Patents by Inventor Isaac Chekroun

Isaac Chekroun 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: 5476941
    Abstract: A compound of formula (1): ##STR1## in which R.sub.1 represents a 1,1-dimethylethyl, triphenylmethyl, methoxymethyl or benzyloxymethyl group; andR.sub.2 represents a C.sub.1 -C.sub.4 alkyl group.
    Type: Grant
    Filed: October 3, 1994
    Date of Patent: December 19, 1995
    Assignee: Synthelabo
    Inventors: Isaac Chekroun, Jose Ruiz-Montes, Guy Rossey
  • Patent number: 5430149
    Abstract: A compound represented by formula (V): ##STR1## in which R.sub.1 is selected from the group consisting of hydrogen, unbranched and branched C.sub.1-7 alkyl, unbranched and branched C.sub.3-9 alkenyl, and (C.sub.3-7)cycloalkyl(C.sub.1-6)alkyl groups, and R.sub.2 is selected from the group consisting of hydrogen, unbranched and branched C.sub.1-7 alkyl,(C.sub.3-7)cycloalkyl(C.sub.1-3)alkyl, aryl(C.sub.1-3)alkyl, aryloxy(C.sub.1-3)alkyl, arylthio(C.sub.1-3) alkyl, arylsulphonyl(C.sub.1-3)alkyl and heteroaryl (C.sub.1-3) alkyl groups.
    Type: Grant
    Filed: February 22, 1994
    Date of Patent: July 4, 1995
    Assignee: Synthelabo
    Inventors: Isaac Chekroun, Manuel Bedoya Zurita, Jose Ruiz-Montes, Guy Rossey
  • Patent number: 5405960
    Abstract: Triarylborane derivatives corresponding to the formula (1) ##STR1## in which R either represents a group --CR.sub.1 R.sub.2 R.sub.3 where R.sub.1, R.sub.2 and R.sub.3 are each, independently of one another, a (C.sub.1 -C.sub.2)alkyl or aryl group, or represents a group --CH.sub.2 OR.sub.4 where R.sub.4 is a (C.sub.1 -C.sub.2)alkyl or benzyl group, or represents a group --Si(R.sub.5).sub.3 where R.sub.5 is a (C.sub.1 -C.sub.2)alkyl or aryl group, R being in the 1 or 2 position of the tetrazole ring, their preparation and their use as synthesis intermediates.
    Type: Grant
    Filed: August 9, 1994
    Date of Patent: April 11, 1995
    Assignee: Synthelabo
    Inventors: Isaac Chekroun, Guy Rossey, Michel Magnat
  • Patent number: 5382672
    Abstract: Derivatives of benzeneborinic acid, preparation thereof and use thereof as synthetic intermediates.
    Type: Grant
    Filed: November 19, 1993
    Date of Patent: January 17, 1995
    Assignee: Synthelabo
    Inventors: Isaac Chekroun, Jose Ruiz-Montes, Manuel Bedoya-Zurita, Guy Rossey
  • Patent number: 5374735
    Abstract: Triarylborane derivatives corresponding to the formula (1) ##STR1## in which R either represents a group --CR.sub.1 R.sub.2 R.sub.3 where R.sub.1, R.sub.2 and R.sub.3 are each, independently of one another, a (C.sub.1 -C.sub.2)alkyl or aryl group, or represents a group --CH.sub.2 OR.sub.4 where R.sub.4 is a (C.sub.1 -C.sub.2)alkyl or benzyl group, or represents a group --Si(R.sub.5).sub.3 where R.sub.5 is a (C.sub.1 -C.sub.2)alkyl or aryl group, R being in the 1 or 2 position of the tetrazole ring, their preparation and their use as synthesis intermediates.
    Type: Grant
    Filed: December 14, 1993
    Date of Patent: December 20, 1994
    Assignee: Synthelabo
    Inventors: Isaac Chekroun, Guy Rossey, Michel Magnat
  • Patent number: 5371233
    Abstract: Compounds corresponding to the formula (I) ##STR1## in which X represents dibromomethyl, formyl, (C.sub.1-4)alkyl, or a group CH(OR.sub.5).sub.2 or CH(OH)OR.sub.5, wherein the or each R.sub.5 is hydrogen (C.sub.1-3)alkyl or the two R.sub.5 's in the case of CH(OR.sub.5).sub.2 are linked to provide a 1,3-dioxolane or 1,3-dioxane ring, and Y represents hydrogen, 1,1-dimethylethyl, triphenylmethyl, trimethylstannyl, tributylstannyl, (1,1-dimethylethyl)dimethylsilyl, (1,1-dimethylethyl)diphenylsilyl, 2-cyanoethyl, or a group CH.sub.2 OR.sub.6 wherein R.sub.6 is methyl, phenylmethyl, 1,1-dimethylethyl, 2,2,2-trichloroethyl, benzyloxycarbonyl or 2,2,2-trichloroethyloxycarbonyl, Y being in position 1 or 2 on the tetrazole ring. The compounds of formula (I) are useful as intermediates in the synthesis of compounds possessing therapeutic activity.
    Type: Grant
    Filed: December 29, 1992
    Date of Patent: December 6, 1994
    Assignee: Synthelabo
    Inventors: Marc Daumas, Christian Hoornaert, Isaac Chekroun, Manuel Bedoya-Zurita, Jose Ruiz-Montes, Guy Rossey, Helene Greciet
  • Patent number: 5312920
    Abstract: A process for preparing a compound represented by formula ##STR1## by deprotecting a compound represented by formula (VII) ##STR2## in which R.sub.1 represents an unbranched or branched C.sub.1-7 alkyl, unbranched or branched C.sub.3-9 alkenyl, or (C.sub.3-7)cycloalkyl(C.sub.1-6)alkyl, and R.sub.2 represents hydrogen, unbranched or branched C.sub.1-7 alkyl, (C.sub.3-7)cycloalkyl(C.sub.1-3)alkyl, aryl(C.sub.1-3)alkyl optionally substituted on the ring-system, aryloxy(C.sub.1-3)alkyl optionally substituted on the ring-system, arylthio(C.sub.1-3)alkyl optionally substituted on the ring-system, arylsulphonyl(C.sub.1-3)alkyl optionally substituted on the ring-system, and heteroaryl(C.sub.1-3)alkyl optionally substituted on the ring-system.
    Type: Grant
    Filed: March 12, 1993
    Date of Patent: May 17, 1994
    Assignee: Synthelabo
    Inventors: Isaac Chekroun, Manuel Bedoya Zurita, Jose Ruiz-Montes, Guy Rossey
  • Patent number: 5278312
    Abstract: Derivatives of benzeneborinic acid corresponding to the formula (1) ##STR1## in which R.sub.1, R.sub.2 and R.sub.3 represent, each independently of the others, either a (C.sub.1 -C.sub.2)alkyl group or an aryl group, the group --CR.sub.1 R.sub.2 R.sub.3 being in position 1 or 2 of the tetrazole ring, preparation thereof, and method of use as synthetic intermediates.
    Type: Grant
    Filed: October 29, 1992
    Date of Patent: January 11, 1994
    Assignee: Synthelabo
    Inventors: Isaac Chekroun, Jose Ruiz-Montes, Manuel Bedoya-Zurita, Guy Rossey
  • Patent number: 5102998
    Abstract: 2-Aminothiophenol is reacted with methyl (-)-(2R,3S)-2,3-epoxy-3-(4-methoxyphenyl)propionate, and the intermediate methyl (2S,3S)-3-[(2-aminophenyl)thio]-2-hydroxy-3-(4-methoxyphenyl)propionate is cyclized in the presence of methanesulfonic acid, in the same vessel and without isolating said intermediate product, using e.g. chlorobenzene as a solvent.
    Type: Grant
    Filed: October 24, 1989
    Date of Patent: April 7, 1992
    Assignee: Synthelabo
    Inventors: Guy Rossey, Isaac Chekroun, Antonio Ugolini, Alexander Wick, Andre Bourbon, Jean-Baptiste Graux
  • Patent number: 5081277
    Abstract: Process for the preparation of compounds of the general formula (I) ##STR1## wherein R is hydrogen or (C.sub.1-4)alkyl.
    Type: Grant
    Filed: October 3, 1989
    Date of Patent: January 14, 1992
    Assignee: Synthelabo
    Inventors: Guy Rossey, Antonio Ugolini, Isaac Chekroun, Abkar Vartanian, Alexander Wick
  • Patent number: 5013835
    Abstract: 2-Aminothiophenol is reacted with (-)-(2R,3S)-2,3-epoxy-3-(4-methoxyphenyl) methylpropionate, and the intermediate (2S,3S)-3-[(2-aminophenyl)thio]-2-hydroxy-3-(4-methoxyphenyl) methylpropionate is then cyclized in the presence of methane sulfonic acid, in the same container and without isolating said intermediate product, using chlorobenzene as a solvent.
    Type: Grant
    Filed: September 14, 1989
    Date of Patent: May 7, 1991
    Assignee: Synthelabo
    Inventors: Guy Rossey, Isaac Chekroun, Antonio Ugolini, Alexander Wick, Bernard Gerin, Andre Bourbon, Jean-Baptiste Graux
  • Patent number: 5008434
    Abstract: A process for the preparation of a methyl (+)-(2S,3S)-3-[(2-aminophenyl)thio]-2-hydroxy-3-(4-methoxyphenyl)propionat e of the formula (I): ##STR1## in which X denotes hydrogen or chlorine, which process comprises reacting a 2-aminothiophenol of formula (II): ##STR2## in which X is as defined above, with methyl (-)-(2R,3S)-2,3-epoxy-3-(4-methoxyphenyl)propionate, in a 1,2-dichloroethane solvent.
    Type: Grant
    Filed: April 18, 1989
    Date of Patent: April 16, 1991
    Assignee: Synthelabo
    Inventors: Guy Rossey, Antonio Ugolini, Isaac Chekroun, Abkar Vartanian, Alexander Wick
  • Patent number: 4493931
    Abstract: The present invention provides a multistep process for the preparation of .beta.-cyclo-substituted ethylamines of the general formula:-Ar--CH.sub.2 --CH.sub.2 --NH.sub.2 (I)in which AR is a heterocyclic or non-heterocyclic aromatic radical, which is optionally mono- or poly- substituted, wherein said compounds represent a class of intermediates which can be converted to 4,5,6,7-tetrahydro[3,2-C] or [2,3-C]pyridines wherein the latter are useful for anti-inflammatory, vasodilator or blood platelet aggregation inhibition activities.
    Type: Grant
    Filed: June 29, 1982
    Date of Patent: January 15, 1985
    Assignee: Sanofi
    Inventors: Isaac Chekroun, Alain Heymes
  • Patent number: 4487931
    Abstract: The present invention provides a multistep process for the preparation of 2-(thien-2-yl)- and 2-(thien-3-yl)-ethylamine intermediates of the general formula:- ##STR1## in which R.sub.1, in the 2-, 3-, 4- or 5-position, is a hydrogen or halogen atom, a nitro, amino, cyano or carboxyl group, a linear or branched alkyl or alkoxy radical or a heterocyclic or non-heterocyclic aromatic radical, which is optionally mono- or polysubstituted, R.sub.2 is a hydrogen atom, a linear or branched alkyl radical or a heterocyclic or non-heterocyclic aromatic radical, which is optionally mono- or polysubstituted, and Ar is a heterocyclic or non-heterocyclic aromatic radical, which is optionally mono- or polysubstituted, when the aminoethyl radical is in the two position and the radical R.sub.1 is in the 4- or 5-position, the above intermediates can be converted into 4,5,6,7-tetrahydrothieno[3,2-c]pyridine derivatives according to a procedure set forth in U.S. Pat. No. 4,127,580.
    Type: Grant
    Filed: June 29, 1982
    Date of Patent: December 11, 1984
    Assignee: Sanofi
    Inventors: Isaac Chekroun, Alain Heym/e/ s
  • Patent number: 4482718
    Abstract: The present invention provides a process for the preparation of 2-(thien-2-yl)- and 2-(thien-3-yl)-ethylamine derivatives of the general formula: ##STR1## in which R.sub.1, in the 2-, 3-, 4- or 5-position, is a hydrogen or halogen atom, a nitro, carboxyl, cyano or amino group, a linear or branched alkyl or alkoxy radical or a heterocyclic or non-heterocyclic aromatic radical, which is optionally mono- or polysubstituted, the aminoethyl chain is in the 2- or 3-position, R.sub.2, R.sub.3 and R.sub.4, which are the same or different, are hydrogen atoms or heterocyclic or non-heterocyclic aromatic radicals, which are optionally mono- or polysubstituted, and Ar is a heterocyclic or non-heterocyclic aromatic radical, which is optionally mono- or polysubstituted.
    Type: Grant
    Filed: June 29, 1982
    Date of Patent: November 13, 1984
    Assignee: Sanofi
    Inventors: Isaac Chekroun, Alain Heymes
  • Patent number: 4458086
    Abstract: The present invention provides a process for the preparation of 2-(thienyl-2)- and 2-(thienyl-3)-ethylamines of the general formula: ##STR1## in which R.sub.1, which is in the 2-, 3-, 4- or 5-position, is a hydrogen atom, a straight-chained or branched alkyl radical or a heterocyclic or non-heterocyclic aromatic radical, which is optionally mono- or polysubstituted, or R.sub.1 is an alkoxy radical, a halogen atom or a nitro, carboxyl, cyano or amino group; the aminoethyl chain is in the 2- or 3-position of the thiophene nucleus; R.sub.2 is a hydrogen atom or a straight-chained or branched alkyl radical or a heterocyclic or non-heterocyclic aromatic radical, which is optionally mono- or poly-substituted; and Ar is a heterocyclic or non-heterocyclic aromatic radical, which is optionally mono- or poly-substituted.
    Type: Grant
    Filed: June 29, 1982
    Date of Patent: July 3, 1984
    Assignee: Sanofi
    Inventors: Isaac Chekroun, Alain Heymes
  • Patent number: RE34935
    Abstract: 2-Aminothiophenol is reacted with methyl (-)-(2R,3S)-2,3-epoxy-3-(4-methoxyphenyl)propionate, and the intermediate methyl (2S,3S)-3-[(2-aminophenyl)thio]-2-hydroxy-3-(4-methoxyphenyl)propionate is cyclized in the presence of methanesulfonic acid, in the same vessel and without isolating said intermediate product, using e.g. chlorobenzene as a solvent.
    Type: Grant
    Filed: April 29, 1993
    Date of Patent: May 9, 1995
    Assignee: Synthelabo
    Inventors: Guy Rossey, Isaac Chekroun, Antonio Ugolini, Alexander Wick, Bernard Gerin, Andre Bourbon, Jean-Baptiste Graux