Endece LLC

James G Yarger

Steven H Nye

Richard J Pariza

Steve Nye

Disclosed are compounds of the formula: and the respective enantiomers, stereochemical isomers, hydrates, solvates, tautomers and pharmaceutically acceptable salts of such compounds; which can be useful in the treatment of various types of cancer.

6-substituted estradiol derivatives and methods of use

Disclosed are compounds of the formula: wherein R, R, Rand Rare independently hydrogen, C-Calkyl, halo, a sulfate, a glucuronide, &#x2014;OH, a bulky group, aryl, cycloalkyl, heteroaryl, heterocycloalkyl, &#x2014;N(CH); a phosphate group, and a phosphinate group; Ris hydrogen, halogen or alkyl; Ris selected from the group consisting of H, C-Calkyl, halogen, a sulfate, a glucoronide, &#x2014;SONH, &#x2014;COOH, &#x2014;CN, &#x2014;CHCN&#x2014;, &#x2014;NHCN&#x2014;, &#x2014;CHO, &#x2550;CHOCH, &#x2014;COO salt, &#x2014;OSOalkyl, &#x2014;NH, and &#x2014;NHCO(CH); Ris selected from the group consisting of H, a C-Calkyl, a sulfate, a glucoronide, a bulky group, aryl, cycloalkyl, heteroaryl and heterocycloalkyl; X is selected from the group consisting of C-Calkyl, C-Calkenyl, C-Calkynyl, halogen, a glucoronide, &#x2014;NH, &#x2014;SONH, &#x2014;COOH, &#x2014;CN, &#x2014;CHCN, &#x2014;NHCN, &#x2014;CHO, &#x2014;COOsalt, &#x2014;OSOalkyl, &#x2014;SH, &#x2014;SCH, &#x2014;CH[(CH)CH]COOCH, &#x2014;(CH)COOCH, &#x2014;(CH)&#x2014;O&#x2014;CH, &#x2014;(CH)&#x2014;O&#x2014;(CH)CH, (CH)&#x2014;S&#x2014;CH, &#x2014;(CH)&#x2014;S&#x2014;(CH)CH, &#x2014;(CH)&#x2014;NH&#x2014;(CH)CH, &#x2014;C-Calkenyl-O&#x2014;(CH)CH, &#x2014;C-Calkenyl-S&#x2014;(CH)CH, &#x2014;C-Calkenyl-N&#x2014;(CH)CH, &#x2014;C-Calkynyl-O&#x2014;(CH)CH, &#x2014;C-Calkynyl-S&#x2014;(CH)CH, &#x2014;C-Calkynyl-N&#x2014;(CH)CH, &#x2014;(CH)&#x2014;OH, &#x2014;(CH)&#x2014;O&#x2014;NH, &#x2014;(CH)&#x2014;S&#x2014;NH, &#x2014;NH(CH)CH, &#x2014;NH(CH)OCH, &#x2014;NH(CH)CHOH&#x2014;COOH, &#x2014;N(CH), &#x2014;(CH)(NH)CHOH, &#x2014;NHCOOH, &#x2014;(CH)NHCOOH, &#x2014;NO, &#x2014;SCN, &#x2014;SOalkyl, &#x2014;B(OH), &#x2014;(CH)N(CH)&#x2014;SO&#x2014;NH, &#x2014;(CH)&#x2014;NH&#x2014;SO&#x2014;NH, &#x2014;NHC(&#x2550;S) CH, and &#x2014;NHNH; and Y is selected from hydrogen, &#x2550;O, &#x2014;OCO(R) and &#x2014;OH; wherein m is an integer between 0-20, n is an integer between 0-8, thesymbol represents either a single or a double bond capable of forming a keto group at position 3 or 17; and thesymbol represents any type of bond regardless of the stereochemistry; and the respective enantiomers, other stereochemical isomers, hydrates, solvates, tautomers and pharmaceutically acceptable salts of said compounds. The compounds are useful in the treatment of various types of cancer.

Disclosed is a method of remyelinating axons with 6-substituted estradiol compounds of the formula  The methods can be used to treat a variety of demyelinating diseases.

6-substituted estradiol derivatives for use in remyelination of nerve axons

Disclosed herein are 6-substituted 13-demethyl-estradiol derivatives as selective ER&#x3b2; agonists. Also disclosed is a method for treating pain by administering these 6-substituted 13-demethyl-estradiol derivatives.

6-substituted demethyl-estradiol derivatives as selective ER-&#x3b2; agonists

A method of inhibiting growth of cancer cells comprising contacting cancer cells with a 6-substituted estradiol derivative in an amount at least partially sufficient to inhibit said growth is disclosed. The compounds have the general formula depicted below, herein R, R, R, R, R, Rand Rare as defined herein. 

A compound having the structure: wherein R, R, R, R, X, Y and Z are as defined herein. The compounds are estrogen receptor modulators useful for the treatment of proliferative disorders.

6-Methyloxaalkyl exemestane compounds and related compositions, as can be used, chemotherapeutically, to inhibit growth and proliferation of cancer cells.

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Cedarburg, WI, United States of America

James G Yarger