Acyclic Chalcogen Bonded Directly To The Hetero Ring Patents (Class 549/395)
  • Publication number: 20150057166
    Abstract: Certain embodiments provide a method for crystallizing a GPCR. The method may employ a fusion protein comprising, from N-terminus to C-terminus: a) a first portion of a family C G-protein coupled receptor (GPCR), wherein the first portion comprises the TM1, TM2 and TM3, regions of the GPCR; b) a stable, folded protein insertion; and c) a second portion of the GPCR, wherein the second portion comprises the TM4, TM5 TM6 and TM7 regions of the GPCR.
    Type: Application
    Filed: October 17, 2014
    Publication date: February 26, 2015
    Inventor: BRIAN KOBILKA
  • Publication number: 20120321714
    Abstract: The present invention relates to a solid pharmaceutical composition including the active principle 6-oxo-6,7,8,9,10,11-hexahydrocyclohepta[c]chromen-3-yl sulfamate. The present invention also relates to polymorphs of the 6-oxo-6,7,8,9,10,11-hexahydrocyclohepta[c]chromen-3-yl sulfamate compound.
    Type: Application
    Filed: March 26, 2012
    Publication date: December 20, 2012
    Applicant: Ipsen Pharma S.A.S.
    Inventors: Nathalie MONDOLY, Bertrand Poirot, Anne Brochard, Joël Richard, Delphine Delahaye, Christian Diolez, Alain Rolland, Francis Diancourt, Gérard Coquerel, Damien Martins, Julie Linol, Marie-Noêlle Petit, Barry Victor Llyod Potter, Lok, Wai Lawrence Woo
  • Patent number: 8039648
    Abstract: Compounds used as dyes comparable to Alexa Fluor 350 dyes. The inventive compounds have high fluorescence quantum yield and high photostability. The dyes facilitate analysis of biological structures with enhanced sensitivity and selectivity.
    Type: Grant
    Filed: June 16, 2009
    Date of Patent: October 18, 2011
    Assignee: Pierce Biotechnology, Inc.
    Inventors: Peter T. Czerney, Surbhi Desai, Matthias S. Wenzel, Boguslawa Dworecki, Frank G. Lehmann, Bernd G. Schweder, Wilhelm G. Frank
  • Publication number: 20110020448
    Abstract: Provided is a pharmaceutical composition for the treatment and prevention of glaucoma, containing (a) a therapeutically effective amount of a compound represented by Formula 1 or a pharmaceutically acceptable salt, prodrug, solvate or isomer thereof, and (b) a pharmaceutically acceptable carrier, diluent or excipient or any combination thereof.
    Type: Application
    Filed: December 18, 2008
    Publication date: January 27, 2011
    Applicants: MAZENCE, INC., KT & G CORPORATION
    Inventors: Myung-Gyu Park, Taehwan Kwak
  • Patent number: 7019024
    Abstract: The invention provides a pharmaceutical for treatment of neurological and neuropsychiatric disorders comprising a compound of the formula: or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: January 9, 2001
    Date of Patent: March 28, 2006
    Assignee: Allelix Neuroscience Inc.
    Inventors: Vassil Iliya Ognyanov, Laurence A. Borden, Stanley Charles Bell, Jing Zhang
  • Publication number: 20030171423
    Abstract: Resistance-repellent and multidrug resistant retroviral protease inhibitors are provided. Pharmaceutical composition comprising such compounds, and methods of using such compounds to treat HIV infections in mammals, are also provided.
    Type: Application
    Filed: January 7, 2003
    Publication date: September 11, 2003
    Inventors: John W. Erickson, Michael Eissenstat, Abelardo Silva, Sergei Gulnik
  • Patent number: 5763625
    Abstract: 3-Substituted-.beta.-lapachone analogs and their use either alone or to augment chemotherapy or radiotherapy to induce programmed neoplastic cell death without exhibiting toxicity to surrounding normal cells are disclosed. In particular, 3-allyl-.beta.-lapachones, 3-alkyl-.beta.-lapachones and 3-halo-.beta.-lapachones were found to be Topoisomerase (Topo I) inhibitors. When these analogs are used alone there is a reversible single-strand break in the DNA of neoplastic cells causing apoptosis and cell death in some cells. However, when these analogs are combined with chemotherapy or X-irradiation, an irreversible Topo I-mediated break is achieved. A new and more efficient chemical synthesis of the compounds is also disclosed.
    Type: Grant
    Filed: April 25, 1995
    Date of Patent: June 9, 1998
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: David A. Boothman, Benjamin J. Frydman, Donald T. Witiak
  • Patent number: 5672621
    Abstract: Carbonarins A, B, C, D, E, F, G, and H have been isolated from the sclerotia of the fungus Aspergillus carbonarius. The carbonarius are effective for controlling Coleopteran and Lepidopteran insects. The carbonarins have the structure: ##STR1## wherein: R.sub.1 is a hydrogen atom or a hydroxy group; R.sub.2 is a hydrogen atom or a methoxy group; R.sub.3 is a hydrogen atom or a naphthopyrone group; and X is an oxygen atom or an NH group.
    Type: Grant
    Filed: February 27, 1996
    Date of Patent: September 30, 1997
    Assignees: The United States of America as represented by the Secretary of Agriculture, University of Iowa Research Foundation and Biotechnology Research and Development Corp.
    Inventors: Ali A. Alfatafta, Patrick F. Dowd, James B. Gloer, Donald T. Wicklow
  • Patent number: 5300646
    Abstract: A novel heterocyclic amine derivative of the general formula: ##STR1## wherein a ring A and a ring B stand independently for an optionally substituted benzene ring, Z.sup.o stands for O or S or ##STR2## stands for --CH.sub.2 --, X stands for O, S or NR.sup.1 wherein R.sup.1 stands for hydrogen atom or an alkyl group, Y stands for NH, O or (CH.sub.2).sub.n wherein n denotes 0 to 2, and R.sup.2 stands for an optionally substituted hydrocarbon group, or their salts.
    Type: Grant
    Filed: December 22, 1992
    Date of Patent: April 5, 1994
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Hideaki Natsugari, Hiroyuki Tawada, Hitoshi Ikeda
  • Patent number: 5189183
    Abstract: Novel aromatic amine derivatives of specific structure are useful intermediates for herbicides. The aromatic amine compounds have the structure shown by formula [I]: ##STR1## wherein Ar and A are as defined herein.
    Type: Grant
    Filed: October 16, 1990
    Date of Patent: February 23, 1993
    Assignee: Mitsui Petrochemical Industries, Ltd.
    Inventors: Daisuke Fukuoka, Katsuya Takahashi, Isao Hashimoto
  • Patent number: 5137911
    Abstract: An isochromane derivative having the general formula I ##STR1## in which each of R.sub.1, R.sub.2, and R.sub.3 is one to four substituents independently selected from hydrogen, hydroxy, alkyl (1-4 C), alkoxy (1-4 C), halogen, or CF.sub.3, or represents a methylenedioxy group;R.sub.4 is selected from hydrogen or alkyl (1-4 C);Alk is an alkylene group with 1-4 carbon atoms;Alk' is an alkylene group with 2-4 carbon atoms, when R.sub.5 is selected from hydrogen or alkyl (1-4 C) and X is O or S; orAlk' is an alkylene group with 1-4 carbon atoms or a bond, when R.sub.5 is an alkyl (1-4 C) group and X is CH.sub.2 or a bond;or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: April 2, 1991
    Date of Patent: August 11, 1992
    Assignee: Akzo N.V.
    Inventors: Michael Combourieu, Jean-Claude Laigle
  • Patent number: 5041565
    Abstract: Novel hydrazinocarbonyloxylabdanes, intermediates and processes for the preparation thereof, and a method for treating cardiac failure utilizing compounds or compositions thereof are disclosed.
    Type: Grant
    Filed: August 30, 1989
    Date of Patent: August 20, 1991
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Raymond W. Kosley, Jr., Gerard J. O'Malley
  • Patent number: 4853410
    Abstract: Racemic and chiral (2R,4R)-4-c-hydroxy-2-4-(substituted)chroman(and thiochroman)-4-acetic acids and their pharmaceutically acceptable salts, their use in the treatment of diabetic complications and intermediates therefor.
    Type: Grant
    Filed: October 9, 1987
    Date of Patent: August 1, 1989
    Assignee: Pfizer Inc.
    Inventor: Christopher A. Lipinski
  • Patent number: 4713453
    Abstract: The present invention relates to a novel oxabicycloheptane derivative of the following formula and a pharmaceutically acceptable salt thereof: ##STR1## where D is a hydrogen atom, a halogen atom, a hydroxyl group, an alkoxy group, an arylalkoxy group, an acyloxy group, a dialkylcarbamoyloxy group or an amidoalkyloxy group; B is a substituted or unsubstituted phenyl, thienyl or furyl group; A is the group ##STR2## (where l is 0 or 1; m and n are each 1 or more, provided that m+n is an interger of 2-8; R.sup.1 is an alkylamino group, a dialkylamino group, an arylalkylamino group, a morpholino group, a thiomorpholino group, a 1-pyrrolidinyl group, a piperidino group, an N-alkylpiperazinyl group, an N-hydroxyalkylpiperazinyl or a pyrrolizidinyl group; and R.sup.2 is a lower alkyl group or a hydroxl group), or the group ##STR3## (where l, m, n, R.sup.1 and R.sup.2 are each the same as defined above), or the group ##STR4## (where R.sup.3 and R.sup.
    Type: Grant
    Filed: February 27, 1987
    Date of Patent: December 15, 1987
    Assignee: Suntori Limited
    Inventors: Toshio Tatsuoka, Kenji Suzuki, Kayoko Imao, Fumio Satoh, Seiji Miyano, Kunihiro Sumoto
  • Patent number: 4598090
    Abstract: The present invention relates to new condensed benzopyrone derivatives, to a process for their preparation and to pharmaceutical compositions containing them.
    Type: Grant
    Filed: March 22, 1984
    Date of Patent: July 1, 1986
    Assignee: Farmitalia Carlo Erba, S.p.A.
    Inventors: Gianfederico Doria, Carlo Passarotti, Ada Buttinoni