5-position Is Unsubstituted Or Alkyl Substituted Only Patents (Class 544/312)
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Patent number: 4871387Abstract: 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: GrantFiled: December 4, 1986Date of Patent: October 3, 1989Assignee: Bayer AktiengesellschaftInventors: Klaus Sasse, Reiner Fischer, Hermann Hagemann, Hans-Joachim Santel, Robert R. Schmidt, Kalus Lurssen
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Patent number: 4851030Abstract: 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: GrantFiled: December 8, 1986Date of Patent: July 25, 1989Assignee: E. I. Du Pont de Nemours and CompanyInventor: Morris P. Rorer
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Patent number: 4826843Abstract: 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: GrantFiled: August 28, 1987Date of Patent: May 2, 1989Assignee: Bristol-MyersInventors: Ronald J. Mattson, Joseph P. Yevich, Michael S. Eison
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Patent number: 4816585Abstract: 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: GrantFiled: October 2, 1987Date of Patent: March 28, 1989Assignee: Olin CorporationInventors: Robert J. Raynor, Francis W. Migliaro, Jr.
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Patent number: 4812164Abstract: 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: GrantFiled: September 15, 1987Date of Patent: March 14, 1989Assignee: Hoffmann-La Roche Inc.Inventors: Jean Wenger, Paul Winternitz
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Patent number: 4798893Abstract: 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: GrantFiled: September 21, 1987Date of Patent: January 17, 1989Assignee: McNeilab, Inc.Inventors: David A. Cherry, Cynthia A. Maryanoff, John E. Mills, Roy A. Olofson, James D. Rodgers
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Patent number: 4781863Abstract: 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: GrantFiled: September 21, 1987Date of Patent: November 1, 1988Assignee: Cornell Research Foundation, Inc.Inventors: Owen W. Griffith, Deborah L. Jenkins
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Patent number: 4771061Abstract: This disclosure describes certain substituted piperazine-1,4-naphthalenediones useful as anti-asthmatic agents.Type: GrantFiled: May 6, 1987Date of Patent: September 13, 1988Assignee: American Cyanamid CompanyInventors: Jeffrey B. Medwid, Lawrence W. Torley, Andrew S. Tomcufcik
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Patent number: 4770691Abstract: 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: GrantFiled: October 15, 1986Date of Patent: September 13, 1988Assignees: Kumiai Chemical Industry Co., Ltd., Ihara Chemical Industry Co., Ltd.Inventors: Yukio Nezu, Kazuhiko Sugiyama, Shoji Kusano, Yasufumi Toyokawa, Takeshige Miyazawa, Ikuo Kajiwara
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Patent number: 4769060Abstract: 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: GrantFiled: February 18, 1987Date of Patent: September 6, 1988Assignee: E. I. Du Pont de Nemours and CompanyInventor: Donald J. Dumas
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Patent number: 4765824Abstract: 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: GrantFiled: November 21, 1986Date of Patent: August 23, 1988Assignee: Bayer AktiengesellschaftInventors: Klaus Sasse, Reiner Fischer, Hermann Hagemann, Hans-Joachim Santel, Robert R. Schmidt, Robert H. Strang
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Patent number: 4762848Abstract: 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: GrantFiled: March 10, 1986Date of Patent: August 9, 1988Assignee: Hoechst AktiengesellschaftInventors: Karl-Heinz Scheunemann, Walter Durckheimer, Jurgen Blumbach, Michael Limbert, Hans-Ulrich Schorlemmer, Gerhard Dickneite, Hans-Harald Sedlacek
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Patent number: 4760163Abstract: 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: GrantFiled: January 25, 1988Date of Patent: July 26, 1988Assignee: Hoffmann-LaRoche Inc.Inventors: Jean Wenger, Paul Winternitz
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Patent number: 4747866Abstract: 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: GrantFiled: August 15, 1986Date of Patent: May 31, 1988Assignee: Ube Industries, Ltd.Inventors: Tetsuo Takematsu, Yasutomo Takeuchi, Mitsuaki Takenaka, Seiji Takamura, Hiroshi Hase
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Patent number: 4748245Abstract: 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: GrantFiled: March 20, 1986Date of Patent: May 31, 1988Assignee: Stauffer Chemical CompanyInventor: Donald R. James
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Patent number: 4746664Abstract: 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: GrantFiled: June 5, 1986Date of Patent: May 24, 1988Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Takao Takaya, Masayoshi Murata, Kiyotaka Ito
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Patent number: 4746352Abstract: 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: GrantFiled: March 10, 1986Date of Patent: May 24, 1988Assignee: Hoffmann-La Roche Inc.Inventors: Jean Wenger, Paul Winternitz
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Patent number: 4737518Abstract: 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: GrantFiled: September 12, 1986Date of Patent: April 12, 1988Assignee: Takeda Chemical Industries, Ltd.Inventors: Hiroaki Nomura, Kohei Nishikawa, Susumu Tsushima, Yoshio Kozai
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Patent number: 4730001Abstract: 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: GrantFiled: January 22, 1986Date of Patent: March 8, 1988Assignee: Southern Research InstituteInventors: Y. Fulmer Shealy, C. Allen O'Dell
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Patent number: 4721717Abstract: 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: GrantFiled: July 29, 1985Date of Patent: January 26, 1988Assignee: Boehringer Mannheim GmbHInventors: Walter-Gunar Friebe, Wolfgang Kampe, Erwin Bohm, Klaus Strein
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Patent number: 4713313Abstract: 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: GrantFiled: May 2, 1984Date of Patent: December 15, 1987Assignee: Polaroid CorporationInventors: James R. Bartels-Keith, deceased, Anthony J. Puttick, Lloyd D. Taylor
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Patent number: 4686220Abstract: This disclosure describes certain substituted piperazine-1,4-naphthalenediones useful as anti-asthmatic agents.Type: GrantFiled: December 19, 1985Date of Patent: August 11, 1987Assignee: American Cyanamid CompanyInventors: Jeffrey B. Medwid, Lawrence W. Torley, Andrew S. Tomcufcik
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Patent number: 4681884Abstract: 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: GrantFiled: May 10, 1985Date of Patent: July 21, 1987Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Karl G. Grozinger, James T. Oliver
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Patent number: 4661147Abstract: 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: GrantFiled: April 29, 1985Date of Patent: April 28, 1987Assignee: E. I. Du Pont de Nemours and CompanyInventor: Donald J. Dumas
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Patent number: 4659502Abstract: 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: GrantFiled: January 17, 1985Date of Patent: April 21, 1987Assignee: Merck Patent Gesellschaft mit Beschrankter HaftungInventors: Julie E. Fearon, Wendy E. Smith, George W. Gray, David Lacey, Kenneth J. Toyne, Georg Weber
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Patent number: 4629496Abstract: 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: GrantFiled: May 3, 1985Date of Patent: December 16, 1986Assignee: E. I. Du Pont de Nemours and CompanyInventor: James J. Reap
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Patent number: 4625028Abstract: This invention relates to selected hydrogenated 5,6-dihydro-6-aryluracils.Type: GrantFiled: July 11, 1983Date of Patent: November 25, 1986Assignee: The Upjohn CompanyInventor: Herman W. Smith
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Patent number: 4612375Abstract: 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: GrantFiled: May 8, 1985Date of Patent: September 16, 1986Assignee: Riker Laboratories, Inc.Inventor: James J. Wade
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Patent number: 4608383Abstract: 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: GrantFiled: October 3, 1983Date of Patent: August 26, 1986Assignee: Boehringer Mannheim GmbHInventors: Fritz Wiedemann, deceased, Wolfgang Kampe, Karl Dietmann, deceased, Gisbert Sponer
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Patent number: 4604466Abstract: Piperidino-substituted pyrimidines which are intermediates for preparing piperidino-substituted imidazo-[1,5-c]pyrimidines which are bronchodilators.Type: GrantFiled: August 16, 1984Date of Patent: August 5, 1986Assignee: Riker Laboratories, Inc.Inventor: James J. Wade
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Patent number: 4596869Abstract: 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: GrantFiled: September 19, 1985Date of Patent: June 24, 1986Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Takashi Kamiya, Tsutomu Teraji, Yoshiharu Nakai, Kazuo Sakane, Jiro Goto
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Patent number: 4595539Abstract: 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: GrantFiled: June 10, 1983Date of Patent: June 17, 1986Assignee: Pfizer Inc.Inventor: Ernest S. Hamanaka
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Patent number: 4590189Abstract: 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: GrantFiled: March 24, 1983Date of Patent: May 20, 1986Assignee: Takeda Chemical Industries, Ltd.Inventors: Kentaro Hiraga, Yoshiaki Saji
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Patent number: 4587051Abstract: 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: GrantFiled: May 21, 1984Date of Patent: May 6, 1986Assignee: E. R. Squibb & Sons, Inc.Inventor: William H. Koster
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Patent number: 4587047Abstract: 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: GrantFiled: April 1, 1982Date of Patent: May 6, 1986Assignee: E. R. Squibb & Sons, Inc.Inventors: Hermann Breuer, William A. Slusarchyk, Theodor Denzel, Uwe D. Treuner
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Patent number: 4576948Abstract: 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: GrantFiled: January 20, 1983Date of Patent: March 18, 1986Assignee: Trustees Boston UniversityInventors: Ronald McCaffrey, George Wright, Earl F. Baril
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Patent number: 4576749Abstract: 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: GrantFiled: April 13, 1984Date of Patent: March 18, 1986Assignee: E. R. Squibb & Sons, Inc.Inventors: Robert Zahler, William H. Koster, William A. Slusarchyk
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Patent number: 4559345Abstract: 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: GrantFiled: July 21, 1982Date of Patent: December 17, 1985Assignee: LBP Istituto Faraceutico S.p.A.Inventors: Piero Gomarasca, Carlo Scolastico, Cesare Sirtori
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Patent number: 4535083Abstract: 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: GrantFiled: September 9, 1983Date of Patent: August 13, 1985Assignee: Bayer AktiengesellschaftInventors: Gunter Benz, Karl G. Metzger, Hans-Joachim Zeiler
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Patent number: 4514403Abstract: 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: GrantFiled: September 17, 1981Date of Patent: April 30, 1985Assignee: Yoshitomi Pharmaceutical Industries Ltd.Inventors: Chiaki Tashiro, Takeshi Kawakita, Ichiro Horii, Koretake Anami
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Patent number: 4474601Abstract: This invention relates to N-(heterocyclicaminocarbonyl)-o-alkenylbenzenesulfonamides which are useful as agricultural chemicals.Type: GrantFiled: September 27, 1982Date of Patent: October 2, 1984Assignee: E. I. Du Pont de Nemours and CompanyInventors: Chi-wan Chen, Gregory W. Schwing
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Patent number: 4473394Abstract: 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: GrantFiled: September 27, 1982Date of Patent: September 25, 1984Assignee: E. I. DuPont De Nemours & CompanyInventors: John C. Budzinski, George Levitt
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Patent number: 4473570Abstract: 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: GrantFiled: August 2, 1983Date of Patent: September 25, 1984Assignee: Riker Laboratories, Inc.Inventor: James J. Wade
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Patent number: 4461640Abstract: Alkenylsulfonylureas have been found to be effective as herbicides and plant growth regulants.Type: GrantFiled: June 2, 1982Date of Patent: July 24, 1984Assignee: E. I. Du Pont de Nemours and CompanyInventors: George Levitt, William T. Zimmerman
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Patent number: 4460588Abstract: 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: GrantFiled: February 5, 1980Date of Patent: July 17, 1984Assignee: ICI Australia LimitedInventors: Alexander Serban, Keith G. Watson, Colin Wilshire, Bruce A. Forsyth
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Patent number: 4455424Abstract: 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: GrantFiled: February 24, 1977Date of Patent: June 19, 1984Assignee: Sandoz Ltd.Inventor: Bansi L. Kaul
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Patent number: 4448961Abstract: Novel 1-substituted pyrimidinediones and thiopyrimidineones, synthesis thereof and intermediates therefor, useful as control agents for pests.Type: GrantFiled: May 27, 1982Date of Patent: May 15, 1984Assignee: Zoecon CorporationInventors: George R. Lindahl, III, Clive A. Henrick
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Patent number: 4438128Abstract: 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: GrantFiled: June 15, 1981Date of Patent: March 20, 1984Assignee: Boehringer Mannheim GmbHInventors: Fritz Wiedemann, Wolfgang Kampe, Karl Dietmann, Gisbert Sponer
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Patent number: 4435205Abstract: 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: GrantFiled: April 15, 1982Date of Patent: March 6, 1984Assignee: E. I. Du Pont de Nemours and CompanyInventor: James J. Reap
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Patent number: 4427437Abstract: 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: GrantFiled: September 5, 1978Date of Patent: January 24, 1984Assignee: ICI Australia LimitedInventors: Alexander Serban, Keith G. Watson, Richard B. Warner