Patents Represented by Attorney Mark R. Buscher
  • Patent number: 7230016
    Abstract: Water-soluble salts of pioglitazone especially pioglitazone sulfate are useful in pharmaceutical applications.
    Type: Grant
    Filed: May 11, 2004
    Date of Patent: June 12, 2007
    Assignee: Synthon IP Inc.
    Inventors: Jie Zhu, Frantisek Picha
  • Patent number: 7217822
    Abstract: A process for making cabergoline uses silyl-protecting agents to protect the indole nitrogen atom.
    Type: Grant
    Filed: March 17, 2006
    Date of Patent: May 15, 2007
    Assignee: Synthon IP Inc.
    Inventors: Jorge Humberto Zenon Comin, Gustavo Ariel Revelli, Fernando Gabriel Bardi
  • Patent number: 7199247
    Abstract: A derivative of amlodipine having the following formula is useful as a pharmaceutical, either alone or in combination with amlodipine, in treating angina and hypertension.
    Type: Grant
    Filed: August 25, 2006
    Date of Patent: April 3, 2007
    Assignee: Synthon IP Inc.
    Inventors: Jacobus M. Lemmens, Theodorus H. A. Peters, Franciscus B. G. Benneker
  • Patent number: 7186854
    Abstract: Bicalutamide and/or its intermediates are made by the use of p-fluorobenzenesulfinic acid salt as a reagent.
    Type: Grant
    Filed: October 10, 2003
    Date of Patent: March 6, 2007
    Assignee: Synthon IP Inc.
    Inventors: Lambertus Thijs, Rolf Keltjens, Gerrit J. B. Ettema
  • Patent number: 7115638
    Abstract: A derivative of amlodipine having the following formula is useful as a pharmaceutical, either alone or in combination with amlodipine, in treating angina and hypertension
    Type: Grant
    Filed: May 12, 2003
    Date of Patent: October 3, 2006
    Assignee: Synthon IP Inc.
    Inventors: Jacobus M. Lemmens, Theodorus H. A. Peters, Franciscus B. G. Benneker
  • Patent number: 7041834
    Abstract: A process useful for making ondansetron that comprises reacting a carbazolone in a reaction mixture comprising a carbazolone of formula (2), a formaldehyde or precursor thereof, and an amine of formula (3) in a non-aqueous polar solvent and in the presence of a water binding agent. The reaction product(s) can be reacted with an amine of formula (5) to form ondansetron.
    Type: Grant
    Filed: January 23, 2004
    Date of Patent: May 9, 2006
    Assignee: Synthon IP Inc.
    Inventors: Dusan Hesoun, Jiri Hykl
  • Patent number: 7018658
    Abstract: Tamsulosin pellets having an advantageous release profile are formed. The pellets have an enteric coating and release less than 10% of the tamsulosin in two hours in SGF.
    Type: Grant
    Filed: November 14, 2002
    Date of Patent: March 28, 2006
    Assignee: Synthon BV
    Inventor: Johannes J. Platteeuw
  • Patent number: 6965051
    Abstract: Optically impure tamsulosin including racemic tamsulosin can be resolved into optically pure (R)- or (S)-tamsulosin by the use of diastereomeric sulfonate salts of tamsulosin in a fractional crystallization technique. Racemic tamsulosin free base is a useful starting material for the resolution process and a method of obtaining the same in solid form, including two crystalline polymorphic forms, is also provided.
    Type: Grant
    Filed: November 15, 2004
    Date of Patent: November 15, 2005
    Assignee: Synthon IP Inc.
    Inventors: Hans J. Hoorn, Theodorus H. A. Peters, Jaroslav Pis, Radim Scigel
  • Patent number: 6919087
    Abstract: An amlodipine maleate pharmaceutical composition is provided with good stability when formulated with a pH within the range of 5.5 to 7, when measured as a 20 wt % aqueous slurry. The stability can also be aided by making the pharmaceutical composition from amlodipine maleate particles having an average particle size of greater than 20 microns, preferably greater than 100 microns.
    Type: Grant
    Filed: August 27, 2001
    Date of Patent: July 19, 2005
    Assignee: Synthon BV
    Inventors: Jacobus M. Lemmens, Frans van Dalen, Arlette Vanderheijden
  • Patent number: 6900327
    Abstract: The invention relates to a compound, and pharmaceutically acceptable salts, having the formula I: wherein: R represents an alkyl or alkynyl group having 1-4 carbon atoms, or a phenyl group optionally substituted by C1-4 alkyl, alkylthio, alkoxy, halogen, nitro, acylamino, methylsulfonyl or methylenedioxy, or represents tetrahydronaphthyl, R1 represents hydrogen, trifluoro (C1-4) alkyl, alkyl or alkynyl, X represents hydrogen, alkyl having 1-4 carbon atoms, alkoxy, trifluoroalkyl, hydroxy, halogen, methylthio or aralkoxy, R2 represents: a C1-C10 alkyl group, a phenyl group optionally substituted by one or more of the following groups: a C1-C10 alkyl group, a halogen group, a nitro group, hydroxy group, and/or an alkoxy group.
    Type: Grant
    Filed: May 16, 2001
    Date of Patent: May 31, 2005
    Assignee: Synthon BCT Technologies, LLC
    Inventors: Franciscus Bernardus Gemma Benneker, Frans Van Dalen, Jacobus Maria Lemmens, Theodorus Hendricus Antonium Peters, Frantisek Picha
  • Patent number: 6858738
    Abstract: Amlodipine and related analogues thereof are prepared by the following general reaction scheme: R1 and R2 each independently represent a C1-C4 alkyl group. The process provides for the formation of compounds of formula (1) in good yield and purity. Further, the compounds of formula (1) can be used as calcium channel blockers or as reference standards or reference markers for checking the purity of amlodipine.
    Type: Grant
    Filed: May 8, 2003
    Date of Patent: February 22, 2005
    Assignee: Synthon BV
    Inventors: Theodorus H. A. Peters, Franciscus B. G. Benneker, Pavel Slanina, Jiri Bartl
  • Patent number: 6835853
    Abstract: Optically impure tamsulosin including racemic tamsulosin can be resolved into optically pure (R)- or (S)-tamsulosin by the use of diastereomeric sulfonate salts of tamsulosin in a fractional crystallization technique. Racemic tamsulosin free base is a useful starting material for the resolution process and a method of obtaining the same in solid form, including two crystalline polymorphic forms, is also provided.
    Type: Grant
    Filed: July 31, 2002
    Date of Patent: December 28, 2004
    Assignee: Synthon BV
    Inventors: Hans J Hoorn, Theodorus H. A. Peters, Jaroslav Pis, Radim Scigel
  • Patent number: 6830933
    Abstract: Amlodipine aspartate and amlodipine maleamide are used as reference standards or markers in determining the purity of amlodipine maleate substances and products.
    Type: Grant
    Filed: August 27, 2001
    Date of Patent: December 14, 2004
    Assignee: Synthon BV
    Inventors: Jacobus M Lemmens, Theodorus H. A. Peters, Peter F. A. Bakker, Frantisek Picha
  • Patent number: 6828339
    Abstract: Amlodipine besylate forms are described, including amlodipine besylate hydrates and novel amlodipine besylate anhydrates. A method of making various amlodipine besylate forms from an aqueous medium as well as the use of the same as a calcium channel blocker are described.
    Type: Grant
    Filed: November 20, 2002
    Date of Patent: December 7, 2004
    Assignee: Synthon BV
    Inventors: Gerrit J. B. Ettema, Hans Hoorn, Jacobus M. Lemmens
  • Patent number: 6818766
    Abstract: Bicalutamide and/or its intermediates are made by the use of p-fluorobenzenesulfinic acid salt as a reagent.
    Type: Grant
    Filed: October 2, 2002
    Date of Patent: November 16, 2004
    Assignee: Synthon BV
    Inventors: Lambertus Thijs, Rolf Keltjens, Gerrit Jan Bouke Ettema
  • Patent number: 6770761
    Abstract: A new process to obtain pramipexole and related products is described. The process involves the reaction of new compounds of formula (6), wherein R is hydrogen or acyl group, R3 and R4 are either the same and each of them represents an alkoxy group of 1-4 carbons or they together form a C2-C5 alkylenedioxy group or an oxo-group, with an alkylamine in the presence of a reducing agent or a hydrogen gas with hydrogenation catalyst. A process to obtain new compounds of formula (6) is also described.
    Type: Grant
    Filed: August 7, 2003
    Date of Patent: August 3, 2004
    Assignee: Synthon BV
    Inventors: Karel Pospisilik, Hans Jan Hoorn, Theodorus Hendricus Antonius Peters, Jacobus Maria Lemmens
  • Patent number: 6717015
    Abstract: Venlafaxine besylate compounds provide certain advantages over venlafaxine hydrochloride and are useful in forming pharmaceutical compositions and n treating venlafaxine-treatable diseases and conditions. Venlafaxine besylate can be easily formulated into an extended release dosage form including a hydrogel tablet as well as other matrix-based tablet compositions. A preferred tablet making process involves hot melt granulation.
    Type: Grant
    Filed: March 27, 2003
    Date of Patent: April 6, 2004
    Assignee: Synthon BV
    Inventors: Rolf Keltjens, Johannes Jan Platteeuw, Juan Cucala Escoi, Inocencia Margallo Lana, Frantisek Picha, Montserrat Gallego Luengo
  • Patent number: 6703408
    Abstract: A compound or composition comprising N-formyl paroxetine of formula (1) is useful as a pharmaceutical and as a synthetic intermediate. The N-formyl paroxetine can be an impurity in paroxetine substances and methods of assaying for such an impurity are also useful.
    Type: Grant
    Filed: October 21, 2002
    Date of Patent: March 9, 2004
    Assignee: Synthon BCT Technologies, LLC
    Inventors: Hans J. Hoorn, Theodorus H. A. Peters, Frantisek Picha
  • Patent number: 6696496
    Abstract: Low water soluble salts of venlafaxine, especially venlafaxine maleate, are provided. Such salts can provide a variety of dosage forms including hydrogel-based extended release dosage forms.
    Type: Grant
    Filed: March 27, 2003
    Date of Patent: February 24, 2004
    Assignee: Synthon BV
    Inventors: Marinus J. M. Oosterbaan, Rolf Keltjens
  • Patent number: 6686473
    Abstract: The synthesis of paroxetine can be made more convenient by using a solvent system comprising an aliphatic alcohol and a hydrocarbon co-solvent. The solvent system is used particularly in the hydrolysis of paroxetine phenylcarbamate and preferably uses butanol and toluene as the system.
    Type: Grant
    Filed: February 15, 2002
    Date of Patent: February 3, 2004
    Assignee: Synthon BCT Technologies, LLC
    Inventors: Jacobus M. Lemmens, Theodorus H. A. Peters, Frantisek Picha