Substituent Q Is Monocyclic Patents (Class 564/90)
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Patent number: 5552419Abstract: The invention relates to the compounds of formula I ##STR1## pharmaceutically acceptable prodrug derivatives and pharmaceutically acceptable salts thereof; methods for preparation thereof; pharmaceutical compositions comprising said compounds; and a method of inhibiting matrix-degrading metalloproteinase and of treating matrix-degrading metalloproteinase dependent conditions in mammals using such compounds.Type: GrantFiled: November 3, 1994Date of Patent: September 3, 1996Assignee: Ciba-Geigy CorporationInventors: Lawrence J. MacPherson, David T. Parker
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Patent number: 5534654Abstract: A novel hydroxamic acid compound of the formula: ##STR1## or a pharmaceutically acceptable salt thereof having cell growth inhibition, vascularization inhibition activities and the like.The compounds of the present invention possess inhibitory activities against the growth of vascular endothelial cells and the expression of lymphocyte adhesive factors and the detransforming activity of cells transformed by ras gene, and inhibit the cell growth and are effective on inflammation and tumor.Type: GrantFiled: August 3, 1993Date of Patent: July 9, 1996Assignee: Shionogi & Co., Ltd.Inventors: Mitsuaki Ohtani, Hitoshi Arita, Kenji Sugita, Takaharu Matsuura, Kazuhiro Shirahase
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Patent number: 5521219Abstract: Sulfonamide-containing hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: August 24, 1993Date of Patent: May 28, 1996Assignee: G. D. Searle & Co.Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel Getman, Gary A. DeCrescenzo, John N. Freskos
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Patent number: 5510388Abstract: Sulfonamide-containing hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: May 31, 1995Date of Patent: April 23, 1996Assignee: G. D. Searle & Co.Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel Getman, Gary A. DeCrescenzo, John N. Freskos
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Patent number: 5506242Abstract: The invention relates to a method of inhibiting metalloellastase activity, of inhibiting the degradation of elastin, or of treating macrophage metalloelastase dependent conditions in mammals which comprises administering to a mammal in need thereof an effective macrophage metalloelastase inhibiting amount of a compound of formula I ##STR1## wherein Ar, R, R.sub.1 and R.sub.2 have meanings as defined, or of a pharmaceutically acceptable prodrug derivative thereof, or of a pharmaceutically acceptable salt thereof, or of pharmaceutical compositions comprising a said compound.Type: GrantFiled: June 24, 1994Date of Patent: April 9, 1996Assignee: Ciba-Geigy CorporationInventors: Lawrence J. MacPherson, David T. Parker, Arco Y. Jeng
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Patent number: 5478941Abstract: Levorotatory and dextrorotatory enantiomers of 1-[(4-chlorophenyl)phenylmethyl]-4-[(4-methylphenyl)sulfonyl]piperazine of the formula ##STR1## their preparation and use for the preparation of substantially optically pure enantiomers of 1-[(4-chlorophenyl)phenylmethyl]piperazine, which are themselves valuable intermediate products for the preparation of optically active therapeutic compounds having a very high degree of optical purity.Type: GrantFiled: March 8, 1994Date of Patent: December 26, 1995Assignee: U C B, S.A.Inventors: Eric Cossement, Guy Bodson, Jean Gobert
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Patent number: 5466712Abstract: The compound of the formula (I) or a pharmaceutically acceptable salt thereof, are smooth muscle relaxants ##STR1##Type: GrantFiled: November 4, 1994Date of Patent: November 14, 1995Assignee: American Home Products CorporationInventors: John A. Butera, Schuyler A. Antane, Bradford H. Hirth
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Patent number: 5464867Abstract: The compound of the formula (I) or a pharmaceutically acceptable salt thereof, are smooth muscle relaxants.Type: GrantFiled: November 16, 1994Date of Patent: November 7, 1995Assignee: American Home Products CorporationInventors: Madelene M. Antane, John A. Butera, Bradford H. Hirth, Schuyler A. Antane
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Patent number: 5457131Abstract: The present invention relates to cyclopentane heptanoic or cyclopentane heptenoic acid, 2-hydrocarbyl sulfonamidomethyl, and derivatives thereof, useful as therapeutic agents. In particular, the therapeutic agents of this invention are useful as ocular hypotensives.Type: GrantFiled: August 18, 1994Date of Patent: October 10, 1995Assignee: Allergan, Inc.Inventor: Steven W. Andrews
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Patent number: 5455258Abstract: Particularly the invention relates to the compounds of formula I ##STR1## (a) wherein Ar is carbocyclic or heterocyclic aryl;R is hydrogen, lower alkyl, carbocyclic aryl-lower alkyl, carbocyclic aryl, heterocyclic aryl, biaryl, biaryl-lower alkyl, heterocyclic aryl-lower alkyl, mono- or poly-halo-lower alkyl, C.sub.3 -C.sub.7 -cycloalkyl, C.sub.3 -C.sub.7 -cycloalkyl-lower alkyl, hydroxy-lower alkyl, acyloxy-lower alkyl, lower alkoxy-lower alkyl, lower alkyl-(thio, sulfinyl or sulfonyl)-lower alkyl, amino, mono- or di-lower alkylamino)-lower alkyl, acylamino-lower alkyl, (N-lower alkyl-piperazino or N-aryl-lower alkylpiperazino)-lower alkyl, or (morpholino, thiomorpholino, piperidino, pyrrolidino, piperidyl or N-lower alkylpiperidyl)-lower alkyl;R.sub.1 is hydrogen, lower alkyl, carbocyclic aryl-lower alkyl, carbocyclic aryl, heterocyclic aryl, biaryl, biaryl-lower alkyl, heterocyclic aryl-lower alkyl, mono- or poly-halo-lower alkyl, C.sub.3 -C.sub.7 -cycloalkyl, C.sub.3 -C.sub.Type: GrantFiled: January 6, 1993Date of Patent: October 3, 1995Assignee: Ciba-Geigy CorporationInventors: Lawrence J. MacPherson, David T. Parker
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Patent number: 5451677Abstract: Substituted phenylsulfonamides are selective .beta..sub.3 adrenergic receptor agonists with very little .beta..sub.1 and .beta..sub.2 adrenergic receptor activity and as such the compounds are capable of increasing lipolysis and energy expenditure in cells. The compounds thus have potent activity in the treatment of Type II diabetes and obesity. The compounds can also be used to lower triglyceride levels and cholesterol levels or raise high density lipoprotein levels or to decrease gut motility. In addition, the compounds can be used to reduced neurogenic inflammation or as antidepressant agents. The compounds are prepared by coupling an aminoalkylphenyl-sulfonamide with an appropriately substituted alkyl epoxide. Compositions and methods for the use of the compounds in the treatment of diabetes and obesity and for lowering triglyceride levels and cholesterol levels or raising high density lipoprotein levels or for increasing gut motility are also disclosed.Type: GrantFiled: December 15, 1993Date of Patent: September 19, 1995Assignee: Merck & Co., Inc.Inventors: Michael H. Fisher, Robert J. Mathvink, Hyun O. Ok, Emma R. Parmee, Ann E. Weber
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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: 5407951Abstract: The present invention provides sulphonamides of the general formula: ##STR1## wherein R.sup.1 and R.sup.2, which can be the same or different, are hydrogen or halogen atoms or C.sub.1 -C.sub.6 -alkyl, trifluoro-methyl, cyano, carboxyl, alkoxycarbonyl, aminocarbonyl, N-alkylaminocarbonyl or N,N-dialkylaminocarbonyl radicals or, when R.sup.1 and R.sup.2 are alkyl radicals ortho to one another, R.sup.1 and R.sup.2 together with the carbon atoms to which they are attached, form a saturated or unsaturated C.sub.5-C.sub.7 -alkylene ring, R.sup.3 is a hydrogen atom, an alkyl radical containing up to 6 carbon atoms, an acyl radical, a phenylalkyl or phenylalkenyl radical, the phenyl moiety of which can be substituted by halogen, alkyl or trifluoromethyl, C is a --(CH.sub.2).sub.m --radical, in which m is 0, 1, 2 or 3, or a branched C.sub.2 -C.sub.5 -alkylene radical, whereby a methylene radical --CH.sub.Type: GrantFiled: June 30, 1992Date of Patent: April 18, 1995Assignee: Boehringer Mannheim GmbHInventors: Ernst-Christian Witte, Karlheinz Stegmeier, Liesel Doerge
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Patent number: 5403853Abstract: The compounds of the formula: ##STR1## wherein R.sub.1 and R.sub.2 are, independently, hydrogen, straight or branched chain alkyl or mono- or bi-cyclic alkyl;A is a substituted phenyl group containing one or two substituents selected from cyano, nitro, alkyl, perfluoroalkyl, alkoxy, perfluoroalkoxy, amino, alkylamino, dialkylamino, sulfamyl, alkylsulfonamido, arylsulfonamido, alkylcarboxamido, arylcarboxamido, alkylsulfone, perfluoroalkylsulfone, arylsulfone, chloro, bromo, fluoro, iodo, 1-imidazolyl or carboxyl; or a pharmaceutically acceptable salt thereof, are smooth muscle relaxants.Type: GrantFiled: June 13, 1994Date of Patent: April 4, 1995Assignee: American Home Products CorporationInventors: John A. Butera, Schuyler A. Antane
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Patent number: 5393790Abstract: A class of substituted spiro compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula III: ##STR1## wherein n is a number selected from 0, 1 and 2; wherein R.sup.3 is methylsulfonyl or sulfamyl; and wherein R.sup.8 is selected from hydrido, fluoro, chloro, bromo, iodo, methyl, ethyl, n-propyl, isopropyl, butyl, tert-butyl, isobutyl, methoxy, ethoxy, propoxy, butoxy, hydroxyl, mercapto, methylthio, ethylthio, cyano, fluoromethyl, difluoromethyl, trifluoromethyl, chloromethyl, dichloromethyl, trichloromethyl, pentafluoroethyl, heptafluoropropyl, difluorochloromethyl, dichlorofluoromethyl, difluoroethyl, difluoropropyl, dichloroethyl, dichloropropyl, trifluoromethoxy, hydroxymethyl, methoxymethyl and ethoxymethyl; or a pharmaceutically-acceptable salt thereof.Type: GrantFiled: February 10, 1994Date of Patent: February 28, 1995Assignee: G.D. Searle & Co.Inventors: David B. Reitz, Robert E. Manning, Horng-Chi Huang, Jinglin Li
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Patent number: 5387608Abstract: The present invention relates to cyclopentane heptanoic or cyclopentane heptenoic acid, 2-hydrocarbyl sulfonamidomethyl, and derivatives thereof, useful as therapeutic agents. In particular, the therapeutic agents of this invention are useful as ocular hypotensives.Type: GrantFiled: August 17, 1993Date of Patent: February 7, 1995Assignee: Allergan, Inc.Inventor: Steven W. Andrews
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Patent number: 5356893Abstract: The invention provides compounds of formula (I): ##STR1## or a physiologically acceptable salt or solvate thereof wherein R.sup.1 represents a halogen or hydrogen atom or a C.sub.1-6 alkyl or C.sub.1-6 alkoxy group;R.sup.2 represents a phenyl group optionally substituted by one or two substituents;R.sup.3 represents the group ##STR2## R.sup.4 and R.sup.5, which may be the same or different, each independently represent a hydrogen atom or a halogen atom, or a group selected from hydroxy, C.sub.1-6 alkoxy or C.sub.1-6 alkyl.The compounds may be used in the treatment or prophylaxis of depression and other CNS disorders.Type: GrantFiled: September 17, 1992Date of Patent: October 18, 1994Assignee: Glaxo Group LimitedInventors: John Bradshaw, John W. Clitherow, Ian B. Campbell
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Patent number: 5338883Abstract: 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 6, 1993Date of Patent: August 16, 1994Assignee: 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: 5318770Abstract: Methods and compositions are disclosed for enhancing .sup.19 F magnetic resonance imaging which utilize trifluorometyl derivatives of iodinated X-ray contrast media. Typical magnetic resonance contrast media within the scope of the present invention include bis(trifluoromethyl)benzene derivatives, tris(trifluoromethyl)benzene derivatives, tetrakis(trifluoromethyl)benzene derivatives, and other related trifluoromethylated benzene derivatives.Type: GrantFiled: October 25, 1991Date of Patent: June 7, 1994Assignee: Mallinckrodt Medical, Inc.Inventors: David H. White, Steven R. Woulfe, Youlin Lin, Mills T. Kneller
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Patent number: 5302724Abstract: This invention provides certain sulfonamide compounds, formulations and method of use of certain sulfonamide compounds in treating susceptible neoplasms.Type: GrantFiled: April 29, 1992Date of Patent: April 12, 1994Assignee: Eli Lilly and CompanyInventors: J. Jeffry Howbert, Fariborz Mohamadi, Michael M. Spees
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Patent number: 5260285Abstract: Novel substituted imidazopyridazines of formula (I) which are useful as angiotensin II antagonists, are disclosed.Type: GrantFiled: November 25, 1991Date of Patent: November 9, 1993Assignee: Merck & Co., Inc.Inventors: Eric E. Allen, William J. Greenlee, Prasun K. Chakravarty, Malcolm MacCoss, Arthur A. Patchett, Thomas F. Walsh
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Patent number: 5233074Abstract: The invention describes a process for selectively preparing ortho-fluorinated substituted aromatic compounds wherein an aromatic compound containing a substituent capable of directing ortho metalation is contacted with a metalating reagent under reaction conditions sufficient to form an ortho-metalated substituted aromatic compound. The ortho-metalated substituted aromatic compound is reacted with an electrophilic fluorinating reagent under reaction conditions sufficient to form the desired ortho-fluorinated substituted aromatic compound which is then recovered from the reaction mixture. The process which utilizes a metalation intermediate prior to effecting the electrophilic fluorination step overcomes problems associated with prior art electrophilic fluorination processes which do not proceed through a regiospecifically controlled intermediate.Type: GrantFiled: June 1, 1992Date of Patent: August 3, 1993Assignee: Air Products and Chemicals, Inc.Inventor: Gauri S. Lal
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Patent number: 5220062Abstract: There is disclosed a multi-step process for the preparation of benzenesulfonamides of general formula ##STR1## wherein R is 3,3-difluorobutyl or 3,3-difluorobuten-1-yl. The benzenesulfonamides obtainable by the process of the invention are intermediates for the synthesis of herbicidally active sulfonyl ureas.Type: GrantFiled: April 29, 1992Date of Patent: June 15, 1993Assignee: Ciba-Geigy CorporationInventors: Willy Meyer, Urs Siegrist
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Patent number: 5166430Abstract: A 2-(2-halogenoethylthio)-phenylsulfonamide of the formula I ##STR1## in which Z.sub.1 and Z.sub.2 independently of one another are hydrogen, fluorine or chlorine, is prepared by a process wherein:a) a 2-halogenophenylsulfonamide of the formula II ##STR2## in which X is fluorine, chlorine or bromine, is converted, in the presence of a base, together with a mercaptan of the formula IIIR-SH (III)in which R is C.sub.1 -C.sub.6 alkyl or C.sub.1 -C.sub.6 alkyl substituted by phenyl, into a 2-sulfenylphenylsulfonamide,b) this compound is oxidized to give the 2-sulfinylphenylsulfonamide,c) the resulting 2-sulfinylphenylsulfonamide is converted, in the presence of an acid, into the disulfide of the formula VI ##STR3## d) the disulfide of the formula VI is reduced to the 2-mercaptophenylsulfonamide,e) this compound is then converted, by means of a trialkylamine of the formula X(R.sub.1).sub.3 N (X)in which R.sub.1 is C.sub.1 -C.sub.Type: GrantFiled: September 20, 1990Date of Patent: November 24, 1992Assignee: Ciba-Geigy CorporationInventors: Henry Szczepanski, Willy Meyer, Franz Weibel
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Patent number: 5120865Abstract: A process suitable for industrially preparing 2,3-trans-1,4-bridged cyclohexane sulfonamide derivatives, especially useful as an intermediate for the synthesis of a trans bicyclo[2,2,1] heptane carboxylic acid derivative, a clinically important thromboxane A.sub.2 antagonist, comprising: allowing to react corresponding a cis/trans mixture of sulfonamide derivatives with an anionoid or water-soluble carbonyl reagent at pH3-7 so that the trans isomer may form a water-soluble adduct with the anionoid or carbonyl reagent, separating the resulting adduct dissolved in an aqueous layer, and recovering the trans isomer by treating the adduct with a base or an acid. Also provided is an alkali metal hydrogen sulfite adduct of 2,3-trans 1,4-bridged cyclohexane sulfonamide derivative.Type: GrantFiled: August 30, 1991Date of Patent: June 9, 1992Assignee: Shionogi & Co., Ltd.Inventors: Masayuki Narisada, Mitsuaki Ohtani, Fumihiko Watanabe, Kyozo Kawata
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Patent number: 5106407Abstract: The present invention discloses the antimicrobial utility of certain iodonium ylide compounds. The particular iodonium ylide compounds are phenyl iodonium ylides having an ortho substituent that stabilizes the positive charge on the polyvalent iodine by a nonbonded electrostatic interaction. The polyvalent iodine is further stabilized by a cyclic 1,3-dicarbonyl anion.Type: GrantFiled: December 4, 1989Date of Patent: April 21, 1992Assignee: The Dow Chemical CompanyInventors: Attila G. Relenyi, Gerald F. Koser, Richard W. Walter, Jr., William J. Kruper, Jr., Ravi B. Shankar, Anthony P. Zelinko
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Patent number: 5087749Abstract: 2-(2-haloethylthio)-phenylsulfonamides of formula I ##STR1## wherein R.sub.1 is hydrogen, C.sub.1 -C.sub.5 alkyl or C.sub.2 -C.sub.5 alkenyl and Z is hydrogen, fluorine or chlorine, are prepared by converting a phenylsulfonamide of formula II ##STR2## wherein Y is a tertiary alkyl group or a silyl group in succession and without isolating intermediates, witha) a strong base MeA, wherein Me is sodium or potassium, A is hydrogen, OH, NH.sub.2 or OR.sub.5 and R.sub.5 is C.sub.1 -C.sub.5 alkyl, into the compound of formula III ##STR3## converting that compound with b) one equivalent of n-butyllithium andc) sulfurinto the compound of formula IV ##STR4## reacting that compound with d) a 2-halofluoroethane of the formula X--CH.sub.2 CHF--Z wherein X is chlorine or bromine, to form a phenylsulfonamide of formula VI ##STR5## and then removing the group Y.Type: GrantFiled: December 3, 1990Date of Patent: February 11, 1992Assignee: Ciba-Geigy CorporationInventors: Bernard Wirz, Willy Meyer, Wolfgang Stutz
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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: 5068427Abstract: A process for the preparation of alkane- and arenesulfonamides in high purity and yield is provided. Ammonia or alkylamine is reacted under boiling conditions with an alkane- or arenesulfonyl halide in the absence of an added solvent. The heat of reaction is dissipated by the heat of vaporization of the ammonia or alkylamine.Type: GrantFiled: November 16, 1989Date of Patent: November 26, 1991Assignee: Atochem North America, Inc.Inventors: Stanley R. Sandler, Steven G. Schon, David M. Gardner
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Patent number: 5057623Abstract: An organic fluorine compound represented by the general formulaR.sub.f -(X).sub.h -R-Mwherein R.sub.f is a group selected from the following (a) and (b); ##STR1## X denotes a linking group selected from --O--, --S--, and --COO--, h denotes 0 or 1, R is a hydrocarbon chain comprising a phenylene group having an alkylene group with a total carbon number of 10 or more, or the derivative thereof, or an aliphatic alkylene group of a carbon number of 10 or more, and M is a group selected from --OH, --COOH, --SH, and --CONH.sub.2.The organic fluorine compound of the present invention greatly improves the dispersibility of magnetic powders in magnetic coating materials, has also an excellent rust prevention effect on metallic magnetic powders, and exhibits a marked dispersing effect even on fluorocarbon resin fine powders, which can be difficultly dispersed with conventional dispersing agents.Type: GrantFiled: October 13, 1989Date of Patent: October 15, 1991Assignee: Matsushita Electric Industrial Co., Ltd.Inventors: Yoshiaki Kai, Takashi Suzuki
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Patent number: 5053430Abstract: Novel compounds having the general formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are as defined herein. These compounds are useful in the treatment of schizophrenia.Type: GrantFiled: September 22, 1989Date of Patent: October 1, 1991Assignee: Boehringer Ingelheim KGInventors: Matthias Grauert, Herbert Merz, Joachim Mierau, Gunter Schingnitz, Claus Schneider
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Patent number: 5041603Abstract: The invention relates to N-phenylsulfonyl-N'-pyrimidinylureas and N-phenylsulfonyl-N-triazinylureas of the general formula ##STR1## wherein R.sub.1 is hydrogen, halogen, nitro, amino, C.sub.1 -C.sub.5 alkyl, C.sub.1 -C.sub.4 haloalkyl or a --Q--R.sub.7, --CO--OR.sub.8 or --(CO).sub.n --NR.sub.9 R.sub.10 radical,R.sub.2 is hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkylthio, C.sub.1 -C.sub.4 haloalkyl, C.sub.1 -C.sub.4 haloalkoxy, halogen or alkoxyalkyl containing not more than 4 carbon atoms,R.sub.3 is C.sub.2 -C.sub.10 alkenyl which is substituted by one or more fluorine or bromine atoms or by one or more hydroxyl, cyano, nitro, --(Y).sub.m --CO--(Z).sub.n --R.sub.8, --SO.sub.2 --NR.sub.11 R.sub.12, --S(O).sub.p --C.sub.1 -C.sub.3 haloalkyl or --S(O).sub.n --C.sub.1 -C.sub.3 alkyl groups and which may additionally be substituted by one or more chlorine atoms,R.sub.4 is C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 haloalkyl, C.sub.1 -C.sub.3 alkoxy or C.sub.1 -C.sub.Type: GrantFiled: January 12, 1990Date of Patent: August 20, 1991Assignee: Ciba-Geigy CorporationInventors: Willy Meyer, Dieter Reinehr, Konrad Oertle, Rolf Schurter
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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: 5002972Abstract: Pharmaceutical compounds and compositions for injectable use in the treatment of thromboxane A.sub.2 mediating diseases, comprising a pharmaceutical carrier and a pharmacologically effective amount of a compound of the formula: ##STR1## wherein R.sup.1 is carboxyl or 5-tetrazolyl; R.sup.2 is hydrogen, methyl, hydroxy, chloro, or bromo; or a pharmaceutically acceptable ester or salt thereof, together with one or more non-toxic pharmaceutically acceptable carriers; and methods for treating thromboxane A.sub.2 mediating diseases.Type: GrantFiled: February 7, 1990Date of Patent: March 26, 1991Assignee: Shionogi & Co., Ltd.Inventors: Masayuki Narisada, Mitsuaki Ohtani, Fumihiko Watanabe, Takaharu Matsuura
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Patent number: 4996360Abstract: The arylsulfonyl(alkyl)amides, notably N-(n-butyl)benzenesulfonamide, well adopted as heat-stable plasticizers for polyamides, e.g., nylon 11 and nylon 12, are directly prepared by (a) intimately contacting an arylsulfonyl halide with a stoichiometric excess of both an alkylamine and an alkaline agent, with the alkaline agent being present in aqueous solution, (b) eliminating water and excess alkylamine from the organic phase produced in stage (a), and (c) separating final product arylsulfonyl(alkyl)amide from the residual organic phase remaining after stage (b).Type: GrantFiled: March 15, 1989Date of Patent: February 26, 1991Assignee: AtochemInventors: Raymond Commandeur, Elie Ghenassia
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Patent number: 4990637Abstract: Herbicidally active novel substituted 1-benzylsulphonyl-3-heteroaryl(thio)-ureas of the formula ##STR1## in whichQ.sub.1 represents oxygen or sulphur,R.sup.1 represents hydrogen, or represents optionally substituted radicals from the series comprising alkyl, alkenyl, alkynyl and aralkyl,R.sup.2 represents hydrogen, halogen, hydroxyl, alkyl, halogenoalkyl, alkoxy, halogenoalkoxy, alkylthio, halogenoalkylthio, amino, alkylamino or dialkylamino,R.sup.3 represents hydrogen or alkyl,R.sup.4 represents halogenoalkyl,X represents nitrogen or a --CH grouping,Y represents nitrogen or a --CR.sup.5 grouping,R.sup.5 represents hydrogen, halogen, cyano, alkyl, formyl, alkyl-carbonyl or alkoxy-carbonyl,Z represents nitrogen or a --CR.sup.6 grouping, andR.sup.6 represents hydrogen, halogen, hydroxyl, alkyl, halogenoalkyl, alkoxy, halogenoalkoxy, alkylthio, alkylamino or dialkylamino,and salts thereof with metals and basic organic nitrogen compounds. The benzylsulphonyl moieties are also new.Type: GrantFiled: January 30, 1990Date of Patent: February 5, 1991Assignee: Bayer AktiengesellschaftInventors: Christa Fest, Klaus-Helmut Muller, Theodor Pfister, Hans-Jochem Riebel, Ernst Kysela, Hans-Joachim Santel, Robert R. Schmidt, Robert H. Strang
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Patent number: 4973733Abstract: Polymers, such as polyisobutylene or ethylene-propylene copolymers, are functionalized by reaction with an activated imine to yield novel polymers.Type: GrantFiled: February 9, 1987Date of Patent: November 27, 1990Assignee: Texaco Inc.Inventors: Phillip B. Valkovich, Kechia J. Chou
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Patent number: 4973732Abstract: Polymers, such as polysiobutylene or ethylene-propylene copolymers, are functionalized by reaction with an activated imine to yield novel polymers.Type: GrantFiled: February 9, 1987Date of Patent: November 27, 1990Assignee: Texaco Inc.Inventors: Phillip B. Valkovich, Kechia J. Chou
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Patent number: 4971990Abstract: Phenoxyethylamine derivatives represented by the general formula (I): ##STR1## wherein R.sub.1 and R.sub.5 represent lower-alkyl, R.sub.2 and R.sub.3, which may be the same or different, each represents hydrogen or lower-alkyl, or ##STR2## represents a 5- or 6-membered ring system which may include nitrogen, oxygen or sulfur as a ring membered atom, R.sub.4 represents hydrogen or lower-alkyl, and n represents an integer selected from 1 to 3, their optical isomers and pharmacologically-acceptable acid addition salts, which exhibit excellent .alpha..sub.1 -blocking activity, a process for their preparation, pharmaceutical compositions thereof, and a method for the treatment of a subject afflicted with hypertension or dysuria by administrating such a compound, are all disclosed.Type: GrantFiled: January 24, 1989Date of Patent: November 20, 1990Assignee: Hokuriku Pharmaceutical Co., Ltd.Inventors: Yasuo Itoh, Hideo Kato, Eiichi Koshinaka, Nobuo Ogawa, Kazuya Mitani, Shunichiro Sakurai
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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: 4908467Abstract: N-Phenylsulfonyl-B'-pyrimidinyl- and -triazinylureas of the formula I ##STR1## wherein A is 3,3,3-trifluoropropyl or 3,3-difluorobutyl,R.sup.1 is hydrogen, halogen, nitro, cyano, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -haloalkyl, C.sub.1 -C.sub.4 -alkoxy, C.sub.1 -C.sub.4 -alkylthio, C.sub.1 -C.sub.4 -alkylsulfinyl, C.sub.1 -C.sub.4 -alkylsulfonyl, --CO--R.sup.6, --NR.sup.7 R.sup.8, --CO--NR.sup.9 R.sup.10 or --SO.sub.2 --NR.sup.11 R.sup.12,R.sup.2 is hydrogen, halogen, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy, C.sub.1 -C.sub.4 -alkylthio, C.sub.1 -C.sub.4 -alkylsulfinyl or C.sub.1 -C.sub.4 -alkylsulfonyl,R.sup.3 and R.sup.4 independently of one another are each hydrogen, halogen C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -haloalkyl, C.sub.2 -C.sub.4 -haloalkoxy, C.sub.1 -C.sub.4 -alkylthio, C.sub.1 -C.sub.4 -haloalkylthio, C.sub.2 -C.sub.4 -alkoxyalkyl, C.sub.1 -C.sub.4 -alkoxy or --NR.sup.12 R.sup.13,R.sup.5 is hydrogen, C.sub.1 -C.sub.4 -alkyl or C.sub.1 -C.sub.4 -alkoxy,R.sup.6 is C.sub.1 -C.Type: GrantFiled: April 8, 1988Date of Patent: March 13, 1990Assignee: Ciba-Geigy CorporationInventors: Willy Meyer, Konrad Oertle
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Patent number: 4899249Abstract: A dielectric medium composition comprising a fluorine-containing amide or a fluorine-containing sulfonamide and capacitors or other electric devices incorporating said composition, are disclosed herein.Type: GrantFiled: April 21, 1988Date of Patent: February 6, 1990Assignee: Pennwalt CorporationInventors: James L. Reilly, Ludwig K. Huber, Gordon R. Leader
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Patent number: 4888043Abstract: The invention concerns compounds of the formula I ##STR1## wherein: Z is selected from hydrogen, alkyl, alkanoyl, sulfamoyl, carboxy and trifluoroacetamido;Y is selected from various carboxy or thiocarboxy groups, haloalkanoyl, alkylsulfonyl and haloalkylsulfonyl;R.sup.1 is selected from hydrogen, acyl and an inorganic or organic cation;R.sup.2 is selected from alkyl, substituted alkyl, alkenyl, haloalkenyl and alkynyl;R.sup.3 is selected from alkyl; andR.sup.4 is selected from hydrogen, alkyl, and alkoxycarbonyl.The compounds of the invention show herbicidal properties and plant growth regulating properties and in further embodiments and the invention provides processes for the preparation of compounds of formula I, intermediates useful in the preparation of the compounds of formula I, compositions containing as active ingredient a compound of formula I, and herbicidal and plant growth regulating processes utilizing compounds of formula I.Type: GrantFiled: June 20, 1986Date of Patent: December 19, 1989Assignee: ICI Australia LimitedInventors: Keith G. Watson, Craig G. Lovel
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Patent number: 4874894Abstract: Process comprises the combination of two steps of interacting a R-benzene, sulfuric acid and phosphorus oxychloride to obtain 4-R-benzenesulfonyl chloride and amidating said sulfonyl chloride to produce 4-R-benzenesulfonamide.Type: GrantFiled: April 29, 1987Date of Patent: October 17, 1989Assignee: Hilton Davis Co.Inventor: Ramamurthi Kannan
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Patent number: 4837307Abstract: A 2,2'-bridged[1,1'-biphenyl]-3-ylmethyl compound of the following formula is an intermediate to insecticidal esters. ##STR1## wherein n is 1-4 and Y is a leaving group readily displaced by carboxylate anions.Type: GrantFiled: January 16, 1984Date of Patent: June 6, 1989Assignee: FMC CorporationInventor: Ernest L. Plummer
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Patent number: 4835272Abstract: A process for formation of a base, which comprises reacting an acetylide compound with a salt. The acetylide compound has the following formula:(R--C.tbd.C--).sub.n Mwherein R is a monovalent group selected from the group consisting of an alkyl group, a cycloalkyl group, an alkenyl group, an alkynyl group, an aralkyl group, an aryl group and a heterocyclic group, each of which may have one or more substituent groups; M is an n-valent transition metal atom; and n is 1, 2 or 3. The salt is composed of an anion having an affinity for the transition metal (M) (the affinity of the anion for the transition metal is more than that of the acetylide anion (R--C.tbd.C.crclbar.)), and a cation derived from one selected from the group consisting of an alkali metal, an alkaline earth metal, ammonia and an organic base. A light-sensitive material containing the acetylide compound and the salt is also disclosed.Type: GrantFiled: July 16, 1987Date of Patent: May 30, 1989Assignee: Fuji Photo Film Co., Ltd.Inventors: Kozo Sato, Shunichi Ishikawa, Ken Kawata
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Patent number: 4826528Abstract: This invention relates to sulfonylureas of the formula ##STR1## These compounds are useful in killing weeds and in regulating the growth of cultivated plants.Type: GrantFiled: June 20, 1985Date of Patent: May 2, 1989Assignee: Celamerck GmbH & Co. KG.Inventors: Rudolf Mengel, W. Pfleiderer, Gerbert Linden, Gerhart Schneider
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Patent number: 4827032Abstract: Cycloalkanol[1,2-b]indole-sulphonamides of the formula ##STR1## where appropriate in an isomeric form, and their salts are disclosed. These compounds are useful to inhibit platelet aggregation and to antagonize thromboxane A.sub.2.Type: GrantFiled: June 29, 1988Date of Patent: May 2, 1989Assignee: Bayer AktiengesellschaftInventors: Horst Boshagen, Ulrich Rosentreter, Folker Lieb, Hermann Oediger, Friedel Seuter, Elisabeth Perzborn, Volker-Bernd Fiedler
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Patent number: 4749407Abstract: There are disclosed an N-propargyl-N-(2-trifluoromethylbenzoyl)-3-substituted benzenesulfonamide represented by the general formula: ##STR1## wherein R.sup.1 represents a halogen atom, a lower alkyl group, a lower alkoxy group, a perfluoro-lower alkyl group having 1 to 4 carbon atoms, a nitro group, a cyano group, a carboxyl group or a lower alkoxycarbonyl group; and R.sup.2 represents a hydrogen atom, a halogen atom, a lower alkyl group, a perfluoro-lower alkyl group having 1 to 4 carbon atoms, a lower alkoxy group, a nitro group, a cyano group, a carboxyl group or a lower alkoxycarbonyl group, and a selective herbicide containing the same as an active ingredient.Type: GrantFiled: June 23, 1986Date of Patent: June 7, 1988Assignees: Sagami Chemical Research Center, Central Glass Co, Ltd.Inventors: Daiei Tunemoto, Hideko Sakai, Kiyosi Kondo, Kaoru Mori, Masahiro Watanabe, Takeo Komata, Kenji Motojima
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Patent number: 4739116Abstract: A process improvement for the preparation of arylsulfonamides that avoids the multistep arylsulfonyl chloride refining operation presently used and, in one step, neutralizes and removes all the acidic by-products of chlorosulfonation simultaneously with arylsulfonamide formation which comprises the steps of (a) reacting an aryl hydrocarbon with chlorosulfonic acid to form a crude chlorosulfonation reaction product, (b) combining in an aqueous media said crude reaction product and a source of ammonia to form an amidation reaction mixture, (c) maintaining the temperature of the amidation reaction mixture at between about 40.degree. C. and 70.degree. C. and the pH at above about 7 with stirring for a period of time sufficient to form an amidation reaction product containing an arylsulfonamide, and optionally (d) separating the resulting arylsulfonamide from the amidation reaction product.Type: GrantFiled: January 16, 1986Date of Patent: April 19, 1988Assignee: Akzo America Inc.Inventors: Gail H. Birum, Richard F. Jansen