Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Reexamination Certificate
2001-04-04
2002-09-24
Powers, Fiona T. (Department: 1626)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
C514S428000, C514S567000, C548S543000, C548S576000
Reexamination Certificate
active
06455572
ABSTRACT:
FIELD OF THE INVENTION
This invention relates to compounds that are mammalian metabolites of (−)-cis-6-phenyl-5-[4-(2-pyrrolidin-1-yl-ethoxy)-phenyl]-5,6,7,8-tetrahydro-naphthalene-2-ol. The compounds of the invention are useful as standards in analytical assays and as therapeutic agents.
BACKGROUND OF THE INVENTION
Pharmacologically, (−)-cis-6-phenyl-5-[4-(2-pyrrolidin-1-yl-ethoxy)-phenyl]-5,6,7,8-tetrahydro-naphthalene-2-ol (PPTN) is an estrogen agonist/antagonist that is disclosed in U.S. Pat. No. 5,552,412. An “estrogen agonist/antagonist” is compound that affects some of the same receptors that estrogen does, but not necessarily all, and in some instances, it antagonises or blocks estrogen. It is also known as a “selective estrogen receptor modulator” (SERM). Estrogen agonists/antagonists may also be referred to as antiestrogens although they have some estrogenic activity at some estrogen receptors. Estrogen agonists/antagonists are therefore not what are commonly referred to as “pure antiestrogens”. Antiestrogens that can also act as agonists are referred to as Type I antiestrogens. Type I antiestrogens activate the estrogen receptor to bind tightly in the nucleus for a prolonged time but with impaired receptor replenishment (Clark, et al.,
Steroids
1973;22:707; Capony, et al.,
Mol Cell Endocrinol
, 1975;3:233).
The compounds of the present invention are metabolites of PPTN and are believed to possess significant pharmacological activities similar or identical to those possessed by the parent compound; PPTN.
REFERENCES:
patent: 3277106 (1966-10-01), Bencze et al.
patent: 5552412 (1996-09-01), Cameron et al.
patent: 5889042 (1999-03-01), MacLeon et al.
patent: 5948809 (1999-09-01), Chiu et al.
patent: 6107331 (2000-08-01), MacLean et al.
patent: 6153622 (2000-11-01), Cameron et al.
patent: 6204286 (2001-03-01), Cameron et al.
patent: 0995748 (2000-04-01), None
Day Wesley W.
Eggler James F.
Johnson Kim A.
Prakash Chandra A.
Benson Gregg C.
Crissey Todd M.
Pfizer Inc.
Powers Fiona T.
Richardson Peter C.
LandOfFree
Estrogen agonist/antagonist metabolites does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Estrogen agonist/antagonist metabolites, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Estrogen agonist/antagonist metabolites will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-2887128