Patents by Inventor Martin Karpf

Martin Karpf 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: 7514580
    Abstract: The present invention relates to a process for the preparation of a 4,5-diamino shikimic acid derivative of formula and pharmaceutically acceptable addition salts thereof wherein R1, R1? are independent of each other H or alkyl, R2 is an alkyl and R3, R4 are independent of each other H or an alkanoyl, with the proviso that not both R3 and R4 are H. 4,5-diamino shikimic acid derivatives of formula I, especially the (3R,4R,5S)-5-amino-4-acetylamino-3-(1-ethyl-propoxy)-cyclohex-1-ene-carboxylic acid ethyl ester and its pharmaceutically acceptable additional salts are potent inhibitors of viral neuraminidase.
    Type: Grant
    Filed: August 30, 2005
    Date of Patent: April 7, 2009
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Martin Karpf, Rene Trussardi
  • Publication number: 20060047002
    Abstract: The present invention relates to a process for the preparation of a 4,5-diamino shikimic acid derivative of formula and pharmaceutically acceptable addition salts thereof wherein R1, R1? are independent of each other H or alkyl, R2 is an alkyl and R3, R4 are independent of each other H or an alkanoyl, with the proviso that not both R3 and R4 are H. 4,5-diamino shikimic acid derivatives of formula I, especially the (3R,4R,5S)-5-amino-4-acetylamino-3-(1-ethyl-propoxy)-cyclohex-1-ene-carboxylic acid ethyl ester and its pharmaceutically acceptable additional salts are potent inhibitors of viral neuraminidase.
    Type: Application
    Filed: August 30, 2005
    Publication date: March 2, 2006
    Inventors: Martin Karpf, Rene Trussardi
  • Patent number: 6939986
    Abstract: The invention provides a multistep process for preparing 1,2-diamino compounds and pharmaceutically acceptable addition salts thereof from 1,2-epoxides.
    Type: Grant
    Filed: February 22, 2002
    Date of Patent: September 6, 2005
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Martin Karpf, René Trussardi
  • Patent number: 6562977
    Abstract: The present invention is concerned with mixed anhydrides. The mixed anhydrides are prepared by adding an adjuvant base to a mixture of acid and reactive acid derivative. The mixed anhydrides play an role primarily in activating and coupling reactions.
    Type: Grant
    Filed: December 6, 2001
    Date of Patent: May 13, 2003
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Martin Karpf, René Trussardi
  • Patent number: 6489479
    Abstract: The present invention is concerned with an improved process for the manufacture of mixed anhydrides. The process comprises adding an adjuvant base to a mixture of acid and reactive acid derivative. It is especially suitable for use in the synthesis of peptides and/or for the manufacture of pharmaceutically active substances or corresponding intermediates.
    Type: Grant
    Filed: July 22, 1999
    Date of Patent: December 3, 2002
    Assignee: Hoffman-La Roche Inc.
    Inventors: Martin Karpf, René Trussardi
  • Patent number: 6437171
    Abstract: The invention provides a multistep process for preparing 1,2-diamino compounds of formula wherein R1, R1′, R2, R2′, R3 and R4 have the meaning given in the specification and pharmaceutically acceptable addition salts thereof, from 1,2-epoxides of formula wherein R1, R′, R2 and R2′ have the meaning given in the specification.
    Type: Grant
    Filed: June 8, 2000
    Date of Patent: August 20, 2002
    Assignee: Hoffman-La Roche Inc.
    Inventors: Martin Karpf, René Trussardi
  • Publication number: 20020095040
    Abstract: The invention provides a multistep process for preparing 1,2-diamino compounds and pharmaceutically acceptable addition salts thereof from 1,2-epoxides.
    Type: Application
    Filed: February 22, 2002
    Publication date: July 18, 2002
    Inventors: Martin Karpf, Rene Trussardi
  • Publication number: 20020077481
    Abstract: The present invention is concerned with an improved process for the manufacture of mixed anhydrides. The process comprises adding an adjuvant base to a mixture of acid and reactive acid derivative. It is especially suitable for use in the synthesis of peptides and/or for the manufacture of pharmaceutically active substances or corresponding intermediates.
    Type: Application
    Filed: December 6, 2001
    Publication date: June 20, 2002
    Inventors: Martin Karpf, Rene Trussardi
  • Patent number: 6403824
    Abstract: The invention provides a multistep synthesis for the preparation of 4,5-diamino shikimic acid derivatives of formula wherein R1, R2, R3 and R4 are defined in the specification, starting from furan. 4,5-Diamino shikimic acid derivatives are potent inhibitors of viral neuraminidase.
    Type: Grant
    Filed: February 6, 2001
    Date of Patent: June 11, 2002
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Stefan Abrecht, Martin Karpf, René Trussardi, Beat Wirz
  • Publication number: 20020006960
    Abstract: The invention provides a multistep synthesis for the preparation of 4,5-diamino shikimic acid derivatives of formula 1
    Type: Application
    Filed: February 6, 2001
    Publication date: January 17, 2002
    Inventors: Stefan Abrecht, Martin Karpf, Rene Trussardi, Beat Wirz
  • Patent number: 5892040
    Abstract: A process for preparing a compound of formula (I) or a phamaceutically-acceptable salt thereof, comprising: 1) reacting a compound. of formula (III), in which R is a straight or branched chain alkyl having from one to four carbon atoms, with an alkali metal hydroxide in an aqueous medium at a temperature of about 80.degree. to 120.degree. C. and time of about 20 to 100 hours to form a reaction product; 2) cyclizing the reaction product of step 1) with formic acid and formaldehyde to form a formiate compound; and 3) neutralizing the formiate compound of step 2) with an aqueous base.
    Type: Grant
    Filed: January 4, 1996
    Date of Patent: April 6, 1999
    Assignee: Pfizer. Inc
    Inventors: Martin Karpf, Rene Trussardi
  • Patent number: 5481008
    Abstract: A catalytic process for the manufacture of optically active compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2 are alkyl, which is optionally interrupted by an O atom in a position other than the .alpha.-or .beta.-position, or optionally substituted benzyl,R.sup.3 is hydrogen, lower alkyl, optionally substituted benzyl, --CO--R.sup.4, --COOR.sup.4 or --CONR.sub.2.sup.4, andR.sup.4 is lower alkyl or aryl,comprising asymmetrically hydrogenating a compound of the formula ##STR2## wherein R.sup.1, R.sup.2 and R.sup.3 have the above significance, in the presence of a complex of an optically active, preferably atropisomeric, diphospine ligand with a metal of Group VIII.
    Type: Grant
    Filed: August 31, 1994
    Date of Patent: January 2, 1996
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Emil A. Broger, Martin Karpf, Ulrich Zutter
  • Patent number: 5399720
    Abstract: The invention relates to a novel process for producing a compound having the formula ##STR1## wherein R.sup.1, R.sup.2 and X are described herein, via corresponding .beta.-keto- and .beta.-hydroxy-.delta.-lactones, as well as novel intermediates which occur in the process.
    Type: Grant
    Filed: June 15, 1993
    Date of Patent: March 21, 1995
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Martin Karpf, Ulrich Zutter
  • Patent number: 5245056
    Abstract: The invention relates to a novel process for producing a compound having the formula ##STR1## wherein R.sup.1, R.sup.2 and X are described herein, via wherein R corresponding .beta.-keto- and .beta.-hydroxy-.delta.-lactones, as well as novel intermediates which occur in the process.
    Type: Grant
    Filed: February 11, 1991
    Date of Patent: September 14, 1993
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Martin Karpf, Ulrich Zutter
  • Patent number: 4908470
    Abstract: Methyl 4-dimethylamino-3,5-dimethoxybenzoate, an intermediate in the preparation of the antibacterially active aditoprim, is obtained from 4-amino-3,5-dibromobenzoic acid by replacement of the bromine atoms by methoxy groups and subsequent methylation.
    Type: Grant
    Filed: November 30, 1988
    Date of Patent: March 13, 1990
    Assignee: Hoffman-La Roche Inc.
    Inventors: Alfredo Guerrato, Martin Karpf, Hanny K. Berger, Ivan Kompis, Markus Schlageter