, the invention relates to compounds having the formula: where R1, R2, R3, X, R4, R5, and R6 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.Type: ApplicationFiled: May 18, 2012Publication date: December 6, 2012Applicant: THERAVANCE, INC.Inventors: Melissa Fleury, Roland Gendron, Adam D. Hughes, Jane Schmidt
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Publication number: 20120301422Abstract: The invention provides a method of enhancing the action of a pharmaceutical agent selected from the group consisting of the anti-infective agents, the group comprising of the antimicrobial agents, the anthelmintic agents and the anti-ectoparasitic agents, but excluding coal tar solution and H1-antagonist antihistamines, and from the group consisting of the CPNS agents selected from the group of compounds acting on the central or peripheral nervous system, but excluding coal tar solution and H1-antagonist antihistamines and also excluding anti-inflammatory, analgesic and antipyretic agents and also provides an enhanced method for the administration of a nucleic acid substance to the cells of an animal, a plant or a micro-organism.Type: ApplicationFiled: January 16, 2003Publication date: November 29, 2012Inventor: Petrus Johannes Meyer
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Publication number: 20120302610Abstract: The present invention is directed to picolanmido-propanoic acid derivatives, pharmaceutical compositions containing them and their use in the treatment and/or prevention of disorders and conditions ameliorated by antagonizing one or more glucagon receptors, including for example metabolic diseases such as Type II diabetes mellitus and obesity.Type: ApplicationFiled: May 23, 2012Publication date: November 29, 2012Inventors: Devraj Chakravarty, Kevin Kreutter, Mark Powell, Brian Shook, Fengbin Song, Guozhang Xu, Shyh-Ming Yang, Rui Zhang, Bao-Ping Zhao
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Patent number: 8318780Abstract: The present invention relates to methods involving avoiding adverse drug interactions with fluvoxamine and pirfenidone or other moderate to strong inhibitors of CYP enzymes.Type: GrantFiled: September 2, 2011Date of Patent: November 27, 2012Assignee: Intermune, Inc.Inventors: Williamson Ziegler Bradford, Javier Szwarcberg
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Patent number: 8309608Abstract: The present invention relates to the use of compounds which enhance the transcription of endothelial nitric oxide synthase (eNOS) for treating stem and progenitor cells in the cell therapy of patients with ischemic heart diseases such as coronary heart disease or ischemic cardiomyopathy. Treatment of such cells which are isolated from bone marrow, for example, with an eNOS transcription enhancer prior to their administration improves their functional activity and ameliorates neovascularization of the heart and cardiac regeneration.Type: GrantFiled: November 2, 2004Date of Patent: November 13, 2012Assignee: Sanofi-Aventis Deutschland GmbHInventors: Andreas Zeiher, Stefanie Dimmeler, Christopher Heeschen, Hartmut Ruetten
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Patent number: 8309596Abstract: The present invention relates to the crystal structure of the serine protease kallikrein 7 and to the use of this crystal structure in drug discovery. The present invention also relates to compounds binding specifically to this active site of kallikrein 7.Type: GrantFiled: June 26, 2008Date of Patent: November 13, 2012Assignee: Novartis AGInventors: Stefanie Flohr, Stefan Andreas Randl, Nils Ostermann, Ulrich Hassiepen, Frederic Berst, Ursula Bodendorf, Bernd Gerhartz, Andreas Marzinzik, Claus Ehrhardt, Josef Gottfried Meingassner
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Patent number: 8304394Abstract: The present invention features a novel, low side-effect pharmaceutical compound complex, comprising the pharmaceutically effective dose of isoniazid (INH) and pharmaceutically effective dose of one of the following compounds.Type: GrantFiled: July 23, 2008Date of Patent: November 6, 2012Assignee: National Defense Education and Research FoundationInventors: Yoapu Oliver Hu, Ton ho Young
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Publication number: 20120270852Abstract: The present invention relates to ethynyl derivatives of formula I wherein Y is N or C—R3; R3 is hydrogen, methyl, halogen or nitrile; R1 is phenyl or pyridinyl, each of which is optionally substituted by halogen, lower alkyl or lower alkoxy; R2/R2? are each independently hydrogen, lower alkyl or lower alkyl substituted by halogen, or R2 and R2? together with the N-atom to which they are attached form a morpholine ring, a piperidine ring or an azetidine ring, each of which is unsubstituted or substituted one or more substituents selected from lower alkoxy, halogen, hydroxy and methyl; R4/R4? are each independently hydrogen or lower alkyl, or R4 and R4? together form a C3-5 cycloalkyl-, tetrahydrofuran- or an oxetane-ring; or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof.Type: ApplicationFiled: April 11, 2012Publication date: October 25, 2012Inventors: Georg Jaeschke, Synese Jolidon, Lothar Lindemann, Antonio Ricci, Daniel Rueher, Heinz Stadler, Eric Vieira
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Publication number: 20120270873Abstract: The present invention provides adamantyl-diamide derivatives of formula (I): wherein R1 and R2 are as defined herein, or a pharmaceutically acceptable salt thereof; and pharmaceutical compositions and methods using the same.Type: ApplicationFiled: May 15, 2012Publication date: October 25, 2012Applicant: H. Lundbeck A/SInventors: Hermogenes N. JIMENEZ, Guiying LI, Dario DOLLER, Michel GRENON, Andrew D. WHITE, Gil MA, Maojun GUO
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METHODS OF USING [3.2.0] HETEROCYCLIC COMPOUNDS AND ANALOGS THEREOF FOR TREATING INFECTIOUS DISEASES
Publication number: 20120264678Abstract: Disclosed are methods of treating infectious diseases comprising administering to an animal, a therapeutically effective amount of a heterocyclic compound. The animal is a mammal, preferably a human or a rodent.Type: ApplicationFiled: June 6, 2012Publication date: October 18, 2012Applicant: NEREUS PHARMACEUTICALS, INC.Inventor: Michael Palladino -
Publication number: 20120252809Abstract: The present invention relates to compounds of the formula I, wherein A, D, E, L, G, R10, R30, R40, R50 and R60 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. They are inhibitors of the protease cathepsin A, and are useful for the treatment of diseases such as atherosclerosis, heart failure, renal diseases, liver diseases or inflammatory diseases, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.Type: ApplicationFiled: January 24, 2012Publication date: October 4, 2012Applicant: SANOFIInventors: Sven RUF, Thorsten SADOWSKI, Klaus WIRTH, Herman SCHREUDER, Christian BUNING
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Publication number: 20120252830Abstract: The present invention provides a compound of formula I?; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, X and n are defined herein. The invention also relates to a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.Type: ApplicationFiled: June 7, 2012Publication date: October 4, 2012Applicant: NOVARTIS AGInventors: Gary Mark Coppola, Yuki Iwaki, Rajeshri Ganesh Karki, Toshio Kawanami, Gary Michael Ksander, Muneto Mogi, Robert Sun
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Patent number: 8278337Abstract: Disclosed are compounds of the formula (I) wherein X is N or CH, and Y is N or CR5. Also disclosed are methods of treating JNK and ERK mediated diseases using the compounds of formula 1.0.Type: GrantFiled: December 17, 2007Date of Patent: October 2, 2012Assignee: Merck Sharp & DohmeInventors: David B. Belanger, M. Arshad Siddiqui, Patrick J. Curran, Blake Hamann, Lianyun Zhao, Panduranga Adulla P. Reddy, Praveen K. Tadikonda, Gerald W. Shipps, Jr., Umar Faruk Mansoor
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Patent number: 8278336Abstract: The present invention relates to new CGRP-antagonists of general formulae Ia and Ib wherein R1, R2, R3, R4 and R5 are defined as mentioned below, the tautomers, the isomers, the diastereomers, the enantiomers, the hydrates, the mixtures and the salts thereof as well as the hydrates of the salts, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, pharmaceutical compositions containing these compounds, the use thereof and processes for the preparation thereof.Type: GrantFiled: November 21, 2008Date of Patent: October 2, 2012Assignee: Boehringer Ingelheim International GmbHInventors: Dirk Gottschling, Georg Dahmann, Henri Doods, Annekatrin Heimann, Stephan Georg Mueller, Klaus Rudolf, Gerhard Georg Schaenzle, Dirk Stenkamp
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Publication number: 20120245185Abstract: In one aspect, the invention relates to sulfone compounds which are useful as allosteric potentiators/positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds, for example, in treating neurological and psychiatric disorders or other disease state associated with glutamate dysfunction.Type: ApplicationFiled: November 8, 2010Publication date: September 27, 2012Applicant: VANDERBILT UNIVERSITYInventors: P. Jeffrey Conn, Craig W. Lindsley, Corey R. Hopkins, Charles David Weaver, Colleen M. Niswender, Yiu-Yin Cheung
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Patent number: 8268891Abstract: Classes of compounds that exhibit effective inhibition of autotaxin enzymes are provided. Such classes include thioureas, diphenyldiazerenes, xanthenes, and isoindoles and exhibit reactivity with autotaxin to ultimately reduce the size of the reactive sites thereon to prevent conversion of lysophosphatidyl choline to lysophophatidic acid. Furthermore, such compounds can be incorporated within delivery forms for human ingestion. As such, these compounds accord an excellent manner of potentially reducing generation of certain cancers attributable to the presence of naturally occurring autotaxin within the human body. Methods of inactivating autotaxin to certain degrees therewith such compounds are encompassed within invention as well.Type: GrantFiled: November 13, 2008Date of Patent: September 18, 2012Assignee: University of Memphis Research FoundationInventors: Abby Louise Parrill-Baker, Daniel Lee Baker
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Publication number: 20120225883Abstract: The invention relates to compounds of structural formulas (I), (VII) and (XI): or a pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof, wherein X1, X2, X3, Y, Z, L, R1, R2, R3, R18 and n are defined herein. These compounds are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.Type: ApplicationFiled: May 14, 2012Publication date: September 6, 2012Applicant: Synta Pharmaceuticals Corp.Inventors: Lijun Sun, Shoujun Chen, Zhi-Qiang Xia, Jun Jiang, Yu Xie, Junyi Zhang
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Publication number: 20120225891Abstract: A compound represented by Formula (1): The compound can be used as insecticides.Type: ApplicationFiled: March 22, 2012Publication date: September 6, 2012Applicant: MITSUI CHEMICALS, INC.Inventors: Kei Yoshida, Takeo Wakita, Hiroyuki Katsuta, Akiyoshi Kai, Yutaka Chiba, Kiyoshi Takahashi, Hiroko Kato, Nobuyuki Kawahara, Michikazu Nomura, Hidenori Daido, Junji Maki, Shinichi Banba
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Patent number: 8247437Abstract: The present invention is related to N-hydroxyamide derivatives of Formula (I) and use thereof in particular for the treatment and/or prophylaxis of autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, cancer, respiratory diseases and fibrosis, including multiple sclerosis, arthritis, emphysema, chronic obstructive pulmonary disease, liver and pulmonary fibrosis.Type: GrantFiled: June 8, 2011Date of Patent: August 21, 2012Assignee: Merck Serono SAInventors: Dominique Swinnen, Agnes Bombrun, Jerome Gonzalez, Stefano Crosignani, Patrick Gerber, Catherine Jorand-Lebrun
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Patent number: 8242161Abstract: The present invention provides for, inter alia, novel topical formulations comprising at least one 1-N-arypyrazole derivative and amitraz and to methods for treating, controlling, or preventing parasite infestations on mammals or birds The inventive formulations include spot-on, pour-on or spray formulations and may include a further ectoparasiticide, such as an IGR compound, an avermectin or milbemycin derivative, or a pyrethroid insecticides, and anthelmintics, such as benzimidazoles and imidazothiazoles. The inventive formulation provides a larger duration of parasite control at a faster rate of control. The inventive formula remains effective up to three months from the first application. Moreover, the inventive formulations prevent tick attachment to the animal, thereby providing protection against tick borne diseases. The ectoparasites which may be controlled, treated or prevented by the present invention includes ticks, fleas, mites, mange, lice, mosquitoes, flies and cattle grubs.Type: GrantFiled: April 8, 2009Date of Patent: August 14, 2012Assignee: Merial LimitedInventors: Albert Boeckh, Luiz Gustavo Cramer, Mark D. Soll
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Patent number: 8242147Abstract: This invention relates to methods of using aryl ureas to treat diseases mediated by the VEGF induced signal transduction pathway characterized by abnormal angiogenesis or hyperpermeability processes.Type: GrantFiled: September 23, 2010Date of Patent: August 14, 2012Assignee: Bayer Healthcare LLCInventors: Jacques Dumas, William J. Scott, James Elting, Holia Hatoum-Makdad
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Patent number: 8242302Abstract: It is intended to provide a drug which is efficacious in treating and preventing diseases wherein ischemia or an inflammatory substance associated with ischemia participates in the onset or worsening thereof. Because of containing as the active ingredient a substance selected from among farnesol, a farnesol derivative, a tocopherol derivative, a tocotrienol derivative, pharmacologically acceptable salts thereof and solvates thereof, the above-described inhibitor of ischemic disorders can exert therapeutic and preventive effects on diseases wherein ischemia or an inflammatory substance associated with ischemia participates in the onset or worsening thereof (for example, brain infarction, brain edema, cardiac infarction, etc.) not only by the administration in the acute ischemic stage but also by the therapeutic administration in subacute and/or chronic stages after ischemia-reperfusion. It is also intended to provide a farnesol carboxylic acid ester derivative and a method of producing the same.Type: GrantFiled: September 1, 2008Date of Patent: August 14, 2012Assignee: Fukuoka UniversityInventors: Jiro Takata, Kenichi Mishima, Manabu Nakashima, Katsunori Iwasaki, Kazuhisa Matsunaga, Yoshiharu Karube, Michihiro Fujiwara
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Publication number: 20120196865Abstract: The present invention relates to acyl guanidine derivatives modulating the hedgehog protein signaling pathway to be used as drugs, in particular for treating diseases involving a tissue dysfunction associated with a deregulation of the hedgehog protein signaling pathway, as well as to pharmaceutical compositions containing same. The present invention also relates to novel acyl guanidine derivatives as such.Type: ApplicationFiled: July 19, 2010Publication date: August 2, 2012Applicants: UNIVERSITE DE STRASBOURG, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUEInventors: Martial Ruat, Hélène Faure, Elisabeth Traiffort, Hermine Roudaut, André Mann, Angèle Schoenfelder, Maurizio Taddei, Fabrizio Manetti, Antonio Solinas
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Patent number: 8232300Abstract: A compound represented by the following general formula (I): [wherein R1 represents hydrogen atom or a C1-6 alkyl group, A and B represent —(CH2)2—, —(CH2)3—or —(CH2)4—, X represents —N(R2)—CO—(R2 represents hydrogen atom or a C1-6 alkyl group), —CO—N(R3)—(R3 represents hydrogen atom or a C1-6 alkyl group), —C(R4)?C(R5)—(R4 and R5 represent hydrogen atom or a C1-6 alkyl group), or —N(R6)—SO2—(R6 represents hydrogen atom or a C1-6 alkyl group), and Ar represents an aryldiyl group or a heteroaryldiyl group], which has a retinoid action and is useful as an active ingredient of a medicament.Type: GrantFiled: August 14, 2008Date of Patent: July 31, 2012Assignee: Research Foundation Itsuu LaboratoryInventors: Yohei Amano, Masayuki Noguchi, Koichi Shudo
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Patent number: 8232295Abstract: The present invention relates to new methods for treating and/or preventing vascular events by inhibiting G-coupled Protease Activating Receptor (PAR)-1 and/or PAR-4 with the administration of statins. In one embodiment, individuals who are at risk for vascular events, but have cholesterol levels (e.g., total cholesterol or Low Density Lipoprotein) in normal ranges, are treated with statins.Type: GrantFiled: November 29, 2010Date of Patent: July 31, 2012Assignee: Heartdrug Research, L.L.C.Inventor: Victor L. Serebruany