Patents Assigned to Synthon BV
  • Process of making crystalline Type II aripiprazole
    Patent number: 7655798
    Abstract: Crystalline aripiprazole Type II can be formed without solid state heat treatment. Instead a liquid is used such as in crystallizing from a solvent, especially 2-propanol, dimethyl sulfoxide, or a combination thereof with ethyl acetate, or in a solvent mediated solid-solid transformation, typically in ethyl acetate.
    Type: Grant
    Filed: March 17, 2006
    Date of Patent: February 2, 2010
    Assignee: Synthon BV
    Inventors: Gerrit J. B. Ettema, Raymond J. H. Westheim, Faysal Kalmoua
  • Process for purification of anastrozole
    Patent number: 7655806
    Abstract: Anastrozole can be purified by crystallization from an aqueous-based solvent system. The aqueous-based solvent system can contain dilute acid, or an alcohol or both.
    Type: Grant
    Filed: May 18, 2007
    Date of Patent: February 2, 2010
    Assignee: Synthon BV
    Inventors: Jaroslav Pis, Rudolf Smrz
  • Process of making crystalline aripiprazole
    Patent number: 7642353
    Abstract: Crystalline aripiprazole Form B can be formed by crystallizing from a solvent selected from 1-propanol, 2-propanol, 1-butanol, ethyl acetate, acetonitrile or a combination thereof.
    Type: Grant
    Filed: November 18, 2005
    Date of Patent: January 5, 2010
    Assignee: Synthon BV
    Inventors: Gerrit Jan Ettema, Raymond Westheim, Faysal Kalmoua
  • Process for making montelukast and intermediates therefor
    Patent number: 7601741
    Abstract: The reaction of methylmagnesium halide is improved by the presence of a cerium (III) salt such as cerium trichloride. The reactions are typically associated with the production of montelukast, a pharmaceutically useful compound of the following formula and salts thereof. Further enhancements can be derived from certain intermediates, salts thereof and/or purification thereof before and/or after the reaction involving methylmagnesium halide.
    Type: Grant
    Filed: November 20, 2006
    Date of Patent: October 13, 2009
    Assignee: Synthon BV
    Inventors: Petr Benovsky, Lambertus Thijs, Arjanne Overeem, Jakub Castulik, Jie Zhu, Petr Bartos, Radomir Skoumal
  • Process for resolving citalopram
    Patent number: 7566793
    Abstract: The (S)-citalopram content of a mixture of (R)- and (S)-citalopram can be enriched by using L-tartaric acid as the resolving agent in the presence of formaldehyde.
    Type: Grant
    Filed: April 22, 2008
    Date of Patent: July 28, 2009
    Assignee: Synthon BV
    Inventor: Jie Zhu
  • Solid-state montelukast
    Patent number: 7553853
    Abstract: A solid form of a compound of formula 1: is provided. The compound of formula 1 can be obtained in solid state by precipitation from a solution containing the same. The compound is useful as leukotriene antagonist and can be formulated into a pharmaceutical composition that also includes a pharmaceutically acceptable excipient.
    Type: Grant
    Filed: October 8, 2004
    Date of Patent: June 30, 2009
    Assignee: Synthon BV
    Inventors: Arjanne Overeem, Dennie J. M. van den Heuvel
  • Process for making aminoalkylphenyl carbamates and intermediates therefor
    Patent number: 7531684
    Abstract: A process for making aminoalkylphenyl carbamates, especially rivastigmine, can use less severe conditions using bis(p-nitrophenyl)carbonate (IX) as a phenol activator compound.
    Type: Grant
    Filed: September 28, 2007
    Date of Patent: May 12, 2009
    Assignee: Synthon BV
    Inventors: Henar Tejedor Vinent, Arjanne Overeem, Lambertus Thijs
  • Process for making montelukast and intermediates therefor
    Patent number: 7476748
    Abstract: A process for making montelukast, a pharmaceutically useful compound of the following formula and salts thereof: using a compound of formula (11) is provided.
    Type: Grant
    Filed: November 20, 2006
    Date of Patent: January 13, 2009
    Assignee: Synthon BV
    Inventors: Petr Benovsky, Lambertus Thijs, Arjanne Overeem, Jakub Castulik, Jie Zhu, Petr Bartos, Radomir Skoumal
  • Montelukast amantadine salt
    Patent number: 7446116
    Abstract: An amantadine salt of montelukast is useful in purification of montelukast or its salts and as a pharmaceutical active ingredient.
    Type: Grant
    Filed: March 16, 2007
    Date of Patent: November 4, 2008
    Assignee: Synthon BV
    Inventors: Jiri Bartl, Frantisek Picha
  • Pharmaceutical pellets comprising tamsulosin
    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
  • Pharmaceutical compositions comprising amlodipine maleate
    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
  • Process for making amlodipine, derivatives thereof, and precursors therefor
    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
  • Process for resolution of tamsulosin and compounds, compositions, and processes associated therewith
    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
  • Reference standards for determining the purity or stability of amlodipine maleate and processes therefor
    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
  • Amlodipine salt forms and processes for preparing them
    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
  • Process for making bicalutamide and intermediates thereof
    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
  • Process for preparation of 2-amino-6 (alkyl) amino-4,5,6,7-tetrahydrobenzothiazoles
    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
  • Process for resolution of 2-amino-6-propylamino-4,5,6,7-tetrahydrobenzthiazole and compounds therefor
    Patent number: 6727367
    Abstract: A process for resolving or enriching (R,S) 2-amino-6-propylamino-4,5,6,7-tetrahydrobenzothiazole (pramipexole) into optical isomers uses a monovalent salt thereof, e.g. pramipexole monohydrochloride, as a substrate. The monovalent salt is treated with an optically active acid, e.g. with L(+)-tartaric acid, to yield a diastereomeric mixed salt. The mixed salt is subjected to fractional crystallization to yield an optically enriched mixed salt. The mixed salt can be treated with base to liberate the desired isomer of pramipexole.
    Type: Grant
    Filed: September 18, 2001
    Date of Patent: April 27, 2004
    Assignee: Synthon BV
    Inventor: Karel Pospisilik
  • Venlafaxine besylate
    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
  • Low water-soluble venlafaxine salts
    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