Plural Chalcogens Attached Directly To The Six-membered Hetero Ring By Nonionic Bonding Patents (Class 546/142)
  • Patent number: 4349677
    Abstract: The compound 3,4-dihydro-3,4-isoquinolinedione 4-oxime is useful as an antifungal agent.
    Type: Grant
    Filed: November 9, 1981
    Date of Patent: September 14, 1982
    Assignee: Morton-Norwich Products, Inc.
    Inventors: Thomas J. Schwan, Homer A. Burch, Joseph E. Gray
  • Patent number: 4344949
    Abstract: Substituted acyl derivatives of 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acids and the pharmaceutically acceptable salts thereof are produced by coupling a suitably substituted 1,2,3,4-tetrahydroisoquinoline with a suitably substituted amino acid and when desired hydrolyzing or removing protecting groups of the resulting product. The compounds of the invention, their salts and pharmaceutical compositions thereof are useful as antihypertensive agents.
    Type: Grant
    Filed: February 20, 1981
    Date of Patent: August 17, 1982
    Assignee: Warner-Lambert Company
    Inventors: Milton L. Hoefle, Sylvester Klutchko
  • Patent number: 4315855
    Abstract: Dyes of the formula ##STR1## where X and Y, for example, can be hydrogen or halogen and R can be alkyl among other substituents. The dyes are derived from an O-nitroaniline diazo component and an N-substituted homophthalimide as coupling component. The dyes are greenish yellow to orange and give clear dyeings of good color strength and having good general fastness properties on polyesters, cellulose esters and in some cases also on polyamides. The fastness to light and the fastness to heat setting are excellent and may easily be influenced by the choice of substituents.
    Type: Grant
    Filed: July 22, 1976
    Date of Patent: February 16, 1982
    Assignee: BASF Aktiengesellschaft
    Inventor: Ernst Schefczik
  • Patent number: 4291042
    Abstract: Compounds of formula: ##STR1## and pharmaceutically acceptable acid addition or quaternary ammonium salts thereof wherein the piperidine ring is substituted in the 3 or 4 position; X represents .dbd.CH-- or .dbd.N--; Y represents --NR.sup.5 --, --O-- or --S-- wherein R.sup.5 is hydrogen or lower alkyl; A is lower alkylene or hydroxy lower alkylene, Z and Z.sup.1 independently represent ##STR2## Z may also represent --CH.sub.2 --, --(CH.sub.2).sub.2 --, --CHMe-- or --CMe.sub.2 --; R.sup.1, R.sup.2, R.sup.3 independently represent hydrogen, halogen, lower alkyl, lower alkoxy, nitro, amino, lower alkylamino, trifluoromethyl, lower-alkanoylamino, hydroxy or aryl lower alkoxy; or R.sup.1 and R.sup.2 when adjacent together with the carbons to which they are attached form a six membered carbocyclic ring; and R.sup.4 represents hydrogen or lower alkyl, are disclosed which possess psychotropic activity and are useful as anti-depressants.
    Type: Grant
    Filed: January 21, 1980
    Date of Patent: September 22, 1981
    Assignee: John Wyeth & Brother Limited
    Inventor: Terence J. Ward
  • Patent number: 4289882
    Abstract: This invention relates to the production of 4a-aryldecahydroisoquinolines where the aryl group is selected as 3-methoxy phenyl and intermediates. These compounds are morphine analogs and show utility similar to the known morphine, codeine, and thebaine.
    Type: Grant
    Filed: September 5, 1978
    Date of Patent: September 15, 1981
    Assignee: The United States of America as represented by the Department of Health & Human Services
    Inventors: Henry Rapoport, Dwight D. Weller, Richard D. Gless
  • Patent number: 4283539
    Abstract: Novel isoquinoline acetic acids and derivatives thereof useful as aldose reductase inhibitors and as therapeutic agents for the treatment of chronic diabetic complications, especially diabetic cataracts are disclosed. Also disclosed are pharmaceutical compositions containing the novel compounds of this invention and a method of treatment of diabetic cataracts by administration of effective amounts of the novel compounds described herein.
    Type: Grant
    Filed: December 18, 1979
    Date of Patent: August 11, 1981
    Assignee: Pfizer Inc.
    Inventor: Rodney C. Schnur
  • Patent number: 4264619
    Abstract: New .alpha.-(cyclic tert. aminophenyl)-aliphatic acids, e.g. those of the formula ##STR1## and functional derivatives thereof, are anti-inflammatory agents.
    Type: Grant
    Filed: November 21, 1978
    Date of Patent: April 28, 1981
    Assignee: Ciba-Geigy Corporation
    Inventors: Richard W. J. Carney, George deStevens
  • Patent number: 4260762
    Abstract: Neuroleptically active octahydro-1H-pyrrolo[2,3-g]isoquinolines of the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4 and X are as hereinafter set forth,are described.
    Type: Grant
    Filed: September 10, 1979
    Date of Patent: April 7, 1981
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Leo Berger, Gary L. Olson
  • Patent number: 4251609
    Abstract: Electrophotosensitive materials having the structure ##STR1## wherein R represents a basic heterocyclic nucleus as well as groups such as hydrogen, alkyl, aryl, aralkyl, etc.;A.sub.1 represents a wide variety of basic heterocyclic nuclei;A.sub.2 represents aryl or may be the same as A.sub.1 ;G represents O or S;M is 0 to 3;N is 0 to 1; andL.sup.1, L.sup.2, L.sup.3, L.sup.4 and L.sup.5 represetn hydrogen, alkyl or aryl.
    Type: Grant
    Filed: April 9, 1979
    Date of Patent: February 17, 1981
    Assignee: Eastman Kodak Company
    Inventors: James R. Nonnemacher, Michael T. Regan, Frank G. Webster
  • Patent number: 4230711
    Abstract: Compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2 are independently alkyl groups containing 1 to 6 carbon atoms; R.sup.3 is a haloalkyl group of the formula C.sub.m Y.sub.(m-1) X.sub.(m+2) wherein X is fluoro, chloro, bromo or iodo and m=1 or 2; Y is hydrogen, fluoro, chloro, bromo or iodo; R.sup.4 is hydrogen, an alkyl group containing 1 to 6 carbon atoms, alkoxy containing 1 to 6 carbon atoms, alkenyl containing 2 to 6 carbon atoms, nitro, hydroxy, alkoxyalkyl containing 2 to 6 carbon atoms, fluoro, bromo, chloro or iodo and n-1, 2, 3 or 4, have fungicidal activity.
    Type: Grant
    Filed: January 31, 1979
    Date of Patent: October 28, 1980
    Assignee: Chevron Research Company
    Inventor: Stephen D. Ziman
  • Patent number: 4202982
    Abstract: N-substituted-14-hydroxy-3-substituted-morphinan derivatives have been found to possess potent narcotic agonist or antagonist activity. In particular, the compound N-Cyclobutylmethyl-3,14-dihydroxymorphinan has been found to possess potent agonist/antagonist activity as a non-narcotic analgesic. A new and efficient total synthesis of these compounds is described herein from the starting material 2-(p-methoxybenzyl)-1,2,3,4,5,6,7,8-octahydroisoquinoline.
    Type: Grant
    Filed: March 22, 1979
    Date of Patent: May 13, 1980
    Assignee: Bristol-Myers Company
    Inventors: Ivo Monkovic, Carol Bachand, Henry Wong
  • Patent number: 4198512
    Abstract: Novel 1-oxo-1,2-dihydroisoquinoline compounds of the formula ##STR1## wherein R.sub.1 represents a lower alkyl group or a phenyl lower alkyl group; R.sub.2 represents a lower alkyl group; R.sub.3 represents a hydrogen atom, a lower alkanoyl group, a lower alkyl group or a hydroxy lower alkyl group; and n is 0, 1 or 2 and the pharmacologically acceptable non-toxic salts thereof.The compounds of this invention are strong analgesic anti-inflammatory agents.
    Type: Grant
    Filed: July 17, 1978
    Date of Patent: April 15, 1980
    Assignee: Yamanouchi Pharmaceutical Co., Ltd.
    Inventors: Kazuo Kubo, Noriki Ito, Isao Souzu, Yasuo Isomura, Hiroshige Homma
  • Patent number: 4179508
    Abstract: Compounds of the formula ##STR1## wherein A is lower alkylene,R is lower alkyl, andn is 0, 1 or 2;the compounds are useful as anti-hyperlipidemics and anti-convulsants.
    Type: Grant
    Filed: July 18, 1978
    Date of Patent: December 18, 1979
    Assignee: Boehringer Ingelheim GmbH
    Inventors: Volkhard Austel, Eberhard Kutter, Wolfgang Eberlein, Joachim Heider, Joachim Kahling
  • Patent number: 4176184
    Abstract: Compounds of the formula ##STR1## wherein R.sub.1 is lower alkyl; phenyl-lower alkyl; cycloalkyl of 3 to 6 carbon atoms; phenyl; mono- or di-substituted phenyl, where the substituents, which may be identical to or different from each other, are each halogen, hydroxyl, methoxy, methylmercapto, methylsulfinyl, methylsulfonyl or benzyloxy; andA is hydrogen or ##STR2## where R.sub.2 is hydrogen or lower alkyl;R.sub.3 is lower alkyl or dimethoxyphenyl-lower alkyl; orR.sub.2 and R.sub.3, together with each other and the nitrogen atom to which they are attached, are piperidino, morpholino or N'-lower alkyl-piperazino; andn is 2 or 3;and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful as cardiotonics, hypotensives, antithrombotics and antiarrhythmics.
    Type: Grant
    Filed: July 17, 1978
    Date of Patent: November 27, 1979
    Assignee: Boehringer Ingelheim GmbH
    Inventors: Volkhard Austel, Eberhard Kutter, Joachim Heider, Wolfgang Eberlein, Walter Kobinger, Christian Lillie, Willi Diederen, Walter Haarmann
  • Patent number: 4163788
    Abstract: New .alpha.-(cyclic tert. aminophenyl)-aliphatic acids, e.g. those of the formula ##STR1## R.sub.1 =H or alkyl, Ph=a phenylene radical R.sub.2 =H, alk(en)yl, cycloalk(en)yl or cycloalk(en)yl-alkyl ##STR2## =bicyclic alkenyleneimino with 1-3 double bonds AND FUNCTIONAL DERIVATIVES THEREOF, ARE ANTI-INFLAMMATORY AGENTS.
    Type: Grant
    Filed: November 7, 1977
    Date of Patent: August 7, 1979
    Assignee: Ciba-Geigy Corporation
    Inventors: Richard W. J. Carney, George DE Stevens
  • Patent number: 4153603
    Abstract: N-substituted-14-hydroxy-3-substituted-morphinan derivatives have been found to possess potent narcotic agonist or antagonist activity. In particular, the compound N-Cyclobutylmethyl-3,14-dihydroxymorphinan has been found to possess potent agonist/antagonist activity as a non-narcotic analgesic. A new and efficient total synthesis of these compounds is described herein from the starting material 2-(p-methoxybenzyl)-1,2,3,4,5,6,7,8-octahydroisoquinoline.
    Type: Grant
    Filed: September 28, 1977
    Date of Patent: May 8, 1979
    Assignee: Bristol-Myers Company
    Inventors: Ivo Monkovic, Carol Bachand, Henry Wong
  • Patent number: 4150135
    Abstract: 4A-Aryl-cis-decahydroisoquinolines, such as N-phenethyl-4a-(m-hydroxyphenyl)-cis-decahydroisoquinoline, useful as analgesics.
    Type: Grant
    Filed: March 4, 1977
    Date of Patent: April 17, 1979
    Assignee: E. I. Du Pont de Nemours and Company
    Inventor: William C. Ripka
  • Patent number: 4139534
    Abstract: N-substituted-14-hydroxy-3-substituted-morphinan derivatives have been found to possess potent narcotic agonist or antagonist activity. In particular, the compound N-Cyclobutylmethyl-3,14-dihydroxymorpinan has been found to posess potent agonist/antagonist activity as a non-narcotic analgesic. An improved total snythesis of these compounds is described herein from the starting material 2-(p-methoxybenzyl)-1,2,3,4,5,6,7,8-octahydroisoquinoline. A preferred feature of the process involves borane reduction of 2-cyclobutylcarbonyl-9,10-dihydroxy-1-(p-methoxybenzyl)perhydroisoquinolin e (Va) to provide the corresponding cyclobutylmethyl derivative complexed with borane which is converted directly to N-cyclobutylmethyl-14.beta.-hydroxy-3-methoxymorphinan (LVa) by treating with acid.
    Type: Grant
    Filed: February 17, 1977
    Date of Patent: February 13, 1979
    Assignee: Bristol-Myers Company
    Inventors: Gary Lim, Ivo Monkovic
  • Patent number: 4133955
    Abstract: A one-stage process for the production of a 2-equivalent acylacetamide yellow coupler, in which one hydrogen atom of the .alpha.-methylene group of the acyl acetamide coupler molecule is substituted by a group which is attached through an oxygen or nitrogen atom and which can be split off during chromogenic development with an oxidized color developer containing a primary aromatic amino group, which process is carried out by reactingA 4-equivalent acylacetamide yellow coupler withA compound containing an aromatic hydroxyl group or an --NH-- group in a heterocyclic ringIn the presence of a halogen, or an agent which releases halogen, andA basic condensation agentIn a substantially aprotic solvent.
    Type: Grant
    Filed: October 6, 1976
    Date of Patent: January 9, 1979
    Assignee: AGFA-Gevaert Aktiengesellschaft
    Inventor: Gunter Renner
  • Patent number: 4129565
    Abstract: Isocarbostyrils of the formula ##STR1## wherein R.sub.1 represents a lower alkyl group having 1 to 4 carbon atoms, and R.sub.3 and R.sub.4, same or different, individually means hydrogen or an alkyl, aralkyl or cycloalkyl group provided at least either one of R.sub.3 and R.sub.4 should not be hydrogen, or R.sub.3 and R.sub.4 together with the adjacent nitrogen atom may form a heterocyclic ring, having anti-arrhythmic activity and low toxicity are prepared by reacting a 4-substituted isocarbostyril derivative of the formula ##STR2## wherein R.sub.1 is the same as defined above and R.sub.2 represents ##STR3## or its functional equivalent, e.g. --Ch.sub.2 --CH(OH)CH.sub.2 X in which X represents a halogen atom, with an alkyl amine of the general formula ##STR4## wherein R.sub.3 and R.sub.4 are same as defined above..
    Type: Grant
    Filed: December 16, 1976
    Date of Patent: December 12, 1978
    Assignee: Nisshin Flour Milling Co., Ltd.
    Inventors: Hideo Fukushima, Yoshikuni Suzuki
  • Patent number: 4126691
    Abstract: New .alpha.-(cyclic tert. aminophenyl)-aliphatic acids, e.g. those of the formula ##STR1## AND FUNCTIONAL DERIVATIVES THEREOF, ARE ANTI-INFLAMMATORY AGENTS.
    Type: Grant
    Filed: December 6, 1976
    Date of Patent: November 21, 1978
    Assignee: Ciba-Geigy Corporation
    Inventors: Richard W. J. Carney, George DEStevens