R Contains Benzene Ring Patents (Class 514/615)
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Patent number: 7666444Abstract: There is provided an improved antiparasitic composition comprising an antiparasitically effective amount of an organic amine salt of closantel optionally a macrocyclic lactone and a non-irritating solvent system consisting essentially of an alcohol and a glycol derivative. Also provided are a method for obtaining increased levels of closantel in the blood of a homeothermic animal and a method for the enhanced protection of said animal from parasitic infection.Type: GrantFiled: January 14, 2005Date of Patent: February 23, 2010Assignee: WyethInventor: Robert Bruce Albright
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Publication number: 20100029773Abstract: The present invention relates to a method of identifying a compound for inhibiting aggregation of proteins involved in diseases linked to protein aggregation and/or neurodegenerative diseases, comprising the steps of: (a) bringing into contact a labeled monomeric protein and a differently labeled aggregate of said protein in the (1) presence and (2) absence of a candidate inhibitor of aggregation, (b) determining the amount of co-localized labels, representing the extent of binding of the monomeric proteins to the aggregates of said protein; and (c) comparing the result obtained in the presence and absence of said compound, wherein a decrease of co-localized labels in the presence of said compound is indicative of the compound's ability to inhibit aggregation of said protein. Moreover, the present invention relates to a pharmaceutical composition containing said inhibitor of aggregation as well as to a kit.Type: ApplicationFiled: May 24, 2005Publication date: February 4, 2010Applicants: LUDWIG-MAXIMILIANS-UNIVERSITAT MUNCHEN, MAX-PLANCK-GESELLSCHAFT FUR FORDERUNG DER WISSENSCHAFTEN E.V.Inventors: Uwe Bertsch, Armin Giese, Hans Kretzschmar, Paul Tavan, Thomas Hirschberger, Jan Bieschke, Petra Weber, Konstanze F. Winklhofer, Jörg Tatzelt, Ulrich F. Hartl, Gerda Mitterregger-Kretzschmar, Tobias Johannes Högen
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Patent number: 7642289Abstract: The present invention relates to nitrooxyderivatives or salts thereof having the following general formula (I): R—NR1c—(K)k0—(B)b0—(C)c0—NO2??(I) wherein c0, b0 and k0 are 0 or 1; R is the radical of an analgesic drug for chronic pain, for instance neurophatic pain; R1c is H or alkyl with from 1 to 5 carbon atoms; B is such that its precursor is selected from amino acids, hydroxy acids, polyalcohol, compounds; C is a bivalent radical containing an aliphatic, heterocyclic or aromatic radical.Type: GrantFiled: December 3, 2003Date of Patent: January 5, 2010Assignee: Nicox S.A.Inventors: Ennio Ongini, Nicoletta Almirante, Piero Del Soldata
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Publication number: 20090281191Abstract: Use of a ERR? agonist Or pharmaceutically acceptable salt thereof, for the prevention, delay of progression or the treatment of diabetes, insulin resistance, metabolic disease/metabolic syndrome, dyslipdemia, obesity, overweight, Neurodegenerative diseases such as Parkinson's disease. Alzheimer's disease, Huntington's disease or improvement of exercise endurance capacity.Type: ApplicationFiled: May 2, 2007Publication date: November 12, 2009Inventors: Shamina M. Rangwala, Susan C. Stevenson, Zhidan Wu
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Publication number: 20090246293Abstract: The present invention relates to compounds and the use of such compounds for increasing the efficacy of fungicides for controlling oomycete pathogen induced disease or diseases in one or more plants.Type: ApplicationFiled: April 1, 2009Publication date: October 1, 2009Applicant: Dow AgroSciences LLCInventors: Robert J. Ehr, Norman R. Pearson, Ronald Ross, JR., Christian Schobert
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Publication number: 20090221712Abstract: Novel mandelic hydrazides of the formula (I), in which R1-R11 have the meanings indicated in claim 1, are SGK inhibitors and can be used for the treatment of SGK-induced diseases and complaints, such as diabetes, obesity, metabolic syndrome (dyslipidaemia), systemic and pulmonary hypertonia, cardiovascular diseases and kidney diseases, generally in fibroses and inflammatory processes of any type.Type: ApplicationFiled: January 18, 2007Publication date: September 3, 2009Inventors: Rolf Gericke, Markus Klein, Werner Mederski, Norbert Beier, Florian Lang
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Patent number: 7563928Abstract: The present invention relates to non-steroidal ligands for use in nuclear receptor-based inducible gene expression system, and a method to modulate exogenous gene expression in which an ecdysone receptor complex comprising: a DNA binding domain; a ligand binding domain; a transactivation domain; and a ligand is contacted with a DNA construct comprising: the exogenous gene and a response element; wherein the exogenous gene is under the control of the response element and binding of the DNA binding domain to the response element in the presence of the ligand results in activation or suppression of the gene.Type: GrantFiled: August 20, 2007Date of Patent: July 21, 2009Assignee: Intrexon CorporationInventors: Robert Eugene Hormann, David W. Potter, Orestes Chortyk, Colin M. Tice, Glenn Richard Carlson, Andrew Meyer, Thomas R. Opie
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Patent number: 7544838Abstract: Estrogen-Related Receptor (ERR) modulating compounds and methods for synthesis of said compounds are described.Type: GrantFiled: January 20, 2006Date of Patent: June 9, 2009Assignee: City of HopeInventors: Barry Forman, Donna Yu
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Publication number: 20090137682Abstract: A method of treating a subject with cancer includes the step of co-administering to the subject over three to five weeks, a taxane in an amount of between about 243 ?mol/m2 to 315 ?mol/m2 (e.g., equivalent to paclitaxel in about 210-270 mg/m2); and a bis(thiohydrazide amide) in an amount between about 1473 ?mol/m2 and about 1722 ?mol/m2 (e.g., Compound (1) in about 590-690 mg/m2). The bis(thiohydrazide amide) is represented by Structural Formula (I), Y is a covalent bond or an optionally substituted straight chained hydrocarbyl group, or, Y, taken together with both >C=Z groups to which it is bonded, is an optionally substituted aromatic group. R1-R4 are independently —H, an optionally substituted aliphatic group, an optionally substituted aryl group, or R1 and R3 taken together with the carbon and nitrogen atoms to which they are bonded, and/or R2 and R4 taken together with the carbon and nitrogen atoms to which they are bonded, form a non-aromatic heterocyclic ring optionally fused to an aromatic ring.Type: ApplicationFiled: April 13, 2006Publication date: May 28, 2009Inventor: Thomas A Dahl
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Publication number: 20090104119Abstract: The present invention relates to novel therapeutic and diagnostic dendrimers. In particular, the present invention is directed to dendrimer based multifunctional compositions and systems for use in disease diagnosis and therapy (e.g., cancer diagnosis and therapy). The compositions and systems comprise one or more components for targeting, imaging, sensing, and/or providing a therapeutic or diagnostic material and monitoring the response to therapy of a cell or tissue (e.g., a tumor).Type: ApplicationFiled: August 25, 2005Publication date: April 23, 2009Inventors: Istvan J. Majoros, Thommey P. Thomas, James R. Baker, Zhengyi Cao, Jolanta F. Kukowska-Latallo
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Patent number: 7507767Abstract: There are disclosed compounds of the formula a prodrug thereof, or a pharmaceutically acceptable salt, solvate or stereoisomer of the compound or of said prodrug; which exhibit anti-inflammatory and immunodulatory activity. Also disclosed are pharmaceutical compositions containing said compounds and methods of using the compounds for the treatment of various diseases and conditions.Type: GrantFiled: February 6, 2002Date of Patent: March 24, 2009Assignee: Schering CorporationInventors: Joseph A. Kozlowski, Neng-Yang Shih, Brian J. Lavey, Razia K. Rizvi, Bandarpalle B. Shankar, James M. Spitler, Ling Tong, Ronald L. Wolin, Michael K. Wong
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Publication number: 20090054450Abstract: Disclosed herein are novel compositions and methods for treating or preventing a variety of disorders and conditions associated with lipid metabolism. The methods generally include administering to a patient in need thereof a therapeutically effective amount of a pharmaceutical composition comprising one or more fibric acid or statin derivative compositions alone or in combination with one or more lipid altering agents and/or PDE inhibitors.Type: ApplicationFiled: June 17, 2008Publication date: February 26, 2009Applicant: IRONWOOD PHARMACEUTICALS, INC.Inventors: Mark G. CURRIE, John Jeffrey TALLEY, Brian CALI
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Publication number: 20090048207Abstract: The invention provides compositions, pharmaceutical preparations and methods for inhibition of cystic fibrosis transmembrane conductance regulator protein (CFTR) that are useful for the study and treatment of CFTR-mediated diseases and conditions. The compositions and pharmaceutical preparations of the invention may comprise one or more hydrazide-containing compounds, and may additionally comprise one or more pharmaceutically acceptable carriers, excipients and/or adjuvants. The methods of the invention comprise, in certain embodiments, administering to a patient suffering from a CFTR-mediated disease or condition, an efficacious amount of a hydrazide-containing compound. In other embodiments the invention provides methods of inhibiting CFTR that comprise contacting cells in a subject with an effective amount of a hydrazide-containing compound.Type: ApplicationFiled: July 18, 2008Publication date: February 19, 2009Applicant: The Regents of the University of CaliforniaInventors: Alan Verkman, Nitin Dattatraya Sonawane, Chatchai Muanprasat
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Publication number: 20090036513Abstract: Compounds, methods and pharmaceutical compositions for treating viral infections, by administering certain novel compounds in therapeutically effective amounts are disclosed. Methods for preparing the compounds and methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment and prophylaxis of viral infections such as caused by hemorrhagic fever viruses is disclosed, i.e., including but not limited to, Arenaviridae (Junin, Machupo, Guanarito, Sabia, Lassa, Tacaribe, and Pichinde), Filoviridae (Ebola and Marburg viruses), Flaviviridae (yellow fever, Omsk hemorrhagic fever and Kyasanur Forest disease viruses), and Bunyaviridae (Rift Valley fever).Type: ApplicationFiled: March 2, 2007Publication date: February 5, 2009Applicant: SIGA TECHNOLOGIES, INC.Inventors: Dennis E. Hruby, Tove C. Bolken, Sean Amberg, Dongcheng Dai
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Patent number: 7485752Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as, for example, obesity, type II diabetes mellitus and metabolic syndrome.Type: GrantFiled: May 5, 2006Date of Patent: February 3, 2009Assignee: Hoffman-La Roche Inc.Inventor: Christophe Michoud
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Publication number: 20080306030Abstract: The present invention is directed to methods of enhancing insulin release, GLP-1 release, and insulin sensitivity, methods of increasing insulin gene expression, methods of decreasing gastric secretion and emptying and glucagons secretion, and methods of inhibiting food intake, and methods of treating diabetes mellitus, insulin resistance syndrome, hyperglycemia, and obesity comprising administering to a subject an effective amount of a TRPM5 inhibitor.Type: ApplicationFiled: February 4, 2008Publication date: December 11, 2008Applicant: Redpoint Bio CorporationInventors: S. Paul Lee, Peihong Zhou, M.N. Tulu Buber, Rok Cerne, Robert Bryant, F. Raymond Salemme, Gillian Morgan
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Publication number: 20080300205Abstract: The invention relates to methods and products for enhancing and improving recovery of lost memories. In particular the methods are accomplished through the increase of histone acetylation.Type: ApplicationFiled: November 30, 2007Publication date: December 4, 2008Applicants: Massachusetts Institute of Technology, President and Fellows of Harvard College, The General Hospital CorporationInventors: Li-Huei Tsai, Andre Fischer, Stephen Haggarty, Weiping Tang
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Publication number: 20080293711Abstract: The invention provides compounds of Formula (I) and pharmaceutical compositions comprising compounds of Formula (I). These compounds are useful treating or preventing HIV infections, and in treating proliferative disorders such as inhibiting the metastasis of various cancers.Type: ApplicationFiled: March 7, 2008Publication date: November 27, 2008Inventors: Michael P. Clark, Mark A. Lockwood, Florence F. Wagner, Michael G. Natchus, Brandon C. Doroh
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Publication number: 20080286264Abstract: The invention provides methods of identifying and making compounds that inhibit the interaction between MUC1 and either p53 or TBP. Also embraced by the invention are in vivo and in vitro methods of inhibiting such an interaction and of inhibiting the expression of MUC1 by a cell.Type: ApplicationFiled: February 14, 2006Publication date: November 20, 2008Applicant: DANA-FARBER CANCER INSTITUTE, INC.Inventor: Donald W. Kufe
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Publication number: 20080269206Abstract: The present invention relates to compositions and methods for treating a disease in an animal, which disease is responsive to inhibiting of functional cystic fibrosis transmembrane conductance regulator (CFTR) polypeptide by administering to a mammal in need thereof an effective amount of a compound defined herein (including those compounds set forth in Tables 1-6 or encompassed by formulas I-VI) or compositions thereof, thereby treating the disease. The present invention particularly, relates to a method of treating diarrhea and polycystic kidney disease.Type: ApplicationFiled: March 28, 2008Publication date: October 30, 2008Inventors: Michael Geoffrey Neil Russell, Huw David Vater, Jacqueline Anne Macritchie, Kevin James Doyle, David Brown, Joanne Peach
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Publication number: 20080262090Abstract: The invention relates to pharmaceutically acceptable salts of guanylhydrazone-containing compounds, for example, Semapimod. The invention also relates to pharmaceutically acceptable compositions comprising the salts and methods for their use.Type: ApplicationFiled: October 31, 2007Publication date: October 23, 2008Applicant: Cytokine PharmaSciences, Inc.Inventor: Thais M. Sielecki-Dzurdz
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Patent number: 7423057Abstract: The present invention relates to a novel compounds that can be used as anti-inflammatory, immunomodulatory and antiproliferatory agents. In particular, the invention refers to new compounds which inhibit dihydroorotate dehydrogenase (DHODH), a process for their manufacture, pharmaceutical compositions containing them and to their use for the treatment and prevention of diseases, in particular their use in diseases where there is an advantage in inhibiting dihydroorotate dehyrogenase (DHODH).Type: GrantFiled: February 17, 2006Date of Patent: September 9, 2008Assignee: 4SC AGInventors: Johan Leban, Bernd Kramer, Wael Saeb, Gabriel Garcia
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Publication number: 20080214674Abstract: Acylhydrazone derivatives of the formula (I) are SGK inhibitors and can be used for the treatment of SGK-induced diseases and conditions, such as diabetes, obesity, metabolic syndrome (dyslipidaemia), systemic and pulmonary hypertonia, cardiovascular diseases and renal diseases, generally in any type of fibrosis and inflammatory process. In which R1, R5 each, independently of one another, H, OH, OA, OAc or methyl, R2, R3, R4, R6, R7, R8, R9, R10 each, independently of one another, H, OH, OA, OAc, OCF3, Hal, NO2, CF3, A, CN, OSO2CH3, SO2CH3, NH2 or COOH, R11H or CH3, A alkyl having 1, 2, 3 or 4 C atoms, X CH2, CH2CH2, OCH2 or —CH(OH)—, Hal F, Cl, Br or I.Type: ApplicationFiled: April 10, 2008Publication date: September 4, 2008Inventors: Rolf Gericke, Norbert Beier, Oliver Poeschke, Lars Burgdorf, Helga Drosdat, Florian Lang
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Publication number: 20080194642Abstract: The present invention provides a topical, high-dose, long-acting ectoparasiticide composition, kit and method for protecting against ectoparasite infestations in a warm-blooded animal for a period of greater than about 6 weeks.Type: ApplicationFiled: February 8, 2008Publication date: August 14, 2008Applicant: WyethInventors: Robert Bruce Albright, Shobhan Shashikant Sabnis, Larry A. Kraft, Susan Joan Holzmer, Robert Alan Pollet, Ramune Marija Cobb
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Patent number: 7405239Abstract: The invention relates to acylhydrazone derivatives of formula (I), which are SGK inhibitors and can be used for the treatment of diseases and afflictions associated with SGK, such as diabetes, obesity, metabolic syndrome (dyslipidaemia), systematic and pulmonary hypertension, cardiovascular diseases and kidney diseases and in general for all types of fibroses and inflammatory processes. In said formula: R1 and R5 independently of one another represent H, OH, OA, OAc or methyl; R2, R3, R4, R6, R7, R8, R9 and R10 independently of one another represent H, OH, OA, OAc, OCF3, Hal, NO2, CF3, A, CN, OSO2CH3, SO2CH3, NH2, or COOH; R11 represents H or CH3; A represents an alkyl comprising 1, 2, 3, or 4 C atoms; X represents CH2, CH2CH2, OCH2 or —CH(OH)— and Hal represents F, Cl, Br or I.Type: GrantFiled: September 16, 2004Date of Patent: July 29, 2008Assignee: Merck Patent GmbHInventors: Rolf Gericke, Norbert Beier, Oliver Poeschke, Lars Burgdorf, Helga Drosdat, Florian Lang
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Patent number: 7399788Abstract: Disclosed is a series of N-deacetylthiocolchicine derivatives of formula (I) in which: the linker is a bivalent straight or branched C1-C8 alkyl residue, C3-C8 cycloalkyl, a phenylene or heterocyclic C4-C6 ring; the G1 and G2 junctions, which can be the same or different, are —CO—, —COHN—, —CR2— groups in which R2 is hydrogen or a straight C1-C4 alkyl residue, or the G1-linker-G2 group is the —CO— group. The compounds of formula (I) have antiproliferative, antinflammatory, antiarthritic and antiviral activity.Type: GrantFiled: February 1, 2005Date of Patent: July 15, 2008Assignee: Indena S.p.A.Inventors: Ezio Bombardelli, Gabriele Fontana
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Publication number: 20080167380Abstract: Novel acyl hydrazides of the formula (I), in which R1-R9 have the meanings indicated in claim 1, are SGK inhibitors and can be used for the treatment of SGK-induced diseases and complaints, such as diabetes, obesity, metabolic syndrome (dyslipidaemia), systemic and pulmonary hypertonia, cardiovascular diseases and renal diseases, generally in fibroses and inflammatory processes of any type.Type: ApplicationFiled: March 10, 2006Publication date: July 10, 2008Inventors: Rolf Gericke, Dieter Dorsch, Werner Mederski, Markus Klein, Norbert Beier, Florian Lang
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Publication number: 20080146445Abstract: The present invention concerns nematicidal compounds, their formulation as nematicidal composition and their use for controlling nematodes, preferably plant parasitic nematodes.Type: ApplicationFiled: December 16, 2005Publication date: June 19, 2008Applicant: Devgen NVInventors: Jan Octaaf De Kerpel, Dirk Leysen
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Publication number: 20080146670Abstract: The invention relates to pharmaceutically acceptable salts of guanylhydrazone-containing compounds, for example, Semapimod. The invention also relates to pharmaceutically acceptable compositions comprising the salts and methods for their use.Type: ApplicationFiled: June 22, 2007Publication date: June 19, 2008Applicant: Cytokine PharmaSciences, Inc.Inventor: THAIS M. SIELECKI-DZURDZ
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Publication number: 20080139585Abstract: The present application describes isoindoles and derivatives thereof, or pharmaceutically acceptable salt forms thereof, which are useful inhibitors of VEGFR.Type: ApplicationFiled: September 21, 2007Publication date: June 12, 2008Applicant: NOVA SOUTHEASTERN UNIVERSITYInventors: Appu Rathinavelu, Sivanesan Dakshanamurthy, Nagarajan Pattabiraman
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Patent number: 7368473Abstract: One embodiment of the present invention is a compound represented by the Structural Formula (I): Y is a covalent bond of a substituted or unsubstituted straight chained hydrocarbyl group. In addition, Y, taken together with both >C?Z groups to which it is bonded, is a substituted or unsubstituted aromatic group. Preferably, Y is a covalent bond or —C(R7R8)—. R1 is an aliphatic group, a substituted aliphatic group, a non-aromatic heterocyclic group, or a substituted non-aromatic heterocyclic group, R2-R4 are independently —H, an aliphatic group, a substituted aliphatic group, a non-aromatic heterocyclic group, a substituted non-aromatic heterocyclic group, an aryl group or a substituted aryl group, or R1 and R3 taken together with the carbon and nitrogen atoms to which they are bonded, and/or R2 and R4 taken together with the carbon and nitrogen atoms to which they are bonded, form a non-aromatic heterocyclic ring optionally fused to an aromatic ring.Type: GrantFiled: October 5, 2005Date of Patent: May 6, 2008Assignee: Synta Pharmaceuticals Corp.Inventors: Keizo Koya, Lijun Sun, Shoujun Chen, Noriaki Tatsuta, Yaming Wu, Mitsunori Ono, Zhi-Qiang Xia
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Patent number: 7345094Abstract: Disclosed is a compound represented by the Structural Formula (I): Y is a covalent bond, a phenylene group or a substituted or unsubstituted straight chained hydrocarbyl group. In addition, Y, taken together with both >C=Z groups to which it is bonded, is a substituted or unsubstituted aromatic group. Preferably, Y is a covalent bond or —C(R7R8)—. R1 and R2 are independently an aryl group or a substituted aryl group, R3 and R4 are independently —H, an aliphatic group, a substituted aliphatic group, an aryl group or a substituted aryl group. R5-R6 are independently —H, an aliphatic group, a substituted aliphatic group, an aryl group or a substituted aryl group. R7 and R8 are each independently —H, an aliphatic or substituted aliphatic group, or R7 is —H and R8 is a substituted or unsubstituted aryl group, or, R7 and R8, taken together, are a C2-C6 substituted or unsubstituted alkylene group. Z is ?O or ?S.Type: GrantFiled: October 5, 2005Date of Patent: March 18, 2008Assignee: Synta Pharmaceuticals Corp.Inventors: Keizo Koya, Lijun Sun, Shoujun Chen, Noriaki Tatsuta, Yaming Wu, Mitsunori Ono
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Patent number: 7317125Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as, for example, obesity, type II diabetes mellitus and metabolic syndrome.Type: GrantFiled: January 31, 2006Date of Patent: January 8, 2008Assignee: Hoffman-La Roche Inc.Inventors: David Robert Bolin, Christophe Michoud
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Patent number: 7288572Abstract: The present invention relates to novel insecticidally and acaricidally active compound combinations of N2-[1,1-dimethyl-2-(methylsulphonyl)ethyl]-3-iodo-N1-{2-methyl-4-[1,2,2,2-tetrafluoro-1-(trifluoromethyl)ethyl]phenyl}phthalamide of the formula (I) and active compounds identified in the disclosure.Type: GrantFiled: September 15, 2006Date of Patent: October 30, 2007Assignee: Bayer CropScience AGInventors: Jörg Konze, Wolfram Andersch, Dietrich Stübler, Rüdiger Fischer
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Patent number: 7241797Abstract: The invention relates generally to the use of pharmaceutical compositions to increase milk production alone or in combination with certain biological active ingredients. Specifically, the method relates to the use of pharmaceutical compositions that will act on the feedback of the intrinsic regulatory pathway in the mammalian mammary gland. The present invention provides for as a method of increasing bovine milk production as well as a method of correcting certain human lactation abnormalities. Preferably, the compounds used in the methods of the present invention are one or more active agents capable of inhibiting peripheral aromatic amino acid decarboxylase (AADC) enzymes, peripheral tryptophan hydroxylase (TPH) enzymes, peripheral serotonin (5-HT) enzymes, or a combination of enzymes thereof.Type: GrantFiled: January 22, 2003Date of Patent: July 10, 2007Assignee: University of CincinnatiInventor: Nelson D. Horseman
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Patent number: 7205001Abstract: The invention relates to the use of arsenic compounds to treat a variety of neoplastic diseases. The present invention encompasses the administration to a mammal of arsenic in the form of a salt, complex, organic compound or ionic solution to treat tumors of epithelial tissue, connective tissue, central nervous system, lymphoid tissue, hematopoietic cells and tumors associated with oncogenic viruses. This invention also encompasses the treatment of hematopoietic disorders in mammals by the administration of one or more arsenic compounds to said mammal. Further, the arsenic compounds may be used to treat metastatic neoplastic diseases.Type: GrantFiled: November 3, 2003Date of Patent: April 17, 2007Assignee: Polarx Biopharmaceuticals, Inc.Inventors: Ralph M. Ellison, Fred H. Marmelstein
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Patent number: 7176242Abstract: Disclosed are compounds of the formula wherein the variables RN, RC, R1, R25, R2, and R3 are as defined herein. These compounds have activity as inhibitors of beta-secretase and are therefore useful in treating a variety of discorders such as Alzheimer's Disease.Type: GrantFiled: November 8, 2002Date of Patent: February 13, 2007Assignees: Elan Pharmaceuticals, Inc., Pharmacia & Upjohn CompanyInventors: Varghese John, Michel Maillard, Barbara Jagodzinska, James Beck, Andrea Gailunas, John Freskos, John Mickelson, Lakshman Samala, Jennifer Sealy, Ruth TenBrink, Lawrence Fang, Roy Hom
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Patent number: 7176241Abstract: The present invention relates to novel compounds that can be used as antiinflammatory, immunomodulatory and antiproliferatory agents. In particular the invention refers to new compounds which inhibit dihydroorotate dehydrogenase (DHODH), a process for their manufacture, pharmaceutical compositions containing them and to their use for the treatment and prevention of diseases, in particular their use in diseases where there is an advantage in inhibiting dihydroorotate dehydrogenase (DHODH).Type: GrantFiled: July 9, 2002Date of Patent: February 13, 2007Assignee: 4SC AGInventors: Johan Leban, Bernd Kramer, Wael Saeb, Gabriel Garcia
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Patent number: 7173063Abstract: Methods for the treatment of a proliferative disorder are provided in which a subject in need of such treatment is administered an effective amount of a compound selected from: compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein X1 and X2 are independently H, Cl, F, Br, I, CN, CF3 or NO2, and Ar1 is a substituted or unsubstituted aryl or a substituted or unsubstituted heteroaryl; and compounds of formula (II) wherein X3 and X4 are each independently H, Cl, F, Br, I, CN, CF3 or NO2; Y is (C2–C6)alkylene or (C2–C6)heteroalkylene; and Z is Cl, F, Br, I, CN, CF3 or NO2.Type: GrantFiled: November 10, 2000Date of Patent: February 6, 2007Assignee: Fred Hutchinson Cancer Research CenterInventors: John R. Lamb, Julian Simon, Heather Dunstan, Stephen H. Friend
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Patent number: 7169816Abstract: Phenylamino benzhydroxamic acid derivatives of the formula where R1, R2, R3, R4, R5, and R6 are hydrogen or substituent groups such as alkyl, and where R7 is hydrogen or an organic radical, are potent inhibitors of MEK and, as such, are effective in treating cancer and other proliferative diseases such as psoriasis and restenosis.Type: GrantFiled: October 12, 2005Date of Patent: January 30, 2007Assignee: Warner-Lambert CompanyInventors: Stephen Douglas Barrett, Alexander James Bridges, Annette Marian Doherty, David Thomas Dudley, Alan Robert Saltiel, Haile Tecle
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Patent number: 7163703Abstract: The invention relates to the use of arsenic compounds to treat a variety of neoplastic diseases. The present invention encompasses the administration to a mammal of arsenic in the form of a salt, complex, organic compound or ionic solution to treat tumors of epithelial tissue, connective tissue, central nervous system, lymphoid tissue, hematopoietic cells and tumors associated with oncogenic viruses. This invention also encompasses the treatment of hematopoietic disorders in mammals by the administration of one or more arsenic compounds to said mammal. Further, the arsenic compounds may be used to treat metastatic neoplastic diseases.Type: GrantFiled: August 14, 2003Date of Patent: January 16, 2007Assignee: PolaRx Biopharmaceuticals, Inc.Inventors: Ralph M. Ellison, Fred H. Mermelstein
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Patent number: 7132116Abstract: The invention relates to the use of arsenic compounds to treat a variety of neoplastic diseases. The present invention encompasses the administration to a mammal of arsenic in the form of a salt, complex, organic compound or ionic solution to treat tumors of epithelial tissue, connective tissue, central nervous system, lymphoid tissue, hematopoietic cells and tumors associated with oncogenic viruses. This invention also encompasses the treatment of hematopoietic disorders in mammals by the administration of one or more arsenic compounds to said mammal. Further, the arsenic compounds may be used to treat metastatic neoplastic diseases.Type: GrantFiled: August 14, 2003Date of Patent: November 7, 2006Assignee: PolaRx Biopharmaceuticals Inc.Inventors: Ralph M. Ellison, Fred H. Mermelstein
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Patent number: 7081473Abstract: The present invention provides a low-molecular inhibitor of GIP functions and, further, an agent for preventing/ameliorating obesity based on inhibition of GIP functions, which comprises, as an active ingredient, a compound represented by the following general formula (I): (wherein R1 represents hydrogen, halogen, a nitro group or a cyano group, R2 and R3 each represent hydrogen or halogen, hydrogen or a methoxy group, or both R2 and R3 may form an optionally substituted benzene or pyrrole ring, and A represents nitrogen or C—R4 whereupon R4 represents hydrogen, an optionally substituted C1 to C6 alkyl group, —OR7, —NR8R9, —NHCO—R10 or —SO2—R11 or may, together with R3, form an optionally substituted benzene or pyrrole ring, R7, R8 and R9 each represent hydrogen or an optionally substituted C1 to C6 alkyl group, R10 represents a C1 to C6 alkyl group or the like, and R1 represents an optionally substituted morpholyl group or the like) or a pharmaceutically acceptable salt thereof.Type: GrantFiled: May 20, 2003Date of Patent: July 25, 2006Assignee: Sanwa Kagaku Kenkyusho Co., Ltd.Inventors: Yoshiharu Tsubamoto, Akira Tashita, Yukari Kobara, Takuji Kakigami
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Patent number: 7001759Abstract: Methods of introducing genetic material into cells of an individual and compositions and kits for practicing the same are disclosed. The methods comprise the steps of contacting cells of an individual with a polynucleotide function enhancer and administering to the cells, a nucleic acid molecule that is free of retroviral particles. The nucleic acid molecule comprises a nucleotide sequence that encodes a protein that comprises at least one epitope that is identical or substantially similar to an epitope of a pathogen antigen or an antigen associated with a hyperproliferative or autoimmune disease, a protein otherwise missing from the individual due to a missing, non-functional, or partially functioning gene, or a protein that produces a therapeutic effect on an individual. Methods of prophylactically and therapeutically immunizing an individual against pathogens are disclosed. Pharmaceutical compositions and kits for practicing methods of the present invention are disclosed.Type: GrantFiled: July 23, 1999Date of Patent: February 21, 2006Assignees: The Trustees of the University of Pennsylvania, The Wistar InstituteInventors: David B. Weiner, William V. Williams, Bin Wang
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Patent number: 6924312Abstract: Disclosed is a compound represented by the Structural Formula (I): Y is a covalent bond, a phenylene group or a substituted or unsubstituted straight chained hydrocarbyl group. In addition, Y, taken together with both >C?Z groups to which it is bonded, is a substituted or unsubstituted aromatic group. Preferably, Y is a covalent bond or —C(R7R8)—. R1 and R2 are independently an aryl group or a substituted aryl group, R3 and R4 are independently —H, an aliphatic group, a substituted aliphatic group, an aryl group or a substituted aryl group. R5-R6 are independently —H, an aliphatic group, a substituted aliphatic group, an aryl group or a substituted aryl group. R7 and R8 are each independently —H, an aliphatic or substituted aliphatic group, or R7 is —H and R8 is a substituted or unsubstituted aryl group, or, R7 and R8, taken together, are a C2-C6 substituted or unsubstituted alkylene group. Z is ?O or ?S.Type: GrantFiled: January 15, 2003Date of Patent: August 2, 2005Assignee: Synta Pharmaceuticals Corp.Inventors: Keizo Koya, Lijun Sun, Shoujun Chen, Noriaki Tatsuta, Yaming Wu, Mitsunori Ono
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Patent number: 6919090Abstract: The invention relates to novel active combinations of certain cyclic ketoenols and certain active compounds that together have unexpectedly good insecticidal and acaricidal properties.Type: GrantFiled: April 2, 2001Date of Patent: July 19, 2005Assignee: Bayer AktiengesellschaftInventors: Reiner Fischer, Christoph Erdelen, Thomas Bretschneider
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Patent number: 6906104Abstract: The present invention relates to compounds of formula (I): useful in treating Alzheimer's disease and other similar diseases. These compounds include inhibitors of the beta-secretase enzyme that are useful in the treatment of Alzheimer's disease and other diseases characterized by deposition of A beta peptide in a mammal. The compounds of the invention are useful in pharmaceutical compositions and methods of treatment to reduce A beta peptide formation.Type: GrantFiled: June 13, 2002Date of Patent: June 14, 2005Assignee: Pharmacia & Upjohn CompanyInventors: Heinrich Josef Schostarez, Robert Alan Chrusciel
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Patent number: 6887863Abstract: Compounds having the formula are methionine aminopeptidase type 2 (MetAP2) inhibitors and are useful for inhibiting angiogenesis. Also disclosed are MetAP2-inhibiting compositions and methods of inhibiting angiogenesis in a mammal.Type: GrantFiled: February 19, 2004Date of Patent: May 3, 2005Assignee: Abbott LaboratoriesInventors: Richard A. Craig, Megumi Kawai, Linda M. Lynch, Jyoti R. Patel, George S. Sheppard, Jieyi Wang, Fan Yang, Nwe Ba-Maung, Xenia Beebe Searle
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Patent number: 6875451Abstract: The invention relates to the use of arsenic compounds to treat a variety of neoplastic diseases. The present invention encompasses the administration to a mammal of arsenic in the form of a salt, complex, organic compound or ionic solution to treat tumors of epithelial tissue, connective tissue, central nervous system, lymphoid tissue, hematopoietic cells and tumors associated with oncogenic viruses. This invention also encompasses the treatment of hematopoietic disorders in mammals by the administration of one or more arsenic compounds to said mammal. Further, the arsenic compounds may be used to treat metastatic neoplastic diseases.Type: GrantFiled: October 15, 1998Date of Patent: April 5, 2005Assignee: PolaRx Biopharmaceuticals Inc.Inventors: Ralph M. Ellison, Fred H. Mermelstein
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Patent number: 6861448Abstract: Disclosed are compounds that inhibit the microbial NAD synthetase enzyme. For example, disclosed are compounds of the formula Ar1—X—Ar2—Y—L—Z—Q, wherein Q is Q1Ar3 or Ar3Q1; Ar1, Ar2, and Ar3 are independently aryl or heteroaryl, optionally substituted with one or more substituents; X, Y, and Z are independently selected from the group consisting of a covalent bond or groups containing one or more of C, H, N, O, S atoms; L is a linker and Q1 is an alkylenyl, alkylenyl carbonyloxy alkyl, or alkylenyl carbonylamino alkyl group, optionally having a substituent; a covalent bond; a group containing amidine or guanidine function wherein the amidine or guanidine may be optionally N-substituted with an alkyl; or a zwitterion; or a pharmaceutically acceptable salt thereof.Type: GrantFiled: February 22, 2002Date of Patent: March 1, 2005Assignees: Virtual Drug Development, Inc., The UAB Research FoundationInventors: Wayne J. Brouillette, Lawrence DeLucas, Christie Brouillette, Sadanandan E. Velu, Yong-Chul Kim, Liyuan Mou, R. Stephen Porter