Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Cyclopentanohydrophenanthrene ring system doai
Patent
1996-02-27
1997-10-14
Reamer, James H.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Cyclopentanohydrophenanthrene ring system doai
552303, 514177, C07J 4100, A61K 31565
Patent
active
056772920
ABSTRACT:
This invention discloses compounds useful as steroid sulfatase inhibitors. The compounds comprise the formula (1) ##STR1## wherein (a) R is selected from the group consisting of hydrogen, a lower alkyl group, an alkoxy group, halogen, NH.sub.2, NO.sub.2, C.tbd.N and N.dbd.C.dbd.S; and (b) the ring system ABCD is a steroid nucleus selected from the group consisting of estrone, dehydroepiandrosterone, estradiols, estradiolesters, pregnenolone, substituted estrones, substituted dehydroepiandrosterones, substituted estradiols, substituted estradiolesters and substituted pregnenolone. The compounds also comprise the formula (5) ##STR2## wherein (a) R.sub.1 is hydrogen and R.sub.2 is selected from the group consisting of SO.sub.2 CF.sub.3, SO.sub.2 NH.sub.2, SO.sub.2 (C.sub.1 -C.sub.6 -alkyl), COCF.sub.3, CONH.sub.2, CO(C.sub.1 -C.sub.6 -alkyl); and (b) the ring system ABCD is a steroid nucleus selected from the group consisting of estrone, dehydroepiandrosterone, estradiol, estradiolester, pregnenolone, substituted estrones, substituted dehydroepiandrosterone, substituted estradiols, substituted estradiolesters and substituted pregnenolone. The invention also discloses methods of treating a patient therapeutically and prophylactically for estrogen dependent diseases with the compounds of this invention.
REFERENCES:
Vignon, F. et al., "effects Of Plasma Estrogen Sulfates In Mammary Cancer Cells", Endocrinology, vol. 106, pp. 1079-1086 (1980).
Wilking, N. et al., "Oestrogen Receptors And Metabolism Of Oestrone Sulphate In Human Mammary Carcinoma", Eur. J. Cancer, vol. 16, pp. 1339-1344 (1980).
Bradlow, H.L., "A Reassessment Of The Role Of Breast Tumor Aromatization", Cancer Research (Suppl.), vol. 42, pp. 3382s-3386s (1982).
Reed, M.J. et al., "Sulphatase Inhibitors: The Rationale For The Development Of A New Endocrine Therapy", Reviews On Endocrine-Related Cancer, vol. 45, pp. 51-62 (1993).
Howarth, N.M. et al., "Estrone Sulfamates: Potent Inhibitors Of Estrone Sulfatase With Therapeutic Potential", J. Med. Chem., vol. 37, pp.219-221 (1994).
Santner, S.J. et al., "In situ Estrogen Production Via The Estrone Sulfatase Pathway In Breast Tumors: Relative Importance versus The Aromatase Pathway", Journal of clinical Endocrinology and Metabolism, vol. 59, No. 1, pp. 29-33 (1984).
Santen, R.J. et al., "Enzymatic Control Of Estrogen Production In Human Breast Cancer: Relative Significance Of Aromatase versus Sulfatase Pathways", Annals New York Academy Of Sciences, vol. 464, pp. 126-137 (1986).
Pasqualini, J.R. et al., "Importance Of Estrogen Sulfates In Breast Cancer", J. Steroid Biochem., vol. 34, Nos. 1-6, pp. 155-163 (1989).
Li Pui-Kai
Selcer Kyle W.
Duquesne University of the Holy Ghost
Reamer James H.
LandOfFree
Derivatives of estra 1,3,5(10)triene-17-one,3-amino compounds an does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Derivatives of estra 1,3,5(10)triene-17-one,3-amino compounds an, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Derivatives of estra 1,3,5(10)triene-17-one,3-amino compounds an will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-1555410