The Hetero Ring Is Five-membered Patents (Class 514/438)
  • Patent number: 10179118
    Abstract: Pharmaceutical compositions and dosage forms of dimethyl fumarate containing low levels of certain impurities are disclosed.
    Type: Grant
    Filed: March 24, 2014
    Date of Patent: January 15, 2019
    Assignee: ARBOR PHARMACEUTICALS, LLC
    Inventors: Sami Karaborni, Wei Chen, Suresh Kumar Manthati
  • Patent number: 10155722
    Abstract: The present application relates to compounds represented by general formula (I), general formula (II) or general formula (III), and pharmaceutically acceptable salts or hydrates thereof, preparation methods thereof, and pharmaceutical compositions thereof. The compounds represented by general formula (I), general formula (II) or general formula (III) have inhibitory activities against isocitrate dehydrogenase 2 (IDH2), thereby being capable of treating IDH2 mutation-induced cancers.
    Type: Grant
    Filed: July 29, 2016
    Date of Patent: December 18, 2018
    Assignees: Chia Tai Tianqing Pharmaceutical Group Co., Ltd., Lianyungang Runzhong Pharmaceutical Co., Ltd., Centaurus Biopharma Co., Ltd.
    Inventors: Shulong Wang, Na Zhao, Xijie Liu, Yuandong Hu, Hui Zhang, Hong Luo, Yong Peng, Dengming Xiao, Yongxin Han, Xiquan Zhang, Xin Tian
  • Patent number: 10112920
    Abstract: Disclosed are beta and gamma-amino isoquinoline amide compounds and substituted benzamide compounds. In particular, the invention provides compounds that affect the function of kinases in a cell and that are useful as therapeutic agents or with therapeutic agents. The compounds of the invention are useful in the treatment of a variety of diseases and conditions including eye diseases such as glaucoma, cardiovascular diseases, and diseases characterized by abnormal growth, such as cancers. The invention further provides compositions containing the beta or gamma-amino isoquinoline amide compounds or substituted benzamide compounds.
    Type: Grant
    Filed: December 15, 2017
    Date of Patent: October 30, 2018
    Assignee: Aerie Pharmaceuticals, Inc.
    Inventors: Mitchell A. deLong, Jill Marie Sturdivant, Susan M. Royalty
  • Patent number: 10112881
    Abstract: The present invention provides a compound of Formula I, wherein R1 is not H when R2 is H and R2 is not H when R1 is H, further wherein R1 is CnH(2n+1)O, wherein n is 1-10, R2 is OH or CnH(2n+1)O, wherein n is 1-10, A, B and R1, R2, R5, R6, and R7 are separately and independently selected from a group consisting of H, alkyl, hydroxyl, halo, nitro and aryl groups, R11 is an alkyl or an aryl group and L is an optional linker or linking group, with x=0 or 1, i.e., if x=0, no linking group is present, or a salt or prodrug or derivative thereof that is a skin-lightening agent useful for the inhibition of melanin synthesis and/or the removal of existing melanin to function as a skin-lightening agent.
    Type: Grant
    Filed: July 21, 2015
    Date of Patent: October 30, 2018
    Assignee: WISYS TECHNOLOGY FOUNDATION, INC.
    Inventors: Cheng-Chen Huang, Aaron P. Monte
  • Patent number: 10040748
    Abstract: This invention relates to novel derivatives of 4-hydroxybutyric acid and prodrugs thereof, and pharmaceutically acceptable salts of the foregoing. This invention also provides pharmaceutical compositions comprising a compound of this invention and the use of such compositions in methods of treating narcolepsy, fibromyalgia, other disorders or conditions that are beneficially treated by improving nocturnal sleep or by administering sodium oxybate.
    Type: Grant
    Filed: April 11, 2016
    Date of Patent: August 7, 2018
    Assignee: Concert Pharmaceuticals, Inc.
    Inventors: Roger D. Tung, Adam J. Morgan
  • Patent number: 10010812
    Abstract: Disclosed is an oxidation process to produce a crude carboxylic acid product carboxylic acid product. The process comprises oxidizing a feed stream comprising at least one oxidizable compound to generate a crude carboxylic acid slurry comprising furan-2,5-dicarboxylic acid (FDCA) and compositions thereof. Also disclosed is a process to produce a dry purified carboxylic acid product by utilizing various purification methods on the crude carboxylic acid.
    Type: Grant
    Filed: February 17, 2017
    Date of Patent: July 3, 2018
    Assignee: Eastman Chemical Company
    Inventors: Kenny Parker, Mesfin Janka, Ashfaq Shaikh, Lee Partin
  • Patent number: 9944615
    Abstract: A process for purifying a crude furan 2,5-dicarboxylic acid composition (cFDCA) by hydrogenation of a FDCA composition dissolved in a hydrogenation solvent such as water, and hydrogenating under mild conditions, such as at a temperature within a range of 130° C. to 225° C. by contacting the solvated FDCA composition with hydrogen in the presence of a hydrogenation catalyst under a hydrogen partial pressure within a range of 10 psi to 900 psi. A product FDCA composition is produced having a low amount of tetrahydrofuran dicarboxylic acid, a low b*, and a low amount of 5-formyl furan-2-carboxylic acid (FFCA).
    Type: Grant
    Filed: July 1, 2016
    Date of Patent: April 17, 2018
    Assignee: EASTMAN CHEMICAL COMPANY
    Inventors: Mesfin Ejerssa Janka, Kenny Randolph Parker, Ashfaq Shahanawaz Shaikh, Lee Reynolds Partin, Charles Edwan Sumner, Jr., Shane Kipley Kirk
  • Patent number: 9889142
    Abstract: Prostamide-containing biodegradable intraocular implants, prostamide compounds, prostamide-containing pharmaceutical compositions, and methods for making and using such implants and compositions for the immediate and sustained reduction of intraocular pressure and treatment of glaucoma in an eye of a patient are described.
    Type: Grant
    Filed: March 21, 2016
    Date of Patent: February 13, 2018
    Assignee: Allergan, Inc.
    Inventors: Patrick M. Hughes, Jie Shen, Michael R. Robinson, David F. Woodward, Robert M. Burk, Hui Liu, Jinping Wan, Chandrasekar Durairaj, Gyorgy F. Ambrus, Ke Wu, Danny T. Dinh
  • Patent number: 9884839
    Abstract: Provided herein are non-steroidal 17beta-hydroxysteroid dehydrogenase type 1 and type 2 (17?-HSD1 and 17?-HSD2) inhibitors, their production and use, especially for the treatment and for prophylaxis of hormone-related diseases.
    Type: Grant
    Filed: January 5, 2015
    Date of Patent: February 6, 2018
    Assignee: ElexoPharm GmbH
    Inventors: Rolf Hartmann, Martin Frotscher, Ahmed Saad Abdelsamie Ahmed, Emmanuel Bey, Chris J. van Koppen, Sandrine Oberwinkler-Marchais, Carsten Börger, Lorenz Siebenbürger, Victor Hernández Olmos
  • Patent number: 9815763
    Abstract: This invention relates to novel derivatives of 4-hydroxybutyric acid and prodrugs thereof, and pharmaceutically acceptable salts of the foregoing. This invention also provides pharmaceutical compositions comprising a compound of this invention and the use of such compositions in methods of treating narcolepsy, fibromyalgia, other disorders or conditions that are beneficially treated by improving nocturnal sleep or by administering sodium oxybate.
    Type: Grant
    Filed: June 8, 2015
    Date of Patent: November 14, 2017
    Assignee: Concert Pharmaceuticals, Inc.
    Inventor: Roger D. Tung
  • Patent number: 9637467
    Abstract: Disclosed herein is a method comprising administering a compound to a mammal suffering from an inflammatory bowel disease for the treatment of said disease, said compound having a structure according to Formula I wherein X, Y, B, R2, R3, R4, R5, R6 and n have the meanings found herein.
    Type: Grant
    Filed: September 4, 2015
    Date of Patent: May 2, 2017
    Assignee: ALLERGAN, INC.
    Inventors: Yariv Donde, Jeremiah H. Nguyen, Karen M. Kedzie, Daniel W. Gil, John E. Donello, Wha-Bin Im
  • Patent number: 9382188
    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: Grant
    Filed: February 12, 2013
    Date of Patent: July 5, 2016
    Assignee: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Seiji Miwatashi, Hideo Suzuki, Tomohiro Okawa, Yasufumi Miyamoto, Takeshi Yamasaki, Yuko Hitomi, Yasuhiro Hirata, Akito Shibuya
  • Patent number: 9353079
    Abstract: Provided herein are multiple solid forms of a defined ?,{acute over (?)}-disubstituted dihydroxy cyclopentyl compound, and methods for the preparation and use thereof. In one aspect, there are provided crystalline forms of said cyclopentyl compound, and methods for the preparation and use thereof. In another aspect, there are provided substantially amorphous forms of said dihydroxy cyclopentyl compound, and methods for the preparation and use thereof. In yet another aspect, there are provided compositions containing compounds according to the present invention. In certain aspects, such compositions are suitable for delivery of active agents according to the present invention to a subject in need thereof. In another aspect of the invention, there are provided methods for the treatment of a variety of indications, including glaucoma, ocular hypertension, and the like.
    Type: Grant
    Filed: December 12, 2014
    Date of Patent: May 31, 2016
    Assignee: ALLERGAN, INC.
    Inventors: Ke Wu, Gyorgy F. Ambrus
  • Patent number: 9296763
    Abstract: Disclosed herein are antimicrobial compounds compositions, pharmaceutical compositions, the use and preparation thereof. Some embodiments relate to 1 cyclic boronic acid ester derivatives and their use as therapeutic agents.
    Type: Grant
    Filed: July 29, 2013
    Date of Patent: March 29, 2016
    Assignee: Rempex Pharmaceuticals, Inc.
    Inventors: Gavin Hirst, Raja Reddy, Scott Hecker, Maxim Totrov, David C. Griffith, Olga Rodny, Michael N. Dudley, Serge Boyer
  • Patent number: 9289413
    Abstract: Prostamide-containing biodegradable intraocular implants, prostamide compounds, prostamide-containing pharmaceutical compositions, and methods for making and using such implants and compositions for the immediate and sustained reduction of intraocular pressure and treatment of glaucoma in an eye of a patient are described.
    Type: Grant
    Filed: March 14, 2014
    Date of Patent: March 22, 2016
    Assignee: Allergan, Inc.
    Inventors: Patrick M. Hughes, Jie Shen, Michael R. Robinson, David F. Woodward, Robert M. Burk, Hui Liu, Jinping Wan, Chandrasekar Durairaj, Gyorgy F. Ambrus, Ke Wu, Danny T. Dinh
  • Patent number: 9156810
    Abstract: Disclosed herein is a method comprising administering a compound to a mammal suffering from an inflammatory bowel disease for the treatment of said disease, said compound having a structure according to Formula I wherein X, Y, B, R2, R3, R4, R5, R6 and n have the meanings found herein.
    Type: Grant
    Filed: May 2, 2014
    Date of Patent: October 13, 2015
    Assignee: Allergan, Inc.
    Inventors: Yariv Donde, Jeremiah H. Nguyen, Karen M. Kedzie, Daniel W. Gil, John E. Donello, Wha-Bin Im
  • Patent number: 9133157
    Abstract: Compounds of Formula I are disclosed: wherein A, R1, R2, R3, R4A, R4B, R5, R6 and R7 are defined herein. The compounds encompassed by Formula I include compounds which are HIV protease inhibitors. The compounds and their pharmaceutically acceptable salts are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
    Type: Grant
    Filed: October 26, 2012
    Date of Patent: September 15, 2015
    Assignee: Merck Canada Inc.
    Inventors: Michael John Boyd, Jean-Francois Chiasson, Sheldon Crane, André Giroux
  • Patent number: 9084774
    Abstract: The present invention relates to co-crystals of duloxetine and co-crystal formers selected from COX-INHIBITORS, processes for preparation of the same and their uses as medicaments or in pharmaceutical formulations, more particularly for the treatment of pain.
    Type: Grant
    Filed: July 15, 2013
    Date of Patent: July 21, 2015
    Assignee: LABORATORIOS DEL DR. ESTEVE, S.A.
    Inventors: Helmut Heinrich Buschmann, Lluis Sola Carandell, Jordi Benet Buchholz, Jordi Carles Ceron Bertran, Jesus Ramirez Artero
  • Patent number: 9062075
    Abstract: The present invention relates to tetrahydropyridine derivatives of formula (1) which may be therapeutically useful as anti-bacterial agents, more particularly FabI inhibitors. in which X, Y, Z and “n” have the same meanings given in the specification, and pharmaceutically acceptable salts and pharmaceutically acceptable stereoisomers thereof that are useful in the treatment and prevention in diseases or disorder, in particular their use in diseases or disorder where there is an advantage in inhibiting Enoyl-ACP reductase enzyme (FabI) activity. The present invention also provides methods for synthesizing and administering the FabI inhibitory compounds. The present invention also provides pharmaceutical formulations comprising at least one of the FabI inhibitory compounds together with a pharmaceutically acceptable carrier, diluent or excipient therefor.
    Type: Grant
    Filed: June 3, 2014
    Date of Patent: June 23, 2015
    Assignees: Aurigene Discovery Technologies Limited, UM Pharmauji Sdn. BHD
    Inventors: Mohamed Takhi, Subramanya Hosahalli, Sunil Kumar Panigrahi
  • Patent number: 9051261
    Abstract: This invention relates to novel derivatives of 4-hydroxybutyric acid and prodrugs thereof, and pharmaceutically acceptable salts of the foregoing. This invention also provides pharmaceutical compositions comprising a compound of this invention and the use of such compositions in methods of treating narcolepsy, fibromyalgia, other disorders or conditions that are beneficially treated by improving nocturnal sleep or by administering sodium oxybate.
    Type: Grant
    Filed: June 10, 2013
    Date of Patent: June 9, 2015
    Assignee: Concert Pharmaceuticals, Inc.
    Inventor: Roger D. Tung
  • Publication number: 20150148359
    Abstract: Uses of a compound of any of Formulas I-VI as a cytotoxic inhibitor of undifferentiated cells are disclosed herein, as well as pharmaceutical compositions comprising a compound of any of Formulas I-VI, and methods for identifying a lead candidate for inhibiting undifferentiated cells. Further disclosed are uses of an SCD-1 inhibitor as a cytotoxic inhibitor of undifferentiated cells.
    Type: Application
    Filed: May 22, 2013
    Publication date: May 28, 2015
    Inventors: Uri Ben-David, Nissim Benvenisty, Payal Arora, Qing-Fen Gan, Ralph J. Garippa
  • Patent number: 9034914
    Abstract: The present invention relates to new salts of 6-(propyl-(2-thiophen-2-ylethyl)amino)tetralin-1-ol(rotigotine), their use as a medicament, for example for the treatment of CNS disorders like Parkinson Disease, RLS, fibromyalgia and/or depression, in particular through electromotive administration. The present invention relates to pharmaceutical formulations suitable for iontophoresis that provide enhanced iontophoretic delivery of rotigotine to at least one target tissue. The formulations are further characterized by good to excellent solubility of the salts in aqueous solutions.
    Type: Grant
    Filed: March 31, 2014
    Date of Patent: May 19, 2015
    Assignee: UCB PHARMA GMBH
    Inventors: Johanna Aaltje Bouwstra, Oliver Ackaert, Jacob Eikelenboom, Hans-Michael Wolff
  • Publication number: 20150126511
    Abstract: The invention relates to novel cyclohexylamine derivatives and their use in the treatment and/or prevention of central nervous system (CNS) disorders, such as depression, anxiety, schizophrenia and sleep disorder as well as methods for their synthesis. The invention also relates to pharmaceutical compositions containing the compounds of the invention, as well as methods of inhibiting reuptake of endogenous monoamines, such as dopamine, serotonin and norepinephrine from the synaptic cleft and methods of modulating one or more monoamine transporter.
    Type: Application
    Filed: September 30, 2014
    Publication date: May 7, 2015
    Inventors: Liming SHAO, Fengjiang WANG, Scott Christopher MALCOLM, Michael Charles HEWITT, Larry R. BUSH, Jianguo MA, Mark A. VARNEY, Una CAMPBELL, Sharon Rae ENGEL, Larry Wendell HARDY, Patrick KOCH, John E. CAMPBELL
  • 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: 20150119383
    Abstract: Embodiments disclosed herein generally relate to acamprosate formulations, methods of use of the formulations, to methods of using the formulations in combination with at least one other medication, and to combination products and compositions comprising the formulations and at least one other medication, such as neuroleptic (antipsychotic) and/or antidepressant drugs.
    Type: Application
    Filed: June 5, 2014
    Publication date: April 30, 2015
    Inventors: Barry S. Fogel, William D. Kerns, Kei-Lai Fong, San-Laung Chow, Edward Lin, David Wong
  • Publication number: 20150119315
    Abstract: This application provides methods of increasing vascularization, muscle performance, muscle rehabilitation, and/or mitochondrial activity in subjects in need thereof, by administering a therapeutically effective amount of one or more agents that increases ERR? activity to the subject. Such agents can include one or more ERR? agonists. In some examples the method does not require that the subject exercise, and as such, the subject may be sedentary (such as bedridden or in a wheelchair).
    Type: Application
    Filed: January 15, 2015
    Publication date: April 30, 2015
    Applicant: Salk Institute for Biological Studies
    Inventors: Vihang A. Narkar, Michael Downes, Ruth T. Yu, Ronald M. Evans
  • Publication number: 20150118282
    Abstract: A method for preventing the precipitation of rotigotine crystals, including a step of mixing rotigotine and one or more crystallization prevention agents selected from the group consisting of fatty alcohols, fatty acids, fatty acid esters, fatty acid amides, and the derivatives thereof, and to a transdermally absorbable preparation that includes rotigotine and crystallization prevention agents.
    Type: Application
    Filed: January 5, 2015
    Publication date: April 30, 2015
    Inventors: Hye-Min KIM, Yong-Youn Hwang, Won-No Youn, Yeo-Jin Park, Joon-Gyo Oh, Jong-Seob Im, Hun-Taek Kim
  • Publication number: 20150118309
    Abstract: Exemplary embodiments of the present invention relate to a method for preparing a preparation for percutaneous absorption, which includes rotigotine as an active ingredient, and more specifically, to a method for preparing a preparation for percutaneous absorption including mixing rotigotine and an ethylene-vinyl acetate adhesive so as to have a weight ratio of 1:(0.1 to 20), a preparation for percutaneous absorption manufactured by the method, and a percutaneous treatment system. The preparation and the system may prevent separation of the rotigotine, thereby increasing long-term storage stability, and effectively release the rotigotine, and thus can be effectively applied to preparing patch medication containing the rotigotine.
    Type: Application
    Filed: January 6, 2015
    Publication date: April 30, 2015
    Inventors: Hye-Min KIM, Yong-Youn HWANG, Won-No YOUN, Yeo-Jin PARK, Joon-Gyo OH, Jong-Seob IM, Hun-Taek KIM
  • Patent number: 9012493
    Abstract: The present invention provides a pest control agent having a novel skeleton, which can be synthesized industrially, and also has excellent biological activity and residual effects. Specifically, the present invention provides a 1-heterodiene derivative represented by Formula (1) or a salt thereof, and a pest control agent including, as an active ingredient, a 1-heterodiene derivative or a salt thereof.
    Type: Grant
    Filed: November 9, 2010
    Date of Patent: April 21, 2015
    Assignee: Nippon Soda Co., Ltd.
    Inventors: Jyun Takahashi, Takehiko Nakamura, Masahiro Miyazawa, Isami Hamamoto, Jyun Kanazawa
  • Patent number: 9012491
    Abstract: Disclosed herein are antimicrobial compounds compositions, pharmaceutical compositions, the use and preparation thereof. Some embodiments relate to cyclic boronate compounds and their use as therapeutic agents.
    Type: Grant
    Filed: August 30, 2012
    Date of Patent: April 21, 2015
    Assignee: Rempex Pharmaceuticals, Inc.
    Inventors: Raja K. Reddy, Serge Henri Boyer, Maxim Totrov, Scott Hecker
  • Publication number: 20150105429
    Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, A, B, C, R1, R2, R3, R4 and R5 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: Application
    Filed: December 18, 2014
    Publication date: April 16, 2015
    Applicant: GENENTECH, INC.
    Inventors: Benjamin Fauber, Olivier Rene
  • Patent number: 9006283
    Abstract: Disclosed are methods of inhibiting, regulating, and/or modulating the formation of soluble, globular, non-fibrillar, neurotoxic amyloid ?1-42 oligomers from amyloid ?1-42 monomers. Also disclosed are methods of treating a patient suffering from diseases associated with the formation of soluble, globular, non-fibrillar, neurotoxic amyloid ?1-42 oligomers.
    Type: Grant
    Filed: July 12, 2007
    Date of Patent: April 14, 2015
    Assignee: Acumen Pharmaceuticals, Inc.
    Inventors: Grant A. Krafft, Todd Pray, William F. Goure
  • Publication number: 20150099015
    Abstract: Methods and compositions are provided for treating neuropsychiatric disorders such as schizophrenia, depression, attention deficit disorder, mild cognitive impairment, dementia, and bipolar disorder. The methods entail administering to a patient diagnosed as having a neuropsychiatric disorder (e.g., schizophrenia, depression, attention deficit disorder, mild cognitive impairment, dementia bipolar disorder, etc.) or as at risk for a neuropsychiatric disorder a benzoic acid, benzoic acid salt, and/or benzoic acid derivative, and/or a sorbic acid, sorbic acid salt, and/or sorbic acid derivative, in combination with a neuropharmacological agent (e.g., an antipsychotic, an antidepressant, medications for attention deficit and hyperactivity disorder, cognitive impairment, or dementia, etc.) where the benzoic acid, benzoic acid salt, or benzoic acid derivative, and/or a sorbic acid, sorbic acid salt, and/or sorbic acid derivative, is in an amount sufficient to increase the efficacy of the neuropharmacological agent.
    Type: Application
    Filed: November 24, 2014
    Publication date: April 9, 2015
    Inventor: Guochuan Emil TSAI
  • Publication number: 20150080386
    Abstract: Disclosed are compounds and pharmaceutical compositions that are useful for treating a subject with a proliferative disorder, such as cancer. The disclosed compounds and pharmaceutical compositions are also useful for treating disorders responsive to Hsp70 induction and/or natural killer induction.
    Type: Application
    Filed: July 21, 2014
    Publication date: March 19, 2015
    Inventors: Keizo Koya, Teresa Kowalczyk Przewloka, Shoujun Chen, Jun Jiang
  • Publication number: 20150080451
    Abstract: Potent low molecular weight, highly selective, competitive non-peptidic serine protease inhibitors and their use in treating serine protease-associated diseases are disclosed.
    Type: Application
    Filed: September 12, 2012
    Publication date: March 19, 2015
    Applicant: THE JOHNS HOPKINS UNIVERSITY
    Inventors: Ernesto Freire, Patrick C. Ross, Rogelio Siles
  • Publication number: 20150065343
    Abstract: The present invention relates to acrylamide compounds which are useful for combating or controlling invertebrate pests, in particular arthropod pests and nematodes, and to a method for producing them. The invention also relates to a method for controlling invertebrate pests by using these compounds and to plant propagation material and to an agricultural and a veterinary composition comprising said compounds.
    Type: Application
    Filed: March 28, 2013
    Publication date: March 5, 2015
    Inventors: Pascal Bindschaedler, Wolfgang Von Deyn, Karsten Koerber, Florian Kaiser, Ralph Paulini, Deborah L. Culbertson, Paul Neese, Franz Josef Braun
  • Publication number: 20150065538
    Abstract: Compounds of formula (I) wherein R1, R2, R3, and Y are defined in the description are TRPA1 antagonists. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also disclosed.
    Type: Application
    Filed: November 4, 2014
    Publication date: March 5, 2015
    Inventors: Richard J. Perner, Michael E. Kort, Stanley DiDomenico, Jun Chen, Anil Vasudevan
  • Patent number: 8969404
    Abstract: A process for purifying a crude furan 2,5-dicarboxylic acid composition (cFDCA) by hydrogenation of a FDCA composition dissolved in a hydrogenation solvent such as water, and hydrogenating under mild conditions, such as at a temperature within a range of 130° C. to 225° C. by contacting the solvated FDCA composition with hydrogen in the presence of a hydrogenation catalyst under a hydrogen partial pressure within a range of 10 psi to 900 psi. A product FDCA composition is produced having a low amount of tetrahydrofuran dicarboxylic acid, a low b*, and a low amount of 5-formyl furan-2-carboxylic acid (FFCA).
    Type: Grant
    Filed: February 4, 2013
    Date of Patent: March 3, 2015
    Assignee: Eastman Chemical Company
    Inventors: Mesfin Ejerssa Janka, Charles Edwan Sumner, Jr., Shane Kipley Kirk, Ashfaq Shahanawaz Shaikh, Kenny Randolph Parker
  • Patent number: 8962677
    Abstract: Disclosed are methods of enhancing cognitive impairment in a patient wherein the cognitive impairment is due to ADDL neurotoxicity. The methods employ non-peptidic compounds having a molecular weight of less than 1000 and which can antagonize against formation of neurotoxic ADDLs from A?1-42 monomers.
    Type: Grant
    Filed: July 12, 2007
    Date of Patent: February 24, 2015
    Assignee: Acumen Pharmaceuticals, Inc.
    Inventors: Grant A. Krafft, Todd Pray, William F. Goure
  • Publication number: 20150045398
    Abstract: The present invention provides a compound of formula (I): said compound is inhibitor of MMP-2, and/or MMP-8, and/or MMP-9, and/or MMP-12 and/or MMP-13, and thus can be employed for the treatment of a disorder or disease characterized by abnormal activity of MMP-2, and/or MMP-8, and/or MMP-9, and/or MMP-12 and/or MMP-13. Accordingly, the compound of formula (I) can be used in treatment of disorders or diseases mediated by MMP-2, and/or MMP-8, and/or MMP-9, and/or MMP-12, and/or MMP-13. Finally, the present invention also provides a pharmaceutical composition.
    Type: Application
    Filed: October 7, 2014
    Publication date: February 12, 2015
    Applicant: NOVARTIS AG
    Inventors: Claus EHRHARDT, Leslie Wighton MCQUIRE, Pascal RIGOLLIER, Olivier ROGEL, Michael David SHULTZ, Ruben Alberto TOMMASI
  • Patent number: 8952041
    Abstract: The invention provides novel compositions and compounds that inhibit CatSper channel activity, that preferentially inhibits sperm hyperactivity over sperm motility, or both. The compounds of the invention are useful as contraceptive agents that may be adminstered to males, females, or concurrently to both sexual partners. The invention further provides methods of conducting drug discovery business and of conducting a reproductive medicine business. The invention also provides methods of identifying compounds that modulate sperm hypermotility.
    Type: Grant
    Filed: November 2, 2012
    Date of Patent: February 10, 2015
    Assignee: Hydra Biosciences, Inc.
    Inventors: Jayhong A. Chong, Magdalene M. Moran
  • Patent number: 8946219
    Abstract: The present invention is directed to pharmaceutical compositions and methods of using combination therapies containing [4-(6-fluoro-7-methylamino-2,4-dioxo-1,4-dihydro-2H-quinazolin-3-yl)-phenyl]-5-chloro-thiophen-2-yl-sulfonylurea, or a pharmaceutically acceptable salt thereof, for the treatment of thrombosis diseases.
    Type: Grant
    Filed: October 20, 2010
    Date of Patent: February 3, 2015
    Assignee: Portola Pharmaceuticals, Inc.
    Inventors: Pamela B. Conley, Patrick Andre, Uma Sinha
  • Publication number: 20150023921
    Abstract: The present invention relates to novel compositions having anti-viral activity and in particular it relates to synergistic compositions active against Hepatitis C virus (HCV). The invention also relates to methods for retarding, reducing or otherwise inhibiting HCV growth and/or functional activity.
    Type: Application
    Filed: April 3, 2014
    Publication date: January 22, 2015
    Applicant: BIOTRON LIMITED
    Inventors: Gary Dinneen EWART, Carolyn Anne LUSCOMBE, Michelle MILLER
  • 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: 20150011604
    Abstract: Compounds and their pharmaceutically acceptable salts for treatment of synucleinopathies, such as Parkinson's disease and tauopathies.
    Type: Application
    Filed: September 15, 2014
    Publication date: January 8, 2015
    Applicant: ProteoTech Inc.
    Inventors: Esposito A Luke, Marisa C Yadon, Joel Cummings, F Michael Hudson, Thomas Lake, Qubai Hu, Judy Cam, Alan D. Snow
  • Publication number: 20140377365
    Abstract: Provided herein are methods and compositions for producing formulations systemic delivery of dopamine agonists via the oral inhalation route. Specifically, provided herein are methods and compositions for a formulation of rotigotine that is suitable for administration via oral inhalation. Such methods and compositions are useful in the treatment or amelioration of one or more Parkinson's disease symptom(s).
    Type: Application
    Filed: June 18, 2014
    Publication date: December 25, 2014
    Inventors: Libo WU, Wiwik WATANABE
  • Publication number: 20140377329
    Abstract: The invention features sublingual film formulations of dopamine agonists and methods of treating Parkinson's disease, tremors, restless leg syndrome, sexual dysfunction, and depressive disorders therewith.
    Type: Application
    Filed: September 5, 2014
    Publication date: December 25, 2014
    Inventors: Nathan John BRYSON, Anthony John GIOVINAZZO, Scott David BARNHART, Michael Clinton KOONS
  • Publication number: 20140377369
    Abstract: The disclosure relates to a composition comprising rotigotine or a pharmaceutically acceptable salt thereof; at least one poly(lactide-co-glycolide) (PLGA); and at least one fatty acid, wherein the at least one fatty acid is at least 0.5% in weight relative to the total weight of the composition. The composition as disclosed herein has significantly reduced burse release effect. The disclosure also provides a method of treating Parkinson's disease comprising administering an effective amount of the composition as disclosed to a subject in need thereof.
    Type: Application
    Filed: November 25, 2011
    Publication date: December 25, 2014
    Inventors: Youxin LI, Aiping WANG, Wanhui LIU, Kaoxiang SUN, Jun LI, Lifang SUN
  • Publication number: 20140378917
    Abstract: The present invention provides transdermal therapeutic systems for dispensing a pharmaceutical product, in particular a pharmaceutical product with a low tendency to spontaneously crystallize. The matrix layer or at least one of the matrix layers in said systems contains a silicone hot-melt adhesive, a pharmaceutical product, and particles made of crosslinked polyvinylpyrrolidone. The invention also relates to a method for producing said transdermal therapeutic systems.
    Type: Application
    Filed: December 28, 2012
    Publication date: December 25, 2014
    Inventors: Horst Dzekan, Hans-Rainer Hoffmann, Michael Horstmann, Walter Mueller, Sandra Wiedersberg
  • 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