Patents by Inventor Gerhard Kretzschmar

Gerhard Kretzschmar 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: 10112973
    Abstract: An enantioselective process for the production of (2S,3aS,6aS)-cyclopenta[b]pyrrole-2-carboxylic acid and its conversion into Ramipril is provided.
    Type: Grant
    Filed: June 8, 2015
    Date of Patent: October 30, 2018
    Assignee: SANOFI-AVENTIS DEUTSCHLAND GMBH
    Inventors: Gerhard Kretzschmar, Jan Oehme, Kai Rossen
  • Publication number: 20170158733
    Abstract: An enantioselective process for the production of (2S,3aS,6aS)-cyclopenta[b]pyrrole-2-carboxylic acid and its conversion into Ramipril is provided.
    Type: Application
    Filed: June 8, 2015
    Publication date: June 8, 2017
    Applicant: SANOFI-AVENTIS DEUTSCHLAND GMBH
    Inventors: Gerhard KRETZSCHMAR, Jan OEHME, Kai ROSSEN
  • Patent number: 8901114
    Abstract: The invention relates to the compounds of formula (I) and physiologically acceptable salts thereof. The compounds are suitable, e.g., for treating hyperglycemia.
    Type: Grant
    Filed: March 7, 2012
    Date of Patent: December 2, 2014
    Assignee: Sanofi
    Inventors: Thomas Boehme, Christian Engel, Stefan Guessregen, Torsten Haack, Gerhard Kretzschmar, Kurt Ritter, Georg Tschank
  • Patent number: 8674121
    Abstract: A process for the production of 2-alkyl-3-aroyl-5-nitrobenzofurans by acylation of 2-(2-hydroxy-5-nitrophenyl)-1-aryl-ethanones and subsequent treatment of the esters with combinations of bases and proton acids or Lewis acids. This process can be used for the production of Dronedarone. Furthermore, novel intermediates for the manufacture of Dronedarone are provided.
    Type: Grant
    Filed: May 26, 2010
    Date of Patent: March 18, 2014
    Assignee: SANOFI
    Inventors: Gerhard Kretzschmar, Volker Kraft, Thomas Olpp, Kai Rossen
  • Patent number: 8658808
    Abstract: A process for the production of Dronedarone intermediates of the formula (I), by acylation of 2-(2-hydroxy-5-nitrophenyl)-1-(4-methoxyphenyl)-ethanone, subsequent treatment of the ester with bases and a zeolite (alumosilicate) catalyst and optional subsequent demethylation. This process can be used for the production of Dronedarone.
    Type: Grant
    Filed: May 26, 2010
    Date of Patent: February 25, 2014
    Assignee: Sanofi
    Inventors: Gerhard Kretzschmar, Volker Kraft, Kai Rossen, Joachim Graeser
  • Publication number: 20130345128
    Abstract: The invention relates to the compounds of formula (I) and physiologically acceptable salts thereof. The compounds are suitable, e.g., for treating hyperglycemia.
    Type: Application
    Filed: March 7, 2012
    Publication date: December 26, 2013
    Applicant: SANOFI
    Inventors: Thomas Boehme, Christian Engel, Stefan Guessregen, Torsten Haack, Gerhard Kretzschmar, Kurt Ritter, Georg Tschank
  • Patent number: 8334392
    Abstract: This application relates to a process for the production of (2R)-dihydroartemisinic acid or (2R)-dihydroartemisinic acid esters from artemisinic acid or artemisinic acid esters, respectively, by diimine hydrogenation of the exocyclic CC-double bond, and use of said process in the production of the antimalarial drug artemisinin.
    Type: Grant
    Filed: September 10, 2010
    Date of Patent: December 18, 2012
    Assignee: Sanofi
    Inventors: Volker Kraft, Gerhard Kretzschmar, Kai Rossen
  • Publication number: 20120077995
    Abstract: A process for the production of Dronedarone intermediates of the formula (I), by acylation of 2-(2-hydroxy-5-nitrophenyl)-1-(4-methoxyphenyl)-ethanone, subsequent treatment of the ester with bases and a zeolite (alumosilicate) catalyst and optional subsequent demethylation. This process can be used for the production of Dronedarone.
    Type: Application
    Filed: May 26, 2010
    Publication date: March 29, 2012
    Applicant: SANOFI
    Inventors: Gerhard Kretzschmar, Volker Kraft, Kai Rossen, Joachim Graser
  • Publication number: 20120065411
    Abstract: A process for the production of 2-alkyl-3-aroyl-5-nitrobenzofurans by acylation of 2-(2-hydroxy-5-nitrophenyl)-1-aryl-ethanones and subsequent treatment of the esters with combinations of bases and proton acids or Lewis acids. This process can be used for the production of Dronedarone. Furthermore, novel intermediates for the manufacture of Dronedarone are provided.
    Type: Application
    Filed: May 26, 2010
    Publication date: March 15, 2012
    Applicant: SANOFI
    Inventors: Gerhard Kretzschmar, Volker Kraft, Thomas Olpp, Kai Rossen
  • Publication number: 20110230669
    Abstract: This application relates to a process for the production of (2R)-dihydroartemisinic acid or (2R)-dihydroartemisinic acid esters from artemisinic acid or artemisinic acid esters, respectively, by diimine hydrogenation of the exocyclic CC-double bond, and use of said process in the production of the antimalarial drug artemisinin.
    Type: Application
    Filed: September 10, 2010
    Publication date: September 22, 2011
    Inventors: VOLKER KRAFT, GERHARD KRETZSCHMAR, KAI ROSSEN
  • Publication number: 20030224936
    Abstract: An aqueous film forming seed treatment composition comprising a) 5-50 wt.-% of a film forming crosslinked proteinaceous material and b) 0.001-50 wt.-% of other active ingredients selected from the following group: pesticides, fertilisers, bioregulating additives, additives for increasing the fertiliser efficiency, plant productivity, growth and nutrient accumulation and adjuvants or any combination thereof.
    Type: Application
    Filed: March 10, 2003
    Publication date: December 4, 2003
    Inventor: Gerhard Kretzschmar
  • Patent number: 6413936
    Abstract: The invention relates to novel mimetics of the tetrasaccharides sialyl-Lewis-X and sialyl-Lewis-A having an improved action as inhibitors of cell adhesion, to a process for the preparation of these compounds and to their use as pharmacological active compounds and diagnostic agents.
    Type: Grant
    Filed: October 30, 1996
    Date of Patent: July 2, 2002
    Assignee: Glycorex AB
    Inventors: Wolfgang Schmidt, Ulrich Sprengard, Gerhard Kretzschmar, Robert Klein, Horst Kunz
  • Patent number: 6406894
    Abstract: A process for preparing polyvalent, physiologically degradable carbohydrate-containing polymers by enzymatic glycosylation reactions is described. The carbohydrate-containing polymers thus prepared may be used for preparing carbohydrate building blocks. The polyvalent carbohydrate-containing polymers of the invention cause no intolerance reactions in vivo, either in their intact form or in the form of degradation products. The carbohydrate side chain of the carbohydrate-containing polymer is assembled by enzymatic glycosylation reactions in homogeneous aqueous buffer systems directly on a biodegradable polymer. The yields of the glycosylation reaction are significantly improved over known processes, and are often quantitative. This also provides a significant increase in the loading densities. A process for preparing free oligosaccharides by means of the carbohydrate-containing polymers of the invention is also described.
    Type: Grant
    Filed: December 11, 1997
    Date of Patent: June 18, 2002
    Assignee: Glycorex AB
    Inventors: Brigitte Hoersch, Michael Ahlers, Gerhard Kretzschmar, Eckart Bartnik, Dick Seiffge
  • Patent number: 6348312
    Abstract: The invention relates to novel stabilized oligonucleotides in which at least one non-terminal pyrimidine nucleoside is modified, and to their use as a diagnostic or pharamaceutical for the treatment of viral infections, cancer or diseases in which integrins or cell-cell adhesion receptors are active.
    Type: Grant
    Filed: November 10, 1994
    Date of Patent: February 19, 2002
    Assignee: Hoescht Aktiengesellschaft
    Inventors: Anuschirwan Peyman, Eugen Uhlmann, Matthias Mag, Gerhard Kretzschmar, Matthias Helsberg, Irvin Winkler
  • Patent number: 6197752
    Abstract: The invention relates to novel mimetics of the tetrasaccharides sialyl- Lewis-X (SLeX) and sialyl- Lewis-A (SLeA) having an improved action as inhibitors of cell adhesion, specifically a compound of the formula I in which R1 is —H, —CH3 or —CH2OH, R2 is —H or —OH, R3, R4 and R5 independently of one another are —H, C1-C4-alkyl or —OH, R6, R7, R8, R9 and R10 independently of one another are —H or C1-C4-alkyl D is —O—C(O)—, —C(O)—or —NR6—C(O)—, E is —CR7R8—, —NR7—, or a nitrogen heterocycle of the formula n is 1 or 2, m is 0 or 1, p is an integer from 0 to 10, q is 1 or 2 and X1 and X2 independently of one another are —H, —COOR9, —NR9R10, —OH, —OSO3H, —CH2COOR9 or —CH2OSO3H or together are ═O, to a process for preparing these compounds and to their use as pharmacological active compounds and diagnostic
    Type: Grant
    Filed: September 5, 1996
    Date of Patent: March 6, 2001
    Assignee: Glycorex AB
    Inventors: Wolfgang Schmidt, Ulrich Sprengard, Gerhard Kretzschmar, Horst Kunz
  • Patent number: 6136790
    Abstract: The invention relates to carbohydrate mimetics, which inhibit the binding of selectin to carbohydrate ligands, of the formula I ##STR1## excluding the compounds sialyl-Lewis-X and -A and their derivatives which, instead of an N-acetyl group, carry the substituents N.sub.3, NH.sub.2 or OH or which, instead of fucose, carry glycerol,and pharmaceutical compositions and diagnostic agents containing these derivatives, and methods for using these pharmaceutical compositions and diagnostic agents.
    Type: Grant
    Filed: July 28, 1997
    Date of Patent: October 24, 2000
    Assignee: Glycorex AB
    Inventors: Alexander Toepfer, Gerhard Kretzschmar, Eckart Bartnik, Dirk Seiffge
  • Patent number: 6110897
    Abstract: The invention relates to compounds of formula Ix and Ia: ##STR1## wherein (Ix) comprises the regioisomeric form sLe.sup.X and (Ia) comprises the regioisomeric form sLe.sup.A, and R.sup.1 is a lipophilic radical formed from aliphatic or cycloaliphatic units, or a sugar residue which is capped by a .beta.1-O-linked aliphatic or cycloaliphatic unit at the reducing end of the terminal sugar. The compounds of the present invention are useful as inhibitors of increased cell-cell adhesion as well as useful in treating diseases associated with increased cell-cell-adhesion. The compounds of the present invention are also incorporated into pharmaceutical compositions.
    Type: Grant
    Filed: October 10, 1997
    Date of Patent: August 29, 2000
    Assignee: Glycorex AB
    Inventors: Carlo Unverzagt, Gregor Kuznik, Gerhard Kretzschmar
  • Patent number: 6037467
    Abstract: Carbohydrate-containing polymers which can have an HLB* of from about 10 to about 20 are disclosed. The compounds comprise a hydrophilic polymer portion, a carbohydrate portion comprising from 1 to about 20 naturally occurring, identical or different, monosaccharide units, at least one bifunctional spacer coupling the carbohydrate portion to the hydrophilic polymer portion, and a potentiator moiety. The potentiator moiety can be is a crosslinking moiety located within the hydrophilic polymer or a hydrophobic, hydrophilic or ionic moiety. Processes for the preparation and use of such polymers are also disclosed.
    Type: Grant
    Filed: July 24, 1997
    Date of Patent: March 14, 2000
    Assignee: Glycorex AB
    Inventors: Wilhelm Stahl, Michael Ahlers, Axel Walch, Eckhart Bartnik, Gerhard Kretzschmar, Susanne Grabley, Rudolf Schleyerbach
  • Patent number: 5858994
    Abstract: The invention relates to novel conjugates of tetrasaccharides, preferably of sialyl-Lewis X (SLeX) and sialyl-Lewis A (SLeA), having improved activity as inhibitors of cell adhesion, a process for the preparation of these compounds, and their use as pharmacological active compounds and as diagnostics and pharmaceuticals which contain these conjugates.
    Type: Grant
    Filed: July 31, 1995
    Date of Patent: January 12, 1999
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Gerhard Kretzschmar, Wolfgang Schmidt, Ulrich Sprengard, Eckart Bartnik, Dirk Seiffge, Horst Kunz
  • Patent number: 5817742
    Abstract: Polymer-based polyvalent malonic acid derivatives having anti-adhesive properties are described. The compounds comprise a polyamino acid linked to a group of formula (I). In formula (I), R.sup.1 and R.sup.2 together form a six-membered carbocylic or heterocyclic ring, containing at least one substituent selected from R.sup.4, R.sup.5, and R.sup.6. R.sup.3 is H, (CH.sub.2) .sub.m X or CH.sub.2 O(CH.sub.2).sup.m X.sup.1. The polyamino acid and the group of formula II are linked via R.sup.4, R.sup.5, or R.sup.6, or optionally via a spacer of formula --?Q.sup.1 --(CH.sub.2).sub.p --Q.sup.2 --!.sub.r. A and B independently are O, S, NH, HN--CO, OC--NH, O--CO, OC--O, NH--CO--O, --O--CO--NH, S--CO, SC--O, O--CS--S, S--CS--OS, NH--CS--S, S--CS--NH, or CH.sub.2. Z is a pyranose, furanose, open-chain polyalcohol or Y--X.sup.6. Y is --O--(CX.sup.2,X.sup.3).sub.n, -(CX.sup.2,X.sup.3).sub.n, --CH.sub.2 --(CX.sup.2,X.sup.3).sub.
    Type: Grant
    Filed: September 11, 1996
    Date of Patent: October 6, 1998
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Alexander Toepfer, Gerhard Kretzschmar, Eckart Bartnik, Wolfgang Schmidt, Brigitte Horsch