IP Library Granted Patent US 7,868,193
Granted Patent B2
US 7,868,193 · App. 10/297,706 · Granted Jan 11, 2011

16,17-carbocyclic condensed steroid compounds having selective estrogenic activity

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Quick Facts
Patent No.
US 7,868,193
App. No.
10/297,706
Granted
Jan 11, 2011
Kind
B2
Abstract

The invention discloses a steroid compound having the formula (1), wherein dotted bonds represent optional double bonds; R 6 is H, ═CH 2 , or —CH 3 , or —CH 2 —CH 3 ; R 7 is H, C 1-4 -alkyl, C 2-5 alkenyl or C 2-5 -alkynyl, wherein the alkyl, alkenyl or alkynyl group may be substituted with 1 to 3 halogen atoms independently chosen from the group of fluorine or chlorine atoms; R 11 is H, C 1-4 -alkyl, C 2-4 -alkenyl, C 2-4 -alkynyl or C 1-4 -alkylidene, wherein the alkyl, alkenyl, alkynyl or alkylidene group may be substituted with 1-3 halogen atoms independently chosen from the group of fluorine or chlorine atoms; E represents together with carbon atoms 16 and 17 of the steroid skeleton a four to seven-membered ring, said ring being α and in cis-configuration with respect to the steroid skeleton, optionally comprising one or two endocyclic bonds; or a prodrug thereof. Such compounds can be used in therapy and for methods for selective modification of the activity of estrogen receptors.

Claims (7)

1. A compound according to formula 2:

2. A steroid compound having formula 1:

wherein R 7 is H, R 11 is C 3 H 7 and n is 0.

3. A pharmaceutical composition, comprising:

the steroid compound according to claim 1 and a pharmaceutically acceptable auxiliary.

4. A pharmaceutical composition, comprising:

the steroid compound according to claim 2 and a pharmaceutically acceptable auxiliary.

Assignments (5)
MERGER Recorded Mar 8, 2013
From: ORGANON BIOSCIENCES NEDERLAND B.V.
To: MERCK SHARP & DOHME B.V.
Reel/Frame 029940/0296 →
MERGER Recorded Mar 7, 2013
From: MSD OSS B.V.
To: ORGANON BIOSCIENCES NEDERLAND B.V.
Reel/Frame 029939/0001 →
MERGER Recorded Dec 1, 2011
From: N.V. ORGANON
To: MSD OSS B.V.
Reel/Frame 027307/0482 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 30, 2007
From: AKZO NOBEL N.V.
To: N.V. ORGANON
Reel/Frame 018816/0737 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 6, 2002
From: LOOZEN, HUBERT JAN JOSEF
To: AKZO NOBEL N.V.
Reel/Frame 014212/0417 →