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1. WO1996005216 - ESTRA-1,3,5(10)-TRIENE DERIVATIVES, METHODS OF PREPARING SUCH COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM

Publication Number WO/1996/005216
Publication Date 22.02.1996
International Application No. PCT/DE1995/000877
International Filing Date 03.07.1995
Chapter 2 Demand Filed 19.12.1995
IPC
C07J 41/00 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
JSTEROIDS
41Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
C07J 43/00 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
JSTEROIDS
43Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopentahydrophenanthrene skeleton
C07J 51/00 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
JSTEROIDS
51Normal steroids with unmodified cyclopentahydrophenanthrene skeleton not provided for in groups C07J1/-C07J43/151
C07J 53/00 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
JSTEROIDS
53Steroids in which the cyclopentahydrophenanthrene skeleton has been modified by condensation with carbocyclic rings or by formation of an additional ring by means of a direct link between two ring carbon atoms
CPC
A61P 15/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
15Drugs for genital or sexual disorders
A61P 15/18
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
15Drugs for genital or sexual disorders
18Feminine contraceptives
C07J 41/0072
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
JSTEROIDS
41Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
0033not covered by C07J41/0005
0072the A ring of the steroid being aromatic
C07J 43/003
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
JSTEROIDS
43Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton
003not condensed
C07J 51/00
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
JSTEROIDS
51Normal steroids with unmodified cyclopenta(a)hydrophenanthrene skeleton not provided for in groups C07J1/00 - C07J43/00
C07J 53/004
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
JSTEROIDS
53Steroids in which the cyclopenta(a)hydrophenanthrene skeleton has been modified by condensation with a carbocyclic rings or by formation of an additional ring by means of a direct link between two ring carbon atoms, ; including carboxyclic rings fused to the cyclopenta(a)hydrophenanthrene skeleton are included in this class
002Carbocyclic rings fused
0043 membered carbocyclic rings
Applicants
  • JENAPHARM GMBH [DE/DE]; Otto-Schott-Strasse 15 D-07745 Jena, DE (AllExceptUS)
  • SIEMANN, Christel [DE/DE]; DE (UsOnly)
  • SCHWARZ, Sigfrid [DE/DE]; DE (UsOnly)
  • ELGER, Walter [DE/DE]; DE (UsOnly)
  • REDDERSEN, Gudrun [DE/DE]; DE (UsOnly)
  • SCHNEIDER, Birgitt [DE/DE]; DE (UsOnly)
Inventors
  • SCHWARZ, Sigfrid; DE
  • ELGER, Walter; DE
  • REDDERSEN, Gudrun; DE
  • SCHNEIDER, Birgitt; DE
  • SIEMANN, Hans-Joachim; null
Agents
  • WABLAT, Wolfgang; Potsdamer Chaussee 48 D-14129 Berlin, DE
Priority Data
P 44 29 397.609.08.1994DE
Publication Language German (DE)
Filing Language German (DE)
Designated States
Title
(DE) ESTRA-1,3,5(10)-TRIEN-DERIVATE, VERFAHREN ZU IHRER HERSTELLUNG UND DIESE VERBINDUNGEN ENTHALTENDE PHARMAZEUTISCHE ZUSAMMENSETZUNGEN
(EN) ESTRA-1,3,5(10)-TRIENE DERIVATIVES, METHODS OF PREPARING SUCH COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
(FR) DERIVES ESTRA-1,3,5(10)-TRIENE, LEURS PROCEDES DE PREPARATION ET COMPOSITIONS PHARMACEUTIQUES LES CONTENANT
Abstract
(DE)
Die Erfindung betrifft neue Estra-1,3,5(10)-trien-Amidosulfamate, welche an der 3-Position eine R-SO2-O-Gruppe tragen, wobei R eine R1R2N-Gruppe ist, worin R1 und R2 unabhängig voneinander ein Wasserstoffatom, einen Alkylrest mit 1-5 C-Atomen oder zusammen mit dem N-Atom einen Polymethyleniminorest mit 4 bis 6 C-Atomen oder einen Morpholinorest bedeuten. Die erfindungsgemäßen Verbindungen sind zur hormonalen Kontrazeption und in der klimakterischen Hormon-Replacement-Therapie (HRT) sowie zur Behandlung gynäkologischer und andrologischer Krankheitsbilder geeignet. Daher weisen die erfindungsgemäßen Verbindungen nur eine geringe hepatische Estrogenität auf. Ferner werden Verfahren zur Herstellung der erfindungsgemäßen Verbindungen beschrieben, sowie zur Herstellung pharmazeutischer Zusammensetzungen.
(EN)
The invention concerns novel estra-1,3,5(10)-triene amidosulphamates with an R-SO2-O- group in the 3-position, R being an R1R2N- group in which R1 and R2, independently of each other, are a hydrogen atom, an alkyl group with 1 to 5 C-atoms or, together with the N-atom, a polymethyleneimino group with 4 to 6 C-atoms or a morpholino group. The compounds described are suitable for use in hormonal contraception and in climacteric hormone-replacement therapy (HRT), as well as in the treatment of gynaecological and andrological conditions. The compounds described thus only have a low hepatic oestrogenicity. Also described are methods of preparing the compounds described, plus the preparation of pharmaceutical compositions containing them.
(FR)
L'invention concerne de nouveaux estra-1,3,5,(10)-triène-amidosulfamates, qui présentent un groupe R-SO2-O- en position 3, R étant un groupe R1R2N où R1 et R2 désignent indépendamment l'un de l'autre un atome d'hydrogène, un reste alkyle ayant entre 1 et 5 atomes de C ou conjointement avec l'atome de N, un reste polyméthylènimino ayant entre 4 et 6 atomes de C ou un reste morpholino. Ces composés s'utilisent dans la contraception hormonale et dans l'hormonothérapie climatérique de substitution, ainsi que dans le traitement de syndromes gynécologiques et andrologiques. Ces composés ne présentent de ce fait qu'une ÷strogénicité hépatique réduite. L'invention concerne en outre des procédés de préparation desdits composés, ainsi que des procédés de préparation de compositions pharmaceutiques les contenant.
Also published as
CZPV1997-274
FI970526
NZ289793
US08750943
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