And Carbon Bonded Directly At The 17 Beta-position Is A Member Of An Acyclic Chain Of Two Or More Uninterrupted Carbons Patents (Class 552/529)
  • Publication number: 20150005518
    Abstract: A process ethynylates 16-methylene-17-keto steroids to the corresponding 16-methylene-17?-ethynyl-17?-hydroxy steroids by treatment with silyl-protected lithium acetylides followed by further desilylation. The resulting products are useful intermediates in the preparation of several pharmaceutically active agents, such as e.g. Nestorone® or melengestrol acetate.
    Type: Application
    Filed: December 19, 2012
    Publication date: January 1, 2015
    Applicants: CRYSTAL PHARMA, S.A.U., THE POPULATION COUNCIL INC.
    Inventors: Luis Gerardo Gutiérrez Fuentes, Celso Miguel Sandoval Rodríguez
  • Publication number: 20110098260
    Abstract: The invention provides methods to treating conditions such as prostate cancer, or for ameliorating one or more symptoms associated with prostate cancer, or for agents that modulate the biological activity of the androgen receptor. The invention also provides methods and compositions suitable for therapeutic applications.
    Type: Application
    Filed: December 1, 2010
    Publication date: April 28, 2011
    Applicant: Harbor BioSciences, Inc.
    Inventor: James M. Frincke
  • Publication number: 20090258847
    Abstract: 4-(3-hydroxy-10,13-dimethyl-hexadecahydro-cyclopenta[a]phenanthren-17-yl)-pentanoic acid amides wherein the nitrogen of the amide group is substituted by a sulfonylaminocarbonyl-(C1-4)-alkyl group; and the use of such compounds as pharmaceuticals.
    Type: Application
    Filed: July 16, 2007
    Publication date: October 15, 2009
    Inventors: Erwin Paul Schreiner, Klemens Hogenauer
  • Patent number: 5986115
    Abstract: This invention describes new, substituted 7.alpha.-(.xi.-aminoalkyl)-estratrienes of general formula I ##STR1## in which side chain SK is a radical of partial formula ##STR2## as well as their physiologically compatible addition salts with organic and inorganic acids.The new compounds represent compounds with very strong antiestrogenic action.The compounds according to the invention are, on the one hand, pure antiestrogens, or, on the other hand, antiestrogens with estrogenic partial action. Based on this spectrum of action, the new compounds are highly suitable for the production of pharmaceutical agents for tumor therapy and hormone replacement treatment.
    Type: Grant
    Filed: January 28, 1999
    Date of Patent: November 16, 1999
    Assignee: Schering AG
    Inventors: Rolf Bohlmann, Dieter Bittler, Josef Heindl, Nikolaus Heinrich, Helmut Hofmeister, Hermann Kunzer, Gerhard Sauer, Christa Hegele-Hartung, Rosemarie Lichtner, Yukishige Nishino, Karsten Parczyk, Martin Schneider
  • Patent number: 5866560
    Abstract: This invention describes new, substituted 7.alpha.-(.xi.-aminoalkyl)-estratrienes of general formula I ##STR1## in which side chain SK is a radical of partial formula ##STR2## as well as their physiologically compatible addition salts with organic and inorganic acids.The new compounds represent compounds with very strong antiestrogenic action.The compounds according to the invention are, on the one hand, pure antiestrogens, or, on the other hand, antiestrogens with estrogenic partial action. Based on this spectrum of action, the new compounds are highly suitable for the production of pharmaceutical agents for tumor therapy and hormone replacement treatment.
    Type: Grant
    Filed: August 20, 1997
    Date of Patent: February 2, 1999
    Assignee: Schering AG
    Inventors: Rolf Bohlmann, Dieter Bittler, Josef Heindl, Nikolaus Heinrich, Helmut Hofmeister, Hermann Kunzer, Gerhard Sauer, Christa Hegele-Hartung, Rosemarie Lichtner, Yukishige Nishino, Karsten Parczyk, Martin Schneider
  • Patent number: 5480913
    Abstract: Disclosed are novel classes of anti-androgens including dihydrophenanthrene derivatives, their method of synthesis and their use in treating disorders associated with excessive androgenic activities.
    Type: Grant
    Filed: May 3, 1993
    Date of Patent: January 2, 1996
    Assignee: Arch Development Corporation
    Inventors: Shutsung Liao, John Pataki, Ronald G. Harvey
  • Patent number: 5252564
    Abstract: A method for decreasing the adrenal secretion of glucocorticoids, especially cortisol, in male livestock without substantially suppressing the animal's immune system by oral or other administration of effective doses of melengesterol acetate (MGA) or derivatives thereof. Ideally, the MGA may be used in admixture with the subject animal feed, although it is understood that the compound may be administered separately.
    Type: Grant
    Filed: March 29, 1991
    Date of Patent: October 12, 1993
    Assignee: The United States of America as represented by the Secretary of Agriculture
    Inventor: Michael T. Zavy
  • Patent number: 4954490
    Abstract: A 11.beta.-aryl-19-norprogesterone steroid of the formula: ##STR1## wherein (i) R.sup.1 is H, C.sub.1-4 alkyl, C.sub.2-4 alkenyl, C.sub.2-4 alkynyl, OH, OC(O)CH.sub.3, or OC(O)R.sup.5, wherein R.sup.5 is C.sub.2-8 alkyl, C.sub.2-8 alkenyl, C.sub.2-8 alkynyl or aryl, R.sub.2 is H, R.sup.3 is H, C.sub.1-4 alkyl, C.sub.2-4 alkenyl or C.sub.2-4 alkynyl, R.sup.4 is H, CH.sub.3, F or Cl, R.sup.6 is H, (CH.sub.3).sub.2 N, CH.sub.3 O, CH.sub.3 CO, CH.sub.3 S, CH.sub.3 SO, CH.sub.3 SO.sub.2, and X is O or NOCH.sub.3 ; or(ii) R.sup.1 and R.sup.2 taken together are a carbon-carbon bond and R.sup.3, R.sup.4, R.sup.6 and X are as defined above; or(iii) R.sup.1 and R.sup.3 taken together are --CH.sub.2 -- or --N.dbd.N--CH.sub.2 --, R.sup.2 is H and R.sup.4, R.sup.6 and X are as defined above; or(iv) R.sup.2 and R.sup.3 taken together are .dbd.CH.sub.2 and R.sup.1, R.sup.4, R.sup.6 and X are as defined above.
    Type: Grant
    Filed: June 23, 1988
    Date of Patent: September 4, 1990
    Assignee: Research Triangle Institute
    Inventors: C. Edgar Cook, Mansukh C. Wani, Y.-W Lee, Jerry R. Reel, Douglas Rector
  • Patent number: 4921638
    Abstract: The invention is the compound 17.beta.-cyano-9.alpha., 17.alpha.-dihydroxyandrost-4-en-3-one (I) which is particularly useful as an intermediate in the production of the 17.alpha.-halo silyl ethers (II).
    Type: Grant
    Filed: October 3, 1988
    Date of Patent: May 1, 1990
    Assignee: The Upjohn Company
    Inventors: Douglas A. Livingston, Bruce A. Pearlman, Scott Denmark, Joel E. Huber
  • Patent number: 4913852
    Abstract: Compounds obtained from the associative synthesis of sulfur-containing or sulfur-free amino acids with derivatives of .DELTA.-4-pregnene-3,20-dione or with derivatives of .DELTA.-1,4-pregnadiene-3,20-dione of the general formulas (I), (II) and (III), having glucocorticoidal and anti-inflammatory properties have been prepared and tested. Pharmaceutical compositions, medicaments containing them as well as their applications are claimed, particularly in the cutaneous and ophthalmic fields.
    Type: Grant
    Filed: February 24, 1988
    Date of Patent: April 3, 1990
    Inventors: Catherine Milioni, Constantin Efthyimiopoulos, Bernard Koch, Louis Jung, Jean Jung