Oxygen Bonded Directly At The 16-position Patents (Class 552/624)
  • Patent number: 9315455
    Abstract: 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: Grant
    Filed: January 24, 2011
    Date of Patent: April 19, 2016
    Assignee: HYBRIGENICS SA
    Inventors: Jean-Luc Moutou, Florent Mouton, Gilles Pellegrino, Jean Lafay
  • 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: 20130072464
    Abstract: 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: Application
    Filed: February 8, 2011
    Publication date: March 21, 2013
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Wolfgang Schwede, Ulrich Klar, Carsten Möller, Andrea Rotgeri, Wilhelm Bone, Christoph Huwe
  • Patent number: 8071575
    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: Grant
    Filed: February 22, 2008
    Date of Patent: December 6, 2011
    Assignee: University of Louisville Research Foundation
    Inventors: William M. Pierce, Jr., K. Grant Taylor, Leonard C. Waite
  • Publication number: 20110178052
    Abstract: 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: Application
    Filed: July 9, 2009
    Publication date: July 21, 2011
    Applicant: Bayer Schering Pharma Aktiengesellschaft
    Inventors: Karl-Heinrich Fritzemeier, Patrick Diel, Torsten Hertrampf
  • Patent number: 7414043
    Abstract: 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: Grant
    Filed: June 11, 2003
    Date of Patent: August 19, 2008
    Assignee: Schering AG
    Inventors: Dirk Kosemund, Gerd Mueller, Alexander Hillisch, Karl-Heinrich Fritzemeier, Peter Muhn
  • Publication number: 20030114431
    Abstract: 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: Application
    Filed: August 26, 2002
    Publication date: June 19, 2003
    Inventor: Michael P. Girouard
  • Patent number: 5892069
    Abstract: The application discloses methods of treating mammalian diseases characterized by abnormal cell mitosis by administering estradiol derivatives including those comprising colchicine or combretastatin A-4 structural motifs of the general formulae found below in a dosage sufficient to inhibit cell mitosis. The application discloses novel compounds used in the methods.
    Type: Grant
    Filed: April 25, 1997
    Date of Patent: April 6, 1999
    Assignee: The Children's Medical Center Corporation
    Inventors: Robert John D'Amato, Moses Judah Folkman
  • Patent number: 5804576
    Abstract: 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: Grant
    Filed: June 6, 1995
    Date of Patent: September 8, 1998
    Assignee: Research Corporation Technologies, Inc.
    Inventors: Arthur G. Schwartz, John R. Williams, Magid Abou-Gharbia, Ann R. Swern, Marvin Louis Lewbart
  • Patent number: 5739302
    Abstract: 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: Grant
    Filed: October 5, 1994
    Date of Patent: April 14, 1998
    Assignee: Institute of Applied Biochemistry
    Inventors: Takehiko Suzuki, Sadaaki Komura, Naoko Ishida, Nobuko Ohishi, Kunio Yagi
  • Patent number: 5714481
    Abstract: 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: Grant
    Filed: May 31, 1995
    Date of Patent: February 3, 1998
    Assignee: Research Corporation Technologies, Inc.
    Inventors: Arthur G. Schwartz, John R. Williams, Magid Abou-Gharbia, Daniel Swern, deceased, Marvin Louis Lewbart
  • Patent number: 5705495
    Abstract: The invention relates to new sulfamate derivatives of 1,3,5(10)-estratriene derivatives of the general formula I ##STR1## wherein the 3-sulfamate moiety is acylated, sulfonated or amidosulfonated. Furthermore, methods for the production of the compound and pharmaceutical preparations containing this compound are described. The compounds according to the invention have an estrogenic effect.
    Type: Grant
    Filed: October 18, 1996
    Date of Patent: January 6, 1998
    Assignee: Jenapharm GmbH & Co. KG.
    Inventors: Sigfrid Schwarz, Walter Elger, Gudrun Reddersen, Birgitt Schneider, Ina Thieme, Margit Richter
  • Patent number: 5700793
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: December 23, 1997
    Assignee: Research Corporation Technologies, Inc.
    Inventors: Arthur G. Schwartz, Marvin Louis Lewbart
  • Patent number: 5597701
    Abstract: 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: Grant
    Filed: March 7, 1995
    Date of Patent: January 28, 1997
    Assignee: Riedel-De Haen Aktiengesellschaft
    Inventors: Rolf P. Claus, Martin Dehnhard
  • Patent number: 5405944
    Abstract: 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: Grant
    Filed: September 25, 1992
    Date of Patent: April 11, 1995
    Assignee: Institute of Applied Biochemistry
    Inventors: Takehiko Suzuki, Sadaaki Komura, Naoko Ishida, Nobuko Ohishi, Kunio Yagi
  • Patent number: 5157031
    Type: Grant
    Filed: March 21, 1989
    Date of Patent: October 20, 1992
    Assignee: Research Corporation Technologies, Inc.
    Inventors: Arthur G. Schwartz, Marvin L. Lewbart