Chalcogen Bonded Directly To Ring Carbon Of The Piperidine Ring Patents (Class 546/242)
  • Patent number: 10370331
    Abstract: Disclosed herein are compositions including between 20 wt % and 50 wt % of a nitroxyl compound such as 2,2,6,6-tetramethylpiperidinyl-1-oxyl. The compositions are stable under field conditions of transportation and storage. The compositions remain homogeneous and pumpable or pourable at temperatures between ?20° C. and 60° C., even when temperatures fluctuate in this range over a period of 10 days to 5 years, and even where the container used to transport and store the composition is made from metal or includes a metal surface contacting the composition.
    Type: Grant
    Filed: March 8, 2018
    Date of Patent: August 6, 2019
    Assignee: Ecolab USA Inc.
    Inventors: Jonathan Masere, Javier Florencio, Ramon Colorado, Jr., Andrew R. Neilson, David Youdong Tong
  • Patent number: 9914701
    Abstract: The present invention generally relates to compounds and methods for inhibiting the radical polymerization of unsaturated compounds, particularly vinyl monomers. More particularly, it relates to the use of stable hydroxyl amines to inhibit the polymerization of unsaturated compounds (e.g., vinyl monomers) wherein said stable hydroxylamine is soluble in organic solvents, particularly hydrocarbon solvents consisting of unsaturated and, therefore, polymerizable constituents.
    Type: Grant
    Filed: March 17, 2016
    Date of Patent: March 13, 2018
    Assignee: Ecolab USA Inc.
    Inventors: Jonathan Masere, Andrew R. Neilson, Russell P. Watson
  • Patent number: 9566316
    Abstract: Described herein are variant, recombinant ?-glucocerebrosidase proteins characterized as having increased stability relative to recombinant wild-type ?-glucocerebrosidase. Also provided herein are variant, recombinant ?-glucocerebrosidase proteins characterized as retaining more catalytic activity relative to recombinant wild-type ?-glucocerebrosidase. Further described herein are variant, recombinant ?-glucocerebrosidase proteins that can have amino acid variations at one or more of the following positions: 316, 317, 321 and 145. Methods of making the variant, recombinant ?-glucocerebrosidase proteins are also described as well as methods of treating patients having lysosomal storage diseases.
    Type: Grant
    Filed: January 4, 2016
    Date of Patent: February 14, 2017
    Assignee: AMICUS THERAPEUTICS, INC.
    Inventor: Hung V. Do
  • Patent number: 9217000
    Abstract: A compound having a structure of:
    Type: Grant
    Filed: February 17, 2012
    Date of Patent: December 22, 2015
    Assignee: Univerisyt of Pittsburgh—of the Commonwealth System of Higher Education
    Inventors: Peter Wipf, Marie-Celine Frantz
  • Patent number: 9199935
    Abstract: Compounds of formula (I): wherein R represents various substituent groups, are useful as inhibitors of glucosylceramide synthase.
    Type: Grant
    Filed: April 7, 2014
    Date of Patent: December 1, 2015
    Assignee: Acetelion Pharmaceuticals Ltd.
    Inventors: Terence D. Butters, Raymond A. Dwek, George W. J. Fleet, Michael Glen Orchard, Frances Mary Platt
  • Patent number: 9150557
    Abstract: The invention relates to the compounds of formula I or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I, and methods for the treatment of hyperglycemia may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of insulin resistance, diabetes mellitus, diabetes insipidus, type 1 diabetes, type 2 diabetes, microvascular complications, macrovascular complications, lipid disorders, prediabetes, obesity, arrhythmia, myocardial infarction, stroke, neuropathy, renal complications, hypertriglyceridemia, cardiovascular complications, and post prandial hyperglycemia.
    Type: Grant
    Filed: November 5, 2014
    Date of Patent: October 6, 2015
    Assignee: CELLIX BIO PRIVATE LIMITED
    Inventor: Mahesh Kandula
  • Patent number: 9035062
    Abstract: A process for preparing the compound of the following formula (E): wherein Bn represents a benzyl group, and tBu represents a tert-butyl group, the process including: (a) subjecting the following compound (B) to trifluoroacetylation, wherein tBu represents a tert-butyl group to produce the following compound (C): wherein tBu represents a tert-butyl group, and TFA represents a trifluoroacetyl group; (b) reacting the compound (C) with benzyloxyamine in the presence of a hydroxyl group activating agent to produce the following compound (D): wherein Bn represents a benzyl group, tBu represents a tert-butyl group, and TFA represents a trifluoroacetyl group; and (c) subjecting the compound (D) to detrifluoroacetylation.
    Type: Grant
    Filed: May 27, 2014
    Date of Patent: May 19, 2015
    Assignee: MEIJI SEIKA PHARMA CO., LTD.
    Inventors: Takao Abe, Masayuki Okue, Yoshiaki Sakamaki
  • Publication number: 20150133431
    Abstract: This invention relates to geranylgeranyl acetone (GGA) derivatives, pharmaceutical compositions comprising GGA derivatives and the use of GGA derivatives.
    Type: Application
    Filed: July 10, 2014
    Publication date: May 14, 2015
    Applicant: COYOTE PHARMACEUTICALS, INC.
    Inventor: Gary C. Look
  • Publication number: 20150126528
    Abstract: The present invention provides a compound, solid forms, and compositions thereof, which are useful as inhibitors of Bruton's tyrosine kinase and which exhibit desirable characteristics for the same. The present invention also provides methods of making provided compound and solid forms.
    Type: Application
    Filed: June 7, 2013
    Publication date: May 7, 2015
    Inventors: Brian T. Hopkins, Xiongwei Cai, Timothy R. Chan, Patrick Conlon, Michael Humora, Tracy J. Jenkins, Michael J. Macphee, Xianglin Shi, Ross A. Miller, Andrew Thompson
  • Publication number: 20150087823
    Abstract: The present invention relates to a novel trans-2-decenoic acid derivative or a pharmaceutically acceptable salt thereof, and a pharmaceutical agent containing the compound as an active ingredient. The trans-2-decenoic acid derivative or a pharmaceutically acceptable salt, which is the compound of the present invention, is specifically represented by the general formula (I): wherein X is a substituent such as a 1-pyrrolidyl, a 3-thiazolizyl, or a piperidino, and the compound is highly useful as a pharmaceutical agent, such as a prophylactic or therapeutic agent for a peripheral nerve disorder induced by administration of an anticancer agent, a prophylactic or therapeutic agent for neurodegenerative diseases or mental diseases such as dementia, Alzheimer's disease, Parkinson's disease, diabetic neuropathy, depression, glaucoma, or autistic disorder spectrum, a therapeutic or repairing agent for spinal cord injury, analgesics against various pain diseases, or the like.
    Type: Application
    Filed: April 26, 2013
    Publication date: March 26, 2015
    Inventors: Munekazu Iinuma, Shoei Furukawa, Mitsuru Naiki, Tomonori Matsumoto, Kunihiko Higashiura
  • Patent number: 8980923
    Abstract: The present invention concerns methods for treating or preventing neurological disorders characterized by dysfunction of nicotinic acetylcholine receptors by administering 2,2,6,6-tetramethylpiperidin-4-yl heptanoate (TMPH), or a pharmaceutically acceptable salt thereof, to the patient. In another aspect, the present invention pertains to pharmaceutical compositions containing TMPH, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier. In another aspect, the present invention pertains to methods for selectively inhibiting nicotinic acetylcholine receptors that lack an ?5, ?6, or ?3 subunit by contacting an effective amount of TMPH, or a pharmaceutically acceptable salt thereof, to the receptor. The method for selectively inhibiting nicotinic acethylcholine receptors that lack an ?5 subunit can be carried out in vivo or in vitro.
    Type: Grant
    Filed: June 18, 2012
    Date of Patent: March 17, 2015
    Assignee: University of Florida Research Foundation, Inc.
    Inventors: Roger L. Papke, Nicole A. Horenstein, Michael M. Francis, Kyung Il Choi
  • Publication number: 20150050263
    Abstract: Described are novel salts of the compound (3R,4R,5S)-5-(difluoromethyl) piperidine-3,4-diol, as well as methods of using the same for preventing and/or treating lysosomal storage disorders and/or degenerative disorders of the central nervous system. In particular, the present invention provides methods for preventing and/or treating Gaucher's disease and/or Parkinson's disease.
    Type: Application
    Filed: March 7, 2013
    Publication date: February 19, 2015
    Inventors: Robert Boyd, Philip J. Rybczynski, Kamlesh Sheth
  • Publication number: 20150045367
    Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which inhibit the activity of histone deacetylase 8 (HDAC8). Also described herein are methods of using such HDAC8 inhibitors, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of HDAC8 activity.
    Type: Application
    Filed: December 19, 2012
    Publication date: February 12, 2015
    Inventors: Erik Verner, Wei Chen, Sriram Balasubramanian
  • Publication number: 20150031879
    Abstract: The present invention relates to novel processes for the preparation of sterically hindered amine ethers by the transformation of a corresponding oxo-piperidin to a hydroxy or amino substituted sterically hindered amine ether and the preparation of a N-propoxy or N-propenoxy substituted sterically hindered amine and some novel compounds obtainable by these processes. The compounds made by these processes are particularly effective in the stabilization of polymer compositions against harmful effects of light, oxygen and/or heat and as flame-retardants for polymers.
    Type: Application
    Filed: October 14, 2014
    Publication date: January 29, 2015
    Applicant: BASF SE
    Inventors: Markus FREY, Valerie Rast, Francisco Martinez, Davide Alvisi
  • Patent number: 8940766
    Abstract: The present invention provides methods for preventing and/or treating lysosomal storage disorders using 5-(fluoromethyl)piperidine-3,4-diol, 5-(chloromethyl)piperidine-3,4-diol, or a pharmaceutically acceptable salt, solvate, or prodrug thereof, or any combination of two or more thereof. In particular, the present invention provides methods for preventing and/or treating Gaucher's disease.
    Type: Grant
    Filed: April 9, 2010
    Date of Patent: January 27, 2015
    Assignee: Amicus Therapeutics, Inc.
    Inventors: Robert Boyd, Gary Lee
  • Patent number: 8937086
    Abstract: The present invention relates to methods of inhibiting one or more signs of aging and/or degenerative disorder in a subject in need of such treatment, which comprise administering, to the subject, an effective amount of one or more of the compounds as set forth herein. “Inhibiting a sign of aging or degenerative disorder” means reducing the risk of occurrence, delaying the onset, slowing the progression, and/or reducing the severity and/or manifestation, of a sign of aging or degenerative disorder, and includes, but is not limited to, preventing the occurrence, development or progression of a sign of aging or degenerative disorder.
    Type: Grant
    Filed: January 14, 2011
    Date of Patent: January 20, 2015
    Assignee: University of Pittsburgh—Of the Commonwealth System of Higher Education
    Inventors: Laura J. Niedernhofer, Paul D. Robbins, Peter Wipf
  • Patent number: 8927557
    Abstract: The compounds of Formula (I), wherein R1, R2, R21, R22, R23, R24, Y and R3 have the meanings as given in the description, the salts thereof, the stereoisomers of the compounds and the salts thereof are effective inhibitors of the type 5 phosphodiesterase.
    Type: Grant
    Filed: August 24, 2010
    Date of Patent: January 6, 2015
    Assignee: Takeda GmbH
    Inventors: Josef Stadlwieser, Beate Schmidt, Heiko Bernsmann, Torsten Dunkern, Ewald Benediktus, Andreas Pahl, Ragna Hussong, Olaf Nimz, Matthias Mueller, Martin Viertelhaus
  • Publication number: 20140363634
    Abstract: Ink contains at least one of a compound represented by the following chemical formula 1, a compound represented by chemical formula 2, a compound represented by chemical formula 3, or a compound represented by chemical formula 4.
    Type: Application
    Filed: May 27, 2014
    Publication date: December 11, 2014
    Inventors: Mitsunobu MORITA, Soh NOGUCHI, Okitoshi KIMURA
  • Publication number: 20140336137
    Abstract: The invention relates to nitroso derivatives including carboxylic acid and phosphoric acid esters of hydroxy nitroso compounds that donate nitroxyl (HNO) under physiological conditions. The compounds and compositions of the invention are useful in treating and/or preventing the onset and/or development of diseases or conditions that are responsive to nitroxyl therapy, including heart failure, ischemia/reperfusion injury and cancer.
    Type: Application
    Filed: July 28, 2014
    Publication date: November 13, 2014
    Inventors: Lisa Marie Frost, Stephen Martin Courtney, Frederick Arthur Brookfield, Vincent Jacob Kalish
  • 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
  • Publication number: 20140309258
    Abstract: Compositions comprising isolated ido-BR1 are described for use in therapy or prophylaxis, including the treatment of inflammatory diseases (for example as anti-inflammatory drugs) and to reduce inflammation. Also described are methods for monitoring the quality of a Cucurbitaceae extract, to processes for producing a Cucurbitaceae extract as well as to Cucurbitaceae extracts obtainable by such processes.
    Type: Application
    Filed: April 11, 2014
    Publication date: October 16, 2014
    Applicant: Phytoquest Limited
    Inventor: Robert James Nash
  • Publication number: 20140303208
    Abstract: Compounds of formula (I): wherein R represents various substituent groups, are useful as inhibitors of glucosylceramide synthase.
    Type: Application
    Filed: April 7, 2014
    Publication date: October 9, 2014
    Applicant: Actelion Pharmaceuticals Ltd.
    Inventors: Terence D. BUTTERS, Raymond A. DWEK, George W. J. FLEET, Michael Glen ORCHARD, Frances Mary PLATT
  • Publication number: 20140303375
    Abstract: A process for preparing the compound of the following formula (E): wherein Bn represents a benzyl group, and tBu represents a tert-butyl group, the process including: (a) subjecting the following compound (B) to trifluoroacetylation, wherein tBu represents a tert-butyl group to produce the following compound (C): wherein tBu represents a tert-butyl group, and TFA represents a trifluoroacetyl group; (b) reacting the compound (C) with benzyloxyamine in the presence of a hydroxyl group activating agent to produce the following compound (D): wherein Bn represents a benzyl group, tBu represents a tert-butyl group, and TFA represents a trifluoroacetyl group; and (c) subjecting the compound (D) to detrifluoroacetylation.
    Type: Application
    Filed: May 27, 2014
    Publication date: October 9, 2014
    Applicant: Meiji Seika Pharma. Co., Ltd.
    Inventors: Takao ABE, Masayuki OKUE, Yoshiaki SAKAMAKI
  • Publication number: 20140296288
    Abstract: The present disclosure relates to iminosugar derivatives and processes for the preparation thereof. The disclosed compounds have glycosidase inhibiting properties, and are useful in the treatment of various diseases, such as type 2 diabetes, neurodegenerative diseases or lysosomal storage disorders. The present disclosure also relates to pharmaceutical compositions containing the disclosed compounds and to their use as biochemical tools.
    Type: Application
    Filed: July 19, 2012
    Publication date: October 2, 2014
    Applicants: UNIVERSITE PIERRE ET MARIE CURIE (PARIS 6), DORPHAN S.A., CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE
    Inventors: Matthieu Sollogoub, Yves Bleriot, Giuseppe Prencipe, Nicolas Auberger
  • Publication number: 20140288081
    Abstract: Compounds of general formula I: and compositions comprising compounds of general formula I that modulate pyruvate kinase are described herein. Also described herein are methods of using the compounds that modulate pyruvate kinase in the treatment of diseases.
    Type: Application
    Filed: March 14, 2014
    Publication date: September 25, 2014
    Applicant: AGIOS PHARMACEUTICALS, INC
    Inventors: Giovanni Cianchetta, Janeta Popovici-Muller, Robert Zahler, Sheldon Cao, Xiaolei Wang, Zhixiong Ye
  • Publication number: 20140205666
    Abstract: Iminosugar, which possesses known activity as a glycosyltransferase inhibitor, and is used, for example, in the treatment of Gaucher's disease, in crystalline form, a process for its preparation and a pharmaceutical composition thereof.
    Type: Application
    Filed: January 7, 2014
    Publication date: July 24, 2014
    Applicant: DIPHARMA FRANCIS S.r.I.
    Inventors: Emanuele ATTOLINO, Andrea MALVESTITI
  • Publication number: 20140203226
    Abstract: A photochromic curable composition that contains a (meth)acrylate compound represented by the following formula (1-X1); (wherein Y is an oxygen atom or a divalent group represented by —NH—, R1 and R2 are hydrogen atoms or methyl groups, R3 is an alkylene group having 1 to 6 carbon atoms, R4 is an alkylene group having 1 to 6 carbon atoms, a cycloalkylene group having 3 to 8 carbon atoms and which may include a double bond, or an arylene group having 6 to 10 carbon atoms, and a is a positive number of 1 to 20), other radically polymerizable monomers and a photochromic compound. The invention provides a lens that features excellent durability and high photochromic property free of the problems of turbidity in the surfaces of the lens caused by bleed out or the peeling in the step of production.
    Type: Application
    Filed: October 15, 2012
    Publication date: July 24, 2014
    Applicant: Tokuyama Corporation
    Inventors: Junji Takenaka, Junji Momoda
  • Patent number: 8785402
    Abstract: Methods of diagnosing Helicobacter pylori infection or associated conditions are based in part on the correlation of the presence of a ?-L-fucosidase 2 marker with the infection. Methods and compositions for treating or preventing Helicobacter pylori infection or associated conditions are based in part on administering an ?-L-fucosidase 2 inhibitor to an infected subject or a subject at risk of developing the infection.
    Type: Grant
    Filed: August 2, 2010
    Date of Patent: July 22, 2014
    Assignee: Academia Sinica
    Inventors: Chun-Hung Lin, Ta-Wei Liu
  • 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: 8772490
    Abstract: Provided are an optically active diazabicyclooctane derivative defined by formula (F) below, which is useful as a pharmaceutical intermediate for ?-lactamase inhibitor, and a process for preparing the same. In formula (F) above, R1 represents CO2R, CO2M, or CONH2, wherein R represents a methyl group, a tert-butyl group, an allyl group, a benzyl group, or a 2,5-dioxopyrrolidin-1-yl group, and M represents a hydrogen atom, an inorganic cation, or an organic cation; and R2 represents a benzyl group or an allyl group.
    Type: Grant
    Filed: June 30, 2011
    Date of Patent: July 8, 2014
    Assignee: Meiji Seika Pharma Co., Ltd.
    Inventors: Takao Abe, Masayuki Okue, Yoshiaki Sakamaki
  • Publication number: 20140086896
    Abstract: The present invention provides novel compositions as well as methods for preventing and/or treating lysosomal storage disorders. In particular, the present invention provides methods for preventing and/or treating Gaucher's disease.
    Type: Application
    Filed: November 19, 2013
    Publication date: March 27, 2014
    Applicant: AMICUS THERAPEUTICS, INC.
    Inventors: Robert Boyd, Gary Lee, Philip Rybczynski
  • Publication number: 20140080871
    Abstract: The present invention provides novel compounds as well as compositions and methods using the same for preventing and/or treating degenerative disorders of the central nervous system. In particular, the present invention provides methods for preventing and/or treating Parkinson's disease.
    Type: Application
    Filed: November 19, 2013
    Publication date: March 20, 2014
    Applicant: AMICUS THERAPEUTICS, INC.
    Inventors: Robert Boyd, Gary Lee, Philip Rybczynski
  • Patent number: 8642622
    Abstract: The present application describes the compound of formula (I): or stereoisomers or pharmaceutically acceptable salts thereof. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and arthrosclerosis using the compound of the invention are disclosed.
    Type: Grant
    Filed: June 15, 2011
    Date of Patent: February 4, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: Robert J. Cherney, John V. Duncia, Daniel S. Gardner, Joseph B. Santella, Zhongyu Wang
  • Publication number: 20130338110
    Abstract: The inventions disclosed include methods of treating cancers and related neoplasias, especially prostate cancer, with pharmaceutically acceptable salts comprising lipophilic cation moieties linked to nitroxide or linked to hydroxylamine anti-oxidant groups.
    Type: Application
    Filed: May 20, 2013
    Publication date: December 19, 2013
    Inventors: David A. ZARLING, Hirak S. BASU, Balaraman KALYANARAMAN, Joy JOSEPH
  • Patent number: 8609850
    Abstract: Provided herein are compositions and related methods useful for free radical scavenging, with particular selectivity for mitochondria. The compounds comprise a nitroxide-containing group attached to a mitochondria-targeting group. The compounds can be cross-linked into dimers without loss of activity. Also provided herein are methods, for preventing, mitigating and treating damage caused by radiation. The method comprises delivering a compound, as described herein, to a patient in an amount and dosage regimen effective to prevent, mitigate or treat damage caused by radiation.
    Type: Grant
    Filed: September 14, 2012
    Date of Patent: December 17, 2013
    Assignee: University of Pittsburgh—Of the Commonwealth System of Higher Education
    Inventors: Peter Wipf, Marie Celine Frantz
  • Patent number: 8603947
    Abstract: A description is given of (4-haloalkyl-3-thiobenzoyl)cyclohexanediones of the formula (I) and of their use as herbicides. In this formula (I), X, Y, R1, R2, R3, and R4 are radicals such as hydrogen and organic radicals such as alkyl. A and Z are oxygen or alkylene.
    Type: Grant
    Filed: July 20, 2011
    Date of Patent: December 10, 2013
    Assignee: Bayer Cropscience AG
    Inventors: Hartmut Ahrens, Dieter Feucht, Elmar Gatzweiler, Isolde Haeuser-Hahn, Christopher Hugh Rosinger
  • Patent number: 8604206
    Abstract: The present invention provides novel compounds as well as compositions and methods using the same for preventing and/or treating degenerative disorders of the central nervous system. In particular, the present invention provides methods for preventing and/or treating Parkinson's disease.
    Type: Grant
    Filed: October 5, 2010
    Date of Patent: December 10, 2013
    Assignee: Amicus Therapeutics, Inc.
    Inventors: Robert Boyd, Gary Lee, Philip Rybczynski
  • Publication number: 20130302728
    Abstract: The present invention relates to a radically polymerizable composition comprising a hydroxylamine ester used to manufacture color filters. The invention further relates to novel hydroxylamine esters. The invention further relates to the use of hydroxylamine esters in all liquid crystal display components requiring post-baking.
    Type: Application
    Filed: July 11, 2013
    Publication date: November 14, 2013
    Applicant: BASF SE
    Inventors: Hisatoshi Kura, Kaori Sameshima, Kazuhiko Kunimoto, Peter Nesvadba, Masaki Ohwa
  • Publication number: 20130289003
    Abstract: A compound having the structure: useful for treating hypertension, Pulmonary Arterial Hypertension (PAH), congestive heart failure, conditions resulting from excessive water retention, cardiovascular disease, diabetes, oxidative stress, endothelial dysfunction, cirrhosis, pre-eclampsia, osteoporosis or nephropathy.
    Type: Application
    Filed: October 25, 2011
    Publication date: October 31, 2013
    Inventors: Amjad Ali, Michael Man-Chu Lo, Robert K. Baker, Zhiqiang Guo, Brent Whitehead, Timothy J. Henderson, Edward Metzger, Lin Yan, Shrenik K. Shah, James Dellureficio, Jun Wang
  • Patent number: 8563732
    Abstract: The invention relates to oxyimino compounds of (Formula I), and pharmaceutically acceptable salts, prodrugs and solvates thereof, wherein: Y is CO or SOm; Z is hydrogen, each optionally substituted lower alkyl, lower alkenyl, aryl, heterocyclyl etc. R1 and R2 are each independently hydrogen, each optionally substituted lower alkyl, lower alkenyl, cycloalkyl, aryl, heterocyclyl etc., each X is independently ?O, optionally substituted lower alkyl, cyano, nitro etc., m is 1 or 2, p is O, 1 or 2 and q is O or 1. The invention is also directed to the use compounds of Formula I to treat, prevent or ameliorate a disorder responsive to the blockade of calcium channels, and particularly N-type calcium channels. Compounds of the present invention are especially useful for treating pain.
    Type: Grant
    Filed: May 30, 2008
    Date of Patent: October 22, 2013
    Assignee: Shionogi & Co., Ltd.
    Inventors: Moriyasu Masui, Hidenori Mikamiyama, Naoki Tsuno
  • Patent number: 8563779
    Abstract: A description is given of (4-trifluoromethyl-3-thiobenzoyl)cyclohexanediones of the formula (I) and of their use as herbicides. In this formula (I), X, R1, R2, R3, and R4 are radicals such as hydrogen and organic radicals such as alkyl. A and Z are oxygen or alkylene.
    Type: Grant
    Filed: July 19, 2011
    Date of Patent: October 22, 2013
    Assignee: Bayer CropScience AG
    Inventors: Hartmut Ahrens, Andreas Van Almsick, Elmar Gatzweiler, Dieter Feucht, Isolde Haeuser-Hahn, Stefan Lehr, Christopher Hugh Rosinger
  • Patent number: 8487110
    Abstract: A method for preparing isofagomine, its derivatives, intermediates and salts thereof using novel processes to make isofagomine from D-(?)-arabinose and L-(?)-xylose.
    Type: Grant
    Filed: November 23, 2009
    Date of Patent: July 16, 2013
    Assignee: Amicus Therapeutics, Inc.
    Inventors: Philip Rybczynski, Alexander Tretyakov, Dan Fuerst, Kamlesh Sheth
  • Patent number: 8466291
    Abstract: 1,5-Dideoxy-1,5-imino-D-glucitol compounds as shown in the specification. Also disclosed is a method of treating a hexosaminidase-associated disease.
    Type: Grant
    Filed: October 30, 2009
    Date of Patent: June 18, 2013
    Assignee: Academia Sinica
    Inventors: Chun-Hung Lin, Ching-Wen Ho
  • Publication number: 20130064871
    Abstract: The present invention relates to a cosmetic composition comprising the combination i) of at least one screening agent of the dibenzoylmethane derivative type and ii) of at least one specific merocyanine dicyano or cyanoacetate derivative. It also relates to a method for the photostabilization, with regard to radiation, of at least one screening agent of the dibenzoylmethane derivative type by an effective amount of at least one specific merocyanine dicyano or cyanoacetate derivative.
    Type: Application
    Filed: March 7, 2011
    Publication date: March 14, 2013
    Applicant: L'OREAL
    Inventors: Herve Richard, Benoit Muller
  • Publication number: 20130058990
    Abstract: The present invention relates to a cosmetic composition containing a combination i) of at least one screening agent of the dibenzoylmethane derivative type and ii) of at least one particular hydrophilic or water-soluble merocyanin UV-screening agent, especially corresponding to one of the formulae (I) or (II) below: in which at least one or two of the radicals contain: either an alkylsulfonate radical in its acid or salified form, or one or two hydroxyl radicals. The invention also relates to a process for the radiation-photostabilization of at least one screening agent of the dibenzoylmethane derivative type with an effective amount of at least one particular hydrophilic or water-soluble merocyanin UV-screening agent, especially corresponding to one of the formulae (I) or (II).
    Type: Application
    Filed: March 7, 2011
    Publication date: March 7, 2013
    Applicant: L'OREAL
    Inventors: Herve Richard, Benoit Muller
  • Publication number: 20130053572
    Abstract: The instant invention provides for novel cationic lipids that can be used in combination with other lipid components such as cholesterol and PEG-lipids to form lipid nanoparticles with oligonucleotides. It is an object of the instant invention to provide a cationic lipid scaffold that is susceptible to hydrolytic instability that may translate into reduced liver residence times and reduced hepatocellular toxicity. The present invention employs acetals and ketals to provide a low pH sensitive chemical handle for degradation.
    Type: Application
    Filed: January 19, 2011
    Publication date: February 28, 2013
    Inventors: Steven L. Colletti, Zhengwu James Deng, Matthew G. Stanton, Weimin Wang, Ivory Hills
  • Publication number: 20130040990
    Abstract: A convenient and scalable synthesis of DGJNAc ID from D-glucuronolactone in an overall yield of 20% is provided. DGJNAc is the first highly potent and specific competitive inhibitor of GalNAcases. DGJNAc ID is also a competitive inhibitor of -hexosaminidases. Synthesis and activity of L-DGJNAc IL is also shown. The use of DGJNAc as a potent and specific inhibitor of GalNAcases will allow useful investigation and treatment of a number of diseases, including Schindler Disease.
    Type: Application
    Filed: January 28, 2011
    Publication date: February 14, 2013
    Inventors: George William John Fleet, Terry Douglas Butters
  • Publication number: 20130041148
    Abstract: The present invention relates to novel processes for the preparation of sterically hindered amine ethers by the transformation of a corresponding oxo-piperidin to a hydroxy or amino substituted sterically hindered amine ether and the preparation of a N-propoxy or N-propenoxy substituted sterically hindered amine and some novel compounds obtainable by these processes. The compounds made by these processes are particularly effective in the stabilization of polymer compositions against harmful effects of light, oxygen and/or heat and as flame-retardants for polymers.
    Type: Application
    Filed: October 15, 2012
    Publication date: February 14, 2013
    Applicant: BASF SE
    Inventor: BASF SE
  • Publication number: 20130023611
    Abstract: Hindered amines represented by the general formula (I): (wherein R is an alkyl or hydroxyalkyl group having 1 to 30 carbon atoms or alkenyl having 2 to 30 carbon atoms; n is an integer of 1 to 4; when n is 1, R1 is alkyl having 1 to 22 carbon atoms, alkenyl having 2 to 22 carbon atoms, or a group represented by the general formula (III): (R is as defined above), while when n is 2 to 4, R1 is an n-valent organic group having 2 to 20 carbon atoms). When added to synthetic resins or coating materials, the amines can impart long-period stabilizing effect to the resins or the materials and exhibit excellent resistance to extraction with acid rain or chemicals.
    Type: Application
    Filed: September 13, 2012
    Publication date: January 24, 2013
    Applicant: ADEKA CORPORATION
    Inventors: Yoshinori NEGISHI, Takashi AYABE, Etsuo TOBITA
  • Publication number: 20130012384
    Abstract: The present invention relates to novel compounds of the formula (I), in which W, X, Y, Z, G, A and t have the meanings given above, to a plurality of processes and intermediates for their preparation and to their use as pesticides and/or herbicides. Moreover, the invention relates to selective herbicidal compositions comprising, firstly, the spiroheterocyclic tetronic acid derivates and, secondly, a crop plant compatibility-improving compound. The present invention furthermore relates to increasing the activity of crop protection compositions comprising in particular phenyl-substituted bicyclooctane-1,3-dione derivates by adding ammonium salts or phosphonium salts and, if appropriate, penetrants, to the corresponding compositions, to processes for their preparation and to their use in crop protection as insecticides and/or acaricides and/or for preventing unwanted plant growth.
    Type: Application
    Filed: September 14, 2012
    Publication date: January 10, 2013
    Applicant: Bayer CropScience AG
    Inventors: Thomas BRETSCHNEIDER, Reiner Fischer, Stefan Lehr, Olga Malsam, Arnd Voerste