Patents by Inventor Alfons Gaston Maria De Knaep

Alfons Gaston Maria De Knaep 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).

  • Synthesis of cisapride
    Patent number: 6218542
    Abstract: A new Process of preparing cisapride, and the pharmaceutically acceptable acid addition salts thereof, by reductively aminating 1-[3-(4-fluorophenoxy)-propyl]-3-methoxy-4-piperidinone in the presence of benzylamine under hydrogen in a reaction-inert solvent, yielding 1-[3-(4-fluorophenoxy)-propyl]-3-methoxy-4-piperidinamine having a cis/trans ratio of about 93/7, which is enriched in the amount of cis-stereoisomer by converting it into its acid addition salt, by treatment with a suitable inorganic acid, in an appropriate solvent, subsequent crystallisation and conversion to its free base form by treatment with an appropriate base, yielding 1-[3-(4-fluorophenoxy)-propyl]-3-methoxy-4-piperidinamine having a cis/trans ratio of equal to or higher than 98/2.
    Type: Grant
    Filed: April 14, 1999
    Date of Patent: April 17, 2001
    Assignee: Jenssen Pharmaceutica N.V.
    Inventors: Alfons Gaston Maria De Knaep, Luc Jozef Raphael Moens, Max Rey
  • Process for preparing enantiomerically pure 6-{4-chlorophenyl) (1 H-1,2,4-triazol-1-YL) methyl}-1-methyl-1 H-benzotriazole
    Patent number: 5746840
    Abstract: A process for preparing (+)-6-?(4-chlorophenyl)(1H- 1,2,4-triazol-1-yl)methyl!-1-methyl-1H-benzotriazole comprising the resolution of (.+-.)-6-!(4-chlorophenyl)-hydrazinomethyl)-1-methyl-1H-benzotriazole and converting the appropriate enantiomerically pure hydrazine intermediate into (+)-6-?(4-chlorophenyl)(H- 1,2,4-triazol-1-yl)methyl!-1-methyl-1H-benzotriazole.
    Type: Grant
    Filed: March 28, 1997
    Date of Patent: May 5, 1998
    Assignee: Janssen Pharmaceutica, N.V.
    Inventors: Albert Louis Anna Willemsens, Walter Louis Antoine Verstappen, Alex Herman Copmans, Anna Maria Jozefa Vandendriessche, Alfons Gaston Maria De Knaep, Marc Gaston Venet
  • Process for preparing enantiomerically pure 6-[(4-chlorophenyl) (1H-1,2,4-triazol-1-yl) methyl]-1-methyl-1H-benzotrizole
    Patent number: 5663354
    Abstract: A process for preparing (+)-6-[(4-chlorophenyl)(1H-1,2,4-triazol-1-yl)methyl]-1-methyl-1H-benzotri azole comprising the resolution of (.+-.)-6-[(4-chlorophenyl)-hydrazinomethyl)-1-methyl-1H-benzotriazole and converting the appropriate enantiomerically pure hydrazine intermediate into (+)-6-[(4-chlorophenyl)(1 H-1,2,4-triazol-1-yl)methyl]-1-methyl-1H-benzotriazole.
    Type: Grant
    Filed: April 18, 1995
    Date of Patent: September 2, 1997
    Assignee: Janssen Pharmaceutica, N.V.
    Inventors: Albert Louis Anna Willemsens, Walter Louis Antoine Verstappen, Alex Herman Copmans, Anna Maria Jozefa Vandendriessche, Alfons Gaston Maria De Knaep, Marc Gaston Venet