IP Library Granted Patent US 7,763,596
Granted Patent B2
US 7,763,596 · App. 11/737,185 · Granted Jul 27, 2010

Selective glucocorticoid receptor agonists

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Quick Facts
Patent No.
US 7,763,596
App. No.
11/737,185
Granted
Jul 27, 2010
Kind
B2
Abstract

This invention is directed to a method for treating an inflammatory condition, treating haematological and other malignancies, causing immunosuppression, or preventing or treating transplant rejection in man or other animals which comprises administering to a patient a compound that has the structure of Formula (I) or Formula (II) as defined below, or a pharmaceutically acceptable derivative thereof or pro-drug therefor, wherein R═NH 2 , NHR 1 , NHOR 2 , NHNHR 2 , NHCOR 2 , and R 1 ═C (1-4) alkyl, C (3-6) cycloalkyl, C n , where n=1-3, R 2 =methyl, ethyl, R 3 =alkyl, cycloalkyl, substituted alkyl, substituted cycloalkyl, aryl, heteroaryl, substituted aryl, or substituted hetrecoaryl; wherein R 4 , R 5 ═C (1-4) alkyl. Novel compounds according to Formula (III), wherein R 6 and R 7 are any of H, CH 3 CO, CH 3 CH 2 CO, CH 3 CH 2 CH 2 CO provided that R 6 and R 7 are not both H, or Formula (IV), wherein R 8 and R 9 are any of H, CH 3 CO, CH 3 CH 2 CO or CH 3 CH 2 CH 2 CO, having use in such methods, are also described.

Claims (6)

1. A pharmaceutical composition which comprises a compound according to Formula I and a pharmaceutically acceptable carrier:

wherein R is H 2 C—O—C(O)—NHR 3 and R 3 is selected from a benzyl or a substituted benzyl group.

2. The pharmaceutical composition of claim 1 wherein the substituted benzyl group is a halobenzyl group.

3. The pharmaceutical composition of claim 2 wherein the halobenzyl group is a fluorobenzyl.

4. A pharmaceutical composition which comprises a compound selected from the following:

and a pharmaceutically acceptable carrier.