Additional Hetero Ring Which Is Unsaturated Patents (Class 544/310)
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Patent number: 5563168Abstract: O-Benzyloxime ethers of the formula I ##STR1## where 5 X is substituted or unsubstituted CH.sub.2, NOalkylY isO, S, NR.sup.5R.sup.1, R.sup.2, R.sup.5 are H, alkylZ.sup.1, Z.sup.2 are H, halogen, methyl, methoxy, cyanoR.sup.3, R.sup.4 are hydrogen, cyano, substituted or unsubstituted alkyl, alkenyl, cycloalkyl, cycloalkenyl, alkynyl, alkoxy, haloalkoxy, alkylthio, benzylthio, alkylcarbonyl, substituted or unsubstituted phenylcarbonyl, substituted or unsubstituted benzylcarbonyl, alkoxycarbonyl, substituted or unsubstituted phenoxycarbonyl, substituted or unsubstituted benzyloxycarbonyl,N(R.sup.6).sub.2, where R.sup.6 is H, alkyl, substituted or unsubstituted phenyl,--CO--N(R.sup.7).sub.2, where R.sup.Type: GrantFiled: June 16, 1995Date of Patent: October 8, 1996Assignee: BASF AktiengesellschaftInventors: Siegbert Brand, Uwe Kardorff, Reinhard Kirstgen, Bernd Mueller, Klaus Oberdorf, Hubert Sauter, Gisela Lorenz, Eberhard Ammermann, Christoph Kuenast, Albrecht Harreus
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Patent number: 5561128Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.Type: GrantFiled: June 6, 1995Date of Patent: October 1, 1996Assignee: Hoechst-Roussel Pharmaceuticals, Inc.Inventors: Edward J. Glamkowski, Yulin Chiang
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Patent number: 5559081Abstract: Herbicidal sulfonamides of the formula: ##STR1## and salts thereof, where: A represents a substituted or unsubstituted benzene ring, or a 5- or 6-membered substituted or unsubstituted heteroaromatic ring; Q is --O--, --S-- or a group --CXX'--; X and X', which may be the same or different, are each hydrogen, halogen, cyano, an optionally-substituted alkyl group, or a group --OR.sup.a, --SR.sup.a, or --COR.sup.b ; or one of X and X' represents hydroxy and the other is as defined above; or X and X' together represent .dbd.O or .dbd.S; R.sup.a is an optionally-substituted alkyl, aryl or acyl group; R.sup.b is an optionally-substituted alkyl or aryl group, or a group --OR.sup.c or --NR.sup.c R.sup.d ; R.sup.c and R.sup.d, which may be the same or different, are each hydrogen, or an optionally-substituted alkyl or aryl group; Y is nitrogen or a group CR.sup.9 ; R.sup.1 is an optionally-substituted alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heterocyclyl, benzoheterocyclyl or amino group; R.sup.Type: GrantFiled: May 6, 1994Date of Patent: September 24, 1996Assignee: Agrevo UK LimitedInventors: Peter S. Gates, Graham P. Jones, David E. Saunders
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Patent number: 5527763Abstract: A herbicide containing a pyrimidine or triazine derivative of the formula (I): ##STR1## [wherein A is a furan ring, a pyrimidine ring, a 1,2,4-triazine ring or the like which may suitably be substituted, R is a hydroxyl group or a lower alkoxy group, each of R.sup.1 and R.sup.2 which may be the same or different, is a halogen atom, a lower alkyl group or a lower alkoxy group, W is an oxygen atom or a sulfur atom, and Z is nitrogen or a methine group] and its salt, as an active ingredient, is presented. The pyrimidine or triazine derivative of the present invention has excellent herbicidal effects against noxious weeds in paddy fields, upland fields and non-agricultural fields.Type: GrantFiled: December 8, 1993Date of Patent: June 18, 1996Assignees: Kumiai Chemical Industry Co., Ltd., Ihara Chemical Industry Co., Ltd.Inventors: Masahiro Miyazaki, Masafumi Matsuzawa, Takumi Yoshimura, Kuniaki Shimizu, Shigehiko Tachikawa
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Patent number: 5525724Abstract: A process for the preparation of chloropyrimidines of the formula ##STR1## in which the substituents may be alkyl, cycloalkyl, aryl or radicals containing heteroatoms, but in which at least one of the substituents R.sup.1 to R.sup.4 must be Cl, which involves:reacting a hydroxy-pyrimidine or its tautomeric keto form with phosphoryl chloride in the presence of an amine or amine hydrochloride;recovering phosphoryl chloride after the reaction by adding phosphorus pentachloride and distilling the phosphoryl chloride; andseparating the chloropyrimidine from the amine hydrochloride by addition of a solvent which will dissolve the chloropyrimidine but not the amine hydrochloride and removing the amine hydrochloride.Type: GrantFiled: February 27, 1995Date of Patent: June 11, 1996Assignee: Huels AktiengesellschaftInventor: Artur Hunds
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Patent number: 5523278Abstract: There are provided substituted benzisoxazole and benzisothiazole compounds having the structural formula I ##STR1## Further provided are compositions and methods comprising those compounds for the control of undesirable plant species.Type: GrantFiled: September 12, 1995Date of Patent: June 4, 1996Assignee: American Cyanamid CompanyInventor: Peter J. Wepplo
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Patent number: 5521147Abstract: Herbicidal 3-(benzofuran-7-yl)-6-haloalkyluracils of the formula ##STR1## in which M is fluoroalkyl (C.sub.1-6); D is hydrogen, alkyl (C.sub.1-6), or alkoxy(C.sub.1-6)-carbonyl; E is hydrogen or alkyl (C.sub.1-6), or D and E taken together are --CH.sub.2 CH.sub.2 --; R is hydrogen, amino, alkyl (C.sub.1-6), 2-alkenyl (C.sub.3-6), 2-alkynyl (C.sub.3-6), alkoxy(C.sub.1-6)methyl, benzyl, amino, fluoroalkyl (C.sub.1-6), alkoxy (C.sub.1-6)-carbonylmethyl; or cyanoalkyl (C.sub.1-6) having preferably one cyano group; X is hydrogen, fluorine, chlorine, bromine, cyano, alkyl(C.sub.1-6), haloalkyl(C.sub.1-6), haloalkoxy(C.sub.1-6), or alkoxy(C.sub.1-6); Y is hydrogen, alkyl (C.sub.1-6), fluorine, chlorine, or bromine; and Z is CH.sub.2, C.dbd.O, C.dbd.S, --CH(OH)--, --CH.sub.2 CH.sub.2 --, --CH.dbd.CH--, --(C.dbd.O)CH.sub.2 --; or C.dbd.N--O--R' wherein R' is alkyl(C.sub.1-6).Type: GrantFiled: February 3, 1995Date of Patent: May 28, 1996Assignee: FMC CorporationInventor: George Theodoridis
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Patent number: 5521189Abstract: The present invention provides methods for treating Pneumocystis carinii pneumonia and Giardia lamblia in a subject in need of such treatment. The methods comprises administering to the subject a compound of Formula I: ##STR1## wherein: X and Y are located in the para or meta positions and are selected from the group consisting of H, loweralkyl, loweralkoxy, and ##STR2## wherein: each R.sub.1 is independently selected from the group consisting of H, loweralkyl, alkoxyalkyl, hydroxyalkyl, aminoalkyl, alkylaminoalkyl, cycloalkyl, aryl, or alkylaryl or two R.sub.1 groups together represent C.sub.2 -C.sub.10 alkyl, hydroxyalkyl, or alkylene, or two R.sub.1 groups together represent ##STR3## wherein m is from 1-3 and R.sub.7 is H or --CONHCR.sub.8 NR.sub.9 R.sub.10.Type: GrantFiled: September 13, 1994Date of Patent: May 28, 1996Assignee: The University of NC at CHInventors: David W. Boykin, Christine C. Dykstra, Richard R. Tidwell, James E. Hall, W. David Wilson, Arvind Kumar
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Patent number: 5519139Abstract: There is disclosed a novel 4-aminopyrimidine derivative containing an optionally esterified carboxyl group at the 5-position which has potent fungicidal activity as well as insecticidal and miticidal activity. The compound is useful as agricultural fungicides, insecticides and miticides.Type: GrantFiled: May 23, 1995Date of Patent: May 21, 1996Assignee: Shionogi & Co., Ltd.Inventors: Toshikazu Ohtsuka, Moriyasu Masui, Takami Takeda, Michio Masuko, Katsuaki Ohba
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Patent number: 5512678Abstract: The present invention provides novel 5-(1-fluorovinyl)-1H-pyrimidine-2,4-dione derivatives which are useful as antineoplastic agents by themselves or in conjunctive therapy with the antineoplastic agent 5-fluorouracil.Type: GrantFiled: April 29, 1994Date of Patent: April 30, 1996Assignee: Merrell Pharmaceuticals Inc.Inventors: James R. McCarthy, Donald P. Matthews, Jeffrey S. Sabol
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Patent number: 5484901Abstract: Isoindolineazo pigments of the general formula I ##STR1## where A is the radical of an active-methylene compound or .dbd.S;L is substituted or unsubstituted 1,4-phenylene, 1,3-phenylene or 1,5-naphthylene;K is the radical of a coupling component K--H; and the benzene ring D is optionally substituted,are useful for pigmenting high polymer organic materials.Type: GrantFiled: March 22, 1995Date of Patent: January 16, 1996Assignee: BASF AktiengesellschaftInventors: Michael Krapp, Georg Henning
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Patent number: 5484763Abstract: There are provided substituted benzisoxazole and benzisothiazole compounds having the structural formula I ##STR1## Further provided are compositions and methods comprising those compounds for the control of undesirable plant species.Type: GrantFiled: February 10, 1995Date of Patent: January 16, 1996Assignee: American Cyanamid CompanyInventor: Peter J. Wepplo
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Patent number: 5476855Abstract: Novel compounds are provided that are effective to inhibit the activity of DHUDase or UrdPase. Such compounds have the general formula ##STR1## where X is S or Se; Y is I, F, Cl, Br, methoxy, benzyl, selenenylphenyl, or thiophenyl, and R.sub.1 is an acyclo tail having the general formula ##STR2## where R.sub.2 is H, CH.sub.2 OH or CH.sub.2 NH.sub.2 ; R.sub.3 is OH, NH.sub.2, or OCOCH.sub.2 CH.sub.2 CO.sub.2 H; and R.sub.4 is O, S, or CH.sub.2.The compounds can be used in pharmaceutical compositions, along with various chemotherapeutic agents to increase the efficacy of the treatment. These compounds can also be used in methods of treating patients by coadministering or sequentially administering the enzyme inhibiting compounds with a chemotherapeutic agent effective to treat cancers, or viral, fungal, bacterial, or parasitic infections. The compounds have further utility in enhancing imaging.Type: GrantFiled: November 2, 1993Date of Patent: December 19, 1995Assignees: Mahmoud H. el Kouni, Fardos N. M. Naguib, F. SchinaziInventors: Mahmoud el Kouni, Fardos N. M. Naguib, Raymond F. Schinazi
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Patent number: 5476834Abstract: There are disclosed novel dihydrobenzofuran derivatives of the formula: ##STR1## wherein X, Y, Z and R.sup.2 are each as defined in the description. Also disclosed are a herbicidal composition containing a herbicidally effective amount of the compound (I) as an active ingredient and a method for exterminating unfavorable weeds by applying a herbicidally effective amount of the compound (I) to an area where the unfavorable weeds grow or will grow.Type: GrantFiled: March 10, 1994Date of Patent: December 19, 1995Assignee: Sumitomo Chemical Company, LimitedInventors: Susumu Takemura, Minoru Takano, Satoru Kizawa, Kazuo Saito
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Patent number: 5470975Abstract: Novel A-II receptor antagonists have the formula ##STR1## and its isomer ##STR2## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7 and R.sub.8 are as defined herein.Type: GrantFiled: January 11, 1994Date of Patent: November 28, 1995Assignee: E.R. Squibb & Sons, Inc.Inventor: Karnail Atwal
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Patent number: 5470819Abstract: This invention relates to derivatives of acrylic acid useful in agriculture (especially as fungicides but also as plant growth regulators, insecticides and nematocides), to processes for preparing them, to agricultural (especially fungicidal) compositions containing them, and to methods of using them to combat fungi, especially fungal infections in plants, to regulate plant growth and to kill or control insect or nematode pests.The invention provides a compound having the formula (I): ##STR1## and stereoisomers thereof, wherein W is a substituted pyridinyl or substituted pyrimidinyl group linked to A by any of its ring carbon atoms; A is either an oxygen atom or S(O).sub.n wherein n is 0, 1 or 2; X, Y and Z, which are the same or different, are hydrogen or halogen atoms, or hydroxy, optionally substituted alkyl (including haloalkyl), optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted alkoxy.Type: GrantFiled: May 9, 1994Date of Patent: November 28, 1995Assignee: Zeneca LimitedInventors: Vivienne M. Anthony, John M. Clough, Paul deFraine, Christopher R. A. Godfrey, Ian Ferguson, Patrick J. Crowley, Michael G. Hutchings
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Patent number: 5466806Abstract: Disclosed are processes for preparing compounds of the formula (I) and pharmaceutically acceptable salts or esters thereof: ##STR1## wherein R.sub.2 is a purine or pyrimidine base or an analogue or derivative thereof; and Z is S, S.dbd.O or SO.sub.2. The invention also relates to intermediates of use in the preparation of these compounds.Type: GrantFiled: March 29, 1993Date of Patent: November 14, 1995Assignee: Biochem Pharma Inc.Inventors: Bernard Belleau, deceased, Tarek Mansour, Allan Tse, Colleen A. Evans, Haolun Jin, Boulos Zacharie, Nghe Nguyen-Ba
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Patent number: 5461060Abstract: The disclosure concerns pyrimidine derivatives represented by the following general formulas [I] and [I'] and having antiviral activity, particularly antiretroviral activity such as anti-HIV activity: ##STR1## and pharmaceutical compositions having antiviral activity and comprising the above-described derivative(s) as an active ingredient.Type: GrantFiled: September 3, 1993Date of Patent: October 24, 1995Assignee: Mitsubishi Kasei CorporationInventors: Tadashi Miyasaka, Hiromichi Tanaka, Erik D. A. De Clercq, Masanori Baba, Richard T. Walker, Masaru Ubasawa
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Patent number: 5461055Abstract: Compounds of the formula ##STR1## wherein R.sub.3, R.sub.4, J, K, Z, and Het are as set forth herein are described.The compounds of formula I are useful as agents in the treatment of fungal infections.Type: GrantFiled: June 3, 1994Date of Patent: October 24, 1995Assignee: Schering CorporationInventors: Alan B. Cooper, Anil K. Saksena, Raymond Lovey, Viyyoor Girijavallabhan, Ashit Ganguly
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Patent number: 5459144Abstract: The invention relates to compounds of the formula ##STR1## wherein Z, X, Q, Y, W, and W' are as described herein. These compounds have antiviral activity, and certain of these compounds have antiinflammatory activity and are PAF inhibitors.Type: GrantFiled: December 17, 1993Date of Patent: October 17, 1995Assignee: Schering CorporationInventors: Viyyoor M. Girijavallabhan, Ashit K. Ganguly, Patrick A. Pinto, Richard W. Versace
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Patent number: 5453427Abstract: The invention discloses compounds of formula I It has now been found that compounds of formula I ##STR1## wherein R.sub.1 is hydrogen, methyl, ethyl or trifluoromethyl, andR.sub.2 is hydrogen, methyl, ethyl, C.sub.1-4 alkylthio, C.sub.1-4 alkoxy, or di-C.sub.1-4 alkylamino, andR.sub.3 is C.sub.1-10 alkyl, C.sub.1-10 haloalkyl, aryl, heteroaryl, aryl-C.sub.1-4 alkyl, heteroaryl-C.sub.1-4 alkyl, aryloxy-C.sub.1-4 alkyl, aryloxyaryl, arylaryl, heteroaryl, aryl-C.sub.1-4 alkoxyaryl, aryl-C.sub.1-4 alkoxy-C.sub.1-4 alkyl, heteroaryloxyaryl, aryloxy-C.sub.1-4 alkylaryl or aryl substituted by a group selected from --C(CH.sub.3).dbd.N--O--CH.sub.2 --aryl, --C(CH.sub.3).dbd.N--O--CH(CH.sub.3)--aryl, --C(CH.sub.3).dbd.N--C.sub.1-4 alkoxy, --C(CH.sub.3).dbd.N--C.sub.3-4 alkenyloxy,--C(CH.sub.3).dbd.N--C.sub.3-4 alkynyloxy, or --CH.sub.2 --O--N.dbd.C(CH.sub.Type: GrantFiled: July 8, 1994Date of Patent: September 26, 1995Assignee: Sandoz Ltd.Inventors: Martin Eberle, Fritz Schaub, Gerald W. Craig
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Patent number: 5446040Abstract: Compounds of the formula ##STR1## wherein the variables R.sub.1 and p and the rings A and B are as defined in claim 1, and, where appropriate, tautomers thereof, in each case in free form or in the form of a salt, can be used as agrochemical active ingredients and can be prepared in a manner known per se.Type: GrantFiled: November 29, 1993Date of Patent: August 29, 1995Assignee: Ciba-Geigy CorporationInventor: Harald Walter
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Patent number: 5446013Abstract: Pyrimidinyl- or triazinyloxy- (or -thio)-carboxylic acid derivatives, processes for their preparation, and their use as herbicides or plant growth regulatorsCompounds of the formula (I) ##STR1## in which A is ##STR2## and R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, X and Y are as defined in claim 1 are suitable as selective herbicides and plant growth regulators.Type: GrantFiled: December 17, 1993Date of Patent: August 29, 1995Assignee: Hoechst AktiengesellschaftInventors: Frank Zurmuhlen, Klaus Bauer, Hermann Bieringer
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Patent number: 5441925Abstract: Herbicidal 1-Amino-3-(bicyclic heterocyclyl)-6-fluoroalkyluracils of the formula ##STR1## in which M is fluoroalkyl(C.sub.1-6); R.sup.1 is hydrogen or alkyl(C.sub.1-6); R.sup.2 is hydrogen or alkyl (C.sub.1-6); Y is hydrogen, fluorine, chlorine, or bromine; X is hydrogen, fluorine, chlorine, bromine, cyano, alkyl(C.sub.1-6), or fluoroalkyl(C.sub.1-6); and n is 0 or 1.Type: GrantFiled: June 28, 1994Date of Patent: August 15, 1995Assignee: FMC CorporationInventor: George Theodoridis
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Patent number: 5439908Abstract: Compounds of the formula ##STR1## wherein A is a substituted or unsubstituted, aromatic or non-aromatic, monocyclic or bicyclic, heterocyclic radical that is bonded by way of a carbon atom to X; each of R.sub.1 and R.sub.2, independently of the other, is hydrogen or C.sub.1 -C.sub.6 alkyl; X is NR.sub.3, O or S; and R.sub.3 is hydrogen or C.sub.1 -C.sub.4 alkyl, in free form or in salt form, can be used as agrochemical active ingredients and can be prepared in a manner known per se.Type: GrantFiled: October 30, 1992Date of Patent: August 8, 1995Assignee: Ciba-Geigy CorporationInventors: Peter Maienfisch, Manfred Boger, Thomas Pitterna
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Patent number: 5439874Abstract: The invention relates to novel substituted bicyclo[3.1.0]hexanes of the formula ##STR1## in which R.sup.1 represents, e. g., hydroxyl or alkoxy,R.sup.2 to R.sup.8 represent, e. g., hydrogen or alkyl,R.sup.9 and R.sup.10 represent, e.g., methyl or methoxy,X represents, e.g., oxygen,Y represents, e.g., oxygen or sulphur andZ represents, e.g., CH or N,as well as salts of the free acid (R.sup.1 =OH) and their further functional derivatives, and furthermore to processes and novel intermediates for their preparation, and to their use as herbicides.In addition, a novel process is described for preparing certain 2-keto-bicyclo[3.1.0]hexanes, which are required as intermediates, starting from correspondingly substituted .alpha.,.beta.-unsaturated carbonyl compounds (of the methacrolein type) and .beta.-keto acid esters (of the acetoacetic acid ester type).Type: GrantFiled: July 21, 1993Date of Patent: August 8, 1995Assignee: Bayer AktiengesellschaftInventors: Mark W. Drewes, Rolf Kirsten, Hans-Joachim Santel, Klaus Lurssen, Robert R. Schmidt
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Patent number: 5440040Abstract: The present invention is directed to compounds of formula (I), ##STR1## wherein R.sup.1 is OH, NH.sub.2 ; R.sup.2 is a heteroaromatic or aromatic substituent; R.sup.3 is H, OH, F, OCH.sub.3 ; R.sup.4 is H, F, OH or an ether or ester residue thereof, OCH.sub.3, CN, C.dbd.CH, N.sub.3 ; R.sup.5 is OH or an ether or ester residue thereof including mono, di- and triphosphate esters (.alpha.), wherein n is 0 or 1 and M is hydrogen or a pharmaceutically acceptable counterion such as sodium, potassium, ammonium or alkylammonium; and pharmaceutically acceptable salts thereof; and pharmaceutical compositions comprising said compounds can be used for therapeutic treatment of virus infections. The present invention is also directed to compounds of formula (I'), ##STR2## wherein R.sup.1 and R.sup.2 are as defined above, as intermediates.Type: GrantFiled: January 18, 1991Date of Patent: August 8, 1995Assignee: Medivir ABInventor: Salo Gronowitz
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Patent number: 5430031Abstract: The present invention provides compounds of the formula (I) ##STR1## wherein A, R.sub.1, R.sub.2 and R.sub.3 are defined as in the specification, or a pharmaceutically acceptable salt thereof. A process for their preparation and the pharmacetical compositions comprising them are also provided.Type: GrantFiled: December 20, 1993Date of Patent: July 4, 1995Assignee: Farmitalia Carlo Erba S.r.l.Inventors: Sergio Mantegani, Enzo Brambilla, Carla Caccia, Nicola Carfagna
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Patent number: 5424442Abstract: A water-soluble methine compound represented by the following general formula (I): ##STR1## wherein Z.sub.1 and Z.sub.2, which may be the same or different, each represents a non-metallic atomic group required for forming a 5-membered or 6-membered nitrogen-containing heterocyclic ring; R.sub.1 and R.sub.2, which may be the same or different, each represents an alkyl group; Q.sub.1 and Q.sub.2 each represents an atomic group required, in combination, for forming a 4-thiazolidinone ring, a 5-thiazolidinone ring, a 4-imidazolidinone ring, a 4-oxazolidinone ring, a 5-oxazolidinone ring, a 5-imidazolidinone ring or a 4-dithiolanone ring; L.sub.1, L.sub.2, L.sub.3, L.sub.4 and L.sub.5, which may be the same or different, each represents a methine group; R represents a hydrogen atom, an alkyl group, an aryl group or a heterocyclic group; m represents 1 or 2; i and h each represents 0 or 1; l represents 1 or 2; and j and k each represents 0, 1, 2 or 3.Type: GrantFiled: June 18, 1993Date of Patent: June 13, 1995Assignee: Fuji Photo Film Co., Ltd.Inventors: Keizo Koya, Toshinao Ukai, Haruo Takei
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Patent number: 5420099Abstract: A compound having the formula ##STR1## wherein A is CR.sub.7 ; and R.sup.1 through R.sup.7 are substituents such as hydrogen, halogen, branched and straight chain hydrocarbons, cyclic hydrocarbons, aromatics, and sulfur and nitrogen containing functional groups. Further, R.sup.5 and R.sup.6 may be taken together with the atom to which they are attached to form a group ##STR2## in which R.sup.9 and R.sup.10 are further functional groups. The compounds are useful in herbicidal compositions, particularly in combination with carriers and surfactants. A process for making this compound is also presented.Type: GrantFiled: December 21, 1992Date of Patent: May 30, 1995Assignee: Shell Research LimitedInventor: Trevor W. Newton
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Patent number: 5420133Abstract: Phenoxyphenylacetic acids and derivatives of general structural formula I ##STR1## have endothelin antagonist activity and are therefore useful in treating cardiovascular disorders, such as hypertension, postischemic renal failure, vasospasm, cerebral and cardiac ischemia, myocardial infarction, inflammatory diseases, Raynaud's disease, and endotoxic shock, and asthma.Type: GrantFiled: March 19, 1993Date of Patent: May 30, 1995Assignee: Merck & Co., Inc.Inventors: Daljit S. Dhanoa, Kenneth J. Fitch, Daniel F. Veber, Thomas F. Walsh, David L. Williams, Jr.
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Patent number: 5420276Abstract: A compound of the formula: ##STR1## wherein B is a purin-9-yl group or a heterocyclic isostere of a purin-9-yl group; or a pyrimidin-1-yl group or a heterocyclic isostere of a pyrimidin-1-yl group; A is --CH-- or A--G taken together is --C(.dbd.O)--, --C(.dbd.CH.sub.2)--, --C(OH)(CH.sub.2 OH)-- or ##STR2## and G and D are functional groups; or a pharmaceutically acceptable salt or ester thereof.Type: GrantFiled: December 7, 1993Date of Patent: May 30, 1995Assignee: Abbott LaboratoriesInventor: Daniel W. Norbeck
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Patent number: 5411935Abstract: There are disclosed novel dihydrobenzofuran derivatives of the formula: ##STR1## wherein A, X, Y, Z, R.sup.1 and R.sup.2 are each as defined in the description. Also disclosed are a herbicidal composition containing a herbicidally effective amount of the compound (I) as an active ingredient and a method for exterminating unfavorable weeds by applying a herbicidally effective amount of the compound (I) to an area where the unfavorable weeds grow or will grow.Type: GrantFiled: March 10, 1994Date of Patent: May 2, 1995Assignee: Sumitomo Chemical Co., Ltd.Inventors: Susumu Takemura, Minoru Takano, Satoru Kizawa, Kazuo Saito
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Patent number: 5397781Abstract: The present invention relates to novel 5-(.omega.-substituted amino-alkanoyl amino)pyrimidine derivatives, processes for producing the derivatives, and pharmaceutical compositions containing said derivatives. The compounds in the present invention have potent effects of inhibiting ACAT activity and lowering serum cholesterol. The compounds of the present invention are extremely useful for the treatment and/or prevention of arteriosclerosis or hyperlipidemia.Type: GrantFiled: February 11, 1993Date of Patent: March 14, 1995Assignee: Mochida Pharmaceutical Company, LimitedInventors: Kazutoshi Yanagibashi, Kiyoshi Mizuguchi, Shuhei Ohnishi, Kimihiro Murakami
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Patent number: 5391537Abstract: The present invention is to provide a novel picolinic acid derivative having the formula, ##STR1## (wherein R is a hydrogen atom, an alkyl group or others, R.sup.1 and R.sup.2 are the same or different, and are an alkyl group, an alkoxy group or others, X is a cyano group, a phenoxy group or others, Y is an oxygen atom or others, and n is 0 or 1) or a salt thereof; a method for preparing the same; and a herbicidal composition containing the same as an active ingredient.The picolinic acid derivative or the salt thereof of the present invention achieves an excellent herbicidal effect at a low dosage, and is effective for controlling the growth of various weeds in a wide range.The picolinic acid derivative or the salt thereof of the present invention can be applied to a paddy field, a cultivated field, a non-agricultural land and the like as a herbicidal composition.Type: GrantFiled: October 14, 1992Date of Patent: February 21, 1995Assignees: Kumiai Chemical Industry Co., Ltd., Ihara Chemical Industry Co., Ltd.Inventors: Fumiaki Takabe, Yoshihiro Saito, Masatoshi Tamaru, Shigehiko Tachikawa, Ryo Hanai
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Patent number: 5391740Abstract: This disclosure relates to a method and reagents for determining ligands in biological fluids such as serum, plasma, spinal fluid, amnionic fluid and urine. In particular, this disclosure relates to a fluorescence polarization immunoassay procedure and to a novel class of tracer compounds employed as reagents in such procedures. The procedure disclosed combines the specificity of an immunoassay with the speed and convenience of fluorescence polarization techniques to provide a means for determining the amount of the specific ligand present in a sample.Type: GrantFiled: April 8, 1993Date of Patent: February 21, 1995Assignee: Abbott LaboratoriesInventors: Chao-Huei J. Wang, Stephen D. Stroupe, Michael E. Jolley
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Patent number: 5387575Abstract: Disclosed are a pyrimidine or triazine compound represented by the following formula (I): ##STR1## wherein R.sup.1 represents cyano group, a halogen atom, hydroxy group or --O--R.sup.7 where R.sup.7 represents a lower alkyl group, a lower alkenyl group, a lower alkynyl group, a halo-lower alkyl group or a cyano-lower alkyl group; R.sup.2 represents hydrogen atom or a lower alkyl group; R.sup.3 represents hydrogen atom or a lower alkyl group; R.sup.4 represents a 1-imidazolyl group, --NHSO.sub.2 --R.sup.8 where R.sup.8 represents a lower alkyl group or a phenyl group which may have a substituent, hydroxy group, a lower alkoxy group or a benzyloxy group when Z is nitrogen atom; or a 1-imidazolyl group, --NHSO.sub.2 --R.sup.8 where R.sup.Type: GrantFiled: June 5, 1992Date of Patent: February 7, 1995Assignee: Ube Industries, Ltd.Inventors: Katsumasa Harada, Takaaki Abe, Yuji Akiyoshi, Akio Matsushita, Mikio Kojima, Ikuo Shiraishi, Kaoru Yamamoto, Takashi Hayama, Shohei Fukuda
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Patent number: 5387587Abstract: Chroman derivatives of the formula I ##STR1## wherein R.sup.1 to R.sup.8 have the meanings defined herein, and their salts have an effect on the cardiovascular system.Type: GrantFiled: September 27, 1991Date of Patent: February 7, 1995Assignee: Merck Patent Gesellschaft mit beschrankter HaftungInventors: Gunther Hausler, Rolf Gericke, Hanns Wurziger, Manfred Baumgarth, Inge Lues, Jacques De Peyer, Rolf Bergmann
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Patent number: 5385880Abstract: Herbicidal composition containing a compound having the following formula or its salt: ##STR1## wherein W is an oxygen atom, a sulfur atom, a NH group or a group of the formula, >NC(O)B;Z is a methine group or a nitrogen group;X is a phenyl group which may be substituted or a group having the formula: ##STR2## and n is an integer of from 1 to 3.Type: GrantFiled: September 17, 1992Date of Patent: January 31, 1995Assignees: Kumiai Chemical Industry Co., Ltd., Ihara Chemical Industry Co., Ltd.Inventors: Masahiro Miyazaki, Masafumi Matsuzawa, Keiji Toriyabe, Michiya Hirata
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Patent number: 5380700Abstract: The present invention provides a novel pyridine derivative having the following general formula and its salt: ##STR1## wherein R is a hydrogen atom, a hydroxyl group, an alkoxy group, an alkoxyalkoxy group, and derivatives;R.sup.1 and R.sup.2 may be the same or different, and are a hydrogen atom, an alkoxy group, a halogen atom, an alkylamino group, a dialkylamino group;Z is a methine group or a nitrogen atom;X.sup.1 is an acylamino group, a cycloalkyl group, a halogen-substituted alkoxy group, an alkenyloxy group, an alkynyloxy group, an alkoxycarbonyl group, an alkylamino group, a dialkylamino group, a phenyl group.The pyridine derivative and its salt of the present invention achieve an excellent herbicidal effect on annual and perennial weeds growing in paddy fields and upland fields at a very small dosage.The pyridine derivative and its salt of the present invention have safety to rice, wheat, cotton and corn, and can be suitably applied as a herbicide to a field where these plants are cultivated.Type: GrantFiled: December 23, 1992Date of Patent: January 10, 1995Assignees: Kumiai Chemical Industries Co., Ltd., Ihara Chemical Industries Co., Ltd.Inventors: Masahiro Miyazaki, Masafumi Matsuzawa, Keiji Toriyabe, Michiya Hirata
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Patent number: 5380701Abstract: The invention relates to 3-aryluracils of formula I ##STR1## wherein W is a group of formula ##STR2## in which the linkage to the ring nitrogen atom is through the carbon atom: R.sub.1 is hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 haloalkyl, C.sub.3 - or C.sub.4 alkenyl or C.sub.3 - or C.sub.4 alkynyl;R.sub.2 is halogen or cyano;R.sub.3 is hydrogen or fluoro;R.sub.4 is hydrogen, halogen or C.sub.1 -C.sub.4 alkyl;R.sub.5 is C.sub.1 -C.sub.4 alkyl or C.sub.1 C.sub.4 haloalkyl;R.sub.6 to R.sub.9 are each independently of one another hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.3 -C.sub.6 alkenyl, C.sub.3 -C.sub.6 alkynyl, C.sub.1 -C.sub.4 haloalkyl or phenyl; orR.sub.6 and R.sub.7 or R.sub.8 and R.sub.9, together with the linking carbon atom, form a 3-, 4-, 5- or 6-membered ring which may be substituted by one or more C.sub.1 -C.sub.4 alkyl groups; or R.sub.7 and R.sub.9, together with the linking carbon atoms, form a 3-, 4-, 5- or 6-membered ring which may be substituted by one or more C.sub.1 -C.sub.Type: GrantFiled: October 12, 1993Date of Patent: January 10, 1995Assignee: Ciba-Geigy CorporationInventors: Paul Winternitz, Martin Zeller
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Patent number: 5376657Abstract: Benzimidazolesulfonic acid derivatives of the formula I ##STR1## in which R.sub.1 is an unsaturated 5-membered heterocycle having not more than two hetero atoms N and/or S or is an unsaturated 6-membered heterocycle having not more than two N atoms, it being possible for each of the heterocycles to be substituted, and X is oxygen or sulfur, while R.sub.2, R.sub.3, R.sub.4 and n are as defined herein, are valuable microbicides. They can be used in crop protection in the form of suitable compositions, for example for controlling fungal disease.Type: GrantFiled: May 21, 1993Date of Patent: December 27, 1994Assignee: Ciba-Geigy CorporationInventors: Adolf Hubele, Bernard Hostettler, Marius Sutter, Urs Muller
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Patent number: 5370821Abstract: The invention relates to optically active compounds represented by the general formula ##STR1## wherein R.sub.1, R.sub.2, Q.sub.1, Q.sub.2, Q.sub.3, ##STR2## and M are defined as in the specification, methods and intermediates for their preparation, liquid crystal compositions comprising at least one optically active compound of formula I and their use in electrooptical display, switching and modulation devices.Type: GrantFiled: January 11, 1993Date of Patent: December 6, 1994Assignees: Takeda Chemical Industries, Ltd., Hitachi, Ltd.Inventors: Koichi Matsumura, Mitsuru Kawada, Yoshitaka Uesugi, Yuka Sudo, Katsumi Kondo, Teruo Kitamura
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Patent number: 5371062Abstract: The present invention relates to new substituted azines, of the general formula (I) ##STR1## in which n, Q.sup.1, Q.sup.2, Q.sup.3, R.sup.1, R.sup.2, R.sup.3, X, Y and Z have the meanings given in the description, to a plurality of processes for their preparation, and to their use as herbicides.Type: GrantFiled: April 1, 1993Date of Patent: December 6, 1994Assignee: Bayer AktiengesellschaftInventors: Roland Andreee, Mark W. Drewes, Hans-Joachim Santel, Klaus Lurssen, Robert R. Schmidt
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Patent number: 5356863Abstract: The present invention relates to an uracil derivative represented by the formula (1): ##STR1## in which R.sup.1 represents hydrogen, alkyl or haloalkyl; R.sup.2 represents haloalkyl; R.sup.3 represents hydrogen, alkyl, haloalkyl, hydroxymethyl, halogen or nitro; R.sup.4 represents hydrogen or halogen; R.sup.5 represents hydrogen, halogen, nitro or cyano; X represents oxygen or sulfur: provided that the case where both of Da and Db represent hydrogen is excluded and a herbicide containing the same. The compound can be safely applied to important crops and shows high effect against many weeds in a low amount.Type: GrantFiled: October 21, 1993Date of Patent: October 18, 1994Assignee: Nissan Chemical Industries, Ltd.Inventors: Jun Satow, Kenzou Fukuda, Kaoru Itoh, Hiroshi Kita, Yasuo Kawamura, Koichi Suzuki, Tsutomu Nawamaki, Shigeomi Watanabe, Toshiharu Endo, Kimihiro Ishikawa
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Patent number: 5354730Abstract: A compound of the formula: ##STR1## wherein R.sup.1 is a trifluoromethyl group or a pentafluoroethyl group, R.sup.2 is a methyl group or an amino group, R.sup.3 is a C.sub.1 -C.sub.7 alkyl group, a C.sub.3 -C.sub.7 alkenyl group, a C.sub.3 -C.sub.7 alkynyl group, a halo (C.sub.1 -C.sub.6) alkyl group, a halo (C.sub.3 -C.sub.6) alkenyl group or a C.sub.1 -C.sub.4 alkoxy(C.sub.1 -C.sub.3)alkyl group and Y is an oxygen atom or a sulfur atom, which is useful as a herbicide.Type: GrantFiled: May 25, 1993Date of Patent: October 11, 1994Assignee: Sumitomo Chemical Company, LimitedInventors: Masayuki Enomoto, Eiki Nagano, Ryo Sato, Masaharu Sakai
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Patent number: 5350750Abstract: .beta.-carboline-3-hydroxyalkylcarboxylic acid ester derivatives of formula I ##STR1## in which R.sup.A, n, R.sup.4 and R.sup.3, have the meaning indicated in the claims, as well as their production and their use in pharmaceutical agents are described.Type: GrantFiled: March 1, 1993Date of Patent: September 27, 1994Assignee: Schering AktiengesellschaftInventors: Andreas Huth, Martin Kruger, Dieter Seidelmann, Ralph Schmiechen, Werner Krause, Herbert Schneider, Lechoslaw Turski
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Patent number: 5346881Abstract: Herbicidal 3-(bicyclic heterocyclyl)-6-fuoroalkyluracils of the formula ##STR1## in which M is fluoroalkyl(C.sub.1-6); R is hydrogen, alkyl(C.sub.1-6), 2-alkynyl(C.sub.3-6); 2-alkenyl(C.sub.3-6,), or cyanoalkyl(C.sub.1-6); R.sup.1 is hydrogen or alkyl(C.sub.1-6); R.sup.2 is hydrogen or alkyl (C.sub.1-6); Y is hydrogen, fluorine, chlorine, or bromine; X is hydrogen, fluorine, chlorine, bromine, cyano, alkyl(C.sub.1-6), or fluoroalkyl(C.sub.1-6); and n is 0 or 1.Type: GrantFiled: August 13, 1993Date of Patent: September 13, 1994Assignee: FMC CorporationInventor: George Theodoridis
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Patent number: 5342958Abstract: Compounds of the formula ##STR1## wherein A is a hydrogen atoms, a halogen atom, a methyl group, or a methoxy group;B is a hydrogen atom, a halogen atom, a methyl group, or a methoxy group, with the proviso that A and B ar not both a hydrogen atom;X and Y each are an oxygen atom or a sulfur atom;R is a hydrogen atom, an alkyl group, a hydroxy group, an alkoxy group, an alkoxymethyl group, an acyl group, or an alkoxycarbonyl group;R.sub.1 is a hydrogen atom, an alkyl group, a halogen substituted alkyl group, an alkoxy substituted alkyl group, an alkylthio substituted alkyl group, a cyano substituted alkyl group, a 1-cycloalkenyl group, a benzyl group, a halogen substituted benzyl group, a hydroxy group, an alkoxy group, an acyl group, an alkoxycarbonyl group, an alkoxythiocarbonyl group, an alkylsulfonyl group, or a phenylsulfonyl group, while furthermore R and R.sub.1 together with the group ##STR2## indicated in the above formula may form a ring system; and R.sub.Type: GrantFiled: August 11, 1993Date of Patent: August 30, 1994Assignee: Solvay Duphar International Research B.V.Inventors: Kobus Wellinga, Rudolf Mulder
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Patent number: 5332717Abstract: The invention relates to compounds of formula ##STR1## wherein W, X, Y.sup.1, Y.sup.2, Z, R.sup.1, R.sup.2 and R.sup.14 are as defined in the description, and to the preparation thereof, to weed control compositions and plant-growth-regulating compositions comprising such compounds as active ingredients, and to the use of the active ingredients or compositions for controlling weeds and for regulating plant growth.Type: GrantFiled: April 15, 1993Date of Patent: July 26, 1994Assignee: Ciba-Geigy CorporationInventors: Christoph Luthy, Jean-Pierre Obrecht