Patents Examined by Lenora A. Miltenberger
  • Patent number: 5162364
    Abstract: A compound of formula (I): ##STR1## in which R, R.sub.1 and R.sub.2 are as defined in the description. Medicinal product, which is useful in treating disorders related to a dysfunction of GABA.sub.B receptors.
    Type: Grant
    Filed: June 11, 1991
    Date of Patent: November 10, 1992
    Assignee: Adir et Compagnie
    Inventors: Michel Debaert, Pascal Berthelot, Claude Vaccher
  • Patent number: 5158949
    Abstract: Compounds of formula (I): ##STR1## wherein n is 2 or 3;p is 0, 1 or 2;q is 0, 1 or 2;X is oxygen or S(O).sub.t where t is 0, 1 or 2;each R.sup.1 is independently halo, lower alkyl, lower alkoxy, or trifluoromethyl;each R.sup.2 is independently halo or lower alkyl;R.sup.3 is nitro or --N(R.sup.5)R.sup.6 whereR.sup.5 is hydrogen or lower alkyl;R.sup.6 is hydrogen lower alkyl, lower alkylsulfonyl or --C(Y)R.sup.7 where Y is oxygen or sulfur and R.sup.7 is hydrogen, lower alkyl, lower alkoxy or --N(R.sup.8)R.sup.9 where R.sup.8 is hydrogen or lower alkyl and R.sup.9 is hydrogen, lower alkyl or lower alkoxycarbonyl; orR.sup.5 and R.sup.6 together with N is pyrrolidino, piperidino, morpholino, thiomorpholino or piperazino, wherein the piperazino is optionally substituted at the 4-position by --N(O)R.sup.10 where R.sup.10 is hydrogen, lower alkyl, lower alkoxy or amino; andR.sup.
    Type: Grant
    Filed: December 20, 1990
    Date of Patent: October 27, 1992
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Keith A. Walker, Pamela M. Burton, David C. Swinney
  • Patent number: 5158981
    Abstract: A antiandrogenic compositions comprising an anti-androgenically effective amount of at least one compound of the formula ##STR1## wherein R is alkyl of 1 to 4 carbon atoms, R.sub.1 is alkyl of 1 to 2 carbon atoms, R.sub.2 is selected from the group consisting of hydrogen, alkyl of 1 to 8 carbon atoms optionally interrupted with a heteroatom, alkenyl and alkynyl of 2 to 8 carbon atoms optionally interrupted with a heteroatom, formyl and acyl of an organic carboxylic acid of 2 to 18 carbon atoms, R.sub.3 is selected from the group consisting of hydrogen, alkyl of 1 to 4 carbon atoms and alkenyl and alkynyl of 2 to 4 carbon atoms, R.sub.4 is selected from the group consisting of hydrogen and alkyl of 1 to 4 carbon atoms, the dotted lines indicate optional presence of a double bond between the 4(5) and 5a(6) carbons and the wavy line indicates that R.sub.4 may be in the .alpha.- or .beta.
    Type: Grant
    Filed: March 30, 1990
    Date of Patent: October 27, 1992
    Assignee: Roussel Uclaf
    Inventors: Marie-Madeleine Bouton, Jean Jacques, Andre Pierdet
  • Patent number: 5159083
    Abstract: This invention encompasses compounds of the formula: ##STR1## where X, Y, Z, T, R.sub.1, R.sub.3, R.sub.4, and R.sub.5 are variables representing various organic and inorganic substituents;M is ##STR2## R.sub.2 and R.sub.6 represent hydrogen or alkyl substituents; or R.sub.1 and R.sub.2 together may represent --(CH.sub.2).sub.n1 where n.sub.1 is 1, 2, or 3; orNR.sub.4 R.sub.5 represents substituted or unsubstituted-tetrahydroisoquinolinyl; or ##STR3## where n is 1, 2, or 3; W is N or CH; and R.sub.7 represents hydrogen or aryl; or W--R.sub.7 is oxygen or sulfur.These compounds are highly selective partial agonists or antagonists at brain dopamine receptor subtypes or prodrugs thereof and are useful in the diagnosis and treatment of affective disorders such as schizophrenia and depression as well as certain movement disorders such as Parkinsonism. Futhermore compounds of this invention may be useful in treating the extraparamidyl side effects associated with the use of conventional neuroleptic agents.
    Type: Grant
    Filed: December 28, 1990
    Date of Patent: October 27, 1992
    Assignee: Neurogen Corporation
    Inventors: Andrew Thurkauf, Alan J. Hutchison
  • Patent number: 5158954
    Abstract: 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: Grant
    Filed: October 15, 1990
    Date of Patent: October 27, 1992
    Assignee: Imperial Chemical Industries PLC
    Inventors: John M. Clough, Christopher R. A. Godfrey, Stephen P. Heaney, Kenneth Anderton
  • Patent number: 5157124
    Abstract: Heterocyclic acetylenic amine compounds having the following structural formula ##STR1## having cholinergic agonist or antagonist activity useful in the treatment of mental disorders, extrapyramidal motor disorders, disorders of theparasympathetic nervous system and glaucoma or as analgesics for the treatment of pain. Typical central nervous system disorders for which the subject compounds can be used include cognitive disorders of all ages, including senile dementia, Alzheimer's disease and other related disorders. The compounds are particularly developed to improve mental performance when a mental deficiency is diagnosed.
    Type: Grant
    Filed: March 19, 1992
    Date of Patent: October 20, 1992
    Assignee: The Upjohn Company
    Inventors: Malcolm W. Moon, Richard F. Heier
  • Patent number: 5153214
    Abstract: The present invention is concerned with compounds of formula I ##STR1## wherein A, B, M, R, Ar and Het are as defined in the specification, pharmaceutically acceptable ester and amide derivatives thereof; N-oxides thereof, tetrazole derivatives thereof, and salts thereof. These compounds have valuable pharmacological activities, especially as inhibitors of thromboxane synthetase and as receptor antagonists of thromboxane A.sub.2 and prostaglandin H.sub.2.
    Type: Grant
    Filed: December 26, 1990
    Date of Patent: October 6, 1992
    Assignee: Ciba-Geigy Corporation
    Inventors: Shripad S. Bhagwat, Alan J. Main, Herman R. Rodriguez
  • Patent number: 5151526
    Abstract: The chemical 4-[1-(1-naphthalenyl)ethyl]-1H-imidazole and a method of mak the same.
    Type: Grant
    Filed: August 2, 1991
    Date of Patent: September 29, 1992
    Assignee: The United States of America as represented by the Secretary of the Army
    Inventors: Fu-Lian Hsu, William P. Ashman
  • Patent number: 5151522
    Abstract: The present invention provides a process for preparing polycarboxylic acid imidazolines of the general formula: ##STR1## wherein X is --Cl, --OH, --O--SO.sub.3 H, --O--PO.sub.3 H.sub.2, --O--CH.sub.2 --CH.sub.2 --COOH, --NH.sub.2, --NHalk or --N(alk).sub.2, alk being an alkyl radical containing up to 6 carbon atoms, n is a whole number of from 2 to 4, R is a C.sub.8 -C.sub.18 hydrocarbon radical which is straight-chained, branched, saturated or one to three times unsaturated, m is a whole number of from 2 to 5, R' is a hydrogen atom or a carboxyl group and R" is a hydrogen atom or a methyl radical. In the process, a compound of the formula ##STR2## in which R, X and n are as defined above, is condensed with about a 2- to 5-fold excess of acrylic acid, methacrylic acid, maleic acid or a mixture thereof.
    Type: Grant
    Filed: July 22, 1991
    Date of Patent: September 29, 1992
    Assignees: Chemisches Institut Schaefer AG, Joh. A. Benckiser GmbH
    Inventors: Hans Hitz, Rolf Schaefer, Heinrich Baust, Wolfgang Gross
  • Patent number: 5149359
    Abstract: 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: Grant
    Filed: February 21, 1990
    Date of Patent: September 22, 1992
    Assignee: Agrimont S.p.A.
    Inventors: Giovanni Camaggi, Giovanni Meazza, Ciro Preziuso
  • Patent number: 5149707
    Abstract: The invention relates to 1-[(2-Fluorophenyl)(4-fluorophenyl)phenylmethyl]-1H-imidazole, useful as antifungal agent.
    Type: Grant
    Filed: December 14, 1990
    Date of Patent: September 22, 1992
    Assignee: J. Uriach & Cia, S.A.
    Inventors: Javier Bartroli, Manuel Anquita
  • Patent number: 5145857
    Abstract: HMG-COA reductase-inhibiting compounds of the formula ##STR1## in which X represents a group of the formula --CH.sub.2 --CH.sub.2 -- or --CH.dbd.CH--,R represents a group of the formula ##STR2## R.sup.1 represents optionally substituted aryl, R.sup.2 represents --CH.sub.2 OR.sup.8 or --X--R, andR.sup.5 represents straight-chain or branched alkyl having up to 10 carbon atoms, orand their pharmaceutically acceptable salts.
    Type: Grant
    Filed: August 15, 1990
    Date of Patent: September 8, 1992
    Assignee: Bayer Aktiengesellschaft
    Inventors: Peter Fey, Rolf Angerbauer, Walter Hubsch, Thomas Philipps, Hilmar Bischoff, Dieter Petzinna, Delf Schmidt
  • Patent number: 5145983
    Abstract: A process for the production of N-acylimidazoles by the reaction of a carboxylic anhydride with carbonyl-diimidazole is disclosed. The products are useful as chemical intermediates.
    Type: Grant
    Filed: May 3, 1991
    Date of Patent: September 8, 1992
    Assignee: E. I. Du Pont de Nemours and Company
    Inventor: Michael West
  • Patent number: 5144040
    Abstract: In a process for preparing 2-substituted 1-(acylaminoalkyl)-2-imidazolines of the general formula I ##STR1## where R is an alkylene radical and R.sup.1 is a fatty acid radical, for example a fatty acid and a dialkylenetriamine are reacted with one another in a molar ratio of (1.8 to 2.0):1 by initially introducing one starting material at a temperature T.sub.1 and metering in the second starting material as a liquid, maintaining in the reaction mixture during the addition a temperature T.sub.1 and after the addition until the start of the cyclization a temperature T.sub.2 and distilling off the resulting water or alcohol via a rectification column and, after the acylation product has been formed, cyclizing in a conventional manner, T.sub.1 being a temperature of 170.degree. C. to the boiling point of the initially introduced starting material, but not higher than 250.degree. C., and T.sub.2 being a temperature of 170.degree. to 250.degree. C.
    Type: Grant
    Filed: September 4, 1990
    Date of Patent: September 1, 1992
    Assignee: Cassella Aktiengesellschaft
    Inventors: Georg-Wolfgang Eckhardt, Karl-Heinz Keil, Manfred Schrod
  • Patent number: 5140036
    Abstract: A class of 1,3,5-trisubstituted-1,2,4-triazole compounds is described for use in treatment of circulatory disorders. Compounds of particular interest are angiotensin II antagonists of the formula ##STR1## wherein m is one; wherein R.sup.1 is selected from ethyl, n-propyl, isopropyl, butyl, isobutyl, tert-butyl, 4-methylbutyl, n-pentyl, neopentyl, benzyl, cyclohexyl, cyclohexymethyl, 2-butenyl, 3-butenyl, 2-butynyl, 3-butynyl and 2-hydroxybutyl; wherein R.sup.
    Type: Grant
    Filed: September 19, 1990
    Date of Patent: August 18, 1992
    Assignee: G. D. Searle & Co.
    Inventor: David B. Reitz
  • Patent number: 5137905
    Abstract: Heterocyclic acetylenic amine compounds having the following structural formula ##STR1## having cholinergic agonist or antagonist activity useful in the treatment of mental disorders, extrapyramidal motor disorders, disorders of the parasympathetic nervous system and glaucoma or as analgesics for the treatment of pain. Typical central nervous system disorders for which the subject compounds can be used include cognitive disorders of all ages, including senile dementia, Alzheimer's disease and other related disorders. The compounds are particularly developed to improve mental performance when a mental deficiency is diagnosed.
    Type: Grant
    Filed: April 5, 1991
    Date of Patent: August 11, 1992
    Assignee: The Upjohn Company
    Inventors: Malcolm W. Moon, Richard F. Heier
  • Patent number: 5131947
    Abstract: 4-Ethyl-3-(phenyl)-1-(3-trifluoromethylphenyl)-2-pyrrolidinones and corresponding compounds bearing a p-substituent on the 1-position phenyl group and/or a substituent on the 3-position phenyl group exhibit selective herbicidal activities against various weeds which cause problems in rice or upland fields, even at extremely low application rates. They can be prepared by reductive dehalogenation of a corresponding .alpha.-haloethyl substituted pyrrolidinone or reductive cyclization of a corresponding N-2-butenyl-N-(substituted phenyl)-haloacetyl-3-trifluoromethylaniline.
    Type: Grant
    Filed: March 14, 1990
    Date of Patent: July 21, 1992
    Assignee: Mitsui Toatsu Chemicals Incorporated
    Inventors: Kengo Oda, Koichi Moriyasu, Kiyoshi Arai, Kanji Tomiya, Miura Tohru, Makoto Nishida, Masami Oyamada, Akie Fujiwara
  • Patent number: 5130434
    Abstract: 3-Methylquinoline-8-carboxylic acid I ##STR1## and derivatives thereof are prepared by reacting o-toluidine II or a derivative thereof ##STR2## with methacrolein II ##STR3## in 70-90% strength by weight sulfuric acid in the presence of iodine or of an iodine compound, and oxidizing the resulting 3,8-dimethylquinoline IV or a derivative thereof ##STR4## with nitric acid in a solution containing sulfuric acid, in the presence of vanadium ions, by a process in which, in the sulfuric acid-containing reaction solution of the 3,8-dimethylquinoline IV, the byproducts of the reaction are first decomposed by oxidation, the resulting 3,8-dimethylquinoline solution is concentrated by distillation and the 3,8-dimethylquinoline is then oxidized in situ with nitric acid to give the 3-methylquinoline-carboxylic acid.
    Type: Grant
    Filed: August 23, 1990
    Date of Patent: July 14, 1992
    Assignee: BASF Aktiengesellschaft
    Inventors: Helmut Hagen, Jacques Dupuis, Karlheinz Arbogast
  • Patent number: 5128361
    Abstract: The present invention relates to agents for systemic combating of ectoperasites in host animals, containing a compound of the formul I ##STR1## in which R.sup.1 denotes hydrogen, (C.sub.1 -C.sub.5)-alkyl, (C.sub.1 -C.sub.3)-halogenoalkyl or halogen;R.sup.2 and R.sup.3 independently of one another denote (c.sub.1 -C.sub.5)-alkyl, (C.sub.2 -C.sub.5)-alkenyl, (C.sub.2 -C.sub.5)-alkynyl, (C.sub.3 -C.sub.7)-cycloalkyl, (C.sub.3 -C.sub.7)-cycloalkenyl, (C.sub.1 -C.sub.3)-halogenoalkyl, halogen, cyano, nitro, (C.sub.1 -C.sub.5)-alkoxy, (C.sub.1 -C.sub.3)-alkoxy-C.sub.1 -C.sub.3)-alkyl, (C.sub.1 -C.sub.3)-halogenoalkoxy or (C.sub.1 -C.sub.3)-alkylthio, or R.sup.2 and R.sup.3 together form a polymethylene chain having 2 to 5 carbon atoms:R.sup.4 denotes hydrogen, (c.sub.1 -C.sub.10)-alkyl, (C.sub.2 -C.sub.5)-alkenyl or (C.sub.3 -C.sub.7)-cycloalkyl;R.sup.5 denotes hydrogen, (C.sub.1 -C.sub.10)-alkyl, (C.sub.3 -C.sub.5)-alkenyl, C.sub.3 -C.sub.5)-alkynyl, (C.sub.3 -C.sub.7)- cycloalkyl, (C.sub.3 -C.sub.
    Type: Grant
    Filed: December 18, 1989
    Date of Patent: July 7, 1992
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Herbert Stark, Gerhard Salbeck, Werner Bonin
  • Patent number: 5128356
    Abstract: Novel imidazole derivatives of the formula (I): ##STR1## wherein R.sup.1 is an optionally substituted alkyl group, R.sup.2 and R.sup.3 are independently a group capable of forming an anion or a group which can be changed thereinto, ring A is a benzene ring optionally having, besides the group shown by R.sup.2, further substituents, and X shows linkage of phenylene group and phenyl group directly or through a spacer whose atomic length is not more than 2 and a salt thereof, show antagonistic actions to angiotensin II, thus being useful as therapeutics for cardiovascular diseases.
    Type: Grant
    Filed: October 19, 1990
    Date of Patent: July 7, 1992
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Takehiko Naka, Kohei Nishikawa