Patents Represented by Attorney Angelo Castellino
  • Patent number: 8309746
    Abstract: The invention relates to processes for preparing 17-alkynyl-7-hydroxy-steroids, such as 17-Ethynyl-10R,13S-dimethyl 2,3,4,7,8R,9S, 10,11,12,13,14S,15,16,17-hexadecahydro-1H-cyclopenta[a]phenanthrene-3R, 7R,17S-triol (also referred to as 17?-ethynyl-androst-5-ene-3?,7?,17?-triol), that are essentially free of process impurities having binding activity at nuclear estrogen receptors.
    Type: Grant
    Filed: June 5, 2009
    Date of Patent: November 13, 2012
    Assignee: Harbor Therapeutics, Inc
    Inventors: Steven K. White, Yu Ge, Yujin Huang
  • 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
  • Patent number: 8106036
    Abstract: The invention provides compositions comprising formula 1 steroids, e.g., 16?-bromo-3?-hydroxy-5?-androstan-17-one hemihydrate and one or more excipients, typically wherein the composition comprises less than about 3% water. The compositions are useful to make improved pharmaceutical formulations. The invention also provides methods of intermittent dosing of steroid compounds such as analogs of 16?-bromo-3?-hydroxy-5?-androstan-17-one and compositions useful in such dosing regimens. The invention further provides compositions and methods to inhibit pathogen (viral) replication, ameliorate symptoms associated with immune dysregulation and to modulate immune responses in a subject using certain steroids and steroid analogs. The invention also provides methods to make and use these immunomodulatory compositions and formulations.
    Type: Grant
    Filed: December 9, 2009
    Date of Patent: January 31, 2012
    Assignee: Harbor Biosciences, Inc.
    Inventor: James M. Frincke
  • Patent number: 7947846
    Abstract: The invention relates to the use of compounds to treat a number of conditions, such as thrombocytopenia, neutropenia or the delayed effects of radiation therapy. Compounds that can be used in the invention include methyl-2,3,4-trihydroxy-1-O-(7,17-dioxoandrost-5 -ene-3?-yl)-?-D-glucopyranosiduronate, 16?,3?-dihydroxy-5?-androstan-17-one or 3,7,16,17 -tetrahydroxyandrost-5-ene, 3,7,16,17-tetrahydroxyandrost-4-ene, 3,7,16,17 -tetrahydroxyandrost-1-ene or 3,7,16,17-tetrahydroxyandrostane that can be used in the treatment method.
    Type: Grant
    Filed: December 8, 2009
    Date of Patent: May 24, 2011
    Assignee: Harbor BioSciences, Inc.
    Inventor: James M. Frincke
  • Patent number: 7935839
    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: October 16, 2006
    Date of Patent: May 3, 2011
    Assignee: Harbor Biosciences, Inc.
    Inventor: James M. Frincke
  • Patent number: 7910755
    Abstract: The invention relates to methods to prevent, treat, ameliorate or slow the progression of one or more of a blood cell deficiency, unwanted inflammation, allergy, immune suppression condition, immunosenescence, autoimmune disorder, infection, neurological disorder, cardiovascular disorder, pulmonary disorder, trauma, hemorrhage, bone fracture or unwanted or excess bone loss with steroid compounds containing carbon-carbon double bonds within the fused four-ring system such that the steroid compounds are unsaturated. The unsaturated steroid compounds include 3,16?,17?-trihydroxy-7-acetoxy-androst-1,3,5(10),6-tetraene, 3,16?,17?-trihydroxy-7-methoxy-androst-1,3,5(10),6-tetraene, 3,17?-dihydroxy-7-acetoxy-16?-fluoro-androst-1,3,5(10),6-tetraene, 3,17?-dihydroxy-7-methoxy-16?-fluoro-androst-1,3,5(10),6-tetraene, 3,17?-dihydroxy-7,16?-diacetoxy-androst-1,3,5(10),6-tetraene and 3,17?-dihydroxy-7-methoxy-16?-acetoxy-androst-1,3,5(10),6-tetraene.
    Type: Grant
    Filed: March 25, 2006
    Date of Patent: March 22, 2011
    Assignee: Harbor Biosciences, Inc.
    Inventor: James M. Frincke
  • Patent number: 7524835
    Abstract: The invention provides compositions comprising formula 1 steroids, e.g., 16?-bromo-3?-hydroxy-5?-androstan-17-one hemihydrate and one or more excipients, typically wherein the composition comprises less than about 3% water. The compositions are useful to make improved pharmaceutical formulations. The invention also provides methods of intermittent dosing of steroid compounds such as analogs of 16?-bromo-3?-hydroxy-5?-androstan-17-one and compositions useful in such dosing regimens. The invention further provides compositions and methods to inhibit pathogen (viral) replication, ameliorate symptoms associated with immune dysregulation and to modulate immune responses in a subject using certain steroids and steroid analogs. The invention also provides methods to make and use these immunomodulatory compositions and formulations.
    Type: Grant
    Filed: June 25, 2003
    Date of Patent: April 28, 2009
    Assignee: Hollis-Eden Pharmaceuticals, Inc.
    Inventor: James M. Frincke