Halogen, Bonded Directly To Carbon, Containing Patents (Class 564/442)
  • Publication number: 20150126511
    Abstract: The invention relates to novel cyclohexylamine derivatives and their use in the treatment and/or prevention of central nervous system (CNS) disorders, such as depression, anxiety, schizophrenia and sleep disorder as well as methods for their synthesis. The invention also relates to pharmaceutical compositions containing the compounds of the invention, as well as methods of inhibiting reuptake of endogenous monoamines, such as dopamine, serotonin and norepinephrine from the synaptic cleft and methods of modulating one or more monoamine transporter.
    Type: Application
    Filed: September 30, 2014
    Publication date: May 7, 2015
    Inventors: Liming SHAO, Fengjiang WANG, Scott Christopher MALCOLM, Michael Charles HEWITT, Larry R. BUSH, Jianguo MA, Mark A. VARNEY, Una CAMPBELL, Sharon Rae ENGEL, Larry Wendell HARDY, Patrick KOCH, John E. CAMPBELL
  • Publication number: 20150099720
    Abstract: Provided herein are compounds having a structure selected from among Formula (I), Formula (II), Formula (III), Formula (IV), Formula (V) and Formula (VI) that are androgen receptor modulators and/or androgen receptor binding agents. Also disclosed are methods of making and using such compounds, including, but not limited to, using such compounds for treating various conditions.
    Type: Application
    Filed: October 20, 2014
    Publication date: April 9, 2015
    Inventors: Lin Zhi, Robert I. Higuchi, E. Adam Kallel, Cornelis Arjan Van Oeveren, Jyun-Hung Chen, Daniel A. Ruppar, Bijan Pedram, Thomas Lot Stevens Lau, Todd A. Miller
  • Patent number: 8981156
    Abstract: This invention relates to methods, which provide access to [F-18]fluoropegylated (aryl/heteroaryl vinyl)-phenyl methyl amine derivatives.
    Type: Grant
    Filed: May 30, 2011
    Date of Patent: March 17, 2015
    Assignee: Piramal Imaging SA
    Inventors: Mathias Berndt, Matthias Friebe, Christina Hultsch, Fabrice Samson, Marianne Patt, Andreas Schildan, Christoph Smuda
  • Publication number: 20150057443
    Abstract: Cycloalkyl amine compounds of Formula (I), wherein ring A is C3-C6 cycloalkyl, optionally substituted with one or more C1-C3 alkyl, and R5 is ORS2, in which RS2 is H or C1-C6 alkyl, or R5 and R6, together with the carbon atom to which they are attached, form C?O, for use in treating CNS disorders, including movement disorders, depressive disorders, sleep disorders, cognitive dysfunctions, obesity, sexual dysfunction and substance abuse.
    Type: Application
    Filed: August 21, 2014
    Publication date: February 26, 2015
    Inventors: Philip Huxley, Jonathan R. Heal, Richard S. Todd
  • Publication number: 20150045548
    Abstract: The present invention relates to a method for labelling fluorine-18, which is a radioisotope, and more specifically, to a method for labelling a [18F]fluoride in a method for preparing an organic [18F]fluoro compound by reacting an alkyl halide or an alkyl sulfonate with a [18F]fluoride, wherein a [18F]fluoride supported on a quaternary alkyl ammonium polymer support is eluted using a solution containing a metal salt or a quaternary ammonium salt with an adjusted pH, and a base is not additionally used. The present invention enables a labeling reaction without an additional base after precisely reflecting the concentration of a base absolutely necessary for the nucleophilic substitution of a [18F]fluoride or eluting a [18F]fluoride using a [18F]fluoride eluent with an adjusted pH, thereby stably obtaining a [18F]fluoride-labelled compound in a high yield, and is thus useful for production of fluorine-18-labelled radioactive medical supplies.
    Type: Application
    Filed: December 21, 2012
    Publication date: February 12, 2015
    Inventors: Sang Ju Lee, Seung Jun Oh, Dae Hyuk Moon, Jin Sook Ryu, Jae Seung Kim, Jong Jin Lee
  • Publication number: 20150045213
    Abstract: Compounds of the formula (I), in which the substituents are as defined in claim 1, are suitable for use as nematicides.
    Type: Application
    Filed: March 6, 2013
    Publication date: February 12, 2015
    Inventors: Anthony Cornelis O'Sullivan, Olivier Loiseleur, Roman Staiger, Torsten Luksch, Thomas Pitterna
  • Publication number: 20150038574
    Abstract: Compounds and compositions are disclosed that are useful for treating ophthalmic conditions caused by or related to production of toxic visual cycle products that accumulate in the eye, such as dry adult macular degeneration, as well as conditions caused by or related to the misfolding of mutant opsin proteins and/or the mis-localization of opsin proteins. Compositions of these compounds alone or in combination with other therapeutic agents are also described, along with therapeutic methods of using such compounds and/or compositions. Methods of synthesizing such agents are also disclosed.
    Type: Application
    Filed: November 29, 2012
    Publication date: February 5, 2015
    Applicant: Bikam Pharmaceuticals, Inc.
    Inventors: David S. Garvey, Judd Berman, Tan Quach
  • Publication number: 20150018548
    Abstract: A process for producing N-methyl or N,N-dimethyl amines, which comprises using amine compound, nitro-containing compound or nitrile compound as a starting material, carbon dioxide as a methylating agent and hydrogen gas as a reducing agent, and allowing them to react in a sealed reactor for 6 to 48 h in a reaction medium at a reaction temperature of 80 to 180 ° C. in the presence of a composite catalyst, so as to provide N-methyl or N,N-dimethyl amines. The process of the present invention is simple and under relative mild reaction conditions. By means of the process of the invention, the target products can be prepared at low cost with a high yield. The catalysts used have a high catalytic activity and can be separated from the reaction system simply and reused. Furthermore, the whole process of the present invention is environmental-friendly and facilitates the cycling use of carbon dioxide.
    Type: Application
    Filed: September 27, 2013
    Publication date: January 15, 2015
    Applicant: Lanzhou Institute of Chemical Physics, Chinese Academy of Sciences
    Inventors: Feng SHI, Xinjiang Cui, Hangkong Yuan, Yan Zhang, Youquan Deng
  • Publication number: 20140350019
    Abstract: The present invention relates to aniline derivatives of formula (I), to their preparation and to their therapeutic application, for example in treating glaucoma: Formula (I), R1a represents H, an halogen, a (C1-C6)alkyl or a CN; R1b represents H, an halogen or a (C1-C6)alkyl; R1c represents H or a (C1-C6)alkyl; R2 represents H, an halogen, an OH, an O—(C1-C6)alkyl or (C1-C6)alkyl; R3 represents H, an halogen, a (C1-C6)alkyl, an OH, an O—(C1-C6)alkyl, a CONH2 or CN; R4 represents H, an halogen or a (C1-C6)alkyl; R5 represents H or F: R7 represents H or F; R8 represents H or F; R9 represents H or (C1-C6)alkyl, or one of its enantiomers.
    Type: Application
    Filed: September 7, 2012
    Publication date: November 27, 2014
    Applicant: FOVEA PHARMACEUTICALS
    Inventors: John Feutrill, Caroline Leriche, David Middlemiss
  • Publication number: 20140343315
    Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.
    Type: Application
    Filed: July 30, 2014
    Publication date: November 20, 2014
    Inventors: Sara Hadida-Ruah, Anna Hazlewood, Peter Grootenhuis, Fredrick Van Goor, Ashvani Singh, Jinglan Zhou, Jason McCartney
  • Patent number: 8877975
    Abstract: The invention relates to novel cyclohexylamine derivatives and their use in the treatment and/or prevention of central nervous system (CNS) disorders, such as depression, anxiety, schizophrenia and sleep disorder as well as methods for their synthesis. The invention also relates to pharmaceutical compositions containing the compounds of the invention, as well as methods of inhibiting reuptake of endogenous monoamines, such as dopamine, serotonin and norepinephrine from the synaptic cleft and methods of modulating one or more monoamine transporter.
    Type: Grant
    Filed: January 15, 2010
    Date of Patent: November 4, 2014
    Assignee: Sunovion Pharmaceuticals Inc.
    Inventors: Liming Shao, Fengjiang Wang, Scott Christopher Malcolm, Michael Charles Hewitt, Larry R. Bush, Jianguo Ma, Mark A. Varney, Una Campbell, Sharon Rae Engel, Larry Wendell Hardy, Patrick Koch, John E. Campbell
  • Publication number: 20140249161
    Abstract: Stilbene analogs and pharmaceutical compositions that are useful for the treatment of various cancers, including without limitation, colorectal cancer (CRC) and breast cancer are disclosed. The halogenated stilbene analogs include nitrogen heteroaryl groups and/or amino groups on the stilbene ring.
    Type: Application
    Filed: February 27, 2014
    Publication date: September 4, 2014
    Applicant: UNIVERSITY OF KENTUCKY RESEARCH FOUNDATION
    Inventors: David WATT, Chunming LIU, Vitaliy M. SVIRIPA, Wen ZHANG
  • Publication number: 20140228445
    Abstract: The present invention relates to alkyne derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
    Type: Application
    Filed: February 11, 2014
    Publication date: August 14, 2014
    Applicant: Allergan, Inc.
    Inventors: Wenkui K. Fang, Ken Chow, Evelyn G. Corpuz, Wha Bin Im
  • Publication number: 20140228588
    Abstract: An object of the present invention is to provide a novel fungicide having an excellent fungicidal activity. The compound used as the fungicide of the present invention is an ethynylphenylamidine compound or a salt thereof, the compound being represented by Formula (1): wherein R1 and R2 are each hydrogen or C1-12 alkyl, or R1 and R2 may be bonded together to form C1-7 alkylene; R3 is hydrogen or C1-4 alkylthio; R4, R5, R6, and R7 are each hydrogen, halogen, etc.; and R8 is hydrogen, C1-20 alkyl, C3-8 cycloalkyl, C1-4 haloalkyl, phenyl, a heterocyclic group, or —(CH2)n-Si(R9)(R10)(R11) wherein R9, R10, and R11 are each C1-6 alkyl, and n is an integer of 0 or 1.
    Type: Application
    Filed: April 15, 2014
    Publication date: August 14, 2014
    Applicant: OTSUKA AGRITECHNO CO., LTD.
    Inventors: Satoru Masumoto, Hitoshi Mutsutani, Sachi Kimura
  • Publication number: 20140163240
    Abstract: The present invention is concerned with novel processes for the preparation of (+)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane or a pharmaceutically acceptable salt thereof, and (?)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane or a pharmaceutically acceptable salt thereof. These compounds have pharmaceutical utility and are known to be useful for treating e.g., depression, anxiety disorders, eating disorders and urinary incontinence.
    Type: Application
    Filed: July 18, 2013
    Publication date: June 12, 2014
    Inventors: Jerry A. Murry, Edwin G. Corley, Feng Xu, Bryon Simmons
  • Publication number: 20140155431
    Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.
    Type: Application
    Filed: December 19, 2013
    Publication date: June 5, 2014
    Applicant: Vertex Pharmaceuticals Incorporated
    Inventors: Sara Hadida-Ruah, Anna Hazlewood, Peter Grootenhuis, Fredrick Van Goor, Ashvani Singh, Jinglan Zhou, Jason McCartney
  • Publication number: 20140142340
    Abstract: Novel fluoroacyl arylamines are disclosed.
    Type: Application
    Filed: November 21, 2012
    Publication date: May 22, 2014
    Applicant: XEROX CORPORATION
    Inventors: Adrien P. Cote, Richard A. Klenkler, Amanda L. Bongers, Gregory M. McGuire
  • Publication number: 20140121282
    Abstract: Phenyl-substituted cyclohexylamine derivatives and method for their synthesis and characterization are disclosed. Use of these compounds to treat/prevent neurological disorders as well as methods for their synthesis are set forth herein. Exemplary compounds of the invention inhibit reuptake of endogenous monoamines, such as dopamine, serotonin and norepinephrine (e.g., from the synaptic cleft) and modulate one or more monoamine transporter. Pharmaceutical formulations incorporating compounds of the invention are also provided.
    Type: Application
    Filed: January 7, 2014
    Publication date: May 1, 2014
    Applicant: Sunovion Pharmaceuticals Inc.
    Inventors: Liming SHAO, Fengjiang WANG, Scott Christopher MALCOLM, Michael Charles HEWITT, Jianguo MA, Seth RIBE, Mark A. VARNEY, Una CAMPBELL, Sharon Rae ENGEL, Larry Wendell HARDY, Patrick KOCH, Rudy SCHREIBER, Kerry L. SPEAR
  • Publication number: 20140121217
    Abstract: The invention relates to compounds of structural formula (I): or a pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof, wherein A, Y, L, R1, W1 and W2 are defined herein. These compounds are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.
    Type: Application
    Filed: January 2, 2014
    Publication date: May 1, 2014
    Applicant: Synta Pharmaceuticals Corp.
    Inventors: Shoujun Chen, Lijun Sun, Jun Jiang, Yu Xie
  • Publication number: 20140080916
    Abstract: Compounds that are central nervous system drug candidates for the treatment of cognitive decline and, more particularly, Alzheimer's disease are provided. Methods for treatment, inhibition, and/or abatement of cognitive decline and/or Alzheimer's disease with a compound or pharmaceutically acceptable salt of the invention are also provided. Also provided are methods of preparing the compounds/compositions of the invention.
    Type: Application
    Filed: February 1, 2012
    Publication date: March 20, 2014
    Applicant: Cognition Therapeutics, Inc.
    Inventors: Gilbert M. Rishton, Susan Catalano
  • Publication number: 20140066466
    Abstract: Described herein are compositions that inhibit the production of TNF? downstream of CD40 activation. As such, also described are various methods of using compositions exhibiting this activity for the treatment or prevention of inflammatory diseases associated with TNF? production or CD40 activation.
    Type: Application
    Filed: March 12, 2012
    Publication date: March 6, 2014
    Applicant: President and Fellows of Harvard College
    Inventor: Junying Yuan
  • Publication number: 20140039074
    Abstract: The invention generally relates to the preparation of 18F-labeled radiopharmaceuticals. In particular, this invention relates to the advanced processes for an efficient eiution of [18F]fluoride trapped in a cartridge filled with quaternary ammonium polymer which comprises inert non-basic and non-nucleophilic counter anions. The said methods and polymer cartridges allow the rapid preparation of suitable [18F]fluoride solution, which is also less basic to reduce the formation of byproducts, finally to increase radiochemical yield and purity of 18F-radiopharmaceuticals.
    Type: Application
    Filed: September 6, 2011
    Publication date: February 6, 2014
    Applicant: PIRAMAL IMAGING SA
    Inventors: Dae Yoon Chi, Byoung Se Lee, Sang Ju Lee, Jin-Sook Ryu, Seung Ju Oh
  • Publication number: 20140041062
    Abstract: The present disclosure relates to an ASD genetically engineered model carrying a deletion of Shank2 gene and having reduced NMDA receptor function. According to the present disclosure, genetically engineered mice that show the clinical features of ASD due to the deletion of the Shank2 gene can be obtained, and the genetically engineered mice can be effectively used to screen candidate therapeutic agents.
    Type: Application
    Filed: August 2, 2013
    Publication date: February 6, 2014
    Applicants: Industry-Academic Cooperation Foundation, Yonsei University, Korea Advanced Institute of Science and Technology, Seoul National University R&DB Foundation
    Inventors: Min Goo Lee, Bong Kiun Kaang, Eunjoon Kim
  • Publication number: 20140024679
    Abstract: The present invention provides novel phenylcycloalkylmethylamine derivatives, and methods of preparing phenylcycloalkylmethylamine derivatives. The present invention also provides methods of using phenylcycloalkylmethylamine derivatives and compositions of phenylcycloalkylmethylamine derivatives. The pharmaceutical compositions of the compounds of the present invention can be used for treating and/or preventing obesity and obesity related co-morbid indications and depression and depression related co-morbid indications.
    Type: Application
    Filed: December 31, 2012
    Publication date: January 23, 2014
    Applicant: Reviva Pharmaceuticals, Inc.
    Inventor: Reviva Pharmaceuticals, Inc.
  • Patent number: 8618327
    Abstract: The present invention relates generally to compounds providing antibacterial therapeutic agents and preparations, and related methods of using and making antibacterial compounds. Antibacterial compounds of the present invention include chalcone, alkylpyrimidine, aminopyrimidine and cyanopyridine compounds and derivatives thereof exhibiting minimum inhibitory concentrations (MIC) similar to or less than conventional antibacterial compounds in wide use. For example, the present invention provides chalcone and cyanopyridine compounds, and derivatives thereof, exhibiting high antibacterial activities having multiple electron withdrawing group substituents, such as halogens and fluorinated alkyl groups, and optionally having hydroxyl and/or alkoxyl groups substituents.
    Type: Grant
    Filed: July 6, 2012
    Date of Patent: December 31, 2013
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Helen E. Blackwell, Matthew D. Bowman, Jennifer C. O'Neill, Joseph R. Stringer
  • Publication number: 20130336890
    Abstract: This invention relates to novel compounds suitable as precursors for the preparation of certain 18F labelled positron emission tomography (PET) tracers. Furthermore the invention relates to the preparation of such precursor molecules and to the preparation of PET tracers by 18F labelling of such precursors.
    Type: Application
    Filed: October 17, 2011
    Publication date: December 19, 2013
    Applicant: PIRAMAL IMAGING SA
    Inventors: Andrea Thiele, Georg Kettschau, Tobias Heinrich, Lutz Lehmann, Christer Halldin, Sangram Nag, Andrea Varrone, Balazs Gulyas
  • Publication number: 20130338369
    Abstract: The present invention relates to a process for the synthesis of 2-aminobiphenylene and derivatives thereof by reacting a benzene diazonium salt with an aniline compound under basic reaction conditions.
    Type: Application
    Filed: March 6, 2012
    Publication date: December 19, 2013
    Applicant: BASF SE
    Inventors: Markus Heinrich, Gerald Pratsch
  • Patent number: 8604189
    Abstract: A simple, cost-effective process for preparation of efavirenz of formula (I) comprising reacting a solution of 5-chloro-?-(cyclopropylethynyl)-2-amino-?-trifluoromethyl) benzene methanol of formula (II) in an organic solvent with triphosgene in the presence of an inorganic base at a temperature range ?5° C. to 25° C., adding water and isolating compound of formula (I).
    Type: Grant
    Filed: May 27, 2009
    Date of Patent: December 10, 2013
    Assignee: Emcure Pharmaceuticals Limited
    Inventors: Mukund Keshav Gurjar, Abdulrakheeb Abdulsubhan Deshmukh, Sanjay Shankar Deshmukh, Satish Ramanial Mehta
  • Publication number: 20130225679
    Abstract: Provided are analgesic compounds, and salts thereof, of formula: (I) wherein A is: (A) Additionally, pharmaceutical formulations and methods of use employing the above compounds are provided.
    Type: Application
    Filed: January 13, 2012
    Publication date: August 29, 2013
    Applicant: ELI LILLY AND COMPANY
    Inventors: Jean Marie Defauw, Scott Dale Holmstrom, Shuhui Chen, Yang Zhang, Wentao Wu, Xian Peng, Yujuan Ma, Lun Lu
  • Publication number: 20130211142
    Abstract: Disclosed are halogenated diethyltoluenediamines of formula wherein either R1 is an amino group and R2 is chlorine or bromine, or R2 is an amino group and R1 is chlorine or bromine, and isomeric mixtures thereof. The halogenated diethyltoluenediamines of formula I are useful as chain extenders for polyurethanes and hardeners for epoxy resins having a relatively long gel time.
    Type: Application
    Filed: October 11, 2011
    Publication date: August 15, 2013
    Applicant: LONZA LTD.
    Inventors: Stefan Ellinger, Gaetano Ladelfa, Constanze Mueller
  • Publication number: 20130197013
    Abstract: The invention relates to cyclopropylamine compounds, in particular the compounds of Formula (I), and their use in therapy, including e.g. in the treatment or prevention of cancer, a neurological disease or condition, or viral infection.
    Type: Application
    Filed: July 27, 2011
    Publication date: August 1, 2013
    Inventors: Mathew Colin Thor Fyfe, Alberto Ortega Muñoz, Julio Castro-Palomino Laria, Marc Martinell Pedemonte, Maria de los Ángeles Estiarte-Martínez, Nuria Valls Vidal
  • Publication number: 20130190332
    Abstract: Compounds of formula (I) which are effective inhibitors of the Pi3K/Akt pathway, processes for their production and their use as pharmaceuticals.
    Type: Application
    Filed: July 7, 2011
    Publication date: July 25, 2013
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Stuart Ince, Andrea Hägebarth, Oliver Politz, Roland Neuhaus, Ulf Bömer, William Scott
  • Publication number: 20130172620
    Abstract: This invention relates to methods, which provide access to [F-18]fluoropegylated (aryl/heteroaryl vinyl)-phenyl methyl amine derivatives.
    Type: Application
    Filed: May 30, 2011
    Publication date: July 4, 2013
    Applicant: PIRAMAL IMAGING SA
    Inventors: Mathias Berndt, Matthias Friebe, Christina Hultsch, Fabrice Samson, Marianne Patt, Andreas Schildan, Christoph Smuda
  • Publication number: 20130165650
    Abstract: A process for the preparation of Efavirenz, (4S)-6-chloro-4-(cyclopropylethynyl)-4-(trifluoromethyl)-1,4-dihydro-2H-3,1-benzoxazin-2-one, of formula (I): comprising reacting the intermediate of formula (II): as a free base or a salt thereof, with diphosgene (TCMCF, trichloromethylchloroformate) Cl3CO—COCl in an organic solvent or in a biphasic medium comprised of an organic solvent and water, preferably but not mandatorily in the presence of a weak base in an amount sufficient to neutralize the reaction mixture or in an up to 30% molar excess of such amount.
    Type: Application
    Filed: February 26, 2013
    Publication date: June 27, 2013
    Applicant: F.I.S. Fabbrica Italiana Sintetici S.p.A
    Inventor: F.I.S. Fabbrica Italiana Sintetici S.p.A
  • Patent number: 8461390
    Abstract: A process for preparing substituted biphenyls of the formula I where R1=nitro or amino, R2=cyano, halogen, C1-C4-haloalkyl, C1-C4-haloalkoxy or C1-C4-haloalkylthio, n=from 0 to 3, and R3=hydrogen, cyano or halogen, which comprises reacting a halobenzene of the formula II in which Hal is chlorine or bromine, in the presence of a base and of a palladium catalyst which consists of palladium and a bidentate phosphorus ligand of the formula III where Ar is phenyl which is substituted if desired and R4 and R5 are each C1-C8-alkyl or C3-C6-cycloalkyl or together form a 2- to 7-membered bridge which may, if desired, bear a C1-C6-alkyl substituent, in a solvent or diluent, with a phenylboronic acid IVa a diphenylborinic acid IVb or a mixture of IVa and IVb.
    Type: Grant
    Filed: June 22, 2009
    Date of Patent: June 11, 2013
    Assignee: BASF SE
    Inventors: Sebastian Peer Smidt, Volker Maywald, Kathrin Wissel-Stoll, Joachim Schmidt-Leithoff, Ansgar Gereon Altenhoff, Michael Keil
  • Publication number: 20130137900
    Abstract: Disclosed is a novel method of preparing a secondary amine compound using a microflow reactor. According to the method, a primary amine compound and a halide compound are allowed to react with each other in the microflow reactor, such that the production of a tertiary amine compound or an ammonium salt is minimized, whereby the secondary amine compound is efficiently prepared.
    Type: Application
    Filed: February 1, 2011
    Publication date: May 30, 2013
    Applicant: UNIVERSITY-INDUSTRY COOPERATION GROUP OF KYUNGHEE UNIVERSITY
    Inventors: Jin-Hyun Jeong, Han-Seo Moon, Liu-Lan Shen, Yong-Sung Choi
  • Publication number: 20130090471
    Abstract: The present invention relates to a method for identifying compounds that modulate cholesterol metabolism by detecting enzyme activities involved in the synthesis or catabolism of cholesterol. Said method enables the lethal risk for mammalian cells when the cholesterol level decreases to be avoided, due to the use of genetically modified yeasts, the survival of which is not strictly dependent upon the cholesterol production.
    Type: Application
    Filed: June 9, 2011
    Publication date: April 11, 2013
    Applicant: SANOFI
    Inventors: Bruno Dumas, Isabelle Maury
  • Publication number: 20130079417
    Abstract: Highly selective 5-HT(2C) receptor agonists receptors are disclosed. The 5-HT(2C) receptor agonists are used in the treatments of disease and conditions wherein modulation of 5-HT(2C) receptors provides a benefit, such as obesity and psychiatric disorders.
    Type: Application
    Filed: February 3, 2011
    Publication date: March 28, 2013
    Applicants: THE UNIVERSITY OF NORTH CAROLINA AT CHAPEL HILL, THE BOARD OF TRUSTEES OF THE UNIVERSITY OF ILLINOIS
    Inventors: Alan Kozikowski, Bryan Roth, Andreas Svennebring, Gang Chen, Sung Jin Cho
  • Publication number: 20130035327
    Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.
    Type: Application
    Filed: October 8, 2012
    Publication date: February 7, 2013
    Inventors: Sara Hadida-Ruah, Anna Hazlewood, Peter Grootenhuis, Fredrick Van Goor, Ashvani Singh, Jinglan Zhou, Jason McCartney
  • Publication number: 20130012704
    Abstract: The invention relates to compounds of formula (I) wherein the substituents X1, R1, R2, R3 and R4 have the meaning as set forth and explained in the description of the invention, to processes for the preparation of these compounds, pharmaceutical compositions containing same, the use thereof optionally in combination with one or more other pharmaceutically active compounds for the therapy of a disease which responds to an inhibition of protein kinase activity, and a method for the treatment of such a disease.
    Type: Application
    Filed: September 14, 2012
    Publication date: January 10, 2013
    Inventors: Qiang DING, Nathanael Schiander GRAY, Bing LI, Yi LIU, Taebo SIM, Tetsuo UNO, Guobao ZHANG, Carole Pissot Soldermann, Werner BREITENSTEIN, Guido BOLD, Giorgio CARAVATTI, Pascal FURET, Vito GUAGNANO, Marc LANG, Paul W. MANLEY, Joseph SCHOEPFER, Carsten SPANKA
  • Publication number: 20130012485
    Abstract: Compounds of the formula (I) are provided: wherein V, W, X, Y, Z, R3, R4, R5, R6, R7 and m are as defined in the specification; and pharmaceutically acceptable salts and prodrugs thereof. The compounds may be useful in the treatment or prevention of various diseases and conditions in which dipeptidylpeptidase-IV (DPP-IV) is implicated.
    Type: Application
    Filed: December 20, 2007
    Publication date: January 10, 2013
    Inventors: Daniel Kaspar Bäschlin, Richard Sedrani, Stefanie Flohr, Kenji Namoto, Nils Ostermann, Finton Sirockin, François Gessier, Garry Fenton, Mandy Christine Beswick, David Edward Clark, Bohdan Waszkowycz
  • Publication number: 20120316341
    Abstract: Methods for fluorinating organic compounds are described herein.
    Type: Application
    Filed: April 11, 2012
    Publication date: December 13, 2012
    Inventors: Tobias Ritter, Pingping Tang
  • Publication number: 20120283101
    Abstract: The present invention pertains to plant additives containing a molecule selected in a family of compounds, wherein said molecule can modulate some molecular markers and physiological modifications observed in cases of phosphate deficiency. The family of compounds comprises the molecule MC2 of formula (I) as well as analogues thereof.
    Type: Application
    Filed: September 17, 2010
    Publication date: November 8, 2012
    Inventors: Mathilde Clement, Thierry Desnos, Laurent Nussaume
  • Publication number: 20120277252
    Abstract: The present invention relates generally to compounds providing antibacterial therapeutic agents and preparations, and related methods of using and making antibacterial compounds. Antibacterial compounds of the present invention include chalcone, alkylpyrimidine, aminopyrimidine and cyanopyridine compounds and derivatives thereof exhibiting minimum inhibitory concentrations (MIC) similar to or less than conventional antibacterial compounds in wide use. For example, the present invention provides chalcone and cyanopyridine compounds, and derivatives thereof, exhibiting high antibacterial activities having multiple electron withdrawing group substituents, such as halogens and fluorinated alkyl groups, and optionally having hydroxyl and/or alkoxyl groups substituents.
    Type: Application
    Filed: July 6, 2012
    Publication date: November 1, 2012
    Inventors: Helen E. Blackwell, Matthew D. Bowman, Jennifer C. O'Neill, Joseph R. Stringer
  • Publication number: 20120277185
    Abstract: To provide novel carboxamides which exhibit an excellent pesticidal activity as pesticides. Carboxamides represented by the following Formula (I) and use thereof as pesticides and an animal parasite control agent: wherein each substituent is as defined in the specification.
    Type: Application
    Filed: July 10, 2010
    Publication date: November 1, 2012
    Applicant: BAYER CROPSCIENDE AG
    Inventors: Jun Mihara, Koichi Araki, Takuma Mori, Tetsuya Murata, Yasushi Yoneta, Eiichi Shimojo, Teruyuki Ichihara, Masashi Ataka, Katsuhiko Shibuya, Ulrich Görgens
  • Publication number: 20120264933
    Abstract: The present invention provides an efficient method to induce the enantioselectivity in procarbonyl compounds using chiral organometallic complexes. The present invention also provides a method for producing chiral organometallic complexes using a chiral additive, achiral additive, a base and a metal salt.
    Type: Application
    Filed: June 22, 2012
    Publication date: October 18, 2012
    Applicant: Laurus Labs Private Limited
    Inventors: Ravindra Babu BOLLU, Narasimha Rao Ketavarapu, Venkata Sunil Kumar Indukuri, Seeta Ramanjaneyulu Gorantla, Satyanarayana Chava
  • Patent number: 8283502
    Abstract: An autocatalytic process for the synthesis of chiral propargylic alcohols.
    Type: Grant
    Filed: April 9, 2010
    Date of Patent: October 9, 2012
    Assignee: Lonza Ltd.
    Inventors: Nicka Chinkov, Aleksander Warm, Erick Carreira
  • Publication number: 20120251449
    Abstract: The present invention claims fluoro- & iodo-containing aldehydes as ALDH substrates for use as diagnostic imaging agents or as therapeutic agents. The aldehydes are both directly and indirectly attached to an aromatic or a straight chain ring. ALDH activity was monitored either by the formation of acid-product or consumption of aldehyde substrates.
    Type: Application
    Filed: December 22, 2010
    Publication date: October 4, 2012
    Inventors: Vijaya Raj Kuniyil Kulangara, Alan Cuthbertson, Peter Iveson, Chitralekha Rangaswamy, Veena Rao, Rajiv Bhalla
  • Patent number: 8269045
    Abstract: Substituted pyrazinecarboxylic acid anilide derivatives represented by the general formula (I) or salts thereof; intermediates of them; pesticides (such as insecticides and acaricides) for agricultural and horticultural use, containing the compounds as the active ingredient; and usage thereof: wherein R1 is H, C1-6 alkyl, halo C1-6 alkyl, or the like; R2 is halogeno, C1-6 alkyl, or the like; G is C2-10 alkyl or the like; Z is oxygen or sulfur; X's are each independently H, halogeno, or the like; Y's are each independently H, halogeno, cyano, or the like; and m and n are each an integer of 1 to 3.
    Type: Grant
    Filed: July 29, 2010
    Date of Patent: September 18, 2012
    Assignee: Nihon Nohyaku Co., Ltd.
    Inventors: Takashi Furuya, Kozo Machiya, Akiyuki Suwa, Shinsuke Fujioka
  • Publication number: 20120220802
    Abstract: Aniline derivatives represented by formula (8) and formula (9): The aniline derivatives can be used as insecticides.
    Type: Application
    Filed: March 13, 2012
    Publication date: August 30, 2012
    Applicant: MITSUI CHEMICALS, INC.
    Inventors: Kei Yoshida, Takeo Wakita, Hiroyuki Katsuta, Akiyoshi Kai, Yutaka Chiba, Kiyoshi Takahashi, Hiroko Kato, Nobuyuki Kawahara, Michikazu Nomura, Hidenori Daido, Junji Maki, Shinichi Banba, Atsuko Kawahara