James G Yarger

US Patent:

7846918, Dec 7, 2010

Filed:

Oct 2, 2006

Appl. No.:

11/541987

Inventors:

Richard J. Pariza - Zion IL, US
James G. Yarger - Cedarburg WI, US

Assignee:

Endece, LLC - Mequon WI

International Classification:

A61K 31/56
C07J 1/00

US Classification:

514177, 552640

Abstract:

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

US Patent:

8168621, May 1, 2012

Filed:

Jun 4, 2008

Appl. No.:

12/132857

Inventors:

James Yarger - Cedarburg WI, US

Assignee:

Endece, LLC - Mequon WI

International Classification:

A61K 31/56
C07J 1/00

US Classification:

514182, 514178, 552626

Abstract:

A compound having the structure:.

US Patent:

8629130, Jan 14, 2014

Filed:

Apr 30, 2012

Appl. No.:

13/459665

Inventors:

James G. Yarger - Cedarburg WI, US

Assignee:

Endece, LLC - Mequon WI

International Classification:

A61K 31/565
A61K 31/566

US Classification:

514178, 514182

Abstract:

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.

US Patent:

20080119447, May 22, 2008

Filed:

Nov 29, 2007

Appl. No.:

11/947645

Inventors:

James Yarger - Cedarburg WI, US

International Classification:

A61K 31/565
C12N 5/00
C07J 1/00
A61P 35/00
A61K 31/566

US Classification:

514178, 552625, 552632, 435375, 514182

Abstract:

A compound having the structure:wherein R, R, R, R, R, R, Rand Rare independently hydrogen, Cto Calkyl or substituted alkyl, halogen, sulfate or glucuronide moieties; the symbol represents either a single or a double bond and when the symbol is a double bond and forms a keto group at position 3 or 17, then no Ror Ris present, respectively; the symbol represent the presence or absence of a bond at position 10; and the symbol represents any type of bond regardless of the stereochemistry. The invention also embraces the enantiomers, other stereochemical isomers, hydrates, solvates, tautomers and pharmaceutically acceptable salts of said compounds.

US Patent:

20100130463, May 27, 2010

Filed:

Nov 30, 2009

Appl. No.:

12/627874

Inventors:

James G. Yarger - Cedarburg WI, US

International Classification:

A61K 31/565
C07J 1/00
A61P 35/00

US Classification:

514182, 552628

Abstract:

Disclosed are compounds of the formula:wherein R, R, Rand Rare independently hydrogen, C-Calkyl, halo, a sulfate, a glucuronide, —OH, a bulky group, aryl, cycloalkyl, heteroaryl, heterocycloalkyl, —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, —SONH, —COOH, —CN, —CHCN—, —NHCN—, —CHO, ═CHOCH, —COO salt, —OSOalkyl, —NH, and —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, —NH, —SONH, —COOH, —CN, —CHCN, —NHCN, —CHO, —COOsalt, —OSOalkyl, —SH, —SCH, —CH[(CH)CH]COOCH, —(CH)COOCH, —(CH)—O—CH, —(CH)—O—(CH)CH, (CH)—S—CH, —(CH)—S—(CH)CH, —(CH)—NH—(CH)CH, —C-Calkenyl-O—(CH)CH, —C-Calkenyl-S—(CH)CH, —C-Calkenyl-N—(CH)CH, —C-Calkynyl-O—(CH)CH, —C-Calkynyl-S—(CH)CH, —C-Calkynyl-N—(CH)CH, —(CH)—OH, —(CH)—O—NH, —(CH)—S—NH, —NH(CH)CH, —NH(CH)OCH, —NH(CH)CHOH—COOH, —N(CH), —(CH)(NH)CHOH, —NHCOOH, —(CH)NHCOOH, —NO, —SCN, —SOalkyl, —B(OH), —(CH)N(CH)—SO—NH, —(CH)—NH—SO—NH, —NHC(═S)CH, and —NHNH; and Y is selected from hydrogen, ═O, —OCO(R) and —OH; wherein m is an integer between 0-20, n is an integer between 0-8, the symbol represents either a single or a double bond capable of forming a keto group at position 3 or 17; and the symbol 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.

US Patent:

20120071455, Mar 22, 2012

Filed:

Sep 14, 2011

Appl. No.:

13/232798

Inventors:

James G. Yarger - Cedarburg WI, US
Steven H. Nye - Mequon WI, US

International Classification:

A61K 31/56
A61P 29/00
C07J 1/00

US Classification:

514182, 552625

Abstract:

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

US Patent:

20120245131, Sep 27, 2012

Filed:

Mar 21, 2012

Appl. No.:

13/426364

Inventors:

James G. Yarger - Cedarburg WI, US
Steve Nye - Mequon WI, US

International Classification:

A61K 31/566
A61P 25/00
C12N 5/079
A61P 29/00
A61P 37/02
A61K 31/565
A61P 25/28

US Classification:

514171, 514178, 514182, 435375

Abstract:

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

US Patent:

20230097440, Mar 30, 2023

Filed:

Oct 20, 2022

Appl. No.:

17/970293

Inventors:

- Mequon WI, US
James G. Yarger - Cedarburg WI, US

International Classification:

C07J 1/00
A61K 9/00
A61P 37/00

Abstract:

Methods for modulating lipoprotein lipase (LPL) and Apoliprotein C2 (ApoC2) expression and/or activity in the treatment of peripheral and central nervous system tissue disease states with C-6 substituted estradiol derivatives are presented herein.