Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Cyclopentanohydrophenanthrene ring system doai
Patent
1997-06-10
2000-03-28
Jordan, Kimberly
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Cyclopentanohydrophenanthrene ring system doai
A61K 3156
Patent
active
060432349
DESCRIPTION:
BRIEF SUMMARY
This application is a 371 of PCT/EP95/02998, filed Jul. 27, 1995.
This invention relates to the use of a combination product that consists of individual dosage units of a competitive progesterone antagonist and individual dosage units of a compound that are provided sequentially in it, having a gestagenic action for the production of a pharmaceutical agent for treating endometriosis or leiomyomata uteri.
It is known that competitive progesterone antagonists (antigestagens=AG's) such as, e.g., RU486 (mifepristones; 11.beta.-[(4-N,N-dimethylamino)-phenyl]-17.beta.-hydroxy-17.alpha.-propiny l-4,9(10)-estradien-3-one) are able to inhibit ovulation in various animal species and in women [1) Uilenbroek, J. TH. J.(1991); Hormone Concentrations and Ovulatory Response in Rats Treated with Antiprogestagens. Journal of Endocrinology, 129, 423-429; 2) Danforth, R. et al (1989): Contraceptive Potential of RU486 by Ovulation Inhibition: III. Preliminary Observations on Once Weekly Administration, Contraception, 40/2, 195-200; 3) Kekkonen, R. et al. (1990): Interference with Ovulation by Sequential Treatment with the Antiprogestin RU486 and Synthetic Progestin. Fertility and Sterility, 53/4, 747-750; 4) Ledger, W. L. et al. (1992): Inhibition of Ovulation by Low Dose Mifepristone (RU486). Human Reproduction, 7/7, 945-950; 5) Nieman, L. K. et al. (1987): The Progesterone Antagonist RU486: A New Potential New Contraceptive Agent. The New England Journal of Medicine, 316/4, 187-1991].
The implantation of a fertilized egg can also be prevented by AG's (implantation inhibition); [6) Glassier A. et al. (1992): Mifepristone (RU 486) Compared with High Dose Estrogen and Progesterone for Emergency Postcoital Contraception: New England Journal of Medicine, 8/15; 1041; 7) Puri, C. P. et al. (1990); Effects of a Progesterone Antagonist, Ilopristone, On Induction of Menstruation, Inhibition of Nidation, and Termination of Pregnancy in Bonnet Monkeys. Biology of Reproduction, 43, 437-443; 8) Ishwad, P. C. et al. (1993): Treatment with a Progesterone Antagonist ZK 98 299 Delays Endometrial Development without Blocking Ovulation in Bonnet Monkeys. Contraception, 48, 57-70; 9) Batista, M. C. et al. (1992): Delayed Endometrial Maturation Induced by Daily Administration of the Antiprogestin RU 486: A Potential New Contraceptive Strategy. AM. J. Obstet. Gynecol. 167/1, 60-65].
It should be possible to use AG's as contraceptive agents because of their ovulation-inhibiting [3), 4), 5)] or implantation-inhibiting action [6), 7), 8), 9)]. The use of competitive progesterone antagonists at a non-ovulation-inhibiting as well as a non-abortion-inducing dose for the production of oral contraceptive agents is described in International Patent Application WO-A 93/23020.
In addition, for gynecological applications, initial clinical studies have shown that AG's can be used for treating endometriosis and leiomyomata uteri (myoma) [10) Kettel, L. M. et al. (1991): Endocrine Responses to Long-Term Administration of the Antiprogesterone RU 486 in Patients with Pelvic Endometriosis. Fertility and Sterility, 56/3, 402-407; 11) Kettel, L. M. et al. (1993): Long-Term, Low-Dose RU486 in the Treatment of Endometriosis. Meeting of the Society of Gynecological Investigation 1993, Abstract p. 136; 12) Murphy, A. A. et al. (1993): Regression of Uterine Leiomyomata in Response to the Antiprogestin RU486, J. Clin. Endocrinol. Metab., 76/2, 513-517].
The findings from these studies also indicate, however, that in the case of chronic treatment with AG's over the entire menstrual cycle, but also in the case of treatment during certain cycle phases with AG's, alteration or lengthening of the cycle with cessation of monthly bleeding (amenorrhea) or reduced menstruation can occur because of the elimination of progesterone action during the luteal phase of the cycle [8), 9), 10)].
Monthly bleeding means, however, natural protection for the endometrium. In the normal menstrual cycle, proliferation of the endometrium results in the follicle phase (proliferation phase) under th
REFERENCES:
CA 102:40106, Azadian-Boulanger et al. 1984.
CA 120:253388, Lipp et al. Mar. 1994.
Chwalisz Kristof
Stockemann Klaus
Jordan Kimberly
Schering Aktiengesellschaft
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