Hetero Ring Is Six-membered Consisting Of One Nitrogen And Five Carbon Atoms Patents (Class 514/277)
  • Patent number: 9161718
    Abstract: Cerebral palsy impaired speech in children and adolescents are effectively treated by administration of a psychostimulant. Low doses of the psychostimulant significantly increases the percentage of correctly pronounced intelligible syllables or words and the ability to more intelligibly communicate. The improvement in speech persists after cessation of or prior to continued psychostimulant treatment.
    Type: Grant
    Filed: August 20, 2014
    Date of Patent: October 20, 2015
    Assignee: GILROSE PHARMACEUTICALS, LLC
    Inventors: Bruce Roseman, Gilla Kaplan
  • Patent number: 9155502
    Abstract: Cerebral palsy impaired speech in children and adolescents are effectively treated by administration of a psychostimulant. Low doses of the psychostimulant significantly increases the percentage of correctly pronounced intelligible syllables or words and the ability to more intelligibly communicate. The improvement in speech persists after cessation of or prior to continued psychostimulant treatment.
    Type: Grant
    Filed: August 6, 2014
    Date of Patent: October 13, 2015
    Assignee: GILROSE PHARMACEUTICALS, LLC
    Inventors: Bruce Roseman, Gilla Kaplan
  • Patent number: 9149468
    Abstract: The invention relates to novel multicomponent crystals, to the production thereof, and to the use thereof for treating pain conditions, in particular of unclear genesis, by means of a simultaneous effect on pains which are caused by muscle tension or degenerative joint diseases as well as on pains that are based on inflammatory processes. The novel multicomponent crystals contain ([2-amino-6-(4-fluoro-benzylamino)-pyridin-3-yl]-carbamic acid ethyl ester (flupirtine) and 2-[2-[(2,6-dichlorphenyl)-amino]-phenyl]-acetic acid (diclofenac) as the sole active ingredient combination and can be produced by dissolving the two components in a molar ratio of 1.0:0.9 to 1.0:1.1 in an inert organic solvent and subsequently crystallizing the complex compound.
    Type: Grant
    Filed: December 20, 2011
    Date of Patent: October 6, 2015
    Assignee: TEVA GmbH
    Inventors: Christoph Martin Hoock, Asal Qadan, Bernd Terhaag
  • Patent number: 9089563
    Abstract: A therapeutic method for treating apraxia of speech in children. The child can also be diagnosed with autism, mental retardation, dyslexia. Verbal development stages and nonverbal development stages are tested and observed. If a child demonstrates at least 18 to 24 month development stage of either the verbal development or the non-verbal development, a therapeutic dosage of dopamine agonistic medicine is administered to the child in addition to speech therapy and language training.
    Type: Grant
    Filed: May 17, 2012
    Date of Patent: July 28, 2015
    Assignee: GILROSE PHARMACEUTICALS, LLC
    Inventor: Bruce Roseman
  • Patent number: 9066938
    Abstract: The present invention provides compositions including anti-tumor agents and inhibitors of Goodpasture antigen binding protein, p21, and ABCC7, and their use in treating cancer.
    Type: Grant
    Filed: July 2, 2013
    Date of Patent: June 30, 2015
    Assignees: Fibrostein, S.L., Universitat de Valencia
    Inventors: Juan Saus, Francisco Revert-Ros, Fernando Revert, Carmen Aguado-Velasco, Ernesto López-Pascual, Alejandra María Pérez-Sastre, Raúl Blasco, Héctor Pérez-Montoyo
  • Patent number: 9051296
    Abstract: The present invention relates to aryl carboxamide derivatives of formula (I), wherein Ar1 is phenyl; Ar2 is aryl; n is 1-4; X is —O—, —S—, —SO— or —SO2—, a prodrug thereof or a pharmaceutically acceptable salt thereof, which have blocking activities of voltage gated sodium channels as the TTX-S channels, and which are useful in the treatment or prevention of such disorders and diseases as pain in which voltage gated sodium channels are involved. The invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases as pain in which voltage gated sodium channels are involved.
    Type: Grant
    Filed: November 16, 2010
    Date of Patent: June 9, 2015
    Assignee: RaQualia Pharma Inc.
    Inventors: Tatsuya Yamagishi, Yoshimasa Arano, Mikio Morita, Tadashi Inoue
  • Publication number: 20150148362
    Abstract: The present invention relates to a pharmaceutical composition or a functional health food comprising a verbenone derivative and pharmaceutically acceptable salts thereof as active ingredients for treating or preventing a neurodegenerative disease. More specifically, the verbenone derivative according to the present invention reduces neuronal cell death and oxidative stress, and is highly effective in preventing ischemic brain damage and inflammatory cell migration in rats, thereby providing the pharmaceutical composition or the functional health food which is useful in treating neurodegenerative diseases.
    Type: Application
    Filed: June 4, 2013
    Publication date: May 28, 2015
    Inventors: Won Ki Kim, Yongseok Choi, Sumi Song
  • Patent number: 9040538
    Abstract: The present invention features compounds having the Formula (Ia) and (Ib) (e.g., a compound of any of Formulas ((Ia-2)-(Ia-21)), including other tautomers, stereoisomers, E/Z stereoisomers, prodrugs, pharmaceutically acceptable salts, and compositions thereof. The invention also features methods for treating or preventing pain (e.g., neuropathic pain), inflammation, or epilepsy in a patient by administering an effective amount of a compound of Formula (Ia) or (Ib). The invention also features a method for treating or preventing pain (e.g., neuropathic pain), inflammation, or epilepsy in a patient that includes administering to a patient in need thereof an effective amount of a compound of Formula (IIa) or (IIb) (e.g., a compound of any of Formulas ((IIa-2)-(IIa-6)). The compounds described herein (e.g., a compound of Formulas (Ia), (Ib), (IIa), or (IIb)) can also be used as anticonvulsants.
    Type: Grant
    Filed: May 21, 2010
    Date of Patent: May 26, 2015
    Assignee: Universite Laval
    Inventors: Giorgio Attardo, Sasmita Tripathy, Martin Gagnon
  • Publication number: 20150141380
    Abstract: A method of treating a subject at risk of or suspected of having Fragile X syndrome or autism spectrum disorder associated with abnormalities of ERK includes administering to the subject a therapeutically effective amount of at least one ERK inhibiting compound that prevents abnormalities in neuronal connectivity, a prodrug thereof that is metabolisable to form the compound, or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: August 5, 2011
    Publication date: May 21, 2015
    Applicant: CASE WESTERN RESERVE UNIVERSITY
    Inventors: Mark A. Smith, Michael Snape
  • Publication number: 20150141471
    Abstract: The present invention relates to compounds of the formula (I), wherein the residues R1 to R6, V, G and M have the meanings indicated in the claims. The compounds of the formula I are valuable pharmacologically active compounds for use in the treatment of diverse disorders, for example cardiovascular disorders like thromboembolic diseases or restenoses. The compounds of the invention are effective antagonists of the platelet LPA receptor LPAR5 (GPR92) and can in general be applied in conditions in which an undesired activation of the platelet LPA receptor LPAR5, the mast cell LPA receptor LPAR5 or the microglia cell LPA receptor LPAR5 is present, or for the cure or prevention of which an inhibition of the platelet, mast cell or microglia cell LPA receptor LPAR5 is intended. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in medicaments, and pharmaceutical compositions comprising them.
    Type: Application
    Filed: May 16, 2013
    Publication date: May 21, 2015
    Inventors: Marc Nazare, Detlef Kozian, Andreas Evers, Werngard Czechtizky
  • Publication number: 20150140061
    Abstract: Stents with coatings comprising a combination of a restenosis inhibitor comprising an HMG-CoA reductase inhibitor and a carrier. Also provided are methods of coating stents with a combination of an HMG-CoA reductase inhibitor and a carrier. A preferred example of a restenosis inhibitor is cerivastatin. The stent coatings have been shown to release restenosis inhibitors in their active forms.
    Type: Application
    Filed: November 12, 2014
    Publication date: May 21, 2015
    Inventor: Chandrashekhar Pathak
  • Patent number: 9029413
    Abstract: Alterations of certain metabolite concentrations and fluxes that occur in response to viral infection are described. Host cell enzymes in the involved metabolic pathways are selected as targets for intervention; i.e., to restore metabolic flux to disadvantage viral replication, or to further derange metabolic flux resulting in “suicide” of viral-infected cells (but not uninfected cells) to limit viral propagation. While any of the enzymes in the relevant metabolic pathway can be selected, pivotal enzymes at key control points in these metabolic pathways are preferred as candidate antiviral drug targets. Inhibitors of these enzymes are used to reverse, or redirect, the effects of the viral infection. Drug candidates are tested for antiviral activity using screening assays in vitro and host cells, and in animal models. Animal models are then used to test efficacy of candidate compounds in preventing and treating viral infections. Antiviral activity of enzyme inhibitors is demonstrated.
    Type: Grant
    Filed: April 3, 2012
    Date of Patent: May 12, 2015
    Assignee: The Trustees of Princeton University
    Inventors: Josh Munger, Bryson Bennett, Thomas Shenk, Joshua Rabinowitz
  • Patent number: 9028854
    Abstract: A pesticidal composition comprising 4-phenoxyphenyl 2-(2-pyridyloxy)propyl ether; a hydrophobic organic solvent capable of dissolving 0.1-fold by weight of 4-phenoxyphenyl 2-(2-pyridyloxy)propyl ether at 0° C.; polyvinyl alcohol; a nonionic surfactant selected from the group consisting of alkoxylated castor oil, alkoxylated hydrogenated castor oil and alkoxylated hydrogenated castor oil fatty acid ester; and water, is excellent in storage stability.
    Type: Grant
    Filed: December 13, 2005
    Date of Patent: May 12, 2015
    Assignee: Sumitomo Chemical Company, Limited
    Inventor: Toshiyuki Tanedani
  • Patent number: 9029386
    Abstract: Derivatives of pyridine of the formula wherein one of Y and A is CR and the other is N are kinase inhibitors useful in treating conditions associated with excess kinase activity.
    Type: Grant
    Filed: January 22, 2013
    Date of Patent: May 12, 2015
    Assignee: Gilead Sciences, Inc.
    Inventors: Christopher John Burns, Michael Francis Harte, James T. Palmer
  • Patent number: 9023874
    Abstract: The invention relates to alkylsulfide derivatives compounds of formula I as hereunder depicted or the enantiomers or veterinarily acceptable salts thereof which are useful for combating or controlling invertebrate pests, in particular arthropod pests and nematodes. The invention also relates to methods for controlling invertebrate pests by using these compounds and to plant propagation material and to agricultural and veterinary compositions comprising said compounds. wherein U, R1, R2, R3U, X, n and p are defined as in the description.
    Type: Grant
    Filed: November 11, 2010
    Date of Patent: May 5, 2015
    Assignee: Merial, Inc.
    Inventors: Sebastian Soergel, Ralph Paulini, Steffen Gross, Carsten Beyer, Matthias Pohlman, Henricus Maria Martinus Bastiaans, Michael Rack, Deborah L. Culbertson, Douglas D. Anspaugh, Sarah Thompson, Vincent Salgado
  • Publication number: 20150119414
    Abstract: A composition and a method of treatment utilizing a combination of statins (or HMG-CoA reductase inhibitors), a class of drug used to lower cholesterol levels by inhibiting the enzyme HMG-CoA reductase, with mixtures of an omega-3 fatty acid formulation containing about 90% or more omega 3 fatty acids by weight including a combination of Eicosapentaenoic acid (EPA), Docosapentaenoic acid (DPA) and Docosahexaenoic acid (DHA) in a weight ratio of EPA:DHA of from 5.7 to 6.3, wherein the sum of the EPA, DHA and DPA represent about 82% by weight of the total formulation and about 92% of the total omega 3 fatty acid content of the composition are taught.
    Type: Application
    Filed: January 2, 2015
    Publication date: April 30, 2015
    Applicant: PIVOTAL THERAPEUTICS INC.
    Inventors: George JACKOWSKI, Rachelle MACSWEENEY, Nisar Ahmad SHAIKH, Jason YANTHA, Valerie B. SCHINI-KERTH
  • Patent number: 9018237
    Abstract: The present disclosure relates to compositions for and methods of improving wound healing, including compositions for and methods of treating chronic wounds, and compositions for the inhibition and treatment of necrosis and extended quiescence that result in cellular necrosis instead of normal proliferation. The methods for wound healing administer one or more compositions including hydroxytyrosol and oleuropein with cells derived from umbilical cord blood.
    Type: Grant
    Filed: July 11, 2014
    Date of Patent: April 28, 2015
    Inventor: Darlene E. McCord
  • Publication number: 20150111891
    Abstract: The invention provides compounds and salts thereof as d herein. The invention also provides pharmaceutical compositions comprising a compound disclosed herein, processes for preparing compounds disclosed herein, intermediates useful for preparing compounds disclosed herein and therapeutic methods for treating an HIV infection, treating the proliferation of the HIV virus, treating AIDS or delaying the onset of AIDS or ARC symptoms in a mammal using compounds disclosed herein.
    Type: Application
    Filed: January 3, 2013
    Publication date: April 23, 2015
    Applicant: Gilead Sciences, Inc.
    Inventors: Kerim Babaoglu, Gediminas Brizgys, Hongyan Guo, Paul Hrvatin, Eric Lansdon, John O. Link, Hongtao Liu, Ryan McFadden, Michael L. Mitchell, Yingmei Qi, Paul A. Roethle, Randall W. Vivian, Lianhong Xu, Hong Yang
  • Patent number: 9000044
    Abstract: The invention is concerned with the compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3 and X are defined in the detailed description and claims. In addition, the present invention relates to methods of manufacturing and using the compounds of formula I as well as pharmaceutical compositions containing such compounds. The compounds of formula I are antagonists or partial agonists at the CRTH2 receptor and may be useful in treating diseases and disorders associated with that receptor such as asthma.
    Type: Grant
    Filed: February 14, 2013
    Date of Patent: April 7, 2015
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Fariborz Firooznia, Tai-An Lin, Eric Mertz, Sung-Sau So, Achyutharao Sidduri, Jefferson Wright Tilley
  • Patent number: 8993509
    Abstract: The present invention relates to agents, and methods for identifying compounds, which agents and compounds are effective in the treatment, and more particularly, that inhibit cachexia, and its associated or related disorders and conditions. In addition, the invention relates to compositions and methods for the use thereof in treating conditions that are characterized by cachexia, and its associated or related disorders and conditions and/or cachexia, and its associated or related disorders and conditions, such as for example, cancer cachexia and cachexia associated with AIDS, autoimmune disorders, drug addiction, alcoholism, chronic inflammatory disorders, cirrhosis of the liver, anorexia and neurodegenerative disease. In particular, the diagnostic marker and drug target of the invention is the ATGL Lipase, which can be inhibited by e.g. siRNAs and compounds with any of the following structures (I).
    Type: Grant
    Filed: March 31, 2010
    Date of Patent: March 31, 2015
    Inventors: Robert Zimmerman, Rudolf Zechner, Günther Haemmerle, Gerald Höfler, Suman Das, Achim Lass
  • Publication number: 20150072980
    Abstract: The present invention is directed to compounds, their synthesis, and their use as antagonists, inverse agonists, modulators and or inhibitors of the Retinoic acid-related orphan nuclear receptor ?t (ROR?t)/ROR?. The compounds of the present invention are useful for modulating ROR?t)/ROR? activity and for treating diseases or conditions mediated by ROR?t)/ROR? such as for example, disease states associated with immunopathology of human autoimmune diseases such as Multiple Sclerosis (MS), Rheumatoid Arthritis (RA), Inflammatory Colitis, Psoriasis, COPD, Pain, Obesity, Diabetes, Dyslipidemia, Osteoporosis, Asthma, Neurodegenerative diseases and Cancer.
    Type: Application
    Filed: August 27, 2014
    Publication date: March 12, 2015
    Inventors: Hariprasad Vankayalapati, Venkatakrishnareddy Yerramreddy
  • Publication number: 20150072014
    Abstract: The present invention relates to pharmaceutical compositions of sodium picosulfate, magnesium oxide and citric acid. In particular, the invention relates to pharmaceutical compositions comprise granules having a layer of sodium picosulfate on neutral carrier/s. The invention also relates to processes for the preparation of such compositions and use thereof for bowel cleansing.
    Type: Application
    Filed: September 10, 2014
    Publication date: March 12, 2015
    Applicant: CADILA HEALTHCARE LIMITED
    Inventors: Kannan Muthaiyyan ESSAKIMUTHU, Jitendra Rameshchandra PATEL, Paritosh Kunwar SINGH
  • Publication number: 20150064168
    Abstract: Cadherin-11 inhibitors and methods for the prevention and treatment of cadherin-11 related diseases are described herein. Cadherin-11 related diseases include cancer and rheumatoid arthritis.
    Type: Application
    Filed: July 3, 2014
    Publication date: March 5, 2015
    Inventors: Stephen W. Byers, Sivanesan Dakshanamurthy, Jaime M. Guidry Auvil, Milton L. Brown
  • Patent number: 8969397
    Abstract: Disclosed herein are systems and methods for contributing to the local treatment of pain. More specifically, the disclosed systems and methods contribute to the local treatment pain by inhibiting the NF?B family of transcription factors.
    Type: Grant
    Filed: February 5, 2010
    Date of Patent: March 3, 2015
    Assignee: Warsaw Orthopedic, Inc.
    Inventors: Eric N. Burright, Lisa L. Shafer, Bill McKay, John Zanella
  • Publication number: 20150045378
    Abstract: Provided is an aromatic ring compound having a GPR40 agonist activity. A compound represented by the formula (I): wherein each symbol is as described in the DESCRIPTION, or a salt thereof has a GPR40 agonist activity, and is useful as an agent for the prophylaxis or treatment of diabetes and the like.
    Type: Application
    Filed: February 12, 2013
    Publication date: February 12, 2015
    Inventors: Seiji Miwatashi, Hideo Suzuki, Tomohiro Okawa, Yasufumi Miyamoto, Takeshi Yamasaki, Yuko Hitomi, Yasuhiro Hirata
  • Patent number: 8946439
    Abstract: Compounds are provided according to formula 1: where A, B, W, X?, L, R1, R3, R4b, and m? are as defined herein. Provided compounds and pharmaceutical compositions thereof are useful for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, cognitive disorders, anxiety, depression, and others.
    Type: Grant
    Filed: February 27, 2009
    Date of Patent: February 3, 2015
    Assignee: Evotec AG
    Inventors: Zhi-Liang Wei, Sumithra Gowlugari, Carl Kaub, Zhan Wang, Yeyu Cao, John Kincaid
  • Patent number: 8946251
    Abstract: The present invention relates to a method for treating a patient suffering from a thermoregulatory dysfunction, especially hot flashes and flushes associated with hormonal changes due to naturally occurring menopause (whether male or female) or due to chemically or surgically induced menopause. The method is also applicable to treating the hot flashes, hot flushes, or night sweats associated with disease states that disrupt normal hormonal regulation of body temperature.
    Type: Grant
    Filed: January 17, 2014
    Date of Patent: February 3, 2015
    Assignee: Noven Therapeutics, LLC
    Inventor: Patricia Allison Tewes Richards
  • Patent number: 8937083
    Abstract: This document discloses molecules having the following formula (“Formula One”): and processes related thereto.
    Type: Grant
    Filed: October 24, 2012
    Date of Patent: January 20, 2015
    Assignee: DowAgroSciences, LLC
    Inventors: Noormohamed M. Niyaz, Negar Garizi, Yu Zhang, Tony K. Trullinger, Ricky Hunter, Ann M. Buysse, Asako Kubota, Paul Renee LePlae, Jr., Daniel Knueppel, Christian T. Lowe, Dan Pernich, David A. Demeter, Timothy C. Johnson
  • Publication number: 20150018341
    Abstract: The invention provides novel ethylene derivatives represented by Formula I, which may be used as selective estrogen receptor modulators (SERMs) and useful in the prophylaxis and/or treatment of estrogen-dependent conditions or conditions.
    Type: Application
    Filed: December 28, 2012
    Publication date: January 15, 2015
    Applicant: CENTAURUS BIOPHARMA CO., LTD.
    Inventors: Dengming Xiao, Li Zhu, Yuandong Hu, Rong Yu, Wei Hu, Na Zhao, Yong Peng, Hong Luo, Yongxin Han
  • Publication number: 20150018321
    Abstract: Derivatives of 1-phenyl-2-pyridinyl alkyl alcohols are useful as inhibitors of the phosphodiesterase 4 (PDE4) enzyme.
    Type: Application
    Filed: September 25, 2014
    Publication date: January 15, 2015
    Applicant: Chiesi Farmaceutici S.p.A.
    Inventors: Maurizio DELCANALE, Elisabetta ARMANI, Gabriele AMARI
  • Patent number: 8933092
    Abstract: Methods and compositions for the alleviation of pain in a patient. The methods and compositions sequentially administer a therapeutically effective amount of first compound having opioid receptor agonist activity, followed by a therapeutic effective amount of a second or subsequent compound(s) having opioid receptor agonist activity, one or more non-opioid analgesic compounds or one or more hybrid opioid compounds, or mixtures thereof. The methods and compositions effectively alleviate pain with a lower incidence of opioid-induced side effects.
    Type: Grant
    Filed: May 31, 2012
    Date of Patent: January 13, 2015
    Assignee: Qrxpharma Limited
    Inventor: John W. Holaday
  • Patent number: 8933091
    Abstract: A method of reducing or inhibiting kinase activity of C-KIT in a cell or a subject, and the use of such compounds for preventing or treating in a subject a cell proliferative disorder and/or disorders related to C-KIT using a compound of the present invention: or a solvate, hydrate, tautomer or pharmaceutically acceptable salt thereof. The present invention is further directed to methods for treating conditions such as cancers and other cell proliferative disorders.
    Type: Grant
    Filed: September 6, 2013
    Date of Patent: January 13, 2015
    Assignee: Janssen Pharmaceutica NV
    Inventors: Carl R. Illig, Shelley K. Ballentine, Jinsheng Chen, Sanath K. Meegalla, M. Jonathan Rudolph, Mark J. Wall, Kenneth J. Wilson, Renee Louise Desjarlais, Carl M. Manthey, Christopher J. Molloy
  • Patent number: 8921394
    Abstract: Compounds of structural formula (I) are inhibitors of prolylcarboxypeptidase (PrCP). The compounds of the present invention are useful for the prevention and treatment of conditions related to the enzymatic activity of PrCP such as abnormal metabolism, including obesity; diabetes; metabolic syndrome; obesity related disorders; and diabetes related disorders.
    Type: Grant
    Filed: April 21, 2011
    Date of Patent: December 30, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Thomas H. Graham, Dong-Ming Shen, Min Shu
  • Patent number: 8921390
    Abstract: A Medicaments for inhibiting thrombus formation contains active ingredients which are triflusal and clopidogrel bisulfate, wherein a mass ratio of triflusal to clopidogrel bisulfate is (100-650):(30-150), preferably (1-20):1, more preferably (3-6):1, and even more preferably 3:1 or 6:1.
    Type: Grant
    Filed: March 17, 2010
    Date of Patent: December 30, 2014
    Assignee: Guizhou Liansheng Pharmaceutical Co. Ltd.
    Inventor: Chunhua Su
  • Publication number: 20140378494
    Abstract: The invention relates to pesticidal mixtures comprising as active compounds 1) at least one cyanosulfoximine compound I of the formula I wherein R1, R2 and G are defined in the description; and 2) at least one active compound II selected from a group A comprising acteylcholine esterase inhibitors, GABA-gated chloride channel antagonists, sodium channel modulators, nicotinic acetylcholine receptor agonists/antagonists, chloride channel activators, juvenile hormone mimics, compounds affecting the oxidative phosphorylation, inhibitors of the chitin biosynthesis, moulting disruptors, inhibitors of the MET, voltage-dependent sodium channel blockers, inhibitors of the lipid synthesis and other compounds as defined in the description, in synergistically effective amounts. The invention relates further to methods and use of these mixtures for combating insects, arachnids or nematodes in and on plants, and for protecting such plants being infested with pests and also for protecting seeds.
    Type: Application
    Filed: September 11, 2014
    Publication date: December 25, 2014
    Inventors: Delphine BREUNINGER, Henricus Maria Martinus BASTIAANS, Wolfgang VON DEYN, Juergen LANGEWALD
  • Patent number: 8916552
    Abstract: The invention provides combinations comprising (or consisting essentially of) one or more ancillary compound(s) and a compound of the formula (I): or salts, tautomers, solvates and N-oxides thereof; wherein R1 is hydroxy or hydrogen; R2 is hydroxy; methoxy or hydrogen; provided that at least one of R1 and R2 is hydroxy; R3 is selected from hydrogen; halogen; cyano; optionally substituted C1-5 hydrocarbyl and optionally substituted C1-5 hydrocarbyloxy; R4 is selected from hydrogen; a group —(O)n—R7 where n is 0 or 1 and R7 is an optionally substituted acyclic C1-5 hydrocarbyl group or a monocyclic carbocyclic or heterocyclic group having 3 to 7 ring members; halogen; cyano; hydroxy; amino; and optionally substituted mono- or di-C1-5 hydrocarbyl-amino; or R3 and R4 together form a monocyclic carbocyclic or heterocyclic ring of 5 to 7 ring members; and NR5R6 forms an optionally substituted bicyclic heterocyclic group having 8 to 12 ring members of which up to 5 ring members are heteroatoms selected from oxyg
    Type: Grant
    Filed: October 12, 2007
    Date of Patent: December 23, 2014
    Assignee: Astex Therapeutics Limited
    Inventors: Neil James Gallagher, John Francis Lyons, Neil Thomas Thompson, Stephen Murray Yule, Christopher William Murray
  • Publication number: 20140370060
    Abstract: The present invention relates to a method of stabilising a tear film in an individual having an ocular surface inflammatory disorder by providing a compound to an ocular surface of the individual to reduce the synthesis of a cholesterol by a meibum-producing tissue.
    Type: Application
    Filed: February 1, 2013
    Publication date: December 18, 2014
    Inventors: Kenneth Gek-Jin Ooi, Stephanie Louise Watson
  • Publication number: 20140371232
    Abstract: Provided are cajanine structure analogous compounds, synthesis method and pharmacological effects thereof, the compounds of the present invention having the structure as represented by general formulas I, II, III, IV and V. Also provided are pharmaceutical compositions containing the compounds as active ingredient, and uses thereof; the compounds of the present invention having the pharmacological activities such as anti-virus, anti-virus-infection, nerve protection, anti-metabolic-diseases and the like. Also provided is a chemical total synthesis preparation method of the natural products cajanine, cajanine A and cajanine C. The present invention lays a foundation for the in-depth study and development of the compounds as clinical drugs in the future.
    Type: Application
    Filed: December 18, 2012
    Publication date: December 18, 2014
    Inventors: Zhuorong Li, Xingyue Ji, Situ Xue, Guanghui Zheng, Yuhuan Li, Peizhen Tao, Jiandong Jiang
  • Publication number: 20140371252
    Abstract: Processes for making and using compounds of formula (I): wherein R1, R2, R3, R4a, R4b, R5 and R6 are defined herein, as well as other indene derivatives are disclosed herein. These compounds are disclosed as being useful in treating inflammatory conditions or diseases.
    Type: Application
    Filed: January 23, 2014
    Publication date: December 18, 2014
    Applicant: Aquinox Pharmaceuticals Inc.
    Inventors: Jeffery R. Raymond, Kang Han, Yuanlin Zhou, Yuehua He, Bradley Noren, James Gee Ken Yee
  • Patent number: 8912209
    Abstract: The present invention relates to new kinase inhibitors, more specifically ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In particular, the present invention relates to new ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In addition, the invention relates to methods of treatment and use of said compounds in the manufacture of a medicament for the application to a number of therapeutic indications including sexual dysfunction, inflammatory diseases, ophthalmic diseases and Respiratory diseases.
    Type: Grant
    Filed: May 20, 2013
    Date of Patent: December 16, 2014
    Assignee: Amakem NV
    Inventors: Dirk Leysen, Oliver Defert, Nadzeya Kaval, Petra Blom, Sandro Boland
  • Patent number: 8912208
    Abstract: The present invention provides (4-{4-[5-(Benzooxazol-2-ylamino)-pyridin-2-yl]-phenyl}-cyclohexyl)-acetic acid which is useful for treating or preventing conditions or disorders associated with DGAT1 activity in animals, particularly humans.
    Type: Grant
    Filed: September 13, 2012
    Date of Patent: December 16, 2014
    Assignee: Novartis AG
    Inventors: Michael H. Serrano-Wu, Young-shin Kwak, Wenming Liu
  • Publication number: 20140363388
    Abstract: The present invention is directed to inhibitors of tyrosinase, pharmaceutical compositions comprising such tyrosinase inhibitors, and methods of making and using the same. Specifically, included in the present invention are compositions of matter comprised of at least one 2,4-dihydroxybenzene analog, which inhibit the activity of tyrosinase and which inhibit the overproduction of melanin.
    Type: Application
    Filed: January 13, 2014
    Publication date: December 11, 2014
    Applicant: UNIGEN, INC.
    Inventors: Sandip K. Nandy, Jiyun Liu, Alexandre Mikhailovitch Nesterov, Carmen Hertel, Abeysinghe A. Padmapriya
  • Patent number: 8906962
    Abstract: A method for treating hair loss in mammals uses compositions containing prostaglandin F analogs. The compositions can be applied topically to the skin. The compositions can arrest hair loss, reverse hair loss, and promote hair growth.
    Type: Grant
    Filed: September 23, 2013
    Date of Patent: December 9, 2014
    Assignee: Duke University
    Inventors: Mitchell A. deLong, John M. McIver, Robert S. Youngquist
  • Publication number: 20140357649
    Abstract: The present invention relates to novel phenyl(oxy/thio)alkanol derivatives, to processes for preparing these compounds, to compositions comprising these compounds and to their use as biologically active compounds, in particular for controlling harmful microorganisms in crop protection and in the protection of materials and as plant growth regulators.
    Type: Application
    Filed: August 13, 2014
    Publication date: December 4, 2014
    Inventors: Carl Friedrich NISING, Klaus Kunz, Jörg Nico Greul, Hendrick Helmke, Gorka Peris, Jürgen Benting, Peter Dahmen, Isolde Hauser-Hahn, Ines Heinemann, Christian Paulitz, Dirk Schmutzler, Ulrike Wachendorff-Neumann, Tomoki Tsuchiya, Christoph Andreas Braun, Ruth Meissner, Thomas Knobloch
  • Patent number: 8901170
    Abstract: Compounds of formula (I) wherein the symbols have the meaning given in the specification, as well as processes for preparing the compounds (I), pesticidal compositions and synergistic mixtures comprising compounds (I), methods for the control of insects, acarids or nematodes by contacting the pests or their food supply, habitat or breeding grounds with a pesticidally effective amount of compounds formula (I), and a method for treating, controlling, preventing or protecting animals against infestation or infection by parasites which comprises orally, topically or parenterally administering or applying to the animals a parasiticidally effective amount of compounds of formula (I).
    Type: Grant
    Filed: June 22, 2007
    Date of Patent: December 2, 2014
    Assignee: BASF SE
    Inventors: Matthias Pohlman, Michael Hofmann, Henricus Maria Martinus Bastiaans, Michael Rack, Deborah L. Culbertson, Hassan Oloumi-Sadeghi, Takeo Hokama, Christopher Palmer
  • Patent number: 8895554
    Abstract: Bis- and tris-dihydroxyaryl compounds and their methylenedioxy analogs and pharmaceutically acceptable esters, their synthesis, pharmaceutical compositions containing them, and their use in the treatment of amyloid diseases, especially A? amyloidosis, such as observed in Alzheimer's disease, IAPP amyloidosis, such as observed in type 2 diabetes, and synucleinopathies, such as observed in Parkinson's disease, and the manufacture of medicaments for such treatment.
    Type: Grant
    Filed: October 1, 2013
    Date of Patent: November 25, 2014
    Assignee: ProteoTech Inc
    Inventors: Alan D. Snow, Beth Nguyen, Gerardo Castillo, Virginia Sanders, Thomas Lake
  • Publication number: 20140343079
    Abstract: The invention provides compounds of formulae (I), (II), (III), and (IV): and salts thereof, as well as pharmaceutical compositions comprising such compounds. The compounds are useful for treating cancers and Alzheimer's disease.
    Type: Application
    Filed: September 13, 2012
    Publication date: November 20, 2014
    Applicants: Behalf of Arizona State University
    Inventors: Carl E. Wagner, Peter W. Jurutka, Pamela A. Marshall
  • Patent number: 8883786
    Abstract: The present invention relates to compounds of formula I wherein A, n, R1a to R1e and R2 to R5 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are glucocorticoid receptor antagonists useful for the treatment and/or prevention of diseases such as diabetes, dyslipidemia, obesity, hypertension, cardiovascular diseases, adrenal imbalance or depression.
    Type: Grant
    Filed: February 13, 2012
    Date of Patent: November 11, 2014
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Jacques Bailly, Cornelia Hertel, Daniel Hunziker, Christian Lerner, Ulrike Obst Sander, Jens-Uwe Peters, Philippe Pflieger, Tanja Schulz-Gasch
  • Patent number: 8883813
    Abstract: Described is a method for treating an individual having a neurological disorder with an associated mutation or mutations in a gene encoding a lysosomal enzyme. Specifically, the individual is administered a specific pharmacological chaperone for the lysosomal enzyme which increases trafficking of the protein from the ER to the lysosome in neural cells, with or without concomitantly increasing enzyme activity in neural cells. Restoration of trafficking relieves cell stress and other toxicities associated with accumulation of mutant proteins. Restoration of enzyme activity relieves substrate accumulation and pathologies associated with lipid accumulation. In a specific embodiment, the neurological disorder is Parkinson's disease or parkinsonism which is associated with mutations in glucocerebrosidase.
    Type: Grant
    Filed: January 7, 2011
    Date of Patent: November 11, 2014
    Assignee: Amacus Therapeutics, Inc.
    Inventor: Brandon Wustman
  • Patent number: 8883814
    Abstract: Compositions and methods are provided that enhance cognition in a human to which the composition is orally administered. Remarkably, clinical studies have proven that contemplated compositions achieve the desired effects using a minimal number of active ingredients at or near threshold active dosages, wherein such compositions almost exclusively comprise huperzine A, vinpocetine or rhodiola, and acetyl-L-carnitine, and optionally further include alpha lipoic acid, rhodiola, and biotin.
    Type: Grant
    Filed: November 30, 2011
    Date of Patent: November 11, 2014
    Assignee: KeyView Labs, Inc.
    Inventor: Josh Reynolds