Patents by Inventor Gerhard Jas

Gerhard Jas 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: 11584708
    Abstract: The invention relates to a method for the preparation of a 4,5-dihydroxyisoleucine derivative comprising the steps of asymmetric Claisen rearrangement of a Z-aminocrotyl-glycin ester and subsequent kinetic resolution of the product diastereomer mix by acylase, and subsequent Sharpless dihydroxylation of the resulting 2-amino-3-methylpent-4-enoic acid derivative.
    Type: Grant
    Filed: March 29, 2019
    Date of Patent: February 21, 2023
    Assignee: Heidelberg Pharma Research GmbH
    Inventors: Caroline Knittel, Mary-Ann Siegert, Roderich Süssmuth, Christoph Wink, Gerhard Jas
  • Publication number: 20210009507
    Abstract: The invention relates to a method for the preparation of a 4,5-dihydroxyisoleucine derivative comprising the steps of asymmetric Claisen rearrangement of a Z-aminocrotyl-glycin ester and subsequent kinetic resolution of the product diastereomer mix by acylase, and subsequent Sharpless dihydroxylation of the resulting 2-amino-3-methylpent-4-enoic acid derivative.
    Type: Application
    Filed: March 29, 2019
    Publication date: January 14, 2021
    Applicants: Heidelberg Pharma Research GmbH, Corden Pharma International GmbH
    Inventors: Caroline Knittel, Mary-Ann Siegert, Roderich Süssmuth, Christoph Wink, Gerhard Jas
  • Publication number: 20180297974
    Abstract: The invention relates to a process for the preparation of a ketone of a general formula 1 with X being Cl or Br, in particular with X being Cl, with Y being F, Cl, Br, I or H, in particular with Y being F, comprising the steps of: activation of a carboxylic acid by using a peptide coupling agent, coupling of the activated carboxylic acid with a malonic acid derivative providing a ?-ketoester precursor and converting the ?-ketoester precursor to the ketone of the general formula 1.
    Type: Application
    Filed: June 21, 2018
    Publication date: October 18, 2018
    Applicant: CORDON PHARMA INTERNATIONAL GmbH
    Inventors: Ilia Freifeld, Gerhard Jas, Kurt Kesseler, Richard Robert Dauer
  • Patent number: 10005755
    Abstract: The invention relates to a process for the preparation of a ketone of a general formula 1 with X being Cl or Br, in particular with X being Cl, with Y being F, Cl, Br, I or H, in particular with Y being F, comprising the steps of: activation of a carboxylic acid by using a peptide coupling agent, coupling of the activated carboxylic acid with a malonic acid derivative providing a ?-ketoester precursor and converting the ?-ketoester precursor to the ketone of the general formula 1.
    Type: Grant
    Filed: February 13, 2015
    Date of Patent: June 26, 2018
    Assignee: CORDON PHARMA INTERNATIONAL GMBH
    Inventors: Ilia Freifeld, Gerhard Jas, Kurt Kesseler, Richard Robert Dauer
  • Patent number: 9822090
    Abstract: The invention relates to a process for producing Nebivolol hydrochloride, (formula I) comprising the steps of: provision of a protected Nebivolol hydrochloride of the general formula (II), with P being an amine protecting group, and hydrogenation of said protected Nebivolol hydrochloride yielding Nebivolol hydrochloride of the formula (I).
    Type: Grant
    Filed: February 13, 2015
    Date of Patent: November 21, 2017
    Assignee: CORDEN PHARMA INTERNATIONAL GMBH
    Inventors: Alexandre Clavel, Ilia Freifeld, Gerhard Jas, Kurt Kesseler
  • Publication number: 20170183323
    Abstract: The invention relates to a process for producing Nebivolol hydrochloride, (formula I) comprising the steps of: provision of a protected Nebivolol hydrochloride of the general formula (II), with P being an amine protecting group, and hydrogenation of said protected Nebivolol hydrochloride yielding Nebivolol hydrochloride of the formula (I).
    Type: Application
    Filed: February 13, 2015
    Publication date: June 29, 2017
    Applicant: CORDON PHARMA INTERNATIONAL GmbH
    Inventors: Alexandre CLAVEL, Ilia FREIFELD, Gerhard JAS, Kurt KESSELER
  • Publication number: 20150232441
    Abstract: The invention relates to a process for the preparation of a ketone of a general formula 1 with X being Cl or Br, in particular with X being Cl, with Y being F, Cl, Br, I or H, in particular with Y being F, comprising the steps of: activation of a carboxylic acid by using a peptide coupling agent, coupling of the activated carboxylic acid with a malonic acid derivative providing a ?-ketoester precursor and converting the ?-ketoester precursor to the ketone of the general formula 1.
    Type: Application
    Filed: February 13, 2015
    Publication date: August 20, 2015
    Applicant: CORDON PHARMA INTERNATIONAL GmbH
    Inventors: Ilia Freifeld, Gerhard Jas, Kurt Kesseler, Richard Robert Dauer
  • Publication number: 20130005001
    Abstract: The present invention relates to a method for producing racemic nebivolol represented by general formula (I) from the enantiomerically-pure compounds represented by formula (IVa) and (IVb); whereby racemic nebivolol is obtained through mixing enantiomerically-pure d-nebivolol and l-nebivolol which are synthesised independent of each other as enantiomerically-pure compounds through individual coupling of the 4 enantiomerically-pure key intermediates represented by formula (IIa-d) to the corresponding precursors represented by formula (IIIa-d); whereby d-nebivolol (Ia) is obtained through coupling (IIa) to (IIIb) or (IIb) to (IIIa) and l-nebivolol (Ib) is obtained through coupling (IIc) to (IIId) or (IId) to (IIIc), and PG in the intermediates represented by formula (IIa-d) is a hydrogen atom or an amine protection group, and X in the precursors represented by formula (IIIa-d) is a halogen atom, a hydroxyl group, an acyl group, an alkylsulfonyloxy group or an arylsulfonyloxy group, whereby intermedi
    Type: Application
    Filed: January 21, 2011
    Publication date: January 3, 2013
    Inventors: Gerhard Jas, Ilia Freifeld, Kurt Kesseler
  • Patent number: 8013117
    Abstract: A process for producing a nonapeptide leuprolide and an intermediate N-protected oligopetides, wherein at least one peptide bond of the compound is formed by reacting an activated carboxylic acid and an amine component in a continuous flow.
    Type: Grant
    Filed: November 21, 2006
    Date of Patent: September 6, 2011
    Assignee: Nanokem S.A.
    Inventors: Daniel Kadzimirsz, Gerhard Jas, Volker Autze
  • Publication number: 20090005535
    Abstract: The invention relates to a process for producing the nonapeptide leuprolide and the intermediate N-protected oligopetides thereof, wherein at least one peptide bond of the compound is formed by reacting an activated carboxylic acid and an amine component in a continuous flow.
    Type: Application
    Filed: November 21, 2006
    Publication date: January 1, 2009
    Applicant: NANOKEM S.A.
    Inventors: Daniel Kadzimirzs, Gerhard Jas, Volker Autze
  • Patent number: 6583265
    Abstract: The present invention relates to novel cyclosporins, processes for their preparation, their use as pharmaceuticals and pharmaceutical compositions comprising them. The novel cyclosporins are represented by the compound of formula I or a pharmaceutically acceptable salt thereof, wherein the letters A to L represent residues of amino acids.
    Type: Grant
    Filed: January 8, 2001
    Date of Patent: June 24, 2003
    Assignee: C-Chem AG
    Inventors: Ernst Ellmerer-Müller, Dagmar Brössner, Najib Maslouh, Horst Dieter Ambrosi, Gerhard Jas, Gunter Fischer