Patents Examined by Henry R. Jiles
  • Patent number: 4732898
    Abstract: The present invention are 2-(2-aryl-2-oxo-alkylidene) analogs of 1,2,3,4-tetrahydropyridine-3,5-pyridinecarboxylic acids and particularly esters thereof having valuable calcium antagonist and positive inotropic activity useful in the treatment of cardiovascular disorders, pharmaceutical compositions and methods of use therefor.
    Type: Grant
    Filed: March 3, 1987
    Date of Patent: March 22, 1988
    Assignee: Warner-Lambert Company
    Inventors: Edward W. Badger, Michael D. Taylor
  • Patent number: 4732985
    Abstract: 1,4-Dihydropyridine anti-ischaemic and antihypertensive agent of the formula: ##STR1## or a pharmaceutically acceptable salt thereof, wherein R is 2-chlorophenyl, 2,3-dichlorophenyl or 2-chloro-3-trifluoromethylphenyl;R.sup.1 and R.sup.2 are each independently C.sub.1 -C.sub.4 alkyl;X is O or S;R.sup.3 is H or C.sub.1 -C.sub.4 alkyl; andR.sup.4 is 1,2,4-triazol-1-ylmethyl, imidazol-1-ylmethyl, azidomethyl, 2,4,5-trimethylimidazol-1-ylmethyl, 3,4-dihydro-4-oxopyrimidin-2-ylthiomethyl, pyrimidin-2-ylthiomethyl; pyrimidin-2-ylaminomethyl, 3,4-dihydro-4-oxopyrimidin-2-ylaminomethyl, 2-aminopyrimidin-4-yloxymethyl, methoxymethyl, 2-furyl, 2-pyridylmethyl, imidazol-2-yl, hydroxymethyl, aminomethyl, 1,2,4-triazol-4-ylmethyl or 2-hydroxyethyl, and intermediates leading thereto.
    Type: Grant
    Filed: November 5, 1986
    Date of Patent: March 22, 1988
    Assignee: Pfizer Inc.
    Inventors: David Alker, Simon F. Campbell, Peter E. Cross
  • Patent number: 4732989
    Abstract: The present invention relates to a class of novel substituted alkyl imidazole compounds that are useful as intermediates and as anti-anaerobic agents.
    Type: Grant
    Filed: October 17, 1986
    Date of Patent: March 22, 1988
    Assignee: G. D. Searle & Co.
    Inventors: Peter L. Myers, Chris D. Floyd
  • Patent number: 4732902
    Abstract: The invention relates to long-acting depot producing antipsychotic pyrroloisoquinolinyl-dimethyloxoalkyl alkanoates of the formula ##STR1## wherein R.sub.1 and R.sub.2 independently, are hydrogen, alkyl of 1 to 4 carbon atoms, cycloalkyl or alkenyl, or taken together are alkylene of 3 to 6 carbon atoms; and R.sub.3 is hydrogen, alkyl, hydroxyalkyl, phenylhydroxyalkyl, halophenylhydroxyalkyl, alkylphenylhydroxyalkyl, alkoxyphenylhydroxyalkyl, alkoxyalkyl, aryloxyhydroxyalkyl, alkoxyhydroxyalkyl, acyloxyalkyl, arylcarbonylalkyl, alkoxycarbonylalkyl, aralkyl, alkenyl, alkylcycloalkyl, alkynyl, thienylalkyl, furylalkyl, arylcarboxamidoalkyl, acylalkyl, cyclic-alkyloxoalkyl, cyclic-alkylhydroxyalkyl, alkenyloxyalkyl, aralkenyl, aryloxyalkyl, or aryl-N-imidazolonylalkyl; R.sub.4 is alkyl; and n is the integer 2 or 3,their corresponding optical isomers, geometric isomers, and mixtures thereof, and the pharmaceutically acceptable acid additional salts.The compounds of formula I are useful as antipsychotic agents.
    Type: Grant
    Filed: May 23, 1986
    Date of Patent: March 22, 1988
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Leo Berger, Gary L. Olson
  • Patent number: 4732899
    Abstract: The invention relates to (di)alkoxycarbonylamino-s-triazine derivatives and their sulfureous representatives of formula I ##STR1## wherein R.sub.1 is C.sub.3 -C.sub.6 alkyl or C.sub.3 -C.sub.6 cycloalkyl;R.sub.2 is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 cycloalkyl or the group --C(X)--ZR.sub.3 ;R.sub.3 is C.sub.1 -C.sub.6 haloalkyl, C.sub.2 -C.sub.4 alkenyl or C.sub.2 -C.sub.4 haloalkenyl;X is oxygen or sulfur; andZ is oxygen or sulfur;and to the acid addition salts thereof. The invention also relates to the preparation of said compounds from the diamino-s-triazines on which they are based and to the use thereof against pests which are pathogens of domestic animals and cultivated plants.
    Type: Grant
    Filed: November 24, 1986
    Date of Patent: March 22, 1988
    Assignee: Ciba-Geigy Corporation
    Inventors: Jean-Claude Gehret, Odd Kristiansen
  • Patent number: 4732908
    Abstract: The use in pest control of 2-(1-indolinylmethyl)-imidazolines of the formula I ##STR1## or salts thereof, wherein R.sub.1 is hydrogen or C.sub.1 -C.sub.12 -alkyl,R.sub.2 and R.sub.2a independently of one another are each hydrogen or C.sub.1 -C.sub.4 -alkyl, or together are C.sub.2 -C.sub.4 -alkylene, andR.sub.3 and R.sub.4 independently of one another are each hydrogen, halogen or C.sub.1 -C.sub.3 -alkoxy, or C.sub.1 -C.sub.4 -alkyl which is unsubstituted or substituted by halogen.There are also described the compounds of the formula Ia ##STR2## wherein R.sub.1 ' is hydrogen or C.sub.1 -C.sub.12 -alkyl,R.sub.2 ' and R.sub.2a ' independently of one another are each hydrogen or C.sub.1 -C.sub.4 -alkyl, or together are C.sub.2 -C.sub.4 -alkylene,R.sub.3 ' is hydrogen, halogen or C.sub.1 -C.sub.3 -alkoxy, or C.sub.1 -C.sub.4 -alkyl which is unsubstituted or substituted by halogen, andR.sub.4 ' is halogen or C.sub.1 -C.sub.3 -alkoxy, or C.sub.1 -C.sub.4 -alkyl which is unsubstituted or substituted by halogen, orR.
    Type: Grant
    Filed: March 9, 1987
    Date of Patent: March 22, 1988
    Assignee: Ciba-Geigy Corporation
    Inventor: Urs Burckhardt
  • Patent number: 4731449
    Abstract: TCNQ complexes with organic pyridinium ions, which may be kept in a molten condition for a relatively long time without the electrical conductivity thereof being substantially reduced after cooling.
    Type: Grant
    Filed: March 3, 1986
    Date of Patent: March 15, 1988
    Assignee: Bayer Aktiengesellschaft
    Inventors: Friedrich Jonas, Jurgen Hocker
  • Patent number: 4731358
    Abstract: New substituted .beta.-carbolines of formula I ##STR1## wherein R.sup.3 is hydrogen or a non-carboxyl based substituent, and R.sup.4-9 have various meanings,are valuable pharmaceutical products with long lasting action on the central nervous system.
    Type: Grant
    Filed: September 2, 1986
    Date of Patent: March 15, 1988
    Assignee: Schering Aktiengesellschaft
    Inventors: Andreas Huth, Dieter Rahtz, Dieter Seidelmann, Helmut Schmiechen, Helmut Biere, Claus T. Braestrup
  • Patent number: 4731370
    Abstract: This invention relates to a novel 1,4-dihydropyridine derivative of the formula ##STR1## wherein R2 is pyridyl, or a salt thereof. These compounds have a vasodilating activity and a platelet aggregation inhibiting activity. Also disclosed are pharmaceutical compositions containing the same.
    Type: Grant
    Filed: June 10, 1986
    Date of Patent: March 15, 1988
    Assignee: Toyama Chemical Co., Ltd.
    Inventors: Isao Watanabe, Kaishu Momonoi, Toru Hiraiwa, Satoshi Ono, Joji Nakano, Katsuyuki Nagumo, Hiroyasu Takagi
  • Patent number: 4731373
    Abstract: Glycerine derivatives of the formula ##STR1## wherein the residues R.sup.1, R.sup.2 and R.sup.3 have the significance given in the description,and their hydrates, which inhibit blood platelet activating factor (PAF), are descried.
    Type: Grant
    Filed: December 10, 1984
    Date of Patent: March 15, 1988
    Assignee: Hoffman-La Roche Inc.
    Inventors: Richard Barner, Kasper Burri, Jean-Marie Cassal, Paul Hadvary, Georges Hirth, Klaus Muller
  • Patent number: 4731450
    Abstract: A process for the perfluoroalkylation of aromatic derivatives. In a first stage, an aromatic derivative, sulfur dioxide and a metal selected from the group consisting of zinc, aluminum, manganese, cadmium, magnesium, tin, iron, nickel and cobalt, are brought into contact in a solvent, preferably a polar aprotic solvent. In a second stage, a perfluoroalkyl bromide or iodide is added to react with the aromatic derivative.
    Type: Grant
    Filed: May 21, 1986
    Date of Patent: March 15, 1988
    Assignee: Rhone-Poulenc Specialites Chimiques
    Inventors: Claude Wakselman, Marc Tordeux
  • Patent number: 4731090
    Abstract: A process for protecting keratinous material with the aid of substantially novel pyridyloxytrifluoromethanesulfonanilides from pests that feed on keratin, said pyridyloxytrifluoromethanesulfonanilides having the formula ##STR1## wherein R.sub.1 and R.sub.2, each independently of the other, are halogen, haloalkyl, alkyl, nitro, cyano, alkoxy or haloalkoxy or alkoxycarbonyl, andn and m, each independently of the other, are 0 or a value from 1 to 3, with the proviso that if n or m>1, the substituents R.sub.1 and R.sub.2 may be identical or different, and that at least one substituent selected from the group consisting of halogen, haloalkyl and haloalkoxy is present in the molecule.The preparation of these compounds and the use thereof as active ingredients of compositions providing a mothproof and beetle-resistant finish are also described herein.
    Type: Grant
    Filed: December 12, 1984
    Date of Patent: March 15, 1988
    Assignee: Ciba-Geigy Corporation
    Inventors: Manfred Boger, Bernardo de Sous, Dieter Reinehr, Werner Schmid, Hermann Rempfler, Hans Tobler
  • Patent number: 4730049
    Abstract: An improved process for the preparation of 5-(2-chlorobenzyl)-4,5,6,7-tetrahydrothieno[3,2-c]pyridine and acid addition salts thereof, which are useful as a medicine. This process comprises effecting reaction between 4,5,6,7-tetrahydrothieno[3,2-c]pyridine and 2-chlorobenzyl halide in the presence of a phase transfer catalyst.
    Type: Grant
    Filed: October 1, 1985
    Date of Patent: March 8, 1988
    Assignees: Nisshin Flour Milling Co., Ltd., Nisshin Chemicals Co., Ltd.
    Inventor: Toshio Suguro
  • Patent number: 4729781
    Abstract: Disclosed are herbicidal compounds of the general formula I: ##STR1## wherein A is O-alkylene of 1 to 5 carbon atoms, O-alkenylene of 3 to 6 carbon atoms in which the unsaturation is non-adjacent the oxygen atom thereof or NH-alkylene in which the alkylene is of 1 to 5 carbon atoms, and --COZR is an acid function or forms certain ester or thioester functions, and the mono- and di-salt forms thereof.
    Type: Grant
    Filed: August 4, 1986
    Date of Patent: March 8, 1988
    Assignee: Sandoz Ltd.
    Inventor: John W. Williams
  • Patent number: 4729843
    Abstract: The present invention provides a new collector for use in the froth flotation of metal values from their ores. The collector comprises a synergistic mixture of alkyl xanthogen alkyl formates and dialkyl thionocarbamates, and yields metal recoveries superior to that achieved with either collector alone. According to the present invention the novel collector for use in froth flotation comprises a mixture of alkyl xanthogen alkyl formates having the general formula: ##STR1## wherein R is a branched or straight chain alkyl substituent having 1 to 6 carbon atoms, and R' is selected from the class consisting of ethyl and methyl; anddialkyl thionocarbamates having the general formula: ##STR2## wherein Y is a branched or straight chain alkyl substituent having 1 to 6 carbon atoms, and Y' is selected from the class consisting of ethyl and methyl.
    Type: Grant
    Filed: March 4, 1986
    Date of Patent: March 8, 1988
    Assignee: Essex Industrial Chemicals, Inc.
    Inventor: Kim N. Unger
  • Patent number: 4728746
    Abstract: .beta.-Aminothiol ester having the general formula (I): ##STR1## which is useful as an intermediate in the preparation of carbapenen beta-lactam antiobiotics, wherein R.sup.1 is alkyl or aryl and R.sup.2 and R.sup.3 are protective groups. The .beta.-Aminothiol ester of formula (I) is prepared by reacting a .beta.-hydroxythiol ester having the general formula (III): ##STR2## wherein R.sup.1 is as above, with a boron compound having the general formula (IV): ##STR3## wherein each of R and R' is alkyl or cycloalkyl, or R and R' taken together, form a ring including the boron atom in the presence of a tertiary amine, the obtained reaction mixture being reacted with an imine having the general formula (V): ##STR4## Wherein R.sup.2 and R.sup.3 are protective groups, followed by treating the resultant product with hydrogen peroxide.
    Type: Grant
    Filed: November 4, 1985
    Date of Patent: March 1, 1988
    Assignee: Sagami Chemical Research Center
    Inventors: Masakatsu Shibasaki, Takamasa Iimori
  • Patent number: 4728652
    Abstract: 1,4-Dihydropyrimidines of the formula ##STR1## wherein X is sulfur or oxygen and R.sub.4 is aryl or heterocyclo and disclosed. These compounds are useful as cardiovacular agents, particularly anti-hypertensive agents, due to their vasodilator activity.
    Type: Grant
    Filed: April 21, 1986
    Date of Patent: March 1, 1988
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Karnail Atwal
  • Patent number: 4728645
    Abstract: Disclosed are compounds of formula I ##STR1## wherein R.sub.1 represents hydrogen, lower alkyl, substituted lower alkyl, nitro, halogen, free, etherified or esterified hydroxy, free, etherified, oxidized etherified or esterified mercapto, unsubstituted, mono- or disubstituted amino, ammonio, free or functionally modified sulfo, free or functionally modified formyl, C.sub.2 -C.sub.20 -acyl, cyano, free or functionally modified carboxy; and R.sub.2 represents hydrogen, lower alkyl, substituted lower alkyl, halogen; free, etherified or esterified hydroxy; free, etherified, oxidized etherified or esterified mercapto; free or functionally modified carboxy, or acyl; the 7,8-dihydro derivatives thereof; and compounds of the formula I* ##STR2## wherein n denotes 0, 1, 2, 3 or 4, and R.sub.1 and R.sub.2 are as defined above under formula I and salts thereof; e.g. as aromatase inhibitors; pharmaceutical compositions containing these compounds; the use of these compounds for the treatment of conditions responsive to e.
    Type: Grant
    Filed: February 4, 1986
    Date of Patent: March 1, 1988
    Assignee: Ciba-Geigy Corporation
    Inventor: Leslie J. Browne
  • Patent number: 4728735
    Abstract: Compounds of the Formula I: ##STR1## are inhibitors of the mammalian 5-lipoxygenase enzyme system of the arachidonic acid cascade. As such, these compounds are useful therapeutic agents for treating allergic conditions, asthma, cardiovascular disorders and inflammation and are useful as cytoprotective agents.
    Type: Grant
    Filed: November 10, 1986
    Date of Patent: March 1, 1988
    Assignee: Merck & Co., Inc.
    Inventors: Patrice C. Belanger, Joshua Rokach, John Scheigetz
  • Patent number: 4728666
    Abstract: Heterocyclic acetylenes of the formula (I): ##STR1## wherein Y and R.sup.1 are substituents such as hydrogen, alkyl, alkoxy, chloro or fluoro, m is 0-2, R.sup.2 is branched alkyl and Het is an aromatic heterocycle. The acetylenes are useful in treating hypertension and/or angina.
    Type: Grant
    Filed: November 24, 1986
    Date of Patent: March 1, 1988
    Assignee: McNeilab, Inc.
    Inventor: John R. Carson