Hydroxy, Bonded Directly To Carbon, Or Ether In A Substituent E (h Of -oh May Be Replaced By A Substituted Or Unsubstituted Ammonium Ion Or A Group Ia Or Iia Light Metal) Patents (Class 564/93)
  • Publication number: 20140329860
    Abstract: Methods of treating or suppressing oxidative stress diseases including mitochondrial diseases, impaired energy processing disorders, neurodegenerative diseases and diseases of aging are disclosed, as well as compounds useful in the methods of the invention, such as 2-substituted-p-quinone derivatives as disclosed herein.
    Type: Application
    Filed: March 24, 2014
    Publication date: November 6, 2014
    Applicant: Edison Pharmaceuticals, Inc.
    Inventors: Andrew W. Hinman, Kieron E. Wesson, Orion D. Jankowski, Paul Mollard, William D. Shrader, Christopher R. Cornell
  • Patent number: 8741960
    Abstract: The invention relates to compounds of structural formula (I): or a pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof, wherein Y, L, A, W1, W2, and R?1 are defined herein. These compounds are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.
    Type: Grant
    Filed: January 25, 2007
    Date of Patent: June 3, 2014
    Assignee: Synta Pharmaceuticals Corp.
    Inventors: Shoujun Chen, Lijun Sun, Yu Xie
  • Patent number: 8501992
    Abstract: The present invention provides compound of Formula (I): or a stereoisomer, tautomer, salt or solvate thereof, wherein the variables are defined herein. The compounds of formula (I) are inhibitors of Bcl-2 family antiapoptotic proteins, compositions containing the compounds and methods of treating diseases using the compounds.
    Type: Grant
    Filed: June 8, 2009
    Date of Patent: August 6, 2013
    Assignee: Bristol-Myers Squibb Company
    Inventors: Kyoung S. Kim, Robert M. Borzilleri, Zhen-Wei Cai, Kap-Sun Yeung
  • Publication number: 20120061325
    Abstract: Novel compounds useful as chelators, intermediates for their production and methods for removing trivalent and tetravalent metal ions from solution are presented.
    Type: Application
    Filed: October 21, 2011
    Publication date: March 15, 2012
    Inventors: Robert A. Yokel, Wesley R. Harris, Christopher D. Spilling, Robert Joseph Kuhn, Surendra Dawadi
  • Patent number: 7884103
    Abstract: The invention relates to N-sulfonyl-?-amino-acetic acid derivatives of the general formula (I): including the optical isomers thereof and mixtures of such isomers, wherein Ar1 and Ar2 independently of each other stand for an optionally substituted aryl or heteroaryl group, R1 and R2 stand independently of each other for hydrogen, optionally substituted C1-C5alkyl, optionally substituted C2-C5alkenyl, C-2C5alkynyl or optionally substituted C3C6Cycloalkyl; R3 designates hydrogen, C-3C5alkenyl, C3-C5 alkynyl or optionally substituted C1-C5alkyl; R4 is optionally substituted C1-C5alkyl, optionally substituted C-2C5alkenyl, C-2C5aklynyl or optionally substituted C-3C6 cycloalkyl; R5 and R6 are independently of each other hydrogen or optionally substituted C1-C5alkyl, optionally substituted C2-C5alkenyl, C-2C5alkynyl or optionally substituted C3-C6cycloalkyl; R7 and R8 are independently of each other hydrogen or optionally substituted C1-C5alkyl, optionally substituted C2-C5alkenyl, C2-C5alkynyl or optionally subst
    Type: Grant
    Filed: August 27, 2004
    Date of Patent: February 8, 2011
    Assignee: Syngenta Crop Protection, Inc.
    Inventor: Urs Müller
  • Publication number: 20100240708
    Abstract: Disclosed are compounds, pharmaceutical compositions containing the compounds, methods for using the compounds and processes for making the compounds. More specifically, the disclosure relates to alpha-(N-benzenesulfonamido)cycloalkyl compounds that may inhibit one or both of: (i) the functioning of a ?-secretase enzyme; or (ii) the production of ?-amyloid. Such compounds may be beneficial in the treatment of Alzheimer's disease and other conditions. Representative compounds have the following formula I: wherein: A, R1, and R2 are described herein.
    Type: Application
    Filed: March 17, 2010
    Publication date: September 23, 2010
    Inventors: Dalton King, Zhaoxing Meng, Ivar M. McDonald, Richard E. Olson, John E. Macor
  • Patent number: 7700654
    Abstract: A process for isolating N-butylbenzenesulfonamide (NBBS) from biological material, the chemical synthesis of benzenesulfonamide derivatives, the use of NBBS and benzenesulfonamide derivatives for treating benign prostatic hyperplasia and/or prostate carcinoma, the production of medicaments for the treatment thereof, and the use of NBBS and benzenesulfonamide derivatives as a lead substance in the development of active substances for treating benign prostatic hyperplasia and/or prostate carcinoma are provided.
    Type: Grant
    Filed: January 28, 2006
    Date of Patent: April 20, 2010
    Assignee: LTS Lohmann Therapie-Systeme AG
    Inventors: Hans-Rainer Hoffmann, Rudolf Matusch, Aria Baniahmad
  • Publication number: 20090221711
    Abstract: A compound of Formula (I), or pharmaceutically acceptable salts and/or hydrates or prodrugs thereof, wherein Formula (I) has the structure: is provided, wherein R1-R7 are defined herein. These compounds are useful in medicaments for treating a disease selected from the group consisting of Alzheimer's disease, amyloid angiopathy, cerebral amyloid angiopathy, systemic amyloidosis, hereditary cerebral hemorrhage with amyloidosis of the Dutch type, inclusion body myositis, mild cognitive impairment (MCI) and Down's syndrome, in a subject.
    Type: Application
    Filed: May 12, 2009
    Publication date: September 3, 2009
    Applicant: Wyeth
    Inventors: Alexander Michael Porte, Thomas Joseph Caggiano, George Diamantidis, Diane Barbara Hauze, Boyd Lynn Harrison, Molly Hoke, Anthony Kreft, Dennis M. Kubrak, Charles William Mann, Scott Mayer, Koi Michele Morris
  • Patent number: 7365196
    Abstract: A class of compounds is disclosed, comprising sulphonamido-substituted bridged bicycloalkyl structures. The compounds are inhibitors of gamma-secretase, and hence are useful in the treatment of and/or prevention of Alzheimer's disease.
    Type: Grant
    Filed: March 15, 2001
    Date of Patent: April 29, 2008
    Assignees: Merck Sharp & Dohme Ltd., Merck Frosst Canada & Co.
    Inventors: Patrice Charles Belanger, Ian James Collins, Joanne Claire Hannam, Timothy Harrison, Stephen John Lewis, Andrew Madin, Edward Giles McIver, Alan John Nadin, Joseph George Neduvelil, Mark Steven Shearman, Adrian Leonard Smith, Timothy Jason Sparey, Graeme Irvine Stevenson, Martin Richard Teall
  • Patent number: 7323596
    Abstract: Compounds of formula (I) and (IA) have antibacterial or antiprotozoal activity: formula (1) formula (2) wherein: Z represents a radical of formula N(OH)CH(?O) or of formula C(?O)NH(OH); R1 represents hydrogen, methyl or trifluoromethyl, or, except when Z is a radical of formula N(OH)CH(?O), a hydroxy or amino group; R2 represents a radical of formula R10—(X)n-(ALK)m- wherein R10 represents hydrogen, or an optionally substituted c1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, cycloalkyl, aryl, or heterocyclyl group, ALK represents a straight or branched divalent C1-C6 alkylene, C2-C6 ?alkenylene, or C2-C6 alkynylene radical, and may be interrupted by one or more non-adjacent NH—, —O— or S— linkages, X represents NH—, —O— or S—, and m and n are independently 0 or 1; R3 represents hydrogen, C1-C6alkyl, or benzyl; and R4 is as defined in the specification.
    Type: Grant
    Filed: December 21, 2001
    Date of Patent: January 29, 2008
    Assignee: De Novo Pharmaceuticals Ltd.
    Inventors: Barry Porter, Paul Gane, Raymond Beckett, Kenneth Keavey, Jac Wijkmans, Lydia Saroglou
  • Patent number: 7169952
    Abstract: A process for the preparation of a sulfonamide of formula (II), comprising reacting at elevated temperature an aniline of formula (I), with a sulfonating agent A of the formula R1—SO2-Z in the presence of a catalytic amount of either: (i) an amide B-1, other than N,N-dimethylformamide, or (ii) a high boiling tertiary amine B-2. Also provided in accordance with the present invention are processes for preparing sulfonamides of formula (II) by reacting an aniline of formula (I) with sulfanating agent A of the formula R1—SO2-Z in the presence of N,N-dimethylformamide, at a temperature in the range of about 120° C. to about 160° C. for about three to about seven hours.
    Type: Grant
    Filed: June 1, 2001
    Date of Patent: January 30, 2007
    Assignee: FMC Corporation
    Inventors: Leland A. Smeltz, Thomas C. Sedergran, Harold C. Jarrow
  • Patent number: 7166622
    Abstract: Compounds of Formula I, wherein R1–R8 are defined herein are provided, together with pharmaceutically acceptable salts, hydrates, metabolites, and/or prodrugs thereof. Uses of these compounds for inhibiting beta amyloid production and for the prevention and treatment of Alzheimer's Disease and Down's syndrome are described.
    Type: Grant
    Filed: June 9, 2003
    Date of Patent: January 23, 2007
    Assignees: Wyeth, ArQule, Inc.
    Inventors: Anthony Frank Kreft, Derek Cecil Cole, Kevin Roger Woller, Joseph Raymond Stock, Kristina Martha Kutterer, Dennis Martin Kubrak, Charles William Mann, William Jay Moore, David Scott Casebier
  • Patent number: 7161031
    Abstract: Compounds useful as antiproliferative agents, including, for example, anticancer agents, are provided according to formula I: wherein: Ar, X, X1, g, R and R3 are as defined herein.
    Type: Grant
    Filed: February 28, 2003
    Date of Patent: January 9, 2007
    Assignees: Temple University - Of The Commonwealth System of Higher Education, Onconova Therapeutics, Inc.
    Inventors: E. Premkumar Reddy, M.V. Ramana Reddy, Stanley C. Bell
  • Patent number: 7038084
    Abstract: Succinoylamino hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
    Type: Grant
    Filed: February 24, 2004
    Date of Patent: May 2, 2006
    Assignee: G.D. Searle & Co.
    Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel Getman, Gary A. DeCrescenzo, John N. Freskos
  • Publication number: 20040110954
    Abstract: Methods of synthesizing phenol-containing compounds are disclosed.
    Type: Application
    Filed: September 29, 2003
    Publication date: June 10, 2004
    Inventors: Michael R. Palovich, Katherine L. Widdowson
  • Patent number: 6743929
    Abstract: Sulfonamide-containing hydroxyethylamine compounds are effecive as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
    Type: Grant
    Filed: September 6, 2000
    Date of Patent: June 1, 2004
    Assignee: G. D. Searle & Co.
    Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel Getman, Gary A. DeCrescenzo, John N. Freskos
  • Patent number: 6583318
    Abstract: A method of synthesizing &agr;-sulfonamido amide, carboxylic acid or hydroxamic acid derivatives comprising providing a set of polymer-bound reactant(s) (sulfonamide, aldehyde or ketone, isocyanide or acid) to react with three sets of the other three reactants to form an array of polymer-bound &agr;-sulfonamido amide-type intermediates and use of such intermediates for the preparation of combinatorial libraries.
    Type: Grant
    Filed: May 15, 2002
    Date of Patent: June 24, 2003
    Assignee: Advanced Syntech, LLC
    Inventors: Eugene Campian, Boliang Lou, Adnan M. M. Mjalli
  • Publication number: 20030096856
    Abstract: Compounds having formula (I) 1
    Type: Application
    Filed: November 21, 2002
    Publication date: May 22, 2003
    Inventors: Qun Li, Hing Sham, Keith W. Woods, Beth A. Steiner, Stephen L. Gwaltney, Kenneth J. Barr, Hovis M. Imade, Saul Rosenberg
  • Patent number: 6429317
    Abstract: The present invention provides novel indane-like compounds which can be useful for treating psychosis and other conditions associated with the modulation of a muscarinic receptor. The invention provides formulations and methods for using the novel compounds.
    Type: Grant
    Filed: September 5, 2000
    Date of Patent: August 6, 2002
    Assignee: Eli Lilly and Company
    Inventors: Sean P. Hollinshead, Michael A. Staszak, John S. Ward, Joseph W. Wilson, Bret E. Huff, Philip F. Hughes, Jose S. Mendoza, Charles H. Mitch
  • Publication number: 20020049352
    Abstract: The present invention relates to a scaleable process for the oxidation of carbon-boron bonds with Oxone®.
    Type: Application
    Filed: June 25, 2001
    Publication date: April 25, 2002
    Inventors: Weiling Cai, David H. Ripin
  • Patent number: 6221914
    Abstract: The present invention is directed to compounds which are capable of inhibiting the activity of tryptase. Such compounds are useful in the treatment or prevention of inflammatory disease, particularly those disease states which are mediated by mast cell activation. Also encompassed by the invention are formulations comprising the noted compounds, processes for preparing such compounds and methods for treating or preventing an inflammatory disease.
    Type: Grant
    Filed: October 27, 1998
    Date of Patent: April 24, 2001
    Assignee: Array Biopharma Inc.
    Inventors: Laurence E. Burgess, James P. Rizzi
  • Patent number: 5965588
    Abstract: Sulfonamide-containing hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
    Type: Grant
    Filed: March 26, 1998
    Date of Patent: October 12, 1999
    Assignee: G.D. Searle & Co.
    Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel Getman, Gary A. DeCrescenzo, John N. Freskos
  • Patent number: 5847210
    Abstract: Disclosed are processes for the production of compounds of formula I ##STR1## comprising reacting the alkylarylsulfonyl chloride with an N-alkylglucamine. The compounds are useful surfactants.
    Type: Grant
    Filed: September 19, 1997
    Date of Patent: December 8, 1998
    Assignee: Condea Vista Company
    Inventors: John Lin, Upali Weerasooriya, Paul A. Filler
  • Patent number: 5760064
    Abstract: Sulfonamide-containing hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
    Type: Grant
    Filed: June 6, 1997
    Date of Patent: June 2, 1998
    Assignee: G.D. Searle
    Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel Getman, Gary A. DeCrescenzo, John N. Freskos
  • Patent number: 5741794
    Abstract: Compounds of formula (I), wherein: A represents: a) a --VR.sup.6 group wherein v is --C(.dbd.O), --C(.dbd.O)O--, --CH.sub.2 O--, --CH.sub.2 OC(.dbd.O)--, --C(.dbd.S)--, --CH.sub.2 OC(.dbd.O)NH--, --C(.dbd.S)O--, --CH.sub.2 S--, --C(.dbd.O)NHSO.sub.2 --, --SO.sub.2 NHC(.dbd.O)-- or --CH.sub.2 OSiPh.sub.2 --; b) a --CH.sub.2 NR.sup.9 R.sup.10 group or a --CONR.sup.9 R.sup.10 group wherein each of R.sup.9 and R.sup.10 is independently hydrogen, -alkyl-, -alkenyl-, -alkynyl, -cycloalkyl, -cycloalkenyl, pyridyl (any of which may optionally be substituted) or a group --D as defined above or R.sup.9 and R.sup.10 together with the nitrogen atom to which they are attached form a nitrogen-containing heterocyclic ring; c) a group Y where Y is a 5- or 6-membered optionally substituted heterocyclic ring containing one or more heteroatoms selected from nitrogen, oxygen and sulphur; or d) a group --CH.sub.2 Y or --C(.dbd.
    Type: Grant
    Filed: September 1, 1994
    Date of Patent: April 21, 1998
    Assignee: British Biotech Pharmaceuticals Limited
    Inventors: Stephen Arthur Bowles, Christopher David Floyd, Andrew Miller, Mark Whittaker, Lars Michael Wood
  • Patent number: 5731461
    Abstract: Disclosed are surfactant compositions comprising a compound of formula I ##STR1## wherein R is an alkyl group having 6 to 20 carbon atoms, R.sub.1 is a short chain alkyl group and Ar is an aryl group having 6 carbon atoms.
    Type: Grant
    Filed: January 3, 1996
    Date of Patent: March 24, 1998
    Assignee: Condea Vista Company
    Inventors: John Lin, Upali Weerasooriya, Paul A. Filler
  • Patent number: 5665877
    Abstract: The present invention provides a novel synthesis of the compounds of Formula (I): ##STR1## The compounds are produced in high yield and without utilizing expensive chromatographic separations. The synthesis is particularly advantageous because it is stereoselective.
    Type: Grant
    Filed: May 17, 1996
    Date of Patent: September 9, 1997
    Assignee: Eli Lilly and Company
    Inventors: Margaret M. Faul, Michael R. Jirousek, Leonard L. Winneroski, II
  • Patent number: 5639769
    Abstract: Sulfonamide-containing hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
    Type: Grant
    Filed: January 17, 1996
    Date of Patent: June 17, 1997
    Assignee: G.D. Searle and Co.
    Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel Getman, Gary A. DeCrescenzo, John N. Freskos
  • Patent number: 5616797
    Abstract: An electrophotographic toner having polymeric binder and a charge control agent selected from the group consisting of sulfonamides having the general structure: ##STR1## and metal salts thereof. T.sup.1 is independently selected from H, alkyl having from 1 to 20 carbons, cycloalkyl having from 3 to 18 carbons, and aromatic and heteroaromatic ring systems having a solitary ring or 2 to 3 linked or fused rings. R.sup.1 is O, S, N--H, N--R.sup.5, or N--L--R.sup.5 ; where L is a linking group selected from: ##STR2## and R.sup.5 is independently selected from alkyl having from 1 to 20 carbons, cycloalkyl having from 3 to 18 carbons, and aromatic and heteroaromatic ring systems having a solitary ring or 2 to 3 linked or fused rings. L.sup.1 and L.sup.2 are each independently a direct link or divalent alkyl or fluoroalkyl having from 1 to 20 carbons. R.sup.a and R.sup.
    Type: Grant
    Filed: December 9, 1994
    Date of Patent: April 1, 1997
    Assignee: Eastman Kodak Company
    Inventors: John C. Wilson, Peter S. Alexandrovich, Steven M. Bonser
  • Patent number: 5614647
    Abstract: The present invention provides a novel synthesis of the compounds of Formula (I): ##STR1## The compounds are produced in high yield and without utilizing expensive chromatographic separations. The synthesis is particularly advantageous because it is stereoselective.
    Type: Grant
    Filed: May 25, 1995
    Date of Patent: March 25, 1997
    Assignee: Eli Lilly and Company
    Inventors: Margaret M. Faul, Michael R. Jirousek, Leonard L. Winneroski, II
  • Patent number: 5587513
    Abstract: The present invention relates to novel polyether-substituted compounds of imides and their use as surface-active agents.
    Type: Grant
    Filed: January 20, 1995
    Date of Patent: December 24, 1996
    Inventors: Klaus Pohmer, Rainer Weber, Cornelia D orzbach-Lange, Reinhard Haida, Hans-Heinrich Moretto
  • Patent number: 5521219
    Abstract: Sulfonamide-containing hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
    Type: Grant
    Filed: August 24, 1993
    Date of Patent: May 28, 1996
    Assignee: G. D. Searle & Co.
    Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel Getman, Gary A. DeCrescenzo, John N. Freskos
  • Patent number: 5510388
    Abstract: Sulfonamide-containing hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
    Type: Grant
    Filed: May 31, 1995
    Date of Patent: April 23, 1996
    Assignee: G. D. Searle & Co.
    Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel Getman, Gary A. DeCrescenzo, John N. Freskos
  • Patent number: 5457131
    Abstract: The present invention relates to cyclopentane heptanoic or cyclopentane heptenoic acid, 2-hydrocarbyl sulfonamidomethyl, and derivatives thereof, useful as therapeutic agents. In particular, the therapeutic agents of this invention are useful as ocular hypotensives.
    Type: Grant
    Filed: August 18, 1994
    Date of Patent: October 10, 1995
    Assignee: Allergan, Inc.
    Inventor: Steven W. Andrews
  • Patent number: 5414120
    Abstract: The present invention relates to novel polyether-substituted compounds of imides and their use as surface-active agents.
    Type: Grant
    Filed: November 12, 1993
    Date of Patent: May 9, 1995
    Assignee: Bayer AG
    Inventors: Klaus Pohmer, Rainer Weber, Cornelia Dorzbach-Lange, Reinhard Haida, Hans-Heinrich Moretto
  • Patent number: 5407951
    Abstract: The present invention provides sulphonamides of the general formula: ##STR1## wherein R.sup.1 and R.sup.2, which can be the same or different, are hydrogen or halogen atoms or C.sub.1 -C.sub.6 -alkyl, trifluoro-methyl, cyano, carboxyl, alkoxycarbonyl, aminocarbonyl, N-alkylaminocarbonyl or N,N-dialkylaminocarbonyl radicals or, when R.sup.1 and R.sup.2 are alkyl radicals ortho to one another, R.sup.1 and R.sup.2 together with the carbon atoms to which they are attached, form a saturated or unsaturated C.sub.5-C.sub.7 -alkylene ring, R.sup.3 is a hydrogen atom, an alkyl radical containing up to 6 carbon atoms, an acyl radical, a phenylalkyl or phenylalkenyl radical, the phenyl moiety of which can be substituted by halogen, alkyl or trifluoromethyl, C is a --(CH.sub.2).sub.m --radical, in which m is 0, 1, 2 or 3, or a branched C.sub.2 -C.sub.5 -alkylene radical, whereby a methylene radical --CH.sub.
    Type: Grant
    Filed: June 30, 1992
    Date of Patent: April 18, 1995
    Assignee: Boehringer Mannheim GmbH
    Inventors: Ernst-Christian Witte, Karlheinz Stegmeier, Liesel Doerge
  • Patent number: 5387608
    Abstract: The present invention relates to cyclopentane heptanoic or cyclopentane heptenoic acid, 2-hydrocarbyl sulfonamidomethyl, and derivatives thereof, useful as therapeutic agents. In particular, the therapeutic agents of this invention are useful as ocular hypotensives.
    Type: Grant
    Filed: August 17, 1993
    Date of Patent: February 7, 1995
    Assignee: Allergan, Inc.
    Inventor: Steven W. Andrews
  • Patent number: 5322939
    Abstract: A process for preparing an azetidin-2-one derivative represented by formula (2): ##STR1## wherein R.sup.4 and R.sup.5, which may be the same or different, each represents a hydrogen atom, an alkyl group having from 1 to 8 carbon atoms, or an alkyl group having from 1 to 8 carbon atoms substituted with an alkoxy group, an acyl group, or an alkoxycarbonyl group; R.sup.6 represents a protective group for an amino group; and R.sup.7 represents a vinylidene group of formula ##STR2## or an acetylene group of formula ##STR3## wherein R.sup.2 and R.sup.3, which may be the same or different, each represents a hydrogen atom or an alkyl group having from 1 to 8 carbon atoms; and R.sup.8 represents an alkyl group having from 1 to 8 carbon atoms corresponding to R.sup.2 or R.sup.3, which comprises reacting a propargyl alcohol derivative represented by formula (1): ##STR4## wherein R.sup.1 represents an alkyl group having from 1 to 6 carbon atoms, a phenyl group, or a halogen-substituted phenyl group; R.sup.2, R.sup.3, R.
    Type: Grant
    Filed: July 7, 1992
    Date of Patent: June 21, 1994
    Assignee: Takasago International Corporation
    Inventors: Tadakatsu Mandai, Jiro Tsuji
  • Patent number: 5322963
    Abstract: Intermediate compounds (formula [III]and [IV]) useful as starting materials for the synthesis of amino acid derivatives which have renin inhibitory activity and which are useful as remedies for hypertension are prepared stereoselectively in high yield, without requiring complicated process steps. In this method, by reaction of .alpha.-amino aldehyde derivative [I] and compound [II] in the presence of BF.sub.3.OEt.sub.2, as shown in the following reaction formula, .alpha.-amino-.beta.-hydroxy-.delta.-ketone derivative [III] is prepared, and furthermore, by reducing it as required, compound [IV] is obtained: ##STR1## (where R.sup.1 is a protective group on the amino group, R.sup.2 is a lower alkyl group which may be branched, and R.sup.4 is a cyclohexyl group or phenyl group).
    Type: Grant
    Filed: October 5, 1992
    Date of Patent: June 21, 1994
    Assignee: Japan Tobacco, Inc.
    Inventors: Saizo Shibata, Eiji Shirakawa, Yasuki Yamada, Koji Ando, Itsuo Uchida
  • Patent number: 5276184
    Abstract: Adducts containing mesogenic or rodlike moieties are prepared by reacting (1) at least one compound containing an average of more than one vicinal epoxide group per molecule with (2) at least one compound containing an average of more than one reactive hydrogen atom per molecule; with the proviso that at least one member of components (1) and (2) contains a mesogenic or rodlike moiety. These compounds are useful as curing agents for epoxy resins.
    Type: Grant
    Filed: August 3, 1990
    Date of Patent: January 4, 1994
    Assignee: The Dow Chemical Company
    Inventors: Robert E. Hefner, Jr., Jimmy D. Earls
  • Patent number: 5168101
    Abstract: A sulfonamide derivative of the general formula:Tx--R.sup.1 (I)wherein, R.sup.1 represents(i) COOR.sup.11,(ii) CH.sub.2 OR.sup.12 or(iii) CONR.sup.13 R.sup.14,Tx--represents ##STR1## X.sub.b represents(i) bond,(ii) alkylene group of from 1 to 4 carbon atoms or(iii) alkenylene group of from 2 to 4 carbon atoms (with the proviso that --CH.dbd.CHCH.sub.2 -- and --CH.sub.2 CH.dbd.CHCH.sub.2 -- are excluded),R.sup.2b represents(i) hydrogen atom,(ii) halogen atom or(iii) alkyl group of from 1 to 4 carbon atom(s), posses an antagonistic activity on TXA.sub.2.
    Type: Grant
    Filed: October 13, 1988
    Date of Patent: December 1, 1992
    Assignee: Ono Pharmaceutical Co., Ltd.
    Inventors: Yoshinobu Arai, Nobuyuki Hamanaka, Tohru Miyazaki
  • Patent number: 5124462
    Abstract: A process for preparing a compound of Formula (I): ##STR1## wherein R' is optionally protected --CH.sub.2 OH or --COOH; R.sup.2 is phenyl or substituted phenyl; and Y is oxygen, methylene, or substituted methylene, which comprises treating a norbornyl acid amide of formula (II): ##STR2## wherein R is optionally protected --CH.sub.2 OH or --COOR.sup.1 ; R.sup.1 is hydrogen or ester-forming group; and Y is oxygen, methylene, or substituted methylene under the reaction conditions for the Hofmann Rearrangement, and then with a substituted sulfonyl halide of formula (III):R.sup.2 SO.sub.2 X (III)wherein R.sup.2 is phenyl or substituted phenyl; and X is halogen atom.
    Type: Grant
    Filed: June 18, 1991
    Date of Patent: June 23, 1992
    Assignee: Shiongi & Co., Ltd.
    Inventors: Mitsuaki Ohtani, Takaharu Matsuura, Yoshinori Hamada, Shoji Shinomoto
  • Patent number: 5106407
    Abstract: The present invention discloses the antimicrobial utility of certain iodonium ylide compounds. The particular iodonium ylide compounds are phenyl iodonium ylides having an ortho substituent that stabilizes the positive charge on the polyvalent iodine by a nonbonded electrostatic interaction. The polyvalent iodine is further stabilized by a cyclic 1,3-dicarbonyl anion.
    Type: Grant
    Filed: December 4, 1989
    Date of Patent: April 21, 1992
    Assignee: The Dow Chemical Company
    Inventors: Attila G. Relenyi, Gerald F. Koser, Richard W. Walter, Jr., William J. Kruper, Jr., Ravi B. Shankar, Anthony P. Zelinko
  • Patent number: 5098924
    Abstract: Compounds of the formula ##STR1## wherein Z is SO or SO.sub.2 possess renin inhibition activity and are useful in treating hypertension and other diseases where the reduction of the levels of circulating angiotensin II are beneficial.
    Type: Grant
    Filed: September 15, 1989
    Date of Patent: March 24, 1992
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Michael A. Poss
  • Patent number: 5002972
    Abstract: Pharmaceutical compounds and compositions for injectable use in the treatment of thromboxane A.sub.2 mediating diseases, comprising a pharmaceutical carrier and a pharmacologically effective amount of a compound of the formula: ##STR1## wherein R.sup.1 is carboxyl or 5-tetrazolyl; R.sup.2 is hydrogen, methyl, hydroxy, chloro, or bromo; or a pharmaceutically acceptable ester or salt thereof, together with one or more non-toxic pharmaceutically acceptable carriers; and methods for treating thromboxane A.sub.2 mediating diseases.
    Type: Grant
    Filed: February 7, 1990
    Date of Patent: March 26, 1991
    Assignee: Shionogi & Co., Ltd.
    Inventors: Masayuki Narisada, Mitsuaki Ohtani, Fumihiko Watanabe, Takaharu Matsuura
  • Patent number: 4983629
    Abstract: 11-Haloprostane derivatives of general Formula I ##STR1## wherein X is F, Cl or Br,R.sub.1 is the residue CH.sub.2 OH or ##STR2## wherein R.sub.2 means a hydrogen atom, an alkyl, cycloalkyl, aryl, phenacyl or heterocyclic residue,A is a --CH.sub.2 --CH.sub.2 -- or cis--CH.dbd.CH--group,B is a --CH.sub.2 --CH.sub.2 -- or trans--CH.dbd.CH-- or a --C.tbd.C--group,W is an ethylenedioxymethylene group or a hydroxymethylene group,D and E together mean a direct bond orD is a C.sub.1-10 -alkylene group,E is an oxygen or sulfur atom, a direct bond, a --C.tbd.C--bond or a --CR.sub.6 .dbd.CR.sub.7 -group with R.sub.6 and R.sub.7 meaning a hydrogen atom, a chlorine atom or an alkyl group,R.sub.4 is a hydroxy group,R.sub.5 is a hydrogen atom, an alkyl, a cycloalkyl, an aryl or a heterocyclic group, andthe salts thereof with physiologically compatible bases, processes for their preparation, and use thereof as agents inhibiting gastric acid secretion.
    Type: Grant
    Filed: June 21, 1989
    Date of Patent: January 8, 1991
    Assignee: Schering Aktiengesellschaft
    Inventors: Helmut Vorbruggen, Norbert Schwarz, Olaf Loge, Claus-Steffen Sturzebecher, Walter Elger
  • Patent number: 4874894
    Abstract: Process comprises the combination of two steps of interacting a R-benzene, sulfuric acid and phosphorus oxychloride to obtain 4-R-benzenesulfonyl chloride and amidating said sulfonyl chloride to produce 4-R-benzenesulfonamide.
    Type: Grant
    Filed: April 29, 1987
    Date of Patent: October 17, 1989
    Assignee: Hilton Davis Co.
    Inventor: Ramamurthi Kannan
  • Patent number: 4870104
    Abstract: 11-Haloprostane derivatives of general formula I ##STR1## wherein X is F, Cl or Br,R.sub.1 is the residue CH.sub.2 OH or ##STR2## wherein R.sub.2 means a hydrogen atom, an alkyl, cycloalkyl, aryl, phenacyl or heterocyclic residue,A is a --CH.sub.2 --CH.sub.2 -- or cis-CH.dbd.CH-group,B is a --CH.sub.2 --CH.sub.2 -- or trans-CH.dbd.CH-- or a --C.tbd.C-group,W is an ethylenedioxymethylene group or a hydroxymethylene group,D and E together mean a direct bond orD is a C.sub.1-10 -alkylene group,E is an oxygen or sulfur atom, a direct bond, a --C.tbd.C-bond or a --CR.sub.6 .dbd.CR.sub.7 -group with R.sub.6 and R.sub.7 meaning a hydrogen atom, a chlorine atom or an alkyl group,R.sub.4 is a hydroxy group,R.sub.5 is a hydrogen atom, an alkyl, a cycloalkyl, an aryl or a heterocyclic group, andthe salts thereof with physiologically compatible bases, processes for their preparation, and use thereof as agents inhibiting gastric acid secretion.
    Type: Grant
    Filed: November 12, 1986
    Date of Patent: September 26, 1989
    Assignee: Schering Aktiengesellschaft
    Inventors: Helmut Vorbruggen, Norbert Schwarz, Olaf Loge, Claus-Steffen Sturzebecher, Walter Elger
  • Patent number: 4845284
    Abstract: This application discloses new substituted 3-nitrobenzensulfonamides which are useful in enhancing the effect of therapeutic radiation. It also discloses pharmaceutical composition of such compounds, and a method of treatment of patients by administering an effective amount of a substituted 3-nitrobenzenesulfonamide to a patient in need of radiation therapy.
    Type: Grant
    Filed: December 3, 1986
    Date of Patent: July 4, 1989
    Assignee: Merck & Co., Inc.
    Inventors: Edward L. Engelhardt, Walfred S. Saari
  • Patent number: 4826960
    Abstract: The process for the reaction of bicyclic amide acetals with reactive protic compounds of the general Formula ##STR1## wherein Y represents a member selected from the group consisting of ##STR2## R.sup.1 represents a member selected from the group consisting of hydrogen, an alkyl group having from 1 to 10 carbon atoms, an aryl group having from 6 to 12 carbon atoms, and R.sup.2 represents a member selected from the group consisting of an alkyl group having from 1 to 10 carbon atoms, an aryl group having from 6 to 12 carbon atoms, an alkylene ether group having from 1 to 50 carbon atoms, an arylene ether group having from 6 to 50 carbon atoms such as ethyl carbamate to form novel products which are useful as curing agents, blowing agents and monomers is disclosed.
    Type: Grant
    Filed: April 11, 1986
    Date of Patent: May 2, 1989
    Assignee: Ashland Oil, Inc.
    Inventor: Anil B. Goel