Chalcogen Bonded Directly At The 2-position Of The Oxazole Ring Patents (Class 548/221)
  • Patent number: 5580886
    Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: December 3, 1996
    Assignee: Hoechst-Roussel Pharmaceuticals, Inc.
    Inventors: Edward J. Glamkowski, Yulin Chiang
  • Patent number: 5580890
    Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: December 3, 1996
    Assignee: Hoechst-Roussel Pharmaceuticals, Inc.
    Inventors: Edward J. Glamkowski, Yulin Chiang
  • Patent number: 5578624
    Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: November 26, 1996
    Assignee: Hoechst-Roussel Pharmaceuticals, Inc.
    Inventors: Joseph T. Strupczewski, Kenneth J. Bordeau
  • Patent number: 5576443
    Abstract: Disclosed is a novel near-infrared absorbing dye of formula: ##STR1## wherein X.sup.1, X.sup.2 independently represents --CR.sup.8 R.sup.9 --, --S--, --Se--, --NR.sup.10 --, --CH.dbd.CH-- or --O--;n is an integer of 2 or 3;R.sup.1 and R.sup.2 independently represent alkyl of 1 to 10 carbons or substituted alkyl of 1 to 10 carbons;R.sup.3 represents a ring chosen from a set consisting of aryl, substituted aryl, and a heterocyclic ring of a type present in photographic emulsions;R.sup.4, R.sup.5, R.sup.6 and R.sup.7 independently represent hydrogen, alkyl of 1-10 carbons, substituted alkyl of 1-10 carbons, R.sup.4 and R.sup.5 taken together or R.sup.6 and R.sup.7 taken together can represent atoms necessary to form a 5 or 6-membered aliphatic ring, an aromatic six-membered ring, an aromatic 10-membered ring, a substituted aromatic six-member ring or a substituted aromatic 10-member ring;R.sup.8, R.sup.
    Type: Grant
    Filed: March 30, 1995
    Date of Patent: November 19, 1996
    Assignee: Sterling Diagnostic Imaging, Inc.
    Inventors: Dietrich M. Fabricius, Gregory C. Weed
  • Patent number: 5576432
    Abstract: A process of preparing a dihydropyrimidine compound of the structure (I): ##STR1## wherein R.sup.1 and R.sup.2 are bonded together to form an aromatic or heterocyclic ring, which may be substituted or unsubstituted, or are individually selected from the group consisting of hydrogen, or a substituted or unsubstituted aliphatic, carbocyclic, or heterocyclic group;R.sup.3, R.sup.4 and R.sup.5 are individually selected from the group consisting of hydrogen or a substituted or unsubstituted aliphatic, carbocyclic or heterocyclic group; andX represents the atoms necessary to form a 5 or 6 membered heterocyclic ring, and is selected from the group consisting of oxygen, sulfur, selenium, ##STR2## wherein R.sup.6, R.sup.7, and R.sup.8 are individually selected from the group consisting of a substituted or unsubstituted aliphatic, carbocyclic or heterocyclic group; comprising combining a compound (A) of the structure: ##STR3## wherein X, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, and R.sup.
    Type: Grant
    Filed: December 23, 1994
    Date of Patent: November 19, 1996
    Assignee: Eastman Kodak Company
    Inventors: Roger Lok, Antony J. Williams
  • Patent number: 5576343
    Abstract: An anticoagulant agent which comprises, as an active ingredient, an aromatic amidine derivative represented by the following general formula (1) or a salt thereof: ##STR1## wherein the group represented by ##STR2## is a group selected from indolyl, benzofuranyl, benzothienyl, benzimidazolyl, benzoxazolyl, benzothiazolyl, naphthyl, tetrahydronaphthyl and indanyl; X is a single bond, an oxygen atom, a sulfur atom or a carbonyl group; and Y is a saturated or unsaturated 5- or 6-membered heterocyclic moiety or cyclic hydrocarbon moiety optionally having a substituent group, an amino group optionally having a substituent group or an aminoalkyl group optionally having a substituent group.The inventive compound has a high anticoagulant capacity based on its excellent FXa inhibition activity.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: November 19, 1996
    Assignee: Daiichi Pharmaceutical Co., Ltd.
    Inventors: Takayasu Nagahara, Naoaki Kanaya, Kazue Inamura, Yukio Yokoyama
  • Patent number: 5573999
    Abstract: .beta.-Substituted cinnamic acid derivatives of the formula 1, ##STR1## where R.sup.1 is alkyl, chlorine or bromine, --X-- is --O--, --S--, ##STR2## m is 0 or 1, --Y is --OR.sup.4, --O--N.dbd.CR.sup.5 R.sup.6, --NR.sup.7 R.sup.8, --N(OR.sup.9)R.sup.10 or --SR.sup.11, where the above-mentioned substituents R.sup.2 to R.sup.11 are alkyl, and R.sup.2, and R.sup.3 and R.sup.5 to R.sup.11 can also be hydrogen,Z is halogen, nitro, cyano, alkyl, cycloalkyl, aralkyl, aryloxyalkyl, arylthioalkyl, hetarylalkyl, hetaryloxyalkyl, hetarylthioalkyl, alkenyl, aralkenyl, aryloxyalkenyl, arylthioalkenyl, hetarylalkenyl, hetaryloxyalkenyl, hetarylthioalkenyl, alkynyl, arylalkynyl, hetarylalkynyl, aryl, hetaryl, arylazo, acylamino, --OR.sup.12, --SR.sup.13, --SOR.sup.14, --SO.sub.2 R.sup.15, --COOR.sup.16, --CONR.sup.17 R.sup.18, --COR.sup.19, --CR.sup.20 .dbd.NR.sup.21, --N.dbd.CR.sup.22, R.sup.23, --CR.sup.24 .dbd.N--OR.sup.25, --CR.sup.25 R.sup.26 --O--, N.dbd.CR.sup.27 R.sup.28, --CH.sub.2 --OCOR.sup.39 or --NR.sup.37 R.
    Type: Grant
    Filed: May 15, 1995
    Date of Patent: November 12, 1996
    Assignee: BASF Aktiengesellschaft
    Inventors: Hubert Sauter, Herbert Bayer, Klaus Oberdorf, Horst Wingert, Wolfgang von Deyn, Wassilios Grammenos, Hartmann Koenig, Harald Rang, Franz Roehl, Gisela Lorenz, Eberhard Ammermann
  • Patent number: 5574032
    Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents, the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: November 12, 1996
    Assignee: Hoechst-Roussel Pharmaceuticals, Inc.
    Inventors: Joseph T. Strupczewski, Grover C. Helsley, Edward J. Glamkowski, Yulin Chiang, Kenneth J. Bordeau, Peter A. Nemoto, John J. Tegeler
  • Patent number: 5571803
    Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents, the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.
    Type: Grant
    Filed: December 22, 1995
    Date of Patent: November 5, 1996
    Assignee: Hoechst-Roussel Pharmaceuticals, Inc.
    Inventors: Joseph T. Strupczewski, Grover C. Helsley, Edward J. Glamkowski, Yulin Chiang, Kenneth J. Bordeau, Peter A. Nemoto, John J. Tegeler
  • Patent number: 5571828
    Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: November 5, 1996
    Assignee: Hoechst-Roussel Pharmaceuticals, Inc.
    Inventors: Joseph T. Strupczewski, Grover C. Helsley, Edward J. Glamkowski, Yulin Chiang, Kenneth J. Bordeau, Peter A. Nemoto, John J. Tegeler
  • Patent number: 5571814
    Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: November 5, 1996
    Assignee: Hoechst-Roussel Pharmaceuticals, Inc.
    Inventors: Joseph T. Strupczewski, Grover C. Helsley, Edward J. Glamkowski, Yulin Chiang, Kenneth J. Bordeau, Peter A. Nemoto, John J. Tegeler
  • Patent number: 5561128
    Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: October 1, 1996
    Assignee: Hoechst-Roussel Pharmaceuticals, Inc.
    Inventors: Edward J. Glamkowski, Yulin Chiang
  • Patent number: 5559116
    Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: September 24, 1996
    Assignee: Hoechst-Roussel Pharmaceuticals, Inc.
    Inventors: Edward J. Glamkowski, Yulin Chiang
  • Patent number: 5559117
    Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: September 24, 1996
    Assignee: Hoechst-Roussel Pharmaceuticals, Inc.
    Inventors: Joseph T. Strupczewski, Edward J. Glamkowski
  • Patent number: 5550130
    Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: August 27, 1996
    Assignee: Hoechst-Roussel Pharmaceuticals, Inc.
    Inventors: Edward J. Glamkowski, Yulin Chiang
  • Patent number: 5534511
    Abstract: The invention relates to a compound selected from those of formula (I): ##STR1## in which R.sub.1, R.sub.2, R.sub.3, X and n are as defined in the description, the optical isomers thereof, and the addition salts thereof with a pharmaceutically acceptable acid or base and medicinal product containing the same, useful for treating a mammal afflicted with a pathology associated with the sigma receptors.
    Type: Grant
    Filed: March 21, 1995
    Date of Patent: July 9, 1996
    Assignee: Adir et Compagnie
    Inventors: Ange Mouithys-Mickalad, Patrick Depreux, Daniel Lesieur, Gerard Adam, Daniel-Henri Caignard, Pierre Renard, Marie-Claire Rettori
  • Patent number: 5534634
    Abstract: Process for preparing trifluoroethyl sulfur compounds from thiolates and 1-chloro-2,2,2-trifluoroethane. The invention relates to the preparation of trifluoroethyl sulfur compounds of the formula RSCH.sub.2 CF.sub.3 by reacting 1-chloro-2,2,2-trifluoroethane CH.sub.2 Cl--CF.sub.3 in a polar aprotic solvent with salts of thiols of the formula RSH, where R can be an alkyl or aryl radical or a heterocyclic radical.
    Type: Grant
    Filed: September 29, 1994
    Date of Patent: July 9, 1996
    Assignee: Hoechst AG
    Inventors: Wolfgang Appel, Frank Ebmeyer, Tobias Metzenthin, Gunter Siegemund
  • Patent number: 5529998
    Abstract: The invention relates to benzoxazolyl- and benzothiazolyloxazolidinones, processes for their preparation and their use as medicaments, in particular as antibacterial medicaments.
    Type: Grant
    Filed: July 27, 1995
    Date of Patent: June 25, 1996
    Assignee: Bayer Aktiengesellschaft
    Inventors: Dieter Habich, Bernd Riedl, Martin Ruppelt, Andreas Stolle, Hanno Wild, Rainer Endermann, Klaus D. Bremm, Hein-Peter Kroll, Harald Labischinski, Klaus Schaller, Hans-Otto Werling
  • Patent number: 5523312
    Abstract: Disclosed herein are compounds and pharmaceutical compositions useful for combating picornaviruses and preventing or treating picornaviral infections. The compounds have the formula: ##STR1## wherein Het.sub.1 is chosen from the group consisting of oxazolyl, isoxazolyl, oxadiazolyl;Y is an alkylene bridge of 3 to 9 carbon atoms;Het.sub.2 is benzofuranyl or indolyl;R.sub.1 and R.sub.2 are each independently chosen from hydrogen, halo, acetyl, alkyl, alkenyl, amino, alkylthio, hydroxy, hydroxyalkyl, alkoxyalkyl, alkylthioalkyl, alkylsulfinyl alkyl, alkylsulfonylalkyl, alkoxy, nitro, carboxy, alkoxycarbonyl, dialkylaminoalkyl, alkylaminoalkyl, aminoalkyl, difluoromethyl, trifluromethyl, or cyano; andR.sub.3 is oxazolyl, oxadiazolyl, isoxazolyl or any of these substituted with alkyl, halo, alkoxyalkyl, cycloalkyl, haloalkyl, hydroxyalkyl, alkoxy, hydroxy, furyl, thienyl, or fluoroalkyl;the N-oxide thereof or a pharmaceutically acceptable acid addition salt thereof.
    Type: Grant
    Filed: September 27, 1994
    Date of Patent: June 4, 1996
    Assignee: Sterling Winthrop Inc.
    Inventors: David J. Aldous, Thomas R. Bailey, Guy D. Diana, Gee-Hong Kuo, Theodore J. Nitz, Michael Reuman
  • Patent number: 5492925
    Abstract: There are provided thienyl- and furylpyrrole compounds of formula I ##STR1## and their use for the control of insects and acarina. Further provided are compositions and methods comprising those compounds for the protection of plants from attack by insects and acarina.
    Type: Grant
    Filed: August 31, 1993
    Date of Patent: February 20, 1996
    Assignee: American Cyanamid Company
    Inventors: Roger W. Addor, Joseph A. Furch, III, Laurelee A. Duncan, Jack K. Siddens, deceased
  • Patent number: 5491156
    Type: Grant
    Filed: February 16, 1994
    Date of Patent: February 13, 1996
    Assignee: Zeneca Limited
    Inventors: Ian T. Streeting, deceased, Paul A. Worthington
  • Patent number: 5472961
    Abstract: Novel acetamides of the formula I ##STR1## in which Q, R, X and Y have the meanings defined herein, have analgesic and neuroprotective properties and bind with high affinity to kappa receptors.
    Type: Grant
    Filed: March 2, 1995
    Date of Patent: December 5, 1995
    Assignee: Merck Patent Gesellschaft mit beschrankter Haftung
    Inventors: Rudolf Gottschlich, Karl-August Ackermann, Christoph Seyfried, Andrew Barber, Gerd Bartoszyk, Hartmut Greiner
  • Patent number: 5462953
    Abstract: The invention concerns a bicyclic heterocyclic derivative of the formula I ##STR1## wherein Q is an optionally substituted 9-membered bicyclic heterocyclic moiety containing 1 or 2 N's and optionally a further N, O or S heteroatom;A.sup.1 is a direct link to X.sup.1 or (1-3C)alkylene;X.sup.1 is oxy, thio, sulphinyl, sulphonyl or imino;Ar is optionally substituted phenylene or pyridylene;R.sup.1 is (1-4C)alkyl, (3-4C)alkenyl or (3-4C)alkynyl; andR.sup.2 and R.sup.3 together form a group of the formula --A.sup.2 --X.sup.2 --A.sup.3 -- which, together with the carbon atom to which A.sup.2 and A.sup.3 are attached, defines a ring having 5 to 7 ring atoms, wherein each of A.sup.2 and A.sup.3 is (1-3C)alkylene and X.sup.2 is oxy, thio, sulphinyl or sulphonyl;or a pharmaceutically-acceptable salt thereof.The compounds of the invention are inhibitors of the enzyme 5-lipoxygenase.
    Type: Grant
    Filed: July 15, 1994
    Date of Patent: October 31, 1995
    Assignees: Imperial Chemical Industries PLC, ICI Pharma
    Inventors: Pierre A. R. Bruneau, Graham C. Crawley, Keith Oldham
  • Patent number: 5461162
    Abstract: A process of synthesizing N-acyl auxiliary compounds is disclosed. A compound of the formula: ##STR1## is reacted with an anhydride in the presence of a lithium salt and an amine base to produce the N-acylated auxiliary.
    Type: Grant
    Filed: July 27, 1994
    Date of Patent: October 24, 1995
    Assignee: Merck & Co., Inc.
    Inventors: Guo-Jie Ho, David J. Mathre
  • Patent number: 5451594
    Abstract: The invention provides compounds of formula (I) having nematicidal, insecticidal, acaricidal and fungicidal properties, compositions comprising them and processes and intermediates for their preparation: ##STR1## wherein: X is oxygen or sulphur;n is 0, 1 or 2;R.sup.1, R.sup.2, R.sup.3, and R.sup.4 are as described in the specification.
    Type: Grant
    Filed: September 10, 1993
    Date of Patent: September 19, 1995
    Assignee: Zeneca Limited
    Inventors: Steven Fitzjohn, Michael P. Robinson, Michael D. Turnbull, Alison M. Smith, Roger Salmon, Robin Taylor
  • Patent number: 5451681
    Abstract: A process for preparing a compound of formula (I) ##STR1## wherein X is oxygen or sulphur, by (a) reacting a substituted ortho-nitro or -nitroso phenol or a substituted ortho-nitro or -nitroso thiophenol with an alkali metal dithionite reducing agent in an alkaline reaction medium in the presence of carbon disulphide, to form a substituted 2-mercaptobenz-oxazole or -thiazole, acidifying the reaction mixture and collecting the 2-mercaptobenz-oxazole or -thiazole; and then (b) reacting the 2-mercaptobenz-oxazole or -thiazole with a compound of formula (IV)CF.sub.2 .dbd.CH--CH.sub.2 --CH.sub.2 --L (IV)wherein L is a good leaving group.
    Type: Grant
    Filed: December 29, 1994
    Date of Patent: September 19, 1995
    Assignee: Zeneca Limited
    Inventors: Harjinder S. Bansal, Peter J. V. Cleare
  • Patent number: 5440042
    Abstract: Disclosed is a novel near-infrared absorbing dye of formula: ##STR1## wherein X.sup.1, X.sup.2 independently represents --CR.sup.8 R.sup.9 --, --S--, --Se--, --NR.sup.10 --, --CH.dbd.CH-- or --O--;n is an integer of 2 or 3;R.sup.1 and R.sup.2 independently represent alkyl of 1 to 10 carbons or substituted alkyl of 1 to 10 carbons;R.sup.3 represents a ring chosen from the set consisting of aryl, substituted aryl, and heterocyclic containing 5 or 6 carbons in the ring;R.sup.4, R.sup.5, R.sup.6 and R.sup.7 independently represent hydrogen, alkyl of 1-10 carbons, substituted alkyl of 1-10 carbons, R.sup.4 and R.sup.5 taken together or R.sup.6 and R.sup.7 taken together may represent the atoms necessary to form a 5 or 6-membered aliphatic ring, an aromatic six-membered ring, an aromatic 10-membered ring, a substituted aromatic six-member ring or a substituted aromatic 10-member ring;R.sup.8, R.sup.
    Type: Grant
    Filed: May 26, 1993
    Date of Patent: August 8, 1995
    Assignee: E. I. Du Pont de Nemours and Company
    Inventors: Dietrich M. Fabricius, Gregory C. Weed
  • Patent number: 5436348
    Abstract: Compounds of general formula (I): ##STR1## where R, X, A, B and p are defined in the description. Medicinal products useful for treating sleep disorders comprising the same.
    Type: Grant
    Filed: April 5, 1994
    Date of Patent: July 25, 1995
    Assignee: Adir et Compagnie
    Inventors: Said Yous, Isabelle Lesieur, Patrick Depreux, Daniel H. Caignard, Beatrice Guardiola, Gerard Adam, Pierre Renard
  • Patent number: 5424455
    Abstract: A heterocyclic compound of the formula, ##STR1## wherein A and B are each hydrogen, halogen, alkyl or alkoxy, R.sup.1 is alkylene having upto 6 carbon atoms, X is direct linkage or divalent group such as --O--, --S--and the like, T and U are each hydrogen or alkyl, l is 0 or 1 to 3, Q is 5-, 6- or 7- membered saturated or unsaturated heterocyclic residue, and Y is hydrogen, halogen, alkyl, alkoxy or ##STR2## and B are taken together with each other to form methylene-dioxy, which is useful for dyeing or printing hydrophobic fiber materials with superior dyeability to give a dyed or printed product of a red color excellent in fastness properties, particularly those such as washing fastness.
    Type: Grant
    Filed: July 28, 1993
    Date of Patent: June 13, 1995
    Assignee: Sumitomo Chemical Co., Ltd.
    Inventors: Jun Yamamoto, Yasuyoshi Ueda, Junichi Sekihachi, Yosuke Yamamoto, Takashi Omura
  • Patent number: 5405969
    Abstract: The invention provides a process for making a thioether compound having the formula:A--S--Rcomprising reacting:(1) Compound I having the formula:A--H (I)where A comprises a carbon atom bonded to H where that carbon is either capable of ionizing to a nucleophilic state or is conjugated to such an atom, with(2) Compound II having the formula:H--SR or RSSR (II)wherein R is selected from the group consisting of:(a) a substituted or-unsubstituted aryl group or alicyclic group, said groups being carbocyclic or heterocyclic, and(b) a thiocarbonyl group,in the presence of a base and an oxidizing agent that is free of reactive halogen and that is capable of oxidizing H--SR to RSSR.
    Type: Grant
    Filed: December 10, 1993
    Date of Patent: April 11, 1995
    Assignee: Eastman Kodak Company
    Inventors: Charles W. Wright, Joan C. Potenza, John E. Leary, Jr., Chang K. Kim
  • Patent number: 5395846
    Abstract: This invention relates to a class of novel amino bi- and tri-carbocyclic alkane compounds having bis-aryl substitution which exhibit squalene synthase inhibition properties. The bi- and tri-carbocyclic alkane ring contains an amino group and the ring is further linked or bridged to two mono- and/or bicyclic rings. Compounds of this invention reduce levels of serum cholesterol in the body without significantly reducing mevalonic metabolite synthesis. This invention relates also to pharmacological compositions and method of treatment for lowering serum cholesterol levels using the compounds of this invention.
    Type: Grant
    Filed: June 25, 1993
    Date of Patent: March 7, 1995
    Assignee: Rhone-Poulenc Rorer Pharmaceuticals Inc.
    Inventors: Robert L. Morris, Kent W. Neuenschwander, Keith S. Learn, Anthony C. Scotese
  • Patent number: 5378839
    Abstract: There are provided 1-(substituted)thioalkylpyrrole compounds of formula I ##STR1## the use thereof for the control of insect, acarid and mollusk pests and methods and compositions for the protection of crops from the ravages of said pests.
    Type: Grant
    Filed: January 26, 1994
    Date of Patent: January 3, 1995
    Assignee: American Cyanamid Company
    Inventors: David G. Kuhn, Venkataraman Kameswaran
  • Patent number: 5364875
    Abstract: Disclosed are imidazoles linked to bicyclic heterocyclic groups, as inhibitors of acyl-CoA:cholesterol acyltransferase (ACAT), processes for their preparation, pharmaceutical compositions, and their use as antihypercholesterolemics and/or antiatherosclerotics.
    Type: Grant
    Filed: May 11, 1992
    Date of Patent: November 15, 1994
    Assignee: The Du Pont Merck Pharmaceutical Company
    Inventor: Richard G. Wilde
  • Patent number: 5338844
    Abstract: A 2-substituted-2-cyclopentenone compound represented by the following formula (I) and an anticancer agent and a bone formation accelerator comprising the same as an effective active ingredient: ##STR1##
    Type: Grant
    Filed: July 16, 1993
    Date of Patent: August 16, 1994
    Assignee: Teijin Limited
    Inventors: Satoshi Sugiura, Toru Minoshima, Atsuo Hazato, Yoshinori Kato
  • Patent number: 5328897
    Abstract: Herbicidal new 2-(2-benzoxazolyloxy)-acetamides of the formula ##STR1## in which R represents hydrogen, halogen, alkyl or halogenoalkyl andAr represents optionally substituted aryl,but with the exception of the compounds N-isopropyl-2-(2-benzoxazolyl-oxy)-acetanilide and N-isopropyl-2-(6-chlorobenzoxazol-2-yl-oxy)-acetanilide.
    Type: Grant
    Filed: October 2, 1992
    Date of Patent: July 12, 1994
    Assignee: Bayer Aktiengesellschaft
    Inventors: Heinz Forster, Klaus Lurssen, Hans-Joachim Santel, Robert R. Schmidt
  • Patent number: 5326775
    Abstract: Compounds of general formula (I): ##STR1## where R, X, A, B and p are defined in the description. Medicinal products useful for treating sleep disorders comprising the same.
    Type: Grant
    Filed: April 28, 1993
    Date of Patent: July 5, 1994
    Assignee: Adir et Compagnie
    Inventors: Said Yous, Isabelle Lesieur, Patrick Depreux, Daniel H. Caignard, Beatrice Guardiola, Gerard Adam, Pierre Renard
  • Patent number: 5326876
    Abstract: A process for preparing an alkyl sulfonate derivative comprises causing a nitrogen-containing heterocyclic compound represented by the following formula (1): ##STR1## wherein X represents --O--, --S--, --NR.sup.1 --, --Se--, --Te-- or --CR.sup.2 R.sup.3 --, in which each of R.sup.1, R.sup.2 and R.sup.3 independently represents a hydrogen atom or a lower alkyl group, Y represents a hydrogen atom, a mercapto group, an arylthio group, an aralkyl group, a sulfo group, a halogen atom, an alkyl group, an alkylthio group, an alkylsulfonyloxy group or an arylsulfonyloxy group and each of R.sup.4, R.sup.5, R.sup.6, R.sup.7 and R.sup.8 represents a hydrogen atom, an alkyl group, an aryl group, an alkoxy group which may be substituted with a sulfo group, an aryloxy group, an alkylthio group, a haloalkyl group, a halogen atom, a cyano group, a carboxy group or a sulfo group, otherwise R.sup.4 and R.sup.5, R.sup.6 and R.sup.6, R.sup.6 and R.sup.7 and R.sup.7 and R.sup.
    Type: Grant
    Filed: March 12, 1993
    Date of Patent: July 5, 1994
    Assignee: Fuji Photo Film Co., Ltd.
    Inventor: Ken Kawata
  • Patent number: 5322944
    Abstract: Process for preparing enantiomers of general formula (I): ##STR1## where Z, R.sub.1, R.sub.2, R.sub.3 and n are defined in the description. The compounds obtained according to the invention are useful as medicinal products.
    Type: Grant
    Filed: June 30, 1992
    Date of Patent: June 21, 1994
    Assignee: Adir et Compagnie
    Inventors: Gerald Guillaumet, Claude Fugier, Jean-Claude J. Souvie, Gerard Adam, Pierre Renard, Daniel-Henri Caignard
  • Patent number: 5318946
    Abstract: 2-(Heteroaryloxyphenoxy)alkylsulfonate compounds which are effective for the selective control of grass weed species in the presence of crops are described. Also described are a method for the selective herbicidal use of the compounds and a method for their preparation.
    Type: Grant
    Filed: November 27, 1991
    Date of Patent: June 7, 1994
    Assignee: American Cyanamid Company
    Inventors: Michael E. Condon, Michael A. Guaciaro
  • Patent number: 5308850
    Abstract: Compounds having the formula I: ##STR1## are inhibitors of leukotriene biosynthesis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating diarrhea, hypertension, angina, platelet aggregation, cerebral spasm, premature labor, spontaneous abortion, dysmenorrhea, and migraine.
    Type: Grant
    Filed: September 25, 1992
    Date of Patent: May 3, 1994
    Assignee: Merck Frosst Canada, Inc.
    Inventors: John W. Gillard, John H. Hutchinson, Richard Frenette, Michel Therien
  • Patent number: 5288749
    Abstract: The present invention provides tertiary and secondary amine compounds of the formula ##STR1## and the pharmaceutically acceptable salts thereof which are antagonists for alpha-2 adrenoreceptors and which inhibit serotonin (5-hydroxytryptamine, 5-HT) uptake.
    Type: Grant
    Filed: December 20, 1991
    Date of Patent: February 22, 1994
    Assignee: Abbott Laboratories
    Inventors: Michael D. Meyer, John F. DeBernardis, Rajnandan Prasad, Kevin B. Sippy, Karin R. Tietje
  • Patent number: 5286881
    Abstract: A benzodifuranone compounds of the formula, ##STR1## wherein R.sup.1 and R.sup.2 are each independently a naphthyl group or an unsubstituted or substituted phenyl group, which is useful for dyeing or printing hydrophobic fiber materials, is prepared in high purity and high yield by allowing benzofuran compounds of the formula, ##STR2## wherein R.sup.1 is as defined above, to react with acetonitrile compounds of the formula, ##STR3## wherein R.sup.2 is as defined above, and then carrying out an oxidation reaction to give the benzodifuranone compound.
    Type: Grant
    Filed: September 30, 1992
    Date of Patent: February 15, 1994
    Assignee: Sumitomo Chemical Company Limited
    Inventors: Junichi Sekihachi, Jun Yamamoto, Yutaka Kayane
  • Patent number: 5273988
    Abstract: Compounds of formula (I): ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are independently hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, alkylcycloalkyl, halogen, haloalkyl, alkoxy, alkenoxy, alkoxyalkyl, haloalkoxy, alkylthio, cyano, nitro, amino, NR.sup.5 R.sup.6, hydroxy, amino, acylamino, --CO.sub.2 R.sup.4, or R.sup.1 and R.sup.3 when taken together form a 5- or 6-membered ring; R.sup.4 and R.sup.6 are hydrogen or C.sub.1-4 alkyl; R.sup.5 is C.sub.1-4 alkyl; n is 0 or 1; provided that R.sup.1, R.sup.2 and R.sup.3 are not all hydrogen when n is 0; are useful as nematicides.
    Type: Grant
    Filed: March 18, 1992
    Date of Patent: December 28, 1993
    Assignee: Imperial Chemical Industries Plc
    Inventor: Michael D. Turnbull
  • Patent number: 5268381
    Abstract: Compounds of general formula (I): ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, n, X and A are defined in the description. Medicinal products containing the same are useful as antidepressives or anxiolytics due to their 5-HT1A receptor agonist activity.
    Type: Grant
    Filed: September 16, 1992
    Date of Patent: December 7, 1993
    Assignee: Adir et Compagnie
    Inventors: Thierry Taverne, Isabelle Lesieur, Patrick Depreux, Daniel H. Caignard, Beatrice Guardiola, Gerard Adam, Pierre Renard
  • Patent number: 5254559
    Abstract: There are provided 1-(substituted)thioalkylpyrrole compounds of formula I ##STR1## the use thereof for the control of insect, acarid and mollusk pests and methods and compositions for the protection of crops from the ravages of said pests.
    Type: Grant
    Filed: December 4, 1991
    Date of Patent: October 19, 1993
    Assignee: American Cyanamid Company
    Inventors: David G. Kuhn, Venkataraman Kameswaran
  • Patent number: 5254527
    Abstract: Optically active enantiomers of the formula I ##STR1## where R is a group of the formulae ##STR2## R.sub.1 and R.sub.2, among others, are halogen or CF.sub.3 and Z is a carboxyl, carboxylate, carboxylic acid ester, thioester, carbonamide, carboxylic acid anilide, carbohydrazide or thioamide group, are interesting herbicides the effect of which is considerably superior to that of the optically inactive racemates.
    Type: Grant
    Filed: November 7, 1991
    Date of Patent: October 19, 1993
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Hans J. Nestler, Gerhard Horlein, Reinhard Handte, Hermann Bieringer, Friedhelm Schwerdtle, Peter Langeluddeke, Peter Frisch
  • Patent number: 5244596
    Abstract: A mesomorphic compound represented by the following formula [I]: ##STR1## wherein R.sub.1 and R.sub.2 independently denote an alkyl group having 1-16 carbon atoms capable of having a substituent; X.sub.1, X.sub.2, X.sub.3 and X.sub.4 independently denote a single bond ##STR2## A.sub.1, A.sub.2 and A.sub.3 independently denote ##STR3## X.sub.5 and X.sub.6 independently denote hydrogen atom, fluorine, chlorine, bromine, CH.sub.3, CN or CF.sub.3 ; n.sub.1 and n.sub.2 are 0 or 1, with provisos that (1) X.sub.2 cannot be a single bond when n.sub.1 is 0, (2) X.sub.3 cannot be a single bond when N.sub.2 is 1 and (3) at least one of X.sub.2 and X.sub.3 denotes ##STR4## when both n.sub.1 and n.sub.2 is O and A.sub.
    Type: Grant
    Filed: June 17, 1991
    Date of Patent: September 14, 1993
    Assignee: Canon Kabushiki Kaisha
    Inventors: Takao Takiguchi, Takashi Iwaki, Takeshi Togano, Yoko Yamada, Shinichi Nakamura
  • Patent number: 5240919
    Abstract: Compounds of general formula (I): ##STR1## where R, X, A, B and p are defined in the description. Medicinal products useful for treating sleep disorders comprising the same.
    Type: Grant
    Filed: March 9, 1992
    Date of Patent: August 31, 1993
    Assignee: Adir et Compagnie
    Inventors: Said Yous, Isabelle Lesieur, Patrick Depreux, Daniel H. Caignard, Beatrice Guardiola, Gerard Adam, Pierre Renard
  • Patent number: 5232899
    Abstract: A herbicidal substituted benzoxazolinones of the formula ##STR1## in which: R is hydrogen, alkyl, alkoxy, alkenyloxy, alkynyloxy, carboxyalkoxy, alkoxycarbonylalkoxy, alkoxyalkoxy, cyanoalkoxy, haloalkysulphonylamino, alkysulphonylamino, alkoxycarbonyl, haloalkyl, halogen, nitro, carboxy, carboxyalkyl, hydroxy, benzyloxy and cyano;n is 0, 1, 2, or 3;R.sup.1 is hydrogen, nitro, halogen, cyano, haloalkyl, alkyl, alkyoxy, and alkythio;R.sup.2 is hydrogen, halogen, haloalkyl, haloalkyoxy, nitro and cyano; andZ is N or C--R.sub.3, wherein R.sub.3 is hydrogen, halogen, nitro, cyano, alkythio, alkoxy and haloalkyl. Also disclosed is an herbicidal composition and method of treating weeds.
    Type: Grant
    Filed: June 8, 1992
    Date of Patent: August 3, 1993
    Assignee: Imperial Chemical Industries plc
    Inventor: Ferenc M. Pallos
  • Patent number: 5231188
    Abstract: The present invention involves tricyclic-fused 6-member ring oxazolidinones ##STR1## and tricyclic-fused 5-member ring oxazolidinones ##STR2## which are useful as antibacterial agents.
    Type: Grant
    Filed: May 13, 1992
    Date of Patent: July 27, 1993
    Assignee: The Upjohn Company
    Inventor: Steven J. Brickner