Nitrogen Attached Indirectly To The Hetero Ring By Nonionic Bonding Patents (Class 549/74)
  • Patent number: 11111227
    Abstract: The present disclosure relates to rotigotine behenate, methods for preparing the same and use of the same for treating diseases associated with dopamine receptor. The rotigotine behenate, the structure of which is shown below, is capable of reducing fluctuation in blood drug concentrations, improving the bioavailability of the drug in vivo, and achieving smooth and extended release of rotigotine.
    Type: Grant
    Filed: April 27, 2020
    Date of Patent: September 7, 2021
    Assignee: Shandong Luye Pharmaceutical Co., Ltd.
    Inventors: Mina Yang, Yongtao Jiang, Ying Meng, Tao Wang, Qian qian Xu, Xin Shao, Chunjie Sha
  • Patent number: 10669249
    Abstract: The present disclosure relates to rotigotine behenate, methods for preparing the same and use of the same for treating diseases associated with dopamine receptor. The rotigotine behenate, the structure of which is shown below, is capable of reducing fluctuation in blood drug concentrations, improving the bioavailability of the drug in vivo, and achieving smooth and extended release of rotigotine.
    Type: Grant
    Filed: July 21, 2016
    Date of Patent: June 2, 2020
    Assignee: Shandong Luye Pharmaceutical Co., Ltd.
    Inventors: Mina Yang, Yongtao Jiang, Ying Meng, Tao Wang, Qian qian Xu, Xin Shao, Chunjie Sha
  • Patent number: 9650329
    Abstract: The present invention relates to transition-metal-free process for the synthesis of tertiary arylamines comprises coupling reaction between arynes and N,N-dimethyl aniline compounds in presence of 18-crown-6, KF and THF.
    Type: Grant
    Filed: June 24, 2014
    Date of Patent: May 16, 2017
    Assignee: COUNCIL OF SCIENTIFIC & INDUSTRIAL RESEARCH
    Inventors: Akkattu Thankappan Biju, Sachin Suresh Bhojgude, Trinadh Kaicharla
  • 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: 20150119582
    Abstract: Naphthyl-containing compounds having structural formula S2R for use in organic light-emitting diodes (OLEDs). R may include an aromatic group, a heterocyclic group, or a group that is both aromatic and heterocylic. In some examples, R is phenyl, biphenyl, and thiophenyl. OLEDs including these compounds are shown to emit in a range between 400 nm and 700 nm. These OLEDs are suitable for devices including televisions, laptop computers, computer monitors, personal digital assistants, mobile phones, portable media players, watches, test devices, advertising displays, information displays, indication displays, and large-area light-emitting elements for general illumination.
    Type: Application
    Filed: May 8, 2013
    Publication date: April 30, 2015
    Inventor: Carl WAGNER
  • Patent number: 9012491
    Abstract: Disclosed herein are antimicrobial compounds compositions, pharmaceutical compositions, the use and preparation thereof. Some embodiments relate to cyclic boronate compounds and their use as therapeutic agents.
    Type: Grant
    Filed: August 30, 2012
    Date of Patent: April 21, 2015
    Assignee: Rempex Pharmaceuticals, Inc.
    Inventors: Raja K. Reddy, Serge Henri Boyer, Maxim Totrov, Scott Hecker
  • Patent number: 8981121
    Abstract: The present invention provides an alternative synthesis of N-substituted aminotetralines comprising resolution of N-substituted aminotetralins of formula (II), wherein R1, R2 and R3 are as defined for compound of formula (I).
    Type: Grant
    Filed: June 24, 2011
    Date of Patent: March 17, 2015
    Assignee: UCB Pharma GmbH
    Inventors: Celal Ates, Arnaud Schule, Magali Palacio, Paul Deutsch, David Vasselin, Nicolas Carly, Ganesh Phadtare, Swapnil Yerande, Jean-Pierre Delatinne, Maria Luisa Escudero Hernandez, Veronique Pinilla
  • Publication number: 20150038705
    Abstract: Compounds, compositions, and methods comprising a polyamine compound are described, which may be used to kill, disperse, treat, reduce biofilms, and/or inhibit or substantially prevent biofilm formation. In certain aspects, the present invention relates to compounds, compositions, and methods comprising polyamine compounds that have antimicrobial or dispersing activity against a variety of bacterial strains capable of forming biofilms.
    Type: Application
    Filed: October 6, 2014
    Publication date: February 5, 2015
    Inventors: DUSTIN WILLIAMS, RYAN LOOPER, SUJEEVINI JEYAPALINA, TRAVIS HAUSSENER, PAUL R. SEBAHAR, HARI KANNA REDDY
  • Patent number: 8916183
    Abstract: This document discloses molecules having the following formulas (“Formula One” &“Formula Two” and “Formula Three”) The Ar1, Het, Ar2, R1, R2, R3, R4, and R5 are further described herein.
    Type: Grant
    Filed: January 22, 2013
    Date of Patent: December 23, 2014
    Assignee: Dow AgroSciences, LLC.
    Inventors: Lindsey G. Fischer, Gary D. Crouse, Thomas C. Sparks, Erich W. Baum
  • Patent number: 8906946
    Abstract: Compounds acting as selective antagonists of Transient Receptor Potential cation channel subfamily M member 8 (hereinafter referred to as TRPM8), having formula: Wherein R is selected from: H, Br, CN, NO2, SO2NH2, SO2NHR? and SO2NR?2, where R? is selected from linear or branched C1-C4 alkyl; X is selected from: F, Cl, C1-C3 alkyl, NH2 and OH Y is selected from: O, CH2, NH and SO2 R1 and R2, independently one from the other, are selected from H, F and linear or branched C1-C4 alkyl; R3 and R4, independently one from the other, are selected from H and linear or branched C1-C4 alkyl; Z is selected from: NR6 and R6R7N+, where R6 and R7 independently one from the other, are selected from: H and linear or branched C1-C4 alkyl R5 is a residue selected from: H and linear or branched C1-C4 alkyl Het is a heteroaryl group selected from a substituted or not substituted pyrrolyl, a substituted or not substituted N-methylpyrrolyl, a substituted or not substituted thiophenyl, a substituted or
    Type: Grant
    Filed: January 27, 2012
    Date of Patent: December 9, 2014
    Assignee: Dompe' S.p.A.
    Inventors: Alessio Moriconi, Gianluca Bianchini, Andrea Aramini, Laura Brandolini, Chiara Liberati, Silvia Bovolenta, Andrea Beccari, Simone Lorenzi
  • Patent number: 8889732
    Abstract: Fused heterocyclic compounds useful for prevention, treatment or improvement of diseases against which activation of the thrombopoietin receptor is effective are provided. A compound represented by the formula (I) (wherein R1 is an aryl group fused to a saturated ring or the like, A, B, L1, R2, L2, L3, Y, L4, R3 and X are defined in the description), a tautomer, prodrug or a pharmaceutically acceptable salt of the compound or a solvate thereof.
    Type: Grant
    Filed: October 22, 2010
    Date of Patent: November 18, 2014
    Assignee: Nissan Chemical Industries, Ltd.
    Inventors: Yukihiro Shigeta, Shingo Umezawa, Shunsuke Iwamoto, Takanori Nakamura
  • Publication number: 20140322596
    Abstract: In an aspect, an additive for an electrolyte of a lithium battery, the additive including a compound including at least three nitrile moieties is provided:
    Type: Application
    Filed: January 8, 2014
    Publication date: October 30, 2014
    Applicant: Samsung SDI Co., Ltd.
    Inventors: Pavel Alexandrovich Shatunov, Woo-Cheol Shin, Sang-Hoon Kim, Jung-Yi Yu, Ha-Rim Lee, In-Haeng Cho, Khasanov Makhmut
  • Patent number: 8754119
    Abstract: The present invention relates to the use of rotigotine [(?)-5,6,7,8-tetrahydro-6-[propyl[2-(2-thienyl)ethyl]amino]-1-naphthol] and its prodrugs and pharmaceutically acceptable salts for producing a pharmaceutical agent for treating depression.
    Type: Grant
    Filed: July 22, 2004
    Date of Patent: June 17, 2014
    Assignee: UCB Pharma GmbH
    Inventors: Dieter Scheller, Alexander Breidenbach, Norma Selve
  • Patent number: 8754120
    Abstract: The present invention relates to new salts of 6-(propyl-(2-thiophen-2-ylethyl)amino)tetralin-1-ol (rotigotine), their use as a medicament, for example for the treatment of CNS disorders like Parkinson Disease, RLS, fybromyalgia and/or depression, in particular through electromotive administration. The present invention relates to pharmaceutical formulations suitable for iontophoresis that provide enhanced iontophoretic delivery of rotigotine to at least one target tissue. The formulations are further characterized by good to excellent solubility of the salts in aqueous solutions.
    Type: Grant
    Filed: June 24, 2010
    Date of Patent: June 17, 2014
    Assignee: UCB Pharma GmbH
    Inventors: Johanna Aaltje Bouwstra, Oliver Ackaert, Jacob Eikelenboom, Hans-Michael Wolff
  • Publication number: 20140100371
    Abstract: A process for preparing azomethines of the general formula (V) where R is an optionally substituted carbocyclic aromatic radical having 6 to 24 carbon atoms or an optionally substituted alkyl radical or an optionally substituted heteroaromatic radical having 5 to 24 carbon atoms, and R1 is an optionally substituted carbocyclic aromatic radical having 6 to 24 carbon atoms or an optionally substituted heteroaromatic radical having 5 to 24 carbon atoms, R2 is hydrogen or an optionally substituted carbocyclic aromatic radical having 6 to 24 carbon atoms or an optionally substituted alkyl radical or an optionally substituted cycloalkyl radical N or an optionally substituted heteroaromatic radical having 5 to 24 carbon atoms by reacting alpha-oxo carboxylates of the general formula (I) where n is a number in the range from 1 to 6, M(n+) is a cation, with aryl bromides of the general formula (IV) and amines of the general formula (II) via the alpha-iminocarboxylate intermediate of the general formula (III), in the p
    Type: Application
    Filed: November 18, 2011
    Publication date: April 10, 2014
    Applicant: Saltigo GmbH
    Inventors: Alain Cotte, Matthias Cotta, Felix Rudolph, Bingrui Song, Lukas Goossen
  • Publication number: 20140077200
    Abstract: The present invention provides a novel aromatic amine derivative having a specific structure and an organic electroluminescence device in which an organic thin film layer comprising a single layer or plural layers including at least a light emitting layer is interposed between a cathode and an anode, wherein at least one layer in the above organic thin film layer, particularly a hole injecting layer contains the aromatic amine derivative described above in the form of a single component or a mixed component. Use of the aromatic amine derivative described above materialize an organic electroluminescence device which reduces an operating voltage and makes molecules less liable to be crystallized and which enhances a yield in producing the organic EL device and has a long lifetime.
    Type: Application
    Filed: November 26, 2013
    Publication date: March 20, 2014
    Applicants: Sony Corporation, Idemitsu Kosan Co., Ltd.
    Inventors: Nobuhiro YABUNOUCHI, Masahiro Kawamura, Hisayuki Kawamura, Chishio Hosokawa, Shigeyuki Matsunami, Tadahiko Yoshinaga, Yasunori Kijima
  • Patent number: 8648111
    Abstract: The present invention provides an N1-2-thiophen-2-ylethyl-N2-substituted biguanide derivative of formula (I) or a pharmaceutically acceptable salt thereof, a method for preparing same, and a pharmaceutical composition comprising same as an active ingredient. The inventive N1-2-thiophen-2-ylethyl-N2-substituted biguanide derivative exhibits improved blood glucose level- and lipid level-lowering effects even with a reduced dosage as compared to conventional drugs, and thus, it is useful for preventing or treating diabetes, metabolic syndromes such as insulin-independent diabetes, obesity and atherosclerosis, or a P53 gene defect-related cancer.
    Type: Grant
    Filed: October 13, 2009
    Date of Patent: February 11, 2014
    Assignees: Hanall Biopharma Co., Ltd., Korea Research Institute of Chemical Technology
    Inventors: Sung Wuk Kim, Sung Soo Jun, Hyae Gyeong Cheon, Kwang Rok Kim, Sang Dal Rhee, Won Hoon Jung, Jong Cheol Lee
  • Publication number: 20140039181
    Abstract: The invention relates to a method for producing a N-substituted amine compound by catalyzed alkylation. The method uses amine and alcohol or two kinds of amines as the reaction materials, employs composite metal oxides catalyst at a reaction temperature of 80-180° C. to catalyze the reaction for 6-36 hours, so as to produce the N-substituted amine compound. The reaction condition of the method of the invention is relatively moderate, using a catalyst made of cheap non-noble metals, which is non-caustic and easy to be separated and reused. The reaction does not need any medium and has relatively high conversion rate and selectivity.
    Type: Application
    Filed: December 28, 2012
    Publication date: February 6, 2014
    Applicant: Lanzhou Institute of Chemical Physics, Chinese Academy of Sciences
    Inventor: Lanzhou Institute of Chemical Physics, Chinese Academy of Sciences
  • Publication number: 20140031398
    Abstract: Compounds acting as selective antagonists of Transient Receptor Potential cation channel subfamily M member 8 (hereinafter referred to as TRPM8), having formula: Wherein R is selected from: H, Br, CN, NO2, SO2NH2, SO2NHR? and SO2NR?2, where R? is selected from linear or branched C1-C4 alkyl; X is selected from: F, Cl, C1-C3 alkyl, NH2 and OH Y is selected from: O, CH2, NH and SO2 R1 and R2, independently one from the other, are selected from H, F and linear or branched C1-C4 alkyl; R3 and R4, independently one from the other, are selected from H and linear or branched C1-C4 alkyl; Z is selected from: NR6 and R6R7N+, where R6 and R7 independently one from the other, are selected from: H and linear or branched C1-C4 alkyl R5 is a residue selected from: H and linear or branched C1-C4 alkyl Het is a heteroaryl group selected from a substituted or not substituted pyrrolyl, a substituted or not substituted N-methylpyrrolyl, a substituted or not substituted thiophenyl, a substituted or
    Type: Application
    Filed: January 27, 2012
    Publication date: January 30, 2014
    Inventors: Alessio Moriconi, Gianluca Bianchini, Andrea Aramini, Laura Brandolini, Chiara Liberati, Silvia Bovolenta, Andrea Beccari, Simone Lorenzi
  • Patent number: 8592424
    Abstract: A method of treating a disease state or condition in humans via topical brainstem afferent stimulation therapy via the administration of a drug to the back of the neck of a human patient at the hairline in close proximity to and under or on the area of skin above the brain stem to provide regional neuro-affective therapy is disclosed.
    Type: Grant
    Filed: June 29, 2009
    Date of Patent: November 26, 2013
    Assignee: Afgin Pharma LLC
    Inventor: Ronald Aung-Din
  • Publication number: 20130296346
    Abstract: The invention relates to compounds of formula (I): or a pharmaceutically acceptable salt, prodrug or solvate thereof, a method of synthesis of said compounds, pharmaceutical compositions comprising them and their use as a medicament for treating inflammatory diseases.
    Type: Application
    Filed: November 22, 2011
    Publication date: November 7, 2013
    Applicant: Faes Farma, S.A.
    Inventors: Rosa Rodes Solanes, Neftali Garcia Dominguez, Beatriz Lopez Ortega, Melchor Alvarez De Mon Soto, Antonio De La Hera Martinez, Ana Munoz Munoz, Francisco Ledo Gomez
  • Publication number: 20130252964
    Abstract: The present disclosure provides compounds, or pharmaceutically acceptable salts thereof, for killing or inhibiting the growth of a Candida or Aspergillus species or preventing or treating a mammal having candidiasis (oral and/or disseminated) or an Aspergillus infection.
    Type: Application
    Filed: January 18, 2013
    Publication date: September 26, 2013
    Applicant: PolyMedix, Inc.
    Inventors: Richard W. Scott, Katie Freeman, Haizhong Tang, Gill Diamond
  • Publication number: 20130236434
    Abstract: A method of enhancing binding of cells to an integrin-binding ligand comprises treating integrin-expressing cells in vitro with an agonist of integrin, wherein the integrin is selected from the group consisting of ?4?1, ?5?1, ?4?7, ?v?3 and ?L?2, and contacting the treated cells with an integrin-binding ligand; integrin agonist compounds having the general formula I; methods of treating integrin-expressing cells with such agonists to enhance binding; and therapeutic methods comprising administering agonist-treated cells or agonist compounds to a mammal.
    Type: Application
    Filed: November 16, 2011
    Publication date: September 12, 2013
    Applicant: TEXAS HEART INSTITUTE
    Inventors: Ronald J. Biediger, William C. Gundlach, IV, Robert V. Market, Michael M. Savage, Peter Vanderslice
  • Patent number: 8525577
    Abstract: A photoelectric conversion device comprising an electrically conductive film, an organic photoelectric conversion film, and a transparent electrically conductive film, wherein the organic photoelectric conversion film contains a compound represented by the following formula (1) and an n-type organic semiconductor: wherein each of R1 and R2 independently represents a substituted aryl group, an unsubstituted aryl group, a substituted heteroaryl group or an unsubstituted heteroaryl group, each of R3 to R11 independently represents a hydrogen atom or a substituent provided that an acidic group is excluded, m represents 0 or 1, n represents an integer of 0 or more, R1 and R2, R3 and R4, R3 and R5, R5 and R6, R6 and R8, R7 and R8, R7 and R9, or R10 and R11 may be combined each other to form a ring, and when n is an integer of 2 or more, out of a plurality of R7's and R8's, a pair of R7's, a pair of R8's, or a pair of R7 and R8 may be combined each other to form a ring.
    Type: Grant
    Filed: September 28, 2010
    Date of Patent: September 3, 2013
    Assignee: FUJIFILM Corporation
    Inventors: Katsuyuki Yofu, Kimiatsu Nomura, Mitsumasa Hamano, Tetsuro Mitsui
  • Publication number: 20130221331
    Abstract: A compound is shown by the following formula (1). wherein l, m, and n are independently an integer from 1 to 3, Ar1 to Ar4 are independently a substituted or unsubstituted aryl group having 6 to 30 ring carbon atoms, or a substituted or unsubstituted heteroaryl group having 5 to 30 ring atoms, Ar5, Ar6, and Ar7 are independently a substituted or unsubstituted arylene group having 6 to 30 ring carbon atoms, or a substituted or unsubstituted heteroarylene group having 5 to 30 ring atoms, and p is an integer from 0 to 2, and Ar6 and N are bonded via a single bond when p is 0, provided that at least one of Ar1 to Ar4 is substituted with a substituted silyl group, a substituted or unsubstituted alkyl group having 1 to 20 carbon atoms, or a substituted or unsubstituted cycloalkyl group having 3 to 10 carbon atoms, and at least one of Ar1 to Ar4 is substituted with a cyano group.
    Type: Application
    Filed: October 24, 2011
    Publication date: August 29, 2013
    Applicant: IDEMITSU KOSAN CO., LTD.
    Inventors: Yumiko Mizuki, Hiroyuki Saito, Yuichiro Kawamura, Hirokatsu Ito, Masahiro Kawamura
  • Publication number: 20130217884
    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: November 2, 2011
    Publication date: August 22, 2013
    Applicant: OTSUKA AGRITECHNO CO., LTD.
    Inventors: Satoru Masumoto, Hitoshi Mutsutani, Sachi Kimura
  • Patent number: 8513438
    Abstract: The present invention describes a novel process for the preparation of (6S)-(?)-5,6,7,8-tetrahydro-6-[propyl-(2-thienyl)ethyl]amino-1-naphthol (Rotigotine) comprising: (a) acetylating (S)-(?)-5-hydroxy-N-n-propyl-2-aminotetraline to afford the acetate; (b) reacting this acetate, (?)-5-acetoxy-N-n-propyl-2-aminotetraline, with 2-(2-thienyl)ethanol 2-nitrobenzenesulfonate; (d) hydrolyzing (6S)-(?)-1-acetoxy-5,6,7,8-tetrahydro-6-[propyl-(2-thienyl)ethyl]amino-1-naphthalene to afford (6S)-(?)-5,6,7,8-tetrahydro-6-[propyl-(2-thienyl)ethyl]amino-1-naphthol (Rotigotine) and (d) purifying rotigotine either by the acetylation reaction and subsequent hydrolysis of the formed acetate or by salification of rotigotine through hydrochloride or hydrobromide formation and subsequent base release. Rotigotine is a dopamine agonist and is indicated for the treatment of Parkinson's disease.
    Type: Grant
    Filed: December 9, 2009
    Date of Patent: August 20, 2013
    Assignee: Interquim, S.A.
    Inventors: Marta Pomares, Francisco Marquillas Olondriz
  • Patent number: 8410241
    Abstract: A process for the preparation of a polymerizable unit for production of a hole transporting polymer for use in an optical device, which process comprises reacting in the presence of S to form wherein each R is the same or different and is independently H or a substituent group; n is O or an integer from 1 to 100; Ar and Ar? are the same or different and are each aromatic or heteroaromatic groups which are substituted or unsubstituted; Y is a direct bond, a light emissive moiety, a hole transporting moiety or an electron transporting moiety; and X is a polymerizable group.
    Type: Grant
    Filed: December 23, 2005
    Date of Patent: April 2, 2013
    Assignee: Cambridge Display Technology Limited
    Inventor: Caroline Towns
  • Patent number: 8357710
    Abstract: There is provided a compound of formula I, wherein R1a, R1b, X, Y1, Y2, Y3, Y4, Z1, Z2, R2 and R3 have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful as selective agonists of the AT2 receptor, and thus, in particular, in the treatment of inter alia gastrointestinal conditions, such as dyspepsia, IBS and MOF, and cardiovascular disorders.
    Type: Grant
    Filed: April 12, 2006
    Date of Patent: January 22, 2013
    Assignee: Vicore Pharma AB
    Inventors: Mathias Alterman, Anders Hallberg, Murugaiah Andappan Murugaiah Subbaiah
  • Publication number: 20120309799
    Abstract: A biguanide derivative compound with N4-N5 substitution, which is represented by Formula 1, or a pharmaceutically acceptable salt thereof, a method of preparing the same, and a pharmaceutical composition containing the same as an active ingredient are provided. The biguanide derivative may exhibit excellent effect on activation of AMPK and inhibition of cancer cell proliferation in a low dose, compared with conventional drugs, and thus, may be useful to treat diabetes mellitus, obesity, hyperlipidemia, hypercholesterolemia, fatty liver, coronary artery disease, osteoporosis, polycystic ovarian syndrome, metabolic syndrome, cancer, etc.
    Type: Application
    Filed: January 6, 2011
    Publication date: December 6, 2012
    Applicant: HANALL BIOPHARMA CO., LTD.
    Inventors: Sung Wuk Kim, Sung Soo Jun, Chang Hee Min, Se Hwan Park, Yong Eun Kim, Duck Kim, Ji Sun Lee, Ju Hoon Oh
  • Publication number: 20120283249
    Abstract: The subject matter of the present invention is novel families of compounds which are aromatic amine, imine, aminoadamantane and benzodiazepine derivatives, medicaments comprising same and the use thereof as inhibitors of the toxic effects of toxins with intracellular activity, such as, for example, ricin, and of viruses that use the internalization pathway for infecting cells.
    Type: Application
    Filed: June 17, 2009
    Publication date: November 8, 2012
    Inventors: Roman Lopez, Séverine Hebbe, Daniel Gillet, Julien Barbier
  • Patent number: 8283376
    Abstract: The invention relates to the use of substituted 2-aminotetralins of general formula (I) as a medicament for the preventive treatment of Parkinson's disease.
    Type: Grant
    Filed: December 23, 2004
    Date of Patent: October 9, 2012
    Assignee: UCB Pharma GmbH
    Inventors: Dieter Scheller, Frank Dressen
  • Publication number: 20120149693
    Abstract: The invention relates to protein binding interacting/binding compounds and methods of identifying and using them. The invention further relates to pharmaceutical compositions and methods for treating 5-HT2C and/or RSK disorders, including diseases and disorders mediated by GPCRs and/or RSKs.
    Type: Application
    Filed: May 5, 2010
    Publication date: June 14, 2012
    Applicant: UNIVERSITY OF FLORIDA RESEARCH FOUNDATION, INC.
    Inventor: Raymond G. Booth
  • Patent number: 8183393
    Abstract: A dye compound is described, which is expressed by formula (I): wherein A1, A2 and A3 each independently represent a substituted or unsubstituted 1,4-phenylene or 2,5-thiophene group, and B1 and B2 each independently represent a substituted or unsubstituted aryl group. The dye compound is suitably used as a dye sensitizer in a dye sensitized solar cell (DSSC).
    Type: Grant
    Filed: May 19, 2009
    Date of Patent: May 22, 2012
    Assignee: Academia Sinica
    Inventors: Tahsin J. Chow, Yuan-Chieh Chang
  • Publication number: 20120101146
    Abstract: The present invention relates to new salts of 6-(propyl-(2-thiophen-2-ylethyl)amino)tetralin-1-ol (rotigotine), their use as a medicament, for example for the treatment of CNS disorders like Parkinson Disease, RLS, fybromyalgia and/or depression, in particular through electromotive administration. The present invention relates to pharmaceutical formulations suitable for iontophoresis that provide enhanced iontophoretic delivery of rotigotine to at least one target tissue. The formulations are further characterized by good to excellent solubility of the salts in aqueous solutions.
    Type: Application
    Filed: June 24, 2010
    Publication date: April 26, 2012
    Applicant: UCB Pharma GmbH
    Inventors: J.A. Bouwstra, O.W.G.M.K. Ackaert, J. Eikelenboom, Hans-Michael Wolff
  • Patent number: 8158790
    Abstract: The present invention provides an excellent antihypertensive medicament. The medicament of the present invention comprises a compound having the general formula (I) and the like: [wherein R1: H, substitutable alkyl, substitutable alkenyl, substitutable cyclic hydrocarbon, substitutable heterocyclyl or the like; R2: H, substitutable alkyl, substitutable alkenyl, substitutable cycloalkyl or the like; R3, R4; H, substitutable alkyl, substitutable alkenyl, substitutable cycloalkyl or the like; R5, R6: H, substitutable alkyl, substitutable cycloalkyl, substitutable alkoxy or the like; R7, R8: H, substitutable alkyl, substitutable cycloalkyl or the like; X: the formula (II) or the like; A: substitutable cyclic hydrocarbon, substitutable heterocyclyl or the like; Y: a single bond, substitutable alkylene, substitutable alkenylene, —(CH2)a—X1—(CH2)b—(X1: the formula —NH—, —O— or the like; a, b: 0-5) or the like; B: substitutable cyclic hydrocarbon, substitutable heterocyclyl or the like].
    Type: Grant
    Filed: June 22, 2007
    Date of Patent: April 17, 2012
    Assignee: Daiichi Sankyo Company, Limited
    Inventors: Shojiro Miyazaki, Yuji Nakamura, Takahiro Nagayama, Taro Tokui, Yasuyuki Ogawa
  • Patent number: 8143069
    Abstract: A compound represented by the following general formula (II): wherein R21 represents hydrogen atom or one to four monovalent substituents substituting on the benzene ring, and when R21 represents two or more substituents, the substituents may be the same or different; R22, R24, R25, and R27 independently represent hydrogen atom, or a monovalent substituent; R23 represents —OH or —N(R28)(R29) (wherein R28 and R29 independently represent an alkyl group which may be substituted); R26 represents —N(R30)(R31) (wherein R30 and R31 independently represent an alkyl group which may be substituted); n represents an integer of 1 to 3; and Y represents —S— or —O—, which is useful for selective measurement of hypochlorite ion.
    Type: Grant
    Filed: March 1, 2007
    Date of Patent: March 27, 2012
    Assignee: The University of Tokyo
    Inventors: Tetsuo Nagano, Yasuteru Urano, Suguru Kenmoku
  • Publication number: 20120041038
    Abstract: Provided are amine derivative compounds, pharmaceutical compositions thereof, and methods of treating ophthalmic diseases and disorders, such as age-related macular degeneration and Stargardt's Disease, using said compounds and compositions.
    Type: Application
    Filed: October 21, 2011
    Publication date: February 16, 2012
    Applicant: Acucela Inc.
    Inventors: Ian L. Scott, Vladimir A. Kuksa, Mark W. Orme, Feng Hong, Thomas L. Little, JR., Ryo Kubota
  • Publication number: 20120041039
    Abstract: Provided are amine derivative compounds, pharmaceutical compositions thereof, and methods of treating ophthalmic diseases and disorders, such as age-related macular degeneration and Stargardt's Disease, using said compounds and compositions.
    Type: Application
    Filed: October 21, 2011
    Publication date: February 16, 2012
    Applicant: Acucela Inc.
    Inventors: Ian L. Scott, Vladimir A. Kuksa, Mark W. Orme, Feng Hong, Thomas L. Little, JR., Ryo Kubota
  • Publication number: 20120029013
    Abstract: The present invention concerns compounds of general formula (1), where in:—-a- is a single or double bond, Ar is an aromatic group, substituted or unsubstituted, R1 and R2 each independently or together are: a hydrogen atom or C1-C6 alkyl group, branched or unbranched, saturated or unsaturated, substituted or unsubstituted; the groups R1 and R2 may also form a heterocycle, R3 and R3? each independently or together are a hydrogen atom or C1-C6 alkyl group, X is an oxygen atom or a sulphur atom, and the addition salts of the compounds of general formula (1) with pharmaceutically acceptable mineral acids or organic acids.
    Type: Application
    Filed: April 2, 2010
    Publication date: February 2, 2012
    Applicant: PIERRE FABRE MEDICAMENT
    Inventors: Stéphane Cuisiat, Adrian Newman-Tancredi, Olivier Vitton, Bernard Vacher
  • Publication number: 20120029211
    Abstract: A catalytic Wittig method utilizing a phosphine including the steps of providing a phosphine oxide precatalyst and reducing the phosphine oxide precatalyst to produce the phosphine; forming a phosphonium ylide precursor from the phosphine and a reactant; generating a phosphonium ylide from the phosphonium ylide precursor; reacting the phosphonium ylide precursor with the aldehyde, ketone, or ester to form the olefin and the phosphine oxide which then reenters the cycle. The invention is also directed to a Mitsunobu reaction catalytic in phosphine.
    Type: Application
    Filed: April 6, 2010
    Publication date: February 2, 2012
    Inventor: Christopher J. O'Brien
  • Publication number: 20120004262
    Abstract: The present invention relates to phenylcyclopropylamine derivatives. In particular, pharmaceutical compositions comprising phenylcyclopropylamine derivatives are provided. The compounds of this invention can, inter alia, be used for the treatment and the prevention of cancer as well as neurodegenerative diseases or disorders.
    Type: Application
    Filed: January 21, 2010
    Publication date: January 5, 2012
    Inventors: Nathalie Guibourt, Alberto Ortega Munoz, Julio Castro-Palomino Laria
  • Patent number: 8084463
    Abstract: Compounds of Formula (I); in salt or zwitterionic form wherein R1, R2, R3 and R4 have the meanings as indicated in the specification, are useful for treating conditions that are mediated by the muscarinic M3 receptor, especially inflammatory or obstructive airways diseases. Pharmaceutical compositions that contain the compounds and a process for preparing the compounds are also described.
    Type: Grant
    Filed: March 11, 2010
    Date of Patent: December 27, 2011
    Assignee: Novartis AG
    Inventors: Neil J Press, Stephen P Collingwood, Urs Baettig, Brian Cox, Sudhakar D Garad, Hyungchul Kim, Dimitris Papoutsakis, Simon J Watson
  • Publication number: 20110285274
    Abstract: An organic material for an organic light emitting diode (OLED) display, and an OLED display are provided, and the organic material includes an anthracene derivative includes at least deuterium.
    Type: Application
    Filed: April 29, 2011
    Publication date: November 24, 2011
    Applicant: Samsung Mobile Display Co., Ltd.
    Inventors: Yuji Hamada, Kwan-Hee Lee
  • Patent number: 8034961
    Abstract: The present invention relates to a process for preparing stereoisomerically enriched 4-aryl-4-hydroxybutanoic acid derivatives by reducing 4-aryl-4-ketobutanoic acid derivatives in the presence of ruthenium-containing catalysts.
    Type: Grant
    Filed: December 17, 2007
    Date of Patent: October 11, 2011
    Assignee: LANXESS Deutschland GmbH
    Inventors: Hans-Christian Militzer, Boris Bosch, Markus Eckert, Benjamin Meseguer
  • Patent number: 8017558
    Abstract: Novel carboxamides of the formula (I) The present application is further directed toward a plurality of processes for preparing these compounds and their use for controlling unwanted microorganisms, and also novel intermediates and their preparation.
    Type: Grant
    Filed: December 5, 2006
    Date of Patent: September 13, 2011
    Assignee: Bayer Cropscience AG
    Inventors: Ralf Dunkel, Hans-Ludwig Elbe, Jörg Nico Greul, Herbert Gayer, Bernd-Wieland Krüger, Arnd Voerste, Ulrike Wachendorff-Neumann, Peter Dahmen
  • Publication number: 20110196015
    Abstract: The present invention provides an N1-2-thiophen-2-ylethyl-N2-substituted biguanide derivative of formula (I) or a pharmaceutically acceptable salt thereof, a method for preparing same, and a pharmaceutical composition comprising same as an active ingredient. The inventive N1-2-thiophen-2-ylethyl-N2-substituted biguanide derivative exhibits improved blood glucose level- and lipid level-lowering effects even with a reduced dosage as compared to conventional drugs, and thus, it is useful for preventing or treating diabetes, metabolic syndromes such as insulin-independent diabetes, obesity and atherosclerosis, or a P53 gene defect-related cancer.
    Type: Application
    Filed: October 13, 2009
    Publication date: August 11, 2011
    Applicants: HANALL BIOPHARMA CO., LTD., KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGY
    Inventors: Sung Wuk Kim, Sung Soo Jun, Hyae Gyeong Cheon, Kwang Rok Kim, Sang Dal Rhee, Won Hoon Jung, Jong Cheol Lee
  • Patent number: 7989497
    Abstract: The present invention relates to compounds of formula (I) wherein X, R1, R2, R3, R4 and R5 are as defined herein, which are useful for treating diseases which respond to CXCR2 receptor mediators. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.
    Type: Grant
    Filed: July 30, 2009
    Date of Patent: August 2, 2011
    Assignee: Novartis AG
    Inventors: Urs Baettig, Anne-Marie D'Souza, Peter Hunt, Neil John Press, Simon James Watson
  • Patent number: 7989488
    Abstract: In one aspect, the present invention provides a novel thiophene-containing polynitrone compound having structure (II) wherein R1 is independently at each occurrence a C1-C20 aliphatic radical, a C3-C20 cycloaliphatic radical, or a C2-C30 aromatic radical; R2 is independently at each occurrence hydrogen, deuterium, a C1-C20 aliphatic radical, a C3-C20 cycloaliphatic radical, or a C2-C30 aromatic radical; and “a” is an integer from 2 to 4.
    Type: Grant
    Filed: September 28, 2007
    Date of Patent: August 2, 2011
    Assignee: General Electric Company
    Inventors: Christoph Georg Erben, Michael Jeffrey Mclaughlin, Kathryn Lynn Longley, Shantaram Narayan Naik, Mahesh Kisan Chaudhari, Jyoti Balkrishna Shet, Varadarajan Sundararaman, Yogendrasinh Bharatsinh Chauhan, Gary Charles Davis, Sumeet Jain, Moitreyee Sinha
  • Publication number: 20110160276
    Abstract: A compound has Formula VIII where, X is —C(O)R, —C(O)OR, —CN, —NO2, —S(O)2R?, —P(O)(OR)2; each R is individually H, alkyl, or alkenyl; R? is alkyl or akenyl; R1 is aryl, alkenyl, arylalkenyl, heterocyclyl, or heteroaryl; and R2, R3, R4, R5, R6, R7, R8, R9, R10, and R11 are individually H, alkoxy, or hydroxy. In some cases, X is NO2. Pharmaceutical compositions of the compound of Formula VIII with a pharmaceutically acceptable carrier may be prepared. The compounds may be used for inhibition of cyclooxygenase-2.
    Type: Application
    Filed: March 4, 2010
    Publication date: June 30, 2011
    Inventors: Irishi N.N. Namboothiri, Narasimham Ayyagari, Deena Jose