Oxygen Bonded Directly At The 7-, 8- Or 9-position Patents (Class 552/562)
  • Patent number: 10995112
    Abstract: Described herein are solid state 17?-ethynylandrost-5-ene-3?,7?,17?-triol including amorphous and crystalline forms and specific polymorphic forms thereof, and use of solid state 17?-ethynylandrost-5-ene-3?,7?,17?-triol in treating numerous diseases and disorders, including hyperglycemic conditions, such as type 2 diabetes and metabolic syndrome, autoimmune conditions, such as rheumatoid arthritis, ulcerative colitis and type 1 diabetes, among other inflammation related conditions, and neurodegenerative conditions in subjects or human patients.
    Type: Grant
    Filed: October 10, 2019
    Date of Patent: May 4, 2021
    Assignee: NeurMedix, Inc.
    Inventors: Steven K. White, Igor Ivanisevic, Kyle Stephens, Mark Andres, Brenton Skylar Wolfe
  • Patent number: 9850271
    Abstract: The invention provides and describes solid state 17?-ethynyl-androst-5-ene-3?,7?,17?-triol including amorphous and crystalline forms and specific polymorphic forms thereof. Anhydrates and solvates of 17?-ethynyl-androst-5-ene-3?,7?,17?-triol include Form I anhydrate and Form IV and Form V solvates. The invention further relates to solid and suspension formulations containing 17?-ethynyl-androst-5-ene-3?,7?,17?-triol in a described solid state form and use of the formulations to treat hyperglycemic conditions, such as type 2 diabetes and metabolic syndrome, and autoimmune conditions, such as rheumatoid arthritis, ulcerative colitis and type 1 diabetes, among other inflammation related conditions in subjects or human patients. The invention also relates to methods to make liquid formulations from solid state forms of 17?-ethynyl-androst-5-ene-3?,7?,17?-triol and uses of such formulations in treating the described conditions.
    Type: Grant
    Filed: November 10, 2016
    Date of Patent: December 26, 2017
    Assignee: NeurMedix, Inc.
    Inventors: Steven K White, Igor Ivanisevic, Kyle Stephens, Mark Andres, Brenton Skylar Wolfe
  • 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: 8252947
    Abstract: The invention provides and describes solid state 17?-ethynyl-androst-5-ene-3?, 7?,17?-triol including amorphous and crystalline forms and specific polymorphic forms thereof. Anhydrates and solvates of 17?-ethynyl-androst-5-ene-3?, ?,17?-triol include Form I anhydrate and Form IV and Form V solvates. The invention further relates to solid and suspension formulations containing 17?-ethynyl-androst-5-ene-3?,7?,17?-triol in a described solid state form and use of the formulations to treat hyperglycemic conditions, such as type 2 diabetes and metabolic syndrome, and autoimmune conditions, such as rheumatoid arthritis, ulcerative colitis and type 1 diabetes, among other inflammation related conditions in subjects or human patients. The invention also relates to methods to make liquid formulations from solid state forms of 17?-ethynyl-androst-5-ene-3?, 7?,17?-triol and uses of such formulations in treating the described conditions.
    Type: Grant
    Filed: April 3, 2009
    Date of Patent: August 28, 2012
    Assignee: Harbor Therapeutics, Inc.
    Inventors: Steven K. White, Igor Ivanisevic, Kyle Stephens, Mark Andres, Brenton Skylar Wolfe
  • Publication number: 20110098260
    Abstract: The invention provides methods to treating conditions such as prostate cancer, or for ameliorating one or more symptoms associated with prostate cancer, or for agents that modulate the biological activity of the androgen receptor. The invention also provides methods and compositions suitable for therapeutic applications.
    Type: Application
    Filed: December 1, 2010
    Publication date: April 28, 2011
    Applicant: Harbor BioSciences, Inc.
    Inventor: James M. Frincke
  • Publication number: 20090061358
    Abstract: Photoacid generators generate sulfonic acids of formula (1a) or (1c) upon exposure to high-energy radiation. R1—COOCH(CF3)CF2SO3+H+??(1a) R1—O—COOCH(CF3)CF2SO3?H+??(1c) R1 is a C20-C50 hydrocarbon group having a steroid structure. The photoacid generators are compatible with resins and can control acid diffusion and are thus suited for use in chemically amplified resist compositions.
    Type: Application
    Filed: September 4, 2008
    Publication date: March 5, 2009
    Inventors: Masaki OHASHI, Youichi Ohsawa, Takeru Watanabe, Takeshi Kinsho
  • Publication number: 20030181742
    Abstract: A process for preparing pregnane derivatives represented by the formula (V), 1
    Type: Application
    Filed: March 4, 2003
    Publication date: September 25, 2003
    Inventors: Makoto Nakazawa, Satoru Kita, Shigeo Ohzono
  • Patent number: 6043603
    Abstract: The invention relates to a low-pressure discharge lamp with at least one porting element (12) placed inside a discharge vessel (10). Said supporting element is provided with a mercurial coating (13) and is coated with a getter material (14). The coated surfaces of the supporting element (12) are inclined at an angle of at least 30 degrees in relation to the longitudinal axis (A--A) of the discharge vessel (10).
    Type: Grant
    Filed: May 21, 1998
    Date of Patent: March 28, 2000
    Assignee: Patent-Treuhand-Gesellschaft fuer elektrische Gluehlampen mbH
    Inventor: Erolf Weinhardt
  • Patent number: 5710293
    Abstract: The present invention relates to a method of using a perchloric acid catalyzed reaction to make acyl derivatives of norprogesterone compounds and, in particular, 16-methylene-17.alpha.-hydroxy-19-norpregn-4-ene-3,20-dione.
    Type: Grant
    Filed: October 13, 1995
    Date of Patent: January 20, 1998
    Assignee: The Population Council, Center for Biomedical Research
    Inventor: Fang Li
  • Patent number: 5565588
    Abstract: New 9-alpha-hydroxy steroids are prepared by the introduction of substituents on the D-ring of 9-alpha-hydroxy-androst-4-ene-3,17-dione.The resulting compounds are useful intermediates in the synthesis of corticosteroids.
    Type: Grant
    Filed: October 4, 1994
    Date of Patent: October 15, 1996
    Assignee: Roussel UCLAF
    Inventors: Jacobus N. M. Batist, Arthur F. Marx, Willem J. Van Zoest, Jagdish C. Kapur
  • Patent number: 5502183
    Abstract: Novel steroids having a 9.alpha.-hydroxy or a 9.alpha.-carbonate substituent can be prepared from 9.alpha.-hydroxyandrostenedione and can be utilized in the synthesis of commercially valuable corticosteroids such as betamethasone. The 9.alpha.-carbonates are prepared by reaction of the corresponding 9.alpha.-hydroxy steroid with a sequence of excess base, trialkylsilyl chloride, alkyl haloformate and alkanol or by using excess base, alkyl haloformate and alkoxide. 9.alpha.-Carbonate-17-keto compounds can be treated with lithium acetylide and a lithium salt to afford the corresponding 17.alpha.-ethynyl-17.beta.-hydroxy-9.alpha.-carbonate. This compound is then esterified with a novel series of reagents to give the 17-ester which can be reduced the corresponding 17-allene. Oxidation of this allene to the bis-epoxide compound, followed by treatment with an alkali metal salt of a carboxylic acid under phase transfer conditions gives the 17.alpha.-hydroxy 21-ester 9.alpha.-carbonate. Elimination of the 9.alpha.
    Type: Grant
    Filed: July 25, 1994
    Date of Patent: March 26, 1996
    Assignee: Schering Corporation
    Inventors: David R. Andrews, Anantha R. Sudhakar
  • Patent number: 5352808
    Abstract: A process for the preparation of a compound of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of hydrogen, alkyl of 1 to 4 carbon atoms optionally substituted by halogen or a nitrogen or oxygen function and alkenyl and alkynyl of 2 to 4 carbon atoms, R.sub.2 is alkyl of 1 to 4 carbon atoms and the A, B, C and D rings are optionally substituted by at least one member of the group consisting of optionally protected --OH or .dbd.0, halogen, alkyl and alkoxy of 1 to 4 carbon atoms and alkenyl and alkynyl of 2 to 4 carbon atoms comprising reacting a compound of the formula ##STR2## wherein R.sub.1 and R.sub.2 and the A, B, C and D rings are defined as above with an oxidizing agent in the presence of water and an at least partially water-miscible solvent to obtain a compound of the formula ##STR3## wherein R.sub.1 and R.sub.
    Type: Grant
    Filed: November 5, 1992
    Date of Patent: October 4, 1994
    Assignee: Roussel Uclaf
    Inventors: Jean Buendia, Michel Vivat
  • Patent number: 5194602
    Abstract: New 9.alpha.-hydroxy-17-methylene steroids are prepared by the introduction of a substituted 17-methylene group in 9.alpha.-hydroxyandrost-4-ene-3, 17-dione.The resulting compounds are useful starting compounds in the synthesis of corticosteroids.
    Type: Grant
    Filed: December 12, 1990
    Date of Patent: March 16, 1993
    Assignee: Gist-Brocades N.V.
    Inventors: Jacobus N. M. Batisi, Arthur F. Marx
  • Patent number: 5112998
    Abstract: There are provided pregnane derivatives represented by formula ##STR1## wherein A.sup.1 represents a hydrogen atom or a hydroxyl group, A.sup.2 represents a substituent such as a hydroxyl group when A.sup.1 represents a hydrogen atom, or A.sup.2 represents a hydrogen atom when A.sup.1 represents a hydroxyl group, or A.sup.1 and A.sup.2 are combined together to form an oxo group; D.sup.1 represents a substitutent such as a hydroxyl group, and D.sup.2 represents a hydrogen atom, or D.sup.1 and D.sup.2 are combined together to form an epoxy group or a single bond; D.sup.3, D.sup.5 and D.sup.7 each represents a hydrogen atom, D.sup.4 represents a hydroxyl group, and D.sup.6 represents a substitutent such as a hydroxyl group, or D.sup.3 and D.sup.4 may be combined together to form an epoxy group or a single bond, or D.sup.4 and D.sup.5 may be combined together to form a single bond, or D.sup.5 and D.sup.6 may be combined together to form an epoxy group or a single bond, or D.sup.6 and D.sup.
    Type: Grant
    Filed: June 15, 1990
    Date of Patent: May 12, 1992
    Assignee: Kuraray Co., Ltd.
    Inventors: Jiro Tsuji, Takashi Takahashi, Masao Tsuji, Naoshi Nakagawa, Tetsuo Takigawa
  • Patent number: 5093502
    Abstract: A process for the preparation of novel 14.alpha., 17.alpha.-dihydroxy-17.beta.-substituted steroids by reacting 14.alpha.-hydroxy-17-oxo-steroids with metal organic compounds and the use of the said novel steroids in the production of 14.alpha., 17.alpha.-methylenedioxy-pregnane derivatives.
    Type: Grant
    Filed: February 16, 1990
    Date of Patent: March 3, 1992
    Assignee: Akzo N.V.
    Inventors: Peter M. Smid, Willem J. Van Zoest, Pieter G. Weber, Arthur F. Marx
  • Patent number: 5028722
    Abstract: Novel 7.beta.-hydroxy-4-pregnene-3,20-dione derivatives are disclosed.The group of these compounds has possibility of being utilized as an intermediate for the synthesis of progesterone derivatives having ovulation-inhibiting activity. These compounds themselves have also cell differentiation activity for M1 cells.
    Type: Grant
    Filed: September 26, 1988
    Date of Patent: July 2, 1991
    Assignee: Snow Brand Milk Products Co., Ltd.
    Inventors: Makoto Yoshihama, Koji Tamura, Nobuo Miyata, Masamichi Nakakoshi