Carbon Chain Having Carbon-to-carbon Unsaturation Bonded Directly At The 17 Position Of The Cyclopentanohydrophenanthrene Ring System Patents (Class 540/40)
  • Patent number: 5756722
    Abstract: The novel intermediates of the formula ##STR1## wherein L, K and M are as defined in the specification which are useful intermediates for the preparation of .DELTA..sup.4,9(11),16 -pregnatriene-3-ones.
    Type: Grant
    Filed: September 6, 1996
    Date of Patent: May 26, 1998
    Assignee: Roussel Uclaf
    Inventors: Francis Brion, Jean Buendia, Christian Diolez, Michel Vivat
  • Patent number: 5594127
    Abstract: A compound having a formula ##STR1## in which K is defined as above, C--P being CH.sub.2 or --C.dbd.CH.sub.2 or ##STR2## and J is --SO.sub.2 R.sub.2, or C--P is C.dbd.O and J is --CH.sub.2 Hal.sub.2, or C--P is --CH SO.sub.2 R.sub.2 and J is CO.sub.2 R or Hal.sub.1, R.sub.2 is methyl, phenyl, tolyl or xylyl, R is alkyl of 1 to 6 carbon atoms, aralkyl of 7 to 15 is carbon atoms or a silylated remainder selected from the group consisting of trimethylsilyl, tert.-butyldimethylsilyl, triphenylsilyl and diphenyltert.-butylsilyl, Hal.sub.1 is halogen, Hal.sub.2 is chlorine, bromine or iodine and the wavy lines symbolize any one of the isomer forms or their mixtures which are intermediates.
    Type: Grant
    Filed: November 14, 1995
    Date of Patent: January 14, 1997
    Assignee: Roussel Uclaf
    Inventors: Francis Brion, Jean Buendia, Christian Diolez, Michel Vivat
  • Patent number: 5401864
    Abstract: A process for the preparation of a compound of the formula ##STR1## wherein R.sub.1 is acyl of 1 to 8 carbon atoms, by reducing an intermediary to form an alcohol, oxidizing the alcohol to form an aidehyde, which is subjected to the action of an acyloxylation agent.
    Type: Grant
    Filed: October 29, 1993
    Date of Patent: March 28, 1995
    Assignee: Roussel-Uclaf
    Inventors: Francis Brion, Jean Buendia, Christian Diolez, Michel Vivat
  • Patent number: 5187273
    Abstract: A compound of the formula ##STR1## wherein Hal is chlorine or bromine, R is selected from the group consisting of alkyl of 1 to 6 carbon atoms, aralkyl of 7 to 15 carbon atoms and a silylated group, K is a protective group selected from the group consisting of ##STR2## n is 2 or 3 and the wavy lines mean the groups may have either isomer form or are mixtures thereof which are intermediates for .DELTA..sup.4,9(11),16 -pregnatriene-3-ones.
    Type: Grant
    Filed: May 18, 1992
    Date of Patent: February 16, 1993
    Assignee: Roussel Uclaf
    Inventors: Francis Brion, Jean Buendia, Christian Diolez, Michel Vivat
  • Patent number: 4945064
    Abstract: Estrane and androstane derivatives of formula I ##STR1## wherein X is bromine, iodine, triphenyltin or trialkyltin of 1 to 6 carbon atoms per alkyl radical,Y represents two hydrogen atoms or methylene,Z represents two hydrogen atoms, oxo or alkylenedioxy of 2 to 6 carbon atoms andV is ethylene, vinylene, 1,3-propylene or cyclopropylene,R.sub.1 is hydrogen or a hydrocarbon radical of up to 8 hydrocarbon atoms, optionally interrupted by an oxa group or substituted by an oxo group,R.sub.2 is methyl or ethyl,R.sub.3 and R.sub.4 represent a carbon-carbon bond or R.sub.3 is hydrogen and R.sub.4 is hydrogen or methyl,.DELTA.symbolizes a 4(5)-double bond if Z signifies two hydrogen atoms or an oxo group; or a 5(6)-double bond or, for the estrane derivatives of formula I, also a 5(10)-double bond, if Z is alkylenedioxy,are pharmacologically effective substances or intermediates for preparation thereof.
    Type: Grant
    Filed: January 19, 1988
    Date of Patent: July 31, 1990
    Assignee: Schering Aktiengesellschaft
    Inventors: Helmut Hofmeister, Henry Laurent, Paul E. Schulze, Klaus Annen, Rudolf Wiechert, Kunhard Pollow, Bernhard Manz, Hans-Joerg Grill
  • Patent number: 4661295
    Abstract: Novel radioactive estradienes labelled with tritium of the formula ##STR1## wherein .sup.3 H is tritium and R is selected from the group consisting of hydrogen, alkyl of 1 to 6 carbon atoms and acyl of an organic carboxylic acid of 1 to 10 carbon atoms and the study and radioimmunological determination of non-radioactive 11.beta.-(4-dimethylaminophenyl)-17.alpha.-(prop-1-ynyl)-.DELTA..sup.4,9 -estradiene-17.beta.-ol-3-one and its metabolites in biological fluids and novel intermediates.
    Type: Grant
    Filed: June 14, 1984
    Date of Patent: April 28, 1987
    Assignee: Roussel Uclaf
    Inventors: Alain Jouquey, Jean-Noel Veltz, Jean Salmon, Michel Mouren
  • Patent number: 4609651
    Abstract: 11.beta.-Arylestradienes of general Formula I are disclosed ##STR1## wherein R.sup.2 is a hydrogen atom, a methyl group, or an ethyl group,R.sup.3 is a hydrogen atom or an acyl group,R.sup.1 and A-B have various meanings,which possess antigestagen and antimineralocorticoid activity.
    Type: Grant
    Filed: December 21, 1984
    Date of Patent: September 2, 1986
    Assignee: Schering Aktiengesellschaft
    Inventors: Ralph Rohde, Klaus Annen, Gunter Neef, Rudolf Wiechert, Sybille Beier, Walter Elger, David Henderson