Nitrogen Double Bonded Directly At 2-position Of The Diazole Ring, Or Tautomeric Equivalent Patents (Class 514/388)
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Patent number: 5763469Abstract: The present invention relates to substituted cyclic ureas and analogs thereof of formula (I): ##STR1## wherein, T is selected from: --N(R.sup.22)C(.dbd.Z)N(R.sup.23)--; --N(R.sup.22)C(.dbd.Z)C(.dbd.Z)N(R.sup.23)--; --N(R.sup.22)S(.dbd.Z')N(R.sup.23)--; --N(R.sup.22)S(.dbd.Z').sub.2 N(R.sup.23)--; or --N(R.sup.22)P(.dbd.O)(R.sup.24a)N(R.sup.23)--;Z is O, S, NR.sup.24 ; and,Z' is O or NR.sup.24 ;or pharmaceutically acceptable salt forms or prodrugs thereof, which are useful as retroviral protease inhibitors, and to pharmaceutical compositions comprising such compounds and methods of using the same for treating viral infection.Type: GrantFiled: August 21, 1996Date of Patent: June 9, 1998Assignee: The DuPont Merck Pharmaceutical CompanyInventor: George Vincent Delucca
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Patent number: 5744494Abstract: The anthelmintic efficacy in animals and humans of a benzimidazole such as fenbendazole, albendazole, oxfendazole or trichlabendazole is potentiated by use with piperonyl butoxide or other methylenedioxyphenyl synergist.Type: GrantFiled: July 25, 1995Date of Patent: April 28, 1998Assignee: British Technology Group LimitedInventors: Quintin Archibald McKellar, Hafid Abdelaali Benchaoui
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Patent number: 5741804Abstract: This invention relates to compounds of the formula: ##STR1## which are effective for inhibiting platelet aggregation, pharmaceutical compositions for effecting such activity, and a method for inhibiting platelet aggregation.Type: GrantFiled: May 30, 1995Date of Patent: April 21, 1998Assignee: SmithKline Beecham CorporationInventors: Richard McCulloch Keenan, William Henry Miller
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Patent number: 5693661Abstract: Certain vinyl acetylene benzimidazole compounds which inhibit the growth of picornaviruses, such as rhinoviruses, enteroviruses, cardioviruses, polioviruses, coxsackieviruses of the A and B groups, echo virus and Mengo virus.Type: GrantFiled: June 7, 1995Date of Patent: December 2, 1997Assignee: Eli Lilly and CompanyInventors: Shawn C. Miller, Frantz Victor, Wayne A. Spitzer, Thomas R. Sattelberg, Sr., Mark J. Tebbe
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Patent number: 5670485Abstract: The present invention is directed to anticoccidial methods, animal feed premixes, and animal feeds, employing a specified o-phenylenediamine or benzimidazole. The present invention is also directed to anticoccidial methods, animal feed premixes, and animal feeds employing two active agents. In such combined therapy, a first substance is a polyether antibiotic, and the second substance is a designated, benzimidazoline.Type: GrantFiled: April 21, 1995Date of Patent: September 23, 1997Assignee: Eli Lilly and CompanyInventor: George O. P. O'Doherty
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Patent number: 5569671Abstract: Novel compounds of formula I ##STR1## wherein R.sup.1 is independently hydrogen, hydroxy, alkyl with 1 to 6 carbon atoms, acyloxy groups with 1 to 6 carbon atoms, alkyloxy with 1 to 6 carbon atoms or from 1 to 5 sugar moieties; and R.sup.2 is independently hydrogen, or alkyl with 1 to 6 carbon atoms.The compounds are producible by aerobic cultivation on suitable nutrient media under suitable conditions of a strain of the fungus Ascochyta sp., subsequent recovery of the active component from the fermentation medium, and optionally modifying the active compound to obtain a compound of the desired formula I.Disclosed is also microorganisms capable of producing said compounds, compositions containing said compounds, and the use of such compositions for controlling fungi in valuable crops, animals, including birds and mammals, and in the preservation of wood, paints and edible products.Type: GrantFiled: April 24, 1995Date of Patent: October 29, 1996Assignee: Novo Nordisk A/SInventors: Ruby I. Nielsen, Frank W. Rasmussen
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Patent number: 5552422Abstract: The invention encompasses the novel compound of Formula I as well as a method of treating cyclooxygenase-2 mediated diseases comprising administration to a patient in need of such treatment of a non-toxic therapeutically effective amount of a compound of Formula I. ##STR1## The invention also encompasses certain pharmaceutical compositions for treatment of cyclooxygenase-2 mediated diseases comprising compounds of Formula I.Type: GrantFiled: January 11, 1995Date of Patent: September 3, 1996Assignee: Merck Frosst Canada, Inc.Inventors: Jacques Y. Gauthier, Cheuk K. Lau, Yves LeBlanc, Chun-Sing Li, Patrick Roy, Michel Therien, Zhaoyin Wang
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Patent number: 5545653Abstract: The present application provides a series of benzimidazole compounds which inhibit the growth of picornaviruses, such as rhinoviruses, enteroviruses, cardioviruses, polioviruses, coxsackieviruses of the A and B groups, echo virus and Mengo virus. Such compounds are also useful as intermediates for preparing additional benzimidazole antiviral compounds.Type: GrantFiled: June 7, 1995Date of Patent: August 13, 1996Assignee: Eli Lilly and CompanyInventors: Shawn C. Miller, Frantz Victor, Wayne A. Spitzer, Thomas R. Sattelberg, Sr., Mark J. Tebbe
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Patent number: 5541204Abstract: Compounds of the formula ##STR1## and pharmaceutically acceptable salts thereof wherein: R.sup.1 to R.sup.9 are as defined herein and m is the integer 0 or 1. These compounds are beta 3 adrenergic receptor agonists and are useful, therefore for example, in the treatment of diabetes, obesity, gastrointestinal diseases and achalasia.Type: GrantFiled: December 2, 1994Date of Patent: July 30, 1996Assignee: Bristol-Myers Squibb CompanyInventors: Philip M. Sher, William N. Washburn, Kathleen M. Poss
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Patent number: 5534535Abstract: Antiviral nucleoside analogues contain a substituted benzimidazole base attached to a carbocyclic ring in place of the conventional sugar residue. Particularly preferred compounds include those in which the 2-, 5- and 6- positions of the benzimidazole base are substituted by halogen. The compounds have activity against herpes virus especially cytomegalovirus and also hepatitis B virus infections.Type: GrantFiled: September 9, 1994Date of Patent: July 9, 1996Assignees: Burroughs Wellcome Co., The Regents of the University of MichiganInventors: Leroy B. Townsend, John C. Drach, Steven S. Good, Susan M. Daluge, Michael T. Martin
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Patent number: 5534534Abstract: A pharmaceutical composition for oral use comprising an effective amount of a compound of the formula (I) having antagonistic action to angiotensin II ##STR1## (wherein the ring W is an optionally substituted N-containing heterocyclic residue; R.sup.3 is a group capable of forming an anion or a group convertible thereinto; X is a direct bond or a spacer having an atomic length of two or less between the phenylene group and the phenyl group; and n is an integer of 1 or 2) and an oily substance having a lower melting point, and a method for preparing a pharmaceutical composition for oral use comprising an effective amount of a compound of the formula (I) and an oily substance having a lower melting point, which comprises admixing the compound of the formula (I) with an oily substance having a lower melting point and then subjecting the mixture to molding.Type: GrantFiled: November 18, 1992Date of Patent: July 9, 1996Assignee: Takeda Chemical Industries, Ltd.Inventors: Tadashi Makino, Yashio Mizukami, Jun-ichi Kikuta
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Patent number: 5532262Abstract: There are described new active compound combinations of a compound of the formula (I) ##STR1## with known fungicidal active compounds, and their use for the control of phytopathogenic fungi.Type: GrantFiled: June 5, 1995Date of Patent: July 2, 1996Assignee: Bayer AktiengesellschaftInventors: Wilhelm Brandes, Heinz-Wilhelm Dehne, Stefan Dutzmann, Karl-Heinz Kuck, Bernd-Wieland Kruger
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Patent number: 5521204Abstract: This invention is directed to certain 2-(alkoxycarbonylamino)- and 2-(alkoxycarbonylimino)benzlmidazole derivatives which are useful in the topical, oral or parenteral treatment of animals suffering from helminth infections.Type: GrantFiled: June 6, 1995Date of Patent: May 28, 1996Assignee: Pfizer Inc.Inventors: Bernard J. Banks, Christopher J. Dutton, Alexander C. Goudie
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Patent number: 5491161Abstract: Pyrroloimidazolyl and imidazopyridinyl substituted 1H-benzimidazole derivatives having the formula ##STR1## wherein n is 0 or 1;R.sup.1 is hydrogen, nitro, amino, mono- or di(C.sub.1-6 alkyl)amino, halo, C.sub.1-6 alkyl, hydroxy or C.sub.1-6 alkyloxy;R.sup.2 is hydrogen; C.sub.1-10 alkyl; C.sub.3-6 alkenyl; C.sub.3-6 alkynyl; C.sub.3-7 cycloalkyl; phenyl; substituted phenyl; C.sub.1-4 alkyl substituted with phenyl, substituted phenyl, naphthalenyl, thienyl, furanyl, C.sub.1-4 alkylfuranyl, C.sub.3-7 cycloalkyl; andR.sup.3 is hydrogen; C.sub.1-8 alkyl; C.sub.3-7 cycloalkyl; hydroxy; amino; C.sub.1-6 alkyloxy; C.sub.1-6 alkyloxycarbonylamino; phenyl; C.sub.1-4 alkyl substituted with phenyl, piperazinyl, 4-(C.sub.1-4 alkyl)piperazinyl or morpholinyl;each substituted phenyl independently is phenyl substituted with a substituent independently selected from halo, hydroxy, hydroxymethyl, trifluoromethyl, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy, C.sub.Type: GrantFiled: May 25, 1995Date of Patent: February 13, 1996Assignee: Janssen Pharmaceutica N.V.Inventors: Marcel A. C. Janssen, Alfons H. M. Raeymaekers, Eddy J. E. Freyne, Michael N. Greco
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Patent number: 5457102Abstract: Pyrroloimidazolyl and imidazopyridinyl substituted 1H-benzimidazole derivatives having the formula ##STR1## wherein n is 0 or 1;R.sup.1 is hydrogen, nitro, amino, mono- or di(C.sub.1-6 alkyl)amino, halo, C.sub.1-6 alkyl, hydroxy or C.sub.1-6 alkyloxy;R.sup.2 is hydrogen; C.sub.1-10 alkyl; C.sub.3-6 alkenyl; C.sub.3-6 alkynyl; C.sub.3-7 cycloalkyl; phenyl; substituted phenyl; C.sub.1-4 alkyl substituted with phenyl, substituted phenyl, naphthalenyl, thienyl, furanyl, C.sub.1-4 alkylfuranyl, C.sub.3-7 cycloalkyl; andR.sup.3 is hydrogen; C.sub.1-8 alkyl; C.sub.3-7 cycloalkyl; hydroxy; amino; C.sub.1-6 alkyloxy; C.sub.1-6 alkyloxycarbonylamino; phenyl; C.sub.1-4 alkyl substituted with phenyl, piperazinyl, 4-(C.sub.1-4 alkyl)piperazinyl or morpholinyl;each substituted phenyl independently is phenyl substituted with a substituent independently selected from halo, hydroxy, hydroxymethyl, trifluoromethyl, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy, C.sub.Type: GrantFiled: July 7, 1994Date of Patent: October 10, 1995Assignee: Janssen Pharmaceutica, N.V.Inventors: Marcel A. C. Janssen, Alfons H. M. Raeymaekers, Eddy J. E. Freyne, Michael N. Greco
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Patent number: 5441969Abstract: The present invention discloses compounds of the formula ##STR1## or a pharmaceutically-acceptable addition salt thereof whereinR' and R" independently of each other are hydrogen or alkyl, or R' and R" together form a 3 to 6 membered alkylene chain;one of R.sup.1 and R.sup.2 is aryl which may be substituted one or more times with halogen, CF.sub.3, CN, OH, alkyl, cycloalkylalkyl, alkenyl, alkynyl, alkoxy, amino, nitro, sulphamoyl, tetrazolyl, CO.sub.2 H, CO.sub.2 -alkyl and the other of R.sup.1 and R.sup.2 is hydrogen, halogen, alkoxy, amino or alkyl; andR.sup.4, R.sup.5, R.sup.6 and R.sup.7 independently of each other are hydrogen, halogen, amino, nitro, CN, OH, CF.sub.3, alkyl or alkoxy; and n is 0 or 1; provided that neither of R.sup.1 and R.sup.2 is phenyl or substituted phenyl when n is 0.The compounds are useful as pharmaceuticals, for example, in the treatment of ischemia, anoxia, migraine and psychosis.Type: GrantFiled: December 22, 1993Date of Patent: August 15, 1995Assignee: NeuroSearch A/SInventors: Oskar Axelsson, Dan Peters, Elsebet O Nielsen
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Patent number: 5432187Abstract: The present inventions relates to the use of certain benzimidazole compounds in the treatment of diseases caused by microsporidia organisms, in particular the treatment of diarrhea in patients infected with human immunodeficiency virus.Type: GrantFiled: September 15, 1993Date of Patent: July 11, 1995Assignee: SmithKline Beecham, p.l.c.Inventor: Brian G. Gazzard
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Patent number: 5369128Abstract: The invention provides a method of synchronizing farrowing in swine comprising the steps of administering an effective amount of a prostaglandin and then administering to the sows an effective amount of a peripheral .alpha..sub.2 adrenergic agonist, such that farrowing is induced.Type: GrantFiled: June 21, 1993Date of Patent: November 29, 1994Assignee: Iowa State University Research Foundation, Inc.Inventor: Walter H. Hsu
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Patent number: 5346704Abstract: This invention provides a dry pulverulent composition which is comprised of (1) a particulated agrochemical ingredient such as a herbicide; and (2) an inorganic salt ingredient such as sodium, potassium or ammonium bicarbonate or a mixture thereof, which is adsorbed on the surface of the agrochemical particles. The agrochemical ingredient can be a mixture of two or more biologically active organic compounds. The adsorbed inorganic salt ingredient also can be in a blend with a water-soluble or water-dispersible organic polymer ingredient as a film coating, and the coating of ingredients can function as a slow-release medium in the presence of moisture.Type: GrantFiled: August 11, 1993Date of Patent: September 13, 1994Assignee: Church & Dwight Co., Inc.Inventor: M. Stephen Lajoie
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Patent number: 5338551Abstract: This invention provides a dry pulverulent composition which is comprised of (1) a particulated agrochemical ingredient such as a herbicide; and (2) an inorganic salt ingredient such as sodium, potassium or ammonium bicarbonate or a mixture thereof, which is adsorbed on the surface of the agrochemical particles. The agrochemical ingredient can be a mixture of two or more biologically active organic compounds. The adsorbed inorganic salt ingredient also can be in a blend with a water-soluble or water-dispersible organic polymer ingredient as a film coating, and the coating of ingredients can function as a slow-release medium in the presence of moisture.Type: GrantFiled: July 2, 1992Date of Patent: August 16, 1994Inventor: M. Stephen Lajoie
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Patent number: 5326777Abstract: Microbicidal synergistic combinations of active compounds composed of known azol and benzimidazole derivatives are described, as is their use in the protection of materials.Type: GrantFiled: July 1, 1992Date of Patent: July 5, 1994Assignee: Bayer AktiengesellschaftInventors: Georg-Wilhelm Ludwig, Otto Exner, Hans-Georg Schmitt, Karl-Heinz Buchel, Graham Holmwood
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Patent number: 5314903Abstract: The present invention discloses compounds of the formula ##STR1## wherein R' and R" independently of each other are hydrogen or alkyl, or R' and R" together form a 3 to 6 membered alkylene chain;n is 1 or 2;R.sup.1 is phenyl which may be substituted one or more times with halogen, CF.sub.3, alkoxy, alkyl, or amino; andR.sup.4, R.sup.5, R.sup.6 and R.sup.7 independently of each other are hydrogen, halogen, amino, CF.sub.3, alkyl or alkoxy; or a pharmaceutically-acceptable addition salt thereof.The compounds are useful as pharmaceuticals, for example, in the treatment of ischemia, anoxia, migraine and psychosis.Type: GrantFiled: November 18, 1992Date of Patent: May 24, 1994Assignee: NeuroSearch A/SInventors: Oskar Axelsson, Mikkel Thaning, Peter Moldt
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Patent number: 5256681Abstract: [5(6)-(benzisoxa-, benzisothia- or indazol-3-yl)-1H-benzimidazol-2-yl]carbamates of formula (I) wherein R.sup.1 is hydrogen, C.sub.1-4 alkyl, halo, hydroxy or C.sub.1-4 alkyloxy; R.sup.2 is C.sub.1-4 alkyl; and X is O, S, SO, SO.sub.2 or NR.sup.3, said R.sup.3 being hydrogen, C.sub.1-4 alkyl, aryl or arylC.sub.1-4 alkyl. The compounds of formula (I) have anthelminthic properties. Compositions containing said compounds as active ingredient, a method of combating helminths, and a process for preparing said compounds and compositions.Type: GrantFiled: August 27, 1991Date of Patent: October 26, 1993Assignee: Janssen Pharmaceutica N.V.Inventors: Alfons H. M. Raeymaekers, Eddy J. E. Freyne, Gustaaf M. Boeckx
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Patent number: 5240940Abstract: Fungicidal compositions comprise a combination of two fungicides, one of which is a quinoline or cinnoline compound of the formula (1) ##STR1## the substituents being as described in the specification.Type: GrantFiled: May 12, 1992Date of Patent: August 31, 1993Assignee: DowElancoInventors: Wendell R. Arnold, Michael J. Coghlan, Glen P. Jourdan, Eriks V. Krumkalns, Robert G. Suhr
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Patent number: 5210091Abstract: The application discloses benzimidazole derivatives, pharmaceutical preparations comprised the compounds, their preparation and use in the treatment of disorders of the Central Nervous System such as ischemia, migraine, epilepsia, psychosis, Parkinsonism and depression.Type: GrantFiled: May 22, 1992Date of Patent: May 11, 1993Assignee: NeuroSearch A/SInventors: Oskar Axelsson, Mikkel Thaning, Peter Moldt
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Patent number: 5200422Abstract: A compound having the formula ##STR1## wherein R.sup.1 is hydrogen, NH.sub.2 or C.sub.1-6 -alkyl which may be branched;X is O, S, NCN;Y is O, S;R.sup.4, R.sup.5, R.sup.6 and R.sup.7 independently of each other are hydrogen, halogen, CF.sub.3, NO.sub.2, NH.sub.2, OH, C.sub.1-6 -alkoxy, C(.dbd.O)-phenyl or SO.sub.2 NR.sup.I R.sup.II wherein R.sup.I and R.sup.II independently are hydrogen or C.sub.1-6 -alkyl;R.sup.11 is hydrogen, halogen, NO.sub.2 or SO.sub.2 NR'R" wherein R' and R" independently are hydrogen or C.sub.1-6 -alkyl;R.sup.13 is hydrogen, halogen, phenyl, CF.sub.3, NO.sub.2 ;R.sup.12 is hydrogen or together with R.sup.13 forms a C.sub.4-7 -carbocyclic ring which may be aromatic or partially saturated;R.sup.14 is hydrogen or together with R.sup.13 forms a C.sub.Type: GrantFiled: July 17, 1991Date of Patent: April 6, 1993Assignee: NeuroSearch A/SInventors: Soren-Peter Olesen, Frank Watjen
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Patent number: 5190932Abstract: The invention relates to the use of water-soluble polymers containing chemically bonded tertiary and/or quaternary ammonium groups as auxiliaries for formulating microbicides, the microbicide formulations prepared using these water-soluble polymers and the use of these formulations for preserving industrial materials.Type: GrantFiled: July 11, 1990Date of Patent: March 2, 1993Assignee: Bayer AktiengesellschaftInventors: Rolf Dhein, Lothar Backer, Otto Exner, Walter Radt, Ingrid Radt, Christian Radt, Hans G. Schmitt
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Patent number: 5185357Abstract: An antifungal composition made up of at least one compound represented by the formula (I): ##STR1## wherein X represents a group of the formula --NHCOOR in which R is --CH.sub.3 or --C.sub.2 H.sub.5, or 4-thiazolyl group and at least one compound represented by the formula (II): ##STR2## wherein Y represents hydrogen or halogen, Z represents halogen and R represents alkyl group of 1 to 8 carbon atoms. The composition preferably comprises 10 to 90% by weight of the compound(s) of formula (I).Type: GrantFiled: February 21, 1991Date of Patent: February 9, 1993Assignee: Shinto Paint Co., Ltd.Inventor: Keiichiro Inui
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Patent number: 5179116Abstract: A wood preservative which is based on a dimethylalkylamine and an acid and contains dimethylalkylamine, a water-soluble acid and a water-insoluble acid and/or 2-(methoxycarbonylamino)-benzimidazole is used for preserving wood.Type: GrantFiled: June 5, 1992Date of Patent: January 12, 1993Assignee: Dr. Wolman GmbHInventors: Reimer Goettsche, Hans-Volker Borck, Hans-Norbert Marx
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Patent number: 5149700Abstract: This invention relates to substituted arylsulfonamides and benzamides possessing aniarrhythmic activity, to pharmaceutical compositions and to methods for production thereof.Type: GrantFiled: October 30, 1991Date of Patent: September 22, 1992Assignee: American Home Products CorporationInventors: John W. Ellingboe, Jehan F. Bagli, Michael W. Winkley
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Patent number: 5147887Abstract: A fungicidal composition comprising a fungicidally effective amount of (i) a substituted 1-hydroxyethyl-triazole of the formula ##STR1## in which A is --CH.sub.2 CH.sub.2 -- or --CH.dbd.CH--, or an addition product thereof with an acid or metal salt, and (ii) at least one member selected from the group consisting ofA) wettable sulphur,B) a polyhalogenoalkylthio derivative,C) a quanidine derivative,D) an aromatic carboxylic acid derivative,E) a dithiocarbamate,F) a benzimidazole derivative,G) an imidazole or triazole derivative,H) a phosphoric acid ester,I) a tetrahydroquinoline derivative,J) an S,N-heterocyclene compound,K) a urea derivative,L) a sulphonamide derivative,M) a polyhydroxy ether derivative,N) a triazine derivative,O) a copper complex salt,P) an N-formyl derivative,Q) a morpholine derivative,R) a quinoxaline derivative, andS) a dicarboximide derivative.Type: GrantFiled: June 6, 1991Date of Patent: September 15, 1992Assignee: Bayer AktiengesellschaftInventors: Wilhelm Brandes, Gerd Hanssler, Paul Reinecke, Hans Scheinpflug, Graham Holmwood
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Patent number: 5135928Abstract: This invention relates to novel triazolo derivatives, a process for the preparation thereof, pharmaceutical compositions comprising the same, to the use of the said triazolo derivatives for the treatment of diseases and also for the preparation of pharmaceutical compositions suitable for the treatment of the said diseases.The new triazolo derivatives of the general formulae (Ia) and (Ib), ##STR1## wherein Q represents hydrogen or a heterocyclic group optionally bearing one or more C.sub.1-4 alkyl substituent(s); or a group of the formula SR.sup.1, whereinR.sup.1 stands for straight or branched chained C.sub.1-4 alkyl or phenyl-(C.sub.1-4 alkyl); or q represents a group of the formula NR.sup.2 R.sup.3, whereinR.sup.2 and R.sup.3 each represent hydrogen, straight or branched chain C.sub.1-12 alkyl, C.sub.2-6 alkenyl or phenyl-(C.sub.1-4 alkyl);R.sup.4 and R.sup.7 each represent hydrogen, C.sub.1-6 alkyl or phenyl-(C.sub.1-4 alkyl) optionally bearing one or more halogen substituent(s);R.sup.5 and R.sup.Type: GrantFiled: October 25, 1990Date of Patent: August 4, 1992Assignee: Egis GyogyszergyarInventors: Jozsef Reiter, Jozsef Barkoczy, Lujza Petocz, Frigyes Gorgenyi, Marton Fekete, Eniko Szirt nee Kiszelly, Gabor Gigler, Istvan Gacsalyi, Istvan Gyertyan, Klara Reiter nee Esses
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Patent number: 5106857Abstract: A method of treating cardiac arrhythmias and muscle tension and spasticity with N-(1-methyl-3-pyrrolidinyl)-1-(phenylmethyl)-1H-benzimidazol-2-amine and analogs and the pharmaceutical compositions are herein disclosed. Illustratively, the compound having the structure: ##STR1## corrects an induced arrhythmia in 7 out of 8 dogs at 7 mg/kg IV and has an ED.sub.50 of 21 mg/kg in the mouse Straub-tail test.Type: GrantFiled: May 9, 1991Date of Patent: April 21, 1992Assignee: A. H. Robins Company, IncorporatedInventors: Albert D. Cale, Jr., Thomas W. Gero
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Patent number: 5043338Abstract: The invention relates to synergistic combinations of known fungicide active ingredients and their application in plant protection.Type: GrantFiled: May 21, 1990Date of Patent: August 27, 1991Assignee: Chinoin Gyogyszer- es Vegyeszeti Termekek Gyara, R.T.Inventors: Tamas Detre, Lajos Rejto, Jozsef Sos, Andras Szego, Erzsebet Schuszler, Sandor ngyan, Katalin Keller Nee Marmarosi, Horst Lyr, Dieter Zanke, Brita Lenner, Marlies Strump, Gyula Oros, Ferenc Viranyi, Tibor rsek, Gyongyver Nagy, Laszlo Hornok, Attila Molnar
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Patent number: 5039691Abstract: Furanone compounds and compositions having anticholinergic activity are described. The compounds have the formula: ##STR1## wherein: the dashed line indicates either the 4,5-unsaturated or the 4,5-dihydrofuranone ring;R.sub.1 and R.sub.2 may be the same or different and are hydrogen, thienyl, furanyl, or cycloalkyl (C.sub.3 -C.sub.6), benzyl, phenyl, substituted phenyl or substituted benzyl wherein the phenyl or benzyl group may be substituted with halogen, trifluoromethyl, lower alkyl, lower alkoxy or hydroxy;R.sub.3, R.sub.4 and R.sub.5 may be the same or different and are hydrogen, lower alkyl, lower alkyl substituted with a halogen, alkoxy, amino or carboxylic acid group, an alkyl or alkylene bridge between R.sub.4 and R.sub.5 or R.sub.3 and the ring N, trifluoromethyl, nitro, a cycloalkyl group containing 3 to 6 carbons, halogen, benzyl, phenyl, substituted phenyl or substituted benzyl, for which the substituents are the same as those set forth for R.sub.1 and R.sub.2 substituted benzyl or phenyl.R.sub.Type: GrantFiled: May 8, 1990Date of Patent: August 13, 1991Assignee: Marion Merrell Dow Inc.Inventors: Ciro J. Spagnuolo, Carl Kaiser, Theodore Adams
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Patent number: 4988693Abstract: The invention relates to synergistic combinations of known fungicide active ingredients and their application in plant protection.Type: GrantFiled: December 5, 1988Date of Patent: January 29, 1991Assignee: Chinoin Gyogyszer- Es Vegyeszeti Termekek Gyara, R. T.Inventors: Tamas Detre, Lajos Rejto, Jozsef Sos, Andras Szego, Ferenc Viranyi, Tibor rsek, Gyongyver Nagy nee Hegyi, Laszlo Hornok, Attila Molnar, Erzsebet Schuszler, Sandor ngyan, Katalin Marmarosi, nee Kellner, Lyr Horst, Dieter Zanke, Brita Lenner, Marlies Strump, Gyula Oros
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Patent number: 4980346Abstract: The invention relates to synergistic fungicidal and acaricidal compositions containing two or three active ingredients in a ratio of 10:1-1:10 and 20:1:1-1:10:10, selected from the group of N-alkyl(ene)-N-(0,0-disubstituted-thiophosphoryl)-N', N'-substituted glycine amide derivatives, Triforine, Carbendazim, copper-oxyquinolate, cycloheximide, Mancozeb, benzimidazole derivatives, phenyl amide derivatives F-849, Folpet, Captofol, Iprodione or S-39475.Type: GrantFiled: January 11, 1989Date of Patent: December 25, 1990Assignee: Eszakmagyarorsuagi VegyimuvekInventors: Karoly Balogh, Marta Bartha nee Kocsis, Zsuzsa Dancs nee Rozsnyai, Erzsebet Grega nee Toth, Magdolna Magyar nee Tomorkenyi, Istvan Nagy, Jozsef Nagy, Gyongyver S. Nagy nee Hegyi, Gyula Oros, Csaba Pavliscsak, Karoly Pasztor, Gyula Tarpai, Eszter Urszin nee Simon
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Patent number: 4940722Abstract: A seed disinfectant composition comprising(A) (E)-1-(2,4-dichlorophenyl)-4,4-dimethyl-2-(1,2,4-triazol-1-yl)-1-penten-3- ol containing not less than 50% by weight of (-)-(E)-1-(2,4-dichlorophenyl)-4,4-dimethyl-2-(1,2,4-triazol-1-yl)-1-pente n-3-ol and(B) At least one benzimidazole thiophanate fungicide and optionally comprising(C) O,O-dimethyl-O-(2,6-dichloro-4-methylphenyl)phosphorothioate and/or(D) 1-Ethyl-1,4-dihydro-6,7-methylenedioxy-4-oxo-3-quinoline carboxylic acid or a salt thereof are disclosed. The seed disinfectant composition of the present invention exhibits a synergistically high preventing effect on various seed born diseases and simultaneously has a wide antifungal spectrum and shows a stable preventing effect on the fungi having resistance to conventional disinfectants.Type: GrantFiled: November 17, 1987Date of Patent: July 10, 1990Assignee: Sumitomo Chemical Companmy, LimitedInventor: Hirotaka Takano
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Patent number: 4906653Abstract: A method for controlling molluscs with 2-(2-chloro-1-methoxyethoxy)phenyl methylcarbamate of the formula ##STR1## and molluscicides containing a mixture of 2-(2-chloro-1-methoxyethoxy)phenyl methylcarbamate with methyl benzimidazol-2-ylcarbamate is described.Type: GrantFiled: February 10, 1988Date of Patent: March 6, 1990Assignee: BASF AktiengesellschaftInventors: Karl Kiehs, Christoph Kuenast
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Patent number: 4874759Abstract: Hydroxyindole-3-carboxylic acid amide compounds of the general formula: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are, the same or different, respectively a hydrogen atom, an alkyl group, an aryl group, an aralkyl group or a heteroaryl group, or R.sup.1 and R.sup.2 and/or R.sup.3 and R.sup.4 are respectively groups which are combined to each other taken together with the adjacent nitrogen atom to form a heterocyclic group, R.sup.5 is an alkyl group, R.sup.6 is a hydrogen atom, an alkyl group, a cycloalkyl group, an aryl group or an aralkyl group and X is a hydrogen atom, a halogen atom or a lower alkanoyl group, or their acid addition salts.These compounds are of use as diuretics or a therapeutic medicine for circulation system diseases.Type: GrantFiled: September 23, 1988Date of Patent: October 17, 1989Assignee: Yoshitomi Pharmaceutical Industries, Ltd.Inventors: Tetsuya Tahara, Tsuguo Ikebe, Ichiro Hakamada, Osamu Yaoka
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Patent number: 4859689Abstract: There is disclosed a fungicidal composition comprising (A) a fungicidal compound selected from the group consisting of (i) benzimidazole compounds of the formula ##STR1## wherein W is H, or alkyl carbamoyl; Y is thiazolyl, dihydrothiazolyl, tetrahydrothiazolyl or furyl; Z is H, halogen or alkyl and (ii) benzimidazole related compounds of the formula ##STR2## wherein R.sub.3 is C.sub.1-2 alkyl, and Z is as defined above, and (B) a synergist alkyl pyridinium salt of the formula ##STR3## wherein R is an alkyl containing 8 to 20 carbon atoms; and X is a monovalent anion.Type: GrantFiled: October 31, 1986Date of Patent: August 22, 1989Assignee: Safer, Inc.Inventors: George S. Puritch, Edward S. Kondo
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Patent number: 4857541Abstract: A fungicide which is particularly effective against benomyl resistant fungi is selected from the group of fungicides represented by the formula: ##STR1## wherein R is C.sub.n H.sub.2n+1 and n is 1, 2, 3 or 6 or R is phenyl. The method comprises applying as a suspension an effective amount of the one or more fungicides selected from the formula to benomyl resistant fungi, such as benomyl resistant isolates of Botrytis cinerea.Type: GrantFiled: August 7, 1986Date of Patent: August 15, 1989Assignee: Canadian Patents and Development Limited/Societe Canadienne Des Brevets et D'Exploitation LimiteeInventor: Mikio Chiba
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Patent number: 4843090Abstract: A controlling composition for Fusarium diseases caused by the benzimidazole-resistant or sensitive strain of Fusarium which comprises as an active ingredient a benzimidazole derivative represented by the general formula (I) (hereinafter referred to as present composition), ##STR1## wherein R represents a C.sub.1 -C.sub.3 lower alkyl group, and n represents 1, 2 or 3.Type: GrantFiled: September 8, 1988Date of Patent: June 27, 1989Assignee: Sumitomo Chemical Company, LimitedInventors: Hiroki Tomioka, Tadashi Ooishi, Naonori Hirata
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Patent number: 4831032Abstract: The present invention provides benzimidazoles of the general formula: ##STR1## wherein R.sub.1, X, A, and R.sub.2 are as defined in the specification. The present invention also provides processes for the preparation of these new benzimidazoles and pharmaceutical compositions containing them, as well as intermediates for the preparation thereof.The new benzimidazoles are useful to treat heart or circulatory diseases which respond to a lowering of blood pressure, a positive inotropic action and/or an improvement in microcirculation.Type: GrantFiled: July 3, 1986Date of Patent: May 16, 1989Assignee: Boehringer Mannheim GmbHInventors: Wolfgang von der Saal, Alfred Mertens, Herbert Berger, Bernd Muller-Beckmann, Klaus Strein
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Patent number: 4826862Abstract: Novel [(5(6) (1H-azole-1-ylmethyl)benzimidazole]carbamates derivatives having anthelminthic properties, compositions containing these compounds as active ingredient, and a method for combating the growth of helminths.Type: GrantFiled: February 12, 1988Date of Patent: May 2, 1989Assignee: Janssen Pharmaceutica, N.V.Inventors: Alfons H. M. Raeymaekers, Eddy J. E. Freyne
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Patent number: 4745125Abstract: Antiulcer amino-benzimidazole compounds substituted on the nitrogen; these compounds correspond to the following general formula: ##STR1## in which the various substituents are defined hereinbelow.Type: GrantFiled: January 20, 1987Date of Patent: May 17, 1988Assignee: NovapharmeInventors: Jacques N. Astoin, Bernard Hublot, Francis Lepage
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Patent number: 4737510Abstract: Novel bioactive metabolites from the Caribbean sponge Agelas coniferin are disclosed. These compounds are generically referred to as halopyrroles. They exhibit antiviral and antibacterial properties, and, thus, are useful for various non-therapeutic and therapeutic purposes.Type: GrantFiled: September 30, 1986Date of Patent: April 12, 1988Assignee: The Board of Trustees of The University of IllinoisInventor: Kenneth L. Rinehart, Jr.
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Patent number: 4730003Abstract: The present invention provides compounds of the general formula: ##STR1## wherein the various substituents are defined hereinbelow. The compounds are used for the treatment and/or prophylaxis of heart and circulatory diseases.Type: GrantFiled: September 4, 1986Date of Patent: March 8, 1988Assignee: Boehringer Mannheim GmbHInventors: Wolfgang von der Saal, Alfred Mertens, Herbert Berger, Bernd Muller-Beckmann
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Patent number: 4721717Abstract: The present invention provides aminoalcohols of the general formula: ##STR1## wherein R.sub.1 and R.sub.2, which can be same or different, are hydrogen atoms, hydroxyl groups, C.sub.1 -C.sub.4 -alkoxy, benzyloxy, C.sub.1 -C.sub.4 -alkoxycarbonyl, C.sub.1 -C.sub.4 -alkanesulphonylamino, C.sub.1 -C.sub.4 -alkanesulphinyl or C.sub.1 -C.sub.4 -alkanesulphonyl radicals, m is 2, 3 or 4, X and Y, which can be the same or different, are hydrogen atoms or benzyl radicals and R.sub.3 is a phenyl radical substituted twice by C.sub.1 -C.sub.6 -alkyl radicals, a nitrophenyl radical, an aminophenyl radical, a 1,3,5-tri-C.sub.1 -C.sub.6 -alkyl-2,4-dioxo-1H,3H-pyrimidin-6-yl radical, an indolyl radical, an indazolyl radical, a benzimidazolyl radical, a 1,4-di-C.sub.1 -C.sub.6 -alkylpyrazol-5-yl radical or a radical of the general formula: ##STR2## wherein R.sub.4 and R.sub.5, which can be the same or different, are C.sub.1 -C.sub.4 -alkyl radicals and R.sub.6 is a C.sub.1 -C.sub.6 -alkyl, C.sub.2 -C.sub.Type: GrantFiled: July 29, 1985Date of Patent: January 26, 1988Assignee: Boehringer Mannheim GmbHInventors: Walter-Gunar Friebe, Wolfgang Kampe, Erwin Bohm, Klaus Strein
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Patent number: 4618620Abstract: A fungicidal composition which comprises an inert carrier and as an active ingredient (E)-1-(2,4-dichlorophenyl)-4,4-dimethyl-2-(1,2,4-triazol-1-yl)-1-penten-3- ol and a benzimidazole-thiophanate type fungicide in the ratio of 1 to 0.1 to 10 by part by weight in a total amount of 0.1 to 99.9% by weight.Type: GrantFiled: August 14, 1985Date of Patent: October 21, 1986Assignee: Sumitomo Chemical Company, LimitedInventors: Yukio Ishiguri, Hirotaka Takano, Yuji Funaki