Patents Represented by Attorney, Agent or Law Firm Irving M. Fishman
  • Patent number: 5204342
    Abstract: 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: Grant
    Filed: March 31, 1992
    Date of Patent: April 20, 1993
    Assignee: Ciba-Geigy Corporation
    Inventors: Wolfgang Frostl, Cesare Mondadori, Dietrich Strub, Armin Zust
  • Patent number: 5190947
    Abstract: 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: Grant
    Filed: August 16, 1991
    Date of Patent: March 2, 1993
    Assignee: Ciba-Geigy Corporation
    Inventors: Walter Riess, Alfred Sallmann
  • Patent number: 5190930
    Abstract: 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: Grant
    Filed: December 20, 1991
    Date of Patent: March 2, 1993
    Assignee: Ciba-Geigy Corporation
    Inventor: Knut A. Jaeggi
  • Patent number: 5190934
    Abstract: 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: Grant
    Filed: March 3, 1992
    Date of Patent: March 2, 1993
    Assignee: Ciba-Geigy Corporation
    Inventors: Stuart J. Mickel, Georg von Sprecher
  • Patent number: 5190933
    Abstract: 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: Grant
    Filed: March 3, 1992
    Date of Patent: March 2, 1993
    Assignee: Ciba-Geigy Corporation
    Inventors: Eric K. Baylis, Ludwig Maier, Stuart J. Mickel, Hans-Rudolf Olpe, Helmut Bittiger, Wolfgang Frostl, Roger G. Hall
  • Patent number: 5189017
    Abstract: 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: Grant
    Filed: October 17, 1990
    Date of Patent: February 23, 1993
    Assignee: Ciba-Geigy Corporation
    Inventors: Bohumir Lukas, Karl H. Schmidt-Ruppin
  • Patent number: 5185368
    Abstract: 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: Grant
    Filed: July 20, 1988
    Date of Patent: February 9, 1993
    Assignee: Ciba-Geigy Corporation
    Inventors: Heinrich Peter, Theophile Moerker
  • Patent number: 5177070
    Abstract: 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: Grant
    Filed: November 15, 1991
    Date of Patent: January 5, 1993
    Assignee: Ciba-Geigy Corporation
    Inventor: Richard Katz
  • Patent number: 5177091
    Abstract: 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: Grant
    Filed: November 20, 1991
    Date of Patent: January 5, 1993
    Assignee: Ciba-Geigy Corporation
    Inventors: Ulrich Feige, Irmgard Wiesenberg, Leo Widler, Pier G. Ferrini, Martin Missbach
  • Patent number: 5177257
    Abstract: 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: Grant
    Filed: November 20, 1991
    Date of Patent: January 5, 1993
    Assignee: Ciba-Geigy Corporation
    Inventors: Andreas von Sprecher, Hansjurg Wetter
  • Patent number: 5175344
    Abstract: 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: Grant
    Filed: July 17, 1991
    Date of Patent: December 29, 1992
    Assignee: Ciba-Geigy Corporation
    Inventors: Christof Angst, Derek E. Brundish, John G. Dingwall, Graham E. Fagg, Hans Allgeier, Guido Bold, Rudolf Duthaler, Roland Heckendorn, Antonio Togni
  • Patent number: 5169867
    Abstract: 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: Grant
    Filed: April 8, 1991
    Date of Patent: December 8, 1992
    Assignee: Ciba-Geigy Corporation
    Inventors: Jaroslav Stanek, Jorg Frei
  • Patent number: 5162310
    Abstract: 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: Grant
    Filed: November 15, 1989
    Date of Patent: November 10, 1992
    Assignee: Ciba-Geigy Corporation
    Inventor: Knut A. Jaeggi
  • Patent number: 5153315
    Abstract: 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: Grant
    Filed: May 18, 1990
    Date of Patent: October 6, 1992
    Assignee: Ciba-Geigy Corporation
    Inventors: Ernst Hungerbuhler, Jaroslav Kalvoda
  • Patent number: 5149717
    Abstract: 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: Grant
    Filed: November 15, 1991
    Date of Patent: September 22, 1992
    Assignee: Ciba-Geigy Corporation
    Inventors: Andreas von Sprecher, Andreas Beck, Bruno Schaub, Robert W. Lang
  • Patent number: 5147889
    Abstract: 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: Grant
    Filed: June 27, 1991
    Date of Patent: September 15, 1992
    Assignee: Ciba-Geigy Corporation
    Inventor: Pier G. Ferrini
  • Patent number: 5145868
    Abstract: 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: Grant
    Filed: November 15, 1991
    Date of Patent: September 8, 1992
    Assignee: Ciba-Geigy Corporation
    Inventors: Andreas von Sprecher, Andreas Beck
  • Patent number: 5139786
    Abstract: 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: Grant
    Filed: December 20, 1991
    Date of Patent: August 18, 1992
    Assignees: Ciba-Geigy Corporation, Henkel Kommanditgesellschaft auf Aktien
    Inventors: Pier G. Ferrini, Carlo Voellmy, Peter H. Stahl, Jonathan Green
  • Patent number: 5137720
    Abstract: 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: Grant
    Filed: August 20, 1991
    Date of Patent: August 11, 1992
    Assignee: Ciba-Geigy Corporation
    Inventors: J. David Gangemi, Heinz-Kurt Hochkeppel
  • Patent number: 5135930
    Abstract: 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: Grant
    Filed: December 3, 1990
    Date of Patent: August 4, 1992
    Assignee: Ciba-Geigy Corporation
    Inventors: Wolfgang Frostl, Cesare Mondadori, Dietrich Strub, Armin Zust