The A Ring Is A Benzene Ring (e.g., Estrones, Estradiols, Etc.) Patents (Class 552/625)
  • Publication number: 20150094291
    Abstract: The invention provides a method for improving the emotional development of an infant by performing controlled exposure of the infant aged less than six months old to human fear pheromone, preferably with visual fear stimuli, so that the natural synaptic connections in the brain associated with normal fear mechanisms are stimulated and exercised. This can reduce the occurrence of mental illness later in life, in particular reduce the occurrence of schizophrenia. Advantageously the exposure to fear pheromone and visual fear stimuli is terminated and followed by comforting stimuli such as feeding, physical contact, or comforting or happy visual or audible stimuli such as laughter.
    Type: Application
    Filed: October 2, 2013
    Publication date: April 2, 2015
    Applicant: Opendot Research Co Limited
    Inventor: Derek John GOLDSMITH
  • Publication number: 20140235882
    Abstract: The present invention relates to a process for the preparation of estra-1,3,5(10)-trien-3,15?,16?,17?-tetraol (estetrol), via a silyl enol ether derivative 17-B-oxy-3-A-oxy-estra-1,3,5(10),16-tetraene, wherein A is a protecting group and B is —Si(R2)3. The invention further relates to a process for the synthesis of 3-A-oxy-estra-1,3,5(10),15-tetraen-17-one, wherein A is a protecting group, via said silyl enol ether derivative.
    Type: Application
    Filed: July 18, 2012
    Publication date: August 21, 2014
    Inventors: Johannes Jan Platteeuw, Herman Jan Tijmen Coelingh Bennink, Franciscus Wilhelmus Petrus Damen, Michiel Christine Alexander Van Vliet
  • Publication number: 20140107091
    Abstract: The present invention relates to a process for the preparation of a compound of formula (I) comprising the steps of a) reacting a compound of formula (II) with a silylating or an acylating agent to produce compound of formula (III), wherein P1 is a protecting group selected from R2Si—R3R4 or R1CO—, R1 is a group selected from C1-6alkyl or C3-6cycloalkyl, each group being optionally substituted by one or more substituents independently selected from fluoro or C1-4alkyl; R2, R3 and R4 are each independently a group selected from C1-6alkyl or phenyl, each group being optionally substituted by one or more substituents independently selected from fluoro or C1-4alkyl; b) halogenation or sulfinylation of the compound of formula (III) to produce a compound of formula (IV); wherein X is halo, or —O—SO—R5, and R5 is a group selected from C6-10aryl or heteroaryl, each group being optionally substituted by one or more substituents independently selected from chloro or C1-4alkyl; c) dehalogenation or desulfinylation of th
    Type: Application
    Filed: June 1, 2012
    Publication date: April 17, 2014
    Applicant: ESTETRA S.A.
    Inventor: Jean-Claude Pascal
  • Publication number: 20140107358
    Abstract: The present invention relates to a process for the preparation of a compound of formula (I) said process comprising the steps of: a) reacting a compound of formula (II), with an acylating or a silylating agent to produce a compound of formula (III), wherein P1 and P2 are each independently a protecting group selected from R2?Si—R3R4, or R1CO—, wherein R1 is a group selected from C1-6alkyl or C3-6cycloalkyl, each group being optionally substituted by one or more substituents independently selected from fluoro or C1-4alkyl; R2, R3 and R4 are each independently a group selected from C1-6alkyl or phenyl, each group being optionally substituted by one or more substituents independently selected from fluoro or C1-4alkyl; b) reacting the compound of formula (III) in the presence of palladium acetate or a derivative thereof to produce compound of formula (IV); and c) reacting the compound of formula (IV) with a reducing agent to produce compound of formula (I).
    Type: Application
    Filed: June 1, 2012
    Publication date: April 17, 2014
    Applicant: ESTETRA S.A.
    Inventor: Jean-Claude Pascal
  • 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
  • Publication number: 20130225845
    Abstract: The present invention relates to the process for the preparation of estradiol valerate (I) which involves isolation of crystalline estradiol divalerate (III) by crystallization from an alcoholic solvent.
    Type: Application
    Filed: October 28, 2011
    Publication date: August 29, 2013
    Applicant: LUPIN LIMITED
    Inventors: Sachin Arun Sasane, Vijay Ashok Ahire, Rajesh Vyas, Nandu Baban Bhise, Girij Pal Singh
  • Publication number: 20130029901
    Abstract: Bone targeted compounds and methods are provided. Compounds can include a Bone Targeting Portion (RT), having an affinity for bone; a Bone Active Portion (RA) for interacting with and affecting bone; and a Linking Portion (RL) connecting the Bone Targeting Portion and the Bone Active Portion.
    Type: Application
    Filed: July 30, 2012
    Publication date: January 31, 2013
    Inventors: William M. PIERCE, JR., K. Grant TAYLOR, Leonard C. WAITE, Kevyn MERTEN
  • Publication number: 20130018022
    Abstract: The present invention relates to a pharmaceutical composition including a testis extract serving as an active ingredient for treating and preventing anemia, in which since the testis extract induces proliferation of hematopoietic stem cell, an increase in the number of red blood cell, and an increase in the amount of hemoglobin, it is effectively used as a therapeutic agent for treating anemia related to red blood cell and hemoglobin in women of childbearing age, post-childbearing age, and during pregnancy, as well as in men.
    Type: Application
    Filed: April 22, 2010
    Publication date: January 17, 2013
    Applicant: INDUSTRY-ACADEMIC COOPERATION FOUNDATION, YEUNGNAM UNIVERSITY
    Inventors: In-Ho Choi, Dong-Mok Lee, Eun-Ju Lee, Ki-Ho Lee, Yong-Pil Cheon, Tae-Hoon Chun
  • Patent number: 8349819
    Abstract: A process in which urine is optionally filtered to remove solid extraneous matter and optionally treated so as to reduce the phenolic content of the urine to give and the resulting fluid is then subjected to a solid extraction of the major concentration steroids content therefrom by a first suitable resin (to yield a first resin laden with major concentration steroids and a minor concentration steroid laden first liquid remainder). The minor concentration steroid liquid remainder is subjected to a solid extraction of the minor concentration steroid content therefrom by a second suitable resin (to yield a second resin laden with minor concentration steroids and a second liquid remainder). The first and second resins laden with their respective steroids are then eluted and the eluates are collected separately and optionally subjected to further purification and chromatographic separations, with each resulting separate collection being analyzed for the steroid content thereof.
    Type: Grant
    Filed: February 10, 2005
    Date of Patent: January 8, 2013
    Assignee: Dr. Reddy's Laboratories New York, Inc.
    Inventors: John Lomans, Carmen Leiva-paredes
  • Patent number: 8273908
    Abstract: Process for the preparation of a compound of general formula (II) wherein R1 and R2 independently are hydrogen or a hydroxy- or hydrocarbyl group; or wherein R1 and R2 together are a double bonded oxygen; R3 is hydrogen; R?4 is a nitrobenzophenone group; and R5 and R6 independently are hydrogen or a hydroxy- or hydrocarbyl group; from a compound of general formula (I) wherein, R1, R2 R3, R5 and R6 are as defined above and R4 is hydrogen; wherein the compound of formula (I) is reacted under alkaline conditions with 2-chloro-5-nitrobenzophenone in the presence of an alkanolic solvent and the compound of formula (II) is directly crystallized from this alkanolic solvent. Complex of an alkanol and a compound of general formula (II) obtainable from the above process and processes wherein the above process or complex are used.
    Type: Grant
    Filed: August 22, 2005
    Date of Patent: September 25, 2012
    Assignee: MSD Oss B.V.
    Inventors: Lambertus Gerardus Maria Willems, Henricus Johannes Franciscus Maas, Martin Ostendorf
  • Publication number: 20120172344
    Abstract: Provided is an insulin-producing cell inducer, an enhancer for glucose intake of muscles, and a therapeutic agent for diabetes or diabetes complications, wherein an active ingredient of those provided is an estrogenic compound such as estrogen and estradiol. With the present invention, functions of insulin-producing cells can be recovered since the insulin-producing cells are induced in pancreatic ducts, and blood glucose level can be immediately lowered since glucose in the blood can be effectively taken up by muscles; therefore, diabetes and diabetes complications can be prevented or treated.
    Type: Application
    Filed: July 16, 2010
    Publication date: July 5, 2012
    Applicant: KYUSHU UNIVERSITY, NATIONAL UNIVERSITY CORPORATION
    Inventor: Akari Inada
  • Publication number: 20120082715
    Abstract: A composition comprising a glassified, stabilized particle preparation having a low water activity (between about 0.1 and 0.9) is provided. The preparations provide improved products with enhanced storage stability, less expensive cost of processing, and extended shelf life. The glassified, stabilized particle preparations are particularly efficacious in the preparation of perishable products, especially pharmaceutical agents, such as human blood and blood products (e.g., red blood cells). A single emulsion process comprising a 2-phase system for preserving food and pharmaceutical products is also provided. Stabilized biological products as glassified beads are also provided, as well as a method for rehydrating and/or reconstituting the glassified beads to provide useful and fully active reconstituted and/or rehydrated materials is also presented.
    Type: Application
    Filed: September 2, 2011
    Publication date: April 5, 2012
    Inventor: David Needham
  • Publication number: 20120071455
    Abstract: Disclosed herein are 6-substituted 13-demethyl-estradiol derivatives as selective ER? agonists. Also disclosed is a method for treating pain by administering these 6-substituted 13-demethyl-estradiol derivatives.
    Type: Application
    Filed: September 14, 2011
    Publication date: March 22, 2012
    Inventors: James G. Yarger, Steven H. Nye
  • Publication number: 20110201585
    Abstract: A method of reducing or inhibiting the risk of infection from sexually transmitted viral infections (STIs), such as HIV and HPV, comprising the topical administration of oestrogenic compounds, analogues or metabolites thereof or oestrogen agonists to a human penis. A method to increase keratinisation of the penile epithelium is also provided. Suitable formulations are also provided.
    Type: Application
    Filed: May 9, 2008
    Publication date: August 18, 2011
    Inventors: Roger Short, Andrew Pask
  • Patent number: 7973185
    Abstract: The invention relates to a process for the preparation of a phenolic hydroxy-substituted compound of the general formula (I) by desalkylation of an alkyl aryl ether of the general formula (II) by treatment with a thiourea/aluminum chloride reagent pair, in said general formulae R1 stands for straight chain or branched C1-6 alkyl group; R2, R3 , R4 , R5, and R6 have the same or different meanings and stand for hydrogen or halogen atom, hydroxy, carboxy, nitro, oxo, C1-6 alkylcarbonyl, straight chain or branched alkyl or -alkoxy, or aryl group, or R2 and R3 together stand for a 5-7 membered ring or fused ring system; said 5-7 membered ring may be a partially saturated ring optionally substituted with an oxo group or can be an unsaturated ring; or said fused ring system may constitute with the first ring a steroid, preferably an estratriene derivative optionally substituted with an oxo or C1-6 alkylcarbonyloxy group in the 17 position.
    Type: Grant
    Filed: December 7, 2005
    Date of Patent: July 5, 2011
    Assignee: Richter Gedeon Nyrt.
    Inventors: András Vass, József Dudás, László Borbély, Ferenc Haász, Péter Jekkel
  • Publication number: 20110158947
    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.
    Type: Application
    Filed: July 9, 2009
    Publication date: June 30, 2011
    Inventor: Aleksandar Jovanovic
  • Publication number: 20110152544
    Abstract: The invention provides a process for the preparation of 2-substituted-derivatives of estrone and estradiol comprising i) the preparation of a compound of general formula (II) by reacting a compound of general formula (I) in one or more steps to a compound of general formula II wherein R1 is a C1-C10 alkyl, alkenyl or aryl group; —Cl, —Br, —I, —F; —CN; —OH; or a —OR2, —O(CO)R2 or —R2-OH group, wherein R2 is an alkyl or alkylene group having 1-6 C atoms; and the bonding between atoms 9 and 10 is a single or a double bond. ii) aromatization of the compound of general formula II to a compound of general formula III wherein R1 and R2 have the above defined meanings; and iii) optionally, reduction of the compound of general formula III to a compound of general formula IV wherein R1 and R2 have the above defined meanings. Furthermore the invention provides several novel compounds, which can be intermediates in the above process, and processes to prepare these novel compounds.
    Type: Application
    Filed: February 22, 2011
    Publication date: June 23, 2011
    Applicant: N. V. Organon
    Inventors: Johannes STOELWINDER, Nicolaas Elisabeth Cornelis MOERS
  • Publication number: 20100317628
    Abstract: The present invention is a method for identifying agents which modulate microRNA activity. The invention involves contacting a cell harboring a microRNA and a microRNA binding sequence, which is operably linked to a nucleic acid molecule encoding a reporter protein, with a test agent increases or decreases the expression of the reporter protein thereby identifying a microRNA modulator. Antagonists identified by this screening assay are provided, as are methods for using the same to inhibit microRNA activity and prevent or treat disease.
    Type: Application
    Filed: February 20, 2009
    Publication date: December 16, 2010
    Inventors: Qihong Huang, Alexander Deiters, Kiranmai Gumireddy
  • Publication number: 20100286105
    Abstract: Compositions and methods for treating hyperandrogenism and conditions associated therewith, including polycystic ovary syndrome are disclosed. The invention is directed to methods for treating hyperandrogenism and conditions associated therewith, in a subject comprising administering a fatty acid ester of an estrogen or an estrogen derivative. Furthermore the invention is directed to compositions for treating hyperandrogenism and conditions associated with hyperandrogenism, including polycystic ovary syndrome, comprising a fatty acid ester of an estrogen or an estrogen derivative.
    Type: Application
    Filed: September 28, 2007
    Publication date: November 11, 2010
    Inventor: Bindu Tejura
  • Patent number: 7795241
    Abstract: The present invention is a prodrug derivative of ethinyl estradiol according to Formula I:
    Type: Grant
    Filed: July 3, 2006
    Date of Patent: September 14, 2010
    Assignee: Warner Chilcott Company, LLC
    Inventors: James Keown, James William McIlroy, John Alexander King, Claire Gilligan, William Paul Armstrong
  • Patent number: 7749987
    Abstract: A method of achieving contraception in a woman which comprises administering orally to said woman an estroprogestative composition comprising nomegestrol acetate and an estrogen is provided.
    Type: Grant
    Filed: January 3, 2007
    Date of Patent: July 6, 2010
    Assignee: Laboratorie Theramek
    Inventors: Jacques Paris, Jean-Louis Thomas, Michel Lanquetin, Anny Lanquetin, legal representative, Jean-Philippe Lanquetin, legal representative
  • Patent number: 7732493
    Abstract: The invention relates to new 2-substituted D-homo-estra-1,3,5(10)-trienes of general formula I in which R2 means a C1-C8-alkyl group, a C1-C8-alkyloxy group or a halogen atom, R13 means a hydrogen atom or a methyl group, R17 means a hydrogen atom or a fluorine atom, as well as their pharmaceutically acceptable salts, their manufacture and use as medicaments for prophylaxis and therapy of estrogen-dependent diseases that can be influenced by inhibition of 17?-hydroxy steroid dehydro-genase type 1.
    Type: Grant
    Filed: August 15, 2008
    Date of Patent: June 8, 2010
    Assignee: Bayer Schering Pharma Aktiengesellschaft
    Inventors: Alexander Hillisch, Olaf Peters, Christian Gege, Wilko Regenhardt, Gabriele Moeller, Dominga Deluca, Jerzy Adamski, Walter Elger, Birgitt Schneider
  • Publication number: 20090312293
    Abstract: A process for the recovery and purification of natural hydrophilic water-soluble products in conjugated form from vegetable aqueous extracts or physiological fluids, by adsorption of the extracts or fluids on a lipophilic resin, followed by desorption and recovery of the eluate, which process is characterized in that the resin is a porous styrene-divinyl benzene polymer brominated at the styrene and/or divinylbenzene portion, with 600 m2/g area, 1.3 ml/g volume (dry weight), about 200 Angstrom pore size.
    Type: Application
    Filed: December 19, 2006
    Publication date: December 17, 2009
    Applicant: EVULTIS S.A.
    Inventors: Giancarlo Mazzola, Anna Anzani
  • Publication number: 20090197842
    Abstract: The present invention provides a therapeutic agent for neuropathic pain having an excellent treating effect on neuropathic pain, which is an intractable disorder. More specifically, the present invention provides a therapeutic agent for neuropathic pain and a pharmaceutical composition for treating neuropathic pain, comprising (1) a compound having an anti-progesterone activity (for example, fulvestrant (ICI182.780), fluocinolone acetonide, triamcinolone acetonide, etc.), (2) a compound having an estrogen activity (for example, 17?-estradiol), or (3) a mixture of a compound having an anti-progesterone activity and a compound having an estrogen activity (for example, 17?-estradiol and fulvestrant), as an active ingredient; a method for treating neuropathic pain using such a compound, and the like.
    Type: Application
    Filed: September 26, 2006
    Publication date: August 6, 2009
    Inventor: Tsutomu Tanabe
  • Publication number: 20090163458
    Abstract: The present disclosure relates generally to methods and compositions for treating symptoms of Parkinson's disease and/or other movement disorders. More particularly, the present disclosure describes a method for treating symptoms of Parkinson's disease and related disorders by administering a composition comprising one or more of the following active agents; estradiol, estriol, testosterone, and 19-nortestosterone. In addition, the compositions of the present invention can be used for enhancing or optimizing the effectiveness of neural stimulation in treating the symptoms of movement disorders such as Parkinson's disease.
    Type: Application
    Filed: November 6, 2008
    Publication date: June 25, 2009
    Inventor: Ellis L Kline
  • Publication number: 20090156843
    Abstract: The present invention relates to a process for aromatizing 19-norandrost-4-en-3-ones (formula (II)) to astra-1,3,5(10)-trienes (formula (I))
    Type: Application
    Filed: December 12, 2008
    Publication date: June 18, 2009
    Inventors: Michael SANDER, Jorg Gries, Armin Schutz
  • Publication number: 20090131698
    Abstract: The present invention relates to a method for obtaining a natural mixture of conjugated estrogens from urine of pragnant mares (PMU) and use of a macroporous adsorption resin in the method. The method for obtaining a natural mixture of conjugated estrogen from PMU includes the steps of pretreating raw PMU; adsorbing the natural mixture of conjugated estrogens contained in PMU with a macroporous adsorption resin; washing the macroporous adsorption resin laden with the mixture of conjugated estrogens with an alkaline aqueous solution; and eluting the washed adsorption resin with an eluting agent to obtain the mixture of conjugated estrogens. The macroporous adsorption resin is a styrene-divinylbenzene semipolar macroporous adsorption resin with ester group structure. The method according to the invention solves the problems of low adsorptive capacity and high cost existed in the conventional methods, and is suitable for large-scale production.
    Type: Application
    Filed: December 5, 2006
    Publication date: May 21, 2009
    Applicant: Xinjiang Tefeng Pharmaceutical Co., Ltd.
    Inventors: Xiaoli Gao, Jianmin Xiao
  • Patent number: 7507725
    Abstract: The invention relates to compounds which, acting as a prodrug and/or support, enable an active agent to be taken up by the erythrocytes and/or an active agent to bind to the erythrocytes. The uptake of these compounds by and/or the binding thereof to the erythrocytes is made possible by a group of formula —SO2NR1R2, wherein R1 and R2, independently of each other, mean a hydrogen atom, an acyl group, an alkyl group, a cycloalkyl group, an aryl group, a cyano group or a hydroxy group. The inventive prodrugs enable active agents such as endogenic substances, natural substances and synthetic substances with therapeutically useful properties which have a high “first path” effect, to be administered orally effectively or significantly improve the oral activity thereof.
    Type: Grant
    Filed: May 8, 2001
    Date of Patent: March 24, 2009
    Assignee: Schering AG
    Inventors: Walter Elger, Alexander Hillisch, Annemarie Hedden, Sigfrid Schwarz, Klaus Schollkopf
  • Publication number: 20090062558
    Abstract: The present invention relates to a new process for preparing estrogen-antagonistic 11?-fluoro-17?-alkylestra-1,3,5(10)-triene-3,17-diols of the general formula I having a 7?-(?-alkylamino-?-perfluoroalkyl)alkyl side chain and to ?-alkyl(amino)-?-perfluoro(alkyl)alkanes of the general formula II, to processes for their preparation and to the intermediates required for this purpose.
    Type: Application
    Filed: August 29, 2008
    Publication date: March 5, 2009
    Inventors: Michael SANDER, Danja Grossbach, Christian Dinter, Jorma Hassfeld, David Voigtlaender
  • Patent number: 7495115
    Abstract: Conjugates comprising one or more steroids conjugated with one or more mammalian proteins are disclosed. The conjugates are useful for diagnosis or treatment of solid cancer and haematological malignancies. Further the conjugates exhibits a synergistic action together with a cytoskeleton acting drug such as Taxol®, which enable the treatment of cancers that otherwise would be non responsive to Taxol®.
    Type: Grant
    Filed: July 14, 2003
    Date of Patent: February 24, 2009
    Assignee: Bionature E.A., Ltd.
    Inventor: Elias Castanas
  • Publication number: 20090023896
    Abstract: This invention relates to compounds that as prodrugs and/or vehicles make it possible for an active ingredient to be taken up into erythrocytes and/or an active ingredient to bind to erythrocytes, whereby the uptake of the compounds into erythrocytes and/or the binding of the compounds to erythrocytes is made possible by a group —SO2NR1R2, whereby R1 and R2, independently of one another, mean a hydrogen atom, an acyl group, an alkyl group, a cycloalkyl group, an aryl group, a cyano group or a hydroxy group. By the prodrugs according to the invention, active ingredients, such as endogenous substances, natural substances and synthetic substances with therapeutically valuable properties with a high “first pass” effect are made available orally to a reasonable extent or are decisively improved relative to oral activity.
    Type: Application
    Filed: June 19, 2008
    Publication date: January 22, 2009
    Inventors: Walter Elger, Alexander Hillisch, Annemarie Hedden, Sigfrid Schwarz, Klaus Schollkopf
  • Publication number: 20090012319
    Abstract: The invention provides a process for the preparation of 2-substituted-derivatives of estrone and estradiol. The invention also provides several novel compounds, which can be intermediates in the process, and processes to prepare these novel compounds. The invention also provides 2-alkoxy-estrone, 2-alkoxy-estradiol or mixtures thereof essentially free from other estrogenic intermediates.
    Type: Application
    Filed: August 1, 2005
    Publication date: January 8, 2009
    Applicant: N.V. Organon
    Inventors: Johannaes Stoelwinder, Nicolaas Elisabeth Moers
  • Publication number: 20080306285
    Abstract: Disclosed herein are heat-labile prodrugs, their preparation and uses.
    Type: Application
    Filed: April 28, 2008
    Publication date: December 11, 2008
    Applicant: ALEXZA PHARMACEUTICALS, INC.
    Inventors: Ron L. Hale, Dennis W. Solas, Kathleen Simis, Amy T. Lu, Peter M. Lloyd
  • Patent number: 7435757
    Abstract: The invention relates to new 2-substituted D-homo-estra-1,3,5(10)-trienes of general formula I in which R2 means a C1-C8-alkyl group, a C1-C8-alkyloxy group or a halogen atom, R13 means a hydrogen atom or a methyl group, R17 means a hydrogen atom or a fluorine atom, as well as their pharmaceutically acceptable salts, their manufacture and use as medicaments for prophylaxis and therapy of estrogen-dependent diseases that can be influenced by inhibition of 17?-hydroxy steroid dehydro-genase type 1.
    Type: Grant
    Filed: July 1, 2005
    Date of Patent: October 14, 2008
    Assignee: Schering AG
    Inventors: Alexander Hillisch, Olaf Peters, Christian Gege, Wilko Regenhardt, Gabriele Moeller, Dominga Deluca, Jerzy Adamski, Walter Elger, Birgitt Schneider
  • Publication number: 20080220069
    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.
    Type: Application
    Filed: September 13, 2005
    Publication date: September 11, 2008
    Applicant: PR PHARMACEUTICALS, INC.
    Inventor: S. Dean Allison
  • Patent number: 7378404
    Abstract: This invention describes the new 8?-substituted estratrienes of general formula I in which R2, R3, R6, R6?, R7, R7?, R9, R11, R11?, R12, R14, R15, R15?, R16, R16?, R17 and R17? have the meanings that are indicated in the description, and R8 means a straight-chain or branched-chain, optionally partially or completely halogenated alkyl or alkenyl radical with up to 5 carbon atoms, an ethinyl- or prop-1-inyl radical, as pharmaceutical active ingredients that have in vitro a higher affinity to estrogen receptor preparations of rat prostates than to estrogen receptor preparations of rat uteri and in vivo preferably a preferential action on bone rather than the uterus and/or a pronounced action with respect to stimulation of the expression of 5HT2a-receptors and 5HT2a-transporters, their production, their therapeutic use and pharmaceutical dispensing forms that contain the new compounds.
    Type: Grant
    Filed: April 12, 2001
    Date of Patent: May 27, 2008
    Assignee: Schering Aktiengesellschaft
    Inventors: Olaf Peters, Alexander Hillisch, Ina Thieme, Walter Elger, Christa Hegele-Hartung, Uwe Kollenkirchen, Karl-Heinrich Fritzemeier, Vladimir Patchev
  • Publication number: 20080119447
    Abstract: A compound having the structure: wherein R1, R2, R3, R4, R5, R6, R7 and R9 are independently hydrogen, C1 to C6 alkyl or substituted alkyl, halogen, sulfate or glucuronide moieties; the symbol represents either a single or a double bond and when the symbol is a double bond and forms a keto group at position 3 or 17, then no R7 or R6 is present, respectively; the symbol represent the presence or absence of a bond at position 10; and the symbol represents any type of bond regardless of the stereochemistry. The invention also embraces the enantiomers, other stereochemical isomers, hydrates, solvates, tautomers and pharmaceutically acceptable salts of said compounds.
    Type: Application
    Filed: November 29, 2007
    Publication date: May 22, 2008
    Inventor: James Yarger
  • Patent number: 7371741
    Abstract: Compositions and methods for treating mammalian disease characterized by undesirable angiogenesis by administering compounds of the general formula: wherein the variables are defined in the specification.
    Type: Grant
    Filed: May 28, 2004
    Date of Patent: May 13, 2008
    Assignee: EntreMed, Inc.
    Inventors: Gregory E. Agoston, Theresa M. LaVallee, Victor S. Pribluda, Jamshed H. Shah, Anthony M. Treston
  • Patent number: 7109360
    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
  • Patent number: 6995278
    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: February 8, 2001
    Date of Patent: February 7, 2006
    Assignee: Entre Med, Inc.
    Inventors: Gregory E. Agoston, Victor Pribluda, Anthony M. Treston, Shawn J. Green
  • Patent number: 6958327
    Abstract: 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: Grant
    Filed: November 2, 2000
    Date of Patent: October 25, 2005
    Assignee: Schering, AG
    Inventors: Alexander Hillisch, Werner Boidol, Wolfgang Schwede, Peter Esperling, Gerhard Sauer, Christa Hegele-Hartung, Uwe Kollenkirchen, Karl-Heinrich Fritzemeier
  • Patent number: 6831073
    Abstract: A method of treating estrogenic deficiencies in women while further avoiding the appearance of osteoporosis, withdrawal bleeding and cardiovascular diseases in post-menopausal women without any androgenic effect, and no deleterious effects on blood vessels comprising continuously without interruption administering to said women, a combination of 0.5 to 3 mg of an estrogenic compound and 1.5 to 3.75 mg of nomegestrol acetate.
    Type: Grant
    Filed: March 17, 1999
    Date of Patent: December 14, 2004
    Assignee: Laboratoire Theramex
    Inventors: Michel Lanquetin, Jacques Paris, Jean-Louis Thomas
  • Publication number: 20040224935
    Abstract: Steroidal antiandrogens and pharmaceutical compositions thereof, are used for reduction of the risk of developing, or for treatment of, androgen-dependent skin related diseases.
    Type: Application
    Filed: March 31, 2004
    Publication date: November 11, 2004
    Applicant: Endorecherche, Inc.
    Inventors: Fernand Labrie, Louis Provencher, Sylvain Gauthier
  • Publication number: 20040157816
    Abstract: The pharmaceutical and/or cosmetic compositions for treatment of obesity and/or overweight contain an effective amount of a fatty-acid monoester of a 2 hydroxy derivative estrogen and a fatty acid wherein the estrogen is preferably a 2 hydroxy derivative of estrone, diethylstilbestrol, estriol, estradiol or ethinyl estradiol and the fatty acid is selected from the group consisting of the fatty acid oleic acid, arachadonic, palmitic, palmitoleic, linoleic, linolenic, cis 13 docosenoic acid, and the fatty acid, cis 15 tetracosenoic acid eicosenoic acid, especially cis 11 eicosenoic, although cis 5, cis 8, and cis 13 eicosenoic acid are also effective. The C-22 fatty acid monoester of estrogen, cis 13 docosenoic acid (Erucic acid), and the C-24 fatty acid monoester of estrogen, cis 15 tetracosenoic acid (Nervonic acid) are also effective and are included in this disclosure.
    Type: Application
    Filed: November 20, 2003
    Publication date: August 12, 2004
    Inventor: Michael P. Girouard
  • Patent number: 6767903
    Abstract: The invention relates to new 7&agr;, 17&agr;, 17&bgr;-substituted testosterone derivatives of general formula (I) and their use as pure antiandrogens for the long-term therapy of androgen-dependent diseases, notably for the long-term antiandrogen therapy of prostate carcinoma.
    Type: Grant
    Filed: June 22, 2001
    Date of Patent: July 27, 2004
    Assignee: Schering AG
    Inventors: Arwed Cleve, Gerhard Sauer, Christoph Huwe, Karsten Parczyk, Jens Hoffmann, Martin Schneider
  • Publication number: 20040142915
    Abstract: The present invention relates to novel 11-&bgr; estradiol ester compounds and their use as locally active estrogens in the treatment of the symptomology of menopause and to treat estrogen sensitive cancers, including breast cancer.
    Type: Application
    Filed: October 1, 2003
    Publication date: July 22, 2004
    Applicant: YALE UNIVERSITY
    Inventor: Richard Hochberg
  • Publication number: 20040072812
    Abstract: The present invention relates to a process for extracting conjugated estrogens from pregnant mare urine. The present invention further relates to a process for obtaining a natural mixture of conjugated estrogens. The mixture of conjugated estrogens can be used to prepare products for estrogen replacement therapy or hormone replacement therapy.
    Type: Application
    Filed: October 9, 2002
    Publication date: April 15, 2004
    Inventors: John Lomans, Carmen Leiva-Paredes
  • Publication number: 20040043972
    Abstract: The invention concerns a 3-methylene steroid derivative selected from the group consisting of (7&agr;,17&bgr;)-7-methyl-3-methyleneestr-5(10)-en-17-ol, (5&bgr;,7&agr;,17&agr;)-5,10-epoxy-7-methyl-3-methylene-19-norpregn-20-yn-17-ol, (5&bgr;,7&agr;,17&bgr;)-5,10-epoxy-7-methyl-3-methyleneestran-17-ol, (5&agr;,7&agr;,17&agr;)-7-methyl-3-methylene-19-norpregn-20-en-17-ol, (5&agr;,7&agr;,17&agr;)-7-methyl-3-methylene-19-norpregn-20-yn-17-ol, (5&bgr;,7&agr;,17&agr;)-7-methyl-3-methylene-19-norpregnan-17-ol, (7&agr;)-7-methyl-3,17-dimethyleneestr-5(10)ene, (7&agr;,16&agr;,17&bgr;)-7,16-dimethyl-3-methylene-17-(1-propynyl)estr-5(10)-en-17-ol, (7&agr;,16&agr;,17&bgr;)-16-ethyl-7-methyl-3-methylene-17-(1-propynyl)estr-5(10)-en-17-ol, (7&agr;,17&bgr;)-7-methyl-3-methylene-17-(1 -propynyl)estr-5(10)-en-17-ol, (7&agr;,16&bgr;,17&bgr;)-16-ethyl-7-methyl-3-methylene-19-norpregn-5(10)-en-20-yn-17-ol, (7&agr;)-3-methylene-7-methylestr-5(10)-ene, (7&agr;)-3-methylene-7-methylestr-5(10)-en-17-one O-methyloxime and (7&agr;)-3-m
    Type: Application
    Filed: April 28, 2003
    Publication date: March 4, 2004
    Inventors: Plate R. Ralf, Bagchus W.M. Wilhelmina Maria
  • Patent number: 6689768
    Abstract: The pharmaceutical preparations for treating side effects, such as hot flashes, prostate enlargement and gynecomastia, during and/or after treatment with analogs or antagonists of gonadotropin-releasing hormone (GnRHa therapy) contain an effective amount of a chemically modified derivative of 17&agr;-estradiol, a chemically modified derivative of 17&bgr;-estradiol and/or a chemical modified derivative of estriol. Pharmaceutical preparations containing 14&agr;, 15&agr;-methylene-1,3,5(10),8-tetraene-3,17&agr;-diol are particularly preferred.
    Type: Grant
    Filed: June 26, 2001
    Date of Patent: February 10, 2004
    Assignee: Jenapharm GmbH & Co. KG
    Inventors: Mcihael Oettel, Ludwig Wildt, Peter Licht, Joachim Neuwinger, Wolfgang Hummel, Ralph Dittrich
  • Patent number: RE39592
    Abstract: An extended release composition comprising a first composition comprising growth promoters and a second composition comprising growth promoters and a biodegradable polymer is described. A method of increasing weight gain in food animals utilizing the composition, a pharmaceutical dosage form containing the composition and a method of preparing the pharmaceutical dosage form are also described, as are pellets of the composition for implantation in food animals.
    Type: Grant
    Filed: December 22, 2004
    Date of Patent: April 24, 2007
    Assignee: Intervet Inc.
    Inventors: Susan Mancini Cady, Claude Macar, John W. Gibson