The Chalcogen, X, Is In A -c(=x)- Group Patents (Class 546/267)
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Patent number: 5112386Abstract: Acrylic acid derivatives having the formula (I): ##STR1## and stereoisomers thereof, wherein W is R.sup.1 O.sub.2 C--C.dbd.CH--ZR.sup.2, R.sup.1 and R.sup.2 are alkyl or fluoroalkyl groups, and Z is oxygen or sulphur, A, B, D and E are hydrogen, halogen, hydroxy or optionally substituted alkyl, alkoxy, aralkyl, arylalkoxy, alkenyl, alkynyl, aryl, aryloxy, arylthio, heteroaryloxy, heteroarylthio, acyloxy, amino, arylazo or acylamino, nitro, cyano, --CO.sub.2 R.sup.3, --CONR.sup.3 R.sup.4, --COR.sup.3, --CR.sup.3 .dbd.NR.sup.4, --N.dbd.CR.sup.3 R.sup.4 --S(O).sub.n R.sup.3 groups; any two of the groups, A, B, D and E, when they are in adjacent positions on the ring, optionally join to form a fused ring, n is 0, 1 or 2; and R.sup.3 and R.sup.4 are hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, alkynyl or optionally substituted aryl or aralkyl; and metal complexes thereof. These compounds are useful as fungicides, insecticides, nematicides or plant growth regulators.Type: GrantFiled: December 30, 1988Date of Patent: May 12, 1992Assignee: Imperial Chemical Industries PLCInventors: Anthony Vivienne, John M. Clough, Paul deFraine, Christopher R. A. Godfrey, Patrick J. Crowley, Kenneth Anderton
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Patent number: 5100460Abstract: Herbicides of formula: ##STR1## in which: n=0,1, 2f=0,1A is chosen from the groups ##STR2## in which: Ar is chosen from the groups ##STR3## B is chosen from optionally substituted C.sub.1 -C.sub.10 alkyl and C.sub.3 -C.sub.Type: GrantFiled: July 13, 1989Date of Patent: March 31, 1992Assignee: Rhone-Poulenc AgrochimieInventors: Philippe Desbordes, Michel Euvrard
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Patent number: 5089168Abstract: Optically active nitrogen-containing heterocycles of the formula I according to claim 1 are suitable as components for ferroelectric liquid crystalline materials.Type: GrantFiled: May 16, 1989Date of Patent: February 18, 1992Assignee: Merck Patent Gesellschaft mit beschrankter HaftungInventors: Joachim Krause, Rudolf Eidenschink, Klaus Bofinger, Reinhard Hopf, Volker Reiffenrath, Eike Poetsch, Bernhard Scheuble, Thomas Geelhaar
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Patent number: 5079361Abstract: Cross-linking reagents which are highly specific for sulphydryl groups and react with thiols at an excellent rate. The essential feature of the reagents is at least one vinyl group conjugated with an armoatic nitrogen heterocycle. Particular examples include vinyl pyridines, vinyl pyrimidines and vinyl triazines.Type: GrantFiled: September 9, 1988Date of Patent: January 7, 1992Assignee: Celltech LimitedInventors: Rikki P. Alexander, Michael A. W. Eaton, Thomas A. Millican, Richard C. D. Titmas
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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: 5047535Abstract: The invention relates to novel compounds which are suited for the production of multilayer films which have piezoelectric, and pyroelectric properties, and which provide second harmonic generation. The novel compounds are amphiphilic and it is possible to prepare from same polar single-layer and multi-layer films by depositing them on a substrate. When such substrate is a solid support, polar Z-type Langmuir-Blodgett films are obtained. Upon compression of films of such compounds, at an air/water interface, stable Langmuir monolayers are formed.Type: GrantFiled: August 5, 1987Date of Patent: September 10, 1991Assignee: Yeda Research and Development Company LimitedInventors: Meir Lahav, Leslie Leiserowitz, Jacob Sagiv, Ronit Popovitz-Biro, Karlheinz Hill, Ehud Landau
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Patent number: 5045550Abstract: Substituted tetrahydropyridines and derivatives thereof are described, as well as methods for the preparation and pharmaceutical composition of same, which are useful as central nervous system agents and are particularly useful as dopaminergic, antipsychotic, and antihypertensive agents as well as for treating hyperprolactinaemia-related conditions and central nervous system disorders.Type: GrantFiled: September 20, 1990Date of Patent: September 3, 1991Assignee: Warner-Lambert Co.Inventors: Juan C. Jaen, David G. Nickell, Donna M. Reynolds, Sarah J. Smith, Lawrence D. Wise, David J. Wustrow
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Patent number: 5002957Abstract: Azaneophyl and silazaneophyl sulfides, processes for their preparation, agents containing them, and their use as pesticides.Compounds of the formula I, their optical isomers and mixtures thereof ##STR1## where M denotes C or Si,R.sup.1 denotes unsubstituted or substituted pyridyl, unsubstituted or substituted pyrimidyl, andwhen M=C- denotes unsubstituted or substituted pyridazinyl, unsubstituted or substituted pyrazinyl, unsubstituted or substituted 1,2,4-triazinyl, unsubstituted or substituted 1,2,4,5-tetrazinyl,R.sup.2, R.sup.3 independently or one another denote alkyl, alkenyl, haloalkyl, phenyl, or R.sup.2 and R.sup.3 denote an alkylene chain which - together with the quaternary central atom (M) - form an unsubstituted or fluorine-substituted ring having four to six ring members (when M=Si) or having three to six ring members (when M=C),R.sup.4 denotes H, F, --CN, --CCl.sub.3, --C.dbd.CH, (C.sub.1 -C.sub.4)alkyl, ##STR2## R.sup.Type: GrantFiled: March 23, 1989Date of Patent: March 26, 1991Assignee: Hoechst AktiengesellschaftInventors: Hans H. Schubert, Gerhard Salbeck, Hans-Peter Krause, Werner Knauf, Anna Waltersdorfer, Manfred Kern
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Patent number: 4973696Abstract: A stereoselective process is described for preparing optically active alpha,beta-disubstituted carbonyl compounds, comprising forming an acetal between an alpha,beta-unsaturated aldehyde or ketone and tartaric acid or a derivative thereof, halogenating the product thus obtained, and restoring the carbonyl compound.Type: GrantFiled: January 17, 1989Date of Patent: November 27, 1990Assignee: Zambon S.p.A.Inventors: Claudio Giordano, Graziano Castaldi, Silvia Cavicchioli, Francesco Minisci
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Patent number: 4970313Abstract: A process for the preparation of optically active 3-de-methylmevalonic acid derivatives, and intermediates A process for the preparation of optically active 3-de-methylmevalonic acid derivatives of the formula I ##STR1## (3,5-dihydroxy carboxylic acid derivatives) or of the formula II ##STR2## (.beta.-hydroxy lactones) in which R, R.sup.1 and Y have the indicated meanings, is described. The invention furthermore relates to aldehydes of the formula XII ##STR3## in which M represents the indicated protective groups. The 3-demethylmevalonic acid derivatives of this invention are useful for lowering cholesterol levels of a host.Type: GrantFiled: December 6, 1988Date of Patent: November 13, 1990Assignee: Hoechst AktiengesellschaftInventors: Gunther Wess, Kurt Kesseler, Ekkehard Baader, Gerhard Beck
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Patent number: 4929751Abstract: A vinyl tricarbonyl compound of the formula ##STR1## or its monohydrate of the formula ##STR2## wherein R.sub.1 is a hydrogen, halogen, unsubstituted or substituted C.sub.1 to C.sub.30 alkyl, unsubstituted or substituted aryl, arylalkyl, and cycloalkyl with 3 to 7 carbon atoms,R.sub.2 is hydrogen, halogen, unsubstituted or substituted C.sub.1 to C.sub.30 alkyl, unsubstituted or substituted aryl, arylalkyl, cycloalkyl with 3 to 7 carbon atoms, cyano, nitro, or a heterocyclic,R.sub.3 is hydrogen, halogen, unsubstituted or substituted C.sub.1 to C.sub.30 alkyl, unsubstituted or substituted aryl, arylalkyl, cycloalkyl with 3 to 7 carbon atoms, cyano, nitro, or a heterocyclic, andR.sub.4 is unsubstituted or substituted C.sub.1 to C.sub.30 alkyl, unsubstituted or substituted aryl, arylalkyl, cycloalkyl are 3 to 7 carbon atoms. Such vinyl tricarbonyl compound is effective against tumor cells.Type: GrantFiled: October 19, 1987Date of Patent: May 29, 1990Assignee: Yale UniversityInventors: Harry H. Wasserman, Natesan Murugesan, John H. Van Duzer
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Patent number: 4908451Abstract: A process is disclosed for the preparation of .alpha.-substituted carbonyl compounds, wherein .alpha.-substituted ketone is prepared by the following reaction: ##STR1## .alpha.-azo ester is prepared by the following reaction: ##STR2## and .alpha.-hydrozono ester is prepared by the following reaction: ##STR3## wherein the .alpha.-azo ester and .alpha.-hydrazono ester obtained by the above reactions include novel compounds, which are also disclosed.Type: GrantFiled: March 23, 1988Date of Patent: March 13, 1990Assignee: Agency of Industrial Science and TechnologyInventors: Masato Tanaka, Toshiyasu Sakakura
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Patent number: 4894181Abstract: Carbocyclic compounds of the formula I ##STR1## wherein Q is a benzene or cyclohexane ring or a naphthalene system, X is in each case --CH.sub.2 --(CH.sub.2).sub.p -- where it is also possible for one or two non-adjacent CH.sub.2 groups to be replaced by --O--, --S--, --CO--, --O--CO--, --CO--O-- or --CH.dbd.CH--,p is 0, 1 or 2,A.sup.1 and A.sup.2 independently of one another are each a 1,4-phenylene group which is unsubstituted or monosubstituted or polysubstituted by halogen atoms and/or CH.sub.3 groups and/or CN groups and in which it would also be possible for one or more CH groups to be replaced by N atoms, a 1,4-cyclohexylene group wherein it would also be possible for one or two non-adjacent CH.sub.2 groups to be replaced by --O-- and/or --S--, a piperidine-1,4-diyl group or a 1,4-bicyclo[2.2.2]octylene group,Z is --CO--O--, --O--CO--, --O--, --CH.sub.2 --, --CH.sub.2 O--, --OCH.sub.2 --, --CH.sub.2 CH.sub.2 --, --CHCN--CH.sub.2 --, --CH.sub.2 --CHCN--, --CH.dbd.CH--, --CH.dbd.N--, --N.dbd.CH--, --NO.Type: GrantFiled: May 16, 1988Date of Patent: January 16, 1990Assignee: Merck Patent Gesellschaft Mit Beschrankter HaftungInventors: Klaus Praefcke, Bernd Kohne, Eike Poetsch
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Patent number: 4889865Abstract: Mono, di and tri-esters of 1,8-dihydroxy-10-phenyl-9-anthrone or -9-anthranol have the formula ##STR1## wherein p is 0 or 1,(a) when p=0, t=1 and R.sub.2 represents hydrogen or --COR.sub.3,(b) when p=1, t=0 and R.sub.1 and R.sub.2 each independently represent hydrogen or --COR.sub.3,R.sub.3 represents linear or branched alkyl having 1-17 carbon atoms, cycloalkyl, phenyl or phenyl substituted by lower alkyl, lower alkoxy, halogen, a nitro function, --CF.sub.3 or a hydroxyl function, and mixtures of said esters. These esters are prepared by reacting 1,8-dihydroxy-10-phenyl-9-anthrone with an activated form of an acid. The esters are useful in human or veterinary medicine and in cosmetic compositions.Type: GrantFiled: February 21, 1989Date of Patent: December 26, 1989Assignee: Centre International de Recherches Dermatologiques C.I.R.D.Inventors: Braham Shroot, Gerard Lang, Jean Maignan, Serge Restle, Christopher Hensby, Michel Colin
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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: 4870174Abstract: The synthesis of 7-n-alkyl-imidazolium[4,5-d]-pyrimidines, 6-substituted-3n-alkyl-benzimidazolium- and 3n-alkyl-5,6-substituted-benzthiazolium salts are described. There N.sup.+ -surfactants having a substituted heterocycle as a head group have distinguished small critical micelle concentrations (CMC) in the range of 10.sup.-5 -10.sup.-7 Mol/Liter. The size and shape of these micelles in watery solutions are determined by the nature of the anion. The N-surfactants can be used as pharmaceuticals as well as reporter groups in fluorescence studies including immunological assays.Type: GrantFiled: August 6, 1987Date of Patent: September 26, 1989Assignee: Medice chem.-pharm. FabrikInventor: Henrich H. Paradies
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Patent number: 4868181Abstract: 1,4-Dihydropyridine derivatives which combine both calcium agonist and alpha.sub.1 -antagonist activity are useful in treating congestive heart failure. These derivatives are compounds having the formula: ##STR1## wherein Ar, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are defined in the specification.Type: GrantFiled: June 30, 1987Date of Patent: September 19, 1989Assignee: E. I. Du Pont de Nemours and CompanyInventors: Alexander L. Johnson, Philip Ma, Petrus B. M. W. M. Timmermans, Ruth R. Wexler
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Patent number: 4843083Abstract: A 2-pyridylacetic acid derivative having the formula (I): ##STR1## wherein R.sup.1 represents an alkyl having 5 to 10 carbon atom or --(CH.sub.2).sub.m --cycloalkyl group having C.sub.5 -C.sub.8 cycloalkyl, which may be substituted with at least one alkyl group having 1 to 6 carbon atoms, where m represents zero or an integer of 1 to 4; R.sup.2 represents hydrogen, a linear alkyl, a hydroxyalkyl group, an alkenyl, an aryl, an aralkyl or a group--(CH.sub.2)--A, where n represents an integer of 0 to 3 and A represents a nitrogen-containing heterocyclic group which may be replaced by an alkyl having 1 to 10 carbon atoms or an aralkyl having 7 to 10 carbon atoms and a pharmacologically acceptable acid addition salt thereof, which has the effects of both an inhibition of gastric acid and a protection of gastric mucosa, and which has a low toxicity.Type: GrantFiled: March 3, 1988Date of Patent: June 27, 1989Assignee: Suntory LimitedInventor: Mitsuhito Okitsu
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Patent number: 4834904Abstract: Optically active nitrogen-containing heterocycles of the formula I according to claim 1 are suitable as components for ferroelectric liquid crystalline materials.Type: GrantFiled: December 24, 1986Date of Patent: May 30, 1989Assignee: Merck Patent Gesellschaft mit Beschrankter HaftungInventors: Joachim Krause, Rudolf Eidenschink, Klaus Bofinger, Bernhard Scheuble, Thomas Geelhaar
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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: 4777179Abstract: The invention provides compounds of the general formula ##STR1## and physiologically acceptable salts and hydrates thereof, in which one of R.sub.1 and R.sub.2 represents hydrogen, halogen or a C.sub.1-4 alkyl group which may be optionally substituted by hydroxy or C.sub.1-4 alkoxy, and the other represents the group R.sub.4 R.sub.5 NAlk-- in which Alk represents a straight or branched alkylene chain of 1 to 6 carbon atoms;R.sub.3, which may be in either the 2 or 3-position, represents the ##STR2## where X represents --CH.sub.2 --, --O-- or --S--; n represents zero, 1 or 2;m represents 2, 3 or 4; andR.sub.7 represents hydrogen, alkyl, alkenyl, aralkyl, or C.sub.2-6 alkyl substituted by hydroxy or alkoxy; andR.sub.8 represents hydrogen, alkyl, alkenyl, aralkyl, hydroxyalkyl, acyloxyalkyl, alkoxyalkyl, aryloxyalkyl, aralkyloxyalkyl, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, hydroxy or alkoxy, or the group NR.sub.10 R.sub.11 ; with the provisos thatwhere R.sub.2 represents the group R.sub.4 R.sub.Type: GrantFiled: October 21, 1985Date of Patent: October 11, 1988Assignee: Glaxo Group LimitedInventors: John Bradshaw, Duncan B. Judd, Barry J. Price, John W. Clitherow, John W. M. Mackinnon, Linda Carey, Roger Hayes
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Certain pyridyl alkenoic acid derivatives which inhibit the action of thromboxane A.sub.2 synthetase
Patent number: 4760068Abstract: Novel compound of the formula: ##STR1## wherein R.sup.1 is pyridyl group, R.sup.2 is a phenyl group, a thienyl group, a furyl group, a naphthyl group, a benzothienyl group or pyridyl group, which may optionally have a lower alkoxy group, a lower alkyl group, a halogen atom, trifluoromethyl group, a lower alkenyl group or methylenedioxy group, R.sup.3 is hydrogen atom or a lower alkyl group, and n is an integer of 0 to 6, Y is sulphur atom, methylene group or a group of the formula: ##STR2## wherein R.sup.4 is hydrogen atom or acetyl group, and m is 0 or 1, and their pharmaceutically acceptable salts having an inhibitory action on bio-synthesis of thromboxane A.sub.2 (TXA.sub.2) and an effect of accelerating the productivility of prostaglandin I.sub.2 (PGI.sub.2), and can be used for mammals to the prophylaxis or therapy of thrombosis caused by platelet aggregation or ischemic diseases caused by vasospasms in cardiac, cerebral and peripheral circulatory system (e.g.Type: GrantFiled: June 6, 1986Date of Patent: July 26, 1988Assignee: Takeda Chemical Industries, Ltd.Inventors: Shinji Terao, Kohei Nishikawa -
Patent number: 4727078Abstract: Novel compound of the formula: ##STR1## wherein R.sup.1 is pyridyl group, R.sup.2 is a phenyl group, a thienyl group, a furyl group, a naphthyl group, a benzothienyl group or pyridyl group, which may optionally have a lower alkoxy group, a lower alkyl group, a halogen atom, trifluoromethyl group, a lower alkenyl group or methylenedioxy group, R.sup.3 is hydrogen atom or a lower alkyl group, and n is an integer of 0 to 6, Y is sulphur atom, methylene group or a group of the formula: ##STR2## wherein R.sup.4 is hydrogen atom or acetyl group, and m is 0 or 1, and their pharmaceutically acceptable salts have an inhibitory action on bio-synthesis of thromboxane A.sub.2 (TXA.sub.2) and an effect of accelerating the productivility of prostaglandin I.sub.2 (PGI.sub.2), and can be used for mammals to the prophylaxis or therapy of thrombosis caused by platelet aggregation or ischemic diseases caused by vasospasms in cardiac, cerebral and peripheral circulatory system (e.g.Type: GrantFiled: June 9, 1983Date of Patent: February 23, 1988Assignee: Takeda Chemical Industries, Ltd.Inventors: Shinji Terao, Kohei Nishikawa
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Patent number: 4719221Abstract: A class of novel thiosemiarbazones has been found to be active against a number of protozoa which cause serious diseases, mainly in the tropical areas of the world.Type: GrantFiled: July 27, 1984Date of Patent: January 12, 1988Assignee: Burroughs Wellcome Co.Inventor: Jr. Morrison
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Patent number: 4650890Abstract: 7-Substituted lower alkyl hept-6-enoates and 4-hydroxy-tetrahydropyran-2-ones bearing 6-olefinic substituents (E), (Z), ethyl erythro-3,5-dihydroxy-7-phenyl-hept-6-enates are prepared by a multi-step process involving lower alkyl 3,5-dihydroxy-hept-6-enates. The final products are useful as anti hypercholesteremic agents.Type: GrantFiled: July 26, 1985Date of Patent: March 17, 1987Assignee: Sandoz Corp.Inventors: Charles F. Jewell, Jr., James R. Wareing
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Patent number: 4555574Abstract: A methacrylic ester which functions as the main unit of a polymer or copolymer which is useful as an agent to optically resolve racemic mixtures of compounds.Type: GrantFiled: July 11, 1984Date of Patent: November 26, 1985Assignee: Daicel Chemical Industries, Ltd.Inventors: Heimei Yuki, Yoshio Okamoto
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Patent number: 4522943Abstract: Compounds of the formula ##STR1## wherein R.sup.12 is a leaving group, Z is S, O or CH.sub.2 and A is a phenyl, furyl, thienyl or pyridyl ring substituted by a ##STR2## moiety, in which R.sup.8 and R.sup.9 are various substituents or, when taken together with the nitrogen, may be a specified heterocyclic ring, are intermediates in the preparation of histamine H.sub.2 -antagonist anti-ulcer agents of the formula ##STR3## in which R.sup.1 and R.sup.2 are any of several specified substituents.Type: GrantFiled: April 21, 1982Date of Patent: June 11, 1985Assignee: Bristol-Myers CompanyInventors: Aldo A. Algieri, Ronnie R. Crenshaw
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Patent number: 4518602Abstract: Novel compound of the formula: ##STR1##wherein R.sup.1 is a pyridyl group; R.sup.2 is a phenyl, thienyl, furyl, naphthyl, benzothienyl or pyridyl group which may have as a substituent a lower alkoxy, a lower alkyl, a halogen, trifluoromethyl, a lower alkenyl or methylenedioxy; R.sup.3 is hydrogen, benzyl or a lower alkyl; one of R.sup.4 and R.sup.5 is hydrogen or a lower alkyl, and the other is an aryloxy, or lower aliphatic hydrocarbon, an alicyclic hydrocarbon having not more than 6 carbon atoms or an aromatic group which may have a substituent, or a group represented by the formula, --S(O).sub.m --R.sup.6 (in which R.sup.6 is phenyl or a lower alkyl group; m is an integer of 0 to 2), or R.sup.4 and R.sup.5 each combine with the other to represent one alkylene group; n is an integer of 2 to 6, or a pharmaceutically acceptable salt thereof has a selective inhibitory action on bio-synthesis of thromboxane A.sub.2 (TXA.sub.2) and an effect of enhancing the production of prostaglandin I.sub.2 (PGI.sub.Type: GrantFiled: September 30, 1983Date of Patent: May 21, 1985Assignee: Takeda Chemical Industries, Ltd.Inventors: Shinji Terao, Kohei Nishikawa
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Patent number: 4513137Abstract: Mono- or bis(iodonium salts) are produced in neutral organic solvents by the reaction of an [hydroxy (organosulfonyloxy)iodo]arene with a bis(triorganosilyl)arene, a bis(trihalosilyl)arene, or with a mono- or bis(triorganosilyl)heterocyclic compound, or a mono- or bis(trihalosilyl)heterocyclic. The iodonium salts are made under conditions of regiospecific control.Type: GrantFiled: April 9, 1981Date of Patent: April 23, 1985Assignee: The University of AkronInventors: Gerald F. Koser, Carol S. Carman
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Patent number: 4507306Abstract: cis-4a-Aryl-1,2,3,4,4a,9b-hexahydro-benzofuro[3,2-c]pyridines and methods of preparing same are described. On the nitrogen atom there may be a substituent including loweralkyl, loweralkenyl, phenylloweralkyl, hydrogen, cyanoloweralkyl, phenylcarbonylloweralkyl, phenoxyloweralkyl and cycloalkylloweralkyl. The 4a-aryl group may be a phenyl, mono-halogen substituted phenyl, tolyl, methoxyphenyl, hydroxyphenyl, or furyl. These compounds are useful as analgesic and anticonvulsant agents.3-o-Fluorophenyl-1-methyl-4-aryl-4-piperidinols which are useful as intermediates for preparing the aforementioned compounds and methods for preparing same are also described.Type: GrantFiled: July 22, 1982Date of Patent: March 26, 1985Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventor: Solomon S. Klioze
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Patent number: 4479950Abstract: Compounds of the structure ##STR1## wherein: P and Q are independently hydrogen, halo, CF.sub.3, OR.sub.1, SR.sub.1, sulfamoyl, alkyl and NR.sub.1 R.sub.2 ;R.sub.1, and R.sub.2 are independently hydrogen, alkyl, aminoalky, aryl, aralkyl, heteroaryl or cycloalkyl;Y is OH, OR.sub.1, NH.sub.2, or, N(R.sub.1 R.sub.2); andM is alkyl, cycloalkyl, aryl, aminoalkyl, aralkyl, heteroaryl or heterocyclicwherein:the alkyl groups and the alkyl moieties of aminoalkyl, alkoxy and thioalkyl contain from 1 to 6 carbon atoms; the cycloalkyl group contains from 3 to 8 carbon atoms; the aryl group contains from 6 to 10 carbon atoms; the aralkyl group contains from 7 to 16 carbon atoms; and the hetero group is selected from pyrrolidyl, piperidinyl, morpholinyl, pyridyl, quinolinyl, furyl, furfuryl and thienyl; and where Y is a hydroxy, their pharmaceutically acceptable, non-toxic alkali, alkaline earth and amine salts, have angiotensin converting enzyme inhibitory activity.Type: GrantFiled: November 5, 1982Date of Patent: October 30, 1984Assignee: USV Pharmaceutical CorporationInventors: Paul R. Menard, Howard Jones, John T. Suh
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Patent number: 4468352Abstract: The distyrylbiphenyls of the formula ##STR1## in which X and X' independently of one another are a direct bond, oxygen, sulfur, --O--C.sub.1-3 -alkylene-CON(R.sub.4)----CON(R.sub.4)--, --O--C.sub.1-3 -alkylene-COO--, OCO or --COO--, with the proviso that if n+n'=O, X and Y' may not be --CON(R.sub.4)-- or O--C.sub.1-3 -alkylene-CON(R.sub.4)--, and if n+n'=2 and X and X' are --CON(R.sub.4)-- or --COO--, A.sup..crclbar. may not be a phosphite or phosphonate anion, and Y and Y' independently of one another are C.sub.1-20 -alkylene, R.sub.1 and R.sub.1 ' independently of one another are unsubstituted or substituted C.sub.1-8 -alkyl or C.sub.3-4 -alkenyl, or R.sub.1 together with R.sub.2, or R.sub.1 ' together with R.sub.2 ', is a heterocyclic ring, R.sub.2 and R.sub.2 ' independently of one another are unsubstituted or substituted C.sub.1-8 -alkyl or C.sub.3-4 -alkenyl, or R.sub.2 together with R.sub.1, or R.sub.2 ' together with R.sub.1 ', is a heterocyclic ring, or R.sub.1 and R.sub.2, or R.sub.1 ' and R.sub.Type: GrantFiled: April 28, 1982Date of Patent: August 28, 1984Assignee: Ciba-Geigy CorporationInventors: Christian Luthi, Hans R. Meyer, Kurt Weber
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Patent number: 4455437Abstract: Herbicidally effective aminoalkyl esters of 2-nitro-5-(o-chloro-p-trifluoromethylphenoxy)-benzoic acid, and acid addition salts and quaternary ammonium salts thereof, are suitable for the selective control of weeds in crops of useful plants, for example soya bean and rice crops.The aminoalkyl esters correspond to the formula ##STR1## wherein A is a C.sub.2 -C.sub.4 -alkylene bridge or the direct bond, and ##STR2## is an open amino group, and ##STR3## is a cyclic amino group.Type: GrantFiled: December 28, 1979Date of Patent: June 19, 1984Assignee: Ciba-Geigy CorporationInventors: Dieter Durr, Otto Rohr, Beat Bohner
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Patent number: 4424359Abstract: Vinyl-substituted 2,2'-bipyridine compounds of the formula ##STR1## and complexes thereof with metals or metal compounds other than alkali metals or alkaline earth metals, or alkali metal compounds, or alkaline earth metal compounds are described, R.sub.1 and R.sub.2 being as defined in patent claim 1 and the vinyl group being bonded in the 4-position or 6-position. The 2,2'-bipyridine compounds (I) are suitable for the preparation of complex-forming or complexed, crosslinked or uncrosslinked polymers. Complexed polymers, obtainable from these, are used, for example, as catalysts, in particular for transvinylation reactions. Uncomplexed polymers, which can be prepared from compounds (I), are suitable as metal ion scavengers in various applications.Type: GrantFiled: July 27, 1981Date of Patent: January 3, 1984Assignee: Ciba-Geigy CorporationInventors: Ju/ rgen Kaschig, Dieter Lohmann
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Patent number: 4391812Abstract: Antimicrobial agents suitable for use in aqueous systems for their preservation against biodeterioration include substitutedpiperidinomethylpropenenitriles and propanenitriles. The unsaturated compounds are prepared by reaction of a suitable piperidine with cyano acetic acid and formaldehyde: the propane derivatives therefrom by nucleophilic addition.Type: GrantFiled: March 24, 1982Date of Patent: July 5, 1983Assignee: Merck & Co., Inc.Inventors: Richard A. Dybas, Nathaniel Grier, Bruce E. Witzel
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Patent number: 4355167Abstract: This invention is directed to telomeric quaternary salt compositions of the formula[A.sub.x B.sub.y ].sub.Zwherein A is a segment selected from vinyl monomers, B is a quaternary salt segment, x and y are numbers representing mole fractions of A and B, the sum of x and y being equal to 1, and Z represents the degree of polymerization, wherein there results a telomeric quaternary salt having a number average molecular weight of from about 1,000 to about 10,000.Type: GrantFiled: May 1, 1981Date of Patent: October 19, 1982Assignee: Xerox CorporationInventor: Roger N. Ciccarelli
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Patent number: 4323566Abstract: The invention relates to compounds of the general formula (I) ##STR1## and physiologically acceptable salts, hydrates and bioprecursors thereof, in whichR.sub.1 and R.sub.2, which may be the same of different, each represent hydrogen, C.sub.1 alkyl, cycloalkyl, alkenyl, alkynyl, aralkyl, trifluoroalkyl, or alkyl substituted by hydroxy, alkoxy, amino alkylamino dialkylamino or cycloalkyl or R.sub.1 and R.sub.2 may together with the nitrogen atom to which they are attached form a 5 to 10 membered ring which may be saturated or may contain at least one double bond, may be unsubstituted or may be substituted by one or more C.sub.1-3 alkyl groups or a hydroxy group and/or may contain another heteroatom which is oxygen or sulphur;Alk represents a straight or branched alkylene chain of 1 to 6 carbon atoms,Q represents a furan or thiophene ring in which incorporation into the rest of the molecule is through bonds at the 2- and 5- positions, the furan ring optionally bearing a further substituent R.sub.Type: GrantFiled: February 29, 1980Date of Patent: April 6, 1982Assignee: Glaxo Group LimitedInventors: John W. Clitherow, Barry J. Price, John Bradshaw, Michael Martin-Smith, John W. M. MacKinnon, Duncan B. Judd, Linda Carey
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Patent number: 4303663Abstract: Butyrophenone compounds having excellent psychotropic activities represented by the formula: ##STR1## wherein R.sup.1 is a halogen atom, R.sup.2 is a lower alkyl group, and Z is a group of either one of the formulae: ##STR2## (wherein the dotted line indicates the optional presence of an additional single bond linkage, R.sup.3 is a hydrogen atom or a hydroxyl group but only when said additional single bond linkage is not present and R.sup.4 is a hydrogen atom or a phenyl or benzyl group optionally substituted with one or two substituents selected from the group consisting of halogen, lower alkyl, lower alkoxy and trifluoromethyl on the benzene ring (except monohalophenyl)), ##STR3## (wherein the dotted line indicates the optional presence of an additional single bond linkage, R.sup.5 is a hydrogen atom or a lower alkyl group and R.sup.6 and R.sup.7 are each a hydrogen atom, a halogen atom or a lower alkyl group), ##STR4## (wherein R.sup.8 is a hydrogen atom or a lower alkyl group and R.sup.Type: GrantFiled: May 9, 1977Date of Patent: December 1, 1981Assignee: Sumitomo Chemical Company, LimitedInventors: Kikuo Sasajima, Keiichi Ono, Masaru Nakao, Hisao Yamamoto
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Patent number: 4294833Abstract: There are prepared 4-hydroxy-isophthalic acid bis (3- or 4-picolyl-amides) of the formula (I) ##STR1## where R' is H or an aliphatic or alicyclic hydrocarbon group with 1 to 16 carbon atoms, R'''' is 3-pyridyl or 4-pyridyl, R''' is H, Cl, NO.sub.2, or --OCH.sub.3, R'' is an aliphatic or alicyclic hydrocarbon group with 1 to 8 carbon atoms with the exception that when R'''' is 3-pyridyl and R' and R''' are both H, then R'' is an aliphatic or alicyclic hydrocarbon radical with 3 to 8 carbon atoms. The compounds are useful in inhibition of blood platelet aggregation.Type: GrantFiled: August 29, 1978Date of Patent: October 13, 1981Assignee: Societa Italo-BritannicaInventors: Franco Innocenti, Giovanni Orzalesi, Ivo Volpato
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Patent number: 4229207Abstract: Esters of 1,2-diphenyl-cyclohex-1-ene-4-carboxylic-acid are effective plant growth regulating agents. They are useful for controlling wild oats in cereal cultures and for growth inhibition in different cultures, e.g. for the inhibition of suckers in tobacco plants.Type: GrantFiled: June 22, 1978Date of Patent: October 21, 1980Assignee: Ciba-Geigy CorporationInventors: Verena Laanio, Werner Fory, Rolf Schurter
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Patent number: 4199590Abstract: Compounds of formula ##STR1## in which hal represents halogen;R represents hydrogen or lower alkyl having 1 to 6 carbon atoms;R.sup.2 represents a subsituted or unsubstituted monocyclic heterocyclic group;and X represents oxygen or sulphur; or a pharmaceutically acceptable acid addition or quaternary ammonium salt thereof, are disclosed which have hypotensive and/or antihypertensive activity.Type: GrantFiled: August 24, 1978Date of Patent: April 22, 1980Assignee: John Wyeth & Brother LimitedInventor: Terence J. Ward
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Patent number: 4189488Abstract: Amidinoformic acids and amidinosulphinic acids which are histamine H.sub.2 -antagonists. Two specific compounds of the present invention are N-[2-(5-methyl-4-imidazolylmethylthio)ethyl]amidinoformic acid and N-methyl-N'-[2-(5-methyl-4-imidazolylmethylthio)ethyl]amidinosulphinic acid.Type: GrantFiled: June 12, 1978Date of Patent: February 19, 1980Assignee: Smith Kline & French Laboratories LimitedInventors: Graham J. Durant, Charon R. Ganellin, Rodney C. Young
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Patent number: 4181807Abstract: The esters are soluble in an aqueous solution of a base before exposure to actinic radiation but, on exposure to actinic radiation, polymerize and become insoluble in such an aqueous solution. Development of photopolymerized images does not therefore require the use of toxic or flammable organic solvents. They contain free carboxyl groups and at least one unit of the formulae I-IV ##STR1## where R.sup.1 is a carbon atom chain containing specified groupings, such as one of formula --CH.dbd.CH--CO--CH.dbd.CH--, --CH.dbd.CHCO--, --COCH.dbd.CHC.sub.6 H.sub.4 CH.dbd.CHCO--, or ##STR2## and Y is oxygen or sulfur. They are obtained by the reaction of an at least dianhydride of a polycarboxylic acid with alcoholic hydroxyl groups of an alcohol containing at least one unit of formula I-IV.Type: GrantFiled: December 27, 1977Date of Patent: January 1, 1980Assignee: Ciba-Geigy CorporationInventor: George E. Green
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Patent number: 4153795Abstract: Complex catalysts for hydroformylation which comprises (A) a cobalt carbo component and (B) at least one component selected from the group consisting of 3-pyridylpropionic acid esters of aliphatic polyhydric alcohols, 3-pyridylpropionic acid esters of aliphatic pyridylalcohols and dipyridyl ethers. The catalysts promote hydroformylation of olefins at low temperature and pressure and are especially easily separated and recovered.Type: GrantFiled: July 22, 1977Date of Patent: May 8, 1979Assignee: Director-General of the Agency of Industrial Science and TechnologyInventor: Akio Matsuda
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Patent number: 4131748Abstract: p-Terphenylene-dicarboxylic acids in which aromatic groups are attached to the middle phenyl group of the terphenylene moiety. The compounds are useful as monomers in the preparation of rod-like, para-ordered aromatic heterocyclic polymers.Type: GrantFiled: June 29, 1977Date of Patent: December 26, 1978Assignee: The United States of America as represented by the Secretary of the Air ForceInventors: Fred E. Arnold, James F. Wolfe