The Other Ring Nitrogen Has A Substituent Which Includes Chalcogen Single Bonded To Acyclic Carbon Patents (Class 544/394)
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Patent number: 4576943Abstract: 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: GrantFiled: October 9, 1984Date of Patent: March 18, 1986Assignee: American Cyanamid CompanyInventors: Andrew S. Tomcufcik, Walter E. Meyer, John P. Dusza, Shin S. Tseng
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Patent number: 4515793Abstract: 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: GrantFiled: July 27, 1983Date of Patent: May 7, 1985Assignee: Edna McConnell Clark FoundationInventors: Leslie M. Werbel, Norman Colbry, William Turner, Donald F. Worth
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Patent number: 4495350Abstract: 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: GrantFiled: September 13, 1982Date of Patent: January 22, 1985Assignee: Ciba-Geigy CorporationInventors: Dieter Durr, Otto Rohr, Beat Bohner
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Patent number: 4459410Abstract: 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: GrantFiled: October 5, 1981Date of Patent: July 10, 1984Assignee: Sumitomo Chemical Company, LimitedInventors: Keiichi Ono, Hajime Kawakami, Junki Katsube
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Patent number: 4438268Abstract: 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: GrantFiled: September 14, 1981Date of Patent: March 20, 1984Inventors: Horst Zaschke, Wolfgang Schafer, Hans-Joachim Deutscher, Dietrich Demus, Gerhard Pelzl
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Patent number: 4411904Abstract: Compounds of the formula ##STR1## where X and Y are hydrogen, halogen, lower alkyl, nitro are useful as neuroleptics.Type: GrantFiled: June 14, 1982Date of Patent: October 25, 1983Assignee: Warner-Lambert CompanyInventor: Ian C. Pattison
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Patent number: 4404384Abstract: 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: GrantFiled: May 28, 1981Date of Patent: September 13, 1983Assignee: Hoechst AktiengesellschaftInventors: Ulrich Gebert, Werner Thorwart, Jaromir Komarek, Carl Cartheuser
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Patent number: 4372958Abstract: 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: GrantFiled: June 10, 1981Date of Patent: February 8, 1983Assignee: A. Menarini S.A.S.Inventors: Vittorio Pestellini, Mario Ghelardoni, Danilo Giannotti, Alberto Meli, Carlo A. Maggi
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Patent number: 4370330Abstract: 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: GrantFiled: October 5, 1981Date of Patent: January 25, 1983Assignee: Merz & CompanyInventors: Arthur Scherm, Dezsoe Peteri
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Patent number: 4370329Abstract: 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: GrantFiled: August 22, 1980Date of Patent: January 25, 1983Assignee: Merz & CompanyInventors: Arthur Scherm, Dezsoe Peteri
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Patent number: 4364954Abstract: Compounds of the formula ##STR1## where X and Y are hydrogen, halogen, lower alkyl, nitro are useful as neuroleptics.Type: GrantFiled: May 29, 1981Date of Patent: December 21, 1982Assignee: Warner-Lambert CompanyInventor: Ian C. Pattison
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Patent number: 4358450Abstract: 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: GrantFiled: August 6, 1979Date of Patent: November 9, 1982Assignee: Hoechst AktiengesellschaftInventors: Ulrich Gebert, Ernold Granzer, Heinz-Gunter Greve, Werner Thorwart
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Patent number: 4357332Abstract: 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: GrantFiled: May 5, 1980Date of Patent: November 2, 1982Assignee: Pfizer Inc.Inventors: Allen R. Kraska, Joseph G. Lombardino
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Patent number: 4342762Abstract: 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: GrantFiled: December 11, 1980Date of Patent: August 3, 1982Assignee: Egyt Gyogyszervegyeszeti GyarInventors: Zoltan Budai, Laszlo Magdanyi, Aranka Lay nee Konya, Tibor Mezei, Katalin Grasser, Lujza Petocz, Ibolya Kosoczky
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Patent number: 4339580Abstract: Piperazinylalkoxyindanes and their pharmaceutically acceptable acid addition salts which have anti-anxiety activity and are effective as sedatives.Type: GrantFiled: June 9, 1980Date of Patent: July 13, 1982Assignee: Mitsubishi Chemical Industries, LimitedInventors: Ryoji Kikumoto, Akihiro Tobe, Harukazu Fukami, Mitsuo Egawa
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Patent number: 4336382Abstract: 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: GrantFiled: August 25, 1980Date of Patent: June 22, 1982Assignee: Hoffmann-La Roche Inc.Inventors: Kenneth E. Fahrenholtz, Robert W. Guthrie, Richard W. Kierstead, Jefferson W. Tilley
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Patent number: 4335126Abstract: 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: GrantFiled: October 3, 1980Date of Patent: June 15, 1982Assignee: Degussa AktiengesellschaftInventors: Axel Kleemann, Vladimir Jakovlev, Klaus Thiemer, Jurgen Engel
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Patent number: 4312877Abstract: 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: GrantFiled: October 31, 1980Date of Patent: January 26, 1982Assignee: Pfizer Inc.Inventor: Allen R. Kraska
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Patent number: 4308266Abstract: The present invention provides tetraline derivatives, useful for the treatment of hypertension, a process for their preparation and compositions containing these compounds.Type: GrantFiled: September 7, 1979Date of Patent: December 29, 1981Assignee: Sandoz Ltd.Inventor: Max-Peter Seiler
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Patent number: 4292321Abstract: 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: GrantFiled: January 10, 1980Date of Patent: September 29, 1981Assignee: Warner-Lambert CompanyInventor: Ian C. Pattison
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Patent number: 4271161Abstract: 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: GrantFiled: July 9, 1979Date of Patent: June 2, 1981Assignee: HexachimieInventor: Jean M. Teulon
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Patent number: 4267328Abstract: 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: GrantFiled: July 27, 1979Date of Patent: May 12, 1981Assignee: SynthelaboInventors: Henry Najer, Philippe Manoury
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Patent number: 4255426Abstract: 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: GrantFiled: July 9, 1979Date of Patent: March 10, 1981Assignee: Pfizer Inc.Inventor: Allen R. Kraska
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Patent number: 4255575Abstract: 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: GrantFiled: May 4, 1979Date of Patent: March 10, 1981Assignee: Richardson-Merrell Inc.Inventors: J. Martin Grisar, George P. Claxton
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Patent number: 4252804Abstract: 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: GrantFiled: January 13, 1978Date of Patent: February 24, 1981Assignee: Metabio-JoullieInventors: Maurice Joullie, Gabriel Maillard, Lucien Lakah, Christian J. M. Warolin
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Patent number: 4247710Abstract: 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: GrantFiled: September 6, 1979Date of Patent: January 27, 1981Assignee: Hoffmann-La Roche Inc.Inventors: Kenneth E. Fahrenholtz, Robert W. Guthrie, Richard W. Kierstead, Jefferson W. Tilley
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Patent number: 4242343Abstract: 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: GrantFiled: June 15, 1979Date of Patent: December 30, 1980Assignee: SynthelaboInventors: Henry Najer, Philippe Manoury
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Patent number: 4216326Abstract: 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: GrantFiled: May 3, 1978Date of Patent: August 5, 1980Assignee: Sterling Drug Inc.Inventor: Bernard L. Zenitz
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Patent number: 4202978Abstract: 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: GrantFiled: February 8, 1978Date of Patent: May 13, 1980Assignee: Hoffmann-La Roche Inc.Inventors: Kenneth E. Fahrenholtz, Robert W. Guthrie, Richard W. Kierstead, Jefferson W. Tilley
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Patent number: 4191765Abstract: 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: GrantFiled: August 10, 1978Date of Patent: March 4, 1980Assignee: Hoechst AktiengesellschaftInventors: Werner Fritsch, Ulrich Stache, Ernst Lindner
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Patent number: 4156011Abstract: 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: GrantFiled: April 5, 1977Date of Patent: May 22, 1979Assignee: Societe Anonyme dite: Laboratoire L. LafonInventors: Victor Lafon, Louis Lafon
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Patent number: 4147790Abstract: 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: GrantFiled: January 13, 1978Date of Patent: April 3, 1979Assignee: Roussel UclafInventors: Andre Allais, Francois Clemence, Roger Deraedt
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Patent number: 4147871Abstract: 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: GrantFiled: April 28, 1978Date of Patent: April 3, 1979Assignee: E. R. Squibb & Sons, Inc.Inventors: Frederic P. Hauck, Rita T. Fox
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Patent number: 4130646Abstract: 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: GrantFiled: April 22, 1976Date of Patent: December 19, 1978Assignee: E. R. Squibb & Sons, Inc.Inventors: B. Richard Vogt, David A. Cullison
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Patent number: 4128643Abstract: (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: GrantFiled: May 26, 1977Date of Patent: December 5, 1978Assignee: Hoechst AktiengesellschaftInventors: Wulf Merkel, Hans G. Alpermann, Karl Geisen, Norbert Kothe, Walter Ried
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Patent number: 4122178Abstract: 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: GrantFiled: June 3, 1976Date of Patent: October 24, 1978Assignee: Yoshitomi Pharmaceutical Industries, Ltd.Inventors: Gen Hasegawa, Takanori Oe, Chiaki Kitami
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Patent number: 4115100Abstract: 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: GrantFiled: February 28, 1977Date of Patent: September 19, 1978Assignee: Ciba-Geigy CorporationInventors: Rolf Schurter, Hermann Rempfler, Werner Fory
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Patent number: 4103094Abstract: 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: GrantFiled: May 10, 1977Date of Patent: July 25, 1978Assignee: E. R. Squibb & Sons, Inc.Inventors: Frederic P. Hauck, Rita T. Fox
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Patent number: 4101659Abstract: Benzhydryl derivatives of guanidine (Formula I) having blood sugar lowering activity; pharmaceutical hypoglycemic compositions thereof and methods of administering same to hyperglycemic individuals.Type: GrantFiled: August 29, 1977Date of Patent: July 18, 1978Assignee: McNeil Laboratories, IncorporatedInventor: Chris Royce Rasmussen
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Patent number: 4101723Abstract: 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: GrantFiled: April 5, 1977Date of Patent: July 18, 1978Assignee: E. R. Squibb & Sons, Inc.Inventors: Frederic P. Hauck, Rita T. Fox, John R. Watrous
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Patent number: 4100282Abstract: 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: GrantFiled: May 4, 1977Date of Patent: July 11, 1978Assignee: Boehringer Ingelheim GmbHInventors: Ernst-Otto Renth, Anton Mentrup, Kurt Schromm, Peter Danneberg
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Patent number: 4093724Abstract: 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: GrantFiled: February 22, 1977Date of Patent: June 6, 1978Assignee: Roussel UclafInventors: Andre Allais, Jean Meier, Roger Deraedt
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Patent number: 4092416Abstract: 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: GrantFiled: December 1, 1976Date of Patent: May 30, 1978Assignee: Boehringer Mannheim GmbHInventors: Werner Winter, Max Thiel, Kurt Stach, deceased, Androniki Roesch, by Werner Plattner, administrator, Wolfgang Schaumann