Patents Issued in August 6, 2015
  • Publication number: 20150218099
    Abstract: Methods for controlling aquatic weeds that involve the use of 4-amino-3-chloro-6-(4-chloro-2-fluoro-3-methoxyphenyl)pyridine-2-carboxylic acids and agriculturally acceptable esters or salts thereof are described. Preferred herbicidal compositions allow for effective control and/or selectivity when treating a body of water to control target aquatic weed populations, such as a hydrilla, Eurasian watermilfoil and/or curlyleaf pondweed.
    Type: Application
    Filed: January 29, 2015
    Publication date: August 6, 2015
    Applicant: DOW AGROSCIENCES LLC
    Inventor: Richard K. Mann
  • Publication number: 20150218100
    Abstract: (E)-2-(2-Quinolin-2-yl-propenyl)-phenol, 2-Quinolin-2-yl-ylethynyl-phenol and salts thereof are useful as medicaments, especially for treatment of an angiogenesis-related disease or disorder.
    Type: Application
    Filed: July 15, 2013
    Publication date: August 6, 2015
    Inventors: Breandan Douglas Kennedy, Alison Reynolds, Claire Kilty, Jacintha O'Sullivan, Andrew Douglas Baxter
  • Publication number: 20150218101
    Abstract: The present invention provides a quinolone compound represented by General Formula (1) or a salt thereof, wherein R1 represents a hydrogen atom, etc.; R2 represents a hydrogen atom, etc.; R3 represents a phenyl group optionally being substituted with one or more substituents, etc.; R4 represents a halogen atom; R5 represents a hydrogen atom or halogen atom; R6 represents a hydrogen atom; and R7 represents a hydroxyl group, etc. The quinolone compound have a functional improvement effect, which suppresses progression of neurological dysfunction by inhibiting the chronic progression of Parkinson's disease or protecting dopamine neurons from the disease etiology, thereby prolonging the period before first administration begins.
    Type: Application
    Filed: April 15, 2015
    Publication date: August 6, 2015
    Applicant: OTSUKA PHARMACEUTICAL CO., LTD.
    Inventors: Kenji OTSUBO, Yuji OCHI, Masami NAKAI, Atsushi MORI
  • Publication number: 20150218102
    Abstract: Compounds of formula (I) and pharmaceutically acceptable salts, esters, amides, or radiolabelled forms thereof, wherein R1, R2, and R3 are as defined in the specification, are useful in treating conditions or disorders prevented by or ameliorated by voltage-gated sodium channels, e.g., Nav1.7 and/or Nav1.8. Methods for making the compounds are disclosed. Also disclosed are pharmaceutical compositions of compounds of formula (I), and methods for using such compounds and compositions.
    Type: Application
    Filed: February 4, 2015
    Publication date: August 6, 2015
    Inventors: Andrew Bogdan, Marlon D. Cowart, David A. DeGoey, Tammie K. Jinkerson, John R. Koenig, Michael E. Kort, Bo Liu, Mark A. Matulenko, Derek W. Nelson, Meena V. Patel, Hillary Peltier, Marc J. Scanio, Brian D. Wakefield
  • Publication number: 20150218103
    Abstract: The present invention provides compounds and composition comprising analogs of deprenyl and their use in the inhibition of nuclear GAPDH-Siahl binding and the activation of p300 and MEF2. Also provided herein are methods of prevention and treatment of stress induced disorders of the body, including, for example, major mental illness, such as schizophrenia, mood disorders, and addiction, as well as stress-associated diseases involving other organs, such as cardiac hypertrophy, in vivo, comprising administering to a mammal a therapeutically effective amount of analogs of deprenyl.
    Type: Application
    Filed: August 19, 2013
    Publication date: August 6, 2015
    Inventors: Akira Sawa, Elki Takimoto, Neelam Shahani, David Kass, Toshiaki Saito
  • Publication number: 20150218104
    Abstract: Disclosed are compounds of Formula (I): wherein R1 is CH2CH2CF3 or CH2CH2CH3; R2 is CH2CH2CF3, CH2CH2CH3, CH2(cyclopropyl), phenyl, or; R3 is H; Ra, Rb, y, and z are defined herein. Also disclosed are methods of using such compounds to inhibit the Notch receptor, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as cancer.
    Type: Application
    Filed: September 20, 2013
    Publication date: August 6, 2015
    Inventor: Ashvinikumar V. Gavai
  • Publication number: 20150218105
    Abstract: The present invention is a method for producing a 1-substituted-3-fluoroalkylpyrazole-4-caroxylic acid ester, the method comprising a step of adding, to a first reaction liquid containing an alkyl hydrazine and a first organic solvent, a second reaction liquid containing an acyl acetic acid ester derivative and a second organic solvent in 0.5 to 30 hours to react the first reaction liquid with the second reaction liquid at a reaction temperature of ?5 to 80° C. under stirring in the absence of a base and an acid, wherein the first organic solvent and the second organic solvent are each at least any one of benzene, toluene, xylene, chlorobenzene, dichlorobenzene, ethyl acetate, butyl acetate, and dimethyl carbonate, a total mass of the first organic solvent and the second organic solvent is 1 to 60 times a mass of the acyl acetic acid ester derivative, and an amount of the first organic solvent in a total amount of the first organic solvent and the second organic solvent is 40 to 95% by mass.
    Type: Application
    Filed: March 14, 2013
    Publication date: August 6, 2015
    Inventors: Hirobumi Nobeshima, Naoki Koyama, Masayuki Harada
  • Publication number: 20150218106
    Abstract: Provided herein are compounds of the formula (I), as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of inflammatory diseases and disorders such pulmonary fibrosis.
    Type: Application
    Filed: September 2, 2013
    Publication date: August 6, 2015
    Inventors: David Budd, Yimin Qian, Ryan Craig Schoenfeld, Achyutharao Sidduri
  • Publication number: 20150218107
    Abstract: The present invention provides compounds having the formula: wherein R1 is selected from methyl, ethyl, propyl, cyclopropyl, and dimethyl, or a pharmaceutically acceptable salt thereof, along with methods and intermediates for their preparation, and uses thereof.
    Type: Application
    Filed: October 18, 2013
    Publication date: August 6, 2015
    Applicant: Eli Lily and Company
    Inventors: Timothy Barrett Durham, Jothirajah Marimuthu, Michael Robert Wiley
  • Publication number: 20150218108
    Abstract: The present invention relates to a carbon nanomaterial having a higher order structure by means of multiple hydrogen bonds and to a method for preparing same. One of the key technical features of the present invention is a carbon nanomaterial having a higher order structure, in which a functional group capable of multiple hydrogen bonds reacts with a conductive carbon nanomaterial, into which said functional group is introduced by a surface modification to be functionalized, thus enabling multiple hydrogen bonds between carbon nanomaterials.
    Type: Application
    Filed: May 9, 2012
    Publication date: August 6, 2015
    Inventors: Joong-tark Han, Geon-woong Lee, Seung-yol Jeong, Hee-jin Jeong, Bo hwa Jeong
  • Publication number: 20150218109
    Abstract: Compounds having a c-Rel inhibiting property according to the formula: (1) wherein R1 and R2 are each independently selected from hydrogen atom and hydrocarbon groups having at least one and up to thirty carbon atoms and optionally substituted with one or more heteroatoms selected from halogen, nitrogen, oxygen, and sulfur; R3 is selected from hydrocarbon groups having at least one and up to thirty carbon atoms and optionally substituted with one or more heteroatoms selected from halogen, nitrogen, oxygen, and sulfur; and X1, X2, and X3 are each independently selected from oxygen and sulfur atoms. Methods for treating diseases and conditions associated with c-Rel overexpression by administering compounds of Formula (1) or a pharmaceutical composition thereof to a subject afflicted with such a disease or condition are also described.
    Type: Application
    Filed: September 19, 2013
    Publication date: August 6, 2015
    Inventors: Hsiou-Chi Liou, Mei-Ling Liou, Samedy Ouk
  • Publication number: 20150218110
    Abstract: The use of substituted benzodiazepinones and benzazepinones of the general formula (I) or salts thereof where the radicals in the general formula (I) correspond to the definitions given in the description, for enhancing stress tolerance in plants to abiotic stress, for strengthening plant growth and/or for increasing plant yield, and to selected processes for preparing the compounds mentioned above.
    Type: Application
    Filed: September 2, 2013
    Publication date: August 6, 2015
    Inventors: Jens Frackenpohl, Ines Heinemann, Thomas Mueller, Guido Bojack, Jan Dittgen, Pascal Von Koskull-Doering, Dirk Schmutzler, Martin Jeffrey Hills, Juan Pedro Ruiz-Santaella Moreno
  • Publication number: 20150218111
    Abstract: Disclosed are compounds of Formula (I): wherein: R2 is phenyl, fluorophenyl, chlorophenyl, trifluorophenyl, methylisoxazolyl, or pyridinyl; R3 is H, CH3, CH2(cyclopropyl), pyridinyl, chloropyridinyl, or methoxypyridinyl: and Ra, Rb, y, and z are defined herein. Also disclosed are methods of using such compounds to inhibit the Notch receptor, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as cancer.
    Type: Application
    Filed: September 20, 2013
    Publication date: August 6, 2015
    Inventors: Ashvinikumar V. Gavai, Weifang Shan, James Aaron Balog, Claude A. Quesnelle, Wen-Ching Han, George V. DeLucca, Daniel O'Malley, Brian E. Fink
  • Publication number: 20150218112
    Abstract: The present invention relates to compounds of formula (I) and (IV), and pharmaceutically acceptable salts, tautomers, stereoisomers thereof, which are inhibitors of histone deacetylase (HDAC). The compounds of the present invention are for use in the treatment of disorders that are ameliorated by inhibition of HDAC such as cancer and hemoglobinopathies like ?-thalassemia or sickle cell anemia.
    Type: Application
    Filed: August 7, 2013
    Publication date: August 6, 2015
    Inventors: Sergio Altamura, Alberto Bresciani, Giulia Breveglieri, Danilo Fabbrini, Roberto Gambari, Steven Harper, Ralph Laufer, Edith Monteagudo, Emanuela Nizi, Paola Pace, Vincenzo Summa
  • Publication number: 20150218113
    Abstract: The present invention provides an industrially advantageous method for producing a 1,4-benzoxazine compound useful as a medicine while avoiding safety and health risks. Specifically, the present invention provides a method for producing a 1,4-benzoxazine compound [A], which comprises the three steps in the following scheme, namely, a step of converting the amino group at 7-position in a compound [a] into a dimesylamino group, a step of coupling a compound [b] with a boronic acid compound, and a step of converting the 7-position in a compound [c] into a monomesylamino group. In the above scheme, Ms is a methanesulfonyl group, and each of R? and R? is a hydrogen atom etc.
    Type: Application
    Filed: August 8, 2013
    Publication date: August 6, 2015
    Applicant: MITSUBISHI TANABE PHARMA CORPORATION
    Inventors: Tomoyuki Okabe, Takeshi Hamada, Kaori Tomikawa, Yukie Okamoto, Toru Iijima, Hidenori Akatsuka, Kenichi Toyama, Atsushi Moroda, Yoshihiro Sugiura
  • Publication number: 20150218114
    Abstract: A compound that can be a therapeutic agent for underactive bladder which has low risk of side effects and can be administered orally is provided. Furthermore, a crystal which is advantageous in view of the stability, long-term storage, handleability, easiness of the drug preparation or the like as a drug substance of medicaments is provided. Since a salt of 2-[(2-{(1R,5R)-2-oxo-5-[(1E,4S)-7,8,8-trifluoro-4-hydroxy-4-methyl-1,7-octadien-1-yl]cyclopentyl}ethyl)thio]-1,3-thiazole-4-carboxylic acid or a diastereomeric mixture thereof and 4-piperidinemethanol is a chemically very stable crystal, it can be stored for a long time, and is very useful as a drug substance of medicaments.
    Type: Application
    Filed: August 30, 2013
    Publication date: August 6, 2015
    Applicant: ONO PHARMACEUTICAL CO., LTD.
    Inventors: Kousuke Tani, Akihiro Kinoshita, Keisuke Hanada, Yoshiyuki Aratani, Takahiro Nekado, Atsushi Shimabukuro
  • Publication number: 20150218115
    Abstract: Various materials and polymers having electron deficient moieties and methods of synthesizing thereof are described herein. Specifically, a C—H bond activation method is disclosed wherein an electron deficient group having one or more activated C—H bonds is coupled to one or more aryl groups to afford materials or polymers which may be used in organic electronic and photonic applications.
    Type: Application
    Filed: January 30, 2015
    Publication date: August 6, 2015
    Inventors: Seth Marder, Junxiang Zhang
  • Publication number: 20150218116
    Abstract: This invention relates to compounds and uses thereof in the treatment or prophylaxis of diseases associated with inflammation.
    Type: Application
    Filed: July 25, 2013
    Publication date: August 6, 2015
    Inventors: Margaret Harnett, William Harnett, Colin J. Suckling, Fraser Scott, Judith K. Huggan, Abedawn I. Khalaf
  • Publication number: 20150218117
    Abstract: The present invention relates to a method for producing tetrahydrofuran, comprising feeding 1,4-butanediol to a reactor and performing a cyclodehydration reaction in the presence of an acid catalyst to obtain tetrahydrofuran, in which a water concentration in a in-reactor liquid phase is within a range of 1.4 to 10 wt %.
    Type: Application
    Filed: April 17, 2015
    Publication date: August 6, 2015
    Applicant: MITSUBISHI CHEMICAL CORPORATION
    Inventors: Ryo YAMASHITA, Seijiro NISHIMURA, Hisashi NAGAHAMA
  • Publication number: 20150218118
    Abstract: A process for the production of furan derivatives from carbohydrates in the presence of an acidic catalyst, characterized in that N-methylpyrrolidone is used as a solvent and that the acidic catalyst is homogeneous.
    Type: Application
    Filed: September 2, 2013
    Publication date: August 6, 2015
    Inventors: Marko Mihovilovic, Michael Schön, Johanna Hölbling
  • Publication number: 20150218119
    Abstract: The present invention relates to novel benzofuran-2-sulfonamide derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.
    Type: Application
    Filed: January 5, 2015
    Publication date: August 6, 2015
    Inventors: HAIQING YUAN, RICHARD L. BEARD, XIAOXIA LIU, JOHN E. DONELLO, VEENA VISWANATH, MICHAEL E. GARST
  • Publication number: 20150218120
    Abstract: Provided herein, inter alia, are novel compounds for the inhibition of HIV integrase. The compounds disclosed herein are useful for methods of treating HIV infection in a subject in need thereof.
    Type: Application
    Filed: February 5, 2015
    Publication date: August 6, 2015
    Inventors: Seth M. Cohen, Arpita Agrawal, Jamie DeSoto, Yves Pommier, Kasthuraiah Maddali
  • Publication number: 20150218121
    Abstract: Described herein are ?9-THC prodrugs, methods of making ?9-THC prodrugs, formulations comprising ?9-THC prodrugs and methods of using ?9-THC. One embodiment described herein relates to the transdermal administration of a ?9-THC prodrug for treating and preventing diseases and/or disorders.
    Type: Application
    Filed: February 11, 2015
    Publication date: August 6, 2015
    Applicant: Zynerba Pharmaceuticals, Inc.
    Inventors: Audra Lynn STINCHCOMB, Miroslaw Jerzy GOLINSKI, Dana Carmel HAMMELL, Jeffrey Lynn HOWARD
  • Publication number: 20150218122
    Abstract: The present invention features processes for preparing compounds, such as (R)-1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)-N-(1-(2,3-dihydroxypropyl)-6-fluoro-2-(1-hydroxy-2-methylpropan-2-yl)-1H-indol-5-yl)cyclopropanecarboxamide (Compound 1), useful for treating CFTR mediated diseases such as cystic fibrosis.
    Type: Application
    Filed: April 15, 2015
    Publication date: August 6, 2015
    Inventors: Gerald J. Tanoury, Cristian Harrison, Benjamin Joseph Littler, Peter Jamison Rose, Robert Michael Hughes, Young Chun Jung, David Andrew Siesel, Elaine Chungmin Lee, Daniel T. Belmont
  • Publication number: 20150218123
    Abstract: An object of the present invention is to provide an optically active bicyclic ?-amino acid derivative in a high purity.
    Type: Application
    Filed: February 6, 2015
    Publication date: August 6, 2015
    Applicant: Daiichi Sankyo Company, Limited
    Inventors: Yoshitaka NAKAMURA, Kazutoshi UKAI, Takafumi KITAWAKI, Takumi NAKAJIMA, Yutaka KITAGAWA, Yukito FURUYA, Makoto IMAI, Eiji NUMAGAMI, Masakazu WAKAYAMA, Ayako SAITO
  • Publication number: 20150218124
    Abstract: Compounds of formula (I), wherein R1 is as defined in the claims, exhibit COMT enzyme inhibiting activity and are thus useful as COMT inhibitors. Methods of treatment and pharmaceutical dosage forms are also disclosed.
    Type: Application
    Filed: May 23, 2013
    Publication date: August 6, 2015
    Inventors: Marko Ahlmark, David Din Belle, Mika Kauppala, Anne Luiro, Taina Pajunen, Jarmo Pystynen, Eija Tianen, Matti Vaismaa, Josef Messinger
  • Publication number: 20150218125
    Abstract: The present invention provides a composition for preventing or treating kidney disease, the composition comprising a pyrazole derivative compound or a pharmaceutically acceptable salt thereof; and the composition of the present invention is effective in reducing proteinuria, reducing cell formation between glomerular blood vessels and suppressing kidney fibrosis.
    Type: Application
    Filed: August 2, 2013
    Publication date: August 6, 2015
    Inventors: Yun Soo Bae, Hun Joo Ha, Kee In Lee, Kyung Hee Song
  • Publication number: 20150218126
    Abstract: The present invention related to crystalline forms of thalidomide having a high polymorphic purity and to processes for their preparation. The present invention also relates to pharmaceutical preparations comprising the crystalline forms for the treatment of patients suffering from autoimmune, inflammatory or angiogenic disorders.
    Type: Application
    Filed: February 12, 2015
    Publication date: August 6, 2015
    Applicant: GENERICS [UK] LIMITED
    Inventors: Vinayak Govind Gore, Vinay Kumar Shukla, Madhukar Patil, Sandeep Mekde
  • Publication number: 20150218127
    Abstract: The invention relates to compound of the formula I or a salt thereof, wherein the substituents are as defined in the specification; to its preparation, to its use as medicament and to medicaments comprising it.
    Type: Application
    Filed: April 14, 2015
    Publication date: August 6, 2015
    Applicant: NOVARTIS AG
    Inventors: Yves AUBERSON, Mark Gary BOCK, Dario BRAGA, Marco CURZI, Stephanie Kay DODD, Stefano Luca GIAFFREDA, Hayang JIANG, Piotr KARPINSKI, Thomas J. TROXLER, Telin WANG, Xiaoyang WANG, Xuechun ZHANG
  • Publication number: 20150218128
    Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of degenerative diseases and disorders.
    Type: Application
    Filed: April 14, 2015
    Publication date: August 6, 2015
    Inventors: Craig C. Beeson, Christopher C. Lindsey, Yuri K. Peterson, Baerbel Rohrer
  • Publication number: 20150218129
    Abstract: The present invention relates to novel acrylamide compounds of formula (I), and their pharmaceutically acceptable salts and process of their preparation. (The chemical formula should be inserted here.) The compounds of formula (I) are useful in the treatment of various disorders that related to Histamine H3 receptors.
    Type: Application
    Filed: December 5, 2012
    Publication date: August 6, 2015
    Inventors: Ramakrishna Nirogi, Anil Karbhari Shinde, Adi Reddy Dwarampudi, Venkateswarlu Jasti
  • Publication number: 20150218130
    Abstract: The disclosed compounds are useful in the treatment of mammalian cancers and especially human cancers. Compounds, pharmaceutical compositions, and methods of Formula I are disclosed: or a pharmaceutically acceptable salt, hydrate, solvate, enantiomer, stereoisomer, or tautomer thereof.
    Type: Application
    Filed: January 22, 2015
    Publication date: August 6, 2015
    Inventors: Daniel L. Flynn, Michael D. Kaufman
  • Publication number: 20150218131
    Abstract: The present invention relates to compounds of formula wherein R1 is phenyl, optionally substituted by halogen, lower alkyl, lower cycloalkyl, lower alkoxy, cyano, lower alkyl substituted by halogen, lower alkyl substituted by hydroxy, lower alkoxy substituted by halogen or lower alkoxy substituted by hydroxy; or is pyridine-2, 3 or 4-yl, optionally substituted by halogen, lower alkyl, lower cycloalkyl, cyano, lower alkyl substituted by halogen, lower alkyl substituted by hydroxy, lower alkoxy, lower alkoxy substituted by halogen or lower alkoxy substituted by hydroxyl; or is pyrimidin-2, 4 or 5-yl, optionally substituted by halogen, lower alkyl, lower cycloalkyl, lower alkyl substituted by hydroxy or lower alkyl substituted by halogen; or is pyrazin-2-yl, optionally substituted by halogen, lower alkyl, lower cycloalkyl, lower alkyl substituted by halogen, lower alkyl substituted by hydroxy or cyano; or is 2,2-difluorobenzo[d][1,3]dioxol-5-yl, or is thiazolyl, optionally substituted by lower alkyl substit
    Type: Application
    Filed: March 13, 2015
    Publication date: August 6, 2015
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Guido Galley, Roger Norcross, Philippe Pflieger
  • Publication number: 20150218132
    Abstract: The present disclosure relates to novel synthetic substituted heterocyclic compounds and pharmaceutical compositions containing the same. The disclosure further concerns the use of such compounds in the treatment and/or prevention of certain types of cancers, pain, inflammation, restenosis, atherosclerosis, psoriasis, thrombosis, Alzheimer's, a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination.
    Type: Application
    Filed: February 5, 2015
    Publication date: August 6, 2015
    Inventor: Jay Jie-Qiang Wu
  • Publication number: 20150218133
    Abstract: The invention is concerned with the compounds of formula (I) and pharmaceutically acceptable salts thereof. 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) can be used as medicament.
    Type: Application
    Filed: April 17, 2015
    Publication date: August 6, 2015
    Applicant: HOFFMANN-LA ROCHE INC.
    Inventors: Zhi Chen, Shawn David Erickson
  • Publication number: 20150218134
    Abstract: Provided are: a method for producing a cycloalkanol derivative that enables the production of an azole derivative at low cost and with high yield; and a method for producing an azole derivative. In a process of producing a cycloalkanol derivative represented by general formula (I), a reaction step of azolylmethylating a cycloalkanone derivative represented by general formula (II) is carried out using an azole compound represented by general formula (III) in the presence of a sulfur ylide. In this step, the sulfur ylide is produced from a sulfonium compound or sulfoxonium compound and an alkali metal methoxide in a reaction system.
    Type: Application
    Filed: October 2, 2013
    Publication date: August 6, 2015
    Inventors: Taiga Masano, Keiichi Sudo
  • Publication number: 20150218135
    Abstract: Novel crystalline polymorphic forms, Forms A, B, C, D, and E of a compound of Formula I, which has been found to be a potent inhibitor of LFA-1, are disclosed. Methods of preparation and uses thereof in the treatment of LFA-1 mediated diseases are also disclosed in this invention.
    Type: Application
    Filed: September 19, 2014
    Publication date: August 6, 2015
    Inventors: John BURNIER, Thomas GADEK, Frederic NAUD
  • Publication number: 20150218136
    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 neurologic diseases may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of depression, Alzheimer's disease, multiple sclerosis, Batten disease, multiple sclerosis, Parkinson's disease (PD) and restless legs syndrome (RLS).
    Type: Application
    Filed: April 19, 2013
    Publication date: August 6, 2015
    Inventor: Mahesh KANDULA
  • Publication number: 20150218137
    Abstract: There are provided compounds of formula I, wherein R, R1, Ra, Rb, Q, X and Y have meanings given in the description, which compounds have antiinflammatory activity (e.g., through inhibition of one or more of members of: the family of p38 mitogen-activated protein kinase enzymes; Syk kinase; and members of the Src family of tyrosine kinases) and have use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, eye and intestines.
    Type: Application
    Filed: August 16, 2013
    Publication date: August 6, 2015
    Inventors: Claire Anne Marie Cariou, Catherine Elisabeth Charron, Euan Alexander Fraser Fordyce, Daniel Hamza, Matthew Colin Thor Fyfe, Kazuhiro Ito, John King-Underwood, Peter John Murray, Stuart Thomas Onions, Stephen Malcolm Thom, Hayley Tegan Angela Watson, Jonathan Gareth Williams
  • Publication number: 20150218138
    Abstract: The present invention provides compounds of the formula (I), or the pharmaceutically acceptable salts thereof, wherein G, W, R2, R3, R4, R5 and R6 are as defined in the specification. Further objects of the invention are processes and intermediates for the preparation of the compounds of the formula (I), pharmaceutical compositions comprising them and methods for treating cell proliferative disorders. As a matter of fact, the compounds of the formula (I) are useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer.
    Type: Application
    Filed: April 16, 2015
    Publication date: August 6, 2015
    Applicant: NERVIANO MEDICAL SCIENCES S.R.L.
    Inventors: Ermes Vanotti, Marina Caldarelli, Alessandra Cirla, Barbara Forte, Antonella Ermoli, Maria Menichincheri, Antonio Pillan, Alessandra Scolaro
  • Publication number: 20150218139
    Abstract: The present invention relates to carbamates of formula (I), wherein the variables are defined according to the description, as well as to a process for manufacturing carbamates of formula (I), and to the use of carbamates of formula (I) in manufacturing benzoxazinones of formula (VII).
    Type: Application
    Filed: July 29, 2013
    Publication date: August 6, 2015
    Inventors: Maximilian Dochnahl, Roland Götz, Joachim Gebhardt, Uwe Josef Vogelbacher, Timo Frassetto, Michael Rack, Volker Maywald, Bernd Wolf
  • Publication number: 20150218140
    Abstract: The present invention relates to a process for manufacturing benzoxazinones of formula (I), wherein the variables are defined according to the description, by reacting carbamates of formula (II) are reacted with carbamat-benzoxazinones of formula (III) in the presence of a base.
    Type: Application
    Filed: August 9, 2013
    Publication date: August 6, 2015
    Inventors: Maximilian Dochnahl, Roland Goetz, Joachim Gebhardt, Uwe Josef Vogelbacher, Timo Frassetto, Michael Rack, Volker Maywald, Bernd Wolf
  • Publication number: 20150218141
    Abstract: The invention is concerned with the compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein Y, R1 and R3 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 of the TRPA1 channel and may be useful in treating inflammatory diseases and disorders associated with that channel.
    Type: Application
    Filed: April 16, 2015
    Publication date: August 6, 2015
    Applicant: HOFFMANN-LA ROCHE INC.
    Inventors: Christine E. Brotherton-Pleiss, Zhi Chen, Shawn David Erickson, Kyungjin Kim, Hongju Li, Allen John Lovey, Yimin Qian, Sung-Sau SO, Peter Michael Wovkulich, Lin Yi
  • Publication number: 20150218142
    Abstract: The present invention relates to compounds characterized by having a structure according to the following Formula I: or a pharmaceutically acceptable salt thereof. Compounds of the present invention are useful for the treatment or prevention of HIV.
    Type: Application
    Filed: December 14, 2012
    Publication date: August 6, 2015
    Applicant: GlaxoSmithKline LLC
    Inventors: Mark Andrew Hatcher, Brian Alvin Johns, Michael Tolar Martin, Elie Amine Tabet, Jun Tang
  • Publication number: 20150218143
    Abstract: Sulfonamide compounds having TRPM8 antagonistic activity are provided. A sulfonamide compound of formula (I) or a pharmaceutically acceptable salt thereof, or a prodrug thereof: wherein Ring A is bicyclic aromatic heterocycle comprised of (a) pyridine is condensed with benzene; or (b) pyridine is condensed with monocyclic aromatic heterocycle, and Ring A binds to a sulfonylamino moiety on a carbon atom adjacent to a nitrogen atom of the pyridine ring constituting Ring A, Ring B is (a) monocyclic or bicyclic aromatic hydrocarbon; (b) monocyclic or bicyclic alicyclic hydrocarbon; (c) monocyclic or bicyclic aromatic heterocycle; or (d) monocyclic or bicyclic non-aromatic heterocycle, Ring C is (a) benzene; or (b) monocyclic aromatic heterocycle, and other symbols are the same as defined in the specification.
    Type: Application
    Filed: February 12, 2015
    Publication date: August 6, 2015
    Applicant: MITSUBISHI TANABE PHARMA CORPORATION
    Inventors: Yasuyuki TSUZUKI, Daisuke SAWAMOTO, Toshiaki SAKAMOTO, Taku KATO, Yasuki NIWA, Nobumasa AWAI
  • Publication number: 20150218144
    Abstract: The invention is concerned with the compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein Y, R1, R2 and R3 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 of the TRPA1 channel and may be useful in treating inflammatory diseases and disorders associated with that channel.
    Type: Application
    Filed: April 10, 2015
    Publication date: August 6, 2015
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Christine E. Brotherton-Pleiss, Zhi Chen, Shawn David Erickson, Kyungjin Kim, Hongju Li, Yimin Qian, Sung-Sau So, Peter Michael Wovkulich, Lin Yi
  • Publication number: 20150218145
    Abstract: The present invention provides a process for the preparation of rivaroxaban in a process that includes cyclizing a compound of Formula (II) with a dialkyl carbonate in the presence of a base.
    Type: Application
    Filed: September 26, 2013
    Publication date: August 6, 2015
    Inventors: Mohammed Salman Hashmi, Yoginder Pal Sachdeva
  • Publication number: 20150218146
    Abstract: The invention relates to novel oxindole derivatives of general formula (I), wherein the substituents R1, R2, A, B, and Y are defined as in Claim 1. The invention further relates to medicaments containing said derivatives, and use thereof for the prevention and/or treatment of vasopressin-dependent diseases.
    Type: Application
    Filed: April 13, 2015
    Publication date: August 6, 2015
    Inventors: Thorsten Oost, Wilfried Lubisch, Wolfgang Wernet, Wilfried Hornberger, Liliane Unger, Hervé Geneste, Astrid Netz
  • Publication number: 20150218147
    Abstract: The invention provides compounds for inhibiting glycosidases, prodrugs of the compounds, and pharmaceutical compositions including the compounds or prodrugs of the compounds. The invention also provides methods of treating diseases and disorders related to deficiency or overexpression of O-GlcNAcase, accumulation or deficiency of O-GlcNAc.
    Type: Application
    Filed: August 29, 2013
    Publication date: August 6, 2015
    Inventors: Ernest J. McEachern, Jianyu Sun, David J. Vocadlo, Yuanxi Zhou, Harold G. Selnick
  • Publication number: 20150218148
    Abstract: Provided are SUMO activators, which can enhance SUMOylation of SERCA2a, which are useful in the treatment of heart failure, cardiovascular diseases, cancer, neurodegenerative disorders, viral infection, bacterial infection, liver disease, inflammation, and other diseases.
    Type: Application
    Filed: August 29, 2013
    Publication date: August 6, 2015
    Inventors: Russell Dahl, Ah Young Lee, Changwon Kho, Roger J. Hajjar