Carbon Bonded Directly At The 11-, 15- Or 16-position Patents (Class 552/629)
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Patent number: 8586770Abstract: 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: GrantFiled: February 18, 2011Date of Patent: November 19, 2013Assignee: Harbor Therapeutics, Inc.Inventor: James M. Frincke
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Patent number: 8435973Abstract: 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: GrantFiled: September 28, 2010Date of Patent: May 7, 2013Assignee: Abbott Products GmbHInventors: Josef Messinger, Heinrich-Hubert Thole, Bettina Husen, Michael Weske, Pasi Koskimies, Lila Pirkkala
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Patent number: 7838516Abstract: The invention provides 15?-substituted steroidal compounds having selective estrogen receptor activity according to Formula I: wherein, R1 is H, C1-5 alkyl, C1-12 acyl, di-(C1-5 alkyl)aminocarbonyl, (C1-5alkyl)oxycarbonyl or sulfamoyl, R2 is H, C1-3 alkyl, C2-3 alkenyl or C2-3 alkynyl, each of which may be optionally substituted with a halogen, R3 is C1-2 alkyl, ethenyl or ethynyl, each of which may be optionally substituted with a halogen, and R4 is H or C1-12 acyl.Type: GrantFiled: September 5, 2005Date of Patent: November 23, 2010Assignee: N.V. OrganonInventors: Hubert Jan Jozef Loozen, Antonius Gerardus Hendrikus Ederveen, Fredericus Antonius Dijcks
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Patent number: 7375098Abstract: This invention relates to 8?-vinyl-11?-(?-substituted)alkyl-estra-1,3,5(10)-trienes of general formula I with ER?-antagonistic activity, process for their production, their intermediate products, pharmaceutical preparations that contain the compounds according to the invention, as well as their use for the production of pharmaceutical agents. The new compounds can be used for contraception in men and women without influencing other estrogen-sensitive organs such as the uterus or the liver. They are also suitable for treating benign or malignant proliferative diseases of the ovary, such as ovarian cancer and granulosa cell tumors.Type: GrantFiled: April 22, 2004Date of Patent: May 20, 2008Assignee: Schering A.G.Inventors: Nico Braeuer, Olaf Peters, Alexander Hillisch, Rolf Bohlmann, Margit Richter, Hans-Peter Muhn
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Patent number: 7250408Abstract: The novel glucocorticoid receptor antagonists are 11?-substituted steroid compounds of formula (I): wherein R1 denotes a methyl group, a methoxy group, or an ethoxy group; wherein R2 denotes a tert.-butyl group, a 1-hydroxy-1-methylethyl group, a 1-methoxy-1-methylethyl group, an ethyl isocrotonate group, or a substituted phenyl group. The method of treating an individual suffering from glucocorticoid-mediated hypogonadism, sexual dysfunctions, and/or infertility includes administering a daily dosage consisting of an effective amount of one of these 11?-substituted steroid compounds.Type: GrantFiled: December 12, 2003Date of Patent: July 31, 2007Assignee: Bayer Schering Pharma AGInventors: Ulrich Bothe, Gerd Schubert, Guenter Kaufmann, Lothar Sobek, Vladimir Patchev, Alexander Hillisch
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Patent number: 7041839Abstract: 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: GrantFiled: June 22, 2001Date of Patent: May 9, 2006Assignee: Northeastern UniversityInventors: Robert N. Hanson, Carolyn Friel, Choon Young Lee
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Patent number: 7015211Abstract: The present invention relates to analogs of estradiol, which, in their most preferred embodiment, act as locally active estrogens without significant systemic action. A series of 15?-estradiol ester compounds is presented which exhibit excellent biological activity for use in pharmaceutical compositions for the treatment of symptomology associated with menopause. The present invention is therefore directed to compounds according to the structure: where X is R is H, a C1 to C5 alkyl group, optionally substituted with at least one halogen group, such as CH2CH2F, or other group (e.g., CH2CHF2, CH2CF3 or CF3 group); and m is from 0–5, preferably from 0–2.Type: GrantFiled: March 9, 2004Date of Patent: March 21, 2006Assignee: Yale UniversityInventor: Richard Hochberg
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Patent number: 6958327Abstract: The invention relates to novel 18-norsteroids (gonatrienes) of general formula (I), wherein R1, R2, R3, R6, R7, R8, R9, R11, R11?, R14, R15, R15?, R16, R17 and R17? have the meaning cited in the description, and to the use of said compounds as pharmaceutical active ingredients. Said compounds exhibit a high affinity in vitro for estrogen receptor preparations of rat prostate and in an estrogen receptor preparation of rat uterus. Said compounds exhibit in vivo preferential activity on bones as compared to the uterus and/or significant activity with regard to stimulating the expression of 5HT2a-receptors and transporter molecules. The invention also relates to the production of said compounds, therapeutic use and galenic form of said compounds contained in the novel compounds of invention.Type: GrantFiled: November 2, 2000Date of Patent: October 25, 2005Assignee: Schering, AGInventors: Alexander Hillisch, Werner Boidol, Wolfgang Schwede, Peter Esperling, Gerhard Sauer, Christa Hegele-Hartung, Uwe Kollenkirchen, Karl-Heinrich Fritzemeier
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Publication number: 20040198711Abstract: The present invention relates to analogs of estradiol, which, in their most preferred embodiment, act as locally active estrogens without significant systemic action. A series of 15&agr;-estradiol ester compounds is presented which exhibit excellent biological activity for use in pharmaceutical compositions for the treatment of symptomology associated with menopause.Type: ApplicationFiled: March 9, 2004Publication date: October 7, 2004Applicant: YALE UNIVERSITYInventor: Richard Hochberg
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Patent number: 6476012Abstract: The present invention relates to analogs of estradiol, which, in their most preferred embodiment, act as locally active estrogens without significant systemic action. A series of 16&agr;-carboxylic acid substituted steroids and their esters is presented which exhibit excellent biological activity for use in pharmaceutical compositions for the treatment of symptomology associated with menopause. The present invention is therefore directed to compounds according to the structure: Where R is H, a C1 to C5 alkyl, vinyl, CF3, CH2CH2F, CH2CHF2 or CH2CF3; and m is from 0-2, or a pharmaceutically acceptable salt thereof. Preferably, R is methyl, ethyl, propyl, iso-propyl, butyl, iso-butyl, pentyl, neo-pentyl, vinyl, CF3, CH2CH2F, CH2CHF2 or CH2CF3 and m is 0. More preferably, R is methyl, ethyl, CH2CH2F, CH2CHF2 or CH2CF3 and m is 0.Type: GrantFiled: January 23, 2002Date of Patent: November 5, 2002Assignee: Yale UniversityInventor: Richard B. Hochberg
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Publication number: 20020143002Abstract: The present invention relates to analogs of estradiol, which, in their most preferred embodiment, act as locally active estrogens without significant systemic action. A series of 16&agr;-carboxylic acid substituted steroids and their esters is presented which exhibit excellent biological activity for use in pharmaceutical compositions for the treatment of symptomology associated with menopause.Type: ApplicationFiled: January 23, 2002Publication date: October 3, 2002Inventor: Richard B. Hochberg
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Patent number: 5986115Abstract: 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: GrantFiled: January 28, 1999Date of Patent: November 16, 1999Assignee: Schering AGInventors: 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
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Patent number: 5679788Abstract: Intermediate compounds of a formula selected from the group consisting of ##STR1## which are useful intermediates for the preparation of final products of the formula ##STR2## wherein the substituents are defined in the specification.Type: GrantFiled: October 16, 1996Date of Patent: October 21, 1997Assignee: Roussel UclafInventors: Francois Nique, Jean-Georges Teutsch, Patrick Van de Velde
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Patent number: 5656622Abstract: New 15,15-dialkyl-substituted derivatives of the estradiol of general formula I ##STR1## in which R.sup.1 and R.sup.2, independently of one another, are each a hydrogen atom or a straight-chain alkanoyl group with 1 to 10 carbon atoms, a branched-chain alkanoyl group with 3-10 carbon atoms, an alkanoyl group of 3-10 carbon atoms containing a cycloaliphatic structure of 3-6 carbon ring atoms or a benzoyl group, andR.sup.3 and R.sup.4, independently of one another, are each a straight-chain alkyl group with 1 to 10 carbon atoms or a branched-chain alkyl group with 3 to 10 carbon atoms,are described, a process for their production and initial products for this process. The new compounds have--also after oral administration--high estrogenic effectiveness and are suitable for the production of pharmaceutical agents.Type: GrantFiled: June 7, 1995Date of Patent: August 12, 1997Assignee: Schering AktiengesellschaftInventors: James Ronald Bull, Karl-Heinrich Fritzemeier, Christa Hegele-Hartung
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Patent number: 5621124Abstract: 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.Type: GrantFiled: May 26, 1995Date of Patent: April 15, 1997Assignee: Schering AktiengesellschaftInventors: Carsten Seilz, Dieter Hubl
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Patent number: 5587496Abstract: New 15,15-dialkyl-substituted derivatives of the estradiol of general formula I ##STR1## in which R.sup.1 and R.sup.2, independently of one another, are each a hydrogen atom or a straight-chain alkanoyl group with 1 to 10 carbon atoms, a branched-chain alkanoyl group with 3-10 carbon atoms, an alkanoyl group of 3-10 carbon atoms containing a cycloaliphatic structure of 3-6 carbon ring atoms or a benzoyl group, andR.sup.3 and R.sup.4, independently of one another, are each a straight-chain alkyl group with 1 to 10 carbon atoms or a branched-chain alkyl group with 3 to 10 carbon atoms,are described, a process for their production and initial products for this process.The new compounds have--also after oral administration--high estrogenic effectiveness and are suitable for the production of pharmaceutical agents.Type: GrantFiled: August 2, 1994Date of Patent: December 24, 1996Assignee: Schering AktiengesellschaftInventors: James R. Bull, Karl-Heinrich Fritzmeier, Christa Hegele-Hartung
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Patent number: 5554602Abstract: 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: GrantFiled: April 12, 1993Date of Patent: September 10, 1996Assignee: LaRegion WalloneInventors: Siden Top, Anne Vessieres, G'erard Jaquen, Jacques Quivy