Carbocyclic Ring Bonded Directly To The Nitrogen Patents (Class 544/165)
  • Patent number: 4375543
    Abstract: 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: Grant
    Filed: July 29, 1981
    Date of Patent: March 1, 1983
    Assignee: Chemie Linz Aktiengesellschaft
    Inventors: Josef Wieser, Josef Krieger
  • Patent number: 4372583
    Abstract: 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: Grant
    Filed: August 17, 1981
    Date of Patent: February 8, 1983
    Inventor: Anthony E. Vassiliades
  • Patent number: 4367339
    Abstract: 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: Grant
    Filed: August 18, 1980
    Date of Patent: January 4, 1983
    Assignee: American Cyanamid Company
    Inventors: Thomas D. O'Neal, Prithvi R. Bhalla, Barrington Cross
  • Patent number: 4362546
    Abstract: 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: Grant
    Filed: May 27, 1980
    Date of Patent: December 7, 1982
    Assignee: Takeda Chemical Industries, Ltd.
    Inventor: Hiroshi Nagase
  • Patent number: 4361516
    Abstract: 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: Grant
    Filed: October 6, 1976
    Date of Patent: November 30, 1982
    Assignee: Societe Anonyme dite: L'Oreal
    Inventors: Gregoire Kalopissis, Andree Bugaut, Francoise Estradier
  • Patent number: 4350518
    Abstract: 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: Grant
    Filed: February 23, 1981
    Date of Patent: September 21, 1982
    Assignee: BASF Aktiengesellschaft
    Inventors: Hubert Sauter, Bernd Zeeh, Ernst Buschmann, Johann Jung
  • Patent number: 4343939
    Abstract: Glyolic acid esters and amides of bis(p-disubstitutedaminophenyl)carbinols are disclosed as color formers for use in transfer sets.
    Type: Grant
    Filed: April 22, 1981
    Date of Patent: August 10, 1982
    Assignee: American Cyanamid Company
    Inventors: Frank F. Cesark, Robert J. Manfre, Daniel W. Thomas
  • Patent number: 4342756
    Abstract: 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: Grant
    Filed: April 29, 1981
    Date of Patent: August 3, 1982
    Assignee: Glaxo Group Limited
    Inventors: Eric W. Collington, Peter Hallett, Christopher J. Wallis, John Bradshaw, Norman F. Hayes
  • Patent number: 4340540
    Abstract: 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: Grant
    Filed: June 26, 1980
    Date of Patent: July 20, 1982
    Assignee: Bayer Aktiengesellschaft
    Inventor: Karl H. Hermann
  • Patent number: 4333929
    Abstract: 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: Grant
    Filed: January 19, 1981
    Date of Patent: June 8, 1982
    Assignee: Beecham Group Limited
    Inventor: Barrie C. C. Cantello
  • Patent number: 4330542
    Abstract: 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: Grant
    Filed: May 16, 1980
    Date of Patent: May 18, 1982
    Assignee: Sanofi
    Inventors: Marcel Descamps, Charles Goldenberg
  • Patent number: 4330476
    Abstract: 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: Grant
    Filed: June 26, 1980
    Date of Patent: May 18, 1982
    Assignee: Bayer Aktiengesellschaft
    Inventor: Karl H. Hermann
  • Patent number: 4310533
    Abstract: 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: Grant
    Filed: August 29, 1980
    Date of Patent: January 12, 1982
    Assignee: Ono Pharmaceutical Co., Ltd.
    Inventors: Yoshiaki Uegai, Tsuyoshi Watanabe, Masashi Shiota, Itsuo Okumoto, Naohiro Kayama
  • Patent number: 4308383
    Abstract: 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: Grant
    Filed: December 22, 1980
    Date of Patent: December 29, 1981
    Assignee: Chemie Linz Aktiengesellschaft
    Inventors: Josef Wieser, Josef Krieger
  • Patent number: 4305940
    Abstract: 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: Grant
    Filed: November 18, 1980
    Date of Patent: December 15, 1981
    Assignee: B.B.R. Boehringer Biochemia Robin S.p.A.
    Inventor: Giuseppe Quadro
  • Patent number: 4285942
    Abstract: 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: Grant
    Filed: December 3, 1979
    Date of Patent: August 25, 1981
    Assignee: Egyt Gyogyszervegyeszeti Gyar
    Inventors: Zoltan Budai, Aranka Lay nee Konya, Tibor Mezei, Katalin Grasser, Lujza Petocz, Eniko Kiszelly, Ibolya Kosoczky
  • Patent number: 4283532
    Abstract: 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: Grant
    Filed: August 7, 1979
    Date of Patent: August 11, 1981
    Assignee: Ikeda Mohando Co., Ltd.
    Inventor: Fujio Nohara
  • Patent number: 4282206
    Abstract: 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: Grant
    Filed: November 15, 1979
    Date of Patent: August 4, 1981
    Assignee: Westwood Pharmaceuticals Inc.
    Inventors: Paul L. Warner, Jr., F. Christopher Zusi
  • Patent number: 4271160
    Abstract: 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: Grant
    Filed: June 20, 1980
    Date of Patent: June 2, 1981
    Assignee: Farmitalia Carlo Erba S.p.A.
    Inventors: Piero Melloni, Arturo Della Torre, Giovanni C. Carniel, Alessandro Rossi
  • Patent number: 4269837
    Abstract: Novel guanylamidines and the pharmaceutically acceptable acid addition salts thereof having activity as hypoglycemic agents are disclosed.
    Type: Grant
    Filed: February 19, 1980
    Date of Patent: May 26, 1981
    Assignee: Pfizer Inc.
    Inventors: David S. Watt, Jeffrey L. Ives
  • Patent number: 4260749
    Abstract: 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: Grant
    Filed: May 9, 1980
    Date of Patent: April 7, 1981
    Assignee: L'Oreal
    Inventors: Andree Bugaut, Monique Laudon
  • Patent number: 4252804
    Abstract: 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: Grant
    Filed: January 13, 1978
    Date of Patent: February 24, 1981
    Assignee: Metabio-Joullie
    Inventors: Maurice Joullie, Gabriel Maillard, Lucien Lakah, Christian J. M. Warolin
  • Patent number: 4252801
    Abstract: 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: Grant
    Filed: January 4, 1980
    Date of Patent: February 24, 1981
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Frederic P. Hauck, Glenn A. Jacobs
  • Patent number: 4246260
    Abstract: 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: Grant
    Filed: March 19, 1979
    Date of Patent: January 20, 1981
    Assignee: Bayer Aktiengesellschaft
    Inventors: Heinrich Kolling, Ekkehard Niemers, Hartmund Wollweber, Herbert Thomas
  • Patent number: 4243804
    Abstract: 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: Grant
    Filed: April 30, 1979
    Date of Patent: January 6, 1981
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: John Krapcho
  • Patent number: 4229449
    Abstract: 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: Grant
    Filed: January 8, 1979
    Date of Patent: October 21, 1980
    Assignee: Farmitalia Carlo Erba, S.p.A.
    Inventors: Piero Melloni, Arturo D. Torre, Giovanni C. Carniel, Alessandro Rossi
  • Patent number: 4216214
    Abstract: 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: Grant
    Filed: December 27, 1977
    Date of Patent: August 5, 1980
    Assignee: PRODESIN (Productos Esteve Internacional S.A.)
    Inventors: Antonio Esteve Subirana, Jose Esteve Soler
  • Patent number: 4214081
    Abstract: 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: Grant
    Filed: December 26, 1978
    Date of Patent: July 22, 1980
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: John Krapcho
  • Patent number: 4209302
    Abstract: 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: Grant
    Filed: May 10, 1979
    Date of Patent: June 24, 1980
    Assignee: Morton-Norwich Products, Inc.
    Inventor: Richard B. Orelup
  • Patent number: 4205168
    Abstract: N-carbamylalkyl-2,6-dialkyl-.alpha.-haloacetanilides have herbicidal activity, particularly in pre-emergent applications against grassy weeds.
    Type: Grant
    Filed: September 24, 1973
    Date of Patent: May 27, 1980
    Assignee: Chevron Research Company
    Inventor: David C. K. Chan
  • Patent number: 4156079
    Abstract: 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: Grant
    Filed: June 19, 1978
    Date of Patent: May 22, 1979
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: John Krapcho
  • Patent number: 4151354
    Abstract: 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: Grant
    Filed: August 2, 1978
    Date of Patent: April 24, 1979
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: John Krapcho
  • Patent number: 4146558
    Abstract: 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: Grant
    Filed: October 6, 1977
    Date of Patent: March 27, 1979
    Assignee: Sterling Drug Inc.
    Inventors: Patrick J. Jefferies, Nathan N. Crounse
  • Patent number: 4137304
    Abstract: 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: Grant
    Filed: June 2, 1977
    Date of Patent: January 30, 1979
    Assignee: Wilkinson Sword Limited
    Inventors: David G. Rowsell, Roger Hems
  • Patent number: 4136256
    Abstract: This disclosure describes 4-(monoalkylamino)benzoic acid amides and imidates useful as hypolipidemic and antiatherosclerotic agents.
    Type: Grant
    Filed: September 27, 1977
    Date of Patent: January 23, 1979
    Assignee: American Cyanamid Company
    Inventor: Robert G. Shepherd
  • Patent number: 4128643
    Abstract: (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: Grant
    Filed: May 26, 1977
    Date of Patent: December 5, 1978
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Wulf Merkel, Hans G. Alpermann, Karl Geisen, Norbert Kothe, Walter Ried
  • Patent number: 4122255
    Abstract: 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: Grant
    Filed: September 21, 1977
    Date of Patent: October 24, 1978
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: John Krapcho
  • Patent number: 4115445
    Abstract: 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: Grant
    Filed: February 12, 1975
    Date of Patent: September 19, 1978
    Assignee: Quimco GmbH
    Inventor: Colin John Hearsey
  • Patent number: 4103087
    Abstract: 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: Grant
    Filed: April 1, 1977
    Date of Patent: July 25, 1978
    Assignee: Texaco Development Corporation
    Inventor: Michael E. Brennan
  • Patent number: 4098789
    Abstract: 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: Grant
    Filed: March 2, 1977
    Date of Patent: July 4, 1978
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: John Krapcho, Chester F. Turk
  • Patent number: 4098895
    Abstract: 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: Grant
    Filed: September 24, 1976
    Date of Patent: July 4, 1978
    Assignee: Ciba-Geigy Corporation
    Inventors: Adolf Hubele, Walter Kunz, Wolfgang Eckhardt
  • Patent number: 4096267
    Abstract: [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: Grant
    Filed: June 10, 1975
    Date of Patent: June 20, 1978
    Assignee: Merck & Co., Inc.
    Inventors: Edward J. Cragoe, Jr., Otto W. Woltersdorf, Jr.
  • Patent number: 4093806
    Abstract: 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: Grant
    Filed: May 20, 1977
    Date of Patent: June 6, 1978
    Assignee: L'Oreal
    Inventors: Gregoire Kalopissis, Andree Bugaut, Francoise Estradier
  • Patent number: 4093734
    Abstract: 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: Grant
    Filed: October 22, 1976
    Date of Patent: June 6, 1978
    Assignee: Boehringer Ingelheim GmbH
    Inventors: Gerd Kruger, Johannes Keck, Klaus Reinhold Noll, Helmut Pieper, Harald Ziegler, Helmut Ballhause, Joachim Kahling
  • Patent number: 4091006
    Abstract: A new series of substituted esters of 3-hydroxyindone compounds have been found to have exceptional miticidal and herbicidal activity.
    Type: Grant
    Filed: October 1, 1975
    Date of Patent: May 23, 1978
    Assignee: Union Carbide Corporation
    Inventors: John A. Durden, Jr., Anthony A. Sousa, John F. Stephen
  • Patent number: 4084052
    Abstract: 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: Grant
    Filed: January 25, 1977
    Date of Patent: April 11, 1978
    Assignee: L'Oreal
    Inventors: Andree Bugaut, Monique Laudon
  • Patent number: 4080452
    Abstract: 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: Grant
    Filed: February 9, 1976
    Date of Patent: March 21, 1978
    Assignee: Science Union et Cie, Societe Francaise de Recherche Medicale
    Inventors: Charles Malen, Pierre Roger, Xavier Pascaud
  • Patent number: 4072705
    Abstract: 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: Grant
    Filed: February 9, 1976
    Date of Patent: February 7, 1978
    Assignee: Orchimed S.A.
    Inventor: Andre Mieville
  • Patent number: 4068079
    Abstract: 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: Grant
    Filed: January 13, 1977
    Date of Patent: January 10, 1978
    Assignee: Stauffer Chemical Company
    Inventor: Edmund J. Gaughan
  • Patent number: RE30577
    Abstract: .[.Ethers.]. .Iadd.An ether .Iaddend.of n-propanolamine, preparation thereof and .[.their.]. .Iadd.its .Iaddend.use in treatment of cardiovascular conditions.
    Type: Grant
    Filed: February 27, 1979
    Date of Patent: April 14, 1981
    Assignee: Centre Europeen de Recherches Mauvernay
    Inventors: Norbert Busch, Jacques Simond, Andre Monteil, Jacques Moleyre, Roland Y. Mauvernay