The -c(=x)- Is Part Of A -c(=x)x- Group, Wherein The X's Are The Same Or Diverse Chalcogens Patents (Class 546/263)
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Patent number: 5130303Abstract: Compounds of the formula (I): ##STR1## in which the nitrogen-containing hetero ring portion is a 1,4-dihydropyridine ring or a pyridine ring, R.sup.1 is only present when the nitrogen-containing hetero ring is a 1,4-dihydropyridine ring, and Z is either a CO.sub.2 R.sup.8 group or a group of the formula (II): ##STR2## in which R.sup.4 and R.sup.5 may be the same or different and together may form one divalent group, are effective agents for enhancing the antitumor effect or antitumor drugs.Type: GrantFiled: July 15, 1991Date of Patent: July 14, 1992Assignee: Nissan Chemical Industries Ltd.Inventors: Shin-ichi Akiyama, Ryozo Sakoda, Kiyotomo Seto, Norimasa Shudo
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Patent number: 5126358Abstract: The invention relates to novel isonicotinoylpyridinyl hydrazine derivatives of formula I ##STR1## wherein Hal is halogen,R.sub.1 is hydrogen, methyl or --COR.sub.5,R.sub.2 is hydrogen, C.sub.1 -C.sub.4 alkyl, or a radical selected from --COR.sub.5 and --CO--Z--R.sub.6,R.sub.3 is hydrogen, halogen, trifluoromethyl, trichloromethyl, --COOH, --COOCH.sub.3, --OH or nitro.R.sub.4 is hydrogen, halogen, methoxy or methyl,R.sub.5,R.sub.6, Z are as defined hereinafter.with the exception of 1-(pyridin-2'-yl)-2-(2,6-dichloroisonicotinoyl) hydrazine.The novel compounds have plant-protective properties and are especially suitable for protecting plants from attack by phytopathogenic microorganisms such as fungi, bacteria and viruses.Type: GrantFiled: December 21, 1990Date of Patent: June 30, 1992Assignee: Ciba-Geigy CorporationInventor: Walter Kunz
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Patent number: 5118683Abstract: Compounds of the formula I ##STR1## wherein R.sup.5 represents C.sub.1 to C.sub.6 -alkyl or the group --(CH.sub.2).sub.n --Z--(CH.sub.2).sub.m --Ar;Z represents O, S or --CH.sub.2 --;n represents an integer of 1 to 8;m represents zero or an integer of 1 to 8;one of R.sup.1 and R.sup.2 represents the group ##STR2## and the other represents hydrogen or R.sup.7 CO--; R.sup.7 is C.sub.1 to C.sub.10 alkyl, C.sub.3 to C.sub.8 cycloalkyl, aryl, heteroaryl, --N(R.sup.9 R.sup.10), or R.sup.11 O--; R.sup.3, R.sup.4, R.sup.9, and R.sup.10 are each independently selected from hydrogen, C.sub.1 to C.sub.6 alkyl and Ar.sup.1 ; R.sup.6 and R.sup.11 are each independently C.sub.1 -C.sub.8 alkyl; Ar and Ar.sup.1 are each independently selected from the group consisting of phenyl or phenyl substituted by one or two substituents selected from the group consisting of R.sup.12, R.sup.13 O--; R.sup.14 S(O).sub.x --, R.sup.15 CO--, (R.sup.16 R.sup.17)NCO--, F, Cl, Br, I, NO.sub.2, CF.sub.3, CN, or phenyl; R.sup.12, R.sup.13, R.sup.Type: GrantFiled: June 13, 1990Date of Patent: June 2, 1992Assignee: Schering CorporationInventors: David J. Blythin, Ho-Jane Shue
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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: 5106957Abstract: A class of fluorescent rare earth chelates and the ligands upon which they are based whose molecular structure incorporates a plurality of substituted arylpyridine diacid units attached to a central template structure is disclosed. These ligands function as efficient energy transfer groups in fluorescent tagging reagents and tracers.Type: GrantFiled: March 27, 1991Date of Patent: April 21, 1992Assignee: Baxter Diagnostics Inc.Inventors: Ron L. Hale, Dennis W. Solas
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Patent number: 5098466Abstract: Substituted semicarbazones, thiosemicarbazones and isothiosemicarbazones and salts thereof, intermediates therefor, synthesis thereof, and the use of said compounds for the control of weeds.Type: GrantFiled: August 21, 1990Date of Patent: March 24, 1992Assignee: Sandoz Ltd.Inventors: Richard J. Anderson, Michael M. Leippe, Joe T. Bamberg
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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: 5075324Abstract: 1,4-dihydropyridines of formula I ##STR1## wherein X is --CO.sub.2 R.sub.1, cyano, nitro, --COCH.sub.3 ; each of R and R.sub.1, which are the same or different, is a primary, secondary or tertiary, saturated or unsaturated, linear or branched C.sub.1 -C.sub.6 alkyl group optionally substituted by one or more hydroxy, C.sub.1 -C.sub.7 -monoalkylamino, di-C.sub.1 -C.sub.7 -alkylamino, benzylamino, C.sub.1 -C.sub.6 -alkoxy, phenoxy groups which are optionally substituted; R.sub.2 is hydrogen; R.sub.3 is hydrogen or hydroxy, --OCOR.sub.5, OSO.sub.2 R.sub.6, azide, amino, --NHPO(OR.sub.7).sub.2, --NHCOR.sub.5, C.sub.1 -C.sub.4 -alkoxy or fluorine, chlorine, bromine or iodine, SH, SCOR.sub.6 or C.sub.1 -C.sub.6 -alkylthio, phenylthio or benzylthio; R.sub.4 is an optionally substituted aromatic or an optionally substituted 5- or 6-membered heteroaromatic group; Y is one or more substituents, which may be the same or different, selected from C.sub.1 -C.sub.4 -alkoxy, halogen, nitro, cyano, C.sub.1 -C.sub.Type: GrantFiled: June 22, 1989Date of Patent: December 24, 1991Assignee: Boehringer Biochemia Robin S.p.A.Inventors: Marco Frigerio, Andrea Zaliani, Carmelo A. Gandolfi, Mauro Germini, Odoardo Tofanetti, Sergio Tognella
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Patent number: 5068337Abstract: The invention concerns compounds of formula ##STR1## or salts thereof; wherein Ar is an optionally substituted aryl radical;R represents hydrogen or an optionally substituted alkyl or aralkyl group;R.sup.1 and R.sup.2 are the same or different and are selected from hydrogen and saturated or unsaturated, cyclic or acyclic aliphatic hydrocarbon residues optionally substituted by one or more groups selected from halogen, OH, carboxy, CN, alkoxy, alkylthio, aryloxy, alkoxycarbonyl, amino, substituted amino, and optionally substituted aryl;A represents a group of formula --XR.sup.3 whereinX is (i) a group of formula --(CHR.sup.6).sub.p --Y--(CHR.sup.7).sub.q --or (ii) a group of formula --(CHR.sup.6).sub.r --O--(CHR.sup.7).sub.qin which formulae: Y represents --S--, NR.sup.8 or a direct bond, p and q each represent 0, 1 or 2 providing that p and q do not both represent 0, 1 or 2 and the other is zero; R.sup.6, R.sup.7 and R.sup.8 independently represent hydrogen or lower alkyl, and R.sup.Type: GrantFiled: November 13, 1986Date of Patent: November 26, 1991Assignee: John Wyeth & Brother LimitedInventors: John L. Archibald, Terence J. Ward, Albert Opalko
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Patent number: 5043443Abstract: Novel aminomethyloxooxazolidinyl arylbenzene derivatives, wherein the aryl includes the phenyl, substituted phenyl, pyridyl, and substituted pyridyl groups, such as (l)-N-{3-[4- (4'-pyridyl)phenyl]-2-oxooxazolidin-5-ylmethyl}acetamide, possess useful antibacterial activity.Type: GrantFiled: July 24, 1990Date of Patent: August 27, 1991Assignee: Du Pont Merck Pharmaceutical CompanyInventors: Randall K. Carlson, Chung-Ho Park, Walter A. Gregory
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Patent number: 5034395Abstract: Dihydropyridine derivatives and salts thereof represented by the general formula, ##STR1## which possess excellent calcium antagonist effect, hypotensive effect, platelets aggregation inhibitory effect, phosphodiesterase inhibitory effect, calmodulin inhibitory effect and peroxidized lipid lowering effect, and thus dihydropyridine derivatives and salts thereof are useful as a coronary blood flow improving agent such as coronary vasodilator, hypotensive agent, prophylaxis and treating agents for thrombosis, phophodiesterase inhibitory agent, peroxidized lipid metabolism lowering agent, anti-inflammatory agent and others.Type: GrantFiled: February 24, 1987Date of Patent: July 23, 1991Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Shigeharu Tamada, Kazuyoshi Nagami, Shuji Teramoto, Tatsuyoshi Tanaka, Kazuyuki Nakagawa
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Patent number: 5032677Abstract: A class of fluorescent rare earth chelates and the ligands upon which they are based whose molecular structure incorporates a plurality of substituted arylpyridine diacid units attached to a central template structure is disclosed. These ligands function as efficient energy transfer groups in fluorescent tagging reagents and tracers.Type: GrantFiled: November 6, 1987Date of Patent: July 16, 1991Assignee: Baxter International Inc.Inventors: Ron L. Hale, Dennis W. Solas
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Patent number: 5021436Abstract: Compounds of formula I ##STR1## wherein R.sub.1 is an alkoxycarbonyl group, acetyl, benzoyl, cyano, nitro or aminocarbonyl;R.sub.2 is an optionally substituted aryl or hetaryl group;R.sub.3 is an alkoxycarbonyl group;.phi. is a thio residue such as alkylthio, cycloalkylthio, arylthio, heteroarylthio, aminoalkylthio,are described.Compounds I are useful in human therapy as antihypertensive, antiulcer, antithrombotic, antiischaemic agents.Type: GrantFiled: September 28, 1989Date of Patent: June 4, 1991Assignee: Boehringer Mannheim Italia, S.p.A.Inventors: Carmelo A. Gandolfi, Marco Frigerio, Silvano Spinelli, Odoardo Tofanetti, Sengio Tognella
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Patent number: 5004743Abstract: Compounds having the formula: ##STR1## are leukotriene antagonists and inhibitors of leukotriene biosynthesis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents.Type: GrantFiled: November 25, 1987Date of Patent: April 2, 1991Assignee: Merck Frosst Canada, Inc.Inventors: Robert N. Young, Robert Zamboni, Jacques Y. Gauthier
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Patent number: 5001148Abstract: Antihypercholesterolemic activity, due to competitive inhibition of HMG CoA reductase, has been found in compounds of the formula ##STR1## wherein: R.sup.1, R.sup.2 and R.sup.3 are independently selected from:(1) alkyl,(2) substituted alkyl in which one or more substituents are selected from(a) halogen,(b) hydroxyl,(c) alkoxy,(d) alkoxycarbonyl,(e) acyloxy,(f) cycloalkyl,(g) phenyl,(h) substituted phenyl in which one or more substituents are X or Y,(i) alkyl-S(O).sub.n,(j) cycloalkyl-S(O).sub.n,(k) phenyl-S(O).sub.n,(l) substituted phenyl-S(O).sub.n in which one or more substituents are X or Y, and(m) oxo,(3) alkoxy,(4) alkenyl,(5) cycloalkyl,(6) substituted cycloalkyl in which one or more substituents are selected from(a) alkyl,(b) substituted alkyl in which one or more substituents are selected from(i) halogen,(ii) hydroxy,(iii) alkoxy,(iv) alkoxycarbonyl(v) acyloxy(vi) phenyl(vii) substituted phenyl in which one or more substituents are X and Y,(viii) alkyl-S(O).sub.n,(ix) cycloalkyl-S(O).sub.Type: GrantFiled: June 7, 1989Date of Patent: March 19, 1991Assignee: E. R. Squibb & Sons, Inc.Inventors: Jeffrey O. Saunders, Eric M. Gordon
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Patent number: 4994465Abstract: Certain trisubstituted urea compounds as potent inhibitors of the enzyme acyl-CoA:cholesterol acyltransferase, their method of manufacture, pharmaceutical compositions containing such compounds as well as methods of inhibiting the interstitial absorption of cholesterol and lowering blood plasma cholesterol with such compounds as described.Type: GrantFiled: February 5, 1990Date of Patent: February 19, 1991Assignee: Warner-Lambert CompanyInventor: Bharat K. Trivedi
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Patent number: 4971984Abstract: Compounds of formula I ##STR1## wherein R.sub.1 is a cyano, nitro, benzoyl, acetyl, amido or alkoxycarbonyl group;R.sub.2 is substituted aryl- or heterocyclic residue;R.sub.3 is alkoxycarbonyl group;R.sub.4 and R.sub.5, being the same or different, are hydrogen, alkyl, aryl or heterocyclic groups;Y is oxygen, sulphur or substituted or unsubstituted nitrogen atom, that can be a part of a heterocyclic ring;n is 0, 1 or 2R6 and R.sub.10, that can be the same or different, are: hydrogen; C.sub.1 -C.sub.6 -alkyl optionally substituted by hydroxy, amino, monoalkyl and dialkylamino, C.sub.1 -C.sub.6 -alkoxy, C.sub.1 -C.sub.6 -alkoxycarbonyl, C.sub.1 -C.sub.3 -carbonyloxy, aryl, heteroaryl and cycloalkyl; a C.sub.1 -C.sub.12 -alkanoyl, aroyl or heteroaryl group optionally substituted by halogen, nitro, amino monoalkylamino, dialkylamino, hydroxy, C.sub.1 -C.sub.6 -alkoxy, C.sub.1 -C.sub.6 -alkoxycarbonyl, C.sub.1 -C.sub.6 -alkylthio, C.sub.1 -C.sub.3 -carbonyloxy, aryl, heteroaryl, cycloalkyl groups.Type: GrantFiled: December 10, 1987Date of Patent: November 20, 1990Assignee: Beehringer Biochemia Robin S.p.A.Inventors: Marco Frigerio, Andrea Zaliani, Carlo Riva, Carmelo Gandolfi, Odoardo Tofanetti, Sergio Tognella
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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: 4968796Abstract: Disclosed is a process for the preparation of a sulphonylisothiourea of the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, X, Y, and Z are as defined herein, which comprises reacting a sulphonic acid amide of the formulaR.sup.1 --SO.sub.2 --NH.sub.2, (II)or a metal salt thereof, with an N-heteroaryl-iminodithiocarbonic acid S,S-diester of the formula ##STR2## at a temperature between about 20.degree. C. and 200.degree. C. Intermediates and a process for their preparation are also disclosed.Type: GrantFiled: August 17, 1989Date of Patent: November 6, 1990Assignee: Bayer AktiengesellschaftInventor: Hans-Jochem Riebel
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Patent number: 4959096Abstract: Novel substituted isonicotinic acid esters of the general formula ##STR1## in which Y is halogen;X is oxygen or sulfur;Q is C.sub.1 -C.sub.3 alkylene, propenylene, C.sub.1 -C.sub.3 alkylene mono- or di-substituted by R, or propenylene mono- or di-substituted by R;R is C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 haloalkyl having from 1 to 3 halogen atoms, cyano, C.sub.2 -C.sub.5 alkoxycarbonyl, C.sub.3 -C.sub.6 cycloalkyl, phenyl, or phenyl substituted by C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, halogen, trifluoromethyl, tricholoromethyl, nitro or by cyano, or benzoyl or benzoyl substituted by C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, trifluoromethyl, trichloromethyl, nitro or by cyano;A is phenyl, biphenyl, phenoxyphenyl, naphthyl, pyridyl, furyl, thienyl, imidazolyl or triazolyl, it being possible for each of these radicals to be unsubstituted or substituted by halogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.3 alkoxy, C.sub.1 -C.sub.Type: GrantFiled: March 17, 1989Date of Patent: September 25, 1990Assignee: Ciba-Geigy CorporationInventors: Helmut Zondler, Walter Kunz
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Patent number: 4946851Abstract: Compounds are described of the formula ##STR1## wherein R.sub.1 and R.sub.4 independently represent a C.sub.1-4 alkylgroup;R.sub.2 and R.sub.3 independently represent a C.sub.1-6 straight orbranched alkyl chain or alkoxy group;R.sub.4 represents a C.sub.1-4 alkyl group;R.sub.5 represents a group CH.dbd.CR.sub.6 R.sub.7 where R.sub.6 is a hydrogen atom or C.sub.1-3 alkyl group and R.sub.7 represents an aryl, pyridyl or cyano group; or R.sub.5 represents the group C.tbd.CR.sub.8 where R.sub.8 is an aryl group.The compounds represented by formula (I) reduce intracellular calcium ion concentration by limiting transmembranal calcium ion influx and thus may be useful for the treatment of cardiovascular disorders such as hypertension.Type: GrantFiled: October 28, 1988Date of Patent: August 7, 1990Assignee: Glaxo, S.p.A.Inventors: Claudio Semeraro, Dino Micheli, Daniele Pieraccioli, Giovanni Gaviraghi, Alan D. Borthwick
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Patent number: 4939160Abstract: Hydropyridine derivatives of the formula ##STR1## in which R.sub.1 represents carboxy, lower alkoxycarbonyl, carbamoyl, N-lower alkylcarbamoyl or N,N-di-lower alkylcarbamoyl, R.sub.2 represents hydrogen, an optionally etherified or acylated hydroxy group or an optionally acylated amino group, and R.sub.3 represents a radical of the formula R- (Ia), R-alk.sub.1 - (Ib) or R'=alk.sub.2 - (Ic) in which R represents a benzocycloalkenyl radical having a total of from 8 to 12 ring carbon atoms which is bonded via a saturated carbon atom and which is unsubstituted or is mono- or poly-substituted in the benzo moiety by hydroxy, lower alkoxy, lower alkanoyloxy, halogen, lower alkyl and/or by trifluoromethyl, and/or substituted in the .alpha.Type: GrantFiled: December 9, 1988Date of Patent: July 3, 1990Assignee: Ciba-Geigy CorporationInventors: Georg von Sprecher, Wolfgang Frostl, Armin Zust
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Patent number: 4931450Abstract: Compounds of the Formula I ##STR1## wherein R.sup.1 represents phenyl, or phenyl substituted by one, or more substituents selected from the group consisting of halogen, C.sub.1-7 -alkyl, and C.sub.1-7 -alkoxy, R.sup.2 represents furanyl, thienyl, pyridyl or pyrrolyl ortho substituted with C.sub.1-7 -alkyl or halogen and wherein R.sup.3 represents 3-carboxypiperidin-1-yl, 3-carboxy-1,2,5,6-tetrahydropyridin-1-yl or 3-carboxymethyl-pyrrolidin-1-yl, pharmaceutical compositions containing effective amounts of a compound of formula I and treatment of central nervous system ailments by administering a compound of formula I.Type: GrantFiled: October 17, 1988Date of Patent: June 5, 1990Assignee: Novo Industri A/SInventor: Ursula Sonnewald
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Patent number: 4931456Abstract: Nicotinic derivatives. They have the formula: ##STR1## with R.sup.1, R.sup.2, which are identical or different,=H, alkyl (C.sub.1 -C.sub.18) optionally substituted phenyl, pyridyl;Y=H, hal, alkyl or alkoxy or C.sub.1 -C.sub.4 ; n=integer from 1 to 3.Agricultural fungal compounds.Type: GrantFiled: November 14, 1988Date of Patent: June 5, 1990Assignee: Rhone-Poulenc AgrochimieInventors: Claude Lambert, Regis Pepin, Marie-Pascale Latorse
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Patent number: 4925590Abstract: Derivatives of 4-cyano-2,3-difluorophenol of the formula I ##STR1## wherein R.sup.1 is an alkyl group which has 1-12 C atoms and in which one or two CH.sub.2 groups can also be replaced by --O--, --CO--, --CO--O-- and/or --CH.dbd.CH--, no two 0 atoms being directly attached to one another,A.sup.1 and A.sup.2 independently of one another are each 1,4-phenylene which is unsubstituted or substituted by one or two F atoms, and in which one or two CH groups can also be replaced by N, or trans-1,4-cyclohexylene in which one or two non-adjacent CH.sub.2 groups can also be replaced by 0 atoms and/or S atoms,Z is --CO--O--, --O--CO--, --CH.sub.2 CH.sub.2 --, OCH.sub.2 --, --CH.sub.2 O, --C.tbd.C-- or a single bond,m is 0, 1 or 2 andQ is --CO-- or --CH.sub.2 --.Type: GrantFiled: March 9, 1989Date of Patent: May 15, 1990Assignee: Merck Patent Gesellschaft Mit Beschrankter HaftungInventors: Volker Reiffenrath, Joachim Krause, Andreas Wachtler, Georg Weber, Ulrich Finkenzeller
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Patent number: 4908398Abstract: Poly-dihydro-2,6-dimethylpyridine-3,5-dicarboxylesters of general formula (I) ##STR1## in which A, B, m, n, k, j, R, R.sup.1 and R.sup.2 have the meanings defined in the text, useful as thermal stabilizers for synthetic polymers, in particular for polyvinylchloride-based masses.The compounds of formula (I) are preferably used in combination with the usual stabilizers based on organic metal derivatives. They can also be used combined with agents which exert a synergic action in maintaining a low color of manufactured articles subjected to heating, and in particular with betadicarbonyl compounds of formula (II):R.sup.3 --CO--CH.sub.2 --CO--R.sup.4 (II)in which R.sup.3 and R.sup.4 have the meanings defined in the text, in masses containing organic calcium and zinc salts as basic stabilizers.Type: GrantFiled: March 29, 1988Date of Patent: March 13, 1990Assignee: Lagor S.p.A.Inventors: Giuseppe Li Bassi, Roberto Ortica
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Patent number: 4892881Abstract: 1,4-Dihydropyridine anti-ischaemic and antihypertensive agent of the formula: ##STR1## or a pharmaceutically acceptable salt thereof, wherein R is 2-chlorophenyl, 2,3-dichlorophenyl or 2-chloro-3-trifluoromethylphenyl;R.sup.1 and R.sup.2 are each independently C.sub.1 -C.sub.4 alkyl;X is O or S;R.sup.3 is H or C.sub.1 -C.sub.4 alkyl; andR.sup.4 is 1,2,4-triazol-1-ylmethyl, imidazol-1-ylmethyl, azidomethyl, 2,4,5-trimethylimidazol-1-ylmethyl, 3,4-dihydro-4-oxopyrimidin-2-ylthiomethyl, pyrimidin-2-ylthiomethyl; pyrimidin-2-ylaminomethyl, 3,4-dihydro-4-oxopyrimidin-2-ylaminomethyl, 2-aminopyrimidin-4-yloxymethyl, methoxymethyl, 2-furyl, 2-pyridylmethyl, imidazol-2-yl, hydroxymethyl, aminomethyl, 1,2,4-triazol-4-ylmethyl or 2-hydroxyethyl, and intermediates leading thereto.Type: GrantFiled: November 2, 1987Date of Patent: January 9, 1990Assignee: Pfizer Inc.Inventors: David Alker, Simon F. Campbell, Peter E. Cross
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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: 4885303Abstract: Circulation active tetrahydropyridines of the formula ##STR1## in which R.sup.1 represents a straight-chain, branched or cyclic, saturated or unsaturated hydrocarbon radical which has up to 20 carbon atoms and can be interrupted in the chain by an oxygen atom or a sulphur atom and/or can be substituted by halogen, cyano, hydroxyl, acyloxy, nitro or nitrooxy, or by a phenyl, phenoxy, phenylthio or phenylsulphonyl group which is optionally substituted by halogen, cyano, dialkylamino with in each case 1 or 2 carbon atoms per alkyl group, alkoxy with 1 to 4 carbon atoms, alkyl with 1 to 4 carbon atoms, trifluoromethyl or nitro, or by an .alpha.-, .beta.- or .gamma.Type: GrantFiled: January 4, 1988Date of Patent: December 5, 1989Assignee: Bayer AktiengesellschaftInventors: Horst Meyer, Eckhard Schwenner, Andreas Knorr
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Patent number: 4882341Abstract: The invention relates to amino substituted propenoates and their use against fungi.Type: GrantFiled: September 9, 1988Date of Patent: November 21, 1989Assignee: Imperial Chemical Industries PLCInventors: John M. Clough, Ian T. Kay
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Patent number: 4877797Abstract: Compounds are described of the formula ##STR1## wherein R.sub.1 is a nitro or trifluoromethyl group; R.sub.2 is a C.sub.1 -C.sub.6 alkyl group; R.sub.3 is a pyridyl or pyridyl N-oxide group which may be substituted with halogen, hydroxyl, haloalkyl, C.sub.1 -C.sub.6 alkoxy or C.sub.1 -C.sub.6 alkyl and further may be fused with a benzene or naphthalene ring, said ring being optionally substituted with C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, halogen or haloalkyl, and a pharmaceutically acceptable acid addition salt thereof. The compounds of the formula (I) are of vasodilating and blood pressure lowering activities and thus may be useful for the treatment of cardiac diseases, cerebrovascular diseases and hypertension.Type: GrantFiled: June 15, 1987Date of Patent: October 31, 1989Assignee: Nisshin Flour Milling Co., Ltd.Inventors: Hiroaki Satoh, Hiroyasu Koyama, Yoshikuni Suzuki, Toshiji Sugai, Koichi Watanabe
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Patent number: 4873254Abstract: A dihydropyridine of the formula: ##STR1## wherein R.sup.1 and R.sup.2 each is alkyl, alkenyl or alkoxyalkyl, wherein R.sup.3 and R.sup.4 each is alkyl, wherein benzene ring A is unsubstituted or bears one or more additional substituents selected from halogeno, cyano, nitro, trifluoromethyl and alkyl, or bears the substituent .dbd.N--O--N.dbd. attached to the 5- and 6-positions, wherein Ar is as defined in the specification, wherein p is 0 or 1, wherein X is --O-- or --S--, and wherein Y is straight-or branched-chain alkylene or alkenylene each of 2 to 12 carbon atoms which may optionally be interrupted by one or two groups selected from oxygen, sulphur, imino, substituted imino, phenylene, substituted phenylene, pyridylene, cycloalkylene, 1,4-piperazinediyl, 1,4-piperidinediyl and amido groups; or an acid-addition salt thereof, processes for their manufacture and pharmaceutical compositions containing them.Type: GrantFiled: February 11, 1986Date of Patent: October 10, 1989Assignee: Imperial Chemical Industries plcInventors: Rodney B. Hargreaves, Bernard J. McLoughlin, Stuart D. Mills
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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: 4853395Abstract: Novel 5-acyl-2-(1H)pyridinones and their use as cardiotonic agents. Typical of the compounds is 5-acetyl-1,2-dihydro-6-methyl-2-oxo-3-pyridinecarbonitrile which is prepared by condensing anionic cyano acetamide with 3-[(dimethylamino)methylenyl]-2,4-pentanedione in an inert organic solvent.Type: GrantFiled: November 17, 1987Date of Patent: August 1, 1989Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Winton D. Jones, Richard A. Schnettler, Richard C. Dage
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Patent number: 4851396Abstract: Nicotinic acid derivatives They are of formula: ##STR1## with: Z=OR, with R=optionally substituted C.sub.1 -C.sub.18 -alkyl, C.sub.2 -C.sub.18 -alkenyl, C.sub.2 -C.sub.5 -alkynyl, phenyl or phenoxy;Y=H, hal, C.sub.1 -C.sub.4 -alkyl or C.sub.1 -C.sub.4 -alkoxy andn=1 to 3.Fungicidal products for agricultural use.Type: GrantFiled: May 18, 1987Date of Patent: July 25, 1989Assignee: Rhone-Poulenc AgrochimieInventors: Claude Lambert, Regis Pepin
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Patent number: 4845113Abstract: Compounds of formula I ##STR1## wherein R is hydrogen or lower alkyl; R.sub.1 is acetyl, benzoyl, cyano, nitro, carboxy, alkoxycarbonyl or aminocarbonyl groups; R.sub.2 is an optionally substituted aryl or hetaryl residue; R.sub.3 is a carboxy or alkoxycarbonyl group; A is a cyclopropyl group or a group of formula --CH.dbd.CH-- and R.sub.4 is a phenyl or heteroaryl group, optionally mono, di or tri-substituted, are useful in radical scavenging therapy.Type: GrantFiled: July 25, 1986Date of Patent: July 4, 1989Assignee: Boehringer Biochemia Robin S.p.A.Inventors: Carmelo A. Gandolfi, Marco Frigerio, Silvano Spinelli, Odoardo Tofanetti, Ernesto Menta, Sergio Tognella
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Patent number: 4839348Abstract: Dihydropyridines of formula I ##STR1## wherein R is hydrogen or lower alkyl; R.sub.1 is a CN, NO.sub.2, COCH.sub.3, COPh group, a carboalkoxy or carboamide group; R.sub.2 is an aromatic or heteroaromatic, mono- or bicyclic eventually substituted phenyl group; R.sub.3 is a carboalkoxy group; while A is a halogen atom or an ammonium or phosphonium residue. The compounds I are useful as antihypertensive, antitumoral, antimetastatic, antithrombotic, and/or antiischemic agent.Type: GrantFiled: July 25, 1986Date of Patent: June 13, 1989Assignee: Boehringer Biochemia Robin S.p.A.Inventors: Carmelo A. Gandolfi, Marco Frigerio, Silvano Spinelli, Odoardo Tofanetti, Sergio Tognella
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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: 4829076Abstract: The invention relates to new substituted dihydropyridine derivatives of the general formula (I), ##STR1## wherein R.sup.1 and R.sup.6 are as defined herein after, the racemic and optically active variants as well as mixtures thereof, furthermore the acid addition salts of these compounds, pharmaceutical compositions containing the same and a process for the preparation thereof.The compounds of the general formula (I) can be advantageously applied for the treatment of pathologically severe hypertensions, their toxicity is low and they possess an advantageous therapeutic index.Type: GrantFiled: September 16, 1987Date of Patent: May 9, 1989Assignee: Alkaloida Vegyeszeti GyarInventors: Geza Szilagyi, Eva Bozo, Laszlo Czollner, Laszlo Jaszlits, Gyorgy Rabloczky, Jozsef Borsi, Istvan Elekes, Gyongyi Nagy nee Csokas, Andras Varro, ZSuzanne Lang nee Rihmer, Gyorgy Cseh, Gyula Horvath, Ilona Bodi
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Patent number: 4824837Abstract: 1,4-Dihydropyridine derivatives of the formula (1): ##STR1## wherein X is a halogen; R.sup.1 is a straight, branched or cyclic alkyl group having 1 to 10 carbon atoms, the group --(CH.sub.2).sub.n -Y [where n is an integer of 0 to 8, provided that n is an integer of 2 to 8 when Y is not bonded to COO-- through carbon; Y is a cyclic alkyl group having 3-6 carbon atoms, an aryl group having 6-10 carbon atoms, a pyrrolidinyl group, an imidazolidinyl group, a thienyl group, a furyl group, an imidazolyl group, a pyridyl group, a pyrimidinyl group, a morpholinyl group, a thiomorpholinyl group or a pyrrolizidinyl group, the group ##STR2## (where D is an aryl or aralkyl group having 6-15 carbon atoms which may be substituted by a halogenated alkyl group), or a 3-piperidinyl group substituted by a phenylalkyl group of 7-10 carbon atoms which may be substituted by one or two halogens], the group --(CH.sub.2).sub.Type: GrantFiled: July 3, 1986Date of Patent: April 25, 1989Assignee: Suntory LimitedInventors: Hidetsura Cho, Masaru Ueda
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Patent number: 4801597Abstract: The present invention relates to pharmaceutical compositions and methods for the treatment of metabolic disorders and to certain inositol-nicotinate dichloroacetate derivatives as the active ingredients therein.Type: GrantFiled: June 11, 1985Date of Patent: January 31, 1989Assignee: University of FloridaInventors: Peter W. Stacpoole, Nicholas S. Bodor
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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: 4772615Abstract: Analogs of nipecotic acid are the novel compounds of the present invention. The analogs are GABA uptake inhibitors for use to treat epilepsy and, thus, the invention is also pharmaceutical compositions and methods of use therefor.Type: GrantFiled: October 14, 1987Date of Patent: September 20, 1988Assignee: Warner-Lambert CompanyInventor: Michael R. Pavia
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Patent number: 4772612Abstract: Novel circulation active dihydropyridines of the formula ##STR1## in which X is CO, SO.sub.2 or CONH,R.sup.4 is H, OH, alkyl, halogen, acyloxy, alkoxyalkoxy, aralkyloxy, or together with R.sup.5 forms a heterocyclic ring, andthe other radicals are conventional in the dihydropyridine art,and pharmaceutically acceptable salts thereof.Type: GrantFiled: June 3, 1986Date of Patent: September 20, 1988Assignee: Bayer AktiengesellschaftInventors: Siegfried Goldmann, Jurgen Stoltefuss, Gerhard Franckowiak, Rainer Gross, Matthias Schramm, Gunter Thomas
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Patent number: 4764516Abstract: Pure enantiomers of 5-nitrodihydropyridine of the formula ##STR1## are mixed, wherein one of the enantiomers has a high vasodilative action and a low negative inotropic activity on heart muscle, the other enantiomer has a low vasoconstrictive action and a high positive inotropic activity on heart muscle, the mixture being high in vasodilative activity and in positive inotropic activity on heart muscle.Type: GrantFiled: December 6, 1985Date of Patent: August 16, 1988Assignee: Bayer AktiengesellschaftInventors: Gerhard Franckowiak, Rolf Grosser, Gunter Thomas, Matthias Schramm, Rainer Gross
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Patent number: 4758669Abstract: Novel nitrone substituted 4-aryl dihydropyridines of the formula: ##STR1## are described along with a process for their preparation. The compounds exhibit calcium channel blocker and antimetastatic acitivity.Type: GrantFiled: May 5, 1986Date of Patent: July 19, 1988Assignee: Radiation Oncology Center Research and Development CorporationInventors: Carl R. Johnson, John D. Taylor, Kenneth V. Honn, Soan Cheng
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Patent number: 4757071Abstract: 2,6-Dimethyl-4-(2- or 3-substituted phenyl)-1,4-dihydropyridine-3,5-dicarboxylic acid diesters, having vasodilating and blood pressure lowering effects, in the ester moiety at the 3-position of which a heterocyclic group is linked to an alkylene group through an ester bond (carbonyloxy group). The diesters are used for treatment of cardiac diseases, cerebrovascular diseases and hypertension.Type: GrantFiled: December 9, 1985Date of Patent: July 12, 1988Assignee: Nisshin Flour Milling Co., Ltd.Inventors: Hiroyasu Koyama, Yoshikuni Suzuki, Koichiro Hagihara
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Patent number: 4745120Abstract: The present invention relates to new pyridines substituted in the 3-position, of the formula ##STR1## and to a process for their preparation. The compounds bring about specific inhibition of thromboxane synthetase and can thus be used as medicaments.Type: GrantFiled: August 21, 1985Date of Patent: May 17, 1988Assignee: Hoechst AktiengesellschaftInventors: Gunther Wess, Wilhelm Bartmann, Gerhard Beck, Hans-Hermann Lau