Patents by Inventor Milan Soukup

Milan Soukup 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).

  • Patent number: 8703976
    Abstract: The present invention relates to a novel manufacturing process and novel intermediates useful in the synthesis of pharmaceutically active compound such as Aliskiren. The invention describes preparation of enantiomerically pure 8-aryloctanoic acid of formula I from a chiral compound of formula IV. Friedel-Crafts reaction of this compound of formula IV with a compound of formula III provides compound of formula II which is converted reductively in a few steps into the compound of formula V, a know intermediate in the synthesis of compound of formula I. According to the disclosed process, Aliskiren can be now prepared from commercial starting materials (Guajacol or 2-bromoanisole, cis- or trans-1,4-dichloro-2-butene and 4(S)-benzyl-3-isovaleroyl-oxazolidin-2-one) in less than 8 process steps.
    Type: Grant
    Filed: December 24, 2011
    Date of Patent: April 22, 2014
    Assignee: Milan Soukup
    Inventor: Milan Soukup
  • Patent number: 8680297
    Abstract: The present invention relates to a novel manufacturing process of pharmaceutically active compound of formula I used as a long-acting anticholinergic bronchodilator. Starting from oxalic acid derivative of formula III the invention describes preparation of a novel cyclic anhydride of formula II which is very efficient precursor in the synthesis of Tiotropium bromide (compound of formula I).
    Type: Grant
    Filed: October 6, 2011
    Date of Patent: March 25, 2014
    Assignee: Drug Process Licensing Assoc., LLC
    Inventor: Milan Soukup
  • Patent number: 8524936
    Abstract: The present invention relates to a novel manufacturing process of pharmaceutically active compound of formula I used as oral anti-diabetic drug. Starting from L-aspartic acid derivate of formula IV the invention describes preparation of the chiral (R)-?-amino acid of formula II known as a precursor in the synthesis of Sitagliptin (formula I).
    Type: Grant
    Filed: May 18, 2011
    Date of Patent: September 3, 2013
    Inventor: Milan Soukup
  • Patent number: 8466297
    Abstract: The present invention relates to a novel manufacturing process and novel intermediates useful in the synthesis of pharmaceutically active compounds of general formula I used for treatment of epilepsy, neuropathic pain, anxiety and social phobia. The invention describes preparation of enantiomerically pure (S)-Pregabalin from chiral pyrrolidin-2-one of formula IV.
    Type: Grant
    Filed: November 1, 2010
    Date of Patent: June 18, 2013
    Inventor: Milan Soukup
  • Patent number: 8450519
    Abstract: The invention relates to a process for preparing chiral octenoic acid derivatives, which constitute important intermediates in the preparation of medicament active ingredients, and also to novel intermediates which are used in the process for preparing the octenoic acid derivatives mentioned.
    Type: Grant
    Filed: March 16, 2012
    Date of Patent: May 28, 2013
    Assignee: Reuter Chemischer Apparatebau KG
    Inventors: Milan Soukup, Karl Reuter, Florian Stolz, Viktor Meier, Jofzsef Balint, Mark Kantor
  • Patent number: 8445708
    Abstract: The invention relates to a process for preparing chiral octenoic acid derivatives, which constitute important intermediates in the preparation of medicament active ingredients, and also to novel intermediates which are used in the process for preparing the octenoic acid derivatives mentioned.
    Type: Grant
    Filed: October 27, 2006
    Date of Patent: May 21, 2013
    Assignee: Reuter Chemischer Apparatebau KG
    Inventors: Milan Soukup, Karl Reuter, Florian Stolz, Viktor Meier, Jofzsef Balint, Mark Kantor
  • Publication number: 20120296100
    Abstract: The present invention relates to a novel manufacturing process and novel intermediates useful in the synthesis of pharmaceutically active compound such as Aliskiren. The invention describes preparation of enantiomerically pure 8-aryloctanoic acid of formula I from a chiral compound of formula IV. Friedel-Crafts reaction of this compound of formula IV with a compound of formula III provides compound of formula II which is converted reductively in a few steps into the compound of formula V, a know intermediate in the synthesis of compound of formula I. According to the disclosed process, Aliskiren can be now prepared from commercial starting materials (Guajacol or 2-bromoanisole, cis- or trans-1,4-dichloro-2-butene and 4(S)-benzyl-3-isovaleroyl-oxazolidin-2-one) in less than 8 process steps.
    Type: Application
    Filed: December 24, 2011
    Publication date: November 22, 2012
    Applicant: CARBODESIGN LLC
    Inventor: MILAN SOUKUP
  • Publication number: 20120178959
    Abstract: The invention relates to a process for preparing chiral octenoic acid derivatives, which constitute important intermediates in the preparation of medicament active ingredients, and also to novel intermediates which are used in the process for preparing the octenoic acid derivatives mentioned.
    Type: Application
    Filed: March 16, 2012
    Publication date: July 12, 2012
    Inventors: Milan SOUKUP, Karl Reuter, Florian Stolz, Viktor Meier, Jofzsef Balint, Mark Kantor
  • Patent number: 8207352
    Abstract: A new technical process for preparation of enantiomerically pure antifungal compounds of formula I by resolution of the racemates has been disclosed.
    Type: Grant
    Filed: October 8, 2009
    Date of Patent: June 26, 2012
    Assignee: Drug Process Licensing Associates LLC
    Inventor: Milan Soukup
  • Patent number: 8203005
    Abstract: The invention describes a novel technical process and novel intermediates useful for the manufacture of enantiomerically pure 8-aryloctanoic acids of the formula I which are pharmaceutically active compounds as rennin inhibitors.
    Type: Grant
    Filed: October 15, 2010
    Date of Patent: June 19, 2012
    Assignee: Carbo Design LLC
    Inventor: Milan Soukup
  • Publication number: 20120123125
    Abstract: The present invention relates to a novel manufacturing process of pharmaceutically active compound of formula I used as a long-acting anticholinergic bronchodilator. Starting from oxalic acid derivative of formula III the invention describes preparation of a novel cyclic anhydride of formula II which is very efficient precursor in the synthesis of Tiotropium bromide (compound of formula I).
    Type: Application
    Filed: October 6, 2011
    Publication date: May 17, 2012
    Applicant: Drug Process Licensing Associates, LLC
    Inventor: Milan SOUKUP
  • Publication number: 20120123134
    Abstract: The present invention relates to a novel manufacturing process and novel intermediates useful in the synthesis of pharmaceutically active compounds of general formula I used for treatment of epilepsy, neuropathic pain, anxiety and social phobia. The invention describes preparation of enantiomerically pure (S)-Pregabalin from chiral pyrrolidin-2-one of formula IV.
    Type: Application
    Filed: November 1, 2010
    Publication date: May 17, 2012
    Applicant: Drug Process Licensing Associates LLC
    Inventor: Milan Soukup
  • Publication number: 20120123124
    Abstract: The present invention relates to a novel manufacturing process of pharmaceutically active compound of formula I, having (6R,12aR)-configuration, used for treatment of erectile dysfunction. Starting from racemic or L-tryptophan the invention describes preparation of an enantiomerically pure intermediate of formula II which is a known precursor in the synthesis of Tadalafil (formula I).
    Type: Application
    Filed: April 22, 2011
    Publication date: May 17, 2012
    Applicant: Drug Process Licensing Associates, LLC
    Inventor: Milan Soukup
  • Publication number: 20120123144
    Abstract: The present invention relates to a novel manufacturing process of pharmaceutically active compound of formula I used as oral anti-diabetic drug. Starting from L-aspartic acid derivate of formula IV the invention describes preparation of the chiral (R)-?-amino acid of formula II known as a precursor in the synthesis of Sitagliptin (formula I).
    Type: Application
    Filed: May 18, 2011
    Publication date: May 17, 2012
    Applicant: Drug Process Licensing Associates, LLC
    Inventor: Milan Soukup
  • Publication number: 20110137047
    Abstract: The present invention relates to a novel manufacturing process and novel intermediates useful in the synthesis of pharmaceutically active compounds, especially rennin inhibitors such as Aliskiren. The invention describes a preparation of enantiomerically pure 8-aryloctanoic acids of general formula I from readily available key intermediate, chiral cis-diacid of formula II, aziridine of formula XI and a monocyclic compound of formula III.
    Type: Application
    Filed: October 15, 2010
    Publication date: June 9, 2011
    Applicant: CarboDesign LLC
    Inventor: Milan Soukup
  • Publication number: 20110105767
    Abstract: The invention describes a novel technical process and novel intermediates useful for the manufacture of enantiomerically pure 8-aryloctanoic acids of the formula I which are pharmaceutically active compounds as rennin inhibitors.
    Type: Application
    Filed: October 15, 2010
    Publication date: May 5, 2011
    Applicant: CarboDesign LLC
    Inventor: Milan Soukup
  • Publication number: 20110092706
    Abstract: The present invention relates to a novel manufacturing process and novel intermediates useful in the synthesis of pharmaceutically active compounds, especially rennin inhibitors such as Aliskiren. The invention describes a preparation of enantiomerically pure 8-aryloctanoic acids of general formula I from readily available key intermediate, a novel bicyclic compound of formula IV.
    Type: Application
    Filed: October 15, 2010
    Publication date: April 21, 2011
    Applicant: CarboDesign LLC
    Inventor: Milan Soukup
  • Publication number: 20110087030
    Abstract: A new technical process for preparation of enantiomerically pure antifungal compounds of formula I by resolution of the racemates has been disclosed.
    Type: Application
    Filed: October 8, 2009
    Publication date: April 14, 2011
    Inventor: Milan Soukup
  • Publication number: 20090221848
    Abstract: The invention relates to a process for preparing chiral octenoic acid derivatives, which constitute important intermediates in the preparation of medicament active ingredients, and also to novel intermediates which are used in the process for preparing the octenoic acid derivatives mentioned.
    Type: Application
    Filed: October 27, 2006
    Publication date: September 3, 2009
    Applicant: REUTER CHEMISCHER APPARATEBAU KG
    Inventors: Milan Soukup, Karl Reuter, Florian Stolz, Viktor Meier, Jofzsef Balint, Mark Kantor
  • Patent number: 7115643
    Abstract: Novel halophenyl derivatives of the general formula (I), wherein R1 is halogen, a leaving group or 1H-1,2,4-triazol-1-yl and R2 is ethynyl or carboxy, X1 is halogen and X2 and X3 are each independently hydrogen or halogen, and their manufacture are described. They are intermediates for manufacturing azole derivatives of the general formula (V) which are valuable medicaments useful for treating systemic mycoses.
    Type: Grant
    Filed: June 17, 2002
    Date of Patent: October 3, 2006
    Assignee: Basilea Pharmaceutica AG
    Inventor: Milan Soukup