エラゴリクス化学構造式

エラゴリクス

化学名:エラゴリクス

CAS番号.834153-87-6

英語名:elagolix

CBNumberCB51518509

MFC32H30F5N3O5

MW631.59

MOL File834153-87-6.mol

别名

エラゴリクス

エラゴリックス

4-{[(1R)-2-[5-(2-フルオロ-3-メトキシフェニル)-3-{[2-フルオロ-6-(トリフルオロメチル)フェニル]メチル}-4-メチル-2,6-ジオキソ-1,2,3,6-テトラヒドロピリミジン-1-イル]-1-フェニルエチル]アミノ}ブタン酸

エラゴリクス物理性質

沸点	728.6±70.0 °C(Predicted)
比重(密度)	1.350
貯蔵温度	Store at -20°C
溶解性	DMSO : ≥ 100 mg/mL (158.33 mM)
酸解離定数(Pka)	4.40±0.10(Predicted)
外見	Solid
色	White to off-white
InChIKey	HEAUOKZIVMZVQL-VWLOTQADSA-N
SMILES	C(O)(=O)CCCN[C@H](C1=CC=CC=C1)CN1C(=O)N(CC2=C(C(F)(F)F)C=CC=C2F)C(C)=C(C2=CC=CC(OC)=C2F)C1=O

危険有害性情報のコード(GHS)

エラゴリクス化学特性,用途語,生産方法

効能
子宮内膜症治療薬, 性腺刺激ホルモン放出ホルモン受容体拮抗薬
説明
Elagolix is a gonadotropin-releasing hormone(GnRH) receptor antagonist indicated for the management of moderate to severe pain associated with endometriosis. Elagolix is an orally administered,nonpeptide small molecule gonadotropin-releasing hormone(GnRH) receptor antagonist that inhibits endogenousGnRH signaling by binding competitively to GnRH receptors in the pituitary gland.
Elagolix results in dose-dependent suppression of luteinizing hormone(LH) and follicle-stimulating hormone(FSH) leading to decreased blood leveis of the ovarian sex hormones, estradiol and progesterone.Elagolix causes a dose-dependent decrease in bone mineral density (BMD).BMD loss is greater with increasing duration of use and may not be completely reversible after stopping treatment.
As milk production is dependent on at least minimal levels of estrogen, this product may reduce milk production.
使用
Elagolix has a potential role for treating uterine bleeding associated to uterine myomas. Elagolix is also used in the methods for treatment of estrogen-dependent disorders including gonadotropin-releasing hormone (GnRH) antagonists in combination with add-back therapy.
製造方法
Elagolix was a gonadotropin-releasing hormone antagonist. It was approved in 2018 by FDA via priority review for clinical treatment of endometriosis. Based on retrosynthetic analysis, five reported synthesis routes of elagolix were summarized. They were compared and evaluated in terms of step numbers, total yields, costs, synthetic conditions and manufacturing safety. At last, the synthetic method of d6-elagolix was introduced. This review would be beneficial to the future process researches of elagolix and its deuterium analogues.

Recent Progress in the Synthesis of Elagolix
Discovery of sodium R-(+)-4-{2-[5-(2-fluoro-3-methoxyphenyl)-3-(2-fluoro-6-[trifluoromethyl]benzyl)-4-methyl-2,6-dioxo-3,6-dihydro-2H-pyrimidin-1-yl]-1-phenylethylamino}butyrate (elagolix), a potent and orally available nonpeptide antagonist of the human gonadotropin-releasing hormone receptor

エラゴリクス上流と下流の製品情報

エラゴリクス生産企業

834153-87-6, エラゴリクスキーワード

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エラゴリクス

危険有害性情報のコード(GHS)

エラゴリクス 化学特性,用途語,生産方法

エラゴリクス 上流と下流の製品情報

エラゴリクス 生産企業

834153-87-6, エラゴリクス キーワード

エラゴリクス化学特性,用途語,生産方法

エラゴリクス上流と下流の製品情報

エラゴリクス生産企業

834153-87-6, エラゴリクスキーワード