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).
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Publication number: 20120226044Abstract: 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: ApplicationFiled: July 4, 2005Publication date: September 6, 2012Inventors: Yves Bessard, David L. Kuo
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Patent number: 7355048Abstract: 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: GrantFiled: January 6, 2005Date of Patent: April 8, 2008Assignees: Lonza Ltd., Merck & Co. Inc.Inventors: David Kuo, James E. Leresche, Ralf Proplesch, Jean-Paul Roduit, Yves Bessard, Erich Armbruster
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Patent number: 7141673Abstract: 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: GrantFiled: January 13, 2000Date of Patent: November 28, 2006Assignee: Lonza AGInventors: Erich Armbruster, Yves Bessard, David Kuo, James E. Leresche, Ralf Proplesch, Jean-Paul Roduit
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Patent number: 7009058Abstract: 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: GrantFiled: May 11, 2000Date of Patent: March 7, 2006Assignee: Lonza AGInventors: Yves Bessard, Gerhard Stucky, Jean-Paul Roduit
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Publication number: 20050159458Abstract: 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: ApplicationFiled: January 6, 2005Publication date: July 21, 2005Inventors: David Kuo, James Leresche, Ralf Proplesch, Jean-Paul Roduit, Yves Bessard, Erich Armbruster
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Patent number: 6600046Abstract: 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: GrantFiled: October 30, 2002Date of Patent: July 29, 2003Assignees: Merck & Co., Inc., Lonza AGInventors: Yves Bessard, James Edward Leresche
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Patent number: 6566527Abstract: 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: GrantFiled: March 14, 2002Date of Patent: May 20, 2003Assignees: Merck & Co., Inc., Lonza AGInventors: Yves Bessard, James Edward Leresche
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Publication number: 20030088107Abstract: A five-step process for preparing 1-(6-methylpyridin-3-yl)-2-[(4-(methylsulphonyl)phenyl]-ethanone of the formula 1Type: ApplicationFiled: October 30, 2002Publication date: May 8, 2003Inventors: Yves Bessard, James Edward Leresche
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Patent number: 6469178Abstract: 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: GrantFiled: December 5, 2001Date of Patent: October 22, 2002Assignee: Lonza AGInventors: Yves Bessard, Josef Heveling
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Publication number: 20020045760Abstract: 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: ApplicationFiled: December 5, 2001Publication date: April 18, 2002Applicant: Lonza AGInventors: Yves Bessard, Josef Heveling
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Publication number: 20010014743Abstract: 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: ApplicationFiled: March 29, 2001Publication date: August 16, 2001Applicant: Lonza AGInventors: Yves Bessard, Josef Heveling
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Patent number: 6258958Abstract: 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: GrantFiled: December 11, 2000Date of Patent: July 10, 2001Assignee: Lonza AGInventors: Yves Bessard, Josef Heveling
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Patent number: 6169183Abstract: 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: GrantFiled: January 27, 1999Date of Patent: January 2, 2001Assignee: Lonza, Ltd.Inventors: Yves Bessard, Gerhard Stucky, Jean-Paul Roduit
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Patent number: 6162921Abstract: 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: GrantFiled: September 20, 1999Date of Patent: December 19, 2000Assignee: Lonza, LtdInventors: Yves Bessard, Gerhard Stucky, Jean-Paul Roduit
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Patent number: 6103906Abstract: 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: GrantFiled: March 12, 1998Date of Patent: August 15, 2000Assignee: Lonza, Ltd.Inventors: Jean-Paul Roduit, Yves Bessard
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Patent number: 6022973Abstract: 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: GrantFiled: March 30, 1999Date of Patent: February 8, 2000Assignee: Lonza Ltd.Inventors: Yves Bessard, Gerhard Stucky, Jean-Paul Roduit
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Patent number: 5925765Abstract: 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: GrantFiled: July 15, 1997Date of Patent: July 20, 1999Assignee: Lonza AGInventors: Yves Bessard, Gerhard Stucky, Jean-Paul Roduit
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Patent number: 5869667Abstract: 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: GrantFiled: July 14, 1997Date of Patent: February 9, 1999Assignee: Lonza AGInventors: Yves Bessard, Gerhard Stucky
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Patent number: 5840892Abstract: 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: GrantFiled: April 8, 1997Date of Patent: November 24, 1998Assignee: Lonza AGInventors: Yves Bessard, Gerhard Stucky
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Patent number: 5821368Abstract: 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: GrantFiled: July 8, 1997Date of Patent: October 13, 1998Assignee: Lonza AGInventors: Yves Bessard, Gerhard Stucky