Oxygen Bonded Directly At The 6- Or 7-position (e.g., Chenodeoxycholic Acids, Ursodeoxycholic Acids, Etc.) Patents (Class 552/551)
  • Patent number: 5061701
    Abstract: A compounds of general formula I ##STR1## wherein R.sub.1 is hydrogen or hydroxy, and the hydroxy group at the 7-position can be either in .alpha. or .beta. configuration, are valuable in human therapy. Compounds I can be prepared by fluorination of the suitably protected 6-hydroxy-7-keto-derivatives.
    Type: Grant
    Filed: April 9, 1990
    Date of Patent: October 29, 1991
    Assignee: Giuliani S.p.A.
    Inventors: Roberto Pellicciari, Aldo Roda, Giuliano Frigerio
  • Patent number: 5057509
    Abstract: Compounds of general formula I ##STR1## wherein R.sub.1 is hydrogen or hydroxy, and the hydroxy group at the 7-position can be either in .alpha. or .beta. configuration, are valuable in human therapy. Compounds I can be prepared by reacting with succinic acid carbonanions the corresponding derivatives which have previously been protected, and subsequently deprotecting and decarboxylating them.
    Type: Grant
    Filed: April 9, 1990
    Date of Patent: October 15, 1991
    Assignee: Giuliani S.p.A.
    Inventors: Roberto Pellicciari, Aldo Roda, Giuliano Frigerio
  • Patent number: 4981983
    Abstract: New derivatives of chenodeoxycholic, ursodeoxy cholic, cholic and ursocholic acids, bearing a methyl group in the side chain in an alfa position to the carboxylic group, the corresponding nor- and di-nor- derivatives, and the corresponding conjugates with taurine and glycine, are described.The compounds of the invention are prepared by methylation of the esters with methyl iodide in the presence of lithium-dialkylamides.
    Type: Grant
    Filed: October 2, 1989
    Date of Patent: January 1, 1991
    Assignee: Gipharmex S.p.A.
    Inventors: Virginio Castagnola, E. Giuliano Frigerio, Roberto Pellicciari, Aldo Roda
  • Patent number: 4962099
    Abstract: A process for the production of disubstituted bile acid analogs, including the disubstituted analogs of such bile acids as, lithocholic, hyodeoxycholic, cholic, chenodeoxycholic and ursodeoxycholic acids.This invention was made in the course of work performed under a grant from the U.S. National Heart Lung and Blood Institute.
    Type: Grant
    Filed: January 5, 1989
    Date of Patent: October 9, 1990
    Assignee: Beth Israel Medical Center
    Inventors: Erwin H. Mosbach, Charles K. McSherry, Mizuho Une, Naoyuki Matoba
  • Patent number: 4950428
    Abstract: A novel process for the preparation of 20-keto-pregnanes.
    Type: Grant
    Filed: May 25, 1989
    Date of Patent: August 21, 1990
    Assignee: Roussel Uclaf
    Inventors: Michel Vivat, Jean Buendia
  • Patent number: 4927921
    Abstract: A compound of the formula ##STR1## wherein R.sub.1 is hydrogen or methyl, R.sub.2 is methyl or ethyl, and A,B,C and D rings optionally containing at least one double bond and optionally substituted with at least one member of the group consisting of optionally protected --OH, .dbd.O, alkyl and alkoxy of 1 to 4 carbon atoms, halogen and alkenyl and alkynyl of 2 to 4 carbon atoms, R is selected from the group consisting of halogen, --OH, alkylthio and alkoxy of 1 to 6 carbon atoms, aralkoxy, arylthio and aralkylthio of 7 to 15 carbon atoms and ##STR2## R.sub.3 and R.sub.4 are individually hydrogen, or alkyl of 1 to 6 carbon atoms or aralkyl of 7 to 15 carbon atoms or taken together with the nitrogen form a heterocycle optionally containing another nitrogen or oxygen atom, excepting the product in which R is methoxy, R.sub.1 and R.sub.2 each represent methyl, A ring carries a 3.beta.-acetoxy function and B ring contains a double bond in 5(6) useful as intermediates for the preparation of 20-keto-pregnanes.
    Type: Grant
    Filed: December 4, 1987
    Date of Patent: May 22, 1990
    Assignee: Roussel Uclaf
    Inventors: Michel Vivat, Jean Buendia
  • Patent number: 4921848
    Abstract: Compounds of formula I ##STR1## wherein: R.sub.1 is hydrogen or hydroxy, and the methyl and hydroxy groups at 6- and 7-positions respectively can be either in .alpha. or .beta. configuration, are useful in human therapy. Compounds I are prepared by methylation of the corresponding appropriately protected 7-keto-derivatives.
    Type: Grant
    Filed: October 19, 1988
    Date of Patent: May 1, 1990
    Assignee: Gipharmex S.P.A.
    Inventors: Giuliano Frigerio, Roberto Pellicciari, Aldo Roda