The Hetero Ring And Acyclic Chalcogen Are Both Bonded Directly At The 17 Position Of The Cyclopentanohydrophenanthrene Ring System Patents (Class 540/101)
  • Patent number: 9562067
    Abstract: The present invention relates to a new stereoselective process for the synthesis of 17(?)-17-acetyl-17-hydroxy-estr-4-en-3-one of formula (I), as well as to the new intermediates of the process. The 17(?)-17-acetyl-17-hydroxy-estr-4-en-3-one (gestonorone) is an important intermediate in the synthesis of the active ingredients having progestogen activity—such as gestonorone capronate and nomegestroi acetate. Formulas (I), (II) and (III).
    Type: Grant
    Filed: December 15, 2014
    Date of Patent: February 7, 2017
    Assignee: RICHTER GEDEON NYRT.
    Inventors: János Csörgei, Anita Horváth, Csaba Sánta, Sándor Mahó, Zoltán Béni, János Horváth
  • Patent number: 6262042
    Abstract: The invention is directed to a novel class of steroids which exhibit potent antiprogestational activity.
    Type: Grant
    Filed: May 29, 1998
    Date of Patent: July 17, 2001
    Assignee: Research Triangle Institute
    Inventors: C. Edgar Cook, John A. Kepler, Gary S. Bartley
  • Patent number: 5792859
    Abstract: Novel intermediate compounds of formula IV, V, VI, VII and VIII which are useful for the preparation of steroids of the formula ##STR1## wherein the substituents are defined in the specification.
    Type: Grant
    Filed: December 2, 1996
    Date of Patent: August 11, 1998
    Assignee: Roussel Uclaf
    Inventors: Robert Lett, Oleg Melnyk
  • Patent number: 5723638
    Abstract: The invention is drawn to a process for the preparation of a steroid of the formula ##STR1## wherein R.sub.1 is hydrogen or alkyl of 1 to 4 carbon atoms, R.sub.2 is alkyl of 1 to 4 carbon atoms and theo A, B, C, and D ring system has at least one double bond and is optionally substituted by at least one optionally protected hydroxy, optionally protected keto, halogen, alkyl and alkoxy of 1 to 4 carbon atoms, and alkenyl and alkynyl of 2 to 4 carbon atoms by reacting the corresponding 17-ketosteroid with a compound of the formula ##STR2## and then by reacting the resulting compound with an aryl sulfenyl halide. The intermediate produced then undergoes rearrangement followed by epimerization with a strong base to obtain a mixture of the corresponding sulfoxide diastereoisomers which is reacted with a thiophilic compound. The intermediate produced undergoes acid hydrolysis to provide the compound of formula I.
    Type: Grant
    Filed: June 26, 1995
    Date of Patent: March 3, 1998
    Assignee: Roussel Uclaf
    Inventors: Robert Lett, Oleg Melnyk
  • Patent number: 5721227
    Abstract: 17-Aryl -5.alpha.,14.beta.-androstane, androstene and androstadiene derivatives of formula (I): ##STR1## wherein the symbol --- represents a single or a double bond; when the double bond is not present in the 4 or 5 position, the hydrogen in position 5 has the .alpha. configuration;Y is oxygen or guanidinoimino, when --- in position 3 is a double bond;Y is hydroxy, OR.sup.2 or SR.sup.2, when in position 3 is a single bond and has an .alpha. or .beta. configuration;R is a substituted or unsubstituted aryl ring; andR.sup.1 is hydrogen, methyl, ethyl or n-propyl substituted by OH or NR.sup.4 R.sup.5.
    Type: Grant
    Filed: November 3, 1995
    Date of Patent: February 24, 1998
    Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.
    Inventors: Piero Melloni, Luigi Bernardi, Mara Ferrandi, Marco Frigerio, Marina Mauro, Luisa Quadri
  • Patent number: 5108996
    Abstract: A compound selected from the group consisting of a compound of the formula ##STR1## wherein R.sub.2 and R'.sub.2 are individually hydrogen or methyl, R.sub.11 is an organo of 1 to 18 carbon atoms optionally containing at least one heteroatom with the atom adjacent to the 11-carbon atom being a carbon, the wavy lines at the 13 and 17-positions indicate that when the 13-methyl is .alpha., R'.sub.17 group is .beta. and R.sub.17 is .alpha. and when the 13-methyl is .sub..beta., R.sub.17 is .sub..beta. and R'.sub.17 is .alpha., R.sub.17 is --OH or acyloxy of 1 to 18 carbon atoms and R'.sub.
    Type: Grant
    Filed: March 21, 1990
    Date of Patent: April 28, 1992
    Assignee: Roussel Uclaf
    Inventors: Andre Claussner, Jacques Leclaire, Lucien Nedelec, Daniel Philibert
  • Patent number: 4612316
    Abstract: Compounds of the formula ##STR1## wherein C.sup.1 and N.sup.4 are in trans configuration to each other, wherein R and Y are defined herein below, as bases and pharmaceutically acceptable acid addition salts thereof, processes for their preparation and pharmaceutical preparations and methods of treatment employing such compounds. The compounds are useful for treatment of disorders in the central nervous system.
    Type: Grant
    Filed: April 19, 1984
    Date of Patent: September 16, 1986
    Assignee: Astra Lakemedel Aktiebolag
    Inventors: Bengt R. Andersson, Folke L. Arvidsson, Per A. E. Carlsson, John S. M. Hjort, Anette M. Johansson, Per L. Lindberg, John L. G. Nilsson, Domingo Sanchez, Kjell A. I. Svensson, Hakan V. Wikstrom