Oxygen Bonded Directly At The 16-position Patents (Class 552/624)
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Patent number: 9315455Abstract: The present invention concerns a process of isomerizing trans fused bicyclic derivatives into cis fused bicyclic derivatives and the preparation of vitamin D or analogs thereof comprising said isomerization step.Type: GrantFiled: January 24, 2011Date of Patent: April 19, 2016Assignee: HYBRIGENICS SAInventors: Jean-Luc Moutou, Florent Mouton, Gilles Pellegrino, Jean Lafay
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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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Publication number: 20130072464Abstract: The invention relates to 17-hydroxy-17-pentafluoroethyl-estra-4,9(10)-dien-11-aryl derivatives of formula I with progesterone-antagonizing action and methods of production thereof, use thereof for the treatment and/or prevention of diseases and use thereof for producing medicinal products for the treatment and/or prevention of diseases, in particular uterine fibroids (myomata, uterine leiomyomata), endometriosis, heavy menstrual bleeding, meningiomata, hormone-dependent breast cancers and menopause-associated complaints or for fertility control and emergency contraception.Type: ApplicationFiled: February 8, 2011Publication date: March 21, 2013Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Wolfgang Schwede, Ulrich Klar, Carsten Möller, Andrea Rotgeri, Wilhelm Bone, Christoph Huwe
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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: 20110178052Abstract: Use of 9?-estra-1,3,5(10)-triene derivatives of formula (I) for the prevention and treatment of intestinal cancer, in particular adenoma and adenocarcinoma of the duodenum, ileum, colon, and rectum.Type: ApplicationFiled: July 9, 2009Publication date: July 21, 2011Applicant: Bayer Schering Pharma AktiengesellschaftInventors: Karl-Heinrich Fritzemeier, Patrick Diel, Torsten Hertrampf
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Patent number: 7414043Abstract: This invention describes the new 9?-substituted estratrienes of general formula I in which R3, R7, R7?, R13, R16 as well as R17 and R17? have the meanings that are indicated in the description and R9 means a straight-chain or branched-chain, optionally partially or completely halogenated alkenyl radical with 2 to 6 carbon atoms, an ethinyl or prop-1-inyl radical, as pharmaceutical active ingredients that exhibit in vitro a higher affinity to estrogen receptor preparations from rat prostates than to estrogen receptor preparations from rat uteri and in vivo preferably a preferential action on the ovary in comparison to the uterus, their production, their therapeutic use and pharmaceutical dispensing forms that contain the new compounds. The invention also describes the use of these compounds for treating estrogen-deficiency-induced diseases and conditions.Type: GrantFiled: June 11, 2003Date of Patent: August 19, 2008Assignee: Schering AGInventors: Dirk Kosemund, Gerd Mueller, Alexander Hillisch, Karl-Heinrich Fritzemeier, Peter Muhn
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Publication number: 20030114431Abstract: The pharmaceutical and/or cosmetic compositions for treatment of obesity and/or overweight contain an effective amount of a fatty-acid monoester of an estrogen and a fatty acid wherein the estrogen is preferably estrone, diethylstilbestrol, estriol, estradiol or ethinyl estradiol and the fatty acid is 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. In addition, synthesized combination molecules formed when a monounsaturated fatty acid of 20 carbon atoms or more is joined via an ester, ether, or amide bond to either a steroid or any molecule containing a perhydrocyclopentanophenanthrene nucleus or perhydrocyclopentanophenanthrene nucleus derivative are also included in this invention.Type: ApplicationFiled: August 26, 2002Publication date: June 19, 2003Inventor: Michael P. Girouard
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Patent number: 5892069Abstract: 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: GrantFiled: April 25, 1997Date of Patent: April 6, 1999Assignee: The Children's Medical Center CorporationInventors: Robert John D'Amato, Moses Judah Folkman
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Patent number: 5804576Abstract: Steroids of the formula: ##STR1## useful as cancer preventive agents, anti-obesity agents, anti-hyperglycemic agents, anti-aging agents, and anti-hypercholesterolemic agents and anti-auto-immune agents.Type: GrantFiled: June 6, 1995Date of Patent: September 8, 1998Assignee: Research Corporation Technologies, Inc.Inventors: Arthur G. Schwartz, John R. Williams, Magid Abou-Gharbia, Ann R. Swern, Marvin Louis Lewbart
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Patent number: 5739302Abstract: There are described novel glycosides of catechol estrogen, a method of preparing the same, and a medicament comprising one of the glycosides as an active ingredient. The glycosides are shown by the formula of ##STR1## wherein X is carbonyl group or ##STR2## R.sub.10 is hydroxyl group or glycosyloxy group, and R.sub.2 is a hydrogen atom or ethynyl group; R.sub.11 is a hydrogen atom, hydroxyl group, or glycosyloxy group; R.sub.12 is hydroxyl group or glycosyloxy group; and R.sub.13 is hydroxyl group or glycosyloxy group, in which glycosyloxy group is selected from the group consisting of glycosyloxy, galactosyloxy, mannosyloxy, arabinosyloxy, ribosyloxy, xylosyloxy, fructosyloxy, rhamnosyloxy, fucosyloxy, maltosyloxy, cellobiosyloxy, lactosyloxy, sucrosyloxy, maltotriosyloxy, maltotetraosyloxy, maltopentaosyloxy, maltohexaosyloxy, maltoheptaosyloxy, and sialosyloxy, and in this case, at least one of R.sub.10, R.sub.11, R.sub.12, and R.sub.13 is glycosyloxy group as defined above.Type: GrantFiled: October 5, 1994Date of Patent: April 14, 1998Assignee: Institute of Applied BiochemistryInventors: Takehiko Suzuki, Sadaaki Komura, Naoko Ishida, Nobuko Ohishi, Kunio Yagi
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Patent number: 5714481Abstract: Steroids of the formula: ##STR1## useful as cancer preventive agents, anti-obesity agents, anti-hyperglycemic agents, anti-aging agents, and anti-hypercholesterolemic agents and anti-auto-immune agents.Type: GrantFiled: May 31, 1995Date of Patent: February 3, 1998Assignee: Research Corporation Technologies, Inc.Inventors: Arthur G. Schwartz, John R. Williams, Magid Abou-Gharbia, Daniel Swern, deceased, Marvin Louis Lewbart
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Patent number: 5705495Abstract: 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: GrantFiled: October 18, 1996Date of Patent: January 6, 1998Assignee: Jenapharm GmbH & Co. KG.Inventors: Sigfrid Schwarz, Walter Elger, Gudrun Reddersen, Birgitt Schneider, Ina Thieme, Margit Richter
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Patent number: 5700793Type: GrantFiled: June 7, 1995Date of Patent: December 23, 1997Assignee: Research Corporation Technologies, Inc.Inventors: Arthur G. Schwartz, Marvin Louis Lewbart
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Patent number: 5597701Abstract: A process and appropriate device are disclosed for determining the androstenone content of adipose tissues in clearly shorter times. The disclosed process has the following steps: (a) liquefying an adipose tissue sample by heating up to a predetermined temperature in the 45.degree. to 60.degree. C.Type: GrantFiled: March 7, 1995Date of Patent: January 28, 1997Assignee: Riedel-De Haen AktiengesellschaftInventors: Rolf P. Claus, Martin Dehnhard
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Patent number: 5405944Abstract: There are described novel glycosides of catechol estrogen, a method of preparing the same, and a medicament comprising one of the glycosides as an active ingredient. The glycosides are shown by the formula of ##STR1## wherein X is carbonyl group or ##STR2## R.sub.10 is hydroxyl group or glycosyloxy group, and R.sub.2 is a hydrogen atom or ethynyl group; R.sub.11 is a hydrogen atom, hydroxyl group, or glycosyloxy group; R.sub.12 is hydroxyl group or glycosyloxy group; and R.sub.13 is hydroxyl group or glycosyloxy group,in which glycosyloxy group is selected from the group consisting of glucosyloxy, galactosyloxy, mannosyloxy, arabinosyloxy, ribosyloxy, xylosyloxy, fructosyloxy, rhamnosyloxy, fucosyloxy, maltosyloxy, cellobiosyloxy, lactosyloxy, sucrosyloxy, maltotriosyloxy, maltotetraosyloxy, maltopentaosyloxy, maltohexaosyloxy, maltoheptaosyloxy, and sialosyloxy, and in this case, at least one of R.sub.10, R.sub.11, R.sub.12, and R.sub.13 is glycosyloxy group as defined above.Type: GrantFiled: September 25, 1992Date of Patent: April 11, 1995Assignee: Institute of Applied BiochemistryInventors: Takehiko Suzuki, Sadaaki Komura, Naoko Ishida, Nobuko Ohishi, Kunio Yagi
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Patent number: 5157031Type: GrantFiled: March 21, 1989Date of Patent: October 20, 1992Assignee: Research Corporation Technologies, Inc.Inventors: Arthur G. Schwartz, Marvin L. Lewbart