Chalcogen Or Nitrogen Bonded Directly At 1-, 2- Or 3-position Of The Diazole Ring By Nonionic Bonding Patents (Class 514/395)
  • SULFONYL CONTAINING COMPOUNDS AS CYSTEINE PROTEASE INHIBITORS
    Publication number: 20110281879
    Abstract: The present invention is directed to compounds that are inhibitors of cysteine proteases, in particular, cathepsins B, K, L, F, and S and are therefore useful in treating diseases mediated by these proteases. The present invention is directed to pharmaceutical compositions comprising these compounds and processes for preparing them.
    Type: Application
    Filed: January 12, 2011
    Publication date: November 17, 2011
    Applicant: ViroBay, Inc.
    Inventor: Craig Mossman
  • NANOPARTICLE PHARMACEUTICAL FORMULATIONS
    Publication number: 20110268775
    Abstract: The present invention is directed to methods of preparing nanoparticles of aqueous-insoluble compounds, particularly aqueous-insoluble bioactive (drug) compounds, and to compositions and medicaments obtained by these methods. These methods, compositions, and other inventive aspects of the present invention are based particularly on the use of bile acid compound(s) to prepare nanoparticles of aqueous-insoluble compounds.
    Type: Application
    Filed: January 5, 2010
    Publication date: November 3, 2011
    Applicant: PHARMANOVA, INC.
    Inventors: Kris Holt, Deepak Thassu, Michael R. Violante
  • Amino-alkyl amide derivatives as CCR3 receptor ligands
    Patent number: 8044078
    Abstract: The invention relates to a compound of the general formula (I), as defined herein which is useful for the treatment of a pathology in a patient wherein a CCR3 receptor plays a role in the development of the pathology, and pharmaceutical preparations containing such compound. The invention is also directed to a process for preparing the compound of the general formula (I), and intermediate useful in the preparation.
    Type: Grant
    Filed: March 19, 2008
    Date of Patent: October 25, 2011
    Assignee: Sanofi-Aventis
    Inventors: Agnes Pappne Behr, Zoltan Kapui, Peter Aranyi, Sandor Batori, Veronika Bartane Bodor, Lajos T. Nagy, Mihalyne Santa, legal representative, Marton Varga, Endre Mikus, Katalin Urban-Szabo, Judit Vargane Szeredi, Tibor Szabo, Edit Susan, Marianna Kovacs
  • Fused heterocyclic compounds
    Patent number: 8039500
    Abstract: There is provided a compound of the formula: wherein R1 is an optionally substituted hydrocarbyl, a substituted amino, etc.; R2 is an aromatic group substituted with one or two substituents at the positions adjacent to the position bonded to Z, and said aromatic group may have additional substituent(s); X is —NR3— wherein R3 is a hydrogen, an optionally substituted hydrocarbyl or an acyl, or sulfur; Y1, Y2 and Y3 are an optionally substituted methine or a nitrogen, etc.; and Z is an optionally substituted methylene, provided that carbonyl is excluded; or a salt thereof or a prodrug thereof, which have CRF receptor antagonist activity and use thereof.
    Type: Grant
    Filed: December 28, 2007
    Date of Patent: October 18, 2011
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Kazuyoshi Aso, Michiyo Mochizuki, Katsumi Kobayashi
  • ARYL GUANIDINE F1F0-ATPASE INHIBITORS AND RELATED METHODS
    Publication number: 20110251200
    Abstract: The invention provides to a family of aryl guanidine-based F1F0-ATPase inhibitors, e.g., mitochondrial F1F0-ATPase inhibitors, methods for their discovery, and their use as therapeutic agents for treating certain disorders.
    Type: Application
    Filed: September 11, 2009
    Publication date: October 13, 2011
    Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN
    Inventors: Gary D. Glick, Peter Toogood, Gina Ney
  • Compositions and Methods for Inhibiting Gastric Acid Secretion
    Publication number: 20110250268
    Abstract: The present invention is related to novel oral compositions comprising an irreversible gastric H+/K+-ATPase proton pump inhibitor (PPI) as a gastric acid secretion inhibitor and one or more small carboxylic acid molecules as parietal cell activators in the gastric lumen. Unexpectedly, the compositions of the present invention are capable of enhancing the anti-acid activity of PPI in the stomach. The present invention further relates to a method of using such compositions to reduce gastric acid secretion in a mammal.
    Type: Application
    Filed: April 19, 2011
    Publication date: October 13, 2011
    Inventors: Aleksey Kostadinov, David Ayelet, Sabina Glozman, Tal Atarot
  • ACTIVE SUBSTANCE AND PHARMACEUTICAL COMPOSITION FOR TREATING ALCOHOL DEPENDENCE, AND A METHOD FOR OBTAINING AND THE USE OF SAID ACTIVE SUBSTANCE
    Publication number: 20110245231
    Abstract: The invention relates to novel drug substance for the treatment of alcohol dependence, pharmaceutical composition, medicament and method for treatment of dependence on using ethyl alcohol containing beverages.
    Type: Application
    Filed: December 15, 2009
    Publication date: October 6, 2011
    Applicant: Alla Chem, LLC
    Inventors: Andrey Alexandrovich Ivashchenko, Nikolay Filippovich Savchuk
  • Cyclopropyl pyrrolidine orexin receptor antagonists
    Patent number: 8030495
    Abstract: The present invention is directed to cyclopropyl proline bis-amide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved.
    Type: Grant
    Filed: May 19, 2008
    Date of Patent: October 4, 2011
    Inventors: Paul J. Coleman, Swati P. Mercer, Anthony J. Roecker
  • Methods of optimizing drug therapeutic efficacy for treatment of immune-mediated gastrointestinal disorders
    Patent number: 8030293
    Abstract: The present invention provides a method of optimizing therapeutic efficacy and reducing toxicity associated with 6-mercaptopurine drug treatment of an immune-mediated gastrointestinal disorder such as inflammatory bowel disease. The method of the invention includes the step of determining the level of one or more 6-mercaptopurine metabolites in the patient having an immune-mediated gastrointestinal disorder.
    Type: Grant
    Filed: August 4, 2009
    Date of Patent: October 4, 2011
    Assignee: Hopital-Sainte-Justine
    Inventors: Ernest G. Seidman, Yves Theoret
  • GUANIDINE COMPOUNDS, AND USE THEREOF AS BINDING PARTNERS FOR 5-HT5 RECEPTORS
    Publication number: 20110237589
    Abstract: The present invention relates to guanidine compounds of the general formula I corresponding enantiomeric, diastereomeric and/or tautomeric forms thereof as well as pharmaceutically acceptable salts thereof. The present compound further relates to the use of guanidine compounds as binding partners for 5-HT5 receptors for the treatment of diseases which are modulated by a 5-HT5 receptor activity, in particular for the treatment of neurodegenerative and neuropsychiatric disorders as well as the associated signs, symptoms and dysfunctions.
    Type: Application
    Filed: February 4, 2011
    Publication date: September 29, 2011
    Inventors: Astrid Netz, Wilhelm Amberg, Udo Lange, Michael Ochse, Charles W. Hutchins, Francisco-Xavier Garcia-Ladona, Wolfgang Wernet, Andreas Kling, Andrea Hager-Wernet
  • Non-pegylated liposomal doxorubicin triple combination therapy
    Patent number: 8026267
    Abstract: The present invention relates to a method for treating metastatic breast cancer in an individual comprising administering to an individual in need thereof a dosing regimen which comprises administering to the individual nonpegylated liposomal doxorubicin, a taxane and a HER2/neu receptor antagonist, wherein the individual previously has been administered an anthracycline.
    Type: Grant
    Filed: September 10, 2010
    Date of Patent: September 27, 2011
    Assignee: Sopherion Therapeutics, LLC
    Inventors: Marcel Rozencweig, Ronald H. Goldfarb, Salvatore Forenza
  • TRANSCRIPTION FACTOR MODULATING COMPOUNDS AND METHODS OF USE THEREOF
    Publication number: 20110230523
    Abstract: Substituted benzoimidazole compounds useful as anti-infectives that decrease resistance, virulence, or growth of microbes are provided. Methods of making and using substituted benzoimidazole compounds, as well as pharmaceutical preparations thereof, in, e.g., reducing antibiotic resistance and inhibiting biofilms.
    Type: Application
    Filed: August 6, 2009
    Publication date: September 22, 2011
    Applicant: Paratek Pharmaceuticals, Inc.
    Inventors: Stuart B. LEVY, Michael N. ALEKSHUN, Brent L. PODLOGAR, Kwasi OHEMENG, Atul K. VERMA, Tadeusz WARCHOL, Beena BHATIA, Todd BOWSER, Mark GRIER
  • Thio-subsituted Anthra [1, 2-d] imidazole- 6, 11-dione Dervatives, Preparation Method and application thereof
    Publication number: 20110207727
    Abstract: A series of novel thio-substituted anthra[1,2-d]imidazole-6,11-dione dervatives, and the preparation method and application of said derivatives, said application having a pharmaceutical composition containing said derivatives with therapeutically effective amount for treating cancer, and said application involves effects of said derivatives for inhibiting telomerase activity, inhibiting the growth of cancer cell, treating cancer and the like.
    Type: Application
    Filed: February 25, 2010
    Publication date: August 25, 2011
    Inventor: Hsu-Shan HUANG
  • Heterocyclic substituted bisarylurea derivatives
    Patent number: 8003657
    Abstract: The present invention relates to heterocyclic substituted bisarylurea derivatives of formula I, the use of the compounds of formula I as inhibitors of one or more kinases, the use of the compounds of formula I for the manufacture of a pharmaceutical composition and a method of treatment, comprising administering said pharmaceutical composition to a patient.
    Type: Grant
    Filed: October 6, 2005
    Date of Patent: August 23, 2011
    Assignee: Merck Patent GmbH
    Inventors: Frank Stieber, Alfred Jonczyk, Guenter Hoelzemann, Hans-Peter Buchstaller, Lars Thore Burgdorf, Wilfried Rautenberg, Hartmut Greiner
  • NOVEL CYCLIC BENZIMIDAZOLE DERIVATIVES USEFUL AS ANTI-DIABETIC AGENTS
    Publication number: 20110195964
    Abstract: Novel compounds of the structural formula (I) are activators of AMP-protein kinase and are useful in the treatment, prevention and suppression of diseases mediated by the AMPK-activated protein kinase. The compounds of the present invention are useful in the treatment of Type 2 diabetes, hyperglycemia, metabolic syndrome, obesity, hypercholesterolemia, and hypertension.
    Type: Application
    Filed: October 19, 2009
    Publication date: August 11, 2011
    Inventors: Qun Dang, De Michael Chung, Tony S. Gibson, Daniel K. Cashion, HongJian Jiang, Jianming Bao, Ping Lan, Huagang Lu, Gergely M. Makara, F. Anthony Romero, Iyassu Sebhat, Dariusz Wodka
  • Antibacterial agents
    Patent number: 7989422
    Abstract: The present invention, in one aspect, provides a method of inhibiting bacterial growth by contacting bacteria with an effective amount of at least one monosaccharide compound of formula (1) as described herein:
    Type: Grant
    Filed: December 20, 2006
    Date of Patent: August 2, 2011
    Assignee: Alchemia Limited
    Inventors: Wim Meutermans, Declan McKeveney, Johannes Zuegg, Rajaratnam Premraj, Craig Muldoon, Giang Thanh Le
  • GUANIDINE COMPOUNDS AS ANESTHETICS AND FOR TREATMENT OF NERVOUS SYSTEM DISORDERS
    Publication number: 20110178079
    Abstract: Novel guanidine compounds having the formula in which R1, R2, and R4 are as defined, are effective as sodium channel dockers in neuronal mammalian cells and as anesthetics and/or analgesics, particularly local spinal and/or epidural anesthetics, for alleviation of neuropathic pain, for providing a neuroprotective effect, and for producing anti-convulsant effects.
    Type: Application
    Filed: March 30, 2011
    Publication date: July 21, 2011
    Inventors: Kenneth Drasner, Kevin T. Weber
  • STEREOSPECIFICITY OF METHYLSULFINYL REDUCTION
    Publication number: 20110178072
    Abstract: This disclosure relates to compositions and methods of use involving compounds (e.g., drugs) containing methylsulfinyl moieties. For example, a compound may be administered in an excess of either the R- or S-epimer of the methylsulfinyl moiety based on whether the compound exhibits higher biological activity when the methylsulfinyl moiety is present in the methylsulfinyl-oxidized form or the methylsulfide-reduced form.
    Type: Application
    Filed: July 23, 2009
    Publication date: July 21, 2011
    Inventors: Vadim Gladyshev, Byung Cheon Lee
  • HETEROCYCLIC COMPOUND AND USE THEREOF
    Publication number: 20110172245
    Abstract: Provided is a heterocyclic compound showing strong Raf inhibitory activity. A compound represented by the formula wherein each symbol is as defined in the specification, or a salt thereof.
    Type: Application
    Filed: August 22, 2008
    Publication date: July 14, 2011
    Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Masaaki Hirose, Masanori Okaniwa, Takashi Imada
  • GUANIDINE COMPOUNDS AS ANESTHETICS AND FOR TREATMENT OF NERVOUS SYSTEM DISORDERS
    Publication number: 20110166181
    Abstract: Novel guanidine compounds having the formula in which R1, R2 and R4 are as defined, are effective as sodium channel dockers in neuronal mammalian cells and as anesthetics and/or analgesics, particularly local spinal and/or epidural anesthetics, for alleviation of neuropathic pain, for providing a neuroprotective effect, and for producing anti-convulsant effects.
    Type: Application
    Filed: December 7, 2010
    Publication date: July 7, 2011
    Inventors: Kenneth Drasner, Kevin T. Weber
  • ARTEMISININ AND DERIVATIVES THEREOF AS ANTIVIRALS
    Publication number: 20110166106
    Abstract: Methods to treat various herpes viral infections using the natural product artemisinin and derivatives of that compound are described. The methods are especially applicable for treatment of conditions associated with HHV-6, and are also applicable to the treatment of conditions that are induced or exacerbated by an HHV-6 infection or by a reactivation of a latent stage of an HHV-6 infection.
    Type: Application
    Filed: June 17, 2009
    Publication date: July 7, 2011
    Inventors: Manfred Marschall, Jens Milbradt, Dharam Ablashi
  • SAMLL MOLECULE INHIBITORS FOR THE TREATMENT OR PREVENTION OF DENGUE VIRUS INFECTION
    Publication number: 20110158940
    Abstract: Methods and pharmaceutical compositions for treating viral infections, by administering certain compounds in therapeutically effective amounts are disclosed. Methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment and prophylaxis of viral infections such as caused by flavivirus is disclosed, i.e., including but not limited to, Dengue virus, West Nile virus, yellow fever virus, Japanese encephalitis virus, and tick-borne encephalitis virus.
    Type: Application
    Filed: June 2, 2009
    Publication date: June 30, 2011
    Inventors: Chelsea M. Byrd, Robert Jordan, Dongcheng Dai, Dennis F. Hruby
  • Preparation and use of aryl alkyl acid derivatives for the treatment of obesity
    Patent number: 7968576
    Abstract: This invention relates to certain aryl alkyl acid compounds, compositions, and methods for treating or preventing obesity and related diseases.
    Type: Grant
    Filed: September 8, 2008
    Date of Patent: June 28, 2011
    Inventors: Roger A. Smith, Ann-Marie Campbell, Philip Coish, Miao Dai, Susan Jenkins, Derek Lowe, Stephen J. O'Connor, Ning Su, Gan Wang, Mingbao Zhang, Lei Zhu
  • Organic compounds
    Publication number: 20110152261
    Abstract: There are described cyclohexyl amide derivatives useful as corticotropin releasing (CRF1) receptor antagonists.
    Type: Application
    Filed: August 5, 2009
    Publication date: June 23, 2011
    Inventors: David Beattie, Anny-Odile Colson, Andrew James Culshaw, Lisa Rooney, Emily Stanley, Lilya Sviridenko
  • Imidazo[4, 5-B]pyridin-2-one and oxazolo[4, 5-B] pyridin-2-one compounds and analogs thereof as cancer therapeutic compounds
    Patent number: 7951819
    Abstract: The present invention pertains to certain imidazo[4,5-b]pyridin-2-one and oxazolo[4,5 b]pyridin-2-one compounds and analogs thereof, which, inter alia, inhibit RAF (e.g., B RAF) activity, inhibit cell proliferation, treat cancer, etc. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit RAF (e.g., B-RAF) activity, to inhibit receptor tyrosine kinase (RTK) activity, to inhibit cell proliferation, and in the treatment of diseases and conditions that are ameliorated by the inhibition of RAF, RTK, etc., proliferative conditions such as cancer (e.g., colorectal cancer, melanoma), etc.
    Type: Grant
    Filed: April 26, 2007
    Date of Patent: May 31, 2011
    Assignees: Cancer Research Technology Limited, The Institute of Cancer Research: Royal Cancer Hospital, Astex Therapeutics Limited
    Inventors: Dan Niculescu-Duvaz, Caroline Joy Springer, Richard Malcolm Marais, Harmen Dijkstra, Delphine Menard, Ion Niculescu-Duvaz, Lawrence Davies, Arnaud Nourry
  • Antiviral agents
    Patent number: 7951955
    Abstract: This invention relates to compounds of formula I their salts, and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions comprising these compounds and their use in the treatment of picornavirus infections in mammals, as well as novel intermediates useful in the preparation of the compounds of formula I.
    Type: Grant
    Filed: May 1, 2008
    Date of Patent: May 31, 2011
    Assignee: Biota Scientific Management Pty Ltd
    Inventors: Keith Watson, Guy Krippner, Pauline Stanislawski, Darryl McConnell
  • Non-nucleoside reverse transcriptase inhibitors
    Patent number: 7947709
    Abstract: Compounds of formula I, wherein R1, R2, R3, X and Ar, are as defined herein or pharmaceutically acceptable salts thereof, inhibit HIV-1 reverse transcriptase and afford a method for prevention and treatment of HIV-1 infections and the treatment of AIDS and/or ARC. The present invention also relates to compositions containing compounds of formula I useful for the prevention and treatment of HIV-1 infections and the treatment of AIDS and/or ARC.
    Type: Grant
    Filed: June 20, 2008
    Date of Patent: May 24, 2011
    Assignee: Roche Palo Alto LLC
    Inventors: Todd Richard Elworthy, Joan Heather Hogg, Joshua Kennedy-Smith, Counde O'Yang, Mark Smith, Zachary Kevin Sweeney, Jeffrey Wu
  • COMPOUND CAPABLE OF INHIBITING 11-BETA HYDROXYSTERIOD DEHYDROGENASE
    Publication number: 20110112151
    Abstract: There is provided a compound of formula R1—CO—X—Y—Z—R2 wherein X and Z are each optional groups that are, independently, saturated or unsaturated carbon chains having a length of 1 to 3 carbons; Y is SO, S, SO2, CH?CH, CH2CH2 or O; R1 is wherein denotes the point of attachment; R2 is a heteroaryl group comprising an optionally substituted 5 or 6 membered ring, which ring contains only carbon and at least one nitrogen, or contains only carbon, and at least two nitrogens and at least one sulfur; and wherein (i) when R1 is and —CO—X—Y—Z— is CO—CH2—SO, CO—CH2—S, or CO—CH2—SO2, R2 is other than and; (ii) when R1 is and —CO—X—Y—Z— is —CO—CH2—O—, R2 is other than
    Type: Application
    Filed: February 25, 2009
    Publication date: May 12, 2011
    Inventors: Nigel Vicker, Xiangdong Su, Fabienne Pradaux-Caggiano, Barry Victor Lioyd Potter
  • DERIVATIVES OF TETRABROMOBENZIMIDAZOLE, A PROCESS FOR THE PREPARATION THEREOF, A PHARMACEUTICAL COMPOSITION COMPRISING THE SAME, A METHOF OF USING THE SAME, A METHOD FOR MODULATING OR REGULATING SERINE/THREONINE KINASES, AND SERINE/THREONINE KINASES MODULATING AGENT
    Publication number: 20110112091
    Abstract: A derivative of tetrabromobenzimidazole, a process for the preparation thereof, a pharmaceutical composition, a method for using the same, a method for modulating or regulating serine/threonine kinases, and a serine/threonine kinases modulating agent. The invention relates to novel small-molecule compounds with kinase inhibitory activity, having superior properties as pharmaceutical agents, production method thereof and uses thereof. In particular, this invention relates to new derivatives of tetrabromobenzimidazole with Pim kinases inhibitory properties, which exhibits superior pharmacological actions, and can be useful for the treatment of disease conditions, especially cancers depending on Pim kinases, such as leukemias and prostate cancer.
    Type: Application
    Filed: November 12, 2009
    Publication date: May 12, 2011
    Applicant: SELVITA SP. Z O.O.
    Inventors: Krzysztof Brzozka, Wojciech Czardybon, Adrian Zarebski, Nicolas Beuzen
  • METHODS AND COMPOSITIONS FOR REDUCING SKIN DAMAGE
    Publication number: 20110091387
    Abstract: The RhoE GTPase pathway has been identified as a target for screening and treatment methods for the prevention and/or reduction of short- and long-term UVB-induced skin damage, e.g., the prevention and/or reduction of UVB-induced wrinkles. The invention thus features screening and treatment methods for prevention or reduction of UVB-induced sin damage, and related compositions, e.g., cosmetic compositions.
    Type: Application
    Filed: November 17, 2008
    Publication date: April 21, 2011
    Applicants: THE GENERAL HOSPITAL CORPORATION, SHISEIDO CO., LTD.
    Inventors: Sam W. Lee, Lakshmi Raj, Anna I. Mandinova, Haruhi Iwaki, Yuji Katsuta, Jotaro Nakanishi
  • TREATMENT OF CANCER
    Publication number: 20110081362
    Abstract: Described herein are methods based, in part, on the discovery of genes or gene products that can be down-modulated to inhibit the growth and survival of a cell, such as a cancer cell. In one embodiment, the genes or gene targets are preferentially expressed in a cell having an activating Ras mutation (e.g., a cancer cell), which permits selective inhibition of growth in cells bearing an activating Ras mutation without affecting cells lacking enhanced Ras activity. In addition, the methods described herein provide for determining cancer prognosis in an individual bearing an activating Ras mutation.
    Type: Application
    Filed: February 2, 2009
    Publication date: April 7, 2011
    Applicant: THE BRIGHAM AND WOMEN'S HOSPITAL, INC.
    Inventors: Stephen J. Elledge, Ji Luo, Michael Schlabach, Nicole Solimini
  • THERAPEUTIC ANTIVIRAL PEPTIDES
    Publication number: 20110082182
    Abstract: Disclosed herein are compounds represented by a formula: Therapeutic methods, compositions, medicaments, and dosage forms related thereto are also disclosed.
    Type: Application
    Filed: September 30, 2010
    Publication date: April 7, 2011
    Applicant: INTERMUNE, INC.
    Inventors: Brad Buckman, Vladimir Serebryany, Scott Seiwert, Leonid Beigelman, Antitsa Stoycheva
  • 2-AMINOBENZIMIDAZOLES FOR TREATING NEURODEGENERATIVE DISEASES
    Publication number: 20110071130
    Abstract: The invention relates to 2-aminobenzimidazoles useful in treating disorders that are mediated by A2a receptor function, including neurodegenerative diseases including Parkinson's disease and inflammation.
    Type: Application
    Filed: May 7, 2007
    Publication date: March 24, 2011
    Applicant: Pharmacopeia, Inc.
    Inventors: Andrew G. Cole, Brian F. McGuinness, Guizhen Dong, Ian Henderson
  • Raf Modulators And Methods Of Use
    Publication number: 20110071145
    Abstract: The present invention relates to compounds of the Formula I, wherein G, A, X1, X2, X3, Z, E, Y, and X are defined herein. The compounds modulate protein kinase enzymatic activity to modulate cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. Compounds of the invention inhibit, regulate and/or modulate kinases, particularly Raf. Methods of using and preparing the compounds, and pharmaceutical compositions thereof, to treat kinase-dependent diseases and conditions are also an aspect of the invention.
    Type: Application
    Filed: October 12, 2010
    Publication date: March 24, 2011
    Applicant: EXELIXIS, INC.
    Inventors: Neel Kumar Anand, Charles M. Blazey, Owen Joseph Bowles, Joerg Bussenius, Simona Costanzo, Jeffry Kimo Curtis, Larisa Dubenko, Abigail R. Kennedy, Steven Charles Defina, Angie I. Kim, Jean-Claire L. Manalo, Csaba J. Peto, Kenneth D. Rice, Tsze H. Tsang, Anagha Abhijit Joshi
  • Compounds that Inhibit Production of sAPPB and AB and Uses Thereof
    Publication number: 20110071124
    Abstract: The present invention relates to compounds with activity as inhibitors of sAPP? and A? production, and methods for treating, preventing, or ameliorating neurodegenerative diseases, such as Alzheimer's disease and pharmaceutical compositions containing such candidate compounds.
    Type: Application
    Filed: August 18, 2010
    Publication date: March 24, 2011
    Applicant: The Trustees of Columbia University in the City of New York
    Inventors: Tae-wan Kim, Donald W. Landry, Jeremy C. Hwang, Shi Xian Deng, Gangli Gong, Yuli Xie, Yidong Liu, Alison Rinderspacher
  • Benzazole Derivatives, Compositions, and Methods of Use as B-Secretase Inhibitors
    Publication number: 20110065713
    Abstract: The present invention is directed to benzazole compounds that inhibit ?-site amyloid precursor protein-cleaving enzyme (BACE) and that may be useful in the treatment or prevention of diseases in which BACE is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which BACE is involved.
    Type: Application
    Filed: November 19, 2010
    Publication date: March 17, 2011
    Applicant: High Point Pharmaceuticals, LLC
    Inventors: Adnan M.M. Mjalli, David Jones, Devi Reddy Gohimmukkula, Guoxiang Huang, Jeff Zhu, Mohan Rao, Robert C. Andrews, Tan Ren
  • TRANSCRIPTION FACTOR MODULATING COMPOUNDS AND METHODS OF USE THEREOF
    Publication number: 20110059962
    Abstract: Substituted benzoimidazole compounds useful as anti-infectives that decrease resistance, virulence, or growth of microbes are provided. Methods of using substituted benzimidazole compounds, in, e.g., reducing virulence and infectivity, inhibiting biofilms and treating bacterial infections, are also provided.
    Type: Application
    Filed: April 22, 2010
    Publication date: March 10, 2011
    Inventors: MICHAEL N. ALEKSHUN, VICTORIA BARTLETT, MICHAEL P. DRAPER, LYNNE GARRITY-RYAN, RAINA GAY, MARK GRIER, OAK K. KIM, STUART B. LEVY
  • BENZOIMIDAZOLES AS PROLYL HYDROXYLASE INHIBITORS
    Publication number: 20110046132
    Abstract: The present invention is directed to benzoimidazole compounds of the formula (1) and enantiomers, diastereomers, racemates, and pharmaceutically acceptable salts thereof. Compounds of the present invention are useful in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions modulated by prolyl hydroxylase activity.
    Type: Application
    Filed: April 28, 2009
    Publication date: February 24, 2011
    Inventors: Frances Meredith Hocutt, Barry Eastman Leonard, JR., Hillary M. Peltier, Victor K. Phuong, Michael H. Rabinowitz, Mark D. Rosen, Kyle T. Tarantino, Hariharan Venkatesan, Lucy Xiumin Zhao
  • Elansolids, Novel Natural Metabolites of Flexibacter and Antibiotically Active Derivatives Thereof
    Publication number: 20110034528
    Abstract: The present invention describes Elansolids, a new class of novel anti-bacterial compounds of formula (I).
    Type: Application
    Filed: February 19, 2009
    Publication date: February 10, 2011
    Inventors: Klaus Gerth, Heinrich Steinmetz, Gerhard Höfle
  • Inhibitors of histone deacetylase
    Patent number: 7868205
    Abstract: The invention relates to the inhibition of histone deacetylase. The invention provides compounds and methods for inhibiting histone deacetylase enzymatic activity. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.
    Type: Grant
    Filed: September 24, 2004
    Date of Patent: January 11, 2011
    Assignee: MethylGene Inc.
    Inventors: Oscar Moradei, Isabelle Paquin, Silvana Leit, Sylvie Frechette, Arkadii Vaisburg, Jeffrey M. Besterman, Pierre Tessier, Tammy C. Mallais
  • BENZIMIDAZOLE DERIVATIVES USEFUL AS TRPM8 CHANNEL MODULATORS
    Publication number: 20110003801
    Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein R0, R1, R2, R3, R4 and a are defined herein.
    Type: Application
    Filed: June 10, 2010
    Publication date: January 6, 2011
    Inventors: Michele C. Jetter, Mark J. Macielag, Mingde Xia, Xiaoqing Xu
  • BENZIMIDAZOLE DERIVATIVES USEFUL AS TRPM8 CHANNEL MODULATORS
    Publication number: 20110003800
    Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein R0, R1, R2, R3, R4 and a are defined herein.
    Type: Application
    Filed: June 10, 2010
    Publication date: January 6, 2011
    Inventors: Mark J. Macielag, Mingde Xia, Xiaoqing Xu
  • Deloxiglumide and proton pump inhibitor combination in the treatment of gastrointestinal disorders
    Patent number: 7863330
    Abstract: Combination of dexloxiglumide and a proton pump inhibitor (PPI) for the treatment of patients suffering from functional dyspepsia and gastroesophageal reflux disease (GERD) is disclosed.
    Type: Grant
    Filed: June 14, 2006
    Date of Patent: January 4, 2011
    Assignee: Rottapharm S.p.A.
    Inventors: Francesco Makovec, Massimo Maria D'Amato, Antonio Giordani, Lucio Claudio Rovati
  • BETA-AMINO ACID DERIVATIVES FOR TREATMENT OF DIABETES
    Publication number: 20100331346
    Abstract: Novel heterocyclic compounds of the formula I in which R1, R2, R2?, R2?, R3, R4, R5, R6, R7 and R8 have the meanings indicated in Claim 1, are activators of glucokinase and can be used for the prevention and/or treatment of Diabetes Typ 1 and 2, obesity, neuropathy and/or nephropathy.
    Type: Application
    Filed: December 23, 2008
    Publication date: December 30, 2010
    Applicant: Merck Patent Gesellschaft Mit Beschrankter Haftung
    Inventors: Stefan Bender, Lars Thore Burgdorf, Ulrich Emde, Norbert Beier, Johannes Gleitz, Christine Charon
  • Glucokinase Activators
    Publication number: 20100331338
    Abstract: Novel compounds of the Formula (I) in which R1, R2, R3, and R4 have the meanings indicated in Claim 1, are activators of glucokinase and can be used for the prevention and/or treatment of Diabetes Type 1 and 2, obesity, neuropathy and/or nephropathy.
    Type: Application
    Filed: February 2, 2009
    Publication date: December 30, 2010
    Applicant: Merck Patent GMBH
    Inventors: Lars Burgdorf, Ulrich Emde, Johannes Gleitz, Norbert Beier, Christine Charon
  • COMPOUNDS AND METHODS
    Publication number: 20100324086
    Abstract: A compound of formula (1) as well as pharmaceutically acceptable salts thereof, and a pharmaceutical composition comprising the compound. The compound is useful for the treatment of disorder from pain, fever, inflammation and cancer.
    Type: Application
    Filed: February 19, 2009
    Publication date: December 23, 2010
    Applicant: Novasaid AB
    Inventors: Johan Wannberg, Mathias Alterman, Patric Stenberg, Jacob Westman
  • HNF4alpha MODULATORS AND METHODS OF USE
    Publication number: 20100317706
    Abstract: Disclosed are methods and compositions relating to modulators, such as agonists and antagonists, of HNF4?.
    Type: Application
    Filed: April 30, 2010
    Publication date: December 16, 2010
    Applicant: Bumham Institute for Medical Research
    Inventors: Fred Levine, Marcia I. Dawson, Mao Ye
  • SUSTAINED-RELEASE TABLET COMPOSITION OF PRAMIPEXOLE
    Publication number: 20100316710
    Abstract: A sustained-release pharmaceutical composition in a form of an orally deliverable tablet comprises a water-soluble salt of pramipexole, dispersed in a matrix comprising a hydrophilic polymer and a starch having a tensile strength of at least about 0.15 kN cm?2 at a solid fraction representative of the tablet.
    Type: Application
    Filed: March 3, 2010
    Publication date: December 16, 2010
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Gregory Everett AMIDON, Loksidh Devi GANORKAR, John Mark HEIMLICH, Ernest J. LEE, Robert Martin NOACK, Joseph Peter REO, Connie Jo SKOUG
  • Parenteral and oral formulations of benzimidazoles
    Publication number: 20100310611
    Abstract: Provided herein are drug delivery systems, such as self-nanoemulsifying drug delivery systems, self-emulsifying drug delivery systems and parenteral microemulsion formulations, suitable for parenteral or oral delivery to a subject. The drug delivery systems may comprise a benzimidazole derivative, e.g., mebendazole, an oil, a surfactant, a cosurfactant and a dipolar aprotic solvent in a microemulsion formulation.
    Type: Application
    Filed: June 10, 2010
    Publication date: December 9, 2010
    Inventors: Diana Shu-Lian Chow, Pranav Gupta, Yulan Qi, Dong Liang
  • TRICYCLIC COMPOUNDS HAVING CORTICOTROPIN-RELEASING FACTOR ANTAGONISTIC ACTIVITY AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
    Publication number: 20100298287
    Abstract: There is provided a compound of the formula (I?): wherein X is a nitrogen or CRx, Rx is a hydrogen, etc., R1 is an optionally substituted hydrocarbon group, etc., R2 is an optionally substituted hydrocarbon group, etc., ring A is 5- to -8-membered heterocyclic ring, etc., and each of Y1, Y2 and Y3 is an optionally substituted carbon or a nitrogen, etc.; or ‘a salt thereof or a prodrug thereof, which have CRF receptor antagonistic activity and use thereof.
    Type: Application
    Filed: January 21, 2009
    Publication date: November 25, 2010
    Inventors: Kazuyoshi Aso, Katsumi Kobayashi, Takafumi Takai, Takuto Kojima, Kazuyuki Tokumaru, Michiyo Mochizuki, Yasutaka Hoashi