Hydroxy, Bonded Directly To Carbon, Or Ether In Substituent Q (h Of -oh May Be Replaced By A Substituted Or Unsubstituted Ammonium Ion Or A Group Ia Or Iia Light Metal) Patents (Class 564/165)
  • Patent number: 4311706
    Abstract: Novel, transient prodrug forms of dopa and dopamine have (i) the structural formula (I): ##STR1## wherein each R is independently selected from the group consisting of hydrogen, R.sup.3 -CO- and ##STR2## wherein X is O, S or NR.sup.6 ; R.sup.1 is hydrogen or --COOR.sup.8 ; R.sup.2 is hydrogen or OR; R.sup.
    Type: Grant
    Filed: January 22, 1980
    Date of Patent: January 19, 1982
    Assignee: INTERx Research Corporation
    Inventors: Nicholas S. Bodor, Kenneth B. Sloan, Stefano A. Pogany
  • Patent number: 4311853
    Abstract: Novel Selenium derivatives of thyroxine and tri-iodothyronine have the formula: ##STR1## wherein M is I or H and either (a) R.sub.1 is OH or a carboxyl protecting group and R.sub.2 contains at least one Se, preferably .sup.75 Se, atom or (b) R.sub.2 is H or an amino protecting group and R.sub.1 contains at least one Se, preferably .sup.75 Se, atom.The compounds are useful in dual isotope assays of thyroid function.
    Type: Grant
    Filed: January 30, 1980
    Date of Patent: January 19, 1982
    Assignee: The Radiochemical Centre Limited
    Inventor: Gavin M. Cree
  • Patent number: 4310429
    Abstract: Novel .alpha.-aminoacetamides are powerful stabilizers for organic materials subject to oxygen and heat degradation, and particularly for synthetic natural rubber and synthetic ester lubricants. A wide range of substituents on the amine and amide N atoms, and also on the saturated carbon atom, yields an array of stabilizers having a wide range of compatibility in compositions comprising various synthetic resinous compounds to be stabilized.Novel syntheses are provided utilizing at least one amine nucleophilic agent, a dichlorocarbene ion generating agent, and an alkoxide ion generating agent, which together in the presence of aqueous alkali and an onium salt, yield novel .alpha.-aminoacetamides in which a wide choice of substituents may be introduced. The nucleophilic agent may be a primary or secondary amine, or one of each. The dichlorocarbene ion generating agent is a haloform. The alkoxide ion generating agent may be a ketone, an aldehyde, or a cyanohydrin which reacts with the haloform. An .alpha.
    Type: Grant
    Filed: June 19, 1978
    Date of Patent: January 12, 1982
    Assignee: The B. F. Goodrich Company
    Inventor: John T. Lai
  • Patent number: 4309443
    Abstract: A compound of the formula (I): ##STR1## or a pharmaceutically acceptable ester, amide or salt thereof wherein R.sub.1 is a hydrogen, fluorine, chlorine or bromine atom or a hydroxyl, hydroxymethyl, methyl, methoxyl, amino, formamido, acetamido, methylsulphonylamido, nitro, benzyloxy, methylsulphonylmethyl, ureido, trifluoromethyl or p-methoxybenzylamino group; R.sub.2 is a hydrogen, fluorine, chlorine or bromine atom or a hydroxyl group; R.sub.3 is a hydrogen, chlorine or bromine atom or a hydroxyl group; R.sub.4 is a hydrogen, chlorine or fluorine atom or a methyl, methoxyl or hydroxyl group or a carboxylic acid group or a salt, ester or amide thereof; R.sub.5 is a hydrogen atom or a methyl group; R.sub.6 is a hydrogen atom or a methyl group; R.sub.7 is a hydrogen atom or a methyl or ethyl group; R.sub.
    Type: Grant
    Filed: September 3, 1980
    Date of Patent: January 5, 1982
    Assignee: Beecham Group Limited
    Inventors: David G. Smith, Anthony T. Ainsworth
  • Patent number: 4307072
    Abstract: Nonionic triiodobenzoyl amino acyl derivatives of polyhydroxy amines. Such amines are useful as nonionic X-ray contrast agents. For Example 2-(3-acetamido-2,4,6-triiodo-5-N-methylacetamidobenzoyl glycylamino)-2-deoxy-D-glucitol is especially useful in angiography.
    Type: Grant
    Filed: July 19, 1977
    Date of Patent: December 22, 1981
    Assignee: Mallinckrodt, Inc.
    Inventor: Kenneth R. Smith
  • Patent number: 4306080
    Abstract: A novel process for the purification of industrial effluents, wherein the effluents are brought into contact with cationically modified, cellulose-containing materials, the cationic constituent of which is bonded to the cellulose part via the grouping of the general formula--O--CH.sub.2 --N<in which the nitrogen belongs to an amide group of the cationic constituent and the oxygen is bonded to the cellulose part.
    Type: Grant
    Filed: February 9, 1979
    Date of Patent: December 15, 1981
    Assignee: Ciba-Geigy Corporation
    Inventors: Jaroslav Haase, Peter Liechti, Hans Wegmuller, Rudolf F. Wurster, Quentin Bowes
  • Patent number: 4277473
    Abstract: Compounds having the formula ##STR1## wherein a is 0 or 1, R.sub.1 is hydrogen or lower alkyl, A is lower alkylene or lower alkylidene, and R.sub.2 and R.sub.3, which can be the same or different, are hydrogen, lower alkyl, cycloalkyl, benzyl or substituted benzyl, or ##STR2## is a saturated heterocyclic ring, and acid addition salts thereof, possess anti-viral activity and reduced activity on the central nervous system.
    Type: Grant
    Filed: December 12, 1979
    Date of Patent: July 7, 1981
    Assignees: Kao Soap Co., Ltd., Sumitomo Chemical Industries Ltd.
    Inventors: Yoshiaki Inamoto, Motoyoshi Osugi, Eiji Kashihara
  • Patent number: 4277471
    Abstract: Biphenylylalkylamines which have anti-arrhythmic activity have been prepared. Pharmaceutical formulations containing such compounds and a method of treating cardiac arrhythmias are provided.
    Type: Grant
    Filed: February 22, 1980
    Date of Patent: July 7, 1981
    Assignee: Eli Lilly and Company
    Inventors: William B. Lacefield, Richard L. Simon
  • Patent number: 4272550
    Abstract: Omega-[4-(polyfluoro-2-hydroxy-2-propyl)-2,3,6-substituted-phenoxy and phenylthio]alkanoic acids and compounds related thereto having antihypertensive activity are preparable by reaction of the appropriate 2,3,6-substituted-4-(polyfluoro-2-hydroxy-2-propyl)phenol or thiophenol with an alkyl ester of a bromoalkanoic acid, followed by hydrolysis to the free acid.
    Type: Grant
    Filed: October 31, 1979
    Date of Patent: June 9, 1981
    Assignee: Schering Corporation
    Inventors: Bernard R. Neustadt, Elijah H. Gold
  • Patent number: 4272536
    Abstract: A compound having the formula ##STR1## wherein a is 0 or 1, R.sub.1 is hydrogen or lower alkyl, A is lower alkylene or lower alkylidene, and R.sub.2 and R.sub.3, which can be the same or different, are hydrogen, lower alkyl, cycloalkyl, benzyl or substituted benzyl, or ##STR2## form a saturated heterocyclic ring, and pharmacologically acceptable acid addition salt thereof, exhibits anti-viral activity and is free from significant effect on the central nervous system.
    Type: Grant
    Filed: December 12, 1979
    Date of Patent: June 9, 1981
    Assignees: Kao Soap Co., Ltd., Sumitomo Chemical Industries Ltd.
    Inventors: Yoshiaki Inamoto, Motoyoshi Osugi, Eiji Kashihara
  • Patent number: 4267374
    Abstract: Novel compounds of the formula ##STR1## wherein A is methylene, ethylene or ethylidene; R.sub.1 is --C.tbd.CH or --CH.dbd.CH.sub.2 ; R.sub.2 is hydrogen or COR wherein R is hydroxy, a straight or branched alkoxy group of from 1 to 8 carbon atoms, --NR.sub.4 R.sub.5 wherein each of R.sub.4 and R.sub.5 is hydrogen or a straight or branched lower alkyl group of from 1 to 4 carbon atoms or ##STR2## wherein R.sub.6 is hydrogen, a straight or branched lower alkyl group of from 1 to 4 carbon atoms, benzyl or p-hydroxybenzyl; R.sub.a is hydrogen, ##STR3## alkylcarbonyl wherein the alkyl moiety has from 1 to 4 carbon atoms and is straight or branched, alkoxycarbonyl wherein the alkoxy moiety has from 1 to 4 carbon atoms and is straight or branched or ##STR4## wherein R.sub.7 is selected from hydrogen, a straight or branched lower alkyl group of from 1 to 4 carbon atoms, benzyl and p-hydroxybenzyl; and R.sub.b has the same meaning as defined for R.sub.a except R.sub.b is not ##STR5## and R.sub.a and R.sub.
    Type: Grant
    Filed: June 25, 1979
    Date of Patent: May 12, 1981
    Assignee: Merrell Toraude et Compagnie
    Inventors: Brian W. Metcalf, Michel Jung, Charles Danzin
  • Patent number: 4267354
    Abstract: Compounds having the formula ##STR1## wherein R.sub.1 is alkoxycarbonyl, amido, alkylamido, or dialkylamido; R'.sub.3 is alkylbenzylamino, dialkylamino, 1-pyrrolidinyl, 1-piperidinyl, 4-morpholinyl, or 4-alkyl-1-piperazinyl; A.sub.1 is an alkylene group having 2 to 5 carbon atoms; and n is 1, 2 or 3; are intermediates useful in the preparation of substituted amides having antiinflammatory activity.
    Type: Grant
    Filed: February 4, 1980
    Date of Patent: May 12, 1981
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: John Krapcho, Chester F. Turk
  • Patent number: 4263323
    Abstract: Amines of the formula I ##STR1## method of preparing the same and pharmaceutical compositions and method for treating cardiovascular disorders by blocking the .beta.-receptors of the heart in combination with a peripheral vasodilating activity.
    Type: Grant
    Filed: April 5, 1979
    Date of Patent: April 21, 1981
    Assignee: Aktiebolaget Hassle
    Inventors: Enar I. Carlsson, Gustav B. R. Samuelsson, Bo T. Lundgren
  • Patent number: 4252804
    Abstract: Compounds of the formula I ##STR1## wherein m and n are 0, 1 or 2, X represents oxygen, imino, benzylimino, or morpholinoethylimino, Y represents CO, CONH, COO or SO.sub.2, and NR.sub.1 R.sub.2 represents a dimethylamino, diethylamino, dipropylamino, dibutylamino, allylamino, isobutenylamino, cyclopentylamino, cyclohexylamino, cycloheptylamino, cyclooctylamino, N-methyl N-cyclopentylamino, N-methyl N-cyclohexylamino, N-allyl N-cyclohexylamino, adamantylamino, diethoxyethylamino, dimethylaminoethylamino, dimethylaminopropylamino, N-methyl N-dimethylaminopropyl-amino, benzylamino, 3,4,5-trimethoxybenzylamino, phenethylamino, p-chlorophenethylamino, tetrahydrofurfurylamino, tetrahydropyranylmethylamino, pyrrolidino, isoxazolidinyl, piperidino, 4-hydroxypiperidino, 4-m-chlorophenyl-4-hydroxypiperidino, homopiperidino, 1,2,3,6-tetrahydropyridyl, morpholino, 2-methylmorpholino, 2,6-dimethylmorpholino, 2-morpholinoethylamino, thiamorpholino, piperazino, 4-methylpiperazino, 4-(.alpha.
    Type: Grant
    Filed: January 13, 1978
    Date of Patent: February 24, 1981
    Assignee: Metabio-Joullie
    Inventors: Maurice Joullie, Gabriel Maillard, Lucien Lakah, Christian J. M. Warolin
  • Patent number: 4243814
    Abstract: A process for the chemical catalytic hydrolysis of an .alpha.-aminonitrile or of one of the salts thereof, characterized in that an aqueous solution containing at least one carbonyl derivative is reacted with the said .alpha.-amine nitrile or with one of the salts thereof in the presence of hydroxide ions.
    Type: Grant
    Filed: December 1, 1977
    Date of Patent: January 6, 1981
    Inventors: Robert Pascal, Monique Lasperas nee Marnier, Alain Rousset, Auguste Commeyras, Jacques Taillades, Louis Mion