Patents Represented by Attorney, Agent or Law Firm Irving M. Fishman
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Patent number: 5204342Abstract: Novel hydrogenated heterocyclic compounds, containing two nitrogen atoms, of the formula ##STR1## in which R.sub.1, R.sub.2, R.sub.3, R.sub.5 and Rhd 7 are each, independently of the others, hydrogen or lower alkyl, m is 2 or 3, n is 1 or 2, and either R.sub.4 and R.sub.6 are each hydrogen or R.sub.4 and R.sub.6 together form an additional bond, in free form or in form of a salt, can be used as pharmaceutical active ingredients and can be manufactured in a manner known per se.Type: GrantFiled: March 31, 1992Date of Patent: April 20, 1993Assignee: Ciba-Geigy CorporationInventors: Wolfgang Frostl, Cesare Mondadori, Dietrich Strub, Armin Zust
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Patent number: 5190947Abstract: The invention relates to the codeine salt of [2-[(2,6-dichlorophenyl)-amino]-phenyl]-acetic acid of formula ##STR1## to processes for the preparation thereof, to pharmaceutical compositions comprising that salt, and to its use as an analgesic drug.Compositions comprising the salt of formula I are used especially in the case of severe painful conditions.Type: GrantFiled: August 16, 1991Date of Patent: March 2, 1993Assignee: Ciba-Geigy CorporationInventors: Walter Riess, Alfred Sallmann
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Patent number: 5190930Abstract: Araliphatylaminoalkanediphosphonic acids of formula ##STR1## wherein R.sub.1 is an aromatically substituted aliphatic radical, R.sub.2 is hydrogen or a monovalent aliphatic radical and alk is a divalent aliphatic radical, and their salts, exhibit a pronounced regulatory action on the calcium metabolism and can be used as medicaments for the treatment of diseases that are attributable to calcium metabolsim disorders. They are prepared, for example, by reacting a compound of formula ##STR2## wherein X.sub.3 is carboxy and R.sub.0 is a radical R.sub.2, with phosphorous acid and phosphorus trichloride and hydrolysing the primary product.Type: GrantFiled: December 20, 1991Date of Patent: March 2, 1993Assignee: Ciba-Geigy CorporationInventor: Knut A. Jaeggi
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Patent number: 5190934Abstract: Compounds of the formula I ##STR1## wherein either R.sub.1 is halogen, R.sub.1 ' is halogen or hydrogen and R.sub.2 and R.sub.2 ' denote hydrogen or R.sub.1 and R.sub.1 ' represent hydrogen, R.sub.2 is an aliphatic or aromatic radical and R.sub.2 ' is hydroxy or R.sub.2 and R.sub.2 ' together represent oxo, and wherein R denotes an aliphatic, cycloaliphatic, cycloaliphatic-aliphatic or araliphatic radical having 2 or more carbon atoms or, if R.sub.1 and R.sub.1 ' denote hydrogen, R.sub.2 represents an aromatic radical and R.sub.2 ' is hydroxy, R represents methyl, and their salts are useful as nootropics, antidepressants and/or anxiolytics. The can be manufacture by replacing any group R.sub.5 by hydrogen and/or converting any group Z.sub.0 into amino in a compound of formula II ##STR2## in which R, R.sub.1, R.sub.1 ', R.sub.2 and R.sub.2 ' have their previous significances, Z represents a protected or latent amino group Z.sub.0 and R.sub.4 denotes hydrogen or a hyddroxy-protective group R.sub.Type: GrantFiled: March 3, 1992Date of Patent: March 2, 1993Assignee: Ciba-Geigy CorporationInventors: Stuart J. Mickel, Georg von Sprecher
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Patent number: 5190933Abstract: Compounds of the formula I ##STR1## wherein R denotes an aliphatic, cycloaliphatic, cycloaliphatic-aliphatic or araliphatic radical having 2 or more carbon atoms, and wherein one of the groups R.sup.1, R.sup.2 and R.sup.3 represents hydrogen or an aliphatic, cycloaliphatic, araliphatic or aromatic radical, another one of R.sup.1, R.sup.2 and R.sup.3 is hydrogen or, in the case of R.sup.1 and R.sup.2, is hydroxy, and the remaining one of R.sup.1, R.sup.2 and R.sup.3 is hydrogen, or wherein R denotes methyl, R.sub.1 denotes hydrogen or hydroxy, R.sub.2 denotes an aromatic radical and R.sub.3 represents hydrogen, and their salts have GABA.sub.B -antagonistic properties and can be used as GABA.sub.B -antagonists. They are obtained when in a compound of formula II ##STR2## in which R, R.sup.1, R.sup.2 and R.sup.3 have their previous significances, Z represents --NH.sub.2 and R.sup.4 denotes a hydroxy-protective group R.sup.5 or, when R.sup.1 and R.sup.3 denote hydrogen and R.sup.Type: GrantFiled: March 3, 1992Date of Patent: March 2, 1993Assignee: Ciba-Geigy CorporationInventors: Eric K. Baylis, Ludwig Maier, Stuart J. Mickel, Hans-Rudolf Olpe, Helmut Bittiger, Wolfgang Frostl, Roger G. Hall
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Patent number: 5189017Abstract: Described are the use of hexopyranose compounds of the formula I ##STR1## for the prophylaxis and treatment of virus infections, and novel pharmaceutical preparations especially suitable for the use in accordance with the invention.The substituents in formula I have the meanings given in the claims.Type: GrantFiled: October 17, 1990Date of Patent: February 23, 1993Assignee: Ciba-Geigy CorporationInventors: Bohumir Lukas, Karl H. Schmidt-Ruppin
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Patent number: 5185368Abstract: Compounds of the formula ##STR1## in which R is alkyl having up to 4 carbon atoms, n has an average value of at least 9, X is a radical of the formula --C(.dbd.O)--(NH--SO.sub.2).sub.m -- in which m is 0 or 1 and, if m is 1, the carbonyl group may be bonded to the oxygen atom or to the nitrogen atom, and each of the radicals A.sub.1, A.sub.2 and A.sub.3, independently of the others, is hydrogen or an acyl radical, and salts of salt-forming compounds of formula I, as well as metal complexes of compounds of formula I, in which A.sub.1, A.sub.2 and A.sub.3, are hydrogen can be used as metal chelators and as auxiliaries in diagnosis.Type: GrantFiled: July 20, 1988Date of Patent: February 9, 1993Assignee: Ciba-Geigy CorporationInventors: Heinrich Peter, Theophile Moerker
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Patent number: 5177070Abstract: Method of treating male erectile impotence secondary to physiological dysfunction by administering, preferably orally, the cholinergic agent galanthamine or a pharmaceutically acceptable salt thereof, most preferably the hydrobromide salt, in amounts of preferably 10-20 mg based on the hydrobromide, up to three to four times a day.Type: GrantFiled: November 15, 1991Date of Patent: January 5, 1993Assignee: Ciba-Geigy CorporationInventor: Richard Katz
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Patent number: 5177091Abstract: Compounds of formula I ##STR1## wherein X and Y are each independently of the other thio or sulfynyl, R.sub.1 is lower alk-2-en-1-yl, lower alk-3-en-2-yl, lower alk-2--yn-1-yl, or lower alkyl that is substituted in the 2,3-position by radicals that can be eliminated to form a double bond, R.sub.2 is hydrogen and R.sub.3 is unsubstituted methyl or methyl substituted by a radical that can be eliminated together with hydrogen Rhd 2 to form a double bond, or R.sub.2 and R.sub.3 are each hydrogen or lower alkyl or together are methylene, R.sub.4 is free or protected hydroxy, or hydrogen, and R.sub.5 is hydrogen, lower alkyl, lower alk-2-en-1-yl, lower alk-2-yn-1-yl, or lower alkyl that is substituted in the 2,3-position by radicals that can be eliminated to form a double bond, and their pharmaceutically acceptable salts may be used in a novel manner for the treatment of disorders of the rheumatoid type.Type: GrantFiled: November 20, 1991Date of Patent: January 5, 1993Assignee: Ciba-Geigy CorporationInventors: Ulrich Feige, Irmgard Wiesenberg, Leo Widler, Pier G. Ferrini, Martin Missbach
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Patent number: 5177257Abstract: The novel (S)-4-(2-bromobenzoyl)-5-hydroxy-benzocyclobutene-1-carboxylic i.e. the compound of the formula ##STR1## in free form or in salt form, can be used as active ingredient in pharmaceutical preparations and can be prepared by a novel process, which is characterized in that racemic 4-(2-bromobenzoyl)-5-hydroxy-benzocyclobutene-1-carboxylic acid is reacted at elevated temperature with at least the equimolar amount of quinine in an alcoholic solvent for from approximately 6 to approximately 48 hours, the quinine salt of the (S)-4-(2-bromobenzoyl)-5-hydroxy-benzocyclobutene-1-carboxylic acid, precipitated in crystalline form as the direct reaction product, is separated from the reaction mixture, and the (S)-4-(2-bromobenzoyl)-5-hydroxy-benzocyclobutene-1-carboxylic acid is set free from this salt by acid treatment in a customary manner, and, if desired, this free acid is converted into a salt.Type: GrantFiled: November 20, 1991Date of Patent: January 5, 1993Assignee: Ciba-Geigy CorporationInventors: Andreas von Sprecher, Hansjurg Wetter
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Patent number: 5175344Abstract: The invention relates to unsaturated amino acids of the formula I ##STR1## in which R.sup.1 represents hydroxy or etherified hydroxy, R.sup.2 represents hydrogen, alkyl, hydroxy or etherified hydroxy, R.sup.3 represents hydrogen, alkyl, haloalkyl, hydroxyalkyl, lower alkoxyalkyl, arylalkyl, lower alkenyl, halogen or aryl, R.sup.4 represents hydrogen, alkyl or aryl, R.sup.5 represents hydrogen or alkyl, R.sup.6 represents carboxy or esterified or amidated carboxy, R.sup.7 represents amino or amino substituted by alkyl or acyl, A represents unsubstituted or alkyl-substituted .alpha.,.omega.-alkylene having from 1 to 3 carbon atoms or represents a bond, and B represents methylene or a bond, with the proviso that A is other than a bond when B represents a bond, and salts thereof. They can be manufactured, for example, in accordance with the Michaelis-Arbuzov reaction and can be used as pharmacologically active substances.Type: GrantFiled: July 17, 1991Date of Patent: December 29, 1992Assignee: Ciba-Geigy CorporationInventors: Christof Angst, Derek E. Brundish, John G. Dingwall, Graham E. Fagg, Hans Allgeier, Guido Bold, Rudolf Duthaler, Roland Heckendorn, Antonio Togni
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Patent number: 5169867Abstract: Compounds of formula ##STR1## wherein R.sub.1 is amino or is a radical ##STR2## wherein R.sub.3 is lower alkyl, hydroxy-lower alkyl, lower alkoxy-lower alkyl, carboxy, lower alkoxycarbonyl, phenyl, phenyl substituted by lower alkyl, halo-lower alkyl, hydroxy-lower alkyl, halogen, hydroxy, lower alkoxy, lower alkanoyloxy and/or by nitro, pyridyl, pyridyl substituted by lower alkyl, hydroxy-lower alkyl, lower alkoxy-lower alkyl, phosphonooxy-lower alkyl, lower alkanoyl, carboxy, lower alkoxycarbonyl, hydroxy, lower alkoxy, lower alkanoyloxy, nitro and/or by oxido, or quinolyl, R.sub.4 is hydrogen, lower alkyl, hydroxy-lower alkyl or halo-lower alkyl, or R.sub.3 and R.sub.4 together are C.sub.4 -C.sub.6 alkylene or benzo-C.sub.4 -C.sub.6 alkylene, and R.sub.2 is straight-chain C.sub.1 -C.sub.4 alkyl, and salts thereof, have a strong specific inhibitory action on the enzyme ornithine decarboxylase. The compounds of Formula I are prepared according to processes known per se.Type: GrantFiled: April 8, 1991Date of Patent: December 8, 1992Assignee: Ciba-Geigy CorporationInventors: Jaroslav Stanek, Jorg Frei
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Patent number: 5162310Abstract: Phenylaliphatylaminoalkanediphosphonic acids of the formula ##STR1## in which R.sub.1 is an aliphatic hydrocarbon radical having 4 and not more than 7 C atoms and substituted by phenyl, R.sub.2 is a monovalent aliphatic hydrocarbon radical having 1 and not more than 4 C atoms and alk is a divalent aliphatic hydrocarbon radical having 2 and not more than 4 C atoms, and their salts, have a particularly pronounced regulating action on calcium metabolism and can be used as medicaments for the treatment of diseases to be attributed to disturbances thereof. They are prepared, for example, for reacting a compound of the formula ##STR2## in which X.sub.3 denotes carboxyl, with a phosphorylating agent and hydrolyzing the primary product.Type: GrantFiled: November 15, 1989Date of Patent: November 10, 1992Assignee: Ciba-Geigy CorporationInventor: Knut A. Jaeggi
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Patent number: 5153315Abstract: The invention relates to an improved process for the preparation of compounds of formula ##STR1## or salts thereof, starting from compounds of formulae ##STR2## via compounds of formulae ##STR3## in which compounds R.sub.1 is hydrogen or lower alkyl, R.sub.2 is an organic radical which may carry a functional group which may be protected by a customary protective group R.sub.2 .degree., R.sub.3 is hydrogen or a customary carboxyl protective group R.sub.3 .degree., W is a group which can be replaced by a thiocarboxylic acid radical of formula III, and Z is oxygen or sulfur.Type: GrantFiled: May 18, 1990Date of Patent: October 6, 1992Assignee: Ciba-Geigy CorporationInventors: Ernst Hungerbuhler, Jaroslav Kalvoda
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Patent number: 5149717Abstract: Substituted alkanophenones of general formula ##STR1## in which R.sub.1 is unsubstituted or fluorinated lower alkyl, R.sub.2 is hydrogen, or unsubstituted or fluorinated lower alkyl or lower alkenyl, X is lower alkylene, oxy, thio or a direct bond, alk is lower alkylene, n is 1 or 2, R.sub.3 is phenyl that is unsubstituted or is substituted by unsubstituted or fluorinated lower alkyl, by etherified or esterified hydroxy, by unsubstituted or lower alkylated amino and/or by free, esterified or amidated carboxy, or is lower alkyl that is unsubstituted, substituted by fluoro and chloro or substituted by free esterified or amidated carboxy, R.sub.4 is free, esterified or amidated carboxy or 5-tetrazolyl, and R.sub.5 is hydrogen or lower alkyl, have leucotriene-antagonistic properties and can be used as anti-allergic active ingredients in medicaments.Type: GrantFiled: November 15, 1991Date of Patent: September 22, 1992Assignee: Ciba-Geigy CorporationInventors: Andreas von Sprecher, Andreas Beck, Bruno Schaub, Robert W. Lang
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Patent number: 5147889Abstract: Benzo[b]thiophene derivatives of formula ##STR1## their tautomers and salts, in which the index n is 0, 1 or 2, alk is lower alkylene, Ar is phenyl, naphthyl or a monocyclic, five- or six-membered heteroaryl radical, wherein the aromatic radical is unsubstituted or is mono- or poly-substituted by lower alkyl, halo-lower alkyl, halogen and/or nitro, and the ring A is unsubstituted or is mono- or poly-substituted by lower alkyl, lower alkoxy, lower alkylthio, lower alkanesulfinyl, lower alkanesulfonyl, halo-lower alkyl, halogen and/or by nitro, can be used, for example, as active ingredients in medicaments.Type: GrantFiled: June 27, 1991Date of Patent: September 15, 1992Assignee: Ciba-Geigy CorporationInventor: Pier G. Ferrini
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Patent number: 5145868Abstract: Substituted alkanophenones of the general formula ##STR1## in which R.sub.1 is unsubstituted or fluorinated lower alkyl, R.sub.2 is hydrogen, or unsubstituted or fluorinated lower alkyl or lower alkenyl, X is lower alkylene, oxy, thio or a direct bond, alk is lower alkylene, n is 1 or 2, R.sub.3 is a 5-membered heteroaryl radical that contains 1N, O or S atom as hetero atom and is unsubstituted or is substituted by unsubstituted or fluorinated lower alkyl, by etherified or esterified hydroxy, by unsubstituted or lower alkylated amino and/or by free, esterfied or amidated carboxy, R.sub.4 is free, esterified or amidated carboxy or 5-tetrazolyl, and R.sub.5 is hydrogen or lower alkyl, have leucotriene-antagonistic properties can e used as antiallergic active ingredients in medicaments.Type: GrantFiled: November 15, 1991Date of Patent: September 8, 1992Assignee: Ciba-Geigy CorporationInventors: Andreas von Sprecher, Andreas Beck
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Patent number: 5139786Abstract: The invention relates to topically administrable pharmaceutical preparations containing pharmaceutically acceptable methanediphosphonic acid derivatives of formula ##STR1## and their salts, wherein R.sub.1 and R.sub.2 are hydrogen or C.sub.1 -C.sub.3 alkyl.Type: GrantFiled: December 20, 1991Date of Patent: August 18, 1992Assignees: Ciba-Geigy Corporation, Henkel Kommanditgesellschaft auf AktienInventors: Pier G. Ferrini, Carlo Voellmy, Peter H. Stahl, Jonathan Green
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Patent number: 5137720Abstract: Described is a synergistic pharmaceutical combination preparation comprising as component A a hybrid .alpha.-interferon the structure of which is derived from human interferon-.alpha.-D and -.alpha.-B gene fragments and as component B a muramylpeptide. The preparation can be used for treating viral diseases or reducing the formation of metastases of certain tumors.Type: GrantFiled: August 20, 1991Date of Patent: August 11, 1992Assignee: Ciba-Geigy CorporationInventors: J. David Gangemi, Heinz-Kurt Hochkeppel
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Patent number: 5135930Abstract: Novel hydrogenated heterocyclic compounds, containing two nitrogen atoms, of the formula ##STR1## in which R.sub.1, R.sub.2, R.sub.3, R.sub.5 and R.sub.7 are each, independently of the others, hydrogen or lower alkyl, m is 2 or 3, n is 1 or 2, and either R.sub.4 and R.sub.6 are each hydrogen or R.sub.4 and R.sub.6 together form an additional bond, in free form or in form of a salt, can be used as pharmaceutical active ingredients for memory improvement and can be manufactured in a manner known per se.Type: GrantFiled: December 3, 1990Date of Patent: August 4, 1992Assignee: Ciba-Geigy CorporationInventors: Wolfgang Frostl, Cesare Mondadori, Dietrich Strub, Armin Zust