Unsaturation Between The 5- And 10-positions Patents (Class 552/644)
  • 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
  • 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: 7361645
    Abstract: The invention relates to 11?-halogen steroids with general formula (I), whereby R11 is halogen, X—Y-Z represents a group with one of the two structures CH?C—C or CH2—C?C and the other radicals have the meaning that is indicated in the claims, also the production and use of these compounds for the production of pharmaceutical agents as well as pharmaceutical preparations that contain 11?-halogen steroids.
    Type: Grant
    Filed: January 24, 2002
    Date of Patent: April 22, 2008
    Assignee: Bayer Schering Pharma AG
    Inventors: Rolf Bohlmann, Hermann Kuenzer, Reinhard Nubbemeyer, Dieter Zopf
  • 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: 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: 6649779
    Abstract: This invention provides a pharmaceutically acceptable salt of 3&bgr;-hydroxy-5(10)-estrene-17-one 3-sulfate ester and a pharmaceutically acceptable salt of 3&agr;-hydroxy-5(10)-estrene-17-one 3-sulfate ester, which are useful as an estrogens.
    Type: Grant
    Filed: June 5, 2002
    Date of Patent: November 18, 2003
    Assignee: Wyeth
    Inventors: Michael Z. Kagan, Fangming Kong, Leonard A. McDonald, Panolil Raveendranath, Syed M. Shah, Joseph Zeldis
  • Patent number: 6458778
    Abstract: This invention provides estra-5(10),7-dien-3&bgr;-ol-17-one or a pharmaceutically acceptable salt of its 3-sulfate ester, estra-5(10),7-dien-3&bgr;-ol-17-one 3-glucuronide or a pharmaceutically acceptable salt thereof, estra-5(10),7-dien-3&agr;-ol-17-one or a pharmaceutically acceptable salt of its 3-sulfate ester, estra-5(10),7-dien-3&bgr;-ol-17-one 3-glucuronide or a pharmaceutically acceptable salt thereof, estra-5(10),7-dien-3&bgr;-ol-17-one 3-alkali metal salt, and estra-5(10),7-dien-3&agr;-ol-17-one 3-alkali metal salt which are useful as estrogenic agents.
    Type: Grant
    Filed: March 27, 1998
    Date of Patent: October 1, 2002
    Assignee: Wyeth
    Inventors: Fangming Kong, Leonard A. McDonald, Michael Z. Kagan, Syed M. Shah, Panolil Raveendranath, Mark A. Collins
  • Patent number: 5994568
    Abstract: The invention relates to estrene steroids, which bind to neuroepithelial receptors. The steroid is preferably administered in the form of a pharmaceutical composition containing one or more pharmaceutically acceptable carriers.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: November 30, 1999
    Assignee: Pherin Corporation
    Inventors: David L. Berliner, Nathan W. Adams, Clive L. Jennings-White
  • Patent number: 4923640
    Abstract: A process for the production of 17.alpha.-ethinyl-17.beta.-hydroxy-18-methyl-4,15-estradien-3-one is described comprising reacting a 17-enolester of formula II ##STR1## wherein R.sub.1 represents an alkyl radical with 1-3 carbon atoms andR.sub.2 represents an acyl or a trialkylsilyl group with 1-10 carbon atomsunder palladium catalysis, with compounds of formula II ##STR2## wherein R.sub.1 represents an alkyl radical with 1-3 carbon atoms, reducing the 17-keto group to the 17-hydroxy group in a manner known in the art, reducing the aromatic A-ring according to Birch, with liquid ammonia, to 3-methoxy-2,5(10),15-estratrien-17.beta.-ol, reoxidizing the 17-hydroxy group to the 17-keto group, ethinylating the 17-keto group and splitting off the 3-enolether to form 17.alpha.-ethinyl-17.beta.-hydroxy-18-methyl-4,15-estradiene-3-one.
    Type: Grant
    Filed: March 31, 1988
    Date of Patent: May 8, 1990
    Assignee: Schering Aktiengesellschaft
    Inventors: Rolf Bohlmann, Henry Laurent, Helmut Hofmeister, Rudolf Wiechert
  • Patent number: 4921845
    Abstract: The invention relates to new 11-arylsteroid compounds, having a strong antiprogestin and a weak or nonexistent antiglucocorticoid activity, to processes for preparing said compounds and also to pharmaceutical preparations which contain these derivatives as active constituent, characterized in that said steroids have the following formula: ##STR1## in which R.sub.1 is an aryl group with a ##STR2## group as substituent, X and Y each being separately H or a (1-4 C) hydrocarbyl group or together a (2-C) hydrocarbyl group which forms a 3- to 7-membered ring together with the nitrogen atom;R.sub.2 is hydrogen, hydroxyl, an acyloxy or an alkoxy group or a saturated or unsaturated hydrocarbyl group containing 1-8 carbon atoms, which hydrocarbyl group is provided with at least one hydroxyl, oxo, azido, cyano and/or halogen group;R.sub.3 is a hydroxyl, an acyloxy or an alkoxy group or an acyl group optionally substituted by a hydroxyl, alkoxy, acyloxy or halogen group; or R.sub.2 and R.sub.
    Type: Grant
    Filed: December 8, 1988
    Date of Patent: May 1, 1990
    Assignee: Akzo N.V.
    Inventors: Hendrick Paul de Jongh, Nicolaas P. van Vliet