The Chalcogen, X, Is In A -c(=x)- Group Patents (Class 544/399)
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Patent number: 5089619Abstract: Certain dithiocarbamates are used as reverse demulsifiers, corrosion and scale inhibitors, flocculants, biocides, flotation aids, water clarifiers, interface control agents and antifoaming agents.Type: GrantFiled: June 30, 1989Date of Patent: February 18, 1992Assignee: Petrolite CorporationInventors: Neil E. S. Thompson, Robert G. Asperger
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Patent number: 5064863Abstract: Tertiary and secondary amines of the formulas ##STR1## wherein n is the integer 1 or 2, p0 R is hydrogen, lower-alkanoyl or phenyl-lower-alkanoyl,X.sup.1 is phenoxymethyl optionally mono-fluorinated or mono-chlorinated in the ortho-position,X.sup.2 is lower-alkyl, phenoxymethyl optionally mono-fluorinated or mono-chlorinated in the ortho-position or phenyl optionally monosubstituted by fluorine, chlorine, trifluoromethyl or lower-alkoxy,Y is hydrogen or methyl, andZ is a phenyl or thienyl residue substituted as hereinafter described,and the physiologically and pharmaceutically compatible salts are described. The compounds of formulas I and V-1 have catabolic activity and can be used for the treatment of obesity and diabetes mellitus or for the treatment of conditions which are associated with an increased protein breakdown, or as feed additives for fattening animals. The compounds of formulas I and V-1 can be prepared starting from corresponding primary amines.Type: GrantFiled: December 10, 1987Date of Patent: November 12, 1991Assignee: Hoffmann-La Roche Inc.Inventors: Leo Alig, Marcel Muller
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Patent number: 5039673Abstract: Compounds are described of the formula (1) ##STR1## where: R.sup.1 is a hydrogen atom or a methyl group;X is cis or trans --CH.dbd.CH-- or --CH.sub.2 CH.sub.2 --, m is 2, 3 or 4 and n is 1; or X is trans --CH.dbd.CH--, m is zero and n is 3;Y is a saturated heterocyclic amino group;Alk is a C.sub.1-5 alkyl chain;l is zero or 1;p is zero, 1, 2, 3 or 4;R.sup.2 is a hydroxyl group or a group selected from --OCOR.sup.3, --CO.sub.2 R.sup.3, CONR.sup.3 R.sup.4, --SO.sub.2 NR.sup.3 R.sup.4, --NHCOR.sup.3, --NHSO.sub.2 R.sup.5, --SO.sub.2 R.sup.5, --SR.sup.5, --NR.sup.3 R.sup.4, --COR.sup.5, --NHCONR.sup.3 R.sup.4 and --NHCSNH.sub.2 ; and their physiologically acceptable salts, solvates and cyclodextrin complexes.These compounds inhibit blood platelet aggregation, bronchoconstriction and vasoconstriction and may be formulated for use as antithrombotic agents.Type: GrantFiled: August 22, 1989Date of Patent: August 13, 1991Assignee: Glaxo Group LimitedInventors: Eric W. Collington, Harry Finch, Roger Hayes, Keith Mills, David F. Woodings
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Patent number: 5026853Abstract: A method of improving sleep in warm-blooded animals suffering from sleep disorders, which method comprises the administration of particular N-aryl-piperazinealkanamide derivatives and compositions containing the same. Novel N-aryl-piperazinealkanamide derivatives.Type: GrantFiled: September 20, 1990Date of Patent: June 25, 1991Assignee: Janssen Pharmaceutica N.V.Inventors: Georges H. P. Van Daele, Freddy F. Vlaeminck, Marc G. C. Verdonck
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Patent number: 5001160Abstract: Compounds are disclosed having the formula: ##STR1## in which R.sub.1 is a C.sub.1 l to C.sub.12 alkyl, said alkyl being straight or branched chain, saturated or unsaturated, monosubstituted or unsubstituted, said substituents being selected from piperidine, pyrrolidine, morpholine, thiomorpholine or cycloalkyl of 3 to 7 carbons, a cycloalkyl of 3 to 9 carbons, a lower alkylcycloalkyl of 4 to 9 carbons, or a polycycloalkyl of 2 to 3 rings containing 7 to 12 carbons;R.sub.Type: GrantFiled: June 27, 1989Date of Patent: March 19, 1991Assignee: Marion Laboratories, Inc.Inventors: Daniel W. McPherson, John P. Carter
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Patent number: 4990592Abstract: An anionic emulsifier obtained from the reaction products of an alkyl phenol, polyamine, and formaldehyde or of an alkyl phenol, fatty acid/polyamine condensate, and formaldehyde followed by the reaction of such products with acrylic acid, and the uses of the emulsifier in anionic bituminous emulsions and paving slurry seal mixtures are disclosed.Type: GrantFiled: November 27, 1989Date of Patent: February 5, 1991Assignee: Westvaco CorporationInventor: Peter Schilling
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Patent number: 4990591Abstract: An anionic emulsifier obtained from the reaction products of an alkyl phenol, polyamine, and formaldehyde or of an alkyl phenol, fatty acid/polyamine condensate, and formaldehyde followed by the reaction of such products with acrylic acid, and the uses of the emulsifier in anionic bituminous emulsions and paving slurry seal mixtures are disclosed.Type: GrantFiled: April 7, 1989Date of Patent: February 5, 1991Assignee: Westvaco CorporationInventor: Peter Schilling
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Patent number: 4988817Abstract: A process is provided for obtaining quaternary ammonium or phosphonium substituted carbonic acid esters. The first step involves reacting the hydroxyl predecessor compound of the ester with phosgene in an aprotic organic solvent to obtain a solution of chloroformate/hydrogen chloride complex. In a second step, the chloroformate/hydrogen chloride complex in solution is admixed with a salt whose conjugate anion, normally a phenol sulfonate, has structure L. During the admixing step, pH is maintained no lower than 6 until all reactants have been combined to form the product ester. Thereupon, pH is lowered to less than 5.5 to stabilize product against hydrolysis.Type: GrantFiled: November 16, 1988Date of Patent: January 29, 1991Assignee: Lever Brothers Company, Division of Conopco, Inc.Inventors: Stephen A. Madison, Jeffrey Bonn, Eddie N. Gutierrez
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Patent number: 4987053Abstract: Compounds of the general formula I ##STR1## are described in which Q denotes ##STR2## R denotes alkyl, hydroxyalkyl or aryl, R.sup.1 and R.sup.2 denote H, alkyl or alkoxyalkyl,R.sup.3 denotes H, methyl or ethyl,D.sup.1 and D.sup.2 denote saturated hydrocarbon groups,E denotes alkylene, cycloalkylene, arylene, saturated or unsaturated heteroyls or a group of the formula II ##STR3## a and b denote integers from 1 to 4. c denotes an integer from 1 to 3,m denotes 2, 3 or 4, depending on the valency of Q, andn denotes an integer from 1 to m, where all radicals of the same definition may be identical to or different from one another.The compounds are suitable as polymerizable compounds for photopolymerizable mixtures and are distinguished by ready polymerizability in combination with photoinitiators and long shelf lives in the layer.Type: GrantFiled: November 14, 1988Date of Patent: January 22, 1991Assignee: Hoechst AktiengesellschaftInventors: Joachim Gersdorf, Klaus Rose
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Patent number: 4985556Abstract: Perfluorocarboxylic acid fluorides represented by the formula A-B, wherein A is either ##STR1## and B stands for a perfluoro-di-substituted amino group, and perfluoro(dialkylaminopropenes) represented by the formula A"-B", wherein A" stands for ##STR2## and B" has the same meaning as B defined above, are novel compounds. Methods for the production of these novel compounds are also disclosed.Type: GrantFiled: September 9, 1988Date of Patent: January 15, 1991Assignees: Agency of Industrial Science & Technology, Ministry of International Trade & IndustryInventors: Takashi Abe, Eiji Hayashi
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Patent number: 4985561Abstract: A process is described for obtaining sulfophenyl quaternary ammonium or phosphonium substituted carbonic acid esters. These esters are prepared through sulfonation with sulfur trioxide of aromatic chloroformates followed by reaction of the sulfonated aromatic chloroformate with quaternary ammonium or phosphonium substituted alcohols. The resultant sulfophenyl esters are useful as bleach precursors in combination with peroxygen compounds such as sodium perborate or percarbonate.Type: GrantFiled: August 29, 1989Date of Patent: January 15, 1991Assignee: Lever Brothers Company, Division of Conopco, Inc.Inventors: Stephen A. Madison, Leonora M. Ilardi, Hans Cerfontain
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Patent number: 4981853Abstract: The compounds of this invention are heterocyclic amides represented by the formula: ##STR1## wherein: R.sub.1 and R.sub.2 are the same or different members of the group consisting of halo, phenyl, substituted phenyl and a ##STR2## group wherein q, r and t are independently an integer of from 1 to 8 provided that q+r+t is equal to or less than 10; Y is thio, sulfinyl or sulfonyl; Alk is straight or branched chain lower alkylene, and R.sub.3 is a heterocyclic amine represented by the formula: ##STR3## wherein R.sub.4 is selected from the group consisting of hydrogen, lower alkyl, phenyl, substituted phenyl, benzyl, substituted benzyl, carboxyl or carboxyloweralkyl; X is selected from the group consisting of N-R.sub.4, O and CH.sub.2 ; m is 2 or 3; n is 2 or 3 when X is O or N-R.sup.4, and n is 1 to 3 when X is CH.sub.2 ; p is 0 to 2; and the pharmaceutically acceptable salts thereof. The compounds are anti-inflammatory and anti-allergy agents.Type: GrantFiled: November 14, 1989Date of Patent: January 1, 1991Assignee: G. D. Searle & Co.Inventors: Richard A. Mueller, Richard A. Partis
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Patent number: 4980378Abstract: Biodegradable absorption enhancers, especially useful in pharmaceutical formulations, are compounds having the formula ##STR1## wherein R is hydrogen, C.sub.1 -C.sub.7 alkyl, benzyl or 4-hydroxybenzyl; n is a whole number from 4 to 18 inclusive; R.sub.1 and R.sub.2 are independently selected from hydrogen and C.sub.1 -C.sub.7 alkyl, or R.sub.1 and R.sub.2 together with the nitrogen atom to which they are attached are combined to form a substituted or unsubstituted heterocycloalkyl radical having a total of 5 to 7 ring atoms, optionally including a hetero ring atom selected from oxygen, sulfur and nitrogen in addition to the indicated nitrogen atom, the substituents when present being one to three C.sub.1 -C.sub.7 alkyl radicals, which may be the same or different; and R.sub.3 and R.sub.4 are independently selected from hydrogen, methyl and ethyl.Type: GrantFiled: June 1, 1988Date of Patent: December 25, 1990Assignee: Odontex, Inc.Inventors: Ooi Wong, Toshiaki Nishiahta, Joseph H. Rytting
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Patent number: 4980377Abstract: The present invention relates to the preparation of new 1-(aminophenyl)-2-aminopropanone derivatives of the general formula: ##STR1## in which X is NH.sub.2, Y is H or a halogen atom, Z is H or a halogen atom, R.sub.1 is C.sub.1 -C.sub.4 alkyl or C.sub.3 -C.sub.6 cycloalkyl and R.sub.2 is H or C.sub.1 -C.sub.4 alkyl, or R.sub.1 and R.sub.2, taken together, can form, with the nitrogen atom to which they are bonded, a heterocyclic group selected from the group consisting of the pyrrolidino, morpholino, thiomorpholino, piperidino, hexamethyleneimino, piperazino, 4-methyl-piperazino, 4-(.beta.-hydroxyethyl)piperzaino, 4-phenylpiperazino and 4-(p-chlorophenyl)piperazino groups, and addition salts thereof.These new derivatives are useful as pharmaceuticals. They are obtained by deacetylation of the corresponding acetylated products.Type: GrantFiled: November 14, 1988Date of Patent: December 25, 1990Assignee: Laboratoire L. LafonInventor: Louis Lafon
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Patent number: 4959366Abstract: A series of [N-alkyl-N-(nitro-, alkylsulphonamido, or amino-phenalkyl)amino]-alkyl, alkoxy or alkylthio phenyl derivatives having utility as anti-arrhythmic agents.Type: GrantFiled: April 29, 1987Date of Patent: September 25, 1990Assignee: Pfizer Inc.Inventors: Peter E. Cross, Geoffrey N. Thomas, John E. Arrowsmith
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Patent number: 4933442Abstract: The present invention relates, by way of new industrial products, to 1-(acetylaminophenyl)-2-amino-propanone derivatives selected from the group consisting of(a) the compounds of the formulaAr--CO--CH(CH.sub.3)--NR.sub.1 R.sub.2 (I)in whichR.sub.1 represents a C.sub.1 -C.sub.4 alkyl group or a C.sub.3 -C.sub.6 cycloalkyl group;R.sub.2 represents the hydrogen atom or a C.sub.1 -C.sub.4 alkyl group;R.sub.1 and R.sub.2, taken together, can form, with the nitrogen atom to which they are bonded, an N-heterocyclic group with 5 to 7 ring members, capable (i) of including a second heteroatom selected from N, O and S, and (ii) of being substituted, the said heterocyclic group NR.sub.1 R.sub.2 being selected from the group comprising pyrrolidino, morpholino, thiomorpholino, piperidino, hexamethyleneimino, piperazino, 4-methylpiperazino, 4-(.beta.-hydroxyethyl) piperazino, 4-phenylpiperazino and 4-(p-chlorophenyl)-piperazino groups; andAr represents an acetylaminophenyl group of the formula ##STR1## in which X is CH.Type: GrantFiled: July 6, 1989Date of Patent: June 12, 1990Assignee: Laboratoire L. LafonInventor: Louis Lafon
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Patent number: 4912220Abstract: Nitroaryl carbonyl Formula (IIA) compounds, their nitrodihydroaryl carbonyl Formula (I) intermediates, processes for preparing Formula (II) compounds, and a process for preparing Formula (I) compounds, wherein each process comprises the reaction of a nitroaryl compound with a silane.Type: GrantFiled: February 3, 1988Date of Patent: March 27, 1990Assignee: E. I. Du Pont de Nemours and CompanyInventor: Thaliyil V. Rajanbabu
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Patent number: 4902818Abstract: The manufacture of optically active bifunctional compounds of the general formula ##STR1## wherein R represents protected hydroxymethyl, protected formyl or alkoxycarbonyl and R.sup.1 represents a group of the formula ##STR2## in which R.sup.2 and R.sup.3 represents lower alkyl or cycloalkyl or R.sup.2 and R.sup.3 together with the nitrogen atom represent a heterocyclic ring, by isomerizing compounds of the general formula ##STR3## wherein R, R.sup.2 and R.sup.3 have the above significance and R.sup.3 can additionally signify hydrogen, is described.The compounds of formula I are potential intermediates in the manufacture of, interalia, natural vitamin E and natural vitamin K.sub.1.Type: GrantFiled: October 5, 1988Date of Patent: February 20, 1990Assignee: Hoffmann-La Roche Inc.Inventors: Hans-Jurgen Hansen, Rudolf Schmid, Max Schmid
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Patent number: 4889953Abstract: Compounds of the formula: ##STR1## wherein R.sup.1 is a higher alkyl group which may be substituted; R.sup.2 is a hydrogen, a lower alkyl group which may be substituted, a lower alkanoyl group which may be substituted or a lower alkylthiocarbamoyl group; R.sup.3 is a primary to tertiary amino group or a quaternary ammonium group; and n is 2 or 3, and salts thereof, have antitumor activity and platelet activating factor inhibitory activity.Type: GrantFiled: July 22, 1987Date of Patent: December 26, 1989Assignee: Takeda Chemical Industries, Ltd.Inventors: Keizo Inoue, Hiroaki Nomura, Tetsuya Okutani
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Patent number: 4880800Abstract: Compounds are described of the formula ##STR1## where: R.sup.1 is --H or --CH.sub.3,n is 1, m is 2-4 and X is --CH.dbd.CH-- or --CH.sub.2 CH.sub.2 --;Y is a saturated heterocyclic amino group,R.sup.2 is (i) substituted or unsubstituted phenylalkyl, thineylalkyl or naphthylalkyl or (ii) cinnamyl, and their salts and solvates.These compounds inhibit blood platelet aggregation, bronchoconstriction and vasoconstriction and may be formualted for use as antithrombotic or antiasthmatic agents.Type: GrantFiled: September 15, 1987Date of Patent: November 14, 1989Assignee: Glaxo Group LimitedInventors: Christopher J. Wallis, Harry Finch, Peter Hallett
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Patent number: 4880808Abstract: A method of improving sleep in warm-blooded animals suffering from sleep disorders, which method comprises the administration of particular N-aryl-piperazinealkanamide derivatives and compositions containing the same. Novel N-aryl-piperazinealkanamide derivatives.Type: GrantFiled: March 9, 1988Date of Patent: November 14, 1989Assignee: Janssen Pharmaceutica N.V.Inventors: Georges H. P. Van Daele, Freddy F. Vlaeminck, Marc G. C. Verdonck
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Patent number: 4877789Abstract: Compound, corresponding to the formulaC.sub.8 H.sub.17 --(C.tbd.C--CH.sub.2).sub.3 --CH.sub.2 CH.sub.2 CH.sub.2 R O (I)in which R is a C.sub.1 -C.sub.8 lower alkoxy or C.sub.4 -C.sub.6 cycloalkoxy group, substituted with one or more hydroxyl groups and/or interrupted by one or more hetero atoms chosen from oxygen and sulphur, an amino group of structure ##STR1## in which R.sub.1 or R.sub.2, which may be identical or different, denote a hydrogen atom or a linear or branched C.sub.1 -C.sub.8 lower alkyl radical, optionally interrupted by one or more hetero atoms chosen from oxygen, sulphur and nitrogen, this alkyl radical being able to be substituted with one or more hydroxyl groups, R.sub.1 and R.sub.2 not being able to denote hydrogen simultaneously, or alternatively R.sub.1 and R.sub.2 form, together with the nitrogen atom, a heterocyclic system optionally containing oxygen, sulphur or nitrogen as an additional hetero atom, one of the radicals R.sub.1 and R.sub.Type: GrantFiled: July 3, 1986Date of Patent: October 31, 1989Assignee: Centre International de Recherches Dermatologiques dite C.I.R.D.Inventors: Braham Shroot, Christopher Hensby, Jean Maignan, Gerard Lang, Serge Restle, Michel Colin
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Patent number: 4877812Abstract: The present invention relates, by way of new industrial products, to 1-(acetylaminophenyl)-2-amino-propanone derivatives selected from the group consisting of(a) the compounds of the formulaAr--CO--CH(CH.sub.3)--NR.sub.1 R.sub.2 (I)in whichR.sub.1 represents a C.sub.1 -C.sub.4 alkyl group or a C.sub.3 -C.sub.6 cycloalkyl group;R.sub.2 represents the hydrogen atom or a C.sub.1 -C.sub.4 alkyl group;R.sub.1 and R.sub.2, taken together, can form, with the nitrogen atom to which they are bonded, an N-heterocyclic group with 5 to 7 ring members, capable (i) of including a second heteroatom selected from N, O and S, and (ii) of being substituted, the said heterocyclic group NR.sub.1 R.sub.2 being selected from the group comprising pyrrolidino, morpholino, thiomorpholino, piperidino, hexamethyleneimino, piperazino, 4-methylpiperazino, 4-(.beta.-hydroxyethyl) piperazino, 4-phenylpiperazino and 4-(p-chlorophenyl)-piperazino groups; andAr represents an acetylaminophenyl group of the formula ##STR1## in which X is CH.Type: GrantFiled: April 16, 1987Date of Patent: October 31, 1989Assignee: Laboratoire L. LafonInventor: Louis Lafon
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Patent number: 4874771Abstract: The synthesis of novel ethanesulfonamide compounds is described. The novel ethanesulfonamide compounds have antisecretory activity and are used in the treatment of peptic ulcer disease.Type: GrantFiled: September 6, 1988Date of Patent: October 17, 1989Assignee: Ortho Pharmaceutical CorporationInventor: Ronald K. Russell
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Patent number: 4855489Abstract: The present invention covers a novel series of 2-acyloxypropylamine derivatives, processes for preparing them, compositions containing them, and methods for using them. The compounds are active in the inhibition of protein kinase C and thrombocyto aggregation stimulated by diacylglycerols.Type: GrantFiled: July 15, 1987Date of Patent: August 8, 1989Assignee: Goedecke AktiengesellschaftInventors: Uwe Trostmann, Christoph Schachtele, Karl Mannhardt, Claus Rudolph, Dieter Marme
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Patent number: 4836958Abstract: The instant invention relates to fluorinated cationic compounds of the formula ##STR1## wherein R.sub.f is a perfluoroalkyl or perfluoroalkoxy-perfluoroalkyl group;R.sub.1 is alkylene optionally interrupted by --O--, --S--, --SO.sub.2 --, --SO.sub.2 NR'--, --CO.sub.2 --, --NR'--, or --CONR'-- where R' is hydrogen or lower alkyl;m is 0, 1 or 2;R.sub.2 is linear or branched alkylene;R.sub.3, R.sub.4, and R.sub.5 independently of one another represent alkyl or arylalkyl groups which are unsubstituted or substituted by hydroxyl, lower alkoxy, halogen, cyano or by polyalkyleneoxy, or R.sub.3 and R.sub.4 together with the nitrogen atom to which they are attached represent a 5- or 6-membered heterocyclic radical or R.sub.3, R.sub.4 and R.sub.5 together with nitrogen atom that links them represent a substituted or unsubstituted pyridine ring; andA.sup..crclbar. represents the anion of an organic or inorganic acid; and their particular use as surfactants.Type: GrantFiled: July 31, 1986Date of Patent: June 6, 1989Assignee: Ciba-Geigy CorporationInventor: Athanasios Karydas
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Patent number: 4810725Abstract: 1-Aryloxy-3-(substituted aminoalkylamino)-2-propanols and pharmaceutically acceptable salts thereof have .beta.-adrenergic blocking activity with some cardioselectivity and hence are useful as anti-hypertensive, antianginal, antiarrhythmic and cardioprotective agents and in the treatment of elevated intraocular pressure such as glaucoma.Type: GrantFiled: October 14, 1986Date of Patent: March 7, 1989Assignee: Merck & Co., Inc.Inventors: John J. Baldwin, Gerald S. Ponticello, Sandor L. Varga
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Patent number: 4797400Abstract: Novel piperazine compounds of the formula: ##STR1## wherein either one of R.sup.1 and R.sup.2 is methoxy group and another is hydrogen atom, or a pharmaceutically acceptable acid addition salt thereof, which have excellent anti-peptic ulcer activities with potent activity for promoting the action of the defensive factor, and hence are useful as an anti-ulcer agent for the prophylaxis and treatment of peptic ulcers.Type: GrantFiled: June 16, 1987Date of Patent: January 10, 1989Assignee: Kanebo, Ltd.Inventors: Hiroshi Ohtaka, Kenji Yoshida, Kenji Suzuki, Koichi Shimohara, Sigeru Tajima, Keizo Ito
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Patent number: 4783535Abstract: A process for the preparation of 1,4-oxazepinones and thiones having the formula: ##STR1## wherein A is an aromatic ring selected from benzene, naphthalene, quinoline or pyridine; n is 1 to 3; Z is an amino radical; R is hydrogen, loweralkyl, cycloalkyl or phenylloweralkyl; and R.sup.4 and R.sup.5 are hydrogen and loweralkyl starting from chloroaromatic carboxylates and alkanolamines is disclosed. The oxazepinones and oxazepinethiones prepared by the process have utility as antihistaminics with low sedative potential. Novel intermediate compounds are also disclosed.Type: GrantFiled: March 18, 1986Date of Patent: November 8, 1988Assignee: A. H. Robins Company, IncorporatedInventors: Young S. Lo, Albert D. Cale, Jr.
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Patent number: 4783537Abstract: Novel .alpha.-aryl-.alpha.-(.omega.-aminoalkyl)-.alpha.-[hydroxy(aralkyl and cycloalkyl)]acetic acid derivatives and .alpha.-aryl-.alpha.-(.omega.-aminoalkyl)-.alpha.[alkanoyloxy(aralkyl and cycloalkyl)]acetic acid derivatives, such as N,N-dimethyl-2-(hydroxyphenylmethyl)-4-dimethylamino-2-phenylbutanamide, 2-(hydroxyphenylmethyl)-5-dimethylamino-2-phenylpentanenitrile, ethyl 2-(hydroxyphenylmethyl)-5-dimethylamino-2-phenylpentanoate, and N,N-dimethyl-2[(acetyloxy)phenylmethyl]-4-dimethylamino-2-phenylbutanamide , useful in the treatment of cardiovascular disease.Type: GrantFiled: November 13, 1985Date of Patent: November 8, 1988Assignee: Pennwalt CorporationInventor: Robert J. Murray
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Patent number: 4766125Abstract: Novel N-aryl-piperazinealkanamides, having particular substituents attached to one of the carbon atoms of the piperazine ring, which compounds are useful to protect hearts from myocardial injury caused by ischaemia, anoxia or hypoxia.Type: GrantFiled: March 29, 1982Date of Patent: August 23, 1988Assignee: Janssen Pharmaceutica N.V.Inventor: Georges Van Daele
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Patent number: 4760146Abstract: Novel compounds and processes for making and using them. The compounds include ethyl 1-[3-(1-piperidinyl)propyl]-6-phenyl-3-cyclohexene-1-carboxylate, 1-[3-(1-piperidinyl)propyl]-6-phenyl-3-cyclohexene-1-carboxyamide, and N,N-dimethyl-1-[3-(1-piperidinyl)propyl]-6-phenyl-3-cyclohexene-1-carboxam ide.Type: GrantFiled: February 18, 1986Date of Patent: July 26, 1988Assignee: Pennwalt CorporationInventor: Bruce H. Toder
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Patent number: 4743690Abstract: Nitroaryl carbonyl Formula (IIA) compounds, their nitrodihydroaryl carbonyl Formula (I) intermediates, processes for preparing Formula (II) compounds, and a process for preparing Formula (I) compounds, wherein each process comprises the reaction of a nitroaryl compound with a silane.Type: GrantFiled: January 16, 1987Date of Patent: May 10, 1988Assignee: E. I. Du Pont de Nemours and CompanyInventor: Thaliyil V. Rajanbabu
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Patent number: 4739052Abstract: Compounds of the formula I, II or III ##STR1## in which Ar and Ar' are an oxygen-containing aromatic radical, R.sup.1 and R.sup.2 are a monovalent hydrocarbon radical which is substituted or unsubstituted, or R.sup.1 and R.sup.2 together form alkylene, oxaalkylene or azaalkylene, R.sup.3 is a direct bond or a divalent hydrocarbon radical, X and X' are a monovalent amino group and Y is a divalent amino or diamino group, are excellent photoinitiators for the photocuring of colored, especially pigmented, compositions containing an olefinically unsaturated, photopolymerizable binder.Type: GrantFiled: October 2, 1985Date of Patent: April 19, 1988Assignee: Ciba-Geigy CorporationInventors: Rinaldo Husler, Rudolf Kirchmayr, Werner Rutsch
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Patent number: 4734500Abstract: A novel sulfone compound represented by the general formula (I) ##STR1## wherein R.sup.1 is cyclohexyl, phenyl; or a phenyl substituted with a group selected from nitro, C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkoxy and halogen; R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are respectively hydrogen, halogen, cyano or carbonyl, wherein R.sup.1 and R.sup.2 may form an o-phenylene or an o-phenylene substituted with at least one group selected from nitro C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkoxy and halogen; X is oxygen or methylene; Y is --(CH.sub.2).sub.n --, wherein n is an integer of 0, 5 or 6, or ##STR2## wherein m is an integer 1-3; R.sup.6 is hydrogen, C.sub.1 -C.sub.3 alkyl, .omega.-alkylaminoalkyl, wherein each alkyl has 1-3 carbon atoms, or .omega.-dialkylaminoalkyl, wherein each alkyl has 1-3 carbon atoms; R.sup.7 is hydrogen or C.sub.1 -C.sub.3 alkyl; and R.sup.6 and R.sup.7 may form a ring together with N, or ##STR3## wherein R.sup.8 is hydrogen, C.sub.1 -C.sub.Type: GrantFiled: March 11, 1986Date of Patent: March 29, 1988Assignee: Mitsubishi Chemical Industries LimitedInventors: Akihiro Tobe, Shinichiro Fujimori, Tomoshi Yamazaki, Mamoru Sugano, Ryoji Kikumoto, Issei Nitta
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Patent number: 4734417Abstract: The invention relates to new derivatives of biphenyl primary alcohols, their preparation and use as medicaments useful in the treatment and prevention of atherosclerotic disorders. The new derivatives have the general formula ##STR1## in which X represents a halogen atom, and more particularly chlorine, bromine or fluorine in ortho or meta position,R represents an alkyl, amino alkyl, pyridyl alkyl or acyl radical and more particularly ##STR2## and acetyl.Type: GrantFiled: July 7, 1986Date of Patent: March 29, 1988Assignee: P.F. MedicamentInventors: Henri Cousse, Andre Delhon, Jean-Pierre Rieu, Gilbert Mouzin
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Patent number: 4713456Abstract: A process for the preparation of a 5-acylpyrimidine of the formula ##STR1## in which R is an organic radical comprising reacting a methyl ketone of the formulaR--CO--CH.sub.3in a first stage with a formylating reagent in the presence of a base to form an enolketone of the formulaR--CO--CH.dbd.CH--OR.sup.10in which R.sup.10 represents hydrogen or a base radical, thereafter reacting the enolketone in 2nd and 3rd stages with formamidine or a formamidine salt, and with an amino-formylating agent, and, in a 4th stage heating to cyclize the compound formed.The end products, some of which are new, are intermediates for making herbicides.Type: GrantFiled: August 26, 1985Date of Patent: December 15, 1987Assignee: Bayer AktiengesellschaftInventors: Hans-Ludwig Elbe, Graham Holmwood
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Patent number: 4680396Abstract: It has now been found that certain phosphonate derivatives of bis(aminoalkyl) piperazines are good threshold agents to prevent metal ion precipitation in aqueous solutions. They also function as sequestering and/or chelating agents as do those which do not contain the phosphonate group.Type: GrantFiled: February 24, 1984Date of Patent: July 14, 1987Assignee: The Dow Chemical CompanyInventors: Druce K. Crump, Jaime Simon, David A. Wilson
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Patent number: 4672136Abstract: Included are monoadduct monomers made from divinyl ketones wherein only one vinyl bond therein has added to it a nucleophilic precursor. Nucleophilic precursors include phenols, thiols, secondary amines, amino acids, hydrocarbyl phosphites and phosphite esters, organic bis(phosphonites, the bisulfite anion and others.Polyadduct polymers made from the monoadduct monomers. The polyadduct polymers may be homo- or copolymers and may contain a pendant nucleophile residue.Type: GrantFiled: December 24, 1985Date of Patent: June 9, 1987Assignee: The Dow Chemical CompanyInventors: Harold E. Doorenbos, Giffin D. Jones
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Patent number: 4659828Abstract: The methyl chloride or dimethyl sulfate quaternary ammonium salt of 1-acryloyl-4-methyl piperazine and polymers thereof.Type: GrantFiled: June 15, 1984Date of Patent: April 21, 1987Assignee: Nalco Chemical CompanyInventor: Dodd W. Fong
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Patent number: 4659862Abstract: Nitroaryl carbonyl Formula (IIA) compounds, their nitrodihydroaryl carbonyl Formula (I) intermediates, processes for preparing Formula (II) compounds, and a process for preparing Formula (I) compounds, wherein each process comprises the reaction of a nitroaryl compound with a silane.Type: GrantFiled: May 3, 1984Date of Patent: April 21, 1987Assignee: E. I. Du Pont de Nemours and CompanyInventor: Thaliyil V. Rajanbabu
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Patent number: 4659721Abstract: Alkanol derivatives corresponding to the general formula IR.sup.1 R.sup.2 N--(CH.sub.2).sub.m --Q--CH.sub.2 X--CH.sub.2 --Y--(CH.sub.2).sub.n --NHR.sup.3 (I)which have a highly selective action on histamine-H.sub.2 receptors are described. Due to this action, these compounds may advantageously be used for treatment of diseases caused by raised gastric secretion.Type: GrantFiled: January 22, 1985Date of Patent: April 21, 1987Assignee: Ludwig Heumann & Co. GmbHInventors: Helmut Schickaneder, Stefan Postius, Istvan Szelenyi, Peter Morsdorf, Rolf Herter, Kurt H. Ahrens
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Patent number: 4656277Abstract: The methyl chloride or dimethyl sulfate quaternary ammonium salt of 1-methacryloyl-4-methyl piperazine.Type: GrantFiled: June 15, 1984Date of Patent: April 7, 1987Assignee: Nalco Chemical CompanyInventors: Dodd W. Fong, David J. Kowalski
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Patent number: 4652649Abstract: A new class of anti-spasmodic compounds having two branch chains is provided. The compounds have the general formula: ##STR1## wherein the substituents are defined hereinbelow.Type: GrantFiled: February 20, 1985Date of Patent: March 24, 1987Assignee: United Pharmaceuticals, Inc.Inventor: William M. Davis
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Patent number: 4652679Abstract: Aziridine and phenethanolamine derivatives of formulae I and II-1 ##STR1## wherein R.sup.1 and R.sup.2 are hydrogen or lower-alkyl; Z.sup.1 is phenyl or a phenyl group substituted in a defined manner; Z.sup.2 and Z.sup.21 are phenyl or thienyl substituted in a defined manner; and, n is an integer from 1-4. The disclosed compounds have catabolic activity and can be used for the treatment of obesity and/or of sugar illnesses. The compounds of formula I are obtained by dehydrating .beta.-aminoalcohols (e.g. those of formula II-1) which, in turn, can be prepared by adding amines to epoxides or by reducing corresponding iminoketones, iminoalcohols a-keto-.beta.-hydroxyamines or .beta.-ketoamines.Type: GrantFiled: May 9, 1983Date of Patent: March 24, 1987Assignee: Hoffmann-La Roche Inc.Inventors: Leo Alig, Marcel Muller
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Patent number: 4647562Abstract: A new class of anti-spasmodic compounds having three branch chains is provided. These compounds have the general formula: ##STR1## where R.sub.1, R.sub.2 and R.sub.3 are saturated straight chain or branched alkyl groups contained from 1 to 8 carbon atoms, and are separated or linked to one another to form an aliphatic ring system. k is an integer from 0 to 5, and the total number of carbon atoms in R.sub.1 plus R.sub.2 plus R.sub.3 plus k are equal to or less than 12. Furthermore, l is an integer from 1 to 3, m is an integer from 1 to 3, n is an integer from 1 to 3, and X may be nonexistent or may be O, S, NH or CH.sub.2 or salts thereof. However, when X is nonexistent the terminal group in both the m chain and the n chain is a methyl group.Type: GrantFiled: February 20, 1985Date of Patent: March 3, 1987Assignee: United Pharmaceuticals, Inc.Inventor: William M. Davis
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Patent number: 4644083Abstract: The present invention relates to a process for the production of N-substituted .alpha.,.beta.-unsaturated carboxylic acid amides, which proceeds from the .alpha.,.beta.-unsaturated carboxylic acid amide that is unsubstituted at the amido nitrogen, which forms the Michael adduct initially by conversion with a polyvalent alcohol having a boiling point of >/=150.degree. C., converts this with a primary or secondary amine with elimination of ammonia to form N-substituted carboxylic acid amide with a protected double bond, the polyvalent alcohol being subsequently eliminated from this product at high temperatures, with formation of the N-substituted .alpha.,.beta.-unsaturated carboxylic acid amide.Type: GrantFiled: January 25, 1985Date of Patent: February 17, 1987Assignee: Chemische Fabrik Stockhausen GmbHInventors: Kurt Dahmen, Erich Kuster, Richard Mertens, Helmut Brehm
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Arylic derivatives of piperazine, the method of preparing same and their application in therapeutics
Patent number: 4639452Abstract: New derivatives are provided corresponding to the formula: ##STR1## in which Ar represents an aromatic nucleus; and X represents: either the trans ##STR2## chain or the ##STR3## chain and A=CONHOH, COOEt, COOH or CONR.sub.2 R.sub.3, either the trans-CH.dbd.CH--CH.sub.2 -- chain or --CH.sub.2 --CH.sub.2 --CH.sub.2 chain and A=carboxamido, N-isopropylcarboxamido, pyrrolidinocarbonyl or piperidinocarbonyl.These derivatives and their salts are used as drug for their activity stimulating, protecting and/or correcting cerebral functions.Type: GrantFiled: February 25, 1983Date of Patent: January 27, 1987Assignee: Delalande S.A.Inventors: Alain Y. Platel, Guy R. Bourgery, Alain Lacour, deceased -
Patent number: 4639453Abstract: New substituted 1-(4-amino-6,7-dialkoxyquinazolinyl)-4-cyclohexenyl derivatives of piperazine and homopiperazine, of the general formula I ##STR1## in which R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5, which can be identical or different, denote hydrogen, straight-chain or branched alkyl groups with in each case 1 to 6 carbon atoms, cyclic aliphatic radicals with in each case 5 to 7 carbon atoms, aromatic radicals or substituted aromatic radicals, which can be monosubstituted or polysubstituted by identical or different substituents from the group comprising halogen and lower alkyl groups with in each case 1 to 4 carbon atoms in the alkyl part, or denote aralkyl radicals, furanyl radicals or thienyl radicals, orR.sup.2 and R.sup.3 together denote the group --(CH.sub.2).sub.a --, wherein a is the number 4 or 5, orR.sup.3 and R.sup.4 together denote the group --(CH.sub.2).sub.b --, wherein b is the number 3, 4 or 5,R.sup.6 and R.sup.Type: GrantFiled: December 7, 1984Date of Patent: January 27, 1987Assignee: Beiersdorf AktiengesellschaftInventor: Werner Hansen
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Patent number: 4620005Abstract: Phenyl tetrahydronaphthylcarboxylate of the formula: ##STR1## wherein A is a direct bond, or a lower alkylene, vinylene or imino group; B is a direct bond, a lower alkylene or --NH-lower alkylene group, or an --OCH.sub.2 CO-- residual group; and R is a lower alkyl group, with the proviso that A and B are not direct bonds simultaneously, and A, B and R are not a lower alkylene group, a direct bond and a methyl group, respectively, at the same time, are effectively useful as chymotrypsin inhibitors.Type: GrantFiled: October 17, 1985Date of Patent: October 28, 1986Assignee: Kowa Co., Ltd.Inventors: Setsuro Fujii, Eizou Hattori, Mitsuteru Hirata, Hisashi Kunieda, Koichiro Watanabe, Hiroshi Ishihama