Patents Examined by Lenora Miltenberger
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Patent number: 5019565Abstract: Fungicidal pyridyl imidates having the general structural formula ##STR1## wherein R is selected from the group consisting of C.sub.1 -C.sub.16 alkyl, C.sub.3 -C.sub.8 cycloalkyl, C.sub.2 -C.sub.8 alkenyl, C.sub.2 -C.sub.8 substituted alkenyl, C.sub.3 -C.sub.4 carboalkoxyalkyl, aryl, arylalkyl having C.sub.1 -C.sub.3 alkyl, substituted aryl and arylalkyl wherein the substituents are -Cl, -Br, -F and -NO.sub.2, furfuryl pyridyl, C.sub.1 -C.sub.6 alkoxyl substituted thiophosphorus, and ##STR2## wherein R.sub.3 and R.sub.4 are C.sub.1 -C.sub.10 alkyl and can form a heterocyclic ring, 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 haloalkoxy, R.sub.2 is selected from the group consisting of methyl and hydrogen, and X is S or O; and fungicidally acceptable organic and inorganic salts thereof.Type: GrantFiled: December 4, 1989Date of Patent: May 28, 1991Assignee: ICI Americas Inc.Inventors: Don R. Baker, Keith H. Brownell
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Patent number: 5011851Abstract: Heterocyclic acids and esters useful as inhibitors of mammalian blood platelet aggregation characterized by Formula I or II are disclosed.HET.sub.1 --(CH.sub.2).sub.n CO.sub.2 R (I) ##STR1## Formula I compounds are those wherein n is 6-9, R is hydrogen, lower alkyl or an alkali metal ion, and HET.sub.1 is the heterocyclic radical 4,5-diphenyl-1H-imidazol-2-yl.Formula II compounds are those wherein R.sub.1 is hydrogen, lower alkyl or an alkali metal ion, and the radical --OCH.sub.2 CO.sub.2 R is attached in the 3 or 4 ring position; and HET.sub.2 is the heterocyclic radical 4,5-diphenyl-1H-imidazol-2-yl.Formula VIII compounds are those wherein R.sub.1 is hydrogen, lower alkyl or an alkali metal ion, and the radical --OCH.sub.2 CO.sub.2 R is attached in the 3 or 4 ring position.Type: GrantFiled: June 20, 1990Date of Patent: April 30, 1991Assignee: Bristol-Myers Squibb Co.Inventor: Nicholas A. Meanwell
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Patent number: 5011838Abstract: 2-substituted 3-(2-ethoxyethyl)imidazo[4,5-b] pyridine derivatives of the formula ##STR1## wherein n is an integer of from 1 to 5 inclusiveR.sub.1 and R.sub.2 represent each a saturated or unsaturated alkyl radical containing from 1 to 4 carbon atoms or they form, together with the adjacent nitrogen atom an optionally substituted heterocyclic ring andthe corresponding non-toxic pharmaceutically acceptable acid addition salts.The compounds of formula (I) are endowed with antiallergic and antihistaminic activity.Type: GrantFiled: May 7, 1990Date of Patent: April 30, 1991Assignee: Dompe Farmaceutici S.p.A.Inventors: Giani Roberto, Parini Ettore, Borsa Massimiliano, Lavezzo Antonio
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Patent number: 5010086Abstract: 1,3-dihydro-2H-imidazo[4,5-b]pyridin-2-ones having an aryl or heteroaryl group in the 6-position, useful as phosphodiesterase inhibitors, are prepared by reacting a 2-amino-5-(aryl or heteroaryl)pyridine-3-carboxylic acid with diphenylphosphoryl azide. The compounds are of the formula ##STR1## where R.sub.1 and R.sub.3 are hydrogen or lower-alkyl, R.sub.5 is lower-alkyl or fluorinated lower-alkyl, and Ar is 4-or 3-pyridinyl, or N-oxides thereof, or phenyl or substituted phenyl.Type: GrantFiled: August 7, 1990Date of Patent: April 23, 1991Assignee: Sterling Drug Inc.Inventors: George Y. Lesher, deceased, Edward R. Bacon, Baldev Singh, Gee-Hong Kuo
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Patent number: 5008392Abstract: The invention relates to a process for the preparation of pyridine-2,3-dicarboxylic acid esters using novel maleic acid esters as starting materials. In the process, in a first process step, 2,3-dihalomaleic acid esters are reacted with ammonia, or ammonium salts, with the exclusion of water at a temperature of at least 50.degree. C. to form novel 2-amino-3-halomaleic acid esters, and these are subsequently reacted further in a second process step with .alpha.,.beta.-unsaturated aldehydes, or ketones, in the presence of an acidic catalyst and acid-binding agents at a temperature of at least 50.degree. C. with heat being supplied until the pyridine-2,3-dicarboxylic acid esters have been formed. Pyridine-2,3-dicarboxylic acid esters of this type can be used, for example, as intermediates for synthesis of herbicides based on imidazoline. The present invention also relates to novel 2-amino-3-halomaleic acid esters, which are useful for producing the final product pyridine-2,3-dicarboxylic acid esters.Type: GrantFiled: November 27, 1989Date of Patent: April 16, 1991Assignee: Wacker-Chemie GmbHInventors: Josef Meier, Wolfgang Deinhammer, Konrad Krageloh
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Patent number: 5006546Abstract: The invention provides: (2S,4R,6S)-6-[(4,5-diphenylimidazol-2-yl)thiomethyl]-4-hydroxy-2-methoxy-3 ,4,5,6-tetrahydro-2H-pyran and (2R,4R,6S)-6-[(4,5-diphenylimidazol-2-yl)thiomethyl]-4-hydroxy-2-methoxy-3 ,4,5,6-tetrahydro-2H-pyran or a mixture thereof; the compounds are anti-atherosclerotic agents.Type: GrantFiled: March 26, 1990Date of Patent: April 9, 1991Assignee: Rhone-Poulenc SanteInventor: Edward C. J. Coffee
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Patent number: 4997951Abstract: Imidazoline compounds of formula ##STR1## where n denotes 2 or 3, is suitable as cure accelerator in curable epoxide resin compositions comprising a latent curing agent.Type: GrantFiled: March 8, 1990Date of Patent: March 5, 1991Assignee: Ciba-Geigy CorporationInventor: Madan M. Bagga
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Patent number: 4994575Abstract: Imidazolines of the formula: ##STR1## wherein n is a whole number integer of from 1 to 6, are metal corrosion inhibitors.Type: GrantFiled: October 30, 1989Date of Patent: February 19, 1991Assignee: Union Camp CorporationInventor: Ewa A. Bardasz
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Patent number: 4992090Abstract: Imidazole derivatives of formula I ##STR1## and stereochemically isomeric forms thereof, and their salts, have useful herbicidal properties. The substituents R.sup.1, L and X have the meanings defined herein.Type: GrantFiled: June 5, 1989Date of Patent: February 12, 1991Assignee: Ciba-Geigy CorporationInventor: Hans-Dieter Schneider
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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: 4985422Abstract: Compounds which are potent and selective antagonists of the effect of 5-HT.sub.3 receptors and are useful in the treatment of psychotic disorders, anxiety, and nausea and vomiting, of the general formula (I) ##STR1## wherein Im represents an imidazolyl group of the formula (a), (b) or (c): ##STR2## one of the groups represented by R.sup.1, R.sup.2 and R.sup.3 is a hydrogen atom or a C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-6 alkenyl, phenyl or phenyl C.sub.1-3 alkyl group, and each of the other two groups, which may be the same or different, represents a hydrogen atom or a C.sub.1-6 alkyl group;n represents 1 or 2;Q represents a hydrogen atom, a halogen atom, or a hydroxy, C.sub.1-4 alkoxy, phenyl C.sub.1-3 alkoxy or C.sub.1-6 alkyl group, or a group --NR.sup.4 R.sup.5 or --CONR.sup.4 R.sup.5 ; andX represents an oxygen or a sulphur atom, and, when Im represents an imidazolyl group of formula (c), X may also represent the group NR.sup.6, where R.sup.Type: GrantFiled: April 26, 1989Date of Patent: January 15, 1991Assignee: Glaxo Group LimitedInventors: Peter C. North, Alexander W. Oxford, Ian H. Coates, Paul J. Beswick
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Patent number: 4983620Abstract: New alkylthiobenzimidazole derivatives are described which belong to the class of formula: ##STR1## wherein R.sub.1 and R.sub.2 each represent a 1-3 carbon atom alkyl radical or they may form with the adjacent nitrogen atom, an optionally substituted heterocyclic ring,X represents a hydrogen atom or methyl radicaln is 1 or 2R.sub.3 represents a 4-6 carbon atom alkoxyalkyl radical, a 7 or 8 carbon atom arylalkyl radical or a 5 or 6 carbon atom cycloalkyl radical with the exception that R.sub.3 may not be an arylalkyl radical when R.sub.1 and R.sub.2 each represent a 1-3 carbon atom alkyl radicalR.sub.4 and R.sub.5 may be the same or different and each represent a hydrogen atom or a 1-2 carbon atom alkyl or they, attached at the positions 5 and 6 of the benzimidazole nucleus, may form together the ring ##STR2## The compounds (I) possess interesting antihistaminic and anti-allergic activities.Type: GrantFiled: March 22, 1989Date of Patent: January 8, 1991Assignee: Dompe Farmaceutici S.p.A.Inventors: Roberto P. Giani, Ettore Parini, Giancarlo Tonon
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Patent number: 4980468Abstract: 3-7-Diheterabicyclo[3.3.1]nonanes and derivatives thereof are disclosed. Their method of preparation and use as antiarrhythmic agents is given.Type: GrantFiled: December 11, 1989Date of Patent: December 25, 1990Assignee: Board of Regents for The Oklahoma Agricultural and Mechanical Colleges Acting for and on Behalf of Oklahoma State UniversityInventors: Kenneth D. Berlin, Mark D. Thompson, Benjamin J. Scherlag, Gary S. Smith
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Patent number: 4980362Abstract: The present invention describes a process to obtain 4-substituted 2-alkoxytetrahydrofuran derivatives of formula I, ##STR1## wherein, --R.sub.1 represents an alkyl or phenylalkyl radical; --R.sub.2 is hydrogen, C.sub.1 -C.sub.4 -acryl or C.sub.1 -C.sub.4 -alkoxycarbonyl; --R.sub.3 is either an electron pair, in which case t means nothing and q is zero, or R.sub.3 is hydrogen or C.sub.1 -C.sub.4 alkyl, in which case t is (+) and q=1; A- is a pharmaceutically acceptable anion. These compounds are antagonists of PAF and, therefore, useful for the treatment of the diseases in which this substance is involved.Type: GrantFiled: January 30, 1990Date of Patent: December 25, 1990Assignee: J. Uriach & CIA. S.A.Inventors: Elena Carceller, Javier Bartroli'
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Patent number: 4977271Abstract: A Reissert compound of bisbenzimidazole can be formed by first reacting benzimidazole with an aliphatic diacid chloride to form bisbenzimidazole and then reacting the bisbenzimidazole with an aliphatic acid chloride and cyanide to form the Reissert compound thereof.Type: GrantFiled: October 6, 1989Date of Patent: December 11, 1990Assignee: Virginia Tech Intellectual Properties Inc.Inventors: Harry W. Gibson, Yajnanarayana H. R. Jois
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Patent number: 4973703Abstract: A process for the purification of N-cyano-N'-methyl-N"-[2-{(5-methyl-1H-imidazol-4-yl)methylthio}-ethyl]guan idine, which comprises bringing a crude product of N-cyano-N'-methyl-N"-[2-{(5-methyl-1H-imidazol-4-yl)-methylthio}ethyl]guan idine into contact with activated carbon in water in the presence of an organic acid.Type: GrantFiled: November 4, 1988Date of Patent: November 27, 1990Assignee: Mitsui Petrochemical Industries, Ltd.Inventors: Junichi Imuta, Noriaki Kihara, Takeshi Ishitoku
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Patent number: 4963561Abstract: Novel 1,3-dihydro-2H-imidazo[4,5-b]pyridin-2-ones having an aryl or heteroaryl group in the 6-position, useful as phosphodiesterase inhibitors, are prepared by reacting a 2-amino-5-(aryl or heteroaryl)pyridine-3-carboxylic acid with diphenylphosphoryl azide. The compounds are of the formula ##STR1## where R.sub.1 and R.sub.3 are hydrogen or lower-alkyl, R.sub.5 is lower-alkyl or fluorinated lower-alkyl, and Ar is 4- or 3-pyridinyl, or phenyl or substituted phenyl.Type: GrantFiled: February 28, 1990Date of Patent: October 16, 1990Assignee: Sterling Drug Inc.Inventors: George Y. Lesher, Edward R. Bacon, Baldev Singh, Gee-Hong Kuo
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Patent number: 4933460Abstract: Novel 3-(piperidinyl)- and 3-(pyrrolidinyl)-1H-indazoles, intermediates and processes for the preparation thereof, and methods for treating psychoses, treating depression, alleviating pain, treating convulsions and treating hypertension utilizing compounds or compositions thereof are disclosed.Type: GrantFiled: May 13, 1989Date of Patent: June 12, 1990Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventor: Joseph T. Strupczewski