Carbon Or Halogen Bonded Directly At The 6- Or 7-position Patents (Class 552/647)
  • 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
  • Patent number: 7820642
    Abstract: Disclosed are compounds of the formula (I) wherein R is C1-C30 alkyl, which may be optionally further substituted with one or more of C5-C8 cycloalkyl groups, or a C5-C12 cycloalkyl, which may be optionally substituted with one or more C1-C30 alkyl groups, R? is hydrogen or lower alkyl, R? is a C1-C30 alkyl or halo, and the bond between C14 and C15 can be a single bond or double bond. Also disclosed are pharmaceutical compositions comprising such compounds and methods of use thereof. These compounds can find use in treating a number of diseases or conditions such as hypogonadism, osteoporosis, and anemia, in providing hormonal therapy and contraception, as an anabolic agent, and in suppressing the release of hormones such as the luteinizing hormone.
    Type: Grant
    Filed: January 24, 2006
    Date of Patent: October 26, 2010
    Assignee: The United States of America as represented by the Department of Health and Human Services
    Inventors: Richard P. Blye, Hyun K. Kim
  • Publication number: 20100204497
    Abstract: The invention relates to a process for the preparation of 7?-methyl hydroxy steroids of the formula I wherein R1 is hydrogen, methyl or C?CH; R2 is (CH2)nOH, wherein n is 0, 1 or 2; by a copper mediated 1,6-conjugate addition of a Grignard reagent CH3MgX, X being a halogen, to the 4,6-unsaturated 3-ketosteroid of formula II, wherein R1 and R2 are as previously defined, comprising protecting the hydroxy group of the steroid of formula II with a trialkylsilyl group, followed by treating the hydroxy protected steroid with the Grignard reagent. The process of the invention is useful for the production of pharmacologically interesting steroids.
    Type: Application
    Filed: April 22, 2010
    Publication date: August 12, 2010
    Inventors: Patrick Arnoldus Maria Van Buggenum, Johannes Stoelwinder, Martin Ostendorf
  • Patent number: 7361645
    Abstract: The invention relates to 11?-halogen steroids with general formula (I), whereby R11 is halogen, X—Y-Z represents a group with one of the two structures CH?C—C or CH2—C?C and the other radicals have the meaning that is indicated in the claims, also the production and use of these compounds for the production of pharmaceutical agents as well as pharmaceutical preparations that contain 11?-halogen steroids.
    Type: Grant
    Filed: January 24, 2002
    Date of Patent: April 22, 2008
    Assignee: Bayer Schering Pharma AG
    Inventors: Rolf Bohlmann, Hermann Kuenzer, Reinhard Nubbemeyer, Dieter Zopf
  • Patent number: 7169769
    Abstract: This invention relates to steroidal compounds having the formula I wherein: R1 is O, (H,H), (H,OH), NOH, whereby OH is optionally etherified or esterified; R2 and R3 are independently hydrogen or (C1-4) alkyl and at least one of R2 and R3 is (C1-4) alkyl; R4 is hydrogen, or (C1-15) acyl for use in androgen-related treatments, such as androgen insufficiency and male or female contraception.
    Type: Grant
    Filed: September 6, 2002
    Date of Patent: January 30, 2007
    Assignee: Akzo Nobel N.V.
    Inventors: J Jaap Van Der Louw, D Dirk Leysen, M.E. Marcel Evert De Gooijer
  • Patent number: 6864248
    Abstract: An androgenic steroid compound of the formula: wherein: X, Y, Z, R1, R2, R3, R5 and R6 are as defined herein.
    Type: Grant
    Filed: November 4, 2003
    Date of Patent: March 8, 2005
    Assignee: Research Triangle Institute
    Inventors: C. Edgar Cook, John A. Kepler, Yue-Wei Lee, Mansukh C. Wani
  • Patent number: 6670352
    Abstract: An androgenic steroid compound of the formula: wherein: X, Y, Z, R1, R2, R3, R5 and R6 are as defined herein.
    Type: Grant
    Filed: January 22, 2002
    Date of Patent: December 30, 2003
    Assignee: Research Triangle Institute
    Inventors: C. Edgar Cook, John A. Kepler, Yue-Wei Lee, Mansukh C. Wani
  • Patent number: 6492536
    Abstract: The subject of the invention is the products of formula (I): in which either R1 represents halogen, hydroxyl, (C1-C8) alkyloxy or (C1-C12) acyloxy, and R2 represents halogen or hydrogen, or R1 and R2 form together a double bond, Z is chosen from optionally substituted (C1-C8) alkylthio, optionally substituted arylthio, (C1-C8) alkyloxy, halogen, cyano, mercapto, thiocyanato and (CH2)0-1—CO2H, optionally esterified, Y represents hydrogen or methyl, the dotted line in position 1-2 or 5-6 optionally representing a second bond, as well as their addition salts, their preparation process, the intermediates of this process and the pharmaceutical compositions containing them.
    Type: Grant
    Filed: June 25, 2001
    Date of Patent: December 10, 2002
    Assignee: Aventis Pharma S.A.
    Inventors: Neerja Bhatnagar, Andre Claussner, Christian Marchandeau, Michele Resche Rigon, Jean-Georges Teutsch
  • 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: 5925630
    Abstract: The invention relates to 3.alpha.-hydroxy, 17-(un)substituted derivatives of the androstane series and 3.alpha.-hydroxy, 21-substituted derivatives of the pregnane series. These derivatives are capable of acting at a recently identified site on the GRC, thereby modulating brain excitability in a manner that will alleviate stress, anxiety, insomnia, mood disorders that are amenable to GRC-active agents (such as depression) and seizure activity. The steroid derivatives of this invention are those having the general structural Formula: ##STR1## wherein R, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8, R.sub.9 and R.sub.10 are further defined herein and the dotted lines are single or double bonds. The structure includes androstanes, pregnanes (R.sub.4 =methyl), 19-norandrostanes, and norpregnanes (R.sub.4 =H).
    Type: Grant
    Filed: June 6, 1996
    Date of Patent: July 20, 1999
    Assignee: CoCensys, Inc.
    Inventors: Ravindra B. Upasani, David B. Fick, Derk J. Hogenkamp, Nancy C. Lan
  • Patent number: 5866558
    Abstract: Compounds of formula I: ##STR1## wherein R, R.sup.1, R.sup.2, R.sup.3, and R.sup.4 have any of the values defined in the specification, and their pharmaceutically acceptable salts, are inhibitors of aromatase, and are useful for treating diseases such as breast cancer, in mammals. Also disclosed are pharmaceutical compositions, processes for preparing compounds of formula (I) and intermediates useful for preparing compounds of formula I.
    Type: Grant
    Filed: May 8, 1997
    Date of Patent: February 2, 1999
    Assignee: Regents of the University of Minnesota
    Inventors: Yusuf J. Abul-Hajj, Abraham Akanni
  • Patent number: 4921845
    Abstract: The invention relates to new 11-arylsteroid compounds, having a strong antiprogestin and a weak or nonexistent antiglucocorticoid activity, to processes for preparing said compounds and also to pharmaceutical preparations which contain these derivatives as active constituent, characterized in that said steroids have the following formula: ##STR1## in which R.sub.1 is an aryl group with a ##STR2## group as substituent, X and Y each being separately H or a (1-4 C) hydrocarbyl group or together a (2-C) hydrocarbyl group which forms a 3- to 7-membered ring together with the nitrogen atom;R.sub.2 is hydrogen, hydroxyl, an acyloxy or an alkoxy group or a saturated or unsaturated hydrocarbyl group containing 1-8 carbon atoms, which hydrocarbyl group is provided with at least one hydroxyl, oxo, azido, cyano and/or halogen group;R.sub.3 is a hydroxyl, an acyloxy or an alkoxy group or an acyl group optionally substituted by a hydroxyl, alkoxy, acyloxy or halogen group; or R.sub.2 and R.sub.
    Type: Grant
    Filed: December 8, 1988
    Date of Patent: May 1, 1990
    Assignee: Akzo N.V.
    Inventors: Hendrick Paul de Jongh, Nicolaas P. van Vliet