The Chalcogen, X, Is In A -c(=x)- Group Patents (Class 546/235)
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Patent number: 4438112Abstract: Prostanoids are described of the formulae ##STR1## (and the salts thereof) in which: X is cis or trans --CH.dbd.CH-- or CH.sub.2 CH.sub.2 --;R.sup.1 is C.sub.1-7 alkyl terminated by --COOR.sup.10 where R.sup.10 is H, C.sub.1-6 alkyl or aralkyl;Y is a saturated heterocyclic amino group; andR.sup.4 is aralkyl (in which the aryl portion is substituted by alkylthio, alkylsulphinyl, alkylsulphonyl, alkanoylamino, aroylamino, phenalkyl, aminosulphonyl, alkanoylaminosulphonyl, phenylsulphonyl, nitro, tetrazolyl, substituted phenyl or thienyl).These compounds inhibit blood platelet aggregation and have bronchodilatory action, and may be formulated for use as anti-asthmatics and antithrombotic agents.Type: GrantFiled: September 17, 1982Date of Patent: March 20, 1984Assignee: Glaxo Group LimitedInventors: Eric W. Collington, Peter Hallett, Christopher J. Wallis, John Bradshaw
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Patent number: 4410521Abstract: Compounds are described of the formula ##STR1## in which --COR.sup.1 is a complex ester or thioester group,W is alkylene,X is cis or trans --CH.dbd.CH or --CH.sub.2 CH.sub.2 --,n is 1 or 2,Y is a saturated heterocyclic amino group having 5-8 ring members, andR.sup.2 is unsubstituted or substituted phenylalkyl, thienylalkyl, naphthylalkyl or cinnamyl,and their salts and solvates.These compounds inhibit blood platelet aggregation and bronchoconstruction and may be formulated for use as antithrombotic and antiasthmatic agents.Type: GrantFiled: September 16, 1982Date of Patent: October 18, 1983Assignee: Glaxo Group LimitedInventors: Eric W. Collington, Peter Hallett, Christopher J. Wallis, Norman F. Hayes, John Bradshaw, Malcolm Carter
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Patent number: 4409213Abstract: Prostanoid compounds are described having the formula: ##STR1## where A is a cyclopentane ring, which is substituted by oxo and/or hydroxy or etherified hydroxy and may be saturated or unsaturated; X is --CH.dbd.CH-- or --(CH.sub.2).sub.2 --; R is alkyl having a terminal --COOH or ester group; and Y is amino or substituted amino, particularly heterocyclic amino.The compounds have bronchodilator activity and/or inhibit blood platelet aggregation.The preparation and pharmaceutical formulation of the compounds is also described.Type: GrantFiled: November 10, 1982Date of Patent: October 11, 1983Assignee: Glaxo Group LimitedInventors: Eric W. Collington, Harry Finch, Roger F. Newton, Christopher J. Wallis
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Patent number: 4409398Abstract: (1R,cis)-Oxyimino-substituted cyclopropanecarboxylic acids are prepared via a (1R,4R,5S)-4-acetoxy-6,6-dimethyl-2-oxo-3-oxabicyclo [3.1.0]hexane intermediate.Type: GrantFiled: August 13, 1981Date of Patent: October 11, 1983Assignee: Shell Oil CompanyInventor: Steven A. Roman
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Patent number: 4408053Abstract: Novel 3-(4-piperidyl)-1,2-benzisoxazoles, intermediates and processes for the preparation thereof, and methods for alleviating pain utilizing compounds or compositions thereof are disclosed.Type: GrantFiled: August 6, 1982Date of Patent: October 4, 1983Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: Joseph T. Strupczewski, Beth A. Gardner, Richard C. Allen
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Patent number: 4408054Abstract: Novel 3-(4-piperidyl)-1,2-benzisoxazoles, intermediates and processes for the preparation thereof, and methods for alleviating pain utilizing compounds or compositions thereof are disclosed.Type: GrantFiled: August 11, 1982Date of Patent: October 4, 1983Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: Joseph T. Strupczewski, Beth A. Gardner, Richard C. Allen
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Patent number: 4395553Abstract: Certain 1-(substituted amino)-2-(amino or substituted amino)cyclobutene-3,4-diones are potent histamine H.sub.2 -antagonists useful in the treatment of peptic ulcers.Type: GrantFiled: February 8, 1982Date of Patent: July 26, 1983Assignee: Bristol-Myers CompanyInventors: Aldo A. Algieri, Ronnie R. Crenshaw
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Patent number: 4390701Abstract: Certain 1-(substituted amino)-2-(amino or substituted amino)cyclobutene-3,4-diones are potent histamine H.sub.2 -antagonists useful in the treatment of peptic ulcers.Type: GrantFiled: May 18, 1981Date of Patent: June 28, 1983Assignee: Bristol-Myers CompanyInventors: Aldo A. Algieri, Ronnie R. Crenshaw
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Patent number: 4370335Abstract: 4-Diphenyl-1-[(oxo and oxo-related alkyl)imino]methyl-piperidine derivatives are disclosed which are useful for the inhibition of gastric acid secretion.Type: GrantFiled: February 2, 1982Date of Patent: January 25, 1983Assignee: McNeilab, Inc.Inventor: Malcolm K. Scott
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Patent number: 4368205Abstract: Disclosed are novel compounds of the formula ##STR1## wherein R.sup.1 is a heterocyclic radical selected from furanyl, thienyl, pyridyl, pyrimidyl, oxazolyl, pyrrolyl, isoxazolyl, thiazolyl, and isothiazolyl, and R.sup.2 is hydrogen, a tetramethylcylopropanecarbonyl group, a 1-(substituted-phenyl)-2-methylpropyl-1-carbonyl group, a 1-(4-ethoxyphenyl)-2-dichlorocyclopropanecarbonyl group, or a substituted-vinyl-cyclopropanecarbonyl group. The compounds wherein R.sup.2 is other than hydrogen are insecticides.Type: GrantFiled: September 17, 1981Date of Patent: January 11, 1983Assignee: FMC CorporationInventor: John F. Engel
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Patent number: 4349452Abstract: Anisotropic compounds of the formula (1) ##STR1## wherein X and Y are each hydrogen, C.sub.1 -C.sub.12 alkyl, C.sub.1 -C.sub.12 alkoxy, N-monoalkaylamine having 1 to 12 carbon atoms in the alkyl group, halogen, cyano, nitro, or a cyclic radical of the formula ##STR2## wherein R is hydrogen, halogen, cyano, nitro, C.sub.1 -C.sub.12 alkyl, or C.sub.1 -C.sub.12 alkoxy, Z.sup.1 is a --COO-- group or a --OOC-- group and Z.sup.2 may be the same as Z.sup.1 or a single convalent bond, with the proviso that:(a) only one of the groups X and Y is a cyclic radical, and(b) neither of the groups X or Y is hydrogen, bromine, or poperidino when the other is hydrogen, have low .DELTA.n-values without a greay tendency to form smectic phases and are useful in preparing liquid crystal devices.Type: GrantFiled: July 15, 1980Date of Patent: September 14, 1982Assignee: Merck Patent GmbHInventors: Maged A. Osman, Laszlo Revesz
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Patent number: 4342756Abstract: Compounds are described of the formula ##STR1## (and their salts and solvates) in which: X is cis or trans --CH.dbd.CH--;R.sup.1 is C.sub.1-7 alkyl terminated by --COOR.sup.3 where R.sup.3 is H, C.sub.1-6 alkyl or C.sub.7-10 aralkyl;Y is a saturated heterocyclic amino group having 5-8 ring members; andR.sup.2 is C.sub.2-4 alkanoyl, C.sub.3-6 alkenyl (optionally substituted), C.sub.1-12 alkyl, or substituted or unsubstituted phenylalkyl, biphenylalkyl or naphthylalkyl.These compounds inhibit blood platelet aggregation and bronchoconstriction and may be formulated for use as antithrombotic and anti-asthmatic agents.Type: GrantFiled: April 29, 1981Date of Patent: August 3, 1982Assignee: Glaxo Group LimitedInventors: Eric W. Collington, Peter Hallett, Christopher J. Wallis, John Bradshaw, Norman F. Hayes
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Patent number: 4339576Abstract: 1-[(3- or 4-Benzoylphenyl)-lower-alkyl]-[(CH.sub.2).sub.n --N.dbd.B]-substituted-piperidines, useful as anti-asthmatic, anti-allergic, anti-cholinergic, bronchodilator and anti-inflammatory agents, are prepared by alkylation of an appropriate substituted piperidine with a (3- or 4-benzoylphenyl)-lower-alkyl halide or tosylate; by reaction of a 1-[2-(3- or 4-lithiophenyl)-lower-alkyl]-[(CH.sub.2).sub.n --N.dbd.B]-substituted-piperidine with benzonitrile and hydrolysis of the resulting benzimidoyl compound; or by reduction of a 1-[.alpha.-(3- or 4-benzoylphenyl)-lower-alkanoyl]-[(CH.sub.2).sub.n --N.dbd.B]-substituted-piperidine. The analogous carbinols are prepared by reduction, with an alkali metal borohydride, of the ketone.Type: GrantFiled: August 24, 1981Date of Patent: July 13, 1982Assignee: Sterling Drug Inc.Inventor: Bernard L. Zenitz
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Patent number: 4303588Abstract: Novel farnesylacetic acid amide compounds represented by general formula ##STR1## wherein A is alkylene of at least 2 carbon atoms, R.sup.1 is H or lower alkyl, and R.sup.2 and R.sup.3 are each independently H, alkyl, cycloalkyl, alkenyl, aryl or aralkyl, or either one of R.sup.2 and R.sup.3 is such a group that forms, together with A, a piperidine or pyrrolidine ring which contains as constituent thereof the nitrogen atom lying therebetween, or R.sup.2 and R.sup.3 combinedly represent a group which forms, together with the nitrogen atom to which they are bonded, a piperidine, pyrrolidine or piperazine ring; and salts thereof have antiulcerogenic and antibacterial activities.Type: GrantFiled: March 21, 1980Date of Patent: December 1, 1981Assignee: Kuraray Co., Ltd.Inventors: Susumu Okabe, Yoshiaki Omura, Yoichi Ninagawa, Yoshiji Fujita
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Patent number: 4294841Abstract: A drug useful as antiarhythmic, antidepressant and anxiolytic containing as an active agent a compound of the formula ##STR1## wherein X and Y are the same or different and represent hydrogen or halogen atoms, or 1-4C alkyl groups, 1-4C alkoxy groups, 1-4C alkylthio groups, CF.sub.3, OH, NH.sub.2, 1-4C monoalkylamino or amino groups substituted by a 1-4C alkylsulfonyl group, a 1-5C alkylcarbonyl group or an aroyl group and A is a CO, CHOH or CH.sub.2 group, or a salt of said compound with a pharmaceutically acceptable acid, is disclosed together with methods for the preparation thereof and its use in human therapy.Type: GrantFiled: November 27, 1979Date of Patent: October 13, 1981Assignee: PharmindustrieInventors: Alain A. Champseix, Gerard R. Le Fur
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Patent number: 4289686Abstract: Compounds which contain, in their molecule, at least one 2-(2'-hydroxyphenyl)-benztriazole group or one 2-hydroxybenzophenone group and at least one polyalkylpiperidine group are effective light stabilizers for organic materials, in particular for polymers. The use of the compounds as light stabilizers for lacquers is of particular importance.Type: GrantFiled: September 17, 1979Date of Patent: September 15, 1981Assignee: Ciba-Geigy CorporationInventors: Jean Rody, Mario Slongo
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Patent number: 4267354Abstract: 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: GrantFiled: February 4, 1980Date of Patent: May 12, 1981Assignee: E. R. Squibb & Sons, Inc.Inventors: John Krapcho, Chester F. Turk
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Patent number: 4263202Abstract: Metal phenolates having at least one piperidinyl group sterically hindered on the nitrogen atom are suitable as additives for organic material.Type: GrantFiled: July 10, 1978Date of Patent: April 21, 1981Assignee: Ciba-Geigy CorporationInventors: Michael Rasberger, Samuel Evans, Paul Moser
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Patent number: 4248779Abstract: A thiolcarbamate having the formula ##STR1## wherein R.sub.1 and R.sub.2 are the same or different and respectively represent an alkyl, alkoxy, alkenyl, cycloalkyl, hydroxyalkyl, phenyl or benzyl group and R.sub.1 and R.sub.2 can form a ring by binding each other with or without oxygen atom; and R.sub.3 represents a lower alkyl or benzyl group or a substituted benzyl group having one or two substituent of halogen atom, alkyl, alkoxy, alkylthio, nitro, or cyano group, which comprises reacting carbonyl sulfide with a sec-amine having the formula ##STR2## wherein R.sub.1 and R.sub.2 are defined above, in an aqueous medium and then reacting a halogenated hydrocarbon having the formulaX--R.sub.3 (IV)wherein R.sub.3 is defined above and X represents a halogen atom, in an aqueous medium.Type: GrantFiled: October 4, 1978Date of Patent: February 3, 1981Assignee: Ihara Chemical Industry Company, LimitedInventors: Zenichi Sato, Fumiya Tabuchi, Keiichiro Takagi, Yoji Imamiya
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Patent number: 4244963Abstract: 1-[2-(Alkyl and arylsulfonyl)-2-propenyl and propyl] substituted piperidines of the formula: ##STR1## where A is ##STR2## and R.sub.1 -R.sub.5 are various substituents, are useful as antimicrobial and anti-inflammatory agents.Type: GrantFiled: September 27, 1979Date of Patent: January 13, 1981Assignee: Merck & Co., Inc.Inventors: Nathaniel Grier, Richard A. Dybas, Bruce E. Witzel
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Patent number: 4238613Abstract: Polyalkylpiperidinylesters and N-polyalkylpiperidinylamides of substituted malonic acids, methane tricarboxylic acids, .beta.-keto-, .alpha.-cyano-, .alpha.-phosphono- or .alpha.-sulfonocarboxylic acids are excellent stabilizers for polymers, especially against photochemical degradation. Polymers which can be stabilized in this way very effectively are polyolefins, styrene homo- and copolymers, polyamides and polyurethanes.Type: GrantFiled: October 13, 1978Date of Patent: December 9, 1980Assignee: Ciba-Geigy CorporationInventors: Michael Rasberger, Friedrich Karrer
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Patent number: 4226999Abstract: A compound of the formula I ##STR1## in which R.sub.2 is an optionally substituted 4-piperidinyl bonded via oxy or imino, or an optionally substituted 2-(piperidino)-ethoxy, n is 1 or 2, R.sub.7 and R.sub.8 are hydrocarbon radicals, R.sub.9 is hydrogen or methyl, R.sub.14 is cyano, --CH.sub.2 OH, a hydroxymethyl which is C-substituted by an optionally substituted 4-piperidinyl bonded via oxy or imino, or by an optionally substituted 2-(piperidino)-ethoxy, or R.sub.14 is also acyl or nitro, and, when n=1, R.sub.15 is hydrogen, a substituted hydroxybenzyl, an optionally substituted hydrocarbon radical, an optionally substituted 4-piperidinyl, or alkylene which is optionally linked to R.sub.14 and optionally substituted, or, when n=2, R.sub.15 is a direct bond or an optionally interrupted hydrocarbon radical, and its salts as stabilizers for organic material.Type: GrantFiled: January 5, 1979Date of Patent: October 7, 1980Assignee: Ciba-Geigy CorporationInventors: Roger Malherbe, Michael Rasberger
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Patent number: 4216335Abstract: Compounds having the formulas ##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: GrantFiled: April 25, 1979Date of Patent: August 5, 1980Assignee: E. R. Squibb & Sons, Inc.Inventors: John Krapcho, Chester F. Turk
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Patent number: 4177290Abstract: Novel acetamide derivatives have been discovered to have useful pharmaceutical activity on the central nervous system. They may be prepared by reacting the corresponding ester or acid halide with the appropriately substituted amine.Type: GrantFiled: March 9, 1978Date of Patent: December 4, 1979Assignee: Laboratoire L. LafonInventor: Louis Lafon
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Patent number: 4153609Abstract: A 3-indolyl-3-bis-aminophenyl-phthalide compound of the formula ##STR1## wherein R.sub.1 represents alkyl which has at most 12 carbon atoms and is unsubstituted or substituted by halogen, hydroxyl, cyano or lower alkoxy, cycloalkyl, or unsubstituted or substituted phenyl or benzyl wherein the substituents are halogen, nitro, lower alkyl or lower alkoxy,R.sub.2 represents hydrogen, alkyl which has at most 12 carbon atoms and is unsubstituted or substituted by halogen, hydroxyl, cyano or lower alkoxy, cycloalkyl, or benzyl which is unsubstituted or substituted by halogen, nitro, lower alkyl or lower alkoxy, orR.sub.1 and R.sub.2 together with the nitrogen atom linking them represent a 5- or 6-membered heterocyclic radical,X.sub.1 and X.sub.2 independently of one another represent hydrogen, lower alkyl, cycloalkyl, benzyl which is unsubstituted or substituted by halogen, nitro, lower alkyl or lower alkoxy, or acyl having 1 to 8 carbon atoms, and X.sub.Type: GrantFiled: January 10, 1977Date of Patent: May 8, 1979Assignee: Ciba-Geigy CorporationInventors: Jean C. Petitpierre, Robert Garner
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Patent number: 4148796Abstract: Novel .gamma.-piperidinobutyrophenone derivatives of the formula, ##STR1## wherein R.sup.1 is halogen, amino, alkanoylamino, alkylamino or N-(alkanoyl)alkylamino;R.sup.2 is hydrogen or halogen, provided that when R.sup.1 is halogen, R.sup.2 must be halogen; andZ is a piperidino group having the formula (A), ##STR2## (wherein each of R.sub.a and R.sub.b is hydrogen, halogen, lower alkyl, lower alkoxy or trifluoromethyl; R.sup.3 is hydrogen or hydroxyl; and n is 1 or 2), or a piperidino group having the formula (B), ##STR3## (wherein R.sub.c is hydrogen or lower alkyl; and each of R.sub.d and R.sub.e is hydrogen, halogen, lower alkyl or lower alkoxy), provided that when R.sup.1 is amino and R.sup.2 is hydrogen, Z cannot be represented by the formula (A), and their pharmaceutically acceptable acid addition salts, which are useful as psychotropic, neuroleptic or analgesic agents.Type: GrantFiled: August 15, 1973Date of Patent: April 10, 1979Assignee: Sumitomo Chemical Company, LimitedInventors: Hisao Yamamoto, Masaru Nakao, Kikuo Sasajima, Isamu Maruyama, Shigenari Katayama
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Patent number: 4146558Abstract: Water-soluble cationic dyestuffs of the formulae ##STR1## WHEREIN R.sup.0 is hydrogen, lower-alkyl or hydroxy-lower-alkyl;R.sup.1 is lower-alkyl, lower-alkenyl or hydroxy-lower-alkyl;R.sup.2 is lower-alkyl, lower-alkenyl, hydroxy-lower-alkyl or -(lower-alkylene)-NR.sup.0 Y or R.sup.1 and R.sup.2 together with the nitrogen atom, are pyrrolidino, piperidino or 4-lower-alkanoyl piperazino;Y is hydrogen or ##STR2## wherein R is hydrogen, lower-alkyl, lower-alkenyl, phenyl or phenyl-lower-alkyl;A is a member selected from the group consisting of an aromatic azo dyestuff residue attached to the quaternary ammonium nitrogen atom through a lower-alkylene bridge.K is a small integer whose value is dependent on the nature of A such that it has a range from one to two;R.sup.8 is lower-alkyl, lower-alkenyl or hydroxy-lower-alkyl;R.sup.9 is lower-alkyl, hydroxy-lower-alkyl or NH.sub.2 ;R.sup.10 is lower-alkyl or lower-alkenyl;A.sup.Type: GrantFiled: October 6, 1977Date of Patent: March 27, 1979Assignee: Sterling Drug Inc.Inventors: Patrick J. Jefferies, Nathan N. Crounse
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Patent number: 4146630Abstract: A 3-(4-phenoxymethylpiperidino)-propyl-phenyl-ether of the formula ##STR1## wherein R.sub.1 and R.sub.2 each independently is hydrogen, lower alkyl, hydroxyalkyl, lower alkanoyloxyalkyl or --CO--Z,Z is hydroxy, lower alkyloxy or ##STR2## R.sub.6 and R.sub.7 each independently is hydrogen, lower alkyl or hydroxyalkyl,R.sub.3 is hydrogen or --O--R.sub.8,R.sub.8 is hydrogen, lower alkanoyl or aroyl optionally substituted by halogen, lower alkyl, lower alkoxy, alkoxycarbonyl, hydroxyl, alkylthio, nitrile, nitro or trifluoromethyl,R.sub.4 and R.sub.5 each independently is hydrogen, halogen, hydroxy, benzyloxy, lower alkyl, lower alkoxy, lower alkylthio, carboxy, benzyloxycarbonyl or lower alkoxycarbonyl,X and Y each independently is nitrogen or ##STR3## R.sub.9 is hydrogen, lower allkyl optionally substituted by --O--R.sub.8, or --CO--Z,or a pharmacologically acceptable salt thereof. The compounds lower blood pressure and inhibit adrenergic .beta.-receptors.Type: GrantFiled: October 27, 1977Date of Patent: March 27, 1979Assignee: Boehringer Mannheim GmbHInventors: Wolfgang Kampe, Walter-Gunar Friebe, Fritz Wiedemann, Gisbert Sponer, Wolfgang Bartsch, Karl Dietmann
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Patent number: 4145426Abstract: Compounds of the structure: ##STR1## where A is either ##STR2## where R.sub.1 to R.sub.4 are various substituents are active as antibacterials and antifungals.Type: GrantFiled: July 18, 1977Date of Patent: March 20, 1979Assignee: Merck & Co., Inc.Inventors: Nathaniel Grier, Richard A. Dybas, Bruce E. Witzel
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Patent number: 4145362Abstract: A process for arylating an olefinic compound by addition of an aryl group to a double bond of said olefinic compound consisting in diazotizing an arylamine in an aqueous acidic solution comprising a lower alkanoic acid to form a solution of an aryldiazonium salt and reacting said aryldiazonium salt solution with an olefinic compound in an organic solvent in the presence of a catalytically effective amount of a copper halide.The amount of alkanoic acid is about 15 to 37% by volume of the total solvents used. The alkanoic acid is preferably acetic acid and the copper halide cuprous chloride.Type: GrantFiled: May 10, 1977Date of Patent: March 20, 1979Assignee: S.A. P R B en Neerlandais PRB N.V.Inventors: Joseph R. Brepoels, Jean-Marie Vaneghem
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Patent number: 4134983Abstract: Novel 3-amino-2-OR-propoxyaryl substituted imidazoles and methods for their preparation are disclosed. These imidazoles, and their salts, exhibit pharmacological activity which includes antihypertensive activity and .beta.-adrenergic blocking activity.Type: GrantFiled: December 17, 1975Date of Patent: January 16, 1979Assignee: Merck & Co., Inc.Inventor: John J. Baldwin