Two Oxygens Bonded Directly To The Cyclopentanohydrophenanthrene Ring System Patents (Class 552/623)
  • Patent number: 5994568
    Abstract: The invention relates to estrene steroids, which bind to neuroepithelial receptors. The steroid is preferably administered in the form of a pharmaceutical composition containing one or more pharmaceutically acceptable carriers.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: November 30, 1999
    Assignee: Pherin Corporation
    Inventors: David L. Berliner, Nathan W. Adams, Clive L. Jennings-White
  • Patent number: 5986115
    Abstract: This invention describes new, substituted 7.alpha.-(.xi.-aminoalkyl)-estratrienes of general formula I ##STR1## in which side chain SK is a radical of partial formula ##STR2## as well as their physiologically compatible addition salts with organic and inorganic acids.The new compounds represent compounds with very strong antiestrogenic action.The compounds according to the invention are, on the one hand, pure antiestrogens, or, on the other hand, antiestrogens with estrogenic partial action. Based on this spectrum of action, the new compounds are highly suitable for the production of pharmaceutical agents for tumor therapy and hormone replacement treatment.
    Type: Grant
    Filed: January 28, 1999
    Date of Patent: November 16, 1999
    Assignee: Schering AG
    Inventors: Rolf Bohlmann, Dieter Bittler, Josef Heindl, Nikolaus Heinrich, Helmut Hofmeister, Hermann Kunzer, Gerhard Sauer, Christa Hegele-Hartung, Rosemarie Lichtner, Yukishige Nishino, Karsten Parczyk, Martin Schneider
  • 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: 5429934
    Abstract: 20 -Methyl-5,7-pregnadiene-3.beta.,21-diol derivatives of general formula I ##STR1## in which R.sub.1 means a hydrogen atom or a lower alkyl group andR.sub.2 means a lower alkyl group orR.sub.1 and R.sub.2 together represent a tetramethylene group or a pentamethylene group and a process for their production are described.
    Type: Grant
    Filed: June 18, 1992
    Date of Patent: July 4, 1995
    Assignee: Schering Aktiengesellschaft
    Inventors: Alfred Weber, Mario Kennekke, Gunter Neef
  • 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: 5364847
    Abstract: Certain steroidal and non-steroidal compounds have been found to inhibit androgen and estrogen formation. Such inhibition may aid in the reduction of the activity of these hormones and may be useful in the treatment of diseases where, for example, inhibition of androgen or estrogen acitivity is desired. Preferred inhibitors also possess antiestrogenic activity, thus providing the advantage of a double inhibitory action both on estrogen formation and on estrogen action.
    Type: Grant
    Filed: October 22, 1992
    Date of Patent: November 15, 1994
    Assignee: Endorecherche
    Inventors: Fernand Labrie, Yves Merand
  • Patent number: 5208263
    Abstract: Disclosed are novel classes of anti-androgen including dihydrophenanthrene derivatives, their method of synthesis and their use in treating disorders associated with excessive androgenic activities.
    Type: Grant
    Filed: September 27, 1989
    Date of Patent: May 4, 1993
    Assignee: Arch Development Corporation
    Inventors: Shutsung Liao, John Pataki, Ronald G. Harvey
  • Patent number: 5182381
    Abstract: Novel 3-keto-19-nor-.DELTA..sup.4,9 -steroids of the formula ##STR1## and their non-toxic, pharmaceutically acceptable acid addition salts possessing a remarkable antiglucocorticoidal activity.
    Type: Grant
    Filed: September 10, 1991
    Date of Patent: January 26, 1993
    Assignee: Roussel Ulcaf
    Inventors: Daniel Philibert, Jean G. Teutsch, Germain Costerousse, Roger Deraedt
  • Patent number: 5132299
    Abstract: New 11.beta. phenyl-4,9,15-estratrienes of formula I ##STR1## are described, where X implies an oxygen atom or a hydroxyimino grouping N.about.OH,R.sup.1 stands for a hydrogen atom or a methyl group,R.sup.2 implies a hydrogen atom, an alkyl radical or an acyl radical with in each case 1 to 10 carbon atoms,R.sup.3 stands for a hydrogen atom, a cyanomethyl group, --(CH.sub.2).sub.n CH.sub.2 Z where n implies the numbers 0, 1, 2, 3, 4 or 5, Z=--H or --OR.sup.5 with R.sup.5 having the significance of a hydrogen atom or an alkyl or acyl group with in each case 1 to 10 carbon atoms, or for --(CH.sub.2).sub.m --C.tbd.C--Y where m=0-2 and Y implies a hydrogen, chlorine, fluorine, iodine or bromine atom, an alkyl, hydroxyalkyl, alkoxyalkyl or acyloxyalkyl group with in each case 1 to 10 carbon atoms,R.sup.4 represents a straight-chain or branched-chain, saturated or unsaturated hydrocarbon radical with up to 8 carbon atoms which contains the grouping ##STR2## with X having the above significance.
    Type: Grant
    Filed: January 16, 1990
    Date of Patent: July 21, 1992
    Assignee: Schering Aktiengesellschaft
    Inventors: Eckhard Ottow, Helmut Hofmeister, Stefan Scholz, Guenter Neef, Walter Elger, Sybille Beier, Krzysztof Chwalisz
  • Patent number: 5086190
    Abstract: The present invention provides a novel compound represented as ##STR1## The present novel compound is prepared by reacting fluorine with pyridine-boron trifluoride and is useful as a fluorinating agent in the fluorination of organic compounds.
    Type: Grant
    Filed: January 29, 1991
    Date of Patent: February 4, 1992
    Assignee: Allied-Signal Inc.
    Inventors: Michael Van Der Puy, David Nalewajek, George A. Shia, William J. Wagner