Patents Assigned to Synthon BV
  • PHARMACEUTICAL COMPOSITION COMPRISING POMALIDOMIDE
    Publication number: 20190183805
    Abstract: The present invention relates to a pharmaceutical composition comprising pomalidomide, maltodextrin and a filler, wherein the weight ratio of maltodextrin to filler ranges from 1:1 to 1:2. The invention further relates to the use of said pharmaceutical composition as medicament in the treatment of multiple myeloma.
    Type: Application
    Filed: July 28, 2017
    Publication date: June 20, 2019
    Applicant: Synthon BV
    Inventors: Sonia GARCIA JIMENEZ, Luis NOGUEIRAS NIETO, Lisardo ALVAREZ FERNANDEZ, Jose VELADA CALZADA
  • Process for purifying a polymer mixture
    Patent number: 9617313
    Abstract: A process of purifying copolymer peptides such as COP-1 polypeptides by ultrafiltration can be improved by treating the polypeptide solution with an acid before, or during the early stages of, the ultrafiltration. By adding the acid and/or forming an acid addition salts of the polypeptide before ultrafiltration is conducted permits for faster ultrafiltration. Likewise, adding the acid in the ultrafiltration process but before polypeptide precipitation or clogging occurs can also improve the efficiency/convenience of the ultrafiltration step.
    Type: Grant
    Filed: December 23, 2009
    Date of Patent: April 11, 2017
    Assignee: Synthon BV
    Inventor: Jordy Luten
  • Process for making bortezomib and intermediates for the process
    Patent number: 8884009
    Abstract: The invention relates to processes of making bortezomib of formula (1) enantiomers thereof and/or intermediates thereof, comprising at least one step of coupling a carboxylic acid with an amine, wherein the coupling step is performed in a presence of the compound of formula (8), wherein A is C1-C6 alkyl group, preferably wherein A is n-propyl group.
    Type: Grant
    Filed: October 14, 2010
    Date of Patent: November 11, 2014
    Assignee: Synthon BV
    Inventors: Jakub Castulik, Miroslav Zabadal
  • Pharmaceutical tablets of crystalline type II aripiprazole
    Patent number: 8529949
    Abstract: Crystalline aripiprazole Type II can be formulated into pharmaceutical tablets having reduced dissolution profile variability upon storage.
    Type: Grant
    Filed: March 17, 2006
    Date of Patent: September 10, 2013
    Assignee: Synthon BV
    Inventors: Gerrit J. B. Ettema, Raymond J. H. Westheim, Faysal Kalmoua, Korinde Annemarie Jansen, Farid Abedin Dorkoosh
  • PROCESS FOR MAKING BORTEZOMIB AND INTERMEDIATES FOR THE PROCESS
    Publication number: 20130203988
    Abstract: The invention relates to processes of making bortezomib of formula (1) enantiomers thereof and/or intermediates thereof, comprising at least one step of coupling a carboxylic acid with an amine, wherein the coupling step is performed in a presence of the compound of formula (8), wherein A is C1-C6 alkyl group, preferably wherein A is n-propyl group.
    Type: Application
    Filed: October 14, 2010
    Publication date: August 8, 2013
    Applicant: Synthon BV
    Inventors: Jakub Castulik, Miroslav Zabadal
  • Low dose controlled release tablet
    Patent number: 8465770
    Abstract: Low dose pharmaceuticals can be delivered for a prolonged period using a tablet-in-tablet design wherein the drug is contained in a controlled release matrix in the outer compression coating layer but not in the inner tablet core.
    Type: Grant
    Filed: December 10, 2009
    Date of Patent: June 18, 2013
    Assignee: Synthon BV
    Inventors: Korinde Annemarie Jansen, Dirk Pamperin
  • Hydrates of erlotinib hydrochloride
    Patent number: 8372856
    Abstract: Erlotinib hydrochloride hydrate is formed from an aqueous solution and is useful as a pharmaceutical and as a purification intermediate.
    Type: Grant
    Filed: October 25, 2007
    Date of Patent: February 12, 2013
    Assignee: Synthon BV
    Inventor: Raymond J. H. Westheim
  • Zolpidem tablets
    Patent number: 8148393
    Abstract: A zolpidem tablet having modified release is designed as a tablet-in-tablet dosage form.
    Type: Grant
    Filed: November 20, 2006
    Date of Patent: April 3, 2012
    Assignee: Synthon BV
    Inventors: Frans van Dalen, Korinde Annemarie Jansen, Farid Abedin Dorkoosh
  • Process of making crystalline type II aripiprazole
    Patent number: 8093387
    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: December 24, 2009
    Date of Patent: January 10, 2012
    Assignee: Synthon BV
    Inventors: Gerrit J. B. Ettema, Raymond J. H. Westheim, Faysal Kalmoua
  • Tablet composition with a prolonged release of tamsulosin
    Patent number: 8030355
    Abstract: A tamsulosin controlled release tablet is formed using a water-swellable matrix-forming composition as a release controlling mechanism. The matrix forming composition comprises (i) a pH-sensitive swellable hydrophilic polymer, which is a cross-linked polyacrylic acid polymer, and (ii) a pH-insensitive swellable hydrophilic polymer. The tablet optionally contains a water insoluble binder as well.
    Type: Grant
    Filed: May 17, 2007
    Date of Patent: October 4, 2011
    Assignee: Synthon BV
    Inventors: Korinde Annemarie Jansen, Farid Abedin Dorkoosh
  • Process for making 1-hydroxyalkylidene-1,1-biphosphonic acids
    Patent number: 8026388
    Abstract: Synthesis of biphosphonate compounds can be advantageously carried out in a solvent/diluent comprising a compound of formula (3) wherein R is hydrogen or a C1-C6 alkyl group; each of R1 is a C1-C6 alkyl group or both R1 groups are linked to form a C1-C3 alkylene group; and R2 is hydrogen, a C1-C6 alkyl group, a C1-C6 alkoxy group, or is linked together with R to form a C3-C7 carbon ring.
    Type: Grant
    Filed: July 10, 2009
    Date of Patent: September 27, 2011
    Assignee: Synthon BV
    Inventor: Jiri Bartl
  • Process for making n-(diphenylmethyl)piperazines
    Patent number: 7989623
    Abstract: The compound of formula (8), in racemic or single enantiomeric form, is useful in making N-(diphenylmethyl)-piperazines such as cetirizine and levocetrizine. wherein Z is preferably phenyl.
    Type: Grant
    Filed: November 21, 2008
    Date of Patent: August 2, 2011
    Assignee: Synthon BV
    Inventor: Jie Zhu
  • Synthesis of paliperidone
    Patent number: 7977480
    Abstract: A 9-hydroxy or 9-acyloxy group can be added to a pyridopyrimidinone ring structure by a process comprising acylating a compound of formula (5) under Vilsmeier-Haack or Friedel-Crafts conditions to form a compound (6); and transforming with a peroxo-compound to obtain the compound (1). R represents hydrogen or a C1-C20 acyl group. The process is useful in the synthesis of paliperidone and derivatives.
    Type: Grant
    Filed: December 10, 2008
    Date of Patent: July 12, 2011
    Assignee: Synthon BV
    Inventors: Jiri Bartl, Jozef Krajcovic, Petr Benovsky
  • Pharmaceutical composition of quetiapine fumarate
    Patent number: 7959948
    Abstract: A pharmaceutical composition comprising (i) quetiapine or a pharmaceutically acceptable salt thereof, especially quetiapine fumarate; (ii) a mixed excipient comprising an intimate admixture of polyvinylacetate and polyvinylpyrrolidone in a weight ratio from 5:2 to 10:2; and, optionally (iii) an acid especially fumaric acid.
    Type: Grant
    Filed: March 7, 2008
    Date of Patent: June 14, 2011
    Assignee: Synthon BV
    Inventor: Korinde Annemarie Jansen
  • Paliperidone ketone
    Patent number: 7932385
    Abstract: A compound of formula (7.2) or an acid addition salt thereof. The compound can be used as a reference standard for monitoring the presence thereof in a paliperidone sample, including monitoring the completion of a paliperidone reaction. Reduction in the amount of the compound in paliperidone can be achieved by crystallization in the presence of a hydride reductant.
    Type: Grant
    Filed: July 10, 2009
    Date of Patent: April 26, 2011
    Assignee: Synthon BV
    Inventors: Jozef Krajcovic, Jiri Bartl, Petr Benovsky
  • Crystalline erlotinib
    Patent number: 7928114
    Abstract: Crystalline Forms of erlotinib are made. The crystalline materials are useful as pharmaceutical active agents in treating various cancers as well as in forming erlotinib salts.
    Type: Grant
    Filed: July 27, 2007
    Date of Patent: April 19, 2011
    Assignee: Synthon BV
    Inventor: Raymond J. H. Westheim
  • Process for making duloxetine and related compounds
    Patent number: 7928250
    Abstract: A compound of formula 10 is useful in making duloxetine.
    Type: Grant
    Filed: December 20, 2007
    Date of Patent: April 19, 2011
    Assignee: Synthon BV
    Inventors: Karel Pospisilik, Bohumil Dymacek
  • Crystalline aripiprazole solvates
    Patent number: 7902198
    Abstract: Alcoholates of aripiprazole are useful as pharmaceuticals and/or as intermediates in making aripiprazole Form A or Form B.
    Type: Grant
    Filed: November 18, 2005
    Date of Patent: March 8, 2011
    Assignee: Synthon BV
    Inventors: Gerrit Jan Ettema, Raymond Westheim, Faysal Kalmoua
  • Process for making asenapine
    Patent number: 7875729
    Abstract: Asenapine and related trans-isomer bicyclic compounds can be obtained by reducing a compound of formula (C) to preferentially form a trans-isomer compound of formula (D), followed by subsequent ring closure to form a compound of formula (B) such as asenapine.
    Type: Grant
    Filed: December 21, 2007
    Date of Patent: January 25, 2011
    Assignee: Synthon BV
    Inventors: Jie Zhu, Rolf Keltjens, Judith Firet
  • Process for making montelukast and intermediates therefor
    Patent number: 7786138
    Abstract: A compound of the following formula wherein R? is a straight or branched C1-C4 alkyl group is useful in processes associated with the synthesis of montelukast and its salts.
    Type: Grant
    Filed: November 20, 2006
    Date of Patent: August 31, 2010
    Assignee: Synthon BV
    Inventors: Petr Benovsky, Lambertus Thijs, Arjanne Overeem, Jakub Castulik, Jie Zhu, Petr Bartos, Radomir Skoumal