Patents by Inventor Rafael Shapiro

Rafael Shapiro 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: 20120232271
    Abstract: A new method for the preparation of optionally 2-substituted 1,6-dihydro-6-oxo-4-pyrimidinecarboxylic acid compounds of Formula 1 is disclosed wherein R1 is H or an optionally substituted carbon moiety. Also disclosed is the method comprising additional steps to prepare optionally substituted 4-pyrimidinecarboxylic acids and esters using the compound of Formula 1 as an intermediate.
    Type: Application
    Filed: May 22, 2012
    Publication date: September 13, 2012
    Applicant: E I DU PONT DE NEMOURS AND COMPANY
    Inventor: RAFAEL SHAPIRO
  • Patent number: 8198442
    Abstract: A new method for the preparation of optionally 2-substituted 1,6-dihydro-6-oxo-4-pyrimidinecarboxylic acid compound of Formula 1 is disclosed wherein R1 is H or an optionally substituted carbon moiety.
    Type: Grant
    Filed: April 28, 2006
    Date of Patent: June 12, 2012
    Assignee: E.I. du Pont de Nemours and Company
    Inventor: Rafael Shapiro
  • Patent number: 8153844
    Abstract: Disclosed is a method for preparing a compound of Formula 1 by contacting compound of Formula 2 with R1—NH2 in the presence of a carboxylic acid and a method for preparing a compound of Formula 2 by contacting a compound of Formula 4 with phosphorus tribromide. wherein R1 is H, C1-C4 alkyl, cyclopropyl, cyclopropylmethyl or methylcyclopropyl; R2 is CH3 or Cl; R3 is C1-C6 alkyl or C3-C6 alkenyl, each optionally substituted with up to 3 halogen and up to 1 phenyl; and X is Cl or Br. Also disclosed is a method for preparing a compound of Formula 5 wherein R4, R5, R6 and Z are as defined in the disclosure, using a compound of Formula 1 that is characterized by preparing the compound of Formula 1 by the method above.
    Type: Grant
    Filed: June 27, 2007
    Date of Patent: April 10, 2012
    Assignee: E. I. du Pont de Nemours and Company
    Inventors: Richard F. Davis, Rafael Shapiro, Eric G. Taylor
  • Publication number: 20120034315
    Abstract: Disclosed are solid forms of 1-[4-[4-[5-(2,6-difluorophenyl)-4,5-dihydro-3-isoxazolyl]-2-thiazolyl]-1-piperidinyl]-2-[5-methyl-3-(trifluoromethyl)-1H-pyrazol-1-yl]ethanone (Compound 1). Methods for the preparation of solid forms of Compound 1 and for the conversion of one solid form of Compound 1 into another are disclosed. Disclosed are fungicidal compositions comprising a fungicidally effective amount of a solid form of Compound 1 and at least one additional component selected from the group consisting of surfactants, solid diluents and liquid carriers. Compositions comprising a mixture of a solid form of Compound 1 and at least one other fungicide or insecticide are also disclosed. Also disclosed are methods for controlling plant diseases caused by fungal plant pathogens comprising applying to a plant or portion thereof, or to a plant seed, a fungicidally effective amount of a solid form of Compound 1.
    Type: Application
    Filed: April 19, 2010
    Publication date: February 9, 2012
    Applicant: E.I. DU PONT DE NEMOURS AND COMPANY
    Inventors: Mary Ann Hanagan, Matthew Richard Oberholzer, Robert James Pasteris, Rafael Shapiro
  • Patent number: 8049029
    Abstract: Disclosed is a method for preparing a compound of Formula 1 comprising contacting a compound of Formula 2 with a metal cyanide reagent, a copper(I) salt reagent, an iodide salt reagent and at least one compound of Formula 3 wherein R1 is NHR3 or OR4; R2 is CH3 or Cl; R3 is H, C1-C4 alkyl, cyclopropyl, cyclopropylcyclopropyl, cyclopropylmethyl or methylcyclopropyl; R4 is H or C1-C4 alkyl; Y is Br or Cl; X is NR13 or O; n is 0 or 1; and R5, R6, R7, R8, R9, R10, R11, R12 and R13 are as defined in the disclosure. Also disclosed is a method for preparing a compound of Formula 2 wherein Y is Br and R1 is NHR3 comprising introducing a gas containing bromine into a liquid containing a compound of Formula 4, and further disclosed is a method for preparing a compound of Formula 5 wherein R14, R15, R16 and Z are as defined in the disclosure using a compound of Formula 1 characterized by preparing the compound of Formula 1 by the method disclosed above.
    Type: Grant
    Filed: December 18, 2007
    Date of Patent: November 1, 2011
    Assignee: E. I. du Pont de Nemours and Company
    Inventors: Joerg Bruening, Gary David Annis, Donald J Dumas, Rafael Shapiro
  • Publication number: 20100280251
    Abstract: Disclosed is a method for preparing a compound of Formula 1 comprising contacting a compound of Formula 2 with a metal cyanide reagent, a copper(I) salt reagent, an iodide salt reagent and at least one compound of Formula 3 wherein R1 is NHR3 or OR4; R2 is CH3 or Cl; R3 is H, C1-C4 alkyl, cyclopropyl, cyclopropylcyclopropyl, cyclopropylmethyl or methylcyclopropyl; R4 is H or C1-C4 alkyl; Y is Br or Cl; X is NR13 or O; n is 0 or 1; and R5, R6, R7, R8, R9, R10, R11, R12 and R13 are as defined in the disclosure. Also disclosed is a method for preparing a compound of Formula 2 wherein Y is Br and R1 is NHR3 comprising introducing a gas containing bromine into a liquid containing a compound of Formula 4, and further disclosed is a method for preparing a compound of Formula 5 wherein R14, R15, R16 and Z are as defined in the disclosure using a compound of Formula 1 characterized by preparing the compound of Formula 1 by the method disclosed above.
    Type: Application
    Filed: December 18, 2007
    Publication date: November 4, 2010
    Applicant: E.I. Du Pont De Nemours and Company
    Inventors: Joerg Bruening, Gary David Annis, Martin James Currie, Donald J. Dumas, Rafael Shapiro
  • Publication number: 20090306372
    Abstract: Disclosed is a method for preparing a compound of Formula 1 by contacting compound of Formula 2 with R1—NH2 in the presence of a carboxylic acid and a method for preparing a compound of Formula 2 by contacting a compound of Formula 4 with phosphorus tribromide. wherein R1 is H, C1-C4 alkyl, cyclopropyl, cyclopropylmethyl or methylcyclopropyl; R2 is CH3 or Cl; R3 is C1-C6 alkyl or C3-C6 alkenyl, each optionally substituted with up to 3 halogen and up to 1 phenyl; and X is Cl or Br. Also disclosed is a method for preparing a compound of Formula 5 wherein R4, R5, R6 and Z are as defined in the disclosure, using a compound of Formula 1 that is characterized by preparing the compound of Formula 1 by the method above.
    Type: Application
    Filed: June 27, 2007
    Publication date: December 10, 2009
    Applicant: E.I. DU PONT DE NEMOURS AND COMPANY
    Inventors: Richard F. Davis, Rafael Shapiro, Eric G. Taylor
  • Publication number: 20090156592
    Abstract: Disclosed are compounds of Formulae 1, 1A, 1B and 1C including all geometric and stereoisomers, N-oxides, and salts thereof, wherein R1, R2, R4a1, R4a2, A, Aa, G, M, W, Z1, Z3, X, J, J1 and n are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention.
    Type: Application
    Filed: July 27, 2007
    Publication date: June 18, 2009
    Applicant: E.I. DU PONT DE NEMOURS AND COMPANY
    Inventors: Robert James Pasteris, Mary Ann Hanagan, Rafael Shapiro
  • Patent number: 7528260
    Abstract: A method is disclosed for preparing compounds of Formula 1 by combining compounds of Formulae 2 and 3 and a sulfonyl chloride. Also disclosed are compounds of Formula 3, which are useful as starting materials for this method.
    Type: Grant
    Filed: December 6, 2005
    Date of Patent: May 5, 2009
    Assignee: E. I. du Pont de Nemours and Company
    Inventors: Rafael Shapiro, Eric de Guyon Taylor, William T. Zimmerman
  • Publication number: 20090043098
    Abstract: A new method for the preparation of optionally 2-substituted 1,6-dihydro-6-oxo-4-pyrimidinecarboxylic acid compound of Formula 1 is disclosed wherein R1 is H or an optionally substituted carbon moiety.
    Type: Application
    Filed: April 28, 2006
    Publication date: February 12, 2009
    Inventor: Rafael Shapiro
  • Patent number: 7396932
    Abstract: A novel process and intermediates thereof for making 4,5-dihydro-pyrazolo[3,4-c]pyrid-2-ones of the type shown below from appropriate phenyl hydrazines is described. These compounds can be useful as factor Xa inhibitors.
    Type: Grant
    Filed: September 26, 2005
    Date of Patent: July 8, 2008
    Assignee: Bristol-Myers Squibb Company
    Inventors: Rafael Shapiro, Lucius T Rossano, Boguslaw M Mudryk, Nicolas Cuniere, Matthew Oberholzer, Huiping Zhang, Bang-Chi Chen
  • Publication number: 20070299265
    Abstract: A method is disclosed for preparing compounds of Formula 1 by combining compounds of Formulae 2 and 3 and a sulfonyl chloride. Also disclosed are compounds of Formula 3, which are useful as starting materials for this method.
    Type: Application
    Filed: December 6, 2005
    Publication date: December 27, 2007
    Inventors: Rafael Shapiro, Eric Taylor, William Zimmerman
  • Publication number: 20070161797
    Abstract: A method for preparing 2,3-dichloropyridine is disclosed in which 3-amino-2-chloropyridine is contacted with an alkali metal nitrite in the presence of aqueous hydrochloric acid to form a diazonium salt; and the diazonium salt is subsequently decomposed in the presence of copper catalyst wherein at least about 50% of the copper is the copper(II) oxidation state.
    Type: Application
    Filed: January 21, 2005
    Publication date: July 12, 2007
    Inventor: Rafael Shapiro
  • Patent number: 7071365
    Abstract: The compositions 3-alkylated-5,5?,6,6?,7,7?,8,8?-octahydro-2,2?-binaphthol and 3,3?-dialkylated-5,5?,6,6?,7,7?,8,8?-octahydro-2,2?-binaphthol are disclosed, as well as various processes for making them, all involving the alkylation of 5,5?,6,6?,7,7?,8,8?-octahydro-2,2?-binaphthol.
    Type: Grant
    Filed: April 11, 2005
    Date of Patent: July 4, 2006
    Assignee: Invista North America S.A.R.L.
    Inventors: Helen S. M. Lu, Weiming Qiu, Rafael Shapiro
  • Publication number: 20060069270
    Abstract: A process for the preparation of 1,3,5-trisubstituted pyrazole compounds, which are useful intermediates in the synthesis of factor Xa inhibitors.
    Type: Application
    Filed: September 6, 2005
    Publication date: March 30, 2006
    Inventors: Rafael Shapiro, Lucius Rossano, Karen Tenhuisen
  • Publication number: 20060069258
    Abstract: A novel process and intermediates thereof for making 4,5-dihydro-pyrazolo[3,4-c]pyrid-2-ones of the type shown below from appropriate phenyl hydrazines is described. These compounds can be useful as factor Xa inhibitors.
    Type: Application
    Filed: September 26, 2005
    Publication date: March 30, 2006
    Inventors: Rafael Shapiro, Lucius Rossano, Boguslaw Mudryk, Nicolas Cuniere, Matthew Oberholzer, Huiping Zhang, Bang-Chi Chen
  • Publication number: 20050182279
    Abstract: The compositions 3-alkylated-5,5?,6,6?,7,7?,8,8?-octahydro-2,2?-binaphthol and 3,3?-dialkylated-5,5?, 6,6?,7,7?,8,8?-octahydro-2,2?-binaphthol are disclosed, as well as various processes for making them, all involving the alkylation of 5,5?,6,6?,7,7?,8,8?-octahydro-2,2?-binaphthol.
    Type: Application
    Filed: April 11, 2005
    Publication date: August 18, 2005
    Inventors: Helen Lu, Weiming Qiu, Rafael Shapiro
  • Publication number: 20040122252
    Abstract: Disclosed herein are methods for preparing nitrile derivatives and their corresponding amines from 1-,2-,4-trivinylcyclohexane by hydrocyanation, followed by hydrogenation. Also disclosed are novel compounds used in the methods described herein.
    Type: Application
    Filed: December 18, 2002
    Publication date: June 24, 2004
    Inventors: Alan M. Allgeier, Christian P. Lenges, Rafael Shapiro, Wilson Tam
  • Publication number: 20040054237
    Abstract: The compositions 3-alkylated-5,5′,6,6′,7,7′,8,8′-octahydro-2,2′-binaphthol and 3,3′-dialkylated-5,5′,6,6′,7,7′,8,8′-octahydro-2,2′-binaphthol are disclosed, as well as various processes for making them, all involving the alkylation of 5,5′,6,6′,7,7′,8,8′-octahydro-2,2′-binaphthol.
    Type: Application
    Filed: July 23, 2003
    Publication date: March 18, 2004
    Inventors: Helen S.M. Lu, Weiming Qiu, Rafael Shapiro
  • Publication number: 20040049087
    Abstract: A process for making a compound of the formula I 1
    Type: Application
    Filed: February 14, 2003
    Publication date: March 11, 2004
    Inventor: Rafael Shapiro