Patents Represented by Attorney, Agent or Law Firm Stephen G. Kalinchak
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Patent number: 6136967Abstract: The invention relates to a new process for the depletion of 7-amino-3-[(E)-1-propen-1-yl]-3-cephem-4-carboxylic acid in mixtures of 7-amino-3-[(Z)-1-propen-1-yl]-3-cephem-4-carboxylic acid and 7-amino-3-[(E)-1-propen-1-yl]-3-cephem-4-carboxylic acid, by means of the crystalline hydrochloride or a metal or amine salt of 7-amino-3-[(Z/E)-1-propen-1-yl]-3-cephem-4-carboxylic acid or by adsorption chromatography.Type: GrantFiled: November 12, 1998Date of Patent: October 24, 2000Assignee: Biochemie Gesellschaft m.b.H.Inventors: Johannes Ludescher, Bernhard Prager, Siegfried Wolf
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Patent number: 6133441Abstract: Process for the production of alkali salts of clavulanic acid of formula ##STR1## by conversion of clavulanic acid into a pharmaceutically acceptable salt of clavulanic acid which is characterised in that the conversion is carried out in n-butanol or iso-butanol (2-methyl-1-propanol) as a solvent; and a potassium salt of clavulanic acid containing n-butanol or iso-butanol.Type: GrantFiled: May 11, 1998Date of Patent: October 17, 2000Assignee: Biochemie Gesellschaft m.b.H.Inventor: Helmut Wagner
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Patent number: 6130250Abstract: Use of the compound of formula I (as described in the specification) in the therapy of veterinary diseases, the expression of which is enhanced by increasing stock density.Type: GrantFiled: July 2, 1999Date of Patent: October 10, 2000Assignee: Biochemie Gesellschaft m.b.H.Inventors: David George Sidney Burch, Paul Howard Ripley, Erich Zeisl
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Patent number: 6114468Abstract: A polystyrene resin which is substituted in skeletal benzene rings thereof by a group of formula--CH.sub.2 --O--Ar.sup.1 --R Iwhere Ar.sup.1 is an unsubstituted or substituted phenylene group and R is a group of formula ##STR1## or a precursor group for a group of formula II, said precursor group being of formula--CH.dbd.N--NH--SO.sub.2 Ar.sup.2 IIIwhere Ar.sup.2 is an aryl group.Type: GrantFiled: June 1, 1998Date of Patent: September 5, 2000Assignee: Novartis AGInventor: Gurdip Bhalay
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Patent number: 6093813Abstract: Cephalosporin derivatives of formula II ##STR1## wherein R.sup.a denotes hydrogen or a silyl group; R.sup.b denotes a group of formula --OR.sup.e, wherein R.sup.e denotes hydrogen or alkyl; and R.sup.c and R.sup.d together denote a bond; in free form or in salt form.Type: GrantFiled: September 30, 1998Date of Patent: July 25, 2000Assignee: Biochemie Gesellschaft m.b.H.Inventors: Gerd Ascher, Johannes Ludescher, Hubert Sturm, Josef Wieser
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Patent number: 6068853Abstract: A delivery mechanism and device for the passive periodic release of a drug or an active ingredient which avoids the need for external power sources and/or electronic controllers. By taking advantage of oscillating chemical systems, one can change the state, i.e. the pH, of a solution, a drug, enhancer or solubilizer resulting in oscillating the ability of an active ingredient to be delivered transdermally. The pH of a solution can be oscillated over a range of pH values from 2 to 10 by the reduction and oxidation (redox) reactions of salts, such as permanganates, iodates, sulfates, chlorates, or bromates. Upon activation, the delivery system conditions begin to oscillate and with it, the delivery of the active agent oscillates.Type: GrantFiled: October 13, 1995Date of Patent: May 30, 2000Assignee: Novartis CorporationInventors: Steven Andrew Giannos, Steven Minh Dinh, Bret Berner
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Patent number: 6063917Abstract: A process for the production of a compound of formula ##STR1## wherein R.sup.a denotes hydrogen or silyl;R.sup.b denotes a group of formula --OR.sup.e, whereinR.sup.e denotes hydrogen or alkyl; andR.sup.c and R.sup.d together denote a bond;in free form or in salt form,which process comprises the step of spitting, in the presence of ozone, the double bond in position 3 of the ring structure of a compound of formula III ##STR2## wherein R.sub.2 and R.sub.3 are the same or different and independently of each other denote hydrogen or an organic group, and X.sup.- denotes the anion of an inorganic or organic acid and optionally silylating the amine group in position 7 of the ring system.Type: GrantFiled: September 30, 1998Date of Patent: May 16, 2000Assignee: Biochemie Gesellschaft m.b.H.Inventors: Gerd Ascher, Johannes Ludescher, Hubert Sturm, Josef Wieser
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Patent number: 6034237Abstract: 3-Imino-cephalosporin derivatives of formula II ##STR1## wherein Y denotes alkyl, aryl or heterocyclyl; and R.sup.a and R.sup.d denote hydrogen or a silyl group; in free form or in salt form, and methods of preparation.Type: GrantFiled: September 30, 1998Date of Patent: March 7, 2000Assignee: Biochemie Gesellschaft m.b.H.Inventors: Gerd Ascher, Johannes Ludescher, Hubert Sturm, Josef Wieser
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Patent number: 6025391Abstract: Disclosed are pharmaceutical compositions which have been modified to release pharmaceutically acceptable mycophenolate salts in the upper part of the intestinal tract and methods of treatment using the pharmaceutical compositions.Type: GrantFiled: May 28, 1998Date of Patent: February 15, 2000Assignee: Novartis AGInventors: Barbara Haeberlin, Ching-Pong Mak, Armin Meinzer, Jacky Vonderscher
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Patent number: 6024978Abstract: Pharmaceutical compositions comprising a cyclosporin, e.g. Ciclosporin or [Nva].sup.2 -Ciclosporin, in "microemulsion pre-concentrate" and microemulsion form. The compositions typically comprise (1.1) a C.sub.1-5 -alkyl or tetrahydrofurfuryl di- or partial-ether of a low molecular weight mono- or poly-oxy-alkane diol, e.g. Transcutol or Glycofurol, as hydrophilic component. Compositions are also provided comprising a cyclosporin and (1.1) and, suitably, also a saccharide monoester, e.g. raffinose or saccharose monolaurate. Dosage forms include topical formulations and, in particular, oral dosage forms.Type: GrantFiled: November 2, 1998Date of Patent: February 15, 2000Assignee: Novartis AGInventors: Birgit Hauer, Armin Meinzer, Ulrich Posanski, Friedrich Richter
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Patent number: 6015919Abstract: The invention relates to a compound of formula I ##STR1## R.sub.1 is C.sub.1 -C.sub.8 alkyl, phenyl or phenyl substituted by from 1 to 3 C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 alkoxy substituents;R.sub.2 and R.sub.3 are each independently of the other hydrogen or C.sub.1 -C.sub.12 alkyl; andHal is F, Cl, Br or I.Compounds of formula I are valuable intermediates for compounds of formula III which are also a subject of this invention: ##STR2## R.sub.1, R.sub.2, R.sub.3 and Hal are as defined above; R.sub.10 and R.sub.11 are identical or different and are C.sub.1 -C.sub.12 alkyl, C.sub.5 -C.sub.12 cycloalkyl, phenyl, C.sub.5 -C.sub.12 cycloalkyl substituted by C.sub.1 -C.sub.4 alkyl or by C.sub.1 -C.sub.4 alkoxy, or phenyl substituted by from one to three C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, --SiR.sub.4 R.sub.5 R.sub.6, halogen, --SO.sub.3 M, --CO.sub.2 M, --PO.sub.3 M, --NR.sub.7 R.sub.8, --[.sup.+ NR.sub.7 R.sub.8 R.sub.9 ]X.sup.- or C.sub.1 -C.sub.5 fluoroalkyl substituents; orthe group --PR.Type: GrantFiled: February 8, 1999Date of Patent: January 18, 2000Assignee: Novartis AGInventor: Benoit Pugin
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Patent number: 6011149Abstract: The present invention relates to photochemically cross-linked derivatives of general formulae (IA) and (IB), wherein R is a polysaccharide radical in which the OH groups have been esterified as OR' groups or converted into a carbamate (urethane), R.sub.1, and R.sub.2 are each independently lower alkyl or unsubstituted or substituted aryl, X is a direct bond or phenylene, m is 0 or 1, and n is 0 or an integer from 1 to 20, to processes from the preparation thereof and to the use thereof. The compounds of general formula (IA) and (IB) can be used as supports in the chromatographic separation of enantiomers.Type: GrantFiled: September 2, 1997Date of Patent: January 4, 2000Assignee: Novartis AGInventor: Eric Francotte
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Patent number: 6008393Abstract: Compounds of formulae I: (DIP)IrX.sub.q Y.sub.r (Z), Ia: (DIP)IrX.sub.s Y.sub.t (Z).sub.2 and Ib: (DIP)Ir(Z).sub.3 or mixtures of at least two of those compounds, wherein DIP is a ditertiary diphosphine, the two phosphine groups of which are bonded to a C.sub.2 -, C.sub.3 - or C.sub.4 -carbon chain, with the result that the diphosphine forms a 5- to 7-membered ring together with the Ir atom, X is Cl, Br or I, Y is a hydrogen atom, q and r are 0, 1 or 2 and the sum of q+r is 2, s and t are 0 or 1 and the sum of s+t is 1, and Z is the anion of an organic oxy acid that contains a group C(.dbd.O), S(.dbd.O)O or P(.dbd.O)O in the anion. The compounds are excellent catalysts for the hydrogenation of imines, especially for the enantioselective hydrogenation of prochiral imines.Type: GrantFiled: January 22, 1998Date of Patent: December 28, 1999Assignee: Novartis AGInventors: Rafael Sablong, John Anthony Osborn, Felix Spindler
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Patent number: 6007840Abstract: Pharmaceutical compositions comprising a cyclosporin, e.g. Ciclosporin or [Nva].sup.2 -Ciclosporin, in "microemulsion pre-concentrate" and microemulsion form. The compositions typically comprise (1.1) a C.sub.1-5 alkyl or tetrahydrofurfuryl di- or partial-ether of a low molecular weight mono- or poly-oxy-alkane diol, e.g. Transcutol or Glycofurol, as hydrophilic component. Compositions are also provided comprising a cyclosporin and (1.1) and, suitably, also a saccharide monoester, e.g. raffinose or saccharose monolaurate. Dosage forms include topical formulations and, in particular, oral dosage forms.Type: GrantFiled: November 2, 1998Date of Patent: December 28, 1999Assignee: Novartis AGInventors: Birgit Hauer, Armin Meinzer, Ulrich Posanski, Friedrich Richter
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Patent number: 5998610Abstract: A process for the silylation of 6-aminopenicillanic acid or 7-amino-desacetoxy-cephalosporanic acid by silylation in certain carboxylic acid esters and its use in the production of 6-alpha-aminoacyl-penicillins and 7-alpha-aminoacyl-desacetoxy-cephalosporins.Type: GrantFiled: July 25, 1997Date of Patent: December 7, 1999Assignee: Biochemie Gesellschaft m.b.H.Inventors: Victor Centellas, Jose Diago, Johannes Ludescher
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Patent number: 5990289Abstract: The instant invention relate to a new method for the purification of proteins using copper chelate-affinity chromatography, wherein the impure or pre-purified protein is adsorbed on immobilized copper(II) ions, optionally washed with buffer and deionized water, washed with a solution of a Lewis-base, and finally eluted with deionized water.Type: GrantFiled: January 2, 1998Date of Patent: November 23, 1999Assignee: Novartis AGInventors: Pierre Fran.cedilla.ois Fauquex, Catherine Georges
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Patent number: 5985321Abstract: Soft gelatin capsules having a capsule shell comprising gelatin, plasticizers and, if desired or required, further auxiliary agents, and a capsule filling containing a solvent including a migrateable solvent such as 1,2-propyleneglycol as a solvent in the capsule filling and in the capsule shell. The manufacture of said capsules is improved, if in the process for making the soft gelatin capsules the gelatin bands are cooled with a liquid, and preferably with water.Type: GrantFiled: April 29, 1997Date of Patent: November 16, 1999Assignees: Novartis AG, R.P. Scherer GmbHInventors: Werner Brox, Armin Meinzer, Horst Zande
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Patent number: 5977290Abstract: The invention relates to a process for the condensation of aldehydes or ketones with C--H acidic compounds (in particular Knoevenagel reaction) in the presence of at least one molecular sieve in the form of a zeolite or sheet silicate and one alkali carbonate, alkaline earth carbonate or ammonium carbonate as catalyst system. The products obtained are important intermediates or end products for the perfume industry.Type: GrantFiled: June 9, 1998Date of Patent: November 2, 1999Assignee: Novartis AGInventor: Bernd Siebenhaar
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Patent number: D420736Type: GrantFiled: December 22, 1997Date of Patent: February 15, 2000Assignee: Novartis AGInventor: Claude Moulin
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Patent number: D420739Type: GrantFiled: May 12, 1998Date of Patent: February 15, 2000Assignees: Novartis AG, EndoscopticInventor: Xavier Moreau-Defarges