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 instant invention provides potent antiandrogen compounds, such as 3?-acetoxyandrost-1,5-diene-17-ethylene ketal and 3?-hydroxyandrost-1,5-diene-17-ethylene ketal, and methods for their use in the prevention and treatment of biological conditions mediated by androgen receptors. Thus, for example, compounds of the invention are useful in the prevention and treatment of prostrate cancer. Furthermore, it has been discovered that compounds of the invention are useful in the prevention and treatment of androgen-independent cancers such as androgen-independent prostrate cancer. Finally, inventive compounds may be used to treat antiandrogen induced withdrawal syndrome.
Type:
Application
Filed:
October 15, 2010
Publication date:
February 3, 2011
Inventors:
Henry A. Lardy, Ashok Marwah, Padma Marwah
Abstract: The instant invention provides potent antiandrogen compounds, such as 3?-acetoxyandrost-1,5-diene-17-ethylene ketal and 3?-hydroxyandrost-1,5-diene-17-ethylene ketal, and methods for their use in the prevention and treatment of biological conditions mediated by androgen receptors. Thus, for example, compounds of the invention are useful in the prevention and treatment of prostrate cancer. Furthermore, it has been discovered that compounds of the invention are useful in the prevention and treatment of androgen-independent cancers such as androgen-independent prostrate cancer. Finally, inventive compounds may be used to treat antiandrogen induced withdrawal syndrome.
Type:
Grant
Filed:
March 17, 2009
Date of Patent:
December 29, 2009
Assignee:
Hollis-Eden Pharmaceuticals, Inc.
Inventors:
Henry A. Lardy, Padma Marwah, Ashok Marwah
Abstract: The invention relates to new C-19-halogen-substituted steroids of the androst-9(11)-ene series, namely 17&bgr;-hydroxy-19-halogen-androsta-4,9(11)-dien-3-ones of general formula (I) and process for their production. In addition, the use of new radiohalogen-labeled compounds of Formula (I) as radiopharmeceutical agents is the subject of the invention as well as the use of non-labeled compounds of Formula (I) as starting products for the production of new biologically active 5&bgr;-substituted androst-9(11)-enes of general formula (II) and the new 6&bgr;,19-cycloandrostadienes of Formula (III) as well as processes for their production and their use.
Type:
Grant
Filed:
July 2, 2002
Date of Patent:
September 14, 2004
Assignee:
Schering AG
Inventors:
Gunter Neef, Roland Golde, Karl-Heinrich Fritzemeier
Abstract: A compound is provided for increasing the concentration of a parent androgen in a subject in vivo. The parent androgen has a skeletal structure including a 1 position and a 17 position, a 17&bgr;-hydroxy group comprising a 17&bgr;-hydroxy oxygen appended to the 17 position, and a 17&bgr;-hydroxy hydrogen appended to the 17&bgr;-hydroxy oxygen. The compound includes a substrate having the skeletal structure of the parent androgen. It includes a 1 position and a 17 position corresponding to the 1 and 17 positions respectively of the parent androgen. The substrate has a carbon—carbon double bond at the 1 position. The compound also has a promoiety appended to the 17&bgr;-hydroxy oxygen of the substrate as a substitute for the 17&bgr;-hydroxy hydrogen of the parent androgen. The promoiety includes, and preferably consists of, an alkylcarbonate ester. A related method also is provided.
Abstract: The invention provides compositions comprising formula 1 steroids, e.g., 16&agr;-bromo-3&bgr;-hydroxy-5&agr;-androstan-17-one hemihydrate and one or more excipients, typically wherein the composition comprises less than about 3% water. The compositions are useful to make improved pharmaceutical formulations. The invention also provides methods of intermittent dosing of steroid compounds such as analogs of 16&agr;-bromo-3&bgr;-hydroxy-5&agr;-androstan-17-one and compositions useful in such dosing regimens. The invention further provides compositions and methods to inhibit pathogen (viral) replication, ameliorate symptoms associated with immune dysregulation and to modulate immune responses in a subject using certain steroids and steroid analogs. The invention also provides methods to make and use these immunomodulatory compositions and formulations.
Type:
Application
Filed:
December 13, 2002
Publication date:
March 4, 2004
Inventors:
Clarence N. Ahlem, William Heggie, Luis D. Carvalho
Abstract: A method is described for stereoselectively reducing an unsaturated alkyl ketone substituent attached to a fused ring base. In this method, the unsaturated alkyl ketone reacts with a chiral oxazaborolidine reagent. This reaction stereoselectively reduces the unsaturated alkyl ketone to an unsaturated alkyl alcohol. The unsaturated alkyl alcohol can be further reduced, if desired, to produce a saturated alkyl alcohol. The fused ring base can be, for example, a steroid ring base or a base of a vitamin D analog. The process in accordance with the invention can be used with an alkeneone substituent (e.g., a 22-ene-24-one substituent) or an alkyneone substituent (e.g., a 22-yne-24-one substituent) on a steroid ring base to make squalamine or other useful aminosterol compounds and intermediates for making aminosterol compounds.
Type:
Grant
Filed:
April 12, 2001
Date of Patent:
August 26, 2003
Assignee:
Magainin Pharmaceuticals, Inc.
Inventors:
William A. Kinney, Steven Jones, Xuehai Zhang, Meena N. Rao, Michel Bulliard, Harold Meckler, Nancy Lee
Abstract: The subject of the invention is the products of formula (I):
in which either R1 represents halogen, hydroxyl, (C1-C8) alkyloxy or (C1-C12) acyloxy, and R2 represents halogen or hydrogen, or R1 and R2 form together a double bond, Z is chosen from optionally substituted (C1-C8) alkylthio, optionally substituted arylthio, (C1-C8) alkyloxy, halogen, cyano, mercapto, thiocyanato and (CH2)0-1—CO2H, optionally esterified, Y represents hydrogen or methyl, the dotted line in position 1-2 or 5-6 optionally representing a second bond, as well as their addition salts, their preparation process, the intermediates of this process and the pharmaceutical compositions containing them.
Type:
Grant
Filed:
June 25, 2001
Date of Patent:
December 10, 2002
Assignee:
Aventis Pharma S.A.
Inventors:
Neerja Bhatnagar, Andre Claussner, Christian Marchandeau, Michele Resche Rigon, Jean-Georges Teutsch
Abstract: The invention relates to 17&bgr;-aryl(arylmethyl)oxy(thio)alkyl-androstane derivatives having general formula (I), wherein R1 is (H,OR), (H,OSO3H) or NOR; with R being H, (C1-6)alkyl or (C1-6)acyl; each of R2 and R3 is independently hydrogen or (C1-6)alyl; n is 0, 1, or 2; X is O, S, S(O) or S(O)2; m is 0 or 1; each of R4, R5 and R6 is independently hydrogen, hydroxy, (C1-4)alkoxy, halogen, NR7R8 or (C1-4)alkyl, optionally substituted by hydroxy, alkoxy, halogen or oxo; each of R7 and R8 is independently hydrogen or (C1-4)alkyl, and wherein the dotted lines indicate a &Dgr;7 or a &Dgr;8 double bond, or a pair of conjugated double bonds selected from &Dgr;7,14, &Dgr;8,14 and &Dgr;6,8(14); or a pharmaceutically acceptable salt thereof. The compounds of the invention have meiosis regulating activity and can be used for the control of fertility.
Abstract: The invention relates to novel, androstane steroids which are the ligand semiochemicals which bind to neuroepithelial receptors. The steroids are useful as ligands to neuroepithelial receptors in the human vomeronasal gland to stimulate autonomic and hypothalamic activity.
Type:
Grant
Filed:
September 29, 1994
Date of Patent:
October 19, 1999
Assignee:
Pherin Corporation
Inventors:
David L. Berliner, Nathan W. Adams, Clive L. Jennings-White
Abstract: 6-hydroxy and 6-oxo-androstane derivatives of formula (I), active on the cardiovascular system. ##STR1## wherein: the symbol A represents CH--OR, C.dbd.N--OR, CH--CH.dbd.N--OR and C.dbd.CH--N--OR; and R.sup.1, R.sup.2 and R.sup.3 are as defined herein.
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: A process and appropriate device are disclosed for determining the androstenone content of adipose tissues in clearly shorter times. The disclosed process has the following steps: (a) liquefying an adipose tissue sample by heating up to a predetermined temperature in the 45.degree. to 60.degree. C.
Abstract: Cardioactive steroidal compounds of the formula I ##STR1## wherein R, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6 and R.sub.7 have the meanings shown in the description, and pharmaceutical compositions containing them.
Type:
Grant
Filed:
January 15, 1993
Date of Patent:
June 13, 1995
Inventors:
Giorgio Bertolini, Cesare Casagrande, Gabriele Norcini, Francesco Santangelo
Abstract: Invented are substituted acrylate analogues of steroidal synthetic compounds, pharmaceutical compositions containing the compounds, and methods of using these compounds to inhibit steroid 5.alpha.-reductase. Also invented are intermediates used in preparing these compounds.
Type:
Grant
Filed:
December 23, 1988
Date of Patent:
August 7, 1990
Assignee:
SmithKline Beecham Corporation
Inventors:
Dennis A. Holt, Mark A. Levy, Brian W. Metcalf