Polycyclo Ring System Which Contains The Hetero Ring As One Of The Cyclos Patents (Class 540/555)
Two of the cyclos share at least three ring members or a ring member is shared by three of the cyclos (e.g., bridged, peri-fused, etc.) (Class 540/556)
Tricyclo ring system which contains the hetero ring as one of the cyclos (Class 540/557)
Bicyclo ring system which contains the hetero ring as one of the cyclos (Class 540/567)
  • Substituted benzo[5,6][1,4]diazepino[1,2-a]indoles for the treatment of proliferative disorders
    Patent number: 11793885
    Abstract: The invention relates to novel benzodiazepine derivatives with antiproliferative activity and more specifically to novel benzodiazepine compounds of formulae (I), (II) and (III). The invention also provides conjugates of the benzodiazepine compounds linked to a cell-binding agent. The invention further provides compositions and methods useful for inhibiting abnormal cell growth or treating a proliferative disorder in a mammal using the compounds or conjugates of the invention.
    Type: Grant
    Filed: December 27, 2018
    Date of Patent: October 24, 2023
    Assignee: IMMUNOGEN, INC.
    Inventors: Michael Louis Miller, Manami Shizuka, Ravi V. J. Chari
  • Antibody-drug conjugates comprising substituted benzo[e]pyrrolo[1,2-?][1,4]diazepines
    Patent number: 11628223
    Abstract: A novel antibody-pyrrolodiazepine derivative and a novel antibody-pyrrolodiazepine derivative conjugate using the same, comprising substituted benzo[e]pyrrolo[1,2-a][1,4]diazepines represented by the [Formula 24], [Formula 25], [Formula 26], and/or [Formula 27].
    Type: Grant
    Filed: September 28, 2018
    Date of Patent: April 18, 2023
    Assignee: DAIICHI SANKYO COMPANY, LIMITED
    Inventors: Narihiro Toda, Yusuke Ota, Fuminao Doi, Masaki Meguro, Ichiro Hayakawa, Shinji Ashida, Takeshi Masuda, Takashi Nakada, Mitsuhiro Iwamoto, Naoya Harada, Tomoko Terauchi, Daisuke Okajima, Kensuke Nakamura, Hiroaki Uchida, Hirofumi Hamada
  • Optoelectronic component and method for producing an optoelectronic component
    Patent number: 10910531
    Abstract: An optoelectronic component and a method for producing an optoelectronic component are disclosed. In an embodiment an optoelectronic component includes an optical element including silicone as a polymer material, the silicone having repeating units of cyclic siloxane and of linear siloxane which are arranged in alternation, wherein the optoelectronic component is configured to emit radiation.
    Type: Grant
    Filed: August 16, 2017
    Date of Patent: February 2, 2021
    Assignee: OSRAM OLED GMBH
    Inventors: Patrick Wenderoth, Ulf Betke, Guido Kickelbick
  • Methods for preparing substituted 12a,13-dihydro-6H-benzo[5,6][1,4]diazepino[1,2-a]indol-6-ones
    Patent number: 10442809
    Abstract: The invention provides novel methods for preparing indolinobenzodiazepine monomer compounds and their synthetic precursors.
    Type: Grant
    Filed: April 19, 2018
    Date of Patent: October 15, 2019
    Assignee: IMMUNOGEN, INC.
    Inventors: Baudouin Gérard, Richard A. Silva, Michael Louis Miller, Manami Shizuka
  • Organic electroluminescent compound and organic electroluminescent device comprising the same
    Patent number: 9997724
    Abstract: The present disclosure relates to an organic electroluminescent compound and an organic electroluminescent device comprising the same. The organic electroluminescent compound of the present disclosure has good color purity, solubility, and thermal stability. By comprising the organic electroluminescent compound of the present disclosure, an organic electroluminescent device showing low driving voltage, excellent current and power efficiencies, and significantly improved lifespan can be provided.
    Type: Grant
    Filed: September 25, 2015
    Date of Patent: June 12, 2018
    Assignee: Rohm and Haas Electronic Materials Korea Ltd.
    Inventors: Bitnari Kim, Hee-Ryong Kang, Hyun-Ju Kang, Jin-Ri Hong, Young-Mook Lim, Doo-Hyeon Moon
  • COMPOUNDS FOR TREATING DISORDERS MEDIATED BY METABOTROPIC GLUTAMATE RECEPTOR 5, AND METHODS OF USE THEREOF
    Publication number: 20140349992
    Abstract: Provided herein are compounds and methods of synthesis thereof. The compounds set forth herein are useful for the treatment, prevention, and/or management of various disorders, such as neurological disorders, neurodegenerative disorders, neuropsychiatric disorders, disorders of cognition, learning or memory, gastrointestinal disorders, lower urinary tract disorder, and cancer. Compounds set forth herein modulate the activity of metabotropic glutamate receptor 5 (mGluR5) in the central nervous system or the periphery. Pharmaceutical formulations containing the compounds and their methods of use are also provided herein.
    Type: Application
    Filed: June 9, 2014
    Publication date: November 27, 2014
    Applicant: Sunovion Pharmaceuticals Inc.
    Inventors: Larry Wendell Hardy, Michele L.R. Heffernan, Frank Xinhe Wu, Lakshmi D. Saraswat, Kerry L. Spear
  • MODULATORS OF OPIOID RECEPTORS AND METHODS OF USE THEREOF
    Publication number: 20140288050
    Abstract: Provided herein are compounds and methods of synthesis thereof. The compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as pain, neurological disorders, psychiatric disorders, and neuromuscular disorders. Compounds provided herein modulate the activity of opioid receptor (e.g., ?-opioid receptor) in the central nervous system or the periphery. Pharmaceutical formulations containing the compounds and their methods of use are also provided herein.
    Type: Application
    Filed: November 7, 2012
    Publication date: September 25, 2014
    Inventors: Scott Malcolm, Carrie Bowen, Laurence Melnick, Linghong Xie
  • TRICYCLIC AND TETRACYCLIC SYSTEMS ACTING UPON THE VASCULAR AND CENTRAL NERVOUS SYSTEMS
    Publication number: 20140275042
    Abstract: Tricyclic and tetracyclic derivatives of benzodiazepine, pyridodiazepine, and pyrimidodiazepine fused with 1,4-dihydropyridine derivatives are disclosed. The present derivatives can be obtained from derivatives containing a dihydropyridine ring reacting with compounds of the ortho-phenyldiamine, ortho-diaminopyridine, and ortho-diaminopyrimidine type, as well as some subsequent transformations and, tricyclic and tetracyclic derivatives can be obtained with a diazepine or diazepinone nucleus fused to a 1,4-dihydropyridine nucleus, having a substituted or unsubstituted ring of benzene, pyridine or pyrimidine. The present derivatives exhibit vascular and central nervous system therapeutic activity.
    Type: Application
    Filed: May 20, 2014
    Publication date: September 18, 2014
    Inventors: YAMILA VERDECIA REYES, Estael Ochoa Rodríguez, Alberto Ruiz Reyes, Yanier Nuñez Figueredo, Carmen Carillo Domínguez, Juan Enrique Tacoronte Morales, Livan Lázaro Alba Gutiérrez, Gilberto Lázaro Pardo Andreu
  • Materials for organic electroluminescent devices
    Patent number: 8835626
    Abstract: The present invention relates to compounds of the formula (1) which are suitable for use in electronic devices, in particular organic electroluminescent devices.
    Type: Grant
    Filed: February 25, 2011
    Date of Patent: September 16, 2014
    Assignee: Merck Patent GmbH
    Inventors: Amir Hossain Parham, Christof Pflumm, Teresa Mujica-Fernaud
  • Compounds for treating disorders mediated by metabotropic glutamate receptor 5, and methods of use thereof
    Patent number: 8772301
    Abstract: Provided herein are compounds and methods of synthesis thereof. The compounds set forth herein are useful for the treatment, prevention, and/or management of various disorders, such as neurological disorders, neurodegenerative disorders, neuropsychiatric disorders, disorders of cognition, learning or memory, gastrointestinal disorders, lower urinary tract disorder, and cancer. Compounds set forth herein modulate the activity of metabotropic glutamate receptor 5 (mGluR5) in the central nervous system or the periphery. Pharmaceutical formulations containing the compounds and their methods of use are also provided herein.
    Type: Grant
    Filed: December 17, 2010
    Date of Patent: July 8, 2014
    Assignee: Sunovion Pharmaceuticals, Inc.
    Inventors: Larry Wendell Hardy, Michele L. R. Heffernan, Frank Xinhe Wu, Kerry L. Spear, Lakshmi D. Saraswat
  • FUSED TETRACYCLE DERIVATIVES AND METHODS OF USE THEREOF FOR THE TREATMENT OF VIRAL DISEASES
    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
  • Methods for preparing pyrimidine derivatives useful as protein kinase inhibitors
    Patent number: 8637666
    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, comprises the step of: a) cyclizing a compound represented by Structural Formula A: under suitable reductive cyclization conditions to form a compound represented by Structural Formula B: wherein R10 is LG1 or —X1R1, and -LG1 is a suitable leaving group; and b) optionally, when R10 of Structural Formula (B) is LG1, further comprising the step of replacing the -LG1 of Structural Formula (B) with —X1R1 to form the compound represented by Structural Formula (I).
    Type: Grant
    Filed: March 20, 2012
    Date of Patent: January 28, 2014
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Jean-Damien Charrier, Steven Durrant, David Kay
  • Dibenzo[B,F][1,4]Oxazepin-11-yl-N-Hydroxybenzamides as HDAC Inhibitors
    Publication number: 20140011988
    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: February 14, 2013
    Publication date: January 9, 2014
    Inventors: Robert Deziel, Silvana Leit, Patrick Beaulieu, Yves Andre Chantigny, John Mancuso, Pierre Tessier, Gideon Shapiro, Richard Chesworth, David Smil
  • TRICYCLIC DERIVATIVES, PROCESS FOR THEIR PREPARATION AND THEIR USE AS KINASE INHIBITORS
    Publication number: 20130302416
    Abstract: New substituted tricyclic compounds of formula (I) are described, wherein R1, R2, X, Y, Z are herein defined, having protein kinase inhibiting activity. The invention includes methods to prepare the compounds of formula (I), pharmaceutical compositions containing them, and their use in therapy, in particular for the treatment of diseases caused by and/or associated with dysregulated activity of protein kinase.
    Type: Application
    Filed: January 19, 2012
    Publication date: November 14, 2013
    Applicant: NERVIANO MEDICAL SCIENCES S.R.L.
    Inventors: Marina Caldarelli, Francesco Casuscelli, Daniele Donati, Danilo Mirizzi, Francesca Quartieri, Marco Silvagni
  • Substituted benzo-pyrido-triazolo-diazepine compounds
    Patent number: 8541407
    Abstract: The present invention relates to substituted benzo-pyrido-triazolo-diazepine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted benzo-pyrido-triazolo-diazepine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds or pharmaceutical compositions to subjects in need thereof.
    Type: Grant
    Filed: March 31, 2011
    Date of Patent: September 24, 2013
    Assignee: ArQule, Inc.
    Inventors: Syed M. Ali, Mark A. Ashwell, Eugene Kelleher, Steffi Koerner, Jean-Marc Lapierre, Jeffrey S. Link, Yanbin Liu, Magdi Moussa, Rocio Palma, Manish Tandon, David Vensel, Neil Westlund, Hui Wu, Rui-Yang Yang
  • BENZODIAZEPINE DERIVATIVES, COMPOSITIONS AND METHODS FOR TREATING COGNITIVE IMPAIRMENT
    Publication number: 20130237530
    Abstract: This invention relates to benzodiazepine derivatives, compositions comprising therapeutically effective amounts of those benzodiazepine derivatives and methods of using those derivatives or compositions in treating central nervous system (CNS) disorders with cognitive impairment that are responsive to agonists of ?5 subunit containing GABAA receptor, e.g., age-related cognitive impairment, Mild Cognitive Impairment (MCI), dementia, Alzheimer's Disease (AD), prodromal AD, post traumatic stress disorder (PTSD), schizophrenia and cancer-therapy-related cognitive impairment.
    Type: Application
    Filed: November 15, 2011
    Publication date: September 12, 2013
    Applicant: AGENEBIO, INC.
    Inventor: John A. Lowe, III
  • Substituted benzo-pyrimido-tetrazolo-diazepine compounds
    Patent number: 8470812
    Abstract: The present invention relates to substituted benzo-pyrimido-tetrazolo-diazepine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted benzo-pyrimido-tetrazolo-diazepine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.
    Type: Grant
    Filed: December 29, 2010
    Date of Patent: June 25, 2013
    Assignee: ArQule, Inc.
    Inventors: Rui-Yang Yang, Jeffrey S. Link
  • Aromatic heterocyclic fused indolobenzadiazepine HCV NS5B inhibitors
    Patent number: 8431568
    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 are useful in treating those infected with HCV.
    Type: Grant
    Filed: March 24, 2009
    Date of Patent: April 30, 2013
    Assignee: Bristol-Myers Squibb Company
    Inventors: John A. Bender, Zhong Yang, John F. Kadow
  • Diazonium-free method to make an indazole intermediate in the synthesis of bicyclic 5-(trifluormethoxy)-1H-3-indazolecarboxylic acid amides
    Patent number: 8354536
    Abstract: The present invention provides novel methods for preparing 5-(trifluoromethoxy)-1H-3-indazolecarboxylic acid (3), which is a useful precursor for the preparation of bicyclic-5-trifluoromethoxy-1H-indazole-3-carboxylic acid amides of Formula (1). Compounds of Formula (1) are active as agonists and partial agonists of the nicotinic ?-7 receptor and are being studied for their use in the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain, such as for the treatment of Alzheimer's disease and schizophrenia, as well as other psychiatric and neurological disorders. The present methods are useful for preparing compound (3) on scale up levels.
    Type: Grant
    Filed: June 21, 2012
    Date of Patent: January 15, 2013
    Assignee: Hoffman-La Roche Inc.
    Inventors: Thomas Cleary, Yaohui Ji, Thimma Rawalpally
  • N-benzyl,N'-arylcarbonylpiperazine derivatives
    Patent number: 8314091
    Abstract: The present invention relates to N-benzyl,N?-arylcarbonylpiperazine derivatives having the general formula I to pharmaceutical compositions comprising the same, and to the use of a these N-benzyl,N?-arylcarbonylpiperazine derivatives for the manufacture of a medicament for treating or preventing atherosclerosis and related disorders associated with cholesterol and bile acids transport and metabolism.
    Type: Grant
    Filed: August 19, 2008
    Date of Patent: November 20, 2012
    Assignees: MSD OSS B.V., Pharmacopeia, Inc.
    Inventors: Koc-Kan Ho, Andrew Laird Roughton, Irina Neagu, Jui-Hsiang Chan, Nasrin Ansari, Michelle Lee Morris, Yajing Rong, Michael Ohlmeyer, Andrew John Cooke, Andrew Stanley Edwards, David Jonathan Bennett
  • COMPOSITION AND METHOD FOR TREATING COGNITIVE IMPAIRMENTS IN DOWN SYNDROM SUBJECTS
    Publication number: 20120283248
    Abstract: Compounds having inverse agonist functional selectivity for GABAA receptors containing the ?5 subunit for use as a medicament in the treatment of cognitive impairments in subjects suffering from Down syndrome. The use of these compounds is disclosed. Pharmaceutical compositions for such treatment can comprise these compounds or suitable pharmaceutically acceptable salt thereof, a polyethoxylated castor oil and dimethyl sulfoxide (DMSO). Methods are disclosed for enhancing cognitive function, or treating or lessening the severity of cognitive impairments, in subjects suffering from Down syndrome by administering to a subject in need thereof a pharmaceutically effective amount of one or more of these compounds.
    Type: Application
    Filed: August 24, 2010
    Publication date: November 8, 2012
    Applicant: CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE - CNRS
    Inventors: Marie-Claude Potier, Robert Dodd, Benoît Delatour, Jérôme Braudeau, Yann Herault
  • INHIBITORS OF HEPATITIS C VIRUS
    Publication number: 20120276051
    Abstract: A class of compounds that inhibit Hepatitis C Virus (HCV) is disclosed, along with compositions containing the compound, and methods of using the composition for treating individuals infected with HCV.
    Type: Application
    Filed: July 9, 2012
    Publication date: November 1, 2012
    Applicant: Presidio Pharmaceuticals, Inc.
    Inventors: Min Zhong, Leping Li
  • Substituted imidazo[1,5-A][1,2,4]triazolo[1,5-D][1,4]benzodiazepine derivatives
    Patent number: 8293730
    Abstract: The present invention is concerned with a method of treating Alzheimer's disease by administering a therapeutically effective amount of a substituted imidazo[1,5-a][1,2,4]triazolo[1,5-d][1,4]benzodiazepine of formula I wherein R1, R2, and R3 are as defined herein, and their pharmaceutically acceptable acid addition salts. The invention also provides novel compounds of formula I-A and pharmaceutical compositions containing them.
    Type: Grant
    Filed: November 16, 2009
    Date of Patent: October 23, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Henner Knust, Heinz Stadler, Andrew William Thomas
  • CHIRAL FUSED [1,2]IMIDAZO[4,5-c] RING COMPOUNDS
    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
  • Condensed Azepine Derivatives As Bromodomain Inhibitors
    Publication number: 20120202799
    Abstract: Benzodiazepine compounds of formula (I) and salts thereof, pharmaceutical compositions containing such compounds and their use in therapy.
    Type: Application
    Filed: November 3, 2010
    Publication date: August 9, 2012
    Inventors: Miriam Crowe, Alain Claude-Marie Daugan, Romain Luc Marie Gosmini, Richard Martin Grimes, Olivier Mirguet, Jacqueline Elizabeth Mordaunt
  • HISTAMINE H3 INVERSE AGONISTS AND ANTAGONISTS AND METHODS OF USE THEREOF
    Publication number: 20120172350
    Abstract: Provided herein are fused imidazolyl compounds, methods of synthesis, and methods of use thereof. The compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, including, e.g., neurological disorders and metabolic disorders. Compounds provided herein inhibit the activity of histamine H3 receptors and modulate the release of various neurotransmitters, such as, e.g., histamine, acetylcholine, norepinephrine, and dopamine (e.g. at the synapse). Pharmaceutical compositions containing the compounds and their methods of use are also provided herein.
    Type: Application
    Filed: September 9, 2010
    Publication date: July 5, 2012
    Applicant: SUNOVION PHARMACEUTICALS INC.
    Inventors: Milan Chytil, Sharon R. Engel, Qun Kevin Fang
  • Heterocyclic Radical or Diradical, The Dimers, Oligomers, Polymers, Dispiro Compounds and Polycycles Thereof, the Use Thereof, Organic Semiconductive Material and Electronic or Optoelectronic Component
    Publication number: 20120146012
    Abstract: The present invention relates to heterocyclic radicals or diradicals, the dimers, oligomers, polymers, dispiro compounds and polycycles thereof, to the use thereof, to organic semiconductive materials and to electronic and optoelectronic components.
    Type: Application
    Filed: February 16, 2012
    Publication date: June 14, 2012
    Applicant: NOVALED AG
    Inventors: Michael Limmert, Olaf Zeika, Martin Amman, Horst Hartmann, Ansgar Werner
  • Substituted Benzo-Imidazo-Pyrido-Diazepine Compounds
    Publication number: 20120108574
    Abstract: The present invention relates to substituted benzo-imidazo-pyrido-diazepine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted benzo-imidazo-pyrido-diazepine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.
    Type: Application
    Filed: November 1, 2011
    Publication date: May 3, 2012
    Applicant: ArQule, Inc.
    Inventors: Mark A. Ashwell, Sudharshan Eathiraj, Anton Filikov, Steffi Koerner, Jean-Marc Lapierre, Yanbin Liu, Rocio Palma, David Vensel, Shin Iimura, Akiko Shiina, Kenichi Yoshida, Takanori Yamazaki, Akihisa Matsuda
  • TETRACYCLIC FUSED HETEROCYCLIC COMPOUND AND USE THEREOF AS HCV POLYMERASE INHIBITOR
    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
  • Non steroidal glucocorticoid receptor modulators
    Patent number: 8133885
    Abstract: The present invention relates to compounds having general Formula (I) or a pharmaceutically acceptable salt thereof. The present invention also relates to pharmaceutical compositions comprising said compounds and the use of these derivatives to modulate glucocorticoid receptor activity.
    Type: Grant
    Filed: February 14, 2006
    Date of Patent: March 13, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Ralf Plate, Guido Jenny Rudolf Zaman, Pedro Harold Han Hermkens, Christiaan Gerardus Johannes Maria Jans, Rogier Christian Buijsman, Adrianus Petrus Antonius De Man, Paolo Giovanni Martino Conti, Scott James Lusher, Willem Hendrik Abraham Dokter
  • ANTIBACTERIAL FLUOROQUINOLONE ANALOGS
    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
  • DIMERIC IAP INHIBITORS
    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
  • Histamine H3 inverse agonists and antagonists and methods of use thereof
    Patent number: 8063032
    Abstract: Provided herein are fused imidazolyl compounds, methods of synthesis, and methods of use thereof. The compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as neurological disorders and metabolic disorders. Compounds provided herein inhibit the activity of histamine H3 receptors and modulate the release of various neurotransmitters, such as histamine, acetylcholine, norepinephrine, and dopamine (e.g. at the synapse). Pharmaceutical formulations containing the compounds and their methods of use are also provided herein.
    Type: Grant
    Filed: February 11, 2010
    Date of Patent: November 22, 2011
    Assignee: Sunovion Pharmaceuticals Inc.
    Inventors: Milan Chytil, Qun Kevin Fang, Kerry L. Spear
  • Polycyclic Tetracycline Compounds
    Publication number: 20110269714
    Abstract: The present invention is directed to a compound represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof. The variables for Structural Formula (I) are defined herein. Also described is a pharmaceutical composition comprising the compound of Structural Formula (I) and its therapeutic use.
    Type: Application
    Filed: March 30, 2011
    Publication date: November 3, 2011
    Applicant: Tetraphase Pharmaceuticals, Inc.
    Inventors: Xiao-Yi Xiao, Roger Clark, Diana Hunt, Magnus Rönn, Louis Plamondon, Minsheng He, Joyce Sutcliffe, Trudy Grossman
  • Thienotriazolodiazepine compound and medicinal use thereof
    Patent number: 8044042
    Abstract: A thienotriazolodiazepine compound of the following formula (I) a pharmaceutical agent containing the compound as an active ingredient, and a production intermediate and a production method of the thienotriazolodiazepine compound. Since this compound has an inhibitory action on costimulatory signal from CD28 on T cell, it is useful for the prophylaxis or suppression of rejection reaction in transplantation of organ or bone marrow and the like, and the prophylaxis or treatment of autoimmune diseases or allergic diseases.
    Type: Grant
    Filed: May 30, 2006
    Date of Patent: October 25, 2011
    Assignee: Mitsubishi Tanabe Pharma Corporation
    Inventors: Kunitomo Adachi, Hidemasa Hikawa, Maiko Hamada, Jun-ichi Endoh, Seigo Ishibuchi, Naoto Fujie, Minoru Tanaka, Kunio Sugahara, Kouichi Oshita, Meguru Murata
  • Substituted Benzo-Pyrido-Triazolo-Diazepine Compounds
    Publication number: 20110245236
    Abstract: The present invention relates to substituted benzo-pyrido-triazolo-diazepine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted benzo-pyrido-triazolo-diazepine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds or pharmaceutical compositions to subjects in need thereof.
    Type: Application
    Filed: March 31, 2011
    Publication date: October 6, 2011
    Applicant: ArQule, Inc.
    Inventors: Syed M. Ali, Mark A. Ashwell, Eugene Kelleher, Steffi Koerner, Jean-Marc Lapierre, Jeffrey S. Link, Yanbin Liu, Magdi Moussa, Rocio Palma, Manish Tandon, David Vensel, Neil Westlund, Hui Wu, Rui-Yang Yang
  • Substituted Benzo-Pyrimido-Tetrazolo-Diazepine Compounds
    Publication number: 20110166127
    Abstract: The present invention relates to substituted benzo-pyrimido-tetrazolo-diazepine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted benzo-pyrimido-tetrazolo-diazepine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.
    Type: Application
    Filed: December 29, 2010
    Publication date: July 7, 2011
    Applicant: ArQule, Inc.
    Inventors: Rui-Yang Yang, Jeffrey S. Link
  • Spirohydantoin tricyclic CGRP receptor antagonists
    Patent number: 7968540
    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: Grant
    Filed: November 14, 2006
    Date of Patent: June 28, 2011
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Ian M. Bell, Craig A. Stump, Cory R. Theberge, Steven N. Gallicchio, C. Blair Zartman
  • Amino-substituted tricyclic derivatives and methods of use
    Patent number: 7951791
    Abstract: Compounds of formula (I) wherein A and B are amine-substituted sidechains, Y1 and Y2 form various tricyclic cores, Xa and Xb are C, CH, or N, as defined herein, and Rx is an optional substituent. Compounds and compositions of formula (I) are contemplated as well as methods for treating conditions or disorders prevented by or ameliorated by ?7 nAChR ligands that encompass compounds of formula (I) and other tricyclic derivatives. Methods of using amino-substituted tricyclic derivatives also are described herein.
    Type: Grant
    Filed: March 12, 2008
    Date of Patent: May 31, 2011
    Assignee: Abbott Laboratories
    Inventors: Michael R. Schrimpf, Kevin B. Sippy, Jianguo Ji, Tao Li, Jennifer M. Frost, Clark A. Briggs, William H. Bunnelle
  • Spirolactam tricyclic CGRP receptor antagonists
    Patent number: 7947677
    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, J, K, 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: Grant
    Filed: November 14, 2006
    Date of Patent: May 24, 2011
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Ian M. Bell, Craig A. Stump, Cory R. Theberge, Steven N. Gallicchio, C. Blair Zartman, Harold G. Selnick
  • 1,4-diaza-bicyclo[3.2.2]nonyl heteroaryl derivatives useful as nicotinic acetylcholine receptor ligands
    Patent number: 7935695
    Abstract: This invention relates to novel 1,4-diaza-bicyclo[3.2.2]nonyl heteroaryl derivatives and their use in the manufacture of pharmaceutical compositions. The compounds of the invention are found to be cholinergic ligands at the nicotinic acetylcholine receptors. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.
    Type: Grant
    Filed: August 14, 2008
    Date of Patent: May 3, 2011
    Assignee: Neurosearch A/S
    Inventors: Dan Peters, Daniel B. Timmermann, Elsebet Ostergaard Nielsen, Gunnar M. Olsen, Tino Dyhring, Jeppe Kejser Christensen
  • FLUORESCENT, HETEROCYCLICALLY FUSED PERYLENES
    Publication number: 20110079733
    Abstract: The reaction of aromatic nitriles with perylenetetracarboximides affords colorants which fluoresce strongly in the long-wave region and are of the formula in which one pair Q1 and Q2 or one pair Q2 and Q3, and optionally from 0 to 3 pairs Q3 and Q4, Q5 and Q6, Q6 and Q7 and/or Q7 and Q8, in each case in pairs, together form a heterocyclic ring the remaining Q1, Q4, Q5 and Q8 which do not form a heterocyclic ring are each hydrogen, and the remaining Q3, Q6 and Q7 which do not form a heterocyclic ring are each independently R5 or R6. R1 to R8 are each H, CN, halogen or optionally mono- or polysubstituted hydrocarbon groups. Establishing a suitable pH achieves a large Stokes shift in these colorants via the ESPT mechanism.
    Type: Application
    Filed: December 12, 2008
    Publication date: April 7, 2011
    Applicant: BASF SE
    Inventors: Heinz Langhals, Simon Kinzel, Andreas Obermeier
  • Histamine H3 Inverse Agonists and Antagonists and Methods of Use Thereof
    Publication number: 20110065694
    Abstract: Provided herein are fused imidazolyl compounds, methods of synthesis, and methods of use thereof. The compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, including, e.g., neurological disorders and metabolic disorders. Compounds provided herein inhibit the activity of histamine H3 receptors and modulate the release of various neurotransmitters, such as, e.g., histamine, acetylcholine, norepinephrine, and dopamine (e.g. at the synapse). Pharmaceutical compositions containing the compounds and their methods of use are also provided herein.
    Type: Application
    Filed: September 9, 2010
    Publication date: March 17, 2011
    Inventors: Milan Chytil, Sharon R. Engel, Qun Kevin Fang
  • Piperazine, [1,4]Diazepane, [1,4]Diazocane, and [1,5]Diazocane fused imidazo ring compounds
    Patent number: 7888349
    Abstract: Piperazine, [1,4]diazepane, [1,4]diazocane, and [1,5]diazocane fused imidazo ring compounds (i.e., imidazoquinolines, tetrahydroimidazoquinolines, imidazonaphthyridines, tetrahydroimidazonaphthyridines, and imidazopyridines), pharmaceutical compositions containing the compounds, intermediates, methods of making, and methods of use of these compounds as immunomodulators, for inducing or inhibiting cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases are disclosed.
    Type: Grant
    Filed: December 22, 2004
    Date of Patent: February 15, 2011
    Assignee: 3M Innovative Properties Company
    Inventors: Tushar A. Kshirsagar, George W. Griesgraber, Azim A. Celebi, Philip D. Heppner
  • Aromatic Heterocyclic Fused Indolobenzadiazepine HCV NS5B Inhibitors
    Publication number: 20110014154
    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 are useful in treating those infected with HCV.
    Type: Application
    Filed: March 24, 2009
    Publication date: January 20, 2011
    Inventors: John A. Bender, Zhong Yang, John F. Kadow
  • SUBSTITUTED DIAZEPINE SULFONAMIDES AS BOMBESIN RECEPTOR SUBTYPE-1 MODULATORS
    Publication number: 20100317645
    Abstract: Certain novel substituted diazepine sulfonamides are ligands of the human bombesin receptor and, in particular, are selective ligands of the human bombesin receptor subtype-3 (BRS-3). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the modulation of BRS-3, such as obesity, and diabetes.
    Type: Application
    Filed: December 7, 2007
    Publication date: December 16, 2010
    Inventors: Robert K. Baker, Linda L. Chang, Marc Chioda, Harry R. Chobanian, Ying-Duo Gao, Yan Guo, Linus S. Lin, Ping Liu, Ravi P. Nargund, Kathleen M. Rupprecht, Shouwu Miao
  • Spirolactam aryl CGRP receptor antagonists
    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
  • Heterocyclic compounds, methods of making them and their use in therapy
    Patent number: 7790709
    Abstract: In part, the present invention is directed to antibacterial compounds of formula (I) wherein A is a bicyclic heteroaryl ring or a tricyclic ring and R2 is an heterocyclic residue; L is a bond, or L is alkyl, alkenyl or cycloalkyl.
    Type: Grant
    Filed: December 5, 2003
    Date of Patent: September 7, 2010
    Assignee: Affinium Pharmaceuticals, Inc.
    Inventors: Judd M. Berman, Peter Sampson, Heinz W. Pauls, Jailall Ramnauth, David Douglas Manning, Matthew D. Surman, Dejian Xie, Helene Y. Decornez
  • Process for preparing quinoline compounds and products obtained therefrom
    Patent number: 7781427
    Abstract: Methods for synthesizing tetrahydroquinoline-containing compounds are provided, along with synthetic intermediates and products associated with such methods.
    Type: Grant
    Filed: November 4, 2005
    Date of Patent: August 24, 2010
    Assignee: Wyeth LLC
    Inventors: Christoph Dehnhardt, Sreenivasulu Megati, Jerry Sun
  • HISTAMINE H3 INVERSE AGONISTS AND ANTAGONISTS AND METHODS OF USE THEREOF
    Publication number: 20100204214
    Abstract: Provided herein are fused imidazolyl compounds, methods of synthesis, and methods of use thereof. The compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as neurological disorders and metabolic disorders. Compounds provided herein inhibit the activity of histamine H3 receptors and modulate the release of various neurotransmitters, such as histamine, acetylcholine, norepinephrine, and dopamine (e.g. at the synapse). Pharmaceutical formulations containing the compounds and their methods of use are also provided herein.
    Type: Application
    Filed: February 11, 2010
    Publication date: August 12, 2010
    Inventors: Milan Chytil, Sharon R. Engel, Qun Kevin Fang, Kerry L. Spear