Polycyclo Ring System Which Contains The Hetero Ring As One Of The Cyclos Patents (Class 540/546)
  • Patent number: 9090627
    Abstract: Compounds relating to batrachotoxin are provided, in particular analogs that modulate the activity of sodium channels. Also provided are pharmaceutical compositions comprising compounds of the invention and a pharmaceutically acceptable carrier, including vehicles that modulate transdermal permeation of the compound. The subject compounds are useful in treatments, including treatments to reduce neuronal activity or to bring about muscular relaxation. The compounds also find use in the treatment of subjects suffering from a voltage-gated sodium channel-enhanced ailment or from pain. Further methods are provided for the preparation of the batrachotoxin-related compounds.
    Type: Grant
    Filed: December 13, 2013
    Date of Patent: July 28, 2015
    Assignee: The Board of Trustees of the Leland Stanford Junior University
    Inventors: Justin Du Bois, Abigail Sloan Devlin, Matthew M. Logan, Frederic Menard, Tatsuya Toma
  • Patent number: 9040519
    Abstract: This disclosure is directed to fused tetracyclic pyrido[4,3-b>]indole and pyrido[3,4-b]indole derivatives. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.
    Type: Grant
    Filed: February 18, 2011
    Date of Patent: May 26, 2015
    Assignee: Medivation Technologies, Inc.
    Inventors: Sarvajit Chakravarty, Barry Patrick Hart, Rajendra Parasmal Jain
  • Patent number: 8980879
    Abstract: The present invention provides for compounds of formula (I) wherein R1, R2, R6, Y1, Y2, A1, A2, A3, and A4 have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions, including inflammatory diseases, cancer, and AIDS. Also provided are pharmaceutical compositions comprising one or more compounds of formula (I).
    Type: Grant
    Filed: March 11, 2014
    Date of Patent: March 17, 2015
    Assignee: AbbVie Inc.
    Inventors: Dachun Liu, John Pratt, Le Wang, Lisa A. Hasvold, Andrew Bogdan
  • Publication number: 20150018298
    Abstract: Compounds for use in the treatment of human immunodeficiency virus (HIV) infection are disclosed. The compounds have the following Formula (I): including stereoisomers and pharmaceutically acceptable salts thereof, wherein R1, X, Y1, Y2, or L are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.
    Type: Application
    Filed: July 11, 2014
    Publication date: January 15, 2015
    Inventors: Mingzhe Ji, Scott E. Lazerwith, Hyung-Jung Pyun
  • Patent number: 8927535
    Abstract: The present invention provides cyclopropyl-fused-1,3-thiazepines of formula I having BACE1 and/or BACE2 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease and type 2 diabetes.
    Type: Grant
    Filed: June 29, 2012
    Date of Patent: January 6, 2015
    Assignee: Hoffman-La Roche Inc.
    Inventor: Thomas Woltering
  • Publication number: 20140343039
    Abstract: There is provided a process for preparing cephalotaxine esters corresponding to the following general formula I, which comprises the cephalotaxine backbone, and that can be written as C(R1)(R2)(XH)COO[CTX], wherein CTX represents the cephalotaxine backbone, being optionally substituted, the process consisting in bringing the corresponding cephalotaxine compound, or salts, isomers or tautomeric forms thereof, which is free or which is in the form of a metal alkoxide CTXOM, into contact with a heterocyclic side chain precursor having both a bifunctional protected (bidentate) and activated (acylating) form of an acid bearing a hydrogenated heteroatom, in the alpha (?) position with respect to the carboxyl group, and corresponding to the following general formula: in a customary aprotic solvent, preferably with a catalyst which may be a hindered tertiary amine, at a temperature of between ?80° C. and +100° C., preferably in the range 0 to 30° C.
    Type: Application
    Filed: June 6, 2014
    Publication date: November 20, 2014
    Inventors: Jean-Pierre ROBIN, Nina RADOSEVIC, Julie BLANCHARD
  • Publication number: 20140303144
    Abstract: Hydrogenated pyrido[4,3-b]indoles, pyrido[3,4-b]indoles and azepino[4,5-b]indoles are described. The compounds may bind to and are adrenergic receptor ?2B antagonists. The compounds may also bind to and antagonize adrenergic receptor ?2B. The compounds may find use in therapy, e.g., to (i) reduce blood pressure and/or (ii) promote renal blood flow and/or (iii) decrease or inhibit sodium reabsorption. The compounds may also be used to treat diseases or conditions that are, or are expected to be, responsive to a decrease in blood pressure. Use of the compounds to treat cardiovascular and renal disorders is particularly described.
    Type: Application
    Filed: February 17, 2012
    Publication date: October 9, 2014
    Applicant: Medivation Technologies, Inc.
    Inventors: Andrew Asher Protter, Sarvajit Chakravarty
  • Publication number: 20140213571
    Abstract: The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.
    Type: Application
    Filed: August 20, 2012
    Publication date: July 31, 2014
    Inventors: Nigel J. Liverton, Casey Cameron McComas, Joerg Habermann, Uwe Koch, Frank Narjes, Peng Li, Xuanjia Peng, Richard Soll, Hao Wu, Anandan Palani, Shuwen He, Xing Dai, Hong Liu, Zhong Lai, Clare London, Dong Xiao, Nicolas Zorn, Ravi Nargund
  • Publication number: 20140170111
    Abstract: The present invention relates to novel Fused Tetracycle Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein A, A?, B, G, R1, U, V, W, W?, X, X?, Y and Y? are as defined herein. The present invention also relates to compositions comprising at least one Fused Tetracycle Derivative, and methods of using the Fused Tetracycle Derivatives for treating or preventing HCV infection in a patient.
    Type: Application
    Filed: September 28, 2011
    Publication date: June 19, 2014
    Applicant: Merck Sharp & Dohmn Corp.
    Inventors: Craig A. Coburn, Brian J. Lavey, Michael P. Dwyer, Joseph A. Kozlowski, Stuart B. Rosenblum
  • Publication number: 20140171410
    Abstract: Compounds relating to batrachotoxin are provided, in particular analogues that modulate the activity of sodium channels. Also provided are pharmaceutical compositions comprising compounds of the invention and a pharmaceutically acceptable carrier, including vehicles that modulate transdermal permeation of the compound. The subject compounds are useful in treatments, including treatments to reduce neuronal activity or to bring about muscular relaxation. The compounds also find use in the treatment of subjects suffering from a voltage-gated sodium channel-enhanced ailment or from pain. Further methods are provided for the preparation of the batrachotoxin-related compounds.
    Type: Application
    Filed: December 13, 2013
    Publication date: June 19, 2014
    Applicant: The Board of Trustees of the Leland Stanford Junior University
    Inventors: Justin Du Bois, Abigail Sloan Devlin, Matthew M. Logan, Frederic Menard, Tatsuya Toma
  • Publication number: 20130237524
    Abstract: Disclosed embodiments concern polycyclic alkaloid compounds and methods for their use and synthesis. Particular embodiments concern polycyclic alkaloids having a fused, six-membered ring, while other embodiments concern polycyclic alkaloids having a fused, five-membered ring. Methods for making the polycyclic alkaloids are disclosed, as well as methods for their use as prophylactics or treatments for certain diseases. Also disclosed are pharmaceutical compositions comprising the polycyclic alkaloids and their use.
    Type: Application
    Filed: March 7, 2013
    Publication date: September 12, 2013
    Applicant: Rigel Pharmaceuticals, Inc.
    Inventors: Dane Goff, Donald G. Payan, Sylvia Braselmann
  • Publication number: 20130225558
    Abstract: This disclosure is directed to fused tetracyclic pyrido[4,3-b>]indole and pyrido[3,4-b]indole derivatives. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.
    Type: Application
    Filed: February 18, 2011
    Publication date: August 29, 2013
    Inventors: Sarvajit Chakravarty, Barry Patrick Hart, Rajendra Parasmal Jain
  • Publication number: 20130217672
    Abstract: A (+)-3-hydroxymorphinan-based polycycle derivative of formula (I) is effective as a neuroprotective agent for neurodegenerative diseases including Alzheimer's disease, Parkinson's disease, Huntington's disease, amyotrophic lateral sclerosis, and ischemic stroke.
    Type: Application
    Filed: May 13, 2011
    Publication date: August 22, 2013
    Applicant: GREEN CROSS CORPORATION
    Inventors: Jinhwa Lee, Jong Yup Kim, Jeongmin Kim, Kwang Woo Ahn
  • Publication number: 20130210803
    Abstract: This disclosure is directed to fused tetracyclic pyrido[4,3-b]indoles and pyrido[3,4-b]indoles. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.
    Type: Application
    Filed: February 18, 2011
    Publication date: August 15, 2013
    Inventors: Sarvajit Chakravarty, Barry Patrick Hart, Rajendra Parasmal Jain
  • Publication number: 20130039904
    Abstract: The present invention discloses a gamboge acid cyclization analogs, their preparation methods and applications by semi-synthesis with the following structural formula I-III: Where ring A, ring B or/and ring C is 4-10 membered saturated or/and unsaturated aliphatic ring aliphatic heterocycle or aryl heterocycle. R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11 or/and R12 is, independently at each occurrence, optionally substituted substituent of glycosyl, multi-hydroxyl, amino acid, acyloxy, phosphoric acid oxy, sulfonyloxy, alkoxy, aryloxy, heterocyclic oxy, thiol, aliphatic or cyclic group containing oxygen, sulfur, nitrogen or phosphorus, one of the substituents or combinations thereof. The present invention has antitumor activity management, antiviral, antibacterial and antifungal activity management, as anti-tumor, anti-viral, immune, antibacterial and antifungal agents, with other known anti-tumor, anti-viral, immune, together with the application of antibacterial and antifungal.
    Type: Application
    Filed: August 2, 2010
    Publication date: February 14, 2013
    Applicant: Liaoning Lifeng Scientific & Technology Development Company Ltd.
    Inventor: Lifeng Xu
  • Patent number: 8367655
    Abstract: The present invention discloses pyridoindolobenzox- and thiazepine compositions of Formula 1, wherein A is —CH(R9)—X—, —XCH(R9)—; —CO—X— or —X—CO—; X is —O—, —S—, —SO—, or —SO2—. Y is a single bond or a double bond. D and E are independently —(CH2)n—; and ‘n’ varies from 0 to 2. R1 to R9 are various electron donating, electron withdrawing, hydrophilic, or lipophilic groups selected to optimize the physicochemical and biological properties of compounds of Formula I.
    Type: Grant
    Filed: July 2, 2010
    Date of Patent: February 5, 2013
    Assignee: Daya Drug Discoveries, Inc.
    Inventor: Parthasarathi Rajagopalan
  • Publication number: 20120253036
    Abstract: An agent for treating fibromyalgia containing a 5-HT2C receptor agonist as an active ingredient
    Type: Application
    Filed: December 10, 2010
    Publication date: October 4, 2012
    Inventors: Yukinori Nagakura, Mina Tsukamoto, Tomonari Watabiki
  • Publication number: 20120232057
    Abstract: Fused [1,2]imidazo[4,5-c] ring compounds (e.g., imidazo[4,5-c]quinolines, 6,7,8,9-tetrahydroimidazo[4,5-c]quinolines, imidazo[4,5-c]naphthyridines, and 6,7,8,9-tetrahydroimidazo[4,5-c]naphthyridines) with a —CH(—X1—R1)— group in the fused ring at the 1-position of the imidazo ring, 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: Application
    Filed: May 25, 2012
    Publication date: September 13, 2012
    Inventors: George W. GRIESGRABER, Tushar A. KSHIRSAGAR, Azim A. CELEBI, Sarah J. SLANIA, Michael E. DANIELSON, Michael J. RICE, Joshua R. WURST
  • Patent number: 8188306
    Abstract: Novel compounds useful for inhibiting the 90kDa heat shock proteins containing a quinone-like moiety and a di-hydroxy phenol like moiety, similar to geldanamycin and radicicol.
    Type: Grant
    Filed: September 30, 2009
    Date of Patent: May 29, 2012
    Assignee: University of Kansas
    Inventors: Brian S. J. Blagg, Gang Shen
  • Publication number: 20120070409
    Abstract: The present invention relates to a tetracyclic fused heterocyclic compound represented by the following formula [I] wherein each symbol is as defined in the specification, or a pharmaceutically acceptable a salt thereof, and a hepatitis C virus (HCV) polymerase inhibitor and a therapeutic agent for hepatitis C containing this compound. The compound of the present invention shows an anti-HCV activity based on the HCV polymerase inhibitory activity, and useful as an agent for the prophylaxis or treatment of hepatitis C.
    Type: Application
    Filed: February 3, 2011
    Publication date: March 22, 2012
    Applicant: Japan Tobacco Inc.
    Inventors: Takahiro Oka, Kazutaka Ikegashira, Shintaro Hirashima, Hiroshi Yamanaka, Satoru Noji, Yasushi Niwa, Yoko Matsumoto, Toshihiro Sato, Izuru Ando, Yukihiro Nomura
  • Publication number: 20120058989
    Abstract: Compounds having antibacterial activity are disclosed. The compounds have the following structure (I): including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein A, B, D, E, G, R1, R2, R3, R4, R5, R6 and R7 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.
    Type: Application
    Filed: April 7, 2011
    Publication date: March 8, 2012
    Applicant: Achaogen, Inc.
    Inventors: Allan S. Wagman, Heinz E. Moser, Glenn A. McEnroe, James B. Aggen, Martin S. Linsell, Adam A. Goldblum, John H. Griffin, Lloyd J. Simons, Thomas R. Belliotti, Christina R. Harris, Toni-Jo Poel, Michael J. Melnick, Ricky D. Gaston
  • 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
  • Patent number: 8063037
    Abstract: The present invention provides new progesterone receptor modulators which are dibenzo[b,f]pyrido[1,2-d]oxazepine-2-amines or dibenzo[b,f]prido[1,2-d]thiazepine-2-amines, and uses thereof.
    Type: Grant
    Filed: May 6, 2008
    Date of Patent: November 22, 2011
    Assignee: N. V. Organon
    Inventors: Johannes Bernardus Maria Rewinkel, Brigitte Johanna Bernita Folmer, Maria Lourdes Ollero, Hemen Ibrahim
  • Publication number: 20110269743
    Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases, disorders or conditions that would benefit from inhibition of SOC channel activity.
    Type: Application
    Filed: September 22, 2009
    Publication date: November 3, 2011
    Applicant: CalciMedica, Inc
    Inventors: Jeffrey P. Whitten, Yazhong Pei, Kenneth A. Stauderman, Jack Roos
  • Publication number: 20110237567
    Abstract: This invention is directed to tricyclic spiro-oxindole derivatives of formula (I), wherein j, k, m, n, w, q, Y, Q, X, R1, R2 and R3 are as defined herein, as a stereoisomer, enantiomer, tautomer thereof or mixtures thereof; or a pharmaceutically acceptable salt, solvate or prodrug thereof, which are useful for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain. Pharmaceutical compositions comprising the compounds and methods of preparing and using the compounds are also disclosed.
    Type: Application
    Filed: October 12, 2007
    Publication date: September 29, 2011
    Applicant: XENON PHARMACEUTICALS INC.
    Inventors: Mikhail Chafeev, Sultan Chowdhury, Jianmin Fu, Ranjender Kamboj
  • Patent number: 8022203
    Abstract: New aminoalkoxyimino derivatives at position 3 of substituted B-homoandrostanes and B-heteroandrostanes, processes for their preparation, and to pharmaceutical compositions containing them for the treatment of cardiovascular disorders, such as heart failure and hypertension. In particular compounds having the general formula (I) are described, where the radicals have the meanings described in detail in the application.
    Type: Grant
    Filed: May 31, 2007
    Date of Patent: September 20, 2011
    Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.
    Inventors: Alberto Cerri, Barbara Moro, Maco Torri, Giulio Carzana, Giuseppe Bianchi, Mara Ferrandi, Patrizia Ferrari, Maria Pia Zappavigna, Leonardo Banfi, Giuseppe Giacalone
  • Patent number: 7989442
    Abstract: The present invention provides new progesterone receptor modulators which are (cis)-8-fluorodibenzo[b,f]pyrido[1,2-d]oxazepine-1-amine compounds and uses thereof.
    Type: Grant
    Filed: September 26, 2007
    Date of Patent: August 2, 2011
    Assignee: N.V. Organon
    Inventors: Johannes Bernardus Maria Rewinkel, Brigitte Johanna Bernita Folmer, Maria Lourdes Ollero, Hemen Ibrahim
  • Publication number: 20110003840
    Abstract: The present invention discloses pyridoindolobenzox- and thiazepine compositions of Formula 1, wherein A is —CH(R9)—X—, —XCH(R9)—; —CO—X— or —X—CO—; X is —O—, —S—, —SO—, or —SO2—. Y is a single bond or a double bond. D and E are independently —(CH2)n—; and ‘n’ varies from 0 to 2. R1 to R9 are various electron donating, electron withdrawing, hydrophilic, or lipophilic groups selected to optimize the physicochemical and biological properties of compounds of Formula I.
    Type: Application
    Filed: July 2, 2010
    Publication date: January 6, 2011
    Applicant: Daya Drug Discoveries, Inc.
    Inventor: Parthasarathi Rajagopalan
  • Publication number: 20100160291
    Abstract: This invention is directed to tricyclic spiro-oxindole derivatives of formula (I), wherein j, k, m, n, w, q, Y, Q, X, R1, R2 and R3 are as defined herein, as a stereoisomer, enantiomer, tautomer thereof or mixtures thereof; or a pharmaceutically acceptable salt, solvate or prodrug thereof, which are useful for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain. Pharmaceutical compositions comprising the compounds and methods of preparing and using the compounds are also disclosed.
    Type: Application
    Filed: October 12, 2007
    Publication date: June 24, 2010
    Applicant: XENON PHARMACEUTICALS INC.
    Inventors: Mikhail Chafeev, Sultan Chowdhury, Jianmin Fu, Ranjender Kamboj
  • Patent number: 7737136
    Abstract: The present invention provides compounds according to general Formula (I), a prodrug thereof, a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable salt of a prodrug thereof. More particularly, the present invention provides high affinity non-steroidal compounds which are agonists, partial agonists or antagonists of the progesterone receptor.
    Type: Grant
    Filed: April 1, 2003
    Date of Patent: June 15, 2010
    Assignee: N.V. Organon
    Inventors: Pedro Harold Han Hermkens, Hans Lucas, Paul Peter Marie Antonius Dols, Johannes Bernardus Maria Rewinkel, Brigitte Johanna Bernita Folmer
  • Publication number: 20100120742
    Abstract: Disclosed is a compound represented by the general formula shown below, which can bind to a retinoid X receptor (RXR), which is one of nuclear receptors, and exhibit an agonistic or antagonistic action. [Wherein, R1 is selected from the group consisting of an alkyl group, an alkenyl group, an alkynyl group and an aryl group. R2 is selected from the group consisting of an alkoxy group, an alkyl group, an alkenyl group, an alkynyl group and an aryl group. W is NR3 or CR3; and R3 is selected from a hydrogen, an alkyl group, an alkenyl group, an alkynyl group and an aryl group. X1 and Y1 are selected from CH or N. X2 and Y2 are selected from CH, CR4 or N. R4 is selected from an alkyl group, an alkenyl group, an alkynyl group, an alkoxy group, a halogen, a nitro group and an amino group. Z is selected from a carboxylic acid, a carboxylate ester or a hydroxamic acid, which is bound directly or via an alkyl group, an alkenyl group or an alkynyl group.
    Type: Application
    Filed: February 26, 2008
    Publication date: May 13, 2010
    Applicant: National University Corporation Okayama University
    Inventors: Hiroki Kakuta, Kenji Sasaki, Kayo Takamatsu, Atsushi Takano, Nobumasa Yakushji, Kazunore Morohashi, Kenichi Morishita
  • Patent number: 7659263
    Abstract: The present invention relates to a thienopyrrole compound represented by the following formula [I] wherein each symbol is as defined in the specification, or a pharmaceutically acceptable a salt thereof, and a hepatitis C virus (HCV) polymerase inhibitor and a therapeutic agent for hepatitis C containing this compound as an active ingredient. The compound of the present invention shows an anti-HCV activity based on the HCV polymerase inhibitory activity, and useful as an agent for the prophylaxis or treatment of hepatitis C.
    Type: Grant
    Filed: November 10, 2005
    Date of Patent: February 9, 2010
    Assignee: Japan Tobacco Inc.
    Inventors: Ryo Mizojiri, Takahiro Oka, Kenta Aoki, Satoru Noji, Yoko Matsumoto, Toshihiro Sato, Izuru Ando, Yasushi Niwa
  • Publication number: 20100029612
    Abstract: The present invention provides a combinatorial approach to a library of novel compounds having four diversity points. The compounds provide for the mapping of urotensin II and somatostatin 5 receptors by differential binding of said receptors. The present invention further relates to a method of treating diseases for which modulation of the urotensin II receptor produces a physiologically beneficial response in said disease, such as those associated with CNS function and cardiovascular diseases. The present invention further relates to pharmaceutical compositions comprising these agents for the treatment of these diseases adapted to modulate the urotensin II receptor.
    Type: Application
    Filed: February 18, 2004
    Publication date: February 4, 2010
    Inventor: Roger Olsson
  • Patent number: 7625929
    Abstract: The invention relates to the compounds of general formula (I) where R1 represents H, a (C1-C4)alkyl, —CO(C1-C4)alkyl, (C1-C4)alkylphenyl or —CO-phenyl group, said phenyl being optionally substituted, R2 represents H, a halogen atom, an —S(O)zR3, —NHSO2R3, —NHSO2-phenyl or —NHSO2—(C1-C4)alkylphenyl group where z is equal to 0, 1 or 2 and where R3 represents a (C1-C4)alkyl group, said phenyl being optionally substituted; A is chosen from where n is equal to 0, 1 or 2, R4 and R5 represent H, a (C1-C4)alkyl, hydroxyl, cyano, phenyl, benzyl, piperidyl, —CONH2, —CO-phenyl, —COOR3, —CH(phenyl) (OH) and —C(phenyl)2(OH) group, or R4 and R5 form together an optionally substituted 6-membered aromatic ring, R6 represents H, a (C1-C4)alkyl, phenyl or benzyl group, and B represents a 5- or 6-membered nitrogen-containing heterocycle or homocycle optionally fused with a phenyl Group or optionally substituted; their addition salts; their method of preparation and their therapeutic application.
    Type: Grant
    Filed: May 26, 2003
    Date of Patent: December 1, 2009
    Assignee: sanofi-aventis
    Inventors: Philippe R. Bovy, Roberto Cecchi, Tiziano Croci, Olivier Venier
  • Patent number: 7605288
    Abstract: Novel compounds useful for inhibiting the 90 kDa heat shock proteins containing a quinone-like moiety and a di-hydroxy phenol like moiety, similar to geldanamycin and radicicol.
    Type: Grant
    Filed: March 26, 2007
    Date of Patent: October 20, 2009
    Assignee: University of Kansas
    Inventors: Brian Blagg, Gang Shen, Randell C. Clevenger
  • Publication number: 20090221551
    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: Application
    Filed: March 14, 2007
    Publication date: September 3, 2009
    Inventors: Tushar A. Kshirsagar, Karl J. Manske, Larry R. Krepski, Joan T. Moseman, George W. Griesgraber, Sarah Johannessen Slania, Philip D. Heppner
  • Publication number: 20090131401
    Abstract: Substituted benzoimidazole compounds useful as anti-infectives that decrease resistance, virulence, or growth of microbes are provided. Methods of making and using substituted benzoimidazole compounds, as well as pharmaceutical preparations thereof, in, e.g., reducing antibiotic resistance and inhibiting biofilms.
    Type: Application
    Filed: February 12, 2008
    Publication date: May 21, 2009
    Applicant: Paratek Pharmaceuticals, Inc.
    Inventors: Stuart B. Levy, Michael N. Alekshun, Brent L. Podlogar, Kwasi Ohemeng, Atul K. Verma, Tadeusz Warchol, Beena Bhatia, Todd Bowser, Mark Grier
  • Patent number: 7527654
    Abstract: The present invention relates to a process for dyeing keratin fibers, in particular human keratin fibers such as the hair, using a dye composition comprising at least one dye of styryl or imine type in the presence of a revealing composition comprising at least one optionally substituted (hetero) aromatic compound of weak acid type. The present invention makes it possible in particular to obtain a chromatic and fast coloration of keratin fibers, which is visible even on dark hair without prior lightening. The invention also makes it possible to obtain a coloration which, under certain conditions, does not stain.
    Type: Grant
    Filed: October 12, 2007
    Date of Patent: May 5, 2009
    Assignee: L'Oreal S.A.
    Inventor: Grégory Plos
  • Publication number: 20090054400
    Abstract: The present invention provides new progesterone receptor modulators which are dibenzo[b,f]pyrido[1,2-d]oxazepine-2-amines or dibenzo[b,f]prido[1,2-d]thiazepine-2-amines, and uses thereof.
    Type: Application
    Filed: May 6, 2008
    Publication date: February 26, 2009
    Inventors: Johannes Bernardus Maria Rewinkel, Brigitte Johanna Bernita Folmer, Maria Lourdes Ollero, Hemen Ibrahim
  • Publication number: 20080269192
    Abstract: Fused [1,2]imidazo[4,5-c] ring compounds (e.g., imidazo[4,5-c]quinolines, 6,7,8,9-tetrahydroimidazo[4,5-c]quinolines, imidazo[4,5-c]naphthyridines, and 6,7,8,9-tetrahydroimidazo[4,5-c]naphthyridines) with a —CH(—X1—R1)-group in the fused ring at the 1-position of the imidazo ring, 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: Application
    Filed: December 29, 2005
    Publication date: October 30, 2008
    Applicant: Coley Pharmaceutical Group, Inc.
    Inventors: George W. Griesgraber, Tushar A. Kshirsagar, Azim A. Celebi, Sarah J. Slania, Michael E. Danielson, Michael J. Rice, Joshua R. Wurst
  • Patent number: 7390797
    Abstract: The present invention provides a novel fused indazole compound having an excellent JNK inhibitory action. More specifically, it provides a compound represented by the following formula, a salt thereof or a hydrate of them. Wherein Z11 and Z12 each independently represent a carbonyl group, a methylene group, etc.; represents a double bond or a single bond; R1a represents a hydrogen atom, etc.; the ring A represents a benzene ring, a naphthalene ring or a 5- to 10-membered aromatic heterocyclic ring, etc.; and R2a, R2b and R2c each independently represent (1) a hydrogen atom, (2) a halogen atom, (3) a nitro group, etc.
    Type: Grant
    Filed: February 21, 2003
    Date of Patent: June 24, 2008
    Assignee: Eisai Co., Ltd.
    Inventors: Norihito Ohi, Nobuaki Sato, Naohiro Kohmura
  • Publication number: 20080113966
    Abstract: Compounds of Formula (I): and Formula (II): (where variables R2, R4, A, B, D, W, X, Y and Z are as defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache. 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: October 12, 2005
    Publication date: May 15, 2008
    Inventors: Christopher S. Burgey, Daniel V. Paone, Anthony W. Shaw, Diem N. Nguyen, Zhengwu J. Deng, Theresa M. Williams, Joseph P. Vacca, Craig M. Potteiger, Harold G. Selnick
  • Publication number: 20080009619
    Abstract: The invention relates to a novel process for the preparation of asenapine, i.e. trans-5-chloro-2-methyl-2,3,3a,12b-tetrahydro-1H-dibenz[2,3:6,7]oxepino[4,5-c]pyrrole, as well as to novel intermediate products for use in said process.
    Type: Application
    Filed: July 3, 2007
    Publication date: January 10, 2008
    Applicant: N.V. Organon
    Inventors: Gerardus Johannes Kemperman, Timothy Lee Stuk, Jacobus Johannes Maria Van Der Linden
  • Patent number: 7304051
    Abstract: Amidophenyl-sulfonylamino-quinoxaline compounds of formula (I) are CCK2 modulators useful in the treatment of CCK2 mediated diseases.
    Type: Grant
    Filed: August 4, 2004
    Date of Patent: December 4, 2007
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Brett D. Allison, Michael D. Hack, Victor K. Phuong, Michael H. Rabinowitz, Mark D. Rosen
  • Patent number: 7148347
    Abstract: Disclosed is a process for preparing a macrocyclic compound of the formula (I): which is carried out using an intermediate of the formula (II): wherein W, R1 through R4, D, A and R12 are as defined herein. The compounds of formula (I) are potent active agents for the treatment of hepatitis C virus (HCV) infection.
    Type: Grant
    Filed: April 6, 2004
    Date of Patent: December 12, 2006
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Joerg Brandenburg, Kai Donsbach, Hans-Dieter Ecker, Rogelio Perez Frutos, Fabrice Gallou, Dieter Gutheil, Nizar Haddad, Robert Hagenkoetter, Dirk Kemmer, Jutta Kroeber, Thomas Nicola, Juergen Schnaubelt, Michael Schul, Robert Donald Simpson, Xudong Wei, Eric Winter, Yibo Xu, Nathan K. Yee
  • Patent number: 7105506
    Abstract: Compounds of structural formula (I) and use of the compounds and salts and solvates thereof, as therapeutic agents.
    Type: Grant
    Filed: May 2, 2002
    Date of Patent: September 12, 2006
    Assignee: Lilly Icos LLC
    Inventors: Mark W. Orme, Jason S. Sawyer, Lisa M. Schultze
  • Patent number: 6852715
    Abstract: The invention provides compounds of formula (1) wherein R1 is a hydrogen atom, an alkyl group having 1 to 6 carbon atoms or an alkoxy group having 1 to 6 carbon atoms; and R2 is a hydrogen atom, an alkyl group having 1 to 6 carbon atoms or an alkoxy group having 1 to 6 carbon atoms; and pharmaceutically acceptable salts thereof. The invention also relates to a process for obtaining the compounds, compositions containing them and their therapeutic use. The compounds display excellent activity against mammalian cancer cell lines.
    Type: Grant
    Filed: June 28, 2000
    Date of Patent: February 8, 2005
    Assignee: Instituto Biomar S.A.
    Inventors: Dolores Garcia Gravalos, Julia Perez, Librada Maria Cañedo, Francisco Romero, Fernando Espliego
  • Patent number: 6849203
    Abstract: The invention relates to photoisomerizable compounds of formula I wherein A, Z, L, R, R1, k, m and r are defined herein.
    Type: Grant
    Filed: April 5, 2002
    Date of Patent: February 1, 2005
    Assignee: Merck Patent Gesellschaft Mit Beschraenkter Haftung
    Inventors: Louise Diane Farrand, Christopher Worrall, Owain Llyr Parri
  • Publication number: 20040254160
    Abstract: The present invention relates to compounds of formula (I), wherein variable groups are as defined within; pharmaceutically acceptable salts, solvates, solvates of such salts and prodrugs thereof and their use as ileal bile acid transport (IBAT) inhibitors for the treatment of hyperlipidaemia. Processes for their manufacture and pharmaceutical compositions containing them are also described.
    Type: Application
    Filed: July 23, 2004
    Publication date: December 16, 2004
    Inventors: Ingemar Starke, Mikael ulf Johan Dahlstrom, David Blomberg, Suzanne Alenfalk, Peter Nordberg, Andreas Christer Wallberg, Stig Jonas Bostrom
  • Patent number: RE39679
    Abstract: The present invention is directed to certain novel compounds represented by structural Formula (I) or pharmaceutically acceptable salt forms thereof, wherein R1, R5, R6a, R6b, R7, R8, R9, X, b, k, m, and n, and the dashed lines are described herein. The invention is also concerned with pharmaceutical formulations comprising these novel compounds as active ingredients and the use of the novel compounds and their formulations in the treatment of certain disorders. The compounds of this invention are serotonin agonists and antagonists and are useful in the control or prevention of central nervous system disorders including obesity, anxiety, depression, psychosis, schizophrenia, sleep disorders, sexual disorders, migraine, conditions associated with cephalic pain, social phobias, and gastrointestinal disorders such as dysfunction of the gastrointestinal tract motility.
    Type: Grant
    Filed: February 16, 2006
    Date of Patent: June 5, 2007
    Assignee: Bristol-Myers Squibb Pharma Company
    Inventors: Albert J. Robichaud, Taekyu Lee, Wei Deng, Ian S. Mitchell, Michael Guang Yang, Simon Haydar, Wenting Chen, Christopher D. McClung, Emile J. B. Calvello, David M. Zawrotny, Parthasarathl Rajagopalan