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Progesterone receptor antagonist dosage form

A dosage form and drug technology, applied in the field of bleeding and improving the quality of life, can solve problems limited to 6 months

Inactive Publication Date: 2015-12-02
BAYER PHARMA AG
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, their use is limited to 6 months due to low estrogenic side effects

Method used

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  • Progesterone receptor antagonist dosage form
  • Progesterone receptor antagonist dosage form
  • Progesterone receptor antagonist dosage form

Examples

Experimental program
Comparison scheme
Effect test

no. 1 approach

[0056] exist first embodiment In, the oral dosage form additionally comprises pharmaceutically acceptable excipients.

[0057] exist second embodiment In the present invention, the oral dosage form additionally comprises pharmaceutically acceptable excipients and / or at least one or more other active substances, especially active substances known for the treatment and / or prevention of the aforementioned diseases.

[0058] Embodiments and preferred features as described above are included therein.

[0059] In a fourth aspect, the present invention relates to an oral dosage form as described in the third aspect for use in the treatment and / or prevention of gynecological diseases. The gynecological disorder is preferably characterized by excessive uterine bleeding. More preferably, the gynecological disorder is uterine fibroids (fibroids, leiomyomas), endometriosis or excessive menstrual bleeding. Even more preferably, the gynecological disease is uterine fibroids (fibroids,...

Embodiment 1

[0081] Embodiment 1: the synthetic route of compound 1

[0082] (11β,17β)-17-Hydroxy-11-[4-(methylsulfonyl)phenyl]-17-(pentafluoroethyl)estr-4,9-dien-3-one

[0083]

[0084] 5 g of the compound described in Example 1b) were dissolved in a mixture of 140 ml THF and 140 ml methanol. A solution of 20 g of Oxone® in 94 ml of water was slowly added dropwise at 0°C. This was followed by further stirring at 0°C for 3.5 hours. A mixture of water and dichloromethane was then added to the reaction mixture. The phases were separated and the aqueous phase was extracted several times with dichloromethane. The combined organic phases were washed with saturated aqueous sodium chloride, dried over sodium sulfate and concentrated under vacuum. The crude product was purified by silica gel chromatography. 3.8 g of the title compound are obtained.

[0085] 1 H-NMR (300MHz, CDCl 3 ):δ=7.86d(2H);7.40d(2H);5.81sbr(1H);4.50dbr(1H);3.07s(3H);0.51s(3H).

Embodiment 2

[0086] Example 2: Dose Effect of Treatment with Compound 1 for 84 Days

[0087] Random Study Population:

[0088] 1. Healthy female subjects, sterilized by tubal ligation

[0089] 2. Screening age: 18-45 years old

[0090] 3. Screened body mass index (BMI): ≥18 and ≤32kg / m2

[0091] 4. At least 3 consecutive normal menstrual periods with a cycle length of 24-35 days prior to the first screening examination based on the subject's history

[0092] 5. Absence of Clinically Relevant Abnormal Findings in Pretreatment Endometrial Biopsy

[0093] 6. Adequate venous access (frequent blood draws).

[0094] Program:

[0095] Table 1: Therapeutic Doses Using Compound 1

[0096] .

[0097] After the pre-treatment cycle, subjects must start taking the study drug on the first or second day of menstrual bleeding. A pretreatment cycle commencing on the first day of a subject's menstrual bleeding following screening checks has indicated that the subject is eligible for further ...

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Abstract

The invention is directed to a pharmaceutical composition comprising a progesterone receptor antagonist namely (11 β,17β)-17-Hydroxy-11-[4-(methylsulphonyl)phenyl]-17-(pentafluoroethyl)estra-4,9-dien-3-one at the dosage of about 0.5 to 5 mg and more particularly 2 mg. Additionally, the invention is directed to the use of the novel pharmaceutical composition for treatment of and / or prophylaxis of gynaecological diseases, such as fibroids of the uterus (myomas, uterine leiomyoma), endometriosis or excessive menstrual bleeds, and method for obtaining such composition and oral dosage form.

Description

[0001] The present invention relates to a dose comprising a progesterone receptor antagonist, i.e. (11β,17β)-17-hydroxy-11-[4-(methylsulfonyl)phenyl]- Pharmaceutical compositions of 17-(pentafluoroethyl)estr-4,9-dien-3-one. Furthermore, the invention relates to the use of the novel pharmaceutical composition for the treatment and / or prevention of gynecological diseases such as uterine fibroids (fibroids, uterine leiomyomas), endometriosis or excessive menstrual bleeding, as well as to obtain such Compositions and methods of oral dosage forms. Background of the invention [0002] Uterine leiomyomas (also known as fibroids or fibroids) are common benign tumors of the myometrium, reported to occur in approximately 30-40% of all women of reproductive age. They can remain asymptomatic or, depending on their number, size, and location, cause bleeding abnormalities and / or bulk-related symptoms. Various drugs are used for symptom-directed therapy of minor illnesses (eg, combined ora...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/567A61P15/00
CPCA61K31/567A61K9/0053A61K9/20A61P15/00A61P15/08A61P35/00A61P43/00A61P5/36A61P7/04
Inventor B.许特M-H.舒尔策-莫斯高A.凯泽
Owner BAYER PHARMA AG
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