Nitrogen Or Sulfur Containing Patents (Class 552/626)
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Publication number: 20150132388Abstract: The present invention relates to pharmaceutically acceptable complex formulae comprising complexes of Fulvestrant, or a salt, or derivatives thereof and complexation agents and pharmaceutically acceptable excipients, process for the preparation thereof and pharmaceutical compositions containing them. The complex formulae of the present invention have improved physicochemical properties which makes the compound orally available and makes oral administration of the compound possible in the treatment of hormone receptor positive metastatic breast cancer in postmenopausal women with disease progression following anti-estrogen therapy.Type: ApplicationFiled: November 11, 2014Publication date: May 14, 2015Inventors: Erzsébet Réka Angi, Richard Balázs Kárpáti, Zsolt Ötvös, László Molnár, Hristos Glavinas, Genovéva Filipcsei
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Publication number: 20150018322Abstract: Various prodrug compounds having the general structure: Active agent-(acid)-(linker)-SO2NR1R2 are described herein. Compounds having this general structure were shown to be more orally active than the unmodified parent molecule.Type: ApplicationFiled: July 11, 2014Publication date: January 15, 2015Inventors: Klaus Nickisch, Bindu Santhamma, Gulzar Ahmed, Frederick Meece, Walter Elger, Ralf Wyrwa, Hareesh Nair
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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: 8492570Abstract: The invention relates to the use of 2-substituted estra-1,3,5(10)-triene-3-yl sulfamates of general formula I, in addition to their pharmaceutically acceptable salts for producing a medicament. Said compounds have an anti-tumour action.Type: GrantFiled: September 22, 2008Date of Patent: July 23, 2013Assignee: Sterix LimitedInventors: Alexander Hillisch, Olaf Peters, Christian Gege, Wilko Regenhardt, Dirk Kosemund, Gerhard Siemeister, Eberhard Unger, Ulrich Bothe
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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: 8258328Abstract: The subject of the invention is a method for preparing compounds of general formula (I): in which A, Z, R3 are as defined in the description, and the intermediate compounds for carrying out this method.Type: GrantFiled: October 29, 2010Date of Patent: September 4, 2012Assignee: Aventis Pharma S.A.Inventors: Denis Prat, Christian Moratille, Francoise Benedetti, Lahlou Nait-Bouda
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Patent number: 8168621Abstract: A compound having the structure: wherein R1, R2, R, R, X, Y and Z are as defined herein. The compounds are estrogen receptor modulators useful for the treatment of proliferative disorders.Type: GrantFiled: June 4, 2008Date of Patent: May 1, 2012Assignee: Endece, LLCInventor: James Yarger
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Publication number: 20120083440Abstract: 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: ApplicationFiled: October 5, 2011Publication date: April 5, 2012Inventors: William M. Pierce, JR., K. Grant Taylor, Leonard C. Waite, Kevyn Merten
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Patent number: 8088758Abstract: 3,15-substituted estrone compounds which act as inhibitors of 17?-hydroxysteroid dehydrogenase type I (17?-HSD1), salts thereof, pharmaceutical preparations containing such compounds, processes for preparing such compounds, and therapeutic uses of such compounds, particularly in the treatment or inhibition of steroid hormone dependent diseases or disorders, such as steroid hormone dependent diseases or disorders requiring the inhibition of 17?-hydroxysteroid dehydrogenase type I enzymes and/or requiring the lowering of the endogenous 17?-estradiol concentration, as well as the general use of selective 17?-hydroxysteroid dehydrogenase type 1 inhibitors which possess in addition no or only pure antagonistic binding affinities to the estrogen receptor for the treatment or inhibition of benign gynecological disorders, particularly endometriosis.Type: GrantFiled: November 9, 2004Date of Patent: January 3, 2012Assignee: Abbott Products GmbHInventors: Josef Messinger, Heinrich-Hubert Thole, Bettina Husen, Bartholomeus Johannes Van Steen, Gyula Schneider, Johannes Bernardus Everardus Hulshof, Pasi Koskimies, Nina Johansson, Jerzy Adamski
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Patent number: 8071575Abstract: 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: GrantFiled: February 22, 2008Date of Patent: December 6, 2011Assignee: University of Louisville Research FoundationInventors: William M. Pierce, Jr., K. Grant Taylor, Leonard C. Waite
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Publication number: 20110269689Abstract: High penetration compositions (HPC) of a parent compound, which are capable of crossing biological barriers with high penetration efficiency. The HPCs are capable of being converted to parent drugs or parent drug-related compounds such as metabolites after crossing one or more biological barriers and thus can render treatments for the conditions that the parent drugs or parent drug-related compounds can. Additionally, the HPCs are capable of reaching areas that their parent drugs or parent drug-related compounds may not be able to access or to render a sufficient concentration at the target areas HPCs of NSAIA, for example, have demonstrated indications such as treating hair loss. A HPC can be administered to a subject through various administration routes, e.g., locally delivered to an action site of a condition with a high concentration or systematically administered to a biological subject and enter the general circulation with a faster rate.Type: ApplicationFiled: December 4, 2009Publication date: November 3, 2011Inventor: Chongxi Yu
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Patent number: 8030296Abstract: There is provided a compound of Formula I wherein X is a ring system; R1 is any one of a sulphamate group, a phosphonate group, a thiophosphonate group, a sulphonate group or a sulphonamide group; R2 is any one of a sulphamate group, a phosphonate group, a thiophosphonate group, a sulphonate group or a sulphonamide group; wherein when X is a steroidal structure and both of R1 and R2 are sulphamate groups, the steroidal ring system (X) represents an oestrogen; and wherein said compound is capable of inhibiting steroid sulphatase (STS) activity and/or is capable of acting as a modulator of cell cycling and/or as a modulator of apoptosis and/or as a modulator of cell growth.Type: GrantFiled: March 3, 2006Date of Patent: October 4, 2011Assignee: Sterix LimitedInventors: Barry Victor Lloyd Potter, Michael John Reed, Lok Wai Lawrence Woo, Hatem Hejaz, Bertrand Leblond, Matthew Paul Leese, Atul Purohit
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Patent number: 8026229Abstract: The present invention relates to the use of 2-alkoxyestrogen sulfamates of general formula I wherein R1 and R2 independently represent H, methyl, C1-C4 acyl, benzoyl R3 represents C1-C4 alkyl or a group of formula CnFmHo, wherein n=1, 2, 3, 4, 5 or 6, m>1, and m+o=2n+1, R4 and R5 in each case represent H or, together, a methylene group or an additional double bond, R6 represents H, R7 represents OH, OC1-C4-alkyl, OC1-C11-acyl or OSO2NR1R2, the dashed lines in the B and C rings of the steroid skeleton additionally representing up to two double bonds, for the production of a medical drug for the treatment of tumor diseases which can be affected positively by inhibiting the tubulin polymerization. The inventive compounds are distinguished by the 2-alkoxy substitution in conjunction with the 17-hydroxy substitution. They have a special effect with regard to inhibiting tubulin polymerization and can be used, for example, for the treatment of prostate cancers.Type: GrantFiled: August 13, 2002Date of Patent: September 27, 2011Assignee: Sterix LimitedInventors: Ina Scherlitz-Hofmann, Jens Hoffmann, Alexander Hillisch, Eberhard Unger, Tobias Neumann, Sigfrid Schwarz, Olaf Peters, Thomas Michel
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Publication number: 20110118225Abstract: 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: ApplicationFiled: May 5, 2009Publication date: May 19, 2011Inventors: Petr Novak, David Sedlak, Petr Bartunek, Martin Kotora
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Patent number: 7910756Abstract: 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: GrantFiled: August 1, 2005Date of Patent: March 22, 2011Assignee: N.V. OrganonInventors: Johannes Stoelwinder, Nicolaas Elisabeth Cornelis Moers
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Patent number: 7893284Abstract: The present invention provides a compound comprising a steroidal ring system and an optional group R1 selected from any one of —OH, a sulphamate group, a phosphonate group, a thiophosphonate group, a sulphonate group or a sulphonamide group; wherein the D ring of the steroidal ring system is substituted by a group R2 of the formula -L-R3, wherein L is an optional linker group and R3 is selected from groups which are or which comprise one of a nitrite group, an alcohol, an ester, an ether, an amine and an alkene, provided that when R3 is or comprises an alcohol, L is present; and wherein the A ring of the steroidal ring system is substituted at position 2 or 4 with a group R4, wherein R4 is a hydrocarbyl group.Type: GrantFiled: September 23, 2005Date of Patent: February 22, 2011Assignee: Sterix LimitedInventors: Matthew Leese, Atul Purohit, Michael John Reed, Simon Paul Newman, Surinder Kuman Chander, Fabrice Jourdan, Barry Victor Lloyd Potter
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Publication number: 20110021480Abstract: 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: ApplicationFiled: September 28, 2010Publication date: January 27, 2011Applicant: Solvay Pharmaceuticals GmbHInventors: Josef Messinger, Heinrich-Hubert Thole, Bettina Husen, Michael Weske, Pasi Koskimies, Lila Pirkkala
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Publication number: 20100317628Abstract: 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: ApplicationFiled: February 20, 2009Publication date: December 16, 2010Inventors: Qihong Huang, Alexander Deiters, Kiranmai Gumireddy
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Publication number: 20100197647Abstract: Disclosed and claimed are compounds suitable for use as an inhibitor of oestrone sulphatase in a subject in need thereof, as well as compositions containing such compounds and methods for using such compounds.Type: ApplicationFiled: December 1, 2009Publication date: August 5, 2010Inventors: Michael John REED, Barry Victor Lloyd POTTER
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Publication number: 20100174101Abstract: The present invention provides a novel multi-step process for the manufacturing Fulvestrant, which is economical and convenient to operate at commercial scale, and requires only simple chromatographic separations after the coupling step of adding the side chain to the 7 position of the steroid.Type: ApplicationFiled: September 24, 2007Publication date: July 8, 2010Applicant: XI'AN LIBAND PHARMACEUTICAL CO., LTD.Inventors: Suoding Cao, Yuanlin Zhou, Yaping Shen, Tao Chen
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Publication number: 20100105934Abstract: A compound of formula (1) wherein R1 represents hydrogen or an acetyl group and R2 represents a methyl, acetyl, or benzyl group, is useful as an intermediate in making fulvestrant. The compound (1) can be isolated as a crystalline material and can be provided in a ratio of 7-alpha epimer to 7-beta epimer in the range of 95:5 to 100:0.Type: ApplicationFiled: October 15, 2009Publication date: April 29, 2010Inventors: Gerrit J. B. Ettema, Reinerus G. Gieling
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Patent number: 7687486Abstract: Compositions and methods for treating a cancer in mammals by administering selective estrogen receptor modulators particularly compounds represented by: or any other of the structures contained herein, or of a stereoisomer, enantiomer, rotomer, tautomer or pharmaceutically acceptable salt form thereof.Type: GrantFiled: March 5, 2005Date of Patent: March 30, 2010Assignee: Florida Agricultural & Mechanical UniversityInventor: John S. Cooperwood
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Publication number: 20090318721Abstract: Processes useful in the preparation of pharmaceutical compounds such as fulvestrant and processes for the preparation of fulvestrant.Type: ApplicationFiled: August 12, 2009Publication date: December 24, 2009Inventors: Peter Lindsay MacDonald, Ettore Bigatti, Pierluigi Rossetto
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Publication number: 20090306417Abstract: Processes useful in the preparation of pharmaceutical compounds such as fulvestrant and processes for the preparation of fulvestrant.Type: ApplicationFiled: August 12, 2009Publication date: December 10, 2009Inventors: Peter Lindsay MacDonald, Ettore Bigatti, Pierluigi Rossetto
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Publication number: 20090197842Abstract: 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: ApplicationFiled: September 26, 2006Publication date: August 6, 2009Inventor: Tsutomu Tanabe
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Patent number: 7538100Abstract: The invention relates to 17?-alkyl-17?-oxy-estra-1,3,5(10)-trienes that have an antiestrogenic action with general formula I. In addition, the invention also relates to 17-oxo-estra-1,3,5(10)-trienes as well as 17?-hydroxy-estra-1,3,5(10)-trienes as intermediate products in the production of the estratrienes according to the invention. The invention also relates to the use of 17?-alkyl-17?-oxy-estratrienes for the production of pharmaceutical agents as well as pharmaceutical preparations that contain at least one 17?-alkyl-17?-oxy-estratriene as well as at least one pharmaceutically compatible vehicle.Type: GrantFiled: July 26, 2005Date of Patent: May 26, 2009Assignee: Bayer Schering Pharma AktiengesellschaftInventors: Rolf Bohlmann, Nikolaus Heinrich, Rolf Jautelat, Jorg Kroll, Orlin Petrov, Andreas Reichel, Jens Hoffmann, Rosemarie Lichtner
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Patent number: 7534780Abstract: The invention relates to estradiol prodrugs of general formula (I), in which group Z is bonded to the steroid, process for their production, pharmaceutical compositions that contain these compounds, as well as their use for the production of pharmaceutical agents with estrogenic action.Type: GrantFiled: May 20, 2005Date of Patent: May 19, 2009Assignee: Bayer Schering Pharma AktiengesellschaftInventors: Ralf Wyrwa, Sven Ring, Peter Droescher, Alexander Hillisch, Walter Elger, Birgitt Schneider, Gudrun Reddersen
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Publication number: 20090118164Abstract: 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: ApplicationFiled: February 22, 2008Publication date: May 7, 2009Inventors: William M. Pierce, JR., K. Grant Taylor, Leonard C. Waite
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Patent number: 7507725Abstract: 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: GrantFiled: May 8, 2001Date of Patent: March 24, 2009Assignee: Schering AGInventors: Walter Elger, Alexander Hillisch, Annemarie Hedden, Sigfrid Schwarz, Klaus Schollkopf
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Patent number: 7427610Abstract: Disclosed are compounds of formula I and use thereof in a method of treating a tumor disease that can be influenced positively by the inhibition of tubulin polymerization.Type: GrantFiled: February 19, 2004Date of Patent: September 23, 2008Assignee: Sterix LimitedInventors: Alexander Hillisch, Olaf Peters, Christian Gege, Wilko Regenhardt, Dirk Kosemund, Gerhard Siemeister, Eberhard Unger, Ulrich Bothe
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Publication number: 20080194533Abstract: The present invention relates to processes for selective sulfation of an aromatic hydroxyl group over an aliphatic hydroxyl group where both are present in the same molecule. This invention also relates to processes for selective sulfation of the aromatic hydroxyl group of equilin, equilenin, estradiol, estra(1,3,5-triene)-3,16,17-triol, dihydroequilenin or dihydroequilin. This invention further relates to alkali metal salts of dihydroequilenin sulfates, dihydroequilin sulfates, estradiol sulfates, and estriol sulfates, processes for making thereof, stable compositions comprising thereof, and the use thereof.Type: ApplicationFiled: February 7, 2008Publication date: August 14, 2008Applicant: WYETHInventors: Sreenivasulu MEGATI, Panolil RAVEENDRANATH, Girija Raveendranath, Vijay Raveendranath, Sanjay Raveendranath
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Patent number: 7381718Abstract: A process for the preparation of compounds of formula (I) in which R1, R2, R3 and n are defined as indicated in the description, use of said compounds as intermediates for the preparation of estrogen derivatives as well as the intermediates of this process.Type: GrantFiled: June 12, 2002Date of Patent: June 3, 2008Assignee: Aventis Pharma S.A.Inventors: Francoise Benedetti, Alain Mazurie, Francois Nique, Denis Prat, Christian Wehrey
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Patent number: 7378404Abstract: 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: GrantFiled: April 12, 2001Date of Patent: May 27, 2008Assignee: Schering AktiengesellschaftInventors: Olaf Peters, Alexander Hillisch, Ina Thieme, Walter Elger, Christa Hegele-Hartung, Uwe Kollenkirchen, Karl-Heinrich Fritzemeier, Vladimir Patchev
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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: 7371741Abstract: 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: GrantFiled: May 28, 2004Date of Patent: May 13, 2008Assignee: EntreMed, Inc.Inventors: Gregory E. Agoston, Theresa M. LaVallee, Victor S. Pribluda, Jamshed H. Shah, Anthony M. Treston
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Patent number: 7119081Abstract: There is provided a compound of Formula I wherein X is a ring system; R1 is any one of a sulphamate group, a phosphonate group, a thiophosphonate group, a sulphonate group or a sulphonamide group; R2 is any one of a sulphamate group, a phosphonate group, a thiophosphonate group, a sulphonate group or a sulphonamide group; wherein when X is a steroidal structure and both of R1 and R2 are sulphamate groups, the steroidal ring system (X) represents an oestrogen; and wherein said compound is capable of inhibiting steroid sulphatase (STS) activity and/or is capable of acting as a modulator of cell cycling and/or as a modulator of apoptosis and/or as a modulator of cell growth.Type: GrantFiled: February 14, 2003Date of Patent: October 10, 2006Assignee: Sterix LimitedInventors: Barry Victor Lloyd Potter, Michael John Reed, Bertrand Leblond, Matthew Paul Leese, Atul Purohit
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Patent number: 7109360Abstract: 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: GrantFiled: February 4, 2000Date of Patent: September 19, 2006Assignee: Schering AGInventors: Hermann Kuenzer, Rudolf Knauthe, Monika Lessl, Karl-Heinrich Fritzemeier, Christa Hegele-Hartung, Ulf Boemer, Gerd Mueller, Dirk Kosemund
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Patent number: 7067683Abstract: This invention describes a safe method for the production of sulfamoyl chloride from chlorosulfonyl isocyanate and formic acid in the presence of a amide catalyst, taming the hazardous nature of this reaction by circumventing heat accumulation processes, as well as the sulfamoylation of alcohols and phenols with the resulting sulfamoyl chloride in N,N-dimethyl acetamide or N-methyl pyrrolidone thereby avoiding the formation of side-products which were inevitable with the methods of the prior art using dimethyl formamide or dichloromethane as a solvent. The current invention allows industrial scale applications and describes as an example the process of manufacture of the biologically active compound 17?-Hydroxyestra-1,3,5(10)-triene-3-yl sulfamate.Type: GrantFiled: December 23, 2002Date of Patent: June 27, 2006Assignee: Schering AGInventors: Jens Geisler, Frank Schneider, Fernando Lopez Holguin, Kai Lovis
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Patent number: 7018994Abstract: The invention relates to 17?-alkyl-17?-oxy-estra-1,3,5(10)-trienes that have an antiestrogenic action with general formula I. In addition, the invention also relates to 17-oxo-estra-1,3,5(10)-trienes as well as 17?-hydroxy-estra-1,3,5(10)-trienes as intermediate products in the production of the estratrienes according to the invention. The invention also relates to the use of 17?-alkyl-17?-oxy-estratrienes for the production of pharmaceutical agents as well as pharmaceutical preparations that contain at least one 17?-alkyl-17?-oxy-estratriene as well as at least one pharmaceutically compatible vehicle.Type: GrantFiled: November 27, 2002Date of Patent: March 28, 2006Assignee: Schering AGInventors: Rolf Bohlmann, Nikolaus Heinrich, Rolf Jautelat, Jorg Kroll, Orlin Petrov, Andreas Reichel, Jens Hoffmann, Rosemarie Lichtner
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Patent number: 6995278Abstract: 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: GrantFiled: February 8, 2001Date of Patent: February 7, 2006Assignee: Entre Med, Inc.Inventors: Gregory E. Agoston, Victor Pribluda, Anthony M. Treston, Shawn J. Green
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Patent number: 6903084Abstract: A method of inhibiting steroid sulphatase activity in a subject in need of same is described. The method comprises administering to said subject a steroid sulphatase inhibiting amount of a ring system compound; which ring system compound comprises a ring to which is attached a sulphamate group of the formula wherein each of R1 and R2 is independently selected from H, alkyl, alkenyl, cycloalkyl and aryl, or together represent allylene optionally containing one or more hetero atoms or groups in the alkylene chain; and wherein said compound is an inhibitor of an enzyme having steroid sulphatase activity (E.C.3.1.6.2); and if the sulphamate group of said compound is replaced with a sulphate group to form a sulphate compound and incubated with a steroid sulphatase enzyme (E.C.3.1.6.2) at a pH 7.4 and 37° C. it would provide a Km value of less than 50 ?M.Type: GrantFiled: February 27, 2001Date of Patent: June 7, 2005Assignee: Sterix LimitedInventors: Michael John Reed, Barry Victor Lloyd Potter
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Patent number: 6858597Abstract: A compound is described. The compound has the formula (Ia) as presented in the FIG. 1; wherein: X is a ring having at least 4 atoms in the ring; K is hydrocarbyl group; Rh1 is an optional halo group; Rh2 is an optional halo group; at least one of Rh1 and Rh2 is present; Rs is any one of a sulphamate group, a phosphonate group, a thiophosphonate group, a sulphonate group or a sulphonamide group. The compound is capable of inhibiting steroid sulphatase (STS) activity.Type: GrantFiled: June 7, 2002Date of Patent: February 22, 2005Assignee: Sterix LimitedInventors: Michael John Reed, Barry Victor Lloyd Potter, Hatem Hejaz, Atul Purohit
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Publication number: 20040229853Abstract: The subject of the invention is a method for preparing compounds of general formula (I): 1Type: ApplicationFiled: April 29, 2004Publication date: November 18, 2004Applicant: Aventis Pharma S.A.Inventors: Denis Prat, Christian Moratille, Francoise Benedetti, Lahlou Nait-Bouda
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Patent number: 6794409Abstract: The present invention discloses the use of ER&bgr;-selective ligands for production of medicaments for regulating fertility without additional use of a progestin. ER&bgr;-agonists are used for treatment of infertility and ER&bgr;-antagonists for contraception.Type: GrantFiled: February 27, 2002Date of Patent: September 21, 2004Assignee: Schering AGInventors: Christa Hegele-Hartung, Karl-Heinrich Fritzemeier, Hiroshi Yamanouchi, Olaf Peters, Dirk Kosemund, Gerd Mueller, Ingo Tornus, Gerd Schubert, Sven Ring
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Patent number: 6790842Abstract: This invention describes a 11&bgr;-long-chain-substituted estratriene of general formula (I), in which R11 is a long-chain radical that has a nitrogen atom and optionally a sulfur atom, which in addition can be functionalized in the terminal position with a perfluoroalkyl group or an optionally substituted arly radical. The compound can have antiestrogenic or tissue-selective estrogenic properties and be suitable for the production of pharmaceutical agents.Type: GrantFiled: May 7, 2002Date of Patent: September 14, 2004Assignee: Schering AktiengesellschaftInventors: Rolf Bohlmann, Nikolaus Heinrich, Jorg Kroll, Gerhard Sauer, Karl-Heinrich Fritzemeier, Christa Hegele-Hartung, Jens Hoffmann, Rosemarie Lichtner, Ludwig Zorn
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Publication number: 20040171595Abstract: A process for the preparation of compounds of formula (I) 1Type: ApplicationFiled: January 12, 2004Publication date: September 2, 2004Inventors: Francoise Benedetti, Alain Mazurie, Francois Nique, Denis Prat, Christian Wehrey
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Patent number: 6780855Abstract: 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: GrantFiled: December 2, 1999Date of Patent: August 24, 2004Assignee: Schering AktiengesellschaftInventors: 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
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Publication number: 20040127473Abstract: Disclosed and claimed are compounds suitable for use as an inhibitor of oestrone sulphatase in a subject in need thereof, as well as compositions containing such compounds and methods for using such compounds.Type: ApplicationFiled: September 30, 2003Publication date: July 1, 2004Inventors: Michael John Reed, Barry Victor Lloyd Potter
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Publication number: 20040043972Abstract: 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-mType: ApplicationFiled: April 28, 2003Publication date: March 4, 2004Inventors: Plate R. Ralf, Bagchus W.M. Wilhelmina Maria
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Patent number: 6693090Abstract: A compound selected from the group consisting of a compound of the formula wherein the substituents are defined as set forth in the specification which compounds are useful for the treatment of osteoporosis.Type: GrantFiled: April 10, 2002Date of Patent: February 17, 2004Assignee: Aventis Pharma S.A.Inventor: Francois Nique