Chalcogen Bonded Directly To Ring Carbon Of The Oxazole Ring Patents (Class 514/376)
  • Publication number: 20130165485
    Abstract: A compound of formula (I): where A, B, C, G, m, n, o, p, R1, R2, R3, R4, R5, R6, X, R7, R8, R9, R10 and R11 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to processes and intermediates for preparing compounds of formula (I), to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising the compounds of formula (I) and to methods of using the compounds of formula (I) to control insect, acarine, nematode and mollusc pests.
    Type: Application
    Filed: February 20, 2013
    Publication date: June 27, 2013
    Applicant: Syngenta Crop Protection LLC
    Inventors: Jerome Yves Cassayre, Peter Renold, Vladimir Bobosik, Myriem El Qacemi, Anne Jacqueline Dalencon, Werner Zambach, Christopher Richard Godfrey, Thomas Pitterna, Pierre Joseph Jung, Jagadish Pabba
  • Publication number: 20130158083
    Abstract: The invention relates to improvements of the physiochemical and/or the pharmaceutical properties of metaxalone. Disclosed herein are several new cocrystals of metaxalone, including: a 1:1 metaxalone adipic acid cocrystal, a 1:0.5 metaxalone fumaric acid cocrystal, a 1:1 metaxalone salicyclic acid cocrystal, a 1:0.5 metaxalone succinic acid cocrystal, and a 1:0.5 metaxalone maleic acid cocrystal. The therapeutic uses of these metaxalone cocrystals are described as well as therapeutic compositions containing them.
    Type: Application
    Filed: December 22, 2010
    Publication date: June 20, 2013
    Inventors: Joanne Holland, Christopher Frampton, Alan Chorlton, Daniel Gooding
  • Publication number: 20130158036
    Abstract: Described herein are compounds that are antagonists of PGD2 receptors. Also described are pharmaceutical compositions and medicaments that include the compounds described herein that are antagonists of PGD2 receptors. Also described herein are methods of using such antagonists of PGD2 receptors, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other PGD2-dependent or PGD2-mediated conditions or diseases.
    Type: Application
    Filed: November 1, 2012
    Publication date: June 20, 2013
    Applicant: PANMIRA PHARMACEUTICALS, LLC
    Inventor: PANMIRA PHARMACEUTICALS, LLC
  • Patent number: 8466280
    Abstract: The present invention relates to a novel cocrystal compound of 5-chloro-N-({(5S)-2-oxo-3-[4-(3-oxo-4-morpholinyl)phenyl]-1,3-oxazolidin-5-yl}methyl)-2-thiophenecarboxamide (rivaroxaban) and malonic acid, to processes for its preparation, to medicaments comprising this compound and to their use for controlling diseases.
    Type: Grant
    Filed: June 3, 2009
    Date of Patent: June 18, 2013
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Alfons Grunenberg, Karsten Fähnrich, Olaf Queckenberg, Christiane Reute, Birgit Keil, Karen Sue Gushurst, Ezra John Still
  • Publication number: 20130143927
    Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.
    Type: Application
    Filed: June 8, 2012
    Publication date: June 6, 2013
    Applicant: CalciMedica, Inc.
    Inventors: Jeffrey P. WHITTEN, Jonathan GREY, Jianguo CAO, Zhijun WANG, Evan ROGERS
  • Patent number: 8455481
    Abstract: Process for the protection of fish and invertebrates and all their stages of development against or for the treatment of mycoses caused by fungi of the genera Saprolegnia, Aphanomyces, Achlyaflagellata and other species important in aquacultures by use of 2-[[[[1-[3-(1-fluoro-2-phenylethyl)oxy]phenyl]ethylidene]amino]oxy]methyl]alpha-(methoxyimino)-N-methyl-alphaE-benzeneacetamide, amisulbrom, cyazofamid, enestrobin, famoxadone, fenamidone, fluoxastrobin, orysastrobin, picoxystrobin and pyribencarb. This use leads to an inhibition or destruction of pathogenic fungi. The composition, comprising at least one fungicide selected from the abovementioned group for use in fish fanning and keeping is suitable for the prophylaxis and therapy of diseases of fish in aquaculture, in breeding ponds, breeding tanks, aquariums, natural stretches of game fish waters, ponds, and marine fish farms. Addition to the water and feed and direct application are the associated use forms.
    Type: Grant
    Filed: September 14, 2012
    Date of Patent: June 4, 2013
    Assignee: Bayer CropScience AG
    Inventors: Isolde Häuser-Hahn, Klaus Stenzel, Ulrike Wachendorff-Neumann
  • Publication number: 20130131042
    Abstract: Substituted spirocyclic amines of structural formula (I) are selective antagonists of the somatostatin subtype receptor 5 (SSTR5) and are useful for the treatment, control or prevention of disorders responsive to antagonism of SSTR5, such as Type 2 diabetes, insulin resistance, lipid disorders, obesity, atherosclerosis, Metabolic Syndrome, depression, and anxiety.
    Type: Application
    Filed: August 12, 2011
    Publication date: May 23, 2013
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Joseph L. Duffy, Jianming Bao, Debra L. Ondeyka, Sriram Tyagarajan, Patrick Shao, Feng Ye, Revathi Katipally, Aaron Zwicker, Edward C. Sherer, Michael A. Plotkin, Remond Moningka, Zahid Hussain, Harold B. Wood, Feroze Ujjainwalla, F. Anthony Romero, Paul E. Finke, Yi Zang, Weiguo Liu
  • Publication number: 20130123252
    Abstract: The present invention provides a compound of formula I: a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
    Type: Application
    Filed: July 21, 2011
    Publication date: May 16, 2013
    Applicant: NOVARTIS AG
    Inventors: David Barnes, Scott Louis Cohen, Jiping Fu, Lei Shu, Rui Zheng
  • Publication number: 20130121978
    Abstract: Compositions and methods for controlling molluscs, members of the Gastropoda and Bivalvia classes which includes but is not limited to lactones, lactams, carbamates, amides, and/or carboxylic acid containing compounds as active ingredients and/or compounds derived from Pseudomonas and/or Erwinia. Also provided are methods and compositions for increasing the efficacy of chemical and biological control for invasive molluscs in open waters, power plants, and drinking water treatment facilities under coldwater conditions.
    Type: Application
    Filed: December 17, 2012
    Publication date: May 16, 2013
    Applicant: MARRONE BIO INNOVATIONS, INC.
    Inventor: Marrone Bio Innovations, Inc.
  • Publication number: 20130116240
    Abstract: Provided is an agent for the treatment or prophylaxis of inflammatory diseases, allergic diseases, autoimmune diseases, transplant rejection or 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 described in the specification.
    Type: Application
    Filed: September 26, 2012
    Publication date: May 9, 2013
    Applicant: JAPAN TOBACCO INC.
    Inventor: Japan Tobacco Inc.
  • Publication number: 20130102617
    Abstract: Phenylacetamide compounds of the formula having sulfonyl group and cycloalkyl group on the phenyl group and having heteroaryl group on the nitrogen atom in the amide have an excellent glucokinase activation action. The compound of the present invention is useful as an agent for treating diabetes, in particular, type II diabetes, as well as metabolic syndrome and obesity.
    Type: Application
    Filed: April 18, 2012
    Publication date: April 25, 2013
    Applicant: ASTELLAS PHARMA INC.
    Inventors: Masahiko Hayakawa, Yoshiyuki Kido, Takahiro Nigawara, Mitsuaki Okumura, Akira Kanai, Keisuke Maki, Nobuaki Amino
  • Publication number: 20130102604
    Abstract: The present invention relates to a compound of formula (I) as well as pharmaceutically acceptable salt thereof, wherein R1 to R4 have the significance given in claim 1. The compound may be used, for example, for the treatment or prophylaxis of obesity, hyperglycemia, dyslipidemia, and type 1 or type 2 diabetes.
    Type: Application
    Filed: December 10, 2012
    Publication date: April 25, 2013
    Applicant: Hoffmann-La Roche Inc.
    Inventor: Hoffmann-La Roche Inc.
  • Patent number: 8426443
    Abstract: Compounds of formula (I) or a salt thereof are provided: wherein R4, R5, R6, Q, A, Y and R are as defined in the description. Uses of the compounds as medicaments and in the manufacture of medicaments for treating psychotic disorders, cognitive impairments and Alzheimer's Disease are disclosed. The invention further discloses pharmaceutical compositions comprising the compounds.
    Type: Grant
    Filed: August 23, 2012
    Date of Patent: April 23, 2013
    Assignee: Glaxo Group Limited
    Inventors: David Gwyn Cooper, Ian Thomson Forbes, Vincenzo Garzya, Dale James Johnson, Graeme Irvine Stevenson, Paul Adrian Wyman
  • Patent number: 8420680
    Abstract: Provided are compounds, pharmaceutical compositions and methods of treatment or prophylaxis of disorders associated with NMDA receptor activity, including neuropathic pain, stroke, traumatic brain injury, epilepsy, and related neurologic events or neurodegeneration. Compounds are of the general Formula I, or a pharmaceutically acceptable salt, ester, prodrug or derivative thereof are provided: wherein: each (L)k-Ar1 is a substituted or unsubstituted, mono or bicyclic aryl or heteroaryl; W is a bond, alkyl, or alkenyl; X is a bond, NR1 or O and each R1 and R2 is independently H, alkyl, alkenyl or aralkyl or R1 and R2 taken together form a 5-8 membered ring; R3?R6 are selected from certain specific substituents or a carbonyl; Y is a bond, O, S, SO, SO2, CH2, NH, N(alkyl), or NHC(?O); and Z is OH, NR6R7, NR8SO2(alkyl), NR8C(O)NR6R7, NR8C(O)O(alkyl), NR8-dihydrothiazole, or NR8-dihydroimidazole or wherein Z can fuse with Ar2 to form selected heterocycles.
    Type: Grant
    Filed: June 30, 2008
    Date of Patent: April 16, 2013
    Assignees: Emory University, NeurOp, Inc.
    Inventors: Dennis C. Liotta, James P. Snyder, Stephen F. Traynelis, Lawrence Wilson, Cara Mosley, Raymond J. Dingledine, Yesim Altas Tahirovic, Scott J. Myers
  • Publication number: 20130085132
    Abstract: The present invention provides a pyrazole compound of the following general Formula [Ib] having SGLT1 inhibitory activity, or a pharmaceutically acceptable salt thereof, a pharmaceutical composition comprising the same, and its pharmaceutical use: wherein each symbol is the same as defined in the description.
    Type: Application
    Filed: August 30, 2012
    Publication date: April 4, 2013
    Applicant: JAPAN TOBACCO INC.
    Inventors: Tomoya MIURA, Yosuke OGOSHI, Kazuhito UEYAMA, Dai MOTODA, Toshihiko IWAYAMA, Koichi SUZAWA, Hironobu NAGAMORI, Hiroshi UENO, Akihiko TAKAHASHI, Kazuyuki SUGIMOTO
  • Publication number: 20130072490
    Abstract: Described herein are compounds that are antagonists of lysophosphatidic receptor(s). Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists, alone and in combination with other compounds, for treating LPA-dependent or LPA-mediated conditions or diseases.
    Type: Application
    Filed: September 29, 2010
    Publication date: March 21, 2013
    Applicant: Amira Pharmaceuticals INC.
    Inventors: Ryan Clark, Brian Andrew Stearns, Jill Melissa Scott, Heather Renee Coate, Lucy Zhao, Thomas Jon Seiders, Deborah Volkots, Jeannie Arruda, Nicholas Simon Stock, Yen Pham Truong, David Nathan Zalatan
  • Publication number: 20130065885
    Abstract: The present invention relates generally to therapeutic formulations. More particularly, this present invention provides an oral delivery system for a therapeutic compound that is a base, a salt of a base or an amphoteric compound or a salt of a amphoteric compound with pharmacological, physiological or biochemical activity or a proactive form thereof. The present invention even more particularly provides a swallow formulation comprising a therapeutic compound that is a base, a salt of a base, an amphoteric compound or a salt of an amphoteric compound which facilitates the rapid delivery of the therapeutic compound to the circulatory system.
    Type: Application
    Filed: September 14, 2012
    Publication date: March 14, 2013
    Applicant: IMAGINOT PTY LTD.
    Inventors: Michael Stephen Roberts, Ruoying Jiang, Keivan Bezanehtak, Greg Andrew Davey, George Alexander Davidson, Geraldine Ann Elliott, Stephen Douglas Chandler, Mantu Sarkar
  • Patent number: 8394788
    Abstract: Provided herein are small molecule compounds that alter the transport activity of solute transporters, particularly urea transporters. The compounds described herein belong to the phenylsulfoxyoxazole, phenylsulfoxyimidazole, phenylsulfoxythiazole class of compounds. The compounds described herein are useful for increasing solute clearance in states of fluid overload and for treating cardiovascular, renal, and metabolic diseases, disorders, and conditions. Methods for identifying and using these agents that inhibit urea transporters are described herein.
    Type: Grant
    Filed: November 16, 2007
    Date of Patent: March 12, 2013
    Assignee: The Regents of the University of California
    Inventors: Alan S. Verkman, Marc Harris Levin
  • Publication number: 20130059821
    Abstract: Compounds that have agonist activity at one or more of the SIP receptors are provided. The compounds are sphingosine analogs that, after phosphorylation, can behave as agonists at SIP receptors.
    Type: Application
    Filed: September 10, 2012
    Publication date: March 7, 2013
    Inventors: Richard D. Caldwell, Kevin M. Guckian, Gnanasambandam Kumaravel, Wen-Cherng Lee, Edward Yin-Shiang Lin, Xiaogao Liu, Bin Ma, Daniel M. Scott, Zhan Shi, Jermaine Thomas, Arthur G. Taveras, Guo Zhu Zheng
  • Patent number: 8383622
    Abstract: Disclosed is a compound which is useful as an 11?-hydroxysteroid dehydrogenase type 1 inhibitor. A compound represented by the formula: its pharmaceutically acceptable salt, or a solvate thereof, wherein Ring A is a group represented by the formula: Ring B is optionally substituted heteroaryl, provided that optionally substituted isoxazole is excluded, or optionally substituted heterocycle, R1 is hydrogen or optionally substituted alkyl, R2 is —OR5, —SR5, halogen, halogenated alkyl or the like, R3 is optionally substituted alkyl or the like, R4 is optionally substituted alkyl or the like, R5 is optionally substituted alkyl or the like, R6 is hydrogen or the like, R7 and R8 are each independently hydrogen or the like, R10 and R11 are each independently hydrogen or the like, R12 is optionally substituted alkyl or the like, m and p are each independently integer of 1 to 3.
    Type: Grant
    Filed: May 7, 2008
    Date of Patent: February 26, 2013
    Assignee: Shionogi & Co., Ltd.
    Inventors: Koji Masuda, Tomoyuki Ogawa, Takuji Nakatani
  • Publication number: 20130045194
    Abstract: Disclosed are compositions and methods for treating conditions characterized by low HDL-CE which can lead to decreased delivery of cholesteryl ester to steroidogenic tissues, reducing the organ's ability to produce steroids especially during periods of demand, stress and or systemic inflammatory response syndrome.
    Type: Application
    Filed: May 6, 2011
    Publication date: February 21, 2013
    Applicant: ALPHACORE PHARMA, LLC
    Inventors: Bruce J. Auerbach, Reynold Homan, Brian R. Krause
  • Publication number: 20130045967
    Abstract: The application describes an assay for the identification of small molecule modulators of integrin CD11b/CD18 and small molecules capable of modulating activity of this receptor. Such compounds may be used in certain embodiments for treating a disease or condition selected from inflammation, immune-related disorders, cancer, ischemia-reperfusion injury, stroke, neointimal thickening associated with vascular injury, bullous pemphigoid, neonatal obstructive nephropathy, and cardiovascular disease, or in other embodiments for the treatment of a disease or condition selected from immune deficiency, acquired immune deficiency syndrome (AIDS), myeloperoxidase deficiency, Wiskott-Aldrich syndrome, chronic granulomatous disease, hyper-IgM syndromes, leukocyte adhesion deficiency, Chediak-Higashi syndrome, and severe combined immunodeficiency.
    Type: Application
    Filed: September 13, 2012
    Publication date: February 21, 2013
    Inventors: Vineet Gupta, M. Amin Arnaout
  • Publication number: 20130040977
    Abstract: This technology relates generally to compounds and methods for stimulating neurogenesis (e.g., post-natal neurogenesis, including post-natal hippocampal and hypothalamic neurogenesis) and/or protecting neuronal cell from cell death. Various compounds are disclosed herein. In vivo activity tests suggest that these compounds may have therapeutic benefits in neuropsychiatric and/or neurodegenerative diseases such as schizophrenia, major depression, bipolar disorder, normal aging, epilepsy, traumatic brain injury, post-traumatic stress disorder, Parkinson's disease, Alzheimer's disease, Down syndrome, spinocerebellar ataxia, amyotrophic lateral sclerosis, Huntington's disease, stroke, radiation therapy, chronic stress, abuse of a neuro-active drug, retinal degeneration, spinal cord injury, peripheral nerve injury, physiological weight loss associated with various conditions, as well as cognitive decline associated with normal aging, chemotherapy, and the like.
    Type: Application
    Filed: August 24, 2012
    Publication date: February 14, 2013
    Inventors: Steven L. McKnight, Andrew A. Pieper, Joseph M. Ready, Jef K. De Brabander
  • Publication number: 20130030000
    Abstract: The present invention is directed to a composition useful for the treatment of a FAAH mediated disease, disorder or conditions comprising a FAAH inhibitor and a second activation, comprising a selected imidazole or oxazole FAAH inhibitor and a second active agent. The compositions will be useful in the treatment of a wide range of disease, disorder, or conditions including osteoarthritis, rheumatoid arthritis, diabetic neuropathy, postherpetic neuralgia, skeletomuscular pain, and fibromyalgia, as well as acute pain, migraine, sleep disorder, Alzheimer disease, and Parkinson's disease. In another aspect the invention discloses herein is directed to compositions useful in the treatment of neuropathic and nociceptive pain, said compositions comprising etoricoxib.
    Type: Application
    Filed: January 25, 2011
    Publication date: January 31, 2013
    Inventors: Harry R. Chobanian, Linus S. Lin, Ping Liu, Marc D. Chioda, Robert J. DeVita, Ravi P. Nargund, Yan Guo, Terence G. Hamill, Wenping Li, Darrell Arthur Henze
  • Publication number: 20130029970
    Abstract: The present disclosure relates to compounds of formula I useful as agonists of cannabinoid receptors. The disclosure also provides pharmaceutically acceptable compositions comprising the compounds of the disclosure and methods of using the compositions in the treatment of various disorders.
    Type: Application
    Filed: July 9, 2010
    Publication date: January 31, 2013
    Applicant: IRONWOOD PHARMACEUTICALS, INC
    Inventors: Kevin Sprott, Jason Rohde, Takashi Nakai, Bo Peng, John Jeffrey Talley
  • Publication number: 20130028966
    Abstract: The invention provides compounds represented by the formulae: (I) and (II) where the compounds are useful in treating, for example, viral and/or parasitic infections. Also provided are pharmaceutical compositions comprising the compounds and methods of treatment using the compounds.
    Type: Application
    Filed: April 13, 2011
    Publication date: January 31, 2013
    Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
    Inventors: Benhur Lee, Michael E. Jung, Jihye Lee, Frederic Vigant, Peter J. Bradley, Michael C. Wolf, Bettina E. Hajagos
  • Publication number: 20130018048
    Abstract: The present invention is directed to certain Oxazole derivatives which are useful as modulators of Fatty Acid Amide Hydrolase (FAAH) and as FAAH imaging agents. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including osteoarthritis, rheumatoid arthritis, diabetic neuropathy, postherpetic neuralgia, skeletomuscular pain, and fibromyalgia, as well as acute pain, migraine, sleep disorder, Alzheimer Disease, and Parkinson's Disease.
    Type: Application
    Filed: April 4, 2011
    Publication date: January 17, 2013
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: ZhiQiang Yang, Philippe G. Nantermet, Constantine Kreatsoulas, Keith P. Moore, Evan Foster Shalen
  • Publication number: 20130012526
    Abstract: The present invention is directed to certain Oxazole derivatives which are useful as modulators of Fatty Acid Amide Hydrolase (FAAH) and as FAAH imaging agents. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including osteoarthritis, rheumatoid arthritis, diabetic neuropathy, postherpetic neuralgia, skeletomuscular pain, and fibromyalgia, as well as acute pain, migraine, sleep disorder, Alzheimer Disease, and Parkinson's Disease.
    Type: Application
    Filed: April 18, 2011
    Publication date: January 10, 2013
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Philippe G. Nantermet, Zhi-Qiang Yang, Constantine Kreatsoulas, Abbas M. Walji, Hong Zhu
  • Publication number: 20130012554
    Abstract: The present invention relates to oxazolidinone derivatives containing new bicyclic group, having antibacterial activity, or a pharmaceutically acceptable salt thereof, a method for preparing the same, an antibacterial composition comprising the oxazolidinone derivative or a pharmaceutically acceptable salt thereof as an active ingredient, and a method for treating an infectious disease caused by pathogen using the same. The oxazolidinone derivative or a pharmaceutically acceptable salt thereof may exhibit excellent antibacterial activity against gram positive bacteria including various resistant strains.
    Type: Application
    Filed: December 8, 2011
    Publication date: January 10, 2013
    Applicant: Korean Institute of Science and Technology
    Inventors: Gyo-Chang KEUM, Eunice Eun-Kyeong Kim, Ae-Nim Pae, Kyung-II Choi, Soon-Bang Kang, Seon-Hee Seo, Deepak Bhattaral, Ju-Hyeon Lee
  • Publication number: 20130004444
    Abstract: The present invention relates to a composition including at least one C7 sugar, or derivative from esterification of said sugar, and a pharmaceutically acceptable carrier for treating alopecia. The present invention also relates to a method for cosmetically treating hair and nails, said method being intended to stimulate the growth thereof and/or slow the loss thereof. According to said method, a cosmetic composition including at least one C7 sugar, or derivative from esterification of said sugar, is administered. The present invention finally relates to a method for cosmetic care of hair and/or eyelashes and/or nails.
    Type: Application
    Filed: December 15, 2010
    Publication date: January 3, 2013
    Inventors: Caroline Baudouin, Philippe Msika
  • Publication number: 20130005701
    Abstract: The invention relates to the field of blood coagulation. Novel oxazolidinone derivatives of the general formula (I) processes for their preparation and their use as medicinally active compounds for the prophylaxis and/or treatment of disorders are described.
    Type: Application
    Filed: January 27, 2012
    Publication date: January 3, 2013
    Applicant: Bayer Pharma Aktiengesellschaft
    Inventors: Alexander Straub, Thomas Lampe, Jens Pohlmann, Susanne Röhrig, Elisabeth Perzborn, Karl-Heinz Schlemmer, Joseph Pernerstorfer
  • Publication number: 20120329799
    Abstract: The present invention provides a composition having an excellent controlling activity on plant disease. The composition comprising the compound represented by the formula (1) and one or more carboxamide fungicidal compound selected from the group (A) shows an excellent controlling activity on a plant disease. Group (A): a group consisting of thifluzamide, oxadixyl, pencycuron, benalaxyl-M, fenhexamid, furametpyr, isopyrazam, isotianil, mepronil, tecloftalam, boscalid, fluopyram, fluopicolide, carpropamid, diclocymet, mandipropamid, dimethomorph, flumorph, penthiopyrad, and bixafen.
    Type: Application
    Filed: March 2, 2011
    Publication date: December 27, 2012
    Applicant: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventors: So Kiguchi, Soichi Tanaka, Mayuko Ozawa, Atsushi Iwata
  • Publication number: 20120328569
    Abstract: Disclosed are compounds of formula (I) that are used as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.
    Type: Application
    Filed: March 2, 2011
    Publication date: December 27, 2012
    Inventors: Casey Cameron McComas, Nigel J. Liverton, Richard Soll, Peng Li, Xuanjia Peng, Hao Wu, Frank Narjes, Joerg Habermann, Uwe Koch, Shilan Liu
  • Publication number: 20120316157
    Abstract: The present invention provides a composition having an excellent controlling activity on plant disease. The composition comprising the compound represented by the formula (1) and one or more heterocyclic fungicidal compound selected from the group (A) shows an excellent controlling activity on a plant disease.
    Type: Application
    Filed: March 2, 2011
    Publication date: December 13, 2012
    Applicant: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventors: So Kiguchi, Soichi Tanaka, Mayuko Ozawa, Atsushi Iwata
  • Patent number: 8329706
    Abstract: The present invention relates to oxazolidinone derivatives of formula (I) wherein Y, R3 and R4 are as described in the description, to their preparation, to pharmaceutically acceptable salts thereof, and to their use as pharmaceuticals, to pharmaceutical compositions containing one or more compounds of formula (I), and especially to their use as orexin receptor antagonists.
    Type: Grant
    Filed: May 11, 2010
    Date of Patent: December 11, 2012
    Assignee: Actelion Pharmaceuticals Ltd.
    Inventors: Hamed Aissaoui, Christoph Boss, Christine Brotschi, Markus Gude, Romain Siegrist, Thierry Sifferlen, Jodi T Williams
  • Publication number: 20120301439
    Abstract: Methods of treatment of diseases that include or are characterized by inappropriate or pathological neovascularization are disclosed. These diseases include diseases of the eye, such as diabetic retinopathy, retinopathy of prematurity, and choroidal neovascularization which can occur in age-related macular degeneration (AMD). Disclosed methods include administering agents that cause directly or indirectly upregulation of the ABCA1 transporter protein in macrophages. These agents include, without limitation, LXR agonists. In some embodiments, inhibitors of CETP expression or activity can also be effective. Administration routes can include, without limitation, intraocular, periocular, or systemic administration.
    Type: Application
    Filed: May 24, 2012
    Publication date: November 29, 2012
    Applicant: WASHINGTON UNIVERSITY
    Inventor: Rajendra S. Apte
  • Publication number: 20120302607
    Abstract: The invention provides a series of C4-substituted oxazole compounds having an alpha keto side chain at the 2 position, for example, compounds of formula I. The compounds can inhibit fatty acid amide hydrolase and can be useful for treatment of malconditions modulated by fatty acid amide hydrolase. The invention further provides methods of making compounds of formula I, useful intermediates in the preparation of compounds of formula I, and methods of using compounds of formula 1 and compositions thereof.
    Type: Application
    Filed: August 2, 2012
    Publication date: November 29, 2012
    Applicant: The Scripps Research Institute
    Inventor: Dale L. Boger
  • Publication number: 20120283264
    Abstract: The disclosure generally relates to compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds are ligands, agonists and partial agonists for the mGluR5 receptor and may be useful for the treatment of various disorders of the central nervous system.
    Type: Application
    Filed: November 2, 2011
    Publication date: November 8, 2012
    Inventors: Andrew P. Degnan, Hong Huang, Lawrence B. Snyder, Fukang Yang, Kevin W. Gillman, Michael F. Parker
  • Publication number: 20120277235
    Abstract: A composition comprising at least one physiologically tolerated film forming agent, at least one physiologically tolerated solvent, at least one plasticizer and a compound of the formula I or a stereoisomeric form or a physiologically tolerated salt of any of the foregoing. The composition is suitable for treatment of androgenic alopecia or hirsutism, that is, for avoiding undesirable hair growth, and for treatment of seborrhea and acne, and can furthermore be employed in cosmetics.
    Type: Application
    Filed: March 30, 2012
    Publication date: November 1, 2012
    Inventors: Karl Theodor Kraemer, Manfred Bohn
  • Publication number: 20120270818
    Abstract: This invention provides methods for treating a subject afflicted with cancer, comprising concurrently administering (i) an HDAC 6-selective inhibitor and (ii) a suitable cytotoxic agent such as SAHA, doxorubicin or etoposide. This invention also provides methods for inducing the death of a transformed cell such as a cancer cell, comprising concurrently contacting the cell with (i) an HDAC 6-selective inhibitor and (ii) a suitable cytotoxic agent such as SAHA, doxorubicin or etoposide.
    Type: Application
    Filed: July 2, 2010
    Publication date: October 25, 2012
    Inventors: Paul A. Marks, Weisheng Xu, Mandana Namdar
  • Publication number: 20120263760
    Abstract: The present invention relates to methods for producing particles of metaxalone using dry milling processes as well as compositions comprising metaxalone, medicaments produced using metaxalone in particulate form and/or compositions, and to methods of treatment of an animal, including man, using a therapeutically effective amount of metaxalone administered by way of said medicaments.
    Type: Application
    Filed: April 23, 2010
    Publication date: October 18, 2012
    Inventors: Aaron Dodd, Felix Meiser, Marck Norret, Adrian Russell, H. William Bosch
  • Patent number: 8278328
    Abstract: Compounds of formula (I) or a salt thereof are provided: wherein R4, R5, R6, Q, A, Y and R are as defined in the description. Uses of the compounds as medicaments and in the manufacture of medicaments for treating psychotic disorders, cognitive impairments and Alzheimer's Disease are disclosed. The invention further discloses pharmaceutical compositions comprising the compounds.
    Type: Grant
    Filed: September 18, 2008
    Date of Patent: October 2, 2012
    Assignee: Glaxo Group Limited
    Inventors: David Gwyn Cooper, Ian Thomson Forbes, Vincenzo Garzya, Dale James Johnson, Graeme Irvine Stevenson, Paul Adrian Wyman
  • Publication number: 20120245191
    Abstract: The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5 and A are as described herein, compositions including the compounds and methods of using the compounds.
    Type: Application
    Filed: March 19, 2012
    Publication date: September 27, 2012
    Inventors: Daniel Hunziker, Werner Neidhart
  • Publication number: 20120238607
    Abstract: The present application relates to new, substituted 2-acetamido-5-aryl-1,2,4-triazolones, to processes for preparing them, to their use alone or in combinations for the treatment and/or prevention of diseases and also to their use for the production of medicaments for the treatment and/or prevention of diseases, more particularly for the treatment and/or prevention of cardiovascular disorders.
    Type: Application
    Filed: March 21, 2012
    Publication date: September 20, 2012
    Applicant: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Ulf BRÜGGEMEIER, Chantal FÜRSTNER, Volker GEISS, Joerg KELDENICH, Armin KERN, Martina DELBECK, Peter KOLKHOF, Axel KRETSCHMER, Elisabeth POOK, Carsten SCHMECK, Hubert TRÜBEL
  • Patent number: 8263624
    Abstract: The invention relates to aryl-substituted heterocycles, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular of thromboembolic disorders.
    Type: Grant
    Filed: May 25, 2007
    Date of Patent: September 11, 2012
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Michael Härter, Tobias Wunberg, Swen Allerheiligen, Marcus Bauser, Ulrich Rester, Stefan Heitmeier
  • Publication number: 20120220622
    Abstract: The present invention relates to a heterocyclic derivative of formula (I) wherein the variables are as defined in the specification, or to a pharmaceutically acceptable salt or solvate thereof. The present invention further relates to pharmaceutical compositions comprising said heterocyclic derivatives and to their use in therapy, for instance in the treatment or prevention of disorders mediated by glutamate dysfunction, such as schizophrenia and generalised anxiety disorder.
    Type: Application
    Filed: November 2, 2010
    Publication date: August 30, 2012
    Inventors: Julia Adam, Jonathan Gillespie, Steven Laats, John Kinnaird Ferguson MacLean, Duncan Robert McArthur
  • Publication number: 20120207826
    Abstract: There is disclosed herein a composition for treating extracellular parasitic infections, the composition comprising one or more of the following combinations: at least one quinolone or fluoroquinolone together with at least one tetracycline, iodoquinol, an azole or imidazole; or at least two agents selected from the group consisting of iodoquinol, thiazolidones, tetracycline, nitroimidazoles, cotrimoxazole and diloxanide furoate.
    Type: Application
    Filed: October 22, 2010
    Publication date: August 16, 2012
    Inventors: Thomas Julius Borody, Soledad Carsula
  • Publication number: 20120208857
    Abstract: The present invention relates to pharmaceutical compositions useful for administration for treating, preventing, or reducing the risk of microbial infections.
    Type: Application
    Filed: October 12, 2010
    Publication date: August 16, 2012
    Inventors: Eric S. Burak, Danping Li
  • Publication number: 20120202694
    Abstract: The present invention relates to methods for producing particles of a biologically active material using dry milling processes as well as compositions comprising such materials, medicaments produced using said biologically active materials in particulate form and/or compositions, and to methods of treatment of an animal, including man, using a therapeutically effective amount of said biologically active materials administered by way of said medicaments.
    Type: Application
    Filed: April 23, 2010
    Publication date: August 9, 2012
    Inventors: Aaron Dodd, Felix Meiser, Marck Norret, Adrian Russell, H William Bosch
  • Publication number: 20120202777
    Abstract: The present invention is directed to a new class of hydroxamic acid derivatives of Formula I, wherein the variables G, T, D, L, A, X, R1 and R2 are as described hereinabove, and their use as LpxC inhibitors, and more specifically their use to treat bacterial infections.
    Type: Application
    Filed: October 4, 2010
    Publication date: August 9, 2012
    Inventors: Matthew Frank Brown, Anthony Marfat, Michael Joseph Melnick, Usa Reilly