Patents by Inventor Silvio Campagna

Silvio Campagna 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).

  • Asymmetric synthesis of amino-pyrrolidinones
    Patent number: 6770763
    Abstract: A novel process for the asymmetric synthesis of an amino-pyrrolidinone of the type shown below from appropriate pyrrolidinones is described. These compounds are useful as intermediates for MMP and TACE inhibitors.
    Type: Grant
    Filed: March 14, 2003
    Date of Patent: August 3, 2004
    Assignee: Bristol-Myers Squibb Company
    Inventors: Nicholas A. Magnus, Pasquale N. Confalone, Scott A. Savage, Matthew Yates, Robert E. Waltermir, David J. Meloni, Silvio Campagna
  • Asymmetric synthesis of amino-pyrrolidinones and a crystalline, free-base amino-pyrrolidinone
    Publication number: 20040006137
    Abstract: A novel process for the asymmetric synthesis of an amino-pyrrolidinone of the type shown below is described.
    Type: Application
    Filed: March 14, 2003
    Publication date: January 8, 2004
    Inventors: Robert E. Waltermire, Silvio Campagna, Scott A. Savage, Shailendra Bordawekar, Thomas P. Maduskuie, Sridhar Desikan, Stephen R. Anderson
  • Asymmetric synthesis of amino-pyrrolidinones
    Publication number: 20030236401
    Abstract: A novel process for the asymmetric synthesis of an amino-pyrrolidinone of the type shown below from appropriate pyrrolidinones is described.
    Type: Application
    Filed: March 14, 2003
    Publication date: December 25, 2003
    Inventors: Nicholas A. Magnus, Pasquale N. Confalone, Scott A. Savage, Matthew Yates, Robert E. Waltermire, David J. Meloni, Silvio Campagna
  • Process for the preparation of macrocyclic metalloprotease inhibitors
    Patent number: 6562963
    Abstract: The present invention is directed to a process for the preparation of a compound of formula (X-a) or a pharmaceutically acceptable salt form thereof, wherein: R1 is selected from the group consisting of: C1-5 alkyl substituted with 0-5 R1a, —(CH2)r—C3-10 cycloalkyl substituted with 0-5 R1a, and —(CH2)r-aryl substituted with 0-5 R1a. Compounds of Formula (X-a) are macrocyclic molecules containing anti-succinate residues which inhibit metalloproteinases such as aggrecanase, and the production of tumor necrosis factor (TNF). The anti-succinates are formed by an Ireland Claisen rearrangement of a silyl ketene acetal which proceeds with high stereoselectivity.
    Type: Grant
    Filed: July 31, 2001
    Date of Patent: May 13, 2003
    Inventors: Roberta L. Dorow, Silvio Campagna, Pasquale N. Confalone, Fuqiang Jin, Zhe Wang
  • Process for the preparation of macrocyclic metalloprotease inhibitors
    Publication number: 20020013459
    Abstract: The present invention relates to processes for the preparation of macrocyclic molecules containing anti-succinate residues which inhibit metalloproteinases such as aggrecanase, and the production of tumor necrosis factor (TNF). The anti-succinates are formed by an Ireland Claisen rearrangement of a silyl ketene acetal which proceeds with high stereoselectivity.
    Type: Application
    Filed: July 31, 2001
    Publication date: January 31, 2002
    Inventors: Roberta L. Dorow, Silvio Campagna, Pasquale N. Confalone, Fuqiang Jin, Zhe Wang
  • Process for the preparation of macrocyclic metalloprotease inhibitors
    Patent number: 6307044
    Abstract: The present invention is directed to a process for the preparation of a compound of formula (X-a): or a pharmaceutically acceptable salt form thereof, wherein: R1 is selected from the group consisting of: C1-5 alkyl substituted with 0-5 R1a, —(CH2)r—C3-10 cycloalkyl substituted with 0-5 R1a, and —(CH2)r-aryl substituted with 0-5 R1a. Compounds of Formula (X-a) are macrocyclic molecules containing anti-succinate residues which inhibit metalloproteinases such as aggrecanase, and the production of tumor necrosis factor (TNF). The anti-succinates are formed by an Ireland Claisen rearrangement of a silyl ketene acetal which proceeds with high stereoselectivity.
    Type: Grant
    Filed: June 10, 1999
    Date of Patent: October 23, 2001
    Assignee: DuPont Pharmaceuticals Company
    Inventors: Roberta L. Dorow, Silvio Campagna, Pasquale N. Confalone, Fuqiang Jin, Zhe Wang
  • Process for the preparation of cyclopropylacetylene
    Patent number: 6288297
    Abstract: The present invention relates generally to novel methods for the synthesis of cyclopropylacetylene which is an essential reagent in the asymmetric synthesis of (S)-6-chloro-4-cyclopropylethynyl-4-trifluoromethyl-1,4-dihydro-2H-3,1-benzoxazin-2-one; a useful human immunodeficiency virus (HIV) reverse transcriptase inhibitor. In the process, for example, cyclopropane carboxaldehyde is alkylated to form 1,1,1-trichloro-2-cyclopropyl-ethanol; which in turn is hydroxy protected to form 1,1,1-trichloro-2-cyclopropylethyltosylate; which in turn undergoes elimination to form cyclopropyl acetylene. This improvement provides for high conversion of inexpensive, readily available starting materials into cyclopropylacetylene, high overall yields and can be conducted on an industrial scale.
    Type: Grant
    Filed: September 30, 1999
    Date of Patent: September 11, 2001
    Assignee: Dupont Pharmaceuticals Company
    Inventors: Zhe Wang, Jianguo Yin, Joseph M. Fortunak, Silvio Campagna