Carbon Chain Having Carbon-to-carbon Unsaturation Bonded Directly At The 17 Position Of The Cyclopentanohydrophenanthrene Ring System Patents (Class 540/40)
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
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
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
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
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
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
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