Chalcogen Bonded Directly At The 2-position Of The Oxazole Ring Patents (Class 548/221)
  • Patent number: 5223517
    Abstract: Heterocyclically substituted cycloalkano[b]-indolesulphonamides can be prepared by reaction of appropriate N-unsubstituted indoles with acrylonitrile, followed by hydrolysis, esterification or amidation, or by reaction of heterocyclically substituted hydrazines with cycloalkanones or by subsequent introduction of the heterocyclic group into appropriate indole derivatives. The heterocyclically substituted cycloalkano[b]-indolesulphonamides can be employed for the treatment of thromboembolic disorders, ischaemias, arteriosclerosis, asthma, allergies and for the prophylaxis of myocardial infarcts.
    Type: Grant
    Filed: August 23, 1991
    Date of Patent: June 29, 1993
    Assignee: Bayer Aktiengesellschaft
    Inventors: Ulrich E. Muller, Ulrich Niewohner, Elisabeth Perzborn, Erwin Bischoff, Hans-Georg Dellweg
  • Patent number: 5223616
    Abstract: A heterocyclic compound which is useful for dyeing or printing hydrophobic fiber materials and which has the following formula (I), ##STR1##wherein A.sub.1, A.sub.2, A.sub.3 and A.sub.4 are each hydrogen, halogen, alkyl, alkoxy or alkenyl, X.sub.1 is --O-- or the like, R.sub.1 is a methylene or the like, X.sub.2 is a direct linkage or a divalent group of --O--, --S--, --SO--, --SO.sub.2 --, ##STR2## in which R.sub.3 is a hydrogen atom or a C.sub.1-4 alkyl group, ##STR3## in which R.sub.3 is as defined above, T and u are each independently hydrogen or a C.sub.1-4 alkyl, l is O or an integer of 1 to 3, Q is an unsubstituted or substituted 5-, 6- or 7-membered saturated or unsaturated heterocyclic residue, Y is hydrogen, C.sub.1-4 alkyl, a C.sub.1-4 alkoxy group or the like.
    Type: Grant
    Filed: November 4, 1991
    Date of Patent: June 29, 1993
    Assignee: Sumitomo Chemical Company, Ltd.
    Inventors: Jun Yamamoto, Junichi Sekihachi, Yosuke Yamamoto, Kazuhiro Machiguchi, Yutaka Kayane
  • Patent number: 5223614
    Abstract: Compounds of formula ##STR1## wherein the substituents are defined hereinbelow, useful in the treatment of bronchospasm are described.
    Type: Grant
    Filed: October 25, 1990
    Date of Patent: June 29, 1993
    Assignee: Boehringer Ingelheim GmbH
    Inventors: Kurt Schromm, Anton Mentrup, Ernst-Otto Renth, Gojko Mualcevic, Werner Traunecker
  • Patent number: 5214169
    Abstract: The present invention as directed to a new class of N-(2,3-epoxycyclopentyl) carbamate derivatives as described by Formula V below, that are useful as chemical intermediates in the production of a new class of anti-hypertensives: ##STR1##
    Type: Grant
    Filed: April 30, 1992
    Date of Patent: May 25, 1993
    Assignee: Merrell Dow Pharmaceuticals Inc.
    Inventor: Theophilus F. Leapheart
  • Patent number: 5213605
    Abstract: N-aryltetrahydrophthalimide compounds of the general formula I ##STR1## where n, R.sup.1, Y, R.sup.2 and R.sup.3 have the meanings stated in the claims and description, and a method for controlling undesirable plant growth.
    Type: Grant
    Filed: September 17, 1991
    Date of Patent: May 25, 1993
    Assignee: BASF Aktiengesellschaft
    Inventors: Lothar Rueb, Karl Eicken, Peter Plath, Barbara Schwalge, Karl-Otto Westphalen, Bruno Wuerzer, Norbert Meyer
  • Patent number: 5196434
    Abstract: Compound of general formula (I): ##STR1## where R.sub.1, R.sub.2, R.sub.3, n, X and A are defined in the description.Medicinal products.
    Type: Grant
    Filed: September 26, 1991
    Date of Patent: March 23, 1993
    Assignee: Adir et Compagnie
    Inventors: Thierry Taverne, Isabelle Lesieur, Patrick Depreux, Daniel H. Caignard, Beatrice Guardiola, Gerard Adam, Pierre Renard
  • Patent number: 5182278
    Abstract: Compounds of general formula (I): ##STR1## in which: R.sub.1 denotes a hydrogen atom or a lower alkyl optionally substituted with a hydroxyl group,R.sub.2 and R.sub.3 :a- identical or different, denote a hydrogen atom, a lower alkyl, a lower alkenyl, a substituted or unsubstituted aryl, a substituted or unsubstituted (lower alkyl)aryl,b- are such that they form, with the nitrogen which carries them, a saturated or unsaturated, mono- or bicyclic heterocyclic system containing at most 3 hetero atoms per ring, substituted or unsubstituted, with the exception of 1-arylpiperazine systems,X denotes a hydrogen atom,Y denotes a hydrogen atom or a hydroxyl,or alternatively X and Y denote an oxygen atom, provided thatR.sub.1 is then other than a methyl group,Z denotes a hydrogen atom or forms a .pi.
    Type: Grant
    Filed: July 29, 1991
    Date of Patent: January 26, 1993
    Assignee: Adir et Compagnie
    Inventors: Daniel Lesieur, Charles Lespagnol, Jacqueline Bonnet
  • Patent number: 5180419
    Abstract: There are provided o-carboxy-(5-oxo-2-imidazolin-2-yl)benzo-(5-membered)-heterocyclic compounds and derivatives thereof and a method for the use therewith to control monocotyledenous and dicotyledenous plant species.
    Type: Grant
    Filed: November 22, 1991
    Date of Patent: January 19, 1993
    Assignee: American Cyanamid Company
    Inventors: David M. Gange, Michael A. Guaciaro, Robert F. Doehner, Jr.
  • Patent number: 5180825
    Abstract: Disclosed in a mitomycin derivative represented by the formula (I): ##STR1## wherein W is a heterocyclic group.
    Type: Grant
    Filed: November 13, 1991
    Date of Patent: January 19, 1993
    Assignee: Kyowa Hakko Kogyo Co., Ltd.
    Inventors: Hitoshi Arai, Motomichi Kono, Masaji Kasai, Katsushige Gomi, Tadashi Ashizawa
  • Patent number: 5180417
    Abstract: Disclosed herein are derivatives of 4-((aryloxy)phenoxy)fluoroalkanoic acid and their use as active herbicides for the pre- and postemergent control of grassy weeds, especially in the presence of broadleaf crops.
    Type: Grant
    Filed: April 12, 1991
    Date of Patent: January 19, 1993
    Assignee: DowElanco
    Inventor: James A. Turner
  • Patent number: 5156667
    Abstract: Derivatives of 4-((aryloxy)phenoxy)alkenols, their preparation and use as active herbicides for the postemergent control of grassy weeds and especially the control of said weeds in the presence of corn plants are disclosed.
    Type: Grant
    Filed: April 12, 1991
    Date of Patent: October 20, 1992
    Assignee: DowElanco
    Inventors: James A. Turner, Paul S. Zorner, Wendy S. Jacks
  • Patent number: 5152929
    Abstract: Compounds of the formula I ##STR1## in which X is --S--, --O-- or --NH--, R is H or a monovalent substituent, n is 0 or 1 and R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are H, alkyl, alkyl which is substituted by OH, halogen, COOH or alkoxy, unsubstituted or substituted aryl or aralkyl, or carboxyl, or R.sup.1 and R.sup.2 or R.sup.1 and R.sup.3 together are alkylene or R.sup.1 and R.sup.2 are a direct bond, at least two of the groups R.sup.1, R.sup.2, R.sup.3 and R.sup.4 being carboxyl or carboxyalkyl groups, and base addition salts thereof are effective corrosion inhibitors. The preparation of these novel polycarboxylic acids can be effected by various processes.
    Type: Grant
    Filed: October 10, 1990
    Date of Patent: October 6, 1992
    Assignee: Ciba-Geigy Corporation
    Inventors: Robert L. Bentley, Michael P. Savage, Kenneth W. Shelton
  • Patent number: 5147883
    Abstract: Compounds of general formula (I): ##STR1## in which: R.sub.1 represents a hydrogen atom or a lower alkyl group,A represents a hydrogen atom, and in this case B represents a group CO-G, G being:either a heteroaryl group selected from furan, indole, pyrrole, pyridine, quinoline, isoquinoline and benzofuran, optionally substituted with one or more lower alkyl or lower alkoxy groups or a halogen atoms,or a linear or branched lower alkyl group substituted with a carboxyl group,or a linear or branched lower alkenyl group substituted with a carboxyl group,or a phenyl or naphthyl group substituted with a carboxyl group,or alternatively A forms with B a group CO(CH.sub.2).sub.n CH(CH.sub.
    Type: Grant
    Filed: May 31, 1991
    Date of Patent: September 15, 1992
    Assignee: Adir et Compagnie
    Inventors: Hocine Aichaioui, Daniel Lesieur, Charles Lespagnol, Michelle Devissaguet, Beatrice Guardiola
  • Patent number: 5147878
    Abstract: Aminoalkoxyphenyl derivatives useful in the treatment of certain pathological syndromes of the cardiovascular system of formula: ##STR1## in which: B represents a --S, --SO--, or --SO.sub.2 -- group,R.sub.1 and R.sub.2, which are identical or different, each denote hydrogen, a methyl or ethyl radical or a halogen such as chlorine, bromine or iodine, A denotes a straight- or branched-alkylene radical having from 2 to 5 carbon atoms or a 2-hydroxypropylene radical in which the hydroxy is optionally substituted by a lower alkyl radical, Ar represents a group ##STR2## R.sub.4 denotes hydrogen or an alkyl radical and Cy represents a cyclic group.
    Type: Grant
    Filed: April 19, 1990
    Date of Patent: September 15, 1992
    Assignee: Sanofi
    Inventors: Jean Gubin, Pierre Chatelain
  • Patent number: 5136043
    Abstract: A process for the preparation of aromatic sulfonyl chlorides of the formula I ##STR1## in which R.sub.1, R.sub.2 and R.sub.3 are identical or different and are hydrogen, fluorine, chlorine, bromine or iodine atoms, alkyl(C.sub.1 -C.sub.4), acetamido, nitro or carboxyl groups, or R.sub.1 and R.sub.2 together form an aromatic or heteroaromatic ring having 5 or 6 ring members, which can be substituted by fluorine, chlorine, bromine or iodine atoms, alkyl(C.sub.1 -C.sub.4), acetamido, nitro or carboxyl groups, by reaction of aromatic compounds of the formula II ##STR2## in which R.sub.1, R.sub.2 and R.sub.3 have the abovementioned meanings, with chlorosulfonic acid in excess or with chlorosulfonic acid or oleum and thionyl chloride, by reacting in the presence of sulfamic acid as a catalyst.
    Type: Grant
    Filed: August 16, 1991
    Date of Patent: August 4, 1992
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Michael Meier, Wolfgang Tronich
  • Patent number: 5132305
    Abstract: Compounds of general formula (I): ##STR1## in which: R.sub.1 denotes a hydrogen atom or a lower alkyl optionally substituted with a hydroxyl group,R.sub.2 and R.sub.3 :a--identical or different, denote a hydrogen atom, a lower alkyl, a lower alkenyl, a substituted or unsubstituted aryl, a substituted or unsubstituted (lower alkyl)aryl,b--are such that they form, with the nitrogen which carries them, a saturated or unsaturated, mono- or bicyclic heterocyclic system containing at most 3 hetero atoms per ring, substituted or unsubstituted, with the exception of 1-arylpiperazine systems,X denotes a hydrogen atom,Y denotes a hydrogen atom or a hydroxyl,or alternatively X and Y denote an oxygen atom, provided that R.sub.1 is then other than a methyl group,Z denotes a hydrogen atom or forms a .pi. bond with Y, andT denotes a hydrogen atom or a lower alkyl, their stereoisomers and their quaternary ammonium salts, as well as their addition salts with a pharmaceutically acceptable acid.
    Type: Grant
    Filed: February 26, 1990
    Date of Patent: July 21, 1992
    Assignee: Adir et Compagnie
    Inventors: Daniel Lesieur, Charles Lespagnol, Jacqueline Bonnet
  • Patent number: 5114952
    Abstract: A series of novel alkanesulphonamidophenyl-N-alkyl-N-(heterocyclic-alkyl)alkylamine derivatives have been prepared, including their pharmaceutically acceptable salts. These compounds are useful in therapy as anti-arrhythmic agents and therefore, are of value in the treatment of various cardiac arrhythmias. Said sulfonamide compounds are of the formula: ##STR1## wherein R and R.sup.1 are each C.sub.1 -C.sub.4 alkyl; X is --CH.sub.2 --, --CO-- or --CH(OH)--; n is two, three or four; and "Het" is a nitrogen-containing heterocyclic group wherein said heterocyclic group is preferably 2H-3,4-dihydroisoquinol-1-on-2-yl or 2H-isoquinol-1-on-2-yl, each optionally substituted with halogen or C.sub.1 -C.sub.4 alkyl.
    Type: Grant
    Filed: November 21, 1990
    Date of Patent: May 19, 1992
    Assignee: Pfizer Inc.
    Inventors: John E. Arrowsmith, Peter E. Cross, Geoffrey N. Thomas
  • Patent number: 5110823
    Abstract: Pyrrolidine derivatives of formula (I) are disclosed. ##STR1## wherein the ring A represents the following heterocyclic ring ##STR2## The compounds of formula (I) are useful as nootropic agents.
    Type: Grant
    Filed: February 26, 1991
    Date of Patent: May 5, 1992
    Assignee: Nisshin Flour Milling Co., Ltd.
    Inventors: Fumiko Hamaguchi, Tatsuo Nagasaka, Rie Hakamada, Einosuke Sakurai
  • Patent number: 5105009
    Abstract: Intermediates of Formula ##STR1## where R is a methylthio, methylsulfoxy, methylsulfonyl or a nitro group; andX1 is hydrogen, 1-6 C alkyl, 1-6 C haloalkyl, 3-6 C cycloalkyl, phenyl or phenylalkyl(1-6C), where the phenyl ring may be substituted by one or two halogen, 1-3 C alkyl, 1-3 C alkoxy or nitro; orX1 together with X2 is an oxygen atom or an alkylene having from two to five Carbon atoms; orX1 together with X2 and R4 is a chain of formula ##STR2## where p is 3 or 4 and q is 1 or 2; and X2 is hydrogen, 1-6 C alkyl, 1-6 C haloalkyl, 3-6 C cycloalkyl or phenyl which may be substituted by one or two halogen, 1-3 C alkyl, 1-3 C alkoxy or nitro; orX2 together with R4 is ##STR3## where n is 1 or 2; m is 0 or 1; X is hydrogen, halogen, 1-3 C alkyl, 1-3 C alkoxy or nitro; andX3 is hydrogen or --CO--R4 where R4 is hydrogen, 1-6 alkyl, 1-6 C haloalkyl, 3-6 C cycloalkyl, phenylalkyl(1-6C) or phenyl where the phenyl ring may be substituted by one or two halogen, 1-3 alkyl, 1-3 alkoxy or nitro; andX4 is --OH, fluorine,
    Type: Grant
    Filed: February 29, 1988
    Date of Patent: April 14, 1992
    Assignee: Zambon S.p.A.
    Inventors: Giancarlo Jommi, Dario Chiarino
  • Patent number: 5103007
    Abstract: Lipid derivatives represented by the formula: ##STR1## wherein R.sup.1 stands for an optionally substituted higher alkyl group, R.sup.2 stands for an optionally substituted lower alkyl group or an optionally substituted nitrogen-containing heterocyclic group, R.sup.3 stands for a tertiary amino group or a quaternary ammonium group, J stands for oxygen atom or S(O)t (where t deontes 0, 1 or 2), m and n respectively denotes 1 or 2, p denotes 0, 1 or 2, q and r respectively denote an integer of 2 to 5.and salts thereof have antitumor activities including differentiation-inducing activity and are useful as antitumor agents.
    Type: Grant
    Filed: October 27, 1989
    Date of Patent: April 7, 1992
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Hiroaki Nomura, Hiroshi Akimoto, Keizo Inoue
  • Patent number: 5102898
    Abstract: Novel compounds of the formula ##STR1## wherein X is I or Br; andY is independently selected from the group consisting of H, halogen, NO.sub.2, (C.sub.1 -C.sub.4) alkyl, (C.sub.1 -C.sub.4) alkoxy, CN, OCO (C.sub.1 -C.sub.4) alkyl, OCOPh or halo (C.sub.1 -C.sub.4) alkyl, are disclosed as having microbicidal activity.
    Type: Grant
    Filed: May 8, 1991
    Date of Patent: April 7, 1992
    Assignee: Rohm and Haas Company
    Inventor: Adam C. Hsu
  • Patent number: 5101034
    Abstract: A process for the preparation of a heteroaryloxyacetamide of the formula ##STR1## in which R is a 5 membered heterocycle which may be benzo-fused, andR.sup.1 and R.sup.2 each independently is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl or cycloalkenyl, halogenoalkyl, alkoxyalkyl, alkoxy, aralkyl or aryl, orR.sup.1 and R.sup.2, together with the nitrogen atom to which they are bonded, form a heterocycle,which comprises reacting a sulphonylated heteroaromatic of the formulaR--SO.sub.2 --R'in whichR' is lower alkyl or benzyl,with an .alpha.-oxyacetamide of the formula ##STR2## in which R" is hydrogen or acyl,in the presence of an inorganic base as an acid acceptor and of solvent as a diluent at a temperature of about -50.degree. C. to +150.degree. C. The products are known herbicides.
    Type: Grant
    Filed: March 7, 1991
    Date of Patent: March 31, 1992
    Assignee: Bayer Aktiengesellschaft
    Inventors: Thomas Schmidt, Hans-Joachim Diehr
  • Patent number: 5099021
    Abstract: Process for the preparation of pure, unsymmetrically disubstituted ureas of the general formula ##STR1## in which R denotes a phenyl radical which is unsubstituted, or monosubstituted or polysubstituted by halogen atoms or alkyl, alkoxy, aryloxy or trifluoromethyl groups, an oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, benzoxazolyl or benzothiazolyl radical which is unsubstituted, or monosubstituted or polysubstituted by halogen atoms or alkyl, alkoxy or trifluoromethyl groups and R.sub.1 and R.sub.2 independently of one another denote a hydrogen atom or an alkyl group, where R.sub.1 and R.sub.2 are not simultaneously hydrogen or R.sub.1 and R.sub.2 together denote a butylene or pentylene group, by reaction of an N-alkyl- or N,N-dialkylurea with an unsubstituted or substituted arylamine or a heterocyclic amine in the presence of that amine which is already present in the starting material, the respective N-alkyl- or N,N-dialkylurea.
    Type: Grant
    Filed: October 30, 1990
    Date of Patent: March 24, 1992
    Assignee: Agrolinz Agrarchemikalien Gesellschaft m.b.H.
    Inventors: Rudolf H. Worther, Horst Korntner, Egmont Auer, Kurt Thonhofer
  • Patent number: 5097034
    Abstract: Color formers of the formula ##STR1## in which X.sup.1 denotes hydroxyl, alkoxy, alkenyloxy, aralkoxy, cycloalkoxy, aryloxy or acyloxy,R.sup.1 denotes hydrogen, halogen, alkyl or alkoxy,R.sup.2 denotes hydrogen, alkoxy, aralkoxy, aryloxy or a radical of the formula ##STR2## Y.sup.1 and Y.sup.2, independently of one another, denote alkyl, cycloalkyl or aralkyl,R.sup.2 can form a heterocyclic ring with A in the o-position, in which a benzene ring can be additionally fused onto ring A in the o-/m-position with respect to R.sup.2,R.sup.3 denotes hydrogen, alkyl, alkenyl, aralkyl, cycloalkyl or aryl, or R.sup.3 is linked to ring B in the o-position with respect to the nitrogen,Z.sup.1 stands for the remaining members of a partially hydrogenated or completely hydrogenated ring, with the proviso that Z.sup.
    Type: Grant
    Filed: May 14, 1991
    Date of Patent: March 17, 1992
    Assignee: Bayer Aktiengesellschaft
    Inventor: Udo Eckstein
  • Patent number: 5091533
    Abstract: Compounds of the formula: ##STR1## where R.sup.2 contains certain aryls or heteroaryls are effective leukotriene inhibitors.
    Type: Grant
    Filed: March 12, 1990
    Date of Patent: February 25, 1992
    Assignee: Merck Frosst Canada, Inc.
    Inventors: Patrice C. Belanger, Claude Dufresne, Brian Fitzsimmons, deceased, Maryann Fitzsimmons, Heir, Yvan Guindon, Cheuk K. Lau, Joshua Rokach, John Schiegetz, Michel Therien, Robert N. Young
  • Patent number: 5086062
    Abstract: This invention relates to certain benzoxazolinones which inhibit lipoxygenase and/or cyclooxygenase enzymes. Such compounds are useful in inhibiting such enzymes, per se, and are useful in treating allergic and inflammatory conditions in a mammal. This invention also relates to methods of inhibiting lipoxygenase and/or cyclooxygenase in a mammal with such benzoxazolinones; methods of treating an allergic condition in a mammal with such compounds; methods of treating an inflammatory condition in a mammal with such compounds; and pharmaceutical compositions comprising the benzoxazolinones hereof.
    Type: Grant
    Filed: May 29, 1990
    Date of Patent: February 4, 1992
    Assignee: Pfizer Inc.
    Inventors: Kazuo Ando, Nobuko Asai, Fumitaka Ito, Takashi Mano, Masami Nakane, Kunio Satake, Kaoru Shimada
  • Patent number: 5081245
    Abstract: A compound represented by the formula: ##STR1## wherein R represents a hydrogen atom or a lower alkyl group;R.sup.1 represents a higher alkyl group which may be substituted;R.sup.2 represents a hydrogen atom or a lower alkyl group, a lower alkanoyl group or a nitrogen-containing 5- to 7-membered heterocyclic group each of which may be substituted; X represents a divalent group represented by the formula:--(OCH.sub.2 CH.sub.2).sub.p --wherein p represents an integer of 1 to 5, a divalent group represented by the formula:--O(CH.sub.2).sub.q --wherein q represents an integer of 3 to 8, or a divalent group represented by the formula:--(OCH.sub.2 CH.sub.2).sub.p --J--(CH.sub.2).sub.q --wherein J represents an oxygen atom or a group represented by the formula: --S(O).sub.
    Type: Grant
    Filed: August 18, 1989
    Date of Patent: January 14, 1992
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Hiroaki Nomura, Hiroshi Akimoto, Eiko Imamiya, Keizo Inoue
  • Patent number: 5077401
    Abstract: Herbicidal benzo-fused cyclic compounds of the formula ##STR1## wherein Q is ##STR2## Y is O or S, W is ##STR3## T is O, S, --NH-- or ##STR4## and R.sup.4 may represent, together with T, chlorine,Z is O or S,X is hydrogen or halogen,n is 0 or 1 andR is C.sub.3-6 cycloalkyl, and optionally substituted 5-membered heterocyclic group or an optionally substituted 6-membered heteroaromatic group which contains one to three nitrogen atoms,and salts thereof.
    Type: Grant
    Filed: October 6, 1989
    Date of Patent: December 31, 1991
    Assignee: Nihon Tokushu Noyaku Seizo K.K.
    Inventors: Toyohiko Kume, Toshio Goto, Atsumi Kamochi, Akihiko Yanagi, Shigeki Yagi, Hiroshi Miyauchi, Katsuhiko Shibuya
  • Patent number: 5077309
    Abstract: Novel compounds have the formula (I) ##STR1## where ##STR2## represents one of the divalent cyclic groups ##STR3## the letters a and b indicating in each case the points of attachment of the substituents R.sup.1 and CV(R.sup.2)-NV'R, respectively; R.sup.1 is a group --(CH.sub.2).sub.b --(A).sub.a --(CH.sub.2).sub.c --B--CH.sub.2 --CO.sub.2 R' in which A and B are each separately oxygen or sulphur, a is 0, b is 0 and c is an integer from 3 to 10, or a is 1, b is 0 or an integer from 1 to 7 and c is an integer from 2 to 9 with the sum of b and c being from 2 to 9, and CO.sub.2 R' is a carboxy group or an amide, ester or salt derivative thereof; V and V' either each separately is hydrogen or together are the second bond of a carbon-nitrogen double bond; R.sup.2 is hydrogen, an aliphatic hydrocarbon group or an aliphatic hydrocarbon group substituted by an aromatic group directly or through an oxygen or sulphur atom; and R is a group --OR.sup.3, --OR.sup.4, --D--R.sup.3, --N.dbd. R.sup.5 or --NW.G.
    Type: Grant
    Filed: March 28, 1990
    Date of Patent: December 31, 1991
    Assignee: National Research Development Corporation
    Inventors: Robert L. Jones, Norman H. Wilson
  • Patent number: 5071863
    Abstract: Certain 6-aryl- or 6-heteroaryl- alkylaminobenzoxazolones, and their pharmaceutically-acceptable salts, are dual inhibitors of lipoxygenase and cyclooxygenase enzymes, and so are useful as antiallergy and antiinflammatory agents.
    Type: Grant
    Filed: July 18, 1990
    Date of Patent: December 10, 1991
    Assignee: Pfizer Inc.
    Inventors: Fumitaka Ito, Takashi Mano, Masami Nakane
  • Patent number: 5055582
    Abstract: This invention relates to a process for preparing useful thromboxane A.sub.2 inhibiting (.+-.)7-[3.alpha.-[1-[[(phenylamino)thioxomethyl]hydrazono]ethyl]-1.alpha. ,4.alpha.-bicyclo[2.2.1]hept-2.beta.-yl]-heptenoic acids and useful derivatives thereof from (.+-.)octahydro-1.alpha.-methyl-3a.alpha.,7a.alpha.-4.alpha.,7.alpha.-meth ano-2H-inden-2-ones.
    Type: Grant
    Filed: December 13, 1988
    Date of Patent: October 8, 1991
    Assignee: National Research Development Corporation
    Inventors: Robert B. Garland, Masateru Miyano
  • Patent number: 5037841
    Abstract: Novel 1,3-disubstituted pyrrolidines active on the central nervous system of the formula ##STR1## wherein A denotes phenyl or hetaryl, which is optionally fused with aromatic, saturated or unsaturated cyclic or heterocyclic hydrocarbons, where this radical can optionally be substituted,X denotes --O--CH.sub.2 --, --CH.sub.2 --O-- or --O--,n denotes a number from 1 to 19, andB denotes cyano or a group of the formula --COOR.sup.1, --CONR.sup.2 R.sup.3, --SO.sub.2 NR.sup.2 R.sup.3, --SO.sub.m R.sup.4, --NR.sup.5 R.sup.6, or --C.tbd.C--CH.sub.2 --NR.sup.5 R.sup.6,and salts thereof.
    Type: Grant
    Filed: April 12, 1989
    Date of Patent: August 6, 1991
    Assignee: Bayer Aktiengesellschaft
    Inventors: Rudolf Schohe, Peter-Rudolf Seidel, Jorg Traber, Thomas Glaser
  • Patent number: 5036088
    Abstract: Compounds of the formula ##STR1## where Y is alkyl, aryl or heterocyclic, n is 1-7, R is hydrogen, alkyl, aralkyl or carboxymethyl, R.sub.1 is acetoxy, thiophenoxy, hydrogen, halo, alkyl, alkoxy or trifluoromethyl, R.sub.2 is hydrogen, alkyl or alkanoyl and X is C.dbd.O, CH.sub.2, NH, O or S as antiallergy and antiinflammatory agents.
    Type: Grant
    Filed: December 3, 1990
    Date of Patent: July 30, 1991
    Assignee: Pfizer Inc.
    Inventors: Yoshihiko Kitaura, Fumitaka Ito, Rodney W. Stevens, Nobuko Asai
  • Patent number: 5034050
    Abstract: Derivatives of 4-((aryloxy)phenoxy)alkenols, their preparation and use as active herbicides for the postemergent control of grassy weeds and especially the control of said weeds in the presence of corn plants are disclosed.
    Type: Grant
    Filed: June 16, 1989
    Date of Patent: July 23, 1991
    Assignee: DowElanco
    Inventors: James A. Turner, Paul S. Zorner, Wendy S. Jacks
  • Patent number: 5032590
    Abstract: Substituted hydroxylamines of the formula ##STR1## in which R.sup.1 stands for an aromatic or heterocyclic radical,are especially useful in the treatment of hyperlipoproteinaemia, lipoproteinaemia and atherosclerosis.
    Type: Grant
    Filed: March 8, 1990
    Date of Patent: July 16, 1991
    Assignee: Bayer Aktiengesellschaft
    Inventors: Walter Hubsch, Rolf Angerbauer, Peter Fey, Hilmar Bischoff, Dieter Petzinna, Delf Schmidt
  • Patent number: 5026848
    Abstract: A heteroaryloxyalkylheterocyclic derivative of the Formula I:R--(CH.sub.2).sub.n --O--R.sup.1 Iis provided wherein:R is a non-fused azole moiety;n is 5, 6, 7 or 8; andR.sup.1 is a non-fused or fused substituted azole, azine, furyl or polycyclic hydrocarbon.
    Type: Grant
    Filed: March 27, 1989
    Date of Patent: June 25, 1991
    Assignee: Synphar Laboratories Incorporated
    Inventors: Mohsen Daneshtalab, Dai Q. Nguyen, Chan M. Ha, Hiep T. Luu, Laurence M. Tempest, Ronald G. Micetich
  • Patent number: 5021438
    Abstract: Novel compounds having an affinity for 5-hydroxytryptamine receptors of the formula ##STR1## in which R.sup.1 stands for H, alkyl, aralkyl or heteroarylalkyl,X stands for H, OCH.sub.3, OH, SCH.sub.3, halogen, CN or CONH.sub.2,Y stands for a straight-chain or branched, saturated or unsaturated alkylene chain having up to 6 carbon atomsandZ stands for a group of the formula ##STR2## --OR.sup.4, --SO.sub.m R.sup.5, --COOR.sup.6 or CONR.sup.7 R.sup.8 or salts thereof.
    Type: Grant
    Filed: March 15, 1989
    Date of Patent: June 4, 1991
    Assignee: Bayer Aktiengesellschaft
    Inventors: Bodo Junge, Bernd Richter, Thomas Glaser, Jorg Traber
  • Patent number: 5007952
    Abstract: Herbicidally active pyrroles of the formula ##STR1## wherein R.sup.1 represents C.sub.1-4 alkyl, or one R.sup.1 together with the other R.sup.1 forms tetramethylene or butenylene,X represents hydrogen or halogen,Y represents O or S,n represents 0 or 1,R.sup.2 represents hydrogen or an organic radical.
    Type: Grant
    Filed: November 9, 1989
    Date of Patent: April 16, 1991
    Assignee: Nihon Tokushu Noyaku Seizo K.K.
    Inventors: Toyohiko Kume, Toshio Goto, Atsumi Kamochi, Akihiko Yanagi, Hiroshi Miyauchi, Tadao Asami
  • Patent number: 4996218
    Abstract: Compounds of the general formula (I) ##STR1## and physiologically acceptable salts and solvates thereof, which have .beta..sub.2 -adrenoreceptor stimulant activity. They may be used in the treatment of diseases associated with reversible airways obstruction, such as asthma and chronic bronchitis.In preferred embodiments, Q represents a chlorine atom or a trifluoromethyl group, X represents a C.sub.3-4 alkylene chain, Y a C.sub.1-5 alkylene chain, R, R.sup.1 and R.sup.2 are each preferably a hydrogen atom or a methyl group and Het represents a pyrimidinyl pyrazinyl, triazinyl, thiazolyl, quinolinyl, benzimidazolyl, benzothiazolyl, benzoxazolyl or pyridyl group.
    Type: Grant
    Filed: August 10, 1988
    Date of Patent: February 26, 1991
    Assignee: Glaxo Group Limited
    Inventor: Lawrence H. C. Lunts
  • Patent number: 4992563
    Abstract: This invention relates to several intermediates useful in preparing thromboxane A.sub.2 inhibiting (.+-.)7-[3.alpha.-[1-[[(phenylamino)-thioxomethyl]hydrazono]ethyl]-1.alpha ., 4.alpha.-bicyclo[2.2.1]hept-2.beta.-yl]-heptenoic acids and useful derivatives thereof from (.+-.)octahydro-1.alpha.-methyl-3a.alpha., 7a.alpha.-4.alpha.,7.alpha.-methano-2H-inden-2-ones.
    Type: Grant
    Filed: December 13, 1988
    Date of Patent: February 12, 1991
    Assignee: National Research Development Corporation
    Inventors: Robert B. Garland, Masateru Miyano
  • Patent number: 4988718
    Abstract: Fungicidal substituted 4-heterocyclyloximinopyrazolin-5-ones of the formula ##STR1## in which R.sup.1 and R.sup.2 independently of one another in each case represent hydrogen, alkyl, alkenyl, alkinyl, cyanoalkyl, hydroxyalkyl, alkoxyalkyl, alkylthioalkyl, alkoxycarbonyl, hydroxycarbonylalkyl, alkoxycarbonylalkyl, aminocarbonylalkyl, alkylaminocarbonylalkyl or dialkylaminocarbonylalkyl, or represent in each case unsubstituted or in each case substituted oxiranylalkyl, aralkyl, heterocyclyl or aryl andHet represents an unsubstituted or substituted heterocycle.
    Type: Grant
    Filed: August 9, 1990
    Date of Patent: January 29, 1991
    Assignee: Bayer Aktiengesellschaft
    Inventors: Kurt Findeisen, Klaus Jelich, Gerd Hanssler
  • Patent number: 4968844
    Abstract: Retinal is prepared by condensing a C.sub.15 sulphide of formula: ##STR1## in which R.sub.1 denotes aryl, aralkyl, pyridyl, 2-thiazolyl, 2-benzothiazolyl, 2-benzimidazolyl or 2-benzoxazolyl, with a haloacetal of formula: ##STR2## in which X denotes a halogen atom and R denotes an alkyl radical containing 1 to 4 carbon atoms, to give a C.sub.20 sulphide acetal of formula: ##STR3## in which R.sub.1 and R are defined as above, hydrolysing the said sulphide acetal to give a C.sub.20 sulphide aldehyde of formula: ##STR4## in which R.sub.1 is defined as above, desulphurizing the said sulphide aldehyde to give retinal, and isolating the retinal obtained.
    Type: Grant
    Filed: October 27, 1988
    Date of Patent: November 6, 1990
    Assignee: Centre National de la Recherche Scientifique (C. N. R. S.)
    Inventor: Marc Julia
  • Patent number: 4968681
    Abstract: Substituted hydroxylamines of the formula ##STR1## in which R.sup.1 stands for an aromatic or heterocyclic radical, are especially useful in the treatment of hyperlipoproteinaemia, lipoproteinaemia and atherosclerosis.
    Type: Grant
    Filed: November 15, 1988
    Date of Patent: November 6, 1990
    Assignee: Bayer Aktiengesellschaft
    Inventors: Walter Hubsch, Rolf Angerbauer, Peter Fey, Hilmar Bischoff, Dieter Petzinna, Delf Schmidt
  • Patent number: 4963576
    Abstract: The invention relates to dithioacetal compounds having 5-lipoxygenase-inhibiting activity, of the formula: ##STR1## wherein R.sup.1 is lower alkyl, di-(lower)alkylamino, aryl, or heterocyclic group which may have one or more substituents selected from halogen, lower alkyl, lower alkoxy and phenyl,R.sup.2 and R.sup.3 are each lower alkyl, aryl or ar-(lower)alkyl, or R.sup.2 and R.sup.3 are together to form 1,3-dithian ring,R.sup.4 is hydrogen or lower alkoxy, andn is O or an integer 1 to 4 and pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: May 6, 1988
    Date of Patent: October 16, 1990
    Assignee: Fujisawa Pharmaceutical Company, Ltd.
    Inventors: Teruo Oku, Yoshio Kawai, Hiroshi Kayakiri, Kazuyoshi Kuratani, Masashi Hashimoto
  • Patent number: 4952599
    Abstract: Novel substituted phenylthioureas, phenylisothioureas and phenylcarbodiimides of formula I ##STR1## wherein R.sub.1 is C.sub.1 -C.sub.10 alkyl, unsubstituted or substituted by one or more halogen atoms and/or C.sub.1 -C.sub.6 alkoxy groups; C.sub.3 -C.sub.6 alkenyl, C.sub.3 -C.sub.8 cycloalkyl, C.sub.3 -C.sub.8 cycloalkyl which is substituted by one or more halogen atoms and/or C.sub.1 -C.sub.4 alkyl groups; C.sub.3 -C.sub.8 cycloalkyl-C.sub.1 -C.sub.4 alkyl, di(C.sub.3 -C.sub.8)cycloalkyl-C.sub.1 -C.sub.4 alkyl; C.sub.1 -C.sub.4 phenylalkyl or C.sub.1 -C.sub.4 phenylalkyl which is substituted in the phenyl nucleus by one or more members selected from the group consisting of halogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy and/or C.sub.1 -C.sub.4 haloalkyl; or is C.sub.5 -C.sub.6 cycloalkenyl,R.sub.2 is hydrogen, C.sub.1 -C.sub.5 alkyl or C.sub.5 -C.sub.6 cycloalkenyl,R.sub.3 is C.sub.1 -C.sub.5 alkyl or C.sub.5 -C.sub.6 cycloalkyl,R.sub.4 is hydrogen or C.sub.1 -C.sub.3 alkyl,R.sub.
    Type: Grant
    Filed: July 20, 1988
    Date of Patent: August 28, 1990
    Assignee: Ciba-Geigy Corporation
    Inventors: Josef Ehrenfreund, Manfred Boger, Jozef Drabek
  • Patent number: 4937255
    Abstract: For inhibiting 3-hydroxy-3-methylglutaryl coenzyme A and cholesterol biosynthesis, the novel disubstituted pyrroles of the formula ##STR1## in which R.sup.1 is aryl or heteroaryl,R.sup.2 is cycloalkyl or optionally substituted alkyl,R.sup.3 is hydrogen or 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, a cation or alkyl, aryl or aralkyl.
    Type: Grant
    Filed: March 16, 1989
    Date of Patent: June 26, 1990
    Assignee: Bayer Aktiengesellschaft
    Inventors: Walter Hubsch, Rolf Angerbauer, Peter Fey, Hilmar Bischoff, Dieter Petzinna, Delf Schmidt, Gunter Thomas
  • Patent number: 4935522
    Abstract: A method for producing ethyl 2-[4'-(6"-chloro-2"-benzoxazolyloxy)phenoxy]propanoate by reacting a hydroxyaromatic ketone derivative with a 2-substituted propanoic ester under basic conditions and thereafter oxidizing the intermediate with subsequent hydrolysis and reaction with 2,6-dichlorobenzoxazole.
    Type: Grant
    Filed: March 21, 1988
    Date of Patent: June 19, 1990
    Assignee: Hoechst Celanese Corporation
    Inventors: Varadaraj Elongo, Kenneth G. Davenport
  • Patent number: 4935423
    Abstract: A substituted, 1,2,4-triazinedione of the formula ##STR1## in which R.sup.1 stands for an unsubstituted or substituted heteroaromatic radicals bonded via carbon,X stands for one or more, identical or different radicals selected from the group consisting of hydrogen, halogen, nitro, alkyl, alkoxy, alkylthio, halogenoalkyl, halogenoalkoxy and halogenoalkylthio.R.sup.3 stands for hydrogen, unsubstituted or substituted alkyl, alkenyl, alkinyl or aralkyl. The substituted 1,2,4-triazinedione is useful to combat parasitic protozoa in warmblooded animals.
    Type: Grant
    Filed: February 14, 1989
    Date of Patent: June 19, 1990
    Assignee: Bayer Aktiengesellschaft
    Inventors: Werner Lindner, Axel Haberkorn
  • Patent number: 4911754
    Abstract: This invention relates to aryloxy dihydrobenzofuran, oxoindole or benzofuranone derivatives having herbicidal activity and to the use of such compounds to control the growth of noxious plants, i.e., weeds.
    Type: Grant
    Filed: July 16, 1987
    Date of Patent: March 27, 1990
    Assignee: American Cyanamid Company
    Inventors: David A. Hunt, James A. Schwindeman
  • Patent number: 4910309
    Abstract: The optical purity of an optically active 2-(4-aryloxyphenoxy)propionic acid is enriched by formation of the hydrate of the enantiomer in excess and its removal from solution.
    Type: Grant
    Filed: July 8, 1988
    Date of Patent: March 20, 1990
    Assignee: The Dow Chemical Company
    Inventors: Larry D. Kershner, Jimmy J. Tai