The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.

The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.

Date of Patent:
Oct. 25, 2005

Filed:

Nov. 02, 2000
Applicants:

Alexander Hillisch, Jena, DE;

Werner Boidol, Berlin, DE;

Wolfgang Schwede, Berlin, DE;

Peter Esperling, Berlin, DE;

Gerhard Sauer, Berlin, DE;

Christa Hegele-hartung, Muelheim/Ruhr, DE;

Uwe Kollenkirchen, Berlin, DE;

Karl-heinrich Fritzemeier, Berlin, DE;

Inventors:

Alexander Hillisch, Jena, DE;

Werner Boidol, Berlin, DE;

Wolfgang Schwede, Berlin, DE;

Peter Esperling, Berlin, DE;

Gerhard Sauer, Berlin, DE;

Christa Hegele-Hartung, Muelheim/Ruhr, DE;

Uwe Kollenkirchen, Berlin, DE;

Karl-Heinrich Fritzemeier, Berlin, DE;

Assignee:

Schering, AG, Berlin, DE;

Attorney:
Primary Examiner:
Int. Cl.
CPC ...
A61K031/56 ; C07J001/00 ;
U.S. Cl.
CPC ...
Abstract

The invention relates to novel 18-norsteroids (gonatrienes) of general formula (I), wherein R, R, R, R, R, R, R, R, R, R, R, R, R, Rand Rhave the meaning cited in the description, and to the use of said compounds as pharmaceutical active ingredients. Said compounds exhibit a high affinity in vitro for estrogen receptor preparations of rat prostate and in an estrogen receptor preparation of rat uterus. Said compounds exhibit in vivo preferential activity on bones as compared to the uterus and/or significant activity with regard to stimulating the expression of 5HT2a-receptors and transporter molecules. The invention also relates to the production of said compounds, therapeutic use and galenic form of said compounds contained in the novel compounds of invention. The invention also relates to utilization of steroids based on the gonatriene molecular skeleton in order to treat estrogen deficiency-induced diseases and disorders, in addition to the use of said gonatriene structural component in the total structure of compounds which dissociate to produce enhanced estrogen activity in bone as compared to the uterus


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