Carbon Bonded Directly At The 13-position (e.g., 19-norandrostenes, Estradienes, Etc.) Patents (Class 552/642)
  • Patent number: 9012667
    Abstract: The invention relates to a process for the preparation of a compound of formula (I): wherein R1 and R2 are as defined in the description, by reaction of a compound of formula (II) with a base. Compound (I) is an intermediate useful in the preparation of gestodene.
    Type: Grant
    Filed: February 8, 2011
    Date of Patent: April 21, 2015
    Assignee: Laboratoire Theramex
    Inventors: Jean-Luc Moutou, Florent Mouton, Gilles Pellegrino, Jean-Marc Dillenschneider, Jean Lafay
  • Patent number: 8586770
    Abstract: The invention relates to methods to manipulate stem cells in vivo and in vitro to treat, e.g., a condition where cell or tissue repair is needed.
    Type: Grant
    Filed: February 18, 2011
    Date of Patent: November 19, 2013
    Assignee: Harbor Therapeutics, Inc.
    Inventor: James M. Frincke
  • Publication number: 20130137885
    Abstract: The invention relates to a process for the preparation of a compound of formula wherein R1 and R2 are as defined in the description, by reaction of a compound of formula (II) with a base. Compound (I) is an intermediate useful in the preparation of gestodene.
    Type: Application
    Filed: February 8, 2011
    Publication date: May 30, 2013
    Applicant: LABORATOIRE THERAMEX
    Inventors: Jean-Luc Moutou, Florent Mouton, Gilles Pellegrino, Jean-Marc Dillenschneider, Jean Lafay
  • Publication number: 20130023498
    Abstract: The present invention is a method for identifying agents which modulate microRNA activity. The invention involves contacting a cell harboring a microRNA and a microRNA binding sequence, which is operably linked to a nucleic acid molecule encoding a reporter protein, with a test agent and determining whether the test agent increases or decreases the expression of the reporter protein thereby identifying a microRNA modulator. Antagonists identified by this screening assay are provided, as are methods for using the same to inhibit microRNA activity and prevent or treat disease.
    Type: Application
    Filed: June 20, 2012
    Publication date: January 24, 2013
    Inventors: Qihong Huang, Alexander Deiters, Kiranmai Gumireddy
  • Patent number: 8198041
    Abstract: A method of producing ?1,4-Tibolone (C21H26O2), 10?-Hydroxy-?4-tibolone (C21H28O3). 11?,15?-Dihydroxytibolone (C21H28O4) and 11?,15?-Dihydroxy-?5-tibolone (C21H28O4) by contacting tibolone and 3?,6?-Dihydroxytibolone (C21H32O3) by contacting 3?-hydroxytibolone with Cunninghamella elegans (ATCC 10028b) is reported.
    Type: Grant
    Filed: January 27, 2011
    Date of Patent: June 12, 2012
    Inventors: Attaur Rahman, Muhammed Iqbal Choudhary, Syed Adnan Ali Shah, Shamsun Nahar Khan
  • Patent number: 8148557
    Abstract: Method of producing ?5-Tibolone (C21H28O2), 6?-Hydroxy-?4-tibolone (C21H28O3), 6?-Hydroxy-?4-tibolone (C21H28O3), 15?-Hydroxy-?4-tibolone (C21H28O3), 6?-Hydroxy-?1,4-tibolone (C21H28O3) and 6?-Methoxy-?4-tibolone (C22H30O3) contacting tibolone with Gibberella fujikuroi (ATCC 10704) is reported.
    Type: Grant
    Filed: January 27, 2011
    Date of Patent: April 3, 2012
    Inventors: Attaur Rahman, Muhammed Iqbal Choudhary, Syed Adnan Ali Shah, Shamsun Nahar Khan
  • Patent number: 7696190
    Abstract: The invention makes a 16?-substituted steroidal compound available having formula 1, wherein the dotted ring is a fully saturated, a fully aromatic or a saturated ring with a ?5-10 double bond; R1 is (C1-C3)alkyl or (C2-C3)alkenyl, and each of these groups can be substituted with one or more halogens; R2 is (C1-C4;)alkyl, (C2-C4)alkenyl or methylene, and each of these groups can be substituted with one or more halogens; R3 is methyl or ethyl; or a prodrug thereof, which compound can be used for an estrogen receptor ? selective treatment
    Type: Grant
    Filed: July 23, 2001
    Date of Patent: April 13, 2010
    Assignee: N.V. Organon
    Inventors: Jordi Mestres, Hubert Jan Jozef Loozen, Gerrit Herman Veeneman
  • Patent number: 7550451
    Abstract: The invention relates to new compounds of general formula I, their production and pharmaceutical preparations that contain these compounds. The compounds according to the invention are preferably used for female birth control and for HRT.
    Type: Grant
    Filed: August 1, 2003
    Date of Patent: June 23, 2009
    Assignee: Bayer Schering Pharma AG
    Inventors: Alexander Hillisch, Walter Elger, Gerd Schubert, Birgitt Schneider, Gudrun Reddersen
  • Patent number: 7528123
    Abstract: Disclosed is a novel class of steroid compounds based on estradiol, and carrying an 11?-substitution. Said substitution is a hydrocarbon group which may be linear or branched, provided that it comprises, as the longest chain on carbon atom no. 11 of the steroid skeleton, one single linear chain having a length of from 5 to 9 carbon atoms, wherein said chain may be saturated or unsaturated. The resulting compounds have a desirable mixed agonist/antagonist profile for estrogen receptor ? and estrogen receptor ?.
    Type: Grant
    Filed: November 18, 1999
    Date of Patent: May 5, 2009
    Assignee: N.V. Organon
    Inventors: Hubert Jan Jozef Loozen, Wilhelmus Gerardus Eduardus Joseph Schoonen
  • Patent number: 6989378
    Abstract: The invention is the novel androgen (7?,17?)-7-methyl-17-[(1-oxoundecyl)oxy]estr-4en-3one (MENT undecanoate). This compound distinguishes favourably from other testosterone derivatives in that it has a good solubility in oily media. It particularly exhibits a good dissolved potency relative to testosterone. The compound is particularly suitable for administration by means of injection.
    Type: Grant
    Filed: October 13, 2004
    Date of Patent: January 24, 2006
    Assignee: Akzo Nobel N.V.
    Inventors: Dirk Leysen, Hendrikus Adrianus Antonius Van Der Voort
  • Patent number: 6693207
    Abstract: This invention provides estrogenic agents having the formula wherein A and B are each, independently, R is SO3−X+; X+ is alkali metal, alkaline earth metal, ammonium, alkylammonium containing 1-6 carbon atoms, or dialkylammonium containing 1-6 carbon atoms in each alkyl group, or trialkylammonium containing 1-6 carbon atoms in each alkyl group; with the proviso that at least one of A or B is
    Type: Grant
    Filed: June 5, 2002
    Date of Patent: February 17, 2004
    Assignee: Wyeth
    Inventors: Michael Z. Kagan, Panolil Raveendranath, Syed M. Shah, Michael W. Winkley
  • Patent number: 6677329
    Abstract: Disclosed are novel, selective estrogens type having a steroid skeleton with a non-aromatic A-ring and a free or capped hydroxyl group at carbon atom No. 3. The estrogens satisfy general formula (I), in which R1 is H, (C1-C3)alkyl or (C2-C3)acyl; R2 is H, &agr;-(C1-C4)alkyl, &agr;-(C2-C4)alkenyl or &agr;-(C2-C4)alkynyl; R3 is H or (C1-C4)alkyl, (C2-C4)alkenyl or (C2-C4)alkynyl, each at location 15 or 16 of the steroid skeleton; R4 is H or (C1-C5)alkyl, (C2-C5)alkenyl or (C2-C5)alkynyl, each optionally substituted with halogen; preferred is ethynyl; R5 is H, (C1-C3)alkyl or (C2-C3)acyl; R6 is (C1-C5)alkyl, (C2-C5)alkenyl, (C2-C5)alkynyl or (C1-C5)alkylidene, each optionally substituted.
    Type: Grant
    Filed: May 29, 2002
    Date of Patent: January 13, 2004
    Assignee: Akzo Nobel N V.
    Inventors: Hubert Jan Jozef Loozen, Gerrit Herman Veeneman, Wilhelmus Gerardus Eduardus Joseph Schoonen
  • Patent number: 6525039
    Abstract: This invention provides 3&bgr;-hydroxy-5,7,9-estratriene-17-one and a pharmaceutically acceptable salt of its 3-sulfate ester, which is useful as an estrogen.
    Type: Grant
    Filed: April 21, 1998
    Date of Patent: February 25, 2003
    Assignee: Wyeth
    Inventors: Syed M. Shah, Panolil Raveendranath, Michael Z. Kagan
  • 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: 5723455
    Abstract: Novel antiandrogenic agents are provided. An exemplary group of compounds has the structural formula (I) ##STR1## wherein R.sup.1 through R.sup.10, a and b are as defined herein. Pharmaceutical compositions and methods for using the compounds of formula (I) to treat androgen-related clinical conditions are provided, as are methods and compositions for using the compounds as contraceptive agents.
    Type: Grant
    Filed: March 11, 1997
    Date of Patent: March 3, 1998
    Assignee: SRI International
    Inventors: Masato Tanabe, Wan-Ru Chao, Wesley K. M. Chong, David F. Crowe
  • Patent number: 5359054
    Abstract: The invention includes compounds of the following formula ##STR1## where A and B either A and B form an additional double bond and D is a hydrogen atom or B and D form an additional double bond and A is a hydrogen atom and the other variables are as defined in the specification. Also disclosed is a process of making the compounds and a process of using the compounds to make compounds of the following formula ##STR2## where the variables are defined in the specification. These compounds are useful as antigestigens.
    Type: Grant
    Filed: November 30, 1992
    Date of Patent: October 25, 1994
    Assignee: Schering Aktiengesellschaft
    Inventors: Eckhard Ottow, Gunter Neef, Arwed Cleve, Rudolf Weichert
  • Patent number: 5272140
    Abstract: The invention relates to 11-aryl steroid derivatives, having the structure ##STR1## wherein: R.sub.1, R.sub.2, R.sub.3, and R.sub.4 are as described in the specificationand to processes for their preparation and to pharmaceuticals comprising these compounds.These compounds exhibit a strong anti-progestinic activity and a weak or non-existent anti-glucocorticoid activity.
    Type: Grant
    Filed: February 27, 1990
    Date of Patent: December 21, 1993
    Assignee: Akzo N.V.
    Inventor: Hubert J. J. Loozen
  • Patent number: 5227375
    Abstract: Novel aromatase inhibitors are disclosed for use in therapeutic preparations for treatment of estrogen-dependent diseases. The compounds are specified 7.alpha.-substituted androstanedione and androstenedione derivatives which show a strong inhibitory activity towards aromatase. The invention includes synthesis and pharmaceutical compositions of said compounds.
    Type: Grant
    Filed: February 8, 1990
    Date of Patent: July 13, 1993
    Assignee: Endorecherche, Inc.
    Inventors: Fernand Labrie, Yves Merand
  • Patent number: 5166146
    Abstract: A compound of the formula ##STR1## wherein R.sub.1 is an aliphatic hydrocarbon of 1 to 8 carbon atoms, R.sub.a and R.sub.b are individually hydrogen or alkyl of 1 to 4 carbon atoms, R.sub.2 is hydrogen or optionally substituted alkyl of 1 to 12 carbon atoms, n is an integer from 1 to 6, Z is free carboxy or salified with an alkali metal, alkaline earth metal or NH.sub.4 and X is the remainder of an optionally substituted and optionally unsaturated 5 or 6-member ring and the wavy line indicates the .alpha.- or .beta.-position for R.sub.1 having anti-glucocorticoid activity.
    Type: Grant
    Filed: August 16, 1990
    Date of Patent: November 24, 1992
    Assignee: Roussel Uclaf
    Inventors: Martine Moguilewsky, Lucien Nedelec, Francois Nique, Daniel Philibert