Chalcogen And Acyclic Nitrogen Bonded Directly To The Same Carbon Patents (Class 546/291)
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Patent number: 5180831Abstract: Quaternary pyridinium compounds, their use in inhibiting acetylcholinesterase, their roles in the prophylaxis and treatment of organophosphate poisoning, their roles in anticholinesterase therapy and their roles as agents mimicking or opposing the actions of the natural neurotransmitter acetylcholine.Type: GrantFiled: August 10, 1990Date of Patent: January 19, 1993Assignee: Georgia Tech Research CorporationInventors: James C. Powers, Sheldon W. May, Maria A. Hernandez, Steve Thornton, Jan Glinski
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Patent number: 5177089Abstract: A butenoic or propenoic acid derivative having the following formula in which G is an aryl or a heterocyclic ring, R11 and R12 are hydroben or an alkyl, X is sulfur or oxygen, R2 and R3 are hydrogen, an substituent such as an alkyl and J is pyridyl or phenyl having substituents and a heterocyclic ring may be formed between R2, R3 and J is provided here and is useful in the pharmacological field.Type: GrantFiled: July 25, 1990Date of Patent: January 5, 1993Assignee: Eisai Co., Ltd.Inventors: Norio Minami, Fumihiro Ozaki, Keiji Ishibashi, Yasuhiro Kabasawa, Megumi Ikemori, Toshiaki Ogawa, Takanori Kawamura
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Patent number: 5166162Abstract: The invention concerns a compound of formula (I) ##STR1## in which: R represents cycloalkyl, bicycloalkyl or polycycloalkyl,X represents oxygen or sulfur, andR1 represents alkyl, cycloalkyl, bicycloalkyl, or polycycloalkyl.Medicaments thereof and use of same is useful in treating a circulatory ailment related to arterial hypertension or peripheral or cerebral oedema.Type: GrantFiled: January 24, 1992Date of Patent: November 24, 1992Assignee: Adir et CompagnieInventors: Bernard Masereel, Bernard Pirotte, Marc Schynts, Jacques Delarge
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Patent number: 5157123Abstract: Site-specific heterobifunctional crosslinkers of the formula:X--COCH(NH.sub.2)--Y--Zwhere X is a carbonyl reactive group, Y is a variable length spacer, and Z is a thiol reactive group, are useful for the specific labelling of biomolecules or bioaffecting molecules.Type: GrantFiled: March 13, 1989Date of Patent: October 20, 1992Assignee: Georgetown UniversityInventors: Jane J. Zara, Richard D. Wood, Reinhard Bredehorst, Carl-Wilhelm Vogel
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Patent number: 5153212Abstract: 2-adamantyl-4-isothiazoline-3-one has the formula ##STR1## wherein R.sub.1 and R.sub.2, each independently, represent hydrogen or halogen,or R.sub.1 and R.sub.2, taken together, form a polymethylene chain having 3-4 carbon atoms, optionally substituted by lower alkyl or halogen,or R.sub.1 and R.sub.2, taken together, form a pyridine ring with the double bond of the 4-isothiazoline-3-one ring andAda represents 1'-adamantyl, 2'-adamantyl or 1'-adamantyl methyl, and its mineral or organic acid salt.The compound is useful as an antibacteria, antialgae or antifungus agent in various industrial fields.Type: GrantFiled: June 3, 1991Date of Patent: October 6, 1992Assignee: Centre International de Recherches Dermatoglogiques (C.I.R.D.)Inventors: Braham Shroot, Jean Maignan, Rainer Schmidt
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Patent number: 5151436Abstract: Therapeutically useful thioformamide derivatives of the formula: ##STR1## wherein R represents alkyl, Het represents pyrid-3-yl, isoquinolin-4-yl, tetrahydroquinolin-3-yl, quinolin-3-yl, pyridazin-4-yl, pyrimid-5-yl, thiazol-5-yl, thieno[2,3-b]-pyridin-5-yl, pyrazin-2-yl, indol-3-yl and thieno[3,2-b]-pyridin-6-yl, Y represents ethylene, methylene or a valency bond, and X represents carbonyl, hydroxymethylene, >C.dbd.NOR.sup.1, >C.dbd.NN(R.sup.1).sub.2 or >C.dbd.NN(R.sup.1)CON(R.sup.1).sub.2 in which R.sup.1 represents hydrogen or optionally substituted alkyl, benzyl, phenethyl, 1-naphthylmethyl, 2-naphthylmethyl or pyrid-3-ylmethyl, or two R.sup.1 substituents on the same nitrogen atom may together form an optionally substituted alkylene radical chain and salts thereof, processes for their preparation and compositions containing them are described.Type: GrantFiled: August 23, 1990Date of Patent: September 29, 1992Assignee: Rhone-Poulenc SanteInventors: David C. Cook, Terance W. Hart, Iain M. Mc Lay, Malcolm N. Palfreyman, Brian W. Sharp, Roger J. A. Walsh
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Patent number: 5149359Abstract: The present invention relates to derivatives of 3,4-dehydropiperidin-5-one having herbicidal activity. The derivatives have the formula ##STR1## as defined in the claims. The present invention further relates to a herbicidal composition and a method for controlling weeds which grow among agricultural crops.Type: GrantFiled: February 21, 1990Date of Patent: September 22, 1992Assignee: Agrimont S.p.A.Inventors: Giovanni Camaggi, Giovanni Meazza, Ciro Preziuso
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Patent number: 5132314Abstract: Anthelmintically active compounds of formula I are described ##STR1## in which R.sub.1 is hydrogen, halogen, C.sub.1 -C.sub.2 alkyl, C.sub.1 -C.sub.2 thioalkyl, C.sub.1 -C.sub.2 haloalkyl, nitro, C.sub.1 -C.sub.2 alkoxy, or the group SO.sub.n R in which R is C.sub.1 -C.sub.2 alkyl or phenyl and n is 0, 1 or 2;R.sub.2 is hydrogen, halogen, C.sub.1 -C.sub.2 alkyl, C.sub.1 -C.sub.2 haloalkyl, C.sub.1 -C.sub.2 haloalkoxy or C.sub.1 -C.sub.2 alkoxy;R.sub.3 is hydrogen or C.sub.1 -C.sub.2 alkyl;R.sub.4 is hydrogen or C.sub.1 -C.sub.2 alkyl;R.sub.5 is hydrogen, halogen or C.sub.1 -C.sub.5 alkyl;R.sub.6 is hydrogen, halogen or C.sub.1 -C.sub.5 alkyl;R.sub.7 is hydrogen, halogen, C.sub.1 -C.sub.2 alkyl, nitro, C.sub.1 -C.sub.2 haloalkyl, C.sub.1 -C.sub.2 haloalkoxy or C.sub.1 -C.sub.2 alkoxy;R.sub.8 is hydrogen, halogen, C.sub.1 -C.sub.2 alkyl, C.sub.1 -C.sub.2 haloalkyl, C.sub.1 -C.sub.2 haloalkoxy or C.sub.1 -C.sub.2 alkoxy;R.sub.9 is hydrogen, halogen, C.sub.1 -C.sub.2 alkyl, C.sub.1 -C.sub.2 haloalkyl, C.sub.1 -C.Type: GrantFiled: October 25, 1991Date of Patent: July 21, 1992Assignee: Ciba-Geigy CorporationInventors: Peter Maienfisch, Christof Hildenbrand, Jean-Claude Gehret
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Patent number: 5128474Abstract: An aminocarbonyl-substituted pyridinesulfinic acid intermediate for production of an herbicide having formula (V): ##STR1## wherein R.sub.3 and R.sub.4 are selected from the group consisting of hydrogen and alkyl groups, or a salt thereof. The aminocarbonyl-substituted pyridinesulfinic acid or salt thereof is useful as the precursor of aminosulfonyl-substituted pyridinecarbonic acid amide, which in turn is useful as the starting material for agricultural chemicals, medicine, etc.Type: GrantFiled: July 27, 1990Date of Patent: July 7, 1992Assignee: Ishihara Sangyo Kaisha Ltd.Inventors: Takahiro Haga, Yasuhiro Tsujii, Tatsuo Isogai, Shigeo Murai, Hisayoshi Jonishi, Tokiya Kimura, Hiroshi Sasaki, Takao Awazu, Toshihiro Tanaka
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Patent number: 5125956Abstract: Disclosed herein are herbicidal pyridine compounds substituted at the 2- or 6-position with an OR.sub.2 moiety where R.sub.2 is hydrogen, lower alkyl, halomethyl, lower cyanoalkyl, alkenyl or alkynyl, as well as herbicidal compositions and herbicidal use of these compounds.Type: GrantFiled: February 25, 1991Date of Patent: June 30, 1992Assignee: Monsanto CompanyInventors: Donald E. Korte, Len F. Lee
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Patent number: 5120752Abstract: Certain carbocyclic aryl- and heterocyclic aryl- substituted cyclopropyl N-hydroxyureas, N-hydroxy-carboxamides, and N-acyl-N-hydroxyamines inhibit 5- and/or 12-lipoxygenase and are useful in the treatment of inflammatory disease states.Type: GrantFiled: December 6, 1990Date of Patent: June 9, 1992Assignee: Abbott LaboratoriesInventors: Dee W. Brooks, Karen E. Rodriques, Bruce W. Horrom, Hormoz Mazdiyasni
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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: 5112981Abstract: There are described compounds of the formula ##STR1## where n is 1, 2 or 3;R.sub.1 is hydrogen, formyl, loweralkylcarbonyl, arylloweralkylcarbonyl, loweralkyl, arylloweralkyl, ##STR2## R.sub.5 and R.sub.6 being independently loweralkyl or alternatively the group ##STR3## taken as a whole is ##STR4## R.sub.2 is hydrogen, loweralkyl, loweralkenyl, arylloweralkyl, --CH.sub.2 C.tbd.CH, ##STR5## R.sub.7 and R.sub.8 being independently loweralkyl or alternatively the group ##STR6## taken as a whole is ##STR7## R.sub.3 is hydrogen or loweralkyl; and R.sub.4 is hydrogen or loweralkyl;which compounds are useful as analgesic agents and also for treating various memory dysfunctions.Type: GrantFiled: June 5, 1991Date of Patent: May 12, 1992Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: Richard C. Effland, David M. Fink
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Patent number: 5112386Abstract: Acrylic acid derivatives having the formula (I): ##STR1## and stereoisomers thereof, wherein W is R.sup.1 O.sub.2 C--C.dbd.CH--ZR.sup.2, R.sup.1 and R.sup.2 are alkyl or fluoroalkyl groups, and Z is oxygen or sulphur, A, B, D and E are hydrogen, halogen, hydroxy or optionally substituted alkyl, alkoxy, aralkyl, arylalkoxy, alkenyl, alkynyl, aryl, aryloxy, arylthio, heteroaryloxy, heteroarylthio, acyloxy, amino, arylazo or acylamino, nitro, cyano, --CO.sub.2 R.sup.3, --CONR.sup.3 R.sup.4, --COR.sup.3, --CR.sup.3 .dbd.NR.sup.4, --N.dbd.CR.sup.3 R.sup.4 --S(O).sub.n R.sup.3 groups; any two of the groups, A, B, D and E, when they are in adjacent positions on the ring, optionally join to form a fused ring, n is 0, 1 or 2; and R.sup.3 and R.sup.4 are hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, alkynyl or optionally substituted aryl or aralkyl; and metal complexes thereof. These compounds are useful as fungicides, insecticides, nematicides or plant growth regulators.Type: GrantFiled: December 30, 1988Date of Patent: May 12, 1992Assignee: Imperial Chemical Industries PLCInventors: Anthony Vivienne, John M. Clough, Paul deFraine, Christopher R. A. Godfrey, Patrick J. Crowley, Kenneth Anderton
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Patent number: 5104883Abstract: Thioformamide derivatives of the formula: ##STR1## wherein: R represents alkyl; A represents an optionally substituted phenyl or heteroaromatic group; R.sup.1 represents hydrogen, alkyl, cyano, carboxyl, formyl, carbamoyl, alkoxycarbonyl or a group --(CH.sub.2).sub.n OR.sup.2, --(CH.sup.2).sub.n SR.sup.2, --(CH.sub.2).sub.n N(R.sup.2).sub.2, --CH.dbd.CHR.sup.3, --CH.dbd.NOR.sup.4, --CONHR.sup.5, or --COR.sup.6 ; R.sup.2 represents hydrogen, alkyl, alkanoyl, aryl, aryl (CH.sub.2).sub.n -- or arylCO--, or, when attached to nitrogen, two R.sup.2 groups may together represent alkylene; R.sup.3 represents hydrogen; alkyl, alkanoyl, carboxyl, carbamoyl, cyano, aryl, arylCO--, aryl(CH.sub.2).sub.n --, or aryl (CH.sub.2).sub.n CO--; R.sup.4 represents hydrogen, alkyl, aryl, aryl (CH.sub.2).sub.n -, optionally substituted alkyl, alkenyl, amino or carbamoyl N,N-disubstituted by alkylene; R.sup.5 represents alkyl, aryl, or aryl (CH.sub.2).sub.n -- or an amino acid residue; R.sup.6 represents alkyl, aryl, or aryl (CH.Type: GrantFiled: January 5, 1990Date of Patent: April 14, 1992Assignee: May & Baker LimitedInventors: Malcolm N. Palfreyman, Nigel Vicker, Roger J. A. Walsh
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Patent number: 5100460Abstract: Herbicides of formula: ##STR1## in which: n=0,1, 2f=0,1A is chosen from the groups ##STR2## in which: Ar is chosen from the groups ##STR3## B is chosen from optionally substituted C.sub.1 -C.sub.10 alkyl and C.sub.3 -C.sub.Type: GrantFiled: July 13, 1989Date of Patent: March 31, 1992Assignee: Rhone-Poulenc AgrochimieInventors: Philippe Desbordes, Michel Euvrard
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Patent number: 5089043Abstract: A heterocyclic oxy-phenoxyacetic acid derivative of the formula: ##STR1## , or its salt, which is useful as a herbicide.Type: GrantFiled: November 6, 1990Date of Patent: February 18, 1992Assignee: Shionogi & Co., Ltd.Inventors: Yoshio Hayase, Kohei Matsumoto, Kazuo Kamei, Kinya Ide, Toshio Takahashi
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Patent number: 5079361Abstract: Cross-linking reagents which are highly specific for sulphydryl groups and react with thiols at an excellent rate. The essential feature of the reagents is at least one vinyl group conjugated with an armoatic nitrogen heterocycle. Particular examples include vinyl pyridines, vinyl pyrimidines and vinyl triazines.Type: GrantFiled: September 9, 1988Date of Patent: January 7, 1992Assignee: Celltech LimitedInventors: Rikki P. Alexander, Michael A. W. Eaton, Thomas A. Millican, Richard C. D. Titmas
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Patent number: 5079366Abstract: The invention provides novel amino acids and peptides containing them which comprise a dihydropyridine.revreaction.pyridinium salt-type redox system and which provide site-specific and sustained delivery of pharmacologically active peptides to the brain. These new amino acids contain a redox system appended directly or via an alkylene bridge to the carbon atom adjacent to the carboxyl carbon and may be incorporated into a peptide chain at a variety of positions, including non-terminal positions.Type: GrantFiled: October 4, 1989Date of Patent: January 7, 1992Assignee: University of FloridaInventor: Nicholas S. Bodor
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Patent number: 5077409Abstract: Methods of preparing bis-aryl amide and urea compounds of the general formula: ##STR1## wherein x is a divalent amide or urea substituent and Y is a nitrogen containing heterocycle, which compounds are inhibitors of platelet activating factor.Type: GrantFiled: May 4, 1990Date of Patent: December 31, 1991Assignee: American Cyanamid CompanyInventor: Allan Wissner
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Patent number: 5066657Abstract: A crotonic acid amide derivative represented by formula (I): ##STR1## wherein X.sub.1, X.sub.2, X.sub.3, X.sub.4, and X.sub.5, which may be the same or different, each represents a hydrogen atom, a halogen atom, a substituted or unsubstituted lower alkyl group, a substituted or unsubstituted lower alkyl group, a lower haloalkyl group, a lower haloalkoxy group, a nitro group, a substituted or unsubstituted lower alkanesulfonyl group, a substituted or unsubstituted alkanesulfonyloxy group, a substituted or unsubstituted benzenesulfonyl group, a substituted or unsubstituted benzenesulfonyloxy group, a substituted or unsubstituted phenoxy group, a substituted or unsubstituted benzyloxy group, a dialkylamino group, a mono- or di-lower alkanesulfonylamino group, a substituted or unsubstituted lower alkythio group, a --SO.sub.2 R.sub.1 wherein R.sub.1 represents a lower alkyl group or a lower haloalkyl group, a lower alkoxycarbonyloxy group, a substituted or unsubstituted alkoxycarbonyl group, a --CH.dbd.N--OR.sub.Type: GrantFiled: May 8, 1990Date of Patent: November 19, 1991Assignee: SDS Biotech K.K.Inventors: Shunji Hayashi, Satoshi Yamanaka, Sayoko Kawaguchi, Teruhiko Ishii, Toshiya Kimata, Naoaki Misu
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Patent number: 5055582Abstract: This invention relates to a process for preparing useful thromboxane A.sub.2 inhibiting (.+-.)7-[3.alpha.-[1-[[(phenylamino)thioxomethyl]hydrazono]ethyl]-1.alpha. ,4.alpha.-bicyclo[2.2.1]hept-2.beta.-yl]-heptenoic acids and useful derivatives thereof from (.+-.)octahydro-1.alpha.-methyl-3a.alpha.,7a.alpha.-4.alpha.,7.alpha.-meth ano-2H-inden-2-ones.Type: GrantFiled: December 13, 1988Date of Patent: October 8, 1991Assignee: National Research Development CorporationInventors: Robert B. Garland, Masateru Miyano
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Patent number: 5047410Abstract: New pharmacologically active amidino and guanidino derivatives which are 5-HT.sub.3 receptor antagonists useful as antiemetic, gastric prokinetic and antimigrainic agents of the following general formula (I) ##STR1## , wherein the substituents are defined hereinbelow, which compounds are 5-HT.sub.3 receptor antagonists useful as antiemetic gastric prokinetic and antimigraine agents, inter alia.Type: GrantFiled: July 12, 1989Date of Patent: September 10, 1991Assignee: Istituto de Angeli S.p.A.Inventors: Arturo Donetti, Marco Turconi, Massimo Nicola, Rosamaria Micheletti
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Patent number: 5047417Abstract: A butenoic or propenoic acid derivative having the following formula in which G is an aryl or a heterocyclic ring, R11 and R12 are hydrogen or an alkyl, X is sulfur or oxygen, R2 and R3 are hydrogen, an substituent such as an alkyl and J is pyridyl or phenyl having substituents and a heterocyclic ring may be formed between R2, R3 and J is provided here and is useful in the pharmacological field.Type: GrantFiled: May 19, 1989Date of Patent: September 10, 1991Assignee: Eisai Co. Ltd.Inventors: Norio Minami, Fumihiro Ozaki, Keiji Ishibashi, Yasuhiro Kabasawa, Megumi Ikemori, Toshiaki Ogawa, Takanori Kawamura
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Patent number: 5047535Abstract: The invention relates to novel compounds which are suited for the production of multilayer films which have piezoelectric, and pyroelectric properties, and which provide second harmonic generation. The novel compounds are amphiphilic and it is possible to prepare from same polar single-layer and multi-layer films by depositing them on a substrate. When such substrate is a solid support, polar Z-type Langmuir-Blodgett films are obtained. Upon compression of films of such compounds, at an air/water interface, stable Langmuir monolayers are formed.Type: GrantFiled: August 5, 1987Date of Patent: September 10, 1991Assignee: Yeda Research and Development Company LimitedInventors: Meir Lahav, Leslie Leiserowitz, Jacob Sagiv, Ronit Popovitz-Biro, Karlheinz Hill, Ehud Landau
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Patent number: 5041452Abstract: Novel diamides having a nitrogen-containing heterocyclic moiety such as pyridyl are disclosed that are useful for improving feed utilization efficiency of ruminants and for improving lactation of lactating ruminants.Type: GrantFiled: September 28, 1989Date of Patent: August 20, 1991Assignee: Eastman Kodak CompanyInventor: Alan W. White
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Patent number: 5023334Abstract: This invention concerns a process for killing internal parasites, especially nematodes and cestodes affecting warm blooded animals such as sheep, cattle, swine, goats, dogs, cats, horses and humans as well as poultry by administering an effective amount of a compound of the Formula I: ##STR1## Certain of the compounds of Formula I are novel and in further embodiments of the invention provide novel compounds and compositions for use in the process of the invention. The compounds are readily prepared by conventional chemical reactions. Various pyridinyl acylhydrazones of Formula I demonstrate broad-spectrum anthelmintic activity in sheep upon oral and/or parenteral administration.Type: GrantFiled: September 1, 1989Date of Patent: June 11, 1991Assignee: The Upjohn CompanyInventors: Douglas L. Rector, George A. Conder, Sylvester D. Folz
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Patent number: 5021578Abstract: Compounds of the formula ##STR1## in which R.sup.1 denotes haloalkyl, haloalkenyl or haloalkynyl, (R.sup.2).sub.n denotes H or up to 3 halogens, A denotes N or N.fwdarw.0, R.sup.3 denotes H or alkyl, and Z denotes, inter alia, a carboxyl group or a functional derivative thereof, are valuable herbicides and growth regulators.Type: GrantFiled: February 22, 1989Date of Patent: June 4, 1991Assignee: Hoechst AktiengesellschaftInventors: Volker Koch, Lothar Willms, Andreas Fuss, Klaus Bauer, Hermann Bieringer, Helmut Burstell
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Patent number: 5011932Abstract: This invention concerns a process for killing internal parasites, especially nematodes and cestodes affecting warm blooded animals such as sheep, cattle, swine, goats, dogs, cats, horses and humans as well as poultry by administering an effective amount of a compound of the Formula I: ##STR1## Certain of the compounds of Formula I are novel and in further embodiments of the invention provide novel compounds and compositions for use in the process of the invention. The compounds are readily prepared by conventional chemical reactions. Various pyridinyl acylhydrazones of Formula I demonstrate broad-spectrum anthelmintic activity in sheep upon oral and/or parenteral administration.Type: GrantFiled: October 3, 1986Date of Patent: April 30, 1991Assignee: Upjohn CompanyInventors: Douglas L. Rector, George A. Conder, Sylvester D. Folz
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Patent number: 5008276Abstract: Fungicidal compounds of the formula (I): ##STR1## and stereoisomers thereof, wherein K is oxygen or sulphur; Z is optionally substituted aryl or optionally substituted heteroaryl; X is O, S(O).sub.n, NR.sup.4, CR.sup.1 R.sup.2, CHR.sup.5, CO, CR.sup.1 (OR.sup.2), C.dbd.CR.sup.1 R.sup.2, CHR.sup.1 CHR.sup.2, CR.sup.1 .dbd.CR.sup.2, CHR.sup.1 CR.sup.2 .dbd.CH, C.dbd.C, OCHR.sup.1, CHR.sup.1 O, OCHR.sup.1 O, S(O).sub.n CHR.sup.1, S(O).sub.n CHR.sup.1 O, CHR.sup.1 S(O).sub.n, CHR.sup.1 OSO.sub.2, NR.sup.4 CHR.sup.1, CHR.sup.1 NR.sup.4, CO.sub.2, O.sub.2 C, SO.sub.2 O, OSO.sub.2, CO.CO, COCHR.sup.1, COCHR.sup.1 O, CHR.sup.1 CO, CHOH.CHR.sup.1, CHR.sup.1.CHOH, ##STR2## CONR.sup.4, OCONR.sup.4, NR.sup.4 CO, CSNR.sup.4, OCS.NR.sup.4, SCO.NR.sup.4, NR.sup.4 CO.sub.2, NR.sup.4 CS, NR.sup.4 CSO, NR.sup.4 COS, NR.sup.4 CONR.sup.4, S(O).sub.n NR.sup.4, NR.sup.4 S(O).sub.n, CS.sub.2, S.sub.2 C, CO.S, SCO, N.dbd.N, N.dbd.CR.sup.1, CR.sup.1 .dbd.N, CHR.sup.1 CHR.sup.2 CH(OH), CHR.sup.1 OCO, CHR.sup.1 SCO, CHR.sup.1 NR.sup.Type: GrantFiled: October 17, 1988Date of Patent: April 16, 1991Assignee: Imperial Chemical Industries PLCInventors: John M. Clough, Christopher R. A. Godfrey, Stephen P. Heaney, Kenneth Anderton
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Patent number: 5008391Abstract: A process and intermediates for the enantioselective synthesis of 5,10-dideaza-5,6,7,8-tetrahydrofolic acid are disclosed.Type: GrantFiled: July 7, 1989Date of Patent: April 16, 1991Assignee: Eli Lilly and CompanyInventors: Charles J. Barnett, Thomas M. Wilson
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Patent number: 5006658Abstract: A compound of Formula I or a salt thereof:Ar--Q--(CH.sub.2).sub.m --A--CH.sub.2).sub.n (CE.sup.1 .dbd.CE.sup.2).sub.a CE.sup.3 .dbd.CE.sup.4 CXNR.sup.1 R.sup.2 (1)whereAr is a 6-membered heteroaromatic ring containing, as the heteroatom or heteroatoms, one or two nitrogen atoms and is optionally substituted by one or more of halogen, cyano, C.sub.1-6 -alkyl (optionally substituted by halogen), or C.sub.1-6 -alkoxy (optionally substituted by one or more of halogen or C.sub.1-6 -alkyl), or RS(O).sub.x where x is 0, 1 or 2 and R is C.sub.1-6 -alkyl optionally substituted by one or more halogen atoms,Q is --CH.sub.2 -- or --O--,m and n are each independently 0 to 7,A is --CH.sub.2 -- or --O--,a is 0 or 1,E.sup.1 to E.sup.4 are independently hydrogen, C.sub.1-4 -alkyl or halo-C.sub.1-4 -alkyl or halogen,X is oxygen or sulphur, andR.sup.1 and R.sup.2 are independently hydrogen, C.sub.1-6 -alkyl or C.sub.3-6 -cycloalkyl, either being optionally substituted by one or more of the C.sub.1-6 -alkyl, C.sub.Type: GrantFiled: November 25, 1987Date of Patent: April 9, 1991Assignee: The Wellcome Foundation Ltd.Inventor: Robert J. Blade
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Patent number: 5004743Abstract: Compounds having the formula: ##STR1## are leukotriene antagonists and inhibitors of leukotriene biosynthesis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents.Type: GrantFiled: November 25, 1987Date of Patent: April 2, 1991Assignee: Merck Frosst Canada, Inc.Inventors: Robert N. Young, Robert Zamboni, Jacques Y. Gauthier
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Patent number: 5001137Abstract: A novel pyridine compound of the formula ##STR1## wherein each symbol is as defined in the specification, or a salt thereof which exhibit inhibitory activity or prolylendopeptidase and a pharmaceutical use thereof are disclosed.Type: GrantFiled: September 14, 1989Date of Patent: March 19, 1991Assignee: Yoshitomi Pharmaceutical Industries, Ltd.Inventors: Takanori Oe, Yuji Ono, Kazuyuki Kawasaki, Tohru Nakajima
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Patent number: 4996218Abstract: Compounds of the general formula (I) ##STR1## and physiologically acceptable salts and solvates thereof, which have .beta..sub.2 -adrenoreceptor stimulant activity. They may be used in the treatment of diseases associated with reversible airways obstruction, such as asthma and chronic bronchitis.In preferred embodiments, Q represents a chlorine atom or a trifluoromethyl group, X represents a C.sub.3-4 alkylene chain, Y a C.sub.1-5 alkylene chain, R, R.sup.1 and R.sup.2 are each preferably a hydrogen atom or a methyl group and Het represents a pyrimidinyl pyrazinyl, triazinyl, thiazolyl, quinolinyl, benzimidazolyl, benzothiazolyl, benzoxazolyl or pyridyl group.Type: GrantFiled: August 10, 1988Date of Patent: February 26, 1991Assignee: Glaxo Group LimitedInventor: Lawrence H. C. Lunts
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Patent number: 4987140Abstract: Novel pyridines of the formula ##STR1## wherein R is selected from the group consisting of (a) phenyl optionally substituted with at least one member of the group consisting of hydroxy, alkyl and alkoxy of 1 to 5 carbon atoms, halogen --CF.sub.3 and --NO.sub.2 and (b) a 5 to 6 member heterocyclic optionally substituted with alkyl of 1 to 5 carbon atoms, R.sub.1 and R.sub.2 are individually selected from the group consisting of (a) alkyl of 1 to 5 carbon atoms, (b) 5 to 6 member heterocyclic optionally substituted with alkyl of 1 to 5 carbon atoms and (c) phenyl and naphthyl optionally substituted with at least one member of the group consisting of hydroxy, alkyl and alkoxy of 1 to 5 carbon atoms, halogen, --NO.sub.3 and --CF.sub.3, R.sub.3 is selected from the group consisting of hydrogen, alkyl of 1 to 5 carbon atoms, --(CF.sub.2).sub.n --CF.sub.Type: GrantFiled: November 27, 1989Date of Patent: January 22, 1991Assignee: Roussel UclafInventors: Francois Clemence, Odile Le Martret, Francoise Delevallee
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Patent number: 4978385Abstract: A compound of the formual (I) ##STR1## or 1-oxide or salt thereof, whereinR.sub.1 is a C.sub.1-11 alkyl group, a lower alkenyl group, a phenyl or group which may be substituted, an aralkyl group whose nucleus may be substituted, a haloalkyl or a 5- or 6-membered heterocycle group;R.sub.2, R.sub.3, R.sub.4, R.sub.5 and R.sub.6 are, the same or different, hydrogen atom, a halogen atom, cyano group, nitro group, amino group, a lower alkyl group, a lower haloalkyl group, hydroxy group, a lower alkoxy group, an aryloxy group, carboxy group or a lower alkoxycarbonyl group;R.sub.7 is hydrogen atom, a halogen atom, a lower alkyl group, a phenyl group which may be substituted, an aralkyl group whose nucleus may be substituted, a lower alkenyl group, a lower alkynyl group, a lower alkoxy group or a haloalkyl group;R.sub.8 is a C.sub.Type: GrantFiled: May 26, 1988Date of Patent: December 18, 1990Assignee: Daicel Chemical Industries Ltd.Inventors: Hiroshi Yagihara, Yukihisa Goto, Kazuhisa Masamoto, Yasuo Morishima, Hirokazu Osabe
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Patent number: 4977169Abstract: The invention relates to the use of N-3-(5-trifluoromethylpyridyl-2-oxy)phenyl-N'-benzoylureas of formula I ##STR1## wherein R.sub.1 is hydrogen, C.sub.1 -C.sub.2 alkoxy, C.sub.1 -C.sub.2 alkylthio, C.sub.1 -C.sub.2 alkyl or halogen,R.sub.2, R.sub.3 and R.sub.5 are independently of each other hydrogen or halogen, andR.sub.4 is hydrogen, C.sub.1 -C.sub.2 alkyl or halogen,for controlling helminths, especially nematodes and trematodes, in domestic animals and productive livestock.Type: GrantFiled: May 15, 1989Date of Patent: December 11, 1990Assignee: Ciba-Geigy CorporationInventors: Walter Hausermann, Max Maurer, Thomas Friedel
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Patent number: 4975442Abstract: Novel fungicidal pyridyl cyclopropane carboxamidines having the general structural formula ##STR1## and tautomers thereof whereinR is selected from the group consisting of hydrogen, pyridyl, substituted pyridyl, C.sub.1 -C.sub.3 alkoxy, C.sub.1 -C.sub.6 alkyl, acyl, carbamoyl, sulfonyl and cyano;R.sub.1 is selected from the group consisting of halogen, C.sub.1 -C.sub.3 alkoxy and C.sub.1 -C.sub.3 alkenyloxy;R.sub.2 is selected from the group consisting of hydrogen and C.sub.1 -C.sub.3 alkyl;R.sub.3 is selected from the group consisting of hydrogen, alkyl, aryl or arylalkyl;and fungicidally acceptable organic and inorganic salts thereof.Type: GrantFiled: February 10, 1989Date of Patent: December 4, 1990Assignee: ICI Americas Inc.Inventors: Don R. Baker, Keith H. Brownell
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Patent number: 4968341Abstract: Novel substituted aryloxyureas, processes for their production, and herbicides comprising them as active ingredients are provided.The substituted aryloxyureas exhibit an excellent herbicidal efficacy against weeds when applied, for example, to the weeds in a wide range of period from a preemergence stage to a growth stage.The substituted aryloxyureas of the invention have the excellent advantage of maintaining high safety on crops or crop plants in spite of their herbicidal efficacy.Type: GrantFiled: August 16, 1988Date of Patent: November 6, 1990Assignees: Kumiai Chemical Industry Co., Mitsui Petrochemical Industries, Ltd.Inventors: Isao Hashimoto, Tatsuyodihi Ishida, Kazutaka Tsuru, Yuji Yamada, Takeshige Miyazawa, Yasuo Nakamura, Susumu Katou, Katsuya Takahashi
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Patent number: 4966974Abstract: The invention relates to 2-phenylsulphinyl-nitro-pyridines of the formula ##STR1## in which R.sub.1 denotes hydrogen, alkyl or halogen andR.sub.2, R.sub.3, R.sub.4, R.sub.5 and R.sub.6 independently of one another represent hydrogen, halogen, alkyl, haloalkyl, alkyoxy, haloalkoxy, cyano, nitro, carboxyl, alkoxycarbonyl, carboxamido, N-alkyl- or N,N-dialkylcarboxamido, acyl or primary, secondary or tertiary amino.processes for their preparation, and their use as microbicides for the protection of materials and fungicides in plant protection.Type: GrantFiled: April 3, 1989Date of Patent: October 30, 1990Assignee: Bayer AktiengesellschaftInventors: Alexander Klausener, Wilfried Paulus, Hans-Georg Schmitt, Wilhelm Brandes
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Patent number: 4954628Abstract: The invention relates to a process for preparing sulphonyl-ureas of the general formula (I) ##STR1## wherein Ar.sub.1 represents a phenyl, naphthyl or thienyl group, the derivatives thereof substituted by C.sub.1-4 alkyl, C.sub.1-4 haloalkyl, (halo)alkoxycarbonyl, (halo)alkyloxy, nitro, cyano groups as well as by halogen atoms,Ar.sub.2 represents a phenyl, pyridyl, pirimidinyl or triazinyl group and the derivatives thereof substituted by C.sub.1-4 (halo)alkyl, C.sub.1-4 (halo)alkyloxy, amino, O-acyl, O-arylsulphonyl, O-(substituted carbamoyl) groups as well as by halogen atoms.Type: GrantFiled: March 2, 1989Date of Patent: September 4, 1990Assignees: Nitrokaelepek, Magyar Tudomanyos Akademia Kozponti Kemiai Kutato IntezeteInventors: Gabor Besenyei, Sandor Nemeth, Laszlo Simandi, Maria Belak, Maria Szabo, Jozsef Dukai, Lajos Nagy, Elemer Tomordi, Csaba Soptei, Erzsebet E. Dioszegine
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Patent number: 4946854Abstract: Novel compounds of formula I ##STR1## wherein each of R.sup.1, R.sup.2, R.sup.3, R.sup.7, R.sup.8 and R.sup.9, independently of the others, is H or halogen,R.sup.4 is H, R.sup.10 CO-- or R.sup.11 NHCO-- wherein R.sup.10 is a C.sub.1 -C.sub.4 alkyl group which is unsubstituted or substituted by one to three identical or different substituents selected from the group consisting of halogen, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 - acyloxy and --COOG, wherein G is H, an alkali metal cation or an alkaline earth metal cation, and R.sup.11 is an unsubstituted or halo-substituted C.sub.1 -C.sub.4 alkyl or phenyl group,each of R.sup.5 and R.sup.6, independently of the other, is H, halogen, alkyl or haloalkyl andX is O, S(O)n or NH wherein n is 0, 1 or 2, the preparation of the novel compounds and their use against parasites in and on productive livestock and against insect pests, and novel starting materials and their preparation.Type: GrantFiled: December 5, 1988Date of Patent: August 7, 1990Assignee: Ciba-Geigy CorporationInventors: Peter Maienfisch, Jean-Claude Gehret, Bruno Frei
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Patent number: 4946497Abstract: A compound of the formula (I) ##STR1## or a salt thereof, wherein R is hydrogen atom, or a group of --(CH.sub.2).sub.n --R.sub.1 wherein n is an integer from 1 to 3 and R.sub.1 is hydrogen atom, hydroxy group, a lower alkoxy group, mercapto group, a lower alkylthio group, amino group, a di-lower alkylamino group, a C.sub.3-11 alkyl group, a lower alkenyl group, a lower alkynyl group, a cycloalkyl group, a 5- or 6-membered heterocyclic group, or a phenyl group which may be substituted by one or two substituents of a halogen, a lower alkyl or a lower alkoxy;R.sub.2 and R.sub.7 are the same, a C.sub.1-11 alkyl group, a lower alkenyl group, a lower alkynyl group, a cycloalkyl group, a lower alkoxyalkyl group, an aralkyl group whose nucleus may be substituted by one or two substituents of a halogen, a lower alkyl or a lower alkoxy, or a halalkyl group;R.sub.3, R.sub.4 and R.sub.Type: GrantFiled: November 22, 1988Date of Patent: August 7, 1990Assignee: Daicel Chemical Industries Ltd.Inventors: Yukihisa Goto, Kazuhisa Masamoto, Hiroshi Yagihara, Yasuo Morishima, Hirokazu Osabe
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Patent number: 4943314Abstract: A compound of the formula (I) ##STR1## or a salt thereof, wherein R is hydrogen atom, phenyl group which may be substituted freely or a group of --(CH.sub.2).sub.n --R.sub.1 wherein n is an interger from 1 to 3 and R.sub.1 is hydrogen atom, hydroxy group, lower alkoxy group, mercapto group, lower alkylthio group, amino group, di-lower alkylamino group, C.sub.3-11 alkyl group, lower alkenyl group, lower alkynyl group, cycloalkyl group, 5- or 6-membered heterocyclic group, or phenyl group which may be substituted by one or two substituents of halogen, lower alkyl or lower alkoxy;R.sub.2 and R.sub.7 are different, hydrogen atom, C.sub.1-11 alkyl group, lower alkenyl group, lower alkylyl group, cycloalkyl group, lower alkoxyalkyl group, lower alkylthioalkyl group, phenyl group which may be substituted freely, aralkyl group whose nucleus may be subsituted by one or two substituents of halogen, lower alkyl or lower alkoxy or haloalkyl group or 5- or 6-membered heterocyclic group;R.sub.3, R.sub.4 and R.sub.Type: GrantFiled: March 3, 1989Date of Patent: July 24, 1990Assignee: Daicel Chemical Industries, Ltd.Inventors: Yukihisa Goto, Kazuhisa Masamoto, Hiroshi Yagihara, Yasuo Morishima, Hirokazu Osabe
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Patent number: 4942242Abstract: Thiazolyl phenoxy derivatives are provided as well as pharmaceutical compositions containing such derivatives. The compositions are useful for lowering lipid activity in a subject and accordingly useful for reducing cholesterol and triglycerides.Type: GrantFiled: October 21, 1988Date of Patent: July 17, 1990Inventors: Tadao Kojima, Shunji Kageyama, Minoru Okada, Isao Ohata, Noboru Sato
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Patent number: 4931448Abstract: Insecticidal compounds having the formula ##STR1## in which R is an optionally substituted aryl moiety; R.sub.2 is an optionally substituted alkyl, cycloalkyl or alkenyl moiety, X is sulfur, amino or C.sub.1 -C.sub.4 monoalkylamino; and R.sub.3 is: (a) an optionally substituted 3-phenoxyphenalkyl, 3-phenoxypyridylalkyl or 3-(4-pyridyloxy)phenalkyl moiety; (b) pentafluorobenzyl; or (c) 2-methyl-3-phenylbenzyl.Type: GrantFiled: November 17, 1987Date of Patent: June 5, 1990Assignee: ICI Americas Inc.Inventors: Michael D. Broadhurst, Thomas H. Cromartie
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Patent number: 4931452Abstract: Substituted N-cyanomethyl-2-pyridinones were prepared by the reaction of alkali metal substituted-2-pyridinates with monohaloacetonitriles and found to possess insecticidal properties. The alkali metal substituted-2-pyridinates can be preformed or prepared from the corresponding 2-halopyridines or 2-pyridinols in the reaction medium. N-cyanomethyl-3-fluoro-5-(trifluoromethyl)-2-pyridinone, for example, was prepared from 2,3-difluoro-5-(trifluoromethyl)pyridine and found to control aster leafhoppers both on contact and systemically.Type: GrantFiled: August 24, 1988Date of Patent: June 5, 1990Assignee: The Dow Chemical CompanyInventors: Sudarshan K. Malhotra, James E. Dripps, Gregory A. Bradfisch, Susan Wollowitz, Ingrid L. Knox
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Patent number: 4927838Abstract: The invention relates to compounds of the formula ##STR1## wherein Y and Y' are hydrogen or taken together are O or S, *A is paraphenylene or *----(CH.sub.2).sub.n --(X).sub.s --(CH.sub.2).sub.r ----, X is O, S or --CH.dbd.CH--, n or r, independently, are integers from 0 to 3, m is an integer from 0 to 1, s is an integer from 0 to 1, provided that when s is 1, n+m must be at least 2, t is an integer from 0 to 10, R.sub.1 and R.sub.2, independently, are lower alkyl, lower alkenyl or aryl, or one of R.sub.1 or R.sub.2 is hydrogen and the other is ##STR2## wherein W is ##STR3## --CH.sub.2 --CH.sub.2 --, --CH.sub.2 --, O, S, or ##STR4## and X.sub.1 is lower alkyl, phenyl unsubstituted or mono-, di- or trisubstituted by lower alkoxy, lower alkyl or halogen, and X.sub.2, X.sub.3 and X.sub.4, independently, are hydrogen, lower alkyl, lower alkoxy or halogen, R.sub.3 is hydrogen, lower alkyl or aryl, R.sub.4 is hydrogen, lower alkyl, aryl, aryl-lower alkyl or acyl, R.sub.5 is hydrogen or lower alkyl,R.sub.Type: GrantFiled: July 5, 1988Date of Patent: May 22, 1990Assignee: Hoffman-La Roche Inc.Inventors: Robert W. Guthrie, Richard W. Kierstead, John G. Mullin, Jefferson W. Tilley
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Patent number: RE33478Abstract: Certain novel pyridinyloxyphenoxy alkanoic acids, pyridinylthiophenoxy alkanoic acids, derivatives thereof and related compounds are described. More specifically, these novel compounds bear a fluorine substituent in the 3-position of the pyridinyl group and in the 5-position the substituent is selected from chlorine, CF.sub.3, CF.sub.2 Cl or CF.sub.2 H. These novel compounds exhibit surprising preemergent and postemergent activity in the control of grassy weeds.Type: GrantFiled: October 31, 1988Date of Patent: December 11, 1990Assignee: The Dow Chemical CompanyInventors: Howard Johnston, Lillian H. Troxell