11-(substituted phenyl)-estra-4,9-diene derivatives

C - Chemistry – Metallurgy – 07 – J

Patent

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C07J 17/00 (2006.01) A61K 31/565 (2006.01) A61K 31/575 (2006.01) A61K 31/58 (2006.01) A61P 5/44 (2006.01) A61P 25/00 (2006.01) C07J 1/00 (2006.01) C07J 7/00 (2006.01) C07J 9/00 (2006.01) C07J 21/00 (2006.01) C07J 33/00 (2006.01) C07J 41/00 (2006.01) C07J 71/00 (2006.01) C07J 75/00 (2006.01)

Patent

CA 2182771

The invention relates to a 11-(substituted phenyl)-estra-4,9-dime derivative of formula I Image wherein A is a residue of a 5- or 6-membered ring containing 2 heteroatoms which are not connected to each other and independently selected from O and S, the ring being optionally substituted with one or more halogen atoms, or A is a residue of a 5- or 6-membered ring wherein no double C-C bonds are present, containing 1 heteroatom selected from O and S, which heteroatom is connected to the phenyl group at the position indicated with an asterisk, the ring being optionally substituted with one or more halogen atoms; R1 is H or 1-oxo(1-4C)alkyl; R2 is H, (1-8C)alkyl, halogen or CF3; X is selected from (H,OH), O, and NOH; and the interrupted line represents an optional bond. The compounds of the invention have anti-glucocorticoid activity and can be used in treating or preventing glucocorticoid-dependent diseases.

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