Non-steroidal sulfatase inhibitor compounds and their method of

Details Non-steroidal sulfatase inhibitor compounds and their method of Non-steroidal sulfatase inhibitor compounds and their method of

1995-08-16

1996-10-22

O'Sullivan, Peter

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

Organic compounds

Fatty compounds having an acid moiety which contains the...

514579, 514600, 514601, 514608, 514625, 514630, 558 50, A61K 3116, A61K 31165, A61K 31185

Patent

active

055678319

ABSTRACT:
This invention discloses compounds useful as non-steroidal sulfatase inhibitors. The compounds comprise the formula (1) ##STR1## wherein (a) R.sub.1 is selected from the group consisting of hydrogen and a lower alkyl group, (b) R.sub.2 is selected from the group consisting of H and a lower alkyl group, (c) m is an integer from 0 to 4, and (d) n is an integer from 5 to 14. R.sub.1 is selected from the group consisting of H and C.sub.1 -C.sub.6 alkyl and R.sub.2 is selected from the group consisting of H and C.sub.1 -C.sub.6 alkyl. The invention also discloses methods of treating a patient prophylactically to provide protection as an estrogen depleting agent for estrogen dependent illnesses and treating a patient therapeutically for estrogen dependent diseases. A method of making the non-steroidal sulfatase inhibitors is also disclosed.

REFERENCES:
patent: 5510379 (1996-04-01), Lee et al.
Lowry, O. H. et al., "Protein Measurement With The Folin Phenol Reagent", J. Biol. Chem., pp. 265-275 (1951).
Millington, D. S., "Determination Of Hormonal Steroid Concentrations In Biological Extracts By High Resolution Mass Fragmentograph", Journal Of Steroid Biochemistry, vol. 6, pp. 239-245 (1975).
Reed, K. C. et al., "Kinetic Properties Of Human Placental Aromatase", Journal Of Biological Chemistry, vol. 251, No 6, pp. 1625-1631 (Mar. 25, 1976).
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).
Duncan, L. et al., "Inhibition Of Estrone Sulfatase Activity By Estrone-3-Methylthiophosphonate: A Potential Therapeutic Agent In Breast Cancer", Cancer Research, vol. 53, pp. 298-302 (1993).
Howarth, N. M. et al., "Phosphonates And Thiophosphonates As Sulfate Surrogates: Synthesis Of Estrone 3-Methylthiophosphonate, A Potent Inhibitor Of Estrone Sulfatase", Bioorganic & Medical Chemistry Letters, vol. 3, No. 2, pp. 313-318 (1993).
Li, Pui-Kai et al., "Synthesis And Biochemical Studies Of Estrone Sulfatase Inhibitors", Steroids, vol. 58, pp. 106-111 (Mar. 1993).
Dibbelt, L. et al., "Inhibition Of Human Placental Sterylsulfatase By Synthetic Analogs Of Estrone Sulfate", J. Steroid Biochem. Molec. Biol., vol. 50, No. 5/6, pp. 261-266 (1994).
Howarth, N. M. et al., "Estrone Sulfamates: Potent Inhibitors Of Estrone Sulfatase With Therapeutic Potential", J. Med. Chem., vol. 37, pp. 219-221 (1994).
Registry of Toxic Effects of Chemical Substances, N.I.O.S.H. RTECS Number UE5093500 (1979) from U.S. Army Armament Research and Development Command, Chemical Systems Laboratory.

Affiliated with

Also associated with

Rating

Non-steroidal sulfatase inhibitor compounds and their method of does not yet have a rating. At this time, there are no reviews or comments for this patent.

If you have personal experience with Non-steroidal sulfatase inhibitor compounds and their method of , we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Non-steroidal sulfatase inhibitor compounds and their method of will most certainly appreciate the feedback.

Rate now

Comments { 0 }

Profile ID: LFUS-PAI-O-2359592