Abstract: Substituted steroid compounds which represent selective inhibitors of 17?-hydroxysteroid dehydrogenase type I (17?-HSD1) and, in addition, which may represent inhibitors of the steroid sulfatase, salts thereof, pharmaceutical preparations containing these compounds, and a process for the preparation of these compounds. Also disclosed is a therapeutic method of using such substituted steroid compounds, particularly in the treatment, inhibition, prophylaxis or prevention of steroid hormone dependent diseases or disorders, such as steroid hormone dependent diseases or disorders requiring the inhibition of 17?-hydroxysteroid dehydrogenase type I and/or steroid sulfatase enzymes and/or requiring lowering of the endogenous 17?-estradiol concentration.
Type:
Grant
Filed:
September 28, 2010
Date of Patent:
May 7, 2013
Assignee:
Abbott Products GmbH
Inventors:
Josef Messinger, Heinrich-Hubert Thole, Bettina Husen, Michael Weske, Pasi Koskimies, Lila Pirkkala
Abstract: The invention relates to novel ligands of the estrogen receptors ? and ? of general formula II, which are useful as an active substance of pharmaceuticals, for example pharmaceutical compositions useful for hormone replacement therapy, as well as for the treatment of tumors and inflammatory diseases. The invention also relates to a novel preparation method of these ligands comprising cyclotrimerization of ethynylestradiol with the appropriate diyne in an organic solvent. Further, the invention relates to pharmaceuticals comprising the novel compounds according to the invention.
Type:
Application
Filed:
May 5, 2009
Publication date:
May 19, 2011
Inventors:
Petr Novak, David Sedlak, Petr Bartunek, Martin Kotora
Abstract: A novel process for preparing a compound of formula (I) which comprises converting a compound of formula (II) to a compound of formula (I) via a compound of formula (III), or a salt thereof, without isolating any intermediates.
Type:
Application
Filed:
June 13, 2007
Publication date:
May 7, 2009
Applicant:
GLAXO GROUP LIMITED
Inventors:
Malcolm Brian Berry, Mark Jason Hughes, David Parry-Jones, Stephen John Skittrall
Abstract: The invention concerns a bioprecursor of formula (I), wherein A1 and A2 represent independently of each other a radical derived from a molecule capable of being used in dermatology or in cosmetology; X and Y represent independently of each other a hydrogen atom, a hydroxy group or a C1-C20 alkyl group; and n represents an integer between 0 and 10.
Type:
Application
Filed:
March 16, 2004
Publication date:
November 25, 2004
Inventors:
Daniel Redoules, Pascal Bordat, Jean-Jacques Perie
Abstract: There is provided a crystalline chemical composition comprising a compound of formula (I) 1
Type:
Application
Filed:
June 8, 2004
Publication date:
November 11, 2004
Inventors:
Keith Biggadike, Steven John Coote, Andrew S. Craig, Victor Jacewicz, Michael J. Millan, Rosalyn K. Nice, Brian M. Noga, John F. Seager, Andrew L. Theophilus, David M. Crowe
Abstract: This invention describes the new 11&bgr;-halogen-7&agr;-substituted estratrienes of general formula I
in which
R11 is a fluorine or chlorine atom, and the other substituents have the meanings that are explained in more detail in the description.
The compounds have antiestrogenic properties or tissue-selective estrogenic properties and are suitable for the production of pharmaceutical agents.
Type:
Grant
Filed:
December 2, 1999
Date of Patent:
August 24, 2004
Assignee:
Schering Aktiengesellschaft
Inventors:
Rolf Bohlmann, Nikolaus Heinrich, Helmut Hofmeister, Jorg Kroll, Hermann Kunzer, Gerhard Sauer, Ludwig Zorn, Karl-Heinrich Fritzemeier, Monika Lessl, Rosemarie Lichtner, Yukishige Nishino, Karsten Parczyk, Martin Schneider
Abstract: The present invention comprises the design, synthesis and development of a new class of chemotherapeutic agents for prophylactic and therapeutic treatments in a mammal, particularly a human, believed to be at risk of suffering from a hormone-responsive disorde. In an embodiment of the invention, such treatments include therapeutic compositions comprising novel steroidal antiestrogen and antiandrogen compounds. In a preferred embodiment, such a novel compound of the present invention has an address and a message component, which are made into a single composite entity for more aggressive intervention and effective treatment of hormone-responsive disorders, thereby prolonging the disease-free interval for the patient and reducing a number of side effects.
Type:
Application
Filed:
December 4, 2002
Publication date:
January 1, 2004
Inventors:
Robert N Hanson, Carolyn Friel, Choon Young Lee
Abstract: The application discloses novel 2-alkoxyestradiol analogs which exhibit anti-proliferative properties, and methods of making and using such compounds to inhibit undesired cell proliferation and tumor growth. Additionally, methods are disclosed of treating diseases associated with undesired angiogenesis and undesired proliferation, and methods of treating infectious disease wherein the infectious agent is particularly susceptible to inhibition by agents that disrupt microtubule organization and function.
Type:
Application
Filed:
April 11, 2003
Publication date:
December 11, 2003
Applicant:
SOUTHWEST FOUNDATION FOR BIOMEDICAL RESEARCH
Inventors:
Pemmaraju Narasimha Rao, Susan L. Mooberry, James W. Cessac, Tina L. Tinley
Abstract: The compositions and methods disclosed herein provide heterobifunctional programmable genotoxic compounds that can be designed to kill selected cells present in a heterogenous cell population. The present compounds comprise a first agent that inflicts damage on cellular DNA, and a second agent that attracts a macromolecular cell component such as a protein, which in turn shields genomic lesions from repair. Unrepaired lesions therefore persist in the cellular genome and contribute to the death of selected cells. In contrast, lesions formed in nonselected cells, which lack the cell component, are unshielded and thus are repaired. As a result, compounds described herein are less toxic to nonselected cells. Compounds of this invention can be designed to cause the selective killing of transformed cells, viral-infected cells and the like.
Type:
Application
Filed:
November 18, 2002
Publication date:
November 27, 2003
Inventors:
John M. Essigmann, Robert G. Croy, Kevin J. Yarema, Marshall Morningstar
Abstract: Compounds represented by the following formula I:
in which:
R1 to R5 can have various meanings of which alkyl, substituted or non-substituted aryl, and m is equal to 0 or 1, X is selected from (CR6R7)n in which n=0 or 1, and CO are disclosed. These compounds are useful as anti-tumor drugs, especially with pro-oxidizing activity.
Type:
Grant
Filed:
August 28, 2000
Date of Patent:
June 18, 2002
Assignee:
Oxis International, Inc.
Inventors:
Jinzhu Xu, Georges Appere, Jean Chaudiere, Jean-Claude Yadan
Abstract: This invention describes new, substituted 7&agr;-(&egr;-aminoalkyl)-estratrienes of general formula I
in which
side chain SK is a radical of partial formula
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:
April 14, 2000
Date of Patent:
August 7, 2001
Assignee:
Schering Aktiengesellschaft
Inventors:
Rolf Bohlmann, Dieter Bittler, Josef Heindl, Nikolaus Heinrich, Helmut Hofmeister, Hermann Künzer, Gerhard Sauer, Christa Hegele-Hartung, Rosemarie Lichtner, Yukishige Nishino, Karsten Parczyk, Martin Schneider
Abstract: Compounds represented by the following formula I: ##STR1## in which: R.sup.1 to R.sup.5 can have various meanings of which alkyl, substituted or non-substituted aryl, and m is equal to 0 or 1, X is selected from (CR.sup.6 R.sup.7).sub.n in which n=0 or 1, and CO are disclosed. These compounds are useful as anti-tumor drugs, especially with pro-oxidizing activity.
Type:
Grant
Filed:
December 20, 1996
Date of Patent:
December 14, 1999
Assignee:
Oxis Isle of Man, Limited
Inventors:
Jinzhu Xu, Georges Appere, Jean Chaudiere, Jean-Claude Yadan
Abstract: This invention provides a method of increasing the level of estrogen receptors in the neural tissue of a subject which comprises administering to the subject estrogen in an amount effective to increase the level of neurotrophin receptors and a neurotrophin in an amount effective to increase the level of estrogen receptors, so as to thereby increase the level of estrogen receptors. This invention also provides a method of increasing the level of estrogen receptors in a sample of neural tissue from a subject which comprises contacting the sample with estrogen in an amount effective to increase the level of neurotrophin receptors and neurotrophin in an amount effective to increase the level of estrogen receptors, so as to thereby increase the level of estrogen receptors. Lastly, this invention provides a method of preventing the onset of Alzheimer's disease.
Type:
Grant
Filed:
July 12, 1996
Date of Patent:
November 23, 1999
Assignee:
The Trustees of Columbia University in the City of New York
Abstract: There are described spontaneously dispersible agents containing sterolester and/or sterolphosphor compounds having a pronounced antitumour activity. Novel sterolesters and sterolphosphor compounds, their use for treating tumors, and processes for their preparation are disclosed.
Type:
Grant
Filed:
August 13, 1992
Date of Patent:
March 5, 1996
Assignee:
Marigen S.A.
Inventors:
Carl Eugster, Conrad H. Eugster, Walter Haldemann, Giorgio Rivara
Abstract: Provided are cyclic hydrocarbons of Formula I ##STR1## with an aminoalkyl sidechain that are useful for treating phospholipase A2 mediated conditions, diabetes, and obesity.
Type:
Grant
Filed:
November 16, 1992
Date of Patent:
August 2, 1994
Assignee:
The Upjohn Company
Inventors:
Roy A. Johnson, Gordon L. Bundy, Gilbert A. Youngdale, Douglas R. Morton, Donald P. Wallach, deceased
Abstract: This invention is a compound of formula 1 and pharmaceutically acceptable salts thereof; ##STR1## wherein R.sub.1 is fluorine, chlorine or bromine; wherein R.sub.2 is hydrogen or (C.sub.1 -C.sub.3) alkyl; wherein n is one or 2; wherein R.sub.3 is phenyl, 2-furyl, 3-furyl, 2-thienyl, 3-thienyl, 2-pyridinyl, 3-pyridinyl, 4-pyridinyl; wherein phenyl is optionally substituted with one substituent selected from the group consisting of halogen, trifluoromethyl or sulfonamide. These compounds are useful as hypoglycemic agents.
Abstract: Estriol and estradiol glycidyl ethers, immunogenic conjugates thereof and processes for their preparation are provided. The immunogenic conjugates are useful for eliciting and purifying antibodies and in performing immunoassays for estriol and estradiol.