Patents Represented by Attorney, Agent or Law Firm John D. Thallemer
  • Patent number: 7271269
    Abstract: Pharmaceutically suitable crystalline and amorphous alkali and earth-alkali salts of 2-n-butyl-4-chloro-5-hidrox-ymethyl-1-[[2?-(1 H-tetrazole-5-yl)[1.1?-biphenyl]-4-yl]-1 Himidazole have been prepared and new manufacturing, purification and isolation procedure for said salts in high purity have been described. Stable pharmaceutical compositions containing new crystalline potassium salts of 2-n-butyl-5-chloro-5hidroxymethyl-1-[[2?-(1H-tetrazole-5-yl)[1.1?-biphenyl]-44-yl]-1H-imidazole have been prepared.
    Type: Grant
    Filed: January 29, 2004
    Date of Patent: September 18, 2007
    Assignee: Lek Pharmaceuticals D.D.
    Inventors: Ljubomir Antoncic, Anton Copar, Peter Svete, Breda Husu-Kovacevic, Zoran Ham, Boris Marolt
  • Patent number: 7153970
    Abstract: 3-ethyl 5-methyl (+/?) 2-[(2-aminoethoxy)methyl]-4-(2-chlorophenyl)-1,4-dihydro-6-methyl-3,5-pyridinedicarboxylate benzenesulfonate, containing overall impurities of significantly less than 0.3% is disclosed, as well as process for its preparation, according to which substance of 3-ethyl 5-methyl (+/?) 2-[2-(N-trialkylamino)ethoxymethyl]-4-(2-chlorophenyl)-1,4-dihydro-6-methyl-3,5-pyridinedicarboxylate is converted with benzenesulfonic acid in ethanol solution, at a temperature between 20° C. and reflux temperature, followed by isolation and purification of 3-ethyl 5-methyl (+/?) 2-[(2-aminoethoxy)methyl]-4-(2-chlorophenyl)-1,4-dihydro-6-methyl-3,5-pyridinedicarboxylate benzenesulfonate. Amlodipine benzenesulfonate is useful as an antiishemic and antihypertensive agent.
    Type: Grant
    Filed: July 5, 2002
    Date of Patent: December 26, 2006
    Assignee: Lek Pharmaceuticals d.d.
    Inventors: Borut Furlan, Marijan Resnik
  • Patent number: 7098362
    Abstract: The present invention relates to new processes for the preparation of gabapentin by the desilylation of a silylated gabapentin or by the silylation-desilylation of an acid addition salt of gabapentin with a silylating agent.
    Type: Grant
    Filed: July 19, 2005
    Date of Patent: August 29, 2006
    Assignee: Sandoz AG
    Inventors: Rafael Garcia, Johannes Ludescher, Jordi Rifa, José Diago
  • Patent number: 7030151
    Abstract: Atorvastatin calcium, the substance known by the chemical name (R—(R*,R*))-2-(4-fluorophenyl)-?, ?-dihydroxy-5-(1-methylethyl)-3-phenyl-((phenylamino)carbonyl)-1H-pyrrole-1-heptanoic acid hemi calcium salt is known as HMG-CoA reductase inhibitor and is used as an antihypercholesterolemic agent. Atorvastatin in the pharmaceutical compositions available in the market, is usually prepared as its calcium salt since it enables atorvastatin to be conveniently formulated in the pharmaceutical formulations, for example, in tablets, capsules, powders and the like for oral administration. Atorvastatin calcium can exist in an amorphous form or in one of the at least four known crystalline forms (Form I, Form II, Form III and Form IV). Atorvastatin calcium is the substance which is sparingly soluble in water, with pKa 4,5, and it has been found that the crystalline forms are less soluble than the amorphous form, which may cause problems in bioavailability of atorvastatin in the body.
    Type: Grant
    Filed: March 13, 2002
    Date of Patent: April 18, 2006
    Assignee: Lek Pharmaceuticals d.d.
    Inventors: Janez Ker{hacek over (c)}, Mateja Salobir, Sa{hacek over (s)}a Bavec
  • Patent number: 6962924
    Abstract: This invention provides a process of preparation of novel polymorphic hemifumarate salts of 8-chloro-6,11-dihyfro-11-(4-piperidylidene)-5H-benzo[5,6]-cyclohepta[1,2-b]pyridine, hereinafter called “desloratadine”. These polymorphic salt forms show much higher solubility in water and also in protic organic solvents compare to the parent desloratadine. The process of preparing the polymorphic forms comprising: a) mixing the ethanolic solution of desloratadine and fumaric acid at a temperature of from about 55° C. to 70° C., and stirring for 30 to 45 minutes after mixing, and thereafter filtering the solid thereby prepared in hot condition; to yield the polymorphic form 2 having a DSC of 232° C.±2° C.; or b) mixing the ethanolic solution of desloratadine and fumaric acid at a temperature of form about 15° C. room temperature (25° C.) and stirring at this temperature for 30 to 45 minutes, then filtering at room temperature; to yield the polymorphic form 1 having a DSC of 224° C.±2° C.
    Type: Grant
    Filed: July 17, 2003
    Date of Patent: November 8, 2005
    Assignee: Sandoz AG
    Inventors: Anup Kumar Ray, Hiren Patel, Mahendra R Patel
  • Patent number: 6949641
    Abstract: The novel intermediate compound crystalline 7-[2-(2-fomylaminothiazol-4-yl)-2 -(Z)-(methoxyimino)acetamido]-3-methoxymethyl-3-cephem-4-carboxylic acid-1 -(isopropoxy/crystallization of cefpodoxime proxetil. The crystallization process comprises dissolving or suspending the intermediate in the presence of a nitrile or a ketone or mixtures thereof; at a ratio of 1 gm of the intermediate to 2-15 ml nitrile; or at a ratio of 1 gm of the intermediate to 3-15 ml ketone; in the presence of 5-80 ml water; and thereafter isolating the intermediate in crystalline form and converting the intermediate by splitting off the formyl group from the amino group attached to the thiazolyl group, to obtain the desired product cefpodoxime proxetil, in the form of a diastereoisomeric mixture in a ratio of B/(A+B) of 0.5 to 0.6.
    Type: Grant
    Filed: October 31, 2001
    Date of Patent: September 27, 2005
    Assignee: Sandoz AG
    Inventors: Julia Greil, Johannes Ludescher, Klaus Totschnig, Siegfried Wolf
  • Patent number: 6949519
    Abstract: Azithromycin in the form of a monohydrate comprising from 4.0% to 6.5% of water, a process for its preparation and its use in pharmaceutical compositions.
    Type: Grant
    Filed: November 26, 2001
    Date of Patent: September 27, 2005
    Assignee: Sandoz AG
    Inventors: Victor Centellas, José Diago, Rafael Garcia, Johannes Ludescher
  • Patent number: 6936455
    Abstract: The present invention relates to a process for the recombinant production of a desired heterologous polypeptide with a clearly defined homogenous N-terminus in a bacteria host cell. A fusion comprising a peptide with the autoproteolytic activity of an autoprotease Npro of a pestivirus and the heterologous polypeptide is initially expressed in the form of cytoplasmic inclusion bodies in the host cell, the inclusion bodies are isolated and subsequently treated so that the desired heterologous polypeptide is cleaved autoproteolytically by the Npro activity of the fusion protein.
    Type: Grant
    Filed: August 7, 2000
    Date of Patent: August 30, 2005
    Assignee: Sandoz AG
    Inventors: Günter Stempfer, Jörg Windisch, Franz Knauseder
  • Patent number: 6911472
    Abstract: A pharmaceutical composition comprising as an active ingredient an HMG-CoA reductase inhibitor and an aminosugar.
    Type: Grant
    Filed: May 3, 2002
    Date of Patent: June 28, 2005
    Assignee: Sandoz AG
    Inventors: Deepak Hegde, Sushrut Kulkarni
  • Patent number: 6869963
    Abstract: A stable pharmaceutical composition comprising about 1 wt. % to about 80 wt. % of an ACE inhibitor or a pharmaceutical acceptable salt thereof, about 1 wt. % to about 70 wt. % of an alkali or alkaline earth metal carbonate, and about 1 wt. % to about 80 wt. % of hydroxypropyl cellulose, wherein the ACE inhibitor is selected from the group consisting of quinapril, enalapril, spirapril, ramipril, perindopril, indolapril, lisinopril, alacepril, trandolapril, benazapril, libenzapril, delapril, cilazapril and combinations thereof; wherein the formation of an internal cyclization product, and/or ester hydrolysis product, and/or oxidation product, has been reduced or eliminated, and the weight percents are based on the total weight of the pharmaceutical composition.
    Type: Grant
    Filed: July 11, 2003
    Date of Patent: March 22, 2005
    Assignee: Sandoz AG
    Inventors: Ashish Anilbhai Patel, Pablo Davila
  • Patent number: 6835838
    Abstract: A method for preparing an alkali metal salt comprising: (a) condensing a disilyloxydiene with an aldehyde in the presence of a titanium (IV) catalyst in an inert solvent to form a 5(S)-hydroxy-3-ketoester; (b) reducing the 5(S)-hydroxy-3-ketoester to a 3(R),5(S)-dihydroxyester in the presence of a di(lower alkyl)methoxyborane; and (c) hydrolyzing the 3(R),5(S)-dihydroxyester in the presence of an aqueous base to form an alkali metal salt.
    Type: Grant
    Filed: January 24, 2003
    Date of Patent: December 28, 2004
    Assignee: Novartis AG
    Inventors: Guang-Pei Chen, Prasad Koteswara Kapa, Eric M. Loeser, Ulrich Beutler, Werner Zaugg, Michael John Girgis
  • Patent number: 6835829
    Abstract: Processes for the depletion of 7-ADCA in mixtures of vinyl-ACA with 7-ADCA via novel salts of vinyl-ACA or via chromatography.
    Type: Grant
    Filed: January 21, 2003
    Date of Patent: December 28, 2004
    Assignee: Sandoz GmbH
    Inventors: Johannes Ludescher, Werner Veit
  • Patent number: 6825345
    Abstract: A process for the purification of cefixime via a novel tert-octylamine salt of a cefixime intermediate of formula V which may be crystalline and which may be produced in a one-pot reaction from 7-amino-3-vinyl-ceph-3-em-4-carboxylic acid.
    Type: Grant
    Filed: September 30, 2002
    Date of Patent: November 30, 2004
    Assignee: Sandoz GmbH
    Inventors: Martin Decristoforo, Johannes Ludescher, Hubert Sturm, Werner Veit
  • Patent number: 6787649
    Abstract: A process which comprises (i) acylating a compound of formula II with a compound of formula IV to obtain a compound of formula I and (ii) deformylating said compound of formula I to obtain a compound of formula III
    Type: Grant
    Filed: February 12, 2003
    Date of Patent: September 7, 2004
    Assignee: Sandoz GmbH
    Inventors: Peter Kremminger, Johannes Ludescher, Siegfried Wolf
  • Patent number: 6784193
    Abstract: A compound of formula (I) wherein R2 is arylene or heterocyclene; or R and R2 together with the nitrogen atom to which they are attached form non-aromatic heterocyclene; and the other residues have various meanings, useful as pharmaceuticals, e.g. antimicrobials.
    Type: Grant
    Filed: January 28, 2002
    Date of Patent: August 31, 2004
    Assignee: Sandoz GmbH
    Inventors: Gerd Ascher, Heinz Berner, Johannes Hildebrandt
  • Patent number: 6777549
    Abstract: A process for the production of a compound of formula comprising i) silylating a compound of formula then reacting a resulting with a compound of formula R′BS—X′  IVB wherein R′B is hydrogen or trialkysilyl and X′ is as defined above, in the presence of a compound of formula wherein R2, R3 and R4 independently of each another are aryl or alkyl, and R5 is alkyl, perfluorinated alkyl, or aryl; and isolating the desired product.
    Type: Grant
    Filed: April 10, 2002
    Date of Patent: August 17, 2004
    Assignee: Sandoz GmbH
    Inventors: Benjamin Gerlach, Johannes Ludescher, Klaus Totschnig
  • Patent number: 6767555
    Abstract: This invention provides composition comprising a cyclosporin and a carrier medium.
    Type: Grant
    Filed: August 13, 2002
    Date of Patent: July 27, 2004
    Assignee: Novartis AG
    Inventors: Michael Ambuhl, Barbara Lückel, Barbara Haberlin, Armin Meinzer
  • Patent number: 6753445
    Abstract: A compound selected from 14—O—[(cycloalkyl-sulfanyl)acetyl]mutilins; 14—O—[(cycloalkyl-alkyl-sulfanyl)acetyl] mutilins; 14—O—[(cycloalkoxy)acetyl] mutilins; and 14—O—[(cycloalkyl-alkoxy)acetyl] mutilins and its use as a pharmaceutical.
    Type: Grant
    Filed: January 9, 2003
    Date of Patent: June 22, 2004
    Assignee: Biochemie Gesellschaft m.b.H.
    Inventors: Gerd Ascher, Heinz Berner
  • Patent number: 6740776
    Abstract: A low temperature process for preparing an aromatic acid having formula (I), said process comprising reacting an aromatic aldehyde having formula (II) with a gas having an oxygen content of 1 to 100 weight percent, based on the total weight of the gas, at a temperature of about 20° C. to less than 100° C. in the presence of a supported Group VIII metal catalyst, and a solvent having a flash point greater than 95° C. and/or a melting point less than 55° C., provided that the flash point of the solvent is greater than the reaction temperature, wherein R1 and R2 are independently selected from the group consisting of hydrogen and a C1-C8 linear, branched or cyclic alkyl group. The process of the invention yields an aromatic acid in excellent yield, and (i) does not involve the use of deleterious oxidizing agents; (ii) is essentially free of by-products; and (iii) is accomplished at a temperature of less than 100° C.
    Type: Grant
    Filed: July 15, 2002
    Date of Patent: May 25, 2004
    Assignee: Novartis AG
    Inventors: Ratna Shekhar, Michael John Girgis
  • Patent number: H2158
    Abstract: Use of the 2-amino-2,4,4-trimethylpentane salt of clavulanic acid as an intermediate in the production of pharmaceutically acceptable salts of clavulanic acid.
    Type: Grant
    Filed: May 13, 2003
    Date of Patent: June 6, 2006
    Assignee: Sandoz AG
    Inventors: Franz Krenmüller, Harald Summer