Ring Oxygen In The Bicyclo Ring System Patents (Class 546/115)
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4-phenyl-tetrahydro-furano-pyridines and anti-depressant pharmaceutical compositions containing same
Patent number: 4636510Abstract: The invention relates to 4-phenyl-tetrahydro-furano-pyridines of the formulas ##STR1## wherein R.sup.1 to R.sup.5 are variously defined. The compounds of the invention are intended to be used as anti-depressants with, in particular, thymoleptic and central-stimulant properties.Type: GrantFiled: April 19, 1984Date of Patent: January 13, 1987Assignee: Boehringer Ingelheim KGInventors: Claus Schneider, Gerhard Walther, Karl-Heinz Weber, Wolf D. Bechtel, Karin Boke-Kuhn -
Patent number: 4610990Abstract: The invention relates to new 5-(1-cyano-1-alkyl-N-methyl-N-methoxy-phenethyl)-alkylamino-2,2,8-trimethy l-4H-dioxino-(4,5-c)-pyridine derivatives of the formula ##STR1## and therapeutically acceptable salts of these compounds, to a preparation process of the same comprising reacting, in stoichiometric proportions, the corresponding 5-(1-cyano-1-R.sub.1)-methyl-2,2,8-trimethyl-4H-dioxino-(4,5-c)-pyridine of the formula ##STR2## on the appropriate [N-methyl-N-(methoxy-phenethyl)]-.omega.-alkyl chloride of the formula ##STR3## The invention relates also to therapeutic compositions containing said derivatives as active ingredients.Type: GrantFiled: October 3, 1985Date of Patent: September 9, 1986Assignee: Societe de Conseils de Recherches et d'Applications Scientifiques (S.C.R.A.S.)Inventor: Andre Esanu
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Patent number: 4593100Abstract: Disclosed herein are 4-phenyl-tetrahydro-isoxazolo[5,4-b]-pyridine-5-carboxylic acid esters of Formula I: ##STR1## wherein Ar is phenyl or phenyl substituted by a halogen, nitro, or trifluoromethyl group; R.sup.1 is C.sub.1-3 alkyl; and R.sup.2 is C.sub.1-5 alkyl, (C.sub.1-5) alkoxy (C.sub.1-3)-alkyl, or mono- or di(C.sub.1-5) alkylamino (C.sub.1-3)alkyl;or physiologically acceptable acid addition salts thereof. The compounds of the invention exhibit calcium antagonist and antihypertensive properties in standard pharmacological procedures.Type: GrantFiled: December 21, 1984Date of Patent: June 3, 1986Assignee: American Home Products CorporationInventor: Dong H. Kim
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Patent number: 4588733Abstract: 2-Phenylpyrano[2,3-b]pyridines are described herein. These compounds are active against a variety of viruses. A number of procedures can be used to prepare the compounds of this invention but, at some point, they would all make use of the cyclization of a (phenyl) (pyridyl)propanol or (phenyl) (pyridyl)propenol.Type: GrantFiled: October 19, 1984Date of Patent: May 13, 1986Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Thomas M. Bargar, John K. Daniel
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Patent number: 4572911Abstract: Hexahydroindolizines of the following formulae (I) and (II): ##STR1## are novel and have been found to possess antisecretory and antidepressant properties. Methods of preparation, intermediates thereto and use are also disclosed.Type: GrantFiled: August 2, 1984Date of Patent: February 25, 1986Assignee: McNeilab, Inc.Inventors: John R. Carson, Bruce E. Maryanoff
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Patent number: 4562201Abstract: The present invention relates to new compounds of the formula ##STR1## where X is ##STR2## alkylene, or --S-- where R.sub.1 is hydrogen, alkyl, or aryl; W is hydrogen, hydroxy, amino, alkyloxy, aryloxy, O-alkyl, or O-aralkyl; (Y).sub.A is --CH.sub.2 NR.sub.2 R.sub.3 where R.sub.2 and R.sub.3 may be hydrogen, substituted alkyls, aryls, or together with N form a 5 to 7 membered heterocyclic group; and Ar is a substituted or unsubstituted aryl. These compounds are useful in the treatment of various cardiac arrhythmias.Type: GrantFiled: July 26, 1982Date of Patent: December 31, 1985Assignee: American Hospital Supply CorporationInventors: David M. Stout, William L. Matier
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Patent number: 4555512Abstract: Dihydropyridines of the formula ##STR1## in which R.sup.1, R.sup.2, R.sup.5 and R.sup.6 can be hydrogen or various halogen or organic radicals,R.sup.4 is an optionally substituted hydrocarbon radical,A is a direct bond, a C.sub.1 -C.sub.20 -alkylene chain or a C.sub.2 -C.sub.20 -alkenylene chain, which chains are optionally interrupted by O or SX is O or S, andY is a direct bond, O, S, --NH--or--N-alkyl with 1 to 8 C atomsor a pharmaceutically acceptable salt,are useful as cardiotonic agents for improving heart contractility, antihypotonic agents, for lowering the blood sugar level, for detumescing mucous membranes and for influencing the salt and/or liquid balance.Type: GrantFiled: March 14, 1984Date of Patent: November 26, 1985Assignee: Bayer AktiengesellschaftInventors: Siegfried Goldmann, Friedrich Bossert, Matthias Schramm, Gunter Thomas, Rainer Gross
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Patent number: 4537963Abstract: Process for preparing analgesic and narcotic antagonistic isoquinolines comprising:(a) contacting and reacting a lithiated anisole or alkyl phenyl ether, optionally substituted at the 3-position to the lithium atom, with a 4-piperidone to yield a 4-aryl-4-piperidinol;(b) dehydrating the piperidinol to a 4-aryl-1,2,3,6-tetrahydropyridine;(c) metalating and acylating the 1,2,3,6-tetrahydropyridine to yield a 1-(4-aryl-1,2,3,4-tetrahydropyrid-4-yl)-4-hydroxy-1-butanone;(d) reducing the ketone moiety of the butanone to yield a 5-aryl-7-oxa-2-azabicyclo[3,2.1]-octane-6-propanol;(e) converting the alcohol moiety of the propanol to L to yield a 5-aryl-6-[3-(L)propyl]-7-oxa-2-azabicyclo[3.3.1]octane in which L is a leaving group selected from the group consisting of --Cl, --Br, --I, p--MeC.sub.6 H.sub.4 SO.sub.3 -- and MeSO.sub.3 --.Type: GrantFiled: August 11, 1983Date of Patent: August 27, 1985Assignee: E. I. Du Pont de Nemours and CompanyInventor: Ashokkumar B. Shenvi
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Patent number: 4517183Abstract: The present invention provides pharmaceutical compositions containing N-substituted aziridine-2-carboxylic acid derivatives of the general formula: ##STR1## wherein X is a carboxyl, a cyano, an alkoxycarbonyl or an optionally substituted carbamoyl radical, R is a hydrogen atom, an aliphatic hydrocarbon radical which is saturated or can contain one or more unsaturations and can be substituted one or more times by halogen, alkoxy, hydroxyl, dialkylamino, dialkylaminoxy, cycloalkylamino, acylamino, acyl, nitro, alkylthio, alkylsulphinyl, alkylsulphonyl, cyano, carboxyl, alkoxycarbonyl or carbamoyl or by cycloalkyl or cycloalkenyl radicals optionally carrying alkyl, alkoxy or alkoxycarbonyl radicals, optionally interrupted by hetero atoms and optionally bridged, or by an aryl, hetaryl, aryloxy, arylthio, acyloxy, alkoxycarbonylamino or isothioureido radical, or R is a cycloalkyl or cycloalkenyl radical optionally substituted by alkyl, alkoxy or oxo groups, optionally interrupted by hetero atoms and optionally briType: GrantFiled: May 17, 1983Date of Patent: May 14, 1985Assignee: Boehringer Mannheim GmbHInventors: Elmar Bosies, Wolfgang Kampe, Max Thiel, Uwe Bicker, Dietmar Boerner
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Patent number: 4482496Abstract: The invention relates to stilbene compounds of the formula ##STR1## wherein Q is hydrogen; a monocyclic 5- or 6-membered aromatic heterocyclic ring which is unsubstituted or substituted by non-chromophoric groups and which contains no fused benzene rings or one or two fused benzene rings; a bicyclic 9-membered aromatic heterocyclic ring or the radical --CH.dbd.C(R.sub.1)(R.sub.2), in which R.sub.1 is hydrogen, C.sub.1 -C.sub.6 alkyl which is unsubstituted or substituted by non-chromophoric groups, and R.sub.2 is alkoxycarbonyl containing altogether 2 to 7 carbons atoms, cyano, carboxyl, carbamoyl, phosphonic acid dialkyl ester, C.sub.1 -C.sub.6 alkyl or arylsulfonyl; or Q may also be ##STR2## R.sub.o is hydrogen or C.sub.1 -C.sub.6 alkyl, R is C.sub.1 -C.sub.6 alkyl which is unsubstituted or substituted by non-chromophoric groups, C.sub.2 -C.sub.5 alkenyl, C.sub.2 -C.sub.5 alkynyl, di(C.sub.1 -C.sub.4)alkylamino(C.sub.1 -C.sub.4)alkyl, C.sub.1 -C.sub.4 hydroxyalkyl, C.sub.1 -C.sub.Type: GrantFiled: June 1, 1982Date of Patent: November 13, 1984Assignee: Ciba-Geigy CorporationInventor: Kurt Weber
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Patent number: 4480098Abstract: Thienopyridines and furopyridines react at the 2-position with non-nucleophilic alkali metal bases to give alkali metal thieno(furo)pyridine salts.Type: GrantFiled: November 12, 1982Date of Patent: October 30, 1984Assignee: Eli Lilly and CompanyInventors: Richard E. Koehler, John A. Webber
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Patent number: 4477276Abstract: Compounds of the formula ##STR1## wherein R is halogen, CF.sub.3, NO.sub.2, CN, Alkyl or alkoxy, n is 0 to 3 X is O, S, NH or N-Alkyl, Y is O, S, SO, SO.sub.2, NH or N-Alkyl, R.sub.1 is H or alkyl and Z is carboxy or hydroxymethyl or functional derivatives of these groups, are valuable herbicides and growth regulators.Type: GrantFiled: September 22, 1982Date of Patent: October 16, 1984Assignee: Hoechst AktiengesellschaftInventors: Lothar Willms, Reinhard Handte, Hilmar Mildenberger, Klaus Bauer, Hermann Bieringer, Helmut Burstell
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Patent number: 4477671Abstract: Processes and intermediates useful in the preparation of bronchodilator compounds of the formula ##STR1## wherein R is hydrogen, methyl or hydroxymethyl are described. Those compounds wherein R is H or CH.sub.3 have been found to have further utility as intermediates for pirbuterol (wherein R is hydroxymethyl).Type: GrantFiled: June 2, 1983Date of Patent: October 16, 1984Assignee: Pfizer Inc.Inventors: Berkeley W. Cue, Stephen S. Massett
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Patent number: 4421916Abstract: Process for preparing analgesic and narcotic antagonistic isoquinolines comprising:(a) contacting and reacting a lithiated anisole or alkyl phenyl ether, optionally substituted at the 3-position to the lithium atom, with a 4-piperidone to yield a 4-aryl-4-piperidinol;(b) dehydrating the piperidinol to a 4-aryl-1,2,3,6-tetrahydropyridine;(c) metalating and acylating the 1,2,3,6-tetrahydropyridine to yield a 1-(4-aryl-1,2,3,4-tetrahydropyrid-4-yl)-4-hydroxy-1-butanone;(d) reducing the ketone moiety of the butanone to yield a 5-aryl-7-oxa-2-azabicyclo[3.2.1]-octane-6-propanol;(e) converting the alcohol moiety of the propanol to L to yield a 5-aryl-6-[3-(L)propyl-7-oxa-2-azabicyclo[3.2.1]octane in which L is a leaving group selected from the group consisting of --Cl, --Br, --I, p-MeC.sub.6 H.sub.4 SO.sub.3 -- and MeSO.sub.3 --.Type: GrantFiled: December 28, 1981Date of Patent: December 20, 1983Assignee: E. I. Du Pont de Nemours & Co.Inventor: Ashokkumar B. Shenvi
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Patent number: 4410532Abstract: A 2-cyanaziridine derivative of the formula ##STR1## wherein R' is a straight-chained or branched, saturated or mono- or polyunsaturated aliphatic hydrocarbon radical with up to 8 carbon atoms, which is substituted by an aromatic nitrogen-containing heterocyclic radical with 5 or 6 ring-members and 1, 2 or 3 nitrogen atoms optionally substituted by halogen, alkoxy with up to 8 carbon atoms, alkyl with up to 8 carbon atoms, hydroxyl, carbalkoxy with up to 9 carbon atoms, carbamoyl, dialkylamino the alkyl moieties of which having up to 8 carbon atoms, cycloalkylamino, the cycloalkyl moiety having 3-10 carbon atoms, acetylamino, nitro, cyano, acetyl, alkylthio with up to 8 carbon atoms, alkylsulphinyl with up to 8 carbon atoms, alkylsulphonyl with up to 8 carbon atoms, sulphamoyl, phenyl, trifluoromethyl, phenoxy, acetoxy or methylenedioxy;or a pharmacologically acceptable salt thereof, exhibits immune stimulating activity.Type: GrantFiled: December 28, 1981Date of Patent: October 18, 1983Assignee: Boehringer Mannheim GmbHInventors: Elmar Bosies, Herbert Berger, Wolfgang Kampe, Uwe Bicker, Alfred Grafe
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Patent number: 4387231Abstract: Process for the production of 4,6-diamino-5-cyano-3-aryl-isoxazole [5,4-b] pyridines having the formula: ##STR1## wherein (a) R.sup.1 and R.sup.2 are --H or (b) R.sup.1 is --Cl and R.sup.2 is --H, or (c) R.sup.1 is --CH.sub.3 and R.sup.2 is --H or (d) R.sup.1 is --NO.sub.2 and R.sup.2 is --H, or (e) R.sup.1 is --H and R.sup.2 is --NO.sub.2. 2-Amino-1-propane-1,1,3-tricarbonitrile having the formula: ##STR2## is reacted with a benzohydroxamino acid chloride having the formula: ##STR3## wherein R.sup.1 and R.sup.2 have the same meaning as above, in the presence of a strong base in at least a molar quantity.Type: GrantFiled: November 18, 1981Date of Patent: June 7, 1983Assignee: Lonza Ltd.Inventors: Hans Junek, Burkhard Thierrichter
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Patent number: 4375544Abstract: Aromatic-.alpha.-halo-{b} fused pyridines are made by reacting an aromatic acetamide, acid halide and amide in particular proportions, with the acid halide always in excess. The process permits the production of compounds having a wide range of substituents, that are new compounds, and that are of value as intermediates in the synthesis of, for instance, pharmaceutical compounds.Type: GrantFiled: June 8, 1979Date of Patent: March 1, 1983Assignee: Croda Synthetic Chemicals LimitedInventors: Otto Meth-Cohn, Brahma Narine
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Patent number: 4374841Abstract: Novel pyridoxine derivatives represented by the general formula: ##STR1## in which: R represents a radical ##STR2## --CH.sub.2 --(CH.sub.2).sub.n --CH.sub.2 --OR.sub.2 or ##STR3## in which n represents 0 or 1, X and X.sub.1, which are different, represent hydrogen or methyl, Y represents hydrogen or methyl and R.sub.2 represents a phenyl group non-substituted or bearing one or two substituents selected from the group consisting of fluorine, chlorine and bromine and of the radicals methyl, ethyl, n-propyl, isopropyl and methoxy,R.sub.1 represents hydrogen or a radical of formula ##STR4## in which R.sub.3 represents a straight-chain alkyl radical having from 1 to 4 carbon atoms and pharmaceutically acceptable acid addition salts thereof.These compounds present .alpha.-antiadrenergic properties some of them also presenting .beta.-antiadrenergic, antihypertensive and central depressant effects.Type: GrantFiled: May 11, 1981Date of Patent: February 22, 1983Assignee: S. A. Labaz N.V.Inventors: Marcel Descamps, Marcel Urbain, deceased, Claire Urbain, legal representative, Jacques J. Z. Urbain, legal representative, Jean P. M. C. Urbain, legal representative, Nadine C. J. Urbain, legal representative
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Patent number: 4350815Abstract: Process for the production of 4,6-diamino-5-cyano-3-aryl-isoxazole [5,4-b] pyridines having the formula: ##STR1## wherein (a) R.sup.1 and R.sup.2 are --H or (b) R.sup.1 is --Cl and R.sup.2 is --H, or (c) R.sup.1 is --CH.sub.3 and R.sup.2 is --H or (d) R.sup.1 is --NO.sub.2 and R.sup.2 is --H, or (e) R.sup.1 is --H and R.sup.2 is --NO.sub.2. 2-Amino-1-propane-1,1,3-tricarbonitrile having the formula: ##STR2## is reacted with a benzohydroxamino acid chloride having the formula: ##STR3## wherein R.sup.1 and R.sup.2 have the same meaning as above, in the presence of a strong base in at least a molar quantity.Type: GrantFiled: November 21, 1980Date of Patent: September 21, 1982Assignee: Lonza Ltd.Inventors: Hans Junek, Burkhard Thierrichter
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Patent number: 4329459Abstract: The present invention provides novel 8-heteroaryltetrahydrobenzopyrans and analogs thereof. These novel compounds are useful as inhibitors of endoperoxide cyclooxygenase which prevents the conversion of unsaturated fatty acids to endoperoxides. Because of this pharmacological activity, these compounds represent potent platelet aggregation inhibitors.Type: GrantFiled: May 5, 1980Date of Patent: May 11, 1982Assignee: The Upjohn CompanyInventor: John M. McCall
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Patent number: 4291042Abstract: Compounds of formula: ##STR1## and pharmaceutically acceptable acid addition or quaternary ammonium salts thereof wherein the piperidine ring is substituted in the 3 or 4 position; X represents .dbd.CH-- or .dbd.N--; Y represents --NR.sup.5 --, --O-- or --S-- wherein R.sup.5 is hydrogen or lower alkyl; A is lower alkylene or hydroxy lower alkylene, Z and Z.sup.1 independently represent ##STR2## Z may also represent --CH.sub.2 --, --(CH.sub.2).sub.2 --, --CHMe-- or --CMe.sub.2 --; R.sup.1, R.sup.2, R.sup.3 independently represent hydrogen, halogen, lower alkyl, lower alkoxy, nitro, amino, lower alkylamino, trifluoromethyl, lower-alkanoylamino, hydroxy or aryl lower alkoxy; or R.sup.1 and R.sup.2 when adjacent together with the carbons to which they are attached form a six membered carbocyclic ring; and R.sup.4 represents hydrogen or lower alkyl, are disclosed which possess psychotropic activity and are useful as anti-depressants.Type: GrantFiled: January 21, 1980Date of Patent: September 22, 1981Assignee: John Wyeth & Brother LimitedInventor: Terence J. Ward
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Patent number: 4284778Abstract: Novel nitrogen-containing heterocyclic compounds shown by the formula ##STR1## wherein one of R.sub.1 and R.sub.2 represents a lower alkyl group, a phenyl group, a halophenyl group, or a lower alkoxyphenyl group and the other of them represents a hydrogen atom, a lower alkyl group, or a phenyl lower alkyl group; said R.sub.1 and R.sub.2 may combine with each other to form a trimethylene group or a tetramethylene group; R.sub.3 represents a hydrogen atom, a lower alkyl group, a phenyl group, or a phenyl lower alkyl group; X represents an oxygen atom, a sulfur atom, an imino group, or a group shown by ##STR2## wherein m represents 1 or 2 and R.sub.4 represents a lower alkyl group, a hydroxy lower alkyl group, a cycloalkyl group or a phenyl lower alkyl group; and Y represents an ethylene group which may be substituted by a lower alkyl group, a trimethylene group, a tetramethylene group, a vinylene group which may be substituted by lower alkyl group, or ##STR3## wherein R.sub.Type: GrantFiled: August 20, 1979Date of Patent: August 18, 1981Assignee: Yamanouchi Pharmaceutical Co., Ltd.Inventors: Kazuo Kubo, Noriki Ito, Isao Souzu, Yasuo Isomura, Hiroshige Homma, Masuo Murakami
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Patent number: 4275206Abstract: Chromogenic compounds of normally colorless form are disclosed having the following structural formula: ##STR1## wherein E represents a six-membered aromatic or heterocyclic ring which may have an aromatic ring or a naphthalene ring and both the E ring and the condensed ring may be substituted, A respresents an optionally substituted aminophenyl, indolyl, benzoindolyl, julolidinyl or kairolyl radical or the radical represented by B, and B represents a family of indolizine radicals. The compounds of this invention are eligible for use in pressure-sensitive and heat-sensitive record materials and manifold marking systems.Type: GrantFiled: January 16, 1980Date of Patent: June 23, 1981Assignee: Appleton Papers Inc.Inventors: William J. Becker, Sheldon Farber, Troy E. Hoover
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Alkoxypyridyl N-cyano or N-carbamoylguanidino alkanes, compositions containing same and uses thereof
Patent number: 4269844Abstract: The compounds are C.sub.2 -C.sub.8 straight chain alkanes terminally substituted, symmetrically or unsymmetrically, by N-(N'-substituted guanidino), N-(N',N"-disubstituted guanidino), N-(N'-substituted thioureido), N-(nitromethylene amidino) or S-(N-substituted isothioureido)groups. Two compounds of the invention are 1,3-bis-[N'-(2-(3-methoxy-2-pyridylmethylthio)ethyl)guanidino]propane and 1-[N-(2-(3-methoxy-pyridylmethylthio)ethyl)guanidino]-3-[N'-2-(5-methyl-4- imidazolylmethylthio)ethyl)guanidino]propane. The compounds of this invention are inhibitors of H-2 histamine receptors.Type: GrantFiled: November 26, 1979Date of Patent: May 26, 1981Assignee: Smith Kline & French Laboratories LimitedInventors: Graham J. Durant, Charon R. Ganellin, George S. Sach -
Patent number: 4264608Abstract: the compounds are alkoxypyridine compounds which are histamine H.sub.2 -antagonists. Two specific compounds of the present invention are N-cyano-N'-methyl-N"-[2-((3-methoxy-2-pyridyl)methylthio)ethyl]guanidine and 1-methylamino-1-[2-((3-methoxy-2-pyridyl)methylthio)ethyl-amino]-2-nitroet hylene.Type: GrantFiled: November 15, 1979Date of Patent: April 28, 1981Assignee: Smith Kline & French Laboratories LimitedInventors: Graham J. Durant, Charon R. Ganellin, George S. Sach
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Patent number: 4246269Abstract: The present invention provides new derivatives of perhydro-aza-heterocycles of the formula ##STR1## in which X is the oxo radical or hydrogen and the radical OR.sub.1, in which R.sub.1 is hydrogen or a substituted or unsubstituted aliphatic hydrocarbon radical, a substituted or unsubstituted araliphatic hydrocarbon radical or a substituted or unsubstituted aromatic hydrocarbon radical or an acyl radical, R.sub.2 is hydrogen or a substituted or unsubstituted aliphatic hydrocarbon radical, Y is oxygen or sulphur, n.sub.1 and n.sub.2 each are values of 1 to 3, n.sub.1 +n.sub.2 being at most four, and Ar is a substituted or unsubstituted aromatic hydrocarbon radical, and the acid addition salts, in particular the pharmaceutically acceptable acid addition salts thereof. These new substances possess valuable pharmacological properties, in particular antidepressant activity, and can be used for the treatment of mental depressions.Type: GrantFiled: April 5, 1979Date of Patent: January 20, 1981Assignee: Ciba-Geigy CorporationInventor: Romeo Paioni
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Patent number: 4244957Abstract: 2-Imino-imidazolidine derivatives of the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are as hereinafter set forth, and pharmaceutically acceptable acid addition salts thereof, are described. The 2-imino-imidazolidine derivatives are useful in the treatment of hypertension.Type: GrantFiled: November 6, 1978Date of Patent: January 13, 1981Assignee: Hoffman-La Roche Inc.Inventor: Henri Ramuz
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Patent number: 4215126Abstract: The compounds are alkoxypyridine compounds which are histamine H.sub.2 -antagonists. Two specific compounds of the present invention are N-cyano-N'-methyl-N"-[2-((3-methoxy-2-pyridyl)methylthio)ethyl]guanidine and 1-methylamino-1-[2-((3-methoxy-2-pyridyl)methylthio)ethylamino]-2-nitroeth ylene.Type: GrantFiled: February 21, 1979Date of Patent: July 29, 1980Assignee: Smith Kline & French Laboratories LimitedInventors: Graham J. Durant, Charon R. Ganellin, George S. Sach
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Patent number: 4212976Abstract: Mercaptoalkylpyridines and various derivatives thereof have utility in the treatment of rheumatoid arthritis. The compounds useful in the method of treatment are generally prepared from known pyridine derivatives and, principally, from pyridoxine and related compounds.Type: GrantFiled: September 20, 1977Date of Patent: July 15, 1980Assignee: Merck & Co., Inc.Inventors: Tsung-Ying Shen, Howard Jones, Dennis M. Mulvey, Conrad P. Dorn
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Patent number: 4139624Abstract: The compounds are C.sub.2 -C.sub.8 straight chain alkanes terminally substituted, symmetrically or unsymmetrically, by N-(N'-substituted guanidino), N-(N',N"-disubstituted guanidino), N-(N'-substituted thioureido), N-(nitromethylene amidino) or S-(N-substituted isothioureido)groups. Two compounds of the invention are 1,3-bis-[N'-(2-(3-methoxy-2-pyridylmethylthio)ethyl)guanidino]propane and 1-[N-(2-(3-methoxy-pyridylmethylthio)ethyl)guanidino]-3-(N'-2-(5-methyl-4- imidazolylmethylthio)ethyl)guanidino]propane. The compounds of this invention are inhibitors of H-2 histamine receptors.Type: GrantFiled: July 18, 1977Date of Patent: February 13, 1979Assignee: SmithKline & French Laboratories LimitedInventors: Graham J. Durant, Charon R. Ganellin, George S. Sach
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Patent number: 4132710Abstract: [2]Benzopyrano[3,4-c]pyridine derivatives characterized by having a 2,3,4,4a,6,10b-hexahydro-1H-[2]benzopyrano[3,4-c]pyridine nucleus bearing a substituent at position 6 are disclosed. The nucleus can be optionally further substituted at positions 2,3,4,6 and on the aromatic ring. The derivatives are useful diuretic, anorexic, antidepressant, anticonvulsant and antihypertensive agents. Methods for their preparation and use also are disclosed.Type: GrantFiled: December 20, 1976Date of Patent: January 2, 1979Assignee: Ayerst, McKenna and Harrison, Ltd.Inventors: Jean A. Gauthier, Leslie G. Humber, Clara Revesz
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Patent number: 4131677Abstract: The various isomers of oxazolo- and thiazolopyridines having utility as antiinflammatory, antipyretic and analgesic agents are prepared by condensation of an appropriate amino-hydroxypyridine or amino-mercaptopyridine with a carboxylic acid, halide or anhydride.Type: GrantFiled: April 27, 1977Date of Patent: December 26, 1978Assignee: Merck & Co., Inc.Inventors: Tsung-Ying Shen, Robert L. Clark, Arsenio A. Pessolano, Bruce E. Witzel, Thomas J. Lanza
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Patent number: 4124714Abstract: This disclosure describes novel compounds of the formula: ##STR1## where R.sub.3 is hydrogen or halo having an atomic weight of about 19 to 36, which are useful as minor tranquilizers, sleep inducers, muscle relaxants, neuroleptics and anti-ulcer agents.Type: GrantFiled: August 5, 1977Date of Patent: November 7, 1978Assignee: Sandoz, Inc.Inventor: Jeffrey Nadelson