Abstract: Compounds and methods of synthesizing oxysterols are provided. The compounds and methods provided allow the oxysterol to be safely produced at a high yield. The compounds and methods provided can produce the oxysterol in a stereoselective manner. The method comprises reacting a diol with borane and hydrogen peroxide to form the oxysterol or a pharmaceutically acceptable salt, hydrate or solvate thereof.
Type:
Grant
Filed:
March 30, 2017
Date of Patent:
March 26, 2019
Assignee:
Warsaw Orthopedic, Inc.
Inventors:
Roger E. Harrington, Jerbrena C. Jacobs, Damodaragounder Gopal, Ke-Qing Ling, Marco Burello
Abstract: Compounds and methods of synthesizing oxysterols are provided. The compounds and methods provided allow the oxysterol to be safely produced at a high yield. The compounds and methods provided can produce the oxysterol in a stereoselective manner.
Type:
Grant
Filed:
December 8, 2015
Date of Patent:
April 4, 2017
Assignee:
Warsaw Orthopedic, Inc.
Inventors:
Roger E. Harrington, Jerbrena C. Jacobs, Damodaragounder Gopal, Ke-Qing Ling, Marco Burello
Abstract: The present invention provides an improved process for the preparation of 17-desoxy corticosteroid derivatives in a single chemical step by reacting the 17-hydroxy starting material with an excess of Trimethylsilyl Iodide. The present invention is specifically advantageous in preparing 17-desoxy corticosteroid derivatives having one or more halogen groups at positions 2, 6, 7 or 9 of the corticosteroid such as Clocortolone of Desoximetasone.
Type:
Application
Filed:
July 20, 2011
Publication date:
August 15, 2013
Applicant:
Taro Pharmaceutical Industries Ltd.
Inventors:
Simon Cherniak, Rosa Cyjon, Ilana Ozer, Igor Nudelman
Abstract: Method, compositions, and compounds for modulating brain excitability to alleviate stress, anxiety, and seizure activity using certain steroid derivatives that act at a newly identified site on the gamma-ammobutyric acid/benzodiazepine receptor-chloride ionpore (GBR) complex.
Abstract: Disclosed is a process for the production of a .DELTA..sup.17(20) -steroid of the formula ##STR1## which comprises starting with a 16-unsaturated corticoid of the formula ##STR2## and contacting the 16-unsaturated corticoid (I) with a methylating agent in the presence of a copper catalyst and a silylating agent.
Abstract: The present invention relates to 21-(3-carboxy-1-oxopropoxy) -17.alpha.-hydroxy-11.alpha.-(3,3-dimethyl-1-oxobutoxy)pregna-1,4-diene-3, 20 dione and pharmaceutically acceptable salts thereof which are useful steroid prodrugs.
Type:
Grant
Filed:
February 16, 1989
Date of Patent:
August 14, 1990
Assignee:
The Upjohn Company
Inventors:
John M. Braughler, Edward D. Hall, Wendell Wierenga, John M. McCall
Abstract: C.sub.16 -unsaturated corticoids are readily transformed to the corresponding 16.alpha.-methyl-17.alpha.-hydroxy corticoids by use of a .DELTA..sup.17 (.sup.20)-20-silyl ether.
Abstract: Copolyester plasticizers useful for the formulation of PVC refrigerator gaskets which exhibit improved resistance to migration and marring and improved processing characteristics are provided. The copolyesters are obtained by reacting an acid component consisting of a mixture of a benzene dicarboxylic acid (or anhydride or methyl ester thereof) and an aliphatic C.sub.5-12 saturated dicarboxylic acid (or methyl ester) with an alcohol component consisting of a mixture of neopentyl glycol and ethylene glycol. An aliphatic C.sub.6-13 saturated monofunctional alcohol or aliphatic C.sub.6-13 saturated monocarboxylic acid terminating agent is also included in the reaction.
Type:
Grant
Filed:
April 23, 1987
Date of Patent:
April 25, 1989
Assignee:
National Distillers and Chemical Corporation
Abstract: Method, compositions, and compounds for modulating brain excitability to alleviate stress, anxiety, and seizure activity using certain steroid derivatives that act at a newly identified site on the gamma-ammobutyric acid/benzodiazepine receptor-chloride ionpore (GBR) complex.
Type:
Grant
Filed:
November 23, 1992
Date of Patent:
May 20, 1997
Assignee:
University of Southern California
Inventors:
Kelvin W. Gee, Michael B. Bolger, Nancy C. Lan