Chalcogen Attached Directly To The Carbocyclic Ring Of The Quinoline Ring System By Nonionic Bonding Patents (Class 546/177)
  • Patent number: 9181191
    Abstract: Compounds that have agonist activity at one or more of the S1P receptors are provided. The compounds are sphingosine analogs that, after phosphorylation, can behave as agonists at S1P receptors.
    Type: Grant
    Filed: October 5, 2012
    Date of Patent: November 10, 2015
    Assignee: BIOGEN MA INC.
    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
  • Publication number: 20150148301
    Abstract: The present invention relates to inhibitors of the activity of Complex (III) of the mitochondrial electron transport chain and use thereof in treatment and/or prevention of cancers presenting tumour-initiating cells. The present invention further relates to pharmaceutical compositions containing said inhibitors alone or in combination with other pharmaceutically active agents, and their use as medicaments or as agrochemicals where their properties as inhibitors of the mitochondrial respiration is of benefit.
    Type: Application
    Filed: May 23, 2013
    Publication date: May 28, 2015
    Inventors: Virginie Clement-Schatlo, Thomas Fessard, Damien Barbaras, Joana Matos, Erick Carreira
  • Publication number: 20150025056
    Abstract: The present invention provides compounds of the formula I: its enantiomers, diastereomers, racemic mixtures thereof, prodrugs, crystalline forms, non-crystalline forms, amorphous forms thereof, solvates thereof, metabolites thereof, and pharmaceutically acceptable salts, wherein the ring A substituent groups are fully defined in the following disclosure. The compounds of formula I are inhibitors of metalloproteases such as matrix metalloproteases and sheddases, and are useful in treating diseases such as rheumatoid arthritis, psoriasis, neoplastic diseases, allergies and all those diseases wherein inhibition of MMPs is desirable.
    Type: Application
    Filed: October 3, 2014
    Publication date: January 22, 2015
    Applicant: Incyte Corporation
    Inventors: Yun-Long Li, Jincong Zhuo, David M. Burns, Wenqing Yao, Ravi Kumar Jalluri
  • Publication number: 20150018334
    Abstract: The present invention relates to aryl pyrazoles, and pharmaceutically acceptable salts thereof. The aryl pyrazoles of the present invention are useful as inhibitors of leukotriene A4 hydrolase (LTA4H) and treating LTA4H related disorders. The present invention also relates to pharmaceutical compositions comprising the aryl pyrazoles of the present invention, methods of using these compounds in the treatment of various diseases and disorders, and processes for preparing these compounds.
    Type: Application
    Filed: July 14, 2014
    Publication date: January 15, 2015
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Asitha ABEYWARDANE, John BROADWATER, Steven Richard BRUNETTE, Thomas Martin KIRRANE, JR., Hossein RAZAVI, Robert SIBLEY, Lana Louise SMITH KEENAN, Qiang ZHANG
  • Patent number: 8906937
    Abstract: Methods of treating, preventing, and/or ameliorating a Flavivirus infection in a subject are disclosed. The methods comprise administering to the subject a therapeutically effective amount of a Flavivirus inhibitor, e.g., a Flavivirus serine protease inhibitor. These methods are useful in treating, preventing, and/or ameliorating Flavivirus infections such as, for example, West Nile Virus, Dengue Virus, and Japanese Encephalitis Virus.
    Type: Grant
    Filed: September 20, 2013
    Date of Patent: December 9, 2014
    Assignee: Georgetown University
    Inventors: Radhakrishnan Padmanabhan, Nagarajan Pattabiraman, Niklaus Mueller, Kuppuswamy Nagarajan
  • Publication number: 20140349986
    Abstract: The invention relates to substituted aminoindanes and analogs thereof of formula I and the pharmaceutical use thereof. Medicaments which comprise compounds of this type are suitable for the prevention or treatment of diverse disorders such as, for example, of respiratory disorders, cystic fibrosis disorders, acute or chronic renal disorders or bowel disorders.
    Type: Application
    Filed: July 24, 2014
    Publication date: November 27, 2014
    Applicant: SANOFI
    Inventors: Nils Rackelmann, Laurent Bialy, Heinrich Englert, Klaus Wirth, Petra Arndt, John Weston, Uwe Heinelt, Markus Follmann
  • Patent number: 8877776
    Abstract: Disclosed are malate salts of N-(4-{[6,7-bis(methyloxy)-quinolin-4-yl]oxy}phenyl)-N?-(4-fluorophenyl)cyclopropane -1,1-dicarboxamide, including a (L)-malate salt, a (D)-malate salt, a (DL) malate salt, and mixtures thereof; and crystalline and amorphous forms of the malate salts. Also disclosed are pharmaceutical compositions comprising at least one malate salts of N-(4-{[6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-N?-(4-fluorophenyl)-cyclopropane-1,1-dicarboxamide; and methods of treating cancer comprising administering at least one malate salt of N-(4-{[6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-N?-(4-ffuorophenyl)cyclopropane-1,1-dicarboxamide.
    Type: Grant
    Filed: January 15, 2010
    Date of Patent: November 4, 2014
    Assignee: Exelixis, Inc.
    Inventors: Adrian St. Clair Brown, Peter Lamb, William P. Gallagher
  • Publication number: 20140303203
    Abstract: Compounds and methods for treating or preventing a neurodegenerative disease, disorder or condition associated with the overall activity of hsp90 but not with the ATPase activity of hsp90, including peripheral neuropathy, such as peripheral neuropathy caused by chemotherapy or diabetes, disorders 5 of the central nervous system, such as Alzheimer's disease and Parkinsons disease, and motor neuron diseases, such as amyotrophic lateral sclerosis (ALS), in a subject are provided.
    Type: Application
    Filed: June 21, 2012
    Publication date: October 9, 2014
    Applicant: THE JOHNS HOPKINS UNIVERSITY
    Inventors: Ahmet Hoke, Weiran Chen, Jing Zhu
  • Publication number: 20140296251
    Abstract: Novel quinoline derivatives are disclosed. Also disclosed are synthesis and use thereof for treating neurodegenerative diseases.
    Type: Application
    Filed: April 2, 2013
    Publication date: October 2, 2014
    Applicant: Annji Pharmaceutical Co., Ltd.
    Inventors: Ji-Wang Chern, Chen-Wei Huang, Pei-Teh Chang, Rahul Subhash Talekar
  • Publication number: 20140296223
    Abstract: This invention relates to a method for regulating skin pigmentation of a subject, comprising the step of administering the agent for inhibiting the expression or activation of Microphthalmia Transcription Factor (MITF) to the subject who is in need of regulation of skin pigmentation.
    Type: Application
    Filed: August 31, 2012
    Publication date: October 2, 2014
    Applicant: THE GENERAL HOSPITAL CORPORATION
    Inventors: David E. Fisher, Rizwan Haq, Hans Ragnar Valdemar Widlund
  • Patent number: 8846864
    Abstract: The present invention relates to a series of compounds useful for effecting purification, in particular for use in purification of synthetic peptides and proteins. The compounds of the invention are particularly efficient at securely anchoring peptides or proteins to a surface and allowing the peptide or protein to become uniformly orientated, thus ensuring that substantially all of the peptide or protein is available for molecular binding to a substrate.
    Type: Grant
    Filed: March 16, 2011
    Date of Patent: September 30, 2014
    Assignee: Almac Sciences (Scotland) Limited
    Inventors: David William Anderson, Graham John Cotton, Alastair Mackie Hay, Paul William Armstrong, Ian Wilson
  • Patent number: 8802712
    Abstract: The invention relates to compounds of the formulae (I), (II) and (III), and/or physiologically acceptable salts, tautomers and stereoisomers thereof, including mixtures thereof in all ratios. The compounds of the formula (I) can be used for the inhibition of serine/threonine protein kinases and for the sensitisation of cancer cells to anticancer agents and/or ionising radiation. The invention also relates to the use of the compounds of the formula (I) in the prophylaxis, therapy or progress control of cancer, tumours, metastases or angiogenesis disorders, in combination with radiotherapy and/or an anticancer agent.
    Type: Grant
    Filed: June 24, 2011
    Date of Patent: August 12, 2014
    Assignee: Merck Patent GmbH
    Inventors: Thomas Fuchss, Werner Mederski, Frank Zenke
  • Publication number: 20140206876
    Abstract: Provided is a 2-(substituted ethynyl)quinoline derivative having an mGluR5 antagonistic activity and pharmaceutically acceptable salts thereof. The compound of the present invention can be useful as a medicament for treating and preventing mGluR5 receptor-mediated diseases such as Alzheimer's disease, senile dementia, Parkinson's disease, L-DOPA-induced dyskinesia, Huntington's chorea, amyotrophic lateral sclerosis, multiple sclerosis, schizophrenia, anxiety disorder, depression, neuropathic pain, drug dependence, fragile X syndrome, autism, migraine and gastroesophageal reflux disease (GERD).
    Type: Application
    Filed: July 16, 2013
    Publication date: July 24, 2014
    Inventors: Sun Joon MIN, Yong Seo CHO, Ae Nim PAE, Eun Jeong LIM, Ji Yeong KIM, Myung Hee SON, Jae Kyun LEE
  • Publication number: 20140186280
    Abstract: 8-Hydroxy-quinoline derivatives and 8-ethers, 8-esters, 8-carbonates, 8-acyloxymethyl, 8-phosphates, (phosphoryloxy)methyl, and 8-carbamates derivatives thereof are described that exhibit iron chelation, neuroprotective, neurorestorative, apoptotic and/or selective MAO-AB inhibitory activities.
    Type: Application
    Filed: March 4, 2014
    Publication date: July 3, 2014
    Inventors: Vincent R. ZURAWSKI, JR., David M. STOUT, Theodore J. NITZ, Moussa B.H. YOUDIM, Orly WEINREB
  • Publication number: 20140163069
    Abstract: Provided herein are compounds having anti-proliferative effect. Also provided are compounds that can modulate the activity of multi-domain proteins comprising a dimerization arm and interdomain tether, such as EGFR, where an untethered, extended conformation is the active state and a tethered conformation is the inactive state, resulting in an autoinhibited configuration. Also provided are methods and pharmacophores for identifying such compounds. Other aspects provide methods or therapeutic treatment for proliferative diseases, disorders, or conditions, such as those associated with EGFR.
    Type: Application
    Filed: December 4, 2013
    Publication date: June 12, 2014
    Inventor: Joseph P. Errico
  • Publication number: 20140157443
    Abstract: Provided herein is a novel mTOR-comprising complex, mT-ORC3, which comprises mTOR and the Ets transcription factor TEL2. Specific mTORC3 binding agents and modulating agents are provided, along with kits and methods for the detection of mTORC3. Methods of modulating the activity of mTORC3 or modulating cell growth and/or survival are also provided. Further provided are methods for screening for mTORC3 binding agents and for mTORC3 modulating agents. Various methods of diagnosis and treatment are further provided.
    Type: Application
    Filed: April 12, 2012
    Publication date: June 5, 2014
    Applicant: ST. JUDE CHILDREN'S RESEARCH HOSPITAL
    Inventors: Gerard C. Grosveld, Frank C. Harwood, Ramon I. Klein-Geltink
  • Publication number: 20140155362
    Abstract: Embodiments of the present disclosure provide for BHQ-conjugates and protected BHQ-conjugate precursor compounds, methods of making BHQ-conjugates and protected BHQ-conjugate precursor compounds, methods of using BHQ-conjugates and protected BHQ-conjugate precursor compounds, and the like.
    Type: Application
    Filed: June 28, 2012
    Publication date: June 5, 2014
    Inventors: Timothy M. Dore, James D. Lauderdale, Adam C. Rea, Adna Muliawan, Duncan McLain
  • Publication number: 20140100195
    Abstract: Compounds that have agonist activity at one or more of the S1P receptors are provided. The compounds are sphingosine analogs that, after phosphorylation, can behave as agonists at S1P receptors.
    Type: Application
    Filed: October 5, 2012
    Publication date: April 10, 2014
    Inventors: Richard D. Caldwell, Kevin M. GUCKIAN, Gnanasambandam KUMARA VEL, Wen-Cherng LEE, Edward Yin-Shiang LIN, Xiaogao LlU, Bin MA, Daniel M. SCOTT, Zhan SHl, Jermaine THOMAS, Arthur G. TAVERAS, Guo Zhu ZHENG
  • Publication number: 20140038962
    Abstract: Methods of treating, preventing, and/or ameliorating a Flavivirus infection in a subject are disclosed. The methods comprise administering to the subject a therapeutically effective amount of a Flavivirus inhibitor, e.g., a Flavivirus serine protease inhibitor. These methods are useful in treating, preventing, and/or ameliorating Flavivirus infections such as, for example, West Nile Virus, Dengue Virus, and Japanese Encephalitis Virus.
    Type: Application
    Filed: September 20, 2013
    Publication date: February 6, 2014
    Applicant: GEORGETOWN UNIVERSITY
    Inventors: Radhakrishnan Padmanabhan, Nagarajan Pattabiraman, Niklaus Mueller, Kuppuswamy Nagarajan
  • Patent number: 8618302
    Abstract: Provided herein are compounds having anti-proliferative effect. Also provided are compounds that can modulate the activity of multi-domain proteins comprising a dimerization arm and interdomain tether, such as EGFR, where an untethered, extended conformation is the active state and a tethered conformation is the inactive state, resulting in an autoinhibited configuration. Also provided are methods and pharmacophores for identifying such compounds. Other aspects provide methods or therapeutic treatment for proliferative diseases, disorders, or conditions, such as those associated with EGFR.
    Type: Grant
    Filed: January 6, 2011
    Date of Patent: December 31, 2013
    Inventors: Joseph P. Errico, Benjamin Mugrage, Ignatius Turchi, Matthew Sills, Jane Ong, John Allocco, Pam Wines
  • Publication number: 20130338105
    Abstract: Compounds of the formula I in which the substituents are as defined in claim 1 are suitable for use as microbiocides.
    Type: Application
    Filed: August 20, 2013
    Publication date: December 19, 2013
    Inventors: Paul Anthony Worthington, Daniel Stierli, Fredrik Cederbaum, Kurt Nebel, Antoine Daina
  • Publication number: 20130330284
    Abstract: 8-Hydroxy-quinoline derivatives and 8-ethers, 8-esters, 8-carbonates, 8-acyloxymethyl, 8-phosphates, (phosphoryloxy)methyl, and 8-carbamates derivatives thereof are described that exhibit iron chelation, neuroprotective, neurorestorative, apoptotic and/or selective MAO-AB inhibitory activities.
    Type: Application
    Filed: August 12, 2011
    Publication date: December 12, 2013
    Applicant: VARINEL INC
    Inventors: Vincent R. Zurawski, David M. Stout, Theodore J. Nitz, Moussa B.H. Youdim, Orly Weinreb
  • Publication number: 20130281366
    Abstract: The present invention relates to compounds of the general formula (I), their tautomeric forms, their stereoisomers, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, methods for their preparation, use of these compounds in medicine and the intermediates involved in their preparation. The present invention is directed towards compounds which can be used to treat diseases such as Hyperlipidemia and also have a beneficial effect on cholesterol.
    Type: Application
    Filed: December 26, 2011
    Publication date: October 24, 2013
    Applicant: CADILA HEALTHCARE LIMITED
    Inventors: Harikishore Pingali, Pankaj Makadia, Vrajesh Pankaj, Sairam Kalapatapu, V.V.M., Mukul R. JAIN
  • Publication number: 20130211047
    Abstract: The present invention relates to a series of compounds useful for effecting purification, in particular for use in purification of synthetic peptides and proteins. The compounds of the invention are particularly efficient at securely anchoring peptides or proteins to a surface and allowing the peptide or protein to become uniformly orientated, thus ensuring that substantially all of the peptide or protein is available for molecular binding to a substrate.
    Type: Application
    Filed: March 16, 2011
    Publication date: August 15, 2013
    Applicant: ALMAC SCIENCES (SCOTLAND) LIMITED
    Inventors: David William Anderson, Graham John Cotton, Alastair Mackie Hay, Paul William Armstrong, Ian Wilson
  • Publication number: 20130203756
    Abstract: The present invention is directed to isoindolinone compounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.
    Type: Application
    Filed: October 24, 2011
    Publication date: August 8, 2013
    Inventors: Jamie L. Bunda, Christopher D. Cox, Vadim Y. Dudkin, Hannah D. Fiji, Michael J. Kelly, Mark E. Layton, Joseph E. Pero, William D. Shipe, Justin T. Sheen
  • Patent number: 8486931
    Abstract: The present invention relates to compounds of the general formula (I) in which A, B, R1, R2 and Het have the meaning given in claim 1; Y is a bivalent group of the formula in which D is C1-C3-alkylene, where D may have a substituent R5; R3 is hydrogen, C1-C8-alkyl or together with R4 is C1-C3-alkylene which may have a radical R5a, or together with R5 is C1-C3-alkylene, and R4 is hydrogen, C1-C8-alkyl or together with R3 is C1-C3-alkylene which may have a radical R5a, or together with R5 is C1-C3-alkylene, where R5 together with R5a, where present, are a bond or C1-C3-alkylene; and where one of the following conditions is satisfied: R3 together with R4 is C1-C3-alkylene which may have a radical R5a; or R3 together with R5 is C1-C3-alkylene; or R4 together with R5 is C1-C3-alkylene where the radical A is different from phenyl when the radical B is phenyl or naphthyl; and medicaments which comprise such compounds and the use thereof for the prophylaxis and/or treatment of vasopressin-dependent and/o
    Type: Grant
    Filed: February 29, 2008
    Date of Patent: July 16, 2013
    Assignee: Abbott GmbH & Co. KG
    Inventors: Herve Genesle, Thorsten Oost, Charles W. Hutchins, Liliane Unger, Wilfried Hornberger, Wilfried Lubisch, Astrid Netz, Alfred Hahn
  • Publication number: 20130150359
    Abstract: The invention relates to compounds of the formulae (I), (II) and (III), and/or physiologically acceptable salts, tautomers and stereoisomers thereof, including mixtures thereof in all ratios. The compounds of the formula (I) can be used for the inhibition of serine/threonine protein kinases and for the sensitisation of cancer cells to anticancer agents and/or ionising radiation. The invention also relates to the use of the compounds of the formula (I) in the prophylaxis, therapy or progress control of cancer, tumours, metastases or angiogenesis disorders, in combination with radiotherapy and/or an anticancer agent.
    Type: Application
    Filed: June 24, 2011
    Publication date: June 13, 2013
    Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNG
    Inventors: Thomas Fuchss, Werner Mederski, Frank Zenke
  • Publication number: 20130137112
    Abstract: Provided are dyes and compositions which are useful in a number of applications, such as the detection and monitoring protein aggregation, kinetic studies of protein aggregation, neurofibrillary plaques analysis, evaluation of protein formulation stability, and analysis of molecular chaperone activity.
    Type: Application
    Filed: November 30, 2010
    Publication date: May 30, 2013
    Inventors: Wayne Forrest Patton, Sergiy M. Yarmoluk, Praveen Pande, Vladyslava Kovalska, Lijun Dai, Kateryna Volkova, Jack Coleman, Mykhaylo Losytskyy, Anthony Ludlam, Anatoliy Balanda, Dee Shen
  • Publication number: 20130131096
    Abstract: The invention relates to compounds of the general formula (I) and their pharmaceutically acceptable salts (in which formula R1 represents a hydrogen atom, lower alkyl group, lower alkenyl group, lower cycloalkyl group, aryl group, aralkyl group or heterocyclic group, wherein, the above groups are optionally substituted in ortho, meta and/or para position with 1, 2, 3 or 4 electron withdrawing groups or electron donating groups; R2 represents a hydrogen atom, lower alkyl group, aryl group, aralkyl group or heterocyclic group wherein the above groups are optionally substituted with one or more halogen atoms; R3 represents a lower alkyl group, aryl group, aralkyl group or heterocyclic group wherein the above groups are optionally substituted in ortho, meta or para position with 1, 2, 3 or 4 electron withdrawing groups or electron donating groups; R4 represents a hydrogen atom, lower alkyl group or any acidic functional group; n is 1 or 2).
    Type: Application
    Filed: May 6, 2011
    Publication date: May 23, 2013
    Inventors: Laszlo Puskas, Csaba Szabo, Ivan Kanizsai, Mario Gyuris, Ramona Madacsi, Bela Ozsvari, Liliana Feher, Gabor Tamas
  • Publication number: 20120329802
    Abstract: The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.
    Type: Application
    Filed: June 20, 2012
    Publication date: December 27, 2012
    Applicant: VIAMET PHARMACEUTICALS, INC.
    Inventors: William J. Hoekstra, Robert J. Schotzinger
  • Publication number: 20120277242
    Abstract: Provided are compounds of Formula (I): wherein R2, R3, R13, L and D2 are as defined in the specification, which are useful in the treatment and/or prevention of diseases or disorders mediated by deficient levels of glucokinase activity or which can be treated by activating glucokinase including, but not limited to, diabetes mellitus, impaired glucose tolerance, IFG (impaired fasting glucose) and IFG (impaired fasting glycemia), as well as other diseases and disorders such as those discussed herein.
    Type: Application
    Filed: June 11, 2012
    Publication date: November 1, 2012
    Applicant: ARRAY BIOPHARMA, INC.
    Inventors: Thomas Daniel AICHER, Steven Armen BOYD, Mark Joseph CHICARELLI, Kevin Ronald CONDROSKI, Jay Bradford FELL, John P. FISCHER, Indrani W. GUNAWARDANA, Ronald Jay HINKLIN, Ajay SINGH, Timothy M. TURNER, Eli M. WALLACE
  • Patent number: 8293732
    Abstract: The present invention relates to novel substituted quinoline derivatives according to the general Formula (Ia) or Formula (Ib): including any stereochemically isomeric form thereof, a N-oxide thereof, a pharmaceutically acceptable salt thereof or a solvate thereof. The claimed compounds are useful for the treatment of a bacterial infection. Also claimed is a composition comprising a pharmaceutically acceptable carrier and, as active ingredient, a therapeutically effective amount of the claimed compounds, the use of the claimed compounds or compositions for the manufacture of a medicament for the treatment of a bacterial infection and a process for preparing the claimed compounds.
    Type: Grant
    Filed: December 4, 2007
    Date of Patent: October 23, 2012
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Jérôme Emile Georges Guillemont, Ismet Dorange, Magali Madeleine Simone Motte, Koenraad Jozef Lodewijk Marcel Andries, Anil Koul
  • Publication number: 20120252770
    Abstract: Compounds of formula (I): The present invention relates to novel indazolyl ester or amide derivatives, to pharmaceutical compositions comprising such derivatives, to processes for preparing such novel derivatives and to the use of such derivatives as medicaments
    Type: Application
    Filed: March 23, 2012
    Publication date: October 4, 2012
    Inventors: Markus Berger, Jan Dahmén, Karl Edman, Anders Eriksson, Balint Gabos, Thomas Hansson, Martin Hemmerling, Krister Henriksson, Svetlana Ivanova, Matti Lepistö, Darren McKerrencher, Magnus Munck af Rosenschöld, Stinabritt Nilsson, Hartmut Rehwinkel, Camilla Taflin
  • Publication number: 20120189537
    Abstract: Disclosed are nitrile derivatives and pharmaceutical compositions comprising nitrile derivatives. The pharmaceutical compositions comprise compounds of the formula I and the pharmaceutically acceptable salts of such compounds. Also disclosed are processes for the preparation of such compounds, intermediates used in the preparation of such compounds, and the uses of such compounds in treating hyperproliferative diseases, inflammatory diseases and viral and bacterial infections and inducing apoptosis in cancer cells.
    Type: Application
    Filed: November 22, 2011
    Publication date: July 26, 2012
    Inventor: Krishna Menon
  • Publication number: 20120129886
    Abstract: The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.
    Type: Application
    Filed: November 10, 2011
    Publication date: May 24, 2012
    Applicant: Viamet Pharmaceuticals, Inc.
    Inventors: William J. Hoekstra, Robert J. Schotzinger, Stephen W. Rafferty
  • Publication number: 20110312911
    Abstract: Glucagon receptor antagonist compounds are disclosed. The compounds are useful for treating type 2 diabetes and related conditions. Pharmaceutical compositions and methods of treatment are also included.
    Type: Application
    Filed: February 3, 2010
    Publication date: December 22, 2011
    Inventors: Roman Kats-Kagan, Christian P. Stevenson, Xibin Liao, Qinghong Fu, Emma R. Parmee, Songnian Lin
  • Publication number: 20110301193
    Abstract: Provided herein are compounds having anti-proliferative effect. Also provided are compounds that can modulate the activity of multi-domain proteins comprising a dimerization arm and interdomain tether, such as EGFR, where an untethered, extended conformation is the active state and a tethered conformation is the inactive state, resulting in an autoinhibited configuration. Also provided are methods and pharmacophores for identifying such compounds. Other aspects provide methods or therapeutic treatment for proliferative diseases, disorders, or conditions, such as those associated with EGFR.
    Type: Application
    Filed: January 6, 2011
    Publication date: December 8, 2011
    Inventors: Joseph P. Errico, Benjamin Mugrage, Ignatius Turchi, Matthew Sills, Jane Ong, John Allocco, Pam Wines
  • Publication number: 20110301163
    Abstract: Described herein are methods of inhibiting methionine aminopeptidase or SirT1, inhibiting angiogenesis, and treating disorders (or symptoms thereof) associated with methionine aminopeptidase, SirT1 and/or angiogenesis, wherein a compound of the invention is administered to a subject.
    Type: Application
    Filed: October 6, 2009
    Publication date: December 8, 2011
    Applicant: THE JOHNS HOPKINS UNIVERSITY
    Inventors: Jun O. Liu, Joong Sup Shim, Curtis R. Chong, Shridhar Bhat
  • Publication number: 20110294848
    Abstract: The invention provides potent quinolinol-based BoNT/A small-molecule inhibitors of botulinum neurotoxins, in particular of Clostridium botulinum serotype A neurotoxins. The invention also provides methods of using these small-molecule inhibitors to inhibit infections by Clostridium botulinum, as well as, methods of preventing infections by Clostridium botulinum through materials that may be ingested.
    Type: Application
    Filed: May 28, 2009
    Publication date: December 1, 2011
    Inventors: Virginia I. Roxas-Duncan, Leonard A. Smith, Nizamettin Gul, John H. Cardellina, II, Rebecca C. Vieira, Susan M. Ensel, David C.H. Yang, Istvan J. Enyedy, Sivanesan Darkshanamurthy, Salimuddin Shah
  • Publication number: 20110281909
    Abstract: The present invention relates to compounds of formula (I), and salts thereof, processes for their preparation, to compositions containing them and to their use in the treatment of various diseases, such as allergic rhinitis.
    Type: Application
    Filed: August 13, 2008
    Publication date: November 17, 2011
    Applicant: GLAXO GROUP LIMITED
    Inventors: Paul Martin Gore, Ashley Paul Hancock, Simon Teanby Hodgson, Panayiotis Alexandrou Procopiou, Sadie Vile
  • Publication number: 20110243850
    Abstract: Provided is a novel probe for a biological specimen for labelling by itself and clearly visualizing one of a specific cell and a specific cell organ in a living body, the probe having excellent spectral characteristics and exhibiting excellent storage stability. The probe for a biological specimen contains, as an active agent, at least one kind of compound represented by a general formula (I).
    Type: Application
    Filed: December 24, 2009
    Publication date: October 6, 2011
    Applicant: CANON KABUSHIKI KAISHA
    Inventors: Taichi Shintou, Takeshi Miyazaki, Masashi Hirose, Taketoshi Okubo, Kohei Watanabe, Tsuyoshi Nomoto, Toshio Tanaka, Yuhei Nishimura, Yasuhito Shimada, Norihiro Nishimura
  • Publication number: 20110224207
    Abstract: Methods of treating, preventing, and/or ameliorating a Flavivirus infection in a subject are disclosed. The methods comprise administering to the subject a therapeutically effective amount of a Flavivirus inhibitor, e.g., a Flavivirus serine protease inhibitor. These methods are useful in treating, preventing, and/or ameliorating Flavivurs infections such as, for example, West Nile Virus, Dengue Virus, and Japanese Encephalitis Virus.
    Type: Application
    Filed: September 23, 2009
    Publication date: September 15, 2011
    Applicant: GEORGETOWN UNIVERSITY
    Inventors: Radhakrishnan Padmanabhan, Nagarajan Pattabiraman, Niklaus Mueller, Kuppuswamy Nagarajan
  • Patent number: 7964729
    Abstract: Peptidyl sensors comprise a metal-binding peptide and one or two kinase recognition sequences with a hydroxyamino acid that can be phosphorylated in the presence of a kinase.
    Type: Grant
    Filed: August 28, 2006
    Date of Patent: June 21, 2011
    Assignee: Massachusetts Institute of Technology
    Inventors: Barbara Imperiali, Elvedin Lukovic, Dora Carrico-Moniz
  • Patent number: 7947711
    Abstract: Compounds of formula (I) are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Also disclosed are pharmaceutical compositions comprising the histamine-3 receptor ligands, methods for using such compounds and compositions, and a process for preparing compounds within the scope of formula (I).
    Type: Grant
    Filed: August 21, 2008
    Date of Patent: May 24, 2011
    Assignee: Abbott Laboratories
    Inventors: Marlon D. Cowart, Yu-ming Pu, Yi-Yin Ku
  • Publication number: 20110092480
    Abstract: Compounds of the general Formula I, wherein X1, X2, X3, X4, X5, X6, X7, R1, R2, R4, R5, R6, R7, R8, R9, R10, Y1, n, m, p and q are defined as above, their preparation and their use as antimicrobial agents.
    Type: Application
    Filed: December 20, 2010
    Publication date: April 21, 2011
    Inventors: Steven Joseph Brickner, Jinshan Michael Chen, Zhengong Bryan Li, Anthony Marfat, Mark Joseph Mitton-Fry, Michael A. Plotkin, Usa Datta Reilly, Chakrapani Subramanyam, Zhijun Zhang, Shaughnessy Robinson
  • Publication number: 20100304966
    Abstract: Compounds of the formula I in which the substituents have the meaning given in the description, processes for preparing these compounds, compositions comprising them and their use for controlling harmful fungi.
    Type: Application
    Filed: October 9, 2008
    Publication date: December 2, 2010
    Applicant: BASF SE
    Inventors: Joachim Rheinheimer, Barbara Nave, Doris Kremzow, Stefan Redlich, Christian Pilger, Claudia Rosenbaum, Wassilios Grammenos
  • Publication number: 20100222349
    Abstract: The present invention relates to compounds of formula (I) and salts thereof, processes for their preparation, to compositions containing them and to their use in the treatment of various diseases, such as allergic rhinitis.
    Type: Application
    Filed: October 15, 2008
    Publication date: September 2, 2010
    Applicant: Glaxo Group Limited
    Inventors: Paul Martin Gore, Ashley Paul Hancock, Simon Teanby Hodgson, Michael Joachim Kranz, Panayiotis Alexandrou Procopiou, Sadie Vile
  • Publication number: 20100204240
    Abstract: Provided are compounds of Formula (I): wherein R2, R3, R13, L and D2 are as defined in the specification, which are useful in the treatment and/or prevention of diseases or disorders mediated by deficient levels of glucokinase activity or which can be treated by activating glucokinase including, but not limited to, diabetes mellitus, impaired glucose tolerance, IFG (impaired fasting glucose) and IFG (impaired fasting glycemia), as well as other diseases and disorders such as those discussed herein.
    Type: Application
    Filed: September 15, 2008
    Publication date: August 12, 2010
    Applicant: ARRAY BIOPHARMA INC.
    Inventors: Thomas Daniel Aicher, Steven Armen Boyd, Mark Joseph Chicarelli, Kevin Ronald Condroski, Jay Bradford Fell, John P. Fischer, Indrani W. Gunawardana, Ronald Jay Hinklin, Ajay Singh, Timothy M. Tumer, Eli M. Wallce
  • Patent number: 7772232
    Abstract: A compound of formula I wherein m, n, A, B, D, E, G, H, Y, R1, R2, R3, R4, R5, and R8, are described herein. Said compounds being useful as inhibitors of potassium channel function and in the treatment of arrhythmia, IKur-associated disorders, and other disorders mediated by ion channel function.
    Type: Grant
    Filed: April 13, 2005
    Date of Patent: August 10, 2010
    Assignee: Bristol-Myers Squibb Company
    Inventors: James A. Johnson, John Lloyd
  • Patent number: 7767672
    Abstract: The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising those compounds and methods of using the compounds and compositions in the treatment of various disease, conditions, and disorders. The invention also provides processes for preparing compounds of the invention.
    Type: Grant
    Filed: November 3, 2006
    Date of Patent: August 3, 2010
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Hayley Binch, Michael Mortimore, Chris Davis, Dean Boyall, Simon Everitt, Daniel Robinson, Sharn Ramaya, Damien Fraysse, John Studley, Andrew Miller, Michael O'Donnell, Alistair Rutherford, Joanne Pinder