IP Library › Granted Patent US 7,696,190
Granted Patent B2
US 7,696,190 · App. 10/343,293 · Granted Apr 13, 2010

16Alpha-methyl or ethyl substituted estrogens

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Quick Facts
Patent No.
US 7,696,190
App. No.
10/343,293
Granted
Apr 13, 2010
Kind
B2
Abstract

The invention makes a 16α-substituted steroidal compound available having formula 1, wherein the dotted ring is a fully saturated, a fully aromatic or a saturated ring with a Δ5-10 double bond; R 1 is (C 1 -C 3 )alkyl or (C 2 -C 3 )alkenyl, and each of these groups can be substituted with one or more halogens; R 2 is (C 1 -C 4 ;)alkyl, (C 2 -C 4 )alkenyl or methylene, and each of these groups can be substituted with one or more halogens; R 3 is methyl or ethyl; or a prodrug thereof, which compound can be used for an estrogen receptor α selective treatment

Claims (9)

1. A 16α-substituted steroidal compound having formula 1,

wherein:

the dotted ring is a fully aromatic or a saturated ring with a Δ5-10 double bond;

R 1 is (C 1 -C 3 )alkyl or (C 2 -C 3 )alkenyl, and each of these groups can be substituted with one or more halogens;

R 2 is (C 1 -C 4 )alkyl, (C 2 -C 4 )alkenyl or methylene, and each of these groups can be substituted with one or more halogens;

R 3 is methyl or ethyl.

2. The 16α-substituted steroidal compound according to claim 1 , wherein the halogens in R 1 and R 2 are selected from a group consisting of chlorine and fluorine.

3. The 16α-substituted steroidal compound according to claim 1 , wherein R 2 is (C 1 -C 2 )alkyl or vinyl.

4. A pharmaceutical composition comprising: the compound according claim 1 and a pharmaceutically acceptable auxiliary.