Plural Hetero Rings Patents (Class 549/414)
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Patent number: 5191093Abstract: Processes for the preparation of these salts and their use in human and veterinary medicine and as a growth promoter in animals are described.Type: GrantFiled: March 12, 1990Date of Patent: March 2, 1993Assignee: Beecham Group p.l.c.Inventors: Geoffrey H. Baker, Merle Beal
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Patent number: 5185342Abstract: A fungicidal composition for agricultural use, which comprises a compound of the formula: ##STR1## wherein R.sup.1 and R.sup.2 are each hydrogen, lower alkyl or cyclo(lower)alkyl; R.sup.3 is lower alkyl or cyclo(lower)alkyl; R.sup.4 and R.sup.5 are each hydrogen, lower alkyl, lower alkoxy, halogen-substituted lower alkyl, lower alkyl-substituted silyl, halogen or nitro; A represents an unsaturated hydrocarbon group, a halogen-substituted unsaturated hydrocarbon group, a phenyl group or a heterocyclic group, among which the phenyl group and the heterocyclic group may be optionally substituted with not more than three substituents; and Z is --CH.sub.2 --, --CH(OH)--, --CO--, --O--, --S--, --NR-- (R being hydrogen or lower alkyl), --CH.sub.2 CH.sub.2 --, --CH.dbd.CH--, --CH.sub.2 O--, --CH.sub.2 S--, --CH.sub.2 SO--, --OCH.sub.2 --, --SCH.sub.2 -- or --SOCH.sub.2 --.Type: GrantFiled: May 16, 1990Date of Patent: February 9, 1993Assignee: Shionogi Seiyaku Kabushiki KaishaInventors: Yoshio Hayase, Takahiro Kataoka, Hideyuki Takenaka, Mitsuhiro Ichinari, Michio Masuko, Toshio Takahashi, Norihiko Tanimoto
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Patent number: 5175314Abstract: This invention relates to certain herbicidal oxatricyclic ethers, agriculturally suitable compositions thereof and a method for their use as broad spectrum preemergent or postemergent herbicides.Type: GrantFiled: January 8, 1992Date of Patent: December 29, 1992Assignee: E. I. Du Pont de Nemours and CompanyInventor: Wendy S. Taylor
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Patent number: 5128368Abstract: Combatting fungi and bacteria with aminomethylheterocyclic compounds of the formula ##STR1## in which R.sup.1 represents hydrogen, alkyl, alkenyl, in each case optionally substituted tetrahydronaphthyl, decahydronaphthyl, cycloalkyl or cycloalkenyl, furthermore alkyl which is substituted by cycloalkyl, cycloalkenyl, cycloalkyloxy or cycloalkylthio, where the cyclic radicals may optionally be substituted, furthermore optionally substituted aryl, in addition alkyl which is substituted by aryl, aryloxy, arylthio, arylsulphinyl or arylsulphonyl, or alkenyl which is substituted by aryl, where the aryl radicals may in each case optionally be substituted;R.sup.2 represents hydrogen or methyl,R.sup.Type: GrantFiled: October 10, 1990Date of Patent: July 7, 1992Assignee: Bayer AktiengesellschaftInventors: Wolfgang Kramer, Joachim Weissmuller, Graham Holmwood, Dieter Berg, Stefan Dutzmann, Wilhelm Brandes, Gerd Hanssler, Paul Reinecke
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Patent number: 5126365Abstract: The invention concerns a bicyclic derivative of the formula I, or a pharmaceutically-acceptable salt thereof, ##STR1## wherein Ar.sup.1 is optionally substituted phenyl or naphthyl; R.sup.1 if (1-6C)alkyl, (3-6C)alkenyl, (3-6C)alkynyl, cyano-(1-4C)alkyl or (2-4C)alkanoyl, or optionally substituted benzoyl; andR.sup.2 and R.sup.3 together form a group of the formula --A.sup.1 --X--A.sup.2 ---, wherein each of A.sup.1 and A.sup.2 is (1-4C)alkylene and X is oxy, thio, sulphinyl, sulphonyl or imino.The invention also concerns processes for the manufacture of a bicyclic derivative of the formula I, or a pharmaceutically-acceptable salt thereof, and pharmaceutical compositions containing said bicyclic derivatives. The compounds of the invention are inhibitors of the enzyme 5-lipoxygenase.Type: GrantFiled: July 25, 1990Date of Patent: June 30, 1992Assignees: Imperial Chemical Industries PLC, ICI PharmaInventors: Thomas G. C. Bird, John F. Kingston, David Waterson
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Patent number: 5122361Abstract: Novel CNS dopamine D-2 receptors, such as the compound 5-iodo-7-N-[(1-ethyl-2-pyrrolidinyl)methyl]carboxamide-2,3-dihydrobenzofur an, are disclosed. These compounds are useful as imaging agents for D-2 receptors in the human brain and exhibit good brain retention and in vivo stability.Type: GrantFiled: April 17, 1989Date of Patent: June 16, 1992Assignee: Trustees of the University of PennsylvaniaInventors: Hank F. Kung, Raymond Murphy
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Patent number: 5120746Abstract: This invention relates to amine derivatives and salts thereof. These compounds have an anti-ulcer activity which is effective to human beings and animals. This disclosure relates to such compound, a process for the preparation thereof and an anti-ulcer agent containing the same.Type: GrantFiled: March 30, 1990Date of Patent: June 9, 1992Assignee: Toyama Chemical Co., Ltd.Inventors: Shiro Hirai, Hiroshi Hirano, Hirotoshi Arai, Yasuo Kiba, Hisanari Shibata, Yoshikazu Kusayanag, Minako Yotsuji, Kazuhiko Hashiba, Kikuko Tanada
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Patent number: 5116869Abstract: 2-Substituted-2-cyclopentenones represented by the formula (I): ##STR1## wherein A is a hydroxyl group or ##STR2## and B is a hydrogen atom or A and B are bonded together to form one bonding arm;R.sup.1 represents a substituted or unsubstituted hydrocarbon group having 1 to 10 carbon atoms;R.sup.2 represents a substituted or unsubstituted aliphatic hydrocarbon group having 1 to 10 carbon atoms;R.sup.3 represents a substituted or unsubstituted aliphatic hydrocarbon group having 1 to 10 carbon atoms; wherein,when R.sup.3 is a single bond bonded to the cyclopentene skeleton, X represents a hydrogen atom, a hydroxyl group or a protected hydroxyl group; andwhen R.sup.3 is a double bond bonded to the pentene skeleton, X represents a bonding arm constituting a part of said double bond; andm and n independently represent 0, 1 or 2.Type: GrantFiled: September 3, 1991Date of Patent: May 26, 1992Assignee: Teijin LimitedInventors: Satoshi Sugiura, Atsuo Hazato, Toru Minoshima, Yoshinori Kato, Yasuko Koshihara, Seizi Kurozumi
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Patent number: 5110825Abstract: The compounds of the present invention inhibit HMG-CoA reductase, subsequently suppress the synthesis of cholesterol; and are useful in the treatment of hypercholesterolemia, hyperlipoproteinemia, and atherosclerosis.Type: GrantFiled: December 7, 1990Date of Patent: May 5, 1992Assignee: Shionogi & Co., Ltd.Inventors: Masaru Ogata, Hiroshi Matsumoto, Sumio Shimizu, Shiro Kida
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Patent number: 5091533Abstract: Compounds of the formula: ##STR1## where R.sup.2 contains certain aryls or heteroaryls are effective leukotriene inhibitors.Type: GrantFiled: March 12, 1990Date of Patent: February 25, 1992Assignee: Merck Frosst Canada, Inc.Inventors: Patrice C. Belanger, Claude Dufresne, Brian Fitzsimmons, deceased, Maryann Fitzsimmons, Heir, Yvan Guindon, Cheuk K. Lau, Joshua Rokach, John Schiegetz, Michel Therien, Robert N. Young
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Patent number: 5089640Abstract: Plant growth-regulating and fungicidal compounds of the formula ##STR1## in which Ar represents optionally substituted aryl or optionally substituted heteroaryl,R.sup.1 represents hydrogen, alkyl, alkenyl, alkinyl, trialkylsilyl, optionally substituted phenylalkyl or an acyl radical,R.sup.2 represents halogen, cyano, thiocyano, alkylcarbonyloxy, alkylcarbonylthio or the groupings --X--R.sup.3 and --NR.sup.4 R.sup.5,R.sup.3 represents alkyl, cycloalkyl, alkenyl, alkinyl, hydroxyalkyl, alkylthioalkyl, carboxyalkyl, alkoxycarbonylalkyl, optionally substituted aryl, optionally substituted aralkyl or the radical of the formula ##STR2## R.sup.4 and R.sup.3 independently of one another represent hydrogen or alkyl, orR.sup.4 and R.sup.5, together with the nitrogen atom to which they are bonded, represent an optionally substituted cycloaliphatic ring which can contain further heteroatoms,X represents oxygen, sulphur, an SO group or an SO.sub.2 group, orR.sup.Type: GrantFiled: September 28, 1988Date of Patent: February 18, 1992Assignee: Bayer AktiengesellschaftInventors: Klaus Bockmann, Erik Regel, Karl H. Buchel, Klaus Lurssen, Jorg Konze, Wilhelm Brandes
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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: 5049495Abstract: High titers of polyether antibiotics are obtained in a fermentation broth by inoculating a nutrient fermentation broth with a microorganism capable of producing a polyether antibiotic. Growth of the microorganism is established in the broth by incubating the inoculated broth at a physiologically acceptable temperature until pH of the broth begins to rise upon establishment of growth of the microorganism. A free fatty acid then is fed into the broth to achieve and maintain a free fatty acid concentration in the broth of about 0.1% by weight or greater but less than a level at which the free fatty acid is toxic to the microorganism. The free fatty acid is fed into the broth during the remainder of fermentation at about a rate at which the free fatty acid is consumed by the microorganism, to product high titers of the polyether antibiotic.Type: GrantFiled: May 29, 1986Date of Patent: September 17, 1991Assignee: International Minerals & Chemical Corp.Inventor: Guido M. Miescher
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Patent number: 5047339Abstract: An aqueous medium having dispersed therein hydrophobic, polyether antibiotic-containing droplets, is mixed to cause the droplets to collide with each other and coalesce to form agglomerates which are separable from the medium.Type: GrantFiled: April 21, 1986Date of Patent: September 10, 1991Assignee: International Minerals & Chemical CorpInventor: Vikram P. Mehrotra
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Patent number: 5047338Abstract: A polyether and antibiotic material is prepared by forming discrete polyether antibiotic-containing agglomerates which are separable from an aqueous medium, by producing a polyether antibiotic through cultivation of a polyether antibiotic-producing microorganism in a generally aqueous nutrient-containing fermentation broth under conditions wherein at the end of fermentation, a lipid is present in the broth in a sufficient amount to form discrete agglomerates with polyether and antibiotic in the fermentation broth, whereupon the applomerates are separated from the broth.Type: GrantFiled: May 29, 1986Date of Patent: September 10, 1991Assignee: International Minerals & Chemical Corp.Inventor: Guido M. Miescher
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Patent number: 5041567Type: GrantFiled: November 28, 1988Date of Patent: August 20, 1991Assignee: Beecham Group plcInventors: Norman H. Rogers, Peter J. O'Hanlon, Graham Walker, Michael J. Crimmin
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Patent number: 5041374Abstract: Polyether antibiotic material is liberated from agglomerates containing a lipid material and the polyether antibiotic material by separating the polyether antibiotic from the lipid through formation of an acid salt of the lipid and a desired acid salt of the polyether antibiotic. The agglomerates can be formed during fermentation or produced by adding lipids afterwards.Type: GrantFiled: May 29, 1986Date of Patent: August 20, 1991Assignee: International Minerals & Chemical Corp.Inventors: Alexander H. T. Chu, Robert J. Urban
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Patent number: 4990647Abstract: Unsymmetric biaryl compounds are prepared by coupling two different halogenoaromatics by reaction with a metal and carrying out the reaction in the presence of catalytic amounts of a nickel compound, a promoter and a phosphorus-containing ligand.Type: GrantFiled: April 24, 1989Date of Patent: February 5, 1991Assignee: Bayer AktiengesellschaftInventors: Thomas Himmler, Rudolf Braden
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Patent number: 4988828Abstract: A phenoxypropyl derivative represented by the following formula ##STR1## wherein A represents a formyl group, a protected formyl group, a hydroxymethyl group, a protected hydroxymethyl group, or a halomethyl group, and Z represents a halogen atom, an amino group, a phthalimide group or a group of the formula ##STR2## in which n is 0, 1 or 2.Type: GrantFiled: November 23, 1988Date of Patent: January 29, 1991Assignee: Fujirebio Kabushiki KaishaInventors: Noriaki Kashiwaba, Hajime Matsumoto, Akihiko Hosoda, Yasuo Sekine
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Patent number: 4988729Abstract: Combattting fungi and bacteria with aminomethylheterocyclic compounds of the formula ##STR1## in which R.sup.1 represents hydrogen, alkyl, alkenyl, in each case optionally substituted tetrahydronaphthyl, decahydronaphthyl, cycloalkyl or cycloalkenyl, furthermore alkyl which is substituted by cycloalkyl, cycloalkenyl, cycloalkyloxy or cycloalkylthio, where the cyclic radicals may optionally be substituted, furthermore optionally substituted aryl, in addition alkyl which is substituted by aryl, aryloxy, arylthio, arylsulphinyl or arylsulphonyl, or alkenyl which is substituted by aryl, where the aryl radicals may in each case optionally be substituted;R.sup.2 represents hydrogen or methyl,R.sup.Type: GrantFiled: October 17, 1989Date of Patent: January 29, 1991Assignee: Bayer AktiengesellschaftInventors: Wolfgang Kramer, Joachim Weissmuller, Graham Holmwood, Dieter Berg, Stefan Dutzmann, Wilhelm Brandes, Gerd Hanssler, Paul Reinecke
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Patent number: 4987132Abstract: A saturated heterocyclic carboxamide derivative of the following general formula (I) and salts thereof which have platelet activating factor (PAF) antagonizing activity.Type: GrantFiled: August 16, 1988Date of Patent: January 22, 1991Assignee: Yamanouchi Pharmaceutical Co., Ltd.Inventors: Toshiyasu Mase, Hiromu Hara, Hitoshi Nagaoka, Takumi Takahashi, Takeshi Suzuki, Kenichi Tomioka, Toshimitsu Yamada
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Patent number: 4983779Abstract: An improved process for the preparation of vinyl ethers by the coupling reaction of an ester of the formula ##STR1## with a carbonyl containing compound of the formula ##STR2## wherein A and R are passive organic groups and OY is a hydroxyl group or OP where P is a protecting group is described. The ester and the carbonyl containing compound are reacted in an organic solvent with a titanium salt, a metallic reducing agent and an amine base to provide the vinyl ether. The reaction is safe and produces high yields. The vinyl ethers are useful for producing dioxetanes which produce light upon triggering.Type: GrantFiled: December 14, 1989Date of Patent: January 8, 1991Assignee: The Board of Governors of Wayne State UniversityInventor: Arthur P. Schaap
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Patent number: 4952710Abstract: This invention relates to a novel cyclopenteneheptenoic acid derivative having the following formula ##STR1## wherein R.sub.1 is hydrogen, --COCH.sub.3, --COCF.sub.3, --CO--phenyl, or a hydroxyl protecting group such as tetrahydropyranyl, tetrahydrofuranyl, or tri-lower alkylsilyl;wherein R.sub.2 is --CH.sub.2 OR.sub.1, --COOH, --COOR, --CHO, --CH.sub.2 --OSi(R.sub.12).sub.3, ##STR2## wherein R is lower alkyl and each R.sub.12 is independently lower alkyl or aryl; andwherein Y is ethylene, cis-vinylene, trans-vinylene, or acetylene.Also disclosed is a novel process for preparation of the above-defined cyclopenteneheptenoic acid derivative. This process involves coupling of a higher order cuprate complex with a chiral cyclopentene compound. The resultant product is particularly useful as a starting compound for high yield synthesis of optically active prostaglandins.Type: GrantFiled: October 7, 1988Date of Patent: August 28, 1990Assignee: G. D. Searle & Co.Inventors: Kevin A. Babiak, Arthur L. Campbell
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Patent number: 4948895Abstract: A 6-tertiary amino-2-(Z.dbd.CH--)benzofuran dye is disclosed, where Z represents the atoms providing an electron withdrawing group and a conjugated methine linkage completing a resonant dye chromophore including the 6-tertiary amino group as an electron donor and the electron withdrawing group as an electron acceptor. The dyes are formed by condensing a 6-tertiary amino-2-formylbenzofuran with an electron withdrawing dye nucleus precursor containing an active methyl or methylene site. The dyes exhibit bathochromically shifted absorption peaks.Type: GrantFiled: October 13, 1989Date of Patent: August 14, 1990Assignee: Eastman Kodak CompanyInventors: Chin H. Chen, John L. Fox
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Patent number: 4916155Abstract: Crystalline calcium pseudomonate or a hydrate thereof, in particular the dihydrate.Processes for the preparation of these salts and their use in human and veterinary medicine and as a growth promoter in animals are described.Type: GrantFiled: April 13, 1989Date of Patent: April 10, 1990Assignee: Beecham Group p.l.c.Inventors: Geoffrey H. Baker, Merle Beal
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Patent number: 4894391Abstract: 5-Cyanoprostacyclins of Formula I ##STR1## wherein A is a --CH.sub.2 --CH.sub.2 --, trans--CH.dbd.CH--, or --C.tbd.C-group,W is a free or functionally modified hydroxymethylene group or a free or functionally modified ##STR2## wherein the OH-group can be in the .alpha.- or .beta.-position, D and E together form a direct bond orD is the group ##STR3## a straight-chain, saturated alkylene group of 1-5 carbon atoms, a branched, saturated or a straight-chain, unsaturated alkylene group of 2-5 carbon atoms, any of which can optionally be substituted by fluorine atoms,n is the number 1, 2, or 3,E is oxygen, sulfur, a --C.tbd.C-bond, a direct bond, or a --CR.sub.4 .dbd.CR.sub.5 -group wherein R.sub.4 and R.sub.5 are different and can be a hydrogen atom or an alkyl group of 1-3 carbon atoms,R.sub.2 is an alkyl, cycloalkyl, optionally substituted aryl, or heterocyclic group,R.sub.1 is a free or functionally modified hydroxy group, andR.sub.3 is an acetal residue ##STR4## wherein R.sub.6, R.sub.7, R.sub.8, R.sub.9, R.Type: GrantFiled: June 25, 1984Date of Patent: January 16, 1990Assignee: Schering AktiengesellschaftInventors: Werner Skuballa, Helmut Dahl, Bernd Raduchel, Helmut Vorbruggen, Olaf Loge
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Patent number: 4892960Abstract: Crystalline lysocellin compositions, and method of making them. These compounds are useful for promoting growth and feed efficiency in food producing mammals by administering growth promoting amounts of the compounds to such mammals. In particular, the crystalline free acid and the crystalline zinc, copper and manganese of lysocellin can be made according to the disclosed methods.Type: GrantFiled: December 20, 1985Date of Patent: January 9, 1990Assignee: International Minerals & Chemical Corp.Inventor: Vernon V. Young
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Patent number: 4876273Abstract: New polyether antibiotic A80577, its acyl ester and alkyl ether derivatives, and salts thereof, are useful antibacterial agents and increase feed-utilization efficiency in animals. Methods of making A80577 by culture of Actinomadura verrucosospora, NRRL 18236, and compositions containing an A80577 compound also are provided.Type: GrantFiled: July 18, 1988Date of Patent: October 24, 1989Assignee: Eli Lilly and CompanyInventors: Robert L. Hamill, Raymond C. Yao
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Patent number: 4876275Abstract: 3,4-dihydro-2H-pyrans of the formula I ##STR1## where R.sup.1 is C.sub.4 -C.sub.20 -alkyl, C.sub.4 -C.sub.20 -alkoxyalkyl, aryl or C.sub.7 -C.sub.20 -arylalkyl, or is aryl or C.sub.7 -C.sub.20 -arylalkyl which bears from one to three substituents selected from the group consisting of halogen, C.sub.1 -C.sub.8 -alkyl, C.sub.1 -C.sub.8 -haloalkyl, C.sub.1 -C.sub.8 -alkoxy or C.sub.1 -C.sub.8 -haloalkoxy, R.sup.2 is hydrogen or C.sub.1 -C.sub.4 -alkyl, R.sup.3 is aryl, or aryl bearing from one to three substituents selected from the group consisting of halogen, C.sub.1 -C.sub.8 -alkyl, C.sub.1 -C.sub.8 -haloalkyl, C.sub.1 -C.sub.8 -alkoxy or C.sub.1 -C.sub.8 -haloalkoxy, or the radical ##STR2## where R.sup.4, R.sup.5 and R.sup.6 are hydrogen or C.sub.1 -C.sub.4 -alkyl, R.sup.7 is phenyl or benzoyl, or phenyl or benzoyl bearing from one to three substituents selected from the group consisting of halogen, C.sub.1 -C.sub.8 -alkyl, C.sub.1 -C.sub.8 -haloalkyl, C.sub.1 -C.sub.8 -alkoxy and C.sub.1 -C.sub.Type: GrantFiled: April 1, 1988Date of Patent: October 24, 1989Assignee: BASF AktiengesellschaftInventors: Walter Himmele, Hans Theobald, Franz Merger, Ernst Hofmann, Christoph Kuenast, Peter Hofmeister
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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: 4871866Abstract: A process for purifying lysocellin which comprises mixing lysocellin solids with sufficient halogen acid to convert fatty acid ester salt impurities into water-soluble metal halogen salts and water-insoluble free fatty acids and to convert lysocellin salts into water-soluble metal halogen salts and water-insoluble lysocellin acid, separating the halogen salts from the lysocellin acid and fatty acid solids, mixing the lysocellin acid and fatty acid solids with sufficient caustic reagent to convert free fatty acids into water-soluble alkali metal salts and to convert lysocellin acid into a water-insoluble alkali metal lysocellin salts, and separating the water-soluble fatty acid alkali metal salts from the alkali metal lysocellin solids.Type: GrantFiled: August 24, 1987Date of Patent: October 3, 1989Assignee: Pitman-Moore, Inc.Inventors: Alexander H. T. Chu, M. James Levi
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Patent number: 4857652Abstract: Novel light producing 1,2-dioxetanes are described of the formula ##STR1## wherein ArOX is an aryl ring substituted with an X oxy group and A are passive organic groups which allow the 1,2-dioxetane to produce light when triggered by removing X. X is a chemically labile group which is removed by an activating agent. The 1,2-dioxetane compounds can be triggered to produce light at room temperatures.Type: GrantFiled: August 23, 1988Date of Patent: August 15, 1989Assignee: Board of Governors of Wayne State UniversityInventor: Arthur P. Schaap
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Patent number: 4842638Abstract: Tetrahydro(thio)pyran-2,4-dione derivatives of the formula ##STR1## where R.sup.1 is hydrogen, a cation, alkylcarbonyl, C.sub.2 -C.sub.10 -alkenylcarbonyl, or benzoyl which is unsubstituted or substituted by alkyl, R.sup.2 is alkyl, R.sup.3 is a non-aromatic, unsubstituted or alkyl-substituted heterocyclic compound of 5 to 7 ring members and having at most one double bond in the heterocyclic ring, X is oxygen or sulfur, and Z is oxygen or the radical NO--R.sup.4, R.sup.4 denoting alkyl, alkenyl, alkynyl, haloalkyl, hal oalkenyl, alkoxyalkyl or the radical CH.sub.2 --R.sup.5, where R.sup.5 is a he terocyclic compound of 5 ring members and containing from 1 to 3 hetero-atoms and from 0 to 2 double bonds and bearing either no substituents or one or two substituents selected from the group consisting of alkyl, alkoxy, halogen, trifluoromethyl, alkoxymethyl, alkylthiomethyl and vinyl, or R.sup.Type: GrantFiled: January 12, 1988Date of Patent: June 27, 1989Assignee: BASF AktiengesellschaftInventors: Juergen Kast, Michael Keil, Dieter Kolassa, Ulrich Schirmer, Bruno Wuerzer, Norbert Meyer, Wilhelm Rademacher, Johann Jung
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Patent number: 4822804Abstract: Pharmaceutically useful compounds are 5,6,7-trinor-4,8-inter-m-phenylene PGI.sub.2 derivatives such as5,6,7-trinor-4,8-inter-m-phenylene-2-nor-16,16-dimethyl PGI.sub.2,5,6,7-trinor-4,8-inter-m-phenylene-2-nor-17(S)-methyl PGI.sub.2,5,6,7-trinor-4,8-inter-m-phenylene-2-nor-17(R)-methyl PGI.sub.2,5,6,7-trinor-4,8-inter-m-phenylene-2-nor-16,16-dimethyl-.omega.-homo PGI.sub.2,5,6,7-trinor-4,8-inter-m-phenylene-2-nor-17(S)-methyl-.omega.-homo PGI.sub.2,5,6,7-trinor-4,8-inter-m-phenylene-2-nor-17(R)-methyl-.omega.-homo PGI.sub.2,5,6, 7-trinor-4,8-inter-m-phenylene-2,17,18,19,20-pentanor-16,16-dimethyl-16-p ropoxy PGI.sub.2,5,6,7-trinor-4,8-inter-m-phenylene-2,18,19,20-tetranor-16,16-dimethyl-17-et ho xy PGI.sub.2,5,6,7-trinor-4,8-inter-m-phenylene-2,18,19,20-tetranor-16,16-dimethyl-17-pr op oxy PGI.sub.2,5,6,7-trinor-4,8-inter-m-phenylene-2,17,18,19,20-pentanor-16-phenoxy PGI.sub.2 and methyl esters thereof.5,6,7-trinor-4,8-inter-m-phenylene-2,17,18,19,20-pentanor-16,16-dimethyl-16 -phenoxy PGI.sub.Type: GrantFiled: September 29, 1987Date of Patent: April 18, 1989Assignee: Toray Industries, Inc.Inventors: Kiyotaka Ohno, Hiroshi Nagase, Mamoru Ishikawa, Kazuhisa Matsumoto, Shintaro Nishio
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Patent number: 4818431Abstract: New tetrahydropyran derivatives of the formula I ##STR1## in which G is H.sub.2 or .dbd.O, R.sup.1 and R.sup.2 are each an alkyl group having 1-10 C atoms, it also being possible for one or two CH.sub.2 groups to be replaced by O atoms, or are F, Cl, Br or CN, R.sup.2 is also H, A.sup.1 and A.sup.2 are each 1,4-phenylene, 1,4-cyclohexylene, 1,3-dioxane-2,5-diyl, piperidine-1,4-diyl, 1,4-bicyclo[2.2.2]octylene or pyrimidine-2,5-diyl groups which are unsubstituted or substituted by 1-4 F atoms, Z.sup.1 and Z.sup.2 are each --CO--O--, --O--CO--, --CH.sub.2 CH.sub.2 --, --OCH.sub.2 --, --CH.sub.2 O--, or a single bond, m and n are each 0, 1, 2 or 3, but (m+n) is at least 1 and at most 3, it being possible, when m is 2 or 3, for the group A.sup.1 and, when n is 2 or 3, for the groups A.sup.2 each to be identical or different from one another, and the acid addition salts of those among these compounds which are basic, are suitable for use as components in liquid-crystal dielectrics.Type: GrantFiled: November 24, 1986Date of Patent: April 4, 1989Assignee: Merck Patent Gesellschaft mit beschrankter HaftungInventors: Rudolf Eidenschink, Joachim Krause, Peter Fuss
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Patent number: 4816062Abstract: The disclosure herein pertains to herbicidal methods and compositions containing 3,5-dicarboxylic acid esters of 2,6-bis-(fluoroalkyl) tetrahydropyrans and piperidines which may be substituted in the 4-position by certain alkyl, phenyalkyl, phenyl, alkoxyalkyl, alkylthioalkyl, cycloalkyl, and heterocyclic radicals wherein the hetero atom is oxygen and sulfur and to a process for the preparation thereof. These compounds are useful as pre-emergent herbicides.Type: GrantFiled: June 2, 1986Date of Patent: March 28, 1989Assignee: Monsanto CompanyInventor: Len F. Lee
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Patent number: 4812582Abstract: This invention pertains to a new method for killing and controlling worms (Helminths), new formulations for killing and controlling worms in animals, new chemical compounds, and a new synthesis of northern hemisphere intermediates for the synthesis of milbemycin and avermectin macrolides.Type: GrantFiled: May 6, 1987Date of Patent: March 14, 1989Assignee: The Upjohn CompanyInventor: Stephen J. Nelson
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Patent number: 4798842Abstract: Novel compounds and compositions which inhibit SRS--A in mammals are disclosed. Methods for preparing said compounds and compositions and methods for their use for treating allergic reactions, inflammation and for reducing the severity of myocardial infarction resulting from heart attack are disclosed.Useful intermediates for preparing said compounds are also disclosed.Type: GrantFiled: November 17, 1987Date of Patent: January 17, 1989Assignee: Schering CorporationInventors: Anil K. Saksena, Jesse K. Wong, Pietro Mangiaracina
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Patent number: 4786742Abstract: This invention relates to a novel salt of an antibacterial compound and to a process for its preparation.Type: GrantFiled: August 8, 1986Date of Patent: November 22, 1988Assignee: Beecham Group p.l.c.Inventor: Alan D. Curzons
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Patent number: 4783483Abstract: Alkenes of the formula (I) and epoxides (II) used to make them are useful as anti-inflammatory and antiallergic pharmaceuticals: ##STR1## wherein R.sup.1 =H or CH.sub.3 ; R.sup.2 =phenyl, substituted phenyl, benzyl or a cysteinyl moiety; R.sup.4 and R.sup.5 =alkyl; n=O or 1; and R.sup.3 is as described.Type: GrantFiled: December 29, 1986Date of Patent: November 8, 1988Assignee: Ortho Pharmaceutical CorporationInventors: Michael P. Ferro, Michael P. Wachter
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Patent number: 4782169Abstract: Compounds of the Formula I, II, III, VI and VII ##STR1## wherein the symbols have defined meanings are herbicides, plant growth regulators or intermediates thereof.Type: GrantFiled: October 6, 1986Date of Patent: November 1, 1988Assignee: E. I. Du Pont de Nemours and CompanyInventors: Samuel B. Soloway, Pierre Vogel, Claude H. Aubin Le Drian, James E. Powell
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Patent number: 4739083Abstract: A new process for preparing a pyrone-3-carboxamide compound of the formula (IV): ##STR1## wherein R.sub.1 is aryl or heterocyclic group optionally substituted, R.sub.2 is alkyl, aralkyl or like group, comprising reacting a compound of the formula (I) or (I'): ##STR2## wherein R.sub.3 is dialkylamino group and n is 0 to 6, and R.sub.1 and R.sub.2 are as above,with a compound of the formula (II): ##STR3## wherein R.sub.4 and R.sub.5 are hydrogen atom, alkyl or like group, or reacting a compound of the formula (III): ##STR4## wherein R.sub.6 is alkyl, aryl or like group, and R.sub.1 and R.sub.2 are as above,with a compound of the formula (II) or diketene in the presence of a tertiary organic base.Type: GrantFiled: January 2, 1986Date of Patent: April 19, 1988Assignee: Daicel Chemical Industries Ltd.Inventors: Yoichiro Ueda, Yukihisa Goto, Kazuhisa Masamoto
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Patent number: 4719287Abstract: The extraction of water soluble antibiotics containing a phenolic or carboxylic group from an aqueous solution or fermentation broth using a N--C.sub.8 --C.sub.14 alkyl pyrrolidone extractant and the process involving the extraction of said antibiotic.Type: GrantFiled: February 12, 1987Date of Patent: January 12, 1988Assignee: GAF CorporationInventors: Robert B. Login, Ratan K. Chaudhuri
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Patent number: 4707554Abstract: A new method has been disclosed for obtaining derivatives of 4.beta.-/1'-alken-1'-yl/-2.xi.,5.dbd.-dihydroxy-3,3a.beta.,4,5,6,6a.beta.- hexahydro-2H-cyclopenta [b] furane useful in the synthesis of prostaglandins or their analogs, and a method for obtaining new sulphonyl initial compounds of the general formula 4, in which Z denotes a hydrogen atom or a protective group, Y denotes a group of the formula .dbd.CHOZ.sup.1, in which Z.sup.1 has the meaning stated for Z, whereby protective groups Z and Z.sup.1 may be the same or different, and Ar denotes optionally a substituted aryl group.In the method according to the invention the new sulphonyl derivative of the general formula 4 is alkylated with an electrophilic agent comprising: carbonyl derivatives, oxiranes and halohydrins or their derivatives; the alkylation product is transformed into derivatives of 4.beta.-/1'-alken-1'-yl/-2.xi.,5.alpha.-dihydroxy-3,3a.beta.,4,5,6,6a.beta .Type: GrantFiled: November 27, 1985Date of Patent: November 17, 1987Assignee: Polska Akademia Nauk-Instytut Chemii OrganicznejInventors: Barbara Achmatowicz, Andrzej R. Daniewski, Stanislaw Marczak, Jacek Pankowski, Jerzy Wicha
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Patent number: 4704462Abstract: Substituted 2,3,3a,6-tetrahydro-6-oxobenzofuran derivatives have been prepared. These neolignans are found to have potent and specific PAF (Platelet-Activating-Factor) antagonistic activities and thereby useful in the treatment of various diseases or disorders mediated by PAF, for example, pain, fever, inflammation, cardiovascular disorder, asthma, lung edema, allergic disorders, skin diseases, psoriasis, toxic shock syndrome and adult respiratory distress syndrome.Type: GrantFiled: August 22, 1985Date of Patent: November 3, 1987Assignee: Merck & Co., Inc.Inventors: Michael N. Chang, San-Bao Hwang, Mitree M. Ponpipom, Robert L. Bugianesi
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Patent number: 4703127Abstract: Compounds of the general formula I are disclosed as useful intermediates in the preparation of prostanoids: ##STR1## wherein A represents O or H, OR.sup.z ;R.sup.z represents hydrogen or a protecting group;R.sup.x represents hydrogen or a protecting group; andR.sup.y represents halogen, a substituted thio group, di-substituted amino group, or a group of the formula R.sup.2, and R.sup.2 represents a straight- or branched-chain alkyl alkenyl or alkynyl group which may optionally be substituted by one or more carboxyl, carboxylic acid ester, or free or protected hydroxyl, thiol, aldehyde or keto groups;with the provisos that R.sup.x is not hydrogen when A is O and R.sup.y is R.sup.2 ; and that when A is H, OR.sup.z R.sup.y and R.sup.2 and R.sup.x and R.sup.z are not both hydrogen.Processes for the preparation of these compounds and of 2-substituted 4-hydroxy-cyclopent-2-en-1-one derivatives are also disclosed.Type: GrantFiled: September 2, 1983Date of Patent: October 27, 1987Assignee: The Australian National UniversityInventors: Rodney W. Rickards, Melvyn Gill, Robert M. Christie
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Patent number: 4701535Abstract: This invention relates to ureas and isoureas which are useful as herbicides and plant growth regulants. In particular, compounds of the instant invention have demonstrated great selectivity.Type: GrantFiled: April 7, 1986Date of Patent: October 20, 1987Assignee: E. I. Du Pont de Nemours and CompanyInventor: George Levitt
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Patent number: 4701536Abstract: Disclosed are a compound of Formula I: ##STR1## wherein R.sub.1 represents a hydrogen atom or a protective group for a hydroxyl group; and Z represents a direct bond (2,3-cis-5R*, 8S*) or an oxygen atom which forms an oxirane ring having a configuration of (2R*, 3R*, 5R*, 8S*),and a process for preparing the same.By use of the above compound as an intermediate, there can be synthesized periplanone-B which is a sex pheromone of periplaneta.Type: GrantFiled: July 7, 1986Date of Patent: October 20, 1987Assignee: UBE Industries, Ltd.Inventors: Jiro Tsuji, Takashi Takahashi
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Patent number: 4687864Abstract: The present invention describes 5-fluoro-3-oxaprostacyclin (PGI.sub.2) derivatives of Formula I. These compounds are useful for the treatment of platelet dysfunction, atherosclerosis, hypertension and tumor cell metastasis. Also disclosed is the process for preparing them and the appropriate intermediates. ##STR1## wherein R.sup.1 is: (a) Na, K, or 1/2 Ca, or other pharmaceutically acceptable cation(b) NR.sup.3 .sub.2 with the adjacent connecting oxygen omitted, where R.sup.3 =H, methyl, ethyl, isopropyl or a combination of these groups;(c) Alkyl of 1 to 6 carbon atoms, either branched or straight chain(d) Hydrogenwherein OH on carbon 15 is optionally on carbon 16;wherein X=OCH.sub.3 or OC.sub.2 H.sub.5 when neither C.sub.5 -C.sub.6 or C.sub.6 -C.sub.7 is a double bond and nothing if C.sub.5 -C.sub.6 or C.sub.6 -C.sub.7 is a double bond;wherein R.sup.Type: GrantFiled: September 18, 1985Date of Patent: August 18, 1987Assignee: G. D. Searle & Co.Inventors: Stevan W. Djuric, Leland J. Chinn, Kurt J. Rorig
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Patent number: 4668803Abstract: Novel organic compound of the basic formula ##STR1## which have substantial luminescent emission characteristics and advantages.Type: GrantFiled: July 1, 1985Date of Patent: May 26, 1987Assignee: Atlantic Richfield CompanyInventors: Elliot Berman, Brian A. Zentner