Plural Double Bonds Between The Ring Members Of The Oxazole Ring Patents (Class 548/235)
  • Publication number: 20140073501
    Abstract: A species of Burkholderia sp with no known pathogenicity to vertebrates but with pesticidal activity (e.g., plants, insects, fungi, weeds and nematodes) is provided. Also provided are natural products derived from a culture of said species and methods of controlling pests using said natural products.
    Type: Application
    Filed: March 15, 2013
    Publication date: March 13, 2014
    Inventors: Ratnakar Asolkar, Marja Koivunen, Pamela Marrone
  • 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: 8658646
    Abstract: The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula I, wherein the variables are defined as described herein, which inhibit JAK and SYK and are useful for the treatment of auto-immune and inflammatory diseases.
    Type: Grant
    Filed: August 31, 2012
    Date of Patent: February 25, 2014
    Assignee: Hoffmann-LaRoche Inc.
    Inventors: Shaoqing Chen, Javier de Vicente Fidalgo, Matthew Michael Hamilton, Johannes Cornelius Hermann, Joshua Kennedy-Smith, Hongju Li, Allen John Lovey, Matthew C. Lucas, Kin-Chun Thomas Luk, Stephen M. Lynch, Counde O'yang, Fernando Padilla, Ryan Craig Schoenfeld, Achyutharao Sidduri, Michael Soth, Ce Wang, Peter Michael Wovkulich, Xiaohu Zhang
  • Publication number: 20140038975
    Abstract: The present invention is directed to a new class of hydroxamic acid derivatives, their use as LpxC inhibitors and, more specifically, their use to treat bacterial infections.
    Type: Application
    Filed: March 27, 2012
    Publication date: February 6, 2014
    Inventors: Matthew Frank Brown, Jinshan Michael Chen, Michael Joseph Melnick, Justin Ian Montgomery, Usa Reilly
  • 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
  • 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: 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: 8637559
    Abstract: The present invention provides a oxazole compound represented by Formula (1), or a salt thereof: wherein R1 is an aryl group which may have one or more substituents; R2 is an aryl group or a nitrogen atom-containing heterocyclic group each of which may have one or more substituents; and W is a divalent group represented by —Y1-A1- or —Y2—C(?O)— wherein Y1 is a group such as —C(?O)—, A1 is a group such as a lower alkylene group, and Y2 is a group such as a piperazinediyl group. The oxazole compound has a specific inhibitory action against phosphodiesterase 4.
    Type: Grant
    Filed: November 14, 2006
    Date of Patent: January 28, 2014
    Assignee: Otsuka Pharmaceutical Co., Ltd.
    Inventors: Minoru Okada, Masaya Kato, Norifumi Sato, Tetsuyuki Uno, Hideki Kitagaki, Junpei Haruta, Hidetaka Hiyama, Tomonori Shibata
  • Publication number: 20130345419
    Abstract: Provided are novel compounds that bind to FKBP12 or pharmaceutically acceptable salts thereof, as well as new therapeutics useful in the prevention or treatment of alopecia which comprise those compounds or pharmaceutically acceptable salts thereof. Specifically, compounds represented by formula (1) [where R1 represents either the following formula (2) or (3)] or pharmaceutically acceptable salts thereof are provided.
    Type: Application
    Filed: March 15, 2012
    Publication date: December 26, 2013
    Applicant: TAISHO PHARMACEUTICAL CO., LTD.
    Inventors: Naoya Ono, Shoichi Kuroda, Yoshihisa Shirasaki, Tetsuo Takayama, Yoshinori Sekiguchi, Fumihito Ushiyama, Yusuke Oka
  • Publication number: 20130338202
    Abstract: Compounds and their pharmaceutically acceptable salts for treatment of synucleinopathies, such as Parkinson's disease and tauopathies.
    Type: Application
    Filed: March 1, 2012
    Publication date: December 19, 2013
    Applicant: PROTEO TECH, INC
    Inventors: Luke A. Esposito, Marisa C. Yadon, Joel Cummings, F. Michael Hudson, Thomas Lake, Franz F. Hefti, Geoffrey Golding, Seok-Rye Choi, Ximin Li, Alan D. Snow, Qubai Hu, Judy Cam
  • Publication number: 20130331419
    Abstract: Disclosed are the compounds of the Formula (I) as well as pharmaceutically acceptable salts thereof, which are useful for treating aldosterone-mediated diseases. The processes for preparing compounds of the Formula (I), the use for the therapy and prophylaxis of the abovementioned diseases and for preparing pharmaceuticals for this purpose, and the pharmaceutical compositions which comprise compounds of the formula (I) are disclosed too.
    Type: Application
    Filed: January 19, 2012
    Publication date: December 12, 2013
    Inventors: Alejandro Crespo, Ping Lan, Rudrajit Mal, Anthony Ogawa, Hong Shen, Peter J. Sinclair, Zhongxiang Sun, Ellen K. Vande Bunte, Zhicai Wu, Kun Liu, Robert J. DeVita, Dong-Ming Shen, Min Shu, John Qiang Tan, Changhe Qi, Yuguang Wang, Richard Beresis
  • Patent number: 8604034
    Abstract: The present invention relates to compounds of formula (I) its salts, isomers or prodrugs thereof useful in the treatment of viral infections, in particular respiratory syncytial virus (RSV) infections. The present invention also relates to processes for preparing the compounds and intermediates used in their preparation.
    Type: Grant
    Filed: February 8, 2011
    Date of Patent: December 10, 2013
    Assignee: Biota Scientific Management Pty Ltd.
    Inventors: Jeffrey Peter Mitchell, Gary Pitt, Alistair George Draffan, Penelope Anne Mayes, Laura Andrau, Kelly Anderson
  • Patent number: 8598212
    Abstract: A therapeutic agent or prophylactic agent for Alzheimer's disease has an effect to inhibit or delay the progress of Alzheimer's disease and exhibits a long-lasting therapeutic effect on Alzheimer's disease even when used for a long period of time. The therapeutic agent or prophylactic agent for Alzheimer's disease includes as an effective ingredient a cyclohexane derivative exemplified by the formula below, or a pharmaceutically acceptable salt thereof or a prodrug thereof.
    Type: Grant
    Filed: April 28, 2011
    Date of Patent: December 3, 2013
    Assignee: Toray Industries, Inc.
    Inventors: Kaoru Nakao, Yohei Miyamoto, Naohiro Yamada
  • Publication number: 20130296274
    Abstract: Compounds of the formula I in which R1, R2, R3 and R4 have the meanings indicated in Claim 1, are inhibitors of methionine aminopeptidase and can be employed for the treatment of tumours.
    Type: Application
    Filed: September 14, 2011
    Publication date: November 7, 2013
    Applicant: Merck Patent GmbH
    Inventors: Timo Heinrich, Frank Zenke, Michel Calderini, Djordje Musil
  • Publication number: 20130296322
    Abstract: In one aspect, the invention relates to compounds of formula I: where Y, R1, R2, n, and Q are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds of formula I are serotonin reuptake inhibitors. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.
    Type: Application
    Filed: July 8, 2013
    Publication date: November 7, 2013
    Applicant: THERAVANCE, INC.
    Inventors: Eric L. Stangeland, Lori Jean Van Orden, Daisuke Roland Saito
  • Publication number: 20130296166
    Abstract: Compositions and processes for controlling nematodes are described herein, e.g., nematodes that infest plants or animals. The compounds include oxazoles, oxadiazoles and thiadiazoles.
    Type: Application
    Filed: April 3, 2013
    Publication date: November 7, 2013
    Inventors: Deryck J. Williams, Matt W. Dimmic, William P. Haakenson, Al Wideman, Barry J. Shortt, Tim Cheeseright, Michael J. Crawford
  • Patent number: 8569331
    Abstract: The present invention relates to substituted benzo[f]imidazo[1,2-d]pyrido[2,3-b][1,4]diazepine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted benzo[f]imidazo[1,2-d]pyrido[2,3-b][1,4]diazepine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.
    Type: Grant
    Filed: November 1, 2011
    Date of Patent: October 29, 2013
    Assignee: ArQule, Inc.
    Inventors: Mark A. Ashwell, Sudharshan Eathiraj, Anton Filikov, Steffi Koerner, Jean-Marc Lapierre, Yanbin Liu, Rocio Palma, David Vensel, Shin Iimura, Akiko Shiina, Kenichi Yoshida, Takanori Yamazaki, Akihisa Matsuda
  • Patent number: 8569349
    Abstract: Compounds comprising formula (I) or a pharmaceutically acceptable salt thereof, a dashed line represent the presence or absence of a double bond, are disclosed, wherein J1, J2, U1, B, Y, and A are as described in claims 1-12. Methods, compositions, and medicaments related thereto are also disclosed, for treating glaucoma, inflammatory bowel disease and baldness.
    Type: Grant
    Filed: May 4, 2009
    Date of Patent: October 29, 2013
    Assignee: Allergan, Inc.
    Inventors: David W. Old, Vinh X. Ngo
  • Publication number: 20130274240
    Abstract: The present invention provides an agent for the prophylactic or treatment of diabetes, diabetic complications, insulin resistance syndrome, metabolic syndrome, hyperglycemia, dyslipidemia, atherosclerosis, cardiac failure, cardiomyopathy, myocardial ischemia, brain ischemia, cerebral apoplexy, pulmonary hypertension, hyperlactacidemia, mitochondrial disease, mitochondrial encephalomyopathy or cancer, namely, a PDHK inhibitor and the like. A compound represented by the following formula [I] or a pharmaceutically acceptable salt thereof, or a solvate thereof: wherein each symbol is as defined in the specification.
    Type: Application
    Filed: November 5, 2012
    Publication date: October 17, 2013
    Inventor: JAPAN TOBACCO INC.
  • Patent number: 8551992
    Abstract: Oxazole derivatives are described. The inventive compounds are useful as kinase inhibitors, and may be used in the treatment of cancer, such as prostate cancer, lung cancer, breast cancer, colon cancer, leukemia, CNS cancer, melanoma, ovarian cancer, and renal cancer.
    Type: Grant
    Filed: May 23, 2012
    Date of Patent: October 8, 2013
    Assignee: Neosome Life Sciences, LLC
    Inventors: Laxman S. Desai, Srinivas Chittaboina
  • Patent number: 8552203
    Abstract: This invention relates to novel indane acetic acid derivatives which are useful in the treatment of diseases such as diabetes, obesity, hyperlipidemia, and atherosclerotic diseases. The invention also relates to intermediates useful in preparation of indane acetic derivatives and to methods of preparation.
    Type: Grant
    Filed: February 25, 2011
    Date of Patent: October 8, 2013
    Assignee: Bayer Healthcare LLC
    Inventors: Derek B. Lowe, Philip L. Wickens, Xin Ma, Mingbao Zhang, William H. Bullock, Philip D. G. Coish, Ingo A. Mugge, Andreas Stolle, Ming Wang, Yamin Wang, Chengzhi Zhang, Hai-Jun Zhang, Lei Zhu, Manami Tsutsumi, James N. Livingston
  • Patent number: 8552205
    Abstract: Derivatives of 6,7-dihydro-5H-imidazo[1,2-?]imidazole-3-carboxylic acid amide exhibit good inhibitory effect upon the interaction of CAMs and Leukointegrins and are thus useful in the treatment of inflammatory disease.
    Type: Grant
    Filed: November 20, 2008
    Date of Patent: October 8, 2013
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Antonio Jose del Moral Barbosa, Jr., Joerg Martin Bentzien, Steven Richard Brunette, Zhidong Chen, Derek Cogan, Donghong A. Gao, Alexander Heim-Riether, Joshua Courtney Horan, Jennifer A. Kowalski, Michael David Lawlor, Rene Marc Lemieux, Weimin Liu, Bryan McKibben, Craig Andrew Miller, Neil Moss, Matt Aaron Tschantz, Zhaoming Xiong, Hui Yu, Yang Yu
  • Publication number: 20130252937
    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: Application
    Filed: March 14, 2013
    Publication date: September 26, 2013
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Matthias ECKHARDT, Sara FRATTINI, Dieter HAMPRECHT, Frank HIMMELSBACH, Elke LANGKOPF, Iain LINGARD, Stefan PETERS, Holger WAGNER
  • Publication number: 20130253008
    Abstract: The present invention relates to novel azoles, novel antiviral active components of the general formulas 1A and 1B, pharmaceutical composition, antiviral medicament, method for prophylaxis and treatment of viral diseases, particularly caused by hepatitis C viruses (HCV). In general formulas 1A and 1B wherein: solid lines with accompanying dotted lines () represent ordinary bond or double bond, provided that one of them is an ordinary bond, the other one is double bond; X and Y accept various meanings, one of them is—nitrogen, the other—oxygen, sulfur or NH group; R1 and R2—optionally the same radicals selected from 2-(R)- and (S)-substituted N-acyl pyrrolidine derivatives; N-methyl-N-[2-(R) and (S)-substituted 2,2-disubstituted acetamides; methyl[2-(R) and (S)-substituted ((methyl)amino)-(1-oxobutan-2-yl)-2-(R)-] and (S)-iso-propyl)-carbamates.
    Type: Application
    Filed: November 28, 2011
    Publication date: September 26, 2013
    Applicant: Alla Chem LLC
    Inventors: Alexandre Vasilievich Ivachtchenko, Vadim Vasilievich Bichko, Oleg Dmitrievich Mitkin
  • Patent number: 8513235
    Abstract: The invention provides a homocysteine synthase inhibitor useful for the prophylaxis or treatment of diseases involving homocysteine synthase. The homocysteine synthase inhibitor is a compound of the formula (I) wherein each symbol is as defined herein, or a pharmacologically acceptable salt thereof, or a solvate thereof.
    Type: Grant
    Filed: April 10, 2009
    Date of Patent: August 20, 2013
    Assignee: Mitsubishi Tanabe Pharma Corporation
    Inventors: Akira Nakao, Hiroko Suzuki, Ryo Tatsumi, Maki Seki, Minoru Tanaka, Tomofumi Setsuta, Hiroshi Iwasaki
  • Publication number: 20130203593
    Abstract: This document discloses molecules having the following formulas (“Formula One” & “Formula Two” and “Formula Three”) The Ar1, Het, Ar2, R1, R2, R3, R4, and R5 are further described herein.
    Type: Application
    Filed: January 23, 2013
    Publication date: August 8, 2013
    Applicant: Dow AgroSciences LLC
    Inventor: Dow AgroSciences LLC
  • Publication number: 20130203592
    Abstract: This document discloses molecules having the following formulas (“Formula One” &“Formula Two” and “Formula Three”) The Ar1, Het, Ar2, R1, R2, R3, R4, and R5 are further described herein.
    Type: Application
    Filed: January 22, 2013
    Publication date: August 8, 2013
    Applicant: Dow AgroSciences LLC
    Inventor: Dow AgroSciences LLC
  • Publication number: 20130197044
    Abstract: The present invention is directed to methods of treating hepatorenal syndrome by administration of a therapeutically effective amount of a thromboxane A2 receptor antagonist to a patient in need thereof. The present invention is also directed to methods of treating hepatic encephalopathy and cerebral edema by administration of a therapeutically effective amount of a thromboxane A2 receptor antagonist to a patient in need thereof.
    Type: Application
    Filed: July 14, 2011
    Publication date: August 1, 2013
    Inventors: Leo Pavliv, Martin Ogletree
  • Publication number: 20130190503
    Abstract: A therapeutic agent or prophylactic agent has an analgesic effect on both nociceptive pain and neuropathic pain and is effective in treatment of fibromyalgia. The agent includes as an effective ingredient a cyclohexane derivative or a pharmaceutically acceptable salt thereof or a prodrug thereof.
    Type: Application
    Filed: March 31, 2011
    Publication date: July 25, 2013
    Applicant: TORAY INDUSTRIES, INC.
    Inventors: Chihiro Yoshida, Kaoru Nakao
  • Publication number: 20130181135
    Abstract: A material according to one embodiment exhibits an optical response signature for neutrons that is different than an optical response signature for gamma rays, said material exhibiting performance comparable to or superior to stilbene in terms of distinguishing neutrons from gamma rays, wherein the material is not stilbene, the material comprising a molecule selected from a group consisting of: two or more benzene rings, one or more benzene rings with a carboxylic acid group, one or more benzene rings with at least one double bound adjacent to said benzene ring, and one or more benzene rings for which at least one atom in the benzene ring is not carbon.
    Type: Application
    Filed: January 8, 2013
    Publication date: July 18, 2013
    Applicant: LAWRENCE LIVERMORE NATIONAL SECURITY, LLC
    Inventor: Lawrence Livermore National Security, LLC
  • Publication number: 20130172339
    Abstract: A compound of formula (I), wherein A is S, O or a double bond, and L is a substituted thiazolyl, phenyl or pyridyl. The compound is useful for the treatment of inflammation and cancer.
    Type: Application
    Filed: September 19, 2011
    Publication date: July 4, 2013
    Applicant: KANCERA AB
    Inventors: Styrbjorn Bystrom, Charles Hedgecock, Evert Homan, Thomas Lundback, Jessica Martinsson, Meral Sari, Katarina Farnegardh, Mattias Jonsson
  • Patent number: 8470810
    Abstract: The invention relates to compounds of the formula (I) wherein n is 0, 1 or 2; G is CH2 or CHR3; R1 is H, C,-C6-alkyl, C,-C6-alkyl substituted by C3-C6-cycloalkyl, C1-C6-hydroxyalkyl, fluorinated C,-C6-alkyl, C3-C6-cycloalkyl, fluorinated C3-C6-cycloalkyl, C3-C6 alkenyl, fluorinated C3-C6-alkenyl, formyl, acetyl or propionyl; R2, R3 and R4 are, independently of each other, H, methyl, fluoromethyl, difluoromethyl, or trifluoromethyl; A is phenylene, pyridylene, pyrimidylene, pyrazinylene, pyridazinylene or thiophenylene, which can be substituted by one or more substituents selected from halogen, methyl, methoxy and CF3; E is NR5 or CH2, wherein R5 is H or C1-C3-alkyl; Ar is a cyclic radical selected from the group consisting of phenyl, a 5- or 6-membered heteroaromatic radical comprising as ring members 1, 2 or 3 heteroatoms selected from N, O and S and a phenyl ring fused to a saturated or unsaturated 5- or 6-membered carbocyclic or heterocyclic ring, where the heterocyclic ring comprises as ring members 1, 2
    Type: Grant
    Filed: August 25, 2010
    Date of Patent: June 25, 2013
    Assignee: Abbott GmbH & Co. KG
    Inventors: Karla Drescher, Andreas Haupt, Liliane Unger, Sean C. Turner, Wilfried Braje, Roland Grandel, Christophe Henry, Gisela Backfisch, Armin Beyerbach, Wilfried Lubisch
  • Publication number: 20130158075
    Abstract: The present invention relates to heterocyclic compounds of formula 1, in all their stereoisomeric and tautomeric forms; and their pharmaceutically acceptable salts, solvates, polymorphs, prodrugs, carboxylic acid isosteres and N-oxides. The invention also relates to processes for the manufacture of the heterocyclic compounds and to pharmaceutical compositions containing them. The said compounds and their pharmaceutical compositions are useful in the prevention and treatment of diseases or disorders mediated by diacylglycerol acyltransferase (DGAT), particularly DGAT1. The present invention further provides a method of treatment of such diseases or disorders by administering a therapeutically effective amount of said compounds or their pharmaceutical compositions, to a mammal in need thereof.
    Type: Application
    Filed: August 31, 2011
    Publication date: June 20, 2013
    Applicant: PIRAMAL ENTERPRISES LIMITED
    Inventors: Rajiv Sharma, Kishorkumar Shivajirao Kadam, Ravindra Dnyandev Jadhav, Shivaji Sadashiv Kandre, Amol Gupte
  • Patent number: 8466149
    Abstract: In its many embodiments, the present invention relates to a novel class of 6-substituted sulfonyl-1,3,3-trialkyl-6-azabicyclo[3.2.1]octane compounds useful to inhibit 11?-hydroxysteroid dehydrogenase type-I, pharmaceutical compositions containing the compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the expression of 11?-hydroxysteroid dehydrogenase type-I using such compounds or pharmaceutical compositions.
    Type: Grant
    Filed: August 12, 2008
    Date of Patent: June 18, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Craig D. Boyle, Samuel Chackalamannil, Unmesh Shah, Claire M. Lankin
  • Publication number: 20130150392
    Abstract: The compound (I) or a salt thereof has an excellent controlling activity against pests. Then the compound (I) or a salt thereof is useful for an active ingredient of a pesticidal composition.
    Type: Application
    Filed: February 8, 2013
    Publication date: June 13, 2013
    Applicant: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventor: SUMITOMO CHEMICAL COMPANY, LIMITED
  • Patent number: 8455525
    Abstract: This invention provides compounds of formulas I, Ia, Ib, Ic, Id, Ie, and or salts thereof, pharmaceutical compositions comprising a compound of formulas I, Ia, Ib, Ic, Id, Ie, and a pharmaceutically acceptable excipient, methods of modulating the androgen receptor, methods of treating diseases beneficially treated by an androgen receptor modulator (e.g., sarcopenia, prostate cancer, contraception, type 2 diabetes related disorders or diseases, anemia, depression, and renal disease) and processes for making compounds of formulas I, Ia, Ib, Ic, Id, Ie, and intermediates useful in the preparation of same.
    Type: Grant
    Filed: August 17, 2010
    Date of Patent: June 4, 2013
    Assignee: Radius Health, Inc.
    Inventor: Chris P. Miller
  • Publication number: 20130137865
    Abstract: A compound represented by formula [I] and a pharmaceutically accepted salt of said compound are a novel compound and a pharmaceutically accepted salt thereof which exert antagonistic activity against group II metabotropic glutamate (mGlu) receptors, and are effective as a novel preventive or therapeutic agent for disorders such as mood disorders (depressive disorder, bipolar disorder, etc.), anxiety disorders (generalized anxiety disorder, panic disorder, obsessive-compulsive disorder, social anxiety disorder, posttraumatic stress disorder, a specific phobic disorder, acute stress disorder, etc.), schizophrenia, Alzheimer's disease, cognitive impairment, dementia, drug dependence, convulsions, shivering, pain, sleep disorders, and the like.
    Type: Application
    Filed: August 11, 2011
    Publication date: May 30, 2013
    Applicant: TAISHO PHARMACEUTICAL CO., LTD.
    Inventors: Toshio Nakamura, Kazunari Sakagami, Kazuhide Konishi, Kanako Yamamoto, Seiji Masuda, Yohei Matsuda, Kumiko Okada, Tsuyoshi Shibata, Hiroshi Ohta, Akito Yasuhara, Hiroshi Kawamoto, Hideaki Amada, Hiroki Urabe, Rie Nishikawa, Shuhei Kashiwa ASHIWA
  • Patent number: 8450245
    Abstract: The present invention relates to novel heterocyclic alkanol derivatives, to processes for preparing these compounds, to compositions comprising these compounds and to their use as biologically active compounds, in particular for controlling harmful microorganisms in crop protection and in the protection of materials and as plant growth regulators.
    Type: Grant
    Filed: May 27, 2011
    Date of Patent: May 28, 2013
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Carl Friedrich Nising, Hendrik Helmke, Pierre Cristau, Gorka Peris, Tomoki Tsuchiya, Pierre Wasnaire, Jürgen Benting
  • Patent number: 8410023
    Abstract: Compositions and processes for controlling nematodes are described herein, e.g., nematodes that infest plants or animals. The compounds include oxazoles, oxadiazoles and thiadiazoles.
    Type: Grant
    Filed: October 14, 2010
    Date of Patent: April 2, 2013
    Assignee: Monsanto Technology LLC
    Inventors: Urszula Slomczynska, Matt W. Dimmic, William P. Haakenson, Jr., Al Wideman
  • Patent number: 8410150
    Abstract: A CPT inhibitor compound is represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof: or a pharmaceutically acceptable salt thereof. A pharmaceutical composition comprises a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. A method of treating a subject having cancer comprises administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: March 6, 2008
    Date of Patent: April 2, 2013
    Assignee: University Health Network
    Inventors: Heinz W. Pauls, Peter Brent Sampson, Bryan T. Forrest, Radoslaw Laufer, Yong Liu, Miklos Feher, Yi Yao, Guohua Pan
  • Patent number: 8404728
    Abstract: This disclosure relates to materials and methods for inhibiting Botulinum neurotoxin, and more particularly to materials and methods for inhibiting the zinc endopeptidase of Botulinum neurotoxin serotypes A, D and/or E (BoNTA, BoNTD and/or BoNTE).
    Type: Grant
    Filed: July 29, 2010
    Date of Patent: March 26, 2013
    Assignees: Mayo Foundation for Medical Education and Research, U.S. Army Medical Research and Material Command
    Inventors: Yuan-Ping Pang, Jewn Giew Park, Shaohua Wang, Anuradha Vummenthala, Rajesh K Mishra, Jon Davis, Charles B. Millard, James J. Schmidt
  • Publication number: 20130065897
    Abstract: The present invention provides novel compounds of the Formula I, pharmaceutical compositions comprising such compounds and methods for using such compounds as agents or drugs for inhibiting perforin activity and for treating a subject at risk of or susceptible to a disease or disorder, or having a disease or disorder associated with undesirable perforin activity.
    Type: Application
    Filed: December 22, 2010
    Publication date: March 14, 2013
    Applicant: PETER MACCALLUM CANCER INSTITUTE
    Inventors: Julie Ann Spicer, Kristiina Maria Huttunen, Dani Michelle Lyons, Joseph Albert Trapani, Mark John Smyth, William Alexander Denny
  • Patent number: 8394841
    Abstract: The invention provides compounds and pharmaceutical compositions thereof, which are useful for modulating G protein-coupled receptor 120 (GPR120), and methods for using such compounds to treat, ameliorate or prevent a condition associated with abnormal or deregulated GPR120.
    Type: Grant
    Filed: January 8, 2008
    Date of Patent: March 12, 2013
    Assignee: IRM LLC
    Inventors: Robert Epple, Mihai Azimioara, Christopher Cow, Ross Russo, Victor Nikulin, Gerald Lelais
  • Publication number: 20130041157
    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: Application
    Filed: March 31, 2011
    Publication date: February 14, 2013
    Applicant: Toray Industries, Inc.
    Inventors: Nana Hareyama, Satoru Yoshikawa, Kaoru Nakao
  • Publication number: 20130041158
    Abstract: A therapeutic agent or prophylactic agent for Alzheimer's disease has an effect to inhibit or delay the progress of Alzheimer's disease and exhibits a long-lasting therapeutic effect on Alzheimer's disease even when used for a long period of time. The therapeutic agent or prophylactic agent for Alzheimer's disease includes as an effective ingredient a cyclohexane derivative exemplified by the formula below, or a pharmaceutically acceptable salt thereof or a prodrug thereof.
    Type: Application
    Filed: April 28, 2011
    Publication date: February 14, 2013
    Applicant: TORAY INDUSTRIES, INC.
    Inventors: Kaoru Nakao, Yohei Miyamoto, Naohiro Yamada
  • Patent number: 8367844
    Abstract: The present invention relates to heterocyclic compounds of formula I which have microbiocidal activity, in particular fungicidal activity as well as methods of using the compounds of formula (I) to control microbes: wherein A is x-C(R10R11)—C(?O)—, x-C(R12R13)—C(?S)—, x-O—C(?O)—, x-O—C(?S)—, x-N(R14)—C(?O)—, x-N(R15)—C(?S)—, x-C(R16R17)—SO2— or X—N?C(R30)—, in each case x indicates the bond that is connected to R1; T is CR18 or N; Y1, Y2, Y3, and Y4 are independently CR19 or N; Q is O or S; n is 1 or 2; p is 1 or 2, providing that when n is 2, p is 1.
    Type: Grant
    Filed: August 6, 2010
    Date of Patent: February 5, 2013
    Assignee: Syngenta Crop Protection LLC
    Inventors: Sarah Sulzer-Mosse, Clemens Lamberth, Laura Quaranta, Mathias Stephan Respondek
  • Publication number: 20130029966
    Abstract: The invention relates to novel oxindole derivatives of general formula (I), wherein the substituents R1, R2, A, B, and Y are defined as in Claim 1. The invention further relates to medicaments containing said derivatives, and use thereof for the prevention and/or treatment of vasopressin-dependent diseases.
    Type: Application
    Filed: September 23, 2011
    Publication date: January 31, 2013
    Applicant: Abbott GmbH & Co. KG
    Inventors: Thorsten Oost, Wilfried Lubisch, Wilfried Hornberger, Liliane Unger, Herve Geneste, Astrid Netz
  • Patent number: 8362003
    Abstract: The present invention relates to 3-aminopyrrolidine derivatives of the formula I: (wherein R1, R2, R3, R4, R5, R6, R7, R8, X, Y and X are as defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of chemokine receptors and more specifically as a modulator of the CCR2 and/or CCR5 receptor. The compounds and compositions of the invention may bind to chemokine receptors, e.g., the CCR2 and/or CCR5 chemokine receptors, and are useful for treating diseases associated with chemokine, e.g., CCR2 and/or CCR5, activity, such as atherosclerosis, restenosis, lupus, organ transplant rejection and rheumatoid arthritis.
    Type: Grant
    Filed: June 16, 2011
    Date of Patent: January 29, 2013
    Assignee: Incyte Corporation
    Inventors: Chu-Biao Xue, Brian W. Metcalf, Hao Feng, Ganfeng Cao, Taisheng Huang, Changsheng Zheng, Darius J. Robinson, Amy Qi Han
  • Patent number: 8354436
    Abstract: The present invention relates to compounds of the general formula (I), and the pharmaceutically acceptable salt or solvate thereof, as anti-inflammatory and immunomodulatory agents.
    Type: Grant
    Filed: January 27, 2012
    Date of Patent: January 15, 2013
    Assignee: 4SC Discovery GmbH
    Inventors: Johann Leban, Stefan Tasler, Wael Saeb, Carine Chevrier
  • Patent number: 8354410
    Abstract: The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.
    Type: Grant
    Filed: March 9, 2011
    Date of Patent: January 15, 2013
    Assignee: Bristol-Meyers Squibb Company
    Inventors: Kap-Sun Yeung, Katharine A. Grant-Young, John F. Kadow