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Methods of treating uterine fibroids and endometriosis

An endometrial, adenomyosis technique for use in the treatment of one or more side effects of gonadotropin-releasing hormone antagonist administration

Active Publication Date: 2019-10-08
梦欧文科学有限责任公司 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Treatment with these therapies may also require additional monitoring for unwanted side effects, such as ultrasound, endometrial biopsy, and / or bone densitometry

Method used

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  • Methods of treating uterine fibroids and endometriosis
  • Methods of treating uterine fibroids and endometriosis
  • Methods of treating uterine fibroids and endometriosis

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0665] Embodiment 1: preparation compound 1

[0666]

[0667] N-(4-(1-(2,6-difluorobenzyl)-3-(6-methoxy-3-pyridazinyl)-5-((methylamino)methyl)-2,4 -Dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl)phenyl)-N'-methoxyurea (150 mg, 0.259 mmol) in DMF (4ml), and iodomethane (0.010ml, 0.164mmol) was added thereto. The reaction mixture was stirred at room temperature for 1 hour, combined with aqueous sodium bicarbonate, and extracted with ethyl acetate. The organic layer was washed with brine, dried over magnesium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (eluent: ethyl acetate / methanol=40 / 1), and recrystallized from dichloromethane / methanol / diethyl ether to give the title compound (17.3 mg, 17 %). 1 H-NMR (CDCl 3 )δ:2.15(6H,s),3.6-3.8(2H,m),3.82(3H,s),4.18(3H,s),5.35(2H),6.92(2H,t,J=8.2Hz), 7.12 (1H, d, J=8.8Hz), 7.2-7.65 (7H, m), 7.69 (1H, s).

Embodiment 2

[0668] Example 2: Preparation of Film Coated Tablets of Compound 1

[0669] By using the compound (40 mg) obtained in Example 1, mannitol (preferably D-mannitol) (122 mg), microcrystalline cellulose (40 mg), hydroxypropyl cellulose (6 mg), croscarmellose Sodium (10 mg), magnesium stearate (2 mg) and sufficient purified water to prepare film-coated tablets. Water is removed during processing. In a fluidized bed drying granulator (LAB-1, Powrex Corporation), the compound obtained in Example 1, D-mannitol, and microcrystalline cellulose were preheated and mixed, an aqueous solution of hydroxypropyl cellulose was sprayed, and the mixture was dried to obtain granular powder. To the obtained granulated powder, croscarmellose sodium and magnesium stearate were added, and they were mixed in a bag to obtain a mixed powder. The mixed powder has Tablets were compressed with a rotary tablet press (compact 10 tablet press, Kikusui Seisakusho Ltd.) with a ram to obtain tablet cores. ...

Embodiment 3

[0670] Example 3: Preparation of Film Coated Tablets of Compound 1

[0671] By using the compound (40 mg) obtained in Example 1, mannitol (including D-mannitol) (51 mg), sodium starch glycolate (Type A) (5 mg), hydroxypropylcellulose (3 mg), stearic acid Magnesium (1 mg) and sufficient purified water to prepare film-coated tablets. Water is removed during processing. In a fluidized bed drying granulator (LAB-1, Powrex Corporation), the compound obtained in Example 1, mannitol, and sodium starch glycolate were preheated and mixed, an aqueous solution of hydroxypropylcellulose was sprayed, and the mixture was dried to A granular powder was obtained. Magnesium stearate was added to the obtained granulated powder, and they were mixed in a bag to obtain a mixed powder. The mixed powder has Tablets were compressed with a rotary tablet press (compact 10 tablet press, Kikusui Seisakusho Ltd.) with a ram to obtain tablet cores. The tablet core was placed in a film coater (DRC-200...

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Abstract

Methods for treating uterine fibroids, endometriosis, adenomyosis, or heavy menstrual bleeding in a subject, which include administering to the subject from 10 mg to 60 mg per day of N-(4-(1-(2,6-difluorobenzyl)-5-((dimethylamino)methyl)-3-(6-methoxy-3-pyridazinyl)-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl)phenyl)-N'-methoxyurea, and from 0.01 mg to 5 mg per day of a hormone replacement medicament. The present disclosure has methods for reducing menstrual bleeding in a subject, reducing bone mineral density loss in a subject caused by administering a GnRH antagonist to the subject, suppressing sex hormones in a subject, reducing vasomotor symptoms or hot flashes in a subject, and reducing symptoms of decreased libido in a subject having uterine fibroids, endometriosis, or adenomyosis. Further provided are methods of maintaining blood glucose profile, maintaining lipid profile, and / or maintaining bone mineral density in a pre-menopausal woman being treated for one or moreconditions or symptoms of endometriosis, adenomyosis, uterine fibroids, or heavy menstrual bleeding; and methods of contraception and treating infertility.

Description

[0001] Cross References to Related Applications [0002] This application claims U.S. Provisional Application No. 62 / 402,034, filed September 30, 2016; U.S. Provisional Application No. 62 / 402,055, filed September 30, 2016; U.S. Provisional Application No. 62 / 402,150, filed September 30, 2016 ; U.S. Provisional Application No. 62 / 492,839, filed May 1, 2017; and U.S. Provisional Application No. 62 / 528,409, filed July 3, 2017; the disclosures of these patents are incorporated herein by reference in their entirety. technical field [0003] The present disclosure relates generally to methods of treating estrogen-sensitive conditions, and more particularly to treating uterine fibroids, endometriosis, adenomyosis, heavy menstrual bleeding, or uterine fibroids in a subject in need thereof , Pain associated with endometriosis or adenomyosis. The present disclosure also relates to methods of treating one or more side effects of administration of a gonadotropin releasing hormone (GnRH) ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/513A61K31/565A61K31/57A61P15/00
CPCA61K31/513A61K31/565A61K31/57A61P15/00A61K2300/00A61K31/519A61K9/0053
Inventor B·M·约翰逊L·西利小保罗·N·马德S·沃洛维茨M·希伯德M·谷本V·R·拉贾塞卡拉M·V·舒卡特梅
Owner 梦欧文科学有限责任公司
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