Nitro Bonded Directly To The Carbocyclic Ring Patents (Class 544/167)
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Patent number: 4837236Abstract: A heterocyclic compound of the formula: ##STR1## wherein A is an oxygen atom or a sulfur atom;B is either one of the groups: --CH.sub.2 --CHR.sup.1 -- or --CH.dbd.CR.sup.1 -- (in which R.sup.1 is a hydrogen atom or a methyl group);W is, the same or different, each a hydrogen atom, a halogen atom, a lower alkyl group or a lower alkoxy group;X is either one of the following groups: ##STR2## (in which R.sup.2 is a hydrogen atom, a lower alkyl group, a lower alkoxy group, a lower alkoxy(lower)alkyl group, a hydroxyl group or a hydroxy(lower)alkyl group, R.sup.3 is a hydrogen atom or a lower alkyl group and n is an integer of 0 or 1);Z is, the same or different, each a hydrogen atom, a halogen atom, a lower alkyl group, a lower alkoxy group, a halo(lower)alkyl group, a halo(lower)alkoxy group, a nitro group, a methylenedioxy group or a cyano group;p is an integer of 0 to 5; andq is an integer of 0 or 1, or its salt, which is useful as a fungicide.Type: GrantFiled: September 24, 1987Date of Patent: June 6, 1989Assignee: Sumitomo Chemical Company, LimitedInventors: Naoto Meki, Hirotaka Takano
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Patent number: 4810725Abstract: 1-Aryloxy-3-(substituted aminoalkylamino)-2-propanols and pharmaceutically acceptable salts thereof have .beta.-adrenergic blocking activity with some cardioselectivity and hence are useful as anti-hypertensive, antianginal, antiarrhythmic and cardioprotective agents and in the treatment of elevated intraocular pressure such as glaucoma.Type: GrantFiled: October 14, 1986Date of Patent: March 7, 1989Assignee: Merck & Co., Inc.Inventors: John J. Baldwin, Gerald S. Ponticello, Sandor L. Varga
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Patent number: 4737498Abstract: Novel N-alkyl-2,6-dimethylmorpholinocarboxamide salts of the general formula I, ##STR1## processes for their preparation, and their use as fungicides for controlling pathogenic fungi. The agents according to the invention additionally possess plant growth-regulating properties. The meanings of R.sup.1, R.sup.2, R.sup.3, R.sup.4 and X.sup.- are given in the description.Type: GrantFiled: July 2, 1986Date of Patent: April 12, 1988Assignee: BASF AktiengesellschaftInventors: Lothar Banasiak, Wilfried Edlich, Horst Lyr, Eva Nega, Marianne Sunkel
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Patent number: 4731383Abstract: The invention relates to new aminoguanidine derivatives of the general formula (I), ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 each represent hydrogen or halogen atom, C.sub.1-4 alkyl, nitro, trifluoromethyl or C.sub.1-4 alkoxy group,R.sup.4 and R.sup.5 represent a C.sub.1-4 alkyl group, furthermore NR.sup.4 R.sup.5 may form a 5 to 7 membered saturated heterocyclic group containing either one or two nitrogen atoms or a nitrogen and an oxygen atom and being optionally substituted by one or two methyl, hydroxymethyl or hydroxyethyl groups,R.sup.6 and R.sup.7 each represent a hydrogen atom, normal or branched C.sub.1-4 alkyl or C.sub.2-4 alkenyl group,and to their pharmaceutically acceptable acid addition salts as well as to a process for the preparation thereof.The new compounds of the invention possess valuable antiarrhythmic activity and are devoid of the undesired circulatory side effects of the known antiarrhythmic compounds.Type: GrantFiled: October 29, 1986Date of Patent: March 15, 1988Assignee: Biogal GyogyszergyarInventors: Istvan Erczi, Jeno Marosfalvi, Gyorgy Rabloczky, Andras Varro, Maria Kuhar nee Kurthy, Istvan Elekes, Laszlo Szatmary, Laszlo Jaszlits
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Patent number: 4693850Abstract: Novel synthetic steps and intermediates leading to guanidines such as the anti-diabetic compound linogliride.Type: GrantFiled: November 26, 1986Date of Patent: September 15, 1987Assignee: McNeilab, Inc.Inventors: Cynthia A. Maryanoff, James N. Plampin, Robin C. Stanzione
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Patent number: 4692446Abstract: Novel compounds of the general formula ##STR1## wherein R.sub.1 is lower alkyl, lower cycloalkyl, lower alkenyl, lower alkynyl, lower alkyl carboxymethyl, aryl carboxymethyl, aryl, or aralkyl; A is a direct bond, lower alkylene, or lower alkenylene; x is 1 or 2, provided that when x is greater than 1, different occurrences of the ##STR2## group may be the same or different; Ar is heterocyclic, unsubstituted aromatic or aromatic substituted with lower alkyl, lower alkenyl, lower alkynyl, lower alkoxy, halogen, acetamido, amino, nitro, lower alkylamino, hydroxy, lower hydroxyalkyl or cyano; W is alkylene containing from 1 to about 10 carbon atoms; and B is --NR.sub.2 COR.sub.3, --NR.sub.2 CONR.sub.3 R.sub.4, --NR.sub.2 SO.sub.2 R.sub.3, --NR.sub.2 SO.sub.2 NR.sub.3 R.sub.4, or --NR.sub.2 COOR.sub.5, wherein R.sub.2, R.sub.3, R.sub.4 and R.sub.5 may be the same or different and may be hydrogen, alkyl, alkoxyalkyl, alkoxyaryl, cycloalkyl, alkenyl, alkynyl, aryl, heteroaryl, or aralkyl, except that R.sub.3 and R.Type: GrantFiled: October 28, 1986Date of Patent: September 8, 1987Assignee: E. I. Du Pont de Nemours & Co., Inc.Inventors: Paul W. Erhardt, William L. Matier
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Patent number: 4656270Abstract: Novel synthetic steps and intermediates leading to guanidines such as the anti-diabetic compound linogliride.Type: GrantFiled: March 15, 1985Date of Patent: April 7, 1987Assignee: McNeilab, Inc.Inventors: Cynthia A. Maryanoff, James N. Plampin, Robin C. Stanzione
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Patent number: 4619666Abstract: Hair coloring preparations containing substantive hair dyes corresponding to the following general formula ##STR1## in which A is an SO.sub.3 H group or a COOH group, and R.sup.1 and R.sup.2 are hydrogen or other substituents, show high fastness properties and favorable toxicological properties. The substantive hair dyes are preferably present in the hair coloring preparations in a quantity of from 0.01 to 5.0% by weight, optionally in conjunction with known oxidation hair dye precursors.Type: GrantFiled: July 8, 1985Date of Patent: October 28, 1986Assignee: Henkel Kommanditgesellschaft auf AktienInventors: David Rose, Edgar Lieske, Norbert Maak
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Patent number: 4610985Abstract: Allophanate derivatives of the formula ##STR1## in which R.sup.1 and R.sup.2 can be identical or different and represent an aliphatic, cycloaliphatic, araliphatic or aromatic radical each of which is optionally monosubstituted or polysubstituted by identical or different substituents andR.sup.3 represents the radical --XR.sup.4 or --NR.sup.5 R.sup.6,whereinR.sup.4 represents alkyl, alkoxyalkyl, or aryl which is optionally monosubstituted or polysubstituted by identical or different substituents, X represents oxygen or sulphur andR.sup.5 and R.sup.6 are identical or different and represent hydrogen, alkyl, or aryl which is optionally monosubstituted or polysubstituted by identical or different substituents, orR.sup.5 and R.sup.6, together with the nitrogen atom on which they stand, form a saturated heterocyclic radical which is optionally monosubstituted or polysubstituted by identical or different substituents and can be interrupted by further hetero-atoms,which possess fungicidal activity.Type: GrantFiled: April 10, 1985Date of Patent: September 9, 1986Assignee: Bayer AktiengesellschaftInventors: Wolfgang Fuhrer, Engelbert Kuhle, Gerd Hanssler
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Patent number: 4609759Abstract: This invention pertains to a process for producing 2,6 dinitroaniline derivates which are suited as intermediates for herbicides. The process involves the formation of a 1,2,6-trinitro-aromatic isomer and the subsequent nucleophilic displacement of the 1-nitrosubstituent with an amine. The reaction products can easily be separated from other organics by forming an amine salt and extracting with water.Type: GrantFiled: May 2, 1984Date of Patent: September 2, 1986Assignee: Air Products and Chemicals, Inc.Inventor: Richard V. C. Carr
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Patent number: 4605654Abstract: The present invention relates to new 2-(arylalkyloxymethyl)morpholine derivatives, the preparation thereof and their application as drugs which are useful in the treatment of disorders of the central nervous system.The 2-(arylalkyloxymethyl)morpholine derivatives according to the invention correspond to the general formula (I): ##STR1## in which: Ar denotes an aromatic group and more especially the following radicals: ##STR2## in the case where Ar denotes a phenyl radical and R denotes a hydrogen atom, an alkyl, alkoxy or halogen group, a trifluoromethyl radical, a nitro or amino group, a hydroxy group or an arylalkyloxy group.Type: GrantFiled: December 17, 1985Date of Patent: August 12, 1986Assignee: P. F. MedicamentInventors: Henri Cousse, Gilbert Mouzin, Jean-Pierre Rieu, Mike Briley, Antoine Stenger
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Patent number: 4550205Abstract: The invention relates to new diphenyl ethers of the general formula ##STR1## wherein X is a hydrogen atom, a halogen atom, a nitro group, an optionally halogenated alkyl, alkoxy or alkylthio group having 1-6 carbon atoms, or an alkanoyl group having 1-4 carbon atoms;Y is a nitrogen atom or a group of the formula CH or CCl;Z is a hydrogen atom, a halogen atom, a nitro group, an optionally halogenated alkyl group having 1-4 carbon atoms, or an alkanoyl group having 1-4 carbon atoms; n is 0-2;R.sub.1 is a hydrogen atom, or an alkyl or alkanoyl group having 1-4 carbon atoms;R.sub.2 and R.sub.3 are equal or different and represent hydrogen atoms or alkyl groups having 1-4 carbon atoms; andA is a group of the general formula ##STR2## wherein R.sub.4 is a hydrogen atom, an alkyl group having 1-6 carbon atoms, or a cation of an alkali metal, alkaline earth metal or an alkylated or non-alkylated ammonium group, andR.sub.5 and R.sub.Type: GrantFiled: November 4, 1982Date of Patent: October 29, 1985Assignee: Duphar International Research B.V.Inventors: Gerard B. Paerels, Cornelis W. Raven
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Patent number: 4536500Abstract: New aromatic derivatives having an activity antagonistic to calcium and corresponding to formula: ##STR1## in which: A represents a chain having any one of the following structures: ##STR2## Ar represents a group of structure: ##STR3## n takes the value 1 or 2 when R is different from H; m takes the value 2 or 3.Type: GrantFiled: December 21, 1982Date of Patent: August 20, 1985Assignee: Delalande S.A.Inventors: Guy R. Bourgery, Alain P. Lacour, Bernard M. Pourrias, Raphael Santamaria
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Patent number: 4500341Abstract: Phenoxycarboxylic acid amide compound of the formula ##STR1## wherein R.sup.1 and R.sup.2 are individually selected from hydrogen and methyl,R.sup.3 is hydrogen or alkyl with from 1 to 5 carbon atomsR.sup.4 is optionally substituted alkoxycarbonylalkyl, aminocarbonylalkyl or dialkylaminocarbonylalkyl, phenyl, or substituted phenyl wherein the substituent is at least one of the group consisting of alkyl, alkoxy or alkylthio of from 1 to 4 carbon atoms, carbalkoxy of from 2 to 4 carbon atoms, halogen, and nitro; orR.sup.3 and R.sup.Type: GrantFiled: October 21, 1981Date of Patent: February 19, 1985Assignee: Bayer AktiengesellschaftInventors: Heinz Forster, Ludwig Eue, Robert R. Schmidt
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Patent number: 4495350Abstract: Herbicidally effective aminoalkyl esters of 2-nitro-5-(o-chloro-p-trifluoromethylphenoxy)-benzoic acid, and acid addition salts and quaternary ammonium salts thereof, are suitable for the selective control of weeds in crops of useful plants, for example soya bean and rice crops.The aminoalkyl esters correspond to the formula ##STR1## wherein A is a C.sub.2 -C.sub.4 -alkylene bridge or the direct bond, and ##STR2## is an open amino group, and ##STR3## is a cyclic amino group.Type: GrantFiled: September 13, 1982Date of Patent: January 22, 1985Assignee: Ciba-Geigy CorporationInventors: Dieter Durr, Otto Rohr, Beat Bohner
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Patent number: 4482549Abstract: Compounds are described of the formula ##STR1## in which --COR.sup.1 is a complex ester or thioester group,W is alkylene,X is cis or trans --CH.dbd.CH or --CH.sub.2 CH.sub.2 --,n is 1 or 2,Y is a saturated heterocyclic amino group having 5-8 ring members, andR.sup.2 is unsubstituted or substituted phenylalkyl, thienzlalkyl, naphthylalkyl or cinnamyl, and their salts and solvates.These compounds inhibit blood platelet aggregation and bronchoconstriction and may be formulated for use as antithrombotic and antiasthmatic agents.Type: GrantFiled: February 8, 1984Date of Patent: November 13, 1984Assignee: Glaxo Group LimitedInventors: Eric W. Collington, Peter Hallett, Christopher J. Wallis, Norman F. Hayes, John Bradshaw, Malcolm Carter, Alan Wadsworth
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Patent number: 4438112Abstract: Prostanoids are described of the formulae ##STR1## (and the salts thereof) in which: X is cis or trans --CH.dbd.CH-- or CH.sub.2 CH.sub.2 --;R.sup.1 is C.sub.1-7 alkyl terminated by --COOR.sup.10 where R.sup.10 is H, C.sub.1-6 alkyl or aralkyl;Y is a saturated heterocyclic amino group; andR.sup.4 is aralkyl (in which the aryl portion is substituted by alkylthio, alkylsulphinyl, alkylsulphonyl, alkanoylamino, aroylamino, phenalkyl, aminosulphonyl, alkanoylaminosulphonyl, phenylsulphonyl, nitro, tetrazolyl, substituted phenyl or thienyl).These compounds inhibit blood platelet aggregation and have bronchodilatory action, and may be formulated for use as anti-asthmatics and antithrombotic agents.Type: GrantFiled: September 17, 1982Date of Patent: March 20, 1984Assignee: Glaxo Group LimitedInventors: Eric W. Collington, Peter Hallett, Christopher J. Wallis, John Bradshaw
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Patent number: 4410521Abstract: Compounds are described of the formula ##STR1## in which --COR.sup.1 is a complex ester or thioester group,W is alkylene,X is cis or trans --CH.dbd.CH or --CH.sub.2 CH.sub.2 --,n is 1 or 2,Y is a saturated heterocyclic amino group having 5-8 ring members, andR.sup.2 is unsubstituted or substituted phenylalkyl, thienylalkyl, naphthylalkyl or cinnamyl,and their salts and solvates.These compounds inhibit blood platelet aggregation and bronchoconstruction and may be formulated for use as antithrombotic and antiasthmatic agents.Type: GrantFiled: September 16, 1982Date of Patent: October 18, 1983Assignee: Glaxo Group LimitedInventors: Eric W. Collington, Peter Hallett, Christopher J. Wallis, Norman F. Hayes, John Bradshaw, Malcolm Carter
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Patent number: 4410697Abstract: The invention relates to a new method for the preparation of N-aryl-N'-(mono- or disubstituted)-urea derivatives having the general formula (I), ##STR1## wherein Aryl is an optionally substituted phenyl group, andR.sup.1 and R.sup.2 each stand for an optionally substituted alkyl, cycloalkyl, alkoxy or phenyl group, orR.sup.1 and R.sup.2 may form, together with the adjacent nitrogen atom, a nitrogen-containing heterocyclic group which may contain a further hetero atom, orone of R.sup.1 and R.sup.2 may also stand for hydrogen,with the proviso that if one of R.sup.1 and R.sup.2 is an optionally substituted phenyl group, the other may represent only hydrogen atom or an optionally substituted alkyl or alkoxy group,by reacting a carbamate of the general formula (II) with an amine of the general formula (III),R.sup.1 R.sup.2 N--CO--X (II)Aryl--NH.sub.2 (III)or a carbamate of the general formula (IV) with an amine of the general formula (V),Aryl--NH--CO--X (IV)R.sup.1 R.sup.2 NH (V)wherein R.sup.1, R.sup.Type: GrantFiled: August 28, 1981Date of Patent: October 18, 1983Assignee: Reanal FinomvegyszergyarInventors: Sandor Torok, Lajos Voroshazy, Peter Galambos, Ivan Daroczi, Zoltan Ormenyi
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Patent number: 4389236Abstract: The invention relates to 3-phenoxymethylene-anilines of the formula ##STR1## wherein R is a ##STR2## radical or C.sub.1 -C.sub.4 alkoxy, R is halogen or C.sub.1 -C.sub.2 haloalkyl,R.sub.2, R.sub.3 and R.sub.4, each independently of the other, are hydrogen or halogenR.sub.5 is hydrogen or C.sub.1 -C.sub.4 alkylR.sub.6 is hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.2 -C.sub.4 alkenyl or C.sub.2 -C.sub.4 alkynyl, andR.sub.7 is hydrogen or C.sub.1 -C.sub.4 alkyl, while R.sub.5 and R.sub.6, or R.sub.6 and R.sub.7, together with the nitrogen atom to which they are attached, can form a heterocyclic ring system which may be interrupted by further hetero-atoms.Where R is a --NR.sub.6 R.sub.7 radical, the salts with acids also fall within the scope of formula I. These compounds have excellent selective herbicidal properties.Type: GrantFiled: August 3, 1981Date of Patent: June 21, 1983Assignee: Ciba-Geigy CorporationInventor: Dieter Durr
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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: 4328226Abstract: The present invention relates to the compounds having the following general formula (1) ##STR1## where: X is a halogen atomQ is a formyl or nitrile (cyano) groupY is a hydroxyl, alkoxyl, alkyl or nitro group"m" is the number of Y substituents 0 or 1"n" equals 1-20U and T are methyl radicals or hydrogen atoms acting strongly towards pathogenic fungi, especially of the Alternaria and Botrytis genera.Type: GrantFiled: April 3, 1980Date of Patent: May 4, 1982Assignee: Instytut Przemyslu Organicznego & Politechnika WroclawskaInventors: Stanislaw Witek, Damian Grobelny, Jadwiga Gorska-Poczopko, Edmund Bakuniak, Irena Bakuniak, Janina Ptaszkowska
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Patent number: 4289770Abstract: New derivatives of 2-benzoyl-4-nitro anilides, their preparation and their use as medicaments.The new chemical derivatives of the invention have the general formula ##STR1## in which R represents a linear or branched alkyl group, an alkenyl group, a cycloalkyl group or a benzyl group,R.sub.1 represents a hydrogen atom, an alkyl group or a hydroxy alkyl group,R.sub.2 represents a hydroxy-alkyl, alkenyl or alkynyl group, possibly substituted one or more times by an alkyl radical, or a cycloalkyl group having three to six carbon atoms;R.sub.1 and R.sub.2 may furthermore form, with the nitrogen atom to which they are attached, a nitrogen heterocycle containing possibly a second heteroatom selected from among oxygen and nitrogen;under the condition, however, that when R.sub.2 represents a hydroxy-alkyl group R.sub.1 may not be a hydrogen atom.Use as hypnotic agents for the treatment of insomnia.Type: GrantFiled: June 13, 1980Date of Patent: September 15, 1981Assignee: Pierre Fabre S.A.Inventors: Henri Cousse, Gilbert Mouzin
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Patent number: 4283399Abstract: A parasiticide containing as an active ingredient the compound with the general formula 1, where:X is a halogen atom,Y is a hydroxyl, alkoxyl, alkyl or nitro group and "n" is the number of Y substituents and equals 0-4,R.sup.1 is an alkyl radical with 1-3 carbon atoms or hydrogen atom,R.sup.2 and R.sup.3 are alkyl or hydroxyalkyl radicals with 1-4 carbon atoms,R.sup.4 is an alkyl radical with 1-18 carbon atomsorR.sup.2 and R.sup.3 together with the nitrogen atom form a ring substituted as in formula 2, where:W is a methylene group or an oxygen atom,U and T are methyl radicals or hydrogen atoms,Z is a hydrogen atomorT and Z together are an oxygen atom.The agent containing an active compound with the general formula 1, where the substituents have the above meaning has strong fungicidal activity towards pathogenic fungi and bacteria, among which are fungi from the Alternaria genus.Type: GrantFiled: May 25, 1979Date of Patent: August 11, 1981Inventors: Stanislaw Witek, Damian Grobelny, Janina Ptaszkowska, Andrzej Bielecki, Edmund Bakuniak, Stefan Fulde, Jadwiga Gorska-Poczopko
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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: 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: 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: 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: 4210754Abstract: Benzamides of the formula ##STR1## wherein X is halogen, trifluoromethyl or C.sub.3-4 -alkyl and Y is hydrogen, halogen or nitro,and N-oxides thereof, prepared inter alia from N-(2-aminoethyl)-morpholine and an acid of the formula ##STR2## wherein X and Y are as hereinbefore set forth, are described. The end products are useful in the treatment of depressive conditions, that is, are useful as antidepressants.Type: GrantFiled: October 20, 1978Date of Patent: July 1, 1980Assignee: Hoffmann-La Roche Inc.Inventors: Willy Burkard, Pierre-Charles Wyss
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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: 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: 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: 4093446Abstract: Compounds of the formula ##STR1## wherein X is a hydrogen atom, a halogen atom, a trihalomethyl group, an alkyl group, or a cyano group,Y is a hydrogen atom, a halogen atom, or a trihalomethyl group, andZ is a substituted alkoxy group,And compositions containing these compounds exhibit herbicidal activity.Type: GrantFiled: August 31, 1976Date of Patent: June 6, 1978Assignee: Rohm and Haas CompanyInventors: Horst O. Bayer, Colin Swithenbank, Roy Y. Yih
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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: 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: 4060609Abstract: Biphenylyl ethers of the formula R--O--CH.sub.2 --CR.sub.1 (OH)--CH.sub.2 Z wherein R.sub.1 is H or CH.sub.3 ; Z is dialkylamino of 2-8 carbon atoms, morpholino, pyrrolidino, piperidino, homopiperidino, hydroxypyrrolidino, hydroxypiperidino or hydroxyhomopiperidino; R is either biphenylyl substituted by at least one of F, Cl, Br, I, CF.sub.3, NO.sub.2 and piperidino or, when R.sub.1 is CH.sub.3 or when Z is homopiperidino, hydroxypyrrolidino, hydroxypiperidino or hydroxyhomopiperidino, unsubstituted biphenyl, and the physiologically acceptable acid addition salts thereof, possess cholesterol blood-level-lowering activity and can be produced by reacting a compound of the formula R--O--CH.sub.2 --Y wherein Y is ##STR1## or --CR.sub.1 (OH)--CH.sub.2 X, X being Cl, Br, I or a free or functionally modified OH-group, with an amine of the formula H-Z.Type: GrantFiled: October 29, 1974Date of Patent: November 29, 1977Assignee: Merch Patent Gesellschaft mit beschrankter HaftungInventors: Erich Schacht, Werner Mehrhof, Rochus Jonas, Herbert Nowak, Zdenek Simane
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Patent number: 4046776Abstract: Lactone compounds of the formula ##STR1## wherein X represents alkyl with 1 to 12 carbon atoms, alkoxy with 1 to 12 carbon atoms or acyloxy with 2 to 12 carbon atoms,Y represents an optionally substituted 2-pyrrolyl, 3-indolyl or 3-carbazolyl radical,The nitrogen ring A represents a heterocyclic radical which optionally includes a further hetero atom as a ring member and the ring B represents a 6-membered aromatic or heterocyclic ring which may have an aromatic condensed ring and both the ring B and the condensed ring may be substituted. These lactone compounds are particularly useful as color formers which give intense green-blue, blue or violet-blue colors when they are brought into contact with an electron-accepting co-reactant.Type: GrantFiled: April 2, 1975Date of Patent: September 6, 1977Assignee: Ciba-Geigy CorporationInventors: Robert Garner, Jean-Claude Petitpierre
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Patent number: 4046798Abstract: Compounds of the formula ##STR1## wherein X is a hydrogen atom, a halogen atom, a trihalomethyl group, an alkyl group, or a cyano group,Y is a hydrogen atom, a halogen atom, or a trihalomethyl group, andZ is a hydroxy group, an alkoxy group, and alkyl group, a halogen atom, an amino group, an alkylthio group, a cyano group, a carboxy group, a carbalkoxy group, a carboxyalkyl group, a carbalkoxyalkyl group, an alkanoyloxy group, or a carbamoyloxy group,And compositions containing these compounds exhibit herbicidal activity.Type: GrantFiled: September 29, 1975Date of Patent: September 6, 1977Assignee: Rohm and Haas CompanyInventors: Horst O. Bayer, Colin Swithenbank, Roy Y. Yih
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Patent number: RE31237Abstract: New derivatives of 2-benzoyl-4-nitro anilides, their preparation and their use as medicaments.The new chemical derivatives of the invention have the general formula ##STR1## in which R represents a linear or branched alkyl group, an alkenyl group, a cycloalkyl group or a benzyl group,R.sub.1 represents a hydrogen atom, an alkyl group or a hydroxy alkyl group,R.sub.2 represents a hydroxy-alkyl, alkenyl or alkynyl group, possibly substituted one or more times by an alkyl radical, or a cycloalkyl group having three to six carbon atoms;R.sub.1 and R.sub.2 may furthermore form, with the nitrogen atom to which they are attached, a nitrogen heterocycle containing possibly a second heteroatom selected from among oxygen and nitrogen;under the condition, however, that when R.sub.2 represents a hydroxy-alkyl group R.sub.1 may not be a hydrogen atom.Use as hypnotic agents for the treatment of insomnia.Type: GrantFiled: February 19, 1982Date of Patent: May 10, 1983Assignee: Pierre Fabre S.A.Inventors: Henri Cousse, Gilbert Mouzin
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Patent number: RE31731Abstract: Compounds of the formula ##STR1## wherein X is a hydrogen atom, a halogen atom, a trihalomethyl group, an alkyl group, or a cyano group,Y is a hydrogen atom, or a trihalomethyl group, andZ is an alkoxy group, an alkoxyalkoxy group, a hydroxyalkoxy group, an alkyl group, a halogen atom, an alkylamino group, a dialkylamino group, an alkylthio group, a carboxy group, a carbalkoxy group, a carboxyalkoxy group, a carbalkoxyalkoxy group, a carboxyalkyl group, a carbalkoxyalkyl group, a dialkylureido group, an alkanoylamino group, or carbalkoxyamino group,and compositions containing these compounds exhibit herbicidal activity.Type: GrantFiled: September 1, 1978Date of Patent: November 13, 1984Inventors: Horst O. Bayer, Colin Swithenbank, Roy Y. Yih