Acyclic Nitrogen Bonded Directly To The Carbonyl Patents (Class 546/316)
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Publication number: 20120171730Abstract: Methods for the synthesis of N-substituted pyridinium compounds by using an N-heteroaryl substituted pyridinium salt (Zincke salt) and reacting it with a nucleophilic amine are provided. Novel purine-substituted pyridyl compounds, which may be useful reagents in the above reaction, are also disclosed.Type: ApplicationFiled: January 27, 2012Publication date: July 5, 2012Applicant: ROCHE DIAGNOSTICS OPERATIONS, INC.Inventors: Dieter Heindl, Heribert Maerz, Axel Schmidt
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Publication number: 20120149910Abstract: The object of the present invention is to provide novel carboxamides which exhibit an excellent pesticidal activity as pesticides. Disclosed are the carboxamides represented by the following Formula (I): wherein each substituent is as defined in the specification, and use thereof as pesticides and animal parasite controlling agents.Type: ApplicationFiled: August 3, 2010Publication date: June 14, 2012Applicant: Bayer CropScience AGInventors: Jun Mihara, Koichi Araki, Takuma Mori, Tetsuya Murata, Yasushi Yoneta, Yukiyoshi Watanabe, Eiichi Shimojo, Teruyuki Ichihara, Masashi Ataka, Katsuhiko Shibuya, Ulrich Gorgens
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Patent number: 8183289Abstract: Compounds of Formula (I): in which R1, R2, R7, R8, R9, R10 and A have the meanings given in the specification, are DP2 receptor modulators useful in the treatment of immunologic diseases.Type: GrantFiled: August 21, 2007Date of Patent: May 22, 2012Assignee: Array BioPharma Inc.Inventors: George Doherty, Adam Cook
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Publication number: 20120122935Abstract: The present invention relates to a method for treating or preventing necrotizing enterocolitis (NEC) in a human neonate in need thereof, comprising administering to the neonate a pharmaceutically effective amount of a composition comprising a poly(ADP-ribose) synthetase/polymerase (PARP) inhibitor. Also contemplated herein is an infant food or treatment composition comprising a PARP inhibitor in an amount that is 5 to 500 times greater than a daily recommended intake dosage for the PARP inhibitor.Type: ApplicationFiled: August 16, 2011Publication date: May 17, 2012Applicant: NATIONWIDE CHILDREN'S HOSPITAL, INC.Inventors: Peter J. Giannone, John A. Bauer
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Publication number: 20120115851Abstract: An objective of the present invention is to provide compounds that can effectively suppress the concentration of phosphorus in serum to effectively prevent or treat diseases induced by an increase in concentration of phosphate in serum. The compounds according to the present invention are compounds represented by formula (I) and pharmaceutically acceptable salts and solvates thereof: wherein A represents an optionally substituted five- to nine-membered unsaturated carbocyclic moiety or a five- to nine-membered unsaturated heterocyclic moiety, and represents a single bond or a double bond, R5 represents optionally substituted aryl or the like, Z represents —N?CHR6R7 or the like, R6 and R7 represent H, optionally substituted alkyl, optionally substituted aryl or the like, R101 and R102 together form ?O, and R103 and R104 represent H, or R101 and R104 together from a bond, and R102 and R103 together form a bond.Type: ApplicationFiled: January 18, 2012Publication date: May 10, 2012Applicant: KYOWA HAKKO KIRIN CO., LTD.Inventors: Nobuaki Eto, Rika Nagao, Tetsuko Kazama
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Publication number: 20120116090Abstract: 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 6, 2011Publication date: May 10, 2012Applicant: Intrexon CorporationInventors: Robert Eugene HORMANN, Bing Li
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Publication number: 20120108602Abstract: DGAT-1 inhibitor compounds of formula (1), pharmaceutically-acceptable salts and pro-drugs thereof are described, together with pharmaceutical compositions, processes for making them and their use in treating, for example, obesity wherein, for example, Ring A is optionally substituted 2,6-pyrazindiyl; X is ?0; Ring B is optionally substituted 1,4-phenylene; Y1 is a direct bond or —O—; Y2 is —(CH2)r— wherein r is 2 or 3; n is 0 or n is 1 when Y1 is a direct bond between Ring B and Ring C and when Ring B is 1,4-phenylene and Ring C is (4-6C)cycloalkane; Ring C is optionally substituted (4-6C)cycloalkane, (7-10C)bicycloalkane, (8-12C)tricycloalkane, phenylene or pryidindiyl; L is a direct bond or —O—; p is 0, 1 or 2 and when p is 1 or 2 RA1 and RA2 are each independently hydrogen or (1-4C)alkyl; Z is carboxy or a mimic or bioisostere thereof.Type: ApplicationFiled: May 5, 2011Publication date: May 3, 2012Applicant: AstraZeneca ABInventors: Udo Andreas BAUER, Jonas Gunnar BARLIND, Petra JOHANNESSON, Jan Magnus JOHANSSON, Alexander Tobias NOESKE, Annika Ulrika PETERSSON, Alan Martin BIRCH, Roger John BUTLIN, Clive GREEN, Andrew LEACH, Ragnar HOVLAND
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Publication number: 20120107902Abstract: The disclosure relates to methods for producing amide bonds and reagents related thereto. In some embodiments, the disclosure relates to methods of producing an amide comprising mixing an O-silylated thionoester and an amine under conditions such that an amide is formed. In another embodiment, the disclosure relates to mixing a thiolacid, a silylating agent, and an amine under conditions such that an amide is formed.Type: ApplicationFiled: October 25, 2011Publication date: May 3, 2012Applicant: EMORY UNIVERSITYInventors: Lanny S. Liebeskind, Wenting Wu, Zhihui Zhang, Hao Li, Angus A. Lamar
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Publication number: 20120095042Abstract: Provided are compounds of formula (I) wherein m is 0, 1 or 2; RI is a mono- or bicyclic heterocyclic ring system including one, two or three heteroatoms selected from nitrogen, sulphur and oxygen; R2 is selected from hydrogen, methyl and ethyl; I) R3 is hydrogen, methyl, or ethyl; and R4 and R5 are independently selected from ethyl and isopropyl; and R3, R4 and R5 together have at least 6 carbon atoms: or II) any two or all of R3, R4 and R5 form together with the carbon atom to which they are attached 3-para-menthyl, bornyl, or adamantyl; having cooling properties, their use as cooling agent and compositions including them.Type: ApplicationFiled: May 4, 2010Publication date: April 19, 2012Inventor: Stefan Michael Furrer
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Publication number: 20120095238Abstract: The invention relates to a continuous method for producing amides of aromatic carboxylic acids by reacting at least one carbonic acid ester of formula (I) R3—OOOR4, wherein R3 represents an optionally substituted aromatic hydrocarbon group with 5 to 100 carbon atoms and R4 represents a hydrocarbon group with 1 to 30 carbon atoms, with at least one amine of formula (II) HNR1R2, wherein R1 and R2 independently represent hydrogen or a hydrocarbon group with 1 to 100 C atoms, in a reaction tube the longitudinal axis of which extends in the direction of propagation of the microwaves of a monomode microwave applicator, under microwave irradiation to form carboxamide.Type: ApplicationFiled: June 9, 2010Publication date: April 19, 2012Applicant: CLARIANT FINANCE (BVI) LIMITEDInventors: Matthias Krull, Roman Morschhaeuser
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Patent number: 8158825Abstract: The present invention relates to a novel class of modified malonate derivatives. The modified malonate compounds can be used to treat cancer. The modified malonate compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.Type: GrantFiled: June 21, 2006Date of Patent: April 17, 2012Assignee: Merck Sharp & Dohme Corp.Inventors: Jonathan Grimm, Paul Harrington, Richard Heidebrecht, Jr., Thomas Miller, Karin Otte, Phieng Siliphaivanh, David Sloman, Matthew Stanton, Kevin Wilson, David Witter, Solomon Kattar, Paul Tempest
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Publication number: 20120088723Abstract: This invention provides a medicament for the treatment of cancer, which cause a reduction of cancer. This invention relates to use of a compound which has inhibitory activities against prostaglandin E2 receptor (EP4 receptor) and is represented by the following general formula (I), (II), (III), or (IV), or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition comprising the compound or the salt for the manufacture of a medicament for the treatment of cancer. The invention relates to a method for treatment of cancer comprising administering the compound or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition comprising the compound or the salt to humans or animals. The compound or a pharmaceutically acceptable salt thereof, or the pharmaceutical composition may be used in combination with one or more second active agents.Type: ApplicationFiled: April 22, 2010Publication date: April 12, 2012Applicant: RAQUALIA PHARMA INC.Inventors: Yukinori Take, Shinichi Koizumi, Takako Okumura, Kazuhiko Nonomura
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Patent number: 8143410Abstract: The present invention relates to drug delivery systems comprising ocular implant, which include organic molecules, capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation, in combination with a polymer, which polymer serves to control, modify, modulate and/or slow the release of the therapeutic component into the environment of the eye in which said composite is placed.Type: GrantFiled: January 5, 2009Date of Patent: March 27, 2012Assignee: Allergan, Inc.Inventors: Lon T. Spada, Jane Guo Shiah, Patrick Hughes, Thomas C. Malone, Gerald W. Devries, Jeffrey L. Edelman, Julie A. Wurster
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Patent number: 8129538Abstract: The invention relates to compounds having the formula: wherein the variables are as defined herein. The invention further relates to methods of making and using these compounds, and pharmaceutical compositions, kits and articles of manufacture comprise the compounds.Type: GrantFiled: March 26, 2008Date of Patent: March 6, 2012Assignee: Takeda Pharmaceutical Company LimitedInventors: Walter Keung, Zhe Li
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Publication number: 20120053300Abstract: The invention relates to functionalized polysulfide silica coupling agents and silica reinforced rubber compositions. Such rubber composition may be used, for example, for tire components such as, for example, tire treads.Type: ApplicationFiled: July 6, 2011Publication date: March 1, 2012Inventors: Junling Zhao, Michael Joseph Rachita
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Patent number: 8101774Abstract: The present invention relates to an ester represented by the formula [1]: or its pharmaceutically acceptable salt, or use of the same. The compound represented by the formula [1] or its pharmaceutically acceptable salt is useful as an agent for the treatment or prophylaxis of hyperlipidemia or the like, since it disappears very rapidly in the living body and has an excellent MTP inhibitory activity.Type: GrantFiled: October 17, 2005Date of Patent: January 24, 2012Assignee: Japan Tobacco Inc.Inventors: Atsushi Hagiwara, Taku Ikenogami, Kazunori Kurihara, Toshio Taniguchi, Mitsuru Takahashi, Akio Iida
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Publication number: 20110306542Abstract: Compounds that bind the glucagon-like peptide 1 receptor (GLP-1) receptor are provided including compounds which are modulators of the GLP-1 receptors and compounds which are capable of inducing a stabilizing effect on the receptor for use in structural analyses of the GLP-1 receptor. Methods of synthesis, methods of therapeutic and/or prophylactic use, and methods of use in stabilizing GLP-1 receptor in vitro for crystallization of the GLP-1 receptor of such compounds are provided.Type: ApplicationFiled: June 9, 2011Publication date: December 15, 2011Applicant: Receptos, Inc.Inventors: Marcus F. Boehm, Esther Martinborough, Manisha Moorjani, Liming Huang, Junko Tamiya, Mark T. Griffith, Thomas Fowler, Andrew Novak, Michael Knaggs, Premji Meghani
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Publication number: 20110306597Abstract: The present invention relates to compounds of the formula (I) and pharmaceutically acceptable salts and solvates thereof, wherein the substituents are defined herein, to compositions containing such compounds and to the uses of such compounds for the treatment of allergic and respiratory conditions.Type: ApplicationFiled: June 12, 2009Publication date: December 15, 2011Inventors: James Michael Crawforth, Paul Alan Glossop, Bruce Cameron Hamper, Wei Huang, Bradley Elwood Neal, Simon John Mantell, Kirk Olson, Atli Thorarensen, Steve Ronald Turner
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Publication number: 20110294793Abstract: The present invention provides compound of Formula (I): or a stereoisomer, tautomer, salt or solvate thereof, wherein the variables are defined herein. The compounds of formula (I) are inhibitors of Bcl-2 family antiapoptotic proteins, compositions containing the compounds and methods of treating diseases using the compounds.Type: ApplicationFiled: June 8, 2009Publication date: December 1, 2011Inventors: kyoung S Kim, Robert M. Borzilleri, Zhen-Wei Cai, Kap-Sun Yeung
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Publication number: 20110294858Abstract: In one aspect, the invention relates to substituted 6-methylnicotinamide analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.Type: ApplicationFiled: May 24, 2011Publication date: December 1, 2011Inventors: P. Jeffrey Conn, Craig W. Lindsley, Shaun R. Stauffer, Ya Zhou, Jason Manka, Gregor McDonald, José Manuel Bartolome-Nebreda
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Patent number: 8067638Abstract: The present invention is to provide a compound represented by the general formula (1) exhibiting a high insecticidal effect and an insecticide comprising the compound as an active ingredient. The compound represented by the general formula (1) and an insecticide comprising the compound as an active ingredient, wherein, in the formula, A1, A2, A3 and A4 each represent a carbon atom or the like; R1 and R2 each represent a hydrogen atom or the like; G1 and G2 represent an oxygen atom or the like; Xs each represent a hydrogen atom, a halogen atom or the like; n represents an integer of 0 to 4; Q1 represents a substituted phenyl group, a substituted heterocyclic group or the like; Q2 represents a substituted phenyl group, a substituted heterocyclic group or the like.Type: GrantFiled: June 20, 2006Date of Patent: November 29, 2011Assignee: Mitsui Chemicals, Inc.Inventors: Akiyoshi Kai, Takeo Wakita, Hiroyuki Katsuta, Kei Yoshida, Hidetaka Tsukada, Yusuke Takahashi, Nobuyuki Kawahara, Michikazu Nomura, Hidenori Daido
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Publication number: 20110288076Abstract: This disclosure relates to sphingosine-1-phosphate (S1P) receptor antagonists, compositions comprising the S1P receptor antagonists and methods for using and processes for making the S1P receptor antagonists. In particularly, this disclosure relates to sphingosine-1-phosphate 1 (S1P1) receptor antagonists, compositions comprising the S1P1 receptor antagonist and methods for using the S1P1 receptor antagonist, such as in the treatment of cancer, and processes for making the S1P1 receptor antagonists.Type: ApplicationFiled: October 16, 2009Publication date: November 24, 2011Applicant: EXELIXIS, INC.Inventors: Mohamed Abdulkader Ibrahim, Joon Won Jeong, Henry William Beecroft Johnson, Patrick Kearney, James W. Leahy, Gary L. Lewis, Robin Tammie Noguchi, John M. Nuss
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Publication number: 20110275615Abstract: An amide of the formula I and its tautomeric forms, possible enantiomeric and diastereomeric forms, E and Z forms, and possible physiologically tolerated salts, in which the variables have the following meanings: A —(CH2)p—R1, where R1 can be pyrrolidine, morpholine, piperidine, —NR5R6 and and R5, R6 and R7 can, independently of one another, be hydrogen, C1-C4-alkyl, CH2Ph, Ph, CH2CH2Ph, it also being possible for the phenyl rings to be substituted by R6, and p can be 1 and 2, and B can be phenyl, pyridyl, pyrimidyl and pyridazyl, it also being possible for the rings to be substituted by up to 2 R8 radicals, and D can be a bond, —(CH2)m—, —CH?CH—, —C?C—, and R2 is chlorine, bromine, fluorine, C1-C6-alkyl, NHCO—C1-C4-alkyl, NHSO2—C1-C4-alkyl, NO2, —O—C1-C4-alkyl and NH2, and R3 is —C1-C6-alkyl, branched or unbranched, and which may also carry a phenyl ring, indolyl ring or cyclohexyl ring which is in turn substituted by a maximum of two R8 radicals, where R8 is hydrogen, C1-C4-alkyl, branched or unType: ApplicationFiled: October 29, 2010Publication date: November 10, 2011Inventors: Hans-Jörg Treiber, Monika Knopp, Wilfried Lubisch, Achim Moeller
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Publication number: 20110275797Abstract: An N-acyl anthranilic acid derivative represented by general formula (1) or a salt thereof is useful for prevention or treatment of diseases associated with excessive production of collagen. (In the formula, R1 represents a carboxyl group or the like; R2 represents a hydrogen atom or the like; R3 represents an optionally substituted aryl group or the like; X1 represents a carbonyl group; X2 represents a bonding hand; X3 represents a bonding hand; X4 represents a bonding hand or the like; and A represents an optionally substituted phenyl group or the like.Type: ApplicationFiled: January 29, 2010Publication date: November 10, 2011Applicant: Toyama Chemical Co., Ltd.Inventors: Junichi Yokotani, Arihiro Takatori, Yukie Tada, Minori Yanai, Hiroshi Kato, Yoichi Taniguchi, Chiharu Tanabe
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Publication number: 20110275603Abstract: The present invention provides dihydroorotate dehydrogenase inhibitors, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of diseases or disorders wherein the inhibition of Dihydroorotate dehydrogenase is known to show beneficial effect.Type: ApplicationFiled: May 5, 2011Publication date: November 10, 2011Applicants: Rhizen Pharmaceuticals SA, Incozen Therapeutics Pvt. Ltd.Inventors: Meyyappan MUTHUPPALANIAPPAN, Prashant K. BHAVAR, Srikant VISWANADHA, Swaroop Kumar V.S. VAKKALANKA, Gayatri S. MERIKAPUDI
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Publication number: 20110269722Abstract: The invention provides the compounds of formula (I) or pharmaceutically acceptable salts thereof. The invention also provides pharmaceutical compositions comprising one or more compounds of formula I or intermediates thereof and one more of pharmaceutically acceptable carriers, vehicles or diluents. The invention further provides methods of preparation and methods of use of prodrugs including NO-releasing prodrugs, double prodrugs and mutual prodrugs comprising the compounds of formula I.Type: ApplicationFiled: December 23, 2010Publication date: November 3, 2011Inventor: Apparao Satyam
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Publication number: 20110269709Abstract: The invention provides the compounds of formula (I) or pharmaceutically acceptable salts thereof. The invention also provides pharmaceutical compositions comprising one or more compounds of formula I or intermediates thereof and one more of pharmaceutically acceptable carriers, vehicles or diluents. The invention further provides methods of preparation and methods of use of prodrugs including NO-releasing prodrugs, double prodrugs and mutual prodrugs comprising the compounds of formula I.Type: ApplicationFiled: December 23, 2010Publication date: November 3, 2011Inventor: Apparao Satyam
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Patent number: 8049037Abstract: This invention provides compounds as shown below, in which either all of Z1-6 are carbon or one of Z1-6 is nitrogen and the rest are carbon, and in which other substituents are defined herein, which are sphingosine-1-phosphate antagonists.Type: GrantFiled: August 12, 2009Date of Patent: November 1, 2011Assignee: Allergan, Inc.Inventors: Phong X. Nguyen, Todd M. Heidelbaugh, Ken Chow
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Publication number: 20110263626Abstract: The present invention relates to compounds of general formula I wherein n, R1, R2, R3, R4, R5, R6, R7 and R8 are defined as stated hereinafter, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with organic or inorganic acids or bases, which have valuable properties, the preparation thereof, the pharmaceutical compositions containing the pharmacologically effective compounds, the preparation thereof and the use thereof.Type: ApplicationFiled: August 28, 2008Publication date: October 27, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Norbert Hauel, Angelo Ceci, Enzo Cereda, Henri Doods, Ingo Konetzki, Juergen Mack, Henning Priepke, Annette Schuler-metz, Rainer Walter
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Publication number: 20110263659Abstract: The present invention is directed to derivatives and analogs of 1-methyl-nicotinamide useful for elevating the blood levels of 1-methylnicotinamide or deuterated species in a subject.Type: ApplicationFiled: May 5, 2009Publication date: October 27, 2011Applicant: Cortria CorporationInventor: Alexander Krantz
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Publication number: 20110262025Abstract: Gene panels, biomarker panels and microarrays relating to lipid formation in stratum corneum of human skin as a function of extrinsic and/or intrinsic aging conditions, and methods for assessing the age status of human skin, methods for identifying or evaluating an agent as effective for improving stratum corneum barrier maintenance and/or repair properties in aged skin, and cosmetic composition comprising the identified agents are all provided.Type: ApplicationFiled: February 7, 2011Publication date: October 27, 2011Inventors: Bradley Bryan Jarrold, Robert Lloyd Binder, Michael Keith Robinson, Leo Timothy Laughlin, II, Karen Marie Lammers
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Patent number: 8030336Abstract: A compound of the general formula (I) or pharmaceutically acceptable prodrugs, salts, hydrates, solvates, crystal forms or diastereomers thereof is described. A method of treating tyrosine kinase-associated disease states in a subject using a compound of formula (I) is also described.Type: GrantFiled: December 15, 2003Date of Patent: October 4, 2011Assignee: YM Biosciences Australia Pty LtdInventors: Christopher John Burns, Marcel Robert Kling
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Publication number: 20110224156Abstract: The invention relates to propionic acids, propionic acid esters, and related compounds, pharmaceutical compositions containing these compounds, and methods of using these compounds for the treatment of various diseases or conditions, including but not limited to diseases and/or conditions of Central Nervous System (CNS).Type: ApplicationFiled: March 8, 2011Publication date: September 15, 2011Inventors: Mark A. Wolf, Keith D. Barnes
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Patent number: 8008297Abstract: The present invention provides lysine based compounds of the formula; and when the compound of formula I comprises an amino group, pharmaceutically acceptable ammonium salts thereof, wherein R1 may be, for example, (HO)2P(O)—, (NaO)2P(O)—, alkyl-CO— or cycloalkyl-CO—, wherein X may be, for example, F, Cl, and Br, and wherein R2 and R3 are as defined herein.Type: GrantFiled: April 4, 2008Date of Patent: August 30, 2011Assignee: Ambrilia Biopharma Inc.Inventors: Brent Richard Stranix, Valerie Perron
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Publication number: 20110201603Abstract: The present invention relates to novel Acylaminobenzamide derivatives represented by the following formula (I) and use thereof as pesticides: wherein V represents an aromatic ring group of V1 to V5 described in the detailed description, Q represents an aromatic ring group of Q1 to Q7 described in the detailed description, G1 and G2 represent O or S, R1 represents hydrogen, alkyl, haloalkyl, alkoxy, haloalkoxy, phenyl or a heterocyclic group and R2 and R3 represent hydrogen, alkyl, haloalkyl, alkylcarbonyl, haloalkylcarbonyl, alkoxycarbonyl or haloalkoxycarbonyl.Type: ApplicationFiled: July 30, 2009Publication date: August 18, 2011Applicant: Bayer CropScience AGInventors: Jun Mihara, Tetsuya Murata, Kei Domon, Yukiyoshi Watanabe, Yasushi Yoneta, Takuma Mori, Eiichi Shimojo, Katsuhiko Shibuya, Teruyuki Ichihara, Masashi Ataka, Ulrich Görgens
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Publication number: 20110178102Abstract: Compounds are disclosed which inhibit SIR2 base exchange more than deacetylation, thus enhancing SIR2 deacetylation activity. Methods of using the compounds for enhancing SIR2 deacetylation activity and increasing longevity of an organism are also disclosed. Methods for screening for compounds that enhance SIR2 deacetylation activity and increase longevity of an organism are additionally disclosed.Type: ApplicationFiled: June 30, 2004Publication date: July 21, 2011Applicant: ALBERT EINSTEIN COLLEGE OF MEDICINE OF YESHIVA UNIVERSITYInventors: Vern L Schramm, Anthony A. Suave
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Publication number: 20110178104Abstract: The present invention provides compounds and methods for antagonizing the anticoagulant effect of an anticoagulant agent that is selected from UFH, LMWH, and a heparin/LMWH derivative in a patient comprising administering to the patient a compound of the invention or a salt thereof, or a composition comprising the same.Type: ApplicationFiled: January 5, 2011Publication date: July 21, 2011Applicant: POLYMEDIX INC.Inventors: Richard W. Scott, Dahui Liu, Robert W. Kavash, Trevor Young, Michael J. Costanzo, Carol Ann Mulrooney
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Patent number: 7977486Abstract: An electron donor-acceptor dyad is provided that can provide a charge-separated state with longevity and not only high oxidizing power but also high reducing power. A compound of the present invention is a quinolinium ion derivative represented by the following formula (I), a stereoisomer or tautomer thereof, or a salt thereof: where R1 is a hydrogen atom or an alkyl group, and Ar1 to Ar3 each are a hydrogen atom or an electron-donating group. The compound of the present invention has the above-mentioned structure and therefore can provide a charge-separated state with longevity and not only high oxidizing power but also high reducing power and can be used for various products such as photocatalysts, photosensitizers, dyes, oxidants, reductants, dye-sensitized solar cells, and organic EL devices.Type: GrantFiled: March 5, 2007Date of Patent: July 12, 2011Assignee: Osaka UniversityInventors: Shunichi Fukuzumi, Hiroaki Kotani, Kei Ohkubo
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Publication number: 20110158947Abstract: We disclose agents useful in the treatment of diseases or conditions that would benefit from improved muscle function and including pharmaceutical compositions and diagnostic tests for determining the predisposition of a subject, in particular a male subject, to cardiovascular disease.Type: ApplicationFiled: July 9, 2009Publication date: June 30, 2011Inventor: Aleksandar Jovanovic
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Patent number: 7964735Abstract: Novel 3-acylaminobenzanilides of the formula (I) wherein R1 represents phenyl which may be substituted or a 5-member or 6-member heterocyclic ring group, which may be substituted, containing at least one hetero-atom selected from the group consisting of N, O, and S; R2 represents halogen, C1-6 alkyl, or C1-6 haloalkyl; R3 represents C1-6 haloalkyl, C1-6 haloalkoxy, C1-6 haloalkylthio, C1-6 haloalkylsulfinyl, or C1-6 haloalkylsulfonyl; R4 represents halogen, C1-6 alkyl, or C1-6 haloalkyl; X represents halogen, C1-6 alkyl, or C1-6 haloalkyl; and n represents 0 or 1 and the compounds are used as insecticides, and a use of the new compounds as insecticides.Type: GrantFiled: July 21, 2006Date of Patent: June 21, 2011Assignee: Bayer Cropscience AGInventors: Akihiko Yanagi, Yukiyoshi Watanabe, Katsuaki Wada, Tetsuya Murata, Jun Mihara, Katsuhiko Shibuya, Eiichi Shimojo, Akira Emoto
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Publication number: 20110144052Abstract: The invention relates to prodrugs of niacin and their use in pharmaceutical composition and therapeutic treatment of disease.Type: ApplicationFiled: November 17, 2010Publication date: June 16, 2011Inventor: Roger Tung
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Publication number: 20110136831Abstract: An N-2-(hetero)arylethylcarboxamide derivative represented by the formula (I) wherein R1 and R2 are each independently a hydrogen atom etc., R3 and R4 are each independently a hydrogen atom etc., each Y is independently a halogen atom; a (C1-C6)alkyl group optionally substituted by halogen atom(s) etc., n is an integer of 1 to 5, A is a specific substituted cyclic group, E is C—H; C—Y (Y is as defined above); or a nitrogen atom, a salt thereof, and a pest controlling agent containing the derivative or salt as an active ingredient show superior performance as compared to the prior art technique, and are is useful particularly as plant disease controlling agents or nematocides having a broad control spectrum at a low dose.Type: ApplicationFiled: March 20, 2007Publication date: June 9, 2011Inventors: Masatsugu Oda, Yoshihiro Matsuzaki, Koji Tanaka, Eiji Takizawa, Motohiro Haseba, Nobutaka Kuroki, Akiyuki Suwa, Kenji Oshima
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Publication number: 20110136877Abstract: The present invention provides novel phenoxyacetic acids useful for the prevention and treatment of inflammatory disorders, including those affecting the respiratory system and skin.Type: ApplicationFiled: January 6, 2009Publication date: June 9, 2011Applicant: LIGAND PHARMACEUTICALS INC.Inventors: Brian F. McGuinness, Thuy X. H. Le, Jingqi Duo, Koc-Kan Ho
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Publication number: 20110136792Abstract: 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 metabolic diseases and disorders such as, for example, type II diabetes mellitus.Type: ApplicationFiled: October 20, 2010Publication date: June 9, 2011Inventors: David Robert Bolin, Stuart Hayden, Yimin Qian, Kshitij Chhabilbhai Thakkar
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Publication number: 20110105760Abstract: The present invention relates to a process for preparing substituted 2-aminobiphenyls and to a process for preparing (Het)arylamides of such 2-aminobiphenyls.Type: ApplicationFiled: July 3, 2009Publication date: May 5, 2011Applicant: BASF SEInventors: Michael Keil, Michael Rack, Thomas Zierke, Markus Heinrich, Alexander Wetzel
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Publication number: 20110105532Abstract: The present invention relates to halogen-substituted amide derivatives of the general formula (I) in which R1 to R6, Q1 to Q8, A, V, W, X, Y, n and m are each defined as described in the description—and to a process for preparation thereof and to the use thereof as insecticides and acaricides.Type: ApplicationFiled: October 27, 2010Publication date: May 5, 2011Applicant: Bayer CropScience AGInventors: Markus HEIL, Eike Kevin Heilmann, Alexander Sudau, Tobias Kapferer, Friedrich August Mühlthau, Peter Jeschke, Arnd Voerste, Ulrich Görgens, Klaus Raming, Ulrich Ebbinghaus-Kintscher, Mark Drewes, Martin Adamczewski, Angela Becker
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Publication number: 20110092695Abstract: A method of generating a chronic myelogenic leukemia (CML) acquired chemoresistant culture model is provided. Such a method may comprise providing a naïve blast crisis CML cell line; administering/contacting the cell line with a mutation-inducing dose of imatinib; maintaining a culture of the treated cell line for a period of time until the treated cell line relapses and repopulates the culture; and determining the repopulated cell culture is a CML acquired chemoresistant cell line by detecting a BCR-ABL mutation, wherein the acquired chemoresistance is achieved by a BCR-ABL mutation.Type: ApplicationFiled: October 8, 2010Publication date: April 21, 2011Inventors: WenYong Chen, Ravi Bhatia, Leila Su, Yate-Ching Yuan
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Publication number: 20110092536Abstract: The invention relates to bi-substrate inhibitor molecules associating (i) a pyridine, pyridinium or dihydropyridine-type structure allied to active metabolites of isoniazide, or related structures, and (ii) a hydrophobic substituent. The invention also relates to the method for producing said molecules, to the pharmaceutical compositions containing said molecules, and to the use thereof as inhibitors of enoyl reductase for the preparation of a medicament, especially an anti-infectious medicament for the treatment of tuberculosis.Type: ApplicationFiled: February 6, 2009Publication date: April 21, 2011Applicants: CENTRE NATIONAL DE LA RECHERCHE SCIENTIFOQUE (C.N., UNIVERSITE PAUL SABATIER TOULOUSE IIIInventors: Jean Bernadou, Vania Bernardes-Genisson, Tamara Delaine, Annaïck Quemard
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Patent number: 7928137Abstract: Compounds of formula I in which R1, R2, R3, each X, L, Y, Cy, Lp, D and n have the meanings as set out in the specification, and corresponding compounds in which the unsubstituted or substituted amidine group is replaced with an unsubstituted or substituted aminomethyl group, are useful as serine protease inhibitors.Type: GrantFiled: March 2, 2007Date of Patent: April 19, 2011Assignee: Tularik LimitedInventors: John Walter Liebeschuetz, William Alexander Wylie, Bohdan Waszkowycz, Christopher William Murray, Andrew David Rimmer, Pauline Mary Welsh, Stuart Donald Jones, Jonathan Michael Ernest Roscoe, Stephen Clinton Young, Phillip John Morgan
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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