Alicyclic Ring And An Atom Other Than Oxygen, Carbon, Or Hydrogen In Substituent Q Patents (Class 564/191)
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Patent number: 5296597Abstract: The present invention is directed towards a series of secondary and tertiary amide derivatives of Partricin A & Partricin B attached at the C-18 carboxyl group. The compounds can be used in the treatment of hypercholesteremia and hyperlipemia conditions, of steroidal imbalances, and as antifungal and antiprotozoan agents.Type: GrantFiled: November 14, 1990Date of Patent: March 22, 1994Assignee: SPA Societa' Prodotti Antibiotici S.P.A.Inventors: Tiberio Bruzzese, Franco Ottoni, Giuseppe Ghielmetti
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Patent number: 5290810Abstract: A compound of the formula ##STR1## in which R.sup.1 and R.sup.2 taken together represent a polymethylene chain having 3 or 4 carbon atoms, or a polymethylene chain having 3 or 4 carbon atoms substituted by at least one lower alkyl radical having 1 to 4 carbon atoms, R.sup.3 is hydrogen, hydrocarbyl or substituted hydrocarbyl and X represents cyano, a group --SO.sub.3 M or a group --S--R.sup.4 where M is hydrogen or an alkali metal such as sodium and R.sup.4 is hydrocarbyl or substituted hydrocarbyl. Typically R.sup.1 and R.sup.2 complete a cyclopentene ring, R.sup.3 is alkyl such as methyl and X is a group --SO.sub.3 Na. The compounds have microbiological activity.Type: GrantFiled: September 24, 1991Date of Patent: March 1, 1994Assignee: Imperial Chemical Industries PLCInventor: Peter W. Austin
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Patent number: 5264606Abstract: A process for the preparation of monomeric polyvinyl compounds and/or oligomers thereof comprising:(i) preactivating a supported rhenium oxide catalyst with a hydrocarbyl metal compound; and(ii) reacting, under metathesis reaction conditions, norbornene or one or more substituted norbornenes, or mixtures thereof, with ethylene in the presence of the activated supported catalyst of step (i).Type: GrantFiled: November 9, 1992Date of Patent: November 23, 1993Assignee: Union Carbide Chemicals & Plastics Technology CorporationInventors: Kenneth G. Moloy, Bernard D. Dombek
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Patent number: 5239118Abstract: The synthesis of stable, ten-membered, cyclic conjugated enediynes is described. Said compounds were successfully employed to cleave double-stranded DNA spontaneously at ambient temperatures.Type: GrantFiled: December 9, 1991Date of Patent: August 24, 1993Assignee: Trustees of the University of Penna.Inventors: Kyriacos C. Nicolaou, Guido Zuccharello, Yuji Ogawa
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Patent number: 5220048Abstract: Benzocyclobutene-1,2-dichlorides, -bromides and -iodides which are substituted in the benzene ring are accessible in good yields and short reaction times by reacting substituted 1,2-(dichloromethyl or dibromomethyl)-benzenes with NaI in acetonitrile as the solvent. They can be used together with dienophils, for example 1,4-quinones, in Diels-Alder reactions.Type: GrantFiled: May 24, 1989Date of Patent: June 15, 1993Assignee: Ciba-Geigy CorporationInventors: Marcus Baumann, Walter Fischer, Vratislav Kvita, Carl W. Mayer
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Patent number: 5192798Abstract: This invention relates to novel lipophilic polyamines of formula I, the method of using these compounds to treat hypercholesterolemia, and intermediates thereto.Z.sub.1 --(CH.sub.2).sub.n --Y.sub.1 --X.sub.1 --R.sub.Type: GrantFiled: August 16, 1990Date of Patent: March 9, 1993Assignee: The Upjohn CompanyInventors: James W. Aiken, Charles H. Spilman, Edward W. Thomas
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Patent number: 5183932Abstract: Herbicidal substituted 4-amino-5-alkylthio-1,2,4-triazol-3-ones of the formula ##STR1## in which R.sup.1 represents in each case straight-chain or branched alkyl, alkenyl or alkinyl, each of which has up to 4 carbon atoms, andR.sup.2 represents sec-butyl, tert.-butyl or optionally substituted C.sub.5 -C.sub.10 -alkyl, alkenyl or alkinyl, or piperidyl- or morpholinyl-alkyl, optionally substituted C.sub.3, C.sub.4, C.sub.5 and C.sub.7 -cycloalkyl, substituted cyclohexyl, or optionally substituted benzyl, phenethyl, naphthylmethyl or naphthylethyl.Type: GrantFiled: February 12, 1991Date of Patent: February 2, 1993Assignee: Bayer AktiengesellschaftInventors: Klaus-Helmut Muller, Joachim Kluth, Klaus Konig, Karl-Rudolf Gassen, Kurt Findeisen, Markus Lindig, Klaus Lurssen, Hans-Joachim Santel, Robert R. Schmidt
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Patent number: 5180418Abstract: Cycloalkanecarboxylic acid derivatives of formula I ##STR1## wherein W is ##STR2## and A is CO--R.sub.3 or CN; R.sub.1 is hydrogen or fluorine; R.sub.2 is halogen or cyano; R.sub.3 is chlorine, X--R.sub.5, amino, C.sub.1 -C.sub.4 alkylamino, d-C.sub.1 -C.sub.4 alkylamino, C.sub.2 -C.sub.4 haloalkylamino, di-C.sub.2 -C.sub.4 haloalkylamino, C.sub.1 -C.sub.4 hydroxyalkylamino, di-C.sub.1 -C.sub.4 hydroxyalkylamino, C.sub.3 -C.sub.4 alkenylamino, diallylamino, --N-pyrrolidino, --N-piperidino, --N-morpholino, --N-thiomorpholino, --N-piperidazino, the group --O--N.dbd.C--(R.sub.9)R.sub.10 or the group --N--R.sub.6 (OR.sub.6); each of R.sub.4 and R.sub.14, independently of the other, is hydrogen, fluorine, chlorine, bromine, C.sub.1 -C.sub.4 alkyl or trifluoromethyl; R.sub.5 is hydrogen, C.sub.1 -C.sub.10 alkyl, C.sub.1 -C.sub.4 alkoxy-C.sub.1 -C.sub.4 alkyl, halo-C.sub.1 -C.sub.8 alkyl, C.sub.1 -C.sub.10 alkylthio-C.sub.1 -C.sub.4 alkyl, di-C.sub.1 -C.sub.4 alkylamino-C.sub.1 -C.sub.4 alkyl, cyano-C.sub.1 -C.sub.Type: GrantFiled: July 19, 1991Date of Patent: January 19, 1993Assignee: Ciba-Geigy CorporationInventors: Georg Pissiotas, Hans Moser, Hans-Georg Brunner, Eginhard Steiner
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Patent number: 5154912Abstract: The peroxides which include the O.sup.17 isotope, especially the hydrogen peroxides and peroxides and hydroperoxides prepared therefrom, are well adapted as nonradioactive labeled compounds for use in the medicinal and biological arts.Type: GrantFiled: September 20, 1990Date of Patent: October 13, 1992Assignee: AtochemInventors: Jean-Pierre Schirmann, Jean-Jacques Barieux
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Patent number: 5153212Abstract: 2-adamantyl-4-isothiazoline-3-one has the formula ##STR1## wherein R.sub.1 and R.sub.2, each independently, represent hydrogen or halogen,or R.sub.1 and R.sub.2, taken together, form a polymethylene chain having 3-4 carbon atoms, optionally substituted by lower alkyl or halogen,or R.sub.1 and R.sub.2, taken together, form a pyridine ring with the double bond of the 4-isothiazoline-3-one ring andAda represents 1'-adamantyl, 2'-adamantyl or 1'-adamantyl methyl, and its mineral or organic acid salt.The compound is useful as an antibacteria, antialgae or antifungus agent in various industrial fields.Type: GrantFiled: June 3, 1991Date of Patent: October 6, 1992Assignee: Centre International de Recherches Dermatoglogiques (C.I.R.D.)Inventors: Braham Shroot, Jean Maignan, Rainer Schmidt
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Patent number: 5145611Abstract: Carboxylic acid derivatives of the formula ##STR1## R.sub.1 is alkoxy, alkylthio, alkylsulphinyl, alkulsulphonyl, alkylamino, cycloalkyl, or cycloalkoxy or optionally substituted aryl, aryloxy, arylthio, arylsulphinyl, arylsulphonyl or arylamino. R.sub.2 is optionally substituted aryl or, when B is alkylene also a hydrogen atom. A is a straight-chained or branched, saturated or unsaturated alkylene containing 3 to 10 carbon atoms which is optionally interrupted by a heteratom attached to a saturated carbon and has a chain length of at least 3 atoms. Y is S(O).sub.n group or oxygen, n being 0, 1 or 2. B is a valency bond or a straight-chained or branched, saturated or unsaturated alkylene containing 1 to 18 carbon atoms. Physiologically acceptable salts, esters and amides thereof are also included. The compounds are useful in the treatment of metabolic diseases.Type: GrantFiled: January 12, 1988Date of Patent: September 8, 1992Assignee: Boehringer Mannheim GmbHInventors: Hans P. Wolff, Ernst-Christian Witte, Hans-Frieder Kuehnle
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Patent number: 5059623Abstract: A substituted cycloalkyl- or heterocyclyl-carboxanilide of the formula (I) ##STR1## in which X stands for an unsubstituted or an alkyl-substituted cycloalkyl or an unsubstituted or an alkyl-substituted heterocyclic,Hal stands for halogen andY.sup.1, Y.sup.2 and Y.sup.3 independently of one another stand for hydrogen, halogen, an unsubstituted or a halogen-substituted alkyl, an unsubstituted or a halogen-substituted alkoxy or an unsubstituted or a halogen-substituted alkylthio. Such substituted cycloalkyl- or heterocyclyl-carboxanilides are useful as fungicides.Type: GrantFiled: April 5, 1989Date of Patent: October 22, 1991Assignee: Bayer AktiengesellschaftInventors: Bernd-Wieland Kruger, Klaus Sasse, Hermann Hagemann, Albrecht Marhold, Wilhelm Brandes
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Patent number: 4987257Abstract: Disclosed is a diacetylene compound comprising, as structural units, (a) at least one member selected from diacetylene group-containing organic groups of the formulae (I) and (II):R.sup.I --C.tbd.C--C.tbd.C--R.sup.II -- (I)and--R.sup.III --C.tbd.C--C.tbd.C--R.sup.IV -- (II)wherein R.sup.I is hydrogen or a (C1-16) monovalent organic group, and R.sup.II, R.sup.III and R.sup.IV are a (C1-13) divalent organic group, (b) at least one organic group having at least one carbon-to-carbon double bond, and (c) at least one connecting group connecting the units (a) and (b), which connecting group is selected from amide, imide, ester, ether, amino, imino, urethane, sulfonyl and carbonyl bonds. A cured shaped article made of this compound exhibits isotropically a high elastic modulus and has excellent mechanical properties.Type: GrantFiled: February 23, 1990Date of Patent: January 22, 1991Assignee: Director-General of Agency of Industrial Science and TechnologyInventors: Katsuyuki Nakamura, Satoru Yamazaki, Jinichiro Kato, Kensaku Tokushige
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Patent number: 4931591Abstract: Compounds of the formula ##STR1## in which R.sub.1 represents hydrogen or acyl, A represents an optionally N-alkylated .alpha.-amino acid residue which is bonded N-terminally to R.sub.1 and C-terminally to the group --NR.sub.2 --, R.sub.2 represents hydrogen or lower alkyl, R.sub.3 represents hydrogen, lower alkyl, optionally etherified or esterified hydroxy-lower alkyl, cycloalkyl, cycloalkyl-lower alkyl, bicycloalkyl-lower alkyl, tricycloalkyl-lower alkyl, aryl or aryl-lower alkyl, R.sub.4 represents hydroxy or etherified or esterified hydroxy, R.sub.5 represents lower alkyl having 2 or more carbon atoms, optionally etherified or esterified hydroxy-lower alkyl, cycloalkyl, cycloalkyl-lower alkyl, bicycloalkyl, bicycloalkyl-lower alkyl, tricycloalkyl, tricycloalkyl-lower alkyl, aryl, aryl-lower alkyl, optionally substituted carbamoyl, optionally substituted amino, optionally substituted hydroxy or optionally substituted mercapto and R.sub.Type: GrantFiled: July 12, 1989Date of Patent: June 5, 1990Assignee: Ciba-Geigy CorporationInventors: Peter Buhlmayer, Vittorio Rasetti, Walter Fuhrer, James L. Stanton, Richard Goschl
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Patent number: 4898977Abstract: The invention relates to novel processes and intermediates for the preparation of 5-amino-4-hydroxyvaleric acid derivatives of the formula ##STR1## in which R.sup.1 represents hydrogen, optionally substituted alkyl, cycloalkyl, cycloalkyl-lower alkyl, aryl, aryl-lower alkyl or the radical of a natural amino acid, R.sup.2 represents hydrogen, optionally substituted alkyl, cycloalkyl, cycloalkyl-lower alkyl, aryl, aryl-lower alkyl, amino, hydroxy, mercapto, sulphinyl, sulphonyl or the radical of a natural amino acid, and R.sup.3 represents optionally substituted hydroxy or amino, by sigmatropic rearrangement of a suitable allyl ester, halolactonisation of the resulting .gamma.,.delta.-unsaturated acid or of a suitable derivative thereof, exchange of halogen for a nitrogen-containing nucleophile, opening of the lactone ring and freeing of the amino group. Compounds of the formula I are starting materials for the preparation of renin-inhibitors which have an anti-hypertensive action.Type: GrantFiled: August 13, 1987Date of Patent: February 6, 1990Assignee: Ciba-Geigy CorporationInventors: Peter Herold, Christof Angst
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Patent number: 4876343Abstract: An improved process for the preparation of statine, the phenyl analog of statine, the cyclohexyl analog of statine and derivatives thereof is described, as well as other valuable intermediates used in the process.Type: GrantFiled: June 15, 1988Date of Patent: October 24, 1989Assignee: Warner-Lambert CompanyInventors: John C. Hodges, Sylvester Klutchko
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Patent number: 4861885Abstract: The present invention relates to amides of formula I ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are independently hydrogen or methyl, m is 1 to 5 and n is 1 to 5 and R.sup.4 is --NH.sub.2 or is derived from a mono- to pentavalent amine.Intermediates of formula VIII ##STR2## wherein R.sup.1, R.sup.2, R.sup.3 and m are as defined above and X is a carboxylic acid or acid ester group, --COCl, --COBr, --CHO or --CN, are also described.The compounds of formula I can be polymerized thermally. They are suitable for the preparation of adhesives, matrix resins or electrical insulating materials.Type: GrantFiled: December 8, 1986Date of Patent: August 29, 1989Assignee: Ciba-Geigy CorporationInventors: Andreas Kramer, Roland Darms
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Patent number: 4851541Abstract: A process for preparing a 4,5-tri or tetramethylene-4-isothiazoline-3-one comprises cyclizing a 2-alkyl or aralkyl thio-1-cycloalkene-1-carboxamide in the form of its sulfoxide in an organic solvent in the presence of a acid chloride and adding to the resulting 4,5-tri or tetramethylene-4-isothiazoline-3-one hydrochloride a mineral or organic base or water so as to free the 4,5-tri or tetramethylene-4-isothiazoline-3-one in the form of a free base.Type: GrantFiled: June 5, 1986Date of Patent: July 25, 1989Assignee: Centre International de Recherches Dermatologiques (C.I.R.D.)Inventors: Jean Maignan, Serge Restle, Michel Colin
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Patent number: 4806570Abstract: Compounds of formula I ##STR1## in which R.sub.1 is C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, C.sub.3-7 cycloalkyl, cycloalkylalkyl or optionally substituted phenyl; R.sub.2 is H or C.sub.1-3 alkyl; R.sub.3 and/or R.sub.4 are H, formyl, C.sub.1-3 alkyl, C.sub.3-6 alkenyl, C.sub.3-6 alkynyl, C.sub.3-7 cycloalkyl or R.sub.3 and R.sub.4 together with the nitrogen atom form a heterocyclic ring system; R.sub.5 and/or R.sub.6 are H, halo, CF.sub.3, C.sub.1-3 alkyl, C.sub.1-3 alkoxy, C.sub.1-3 alkylthio or R.sub.5 and R.sub.6 together with the carbon atoms to which they are attached form a second benzene ring show therapeutic activity in the treatment of depression. Pharmaceutical compositions and processes for preparing compounds of formula I are disclosed.Type: GrantFiled: December 23, 1985Date of Patent: February 21, 1989Assignee: The Boots Company plcInventors: James E. Jeffery, Antonin Kozlik, Eric C. Wilmhurst
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Patent number: 4797152Abstract: Novel cyclohexenonecarboxylic acid derivatives exhibit herbicidal and plant growth regulating activity.The cyclohexanedionecarboxylic derivatives are of the formula I ##STR1## wherein A is an aliphatic or aromatic alcohol, or is an amino group which may be substituted by halogen, lower alkoxy, lower alkylthio, nitro or cyano, or is a heterocyclic amino group which is unsubstituted or substituted,R is C.sub.1 -C.sub.6 alkyl or C.sub.3 -C.sub.6 cycloalkyl, each unsubstituted or substituted by halogen, C.sub.1 -C.sub.4 alkoxy or C.sub.1 -C.sub.4 alkylthio,R.sub.1 is C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 haloalkyl, C.sub.3 -C.sub.6 alkenyl, C.sub.3 -C.sub.6 haloalkenyl or C.sub.3 -C.sub.6 alkylnyl,B is an aliphatic or aromatic radical or is an aliphatic or aromatic carbonyl or sulfonyl group which may be substitued by halogen, lower alkoxy, lower alkylthio, nitro or cyano.The compounds are suitable for selectively controlling grasses in crops of useful plants.Type: GrantFiled: November 14, 1986Date of Patent: January 10, 1989Assignee: Ciba-Geigy CorporationInventor: Hans-Georg Brunner
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Patent number: 4794197Abstract: All-cis-1,3,5-Triamino-2,4,6-trihydroxycyclohexane derivatives corresponding to the general formula I ##STR1## wherein the symbols R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 and R.sub.6 are identical or different and represent hydrogen atoms, alkyl groups or --CO-alkyl groups wherein the alkyl in the alkyl or --CO-alkyl group has 1 to 18 carbon atoms and the alkyl and --CO-alkyl groups may contain, independently of one another, one or more identical or different functional groups, and at least one of the groups R.sub.1 to R.sub.6 is one of the above mentioned unsubstituted or substituted alkyl groups or --CO-alkyl groups, and their salts with pharmacologically conventionally used inorganic or organic acids and their quaternary ammonium salts, processes for their preparation and their use, and pharmaceutical preparations containing these compounds.Type: GrantFiled: January 31, 1986Date of Patent: December 27, 1988Inventors: Walter Schneider, Isidor Erni, Hans K. Hegetschweiler
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Patent number: 4781751Abstract: Compounds of the formula ##STR1## wherein R is halogen; C.sub.1 -C.sub.2 alkyl; C.sub.1 -C.sub.2 alkoxy; trifluoromethoxy; difluoromethoxy; nitro; cyano; C.sub.1 -C.sub.2 haloalkyl; R.sup.a SO.sub.n -- wherein n is 0 or 2 and R.sup.a is C.sub.1 -C.sub.2 alkyl; trifluoromethyl or difluoromethyl;R.sup.1 is hydrogen, C.sub.1 -C.sub.4 alkyl, halogen, phenyl or substituted phenyl;R.sup.2 is hydrogen or C.sub.1 -C.sub.4 alkyl; orR.sup.1 and R.sup.2 together are C.sub.2 -C.sub.5 alkylene;R.sup.3 is hydrogen, C.sub.1 -C.sub.4 alkyl, phenyl or substituted phenyl, with the proviso that R.sup.1 and R.sup.3 are not both phenyl or substituted phenyl;R.sup.4 is hydrogen or C.sub.1 -C.sub.4 alkyl;R.sup.5 is hydrogen, halogen or C.sub.1 -C.sub.4 alkyl;R.sup.6 is halogen, cyano, nitro, trifluoromethyl, --C(O)--OR.sup.f wherein R.sup.f is C.sub.1 -C.sub.4 alkyl, or --C(O)NR.sub.2.sup.b wherein R.sup.b is hydrogen or C.sub.1 -C.sub.2 alkyl;R.sup.7 and R.sup.8 independently are (1) hydrogen; (2) halogen; (3) C.sub.1 -C.sub.Type: GrantFiled: October 2, 1987Date of Patent: November 1, 1988Assignee: Stauffer Chemical CompanyInventor: Hsiao-Ling M. Chin
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Patent number: 4760179Abstract: Substituted aminoxy propionamide derivatives corrsponding to the formula ##STR1## said derivatives being useful as color improvers and stabilizers in various polymeric substrates.Type: GrantFiled: April 4, 1986Date of Patent: July 26, 1988Assignee: Ciba-Geigy CorporationInventor: Ramanathan Ravichandran
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Patent number: 4736055Abstract: Oxime sulfonates of formula I ##STR1## wherein Y is a polymerizable unsaturated group or epoxide group or an --OH, --NHR.sup.5, --COOH, COOR.sup.6, --COCl, --CH.sub.2 Hal, --SO.sub.2 Cl or --NCO group, Z is an (x+y)-valent connecting member, R.sup.1 and R.sup.2 are monovalent organic radicals, m is 0 or 1, x is 1 or 2 and y is 1 or 2, can be converted into polymers which can be thermally or photochemically dissociated to form free sulfonic acid groups. Said polymers can therefore be used as photoresists which can be developed with aqueous alkalis.Type: GrantFiled: April 11, 1986Date of Patent: April 5, 1988Assignee: Ciba-Geigy CorporationInventors: Kurt Dietliker, Werner Rutsch, Godwin Berner, Max Hunziker, Christopher G. Demmer
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Patent number: 4711958Abstract: Amino acid derivatives represented by formula ##STR1## wherein His represents an L-histidyl group, X represents a straight or branched alkoxy group having 1 to 7 carbon atoms, a straight or branched alkylamino group having 1 to 7 carbon atoms, a cycloalkyloxy group having 3 to 7 carbon atoms, a morpholino group, said alkoxy group having one or more halogen atoms as substituents; or a pharmaceutically acceptable salt, are useful in the treatment of hypertension.Type: GrantFiled: April 1, 1987Date of Patent: December 8, 1987Assignee: Kissei Pharmaceutical Co., Ltd.Inventors: Kinji Iizuka, Tetsuhide Kamijo, Tetsuhiro Kubota, Kenji Akahane, Hideaki Umeyama, Yoshiaki Kiso
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Patent number: 4693745Abstract: Novel cyclohexanedionecarboxylic acid derivatives have herbicidal and plant growth regulating properties. The cyclohexanedionecarboxylic acid derivatives have the formula I ##STR1## wherein A is an --OR.sub.2 or --NR.sub.3 R.sub.4 radical,R is C.sub.3 -C.sub.6 cycloalkyl,R.sub.2, R.sub.3 and R.sub.4 are each independently hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 haloalkyl, C.sub.2 -C.sub.10 alkoxyalkyl, C.sub.2 -C.sub.10 alkylthioalkyl; C.sub.3 -C.sub.6 alkenyl which is unsubstituted or substituted by halogen, C.sub.1 -C.sub.4 alkoxy or C.sub.1 -C.sub.4 alkylthio; C.sub.3 -C.sub.6 alkynyl; phenyl or C.sub.1 -C.sub.6 aralkyl, wherein the phenyl nucleus is unsubstituted or substituted by halogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 haloalkyl, nitro or cyano; one of R.sub.3 and R.sub.4 is methoxy; orR.sub.3 and R.sub.Type: GrantFiled: October 9, 1985Date of Patent: September 15, 1987Assignee: Ciba-Geigy CorporationInventor: Hans-Georg Brunner
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Patent number: 4636505Abstract: Acylanilides of the formula ##STR1## wherein R.sup.1 and R.sup.2, the same or different, each is cyano, carbamoyl, nitro, halogeno, perfluoroalkyl or other defined substituents;R.sup.3 is hydrogen or halogen;R.sup.4 is hydrogen or alkyl, or is joined to R.sup.5 ;R.sup.5 is hydrogen, hydroxy, alkoxy or acyloxy or is joined to R.sup.4 ;R.sup.6 is alkyl or halogenoalkyl, or has the formula --A.sup.3 --R.sup.8 or --A.sup.4 --X.sup.2 --A.sup.5 --R.sup.9 ;A.sup.1 and A.sup.4, the same or different, each is alkylene;A.sup.2, A.sup.3 and A.sup.5, the same or different, each is a direct link or alkylene;X.sup.1 and X.sup.2, the same or different, each is oxygen, sulphur, sulphinyl, sulphonyl, imino or alkylimino;R.sup.7 and R.sup.9, the same or different, each is alkyl, alkenyl, hydroxyalkyl, cycloalkyl, phenyl optionally substituted, naphthyl or heterocyclic optionally substituted;and R.sup.8 is phenyl, naphthyl or heterocyclic as defined above for R.sup.7 or R.sup.Type: GrantFiled: July 15, 1983Date of Patent: January 13, 1987Assignee: Imperial Chemical Industries PLCInventor: Howard Tucker
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Patent number: 4623382Abstract: Novel cyclohexanedionecarboxylic acid derivatives have herbicidal and plant growth regulating properties. The cyclohexanedionecarboxylic acid derivatives have the formula I ##STR1## wherein A is an --OR.sub.2 or --NR.sub.3 R.sub.4 radical,R is C.sub.1 -C.sub.6 alkyl or C.sub.3 -C.sub.6 cycloaklyl, each unsubstituted or substituted by halogen, C.sub.1 -C.sub.6 alkoxy or C.sub.2 -C.sub.4 alkylthio,R.sub.1 is C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 haloalkyl, C.sub.3 -C.sub.6 -alkenyl, C.sub.3 -C.sub.6 haloalkenyl or C.sub.3 -C.sub.6 -alkynyl,R.sub.2, R.sub.3 and R.sub.4 are each independently hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 haloalkyl, C.sub.2 -C.sub.10 alkoxyalkyl, C.sub.2 -C.sub.10 alkylthioalkyl; C.sub.3 -C.sub.6 alkenyl which is unsubstituted or substituted by halogen, C.sub.1 -C.sub.4 alkoxy or C.sub.1 -C.sub.4 alkylthio; C.sub.3 -C.sub.6 alkynyl; phenyl or C.sub.1 -C.sub.6 aralkyl, wherein the phenyl nucleus is unsubstituted or substituted by halogen; C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.Type: GrantFiled: October 16, 1985Date of Patent: November 18, 1986Assignee: Ciba-Geigy CorporationInventor: Hans-Georg Brunner
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Patent number: 4619944Abstract: Provided are antihypertensive compounds of the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, and R.sub.6 are hydrogen, alkyl, alkenyl, alkynyl, phenyl-alkyl, or cycloalkyl, and may be the same or different,m is an integer from 0 to 2 inclusive,n is an integer from 0 to 4 inclusive,M is alkenyl, alkynyl, cycloalkyl, cycloalkyl-alkyl, polycycloalkyl, polycycloalkyl-alkyl, aryl, aralkyl, heteroaryl, heteroaryl-alkyl, hetero-cycloalkyl, hetero-cycloalkyl-alkyl, fused aryl-cycloalkyl, fused aryl-cycloalkyl-alkyl, fused heteroaryl-cycloalkyl, fused heteroaryl-cycloalkyl-alkyl, alkoxyalkyl, alkylthioalkyl, alkylamino-alkyl, or dialkylaminoalkyl.Y is hydroxy, alkoxy, amino, or substituted amino, aminoalkanoyl, aryloxy, aminoalkoxy, or hydroxyalkoxy, andR.sub.7 is alkyl, aryl, aralkyl, cycloalkyl, cycloalkyl-alkyl, heterocyclic, --CO--SR, --CS--SR, ##STR2## CH.sub.2 CO.sub.2 R, --CHM--CO.sub.2 R, --CH.sub.2 --CO--SR, --CN, ##STR3## --CO--NH--CH.sub.2 CO.sub.2 R, ##STR4## or --CO--CO.sub.Type: GrantFiled: February 19, 1985Date of Patent: October 28, 1986Assignee: USV Pharmaceutical CorporationInventors: Raymond D. Youssefyeh, Howard Jones
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Patent number: 4618360Abstract: Novel cyclohexanedionecarboxylic acid derivatives have herbicidal and plant growth regulating properties. The cyclohexanedionecarboxylic acid derivatives have the formula I ##STR1## wherein A is an --OR.sub.2 or --NR.sub.3 R.sub.4 radical,B is hydroxyl, an --NHOR.sub.1 radical or a metal or ammonium salt thereofR is C.sub.1 -C.sub.6 alkyl or C.sub.3 -C.sub.6 cycloalkyl, each unsubstituted or substituted by halogen, C.sub.1 -C.sub.6 alkoxy or C.sub.2 -C.sub.4 alkythio,R.sub.1 is C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 haloalkyl, C.sub.3 -C.sub.6 alkenyl, C.sub.3 -C.sub.6 haloalkenyl or C.sub.3 -C.sub.6 alkynyl,R.sub.2, R.sub.3 and R.sub.4 are each independently hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 haloalkyl, C.sub.2 -C.sub.10 alkoxyalkyl, C.sub.2 -C.sub.10 alkylthioalkyl; C.sub.3 -C.sub.6 alkenyl which is unsubstituted or substituted by halogen, C.sub.1 -C.sub.4 alkoxy or C.sub.1 -C.sub.4 alkylthio; C.sub.3 -C.sub.6 alkynyl; phenyl or C.sub.1 -C.sub.Type: GrantFiled: November 19, 1984Date of Patent: October 21, 1986Assignee: Ciba-Geigy CorporationInventor: Hans-Georg Brunner
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Patent number: 4584013Abstract: Novel cyclohexanedionecarboxylic acid derivatives have herbicidal and plant growth regulating properties.The cyclohexanedionecarboxylic acid derivatives have the formula I ##STR1## wherein A is an --OR.sub.2 or --NR.sub.3 R.sub.4 radical,B is hydroxyl, an --NHOR.sub.1 radical or a metal or ammonium salt thereofR is C.sub.1 -C.sub.6 alkyl or C.sub.3 -C.sub.6 cycloalkyl, each unsubstituted or substituted by halogen, C.sub.1 -C.sub.6 alkoxy or C.sub.2 -C.sub.4 alkylthio,R.sub.1 is C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 haloalkyl, C.sub.3 -C.sub.6 alkenyl, C.sub.3 -C.sub.6 haloalkenyl or C.sub.3 -C.sub.6 alkynyl,R.sub.2, R.sub.3 and R.sub.4 are each independently hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 haloalkyl, C.sub.2 -C.sub.10 alkoxyalkyl, C.sub.2 -C.sub.10 alkylthioalkyl; C.sub.3 -C.sub.6 alkenyl which is unsubstituted or substituted by halogen, C.sub.1 -C.sub.4 alkoxy or C.sub.1 -C.sub.4 alkylthio; C.sub.3 -C.sub.6 alkynyl; phenyl or C.sub.1 -C.sub.Type: GrantFiled: May 14, 1984Date of Patent: April 22, 1986Assignee: Ciba-Geigy CorporationInventor: Hans-Georg Brunner
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Patent number: 4569689Abstract: Aniline derivatives of the formula ##STR1## where R.sup.1 is alkoxy, alkylthio, unsubstituted or substituted cycloalkoxy or the radical --NR.sup.2 R.sup.3, X is --CH.sub.2 --, --CH(OH)-- or --CO--, A is an unsubstituted or substituted alkylene chain, B is unsubstituted or substituted methylene or dimethylene, Z is hydrogen, halogen, alkyl, alkoxy, haloalkyl or haloalkoxy, and n is 1, 2 or 3, are used for controlling undesirable plant growth.Type: GrantFiled: June 14, 1984Date of Patent: February 11, 1986Assignee: BASF AktiengesellschaftInventors: Ulrich Schirmer, Norbert Goetz, Bruno Wuerzer
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Patent number: 4570014Abstract: Novel plant growth regulant composition comprising as an active ingredient at least one cycloalkanecarboxylic acid compound of the formula ##STR1## in which R is hydroxyl, alkoxy, aralkoxy, amino, alkylamino, dialkylamino or the radicalO.sup..crclbar. M.sup..sym.whereinM.sup..sym. is one alkali metal ion equivalent or alkaline earth metal ion equivalent, or an ammonium, alkylammonium, dialkylammonium, trialkylammonium or tetraalkylammonium ion,R.sup.1 is amino or the radical ##STR2## wherein R.sup.2 is hydrogen, alkyl or aryl, orR.sup.1 is the radical --N.sup..sym. H.sub.3 X.sup..crclbar.,wherein X.sup.63 is chloride, bromide or iodide, and n is 1, 2, 3, 4 or 5,in admixture with a solid or liquefied gaseous diluent or carrier or in admixture with a liquid diluent or carrier containing a surface-active agent.Type: GrantFiled: December 15, 1981Date of Patent: February 11, 1986Assignee: Bayer AktiengesellschaftInventors: Rolf Schroder, Klaus Lurssen
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Patent number: 4529813Abstract: Insecticidally active vinyl-cyclopropane carboxylic acid esters of the formula ##STR1## are prepared by reacting ##STR2## in which R.sup.12 is a radical selected from the group consisting of ##STR3## with an alcoholate of the formulaM--O--R.sup.8.Various processes for making the intermediates are also described. Many of the intermediates and end products are new.Type: GrantFiled: March 14, 1980Date of Patent: July 16, 1985Assignee: Bayer AktiengesellschaftInventors: Hans-Georg Heine, Willy Hartmann
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Patent number: 4515982Abstract: Organic materials which contain from 0.001 to 10% by weight of an aminoreductone I ##STR1## where R.sup.1, R.sup.2 and R.sup.3 are H, methyl or ethyl and R.sup.4 is the radical of a naturally occurring .alpha.- or .beta.-aminoacid or of a C.sub.1 -C.sub.10 -alkyl ester thereof or, in the case of an .alpha.-aminoacid, a lactone having a 2--OH group in the cyclohexenone ring, or R.sup.4 is C.sub.1 -C.sub.20 -alkyl which is unsubstituted or substituted by --OH, C.sub.1 -C.sub.4 -alkoxy or C.sub.1 -C.sub.4 -acyloxy, or is --(CH.sub.2 --CH.sub.2 --O).sub.n H, which may be etherified with a C.sub.1 -C.sub.4 -alkanol or esterified with a C.sub.1 -C.sub.4 -fatty acid, and where n is from 2 to 10, or a mineral salt thereof.Novel compounds Ia differ from I in having the radical R.sup.4a, where R.sup.4a is R.sup.4 with the exception of methyl. Compounds I are prepared by reacting the corresponding 2,3-dihydroxycyclohex-2-en-1-one with an amine HN(R.sup.3)R.sup.4 or a mineral acid salt thereof.Type: GrantFiled: December 15, 1982Date of Patent: May 7, 1985Assignee: BASF AktiengesellschaftInventors: Peter Lechtken, Gerhard Mueller, Klaus Schmieder
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Patent number: 4503232Abstract: The invention provides a novel method for the preparation of an .alpha.-ketoamide imine having a characteristic structure expressed by the formula ##STR1## in which R is a group such as an alkyl, aryl or the like group, in a one-step reaction in which a halogen-containing organic compound reacts with a primary amine and carbon monoxide in the presence of a carbonylation catalyst. The product compound is useful as an intermediate for the synthesis of various kinds of organic compounds including medicines and agricultural chemicals.Type: GrantFiled: September 24, 1982Date of Patent: March 5, 1985Assignee: Agency of Industrial Science & TechnologyInventors: Toshiaki Kobayashi, Masato Tanaka
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Patent number: 4476061Abstract: The present invention relates to 2'-(ortho-chlorobenzoyl)-4'-chloroglycylanilides, compositions thereof, and their use as medicaments, e.g., as anxiolytic agents.The compounds of the invention have the general formula I ##STR1## in which R represents hydrogen or alkyl,R.sub.1 and R.sub.2 may be identical or different and are selected from hydrogen, alkyl, hydroxyalkyl, alkenyl, and alkynyl, possibly substituted by alkyl, and cycloalkyl having three to six members, possibly substituted by alkyl, with the proviso that, when one of R.sub.1 and R.sub.2 represents hydrogen, the other is not lower alkyl or hydroxyalkyl; and with the further proviso that R.sub.1 and R.sub.2 may not simultaneously represent either hydrogen or lower-alkyl. R.sub.1 and R.sub.2 may furthermore form, with the nitrogen atom to which they are connected, a nitrogen heterocycle possibly containing a second heteroatom selected from oxygen and nitrogen.Type: GrantFiled: August 18, 1982Date of Patent: October 9, 1984Assignee: Pierre Fabre, SAInventors: Gilbert Mouzin, Henri Cousse, Antoine Stenger
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Patent number: 4474806Abstract: Sulfonyl or carbonyl derivatives of inositols are found to be effective phospholipase C inhibitors and thereby potent anti-inflammatory and analgesic agents. These inositol derivatives are prepared by condensation of a protected inositol with a substituted sulfonic or carboxylic acid derivative followed by removal of protecting groups.Type: GrantFiled: May 10, 1982Date of Patent: October 2, 1984Assignee: Merck & Co., Inc.Inventors: Thomas R. Beattie, Shu S. Yang
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Patent number: 4473694Abstract: Process for the synthesis of hindered polysubstituted .alpha.-amino acetamides which comprises first reacting an .alpha.-haloacetamide with a base to form an intermediate .alpha.-lactam which in turn is reacted with a primary or secondary amine. The product thus obtained can comprise a multifunctional compound having one or more hindered amino moieties. These compounds are highly effective as UV stabilizers in a variety of plastics, especially the alpha monoolefins.Type: GrantFiled: September 29, 1982Date of Patent: September 25, 1984Assignee: The B. F. Goodrich CompanyInventor: John T. Lai
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Patent number: 4455263Abstract: Mono- and di-2-hydroxyethane sulfonate derivatives and 2-aminoethane sulfonate derivatives of C.sub.21 -cycloaliphatic dicarboxylic acid having the general formula ##STR1## where x and y are integers from 3 to 9, x and y together equal 12, R is ##STR2## and M.sup.+ is an alkali metal, ammonium or amine cation, are disclosed as emulsion polymerization emulsifiers.Type: GrantFiled: March 15, 1983Date of Patent: June 19, 1984Assignee: Westvaco CorporationInventor: John W. Noble
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Patent number: 4425360Abstract: The present invention provides pyruvic acid oximes of the general formula: ##STR1## wherein R is a hydrogen atom, a C.sub.3 -C.sub.8 cycloalkyl, C.sub.1 -C.sub.6 alkoxy, cinnamyloxy, phenylamino, phenyl-N-alkylamino or phenylthio radical or an aryl or aryloxy radical, the aryl moiety of which can be substituted one or more times by C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, halogen, hydroxyl, trifluoromethyl, amino, acetylamino, nitrile, nitro or methylenedioxy, A is a straight-chained or branched, saturated or unsaturated aliphatic hydrocarbon chain containing up to 10 carbon atoms, which can be substituted one or more times by halogen or hydroxyl, and R.sub.1 is a C.sub.1 -C.sub.8 alkyl radical, which can be substituted one or more times by halogen, hydroxyl, nitrile, phenyl or carboxyl, or is a nitrile or formyl group, with the proviso that when R--A-- is a methyl or ethyl radical, R.sub.1 is not a methyl radical or a nitrile group and when R--A-- is a benzyl radical, R.sub.Type: GrantFiled: September 8, 1981Date of Patent: January 10, 1984Assignee: Boehringer Mannheim GmbHInventors: Hans P. Wolff, Ruth Heerdt, Manfred Hubner, deceased, Hans Kuhnle, Felix H. Schmidt
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Patent number: 4380667Abstract: The present invention relates to 2'-(ortho-chlorobenzoyl)-4'-chloroglycylanilides, compositions thereof, and their use as medicaments, e.g., as anxiolytic agents.The compounds of the invention have the general formula I ##STR1## in which R represents hydrogen or alkyl,R.sub.1 and R.sub.2 may be identical or different and are selected from hydrogen, alkyl, hydroxyalkyl, alkenyl, and alkynyl, possibly substituted by alkyl, and cycloalkyl having three to six members, possibly substituted by alkyl, with the proviso that, when one of R.sub.1 and R.sub.2 represents hydrogen, the other is not lower alkyl or hydroxyalkyl; and with the further proviso that R.sub.1 and R.sub.2 may not simultaneously represent either hydrogen or lower alkyl. R.sub.1 and R.sub.2 may furthermore form, with the nitrogen atom to which they are connected, a nitrogen heterocycle possibly containing a second heteroatom selected from oxygen and nitrogen.Type: GrantFiled: September 19, 1979Date of Patent: April 19, 1983Assignee: Pierre Fabre S.A.Inventors: Gilbert Mouzin, Henri Cousse, Antoine Stenger
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Patent number: 4370497Abstract: The present invention relates to the use of telluroxides as mild and selective oxidizing agents serving to oxidize certain functions, notably >C.dbd.S groups, in the presence of other relatively easily oxidized functions which remain unaffected; telluroxides of interest as oxidizing agents include, for example, compounds of the formula: ##STR1## wherein R and R.sup.1, which may be the same or different, each represent an optionally substituted aryl or heterocyclic group; or R and R.sup.1 together with the tellurium atom therebetween represent a heterocyclic ring, which may contain one or more further heteroatoms, and which may carry substituents and/or fused aromatic rings.Type: GrantFiled: August 7, 1980Date of Patent: January 25, 1983Inventors: Derek H. R. Barton, Steven V. Ley, Clive A. Meerholz
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Patent number: 4347379Abstract: Numerous alpha-carboxylic acids are prepared in a liquid medium by the reaction of an organic compound having at least one reactive hydroxyl or thiol group, with a monoketone, and a haloform, in the presence of a phase transfer catalyst and an alkali metal hydroxide. The term "alpha-alkoxycarboxylic acids" includes alpha-phenoxycarboxylic acids, alpha-thioalkoxycarboxylic acids and alpha-thiophenoxycarboxylic acids. Specific substituents on the beta carbon atom of an alpha-alkoxycarboxylic (or "2-alkoxycarboxylic") acid reaction product formed in this novel synthesis, are introduced by appropriate choice of the ketone reactant; alkoxy and phenoxy substituents on the alpha carbon atom of a 2-alkoxycarboxylic acid are introduced by appropriate choice of the organic compound having a hydroxyl or thiol group. De-alkoxylation of the 2-alkoxycarboxylic acid yields alpha-beta monoolefinically unsaturated carboxylic acids which are necessarily alpha substituted, and may also be beta-substituted.Type: GrantFiled: March 10, 1980Date of Patent: August 31, 1982Assignee: The B. F. Goodrich CompanyInventor: John T. Lai
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Patent number: 4342705Abstract: Vulcanizable rubber compositions are described which are inhibited from premature vulcanization by activated methylene di(thioethers) in which the adjacent activating groups are either carbonyl or cyano. Novel compounds are also described.Type: GrantFiled: December 1, 1980Date of Patent: August 3, 1982Assignee: Monsanto CompanyInventors: Otto W. Maender, Eiichi Morita
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Patent number: 4329363Abstract: The present application discloses a method of correcting an imbalance of immune homeostasis caused by cytostatic treatment or radiotherapy by administering to a patient in need of such treatment an effective amount of a novel substituted mercapto acid amide and pharmaceutical compositions containing such novel substituted mercapto acid amides.Type: GrantFiled: January 16, 1980Date of Patent: May 11, 1982Assignee: Merck & Co., Inc.Inventors: Conrad P. Dorn, Howard Jones
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Patent number: 4327111Abstract: Mammalian collagenase is inhibited by compounds having the formula ##STR1## or a salt thereof, wherein R.sub.1 is hydrogen, alkanoyl of 2 to 10 carbon atoms, or arylcarbonyl; ##STR2## wherein R.sub.4 is hydrogen, alkyl or aryl; R.sub.3 is alkyl of 3 to 8 carbon atoms, cycloalkyl of 3 to 7 carbon atoms, aryl or arylalkyl; andn is an integer of 1 to 20.Type: GrantFiled: July 14, 1980Date of Patent: April 27, 1982Assignee: E. R. Squibb & Sons, Inc.Inventors: Joseph E. Sundeen, Tamara Dejneka
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Patent number: 4322553Abstract: The disclosure herein relates to a new process for the preparation of N-(halomethyl)acylamides by reacting the corresponding N-(alkoxymethyl)acylamide with thionyl chloride or thionyl bromide in the presence of a Lewis Acid catalyst.Type: GrantFiled: February 2, 1981Date of Patent: March 30, 1982Assignee: Monsanto CompanyInventor: John P. Chupp
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Patent number: 4315031Abstract: This invention relates to thiosubstituted cyclic amino acids, to a process for their preparation and to pharmaceutical compositions containing them together with an inert non toxic pharmaceutical carrier.Type: GrantFiled: August 28, 1978Date of Patent: February 9, 1982Assignee: Science Union et CieInventors: Michel Vincent, Georges Remond, Jacques Bure
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Patent number: RE31237Abstract: New derivatives of 2-benzoyl-4-nitro anilides, their preparation and their use as medicaments.The new chemical derivatives of the invention have the general formula ##STR1## in which R represents a linear or branched alkyl group, an alkenyl group, a cycloalkyl group or a benzyl group,R.sub.1 represents a hydrogen atom, an alkyl group or a hydroxy alkyl group,R.sub.2 represents a hydroxy-alkyl, alkenyl or alkynyl group, possibly substituted one or more times by an alkyl radical, or a cycloalkyl group having three to six carbon atoms;R.sub.1 and R.sub.2 may furthermore form, with the nitrogen atom to which they are attached, a nitrogen heterocycle containing possibly a second heteroatom selected from among oxygen and nitrogen;under the condition, however, that when R.sub.2 represents a hydroxy-alkyl group R.sub.1 may not be a hydrogen atom.Use as hypnotic agents for the treatment of insomnia.Type: GrantFiled: February 19, 1982Date of Patent: May 10, 1983Assignee: Pierre Fabre S.A.Inventors: Henri Cousse, Gilbert Mouzin