Patents by Inventor Michelangelo Scalone

Michelangelo Scalone 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).

  • Salt and polymorphs of a DPPIV inhibitor
    Publication number: 20060217428
    Abstract: The invention is concerned with (S)-1-{[2-(5-Methyl-2-phenyl-oxazol-4-yl)-ethylamino]-acetyl}-pyrrolidine-2-carbonitrile mesylate and crystalline polymorphs of this compound. This compound and its polymorphic forms exhibits superior properties compared to the previously known compounds and can be used as medicament for the treatment of disorders which are associated with DPP-IV.
    Type: Application
    Filed: March 16, 2006
    Publication date: September 28, 2006
    Inventors: Stefan Abrecht, Andre Bubendorf, Stephan Goetzoe, Olaf Grassmann, Francois Montavon, Regina Moog, Franziska Rohrer, Armin Ruf, Michelangelo Scalone, Urs Schwitter, Shaoning Wang
  • Process for asymmetric hydrogenation of hexahydroquinoline salts
    Publication number: 20050148776
    Abstract: The asymmetrical hydrogenation of 1-(4-methoxybenzyl)-3,4,5,6,7,8-hexahydroisoquinolinium salts to yield (S) or (R)-1-(4-methoxybenzyl)-1,2,3,4,5,6,7,8-hexahydroisoquinolinium salts can be effected with superior optical yield by the use of an iridium or rhodium complex catalyst comprising a chiral dipohsphine ligand of the general formula (I) or (II), (S)-1-(4-methoxybenzyl)-1,2,3,4,5,6,7,8-hexahydroisoquinoline and salts thereof are intermediate products in the manufacture of dextromethorphan, a known antitussive agent.
    Type: Application
    Filed: March 13, 2003
    Publication date: July 7, 2005
    Applicant: DSM IP ASSETS B.V.
    Inventors: Kurt Puntener, Michelangelo Scalone, Shaoning Wang
  • Asymmetric synthesis process
    Patent number: 6914140
    Abstract: A novel process for the manufacture of compounds of the formula wherein R1 and R2 independently represent aroyl. The present invention also concerns novel intermediates used in the novel process for making compounds of formula I.
    Type: Grant
    Filed: April 10, 2000
    Date of Patent: July 5, 2005
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Peter Karl Matzinger, Michelangelo Scalone, Ulrich Zutter
  • Process for the production of chiral propionic acid derivatives
    Publication number: 20050070714
    Abstract: The present invention is concerned with a novel process for the preparation of compounds of formula I comprising catalytic asymmetric hydrogenation of a compound of formula (II) in the presence of a catalyst comprising ruthenium and a chiral diphosphine ligand or comprising rhodium and a chiral diphosphine ligand, wherein R1, R2, R3 and R4 are as defined in the specification and claims. The compounds of formula I and the corresponding salts and/or esters are pharmaceutically active substances.
    Type: Application
    Filed: September 2, 2004
    Publication date: March 31, 2005
    Inventors: Kurt Puentener, Michelangelo Scalone
  • Synthesis of 3,6-dialkyl-5,6-dihydro-4-hydroxy-pyran-2-one
    Patent number: 6858749
    Abstract: The present invention relates to a novel process for producing a ?-lactone of the formula: using an acyl halide of the formula: wherein R1, R2 R3 and X are described herein, as well as novel intermediates. In particular, the present invention relates to a process for enantioselectively producing the (R)-?-lactone.
    Type: Grant
    Filed: February 10, 2003
    Date of Patent: February 22, 2005
    Assignee: Roche Colorado Corporation
    Inventors: Michael P. Fleming, Yeun-Kwei Han, Lewis M. Hodges, David A. Johnston, Roger P. Micheli, Kurt Puentener, Chris R. Roberts, Michelangelo Scalone, Mark A. Schwindt, Robert J. Topping
  • Novel process for the preparation of the insulin sensitizer
    Publication number: 20040267023
    Abstract: A novel process for the preparation of compounds of formula I 1
    Type: Application
    Filed: June 21, 2004
    Publication date: December 30, 2004
    Inventors: Wolfgang Goehring, Ursula Hoffmann, Michelangelo Scalone, Helmut Stahr, Shaoning Wang
  • Synthesis of 3,6-dialkyl-5,6-dihydro-4-hydroxy-pyran-2-one
    Patent number: 6818789
    Abstract: The present invention relates to a novel process for producing a &dgr;-lactone of the formula: using an acyl halide of the formula: wherein R1, R2 R3 and X are described herein, as well as novel intermediates. In particular, the present invention relates to a process for enantioselectively producing the (R)-&dgr;-lactone.
    Type: Grant
    Filed: February 10, 2003
    Date of Patent: November 16, 2004
    Assignee: Roche Colorado Corporation
    Inventors: Michael P. Fleming, Yeun-Kwei Han, Lewis M. Hodges, David A. Johnston, Roger P. Micheli, Kurt Puentener, Chris R. Roberts, Michelangelo Scalone, Mark A. Schwindt, Robert J. Topping
  • Isoquinoline derivatives
    Patent number: 6818774
    Abstract: Disclosed are isoquinolino derivatives of the formula wherein Y is >C═O or —CH2—, Z is >C═O or —CH2—, and R1, R2 and m are as defined herein as well as the pharmaceutically acceptable salts thereof. These compounds are MAO-B selective inhibitors useful, inter alia, in the treatment of Alzheimer's disease and/or senile dementia.
    Type: Grant
    Filed: April 16, 2003
    Date of Patent: November 16, 2004
    Assignee: Hoffman-La Roche Inc.
    Inventors: Andrea Cesura, Rosa Maria Rodriguez Sarmiento, Michelangelo Scalone, Andrew William Thomas, Rene Wyler
  • Process for preparing heterocyclic indene analogs
    Patent number: 6777559
    Abstract: A process for the preparation heterocyclic indene analogs, especially with the preparation of 4-hydroxycarbazole or N-protected 4-hydroxycarbazole, involves cyclocarbonylation followed by saponification. This process avoids high temperatures and high catalyst loadings.
    Type: Grant
    Filed: January 22, 2002
    Date of Patent: August 17, 2004
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Michelangelo Scalone, Thomas Albert Zeibig
  • Process for preparing heterocyclic indene analogs
    Publication number: 20040127723
    Abstract: A process for the preparation heterocyclic indene analogs, especially with the preparation of 4-hydroxycarbazole or N-protected 4-hydroxycarbazole, involves cyclocarbonylation followed by saponification. This process avoids high temperatures and high catalyst loadings.
    Type: Application
    Filed: January 22, 2004
    Publication date: July 1, 2004
    Inventors: Michelangelo Scalone, Thomas Albert Zeibig
  • Process for the preparation of thiazolidinedione derivatives
    Patent number: 6753432
    Abstract: The present invention is concerned with a novel process for the preparation of compounds of formula I comprising bromomethylation or chloromethylation of a compound of formula II and subsequent reaction with a compound of formula IV The compounds of formula I and the corresponding salts, e.g. the sodium salts, are pharmaceutically active substances.
    Type: Grant
    Filed: August 5, 2003
    Date of Patent: June 22, 2004
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Michelangelo Scalone
  • Synthesis of 3,6-dialkyl-5,6-dihydro-4-hydroxy-pyran-2-one
    Patent number: 6743927
    Abstract: The present invention relates to a novel process for producing a &dgr;-lactone of the formula: using an acyl halide of the formula: wherein R1, R2 R3 and X are described herein, as well as novel intermediates. In particular, the present invention relates to a process for enantioselectively producing the (R)-&dgr;-lactone.
    Type: Grant
    Filed: February 10, 2003
    Date of Patent: June 1, 2004
    Assignee: Roche Colorado Corporation
    Inventors: Michael P. Fleming, Yeun-Kwei Han, Lewis M. Hodges, David A. Johnston, Roger P. Micheli, Kurt Puentener, Chris R. Roberts, Michelangelo Scalone, Mark A. Schwindt, Robert J. Topping
  • Process for the preparation of thiazolidinedione derivatives
    Publication number: 20040024222
    Abstract: The present invention is concerned with a novel process for the preparation of compounds of formula I 1
    Type: Application
    Filed: August 5, 2003
    Publication date: February 5, 2004
    Inventor: Michelangelo Scalone
  • Isoquinoline derivatives
    Publication number: 20030225122
    Abstract: Disclosed are isoquinolino derivatives of the formula 1
    Type: Application
    Filed: April 16, 2003
    Publication date: December 4, 2003
    Inventors: Andrea Cesura, Rosa Maria Rodriquez Sarmiento, Michelangelo Scalone, Andrew William Thomas, Rene Wyler
  • Process for the preparation of thiazolidinedione derivatives
    Patent number: 6620941
    Abstract: The present invention is concerned with a novel process for the preparation of compounds of formula I comprising bromomethylation or chloromethylation of a compound of formula II and subsequent reaction with a compound of formula IV The compounds of formula I and the corresponding salts, e.g. the sodium salts, are pharmaceutically active substances.
    Type: Grant
    Filed: November 5, 2002
    Date of Patent: September 16, 2003
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Michelangelo Scalone
  • Synthesis of 3,6-dialkyl-5,6-dihydro-4-hydroxy-pyran-2-one
    Publication number: 20030171602
    Abstract: The present invention relates to a novel process for producing a &dgr;-lactone of the formula: 1
    Type: Application
    Filed: February 10, 2003
    Publication date: September 11, 2003
    Applicant: Roche Colorado Corporation
    Inventors: Michael P. Fleming, Yeun-Kwei Han, Lewis M. Hodges, David A. Johnston, Roger P. Micheli, Kurt Puentener, Chris R. Roberts, Michelangelo Scalone, Mark A. Schwindt, Rober J. Topping
  • Synthesis of 3,6-dialkyl-5,6-dihydro-4-hydroxy-pyran-2-one
    Publication number: 20030158423
    Abstract: The present invention relates to a novel process for producing a &dgr;-lactone of the formula: 1
    Type: Application
    Filed: February 10, 2003
    Publication date: August 21, 2003
    Applicant: Roche Colorado Corporation
    Inventors: Michael P. Fleming, Yeun-Kwei Han, Lewis M. Hodges, David A. Johnston, Roger P. Micheli, Kurt Puentener, Chris R. Roberts, Michelangelo Scalone, Mark A. Schwindt, Robert J. Topping
  • Synthesis of 3,6-dialkyl-5,6-dihydro-4-hydroxy-pyran-2-one
    Publication number: 20030158422
    Abstract: The present invention relates to a novel process for producing a &dgr;-lactone of the formula: 1
    Type: Application
    Filed: February 10, 2003
    Publication date: August 21, 2003
    Applicant: Roche Colorado Corporation
    Inventors: Michael P. Fleming, Yeun-Kwei Han, Lewis M. Hodges, David A. Johnston, Roger P. Mitcheli, Kurt Puentener, Chris R. Roberts, Michelangelo Scalone, Mark A. Schwindt, Robert J. Topping
  • Process for the preparation of ethanesul fonyl-piperidine derivatives
    Patent number: 6605723
    Abstract: The present invention relates to a new process for the preparation of compounds of the formulae and their pharmaceutically acceptable acid addition salts, which are NMDA (N-methyl-D-aspartate)-receptor-subtype selective blockers.
    Type: Grant
    Filed: March 15, 2001
    Date of Patent: August 12, 2003
    Assignee: Hoffman-La Roche Inc.
    Inventors: Yvo Crameri, Michelangelo Scalone, Pius Waldmeier, Ulrich Widmer
  • Process for the preparation of thiazolidinedione derivatives
    Publication number: 20030092916
    Abstract: The present invention is concerned with a novel process for the preparation of compounds of formula I 1
    Type: Application
    Filed: November 5, 2002
    Publication date: May 15, 2003
    Inventor: Michelangelo Scalone