Nitrogen Containing Patents (Class 514/466)
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Publication number: 20130281490Abstract: The present invention provides compounds and pharmaceutical compositions for inhibiting N-acylethanolamine acid amidase (NAAA). Inhibition of NAAA is contemplated as a method to sustain the levels of palmitoylethanolamide (PEA) and oleylethanolamide (OEA), two substrates of NAAA, in conditions characterized by reduced concentrations of PEA and OEA. The invention also provides methods for treating inflammatory diseases and pain, and other disorders in which decreased levels of PEA and OEA are associated with the disorder.Type: ApplicationFiled: November 21, 2012Publication date: October 24, 2013Inventors: The Regents of the University of California, Fondazione Istituto Italiano Di Tecnologia, Universita Degli Studi Di Parma, Universita Degli Studi Di Urbino "Carlo Bo"
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Publication number: 20130236434Abstract: A method of enhancing binding of cells to an integrin-binding ligand comprises treating integrin-expressing cells in vitro with an agonist of integrin, wherein the integrin is selected from the group consisting of ?4?1, ?5?1, ?4?7, ?v?3 and ?L?2, and contacting the treated cells with an integrin-binding ligand; integrin agonist compounds having the general formula I; methods of treating integrin-expressing cells with such agonists to enhance binding; and therapeutic methods comprising administering agonist-treated cells or agonist compounds to a mammal.Type: ApplicationFiled: November 16, 2011Publication date: September 12, 2013Applicant: TEXAS HEART INSTITUTEInventors: Ronald J. Biediger, William C. Gundlach, IV, Robert V. Market, Michael M. Savage, Peter Vanderslice
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Patent number: 8518940Abstract: The present invention embraces compounds selected for interacting with the Fingers-Palm pocket of telomerase and use thereof for modulating the activity of telomerase and preventing or treating diseases or conditions associated with telomerase.Type: GrantFiled: February 8, 2010Date of Patent: August 27, 2013Assignee: The Wistar InstituteInventor: Emmanuel Skordalakes
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Publication number: 20130203709Abstract: The present disclosure relates to acylsulfonamides and processes for their preparation. The processes involve a target-guided synthesis approach, whereby a thioacid and a sulfonyl azide are reacted in the presence of a biological target protein, a Bcl-2 family protein, to form the acylsulfonamide.Type: ApplicationFiled: August 9, 2011Publication date: August 8, 2013Applicants: THE PENN STATE RESEARCH FOUNDATION, UNIVERSITY OF SOUTH FLORIDAInventors: Roman Manetsch, Sameer Kulkarni, Iredia D. Iyamu, Hong-Gang Wang, Kenichiro Doi, Wayne Guida, Daniel Santiago, Courtney du Boulay
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Publication number: 20130184222Abstract: Provided are methods of treating a cancer characterized by the presence of a mutant allele of IDH1 comprising administering to a subject in need thereof a compound described here.Type: ApplicationFiled: July 15, 2011Publication date: July 18, 2013Applicant: AGIOS PHARMACEUTICALS, INCInventors: Janeta Popovici-Muller, Francesco G. Salituro, Jeffrey Saunders, Jeremy Travins, Shunqi Yan
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Publication number: 20130178520Abstract: Described herein are methods of treating Parkinson's disease using arylcyclopropylamine compounds.Type: ApplicationFiled: December 21, 2012Publication date: July 11, 2013Applicant: DUKE UNIVERSITYInventor: Duke University
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Publication number: 20130171158Abstract: A method of treating or preventing an abnormality of glucose metabolism in a subject, the method comprising administering an antagonist of Inhibitor of Differentiation 1 (Id1) to the subject.Type: ApplicationFiled: June 29, 2011Publication date: July 4, 2013Applicant: GARVAN INSTITUTE OF MEDICAL RESEARCHInventors: Mia Akerfeldt, Ross Laybutt
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Publication number: 20130165507Abstract: The invention relates to novel guanidine derivatives in the cinnamic series of general formula (I): The invention also relates to the process for preparing said guanidine derivatives and also to synthetic intermediates. Finally, the invention relates to the use of the guanidine derivatives for the preparation of compositions with anti-glycation properties, especially in cosmetology.Type: ApplicationFiled: September 6, 2011Publication date: June 27, 2013Applicant: PRODUITS CHIMIQUES AUXILIAIRES ET DE SYNTHESEInventors: Sylvain Rault, Jean Charles Lancelot, Peggy Suzanne, Anne-Sophie Voisin-Chiret, Regis Pecquet, Jean-Christophe Joseph
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Publication number: 20130157986Abstract: Pharmaceutical compounds and compositions are provided which are methylenedioxy phenolic compounds and their derivatives, along with methods of making them and methods of using them for therapeutic purposes. The compounds and compositions are advantageous in that they can be used to treat or prevent cardiovascular disease, vascular disease and/or inflammatory disease, as well as Type I and Type II Diabetes and Dyslipidemia patients at risk for hypertension, stroke, cardiovascular and renal disease.Type: ApplicationFiled: June 12, 2012Publication date: June 20, 2013Applicants: INVASC THERAPEUTICS, INC., OHIO STATE UNIVERSITY RESEARCH FOUNDATIONInventors: SAMPATH PARTHASARATHY, SANJAY RAJAGOPALAN, DESIKAN RAJAGOPAL
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Patent number: 8450525Abstract: Novel compounds of the general formula (I), having histone deacetylase (HDAC) inhibiting enzymatic activity, their derivatives, analogs, tautomeric forms, stereoisomers, polymorphs, hydrates, solvates, intermediates, pharmaceutically acceptable salts, pharmaceutical compositions, metabolites and prodrugs thereof. The present invention more particularly provides novel compounds of the general formula (I). Also included is a method for treatment of cancer, psoriasis, proliferative conditions and conditions mediated by HDAC, in a mammal comprising administering an effective amount of a novel compound of formula (I).Type: GrantFiled: October 21, 2008Date of Patent: May 28, 2013Assignee: Orchid Chemicals & Pharmaceuticals LimitedInventors: Sridharan Rajagopal, Virendra Kachhadia, Thanasekaran Ponpandian, Abdul Raheem Keeri, Karnambaram Anandhan, Sriram Rajagopal, Rajendran Praveen, Prabhu Daivasigamani
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Publication number: 20130116203Abstract: The present invention provides glucosinolate and isothiocyanate compounds and related methods for synthesizing these compounds and analogs. In certain embodiments, these glucosinolate and isothiocyanate compounds are useful and chemopreventive and or chemotherapeutic agents.Type: ApplicationFiled: November 7, 2011Publication date: May 9, 2013Inventors: Scott R. Rajski, Jared Rae Mays
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Publication number: 20130109714Abstract: Provided is an unprecedented composition that is not a conventional symptomatic treatment, but makes possible the fundamental treatment of current neurodegenerative diseases by inhibiting oxidative-stress induced nerve-cell death. The disclosed neurodegenerative disease therapeutic agent includes a compound, or a salt of said compound, that inhibits oxidative-stress induced nerve-cell death to a high degree and is an agent used in the treatment of neurodegenerative diseases such as Parkinson's disease.Type: ApplicationFiled: March 25, 2011Publication date: May 2, 2013Applicant: National University Corporation Hokkaido UniversityInventor: Hiroyoshi Ariga
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Publication number: 20130095140Abstract: Provided herein are methods for treating certain conditions, including diabetes, obesity, and other metabolic diseases, disorders or conditions by administrating a composition comprising a biguanide or related heterocyclic compound, e.g., metformin. Also provided herein are biguanide or related heterocyclic compound compositions, and methods for the preparation thereof for use in the methods of the present invention. Also provided herein are compositions comprising metformin and salts thereof and methods of use.Type: ApplicationFiled: July 11, 2012Publication date: April 18, 2013Applicant: Elcelyx Therapeutics, Inc.Inventors: Alain D. Baron, Mark S. Fineman, Nigel R. A. Beeley
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Publication number: 20130071353Abstract: Inhibitors of retroviral propagation, methods of treatment and prevention of retroviral infections using the inhibitors, and pharmaceutical compositions including the inhibitors, are disclosed.Type: ApplicationFiled: March 14, 2011Publication date: March 21, 2013Applicant: TRANA DISCOVERY, INCInventors: Richard H. Guenther, Jerzy R. Szewczyk
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Publication number: 20130071328Abstract: This invention discloses a series of novel propynoic acid carbamoyl methyl-amides (PACMAs), methods for synthesizing the PACMAs and pharmaceutical compositions containing the PACMAs. These novel compounds and compositions show cytotoxicity in cancer cells and are useful as lead compounds for anti-cancer drugs or pharmaceutical agents. This invention also discloses treatment methods that uses the PACMAs and pharmaceutical compositions as well as methods for promoting the release and nuclear localization of the transcription factor Nrf2.Type: ApplicationFiled: March 22, 2012Publication date: March 21, 2013Applicant: UNIVERSITY OF SOUTHERN CALIFORNIAInventors: Nouri NEAMATI, Nicos A. PETASIS, Roppei YAMADA
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Publication number: 20130005782Abstract: This invention relates generally to integrin ligand discovery and to a method of integrin ligand discovery base upon induction of ligand-induced epitopes. Such ligands have the potential to be active agent as anti-inflammatory, anti-angiogenesis and/or anti-thrombotic agents and for the treatment of integrin mediated diseases and/or conditions.Type: ApplicationFiled: March 23, 2011Publication date: January 3, 2013Inventors: Alexandre Chigaev, Larry A. Sklar
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Publication number: 20120329786Abstract: The invention relates to compounds, pharmaceutical compositions and methods useful for treating cancer, systemic or chronic inflammation, rheumatoid arthritis, diabetes, obesity, T-cell mediated autoimmune disease, ischemia, and other complications associated with these diseases and disorders.Type: ApplicationFiled: August 31, 2012Publication date: December 27, 2012Applicant: Myrexis, Inc.Inventors: J. Adam Willardsen, Jeffrey W. Lockman, Brett R. Murphy, Weston R. Judd, In Chul Kim, Se-Ho Kim, Daniel Feodore Zigar, Kraig M. Yager, Tracey C. Fleischer, Ryan T. Terry-Lorenzo, J. Jay Boniface, Daniel P. Parker, Ian A. McAlexander, Matthew Gregory Bursavich, David M. Dastrup
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Publication number: 20120322796Abstract: The present invention relates to a compound of formula (I) including any stereochemically isomeric form thereof, wherein the substituents are as defined in the specification and the claims; a N-oxide thereof, a pharmaceutically acceptable salt thereof or a solvate thereof; provided that the compound is other than or a pharmaceutically acceptable salt thereof. The claimed compounds are useful for the treatment of a disease, the treatment of which is affected, mediated or facilitated by activating the GHS1A-r receptor. The invention also relates to pharmaceutical compositions thereof and processes for the preparation thereof.Type: ApplicationFiled: August 29, 2012Publication date: December 20, 2012Inventors: Bruno SCHOENTJES, Alain Philippe PONCELET, Julien Georges Pierre-Olivier DOYON, Joannes Theodorus Maria LINDERS, Lieven MEERPOEL, Luc August Laurentius VER DONCK
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Publication number: 20120316066Abstract: The present invention provides diacylhydrazine ligands and chiral diacylhydrazine ligands for use with ecdysone receptor-based inducible gene expression systems. Thus, the present invention is useful for applications such as gene therapy, large scale production of proteins and antibodies, cell-based screening assays, functional genomics, proteomics, metabolomics, and regulation of traits in transgenic organisms, where control of gene expression levels is desirable. An advantage of the present invention is that it provides a means to regulate gene expression and to tailor expression levels to suit the user's requirements.Type: ApplicationFiled: December 2, 2011Publication date: December 13, 2012Applicant: Intrexon CorporationInventors: Robert Eugene HORMANN, Bing Li
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Patent number: 8318772Abstract: The present invention relates to a new amine compound or a pharmaceutically acceptable salt thereof, wherein the definitions of X, R1, R2 and n are given in the description, to a pharmaceutical composition containing the compound as active ingredient, and to use of the amine compound or its pharmaceutically acceptable salt for the manufacture of an anti-depressent drug.Type: GrantFiled: June 23, 2009Date of Patent: November 27, 2012Assignee: Institute of Pharmacology and Toxicology Academy of Military Medical Sciences P.L.A. ChinaInventors: Bohua Zhong, Youzhi Zhang, Yanping Zhang, Rui Xue, Xinhua He, Yunfeng Li, Hongxia Chen, Nan Zhao, Meiying Li
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Patent number: 8318798Abstract: [Problems] To provide a neuronal cell death inhibitor and a therapeutic agent for a neurodegenerative disease, particularly Parkinson's disease. [Means for Solving Problems] It is known that DJ-1 protein is involved in Parkinson's disease and is capable of inhibiting neuronal cell death caused by oxidative stress. Based on this knowledge, screening is made for a low molecular weight molecule capable of binding to an active site of DJ-1 protein (i.e., a region around a cysteine residue at position-106) using an analysis softwear FastDock (Fujitsu Ltd.). When various tests are made using candidate low molecular weight compounds each having a binding energy of ?60 kcal/mol or lower, these compounds show a therapeutic effect on a neurodegenerative disease.Type: GrantFiled: November 17, 2006Date of Patent: November 27, 2012Assignee: National University Corporation Hokkaldo UniversityInventor: Hiroyoshi Ariga
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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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Publication number: 20120283200Abstract: The present invention provides a pharmaceutical composition for preventing or treating a chronic heart disease, comprising a compound of a formula (I): wherein: R1 is one independently selected from a group consisting of a hydrogen, a methyl and an ethyl; R2 is one of a hydrogen and a methyl; and R3 is one selected from a group consisting of a hydrogen, (CH2)nAr and (CH2)nArR?R?, wherein n is one of 1 and 2, R? and R? is located at C-3 and C-4 positions, respectively, R? is a hydrogen and R? is one of a hydroxy, a fluorine, a bromine and a OMe, or R?+R?=—OCH2O—; or R2+R3 is one of wherein n is one of 4 and 5.Type: ApplicationFiled: March 27, 2012Publication date: November 8, 2012Applicants: CHINA MEDICAL UNIVERSITY, National Taiwan UniversityInventors: MING-JAI SU, YUEH-HSIUNG KUO
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Publication number: 20120270902Abstract: The invention provides N-substituted benzenesulfonamides for use in treating or preventing cognitive disorders, such as Alzheimer's Disease. Compounds of particular interest are defined by Formula (I), wherein R1, R2, R3, R4, and R3?, are as described in the specification. The invention also encompasses pharmaceutical compositions comprising compounds of Formula (I) as well as methods of treating cognitive disorders, including Alzheimer's disease using compounds of Formula (I).Type: ApplicationFiled: February 13, 2012Publication date: October 25, 2012Applicant: ELAN PHARMACEUTICALS, INC.Inventors: Martin Neitzel, Jennifer Marugg
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Patent number: 8293794Abstract: The present invention provides novel methods and compositions for the treatment and prevention of CNS-related conditions. One of the CNS-related conditions treated by the methods and compositions of the invention is Alzheimer's disease.Type: GrantFiled: April 2, 2010Date of Patent: October 23, 2012Assignee: Adamas Pharmaceuticals, Inc.Inventors: Gregory T. Went, Timothy J. Fultz, Laurence R. Meyerson
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Publication number: 20120263659Abstract: The invention relates to a TRPM8 modulator for achieving a cooling effect on the skin or a mucous membrane.Type: ApplicationFiled: November 22, 2010Publication date: October 18, 2012Applicants: BASF SE, SYMRISE AGInventors: Thomas Subkowski, Michael Backes, Heiko Oertling, Arnold Machinek, Hubert Loges, Ulrike Simchen, Horst Surburg, Claus Bollschweiler, Jens Wittenberg, Wolfgang Siegel
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Publication number: 20120238604Abstract: The present invention relates to a compound of general formula (I) or a pharmaceutically acceptable salt or solvate or thereof. In particular, the present invention relates to a method treating diseases involving cell proliferation, migration, apoptosis, or adhesion, comprising administering to a human or non-human mammalian patient an effective amount of a compound of general formula (I) or a pharmaceutically acceptable salt or solvate or thereof.Type: ApplicationFiled: September 3, 2010Publication date: September 20, 2012Applicant: Molecular Discovery SystemsInventor: Robin Scaife
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Publication number: 20120225935Abstract: Disclosed is a method of treatment and/or prophylaxis of a microbial infection, employing compounds of formula (I), in which X and Y are either the same of different and selected from a hereroatiom; is a double or single bond depending on the heteroatoms X and Y; R1 to R5 are either the same or different and selected from hydrogen or a non-deleterious substituent; and R6 to R7 are either the same or different and selected from hydrogen and a non-deleterious substituent or one of R6 to R7 are absent when there is a double bond present. Also disclosed are methods for protecting a subject from radiation damage, methods of cancer radiotherapy, and use of the disclosed compounds as an antimicrobial or radioprotective agent.Type: ApplicationFiled: March 20, 2012Publication date: September 6, 2012Applicant: BIODIEM LTD.Inventors: Peter Prokofievich Denisenko, Nikolay Sergeevich Sapronov, Alexander Alexandrovich Tarasenko
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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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Publication number: 20120184607Abstract: The present invention relates to the use of piperphentonamine or pharmaceutically acceptable salts thereof to prevent/treat encephalopathy in mammals, and the use of a combination of piperphentonamine or pharmaceutically acceptable salts thereof and other medicines in manufacture a medicine to prevent/treat encephalopathy in mammals. The mammals include human beings, and the encephalopathy includes cerebral injury related diseases or cerebrovascular diseases. The cerebrovascular diseases refer to cerebral ischemia, cerebral ischemia/reperfusion-induced injury or cerebral hemorrhage. The cerebral hemorrhage includes hypertensive cerebral hemorrhage, cerebral hemorrhage secondary to infarction, tumor cerebral hemorrhage or cerebral hemorrhage caused by arteritis. The cerebral ischemia means carotid system cerebral ischemia or vertebrobasilar cerebral ischemia.Type: ApplicationFiled: October 20, 2009Publication date: July 19, 2012Inventors: Huayin Wan, Rubing Li, Lijian Zhou, Tieqiu Liu, Yanshu Chen, Yonghe Li
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Publication number: 20120157462Abstract: Compounds having the formula wherein the symbols have the meaning described in the specification are hydroxamic acid derivatives of aniline and capable of inhibiting the lethal effects of infection by anthrax bacteria and are useful in the treatment of poisoning by anthrax.Type: ApplicationFiled: January 30, 2008Publication date: June 21, 2012Inventors: Alan T. Johnson, Guan-Sheng Jiao
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Publication number: 20120135984Abstract: Provided are compounds, compositions, and methods for treating diseases and conditions wherein an inhibitor of a kinase, such as rho kinase (ROCK), and an inhibitor of one or more of the monoamine transporters, such as NET or SERT, act in concert to improve the condition.Type: ApplicationFiled: May 1, 2010Publication date: May 31, 2012Inventors: Mitchell A. deLong, Jill Marie Sturdivant, Susan M. Royalty, Geoffrey Richard Heintzelman, Jeffrey D. Yingling, Casey Kopczynski
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Publication number: 20120122784Abstract: The invention relates to novel calcium-sensing receptor (CaSR) modulating substituted cyclopentylene compounds represented in formula I and derivatives thereof, to said compounds for use as a medicament, to said compounds for use in therapy, to pharmaceutical compositions comprising said compounds, to methods of treating diseases with said compounds, and to the use of said compounds in the manufacture of medicaments.Type: ApplicationFiled: May 26, 2010Publication date: May 17, 2012Applicant: LEO PHARMA A/SInventors: Bjarne Nørremark, Lars Kristian Albert Blæhr, Anne Eeg Knapp, Kristoffer Månsson
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Publication number: 20120122870Abstract: Ischemia-reperfusion injury remains a primary cause of morbidity and mortality in individuals who experience disruption of normal blood flow to one or more major organs. For example, there are no clinically proven strategies that prevent acute renal failure following cardiac surgery. The present invention provides a variety of methods for the treatment or prevention of ischemia-reperfusion injury. In one aspect of the invention, a method for treating or preventing ischemia-reperfusion injury includes administering to a subject an effective amount of a sphingosine kinase inhibitor. Sphingosine kinase inhibitors are very effective in the protection against IR-induced acute renal failure and liver failure. Moreover, the effects occur very early after administration, requiring only a very short time of treatment. Toxicology studies with sphingosine kinase inhibitors demonstrate that they have low toxicity, even in long-term treatment.Type: ApplicationFiled: May 10, 2010Publication date: May 17, 2012Applicants: MUSC FOUNDATION FOR RESEARCH DEVELOPMENT, APOGEE BIOTECHNOLOGY CORPORATIONInventors: Charles D. Smith, Zhi Zhong, Lynn W. Maines
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Publication number: 20120122844Abstract: The present invention provides the use of a neutral endopeptidase inhibitor, in the manufacture of a medicament for the treatment, amelioration and/or prevention of contrast-induced nephropathy. The invention also relates to the use of a compound of Formula I: wherein R1, R2, R3, R5, X, A3, B1, s and n are defined herein, for the treatment, amelioration and/or prevention of contrast-induced nephropathy. The present invention further provides a combination of pharmacologically active agents for use in the treatment, amelioration and/or prevention of contrast-induced nephropathy.Type: ApplicationFiled: November 11, 2011Publication date: May 17, 2012Applicant: NOVARTIS AGInventor: Shi Yin FOO
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Publication number: 20120114633Abstract: Organic compounds showing the ability to inhibit effector toxin secretion or translocation mediated by bacterial type III secretion systems are disclosed. The disclosed type III secretion system inhibitor compounds are useful for combating infections by Gram-negative bacteria such as Salmonella spp., Shigella flexneri, Pseudomonas spp., Yersinia spp., enteropathogenic and enteroinvasive Escherichia coli, and Chlamydia spp. having such type III secretion systems.Type: ApplicationFiled: April 6, 2010Publication date: May 10, 2012Inventors: Donald T. Moir, Daniel Aiello, Norton P. Peet, John D. Williams
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Patent number: 8173708Abstract: The invention provides methods and compositions for administering an NMDA receptor antagonist (e.g., memantine) to a subject.Type: GrantFiled: April 9, 2010Date of Patent: May 8, 2012Assignee: Adamas Pharmaceuticals, Inc.Inventors: Gregory T. Went, Timothy J. Fultz, Laurence R. Meyerson
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Publication number: 20120093742Abstract: A method of modulating the flavour of an orally-receivable product, such as a foodstuff, beverage, dentifrice or medicine, comprising the addition thereto of a flavour-modulating proportion of at least one compound of the formula I in which X is selected from CHOH, C?O, CH2—CO and CH?C(OH), Y is selected from C1-C7 linear and branched alkyl and CH2CH2OH, Z is selected from CH3 and a moiety of the formula II in which the wavy bond represents bond linking Z to X and R1 and R2 are selected from the possibilities (i) both hydrogen; (ii) independently OH and OCH3; and (iii) R1 and R2 together with their bonds to the phenyl ring form a ring of the formula —O—CH2—O—; such that, when Z is CH3, X is C?O and Y is CH2CH2OH.Type: ApplicationFiled: June 24, 2010Publication date: April 19, 2012Applicant: Givaudan S.A.Inventors: Abdelmajid Kaouas, Harry Renes, Alexander P. Tondeur, Cornelis Winkel
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Patent number: 8158664Abstract: The present invention relates to a method of treatment and/or prophylaxis of a microbial infection, comprising the step of administering an effective amount of a compound of formula (I), in which X and Y are either the same or different and selected from a heteroatom; is a double or single bond depending on the heteroatoms X and Y; R1 to R5 are either the same or different and selected from hydrogen or a non-deleterious substituent; and R6 and R7 are either the same or different and selected from hydrogen and a non-deleterious substituent or one of R6 and R7 are absent when there is a double bond present, pharmaceutically acceptable salts or derivatives, pro-drugs, tautomers and/or isomers thereof. The present invention also relates to a method for protecting a subject from radiation damage, a method of cancer radiotherapy and use as an antimicrobial or radioprotective agent of the compound of formula (I) defined above.Type: GrantFiled: May 10, 2010Date of Patent: April 17, 2012Assignee: Biodiem Ltd.Inventors: Peter Prokofievich Denisenko, Nikolay Sergeevich Sapronov, Alexander Alexandrovich Tarasenko
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Publication number: 20120046288Abstract: The present invention relates to substituted hydrazonamide compounds. The invention further relates to methods of inhibiting the activity of Hs?90 in a subject in need thereof and methods for treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted hydrazonamide compound of the invention, or a pharmaceutical composition comprising such a compound.Type: ApplicationFiled: June 26, 2009Publication date: February 23, 2012Inventors: Joseph A. Burlison, Dinesh U. Chimmanamada, Weiwen Ying, Shijie Zhang, David James
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Publication number: 20120041025Abstract: Compounds are provided that comprise dinitroso-derivatives of dihydrolipoic acid. Pharmaceutical compositions comprising the compounds and methods of using the compounds for treating various diseases and disorders, including angina, hypertension, diabetes, dyslipidemia, renal insufficiency, myocardial infarction, stroke, atherosclerosis, and the target organ damage that accompanies these various diseases and disorders, are further provided. The compounds are useful in improving vasodilation, reducing low-density lipoprotein oxidation, and reducing inflammation in a subject.Type: ApplicationFiled: February 19, 2010Publication date: February 16, 2012Inventor: Sampath Parthasarathy
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Publication number: 20120022086Abstract: Novel compounds, compositions, and methods related to the activation of the TrkB receptor are provided. The methods include administering in vivo or in vitro a therapeutically effective amount of a compound containing a catecholamine backbone and pharmaceutically acceptable salts, prodrugs, and derivatives thereof. Specifically, methods, compositions, and compounds for the treatment of disorders including neurological disorders, neuropsychiatric disorders, and metabolic disorders are provided. For example, a first method is provided of treating or reducing the risk of depression, anxiety, or obesity in a subject, which includes administering to the subject a therapeutically effective amount of the described compounds. A further method of promoting neuroprotection in a subject also is provided, which includes administering to the subject a therapeutically effective amount of the described compounds.Type: ApplicationFiled: March 17, 2010Publication date: January 26, 2012Applicant: EMORY UNIVERSITYInventor: Keqiang Ye
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Publication number: 20120010075Abstract: The present invention relates to the use of mixtures containing hydrazone compounds and copper for controlling the growth of fungi.Type: ApplicationFiled: January 14, 2010Publication date: January 12, 2012Applicant: Dow Agrosciences LLCInventors: David H. Young, Steven Howard Shaber, Cruz Avila-Adame, Nneka T. Breaux, James M. Ruiz, Thomas L. Siddall, Jeffery D. Webster
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Publication number: 20120010248Abstract: The present invention provides compounds that function as modulators of mitochondrial aldehyde dehydrogenase-2 (ALDH2) activity; and pharmaceutical compositions comprising the compounds. The present invention provides therapeutic methods involving administering a subject compound, or a subject pharmaceutical composition. The present invention further provides assays for identifying agonists of ALDH2.Type: ApplicationFiled: August 22, 2011Publication date: January 12, 2012Inventors: Daria Mochly-Rosen, Che-Hong Chen, Xiaohu Ouyang
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Patent number: 8088820Abstract: This invention provides a method for treating or preventing malaria in a subject. The method includes administering to the subject an effective amount of a substituted tetracycline compound, such that malaria is treated or prevented. In one aspect, the invention relates to pharmaceutical compositions which include an effective amount of a tetracycline compound to treat malaria in a subject and a pharmaceutically acceptable carrier. The substituted tetracycline compounds of the invention can be used to in combination with one or more anti-malarial compounds or can be used to treat or prevent malaria which is resistant to one or more other anti-malarial compounds.Type: GrantFiled: October 24, 2003Date of Patent: January 3, 2012Assignee: Paratek Pharmaceuticals, Inc.Inventors: Michael Draper, Mark L. Nelson
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Publication number: 20110275663Abstract: The present invention relates to the use of acylthiourea or acylurea derivatives for the treatment of pathologies involving a tissue dysfunction associated with a deregulation of the Hedgehog protein signalling pathway, and also to novel acylthiourea or acylurea derivatives as such, to their use as a medicinal product, and to pharmaceutical compositions containing them.Type: ApplicationFiled: April 16, 2009Publication date: November 10, 2011Inventors: Martial Ruat, Hélène Faure, Elisabeth Traiffort, Angèle Schoenfelder, André Mann, Maurizio Taddei, Antonio Solinas, Fabrizio Manetti
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Publication number: 20110207810Abstract: The present invention provides an N1-benzo[1,3]dioxol-5-ylmethyl-N2-substituted biguanide derivative of formula (I) or a pharmaceutically acceptable salt thereof, a method for preparing same, and a pharmaceutical composition comprising same as an active ingredient. The inventive N1-benzo[1,3]dioxol-5-ylmethyl-N2-substituted biguanide derivative exhibits improved blood glucose level- and lipid level-lowering effects even with a reduced dosage as compared to conventional drugs, and thus, it is useful for preventing or treating diabetes, metabolic syndromes such as insulin-independent diabetes, obesity and atherosclerosis, or a P53 gene defect-related cancer.Type: ApplicationFiled: October 13, 2009Publication date: August 25, 2011Applicants: HANALL BIOPHARMA CO., LTD., KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGYInventors: Sung Wuk Kim, Sung Soo Jun, Hyae Gyeong Cheon, Kwang Rok Kim, Sang Dal Rhee, Won Hoon Jung, Jong Cheol Lee
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Publication number: 20110189306Abstract: The present invention relates to therapeutic and/or prophylactic uses of hydrazide compounds and to pharmaceutical compositions containing one or more of these compounds as an active component for treating a disease or disorder requiring modulation of vacuolar (H+)-ATPases.Type: ApplicationFiled: January 13, 2011Publication date: August 4, 2011Inventors: Norbert Kartner, Morris Frank Manolson
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Patent number: RE42889Abstract: ?- and ?-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: April 23, 2007Date of Patent: November 1, 2011Assignee: G.D. Searle LLCInventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, John N. Freskos, Robert M. Heintz, Deborah E. Bertenshaw
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Patent number: RE43802Abstract: ?- and ?-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: September 21, 2011Date of Patent: November 13, 2012Assignee: G.D. Searle LLCInventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, John N. Freskos, Deborah E. Bertenshaw, Robert M. Heintz