Pfizer Corporation

Wesley W Day

David D Thompson

Andrew G Lee

James F Eggler

Chandra A Prakash

Kim A Johnson

Robert L Rosati

This invention relates to compounds that are mammalian metabolites of (&#x2212;)-cis-6-phenyl-5-[4-(2-pyrrolidin-1-yl-ethoxy)-phenyl]-5,6,7,8-tetrahydro-naphthalene-2-ol. The compounds of the invention can be used as standards for analytical assays or as intermediates for the further chemical synthesis or biosynthesis of chemical entities. The invention also relates to pharmaceutical compositions for the treatment of disease and methods of treating disease.

Estrogen agonist/antagonist metabolites

This invention relates to methods, pharmaceutical compositions and kits useful in promoting bone formation and/or preventing bone loss and lowering blood cholesterol. The compositions are comprised of an estrogen agonist/antagonist as a first active component and a statin as a second active component and a pharmaceutically acceptable vehicle, carrier or diluent. The compositions and methods of treatment are effective while substantially reducing the concomitant liability of adverse effects associated with estrogen administration.

Compositions and methods for treating osteoporosis and lowering cholesterol

This invention relates to methods, pharmaceutical compositions and kits useful in treating conditions responsive to estrogen by the administration of estrogen agonists/antagonists. Conditions responsive to the compositions and methods include rheumatoid arthritis, colon cancer, tissue wounds, skin wrinkles and cataracts. The compositions are comprised of an estrogen agonist/antagonist and a pharmaceutically acceptable vehicle, carrier or diluent. The compositions and methods of treatment are effective while substantially reducing the concomitant liability of adverse effects associated with estrogen administration.

Compositions and methods for treating conditions responsive to estrogen

The present invention provides methods and kits for improving or maintaining vascular health, including preventing myocardial infarction or stroke; maintaining or improving vascular reactivity; treating acute or chronic renal failure, peripheral arterial occlusive disease, coronary artery disease, or Raynaud's phenomenon; or lowering plasma levels of Lp(a) using an estrogen agonist/antagonist.

Methods and kits for improving vascular health

This invention relates to methods and pharmaceutical compositions useful in the treatment of conditions that are responsive to the elevation of testosterone levels in the body and the use of estrogen agonists/antagonists for the manufacture of medicaments for the treatment of conditions that are responsive to the elevation of testosterone levels in the body. The compositions are comprised of an estrogen agonist/antagonist and a pharmaceutically acceptable vehicle, carrier or diluent. These compositions are effective in treating male subject sexual dysfunction and timidity in female subjects including post-menopausal women and are effective in increasing libido in female subjects including post-menopausal women. In the case of male subject sexual dysfunction, the compositions may also include a compound which is an elevator of cyclic guanosine 3&prime;,5&prime;-monophosphate (cGMP). Additionally, the compositions are effective in other conditions whose etiology is a result of testosterone deficiency or which can be ameliorated by increasing testosterone levels within the body. Methods of the invention include the treatment of conditions that are responsive to elevation of testosterone levels such as treating male subject sexual dysfunction and timidity in female subjects including post-menopausal women and the increase of libido of female subjects including post-menopausal women. The methods of treatment are effective while substantially reducing the concomitant liability of adverse effects associated with testosterone administration.

Methods of treatment for premature ejaculation in a male

This invention relates to compounds that are mammalian metabolites of (&minus;)-cis-6-phenyl-5-&lsqb;4-(2-pyrrolidin-1-yl-ethoxy)-phenyl&rsqb;-5,6,7,8-tetrahydro-naphthalene-2-ol. The compounds of the invention can be used as standards for analytical assays or as intermediates for the further chemical synthesis or biosynthesis of chemical entities. The invention also relates to pharmaceutical compositions for the treatment of disease and methods of treating disease.

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Old Lyme, CT, United States of America

Wesley W Day