Patents by Inventor Karel Pospisilik

Karel Pospisilik has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).

  • 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
  • Process for making desvenlafaxine
    Patent number: 7491848
    Abstract: Desvenlafaxine is formed from venlafaxine by the use of a demethylating agent comprising a metal sulfide, such as sodium sulfide, and optionally selenium.
    Type: Grant
    Filed: December 20, 2006
    Date of Patent: February 17, 2009
    Assignee: Synthon IP Inc.
    Inventors: Karel Pospisilik, Lambertus Thijs
  • Process for making duloxetine and related compounds
    Publication number: 20080171887
    Abstract: A compound of formula 10 is useful in making duloxetine.
    Type: Application
    Filed: December 20, 2007
    Publication date: July 17, 2008
    Inventors: Karel Pospisilik, Bohumil Dymacek
  • Process for making desvenlafaxine
    Publication number: 20070299283
    Abstract: Desvenlafaxine is formed from venlafaxine by the use of a demethylating agent comprising a metal sulfide, such as sodium sulfide, and optionally selenium.
    Type: Application
    Filed: December 20, 2006
    Publication date: December 27, 2007
    Inventors: Karel Pospisilik, Lambertus Thijs
  • PROCESS FOR MAKING DONEPEZIL
    Publication number: 20070135644
    Abstract: A process for making donepezil using a new intermediate salt of formula (VIIIa), especially the tosylate, can achieve good yields.
    Type: Application
    Filed: November 20, 2006
    Publication date: June 14, 2007
    Inventor: Karel Pospisilik
  • Stabilised pharmaceutical compositions on the basis of polyoxyethlated castor oil and method for manufacturing the same
    Publication number: 20050142225
    Abstract: The invention relates to a stabilised pharmaceutical composition comprising a pharmaceutically active substance poorly soluble in water, a solubilising agent with a low content of both basic and acidlic compounds and a polar organic solvent, in particular a stabilised injection concentrate, methods for preparing such stabilised pharmaceutical compositions and the use of a solubilising agent with a low content of both basic and acidic compounds to stabilise pharmaceutical compositions for pharmaceutically active substances.
    Type: Application
    Filed: May 16, 2003
    Publication date: June 30, 2005
    Applicant: Pliva-Lachema A.S.
    Inventors: Vladimir Kysilka, Libuse Zatloukalova, Borek Zaludek, Karel Pospisilik, Mario Cigankova, Martin Kubat, Ales Cirkva
  • Processes for making thiazolidinedione derivatives and compounds thereof
    Publication number: 20050059708
    Abstract: A compound of the formula: wherein A represents a ring group connected to the oxygen atom by a C1 to C6 hydrocarbon chain, R is hydrogen or a C1-C4 alkyl, and Q is hydrogen, or an amine protecting group such as acetyl, trifluoroacetyl, benzoyl, benzyl, or trityl, is useful in making thiazolidinedione derivatives such as pioglitazone, rosiglitazone and troglitazone.
    Type: Application
    Filed: May 11, 2004
    Publication date: March 17, 2005
    Inventors: Karel Pospisilik, Frantisek Picha, Jie Zhu
  • 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
  • Process for resolution of 2-amino-6-propylamino-4,5,6,7-tetrahydrobenzthiazole and compounds therefor
    Publication number: 20040068119
    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: Application
    Filed: October 6, 2003
    Publication date: April 8, 2004
    Inventor: Karel Pospisilik
  • Process for preparation of 2-amino-6 (alkyl) amino-4,5,6,7-tetrahydrobenzothiazoles
    Publication number: 20040029936
    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: Application
    Filed: August 7, 2003
    Publication date: February 12, 2004
    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
    Publication number: 20020103240
    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: Application
    Filed: September 18, 2001
    Publication date: August 1, 2002
    Inventor: Karel Pospisilik