The Sulfur Is Bonded Directly At The 16- Or 17-position Patents (Class 552/525)
  • Publication number: 20140094619
    Abstract: This invention describes compounds of Structures 1, 2, and 3 and their use as allosteric modulators of the GABA receptor chloride ionophore complex to alleviate stress, anxiety, mood disorders, seizures, depression, treatment of drug and alcohol abuse, memory, premenstrual disorders, and neural system damage.
    Type: Application
    Filed: August 23, 2013
    Publication date: April 3, 2014
    Applicants: US GOV BY THE SEC. OF DEPT. OF HEALTH & HUMAN SERV, RESEARCH TRIANGLE INSTITUTE
    Inventors: Scott P. RUNYON, Michael ROGAWSKI, Edgar COOK, John KEPLER, Hernan NAVARRO, Rafal KAMINSKI, Matthew ORR
  • Publication number: 20110092473
    Abstract: This invention describes compounds of Structures 1, 2, and 3 and their use as allosteric modulators of the GABA receptor chloride ionophore complex to alleviate stress, anxiety, mood disorders, seizures, depression, treatment of drug and alcohol abuse, memory, premenstrual disorders, and neural system damage.
    Type: Application
    Filed: June 16, 2008
    Publication date: April 21, 2011
    Applicants: Research Triangle Institute, US GOV BY THE SEC. OF DEPT. OF HEALTH & HUMAN SERV.
    Inventors: Scott P. Runyon, Michael Rogawski, Edgar Cook, Kevin M. Cook, John Kepler, Hernan Navarro, Rafal Kaminski, Matthew Orr
  • Patent number: 7419972
    Abstract: The invention relates to new 2-substituted estra-1,3,5(10)-trien-17-ones of formula I as well as their pharmaceutically acceptable salts, their methods of manufacture and use as medicaments for prophylaxis and/or therapy of estrogen-dependent diseases that can be influenced by the inhibition of 17?-hydroxy steroid dehydrogenase type 1.
    Type: Grant
    Filed: June 17, 2005
    Date of Patent: September 2, 2008
    Assignee: Schering AG
    Inventors: Alexander Hillisch, Olaf Peters, Christian Gege, Wilko Regenhardt, Andrea Rosinus, Jerzy Adamski, Gabriele Moeller, Walter Elger, Birgitt Schneider, Ulrich Bothe
  • Patent number: 7196074
    Abstract: Methods of using 7?,11?-dimethyl-17?-hydroxyestra-4,14-dien-3-one (III) and 17 esters thereof for various hormonal therapies, oral and parenteral dosage forms comprising these actives, and processes for their preparation.
    Type: Grant
    Filed: October 28, 2002
    Date of Patent: March 27, 2007
    Assignee: The United States of America as represented by the Department of Health and Human Services
    Inventors: Richard P. Blye, Hyun K. Kim, Pemmaraju Narasimha Rao, Carmie Kirk Acosta
  • Patent number: 6756366
    Abstract: Orally Active androgens are derivative of 7&agr;-methyl-19-nortestosterone. The compounds satisfy formula (I) wherein R1 is O, (H,H), (H,OR), NOR, with R being hydrogen, (C1-6)alkyl, or (C1-6)acyl; R2 is selected from the group consisting of (C2-3)alkyl, isopropyl, (C2-3)1-alkenyl, isopropenyl, 1,2-proandienyl, or (C2-3)1-alynyl, each optionally substituted by halogen; or R2 is cyclopropyl, or cyclopropenyl, each optionally substituted by (C1-2)alkyl, or halogen; R3 is hydrogen, (C1-2)alkyl, or ethenyl; R4 is (C1-2)alkyl; R5 is hydrogen, or (C1-15)acyl; and the dotted lines indicate optional bonds.
    Type: Grant
    Filed: September 24, 2001
    Date of Patent: June 29, 2004
    Assignee: Akzo Nobel N.V.
    Inventors: Jaap van der Louw, Dirk Leysen, Roberta Burma Bursi
  • Patent number: 6673783
    Abstract: Novel 17,20-methanofusidic acid derivatives are used in pharmaceutical compositions for the treatment of infections, in particular in topical compositions for the treatment of skin or eye infections.
    Type: Grant
    Filed: March 7, 2002
    Date of Patent: January 6, 2004
    Assignee: Leo Pharmaceutical Products Ltd. A/S
    Inventor: Tore Duvold
  • Patent number: 6593319
    Abstract: Novel 17,20-dihydrofusidic acid derivatives are used in pharmaceutical compositions for the treatment of infections, in particular in topical compositions for the treatment of skin or eye infections.
    Type: Grant
    Filed: August 14, 2001
    Date of Patent: July 15, 2003
    Assignee: Leo Pharmaceutical Products, Ltd. A/S
    Inventors: Tore Duvold, Welf von Daehne
  • Patent number: 6562805
    Abstract: The present invention relates to methods, compounds and compositions for inhibiting effective binding of a chemokine to its cellular receptor. In one form of the invention, a method includes contacting a cellular population with an effective amount of cosalane or an analog thereof. The invention further relates to methods, compounds and compositions for treating inflammatory diseases. In one form, a method includes administering to a patient a therapeutically effective amount of cosalane or an analog thereof.
    Type: Grant
    Filed: January 29, 2001
    Date of Patent: May 13, 2003
    Assignees: Purdue Research Foundation, The United States of America as represented by the Department of Health and Human Services
    Inventors: Mark S. Cushman, O. M. Zack Howard
  • Patent number: 6541465
    Abstract: Novel, orally active androgens are 7&agr;-substituted &Dgr;14-nandrolone derivatives. The compounds satisfy the general formula: wherein R1 is O, (H,H), (H,OR), NOR, with R being hydrogen, (C1-6) alkyl, or (C1-6) acyl; R2 is selected from the group consisting of (C2-4) alkyl, (C2-4) alkenyl, or (C2-4) alkynyl, each optionally substituted by halogen; or R2 is cyclopropyl, or cyclopropenyl, each optionally substituted by (C1-2) alkyl, or halogen; R3 is hydrogen, (C1-2) alkyl, or ethenyl; R4 is (C1-2) alkyl; R5 is hydrogen, or (C1-15) acyl; and the dotted lines indicate optional bonds.
    Type: Grant
    Filed: July 31, 2001
    Date of Patent: April 1, 2003
    Assignee: Akzo Nobel N.V.
    Inventors: Hubert Jan Jozef Loozen, Dirk Leysen, Jaap van der Louw
  • Patent number: 6534490
    Abstract: Described are new, unsaturated 14,15-cyclopropano-androstanes of general formula (I) and their pharmaceutically acceptable salts, a process for their production and pharmaceutical preparations that contain these compounds. The compounds are characterized by hormonal (gestagenic and/or androgenic) activity and may be used for hormone replacement therapy.
    Type: Grant
    Filed: December 21, 2000
    Date of Patent: March 18, 2003
    Assignee: Jenapharm GmbH & Co. KG.
    Inventors: Sven Ring, Sigfrid Schwarz, Walter Elger, Birgitt Schneider, Günter Kaufmann, Lothar Sobek
  • Patent number: 6388109
    Abstract: Described are new 14,15-cyclopropano steroids of the 19-norandrostane series of general formula (I) and their pharmaceutically acceptable salts, a process for their production and pharmaceutical preparations that contain these compounds. The compounds are distinguished by hormonal (gestagenic and/or androgenic) activity.
    Type: Grant
    Filed: December 20, 2000
    Date of Patent: May 14, 2002
    Assignee: Jenapharm GmbH & Co. KG
    Inventors: Sigfrid Schwarz, Gerd Schubert, Sven Ring, Walter Elger, Birgitt Schneider, Günter Kaufmann, Lothar Sobek
  • Patent number: 6313108
    Abstract: Novel, orally active androgens are 7&agr;-substituted &Dgr;14-nandrolone derivatives. The compounds satisfy the general formula: wherein R1 is O, (H,H), (H,OR), NOR, with R being hydrogen, (C1-6) alkyl, or (C1-6) acyl; R2 is selected from the group consisting of (C2-4) alkyl, (C2-4) alkenyl, or (C2-4) alkynyl, each optionally substituted by halogen; or R2 is cyclopropyl, or cyclopropenyl, each optionally substituted by (C1-2) alkyl, or halogen; R3 is hydrogen, (C1-2) alkyl, or ethenyl; R4 is (C1-2) alkyl; R5 is hydrogen, or (C1-15) acyl; and the dotted lines indicate optional bonds.
    Type: Grant
    Filed: July 11, 2000
    Date of Patent: November 6, 2001
    Assignee: Akzo Nobel N.V.
    Inventors: Hubert Jan Jozef Loozen, Dirk Leysen, Jaap van der Louw
  • Patent number: 5916975
    Abstract: A process for enantioselectively epoxidising a prochiral olefin, which process comprises reacting a prochiral olefin with a source of oxygen in the presence of a salen catalyst and a source of an electron donating ligand, characterized in that the donor ligand is isoquinoline N-oxide or a compound having donor ligand activity and having substantially the same solubility characteristics as isoquinoline N-oxide.
    Type: Grant
    Filed: August 5, 1996
    Date of Patent: June 29, 1999
    Assignee: SmithKline Beecham p.l.c.
    Inventors: David Bell, Frances Finney, Robin Patrick Attrill, David Miller, Gillian Turner
  • Patent number: 5892069
    Abstract: The application discloses methods of treating mammalian diseases characterized by abnormal cell mitosis by administering estradiol derivatives including those comprising colchicine or combretastatin A-4 structural motifs of the general formulae found below in a dosage sufficient to inhibit cell mitosis. The application discloses novel compounds used in the methods.
    Type: Grant
    Filed: April 25, 1997
    Date of Patent: April 6, 1999
    Assignee: The Children's Medical Center Corporation
    Inventors: Robert John D'Amato, Moses Judah Folkman
  • Patent number: 5801165
    Abstract: Compounds of formula I ##STR1## where R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, n, and are as defined herein, their use as antiinflammatory, immunosuppressive, and antiallergic agents, pharmaceutical compositions comprising them, and methods for their preparation comprising irradiating compounds of formula II ##STR2## under an inert atmosphere, in the presence or absence of a compound of formula R.sub.3 --S--S(O).sub.m --R.sub.8, where R.sub.7, R.sub.8, and m are as defined herein, and methods for their preparation comprising oxidizing, reducing, halogenating, or alkylating compounds of formula I are disclosed.
    Type: Grant
    Filed: June 2, 1995
    Date of Patent: September 1, 1998
    Assignee: Rhone-Poulenc Rorer Limited
    Inventors: Michael John Ashton, Sven Jan-Anders Karlsson, Bernard Yvon Jack Vacher, Michael Thomas Withnall
  • Patent number: 5439899
    Abstract: Novel compounds having anti-HIV activity are disclosed along with formulations and methods for treating human immunodeficiency viral infections employing these compounds.
    Type: Grant
    Filed: March 10, 1993
    Date of Patent: August 8, 1995
    Assignees: Purdue Research Foundation, The United States of America as represented by the Department of Health and Human Services
    Inventors: Mark Cushman, Rudiger D. Haugwitz, Wieslaw M. Golebiewski