Patents by Inventor Eric N. Jacobsen

Eric N. Jacobsen 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).

  • Compound reagents and method for synthesizing enantiomerically enriched amino acids
    Patent number: 8859812
    Abstract: Described herein are compounds of formula (I), related compositions, and their use, for example in the formation of ?-amino acids or a precursor thereof such as an ?-aminonitrile.
    Type: Grant
    Filed: September 8, 2010
    Date of Patent: October 14, 2014
    Assignee: President and Fellows of Harvard College
    Inventors: Eric N. Jacobsen, Stephan J. Zuend
  • COMPOUNDS AND RELATED METHODS OF USE
    Publication number: 20130066109
    Abstract: Described herein are compounds of formula (I), related compositions, and their use, for example in the formation of ?-amino acids or a precursor thereof such as an ?-aminonitrile.
    Type: Application
    Filed: September 8, 2010
    Publication date: March 14, 2013
    Applicant: PRESIDENTS AND FELLOWS OF HARVARD COLLEGE
    Inventors: Eric N. Jacobsen, Stephan J. Zuend
  • Process for Synthesizing 7-Alkynyl-4- Aminoquinazolines and a Related Intermediate
    Publication number: 20100048898
    Abstract: A process for synthesizing 7-alkynyl-4-aminoquinazolines from 7-haloquinazolines is disclosed. In one specific synthesis, 4-[N-3-chloro-4-fluorophenyl)]-7-[3-methyl-3-(4-methyl-1-piperazinyl)-1-butynyl]-6-[N-methyl acrylamide]quinazoline is prepared from 7-chloro-6-nitro-3H-quinazolin-4-one. Also disclosed is an intermediate useful in the syntheses of 7-alkynyl-4-ammoquinaozolines and a process for making the intermediate. The 7-alkynyl-4-aminoquinaozolines prepared by processes of the invention are useful as pharmaceutically active compounds.
    Type: Application
    Filed: March 2, 2007
    Publication date: February 25, 2010
    Inventor: Eric N. Jacobsen
  • Hydrolytic kinetic resolution of cyclic substrates
    Patent number: 7220870
    Abstract: The present invention relates to a process for stereoselective or regioselective chemical synthesis which generally comprises reacting a nucleophile and a chiral or prochiral cyclic substrate in the presence of a non-racemic, chiral catalyst to produce a stereoisomerically- and/or regioisomerically-enriched product. The present invention also relates to hydrolytic kinetic resolutions of racemic and diastereomeric mixtures of epoxides.
    Type: Grant
    Filed: January 5, 2005
    Date of Patent: May 22, 2007
    Assignee: President and Fellows of Harvard College
    Inventors: Eric N. Jacobsen, Makoto Tokunaga, Jay F. Larrow
  • Main-group metal-based asymmetric catalysts and applications thereof
    Patent number: 6844448
    Abstract: The present invention relates to a method and catalysts for the stereoselective addition of a nucleophile to a reactive ?-bond of a substrate. The chiral, non-racemic catalysts of the present invention constitute the first examples of catalysts for nucleophilic additions that comprise a main-group metal and a tri- or tetra-dentate ligand.
    Type: Grant
    Filed: December 20, 2002
    Date of Patent: January 18, 2005
    Assignee: President and Fellows of Harvard College
    Inventors: Eric N. Jacobsen, Matthew S. Sigman
  • Nucleophilic kinetic resolution of cyclic substrates using silyl azides
    Patent number: 6841667
    Abstract: The present invention relates to a process for stereoselective or regioselective chemical synthesis which generally comprises reacting a nucleophile and a chiral or prochiral cyclic substrate in the presence of a non-racemic, chiral catalyst to produce a stereoisomerically- and/or regioisomerically-enriched product. The present invention also relates to hydrolytic kinetic resolutions of racemic and diastereomeric mixtures of epoxides.
    Type: Grant
    Filed: July 7, 2003
    Date of Patent: January 11, 2005
    Assignee: President and Fellows of Harvard College
    Inventors: Eric N. Jacobsen, Makoto Tokunaga, Jay F. Larrow
  • Parallel combinatorial approach to the discovery and optimization of catalysts and uses thereof
    Publication number: 20040235023
    Abstract: The present invention provides methods and compositions, i.e. synthetic libraries of candidate compounds, useful in the discovery and optimization of compounds which catalyze at least one chemical transformation. In certain instances, the subject compounds catalyze a chemoselective, regioselective, stereoselective or enantioselective transformation.
    Type: Application
    Filed: March 17, 2004
    Publication date: November 25, 2004
    Inventors: Eric N. Jacobsen, Matthew S. Sigman
  • Hydrolytic kinetic resolution of cyclic substrates
    Patent number: 6800766
    Abstract: The present invention relates to a process for stereoselective or regioselective chemical synthesis which generally comprises reacting a nucleophile and a chiral or prochiral cyclic substrate in the presence of a non-racemic, chiral catalyst to produce a stereoisomerically- and/or regioisomerically-enriched product. The present invention also relates to hydrolytic kinetic resolutions of racemic and diastereomeric mixtures of epoxides.
    Type: Grant
    Filed: July 26, 2002
    Date of Patent: October 5, 2004
    Assignee: President and Fellows of Harvard College
    Inventors: Eric N. Jacobsen, Makoto Tokunaga, Jay F. Larrow
  • Parallel combinatorial approach to the discovery and optimization of catalysts and uses thereof
    Patent number: 6709824
    Abstract: The present invention provides methods and compositions, i.e. synthetic libraries of candidate compounds, useful in the discovery and optimization of compounds which catalyze at least one chemical transformation. In certain instances, the subject compounds catalyze a chemoselective, regioselective, stereoselective or enantioselective transformation.
    Type: Grant
    Filed: September 24, 2001
    Date of Patent: March 23, 2004
    Assignee: President and Fellows of Harvard College
    Inventors: Eric N. Jacobsen, Matthew S. Sigman
  • Nucleophilic kinetic resolution of cyclic substrates using silyl azides
    Publication number: 20040044233
    Abstract: The present invention relates to a process for stereoselective or regioselective chemical synthesis which generally comprises reacting a nucleophile and a chiral or prochiral cyclic substrate in the presence of a non-racemic, chiral catalyst to produce a stereoisomerically- and/or regioisomerically-enriched product. The present invention also relates to hydrolytic kinetic resolutions of racemic and diastereomeric mixtures of epoxides.
    Type: Application
    Filed: July 7, 2003
    Publication date: March 4, 2004
    Inventors: Eric N. Jacobsen, Makoto Tokunaga, Jay F. Larrow
  • Hydrolytic kinetic resolution of epoxides
    Patent number: 6693206
    Abstract: The present invention provides a process for the preparation of an enantiomerically enriched non-racemic chiral diol and an enantiomerically enriched non-racemic chiral epoxy compound by a hydrolytic kinetic resolution reaction. The process includes the step of contacting oxygen and mixture including a racemic chiral epoxy compound, a non-racemic Co(II) complex catalyst, an aromatic carboxylic acid and water, at a temperature and length of time sufficient to produce a mixture of said non-racemic chiral diol and said non-racemic chiral epoxy compound. The present invention also provides a process for the preparation of an enantiomerically enriched non-racemic chiral diol and an enantiomerically enriched non-racemic chiral epoxy compound by a hydrolytic kinetic resolution reaction.
    Type: Grant
    Filed: August 22, 2002
    Date of Patent: February 17, 2004
    Assignee: Rhodia Chirex, Inc.
    Inventors: Yi Liu, Marcello DiMare, Salvatore Anthony Marchese, Eric N. Jacobsen, Serge Jasmin
  • Main-group metal-based asymmetric catalysts and applications thereof
    Publication number: 20030187249
    Abstract: The present invention relates to a method and catalysts for the stereoselective addition of a nucleophile to a reactive &pgr;-bond of a substrate. The chiral, non-racemic catalysts of the present invention constitute the first examples of catalysts for nucleophilic additions that comprise a main-group metal and a tri- or tetra-dentate ligand.
    Type: Application
    Filed: December 20, 2002
    Publication date: October 2, 2003
    Inventors: Eric N. Jacobsen, Matthew S. Sigman
  • Hydrolytic kinetic resolution of cyclic substrates
    Publication number: 20030139614
    Abstract: The present invention relates to a process for stereoselective or regioselective chemical synthesis which generally comprises reacting a nucleophile and a chiral or prochiral cyclic substrate in the presence of a non-racemic, chiral catalyst to produce a stereoisomerically- and/or regioisomerically-enriched product. The present invention also relates to hydrolytic kinetic resolutions of racemic and diastereomeric mixtures of epoxides.
    Type: Application
    Filed: July 26, 2002
    Publication date: July 24, 2003
    Inventors: Eric N. Jacobsen, Makoto Tokunaga, Jay F. Larrow
  • Hydrolytic kinetic resolution of epoxides
    Publication number: 20030073855
    Abstract: The present invention provides a process for the preparation of an enantiomerically enriched non-racemic chiral diol and an enantiomerically enriched non-racemic chiral epoxy compound by a hydrolytic kinetic resolution reaction. The process includes the step of contacting oxygen and mixture including a racemic chiral epoxy compound, a non-racemic Co(II) complex catalyst, an aromatic carboxylic acid and water, at a temperature and length of time sufficient to produce a mixture of said non-racemic chiral diol and said non-racemic chiral epoxy compound. The present invention also provides a process for the preparation of an enantiomerically enriched non-racemic chiral diol and an enantiomerically enriched non-racemic chiral epoxy compound by a hydrolytic kinetic resolution reaction.
    Type: Application
    Filed: August 22, 2002
    Publication date: April 17, 2003
    Applicant: Rhodia ChiRex, Inc.
    Inventors: Yi Liu, Marcello DiMare, Salvatore Anthony Marchese, Eric N. Jacobsen, Serge Jasmin
  • Main-group metal based asymmetric catalysts and applications thereof
    Patent number: 6521561
    Abstract: The present invention relates to a method and catalysts for the stereoselective addition of a nucleophile to a reactive &pgr;-bond of a substrate. The chiral, non-racemic catalysts of the present invention constitute the first examples of catalysts for nucleophilic additions that comprise a main-group metal and a tri- or tetra-dentate ligand.
    Type: Grant
    Filed: May 1, 1998
    Date of Patent: February 18, 2003
    Assignee: President and Fellows of Harvard College
    Inventors: Eric N. Jacobsen, Matthew S. Sigman
  • Combinatorial approach for generating novel coordination complexes
    Patent number: 6489093
    Abstract: The present invention provides methods and compositions, i.e. synthetic libraries of binding moities, for identifying compounds which bind to a metal atom or to non-metal ions, e.g., cationic or anionic molecules.
    Type: Grant
    Filed: September 19, 1997
    Date of Patent: December 3, 2002
    Assignee: President and Fellows of Harvard College
    Inventors: Eric N. Jacobsen, Matthew B. Francis, Nathaniel S. Finney
  • Hydrolytic kinetic resolution of cyclic substrates
    Patent number: 6448414
    Abstract: The present invention relates to a process for stereoselective or regioselective chemical synthesis which generally comprises reacting a nucleophile and a chiral or prochiral cyclic substrate in the presence of a non-racemic, chiral catalyst to produce a stereoisomerically- and/or regioisomerically-enriched product. The present invention also relates to hydrolytic kinetic resolutions of racemic and diastereomeric mixtures of epoxides.
    Type: Grant
    Filed: July 5, 2001
    Date of Patent: September 10, 2002
    Assignee: President and Fellows of Harvard College
    Inventors: Eric N. Jacobsen, Makoto Tokunaga, Jay F. Larrow
  • Parallel combinatorial approach to the discovery and optimization of catalysts and uses thereof
    Publication number: 20020102612
    Abstract: The present invention provides methods and compositions, i.e. synthetic libraries of candidate compounds, useful in the discovery and optimization of compounds which catalyze at least one chemical transformation. In certain instances, the subject compounds catalyze a chemoselective, regioselective, stereoselective or enantioselective transformation.
    Type: Application
    Filed: September 24, 2001
    Publication date: August 1, 2002
    Inventors: Eric N. Jacobsen, Matthew S. Sigman
  • Asymmetric cycloaddition reactions
    Patent number: 6369223
    Abstract: The present invention relates to a process for stereoselective cycloaddition reactions which generally comprises a cycloaddition reaction between a pair of substrates, each either chiral or prochiral, that contain reactive &pgr;-systems, in the presence of a non-racemic chiral catalyst, to produce a stereoisomerically enriched product. The present invention also relates to novel asymmetric catalyst complexes comprising a metal and an asymmetric tridentate ligand.
    Type: Grant
    Filed: January 4, 2001
    Date of Patent: April 9, 2002
    Assignee: President and Fellows of Harvard College
    Inventors: Eric N. Jacobsen, Scott E. Schaus, Alexander G. Dossetter, Timothy F. Jamison
  • Hydrolytic kinetic resolution of cyclic substrates
    Publication number: 20020032338
    Abstract: The present invention relates to a process for stereoselective or regioselective chemical synthesis which generally comprises reacting a nucleophile and a chiral or prochiral cyclic substrate in the presence of a non-racemic, chiral catalyst to produce a stereoisomerically- and/or regioisomerically-enriched product. The present invention also relates to hydrolytic kinetic resolutions of racemic and diastereomeric mixtures of epoxides.
    Type: Application
    Filed: July 5, 2001
    Publication date: March 14, 2002
    Inventors: Eric N. Jacobsen, Makoto Tokunaga, Jay F. Larrow