The Chalcogen, X, Is In A -c(=x)- Group Patents (Class 548/170)
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Patent number: 5648370Abstract: There are disclosed compounds of formula I,Ar--CH.sub.2 CH.sub.2 --NH--CR.sup.1 R.sup.2 --X--Y Iin whichAr represents a group, ##STR1## X represents a C.sub.1-12 alkylene chain optionally interrupted or terminated by one or more groups selected from --S(O).sub.n --, --O--, --C(Z)--, CR.sup.6 R.sup.7, phenylmethyne, --NR.sup.8 --, --CONH--, --NHCO-- and --NHCONH--,Y represents an optionally substituted aryl or cycloalkyl group,Z represents O or S,R.sup.1, R.sup.2, R.sup.5 and R.sup.9 each independently represent hydrogen or alkyl C.sub.1-6,R.sup.3 and R.sup.4 represent hydrogen, or R.sup.3 and R.sup.4 together form a group --S--, --NR.sup.9 -- or --CH.sub.2 --,R.sup.6 and R.sup.7 independently represent hydrogen, alkyl C.sub.1-6, fluoro, cyano, or CF.sub.3, provided that at least one of R.sup.6 and R.sup.7 is other than hydrogen,R.sup.8 represents hydrogen or alkyl C.sub.1-6, or when X is interrupted or terminated by more than one --NR.sup.8 -- group may together with another R.sup.8 group form the chain --CH.Type: GrantFiled: November 28, 1994Date of Patent: July 15, 1997Assignee: Astra Pharmaceuticals LimitedInventors: Roger V. Bonnert, Roger C. Brown, David R. Cheshire, Francis Ince, John Dixon
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Patent number: 5629265Abstract: Disclosed herein are cyanoketone derivatives of the following formula (1) ##STR1## such as 1-cyano-1-piperidinocarbonyl-3-[4-(2-chloro-4-trifluoromethylphenoxy)pheno xy]-2-butanone, 1-cyano-1-piperidinocarbonyl-3-[4-(3-chloro-5-trifluoromethyl-2-pyridyloxy )phenoxy]-2-butanone, 1-cyano-1-(N-methyl-N-dichlorophenyl)aminocarbonyl-3-[4-(2-quinoxalyloxy)p henoxy]-2-butanone, 1-cyano-1-(N,N-dibutyl)aminocarbonyl-3-[4-(3-chloro-5-trifluoromethyl-2-py ridyloxy)phenoxy-2-butanone, and the like, which are characterized by excellent herbicidal activity and effectiveness against a variety of gramineous weeds.Type: GrantFiled: June 22, 1994Date of Patent: May 13, 1997Assignee: Tokuyama CorporationInventors: Masahiko Ishizaki, Seiji Nagata, Junji Takenaka
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Patent number: 5618775Abstract: Mixtures of optically active cyclohexenone oxime ethers having R- and S-configuration in the oxime ether moiety of the formula I ##STR1## (R.sup.1 =C.sub.1 -C.sub.6 -alkyl; ##STR2## X=C.sub.1-C.sub.4 -alkyl, C.sub.1 -C.sub.4 -haloalkyl; m=0-3 or 1-4 where all X's are halogen;n=0-3 or 1-5 where all X's are halogen;R.sup.2 =C.sub.1 -C.sub.4 -alkoxy-C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.4 -alkylthio-C.sub.1 -C.sub.6 -alkyl, substituted or unsubstituted C.sub.3 -C.sub.7 -cycloalkyl, substituted or unsubstituted C.sub.5 -C.sub.7 -cycloalkenyl, substituted or unsubstituted 5-membered saturated heterocyclic structure, substituted or unsubstituted 6- or 7-membered heterocyclic structure, substituted or unsubstituted 5-membered heteroaromatic structure, substituted or unsubstituted phenyl or pyridyl)and their agriculturally useful salts and esters with C.sub.1 -C.sub.10 -carboxylic acids and inorganic acids.Type: GrantFiled: August 11, 1994Date of Patent: April 8, 1997Assignee: BASF AktiengesellschaftInventors: Ulf Misslitz, Norbert Meyer, Juergen Kast, Wolfgang Ladner, Helmut Walter, Karl-Otto Westphalen, Uwe Kardorff, Matthias Gerber
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Patent number: 5597819Abstract: New benzothiazine derivatives corresponding to the general formula I: ##STR1## in which: X represents halogen,n represents 0, 1, or 2,B represents the following formula: ##STR2## in which: R.sub.1 & R.sub.2 together with the carbons to which they are attached form a 6-carbon-atom aromatic ring which is optionally substituted by a group X' representing halogen, andY represents the radical --(SO.sub.2).sub.x --Alk--Z, x, Alk, and Z are as defined in the specification;as well as their possible stereoisomers, epimers, N-oxides and pharmaceutically-acceptable acid or base addition salts; and medicinal products containing the same, useful in the treatment of inflammatory disorders requiring an inhibitor of cytokines.Type: GrantFiled: February 13, 1995Date of Patent: January 28, 1997Assignee: Adir Et CompagnieInventors: Jean-Daniel Brion, Anne-Marie Chollet, Luc Demuynck, Lucy De Montarby, Yves Rolland, Jacqueline Bonnet, Pietro Ghezzi, Armel Fradin
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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: 5556990Abstract: This invention relates to a class of novel dicarboxy amide derivatives of lipophilic amines which exhibit squalene synthase inhibition properties. More specifically the compounds are bis-aryl and/or heteroaryl alkyl or cycloalkylamino dicarboxy amides. Compounds of this invention reduce levels of serum cholesterol in the body without significantly reducing mevalonic metabolite synthesis. This invention relates also to pharmacological compositions and method of treatment for lowering serum cholesterol levels using the compounds of this invention.Type: GrantFiled: December 16, 1994Date of Patent: September 17, 1996Assignee: Rhone-Poulenc Rorer Pharmaceuticals Inc.Inventors: Henry W. Pauls, Yong-Mi Choi, Robert W. Studt, Martin P. Maguire, Alfred P. Spada, Don D. Cha
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Patent number: 5550229Abstract: Novel process for preparing azetidinone compound of the formula [III]: ##STR1## wherein R.sup.1 is H or lower alkyl, R.sup.2 and R.sup.3 combine together with the adjacent nitrogen to form heterocyclic group, and R.sup.4 is protected or unprotected hydroxy-substituted lower alkyl, which comprises reacting an alkanamide compound of the formula [I]: ##STR2## wherein R.sup.1, R.sup.2 and R.sup.3 are the same as defined above, with a compound of the formula [II]: ##STR3## wherein L.sup.1 is a leaving group and R.sup.4 is the same as defined above, in the presence of a base, said compound [III] being useful as synthetic intermediate for 1-methylcarbapenem derivative having excellent antibacterial activity.Type: GrantFiled: June 21, 1994Date of Patent: August 27, 1996Assignee: Tanabe Seiyaku Co., Ltd.Inventors: Tameo Iwasaki, Kazuhiko Kondo, Hiroshi Ohmizu
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Patent number: 5550143Abstract: A compound of formula (I): ##STR1## in which X, n, B and Y are as defined in the description. useful as cytokine inhibitors.Type: GrantFiled: April 12, 1994Date of Patent: August 27, 1996Assignee: Adir et CompagnieInventors: Jean-Daniel Brion, Anne-Marie Chollet, Luc Demuynck, Lucy De Montarby, Yves Rolland, Jacqueline Bonnet, Pietro Ghezzi, Armel Fradin
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Patent number: 5529998Abstract: The invention relates to benzoxazolyl- and benzothiazolyloxazolidinones, processes for their preparation and their use as medicaments, in particular as antibacterial medicaments.Type: GrantFiled: July 27, 1995Date of Patent: June 25, 1996Assignee: Bayer AktiengesellschaftInventors: Dieter Habich, Bernd Riedl, Martin Ruppelt, Andreas Stolle, Hanno Wild, Rainer Endermann, Klaus D. Bremm, Hein-Peter Kroll, Harald Labischinski, Klaus Schaller, Hans-Otto Werling
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Patent number: 5521145Abstract: There is disclosed an iminothiazoline derivative of the general formula: ##STR1## wherein R.sub.1 is (halo)alkyl, (halo)alkenyl, (halo)alkynyl or the like; R.sub.2 is (halo)alkyl, optionally substituted aryl, formyl, cyano or the like; R.sub.3 is hydrogen, (halo)alkyl or the like; and Q is a group of the particular general formula. Also disclosed are a herbicide containing a herbicidally effective amount of the iminothiazoline derivative and a method for controlling unfavorable weeds, which includes applying a herbicidally effective amount of the iminothiazoline derivative to an area where the unfavorable weeds grow or will grow.Type: GrantFiled: April 3, 1995Date of Patent: May 28, 1996Assignee: Sumitomo Chemical Company, Ltd.Inventors: Minoru Takano, Masayuki Enomoto, Kazuo Saito, Satoru Kizawa
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Patent number: 5519136Abstract: A radiation-sensitive compound has the general formula ##STR1## wherein A represents the ring members required to complete a 5- or 6-membered heterocyclic ring which may optionally be fused to an optionally substituted aromatic nucleus,B represents H, acryl, aroyl, heterocyclyl carbonyl or ##STR2## R represents an optionally substituted alkyl group, E and G, which may be the same or different, each represents H or CH.sub.p X.sub.3-p,J and K, which may be the same or different, each represents an aryl or heterocyclic group, which may optionally include a substitutent additional to E or G,X represents Cl or Br, andm, n and p, which may be the same or different, each represents an integer equal to 0, 1 or 2.The compound can be used to form radiation sensitive compositions for the production of radiation sensitive plates in lithographic printing plate manufacture.Type: GrantFiled: May 22, 1992Date of Patent: May 21, 1996Inventor: John R. Wade
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Patent number: 5492925Abstract: There are provided thienyl- and furylpyrrole compounds of formula I ##STR1## and their use for the control of insects and acarina. Further provided are compositions and methods comprising those compounds for the protection of plants from attack by insects and acarina.Type: GrantFiled: August 31, 1993Date of Patent: February 20, 1996Assignee: American Cyanamid CompanyInventors: Roger W. Addor, Joseph A. Furch, III, Laurelee A. Duncan, Jack K. Siddens, deceased
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Patent number: 5491156Type: GrantFiled: February 16, 1994Date of Patent: February 13, 1996Assignee: Zeneca LimitedInventors: Ian T. Streeting, deceased, Paul A. Worthington
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Patent number: 5470863Abstract: A description follows of oximic derivatives with a fungicide activity, for agricultural use, having the formula (I): ##STR1## wherein: A, B, D, are N, or .dbd.C--G;G is H, halogen, NO.sub.2, CN, --COOR.sub.4, C.sub.1 -C.sub.6 (halo)alkylR.sub.1, R.sub.2, R.sub.4 and R.sub.5, are C.sub.1 -C.sub.6 (halo)alkyl;R.sub.3 is H, C.sub.1 -C.sub.6 (halo)alkyl or --COOR.sub.5 ;W is C.sub.2 -C.sub.10 alkylene;L represents O or S;Y represents phenyl, naphthyl, heterocycle, substituted alkyl.Type: GrantFiled: September 10, 1992Date of Patent: November 28, 1995Assignees: Ministero Dell'Universita' E Della Ricerca Scientifica E TechnologicaInventors: Giovanni Camaggi, Lucio Filippini, Marilena Gusmeroli, Giovanni Meazza, Giampaolo Zanardi, Carlo Garavaglia, Luigi Mirenna
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Patent number: 5451594Abstract: The invention provides compounds of formula (I) having nematicidal, insecticidal, acaricidal and fungicidal properties, compositions comprising them and processes and intermediates for their preparation: ##STR1## wherein: X is oxygen or sulphur;n is 0, 1 or 2;R.sup.1, R.sup.2, R.sup.3, and R.sup.4 are as described in the specification.Type: GrantFiled: September 10, 1993Date of Patent: September 19, 1995Assignee: Zeneca LimitedInventors: Steven Fitzjohn, Michael P. Robinson, Michael D. Turnbull, Alison M. Smith, Roger Salmon, Robin Taylor
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Patent number: 5380735Abstract: The present invention relates to a novel benzothiazole derivative of the following general formula (I) or its (E) , (Z)isomer, and processes for preparation thereof, ##STR1## in which R.sup.1, R.sup.2 and R.sup.3 independently of one another represent hydrogen, halogen, straight and branched (C.sub.1 -C.sub.8)alkyl, (C.sub.1 -C.sub.8)halogenoalkyl or (C.sub.1 -C.sub.8)alkoxy,X represents N or CH,Y represents a group -OR.sup.4, SR.sup.5 or ##STR2## R.sup.4, R.sup.5, R.sup.6 and R.sup.7 independently of one another represent hydrogen, straight and branched (C.sub.1 -C.sub.16)alkyl, (C.sub.3 -C.sub.8)alkenyl, (C.sub.3 -C.sub.8)alkynyl, (C.sub.3 -C.sub.8)cycloalkyl, alkyl substituted with (C.sub.1 -C.sub.6)alkoxy or (C.sub.1 -C.sub.6)halogenoalkyl, or represent a substituted phenyl, phenylacyl or benzyl group wherein the possible substituent on the phenyl, phenylacyl or benzyl group includes halogen, straight and branched (C.sub.1 -C.sub.8)alkyl, (C.sub.1 -C.sub.8)alkoxy, (C.sub.3 -C.sub.8)alkenyl, (C.sub.3 -C.Type: GrantFiled: September 27, 1993Date of Patent: January 10, 1995Assignee: Lucky, Ltd.Inventors: Bon Y. Jung, Choon S. Ra, Yo S. Rew, Young H. Rhee, Ho S. Yeo, Man Y. Yoon, Woo B. Choi
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Patent number: 5347008Abstract: Compounds of the formula ##STR1## in which X is --S--, --O-- or --NH--, R is H or a monovalent substituent, n is 0 or 1 and R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are H, alkyl, alkyl which is substituted by OH, halogen, COOH or alkoxy, unsubstituted or substituted aryl or aralkyl, or carboxyl, or R.sup.1 and R.sup.2 or R.sup.1 and R.sup.3 together are alkylene or R.sup.1 and R.sup.2 are a direct bond, at least two of the groups R.sup.1, R.sup.2, R.sup.3 and R.sup.4 being carboxyl or carboxyalkyl groups, and base addition salts thereof are effective corrosion inhibitors. The preparation of these novel polycarboxylic acids can be effected by various processes.Type: GrantFiled: November 12, 1992Date of Patent: September 13, 1994Assignee: Ciba-Geigy CorporationInventors: Robert L. Bentley, Michael P. Savage, Kenneth W. Shelton
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Patent number: 5338844Abstract: A 2-substituted-2-cyclopentenone compound represented by the following formula (I) and an anticancer agent and a bone formation accelerator comprising the same as an effective active ingredient: ##STR1##Type: GrantFiled: July 16, 1993Date of Patent: August 16, 1994Assignee: Teijin LimitedInventors: Satoshi Sugiura, Toru Minoshima, Atsuo Hazato, Yoshinori Kato
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Patent number: 5300521Abstract: The invention compounds of formula I ##STR1## wherein R is H, C.sub.1-4 alkyl; optionally substituted aryl or CF.sub.3 ;Y is C.sub.1-4 alkyl or optionally substituted aryl;A is nitrogen or CH; andZ is optionally substituted hydrocarbyl or optionally substituted heteroaryl;the use of such compounds for the control of phytopathogens, compositions for facilitating such use, and the preparation of compounds of formula I.Type: GrantFiled: September 1, 1993Date of Patent: April 5, 1994Assignee: Sandoz Ltd.Inventors: Martin Eberle, Fritz Schaub
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Patent number: 5258395Abstract: Novel heterocyclic compounds shown by the general formula ##STR1## or the pharmaceutically acceptable salts thereof useful as medicament in particular as antagonist of slow reacting substance of anaphylaxis (SRS-A).Type: GrantFiled: October 13, 1992Date of Patent: November 2, 1993Assignee: Yamanouchi Pharmaceutical Co., Ltd.Inventors: Kiyoshi Murase, Toshiyasyu Mase, Hiromu Hara, Kenichi Tomioka
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Patent number: 5258521Abstract: Processes for producing optically active ester derivatives are disclosed. According to the present invention an optically active aryloxyphenoxy propionate derivative is produced by reacting a chlorinated heterocyclic aromatic compound with (2R)-2-(4-hydroxyphenoxy)propionic acid tetrahydrofurfuryl ester in an anhydrous solvent in the presence of a base. According to the present invention, an optically active propionate derivative of the formula [I] ##STR1## (wherein R represents hydrogen or 3-chloro-5-trifluoromethyl-2-pyridyl group) is produced by reacting a corresponding optically active methyl propionate derivative with tetrahydrofurfuryl alcohol, or by reacting a corresponding optically active propionic acid derivative with tetrahydrofurfuryl alcohol, or by reacting (2S)-tetrahydrofurfuryl 2-chloropropionate with a corresponding phenol derivative in specific conditions.Type: GrantFiled: July 25, 1990Date of Patent: November 2, 1993Assignee: Tosoh CorporationInventors: Takumi Kagawa, Mikio Ito, Syunji Aman, Takashi Morooka, Hiroyuki Watanabe, Kenji Tsuzuki
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Patent number: 5240919Abstract: Compounds of general formula (I): ##STR1## where R, X, A, B and p are defined in the description. Medicinal products useful for treating sleep disorders comprising the same.Type: GrantFiled: March 9, 1992Date of Patent: August 31, 1993Assignee: Adir et CompagnieInventors: Said Yous, Isabelle Lesieur, Patrick Depreux, Daniel H. Caignard, Beatrice Guardiola, Gerard Adam, Pierre Renard
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Patent number: 5240949Abstract: Compounds of general formula (I): ##STR1## in which: R.sub.1 represents a hydrogen atom or a lower alkyl group,R.sub.2 represents a substituted or unsubstituted alkyl group, a substituted or unsubstituted aryl group, a substituted or unsubstituted alkenyl group, a substituted or unsubstituted thienyl, furyl, pyrrolyl or pyridinyl group,X represents a hydrogen atom,Y represents a hydroxyl group,or else X and Y together represent an oxygen atom, their enantiomers, diastereoisomers and epimers. Medicaments.Type: GrantFiled: March 27, 1992Date of Patent: August 31, 1993Assignee: Adir et CompagnieInventors: Daniel Lesieur, Charles Lespagnol, Said Yous
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Patent number: 5236619Abstract: A mesomorphic compound represented by the following formula (I):R.sub.1 --A.sub.1 --B.sub.1 --A.sub.2 --R.sub.2 (I),wherein R.sub.1 and R.sub.2 respectively denote a linear or branched alkyl group having 3-18 carbon atoms capable of including one or non-neighboring two or more methylene groups which can be replaced with at least one species of ##STR1## wherein Z denotes --O-- or --S-- and R.sub.3 denotes hydrogen or an alkyl group having 1-5 carbon atoms; B.sub.1 denotes ##STR2## A.sub.1 denotes a single bond, ##STR3## A.sub.2 denotes a single bond, --A.sub.3 -- or --A.sub.3 --A.sub.4 -- wherein A.sub.3 and A.sub.4 respectively denote any one of ##STR4## and Y.sub.1 and Y.sub.2 respectively denote any one of hydrogen, fluorine, chlorine, bromine, --CH.sub.3, --CN and --CF.sub.3.Type: GrantFiled: January 22, 1991Date of Patent: August 17, 1993Assignee: Canon Kabushiki KaishaInventors: Takashi Iwaki, Takao Takiguchi, Takeshi Togano, Yoko Yamada, Shinichi Nakamura
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Patent number: 5156667Abstract: Derivatives of 4-((aryloxy)phenoxy)alkenols, their preparation and use as active herbicides for the postemergent control of grassy weeds and especially the control of said weeds in the presence of corn plants are disclosed.Type: GrantFiled: April 12, 1991Date of Patent: October 20, 1992Assignee: DowElancoInventors: James A. Turner, Paul S. Zorner, Wendy S. Jacks
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Patent number: 5152929Abstract: Compounds of the formula I ##STR1## in which X is --S--, --O-- or --NH--, R is H or a monovalent substituent, n is 0 or 1 and R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are H, alkyl, alkyl which is substituted by OH, halogen, COOH or alkoxy, unsubstituted or substituted aryl or aralkyl, or carboxyl, or R.sup.1 and R.sup.2 or R.sup.1 and R.sup.3 together are alkylene or R.sup.1 and R.sup.2 are a direct bond, at least two of the groups R.sup.1, R.sup.2, R.sup.3 and R.sup.4 being carboxyl or carboxyalkyl groups, and base addition salts thereof are effective corrosion inhibitors. The preparation of these novel polycarboxylic acids can be effected by various processes.Type: GrantFiled: October 10, 1990Date of Patent: October 6, 1992Assignee: Ciba-Geigy CorporationInventors: Robert L. Bentley, Michael P. Savage, Kenneth W. Shelton
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Patent number: 5128481Abstract: A pyrazolyl acrylic acid derivative having plant fungicidal activity of formula (I): ##STR1## wherein: R.sub.1 and R.sub.2 are independently hydrogen or C.sub.1 -C.sub.5 alkyl;A is a group of the formula: ##STR2## wherein X is independently hydrogen; halogen; cyano; nitro; C.sub.1 -C.sub.10 alkyl, C.sub.2 -C.sub.11 alkenyl, C.sub.1 -C.sub.10 alkoxy, C.sub.2 -C.sub.11 alkenyloxy, C.sub.2 -C.sub.11 alkynyloxy, C.sub.2 -C.sub.11 alkylcarbonyl or C.sub.2 -C.sub.11 alkylcarbonyloxy optionally substituted with one or more substituents selected from halogen, nitro, cyano, trifluoromethyl and C.sub.1 -C.sub.5 alkoxy; or C.sub.7 -C.sub.13 arylcarbonyl, C.sub.4 -C.sub.9 cycloalkylcarbonyloxy, C.sub.7 -C.sub.13 arylcarbonyloxy, C.sub.6 -C.sub.12 aryl, C.sub.6 -C.sub.12 aryloxy, C.sub.2 -C.sub.13 heteroaryl having 1-3 heteroatom(s) selected from oxygen, sulfur, and nitrogen, C.sub.2 -C.sub.13 heteroaryloxy having 1-3 heteroatom(s) selected from oxygen, sulfur, and nitrogen, C.sub.7 -C.sub.12 aralkyl or C.sub.7 -C.sub.Type: GrantFiled: July 17, 1991Date of Patent: July 7, 1992Assignee: Mitsubishi Kasei CorporationInventors: Masatsugu Oda, Toshiro Sakaki, Kazuhiko Kikutake
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Patent number: 5124342Abstract: A composition for the inhibition of lipoxygenase enzymes comprising a pharmaceutically acceptable carrier and a compound of the formula: ##STR1## wherein R.sub.1 and R.sub.2 are independently selected from the group consisting of alkyl, alkenyl, cycloalkyl, cycloalkenyl, aryl, arylalkyl, arylalkenyl, reduced heteroaryl, and reduced heteroarylalkyl and substituted derivatives thereof having one or more substituents independently selected from the group consisting of halogen, alkyl, halosubstituted alkyl, aryl, arylalkyl, reduced heteroaryl, arylalkoxy, cyano, nitro, COR.sub.4, SO.sub.2 R.sub.4, NR.sub.5 R.sub.6, OR.sub.6, COCX.sub.1 X.sub.2 NR.sub.6 R.sub.7, CON(OH)R.sub.6, NR.sub.6 COR.sub.4, CR.sub.5 (NH.sub.2)CO.sub.2 R.sub.5, NHCX.sub.1 X.sub.2 CO.sub.2 R.sub.5, N(OH)CONR.sub.5 R.sub.6, N(OH)COR.sub.4, NHCONR.sub.5 R.sub.6, C(NOH)NHOH and CONHNR.sub.5 R.sub.6 ;R.sub.3 is selected from the group consisting of hydrogen, a pharmaceutically acceptable salt, COR.sub.4, COCX.sub.1 X.sub.2 NR.sub.6 R.sub.7, CR.Type: GrantFiled: July 18, 1990Date of Patent: June 23, 1992Assignee: Abbott LaboratoriesInventors: Francis A. J. Kerdesky, James H. Holms, Dee W. Brooks
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Patent number: 5103007Abstract: Lipid derivatives represented by the formula: ##STR1## wherein R.sup.1 stands for an optionally substituted higher alkyl group, R.sup.2 stands for an optionally substituted lower alkyl group or an optionally substituted nitrogen-containing heterocyclic group, R.sup.3 stands for a tertiary amino group or a quaternary ammonium group, J stands for oxygen atom or S(O)t (where t deontes 0, 1 or 2), m and n respectively denotes 1 or 2, p denotes 0, 1 or 2, q and r respectively denote an integer of 2 to 5.and salts thereof have antitumor activities including differentiation-inducing activity and are useful as antitumor agents.Type: GrantFiled: October 27, 1989Date of Patent: April 7, 1992Assignee: Takeda Chemical Industries, Ltd.Inventors: Hiroaki Nomura, Hiroshi Akimoto, Keizo Inoue
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Patent number: 5097039Abstract: Compounds of the formula I ##STR1## wherein R, R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 have the meaning given in claim 1 are formed by thermal rearrangement of the isomers of formula V ##STR2## especially in the presence of basic catalysts. The compounds are corrosion inhibitors for organic materials, in particular coating materials and lubricants. In these substrates they also act as antioxidants and light-stabilizers and are very stable to heat.Type: GrantFiled: August 14, 1989Date of Patent: March 17, 1992Assignee: Ciba-Geigy CorporationInventors: Adalbert Braig, Hans-Rudolf Meier, David G. Leppard, Robert C. Wasson, Emyr Phillips
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Patent number: 5093345Abstract: Fungicidal nitro-substituted benzothiazolones of the formula ##STR1## in which R represents alkyl which is monosubstituted or disubstituted by identical or different substituents from the group consisting of cyano, carboxyl, alkylcarbonyl, alkoxycarbonyl, and alkylaminocarbonyl or and phenyl or phenylcarbonyl in each case optionally monosubstituted to pentasubstituted by identical or different substituents from the group consisting of halogen, alkyl, halogenoalkyl and alkoxy, or R is the radical --CONHR.sup.1, in which R.sup.1 represents alkyl which is monosubstituted or disubstituted by identical or different substituents from the group consisting of cyano, carboxyl and alkoxycarbonyl, andX represents hydrogen, halogen, alkyl or halogenoalkyl.Type: GrantFiled: April 2, 1990Date of Patent: March 3, 1992Assignee: Bayer AktiengesellschaftInventors: Klaus Wagner, Gerd Hanssler, Wilhelm Brandes
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Patent number: 5084469Abstract: Compounds of general formula (I): ##STR1## in which: R.sub.1 represents a hydrogen atom or a lower alkyl group, andR.sub.2 represents a substituted or unsubstituted alkyl, a phenyl or a substituted or unsubstituted heteroaryl,their enantiomers, diastereoisomers and epimers and their addition salts with a pharmaceutically acceptable base when R.sub.1 represents a hydrogen atom or when R.sub.2 comprises a carboxylic acid group. Medicinal products.Type: GrantFiled: November 9, 1990Date of Patent: January 28, 1992Assignee: Adir et CompagnieInventors: Isabelle Lesieur, Said Yous, Michelle Devissaguet, Yannis Tsouderos
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Patent number: 5081245Abstract: A compound represented by the formula: ##STR1## wherein R represents a hydrogen atom or a lower alkyl group;R.sup.1 represents a higher alkyl group which may be substituted;R.sup.2 represents a hydrogen atom or a lower alkyl group, a lower alkanoyl group or a nitrogen-containing 5- to 7-membered heterocyclic group each of which may be substituted; X represents a divalent group represented by the formula:--(OCH.sub.2 CH.sub.2).sub.p --wherein p represents an integer of 1 to 5, a divalent group represented by the formula:--O(CH.sub.2).sub.q --wherein q represents an integer of 3 to 8, or a divalent group represented by the formula:--(OCH.sub.2 CH.sub.2).sub.p --J--(CH.sub.2).sub.q --wherein J represents an oxygen atom or a group represented by the formula: --S(O).sub.Type: GrantFiled: August 18, 1989Date of Patent: January 14, 1992Assignee: Takeda Chemical Industries, Ltd.Inventors: Hiroaki Nomura, Hiroshi Akimoto, Eiko Imamiya, Keizo Inoue
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Patent number: 5077309Abstract: Novel compounds have the formula (I) ##STR1## where ##STR2## represents one of the divalent cyclic groups ##STR3## the letters a and b indicating in each case the points of attachment of the substituents R.sup.1 and CV(R.sup.2)-NV'R, respectively; R.sup.1 is a group --(CH.sub.2).sub.b --(A).sub.a --(CH.sub.2).sub.c --B--CH.sub.2 --CO.sub.2 R' in which A and B are each separately oxygen or sulphur, a is 0, b is 0 and c is an integer from 3 to 10, or a is 1, b is 0 or an integer from 1 to 7 and c is an integer from 2 to 9 with the sum of b and c being from 2 to 9, and CO.sub.2 R' is a carboxy group or an amide, ester or salt derivative thereof; V and V' either each separately is hydrogen or together are the second bond of a carbon-nitrogen double bond; R.sup.2 is hydrogen, an aliphatic hydrocarbon group or an aliphatic hydrocarbon group substituted by an aromatic group directly or through an oxygen or sulphur atom; and R is a group --OR.sup.3, --OR.sup.4, --D--R.sup.3, --N.dbd. R.sup.5 or --NW.G.Type: GrantFiled: March 28, 1990Date of Patent: December 31, 1991Assignee: National Research Development CorporationInventors: Robert L. Jones, Norman H. Wilson
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Patent number: 5075300Abstract: A compound of formula (I): ##STR1## or a tautomeric form thereof and/or a pharamaceutically acceptable salt thereof, and/or a pharmaceutically acceptable solvate thereof, wherein:A.sup.1 represents a substituted or unsubstituted aromatic heterocyclyl group;A.sup.2 represents a benzene ring having in total up to five substituents;X represents O, S or NR.sup.1 l wherein R.sup.1 represents a hydrogen atom, an alkyl group, an acyl group, an aralkyl group, wherein the aryl moiety may be substituted or unsubstituted, or a substituted or unsubstituted aryl group;Y represents O or S providing that Y does not represent O when X represents NR.sup.1 ;R.sup.2 and R.sup.3 each represent hydrogen, or R.sup.2 and R.sup.3 together represent a bond; andn represents an integer in the range of from 2 to 6; a process for preparing such a compound; a pharmaceutical composition comprising such a compound; and the use of such a compound and a composition in medicine.Type: GrantFiled: August 25, 1989Date of Patent: December 24, 1991Assignee: Beecham Group p.l.c.Inventors: Richard M. Hindley, David Haigh, Peter T. Duff
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Patent number: 5055582Abstract: This invention relates to a process for preparing useful thromboxane A.sub.2 inhibiting (.+-.)7-[3.alpha.-[1-[[(phenylamino)thioxomethyl]hydrazono]ethyl]-1.alpha. ,4.alpha.-bicyclo[2.2.1]hept-2.beta.-yl]-heptenoic acids and useful derivatives thereof from (.+-.)octahydro-1.alpha.-methyl-3a.alpha.,7a.alpha.-4.alpha.,7.alpha.-meth ano-2H-inden-2-ones.Type: GrantFiled: December 13, 1988Date of Patent: October 8, 1991Assignee: National Research Development CorporationInventors: Robert B. Garland, Masateru Miyano
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Patent number: 5037840Abstract: Compounds having the formula: ##STR1## are leukotriene antagonists and inhibitors of leukotriene biosynthesis. These compounds are useful an anti-asthmatic, antiallergic, anti-inflammatory, and cytoprotective agents.Type: GrantFiled: March 5, 1990Date of Patent: August 6, 1991Assignee: Merck Frosst Canada, Inc.Inventors: Robert N. Young, Robert Zamboni
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Patent number: 5032590Abstract: Substituted hydroxylamines of the formula ##STR1## in which R.sup.1 stands for an aromatic or heterocyclic radical,are especially useful in the treatment of hyperlipoproteinaemia, lipoproteinaemia and atherosclerosis.Type: GrantFiled: March 8, 1990Date of Patent: July 16, 1991Assignee: Bayer AktiengesellschaftInventors: Walter Hubsch, Rolf Angerbauer, Peter Fey, Hilmar Bischoff, Dieter Petzinna, Delf Schmidt
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Patent number: 5028733Abstract: Bicyclooctane and bicycloheptane prostaglandin intermediates have been synthesized.Type: GrantFiled: December 12, 1989Date of Patent: July 2, 1991Assignee: National Research Development CorporationInventors: Robert L. Jones, Norman H. Wilson
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Patent number: 5007952Abstract: Herbicidally active pyrroles of the formula ##STR1## wherein R.sup.1 represents C.sub.1-4 alkyl, or one R.sup.1 together with the other R.sup.1 forms tetramethylene or butenylene,X represents hydrogen or halogen,Y represents O or S,n represents 0 or 1,R.sup.2 represents hydrogen or an organic radical.Type: GrantFiled: November 9, 1989Date of Patent: April 16, 1991Assignee: Nihon Tokushu Noyaku Seizo K.K.Inventors: Toyohiko Kume, Toshio Goto, Atsumi Kamochi, Akihiko Yanagi, Hiroshi Miyauchi, Tadao Asami
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Patent number: 5006541Abstract: Compounds of the formula ##STR1## where Y is alkyl, aryl or heterocyclic, n is 1-7, R is hydrogen, alkyl, aralkyl or carboxymethyl, R.sub.1 is acetoxy, thiophenoxy, hydrogen, halo, alkyl, alkoxy or trifluoromethyl, R.sub.2 is hydrogen, alkyl or alkanoyl and X is C.dbd.O, CH.sub.2, NH, O or S as antiallergy and antiinflammatory agents.Type: GrantFiled: October 25, 1989Date of Patent: April 9, 1991Assignee: Pfizer Inc.Inventors: Yoshihiko Kitaura, Fumitaka Ito, Rodney W. Stevens, Nobuko Asai
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Patent number: 5003073Abstract: Process for the production of known 2-oximinoacetamido-3-cephem-4-carboxylic derivatives comprising acylation of 7-amino-3-cephem-4-carboxylic acid derivatives with novel 2-oximinoacetic acid thio esters, as well as such thioesters and their production.Type: GrantFiled: July 24, 1989Date of Patent: March 26, 1991Assignee: Sandoz Ltd.Inventor: Gerd Ascher
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Patent number: 4987146Abstract: N-hetaryl imidazole derivatives of general Formula I ##STR1##are disclosed in whichHet represents an optionally substituted monocyclic or bicyclic heteroaromate,R.sup.3 represents hydrogen, a straight or branched C.sub.1-6 -alkyl group, or a C.sub.1-6 -alkoxy-alkyl group, andR.sup.4 represents --COOR.sup.5 --CONR.sup.6 R.sup.7 --CN, ##STR2##with R.sup.5 meaning hydrogen, a straight or branched C.sub.1-6 -alkyl group, R.sup.6 and R.sup.7 are the same of different and represent hydrogen or a straight, branched, or cyclic alkyl group with up to 7 carbon atoms or, together with the nitrogen atom, form a saturated five or six ring optionally containing another heteroatom and R.sup.8 means hydrogen or a straight, branched or cyclic alkyl group with up to 7 carbon atoms.Type: GrantFiled: July 14, 1989Date of Patent: January 22, 1991Assignee: Schering AktiengesellschaftInventors: Ralph Rohde, Helmut Biere, Ralph Schmiechen, John S. Andrews, David N. Stephens
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Patent number: 4968844Abstract: Retinal is prepared by condensing a C.sub.15 sulphide of formula: ##STR1## in which R.sub.1 denotes aryl, aralkyl, pyridyl, 2-thiazolyl, 2-benzothiazolyl, 2-benzimidazolyl or 2-benzoxazolyl, with a haloacetal of formula: ##STR2## in which X denotes a halogen atom and R denotes an alkyl radical containing 1 to 4 carbon atoms, to give a C.sub.20 sulphide acetal of formula: ##STR3## in which R.sub.1 and R are defined as above, hydrolysing the said sulphide acetal to give a C.sub.20 sulphide aldehyde of formula: ##STR4## in which R.sub.1 is defined as above, desulphurizing the said sulphide aldehyde to give retinal, and isolating the retinal obtained.Type: GrantFiled: October 27, 1988Date of Patent: November 6, 1990Assignee: Centre National de la Recherche Scientifique (C. N. R. S.)Inventor: Marc Julia
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Patent number: 4968681Abstract: Substituted hydroxylamines of the formula ##STR1## in which R.sup.1 stands for an aromatic or heterocyclic radical, are especially useful in the treatment of hyperlipoproteinaemia, lipoproteinaemia and atherosclerosis.Type: GrantFiled: November 15, 1988Date of Patent: November 6, 1990Assignee: Bayer AktiengesellschaftInventors: Walter Hubsch, Rolf Angerbauer, Peter Fey, Hilmar Bischoff, Dieter Petzinna, Delf Schmidt
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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: 4897481Abstract: One of the routes to prepare optically active 2-(4-aryloxyphenoxy)propionic acid ester herbicide is to couple optically active 2-(4-hydrophenoxy)propionic acid esters with halogenated aromatic or heteroaromatic compounds. Conversion of the optically active 2-(4-hydroxyphenoxy)propionic acid ester into the acid salt prior to the coupling step effectively prevents the racemization that unexpectedly occurs otherwise.Type: GrantFiled: May 31, 1988Date of Patent: January 30, 1990Assignee: The Dow Chemical CompanyInventors: Larry D. Kershner, Jimmy J. Tai
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Patent number: 4888428Abstract: A compound of the formula: ##STR1## wherein R is a hydrogen atom, a C.sub.1 -C.sub.5 alkyl group, a C.sub.3 -C.sub.4 alkenyl group, a C.sub.3 -C.sub.4 alkynyl group, a halo(C.sub.1 -C.sub.4)alkyl group, a halo(C.sub.3 -C.sub.4)alkenyl group, a halo(C.sub.3 -C.sub.4)alkynyl group, a C.sub.1 -C.sub.2 alkoxy(C.sub.1 -C.sub.2) alkyl group, a C.sub.1 -C.sub.2 alkoxy(C.sub.1 -C.sub.2)alkoxy(C.sub.1 -C.sub.2)alkyl group, a cinnamyl group, a cyano(C.sub.1 -C.sub.3)alkyl group, a carboxy(C.sub.1 -C.sub.3)alkyl group, a C.sub.1 -C.sub.5 alkoxycarbonyl(C.sub.1 -C.sub.3)alkyl group, a halo(C.sub.1 -C.sub.5)alkoxycarbonyl(C.sub.1 -C.sub.3)alkyl group, a C.sub.1 -C.sub.2 alkoxyalkoxycarbonyl(C.sub. 1 -C.sub.3)alkyl group, a C.sub.1 -C.sub.2 alkoxy (C.sub.1 -C.sub.2)alkoxycarbonyl(C.sub.1 -C.sub.3)alkyl group, a C.sub.1 -C.sub.5 alkoxycarbonyl(C.sub.1 -C.sub.2)-alkoxycarbonyl(C.sub.1 -C.sub.3)alkyl group, a cyclo(C.sub.3 -C.sub.6)alkoxycarbonyl(C.sub.1 -C.sub.3)alkyl group, a C.sub.1 -C.sub.5 alkylaminocarbonyl(C.sub.1 -C.Type: GrantFiled: October 21, 1987Date of Patent: December 19, 1989Assignee: Sumitomo Chemical Company, LimitedInventors: Toru Haga, Eiki Nagano, Ryo Sato, Kouichi Morita
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Patent number: 4873346Abstract: The present invention provides certain novel substituted benzothiazoles, benzimidazoles and benzoxazoles which are useful as inhibitors of leukotriene biosynthesis and/or as inhibitors of the action of lipoxygenase and/or as inhibitors of mucus secretion in mammalian metabolism. They are thus employed wherever it is medically necessary or desirable to inhibit these systems.Type: GrantFiled: September 20, 1985Date of Patent: October 10, 1989Assignee: The Upjohn CompanyInventor: David J. Anderson
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Patent number: 4873338Abstract: Compounds corresponding to Formula I ##STR1## wherein R.sup.1 denotes an acyl group andX denotes hydrogen, halogen, alkoxy, aroxy, SO.sub.3 H or a heterocyclic group attached through --O-- or --N<are prepared form a compound corresponding to Formula II ##STR2## wherein X has the meaning already indicated and Q denotes the group required for completing a dicarbonimide ringby reduction of the said compound to the amino compound and acylation into a compound corresponding to Formula III ##STR3## wherein X, Q and R.sup.1 have the meanings indicatedfollowed by conversion of the compound corresponding to Formula III into a compound corresponding to Formula I by hydrazinolytic or hydrolytic decomposition of the dicarbonimide ring.Type: GrantFiled: November 23, 1987Date of Patent: October 10, 1989Assignee: Agfa-Gevaert AktiengesellschaftInventors: Heinz Wiesen, Erich Wolff