Abstract: The invention provides and describes solid state 17?-ethynyl-5?-androstane-3?,17?-diol including amorphous and crystalline forms and specific polymorphic forms thereof. Anhydrates and solvates of 17?-ethynyl-5?-androstane-3?,17?-diol include Form III anhydrate and Form I solvate. The invention further relates to solid and suspension formulations containing 17?-ethynyl-5?-androstane-3?,17?-diol in a described solid state form and use of the formulations to treat cancers or precancers such as prostate cancer or breast cancer in subjects or human patients. The invention also relates to methods to make liquid formulations from solid state forms of 17?-ethynyl-5?-androstane-3?,17?-diol and uses of such formulations in treating the described conditions.

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.

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.

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.

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.

Abstract: The invention relates to solid state forms of androst-5-ene-3?,7?,16?,17?-tetrol, formulations containing or prepared from such solid state forms and use of these materials for modulating unwanted inflammation including acute and chronic non-productive inflammation. The formulations can be used to prevent, treat or slow the progression of conditions related to autoimmunity and metabolic disorders such as arthritis, multiple sclerosis, ulcerative colitis, Type 1 diabetes and Type 2 diabetes.

Abstract: The invention relates to solid state forms of androst-5-ene-3?,7?,16?,17?-tetrol, formulations containing or prepared from such solid state forms and use of these materials for modulating unwanted inflammation including acute and chronic non-productive inflammation. The formulations can be used to prevent, treat or slow the progression of conditions related to autoimmunity and metabolic disorders such as arthritis, multiple sclerosis, ulcerative colitis, Type 1 diabetes and Type 2 diabetes.

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.

Abstract: The invention relates to processes for preparing 3?-O-linked steroids including 3?-O-linked-androst-5-ene steroids and 3?-O-linked-5a-androstane steroids. In one process a 3?,4?-epoxy androst-5-en-17-one is predominately reduced at the epoxy moiety wherein reduction of the 3?,4? epoxy functional group occurs preferentially at position C4 with retention of configuration at position C3 to provide a 3?-O-linked-androst-5-ene steroid. In another process, conditions are provided for inversion of configuration of a 3?-hydroxy-androst-5-ene steroid by the Mitsunobu reaction to provide a 3?-O-linked-androst-5-ene steroid with reduced amounts of 3?,5?-cycloandrostane side-product impurities.

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.

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.

Abstract: The invention provides and describes solid state 17?-ethynyl-5?-androstane-3?,17?-diol including amorphous and crystalline forms and specific polymorphic forms thereof. Anhydrates and solvates of 17?-ethynyl-5?-androstane-3?,17?-diol include Form III anhydrate and Form I solvate. The invention further relates to solid and suspension formulations containing 17?-ethynyl-5?-androstane-3?,17?-diol in a described solid state form and use of the formulations to treat cancers or precancers such as prostate cancer or breast cancer in subjects or human patients. The invention also relates to methods to make liquid formulations from solid state forms of 17?-ethynyl-5?-androstane-3?,17?-diol and uses of such formulations in treating the described conditions.

Abstract: The invention relates to pharmaceutically acceptable formulations comprising an active pharmaceutical ingredient such as androst-5-ene-3?,17?-diol, androst-5-ene-3?,7?,17?-triol or derivatives of either of these compounds and an air oxidizable excipient that have been stabilized with respect to efficacy. Use of the efficacy-stabilized formulations to treat a number of conditions or symptoms thereof, such as a symptom associated with exposure to radiation is described.

Abstract: The invention relates to the use of compounds to ameliorate or treat a 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.

Abstract: The invention relates to the use of compounds to ameliorate or treat a 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.

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.

Abstract: The invention relates to the use of compounds to ameliorate or treat a 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.

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&bgr;-hydroxy-17&bgr;-aminoandrost-5-ene, 3&bgr;-hydroxy-16&agr;-fluoro-17&bgr;-aminoandrost-5-ene, 3&agr;-hydroxy-16&agr;-fluoro-17&bgr;-aminoandrost-5-ene, 3&bgr;-hydroxy-16&bgr;-fluoro-17&bgr;-aminoandrost-5-ene, 1&agr;,3&bgr;-dihydroxy-4&agr;-fluoroandrost-5-ene-17-one, 1&agr;,3&bgr;,17&bgr;-trihydroxy-4&agr;-fluoroandrost-5-ene, 1&bgr;,3&bgr;-dihydroxy-6&agr;-bromoandrost-5-ene, 1&agr;-fluoro-3&bgr;,12&agr;-dihydroxyandrost-5-ene-17-one, 1&agr;-fluoro-3&bgr;,4&agr;-dihydroxyandrost-5-ene and 4&agr;-fluoro-3&bgr;,6&agr;,17&bgr;-trihydroxyandrostane.

Abstract: Methods for stereospecific synthesis of 9-cis olefins and retinoids. In one particular aspect, a cis olefin is generated via a lactol ring opening with complete retention of double bond configuration.

Abstract: Tricyclic retinoids having activity for retinoic acid receptors and/or retinoid X receptors are provided. Also provided are pharmaceutical compositions incorporating such tricyclic retinoid compounds and methods for their therapeutic use.