The Chalcogen Is In An -oh Or -om Group (m Is Group Ia Or Group Iia Light Metal) Patents (Class 546/344)
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Patent number: 4338316Abstract: The disclosure relates to 9.beta.-aryloxy prostane derivatives, for example 16-(3-chlorophenoxy)-11.alpha.,15.alpha.-dihydroxy-16-methyl-9.beta.-pheno xy-18,19,20-trinor-5-cis,13-trans-prostadienoic acid, which possess high activity as abortifacients, cervical softeners, inducers of parturition or inhibitors of gastric acid production in mammals. These properties are typical of prostaglandin analogues of the E series, but chemically the new 9.beta.-aryloxy prostane derivatives are prostaglandin F series analogues and are therefore more stable than the E series analogues previously used for the above purposes. The new derivatives are manufactured by known analogy processes, and are formulated in conventional manner.Type: GrantFiled: September 26, 1979Date of Patent: July 6, 1982Assignee: Imperial Chemical Industries LimitedInventor: Peter R. Marsham
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Patent number: 4332967Abstract: This invention relates to the following:(1) An amino-containing composition characterized by polymercapto groups,(2) A polyamino-containing composition characterized by mercapto or polymercapto groups,(3) A composition characterized by the presence ofA. a mercapto or polymercapto groups, andB. a nitrogen-containing group characterized by at least one of the following:1. an amido or a polyamido group,2. a cyclic amidine or a polycyclic amidine group,3. an epihalohydrin-derived amino-containing group.This invention also relates to the use of the above compositions as corrosion inhibitors.Type: GrantFiled: June 19, 1980Date of Patent: June 1, 1982Assignee: Petrolite CorporationInventors: Neil E. S. Thompson, Derek Redmore, Bernardus A. Oude Alink, Benjamin T. Outlaw
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Patent number: 4311703Abstract: Novel azacycloalkanes, azacycloalkenes and derivatives thereof and methods of preparing same are described. These compounds are useful as antidepressants, anticonvulsants, tranquilizers and analgetics.Type: GrantFiled: August 1, 1980Date of Patent: January 19, 1982Assignee: American Hoechst CorporationInventors: Lawrence L. Martin, Helen H. Ong, Vernon B. Anderson, Charles A. Crichlow
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Patent number: 4302462Abstract: 4(or 3)-(3,4-Dihydroxyphenyl)pyridine, a cardiotonic agent, is prepared by demethylating 4(or 3)-(3,4-dimethoxyphenyl)pyridine, preferably by heating with aqueous hydrogen bromide. 4(or3)-[3,4-di-(OR)-phenyl]pyridine, where R is hydrogen or methyl, or pharmaceutically-acceptable acid-addition salt thereof is disclosed as the active component in a cardiotonic composition for increasing cardiac contractility and in the method for increasing cardiac contractility in a patient requiring such treatment. The novel isomeric 2-[3,4-di-(OR)-phenyl]pyridine, where R is hydrogen or methyl, is shown for comparative purposes.Type: GrantFiled: August 4, 1980Date of Patent: November 24, 1981Assignee: Sterling Drug Inc.Inventors: Joseph C. Collins, George Y. Lesher, Baldev Singh
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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: 4285867Abstract: Compounds having the formula ##STR1## wherein ##STR2## R.sub.1 is hydrogen, benzyl or alkanoyl, X is C.sub.2-4 alkylene; andZ-W is alkyl, phenylalkyl or pyridylalkyl which can have an oxygen atom as part of the alkyl chain and their use as CNS agents, antidiarrheals and antiemetics. Processes for their preparation and intermediates therefor are described.Type: GrantFiled: September 19, 1980Date of Patent: August 25, 1981Assignee: Pfizer Inc.Inventors: Michael R. Johnson, Lawrence S. Melvin, Jr.
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Patent number: 4284635Abstract: 4-Phenylpiperidines bearing substituents at the 1,2,4 and 5-positions are potent analgesics. Pharmaceutical formulations containing such compounds and a method for effecting analgesia are provided.Type: GrantFiled: November 29, 1978Date of Patent: August 18, 1981Assignee: Eli Lilly and CompanyInventor: Dennis M. Zimmerman
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Patent number: 4283569Abstract: Compounds useful for pharmacological and medicinal purposes having the formulae ##STR1## wherein R is H, C.sub.1 -C.sub.5 alkanoyl; R.sub.1 is H, benzyl, C.sub.1 -C.sub.5 alkanoyl, P(O)(OH).sub.2, --CO(CH.sub.2).sub.2 COOH or a basic acyl group; each of R.sub.2 and R.sub.4 is H, C.sub.1 -C.sub.6 alkyl, phenyl, pyridyl or (CH.sub.2).sub.y C.sub.6 H.sub.5 ; y is 1-4; R.sub.3 is H or CH.sub.3 ; Z is C.sub.1 -C.sub.13 alkylene or --(alk.sub.1).sub.m --O--(alk.sub.2).sub.n --; each of (alk.sub.1) and (alk.sub.2) is C.sub.1 -C.sub.13 alkylene with the proviso that the summation of carbon atoms in (alk.sub.1) plus (alk.sub.2) is not greater than 13; each of m and n is 0 or 1; and W is H, pyridyl, phenyl, fluorophenyl or chlorophenyl; intermediates therefor and methods for their preparation and use.Type: GrantFiled: September 13, 1977Date of Patent: August 11, 1981Assignee: Pfizer Inc.Inventors: Thomas H. Althuis, Charles A. Harbert, Michael R. Johnson, Lawrence S. Melvin, Jr.
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Patent number: 4278797Abstract: Phenylmorphans having substituents at the 2, 3 and 7 positions and intermediates thereof are disclosed. The compounds exhibit potent analgesic activity. Formulations and a method of relieving pain are provided.Type: GrantFiled: May 19, 1980Date of Patent: July 14, 1981Assignee: Eli Lilly and CompanyInventor: Dennis M. Zimmerman
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Patent number: 4273931Abstract: There is disclosed the reduction of alkyl esters of carbonic-carboxylic acid anhydrides at elevated temperature and pressure in the presence of platinum group metal catalysts, especially palladium on activated carbon, to make alcohols. Novel alkyl esters of carbonic-carboxylic acid anhydrides are disclosed, and can be used to make the corresponding alcohols, e.g., substituted benzyl alcohols. The alcohols can be converted to the corresponding halo, e.g., chloro, compounds. The substituted benzyl halides can be reacted with di(lower alkoxy)propionitriles, and the resulting 5-benzyl pyrimidines such as trimethoprim, 2,4-diamino-5-(3,4,5-trimethoxybenzyl)-pyrimidine, which is a known anti-bacterial agent, are especially useful in combination with sulfa drugs such as sulfamethoxazole.Type: GrantFiled: December 20, 1979Date of Patent: June 16, 1981Assignee: Istituto Chemioterapico Italiano, S.p.A.Inventors: Aldo Garzia, Giorgio Vittadini, Andrea Bottazzi, Domenico Pelagalli, Costantino Coccoli
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Patent number: 4271170Abstract: The pyridine derivatives of the general formula: ##STR1## [wherein A represents an alkylene group containing from 1 to 5 carbon atoms unsubstituted or substituted by a hydroxy group, B represents a single bond, or an oxygen or sulphur atom, or an alkylene group containing from 1 to 5 carbon atoms, D represents a single bond, or an alkylene group containing from 1 to 5 carbon atoms, R represents a grouping of the formula: ##STR2## (in which R.sup.6 represents a hydrogen atom, or an alkyl group containing from 1 to 4 carbon atoms), Z represents a single bond, or an ethynylene group, or a grouping of the formula: ##STR3## in which R.sup.2 represents a hydrogen atom, or an alkyl group containing from 1 to 4 carbon atoms, R.sup.3 represents a hydrogen, bromine or chlorine atom, or an alkyl group containing from 1 to 4 carbom atoms; the symbol represents a single or double bond, the carbon atom attached to R.sup.2 binds to B, and the carbon atom attached to R.sup.3 binds to D, R.sup.Type: GrantFiled: December 20, 1979Date of Patent: June 2, 1981Assignees: Ono Pharmaceutical Co., Ltd.,, Kissei Pharmaceutical Co., Ltd.Inventors: Tadao Tanouchi, Masanori Kawamura, Masaki Hayashi
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Patent number: 4267329Abstract: A process is described for the catalytic, selective preparation of 2-vinylpyridine from acetylene and acrylonitrile using a cyclopentadienylcobalt catalyst or .pi.-allylcobalt catalyst at elevated temperature in an inert solvent, wherein the acrylonitrile concentration is up to 2 mols/liter and the reaction is carried out at a temperature over 140.degree. C. and up to 180.degree. C., the reaction time being not more than 50 minutes.Type: GrantFiled: June 2, 1980Date of Patent: May 12, 1981Assignee: Studiengesellschaft Kohle GmbHInventors: Helmut Bonnemann, Marc Samson
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Patent number: 4246263Abstract: A series of 4-(2-hydroxyethylthiomethyl)pyridines and related compounds, and their pharmaceutically acceptable acid addition salts, having antiinflammatory and immunoregulatory activity are disclosed. Preferred compounds include 4-(2-hydroxyethylthiomethyl)pyridine itself, as well as 4-(2-hydroxyphenylthiomethyl)pyridine, 4-(2-hydroxy-1-propylthiomethyl)pyridine, 4-(3-hydroxy-2-butylthiomethyl)pyridine, 4-(2-hydroxyethylthiomethyl)pyrimidine, the acetate esters corresponding to the above compounds, and 4-(2,3-dihydroxy-1-propylthiomethyl)pyridine.Type: GrantFiled: October 15, 1979Date of Patent: January 20, 1981Assignee: Pfizer Inc.Inventors: Joseph G. Lombardino, Charles A. Harbert
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Patent number: 4228288Abstract: 4-Phenylpiperidines bearing substituents at the 1,2,4 and 5-positions are potent analgesics. Pharmaceutical formulations containing such compounds and a method for effecting analgesia are provided.Type: GrantFiled: August 27, 1979Date of Patent: October 14, 1980Assignee: Eli Lilly and CompanyInventor: Dennis M. Zimmerman
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Patent number: 4223138Abstract: A process for the preparation of an aminoethanol is described wherein an amine is vaporized in a collection vessel and the vapors are caused to pass upwardly through a defined reaction zone into a condensation zone where they are condensed and caused to flow downwardly into the reaction zone. In the reaction zone the flow toward the collection zone is retarded and, while retarded, epoxide reactant is directed thereagainst. The aminoethanol so formed is removed into the collection zone such as by directing condensed amine thereagainst.Type: GrantFiled: March 29, 1978Date of Patent: September 16, 1980Assignee: Bayer AktiengesellschaftInventor: Rudiger Schubart
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Patent number: 4191828Abstract: 2-(2,2-Dicyclohexylethyl)piperidine is prepared via the catalytic hydrogenation of 2-(2,2-diphenylethenyl)pyridine in a single step. High yields are obtained using a rhodium supported catalyst.Type: GrantFiled: April 14, 1976Date of Patent: March 4, 1980Assignee: Richardson-Merrell Inc.Inventors: Stephen W. Horgan, Frank P. Palopoli, David L. Wenstrup
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Patent number: 4189486Abstract: 1-(3-Pyridyl)-2,2,2-trihaloethyl compounds of the general formula I ##STR1## in which n is 0 or 1, R represents oxygen, hydrogen or an organic radical having at the most 12 C-atoms, m is 0 when R is oxygen, m is 1/2 or 1 when R is hydrogen or an aliphatic or aralkyl radical, and X represents a negative ion, R' represents a radical of the general formula II ##STR2## wherein V, Y, Z represent chlorine or bromine and may be identical or different, but are preferably identical; A represents hydrogen or a radical of the general formula III ##STR3## wherein B' is oxygen or sulphur, and B stands for an organic radical having up to 12 C atoms, or for an amino group of the general formula IV ##STR4## wherein F and D are identical or different, and represent hydrogen or organic radicals having at most 12 C-atoms; A may further be a sulphonyl group of the general formula --SO.sub.2 --B, in which B has the same meaning as in formula III.Type: GrantFiled: December 23, 1977Date of Patent: February 19, 1980Assignee: Consortium fur Elektrochemische Industrie GmbHInventors: Fritz Sauter, Otto Eberle, Beate Suss, Rudolf Weissgerber
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Patent number: 4180669Abstract: This invention provides 2-(N-substituted piperidino)-5-alkyl resorcinols of the structure ##STR1## wherein R.sub.1 is H, loweralkyl, loweralkynyl or aralkyl; R.sub.2 and R.sub.3 are each H or when taken together R.sub.2 R.sub.3 =CH.sub.2 CH.sub.2 ; R.sub.4 is a C.sub.1 -C.sub.10 alkyl and R.sub.5 is H or loweralkyl, and the pharmaceutically acceptable salts thereof.These compounds are useful as antisecretory agents.Type: GrantFiled: March 27, 1978Date of Patent: December 25, 1979Assignee: Abbott LaboratoriesInventor: Martin Winn
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Patent number: 4175197Abstract: Novel 1,3,4-trisubstituted-4-arylpiperidines are prepared by alkylating a 2,3-disubstituted-3-arylpyrroline to afford a 1,2,3-trisubstituted-3-aryl-1-pyrrolinium salt, reacting the salt with diazomethane to provide a 1,2,3-trisubstituted-3-aryl-1,2-methylene-pyrrolidinium salt, heating the pyrrolidinium salt to effect a ring expansion to the corresponding 1,3,4-trisubstituted-4-aryl-1,4,5,6-tetrahydropyridinium salt, neutralizing the salt and reducing the tetrahydropyridine to provide a 1,3,4-trisubstituted-4-arylpiperidine. The piperidines so formed are useful as pharmacological agents and as intermediates in the preparation of other piperidines of the invention. The compounds provided herein are especially useful as narcotic agonists analgesics and as narcotic antagonists.Type: GrantFiled: May 12, 1978Date of Patent: November 20, 1979Assignee: Eli Lilly and CompanyInventor: Dennis M. Zimmerman
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Patent number: 4154834Abstract: The compounds are substituted isocytosines which are histamine H.sub.2 -antagonists. Two specific compounds of the present inventon are 2-[2-(5-methyl-4-imidazolylmethylthio)ethylamino]-5-(3-pyridylmethyl)-4-py rimidone and 2-[2-(3-bromo-2-pyridylmethylthio)ethylamino]-5-(4-pyridylmethyl)-4-pyrimi done.Type: GrantFiled: December 16, 1977Date of Patent: May 15, 1979Assignee: Smith Kline & French Laboratories LimitedInventors: Thomas H. Brown, Graham J. Durant, Charon R. Ganellin
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Patent number: 4148797Abstract: Novel pyridyl alkyl sulfonic acid betaines useful as additives to nickel electroplating baths.Type: GrantFiled: June 15, 1978Date of Patent: April 10, 1979Assignee: Cilag-Chemie A.G.Inventors: Kurt Pluss, Bruno R. DeMartin
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Patent number: 4147872Abstract: Azacycloalkanes, and derivatives thereof, including unsaturated analogs, each of which has at the 3-position a 2-hydroxy-4-substituted phenyl group wherein the 4-position substituent is alkyl which can have an oxygen atom as part of the chain, or aralkyl which can have an oxygen atom as part of the alkyl chain, their use for pharmacological and medicinal purposes, intermediates therefor and processes for their preparation.Type: GrantFiled: September 13, 1977Date of Patent: April 3, 1979Assignee: Pfizer Inc.Inventors: Thomas H. Althuis, Charles A. Harbert, Michael R. Johnson, Lawrence S. Melvin, Jr.
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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: 4132723Abstract: Novel 9-substituted phenyl- or cyclohex-1-en-1-yl-3,7-dimethyl-nona-2,4,6-trienoic acids or derivatives thereof, -trienal or -trienol derivatives are described. The subject compounds are useful in the treatment of neoplasias, certain dermatoses and inflammatory and allergic dermatological conditions.Type: GrantFiled: February 23, 1977Date of Patent: January 2, 1979Assignee: Hoffmann-La Roche Inc.Inventor: Beverly A. Pawson
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Patent number: RE30309Abstract: The present invention relates to new chemical compounds which can be used as inhibitors of dental plaque, and orally-acceptable compositions thereof, combinations thereof with known compounds having an inhibitory action on the formation of dental plaque, such as biguanidines, and method of treating therewith for the prevention of dental plaque or tartar and dental caries.The new compounds have the general formula ##STR1## in which R.sub.1 =H or alkylR.sub.2 =CH.sub.2 OH, alkyl carboxylate, ##STR2## and R.sub.2 is in 2 or 3 position.Compositions containing these active principles are useful in particular in the preventive treatment of periodontopathies and odontopathies and in the field of oral-dental hydgiene.Type: GrantFiled: March 15, 1979Date of Patent: June 17, 1980Assignee: Pierre Fabre S.A.Inventors: Henri Cousse, Gilbert Mouzin, Jean-Claude Vezin, Lucien D. d'Hinterland, Jacques Dubois