Nitrogen Bonded Directly To Ring Carbon Of The Hetero Ring Patents (Class 514/245)
  • Patent number: 8822448
    Abstract: The present inventors have investigated a compound which has a PDE9-inhibiting action and is useful as an active ingredient for an agent for treating and/or preventing storage dysfunction, voiding dysfunction, bladder/urethral diseases, and the like, and thus, have found that a pyrazoloquinoline compound has a PDE9-inhibiting action, thereby completing the present invention.
    Type: Grant
    Filed: March 7, 2013
    Date of Patent: September 2, 2014
    Assignee: Astellas Pharma Inc.
    Inventors: Hiroyuki Kaizawa, Hirofumi Yamamoto, Kazunori Kamijo, Mari Sugita, Ryushi Seo, Satoshi Yamamoto, Atsushi Ukai
  • Patent number: 8822464
    Abstract: This invention relates to compounds of formula I their use as positive allosteric modulators of mGlu5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline such as dementia or cognitive impairment. A, B, Ar, R1, R2, R3 have meanings given in the description.
    Type: Grant
    Filed: November 26, 2012
    Date of Patent: September 2, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Matthias Grauert, Daniel Bischoff, Georg Dahmann, Raimund Kuelzer, Klaus Rudolf
  • Publication number: 20140243273
    Abstract: The present invention provides method of treating or lessening the severity of a disease selected from spondyloarthropathy, systemic lupus erythematosus, rheumatoid arthritis, or any combination thereof comprising the administration of a compound of Formula I and an optional co-therapy (e.g., chemotherapy agent, DMARD, or any combination thereof). The present invention also provides a pharmaceutical composition comprising a compound of Formula I, a method of manufacturing a pharmaceutical composition comprising a compound of Formula I, and a method of administering a pharmaceutical composition comprising a solid form of a compound of Formula I.
    Type: Application
    Filed: May 7, 2014
    Publication date: August 28, 2014
    Applicant: Vertex Pharmaceuticals Incorporated
    Inventors: Irina Nikolaevna Kadiyala, Shahla Jamzad, Thomas Carl Hoock, Lori Kell Taylor, Kathryn Lea Sewell
  • Publication number: 20140235442
    Abstract: A composition comprising at least a pyridylethylbenzamide derivative of general formula (I) (a) and an insecticide compound (b) in a (a)/(b) weight ratio of from 1/1000 to 1000/1. A composition further comprising an additional fungicidal compound. A method for preventively or curatively combating the pests and diseases of crops by using this composition.
    Type: Application
    Filed: April 25, 2014
    Publication date: August 21, 2014
    Inventors: Heike HUNGENBERG, Gilbert LABOURDETTE, Albert SCHIRRING, Burkhard SCHUETZ, Anne SUTY-HEINZE, Wolfgang THIELERT, Martin VAUPEL
  • Publication number: 20140228338
    Abstract: The topical ophthalmic use of certain 2,4-diamino-substituted 1,3-triazines for preventing or alleviating ocular pain in patients is disclosed. Topcial ocular pharmaceutical composition are also disclosed.
    Type: Application
    Filed: February 13, 2014
    Publication date: August 14, 2014
    Applicant: Novartis AG
    Inventors: Martha E. Gadd, Peter G. Klimko, Karen C. David, Kenneth C. Appell, Mark R. Hellberg
  • Publication number: 20140227260
    Abstract: The present invention relates to new aminopyrimidine inhibitors of tyrosine kinase activity, pharmaceutical compositions thereof, and methods of use thereof.
    Type: Application
    Filed: April 21, 2014
    Publication date: August 14, 2014
    Applicant: Auspex Pharmaceuticals, Inc.
    Inventor: Chengzhi Zhang
  • Patent number: 8795701
    Abstract: The invention relates to a method for improving the utilization of the production potential of transgenic plants which comprises treating the plant with active compound combinations comprising an active compound from the group of the anthranilamides and at least one further insecticide.
    Type: Grant
    Filed: April 8, 2008
    Date of Patent: August 5, 2014
    Assignee: Bayer CropScience AG
    Inventors: Wolfram Andersch, Christian Funke, Heike Hungenberg, Wolfgang Thielert
  • Patent number: 8796449
    Abstract: Novel s-triazine compounds are disclosed that have a formula represented by the following: L1, L2, L3, R1, R2, R3, R4, R5a, R5b, and R5c are as described herein. The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, where microbial infection is either a direct cause or a related condition.
    Type: Grant
    Filed: March 17, 2011
    Date of Patent: August 5, 2014
    Assignee: New York University
    Inventor: Neville Robert Kallenbach
  • Patent number: 8791115
    Abstract: The present invention relates to combinations of triazine derivatives and of insulin sensitizers.
    Type: Grant
    Filed: December 18, 2006
    Date of Patent: July 29, 2014
    Assignee: Poxel SAS
    Inventors: Gérard Moinet, Daniel Cravo, Didier Mesangeau
  • Patent number: 8791049
    Abstract: Provided are improved agricultural processes for the improved cultivation of rice wherein the crops are treated to control undesired vegetative growth using a plant treatment composition comprising both halosulfuron and thifensulfuron to provide improved herbicidal efficacy against Heteranthera limosa, commonly referred to as “duck salad”. Also provided are compositions useful in the improved agricultural processes, as well as herbicidal treatment regimens. Unexpectedly high rates of efficacy against Heteranthera limosa, amongst rice plant in rice crops are disclosed.
    Type: Grant
    Filed: December 13, 2010
    Date of Patent: July 29, 2014
    Assignee: Gowan Co.
    Inventors: Eric Paige Webster, Dominic Frank Alonso, Sergio Comparini, Wallace Keith Majure, Sandra Alcaraz, Charles Paul Grasso, Eric James McEwen, Tak Wai Cheung
  • Publication number: 20140206633
    Abstract: The present invention relates to processes for the preparation of compounds of formula IB wherein A1, A2, A3, A4, L, Y1, Y2, R1, R2, R3, R4 and R5 are as defined in the claims, comprising reacting a compound of formula (II) wherein Y1, Y2, L, A1, A2, R1, R2, R3, R4 and R5 are as defined for the compound of formula (I); with hydroxylamine in the presence of water, a base and a chiral phase transfer catalyst, which chiral phase transfer catalyst is a quinine derivative. The invention also relates to compounds of formula IB and enantiomerically enriched mixtures comprising compounds of formula IB.
    Type: Application
    Filed: February 3, 2011
    Publication date: July 24, 2014
    Applicant: SYNGENTA CROP PROTECTION LLC
    Inventors: Nicholas Phillip Mulholland, Edouard Godineau, Jérôme Yves Cassayre, Peter Renold, Myriem El Qacemi, Guillaume Revol
  • Patent number: 8778835
    Abstract: A composition comprising at least a pyridylethylbenzamide derivative of general formula (I) (a) and an insecticide compound (b) in a (a)/(b) weight ratio of from 1/1000 to 1000/1. A composition further comprising an additional fungicidal compound. A method for preventively or curatively combating the pests and diseases of crops by using this composition.
    Type: Grant
    Filed: July 5, 2007
    Date of Patent: July 15, 2014
    Assignee: Bayer Cropscience AG
    Inventors: Heike Hungenberg, Gilbert Labourdette, Albert Schirring, Burkhard Schuetz, Anne Suty-Heinze, Wolfgang Thielert, Martin Vaupel
  • Patent number: 8778836
    Abstract: This invention relates to a new herbicidal composition comprising desmedipham and optionally phenmedipham and/or ethofumesate.
    Type: Grant
    Filed: April 25, 2013
    Date of Patent: July 15, 2014
    Assignee: Bayer Cropscience LP
    Inventor: David A. Long
  • Patent number: 8778837
    Abstract: The invention relates to the novel use of known active substance combinations which consist firstly of 3,4-dichloro-2?-cyano-1,2-thiazole-5-carboxanilide, of the formula which is known, and secondly further known insecticidal active substances, for controlling animal pests, especially arthropods, in particular insects.
    Type: Grant
    Filed: November 27, 2008
    Date of Patent: July 15, 2014
    Assignee: Bayer CropScience AG
    Inventors: Lutz Assmann, Ulrike Wachendorff-Neumann, Heike Hungenberg, Wolfgang Thielert
  • Publication number: 20140194429
    Abstract: Compounds that are specifically toxic to cancer stem cells are disclosed.
    Type: Application
    Filed: March 13, 2013
    Publication date: July 10, 2014
    Inventors: Feridoun KARIMI-BUSHERI, Habib FAKHRAI
  • Publication number: 20140193519
    Abstract: The invention provides combination therapy, wherein one or more other therapeutic agents are administered with indibulin or a pharmaceutically acceptable salt thereof and the combination is synergistic. Another aspect of the invention relates to the treatment of cancer with indibulin as a single agent. Another aspect of the invention relates to dosing regimen for administration of oral dosage forms of indibulin.
    Type: Application
    Filed: August 2, 2013
    Publication date: July 10, 2014
    Applicant: ZIOPHARM ONCOLOGY, INC.
    Inventors: Barbara P. Wallner, Brian Eric Schwartz, Philip B. Komarnitsky, Gerald Bacher, Bernhard Kutscher, Gerhard Raab
  • Patent number: 8765944
    Abstract: The disclosure provides compounds of formula I, including pharmaceutically acceptable salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.
    Type: Grant
    Filed: August 16, 2011
    Date of Patent: July 1, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: Li-Qiang Sun, Eric Mull, Qian Zhao, Tao Wang, Zhongxing Zhang, Paul Michael Scola
  • Publication number: 20140179637
    Abstract: A compound having an antiviral activity for inhibiting release of an enveloped virus from a cell is disclosed, including methods of inhibiting release of an enveloped virus from a cell. The antiviral activity of the compound includes inhibiting formation of an associative complex or disrupting formation of an associative complex. The associative complex comprises an L-domain motif of the enveloped virus and at least one cellular polypeptide, or fragment thereof, capable of binding the L-domain motif of the enveloped virus.
    Type: Application
    Filed: December 21, 2013
    Publication date: June 26, 2014
    Applicants: The Research Foundation for The State University of New York, Northwestern University
    Inventors: Jonathan Leis, Carol Carter
  • Publication number: 20140179662
    Abstract: The present invention relates to disubstituted triazine derivatives and/or pharmaceutically acceptable salts thereof, the use of these derivatives as pharmaceutically active agents, especially for the prophylaxis and/or treatment of infectious diseases, including opportunistic diseases, immunological diseases, autoimmune diseases, cardiovascular diseases, cell proliferative diseases, inflammation, erectile dysfunction and stroke, and pharmaceutical compositions containing at least one of said disubstituted triazine derivatives and/or pharmaceutically acceptable salts thereof. Furthermore, the present invention relates to the use of said disubstituted triazine derivatives as inhibitors for a protein kinase.
    Type: Application
    Filed: March 1, 2012
    Publication date: June 26, 2014
    Applicants: LEAD DISCOVERY CENTER GMBH, BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Gerd Rühter, Uwe Koch, Peter Nussbaumer, Carsten Schulz-Fademrecht, Jan Eickhoff
  • Publication number: 20140179697
    Abstract: Disubstituted octahydropyrrolo[3,4-c]pyrrole compounds are described, which are useful as orexin receptor modulators. Such compounds may be useful in pharmaceutical compositions and methods for the treatment of diseased states, disorders, and conditions mediated by orexin activity, such as insomnia.
    Type: Application
    Filed: December 23, 2013
    Publication date: June 26, 2014
    Applicant: JANSSEN PHARMACEUTICA NV
    Inventors: Wenying Chai, Michael A. Letavic, Kiev S. Ly, Daniel J. Pippel, Dale A. Rudolph, Kathleen C. Sappey, Brad M. Savall, Chandravadan R. Shah, Brock T. Shireman, Akinola Soyode Johnson, Emily M. Stocking, Devin M. Swanson
  • Publication number: 20140171430
    Abstract: Disubstituted octahydropyrrolo[3,4-c]pyrrole compounds are described, which are useful as orexin receptor modulators. Such compounds may be useful in pharmaceutical compositions and methods for the treatment of diseased states, disorders, and conditions mediated by orexin activity, such as insomnia.
    Type: Application
    Filed: April 20, 2012
    Publication date: June 19, 2014
    Applicant: JANSSEN PHARMACEUTICA NV
    Inventors: Michael A. Letavic, Rudolph A. Dale, Brad M. Savall, Brock T. Shireman, Devin Swanson
  • Patent number: 8754084
    Abstract: The invention provides compounds, compositions and methods for treating myotonic dystrophy. The compounds can selectively bind to CUG repeats in RNA, or to CTG repeats in DNA, and inhibit replication of the nucleic acids.
    Type: Grant
    Filed: March 27, 2013
    Date of Patent: June 17, 2014
    Assignee: The Board of Trustees of the University of Illinois
    Inventors: Steven C. Zimmerman, Chun-Ho Wong, Paul J. Hergenrother, Jessie Peh
  • Publication number: 20140161845
    Abstract: The present invention provides non-peptide compounds of formula (I) wherein: X is —(C1-C8)allcyl-, aryl or -aryl(C1-C8)alkyl-; Y is —(C1-C8)alkyl- or absent; W is heteroaryl, (C3-C7)carbocycle or aryl, wherein any heteroaryl, (C3-C7)carbocycle or, aryl of W is optionally substituted with one or more (e.g. 1, 2, 3, 4 or 5) Z1 groups; R1 is (C1-C8)alkyl, (C2-C8)alkenyl, (C2-C8)alkynyl or aryl, wherein aryl is optionally substituted with one or more (e.g. 1, 2, 3, 4 or 5) groups selected from (C1-C8)alkyl, (C2-C8)alkenyl, (C2-C8)alkynyl, (C3-C7)carbocycle, halo(C1-C3)alkyl, —CN, NO2, halogen, —ORa, —SRa, —S(O)2NRbRc, —NRbRc, —NRaCORd, —C(O)Ra, —C(O)ORa, and —C(O)NRbRc; R2 is (C1-C8)alkyl, (C2-C8)alkenyl, (C2-C8)Jalkynyl or aryl, wherein aryl is optionally substituted with one or more (e.g.
    Type: Application
    Filed: July 20, 2012
    Publication date: June 12, 2014
    Applicant: University of Louisville Research Foundation Inc.
    Inventors: Donald R. Demuth, Frederick A. Luzzio
  • Patent number: 8748411
    Abstract: Chemical compounds derived by in silico molecular modelling, having a well defined structure suitable for the blocking of the phosphorylation event, through the specific interaction of the chemical with the Casein Kinase 2 enzyme substrate phosphorylation domain or it's neighbourhood. This invention comprises also the pharmaceutical compositions containing such compounds, and their use in the preparation of medicines or agents for the treatment of diseases or conditions related with neoplasic processes.
    Type: Grant
    Filed: May 5, 2006
    Date of Patent: June 10, 2014
    Assignee: Centro de Ingenieria Genetica y Biotechnologia
    Inventors: Rolando Eduardo Rodriguez Fernandez, Roberto Vera Alvarez, Ania De La Nuez Veulens, Yuliet Mazola Reyes, Silvio Ernesto Perea Rodriguez, Boris Ernesto Acevedo Castro, Alexis Musacchio Lasa, Raimundo Ubieta Gómez
  • Publication number: 20140155379
    Abstract: Compounds and methods in the fields of chemistry and medicine are disclosed. Some of the disclosed embodiments include compounds, compositions and methods of using heterocycle amines. Some of the disclosed embodiments include heterocycle amines useful to treat inflammatory disorders.
    Type: Application
    Filed: December 20, 2013
    Publication date: June 5, 2014
    Applicant: Ligand Pharmaceuticals Incorporated
    Inventors: Koc-Kan Ho, David Diller, Jeffrey J. Letourneau, Brian F. McGuinness, Andrew G. Cole, David Rosen, Cornelis A. van Oeveren, Jason C. Pickens, Lin Zhi, Yixing Shen, Bijan Pedram
  • Publication number: 20140155263
    Abstract: Fungicidal mixtures comprising, as active components, 1) azolopyrimidinylamines of the formula I, in which the substituents are as defined in the description and 2) at least one active compound II selected from the following groups: azoles, strobilurins, carboxamides, heterocylic compounds, carbamates and other active compounds selected from the group consisting of guanidines, antibiotics, sulfur-containing heterocyclyl compounds, organophosphorus compounds, organochlorine compounds, inorganic active compounds, growth retardants and cyflufenamid, cymoxanil, dimethirimol, ethirimol, furalaxyl, metrafenone and spiroxamine; in a synergistically effective amount. Methods for controlling harmful fungi using mixtures of the compound I with active compounds II and the use of the compound I with active compounds II for preparing such mixtures, and also compositions comprising these mixtures.
    Type: Application
    Filed: February 10, 2014
    Publication date: June 5, 2014
    Applicant: BASF SE
    Inventors: Christine Beck, Matthias NIEDENBRÜCK, Maria Scherer, Reinhard Stierl, Siegfried Strathmann, Udo HÜNGER
  • Patent number: 8742101
    Abstract: This invention is directed to a method for treating a host, especially a human, infected with hepatitis C, flavivirus and/or pestivirus, comprising administering to that host an effective amount of an anti-HCV biologically active pentofuranonucleoside where the pentofuranonucleoside base is an optionally substituted 2-azapurine. The optionally substituted pentofuranonucleoside, or a salt or prodrug thereof, may be administered alone or in combination with one or more optionally substituted pentofuranonucleosides or other anti-viral agents.
    Type: Grant
    Filed: November 13, 2008
    Date of Patent: June 3, 2014
    Assignees: Idenix Pharmaceuticals, Inc., Centre National de la Recherche Scientifique, L'Universite Montpellier II
    Inventors: Richard Storer, Gilles Gosselin, David Dukhan, Frederic Leroy
  • Publication number: 20140141972
    Abstract: This invention pertains to methods for protecting a propagule or a plant grown therefrom from invertebrate pests comprising contacting the propagule or the locus of the propagule with a biologically effective amount of a compound of Formula I, its N-oxide or an agriculturally suitable salt thereof wherein A and B and R1 through R8 are as defined in the disclosure. This invention also relates to propagules treated with a compound of Formula I and compositions comprising a Formula I compound for coating propagules.
    Type: Application
    Filed: January 27, 2014
    Publication date: May 22, 2014
    Applicant: E I DU PONT NEMOURS AND COMPANY
    Inventors: RICHARD ALAN BERGER, Isaac Billy Annan, George Philip Lahm, John Lindsey Flexner, Thomas Paul Selby, Thomas Martin Stevenson
  • Publication number: 20140140973
    Abstract: This invention pertains to a method for controlling lepidopteran, homopteran, hemipteran, thysanopteran and coleopteran insect pests comprising contacting the insects or their environment with an arthropodicidally effective amount of a compound of Formula I, its N-oxide or an agriculturally suitable salt thereof wherein A and B and R1 through R8 are as defined in the disclosure. This invention further relates to a bezoxazinone compound of Formula 10 wherein R4 through R8 are as defined in the disclosure, useful for preparation of a compound of Formula I.
    Type: Application
    Filed: January 27, 2014
    Publication date: May 22, 2014
    Applicant: E I DU PONT DE NEMOURS AND COMPANY
    Inventors: GEORGE PHILIP LAHM, Stephen Frederick McCann, Kanu Maganbhai Patel, Thomas Paul Selby, Thomas Martin Stevenson
  • Publication number: 20140135335
    Abstract: Compounds of Formula I, including pharmaceutically acceptable salts, as well as compositions containing these compounds, have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV:
    Type: Application
    Filed: November 7, 2013
    Publication date: May 15, 2014
    Inventors: TAO WANG, Zhiwei Yin, Paul Michael Scola
  • Publication number: 20140135281
    Abstract: The present invention relates to methods and compositions comprising cyromazine for the control of bee mites and for the reduction of bee mite infestations, such as the control and reduction of infestations of parasitic bee mites, such as Varroa destructor in bee, preferably honey bee, colonies, and to the treatment of varroatosis in bees.
    Type: Application
    Filed: May 14, 2012
    Publication date: May 15, 2014
    Applicant: SYNGENTA PARTICIPATIONS AG
    Inventor: Andre Fougeroux
  • Publication number: 20140134130
    Abstract: Compounds of Formula I, including pharmaceutically acceptable salts thereof, as well as compositions containing these compounds, have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV:
    Type: Application
    Filed: November 7, 2013
    Publication date: May 15, 2014
    Inventors: Tao Wang, Zhiwei Yin, Paul Michael Scola
  • Patent number: 8722674
    Abstract: Disclosed herein are a 1,3,5-triazine-2,4,6-triamine compound or a pharmaceutically acceptable salt thereof, a preparation method thereof, and a composition for preventing or treating metabolic syndromes, diabetes, or cancers with deletion of P53 gene, which comprises the same.
    Type: Grant
    Filed: August 28, 2008
    Date of Patent: May 13, 2014
    Assignee: Hanall Biopharma Co., Ltd.
    Inventors: Hyae Gyeong Cheon, Kwang-Rok Kim, Sang Dal Rhee, Won Hoon Jung, Jong-Cheol Lee, Sung Wuk Kim, Sung Soo Jun
  • Patent number: 8722071
    Abstract: The present invention provides polymer microcapsules of biocide, useful for preparing coating materials such as interior and exterior paints, which comprises of an active agent biocide and an encapsulating polymer. Microcapsules described in this invention are prepared by dispersing an organic phase containing an active agent either in dissolved state or dispersed state in a polymer solution using a low boiling point solvent, in an aqueous phase containing an emulsifying agent; agitating the emulsion at 800-1200 resolution per minute for 3-5 hours at 25 -27° C. to evaporate the low boiling point solvent and thus to permit the formation of the microcapsules; separating the microcapsules, washing with water and drying the microcapsules at temperature between 25-35° C.
    Type: Grant
    Filed: February 27, 2006
    Date of Patent: May 13, 2014
    Assignee: Council of Scientific & Industrial Research
    Inventors: Shukla Parshuram Gajanan, Swaminathan Sivaram
  • Patent number: 8716301
    Abstract: A method is provided herein to increase an immune response to an antigen. The method includes administering an agent that inhibits extracellular adenosine or inhibits adenosine receptors. Also disclosed are methods to increase the efficacy of a vaccine and to increase an immune response to a tumor antigen or immune cell-mediated tumor destruction.
    Type: Grant
    Filed: December 2, 2011
    Date of Patent: May 6, 2014
    Assignee: The United States of America, as represented by the Secretary, Department of Health and Human Services
    Inventors: Michail V. Sitkovsky, Akio Ohta
  • Publication number: 20140113900
    Abstract: The present application relates to novel substituted imidazopyridazines, to processes for their preparation, to their use, alone or in combinations, for the treatment and/or prophylaxis of diseases and to their use for production of medicaments for the treatment and/or prophylaxis of diseases, especially for the treatment and/or prophylaxis of cardiovascular disorders.
    Type: Application
    Filed: May 2, 2012
    Publication date: April 24, 2014
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Markus Follmann, Johannes-Peter Stasch, Gorden Redlich, Alexander Straub, Jens Ackerstaff, Nils Griebenow, Andreas Knorr, Frank Wunder, Volkhart Min-Jian Li
  • Publication number: 20140100230
    Abstract: Methods of treating a TRPC5 mediated disorder in a subject by administering an effective amount of a TRPC5 antagonist, such as a compound disclosed herein, are described.
    Type: Application
    Filed: December 10, 2013
    Publication date: April 10, 2014
    Applicant: HYDRA BIOSCIENCES, INC.
    Inventors: Jayhong A. Chong, Christopher Fanger, Magdalene M. Moran, Elisha Singer, Timothy Strassmaier, Howard Ng
  • Publication number: 20140094448
    Abstract: The invention provides compounds that inhibit protein kinase CK2 activity (CK2 activity), and compositions containing such compounds.
    Type: Application
    Filed: September 13, 2013
    Publication date: April 3, 2014
    Applicant: SENHWA BIOSCIENCES, INC.
    Inventors: Mustapha Haddach, Joe A. Tran, Fabrice Pierre, Collin F. Regan, Nicholas Raffaele, Suchitra Ravula, David M. Ryckman
  • Patent number: 8685976
    Abstract: The subject invention discloses an agent for promoting cell adhesion to a support, comprising a dispirotripiperazine derivative represented by Formula I below or a salt thereof; a method for promoting cell adhesion to a support comprising adding the dispirotripiperazine derivative represented by Formula I below or a salt thereof to a culture medium, or applying the same to a support; and an agonist of a heparin sulfate that comprises the dispirotripiperazine derivative represented by Formula I below or a salt thereof, and that promotes cell adhesion and/or cell growth.
    Type: Grant
    Filed: June 16, 2009
    Date of Patent: April 1, 2014
    Assignee: Kyoto University
    Inventors: Motonari Uesugi, Sayumi Yamazoe
  • Publication number: 20140088080
    Abstract: [Problem] An excellent drug for treating or preventing cardiovascular diseases, based on cGMP production enhancing action due to soluble guanylate cyclase activating action, is provided. [Means for Solution] It was found that imidazopyridine compounds having a carbamoyl group at the 3-position and a substituent bonded at the 8-position via an oxygen atom in an imidazo[1,2-a]pyridine skeleton exhibits a cGMP production enhancing action by a potent soluble guanylate cyclase activating action, and is useful as a drug for treating or preventing various soluble guanylate cyclase-related cardiovascular diseases, thereby completing the present invention.
    Type: Application
    Filed: November 26, 2013
    Publication date: March 27, 2014
    Applicant: ASTELLAS PHARMA INC.
    Inventors: Yuji KOGA, Kyoichi MAENO, Ippei SATO, Yoshimasa IMAMURA, Takeshi HANAZAWA, Maiko IIDA, Kazuhiko OHNE, Kenichiro IMAMURA, Tsubasa WATANABE, Eisuke NOZAWA, Hiroshi SHIBATA
  • Publication number: 20140088109
    Abstract: The present invention provides a novel antagonist: N-((1R,2S,5R)-5-(tert-butylamino)-2-((S)-3-(7-tert-butylpyrazolo[1,5-a][1,3,5]triazin-4-ylamino)-2-oxopyrrolidin -1-yl)cyclohexyl)acetamide: or a pharmaceutically acceptable salt, solvate or prodrug, thereof, having unexpected dual CCR-2 and CCR-5 receptor activity. Crystalline forms, metabolites, pharmaceutical compositions containing the same and methods of using the same as agents for the treatment of inflammatory diseases, allergic, autoimmune, metabolic, cancer and/or cardiovascular diseases are also disclosed. The present disclosure also provides processes for preparing compounds of Formula (I) as provided herein, including N-((1R,2S,5R)-5-(tert-butylamino)-2-((S)-3-(7-tert-butylpyrazolo[1,5-a][1,3,5]triazin-4-ylamino)-2-oxopyrrolidin-1-yl)cyclohexyl)acetamide. Compounds that are useful intermediates of the process are also provided herein.
    Type: Application
    Filed: November 27, 2013
    Publication date: March 27, 2014
    Applicant: Bristol-Myers Squibb Company
    Inventors: Percy H. Carter, Robert J. Cherney
  • Publication number: 20140088099
    Abstract: Chemical compounds that modulate kinase activity, including PI3 kinase activity, and chemical compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including P13 kinase activity, are described herein.
    Type: Application
    Filed: November 20, 2013
    Publication date: March 27, 2014
    Applicant: Infinity Pharmaceuticals, Inc.
    Inventors: Pingda REN, Yi Liu, Liansheng Li, Katrina Chan, Alfredo C. Castro, Catherine A. Evans
  • Publication number: 20140073632
    Abstract: Novel CFTR corrector compounds that are effective in rescuing halide efflux in a cell are provided. Also provided are methods for treating protein folding disorders (e.g., cystic fibrosis). The methods include administering a CFTR corrector compound or pharmaceutically acceptable salt or prodrug thereof. Methods of screening for CFTR corrector compounds are also described herein. The methods of screening include contacting a cell that endogenously expresses a CFTR mutation with the compound to be screened and detecting a rescue of halide efflux from the cell.
    Type: Application
    Filed: May 17, 2012
    Publication date: March 13, 2014
    Applicants: THE UAB RESEARCH FOUNDATION, DISCOVERYBIOMED INC.
    Inventors: Erik M. Schwiebert, James F. Collawn, Zsuzsa Bebok
  • Publication number: 20140066430
    Abstract: The present invention relates to chemical compounds having a general formula I wherein A1, A2, C1, C2, D, L1, L2, Z and R3, R4, R6, R7 and R8 are defined herein, which are capable of modulating Aurora kinase protein activity, thereby influencing various disease states and conditions related to the activities of Aurora kinase proteins. For example, the compounds are capable of influencing the process of cell cycle and cell proliferation to treat cancer and cancer-related diseases. The invention also includes pharmaceutical compositions, processes of preparing compounds of the invention, synthetic intermediates and methods of treatment of conditions related to the activity of Aurora kinase.
    Type: Application
    Filed: October 3, 2013
    Publication date: March 6, 2014
    Applicant: Amgen Inc.
    Inventors: Victor J. CEE, Holly L. DEAK, Bingfan DU, Stephanie D. GEUNS-MEYER, Brian L. HODOUS, Hanh Nho NGUYEN, Philip R. Olivieri, Vinod F. Patel, Karina ROMERO, Laurie Schenkel
  • Publication number: 20140066434
    Abstract: The invention discloses methods and compositions for treating or preventing Parkinson's disease by administering a compound of Formula (I): or a pharmaceutically acceptable salt, solvate or hydrate thereof, wherein the variables are defined as herein.
    Type: Application
    Filed: April 6, 2012
    Publication date: March 6, 2014
    Applicant: ARIAD PHARMACEUTICALS, INC.
    Inventor: William C. Shakespeare
  • Publication number: 20140050786
    Abstract: The present invention relates to combinations of triazine derivatives and of insulin sensitisers.
    Type: Application
    Filed: October 25, 2013
    Publication date: February 20, 2014
    Applicant: POXEL SAS
    Inventors: Gerard MOINET, Daniel CRAVO, Didier MESANGEAU
  • Publication number: 20140051676
    Abstract: The invention relates to new derivatives of formula (I), wherein the substituents are as defined in the specification; to processes for the preparation of such derivatives; pharmaceutical compositions comprising such derivatives; such derivatives as a medicament; such derivatives for the treatment of chronic pain.
    Type: Application
    Filed: October 15, 2013
    Publication date: February 20, 2014
    Applicant: NOVARTIS AG
    Inventors: Oliver BARKER, Jonathan Mark BENTLY, Mark Gary BOCK, Thomas CAIN, Praful CHOVATIA, Jennifer Ruth DOD, Florence EUSTACHE, Laura GLEAVE, Jonathan HARGRAVE, Alexander HEIFETZ, Richard LAW, Ali RAOOF, David WILLOWS
  • Publication number: 20140045852
    Abstract: The present invention relates to substituted 4-Aryl-N-phenyl-1,3,5-triazin-2-amines of general formula (I) as described and defined herein, and methods for their preparation, their use for the treatment and/or prophylaxis of disorders, in particular of hyper-proliferative disorders and/or virally induced infectious diseases and/or of cardiovascular diseases. The invention further relates to intermediate compounds useful in the preparation of said compounds of general formula (I).
    Type: Application
    Filed: April 18, 2012
    Publication date: February 13, 2014
    Applicants: BAYER PHARMA AKTIENGESELLSCHAFT, BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Ulrich Lücking, Rolf Bohlmann, Arne Scholz, Gerhard Siemeister, Mark Jean Gnoth, Ulf Bomer, Gerd Rühter, Carsten Schultz-Fademrecht, Dirk Kosemund, Philip Lienau
  • Publication number: 20140045826
    Abstract: The invention discloses methods and compositions for treating or preventing neurodegenerative disease by administering a compound of Formula I: or a pharmaceutically acceptable salt, solvate or hydrate thereof, wherein the variables are defined as herein.
    Type: Application
    Filed: April 6, 2012
    Publication date: February 13, 2014
    Applicant: ARIAD PHARMACEUTICALS, INC.
    Inventors: William C. Shakespeare, Frank G. Haluska
  • Publication number: 20140038968
    Abstract: The present invention relates to certain novel compounds of Formula (I): and methods for preparing these compounds, compositions, intermediates and derivatives thereof and for the treatment of prokineticin 1 or prokinetin 1 receptor mediated disorders.
    Type: Application
    Filed: October 17, 2012
    Publication date: February 6, 2014
    Inventors: Steven J. Coats, Alexey B. Dyatkin, Wei He, Joseph Lisko, Tamara A. Miskowski, Janet L. Ralbovsky, Mark J. Schulz