Arch Development Corporation

The University of Chicago

Shutsung Liao

Ching Song

Richard Hiipakka

Tehming Liang

John Pataki

Ronald G Harvey

Chawnshang Chang

Dacheng Peng

John Kokontis

Yung-Hsi Kao

Compounds of formula (I): in which R, R, R, R, R, R, R, R, R, R, R, R, R, R, R, R, R, R, R, A, D, X, Y, and Z are defined in the specification. Also disclosed is a method of using one of the compounds to lower the blood cholesterol level and treat cancer, atherosclerosis, diabetes, Alzheimer's disease, and corneal arcus.

Liver X receptor agonists

A method of treating a disorder related to a high cholesterol concentration, comprising administering to a subject in need thereof a compound of formula (I): Also disclosed are methods, kits, combinations, and compositions for treating a disorder in a subject where an activator of liver X alpha is indicated, such as in, for example, treating a high cholesterol disease.

Method of treating disorder related to high cholesterol concentration

A compound of formula (I):Each of R, R, R, R, R, R, R, R, R, R, R, R, and R, independently, is hydrogen, halo, alkyl, haloalkyl, hydroxy, amino, carboxyl, oxo, sulfonic acid, or alkyl that is optionally inserted with &#x2014;NH&#x2014;, &#x2014;N(alkyl)&#x2014;, &#x2014;O&#x2014;, &#x2014;S&#x2014;, &#x2014;SO&#x2014;, &#x2014;SO&#x2014;, &#x2014;O&#x2014;SO&#x2014;, &#x2014;SO&#x2014;O&#x2014;, &#x2014;SO&#x2014;O&#x2014;, &#x2014;CO&#x2014;, &#x2014;CO&#x2014;O&#x2014;, &#x2014;O&#x2014;CO&#x2014;, &#x2014;CO&#x2014;NR'&#x2014;, or &#x2014;NR&#x2032;&#x2014;CO&#x2014;; or Rand Rtogether, Rand Rtogether, Rand Rtogether, or Rand Rtogether are eliminated so that a C&#x2550;C bond is formed between the carbons to which they are attached; each of R, R, R, R, and R, independently, is hydrogen, halo, alkyl, haloalkyl, hydroxyalkyl, alkoxy, hydroxy, or amino; n is 0, 1, or 2; A is alkylene, alkenylene, or alkynylene; and each of X, Y, and Z, independently, is alkyl, haloalkyl, &#x2014;OR&#x2032;, &#x2014;SR&#x2032;, &#x2014;NR&#x2032;R&#x2033;, &#x2014;N(OR&#x2032;)R&#x2033;, or &#x2014;N(SR&#x2032;)R&#x2033;; or X and Y together are &#x2550;O, &#x2550;S, or &#x2550;NR&#x2032;; wherein each of R&#x2032; and R&#x2033;, independently, is hydrogen, alkyl, or haloalkyl.

Pharmaceutical compositions and methods for treating androgen related disorders. The pharmaceutical compositions may include a 5&agr;-reductase inhibitor, such as natural and synthetic flavanoids, catechols, curcumin-related substances, quinones, catechins, particularly epigallocatechin derivatives, fatty acids, and the salts, esters, analogues, pro-drugs, isomers, racemic mixtures, or derivatives of any of the foregoing. The use of testosterone (or DHT) combinations with the aforementioned 5&agr;-reductase inhibitor compounds is also contemplated.

Method and compositions for regulation of 5-alpha reductase activity

Steroid derivatives of this invention interact with nuclear liver X receptor (LXR) and ubiquitous receptor (UR) and can be used to treat a variety of LXR- or UR-mediated disorders.

3,6-dihydroxy-24-amidyl steroid derivatives

Polyhydroxylated benzene-containing compounds

Compounds that inhibit 5-alpha-reductase are provided. The compounds are used to treat prostate cancer, breast cancer, obesity, skin disorders and baldness.

Methods and compositions for regulation of 5-&agr;-reductase activity

The invention relates generally to compositions of and methods for obtaining ubiquitous, nuclear receptor (UR) polypeptides. The invention also relates to polynucleotides encoding UR polypeptides, recombinant host cells and vectors containing UR-encoding polynucleotide sequences, and recombinant UR polypeptides. By way of example, the invention discloses the cloning and functional expression of at least two different UR polypeptides. The invention also includes methods for using the isolated, recombinant receptor polypeptides in assays designed to select substances which interact with UR polypeptides for use in diagnostic, drug design and therapeutic applications.

Isolated nucleic acid encoding a ubiquitous nuclear receptor

Disclosed are DNA sequences encoding DNA binding polypeptides including androgen receptor (AR) and TR2 polypeptides. Illustratively, human and rat AR-cDNA have 79 kD and 98 kD polypeptide expression products which are immunoprecipitable by human auto-immune anti-androgen receptor antibodies and are capable of binding androgens specifically and with high affinity. Also disclosed are antibodies and immunological methods and materials for detection of androgen receptor and TR2 polypeptides and hybridization methods and materials for detection of AR-and TR2-related nucleic acids.

DNA binding proteins including androgen receptor

Disclosed are a novel class of antiandrogenic compounds including saturated and unsaturated fatty acids, catechin gallates, their derivatives, and synthetic analogs, their method of synthesis, and their use in treating disorders associated with androgenic activities. Also disclosed is the use of known compounds not previously known for their antiandrogenic activity in treating disorders related to androgenic activities and cancers.

Methods and compositions for inhibiting 5.alpha.-reductase activity

Disclosed are novel classes of anti-androgens including dihydrophenanthrene derivatives, their method of synthesis and their use in treating disorders associated with excessive androgenic activities.

Anti-androgen compounds

Disclosed are a novel class of anti-androgenic compounds including saturated and unsaturated fatty acids, their derivatives, and synthetic analogs, according to the following formula:

Disclosed are novel classes of anti-androgen including dihydrophenanthrene derivatives, their method of synthesis and their use in treating disorders associated with excessive androgenic activities.

Growing community of inventors

Chicago, IL, United States of America

Shutsung Liao