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Selective progesterone receptor modulator (SPRM) regimen

A variant, solvate technology, applied in the field of treatment of heavy menstrual bleeding, can solve problems such as endometrial thickening

Inactive Publication Date: 2018-01-26
BAYER PHARMA AG
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Unfortunately, taking lower concentrations of CDB-4124 resulted in significant thickening of the endometrium during treatment

Method used

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  • Selective progesterone receptor modulator (SPRM) regimen
  • Selective progesterone receptor modulator (SPRM) regimen
  • Selective progesterone receptor modulator (SPRM) regimen

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0124] Embodiment 1: the synthetic route of compound 1

[0125] (11β,17β)-17-Hydroxy-11-[4-(methylsulfonyl)phenyl]-17-(pentafluoroethyl)estr-4,9-dien-3-one

[0126]

[0127] 5 g of the above compound were dissolved in a mixture of 140 ml THF and 140 ml methanol. At 0°C, slowly drop 20g Solution in 94ml of water. It was then stirred for a further 3.5 hours at 0°C. A mixture of water and dichloromethane was then added to the reaction mixture. The phases are separated and the aqueous phase is extracted several times with dichloromethane. The combined organic phases were washed with saturated aqueous sodium chloride, dried over sodium sulfate and concentrated in vacuo. The crude product was purified by silica gel chromatography. This gave 3.8 g of the title compound.

[0128] 1H-NMR (300MHz, CDCl3): δ=7.86d(2H); 7.40d(2H); 5.81sbr(1H); 4.50dbr(1H); 3.07s(3H); 0.51s(3H).

Embodiment 2

[0129] Example 2: Efficacy and Safety of Compound 1 in Patients Diagnosed with Uterine Fibroids:

[0130] Research proposal:

[0131] Females, 18 to 50 years old, with vaginal or abdominal ultrasonography at screening showing uterine fibroids, having at least one uterine fibroid with a maximum diameter ≥ 3.0 cm and heavy menstrual bleeding (HMB) > 80 mL, such women are treated as Subjects participate in research studies. The primary efficacy variable was amenorrhea (yes / no), defined as the absence of monitored bleeding / spotting scheduled after the end of the initial bleeding event until the end of each treatment.

[0132] Treatment groups A1, B1: 30 subjects in each group

[0133] Treatment groups A2, B2: 6 subjects in each group

[0134] A1: Compound 1: 2 mg (12 weeks), Compound 1: 2 mg (12 weeks),

[0135] A2: placebo (12 weeks), compound 1: 2 mg (12 weeks),

[0136] B1: Compound 1: 2 mg (12 weeks), 1 bleeding event, Compound 1: 2 mg (12 weeks),

[0137] • B2: placebo ...

Embodiment 3

[0140] Example 3: Endometrial Thickness and PAEC Using Compound 1 for 3 Months of Treatment

[0141] Randomized, parallel-group, double-blind, placebo-controlled, multicenter study in subjects with uterine fibroids to evaluate different doses of The curative effect of compound 1, in which the primary curative effect variable is endometrial thickness, and the secondary curative effect variable is PAEC.

[0142] Research Protocol (N°15788):

[0143] Test drug: Compound 1

[0144] Dose: 0.5mg, 1mg, 2mg or 4mg, once a day

[0145] Administration route: Oral

[0146] Duration of treatment: 1 x 12 weeks (84 days)

[0147] Comparing drug: placebo

[0148] Duration of treatment: 1 x 12 weeks (84 days)

[0149] Included diagnoses and major criteria:

[0150] Females, 18 to 50 years of age, who have uterine fibroids as a result of transvaginal or abdominal ultrasound at screening, have at least one uterine fibroid with a maximum diameter of 3 cm and heavy menstrual bleeding (HMB) o...

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Abstract

The invention is directed to a pharmaceutical composition comprising a progesterone receptor antagonist namely (11beta,17beta)-17-Hydroxy-11-[4-(methylsulphonyl)phenyl]-17-(pentafluoroethyl)estra-4,9-dien-3-one for the treatment and / or prophylaxis of Uterine Fibroids (myomas, uterine leiomyoma) that is administered to a patient diagnosed with Uterine Fibroids following a specific regimen. Additionally, the invention is directed to a method for treating Uterine Fibroids (myomas, uterine leiomyoma) and / or for reducing Uterine Fibroids (myomas, uterine leiomyoma) size and symptoms related to Uterine Fibroids following a specific regimen as well as treatment of Heavy Menstrual Bleeding (HMB).

Description

technical field [0001] The present invention is directed to the treatment and / or prevention of uterine fibroids (fibroids, uterine leiomyomas) containing progesterone receptor modulators—that is, (11β,17β)-17-hydroxy-11-[4-(methyl sulfonyl)phenyl]-17-(pentafluoroethyl)est-4,9-dien-3-one—the pharmaceutical composition, which follows a specific regimen for daily administration to diagnosed patients Patients with uterine fibroids. [0002] In addition, the present invention is directed to a method for treating and / or reducing the size of uterine fibroids (fibroids, leiomyomas) and associated with uterine fibroids following a specific regimen. A method for the symptoms of , and a method for treating heavy menstrual bleeding (HMB). Background technique [0003] Uterine fibroids (also known as uterine leiomyomas or fibroids) are common benign tumors of the uterine myometrium. It has been reported that about 30-40% of reproductive age women have uterine fibroids. Depending on nu...

Claims

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Application Information

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IPC IPC(8): A61K31/57A61P15/08A61P35/00A61P15/00A61P7/04
CPCA61K31/567A61P15/00A61P35/00C07J31/006
Inventor C·塞茨R·克瑙斯S·佐恩
Owner BAYER PHARMA AG
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