The Other Ring Nitrogen Has A Substituent Which Includes Chalcogen Single Bonded To Acyclic Carbon Patents (Class 544/394)
  • Patent number: 4576943
    Abstract: This disclosure describes certain pyrazolo[1,5-a]pyrimidines useful as hypotensive and/or anxiolytic agents, or as agents for the treatment of cognitive and related neural behavioral problems in mammals.
    Type: Grant
    Filed: October 9, 1984
    Date of Patent: March 18, 1986
    Assignee: American Cyanamid Company
    Inventors: Andrew S. Tomcufcik, Walter E. Meyer, John P. Dusza, Shin S. Tseng
  • Patent number: 4515793
    Abstract: A compound of the formula ##STR1## in which A is ##STR2## n is 1, 2 or 3, and R is phenyl optionally substituted with halogen, alkyl, phenyl, cyano, hydroxy, alkoxy, mercapto, sulfinyl, sulfonyl, amino, nitro, trifluoromethyl and/or naphthyl radicals; or a furan, thiophene, pyridine, benzofuran, dibenzothiophene or thianthrene radical,or a pharmacologically acceptable salt thereof, for treating schistosomiasis.
    Type: Grant
    Filed: July 27, 1983
    Date of Patent: May 7, 1985
    Assignee: Edna McConnell Clark Foundation
    Inventors: Leslie M. Werbel, Norman Colbry, William Turner, Donald F. Worth
  • Patent number: 4495350
    Abstract: Herbicidally effective aminoalkyl esters of 2-nitro-5-(o-chloro-p-trifluoromethylphenoxy)-benzoic acid, and acid addition salts and quaternary ammonium salts thereof, are suitable for the selective control of weeds in crops of useful plants, for example soya bean and rice crops.The aminoalkyl esters correspond to the formula ##STR1## wherein A is a C.sub.2 -C.sub.4 -alkylene bridge or the direct bond, and ##STR2## is an open amino group, and ##STR3## is a cyclic amino group.
    Type: Grant
    Filed: September 13, 1982
    Date of Patent: January 22, 1985
    Assignee: Ciba-Geigy Corporation
    Inventors: Dieter Durr, Otto Rohr, Beat Bohner
  • Patent number: 4459410
    Abstract: Diphenylalkanoether and diphenylalkanone oximeether derivatives of the formula: ##STR1## wherein R.sup.1 and R.sup.2 are each independently an aryl group optionally substituted with 1 to 3 substituents selected from the group consisting of halogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, nitro, cyano, di(C.sub.1 -C.sub.4)alkylamino, amino, benzyloxy, hydroxyl, C.sub.1 -C.sub.4 alkylthio, C.sub.1 -C.sub.4 alkylsulfinyl, C.sub.1 -C.sub.4 alkysulfonyl, C.sub.1 -C.sub.4 alkanoylamino, C.sub.1 -C.sub.4 alkylmino and N-(C.sub.1 -C.sub.4)alkyl-N-(C.sub.1 -C.sub.4)alkanoylamino, Z.sup.1 is a group of the formula: ##STR2## (wherein R.sup.3 and R.sup.4 are each independently a hydrogen atom, a C.sub.1 -C.sub.4 alkyl group or an ar(C.sub.1 -C.sub.
    Type: Grant
    Filed: October 5, 1981
    Date of Patent: July 10, 1984
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Keiichi Ono, Hajime Kawakami, Junki Katsube
  • Patent number: 4438268
    Abstract: This invention relates to new nematic liquid crystal substances for electro-optical components.The object of this invention is to create substances for electro-optical components combining chemical and thermal stability with low melting and high clear points at low operational voltage, as well as to processes for their production.It has been found that new liquid-crystal trans-6-n-alkyl-decalin-2-carbonic acid ester of the general formula ##STR1## can be introduced into electro-optical components. These substances are produced by the catalytic high-pressure hydrogenation of 6-n-alkylnaphthalene-2-carbonic acids, separation of the trans-isomers by distillation, and esterification with the corresponding hydroxy compounds of the acyl chlorides obtained through reaction with thionyl chloride.
    Type: Grant
    Filed: September 14, 1981
    Date of Patent: March 20, 1984
    Inventors: Horst Zaschke, Wolfgang Schafer, Hans-Joachim Deutscher, Dietrich Demus, Gerhard Pelzl
  • Patent number: 4411904
    Abstract: Compounds of the formula ##STR1## where X and Y are hydrogen, halogen, lower alkyl, nitro are useful as neuroleptics.
    Type: Grant
    Filed: June 14, 1982
    Date of Patent: October 25, 1983
    Assignee: Warner-Lambert Company
    Inventor: Ian C. Pattison
  • Patent number: 4404384
    Abstract: A compound of general formula ##STR1## wherein X represents a radical selected from the group consisting of one of the formulae ##STR2## in which R.sup.1 represents a radical selected from the group(a) a hydrogen atom,(b) an amino group, when X represents an --OR.sup.1 moiety,(c) an alkyl group having from 1 to 6 carbon atoms(d) an at most binuclear aryl group being unsubstituted or substituted by at most 3 substituents of the group halogen atoms, alkyl, alkoxy, halogenalkyl groups each having up to 4 carbon atoms, cycloalkyl groups having 3 to 6 carbon atoms, nitro and cyano groups; andR.sup.2 and R.sup.
    Type: Grant
    Filed: May 28, 1981
    Date of Patent: September 13, 1983
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Ulrich Gebert, Werner Thorwart, Jaromir Komarek, Carl Cartheuser
  • Patent number: 4372958
    Abstract: A new compound 3(4-phenyl-1-piperazinio-1-yl)-1,2-propanediol 3(theophyllin-7-yl)-1-propanesulphonate, possesses antitussive action and is therefore usable in therapy. The compound is obtained by treating 3(theophyllin-7-yl)-1-propanesulphonic acid with 3(4-phenylpiperazin-1-yl)-1,2-propanediol in a suitable solvent.
    Type: Grant
    Filed: June 10, 1981
    Date of Patent: February 8, 1983
    Assignee: A. Menarini S.A.S.
    Inventors: Vittorio Pestellini, Mario Ghelardoni, Danilo Giannotti, Alberto Meli, Carlo A. Maggi
  • Patent number: 4370330
    Abstract: Novel N-(trimethoxybenzyl)-piperazines of the formula: ##STR1## wherein A= ##STR2## wherein R is trifluoromethyl, hydroxy, nitro, halogen, lower-alkyl, or lower-alkoxy;R' is hydrogen, trifluoromethyl, halogen, lower-alkyl, or lower-alkoxy;R" is hydrogen or lower-alkoxy,or wherein R and either R' or R" together stand for lower-alkylene dioxy, and acid addition salts thereof, a method of preparing same, pharmaceutical compositions thereof, and a method of enhancing circulation, especially cerebrovascular circulation, therewith, are disclosed.
    Type: Grant
    Filed: October 5, 1981
    Date of Patent: January 25, 1983
    Assignee: Merz & Company
    Inventors: Arthur Scherm, Dezsoe Peteri
  • Patent number: 4370329
    Abstract: Novel N-(trimethoxybenzyl)-piperazines of the formula: ##STR1## wherein R is trifluoromethyl, hydroxy, nitro, halogen, lower-alkyl, or lower-alkoxy;R' is hydrogen, trifluoromethyl, halogen, lower-alkyl, or lower-alkoxy;R" is hydrogen or lower-alkoxy,or wherein R and either R' or R" together stand for lower-alkylene dioxy, and acid addition salts thereof, a method of preparing same, pharmaceutical compositions thereof, and a method of enhancing circulation, especially cerebrovascular circulation, therewith, are disclosed.
    Type: Grant
    Filed: August 22, 1980
    Date of Patent: January 25, 1983
    Assignee: Merz & Company
    Inventors: Arthur Scherm, Dezsoe Peteri
  • Patent number: 4364954
    Abstract: Compounds of the formula ##STR1## where X and Y are hydrogen, halogen, lower alkyl, nitro are useful as neuroleptics.
    Type: Grant
    Filed: May 29, 1981
    Date of Patent: December 21, 1982
    Assignee: Warner-Lambert Company
    Inventor: Ian C. Pattison
  • Patent number: 4358450
    Abstract: Compounds of general formula ##STR1## wherein R.sup.1 represents a member selected from the group consisting of (a) an unsubstituted at most binuclear aryl group having from 6 to 10 carbon atoms, such groups substituted by from 1 to 3 equal or different radicals selected from the group consisting of alkyl, halogenoalkyl, alkoxy, dialkylamino each having up to 4 carbon atoms in the alkyl moiety, halogen phenyl, carboxyl, cyano, nitro and hydroxy groups,(b) a 5- to 6-membered heteroaromatic ring wherein the heteroatom is selected from nitrogen, oxygen and sulfur atoms and such rings anellated to a benzene nucleus;R.sup.2 represents a member selected from the group consisting of hydrogen, alkyl having up to 3 carbon atoms, phenyl, cycloalkyl having up to 6 carbon atoms in the ring and cycloalkyl bearing a hydrocarbon bridging radical having up to 2 carbon atoms;R.sup.3 represents hydrogen, hydroxy or acyloxy;R.sup.4 and R.sup.
    Type: Grant
    Filed: August 6, 1979
    Date of Patent: November 9, 1982
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Ulrich Gebert, Ernold Granzer, Heinz-Gunter Greve, Werner Thorwart
  • Patent number: 4357332
    Abstract: 1-Benzyl- and 1-phenyl-4-(2-hydroxy-3-benzyloxypropyl)-piperazines useful as immune regulants are disclosed. Also disclosed are pharmaceutical compositions containing the novel compounds and a method of regulating immune response of a warm blooded animal by administration of the novel compounds.
    Type: Grant
    Filed: May 5, 1980
    Date of Patent: November 2, 1982
    Assignee: Pfizer Inc.
    Inventors: Allen R. Kraska, Joseph G. Lombardino
  • Patent number: 4342762
    Abstract: The invention relates to novel basic ethers of the general formula /I/ and pharmaceutically acceptable acid addition salts and quaternary salts thereof, ##STR1## wherein R.sup.1 and R.sup.2 may be the same or different and represent a C.sub.1-5 alkyl group or a C.sub.3-6 cycloalkyl group or they form, together with the adjacent nitrogen atom, a heterocyclic ring containing 4-7 carbon atoms and optionally a further hetero atom, e.g. an oxygen, sulfur or nitrogen atom, and this latter may be optionally substituted by a C.sub.1-3 alkyl, benzyl or phenyl group,R represents a phenyl, phenyl-/C.sub.1-3 alkyl/ or thienyl group optionally substituted by one or more halogen or C.sub.1-3 alkoxy substituent/s/,A represents a C.sub.2-5 straight or branched alkylene chain, and represents a valence bond of .alpha. or .beta. configuration.
    Type: Grant
    Filed: December 11, 1980
    Date of Patent: August 3, 1982
    Assignee: Egyt Gyogyszervegyeszeti Gyar
    Inventors: Zoltan Budai, Laszlo Magdanyi, Aranka Lay nee Konya, Tibor Mezei, Katalin Grasser, Lujza Petocz, Ibolya Kosoczky
  • Patent number: 4339580
    Abstract: Piperazinylalkoxyindanes and their pharmaceutically acceptable acid addition salts which have anti-anxiety activity and are effective as sedatives.
    Type: Grant
    Filed: June 9, 1980
    Date of Patent: July 13, 1982
    Assignee: Mitsubishi Chemical Industries, Limited
    Inventors: Ryoji Kikumoto, Akihiro Tobe, Harukazu Fukami, Mitsuo Egawa
  • Patent number: 4336382
    Abstract: There are disclosed compounds of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of lower alkyl; R.sub.8 is selected from the group consisting of --O--(CH.sub.2).sub.n --wherein n is 2 to 20, ##STR2## and R.sub.6 is selected from the group consisting of hydrogen or lower alkoxy, and ##STR3## wherein R.sub.1 is selected from the group consisting of lower alkyl; R.sub.8 is selected from the group consisting of --O--(CH.sub.2).sub.n --wherein n is 2 to 20, ##STR4## and R.sub.6 is selected from the group consisting of hydrogen or lower alkoxy and racemates thereof.There are also disclosed processes and intermediates utilized to produce the end products.The end products have utility as agents exhibiting both .alpha. and selective .beta. adrenergic blocking action.
    Type: Grant
    Filed: August 25, 1980
    Date of Patent: June 22, 1982
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Kenneth E. Fahrenholtz, Robert W. Guthrie, Richard W. Kierstead, Jefferson W. Tilley
  • Patent number: 4335126
    Abstract: There are prepared compounds corresponding to the general formula ##STR1## in which R.sup.1 is a hydrogen atom, a C.sub.2 to C.sub.6 -alkanoyl group, a C.sub.3 to C.sub.6 -alkenoyl group, a C.sub.3 to C.sub.6 -cycloalkyl carbonyl group, a benzoyl group, an alkoxybenzoyl group, a nicotinoyl group, a thienyl carbonyl group, a furyl carbonyl group, a phenylacetyl group or a C.sub.1 to C.sub.4 -alkoxyphenyl acetyl group and R.sup.2 represents a phenyl, naphthyl or pyridyl group or such group substituted by the groups R.sup.3 and R.sup.4, the groups R.sup.3 and R.sup.4, which may be the same or different, each representing hydrogen, hydroxyl, fluorine, chlorine, bromine, a nitro group, a trifluoromethyl group, a C.sub.1 to C.sub.6 -alkyl group, a C.sub.1 to C.sub.6 -alkoxy group, a C.sub.1 to C.sub.6 -alkyl thio group, a C.sub.1 to C.sub.6 -alkyl sulphonyl group, a C.sub.2 to C.sub.6 -alkanoyl group, an amino group, an acylamino group or an acyloxy group in which the acyl is of the type defined in respect to R.
    Type: Grant
    Filed: October 3, 1980
    Date of Patent: June 15, 1982
    Assignee: Degussa Aktiengesellschaft
    Inventors: Axel Kleemann, Vladimir Jakovlev, Klaus Thiemer, Jurgen Engel
  • Patent number: 4312877
    Abstract: 1-(2-Hydroxy-3-n-alkoxypropyl)-4-substituted-piperazines and piperidines and derivatives thereof useful as immune regulants are disclosed. Also disclosed are pharmaceutical compositions containing the novel compounds and a method of regulating the immune response of a subject by administration of the novel compounds.
    Type: Grant
    Filed: October 31, 1980
    Date of Patent: January 26, 1982
    Assignee: Pfizer Inc.
    Inventor: Allen R. Kraska
  • Patent number: 4308266
    Abstract: The present invention provides tetraline derivatives, useful for the treatment of hypertension, a process for their preparation and compositions containing these compounds.
    Type: Grant
    Filed: September 7, 1979
    Date of Patent: December 29, 1981
    Assignee: Sandoz Ltd.
    Inventor: Max-Peter Seiler
  • Patent number: 4292321
    Abstract: Compounds of the formula ##STR1## where Q is defined hereinafter and X and Y are hydrogen, halogen, lower alkyl, nitro are useful as neuroleptics.
    Type: Grant
    Filed: January 10, 1980
    Date of Patent: September 29, 1981
    Assignee: Warner-Lambert Company
    Inventor: Ian C. Pattison
  • Patent number: 4271161
    Abstract: Compounds of the formula: ##STR1## in which R represents an ethyl or isopropyl group, and their addition salts with acids or quaternary ammonium salts can be prepared from the compounds: ##STR2## in which R has the same meaning as above, and are valuable as analgesics.
    Type: Grant
    Filed: July 9, 1979
    Date of Patent: June 2, 1981
    Assignee: Hexachimie
    Inventor: Jean M. Teulon
  • Patent number: 4267328
    Abstract: Phenylpiperazine derivatives having the general formula (I) ##STR1## in which R.sub.1 represents a radical S(O).sub.m R.sub.3, S(O).sub.n CF.sub.3 or ##STR2## in which radicals m is 0, 1 or 2, n is 1 or 2, R.sub.3 is an alkyl radical having 1 to 10 carbon atoms and R.sub.4 and R.sub.5 independently represent a hydrogen atom or an alkyl radical having 1 to 4 carbon atoms, or the N atom, R.sub.4 and R.sub.5 together form a heterocyclic ring, which can contain another hetero-atom, and R.sub.2 represents a hydrogen atom, the radical CH.sub.2 --CH.sub.2 --OH or a radical of formula CH.sub.2 --CH.sub.2 --O--COR.sub.6, CH.sub.2 --CH.sub.2 --O--CONHR.sub.6 or CH.sub.2 --CH.sub.2 --O--R.sub.6 in which radicals R.sub.6 being an alkyl radical having 1 to 6 carbon atoms and their pharmaceutically acceptable acid addition salts are useful psychotropic agents and analgesics. Compounds in which R.sub.1 is --SCH.sub.3 and simultaneously R.sub.2 is H are not part of the invention.
    Type: Grant
    Filed: July 27, 1979
    Date of Patent: May 12, 1981
    Assignee: Synthelabo
    Inventors: Henry Najer, Philippe Manoury
  • Patent number: 4255426
    Abstract: 1-(2-Hydroxy-3-n-alkoxypropyl)-4-substituted-piperazines and piperidines and derivatives thereof useful as immune regulants are disclosed. Also disclosed are pharmaceutical compositions containing the novel compounds and a method of regulating the immune response of a subject by administration of the novel compounds.
    Type: Grant
    Filed: July 9, 1979
    Date of Patent: March 10, 1981
    Assignee: Pfizer Inc.
    Inventor: Allen R. Kraska
  • Patent number: 4255575
    Abstract: Derivatives of 2-hydroxy-5-(1-hydroxy-2-piperazinylethyl)benzoic acid are prepared which are useful for their blocking action on .alpha. and .beta.-adrenergic receptors. In addition, these compounds are useful as spasmolytic and antihypertensive agents.
    Type: Grant
    Filed: May 4, 1979
    Date of Patent: March 10, 1981
    Assignee: Richardson-Merrell Inc.
    Inventors: J. Martin Grisar, George P. Claxton
  • 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: 4247710
    Abstract: There are disclosed compounds of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of lower alkyl; R.sub.8 is selected from the group consisting of --O--(CH.sub.2).sub.n --wherein n is 2 to 20, ##STR2## R.sub.6 is selected from the group consisting of hydrogen or lower alkoxy, and ##STR3## wherein R.sub.1 is selected from the group consisting of lower alkyl; R.sub.8 is selected from the group consisting of --O--(CH.sub.2).sub.n --wherein n is 2 to 20, ##STR4## and R.sub.6 is selected from the group consisting of hydrogen or lower alkoxy and racemates thereof.There are also disclosed processes and intermediate utilized to produce the end products.The end products have utility as agents exhibiting both .alpha. and selective .beta. adrenergic blocking action.
    Type: Grant
    Filed: September 6, 1979
    Date of Patent: January 27, 1981
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Kenneth E. Fahrenholtz, Robert W. Guthrie, Richard W. Kierstead, Jefferson W. Tilley
  • Patent number: 4242343
    Abstract: Phenylpiperazine derivatives corresponding to the formula (I) ##STR1## in which n is 1, 2 or 3 and R represents the tetrahydrofuryl-2 radical, or the radical CH.sub.2 -SH, or a radical CH.sub.2 -S-alkyl, or a radical CH.sub.2 -O-alkyl or a radical CH.sub.2 -S-CO-alkyl, the alkyls having from 1 to 8 carbon atoms,and also their addition salts with pharmaceutically acceptable acids.These compounds are tranquilizers with psychotropic properties which permit their use in anxiety and depression.
    Type: Grant
    Filed: June 15, 1979
    Date of Patent: December 30, 1980
    Assignee: Synthelabo
    Inventors: Henry Najer, Philippe Manoury
  • Patent number: 4216326
    Abstract: N-{3- and 4-[R.sub.1 -(phenyl)-C(.dbd.X)]-phenyl-lower-alkyl}amines, useful as anti-inflammatory agents, are prepared either by reduction of 3- or 4-[R.sub.1 -(phenyl)-CO]-phenyl-lower-alkanoylamines, which are also useful as anti-inflammatory agents; by benzoylating a phenyl-lower-alkylamine; by reaction of a 3- or 4-lithiophenyl-lower-alkylamine with a R.sub.1 -(phenyl)-carboxaldehyde, a R.sub.1 -(phenyl)-lower-alkyl ketone or a R.sub.1 -(phenyl)-carbonitrile or by transformations involving manipulations of a carbonyl or carbinol group.
    Type: Grant
    Filed: May 3, 1978
    Date of Patent: August 5, 1980
    Assignee: Sterling Drug Inc.
    Inventor: Bernard L. Zenitz
  • Patent number: 4202978
    Abstract: There are disclosed compounds of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of lower alkyl; R.sub.8 is selected from the group consisting of --O--(CH.sub.2).sub.n --wherein n is 2 to 20, ##STR2## and R.sub.6 is selected from the group consisting of hydrogen or lower alkoxy, and ##STR3## wherein R.sub.1 is selected from the group consisting of lower alkyl; R.sub.8 is selected from the group consisting of --O--(CH.sub.2).sub.n --wherein n is 2 to 20, ##STR4## and R.sub.6 is selected from the group consisting of hydrogen or lower alkoxy and racemates thereof.There are also disclosed processes and intermediates utilized to produce the end products.The end products have utility as agents exhibiting both .alpha. and selective .beta. adrenergic blocking action.
    Type: Grant
    Filed: February 8, 1978
    Date of Patent: May 13, 1980
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Kenneth E. Fahrenholtz, Robert W. Guthrie, Richard W. Kierstead, Jefferson W. Tilley
  • Patent number: 4191765
    Abstract: Compounds of formula I ##STR1## wherein R.sup.1 and R.sup.1' are identical or different and represent hydrogen, an alkyl radical or alkoxy radical having 1-4 carbon atoms, the allyl group, a halogen atom or the nitro group, R.sup.2 represents an acrylic acid radical or an acrylic acid nitrile radical of the formulae ##STR2## wherein R.sup.5 represents hydrogen, an alkyl radical having 1-5 carbon atoms, an aryl radical or aryl-lower alkyl radical either unsubstituted or substituted by lower alkyl or alkoxy, R.sup.6 represents hydrogen or an alkyl radical having 1-8 carbon atoms, R.sup.7 represents hydrogen, a lower alkyl radical or an aryl-lower alkyl radical, R.sup.3 and R.sup.4 represent together with the nitrogen atom a heterocyclic ring with 5-7 members being optionally substituted by C.sub.1 -C.sub.4 alkyl, in which ring one carbon atom may be replaced by one oxygen atom, sulfur atom or one further nitrogen atom, the latter may be substituted, or wherein R.sup.3 represents hydrogen and R.sup.
    Type: Grant
    Filed: August 10, 1978
    Date of Patent: March 4, 1980
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Werner Fritsch, Ulrich Stache, Ernst Lindner
  • Patent number: 4156011
    Abstract: The sulphur- and oxygen-containing diaryl compounds of the formula: ##STR1## in which A and B, which may be the same or different, represent O, S, SO or SO.sub.2,Alk is a C.sub.1 -C.sub.4 hydrocarbon radical with a straight or branched chain, R represents COOH, an esterified COOH group, a carboxylic amide group, OH, O-SO.sub.2 CH.sub.3, NH.sub.2, NHR.sub.1, NR.sub.1 R.sub.2, NHZOH, NHZNR.sub.1 R.sub.2, C(.dbd.NH)NH.sub.2, C(.dbd.NH)NHOH or 2-.DELTA..sup.2 -imidazolinyl, Z is a C.sub.2 -C.sub.4 hydrocarbon radical with a straight or branched chain, and R.sub.1 and R.sub.2 each represent a C.sub.1 -C.sub.
    Type: Grant
    Filed: April 5, 1977
    Date of Patent: May 22, 1979
    Assignee: Societe Anonyme dite: Laboratoire L. Lafon
    Inventors: Victor Lafon, Louis Lafon
  • Patent number: 4147790
    Abstract: Benzophenones of the formula ##STR1## wherein X.sub.1 is selected from the group consisting of hydrogen and alkyl of 1 to 5 carbon atoms, X.sub.2 is selected from the group consisting of hydrogen, halogen and alkoxy of 1 to 5 carbon atoms, m is a whole number from 1 to 10, n is a whole number from 2 to 5 and Y is in the 2,3 or 4-position and is selected from the group consisting of hydrogen, halogen, CF.sub.3 --, CF.sub.3 O--, CF.sub.3 S--, alkyl of 1 to 8 carbon atoms and alkoxy of 1 to 8 carbon atoms and their non-toxic, pharmaceutically acceptable acid addition salts having analgesic activity and their preparation.
    Type: Grant
    Filed: January 13, 1978
    Date of Patent: April 3, 1979
    Assignee: Roussel Uclaf
    Inventors: Andre Allais, Francois Clemence, Roger Deraedt
  • Patent number: 4147871
    Abstract: Compounds having the formula ##STR1## and the pharmaceutically acceptable salts thereof, wherein R.sub.1 is alkanoyl; R.sub.2 is alkyl; R.sub.3 is alkylamino, dialkylamino, a 1-piperazinyl group, 4-aryl-1,2,3,6-tetrahydro-1-pyridinyl, or N-alkyl-N-(pyridinylalkyl)amino; and n is 1, 2 or 3; have useful hypotensive activity.
    Type: Grant
    Filed: April 28, 1978
    Date of Patent: April 3, 1979
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Frederic P. Hauck, Rita T. Fox
  • Patent number: 4130646
    Abstract: Compounds having the structure ##STR1## and pharmaceutically acceptible salts thereof, wherein R.sub.1 is hydrogen, halogen, hydroxy, alkanoyloxy, alkoxy, alkylthio, alkyl, trifluoromethyl or methylenedioxy; R.sub.2 is hydrogen, halogen, alkyl, alkoxy, alkylthio, or trifluoromethyl; R.sub.3 is formyl or alkanoyl; m is 1 or 2; and n is 0, 1 or 2, have useful sedative and muscle relaxant activity, and can be used as tranquilizers.
    Type: Grant
    Filed: April 22, 1976
    Date of Patent: December 19, 1978
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: B. Richard Vogt, David A. Cullison
  • Patent number: 4128643
    Abstract: (2-Amino-4-quinazolinyl)-quanidines of the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and n have the defined meanings, and their physiologically tolerable acid addition salts, process for preparing these compounds, pharmaceutical preparations containing them and their use as medicines.
    Type: Grant
    Filed: May 26, 1977
    Date of Patent: December 5, 1978
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Wulf Merkel, Hans G. Alpermann, Karl Geisen, Norbert Kothe, Walter Ried
  • Patent number: 4122178
    Abstract: Piperazine compounds useful as analgesics, and having the formula: ##STR1## wherein each of R.sup.1 and R.sup.2 is hydrogen, halogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy or CF.sub.3 ; R.sup.3 is hydrogen, hydroxyl, an optionally substituted phenyl (e.g. phenyl, halo-phenyl, C.sub.1-4 alkyl-phenyl, C.sub.1-4 alkoxy-phenyl or CF.sub.3 -phenyl), pyridyl, 2-thienyl or 2-pyrimidinyl; m is 2 or 3; and n is 0, 1 or 2, and pharmaceutically acceptable acid addition salts thereof are disclosed.
    Type: Grant
    Filed: June 3, 1976
    Date of Patent: October 24, 1978
    Assignee: Yoshitomi Pharmaceutical Industries, Ltd.
    Inventors: Gen Hasegawa, Takanori Oe, Chiaki Kitami
  • Patent number: 4115100
    Abstract: This invention relates to the selective control of weeds and wild grasses in crops of useful plants by means of 2-pyridinol compounds of formula ##STR1## wherein A is an alkylene or alkenylene bridgeB is a group --OR.sub.1 or --SR.sub.2,R.sub.1 is alkyl, aralkyl, cycloalkyl, alkenyl, alkinyl or phenylR.sub.2 is alkyl, benzyl or phenylR.sub.3 is alkyl or phenyl andHal is chlorine or bromine,And to compositions therefor.
    Type: Grant
    Filed: February 28, 1977
    Date of Patent: September 19, 1978
    Assignee: Ciba-Geigy Corporation
    Inventors: Rolf Schurter, Hermann Rempfler, Werner Fory
  • Patent number: 4103094
    Abstract: Compounds having the formula ##STR1## and the pharmaceutically acceptable salts thereof, wherein R.sub.1 is alkanoyl; R.sub.2 is alkyl; R.sub.3 is alkylamino, dialkylamino, a 1-piperazinyl group, 4-aryl-1,2,3,6-tetrahydro-1-pyridinyl, or N-alkyl-N-(pyridinylalkyl)amino; and n is 1, 2 or 3; have useful hypotensive activity.
    Type: Grant
    Filed: May 10, 1977
    Date of Patent: July 25, 1978
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Frederic P. Hauck, Rita T. Fox
  • Patent number: 4101659
    Abstract: Benzhydryl derivatives of guanidine (Formula I) having blood sugar lowering activity; pharmaceutical hypoglycemic compositions thereof and methods of administering same to hyperglycemic individuals.
    Type: Grant
    Filed: August 29, 1977
    Date of Patent: July 18, 1978
    Assignee: McNeil Laboratories, Incorporated
    Inventor: Chris Royce Rasmussen
  • Patent number: 4101723
    Abstract: Compounds having the formula ##STR1## and the pharmaceutically acceptable salts thereof, wherein R.sub.1 is alkanoyl; R.sub.2 is aryl or pyridinyl; and n is 0, 1 or 2; have useful hypotensive properties.
    Type: Grant
    Filed: April 5, 1977
    Date of Patent: July 18, 1978
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Frederic P. Hauck, Rita T. Fox, John R. Watrous
  • Patent number: 4100282
    Abstract: Compounds of the formula ##STR1## wherein R is phenyl; phenyl having one or two substituents attached thereto, said substituents being selected from the group consisting of alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms, alkylthio of 1 to 4 carbon atoms, chlorine and trifluoromethyl; naphthyl; tetrahydronaphthyl; indanyl; pyridyl; isoquinolyl; or thiazolyl;R.sub.1 is ##STR2## where R.sub.3 is hydrogen, alkyl of 1 to 4 carbon atoms,R.sub.4 and R.sub.5 are each hydrogen or alkyl of 1 to 4 carbon atoms, andQ is oxygen or two hydrogens,R.sub.2 is hydrogen, alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms or halogen,A is a single carbon-to-carbon bond or --OCH.sub.2 --,R.sub.6 is hydrogen, hydroxyl, alkoxy of 1 to 4 carbon atoms or alkanoyloxy of 1 to 4 carbon atoms, andm is 0, 1, 2, 3, 4 or 5, but other than 0 when R.sub.
    Type: Grant
    Filed: May 4, 1977
    Date of Patent: July 11, 1978
    Assignee: Boehringer Ingelheim GmbH
    Inventors: Ernst-Otto Renth, Anton Mentrup, Kurt Schromm, Peter Danneberg
  • Patent number: 4093724
    Abstract: Novel 3-(4-quinolylamino)-2-thiophene-carboxylates of the formula ##STR1## wherein X is in the 6, 7 or 8-position and is selected from the group consisting of hydrogen, halogen, --CF.sub.3 and alkyl and alkoxy of 1 to 8 carbon atoms, n is 2, 3, 4 or 5, Y is in the 2, 3 or 4-position and is selected from the group consisting of hydrogen, halogen, --CF.sub.3 and alkyl and alkoxy of 1 to 8 carbon atoms and their non-toxic, pharmaceutically acceptable acid addition salts having analgesic activity and process and intermediates for their preparation.
    Type: Grant
    Filed: February 22, 1977
    Date of Patent: June 6, 1978
    Assignee: Roussel Uclaf
    Inventors: Andre Allais, Jean Meier, Roger Deraedt
  • Patent number: 4092416
    Abstract: Benzopyrones of the formula ##STR1## wherein R.sub.1 is a hydrogen or halogen atom or a hydroxyl, lower alkyl, alkoxy, alkylthio or trifluoromethyl radical,R.sub.2, r.sub.3, r.sub.4 and R.sub.5 each independently is hydrogen, a halogen atom, a hydroxyl radical, a lower alkyl or lower alkoxy radical, or a lower alkyl or lower alkoxy radical substituted by at least one of hydroxyl, halogen, mesyloxy or tosyloxy or by an oxirane, dioxane or dioxolane ring,A is a lower alkylene radical, andn is 0, 1 or 2,And salts thereof exhibit anti-allergic activity.
    Type: Grant
    Filed: December 1, 1976
    Date of Patent: May 30, 1978
    Assignee: Boehringer Mannheim GmbH
    Inventors: Werner Winter, Max Thiel, Kurt Stach, deceased, Androniki Roesch, by Werner Plattner, administrator, Wolfgang Schaumann