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.
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.
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.
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
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
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
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
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
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
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
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
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
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
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
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
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.
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.
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