Thiocarbazides Or Thiosemicarbazides (i.e., N-n-c(=s)-n Containing) Patents (Class 514/581)
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Publication number: 20140371291Abstract: A novel serine racemase inhibitor exhibits sufficient activity and specificity. The serine racemase inhibitor includes one or more compounds selected from compounds respectively represented by the following general formulas [MM_1], [DR_1], [DR?_1], [LW_1], and [ED_1] as an active ingredient.Type: ApplicationFiled: January 24, 2013Publication date: December 18, 2014Inventors: Hisashi Mori, Naoki Toyooka, Mineyuki Mizuguchi, Takayuki Obita, Syuichi Hirono, Hiroaki Goda
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Patent number: 8501811Abstract: Provided herein are small molecule inhibitors of Taspase1 and methods of using the small molecule inhibitors of Taspase1 to treat neoplasm in subjects in need thereof.Type: GrantFiled: June 17, 2011Date of Patent: August 6, 2013Assignee: Washington UniversityInventors: James Hsieh, Emily Cheng
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Publication number: 20120015990Abstract: Provided herein are small molecule inhibitors of Taspase1 and methods of using the small molecule inhibitors of Taspase1 to treat neoplasm in subjects in need thereof.Type: ApplicationFiled: June 17, 2011Publication date: January 19, 2012Applicant: THE WASHINGTON UNIVERSITYInventors: James Hsieh, Emily Cheng
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Publication number: 20110118338Abstract: A method for identifying compounds that inhibit amyloid-beta precursor protein processing in cells, comprising contacting a test compound with a GPCR polypeptide, or fragment thereof, and measuring a compound-GPCR property related to the production of amyloid-beta peptide. Cellular assays of the method measure indicators including second messenger and/or amyloid beta peptide levels. Therapeutic methods, and pharmaceutical compositions including effective amyloid-beta precursor processing-inhibiting amounts of GPCR expression inhibitors, are useful for treating conditions involving cognitive impairment such as Alzheimers Disease.Type: ApplicationFiled: February 1, 2011Publication date: May 19, 2011Applicant: GALAPAGOS BVInventors: Reginald Brys, Nick Vandeghinste, Peter Herwig Maria Tomme
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Publication number: 20110053880Abstract: The invention relates to a pharmaceutical composition comprising a compound preventing EthR from binding to the ethA promoter, for example a compound of formula 1 wherein R1 is optionally substituted phenyl or optionally substituted pyridyl; R2 (CH2)n wherein n is 1, 2, 3 or 4; R3 is CH3(CH2)m wherein m is 0, 1, 2 or 3; X1 is O, S, NH, N(CH3) or CH2; and X2 is O, S or NH; in particular 2-phenylethyl butyrate, and a thioamide or thiourea of formula 2 wherein R4 is optionally substituted phenyl, optionally substituted pyridyl, optionally substituted indolyl, —NR7R8; or —NH—N?CH—R9; and substituents R5 to R9 have the meanings indicated in the description, in particular ethionamide. The pharmaceutical composition is useful, e.g., in the treatment of multidrug-resistant tuberculosis.Type: ApplicationFiled: November 25, 2008Publication date: March 3, 2011Inventors: Martin Fussenegger, Wilfried Weber, Ronald Schoenmakers
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Patent number: 7893108Abstract: Disclosed herein are antiviral compounds, such as anti-human cytomegalovirus antiviral compounds, pharmaceutical compositions and antiviral methods.Type: GrantFiled: January 11, 2007Date of Patent: February 22, 2011Assignee: President and Fellows of Harvard CollegeInventors: Donald M. Coen, Arianna Loregian
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Publication number: 20100316655Abstract: Disclosed herein are drug compounds that have MDR-inverse activity and thus are effective against multidrug-resistant cells. Exemplary compounds disclosed herein have the structure: Examples of the disclosed compounds have been found to have, inter alia, efficacy in directly treating multidrug resistant cells, rendering multidrug resistant cells susceptible to other chemotherapeutics and in some instances reversing multidrug resistance.Type: ApplicationFiled: February 10, 2009Publication date: December 16, 2010Inventors: Matthew D. Hall, Michael M. Gottesman, Jennifer L. Hellawell, Joseph A. Ludwig, Henry M. Fales, Noeris K. Salam, Gergely Szakács
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Patent number: 7842728Abstract: The present invention provides a synergistic insecticidal composition comprising as essential active ingredients a neuronal sodium channel antagonist in combination with one or more compounds selected from the group consisting of pyrethroids, pyrethroid-type compounds, recombinant nucleopolyhedroviruses capable of expressing an insect toxin, organophosphates, carbamates, formamidines, macrocyclic lactones, amidinohydrazones, GABA antagonists and acetylcholine receptor ligands. Also provided are methods for synergistic insect control and crop protection.Type: GrantFiled: October 31, 2007Date of Patent: November 30, 2010Assignee: BASF AktiengesellschaftInventors: Michael Frank Treacy, Raymond Frank Borysewicz, Kurt Allen Schwinghammer, Paul E. Rensner, Hassan Oloumi-Sadeghi
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Publication number: 20100298340Abstract: This invention relates to novel compounds having the structural formula I below: and to their pharmaceutically acceptable salt, compositions and methods of use. These novel compounds provide a treatment or prophylaxis of cognitive impairment, Alzheimer Disease, neurodegeneration and dementia.Type: ApplicationFiled: April 12, 2007Publication date: November 25, 2010Applicants: AstraZeneca AB, Astex Therapeutics Ltd.Inventors: Stefan Berg, Karin Kolmodin
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Patent number: 7838559Abstract: The present invention provides a synergistic insecticidal composition comprising as essential active ingredients a neuronal sodium channel antagonist in combination with one or more compounds selected from the group consisting of pyrethroids, pyrethroid-type compounds, recombinant nucleopolyhedroviruses capable of expressing an insect toxin, organophosphates, carbamates, formamidines, macrocyclic lactones, amidinohydrazones, GABA antagonists and acetylcholine receptor ligands. Also provided are methods for synergistic insect control and crop protection.Type: GrantFiled: October 31, 2007Date of Patent: November 23, 2010Assignee: BASF AktiengesellschaftInventors: Michael Frank Treacy, Raymond Frank Borysewicz, Kurt Allen Schwinghammer, Paul E. Rensner, Hassan Oloumi-Sadeghi
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Patent number: 7820656Abstract: Disclosed is a medicament comprising N-aryl N? morpholino/piperidino thiocarbamide derivatives represented by the following formula 1 for preventing and treating diabetes, diabetic complications, insulin resistance and insulin resistance syndrome, and can be used in drugs, foods, and beverages inducing an effect of preventing and treating diabetes, diabetic complications, insulin resistance and insulin resistance syndrome of modern people who suffer from the increasing development of diabetes resulting from environmental factors, such as intake of westernized foods, obesity, and so on: wherein, X is O or C, and R represents 4-chlorophenyl, 2-methylphenyl, 3-methoxypheny, 3-methylphenyl, or phenyl group.Type: GrantFiled: December 22, 2005Date of Patent: October 26, 2010Inventor: Sung-Jin Kim
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Patent number: 7772281Abstract: The present invention provides a synergistic insecticidal composition comprising as essential active ingredients a neuronal sodium channel antagonist in combination with one or more compounds selected from the group consisting of pyrethroids, pyrethroid-type compounds, recombinant nucleopolyhedroviruses capable of expressing an insect toxin, organophosphates, carbamates, formamidines, macrocyclic lactones, amidinohydrazones, GABA antagonists and acetylcholine receptor ligands. Also provided are methods for synergistic insect control and crop protection.Type: GrantFiled: October 31, 2007Date of Patent: August 10, 2010Assignee: BASF AktiengesellschaftInventors: Michael Frank Treacy, Raymond Frank Borysewicz, Kurt Allen Schwinghammer, Paul E. Rensner, Hassan Oloumi-Sadeghi
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Patent number: 7772282Abstract: The present invention provides a synergistic insecticidal composition comprising as essential active ingredients a neuronal sodium channel antagonist in combination with one or more compounds selected from the group consisting of pyrethroids, pyrethroid-type compounds, recombinant nucleopolyhedroviruses capable of expressing an insect toxin, organophosphates, carbamates, formamidines, macrocyclic lactones, amidinohydrazones, GABA antagonists and acetylcholine receptor ligands. Also provided are methods for synergistic insect control and crop protection.Type: GrantFiled: October 31, 2007Date of Patent: August 10, 2010Assignee: BASF AktiengesellschaftInventors: Michael Frank Treacy, Raymond Frank Borysewicz, Kurt Allen Schwinghammer, Paul E. Rensner, Hassan Oloumi-Sadeghi
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Patent number: 7772283Abstract: The present invention provides a synergistic insecticidal composition comprising as essential active ingredients a neuronal sodium channel antagonist in combination with one or more compounds selected from the group consisting of pyrethroids, pyrethroid-type compounds, recombinant nucleopolyhedroviruses capable of expressing an insect toxin, organophosphates, carbamates, formamidines, macrocyclic lactones, amidinohydrazones, GABA antagonists and acetylcholine receptor ligands. Also provided are methods for synergistic insect control and crop protection.Type: GrantFiled: October 31, 2007Date of Patent: August 10, 2010Assignee: BASF AktiengesellschaftInventors: Michael Frank Treacy, Raymond Frank Borysewicz, Kurt Allen Schwinghammer, Paul E. Rensner, Hassan Oloumi-Sadeghi
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Publication number: 20090324580Abstract: The present invention relates to the use of inhibitors of scavenger receptor class proteins, in particular ScarB1 for the production of a medicament for treatment of and/or prophylaxis against infections, involving liver cells and/or hematopoietic cells, in particular malaria.Type: ApplicationFiled: March 9, 2007Publication date: December 31, 2009Applicants: CENIX BIOSCIENCE GMBH, INSTITUTO DE MEDICINA MOLECULAR , FACULDADE DE MEDICINA DA UNIVERSIDADA DE LISBOAInventors: Michael Hannus, Cecilie Martin, Maria M. Mota, Miguel Prudencio, Christina Dias Rodrigues
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Patent number: 6911460Abstract: The present invention relates to methods of treating viral or fungal infections using 3-aminopyridine-2-carboxyaldehyde thiosemicarbazone (3-AP) and 3-amino-4-methylpyridine-2-carboxaldehyde thiosemicarbazone (3-AMP) and its prodrug forms and to pharmaceutical compositions comprising these compounds.Type: GrantFiled: April 18, 2002Date of Patent: June 28, 2005Assignees: Vion Pharmaceuticals, Inc., Yale UniversityInventors: Ivan C. King, Terrance W. Doyle, Mario Sznol, Alan C. Sartorelli, Yung-Chi Cheng
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Publication number: 20040110730Abstract: Reagents and methods are provided for crosslinking and immobilizing biomolecules, drugs and synthetic polymers. The reagents possess (i) a thiol or amino reactive group; and (ii) a hydrazino or oxyamino moiety. Conjugates and immobilized biomolecules are also provided.Type: ApplicationFiled: November 24, 2003Publication date: June 10, 2004Inventor: David A. Schwartz
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Publication number: 20040058990Abstract: Invented are non-peptide TPO mimetics. also invented is a method of treating thrombocytopenia, in a mammal, including a human, in need thereof which comprises administering to such mammal an effective amount of a selected substituted thiosemicarbazone derivative.Type: ApplicationFiled: June 19, 2003Publication date: March 25, 2004Inventors: Kevin J. Duffy, Juan I Luengo, Stephen G. Miller, Julian Jenkins, Alan T. Price, Antony N. Shaw
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Publication number: 20030114531Abstract: Halogenated derivatives of two synthetic anti-tuberculosis agents, thioacetazone and p-aminosalicylic acid, have been synthesized.Type: ApplicationFiled: September 9, 2002Publication date: June 19, 2003Inventors: Farzad Kobarfard, Joel M. Kauffman
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Publication number: 20020173548Abstract: Halogenated derivatives of two synthetic anti-tuberculosis agents, thioacetazone and p-aminosalicylic acid, have been synthesized.Type: ApplicationFiled: March 9, 2001Publication date: November 21, 2002Inventors: Farzad Kobarfard, Joel M. Kauffman
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Publication number: 20020061886Abstract: This invention is related to carbocyclic and heterocyclic substituted semicarbazones and thiosemicarbazones represented by Formula I: 1Type: ApplicationFiled: December 6, 2001Publication date: May 23, 2002Applicant: CoCensys, Inc.Inventors: Yan Wang, Sui Xiong Cai, John FW Keana
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Patent number: 6323191Abstract: Cystic fibrosis transmembrane conductance regulator (CFTR) is a chloride (Cl−) channel regulated by phosphorylation and intracellular nucleotides. CFTR is the major Cl− transport pathway in airway epithelial cells. The abnormal transepithelial Cl− transport and subsequent defective fluid transport caused by CF is a result of the genetic mutations of the gene coding for the CFTR protein. The present invention is directed to the novel use of ionophores as artificial Cl− transport pathways into CF epithelia to treat the defective Cl− and fluid transport lonophores and in particular, small molecule ionophores, represent a potential novel means of treating CF. The invention also includes using an ionophore to generate chloride secretion on intact monolayers of airway epithelia cells and other epithelia cells by administering an ionophore to a mammal.Type: GrantFiled: June 17, 1999Date of Patent: November 27, 2001Assignee: Genzyme CorporationInventors: David J. Harris, Edward R. Lee, Canwen Jiang, Seng H. Cheng, Mathieu Lane
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Patent number: 6316467Abstract: Compounds of this invention increase plasma levels of high density lipoprotein or HDL, the “good” cholesterol and as such may be useful for treating diseases such as atherosclerosis.Type: GrantFiled: November 16, 1998Date of Patent: November 13, 2001Assignee: American Home Products CorporationInventor: Thomas J. Commons
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Patent number: 6207715Abstract: Compounds of the formula: are useful in the treatment of diseases associated with herpes viruses including human cytomegalovirus, herpes simplex viruses, Epstein-Barr virus, varicella-zoster virus, human herpesviruses-6 and -7, and Kaposi herpes virus.Type: GrantFiled: November 22, 1999Date of Patent: March 27, 2001Assignee: American Home Products CorporationInventors: Jonathan Bloom, Kevin Curran, Martin DiGrandi, Russell Dushin, Stanley Lang, Emily Norton, Adma Ross, Bryan O'Hara
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Patent number: 5571843Abstract: Therapeutic compounds having the formula: ##STR1## in which R.sub.2 and R.sub.3 independently denote H, C.sub.1 -C.sub.4 alkoxy or OH and (A, B)=(oxygen, oxygen) in which case one out of R and R.sub.1 denotes OH, halogen, secondary amino or tertiary amine and the other denotes NHNHCONHR.sub.4 or R and R.sub.1 together denote .dbd.N--NH--CX--NHR.sub.5, .dbd.N--NH--CX--N(phenyl).sub.2, .dbd.N--NH--CX--NH--NH--R.sub.5, .dbd.N--NH--C(SCH.sub.3).dbd.N--R.sub.6 or .dbd.N--N.dbd.C(SCH.sub.3)--NH--R.sub.6 ; or (A, B)=(N--OH, oxygen) in which case R and R.sub.1 together form .dbd.N--NH--CX--NHR.sub.5 or .dbd.N--NH--CX--N(phenyl).sub.2 ; or (A, B)=(N--NH--CX--NHR.sub.5, oxygen) in which case R and R.sub.1 together form .dbd.N--NH--CX--NHR.sub.5 ; or (A, B)=(N--OH, N--OH) in which case R and R.sub.1 together form .dbd.N--NH--CX--NHR.sub.5 or .dbd.N--NH--CX--N(phenyl).sub.2.Type: GrantFiled: March 24, 1994Date of Patent: November 5, 1996Assignee: InnotheraInventors: Michel P. Cugnon de Sevricourt, Catherine G. Dacquet, Michel A. Finet, Florence J. Le Marquer, Max F. Robba, Norbert O. Tembo, Sylvie J. Yannic-Arnoult, Jean-Luc Torregrosa
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Patent number: 5137877Abstract: The present invention provides novel N-substituted hydrazine bifunctional compounds, novel N-subhstituted hydrazone derivatives of a cytotoxic reagent incorporating the bifunctional compounds, novel conjugates containing at least one cytotoxic reagent molecule reacted with the bifunctional compound and bound to a molecule reactive with a target cell population, methods for their production, and pharmaceutical compositions and methods for delivering cytotoxic reagents to a target population of cells. The hydrazone bonds of the conjugates of the invention permit the release of free cytotoxic reagent from the conjugates in the acidic external or internal environment of the target cells. The bifunctional compounds, derivatives, conjugates and methods of the invention are useful in antibody-or ligand-mediated drug delivery systems for the perferential killing of a target cell population to treat diseases such as cancers, infections and autoimmune disorders.Type: GrantFiled: May 14, 1990Date of Patent: August 11, 1992Assignee: Bristol-Myers SquibbInventors: Takushi Kaneko, David Willner, Ivo Monkovic, Robert S. Greenfield, Gary R. Braslawsky
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Patent number: 5010104Abstract: Novel tricyclic compounds having a TXA.sub.2 -antagonizing activity represented by formul (I): ##STR1## which strongly antagonize an action of thromboxane A.sub.2 and are expected to have preventive and therapeutic effects on ischemica diseases, cerebro-vascular diseases, etc.Type: GrantFiled: June 29, 1989Date of Patent: April 23, 1991Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Etsuo Oshima, Hiroyuki Obase, Akira Karasawa, Kazuhiro Kubo, Ichiro Miki, Akio Ishii
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Patent number: 4882339Abstract: Disclosed are compounds of the formula ##STR1## wherein R.sub.1 represents unsubstituted or lower alkyl-substituted C.sub.3 -C.sub.7 -cycloalkyl, unsubstituted or lower alkyl substituted C.sub.7 -or C.sub.8 -bicycloalkyl, unsubstituted or lower alkyl-substituted adamantyl, 4-piperidinyl or N-lower alkyl or aryl-lower alkyl-substituted piperidinyl, 1- or 2-indanyl, 1- or 2-tetrahydronaphthyl, 1- or 2-perhydroindanyl, 1- or 2-perhydronaphthyl; R.sub.2 represents hydrogen, lower alkyl, C.sub.3 -C.sub.7 -cycloalkyl, aryl-lower alkyl, C.sub.3 -C.sub.7 -cycloalkyl-lower alkyl, lower alkanoyl or aryl-lower alkanoyl; or R.sub.1 and R.sub.2 combined with the nitrogen to which they are attached represent pyrrolidino, piperidino, perhydroazepino, morpholino, thiomorpholino, tetrahydro- or perhydro-(isoquinolinyl or quinolinyl), dihydro- or perhydroindolyl, piperazino or N-lower alkyl-piperazino; R.sub.Type: GrantFiled: July 10, 1987Date of Patent: November 21, 1989Assignee: Ciba-Geigy CorporationInventor: Jan W. F. Wasley
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Patent number: 4514419Abstract: Hydrazinecarboxamides and carbothioamides of the formula ##STR1## wherein R.sub.1 is selected from alkyl, cyanoalkyl, hydroxyalkyl, and benzyl, R.sub.2 is hydrogen or alkyl, Y is oxygen or sulfur, n is 0-5, and Z is substituted for hydrogen and independently selected from halogen, alkyl, alkoxy, phenoxy, trifluoromethyl, and nitro are useful as nematicides when applied to or incorporated into nematode-infested soil.Type: GrantFiled: May 18, 1983Date of Patent: April 30, 1985Assignees: FMC Corporation, Kanagawa Chemical Laboratory, Ltd.Inventors: Philip A. Cruickshank, Carmine P. DiSanzo, Kiyosi Kondo, Hiromichi Kono