Exactly One Oxygen Bonded Directly To The Cyclopentanohydrophenanthrene Ring System (e.g., 3-hydroxycholanic Acids, Lithocholic Acids, Etc.) Patents (Class 552/552)
  • Patent number: 5120724
    Abstract: Aldosterone biosynthesis inhibitors having substantially no intrinsic antiandrogenic activity are disclosed as well as pharmaceutical compositions containing such compounds and methods of treatment utilizing these compositions.
    Type: Grant
    Filed: October 15, 1991
    Date of Patent: June 9, 1992
    Assignee: Baker Cummins Pharmaceuticals, Inc.
    Inventors: Jack Fishman, Elliot Hahn, Gregory A. Smith
  • Patent number: 5086047
    Abstract: A compound selected from the group consisting of a compound of the formula ##STR1## wherein R is selected from the group consisting of hydrogen, alkyl, alkylthio and haloalkyl of 1 to 6 carbon atoms, alkenyl and alkynyl of 2 to 6 carbon atoms, optionally substituted arylthio of 6 to 10 carbon atoms, aryl of 6 to 12 carbon atoms, acyl of an organic carboxylic acid of 1 to 12 carbon atoms, --CN, cycloalkyl of 3 to 6 carbon atoms and --(CH.sub.2).sub.m --Re, m is an integer from 1 to 3, Re is --OH or --SH or --Salk, Alk is alkyl of 1 to 6 carbon atoms, X is selected from the group consisting of oxygen, N--O--R.sub.1, ##STR2## or =X is H.sub.2 or ##STR3## R.sub.A and R.sub.B are individually selected from the group consisting of hydrogen, halogen and alkyl of 1 to 6 carbon atoms, R.sub.1 is hydrogen or alkyl of 1 to 6 carbon, R' is hydrogen or acyl, the wavy lines indicate --or -position, Y is selected from the group consisting of oxygen, NOR, ##STR4## or =Y is ##STR5## H.sub.
    Type: Grant
    Filed: December 24, 1990
    Date of Patent: February 4, 1992
    Assignee: Roussel Uclaf, Department des Brevets
    Inventors: Jean-Francois Gourvest, Dominique Lesuisse
  • Patent number: 5064822
    Abstract: Novel 3-keto-19-nor-.DELTA..sup.4,9 -steroids of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of naphthyl, phenylphenyl, alkyl of 1 to 6 carbon atoms, alkenyl of 2 to 6 carbon atoms optionally containing additional unsaturations, phenoxy, furyl, cycloalkyl of 3 to 6 carbon atoms, thienyl optionally substituted with at least one member of the group consisting of halogen and alkyl and haloalkyl of 1 to 6 carbon atoms and phenyl optionally substituted with at least one member of the group consisting of --OH, halogen, --CF.sub.3, alkyl and alkoxy of 1 to 6 carbon atoms, alkenyloxy of 2 to 6 carbon atoms, phenoxy and alkylthio of 1 to 6 carbon atoms optionally oxidized to the sulfoxide or sulfone, R.sub.2 is selected from the group consisting of methyl and ethyl, R.sub.
    Type: Grant
    Filed: November 16, 1989
    Date of Patent: November 12, 1991
    Assignee: Roussel Uclaf
    Inventors: Daniel Philibert, Jean G. Teutsch, Germain Costerousse, Roger Deraedt
  • Patent number: 5041433
    Abstract: Invented are carboxyl and carboxyl alkyl ester substituted 11-keto and hydroxy analogues of synthetic steroidal compounds, pharmaceutical compositions containing these compounds, and methods of using these compounds to inhibit steroid 5-.alpha.-reductase.
    Type: Grant
    Filed: November 1, 1989
    Date of Patent: August 20, 1991
    Assignee: SmithKline Beecham Corporation
    Inventors: Dennis A. Holt, Brian W. Metcalf, Mark A. Levy
  • 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: 4954446
    Abstract: Invented are substituted acrylate analogues of steroidal synthetic compounds, pharmaceutial compositions containing the compounds, and methods of using these compounds to inhibit steroid 5-.alpha.-reductase including using these compounds to reduce prostate size. Also invented are intermediates used in preparing these compounds.
    Type: Grant
    Filed: July 14, 1989
    Date of Patent: September 4, 1990
    Assignee: SmithKline Beecham Corporation
    Inventors: Dennis A. Holt, Mark A. Levy, Brian W. Metcalf
  • 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