The Sulfur Is Bonded Directly At The 1- Or 3-position Patents (Class 552/524)
  • Patent number: 9464108
    Abstract: The present invention relates to a synthesis route and to steroid derivatives of general formula VI and VII useful in the synthesis of desogestrel and etonogestrel.
    Type: Grant
    Filed: March 13, 2013
    Date of Patent: October 11, 2016
    Assignee: Merck Sharp & Dohme B.V.
    Inventor: Martin Ostendorf
  • Publication number: 20150072962
    Abstract: 5-cholesten, 3?, 25-diol, disulfate (25HCDS) has been found to be an authentic PPAR? agonist and LXR antagonist, and is used for the therapy of lipid disorders and inflammatory diseases, including without limitation fatty liver, inflammatory bowel, and atherosclerotic diseases.
    Type: Application
    Filed: March 15, 2013
    Publication date: March 12, 2015
    Inventor: Shunlin Ren
  • Publication number: 20140288160
    Abstract: Disclosed herein are novel compounds, pharmaceutical compositions comprising such compounds and related methods of their use. The compounds described herein are useful, e.g., as liposomal delivery vehicles to facilitate the delivery of encapsulated polynucleotides to target cells and subsequent transfection of said target cells, and in certain embodiments are characterized as having one or more properties that afford such compounds advantages relative to other similarly classified lipids.
    Type: Application
    Filed: June 8, 2012
    Publication date: September 25, 2014
    Applicant: Shire Human Genetic Therapies, Inc.
    Inventors: Braydon Charles Guild, Michael Heartlein, Frank DeRosa, Jerry Chi Zhang
  • Patent number: 8569275
    Abstract: The invention relates to the use of compounds to ameliorate or treat an condition such as a cystic fibrosis, neutropenia or other exemplified conditions. Exemplary compounds that can be used include 3?-hydroxy-17?-aminoandrost-5-ene, 3?-hydroxy-16?-fluoro-17?-aminoandrost-5-ene, 3?-hydroxy-16?-fluoro-17?-aminoandrost-5-ene, 3?-hydroxy-16?-fluoro-17?-aminoandrost-5-ene, 1?,3?-dihydroxy-4?-fluoroandrost-5-ene-17-one, 1?,3?,17?-trihydroxy-4?-fluoroandrost-5-ene, 1?,3?-dihydroxy-6?-bromoandrost-5-ene, 1?-fluoro-3?,12?-dihydroxyandrost-5-ene-17-one, 1?-fluoro-3?,4?-dihydroxyandrost-5-ene and 4?-fluoro-3?,6?,17?-trihydroxyandrostane.
    Type: Grant
    Filed: April 27, 2011
    Date of Patent: October 29, 2013
    Assignee: Harbor Therapeutics, Inc.
    Inventor: James M. Frincke
  • Publication number: 20130102577
    Abstract: The present invention relates to SHIP inhibitor compounds and methods for using these compounds. In particular, the present invention discloses the following methods: (i) a method of treating graft versus host disease in a subject; (ii) a method of inhibiting a SHIP1 protein in a cell; (iii) a method of selectively inhibiting a SHIP1 protein in a cell; (iv) a method for treating or preventing graft-versus-host disease (GVHD) in a recipient of an organ or tissue transplant; (v) a method of modulating SHIP activity in a cell expressing SHIP1 or SHIP2; (vi) a method of ex vivo or in vitro treatment of transplants; (vii) a method of inhibiting tumor growth and metastasis in a subject; (viii) a method of treating a hematologic malignancy in a subject; (ix) a method of inducing apoptosis of multiple myeloma cells; (x) a method of treating multiple myeloma in a subject; (xi) a method of inhibiting the proliferation of a human breast cancer cell; and (xii) a method of treating breast cancer in a subject.
    Type: Application
    Filed: April 11, 2011
    Publication date: April 25, 2013
    Applicant: The Research Foundation of the State University of New York
    Inventors: William G. Kerr, John D. Chisholm
  • Publication number: 20020183283
    Abstract: Certain novel sterol derivatives can be used for regulating the meiosis in oocytes and in male germ cells.
    Type: Application
    Filed: June 4, 2002
    Publication date: December 5, 2002
    Inventors: Peter Faarup, Frederick Christian Gronvald, Thorsten Blume, Anthony Murray, Jens Breinholt
  • Publication number: 20010018435
    Abstract: A method of inhibiting steroid sulphatase activity in a subject in need of same is described.
    Type: Application
    Filed: February 27, 2001
    Publication date: August 30, 2001
    Applicant: STERIX LIMITED
    Inventors: Michael John Reed, Barry Victor Lloyd Potter
  • Patent number: 5942634
    Abstract: Cationic amphiphiles are provided that facilitate transport of biologically active (therapeutic) molecules into cells. There are provided also therapeutic compositions prepared typically by contacting a dispersion of one or more cationic amphiphiles with the therapeutic molecules. Therapeutic molecules that can be delivered into cells according to the practice of the invention include DNA, RNA, and polypeptides. Representative uses of the therapeutic compositions of the invention include providing gene therapy, and delivery of antisense polynucleotides or biologically active polypeptides to cells. With respect to therapeutic compositions for gene therapy, the DNA is provided typically in the form of a plasmid for complexing with the cationic amphiphile.
    Type: Grant
    Filed: May 9, 1997
    Date of Patent: August 24, 1999
    Assignee: Genzyme Corporation
    Inventors: Craig S. Siegel, Edward R. Lee, David J. Harris
  • Patent number: 5916975
    Abstract: A process for enantioselectively epoxidising a prochiral olefin, which process comprises reacting a prochiral olefin with a source of oxygen in the presence of a salen catalyst and a source of an electron donating ligand, characterized in that the donor ligand is isoquinoline N-oxide or a compound having donor ligand activity and having substantially the same solubility characteristics as isoquinoline N-oxide.
    Type: Grant
    Filed: August 5, 1996
    Date of Patent: June 29, 1999
    Assignee: SmithKline Beecham p.l.c.
    Inventors: David Bell, Frances Finney, Robin Patrick Attrill, David Miller, Gillian Turner
  • 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: 5646316
    Abstract: The present invention relates to a bile acid derivative, which comprises a bile acid derivatized at the carboxyl group with a hydroxamic acid or hydroxamate ester. The carboxyl group in the bile acid compound can also be derivatized with an amino acid or oligopeptide, whose C-terminus is derivatized with a hydroxamic acid or a hydroxamate ester. The present invention also relates to a method of use of a bile acid or a bile acid derivative to inhibit a metalloproteinase enzyme, comprising contacting a metalloproteinase with an effective amount of a bile acid or bile acid derivative. In another embodiment, the present invention further relates to a method of use of a bile acid or bile acid derivative to therapeutically treat a disease, which is ameliorated by inhibiting a metalloproteinase enzyme. In this method, a therapeutically effective amount of a bile acid, a bile acid derivative or physiologically acceptable salts thereof, is administered to a human or other mammal.
    Type: Grant
    Filed: April 25, 1995
    Date of Patent: July 8, 1997
    Assignee: OsteoArthritis Sciences, Inc.
    Inventors: Alan R. Jacobson, Douglas G. Gabler, Jozef Oleksyszyn
  • Patent number: 5637691
    Abstract: Compounds having a broad range of antimicrobial activity generally have a structure including asteroid nucleus with a cationic, preferably polyamine, side chain (X) and an anionic side chain (Y). The invention is also directed to compounds of the Formula III: ##STR1## preferably where the steroid ring nucleus is saturated; the steroid ring substituent Z.sub.5 is .alpha.-H; one Z.sub.7 is .beta.-H and the other is .alpha.-H or .alpha.-OH; both substituents Z.sub.12 are hydrogen; X' is a polyamine side chain of the formula --NH--(CH.sub.2).sub.p --NH--(CH.sub.2).sub.q --N(R.sup.II)(R.sup.III) where p and q are each independently 3 or 4, and R.sup.II and R.sup.III are each independently hydrogen or methyl; R' is methyl; and Y' is (C.sub.1 -C.sub.10)-alkyl substituted with a group such as --CO.sub.2 H or --SO.sub.3 H.
    Type: Grant
    Filed: August 18, 1994
    Date of Patent: June 10, 1997
    Assignee: Magainin Pharmaceuticals, Inc.
    Inventors: Leah L. Frye, Michael A. Zasloff, William A. Kinney, Robert Moriarty
  • Patent number: 5561124
    Abstract: The invention relates to substituted 17.alpha.-acyl steroidal 5.alpha.-reductase inhibiting compounds. The invention also relates to pharmaceutical compositions containing these compounds and their use for reducing prostate size and treating prostate adenocarcinoma. Further, the invention describes a process for making these compounds by heating the corresponding substituted 17.beta.-acyl steroid in a solvent, such as ethylene glycol or dimethyl sulfoxide (DMSO), in a base, such as sodium or potassium hydroxide.
    Type: Grant
    Filed: May 17, 1995
    Date of Patent: October 1, 1996
    Inventor: Robert L. Webb
  • Patent number: 5399685
    Abstract: A process for the preparation of a compound of the formula ##STR1## wherein R.sub.1 is alkyl of 1 to 3 carbon atoms, R.sub.2 is alkyl of 1 to 12 carbon atoms, R.sub.3 is alkyl of 1 to 4 carbon atoms comprising reacting a compound of the formula ##STR2## wherein R.sub.4 is a remainder of an easily cleavable ether, K is a protected ketone function in the form of ketal, thioketal or mixed ketal and R.sub.1 has the above definition with a magnesium organic compound reagent of the formulaHalMg--CH.sub.2 --R.sub.2 Awherein Hal is a halogen and R.sub.2 is defined as above to obtain a compound of the formula ##STR3## wherein R.sub.1, R.sub.2 and K are defined as above, reacting the latter with an acylation agent to obtain a compound of the formula ##STR4## wherein R.sub.5 is alkyl of 1 to 6 carbon atoms or aryl of 6 to 10 carbon atoms and R.sub.1, R.sub.2 and K are defined as above, reacting the latter with an appropriate alkylation agent to obtain a compound of the formula ##STR5## wherein R.sub.1, R.sub.2, R.sub.
    Type: Grant
    Filed: June 11, 1993
    Date of Patent: March 21, 1995
    Assignee: Roussel-Uclaf
    Inventors: Jean Buendia, Veronique Crocq, Christian Masson, Denis Prat, Michel Vivat
  • Patent number: 5321019
    Abstract: Compounds of formula I: ##STR1## in which the various R groups have the meanings defined in the disclosure are useful as medicaments for the treatment of hepatobiliary diseases.
    Type: Grant
    Filed: January 11, 1993
    Date of Patent: June 14, 1994
    Assignee: Giuliani S.p.A.
    Inventors: Giangermano Giuliani, Giuliano Frigerio, Roberto Pellicciari