Chalcogen Bonded Directly To Ring Carbon Of The Hetero Ring Patents (Class 514/445)
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Patent number: 5158971Abstract: A pharmaceutical compound of the formula ##STR1## in which R.sup.1 is halo-C.sub.1-10 alkyl, C.sub.1-10 alkylthio, halo-C.sub.1-10 alkylthio or optionally substituted phenylthio, R.sup.2 is hydrogen or C.sub.1-4 alkyl, R.sup.3 and R.sup.4 are each hydrogen or C.sub.1-4 alkyl, and X is oxygen or sulphur; and salts thereof.Type: GrantFiled: May 24, 1991Date of Patent: October 27, 1992Assignee: Lilly Industries limitedInventors: Trafford Clarke, David J. Steggles
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Patent number: 5158966Abstract: Provided is a method for treating Type I diabetes in mammals utilizing certain aryl-substituted rhodanine derivatives.Type: GrantFiled: February 22, 1991Date of Patent: October 27, 1992Assignee: The University of Colorado Foundation, Inc.Inventors: Kevin Lafferty, Jill A. Panetta
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Patent number: 5145703Abstract: The invention relates to new thio-alkanones of the formula ##STR1## in which X represents an oxygen or sulphur atom,R.sub.1 represents hydrogen or a C.sub.1 -C.sub.2 -alkyl group and the broken lines represent a single bond or no bond,to a process for their preparation and their use as flavorings.Type: GrantFiled: May 16, 1991Date of Patent: September 8, 1992Assignee: Haarmann & ReimerInventors: Roland Emberger, Matthias Gunter, Rudolf Hopp, Manfred Kopsel, Walter Kuhn, Peter Werkhoff
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Patent number: 5145867Abstract: Naphthylalkylamino-substituted sulfamoylbenzoic acid derivatives, processes for the preparation thereof and the use thereof as medicines.Compounds I ##STR1## R(1) hydrogen, (C.sub.1 -C.sub.4)-alkyl and Na, K, NH.sub.4, Ca, Mg, R(2) and R(3) hydrogen, alkyl groups which can also be linked together in a ring,X oxygen, sulfur, SO, SO.sub.2, NR(6) [with R(6)=hydrogen-alkyl], CH.sub.2, CO, or a bond,R(4) phenyl, thienyl, which are unsubstituted or substitutedR(5) hydrogen, (C.sub.1 -C.sub.4)-alkyl,n 1, 2, 3 or 4,where the naphthyl system is unsubstituted or substituted like the phenyl radical of R(4),and where X and R(4) together can also be Cl are medicaments for treating sickle-cell anemia.Type: GrantFiled: April 6, 1990Date of Patent: September 8, 1992Assignee: Hoechst AktiengesellschaftInventors: John C. Ellory, Heinrich C. Englert, Hans-Jochen Lang, Dieter Mania, Wulf Merkel
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Patent number: 5133969Abstract: An antimicrobial composition comprises a clathrate compound containing a water-soluble microbicide, and a dispersion medium.For example, the composition may comprise of a clathrate compound containing a water-soluble microbicide and having a particle size of 200 mesh at maximum, said clathrate compound being formed of 5-chloro-2-methyl-4-isothiazoline-3-one and at least one polymolecular host compound selected from the group consisting of 1, 1-di (2,4-dimethylphenyl)-2-propyne-1-ol; 1,1,6,6-tetra(2,4-dimethylphenyl)-2,4-hexadiyne-1,6-diol; 1,1-bis(4-hydroxyphenyl)cyclohexane; N,N,N',N'-tetra(cyclohexyl)-[1,1'biphenyl]-2,2'-dicarboxyamide; 2,2'-methylenebis(4-chlorophenol), deoxycholic acid; and 2,5-di-tert-butylhydroquinone and a dispersion medium.Type: GrantFiled: November 28, 1990Date of Patent: July 28, 1992Assignee: Kurita Water Industries Ltd.Inventors: Ayako Sekikawa, Hideo Sugi, Ryoichi Takahashi, Kenji Tahara
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Patent number: 5125967Abstract: A composition comprises an isothiazolinone or an isothiazolothione and a substituted urea or a halogen-containing aromatic alkyl sulphoxide or sulphone. The isothiazolinone derivative can be 1,2-benzisothiazolin-3-one. The substituted urea may be 3-(3,4-dichlorophenyl)-1-1-dimethylurea. The sulphoxide or sulphone may be a sulphone derivative such as di-iodomethyl-4-methylphenyl sulphone. A useful composition comprises 1,2-benzisothiazolin-3-one and the specified urea or sulphone derivative. The composition may include other materials including other compounds having anti-microbial properties.Type: GrantFiled: March 29, 1990Date of Patent: June 30, 1992Assignee: Imperial Chemical Industries PLCInventors: Fraser F. Morpeth, Malcolm Greenhalgh
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Patent number: 5118672Abstract: This invention provides compounds and pharmaceutical compositions that include compounds of the formula: ##STR1## in which A, B, and C are hydrogen, halogen, or azido; D is hydrogen, halogen, azido, or OH; A and B or C and D can be replaced with a double bond; R is an aldohexose, aldohexosamine, or N-acetyl aldohexosamine, W is O or S; X is O, S, or CH.sub.2 ; Y is a purine or pyrimidine base, Z is C, S, or O, and wherein when Z is S or O, A and C are not present. The compounds of this inverntion have enhanced pharmaceutical or biological activity or increased intracellular absorption compared to the corresponding parent nucleoside as a function of the 5'-diphosphohexose moiety. Many of these compounds have antiviral, including anti-HIV, activity. Others have antibacterial activity. In one embodiment, the invention is a method to treat HIV infection and opportunistic infections concomitantly.Type: GrantFiled: July 11, 1990Date of Patent: June 2, 1992Assignees: University of Georgia Research Foundation, Emory University, UAB Research FoundationInventors: Raymond F. Schinazi, Jean-Pierre Sommadossi, Chung K. Chu, William M. Shafer
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Patent number: 5116848Abstract: Certain N-2,6-dialkyl- or N-2,6-dialkoxphenyl-N'-diarylalkylurea compounds are potent inhibitors of the enzyme acyl CoA:cholesterol acyltransferase (ACAT), and are thus useful agents for the treatment of hypercholesterolemia or atherosclerosis with urea and thiourea compounds.Type: GrantFiled: March 30, 1988Date of Patent: May 26, 1992Assignee: Warner-Lambert CompanyInventor: Bharat K. Trivedi
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Patent number: 5112860Abstract: Thiocarboxylic esters of the formula I ##STR1## where the substituents have the following meanings: X is oxygen, sulfur, oxymethylene, methyleneoxy, thiomethylene, methylenethio, ethylene, ethenylene or ethynylene,Y, Z are each sulfur or oxygen, but Y and Z are not simultaneously oxygen,R is alkyl, mononuclear, dinuclear or trinuclear aryl or hetaryl, where aryl and hetaryl may be substituted,and fungicidal agents containing these compounds.Type: GrantFiled: November 2, 1990Date of Patent: May 12, 1992Assignee: BASF AktiengesellschaftInventors: Horst Wingert, Hubert Sauter, Siegbert Brand, Bernd Wenderoth, Gisela Lorenz, Eberhard Ammermann
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Patent number: 5102905Abstract: The invention concerns heterocyclic nitromethane derivatives of the formula 1 as defined hereinafter (and their non-toxic salts) wherein the heterocyclic moiety Q is thienyl, benzothienyl or dibenzothienyl and may bear a wide variety of optional substituents, together with pharmaceutical compositions containing them. The nitromethane derivatives are inhibitors of the enzyme aldose reductase and are of value in the treatment of certain complications of diabetes and galactosemia.Type: GrantFiled: April 28, 1989Date of Patent: April 7, 1992Assignee: Imperial Chemical Industries PLCInventors: Steven P. Brown, Anthony L. Cooper, Jethro L. Longridge, Jeffrey Morris, John Preston
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Patent number: 5073184Abstract: Compounds of formula (I): ##STR1## and stereoisomers thereof, wherein W is R.sup.1 O.sub.2 C--C.dbd.CH--ZR.sup.2, wherein R.sup.1 and R.sup.2, which are the same or different, are alkyl or fluoroalkyl groups, and Z is either an oxygen or sulphur atom; A is an oxygen or sulphur atom, --NR.sup.3 --, or --CR.sup.4 R.sup.5 --; X, Y and Z.sup.Type: GrantFiled: April 9, 1990Date of Patent: December 17, 1991Assignee: Imperial Chemical Industries PLCInventors: Vivienne M. Anthony, John M. Clough, Paul deFraine, Christopher R. A. Godfrey, Kevin Beautement
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Patent number: 5063243Abstract: Novel derivatives of caffeic acid of the general formula (I): ##STR1## wherein X is hydrogen atom or hydroxy; R.sup.1 is hydrogen atom, a straight or branched alkyl or alkenyl having 1 to 20 carbon atoms or a group of the formula:--(CH.sub.2).sub.n --Z--R.sup.2wherein n is an integer of 1 to 10; Z is oxygen atom, vinylene residue or a single bond; and R.sup.2 is a substituted or unsubstituted phenyl or heterocyclic residue is provided. These derivatives possess 12-lipoxygenase inhibitory activity and are useful for curing and preventing circulatory diseases. A pharmaceutical composition containing said derivtive is also provided.Type: GrantFiled: April 28, 1989Date of Patent: November 5, 1991Assignee: Suntory, Ltd.Inventors: Hidetsura Cho, Masaru Ueda, Mie Tamaoka, Mikiko Hamaguchi, Seiitsu Murota, Ikuo Morita
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Patent number: 5055471Abstract: This invention relates to derivatives of propanoic acid of the formula ##STR1## Useful as fungicides, insecticides and miticides, to processes for preparing them, to compositions containing them, and to methods of using them to combat fungi, especially fungal infections of plants, and to kill or control insects and mites.Type: GrantFiled: November 15, 1989Date of Patent: October 8, 1991Assignee: Imperial Chemical Industries PLCInventors: Paul J. de Fraine, Anne Martin
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Patent number: 5053430Abstract: Novel compounds having the general formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are as defined herein. These compounds are useful in the treatment of schizophrenia.Type: GrantFiled: September 22, 1989Date of Patent: October 1, 1991Assignee: Boehringer Ingelheim KGInventors: Matthias Grauert, Herbert Merz, Joachim Mierau, Gunter Schingnitz, Claus Schneider
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Patent number: 5039685Abstract: Novel O-alkylated oximes of the general formula I ##STR1## wherein R.sup.1 and R.sup.2 are optionally substituted aromatic or heteroaromatic rings, R.sup.3 is hydrogen or lower alkyl, R.sup.4 is a nitrogen containing, substituted ring or an amino group carrying a substituted ring, and n and m independently are 0, 1 or 2, are potent inhibitors of GABA reuptake from the synaptic cleft.Type: GrantFiled: May 10, 1989Date of Patent: August 13, 1991Assignee: Novo Nordisk A/SInventors: Lars J. S. Knutsen, Knud E. Andersen, Anker S. Jorgensen, Ursula Sonnewald
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Patent number: 5032609Abstract: The invention relates to compounds of general formula (I) and physiologically acceptable salts and solvates thereof, methods for their preparation and pharmaceutical formulations thereof. ##STR1## wherein Ar represents a substituted phenyl or nitrogen-containing heterocyclic ring;X and Y represent alkylene, alkenylene or alkynylene chains;R.sup.1, R.sup.2 and R.sup.18 each represent hydrogen or alkyl groups; andQ represents an optionally substituted furan or thiophene ring.The compounds of the invention have a stimulant action at .beta..sub.2 -adrenoreceptors and are useful in the treatment of diseases associated with reversible airways obstruction such as asthma and chronic bronchitis.Type: GrantFiled: December 16, 1988Date of Patent: July 16, 1991Assignee: Glaxo Group LimitedInventors: Ian F. Skidmore, Harry Finch, Alan Naylor, Lawrence H. C. Lunts, Charles Willbe, David Middlemiss
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Patent number: 5015656Abstract: A pharmaceutical compound of the formula ##STR1## in which R.sup.1, R.sup.2 and R.sup.3 independently are hydrogen, hydroxy, halo, nitro, amino, C.sub.2-5 acylamino, C.sub.1-4 alkyl, --CHO, --CH.sub.2 OH, --CH.sub.2 OC.sub.1-4 alkyl, --COOH, --COC.sub.1-3 alkyl, --CH(OH)C.sub.1-3 alkyl, C.sub.1-4 alkoxy, C.sub.2-4 alkenyloxy, C.sub.1-4 alkylthio, C.sub.1-4 alkylsulphinyl, C.sub.1-4 alkylsulphonyl, N-substituted heterocyclyl, optionally substituted phenyl, optionally substituted phenylthio, optionally substituted phenylsulphinyl, optionally substituted phenylsulphonyl or optionally substituted phenylsulphonamido, or R.sup.1 and R.sup.2 together form a C.sub.3-5 alkylene bridge; provided that at least one of R.sup.2 and R.sup.3 is C.sub.1-4 alkoxy or C.sub.2-4 alkenyloxy; and X is (i) --(CH.sub.2).sub.n N(R.sup.4).sub.2 where each R.sup.4 independently is C.sub.1-4 alkyl, C.sub.2-4 alkenyl or optionally substituted C.sub.6 H.sub.5 CH.sub.Type: GrantFiled: September 26, 1989Date of Patent: May 14, 1991Assignees: Lilly S.A., Lilly Industries LimitedInventors: Maria I. F. Fernandez, Terrence M. Hotten, David E. Tupper
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Patent number: 5010104Abstract: Novel tricyclic compounds having a TXA.sub.2 -antagonizing activity represented by formul (I): ##STR1## which strongly antagonize an action of thromboxane A.sub.2 and are expected to have preventive and therapeutic effects on ischemica diseases, cerebro-vascular diseases, etc.Type: GrantFiled: June 29, 1989Date of Patent: April 23, 1991Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Etsuo Oshima, Hiroyuki Obase, Akira Karasawa, Kazuhiro Kubo, Ichiro Miki, Akio Ishii
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Patent number: 4997847Abstract: The invention relates to phenylsulphonamidolkanoic acids which have thromboxane A.sub.2 receptor antagonist activity.Type: GrantFiled: August 22, 1988Date of Patent: March 5, 1991Assignees: Smith Kline & French Laboratories Limited, Boehringer Mannheim GmbHInventors: Robert J. Ife, David G. Cooper, Robert A. Slater, Karlheinz Stegmeier, Ernst-Christian Witte
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Patent number: 4997848Abstract: Compounds of formula (I): ##STR1## in which: R represents hydrogen, methyl of hydroxy; X represents an alkyl, alkenyl, cycloalkyl, aryl, aralkyl, or heterocyclic group; A represents a single bond, or an alkylene, alkenylene, alkynylene or alkadienylene group; Y represents hydrogen, or an aryl, cycloalkyl or heterocyclic group] have valuable antihypercholesteremic activities and may be used in the treatment of disorders arising from a blood cholesterol imbalance in humans and other animals.Type: GrantFiled: October 21, 1988Date of Patent: March 5, 1991Assignee: Sankyo Company, LimitedInventors: Masaaki Kurabayashi, Hiroshi Kogen, Hiroshi Kadokawa, Hideshi Kurihara, Kazuo Hasegawa, Masao Kuroda
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Patent number: 4994484Abstract: 1-(3-(2-hydroxy-3-alkylaminopropoxy)-2-thienyl)-3-phenyl-1-propanones represented by formula (I) ##STR1## wherein R.sub.1 and R.sub.2 each represent a lower alkyl group, and a process for the preparation of the same. The compounds of the present invention are useful in the treatment of cardiac arrhythmias.Type: GrantFiled: January 24, 1990Date of Patent: February 19, 1991Assignee: Laevosan-Gesellschaft m.b.H.Inventors: Dieter Binder, Gerhard Greier
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Patent number: 4994485Abstract: The invention relates to new thio compounds of the general formula ##STR1## wherein R is an alkyl group substituted or not substituted with halogen and having 1-12 carbon atoms, an alkenyl or alkynyl group having 2-4 carbon atoms, an alkadienyl group having 3 or 4 carbon atoms or a substituted or unsubstituted phenyl or phenyl(C.sub.1 -C.sub.4)alkyl group;R.sub.1 is a cyano group, a formyl group, an alkylcarbonyl or alkoxycarbonyl group substituted or unsubstituted with halogen and having 2-5 carbon atoms, a substituted or unsubstituted benzoyl group, or an alkylsulphonyl group having 1-4 carbon atoms;R.sub.2 is a hydrogen atom, a halogen atom, an amino group unsubstituted or substituted with one or two groups selected from C.sub.1 -C.sub.4 alkyl and C.sub.2 -C.sub.5 alkylcarbonyl, an amino group forming part of a heterocyclic ring which may comprise 1 or 2 additional heteroatoms selected from N, O and S, an alkyl or alkoxy group having 1-4 carbon atoms and optionally substituted with C.sub.2 -C.sub.Type: GrantFiled: August 14, 1990Date of Patent: February 19, 1991Assignee: Duphar International Research B.V.Inventors: Hendrik Dolman, Johannes Kuipers
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Patent number: 4983207Abstract: The invention relates to synergistic antifungal and plant-growth regulating compositions and to their application in plant-protection.The fungicides according to the invention contain the mixture of fungicide from the group of morpholines and acylalanines as active ingredients.Type: GrantFiled: March 3, 1986Date of Patent: January 8, 1991Assignee: Chinoin Gyogyszer es Vegyeszeti Termekek Gyara R.T.Inventors: Thomas Strumpf, Horst Lyr, Dieter Zanke, Gerlinde Zollfrank nee Baumann, Gyula Oros, Ferenc Viranyi, Tibor Ersek
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Patent number: 4981868Abstract: This invention relates to novel 3-heteroaryl-2-fluoro-1-olefins and their pharmacological use as dopamine beta-hydroxylase DBH inhibitors in the treatment of DBH mediated conditions such as hypertension.Type: GrantFiled: July 25, 1989Date of Patent: January 1, 1991Assignee: Merrell Dow PharmaceuticalInventors: James R. McCarthy, Donald P. Matthews, Charlotte L. Barney
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Patent number: 4980349Abstract: The invention relates to new compounds corresponding to formula I: ##STR1## in which: W represents C=O, CH.sub.2 or CHOH,Z represents ##STR2## R.sub.1 and R.sub.2 represent especially Cl or F, R, R' and R" represent especially H,X represents especially CH.sub.2,Y represents especially COOH,u and v are two integers ranging from 0 to 10,p and q take the value 0 or 1,n and m are two integers ranging 0 to 10 andt is 0 or 1the total number of carbon atoms in the chain ##STR3## ranging from 2 to 20, and to their physiologically acceptable salts obtained with organic or inorganic acids.These compounds are useful for preparing medicinal products which have, especially, anti-inflammatory properties.Type: GrantFiled: November 12, 1987Date of Patent: December 25, 1990Assignee: SANOFIInventors: Pierre Roger, Jean-Paul Fournier, Alain Martin, Jean Choay
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Patent number: 4978674Abstract: New antiarrythmic diamines are disclosed. pa These new compounds are represented by the following general formula: ##STR1## wherein: A is NO.sub.2, RSO.sub.2 NH or RSO.sub.2, whereinR represents a lower alkyl group.B is >CH.sub.2 or >C.dbd.O,Y is a lower alkyl group,Z is a lower alkyl or benzyl group,n is an integer 2 or 3.The compounds of the present invention are useful as antiarrhythmic agents.Type: GrantFiled: August 2, 1989Date of Patent: December 18, 1990Assignee: Kotobuki Seiyaku Co. Ltd.Inventors: Tsuyoshi Tomiyama, Akira Tomiyama, Shuichi Wakabayshi, Hironao Sajiki, Junko Sekiguchi
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Patent number: 4965254Abstract: The present invention relates to the use of the sulphenic acid amides of the general formula (I) ##STR1## in which X represents identical or different halogen atoms, Y.sup.1 and Y.sup.2 are identical or different and represent hydrogen, halogen, alkyl, alkoxy, halogenoalkyl or NO.sub.2 andZ represents halogen, --OH, --NHOH or the group --OR.sup.1,in whichR.sup.1 denotes optionally substituted radicals from the series comprising alkyl, alkenyl, alkinyl, cycloalkyl, aryl, aralkyl and heterocyclyl, orZ represents the group ##STR2## in which R.sup.2 and R.sup.3 are identical or different and denote hydrogen or a heterocyclic radical, orZ represents the group --OMin whichM denotes ammonium or the equivalent of an alkali metal, alkaline earth metal or heavy metal cation,for prolonging the duration of a high activity in agents for combating soil pests.Type: GrantFiled: September 25, 1986Date of Patent: October 23, 1990Assignees: Bayer Aktiengesellschaft, Mobay CorporationInventors: John Anderson, Bernhard Homeyer, Engelbert Kuhle, Hans Scheinpflug, Walter M. Zeck, Donald E. Simonet
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Patent number: 4962104Abstract: Fungicidal substituted 2-phenyl-2,2-difluoroethylthiolcarbonates of the formula ##STR1## in which R.sup.1 represents hydrogen, alkoxycarbonyl, alkoxyalkoxycarbonyl, alkylthioalkoxycarbonyl, halogenoalkoxycarbonyl, cyanoalkoxycarbonyl, alkenoxycarbonyl, alkynoxycarbonyl and cycloalkyloxycarbonyl, or represents cycloalkylalkoxycarbonyl,R.sup.2 represents hydrogen or alkyl, or represents phenyl, orR.sup.1 and R.sup.2 together represent the butadiene-1,4-diyl radical,R.sup.3 represents alkoxy, alkoxyalkoxy, alkylthioalkoxy, fluoroalkoxy, cyanoalkoxy, alkenoxy, alkynoxy, cycloalkyloxy and cycloalkylalkoxy, or represents the group ##STR2## in which R.sup.4 represents alkyl, alkoxyalkyl, alkylthioalkyl, cyanoalkyl, fluoroalkyl, alkenyl, alkinyl or cycloalkyl,R.sup.5 represents hydrogen, alkyl, alkoxyalkyl, alkylthioalkyl, fluoroalkyl, cyanoalkyl, alkenyl, alkinyl or cycloalkyl, orR.sup.4 and R.sup.Type: GrantFiled: December 6, 1989Date of Patent: October 9, 1990Assignee: Bayer AktiengesellschaftInventors: Werner Daum, Dietmar Bielefeldt, Wilhelm Brandes
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Patent number: 4962114Abstract: Compounds of the formula: ##STR1## wherein R.sub.1 is a lower alkyl of 1-6 carbon atoms, benzyl, phenyl or phenyl substituted by halogen, alkoxy of 1 to 4 carbon atoms, alkyl of 1 to 4 carbon atoms, amino, or carbonyl substitutents, or --RN(R').sub.2 wherein R and R' are each independently alkyl of 1 to 4 carbon atoms; R.sub.2 is an aromatic substituent, and each A is an aromatic substitution indpendently selected from the group consisting of hydrogen, alkyl of 1-4 carbon atoms, alkoxy of 1-4 carbon atoms, halogen, --NO.sub.2, --NH.sub.2,--COOH, and --NHCOCH.sub.3. The compounds have been found to be alkylating agents having antineoplastic activity for use in inhibiting the growth of tumors.Type: GrantFiled: June 4, 1987Date of Patent: October 9, 1990Assignee: Yale UniversityInventors: Alan C. Sartorelli, Krishnamurthy Shyam, Robert T. Hrubiec
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Patent number: 4960798Abstract: Acetylene compounds of the formula (I): ##STR1## wherein Y, R.sub.1, R.sub.2 R.sub.3, and R.sub.4 are as described herein, m is 0-3, n is 0-2 and Ar is phenyl or an aromatic heterocycle are disclosed. The compounds possess anti-hypertensive and anti-anginal properties and may be used in the treatment of humans. Methods for the preparation and use of such acetylene compounds are also disclosed.Type: GrantFiled: January 26, 1990Date of Patent: October 2, 1990Assignee: McNeilab, Inc.Inventor: John R. Carson
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Patent number: 4952580Abstract: Polyhaloalkene compounds of the formula: ##STR1## wherein X is sulfur, oxygen, or nitrogen, Y.sup.1 and Y.sup.2 are fluorine, Z is hydrogen or the same as Y.sup.1 and Y.sup.2, and n is 1-4; provided that:(A) when X is sulfur, Z is fluorine and R is thienyl or substituted thienyl, thianaphthyl or substituted thianaphthyl, thiazolinyl or substituted thiazolinyl, oxadiazolyl or substituted oxadiazolyl, 3,4,4-trifluoro-3-butenyloxycarbonylmethyl, thiadiazolyl substituted by halogen or R.sup.2 S, wherein R.sup.2 is 3,4,4-trifluoro-3-butenyl or R.sup.2 is phenylmethyl or phenylthiomethyl each optionally substituted by halogen or nitro; or R is thiadiazolyl substituted by R.sup.3, wherein R.sup.3 is substituted aryl, arylalkyl, aryloxyalkyl, alkylthio, haloalkylthio, haloarylthio, cyanoalkylthio, arylalkylthio, aryloxyalkylthio, arylthioalkylthio, heterocycloalkylthio, alkenylthio, haloalkenylthio, halocycloalkylalkenylthio, wherein said aryl or heterocyclic groups of R.sup.Type: GrantFiled: November 9, 1988Date of Patent: August 28, 1990Assignee: FMC CorporationInventors: Anthony J. Martinez, Thomas G. Cullen
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Patent number: 4952599Abstract: Novel substituted phenylthioureas, phenylisothioureas and phenylcarbodiimides of formula I ##STR1## wherein R.sub.1 is C.sub.1 -C.sub.10 alkyl, unsubstituted or substituted by one or more halogen atoms and/or C.sub.1 -C.sub.6 alkoxy groups; C.sub.3 -C.sub.6 alkenyl, C.sub.3 -C.sub.8 cycloalkyl, C.sub.3 -C.sub.8 cycloalkyl which is substituted by one or more halogen atoms and/or C.sub.1 -C.sub.4 alkyl groups; C.sub.3 -C.sub.8 cycloalkyl-C.sub.1 -C.sub.4 alkyl, di(C.sub.3 -C.sub.8)cycloalkyl-C.sub.1 -C.sub.4 alkyl; C.sub.1 -C.sub.4 phenylalkyl or C.sub.1 -C.sub.4 phenylalkyl which is substituted in the phenyl nucleus by one or more members selected from the group consisting of halogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy and/or C.sub.1 -C.sub.4 haloalkyl; or is C.sub.5 -C.sub.6 cycloalkenyl,R.sub.2 is hydrogen, C.sub.1 -C.sub.5 alkyl or C.sub.5 -C.sub.6 cycloalkenyl,R.sub.3 is C.sub.1 -C.sub.5 alkyl or C.sub.5 -C.sub.6 cycloalkyl,R.sub.4 is hydrogen or C.sub.1 -C.sub.3 alkyl,R.sub.Type: GrantFiled: July 20, 1988Date of Patent: August 28, 1990Assignee: Ciba-Geigy CorporationInventors: Josef Ehrenfreund, Manfred Boger, Jozef Drabek
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Patent number: 4948810Abstract: Novel phenoxyacetic acid derivative of the formula: ##STR1## wherein R is a substituted or unsubstituted phenyl group, naphthyl group or a sulfur-containing 5-membered hetero-monocyclic group, R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are hydrogen atom, a lower alkyl group, a phenyl-lower alkyl group or phenyl group, R.sup.5 is hydrogen atom or a lower alkyl group, R.sup.6 is carboxyl group, a protected carboxyl group, hydroxy group or a di(lower alkyl)-amino group, Ring A is a substituted or unsubstituted phenylene group, m is 0 or 1 and n is an integer 0 to 5, provided that, when m is 0,(1) at least either one of R.sup.1 to R.sup.4 is or/are a phenyl-lower alkyl group or phenyl group,(2) at least either one of R.sup.1 to R.sup.4 is or/are a lower alkyl group, and R.sup.6 is hydroxy group, or(3) all of R.sup.1 to R.sup.4 are hydrogen atom, and Ring A is a substituted phenylene group,or a pharmaceutically acceptable salt thereof are disclosed.Type: GrantFiled: February 6, 1989Date of Patent: August 14, 1990Assignee: Tanabe Seiyaku Co., Ltd.Inventors: Takeo Iwakuma, Takayuki Kawaguchi, Toyoharu Yamashita, Yasuhiko Sasaki, Tamotu Shimazaki
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Patent number: 4943584Abstract: Novel (p-phenoxyphenoxy)-methyl-five-membered heeroaromatic radicals of the formula ##STR1## where the substituents have the following meanings: R.sup.1, R.sup.2, R.sup.3 hydrogen, halogen, C.sub.1 -C.sub.8 -alkyl, C.sub.1 -C.sub.8 -alkoxy, C.sub.1 -C.sub.4 -haloalkyl, C.sub.1 -C.sub.4 -haloalkoxy, C.sub.3 -C.sub.10 -cycloalkyl, nitro or cyano,R.sup.4 hydrogen or C.sub.1 -C.sub.4 -alkyl, and a five-membered heteroaromatic ring, and their use for combating pests.Type: GrantFiled: April 20, 1988Date of Patent: July 24, 1990Assignee: BASF AktiengesellschaftInventors: Hans Theobald, Christoph Kuenast, Peter Hofmeister, Hans-Juergen Neubauer, Thomas Kuekenhoehner, Wolfgang Krieg, Joachim Leyendecker, Uwe Kardorff
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Patent number: 4933369Abstract: The present invention relates to new compounds of the formula ##STR1## and the pharmaceutically acceptable salts thereof and the enantiomers thereof, wherein R.sup.1 is H, lower alkyl, alkenyl, aralkyl, or C(O)R.sup.2 wherein R.sup.2 is lower alkyl, alkenyl, alkoxy, or aralkyl; n is an integer of from 2-4; m is an integer of from 0-4; A is S(O).sub.x wherein x is an integer of from 0-2; and Ar is phenyl or thienyl. These compounds are useful as analgesics.Type: GrantFiled: September 30, 1988Date of Patent: June 12, 1990Assignee: G. D. Searle & Co.Inventors: Barnett S. Pitzele, Nizal S. Chandrakumar, Donald W. Hansen, Jr., Gilbert W. Adelstein
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Patent number: 4929637Abstract: Thiophene-2-sulfonamides with an alkyl or substituted-alkyl and an alkyl-S(O).sub.n -substituent are carbonic anhydrase inhibitors useful in the treatment of elevated intraocular pressure.Type: GrantFiled: December 14, 1988Date of Patent: May 29, 1990Assignee: Merck & Co., Inc.Inventors: John J. Baldwin, Gerald S. Ponticello, Charles N. Habecker
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Patent number: 4920110Abstract: Propargyl furan- and thiophenecarboxylates of the formulae Ia and Ib ##STR1## where R.sup.1, R.sup.2 and R.sup.3 are each hydrogen, chlorine, bromine, nitro, C.sub.1 -C.sub.4 -alkyl, C.sub.2 -C.sub.4 -alkenyl, C.sub.1 -C.sub.4 -haloalkyl, C.sub.2 -C.sub.4 -haloalkenyl, or phenyl which is unsubstituted or substituted by halogen, C.sub.1 -C.sub.4 -alkyl, or C.sub.1 -C.sub.4 -alkoxy, X is oxygen or sulfur, n is the integer 0 or 1, and, if X is sulfur, R.sup.1, R.sup.2 and R.sup.3 may furthermore be fluorine, cyano, C.sub.1 -C.sub.4 -alkoxy, C.sub.1 -C.sub.4 -haloalkoxy, C.sub.2 -C.sub.4 -alkenyloxy or C.sub.2 -C.sub.4 -haloalkenyloxy, processes for their manufacture, and their use for combating pests.Type: GrantFiled: April 14, 1989Date of Patent: April 24, 1990Assignee: BASF AktiengesellschaftInventors: Hans-Jurgen Neubauer, Wolfgang Seppelt, Rainer Burstinghaus, Peter Hofmeister, Christoph Kuenast
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Patent number: 4913721Abstract: Compounds of formula (I): ##STR1## and stereoisomers thereof, wherein V is an oxygen or a sulphur atom; X and Y, which may be the same or different, are hydrogen or halogen atoms, or optionally substituted alkyl, optionally substituted alkenyl, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted alkynyl, haloalkyl, alkoxy, haloalkoxy, optionally substituted aryloxy, optionally substituted arylalkoxy, optionally substituted acyloxy, optionally substituted amino, acylamino, nitro, nitrile, --CO.sub.2 R.sup.3, --CONR.sup.4 R.sup.5, or --COR.sup.6 groups; or the groups X and Y, when they are in adjacent positions on the phenyl ring, may join to form a fused ring, either aromatic or aliphatic, optionally containing one or more heteroatoms; and Z is optionally substituted methylene, optionally substituted amino, oxygen or sulphur and when Z is a substituted methylene group, the substituent may join the 2-position of the phenyl ring to form a non-aromatic fused ring; R.sup.1 and R.Type: GrantFiled: October 31, 1988Date of Patent: April 3, 1990Assignee: Imperial Chemical Industries PLCInventors: John M. Clough, Christopher R. A. Godfrey
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Patent number: 4914123Abstract: Acyloxythiophenes of the formula ##STR1## in which R.sup.1 represents alkyl, alkoxyalkyl, alkylthioalkyl, halogenoalkyl, cyanoalkyl, trialkylsilylmethyl, alkenyl or alkinyl,R.sup.2 represents alkyl,n represents 0 or 1 andR.sup.3 to R.sup.5 are identical or different and represent hydrogen, alkyl, alkoxy, halogenoalkyl, halogenoalkoxy, halogenoalkylthio, halogenoalkylsulphinyl, halogenoalkylsulphonyl, N-halogenoalkyl-N-halogenoalkylthioamino, chlorine or fluorine andR.sup.6 and R.sup.7 represent hydrogen, fluorine, chlorine, nitro or trifluoromethyl, with the proviso that one of the radicals R.sup.3 to R.sup.7 is a fluorine-containing radical or at least 3 of the radicals R.sup.3 to R.sup.7 represent fluorine and/or chlorine,which possess fungicidal activity.Type: GrantFiled: January 11, 1985Date of Patent: April 3, 1990Assignee: Bayer AktiengesellschaftInventors: Werner Daum, Erich Klauke, Engelbert Kuhle, Wilhelm Brandes, Paul Reinecke
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Patent number: 4914126Type: GrantFiled: September 23, 1987Date of Patent: April 3, 1990Assignee: Fisons plcInventors: John Dixon, Francis Ince
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Patent number: 4914111Abstract: Thiophene (or furan)-2-sulfonamides with a 4-benzyl substituent are effective in the treatment of elevated intraocular pressure and glaucoma following topical ocular administration.Type: GrantFiled: March 23, 1987Date of Patent: April 3, 1990Assignee: Merck & Co., Inc.Inventors: George D. Hartman, Wasyl Halczenko
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Patent number: 4904686Abstract: Compounds of the following formula have pharmacutical properties: ##STR1## in which R.sup.1 and R.sup.2 independently are hydrogen, halo, nitro, amino, C.sub.2-5 acylamino, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 alkylthio, C.sub.1-4 alkylsulphonyl, N-substituted heterocyclyl, optionally substituted phenyl, optionally substituted phenylthio, optionally substituted phenylsulphonyl or optionally substituted phenylsulphonamido, or R.sup.1 and R.sup.2 together form a C.sub.3-5 alkylene bridge, R.sup.3 is C.sub.1-4 alkyl or C.sub.2-4 alkenyl, and X is (i) --(CH.sub.2).sub.n N(R.sup.4).sub.2 where each R.sup.4 independently is C.sub.1-4 alkyl, C.sub.2-4 alkenyl or optionally substituted C.sub.6 H.sub.5 CH.sub.2 --, and n is 1, 2 or 3, or (ii) a 5- to 8-membered alicyclic group containing one or two nitrogen atoms and directly attached to the amido nitrogen or attached by a C.sub.1-3 alkylene chain; and salts thereof.Type: GrantFiled: April 11, 1988Date of Patent: February 27, 1990Assignee: Lilly Industries LimitedInventors: Maria I. F. Fernandez, Terrence M. Hotten, David E. Tupper
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Patent number: 4898863Abstract: This invention provides a series of novel heterocyclic carboxamides of formula I in which the group --Y--Z< is selected from --C(Ra).dbd.C<, --N.dbd.C<, and --CH(Ra)--CH< and the other radicals have the meanings defined in the following specification.The compounds of formula I are leukotriene antagonists. The invention also provides pharmaceutically acceptable salts of the formula I compounds; pharmaceutical compositions containing the formula I compound, or their salts, for use in the treatment of, for example, allergic or inflammatory diseasxes, or endotoxic or traumatic shock conditions; and processes for the manufacture of the formula I compounds, as well as intermediates for use in such manufacture.Type: GrantFiled: April 15, 1987Date of Patent: February 6, 1990Assignee: ICI Americas Inc.Inventors: Frederick J. Brown, Ying K. Yee
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Patent number: 4898889Abstract: Acetylene compounds of the formula (I): ##STR1## wherein Y, R.sub.1, R.sub.2, R.sub.3, and R.sub.4 are as described herein, m is 0-3, n is 0-2 and Ar is phenyl or an aromatic heterocycle are disclosed. The compounds possess antihypertensive and anti-anginal properties and may be used in the treatment of humans. Methods for the preparation and use of such acetylene compounds are also disclosed.Type: GrantFiled: March 27, 1989Date of Patent: February 6, 1990Assignee: McNeilab, Inc.Inventor: John R. Carson
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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: 4880829Abstract: The invention relates to novel substituted tyrosyl alanine dipeptide amides of the formula: ##STR1## and the pharmaceutically acceptable acid addition salts thereof wherein R.sup.1 is hydrogen, lower alkyl, hydroxy, --OCO.sub.2 lower alkyl, lower alkoxy, --O(CH.sub.2).sub.n --phenyl with the phenyl optionally substituted by halogen, --NO.sub.2, --CN, --NH.sub.2 or lower alkyl wherein n is 1 to 4; R.sup.2 and R.sup.3 represent lower alkyl, halogen, or lower alkoxy, or either one of R.sup.2 or R.sup.3 is hydrogen and the other is lower alkyl, lower alkoxy or halogen; R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, and R.sup.9 may be the same or different and represent hydrogen or lower alkyl; R.sup.Type: GrantFiled: January 20, 1988Date of Patent: November 14, 1989Assignee: G. D. Searle and CompanyInventors: Donald W. Hansen, Jr., Barnett S. Pitzele, Michael Clare, Robert W. Hamilton
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Patent number: 4871761Abstract: Novel pesticides of the formula ##STR1## in which R.sup.1 represents in each case optionally substituted cycloalkyl, cycloalkenyl, tetrahydronaphthyl, decahydronaphthyl, phenyl, naphthyl or thienyl,R.sup.2 represents alkyl,R.sup.3 represents hydrogen alkyl, alkenyl, alkinyl, hydroxyalkyl, alkoxyalkyl, dialkoxyalkyl, hydroxyalkoxyalkyl, cyano or formyl, or in each case optionally substituted cycloaklyl, cycloalkenyl, cycloalkylalkyl, cycloalkenylalkyl, aralkyl, aryl, furanylmethyl or tetrahydrofuranylmethyl,R.sup.4 represents hydrogen or alkyl, andHet represents an optionally substituted heterocyclic ring of the formula ##STR2## and acid-addition salts thereof.Type: GrantFiled: March 18, 1988Date of Patent: October 3, 1989Assignee: Bayer AktiengesellschaftInventors: Detlef Wollweber, Stefan Dutzmann
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Patent number: 4868183Abstract: Disclosed are compounds of the formula ##STR1## wherein: R.sup.1 is a lower alkyl group;R.sup.2 and R.sup.3 are each hydrogen or lower alkyl or R.sup.2 and R.sup.3 taken together may form --(CH.sub.2 (.sub.4)-- or --CH.dbd.CH--CH.dbd.CH--;.alpha. is a 5- or 6-membered heteroaromatic ring group containing 1 to 3 hetero-atoms selected from the group consisting of nitrogen, oxygen and sulfur, or a pyrazine-N-oxide ring, pyridazine-N-oxide ring or pyrimidine-N-oxide ring group, wherein each of these heteroaromatic ring groups may optionally have 1 to 3 substituents selected from the group consisting of a lower alkyl, halogen, phenyl, lower alkoxycarbonyl, amino, lower alkoxy and hydroxy-lower alkyl, with the proviso that said 5- or 6-membered heteroaromatic ring group is not thiazolyl, isothiazolyl, pyridyl or 1,3,5-triazinyl group; or salts thereof. These compounds and salts thereof have anti-inflammatory activity and lipoxygenase-inhibitory activity.Type: GrantFiled: July 20, 1987Date of Patent: September 19, 1989Assignee: Otsuka Pharmaceutical Factory, Inc.Inventors: Kenichi Kanai, Kiyoto Goto, Kinji Hashimoto
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Patent number: 4863954Abstract: Novel fungicidally active acyloxythiophene-carboxamides of the formula ##STR1## in which R.sup.1 represents alkyl, alkoxyalkyl, alkylthioalky, fluoroalkyl, cyanoalkyl, alkenyl, alkinyl or cycloalkyl,R.sup.2 represents alkyl or optionally substituted phenyl,R.sup.Type: GrantFiled: May 17, 1988Date of Patent: September 5, 1989Assignee: Bayer AktiengesellschaftInventors: Werner Daum, Gerd Hanssler
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Patent number: 4863503Abstract: Compounds of formula (I): ##STR1## and stereoisomers thereof, wherein W is R.sup.1 O.sub.2 C--C.dbd.CH--ZR.sup.2, wherein R.sup.1 and R.sup.2, which are the same or different, are alkyl or fluoroalkyl groups, and Z is either an oxygen or sulphur atom; A is an oxygen or sulphur atom, --NR.sup.3 --, or --CR.sup.4 R.sup.5 --; X, Y and Z.sup.Type: GrantFiled: April 17, 1987Date of Patent: September 5, 1989Assignee: Imperial Chemical Industries PLCInventors: Vivienne M. Anthony, John M. Clough, Paul de Fraine, Christopher R. A. Godfrey, Kevin Beautement