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).

  • Patent number: 5902882
    Abstract: A novel process for the manufacture of compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2 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 3, 1997
    Date of Patent: May 11, 1999
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Peter Karl Matzinger, Michelangelo Scalone, Ulrich Zutter
  • Patent number: 5880285
    Abstract: A process for the manufacture of optically active (R)- or (S)-1-(4-methoxy-benzyl)-1,2,3,4,5,6,7,8-octahydro-isoquinoline adducts of the formula ##STR1## wherein HX signifies a mineral acid from the group of HBF.sub.4, H.sub.2 SO.sub.4, HPF.sub.6, HBr, HI, HCl,HSbF.sub.6 or HClO.sub.4, or a strong organic acid from the group of C.sub.1-8 -alkylSO.sub.3 H, picric acid, formic acid, a lower alkylsulphonic acid or arylcarboxylic acid or a dicarboxylic acid,from a compound of the formula ##STR2## wherein HX has the significance given above, by asymmetric hydrogenation in the presence of a complex consisting of optically active diphosphine ligands with iridium, optionally in the presence of an additive.
    Type: Grant
    Filed: December 18, 1997
    Date of Patent: March 9, 1999
    Assignee: Roche Vitamins Inc.
    Inventors: Emil Albin Broger, Michelangelo Scalone, Christof Wehrli
  • Patent number: 5534635
    Abstract: It has been found that pyridine-2-carboxamides of the formula ##STR1## wherein R is amino or a residue convertible into amino, and pharmaceutically usable acid addition salts of that carboxamide in which R is amino can be prepared in a simple manner and in good yield by reacting 2,5-dichloropyridine in the presence of a palladium-phosphine catalyst with an alkyne of the formulaR.sup.1 --C.tbd.CH IIIwherein R.sup.1 is hydrogen, lower-alkyl, trimethylsilyl or the group --(R.sup.2)(R.sup.3)--COH and R.sup.2 and R.sup.3 each independently are hydrogen or lower-alkyl or together are cyclopentyl or cyclohexyl,oxidizing the resulting alkyne to give 5-chloropyridine-2-carboxylic acid and reacting this acid or a reactive functional derivative thereof with an amino compound of the formulaor with carbon monoxide and an amino compound of formula VI or with carbon monoxide and a lower alkanol which is optionally mixed with water and reacting the resulting acid or the resulting ester with an amino compound of formula VI.
    Type: Grant
    Filed: September 12, 1994
    Date of Patent: July 9, 1996
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Michelangelo Scalone, Peter Vogt
  • Patent number: 5393900
    Abstract: The invention comprises compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2 are hydrogen or acyl; provided that only one of R.sup.1 or R.sup.2 is hydrogen, useful in the treatment of hyperproliferative skin diseases and sebaceous gland diseases. The invention also includes a process for making these compounds and steroid intermediates of the process.
    Type: Grant
    Filed: June 7, 1994
    Date of Patent: February 28, 1995
    Assignee: Hoffmann-La Roche inc.
    Inventors: Thomas I. Doran, John A. McLane, Masami Okabe, Michelangelo Scalone, Milan R. Uskokovic
  • Patent number: 5380861
    Abstract: It has been found that pyridine-2-carboxamides of the formula ##STR1## wherein R is amino or a residue convertible into amino, and pharmaceutically usable acid addition salts of that carboxamide in which R is amino can be prepared in a simple manner and in good yield by reacting 2,5-dichloropyridine in the presence of a palladium-phosphine catalyst with an alkyne of the formulaR.sup.1 -C.tbd.CH IIIwherein R.sup.1 is hydrogen, lower-alkyl, trimethylsilyl or the group --(R.sup.2)(R.sup.3)--COH and R.sup.2 and R.sup.3 each independently are hydrogen or lower-alkyl or together are cyclopentyl or cyclohexyl,oxidizing the resulting alkyne to give 5-chloropyridine-2-carboxylic acid and reacting this acid or a reactive functional derivative thereof with an amino compound of the formula VI. The compound of formula I in which R is amino is a known compound which is a reversible and highly active MAO-B inhibitor.
    Type: Grant
    Filed: May 25, 1993
    Date of Patent: January 10, 1995
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Michelangelo Scalone, Peter Vogt
  • Patent number: 5342833
    Abstract: The invention is drawn to compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2 are hydrogen or acyl; provided that only one of R.sup.1 or R.sup.2 is hydrogen, useful in the treatment of hyperproliferative skin diseases and sebaceous gland diseases.
    Type: Grant
    Filed: November 22, 1993
    Date of Patent: August 30, 1994
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Thomas I. Doran, John A. McLane, Masami Okabe, Michelangelo Scalone, Milan R. Uskokovic
  • Patent number: 5110955
    Abstract: The invention relates to a process for the manufacture of vinylchromanes. This process is concerned with the manufacture of the compounds having the formula ##STR1## wherein R.sup.o is hydrogen or a cleavable protecting group, and comprises cyclizing a compound having the formula ##STR2## wherein R.sup.o is defined above and R.sup.1 is--CH.sub.2 --CH.sub.2 --C(W)(CH.sub.3)--CH.dbd.CH.sub.2 or--CH.sub.2 --CH.sub.2 C(CH.sub.3).dbd.CH--CH.sub.2 --Wwhere W is a leaving group,by means of a chiral transition metal-diphosphine complex.The compounds of formula I are useful intermediates, e.g. in the manufacture of (R,R,R)-.alpha.-tocopherol.
    Type: Grant
    Filed: April 5, 1990
    Date of Patent: May 5, 1992
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Andreas Knierzinger, Michelangelo Scalone