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 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.
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.
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.
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.
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 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
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
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
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
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: 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
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.
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
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
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.
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.