Polycyclo Ring System Having A 1,2-diazine Ring As One Of The Cyclos Patents (Class 544/233)
  • Patent number: 10160766
    Abstract: The present invention relates a novel compound represented by the following Formula 3 or Formula 5, and a pharmaceutical composition having superior anti-inflammatory effect comprising the above. The above compound inhibits the translocation of HMGB1 form nucleus to cytosol, and then has remarkable effect of treating or preventing inflammatory disease, especially sepsis.
    Type: Grant
    Filed: November 1, 2017
    Date of Patent: December 25, 2018
    Assignees: Spark Biopharma, Inc., Seoul National University R&DB Foundation
    Inventors: Seung Bum Park, Wan Sang Cho, Ja Young Koo
  • Patent number: 9034485
    Abstract: The present invention relates to compounds of the formula (1) and to the use thereof in organic electronic devices, and to organic electronic devices which comprise compounds of the formula (1), preferably as hole-transport materials and/or as emitting materials.
    Type: Grant
    Filed: December 22, 2009
    Date of Patent: May 19, 2015
    Assignee: Merck Patent GmbH
    Inventors: Arne Buesing, Holger Heil, Philipp Stoessel, Amir Hossain Parham, Rocco Fortte, Jonas Valentin Kroeber
  • Publication number: 20150073145
    Abstract: A method for the synthesis of carbon-based structures, particularly graphene substructures and ribbons, from oligo- and poly-alkyne starting materials.
    Type: Application
    Filed: November 14, 2014
    Publication date: March 12, 2015
    Inventors: Igor Alabugin, Philip M. Byers
  • Patent number: 8940412
    Abstract: An organic electroluminescence device and a material for producing the organic electroluminescence device. The organic electroluminescence device includes an organic thin film layer between a cathode and an anode, the organic thin film layer including one or more layers, in which the organic thin film layer includes one or more light emitting layers and at least one of the light emitting layers includes a phosphorescent material and a host material. The host material has an essential structure in which a naphthalene ring is bonded to a fluorene skeleton, dibenzofuran skeleton, or dibenzothiophene skeleton. The organic electroluminescence device is a phosphorescent device having high efficiency and long lifetime.
    Type: Grant
    Filed: December 22, 2009
    Date of Patent: January 27, 2015
    Assignee: Idemitsu Kosan Co., Ltd.
    Inventors: Yoriyuki Takashima, Toshihiro Iwakuma, Toshinari Ogiwara, Chishio Hosokawa, Mitsunori Ito
  • Publication number: 20150018356
    Abstract: Provided are certain fused tetra or penta-cyclic compounds and salts thereof, compositions thereof, and methods of use thereof.
    Type: Application
    Filed: December 31, 2011
    Publication date: January 15, 2015
    Inventors: Changyou Zhou, Bo Ren, Hexiang Wang
  • Publication number: 20140256717
    Abstract: There is provided compounds of formula I, wherein R1, R2a, R2b, R2c, X, Y, Z, R3 and ring A/B have meanings given in the description, and pharmaceutically-acceptable esters, amides, solvates or salts thereof, which compounds are useful in the treatment of diseases in which inhibition of a protein or lipid kinase (e.g. PI3-K, particularly class I PI3K, PIM family kinase and/or mTOR) is desired and/or required, and particularly in the treatment of cancer. The invention also relates to combinations containing such compounds.
    Type: Application
    Filed: May 18, 2012
    Publication date: September 11, 2014
    Applicant: Centro Nacional de Investigaciones Oncológicas (CNIO)
    Inventors: Joaquín Pastor Fernández, Rosa Maria Álvarez Escobar, Rosario Concepción Riesco Fagundo, Ana Belén García García, Antonio Rodríguez Hergueta, Jose Ignacio Martin Hernando, Carmen Blanco Aparicio, David Álvaro Cebrián Muñoz
  • Patent number: 8815863
    Abstract: Novel compound having the following formula: (I) wherein Y is N, O, or S. Also disclosed are a pharmaceutical compositions comprising the same, methods for treating cancer using the same, and methods for the synthesis of the same. The novel compounds of the present invention are found to inhibit protein kinases, especially Checkpoint kinase Chk1/Chk2.
    Type: Grant
    Filed: September 17, 2010
    Date of Patent: August 26, 2014
    Inventor: Zhanggui Wu
  • Patent number: 8772295
    Abstract: The present disclosure provides compounds that function as modulators of aldehyde dehydrogenase (ALDH) enzymatic activity, as well as compositions and formulations comprising the compounds. The present disclosure provides therapeutic methods involving administering a subject compound, or a subject pharmaceutical composition.
    Type: Grant
    Filed: January 22, 2013
    Date of Patent: July 8, 2014
    Assignee: The Board of Trustees of the Leland Stanford Junior University
    Inventors: Daria Mochly-Rosen, Che-Hong Chen, Wenjin Yang
  • Publication number: 20140031357
    Abstract: The invention relates to the new, asymmetrically substituted derivatives of 2,7-dihydro-3H-dibenzo[de,h]cinnoline-3,7-dione and their use as cytostatics exhibiting activity against tumor cells, especially against cells with multidrug resistance (MDR). In particular, the invention concerns derivatives of 2,7-dihydro-3H-dibenzo[de,h]cinnoline-3,7-dione represented by the general formula (I).
    Type: Application
    Filed: April 13, 2012
    Publication date: January 30, 2014
    Applicant: BS-154 SP. Z O.O.
    Inventors: Edward Borowski, Barbara Stefanska, Maria Dzieduszycka, Marcin Cybulski, Wieslaw Szelejewski, Janusz Obukowicz, Maria Bontemps-Gracz, Malgorzata Wysocka, Jan Mazerski, Pawel Punda, Joanna Wietrzyk
  • Patent number: 8623901
    Abstract: The invention relates to novel 1,6-disubstituted pyrazolopyrimidinones of formula (I), in which Hc is a tetrahydropyranyl-group and R1 is the group V?W?*, whereby V and W independently of each other may be an aryl group or an heteroaryl group, which independently of each other may optionally be substituted. According to one aspect of the invention the new compounds are for use as medicaments or for the manufacture of medicaments, in particular medicaments for the treatment of conditions concerning deficits in perception, concentration, learning or memory. The new compounds are also for the manufacture of medicaments and/or for use in the treatment of e.g. Alzheimer's disease, in particular for cognitive impairment associated with Alzheimer's disease.
    Type: Grant
    Filed: March 30, 2010
    Date of Patent: January 7, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Riccardo Giovannini, Cornelia Dorner-Ciossek, Christian Eickmeier, Dennis Fiegen, Thomas Fox, Klaus Fuchs, Niklas Heine, Holger Rosenbrock, Gerhard Schaenzle
  • Publication number: 20130296307
    Abstract: Provided herein are compounds according to Formula I and pharmaceutically acceptable salts thereof, and compositions comprising the same, for use in various methods, including treating cancers such as colon, ovarian, pancreatic, breast, liver, prostate and hematologic cancers:
    Type: Application
    Filed: July 10, 2013
    Publication date: November 7, 2013
    Inventors: John Hood, Sunil Kumar KC, David Mark Wallace
  • Publication number: 20130285036
    Abstract: The present invention relates to aromatic nitrogen heterocycles, and to electronic devices, in particular organic electroluminescent devices, which comprise these aromatic nitrogen heterocycles, in particular in a hole-injection layer and/or in a hole-transport layer and/or in a hole-blocking layer and/or in an electron-transport layer and/or in an emitting layer.
    Type: Application
    Filed: December 15, 2011
    Publication date: October 31, 2013
    Applicant: MERCK PATENT GMBH
    Inventors: Philipp Stoessel, Arne Buesing, Esther Breuning, Christof Pflumm, Amir Hossain, Thomas Eberle, Teresa Mujica-Fernaud
  • Patent number: 8552201
    Abstract: The present invention relates to derivatives of 5,6-bisaryl-2-pyridine-carboxamide, their preparation and their application in therapeutics as antagonists of urotensin II receptors.
    Type: Grant
    Filed: December 29, 2011
    Date of Patent: October 8, 2013
    Assignee: Sanofi
    Inventors: Jean-Michel Altenburger, Valérie Fossey, Philip Janiak, Gilbert Lassalle, Frédéric Petit, Jean Claude Vernieres
  • Patent number: 8552183
    Abstract: The present invention relates to a process for linking two molecules by means of a Diels Alder reaction with inverse electron requirement (DARinv), comprising the following steps: reaction of a (a) triazine or tetrazine with one or more electron-attracting substituents on the ring as a diene component, the electron-attracting substituents being selected from: COOR C(O)NR2 CX3 (X=halogen) halogen CN SO2—R or SO3—R PR2 wherein R?H, alkyl, aryl, heterocycle, which in turn may be substituted, where appropriate, with alkyl, OH, SH, halogen, aryl, heterocycle, nitro, carboxyamido or amine group.
    Type: Grant
    Filed: June 18, 2007
    Date of Patent: October 8, 2013
    Assignee: Deutsches Krebsforschungszentrum Stiftung des Offentlichen Rechts
    Inventors: Manfred Wiessler, Eduard Müller, Peter Lorenz, Christian Kliem, Heinz Fleischhacker
  • Patent number: 8541423
    Abstract: The present application relates to compounds and methods for treating pain, incontinence and other conditions.
    Type: Grant
    Filed: April 11, 2012
    Date of Patent: September 24, 2013
    Assignee: Hydra Biosciences, Inc.
    Inventors: Magdalene M. Moran, Christopher Fanger, Jayhong A. Chong, Colleen McNamara, Xiaoguang Zhen, Josh Mandel-Brehm
  • Patent number: 8389522
    Abstract: The present disclosure provides compounds that function as modulators of aldehyde dehydrogenase (ALDH) enzymatic activity, as well as compositions and formulations comprising the compounds. The present disclosure provides therapeutic methods involving administering a subject compound, or a subject pharmaceutical composition.
    Type: Grant
    Filed: October 19, 2009
    Date of Patent: March 5, 2013
    Assignee: The Board of Trustees of the Leland Stanford Junior University
    Inventors: Daria Mochly-Rosen, Che-Hong Chen, Wenjin Yang
  • Patent number: 8278311
    Abstract: The present application describes substituted pyrimidine compounds of formula (I) wherein X, A1, R1, R2, R3, R4, R5, R6, R7, R8, R9, p, q, r, v, and w are defined in the specification, compositions comprising such compounds, methods for making the compounds, and methods of treating and preventing the progression of diseases, conditions and disorders using such compounds and compositions.
    Type: Grant
    Filed: April 27, 2009
    Date of Patent: October 2, 2012
    Assignee: Abbott Laboratories
    Inventors: Huaqing Liu, Irene Drizin, Marlon D. Cowart, Robert J. Altenbach
  • Patent number: 8188087
    Abstract: The present invention relates to novel crystalline forms of (3-cyano-1H-indol-7-yl)-[4-(4-fluorophenethyl)piperazin-1-yl]methanone phosphate and to pharmaceutical compositions containing said forms.
    Type: Grant
    Filed: April 24, 2007
    Date of Patent: May 29, 2012
    Assignee: Merck Patent GmbH
    Inventors: Susan Marie Reutzel-Eden, Gregory Alan Stephenson
  • Patent number: 8153647
    Abstract: Disclosed are compounds according to formula (I): wherein A, Q, X, Y, Z, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 and R11 are as defined herein. The disclosure also relates to pharmaceutical compositions containing a compound of formula (I), to processes for preparing the compounds of formula (I), and to methods of using the compounds of formula (I).
    Type: Grant
    Filed: December 15, 2008
    Date of Patent: April 10, 2012
    Assignee: Sanofi-Aventis
    Inventors: Jozsef Zsolt Bocskei, Gary McCort, Hans Matter, Henning Steinhagen, Bérangère Thiers
  • Publication number: 20120001154
    Abstract: An aromatic amine derivative represented by the following formula (1), wherein at least one of Ar1 to Ar3 is represented by the following formula (2), wherein X1 to X3 are independently a nitrogen atom or CR2, provided that two of X1 to X3 are a nitrogen atom and X1 and X3 are not simultaneously a nitrogen atom.
    Type: Application
    Filed: August 27, 2010
    Publication date: January 5, 2012
    Inventor: Tomoki Kato
  • Patent number: 8088788
    Abstract: [1,2]Imidazo[4,5-c] ring compounds (e.g., imidazo[4,5-c]quinolines, imidazo[4,5-c]naphthyridines, and imidazo[4,5-c]pyridines) substituted with a fused ring containing an oxygen and/or nitrogen atom attached at the 1- and/or 2-position, pharmaceutical compositions containing the compounds, intermediates, methods of making the compounds, and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases, are disclosed.
    Type: Grant
    Filed: March 14, 2007
    Date of Patent: January 3, 2012
    Assignee: 3M Innovative Properties Company
    Inventors: Tushar A. Kshirsagar, Karl J. Manske, Larry R. Krepski, Joan T. Moseman, George W. Griesgraber, Sarah Johannessen Slania, Scott E. Langer, Philip D. Heppner
  • Publication number: 20110301151
    Abstract: Molecular mimics of Smac are capable of modulating apoptosis through their interaction with cellular IAPs (inhibitor of apoptosis proteins). The mimetics are based on a monomer or dimer of the N-terminal tetrapeptide of IAP-binding proteins, such as Smac/DIABLO, Hid, Grim and Reaper, which interact with a specific surface groove of IAP. Also disclosed are methods of using these peptidomimetics for therapeutic purposes.
    Type: Application
    Filed: August 2, 2011
    Publication date: December 8, 2011
    Inventors: Stephen M. Condon, Matthew G. LaPorte, Yijun Deng, Susan R. Rippin
  • Patent number: 8058457
    Abstract: A star-shaped oligothiophene-arylene derivative in which an oligothiophene having p-type semiconductor characteristics is bonded to an arylene having n-type semiconductor characteristics positioned in the central moiety of the molecule and forms a star shape with the arylene, thereby simultaneously exhibiting both p-type and n-type semiconductor characteristics. Further, an organic thin film transistor using the oligothiophene-arylene derivative. The star-shaped oligothiophene-arylene derivative can be spin-coated at room temperature, leading to the fabrication of organic thin film transistors simultaneously satisfying the requirements of high charge carrier mobility and low off-state leakage current.
    Type: Grant
    Filed: February 17, 2010
    Date of Patent: November 15, 2011
    Assignee: Samsung Electronics Co., Ltd.
    Inventors: Kook Min Han, Eun Jeong Jeong, Chang Ju Kim, Eun Kyung Lee
  • Patent number: 7994187
    Abstract: HIV inhibitory compounds of formula: salts, hydrates, solvates, N-oxides, or stereoisomers thereof, wherein A forms pyridine, pyrimidine, pyrazine, pyridazine, triazine, imidazole, pyrazole, triazole, tetrazole, oxazole, isoxazole, oxadiazole, thiazole, isothiazole, and thiadiazole; R1 is halo, cyano, nitro, C1-6alkyl, polyhaloC1-6alkyl, —C1-6alkyl-OR4, —C(?O)—R5, —C(?O)—OR4, —C(?O)—NR6R7, —OR4, —O—C(?O)—C1-6alkyl, —O—C1-6alkyl-OR4, —O—C1-6alkyl-NR6R7, —O—C1-6alkyl-O—C(?O)—C1-6alkyl, —O—C1-6alkyl-C(?O)—OR4, —O—C1-6alkyl-C(?O)—NR6R7, —NR6R7, —NR8—C(?O)—R5, —NR8—C(?O)—OR4, —NR8—C(?O)—NR6R7, —NR8—C(?O)—C1-6alkyl-C(?O)—OR4, —NR8—C1-6alkyl-OR4, —NR8—C1-6alkyl-NR6R7, —NR8—C1-6alkyl-imidazolyl, —NR8—SO2R9, —N?CH—NR6R7, —NH—C(?NH)—NH2, —SO2NR6R7, and —O—PO(OR8)2; D forms pyridine, pyrimidine, pyrazine, pyridazine, pyrrole, imidazole, pyrazole, furane, oxazole, isoxazole, thiophene, thiazole, and isothiazole; R2 is C1-6alkyl, polyhaloC1-6alkyl, halo, cyano, —COOR4, —OR4, and —NR6R7; R3 is phenyl, pyridyl, pyrimid
    Type: Grant
    Filed: April 3, 2007
    Date of Patent: August 9, 2011
    Assignee: Tibotec Pharmaceuticals Ltd.
    Inventors: Bart Rudolf Romanie Kesteleyn, Wim Bert Griet Schepens
  • Publication number: 20110136812
    Abstract: The invention provides compounds of formula I: wherein A, B, W, Y, Z, and R1 have any of the meanings defined in the specification and their pharmaceutically acceptable salts. The invention also provides pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I, and therapeutic methods for treating cancer using compounds of formula I.
    Type: Application
    Filed: August 5, 2010
    Publication date: June 9, 2011
    Applicant: Rutgers, The State University of New Jersey
    Inventors: Edmond J. LaVoie, Alexander L. Ruchelman, Leroy F. Liu
  • Patent number: 7951817
    Abstract: Compounds represented by the formula: wherein R is C1-6 alkyl; C4-6 cycloalkylalkyl; or C3-6 alkenyl; R? is H or C1-6 alkyl; X is H or OH; Y is alkyl, cycloalkyl, aryl, heteroaryl, arylalkyl or aroyl; and Z is CH or N; provided that X is H, when Z is CH and R is C4 cycloalkylalkyl or C4 alkenyl; prodrugs thereof; and pharmaceutically acceptable salts thereof are provided. Compounds of the above formula are useful as analgesics for treating pain; as immunomodulators, to modulate the behavioral effects of drugs of abuse and to modulate the development of tolerance and dependence to ? agonists.
    Type: Grant
    Filed: March 19, 2009
    Date of Patent: May 31, 2011
    Assignees: The United States of America as represented by the Department of Health and Human Services, Southern Research Institute, University of New England College of Osteopathic Medicine, The Arizona Board of Regents on Behalf of the University of Arizona
    Inventors: Subramaniam Ananthan, Richard B. Rothman, Edward J. Bilsky, Frank Porreca
  • Patent number: 7858627
    Abstract: The invention provides compounds of formula I or formula II: wherein: the bond represented by is a single bond or a double bond, and R1—R5, X, and Y have any of the meanings defined in the specification and their pharmaceutically acceptable salts. The invention also provides pharmaceutical compositions comprising a compound of formula I or II, processes for preparing compounds of formula I or II, intermediates useful for preparing compounds of formula I or II, and therapeutic methods for treating cancer and other topoisomerase related conditions using compounds of formula I or II.
    Type: Grant
    Filed: April 13, 2009
    Date of Patent: December 28, 2010
    Assignee: Rutgers, The State University of New Jersey
    Inventors: Edmond J. LaVoie, Alexander L. Ruchelman, Leroy F. Liu
  • Patent number: 7851464
    Abstract: Compounds of formula I: (wherein variables A1, A2, A3, A4, A5, A6, A7, E1, E2, E3, E4, E5, G1, G2, J and K 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: Grant
    Filed: November 14, 2006
    Date of Patent: December 14, 2010
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Ian M. Bell, Harold G. Selnick, Michael R. Wood, Cory R. Theberge, Craig A. Stump, Steven N. Gallicchio, C. Blair Zartman
  • Publication number: 20100273801
    Abstract: The invention relates to compouns derived from betulin, and to the use thereof as antibacterial agents in pharmaceutical and cosmetic applications.
    Type: Application
    Filed: June 6, 2007
    Publication date: October 28, 2010
    Applicant: Valition teknillinen tutikimuskeskus
    Inventors: Jari Yli-Kauhaluoma, Salme Koskimies, Sami Alakurtti, Taru Mäkelä, Päivi Tammela
  • Publication number: 20100240664
    Abstract: The invention provides compounds of formula I: wherein A, B, W, Y, Z, and R1 have any of the meanings defined in the specification and their pharmaceutically acceptable salts. The invention also provides pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I, and therapeutic methods for treating cancer using compounds of formula I.
    Type: Application
    Filed: May 28, 2010
    Publication date: September 23, 2010
    Applicant: Rutgers, the State University of New Jersey
    Inventors: Edmond J. LaVoie, Alexander L. Ruchelman
  • Patent number: 7781587
    Abstract: The invention provides compounds of formula I: wherein A, B, W, Y, Z, and R1 have any of the meanings defined in the specification and their pharmaceutically acceptable salts. The invention also provides pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I, and therapeutic methods for treating cancer using compounds of formula I.
    Type: Grant
    Filed: March 27, 2009
    Date of Patent: August 24, 2010
    Assignee: Rutgers, the State University of New Jersey
    Inventors: Edmond J. LaVoie, Alexander L. Ruchelman, Leroy F. Liu
  • Publication number: 20100190795
    Abstract: The invention relates to betulin derivatives, and to the use thereof as agents against protozoa of the genus Leishmania and against leishmaniasis in applications of pharmaceutical industry.
    Type: Application
    Filed: June 6, 2007
    Publication date: July 29, 2010
    Applicant: Valtion Teknillinen tutkimuskeskus
    Inventors: Jari Yli-Kauhaluoma, Sami Alakurtti, Jaana Minkkinen, Nina Sarcerdoti-Sierra, Charles L. Jaffe, Tuomo Heiska
  • Patent number: 7754718
    Abstract: The present invention relates to novel antiviral helioxanthin analogs. These compounds may particularly be used alone or in combination with other drugs for the treatment of the following: hepadnaviruses, flaviviruses, herpesviruses and human immunodeficiency virus. In addition, compounds according to the present invention can be used to prevent or reduce the likelihood of the occurrence of tumors secondary to virus infection as well as other infections or disease states that are secondary to the virus infection.
    Type: Grant
    Filed: May 2, 2005
    Date of Patent: July 13, 2010
    Assignee: Yale University
    Inventors: Hosup Yeo, David J. Austin, Ling Li, Yung-chi Cheng
  • Patent number: 7750006
    Abstract: A method of treatment of a disease of the human or animal body mediated by PARP comprising administering to such a subject a therapeutically effective amount of a compound of formula: or an isomer, salt, solvate, chemically protected form, and prodrug thereof, wherein: A and B together represent an optionally substituted, fused aromatic ring; RC is represented by -L-RL, where L is of formula: —(CH2)n1-Qn2-(CH2)n3— wherein n1, n2 and n3 are each selected from 0, 1, 2 and 3, the sum of n1, n2 and n3 is 1, 2 or 3 and Q is selected from O, S, NH, C(?O) or —CR1R2—, where R1 and R2 are independently selected from hydrogen, halogen or optionally substituted C1-7 alkyl, or may together with the carbon atom to which they are attached form a C3-7 cyclic alkyl group, which may be saturated (a C3-7 cycloalkyl group) or unsaturated (a C3-7 cycloalkenyl group), or one of R1 and R2 may be attached to an atom in RL to form an unsaturated C3-7 cycloalkenyl group which comprises the carbon atoms to which R1 and R2 are a
    Type: Grant
    Filed: February 10, 2006
    Date of Patent: July 6, 2010
    Assignees: Kudos Pharmaceuticals Limited, Maybridge PLC
    Inventors: Niall Morrison Barr Martin, Graeme Cameron Murray Smith, Charles Richard White, Roger Frank Newton, Diane Gillian Douglas, Penny Jane Eversley, Julia Vile
  • Patent number: 7737272
    Abstract: Transition metal complexes include a diazaphosphacycle of formula III and a transition metal. The phosphorus atom of the diazaphosphacycle is bonded to the transition metal and the diazaphosphacycle of formula III has the following structure where the variables have the values set forth herein.
    Type: Grant
    Filed: February 15, 2008
    Date of Patent: June 15, 2010
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Clark R. Landis, Wiechang Jin, Jonathan S. Owen, Thomas P. Clark
  • Patent number: 7713975
    Abstract: Methods for treating an allergic or inflammatory disease or other Syk-mediated disease or Syk-mediated condition characterized by administering a composition which contains a therapeutically effective amount of a 3,6-substituted imidazol[1,2-b]pyridazine compound.
    Type: Grant
    Filed: January 12, 2006
    Date of Patent: May 11, 2010
    Assignee: Alcon, Inc.
    Inventors: Mark R. Hellberg, Steven T. Miller, Andrew Rusinko
  • Patent number: 7692029
    Abstract: A star-shaped oligothiophene-arylene derivative in which an oligothiophene having p-type semiconductor characteristics is bonded to an arylene having n-type semiconductor characteristics positioned in the central moiety of the molecule and forms a star shape with the arylene, thereby simultaneously exhibiting both p-type and n-type semiconductor characteristics. Further, an organic thin film transistor using the oligothiophene-arylene derivative. The star-shaped oligothiophene-arylene derivative can be spin-coated at room temperature, leading to the fabrication of organic thin film transistors simultaneously satisfying the requirements of high charge carrier mobility and low off-state leakage current.
    Type: Grant
    Filed: April 28, 2005
    Date of Patent: April 6, 2010
    Assignee: Samsung Electronics Co., Ltd.
    Inventors: Kook Min Han, Eun Jeong Jeong, Chang Ju Kim, Eun Kyung Lee
  • Publication number: 20100069360
    Abstract: A compound of formula (I) or a pharmaceutically acceptable salt or prodrug ester thereof: wherein the groups R1, R2, R3, R7 and X are as defined in the specification.
    Type: Application
    Filed: August 28, 2007
    Publication date: March 18, 2010
    Inventors: Laszlo Revesz, Achim Schlapbach, Rudolf Walchli
  • Patent number: 7662821
    Abstract: The invention relates to tetrahydronaphthalene derivatives, process for their production and their use as anti-inflammatory agents.
    Type: Grant
    Filed: October 12, 2004
    Date of Patent: February 16, 2010
    Assignee: Bayer Schering Pharma AG
    Inventors: Hartmut Rehwinkel, Stefan Baeurle, Markus Berger, Norbert Schmees, Heike Schaecke, Konrad Krolikiewicz, Anne Mengel, Duy Nguyen, Stefan Jaroch, Werner Skuballa
  • Patent number: 7662818
    Abstract: Compounds of the formula (I): wherein A and B together represent an optionally substituted, fused aromatic ring; X can be NRX or CRXRY; if X=NRX then n is 1 or 2 and if X=CRXRY then n is 1; RX is selected from the group consisting of H, optionally substituted C1-20 alkyl, C5-20 aryl, C3-20 heterocyclyl, amido, thioamido, ester, acyl, and sulfonyl groups; RY is selected from H, hydroxy, amino; or RX and RY may together form a spiro-C3-7 cycloalkyl or heterocyclyl group; RC1 and RC2 are both hydrogen, or when X is CRXRY, RC1, RC2, RX and RY, together with the carbon atoms to which they are attached, may form an optionally substituted fused aromatic ring; and R1 is selected from H and halo.
    Type: Grant
    Filed: December 23, 2005
    Date of Patent: February 16, 2010
    Assignees: Kudos Pharmaceuticals Limited, Maybridge Limited
    Inventors: Niall Morrison Barr Martin, Graeme Cameron Smith, Stephen Philip Jackson, Vincent Junior M Loh, Xiao-Ling Fan Cockcroft, Ian Timothy Williams Matthews, Keith Allan Menear, Frank Kerrigan, Alan Ashworth
  • Publication number: 20100016545
    Abstract: The present invention relates to a process for linking two molecules by means of a Diels Alder reaction with inverse electron requirement (DARinv), comprising the following steps: reaction of a (a) triazine or tetrazine with one or more electron-attracting substituents on the ring as a diene component, the electron-attracting substituents being selected from: COOR C(O)NR2 CX3 (X=halogen) halogen CN SO2—R or SO3—R PR2 wherein R?H, alkyl, aryl, heterocycle, which in turn may be substituted, where appropriate, with alkyl, OH, SH, halogen, aryl, heterocycle, nitro, carboxyamido or amine group.
    Type: Application
    Filed: June 18, 2007
    Publication date: January 21, 2010
    Applicant: DEUTSCHES KREBSFORSCHUNGSZENTRUM STIFTUNG DES OFFENTLICHEN RECHTS
    Inventors: Manfred Wiessler, Eduard Müller, Peter Lorenz, Christian Kliem, Heinz Fleischhacker
  • Publication number: 20090239871
    Abstract: The invention provides compounds of formula I: wherein A, B, W, Y, Z, and R1 have any of the meanings defined in the specification and their pharmaceutically acceptable salts. The invention also provides pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I, and therapeutic methods for treating cancer using compounds of formula I.
    Type: Application
    Filed: March 27, 2009
    Publication date: September 24, 2009
    Applicant: Rutgers, The State University of New Jersey
    Inventors: Edmond J. LaVoie, Alexander L. Ruchelman, Leroy F. Liu
  • Publication number: 20090221529
    Abstract: This invention relates to the design, synthesis and use of synthetic vitamin D and other steroidal analogs. It further relates to the therapeutic use of such analogs and their manufacture.
    Type: Application
    Filed: December 12, 2006
    Publication date: September 3, 2009
    Applicant: Women's & Infants Hospital of Rhode Island
    Inventors: Laurent Brard, Satyan Kalkunde, Rakesh Kumar Singh
  • Publication number: 20090215766
    Abstract: The present invention provides compounds that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases and cancer.
    Type: Application
    Filed: August 6, 2008
    Publication date: August 27, 2009
    Inventors: James D. Rodgers, Darius J. Robinson, Argyrios G. Arvanitis, Thomas P. Maduskuie, JR., Stacey Shepard, Louis Storace, Haisheng Wang, Maria Rafalski, Ravi Kumar Jalluri, Andrew P. Combs, Matthew L. Crawley
  • Patent number: 7576201
    Abstract: A compound for electrochromic devices. One such compound of the invention is dihydro-disubstituted phenazine (VI): wherein R9 is and n=1-10.
    Type: Grant
    Filed: February 28, 2008
    Date of Patent: August 18, 2009
    Assignee: Ntera Limited
    Inventors: Donald Fitzmaurice, David Cummins, David Corr, S. Nagaraja Rao, Gerrit Boschloo
  • Publication number: 20090198051
    Abstract: An intermediate compound for total synthesis of ecteinascidins comprising, a compound represented by general formula 2 having thioether group at C4 site, and the substituent R2 of N12 site is trichloroethoxicarbonyl (Troc) to which various substituents can be introduced by mild condition, further having 10 members ring structure which can be converted to a ring of other numbered members.
    Type: Application
    Filed: April 25, 2007
    Publication date: August 6, 2009
    Inventors: Tohru FUKUYAMA, Toshiyuki KAN
  • Publication number: 20090170855
    Abstract: HIV inhibitory compounds of formula: salts, hydrates, solvates, N-oxides, or stereoisomers thereof, wherein A forms pyridine, pyrimidine, pyrazine, pyridazine, triazine, imidazole, pyrazole, triazole, tetrazole, oxazole, isoxazole, oxadiazole, thiazole, isothiazole, and thiadiazole; R1 is halo, cyano, nitro, C1-6alkyl, polyhaloC1-6alkyl, —C1-6alkyl-OR4, —C(?O)—R5, —C(?O)—OR4, —C(?O)—NR6R7, —OR4, —O—C(?O)—C1-6alkyl, —O—C1-6alkyl-OR4, —O—C1-6alkyl-NR6R7, —O—C1-6alkyl-O—C(?O)—C1-6alkyl, —O—C1-6alkyl-C(?O)—OR4, —O—C1-6alkyl-C(?O)—NR6R7, —NR6R7, —NR8—C(?O)—R5, —NR8—C(?O)—OR4, —NR8—C(?O)—NR6R7, —NR8—C(?O)—C1-6alkyl-C(?O)—OR4, —NR8—C1-6alkyl-OR4, —NR8—C1-6alkyl-NR6R7, —NR8—C1-6alkyl-imidazolyl, —NR8—SO2R9, —N?CH—NR6R7, —NH—C(?NH)—NH2, —SO2NR6R7, and —O—PO(OR8)2; D forms pyridine, pyrimidine, pyrazine, pyridazine, pyrrole, imidazole, pyrazole, furane, oxazole, isoxazole, thiophene, thiazole, and isothiazole; R2 is C1-C6alkyl, polyhaloC1-C6alkyl, halo, cyano, —COOR4, —OR4, and —NR6R7; R3 is phenyl, pyridyl, p
    Type: Application
    Filed: April 3, 2007
    Publication date: July 2, 2009
    Inventors: Bart Rudolf Romanie Kesteleyn, Wim Bert Griet Schepens
  • Patent number: 7541364
    Abstract: Compounds represented by the formula: wherein R is C1-6 alkyl; C4-6 cycloalkylalkyl; or C3-6 alkenyl; R? is H or C1-6 alkyl; X is H or OH; Y is alkyl, cycloalkyl, aryl, heteroaryl, arylalkyl or aroyl; and Z is CH or N; provided that X is H, when Z is CH and R is C4 cycloalkylalkyl or C4 alkenyl; prodrugs thereof; and pharmaceutically acceptable salts thereof are provided. Compounds of the above formula are useful as analgesics for treating pain; as immunomodulators, to modulate the behavioral effects of drugs of abuse and to modulate the development of tolerance and dependence to ? agonists.
    Type: Grant
    Filed: August 27, 2004
    Date of Patent: June 2, 2009
    Assignee: Southern Research Institute
    Inventors: Subramaniam Ananthan, Richard B. Rothman, Edward J. Bilsky, Frank Porreca
  • Patent number: RE44338
    Abstract: This invention relates to a method of imaging amyloid deposits and to labeled compounds, and methods of making labeled compounds useful in imaging amyloid deposits. This invention also relates to compounds, and methods of making compounds for inhibiting the aggregation of amyloid proteins to form amyloid deposits, and a method of delivering a therapeutic agent to amyloid deposits.
    Type: Grant
    Filed: July 17, 2012
    Date of Patent: July 2, 2013
    Assignee: The Trustees Of The University Of Pennsylvania
    Inventors: Hank F. Kung, Mei-Ping Kung, Zhi-Ping Zhuang, Virginia M. Y. Lee, John Q. Trojanowski, Daniel M. Skovronsky
  • Patent number: RE44354
    Abstract: This invention relates to a method of imaging amyloid deposits and to labeled compounds, and methods of making labeled compounds useful in imaging amyloid deposits. This invention also relates to compounds, and methods of making compounds for inhibiting the aggregation of amyloid proteins to form-amyloid deposits, and a method of delivering a therapeutic agent to amyloid deposits.
    Type: Grant
    Filed: July 17, 2012
    Date of Patent: July 9, 2013
    Assignee: The Trustees Of The University Of Pennsylvania
    Inventors: Hank F. Kung, Mei-Ping Kung, Zhi-Ping Zhuang, Virginia M. Y. Lee, John Q. Trojanowski, Daniel M. Skovronsky