Patents by Inventor Yves Bessard

Yves Bessard 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).

  • Publication number: 20120226044
    Abstract: A process for the preparation of 4-steroids of the formula: R1 and R2 are independently selected from the group that is hydrogen, F, Cl, Br, I, C1-6-allyl and C1-6-alkoxy, and R4 is selected from the group that is hydrogen, (N,N-di-C1-6-allylamino)methyl, allylamino)ethyl, C1-6-alkyl, C1-6-alkoxy, phenyl and benzyl, and Q7 represents a carbonyl oxygen atom or is R7-1 and R7-2, wherein one of R7-1 and R7-2 is hydrogen and the other is selected from the group that is hydrogen, F, Cl, Br, I, C1-6-alkyl and C1-6-alkoxy, and R9 represents hydrogen or F, and Q11 represents a carbonyl oxygen atom or is R11-1 and R11-2, wherein one of R11-1 and R11-2 is hydrogen and the other is selected from the group that is hydrogen, cyano, cyano-C1-3-alkyl, acetoxy, COOH and COO?M+, wherein M+ is Na+, K+ or NH+4, and R16 is selected from the group that is hydrogen, cyano, cyano-C1-3-alkyl, acetoxy, COOH and COO?M+, wherein M+ is Na+, K+ or NH+4, and COOR represents COOH or COO?M+, wherein M+ is Na+, K+ or NH+4.
    Type: Application
    Filed: July 4, 2005
    Publication date: September 6, 2012
    Inventors: Yves Bessard, David L. Kuo
  • Patent number: 7355048
    Abstract: A four-step process for preparing 1-(6-methylpyridin-3-yl)-2-[4-(methylsulfonyl)phenyl]ethanone of the formula: starting from 2-methyl-5-ethylpyridine. 1-(6-Methylpyridin-3yl)-2-[4-(methylsulfonyl)phenyl]ethanone is an intermediate for preparing inhibitors.
    Type: Grant
    Filed: January 6, 2005
    Date of Patent: April 8, 2008
    Assignees: Lonza Ltd., Merck & Co. Inc.
    Inventors: David Kuo, James E. Leresche, Ralf Proplesch, Jean-Paul Roduit, Yves Bessard, Erich Armbruster
  • Patent number: 7141673
    Abstract: A starting product for the preparation of COX-2 inhibitors, notably the compound 1-(6-methylpyridine-3-yl)-2-[(4-(methylsulfonyl)phenyl]ethanone of the formula (I): A method for making the compound.
    Type: Grant
    Filed: January 13, 2000
    Date of Patent: November 28, 2006
    Assignee: Lonza AG
    Inventors: Erich Armbruster, Yves Bessard, David Kuo, James E. Leresche, Ralf Proplesch, Jean-Paul Roduit
  • Patent number: 7009058
    Abstract: A method for preparing pyridine-2,3-dicarboxylic acid esters of the general formula: wherein R is C1-6-alkyl, C3-6-cycloalkyl, aryl or arylalkyl, and R1 to R3, independently of one another, represent hydrogen, C1-6-alkyl, fluorinated C1-6-alkyl, C1-6-alkoxy, (C1-6-alkoxy)-C1-6-alkyl or (C1-6-alkoxy)carbonyl. These esters are obtained from the corresponding 2,3-dichloropyridine, the corresponding alcohol ROH and carbon monoxide in the presence of a palladium-diphosphine complex and a weak base. Pyridine-2,3-dicarboxylic acid esters are herbicides or intermediates for the preparation of herbicides.
    Type: Grant
    Filed: May 11, 2000
    Date of Patent: March 7, 2006
    Assignee: Lonza AG
    Inventors: Yves Bessard, Gerhard Stucky, Jean-Paul Roduit
  • Publication number: 20050159458
    Abstract: A four-step process for preparing 1-(6-methylpyridin-3-yl)-2-[4-(methylsulfonyl)phenyl]ethanone of the formula: starting from 2-methyl-5-ethylpyridine. 1-(6-Methylpyridin-3yl)-2-[4-(methylsulfonyl)phenyl]ethanone is an intermediate for preparing inhibitors.
    Type: Application
    Filed: January 6, 2005
    Publication date: July 21, 2005
    Inventors: David Kuo, James Leresche, Ralf Proplesch, Jean-Paul Roduit, Yves Bessard, Erich Armbruster
  • Patent number: 6600046
    Abstract: The process for preparing 1-(6-methylpyridin-3-yl)-2-[(4-methlsulfonyl)-phenyl]ethanone of the formula I: In a first step, 4-(methylthio)phenylacetonitrile is condensed with a 6-methylnicotinic ester to give 3-[2-(4-(methlthio)phenyl)-2-cyanoacetyl](6-methyl)pyridine of the formula II: In a second step, the compound of formula II is hydrolyzed and decarboxylated under acidic conditions using a mixture of acetic acid and a mineral acid, to give 3-[2-(4-(methylthio)phenyl)acetyl](6-methyl)pyridine of the formula III: Finally, in a last step, the compound of formula III is oxidized to give the end product.
    Type: Grant
    Filed: October 30, 2002
    Date of Patent: July 29, 2003
    Assignees: Merck & Co., Inc., Lonza AG
    Inventors: Yves Bessard, James Edward Leresche
  • Patent number: 6566527
    Abstract: A five-step process for preparing 1-(6-methylpyridin-3-yl)-2-[4-methylsulfonyl)phenyl]ethanone of formula (I): The process involves the following steps: (a) 4-(methylthio)benzyl alcohol is converted into 4-(methylthio)benzyl chloride; (b) 4-(methylthio)benzyl chloride is converted with an alkali metal cyanide into 4-(methylthio)phenylacetonitrile; (c) 4-(methylthio)phenylacetonitrile is condensed with a 6-methyinicotinic ester to give 3-[2-(2-(methylthio)phenyl)-2-cyanoacetyl](6-methyl)pyridine; (d) 3-[2-(4-(methylthio)phenyl-2-cyanoacetyl](6-methyl)pyridine is hydrolyzed and decarboxylated under acidic conditions to give 3-[2-(4-(methylthio)-phenyl)acetyl](6-methyl)pyridine is hydrolyzed and decarboxylated under acidic conditions to give 3-[2-(4-(methylthio)phenyl)acetyl(6-methyl)pyridine; and (e) 3-[2(4-(methylthio)phenyl)acetyl](6-methyl)pyridine is oxidized to give the end product.
    Type: Grant
    Filed: March 14, 2002
    Date of Patent: May 20, 2003
    Assignees: Merck & Co., Inc., Lonza AG
    Inventors: Yves Bessard, James Edward Leresche
  • Publication number: 20030088107
    Abstract: A five-step process for preparing 1-(6-methylpyridin-3-yl)-2-[(4-(methylsulphonyl)phenyl]-ethanone of the formula 1
    Type: Application
    Filed: October 30, 2002
    Publication date: May 8, 2003
    Inventors: Yves Bessard, James Edward Leresche
  • Patent number: 6469178
    Abstract: A new process for the catalytic conversion of hydroxymethyl imidazoles to formylimidazoles is described. The reaction takes place in the presence of a peroxide. Formylimidazoles are important intermediate products for pharmaceutical substances.
    Type: Grant
    Filed: December 5, 2001
    Date of Patent: October 22, 2002
    Assignee: Lonza AG
    Inventors: Yves Bessard, Josef Heveling
  • Publication number: 20020045760
    Abstract: A new process for the catalytic conversion of hydroxymethyl imidazoles to formylimidazoles is described. The reaction takes place in the presence of a peroxide. Formylimidazoles are important intermediate products for pharmaceutical substances.
    Type: Application
    Filed: December 5, 2001
    Publication date: April 18, 2002
    Applicant: Lonza AG
    Inventors: Yves Bessard, Josef Heveling
  • Publication number: 20010014743
    Abstract: A new process for the catalytic conversion of hydroxymethyl imidazoles to formylimidazoles is described. The reaction takes place in the presence of a peroxide. Formylimidazoles are important intermediate products for pharmaceutical substances.
    Type: Application
    Filed: March 29, 2001
    Publication date: August 16, 2001
    Applicant: Lonza AG
    Inventors: Yves Bessard, Josef Heveling
  • Patent number: 6258958
    Abstract: A new procedure for the catalytic conversion of hydroxy methyl imidazoles to formyl imidazoles is described. The catalysis takes place in the presence of a peroxide. Formyl imidazoles are important intermediate products for pharmaceutical substances.
    Type: Grant
    Filed: December 11, 2000
    Date of Patent: July 10, 2001
    Assignee: Lonza AG
    Inventors: Yves Bessard, Josef Heveling
  • Patent number: 6169183
    Abstract: A process for preparing pyridinecarboxylic esters of the general formula: wherein R1 is hydrogen, a C1-6-alkyl group, a C1-4-alkoxycarbonyl group, a C1-4-alkoxymethyl group or a fluorinated C1-6-alkyl group, R2 is a C1-4-alkyl group and X is chlorine or bromine. The pyridinecarboxylic esters are obtained by reacing the corresponding 2,3-dihalopyridines with carbon monoxide and a C1-4-alkanol in the presence of a weak base and a complex of palladium with a bis(diphenylphosphine). Pyridinecarboxylic esters are intermediates for preparing herbicides and drugs against fibrotic diseases.
    Type: Grant
    Filed: January 27, 1999
    Date of Patent: January 2, 2001
    Assignee: Lonza, Ltd.
    Inventors: Yves Bessard, Gerhard Stucky, Jean-Paul Roduit
  • Patent number: 6162921
    Abstract: A process for preparing pyridinecarboxylic esters of the general formula: ##STR1## wherein R.sup.1 is hydrogen, a C.sub.1 -C.sub.6 -alkyl group, a C.sub.1 -C.sub.4 -alkoxycarbonyl group or a C.sub.1 -C.sub.4 -alkoxymethyl group, R.sup.2 is a C.sub.1 -C.sub.4 -alkyl group and X is chlorine or bromine. The pyridinecarboxylic esters are obtained by reacting the corresponding 2,3-dihalopyridines with carbon monoxide and a C.sub.1 -C.sub.4 -alkanol in the presence of a weak base and a complex of palladium with a bis(diphenylphosphine). Pyridinecarboxylic esters are intermediates for preparing herbicides and drugs against fibrotic diseases.
    Type: Grant
    Filed: September 20, 1999
    Date of Patent: December 19, 2000
    Assignee: Lonza, Ltd
    Inventors: Yves Bessard, Gerhard Stucky, Jean-Paul Roduit
  • Patent number: 6103906
    Abstract: A process for the preparation of 2,6-pyridinedicarboxylic acid esters of the general formula: ##STR1## wherein R.sup.1 is a C.sub.1 -C.sub.6 -alkyl group, a C.sub.3 -C.sub.6 -cycloalkyl group, an aryl group or an arylalkyl group, and R.sup.2 and R.sup.3 independently of one another are hydrogen or chlorine and R.sup.4 is hydrogen, a C.sub.1 -C.sub.6 -alkyl group, a C.sub.1 -C.sub.6 -alkoxy group or fluorine. The 2,6-pyridinedicarboxylic acid esters are obtained by reaction of the corresponding halopyridines with carbon monoxide and an alcohol of the general formula:R.sup.1 --OH IIIwherein R.sup.1 has the abovementioned meaning, in the presence of a base and of a complex of palladium with a bis-diphenylphosphine. 2,6-Pyridinedicarboxylic acid esters are intermediates for the preparation of compounds having anti-inflammatory action.
    Type: Grant
    Filed: March 12, 1998
    Date of Patent: August 15, 2000
    Assignee: Lonza, Ltd.
    Inventors: Jean-Paul Roduit, Yves Bessard
  • Patent number: 6022973
    Abstract: A process for preparing pyridinecarboxylic esters of the general formula: ##STR1## wherein R.sup.1 is hydrogen, a C.sub.1 -C.sub.6 -alkyl group, a C.sub.1 -C.sub.4 -alkoxycarbonyl group or a C.sub.1 -C.sub.4 -alkoxymethyl group, R.sup.2 is a C.sub.1 -C.sub.4 -alkyl group and X is chlorine or bromine. The pyridinecarboxylic esters are obtained by reacting the corresponding 2,3-dihalopyridines with carbon monoxide and a C.sub.1 -C.sub.4 -alkanol in the presence of a weak base and a complex of palladium with a bis(diphenylphosphine). Pyridinecarboxylic esters are intermediates for preparing herbicides and drugs against fibrotic diseases.
    Type: Grant
    Filed: March 30, 1999
    Date of Patent: February 8, 2000
    Assignee: Lonza Ltd.
    Inventors: Yves Bessard, Gerhard Stucky, Jean-Paul Roduit
  • Patent number: 5925765
    Abstract: A process for preparing pyridinecarboxylic esters of the general formula: ##STR1## wherein R.sup.1 is hydrogen, a C.sub.1 -C.sub.6 -alkyl group, a C.sub.1 -C.sub.4 -alkoxycarbonyl group or a C.sub.1 -C.sub.4 -alkoxymethyl group, R.sup.2 is a C.sub.1 -C.sub.4 -alkyl group and X is chlorine or bromine. The pyridinecarboxylic esters are obtained by reacting the corresponding 2,3-dihalopyridines with carbon monoxide and a C.sub.1 -C.sub.4 -alkanol in the presence of a weak base and a complex of palladium with a bis(diphenylphosphine). Pyridinecarboxylic esters are intermediates for preparing herbicides and drugs against fibrotic diseases.
    Type: Grant
    Filed: July 15, 1997
    Date of Patent: July 20, 1999
    Assignee: Lonza AG
    Inventors: Yves Bessard, Gerhard Stucky, Jean-Paul Roduit
  • Patent number: 5869667
    Abstract: A process for preparing 2-pyrimidinecarboxylates of the general formula: ##STR1## wherein R is C.sub.1-6 -alkyl, C.sub.3-6 -cycloalkyl, aryl or arylalkyl, and R.sup.1 to R.sup.3 are, independently of one another, hydrogen, C.sub.1-6 -alkyl, fluorinated C.sub.1-6 -alkyl, C.sub.1-6 -alkoxy, (C.sub.1-6 -alkoxy)-C.sub.1-6 -alkyl or (C.sub.1-6 -alkoxy)carbonyl. These are obtained from the corresponding 2-halopyrimidine, the corresponding alcohol ROH and carbon monoxide in the presence of a palladium/phosphine complex and a base. 2-pyrimidinecarboxylates are intermediates for preparing herbicides.
    Type: Grant
    Filed: July 14, 1997
    Date of Patent: February 9, 1999
    Assignee: Lonza AG
    Inventors: Yves Bessard, Gerhard Stucky
  • Patent number: 5840892
    Abstract: A novel process for the preparation of substituted pyrimidine derivatives of the general formula: ##STR1## in which a halopyrimidine is reacted in the presence of a sulfinate with a compound selected from the series: ##STR2## The compounds of the general formula I are precursors of, for example, compounds with herbicidal activity.
    Type: Grant
    Filed: April 8, 1997
    Date of Patent: November 24, 1998
    Assignee: Lonza AG
    Inventors: Yves Bessard, Gerhard Stucky
  • Patent number: 5821368
    Abstract: A method for preparing pyrimidin-2-ylacetic acid esters of the general formula: ##STR1## wherein R is C.sub.1-6 -alkyl, C.sub.3-6 -cycloalkyl, aryl or arylalkyl and R.sup.1 to R.sup.3, independently of one another, are hydrogen, C.sub.1-6 -alkyl, fluorinated C.sub.1-6 -alkyl, C.sub.1-6 -alkoxy, (C.sub.1-6 -alkoxy)-C.sub.1-6 -alkyl or (C.sub.1-6 -alkoxy)carbonyl. These esters are obtained from the corresponding 2-(halomethyl)-pyrimidine, the corresponding alcohol ROH and carbon monoxide in the presence of a palladium-phosphine complex and a base. Pyrimidin-2-ylacetic acid esters are intermediates in the preparation of herbicides.
    Type: Grant
    Filed: July 8, 1997
    Date of Patent: October 13, 1998
    Assignee: Lonza AG
    Inventors: Yves Bessard, Gerhard Stucky