Chalcogen Bonded Directly To Ring Carbon Of The Hetero Ring Patents (Class 514/445)
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Patent number: 4859699Abstract: Substituted N-benzoyl-N'-thienylureas, processes for making these compounds, intermediates therefor and the use of the compounds for the control of pests, and in particular for the control of insects and acarids.Type: GrantFiled: February 23, 1989Date of Patent: August 22, 1989Assignee: Sandoz Ltd.Inventors: Robert L. Carney, Alfred S. T. Lui, Fred Kuhnen, John M. Gruber
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Novel class of acyl-derivatives of carnitine, process for preparing same and therapeutic use thereof
Patent number: 4859698Abstract: A novel class of acyl-derivatives of carnitine is disclosed wherein the acyl radical is either the radical of unsaturated organic acids (typically, acrylic acid) or the radical of saturated organic acids substituted with tert-alkyl, cycloalkyl, cycloalkenyl, alkoxyl, heterocyclic and carboalkoxylradicals, or with aldehyde or hydroxy groups. These acyl-derivatives of carnitine are useful therapeutical agents in the treatment of cardiac disorders, hyperlipidaemias and hyperlipoproteinaemias.Type: GrantFiled: May 31, 1988Date of Patent: August 22, 1989Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.Inventors: Claudio Cavazza, Paolo De Witt, Maria O. Tinti -
Patent number: 4847288Abstract: The present invention relates to compounds which are allenyl amines, more specifically, .beta.-ethenylidene-(substituted)ethanamines, possessing antihypertensive activity. They are prepared by a noval reaction of a protected N,N-bis(trimethylsilyl)-4-methoxy-2-butynylamine compound with a metallo-organic compound, with subsequent removal of the silyl protecting groups to provide the desired compound.Type: GrantFiled: February 8, 1988Date of Patent: July 11, 1989Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: James R. McCarthy, Thomas M. Bargar, Charlotte L. Barney, Donald P. Matthews, Robert J. Broersma
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Patent number: 4847289Abstract: Aryl (or aralkyl)-sulfonylthiophene-2-sulfonamides containing a basic functional group as a substituent are efficacious in the treatment of elevated intraocular pressure and glaucoma following topical ocular administration.Type: GrantFiled: June 8, 1987Date of Patent: July 11, 1989Assignee: Merck & Co., Inc.Inventors: John J. Baldwin, Charles M. Habecker, Samuel L. Graham, Wasyl Halczenko, George D. Hartman, Harvey Schwam, Gerald S. Ponticello, Kenneth L. Shepard
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Patent number: 4833161Abstract: The present invention provides carboxylic acid derivatives of the general formula: ##STR1## wherein R.sub.1 and R.sub.2, which can be the same or different, are optionally substituted aryl radicals or optionally substituted heterocyclic radicals, A is a straight-chained or branched, saturated or unsaturated alkylene chain containing up to 10 carbon atoms which can contain an oxygen, sulphur or nitrogen atom and is optionally substituted by a hydroxyl group, Y is an S(O).sub.n group or an oxygen atom, n is 0, 1 or 2 and B is a valency bond or a saturated or unsaturated alkylene radical containing up to 5 carbon atoms; as well as the physiologically acceptable salts, esters and amides thereof, with the proviso that(a) R.sub.1 and R.sub.2 are not simultaneously aryl radicals and(b) when an unsaturated alkylene chain is present which contains a heteroatom, the heteroatom is not connected to an unsaturated aliphatic carbon atom.Type: GrantFiled: January 6, 1988Date of Patent: May 23, 1989Assignee: Boehringer Mannheim GmbHInventors: Hans P. Wolff, Hans-Frieder Kuhnle
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Patent number: 4829078Abstract: This invention relates to compounds presented by the general formula: ##STR1## [wherein R.sup.1 and R.sup.2 are: (i) R.sup.1, R.sup.2 and carbon atoms to which R.sup.1 and R.sup.2 are linked, together represent the group of the general formula: ##STR2## (wherein R.sup.5 and R.sup.6 represent hydrogen, alkyl, cycloalkyl, cycloalkyl-alkyl or phenyl, independently, with the proviso that R.sup.5 and R.sup.6 is not hydrogen atoms at the same time), or(ii) R.sup.1 represents hydrogen and R.sup.2 represents the group of the formula: --COR.sup.7 (wherein R.sup.7 represents the group of the formula: ##STR3## (wherein Y represents a single-bond, alkylene, alkenylene, W represents oxygen or sulfur, m represents 1 to 3, R.sup.8 represents hydrogen, halogen, nitro, hydroxy, alkyl or alkoxy, with the proviso that when m represents two or more, plural R.sup.8 s may be different each, and R.sup.9 represents hydrogen, alkyl or phenyl group, with the proviso that two of R.sup.9 may be different each)), R.sup.Type: GrantFiled: February 22, 1988Date of Patent: May 9, 1989Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Katsuhiro Imaki, Tadao Okegawa, Yoshinobu Arai
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Patent number: 4814330Abstract: Therapeutically useful 1-[3-(2-dialkylaminoethoxy)-2-thienyl]-3-phenyl-1-propanones of the formula ##STR1## and acid addition salts thereof, wherein R and R.sub.1 each are hydrogen or methyl,R.sub.2 and R.sub.3, which are the same or different, each are alkyl, cycloalkyl, alkenyl or alkynyl each containing up to 8 carbon atoms, orR.sub.2 and R.sub.3 together with the nitrogen atom to which they are attached form a 5 to 7-membered saturated ring or a saturated heterocyclic ring which may contain optionally an oxygen or nitrogen atom as further hetero atom in the ring, a further nitrogen atom being unsubstituted or substituted by an alkyl radical containing 1 to 3 carbon atoms.The compounds are useful for the treatment of various disturbances of the heart rhythm.Type: GrantFiled: March 11, 1987Date of Patent: March 21, 1989Inventor: Dieter Binder
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Patent number: 4812463Abstract: Alkane sulfonamides with an electron withdrawing function .beta. to the sulfonamide group are topically effective carbonic anhydrase inhibitors useful in the treatment of elevated intraocular pressure and glaucoma.Type: GrantFiled: December 10, 1987Date of Patent: March 14, 1989Assignee: Merck & Co., Inc.Inventors: Samuel L. Graham, Thomas H. Scholz
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Patent number: 4808762Abstract: Compounds of the formula ##STR1## in which Ar is substituted or unsubstituted phenyl, naphthyl, or thienyl; Z is oxygen, sulfur, or methylene; and Ar' is 2-methyl[1,1'-biphenyl]-3-yl, 3-phenoxyphenyl, 4-fluoro-3-phenoxyphenyl, or 6-phenoxy-2-pyridyl exhibit pyrethroid-like insecticidal and acaricidal activity and are relatively harmless to aquatic fauna.Type: GrantFiled: September 9, 1987Date of Patent: February 28, 1989Assignee: FMC CorporationInventors: Gary A. Meier, Scott M. Sieburth, Thomas G. Cullen, John F. Engel
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Patent number: 4802913Abstract: 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: August 5, 1986Date of Patent: February 7, 1989Assignee: Imperial Chemical Industries PLCInventors: John Clough, Christopher R. A. Godfrey
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Patent number: 4788184Abstract: 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: November 13, 1987Date of Patent: November 29, 1988Assignee: Bristol-Myers CompanyInventors: Aldo A. Algieri, Ronnie R. Crenshaw
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Patent number: 4780317Abstract: A sustained release antimicrobial agent comprises a clathrate compound composed of a water-soluble microbicide and at least one of the compounds shown at (I) to (V) below:(I) 1,1'-bi-2-naphthol;(II) 1,1,4,4-tetraphenyl-2-butyn-1,4-diol;(III) 9,10-di(4-methylphenyl)-9,10-dihydroznthracene-9,10-diol;(IV) 1,1-bis(4-hydroxyphenyl)-cyclohexane; and(V) 1,1,6,6-tetra(2,4-dimethylphenyl)-2,4-hexadiyne-1,6-diol.A method which uses it for preventing the fouling of a water system is also disclosed.Type: GrantFiled: January 22, 1987Date of Patent: October 25, 1988Assignee: Kurita Water Industries Ltd.Inventors: Ayako Sekikawa, Hideo Sugi, Kenji Tahara, Fumio Toda
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Patent number: 4778818Abstract: Substituted cinnamyl-2,3-dihydrobenzofurans and analogs were prepared from the nucleophlic substitution of a cinnamylhalide with a 2,3-dihydrobenzofuran anion or an analog thereof. These compounds were found to be potent topical anti-inflammatory agents.Type: GrantFiled: April 17, 1987Date of Patent: October 18, 1988Assignee: Merck & Co., Inc.Inventors: Michael N. Chang, Norman P. Jensen, Milton L. Hammond, Robert A. Zambias, John McDonald, Kathleen M. Rupprecht
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Patent number: 4767758Abstract: A pharmaceutical composition containing a thiophene compound of formula: ##STR1## where R.sub.1, R.sub.2, R.sub.3 and R.sub.4 have the meanings given in the description, or a pharmaceutically acceptable addition salt thereof.Said pharmaceutical compositions are useful in treating tumors.New thiophene compounds are also described.Type: GrantFiled: February 26, 1987Date of Patent: August 30, 1988Assignee: Consiglio Nazionale Delle RicercheInventors: Alberto Breccia, Adamo Fini
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Patent number: 4767757Abstract: Novel fungicidally active acyloxythiophene-carboxamides of the formula ##STR1##Type: GrantFiled: March 19, 1987Date of Patent: August 30, 1988Assignee: Bayer AktiengesellschaftInventors: Werner Daum, Gerd Hanssler
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Patent number: 4760067Abstract: Organic sulfoxides having a latent allyl group bound to the sulfur are enzyme inhibitors of the suicide or K.sub.cat type.Type: GrantFiled: March 9, 1987Date of Patent: July 26, 1988Assignee: Merck & Co., Inc.Inventor: Raymond A. Firestone
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Patent number: 4757085Abstract: Fungicidally active carbamoyloxythiophene derivatives of the formula ##STR1## in which R.sup.1 represents alkyl, alkoxyalkyl, alkylthioalkyl, fluoroalkyl, cyanoalkyl, alkenyl, alkynyl, or cycloalkyl,R.sup.2 represents alkyl, optionally substituted furyl or optionally substituted phenyl,R.sup.3 represents aliphatic or carbocyclic cyanoalkyl, the ##STR2## radical or the --A.sup.2 --CO--OR.sup.6 radical, where A.sup.1 represents an alkylene radical,A.sup.2 represents an alkylene radical or denotes a direct bond,R.sup.4 and R.sup.5, independently of one another, represent alkyl, orR.sup.4 and R.sup.5, together with the nitrogen atom which they neighbor, form a heterocyclic ring which may contain further hetero atoms and is optionally substituted, andR.sup.6 represents alkyl,and novel intermediates therefor.Type: GrantFiled: April 13, 1987Date of Patent: July 12, 1988Assignee: Bayer AktiengesellschaftInventors: Werner Daum, Gerd Hanssler, Pieter Ooms
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Patent number: 4755527Abstract: The present invention relates to new compounds of the formula ##STR1## where X is ##STR2## alkylene, or --S--where R.sub.1 is hydrogen, alkyl, or aryl; W is hydrogen, hydroxy, amino, alkyloxy, aryloxy, O-alkyl, or O-aralkyl; (Y).sub.A) is --CH.sub.2 NR.sub.2 R.sub.3 where R.sub.2 and R.sub.3 may be hydrogen, substituted alkyls, aryls, or together with N form a 5 to 7 membered heterocyclic group; and Ar is a substituted or unsubstituted aryl. These compounds are useful in the treatment of various cardiac arrhythmias.Type: GrantFiled: December 27, 1985Date of Patent: July 5, 1988Assignee: E. I. Du Pont de Nemours and CompanyInventors: David M. Stout, William L. Matier
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Patent number: 4752607Abstract: Alkoxycarbonyl-substituted hydroxythiophenecarboxamides of the formula ##STR1## in which R.sup.1 represents alkyl, alkoxyalkyl, alkylthioalkyl, fluoroalkyl, cyanoalkyl, alkenyl or alkinyl or represents cycloalkyl,R.sup.2 represents alkyl or optionally substituted phenyl,R.sup.3 represents alkyl, alkoxyalkyl, alkylthioalkyl, cyanoalkyl, fluoroalkyl, alkenyl, alkinyl, cycloalkyl or alkoxy andR.sup.4 represents hydrogen, alkyl, alkoxyalkyl, alkylthioalkyl, fluoroalkyl, cyanoalkyl, alkenyl, alkinyl or cycloalkyl, orR.sup.3 and R.sup.4, together with the nitrogen atom, represent a heterocyclic radical which is optionally substituted by alkyl and can be further substituted in the alkylene chain by oxygen, sulphur or nitrogen,are useful as fungicides and intermediates.Type: GrantFiled: June 17, 1986Date of Patent: June 21, 1988Assignee: Bayer AktiengesellschaftInventors: Werner Daum, Gerd Hanssler
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Patent number: 4743617Abstract: This invention relates to novel heterocyclyl-2-propyn-1-amines which are useful as dopamine beta hydroxylase inhibitors in the treatment of hypertension.Type: GrantFiled: August 31, 1987Date of Patent: May 10, 1988Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Thomas M. Bargar, Lawrence C. Creemer, James R. McCarthy
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Patent number: 4743602Abstract: According to the invention there are provided compounds useful for combatting fungi having the general formula (I): ##STR1## and stereoisomers thereof, wherein one of X and Y, but not both, is a group of the formula (II): ##STR2## and the other of X and Y is a hydrogen atom, a halogen atom, or an alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, alkynyl, aryl, aralkyl, alkoxy, aryloxy or haloalkyl group or a ##STR3## group wherein R.sup.9, R.sup.10 and R.sup.11 can be alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl or aryl, Z is an oxygen atom, a sulphur atom or an --NH-group, A and B have the same significance as X or Y excluding a group of formula (II), R.sup.1, R.sup.2, R.sup.3 and R.sup.4 each represent a hydrogen atom, a halogen atom or an alkyl group containing from 1 to 4 carbon atoms, R.sup.5 and R.sup.6 each represent a hydrogen atom or an alkyl group containing from 1 to 4 carbon atoms, and R.sup.7 and R.sup.8 each represent an alkyl group containing from 1 to 4 carbon atoms or R.sup.7 and R.sup.Type: GrantFiled: June 30, 1987Date of Patent: May 10, 1988Assignee: Imperial Chemical Industries PLCInventors: Paul A. Worthington, Vivienne M. Anthony
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Patent number: 4742077Abstract: Compounds of formula I ##STR1## wherein R.sub.1 represents a group of formula ##STR2## whereby R.sub.4 and R.sub.5 are the same or different and represent hydrogen, halogen, lower alkyl, lower alkoxy or trifluoromethyl and X represents oxygen, sulfur, imino, lower alkylimino, --(CH.sub.2)--, --(S.CH.sub.2)-- or --(O.CH.sub.2)--,R.sub.2 represents hydrogen or lower alkyl,R.sub.3 represents a group of formula ##STR3## whereby R.sub.6, R.sub.7 and R.sub.8 are the same or different and represent hydrogen or alkyl or R.sub.6 together with R.sub.7 or R.sub.7 together with R.sub.8 represent --(CH.sub.2).sub.m -- wherein m is 3 to 6,R.sub.9 represents alkyl, alkenyl, trialkylsilyl or alkyl substituted by hydroxy, lower alkoxy, lower halogenalkyl or aryl andn stands for 1, 2 or 3,which possess pharmaceutical in particular antimycotic activity as well as activity against phytopathogenic fungi.Type: GrantFiled: September 8, 1986Date of Patent: May 3, 1988Assignee: Sandoz Ltd.Inventor: Anton Stutz
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Patent number: 4730005Abstract: The compounds represented by the following structural formula (I) ##STR1## wherein m is 1 or 2; n is 1, 2 or 3; R' is hydrogen or methyl; R is a radical selected from the group consisting of: ##STR2## wherein R.sub.1 is C.sub.8 to C.sub.13 alkyl, C.sub.7 to C.sub.12 alkoxy, C.sub.7 to C.sub.12 thioalkyl, C.sub.10 to C.sub.12 1-alkynyl, 11-dodecynyl, 1-trans-dodecenyl, 5-(4-acetyl-3-hydroxy-2-propylphenoxypentoxy, 2(Z), 5(Z)-undecadienyloxy, phenyl-C.sub.4 to C.sub.10 alkyl with the phenyl optionally mono substituted with bromo, chloro, trifluoromethyl, methoxy, methylthio or trifluoromethylthio, phenylthio-C.sub.3 to C.sub.9 alkyl with the phenyl optionally mono substituted with bromo, chloro, trifluoromethyl, methoxy, methylthio or trifluoromethylthio, phenyl-CH.dbd.CH--(CH.sub.2).sub.2-8, phenyl-C.sub.3 to C.sub.9 alkoxy, trifluoromethyl-C.sub.7 to C.sub.12 alkyl, cyclohexyl- C.sub.4 to C.sub.10 alkyl or ##STR3## wherein each q is 0, 1, 2 or 3 but the sum of both q's does not exceed 3, and R.sub.Type: GrantFiled: May 16, 1986Date of Patent: March 8, 1988Assignee: SmithKline Beckman CorporationInventors: John G. Gleason, Carl D. Perchonock
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Patent number: 4728666Abstract: Heterocyclic acetylenes of the formula (I): ##STR1## wherein Y and R.sup.1 are substituents such as hydrogen, alkyl, alkoxy, chloro or fluoro, m is 0-2, R.sup.2 is branched alkyl and Het is an aromatic heterocycle. The acetylenes are useful in treating hypertension and/or angina.Type: GrantFiled: November 24, 1986Date of Patent: March 1, 1988Assignee: McNeilab, Inc.Inventor: John R. Carson
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Patent number: 4725602Abstract: Acetylenes of the following formula (I): ##STR1## wherein Y, m, R.sup.1, R.sup.2, R.sup.3, n and R.sup.4 are defined herein and R.sup.5 is hydrogen, alkyl, cycloalkyl or substituted alkyl are useful vasodilators and antihypertensives.Type: GrantFiled: October 24, 1985Date of Patent: February 16, 1988Assignee: McNeilab, Inc.Inventor: John R. Carson
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Patent number: 4721794Abstract: Thiophene-2-sulfonamides with a 5-alkyl-S(O).sub.n -substituent are carbonic anhydrase inhibitors useful in the treatment of elevated intraocular pressure.Type: GrantFiled: July 30, 1986Date of Patent: January 26, 1988Assignee: Merck & Co., Inc.Inventors: Kenneth L. Shepard, Samuel L. Graham
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Patent number: 4707491Abstract: .gamma.-Thiobutyrolactone derivatives having short chain .alpha.- and/or .gamma.-alkyl or alkenyl substituents have useful anticonvulsant properties.Type: GrantFiled: December 20, 1985Date of Patent: November 17, 1987Assignee: Washington UniversityInventors: Douglas F. Covey, Jeffrey A. Levine, James A. Ferrendelli
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Patent number: 4690944Abstract: Compounds of formula I ##STR1## wherein A represents: a saturated cyclic or heterocyclic aromatic or heteroaromatic residue;a saturated or unsaturated bicyclic residue; and R represents H, an alkyl, cycloalkyl or alkoxyalkyl group.Compounds I are endowed with valuable therapeutic characteristics.Type: GrantFiled: February 19, 1986Date of Patent: September 1, 1987Assignee: Chiesi Farmaceutici S.p.A.Inventors: Paolo Chiesi, Vittorino Servadio
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Patent number: 4689343Abstract: Novel fungicidal active thiolane-2,4-dione-3-carboxamides of the formula ##STR1## in which R is alkyl, cycloalkyl, optionally substituted aralkyl or optionally substituted aryl, andR.sup.1 and R.sup.2 each independently is hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, aralkyl or aryl.Type: GrantFiled: April 21, 1986Date of Patent: August 25, 1987Assignee: Bayer AktiengesellschaftInventors: Herbert Gayer, Wilhelm Brandes, Gerd Hanssler, Paul Reinecke
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Patent number: 4668697Abstract: Novel 2-sulfamoylbenzo[b]thiophenes and derivatives thereof are shown to be useful for the treatment of elevated intraocular pressure in compositions including ophthalmic drops and inserts.Type: GrantFiled: April 16, 1984Date of Patent: May 26, 1987Assignee: Merck & Co., Inc.Inventors: Kenneth L. Shepard, Samuel L. Graham
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Patent number: 4665090Abstract: Thiophene-2-sulfonamides with a 5-alkyl-substituent are carbonic anhydrase inhibitors useful in the treatment of elevated intraocular pressure.Type: GrantFiled: October 9, 1985Date of Patent: May 12, 1987Assignee: Merck & Co., Inc.Inventor: Samuel L. Graham
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Patent number: 4656180Abstract: Diamine derivatives corresponding to the general formula IR.sup.1 R.sup.2 N--(CH.sub.2).sub.m --Q--A--NH--R--NH--B--Q'--(CH.sub.2).sub.n NR.sup.3 R.sup.4 (I)which have a highly selective action on histamine-H.sub.2 receptors and are therefore suitable for use as anti-ulcerative agents are described. Processes for the preparation of these compounds and pharmaceutical preparations containing these compounds are also described.Type: GrantFiled: March 5, 1985Date of Patent: April 7, 1987Assignee: Ludwig Heumann & Co., GmbHInventors: Stefan Postius, Rolf Herter, Peter Morsdorf, Helmut Schickaneder, Istvan Szelenyi, Kurt H. Ahrens
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Patent number: 4649154Abstract: The invention relates to new nitrothiophenes of the general formula ##STR1## wherein R is an alkyl group having 1 to 12 carbon atoms, which alkyl group may be substituted with a phenyl group substituted, if desired, with nitro, halogen, alkyl with 1 to 4 carbon atoms or alkoxy with 1 to 4 carbon atoms, with an alkoxycarbonyl group having 2 to 5 carbon atoms, or with a thiocyanato group,or R is a phenyl group, a pyridyl group or an N-oxypyridyl group, which groups may be substituted with nitro, halogen, alkyl with 1 to 4 carbon atoms, or alkoxy with 1 to 4 carbon atoms;R.sub.1 is a hydrogen atom, a halogen atom, an alkyl group having 1 to 4 carbon atoms, or a phenyl group substituted or not substituted with nitro, halogen, alkyl with 1 to 4 carbon atoms, or alkoxy with 1 to 4 carbon atoms;R.sub.2 is a hydrogen atom, an alkyl group having 1 to 4 carbon atoms, a cyano group, an alkanoyl group having 1 to 5 carbon atoms, an .alpha.,.alpha.-dialkoxyalkyl- or .alpha.,.alpha.Type: GrantFiled: October 20, 1983Date of Patent: March 10, 1987Assignee: Duphar International Research B.V.Inventors: Hendrik Dolman, Johannes Kuipers
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Patent number: 4636505Abstract: Acylanilides of the formula ##STR1## wherein R.sup.1 and R.sup.2, the same or different, each is cyano, carbamoyl, nitro, halogeno, perfluoroalkyl or other defined substituents;R.sup.3 is hydrogen or halogen;R.sup.4 is hydrogen or alkyl, or is joined to R.sup.5 ;R.sup.5 is hydrogen, hydroxy, alkoxy or acyloxy or is joined to R.sup.4 ;R.sup.6 is alkyl or halogenoalkyl, or has the formula --A.sup.3 --R.sup.8 or --A.sup.4 --X.sup.2 --A.sup.5 --R.sup.9 ;A.sup.1 and A.sup.4, the same or different, each is alkylene;A.sup.2, A.sup.3 and A.sup.5, the same or different, each is a direct link or alkylene;X.sup.1 and X.sup.2, the same or different, each is oxygen, sulphur, sulphinyl, sulphonyl, imino or alkylimino;R.sup.7 and R.sup.9, the same or different, each is alkyl, alkenyl, hydroxyalkyl, cycloalkyl, phenyl optionally substituted, naphthyl or heterocyclic optionally substituted;and R.sup.8 is phenyl, naphthyl or heterocyclic as defined above for R.sup.7 or R.sup.Type: GrantFiled: July 15, 1983Date of Patent: January 13, 1987Assignee: Imperial Chemical Industries PLCInventor: Howard Tucker
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Patent number: 4608385Abstract: Use of an N-phenylcarbamate of the formula: ##STR1## as a fungicidal agent against phytopathogenic fungi, particularly their strains resistant to benzimidazole thiophanate fungicides and/or cyclic imide fungicides.Type: GrantFiled: October 22, 1982Date of Patent: August 26, 1986Assignee: Sumitomo Chemical Company, LimitedInventors: Hiroshi Noguchi, Toshiro Kato, Junya Takahashi, Yukio Ishiguri, Shigeo Yamamoto, Katsuzo Kamoshita
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Patent number: 4599350Abstract: Novel fungicidal active thiolane-2,4-dione-3-carboxamides of the formula ##STR1## in which R is alkyl, cycloalkyl, optionally substituted aralkyl or optionally substituted aryl, andR.sup.1 and R.sup.2 each independently is hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, aralkyl or aryl.Type: GrantFiled: November 27, 1984Date of Patent: July 8, 1986Assignee: Bayer AktiengesellschaftInventors: Herbert Gayer, Wilhelm Brandes, Gerd Hanssler, Paul Reinecke
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Patent number: 4585787Abstract: 5-[2(or 3)-Hydroxyphenylsulfonyl]thiophene-2-sulfonamides are useful for the topical treatment of elevated intraocular pressure. Ophthalmic compositions including drops and inserts are disclosed.Type: GrantFiled: August 12, 1985Date of Patent: April 29, 1986Assignee: Merck & Co., Inc.Inventor: Kenneth L. Shepard
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Patent number: 4565826Abstract: This invention relates to a novel class of heterocyclic amidinourea and heterocyclic amidinothiourea compounds wherein the heterocyclic substitution is at the 1-N urea nitrogen atom. These compounds exhibit pharmaceutical activity and may be incorporated into pharmaceutical preparations for producing anti-ulcerogenic, antisecretory, antispasmodic, antimotility, cardiovascular, antidiarrheal or antiparasitic action.Type: GrantFiled: February 24, 1984Date of Patent: January 21, 1986Assignee: William H. Rorer, Inc.Inventors: William L. Studt, Harry K. Zimmerman, George H. Douglas
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Patent number: 4542152Abstract: 5-[Phenylsulfonyl(or sulfinyl)]thiophene-2-sulfonamides are useful for the topical treatment of elevated intraocular pressure. Ophthalmic compositions including drops and inserts are disclosed.Type: GrantFiled: June 20, 1983Date of Patent: September 17, 1985Assignee: Merck & Co., Inc.Inventor: Kenneth L. Shepard
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Patent number: 4537897Abstract: Novel 3-(1,2-propadienyl)-cyclopropane-carboxylates of the formula ##STR1## wherein R is alcohol used in pyrethrinoid synthesis, X and Y are both hydrogen or individually halogen or X is hydrogen or halogen and Y is alkyl of 1 to 18 carbon atoms or halogen or X is hydrogen or halogen or alkyl of 1 to 18 carbon atoms and Y is --COOR' or --CN or ##STR2## R' is alkyl of 1 to 18 carbon atoms, R.sub.2 and R.sub.3 are individually hydrogen or alkyl of 1 to 18 carbon atoms or R.sub.2 and R.sub.3 together with the nitrogen atom form a heterocycle having pesticidal properties.Type: GrantFiled: September 15, 1983Date of Patent: August 27, 1985Assignee: Roussel UclafInventors: Jean Tessier, Jean-Pierre Demoute, Joseph Cadiergue
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Patent number: 4535086Abstract: Heterocyclic compounds of the formula ##STR1## wherein X is --CH.dbd.CH--, --O-- or --S--; R.sup.1 is a group Ar--R.sup.2 or --CH.dbd.CH--C(CH.sub.3).dbd.CH--R.sup.21 ; Ar is phenyl, pyridyl, furyl or thienyl; R.sup.2 is a group --CO.sub.2 R.sup.3, --C(O)R.sup.4, --CH.sub.2 OR.sup.3, lower-alkylsulphonyl or formyl; R.sup.21 is a group--CO.sub.2 R.sup.3, --C(O)R.sup.4, --CH.sub.2 OR.sup.3 or formyl; R.sup.3 is hydrogen or lower-alkyl and R.sup.4 is hydrogen, hydroxy, amino, lower alkylamino, di-(lower alkyl)amino or lower-alkyl; at least one ring of the molecule being heterocyclic, salts thereof, processes for their preparation, rodenticidal compositions containing these compounds as the active ingredient and methods of use of the rodenticidal compositions are disclosed.Type: GrantFiled: June 27, 1983Date of Patent: August 13, 1985Assignee: Hoffmann-La Roche Inc.Inventors: Michael Klaus, Peter Loeliger, Harald Weiser
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Patent number: 4535092Abstract: Acylanilides of the formula ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are substituents defined in claim 1; wherein R.sup.4 is hydrogen or alkyl of up to 4 carbon atoms, or is joined to R.sup.5 as stated below;wherein R.sup.5 is hydrogen, hydroxy, or alkoxy or acyloxy each of up to 15 carbon atoms, or is joined to R.sup.4 to form an oxycarbonyl group such that together with the --N--CO--C-- part of the molecule it forms an oxazolidinedione group;wherein R.sup.6 is alkyl or halogenoalkyl of up to 4 carbon atoms;and wherein R.sup.7 is 5- or 6- membered saturated or unsaturated heterocyclic which contains one, two or three hetero atoms selected from oxygen, nitrogen and sulphur, which heterocyclic may be a single ring or may be fused to a benzo-ring, and which heterocyclic is unsubstituted or bears one or two substituents defined in claim 1;processes for their manufacture and pharmaceutical compositions containing them. The compounds possess antiandrogenic activity.Type: GrantFiled: November 1, 1982Date of Patent: August 13, 1985Assignee: Imperial Chemical Industries PLCInventor: Leslie R. Hughes
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Patent number: 4515803Abstract: Compounds of the formula I ##STR1## in which n denotes 0-3,R.sup.1 and R.sup.1' are the same or different and denote hydrogen, alkyl or alkenyl, phenyl or benzyl, each substituted as desired;R.sup.2 denotes hydrogen, alkyl or alkenyl;R.sup.3 denotes hydrogen, alkyl, hydroxyalkyl, alkoxyalkyl or aminoalkyl, alkanoylaminoalkyl, guanidinoalkyl, imidazolylalkyl, indolylalkyl, mercaptoalkyl or alkylthioalkyl, phenylalkyl, hydroxyphenylalkyl, phenoxyalkyl or phenylthioalkyl, or R.sup.2 and R.sup.3, together with the C and N atoms carrying them, denote a saturated or unsaturated 4- to 8-membered monocyclic or 8- to 10-membered bicyclic isocycle or heterocycle, optionally monosubstituted or disubstituted by hydroxyl, alkoxy having 1 to 3 C atoms or alkyl,R.sup.4 denotes hydrogen, alkyl, alkenyl, alkadienyl, alkinyl, alkeninyl or alkadiinyl, cycloalkyl, phenyl, benzyl, phenethyl or phenylpropyl, each of which can be optionally monosubstituted or disubstituted;R.sup.5 denotes hydrogen or alkyl, hydroxyl or alkoxy andR.Type: GrantFiled: September 1, 1982Date of Patent: May 7, 1985Assignee: Hoechst AktiengesellschafatInventors: Rainer Henning, Hansjorg Urbach, Rolf Geiger, Volker Teetz, Bernward Scholkens
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Patent number: 4508731Abstract: Compounds of the formula ##STR1## in which Ar is 2-alkyl-, -alkoxy- or -halo-methyl-phenyl or .alpha.-naphthyl, each of which is further substituted,R.sub.1 is 2-furyl, 2-tetrahydrofuryl, alkenyl, cyclopropyl, .beta.-alkoxyethyl, hydroxymethyl, triazolylmethyl, imidazolylmethyl, pyrazolylmethyl, alkylsulfinyl, alkylsulfonyl, alkoxy, alkenyloxy, alkynyloxy, alkylthio, alkenylthio, alkynylthio, alkylsulfinyloxy, dialkylaminosulfinyloxy, phosphoric or thiophosphoric esters or amides, or alkylcarbonyloxy, andR.sub.9 is hydrogen or methyl,are microbicidally, in particular fungicidally active. The preferred compounds are those in which Ar is 2-methylphenyl, 2-methoxyphenyl, 2-chlorophenyl or .alpha.-naphthyl, each of which is further substituted by azido, and R.sub.9 is hydrogen.Type: GrantFiled: February 13, 1984Date of Patent: April 2, 1985Assignee: Ciba Geigy CorporationInventors: Peter Riebli, Hanspeter Fischer, Rudolph C. Thummel, Adolf Hubele
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Patent number: 4503051Abstract: 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: June 13, 1983Date of Patent: March 5, 1985Assignee: Bristol-Myers CompanyInventors: Aldo A. Algieri, Ronnie R. Crenshaw