1,3-thiazoles (including Hydrogenated) Patents (Class 514/365)
  • Publication number: 20140080820
    Abstract: The invention relates to novel fungicidally active compound combinations of 2?-cyano-3,4-dichloroisothiazole-5-carboxanilide of the formula and active compounds listed in the disclosure.
    Type: Application
    Filed: November 19, 2013
    Publication date: March 20, 2014
    Applicant: BAYER CROPSCIENCE AG
    Inventors: Peter DAHMEN, Ulrike WACHENDORFF-NEUMANN, Rolf PONTZEN, Wolfram ANDERSCH, Lutz ASSMANN
  • Publication number: 20140079630
    Abstract: The invention provides compositions and methods for visualizing particular tissues and delivering one or more therapeutics to that tissue using single-walled carbon nanotubes (SWNTs), which are taken up and delivered to target tissues by specific monocytes in the body. The delivery of SWNT to target tissues allows the visualization of the affected tissue for diagnostics and therapy in diseases where the specific monocyte is implicated in the disease pathogenesis. These nanotubes can be conjugated to a peptide, such as RGD, which helps direct the SWNT-containing monocytes to the vascular endothelium.
    Type: Application
    Filed: September 7, 2013
    Publication date: March 20, 2014
    Applicant: The Board of Trustees of the Leland Stanford Junior University
    Inventors: Bryan R. Smith, Eliver Ghosn
  • Patent number: 8673911
    Abstract: This invention relates to compounds and methods for the inhibition of HDAC enzymatic activity. More particularly, the invention provides for compounds of formula (I), (I) and N-oxides, hydrates, solvates, pharmaceutically acceptable salts, prodrugs and complexes thereof, and racemic and scalemic mixtures, diastereomers and enantiomers thereof, wherein L, M, n, R, W, X and Y are as defined in the specification.
    Type: Grant
    Filed: November 3, 2008
    Date of Patent: March 18, 2014
    Assignee: MethylGene Inc.
    Inventors: Tammy Mallais, Oscar Moradei, Alain Ajamian, Pierre Tessier, David Smil, Sylvie Frechette, Silvana Leit, Patrick Beaulieu, Robert Deziel, John Mancuso
  • Patent number: 8673946
    Abstract: This invention relates to novel 4-trimethylammoniobutyrates of the formula wherein A1, R1, m and n are as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds inhibit carnitine palmitoyl transferase (CPT) activity, in particular CPT2 activity, and can be used as medicaments.
    Type: Grant
    Filed: October 5, 2012
    Date of Patent: March 18, 2014
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Mirjana Andjelkovic, Simona M. Ceccarelli, Odile Chomienne, Patrizio Mattei
  • Patent number: 8673949
    Abstract: Methods of treating Tau-associated diseases, preferably tauopathies, are described using epothilone D that exhibit good brain penetration, long half-life, and high selective retention in brain, and provides effective therapies in treating tauopathies including Alzheimer's disease.
    Type: Grant
    Filed: June 1, 2011
    Date of Patent: March 18, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: Charles F. Albright, Donna Marie Barten, Francis Y. Lee
  • Publication number: 20140073676
    Abstract: Since a compound represented by the general formula (I) (wherein definition of each group is as described in the specification), a salt thereof, a solvate thereof, or a prodrug thereof has strong and sustaining intraocular pressure lowering activity and, further, has no side effect on eyes such as ocular stimulating property (hyperemia, corneal clouding etc.), aqueous humor protein rise etc., it has high safety, and can be an excellent agent for preventing and/or treating glaucoma etc.
    Type: Application
    Filed: November 15, 2013
    Publication date: March 13, 2014
    Applicant: ONO PHARMACEUTICAL CO., LTD.
    Inventors: Tohru KAMBE, Toru MARUYAMA, Shinsaku YAMANE, Satoshi NAKAYAMA, Kousuke TANI
  • Publication number: 20140073622
    Abstract: To develop an antibiotic having a novel mechanism of action, the present inventors have searched for a compound that has weak cytotoxicity, the physical property of high solubility in water, the effect of inhibiting both DNA gyrase GyrB and topoisomerase IV ParE subunits, and sufficient antibacterial activity. As a result, the present inventors have completed the present invention by finding that a compound of the present invention represented by the general formula (1), a pharmacologically acceptable salt thereof, and a prodrug thereof have desirable properties. The present invention provides a pharmaceutical composition (particularly, a preventive or therapeutic composition for infectious disease) comprising a compound represented by the formula (1), a pharmacologically acceptable salt thereof, or a prodrug thereof as an active ingredient.
    Type: Application
    Filed: September 13, 2013
    Publication date: March 13, 2014
    Applicant: Daiichi Sankyo Company, Limited
    Inventors: Tsuyoshi Soneda, Hiroshi Takeshita, Yoshiko Kagoshima, Yuko Yamamoto, Takafumi Hosokawa, Toshiyuki Konosu, Nobuhisa Masuda, Takuya Uchida, Issei Achiwa, Junichi Kuroyanagi, Tetsunori Fujisawa, Aki Yokomizo, Tetsuji Noguchi
  • Publication number: 20140066457
    Abstract: This invention provides novel compounds and the novel compounds for use as a medicine, more in particular for the prevention or treatment of neurodegenerative disorders, more specifically certain neurological disorders, such as disorders collectively known as tauopathies, and disorders characterized by cytotoxic ?-synuclein amyloidogenesis. The present invention also relates to the use of said novel compounds for the manufacture of medicaments useful for treating such neurodegenerative disorders. The present invention further relates to pharmaceutical compositions including said novel compounds and to methods for the preparation of said novel compounds.
    Type: Application
    Filed: October 22, 2013
    Publication date: March 6, 2014
    Applicants: reMYND, Katholieke Universiteit Leuven, K.U.Leuven R&D
    Inventors: Gerard Griffioen, Tom Van Dooren, Veronica Rojas De La Parra, Arnaud Marchand, Sara Allasia, Amuri Kilonda, Patrick Chaltin
  • Publication number: 20140065103
    Abstract: A compound is selected from the structural formulae depicted in FIG. 1 or a pharmaceutically acceptable salt thereof. A pharmaceutical composition comprises a compound selected from the structural formulae depicted in FIG. 1 or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier of excipient. A method of treating a HCV infection in a subject comprises administering to the subject a therapeutically effective amount of selected from the structural formulae depicted in FIG. 1 or a pharmaceutically acceptable salt thereof. A method of inhibiting or reducing the activity of HCV polymerase in a subject or in a biological in vitro sample comprises administering to the subject or to the sample a therapeutically effective amount of selected from the structural formulae depicted in FIG. 1 or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: February 14, 2013
    Publication date: March 6, 2014
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventor: VERTEX PHARMACEUTICALS INCORPORATED
  • Publication number: 20140066458
    Abstract: Disclosed are methods for treating Vascular Leak Syndrome. Further disclosed are methods for treating vascular leakage due to inflammatory diseases, inter alia, sepsis, lupus, irritable bowel disease. Yet further disclosed are methods for treating renal cell carcinoma and melanoma. Still further disclosed are methods for reducing metastasis of malignant cells and/or preventing the proliferation of carcinoma cells via spreading due to vascular leakage.
    Type: Application
    Filed: November 8, 2013
    Publication date: March 6, 2014
    Inventors: Robert Shalwitz, Kevin Gene Peters
  • Publication number: 20140066424
    Abstract: The present invention relates to compounds and methods which may be useful as inhibitors of HIF pathway activity for the treatment or prevention of cancer and other hypoxia-mediated diseases.
    Type: Application
    Filed: August 23, 2013
    Publication date: March 6, 2014
    Applicant: Institute For Applied Cancer Science/The University of Texas MD Anderson Cancer Center
    Inventors: Philip Jones, Maria Emilia DiFrancesco, Alessia Petrocchi, Christopher L. Carroll, Joe Marszalek, Barbara Czako, Ryan Johnson, Jay Theroff
  • Patent number: 8663606
    Abstract: A method for producing a cationic liposomal preparation comprising a lipophilic active compound with physical and chemical stability during manufacturing, storing and reconstituting, and further a cationic liposomal preparation obtainable by this method as well as specific cationic liposomal preparations as well as pharmaceutical compositions are disclosed.
    Type: Grant
    Filed: October 21, 2011
    Date of Patent: March 4, 2014
    Assignee: Medigene AG
    Inventors: Carsten Mundus, Christian Welz, Oliver Schramel, Heinrich Haas, Thomas Fichert, Brita Schulze, Toralf Peymann, Uwe Michaelis, Michael Teifel, Friedrich Gruber, Gerhard Winter
  • Publication number: 20140057903
    Abstract: This invention provides methods for identifying genes associated with cognitive impairment and for identifying compounds useful in the treatment of cognitive impairment. The methods can in particular be used to identify genes associated with, and compounds useful in treating, cognitive impairment in aging.
    Type: Application
    Filed: July 10, 2013
    Publication date: February 27, 2014
    Applicant: THE JOHNS HOPKINS UNIVERSITY
    Inventors: Michela Gallagher, Rebecca Haberman
  • Publication number: 20140057953
    Abstract: The invention relates to selective, non-steroidal 17beta-hydroxysteroid dehydrogenase type 2 (l7beta-HSD2) inhibitors of formula (I), their production and use, notably for the treatment and prophylaxis of sex steroid deficient diseases like osteoporosis in men and women.
    Type: Application
    Filed: March 2, 2012
    Publication date: February 27, 2014
    Inventors: Rolf Hartmann, Sandrine Marchais-Oberwinkler, Kuiying Xu, Ruth Werth
  • Patent number: 8658678
    Abstract: The combination of any two of a polyol, a polyol ether, and a low carbon organic alcohol provides a synergistic effect on the solubility of azole compounds, such as metronidazole, in aqueous fluid.
    Type: Grant
    Filed: December 8, 2010
    Date of Patent: February 25, 2014
    Assignee: Dow Pharmaceutical Sciences, Inc.
    Inventors: Meidong Yang, Haigang Chen
  • Patent number: 8658635
    Abstract: The invention is directed to certain novel compounds of formula (I) and salts thereof. The compounds of the invention are inhibitors of PI3-kinase activity.
    Type: Grant
    Filed: June 3, 2009
    Date of Patent: February 25, 2014
    Assignee: GlaxoSmithKline Intellectual Property Development Limited
    Inventors: Ian Robert Baldwin, Kenneth David Down, Paul Faulder, Simon Gaines, Julie Nicole Hamblin, Joelle Le, Christopher James Lunniss, Nigel James Parr, Timothy John Ritchie, John Edward Robinson, Juliet Kay Simpson, Christian Alan Paul Smethurst
  • Publication number: 20140051729
    Abstract: Methods and compositions for treating degenerative muscle conditions are disclosed. The compositions disclosed herein include S1P promoting compositions that include an S1P promoting agent. Embodiments of the methods disclosed herein include administering therapeutically effective amounts to subjects suffering from a degenerative muscle condition, such as, for example, subjects suffering from sarcopenia and subjects suffering from muscular dystrophy, including subjects suffering from Duchenne Muscular Dystrophy and Becker Muscular Dystrophy.
    Type: Application
    Filed: July 12, 2013
    Publication date: February 20, 2014
    Applicant: University of Washington
    Inventors: Nicholas Ieronimakis, Hannele Ruohola-Baker, Morayma Reyes, Junlin Qi, Mario Pantoja, Karin Fischer
  • Publication number: 20140050683
    Abstract: The invention relates to a compound of general formula (I) characterized in that: R1 is a C1-C4 alkyl group, and R2 is an optionally substituted nitrogen, sulfur or oxygen containing heteroaromatic ring.
    Type: Application
    Filed: February 7, 2012
    Publication date: February 20, 2014
    Applicant: PIERRE FABRE DERMO-COSMETIQUE
    Inventors: Stéphane Poigny, Françoise Belaubre
  • Publication number: 20140051733
    Abstract: The present application discloses stable pharmaceutical compositions for the oral administration of febuxostat with pharmaceutical excipients which provide improved dissolution rate and polymorphic stability both while manufacturing and during storage and process for preparing the stable compositions, packaging and their use in the treatment of gout of hyperuricemia.
    Type: Application
    Filed: August 12, 2013
    Publication date: February 20, 2014
    Applicant: Dr. Reddy's Laboratories Ltd.
    Inventors: Sunil Beeram Reddy, Amarnath Suseendharnath, Manikandan Ramalingam, Venkatesh Madhavacharya, Navin Vaya, Harshal Prabhakar Bhagwatwar, Venkateswarlu Vobalaboina
  • Publication number: 20140051734
    Abstract: This invention relates to a therapeutic method for glycaemic control, in particular to a method for the treatment of Pi-type 2 diabetes, comprising the administration of a DPIV inhibitor together with metformin or a thiazolidinedione
    Type: Application
    Filed: October 23, 2013
    Publication date: February 20, 2014
    Applicant: Royalty Pharma Collection Trust
    Inventor: Jonathan Rachman
  • Publication number: 20140051680
    Abstract: This invention relates to generally inhibiting histone deacetylase (HDAC) enzymes (e.g., HDAC1, HDAC2, and HDAC3).
    Type: Application
    Filed: February 28, 2012
    Publication date: February 20, 2014
    Applicant: REPLIGEN CORPORATION
    Inventors: Vincent Jacques, James R. Rusche, Norton P. Peet, Jasbir Singh
  • Publication number: 20140051709
    Abstract: Disclosed is a compound for treatment of Myotonic Dystrophy type 1 having the formula: Wherein X is selected from the group consisting of O, N, C, or S, Y is a homo- or heteroatomic 5-membered ring comprising one or more atoms selected from the group consisting of N, O, S, and C, Z is an optionally substituted aryl group or optionally substituted heteroaryl, including but not limited to halogenated benzenes, pyridines, substituted benzene, substituted pyridine, R2=hydroxy, acyl, alkoxyl, esters, ethers, cyclic ethers, and lactones, R3=H, alkyl, an optionally substituted alkyl, aliphatic ether, ester, cyclic unsaturated and aromatic ring groups, and R1, R4 and R5 are independently selected from the group consisting of hydrogen, halogen, alkyl, and alkoxyl or a pharmaceutically or cosmetically acceptable salt, solvate, or hydrate thereof.
    Type: Application
    Filed: August 16, 2012
    Publication date: February 20, 2014
    Applicant: UNIVERSITY OF SOUTHERN CALIFORNIA
    Inventors: Sita REDDY, Lucio Comai, Nouri Neamati
  • Patent number: 8653062
    Abstract: The present invention relates to novel cyclic amine and cycloalkyl derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
    Type: Grant
    Filed: November 22, 2010
    Date of Patent: February 18, 2014
    Assignee: Allergan, Inc.
    Inventors: Phong X. Nguyen, Todd M. Heidelbaugh
  • Patent number: 8653114
    Abstract: The present invention relates to O-CYCLOPROPYLCYCLOHEXYL-CARBOXANILIDES derivatives of formula (I); their process of preparation, their use as fungicide, particularly in the form of fungicide compositions, and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions.
    Type: Grant
    Filed: June 1, 2011
    Date of Patent: February 18, 2014
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Jörg Nico Greul, Jürgen Benting, Peter Dahmen, Ulrike Wachendorff-Neumann
  • Patent number: 8653072
    Abstract: The invention provides a compound of formula (I) or a pharmaceutically acceptable ester, amide, carbamate, solvate or salt thereof, including a salt of such an ester, amide or carbamate, and a solvate of such an ester, amide, carbamate or salt. The invention also provides also provides the use of such compounds in the treatment or prophylaxis of a condition associated with a disease or disorder associated with estrogen receptor activity, wherein R1, R2, R3, R5 and R6 are as defined in the specification.
    Type: Grant
    Filed: January 11, 2013
    Date of Patent: February 18, 2014
    Assignee: Karo Bio AB
    Inventors: Patrik Rhonnstad, Elisabet Kallin, Theresa Apelqvist, Mattias Wennerstal, Aiping Cheng
  • Patent number: 8653070
    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: December 14, 2010
    Date of Patent: February 18, 2014
    Assignee: Enanta Pharmaceuticals, Inc.
    Inventors: Yao-Ling Qiu, Ce Wang, Xiaowen Peng, Hui Cao, Lu Ying, Yat Sun Or
  • Patent number: 8653115
    Abstract: The invention relates a kind of antiviral agents, more concretely, relates to a kind of heterocyclic non-nucleoside compounds with the following structures, their preparation and pharmaceutical compositions including the compounds. The said compounds can be used as antiviral agents and as medicaments for treating diseases such as hepatitis B, influenza, herpes, HIV and so on.
    Type: Grant
    Filed: June 13, 2007
    Date of Patent: February 18, 2014
    Assignee: Shanghai Institute of Materia Medica, Chinese Academy of Sciences
    Inventors: Fajun Nan, Jianping Zuo, Haijun Chen, Guifeng Wang, Min Gu, Fenghua Zhu, Wei Tang
  • Publication number: 20140045971
    Abstract: A synergistic antimicrobial composition containing 3-iodo-2-propynyl-butylcarbamate and fluometuron.
    Type: Application
    Filed: October 18, 2013
    Publication date: February 13, 2014
    Inventors: Emerentiana Sianawati, Sangeeta Ganguly
  • Publication number: 20140045813
    Abstract: The present invention encompasses compounds of the formula (I) wherein the groups A, Cy, X1 and Y are defined herein, which are suitable for the treatment of diseases related to BTK, process of making, pharmaceutical preparations which contain compounds and their methods of use.
    Type: Application
    Filed: August 8, 2013
    Publication date: February 13, 2014
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Joerg Martin BENTZIEN, Angela Kay BERRY, Todd BOSANAC, Michael Jason BURKE, Darren Todd DISALVO, Joshua Courtney HORAN, Shuang LIANG, Can MAO, Wang MAO, Yue SHEN, Fariba SOLEYMANZADEH, Renee M. ZINDELL
  • Publication number: 20140045854
    Abstract: The present invention relates to methods of treating a disease related to cell hyper-proliferation 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.
    Type: Application
    Filed: October 11, 2013
    Publication date: February 13, 2014
    Inventors: Motonari Uesugi, Salih J. Wakil, Lutfi Al-Elheiga, Mizuki Watanabe
  • Publication number: 20140045850
    Abstract: This invention relates to compounds and methods for the inhibition of HDAC enzymatic activity. More particularly, the invention provides for compounds of formula (I), (I) and N-oxides, hydrates, solvates, pharmaceutically acceptable salts, prodrugs and complexes thereof, and racemic and scalemic mixtures, diastereomers and enantiomers thereof, wherein L, M, n, R, W, X and Y are as defined in the specification.
    Type: Application
    Filed: March 14, 2013
    Publication date: February 13, 2014
    Applicant: METHYLGENE INC.
    Inventor: METHYLGENE INC.
  • Patent number: 8648103
    Abstract: The present invention provides a compound having excellent regulating action on blood lipid level that is represented by the following general formula (I) or a pharmacologically acceptable salt thereof, wherein, in one embodiment, A represents a 5-membered nitrogen-containing aromatic heterocyclyl group; R1 represents COOH; each R2 represents an alkyl; each R3 represents an optionally substituted phenyl, an optionally substituted phenylalkyl; m represents 0, 1, 2, or 3; n represents 0 or 1; each of R4, R5, R6, and R7 represents H, an alkyl; and B represents an optionally substituted naphthyl, an optionally substituted aromatic heterocyclyl, or a group represented by the following formula (II) wherein each of B1 and B2 represents an optionally substituted phenyl or an optionally substituted aromatic heterocyclyl.
    Type: Grant
    Filed: July 7, 2009
    Date of Patent: February 11, 2014
    Assignee: Daiichi Sankyo Company, Limited
    Inventors: Keiko Suzuki, Takahiro Yamaguchi, Akihiro Tamura, Tomohiro Nishizawa, Mitsuhiro Yamaguchi
  • Publication number: 20140039009
    Abstract: The invention relates to compounds of structural formulas (I), (VII) and (XI): or a pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof, wherein X1, X2, X3, Y, Z, L, R1, R2, R3, R18 and n 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: October 15, 2013
    Publication date: February 6, 2014
    Applicant: Synta Pharmaceuticals Corp.
    Inventors: Lijun Sun, Shoujun Chen, Zhiqiang Xia, Jun Jiang, Yu Xie, Junyi Zhang
  • Publication number: 20140038919
    Abstract: This disclosure relates to: (a) compounds and salts thereof that, inter alia, inhibit HCV; (b) intermediates useful for the preparation of such compounds and salts; (c) compositions comprising such compounds and salts; (d) methods for preparing such intermediates, compounds, salts, and compositions; (e) methods of use of such compounds, salts, and compositions; and (f) kits comprising such compounds, salts, and compositions.
    Type: Application
    Filed: December 16, 2011
    Publication date: February 6, 2014
    Applicant: AbbVie Inc.
    Inventors: Clarence J. Maring, John K. Pratt, William A. Carroll, Dachun Liu, David A. Betebenner, Douglas K. Hutchinson, Michael D. Tufano, Todd W. Rockway, Uwe Schoen, Axel Pahl, Andreas Witte
  • Publication number: 20140038956
    Abstract: The use of sGC stimulators, sGC activators alone, or in combination with PDE5 inhibitors for the prevention and treatment of fibrotic diseases, such as systemic sclerosis, scleroderma, and the concomitant fibrosis of internal organs.
    Type: Application
    Filed: May 24, 2011
    Publication date: February 6, 2014
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Claudia Hirth-Dietrich, Peter Sandner, Johannes-Peter Stasch, Andreas Knorr, Georges Von Degenfeld, Michael Hahn, Markus Follmann
  • Publication number: 20140038964
    Abstract: Methods of using compounds of the invention, such as compounds of Formulae IIa, IIb, IIc, or IId and pharmaceutically acceptable salts thereof are disclosed. The compounds are useful in treating, preventing, inhibiting or ameliorating the symptoms of a disease or disorder that is modulated or otherwise affected by nuclear receptor activity, or in which nuclear receptor activity is implicated.
    Type: Application
    Filed: July 25, 2013
    Publication date: February 6, 2014
    Applicant: Exelixis Patent Company LLC
    Inventors: Brett B. Busch, Brenton T. Flatt, Xiao-Hui Gu, Shao Po Lu, Richard Martin, Raju Mohan, Michael Charles Nyman, Edwin J. Schweiger, William C. Stevens, JR., Tie-Lin Wang, Yinong Xie
  • Publication number: 20140038984
    Abstract: The present invention relates to 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, for example, but not limited to, heterocyclic, phenyl or benzyl ring structures with or without substitutions and are described in detail herein. Also provided are methods for the treatment and/or prevention of one or more metabolic disorders, for example, obesity or diabetes, utilizing fatostatin A and/or a derivative and/or analog thereof and/or the A-B-C tripartite compounds.
    Type: Application
    Filed: August 29, 2013
    Publication date: February 6, 2014
    Inventors: Motonari Uesugi, Salih J. Wakil, Lutfi Al-Elheiga, Mizuki Watanabe
  • Patent number: 8642634
    Abstract: Disclosed are compounds of Formulae 1, 1A, 1B and 1C including all geometric and stereoisomers, N-oxides, and salts thereof, wherein R1, R2, R4a1, R4a2, A, Aa, G, M, W, Z1, Z3, X, J, J1 and n are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention.
    Type: Grant
    Filed: July 27, 2007
    Date of Patent: February 4, 2014
    Assignee: E I du Pont de Nemours and Company
    Inventors: Robert James Pasteris, Mary Ann Hanagan
  • Patent number: 8642642
    Abstract: The invention relates to compounds of the formula (I) wherein the variables have meanings given in the claims and the description. The invention also relates to the use of a compound of the formula (I) or a pharmaceutically acceptable salt thereof for preparing a medicament for the treatment of a medical disorder susceptible to the treatment with a 5HT6 receptor ligand.
    Type: Grant
    Filed: April 18, 2007
    Date of Patent: February 4, 2014
    Assignees: Abbott Laboratories, AbbVie Deutschland GmbH & Co. KG
    Inventors: Roland Grandel, Wilfried Martin Braje, Andreas Haupt, Sean Colm Turner, Udo Lange, Karla Drescher, Liliane Unger, Dan Plata
  • Patent number: 8642625
    Abstract: A therapeutic agent or prophylactic agent is effective for therapy of urine storage disorders, by which agent improvement of side effects due to an anticholinergic action is attained as well as which agent also has an analgesic effect. The agent includes as an effective ingredient a cyclohexane derivative exemplified by the formula below, a pharmaceutically acceptable salt thereof, or a prodrug thereof.
    Type: Grant
    Filed: March 31, 2011
    Date of Patent: February 4, 2014
    Assignee: Toray Industries, Inc.
    Inventors: Nana Hareyama, Satoru Yoshikawa, Kaoru Nakao
  • Patent number: 8642585
    Abstract: The present invention relates to compounds of general formula I, wherein the groups R1, R2 and m are defined as in claim 1, which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2.
    Type: Grant
    Filed: March 14, 2013
    Date of Patent: February 4, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Matthias Eckhardt, Sara Frattini, Dieter Hamprecht, Frank Himmelsbach, Elke Langkopf, Iain Lingard, Stefan Peters, Holger Wagner
  • Publication number: 20140030351
    Abstract: The present disclosure relates in part to pharmaceutical compositions comprising polymeric nanoparticles having certain glass transition temperatures. Other aspects of the invention include methods of making such nanoparticles.
    Type: Application
    Filed: September 27, 2013
    Publication date: January 30, 2014
    Applicant: BIND Therapeutics, Inc.
    Inventors: Stephen E. Zale, Greg Troiano, Mir Mukkaram Ali, Jeff Hrkach, James Wright
  • Publication number: 20140031353
    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: Application
    Filed: January 30, 2011
    Publication date: January 30, 2014
    Applicant: CUREGENIX, INC.
    Inventors: Songzhu An, Chufang Li, Guisheng Zhou, Chen Huang
  • Publication number: 20140031207
    Abstract: The present invention relates to novel pesticidal compositions comprising Hither as component A: clothianidin, as component B: ipconazole Or as component A: clothianidin, as component B: ipconazole as component C: metalaxyl that show surprisingly good insecticidal, acaricidal, nematicidal and fungicidal activities. In particular, these compositions are suited for the treatment of seed.
    Type: Application
    Filed: September 25, 2013
    Publication date: January 30, 2014
    Inventors: Wolfram ANDERSCH, Heike Hungenberg, Peter-Wilhelm Krohn
  • Patent number: 8637557
    Abstract: A compound represented by formula (1) or a pharmaceutically acceptable salt thereof, which has a PI3 kinase ? inhibitory effect and is useful as a prophylactic or therapeutic agent for articular rheumatism, Crohn's disease, irritable colitis, Sjoegren's syndrome, multiple sclerosis, systemic lupus erythematosus, asthma, atopic dermatitis, arteriosclerosis, organ transplant rejection, cancer, retinopathy, psoriasis, arthrosis deformans, age-related macular degeneration, type II diabetes, insulin resistance, obesity, non-alcoholic fatty liver disease (NAFLD), non-alcoholic steatohepatitis (NASH), hyperlipemia, etc.
    Type: Grant
    Filed: October 4, 2010
    Date of Patent: January 28, 2014
    Assignee: Taisho Pharmaceutical Co., Ltd
    Inventors: Tetsuya Yabuuchi, Yusuke Oka, Shoichi Kuroda, Takahiro Oi, Yoshinori Sekiguchi
  • Patent number: 8637552
    Abstract: This invention pertains to methods for protecting a propagule or a plant grown therefrom from invertebrate pests comprising contacting the propagule or the locus of the propagule with a biologically effective amount of a compound of Formula I, its N-oxide or an agriculturally suitable salt thereof wherein A and B and R1 through R8 are as defined in the disclosure. This invention also relates to propagules treated with a compound of Formula I and compositions comprising a Formula I compound for coating propagules.
    Type: Grant
    Filed: August 10, 2012
    Date of Patent: January 28, 2014
    Assignee: E I du Pont de Nemours and Company
    Inventors: Richard Alan Berger, Isaac Billy Annan, George Philip Lahm, John Lindsey Flexner, Thomas Paul Selby, Thomas Martin Stevenson
  • Patent number: 8637567
    Abstract: This invention provides compounds, compositions and methods for treating a cognitive disorder or memory disorder in animals that result from aging or other neurodegenerative condition. In particular, compounds of this invention can stimulate neural cell growth, increased amounts of cells containing a key enzyme needed for production of the cholinergic neurotransmitter, and can improve memory and cognitive function in animals who have experienced a loss of memory or cognitive function.
    Type: Grant
    Filed: October 13, 2010
    Date of Patent: January 28, 2014
    Assignee: Neuren Pharmaceuticals Ltd.
    Inventors: Peter David Gluckman, Jian Guan, Mary-Anne Woodnorth, Margaret Anne Brimble
  • Publication number: 20140024618
    Abstract: The present invention relates to new indole compounds, pharmaceutically acceptable salts or isomers thereof which are useful for the prevention or treatment of cellular necrosis and necrosis-associated diseases. The present invention also relates to a method and a composition for the prevention or treatment of cellular necrosis and necrosis-associated diseases, comprising said indole compounds as an active ingredient.
    Type: Application
    Filed: September 23, 2013
    Publication date: January 23, 2014
    Applicant: LG LIFE SCIENCES LTD.
    Inventors: Soon Ha KIM, Hyoung Jin KIM, Sun Young KOO, Sung Bae LEE, Heui Sul PARK, Seung Hyun YOON, Seung Yup PAEK, Hyo Shin KWAK, Dong Ook SEO, Eok PARK
  • Publication number: 20140024671
    Abstract: Methods of inhibiting cytochrome P450 enzymes are provided that can be used for improving the treatment of diseases by preventing degradation of drugs or other molecules by cytochrome P450. Pharmaceutical compositions are provided that can act as boosters to improve the pharmacokinetics, enhance the bioavailability, and enhance the therapeutic effect of drugs that undergo in vivo degradation by cytochrome P450 enzymes.
    Type: Application
    Filed: July 9, 2013
    Publication date: January 23, 2014
    Inventors: Michael EISSENSTAT, Dehui DUAN
  • Publication number: 20140024603
    Abstract: New fibroblast growth factor receptor 1 (FGFR1) inhibitors have been identified which are useful for promoting the retention and/or growth of keratin fibers, such as hair of the scalp, hair of the face (moustache, beard, etc.), eyebrows, eyelashes, and the like. The FGFR1 inhibitors may be formulated in effective amounts in a variety of cosmetic and personal care products.
    Type: Application
    Filed: September 25, 2013
    Publication date: January 23, 2014
    Applicant: Avon Products, Inc.
    Inventors: Michele C. Duggan, Satish Parimoo, Cheng S. Hwang