Nitrogen In Q Patents (Class 514/603)
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Patent number: 4751240Abstract: A phenol derivative of the formulaNU--A--X--R.sup.1wherein NU is a defined phenolic nucleus including a phenyl-hydroxynaphthyl; hydroxyphenyl-naphthyl; phenyl-hydroxyindanyl, phenyl-hydroxybenzothienyl or mono-hydroxyphenyl-ethylene or vinylene nucleus; wherein A is alkylene, alkenylene or alkynylene which may be interrupted by phenylene or other linkages, wherein R.sup.1 is hydrogen, or alkyl, alkenyl, alkynyl, cycloalkyl, halogenoalkyl, alkoxyalkyl, halogenoalkoxyalkyl, aryl or arylalkyl, or R.sup.1 is joined to R.sup.2, and wherein X is --CONR.sup.2 --, --CSNR.sup.2 --, --NR.sup.12 CO--, --NR.sup.12 CS--, --NR.sup.12 CONR.sup.2 --, ##STR1## --SO.sub.2 NR.sup.2 --or --CO--, or, when R.sup.1 is not hydrogen, is --NR.sup.12 COO--, --(PO)R.sup.2 13 , --S--, --SO--or --SO.sub.2 --, wherein R.sup.2 is hydrogen or alkyl, or R.sup.1 and R.sup.2 together form alkylene; wherein R.sup.12 is hydrogen or alkyl, and wherein R.sup.22 is hydrogen, cyano or nitro; or a salt thereof when appropriate.Type: GrantFiled: April 24, 1985Date of Patent: June 14, 1988Assignee: Imperial Chemical Industries PLCInventors: Jean Bowler, Graham C. Crawley, Philip N. Edwards, Alasdair T. Glen, Michael S. Large, Brian S. Tait
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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: 4703063Abstract: Novel sulfamoyl-substituted phenethylamine derivatives which exhibit .alpha.-adrenergic blocking action and are useful as an antihypertensive agent and an agent for the treatment of congestive heart failure.Type: GrantFiled: July 18, 1985Date of Patent: October 27, 1987Assignee: Yamanouchi Pharmaceutical Co., Ltd.Inventors: Kazuo Imai, Kunihiro Niigata, Takashi Fujikura, Shinichi Hashimoto, Toichi Takenaka
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Patent number: 4698333Abstract: Pesticidally active compounds of the formula ##STR1## in which R.sup.1 is an organic radical,R.sup.2 is hydrogen, trialkylsilyl, a hydrocarbon or acyl radical, andR.sup.3 and R.sup.4 independently are an amino, hydroxyl, hydroximino, alkoxy or like radical.Most of the compounds are new, as are various intermediates therefor.Type: GrantFiled: October 28, 1983Date of Patent: October 6, 1987Assignee: Bayer AktiengesellschaftInventors: Rudolf Fauss, Reinhard Lantzsch, Kurt Findeisen, Gerhard Jager, Ingeborg Hammann, Benedikt Becker, Bernhard Homeyer
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Patent number: 4661515Abstract: Novel compounds possessing both angiotensin enzyme inhibitory activity and diuretic activity are disclosed. The compounds are represented by the general formula ##STR1## in which X is ##STR2## in which R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 and R.sub.6 are hydrogen, alkyl, alkenyl, alkynyl, phenyl-alkyl, and cycloalkyl, and may be the same or different; n is an integer from 0 to 4 inclusive; M is alkenyl, alkynyl, cycloalkyl, cycloalkyl-alkyl, polycycloalkyl, polycycloalkyl-alkyl, aryl, aralkyl, heteroaryl, heteroaryl-alkyl, hetero-cyloalkyl, hetero-cycloalkyl-alkyl, fused aryl-cycloalkyl, fused aryl-cycloalkyl-alkyl, fused heteroaryl-cycloalkyl, fused heteroaryl-cycloalkyl-alkyl, alkoxyalkyl, alkylthioalkyl, alkylamino-alkyl, or dialkylaminoalkyl, or M and R.sub.6 taken together with the nitrogen to which M is bonded and the carbon to which R.sub.Type: GrantFiled: January 17, 1986Date of Patent: April 28, 1987Assignee: USV Pharmaceutical CorporationInventors: Edward S. Neiss, John T. Suh, John J. Piwinski
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Patent number: 4647588Abstract: 2-(Substituted sulfamyl) derivatives of 6-nitrobenzoic acid wherein at least one of the sulfamyl substituents is a basic substituent selected from amino-(lower alkyl), (lower alkyl)-amino-(lower alkyl), or di(lower alkyl)-amino-(lower alkyl) are disclosed to have activity in increasing the sensitivity of hypoxic tumor cells to therapeutic radiation. Also disclosed are methods of preparing such compounds and pharmaceutical compositions including such compounds.Type: GrantFiled: November 6, 1985Date of Patent: March 3, 1987Assignee: Merck & Co., Inc.Inventors: Edward L. Engelhardt, Walfred S. Saari
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Patent number: 4636515Abstract: A topical composition for eye treatment of glaucoma, comprising a small but pharmaceutically effective amount of a non-classical carbonic anhydrase inhibitor. The most preferred compound is methyl acetazolamide. The invention also relates to a method of topically treating glaucoma with eye drops of a non-classical carbonic anhydrase inhibitor to reduce intraocular pressure.Type: GrantFiled: June 25, 1984Date of Patent: January 13, 1987Assignee: University of Iowa Research FoundationInventors: Charles F. Barfknecht, Ronald D. Schoenwald
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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: 4629738Abstract: A topical composition for eye treatment of glaucoma, comprising a small but pharmaceutically effective amount of a non-classical carbonic anhydrase inhibitor. The most preferred compound is methyl acetazolamide. The invention also relates to a method of topically treating glaucoma with eye drops of a non-classical carbonic anhydrase inhibitor to reduce intraocular pressure.Type: GrantFiled: June 25, 1984Date of Patent: December 16, 1986Assignee: University of Iowa Research FoundationInventors: Charles F. Barfknecht, Ronald D. Schoenwald
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Patent number: 4628062Abstract: New compounds of the formula ##STR1## in which R.sub.1 is an allylamino, acetylamino or propionylamino radical,R.sub.2 is hydrogen or a 2-methoxyethoxy or ethoxy radical,R.sub.3 is hydrogen or a sulphamoyl radical, andR.sub.4 is hydrogen,and of the formula ##STR2## in which R.sub.1 is a halogen atom or a free or substituted hydroxyl, sulphhydryl or amino group,R.sub.2 is a hydrogen atom, an alkyl radical, a halogen atom, or a free or substituted hydroxyl, sulphhydryl or amino group,R.sub.3 and R.sub.4 each independently is hydrogen, alkyl, hydroxyl, alkoxy, sulphonamido or halogen, with the proviso that R.sub.2, R.sub.3 and R.sub.4 are hydrogen when R.sub.1 is hydroxyl,exhibit anti-inflammatory activity.Type: GrantFiled: December 17, 1984Date of Patent: December 9, 1986Assignee: Troponwerke GmbH & Co., KGInventors: Wolfgang Opitz, Bernhard Pelster, Romanis Fruchtmann, Udo Krupka, Walter Gauss, Hartmut Kiehne, Hermann Oediger
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Patent number: 4619944Abstract: Provided are antihypertensive compounds of the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, and R.sub.6 are hydrogen, alkyl, alkenyl, alkynyl, phenyl-alkyl, or cycloalkyl, and may be the same or different,m is an integer from 0 to 2 inclusive,n is an integer from 0 to 4 inclusive,M is alkenyl, alkynyl, cycloalkyl, cycloalkyl-alkyl, polycycloalkyl, polycycloalkyl-alkyl, aryl, aralkyl, heteroaryl, heteroaryl-alkyl, hetero-cycloalkyl, hetero-cycloalkyl-alkyl, fused aryl-cycloalkyl, fused aryl-cycloalkyl-alkyl, fused heteroaryl-cycloalkyl, fused heteroaryl-cycloalkyl-alkyl, alkoxyalkyl, alkylthioalkyl, alkylamino-alkyl, or dialkylaminoalkyl.Y is hydroxy, alkoxy, amino, or substituted amino, aminoalkanoyl, aryloxy, aminoalkoxy, or hydroxyalkoxy, andR.sub.7 is alkyl, aryl, aralkyl, cycloalkyl, cycloalkyl-alkyl, heterocyclic, --CO--SR, --CS--SR, ##STR2## CH.sub.2 CO.sub.2 R, --CHM--CO.sub.2 R, --CH.sub.2 --CO--SR, --CN, ##STR3## --CO--NH--CH.sub.2 CO.sub.2 R, ##STR4## or --CO--CO.sub.Type: GrantFiled: February 19, 1985Date of Patent: October 28, 1986Assignee: USV Pharmaceutical CorporationInventors: Raymond D. Youssefyeh, Howard Jones
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Patent number: 4587360Abstract: An anti-arrhythmic agent which is N-[3-[[2-(3,4-dimethoxyphenyl)ethyl]methylamino]propyl]-N-(1-methylethyl)- 2,3,4-trimethoxy-benzenesulfonamide or a pharmaceutically acceptable salt thereof.Type: GrantFiled: April 16, 1985Date of Patent: May 6, 1986Assignee: American Home Products CorporationInventor: George C. Buzby, Jr.
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Patent number: 4585796Abstract: The tertiary amines of the formula ##STR1## wherein n represents a whole number of 1 to 5;X.sup.1 represents phenyl or phenyl mono-, di- or tri-substituted by R.sup.1, R.sup.2 and R.sup.3 ;X.sup.2 represents hydrogen, lower-alkyl, phenyl or phenyl mono-, di- or tri-substituted by R.sup.1, R.sup.2 and R.sup.3 ;Y represents hydrogen, lower-alkyl, hydroxymethyl, carboxy or lower-alkoxycarbonyl;Z represents a group of the formula ##STR2## R.sup.1, R.sup.2 and R.sup.3 represent hydrogen, halogen, hydroxy, benzyloxy, lower-alkyl, lower-alkoxy, hydroxymethyl, amino, acylamino, lower-alkoxybenzylamino, nitro, carbamoyl, trifluoromethyl or lower-alkylsulphonylmethyl;R.sup.4, R.sup.5 and R.sup.51 represent hydrogen, lower-alkyl, lower-alkoxy, lower alkanoyl, carboxy, cyano, hydroxy, hydroxy-lower-alkyl, acyloxy or a group --C(R.sup.6).dbd.C(R.sup.7)COOR.sup.8, --SO.sub.2 R.sup.9, --C(O)R.sup.9 or --CH.sub.2 R.sup.10, with the proviso that R.sup.4 does not represent hydrogen when R.sup.Type: GrantFiled: August 1, 1983Date of Patent: April 29, 1986Assignee: Hoffmann-La Roche Inc.Inventors: Leo Alig, Marcel Muller
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Patent number: 4554282Abstract: New substituted 2,2-dimethyl-5-phenoxypentanoic acid benzamides which are useful as anti-arteriosclerotic agents are disclosed. These compounds elevate the high density lipoprotein fraction of cholesterol, and also lower the low density lipoprotein fraction of cholesterol.Type: GrantFiled: August 5, 1983Date of Patent: November 19, 1985Assignee: Warner-Lambert CompanyInventors: Ila Sircar, Ann Holmes
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Patent number: 4551478Abstract: Disclosed are novel 3-nitrobenzene sulfonanilide derivatives and, among others, that of the formula ##STR1## as well as fungicidal compositions containing such compounds as the active ingredient. The compounds of the invention are markedly effective in controlling plant diseases and, in particular, clubroot disease of Brassica spp., have no toxicity to men, beasts, and fishes, exert no phytotoxicity on crops, have neither irritant nor unpleasant odor, and manifest their excellent fungicidal effect at low concentrations. Accordingly, they are ideally useful in fungicidal compositions.Type: GrantFiled: December 30, 1982Date of Patent: November 5, 1985Assignee: Mitsui Toatsu Chemicals, Inc.Inventors: Tekeo Yoshimoto, Mitsumasa Umemoto, Keiichi Igarashi, Hideo Yamazaki, Yoshio Takasawa, Hirohisa Yanagita
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Patent number: 4545995Abstract: The novel unsaturated arylalkyl ammonium salts described herein are useful as antiarrhythmic agents. A method of treating arrhythmia by increasing the refractoriness of cardiac tissue is provided, as well as pharmaceutical formulations containing such ammonium salts.Type: GrantFiled: July 12, 1983Date of Patent: October 8, 1985Assignee: Schering A.G.Inventors: William C. Lumma, Jr., Ronald A. Wohl
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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: 4521619Abstract: Benzylidene derivatives of the formula: ##STR1## wherein n represents an integer from 1 through 4, R represents an amino radical, a monoalkylamino group containing 1 through 4 carbon atoms in the alkyl radical, a dialkylamino group containing 1 through 4 carbon atoms in each alkyl radical, or when n represents 2, 3 or 4 a group ##STR2## in which m represents 4 or 5, or a group --OM in which M represents an alkali metal or alkaline earth metal, and X.sub.1 X.sub.2, X.sub.3 and X.sub.4 each represent a hydrogen atom, a halogen atom, or an alkyl radical containing 1 through 6 carbon atoms, are new therapeutically useful compounds. They possess antidepressant, anticonvulsant, anxiolytic, analgesic, anti-inflammatory, ulcer-inhibiting, gastric antisecretory and antihypertensive properties.Type: GrantFiled: November 17, 1983Date of Patent: June 4, 1985Assignee: SynthelaboInventor: Jean-Pierre Kaplan
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Patent number: 4504492Abstract: Compounds of the general formula ##STR1## wherein Ph is a phenyl group which is optionally substituted by one or more substituents selected from halo (i.e. fluoro, chloro, bromo or iodo), C.sub.1-4 alkyl, amino, C.sub.1-4 alkylamino, di-C.sub.1-4 alkylamino, nitro, sulphonyl, aminosulphonyl, trihalomethyl, carboxy, C.sub.1-4 alkoxycarbonyl, amido, C.sub.1-4 alkylamido, C.sub.1-4 alkoxy, C.sub.2-4 alkenyl, cyano, aminomethyl, or methylsulphonyl; Y is a group of formula ##STR2## where R.sup.1 is hydrogen or methyl; R.sup.2 is alkyl of 1 to 3 carbon atoms or is methylthiomethyl; and Z is --OR.sup.3 or --NR.sup.4 R.sup.5 where R.sup.3, R.sup.4 and R.sup.5 are each hydrogen or alkyl of 1 to 4 carbon atoms and R.sup.3 can further be phenylalkyl having 1 to 3 carbon atoms in the alkylene moiety thereof, or phenyl; and basic salts thereof. These compounds have an advantageous enkephalinase inhibitory activity which renders the compounds useful in medical therapy, e.g.Type: GrantFiled: September 24, 1982Date of Patent: March 12, 1985Assignee: Burroughs Wellcome Co.Inventors: Samuel Wilkinson, George W. Hardy
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Patent number: 4499106Abstract: Lipolytic pharmaceutical composition containing 1-(4-hydroxy-3-dimethylamino-sulfonamidophenyl)-1-hydroxy-2-(1-phenoxy-iso propylamino)ethane or a pharmaceutically acceptable acid addition salt thereof as the active ingredient, and a method of combatting obesity therewith.Type: GrantFiled: May 20, 1983Date of Patent: February 12, 1985Assignee: Boehringer Ingelheim KGInventors: Werner Traunecker, Wilhelm Frolke, Heinrich Kreuzer, Hans P. Kollmer
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Patent number: 4497828Abstract: 3-nitro-4-methylbenzene sulfon-2-chloro-4-nitroanilide ##STR1## as a novel compound as well as fungicidal composition containing the compound as the active ingredient. The compound of the invention is markedly effective in controlling plant diseases and, in particular, clubroot disease of Brassica spp., has no toxicity to men, beasts, and fishes, exerts no phytotoxicity on crops, has neither irritant nor unpleasant odor, and manifests its excellent fungicidal effect at low concentrations. Accordingly, it is ideally useful in fungicidal composition.Type: GrantFiled: December 30, 1982Date of Patent: February 5, 1985Assignee: Mitsui Toatsu Chemicals, IncorporatedInventors: Takeo Yoshimoto, Keiichi Igarashi, Hideo Yamazaki, Yoshio Takasawa, Hirohisa Yanagita