Chalcogen Bonded Directly To Ring Carbon Of The Five-membered Hetero Ring Patents (Class 514/418)
  • Publication number: 20110195109
    Abstract: Provided is a patch 1 containing a backing layer 2 and a pressure-sensitive adhesive layer 3 formed on the backing layer 2, where the pressure-sensitive adhesive layer 3 contains (i) ropinirole and a metal salt produced by the reaction of a ropinirole acid adduct and a metal ion containing desalting agent in an equivalent mole or less to the acid adduct and (ii) an adhesive base free of a hydroxyl group and a carboxy group.
    Type: Application
    Filed: February 9, 2009
    Publication date: August 11, 2011
    Applicant: HISAMITSU PHARMACEUTICAL CO., INC.
    Inventors: Yasunari Michinaka, Yuka Ansai
  • Publication number: 20110189308
    Abstract: The disclosure provides that components of a PTEN cell signaling pathway may be utilized as therapeutic targets for treating, preventing, slowing the progression of or delaying the onset of a neurodegenerative disease or disorder. Such components that may be targeted include, phosphatase and tensin homologue (PTEN), glycogen synthase kinase 3 beta (GSK3?), and AKT. The subject matter disclosed herein relates to the therapeutic use of inhibitors of PTEN, inhibitors of GSK3?, or activators of AKT to treat a neurodegenerative disease or disorder in a subject. Compounds are disclosed which may be used in the methods provided.
    Type: Application
    Filed: March 17, 2009
    Publication date: August 4, 2011
    Inventors: Asa Abeliovich, Keiichi Inoue
  • Publication number: 20110190294
    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, R4, R5 and R6 are as defined in the specification.
    Type: Application
    Filed: April 16, 2009
    Publication date: August 4, 2011
    Inventors: Patrik Rhönnstad, Elisabet Kallin, Theresa Apelqvist, Mattias Wennerstål, Aiping Cheng
  • Publication number: 20110178125
    Abstract: This invention is directed to indolone derivatives which are antagonists for the GALR3 receptor. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a pharmaceutical composition made by combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier.
    Type: Application
    Filed: January 10, 2011
    Publication date: July 21, 2011
    Inventors: Michael Konkel, John M. Werzel, Jamie Talisman
  • Patent number: 7981880
    Abstract: The present invention encompasses compounds of general formula (1) wherein R1, R2, R3 and X are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the use thereof for preparing a pharmaceutical composition having the above-mentioned properties.
    Type: Grant
    Filed: April 23, 2007
    Date of Patent: July 19, 2011
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Matthias Treu, Andreas Mantoulidis, Ulrike Tontsch-Grunt
  • Publication number: 20110172244
    Abstract: The invention provides compounds, of Formula I: pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of GPR119.
    Type: Application
    Filed: February 20, 2009
    Publication date: July 14, 2011
    Applicant: IRM LLC
    Inventors: Phillip B. Alper, Robert Epple, Pierre-Yves Michellys, Daniel Mutnick, Victor Nikulin
  • Publication number: 20110160130
    Abstract: Invented is a method of treating cancer and pre-cancerous syndromes in a mammal, including a human, in need thereof which comprises the administration of a therapeutically effective amount of a combination of a non-peptide TPO receptor agonist or a peptide TPO mimetic and a cell cycle signalling inhibitor compound to such mammal.
    Type: Application
    Filed: August 2, 2010
    Publication date: June 30, 2011
    Inventor: Connie ERICKSON-MILLER
  • Publication number: 20110159066
    Abstract: Methods for restoring normal patterns of activity in a subject suffering from Parkinson's Disease are disclosed that include administering an effective steady state concentration of a dopamine modulating compound continuously for a prolonged period of time such that normal patterns of activity are substantially restored in the subject.
    Type: Application
    Filed: November 2, 2010
    Publication date: June 30, 2011
    Inventors: Terri B. Sebree, Steven J. Siegel
  • Patent number: 7968730
    Abstract: The invention relates in a first embodiment to a method for the manufacture of esters of the formula I, or especially of amides of the formula II, wherein the symbols have the meanings given in the specification, as well as other intermediates and compounds useful in the synthesis of tryptamines and other substances mentioned in the title. The synthesis methods and intermediates are useful in the synthesis of pharmaceuticals.
    Type: Grant
    Filed: December 7, 2009
    Date of Patent: June 28, 2011
    Assignee: BASF SE
    Inventors: Ulrich Berens, Oliver Dosenbach, Daniel Sprenger
  • Publication number: 20110135594
    Abstract: A compound of general Formula (I) having histone deacetylase (HDAC) and/or CDK inhibitory activity, a pharmaceutical composition comprising the compound, and a method useful to treat diseases using the compound.
    Type: Application
    Filed: July 14, 2009
    Publication date: June 9, 2011
    Inventors: Michael Graupe, Chandrasekar Venkataramani
  • Patent number: 7956081
    Abstract: A low salt protein solution not capable of forming a gel is obtained from animal muscle tissue by forming an aqueous acidic protein solution which is filtered to remove salt and acid. The low salt protein solution can be formed into a gel by adding a physiologically acceptable salt to the low salt protein solution and heating the resultant protein solution with added salt.
    Type: Grant
    Filed: October 26, 2007
    Date of Patent: June 7, 2011
    Assignee: Proteus Industries, Inc.
    Inventor: Stephen D. Kelleher
  • Publication number: 20110130437
    Abstract: The present invention relates to salt forms of the compound 4-[(Z)-[[4-[(dimethylaminoJmethyllphenyllaminolCe-fluoro-1,2-dihydro2-oxo-3H-indol-3-ylidene)methyl]-benzenepropanoic acid which are suitable for pharmaceutical development and to a process for their manufacture.
    Type: Application
    Filed: January 22, 2009
    Publication date: June 2, 2011
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Ulrike Werthmann, Christian Kulinna, Waldemar Pfrengle, Werner Rall
  • Publication number: 20110130361
    Abstract: The present invention relates to a novel class of Silicon derivatives. The Silicon compounds can be used to treat cancer. The Silicon compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.
    Type: Application
    Filed: August 5, 2008
    Publication date: June 2, 2011
    Inventors: Jonathan Grimm, Richard W. Heidebrecht, JR., Dawn M. Mampreian, Joey L. Methot, Thomas A. Miller, Karin M. Otte, Scott Peterson, Phieng Siliphaivanh, Kevin J. Wilson, David J. Witter
  • Publication number: 20110110891
    Abstract: The present disclosure provides methods of treating a hepatitis C virus infection. The methods generally involve administering to an individual in need thereof an effective amount of an active agent that inhibits a RAS-RAF-MEK-ERK signal transduction pathway.
    Type: Application
    Filed: May 11, 2009
    Publication date: May 12, 2011
    Inventors: Melanie Ott, Eva Herker
  • Publication number: 20110098333
    Abstract: The invention is directed to methods of treating organ specific infections in a host organism by administering compounds that target host receptors and/or host cellular signaling molecules to prevent a pathogen from infecting the organ. For example, the administration of a compound to prevent a pathogen from crossing the blood-brain barrier to prevent a brain infection.
    Type: Application
    Filed: June 12, 2009
    Publication date: April 28, 2011
    Applicant: The Johns Hopkins University
    Inventor: Kwang Sik Kim
  • Publication number: 20110098253
    Abstract: The invention also provides methods for treating inflammation, pain and fever; for treating gastrointestinal disorders; for facilitating wound healing; for treating and/or preventing gastrointestinal, renal and/or respiratory toxicities resulting from the use of nonsteroidal antiinflammatory compounds; for treating inflammatory disease states and/or disorders; and for treating and/or preventing ophthalmic diseases and/or disorders comprising administration of novel compositions comprising at least one nitrosated NSAID, and, optionally, at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one therapeutic agent.
    Type: Application
    Filed: December 28, 2010
    Publication date: April 28, 2011
    Applicant: Nicox S.A.
    Inventors: Richard Earl, Maiko Ezawa, Xinquin Fang, David S. Garvey, Ricky D. Gaston, Subhash P. Khanapure, L. Gordon Letts, Chia-En Lin, Ramani R. Ranatunge, Stewart K. Richardson, Joseph D. Schroeder, Cheri A. Stevenson, Shiow-Jyi Wey
  • Patent number: 7927624
    Abstract: An oral dosage form comprising a pharmaceutical tablet of one or more layers, one of which carries a biologically active substance; the formulation of said tablet includes different percentages of hydrophilic and lipophilic polymeric materials, and adjuvant substances. The tablets of the present invention show a release rate which is independent from the amounts of active substance present in the tablet.
    Type: Grant
    Filed: March 12, 2007
    Date of Patent: April 19, 2011
    Assignee: Jagotec AG
    Inventors: Guy Vergnault, Pascal Grenier, Lauretta Maggi, Ubaldo Conte
  • Publication number: 20110086088
    Abstract: Compositions useful for treatment of a wide range of skin disorders including: pre-cancerous lesions, keratotic lesions, superficial basal cell carcinomae; squamous cell carcinomae; malignant melanoma, and radiation-induced burns. In some embodiments the treatments comprise contacting human or other mammalian skin with a composition according to the disclosure. In other embodiments, administration of compositions provided is by injection. Some embodiments provide for preventive use of compositions provided towards preventing some forms of skin cancer and skin cancer-related disorders by repeated application to healthy-looking skin. Methods for providing the compositions are disclosed.
    Type: Application
    Filed: March 19, 2010
    Publication date: April 14, 2011
    Inventor: Don Wayne Berry
  • Publication number: 20110071195
    Abstract: The present invention provides compounds of formula (I), as well as pharmaceutical acceptable salt thereof, wherein R1 to R7 have the significance given herein. The compounds are useful in the treatment of prophylaxis of diseases that are related to AMPK regulation.
    Type: Application
    Filed: September 14, 2010
    Publication date: March 24, 2011
    Inventors: Li Chen, Lichun Feng, Mengwei Huang, Jia Li, Fajung Nan, Tao Pang, Lifang Yu, Mei Zhang
  • Publication number: 20110071132
    Abstract: The invention relates to novel oxindol derivative of general formula (I), wherein substituents R1, R2, A, B and Y are such as defined in a claim 1. Drugs containing said derivatives and the use thereof for preventing and/or treating vassopress- and/or oxytocin-dependent-diseases are also disclosed.
    Type: Application
    Filed: July 30, 2010
    Publication date: March 24, 2011
    Applicant: Abbott GmbH & Co. KG
    Inventors: Thorsten Oost, Wilfried Lubisch, Wolfgang Wernet, Andrea Hager-Wernet, Wilfried Hornberger, Liliane Unger
  • Publication number: 20110065768
    Abstract: This invention provides non-steroidal compounds with affinity for the androgen receptor and utility for androgen-receptor related treatments, having a structure according to the formula or a salt or hydrate form thereof.
    Type: Application
    Filed: September 3, 2010
    Publication date: March 17, 2011
    Inventors: PEDRO HAROLD HAN HERMKENS, HERMAN THIJS STOCK, JAAP VAN DER LOUW, NEELTJE MIRANDA TEERHUIS, JOHANNES PETRUS MARIA LOMMERSE
  • Publication number: 20110008258
    Abstract: Methods for treating breathing disorders by inhibition of the induced PGE2 pathway in a mammalian subject, methods for assessing apnea, hypoxic ischemic encephalopathy or perinatal asphyxia by detecting an elevated level of PGE2, or a metabolite thereof, in a sample from the subject compared with a control level, and in vitro and in vivo screening methods for medicaments for treating breathing disorders are disclosed.
    Type: Application
    Filed: November 12, 2008
    Publication date: January 13, 2011
    Applicant: SAMSARA MEDICIN AB
    Inventors: Eric Herlenius, Per-Johan Jakobsson, Annika Hofstetter Olsson
  • Publication number: 20110009428
    Abstract: The compounds of the subject invention have a structure according to formula I: wherein X is S or SO2; R1 is (1C-6C)alkyl, (3C-6C)alkenyl, or (3C-6C)alkynyl, each optionally substituted with (3C-6C)cycloalkyl, OH, OC(O)(1C-4C)alkyl, (1C-4C)alkoxy, halogen, cyano, formyl, C(O)(1C-4C)alkyl, CO2H, CO2(1C-4C)alkyl, C(O)NR5R6, S(O)(1C-4C)alkyl or S(O)2(1C-4C)alkyl; R2 is hydrogen, (1C-4C)alkyl or C(O)(1C-4C)alkyl; R3 is a phenyl group optionally substituted with (1C-4C)alkyl, (1C-4C)fluoroalkyl, (1C-4C)alkoxy, (1C-4C)fluoroalkoxy, halogen, cyano or nitro; or R3 is a 5- or 6-membered aromatic heterocyclic ring structure optionally substituted with (1C-4C)alkyl, (1C-4C)fluoroalkyl, (1C-4C)alkoxy, halogen or cyano; R4 is a phenyl group or an aromatic 6-membered heterocycle, substituted at the ortho position with 1-hydroxy(1C-4C)alkyl, (1C-4C)alkoxy, C(O)(1C-4C)alkyl, CO2(1C-4C)alkyl, C(O)NH2, cyano, nitro, or CH?NOR7, and optionally further substituted with (1C-2C)alkyl, (1C-2C)fluoroalkyl or halogen; or R4
    Type: Application
    Filed: September 22, 2010
    Publication date: January 13, 2011
    Applicant: N.V. Organon
    Inventors: Jaap Van Der Louw, Neeltje Miranda Teerhuis, Johannes Petrus Maria Lommerse, Herman Thijs Stock, Pedro Harold Han Hermkens
  • Publication number: 20110009379
    Abstract: [Problems] A compound, which is useful as an active ingredient for a pharmaceutical composition, for example a pharmaceutical composition for treating constipation-type irritable bowel syndrome, atonic constipation and/or functional gastrointestinal disorder, is provided. [Means for Solution] The present inventors have extensively studied compounds having TRPA1 channel activation activity, and confirmed that an indolinone compound has a TRPA1 channel activation activity, and thus completed the present invention. The indolinone compound of the present invention has a TRPA1 channel activation activity and can be used as an active ingredient of a pharmaceutical composition for preventing and/or treating constipation-type irritable bowel syndrome, atonic constipation and/or functional gastrointestinal disorder or the like.
    Type: Application
    Filed: March 30, 2009
    Publication date: January 13, 2011
    Applicant: ASTELLAS PHARMA INC.
    Inventors: Hidetaka Kaku, Tomofumi Takuwa, Michihito Kageyama, Katsura Nozawa, Hitoshi Doihara
  • Patent number: 7868034
    Abstract: This invention is directed to indolone derivatives which are antagonists or the GALR3 receptor. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a pharmaceutical composition made by combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier.
    Type: Grant
    Filed: June 17, 2008
    Date of Patent: January 11, 2011
    Assignee: H. Lundbeck A/S
    Inventors: Michael Konkel, John M. Werzel, Jamie Talisman
  • Patent number: 7863315
    Abstract: Provided herein are isolated compounds of formula I: processes for their preparation and isolation, as well as pharmaceutical compositions which comprise these therapeutic agents, and methods of use therefore the treatment and/or control of conditions associated with or mediated by effects of histone deacetylase.
    Type: Grant
    Filed: January 14, 2009
    Date of Patent: January 4, 2011
    Assignee: Shenzhen Chipscreen Biosciences, Ltd.
    Inventors: Xian-Ping Lu, Zhi-bin Li, Zhi-Qiang Ning
  • Publication number: 20100331280
    Abstract: There is provided a method of modifying vasoactivity by regulating a soluble A? pro-inflammatory pathway. Also provided is a method of modifying inflammatory reactions in microglia and neurons by regulating a soluble A? pro-inflammatory pathway. A method of treating patients with vascular disease by modifying an intracellular soluble A? pro-inflammatory pathway is also provided. A pharmaceutical composition consisting essentially of an effective amount of a soluble A? pro-inflammatory pathway regulator in a pharmaceutically effective carrier is also provided.
    Type: Application
    Filed: October 20, 2009
    Publication date: December 30, 2010
    Inventors: Daniel C. Paris, Terrence C. Town, Michael J. Mullan
  • Patent number: 7858616
    Abstract: The present invention relates to indolinone derivatives, substituted in the 6-position, of the formula in which R1 to R6 and X are as defined in Claim 1, to their tautomers, enantiomers, diastereomers, to their mixtures and to their salts, in particular their physiologically acceptable salts, which have useful pharmacological properties, in particular in inhibiting action on various receptor tyrosine kinases and on the proliferation of endothelial cells and various tumour cells, to medicaments comprising these compounds, to their use and to processes for their preparation.
    Type: Grant
    Filed: April 10, 2009
    Date of Patent: December 28, 2010
    Assignee: Boehringer Ingelheim Pharma GmbH & Co. KG
    Inventors: Gerald Juergen Roth, Armin Heckel, Thorsten Lehmann-Lintz, Joerg Kley, Frank Hilberg, Jacobus C. A. Van Meel, Ulrike Tontsch-Grunt
  • Publication number: 20100316655
    Abstract: Disclosed herein are drug compounds that have MDR-inverse activity and thus are effective against multidrug-resistant cells. Exemplary compounds disclosed herein have the structure: Examples of the disclosed compounds have been found to have, inter alia, efficacy in directly treating multidrug resistant cells, rendering multidrug resistant cells susceptible to other chemotherapeutics and in some instances reversing multidrug resistance.
    Type: Application
    Filed: February 10, 2009
    Publication date: December 16, 2010
    Inventors: Matthew D. Hall, Michael M. Gottesman, Jennifer L. Hellawell, Joseph A. Ludwig, Henry M. Fales, Noeris K. Salam, Gergely Szakács
  • Publication number: 20100311717
    Abstract: Methods and compositions for preventing or reducing weight gain and associated metabolic syndrome in patients receiving atypical antipsychotic drugs for treatment of mental illnesses are described. The invention comprises administering to a patient in need of treatment an effective amount of a dopamine agonist in conjunction with an effective amount of an atypical antipsyochotic drug. In one embodiment of the invention, the dopamine agonist is pramipexole. The dopamine agonist may be administered in a low dose, such as less than 1 mg per day of pramipexole. Examples of atypical antipsychotic drugs which may be administered in conjunction with the dopamine agonist include clozapine, olanzapine, quetiapine and risperadone.
    Type: Application
    Filed: November 5, 2008
    Publication date: December 9, 2010
    Inventors: Diane McIntosh, Kevin Kjernisted
  • Publication number: 20100311797
    Abstract: The present invention relates to substituted indoles of formula (I), useful as pharmaceutical compounds for treating respiratory disorders.
    Type: Application
    Filed: June 2, 2010
    Publication date: December 9, 2010
    Inventors: Roger Victor Bonnert, Timothy Jon Luker, John Cumming
  • Patent number: 7846962
    Abstract: Compositions and methods for inhibiting translation using 3-(5-tert-Butyl-2-Hydroxy-phenyl)-3-phenyl-1,3-dihydro-indol-2-one and/or its derivatives are provided. Compositions, methods and kits for treating (1) cellular proliferative disorders, (2) non-proliferative, degenerative disorders, (3) viral infections, and/or (4) disorders associated with viral infections, using 3-(5-tert-butyl-2-hydroxy-phenyl)-3-phenyl-1,3-dihydro-indol-2-one and/or its derivatives are described.
    Type: Grant
    Filed: February 10, 2009
    Date of Patent: December 7, 2010
    Assignee: President and Fellows of Harvard College
    Inventors: José A. Halperin, Amarnath Natarajan, Huseyin Aktas, Yun-Hua Fan, Han Chen
  • Publication number: 20100305152
    Abstract: The shikimate pathway links metabolism of carbohydrates to biosynthesis of aromatic compounds, which is an attractive target for the rational drug and herbicide design because it is essential in algae, higher plants, bacteria, and fungi, but absent from mammals. Thus, the present invention provides a method of inhibiting the growth of bacteria or fungi, especially Helicobacter pylori, through inhibiting enzymes in the shikimate pathway.
    Type: Application
    Filed: May 27, 2009
    Publication date: December 2, 2010
    Applicant: NATIONAL TSING HUA UNIVERSITY
    Inventors: WEN-CHING WANG, WEN-CHI CHENG, JINN-MOON YANG
  • Publication number: 20100298304
    Abstract: The invention relates to methods for diagnosis and treatment of autism spectrum disorders, particularly for autism spectrum disorders characterized by increased head size (circumference) and deficits in social behavior.
    Type: Application
    Filed: January 15, 2010
    Publication date: November 25, 2010
    Applicant: Massachusetts Institute of Technology
    Inventors: Damon Theron Page, Mriganka Sur
  • Publication number: 20100298376
    Abstract: The present invention provides compositions and methods of synthesizing optionally substituted 3-substituted indolin-2-ones and methods to employ the resultant compounds to protect against neurodegeneration including diseases such as Alzheimer's disease, Parkinson's disease, or Huntington's disease, and conditions such as ischemic stroke.
    Type: Application
    Filed: May 13, 2010
    Publication date: November 25, 2010
    Applicants: BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEM, SOUTHERN METHODIST UNIVERSITY
    Inventors: Santosh R. D'Mello, Edward A. Biehl
  • Patent number: 7834037
    Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of 5-lipoxygenase-activating protein (FLAP). Also described herein are methods of using such FLAP modulators, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other leukotriene-dependent or leukotriene mediated conditions or diseases.
    Type: Grant
    Filed: October 27, 2007
    Date of Patent: November 16, 2010
    Assignee: Amira Pharmaceuticals, Inc.
    Inventors: John Howard Hutchinson, Nicholas Simon Stock, Jeffrey Roger Roppe
  • Publication number: 20100286226
    Abstract: The present invention relates to combination therapies and pharmaceutical compositions comprising a combination of 5-hydroxytryptophan and a serotonin reuptake inhibitor that binds to an ailosteric site of the serotonin transporter. The present invention further provides a pharmaceutical composition comprising (i) 5-hydroxytryptophan in an amount ranging from about 1 mg to about 75 mg; and (ii) a serotonin reuptake inhibitor that binds to an allosteric site of the serotonin transporter.
    Type: Application
    Filed: September 24, 2008
    Publication date: November 11, 2010
    Applicant: H. LUNDBECK A/S
    Inventors: Connie Sanchez Morillo, Toni D. Wolinsky
  • Patent number: 7825155
    Abstract: Disclosed is a compound represented by the formula (1) below, a prodrug thereof or a pharmaceutically acceptable salt of either, which is useful as a therapeutic, preventive or ameliorating agent for diabetes and the like. (In the formula, R3 represents an optionally substituted carbamoyl group or the like; X represents a hydroxyl group or the like; W1 and W2 independently represent a single bond or methylene; R7 and R8 independently represent a hydrogen atom, an optionally substituted alkyl group or the like; and Ar represents an optionally substituted aryl group or the like.
    Type: Grant
    Filed: September 13, 2006
    Date of Patent: November 2, 2010
    Assignee: Dainippon Sumitomo Pharma Co., Ltd.
    Inventors: Teruhisa Tokunaga, Tsuyoshi Takasaki, Kozo Yoshida, Ryu Nagata
  • Publication number: 20100267652
    Abstract: Disclosed are methods of enhancing the chemotherapeutic treatment of tumor cells, reducing resistance of a cancer cell to a chemotherapeutic agent, a method of inhibiting ABCG2 or MRP1 in a mammal afflicted with cancer, and a method of increasing the bioavailability of an ABCG2 substrate drug in a mammal. The methods comprise administering peliomycin and other compounds described herein.
    Type: Application
    Filed: November 5, 2008
    Publication date: October 21, 2010
    Inventors: Curtis J. Henrich, Heidi R. Bokesch, Susan E. Bates, Robert W. Robey, Suneet Shukla, Suresh V. Ambudkar, Michael C. Dean, James B. McMahon
  • Publication number: 20100249201
    Abstract: Compositions and methods for inhibiting translation using 3-(5-tert-Butyl-2-Hydroxy-phenyl)-3-phenyl-1,3-dihydro-indol-2-one and/or its derivatives are provided. Compositions, methods and kits for treating (1) cellular proliferative disorders, (2) non-proliferative, degenerative disorders, (3) viral infections, and/or (4) disorders associated with viral infections, using 3-(5-tert-butyl-2-hydroxy-phenyl)-3-phenyl-1,3-dihydro-indol-2-one and/or its derivatives are described.
    Type: Application
    Filed: June 9, 2010
    Publication date: September 30, 2010
    Applicant: President and Fellows of Harvard College
    Inventors: José A. Halperin, Amarnath Natarajan, Huseyin Aktas, Yun-Hua Fan, Han Chen
  • Patent number: 7803834
    Abstract: The invention relates to novel oxindol derivative of general formula (I), wherein substituents R1, R2, A, B and Y are such as defined in a claim 1. Drugs containing said derivatives and the use thereof for preventing and/or treating vassopress- and/or oxytocin-dependent-diseases are also disclosed.
    Type: Grant
    Filed: March 23, 2006
    Date of Patent: September 28, 2010
    Assignee: Abbott GmbH & Co. KG
    Inventors: Thorsten Oost, Wilfried Lubisch, Wolfgang Wernet, Wilfried Hornberger, Liliane Unger
  • Publication number: 20100240724
    Abstract: The present invention relates to an edible film composition comprising a waxy starch hydrolysate, a modified starch and a water-soluble polymer, and an edible film comprising the same. The present edible film may not only have an excellent film forming property, solubility and feeling in the oral cavity, but also be easily prepared at low cost, and thus be usefully used as an oral cleanser or a bad breath remover for oral cleansing, and a soluble formulation on tongue for uptake of drug in the oral cavity.
    Type: Application
    Filed: September 25, 2008
    Publication date: September 23, 2010
    Applicant: C.L. PHARM
    Inventors: Seok Hoon Chang, Kyoung Tae Jung
  • Publication number: 20100240726
    Abstract: Indole derivatives, compositions including same, and methods utilizing same for the treatment of amyloid associated diseases, such as type II diabetes mellitus, Alzheimer's dementia or diseases, systemic and localized amyloidosis, and prion-related encephalopathies are provided.
    Type: Application
    Filed: June 6, 2010
    Publication date: September 23, 2010
    Applicant: Tel Aviv University Future Technology Development L.P.
    Inventors: Ehud GAZIT, Tomer Cohen
  • Publication number: 20100233259
    Abstract: The present invention relates to a dosage form of Ropinirole. The dosage formulation of the invention is intended to control the release rate of one or more therapeutically active agents.
    Type: Application
    Filed: December 14, 2009
    Publication date: September 16, 2010
    Inventors: Pascal Grenier, Emeric Reynaud, Alain Nhamias, Guy Vergnault
  • Publication number: 20100227863
    Abstract: The present application discloses substituted 3-(4-hydroxyphenyl)-indolin-2-one compounds (oxindole compounds) of the formula and the use of such compounds for the preparation of a medicament for the treatment of cancer in a mammal, in particular in humans.
    Type: Application
    Filed: April 28, 2008
    Publication date: September 9, 2010
    Applicant: TOPOTARGET A/S
    Inventors: Mette Knak Christensen, Fredrik Bjoerkling
  • Publication number: 20100216835
    Abstract: The present invention provides compositions and methods for modulating bacterial quorum sensing using antagonist or agonist compounds. Further, the present invention provides methods of treating or preventing microbial damages and diseases, in particular for diseases where there is an advantage in inhibiting quorum sensing regulated phenotypes of pathogens.
    Type: Application
    Filed: February 25, 2010
    Publication date: August 26, 2010
    Inventors: Jo E. Handelsman, Bradley R. Borlee
  • Patent number: 7776907
    Abstract: Methods of treating, preventing and/or managing macular degeneration are disclosed. Specific embodiments encompass the administration of a selective cytokine inhibitory drug, or a pharmaceutically acceptable salt, solvate, hydrate, stereoisomer, clathrate, or prodrug thereof, alone or in combination with a second active agent and/or surgery. Pharmaceutical compositions, single unit dosage forms, and kits suitable for use in methods of the invention are also disclosed.
    Type: Grant
    Filed: October 30, 2003
    Date of Patent: August 17, 2010
    Assignee: Celgene Corporation
    Inventor: Jerome B. Zeldis
  • Publication number: 20100204211
    Abstract: The present invention relates to the use of indolinones of general formula substituted in the 6 position, wherein R1 to R5 and X are defined as in claim 1, the isomers and the salts thereof, particularly the physiologically acceptable salts thereof, as a medicament for the prevention or treatment of specific fibrotic diseases.
    Type: Application
    Filed: December 22, 2009
    Publication date: August 12, 2010
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: John Edward PARK, Gerald Juergen ROTH, Armin HECKEL, Nveed CHAUDHARY, Trixi BRANDL, Georg DAHMANN, Matthias GRAUERT
  • Publication number: 20100203175
    Abstract: The invention relates to the use, as an active ingredient, of at least one substance that promotes the deglycation of AGEs for preparing a composition, especially for limiting the presence of AGEs in a tissue. The invention particularly relates to the use of such a substance for preparing a composition intended to prevent and/or combat a reduction in flexibility and/or plasticity and/or elasticity and/or functionality of a tissue, and/or to prevent and/or combat the ageing of a tissue, by promoting the deglycation of AGEs in the tissue, said tissue preferably being the skin, or the tissue wall of a blood vessel or of an organ.
    Type: Application
    Filed: July 9, 2008
    Publication date: August 12, 2010
    Applicant: BASF BEAUTY CARE SOLUTIONS FRANCE S.A.S.
    Inventors: Nabil ABDUL-MALAK, Cecile ALTOBELLI, Eric PERRIER
  • Publication number: 20100197756
    Abstract: The present invention relates to substituted indoles useful as pharmaceutical compounds for treating respiratory disorders.
    Type: Application
    Filed: April 12, 2010
    Publication date: August 5, 2010
    Inventors: Roger Bonnert, Mark Dickinson, Rukhsana Rasul, Hitesh Sanganee, Simon Teague