1,3-thiazoles (including Hydrogenated) Patents (Class 514/365)
  • Patent number: 8829033
    Abstract: A first aspect of the invention is a compound (sometimes also referred to herein as an “active agent” or “active compound”) of Formula Ia, or more particularly Formula Ib, or a pharmaceutically acceptable salt or prodrug thereof. Compositions thereof and methods of using the same (e.g. for the treatment of a neurological disease) are also described.
    Type: Grant
    Filed: September 17, 2010
    Date of Patent: September 9, 2014
    Assignee: The University of North Carolina at Chapel Hill
    Inventors: Harold L. Kohn, Christophe Salomé, Elise Salomé-Grosjean
  • Publication number: 20140249100
    Abstract: Disclosed are methods for preventing metastasis of cancer cells. The disclosed compounds can be used to prevent the spread of tumor or other types of cancer cells.
    Type: Application
    Filed: March 3, 2013
    Publication date: September 4, 2014
    Applicant: Aerpio Therapeutics Inc.
    Inventors: Robert Shalwitz Shalwitz, Kevin Gene Peters
  • Publication number: 20140249155
    Abstract: Novel 3?-deoxy-3?-acylaminospectinomycin compounds are described. Also described are methods of using the 3?-deoxy-3-acylaminospectinomycin compounds and other spectinomycin analogs in treating tuberculosis and in treating microbial infections.
    Type: Application
    Filed: March 23, 2014
    Publication date: September 4, 2014
    Applicant: UNIVERSITY OF TENNESSEE RESEARCH FOUNDATION
    Inventors: Richard E. Lee, Jianjun Qi, Julian G. Hurdle, Bernd Meibohm, VNR Pavan Kumar Vaddady, Rakesh, Jiuyu Liu
  • Publication number: 20140249203
    Abstract: Described herein are carrier nanoparticles comprising a polymer containing a polyol coupled to a polymer containing a boronic acid, configured to present the polymer containing a boronic acid to an environment external to the nanoparticle. Targeted versions of the described nanoparticles are also described, as are related compositions, methods and systems.
    Type: Application
    Filed: March 1, 2013
    Publication date: September 4, 2014
    Inventors: Mark E. Davis, Han Han
  • Patent number: 8822466
    Abstract: The invention relates to new isoxazoline compounds of formula wherein the variables have the meaning as indicated in the claims; in free form and in salt form; and optionally the enantiomers and geometrical isomers thereof. The compounds of formula (I) are useful in the control of parasites, in particular ectoparasites, in and on vertebrates.
    Type: Grant
    Filed: March 9, 2012
    Date of Patent: September 2, 2014
    Assignee: Novartis AG
    Inventors: Noëlle Gauvry, Steve Nanchen
  • Patent number: 8822512
    Abstract: The disclosure features crystalline tripeptide keto epoxide compounds, methods of their preparation, and related pharmaceutical compositions.
    Type: Grant
    Filed: September 20, 2011
    Date of Patent: September 2, 2014
    Assignee: Onyx Therapeutics, Inc.
    Inventors: Pasit Phiasivongsa, Louis C. Sehl
  • Publication number: 20140242135
    Abstract: In one aspect, the invention relates to chemical modulators of insect olfactory receptors. In particular, compounds and compositions are provided that can inhibit sensory (e.g., host targeting) functions in airborne insects such as mosquitos. Method of employing such agents, and articles incorporating the same, are also provided. 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: Application
    Filed: April 25, 2012
    Publication date: August 28, 2014
    Applicant: Vanderbilt University
    Inventors: Laurence Zwiebel, Gregory M. Pask, David C. Rinker, Ian M. Romaine, Gary A. Sulikowski, Paul R. Reid, Alex G. Waterson, Kwangho Kim, Patrick L. Jones, Robert W. Taylor
  • Publication number: 20140243340
    Abstract: The present invention features compounds of formula I or pharmaceutically acceptable salts, solvates or prodrugs thereof, and methods of using the same to inhibit the metabolizing activities of CYP enzymes. The present invention also features methods of using these compounds, salts, solvates or prodrugs to improve the pharmacokinetics of drugs that are metabolized by CYP enzymes.
    Type: Application
    Filed: May 8, 2014
    Publication date: August 28, 2014
    Applicant: AbbVie Inc.
    Inventors: Larry L. Klein, Hui-Ju CHEN, Ming C. YEUNG, Charles A. Flentge, John T. Randolph, Peggy Huang, Douglas K. Hutchinson, Dale J. Kempf
  • Publication number: 20140243296
    Abstract: A treatment regimen and dosage form comprising ritonavir and darunavir and their use in the treatment of HIV infection.
    Type: Application
    Filed: October 5, 2012
    Publication date: August 28, 2014
    Applicant: JAGOTEC AG
    Inventors: Pascal Grenier, Guy Vergnault, Patricia Ibarra
  • Publication number: 20140243326
    Abstract: The invention relates to insecticide mixtures comprising thiodicarb and at least one other known active ingredient from the category of chloronicotinyls, as well as the use of these mixtures to control animal pests.
    Type: Application
    Filed: May 9, 2014
    Publication date: August 28, 2014
    Applicant: Bayer CropScience Ag
    Inventors: Wolfram Andersch, Heike Hungenberg, Wolfgang Thielert
  • Publication number: 20140242026
    Abstract: Disclosed are methods for preventing metastasis of cancer cells. The disclosed compounds can be used to prevent the spread of tumor or other types of cancer cells.
    Type: Application
    Filed: May 8, 2014
    Publication date: August 28, 2014
    Inventors: Robert Shalwitz, Kevin Gene Peters
  • Publication number: 20140242120
    Abstract: The invention relates to compounds of structural formula (I): or a pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof, wherein Y, L, A, W1, W2, and R?1 are defined herein. These compounds are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.
    Type: Application
    Filed: May 8, 2014
    Publication date: August 28, 2014
    Applicant: Synta Pharmaceuticals Corp.
    Inventors: Shoujun Chen, Lijun Sun, Yu Xie
  • Publication number: 20140243338
    Abstract: The present invention provides compounds of Formula (I): or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective ROCK inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating cardiovascular, smooth muscle, oncologic, neuropathologic, autoimmune, fibrotic, and/or inflammatory disorders using the same.
    Type: Application
    Filed: February 28, 2014
    Publication date: August 28, 2014
    Inventors: Mimi L. Quan, Zilun Hu, Cailan Wang
  • Patent number: 8815903
    Abstract: The present invention provides a compound represented by the general formula (I) of the present invention, which has EP1 receptor antagonism: wherein A represents a benzene ring, a pyridine ring, or the like; Y1 represents a C1-6 alkylene group or the like; Y2 represents a single bond or the like; Z represents —C(?O)—NHSO2R6, an acidic 5-membered hetero ring group, or the like; R1 represents a hydrogen atom or the like; R2 represents a phenyl group, a 5-membered aromatic heterocyclic group, or the like; R3 represents a halogen atom, a C1-6 alkoxy group, or the like; R4 represents a hydrogen atom, a halogen atom, or the like; R5 represents a hydrogen atom or the like; and R6 represents a C1-6 alkyl group or the like], or a pharmaceutically acceptable salt thereof. Furthermore, the compound (I) of the present invention can be used as an agent for treating or preventing LUTS, in particular, various symptoms of OABs.
    Type: Grant
    Filed: January 24, 2012
    Date of Patent: August 26, 2014
    Assignees: Kissei Pharmaceutical Co., Ltd., Kyorin Pharmaceutical Co., Ltd.
    Inventors: Kazuya Tatani, Atsushi Kondo, Tatsuhiro Kondo, Naohiro Kawamura, Shigeki Seto, Yasushi Kohno
  • Patent number: 8815920
    Abstract: A substituted amide compound is useful as an active ingredient of a pharmaceutical composition, in particular a pharmaceutical composition for treating diseases caused by lysophosphatidic acid (LPA). The compound is of a formula: In this formula, A is an optionally substituted aryl, etc.; B is an optionally substituted 5-membered aromatic hetero ring group; X is a single bond or —(CRX1RX2)n—; n is 1, 2, 3, or 4; RX1 and RX2 are hydrogen, etc.; Y1 to Y5 are each CRY or N; each RY is hydrogen, etc.; R1 and R2 are hydrogen, etc.; m is 1, 2, or 3; R3 is hydrogen, etc.; and R4 is an optically substituted lower alkyl, etc.
    Type: Grant
    Filed: March 4, 2013
    Date of Patent: August 26, 2014
    Assignee: Astellas Pharma Inc.
    Inventors: Eiji Kawaminami, Tatsuhisa Takahashi, Takatoshi Kanayama, Yuta Fukuda, Hiroyuki Kaizawa, Yutaka Kondoh, Ryushi Seo, Kazuyuki Kuramoto, Kazuhiko Take, Kazuyuki Sakamoto
  • Patent number: 8815844
    Abstract: The present invention relates to the compounds useful in the prevention and/or treatment of tumors. More specifically the present invention relates to inhibitors of the activity of the electron transport chains and/or the mitochondrial TCA cycle in glioma-initiating cells (GICs) for use in a method for preventing and/or treating tumors presenting glioma-initiating cells (GICs) in a subject who has undergone a prior removal of a tumor glioma bulk. The present invention further provides a pharmaceutical composition containing the inhibitors of the invention and a screening method for identifying the inhibitors of the invention.
    Type: Grant
    Filed: May 20, 2010
    Date of Patent: August 26, 2014
    Assignees: Universite de Geneve, Hopitaux Universitaires de Geneve
    Inventors: Virginie Clement, Ivan Radovanovic
  • Publication number: 20140235622
    Abstract: The present invention pertains to certain compounds of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the 5-HT2A serotonin receptor. Compounds and pharmaceutical compositions thereof are directed to methods useful in the treatment of platelet aggreagation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, blood clot formation, asthma or symptoms thereof, agitation or a symptom thereof, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de la Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorder, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, and sleep disorders, sleep disorders, diabetic-related disorders, progressive multifocal leukoencephalopathy and the like.
    Type: Application
    Filed: January 28, 2014
    Publication date: August 21, 2014
    Applicant: Arena Pharmaceuticals, Inc.
    Inventors: Bradley Teegarden, Dennis Chapman, Juyi Choi, Konrad Feichtinger, Sangdon Han, Honnappa Jayakumar, Thuy-Anh Tran, Jay Xu, Ning Zou
  • Publication number: 20140235680
    Abstract: Compounds represented by structural formulas described herein, such as Structural Formula (I): or a pharmaceutically acceptable salt thereof are useful in treating conditions such as metal overload, oxidative stress, and neoplastic and preneoplastic conditions.
    Type: Application
    Filed: April 29, 2014
    Publication date: August 21, 2014
    Applicant: UNIVERSITY OF FLORIDA RESEARCH FOUNDATION, INC.
    Inventor: Raymond J. Bergeron, JR.
  • Publication number: 20140235646
    Abstract: The present invention relates to methods for reducing body weight in an animal in need thereof via administration of a therapeutically effective amount of a compound having a general tripartite structure A-B-C. In the tripartite structure A, B, and C are identical or non-identical structures, for example, but not limited to, heterocyclic, phenyl or benzyl ring structures with or without substitutions and are described in detail herein. The methods may utilize particular compounds, for example, having a piperidinyl, a pyrrolinyl or pyridinyl A ring, a thiazole B ring, and a phenyl C ring which may be further substituted independently. Also provided are methods for increasing thermogenesis without reducing lean body mass during weight loss in an animal by administering of a therapeutically effective amount of the compounds described.
    Type: Application
    Filed: May 5, 2014
    Publication date: August 21, 2014
    Inventors: Motonari Uesugi, Salih J. Wakil, Lutfi Al-Elheiga, Mizuki Watanabe
  • Patent number: 8808720
    Abstract: A product comprising microcapsules which themselves comprise (a) a polymeric shell; and (b) a core which comprises (i) a solid agrochemical dispersed in a matrix and (ii) a water-immiscible liquid characterized in that the matrix is distributed non-continuously throughout the water-immiscible liquid.
    Type: Grant
    Filed: December 22, 2006
    Date of Patent: August 19, 2014
    Assignee: Syngenta Limited
    Inventors: Patrick Joseph Mulqueen, Anne Waller, Julia Lynne Ramsay, Geoffrey William Smith
  • Patent number: 8809315
    Abstract: Use of a monobactam antibiotic of formula (I) wherein the oxyimino group i.e. >C?N—O— has Z-orientation, or a pharmaceutically acceptable salt thereof for the manufacture of a medicament for the treatment of a bacterial infection in combination with a carbapenem antibiotic or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: June 12, 2013
    Date of Patent: August 19, 2014
    Assignee: Basilea Pharmaceutica AG
    Inventors: Eric Desarbre, Malcolm G. P. Page
  • Publication number: 20140228416
    Abstract: This invention provides compounds of formula (I): wherein X1, X2, X3, R2, R4b, R1, and G have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.
    Type: Application
    Filed: September 12, 2013
    Publication date: August 14, 2014
    Applicant: Millennium Pharmaceuticals, Inc.
    Inventors: Christopher Blackburn, Kenneth M. Gigstad, He Xu
  • Publication number: 20140228417
    Abstract: The present invention relates to processes and intermediates for the preparation of derivatives of 2-arylthiazole such as Febuxostat and its analogs. Febuxostat which is an inhibitor of xanthine oxidase, is used for the treatment of chronic hyperuricaemia in conditions in which urate deposition has occurred, such as gouty arthritis.
    Type: Application
    Filed: January 23, 2012
    Publication date: August 14, 2014
    Applicant: MAPI PHARMA LTD.
    Inventors: Michael Mizhiritskii, Ehud Marom, Shai Rubnov
  • Patent number: 8802705
    Abstract: Provision of an agent for promoting proliferation of meibomian gland epithelial cells or corneal epithelial cells, and a therapeutic agent for ocular diseases such as meibomian gland dysfunction, dry eye and the like. A preparation containing [3-[2-[4-isopropyl-2-(4-trifluoromethyl)phenyl-5-thiazolyl]ethyl]-5-methyl-1,2-benzisoxazol-6-yl]oxyacetic acid, [4-[3-[2-(4-trifluoromethyl)phenyl-4-isopropyl-5-thiazolyl]propionyl]-2-methylphenoxy]acetic acid or [4-[3-[2-(2-hydroxy-4-chlorophenyl)-5-isopropyl-4-oxazolyl]propionyl]-2-methylphenoxy]acetic acid, or a pharmacologically acceptable salt thereof as an active ingredient is used as an agent for promoting proliferation of meibomian gland epithelial cells or corneal epithelial cells, as well as a therapeutic agent for ocular diseases such as meibomian gland dysfunction, dry eye and the like.
    Type: Grant
    Filed: May 20, 2008
    Date of Patent: August 12, 2014
    Assignees: Senju Pharmaceutical Co., Ltd., Nippon Chemiphar Co., Ltd.
    Inventors: Yoshikuni Nakamura, Ikuko Hanano, Jun Inoue
  • Publication number: 20140221363
    Abstract: The present invention provides a composition for controlling harmful arthropods having an excellent control efficacy on harmful arthropods. A composition for controlling harmful arthropods comprising an amide compound represented by a formula (I); wherein each of symbols are the same as defined in the Description; or salts thereof, and at least one kind of neonicotinoid compounds selected from the group (A) consisting of imidacloprid, clothianidin, thiamethoxiam, dinotefuran, acetamiprid, thiacloprid and nitenpyram, shows an excellent controlling efficacy on harmful arthropods.
    Type: Application
    Filed: July 20, 2012
    Publication date: August 7, 2014
    Applicant: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventors: Atsushi Iwata, Chie Shimizu, Miki Suzuki
  • Publication number: 20140221383
    Abstract: Compounds having the structures of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis: In the compounds of Formula I, B or R2 is a phenyl group which has an ortho aryl, heterocyclic, benzoheterocyclic or benzocycloalkyl substituent, and one other position on the 5-membered ring has an aromatic, heterocyclic, cycloalkyl, benzoheterocyclic or benzocycloalkyl substituent connected directly to the ring or attached to the ring through a —CH2—.
    Type: Application
    Filed: April 14, 2014
    Publication date: August 7, 2014
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Amjad Ali, Joann M. Napolitano, Qiaolin Deng, Zhijian Lu, Peter J. Sinclair, Gayle E. Hallet, Christopher F. Thompson, Nazia Quraishi, Cameron J. Smith, Julianne A. Hunt, Adrian A. Dowst, Yi-Heng Chen, Hong Li
  • Publication number: 20140220141
    Abstract: The present inventions relates to a solid composition and an aqueous dispersion comprising nanoparticles of the anti-retroviral drugs lopinavir and ritonavir. The solid composition and aqueous dispersion additionally comprise a mixture of a hydrophilic polymer and a surfactant. The surfactant is selected from vitamin-E-polyethylene glycol-succinate (Vit-E-PEG-succinate), a polyoxyethylene sorbitan fatty acid ester, N-alkyldimethylbenzylammonium chloride, sodium deoxycholate, dioctyl sodium sulfosuccinate, polyethyleneglycol-12-hydroxystearate, polyvinyl alcohol (PVA), and a block copolymer of polyoxyethylene and polyoxypropylene, or a combination thereof. The hydrophilic polymer is suitably selected from polyvinyl alcohol (PVA), a polyvinyl alcohol-polyethylene glycol graft copolymer, a block copolymer of polyoxyethylene and polyoxypropylene, polyethylene glycol, hydroxypropyl methyl cellulose (HPMC), and polyvinylpyrrolidone, or a combination thereof.
    Type: Application
    Filed: September 7, 2012
    Publication date: August 7, 2014
    Applicant: THE UNIVERSITY OF LIVERPOOL
    Inventors: Marco Norman Giardiello, Thomas Oliver McDonald, Andrew Owen, Steven Paul Rannard, Philip John Martin, Darren Lee Smith
  • Publication number: 20140221421
    Abstract: Compounds of formula I: or salts thereof are disclosed. Also disclosed are pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I and therapeutic methods for treating a Retroviridae viral infection including an infection caused by the HIV virus.
    Type: Application
    Filed: January 9, 2014
    Publication date: August 7, 2014
    Applicant: GILEAD SCIENCES, INC.
    Inventors: Steven S. BONDY, Carina E. CANNIZZARO, Chien-Hung CHOU, John O. LINK, Qi LIU, Scott D. SCHROEDER, Winston C. TSE, Jennifer R. ZHANG
  • Publication number: 20140221384
    Abstract: The present invention relates to nordihydroguaiaretic acid derivative compounds, namely, butane bridge modified nordihydroguaiaretic acid (NDGA) compounds and butane bridge modified tetra-O-substituted NDGA compounds, pharmaceutical compositions containing them, methods of making them, and methods of using them and kits including them for the treatment of diseases and disorders, in particular, diseases resulting from or associated with a virus infection, such as HIV infection, HPV infection, or HSV infection, an inflammatory disease, such as various types of arthritis and inflammatory bowel diseases, metabolic diseases, such as diabetes and hypertension, or a proliferative disease, such as diverse types of cancers.
    Type: Application
    Filed: April 7, 2014
    Publication date: August 7, 2014
    Applicant: ERIMOS PHARMACEUTICALS LLC
    Inventors: Jonathan Daniel Heller, Qingqi Chen, Rocio Alejandra Lopez, Amanda Jean Morris
  • Publication number: 20140221432
    Abstract: The present invention provides a composition for controlling harmful arthropods having an excellent control efficacy on harmful arthropods. A composition for controlling harmful arthropods comprising an amide compound represented by a formula (I); wherein each of symbols are the same as defined in the Description; or salts thereof and at least one kind of neonicotinoid compounds selected from the group (A) consisting of imidacloprid, clothianidin, thiamethoxiam, dinotefuran, acetamiprid, thiacloprid and nitenpyram, shows an excellent controlling efficacy on harmful arthropods.
    Type: Application
    Filed: July 20, 2012
    Publication date: August 7, 2014
    Inventors: Atsushi Iwata, Chie Shimizu, Miki Suzuki
  • Patent number: 8795701
    Abstract: The invention relates to a method for improving the utilization of the production potential of transgenic plants which comprises treating the plant with active compound combinations comprising an active compound from the group of the anthranilamides and at least one further insecticide.
    Type: Grant
    Filed: April 8, 2008
    Date of Patent: August 5, 2014
    Assignee: Bayer CropScience AG
    Inventors: Wolfram Andersch, Christian Funke, Heike Hungenberg, Wolfgang Thielert
  • Patent number: 8795729
    Abstract: The present invention provides methods for feeding older sows that beneficially reduce feed intake in older sows, yet improve pig survival and weaning weight of pigs from older sows.
    Type: Grant
    Filed: December 30, 2013
    Date of Patent: August 5, 2014
    Assignee: APC, Inc.
    Inventors: Joe David Crenshaw, Joy Campbell, Louis E. Russell
  • Patent number: 8796176
    Abstract: PROBLEM Provided is a composition for controlling pests having excellent control effect for pests and a method for controlling pests. SOLUTION A composition for controlling pests comprising an ?-alkoxyphenylacetic acid compound and a neonicotinoid compound as active ingredients.
    Type: Grant
    Filed: September 17, 2009
    Date of Patent: August 5, 2014
    Assignee: Sumitomo Chemical Company, Ltd
    Inventors: Masanao Takaishi, Atsushi Iwata
  • Publication number: 20140213618
    Abstract: The present invention provides compounds of formula (I): as described generally and in classes and subclasses herein. The present invention additionally provides pharmaceutical compositions comprising compounds of formula (I) and provides methods of treating cancer comprising administering a compound of formula (I).
    Type: Application
    Filed: August 20, 2013
    Publication date: July 31, 2014
    Inventors: Samuel J. Danishefsky, Alexey Rivkin, Yoshimura Fumihiko, Ting-Chao Chou, Ana E. Gabarda, Huajin Dong
  • Publication number: 20140213588
    Abstract: The present invention provides compounds of Formula (I): as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicaments. The disclosure also provides a novel method of treating diseases or conditions related to the activity of endothelial lipase by use of compounds according to Formula (II): as defined in the specification and compositions comprising any of the compounds.
    Type: Application
    Filed: September 26, 2012
    Publication date: July 31, 2014
    Applicant: Bristol-Myers Squibb Company
    Inventors: Lynn Abell, Leonard Adam, Cullen L. Cavallaro, Heather Finlay, Todd J. Friends, Jon J. Hangeland, Ji Jiang, R. Michael Lawrence, Jennifer X. Qiao, Carol Hui Hu, Tammy C. Wang
  • Patent number: 8791114
    Abstract: Novel dihydropyrazole derivatives of formula (I) wherein L, R, R3, R4, R5, R6, R7, X1, X2, X3, X4, Y, m and n have the meaning according to the claims, are positive allosteric modulators of the FSH receptor, and can be employed, inter alia, for the treatment of fertility disorders.
    Type: Grant
    Filed: June 26, 2012
    Date of Patent: July 29, 2014
    Assignee: Merck Patent GmbH
    Inventors: Henry Yu, Thomas E. Richardson, Robert James Foglesong, Lizbeth Celeste DeSelm, Andreas Goutopoulos
  • Patent number: 8790676
    Abstract: A microcapsule can be produced readily by (a) pulverizing a solid pesticidal compound in terpineol, dihydroterpineol, terpinel acetate, dihydroterpinel acetate or a mixture thereof to form a suspension, (b) mixing the resulting suspension and water to prepare a liquid droplet, and (c) forming a coating film of a resin around the liquid droplet. The microcapsule obtained by such a method contains most of the solid pesticidal compound within the microcapsule.
    Type: Grant
    Filed: November 21, 2006
    Date of Patent: July 29, 2014
    Assignee: Sumitomo Chemical Company, Limited
    Inventor: Toshiyuki Tanedani
  • Publication number: 20140206651
    Abstract: The invention relates to a compound of formula (I): or a pharmaceutically acceptable salt thereof, thereof, wherein: G is a group of formula (II): and pharmaceutically acceptable salts, prodrugs, hydrates, or solvates, thereof, wherein A, B, L1-L4, A, B, R1-R4, and m are as defined herein. The invention also relates to pharmaceutical compositions comprising the compounds of formula (I) and their use in treating a bacterial infection.
    Type: Application
    Filed: March 24, 2014
    Publication date: July 24, 2014
    Applicant: Pfizer Inc.
    Inventors: Matthew Frank Brown, Charles Francis Donovan, Edmund Lee Ellsworth, Denton Wade Hoyer, Timothy Allan Johnson, Manjinder Singh Lall, Chris Limberakis, Sean Timothy Murphy, Debra Ann Sherry, Clarke Bentley Taylor, Joseph Scott Warmus
  • Publication number: 20140206706
    Abstract: The present invention provides a method for treating a thrombotic or an inflammatory disorder administering to a patient in need thereof a therapeutically effective amount of at least one compound of Formula (I) or Formula (V): or a stereoisomer or pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, L, Z, R3, R4, R6, R11, X1, X2, and X3 are as defined herein. The compounds of Formula (I) are useful as selective inhibitors of serine protease enzymes of the coagulation cascade and/or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and/or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors. This invention also provides compounds within the scope of Formula I and relates to pharmaceutical compositions comprising these compounds.
    Type: Application
    Filed: March 19, 2014
    Publication date: July 24, 2014
    Inventors: Jon J. Hangeland, Mimi L. Quan, Joanne M. Smallheer, Gregory S. Bisacchi, James R. Corte, Todd J. Friends, Zhong Sun, Karen A. Rossi, Cullen L. Cavallaro
  • Publication number: 20140205567
    Abstract: The present invention discloses a class of novel macro-heterocyclic compounds represented by the formula Ia or Ib, and their intermediates, preparation methods and the uses. The macro-heterocyclic compounds of the present invention have good inhibitory activities against hepatitis C virus (HCV), and can be used to treat HCV infection effectively by its excellent inhibition against HCV, low toxicity and side effects.
    Type: Application
    Filed: June 14, 2012
    Publication date: July 24, 2014
    Applicant: AB Pharma Ltd.
    Inventor: Zheng-yun James Zhan
  • Patent number: 8785442
    Abstract: The present invention relates to a compound as antagonist of LPA receptor, and a pharmaceutical composition comprising the same. The present invention also relates to the use of the compound and the composition, and a method of using the compound to treat, prevent or diagnose diseases, disorders or conditions associated with one or more of the LPA receptors.
    Type: Grant
    Filed: January 30, 2011
    Date of Patent: July 22, 2014
    Assignee: Curegenix, Inc.
    Inventors: Songzhu An, Chufang Li, Guisheng Zhou, Chen Huang
  • Patent number: 8785478
    Abstract: The present invention relates to viral polymerase inhibitors of formula (I) or salts, N-oxides, solvates, hydrates, racemates, enantiomers or isomers thereof, processes for their preparation and their use in the treatment of Flaviviridae viral infections such as Hepatitis C virus (HCV) infections.
    Type: Grant
    Filed: April 11, 2013
    Date of Patent: July 22, 2014
    Assignee: Biota Scientific Management Pty Ltd.
    Inventors: Silas Bond, Rosliana Halim, Tyrone Pieter Jeynes, Alistair George Draffan, Michael Harding
  • Patent number: 8785468
    Abstract: Provided herein are compounds of formula I: wherein A, B, X, R1, R2 and subscript n are as defined in the following disclosure. Compositions comprising the compounds are also provided, as well as methods for their use, for example, in treatment of type 2 diabetes and type 2 diabetes-related conditions.
    Type: Grant
    Filed: February 12, 2010
    Date of Patent: July 22, 2014
    Assignee: Amgen Inc.
    Inventors: Xiaohui Du, Zice Fu, Jonathan B. Houze, XianYun Jiao, Yong-Jae Kim, Leping Li, Jinqian Liu, Mike Elias Lizarzaburu, Julio C. Medina, Wang Shen, Simon Turcotte, Ming Yu
  • Patent number: 8785489
    Abstract: Disclosed are compounds and compositions of the formula I as described herein which are inhibitors of MMP-13. Also disclosed are methods of using and making compounds of the formula I.
    Type: Grant
    Filed: October 13, 2009
    Date of Patent: July 22, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Asitha Abeywardane, Bennett Farmer, Neil Alexander Farrow, Donghong Amy Gao, Alexander Heim-Riether, Lana Louise Smith Keenan, Ingo Andreas Mugge, Steven John Taylor, Zhaoming Xiong, Yang Yu, Qiang Zhang
  • Publication number: 20140200260
    Abstract: The invention provides methods for determining whether a subject is suffering from a rheumatoid arthritis associated with the BRAF oncogene comprising contacting isolated fibroblasts from the subject with a molecule or pool of molecules directed to the BRAF oncogene; and culturing the sample in the presence of the agent and determining whether BRAF oncogene expression by the cell is decreased and/or whether cells in the sample return to a less transformed phenotype, exhibit decreased cell proliferation and/or exhibit increased contact inhibition, any of which is indicative that the subject is suffering from a rheumatoid arthritis associated with the BRAF oncogene.
    Type: Application
    Filed: March 18, 2014
    Publication date: July 17, 2014
    Inventor: Richard H. Weisbart
  • Publication number: 20140200223
    Abstract: The present invention is directed to a compound represented by the following structural formula or a pharmaceutically acceptable salt thereof. Pharmaceutical compositions and method of use of the compounds are also described.
    Type: Application
    Filed: December 18, 2013
    Publication date: July 17, 2014
    Inventors: Salvacion Cacatian, David A. Claremon, Lawrence Wayne Dillard, Klaus Fuchs, Niklas Heine, Lanqi Jia, Katerina Leftheris, Brian Mckeever, Angel Morales-Ramos, Suresh B. Singh, Shankar Venkatraman, Guosheng Wu, Zhongren Wu, Zhenrong Xu, Jing Yuan, Yajun Zheng
  • Patent number: 8778938
    Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the Hepatitis C Virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the Hepatitis C Virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
    Type: Grant
    Filed: June 3, 2011
    Date of Patent: July 15, 2014
    Assignee: Enanta Pharmaceuticals, Inc.
    Inventors: Yao-Ling Qiu, Ce Wang, Hui Cao, Xiaowen Peng, Datong Tang, Yat Sun Or
  • Patent number: 8778976
    Abstract: The present invention relates to treatment and/or prevention of one or more metabolic disorders utilizing fatostatin A and/or a derivative and/or analog thereof. In other aspects, the compound for treatment and/or prevention of one or more metabolic disorders utilizes an A-B-C tripartite structure, wherein A, B, and C are identical or non-identical structures and are described in detail herein. In specific aspects, the metabolic disorder includes obesity or diabetes, for example.
    Type: Grant
    Filed: May 31, 2012
    Date of Patent: July 15, 2014
    Assignee: Baylor College of Medicine
    Inventors: Motonari Uesugi, Salih J. Wakil, Lutfi Abu-Elheiga, Qian Mao, Shinji Kamisuki, Akira Kugimiya
  • Patent number: 8778940
    Abstract: The present invention relates to compounds and methods for inducing neuronal differentiation in normal neural stem cells and brain cancer stem cells. The methods may take place in vitro, such as in isolates from the adult mammalian brain, or in vivo. Compounds and methods described herein may find use in the treatment of neurodegenerative and psychiatric diseases, the repair and regeneration of the nervous system, and in treatment of neurologic malignancy.
    Type: Grant
    Filed: June 4, 2012
    Date of Patent: July 15, 2014
    Assignee: The Board of Regents of the University of Texas System
    Inventors: Jay Schneider, Jenny Hsieh, Douglas Frantz, Steven L. McKnight, Joseph M. Ready
  • Patent number: 8778835
    Abstract: A composition comprising at least a pyridylethylbenzamide derivative of general formula (I) (a) and an insecticide compound (b) in a (a)/(b) weight ratio of from 1/1000 to 1000/1. A composition further comprising an additional fungicidal compound. A method for preventively or curatively combating the pests and diseases of crops by using this composition.
    Type: Grant
    Filed: July 5, 2007
    Date of Patent: July 15, 2014
    Assignee: Bayer Cropscience AG
    Inventors: Heike Hungenberg, Gilbert Labourdette, Albert Schirring, Burkhard Schuetz, Anne Suty-Heinze, Wolfgang Thielert, Martin Vaupel