The Chalcogen, X, Is In A -c(=x)- Group Patents (Class 546/237)
  • Patent number: 4418068
    Abstract: 6-Hydroxy-2-(4-hydroxyphenyl)-3-[4-(2-piperidinoethoxy)benzoyl]benzo[b]thio phene, its ethers and esters, and the physiologically acceptable acid addition salts thereof, are valuable antiestrogens and antiendrogens.
    Type: Grant
    Filed: December 16, 1981
    Date of Patent: November 29, 1983
    Assignee: Eli Lilly and Company
    Inventor: Charles D. Jones
  • Patent number: 4415687
    Abstract: 1,3-dihydroxy-4,6-bis-4'-(2',2',6',6',-tetramethylpiperidyl) benzene, its 1'-alkyl or 1'-(substituted alkyl) derivatives and monomeric or polymeric products derived from these compounds by substitution of 1- and 3-hydroxy groups and/or by the linking of hydroxy groups on adjacent units through a bridging groups, are useful as light and heat stabilizers for polymeric organic materials.Corresponding bis(3',4'-dehydro) unsaturated compounds are useful as intermediates.
    Type: Grant
    Filed: July 2, 1982
    Date of Patent: November 15, 1983
    Assignee: Sandoz Ltd.
    Inventors: Lajos Avar, Evelyne Kalt, Hellmuth Reinshagen
  • Patent number: 4390537
    Abstract: 1-(Substituted-aminoalkoxyphenyl)-2-methylene-1-alkanones, a class of compounds possessing anti-allergic properties for use in the treatment of allergic conditions, such as asthma prepared by etherifying an alkanoylphenol with an aminoalkyl halide, converting the ether formed to a salt of Mannich base by reacting it with a salt of a secondary amine in the presence of formaldehyde or paraformaldehyde and treating the Mannich salt with a weak base to deaminate the same and form the final product.
    Type: Grant
    Filed: May 19, 1982
    Date of Patent: June 28, 1983
    Assignee: Merck & Co., Inc.
    Inventor: Edward J. Cragoe, Jr.
  • Patent number: 4374984
    Abstract: Compounds of the formula ##STR1## wherein the substituents A, Z, R.sup.1, R.sup.2, R.sup.3, R.sup.4, X, n and m are defined hereinbeloware effective photoinitiators, especially for the photopolymerization of ethylenically unsaturated compounds and for the curing of printing inks.
    Type: Grant
    Filed: March 4, 1981
    Date of Patent: February 22, 1983
    Assignee: Merck Patent Gesellschaft mit Beschrankter Haftung
    Inventors: Jurgen Eichler, Claus Herz, Karl-Heinz Neisius, Gregor Wehner
  • Patent number: 4352760
    Abstract: The present invention provides novel substituted heptadeca-5,9- and 5,10-dienoic acid and similar fatty acid compounds which are derivatives of certain prostaglandins and are potent thromboxane A.sub.2 inhibitors. By virtue of this pharmacological property, they represent useful pharmacological agents for a wide variety of purposes.
    Type: Grant
    Filed: December 29, 1980
    Date of Patent: October 5, 1982
    Assignee: The Upjohn Company
    Inventor: Kirk M. Maxey
  • Patent number: 4350518
    Abstract: Substituted alkylammonium salts of the formula ##STR1## where Ar denotes substituted phenyl, X denotes oxygen or sulfur, n denotes one of the integers 0, 1 and 2, B denotes bicyclic quinuclidine, bicyclic pyrrolizidine or substituted ammonium, and Z denotes the anion of a nonphytotoxic acid, the manufacture of these compounds, and their use as plant growth regulators.
    Type: Grant
    Filed: February 23, 1981
    Date of Patent: September 21, 1982
    Assignee: BASF Aktiengesellschaft
    Inventors: Hubert Sauter, Bernd Zeeh, Ernst Buschmann, Johann Jung
  • Patent number: 4308400
    Abstract: Aromatic-aliphatic ketones of the formulae I, II, III or IV ##STR1## wherein n is 1 or 2, Ar is an aryl radical, R.sup.1 and R.sup.2 are monvalent aliphatic, cycloaliphatic or araliphatic radicals, R.sup.3 is a direct bond or a divalent organic radical, X is a hydroxyl or amino group or the monovalent etherification or silylation products thereof, and X' is a divalent amino, ether or silyloxy group, Y is a direct bond or CH.sub.2 and Z is O, S, SO.sub.2, CH.sub.2 or C(CH.sub.3).sub.2, are suitable sensitizers for the photopolymerization of unsaturated compounds and for the photochemical crosslinking of polyolefins. Some of these compounds are novel and can be obtained by methods analogous to those for obtaining the known compounds of this type.
    Type: Grant
    Filed: December 28, 1979
    Date of Patent: December 29, 1981
    Assignee: Ciba-Geigy A.G.
    Inventors: Louis Felder, Rudolf Kirchmayr, Rinaldo Husler
  • Patent number: 4294841
    Abstract: 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: Grant
    Filed: November 27, 1979
    Date of Patent: October 13, 1981
    Assignee: Pharmindustrie
    Inventors: Alain A. Champseix, Gerard R. Le Fur
  • Patent number: 4289686
    Abstract: 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: Grant
    Filed: September 17, 1979
    Date of Patent: September 15, 1981
    Assignee: Ciba-Geigy Corporation
    Inventors: Jean Rody, Mario Slongo
  • Patent number: 4285958
    Abstract: Pharmaceutically useful compounds of the following formula: ##STR1## wherein R.sub.1 represents hydrogen or hydroxy; R.sub.2 represents hydrogen; or R.sub.1 and R.sub.2 taken together form a second bond between the carbon atoms bearing R.sub.1 and R.sub.2 ; n is a positive whole integer of from 1 to 5; R.sub.3 is --CH.sub.3, --CH.sub.2 OH, --COOH or --COOalkyl wherein the alkyl moiety has from 1 to 6 carbon atoms and is straight or branched; and A and B are individually hydrogen or hydroxy; with the provisos that at least one of A or B is hydrogen and one of A or B is other than hydrogen when R.sub.3 is --CH.sub.3 ; and pharmaceutically acceptable acid addition salts thereof.
    Type: Grant
    Filed: October 14, 1980
    Date of Patent: August 25, 1981
    Assignee: Richardson-Merrell Inc.
    Inventors: Albert A. Carr, Joseph E. Dolfini, George J. Wright
  • Patent number: 4285957
    Abstract: Novel compounds of the following formula: ##STR1## wherein R.sub.1 is hydrogen or hydroxy; R.sub.2 is hydrogen; or R.sub.1 and R.sub.2 taken together form a second bond between the carbon atoms bearing R.sub.1 and R.sub.2 ; n is an integer of from 1 to 5; R.sub.3 is --CH.sub.3, --CH.sub.2 OH, --COOH or --COOalkyl wherein the alkyl moiety has from 1 to 6 carbon atoms and is straight or branched; and each of A and B is hydrogen or hydroxy; with the provisos that at least one of A or B is hydrogen and one of A or B is other than hydrogen when R.sub.3 is --CH.sub.3 ; and pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: October 14, 1980
    Date of Patent: August 25, 1981
    Assignee: Richardson-Merrell Inc.
    Inventors: Albert A. Carr, Joseph E. Dolfini, George J. Wright
  • Patent number: 4277474
    Abstract: New propanone derivatives, useful for treating allergic diseases, the pharmacologically allowable salts thereof, their manufacturing process and pharmaceutical composition containing at least one of them as the active ingredient.
    Type: Grant
    Filed: September 27, 1979
    Date of Patent: July 7, 1981
    Assignee: Nippon Zoki Pharmaceutical Co., Ltd.
    Inventors: Akihide Kohda, Teikichi Kurosaki
  • Patent number: 4273787
    Abstract: The compounds are 4-phenyl-4-lower alkyl-substituted-3-buten-2-ones, and -2-halo-1,3-butadienes, e.g., 2-(p-biphenylyl)-2-penten-4-one, and are useful as pharmaceuticals.
    Type: Grant
    Filed: August 9, 1979
    Date of Patent: June 16, 1981
    Assignee: Sandoz, Inc.
    Inventor: Eugene E. Galantay
  • Patent number: 4271294
    Abstract: Compounds of the formula I ##STR1## wherein Ar.sup.1 and Ar.sup.2 represent unsubstituted or substituted phenyl, R.sup.1 represents hydrogen, alkyl, alkoxy, hydroxyalkyl, allyl, benzyl or a group --O--R.sup.2 -NR.sup.3 R.sup.4, R.sup.2 represents alkylene and --NR.sup.3 R.sup.4 is an open chain or cyclic organic amino group, are effective initiators for the photopolymerization of unsaturated compounds or for the photocrosslinking of polyolefins. They can be obtained by different methods which are in themselves known, in particular by reaction of the corresponding haloalkyl ethers or haloalkyl ketals with primary or secondary amines.
    Type: Grant
    Filed: March 13, 1980
    Date of Patent: June 2, 1981
    Assignee: Ciba-Geigy Corporation
    Inventors: Louis Felder, Rudolf Kirchmayr, Rinaldo Kusler
  • Patent number: 4268688
    Abstract: This invention relates to a process for the preparation of optically active aldehydes by the asymmetric catalytic hydroformylation of olefins. The process comprises the hydroformylation of olefinically unsaturated prochiral compounds in the presence of an optically active coordination compound containing a metal which is selected from the group consisting of rhodium, iridium, and cobalt.This invention describes a generalized process for the asymmetric hydroformylation of a wide variety of olefins in which a preponderance of one optical isomer is produced. It is especially useful for the preparation of natural products which may require the presence of only one optical isomer for their utilization, for example, as flavors, fragrances, and medications.The catalyst systems for the process of this invention are formed in the presence of carbon monoxide and hydrogen, from coordination compounds consisting of a central metal atom, rhodium, iridium, or cobalt, and at least one optically active ligand, e.g.
    Type: Grant
    Filed: February 16, 1973
    Date of Patent: May 19, 1981
    Assignee: Monsanto Company
    Inventors: Harold B. Tinker, Arthur J. Solodar
  • Patent number: 4263202
    Abstract: Metal phenolates having at least one piperidinyl group sterically hindered on the nitrogen atom are suitable as additives for organic material.
    Type: Grant
    Filed: July 10, 1978
    Date of Patent: April 21, 1981
    Assignee: Ciba-Geigy Corporation
    Inventors: Michael Rasberger, Samuel Evans, Paul Moser
  • Patent number: 4257859
    Abstract: Quaternary ammonium compounds of the formula ##STR1## where R.sup.1 and R.sup.2 are identical or different and each is H, halogen, phenyl, alkyl, alkoxy or alkylthio,R.sup.3 is H or alkyl, hydroxyalkyl, cycloalkyl or aralkyl,R.sup.4 and R.sup.5 are identical or different and each is alkyl, phenyl, cycloalkyl or aralkyl orR.sup.4 and R.sup.5 together are a --(CH.sub.2).sub.4 -- bridge, a --(CH.sub.2).sub.5 -- bridge or a --(CH.sub.2).sub.2 --O--(CH.sub.2).sub.2 -- bridge,R.sup.6 is alkyl andX.sup..crclbar. is Cl.sup..crclbar., Br.sup..crclbar., I.sup..crclbar., CH.sub.3 SO.sub.4.sup..crclbar. or C.sub.2 H.sub.5 SO.sub.4.sup..crclbar., a process for their preparation from Mannich bases of the formula ##STR2## and alkylating agents, and the use of these quaternary ammonium compounds as initiators for the photopolymerization of polymerizable mixtures containing olefinically unsaturated compounds, especially for the preparation of aqueous polymer dispersions or polymer solutions.
    Type: Grant
    Filed: July 12, 1979
    Date of Patent: March 24, 1981
    Assignee: BASF Aktiengesellschaft
    Inventors: Martin Fischer, Werner Kuesters, Erich Penzel, Wolfgang Rehder, Walter Trautmann
  • Patent number: 4254130
    Abstract: Pharmaceutically useful compounds of the following formula: ##STR1## wherein R.sub.1 represents hydrogen or hydroxy; R.sub.2 represents hydrogen; or R.sub.1 and R.sub.2 taken together form a second bond between the carbon atoms bearing R.sub.1 and R.sub.2 ; n is a positive whole integer of from 1 to 5; R.sub.3 is --CH.sub.3, --CH.sub.2 OH, --COOH or --COOalkyl wherein the alkyl moiety has from 1 to 6 carbon atoms and is straight or branched; and A and B are individually hydrogen or hydroxy; with the provisos that at least one of A or B is hydrogen and one of A or B is other than hydrogen when R.sub.3 is --CH.sub.3 ; and pharmaceutically acceptable acid addition salts thereof.
    Type: Grant
    Filed: April 10, 1979
    Date of Patent: March 3, 1981
    Assignee: Richardson-Merrell Inc.
    Inventors: Albert A. Carr, Joseph E. Dolfini, George J. Wright
  • Patent number: 4252804
    Abstract: Compounds of the formula I ##STR1## wherein m and n are 0, 1 or 2, X represents oxygen, imino, benzylimino, or morpholinoethylimino, Y represents CO, CONH, COO or SO.sub.2, and NR.sub.1 R.sub.2 represents a dimethylamino, diethylamino, dipropylamino, dibutylamino, allylamino, isobutenylamino, cyclopentylamino, cyclohexylamino, cycloheptylamino, cyclooctylamino, N-methyl N-cyclopentylamino, N-methyl N-cyclohexylamino, N-allyl N-cyclohexylamino, adamantylamino, diethoxyethylamino, dimethylaminoethylamino, dimethylaminopropylamino, N-methyl N-dimethylaminopropyl-amino, benzylamino, 3,4,5-trimethoxybenzylamino, phenethylamino, p-chlorophenethylamino, tetrahydrofurfurylamino, tetrahydropyranylmethylamino, pyrrolidino, isoxazolidinyl, piperidino, 4-hydroxypiperidino, 4-m-chlorophenyl-4-hydroxypiperidino, homopiperidino, 1,2,3,6-tetrahydropyridyl, morpholino, 2-methylmorpholino, 2,6-dimethylmorpholino, 2-morpholinoethylamino, thiamorpholino, piperazino, 4-methylpiperazino, 4-(.alpha.
    Type: Grant
    Filed: January 13, 1978
    Date of Patent: February 24, 1981
    Assignee: Metabio-Joullie
    Inventors: Maurice Joullie, Gabriel Maillard, Lucien Lakah, Christian J. M. Warolin
  • Patent number: 4248779
    Abstract: 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: Grant
    Filed: October 4, 1978
    Date of Patent: February 3, 1981
    Assignee: Ihara Chemical Industry Company, Limited
    Inventors: Zenichi Sato, Fumiya Tabuchi, Keiichiro Takagi, Yoji Imamiya
  • Patent number: 4244963
    Abstract: 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: Grant
    Filed: September 27, 1979
    Date of Patent: January 13, 1981
    Assignee: Merck & Co., Inc.
    Inventors: Nathaniel Grier, Richard A. Dybas, Bruce E. Witzel
  • Patent number: 4241071
    Abstract: Novel azacycloalkanes, azacycloalkenes and derivatives thereof and methods of preparing same are described. These compounds are useful as antidepressants, anticonvulsants, tranquilizers and analgetics.
    Type: Grant
    Filed: January 25, 1979
    Date of Patent: December 23, 1980
    Assignee: American Hoechst Corporation
    Inventors: Lawrence L. Martin, Helen H. Ong, Vernon B. Anderson, Charles A. Crichlow
  • Patent number: 4238612
    Abstract: A process for the conversion of compounds of the formula: ##STR1## in which R is a hydrogen atom or a substituent and for which the carbon carrying the vinyl group has the rectus configuration, into the corresponding compounds of formula (I) for which the carbon carrying the vinyl group has the sinister configuration, and vice versa, which comprises subjecting a compound of formula (I) for which the carbon carrying the vinyl group has the rectus or sinister configuration, partially or entirely salified, to a heating at a temperature above 50.degree. C. in a protic solvent or a mixture of protic solvents in the presence or absence of formaldehyde, and isolating the compound of formula (I) for which the carbon carrying the vinyl group has the sinister or rectus configuration thus formed.
    Type: Grant
    Filed: March 21, 1979
    Date of Patent: December 9, 1980
    Assignee: Pharmindustrie
    Inventors: Jean-Jacques Barieux, Marie-Christine Dubroeucq, Francois Rocquet
  • Patent number: 4238613
    Abstract: 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: Grant
    Filed: October 13, 1978
    Date of Patent: December 9, 1980
    Assignee: Ciba-Geigy Corporation
    Inventors: Michael Rasberger, Friedrich Karrer
  • Patent number: 4237141
    Abstract: Novel .alpha.-methyl-.beta.-aminopropiophenone derivatives having bronchodilator activity represented by the following general formula: ##STR1## where R represents alkyl having 1-6 carbon atom benzyl or phenyl; R.sub.1 and R.sub.2 individually represent alkyl having 1-6 carbon atom or they form, joining to each other together with the adjacent nitrogen atom with or without intervening an atom other than carbon atom, a saturated heterocyclic ring which may be substituted with lower alkyl; n is an integer of 0, 1 or 2 on the proviso that R represents methyl or ethyl if n is 0, as well as their non-toxic salts are presented. Method of producing the new derivatives and the bronchodilatation method using them are disclosed as well.
    Type: Grant
    Filed: May 26, 1978
    Date of Patent: December 2, 1980
    Assignee: Nippon Kayaku Kabushiki Kaisha
    Inventors: Akira Shiozawa, Shuji Kurashige, Hiroaki Hamano, Yasuhiko Furuta, Masako Ikeda, Hiroshi Miyazaki, Chiyoko Aoyagi, Yasuo Ishii
  • Patent number: 4233055
    Abstract: This invention comprises new compounds and a composition for influencing, in particular for inhibiting, plant growth, which contains as active compound at least one quaternary ammonioalkancarboxylic acid anilide of the formula I ##STR1## wherein each of R.sub.1 to R.sub.5 independently represents a hydrogen atom or any indentical or different substituent,each of R.sub.6 to R.sub.8 independently represents an identical or different radical selected from the group consisting of alkyl, substituted alkyl, cycloalkyl, alkenyl, alkynyl, while two alkyl group together with the nitrogen atom can also form a saturated heterocyclic ring or three groups together can form an unsaturated heterocyclic ring a "alkylene" represents a saturated or unsaturated hydrocarbon bridge of 1 to 3 carbon atoms andX represents the anion of a non-phytotoxic acid HX.
    Type: Grant
    Filed: December 11, 1978
    Date of Patent: November 11, 1980
    Assignee: Ciba-Geigy Corporation
    Inventor: Henry Martin
  • Patent number: 4230862
    Abstract: Derivatives of 3-phenyl-4-aroyl-1,2-dihydronaphthalenes and 1-aroyl-2-phenylnaphthalenes are useful both as antifertility agents and in suppressing the growth of mammary tumors.
    Type: Grant
    Filed: August 3, 1978
    Date of Patent: October 28, 1980
    Assignee: Eli Lilly and Company
    Inventors: Tulio Suarez, C. David Jones
  • Patent number: 4228105
    Abstract: A process for the production of compounds of formula I, ##STR1## wherein R.sub.1 is alkyl of 1 to 3 carbon atoms,R.sub.2 is hydrogen, fluorine, chlorine or bromine, andR.sub.3 is bromine, iodine, isobutyl, tert. butyl, cyclohexyl, cyclohexenyl; or phenyl, optionally substituted by fluorine, chlorine, bromine or alkoxy of 1 to 4 carbon atoms; or a radical of formula II, ##STR2## in which either R.sub.4 and R.sub.5 are the same or different and each signifies alkyl of 1 to 3 carbon atoms,orR.sub.4 and R.sub.5 together signify the radical --(CH.sub.2).sub.n --, in which n is 4 or 5, the radical --CH.sub.2 --CH.sub.2 --0--CH.sub.2 --CH.sub.2 --, the radical --CH.sub.2 --CH.dbd.CH--CH.sub.2 --, or the radical --CH.sub.2 --CH.sub.2 --N(R.sub.6)--CH.sub.2 --CH.sub.2 --, in which R.sub.6 is hydrogen or alkyl of 1 to 3 carbon atoms. Hydroxyketone and hydroxy imine intermediates are also disclosed.The compounds of formula I are known to exhibit anti-inflammatory activity.
    Type: Grant
    Filed: November 27, 1978
    Date of Patent: October 14, 1980
    Assignee: Sandoz Ltd.
    Inventor: Rudiger Jeck
  • Patent number: 4222938
    Abstract: Thiolcarbamates are prepared from carbamoyl halides and xanthates.
    Type: Grant
    Filed: September 29, 1978
    Date of Patent: September 16, 1980
    Assignee: Monsanto Company
    Inventor: John J. D'Amico
  • Patent number: 4182877
    Abstract: Anthranilic acid derivatives exhibiting fungicidal properties and useful as synthesis intermediates have the formula: ##STR1## wherein R is selected from the group consisting of a hydrogen atom; a --COOR.sup.3 group and a --CH.sub.2 OH group; R.sup.1 and R.sup.2 are the same or different and selected from the group consisting of a hydrogen atom and alkyl and cycloalkyl groups (provided that R.sup.1 and R.sup.2 are not both hydrogen atoms), or R.sup.1 and R.sup.2, together with the nitrogen atom to which they are attached, form a non-aromatic heterocyclic ring structure;R.sup.3 is selected from the group consisting of a hydrogen atom and an alkyl group;R.sup.4 is selected from the group consisting of a hydrogen atom, a halogen atom and a hydroxyl group;R.sup.6 is selected from the group consisting of a hydrogen atom and a halogen atom; andR.sup.5 is selected from the group consisting of a hydrogen atom, a halogen atom, and nitro, thiocyano and formyl groups.
    Type: Grant
    Filed: May 10, 1977
    Date of Patent: January 8, 1980
    Assignee: Commonwealth Scientific and Industrial Research Organization
    Inventors: Roger L. N. Harris, John L. Huppatz, John N. Phillips, Barbara Witrzens
  • Patent number: 4181803
    Abstract: New propiophenone derivatives prepared by the reaction of propiophenone, formaldehyde and piperidine, as well as pharmacologically acceptable acid-addition salts thereof are provided, which possess improved pharmacological activities such as anti-tramorine and anti-nicotine activities superior to those of the known analoguous compound. The new compounds are useful for the therapeutic treatment of human patient suffering from pathological muscular contracture, spastic paralysis due to cerebral apoplexy, spinal and cerebral palsies and the like.
    Type: Grant
    Filed: March 11, 1976
    Date of Patent: January 1, 1980
    Assignee: Eisai Co., Ltd.
    Inventors: Eiichi Morita, Takeo Kanai
  • Patent number: 4153797
    Abstract: Novel .alpha.-aryl-.alpha.,.alpha.-bis[.omega.-(disubstituted amino)alkyl]-acetamides are described herein. The compounds are useful as anti-arrhythmic agents. The compounds are prepared by reacting an appropriate disubstituted acetonitrile with an appropriate haloalkyl amine and subsequently hydrolyzing the resulting nitrile with concentrated sulfuric acid.
    Type: Grant
    Filed: May 1, 1978
    Date of Patent: May 8, 1979
    Assignee: G. D. Searle & Co.
    Inventors: Jerry J. Renbarger, Peter K. Yonan
  • Patent number: 4148796
    Abstract: 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: Grant
    Filed: August 15, 1973
    Date of Patent: April 10, 1979
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Hisao Yamamoto, Masaru Nakao, Kikuo Sasajima, Isamu Maruyama, Shigenari Katayama
  • Patent number: 4146630
    Abstract: 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: Grant
    Filed: October 27, 1977
    Date of Patent: March 27, 1979
    Assignee: Boehringer Mannheim GmbH
    Inventors: Wolfgang Kampe, Walter-Gunar Friebe, Fritz Wiedemann, Gisbert Sponer, Wolfgang Bartsch, Karl Dietmann
  • Patent number: 4145426
    Abstract: 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: Grant
    Filed: July 18, 1977
    Date of Patent: March 20, 1979
    Assignee: Merck & Co., Inc.
    Inventors: Nathaniel Grier, Richard A. Dybas, Bruce E. Witzel
  • Patent number: 4141718
    Abstract: This invention comprises new compounds and a composition for influencing, in particular for inhibiting, plant growth, which contains as active compound at least one quaternary ammonioalkancarboxylic acid anilide of the formula I ##STR1## wherein EACH OF R.sub.1 to R.sub.5 independently represents a hydrogen atom or any identical or different substituent,Each of R.sub.6 to R.sub.8 independently represents an identical or different radical selected from the group consisting of alkyl, substituted alkyl, cycloalkyl, alkenyl, alkynyl, while two alkyl group together with the nitrogen atom can also form a saturated heterocyclic ring or three groups together can form an unsaturated heterocyclic ring a "alkylene" represents a saturated or unsaturated hydrocarbon bridge of 1 to 3 carbon atoms andX represents the anion of a non-phytotoxic acid HX.
    Type: Grant
    Filed: December 16, 1976
    Date of Patent: February 27, 1979
    Assignee: Ciba-Geigy Corporation
    Inventor: Henry Martin
  • Patent number: 4140770
    Abstract: Processes for preparing benzoylethers, their acid additive salts and their quaternary ammonium salts are disclosed. These compounds have useful pharmacodynamic properties.
    Type: Grant
    Filed: April 12, 1977
    Date of Patent: February 20, 1979
    Assignee: A. Nattermann & Cie. GmbH
    Inventors: Gudrun Repplinger, Hans Betzing
  • Patent number: 4134983
    Abstract: 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: Grant
    Filed: December 17, 1975
    Date of Patent: January 16, 1979
    Assignee: Merck & Co., Inc.
    Inventor: John J. Baldwin