Carbocyclic Ring Bonded Directly To The Nitrogen Patents (Class 544/165)
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Patent number: 4375543Abstract: The present invention relates to the novel compound N-[3-(1'-3"-Oxapentamethyleneamino-ethylideneamino)-2,4,6-triiodobenzoyl]- .beta.-amino-.alpha.methylpropionitrile which due to the sparing solubility in water, can be purified readily in a simple manner and can be used for the preparation of the known active compound for agents for peroral rapid cholecystography N-[3-(1'-3"-oxapentamethyleneamino-ethylideneamino)-2,4,6-triiodobenzoyl]- .beta.-amino-.alpha.-methyl propionic acid.Type: GrantFiled: July 29, 1981Date of Patent: March 1, 1983Assignee: Chemie Linz AktiengesellschaftInventors: Josef Wieser, Josef Krieger
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Patent number: 4372583Abstract: A pressure-sensitive chromogenic copy system utilizing a color developer capable of reacting with a chromogen to form a color image, said color developer comprising an oligomeric aromatic carboxylic acid and the method of making such oligomer by reaction of the acid with an aldehyde under alkaline conditions.Type: GrantFiled: August 17, 1981Date of Patent: February 8, 1983Inventor: Anthony E. Vassiliades
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Patent number: 4367339Abstract: There are provided di- tri- and tetrasubstituted N-nitroaniline compounds and inorganic and organic salts thereof which are effective for increasing axillary branching, improving canopy and enhancing flowering of herbaceous ornamental plants and graminaceous crops, leguminous crops, cotton and sunflowers. The salts are also effective as yield enhancing agents and lodging inhibitors for the crops.Type: GrantFiled: August 18, 1980Date of Patent: January 4, 1983Assignee: American Cyanamid CompanyInventors: Thomas D. O'Neal, Prithvi R. Bhalla, Barrington Cross
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Patent number: 4362546Abstract: Tetrahydrophthalamide derivatives of the general formula: ##STR1## wherein X.sub.1 is hydrogen or halogen; X.sub.2 is halogen, alkoxy or substituted benzyloxy; X.sub.3 is hydrogen, alkoxy or alkenyloxy; R and R' are the same or different alkyl, cycloalkyl, alkenyl or phenyl, each of which may be optionally substituted, or may jointly, together with nitrogen atom adjacent to R and R', form aliphatic heterocyclic ring containing one or two nitrogens or nitrogen and oxygen, which have a herbicidal activity against a broad spectrum of monocotyledonous and dicotyledonous weeds.Type: GrantFiled: May 27, 1980Date of Patent: December 7, 1982Assignee: Takeda Chemical Industries, Ltd.Inventor: Hiroshi Nagase
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Patent number: 4361516Abstract: New dyestuffs are described for keratinic fibers which produce particularly luminous shades without the need for an oxidizing agent. These dyestuffs have the formula: ##STR1## or a tautomeric form thereof wherein each of R.sub.1 and R.sub.4, which may be identical or different, represents a member selected from hydrogen, halogen, alkyl having 1 to 6 carbon atoms, alkoxy having 1 to 6 carbon atoms, acylamino and ureido;each of R.sub.2 and R.sub.3, which may be identical or different, represents a member selected from hydrogen, halogen, alkyl having 1 to 6 carbon atoms, alkoxy having 1 to 6 carbon atoms, amino, N-alkylamino, N-(hydroxyalkyl)-amino, N-(carbamyl-alkyl)-amino, acylamino and ureido, each of said alkyls containing 1 to 6 carbon atoms;each of R.sub.5 and R.sub.6, which may be identical or different, represents a member selected from hydrogen, halogen, alkyl containing 1 to 6 carbon atoms and alkoxy containing 1 to 6 carbon atoms, with the proviso that when R.sub.5 and R.sub.Type: GrantFiled: October 6, 1976Date of Patent: November 30, 1982Assignee: Societe Anonyme dite: L'OrealInventors: Gregoire Kalopissis, Andree Bugaut, Francoise Estradier
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Patent number: 4350518Abstract: Substituted alkylammonium salts of the formula ##STR1## where Ar denotes substituted phenyl, X denotes oxygen or sulfur, n denotes one of the integers 0, 1 and 2, B denotes bicyclic quinuclidine, bicyclic pyrrolizidine or substituted ammonium, and Z denotes the anion of a nonphytotoxic acid, the manufacture of these compounds, and their use as plant growth regulators.Type: GrantFiled: February 23, 1981Date of Patent: September 21, 1982Assignee: BASF AktiengesellschaftInventors: Hubert Sauter, Bernd Zeeh, Ernst Buschmann, Johann Jung
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Patent number: 4343939Abstract: Glyolic acid esters and amides of bis(p-disubstitutedaminophenyl)carbinols are disclosed as color formers for use in transfer sets.Type: GrantFiled: April 22, 1981Date of Patent: August 10, 1982Assignee: American Cyanamid CompanyInventors: Frank F. Cesark, Robert J. Manfre, Daniel W. Thomas
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Patent number: 4342756Abstract: Compounds are described of the formula ##STR1## (and their salts and solvates) in which: X is cis or trans --CH.dbd.CH--;R.sup.1 is C.sub.1-7 alkyl terminated by --COOR.sup.3 where R.sup.3 is H, C.sub.1-6 alkyl or C.sub.7-10 aralkyl;Y is a saturated heterocyclic amino group having 5-8 ring members; andR.sup.2 is C.sub.2-4 alkanoyl, C.sub.3-6 alkenyl (optionally substituted), C.sub.1-12 alkyl, or substituted or unsubstituted phenylalkyl, biphenylalkyl or naphthylalkyl.These compounds inhibit blood platelet aggregation and bronchoconstriction and may be formulated for use as antithrombotic and anti-asthmatic agents.Type: GrantFiled: April 29, 1981Date of Patent: August 3, 1982Assignee: Glaxo Group LimitedInventors: Eric W. Collington, Peter Hallett, Christopher J. Wallis, John Bradshaw, Norman F. Hayes
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Patent number: 4340540Abstract: To prepare basic dyestuffs of the general formula ##STR1## in which A and B independently of one another represent a hetero-aromatic radical or a radical of the general formula ##STR2## compounds of the general formulaA--CH.sub.2 --BA and B have the abovementioned meaning,are oxidized with oxygen in the presence of a nucleophilic compound of the general formulaD--Hand in the presence of catalytic amounts of benzoquinones substituted by halogen or cyano or of phenanthrenequinones substituted by nitro, and in the presence of catalytic amounts of nitrogen oxides--with the exception of dinitrogen monoxide--or of substances which produce such nitrogen oxides under the reaction conditions.Type: GrantFiled: June 26, 1980Date of Patent: July 20, 1982Assignee: Bayer AktiengesellschaftInventor: Karl H. Hermann
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Patent number: 4333929Abstract: A compound of formula (II) or a pharmaceutically acceptable acid addition salt thereof ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are the same or different and each represents C.sub.1-6 alkyl; R.sup.5 represents hydrogen or C.sub.1-6 alkyl; R.sup.6 represents C.sub.1-6 alkyl, phenyl optionally substituted with up to 3 groups selected from halogen, C.sub.1-6 alkyl, and C.sub.1-6 alkoxy; or benzyl optionally substituted with up to 3 groups selected from halogen, C.sub.1-6 alkyl and C.sub.1-6 alkoxy; or R.sup.5 and R.sup.6 together represent the remaining members of a 5- or 6-membered ring optionally containing an oxygen, sulphur or additional nitrogen atom and being optionally substituted with C.sub.1-6 alkyl, carboxy or C.sub.1-6 alkoxycarbonyl; and R.sup.7 represents C.sub.1-6 alkyl, phenyl optionally substituted with up to 3 groups selected from halogen, C.sub.1-6 alkyl and C.sub.1-6 alkoxy; or benzyl optionally substituted with up to 3 groups selected from halogen, C.sub.1-6 alkyl and C.sub.Type: GrantFiled: January 19, 1981Date of Patent: June 8, 1982Assignee: Beecham Group LimitedInventor: Barrie C. C. Cantello
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Patent number: 4330542Abstract: The invention relates to novel aniline derivatives of the formula: ##STR1## wherein R.sub.1 and R.sub.2 represent a hydrogen or chlorine atom, an allyloxy, acetamide or carboxamide group, R.sub.3 represents a methyl or an optionally substituted phenyl group, R.sub.4 represents a hydrogen atom and R.sub.5 an isopropyl, terbutyl, 2-phenoxy-ethyl or 3-phenyl-propyl group or R.sub.3 and R.sub.5 taken together form with the nitrogen atom a substituted heterocyclic group.The compounds of the invention are useful for the treatment of angina pectoris.Type: GrantFiled: May 16, 1980Date of Patent: May 18, 1982Assignee: SanofiInventors: Marcel Descamps, Charles Goldenberg
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Patent number: 4330476Abstract: To synthesize triarylmethane dyestuffs of the general formula ##STR1## in which R.sup.1 and R.sup.2 represent optionally substituted alkyl, aryl or aralkyl orR.sup.1 and R.sup.2, together or with the ortho-position of the phenyl ring, form a heterocyclic ring and R.sup.1 can additionally represent hydrogen,R.sup.3 and R.sup.4 denote hydrogen or non-ionic substituents,n represents an integer from 1 to 4 andX.sup.- denotes an anion,by a one-pot process, an aldehyde of the general formula ##STR2## in which R.sup.4 and n have the abovementioned meaning,is subjected to a condensation reaction with an aromatic amine of the general formula ##STR3## in which R.sup.1, R.sup.2, R.sup.Type: GrantFiled: June 26, 1980Date of Patent: May 18, 1982Assignee: Bayer AktiengesellschaftInventor: Karl H. Hermann
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Patent number: 4310533Abstract: The guanidinobenzoic acid derivatives of the general formula: ##STR1## wherein Z represents a carbon-carbon covalent bond, or a methylene, ethylene or vinylene group, R.sup.1 represents a hydrogen atom, or a straight- or branched-chain alkyl group containing from 1 to 4 carbon atoms, R.sup.2 represents a straight- or branched-chain alkyl group containing from 4 to 10 carbon atoms, or a cycloalkyl or cycloalkenyl or straight- or branched-chain alkenyl group containing from 3 to 8 carbon atoms, or a phenyl or benzyl group, or NR.sup.1 R.sup.2 represents a 4- to 8-membered heterocyclic ring, and acid addition salts thereof, have anti-plasmin and anti-trypsin activities.Type: GrantFiled: August 29, 1980Date of Patent: January 12, 1982Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Yoshiaki Uegai, Tsuyoshi Watanabe, Masashi Shiota, Itsuo Okumoto, Naohiro Kayama
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Patent number: 4308383Abstract: The present invention relates to the novel compound N-[3-(1'-3"-Oxapentamethyleneamino-ethylideneamino)-2,4,6-triiodobenzoyl]- .beta.-amino-.alpha.-methylpropionitrile which due to the sparing solubility in water, can be purified readily in a simple manner and can be used for the preparation of the known active compound for agents for peroral rapid cholecystography N-[3-(1'-3"-oxapentamethyleneamino-ethylideneamino)-2,4,6-triiodobenzoyl]- .beta.-amino-.alpha.-methyl propionic acid.Type: GrantFiled: December 22, 1980Date of Patent: December 29, 1981Assignee: Chemie Linz AktiengesellschaftInventors: Josef Wieser, Josef Krieger
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Patent number: 4305940Abstract: Benzamides of formula I ##STR1## are described, in which R=CH.sub.3, Cl or COOCH.sub.3 ; R' is a member selected from the group of dialkylamine, pyrrolidine, piperidine, and morpholine radicals. CH.sub.2 R' is in position ortho, meta, or para with respect to the carbonyl group; and their salts thereof with pharmaceutically acceptable acids are described. The novel compounds exhibit local anaesthetic and antiarrhythmic activity.Type: GrantFiled: November 18, 1980Date of Patent: December 15, 1981Assignee: B.B.R. Boehringer Biochemia Robin S.p.A.Inventor: Giuseppe Quadro
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Patent number: 4285942Abstract: The invention relates to novel cyclododecane derivatives of the general formula ##STR1## wherein R.sup.1 and R.sup.2 represent independently from each other a hydrogen atom, a C.sub.1-6 alkyl group or a C.sub.3-8 cycloalkyl group, or R.sup.1 and R.sup.2 form together with the nitrogen atom to which they are attached a heterocyclic ring containing 4 to 7 carbon atoms and optionally a further heteroatom selected from the group consisting of oxygen, sulphur and nitrogen, said ring may be optionally substituted by a C.sub.1-3 alkyl or benzyl group; and A represents a C.sub.2-6 straight or branched alkylene chain, and optically active isomers, acid addition salts and quaternary ammonium derivatives thereof. The invention relates further to an analogous process for the preparation of said compounds, to pharmaceutical compositions containing said compounds as the active ingredient and to a process for the preparation of said pharmaceutical compositions.Type: GrantFiled: December 3, 1979Date of Patent: August 25, 1981Assignee: Egyt Gyogyszervegyeszeti GyarInventors: Zoltan Budai, Aranka Lay nee Konya, Tibor Mezei, Katalin Grasser, Lujza Petocz, Eniko Kiszelly, Ibolya Kosoczky
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Patent number: 4283532Abstract: Disclosed is a process for the preparation of o-(2,6-dichloroanilino)phenylacetic acid (Diclofenac) or its pharmacologically acceptable acid addition salt, which comprises hydrolyzing an N,N-disubstituted-o-(2,6-dichloroanilino)phenylacetamide derivative with an alkali. Also a novel intermediate for use in the preparation of Diclofenac, that is, an N,N-disubstituted-o-halogenophenylacetamide in which the halogen is iodine or bromine, is disclosed.Type: GrantFiled: August 7, 1979Date of Patent: August 11, 1981Assignee: Ikeda Mohando Co., Ltd.Inventor: Fujio Nohara
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Patent number: 4282206Abstract: Reaction of 4-nitrophenacyl bromide with morpholine affords the novel intermediate 1-(4-nitrophenyl)-2-morpholinylethanone which when reduced yields the novel sunscreen 1-(4-aminophenyl)-2-morpholinylethanone.Type: GrantFiled: November 15, 1979Date of Patent: August 4, 1981Assignee: Westwood Pharmaceuticals Inc.Inventors: Paul L. Warner, Jr., F. Christopher Zusi
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Patent number: 4271160Abstract: Substituted morpholine derivatives, such as, for instance the compound 2-[.alpha.-(3,4-methylendioxy-phenoxy)-benzyl]-morpholine are disclosed.The claimed compounds are active on the central nervous system, and may be used as antidepressant agents.Type: GrantFiled: June 20, 1980Date of Patent: June 2, 1981Assignee: Farmitalia Carlo Erba S.p.A.Inventors: Piero Melloni, Arturo Della Torre, Giovanni C. Carniel, Alessandro Rossi
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Patent number: 4269837Abstract: Novel guanylamidines and the pharmaceutically acceptable acid addition salts thereof having activity as hypoglycemic agents are disclosed.Type: GrantFiled: February 19, 1980Date of Patent: May 26, 1981Assignee: Pfizer Inc.Inventors: David S. Watt, Jeffrey L. Ives
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Patent number: 4260749Abstract: 2,5-diamino-1,4-benzoquinones are used in the production of hair dye compositions and can be prepared by condensing a corresponding 3-amino-4-methoxy phenol derivative on one of a corresponding hydroxy aniline or phenylenediamine derivative, a corresponding benzoquinone imine derivative or a corresponding nitroso derivative.Type: GrantFiled: May 9, 1980Date of Patent: April 7, 1981Assignee: L'OrealInventors: Andree Bugaut, Monique Laudon
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Patent number: 4252804Abstract: Compounds of the formula I ##STR1## wherein m and n are 0, 1 or 2, X represents oxygen, imino, benzylimino, or morpholinoethylimino, Y represents CO, CONH, COO or SO.sub.2, and NR.sub.1 R.sub.2 represents a dimethylamino, diethylamino, dipropylamino, dibutylamino, allylamino, isobutenylamino, cyclopentylamino, cyclohexylamino, cycloheptylamino, cyclooctylamino, N-methyl N-cyclopentylamino, N-methyl N-cyclohexylamino, N-allyl N-cyclohexylamino, adamantylamino, diethoxyethylamino, dimethylaminoethylamino, dimethylaminopropylamino, N-methyl N-dimethylaminopropyl-amino, benzylamino, 3,4,5-trimethoxybenzylamino, phenethylamino, p-chlorophenethylamino, tetrahydrofurfurylamino, tetrahydropyranylmethylamino, pyrrolidino, isoxazolidinyl, piperidino, 4-hydroxypiperidino, 4-m-chlorophenyl-4-hydroxypiperidino, homopiperidino, 1,2,3,6-tetrahydropyridyl, morpholino, 2-methylmorpholino, 2,6-dimethylmorpholino, 2-morpholinoethylamino, thiamorpholino, piperazino, 4-methylpiperazino, 4-(.alpha.Type: GrantFiled: January 13, 1978Date of Patent: February 24, 1981Assignee: Metabio-JoullieInventors: Maurice Joullie, Gabriel Maillard, Lucien Lakah, Christian J. M. Warolin
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Patent number: 4252801Abstract: Morpholinyl acetamide derivatives are provided having the structure ##STR1## wherein R is hydrogen, lower alkyl, lower alkenyl or lower alkanoyl, R.sup.1 and R.sup.2 may be the same or different and are lower alkyl, lower alkenyl, phenyl-lower alkyl or lower alkoxy, or ##STR2## may be taken together to form a 5- to 7-membered heterocyclic ring optionally containing one other hetero atom, such as nitrogen, sulfur or oxygen; Y is hydroxyl, OR wherein R is as defined above, or ##STR3## wherein R.sup.1 and R.sup.2 and R.sup.1 and R.sup.2 taken together with the nitrogen to which they are attached are as defined above, and n is 1 to 6.These compounds are useful as anti-arrhythmia agents and have been found to be effective in the treatment of acute myocardial infarction.Type: GrantFiled: January 4, 1980Date of Patent: February 24, 1981Assignee: E. R. Squibb & Sons, Inc.Inventors: Frederic P. Hauck, Glenn A. Jacobs
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Patent number: 4246260Abstract: The invention relates to new substituted o-phenylenediamine derivatives of the general formula ##STR1## in which R represents optionally substituted alkyl, optionally substituted alkenyl or optionally substituted alkinyl,X represents O, S, SO or SO.sub.2 andR.sup.1 and R.sup.2 are different from one another and individually represent ##STR2## in which R.sup.3 and R.sup.4 are identical or different and represent alkyl andR.sup.5 represents hydrogen, optionally substituted alkyl or optionally substituted alkoxy, and salts thereof.Also included in the invention are (1) methods for preparing the above-described compounds, (2) compositions containing the above-described compounds and (3) methods for the treatment of helminthiasis.Type: GrantFiled: March 19, 1979Date of Patent: January 20, 1981Assignee: Bayer AktiengesellschaftInventors: Heinrich Kolling, Ekkehard Niemers, Hartmund Wollweber, Herbert Thomas
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Patent number: 4243804Abstract: Compounds having the formula ##STR1## or a pharmaceutically acceptable salt thereof, wherein R.sub.1 is alkyl, cycloalkyl or aryl; R.sub.2 is acyl or sulfonyl; R.sub.3 is alkylamino, dialkylamino or a nitrogen containing heterocyclic group; R.sub.4 is alkoxy; A.sub.1 is a saturated bond or an alkylene group having 1 to 4 carbon atoms; and A.sub.2 is an alkylene group having 2 to 5 carbon atoms; have antiinflammatory activity.Type: GrantFiled: April 30, 1979Date of Patent: January 6, 1981Assignee: E. R. Squibb & Sons, Inc.Inventor: John Krapcho
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Patent number: 4229449Abstract: Substituted morpholine derivatives, such as, for instance, the compound 2-[.alpha.-(2-methoxy-phenoxy)-benzyl]-morpholine are disclosed.The claimed compounds are active on the central nervous system, and may be used as antidepressant agents.Type: GrantFiled: January 8, 1979Date of Patent: October 21, 1980Assignee: Farmitalia Carlo Erba, S.p.A.Inventors: Piero Melloni, Arturo D. Torre, Giovanni C. Carniel, Alessandro Rossi
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Patent number: 4216214Abstract: Novel derivatives of formula (I) and the pharmaceutically acceptable salts thereof. ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and each is a lower alkyl group, or R.sup.1 and R.sup.2 together with the nitrogen atom to which they are attached, form a saturated heterocyclic group optionally containing, in addition to the said nitrogen atom, a second hetero atom, a process for the preparation thereof, and their use as anti-histamine anti "H.sub.2 " agents.Type: GrantFiled: December 27, 1977Date of Patent: August 5, 1980Assignee: PRODESIN (Productos Esteve Internacional S.A.)Inventors: Antonio Esteve Subirana, Jose Esteve Soler
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Patent number: 4214081Abstract: Compounds having the formula ##STR1## or a pharmaceutically acceptable salt thereof, wherein R.sub.1 is alkyl, cycloalkyl or aryl; R.sub.2 is acyl or sulfonyl; R.sub.3 is alkylamino, dialkylamino or a nitrogen containing heterocyclic group; R.sub.4 is alkoxy; A.sub.1 is a saturated bond or an alkylene group having 1 to 4 carbon atoms; and A.sub.2 is an alkylene group having 2 to 5 carbon atoms; have antiinflammatory activity.Type: GrantFiled: December 26, 1978Date of Patent: July 22, 1980Assignee: E. R. Squibb & Sons, Inc.Inventor: John Krapcho
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Patent number: 4209302Abstract: New markers for petroleum fuels; a method of marking said fuels with a marker and of subsequently detecting the presence of said marker; and marked fuels are provided. The markers include the following compounds: ##STR1## 1-(4-morpholino)-3-(alpha naphthylamino)-propane, ##STR2## 1-(4-morpholino)-3-(beta naphthylamino)-propane, ##STR3## where R.sub.1 and R.sub.2 may be hydrogen or alkyl having from one to twenty carbon atoms.The marker is detected in said marked fuel by (1) extraction with an acidic aqueous solution and (2) admixture with a stabilized solution of diazotized 2-chlor-4-nitroaniline to yield a color characteristic of the marker.Type: GrantFiled: May 10, 1979Date of Patent: June 24, 1980Assignee: Morton-Norwich Products, Inc.Inventor: Richard B. Orelup
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Patent number: 4205168Abstract: N-carbamylalkyl-2,6-dialkyl-.alpha.-haloacetanilides have herbicidal activity, particularly in pre-emergent applications against grassy weeds.Type: GrantFiled: September 24, 1973Date of Patent: May 27, 1980Assignee: Chevron Research CompanyInventor: David C. K. Chan
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Patent number: 4156079Abstract: Compounds having the formula ##STR1## or a pharmaceutically acceptable salt thereof, wherein R.sub.1 is alkyl, cycloalkyl or aryl; R.sub.2 is acyl or sulfonyl; R.sub.3 is alkylamino, dialkylamino or a nitrogen containing heterocyclic group; R.sub.4 is alkoxy; A.sub.1 is a saturated bond or an alkylene group having 1 to 4 carbon atoms; and A.sub.2 is an alkylene group having 2 to 5 carbon atoms; have antiinflammatory activity.Type: GrantFiled: June 19, 1978Date of Patent: May 22, 1979Assignee: E. R. Squibb & Sons, Inc.Inventor: John Krapcho
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Patent number: 4151354Abstract: Compounds having the formula ##STR1## wherein R.sub.1 is alkyl, cycloalkyl or aryl; R.sub.2 is acyl or sulfonyl; R.sub.3 is a nitrogen containing heterocyclic group; A.sub.1 is a saturated bond or an alkylene group having 1 to 4 carbon atoms; and A.sub.2 is an alkylene group having 2 to 5 carbon atoms; have antiinflammatory activity.Type: GrantFiled: August 2, 1978Date of Patent: April 24, 1979Assignee: E. R. Squibb & Sons, Inc.Inventor: John Krapcho
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Patent number: 4146558Abstract: Water-soluble cationic dyestuffs of the formulae ##STR1## WHEREIN R.sup.0 is hydrogen, lower-alkyl or hydroxy-lower-alkyl;R.sup.1 is lower-alkyl, lower-alkenyl or hydroxy-lower-alkyl;R.sup.2 is lower-alkyl, lower-alkenyl, hydroxy-lower-alkyl or -(lower-alkylene)-NR.sup.0 Y or R.sup.1 and R.sup.2 together with the nitrogen atom, are pyrrolidino, piperidino or 4-lower-alkanoyl piperazino;Y is hydrogen or ##STR2## wherein R is hydrogen, lower-alkyl, lower-alkenyl, phenyl or phenyl-lower-alkyl;A is a member selected from the group consisting of an aromatic azo dyestuff residue attached to the quaternary ammonium nitrogen atom through a lower-alkylene bridge.K is a small integer whose value is dependent on the nature of A such that it has a range from one to two;R.sup.8 is lower-alkyl, lower-alkenyl or hydroxy-lower-alkyl;R.sup.9 is lower-alkyl, hydroxy-lower-alkyl or NH.sub.2 ;R.sup.10 is lower-alkyl or lower-alkenyl;A.sup.Type: GrantFiled: October 6, 1977Date of Patent: March 27, 1979Assignee: Sterling Drug Inc.Inventors: Patrick J. Jefferies, Nathan N. Crounse
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Patent number: 4137304Abstract: Cyclic and acyclic amides, substituted ureas and sulphonamides are disclosed having the property of stimulating the cold receptors of the nervous system of the body to produce a cold sensation and are used for this purpose in a variety of edible and topical preparations.Type: GrantFiled: June 2, 1977Date of Patent: January 30, 1979Assignee: Wilkinson Sword LimitedInventors: David G. Rowsell, Roger Hems
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Patent number: 4136256Abstract: This disclosure describes 4-(monoalkylamino)benzoic acid amides and imidates useful as hypolipidemic and antiatherosclerotic agents.Type: GrantFiled: September 27, 1977Date of Patent: January 23, 1979Assignee: American Cyanamid CompanyInventor: Robert G. Shepherd
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Patent number: 4128643Abstract: (2-Amino-4-quinazolinyl)-quanidines of the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and n have the defined meanings, and their physiologically tolerable acid addition salts, process for preparing these compounds, pharmaceutical preparations containing them and their use as medicines.Type: GrantFiled: May 26, 1977Date of Patent: December 5, 1978Assignee: Hoechst AktiengesellschaftInventors: Wulf Merkel, Hans G. Alpermann, Karl Geisen, Norbert Kothe, Walter Ried
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Substituted amides and sulfonamides containing a heterocyclic group having antiinflammatory activity
Patent number: 4122255Abstract: Compounds having the formula ##STR1## wherein R.sub.1 is alkyl, cycloalkyl or aryl; R.sub.2 is acyl or sulfonyl; R.sub.3 is a nitrogen containing heterocyclic group; A.sub.1 is a saturated bond or an alkylene group having 1 to 4 carbon atoms; and A.sub.2 is an alkylene group having 2 to 5 carbon atoms; have antiinflammatory activity.Type: GrantFiled: September 21, 1977Date of Patent: October 24, 1978Assignee: E. R. Squibb & Sons, Inc.Inventor: John Krapcho -
Patent number: 4115445Abstract: The present invention provides a process for preparing a trisubstituted urea of the general formula:R(NHCONR'R").sub.nin which R is a substituted or unsubstituted mono-, di- or polyvalent aromatic radical, R' is a substituted or unsubstituted monovalent aliphatic or aromatic radical and R" is a substituted or unsubstituted monovalent aliphatic radical or R' and R" together represent a substituted or unsubstituted divalent radical in which at least one of the two carbon atoms adjoining the nitrogen atom of the urea is aliphatic, and n is an integer, wherein an aromatic nitrocompound of the general formula:--R(NO.sub.2).sub.n or an aromatic nitrosocompound of the general formula:--R(NO).sub.n is allowed to react with a secondary ammonium N,N-disubstituted thiolcarbamate of the general formula:R'R"NCOS.sup.-.NH.sub.2.sup.Type: GrantFiled: February 12, 1975Date of Patent: September 19, 1978Assignee: Quimco GmbHInventor: Colin John Hearsey
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Patent number: 4103087Abstract: An improved process is disclosed for selectively producing a di-(N,N-disubstituted amino) alkane compound which includes contacting an (N,N-disubstituted) amino alkanol compound with an (N,N-disubstituted) amine compound in the presence of a catalytically effective amount of an aluminum phosphate catalyst at a temperature of from about 240.degree. C to 320.degree. C under a pressure sufficient to maintain the mixture substantially in liquid phase and recovering from the resultant reaction mixture the di-(N,N-disubstituted amino) alkane compound.According to a preferred embodiment, N-(2-hydroxyethyl) morpholine is contacted with morpholine in the presence of a catalytically effective amount of a heterogeneous aluminum phosphate catalyst at temperatures of from about 260.degree. C to about 300.degree. C in liquid phase to selectively produce the corresponding N,N'-dimorpholino ethane (DMORE).Type: GrantFiled: April 1, 1977Date of Patent: July 25, 1978Assignee: Texaco Development CorporationInventor: Michael E. Brennan
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Patent number: 4098789Abstract: Compounds having the formula ##STR1## and the pharmaceutically acceptable salts thereof, wherein R.sub.1 is alkoxycarbonyl, amido or substituted amido; R.sub.2 is acyl or sulfonyl; R.sub.3 is alkylamino, dialkylamino or a nitrogen containing heterocyclic group; A.sub.1 is an alkylene group having 2 to 5 carbon atoms; and n is 1, 2 or 3; have antiinflammatory activity.Type: GrantFiled: March 2, 1977Date of Patent: July 4, 1978Assignee: E. R. Squibb & Sons, Inc.Inventors: John Krapcho, Chester F. Turk
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Patent number: 4098895Abstract: Amino aceto anilides of the formula I shown hereinafter are effective microbicides. They may be used to control fungi on plants or parts of plants or to prevent them from fungi attack.Type: GrantFiled: September 24, 1976Date of Patent: July 4, 1978Assignee: Ciba-Geigy CorporationInventors: Adolf Hubele, Walter Kunz, Wolfgang Eckhardt
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Patent number: 4096267Abstract: [1-Oxo-2-aryl or thienyl-2-substituted-5-indanyloxy (or thio)]aklanoic acid, derivatives thereof, their salts, esters and amides are disclosed. The products display a dual pharmaceutical utility in that they exhibit diuretic, saluretic and uricosuric activity. Also disclosed are processes for the preparation of such [1-oxo-2-aryl or thienyl-2-substituted-5-indanyloxy (or thio)]alkanoic acids, pharmaceutical compositions comprising therapeutically effective amounts of such compounds and methods of treatment comprising administering such compounds and compositions.Type: GrantFiled: June 10, 1975Date of Patent: June 20, 1978Assignee: Merck & Co., Inc.Inventors: Edward J. Cragoe, Jr., Otto W. Woltersdorf, Jr.
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Patent number: 4093806Abstract: Indoaniline of the formula ##STR1## wherein R.sub.1 represents hydrogen, halogen, alkyl or alkoxy; R.sub.2 represents alkyl, hydroxyalkyl, carbamylalkyl, piperidinoalkyl, morpholinoalkyl, sulfoalkyl, dialkylaminoalkyl, acylaminoalkyl, (preferably acetylaminoalkyl or benzoylaminoalkyl) and mesylaminoalkyl;R.sub.3 represents hydroxyalkyl, carbamylalkyl, piperidonoalkyl, morpholinoalkyl, sulfoalkyl, dialkylaminoalkyl, acylaminoalkyl, (preferably acetylaminoalkyl or benzoylaminoalkyl), mesylaminoalkyl; or R.sub.2 and R.sub.3 together form with the nitrogen atom to which they are attached a heterocycle selected from piperidino or morpholino;R.sub.4, r.sub.5 and R.sub.6 each independently represents hydrogen, halogen, alkyl, alkoxy, acylamino, ureido or carbalkoxyamino, and R.sub.5 can also represent amino, alkylamino, hydroxyalkylamino or carbamylalkylamino. The alkyl and alkoxy groups above can contain from 1 to 6 carbon atoms and the acyl group can contain from 2 to 7 carbon atoms.Type: GrantFiled: May 20, 1977Date of Patent: June 6, 1978Assignee: L'OrealInventors: Gregoire Kalopissis, Andree Bugaut, Francoise Estradier
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Patent number: 4093734Abstract: Compounds of the formula ##STR1## wherein (A) WHEN THE AMINO-SUBSTITUENT IS IN THE P-POSITION WITH RESPECT TO THE CARBONYL GROUP,R.sub.1 is chlorine in the o-position with respect to the carbonyl group,R.sub.2 is hydrogen, andR.sub.3 is ethylamino, cyclopentylamino, cyclohexylamino, cycloheptylamino, N-methyl-cyclohexylamino, benzylamino or 1-ethyl-pyrrolidyl-(2)-aminomethyl, or(b) when the amino-substituent is in the o--, m-- or p-position with respect to the carbonyl group,R.sub.1 is hydrogen, chlorine or bromine,R.sub.2 is trifluoromethyl, nitro or, when R.sub.4 is 1-(alkyl of 1 to 3 carbon atoms)-pyrrolidyl or 1-(alkyl of 1 to 3 carbon atoms)-piperidyl, also fluorine, chlorine, bromine or methyl,R.sub.3 is (alkyl of 1 to 5 carbon atoms)-amino, (cycloalkyl of 3 to 7 carbon atoms)-amino, benzylamino, quinuclidinyl-amino or --NH--(CH.sub.2).sub.n --R.sub.4where R.sub.Type: GrantFiled: October 22, 1976Date of Patent: June 6, 1978Assignee: Boehringer Ingelheim GmbHInventors: Gerd Kruger, Johannes Keck, Klaus Reinhold Noll, Helmut Pieper, Harald Ziegler, Helmut Ballhause, Joachim Kahling
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Patent number: 4091006Abstract: A new series of substituted esters of 3-hydroxyindone compounds have been found to have exceptional miticidal and herbicidal activity.Type: GrantFiled: October 1, 1975Date of Patent: May 23, 1978Assignee: Union Carbide CorporationInventors: John A. Durden, Jr., Anthony A. Sousa, John F. Stephen
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Patent number: 4084052Abstract: 2,5-DIAMINO-1,4-BENZOQUINONES ARE USED IN THE PRODUCTION OF HAIR DYE COMPOSITIONS AND CAN BE PREPARED BY CONDENSING A CORRESPONDING 3-AMINO-4-METHOXY PHENOL DERIVATIVE ON ONE OF A CORRESPONDING HYDROXY ANILINE OR PHENYLENEDIAMINE DERIVATIVE, A CORRESPONDING BENZOQUINONE IMINE DERIVATIVE OR A CORRESPONDING NITROSO DERIVATIVE.Type: GrantFiled: January 25, 1977Date of Patent: April 11, 1978Assignee: L'OrealInventors: Andree Bugaut, Monique Laudon
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Patent number: 4080452Abstract: This invention relates to novel N-acyl anilines, to a process for their preparation and to pharmaceutical compositions containing them. The N-acyl anilines are obtained by condensing a substituted aniline with an aminolower alkyl carboxylic acid or a functional derivative thereof.The compounds of the invention have therapeutic utility namely in the gastro-enterologic field.Type: GrantFiled: February 9, 1976Date of Patent: March 21, 1978Assignee: Science Union et Cie, Societe Francaise de Recherche MedicaleInventors: Charles Malen, Pierre Roger, Xavier Pascaud
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Patent number: 4072705Abstract: Compounds of the formula ##STR1## in which A is lower alkyl, or a substituted or unsubstituted phenyl, thienyl, furyl, indolyl or thiaindolyl radical, R, X.sub.4 and X.sub.5 are hydrogen or lower alkyl, Y is hydrogen, hydroxy, etherified hydroxy, substituted amino, or N-attached heterocyclyl, X.sub.0 is O or OCH.sub.2 CH.sub.2 O, R' represents hydrogen, lower alkyl or acetyl; and acid-addition salts thereof, are novel and useful in pharmacy as hypolipaemiant, hypocholesterolaemiant and cholagogic agents or in the preparation of such agents.Type: GrantFiled: February 9, 1976Date of Patent: February 7, 1978Assignee: Orchimed S.A.Inventor: Andre Mieville
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Patent number: 4068079Abstract: A composition of matter is described herein which has herbicidal activity and methods of use. The composition is defined by the following generic formula ##STR1## wherein X and Y are independently selected from the group consisting of chloro, bromo, and trifluoromethyl; n is either 0 or 1; m is either 0 or 1; and R and R.sub.1 are independently selected from the group consisting of lower alkyl from C.sub.1 to C.sub.3, inclusive, and lower alkoxy from C.sub.1 to C.sub.3, inclusive, or R and R.sub.Type: GrantFiled: January 13, 1977Date of Patent: January 10, 1978Assignee: Stauffer Chemical CompanyInventor: Edmund J. Gaughan
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Patent number: RE30577Abstract: .[.Ethers.]. .Iadd.An ether .Iaddend.of n-propanolamine, preparation thereof and .[.their.]. .Iadd.its .Iaddend.use in treatment of cardiovascular conditions.Type: GrantFiled: February 27, 1979Date of Patent: April 14, 1981Assignee: Centre Europeen de Recherches MauvernayInventors: Norbert Busch, Jacques Simond, Andre Monteil, Jacques Moleyre, Roland Y. Mauvernay