Selective progesterone receptor modulator (SPRM) regimen

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

Pending Publication Date: 2021-12-17
BAYER PHARMA AG
View PDF5 Cites 0 Cited by
  • 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

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • 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

[0123] Embodiment 1: the synthetic route of compound 1

[0124] (11β,17β)-17-Hydroxy-11-[4-(methylsulfonyl)phenyl]-17-(pentafluoroethyl)estr-4,9-dien-3-one

[0125]

[0126] 5 g of the above compound were dissolved in a mixture of 140 ml THF and 140 ml methanol. At 0 ℃, 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.

[0127] 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

[0128] Example 2: Efficacy and Safety of Compound 1 in Patients Diagnosed with Uterine Fibroids:

[0129] Research proposal:

[0130] Females, 18 to 50 years old, with vaginal or abdominal ultrasonography at screening showing uterine fibroids, with at least one fibroid ≥ 3.0 cm in greatest diameter and heavy menstrual bleeding (HMB) > 80 mL, are considered 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.

[0131] Treatment groups A1, B1: 30 subjects in each group

[0132] Treatment groups A2, B2: 6 subjects in each group

[0133] A1: Compound 1: 2 mg (12 weeks), Compound 1: 2 mg (12 weeks),

[0134] A2: placebo (12 weeks), compound 1: 2 mg (12 weeks),

[0135] B1: Compound 1: 2 mg (12 weeks), 1 bleeding event, Compound 1: 2 mg (12 weeks),

[0136] • B2: placebo (12 weeks), 1 bleedin...

Embodiment 3

[0139] Example 3: Endometrial Thickness and PAEC Using Compound 1 for 3 Months of Treatment

[0140] 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.

[0141] Research Protocol (N°15788):

[0142] Test drug: Compound 1

[0143] Dose: 0.5mg, 1mg, 2mg or 4mg, once a day

[0144] Administration route: Oral

[0145] Duration of treatment: 1 x 12 weeks (84 days)

[0146] Comparing drug: placebo

[0147] Duration of treatment: 1 x 12 weeks (84 days)

[0148] Included diagnoses and major criteria:

[0149] 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)...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

PUM

No PUM Login to view more

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

[0001] This application is a divisional application of the No. 201680029060.3 invention patent application entitled "Selective Progesterone Receptor Modulator (SPRM) Scheme". The original application corresponds to the international application PCT / EP2016 / 061037, the filing date is May 17, 2016, and the priority date is May 18, 2015. technical field [0002] 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. [0003] 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 m...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

Application Information

Patent Timeline
no application Login to view more
Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/567A61P15/00A61P35/00
CPCA61K31/567A61P15/00A61P35/00C07J31/006
Inventor C·塞茨R·克瑙斯S·佐恩
Owner BAYER PHARMA AG
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Try Eureka
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap