Bicyclo Ring System Patents (Class 514/657)
  • Patent number: 4906662
    Abstract: Disclosed are phenol derivatives of the formula ##STR1## wherein R.sup.1 is a substituted phenyl group, R.sup.2 and R.sup.3 are C.sub.1 -C.sub.6 alkyl group and of the formula ##STR2## wherein R.sup.8, R.sup.9 and R.sup.10 are C.sub.1 -C.sub.6 alkyl and the like and A is H, C.sub.1 -C.sub.6 alkylsulfonyl and the like substituents. These compounds and some related compounds have anti-inflammatory activity and lipoxygenase inhibitory activity.
    Type: Grant
    Filed: January 27, 1987
    Date of Patent: March 6, 1990
    Assignee: Otsuka Pharmaceutical Factory, Inc.
    Inventors: Kinji Hashimoto, Kiyoto Goto, Ken-ichi Kanai, Yoshiaki Tsuda
  • Patent number: 4888354
    Abstract: The invention is directed to compositions for topical application made up of active pharmaceutical permeants capable of existing in both free base and acid addition salt form. The permeants are present as a combination of both free base and acid addition salt forms. These combined forms provide skin penetration rates which are greater than the penetration rate of either the free base or acid addition salt forms utilized separately. The combined free base-acid addition salt permeants are formulated in a carrier vehicle which preferably also possesses skin penetration enhancement activity.
    Type: Grant
    Filed: December 21, 1987
    Date of Patent: December 19, 1989
    Assignee: Theratech, Inc.
    Inventors: Yunik Chang, Dinesh C. Patel
  • Patent number: 4882352
    Abstract: This invention provides a method for treating the symptoms of schizophrenia which comprises administering to a schizophrenic an effective amount of a compound selected from the group consisting of optically-active or racemic compounds represented by the general formula: ##STR1## wherein R.sub.1 is selected from the group consisting of organic radicals having fused rings, phenyl, pyridyl ##STR2## X is oxygen or sulfur, Y, if present, is selected from the group consisting of hydroxy, nitro, cyano, azido, amino, acylamino, carboxyamido, trifluoromethyl, sulfate, sulfonamido halogen, hydrocarbyl and hetero atom-substituted hydrocarbyl radicals, wherein said heteroatoms are selected from the group consisting of halogen, nitrogen, oxygen, sulfur and phosphorus and said hydrocarbyl radicals comprise from 1 to 12 carbon atoms, and a is an integer between zero and 3. R.sub.2, R.sub.3 and R.sub.
    Type: Grant
    Filed: May 8, 1987
    Date of Patent: November 21, 1989
    Assignee: Nelson Research & Development Co.
    Inventor: Alan S. Horn
  • Patent number: 4882339
    Abstract: Disclosed are compounds of the formula ##STR1## wherein R.sub.1 represents unsubstituted or lower alkyl-substituted C.sub.3 -C.sub.7 -cycloalkyl, unsubstituted or lower alkyl substituted C.sub.7 -or C.sub.8 -bicycloalkyl, unsubstituted or lower alkyl-substituted adamantyl, 4-piperidinyl or N-lower alkyl or aryl-lower alkyl-substituted piperidinyl, 1- or 2-indanyl, 1- or 2-tetrahydronaphthyl, 1- or 2-perhydroindanyl, 1- or 2-perhydronaphthyl; R.sub.2 represents hydrogen, lower alkyl, C.sub.3 -C.sub.7 -cycloalkyl, aryl-lower alkyl, C.sub.3 -C.sub.7 -cycloalkyl-lower alkyl, lower alkanoyl or aryl-lower alkanoyl; or R.sub.1 and R.sub.2 combined with the nitrogen to which they are attached represent pyrrolidino, piperidino, perhydroazepino, morpholino, thiomorpholino, tetrahydro- or perhydro-(isoquinolinyl or quinolinyl), dihydro- or perhydroindolyl, piperazino or N-lower alkyl-piperazino; R.sub.
    Type: Grant
    Filed: July 10, 1987
    Date of Patent: November 21, 1989
    Assignee: Ciba-Geigy Corporation
    Inventor: Jan W. F. Wasley
  • Patent number: 4880802
    Abstract: For treatment of disorders of the central nervous system, the cardiovascular system or the intestinal tract, the new substituted basic 2-aminotetralins of the formula ##STR1## in which R.sup.1 represents hydrogen or alkyl,R.sup.2 represents hydrogen, alkyl or acyl, andR.sup.3 represents quinuclidine or a group of the formula --(CH.sub.2).sub.a --R.sup.4, --CH.sub.2 --CH.dbd.CH--(CH.sub.2).sub.b --R.sup.4, --CH.sub.2 --C.tbd.(CH.sub.2).sub.b --R.sup.4, ##STR2## wherein a denotes a number from 1 to 10,b denotes a number 0, 1, 2, 3 or 4,d denotes a number 2 or 3, andX denotes oxygen, sulphur, or NR.sup.5,and their salts.
    Type: Grant
    Filed: December 8, 1987
    Date of Patent: November 14, 1989
    Assignee: Bayer Aktiengesellschaft
    Inventors: Rudolf Schohe, Thomas Glaser, Jorg Traber, George S. Allen
  • Patent number: 4876284
    Abstract: Compounds of the formula ##STR1## wherein R.sup.3 and the NR.sup.1 R.sup.2 group are in a cis-position to each other and wherein Y is OH, R.sup.4 COO, (R.sup.5).sub.2 NCOO or R.sup.6 O either in position 5 or position 7, whereby R.sup.4 is an alkyl group having 1-5 carbon atoms or a possibly substituted phenyl group, R.sup.5 is an alkyl group having 1-5 carbon atoms and R.sup.6 is an allyl or benzyl group, R.sup.1 is hydrogen or an alkyl group having 1-3 carbon atoms, R.sup.2 is an alkyl group having 1-6 carbon atoms, a phenylalkyl- or m-hydroxyphenylalkyl group with 2-4 carbon atoms in the alkyl part, or an alkenyl group with 3-6 carbon atoms other than 1-alkenyl, and R.sup.3 is an alkyl group having 1-3 carbon atoms, processes and intermediates for their preparation, pharmaceutical preparations and methods of treatment employing such compounds. The compounds are useful for therapeutic purposes, especially for treatment of disorders in the central nervous system.
    Type: Grant
    Filed: January 11, 1988
    Date of Patent: October 24, 1989
    Assignee: Per Arvid Emil Carlsson
    Inventors: Folke L. E. Arvidsson, Per A. E. Carlsson, Uli A. Hacksell, John S. M. Hjorth, Anette M. Johansson, Per L. Lindberg
  • Patent number: 4873262
    Abstract: New 8-substituted 2-aminotetralins can be prepared from the corresponding aminotetralins or tetralones. They can be used in medicaments.
    Type: Grant
    Filed: December 15, 1987
    Date of Patent: October 10, 1989
    Assignee: Bayer Aktiengesellschaft
    Inventors: Bodo Junge, Bernd Richter, Thomas Glaser, Jorg Traber, George S. Allen
  • Patent number: 4853402
    Abstract: By using .alpha.-mimetics, particularly compounds of general formulae I to III and the compounds listed in Table I, as feed additives in fattening animals, it has surprisingly been possible to improve the daily weight gain, the utilisation of fodder and the ratio of muscle to fat in favor of the proportion of muscle and protein.
    Type: Grant
    Filed: February 26, 1987
    Date of Patent: August 1, 1989
    Assignee: Boehringer Ingelheim Vetmedica GmbH
    Inventors: Werner Bomann, Franz Esser, Ulrich Hamel, Helmut Stable
  • Patent number: 4847302
    Abstract: A method is described in which the feed utilization by livestock is improved by the incorporation in the feed or drinking water of the said livestock of certain compounds, with resultant increase in body weight, decrease in body fat and increase in body protein for the same food intake.
    Type: Grant
    Filed: April 4, 1988
    Date of Patent: July 11, 1989
    Assignee: Merck & Co., Inc.
    Inventor: Larry A. Muir
  • Patent number: 4829089
    Abstract: This disclosure describes certain substituted piperazine-1,4-naphthalenediones useful as anti-asthmatic agents.
    Type: Grant
    Filed: July 22, 1988
    Date of Patent: May 9, 1989
    Assignee: American Cyanamid Company
    Inventors: Jeffrey B. Medwid, Lawrence W. Torley, Andrew S. Tomcufcik
  • Patent number: 4826879
    Abstract: An ocular antihypertensive composition for topical use which contains an effective amount of a compound represented by the formula ##STR1## or a salt thereof having, in low concentrations, intraocular pressure lowering activity in mammals, low toxicity and no influence on the pupil size and, therefore, is useful as a therapeutic agent for glaucoma, for instance.Furthermore, since the compound is effective in low concentrations, the possibility of tolerance development is considered to be scarce.
    Type: Grant
    Filed: January 14, 1987
    Date of Patent: May 2, 1989
    Assignee: Senju Pharmaceutical Co., Ltd.
    Inventors: Yujiro Yamamoto, Takahiro Ogawa, Yoshikazu Kuribayashi
  • Patent number: 4804406
    Abstract: Fungicidally active novel .beta.-naphthylalkylamines of the formula ##STR1## in which Ar represents optionally substituted .beta.-naphthyl andR.sup.1 and R.sup.2, which can be identical or different, represent alkyl or alkenyl orR.sup.1 and R.sup.2, together with the nitrogen atom to which they are bonded, represent an optionally substituted saturated heterocyclic radical, which can contain further hetero-atoms,or plant-tolerated acid addition salts thereof.
    Type: Grant
    Filed: September 3, 1987
    Date of Patent: February 14, 1989
    Assignee: Bayer Aktiengesellschaft
    Inventors: Joachim Weissmuller, Wilhelm Brandes, Gerd Hanssler, Paul Reinecke
  • Patent number: 4791139
    Abstract: A compound of formula: ##STR1## wherein W represents one or more substituents selected from halo, alkyl, alkoxy, alkoxyalkyl, haloalkyl and haloalkoxy or W represents a bidentate group linking adjacent carbon atoms selected from alkylene and alkylenedioxy; Y is a group of formula ##STR2## wherein X is a group of formula --(CF.sub.2).sub.n R.sup.3, where R.sup.3 is selected from hydrogen, chloro and fluoro, and n is one or two, R.sup.1 is selected from hydrogen, chloro, fluoro and hydroxy and R.sup.2 is selected from methyl, cyano, ethynyl and hydrogen; Q is selected from carbon bearing a hydrogen atom and nitrogen; and Z represents one or more substituents selected from fluoro, benzyl, phenoxy, chlorophenoxy, fluorophenoxy and bromophenoxy, or any isomer thereof. Processes for preparing these compounds and intermediates for use therein, insecticidal compositions containing these compounds and the use thereof are also disclosed.
    Type: Grant
    Filed: February 25, 1987
    Date of Patent: December 13, 1988
    Assignee: Imperial Chemical Industries PLC
    Inventors: Michael J. Bushell, Robin A. E. Carr
  • Patent number: 4791123
    Abstract: There are provided new alkane and alkoxyalkane derivatives of the general formula I ##STR1## in which R.sub.1, R.sub.2, R.sub.3, R.sub.4 and A have the meanings given in the description, processes for their preparation and insecticidal and acaricidal compositions containing these compounds.
    Type: Grant
    Filed: January 22, 1987
    Date of Patent: December 13, 1988
    Assignee: Schering Akt.
    Inventors: Helga Franke, Heinrich Franke, Hans-Rudolf Kruger, Hartmut Joppien, Dietrich Baumert, David Giles
  • Patent number: 4782059
    Abstract: Certain fungistats when employed in combination have been found to exhibit synergistic antifungal properties and further exhibit fungicidal properties.
    Type: Grant
    Filed: September 29, 1986
    Date of Patent: November 1, 1988
    Assignee: Merck & Co., Inc.
    Inventors: Hans H. Gadebusch, Mary E. Valiant
  • Patent number: 4764534
    Abstract: 4-Substituted-N-[2,4-dinitro-6-(trifluoromethyl)phenyl]-1-naphthalenamine derivatives, useful as anticoccidial agents both alone and in combination with polyether antibiotics.
    Type: Grant
    Filed: July 17, 1984
    Date of Patent: August 16, 1988
    Assignee: Eli Lilly and Company
    Inventors: Albert J. Clinton, deceased, George O. P. O'Doherty
  • Patent number: 4761421
    Abstract: A method is described in which the feed utilization by livestock is improved by the incorporation in the feed or drinking water of the said livestock of certain compounds, with resultant increase in body weight, decrease in body fat and increase in body protein for the same food intake.
    Type: Grant
    Filed: September 18, 1986
    Date of Patent: August 2, 1988
    Assignee: Merck & Co., Inc.
    Inventor: Larry A. Muir
  • Patent number: 4758561
    Abstract: The present invention to pharmaceutical composition comprising an effective amount of products having the structural formula ##STR1## where R.sub.1 is a hydrogen atom or a lower alkyl group such as methyl or ethyl,R.sub.2 is a straight or branched cyclopropylmethyl, 2-furyl methyl, benzyl, phenyl or lower alkyl group from C.sub.1 to C.sub.4 such as methyl, ethyl, propyl, isopropyl, butyl, isobutyl, tertiary butyl; the NR.sub.1 R.sub.2 group can also represent a nitrogenous heterocyclic compound N(CH.sub.2).sub.n in which n can be any value between 4 and 6.The products are useful in human and veterinary therapy because of their anti-inflammatory, diuretic, bronchodilating, anticholinergic, antispasmodic and antidepressant properties.
    Type: Grant
    Filed: July 22, 1985
    Date of Patent: July 19, 1988
    Assignee: Societe Cortial, S.A.
    Inventors: Guillaume Le Baut, Louis Sparfel, Marie-Helene Creuzet, Claude Feniou, Henri Pontagnier, Gisele Prat
  • Patent number: 4757067
    Abstract: The present invention to pharmaceutical composition comprising an effective amount of products having the structural formula ##STR1## where R.sub.1 is a hydrogen atom or a lower alkyl group such as methyl or ethyl,R.sub.2 is a straight or branched cyclopropylmethyl, 2-furyl methyl, benzyl, phenyl or lower alkyl group from C.sub.1 to C.sub.4 such as methyl, ethyl, propyl, isopropyl, butyl, isobutyl, tertiary butyl; the NR.sub.1 R.sub.2 group can also represent a nitrogenous heterocyclic compound N(CH.sub.2).sub.n in which n can be any value between 4 and 6.The products are useful in human and veterinary therapy because of their anti-inflammatory, diuretic, bronchodilating, anticholinergic, antispasmodic and antidepressant properties.
    Type: Grant
    Filed: January 21, 1987
    Date of Patent: July 12, 1988
    Assignee: Societe Cortial, S.A.
    Inventors: Guillaume Le Baut, Louis Sparfel, Marie-Helene Creuzet, Claude Feniou, Henri Pontagnier, Gisele Prat
  • Patent number: 4735969
    Abstract: A novel bisulfite adduct of menadione, the menadione choline bisulfite adduct, a process for its preparation, and its use as an antihemorrhagic agent.
    Type: Grant
    Filed: November 18, 1985
    Date of Patent: April 5, 1988
    Assignee: BASF Aktiengesellschaft
    Inventors: Joachim U. Schneider, Hans Kiefer
  • Patent number: 4684661
    Abstract: The invention relates to novel homopropargylamines of formula I ##STR1## wherein n is 2 or 3,R.sub.1 is a group of formula IIa, IIb or IIc ##STR2## in which R.sub.6 and R.sub.7 independently are H, halogen, CF.sub.3, lower alkyl or lower alkoxy,s is a number of 3 to 5,X is O, S, OCH.sub.2, SCH.sub.2, CH.sub.2 or NR.sub.8, andR.sub.8 is H or lower alkyl,R.sub.2 is H or lower alkyl, eitherR.sub.3 and R.sub.4, independently, are H or lower alkyl, orR.sub.3 and R.sub.4 together are (CH.sub.2).sub.u, in which u is a number of 3 to 5, andR.sub.5 is H, alkenyl or is a group selected from alkyl, trialkylsilyl, dialkylphenylsilyl, phenyl, phenylalkyl and cycloalkyl, in which alkyl, phenyl and cycloalkyl groups or moieties are unsubstituted or substituted by OH, lower alkyl, lower alkoxy, phenyl or halogen,in free base form or acid addition salt form thereof, their preparation, their chemotherapeutical and agricultural use and to compositions comprising such novel compounds and suitable for such use.
    Type: Grant
    Filed: November 20, 1985
    Date of Patent: August 4, 1987
    Assignee: Sandoz Ltd.
    Inventor: Anton Stuetz
  • Patent number: 4656192
    Abstract: New tropolone derivatives of the general formula: ##STR1## wherein R.sup.1 represents H or an alkyl group, R.sup.2 represents an alkyl, aryl, aralkyl or heterocyclic group and R.sup.3 represents an alkoxyl, aryl or heterocyclic group or a group of the formula: ##STR2## or R.sup.2 and R.sup.3 may form together a part of a heterocyclic group, their metal complex salts, processes for the preparation thereof and the use thereof as anti-tumor agents.
    Type: Grant
    Filed: June 14, 1984
    Date of Patent: April 7, 1987
    Assignee: Mect Corporation
    Inventor: Masatoshi Yamato
  • Patent number: 4628062
    Abstract: New compounds of the formula ##STR1## in which R.sub.1 is an allylamino, acetylamino or propionylamino radical,R.sub.2 is hydrogen or a 2-methoxyethoxy or ethoxy radical,R.sub.3 is hydrogen or a sulphamoyl radical, andR.sub.4 is hydrogen,and of the formula ##STR2## in which R.sub.1 is a halogen atom or a free or substituted hydroxyl, sulphhydryl or amino group,R.sub.2 is a hydrogen atom, an alkyl radical, a halogen atom, or a free or substituted hydroxyl, sulphhydryl or amino group,R.sub.3 and R.sub.4 each independently is hydrogen, alkyl, hydroxyl, alkoxy, sulphonamido or halogen, with the proviso that R.sub.2, R.sub.3 and R.sub.4 are hydrogen when R.sub.1 is hydroxyl,exhibit anti-inflammatory activity.
    Type: Grant
    Filed: December 17, 1984
    Date of Patent: December 9, 1986
    Assignee: Troponwerke GmbH & Co., KG
    Inventors: Wolfgang Opitz, Bernhard Pelster, Romanis Fruchtmann, Udo Krupka, Walter Gauss, Hartmut Kiehne, Hermann Oediger
  • Patent number: 4600708
    Abstract: Therapeutic liquid oral dosage formulations of propranolol hydrochloride are provided which contain lecithin and/or a basic amino acid to impart taste masking characteristics and/or contain a basic amino acid to impart anesthesia masking characteristics.
    Type: Grant
    Filed: July 19, 1985
    Date of Patent: July 15, 1986
    Assignee: American Home Products Corporation
    Inventors: Gerald L. Reuter, Mark E. Coons
  • Patent number: 4551479
    Abstract: The present invention relates to the use of a compound of the general formula I ##STR1## wherein R.sub.1 and R.sub.2 represent hydrogen or a lower alkyl group (1-4 C), preferably methyl, ethyl, propyl or isopropyl, the broken line indicates an optional extra bond, and X and Y represent hydrogen, alkyl (1-4 C) or halogen (preferably fluorine), or a pharmaceutically acceptable acid addition salt thereof, for its anti-convulsive property.
    Type: Grant
    Filed: March 22, 1984
    Date of Patent: November 5, 1985
    Assignee: Akzo N.V.
    Inventors: David S. Savage, James Redpath
  • Patent number: 4508732
    Abstract: Basic ethers of the formula ##STR1## wherein Z is CH.sub.3 -NR.sup.2 -CH.sub.2 CH.sub.2 -CHR.sup.1 --, (1-R.sup.2 -3-piperidyl)-CHR.sup.3 --, (1-R.sup.2 -2-piperidyl)-CH.sub.2 -CHR.sup.3 -- or 1-R.sup.2 -3-R.sup.4 -- hexahydroazepinyl; R.sup.1 is cyclopropyl or Ar; R.sup.2 is H, alkyl of 1-4 C atoms, alkenyl of 2-4 C atoms, cycloalkylalkyl of 4-8 C atoms or benzyl; R.sup.3 is H or Ar; R.sup.4 is H or alkyl of 1-4 C atoms, Y is --O-CHQ.sup.1 -CHQ.sup.2 -CH.sub.2 --, --O-CHQ.sup.1 -CHQ.sup.2 -CO--, --O-CQ.sup.1 .dbd.CQ.sup.2 -CO-- or --CH.sub.2 -CHQ.sup.1 -CHQ.sup.2 -CO--; Q.sup.1 and Q.sup.2 are independently each H, alkyl of 1-4 C atoms, cycloalkyl or alkylcycloalkyl each of 3-6 total C atoms or Ar; and Ar is phenyl or phenyl substituted by F, Cl, alkoxy or alkylthio, each of 1-4 C atoms, methylenedioxy or CF.sub.3 ; with the proviso that when Z is (CH.sub.3).sub.2 N-CH.sub.2 CH.sub.2 -CHR.sup.1 in 7-position and Y is --O-C(C.sub.6 H.sub.5).dbd.CH-CO-- or --O-C(C.sub.6 H.sub.5).dbd.C(CH.sub.3)-CO--, R.sup.
    Type: Grant
    Filed: January 21, 1983
    Date of Patent: April 2, 1985
    Assignee: Merck Patent Gesellschaft mit beschrankter Haftung
    Inventors: Hans-Heinrich Hausberg, Helmut Prucher, Jurgen Uhl, Christoph Seyfried, Klaus Minck