1,2-oxazoles (including Hydrogenated) Patents (Class 514/378)
  • Patent number: 10561641
    Abstract: This invention relates to long-acting injectable formulations for combating parasites in animals, comprising at least one isoxazoline active agent, a poloxamer, and a co-solvent. This invention also provides for improved methods for eradicating, controlling, and preventing parasite infections and infestations in an animal comprising administering the long-acting injectable formulations of the invention to the animal in need thereof.
    Type: Grant
    Filed: February 26, 2016
    Date of Patent: February 18, 2020
    Assignee: BOEHRINGER INGELHEIM ANIMAL HEALTH USA INC.
    Inventors: Susan Mancini Cady, Peter Cheifetz, Izabela Galeska, Loic Le Hir de Fallois
  • Patent number: 10508309
    Abstract: Disclosed herein are assays and methods for distinguishing a keratoacanthoma from squamous cell carcinoma. Methods for diagnosing a keratoacanthoma are also provided. Methods for treating variants of seborrheic keratoses (i.e., keratoacanthoma, acanthosis nigricans, or epidermal nevus) are also provided.
    Type: Grant
    Filed: May 16, 2014
    Date of Patent: December 17, 2019
    Assignee: THE GENERAL HOSPITAL CORPORATION
    Inventors: Victor A. Neel, Anna I. Mandinova
  • Patent number: 10472324
    Abstract: A compound of the formula (I) or a tautomeric isoform thereof wherein R1 is selected from the group consisting of halogen, nitro, lower alkyl sulfonyl, cyano, trifluromethyl lower alkyl, lower alkoxy, lower alkoxycarbonyl, carboxy, lower alkyl aminosulfonyl, perfluoro lower alkyl, lower alkylthio, hydroxy lower alkyl, alkoxy lower alkyl, lower alkylthio lower alkyl, lower alkylsulfinyl lower alkyl, lower alkylsulfonyl lower alkyl, lower alkylsulfonyl, lower alkanoyl, aroyl, aryl, aryloxy and R2 is selected from the group consisting of hydrogen, alkyl, alkoxy, alkylthio, and alkylcarbonyl, and their non-toxic, pharmaceutically acceptable base addition salts or pro-drugs thereof. The compounds of the invention are useful in the treatment of nervous system diseases and disorders, which are responsive to modulation of the GABAA receptor complex.
    Type: Grant
    Filed: March 15, 2015
    Date of Patent: November 12, 2019
    Assignee: ALGIAX PHARMACEUTICALS GMBH
    Inventors: Birgit Hasse, Guido Koopmans
  • Patent number: 10450277
    Abstract: Novel compounds having a formula embodiments of a method of making the same, and of a composition comprising them are disclosed herein. Also disclosed are embodiments of a method of treating or preventing a metabolic disorder in a subject, comprising administering to a subject (e.g., via the gastrointestinal tract) a therapeutically effective amount of one or more of the disclosed compounds, thereby activating FXR receptors in the intestines, and treating or preventing a metabolic disorder in the subject. Additionally disclosed are embodiments of a method of treating or preventing inflammation in an intestinal region of a subject, comprising administering to the subject (e.g., via the gastrointestinal tract) a therapeutically effective amount of one or more of the disclosed compounds, thereby activating FXR receptors in the intestines, and thereby treating or preventing inflammation in the intestinal region of the subject.
    Type: Grant
    Filed: November 27, 2018
    Date of Patent: October 22, 2019
    Assignees: The Salk Institute for Biological Studies, University of Sydney
    Inventors: Ronald M. Evans, Michael Downes, Annette Atkins, Sungsoon Fang, Jae Myoung Suh, Thomas J. Baiga, Ruth T. Yu, John F. W. Keana, Christopher Liddle
  • Patent number: 10273231
    Abstract: The present invention relates to compounds of formula I wherein the variables are as defined in the claims and the description. The invention further relates to the use of these compounds for controlling invertebrate pests and to plant propagation material and [o an agricultural and a veterinary composition comprising said compounds. The invention also relates to novel compounds useful as intermediate compounds in the preparation of compounds I.
    Type: Grant
    Filed: October 8, 2018
    Date of Patent: April 30, 2019
    Assignee: BASF SE
    Inventors: Pascal Bindschaedler, Gopal Krishna Datta, Wolfgang von Deyn, Matthias Pohlman, Franz-Josef Braun
  • Patent number: 10174014
    Abstract: The present disclosure features disclosed compounds which can increase cystic fibrosis transmembrane conductance regulator (CFTR) activity as measured in human bronchial epithelial (hBE) cells. The present disclosure also features methods of treating a condition associated with decreased CFTR activity or a condition associated with a dysfunction of proteostasis comprising administering to a subject an effective amount of a disclosed compound.
    Type: Grant
    Filed: June 19, 2015
    Date of Patent: January 8, 2019
    Assignee: Proteostasis Therapeutics, Inc.
    Inventors: Cecilia M. Bastos, Benito Munoz, Bradley Tait
  • Patent number: 10106510
    Abstract: The present disclosure provides substituted cyclohexylamine compounds having Formula (I): and the pharmaceutically acceptable salts and solvates thereof, wherein R1, R2a, R2b, R3a, R3b, R4, R5, and R7 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 SMYD proteins such as SMYD3 or SMYD2. Compounds of the present disclosure are especially useful for treating cancer.
    Type: Grant
    Filed: September 9, 2015
    Date of Patent: October 23, 2018
    Assignee: EPIZYME, INC.
    Inventors: Megan Alene Cloonan Foley, Kevin Wayne Kuntz, Lorna Helen Mitchell, Michael John Munchhof
  • Patent number: 10029994
    Abstract: This invention pertains generally to compounds of Formula I as described herein and compositions containing such compounds, as well as methods of using such compounds to treat bacterial infections. In certain aspects, the invention provides methods and compositions comprising these compounds for treating infections caused by Gram-negative bacteria.
    Type: Grant
    Filed: October 9, 2017
    Date of Patent: July 24, 2018
    Assignee: Novartis AG
    Inventors: Jiping Fu, Xianming Jin, Subramanian Karur, Guillaume Lapointe, Ann Marie Madera, Zachary Kevin Sweeney
  • Patent number: 10023563
    Abstract: Compounds of formula I defined herein are provided. Uses of these compounds for controlling invertebrate pests, protecting plant propagation material and providing an agricultural and a veterinary composition including the compounds are also described. Compounds for use as intermediate compounds in the preparation of compounds I are also described.
    Type: Grant
    Filed: December 21, 2015
    Date of Patent: July 17, 2018
    Assignee: BASF SE
    Inventors: Pascal Bindschaedler, Gopal Krishna Datta, Wolfgang von Deyn, Franz-Josef Braun
  • Patent number: 10000456
    Abstract: Described herein are compounds that are antagonists of lysophosphatidic receptor(s). Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists, alone and in combination with other compounds, for treating LPA-dependent or LPA-mediated conditions or diseases.
    Type: Grant
    Filed: May 21, 2014
    Date of Patent: June 19, 2018
    Assignee: AMIRA PHARMACEUTICALS, INC.
    Inventors: Ryan Clark, Brian Andrew Stearns, Lucy Zhao, Thomas Jon Seiders, Deborah Volkots, Jeannie M. Arruda
  • Patent number: 9974776
    Abstract: The invention provides a treatment of mesothelioma, especially malignant pleural mesothelioma, using an estrogen receptor ? subtype (ER?) agonist, wherein the treatment comprises administering the ER? agonist to the patient, and then after a time, t, of up to 24 hours; administering a platinum-containing anti-cancer drug to the patient. The invention also provides an ER? agonist and a platinum-containing anti-cancer drug for use in the treatment of mesothelioma in a patient, wherein the treatment comprises administering the ER? agonist to the patient, and then after a time, t, of up to 24 hours, administering the platinum-containing anti-cancer drug to the patient; and a kit comprising a platinum-containing anti-cancer drug and an ER? agonist.
    Type: Grant
    Filed: December 4, 2014
    Date of Patent: May 22, 2018
    Inventors: Stefan Nilsson, Laura Moro, Giulia Pinton, Arcangela Gabriella Manente
  • Patent number: 9968087
    Abstract: The present invention relates to azoline compounds of formula I wherein A, B1, B2, B3, G1, G2, X1, R1, R3a, R3b, Rg1 and Rg2 are as defined in the claims and the description. The compounds are useful for combating or controlling invertebrate pests, in particular arthropod pests and nematodes. 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: Grant
    Filed: February 25, 2015
    Date of Patent: May 15, 2018
    Assignee: BASF SE
    Inventors: Pascal Bindschaedler, Wolfgang Von Deyn
  • Patent number: 9907308
    Abstract: There is provided an aqueous suspension agrochemical composition including (Z)-4-[5-(3,5-dichlorophenyl)-5-trifluoromethyl-4,5-dihydroisoxazol-3-yl]-N-(methoxyiminomethyl)-2-methylbenzamide, a thickener, a surfactant, and water, which is excellent in homogeneity stability during storage, and simultaneously excellent in ease of discharge from a storage container. An aqueous suspension agrochemical composition comprising (a) (Z)-4-[5-(3,5-dichlorophenyl)-5-trifluoromethyl-4,5-dihydroisoxazol-3-yl]-N-(methoxyiminomethyl)-2-methylbenzamide, (b) xanthan gum, (c) a surfactant, and (d) water, wherein the xanthan gum is contained in an amount of 0.15 to 0.65% by mass in the aqueous suspension agrochemical composition. The surfactant is preferably one selected from the group consisting of polyoxyethylene styryl phenyl ethers, polyoxyethylene polyoxypropylene block polymers, and mixtures thereof.
    Type: Grant
    Filed: July 11, 2017
    Date of Patent: March 6, 2018
    Assignee: NISSAN CHEMICAL INDUSTRIES, LTD.
    Inventors: Masahito Hori, Hirokazu Kamatani
  • Patent number: 9895370
    Abstract: Provided is a pharmaceutical composition for preventing or treating liver fibrosis, comprising a GPR119 ligand as an active ingredient. The composition comprising the GPR119 ligand as an active ingredient significantly inhibits the expression of collagen I, transforming growth factor ? (TGF?) and ?-smooth muscle actin (?-SMA), thereby inhibiting HSC activation, and also significantly inhibits HSC proliferation. Therefore, the composition may be effectively applied in improvement, prevention, inhibition or treatment of liver fibrosis.
    Type: Grant
    Filed: November 18, 2016
    Date of Patent: February 20, 2018
    Assignee: PHARMEDIX.CO., LTD
    Inventors: Keon Wook Kang, Kyeong Lee, Jin Won Yang
  • Patent number: 9814235
    Abstract: An amide compound represented by formula (I): [wherein A represents a 3- to 7-membered saturated heterocyclic ring which contains, as ring-forming component(s), one or more atoms or groups selected from the group consisting of an oxygen atom and —S(O)t—, t represents 0, etc., R1 and R2 are the same or different and represent a hydrogen atom, etc., n represents 0, etc., the following formula (II): represents a 5-membered aromatic ring, in which Z represents a nitrogen atom or a carbon atom and X1, X2 and X3 are the same or different and represent a nitrogen atom, etc., R3 and R4 are the same or different and represent a hydrogen atom, etc., m represents 0 to 2, Q represents one group selected from group A or a C1 to C8 chain hydrocarbon group optionally having one group selected from group A, Y represents an oxygen atom, etc., u represents 0, etc., and v represents 0, etc.] has excellent arthropod pest controlling effects.
    Type: Grant
    Filed: January 24, 2014
    Date of Patent: November 14, 2017
    Assignee: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventors: Hiromasa Mitsudera, Kenichiro Awasaguchi, Tomotsugu Awano, Kazuya Ujihara
  • Patent number: 9815804
    Abstract: This invention pertains generally to compounds of Formula I as described herein and compositions containing such compounds, as well as methods of using such compounds to treat bacterial infections. In certain aspects, the invention provides methods and compositions comprising these compounds for treating infections caused by Gram-negative bacteria.
    Type: Grant
    Filed: December 12, 2016
    Date of Patent: November 14, 2017
    Assignee: Novartis AG
    Inventors: Jiping Fu, Xianming Jin, Subramanian Karur, Guillaume Lapointe, Ann Marie Madera, Zachary Kevin Sweeney
  • Patent number: 9783510
    Abstract: In one aspect, the invention relates to N-acetamidoalkyl-5-arylisoxazole-3-carboxamide analogs, derivatives thereof, and related compounds, which are useful as mediators of transcriptional induction of E-cadherin; synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating disorders associated with E-cadherin activity using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Grant
    Filed: August 17, 2015
    Date of Patent: October 10, 2017
    Assignee: Vanderbilt University
    Inventors: Craig W. Lindsley, Alex G. Waterson, R. Daniel Beauchamp
  • Patent number: 9776993
    Abstract: The present invention relates to novel isoxazoline carboxamide derivatives, to processes for preparing these compounds, to compositions comprising these compounds, and to the use thereof as biologically active compounds, especially for control of harmful microorganisms in crop protection and in the protection of materials.
    Type: Grant
    Filed: October 27, 2016
    Date of Patent: October 3, 2017
    Assignee: BAYER CROPSCIENCE AG
    Inventors: Lothar Willms, Monika H. Schmitt, Thomas Frenzel, Klaus Bernhard Haaf, Isolde Haeuser-Hahn, Ines Heinemann, Elmar Gatzweiler, Christopher Hugh Rosinger, Heinz Kehne, Jan Dittgen, Dieter Feucht, Martin Hills, Jan Peter Schmidt, Mazen Es-Sayed, Philipe Rinolfi, Stephane Brunet, Marie-Claire Grosjean-Cournoyer, Helene Lachaise, Jacky Vidal, Pierre-Yves Coqueron, Arounarith Tuch
  • Patent number: 9758485
    Abstract: The invention relates inter alia to compounds of the general formula (I) in which the A1-A4, T, n, W, Q, R1 and B1-B4 radicals are each as defined in the description. Also described are processes for preparing the compounds of the formula (I). The inventive compounds are especially suitable for controlling insects, arachnids and nematodes in agriculture, and ectoparasites in veterinary medicine.
    Type: Grant
    Filed: November 5, 2014
    Date of Patent: September 12, 2017
    Assignee: BAYER CROPSCIENCE AKTIENGESELLSCHAFT
    Inventors: Werner Hallenbach, Hans-Georg Schwarz, Kerstin Ilg, Ulrich Goergens, Johannes Koebberling, Andreas Turgerg, Niels Boehnke, Michael Maue, Robert Velten, Tobias Harschneck, Julia Johanna Hahn, Sebastian Horstmann
  • Patent number: 9745292
    Abstract: The disclosure encompasses compounds having e.g., Formula (Ia) or (Ib), compositions thereof, and methods of modulating CFTR activity. The disclosure also encompasses methods of treating a condition associated with CFTR activity or condition associated with a dysfunction of proteostasis comprising administering to a subject an effective amount of a compound of Formula (I) or (Ib).
    Type: Grant
    Filed: March 13, 2015
    Date of Patent: August 29, 2017
    Assignee: Proteostasis Therapeutics, Inc.
    Inventors: Cecilia M. Bastos, Benito Munoz, Bradley Tait
  • Patent number: 9676704
    Abstract: This disclosure relates to the field of molecules having pesticidal utility against pests in Phyla Nematoda, Arthropoda, and/or Mollusca, processes to produce such molecules and intermediates used in such processes, compositions containing such molecules, and processes of using such molecules against such pests. These molecules may be used, for example, as nematicides, acaricides, insecticides, miticides, and/or molluscicides. This document discloses molecules having the following formula (“Formula One”).
    Type: Grant
    Filed: June 8, 2015
    Date of Patent: June 13, 2017
    Assignee: Dow AgroSciences LLC
    Inventors: Paul Renee LePlae, Jr., James E. Hunter, Gerald B. Watson, William C. Lo, John Herbert
  • Patent number: 9655884
    Abstract: This invention relates to methods for preventing infestations of animals and their environments with adult fleas by systemic administration of isoxazoline compounds.
    Type: Grant
    Filed: December 9, 2014
    Date of Patent: May 23, 2017
    Assignee: Intervet Inc.
    Inventors: Heike Williams, Hartmut Zoller, Anja Regina Heckeroth
  • Patent number: 9624182
    Abstract: Described herein are compounds that are antagonists of lysophosphatidic receptor(s). Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists, alone and in combination with other compounds, for treating LPA-dependent or LPA-mediated conditions or diseases.
    Type: Grant
    Filed: June 30, 2015
    Date of Patent: April 18, 2017
    Assignee: AMIRA PHARMACEUTICALS, INC.
    Inventors: Thomas J. Seiders, Lucy Zhao, Jeannie Arruda, Bowei Wang, Brian Andrew Stearns, Yen Pham Truong, Jill Melissa Scott, John Howard Hutchinson, Ryan Clark, Heather Renee Coate, Nicholas Simon Stock, Deborah Volkots
  • Patent number: 9567306
    Abstract: Compounds and compositions are provided which inhibit MIF. Methods of treatment of melanoma and colon cancers are also provided.
    Type: Grant
    Filed: June 16, 2015
    Date of Patent: February 14, 2017
    Assignee: The Feinstein Institute for Medical Research
    Inventor: Yousef Al-Abed
  • Patent number: 9549916
    Abstract: This invention pertains generally to compounds of Formula I as described herein and compositions containing such compounds, as well as methods of using such compounds to treat bacterial infections. In certain aspects, the invention provides methods and compositions comprising these compounds for treating infections caused by Gram-negative bacteria.
    Type: Grant
    Filed: December 15, 2015
    Date of Patent: January 24, 2017
    Assignee: Novartis AG
    Inventors: Jiping Fu, Xianming Jin, Subramanian Karur, Guillaume Lapointe, Ann Marie Madera, Zachary Kevin Sweeney
  • Patent number: 9498484
    Abstract: The present invention relates to a method for inhibiting fibrosis that occurs in an organ where the farnesoid X receptor (FXR) is expressed. This method involves the step of administering a high potency, activating ligand of FXR in an effective amount to a patient who is not suffering from a cholestatic condition. The invention also provides pharmaceutical compositions containing an effective amount of an FXR ligand and kits for dispensing the pharmaceutical compositions.
    Type: Grant
    Filed: March 14, 2005
    Date of Patent: November 22, 2016
    Assignee: Intercept Pharmaceuticals, Inc.
    Inventors: Stefano Fiorucci, Roberto Pellicciari, Mark Pruzanski
  • Patent number: 9307766
    Abstract: The present invention provides compounds of formula (I) wherein G1 is oxygen; R1 is hydrogen; R2 is group (P) L is a bond, methylene or ethylene; one of A1 and A2 is S, SO or SO2 and the other is —C(R4)R4—; R3 is hydrogen or methyl; each R4 is independently hydrogen or methyl; Y2 and Y3 are independently CH or nitrogen, wherein Y2 and Y3 are not both nitrogen; X2 is C—X6 or nitrogen; X1, X3 and X6 are independently hydrogen, halogen or trihalomethyl, wherein at least two of X1, X3 and X6 are not hydrogen; X4 is trifluoromethyl, difluoromethyl or chlorodifluoromethyl. The invention also provides intermediates useful for the preparation of compounds of formula (I), as well as methods of controlling insects, acarines, nematodes or molluscs using the compounds of formula (I).
    Type: Grant
    Filed: August 24, 2012
    Date of Patent: April 12, 2016
    Assignee: Syngenta Participations AG
    Inventors: Jerome Yves Cassayre, Peter Renold, Thomas Pitterna, Myriem El Qacemi
  • Patent number: 9186411
    Abstract: The present invention provides a pharmaceutical composition or a solid preparation containing a stabilized pharmaceutically active ingredient and a stabilizing method thereof. According to the present invention, a pharmaceutical composition can be stabilized by containing a nonpeptidic pharmaceutically active ingredient having a primary or secondary amino group, an excipient and an acidic compound. In addition, a solid preparation containing a pharmaceutically active ingredient, titanium oxide, a plasticizer and a chain organic acid can enhance the stability of the pharmaceutically active ingredient during light irradiation.
    Type: Grant
    Filed: July 27, 2009
    Date of Patent: November 17, 2015
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Yasuhiro Hiraishi, Muneo Nonomura
  • Patent number: 9139539
    Abstract: The present invention relates to compounds which bind to the NR1H4 receptor (FXR) and act as agonists of FXR. The invention further relates to the use of the compounds for the preparation of a medicament for the treatment of diseases and/or conditions through binding of said nuclear receptor by said compounds and to a process for the synthesis of said compounds.
    Type: Grant
    Filed: July 12, 2012
    Date of Patent: September 22, 2015
    Assignee: Gilead Sciences, Inc.
    Inventors: Olaf Kinzel, Christoph Steeneck, Claus Kremoser
  • Patent number: 9138466
    Abstract: The present invention provides a method for preventing or inhibiting allograft rejection by a recipient of that allograft by treating the recipient with a composition comprising Factor H (FH). The invention also encompasses methods in which the recipient is also administered one or more immunosuppressants in addition to the Factor H.
    Type: Grant
    Filed: March 13, 2014
    Date of Patent: September 22, 2015
    Assignees: Baxalta Incorporated, Baxalta GmbH
    Inventors: Richard Johnson, Zheng Jenny Zhang
  • Patent number: 9062010
    Abstract: A method for manufacturing a crystal and a crystal of (S)-4-[5-(3,5-dichlorophenyl)-5-(trifluoromethyl)-4,5-dihydroisoxazol-3-yl]-2-methyl-N-[2-oxo-2-(2,2,2-trifluoroethylamino)ethyl]benzamide and a method for manufacturing the crystal. It is elucidated that (S)-4-[5-(3,5-dichlorophenyl)-5-(trifluoromethyl)-4,5-dihydroisoxazol-3-yl]-2-methyl-N-[2-oxo-2-(2,2,2-trifluoroethylamino)ethyl]benzamide that has a crystalline polymorph.
    Type: Grant
    Filed: June 27, 2014
    Date of Patent: June 23, 2015
    Assignee: Nissan Chemical Industries, Ltd.
    Inventors: Kazutaka Matoba, Takeshi Mita, Kotatsu Matsubara, Takahiro Kagami, Kunimitsu Nakahira, Masaki Kobayashi, Hotaka Imanaka, Rika Miyachi, Masashi Ohno
  • Publication number: 20150148373
    Abstract: The invention provides heterocyclic guanidine compounds that inhibit F1F0-ATPase, and methods of using heterocyclic guanidine compounds as therapeutic agents to treat medical disorders, such as an immune disorder, inflammatory condition, or cancer.
    Type: Application
    Filed: June 7, 2013
    Publication date: May 28, 2015
    Inventors: Alexander R. Hurd, Clarke B. Taylor, Peter L. Toogood
  • Patent number: 9040563
    Abstract: Many GTPases such as Ras, Ral and Rho require post-translational farnestylation or geranylgeranylation for mediating malignant transformation. Dual farnesyltransferase (FT) (FTI) and geranylgeranyltransferase-I (GGT-1) inhibitors (GGTI) were developed as anticancer agents from based on an ethylenediamine scaffold. On the basis of a 4-fold substituted ethylenediamine scaffold, the inhibitors are structurally simple and readily derivatized, facilitating extensive structure-activity relationship studies. The most potent inhibitor is compound exhibited an in vitro hFTase IC50 value of 25 nM and a whole cell H-Ras processing IC50 value of 90 nM. Several of the inhibitors proved highly selective for hFTase over the related prenyltransferase enzyme geranylgeranyltransferase-I (GGTase-I).
    Type: Grant
    Filed: March 11, 2013
    Date of Patent: May 26, 2015
    Assignees: H. Lee Moffitt Cancer Center and Research Institute, Inc., Yale University
    Inventors: Said M. Sebti, Andrew Hamilton
  • Patent number: 9034820
    Abstract: The invention generally relates to compositions and methods of their use. More specifically, the invention relates to the use of a compound in modulating erythropoiesis in a subject by mediating the activity and/or quantity of a member present in the LPA3-mediated signaling pathway, such as lysophosphatidic acid receptor subtype 3 (LPA3).
    Type: Grant
    Filed: March 13, 2012
    Date of Patent: May 19, 2015
    Inventor: Hsinyu Lee
  • Publication number: 20150133400
    Abstract: Heterocyclic compounds of formula (I), methods for their preparation, pharmaceutical compositions containing such a compound and their therapeutic uses.
    Type: Application
    Filed: September 15, 2014
    Publication date: May 14, 2015
    Inventors: Jiazhong Zhang, John Buell, Katrina Chan, Prabha N. Ibrahim, Jack Lin, Phuongly Pham, Songyuan Shi, Wayne Spevak, Guoxian Wu, Jeffrey Wu
  • Publication number: 20150133495
    Abstract: Disclosed herein is a compound of Formula I or a pharmaceutically acceptable salt thereof, in which A, G, R1 and R2 are as defined herein. The compounds and pharmaceutical compositions of the compounds are suitable for the treatment of HCV infection in mammals and are also useful to modulate or inhibit NS3/4 dimerization.
    Type: Application
    Filed: November 13, 2014
    Publication date: May 14, 2015
    Inventor: Daniel Lamarre
  • Publication number: 20150133515
    Abstract: This invention relates generally to integrin ligand discovery and to a method of integrin ligand discovery based upon induction of ligand-induced epitopes. Such ligands have the potential to be active agent as anti-inflammatory, anti-angiogenesis and/or anti-thrombotic agents and for the treatment of integrin mediated diseases and/or conditions.
    Type: Application
    Filed: November 6, 2014
    Publication date: May 14, 2015
    Inventors: ALEXANDRE CHIGAEV, LARRY A. SKLAR
  • Patent number: 9029377
    Abstract: Cyclohexyl sulfonamide compounds which are platelet-activating factor (PAF) receptor antagonists. Said compounds may be useful, for example, for the treatment of atherosclerosis or other PAF-mediated disorders, including inflammatory, cardiovascular, and immune disorders.
    Type: Grant
    Filed: June 28, 2010
    Date of Patent: May 12, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Anthony Ogawa, Feroze Ujjainwalla, Lin Chu, Bing Li, Lan Wei, Jinyou Xu, Hyun Ok, Aaron Lackner, Ihor Kopka
  • Patent number: 9029409
    Abstract: The present invention provides compound of Formula (I) biologically active metabolites, pro-drugs, isomers, stereoisomers, solvates, hydrates and pharmaceutically acceptable salts thereof wherein the variables are defined herein. The compounds of the invention are useful for treating immunological conditions.
    Type: Grant
    Filed: April 30, 2012
    Date of Patent: May 12, 2015
    Assignee: AbbVie Inc.
    Inventors: David J. Calderwood, Eric C. Breinlinger, Steven L. Swann, Venkata Srikanth Chitty, Subramanya Seetharama Shastry Hosahalli, Subhendu Mukherjee, Siva Sanjeeva Rao Thunuguntla
  • Publication number: 20150126371
    Abstract: The present invention relates to a pyrazolopyran of the general formula I wherein the variables are defined according to the description, including a tautomer, salt, cleavable prodrug, or mixtures thereof, in particular to said pyrazolopyran for use as a medicament and/or an inhibitor of the enzyme serinehydroxymethyltransferase (SHMT). The invention also relates to a process the preparation of a pyrazolopyran of the formula I, to compositions comprising said compound and processes for the preparation of these compositions. Further it relates to use of the pyrazolopyran of formula I as an herbicide as well as to a method of controlling undesired vegetation.
    Type: Application
    Filed: May 29, 2013
    Publication date: May 7, 2015
    Inventors: Matthias Witschel, Frank Stelzer, Johannes Hutzler, Tao Qu, Thomas Mietzner, Klaus Kreuz, Klaus Grossmann, Raphael Aponte, Hans Wolfgang Hoeffken, Frederick Calo, Thomas Ehrhardt, Anja Simon, Liliana Parra Rapado
  • Publication number: 20150126523
    Abstract: The present invention relates to novel and inventive isoxazoline of formula (I) and salts thereof: wherein variables D1, D2, D3, D4, D5, R1, B1, B2, B3, R2, R3, R4, R5, R6, Y, Z, L, a and b are described herein are as defined in the description. The invention also relates to parasiticidal and pesticidal compositions comprising the isoxazoline compounds of formula (I), processes for their preparation and their uses to prevent or treat parasitic infections or infestations in animals and as pesticides.
    Type: Application
    Filed: October 30, 2014
    Publication date: May 7, 2015
    Applicant: MERIAL LIMITED
    Inventor: Charles Q. Meng
  • Patent number: 9023836
    Abstract: The present invention relates to the use of compounds of formula wherein the variables are as defined in the description, in the free form or in salt form, for controlling sea lice on fish.
    Type: Grant
    Filed: June 15, 2011
    Date of Patent: May 5, 2015
    Assignee: Novartis Tiergesundheit AG
    Inventors: Jean-Luc Perret, David Blaser, Steve Nanchen
  • 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: 20150119433
    Abstract: The invention relates to the topical treatment of actinic keratosis on the full balding scalp with ingenol 3-(3,5-diethylisoxazole-4-carboxylate).
    Type: Application
    Filed: October 27, 2014
    Publication date: April 30, 2015
    Inventors: Johan Selmer, Kim Mark Knudsen
  • Publication number: 20150119375
    Abstract: The present invention relates to novel 1-methyl-pyrazole(thio)indanyl carboxamides, to processes for preparing these compounds, to compositions comprising these compounds, and to the use thereof as biologically active compounds, especially for control of harmful microorganisms in crop protection and in the protection of materials.
    Type: Application
    Filed: May 6, 2013
    Publication date: April 30, 2015
    Applicant: Bayer Cropscience AG
    Inventors: Pierre-Yves Coqueron, Mazen Es-Sayed, Simon Maechling, Pierre Wasnaire, Peter Dahmen, Ulrike Wachendorff-Neumann, David Bernier, Lionel Carles, Christophe Dubost, Stephane Brunet, Helene Lachaise, Jean-Pierre Vors
  • Publication number: 20150119434
    Abstract: The invention relates to the topical treatment of actinic keratosis with ingenol 3-(3,5-diethylisoxazole-4-carboxylate).
    Type: Application
    Filed: October 27, 2014
    Publication date: April 30, 2015
    Inventors: Johan Selmer, Kim Mark Knudsen
  • Publication number: 20150119432
    Abstract: The present invention relates to a composition comprising an isoxazoline compound, the isoxazoline compound being dispersed in a solid vehicle of one or more polymer compounds selected from cellulose polymers and vinyl polymers.
    Type: Application
    Filed: October 21, 2014
    Publication date: April 30, 2015
    Inventors: Naonobu NISHIGUCHI, Kaori IKARI
  • Patent number: 9018238
    Abstract: There is provided an inhibitor that inhibits casein kinase 1? and casein kinase 1?, and thus, there is also provided a pharmaceutical agent useful for the treatment and/or prevention of a disease, with the pathological condition of which the mechanism of activation of casein kinase 1? or casein kinase 1? is associated. Particularly, the above-described inhibitor is used to provide a pharmaceutical agent useful for the treatment of circadian rhythm disorder (including sleep disorder), central neurodegenerative disease, and cancer.
    Type: Grant
    Filed: December 28, 2009
    Date of Patent: April 28, 2015
    Assignees: Pharmadesign, Inc., NB Health Laboratory Co., Ltd.
    Inventors: Masako Okamoto, Kiyoshi Takayama
  • Publication number: 20150110809
    Abstract: Embodiments of the invention are directed to compounds that inhibit an activity of EP AC proteins and methods of using the same. The inventors have developed a sensitive and robust high throughput screening (HTS) assay for the purpose of identifying EPAC specific inhibitors (Tsalkova et al. (2012) PLOS ONE 7 (1):e30441).
    Type: Application
    Filed: February 8, 2013
    Publication date: April 23, 2015
    Applicant: The Board of Regents of the University of Texas System
    Inventors: Xiaodong Cheng, Jia Zhou, Tamara Tsalkova, Fang Mei, Haijun Chen
  • Publication number: 20150111936
    Abstract: This invention relates to methods for controlling parasitic infestations of animals and their environments, and, more particularly, to methods using isoxazolines to control parasites in or on animals or in their environments, as well as treat parasitoses of animals. The isoxazolines include 4-(isoxazolinyl)-benzamides (specifically, substituted 4-(5-(halomethyl)-5-phenyl-isoxazolin-3-yl)-benzamides) and 4-(isoxazolinyl)-benzothioamides (specifically, substituted 4-(5-(halomethyl)-5-phenyl-isoxazolin-3-yl)-benzothioamides). This invention also relates to compositions comprising the isoxazolines for use in such methods, the use of the isoxazolines to make medicaments for use in such methods, and kits comprising the isoxazolines for carrying out such methods. This invention further relates to the use of the isoxazolines as medicaments, particularly medicaments that can be used in the above-referenced methods.
    Type: Application
    Filed: December 22, 2014
    Publication date: April 23, 2015
    Inventors: Anja Regina Heckeroth, Jürgen Lutz, Christina Mertens, Heike Williams, Hartmut Zoller, Takeshi Mita