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: We disclose agents useful in the treatment of diseases or conditions that would benefit from improved muscle function and including pharmaceutical compositions and diagnostic tests for determining the predisposition of a subject, in particular a male subject, to cardiovascular disease.
Abstract: The present invention provides sustained release formulations of estradiol metabolites whereby the in vivo pharmacokinetics are manipulated by a method selected from the group consisting of chemical modification, crystal packing formation, particle size or a combination thereof. Such compositions are useful in the long-term treatment of a wide variety of diseases.
Abstract: Compositions and methods for treating mammalian disease characterized by undesirable angiogenesis by administering derivatives of 2-methoxyestradiol of the general formula: wherein the variables are defined in the specification.
Type:
Grant
Filed:
August 24, 2001
Date of Patent:
November 14, 2006
Assignee:
Entremed, Inc.
Inventors:
Gregory E. Agoston, Jamshed H. Shah, Kimberly A. Hunsucker, Victor S. Pribluda, Theresa M. LaVallee, Shawn J. Green, Christopher J. Herbstritt, Xiaoguo H. Zhan, Anthony M. Treston
Abstract: The invention describes new compounds as pharmaceutical active ingredients, which have in vitro a higher affinity to estrogen receptor preparations from rat prostates than to estrogen receptor preparations from rat uteri and in vivo a preferential action on bone rather than the uterus, their production, their therapeutic use and pharmaceutical dispensing forms that contain the new compounds. The new compounds are 16?- and 16?-hydroxy-estra-1,3,5(10)-estratrienes, which carry additional substituents on the steroid skeleton and can have one or more additional double bonds in the B-, C- and/or D-rings.
Type:
Grant
Filed:
February 4, 2000
Date of Patent:
September 19, 2006
Assignee:
Schering AG
Inventors:
Hermann Kuenzer, Rudolf Knauthe, Monika Lessl, Karl-Heinrich Fritzemeier, Christa Hegele-Hartung, Ulf Boemer, Gerd Mueller, Dirk Kosemund
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:
Grant
Filed:
June 22, 2001
Date of Patent:
May 9, 2006
Assignee:
Northeastern University
Inventors:
Robert N. Hanson, Carolyn Friel, Choon Young Lee
Abstract: The present invention relates to novel estrogenic compounds. The present invention also relates to methods of treating estrogen deprivation in a subject comprising administering novel estrogenic compounds. Additionally, the present invention relates to methods of synthesizing novel estrogenic compounds.
Type:
Grant
Filed:
April 4, 2003
Date of Patent:
January 31, 2006
Assignee:
Barr Laboratories, Inc.
Inventors:
Edward N. Hill, Thomas W. Leonard, Robert R. Whittle
Abstract: A compound of the formula
wherein the substituents are as defined in the application and its non-toxic, pharmaceutically acceptable acid and base salts useful for hormone replacement for treating menopause or perimenopause without activity at the uterine level treating osteoporosis and strengthening cardiovascular protection in warm-blooded animals.
Type:
Grant
Filed:
January 5, 2001
Date of Patent:
July 23, 2002
Assignee:
Aventis Pharma S.A.
Inventors:
Yasmina Bouali, Jacques Mauger, Patrick Van De Velde, Francois Nique
Abstract: This invention is relating to new estra-1,3,5(10)-trien-sulfamates carrying at the 3-position an R--SO.sub.2 --O--group, with R being an R.sup.1 R.sup.2 N--group in which R.sup.1 and R.sup.2, independently of each other, represent a hydrogen atom, an alkyl residue with 1-5 C atoms or, together with the N atom, a polymethylene-imino residue with 4-6 C atoms or a morpholino residue.The compounds, according to this invention, are suitable for hormonal contraception and climacteric hormone replacement therapy (HRT) as well as for treatment of gynecological and andrological diseases. Hence, only low hepatic estrogenicity is exhibited by the compounds according to this invention.Also described are processes for preparation of the compounds according to this invention and for preparation of pharmaceutical compositions.
Type:
Grant
Filed:
February 2, 1998
Date of Patent:
June 27, 2000
Assignee:
Jenapharm GmbH & Co. KG
Inventors:
Sigfrid Schwarz, Walter Elger, Hans-Joachim Siemann, deceased, by Margit Lucas, heir, by Frank Siemann, heir, Gudrun Reddersen, Birgitt Schneider
Abstract: Novel compounds useful as inhibitors of estrone sulfatase are provided. The compounds have the structural formula (I) wherein r1 is an optional double bond, R.sup.1 and R.sup.2 are selected from the group consisting of hydrogen and lower alky, or together form a cyclic substituent (II) ##STR1## wherein Q is NH, O or CH.sub.2, and the other various substituents are as defined herein. Pharmaceutical compositions and methods for using the compounds of formula (I) to treat estrogen-dependent disorders are provided as well.
Type:
Grant
Filed:
December 24, 1997
Date of Patent:
April 4, 2000
Assignee:
SRI International
Inventors:
Masato Tanabe, Richard H. Peters, Wan-Ru Chao, Kazuhiko Shigeno
Abstract: The application discloses methods of treating mammalian diseases characterized by abnormal cell mitosis by administering estradiol derivatives including those comprising colchicine or combretastatin A-4 structural motifs of the general formulae found below in a dosage sufficient to inhibit cell mitosis. The application discloses novel compounds used in the methods.
Type:
Grant
Filed:
April 25, 1997
Date of Patent:
April 6, 1999
Assignee:
The Children's Medical Center Corporation
Inventors:
Robert John D'Amato, Moses Judah Folkman
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 invention relates to new sulfamate derivatives of 1,3,5(10)-estratriene derivatives of the general formula I ##STR1## wherein the 3-sulfamate moiety is acylated, sulfonated or amidosulfonated. Furthermore, methods for the production of the compound and pharmaceutical preparations containing this compound are described. The compounds according to the invention have an estrogenic effect.
Type:
Grant
Filed:
October 18, 1996
Date of Patent:
January 6, 1998
Assignee:
Jenapharm GmbH & Co. KG.
Inventors:
Sigfrid Schwarz, Walter Elger, Gudrun Reddersen, Birgitt Schneider, Ina Thieme, Margit Richter
Abstract: Conjugates of the formula ##STR1## are prepared by reacting an estradiol derivative with a compound of the formula: ##STR2## in the presence of thionyl chloride or a metal hydride at -30.degree. to 150.degree. C. for 3 minutes to 48 hours and then recovering and purifying the product.
Abstract: The invention relates to a process for the alkylation of estrone derivatives, which is characterized in that a suspension of the estrone derivatives in dimethylformamide is produced and carbonic acid diester and guanidine and/or alkyl guanidines are dissolved in it and in the largely oxygen-free mixture, the reaction is performed at 100.degree.-200.degree. C. under the reaction pressure being established.
Abstract: New 9-alpha-hydroxy steroids are prepared by the introduction of substituents on the D-ring of 9-alpha-hydroxy-androst-4-ene-3,17-dione.The resulting compounds are useful intermediates in the synthesis of corticosteroids.
Type:
Grant
Filed:
October 4, 1994
Date of Patent:
October 15, 1996
Assignee:
Roussel UCLAF
Inventors:
Jacobus N. M. Batist, Arthur F. Marx, Willem J. Van Zoest, Jagdish C. Kapur
Abstract: Estradiol derivatives of the formula: ##STR1## wherein R.sup.1 is C.sub.1-4 alky or C.sub.1-4 alkoxy; R.sup.2 is acyl or benzyl; m is an integer of 1 to 3; n is an integer of 1 to 3; and X is hydroxy or halogen are useful as tumor growth inhibiting agents.
Abstract: The invention presents 17.beta.-nitro and 11.beta., 17.beta.-dinitro esters of estradiol which are made from 3-acyloxy-17-keto- or 3,17-dihydroxy-1,3,5-estratrienes by processes known in the art. The compounds exhibit estrogenic activity.
Type:
Grant
Filed:
September 17, 1993
Date of Patent:
September 10, 1996
Assignee:
The United States of America as represented by the Department of Health and Human Services
Inventors:
Hyun K. Kim, Richard P. Blye, Gabriel Bialy
Abstract: The disclosed invention is drawn to the organometallic oestrogen complex of formula (I): ##STR1## in which A is a C.sub.1-7 alkylene radical or C.sub.2-7 alkenylene or alkynylene radical; M.sub.x is one or more identical or different transition metals; L'.sub.y is one or more identical or different ligands complexing the metal(s) of M.sub.x ; and L is a ligand for covalently coupling M.sub.x to A; and R is H or a C.sub.1-7 alkyl or alkoxy group which may be optionally substituted, particularly with one or more halogens. These complexes are useful for the treatment of hormone-dependent cancers. Also, when the metals of the complex M.sub.x are radioactive isotopes suitable for imaging, the complexes are useful as imaging agents.
Type:
Grant
Filed:
April 12, 1993
Date of Patent:
September 10, 1996
Assignee:
LaRegion Wallone
Inventors:
Siden Top, Anne Vessieres, G'erard Jaquen, Jacques Quivy
Abstract: Disclosed is a method of inhibiting the growth of tumors by administering an estradiol derivative-alkylating agent conjugate of the formula (I'): ##STR1## wherein R.sup.1 is C.sub.1-4 alkyl or C.sub.1-4 alkoxy; R.sup.2 is acyl or benzyl; m is an integer of 1 to 3; and n is an integer of 0 to 3. Also disclosed is a method of inhibiting the growth of tumors by administering a compound of the formula (II); ##STR2## wherein R.sup.1 is C.sub.1-4 alkyl or C.sub.1-4 alkoxy; R.sup.2 is acyl or benzyl; m is an integer of 1 to 3; n is an integer of 0 to 3; and X is hydroxy or halogen.
Abstract: Disclosed is an estradiol derivative-alkylating agent conjugate of the formula (I'): ##STR1## wherein R.sup.1 is C.sub.1-4 alkyl or C.sub.1-4 alkoxy; R.sup.2 is acyl or benzyl; m is an integer of 1 to 3; and n is an integer of 0 to 3, which is useful a growth inhibiting agent.
Abstract: The unsaturated 17.alpha.-cyanomethyl-17.beta.-hydroxy steroids of the formula I, ##STR1## in which R.sub.1 =Me, Eth; R.sub.2 =H, Me; R.sub.3 =H, OH, an acetoxy or alkoxy group; R.sub.4 =H, R.sub.5 =OH, an acetoxy, alkoxy group of R.sub.4 and R.sub.5 together represent a keto- or ketal group and double bonds are contained in the basic structure of the steroid, particularly between the 15 and 16 position in the steroid ring, from unsaturated 17-ketosteroids of the general formula II as described herein with the aforementioned meanings of R.sub.1 to R.sub.5 by reacting the unsaturated 17-ketosteroids with LiCH.sub.2 CN and subsequently hydrolyzing.The compounds of formula I are pharmacologically interesting steroid compounds or also intermediate products for the synthesis of highly-effective steroid products which can be used in human and veterinary medicine for the treatment of endocrine disorders and for reproductive control based on their specific hormonal/anti-hormonal actions.
Abstract: An estradiol derivative-chlorambucil conjugate of the formula (I): ##STR1## wherein R.sup.1 is alkyl or alkoxyl of 1 to 4 carbon atoms; R.sup.2 is acyl, dansyl, or alkyl; R.sup.3, R.sup.4, and R.sup.5 independently are H, oxo, OH, or acyloxy; m is an integer of 1 to 3; and n is an integer of 0 to 3; provided that when n is 0, all of R.sup.3, R.sup.4, and R.sup.5 are not H at the same time, and at least one of R.sup.3, R.sup.4, and R.sup.5 is a group other than H and OH; and further, when n is 2 or 3, the groups R.sup.1 are the same or different; a process for preparing the same, and a pharmaceutical composition containing the conjugate are described.
Abstract: The present invention is directed toward a process for extracting compounds from plant material, comprisinga) contacting hydrolyzed plant material with a supercritical fluid and optionally with a co-solvent and p1 b) recovering the compound from the supercritical fluid.In another embodiment, the present invention is directed toward a process for removing a compound from plant material, comprising contacting the plant material with an acid, a supercritical fluid and a co-solvent, and recovering the compound from the supercritical fluid. The sterols, diosgenin and sarsapogenin, are efficiently extracted from barbasco root and Yucca seed, respectively.
Type:
Grant
Filed:
October 23, 1991
Date of Patent:
October 12, 1993
Assignee:
Schering Corporation
Inventors:
Michelle A. De Crosta, Peter Kabasakalian, Frederick J. F. Honold, Sr.