The Sulfur Is Bonded Directly At The 16- Or 17-position Patents (Class 552/525)
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Publication number: 20140094619Abstract: 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: ApplicationFiled: August 23, 2013Publication date: April 3, 2014Applicants: US GOV BY THE SEC. OF DEPT. OF HEALTH & HUMAN SERV, RESEARCH TRIANGLE INSTITUTEInventors: Scott P. RUNYON, Michael ROGAWSKI, Edgar COOK, John KEPLER, Hernan NAVARRO, Rafal KAMINSKI, Matthew ORR
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Publication number: 20110092473Abstract: 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: ApplicationFiled: June 16, 2008Publication date: April 21, 2011Applicants: 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
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Patent number: 7419972Abstract: 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: GrantFiled: June 17, 2005Date of Patent: September 2, 2008Assignee: Schering AGInventors: Alexander Hillisch, Olaf Peters, Christian Gege, Wilko Regenhardt, Andrea Rosinus, Jerzy Adamski, Gabriele Moeller, Walter Elger, Birgitt Schneider, Ulrich Bothe
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Patent number: 7196074Abstract: 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: GrantFiled: October 28, 2002Date of Patent: March 27, 2007Assignee: The United States of America as represented by the Department of Health and Human ServicesInventors: Richard P. Blye, Hyun K. Kim, Pemmaraju Narasimha Rao, Carmie Kirk Acosta
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Patent number: 6756366Abstract: 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: GrantFiled: September 24, 2001Date of Patent: June 29, 2004Assignee: Akzo Nobel N.V.Inventors: Jaap van der Louw, Dirk Leysen, Roberta Burma Bursi
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Patent number: 6673783Abstract: 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: GrantFiled: March 7, 2002Date of Patent: January 6, 2004Assignee: Leo Pharmaceutical Products Ltd. A/SInventor: Tore Duvold
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Patent number: 6593319Abstract: 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: GrantFiled: August 14, 2001Date of Patent: July 15, 2003Assignee: Leo Pharmaceutical Products, Ltd. A/SInventors: Tore Duvold, Welf von Daehne
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Patent number: 6562805Abstract: 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: GrantFiled: January 29, 2001Date of Patent: May 13, 2003Assignees: Purdue Research Foundation, The United States of America as represented by the Department of Health and Human ServicesInventors: Mark S. Cushman, O. M. Zack Howard
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Patent number: 6541465Abstract: 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: GrantFiled: July 31, 2001Date of Patent: April 1, 2003Assignee: Akzo Nobel N.V.Inventors: Hubert Jan Jozef Loozen, Dirk Leysen, Jaap van der Louw
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Patent number: 6534490Abstract: 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: GrantFiled: December 21, 2000Date of Patent: March 18, 2003Assignee: Jenapharm GmbH & Co. KG.Inventors: Sven Ring, Sigfrid Schwarz, Walter Elger, Birgitt Schneider, Günter Kaufmann, Lothar Sobek
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Patent number: 6388109Abstract: 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: GrantFiled: December 20, 2000Date of Patent: May 14, 2002Assignee: Jenapharm GmbH & Co. KGInventors: Sigfrid Schwarz, Gerd Schubert, Sven Ring, Walter Elger, Birgitt Schneider, Günter Kaufmann, Lothar Sobek
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Patent number: 6313108Abstract: 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: GrantFiled: July 11, 2000Date of Patent: November 6, 2001Assignee: Akzo Nobel N.V.Inventors: Hubert Jan Jozef Loozen, Dirk Leysen, Jaap van der Louw
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Patent number: 5916975Abstract: 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: GrantFiled: August 5, 1996Date of Patent: June 29, 1999Assignee: SmithKline Beecham p.l.c.Inventors: David Bell, Frances Finney, Robin Patrick Attrill, David Miller, Gillian Turner
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Patent number: 5892069Abstract: 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: GrantFiled: April 25, 1997Date of Patent: April 6, 1999Assignee: The Children's Medical Center CorporationInventors: Robert John D'Amato, Moses Judah Folkman
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Patent number: 5801165Abstract: 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: GrantFiled: June 2, 1995Date of Patent: September 1, 1998Assignee: Rhone-Poulenc Rorer LimitedInventors: Michael John Ashton, Sven Jan-Anders Karlsson, Bernard Yvon Jack Vacher, Michael Thomas Withnall
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Patent number: 5439899Abstract: Novel compounds having anti-HIV activity are disclosed along with formulations and methods for treating human immunodeficiency viral infections employing these compounds.Type: GrantFiled: March 10, 1993Date of Patent: August 8, 1995Assignees: Purdue Research Foundation, The United States of America as represented by the Department of Health and Human ServicesInventors: Mark Cushman, Rudiger D. Haugwitz, Wieslaw M. Golebiewski