The Chalcogen, X, Is In A -c(=x)- Group Patents (Class 548/187)
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Patent number: 4948415Abstract: Agents for regulating plant growth containing an effective amount of at least one cyclohexenone derivative of the formula ##STR1## where R.sup.1, R.sup.2 and R.sup.3 have the meanings given in the disclosure, or a salt thereof, and a process from regulating plant growth.Type: GrantFiled: February 2, 1989Date of Patent: August 14, 1990Assignee: BASF AktiengesellschaftInventors: Michael Keil, Dieter Jahn, Dieter Kolassa, Ulrich Schirmer, Rainer Becker, Johann Jung, Wilhelm Rademacher
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Patent number: 4946962Abstract: Two classes of certain compounds known as bis(thiazolinethiones), more particularly bis[(3,4-disubstituted)-thiazole-2-thiones], have thiazolinethione heterocycle units linked by alkylene, arylene, or arene groups or by a carbon to carbon single bond. These compounds are useful in the graphic arts because of their reduced volatility, reduced migrating aptitude, and reduced hydrophilicity compared to mono thiazolinethiones.Type: GrantFiled: May 23, 1989Date of Patent: August 7, 1990Assignee: Minnesota Mining and Manufacturing CompanyInventors: Steven J. Heilmann, Larry R. Krepski, Jerald K. Rasmussen, Alan R. Katritzky, Richard D. Tarr
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Patent number: 4939172Abstract: Novel cyclopropane carboxylic acid esters of all possible stereoisomeric forms and mixtures thereof of the formula ##STR1## wherein X is selected from the group consisting of hydrogen, fluorine, chlorine and bromine, R is selected from the group consisting of optionally unsaturated alkyl of 1 to 8 carbon atoms optionally substituted, optionally unsaturated cycloalkyl of 3 to 8 carbon atoms optionally substituted, optionally substituted aryl of 6 to 14 carbon atoms and optionally substituted heterocycle, Z is selected from the group consisting of hydrogen, --CH.sub.3, --CN and --C.tbd.CH and Y is selected from the group consisting of hydrogen, --OH, optionally unsaturated alkyl of 1 to 8 carbon atoms optionally substituted, --CN, --(CH.sub.2).sub.m --OAlk, --(CH.sub.2).sub.m --S--Alk, ##STR2## m is 0,1,2,3 or 4, Alk is alkyl of 1 to 12 carbon atoms, --Si(Alk').sub.3, Alk' is optionally unsaturated alkyl of 1 to 8 carbon atoms optionally substituted, --O--Ar and --(CH.sub.2).sub.Type: GrantFiled: February 8, 1988Date of Patent: July 3, 1990Assignee: Roussel UclafInventors: Joseph Cadiergue, Jacques Demassey, Jean-Pierre Demoute, Jean Tessier
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Patent number: 4937255Abstract: For inhibiting 3-hydroxy-3-methylglutaryl coenzyme A and cholesterol biosynthesis, the novel disubstituted pyrroles of the formula ##STR1## in which R.sup.1 is aryl or heteroaryl,R.sup.2 is cycloalkyl or optionally substituted alkyl,R.sup.3 is hydrogen or cycloalkyl, or optionally substituted alkyl, aryl or heteroaryl,X is --CH.sub.2 --CH.sub.2 -- or --CH.dbd.CH--,A is ##STR2## R.sup.6 is hydrogen or alkyl, and R.sup.7 is hydrogen, a cation or alkyl, aryl or aralkyl.Type: GrantFiled: March 16, 1989Date of Patent: June 26, 1990Assignee: Bayer AktiengesellschaftInventors: Walter Hubsch, Rolf Angerbauer, Peter Fey, Hilmar Bischoff, Dieter Petzinna, Delf Schmidt, Gunter Thomas
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Patent number: 4929743Abstract: Herbicidally active novel 4,5-disubstituted 1,3-thiazol-2-yloxyacetamides of the formula ##STR1## in which R.sup.1 is fluorine or chlorine,R.sup.2 is alkyl or halogenoalkyl, andR.sup.3 and R.sup.4 each independently is alkyl, alkenyl, alkinyl, optionally substituted cycloalkyl, optionally substituted cycloalkenyl, halogenoalkyl, alkoxyalkyl, alkoxyalkyleneoxy, alkoxy, aralkyl or optionally substituted aryl, orR.sub.3 and R.sub.4, conjointly with the nitrogen atom to which they are bonded form an optionally substituted, heterocyclic ring which can contain further hetero-atoms.Type: GrantFiled: June 15, 1988Date of Patent: May 29, 1990Assignee: Bayer AktiengesellschaftInventors: Heinz Forster, Gunther Beck, Erich Klauke, Hans-Joachim Santel, Robert R. Schmidt
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Patent number: 4925862Abstract: All stereoisomeric forms and mixtures thereof of a compound of the formula ##STR1## wherein X is --O-- or --S--, Y is --C.dbd.O, ##STR2## or --CH.sub.2 --, R.sub.1 is selected from the group consisting of hydrogen, halogen, optionally unsaturated alkyl of 1 to 8 carbon atoms and optionally unsaturated cycloalkyl of 3 to 8 carbon atoms, the latter two being optionally substituted with one or more halogen and aryl of 6 to 14 carbon atoms, R.sub.2 is selected from the group consisting of hydrogen, --CF.sub.3, --NO.sub.2, --CN, halogen, alkoxy of 1 to 8 carbon atoms, aryl of 6 to 14 carbon atoms, an ester, optionally unsaturated alkyl of 1 to 8 carbon atoms and optionally unsaturated cycloalkyl of 3 to 8 carbon atoms the latter two being optionally substituted with one or more halogen, R.sub.3 is selected from the group consisting of hydrogen, alkyl of 1 to 3 carbon atoms, --CN and --C.tbd.CH and A is the residue of an ACOOH pyrethrinoid acid having pesticidal properties.Type: GrantFiled: July 20, 1988Date of Patent: May 15, 1990Assignee: Roussel UclafInventors: Jacques Demassey, Jean-Pierre Demoute, Jean Tessier
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Patent number: 4914206Abstract: The present invention provides lankacidin derivatives of the formula ##STR1## and procedures for the production thereof. The lankacidin derivatives [1] show excellent antimicrobial activities and thus can be used for prophylaxis and treatment of infectious disease in animals.Type: GrantFiled: December 15, 1988Date of Patent: April 3, 1990Assignee: Takeda Chemical Industries, LTD.Inventors: Isao Minamida, Naoto Hashimoto
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Patent number: 4897397Abstract: Certain aryl-alkynoic, alkenoic and alkanoic acids and derivatives and their use in treating inflammation, allergy and hyperproliferative skin disease are disclosed.Type: GrantFiled: December 16, 1988Date of Patent: January 30, 1990Assignee: Schering CorporationInventors: Neng Y. Shih, David J. Blythin
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Patent number: 4891432Abstract: Novel phenoxy derivatives are provided which can be represented by the general formula: ##STR1## wherein the various substituents are as defined, and include compounds such as benzyl 6-[p-[5-(1-imidazolyl)pentyloxy]phenoxy]-2,2-dimethylhexanoate.The invention also encompasses pharmaceutical compositions containing the derivatives and their use in treating tumors.Type: GrantFiled: July 16, 1987Date of Patent: January 2, 1990Assignee: Yamanouchi Pharmaceutical Co., Ltd.Inventors: Noriki Ito, Yoshinobu Nagano, Akihiro Tanaka, Yoso Numasaki, Koichiro Takahashi
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Patent number: 4889863Abstract: The invention relates to new thiazole compounds of the general formula ##STR1## wherein R is an C.sub.1 -C.sub.12 alkyl group or a phenyl group, which groups are unsubstituted or substituted with halogen, nitro or cyano;R.sub.1 is a cyano group; a formyl group; an alkylcarbonyl or alkoxycarbonyl group having 2-5 carbon atoms; or a substituted or non-substituted benzoyl group;R.sub.2 is a hydrogen atom; a halogen atom; an amino group; an amino group substituted with 1 or 2 substituents selected from the group consisting of C.sub.1 -C.sub.4 alkyl, C.sub.2 -C.sub.5 alkynyl, C.sub.2 -C.sub.5 alkylcarbonyl and C.sub.2 -C.sub.5 alkoxycarbonyl; an alkyl, alkoxy, alkylthio, alkylsulphinyl or alkyl-sulphonyl group having 1-4 carbon atoms; or a substituted or non-substituted aryl, aryloxy, arylthio, arylsulphinyl or arylsulphonyl group; andn is 1 or 2.The new compounds show a fungicidal activity and may be used in particular against plant pathogenic seed fungi and soil fungi.Type: GrantFiled: July 22, 1988Date of Patent: December 26, 1989Assignee: Duphar International Research B.V.Inventors: Hendrik Dolman, Johannes Kuipers
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Patent number: 4889953Abstract: Compounds of the formula: ##STR1## wherein R.sup.1 is a higher alkyl group which may be substituted; R.sup.2 is a hydrogen, a lower alkyl group which may be substituted, a lower alkanoyl group which may be substituted or a lower alkylthiocarbamoyl group; R.sup.3 is a primary to tertiary amino group or a quaternary ammonium group; and n is 2 or 3, and salts thereof, have antitumor activity and platelet activating factor inhibitory activity.Type: GrantFiled: July 22, 1987Date of Patent: December 26, 1989Assignee: Takeda Chemical Industries, Ltd.Inventors: Keizo Inoue, Hiroaki Nomura, Tetsuya Okutani
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Patent number: 4888348Abstract: The invention relates to novel substituted phenylthioureas, phenylisothioureas and phenylcarbodiimides of formula I ##STR1## wherein Z is ##STR2## or --N.dbd.C.dbd.N--; R.sub.1 is C.sub.1 -C.sub.12 alkyl, C.sub.3 -C.sub.10 alkenyl, C.sub.3 -C.sub.10 alkynyl, C.sub.3 -C.sub.8 cycloalkyl, C.sub.1 -C.sub.3 alkyl substituted by 1 or 2 C.sub.3 -C.sub.6 cycloalkyl radicals, or is alkoxyalkyl containing a total of 3 to 10 carbon atoms, halogen-substituted C.sub.1 -C.sub.12 alkyl, polycyclic C.sub.7 -C.sub.10 cycloalkyl, or phenyl(C.sub.1 -C.sub.5)alkyl which may be substituted in the phenyl moiety by 1 or 2 identical or different members selected from the group consisting of halogen, methoxy, ethoxy and C.sub.1 -C.sub.5 alkyl,R.sub.2 is hydrogen or C.sub.1 -C.sub.5 alkyl,R.sub.3 is C.sub.1 -C.sub.5 alkyl or C.sub.3 -C.sub.6 cycloalkyl,R.sub.4 is hydrogen or C.sub.1 -C.sub.4 alkyl,R.sub.Type: GrantFiled: August 28, 1987Date of Patent: December 19, 1989Assignee: Ciba-Geigy CorporationInventors: Josef Ehrenfreund, Manfred Boger, Odd Kristiansen, Jozef Drabek, Haukur Kristinsson
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Patent number: 4873253Abstract: A phenylalanine derivative having the formula (I): ##STR1## wherein A represents ##STR2## B represents ##STR3## wherein m is 0, 1, or 2 and n is 3, 4, or 5; X represents (a) hydroxy, (b) nitro, (c) amino, (d) phenoxy which may be substituted with (i) halogen or (ii) nitro, (e) c.sub.1 -C.sub.4 alkyloxy which may be substituted wit (i) phenyl or (ii) benzoyl, (f) benzoyl, (g) pyridyloxy which may be substituted with (i) halogen or (ii) nitro, or (h) c.sub.1 -C.sub.4 alkyl which may by substituted with halogen;Y represents ##STR4## or --OR.sup.3 wherein R.sup.1 R.sup.2 are independently (a) hydrogen, (b) phenyl which may be substituted with (i) benzoyl, (ii) C.sub.1 -C.sub.4 alkylcarbonyl, (iii) C.sub.1 -C.sub.4 alkyl which may be further substituted with C.sub.1 -C.sub.4 alkoxycarbonyl or hydroxycarbonyl, (iv) C.sub.2 -C.sub.5 alkenyl which may be further substituted with hydroxycarbonyl or C.sub.1 -C.sub.4 alkoxycarbonyl, (v) C.sub.1 -C.sub.Type: GrantFiled: March 30, 1987Date of Patent: October 10, 1989Assignees: Shosuke Okamoto, Showa Denko Kabushiki KaishaInventors: Shosuke Okamoto, Yoshio Okada, Akiko Okunomiya, Taketoshi Naito, Yoshio Kimura, Morihiko Yamada, Norio Ohno, Yasuhiro Katsuura, Hiroshi Nojima, Takashi Shishikura
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Patent number: 4865641Abstract: Herbicidally active compounds of the formula ##STR1## in which R.sup.1 represents hydrogen or alkyl,R.sup.2 represents hydrogen or alkyl,with the proviso that R.sup.1 and R.sup.2 do not simultaneously represent hydrogen,X represents oxygen or sulphur,R.sup.3 represents hydrogen, halogen, nitro, amino, cyano, alkyl, halogenoalkyl, alkoxy or halogenoalkoxy,wherein the radicals R.sup.3 can be identical or different,n represents a number from 1-4,U represents oxygen or sulphur,V represents a ##STR2## group, R.sup.4 and R.sup.5 independently of one another repreesnt hydrogen, alkyl, alkoxyalkyl or halogenoalkyl,W represents a radical ##STR3## D represents carbon or silicon, E represents oxygen or sulphur, andR.sup.6 through R.sup.12 can have various meanings.The starting materials wherein -U-V-W together are OH are also new.Type: GrantFiled: March 9, 1988Date of Patent: September 12, 1989Assignee: Bayer AktiengesellschaftInventors: Klaus Sasse, Reiner Fischer, Hermann Hagemann, Andreas Krebs, Michael Schwamborn, Hans-Joachim Santel, Robert R. Schmidt, Robert H. Strang
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Patent number: 4863945Abstract: Pyrrolobenzimidazoles of the formula: ##STR1## are useful for treatment of heart and circulatory diseases. R.sub.1 is substituted phenyl; or optionally substituted naphthyl or a five- or six-membered heterocyclic group which can be condensed with a phenyl ring to form a bicyclic radical. R.sub.2 is hydrogen, alkyl, alkenyl or cycloalkenyl; R.sub.3 is alkyl, alkenyl or hydroxyalkyl or with R.sub.2 together forms cycloakylene; or R.sub.2 and R.sub.3 together form alkylidene or cycloalkylidene. R.sub.4 is hydrogen or lower alkanoyl. X is a valency bond, alkylene, vinylene, imino or carbonylamino. T stands for two hydrogen atoms. When X is a valency bond, R.sub.1 can also be hydrogen, hydrocarbyl which may also contain oxygen, amino, sulfur, carbonyl and sulfonyl groups. When X is imino or carbonylamino or when R.sub.1 is a bicyclic radical, T can also be oxygen. The compounds also include the tautomers and physiologically acceptable salts with inorganic and organic acids.Type: GrantFiled: December 10, 1987Date of Patent: September 5, 1989Assignee: Boehringer Mannheim GmbHInventors: Walter-Gunar Friebe, Alfred Mertens, Klaus Strein, Erwin Boehm
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Patent number: 4863947Abstract: This invention relates to novel N-aryl-3-aryl-4,5-dihydro-1H-pyrazole-1-carboxamide compounds which are useful as pesticides, compositions containing those compounds, methods of controlling pests and processes for preparing these compounds.Type: GrantFiled: August 11, 1986Date of Patent: September 5, 1989Assignee: Rohm and HaasInventor: Richard M. Jacobson
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Patent number: 4857538Abstract: A compound, and composition including same, for effecting irreversible change in cell morphology having the following structures: ##STR1## wherein R is --(CH.sub.2).sub.n ZH in which n=1, 2, 3 and 4 and Z is O, S, or NH, and ##STR2## wherein R.sub.1 and R.sub.2 can be --OH, alkyl and acyl.Type: GrantFiled: November 30, 1987Date of Patent: August 15, 1989Assignee: The Research Foundation of State University of New YorkInventors: Yoel Kashman, Ilan Spector, Shmuel Carmely, Dina Blasberger
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Patent number: 4849449Abstract: Novel stereoisomers or mixtures of stereoisomers of compounds of the formula ##STR1## wherein R is the residue of an alcohol used in the pyrethrinoid field having remarkable pesticidal properties and being surprisingly stable.Type: GrantFiled: December 9, 1986Date of Patent: July 18, 1989Assignee: Roussel UclafInventors: Jean Tessier, Jean-Pierre DeMoute, Joseph Cadiergue
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Patent number: 4826992Abstract: 2,3-(Dihydro) bicyclic pyrazolidinones are intermediates for bicyclic pyrazolidinone antimicrobials.Type: GrantFiled: November 24, 1986Date of Patent: May 2, 1989Assignee: Eli Lilly and CompanyInventors: Louis N. Jungheim, Sandra K. Sigmund
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Patent number: 4826990Abstract: There are disclosed compounds of the formula ##STR1## wherein X is ##STR2## Y is ##STR3## Z is ##STR4## R.sup.1 is ##STR5## n is 0-5; R.sup.2 is hydrogen, loweralkyl, loweralkoxy, lower alkoxycarbonyl, trifluoromethyl, nitro, cyano or halo;R.sup.3 is ##STR6## W represents a bond or ##STR7## m is 1-15; R.sup.4 is hydrogen or loweralkyl;R.sup.5 is lower alkyl, monofluoroloweralkyl, difluoroloweralkyl, polyfluoroloweralkyl, perfluoroloweralkyl or ##STR8## R.sup.6 is hydrogen, lower alkyl, ##STR9## and the pharmaceutically acceptable salts thereof, and their use in the treatment of leukotriene-mediated naso-bronchial obstructive airpassageway conditions, such as allergic rhinitis, allergic bronchial asthma and the like, and as antiinflammatory agents.Type: GrantFiled: September 30, 1987Date of Patent: May 2, 1989Assignee: American Home Products CorporationInventors: John H. Musser, Reinhold H. W. Bender, Anthony F. Kreft, III
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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: 4792606Abstract: A process for the preparation of a dimeric aromatic acyl cyanide of the formula ##STR1## in which Ar is optionally substituted phenyl, naphthyl or hetaryl,comprising reaction an acyl halide of the formulaAr--CO--Halin whichHal is fluorine, chlorine or bromine, with an alkali metal cyanide in a two-phase system comprising water and a water-immiscible or only sparingly water-miscible aliphatic ketone, and in the presence of a phase-transfer catalyst. The products are known intermediates for pesticides.Type: GrantFiled: July 16, 1987Date of Patent: December 20, 1988Assignee: Bayer AktiengesellschaftInventors: Reinhard Lantzsch, Hermann-Dieter Krall
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Patent number: 4788291Abstract: Herbicidally active novel 4,5-disubstituted 1,3-thiazol-2-yloxyacetamides of the formula ##STR1## in which R.sup.1 is fluorine or chlorine,R.sup.2 is alkyl or halogenoalkyl, andR.sup.3 and R.sup.4 each independently is alkyl, alkenyl, alkinyl, optionally substituted cycloalkyl, optionally substituted cycloalkenyl, halogenoalkyl, alkoxyalkyl, alkoxyalkyleneoxy, alkoxy, aralkyl or optionally substituted aryl, orR.sub.3 and R.sub.4, conjointly with the nitrogen atom to which they are bonded form an optionally substituted, heterocyclic ring which can contain further hetero-atoms.Type: GrantFiled: February 5, 1986Date of Patent: November 29, 1988Assignee: Bayer AktiengesellschaftInventors: Heinz Forster, Gunther Beck, Erich Klauke, Hans-Joachim Santel, Robert R. Schmidt
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Patent number: 4772309Abstract: A 5-Acylamino-pyrazole derivatives of the formula ##STR1## in which R.sup.1 represents hydrogen, halogen or nitro,R.sup.2 represents hydrogen, alkyl, alkenyl, alkinyl or optionally substituted cycloalkyl,R.sup.3 represents hydrogen or alkyl,R.sup.4 represents hydrogen or alkyl,X represents oxygen or sulphur,n represents the integer 0, 1 or 2,Ar represents in each case optionally substituted phenyl or pyridyl andHet represents an optionally substituted 5- or 6- membered heterocyclic radical linked via a carbon atom,which exhibit herbicidal and plant growth regulating activity.Type: GrantFiled: March 19, 1987Date of Patent: September 20, 1988Assignee: Bayer AktiengesellschaftInventors: Jorg Stetter, Reinhold Gehring, Otto Schallner, Hans-Joachim Santel, Robert R. Schmidt, Klaus Lurssen
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Patent number: 4764514Abstract: This invention provides a oxothiazolidine compound of the formula: ##STR1## wherein R.sup.1 is acyl;di(lower)alkylamino(lower)alkylcarbamoyl(lower)alkyl; arylcarbamoyl(lower)alkyl;ar(lower)alkylcarbamoyl(lower)alkyl;heterocyclic carbamoyl(lower)alkyl;heterocyclic(lower)alkylcarbamoyl(lower)alkyl;thiazolidinylcarbonyl(lower)alkyl;morpholinylcarbonyl(lower)alkyl or a group of the formula: ##STR2## in which A is lower alkylene;n is an integer of 0 or 1;m is an integer of 2 or 3;X is --N--, ##STR3## or --CH-- and R.sup.2 is hydroxy;lower alkyl which may have hydroxy;ar(lower)alkyl which may have halogen;arylthio which may have halogen;acyl or heterocyclic group andY is --S--, ##STR4## or pharmaceutically acceptable salt thereof. This compound is useful as cognition activator. This invention further provides processes for the preparation of this compound and pharmaceutical composition comprising compound of the above formula.Type: GrantFiled: April 24, 1986Date of Patent: August 16, 1988Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Ikuo Ueda, Yousuke Katsura
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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: 4760067Abstract: Organic sulfoxides having a latent allyl group bound to the sulfur are enzyme inhibitors of the suicide or K.sub.cat type.Type: GrantFiled: March 9, 1987Date of Patent: July 26, 1988Assignee: Merck & Co., Inc.Inventor: Raymond A. Firestone
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Patent number: 4748174Abstract: The water soluble acid addition salts of an NSAID, such as acetylsalicylic acid, fenbufen, diflunisal, piroxicam, naproxen, or the like, with either glucamine or meglumine (N-methylglucamine) are useful anti-inflammatory and analgesic drugs, well adopted for parenteral, oral, rectal or topical administration.Type: GrantFiled: January 5, 1987Date of Patent: May 31, 1988Assignee: Therapicon s.r.l.Inventor: Paolo A. Veronesi
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Patent number: 4746669Abstract: Thiazole derivatives have been made, for example, by reacting a 2-aryl-2,2-dialkoxyethylamine with an appropriately substituted aryl acetyl halide followed by treating the resulting amide with diphosphoryl pentasulfide. The thiazole derivatives are found to be effective immunoregulants.Type: GrantFiled: March 26, 1987Date of Patent: May 24, 1988Assignee: Merck & Co., Inc.Inventors: Charles G. Caldwell, Ihor Kopka, Milton L. Hammond, Robert A. Zambias
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Patent number: 4742060Abstract: Novel insecticides of the formula ##STR1## in which n is 0 or 1,X is S, O, ##STR2## Y is N or ##STR3## Z is a 5- or 6-membered nitrogen-containing heterocyclic ring, and R to R.sup.9 variously represent hydrogen or specified organic radicals.Type: GrantFiled: January 21, 1986Date of Patent: May 3, 1988Assignee: Nihon Tokushu Noyaku Seizo K. K.Inventors: Kozo Shiokawa, Shinichi Tsuboi, Shinzo Kagabu, Koichi Moriya
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Patent number: 4741756Abstract: A propionic acid thiol ester derivative having the formula: ##STR1## wherein R.sub.1 is a cyano group, a trifluoromethyl group, a halogen atom or a nitro group, R.sub.2 is a hydrogen atom, a halogen atom or a cyano group, R.sub.3 is a thiazolin-2-yl group or a benzothiazol-2-yl group, and A is a methine group or a nitrogen atom.Type: GrantFiled: May 12, 1987Date of Patent: May 3, 1988Assignees: Toyo Soda Mfg. Co., Agro-Kenesho Co., Ltd.Inventors: Shinzo Someya, Seigo Koura, Mikio Ito, Akira Nakanishi, Yuji Nonaka
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Patent number: 4735957Abstract: New thiazole derivatives of the formula: ##STR1## wherein R.sup.1 is lower alkyl, carboxy, a drivative of carboxy, hydroxymethyl, halomethyl, lower alkylthiomethyl, hydroxyiminomethyl or alkenyl which may be substituted with lower alkoxycarbonyl, pyridyl or cyano,R.sup.2 is hydrogen, hydroxy, lower alkyl, pyridyl, amino, lower alkylamino, pyridylamino, arylamino, acylamino, N-(lower)alkylN-acylamino, guanidino optionally substituted with dimethylaminomethylene, or ar(lower)alkylamino optionally substituted with lower alkoxy,R.sup.3 is lower alkyl, halo(lower)alkyl or N-containing unsaturated heterocyclic group which may be substituted with halogen, lower alkyl, lower alkoxy, carboxy, a derivative of carboxy, hydroxy, pyridyl, amino, lower alkylamino, pyridylamino, arylamino, acylamino, N-(lower)alkyl-N-acylamino, guanidino, N-oxide or ar(lower)alkylamino optionally substituted with lower alkoxy,Q is --CO--, andn is an integer of 0 or 1,provided that when both of R.sup.1 and R.sup.Type: GrantFiled: November 18, 1986Date of Patent: April 5, 1988Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Takao Takaya, Hisashi Takasugi
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Patent number: 4722932Abstract: Disclosed herein novel compounds, 2-substituted-4-thiazolidones having anti-peptic ulcer activity, and methods for producing the same.Type: GrantFiled: August 30, 1985Date of Patent: February 2, 1988Assignee: Kureha Kagaku Kogyo Kabushiki KaishaInventors: Takao Kawasaki, Tadashi Tsuchiya, Yoshiaki Osaka
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Patent number: 4666502Abstract: The invention provides 5-membered heteroaromatic compounds of formula IArN(Y)COCH.sub.2 Cl Iwherein Ar is a 5-membered heteroaromatic group comprising 1 or 2 heteroatoms selected from O, S and N and linked by a ring C-atom to the N-atom of the N(Y)COCH.sub.2 Cl group to which it is bound, whereby where Ar is pyrazolyl, said N(Y)COCH.sub.2 Cl group is in the 4-position,and Y is as specified in the description,the use of these compounds as herbicides, compositions for facilitating such use and the preparation of the chloroacetamides.Type: GrantFiled: February 3, 1983Date of Patent: May 19, 1987Assignee: Sandoz Ltd.Inventors: Karl Seckinger, Fred Kuhnen, Karlheinz Milzner
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Patent number: 4663341Abstract: This invention relates to N-aryl-3-aryl-4,5-dihydro-1H-pyrazole-1-carboxamide compounds which are useful as pesticides, compositions containing those compounds, methods of controlling pests and processes for preparing these compounds.Type: GrantFiled: January 11, 1985Date of Patent: May 5, 1987Assignee: Rohm and Haas CompanyInventor: Richard M. Jacobson
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Patent number: 4636245Abstract: Novel substituted tetrahydrothiopyran-2,4-dione herbicides of the formula ##STR1## in which R.sup.1 is hydrogen, alkyl, alkenyl, alkinyl, alkoxyalkyl, alkylthioalkyl, halogenoalkyl, cycloalkyl or optionally substituted aryl,R.sup.2 is alkyl, alkenyl, alkinyl, alkoxyalkyl, alkylthioalkyl, halogenoalkyl, halogenoalkenyl, alkoxycarbonylalkyl, alkoximinoalkyl, optionally substituted aralkyl or optionally substituted heterocyclylalkyl, andR.sup.3 and R.sup.4 each independently is hydrogen, alkyl, alkoxyalkyl, alkylthioalkyl, cycloalkyl, optionally substituted aryl, optionally substituted aryloxyalkyl or optionally substituted aralkyl,or metal salts thereof.Type: GrantFiled: May 23, 1985Date of Patent: January 13, 1987Assignee: Bayer AktiengesellschaftInventors: Heinz-Jurgen Wroblowsky, Jorg Stetter, Ludwig Eue, Robert R. Schmidt, Hans-Joachim Santel
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Patent number: 4624962Abstract: Compounds of the formula I ##STR1## in which n denotes 0-3,R.sup.1 and R.sup.1' are the same or different and denote hydrogen, alkyl or alkenyl, phenyl or benzyl, each substituted as desired;R.sup.2 denotes hydrogen, alkyl or alkenyl;R.sup.3 denotes hydrogen, alkyl, hydroxyalkyl, alkoxyalkyl or aminoalkyl, alkanoylaminoalkyl, guanidinoalkyl, imidazolylalkyl, indolylalkyl, mercaptoalkyl or alkylthioalkyl, phenylalkyl, hydroxphenylalkyl, phenoxyalkyl or phenylthioalkyl, or R.sup.2 and R.sup.3, together with the C and N atoms carrying them, denote a saturated or unsaturated 4- to 8-membered monocyclic or 8- to 10-membered bicyclic isocycle or heterocycle, optionally monosubstituted or disubstituted by hydroxyl, alkoxy having 1 to 3 C atoms or alkyl,R.sup.4 denotes hydrogen, alkyl, alkenyl, alkadienyl, alkinyl, alkeninyl or alkadiinyl, cycloalkyl, phenyl, benzyl, phenethyl or phenylpropyl, each of which can be optionally monosubstituted or disubstituted;R.sup.5 denotes hydrogen or alkyl, hydroxyl or alkoxy andR.Type: GrantFiled: February 1, 1985Date of Patent: November 25, 1986Assignee: Hoechst AktiengesellschaftInventors: Rainer Henning, Hansjorg Urbach, Rolf Geiger, Volker Teetz, Bernward Scholkens
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Patent number: 4604132Abstract: The invention concerns novel compounds of the formula I ##STR1## wherein: A, B and D are selected from CH and N;E is selected from oxygen and sulfur;X are selected from halogen, nitro, cyano, alkyl, substituted alkyl, hydroxy, alkoxy, substituted alkoxy, alkenyl, alkenyloxy, alkynyl, alkynyloxy, acyloxy, alkoxycarbonyl, alkylthio, alkylsulfinyl, alkylsulfonyl, sulfamoyl, substituted sulfamoyl, alkanoyloxy, benzyloxy, substituted benzyloxy, phenyl, substituted phenyl, amino, substituted amino, and the groups formyl and alkanoyl and the oxime, imine and Schiff base derivatives thereof;R.sup.1 is selected from hydrogen, alkyl, alkenyl, alkynyl, substituted alkyl, alkylsulfonyl, arylsulfonyl, acyl and an inorganic or organic cation;R.sup.2 is selected from alkyl substituted alkyl, alkenyl, haloalkenyl, alkynyl and haloalkynyl;R.sup.3 is selected from alkyl, fluoroalkyl, alkenyl, alkynyl, and phenyl;R.sup.Type: GrantFiled: April 27, 1984Date of Patent: August 5, 1986Assignee: ICI Australia LimitedInventors: Richard J. Conway, Keith G. Watson, Graeme J. Farquharson
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Patent number: 4602940Abstract: This invention relates to ortho-heterocyclic benzene sulfonylureas which are useful as herbicides and growth regulants.Type: GrantFiled: May 20, 1985Date of Patent: July 29, 1986Assignee: E. I. Du Pont de Nemours and CompanyInventor: Anthony D. Wolf
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Patent number: 4602095Abstract: Novel 3-hydroxy-4-alkyloxphenyl heterocyclic aromatic carboxylate compounds particularly well suited as sweeteners in foodstuff.Type: GrantFiled: December 29, 1983Date of Patent: July 22, 1986Assignee: General Foods CorporationInventors: Paul R. Zanno, Ronald E. Barnett, Jed A. Riemer
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Patent number: 4585574Abstract: Anthraquinone dyestuffs of the formula ##STR1## in which R.sub.1 and R.sub.2 denote hydrogen, alkyl, cycloalkyl, aryl or aralkyl, and the said hydrocarbon radicals can be substituted, andQ denotes an aryl radical or heterocyclic radical or an --OR', --SR', --CH.dbd.N--R', ##STR2## --CHO or --SO.sub.2 --O--R' radical, whereinR' represents an aryl, aralkyl or heterocyclic radical, and the radicals mentioned for R' can be substituted,processes for their preparation, and liquid-crystalline materials containing anthraquinone dyestuffs.Type: GrantFiled: November 25, 1981Date of Patent: April 29, 1986Assignee: Bayer AktiengesellschaftInventors: Martin Blunck, Uwer Claussen, Rutger Neeff
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Patent number: 4584306Abstract: Compounds of the formula ##STR1## their preparation, and use for the control of nematodes are disclosed and exemplified.Type: GrantFiled: April 4, 1984Date of Patent: April 22, 1986Assignee: FMC CorporationInventor: Anthony J. Martinez
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Patent number: 4581453Abstract: The invention relates to guanidinothiazol derivatives of Formula (I) as defined herein, said compounds being useful for influencing lipid metabolism, as antithombotic agents and as antimycotic agents. Also included in the invention are compositions containing said guanidinothiazol derivatives of Formula (I) and the use of said compounds and compositions for treatment of the above-mentioned conditions. In addition, the invention includes methods for the manufacture of the guanidinothiazole derivatives of Formula (I).Type: GrantFiled: May 9, 1983Date of Patent: April 8, 1986Assignee: Bayer AktiengesellschaftInventors: Joachim Ippen, Elisabeth Perzborn, Walter Puls, Klaus Schaller, Friedel Seuter
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Patent number: 4578388Abstract: The compounds are C.sub.2 -C.sub.8 straight chain alkanes terminally substituted, symmetrically or unsymmetrically, by N-(N'-substituted guanidino), N-(N',N"-disubstituted guanidino). N-(N'-substituted thioureido), N-(nitromethylene amidino) or S-(N-substituted isothioureido) groups. Two compounds of the invention are 1,3-bis-[N'-(2-(5-methyl-4-imidazolylmethylthio)ethyl)guanidino]propane and 1,3-bis-[S-(N-2-(5-methyl-4-imidazolylmethylthio)ethyl)isothioureido]p ropane. The compounds of this invention are inhibitors of H-2 histamine receptors.Type: GrantFiled: June 30, 1983Date of Patent: March 25, 1986Assignee: SmithKline & French Laboratories LimitedInventors: Graham J. Durant, Charon R. Ganellin
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Patent number: 4563471Abstract: 4-Oxothiazolidin-2-ylidene-acetamide derivatives, processes for their preparation, pharmaceutical compositions and a method for treating diseases of the central nervous system such as epilepsy are described.Type: GrantFiled: May 8, 1984Date of Patent: January 7, 1986Assignee: Warner-Lambert CompanyInventors: Gerhard Satzinger, Manfred Herrmann, Edgar Fritschi, Johannes Hartenstein, Gerd Bartoszyk
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Patent number: 4540702Abstract: Disclosed herein novel compounds, 2-substituted-4-thiazolidones having anti-peptic ulcer activity, and methods for producing the same.Type: GrantFiled: August 30, 1982Date of Patent: September 10, 1985Assignee: Kureha Kagaku Kogyo Kabushiki KaishaInventors: Takao Kawasaki, Tadashi Tsuchiya, Yoshiaki Osaka
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Patent number: 4535164Abstract: A process is disclosed for preparing 4-thiazolidinones having the formula: ##STR1## by cyclizing a compound of the formula:(R.sup.2 --NHCO--CH.sub.2 S).sub.2 ----CRR.sup.1in an aprotic reaction medium in the presence of a metal catalyst.Type: GrantFiled: March 30, 1983Date of Patent: August 13, 1985Assignee: Merck & Co., Inc.Inventors: Robert M. Di Pardo, Mark G. Bock
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Patent number: 4535092Abstract: Acylanilides of the formula ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are substituents defined in claim 1; wherein R.sup.4 is hydrogen or alkyl of up to 4 carbon atoms, or is joined to R.sup.5 as stated below;wherein R.sup.5 is hydrogen, hydroxy, or alkoxy or acyloxy each of up to 15 carbon atoms, or is joined to R.sup.4 to form an oxycarbonyl group such that together with the --N--CO--C-- part of the molecule it forms an oxazolidinedione group;wherein R.sup.6 is alkyl or halogenoalkyl of up to 4 carbon atoms;and wherein R.sup.7 is 5- or 6- membered saturated or unsaturated heterocyclic which contains one, two or three hetero atoms selected from oxygen, nitrogen and sulphur, which heterocyclic may be a single ring or may be fused to a benzo-ring, and which heterocyclic is unsubstituted or bears one or two substituents defined in claim 1;processes for their manufacture and pharmaceutical compositions containing them. The compounds possess antiandrogenic activity.Type: GrantFiled: November 1, 1982Date of Patent: August 13, 1985Assignee: Imperial Chemical Industries PLCInventor: Leslie R. Hughes
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Patent number: 4532138Abstract: Compounds of the formula: ##STR1## and the pharmaceutically acceptable, non-toxic salts and esters (alkyl, 1-6C) thereof, wherein:X is O or S;R.sup.1 is selected from the group consisting of:(a) alkyl or cycloalkyl of 3-8 carbons,(b) ##STR2## in which Z is O, S or --CH.sub.2, and Y is lower alkyl (1-4C), lower alkoxy (1-4C), halo, or --CF.sub.3, and(c) ##STR3## in which Z and X are as herein defined; and R.sup.2 is hydrogen or methyl;exhibit prostaglandin-like activity and are, thus, useful as platelet aggregation inhibitors.Type: GrantFiled: November 2, 1983Date of Patent: July 30, 1985Assignee: Syntex (U.S.A.) Inc.Inventors: Joseph M. Muchowski, Angel Guzman
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Patent number: RE33125Type: GrantFiled: July 11, 1986Date of Patent: December 5, 1989Assignee: Rorer Pharmaceutical CorporationInventors: Henry F. Campbell, Thomas H. Scholtz, George H. Douglas