Tricyclo Ring System Having The Hetero Ring As One Of The Cyclos Patents (Class 540/495)
  • Patent number: 10364317
    Abstract: The invention relates to novel conjugated polymers containing one or more units based on dithieno[3,2-c;2?,3?-e]azepine-4,6-dione that is fused to further aromatic rings, to methods for their preparation and educts or intermediates used therein, to polymer blends, mixtures and formulations containing them, to the use of the polymers, polymer blends, mixtures and formulations as organic semiconductors in, or for the preparation of, organic electronic (OE) devices, especially organic photovoltaic (OPV) devices and organic photodetectors (OPD), and to OE, OPV and OPD devices comprising, or being prepared from, these polymers, polymer blends, mixtures or formulations.
    Type: Grant
    Filed: August 12, 2015
    Date of Patent: July 30, 2019
    Assignees: Merck Patent GmbH, IMPERIAL INNOVATIONS LIMITED
    Inventors: Nicolas Blouin, William Mitchell, Martin Heeney, Jessica Shaw
  • Patent number: 8962613
    Abstract: A diazepine derivative having the following formula (III) or a pharmacologically acceptable salt thereof is used as A P2X4 receptor antagonist: wherein each of R21 and R22 is hydrogen, a C1-8 alkyl group or the like; R23 is hydrogen, a C1-8 alkyl group or the like; each of R24 and R25 is hydrogen, a C1-8 alkyl group or the like; R26 is hydrogen, a C1-8 alkyl group, a halogen atom, hydroxyl, nitro, cyano, phenyl optionally having one or more substituents, or a heterocyclic group optionally having one or more substituents or the like; and p is 0 or 1.
    Type: Grant
    Filed: July 13, 2011
    Date of Patent: February 24, 2015
    Assignee: Nippon Chemiphar Co., Ltd.
    Inventors: Shogo Sakuma, Masahiko Arai, Kunio Kobayashi, Yoshikazu Watanabe, Toshiyasu Imai, Kazuhide Inoue
  • Publication number: 20140357858
    Abstract: The present invention relates to a diazepine derivative represented by the following general formula (I) (in the formula, R1 and R2 represent hydrogen atom and the like, or R1 and R2 bind together to form a naphthalene ring and the like together with the benzene ring to which they bind, R3 and R4 represent hydrogen atom and the like, R5 represents hydrogen atom and the like, R6 and R7 represent hydrogen atom and the like, X represents C, CH or N, Y represents N, NH or C(?O), provided that when X is N, Y is not N or NH, and when X is C or CH, Y is not C(?O), Z represents oxygen atom or sulfur atom, A represents benzene ring and the like, B represents NHC(?O) and the like, D represents an atomic bond and the like, E represents an atomic bond and the like, G represents benzene which may be substituted and the like, and m represents an integer of 0 to 5) or a pharmacologically acceptable salt thereof, and a P2X4 receptor antagonist.
    Type: Application
    Filed: January 10, 2013
    Publication date: December 4, 2014
    Inventors: Masatoshi Ushioda, Kunio Kobayashi, Daisuke Saito, Shogo Sakuma, Toshiyasu Imai, Kazuhide Inoue
  • Publication number: 20140329804
    Abstract: The invention provides for novel benzonaphthyridine derivatives and compositions comprising novel benzonaphthyridine derivatives. In some embodiments, the compounds are phosphodiesterase inhibitors. The invention further provides for methods for inhibition of phosphodiesterase comprising contacting phosphodiesterase with novel benzonaphthyridine derivatives or compositions comprising novel benzonaphthyridine derivatives. The invention further provides for methods for treatment of neurodegenerative diseases, increasing memory or long term potentiation with novel benzonaphthyridine derivatives or compositions comprising novel benzonaphthyridine derivatives. In some embodiments, the phosphodiesterase is PDE5.
    Type: Application
    Filed: July 17, 2014
    Publication date: November 6, 2014
    Inventors: Donald W. LANDRY, Shixian DENG, Ottavio ARANCIO, Jole FIORITO, Andrew WASMUTH
  • Patent number: 8822453
    Abstract: The present invention provides a novel diazepine compound that blocks the IKur current or the Kv1.5 channel potently and more selectively than other K+ channels. The present invention relates to a diazepine compound represented by General Formula (1) or a salt thereof, wherein R1, R2, R3, and R4 are each independently hydrogen, lower alkyl, cyclo lower alkyl or lower alkoxy lower alkyl; R2 and R3 may be linked to form lower alkylene; A1 is lower alkylene optionally substituted with one or more substituents selected from the group consisting of hydroxyl and oxo; Y1 and Y2 are each independently —N? or —CH?; and R5 is group represented by wherein R6 and R7 are each independently hydrogen or organic group; R6 and R7 may be linked to form a ring together with the neighboring group —XA—N—XB—; XA and XB are each independently a bond, lower alkylene, etc.
    Type: Grant
    Filed: August 20, 2010
    Date of Patent: September 2, 2014
    Assignee: Otsuka Pharmaceutical Co., Ltd.
    Inventors: Shuuji Matsumura, Hokuto Yamabe, Naohiro Isono, Noriaki Takemura, Takashi Oshiyama, Tsuyoshi Nagase, Masataka Ueda, Kuninori Tai
  • Patent number: 8563542
    Abstract: The present invention relates to a compound of formula (VII)I, or a pharmaceutically acceptable salt or ester thereof, wherein: X is NR7; Y is O or N—(CH2)nR19; n is 1, 2 or 3; m is 1 or 2; R1 and R2 are each independently H, alkyl or cycloalkyl; R4 and R4? each independently H alkyl; or R4 and R4? together form a spiro cycloalkyl group; R19 is H, alkyl, aryl or a cycloalkyl group; R6 is OR8 or halogen; and R7 and R8 are each independently H or alkyl. Further aspects relate to pharmaceutical compositions comprising said compounds and use therefore in the treatment of proliferative disorders and the like.
    Type: Grant
    Filed: September 29, 2008
    Date of Patent: October 22, 2013
    Assignee: Cyclacel Limited
    Inventors: Jonathan James Hollick, Stuart Donald Jones, Claire June Flynn, Michael George Thomas
  • Patent number: 8501750
    Abstract: Heterocyclic compounds, pharmaceutical agent and methods thereof, having superior pharmacological action and/or physicochemical properties, which are useful for the prophylaxis or treatment of circulatory diseases such as hypertension, cardiac diseases, arteriosclerosis, renal diseases and cerebral apoplexy and/or metabolic diseases such as hyperlipidemia, obesity and diabetes and/or central nervous disorders such as cerebral infarction, and/or mental diseases such as dementia depression and depression.
    Type: Grant
    Filed: May 20, 2008
    Date of Patent: August 6, 2013
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Takanobu Kuroita, Hideyuki Igawa, Hiroki Sakamoto, Kouhei Asano, Minoru Sasaki
  • Publication number: 20130172550
    Abstract: A diazepine derivative having the following formula (III) or a pharmacologically acceptable salt thereof is used as A P2X4 receptor antagonist: wherein each of R21 and R22 is hydrogen, a C1-8 alkyl group or the like; R23 is hydrogen, a C1-8 alkyl group or the like; each of R24 and R25 is hydrogen, a C1-8 alkyl group or the like; R26 is hydrogen, a C1-8 alkyl group, a halogen atom, hydroxyl, nitro, cyano, phenyl optionally having one or more substituents, or a heterocyclic group optionally having one or more substituents or the like; and p is 0 or 1.
    Type: Application
    Filed: July 13, 2011
    Publication date: July 4, 2013
    Applicant: Nippon Chemiphar Co., Ltd.
    Inventors: Shogo Sakuma, Masahiko Arai, Kunio Kobayashi, Yoshikazu Watanabe, Toshiyasu Imai, Kazuhide Inoue
  • Patent number: 8470814
    Abstract: A diazepinedione derivative represented by the formula (I) or a pharmacologically acceptable salt thereof is used as a P2X4 receptor antagonist: wherein R1 represents a hydrogen atom, an alkyl group having 1 to 8 carbon atoms, or the like, R2 and R3 represent a hydrogen atom, an alkyl group having 1 to 8 carbon atoms, a halogen atom, or the like, R4 and R5 represent a hydrogen atom, an alkyl group having 1 to 8 carbon atoms, or the like, and W represents tetrazole or the like.
    Type: Grant
    Filed: February 15, 2010
    Date of Patent: June 25, 2013
    Assignee: Nippon Chemiphar Co., Ltd.
    Inventors: Shogo Sakuma, Toshihiro Takahashi, Masatoshi Ushioda, Toshiyasu Imai, Kazuhide Inoue
  • Publication number: 20130150350
    Abstract: Compounds of formula (I) wherein m, R1, R2, R3, X and Y are defined herein, are useful as inhibitors of HIV replication.
    Type: Application
    Filed: February 9, 2011
    Publication date: June 13, 2013
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Bruno Simoneau, Patrick Deroy, Lee Fader, Anne-Marie Faucher, Alexander Gagnon, Chantal Grand-Maitre, Stephen Kawai, Serge Landry, Jean-Francois Mercier, Jean Rancourt
  • Patent number: 8461149
    Abstract: The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.
    Type: Grant
    Filed: August 15, 2008
    Date of Patent: June 11, 2013
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Francoise Pierard, Jean-Damien Charrier
  • Patent number: 8460704
    Abstract: The invention relates to an extended release pharmaceutical composition comprising nevirapine.
    Type: Grant
    Filed: June 4, 2008
    Date of Patent: June 11, 2013
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Michael L. Cappola, Svetlana Sienkiewicz, Glenn Charles Snow, Feng-Jing Chen
  • Publication number: 20130129677
    Abstract: Methods and pharmaceutical compositions for treating viral infections, by administering certain thienopyridine derivative compounds in therapeutically effective amounts are disclosed. Methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment 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: December 7, 2012
    Publication date: May 23, 2013
    Applicant: Siga Technologies, Inc.
    Inventor: Siga Technologies, Inc.
  • Patent number: 8394952
    Abstract: The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.
    Type: Grant
    Filed: August 10, 2011
    Date of Patent: March 12, 2013
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: David Kay, Ronald Knetgel, Jean-Damien Charrier, Heather Twin
  • Publication number: 20130039987
    Abstract: The invention provides a method for increasing the solubility of nevirapine, including the steps of rendering nevirapine in a gaseous phase; and rendering the gaseous phase in a relatively more soluble solid particulate form. The invention further provides for a crystalline Form-VI (36) of nevirapine having an X-ray diffraction pattern of (2-theta values in degrees) 9.2953, 11.2023, 12.7019, 12.9796, 13.5273, 15.4670, 17.2597, 19.1038, 19.7267, 21.1303, 22.9381, 25.5589, 26.4913, 27.2150, 27.7283, 29.7134, and 33.8343 degrees two theta. The invention further provides for the preparation of microspherical and/or nanospherical Form-V (34) and crystalline Form-VI (36) of nevirapine as well as novel dosage forms including parenteral-, inhalant-, transdermal- and oral dosage forms.
    Type: Application
    Filed: November 9, 2010
    Publication date: February 14, 2013
    Applicant: North-West University
    Inventors: Wilna Liebenberg, Nicole Stieger
  • Patent number: 8361759
    Abstract: The present invention provides a scalable process for producing a concentrate containing a mass of a farnesylated dibenzodiazepinone by fermenting in an aqueous culture medium a strain of a microorganism that is capable of producing the farnesylated dibenzodiazepinone, upon completion of fermentation harvesting the fermentation broth and extracting the fermentation broth to provide an extract, and thereafter treating the extract to form the concentrate. The concentrate so produced may be utilized in downstream processes for producing pharmaceutical compounds. A strain of a Micromonospora species capable of producing a farnesylated dibenzodiazepinone at a high yield rate is provided, together with culture media for culturing microorganisms, and fermentation conditions for production of the farnesylated dibenzodiazepinone of the concentrate.
    Type: Grant
    Filed: April 21, 2010
    Date of Patent: January 29, 2013
    Assignee: Thallion Pharmaceuticals Inc.
    Inventors: Faustinus Yeboah, Mahmood Piraee
  • Publication number: 20120322793
    Abstract: In one aspect, the invention provides compounds of Formula I or pharmaceutically acceptable salts thereof. In another aspect, the invention provides methods for treatment of diseases or disorders mediated by a protein kinase, comprising administering a therapeutically effective amount of a compound of this invention.
    Type: Application
    Filed: August 24, 2012
    Publication date: December 20, 2012
    Applicant: Vertex Pharmaceuticals Incorporated
    Inventors: Jean-Damien Charrier, Steven Durrant
  • Publication number: 20120283249
    Abstract: The subject matter of the present invention is novel families of compounds which are aromatic amine, imine, aminoadamantane and benzodiazepine derivatives, medicaments comprising same and the use thereof as inhibitors of the toxic effects of toxins with intracellular activity, such as, for example, ricin, and of viruses that use the internalization pathway for infecting cells.
    Type: Application
    Filed: June 17, 2009
    Publication date: November 8, 2012
    Inventors: Roman Lopez, Séverine Hebbe, Daniel Gillet, Julien Barbier
  • Publication number: 20120271045
    Abstract: A method of preparing a compound represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof, wherein the variables of Structural Formula (I) are as described in the specification and claims. Additionally, the present invention relates to compounds of Structural Formula (I), which are useful as inhibitors of protein kinase.
    Type: Application
    Filed: March 20, 2012
    Publication date: October 25, 2012
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: Jean-Damien Charrier, Steven Durrant, Michael O'Donnell
  • Patent number: 8293731
    Abstract: Tricyclic compounds of Formula I are inhibitors of HIV integrase and inhibitors of HIV replication: wherein bond a, ring A, R1, R2 and R3 are defined herein. The compounds are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
    Type: Grant
    Filed: May 13, 2011
    Date of Patent: October 23, 2012
    Assignee: Merck Sharp + Dohme Corp.
    Inventors: Joseph P. Vacca, John S. Wai, Linda S. Payne
  • Patent number: 8212025
    Abstract: An improved process for preparing 11-cyclopropyl-5,11-dihydro-4-methyl-6H-dipyrido[3,2-b:2?,3?-e][1,4]diazepin-6-one of Formula (I).
    Type: Grant
    Filed: May 14, 2008
    Date of Patent: July 3, 2012
    Assignee: Aurobindo Pharma Ltd.
    Inventors: Jagan Mohan Reddy Sanapureddy, Ramesh Dandala, Sivakumaran Meenakshisunderam
  • Publication number: 20120149898
    Abstract: The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.
    Type: Application
    Filed: August 10, 2011
    Publication date: June 14, 2012
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: David Kay, Ronald Knetgel, Jean-Damien Charrier, Heather Twin
  • Publication number: 20120116073
    Abstract: A compound having the following formula (II) or its pharmacologically acceptable salt is used as a P2X4 receptor antagonist: in which R11 represents hydrogen or an alkyl group having 1-8 carbon atoms; R21 represents an alkyl group having 1-8 carbon atoms, an alkoxy group having 1-8 carbon atoms, an alkyl group having 1-8 carbon atoms and having 1-3 halogen substituents, or hydroxyl; and R31 is hydrogen or a halogen atom.
    Type: Application
    Filed: January 20, 2012
    Publication date: May 10, 2012
    Applicant: NIPPON CHEMIPHAR COL, LTD.
    Inventors: Shogo SAKUMA, Tsuyoshi Endo, Toshiyasu Imai, Noriko Kanakubo, Masahiko Arai, Toshihiro Takahashi, Kenji Hirate, Takako Hirate, Tomio Yamakawa, Makoto Tsuda, Kazuhide Inoue
  • Publication number: 20120040961
    Abstract: The present invention relates to novel pyrimido-diazepinone compounds, methods of modulating protein kinases, including MPS1 (TTK), ERK5 (BMK1, MAPK7), polo kinase 1, 2, 3, or 4, Ack1, Ack2, AbI, DCAMKL1, ABL1, AbI mutants, DCAMKL2, ARK5, BRK, MKNK2, FGFR4, TNK1, PLK1, ULK2, PLK4, PRKD1, PRKD2, PRKD3, ROS 1, RPS6KA6, TAOK1, TAOK3, TNK2, Bcr-Abl, GAK, cSrc, TPR-Met, Tie2, MET, FGFR3, Aurora, AxI, Bmx, BTK, c-kit, CHK2, Flt3, MST2, p70S6K, PDGFR, PKB, PKC, Raf, ROCK-H, Rsk1, SGK, TrkA, TrkB and TrkC, and the use of such compounds in the treatment of various diseases, disorders or conditions.
    Type: Application
    Filed: January 6, 2010
    Publication date: February 16, 2012
    Applicant: DANA-FARBER CANCER INSTITUTE
    Inventors: Nathanael S. Gray, Xianming Deng, Nicholas Paul Kwiatkowski
  • Publication number: 20110300116
    Abstract: A method for generating a recombinant clonal cell line expressing a target cell surface receptor at a specific level of expression from a cell population comprising cells transfected with a plasmid encoding the cDNA sequence of the target receptor and expressing the target cell surface receptor, the method comprising (c) incubating the cell population with a receptor specific fluorescent ligand (d) selecting single cells from step (c) expressing the target cell surface receptor by monitoring the specific binding of the fluorescent ligand using flow cytometry; and novel fluorescent ligands.
    Type: Application
    Filed: September 29, 2008
    Publication date: December 8, 2011
    Applicant: CELLAURA TECHNOLOGIES LTD
    Inventors: Stephen John Hill, Barrie Kellam, Richard John Middleton
  • Publication number: 20110294791
    Abstract: The present invention generally relates to the neuroprotective activity of condensed diazepinones, e.g. condensed benzodiazepinones such as pirenzepine or compounds which are metabolized to condensed benzodiazepinones such as olanzapine. These compounds are suitable as co-medicaments for the prevention and/or treatment of drug-induced neurotoxic effects in general and neurotoxic side effects during cancer treatments with cytostatic drugs such as platinum-derivatives, e.g. cis-, carbo- and oxaliplatin, taxanes, bleomycin, cyclophosphamide and vincristine etc. Further, these compounds have an intrinsic anti-cancer activity on their own due to PARP-1 inhibition, which prevents NADH depletion in oxidative metabolism of healthy cells thus preventing the shift to anoxygenic, glycolytic metabolism present in many types of tumour cells thus eliminating this crucial metabolic advantage favoring tumour growth.
    Type: Application
    Filed: January 13, 2010
    Publication date: December 1, 2011
    Applicant: PROTEOSYS AG
    Inventor: Andre Schrattenholz
  • Publication number: 20110263574
    Abstract: The present invention generally relates to the otoprotective activity of condensed diazepinones, e.g. condensed benzodiazepines such as pirenzepine or compounds which are metabolized to condensed benzodiazepinones such as olanzapine. These compounds are suitable as medicaments for the prevention and/or treatment of otic diseases, e.g. diseases associated with loss of hearing.
    Type: Application
    Filed: January 13, 2010
    Publication date: October 27, 2011
    Applicant: PROTEOSYS AG
    Inventor: Andre Schrattenholz
  • Patent number: 8022202
    Abstract: The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.
    Type: Grant
    Filed: September 29, 2009
    Date of Patent: September 20, 2011
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: David Kay, Ronald Knegtel, Jean-Damien Charrier, Heather Twin
  • Publication number: 20110196147
    Abstract: This invention relates to compounds for the inhibition of histone deacetylase. More particularly, the invention provides for compounds of formula (I) wherein Q, J, L and Z are as defined in the specification.
    Type: Application
    Filed: April 4, 2011
    Publication date: August 11, 2011
    Inventors: Robert Déziel, Silvana Leit, Patrick Beaulieu, Yves Andre Chantigny, John Mancuso, Pierre Tessier, Gideon Shapiro, Richard Chesworth, David Smil
  • Patent number: 7994160
    Abstract: Disclosed are pyridazine compounds of the formula I which are useful for inhibiting glycogen synthase kinase 3 (GSK-3), methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds: In formula I indicates a single bond or a double bond; X is O, S or N—R5; R1, R2 are independently selected from the group consisting of H, NH2, NH—C1-C6-alkyl, OH, ?O, (i.e.
    Type: Grant
    Filed: July 12, 2006
    Date of Patent: August 9, 2011
    Assignee: Abbott GmbH & Co. KG
    Inventors: Sean C. Turner, Margaretha Bakker, Roland Grandel, Michael Vierling
  • Patent number: 7943608
    Abstract: The invention relates to compounds of the formula (I), to the preparation and use thereof for the preparation of a medicament for the treatment of diseases, in particular tumours and/or diseases in the development or course of which kinases are involved.
    Type: Grant
    Filed: November 28, 2006
    Date of Patent: May 17, 2011
    Assignee: Merck Patent GmbH
    Inventors: Melanie Schultz, Lars Thore Burgdorf, Dirk Finsinger, Andree Blaukat, Hartmut Greiner, Christina Esdar
  • Publication number: 20110046093
    Abstract: The present invention relates to a compound of formula (VII)I, or a pharmaceutically acceptable salt or ester thereof, wherein: X is NR7; Y is O or N—(CH2)nR19; n is 1, 2 or 3; m is 1 or 2; R1 and R2 are each independently H, alkyl or cycloalkyl; R4 and R4? each independently H alkyl; or R4 and R4? together form a spiro cycloalkyl group; R19 is H, alkyl, aryl or a cycloalkyl group; R6 is OR8 or halogen; and R7 and R8 are each independently H or alkyl. Further aspects relate to pharmaceutical compositions comprising said compounds and use therefore in the treatment of proliferative disorders and the like.
    Type: Application
    Filed: September 29, 2008
    Publication date: February 24, 2011
    Applicant: CYCLACEL LIMITED
    Inventors: Jonathan James Hollick, Stuart Donald Jones, Claire June Flynn, Michael George Thomas
  • Publication number: 20100256123
    Abstract: A compound having the following formula (II) or its pharmacologically acceptable salt is used as a P2X4 receptor antagonist: in which R11 represents hydrogen or an alkyl group having 1-8 carbon atoms; R21 represents an alkyl group having 1-8 carbon atoms, an alkoxy group having 1-8 carbon atoms, an alkyl group having 1-8 carbon atoms and having 1-3 halogen substituents, or hydroxyl; and R31 is hydrogen or a halogen atom.
    Type: Application
    Filed: August 24, 2007
    Publication date: October 7, 2010
    Applicant: NIPPON CHEMIPHAR CO., LTD.
    Inventors: Shogo Sakuma, Tsuyoshi Endo, Toshiyasu Imai, Noriko Kanakubo, Masahiko Arai, Toshihiro Takahashi, Tomio Yamakawa, Makoto Tsuda, Kazuhide Inoue, Kenji Hirate, Takako Hirate
  • Publication number: 20100249094
    Abstract: The disclosure provides compounds of formula I, including their 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: Application
    Filed: March 10, 2010
    Publication date: September 30, 2010
    Inventors: Kap-Sun Yeung, Kyle E. Parcella, John A. Bender, Brett R. Beno, Katharine A. Grant-Young, Ying Han, Piyasena Hewawasam, John F. Kadow, Andrew Nickel
  • Publication number: 20100247688
    Abstract: The present invention relates to a compound that is capable of inhibiting the formation of ?-amyloid plaques, of reducing and/or retarding the increase the ?-amyloid plaque load in the brain of an animal, particularly a mammal, but especially a human. In particular, the invention relates to compounds of formula (I) and to metabolites thereof.
    Type: Application
    Filed: July 2, 2008
    Publication date: September 30, 2010
    Inventors: Andrea Pfeifer, André Schrattenholz, Andreas Muhs
  • Publication number: 20100228023
    Abstract: The present invention provides one step processes for the preparation of substituted dibenzo[b,e][1,4]-diazepine-11-ones by the reaction of substituted isatoic anhydrides with substituted 1,2-phenylenediamines in the presence of aqueous acetic acid.
    Type: Application
    Filed: January 8, 2010
    Publication date: September 9, 2010
    Applicant: COUNCIL OF SCIENTIFIC AND INDUSTRIAL RESEARCH
    Inventors: Harshadas Mitaram Meshram, Palakuri Ramesh Goud, Bandi Chennakesava Reddy, Jhillu Singh Yadav
  • Patent number: 7786107
    Abstract: The present invention relates to modulators of muscarinic receptors. The present invention also provides compositions comprising such modulators, and methods therewith for treating muscarinic receptor mediated diseases.
    Type: Grant
    Filed: August 20, 2007
    Date of Patent: August 31, 2010
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Robert J. Davies, Jinwang Xu
  • Publication number: 20100204468
    Abstract: The present invention provides a scalable process for producing a concentrate containing a mass of a farnesylated dibenzodiazepinone by fermenting in an aqueous culture medium a strain of a microorganism that is capable of producing the farnesylated dibenzodiazepinone, upon completion of fermentation harvesting the fermentation broth and extracting the fermentation broth to provide an extract, and thereafter treating the extract to form the concentrate. The concentrate so produced may be utilized in downstream processes for producing pharmaceutical compounds. A strain of a Micromonospora species capable of producing a farnesylated dibenzodiazepinone at a high yield rate is provided, together with culture media for culturing microorganisms, and fermentation conditions for production of the farnesylated dibenzodiazepinone of the concentrate.
    Type: Application
    Filed: April 21, 2010
    Publication date: August 12, 2010
    Applicant: THALLION PHARMACEUTICALS INC.
    Inventors: Faustinus YEBOAH, Mahmood PIRAEE
  • Publication number: 20100189762
    Abstract: Compounds, pharmaceutical compositions including the compounds, and methods of preparation and use thereof are disclosed. The compounds are triphenyl methane analogs. The compounds and compositions can be used to treat and/or prevent a wide variety of cancers, including drug resistant cancers, inflammatory, degenerative and vascular diseases, including various ocular diseases, and parasitic infections. Representative triphenyl methane analogs include triphenyl methane analogues of various dyes, hormones, sugars, peptides, oligonucleotides, amino acids, nucleotides, nucleosides, and polyols. The compounds are believed to function by inhibiting tNOX expression, the effects of ROS, and/or the production of HIF2. Thus, the compounds are novel therapeutic agents for a variety of cancers and other diseases.
    Type: Application
    Filed: December 21, 2009
    Publication date: July 29, 2010
    Applicant: EMORY UNIVERSITY
    Inventor: Jack L. Arbiser
  • Publication number: 20100125137
    Abstract: An improved process for preparing 11-cyclopropyl-5,11-dihydro-4-methyl-6H-dipyrido[3,2-b:2?,3?-e][1,4]diazepin-6-one of Formula (I).
    Type: Application
    Filed: May 14, 2008
    Publication date: May 20, 2010
    Inventors: Jagan mohan Reddy Sanapureddy, Ramesh Dandala, Sivakumaran Meenakshisunderam
  • Patent number: 7709471
    Abstract: There is provided a compound of formula (I): processes for the manufacture thereof, pharmaceutical compositions thereof and uses in therapy.
    Type: Grant
    Filed: July 5, 2007
    Date of Patent: May 4, 2010
    Assignee: AstraZeneca AB
    Inventors: Christopher Thomas Halsall, David Alan Rudge, Iain Simpson, Richard Andrew Ward
  • Patent number: 7655646
    Abstract: The invention relates to biologically active dibenzodiazepinone analogs represented by Formula I, to methods of producing them, to pharmaceutical compositions comprising them and to methods of treating neoplastic conditions.
    Type: Grant
    Filed: December 21, 2007
    Date of Patent: February 2, 2010
    Assignee: Thallion Pharmaceuticals, Inc.
    Inventors: James B. McAlpine, Arjun H. Banskota, Mustapha Aouidate
  • Publication number: 20090291938
    Abstract: Compounds of the following formula are provided for use with kinases: wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.
    Type: Application
    Filed: November 19, 2008
    Publication date: November 26, 2009
    Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Sheldon X. Cao, Victoria Feher, Takashi Ichikawa, Benjamin Jones, Stephen W. Kaldor, Andre A. Kiryanov, Betty Lam, Yan Liu, Christopher McBride, Srinivasa Reddy Natala, Zhe Nie, Jeffrey A. Stafford
  • Patent number: 7622463
    Abstract: The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.
    Type: Grant
    Filed: February 13, 2007
    Date of Patent: November 24, 2009
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: David Kay, Ronald Knegtel, Jean-Damien Charrier, Heather Twin
  • Publication number: 20090281080
    Abstract: Compounds of formula I: (wherein variables A1, A2, A3, A4, A5, A6, A7, B1, B2, B3, B4, D1, D2, E1, E2, E3, E4, E5, G1, G2, R6, T, U, V, W, X, Y and Z are as described herein) which are antagonists of CGRP receptors and which are useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. 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 CGRP is involved.
    Type: Application
    Filed: November 14, 2006
    Publication date: November 12, 2009
    Inventors: Ian M. Bell, Craig A. Stump, Cory R. Theberge, Steven N. Gallicchio, C. Blair Zartman
  • Publication number: 20090239849
    Abstract: The present invention relates to a novel class of aryl-fused spirocyclic compounds. These compounds can inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.
    Type: Application
    Filed: May 14, 2007
    Publication date: September 24, 2009
    Inventors: Christopher Hamblett, Solomon Kattar, Dawn Mampreian, Joey Methot, Thomas Miller, Paul Tempest
  • Publication number: 20090203901
    Abstract: The present invention provides innovative strategies for synthesizing pyrazole ring-functionalized benzodiazepinones. Alternative intermediates and high conversion strategies for forming alpha-aminobenzophenone intermediates involve a combination of aromatic acylation, displacement of electronegative leaving groups with amine, and then N-displacement strategies to produce the desired alpha-aminobenzophenone with primary amine functionality. Reaction strategies are then provided for converting alpha-aminobenzophenones to alpha-aminoamidobenzophenone intermediates with high yield and convenient reaction strategies. These alpha-aminoamidobenzophenone intermediates are then converted into benzodiazepinones. These benzodiazepinones are then converted to pyrazole ring functionalized benzodiazepinones through a series of innovative intermediates and/or reaction strategies.
    Type: Application
    Filed: February 12, 2009
    Publication date: August 13, 2009
    Inventors: Peter J. Harrington, Valerie Grace Paulsen, Charles E. Tucker
  • Patent number: 7569561
    Abstract: The present invention encompasses compounds of general formula (1) wherein R1 to R6, X and Y are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or anomalous cell proliferation, as well as the use thereof for preparing a pharmaceutical composition with the above-mentioned properties.
    Type: Grant
    Filed: February 16, 2007
    Date of Patent: August 4, 2009
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Heinz Stadtmueller, Anke Baum, Guido Boehmelt, Harald Engelhardt, Jens Juergen Quant, Flavio Solca, Martin Steegmaier, Stephan Karl Zahn
  • Publication number: 20090186878
    Abstract: The present invention relates to crystalline forms of ECO-4601 and the processes for providing them. The invention further relates to pharmaceutical compositions comprising the crystalline forms and to methods of use of the crystalline forms as pharmaceuticals.
    Type: Application
    Filed: January 26, 2007
    Publication date: July 23, 2009
    Applicant: THALLION PHARMACEUTICALS INC.
    Inventors: Patrick Morris, Faustinus Yeboah, James McAlpine, Maxime Ranger, Emmanuelle Roux, Michael Harvey
  • Patent number: 7501510
    Abstract: The invention provides N,N?-disubstituted monothiourea or bis-thiourea-Pd(0) complexes that are useful as catalysts for palladium-catalyzed Heck reaction of aryl iodides and bromides with olefins, and as catalysts for palladium catalyzed Suzuki reactions of organoboric compounds and aryl halides.
    Type: Grant
    Filed: March 24, 2005
    Date of Patent: March 10, 2009
    Assignee: The University of Hong Kong
    Inventors: Dan Yang, Ying-Chun Chen