Additional Ring Containing Patents (Class 546/342)
  • Patent number: 5599816
    Abstract: Antibacterial compounds having the formula ##STR1## and the pharmaceutically acceptable salts, esters and amides thereof, selected preferred examples of which include those compounds whereinA is.dbd.CR.sup.6 --;R.sup.1 is cycloalkyl of from three to eight carbon atoms or substituted phenyl;R.sup.2 is selected from the group consisting of ##STR2## R.sup.3 is halogen; R.sup.4 is hydrogen, loweralkyl, a pharmaceutically acceptable cation, or a prodrug ester group;R.sup.5 is hydrogen, loweralkyl, halo(loweralkyl), or --NR.sup.13 R.sup.14 ; andR.sup.6 is halogen, loweralkyl, halo(loweralkyl), hydroxy-substituted loweralkyl, loweralkoxy(loweralkyl), loweralkoxy, or amino(loweralkyl),as well as pharmaceutical compositions containing such compounds and the use of the same in the treatment of bacterial infections.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: February 4, 1997
    Assignee: Abbott Laboratories
    Inventors: Daniel T. Chu, Qun Li, Curt S. Cooper, Anthony K. L. Fung, Cheuk M. Lee, Jacob J. Plattner, Zhenkun Ma, Wei-Bo Wang
  • Patent number: 5599951
    Abstract: Amino acid derivatives of formula (Ia) and (Ib) and prodrugs thereof containing a group responsible for chelating the zinc atom of enkephalinase and angiotensin convertase enzymes are disclosed as inhibitors of these enzymes.
    Type: Grant
    Filed: April 14, 1995
    Date of Patent: February 4, 1997
    Assignee: Societe Civile Bioprojet
    Inventors: Jean-Christophe Plaquevent, Denis Danvy, Thierry Monteil, Claude Gros, Jean-Charles Schwartz, Jeanne-Marie LeComte, Helene Greciet, Lucette Duhamel, Pierre Duhamel
  • Patent number: 5597839
    Abstract: Di(aromatic) compounds corresponding to the following formula: ##STR1## in which: Ar represents either ##STR2## X represents a divalent radical, Z represents O, S or a divalent radical,and R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 represent a hydrogen atom or various organic radicals, and the salts of the compounds of formula (I) when R.sub.1 is a carboxylic acid function.Use in human and veterinary medicine and in cosmetics.
    Type: Grant
    Filed: April 28, 1995
    Date of Patent: January 28, 1997
    Assignee: Centre International de Recherches Dermatologiques Galderma (Cird Galderma)
    Inventors: Jean-Michel Bernardon, William R. Pilgrim
  • Patent number: 5595995
    Abstract: Compounds having the general formula: ##STR1## wherein each of R.sup.1 and R.sup.2 independently represents hydrogen or alkyl of 1 to 4 carbon atoms;A represents --O-- or --CR.sup.4 R.sup.5, where R.sup.4 and R.sup.5 are defined as for R.sup.1 or R.sup.2 ;R.sup.3 represents an adamantyl group; andPy represents a 3- or 4-pyridyl group, as free bases or their pharmaceutically acceptable salts are useful in treating androgen-dependent, especially prostatic, cancer.
    Type: Grant
    Filed: January 18, 1995
    Date of Patent: January 21, 1997
    Assignee: British Technology Group Limited
    Inventors: Ferdinand Chan, Michael Jarman, Gerard A. Potter
  • 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: 5557006
    Abstract: Novel 1-alkyl-, 1-alkenyl-, and 1-alkynylaryl-2-amino-1,3-propanediols, intermediates and processes for the preparation thereof, and methods of reducing inflammation and cell proliferation, and relieving memory dysfunction, and inhibiting bacterial and fungal growth fire disclosed.
    Type: Grant
    Filed: April 20, 1995
    Date of Patent: September 17, 1996
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: John J. Tegeler, Barbara S. Rauckman, Russell R. L. Hamer, Brian S. Freed, Gregory H. Merriman
  • Patent number: 5554641
    Abstract: The small nonpeptides of the instant invention are tachykinin antagonists. The compounds are highly selective and functional NK.sub.3 antagonists expected to be useful in the treatment of pain, depression, anxiety, panic, schizophrenia, neuralgia, addiction disorders, inflammatory diseases, gastrointestinal disorders, vascular disorders, and neuropathological disorders.
    Type: Grant
    Filed: March 20, 1995
    Date of Patent: September 10, 1996
    Inventors: David C. Horwell, Martyn C. Pritchard, Jennifer Raphy
  • Patent number: 5534188
    Abstract: An acetylene derivative represented by general formula (I): ##STR1## wherein R.sup.1 is saturated or unsaturated alkyl group having 3-20 carbon atoms, R.sup.2 is saturated or unsaturated alkyl group having 1-20 carbon atoms which may optionally be substituted by halogen atom or alkoxyalkyl group having 2-20 carbon atoms, A and B represent phenylene group or the like or taken as --A--B-- represent naphthalene group or the like, m and s are each 0 or 1, n is integer of 1-6, and * means asymmetric carbon atom; a process for producing said acetylene derivative, a liquid crystal composition using the same as active ingredient, and a liquid crystal element using said composition.
    Type: Grant
    Filed: June 24, 1994
    Date of Patent: July 9, 1996
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Masayoshi Minai, Takayuki Higashii, Shoji Toda, Naoyuki Takano, Kayoko Ueda, Koichi Fujisawa
  • Patent number: 5527827
    Abstract: Compounds having the Formula I:R.sup.1 R.sup.2 C(OR.sup.3)--Ar.sup.1 --X--Ar.sup.2 --C(Ar.sup.3).dbd.CHCO.sub.2 H Iare inhibitors of leukotriene biosynthesis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating angina, cerebral spasm, glomerular nephritis, hepatitis, endotoxemia, uveitis, and allograft rejection and in preventing the formation of atherosclerotic plaques.
    Type: Grant
    Filed: October 27, 1994
    Date of Patent: June 18, 1996
    Assignee: Merck Frosst Canada, Inc.
    Inventors: Daniel Delorme, Yves Ducharme, Richard Friesen, Erich L. Grimm, Carole Lepine
  • Patent number: 5510491
    Abstract: This invention relates to compounds of the formula: ##STR1## wherein R is an electron withdrawing group; R.sub.1 is H or COZ;X.sub.1 and X.sub.2 are independently H, lower alkyl,aryl, aryl lower-alkyl or polystyrene orR and X.sub.1 taken together with the carbon atoms to which they are attached form a ring containing from 4 to 15 ring carbon atoms and may contain up to 2 heteroatoms, wherein the heteroatoms are O, S, or N; andZ is an amino acid residue, a peptide residue or a leaving group. The compounds of the present invention are adaptable as blocking or protecting groups for an amine composition useful in peptide synthesis. The present invention is also directed to a method of protecting an amino group of an organic molecule during a reaction which modifies a portion of the molecule other than the protected amino group.
    Type: Grant
    Filed: March 29, 1993
    Date of Patent: April 23, 1996
    Assignee: Research Corporation Technologies, Inc.
    Inventors: Louis A. Carpino, Michael Philbin
  • Patent number: 5502057
    Abstract: For the treatment of lipoproteinaemia and arteriosclerosis, the new disubstituted pyridines of the formula ##STR1## in which R.sup.1 is optionally substituted aryl or heteroaryl,R.sup.2 is cycloalkyl or optionally substituted alkyl,R.sup.3 is hydrogen, cycloalkyl, or optionally substituted alkyl, aryl or heteroaryl,x is --CH.sub.2 --CH.sub.2 -- or --CH.dbd.CH--,A is ##STR2## R.sup.6 is hydrogen or alkyl, and R.sup.7 is hydrogen, alkyl, aralkyl or a cation.
    Type: Grant
    Filed: July 14, 1993
    Date of Patent: March 26, 1996
    Assignee: Bayer Aktiengesellschaft
    Inventors: Rolf Angerbauer, Peter Fey, Walter Hu/ bsch, Thomas Philipps, Hilmar Bischoff, Dieter Petzinna, Delf Schmidt, Gu/ nter Thomas
  • Patent number: 5502199
    Abstract: Enantiomerically pure sodium 3R,5S-(+)-erythro-(E)-7- 4-(4-fluorophenyl)-2,6-diisopropyl-5-methoxy-meth yl-pyrid-3-yl!-3,5-dihydroxy-hept-6-enoate is prepared by initially cyclizing a corresponding racemic ester to give the racemic lactones and then separating the latter by chromatography on a chiral stationary phase. Cleavage of the enantiomerically pure lactones with the aid of a base yields the enantiomerically pure end products.
    Type: Grant
    Filed: March 17, 1994
    Date of Patent: March 26, 1996
    Assignee: Bayer Aktiengesellschaft
    Inventors: Rolf Angerbauer, Rolf Grosser, Werner Hinsken, Joachim Rehse
  • Patent number: 5498795
    Abstract: Compounds of the formula ##STR1## wherein R.sub.1 -R.sub.3 and R.sub.5 independently are hydrogen, lower alkyl of 1 to 6 carbons, branched chain alkyl or cycloalkyl of 3 to 15 carbons, lower alkyl substituted cycloalkyl of 3 to 15 carbons; R.sub.4 is lower alkyl of 1 to 6 carbons, branched chain alkyl or cycloalkyl of 3 to 15 carbons or lower alkyl substituted cycloalkyl of 3 to 15 carbons; X is S or O; Y is a phenyl group, or heteroaryl selected from a group consisting of pyridyl, thienyl, furyl, pyridazinyl, pyrimidinyl, pyrazinyl, thiazolyl, imidazolyl and oxazolyl, said groups being substituted with the R.sub.5 group defined above; A is (CH.sub.2).sub.n where n is 0-5, lower branched chain alkyl having 3-6 carbons, cycloalkyl having 3-6 carbons, alkenyl having 2-6 carbons and 1 or 2 double bonds, alkynyl having 2-6 carbons and 1 or 2 triple bonds; B is hydrogen, COOH or a pharmaceutically acceptable salt thereof, COOR.sub.8, CONR.sub.9 R.sub.10, --CH.sub.2 OH, CH.sub.2 OR.sub.11, CH.sub.2 OCOR.sub.
    Type: Grant
    Filed: December 29, 1994
    Date of Patent: March 12, 1996
    Assignee: Allergan, Inc.
    Inventors: Tae K. Song, Roshantha A. Chandraratna
  • Patent number: 5496952
    Abstract: The present invention is directed towards new methods of making DE ring intermediates of Formula (III), ##STR1## wherein Y is H or halogen and R is loweralkyl, which in turn are useful in methods of making camptothecin and camptothecin analogs. The present invention also provides new compounds useful in the methods of making compounds of Formula (III).
    Type: Grant
    Filed: February 7, 1995
    Date of Patent: March 5, 1996
    Assignee: North Carolina State University
    Inventor: Daniel L. Comins
  • Patent number: 5470982
    Abstract: For the treatment of lipoproteinaemia and arteriosclerosis, the new disubstituted pyridines of the formula ##STR1## in which R.sup.1 is optionally substituted aryl or heteroaryl,R.sup.2 is cycloalkyl or optionally substituted alkyl,R.sup.3 is hydrogen, cycloalkyl, or optionally substituted alkyl, aryl or heteroaryl,X is --CH.sub.2 --CH.sub.2 -- or --CH.dbd.CH--,A is ##STR2## R.sup.6 is hydrogen or alkyl, and R.sup.7 is hydrogen, alkyl, aralkyl or a cation.
    Type: Grant
    Filed: September 24, 1992
    Date of Patent: November 28, 1995
    Assignee: Bayer Aktiengesellschaft
    Inventors: Rolf Angerbauer, Peter Fey, Walter Hubsch, Thomas Philipps, Hilmar Bischoff, Dieter Petzinna, Delf Schmidt, Gunter Thomas
  • Patent number: 5457118
    Type: Grant
    Filed: April 20, 1994
    Date of Patent: October 10, 1995
    Assignee: Pfizer Inc.
    Inventors: Roger P. Dickinson, Kevin N. Dack, John Steele
  • Patent number: 5449782
    Abstract: A compound represented by formula IAr.sub.1 --O--M--O--AR.sub.2 Iwherein Ar.sub.1 and Ar.sub.2 are independently substituted phenyl or substituted pyridinyl, the substituents on said phenyl or pyridinyl being independently selected from one, two or three of (C.sub.1 -C.sub.10)alkyl, (C.sub.1 -C.sub.10) alkoxy, halogen, carbamyl, (C.sub.1 -C.sub.10) alkoxycarbonyl, oxazoyl, and (C.sub.1 -C.sub.10) alkyl substituted by halogen, (C.sub.1 -C.sub.10) alkoxy, hydroxy, or (C.sub.1 -C.sub.10) alkoxycarbonyl; ##STR1## M is (C.sub.4 -C.sub.8) alkylene, (C.sub.4 -C.sub.8) alkenylene or(C.sub.4 -C.sub.8)-alkynylene;O is oxygen;or pharmaceutically acceptable salts thereof.as well as pharmaceutical compositions containing the compounds and methods of treating or preventing viral infections, especially picornaviral infections, are disclosed.
    Type: Grant
    Filed: August 8, 1994
    Date of Patent: September 12, 1995
    Assignee: Schering Corporation
    Inventors: Viyyoor M. Girijavallabhan, Ashit K. Ganguly, Richard W. Versace
  • Patent number: 5434267
    Abstract: Process for the preparation of compounds of the formula (I) ##STR1## in which R.sup.1, R.sup.2, R.sup.3, X and n have the meaning given in the description, by reacting acetates with carbon monoxide in the presence of a basic auxiliary, followed by alkylation. The products are intermediates for fungicidal acrylates.
    Type: Grant
    Filed: March 14, 1994
    Date of Patent: July 18, 1995
    Assignee: Bayer Aktiengesellschaft
    Inventors: Helmut Kraus, Alexander Klausener, Hans-Joachim Diehr
  • Patent number: 5426109
    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 angina, cerebral spasm, glomerular nephritis, hepatitis, endotoxemia, uveitis, and allograft rejection and in preventing the formation of atherosclerotic plaques.
    Type: Grant
    Filed: August 27, 1992
    Date of Patent: June 20, 1995
    Assignee: Merck Frosst Canada, Inc.
    Inventors: Yves Girard, Pierre Hamel
  • Patent number: 5426111
    Abstract: Compounds of formula ##STR1## Ar is selected from (a) phenyl, (b) phenyl substituted with one or more groups selected from halogen, cyano, alkyl, haloalkyl, alkoxy, and alkoxycarbonyl, (c) furyl, (d) furyl substituted with one or more groups selected from halogen, alkyl, and alkoxy, (e) pyridyl, (f) pyridyl substituted with one or more groups selected from halogen, alkyl, and alkoxy, (g) thienyl, and (h) thienyl substituted with one or more groups selected from halogen, alkyl, and alkoxy; L is selected from alkylene of one to three carbon atoms, alkenylene of two to three carbon atoms, and alkynylene of two to three carbon atoms, and ##STR2## wherein p is an integer of 1 to 4, inclusive, and R.sup.4 is selected from the group consisting of hydrogen, alkyl of one to four carbon atoms, halogen, haloalkyl of one to four carbon atoms, and alkoxy of one to six carbon atoms;R.sup.1 is alkyl; R.sup.2 is hydrogen or alkyl; m is 1 or 2; Z is oxygen or CHOR.sup.
    Type: Grant
    Filed: November 23, 1994
    Date of Patent: June 20, 1995
    Assignee: Abbott Laboratories
    Inventors: Joseph F. Dellaria, James D. Ratajczyk, Clint D. W. Brooks, Anwer Basha
  • Patent number: 5420287
    Abstract: A class of 1,2-diarylcyclopentenyl compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula I: ##STR1## wherein A is selected from ##STR2## wherein each of R.sup.1 and R.sup.2 is independently selected from hydrido, methyl, ethyl, fluoro, hydroxymethyl, carbomethoxy, trifluoromethyl, carboxyl and fluoromethyl; wherein each of R.sup.3, R.sup.4, R.sup.6 through R.sup.9, R.sup.11 and R.sup.12 is independently selected from hydrido, methyl, fluoro and chloro; and wherein each of R.sup.5 and R.sup.10 is independently selected from hydrido, fluoro, chloro, bromo, iodo, methyl, ethyl, methoxy, methylthio, cyano, trifluoromethyl, hydroxymethyl, methoxymethyl, methylsulfonyl and sulfamyl; provided that when A is ##STR3## R.sup.5 cannot be hydrido when R.sup.10 is selected from hydrido, cyano, halo, methyl, trifluoromethyl and methoxy.; further provided that R.sup.10 cannot be hydrido when R.sup.
    Type: Grant
    Filed: June 3, 1994
    Date of Patent: May 30, 1995
    Assignee: G. D. Searle & Co.
    Inventors: David B. Reitz, Jinglin Li
  • Patent number: 5411936
    Abstract: Cyclohexenone oxime ethers of the general formula I ##STR1## where R.sup.1 is C.sub.1 -C.sub.6 -alkyl, A is substituted or unsubstituted C.sub.4 -alkylene or C.sub.4 -alkenylene,x is nitro, cyano, halogen, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy, C.sub.1 -C.sub.4 -alkylthio, C.sub.1 -C.sub.4 -haloalkyl, C.sub.1 -C.sub.4 -haloalkoxy, carboxyl, C.sub.1 -C.sub.4 -alkoxycarbonyl, substituted or unsubstituted benzyloxycarbonyl and/or phenyl,n is from 0 to 3 or from 1 to 5 when X is halogen,R.sup.2 is C.sub.1 -C.sub.6 -alkoxy-C.sub.1 -C.sub.6 -alkyl or C.sub.1 -C.sub.4 -alkylthio-C.sub.1 -C.sub.6 -alkyl, substituted or unsubstituted C.sub.3 -C.sub.7 -cycloalkyl or C.sub.5 -C.sub.
    Type: Grant
    Filed: January 19, 1993
    Date of Patent: May 2, 1995
    Assignee: BASF Aktiengesellschaft
    Inventors: Juergen Kast, Dieter Kolassa, Norbert Meyer, Ulrich Schirmer, Albrecht Harreus, Jochen Wild, Karl-Otto Westphalen, Bruno Wuerzer
  • Patent number: 5401746
    Abstract: Novel compounds for treating hyperproteinaemia, lipoproteinaemia or arteriosclerosis of the formula ##STR1## in which A, B, D and E can have varied meanings,X is --CH.sub.2 --CH.sub.2 or --CH.dbd.CH--, andR is ##STR2## wherein R.sup.21 --denotes hydrogen or alkyl andR.sup.22 --denotes hydrogen,denotes alkyl, aryl or aralkyl, ordenotes a cation,and their oxidation products.
    Type: Grant
    Filed: July 20, 1992
    Date of Patent: March 28, 1995
    Assignee: Bayer Aktiengesellschaft
    Inventors: Rolf Angerbauer, Peter Fey, Walter Hubsch, Thomas Philipps, Hilmar Bischoff, Dieter Petzinna, Delf Schmidt, Gunter Thomas
  • Patent number: 5384070
    Abstract: The use of optically active tetrahydrofuran-2-carboxylic acid esters as dopants in liquid-crystal mixtures, liquid-crystal mixtures containing same and novel optically active tetrahydrofuran-2-carboxylic acid esters.Optically active tetrahydrofuran-2-carboxylic acid esters containing a mesogenic molecular building unit are suitable as dopants in liquid-crystal mixtures. They result in liquid-crystalline ferroelectric phases having short switching times and in electroclinic phases having large electroclinic coefficients. A further advantage is that they induce a helix having a very small pitch so that they are also suitable for helix compensation in LC mixtures.The compounds are symbolized by the general formula: ##STR1## in which the symbols and indices essentially denote: R.sup.1 =alkyl/alkenyl or tetrahydrofurancarbonyloxy or -thio; j, l, n=zero, 1 or 2; k, m=zero or 1; --A.sup.1, --A.sup.2, --A.sup.3 =phenylene, cycloalkylene or corresponding heterocyclates containing nitrogen, oxygen or sulfur; --M.sup.
    Type: Grant
    Filed: May 20, 1993
    Date of Patent: January 24, 1995
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Wolfgang Hemmerling, Hans-Rolf Dubal, Claus Escher, Gerhard Illian, Yoshio Inoguchi, Ingrid Muller, Mikio Murakami, Dieter Ohlendorf, Rainer Wingen
  • Patent number: 5380462
    Abstract: Compounds having the Formula: ##STR1## wherein R.sup.1 denotes an alkenyl group;A.sup.1 and A.sup.2 each independently represent 1,4-phenylene, which is unsubstituted or substituted with halogen and in which, when it is unsubstituted, optionally 1 or 2 CH group(s) is/are replaced by nitrogen, or trans-1,4-cyclohexylene or trans-1,3-dioxane-2,5-diyl;Z.sup.1 and Z.sup.2 each independently signify a single covalent bond, --CH.sub.2 CH.sub.2 --, --COO--, --OOC--, --OCH.sub.2 --, --CH.sub.2 O--, --C.dbd.C--, --(CH.sub.2).sub.4 --, --O(CH.sub.2).sub.3 --, --(CH.sub.2).sub.3 O-- or the trans form of --OCH.sub.2 CH.dbd.CH--, --CH.dbd.CHCH.sub.2 O--, --(CH.sub.2).sub.2 CH.dbd.CH-- or --CH.dbd.CH(CH.sub.2).sub.2 --;n is either 0, 1 or 2; andR.sup.2 is halogen, cyano or alkyl with 1 to 12 carbon atoms, which is optionally substituted with fluorine and in which optionally 1 --CH.sub.2 -- group or 2 non-adjacent --CH.sub.2 -- groups is/are replaced by oxygen, --COO--, --OOC--, --CO-- and/or a --CH.sub.2 --CH.sub.
    Type: Grant
    Filed: October 20, 1993
    Date of Patent: January 10, 1995
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Stephen Kelly, Martin Schadt
  • Patent number: 5371230
    Abstract: Compounds of the formula ##STR1## wherein R.sup.1 signifies a straight-chain alkyl group with 7 to 9 carbon atoms; and R.sup.2 represents a straight-chain alkyl group with 6 to 11 carbon atoms.their manufacture, liquid crystalline mixtures which contain these compounds and their use for electro-optical purposes.
    Type: Grant
    Filed: November 29, 1993
    Date of Patent: December 6, 1994
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Jurg Funfschilling, Stephen Kelly, Alois Villiger
  • Patent number: 5359126
    Abstract: Preparing cyclohexanediones of the formula ##STR1## an aldehyde is reacted with a ketene to give a polymer having the repeating unit ##STR2## wherein n ranges from about 2 to about 1,000. The polymer is hydrolyzed to produce a mixture of an unsaturated acid of the formula R--CH.dbd.C(R.sub.1)--COOH and a hydroxy ester or acid of the formula R--CH(OH)C(R.sub.1)(R.sub.2)--COOR.sub.3, the mixture is then contacted with an esterifying agent to convert the acids to esters. The ester mixture is contacted with a dehydrating agent to convert the hydroxy ester to unsaturated ester of the formula R--CH.dbd.C(R.sub.1)--COOR.sub.3. The unsaturated ester is contacted with a basic catalyst to cyclize it to the cyclic dione ester of the formula ##STR3## and this ester is then hydrolyzed and decarboxylated to give the cyclohexanedione give the productwherein:R is selected, e.g.
    Type: Grant
    Filed: February 7, 1994
    Date of Patent: October 25, 1994
    Assignee: Eastman Chemical Company
    Inventor: Charles A. McCombs
  • Patent number: 5352822
    Abstract: The present invention discloses pesticidally active compounds of formula (II) ##STR1## or a salt thereof, wherein Q is an monocyclic aromatic ring, or fused bicyclic ring system of which at least one ring is aromatic containing 9 or 10 atoms of which one may be nitrogen and the rest carbon each ring system being optionally substituted, or Q is a dihalovinyl group or a group R.sup.6 --C.tbd.C-- where R.sup.6 is C.sub.1-4 alkyl, tri C.sub.1-4 alkylsilyl, halogen or hydrogen; R.sup.2, R.sup.3 , R.sup.4 and R.sup.5 are the same or different with at least one being hydrogen and the others being independently selected from hydrogen, halo, C.sub.1-4 alkyl or C.sub.1-4 haloalkyl; and R.sup.1 is selected from hydrogen and C.sub.1-8 hydrocarbyl optionally substituted by dioxalanyl, halo, cyano, trifluoromethyl, trifluoromethylthio or C.sub.1-6 alkoxy and X.sup.1 is hydrogen, fluoro or chloro.
    Type: Grant
    Filed: April 7, 1993
    Date of Patent: October 4, 1994
    Assignee: Roussel Uclaf
    Inventors: Robert J. Blade, George S. Cockerill, John E. Robinson
  • Patent number: 5342941
    Abstract: Naphthalene derivative of the formula [I]: ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and are hydrogen atom, hydroxy group, cyclo-lower alkyloxy group, substituted or unsubstituted lower alkoxy group, or both combine each other to form lower alkylenedioxy group, R.sup.3 is substituted or unsubstituted nitrogen-containing 6-membered heterocyclic group, and groups of the formulae: --OR.sup.4 and --OR.sup.5 are the same or different and are protected or unprotected hydroxy group, processes for preparing thereof, and synthetic intermediates therefor, these compounds have excellent bronchodilating activity, and are useful in the prophylaxis and treatment of asthma.
    Type: Grant
    Filed: February 19, 1993
    Date of Patent: August 30, 1994
    Assignee: Tanabe Seiyaku Co., Ltd.
    Inventors: Tameo Iwasaki, Kazuhiko Kondo, Katsuo Ikezawa, Hideo Kikkawa, Shinsuke Yamagata
  • Patent number: 5329010
    Abstract: The present invention is a quinone derivative which exhibits excellent therapeutic activity represented by the general formula (I) or a pharmacologically acceptable salt thereof: ##STR1## wherein A stands for a group represented by the formula: ##STR2## (wherein R.sup.3, R.sup.4 and R.sup.5 is the same or different from each other and each stand for a hydrogen atom, a hydroxyl group, a lower alkyl group, a lower alkoxy group, an alkoxyalkyl group, an alkoxyalkoxy group, a cycloalkylalkoxy group, a thiol group or a thioalkyl group, with the proviso that R.sup.3 and R.sup.4 are each a lower alkoxy groupR.sup.1 stands for a heteroarylalkyl group; andB stands for a carboxyl group or a protected carboxyl group.
    Type: Grant
    Filed: February 25, 1992
    Date of Patent: July 12, 1994
    Assignee: Eisai Co., Ltd.
    Inventors: Yasushi Okamoto, Katsuya Tagami, Shigeki Hibi, Hirotoshi Numata, Tetsuya Kawahara, Naoki Kobayashi, Masanobu Shinoda, Koukichi Harada, Kaname Miyamoto, Koichi Abe
  • Patent number: 5324840
    Abstract: Compounds that provide non-teratogenic effects and lack irritation to the skin are shown in the formula below where the partially drawn ring signifies an aromatic ring which may be carbocyclic or heteroaromatic, 6-membered or 5-membered, and may be condensed with another ring. R.sub.1 is lower alkyl, Cl, Br, or I, R.sub.2 is H, lower alkyl, Cl, Br, or I, and R.sub.3 is lower alkyl, Cl, Br, I, or is an ether, thioether, ester, thioester, amine or substituted amine group.
    Type: Grant
    Filed: June 11, 1992
    Date of Patent: June 28, 1994
    Assignee: Allergan, Inc.
    Inventor: Roshantha A. S. Chandraratna
  • Patent number: 5321000
    Abstract: Acids, esters, amides and salts of benzhydryl compounds are antidotes for thiocarbamate and acetamide herbicides. These antidote compounds are especially effective to safen acetamide herbicides used to control grassy weeds and broadleaf weeds in rice, sorghum, corn and wheat.
    Type: Grant
    Filed: June 29, 1992
    Date of Patent: June 14, 1994
    Assignee: Monsanto Company
    Inventors: Lawrence H. Brannigan, Ronald J. Brinker, Robert J. Kaufman, Suzanne Metz
  • Patent number: 5314918
    Abstract: This invention relates to alkanoic acid compounds having phenyl and heteroarylthio substituents which are useful as leukotriene antagonists, processes for the preparation thereof, and pharmaceutical compositions containing such compounds.This invention also relates to methods of treating diseases in which leukotrienes are a factor by administration of an effective amount of the above compounds or compositions.
    Type: Grant
    Filed: April 2, 1992
    Date of Patent: May 24, 1994
    Assignee: SmithKline Beecham Corporation
    Inventors: James S. Frazee, John G. Gleason, Ralph F. Hall
  • Patent number: 5300676
    Abstract: Fluorine-substituted .alpha.-(5-aryloxy-naphthalen-1-yl-oxy)-propionic derivatives of the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5, as defined herein, are useful as herbicides. Processes and intermediates for their preparation are also disclosed.
    Type: Grant
    Filed: April 11, 1991
    Date of Patent: April 5, 1994
    Assignee: Bayer Aktiengesellschaft
    Inventors: Roland Andree, Michael Haug, Klaus Lurssen, Hans-Joachim Santel, Robert R. Schmidt
  • Patent number: 5288750
    Type: Grant
    Filed: January 31, 1991
    Date of Patent: February 22, 1994
    Assignee: Orion-yhtyma Oy
    Inventors: Pentti Pohto, Paivi A. Aho, Reijo J. Backstrom, Erkki J. Honkanen, Inge-Britt Y. Linden, Erkki A. O. Nissinen
  • Patent number: 5274184
    Abstract: The present invention relates to compounds of the general formula I ##STR1## wherein A.sup..sym. and B.sup..sym. independently of one another denote a proton, with the limitation that they do not both simultaneously denote protons, the equivalent part of the barium ion, an ion of the general formula II ##STR2## or an ion of the general formula III ##STR3## and wherein R.sup.1 to R.sup.8, R.sup.11 to R.sup.16, X and m and n are as defined in the description, processes for their preparation and their use as charge control agents in toners and developers and as charge improving agents in powders and varnishes.
    Type: Grant
    Filed: October 2, 1991
    Date of Patent: December 28, 1993
    Assignee: Cassella Aktiengesellschaft
    Inventors: Gert Nagl, Hans-Tobias Macholdt
  • Patent number: 5266579
    Abstract: Pyridines of the formula ##STR1## where R.sup.1 is hydrogen, C.sub.1 -C.sub.6 -alkyl, C.sub.3 -C.sub.6 -alkenyl, C.sub.3 -C.sub.6 -alkynyl or an acyl radical COR.sup.2 ; R.sup.2 is C.sub.1 -C.sub.6 -alkyl, C.sub.3 -C.sub.6 -alkenyl, C.sub.3 -C.sub.6 -alkynyl, C.sub.1 -C.sub.6 -haloalkyl or substituted or unsubstituted aryl; A is one of the groups ##STR2## where R.sup.3 and R.sup.4 are identical or differ and each is C.sub.1 -C.sub.6 -alkyl, with the proviso that R.sup.3 and R.sup.4 are not simultaneously methyl; R.sup.5 is one of the groups (CH.sub.2).sub.n, CH.sub.2 OCH.sub.2, CH.sub.2 S(O).sub.m CH.sub.2, CH.sub.2 CH.sub.2 O or CH.sub.2 CH.sub.2 S(O).sub.m, n denoting 1, 2, 3, 4 or 5, and m being 0, 1 or 2; Ar is aryl which is unsubstituted or bears from one to five substituents selected from the group consisting of C.sub.1 -C.sub.6 -alkyl, phenyl, halogen, C.sub.1 -C.sub.6 -haloalkyl, C.sub.1 -C.sub.6 -alkoxy, C.sub.1 -C.sub.6 -haloalkoxy, C.sub.1 -C.sub.
    Type: Grant
    Filed: February 5, 1992
    Date of Patent: November 30, 1993
    Assignee: BASF Aktiengesellschaft
    Inventors: Bernhard Zipperer, Hubert Sauter, Eberhard Ammermann, Gisela Lorenz
  • Patent number: 5248780
    Abstract: The invention concerns novel, pharmaceutically useful 1,3-dioxane alkenoic acid derivatives of the formula I containing a pyridyl moiety at position 4 of the dioxane ring and in which the groups at positions 2, 4 and 5 have cis-relative stereochemistry, X is hydrogen, alkoxy or hydroxy, Y is vinylene, n is 1 or 2, A.sup.1 is alkylene, R.sup.1 is a variety of substituents defined hereinafter, and R.sup.2 is hydroxy, a physiologically acceptable alcohol residue or alkanesulphonamido, and the pharmaceutically acceptable salts thereof. The invention also includes processes for the manufacture and use of the acid derivatives as well as pharmaceutical compositions for therapeutic use in one or more of a variety of diseases such as ischaemic heart disease, cerebrovascular disease, asthmatic disease and/or inflammatory disease.
    Type: Grant
    Filed: September 25, 1992
    Date of Patent: September 28, 1993
    Assignee: Imperial Chemical Industries, Plc
    Inventors: Andrew G. Brewster, George R. Brown, Alan W. Faull, Reginald Jessup, Michael J. Smithers
  • Patent number: 5229393
    Abstract: Compounds of formula (I): ##STR1## and stereoisomers thereof, wherein V is an oxygen or a sulphur atom; X and Y, which may be the same or different, are hydrogen or halogen atoms, or optionally substituted alkyl, optionally substituted alkenyl, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted alkynyl, haloalkyl, alkoxy, haloalkoxy, optionally substituted aryloxy, optionally substituted arylalkoxy, optionally substituted acyloxy, optionally substituted amino, acylamino, nitro, nitrile, --CO.sub.2 R.sup.3, --CONR.sup.4 R.sup.5, or --COR.sup.6 groups; or the groups X and Y, when they are in adjacent positions on the phenyl ring, may join to form a fused ring, either aromatic or aliphatic, optionally containing one or more heteroatoms; and Z is optionally substituted methylene, optionally substituted amino, oxygen or sulphur and when Z is a substituted methylene group, the substituent may join the 2-position of the phenyl ring to form a non-aromatic fused ring; R.sup.1 and R.
    Type: Grant
    Filed: April 6, 1992
    Date of Patent: July 20, 1993
    Assignee: Imperial Chemical Industries PLC
    Inventors: John M. Clough, Christopher R. A. Godfrey
  • Patent number: 5225607
    Abstract: This invention relates to novel fluorinated ethers, useful as insecticides and acaricides, to processes and intermediates for their preparation, to insecticidal and acaricidal compositions thereof and to methods of combating and controlling insect and acarine pests therewith.
    Type: Grant
    Filed: December 30, 1987
    Date of Patent: July 6, 1993
    Assignee: Imperial Chemical Industries PLC
    Inventors: Michael J. Bushell, Robin A. E. Carr, Alan J. Whittle
  • Patent number: 5212316
    Abstract: Compounds of formula I ##STR1## wherein Ar is an optionally substituted phenyl ring; B is a single bond, a group --(CH.sub.2 OCH.sub.2).sub.n being n=or 2, a a 2,4-disubstituted-1,3-dioxolane ring or a 2,4-disubstituted-1,3-thioxolane ring, R is a single bond, an optionally substituted methylene or ethylene group and T is 2, 3- or 4-pyridyl, an optionally salified or esterified carboxy group or a carboxyamide group. Said compounds are useful in treatment of respiratory diseases.
    Type: Grant
    Filed: July 30, 1990
    Date of Patent: May 18, 1993
    Assignee: Boehringer Mannheim Italia
    Inventors: Silvano Spinelli, Roberto Di Domenico, Ernesto Menta, Bruno Lumachi, Licia Gallico, Sergio Tognella
  • Patent number: 5204018
    Abstract: Compounds of the formula ##STR1## wherein n stands for the number 0 or 1; R.sup.1 denotes a group R.sup.3 or R.sup.3 --A.sup.3 --Z.sup.2 -- and R.sup.2 denotes a group R.sup.4 or R.sup.4 --A.sup.4 --Z.sup.3 --; ring A.sup.1 signifies unsubstituted or halogen-, cyano- and/or methyl-substituted 1,4-phenylene in which optionally 1 CH group or 2 CH groups is/are replaced by nitrogen; A.sup.3, A.sup.4 and ring A.sup.2 each independently represent unsubstituted or halogen-, cyano- and/or methyl-substituted 1,4-phenylene in which optionally 1 CH group or 2 CH groups is/are replaced by nitrogen or trans-1,4-cyclohexylene, trans-1,3-dioxane-2,5-diyl, 1-cyano-trans-1,4-cyclohexylene, bicyclo[2.2.2]octane-1,4-diyl, naphthalene-2,6-diyl, tetralin-2,6-diyl or trans-decalin-2,6-diyl; Z.sup.1, Z.sup.2 and Z.sup.3 each independently signify a single covalent bond, --COO--, --OOC--, --CH.sub.2 O--, --OCH.sub.2 --, --CH.tbd.C--, --(CH.sub.2).sub.3 O--, --O(CH.sub.2).sub.3 --, --(CH.sub.2).sub.4 -- or the trans form of --CH.
    Type: Grant
    Filed: January 22, 1991
    Date of Patent: April 20, 1993
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Stephen Kelly
  • Patent number: 5196538
    Abstract: New ester-containing quaternary pyridinium salts are provided having advantageous utility as charge control agents in electrostatographic toners and developers. The salts have the structure: ##STR1## wherein R.sub.1 is alkyl or aryl, X is --CH.sub.2 --.sub.n, Y is hydrogen, alkyl, alkoxy or halogen, Z.crclbar. is an anion and n is an integer from 1 to 6.Such ester-containing quaternary pyridinium salts also cause toner particles containing them to display lower fusing temperatures and improved paper adhesion indexes.
    Type: Grant
    Filed: July 18, 1991
    Date of Patent: March 23, 1993
    Assignee: Eastman Kodak Company
    Inventors: John W. Wilson, Alexandra D. Bermel
  • Patent number: 5196539
    Abstract: New ester-containing quaternary pyridinium salts are provided having advantageous utility as charge control agents in electrostatographic toners and developers. The salts have the structure: ##STR1## wherein R.sub.1 is alkyl or aryl, X is --CH.sub.2 --.sub.n, Y is hydrogen, alkyl, alkoxy or halogen, Z.sup..crclbar. is an anion and n is an integer from 2 to 6.Such ester-containing quaternary pyridinium salts also cause toner particles containing them to display lower fusing temperature and improved paper adhesion indexes.
    Type: Grant
    Filed: July 18, 1991
    Date of Patent: March 23, 1993
    Assignee: Eastman Kodak Company
    Inventors: John W. Wilson, Alexandra D. Bermel
  • Patent number: 5194441
    Abstract: R.sup.2 is additionally H when X+Y=--O--CH(W.sup.3 R.sup.3)--O--, --O--CH(O--W.sup.4 R.sup.4)--O-- or --O--C(W.sup.3 R.sup.3)(O--W.sup.4 R.sup.4)--O-- and W.sup.2 =direct bond,except cis-1-(2,4-dichlorophenyl)-2-(pryid-3-yl)-1,2-epoxypropane, trans-1-(2,4-dichlorophenyl)-2-(pyrid-3-yl)-1,2-epoxypropane, 1-(2,4- dichlorophenyl)-2-(pryid-3-yl)-1,2-epoxybutane and 2,4-dichloro- .alpha.[1-hydroxy-1-(pyrid-3-yl)-ethyl]-benzyl methanesulfonate,and the N-oxides and the plant-tolerated mineral acid salts and metal complexes of I.The compounds I are suitable as fungicides.
    Type: Grant
    Filed: December 21, 1990
    Date of Patent: March 16, 1993
    Assignee: BASF Aktiengesellschaft
    Inventors: Thomas Zierke, Bernhard Zipperer, Hubert Sauter, Eberhard Ammermann, Gisela Lorenz
  • Patent number: 5187170
    Abstract: Thiocarboxylic esters of the formula I ##STR1## where the substituents have the following meanings: X is oxygen, sulfur, oxymethylene, methyleneoxy, thiomethylene, methylenethio, ethylene, ethenylene or ethynylene,Y,Z are each sulfur or oxygen, but Y and Z are not simultaneously oxygen,R is alkyl, mononuclear, dinuclear or trinuclear aryl or hetaryl, where aryl and hetaryl may be substituted,and fungicidal agents containing these compounds.
    Type: Grant
    Filed: February 4, 1992
    Date of Patent: February 16, 1993
    Assignee: BASF Aktiengesellschaft
    Inventors: Horst Wingert, Hubert Sauter, Siegbert Brand, Bernd Wenderoth, Gisela Lorenz, Eberhard Ammermann
  • Patent number: 5177080
    Abstract: Substituted pyridyl-dihydroxy-heptenoic acid of the formula ##STR1## and its salts, if desired in an isomeric form, have a superior inhibitory action on HMG-CoA reductase and thus bring about a surprisingly good lowering of the cholesterol content in the blood.
    Type: Grant
    Filed: November 26, 1991
    Date of Patent: January 5, 1993
    Assignee: Bayer Aktiengesellschaft
    Inventors: Rolf Angerbauer, Peter Fey, Walter Hubsch, Thomas Philipps, Hilmar Bischoff, Dieter Petzinna, Delf Schmidt, Gunter Thomas
  • Patent number: 5169857
    Abstract: Novel compounds for treating hyperproteinaemia, lipoproteinaemia or arteriosclerosis of the formula ##STR1## in which A, B, D and E can have varied meanings,X is --CH.sub.2 --CH.sub.2 or --CH.dbd.CH--, andR is ##STR2## wherein R.sup.21 denotes hydrogen or alkyl andR.sup.22denotes hydrogen,deontes alkyl, aryl or aralkyl, ordenotes a cation,and their oxidation products.
    Type: Grant
    Filed: December 13, 1990
    Date of Patent: December 8, 1992
    Assignee: Bayer Aktiengesellschaft
    Inventors: Rolf Angerbauer, Peter Fey, Walter Hubsch, Thomas Philipps, Hilmar Bischoff, Dieter Petzinna, Delf Schmidt, Gunter Thomas
  • Patent number: 5164112
    Abstract: .alpha.-hydroxyketone derivatives represented by the general formula (I) which are novel optically active compounds; liquid crystal compositions, such as chiral smectic or chiral nematic compositions, containing the derivatives; and liquid crystal devices using the compositions. ##STR1## wherein A and B are independently a radical represented by the general formula (II): ##STR2## wherein R.sup.2 is an aliphatic hydrocarbon having 1 to 16 carbon atoms, which may contain --O-- and may be substituted by a cyano group and/or a halogen atom, ##STR3## are independently a single bond, ##STR4## etc., X and Y are independently a single bond, or --CH.sub.2 CH.sub.2 --, etc., or an aliphatic hydrocarbon having 1 to 16 carbon atoms; R.sup.1 is an alkyl group, a phenyl group, or a cyclohexyl group; n is 0 or 1; and the asterisk (*) indicates an asymmetric carbon atom.
    Type: Grant
    Filed: July 17, 1990
    Date of Patent: November 17, 1992
    Assignee: Chisso Corporation
    Inventors: Shinichi Saito, Hiromichi Inoue, Kouji Ohno
  • Patent number: 5162573
    Abstract: 2-Propyl-2-pentanoic acid (valproic acid) esters and (E)-2-propyl-2-pentenoic acid [(E)-2-valproenoic acid] esters surprisingly proved to have valuable properties, in that they show anticonvulsive and antiepileptic activities comparable with those of valproic acid, as well as an improved bioavailability and a markedly reduced toxicity.
    Type: Grant
    Filed: June 17, 1987
    Date of Patent: November 10, 1992
    Assignee: Chiesi Farmaceutici S.p.A.
    Inventors: Paolo Chiesi, Vittorino Servadio, Flavio Villani