Patents Represented by Attorney, Agent or Law Firm Irving M. Fishman
  • Patent number: 5424441
    Abstract: N-aralkyl- and N-heteroaralkyl-aminoalkanephosphinic acids of formula I ##STR1## wherein R is an aliphatic, cycloaliphatic, cycloaliphatic-aliphatic, araliphatic or heteroarylaliphatic radical having at least 2 carbon atoms, R.sub.1 is hydrogen or hydroxy, R.sub.2 is an araliphatic or heteroarylaliphatic radical substituted by free or functionally modified carboxy that is bonded directly or by way of a spacer, and R.sub.3 is hydrogen, lower alkyl or a group R.sub.2, and the salts thereof have valuable nootropic and anti-epileptic properties and can be used in the preparation of a nootropic or anti-epileptic medicament.
    Type: Grant
    Filed: May 4, 1994
    Date of Patent: June 13, 1995
    Assignee: Ciba-Geigy Corporation
    Inventors: Stuart J. Mickel, Wolfgang Frostl, Pascal Furet
  • Patent number: 5413994
    Abstract: Compounds of formula I ##STR1## wherein R, R.sub.1, R.sub.2 and q are as defined in the description, have valuable pharmacological properties and are especially effective as calcium metabolism regulators. They are prepared in a manner known per se.
    Type: Grant
    Filed: June 9, 1993
    Date of Patent: May 9, 1995
    Assignee: Ciba-Geigy Corporation
    Inventor: Knut A. Jaeggi
  • Patent number: 5409927
    Abstract: There are described compounds of formula I ##STR1## wherein R.sub.1 is hydrogen or lower alkyl,R.sub.2 is hydrogen, lower alkyl, lower alkoxycarbonyl, phenyl- or naphthyl-lower alkoxycarbonyl, heterocyclylcarbonyl wherein heterocyclyl contains 5 or 6 ring atoms, is saturated and is bonded to the carbonyl group via a ring nitrogen atom and, in addition to the bonding nitrogen atom, contains as ring member one or more further hetero atoms selected from unsubstituted or C.sub.1 -C.sub.4 alkyl-substituted NH, O, S, S.dbd.O and SO.sub.2, or is lower alkanoyl, phenyl- or naphthyl-lower alkanoyl or lower alkanesulfonyl,R.sub.3 is morpholino, thiomorpholino, S-oxothiomorpholino or S,S-dioxothiomorpholino, the heterocyclyl radical in heterocyclylcarbonyl R.sub.2 having the same definition as R.sub.3 or having a definition other than R.sub.3, andR.sub.4 is hydrogen, hydroxy, C.sub.1 -C.sub.4 alkoxy, cyano, trifluoromethyl or fluorine, and salts of those compounds where salt-forming groups are present.
    Type: Grant
    Filed: March 25, 1993
    Date of Patent: April 25, 1995
    Assignee: Ciba-Geigy Corporation
    Inventors: Guido Bold, Alexander Fassler, Marc Lang, Peter Schneider
  • Patent number: 5407922
    Abstract: Compounds having GABA.sub.B -antagonistic properties, for example those of formula I ##STR1## wherein one of the radicals R.sub.1, R.sub.2 and R.sub.3 is hydrogen or an aliphatic, cycloaliphatic, araliphatic or aromatic radical, another is hydrogen or, in the case of R.sub.1 or R.sub.2, hydroxy or, in the case of R.sub.1, halogen or, in the case of R.sub.2 together with R.sub.2 ', oxo, and the remaining radical is hydrogen, R.sub.1 ' is hydrogen or halogen, R.sub.2 ' is hydrogen, hydroxy or, together with R.sub.2, is oxo, R.sub.4 and R.sub.5 are hydrogen or R.sub.4 is an araliphatic or heteroarylaliphatic radical and R.sub.5 is hydrogen or an aliphatic radical, and R is an aliphatic, cycloaliphatic, cycloaliphatic-aliphatic, araliphatic, heteroarylaliphatic or aromatic radical having at least 2 carbon atoms or, when R.sub.1 is hydrogen or hydroxy, R.sub.2 is an aromatic radical and R.sub.1 ', R.sub.2 ' and R.sub.
    Type: Grant
    Filed: May 3, 1993
    Date of Patent: April 18, 1995
    Assignee: Ciba-Geigy Corporation
    Inventors: Christian Marescaux, Raymond Bernasconi, Markus Schmutz, Wolfgang Frostl, Stuart J. Mickel
  • Patent number: 5399578
    Abstract: Compounds of the formula ##STR1## in which R.sub.1 is an aliphatic hydrocarbon radical which is unsubstituted or substituted by halogen or hydroxyl, or a cycloaliphatic or araliphatic hydrocarbon radical; X.sub.1 is CO, SO.sub.2, or --O--C(.dbd.O)-- with the carbon atom of the carbonyl group being attached to the nitrogen atom shown in formula I; X.sub.2 is a divalent aliphatic hydrocarbon radical which is unsubstituted or substituted by hydroxyl, carboxyl, amino, guanidino or a cycloaliphatic or aromatic radical, or is a divalent cycloaliphatic hydrocarbon radical, it being possible for a carbon atom of the aliphatic hydrocarbon radical to be additionally bridged by a divalent aliphatic hydrocarbon radical; R.sub.2 is carboxyl which, if desired, is esterified or amidated, substituted or unsubstituted amino, formyl which, if desired, is acetalized, 1H-tetrazol-5-yl, pyridyl, hydroxyl which, if desired, is etherified, S(O).sub.
    Type: Grant
    Filed: December 29, 1992
    Date of Patent: March 21, 1995
    Assignee: Ciba-Geigy Corp
    Inventors: Peter Buhlmayer, Franz Ostermayer, Tibur Schmidlin
  • Patent number: 5399714
    Abstract: The invention relates to a novel process for the preparation of compounds of formula I ##STR1## wherein R is straight-chain C.sub.2 -C.sub.4 alk-1-en-1-yl, and salts thereof, and to a novel starting material and the use thereof.
    Type: Grant
    Filed: July 5, 1994
    Date of Patent: March 21, 1995
    Assignee: Ciba-Geigy Corporation
    Inventors: Marc Gerspacher, Alfred Sallman
  • Patent number: 5399576
    Abstract: Novel thiazoles of formula I ##STR1## wherein R.sub.1 and R.sub.4 are lower alkyl, lower alk-2-en-1-yl or lower alk-2-yn-1-yl,R.sub.2 and R.sub.3 are each independently of the other hydrogen or lower alkyl or together form lower alkylidene, andR.sub.5 and R.sub.6 are each hydrogen or lower alkyl or together form oxo, andR.sub.5 ' and R.sub.6 ' have the same definitions as R.sub.5 and R.sub.6,with the proviso that at least one of the substituent pairs R.sub.5 and R.sub.6 or R.sub.5 ' and R.sub.6 ' together form oxo, and salts thereof, processes for the preparation of the said compounds, pharmaceutical compositions comprising them and the use thereof as medicinal active ingredients.
    Type: Grant
    Filed: February 25, 1994
    Date of Patent: March 21, 1995
    Assignee: Ciba-Geigy Corporation
    Inventor: Martin Missbach
  • Patent number: 5395855
    Abstract: Compounds of formula I ##STR1## wherein A, X, Z and R.sub.1 -R.sub.5 are as defined in the description, and their salts have valuable pharmaceutical properties and are effective especially against tumors. They are prepared in a manner known per se.
    Type: Grant
    Filed: March 28, 1994
    Date of Patent: March 7, 1995
    Assignee: Ciba-Geigy Corporation
    Inventors: Jaroslav Stanek, Jorg Frei, Giorgio Caravatti
  • Patent number: 5389681
    Abstract: The invention relates to a pharmaceutical composition in the form of a sterilizable parenteral solution comprising a diclofenac salt and stabilizers, such as ethyl lactate combined with glutathione or N-acetylcysteine.
    Type: Grant
    Filed: September 30, 1993
    Date of Patent: February 14, 1995
    Assignee: Ciba-Geigy Corporation
    Inventor: Bruno Galli
  • Patent number: 5386637
    Abstract: A blade holder for a manual cutting tool having a rigid open-ended frame shaped to provide support for a blade between the ends of the frame so that the cutting edge of the blade is proud of the ends of the frame, a clamp pivotally mounted on the frame, and a spring mounted on the frame and acting on the clamp. The clamp is moveable between an open position and a closed position. Manual pressure on the clamp against the spring forces the clamp apart from the ends of the frame to leave a gap (the open position) for the insertion or removal of a blade. Release of the manual pressure results in the spring holding the clamp against the ends of the frame (the closed position) so as to provide for retention of the blade in position between the clamp and the frame during a cutting operation.
    Type: Grant
    Filed: October 21, 1993
    Date of Patent: February 7, 1995
    Assignee: Ciba-Geigy Corporation
    Inventors: Lawrence C. Saddoo, Robert M. Williams
  • Patent number: 5386029
    Abstract: The invention relates to a novel process for the manufacture of (3R,1'R)-4-acyloxy-3-(1'-hydroxyethyl)-2-azetidinones of formula ##STR1## in which R.sup.1 represents lower alkyl or aryl, by enantioselective reduction of the carbonyl group in a suitable .alpha.-acylaminomethyl-acetoacetic acid ester, cyclization of the resulting .alpha.-acylaminomethyl-.beta.-hydroxybutyric acid ester to a 5,6-dihydro-1,3,4H-oxazine with inversion of the carbon atom carrying the hydroxy group, equilibration to form the preferred trans-substituted dihydrooxazine, recleaving to form the configuratively uniform .alpha.-aminomethyl-.beta.-hydroxybutyric acid, ring-closure to form the .beta.-lactam and oxidative acylation at C(4) of the .beta.-lactam. Compounds of formula I can be used as starting materials for the manufacture of .beta.-lactam antibiotics. The invention relates also to novel intermediates.
    Type: Grant
    Filed: July 16, 1993
    Date of Patent: January 31, 1995
    Assignee: Ciba-Geigy Corporation
    Inventors: Peter Schneider, Gerardo Ramos
  • Patent number: 5384319
    Abstract: Aminoalkylphenyl derivatives of formula I ##STR1## wherein alk, R.sub.1 -R.sub.6, X and Y are as defined in the description, and salts thereof, exhibit properties inhibiting the biosynthesis of interleukin-1 (IL-1) and analgesic properties and can therefore be used as active ingredients in medicaments. They are prepared in a manner known per se.
    Type: Grant
    Filed: December 20, 1993
    Date of Patent: January 24, 1995
    Assignee: Ciba-Geigy Corporation
    Inventor: Pier G. Ferrini
  • Patent number: 5382659
    Abstract: The invention relates to novel aromatic acids, especially to compounds of formula ##STR1## wherein R.sub.1 is lower alkyl, R.sub.2 is lower alkyl, R.sub.3 is hydrogen, carboxy or sulfo, R.sub.4 is carboxy or sulfo, G is an unsubstituted or substituted 1,4-phenylene group or an unsubstituted or substituted 1,4-naphthylene group, and wherein either R.sub.5 and R.sub.6 together are an additional bond and L is an oxygen or sulfur atom or wherein R.sub.5 is hydrogen, R.sub.6 is halomethyl and L is an oxygen atom, and salts thereof, to the use of compounds I and their salts, to a process for the preparation of compounds I and their salts, to starting materials used in that preparation process, and salts thereof, to a process for the preparation of those starting materials and their salts, to a device in which the compounds I and their salts are used, and to a process in which that device is used.
    Type: Grant
    Filed: June 7, 1994
    Date of Patent: January 17, 1995
    Assignee: Ciba-Geigy Corp.
    Inventor: Jui Y. Chang
  • Patent number: 5382675
    Abstract: A tetrahydropyran-4-yloxy-alkanoic acid of formula III ##STR1## wherein R.sub.2 is hydrogen or C.sub.1-4 alkyl and R.sub.3 is hydrogen or C.sub.1-4 alkyl.
    Type: Grant
    Filed: April 28, 1994
    Date of Patent: January 17, 1995
    Assignee: Ciba-Geigy Corporation
    Inventor: Oskar Wacker
  • Patent number: 5380726
    Abstract: Substituted dialkylthio ethers of formula I ##STR1## wherein R.sub.1 -R.sub.6, alk, X and Y are as defined in the description, and salts thereof, exhibit properties inhibiting the biosynthesis of interleukin-1 (IL-1) and analgesic properties and can therefore be used as active ingredients in medicaments. They are prepared in a manner known per se.
    Type: Grant
    Filed: December 20, 1993
    Date of Patent: January 10, 1995
    Assignee: Ciba-Geigy Corporation
    Inventor: Pier G. Ferrini
  • Patent number: 5378719
    Abstract: Novel imidazoles of formula I ##STR1## wherein R.sub.1 and R.sub.4 are lower alkyl, lower alk-2-en-1-yl or lower alk-2-yn-1-yl,R.sub.2 and R.sub.3 are each independently of the other hydrogen or lower alkyl or together form lower alkylidene, andR.sub.5 and R.sub.6 are each hydrogen or lower alkyl or together form oxo, andR.sub.5 ' and R.sub.6 ' have the same definitions as R.sub.5 and R.sub.6,with the proviso that at least one of the substituent pairs R.sub.5 and R.sub.6 or R.sub.5 ' and R.sub.6 ' together form oxo, and salts thereof, processes for the preparation of the said compounds, pharmaceutical compositions comprising them and the use thereof as medicinal active ingredients.
    Type: Grant
    Filed: February 15, 1994
    Date of Patent: January 3, 1995
    Assignee: Ciba-Geigy Corporation
    Inventor: Martin Missbach
  • Patent number: 5378710
    Abstract: Compounds of the formula ##STR1## wherein carbon atoms 1 and 2 are linked by a single bond or a double bond, R.sub.1 is hydrogen, methyl or ethyl, and A is a group of the formula --N(--R.sub.2)--X-- wherein R.sub.2 is hydrogen or C.sub.1 -C.sub.4 alkyl and X is C.sub.1 -C.sub.12 alkylene or C.sub.3 -C.sub.6 cycloalkylidene; a group of the formula --N(--R.sub.2)--Y--Phe-- wherein R.sub.2 is as defined above, Y is a direct bond or C.sub.1 -C.sub.6 -alkylene and Phe is an unsubstituted or substituted phenylene radical; a group of the formula --O--X-- wherein X is as defined above, or a group --O--Y--Phe-- wherein Y and Phe are as defined above, are inhibitors of 5.alpha.-reductase and can be used for the therapeutic treatment of the human and animal body.
    Type: Grant
    Filed: October 6, 1993
    Date of Patent: January 3, 1995
    Assignee: Ciba-Geigy Corp.
    Inventor: Michel Biollaz
  • Patent number: 5378721
    Abstract: Compounds of formula I ##STR1## wherein Z, X, R, R.sub.0, R.sub.1, R.sub.2 and R.sub.3 are as defined in the description, have valuable pharmaceutical properties and are effective especially against tumors. They are prepared in a manner known per se.
    Type: Grant
    Filed: June 24, 1993
    Date of Patent: January 3, 1995
    Assignee: Ciba-Geigy Corporation
    Inventor: Marc Lang
  • Patent number: 5376685
    Abstract: Compounds of formula I ##STR1## wherein A, X.sub.1, X.sub.2, X.sub.3, X.sub.4, Y, Z and R.sub.1 to R.sub.6 have the meanings given in the description, have valuable pharmaceutical properties and are effective especially against tumors. They are prepared in a manner known per se.
    Type: Grant
    Filed: May 7, 1993
    Date of Patent: December 27, 1994
    Assignee: Ciba-Geigy Corporation
    Inventors: Jaroslav Stanek, Giorgio Caravatti, Jorg Frei, Hans-Georg Capraro
  • Patent number: 5376669
    Abstract: Compounds of formula I ##STR1## wherein Z, R, R.sub.1, R.sub.2 and X are as defined in the description, have valuable pharmaceutical properties and are effective especially against tumors. They are prepared in a manner known per se.
    Type: Grant
    Filed: March 17, 1993
    Date of Patent: December 27, 1994
    Assignee: Ciba-Geigy Corp.
    Inventors: Marc Lang, Edmond Differding, Jaroslav Stanek