C=o Bonded Directly To The Six-membered Hetero Ring Patents (Class 514/354)
  • Patent number: 11147804
    Abstract: The invention relates to the field of animal health. In particular, the invention relates to an oral solid dosage form comprising, as pharmaceutically active compounds, amlodipine. The invention relates to an oral solid dosage forms comprising an amlodipine besylate according to a particular posology for the treatment of hypertension in non-human mammal animals.
    Type: Grant
    Filed: March 31, 2016
    Date of Patent: October 19, 2021
    Assignee: CEVA SANTE ANIMALE
    Inventors: Romain Charles, Rosita Garcia
  • Patent number: 11135208
    Abstract: Provided herein are pharmaceutical compositions comprising a class of calcium channel blockers and at least one chelating agent. More specifically, the pharmaceutical compositions comprise at least one 1,4-dihydropyridine (DHP) compound and at least one chelating agent. The chelating agents used in this disclosure can decrease the degradation of the constituent DHPs of the DHP compositions. The DHP compositions can be used to treat cardiovascular disorders and are more stable for prolonged periods of time.
    Type: Grant
    Filed: March 11, 2020
    Date of Patent: October 5, 2021
    Assignee: American Regent, Inc.
    Inventors: Daniel Walter Wehrung, Meng Zhong, Saral Pinkal Patel, Bindhu Madhavi Rayaprolu
  • Patent number: 11053219
    Abstract: Described herein are pyridine compounds of Formula (XIII) that are useful in treating a TYK2-mediated disorder.
    Type: Grant
    Filed: July 24, 2020
    Date of Patent: July 6, 2021
    Assignee: Esker Therapeutics, Inc.
    Inventors: Bohan Jin, Qing Dong, Gene Hung, Stephen W. Kaldor
  • Patent number: 9955690
    Abstract: A fungicidal composition containing a fungicidally effective amount of a compound of Formula I-V and at least one fungicide selected from the group consisting of epoxiconazole, prothioconazole, azoxystrobin, pyraclostrobin, penthiopyrad, isopyrazam, bixafen, boscalid, prochloraz, and chlorothalonil provides synergistic control of selected fungi.
    Type: Grant
    Filed: November 11, 2014
    Date of Patent: May 1, 2018
    Assignee: DOW AGROSCIENCES LLC
    Inventors: W. John Owen, Chenglin Yao
  • Patent number: 9834521
    Abstract: This invention relates to compounds of the general formula (I): in which the variable groups are as identified herein, and to preparation and use of the compounds.
    Type: Grant
    Filed: March 13, 2014
    Date of Patent: December 5, 2017
    Assignee: ARIAD Pharmaceuticals, Inc.
    Inventors: Stephan G. Zech, Anna Kohlmann, Feng Li, Yihan Wang, Tianjun Zhou, David C. Dalgarno, William C. Shakespeare, Xiaotian Zhu
  • Patent number: 9642897
    Abstract: The invention relates generally to the field of bone diseases. More specifically, the invention relates to methods and compositions for the treatment of osteoporosis and related disorders.
    Type: Grant
    Filed: September 13, 2012
    Date of Patent: May 9, 2017
    Assignee: THE UNIVERSITY OF SYDNEY
    Inventors: Gustavo Duque, Christopher Vidal
  • Patent number: 9579381
    Abstract: The invention provides method of treating a subject suffering from, or at risk of developing, a Mycobacterium infection by administering to the subject a therapeutically-effective amount of isotopically labeled isoniazid and/or ethionamide, or an analog, derivative or prodrug thereof, and exposing the subject to a magnetic field.
    Type: Grant
    Filed: September 6, 2013
    Date of Patent: February 28, 2017
    Assignee: STC.UNM
    Inventors: Graham Timmins, Seong Won Choi
  • Patent number: 9499487
    Abstract: In one aspect, the invention relates to compounds having the formula: where R1, R2, R3, X, R4, R5, and R6 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
    Type: Grant
    Filed: May 18, 2012
    Date of Patent: November 22, 2016
    Assignee: Theravance Biopharma R&D IP, LLC
    Inventors: Melissa Fleury, Roland Gendron, Adam D. Hughes, Jane Schmidt
  • Patent number: 9321716
    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 metabolic syndrome may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of hyperuricemia, gout, dyslipidemia, obesity, urea cycle disorders, hyperglycemia, insulin resistance, diabetes mellitus, diabetes insipidus, type 1 diabetes, type 2 diabetes, microvascular complications, macrovascular complications, lipid disorders, prediabetes, obesity, arrhythmia, myocardial infarction, stroke, neuropathy, renal complications, hypertriglyceridemia, cardiovascular complications, and post prandial hyperglycemia.
    Type: Grant
    Filed: November 5, 2014
    Date of Patent: April 26, 2016
    Assignee: CELLIX BIO PRIVATE LIMITED
    Inventor: Mahesh Kandula
  • Patent number: 9174977
    Abstract: The present invention provides compounds of formula (I) including stereoisomers or a racemate or a mixture or a pharmaceutically acceptable salt thereof: wherein X is NH, or O; Q is 5-6 membered heteroaryl group, which may be substituted by one or more substituents independently selected from a group consisting of: C1-C4 alkyl, halogen, halo C1-C4 alkyl, C1-C4 alkoxy, CN; A is phenyl or a 5-6 heteroaryl group, which may be substituted by one or more substituents independently selected from a group consisting of: C1-C4 alkyl, halogen, halo C1-C4 alkyl, C1-C4 alkoxy, CN; B may assume different meanings from A and is phenyl or a 5-6 membered heteroaryl group, which may be substituted by one or more substituents independently selected from a group consisting of: C1-C4 alkyl, halogen, halo C1-C4 alkyl, C1-C4 alkoxy, CN; and processes for their preparation, pharmaceutical compositions containing them and their use as dual antagonists of the Orexin 1 and Orexin 2 receptors.
    Type: Grant
    Filed: March 18, 2013
    Date of Patent: November 3, 2015
    Assignee: Rottapharm Biotech S.R.L.
    Inventors: Luigi Piero Stasi, Lucio Claudio Rovati
  • Patent number: 9144572
    Abstract: Compositions for topical use including menthyl nicotinate as primary active ingredient, in such a dose as to stimulate in a subject the sexual response, preferably in such a dose as to maximize this response in a relative short time, and at least one appropriate lipophilic vehicle so as to solubilize the menthyl nicotinate and allow a rapid absorption thereof in the epithelial tissues of the female and/or male erogenous zones.
    Type: Grant
    Filed: July 30, 2014
    Date of Patent: September 29, 2015
    Assignee: MULTICHEM S.A.S. DI GABRIELE SEGALLA
    Inventor: Gabriele Segalla
  • 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
  • Publication number: 20150141415
    Abstract: The present invention relates to methods for treating an infectious disease in a subject in need thereof via administration of a therapeutically effective amount of compounds described herein. The methods may utilize particular compounds, for example, a quinoline, a hydrazone, a quinone, or a pyrimidine derivatives thereof or a pharmaceutical salts thereof.
    Type: Application
    Filed: November 7, 2014
    Publication date: May 21, 2015
    Inventors: Omonike Arike Olaleye, Sarah Finney John, Adaugo Chimzurum Isichei, Jun O Liu, Rosa Maldonado, Janice Endsley
  • Publication number: 20150141433
    Abstract: Compounds that selectively negatively modulate NMDA receptors containing an NR2A subunit, pharmaceutical compositions comprising the compounds, and methods of treating a disease using the compounds are disclosed.
    Type: Application
    Filed: September 26, 2014
    Publication date: May 21, 2015
    Inventors: David R. Anderson, Robert A. Volkmann
  • Publication number: 20150133430
    Abstract: Provide herein are compounds and pharmaceutical compositions suitable as modulators of hemoglobin, methods and intermediates for their preparation, and methods for their use in treating disorders mediated by hemoglobin and disorders that would benefit from tissue and/or cellular oxygenation.
    Type: Application
    Filed: January 16, 2015
    Publication date: May 14, 2015
    Inventors: Qing XU, Zhe LI
  • Patent number: 9029559
    Abstract: The present invention relates to compounds of the formula I, wherein A, D, E, L, G, R10, R30, R40, R50 and R60 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. They are inhibitors of the protease cathepsin A, and are useful for the treatment of diseases such as atherosclerosis, heart failure, renal diseases, liver diseases or inflammatory diseases, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.
    Type: Grant
    Filed: January 17, 2014
    Date of Patent: May 12, 2015
    Assignee: SANOFI
    Inventors: Sven Ruf, Thorsten Sadowski, Klaus Wirth, Herman Schreuder, Christian Buning
  • Patent number: 9018383
    Abstract: The present invention relates to compounds of the formula I, wherein A, Y, Z, R20 to R22 and R50 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. Specifically, they are inhibitors of the endothelial differentiation gene receptor 2 (Edg-2, EDG2), which is activated by lysophosphatidic acid (LPA) and is also termed as LPA1 receptor, and are useful for the treatment of diseases such as atherosclerosis, myocardial infarction and heart failure, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.
    Type: Grant
    Filed: November 27, 2013
    Date of Patent: April 28, 2015
    Assignee: Sanofi
    Inventors: Josef Pernerstorfer, Heinz-Werner Kleemann, Matthias Schaefer, Alena Safarova, Marcel Patek
  • Patent number: 9006249
    Abstract: The present invention provides a compound of formula I?; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, X and n are defined herein. The invention also relates to a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
    Type: Grant
    Filed: June 7, 2012
    Date of Patent: April 14, 2015
    Assignee: Novartis AG
    Inventors: Gary Mark Coppola, Yuki Iwaki, Rajeshri Ganesh Karki, Toshio Kawanami, Gary Michael Ksander, Muneto Mogi, Robert Sun
  • Publication number: 20150094294
    Abstract: The present disclosure provides compounds, specifically pyrimidin-4,6-dicarboxylic acid amide derivatives, or pharmaceutically acceptable salts thereof and pharmaceutical compositions containing said compounds. Also provided are methods for treating a mammal having malaria, or killing or inhibiting the growth of a Plasmodium species, comprising administering to said mammal or contacting said Plasmodium species with, an effective amount of a pyrimidin-4,6-dicarboxylic acid amide derivative.
    Type: Application
    Filed: February 28, 2013
    Publication date: April 2, 2015
    Inventors: Richard W. Scott, Robert W. Kavash, Wenxi Pan, Katie Freeman, Michael J. Costanzo, Doron Greenbaum, Yongjiang Xu, Trevor Young
  • Patent number: 8986664
    Abstract: The invention provides a method for improving hair biology, e.g., hair growth. The method comprises administering to a subject a monoamine oxidase inhibitor and a vasodilator, a zinc salt of a carboxylic acid, a xanthine compound, pyrithione or a salt thereof, saponin, tritapene, crataegolic acid, celastrol, asiatic acid, an inhibitor of 5-alpha-reductase, 1,4-methyl-4-azasteroid, an androgen receptor antagonist, azelaic acid or a derivate thereof, cyclosporin, triiodothyronine, diazoxide, retinoic acid, a prostaglandin analog, aminexil, carnitine tartrate, apigenin, procapil, or adenosine, in an amount effective to achieve a desired effect. The invention further provides a method of reducing or delaying the appearance of an age-related skin imperfection. The method comprises administering to the subject a composition comprising an MAO inhibitor. A kit for improving hair growth also is provided.
    Type: Grant
    Filed: October 13, 2011
    Date of Patent: March 24, 2015
    Assignee: The Procter & Gamble Company
    Inventors: Teresa DiColandrea, Robert Scott Youngquist, Sancai Xie, Robert Lloyd Binder, Gary Richard Fuentes, Deborah Lade
  • Patent number: 8987304
    Abstract: The present invention provides antituberculous therapeutic drugs with a higher potency. The present invention provides also antituberculous therapeutic drugs containing oxazole compounds represented by (I) general formula (1): [wherein R1 represents a hydrogen atom or C1-6 alkyl group, n represents an integer of 0-6, and R2 represents general formula (A) or the like, wherein R3 represents a phenoxy group (at least one group selected from the group consisting of a halogen atom, an optionally halogen-substituted C1-6 alkyl group and an optionally halogen-substituted C1-6 alkoxy group may be substituted on the phenyl ring) or the like], optically active forms thereof or salts thereof, and drugs (II) such as primary antituberculous drugs.
    Type: Grant
    Filed: October 4, 2006
    Date of Patent: March 24, 2015
    Assignee: Otsuka Pharmaceutical Co., Ltd.
    Inventors: Makoto Matsumoto, Hiroyuki Hashizume, Tatsuo Tomishige, Masanori Kawasaki, Yoshihiko Shimokawa
  • Publication number: 20150080351
    Abstract: Compounds are provided that act as potent antagonists of the CCR9 receptor, and which have been further confirmed in animal testing for inflammation, one of the hallmark disease states for CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR9-mediated diseases, and as controls in assays for the identification of CCR9 antagonists.
    Type: Application
    Filed: November 24, 2014
    Publication date: March 19, 2015
    Inventors: Solomon Ungashe, John J. Wright, Andrew Pennell, Zheng Wei
  • Patent number: 8975256
    Abstract: A 1,2,3,4-tetrahydroquinoxaline compound represented by the following formula: In the formula (1), R1 represents substituents such as a halogen, an alkyl, a cycloalkyl, an aryl or a heterocyclic group; p represents 0 to 5; R2 represents substituents such as a halogen, an alkyl, a hydroxyl or an alkoxy group; q represents 0 to 2; R3 represents substituents such as hydrogen, an alkyl, an alkenyl, an alkylcarbonyl or an arylcarbonyl group; R4 and R5 independently represent substituents such as hydrogen, a halogen, an alkyl, an alkenyl, an alkynyl, a cycloalkyl, an aryl or a heterocyclic group; R6 represents substituents such as hydrogen, an alkyl, an alkenyl, an alkynyl, a cycloalkyl, an aryl or a heterocyclic group; A represents an alkylene; R7 represents OR8, NR8R9, SR8, S(O)R8, S(O)2R8; R8 and R9 independently represent substituents such as hydrogen, an alkyl or an alkenyl; and X represents O or S.
    Type: Grant
    Filed: July 9, 2013
    Date of Patent: March 10, 2015
    Assignee: Santen Pharmaceutical Co., Ltd.
    Inventors: Mamoru Matsuda, Toshiyuki Mori, Kenji Kawashima, Minoru Yamamoto, Masatomo Kato, Miwa Takai, Masato Nagatsuka, Sachiko Kobayashi
  • Patent number: 8969312
    Abstract: A pharmaceutical composition for treating tuberculotic diseases with no side effect/low side effect is provided by the present invention, which pharmaceutically effective amount of one or more compounds chosen from isoniazid, rifampin, pyrazinamide and ethambutol, and pharmaceutically effective amount of substances which can reduce the side effect of the antituberculosis agents.
    Type: Grant
    Filed: April 20, 2011
    Date of Patent: March 3, 2015
    Assignee: National Defense Education and Research Foundation
    Inventors: Oliver Yaopu Hu, Tonho Young, Chenghuei Hsiong, Wenliang Chang, Tungyuan Shih, Hsintien Ho
  • Publication number: 20150057289
    Abstract: The present invention provides bicyclo[3.2.1]octyl amide derivatives of formula (I): wherein L, R1 and R2 are as defined herein, or a pharmaceutically acceptable salt thereof; and pharmaceutical compositions and methods using the same.
    Type: Application
    Filed: November 4, 2014
    Publication date: February 26, 2015
    Inventors: Guiying Li, Hao Zhou, Jesse Weiss, Dario Doller, James Ford Burns
  • Patent number: 8962661
    Abstract: To provide a fungicidal composition having stable and high fungicidal effects against cultivated crops infected with plant diseases resulting from plant diseases. A fungicidal composition containing, as active ingredients, (a) a benzoylpyridine derivative represented by the formula (I) or its salt: wherein when A is —N?, B is —CX4?; when A is —CH?, B is —N?; each of X1 and X2 which are independent of each other, is a halogen atom, an alkoxy group, a hydroxyl group, an alkyl group, a CF3 group or an alkylthio group; X3 is a hydrogen atom, a halogen atom, an alkoxy group, an alkyl group, a CF3 group or an alkylthio group; X4 is a hydrogen atom, a halogen atom, an alkoxy group, an alkyl group, a CF3 group or an alkylthio group; R1 is an alkyl group; R2? is an alkoxy group; p is 0, 1 or 2; and each of R2? and R2?? is an alkoxy group, and (b) at least one additional fungicide.
    Type: Grant
    Filed: June 30, 2009
    Date of Patent: February 24, 2015
    Assignee: Ishihara Sangyo Kaisha, Ltd.
    Inventors: Munekazu Ogawa, Akihiro Nishimura
  • Patent number: 8962003
    Abstract: The invention provides methods for controlling thrips populations using thrips-repelling and/or thrips-attracting agents. The invention also provides methods of preventing or minimizing damage to plants by use of the same.
    Type: Grant
    Filed: November 12, 2004
    Date of Patent: February 24, 2015
    Assignee: The New Zealand Institute for Plant and Food Research Limited
    Inventors: Melanie Millicent Davidson, David Austin John Teulon, Nigel Brian Perry
  • Publication number: 20150045397
    Abstract: The invention relates to substituted pyridine and pyrimidine compounds of Formula (I) and the pharmaceutically acceptable salts, prodrugs, and solvates thereof, wherein R1, R2a, R2b, A1, A2, X, and Z are defined as set forth in the specification. The invention is also directed to the use of compounds of Formula (I) to treat a disorder responsive to the blockade of sodium channels. Compounds of the present invention are especially useful for treating pain.
    Type: Application
    Filed: March 15, 2013
    Publication date: February 12, 2015
    Inventors: Laykea Tafesse, Jiangchao Yao
  • Patent number: 8952040
    Abstract: Pharmaceutical composition for treating coagulation disorder hemorrhage. The pharmaceutical composition comprises (per unit): L-ornithine 0.5˜8 g, aspartic acid 1˜5 g, arginine 3˜10 g and vitamin B6 3˜10 g. A method of administrating the pharmaceutical composition to treat hemorrhage patients caused by coagulation dysfunction, especially critically ill patients.
    Type: Grant
    Filed: December 10, 2010
    Date of Patent: February 10, 2015
    Inventors: Maoxing Yue, Honggui Wan, Tongge Huang
  • Patent number: 8952171
    Abstract: Provide herein are compounds and pharmaceutical compositions suitable as modulators of hemoglobin, methods and intermediates for their preparation, and methods for their use in treating disorders mediated by hemoglobin and disorders that would benefit from tissue and/or cellular oxygenation.
    Type: Grant
    Filed: March 15, 2013
    Date of Patent: February 10, 2015
    Assignee: Global Blood Therapeutics, Inc.
    Inventors: Qing Xu, Zhe Li
  • Patent number: 8946270
    Abstract: The subject matter disclosed herein is directed to amido-pyridyl ether compounds of formula I: wherein, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, Ra, a, b and d are as described herein, compositions comprising the compounds of formula I, methods for their preparation and methods for their uses against parasites.
    Type: Grant
    Filed: June 27, 2012
    Date of Patent: February 3, 2015
    Assignee: Merial Limited
    Inventors: Charles Q. Meng, Clare Louise Murray, Itta Bluhn-Chertudi, Mustapha Soukri, Mary George Johnson
  • Patent number: 8937091
    Abstract: The present invention relates to: a ketone compound having transglutaminase-inhibiting activity, which is represented by the following Formula 1, 2, or 3: wherein R1 is a substituted or unsubstituted aryl or heterocyclyl group, R2, R3, and R4 are hydrogen atoms, n is 2, X is halogen, R5 and R6 independently represent a hydrogen atom or a substituted or unsubstituted C1-C10 alkyl, aryl, or aralkyl group, wherein R5 and R6 are not hydrogen atoms at the same time, or R5 and R6 may be taken together to form a saturated or unsaturated and substituted or unsubstituted heterocyclyl group containing a nitrogen atom (N); an inhibitor of protein crosslinking comprising the compound; and a composition for preventing or treating a protein-crosslinking causative disease, which comprises the compound or the protein crosslinking inhibitor.
    Type: Grant
    Filed: May 19, 2010
    Date of Patent: January 20, 2015
    Assignee: Japan Science and Technology Agency
    Inventors: Katsuhiko Mikoshiba, Kozo Hamada, Akiko Terauchi, Shouichirou Ozaki, Jun-ichi Goto, Etsuko Ebisui, Akinobu Suzuki
  • Publication number: 20150005320
    Abstract: The invention relates to compounds of formula (I): or a pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof wherein X, Y, A, Z, L and n are defined herein. These compounds are useful as immunosuppressive agents and for treating and preventing inflammatory conditions and immune disorders.
    Type: Application
    Filed: September 27, 2013
    Publication date: January 1, 2015
    Applicant: Synta Pharmaceuticals Corp.
    Inventors: Yu Xie, Mats Holmqvist, Jerome Mahiou, Mitsunori Ono, Lijun Sun, Shoujun Chen, Shijie Zhang, Jun Jiang, Dinesh Chimmanamada, Chih-Yi Yu
  • Patent number: 8920843
    Abstract: Particles of an organic acid salt of an amino acid amide or ester local anesthetic are employed as agents for the improved alleviation of pain. Particularly, the particles find use with surgically created wounds, where the particles may be administered directly into the bed of the wound or topically for transdermal transport.
    Type: Grant
    Filed: November 7, 2008
    Date of Patent: December 30, 2014
    Assignee: SVIP5 LLC
    Inventors: Samuel P. Sawan, Daniel Jacobs, Tadmor Shalon
  • Patent number: 8921370
    Abstract: The present invention provides bicyclo[3.2.1]octyl amide derivatives of formula (I): wherein L, R1 and R2 are as defined herein, or a pharmaceutically acceptable salt thereof; and pharmaceutical compositions and methods using the same.
    Type: Grant
    Filed: December 22, 2011
    Date of Patent: December 30, 2014
    Assignee: H. Lundbeck A/S
    Inventors: Guiying Li, Hao Zhou, Jesse Weiss, Dario Doller, James Ford Burns
  • Publication number: 20140378461
    Abstract: Compounds of the formula (I), in which the substituents are as defined in claim 1, are suitable for use as nematicides.
    Type: Application
    Filed: February 14, 2013
    Publication date: December 25, 2014
    Applicant: SYNGENTA PARTICIPATIONS AG
    Inventors: Anthony Cornelius O'Sullivan, Olivier Loiseleur, Daniel Stierli, Torsten Luksch, Thomas Pitterna
  • Publication number: 20140371195
    Abstract: The present application discloses compounds capable of modulating the activity of histone demethylases (HDMEs), which are useful for prevention and/or treatment of diseases in which genomic dysregulation is involved in the pathogenesis, such as e.g. cancer. The present application also discloses pharmaceutical compositions comprising said compounds and the use of such compounds as a medicament.
    Type: Application
    Filed: August 28, 2014
    Publication date: December 18, 2014
    Inventors: Marc Labelle, Thomas Boesen, Mukund Mehrotra, Qasim Khan, Farman Ullah
  • Publication number: 20140357677
    Abstract: The present application relates to a new salt of N-methyl-4-benzylcarbami-dopyridine, a process for its preparation, a pharmaceutical composition comprising this compound and its use for the treatment or prevention of viral diseases.
    Type: Application
    Filed: May 16, 2013
    Publication date: December 4, 2014
    Inventors: Filya Zhebrovska, Grygorii Kostiuk, Mykhailo Vanat, Viktor Margitych
  • Publication number: 20140357678
    Abstract: A pharmaceutically acceptable salt, prodrug or derivative compound of the formula I, wherein R1 is selected from H, a (C1-C5) alkyl group and a COR4 group; R2 is selected from H, a (C1-C5) alkyl group and a COR5 group; R3 is selected from H, a (C1-C5) alkyl group, a (C1-C5)-O-alkyl group, a cycloalkyl of (C5-C6) carbon atoms, an aryl group, and an aryl (C1-C5) alkyl group wherein the aryl group can be an unsubstituted aryl or substituted with one or more R6 groups and an NHCOR5 group, or the R2 and R3 groups together with N may form a piperidine, morpholine or piperazine group; R4 is selected from H and a (C1-C5)alkyl group; R5 is selected from an aryl group unsubstituted or substituted with one or more R6, linear or branched(C1-C5) alkyl or pyridyne groups and a pyridine group; R6 is selected from (C1-C5)alkyl groups, halogen and nitro.
    Type: Application
    Filed: January 10, 2013
    Publication date: December 4, 2014
    Inventors: Gerardo Burton, Javier Duran, David Martinez, Elvira Zini, Veronica Mora Munoz, Lucila Bertoncello
  • Patent number: 8889678
    Abstract: The present invention relates to acyl guanidine derivatives modulating the hedgehog protein signaling pathway to be used as drugs, in particular for treating diseases involving a tissue dysfunction associated with a deregulation of the hedgehog protein signaling pathway, as well as to pharmaceutical compositions containing same. The present invention also relates to novel acyl guanidine derivatives as such.
    Type: Grant
    Filed: July 19, 2010
    Date of Patent: November 18, 2014
    Assignees: Centre National de la Recherche Scientifique, Universite de Strasbourg
    Inventors: Martial Ruat, Hélène Faure, Elisabeth Traiffort, Hermine Roudaut, André Mann, Angèle Schoenfelder, Maurizio Taddei, Fabrizio Manetti, Antonio Solinas
  • Patent number: 8889262
    Abstract: The present application relates to wood preservation, for example, surfactants and phospholipids for improving wood preservation. Included are surfactants and phospholipids containing a 2-amino-N,N-dimethylacetamide. Provided are wood preservative compositions containing these surfactants or phospholipids, methods of applying such wood preservative compositions to wood, and wood products resultant from some such methods. Also provided are wood products containing the wood preservative compositions provided herein.
    Type: Grant
    Filed: July 16, 2012
    Date of Patent: November 18, 2014
    Assignee: Empire Technology Development LLC
    Inventor: Atsushi Mizusawa
  • Publication number: 20140329854
    Abstract: Provided are novel heterocyclic sirtuin binding agents, e.g., N-aryl substituted pyridine dicarboxamides, which are useful as sirtuin modulators. Also provided are methods of using the pyridine dicarboxamide compounds for treating sirtuin mediated disorders and conditions, such as diabetes, cancers, and obesity and diseases related to aging.
    Type: Application
    Filed: December 12, 2012
    Publication date: November 6, 2014
    Applicant: SMB Innovation
    Inventors: Bjarne Due Larsen, Soren Andersen, Marianne Spanget Larsen
  • Publication number: 20140323528
    Abstract: The present invention relates to novel triazole derivatives of formula (I) having insecticidal activity, to processes and intermediates for preparing them, to insecticidal, acaricidal, nematicidal or molluscicidal compositions comprising them and to methods of using them to combat and control insect, acarine, nematode or mollusc pests wherein R1, R2, G1, G2, Q1 and Q2 are as defined in claim 1; or salts or N-oxides thereof.
    Type: Application
    Filed: September 21, 2012
    Publication date: October 30, 2014
    Applicant: SYNGENTA PARTICIPATIONS AG
    Inventors: Ottmar Franz Hueter, Peter Renold, Peter Maienfisch, Pierre Joseph Marcel Jung, Thomas Pitterna, Christopher Richard Ayles Godfrey, Elke Maria Hillesheim, Andre Stoller
  • Publication number: 20140309228
    Abstract: The present disclosure provides substituted pyridine and pyrimidine compounds of Formula (I): A1-X-A2-Z-R1 (I) and the pharmaceutically acceptable salts, solvates and prodrugs thereof, wherein A, X, A, Z, and R are defined as set forth in the specification. The present disclosure is also directed to the use of compounds of Formula (I) to treat a disorder responsive to the blockade of sodium channels. Compounds of the present disclosure are especially useful for treating pain.
    Type: Application
    Filed: October 30, 2012
    Publication date: October 16, 2014
    Applicant: Purdue Pharma L.P.
    Inventor: John J. Engel
  • Patent number: 8859591
    Abstract: The present invention provides a compound of Formula (I) or a pharmaceutically acceptable salt thereof wherein R1, R2, R3, A1, A2, A3, A4, L, B1, B2, B3 and B4 are as defined herein. The compounds of Formula I have been found to act as glucagon antagonists or inverse agonists. Consequently, the compounds of Formula I and the pharmaceutical compositions thereof are useful for the treatment of diseases, disorders, or conditions mediated by glucagon.
    Type: Grant
    Filed: July 3, 2013
    Date of Patent: October 14, 2014
    Assignee: Pfizer Inc.
    Inventors: Gary Erik Aspnes, Mary Theresa Didiuk, Kevin James Filipski, Angel Guzman-Perez, Esther Cheng Yin Lee, Jeffrey Allen Pfefferkorn, Benjamin Dawson Stevens, Meihua Mike Tu
  • Publication number: 20140288034
    Abstract: A compound having an ability to bind to an S1P receptor and represented by formula (I), a salt thereof, a solvate thereof or a prodrug thereof is useful for prevention and/or treatment of rejection of transplantation, graft-versus-host disease, autoimmune disease, allergic disease and the like: wherein ring A is a cyclic group; ring B is a cyclic group which may have substituent(s); X is a spacer having 1 to 8 atoms in its main chain, etc.; Y is a spacer having 1 to 10 atoms in its main chain, etc.; n is 0 or 1, wherein when n is 0, m is 1 and R1 is a hydrogen atom or a substituent, and wherein when n is 1, m is 0 or an integer of 1 to 7 and R1 is a substituent, and wherein m is 2 or more, R1s are the same or different.
    Type: Application
    Filed: June 4, 2014
    Publication date: September 25, 2014
    Applicant: ONO PHARMACEUTICAL CO., LTD.
    Inventors: Shinji NAKADE, Hirotaka Mizuno, Takeji ONO, Masashi Minami, Hiroshi Saga, Hiroshi Hagiya, Takaki Komiya, Hiromu Habashita, Haruto Kurata, Kazuhiro Ohtsuki, Kensuke Kusumi
  • Patent number: 8841331
    Abstract: Compounds of formula I: wherein a, R1, R2, R3, R4, R5 and R6 are defined herein, are useful as inhibitors of HIV replication.
    Type: Grant
    Filed: November 21, 2012
    Date of Patent: September 23, 2014
    Assignee: Gilead Sciences, Inc.
    Inventors: Christiane Yoakim, Murray D. Bailey, Francois Bilodeau, Rebekah Carson, Lee Fader, Stephen Kawai, Sebastien Morin, Carl Thibeault, Bruno Simoneau, Simon Surprenant, Youla S. Tsantrizos, Steven R. Laplante
  • Patent number: 8841457
    Abstract: The present invention describes a process for preparing a cyclooxygenase-2 selective inhibitor. It provides a synthetic procedure for the said substance namely 5-chloro-3-(4-methylsulphonyl)phenyl-2-(2-methyl-5-pyridinyl)pyridine of formula (I). The invention also relates to preparation of a new intermediate of formula (IV) and a process to prepare it. Furthermore, the invention describes a process for preparing another key intermediate of formula (II). Compounds of formula (IV) and formula (II) are useful intermediates in synthesis of the said cyclooxygenase-2 inhibitor.
    Type: Grant
    Filed: November 15, 2011
    Date of Patent: September 23, 2014
    Assignee: Virdev Intermediates Pvt. Ltd.
    Inventors: Dharmesh Mahendra Shah, Sanjay Amratlal Solanki, Viral Narendra Jariwala, Ashok Vasantray Vyas, Ashokkumar Bhikhubhai Mistry
  • Publication number: 20140275008
    Abstract: Provide herein are compounds and pharmaceutical compositions suitable as modulators of hemoglobin, methods and intermediates for their preparation, and methods for their use in treating disorders mediated by hemoglobin and disorders that would benefit from tissue and/or cellular oxygenation.
    Type: Application
    Filed: March 15, 2013
    Publication date: September 18, 2014
    Inventors: Qing Xu, Zhe Li
  • Patent number: RE45499
    Abstract: The crystalline Polymorph B of N-(2-aminophenyl)-4-[N-(pyridine-3-yl)methoxy-carbonyaminomethyl]benzamide (MS-275) of formula I is described, as well as the process for the production of said compound, and its use as a medicament for the treatment of selected diseases.
    Type: Grant
    Filed: March 7, 2014
    Date of Patent: April 28, 2015
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Matthias Schneider, Michael Gottfried, Jens Geisler, Gabriele Winter, Joji Suzuki, Tomoyuki Ando, Masaru Honjo