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WO1992010194A1 - Utilisation d'antigestagenes pour la production de medicaments - Google Patents

Utilisation d'antigestagenes pour la production de medicaments Download PDF

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Publication number
WO1992010194A1
WO1992010194A1 PCT/EP1991/002358 EP9102358W WO9210194A1 WO 1992010194 A1 WO1992010194 A1 WO 1992010194A1 EP 9102358 W EP9102358 W EP 9102358W WO 9210194 A1 WO9210194 A1 WO 9210194A1
Authority
WO
WIPO (PCT)
Prior art keywords
treatment
antigestagens
sperm
antigestagenes
ejakulat
Prior art date
Application number
PCT/EP1991/002358
Other languages
German (de)
English (en)
Inventor
Chander P. Puri
Original Assignee
Schering Aktiengesellschaft Berlin Und Bergkamen
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Schering Aktiengesellschaft Berlin Und Bergkamen filed Critical Schering Aktiengesellschaft Berlin Und Bergkamen
Publication of WO1992010194A1 publication Critical patent/WO1992010194A1/fr

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Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/565—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol

Definitions

  • the present invention relates to the use of antigestagens (competitive progesterone antagonists) for the production of medicaments for controlling male fertility and / or for the treatment of andrological clinical pictures.
  • RU 486 11ß- [4-N, N- (Dimethylamino) phenyl] -17ß-hydroxy-17 ⁇ -propynyl-estra-4,9 (10) -dien-3-one; EP-A-0057115) and others 11ß -aryl- or 11ß.l9-arylene-substituted steroids are substances that can displace progesterone and glucocorticoids from their respective receptors. Pharmacologically, these substances are characterized by strong progesterone and glucocorticoid antagonistic effects. These properties determine the therapeutic application so far practiced. EU 486 is e.g. as a progesterone antagonist for the therapeutic termination of pregnancy, but also as a glucocorticoid antagonist for the treatment of
  • Cushing's syndrome used in the wake of a pathologically increased secretory activity of the adrenal cortex.
  • antigestagens competitive progesterone antagonists
  • FSH pituitary hormone
  • Blood sample collection Every fifth day, before, during and after the treatment period. Two samples (10:00 a.m. and 10:00 p.m.) were taken on the day of blood collection.
  • Morphological abnormalities such as spiral tails and defective sperm heads
  • Testosterone didhydrotestosterone and FSH. The diurnal rhythm of testosterone and dihydrotestosterone levels is not affected.
  • Ejaculate volume, ejaculate weight, sperm concentration per ejaculate, volume concentration of the sperm and the motility of the sperm of the animals in the treated and in the control group are shown in the following Tables 1-6.
  • Prostate hypertrophy and prostate cancer the observed phenomena can only be explained by inhibitory effects in the accessory sex glands, which also includes the prostate.
  • Trigger menstruation a reversible inhibition of male fertility is achieved.
  • progestogen receptor progesterone receptor
  • the antigestagens can be used according to different treatment regimens.

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)

Abstract

Des antigestagènes (antagonistes compétitifs de la progestérone) inhibent de manière réversible à des doses très faibles différents paramètres de la fonction sexuelle masculine et sont utiles pour produire des médicaments réducteurs de la fertilité masculine et/ou de traitement d'états pathologiques andrologiques.
PCT/EP1991/002358 1990-12-07 1991-12-09 Utilisation d'antigestagenes pour la production de medicaments WO1992010194A1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DEP4039561.8 1990-12-07
DE19904039561 DE4039561A1 (de) 1990-12-07 1990-12-07 Verwendung von antigestagenen zur herstellung von arzneimitteln

Publications (1)

Publication Number Publication Date
WO1992010194A1 true WO1992010194A1 (fr) 1992-06-25

Family

ID=6420084

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP1991/002358 WO1992010194A1 (fr) 1990-12-07 1991-12-09 Utilisation d'antigestagenes pour la production de medicaments

Country Status (4)

Country Link
CN (1) CN1063040A (fr)
DE (1) DE4039561A1 (fr)
PT (1) PT99724B (fr)
WO (1) WO1992010194A1 (fr)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1994027610A1 (fr) * 1993-05-28 1994-12-08 Schering Aktiengesellschaft Agents contenant un compose a action anti-androgene ainsi qu'un compose a action competitive antagoniste de la progesterone
EP2664325A1 (fr) * 2012-05-16 2013-11-20 PregLem S.A. Procédés de prévention ou de traitement des maladies induites par les androgènes

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
UY27301A1 (es) * 2001-05-25 2003-02-28 Schering Ag Uso y composiciones de antiprogestinas para el tratamiento de enfermedades de la próstata

Non-Patent Citations (5)

* Cited by examiner, † Cited by third party
Title
CHEMICAL ABSTRACTS, Vol. 109, Nr. 25, 19 December 1988, (Columbus, Ohio, US), LINDZEY J. et al., "Effects of Progestins on Sexual Behaviour in Castrated Lizards (Cnemidophorus Inornatus)", page 521, Abstract 227150s; & J. ENDOCRINOL., 1988, 119(2), 265-273. *
CHEMICAL ABSTRACTS, Vol. 113, Nr. 2, 9 July 1990, (Columbus, Ohio, US), KHOLKUTE S.D. et al., "Suppression of Bioactive Luteinizing Hormone and Testosterone by a Progesterone Antagonist ZK 98734 in Adult Male Common Marmosets, Callithrix Jaccus", page 82, Abstract 52723j; & BIOL. REPROD., 1990, 42(56), 808-814. *
CHEMICAL ABSTRACTS, Vol. 114, Nr. 5, 4 February 1991, (Columbus, Ohio, US), VAN DER SCHOOT P. et al., "Effects of Treatment of Male and Female Rats in Infancy With Mifepristone on Reproductive Function in Adulthood", page 94, Abstract 36156s; & J. REPROD. FERTIL., 1990, 90(1), 255-266. *
CHEMICAL ABSTRACTS, Vol. 116, Nr. 5, 3 February 1992, (Columbus, Ohio, US), MOBBS B.G. et al., "Suppression of the Growth of the Androgen-insensitive R3327 HI Rat Prostatic Carcinoma by Combined Estrogen and Antiprogestin Treatment", page 114, Abstract 34787r; & J. STEROID BIOCHEM. MOL. BIOL., 1991, 39(5A), 713-722. *
STN INTERNATIONAL, File Medline, Medline Accession No. 91346518, GRUBB G.S., "Experimental Methods of Contraception"; & CURR. OPIN. OBSTET. GYNECOL., (Aug. 1991), 3(4), 491-5, Ref:27. *

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1994027610A1 (fr) * 1993-05-28 1994-12-08 Schering Aktiengesellschaft Agents contenant un compose a action anti-androgene ainsi qu'un compose a action competitive antagoniste de la progesterone
EP2664325A1 (fr) * 2012-05-16 2013-11-20 PregLem S.A. Procédés de prévention ou de traitement des maladies induites par les androgènes
WO2013171684A1 (fr) * 2012-05-16 2013-11-21 Preglem Sa Modulateurs des récepteurs à la progestérone pour leur utilisation dans la prévention ou le traitement des maladies médiées par les androgènes

Also Published As

Publication number Publication date
DE4039561A1 (de) 1992-07-09
PT99724A (pt) 1992-10-30
CN1063040A (zh) 1992-07-29
PT99724B (pt) 1999-05-31

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