Halogenated sulphamate-, phosphonate-, thiophosphonate-,...

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Cyclopentanohydrophenanthrene ring system doai

Reexamination Certificate

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Details

C552S626000

Reexamination Certificate

active

06858597

ABSTRACT:
A compound is described. The compound has the formula (Ia) as presented in the FIG.1;wherein: X is a ring having at least 4 atoms in the ring; K is hydrocarbyl group; Rh1 is an optional halo group; Rh2 is an optional halo group; at least one of Rh1 and Rh2 is present; Rs is any one of a sulphamate group, a phosphonate group, a thiophosphonate group, a sulphonate group or a sulphonamide group. The compound is capable of inhibiting steroid sulphatase (STS) activity.

REFERENCES:
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patent: WO9927936 (1999-06-01), None
Purohit et al., “The Development of A-Ring Modified Analogues of Oestrone-3-0-Sulphamate as Potent Steroid Sulphatase Inhibitors with Reduced Oestrogenicity”, Journal of Steroid Biochem . . . , vol. 64, no 5, pp. 269-275, 1998 (XP000852539).
Woo et al., “Heteroatom-substituted analogues of the active-site directed inhibitor estra-1,3,5(10)-trein-17-one-3-sulphamate inhibit estrone sulphatase by a different mechanism”, Journal of Steroid Biochem . . . , vol 57 no 1-2, pp. 79-88, 1996 (XP002164108) Abstract.
Purohit et al., “Inhibition of steroid sulphatase activity by steroidal methylthiophosphonates: Potential therapeutic agents in breast cancer”, Journal of Steroid Biochem., vol 48 no 5-6, pp. 523-527, 1994 (XP002164109) Abstract.
Howart et al., “PHosphonates and thiophosphonates as sulfate surrogates: Synthesis of estrone 3-methylthiophosphonate, a potent inhibitor of estrone sulfatase.”, Bioorganic & Medicinal , vol. 3, No. 2 pp. 313-318, 1993 (XP002164110) Abstract.
Townsley J.D., “Furhter, Studies on the Regulation of Human Placental Steroid 3-Sulfatase Activity”, Endocrinology, vol. 93, No. 1, pp. 172-181, 1973 (XP002068155).
Horwitz et al., “In vitro inhibition of estrogen sulfoconjugation by some 2- and 4- substituted estra-1, 3, 5(10)-trein-17.beta.-ols”, J. Med. Chem., vol. 29, pp. 692-698, 1986 (XP002164107).

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