5-position Is Unsubstituted Or Alkyl Substituted Only Patents (Class 544/312)
  • Patent number: 4871387
    Abstract: New pyri(mi)dyl-oxy- or -thio-benzoic acid derivatives of the formula ##STR1## are taught which have herbicidal and plant growth regulating activity. In the formula Z can be Ch or N, X is oxygen or sulphur, A is oxygen, sulphur, a radical R.sup.5 --N.dbd.or a radical R.sup.6 O--N.dbd.and B is oxygen, sulphur, a radical ##STR2## with the proviso that at least one of the radicals R.sup.1, R.sup.2 or R.sup.3 represents alkyl or a part of a 3- to 6-membered fused carbocyclic ring.
    Type: Grant
    Filed: December 4, 1986
    Date of Patent: October 3, 1989
    Assignee: Bayer Aktiengesellschaft
    Inventors: Klaus Sasse, Reiner Fischer, Hermann Hagemann, Hans-Joachim Santel, Robert R. Schmidt, Kalus Lurssen
  • Patent number: 4851030
    Abstract: Novel benzenesulfonamide compounds containing an ortho-heterocyclicmethylene substituent such as N-[(4,6-dimethoxypyrimidin-2-yl)aminocarbonyl]-2-(5-methylthio-1,3,4-thiad iazol-2-ylmethyl)benzenesulfonamide are useful as preemergent and/or postemergent herbicides and/or plant growth regulants.
    Type: Grant
    Filed: December 8, 1986
    Date of Patent: July 25, 1989
    Assignee: E. I. Du Pont de Nemours and Company
    Inventor: Morris P. Rorer
  • Patent number: 4826843
    Abstract: A series of diazinylpiperidine compounds of Formula I ##STR1## wherein X is an ethylene chain or a 1,2-benzo ring; Y is carbonyl or methylene; R.sup.1 is hydrogen or lower alkyl; and Z is an R.sup.2, R.sup.3 -disubstituted diazinyl ring selected from pyridazine, pyrimidine, and pyrazine ring systems. Pharmacologic and neuroanatomical testing demonstrates that compounds of the series act to enhance cerebral function in mammals, particularly when there is a deficit in normal cerebral functioning. Specific pharmacologic test results indicate that compounds of Formula I possess cognition and memory enhancing activity.
    Type: Grant
    Filed: August 28, 1987
    Date of Patent: May 2, 1989
    Assignee: Bristol-Myers
    Inventors: Ronald J. Mattson, Joseph P. Yevich, Michael S. Eison
  • Patent number: 4816585
    Abstract: Tetraalkylpiperidinyl substituted uracil derivatives are disclosed which can be represented by the formula ##STR1## wherein each R' is independently an alkyl radical, n is 1 or 2 and R is a substituted or unsubstituted aliphatic radical, cycloaliphatic radical, aromatic radical or aromatic-aliphatic radical.These derivatives are useful as UV light stabilizers in synthetic resins.
    Type: Grant
    Filed: October 2, 1987
    Date of Patent: March 28, 1989
    Assignee: Olin Corporation
    Inventors: Robert J. Raynor, Francis W. Migliaro, Jr.
  • Patent number: 4812164
    Abstract: The invention is concerned with novel C.sub.1-4 -alkyl, C.sub.2-4 -alkenyl and C.sub.3 or 4 -alkynyl enol ethers of 3-aryluracils of the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and X are as defined in the specification, their manufacture, weed control compositions which contain such enol ethers as the active substance and the use of the active substances or compositions for the control of weeds. The invention is also concerned with certain novel intermediates, some of which possess herbicidal activity, and with weed control compositions containing such active substances.
    Type: Grant
    Filed: September 15, 1987
    Date of Patent: March 14, 1989
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Jean Wenger, Paul Winternitz
  • Patent number: 4798893
    Abstract: A method for the synthesis of the 2-propanone (I) is described starting from alkoxide (II) through the lactone (IV). ##STR1## Excellent control of the location of the substitution on the phenyl ring is achieved and the reaction proceeds in high yield.
    Type: Grant
    Filed: September 21, 1987
    Date of Patent: January 17, 1989
    Assignee: McNeilab, Inc.
    Inventors: David A. Cherry, Cynthia A. Maryanoff, John E. Mills, Roy A. Olofson, James D. Rodgers
  • Patent number: 4781863
    Abstract: Acylated aminocarnitines have utility as competitive inhibitors of carnitine acyl transferases and the unacylated compounds have utility as intermediates for making the acylated compounds.
    Type: Grant
    Filed: September 21, 1987
    Date of Patent: November 1, 1988
    Assignee: Cornell Research Foundation, Inc.
    Inventors: Owen W. Griffith, Deborah L. Jenkins
  • Patent number: 4771061
    Abstract: This disclosure describes certain substituted piperazine-1,4-naphthalenediones useful as anti-asthmatic agents.
    Type: Grant
    Filed: May 6, 1987
    Date of Patent: September 13, 1988
    Assignee: American Cyanamid Company
    Inventors: Jeffrey B. Medwid, Lawrence W. Torley, Andrew S. Tomcufcik
  • Patent number: 4770691
    Abstract: As new compounds are provided 2-(4',6'-di-substituted pyrimidine-2'-yl)oxy- or thio-benzoic acid derivatives of the formula ##STR1## wherein R is hydrogen, hydroxy, alkoxy, alkenyloxy, alkylthio or other substituents, R.sup.1 and R.sup.2 are each a halo, alkyl, alkoxy or other substituents; and X is oxygen or sulfur atom. These new compounds are useful as herbicidal agent effective to inhibit the growth of annual weeds and also perennial weeds predominant in irrigated fields of aquatic rice plants and in plowed fields.
    Type: Grant
    Filed: October 15, 1986
    Date of Patent: September 13, 1988
    Assignees: Kumiai Chemical Industry Co., Ltd., Ihara Chemical Industry Co., Ltd.
    Inventors: Yukio Nezu, Kazuhiko Sugiyama, Shoji Kusano, Yasufumi Toyokawa, Takeshige Miyazawa, Ikuo Kajiwara
  • Patent number: 4769060
    Abstract: The invention relates to certain sulfonylurea compounds having an ester group ortho to the sulfonylurea linkage which have been found to be excellent preemergent and postemergent herbicides or plant growth regulators.
    Type: Grant
    Filed: February 18, 1987
    Date of Patent: September 6, 1988
    Assignee: E. I. Du Pont de Nemours and Company
    Inventor: Donald J. Dumas
  • Patent number: 4765824
    Abstract: A pyrimidyl-thio-carboxanilide of the formula (I), ##STR1## in which R.sup.1 represents hydrogen or halogen, alkyl, alkoxy or alkylthio having 1 to 6 carbon atoms in each case, trifluoromethyl, or phenyl which is unsubstituted or mono- or poly-substituted, identically or differently, by halogen, methyl, ethyl, methoxy or trifluoromethyl,R.sup.2 represents hydrogen, halogen, alkyl having 1 to 6 carbon atoms or trifluoromethyl,R.sup.3 represents halogen, methyl or methoxy,n represents an integer 0, 1 or 2, andZ represents the radical ##STR2## where X represents oxygen or sulphur,R.sup.4 represents hydrogen or hydroxyl, alkyl or alkoxy having 1 to 6 carbon atoms in each case, alkenyl or alkynyl having 3 to 6 carbon atoms in each case, with the proviso that R.sup.4 does not represent hydrogen when X represents oxygen,R.sup.5 represents hydrogen, halogen or alkyl having 1 to 6 carbon atoms which is unsubstituted or mono- or poly-substituted by halogen orR.sup.4 and R.sup.
    Type: Grant
    Filed: November 21, 1986
    Date of Patent: August 23, 1988
    Assignee: Bayer Aktiengesellschaft
    Inventors: Klaus Sasse, Reiner Fischer, Hermann Hagemann, Hans-Joachim Santel, Robert R. Schmidt, Robert H. Strang
  • Patent number: 4762848
    Abstract: Heterocyclic sulfides of the general formula heterocycle-S-R, a process for their preparation and, in particular, their use for immunostimulation, immunorestoration and cytostatic treatment, and pharmaceutical agents, which contain a sulfide of this type, for these indications.
    Type: Grant
    Filed: March 10, 1986
    Date of Patent: August 9, 1988
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Karl-Heinz Scheunemann, Walter Durckheimer, Jurgen Blumbach, Michael Limbert, Hans-Ulrich Schorlemmer, Gerhard Dickneite, Hans-Harald Sedlacek
  • Patent number: 4760163
    Abstract: The disclosure is concerned with novel 3-aryluracils of the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and X have the significances given in the description, as well as salts thereof and their manufacture, weed control compositions which contain such compounds as active ingredients and the use of the active ingredients or compositions for the control of weeds. The disclosure also concerns certain herbicidally active starting materials and weed control compositions containing these as active ingredients.
    Type: Grant
    Filed: January 25, 1988
    Date of Patent: July 26, 1988
    Assignee: Hoffmann-LaRoche Inc.
    Inventors: Jean Wenger, Paul Winternitz
  • Patent number: 4747866
    Abstract: A pirimidinyloxyalkanamide derivative of Formula 1: ##STR1## wherein R.sub.1 represents a hydrogen atom, a halogen atom, a lower alkyl group, a lower alkylthio group, a lower alkenylthio group, a lower alkynylthio group, a halogenated lower alkenylthio group, a cycloalkylthio group, an aroxyalkylthio group, a lower alkoxyl group, an amino group, a methanesulfonyl group, a trifluoromethyl group, an anilino group which may be substituted with a halogen atom or a benzylthio group which may be substituted with a halogen atom; R.sub.2 represents a hydrogen atom, a halogen atom, a lower alkyl group, a trifluoromethyl group, an amino group, a lower alkoxy group or a lower alkylthio group; R.sub.3 represents an ethyl group or an n-propyl group; and R.sub.
    Type: Grant
    Filed: August 15, 1986
    Date of Patent: May 31, 1988
    Assignee: Ube Industries, Ltd.
    Inventors: Tetsuo Takematsu, Yasutomo Takeuchi, Mitsuaki Takenaka, Seiji Takamura, Hiroshi Hase
  • Patent number: 4748245
    Abstract: A process for the preparation of phenylthiopyrimidines which comprises: (a) reacting a thiopyrimidine; with sulfuryl chloride in the presence of a suitable solvent to form the sulfenyl chloride of said thiopyrimidine; (b) reacting said sulfenyl chloride of said thiopyrimidine with a phenol or substituted phenol, optionally in the presence of a Friedal-Crafts catalyst, to form a thiopyrimidinyl phenol; and (c) reacting said thiopyrimidinylphenol formed in step (b) with a base and an alkylating agent to form the end product.
    Type: Grant
    Filed: March 20, 1986
    Date of Patent: May 31, 1988
    Assignee: Stauffer Chemical Company
    Inventor: Donald R. James
  • Patent number: 4746664
    Abstract: New pyrimidine derivatives of the formula: ##STR1## wherein Z is a group selected from ##STR2## in which R.sup.1 and R.sup.2 are each hydrogen, alkenyl, ar(lower)alkyl or lower alkyl optionally substituted with epoxy, hydroxy, amino and/or lower alkylamino and R.sup.5 is lower alkyl,R.sup.3 is hydrogen, aryl optionally substituted with lower alkyl, lower alkoxy and/or halogen, or pyridyl optionally substituted with lower alkyl,R.sup.4 is hydrogen, lower alkyl or phenyl optionally substituted with lower alkoxy, andY is .dbd.O, .dbd.S or .dbd.N--R.sup.6, in which R.sup.6 is lower alkyl; cyclo(lower)alkyl; ar(lower)alkyl optionally substituted with lower alkoxy; N-containing unsaturated heterocyclic group optionally substituted with lower alkyl; or aryl optionally substituted with hydroxy, lower alkyl, halogen or lower alkoxy, in which lower alkoxy substituent may be substituted with epoxy, hydroxy, amino and/or lower alkylamino,provided that Y is .dbd.N--R.sup.6 when R.sup.3 and R.sup.
    Type: Grant
    Filed: June 5, 1986
    Date of Patent: May 24, 1988
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Takao Takaya, Masayoshi Murata, Kiyotaka Ito
  • Patent number: 4746352
    Abstract: The disclosure is concerned with novel 3-aryluracils of the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and X have the significances given in the description, as well as salts thereof and their manufacture, weed control compositions which contain such compounds as active ingredients and the use of the active ingredients or compositions for the control of weeds. The disclosure also concerns certain herbicidally active starting materials and weed control compositions containing these as active ingredients.
    Type: Grant
    Filed: March 10, 1986
    Date of Patent: May 24, 1988
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Jean Wenger, Paul Winternitz
  • Patent number: 4737518
    Abstract: Novel lipid derivatives of the formula ##STR1## [wherein R.sup.1 is alkyl or alkylcarbamoyl; R.sup.2 is hydrogen, hydroxy which may be substituted, amino which may be substituted or cyclic amino; R.sup.3 is a chemical binding or alkylene which may be substituted; R.sup.4 is hydrogen, alkyl or aralkyl; X and Y are independently O, S or an imino group which may be substituted, and when Y is an imino group, Y, together with the imino group represented by X or R.sup.4, may form a ring; and Z is imino or a nitrogen-containing heterocyclic ring which may be substituted] and salts thereof have inhibiting activity on platelet activating factor and are useful as a preventive or therapeutic agent for a variety of circulatory diseases and allergic disorders and also as an antineoplastic agent.
    Type: Grant
    Filed: September 12, 1986
    Date of Patent: April 12, 1988
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Hiroaki Nomura, Kohei Nishikawa, Susumu Tsushima, Yoshio Kozai
  • Patent number: 4730001
    Abstract: There are disclosed compounds represented by Formulas I-III: ##STR1## wherein X is an azido group or an amino group and R is hydrogen or an acyl group. These compounds are useful for the treatment of viral infections and/or as intermediates in the production of compounds which are useful in the treatment of viral infections.
    Type: Grant
    Filed: January 22, 1986
    Date of Patent: March 8, 1988
    Assignee: Southern Research Institute
    Inventors: Y. Fulmer Shealy, C. Allen O'Dell
  • Patent number: 4721717
    Abstract: The present invention provides aminoalcohols of the general formula: ##STR1## wherein R.sub.1 and R.sub.2, which can be same or different, are hydrogen atoms, hydroxyl groups, C.sub.1 -C.sub.4 -alkoxy, benzyloxy, C.sub.1 -C.sub.4 -alkoxycarbonyl, C.sub.1 -C.sub.4 -alkanesulphonylamino, C.sub.1 -C.sub.4 -alkanesulphinyl or C.sub.1 -C.sub.4 -alkanesulphonyl radicals, m is 2, 3 or 4, X and Y, which can be the same or different, are hydrogen atoms or benzyl radicals and R.sub.3 is a phenyl radical substituted twice by C.sub.1 -C.sub.6 -alkyl radicals, a nitrophenyl radical, an aminophenyl radical, a 1,3,5-tri-C.sub.1 -C.sub.6 -alkyl-2,4-dioxo-1H,3H-pyrimidin-6-yl radical, an indolyl radical, an indazolyl radical, a benzimidazolyl radical, a 1,4-di-C.sub.1 -C.sub.6 -alkylpyrazol-5-yl radical or a radical of the general formula: ##STR2## wherein R.sub.4 and R.sub.5, which can be the same or different, are C.sub.1 -C.sub.4 -alkyl radicals and R.sub.6 is a C.sub.1 -C.sub.6 -alkyl, C.sub.2 -C.sub.
    Type: Grant
    Filed: July 29, 1985
    Date of Patent: January 26, 1988
    Assignee: Boehringer Mannheim GmbH
    Inventors: Walter-Gunar Friebe, Wolfgang Kampe, Erwin Bohm, Klaus Strein
  • Patent number: 4713313
    Abstract: Compounds which include a quaternary group connected to a pyrimidine residue through a linkage are disclosed. These compounds are useful as silver halide solvents in photographic products, processes and compositions.
    Type: Grant
    Filed: May 2, 1984
    Date of Patent: December 15, 1987
    Assignee: Polaroid Corporation
    Inventors: James R. Bartels-Keith, deceased, Anthony J. Puttick, Lloyd D. Taylor
  • Patent number: 4686220
    Abstract: This disclosure describes certain substituted piperazine-1,4-naphthalenediones useful as anti-asthmatic agents.
    Type: Grant
    Filed: December 19, 1985
    Date of Patent: August 11, 1987
    Assignee: American Cyanamid Company
    Inventors: Jeffrey B. Medwid, Lawrence W. Torley, Andrew S. Tomcufcik
  • Patent number: 4681884
    Abstract: Compounds of the formula ##STR1## wherein R.sub.1 is hydrogen or alkyl of 1 to 4 carbon atoms;R.sub.2 is hydrogen, methyl, hydroxyl, alkoxy of 1 to 4 carbon atoms, di(alkyl of 1 to 2 carbon atoms)amino-(alkoxy of 1 to 4 carbon atoms) or NHCOCOOR.sub.1 ;R.sub.3 is hydrogen or NHCOCOOR.sub.1 ;A is ##STR2## R.sub.4 is hydrogen, methyl, alkoxy of 1 to 4 carbon atoms, hydroxyl, amino, alkanoyloxy of 1 to 2 carbon atoms, di(alkyl of 1 to 2 carbon atoms)-amino-(alkoxy of 1 to 4 carbon atoms) or acetamido; andR.sub.5 is hydrogen, amino, alkoxy of 1 to 4 carbon atoms, halogen or NHCOCOOR.sub.1 ;and, when R.sub.1 is hydrogen, nontoxic, pharmaceutically acceptable salts thereof. The compounds as well as their salts are useful for the treatment of immunological, inflammatory and allergic disorders such as asthma, rhinitis, conjunctivitis, hay fever, urticaria, food allergies and the like.
    Type: Grant
    Filed: May 10, 1985
    Date of Patent: July 21, 1987
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Karl G. Grozinger, James T. Oliver
  • Patent number: 4661147
    Abstract: The invention relates to certain sulfonylurea compounds having an ester group ortho to the sulfonylurea linkage which have been found to be excellent preemergent and postemergent herbicides or plant growth regulators.
    Type: Grant
    Filed: April 29, 1985
    Date of Patent: April 28, 1987
    Assignee: E. I. Du Pont de Nemours and Company
    Inventor: Donald J. Dumas
  • Patent number: 4659502
    Abstract: Ethane derivatives of the formula IR.sup.1 --A.sup.1 --CH.sub.2 CH.sub.2 --A.sup.2 --(A.sup.3).sub.n --R.sup.2 IwhereinR.sup.1 is H, an alkyl group with 1-12 C atoms, in which one or two non adjacent CH.sub.2 groups can also be replaced by O atoms and/or CO groups and/or --O--CO-- groups and/or --CO--O groups, F, Cl, Br or R.sup.3 --A.sup.4 --Z.sup.1 --,R.sup.2 is --CN or --Z.sup.2 --A.sup.4 --CN,A.sup.1 is --A--, --A--A.sup.5 -- or --A.sup.5 --A--,A.sup.2 is an 1,4-phenylene group which is unsubstituted or substituted by one or two F and/or Cl atoms and/or CH.sub.3 groups and/or CN groups and in which one or two CH groups can also be replaced by N atoms,A is a 1,4-cyclohexylene group, in which one or two non adjacent CH.sub.2 groups can also be replaced by O atoms, or is a 1,3-dithiane-2,5-diyl group or 1,4-bicyclo(2,2,2)-octylene group,A.sup.3, A.sub.4 are each a 1,4-cyclohexylene group, in which one or two non adjacent CH.sub.
    Type: Grant
    Filed: January 17, 1985
    Date of Patent: April 21, 1987
    Assignee: Merck Patent Gesellschaft mit Beschrankter Haftung
    Inventors: Julie E. Fearon, Wendy E. Smith, George W. Gray, David Lacey, Kenneth J. Toyne, Georg Weber
  • Patent number: 4629496
    Abstract: N-(heterocycliccarbamoyl)arylsulfonamides, such as N-[(4,6-dimethoxypyrimidin-2-yl)aminocarbonyl]-2-hydroxybenzenesulfonamide , methanesulfonate are useful for plant growth retardation, brush control and weed control in crops.
    Type: Grant
    Filed: May 3, 1985
    Date of Patent: December 16, 1986
    Assignee: E. I. Du Pont de Nemours and Company
    Inventor: James J. Reap
  • Patent number: 4625028
    Abstract: This invention relates to selected hydrogenated 5,6-dihydro-6-aryluracils.
    Type: Grant
    Filed: July 11, 1983
    Date of Patent: November 25, 1986
    Assignee: The Upjohn Company
    Inventor: Herman W. Smith
  • Patent number: 4612375
    Abstract: Substituted triazolo[4,3-c]pyrimidines which are bronchodilators. The pharmacological use of these compounds, pharmaceutical compositions containing these compounds, and synthetic intermediates for the preparation of these compounds are also described.
    Type: Grant
    Filed: May 8, 1985
    Date of Patent: September 16, 1986
    Assignee: Riker Laboratories, Inc.
    Inventor: James J. Wade
  • Patent number: 4608383
    Abstract: The present invention provides aryloxypropanolamines of the general formula: ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4, which may be the same or different, are hydrogen or halogen atoms or lower alkyl, cyano, carboxamide, hydroxyl, lower acyloxy, lower alkoxy, lower alkenyloxy or aryl lower alkoxy radicals, R.sub.5 and R.sub.6, which may be the same or different, are hydrogen atoms or lower alkyl radicals, X is a straight or branched alkylene chain containing 2 to 6 carbon atoms, A is a mono-, bi- or tricyclic heteroaromatic or hydroheteroaromatic radical or, when at least one of the symbols R.sub.1, R.sub.2, R.sub.3 and R.sub.4 is other than a hydrogen atom, may also be a phenyl radical, with the proviso that when A is a uracil-6-yl radical, the 5-position of the uracil moiety does not contain a hydrogen atom, R.sub.7, R.sub.8, R.sub.9, R.sub.10 and R.sub.
    Type: Grant
    Filed: October 3, 1983
    Date of Patent: August 26, 1986
    Assignee: Boehringer Mannheim GmbH
    Inventors: Fritz Wiedemann, deceased, Wolfgang Kampe, Karl Dietmann, deceased, Gisbert Sponer
  • Patent number: 4604466
    Abstract: Piperidino-substituted pyrimidines which are intermediates for preparing piperidino-substituted imidazo-[1,5-c]pyrimidines which are bronchodilators.
    Type: Grant
    Filed: August 16, 1984
    Date of Patent: August 5, 1986
    Assignee: Riker Laboratories, Inc.
    Inventor: James J. Wade
  • Patent number: 4596869
    Abstract: A novel compound, useful as an intermediate in the production of compounds of high antimicrobial activity, of the formula: ##STR1## wherein R.sub.a.sup.1 is hydrogen, amino or a protected amino group,R.sub.b.sup.1 and R.sub.c.sup.1 are each hydrogen, halogen, lower alkoxy or arylthio,R.sup.14 is carboxy or a protected carboxy group,X is lower alkylene or a group of the formula: ##STR2## in which R.sup.6 is hydrogen or an organic residue which may have suitable substituent(s), andZ is N or CH,or a salt thereof.
    Type: Grant
    Filed: September 19, 1985
    Date of Patent: June 24, 1986
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Takashi Kamiya, Tsutomu Teraji, Yoshiharu Nakai, Kazuo Sakane, Jiro Goto
  • Patent number: 4595539
    Abstract: Certain 2-substituted-2-penem-3-carboxylic acid compounds and pharmaceutically-acceptable salts thereof can be prepared from the appropriate xanthate or trithiocarbonate by desulfurization and addition of an electrophilic sulfur compound followed by halogenation and ring closure. The corresponding desulfurized and halogenated olefinic intermediates are disclosed.
    Type: Grant
    Filed: June 10, 1983
    Date of Patent: June 17, 1986
    Assignee: Pfizer Inc.
    Inventor: Ernest S. Hamanaka
  • Patent number: 4590189
    Abstract: The compound of the formula ##STR1## wherein X is a cyclic group which may optionally be substituted; Y is a carboxyl group which may optionally be esterified or amidated; Z is --CH.dbd.CH--CH.dbd.CH--, --S--(CH.sub.2).sub.l --S--(l is an integer of 1 to 3), --N.dbd.CH--CH.dbd.N-- or --(CH.sub.2).sub.m --(m is an integer of 3 to 5); ring A may optionally be substituted with halogen, nitro, amino, alkanoylamino, alkoxycarbonyl, carboxyl or carbamoyl; and n is an integer of 1 to 3, and salts thereof. The compounds display a strong antianxiety effect to mammalian animals and are useful for the prevention or treatment of a disease such as psychosomatic disease and anxiety neurosis.
    Type: Grant
    Filed: March 24, 1983
    Date of Patent: May 20, 1986
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Kentaro Hiraga, Yoshiaki Saji
  • Patent number: 4587051
    Abstract: A compound having the formula ##STR1## can be prepared by heating an anion having the formula ##STR2## with a cation having the formula ##STR3## or a cation having the formula ##STR4##
    Type: Grant
    Filed: May 21, 1984
    Date of Patent: May 6, 1986
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: William H. Koster
  • Patent number: 4587047
    Abstract: Antibacterial activity is exhibited by .beta.-lactams having a ##STR1## substituent in the 1-position and an acylamino substituent in the 3-position wherein Z is oxygen or sulfur, and R is alkyl, alkenyl, alkynyl, substituted alkyl, phenyl, substituted phenyl, a 5,6 or 7-membered heterocycle (R.sub.c), phenylalkyl, (substituted phenyl)alkyl, R.sub.c -alkyl or --NR.sub.a R.sub.b wherein R.sub.a and R.sub.b are the same or different and each is hydrogen, alkyl, substituted alkyl, phenyl, substituted phenyl, phenylalkyl, or (substituted phenyl)alkyl or one of R.sub.a and R.sub.b is hydrogen, alkyl, phenyl, substituted phenyl, phenylalkyl or (substituted phenyl)alkyl and the other is amino, alkanoylamino, arylcarbonylamino, alkoxycarbonylamino, alkylsulfonylamino, alkylamino, dialkylamino, phenylamino, (substituted phenyl)amino, hydroxy, cyano, alkoxy, phenyloxy, (substituted phenyl)oxy, phenylalkoxy, (substituted phenyl)alkoxy, R.sub.c, R.sub.c -alkyl, R.sub.
    Type: Grant
    Filed: April 1, 1982
    Date of Patent: May 6, 1986
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Hermann Breuer, William A. Slusarchyk, Theodor Denzel, Uwe D. Treuner
  • Patent number: 4576948
    Abstract: New uracil compounds having the formula: ##STR1## wherein X is C.sub.1 -C.sub.10 alkoxy or amino are provided. These compounds are useful in treating patients having leukemia, the cells of which express terminal deoxynucleootidyl transferase.
    Type: Grant
    Filed: January 20, 1983
    Date of Patent: March 18, 1986
    Assignee: Trustees Boston University
    Inventors: Ronald McCaffrey, George Wright, Earl F. Baril
  • Patent number: 4576749
    Abstract: Antibacterial activity is exhibited by 2-azetidinones having a 3-acylamino substituent and a 1-substituent of the formula ##STR1## (or a salt or ester thereof).
    Type: Grant
    Filed: April 13, 1984
    Date of Patent: March 18, 1986
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Robert Zahler, William H. Koster, William A. Slusarchyk
  • Patent number: 4559345
    Abstract: Pyrimidine and s-triazine derivatives of formula (I) ##STR1## in which X=CH or N; Y=for example halogen, alkoxy; W=for example --S--CH.sub.2 --COOH, --O--CH.sub.2 --COO alkyl, --NH--CH.sub.2 --CONHCH.sub.2 CH.sub.2 OH; Z=for example 2,3-xylidino, and methods for the preparation thereof are described. The compounds show high antilipemic activity.
    Type: Grant
    Filed: July 21, 1982
    Date of Patent: December 17, 1985
    Assignee: LBP Istituto Faraceutico S.p.A.
    Inventors: Piero Gomarasca, Carlo Scolastico, Cesare Sirtori
  • Patent number: 4535083
    Abstract: The invention relates to compounds of the formula ##STR1## said compounds being obtainable by cleavage of compounds of formula ##STR2## The compounds of the invention as well as compositions and medicaments containing a compound of the invention are useful as antimicrobial agents.
    Type: Grant
    Filed: September 9, 1983
    Date of Patent: August 13, 1985
    Assignee: Bayer Aktiengesellschaft
    Inventors: Gunter Benz, Karl G. Metzger, Hans-Joachim Zeiler
  • Patent number: 4514403
    Abstract: A hydrouracil compound of the formula: ##STR1## or a pharmaceutically acceptable acid addition salt thereof, wherein A represents --CH.dbd.CH--CH.sub.2 -- or --CH.sub.2 CH.sub.2 --, and R represents hydrogen or methyl. Such compounds are useful as analgesics.
    Type: Grant
    Filed: September 17, 1981
    Date of Patent: April 30, 1985
    Assignee: Yoshitomi Pharmaceutical Industries Ltd.
    Inventors: Chiaki Tashiro, Takeshi Kawakita, Ichiro Horii, Koretake Anami
  • Patent number: 4474601
    Abstract: This invention relates to N-(heterocyclicaminocarbonyl)-o-alkenylbenzenesulfonamides which are useful as agricultural chemicals.
    Type: Grant
    Filed: September 27, 1982
    Date of Patent: October 2, 1984
    Assignee: E. I. Du Pont de Nemours and Company
    Inventors: Chi-wan Chen, Gregory W. Schwing
  • Patent number: 4473394
    Abstract: This invention relates to pyrrole sulfonamides which are useful as herbicides. Typical of the pyrrole sulfonamides of the instant application in N-[(4-methoxy-6-methyl-1,3,5-triazin-2-yl)aminocarbonyl]-2,5-dimethyl-1H-p yrrole-3-sulfonamide.
    Type: Grant
    Filed: September 27, 1982
    Date of Patent: September 25, 1984
    Assignee: E. I. DuPont De Nemours & Company
    Inventors: John C. Budzinski, George Levitt
  • Patent number: 4473570
    Abstract: Imidazo[1,5-c]pyrimidin-5-ones have been found to have potent bronchodilator activity. Pharmacological methods of using these compounds and pharmaceutical compositions containing these compounds are also disclosed.
    Type: Grant
    Filed: August 2, 1983
    Date of Patent: September 25, 1984
    Assignee: Riker Laboratories, Inc.
    Inventor: James J. Wade
  • Patent number: 4461640
    Abstract: Alkenylsulfonylureas have been found to be effective as herbicides and plant growth regulants.
    Type: Grant
    Filed: June 2, 1982
    Date of Patent: July 24, 1984
    Assignee: E. I. Du Pont de Nemours and Company
    Inventors: George Levitt, William T. Zimmerman
  • Patent number: 4460588
    Abstract: The invention concerns a process for killing internal parasites, especially trematodes or nematodes, affecting warm blooded animals such as cattle, sheep and goats by administering an effective amount of a composition containing as active ingredient a compound of the formula ##STR1## Certain of the compounds of formula I are novel and in further embodiments the invention provides novel compounds and compositions for use in the process of the invention. The process of the invention is especially applicable to the tretment of warm blooded animals infected with the trematodes Fasciola hepatica (liver fluke).
    Type: Grant
    Filed: February 5, 1980
    Date of Patent: July 17, 1984
    Assignee: ICI Australia Limited
    Inventors: Alexander Serban, Keith G. Watson, Colin Wilshire, Bruce A. Forsyth
  • Patent number: 4455424
    Abstract: The present invention relates to naphthoquinone derivatives of formula I, ##STR1## in which R.sub.1 signifies a halogen atom, a nitro group or an unsubstituted or substituted alkoxy or amino group,R.sub.2 signifies the atoms necessary to form an unsaturated ring system, which ring system has 1 or 2 nuclei and is unsubstituted or substituted,R.sub.3 signifies an unsubstituted or substituted s-triazinyl or pyrimidyl radical, andn is 0, 1 or 2,which compounds are free from sulphonic acid groups are useful as pigments or disperse dyes.
    Type: Grant
    Filed: February 24, 1977
    Date of Patent: June 19, 1984
    Assignee: Sandoz Ltd.
    Inventor: Bansi L. Kaul
  • Patent number: 4448961
    Abstract: Novel 1-substituted pyrimidinediones and thiopyrimidineones, synthesis thereof and intermediates therefor, useful as control agents for pests.
    Type: Grant
    Filed: May 27, 1982
    Date of Patent: May 15, 1984
    Assignee: Zoecon Corporation
    Inventors: George R. Lindahl, III, Clive A. Henrick
  • Patent number: 4438128
    Abstract: The present invention provides aryloxypropanolamines of the general formula: ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4, which may be the same or different, are hydrogen or halogen atoms or lower alkyl, cyano, carboxamido, hydroxyl, lower acyloxy, lower alkoxy, lower alkenyloxy or aryl lower alkoxy radicals, R.sub.5 and R.sub.6, which may be the same or different, are hydrogen atoms or lower alkyl radicals, X is a straight or branched alkylene chain containing 2 to 6 carbon atoms, A is a mono-, bi- or tricyclic heteroaromatic or hydroheteroaromatic radical or, when at least one of the symbols R.sub.1, R.sub.2, R.sub.3 and R.sub.4 is other than a hydrogen atom, may also be a phenyl radical, with the proviso that when A is a uracil-6-yl radical, the 5-position of the uracil moiety does not contain a hydrogen atom, R.sub.7, R.sub.8, R.sub.9, R.sub.10 and R.sub.
    Type: Grant
    Filed: June 15, 1981
    Date of Patent: March 20, 1984
    Assignee: Boehringer Mannheim GmbH
    Inventors: Fritz Wiedemann, Wolfgang Kampe, Karl Dietmann, Gisbert Sponer
  • Patent number: 4435205
    Abstract: N-(Heterocycliccarbamoyl)arylsulfonamides, such as N-[(4,6-dimethoxypyrimidin-2-yl)aminocarbonyl]-2-hydroxybenzenesulfonamide , methanesulfonate are useful for plant growth retardation, brush control and weed control in crops.
    Type: Grant
    Filed: April 15, 1982
    Date of Patent: March 6, 1984
    Assignee: E. I. Du Pont de Nemours and Company
    Inventor: James J. Reap
  • Patent number: 4427437
    Abstract: A process of inhibiting the growth of, severely damaging, or killing plants which process comprises applying to the plant or to the growth medium thereof an effective amount of a composition comprising as active ingredient a compound of formula I: ##STR1## wherein A, B and D are independently chosen from the group consisting of hydrogen, halogen, hydroxy, nitro, cyano, thiocyano, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkoxy, optionally substituted alkenyloxy, optionally substituted alkynyloxy, optionally substituted alkylthio, optionally substituted cycloalkyl, optionally substituted amino, optionally substituted phenyl, carboxy, alkoxycarbonyl, optionally substituted carbamoyl, sulfo, alkylsulfonyl and optionally substituted sulfamoyl; R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.
    Type: Grant
    Filed: September 5, 1978
    Date of Patent: January 24, 1984
    Assignee: ICI Australia Limited
    Inventors: Alexander Serban, Keith G. Watson, Richard B. Warner