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.
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.
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
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
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.
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