Halogen Bonded Directly At The 16-position Of The Cyclopentanohydrophenanthrene Ring System Patents (Class 552/536)
  • 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: 8569275
    Abstract: The invention relates to the use of compounds to ameliorate or treat an condition such as a cystic fibrosis, neutropenia or other exemplified conditions. Exemplary compounds that can be used include 3?-hydroxy-17?-aminoandrost-5-ene, 3?-hydroxy-16?-fluoro-17?-aminoandrost-5-ene, 3?-hydroxy-16?-fluoro-17?-aminoandrost-5-ene, 3?-hydroxy-16?-fluoro-17?-aminoandrost-5-ene, 1?,3?-dihydroxy-4?-fluoroandrost-5-ene-17-one, 1?,3?,17?-trihydroxy-4?-fluoroandrost-5-ene, 1?,3?-dihydroxy-6?-bromoandrost-5-ene, 1?-fluoro-3?,12?-dihydroxyandrost-5-ene-17-one, 1?-fluoro-3?,4?-dihydroxyandrost-5-ene and 4?-fluoro-3?,6?,17?-trihydroxyandrostane.
    Type: Grant
    Filed: April 27, 2011
    Date of Patent: October 29, 2013
    Assignee: Harbor Therapeutics, Inc.
    Inventor: James M. Frincke
  • Patent number: 8354396
    Abstract: The invention relates to methods to identify compounds that can treat autoimmune conditions and treat specified clinical disorders such as multiple sclerosis, ulcerative colitis or arthritis. Compounds include 17?-ethynylandrost-5-ene-3?,11?,7?,17?-tetrol, 4?-acetoxy-17?-ethynylandrost-5-ene-3?,7?,17?-triol, 17?-ethynylandrost-5-ene-3?,4?,7?,17?-tetrol, 17?-ethynylandrost-5-ene-3?,4?,7?,17?-tetrol and 17?-ethynylandrost-5-ene-3?,4?,17?-triol-7-one.
    Type: Grant
    Filed: November 17, 2007
    Date of Patent: January 15, 2013
    Assignee: Harbor Therapeutics, Inc.
    Inventors: James M. Frincke, Christopher Reading
  • Patent number: 8106036
    Abstract: The invention provides compositions comprising formula 1 steroids, e.g., 16?-bromo-3?-hydroxy-5?-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?-bromo-3?-hydroxy-5?-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: Grant
    Filed: December 9, 2009
    Date of Patent: January 31, 2012
    Assignee: Harbor Biosciences, Inc.
    Inventor: James M. Frincke
  • Patent number: 8022234
    Abstract: The invention provides compositions comprising formula 1 steroids, e.g., 16?-bromo-3?-hydroxy-5?-androstan-17-one hemihydrate and one or more excipients, including compositions that comprise a liquid formulation comprising less than about 3% v/v 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?-bromo-3?-hydroxy-5?-androstan-17-one and compositions useful in such dosing regimens. The invention further provides compositions and methods to inhibit pathogen replication, ameliorate symptoms associated with immune dysregulation and to modulate immune responses in a subject using the compounds. The invention also provides methods to make and use these immunomodulatory compositions and formulations.
    Type: Grant
    Filed: September 30, 2009
    Date of Patent: September 20, 2011
    Assignee: Harbor BioSciences, Inc.
    Inventor: James M. Frincke
  • Publication number: 20110137057
    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: Application
    Filed: February 18, 2011
    Publication date: June 9, 2011
    Inventor: James M. Frincke
  • Patent number: 7419972
    Abstract: The invention relates to new 2-substituted estra-1,3,5(10)-trien-17-ones of formula I as well as their pharmaceutically acceptable salts, their methods of manufacture and use as medicaments for prophylaxis and/or therapy of estrogen-dependent diseases that can be influenced by the inhibition of 17?-hydroxy steroid dehydrogenase type 1.
    Type: Grant
    Filed: June 17, 2005
    Date of Patent: September 2, 2008
    Assignee: Schering AG
    Inventors: Alexander Hillisch, Olaf Peters, Christian Gege, Wilko Regenhardt, Andrea Rosinus, Jerzy Adamski, Gabriele Moeller, Walter Elger, Birgitt Schneider, Ulrich Bothe
  • Patent number: 6737417
    Abstract: The present invention provides a compound consisting of a moiety and a group chemically bonded to said moiety, wherein said moiety contains a compound having low activity following oral administration or its parent scaffold and said group has the following general formula (1): in which R1 represents a hydrogen atom, etc., R2 represents a C1-C7 halogenoalkyl group, etc., m represents an integer of 2 to 14, and n represents an integer of 2 to 7, or enantiomers of the compound, or hydrates or pharmaceutically acceptable salts of the compound or enantiomers thereof. The above compound is advantageous in pharmaceutical use because the group of general formula (1) allows compounds such as anti-estrogenic ones to show a significantly increased activity following oral administration when attached to the parent scaffolds of the compounds.
    Type: Grant
    Filed: June 13, 2002
    Date of Patent: May 18, 2004
    Assignee: Chugai Seiyaku Kabushiki Kaisha
    Inventors: JaeChon Jo, HeeAn Kwon, HyunSuk Lim, JaeYoung Choi, Kazumi Morikawa, Yoshitake Kanbe, Masahiro Nishimoto, MyungHwa Kim, Yoshikazu Nishimura
  • Patent number: 6667299
    Abstract: The invention provides compositions comprising, 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: Grant
    Filed: March 23, 2000
    Date of Patent: December 23, 2003
    Assignee: Hollis-Eden Pharmaceuticals, Inc.
    Inventors: Clarence Nathaniel Ahlem, Luis Daniel dos Anjos de Carvalho, William Heggie
  • Publication number: 20030022874
    Abstract: A process for the preparation of a compound of the formula 1
    Type: Application
    Filed: June 18, 2002
    Publication date: January 30, 2003
    Inventors: Yasmina Bouali, Jacques Mauger, Patrick Van De Velde, Francois Nique
  • Patent number: 5994333
    Abstract: The invention relates to a method of altering hypothalamic function in an individual. The method comprises nasally administering a human vomeropherin, e.g. a pregnane or cholane steroid, or a pharmaceutical composition containing a vomeropherin, such that the vomeropherin binds to a specific neuroepithelial receptor. The steroid or steroids is/are preferably administered in the form of a pharmaceutical composition containing one or more pharmaceutically acceptable carriers. Other embodiments of the invention include pharmaceutical compositions containing the steroids.
    Type: Grant
    Filed: August 3, 1995
    Date of Patent: November 30, 1999
    Assignee: Pherin Corporation
    Inventors: Clive L. Jennings-White, David L. Berliner, Nathan William Adams
  • 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: 5808051
    Abstract: The present invention provides new process of preparing neuromuscular blocking agents. The process include preparing neuromuscular blocking agents using the compounds of formula I: ##STR1## wherein R.sub.1 is .dbd.O and X is halo; and formula II: ##STR2## wherein R.sub.1 and X are as defined above.
    Type: Grant
    Filed: October 27, 1997
    Date of Patent: September 15, 1998
    Assignee: Poli Industria Chimica, S.p.a.
    Inventors: Ambrogio Magni, Paride Grisenti
  • Patent number: 5804576
    Abstract: Steroids of the formula: ##STR1## useful as cancer preventive agents, anti-obesity agents, anti-hyperglycemic agents, anti-aging agents, and anti-hypercholesterolemic agents and anti-auto-immune agents.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: September 8, 1998
    Assignee: Research Corporation Technologies, Inc.
    Inventors: Arthur G. Schwartz, John R. Williams, Magid Abou-Gharbia, Ann R. Swern, Marvin Louis Lewbart
  • Patent number: 5714481
    Abstract: Steroids of the formula: ##STR1## useful as cancer preventive agents, anti-obesity agents, anti-hyperglycemic agents, anti-aging agents, and anti-hypercholesterolemic agents and anti-auto-immune agents.
    Type: Grant
    Filed: May 31, 1995
    Date of Patent: February 3, 1998
    Assignee: Research Corporation Technologies, Inc.
    Inventors: Arthur G. Schwartz, John R. Williams, Magid Abou-Gharbia, Daniel Swern, deceased, Marvin Louis Lewbart
  • Patent number: 5700793
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: December 23, 1997
    Assignee: Research Corporation Technologies, Inc.
    Inventors: Arthur G. Schwartz, Marvin Louis Lewbart
  • Patent number: 5364847
    Abstract: Certain steroidal and non-steroidal compounds have been found to inhibit androgen and estrogen formation. Such inhibition may aid in the reduction of the activity of these hormones and may be useful in the treatment of diseases where, for example, inhibition of androgen or estrogen acitivity is desired. Preferred inhibitors also possess antiestrogenic activity, thus providing the advantage of a double inhibitory action both on estrogen formation and on estrogen action.
    Type: Grant
    Filed: October 22, 1992
    Date of Patent: November 15, 1994
    Assignee: Endorecherche
    Inventors: Fernand Labrie, Yves Merand
  • Patent number: 5204337
    Abstract: Novel compounds for the inhibition of sex steroid activity for the treatment of both androgen-related and estrogen-related diseases include for example 15- and 16-halo substituted compounds such as: ##STR1## The compounds are characterized by an estrogenic nucleus substituted with a substituent of the formula --R.sup.1 [B--R.sup.2 --].sub.x L--G whereinat least one of L and G is a polar moiety distanced from a ring carbon of the estrogenic nucleus by a least three intervening atoms:x is an integer from 0-6;R.sup.1 and R.sup.2 are independently either absent or selected from the group consisting of straight- or branched-chain alkylene, straight- or branched-chain alkynylene, straight- or branched-chain alkenylene, phenylene, and fluoro-substituted analogs of the foregoing; andB is either absent or selected from the group consisting of --O--, --Se--, --SO--, --SO.sub.2 --, --NR.sup.3 --, --SiR.sup.3.sub.2, --CR.sup.3 OR.sup.3 --, NR.sup.3 CO--, NR.sup.3 CS--, --CONR.sup.3 --, CSNR.sup.
    Type: Grant
    Filed: July 21, 1992
    Date of Patent: April 20, 1993
    Assignee: Endorecherche Inc.
    Inventors: Fernand Labrie, Yves Merand
  • Patent number: 5157031
    Type: Grant
    Filed: March 21, 1989
    Date of Patent: October 20, 1992
    Assignee: Research Corporation Technologies, Inc.
    Inventors: Arthur G. Schwartz, Marvin L. Lewbart