Patents Represented by Attorney John J. Maitner
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Patent number: 4209516Abstract: The present invention relates to new triazole derivatives of the formula ##STR1## wherein R.sub.1 represents hydrogen, lower alkyl, optionally esterified or etherified hydroxymethyl, formyl, optionally functionally modified carboxy, or optionally mono- or disubstituted aminomethyl,R.sub.2 represents lower alkyl, and R.sub.3 represents hydrogen or lower alkyl, whereby R.sub.2 and R.sub.3 as lower alkyl can be bound directly, or in .beta.- or .gamma.-position also by way of oxygen, sulphur or the imino radical or a lower alkylimino radical, and the rings A and B independently of each other can be unsubstituted or substituted, and to their addition salts with inorganic and organic acids, in particular the pharmaceutically acceptable acid addition salts. These new compounds possess valuable pharmacological properties. In particular they have an anti-convulsive activity and are useful for the treatment of epilepsy and of conditions of tension and of agitation.Type: GrantFiled: August 31, 1978Date of Patent: June 24, 1980Assignee: Ciba-Geigy CorporationInventors: Roland Heckendorn, Rene Meier
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Patent number: 4209515Abstract: The present invention relates to new triazole derivatives of the formula ##STR1## wherein R.sub.1 represents hydrogen, lower alkyl, optionally esterified or etherified hydroxymethyl, formyl, optionally functionally modified carboxy, or optionally mono- or disubstituted aminomethyl, R.sub.2 represents lower alkyl, and R.sub.3 represents hydrogen or lower alkyl, whereby R.sub.2 and R.sub.3 as lower alkyl can be bound directly, or in .beta.- or .gamma.-position also by way of oxygen, sulphur or the imino radical or a lower alkylimino radical, and the rings A and B independently of each other can be unsubstituted or substituted, and to their addition salts with inorganic and organic acids, in particular the pharmaceutically acceptable acid addition salts. These new compounds possess valuable pharmacological properties. In particular they have an anticonvulsive activity and are useful for the treatment of epilepsy and of conditions of tension and of agitation.Type: GrantFiled: September 13, 1978Date of Patent: June 24, 1980Assignee: Ciba-Geigy CorporationInventors: Roland Heckendorn, Rene Meier
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Patent number: 4206152Abstract: The present invention provides a process for the production of unsubstituted or substituted o-phthalaldehydes by hydrolysis of .alpha.,.alpha., .alpha.',.alpha.'-tetrahalogeno-o-xylenes with a carboxylate in an aqueous medium in the presence of a phase transfer catalyst and an organic base.Type: GrantFiled: December 21, 1978Date of Patent: June 3, 1980Assignee: Ciba-Geigy CorporationInventor: Jacques Gosteli
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Patent number: 4205082Abstract: New benzopyrane derivatives of the general formula ##STR1## in which R is free, esterified or amidated carboxyl, Ph is 1,2-phenylene which contains the group R--CO--NR.sub.3 -- and is otherwise unsubstituted or is substituted, X is a group of the formula --CO--CR.sub.1 .dbd.CR.sub.2 --, in which R.sub.1 and R.sub.2 independently of one another are hydrogen, acyl or a substituted or unsubstituted hydrocarbon radical or a hetero-analogue thereof, or conjointly are 3-membered to 5-membered lower alkylene, and R.sub.2 can also be free or etherified hydroxyl or hydroxyl etherified by an organic carboxylic acid, and R.sub.3 is hydrogen or lower alkyl, are useful as anti-allergic agents.Type: GrantFiled: August 19, 1977Date of Patent: May 27, 1980Assignee: Ciba-Geigy CorporationInventor: Pier G. Ferrini
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Patent number: 4202900Abstract: 6-Acylamino-penam-3-carboxylic acids and 7-acylamino-3-cephem-4-carboxylic acids in which the acyl group has the formula ##STR1## in which R.sub.1 is hydrogen, R.sub.2 is optionally substituted phenyl, thienyl or furyl or R.sub.1 and R.sub.2 together are optionally substituted cycloalkyl, n and m independently of one another represent 0 or 1 and B represents an optionally substituted 2,6-dioxo- or 2,6-dithioxo-1,2,3,6-tetrahydro-pyrimidyl, 2-thioxo-6-oxo-1,2,3,6-tetrahydropyrimidyl, 2,6-dihydroxy- or 2,6-dimercapto-pyrimidyl, 2-mercapto-6-hydroxy-pyrimidyl, 2,6-diaminopyrimidyl, 2-amino-6-hydroxy-pyrimidyl or 2,6-dihalogenopyrimidyl radical, these radicals being bonded in the 4- or 5-position.Type: GrantFiled: April 28, 1978Date of Patent: May 13, 1980Assignee: Ciba-Geigy CorporationInventors: Karoly Kocsis, Bruno Fechtig, Hans Bickel
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Patent number: 4195090Abstract: Heterocyclic compounds of the formula ##STR1## wherein Het denotes optionally substituted pyridazinyl, pyrimidinyl, pyrazinyl or substituted pyridyl, R.sub.1 is hydrogen or methyl and R.sub.2 is lower alkyl, optionally substituted phenyl-lower alkyl, carboxy-lower alkyl or functionally modified carboxy-lower alkyl, their condensation products with aldehydes, ketones or carbonic acid and their N-oxides, which are valuable (cardioselective) .beta.-rezeptor blocking agents, and/or (cardioselective) .beta.-rezeptor-stimulants.Type: GrantFiled: March 3, 1978Date of Patent: March 25, 1980Assignee: Ciba-Geigy CorporationInventors: Jurg Frei, Knut A. Jaeggi, Franz Ostermayer, Herbert Schroter
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Patent number: 4192868Abstract: The invention relates to processes for the preparation of novel aryl-hexafuranosides of the formula ##STR1## in which R.sub.1 is lower alkyl or cycloalkyl and R.sub.2 is hydrogen, lower alkyl or acyl, or R.sub.1 and R.sub.2 together are alkylidene or cycloalkylidene, R.sub.3 is hydrogen, lower alkyl, lower alkenyl or aryl-lower alkyl, R.sub.5a and R.sub.6a independently of one another are hydrogen or lower alkyl, R.sub.5b and R.sub.6b independently of one another are hydrogen, hydroxyl, lower alkoxy or amino, or R.sub.5b and R.sub.6b together are a C--C bond, epoxy or lower alkylidene, and R.sub.6c is aryl, by methods known per se.These novel compounds have an anti-inflammatory and/or antinociceptive action.Type: GrantFiled: February 22, 1978Date of Patent: March 11, 1980Assignee: Ciba-Geigy CorporationInventors: Jean M. J. Tronchet, Bruno Baehler, Alberto Rossi, Gerhard Baschang, Alex Sele
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Patent number: 4188396Abstract: New 4-(phenyl)-piperidine compounds of the general formula I ##STR1## in which R.sub.1 represents hydrogen or lower alkyl, Ph represents a p-phenylene group optionally substituted by lower alkyl, lower alkoxy, nitro and/or halogen, and R.sub.2 represents lower alkyl, and pharmaceutically acceptable acid addition salts thereof are useful as antidepressant agents.Type: GrantFiled: January 6, 1978Date of Patent: February 12, 1980Assignee: Ciba-Geigy CorporationInventors: Georges Haas, Alberto Rossi, Pier G. Ferrini, Oswald Schier
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Patent number: 4185110Abstract: Novel benzoheterocyclylglyoxylic acid derivatives of the formula ##STR1## in which Z is free, etherified or acylated hydroxyl, X is thio or oxy, R is free or etherified hydroxyl, R.sub.1 is lower alkyl, cycloalkyl, hydroxyl, lower alkoxy, substituted or unsubstituted phenoxy, substituted or unsubstituted amino, acyl, carboxyl, halogen, nitro or, if Z is acylated hydroxyl and/or X is oxy, hydrogen, R.sub.2 is hydrogen, lower alkyl, hydroxyl or halogen and R.sub.3 and R.sub.4 are each hydrogen or lower alkyl, or in which two adjacent radicals R.sub.1, R.sub.2, R.sub.3 and R.sub.4 together form lower alkylene having 3 to 5 chain carbon atoms or 1,4-butadienylene and the other two radicals are each hydrogen, and their pharmaceutically acceptable salts are useful as anti-allergic agents.Type: GrantFiled: February 9, 1978Date of Patent: January 22, 1980Assignee: Ciba-Geigy CorporationInventors: Kurt Eichenberger, Hans Bosshard, Niklaus Buhler, Richard Goschke, Knut A. Jaeggi
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Patent number: 4178378Abstract: Etherified diazepine derivatives of the formula ##STR1## in which R.sub.1 represents hydrogen or alkyl having up to 3 carbon atoms, R.sub.2 and R.sub.3 independently of one another each represent hydrogen or alkyl having up to 7 carbon atoms, or represent the partial formula R.sub.4 --(OCH.sub.2 --CH.sub.2).sub.m, in which R.sub.4 represents hydrogen or alkyl having up to 7 carbon atoms and m represents the number 1 to 3, A.sub.1 represents alkylidene or alkylene having up to 3 carbon atoms, A.sub.2, depending on the meaning of n, represents alkylene or alkanetriyl having up to 5 carbon atoms, no carbon atom in the radical A.sub.2 being bonded to more than one oxygen atom, n represents the number 0 or 1, Ph represents substituted or unsubstituted 1,2-phenylene and Ar represents an aromatic radical, and their addition salts are manufactured according to methods known per se. They are useful in the treatment of states of epilepsy, stress and agitation.Type: GrantFiled: September 15, 1977Date of Patent: December 11, 1979Assignee: Ciba-Geigy CorporationInventors: Hans Allgeier, Andre Gagneux
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Patent number: 4177344Abstract: The invention relates to novel 1,6-anhydro-.beta.-D-hexopyranose derivatives of the formula I ##STR1## in which R.sub.2 is hydrogen, methyl or aromatic acyl, R.sub.3 and R.sub.4 are alkyl, alkenyl or aralkyl and one of the radicals R.sub.3 and R.sub.4 is also an aroyl radical and R.sub.4 can also be hydrogen, with the proviso that the radicals R.sub.3 and R.sub.4 together contain at least 3 carbon atoms and, if R.sub.4 is the benzyl radical, the radical R.sub.3 contains at least 2 carbon atoms, and, if one of the radicals R.sub.3 and R.sub.4 is an aroyl radical, R.sub.2 is hydrogen.These compounds especially the 1,6-anhydro-3,4-di-O-benzyl-.beta.-D-glucopyranose or the 1,6-anhydro-.beta.-D-glucopyranose, can be used as fibrinolytic agents and thrombolytic agents.Type: GrantFiled: September 16, 1977Date of Patent: December 4, 1979Assignee: Ciba-Geigy CorporationInventors: Gerhard Baschang, Jaroslav Stanek, Alberto Rossi, Alex Sele
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Patent number: 4172832Abstract: The invention concerns 3-amino-4-(2-hydroxyethylthio)-2-oxo-azetidine compounds of the formula ##STR1## wherein R.sub.1.sup.a represents hydrogen or an amino protective group R.sub.1.sup.A, R.sub.1.sup.b represents hydrogen or an acyl group Ac.sub.1, or R.sub.1.sup.a and R.sub.1.sup.b together denote a bivalent amino protective group, R.sub.2 represents hydrogen or an acyl radical Ac.sub.2, and each of the radicals R.sub.3 and R.sub.4 represents hydrogen or an organic radical bonded via a carbon atom, or salts of such compounds having salt-forming groups.Type: GrantFiled: December 11, 1973Date of Patent: October 30, 1979Assignee: Ciba-Geigy CorporationInventors: Riccardo Scartazzini, Hans Bickel, Karl Heusler
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Patent number: 4171366Abstract: The present invention provides imidazole derivatives of the formula I ##STR1## wherein Het represents 1H-imidazol-1-yl which is unsubstituted or is substituted by lower alkyl,One of the symbols X and Y represents the epithio radical -S- or the ethenylene group --CH.dbd.CH--, and the other represents the direct bond, andN represents 1 to 4,And the rings A and B, besides being substituted by the radical -C.sub.n H.sub.2n -Het, are not substituted or are further substituted, and the ring C is unsubstituted or substituted, and the monoacid acid addition salts, in particular the pharmaceutically acceptable monoacid acid addition salts thereof.These new substances possess valuable pharmacological properties, in particular antidepressant activity, and can be used for the treatment of mental depressions. Specific embodiments are 1-[(naphtho[1,2-b]thien-4-yl)-methyl]-1H-imidazole and its pharmaceutically acceptable monoacid acid addition salts, and pharmaceutical compositions containing them.Type: GrantFiled: November 25, 1977Date of Patent: October 16, 1979Assignee: Ciba-Geigy CorporationInventors: Hans Blattner, Angelo Storni
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Patent number: 4161476Abstract: .alpha.-Hydroxy-2-oxo-1-azetidinemethane-carboxylic acid compounds of formula ##STR1## wherein R.sub.1 represents a hydrogen atom or the organic residue of an alcohol, R.sub.2 represents a hydrogen atom or an acyl residue, R.sub.3 represents an organic residue and R.sub.4 represents a hydrogen atom, when R.sub.2 stands for an acyl residue, or the two groups R.sub.3 and R.sub.4 together represent a disubstituted carbon atom, when R.sub.2 stands for a hydrogen atom or an acyl group, are useful as intermediates for the manufacture of pharmacologically active compounds.Type: GrantFiled: July 11, 1977Date of Patent: July 17, 1979Assignee: Ciba-Geigy CorporationInventors: Karl Heusler, Robert B. Woodward
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Patent number: 4161530Abstract: Pharmaceutical Combination Preparations useful as hypnotics which contain as pharmacological active compounds a beta-receptor-blocking compound and L-tryptophane or a non-toxic salt thereof.Type: GrantFiled: March 17, 1978Date of Patent: July 17, 1979Assignee: Ciba-Geigy CorporationInventor: Werner P. Koella
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Patent number: 4160837Abstract: The present invention provides new derivatives of perhydro-aza-heterocycles of the formula ##STR1## in which X is the oxo radical or hydrogen and the radical OR.sub.1, in which R.sub.1 is hydrogen or a substituted or unsubstituted aliphatic hydrocarbon radical, a substituted or unsubstituted araliphatic hydrocarbon radical or a substituted or unsubstituted aromatic hydrocarbon radical or an acyl radical, R.sub.2 is hydrogen or a substituted or unsubstituted aliphatic hydrocarbon radical, Y is oxygen or sulphur, n.sub.1 and n.sub.2 each are values of 1 to 3, n.sub.1 +n.sub.2 being at most four, and Ar is a substituted or unsubstituted aromatic hydrocarbon radical, and the acid addition salts, in particular the pharmaceutically acceptable acid addition salts thereof. These new substances possess valuable pharmacological properties, in particular antidepressant activity, and can be used for the treatment of mental depressions.Type: GrantFiled: August 24, 1977Date of Patent: July 10, 1979Assignee: Ciba-Geigy CorporationInventor: Romeo Paioni
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Patent number: 4159981Abstract: The new hypocalcaemically active peptides of formula I ##STR1## and corresponding compounds in which one or more of the asparagine and glutamic acid radicals are replaced by the aspartic acid or glutamic acid radical and/or the aspartic acid radical is replaced by the asparagine radical, their dimers, especially those in which 2 identical peptide sequences (1-32 and 1'-32') are joined in an anti-parallel arrangement via the cysteine radicals 1,7' and 7,1' by means of a disulfide bond, and derivatives are useful as hypocalcaemic agents and are prepared by splitting off groups protecting at least one amino or one carboxyl group or oxidizing the corresponding sulfides to the disulfides or condensing together adequate peptides.Type: GrantFiled: October 4, 1977Date of Patent: July 3, 1979Assignee: Ciba-Geigy CorporationInventors: Werner Rittel, Max Brugger, Bruno Kamber, Bernhard Riniker, Peter Sieber, Hendrik M. Greven
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Patent number: 4154831Abstract: Compounds of the formula ##STR1## wherein R.sub.1 denotes optionally substituted phenyl, thienyl, furyl or 1,4-cyclohexadienyl, R.sub.2 represents a free carboxyl group or an esterified carboxyl group which can be split physiologically, R.sub.3 represents hydrogen, lower alkoxy or an optionally substituted methyl group and B represents an optionally substituted six-membered ring with 1 to 3 ring nitrogen atoms, which is bonded to the carbonyl group --C(.dbd.O)-- by one of its carbon atoms, the nitrogen atoms of a monocyclic six-membered ring having 2 nitrogen atoms being either adjacent or separated by two ring carbon atoms, and the salts of such compounds which have a salt-forming group, including the inner salts, for example the 7.beta.-[D(-)-.alpha.-(3,5-Dioxo-2,3,4,5-tetrahydro-1,2,4-triazine-6-c arboxamido)-phenylacetamido]-cephalosporanic acid, have antibiotic activity.Type: GrantFiled: April 20, 1977Date of Patent: May 15, 1979Assignee: Ciba-Geigy CorporationInventors: Karoly Kocsis, Heinrich Peter, Hans Bickel
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Patent number: 4152444Abstract: The invention is directed to pharmaceutical and veterinary preparations having antibacterial action characterized by the contents of the following two bactericidally active substances(1) a rifamycin compound(2) a nitrofuran compoundThey show a synergistic enhancement of the bactericidal action as compared with the single antibactericidal components when given alone and they also suppress or prevent the development of resistance towards these antibiotics or antibacterial agents, especially towards rifampicin. Preferred ratios of the quantities of (1) and (2) contained in these preparations are 6:1 and 2:1. An especially suitable combination is rifampicin and nitrofurantoin. Other examples are the combination of 3-amino-rifamycin SV derivaties with known nitrofuran derivatives, such as nitrofurantoin, furzolidone or furaltadone.Type: GrantFiled: August 29, 1977Date of Patent: May 1, 1979Assignee: Ciba-Geigy CorporationInventors: Wolfgang Vischer, Friedrich Kradolfer
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Patent number: 4147780Abstract: The present invention relates to new phosphonous acid derivatives, especially to .alpha.-amino-phosphonous acids and processes for their production. The new phosphonous acids are valuable chemotherapeutica in the treatment of pathogenic bacteria, gram-negative bacteria and yeast.Type: GrantFiled: May 23, 1977Date of Patent: April 3, 1979Assignee: Ciba-Geigy CorporationInventors: John G. Dingwall, Eric K. Baylis, Colin D. Campbell