Oestrogen derivatives as inhibitors of steroid sulphatase

Details Oestrogen derivatives as inhibitors of steroid sulphatase Oestrogen derivatives as inhibitors of steroid sulphatase

2011-02-22

2011-02-22

Lundgren, Jeffrey S (Department: 1613)

Organic compounds -- part of the class 532-570 series

Organic compounds

Cyclopentanohydrophenanthrene ring system containing

C552S626000, C552S631000

Reexamination Certificate

active

07893284

ABSTRACT:
The present invention provides a compound comprising a steroidal ring system and an optional group R1selected from any one of —OH, a sulphamate group, a phosphonate group, a thiophosphonate group, a sulphonate group or a sulphonamide group; wherein the D ring of the steroidal ring system is substituted by a group R2of the formula -L-R3, wherein L is an optional linker group and R3is selected from groups which are or which comprise one of a nitrite group, an alcohol, an ester, an ether, an amine and an alkene, provided that when R3is or comprises an alcohol, L is present; and wherein the A ring of the steroidal ring system is substituted at position 2 or 4 with a group R4, wherein R4is a hydrocarbyl group.

REFERENCES:
patent: 4994439 (1991-02-01), Longenecker et al.
patent: 6046186 (2000-04-01), Tanabe et al.
patent: 6436917 (2002-08-01), Droescher et al.
patent: 2007/0225256 (2007-09-01), Leese et al.
patent: 1284272 (2003-02-01), None
patent: 2002-510295 (2002-04-01), None
patent: 99/27936 (1999-07-01), None
patent: 99/33858 (1999-07-01), None
patent: 99/64013 (1999-12-01), None
patent: 00/43408 (2000-07-01), None
patent: 00/66095 (2000-11-01), None
patent: WO 01/85755 (2001-11-01), None
patent: 02/16392 (2002-02-01), None
patent: WO 02/16395 (2002-02-01), None
patent: WO 02/062347 (2002-08-01), None
J.R. Bull and AJ. Hodgkinson, Steroidal Analogues of Unnatural Configuration—VIII, 29 Tetrahedron 1109 (1973).
G. Hobe, et al, Species Differences in Biotransformation of 17a-cyanomethylestradiol 3-methyl ether, 36 Steroids 131 (1980).
Roch P. Boivin, et al “Structure-Activity Relationships of 17 α-Derivatives of Estradiol as Inhibitors of Steriod Sulfatase” 43 J. Med Chem (2000): 4465-4478.
Lucy MacCarthy-Morrogh, et al “Differential Effects of Estrone and Estrone-3-O-Sulfamate Derivatives on Mitotic Arrest, Apoptosis, and Microtubule Assembly in Human Breast Cancer Cells” 60 Cancer Research (2000): 5441-5450.
G. Hobe, et al “Species Differences in Biotranformation of 17 α-Cyanomethylestradiol 3-Methyl Ester” 36 Steroids (1980): 131-147.
Y. Hirmai, et al “Synthesis and Antimicrobial Activities of Some Steroidal Amines” 39 Agr. Biol. Chem. (1975): 843-850.

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