Polycyclo Ring System Having The Hetero Ring As One Of The Cyclos Patents (Class 549/23)
  • Patent number: 10029241
    Abstract: A method for easily producing a heterogeneous catalyst having excellent catalytic activity at a low cost is provided. The heterogeneous catalyst is used for the purpose of synthesizing a cyclic carbonate by reacting an epoxide and carbon dioxide. A catalyst obtained by this production method and a method for synthesizing a cyclic carbonate with use of this catalyst are also provided.
    Type: Grant
    Filed: April 22, 2014
    Date of Patent: July 24, 2018
    Assignees: MARUZEN PETROCHEMICAL CO., LTD., National Institute of Advanced Industrial Science and Technology
    Inventors: Takashi Naniki, Toshikazu Takahashi, Hiroyuki Yasuda, Shouji Yamamoto
  • Patent number: 9926326
    Abstract: Autophagy inhibitors useful for the treatment of cancer and other diseases are described. The autophagy inhibitors are a compound of formula: I wherein R1 is a group selected from lower alkyl, lower alkyl amide, lower alkyl ester, lower alkyl ketone, and lower alkyl ether; R2 and R3 are H or a group selected from cycloalkyl, lower alkyl, lower alkyl amide, lower alkyl ester, lower alkyl ketone, and lower alkyl ether; R4 is a heteroaryl group; and L is a —(CH2)n—X—(CH2)n— group, wherein n is 1, 2, 3, or 4, X is absent, O, S, or N—R5, wherein R5 is H or a lower alkyl group, or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: July 14, 2015
    Date of Patent: March 27, 2018
    Assignee: The Cleveland Clinic Foundation
    Inventors: Jennifer Carew, James G. Phillips
  • Publication number: 20150133493
    Abstract: Compounds including those of the Formula I where X, R1, R2 and subscript t are as defined herein, useful as ?-secretase inhibitors, are provided, as are compositions comprising the compounds, as well as methods for use of the compounds for treating or preventing neurodegenerative diseases, such as, for instance, Alzheimer's disease.
    Type: Application
    Filed: July 3, 2014
    Publication date: May 14, 2015
    Inventors: Lei Zhu, Hakim Djaballah, Yueming Li, Christopher Chad Shelton
  • Publication number: 20150133442
    Abstract: The invention features compositions and methods for inhibiting the Pin1 protein, and the treatment of disorders characterized by elevated Pin1 levels.
    Type: Application
    Filed: June 7, 2013
    Publication date: May 14, 2015
    Inventors: Kun Ping Lu, Matthew Brian Boxer, Mindy Irene Emily Davis, Rajan Pragani, Min Shen, Anton Momtchilov Simeonov, Shuo Wei, Xiao Zhen Zhou
  • Publication number: 20150119418
    Abstract: Provided is a pharmaceutical agent containing a compound represented by General Formula (1), a pharmaceutically acceptable salt thereof, or a solvate thereof: wherein A represents a C1-C3 linear alkylene group, in which one methylene group is optionally substituted with O or S; n represents an integer of from 3 to 5; X1 and X2 each independently represent CH or N; W1 and W2 each independently represent a carboxyl group or a tetrazolyl group; V represents a C1-C8 linear or branched alkylene group, in which one methylene group is optionally substituted with O or S; and R represents a substituted phenyl group, for example.
    Type: Application
    Filed: April 15, 2013
    Publication date: April 30, 2015
    Applicant: TOA EIYO LTD.
    Inventors: Kazuhiro Uemoto, Yoshimichi Sato, Naoki Okada, Emiko Iimori, Masayuki Kageyama
  • Patent number: 8927740
    Abstract: The present invention relates to a stereoselective reduction procedure to obtain, by means of catalytic asymmetric hydrogenation by hydrogen transfer, a compound of formula (I) in which X is S or SO2 and R4 is hydrogen or an SO2NH2 group, from the corresponding ketone precursor, said compound of formula (I) being useful as an intermediate in the preparation of dorzolamide or of the hydrochloride salt thereof.
    Type: Grant
    Filed: March 8, 2012
    Date of Patent: January 6, 2015
    Assignee: Zach System S.P.A.
    Inventors: Raffaella Volpicelli, Mauro Andretto, Livius Cotarca, Antonio Nardi, Massimo Verzini
  • Patent number: 8927591
    Abstract: The present invention relates to novel compounds, methods, and compositions capable of decreasing HIF hydroxylase enzyme activity, thereby increasing the stability and/or activity of hypoxia inducible factor (HIF).
    Type: Grant
    Filed: November 11, 2009
    Date of Patent: January 6, 2015
    Assignee: Fibrogen, Inc.
    Inventors: Wen-Bin Ho, Lee R. Wright, Eric D. Turtle, Craig Mossman, Lee A. Flippin
  • Patent number: 8877683
    Abstract: The present invention provides substituted pyridine compounds of the formula I or N-oxides or agriculturally suitable salts thereof, wherein the variables in the formula I are defined as in the description. Substituted pyridines of formula I are useful as herbicides.
    Type: Grant
    Filed: December 19, 2011
    Date of Patent: November 4, 2014
    Assignee: BASF SE
    Inventors: Matthias Witschel, William Karl Moberg, Liliana Parra Rapado, Gilbert Besong, Michael Rack, Andree Van Der Kloet, Thomas Seitz, Ruediger Reingruber, Helmut Kraus, Johannes Hutzler, Trevor William Newton, Jens Lerchl, Klaus Kreuz, Klaus Grossmann, Richard Roger Evans
  • Publication number: 20140235665
    Abstract: An object of the present invention is to provide an anti-constipation composition containing a halogenated-bi-cyclic compound as an active ingredient in a ratio of bi-cyclic/mono-cyclic structure of at least 1:1. The halogenated-bi-cyclic compound is represented by Formula (I): where X1 and X2 are preferably both fluorine atoms. The composition can be used to treat constipation without substantive side-effects, such as stomachache.
    Type: Application
    Filed: April 30, 2014
    Publication date: August 21, 2014
    Applicant: SUCAMPO AG
    Inventor: Ryuji UENO
  • Patent number: 8728708
    Abstract: Disclosed is a photosensitive resin composition comprising: (Component A) an oxime sulfonate compound represented by Formula (1); (Component B) a resin comprising a constituent unit having an acid-decomposable group that is decomposed by an acid to form a carboxyl group or a phenolic hydroxy group; and (Component C) a solvent wherein in Formula (1) R1 denotes an alkyl group, an aryl group, or a heteroaryl group, each R2 independently denotes a hydrogen atom, an alkyl group, an aryl group, or a halogen atom, Ar1 denotes an o-arylene group or an o-heteroarylene group, X denotes O or S, and n denotes 1 or 2, provided that of two or more R2s present in the compound, at least one denotes an alkyl group, an aryl group, or a halogen atom.
    Type: Grant
    Filed: February 27, 2013
    Date of Patent: May 20, 2014
    Assignee: FUJIFILM Corporation
    Inventors: Kyouhei Sakita, Wataru Kikuchi, Masatoshi Yumoto, Masanori Hikita
  • Publication number: 20130338377
    Abstract: The present invention relates to a stereoselective reduction procedure to obtain, by means of catalytic asymmetric hydrogenation by hydrogen transfer, a compound of formula (I) in which X is S or SO2 and R4 is hydrogen or an SO2NH2 group, from the corresponding ketone precursor, said compound of formula (I) being useful as an intermediate in the preparation of dorzolamide or of the hydrochloride salt thereof.
    Type: Application
    Filed: March 8, 2012
    Publication date: December 19, 2013
    Applicant: ZACH SYSTEM S.P.A.
    Inventors: Raffaella Volpicelli, Mauro Andretto, Livius Cotarca, Antonio Nardi, Massimo Verzini
  • Patent number: 8598249
    Abstract: The present invention is related to novel photoinitiators, in particular to photoinitiators comprising amino groups within the molecule.
    Type: Grant
    Filed: April 19, 2010
    Date of Patent: December 3, 2013
    Assignee: Siegwerk Druckfarben AG & Co. KGaA
    Inventors: Pierre-Antoine Noirot, Thierry Marsille, Matthieu Carni, Gilles Catherin
  • Publication number: 20130310254
    Abstract: The present application relates to novel alpha, beta-unsaturated imines, to processes for their preparation, to their use for controlling animal pests including arthropods and in particular insects and to their use in the control of vectors.
    Type: Application
    Filed: November 24, 2011
    Publication date: November 21, 2013
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Stefan Werner, Ulrich Ebbinghaus-Kintscher, Sebastian Horstmann, Michael Maue, Hans-Georg Schwarz, Robert Velten, Arnd Voerste, Ulrich Görgens, Andreas Turberg
  • Publication number: 20130310438
    Abstract: Provided is a compound which has strong intraocular pressure lowering action and has no side effect on eyes such as ocular stimulating property, humor protein rise etc. Since a compound represented by the formula (I): (wherein definition of each group is as described in the specification), or a salt thereof, a solvate thereof, or a prodrug thereof has strong intraocular pressure lowering activity and, further, has no side effect on eyes such as ocular stimulating property (hyperemia, corneal clouding etc.), aqueous humor protein rise etc., it has high safety, and can be an excellent agent for preventing and/or treating glaucoma etc.
    Type: Application
    Filed: January 26, 2012
    Publication date: November 21, 2013
    Applicant: ONO PHARMACEUTICAL CO., LTD.
    Inventors: Toru Maruyama, Tohru Kambe, Shinsaku Yamane, Satoshi Nakayama
  • Patent number: 8580975
    Abstract: Herein are described a process for forming a quaternary carbon useful in the preparation of macrolactones, an enantioselective synthesis of (+)-peloruside A, and methods for treating a patient in need of relief from cancer or a cancer-related disease. The described processes are useful for preparing compounds containing quaternary carbons, including structural analogs and derivatives of peloruside A.
    Type: Grant
    Filed: January 9, 2009
    Date of Patent: November 12, 2013
    Assignee: Purdue Research Foundation
    Inventors: Arun K Ghosh, Xiaoming Xu
  • Patent number: 8569356
    Abstract: The invention relates to cyclin dependent kinase inhibitor compounds and methods of identifying and using them. The invention further relates to pharmaceutical compositions for treating cell proliferative disorders, especially cancer.
    Type: Grant
    Filed: October 25, 2006
    Date of Patent: October 29, 2013
    Assignee: University of Florida Research Foundation, Inc.
    Inventors: David A. Ostrov, Brian K. Law, Patrick Corsino
  • Publication number: 20130171415
    Abstract: Disclosed is a photosensitive resin composition comprising: (Component A) an oxime sulfonate compound represented by Formula (1); (Component B) a resin comprising a constituent unit having an acid-decomposable group that is decomposed by an acid to form a carboxyl group or a phenolic hydroxy group; and (Component C) a solvent wherein in Formula (1) R1 denotes an alkyl group, an aryl group, or a heteroaryl group, each R2 independently denotes a hydrogen atom, an alkyl group, an aryl group, or a halogen atom, Ar1 denotes an o-arylene group or an o-heteroarylene group, X denotes O or S, and n denotes 1 or 2, provided that of two or more R2s present in the compound, at least one denotes an alkyl group, an aryl group, or a halogen atom.
    Type: Application
    Filed: February 27, 2013
    Publication date: July 4, 2013
    Applicant: FUJIFILM Corporation
    Inventor: FUJIFILM Corporation
  • Patent number: 8440842
    Abstract: The present invention relates to compounds of Formula (I) or salts thereof wherein R1, R2, R3, R4, R5, R6, and other variables enumerated under one or more of same are as defined herein. Compounds of Formula I have activity as antimicrobial agents. Also disclosed are pharmaceutical compositions and methods of treating and preventing microbial infections in mammals, for example, a tuberculosis or leprosy infection, which employ compounds of Formula (I) or salts thereof.
    Type: Grant
    Filed: June 25, 2008
    Date of Patent: May 14, 2013
    Assignee: Leibniz-Institut fuer Naturstoff-Forschung und Infektionsbiologie e.V. Hans-Knoell-Institut
    Inventors: Ute Moellmann, Vadim Makarov, Cole T. Stewart
  • Publication number: 20130079524
    Abstract: The present invention relates N-cycloalkyl-N-bicyclic-carboxamide, thiocarboxamide or N-substituted carboximidamide derivatives of formula (I) wherein A represents a carbo-linked, 5-membered heterocyclyl group; T represents O, S, N-Ra, N—ORa, N—NRaRb or N—CN; Z1 represents a C3-C7-cycloalkyl group; X represents N or a CZ7 and Z2; Z3; L1 and L2 represent various substituents; their process of preparation; preparation intermediate compounds; their use as fungicide active agents, particularly in the form of fungicide compositions and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions.
    Type: Application
    Filed: November 21, 2012
    Publication date: March 28, 2013
    Inventors: Philippe Desbordes, Stephanie Gary, Marie-Clarie Grosjean-Cournoyer, Benoit Hartmann, Hadano Hiroyuki, Philippe Rinolfi, Jean-Pierre Vors
  • Patent number: 8372380
    Abstract: Radiolabeled tracers for sulfotransferases (SULTs), their synthesis, and their use are provided. Included are substituted phenols, naphthols, coumarins, and flavones radiolabeled with 18F, 123I, 124I, 125I, or 11C. Also provided are in vivo techniques for using these and other tracers as analytical and diagnostic tools to study sulfotransferase distribution and activity, in health and disease, and to evaluate therapeutic interventions.
    Type: Grant
    Filed: March 31, 2008
    Date of Patent: February 12, 2013
    Assignee: The Regents of the University of California
    Inventors: Jorge R. Barrio, Vladimir Kepe, Gary W. Small, Nagichettiar Satyamurthy
  • Patent number: 8338431
    Abstract: The present invention relates to a compound according to formula I, wherein X, A, G, E, R1, R2, R3 are as shown herein; and pharmaceutically acceptable salts, hydrates, N-oxides or solvates hereof. The invention further relates to said compounds for use in therapy, to pharmaceutical compositions comprising said compounds, to methods of treating diseases, e.g. dermal diseases, with said compounds, and to the use of said compounds in the manufacture of medicaments.
    Type: Grant
    Filed: February 26, 2008
    Date of Patent: December 25, 2012
    Assignee: Leo Pharma A/S
    Inventors: Ravindra Babu Bollu, Jakob Felding, Simon Feldbæk Nielsen, Jens Christian Højland Larsen
  • Patent number: 8323745
    Abstract: An application liquid capable of forming a dense silica-based coating film even when embedded into a fine groove, and a method for formation of a silica-based coating film using the application liquid are provided. An application liquid is used including (A) a siloxane polymer, and (B) a base generator represented by the following general formula (I): wherein, R1 and R2 are a hydrocarbon group having 1 to 5 carbon atoms and which may be the same or different; or one of R1 and R2 is a hydrogen atom and the other is a hydrocarbon group having 1 to 5 carbon atoms; when R1 and R2 are both a hydrocarbon group, these may bind to one another to form a ring structure; R3 is a linking group; and R4 is a condensed ring.
    Type: Grant
    Filed: March 26, 2010
    Date of Patent: December 4, 2012
    Assignee: Tokyo Ohka Kogyo Co., Ltd.
    Inventors: Tokonori Yamadaya, Kiyoshi Ishikawa, Atsushi Sawano
  • Publication number: 20120289555
    Abstract: The present invention is directed to inhibitors of S-nitrosoglutathione reductase (GSNOR), pharmaceutical compositions comprising such GSNOR inhibitors, and methods of making and using the same.
    Type: Application
    Filed: February 10, 2011
    Publication date: November 15, 2012
    Applicant: N30 PHARMACEUTICALS, LLC
    Inventors: Xicheng Sun, Jian Qiu
  • Patent number: 8263787
    Abstract: There is provided a process for preparing dorzolamide and processes for preparing intermediates useful in the preparation of dorzolamide. In particular, there is provided a process for preparing an acetoamido sulfone of formula (viii) comprising oxidation of a hydroxysulfonamide of formula (vii) in the presence of an oxidizing agent selected from the group consisting of: a peracid, tert-butyl hydroperoxide, dimethyl dioxirane, selenium dioxide, m-phenanthroline di-N-oxide, nitric acid and hydrogen peroxide. There is also provided a process for preparing an acetoamidosulfone of formula (ix-a) comprising converting a hydroxysulfone of formula (viii) to the acetoamidosulfone of formula (ix-a) in the presence of acetonitrile and an acid. There is also provided a process for separating the cis- and trans-isomers of dorzolamide from a mixture of the trans-isomer of dorzolamide and the cis-isomer of dorzolamide comprising reacting the mixture of isomers with a carboxylic acid.
    Type: Grant
    Filed: May 7, 2008
    Date of Patent: September 11, 2012
    Assignee: CIPLA Limited
    Inventors: Rajendra Narayanrao Kankan, Dharmaraj Ramachandra Rao, Shrikant Suresh Mudgal
  • Patent number: 8222429
    Abstract: The present invention provides a photolabile protecting group that can be removed by light irradiation under mild conditions. More specifically, the present invention provides a method comprising protecting a reactive functional group (e.g., a hydroxyl group, amino group, carboxyl group, carbonyl group, phosphodiester group, etc.) by the photolabile protecting group, and then removing the photolabile protecting group simply by light irradiation under neutral conditions. The present invention relates to a compound represented by Formula (3): wherein Ar1 is an optionally substituted aromatic or heteroaromatic ring, Ar2 is an optionally substituted aryl or heteroaryl group, X is a leaving group, and n is an integer of 1 or 2; and a method of protecting and deprotecting an amino group etc. using the compound.
    Type: Grant
    Filed: January 8, 2009
    Date of Patent: July 17, 2012
    Assignee: National University Corporation Nara Institute of Science and Technology
    Inventors: Kazuki Sugawara, Yoshinori Gosyo
  • Patent number: 8198316
    Abstract: The present invention relates to resolution of (cis,trans)5,6-dihydro-4H-4-ethylamino-6-methylthieno[2,3-b]thiopyran-2-sulfonamide-7,7-dioxide using dibenzoyl-L-tartaric acid monohydrate or di-p-toluoyl-L-tarrtaric acid monohydrate as a chiral resolving agent in presence of methanol to obtain hemitartarate salt, purifying it to obtain hemitartarate salt of 5,6-dihydro-4H-4(S)-ethylamino-6(S)methylthieno[2,3-b]thiopyran-2-sulfonamide-7,7-dioxide with de of >99%, Chemical purity >99.5% with cis isomer content of <0.1% and further converting into its pharmaceutically acceptable salts, preferably hydrochloride salt.
    Type: Grant
    Filed: July 6, 2005
    Date of Patent: June 12, 2012
    Assignee: FDC Ltd
    Inventors: Anand Mohan Chandavarkar, Rajaram Uday Bapat, Anand Atul Bade, Anand Pandurang Chavan
  • Patent number: 8183391
    Abstract: A process for resolving dorzolamide trans racemate, which comprises reacting said racemate with (1S)-(+)-10-camphorsulfonic acid so obtaining the (4S,6S) enantiomer by selectively precipitating and recovering the camphorsulfonic acid salt thereof (dorzolamide camphorsulfonate), and neutralizing dorzolamide camphorsulfonate to obtain dorzolamide.
    Type: Grant
    Filed: April 16, 2007
    Date of Patent: May 22, 2012
    Assignee: Zach Systems S.p.A.
    Inventors: Paolo Maragni, Ivan Michieletto, Livius Cotarca
  • Patent number: 8154787
    Abstract: Green electrochromic (EC) materials based on thiophene, and a green EC material based on pyrazine are disclosed. A first thiophene derivative (2,3-Di-thiophen-2-yl-thieno[3,4-b]pyrazine), which was previously investigated as a nonlinear optical material, is here disclosed for its use as an EC material and for its incorporation into an EC device. Synthesis of two new thiophene derivatives (2,5-di(thien-2-yl)-3,4-di(2,2,2-trifluoro-ethoxy)-thiophene and 2,5-(2,3-dihydro-thieno[3,4-b][1,4]dioxin-5-yl)-3,4-di(2,2,2-trifluoro-ethoxy)-thiophene), and a new pyrazine derivative (2,3-dibenzyl-5,7-di(thien-2-yl) thieno[3,4-b]pyrazine) are also disclosed, since these materials are all able to selectively change state to appear a green color and can be polymerized to achieve a green EC polymer.
    Type: Grant
    Filed: August 27, 2010
    Date of Patent: April 10, 2012
    Assignee: University of Washington
    Inventors: Lu Liu, Chunye Xu, Minoru Taya
  • Publication number: 20120035206
    Abstract: Novel antibiotic and anticancer compounds of formula I, II, III, IV, derivatives, ostereoisomer, racemic and noracemic mixture of ostereoisomer, or the pharmaceutically acceptable salts or solvates of these compounds are disclosed. The preparation, pharmaceutical composition and biological activity of these compounds are disclosed.
    Type: Application
    Filed: April 9, 2010
    Publication date: February 9, 2012
    Inventors: Gengliang Yang, Zhengyue Ma, Wei Tian, Baoling Fang, Ge Wang, Linbo Li, Chunliu Yang, Ligai Bai
  • Patent number: 8084649
    Abstract: Cyclohexanedione compounds, and derivatives thereof, which are substituted in 5-position, are suitable for use as herbicides. The cyclohexanedione compounds and derivatives of the invention are compounds of formula (I) wherein the substituents are as defined in the description.
    Type: Grant
    Filed: March 7, 2008
    Date of Patent: December 27, 2011
    Assignee: Syngenta Crop Protection, inc.
    Inventors: Michel Muehlebach, William Lutz, Jean Wenger, John Finney, Christopher John Mathews, Delphine Raymonde Suzanne Fawke
  • Patent number: 8080664
    Abstract: Use of the general formula compound (I), or any salt thereof, for preparation of a pharmaceutical compound for the treatment of infections illnesses, in particular for the treatment of Helicobacter. Y is NO2, COOH or SO3H; Z is O, N or S; X1 and X2 are halogen atoms which may be the same or different; and m and n take values from 0 to 3 and may be equal or different.
    Type: Grant
    Filed: February 20, 2008
    Date of Patent: December 20, 2011
    Assignee: Universidad De Zaragoza
    Inventors: Javier Sancho Sanz, Adrián Velazquez Campoy, Nunilo Cremades Casasin
  • Publication number: 20110305776
    Abstract: The present invention relates to novel compounds, methods, and compositions capable of decreasing HIF hydroxylase enzyme activity, thereby increasing the stability and/or activity of hypoxia inducible factor (HIF).
    Type: Application
    Filed: November 11, 2009
    Publication date: December 15, 2011
    Applicant: FibroGen, Inc.
    Inventors: Wen-Bin Ho, Lee A. Flippin, Craig Mossman, Eric D. Turtle, Lee R. Wright
  • Patent number: 8058307
    Abstract: Compounds of the general formula (formula I) in which the meanings of the substituents R1 to R6 are as indicated in claim 1, have renin-inhibiting properties and can be used as medicines.
    Type: Grant
    Filed: September 14, 2006
    Date of Patent: November 15, 2011
    Assignee: Novartis AG
    Inventors: Peter Herold, Robert Mah, Vincenzo Tschinke, Stefan Stutz, Aleksandar Stojanovic, Stjepan Jelakovic, Christiane Marti
  • Patent number: 8044097
    Abstract: The invention relates to novel chroman derivatives, stereoisomers and pharmaceutically acceptable salts of Formula I wherein the substituents are as defined in the specification. They are useful in the treatment of disorders mediated by lipoxygenase, such as immune diseases, respiratory diseases and cardiovascular diseases, as well as in the treatment of neurodegenerative disorders and/or mitochondria) disorders. They are also useful in the manufacture of pharmaceutical formulations for the treatment of such conditions.
    Type: Grant
    Filed: February 26, 2009
    Date of Patent: October 25, 2011
    Assignee: Ampere Life Sciences, Inc.
    Inventors: Bing Wang, Jian Chen
  • Patent number: 7973072
    Abstract: The invention relates to substituted benzo-condensed cyclohexanone derivatives, to a method for the production thereof, to medicaments containing said derivatives and to the use of the inventive compounds for producing medicaments.
    Type: Grant
    Filed: May 17, 2006
    Date of Patent: July 5, 2011
    Assignee: Gruenenthal GmbH
    Inventors: Robert Frank, Michael Przewosny, Ruth Jostock
  • Patent number: 7968593
    Abstract: This invention provides new compounds, pharmaceutical compositions and diagnostic kits comprising such compounds, and methods of using such compounds for inhibiting NAALADase enzyme activity, detecting diseases where NAALADase levels are altered, inhibiting angiogenesis, effecting a TGF-? activity or a neuronal activity, and treating a glutamate abnormality, a compulsive disorder, neuropathy, pain, a prostate disease, cancer, Huntington's disease, diabetes, a retinal disorder or glaucoma.
    Type: Grant
    Filed: May 26, 2009
    Date of Patent: June 28, 2011
    Assignee: Eisai Inc.
    Inventors: Barbara S. Slusher, Takashi Tsukamoto
  • Patent number: 7960369
    Abstract: The GPR40 receptor function regulator of the present invention, which comprises a compound having an aromatic ring and a group capable of releasing cation is useful as an insulin secretagogue or an agent for the prophylaxis or treatment of diabetes and the like.
    Type: Grant
    Filed: November 6, 2003
    Date of Patent: June 14, 2011
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Kohji Fukatsu, Shinobu Sasaki, Shuji Hinuma, Yasuaki Ito, Nobuhiro Suzuki, Masataka Harada, Tsuneo Yasuma
  • Publication number: 20110136888
    Abstract: The present invention involves substituted 1,3-diphenylpropane derivatives, pharmaceutical compositions comprising them and the therapeutic uses thereof, in particular in the fields of human and animal health.
    Type: Application
    Filed: June 21, 2007
    Publication date: June 9, 2011
    Inventors: Jean-Francois Delhomel, Rémy Hanf, Karine Caumont-Bertrand
  • Patent number: 7943661
    Abstract: The invention concerns novel substituted 1,3-diphenylprop-2-en-1-one derivatives, pharmaceutical compositions comprising same, their therapeutic uses, in particular for treating cerebral ischemia. The invention also concerns a method for preparing said derivatives.
    Type: Grant
    Filed: July 8, 2003
    Date of Patent: May 17, 2011
    Assignee: Genfit
    Inventors: Jamila Najib, Karine Caumont-Bertrand
  • Publication number: 20110028738
    Abstract: The present invention provides a photolabile protecting group that can be removed by light irradiation under mild conditions. More specifically, the present invention provides a method comprising protecting a reactive functional group (e.g., a hydroxyl group, amino group, carboxyl group, carbonyl group, phosphodiester group, etc.) by the photolabile protecting group, and then removing the photolabile protecting group simply by light irradiation under neutral conditions. The present invention relates to a compound represented by Formula (3): wherein Ar1 is an optionally substituted aromatic or heteroaromatic ring, Ar2 is an optionally substituted aryl or heteroaryl group, X is a leaving group, and n is an integer of 1 or 2; and a method of protecting and deprotecting an amino group etc. using the compound.
    Type: Application
    Filed: January 8, 2009
    Publication date: February 3, 2011
    Applicant: National University Corporation Nara Institute of Science and Technology
    Inventors: Kiyomi Kakiuchi, Ken Tsutsumi, Satoru Kitani, Kazuki Sugawara, Yoshinori Gosyo
  • Publication number: 20110028540
    Abstract: Herein are described a process for forming a quaternary carbon useful in the preparation of macrolactones, an enantioselective synthesis of (+)-peloruside A, and methods for treating a patient in need of relief from cancer or a cancer-related disease. The described processes are useful for preparing compounds containing quaternary carbons, including structural analogs and derivatives of peloruside A.
    Type: Application
    Filed: January 9, 2009
    Publication date: February 3, 2011
    Inventors: Arun K Ghosh, Xiaoming Xu
  • Patent number: 7880021
    Abstract: 3-hydroxyflavone derivatives are useful in the detection and the quantification of cell apoptosis. Such derivatives are also useful as fluorescent probes in studying lipid asymmetry of cell plasma membrane and in detecting apopoptic cells. The derivatives can be used to monitor the evolution of diseases involving cell apoptosis.
    Type: Grant
    Filed: October 11, 2006
    Date of Patent: February 1, 2011
    Assignees: Centre National de la Recherche Scientifique (CNRS), Universite Louis Pasteur (Strasbourg I)
    Inventors: Yves Mely, Andrey Klymchenko, Oleksandr Demchenko, Vasyl Shynkar
  • Publication number: 20100324306
    Abstract: Green electrochromic (EC) materials based on thiophene, and a green EC material based on pyrazine are disclosed. A first thiophene derivative (2,3-Di-thiophen-2-yl-thieno[3,4-b]pyrazine), which was previously investigated as a nonlinear optical material, is here disclosed for its use as an EC material and for its incorporation into an EC device. Synthesis of two new thiophene derivatives (2,5-di(thien-2-yl)-3,4-di(2,2,2-trifluoro-ethoxy)-thiophene and 2,5-(2,3-dihydro-thieno[3,4-b][1,4]dioxin-5-yl)-3,4-di(2,2,2-trifluoro-ethoxy)-thiophene), and a new pyrazine derivative (2,3-dibenzyl-5,7-di(thien-2-yl) thieno[3,4-b]pyrazine) are also disclosed, since these materials are all able to selectively change state to appear a green color and can be polymerized to achieve a green EC polymer.
    Type: Application
    Filed: August 27, 2010
    Publication date: December 23, 2010
    Applicant: University of Washington
    Inventors: Lu Liu, Chunye Xu, Minoru Taya
  • Publication number: 20100317862
    Abstract: Use of the general formula compound (I), or any salt thereof, for preparation of a pharmaceutical compound for the treatment of infections illnesses, in particular for the treatment of Helicobacter. Y is NO2, COOH or SO3H; Z is O, N or S; X1 and X2 are halogen atoms which may be the same or different; and m and n take values from 0 to 3 and may be equal or different.
    Type: Application
    Filed: February 20, 2008
    Publication date: December 16, 2010
    Inventors: Javier Sancho Sanz, Adrián Velazquez Campoy, Nunilo Cremades Casasin
  • Publication number: 20100311778
    Abstract: The present invention provides transient receptor potential vanilloid (TRPV) modulators. In particular, compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by TRPV3. Also provided herein are processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders modulated by TRPV3.
    Type: Application
    Filed: December 16, 2008
    Publication date: December 9, 2010
    Inventors: V S Prasadarao Lingam, Abraham Thomas, Laxmikant Atmaram Gharat, Deepak Vitthal Ukirde, Shantaram Kashinath Phatangare, Ajit Shankar Mindhe, Neelima Khairatkar-Joshi, Vidya Ganapati Kattige
  • Publication number: 20100310657
    Abstract: Provided is a pharmaceutical composition for the treatment and prevention of kidney diseases, containing (a) a therapeutically effective amount of a compound represented by Formulae 1 or 2 or a pharmaceutically acceptable salt, prodrug, solvate or isomer thereof, and (b) a pharmaceutically acceptable carrier, diluent or excipient or any combination thereof.
    Type: Application
    Filed: December 18, 2008
    Publication date: December 9, 2010
    Applicants: MAZENCE INC., KT & G CORPORATION
    Inventors: Taehwan Kwak, Myung-Gyu Park, Kyoung Hoon Jung
  • Publication number: 20100305095
    Abstract: The present invention relates to, inter alia, the use of a compound capable of inhibiting 4-hydroxyphenylpyruvate dioxygenase (HPPD) in an animal in the manufacture of a medicament for use in the treatment and/or prevention of depression. The invention also provides for the use of a compound capable of inhibiting HPPD in an animal in the manufacture of a medicament for use in the treatment of the withdrawal symptoms associated with an addictive drug which causes dopamine dependant associative learning disorders in said animal. In a particular embodiment said HPPD inhibitor is selected from the group consisting of the compound depicted as compound 1; 2; and 3.22.
    Type: Application
    Filed: August 18, 2006
    Publication date: December 2, 2010
    Inventors: Kim Zachary Travis, John Posner
  • Patent number: 7842821
    Abstract: The invention is aimed at a compound of formula (I) wherein n is 0, 1 or 2, R1 is a linear or branched alkyl group, R2 is selected from a substituted or non substituted alkyl group, substituted or non substituted aryl group, substituted or non substituted aralkyl group, substituted or non substituted heterocyclyl group, or a substituted or non substituted heterocyclylalkyl group. Another object of the invention is a process for obtaining these compounds from the corresponding compound with a hydroxy group in position 4 by means of reacting with a sulfonamide in the presence of a phosphine and a dialkyl azadicarboxylate. The deprotection of the compound of formula (I) gives rise to the corresponding amine. The intermediate and the processes described are very useful in the synthesis of pharmaceutical products.
    Type: Grant
    Filed: November 4, 2005
    Date of Patent: November 30, 2010
    Assignee: Ragactives, S.L.
    Inventors: José María Gorgojo Lobato, Luis Octavio Silva Guisasola, Jorge Martín Juárez
  • Patent number: 7833691
    Abstract: The present invention relates to a heterocycle-containing onium salt useful as, for example, a cationic photopolymerization initiator and an acid generator for a chemically amplified resist, and provides a heterocycle-containing onium salt shown in the specification.
    Type: Grant
    Filed: November 20, 2007
    Date of Patent: November 16, 2010
    Assignee: Wako Pure Chemical Industries, Ltd.
    Inventors: Masami Ishihara, Yoji Urano, Masahiro Takahashi
  • Patent number: 7816476
    Abstract: Cyclopropyl acrylate of general formula (1), constitutional and stereoisomers thereof and their mixtures in which A is selected from:
    Type: Grant
    Filed: August 9, 2005
    Date of Patent: October 19, 2010
    Assignee: Ivoclar Vivadent AG
    Inventors: Norbert Moszner, Frank Zeuner, Urs-Karl Fischer, Volker M. Rheinberger, Armin de Meijere, Viktor Bahutski