Piperidines Patents (Class 546/184)
  • Patent number: 10556905
    Abstract: A process for preparing a diazabicyclooctane compound represented by the following formula (I): wherein A represents RcO—; B represents NH or NC1-6 alkyl; C represents a benzyl group; Rc represents a C1-6 alkyl group; A is substituted with one substituent Fn1, wherein Fn1 represents an azetidine group; the process including: (a) silylating the compound represented by the following formula (IV-c): wherein in the formula (IV-c), OBn represents benzyloxy, and (b) carrying out an intramolecular urea formation reaction.
    Type: Grant
    Filed: May 8, 2018
    Date of Patent: February 11, 2020
    Assignee: MEIJI SEIKA PHARMA CO., LTD.
    Inventors: Takao Abe, Takeshi Furuuchi, Yoshiaki Sakamaki, Seiichi Inamura, Akihiro Morinaka
  • Patent number: 10420754
    Abstract: The present invention is related to a compound of formula (I): a pharmaceutically acceptable salt thereof, a hydrate thereof, a solvate thereof, a metabolite thereof or a prodrug thereof; for use in a method for the treatment and/or prevention of cancer, wherein X is selected from the group consisting of N—R1, O and S; R1 is selected from the group consisting of alkyl, cycloalkyl, aryl, arylalkyl and hydrogen; R2 is selected from the group consisting of indolyl, substituted indolyl, azaindolyl and substituted azaindolyl; and R3 is selected from the group consisting of aryl, substituted aryl, unsubstituted heteroaryl, heterocyclyl and substituted heterocyclyl.
    Type: Grant
    Filed: June 11, 2018
    Date of Patent: September 24, 2019
    Assignee: Centogene AG
    Inventors: Matthias Beller, Jan Lukas, Moritz Frech, Christian Junghanss, Anahit Pews-Davtyan
  • Patent number: 10370457
    Abstract: Disclosed is an antibody which binds to paliperidone, which can be used to detect paliperidone in a sample such as in a competitive immunoassay method. The antibody can be used in a lateral flow assay device for point-of-care detection of paliperidone, including multiplex detection of aripiprazole, olanzapine, quetiapine, risperidone and paliperidone in a single lateral flow assay device.
    Type: Grant
    Filed: January 19, 2017
    Date of Patent: August 6, 2019
    Assignee: Janssen Pharmaceutica NV
    Inventors: Eric Hryhorenko, Banumathi Sankaran, Thomas R. DeCory, Theresa Tubbs, Linda Colt, Maarten Vliegen, Pieter Rik Haspeslagh
  • Patent number: 10259802
    Abstract: This invention relates to compounds (Formula (1)) that are agonists of the muscarinic M1 receptor and which are useful in the treatment of muscarinic M1 receptor mediated diseases. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds. Compounds provided are of formula where R1-R5, X1, X2 and p are as defined herein.
    Type: Grant
    Filed: May 15, 2018
    Date of Patent: April 16, 2019
    Assignee: Heptares Therapeutics Limited
    Inventors: Giles Albert Brown, Julie Elaine Cansfield, Miles Stuart Congreve, Mark Pickworth, Benjamin Gerald Tehan
  • Patent number: 10252996
    Abstract: The present invention provides an N1-cyclic amine-N5-substituted biguanide derivative compound represented by Formula 1, a method of preparing the same and a pharmaceutical composition including the biguanide derivative or the pharmaceutically acceptable salt thereof as an active ingredient. The biguanide derivatives have an effect of inhibiting cancer cell proliferation, cancer metastasis and cancer recurrence by activation of AMPK, even when administered in a small dose compared with conventional drugs.
    Type: Grant
    Filed: December 14, 2017
    Date of Patent: April 9, 2019
    Assignee: ImmunoMet Therapeutics Inc.
    Inventors: Chang Hee Min, Yong Eun Kim, Byung Kyu Oh, Ji Sun Lee, Hye Jin Heo, Ju Hoon Oh, Woong Cho
  • Patent number: 10167255
    Abstract: The present invention refers to a process for preparing amines comprising reacting a compound of the formula R1—CO—R2 comprising a carbonyl moiety with a amine compound of the formula HNR3R4 and carbon monoxide in the presence of a catalyst.
    Type: Grant
    Filed: December 10, 2013
    Date of Patent: January 1, 2019
    Assignee: STUDIENGESELLSCHAFT KOHLE MBH
    Inventors: Benjamin List, Denis Alexandrovich Chusov
  • Patent number: 9999690
    Abstract: Novel labeled compounds and metabolites thereof are disclosed, as well as pharmaceutical compositions including the compounds, and methods of using the labeled and unlabeled compounds, and specifically, 2-Amino-5-guanidino-pentanoic acid (3-{4-[3-(2-amino-5-guanidino-pentanoylamino)-propyl]-piperazin-1-yl}-propyl)-amide and metabolites thereof, for imaging, detecting and assessing disorders and diseases, such as arthritis and, more specifically, osteoarthritis by tracking proteoglycan and glycosaminoglycan content of cartilage. Also, pharmaceutical compositions comprising labeled and/or unlabeled 1,4-Bis(3-aminopropyl)piperazine are disclosed and methods of using the same.
    Type: Grant
    Filed: November 6, 2014
    Date of Patent: June 19, 2018
    Assignee: PEROSPHERE PHARMACEUTICALS INC.
    Inventors: Bryan E. Laulicht, Sasha H. Bakhru, James Costin, Solomon S. Steiner
  • Patent number: 9993463
    Abstract: The present invention is related to a compound of formula (I) a pharmaceutically acceptable salt thereof, a hydrate thereof, a solvate thereof, a metabolite thereof or a prodrug thereof; for use in a method for the treatment and/or prevention of cancer, wherein X is selected from the group consisting of N—R1, O and S; R1 is selected from the group consisting of alkyl, cycloalkyl, aryl, arylalkyl and hydrogen; R2 is selected from the group consisting of indolyl, substituted indolyl, azaindolyl and substituted azaindolyl; and R3 is selected from the group consisting of aryl, substituted aryl, unsubstituted heteroaryl, heterocyclyl and substituted heterocyclyl.
    Type: Grant
    Filed: December 10, 2013
    Date of Patent: June 12, 2018
    Assignee: Centogene AG
    Inventors: Matthias Beller, Jan Lukas, Moritz Frech, Christian Junghanss, Arndt Rolfs, Anahit Pews-Davtyan
  • Patent number: 9975890
    Abstract: This invention relates to compounds (Formula (1)) that are agonists of the muscarinic M1 receptor and which are useful in the treatment of muscarinic M1 receptor mediated diseases. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds. Compounds provided are of formula where R1-R5, X1, X2 and p are as defined herein.
    Type: Grant
    Filed: May 15, 2017
    Date of Patent: May 22, 2018
    Assignee: Heptares Therapeutics Limited
    Inventors: Giles Albert Brown, Julie Elaine Cansfield, Miles Stuart Congreve, Mark Pickworth, Benjamin Gerald Tehan
  • Patent number: 9855202
    Abstract: Described herein is a hair color composition for dyeing the hair. The hair color composition includes one or more direct dye compounds and one or more additional ingredients. The one or more direct dye compounds each include a chromophore, one or two permanent cations, and one to four incipient cations. The one to four incipient cations are pendant to the core structure and are neutral. The one or more direct dye compounds enter the hair shaft after the hair color composition is applied to the hair. The hair color composition has a pH of from about 7 to about 11.
    Type: Grant
    Filed: March 17, 2016
    Date of Patent: January 2, 2018
    Assignee: Noxell Corporation
    Inventors: Guiru Zhang, Bryan Patrick Murphy, Peter Marte Torgerson
  • Patent number: 9777010
    Abstract: The present invention provides a compound having the structure: wherein R1, R2, R3, R4, and R5 are each independently H, halogen, CF3 or C1-C4 alkyl, wherein two or more of R1, R2, R3, R4, or R5 are other than H; R6 is H, OH, or halogen; and B is a substituted or unsubstituted heterobicycle, wherein when R1 is CF3, R2 is H, R3 is F, R4 is H, and R5 is H, or R1 is H, R2 is CF3, R3 is H, R4 is CF3, and R5 is H, or R1 is Cl, R2 is H, R3 is H, R4 is F, and R5 is H, or R1 is CF3, R2 is H, R3 is F, R4 is H, and R5 is H, or R1 is CF3, R2 is F, R3 is H, R4 is H, and R5 is H, or R1 is Cl, R2 is F, R3 is H, R4 is H, and R5 is H, then B is other than or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: September 1, 2016
    Date of Patent: October 3, 2017
    Assignee: THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORK
    Inventors: Konstantin Petrukhin, Christopher Cioffi, Graham Johnson, Rando Allikmets, Emily Freeman, Ping Chen, Michael Conlon, Lei Zhu
  • Patent number: 9724331
    Abstract: The present invention is related to a compound of formula (I): a pharmaceutically acceptable salt thereof, a hydrate thereof, a solvate thereof, a metabolite thereof or a prodrug thereof; for use in a method for the treatment and/or prevention of leukemia, wherein X is selected from the group consisting of N—R1, O and S; R1 is selected from the group consisting of alkyl, cycloalkyl, aryl, arylalkyl and hydrogen; R2 is selected from the group consisting of indolyl, substituted indolyl, azaindolyl and substituted azaindolyl; and R3 is selected from the group consisting of aryl, substituted aryl, unsubstituted heteroaryl, heterocyclyl and substituted heterocyclyl.
    Type: Grant
    Filed: December 10, 2013
    Date of Patent: August 8, 2017
    Assignee: Centogene AG
    Inventors: Matthias Beller, Jan Lukas, Moritz Frech, Christian Junghanss, Arndt Rolfs, Anahit Pews-Davtyan, Christian Eisenloeffel
  • Patent number: 9688701
    Abstract: Compounds, methods of making the compounds and methods of using the compounds are generally described herein. The compounds are generally of formula R1R2N—ZnY LiY, wherein R1 and R2 are independently selected from H, aryl, heteroaryl containing one or more heteroatoms, alkyl, alkenyl, alkynyl, and silicon derivatives thereof; and each Y is independently selected from F, Cl, Br, I, CN, SCN, NCO, HalO3, HalO4, NO3, BF4, PF6, H, an alcoholate of formula OR5, a carboxylate of formula R5CO2; a thiolate of formula SR5, R5P(O)O2, SCOR5, SCSR5, OnSR5 and NOn, wherein n=2 or 3; wherein R5 is selected from substituted or unsubstituted aryls or heteroaryls containing 3 to 24 carbon atoms and one or more heteroatoms selected from B, O, N, S, Se, P, linear, branched or cyclic, substituted or unsubstituted alkyls, alkenyls, alkynyls or H; and wherein Hal is a halogen selected from Cl, Br and I.
    Type: Grant
    Filed: April 1, 2016
    Date of Patent: June 27, 2017
    Assignee: Ludwig-Maximilians-Universitat Munchen
    Inventors: Paul Knochel, Marc Mosrin
  • Patent number: 9670173
    Abstract: It is an object of the present invention to provide a medicament for preventing or treating hyperphosphatemia. Solution: A compound represented by a general formula (I) or a pharmacologically acceptable salt thereof. (In the formula, R1: a methyl group or the like, R2: a hydrogen atom or the like, R3: a hydrogen atom or the like, A: a cyclohexyl ring or the like, X: CH or the like, Y: CH or the like, Z: CH or the like, and n: 2 or the like).
    Type: Grant
    Filed: September 30, 2016
    Date of Patent: June 6, 2017
    Assignee: DAIICHI SANKYO COMPANY, LIMITED
    Inventors: Yoshikazu Uto, Mikio Kato, Hidenori Takahashi, Yasuyuki Ogawa, Osamu Iwamoto, Hiroko Kono, Kazumasa Aoki
  • Patent number: 9505667
    Abstract: There is provided a method for deuterating an aromatic compound having aromatic hydrogens. The method includes the steps: (a) providing a liquid composition including deuterium oxide having dissolved or dispersed therein the aromatic compound and a transition metal catalyst; and (b) heating the liquid composition at a temperature of 120° C. or greater, and a pressure of 50 psi or greater, for a period of 24 hours or less, to form a deuterated aromatic compound.
    Type: Grant
    Filed: November 6, 2014
    Date of Patent: November 29, 2016
    Assignee: E I DU PONT DE NEMOURS AND COMPANY
    Inventors: Michael Henry Howard, Jr., David P Bellon, David P Dickson, Jeffrey A Merlo
  • Patent number: 9504637
    Abstract: Dyes, compositions comprising dyes and methods for using the same are provided.
    Type: Grant
    Filed: October 22, 2015
    Date of Patent: November 29, 2016
    Assignee: Living Proof, Inc.
    Inventors: Jana Lewis, Lorna Nagamoottoo-Casse, David Puerta
  • Patent number: 9481625
    Abstract: The invention has an object of providing an economical and highly efficient process for producing a cyclohexanone compound such as cyclohexanone. An aspect of the invention resides in a process for producing a cyclohexanone compound by performing hydrogenation reaction of a phenol compound in a gas phase in the presence of a palladium catalyst supported on a carrier to produce the corresponding cyclohexanone compound, wherein the hydrogenation reaction is carried out in the presence of at least one nitrogen compound selected from ammonia, amine compounds and heteroaromatic compounds.
    Type: Grant
    Filed: April 1, 2014
    Date of Patent: November 1, 2016
    Assignee: MITSUI CHEMICALS, INC.
    Inventors: Akira Matsuura, Takuro Watanabe
  • Patent number: 9284273
    Abstract: A compound of the following compound (B): wherein tBu represents a tert-butyl group. A compound of the following compound (C): wherein tBu represents a tert-butyl group, and TFA represents a trifluoroacetyl group.
    Type: Grant
    Filed: April 1, 2015
    Date of Patent: March 15, 2016
    Assignee: MEIJI SEIKA PHARMA CO., LTD.
    Inventors: Takao Abe, Masayuki Okue, Yoshiaki Sakamaki
  • Patent number: 9181250
    Abstract: A diazabicyclooctane compound, which is a beta-lactame inhibitor, represented by the following formula (I): wherein A represents Ra(Rb)N— or RcO—; B represents NH or NC1-6 alkyl; C represents benzyl, H or SO3M, wherein M represents H, an inorganic or an organic cation; Ra and Rb represent H, C1-6 alkyl or acyl; Rc represents C1-6 alkyl or a heterocyclyl; A is unsubstituted or substituted with 0 to 4 substituents Fn1, wherein Fn1 represents C1-6 alkyl, O?, or Rg-(CH2)0-3—, wherein Rg represents a heterocyclyl, phenyl, heteroaryl, acyl, RdO2S—, Re(Rf)N—, Re(Rf)NCO—, ReO—, ReOCO— or a protective group, wherein Rd represents C1-6 alkyl or MO—; Re and Rf represent H or C1-6 alkyl, and a heterocycle having at least one nitrogen atom may be formed between Ra and Rb, between Rc and B, or between Re and Rf.
    Type: Grant
    Filed: May 30, 2013
    Date of Patent: November 10, 2015
    Assignee: MEIJI SEIKA PHARMA CO., LTD.
    Inventors: Takao Abe, Takeshi Furuuchi, Yoshiaki Sakamaki
  • Patent number: 9102669
    Abstract: The present invention is directed to novel piperidinyl-pyridazinyl derivatives, pharmaceutical compositions containing them and their use as inhibitors of SCD1, useful in the treatment of obesity, type-II diabetes and other related metabolic disorders.
    Type: Grant
    Filed: December 5, 2012
    Date of Patent: August 11, 2015
    Assignee: Janssen Pharmaceutica NV
    Inventors: Shyh-Ming Yang, Gee-Hong Kuo, Micheal D. Gaul, Thomas A. Rano
  • Patent number: 9012648
    Abstract: The invention relates to compounds of Formula I, wherein R1 and R2 are defined in the specification, useful for the synthesis of novel conjugates and immunogens derived from risperidone and paliperidone. The invention also relates to conjugates of a risperidone or paliperidone hapten and a protein.
    Type: Grant
    Filed: August 20, 2013
    Date of Patent: April 21, 2015
    Assignee: Janssen Pharmaceutica NV
    Inventors: Pieter Rik Haspeslagh, Maarten Vliegen, Eric Hryhorenko, Thomas R. DeCory, Banumathi Sankaran
  • Patent number: 9012647
    Abstract: Disclosed are nitroxide modified NSAID compounds of the formula (I) or a pharmaceutically acceptable salt or enantiomer thereof: in which R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, and n are defined herein and pharmaceutical compositions thereof. Further disclosed is a method of treating or preventing various disorders, such as inflammation, cancer, diabetes, a cardiovascular disorder, weight gain, polyps, and/or chronic pain, in a patient comprising administering an effective amount of a compound or pharmaceutically acceptable salt or enantiomer of formula (I). A method of imaging the compound or pharmaceutically acceptable salt or enantiomer of formula (I) in the body of the animal is also provided.
    Type: Grant
    Filed: April 5, 2012
    Date of Patent: April 21, 2015
    Assignees: The United States of America, as Represented by the Secretary, Department of Health and Human Services, Wake Forest University
    Inventors: David A. Wink, Wilmarie Flores-Santana, S. Bruce King, Murali Krishna Cherukuri, James B. Mitchell
  • Publication number: 20150083223
    Abstract: A fullerene derivative represented by the following formula (1): wherein “FLN” represents a fullerene core, R1 represents an optionally substituted C1-C24 alkyl group or an optionally substituted C7-C24 aralkyl group, R2 and R3 independently represent a hydrogen atom or an optionally substituted C1-C24 hydrocarbon group but excluding a case where both of R2 and R3 are hydrogen atoms, and R2 and R3 may combine together to form a ring.
    Type: Application
    Filed: September 25, 2013
    Publication date: March 26, 2015
    Applicants: Tohoku University, Showa Denko K.K.
    Inventors: Tienan JIN, Weili Si, Yoshinori Yamamoto, Takeshi Igarashi
  • Publication number: 20150087841
    Abstract: A method of synthesizing a crystalline molecular sieve having an MSE framework type comprises crystallizing a reaction mixture comprising a source of water, a source of an oxide of a tetravalent element, Y, selected from at least one of silicon, tin, titanium, vanadium, and germanium, optionally a source of a trivalent element, X, a source of an alkali or alkaline earth metal, M, and a source of organic dications, Q, such as 3-hydroxy-1-(4-(1-methylpiperidin-1-ium-1-yl)butyl)quinuclidin-1-ium, 3-hydroxy-1-(5-(1-methylpiperidin-1-ium-1-yl)pentyl)quinuclidin-1-ium, 1,1?-(butane-1,4-diyl)bis(1-methylpiperidin-1-ium), 1,1?-(pentane-1,5-diyl)bis(1-methylpiperidin-1-ium), 1,1?-(hexane-1,6-diyl)bis(1-methylpiperidin-1-ium), and 1,1?-((3as,6as)-octahydropentalene-2,5-diyl)bis(1-methylpiperidin-1-ium).
    Type: Application
    Filed: November 14, 2014
    Publication date: March 26, 2015
    Applicant: ExxonMobil Research and Engineering Company
    Inventors: Simon C. Weston, Karl G. Strohmaier, Hilda B. Vroman
  • Patent number: 8987303
    Abstract: Disclosed are substituted pyridine compounds as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure wherein E, J, T, the ring system denoted by “B”, T, R3, R4, w and x are as described herein. In certain embodiments, a compound disclosed herein activates the AMPK pathway, and can be used to treat metabolism-related disorders and conditions.
    Type: Grant
    Filed: March 13, 2013
    Date of Patent: March 24, 2015
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Dane Goff, Donald Payan, Rajinder Singh, Simon Shaw, David Carroll, Yasumichi Hitoshi
  • Patent number: 8981119
    Abstract: The present invention is directed to compounds of Formula I: wherein R1, R2, R3, R4, R5, X and n are described herein. These compounds and their pharmaceutically acceptable salts thereof are useful as IK1 channel activators.
    Type: Grant
    Filed: June 6, 2014
    Date of Patent: March 17, 2015
    Assignee: Astellas Pharma Inc.
    Inventors: Tsukasa Ishihara, Kazuhiro Ikegai, Ikumi Kuriwaki, Hiroyuki Hisamichi, Nobuaki Takeshita, Ryuichi Takezawa
  • Patent number: 8980921
    Abstract: Disclosed are substituted pyridine compounds as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure wherein E, J, T, the ring system denoted by “B”, T, R3, R4, w and x are as described herein. In certain embodiments, a compound disclosed herein activates the AMPK pathway, and can be used to treat metabolism-related disorders and conditions.
    Type: Grant
    Filed: March 13, 2013
    Date of Patent: March 17, 2015
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Dane Goff, Donald Payan, Rajinder Singh, Simon Shaw, David Carroll, Yasumichi Hitoshi
  • Patent number: 8962845
    Abstract: Compounds of formula (I): wherein R1, R2, R3, R4, R5, and X are defined herein. Also disclosed are pharmaceutical compositions and methods related to use of these compounds.
    Type: Grant
    Filed: September 25, 2012
    Date of Patent: February 24, 2015
    Assignee: National Health Research Institutes
    Inventors: Kak-Shan Shia, Chun-Ping Chang, Yu-Sheng Chao
  • Publication number: 20150025245
    Abstract: The present application relates to a process for preparing chloroamines which can be used as precursors for syntheses of fine chemicals and active ingredients from pharmaceuticals and/or agriculture, by reaction of secondary amines of the formula (II) with chlorine gas in the presence of an aqueous alkali metal or alkaline earth metal oxide base.
    Type: Application
    Filed: February 13, 2013
    Publication date: January 22, 2015
    Inventor: Mark James Ford
  • 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
  • Patent number: 8933223
    Abstract: A process for preparing a cyclic tertiary amine of the formula I where A is a C4-alkylene group, a C5-alkylene group or a —(CH2)2—B—(CH2)2— group, where B is oxygen (O) or an N—R1 radical and R1 is C1-C5-alkyl, aryl or C5-C7-cycloalkyl, and the radical R2 is a linear or branched C2-C16-alkyl, C5-C7-cycloalkyl or C7-C20-aralkyl, in which (i) an amino alcohol II from the group consisting of 1,4-aminobutanol, 1,5-aminopentanol, aminodiglycol (ADG) and aminoethylethanolamine of the formula IIa where R1 is as defined above or hydrogen (H), in which case R1=R2 in the amine I, is reacted with a primary or secondary alcohol R2OH (III) at a temperature in the range from 150 to 270° C. in the liquid phase in the presence of a copper-comprising heterogeneous catalyst in a reactor.
    Type: Grant
    Filed: October 14, 2011
    Date of Patent: January 13, 2015
    Assignee: BASF SE
    Inventors: Christof Wilhelm Wigbers, Johann-Peter Melder, Bernd Stein, Harald Meiβner
  • Publication number: 20140377667
    Abstract: The invention relates to lithium-2-methoxy-1,1,2,2-tetrafluoro-ethanesulfonate, to the use thereof as conductive salt in lithium-based energy accumulators, and ionic liquids comprising 2-methoxy-1,1,2,2-tetrafluoro-ethanesulfonate as an anion.
    Type: Application
    Filed: July 25, 2012
    Publication date: December 25, 2014
    Applicants: JACOBS UNIVERSITY BREMEN gGMBH, WESTFALISCHE WILHELMS UNIVERSITAT MUNSTER
    Inventors: Gerd-Volker Roschenthaler, Martin Winter, Katja Vlasov, Nataliya Kalinovich, Christian Schreiner, Raphael Wilhelm Schmitz, Romek Ansgar Muller, Rene Schmitz, Alexandra Lex-Balducci, Miriam Kunze
  • Publication number: 20140370441
    Abstract: An aqueous solution containing 0.1-20 wt % of a cyclic ammonium hydroxide is a useful developer for photosensitive resist materials. A resist pattern is formed by applying a chemically amplified positive resist composition onto a substrate to form a resist film, exposing the resist film to high-energy radiation, and developing the exposed resist film in a cyclic ammonium hydroxide-containing aqueous solution.
    Type: Application
    Filed: May 27, 2014
    Publication date: December 18, 2014
    Applicant: SHIN-ETSU CHEMICAL CO., LTD.
    Inventors: Jun Hatakeyama, Masaki Ohashi
  • Publication number: 20140371293
    Abstract: The present invention relates to lipid compounds and uses thereof. In particular, the compounds include a class of cationic lipids having an amine moiety, such as an amino-amine or an amino-amide moiety. The lipid compounds are useful for in vivo or in vitro delivery of one or more agents (e.g., a polyanionic payload or an antisense payload, such as an RNAi agent).
    Type: Application
    Filed: April 17, 2014
    Publication date: December 18, 2014
    Applicant: Dicerna Pharmaceuticals, Inc.
    Inventors: Bob Dale Brown, Sujit Kumar Basu, David A. Schwartz, Allister Fraser
  • Patent number: 8912219
    Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, n, p, q, r, A, X1, X2, X3, X4, X5, X6, Y, Z, G, R1a, R2a, R1b, R2b, R3, R4, R5 and R6 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis.
    Type: Grant
    Filed: March 14, 2014
    Date of Patent: December 16, 2014
    Assignee: Genentech, Inc.
    Inventors: Benjamin Fauber, Olivier Rene, Monique Bodil van Niel, Stuart Ward
  • Publication number: 20140335079
    Abstract: This disclosure relates to solenopsin derivatives, pharmaceutical compositions, and therapeutic uses related thereto. In certain embodiments, the disclosure relates to compounds of the following formula: or salts, esters or prodrugs thereof as described herein.
    Type: Application
    Filed: May 7, 2014
    Publication date: November 13, 2014
    Applicants: EMORY UNIVERSITY, UNION UNIVERSITY, MERCER UNIVERSITY
    Inventors: Jack L. Arbiser, J. Philip Bowen, E. Blake Watkins
  • Patent number: 8865886
    Abstract: An effluent produced in oxidation of a cellulosic material with an oxidizing agent in the presence of an N-oxyl compound and a bromide and/or iodide is deionized by electrodialysis to an inorganic salt concentration of less than 0.4%, whereby the N-oxyl compound in the effluent is concentrated and recovered. The N-oxyl compound thus recovered can be reused in oxidation of a cellulosic material. Preferably, the effluent is subjected to reduction treatment and ion exchange resin treatment prior to the electrodialysis.
    Type: Grant
    Filed: February 16, 2010
    Date of Patent: October 21, 2014
    Assignee: Nippon Paper Industries Co., Ltd.
    Inventors: Shoichi Miyawaki, Shiho Katsukawa, Hiroshi Abe, Yuko Iijima, Akira Isogai
  • Publication number: 20140309114
    Abstract: Amine salts of certain herbicides that in free acid form include at least one carboxylic acid moiety are described. Herbicide salts comprising the cation of various imidazole, piperazine, piperidine, and morpholine compounds are provided. The herbicide amine salts described are suitable for formulation into herbicidal application mixtures and/or stable concentration compositions that exhibit acceptable volatility characteristics upon application.
    Type: Application
    Filed: October 26, 2012
    Publication date: October 16, 2014
    Applicant: MONSANTO TECHNOLOGY LLC
    Inventors: Junhua Zhang, Daniel R. Wright, William Abraham
  • Patent number: 8846929
    Abstract: The invention relates to Substituted-Quinoxaline-Type Piperidine Compounds, compositions comprising an effective amount of a Substituted-Quinoxaline-Type Piperidine Compound and methods to treat or prevent a condition, such as pain, comprising administering to an animal in need thereof an effective amount of a Substituted-Quinoxaline-Type Piperidine Compound.
    Type: Grant
    Filed: February 24, 2010
    Date of Patent: September 30, 2014
    Assignees: Purdue Pharma L.P., Shionogi & Co., Ltd.
    Inventors: Kouki Fuchino, R. Richard Goehring, Bin Shao, Yoshiyuki Taoda, Naoki Tsuno, John William Frank Whitehead, Jiangchao Yao
  • Patent number: 8841325
    Abstract: Provided herein are methods of restoring vitamin D sensitivity in tumor cells that are vitamin D resistant. Also provided are methods of treating, preventing or managing cancer using an immunomodulatory compound in combination with a vitamin D agent. Pharmaceutical compositions and single unit dosage forms suitable for use in the methods provided herein are also disclosed.
    Type: Grant
    Filed: November 24, 2010
    Date of Patent: September 23, 2014
    Assignee: Celgene Corporation
    Inventors: Carole Brosseau, Justin Blake Bartlett, Angus George Dalgleish, Kay Winifred Colston, Christine Galustian
  • Patent number: 8829192
    Abstract: Described is the use of specific merocyanine derivatives for protecting body-care and household products from photolytic and oxidative degradation. These compounds perform outstanding UV absorber properties.
    Type: Grant
    Filed: July 19, 2006
    Date of Patent: September 9, 2014
    Assignee: BASF SE
    Inventors: Barbara Wagner, Oliver Reich
  • Patent number: 8815775
    Abstract: Bis(difluoromethyl)pyrazole derivatives of the formula (I) in which the symbols R1, X, Y and Q are each as defined in the description, and agrochemically active salts thereof, and use thereof for controlling phytopathogenic harmful fungi, and also processes for preparing compounds of the formula (I).
    Type: Grant
    Filed: May 16, 2011
    Date of Patent: August 26, 2014
    Assignee: Bayer CropScience AG
    Inventors: Pierre Cristau, Sebastian Hoffmann, Joachim Kluth, Thomas Seitz, Tomoki Tsuchiya, Pierre Wasnaire, Jürgen Benting, Ulrike Wachendorff-Neumann
  • Patent number: 8809370
    Abstract: Disclosed are substituted pyridine compounds as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure wherein E, J, T, the ring system denoted by “B”, T, R3, R4, w and x are as described herein. In certain embodiments, a compound disclosed herein activates the AMPK pathway, and can be used to treat metabolism-related disorders and conditions.
    Type: Grant
    Filed: March 13, 2013
    Date of Patent: August 19, 2014
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Dane Goff, Donald Payan, Rajinder Singh, Simon Shaw, David Carroll, Yasumichi Hitoshi
  • Patent number: 8791136
    Abstract: Disclosed are substituted pyridine compounds as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure wherein E, J, T, the ring system denoted by “B”, T, R3, R4, w and x are as described herein. In certain embodiments, a compound disclosed herein activates the AMPK pathway, and can be used to treat metabolism-related disorders and conditions.
    Type: Grant
    Filed: July 29, 2011
    Date of Patent: July 29, 2014
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Dane Goff, Donald Payan, Rajinder Singh, Simon Shaw, David Carroll, Yasumichi Hitoshi
  • Patent number: 8791135
    Abstract: Novel compounds and compositions for treating patients in need of relief from HIV, AIDS, and AIDS-related diseases are described. Methods for treating HIV, AIDS, and AIDS-related diseases using the compounds described herein are also described.
    Type: Grant
    Filed: July 1, 2009
    Date of Patent: July 29, 2014
    Assignee: Purdue Research Foundation
    Inventor: Arun K. Ghosh
  • Patent number: 8778969
    Abstract: Nitrone, nitroso, and nitroxide spintraps and spin labels and their reduction products are claimed for the prevention and treatment of fibrocystic disease of breast, premenstrual dysphoric syndrome and associated symptomology, prevention and treatment of migraine headache, cyclic vomiting syndrome, rectal hemorrhoids, trigeminal neuralgia, peripheral vascular disease, influenza, peridontitis and gingivitis, herpes zoster, herpes simplex, and post-herpetic neuralgia.
    Type: Grant
    Filed: November 7, 2010
    Date of Patent: July 15, 2014
    Inventor: Peter H Proctor
  • Patent number: 8772318
    Abstract: This invention provides compounds that selectively inhibit monoacylglycerol lipase (MAGL). The invention also provides methods of using the MAGL selective inhibitors to stimulate 2-Arachidonoylglycerol (2-AG) mediated endocannabinoid signaling in vivo, and to treat conditions that are associated with or linked to endocannabinoid signaling. The invention additionally provides methods of treating cancer or inhibiting tumor growth by targeting MAGL with MAGL specific inhibitors. The invention further provides methods of screening for MAGL inhibitors with improved biochemical and pharmaceutical properties.
    Type: Grant
    Filed: November 10, 2009
    Date of Patent: July 8, 2014
    Assignee: The Scripps Research Institute
    Inventors: Benjamin F. Cravatt, Jonathan Z. Long, Weiwei Li, Daniel K. Nomura
  • Patent number: 8765959
    Abstract: Piperidine derivatives of which the following is exemplary and their use in the treatment of obesity, diabetes or dyslipidemia.
    Type: Grant
    Filed: December 14, 2012
    Date of Patent: July 1, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Gerald Juergen Roth, Martin Fleck, Bernd Nosse, Thorsten Lehmann-Lintz
  • Patent number: 8748613
    Abstract: Compounds of formula (I): wherein A, R1, R2, X, m, and n are as defined in the specification, are selective M3 receptor antagonists and may be used in the treatment of, inter alia, a respiratory disease such as asthma and COPD.
    Type: Grant
    Filed: December 28, 2012
    Date of Patent: June 10, 2014
    Assignee: Chiesi Farmaceutici S.p.A.
    Inventors: Gabriele Amari, Cristina Pesenti, Stefano Bossolo
  • Patent number: 8716527
    Abstract: Methods of treating or suppressing oxidative stress diseases including mitochondrial diseases, impaired energy processing disorders, neurodegenerative diseases and diseases of aging are disclosed, as well as compounds useful in the methods of the invention, such as 2- substituted-p-quinone derivatives as disclosed herein.
    Type: Grant
    Filed: March 4, 2009
    Date of Patent: May 6, 2014
    Assignee: Edison Pharmaceuticals, Inc.
    Inventors: Andrew W. Hinman, Kieron E. Wesson, Orion D. Jankowski, Paul Mollard, William D. Shrader, Christopher R. Cornell