Novel, orally active androgens are 7&agr;-substituted &Dgr;
14
-nandrolone derivatives. The compounds satisfy the general formula:
1
wherein
R
1
is O, (H,H), (H,OR), NOR, with R being hydrogen, (C
1-6
) alkyl, or (C
1-6
) acyl;
R
2
is selected from the group consisting of (C
2-4
) alkyl, (C
2-4
) alkenyl, or (C
2-4
) alkynyl, each optionally substituted by halogen; or
R
2
is cyclopropyl, or cyclopropenyl, each optionally substituted by (C
1-2
) alkyl, or halogen;
R
3
is hydrogen, (C
1-2
) alkyl, or ethenyl;
R
4
is (C
1-2
) alkyl;
R
5
is hydrogen, or (C
1-15
) acyl;
and the dotted lines indicate optional bonds.
The disclosed invention relates to the unexpected finding of novel steroids which are characterized by a 14&bgr;,15&bgr;-cyclopropane ring and a 17&agr; hydroxymethyl group. These steroids according to the invention are found to have in common an androgenic activity. They can be used for the preparation of an agent for male contraception, as well as for the preparation of a medicament for the treatment of androgen insufficiency.
Process and new intermediates for the preparation of steroids with a progestogen activity
申请人:Grisenti Paride
公开号:US20050234251A1
公开(公告)日:2005-10-20
The present invention relates to a new process of synthesis and to some new intermediates for the preparation of steroids with progestogen activity, more particularly, for the preparation of Desogestrel of formula (1). Said process is characterized by the regioselective reduction of the compound of formula (II) to give the intermediate of formula (III).
14(15)-unsaturated 15- and/or 16-substituted androgens with mixed androgen-progrestational profile
申请人:——
公开号:US20040059140A1
公开(公告)日:2004-03-25
Disclosed are androgen-related steroids having a &Dgr;14 double bond and carrying a substituent at either or both of the carbon atoms nos. 15 and 16. The present steroids are characterized by possessing a mixed profile of androgenic and progestagenic activities. This makes these compounds suitable for male or female hormone replacement therapy, as well as male contraception.
Verfahren zur Steigerung von Enzym-Aktivitäten und der Syntheseleistung von Mikroorganismen und höheren Pflanzen
申请人:SCHERING AKTIENGESELLSCHAFT
公开号:EP0325933A1
公开(公告)日:1989-08-02
Ein Verfahren zur Steigerung von Enzym-Aktivitäten und der Syntheseleistung von Organismen wird beschrieben, welches dadurch gekennzeichnet ist, daß man dieselben mit inaktivierten Elicitoren-haltigen Mikrrorganismen, Fragmenten derselben oder Exkretionen Elicitoren-haltiger Mikroorganismen in Kontakt bringt, mit der Maßgabe, daß man zur Steigerung von Enzym-Aktivitäten und der Syntheseleistung nicht-mikrobieller Organismen inaktivierte Elicitoren-haltige Baktrien, Fragmente derselben oder Exkretionen Elicitoren-haltiger Bakterien verwendet. Das erfindungsgemäße Verfahren ermöglicht es, beispielsweise die Syntheseleistung von Farbstoffe, Antibiotika, Alkaloide oder Phytoalexine bildenden Mikroorganismen oder Pflanzen zu steigern oder die Enzymaktivitäten von zur Steroidtransformation befähigten Mikroorganismen zu erhöhen.