Carbonyl, Cyano, Nitro, Nitroso, Halogen, Or Sulfur Attached Directly To The Sulfonamide Nitrogen Or To An Amino Nitrogen In A Substituent E By Nonionic Bonding Patents (Class 564/91)
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Patent number: 5492896Abstract: The invention relates to new pseudopeptides having an antiviral action, oft he general formula (I) ##STR1## with the meanings given in the description for the substituents, to a process for their preparation and to their use as antiviral agents, in particular against cytomegaloviruses.Type: GrantFiled: February 15, 1994Date of Patent: February 20, 1996Assignee: Bayer AktiengesellschaftInventors: Dieter Habich, Michael Matzke, Klaus Frobel, Thomas Henkel, Hartwig Muller, Karl-Heinz Weber, Jurgen Reefschlager, Gert Streissle, Jutta Hansen, Rainer Neumann, Arnold Paessens
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Patent number: 5488160Abstract: The invention relates to the compounds of the formula ##STR1##Type: GrantFiled: December 9, 1993Date of Patent: January 30, 1996Assignee: Ciba-Geigy CorporationInventor: Michael M. Morrissey
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Patent number: 5481005Abstract: The invention relates to N-sulfonyl derivatives of formulae (I) and (I)' ##STR1## to their preparation, and to pharmaceutical compositions in which they are present. The compounds of formulae (I) and (I)' have an affinity for the vasopressin and ocytocin receptors.Type: GrantFiled: November 28, 1994Date of Patent: January 2, 1996Assignee: SanofiInventors: Jean Wagnon, Paul de Cointet, Dino Nisato, Claude Plouzane, Claudine Serradeil-Legal, Bernard Tonnerre
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Patent number: 5476874Abstract: Oligopeptide analogs containing sulfonamide, urea or carbamate linkages in the backbone are described. These compounds are useful in the inhibition of HIV protease, the prevention or treatment of infection by HIV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.Type: GrantFiled: June 22, 1994Date of Patent: December 19, 1995Assignee: Merck & Co., Inc.Inventors: Randall W. Hungate, Joseph P. Vacca
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Patent number: 5463122Abstract: Antibacterial and antiviral phenylthiols and dithiobisbenzamides have the formula ##STR1## where n is 1 or 2, Y is hydrogen when n is 1, and a single bond when n is 2; and R.sup.1 and R.sup.11 are substituent groups, R.sup.4 is hydrogen or alkyl, and Z is hydrogen, alkyl, cycloalkyl or sulfamoylphenyl.Type: GrantFiled: August 5, 1994Date of Patent: October 31, 1995Assignee: Warner-Lambert CompanyInventors: Edward F. Elslager, Rocco D. Gogliotti
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Patent number: 5451700Abstract: The invention relates to the compounds of the formula ##STR1## wherein the C(.dbd.NH)--NHR.sub.3 group may be in tautomeric or isomeric form, and phamaceutically acceptable salts thereof. The compounds are useful as selective LTB.sub.4 receptor antagonists.Type: GrantFiled: November 18, 1992Date of Patent: September 19, 1995Assignee: Ciba-Geigy CorporationInventors: Michael M. Morrissey, Hongsuk Suh
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Patent number: 5416117Abstract: A novel cyclopropenone derivative (I) which possesses a potent inhibitory activity against thiol protease such as papain, cathepsin B, cathepsin H, cathepsin L, calpain or the like with excellent properties regarding oral absorbance, tissue transference and cell membrane permeability, and are clinically useful in the treatment of various diseases such as muscular dystrophy, amyotrophy. Also provided are a process for producing the compound (I) and a pharmaceutical composition containing the same.Type: GrantFiled: February 28, 1994Date of Patent: May 16, 1995Assignee: Mitsubishi Kasei CorporationInventors: Ryoichi Ando, Yasuhiro Morinaka, Chizuko Takahashi, Yoshikuni Tamao, Akihiro Tobe
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Patent number: 5414120Abstract: The present invention relates to novel polyether-substituted compounds of imides and their use as surface-active agents.Type: GrantFiled: November 12, 1993Date of Patent: May 9, 1995Assignee: Bayer AGInventors: Klaus Pohmer, Rainer Weber, Cornelia Dorzbach-Lange, Reinhard Haida, Hans-Heinrich Moretto
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Patent number: 5328909Abstract: A novel cyclopropenone derivative (I) which possesses a potent inhibitory activity against thiol protease such as papain, cathepsin B, cathepsin H, cathepsin L, calpain or the like with excellent properties regarding oral absorbance, tissue transference and cell membrane permeability, and are clinically useful in the treatment of various diseases such as muscular dystrophy, amyotrophy. Also provided are a process for producing the compound (I) and a pharmaceutical composition containing the same.Type: GrantFiled: June 25, 1992Date of Patent: July 12, 1994Assignee: Mitsubishi Kasei CorporationInventors: Ryoichi Ando, Yasuhiro Morinaka, Chizuko Takahashi, Yoshikuni Tamao, Akihiro Tobe
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Patent number: 5280043Abstract: Phenylalkanoic acids containing a sulphonamido group, and their use in a method of treatment of thromboxane-A.sub.2 mediated diseases are disclosed. A compound of the invention is 4-[4-(phenyl-sulphonamido)phenyl]butyric acid.Type: GrantFiled: April 2, 1992Date of Patent: January 18, 1994Assignee: Smith Kline & French Laboratories Ltd.Inventors: David G. Cooper, Andrew D. Gribble
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Patent number: 5270301Abstract: The present invention relates to certain fluoro-amide derivatives, as described herein, which are human leukocyte elastase (HLE) inhibitors making them useful whenever such inhibition is desired, such as for research tools in pharmacological, diagnostic and related studies and in the treatment of diseases in mammals in which HLE is implicated, including treatment of tissue degenerative diseases such as pulmonary emphysema. The invention also includes intermediates useful in the synthesis of these fluoro-amide derivatives, processes for preparing them, pharmaceutical compositions containing such peptide derivatives and methods for their use.Type: GrantFiled: May 7, 1990Date of Patent: December 14, 1993Assignee: ICI Americas Inc.Inventor: Donald J. Wolanin
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Patent number: 5168101Abstract: A sulfonamide derivative of the general formula:Tx--R.sup.1 (I)wherein, R.sup.1 represents(i) COOR.sup.11,(ii) CH.sub.2 OR.sup.12 or(iii) CONR.sup.13 R.sup.14,Tx--represents ##STR1## X.sub.b represents(i) bond,(ii) alkylene group of from 1 to 4 carbon atoms or(iii) alkenylene group of from 2 to 4 carbon atoms (with the proviso that --CH.dbd.CHCH.sub.2 -- and --CH.sub.2 CH.dbd.CHCH.sub.2 -- are excluded),R.sup.2b represents(i) hydrogen atom,(ii) halogen atom or(iii) alkyl group of from 1 to 4 carbon atom(s), posses an antagonistic activity on TXA.sub.2.Type: GrantFiled: October 13, 1988Date of Patent: December 1, 1992Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Yoshinobu Arai, Nobuyuki Hamanaka, Tohru Miyazaki
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Patent number: 5135941Abstract: This invention relates to a compound of the formula: ##STR1## or a pharmaceutically acceptable salt thereof wherein X is oxygen, sulfur, --CH.dbd.CH-- or --CH.dbd.N--; wherein R.sub.1 is alkyl, alkenyl or alkynyl of about 1 to 20 carbon atoms; wherein R is --CO.sub.2 R.sup.2, tetrazole, methylsulfonamide or benzenesulfonamide, wherein R.sup.2 is hydrogen, alkyl of 1 to 6 carbon atoms or a pharmaceutically acceptable cation and R.sup.3 is hydroxyl or halogen, having utility as LTB.sub.4 synthesis inhibitors.Type: GrantFiled: November 4, 1991Date of Patent: August 4, 1992Assignee: G. D. Searle & Co.Inventors: Stevan W. Djuric, Richard A. Haack, Julie M. Miyashiro
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Patent number: 5124348Abstract: A compound of Formula (I):R.sup.1 (CA.dbd.CA.sup.1).sub.x --C(.dbd.X)NR.sup.2 R.sup.3 (I)where R.sup.1 is alkyl optionally substituted by a group selected from alkoxy, alkenyl, alkynyl, alkenyloxy, alkynyloxy, aryl, aryloxy, arylalkoxy and cycloalkyl fused to an aryl ring; x=1 or 2; X=O or S; each A and A.sup.1 is independently hydrogen, alkyl or haloalkyl; R.sup.2 is alkyl, alkenyl or cycloalkyl any of which may be substituted by halo, alkenyl, alkyl, cycloalkyl, alkynyl, dioxalanylalkyl or alkoxy; and R.sup.3 is selected from groups (A) to (D):(A) --Y.dbd.X.sup.1 --(R.sup.4).sub.a where X.sup.1 is O or S, Y is phosphorus or carbon, R.sup.4 is hydrogen, alkyl, alkoxy, acyl or CO.sub.2 R.sup.5 where R.sup.5 is alkyl or aryl, and a is 1 or 2(B) --S(R.sup.6)(O).sub.b where R.sup.6 is alkyl, aryl, aryloxy, alkoxy, thioalkoxy, thioaryl, alkythio, alkoxythio or arylthio and b is 0, 1 or 2(C) --S(O).sub.c NR.sup.7 R.sup.8 where c is 0, 1 or 2, R.sup.7 is --COR.sup.9 or --CO.sub.2 R.sup.9 where R.sup.Type: GrantFiled: May 17, 1991Date of Patent: June 23, 1992Assignee: Burroughs Wellcome Co.Inventors: Malcolm H. Black, Robert J. Blade, Robert J. Peek
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Patent number: 5081284Abstract: A novel N-substituted peptidyl compound represented by the general formula (1): ##STR1## where R.sub.1 is a straight-chained or branched acyl group having 2-10 carbon atoms, a branched, cyclic or partly branched cyclic alkyloxycarbonyl group having 4-15 carbon atoms, a substituted or unsubstituted benzyloxycarbonyl group, a 2,2,2-trichloroethyloxycarbonyl group, a 2-(trimethylsilyl)ethyloxycarbonyl group, a p-toluensulfonyl group, an o-nitrophenylsulfenyl group, a diphenylphosphonothioyl group, a triphenylmethyl group, a 2-benzoyl-1-methylvinyl group or a 4-phenylbutyryl group; R.sub.2 is a hydrogen atom or when taken together with R.sub.1, may form a phthaloyl group; R.sub.3 is an isobutyl group, a n-butyl group or an isopropyl group; R.sub.4 is a butyl group, a benzyl group or a methylthioethyl group; and R.sub.5 is a hydrogen atom or a chloromethyl group, which inhibits the activity of cysteine proteinases.Type: GrantFiled: June 29, 1989Date of Patent: January 14, 1992Assignee: Suntory LimitedInventors: Naoki Higuchi, Masayuki Saitoh, Norio Iwasawa, Motoo Sumida, Hiroshi Shibata
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Patent number: 5068365Abstract: Disclosed is novel hexahydrophthalic anilide derivatives and herbicide compositions comprising the derivatives. The hexahydrophthalic anilide derivatives of this invention are represented by the formula [I], [II] or [III]. ##STR1## (wherein R.sup.1 represents non-substituted or substituted phenyl, R.sup.2 represents hydrogen or C.sub.1 -C.sub.4 alkyl, R.sup.3 represents C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 alkenyl) ##STR2## (wherein R.sup.4 and R.sup.5, the same or different, represent C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkenyl or C.sub.1 -C.sub.4 alkynyl, provided R.sup.4 and R.sup.5 are not C.sub.1 -C.sub.4 alkyl simultaneously) ##STR3## (wherein X.sup.1 and X.sup.2, the same or different, represent halogen, Y represents oxygen or sulfur, R.sup.6 represents C.sub.1 -C.sub.6 straight or cyclic alkyl which may be substituted with oxygen, R.sup.7 represents hydrogen or methyl, R.sup.8 represents cyano, C.sub.1 -C.sub.3 alkyl, C.sub.2 or C.sub.3 alkenyl, C.sub.2 -C.sub.4 alkynyl, C.sub.3 -C.sub.Type: GrantFiled: December 30, 1988Date of Patent: November 26, 1991Assignees: Tosoh Corporation, Agro-Kanesho Co., Ltd.Inventors: Takumi Tokunaga, Hiroyuki Watanabe, Kenji Tsuzuki, Sinzo Someya, Seigo Koura, Mikio Ito
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Patent number: 5006523Abstract: Novel compounds of the formula ##STR1## and tautomers thereof are disclosed. These compounds possess potassium channel blocking activity and, as such, are useful as antiarrhythmic agents.Type: GrantFiled: October 26, 1989Date of Patent: April 9, 1991Assignee: E. R. Squibb & Sons, Inc.Inventor: Karnail Atwal
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Patent number: 5006542Abstract: Arylthioalkylphenylcarboxylic acids are provided which have the structure ##STR1## wherein Ar represents an aryl group including phenyl or naphthyl which may or may not include one or more substituents, X is COOR where R is hydrogen, alkali metal, or lower alkyl, or X is 5-tetrazolyl or ##STR2## where R.sup.1 is lower alkyl or aryl, p is 1 to 5, and m is 1 to 4. These compounds are cardiovascular agents which exhibit thromboxane antagonist activity and thus are useful in the treatment of thrombotic and vasopastic diseases.Type: GrantFiled: October 31, 1988Date of Patent: April 9, 1991Assignee: E. R. Squibb & Sons, Inc.Inventors: Steven E. Hall, Philip D. Stein
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Patent number: 4992583Abstract: The present invention relates to a process for synthesizing N-chlorothio-sulfonamides of the formula: ##STR1## comprising reacting a N,N'-dithiobis(sulfonamide) of the formula: ##STR2## with chlorine gas or sulfuryl chloride in the presence of a liquid solvent comprising a N-chlorothio-sulfonamide of formula I, wherein R.sup.1 and R.sup.2 are independently selected from the group consisting of alkyl radicals having from about 1 to about 20 carbon atoms, aralkyl radicals having 7 to 20 carbon atoms, cycloalkyl radicals having from about 5 to about 20 carbon atoms, phenyl radicals, alkaryl radicals having from about 7 to 20 carbon atoms, and haloaryl radicals having about 6 to about 10 carbon atoms and where R.sup.1 is also selected from radicals having the formula: ##STR3## wherein R.sup.3 and R.sup.4 are individually selected from said alkyl, aralkyl, cycloalkyl, phenyl, alkaryl and haloaryl radicals and wherein R.sup.3 and R.sup.4 can be joined together to represent radicals selected from --CH.sub.2).sub.Type: GrantFiled: January 6, 1989Date of Patent: February 12, 1991Assignee: The Goodyear Tire & Rubber CompanyInventors: Steven M. Ryba, Timothy Sabo
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Patent number: 4965279Abstract: Novel cyclopropyl aza prostaglandin analogs are disclosed having the formula ##STR1## wherein A can be carbonyl, sulfonyl or a single bond. These compounds are useful, for example, as thromboxane antagonists.Type: GrantFiled: November 18, 1988Date of Patent: October 23, 1990Assignee: E. R. Squibb & Sons, Inc.Inventors: Raj N. Misra, David M. Floyd, Steven E. Hall
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Patent number: 4920116Abstract: N-(aminoalkyl)-substituted(N or C alkyl)-aryl-4-(methylsylfonylamino)benzamides of the formula ##STR1## wherein R is C.sub.1 -C.sub.4 straight chain alkyl, one of R.sub.1, R.sub.2 and R.sub.3 is a phenyl or naphthyl group and the others are hydrogen, --NR.sub.4 R.sub.5 is a secondary or teritary amino group, X and X.sub.1 are hydrogen or alkyl and n is 0 or 1, are useful as antiarrhythmic agents in the treatment of cardiac arrhythmias especially as combination Class I/Class III agents.Type: GrantFiled: December 13, 1988Date of Patent: April 24, 1990Assignee: Schering A.G.Inventors: Thomas K. Morgan, Jr., Klaus Nickisch
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Patent number: 4900867Abstract: A process for producing N-fluorosulfonamides by reaction of a sulfonamide with fluorine in a solvent mixture of halogenated hydrocarbon an nitrile is described together with new N-fluorosulfonamides which are produced in accordance with this process.Type: GrantFiled: July 2, 1987Date of Patent: February 13, 1990Assignee: Kali-Chemie AktiengesellschaftInventors: Bernd Wilkes, Dieter Naumann, Werner Rudolph, Ruediger Sander
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Patent number: 4883914Abstract: There are provided novel benzenesulfonyl carboxamide compounds and novel intermediate benzenesulfonyl-2-imidazolin-5-one compounds, novel intermediates and methods for the preparation of said compounds, and a method for controlling a variety of annual and perennial plant species utilizing novel benzenesulfonyl carboxamide compounds and novel intermediate benzenesulfonyl 2-imidazolin-5-one compounds.Type: GrantFiled: July 7, 1988Date of Patent: November 28, 1989Assignee: American Cyanamid CompanyInventors: Sergio I. Alvarado, Alvin D. Crews, Jr., Peter J. Wepplo, Robert F. Doehner, Jr., Thomas E. Brady, David M. Gange, Desiree L. Little
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Patent number: 4874846Abstract: Process for the preparation of aryloxy-benzoic acids containing a sulphonamide group by the direct reaction of a phenoxy-benzoic acid with a sulphonamide, in the presence of a halogenating agent such as P(O)Cl.sub.3.Type: GrantFiled: May 26, 1987Date of Patent: October 17, 1989Assignee: Rhone-Poulenc Agrochimie S.A.Inventor: Alain Chene
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Patent number: 4792628Abstract: Indane derivatives and their salts represented by the general formula (1), ##STR1## wherein R.sup.1 is an amino group which may have lower alkyl groups as the substituents, a hydroxylimino group, an alkanoylamino group having 1 to 10 carbon atoms which may have halogen atoms as the substituents, a lower alkylsulfonylamino group, a phenylsulfonylamino group which may have lower alkyl groups as the substituents on the phenyl ring, a benzoylamino group having lower alkyl groups as the substituents on the phenyl ring, and a phenyl-lower alkylamino group having a hydroxyl groups or a lower alkyl groups as the substituents on the phenyl ring, R.sup.2 is a hydrogen atom, a lower alkyl group, a halogen atom, a nitro group, an amino group, an amino-lower alkyl group, a lower alkanoylamino group, a lower alkanoylamino-lower alkyl group which may have halogen atoms as the substituents, a lower alkylthio group, a 1-piperidinesulfonyl group, or a lower alkenyl group; R.sup.Type: GrantFiled: April 16, 1987Date of Patent: December 20, 1988Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Yasuo Oshiro, Hiraki Ueda, Kazuyuki Nakagawa
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Patent number: 4791102Abstract: The present invention is concerned with compounds with the formula: ##STR1## in which: R.sub.1 represents a lower alkyl, a lower hydroxy alkyl or a benzyl group, a phenyl group or a 4-hydroxy phenyl group:R.sub.2 and R.sub.Type: GrantFiled: January 23, 1987Date of Patent: December 13, 1988Assignee: SanofiInventors: Andre Bernat, Denis Delebassee, Daniel Frehel, Jean-Pierre Maffrand, Eric Vallee
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Patent number: 4737522Abstract: Fungicidally active novel N-sulphenylated benzene sulphonic acid amides of the formula ##STR1## in which R.sup.1, R.sup.2 and R.sup.3 independently of one another represent hydrogen, halogen, nitro, alkyl or halogenoalkyl andR.sup.4 represents alkyl, alkenyl, halogenoalkinyl, cycloalkyl which is optionally substituted by alkyl, alkoxyalkyl or alkylthioalkyl, excluding the compounds in which (a) R.sup.4 represents methyl and (i) R.sup.1, R.sup.2 and R.sup.3 represents hydrogen, or (ii) R.sup.1 represents chlorine or nitro, R.sup.2 represents chlorine and R.sup.3 represents hydrogen, or (iii) R.sup.1 represents nitro and R.sup.2 and R.sup.3 represent hydrogen, or (iv) R.sup.1 and R.sup.3 represent chlorine and R.sup.2 represents hdyrogen and (b) R.sup.4 represents n-butyl, R.sup.1 and R.sup.3 represent hydrogen and R.sup.2 represents chlorine.Type: GrantFiled: August 21, 1986Date of Patent: April 12, 1988Assignee: Bayer AktiengesellschaftInventors: Engelbert Kuhle, Hans-Georg Schmitt, Wilhelm Brandes, Paul Reinecke
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Patent number: 4734444Abstract: Mixtures which are curable by heating or irradiation with actinic light contain one or more cationically curable compounds, such as an epoxy, an olefinically unsaturated monomer, amino resin or phenolic resin, and as a cationically active curing catalyst one or more N-sulfonylamino-sulfonium salts of the formula ##STR1## such as N-p-toluenesulfonyl-N-methylaminodiphenylsulfonium hexafluorophosphate with or without quinones or peroxides are suitable, inter alia, for producing moldings, coatings, relief images and resist patterns.Type: GrantFiled: February 12, 1987Date of Patent: March 29, 1988Assignee: BASF AktiengesellschaftInventors: Andreas Henne, Wolfram Ochs, Helmut Tesch, Gunnar Schornick, Reinhold J. Leyrer
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Patent number: 4721770Abstract: N-Cyanocarboxylic acid amide derivatives which contain two or three ##STR1## groupings in the molecule are useful as hardeners for epoxide resins.Type: GrantFiled: June 24, 1986Date of Patent: January 26, 1988Assignee: Ciba-Geigy CorporationInventors: Friedrich Stockinger, Friedrich Lohse, Roland Moser
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Patent number: 4672139Abstract: Benzoylurea compounds of the formula ##STR1## wherein the meaning of each of the symbols is described in the specification.Type: GrantFiled: July 21, 1986Date of Patent: June 9, 1987Assignee: E. I. Du Pont de Nemours and CompanyInventor: Martin Anderson
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Patent number: 4652303Abstract: The invention concerns novel compounds of the formula I ##STR1## wherein: W are selected from the group consisting of:the groups R.sup.5 --CO-- and R.sup.5 --CS-- wherein: R.sup.5 is selected from alkenyl, alkynyl, benzyl, phenyl, substituted alkyl, substituted alkenyl, substituted alkynyl, substituted benzyl, substituted phenyl and the acetal, hemiacetal, oxime, imine and Schiff base derivatives of the group R.sup.5 --CO--;the groups Y--CO-- and Y--CS-- wherein Y is selected from hydroxy, mercapto, alkylthio and the groups MO-- and MS-- wherein M is an organic or an inorganic cation;the groups R.sup.6 R.sup.7 NCO-- and R.sup.6 R.sup.7 NCS-- wherein R.sup.6 and R.sup.7 are independently selected from hydrogen, alkyl, substituted alkyl, alkanoyl, carboxy, alkoxycarbonyl, alkylsulfonyl, benzoyl, benzenesulfonyl, substituted benzoyl, substituted benzenesulfonyl, or R.sup.6 and R.sup.Type: GrantFiled: July 2, 1984Date of Patent: March 24, 1987Assignee: ICI Australia LimitedInventors: Keith G. Watson, Graham J. Bird, Graeme J. Farquharson
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Patent number: 4629739Abstract: Novel substituted sulfonamidobenzamides are described as useful antiarrhythmic agents. Their use in the treatment of cardiac arrhythmias, especially re-entrant arrhythmias, via the prolongation of the action potential of cardiac tissue is provided. Pharmaceutical formulations containing such compounds are also disclosed.Type: GrantFiled: September 23, 1985Date of Patent: December 16, 1986Assignee: Schering A.G.Inventors: David D. Davey, William C. Lumma, Jr., Ronald A. Wohl
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Patent number: 4628110Abstract: Novel compounds of the following general formula: ##STR1##Type: GrantFiled: October 30, 1984Date of Patent: December 9, 1986Assignee: The Upjohn CompanyInventor: Paul A. Aristoff
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Patent number: 4618711Abstract: Compounds of the formula: ##STR1## in which Z is ##STR2## where R is hydrogen, alkyl, polyfluorinated alkyl, --CN, cyanoalkyl, cycloalkyl or cycloalkylalkyl;R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and R.sup.7, independently, are hydrogen, alkoxy, trifluoromethyl or halo;R.sup.8 is hydrogen or alkyl;or a pharmaceutically acceptable salt thereof, are useful as anti-arrhythmic agents.Type: GrantFiled: March 29, 1985Date of Patent: October 21, 1986Assignee: American Home Products CorporationInventor: George C. Buzby, Jr.
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Patent number: 4618712Abstract: N-Cyanocarboxlic acid amide derivatives which contain two or three ##STR1## groupings in the molecule are obtained by reacting 1 mol of a dicyanodiamine with 2 mols of a carboxylic acid anhydride or 1 mol of a dicyandiamine salt with 2 mols of a carboxylic acid halide or 1 mol of a dihalogeno compound with 2 mols of an N-cyanocarboxylic acid amide salt, or by reacting 1 mol of a carboxylic acid dichloride or trichloride with 2 or, respectively, 3 mols of a cyanamide or 1 mol of a carboxylic acid dicyandiamide or tricyantriamide salt with 2 or 3 mols of an alkylating agent.The N-cyanocarboxylic acid amide derivatives according to the invention are useful hardeners for epoxide resins.Type: GrantFiled: February 15, 1983Date of Patent: October 21, 1986Assignee: Ciba-Geigy CorporationInventors: Friedrich Stockinger, Friedrich Lohse, Roland Moser
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Patent number: 4603125Abstract: Compounds represented by the general formula (I): ##STR1## in which R.sub.1 represents ##STR2## A and B each represent H or a lower alkane optionally substituted with amino and/or hydroxyl functions, except that A and B are not both H; R.sub.3 represents H, OCH.sub.3, CH.sub.3, halogen, NH.sub.2, NO.sub.2, NHCH.sub.3, N.sub.3 (CH.sub.3).sub.2, N.sub.3, NHCOCH.sub.3, NHCOOCH.sub.3, N(CH.sub.3)COOCH.sub.3, CONH.sub.2 or CONHCH.sub.3 ; R.sub.4 represents H, alkyl, O-alkyl, CONH.sub.2, CONHCH.sub.3 or CONHCH.sub.2 CONHCH.sub.3, except that R.sub.3 and R.sub.4 taken together can represent --C.dbd.CH--CH.dbd.N--; R.sub.5 represents H, alkyl, O-alkyl, CONH.sub.2, CONHCH.sub.3 or CONH.sub.2 CH.sub.2 CONHCH.sub.3 ; R.sub.6 represents lower alkyl; R.sub.7 represents CH.sub.3 or C.sub.6 H.sub.5 (phenyl); R.sub.8 represents lower alkyl or C.sub.6 H.sub.5 (phenyl); R.sub.9 represents H, NHCOCH.sub.3, NH.sub.2 or N.dbd.CHN(CH.sub.3).sub.2 ; and R.sub.10 represents H or NH.sub.Type: GrantFiled: November 14, 1983Date of Patent: July 29, 1986Assignee: Development Finance Corporation of New ZealandInventors: Graham J. Atwell, Bruce C. Baguley, William A. Denny, Gordon W. Rewcastle
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Patent number: 4588823Abstract: Novel compounds of the following general formula: ##STR1##Type: GrantFiled: September 27, 1984Date of Patent: May 13, 1986Assignee: The Upjohn CompanyInventor: Paul A. Aristoff
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Patent number: 4565787Abstract: A method for the simultaneous detection, separation and analysis by reverse hase HPLC of sulfur mustard type compounds and their major hydrolysis and oxidation by-products utilizes a novel precolumn enhancement derivatization procedure. The method involves the reaction of these nonchromophoric sulfides with N-halogeno-N-metal arylsulfonamidates on a microscale to produce UV or visible absorbing or fluorescing arylsulfonylsulfilimine compounds. These arylsulfonylsulfilimine derivatives can then be readily separated on a low polarity C-18 column by reverse phase HPLC. The method permits quantitation of these sulfides by UV detector response in quantities as small as 20 nanograms.Type: GrantFiled: May 9, 1983Date of Patent: January 21, 1986Assignee: The United States of America as represented by the Secretary of the ArmyInventors: Paul C. Bossle, John J. Martin, Emory W. Sarver, Harold Z. Sommer
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Patent number: 4549901Abstract: As new compounds, 2-[4-(substituted aryloxy)phenoxy]-N-substituted phenylsulfonyl]propionamides having the formula ##STR1## wherein A is CH, or nitrogen, X is hydrogen or chlorine and Ar is phenyl or substituted phenyl.Type: GrantFiled: February 16, 1984Date of Patent: October 29, 1985Assignee: Stauffer Chemical CompanyInventor: Donald R. James
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Patent number: 4544654Abstract: Novel substituted sulfonamidobenzamides are described as useful antiarrhythmic agents. Their use in the treatment of cardiac arrhythmias, especially re-entrant arrhythmias, via the prolongation of the action potential of cardiac tissue is provided. Pharmaceutical formulations containing such compounds are also disclosed.Type: GrantFiled: March 20, 1984Date of Patent: October 1, 1985Assignee: Schering A.G.Inventors: David D. Davey, William C. Lumma, Jr., Ronald A. Wohl
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Patent number: 4537896Abstract: New thrombin inhibiting N.sup..alpha. -arylsulfonyl-p-guanidinophenylalanine amides of the formula ##STR1## wherein Ar is a substituted aryl and R.sub.1 and R.sub.2 are an alkyl group having 1-5 carbon atoms or together with the amine nitrogen form an heterocyclic ring, in racemate form as well as in form of optical active antipodes, theirs pharmaceutically acceptable salts, methods for their preparation, pharmaceutical composition and diagnostical preparation containing these compounds, use of the compounds in treatments of thrombosis and methods of treatment of thrombosis as well as methods for determination of thrombin concentration in blood.Type: GrantFiled: June 14, 1983Date of Patent: August 27, 1985Assignee: KabiVitrum ABInventors: Carl G. Claeson, Stig I. Gustavsson
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Patent number: 4533749Abstract: Novel compounds of the following general formula: ##STR1##Type: GrantFiled: February 16, 1982Date of Patent: August 6, 1985Assignee: The Upjohn CompanyInventors: Paul A. Aristoff, John C. Sih
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Patent number: 4525586Abstract: The present specification provides novel analogs of carbacyclin (CBA.sub.2), 6a-carba-prostacyclin (6a-carba-PGI.sub.2), which have pronounced prostacyclin-like pharmacological activity, e.g., as platelet anti-aggregatory agents. Specifically the novel chemical analogs of CBA.sub.2 are those substituted by fluoro (C-5), alkyl (C-9), interphenylene (C-5), methano (C-6a,9), and an additional (olefinic) valence bond (C-6a,9). Further provided are benzindene analogs of CBA.sub.2 and substituted forms thereof, i.e., 9-deoxy-2', 9-methano (or 2', 9-methano)-3-oxa-4,5,6-trinor-3,7-(1',3'-interphenylene)-PGF.sub.1 compounds. Also provided are a variety of novel chemical intermediates, e.g., substituted bicyclo[3.3.0]octane intermediates, and chemical process utilizing such intermediates which are useful in the preparation of the novel CBA.sub.2 analogs.Type: GrantFiled: September 19, 1983Date of Patent: June 25, 1985Assignee: The Upjohn CompanyInventor: Paul A. Aristoff
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Patent number: 4495365Abstract: Described herein are herbicidal compositions comprised of a thiocarbamate or haloacetanilide herbicide and an antidotally effective amount of an N-acylsulfonamide compound corresponding to the formula ##STR1## in which R is selected from the group consisting of hydrogen, methyl, chloro, acetamido, and 1-4 carbon alkoxyamido;R.sub.1 is selected from the group consisting of hydrogen, allyl, and metal ion;R.sub.2 is selected from the group consisting of 1-10 carbon alkyl, 1-4 carbon haloalkyl, 2-4 carbon alkenyl, 2-4 carbon haloalkenyl, acetonyl, 1-6 carbon alkoxy, 1-4 carbon alkoxycarbonyl, 1-4 carbon alkylthioalkyl, alkoxyalkyl, O,O-dialkylphosphorodithioylalkyl, phenyl, halophenyl, halophenylthioalkyl, cyclohexanedione, and dimethyl barbituric acid; orR.sub.1 and R.sub.2 together with the carbonyl group to which R.sub.2 is attached are selected from the group consisting of succinimide, substituted succinimide, phthalimide, and substituted phthalimide.Type: GrantFiled: April 29, 1982Date of Patent: January 22, 1985Assignee: Stauffer Chemical Co.Inventor: Ferenc M. Pallos
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Patent number: 4490555Abstract: Novel compounds of the following general formula: ##STR1##Type: GrantFiled: March 19, 1982Date of Patent: December 25, 1984Assignee: The Upjohn CompanyInventor: John C. Sih
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Patent number: 4487961Abstract: Novel compounds of the following general formula: ##STR1##Type: GrantFiled: February 16, 1982Date of Patent: December 11, 1984Assignee: The Upjohn CompanyInventor: Paul A. Aristoff
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Patent number: 4487960Abstract: Novel compounds of the following formula: ##STR1##Type: GrantFiled: April 19, 1982Date of Patent: December 11, 1984Assignee: The Upjohn CompanyInventor: Chiu-Hong Lin
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Patent number: 4479901Abstract: Process for fluorinating an organic carbanion, which process comprises contacting and reacting, in a dry inert atmosphere, the compound of the formula selected from ##STR1## wherein ##STR2## is the carbanion, M is a counter ion, and X is a halide and a selected N-flouro-N-alkylsulfonamide.Type: GrantFiled: August 15, 1983Date of Patent: October 30, 1984Assignee: E. I. Du Pont de Nemours and CompanyInventor: William E. Barnette
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Patent number: 4447634Abstract: There is provided herbicidal arylsulfonamide derivatives of phenoxybenzoic acids. These compounds are particularly useful when applied in a post-emergence application to soybean fields containing broadleaf weeds.Type: GrantFiled: April 30, 1981Date of Patent: May 8, 1984Assignee: Rhone-Poulenc AgrochimieInventor: Guang-Huei Lee
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Patent number: 4443477Abstract: The invention provides sulphonamides of the formula ##STR1## wherein R is a hydrogen atom or a lower alkyl radical;R.sub.1 is alkyl, aryl, aralkyl or aralkenyl, the aryl moiety of which in each case can be optionally substituted one or more times by hydroxyl, halogen, trifluoromethyl, lower alkyl or alkoxy or by acyl, carboxy or alkoxycarbonyl;n is 1, 2 or 3; andW is a valence bond or a divalent aliphatic hydrocarbon linkageand the physiologically acceptable salts, esters and amides of such compound. These compounds have excellent pharmacological lipid depressing activity and inhibit thrombocyte aggregation.Type: GrantFiled: July 7, 1982Date of Patent: April 17, 1984Assignee: Boehringer Mannheim GmbHInventors: Ernst-Christian Witte, Hans P. Wolfe, Karlheinz Stegmeier, Egon Roesch