Patents Examined by Lenora Miltenberger
  • Patent number: 5019565
    Abstract: 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: Grant
    Filed: December 4, 1989
    Date of Patent: May 28, 1991
    Assignee: ICI Americas Inc.
    Inventors: Don R. Baker, Keith H. Brownell
  • Patent number: 5011851
    Abstract: 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: Grant
    Filed: June 20, 1990
    Date of Patent: April 30, 1991
    Assignee: Bristol-Myers Squibb Co.
    Inventor: Nicholas A. Meanwell
  • Patent number: 5011838
    Abstract: 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: Grant
    Filed: May 7, 1990
    Date of Patent: April 30, 1991
    Assignee: Dompe Farmaceutici S.p.A.
    Inventors: Giani Roberto, Parini Ettore, Borsa Massimiliano, Lavezzo Antonio
  • Patent number: 5010086
    Abstract: 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: Grant
    Filed: August 7, 1990
    Date of Patent: April 23, 1991
    Assignee: Sterling Drug Inc.
    Inventors: George Y. Lesher, deceased, Edward R. Bacon, Baldev Singh, Gee-Hong Kuo
  • Patent number: 5008392
    Abstract: 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: Grant
    Filed: November 27, 1989
    Date of Patent: April 16, 1991
    Assignee: Wacker-Chemie GmbH
    Inventors: Josef Meier, Wolfgang Deinhammer, Konrad Krageloh
  • Patent number: 5006546
    Abstract: 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: Grant
    Filed: March 26, 1990
    Date of Patent: April 9, 1991
    Assignee: Rhone-Poulenc Sante
    Inventor: Edward C. J. Coffee
  • Patent number: 4997951
    Abstract: 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: Grant
    Filed: March 8, 1990
    Date of Patent: March 5, 1991
    Assignee: Ciba-Geigy Corporation
    Inventor: Madan M. Bagga
  • Patent number: 4994575
    Abstract: Imidazolines of the formula: ##STR1## wherein n is a whole number integer of from 1 to 6, are metal corrosion inhibitors.
    Type: Grant
    Filed: October 30, 1989
    Date of Patent: February 19, 1991
    Assignee: Union Camp Corporation
    Inventor: Ewa A. Bardasz
  • Patent number: 4992090
    Abstract: 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: Grant
    Filed: June 5, 1989
    Date of Patent: February 12, 1991
    Assignee: Ciba-Geigy Corporation
    Inventor: Hans-Dieter Schneider
  • Patent number: 4987140
    Abstract: 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: Grant
    Filed: November 27, 1989
    Date of Patent: January 22, 1991
    Assignee: Roussel Uclaf
    Inventors: Francois Clemence, Odile Le Martret, Francoise Delevallee
  • Patent number: 4985422
    Abstract: 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: Grant
    Filed: April 26, 1989
    Date of Patent: January 15, 1991
    Assignee: Glaxo Group Limited
    Inventors: Peter C. North, Alexander W. Oxford, Ian H. Coates, Paul J. Beswick
  • Patent number: 4983620
    Abstract: 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: Grant
    Filed: March 22, 1989
    Date of Patent: January 8, 1991
    Assignee: Dompe Farmaceutici S.p.A.
    Inventors: Roberto P. Giani, Ettore Parini, Giancarlo Tonon
  • Patent number: 4980468
    Abstract: 3-7-Diheterabicyclo[3.3.1]nonanes and derivatives thereof are disclosed. Their method of preparation and use as antiarrhythmic agents is given.
    Type: Grant
    Filed: December 11, 1989
    Date of Patent: December 25, 1990
    Assignee: Board of Regents for The Oklahoma Agricultural and Mechanical Colleges Acting for and on Behalf of Oklahoma State University
    Inventors: Kenneth D. Berlin, Mark D. Thompson, Benjamin J. Scherlag, Gary S. Smith
  • Patent number: 4980362
    Abstract: 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: Grant
    Filed: January 30, 1990
    Date of Patent: December 25, 1990
    Assignee: J. Uriach & CIA. S.A.
    Inventors: Elena Carceller, Javier Bartroli'
  • Patent number: 4977271
    Abstract: 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: Grant
    Filed: October 6, 1989
    Date of Patent: December 11, 1990
    Assignee: Virginia Tech Intellectual Properties Inc.
    Inventors: Harry W. Gibson, Yajnanarayana H. R. Jois
  • Patent number: 4973703
    Abstract: 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: Grant
    Filed: November 4, 1988
    Date of Patent: November 27, 1990
    Assignee: Mitsui Petrochemical Industries, Ltd.
    Inventors: Junichi Imuta, Noriaki Kihara, Takeshi Ishitoku
  • Patent number: 4963561
    Abstract: 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: Grant
    Filed: February 28, 1990
    Date of Patent: October 16, 1990
    Assignee: Sterling Drug Inc.
    Inventors: George Y. Lesher, Edward R. Bacon, Baldev Singh, Gee-Hong Kuo
  • Patent number: 4933460
    Abstract: 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: Grant
    Filed: May 13, 1989
    Date of Patent: June 12, 1990
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventor: Joseph T. Strupczewski