Bicyclo Ring System Patents (Class 514/657)
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Patent number: 4906662Abstract: 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: GrantFiled: January 27, 1987Date of Patent: March 6, 1990Assignee: Otsuka Pharmaceutical Factory, Inc.Inventors: Kinji Hashimoto, Kiyoto Goto, Ken-ichi Kanai, Yoshiaki Tsuda
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Patent number: 4888354Abstract: 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: GrantFiled: December 21, 1987Date of Patent: December 19, 1989Assignee: Theratech, Inc.Inventors: Yunik Chang, Dinesh C. Patel
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Patent number: 4882352Abstract: 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: GrantFiled: May 8, 1987Date of Patent: November 21, 1989Assignee: Nelson Research & Development Co.Inventor: Alan S. Horn
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Patent number: 4882339Abstract: 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: GrantFiled: July 10, 1987Date of Patent: November 21, 1989Assignee: Ciba-Geigy CorporationInventor: Jan W. F. Wasley
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Patent number: 4880802Abstract: 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: GrantFiled: December 8, 1987Date of Patent: November 14, 1989Assignee: Bayer AktiengesellschaftInventors: Rudolf Schohe, Thomas Glaser, Jorg Traber, George S. Allen
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Patent number: 4876284Abstract: 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: GrantFiled: January 11, 1988Date of Patent: October 24, 1989Assignee: Per Arvid Emil CarlssonInventors: Folke L. E. Arvidsson, Per A. E. Carlsson, Uli A. Hacksell, John S. M. Hjorth, Anette M. Johansson, Per L. Lindberg
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Patent number: 4873262Abstract: New 8-substituted 2-aminotetralins can be prepared from the corresponding aminotetralins or tetralones. They can be used in medicaments.Type: GrantFiled: December 15, 1987Date of Patent: October 10, 1989Assignee: Bayer AktiengesellschaftInventors: Bodo Junge, Bernd Richter, Thomas Glaser, Jorg Traber, George S. Allen
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Patent number: 4853402Abstract: 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: GrantFiled: February 26, 1987Date of Patent: August 1, 1989Assignee: Boehringer Ingelheim Vetmedica GmbHInventors: Werner Bomann, Franz Esser, Ulrich Hamel, Helmut Stable
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Patent number: 4847302Abstract: 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: GrantFiled: April 4, 1988Date of Patent: July 11, 1989Assignee: Merck & Co., Inc.Inventor: Larry A. Muir
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Patent number: 4829089Abstract: This disclosure describes certain substituted piperazine-1,4-naphthalenediones useful as anti-asthmatic agents.Type: GrantFiled: July 22, 1988Date of Patent: May 9, 1989Assignee: American Cyanamid CompanyInventors: Jeffrey B. Medwid, Lawrence W. Torley, Andrew S. Tomcufcik
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Patent number: 4826879Abstract: 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: GrantFiled: January 14, 1987Date of Patent: May 2, 1989Assignee: Senju Pharmaceutical Co., Ltd.Inventors: Yujiro Yamamoto, Takahiro Ogawa, Yoshikazu Kuribayashi
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Patent number: 4804406Abstract: 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: GrantFiled: September 3, 1987Date of Patent: February 14, 1989Assignee: Bayer AktiengesellschaftInventors: Joachim Weissmuller, Wilhelm Brandes, Gerd Hanssler, Paul Reinecke
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Patent number: 4791139Abstract: 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: GrantFiled: February 25, 1987Date of Patent: December 13, 1988Assignee: Imperial Chemical Industries PLCInventors: Michael J. Bushell, Robin A. E. Carr
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Patent number: 4791123Abstract: 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: GrantFiled: January 22, 1987Date of Patent: December 13, 1988Assignee: Schering Akt.Inventors: Helga Franke, Heinrich Franke, Hans-Rudolf Kruger, Hartmut Joppien, Dietrich Baumert, David Giles
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Patent number: 4782059Abstract: Certain fungistats when employed in combination have been found to exhibit synergistic antifungal properties and further exhibit fungicidal properties.Type: GrantFiled: September 29, 1986Date of Patent: November 1, 1988Assignee: Merck & Co., Inc.Inventors: Hans H. Gadebusch, Mary E. Valiant
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Patent number: 4764534Abstract: 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: GrantFiled: July 17, 1984Date of Patent: August 16, 1988Assignee: Eli Lilly and CompanyInventors: Albert J. Clinton, deceased, George O. P. O'Doherty
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Patent number: 4761421Abstract: 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: GrantFiled: September 18, 1986Date of Patent: August 2, 1988Assignee: Merck & Co., Inc.Inventor: Larry A. Muir
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Patent number: 4758561Abstract: 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: GrantFiled: July 22, 1985Date of Patent: July 19, 1988Assignee: Societe Cortial, S.A.Inventors: Guillaume Le Baut, Louis Sparfel, Marie-Helene Creuzet, Claude Feniou, Henri Pontagnier, Gisele Prat
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Patent number: 4757067Abstract: 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: GrantFiled: January 21, 1987Date of Patent: July 12, 1988Assignee: Societe Cortial, S.A.Inventors: Guillaume Le Baut, Louis Sparfel, Marie-Helene Creuzet, Claude Feniou, Henri Pontagnier, Gisele Prat
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Patent number: 4735969Abstract: A novel bisulfite adduct of menadione, the menadione choline bisulfite adduct, a process for its preparation, and its use as an antihemorrhagic agent.Type: GrantFiled: November 18, 1985Date of Patent: April 5, 1988Assignee: BASF AktiengesellschaftInventors: Joachim U. Schneider, Hans Kiefer
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Patent number: 4684661Abstract: 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: GrantFiled: November 20, 1985Date of Patent: August 4, 1987Assignee: Sandoz Ltd.Inventor: Anton Stuetz
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Patent number: 4656192Abstract: 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: GrantFiled: June 14, 1984Date of Patent: April 7, 1987Assignee: Mect CorporationInventor: Masatoshi Yamato
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Patent number: 4628062Abstract: 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: GrantFiled: December 17, 1984Date of Patent: December 9, 1986Assignee: Troponwerke GmbH & Co., KGInventors: Wolfgang Opitz, Bernhard Pelster, Romanis Fruchtmann, Udo Krupka, Walter Gauss, Hartmut Kiehne, Hermann Oediger
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Patent number: 4600708Abstract: 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: GrantFiled: July 19, 1985Date of Patent: July 15, 1986Assignee: American Home Products CorporationInventors: Gerald L. Reuter, Mark E. Coons
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Patent number: 4551479Abstract: 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: GrantFiled: March 22, 1984Date of Patent: November 5, 1985Assignee: Akzo N.V.Inventors: David S. Savage, James Redpath
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Patent number: 4508732Abstract: 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: GrantFiled: January 21, 1983Date of Patent: April 2, 1985Assignee: Merck Patent Gesellschaft mit beschrankter HaftungInventors: Hans-Heinrich Hausberg, Helmut Prucher, Jurgen Uhl, Christoph Seyfried, Klaus Minck