KR101139148B1 - 고나도트로핀-방출 호르몬 수용체 길항제로서의피리미딘-2,4-디온 유도체 - Google Patents

고나도트로핀-방출 호르몬 수용체 길항제로서의피리미딘-2,4-디온 유도체 Download PDF

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KR101139148B1
KR101139148B1 KR1020067000436A KR20067000436A KR101139148B1 KR 101139148 B1 KR101139148 B1 KR 101139148B1 KR 1020067000436 A KR1020067000436 A KR 1020067000436A KR 20067000436 A KR20067000436 A KR 20067000436A KR 101139148 B1 KR101139148 B1 KR 101139148B1
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compound
fluoro
dione
trifluoromethyl
methyl
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KR20060031851A (ko
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치퀴앙 구오
용쉥 첸
동뻬이 우
첸 첸
워렌 웨이드
웨슬리 제이. 드와이트
찰스 큐. 후앙
파비오 쎄. 뚜씨
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뉴로크린 바이오사이언시즈 인코퍼레이티드
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/52—Two oxygen atoms
    • C07D239/54—Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/513—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/14—Drugs for dermatological disorders for baldness or alopecia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/20—Hypnotics; Sedatives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/02—Drugs for disorders of the endocrine system of the hypothalamic hormones, e.g. TRH, GnRH, CRH, GRH, somatostatin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/02—Drugs for disorders of the endocrine system of the hypothalamic hormones, e.g. TRH, GnRH, CRH, GRH, somatostatin
    • A61P5/04—Drugs for disorders of the endocrine system of the hypothalamic hormones, e.g. TRH, GnRH, CRH, GRH, somatostatin for decreasing, blocking or antagonising the activity of the hypothalamic hormones
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/06—Drugs for disorders of the endocrine system of the anterior pituitary hormones, e.g. TSH, ACTH, FSH, LH, PRL, GH
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/52—Two oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/04—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Endocrinology (AREA)
  • Diabetes (AREA)
  • Reproductive Health (AREA)
  • Immunology (AREA)
  • Urology & Nephrology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Anesthesiology (AREA)
  • Dermatology (AREA)
  • Biomedical Technology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Pregnancy & Childbirth (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Steroid Compounds (AREA)
KR1020067000436A 2003-07-07 2004-07-06 고나도트로핀-방출 호르몬 수용체 길항제로서의피리미딘-2,4-디온 유도체 Expired - Lifetime KR101139148B1 (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US48543403P 2003-07-07 2003-07-07
US60/485,434 2003-07-07
PCT/US2004/021593 WO2005007165A1 (en) 2003-07-07 2004-07-06 Pyrimidine-2, 4-dione derivatives as gonadotropin-releasing hormone receptor antagonists

Publications (2)

Publication Number Publication Date
KR20060031851A KR20060031851A (ko) 2006-04-13
KR101139148B1 true KR101139148B1 (ko) 2012-04-26

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KR1020067000436A Expired - Lifetime KR101139148B1 (ko) 2003-07-07 2004-07-06 고나도트로핀-방출 호르몬 수용체 길항제로서의피리미딘-2,4-디온 유도체

Country Status (24)

Country Link
US (3) US7056927B2 (https=)
EP (1) EP1646389B1 (https=)
JP (2) JP4722844B2 (https=)
KR (1) KR101139148B1 (https=)
CN (1) CN100424078C (https=)
AT (1) ATE407679T1 (https=)
AU (1) AU2004257639B2 (https=)
BR (1) BRPI0412314B8 (https=)
CA (1) CA2531508C (https=)
CY (1) CY1108656T1 (https=)
DE (1) DE602004016516D1 (https=)
DK (1) DK1646389T3 (https=)
EA (1) EA010370B1 (https=)
ES (1) ES2314448T3 (https=)
HR (1) HRP20080646T3 (https=)
IL (1) IL172833A (https=)
MX (1) MXPA06000297A (https=)
NO (1) NO334897B1 (https=)
NZ (1) NZ544747A (https=)
PL (1) PL1646389T3 (https=)
PT (1) PT1646389E (https=)
SI (1) SI1646389T1 (https=)
WO (1) WO2005007165A1 (https=)
ZA (1) ZA200600475B (https=)

Families Citing this family (81)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PT1255738E (pt) * 2000-01-25 2012-06-19 Neurocrine Biosciences Inc Antagonistas do receptor da hormona de libertação da gonadotrofina e métodos relacionados com os mesmos
ATE428427T1 (de) * 2003-07-07 2009-05-15 Neurocrine Biosciences Inc Pyrimidin-2,4-dion-derivate als gonadotropin freisetzende hormon-rezeptor-antagonisten
US7015226B2 (en) * 2003-07-07 2006-03-21 Neurocrine Biosciences, Inc. Gonadotropin-releasing hormone receptor antagonists and methods relating thereto
CN100424078C (zh) * 2003-07-07 2008-10-08 纽罗克里生物科学有限公司 作为促性激素释放激素受体拮抗剂的嘧啶-2,4-二酮衍生物
CN102127057A (zh) * 2004-03-15 2011-07-20 武田药品工业株式会社 二肽基肽酶抑制剂
CL2008000986A1 (es) 2007-04-06 2008-10-17 Neurocrine Biosciences Inc COMPUESTO DERIVADO DE HETEROCICLOS DE NITROGENO, AGONISTAS DEL RECEPTOR GnRH; COMPOSICION FARMACEUTICA QUE COMPRENDE A DICHO COMPUESTO; Y USO PARA TRATAR UNA AFECCION RELACIONADA CON LAS HORMONAS SEXUALES, ENDOMETRIOSIS, DISMENORREA, ENFERMEDAD DE OV
PE20090044A1 (es) 2007-04-06 2009-01-23 Neurocrine Biosciences Inc Antagonistas del receptor de la hormona liberadora de gonadotropina y procedimientos relacionados con los mismos
KR101666228B1 (ko) 2007-09-28 2016-10-13 인트렉손 코포레이션 생물치료학적 분자를 발현시키기 위한 치료학적 유전자-스위치 작제물 및 생물반응기, 및 이의 용도
US8765948B2 (en) * 2007-11-07 2014-07-01 Neurocrine Biosciences, Inc. Processes for the preparation of uracil derivatives
US9034850B2 (en) 2009-11-20 2015-05-19 Sk Chemicals Co., Ltd. Gonadotropin releasing hormone receptor antagonist, preparation method thereof and pharmaceutical composition comprising the same
US10881659B2 (en) 2013-03-15 2021-01-05 Abbvie Inc. Methods of treating heavy menstrual bleeding
EP2881391A1 (en) 2013-12-05 2015-06-10 Bayer Pharma Aktiengesellschaft Spiroindoline carbocycle derivatives and pharmaceutical compositions thereof
EP3185881B1 (en) 2014-08-26 2022-03-09 Betanien Hospital Methods, agents and compositions for treatment of inflammatory conditions
WO2017221144A1 (en) * 2016-06-20 2017-12-28 Dr. Reddy's Laboratories Limited Process for the preparation of elagolix sodium and its polymorph
CN115590849A (zh) 2016-07-21 2023-01-13 奥布赛瓦股份公司（Ch） 促进胚胎植入和预防流产的催产素拮抗剂给药方案
CN109789375B (zh) 2016-08-23 2023-06-06 Swan水质分析仪表公司 用于对液体进行电去离子化的装置和方法
ES2912929T5 (en) 2016-09-30 2025-05-09 Sumitomo Pharma Switzerland Gmbh Methods of treating uterine fibroids and endometriosis
MA46361A (fr) 2016-09-30 2021-03-31 Myovant Sciences Gmbh Traitement du cancer de la prostate
MA46353A (fr) 2016-09-30 2019-08-07 Myovant Sciences Gmbh Méthodes de traitement de l'infertilité féminine
JP7184775B2 (ja) 2016-12-14 2022-12-06 パーデュー・リサーチ・ファウンデイション 黄体化ホルモン放出ホルモン受容体（ｌｈｒｈ－ｒ）コンジュゲートおよびその使用
CA3059815C (en) 2017-04-12 2020-10-27 Sandoz Ag Acid addition salts of an orally available gonadotropin-releasing hormone receptor antagonist, elagolix
EP3388421B1 (en) 2017-04-13 2019-12-04 Sandoz AG Acid addition salts of an orally available gonadotropin-releasing hormone receptor antagonist
EP3388422B1 (en) 2017-04-13 2019-11-20 Sandoz AG Amorphous solid dispersion of an orally available gonadotropin-releasing hormone receptor antagonist
WO2018198086A1 (en) * 2017-04-28 2018-11-01 Lupin Limited Process for the preparation of elagolix and pharmaceutically acceptable salts thereof
EA201992612A1 (ru) 2017-06-05 2020-05-20 Обсева С.А. Схемы применения антагониста гонадотропин-высвобождающего гормона для лечения эндометриоза
WO2018224063A2 (en) * 2017-06-08 2018-12-13 Zentiva, K.S. Solid forms of elagolix
US12083227B2 (en) 2017-08-18 2024-09-10 Abbvie Inc. Solid pharmaceutical formulations for treating endometriosis, uterine fibroids, polycystic ovary syndrome or adenomyosis
US20190054088A1 (en) * 2017-08-18 2019-02-21 Abbvie Inc. Pharmaceutical Formulations for Treating Endometriosis, Uterine Fibroids, Polycystic Ovary Syndrome or Adenomyosis
MX2020001877A (es) * 2017-08-18 2020-09-14 Abbvie Inc Formulaciones farmacéuticas para tratar la endometriosis, los fibromas uterinos, el síndrome de ovario poliquístico o la adenomiosis.
CN107935863A (zh) * 2017-11-30 2018-04-20 厦门海乐景生化有限公司 Elagolix的关键原料化合物C的合成方法
JP7200261B2 (ja) * 2017-12-05 2023-01-06 スージョウ ポンシュー ファーマテック カンパニー リミテッド エラゴリクスを作製するプロセス
CN110938037A (zh) * 2018-09-21 2020-03-31 苏州鹏旭医药科技有限公司 一种依拉戈利钠盐药物中间体的制备方法
WO2019115019A1 (en) 2017-12-11 2019-06-20 Synthon B.V. Process for preparing elagolix
CN109970663B (zh) * 2017-12-27 2023-04-11 上海科胜药物研发有限公司 一种制备噁拉戈利中间体的方法
CN108129400B (zh) * 2017-12-29 2021-10-15 安帝康（无锡）生物科技有限公司 氘代噁拉戈利衍生物及其用途
CN112261942A (zh) 2018-04-19 2021-01-22 艾伯维公司 治疗重度月经出血的方法
CN110669013A (zh) * 2018-07-03 2020-01-10 江苏海悦康医药科技有限公司 一种噁拉戈利中间体的制备方法
EP3826638A4 (en) * 2018-07-23 2022-04-06 Abbvie Inc. ELAGOLIX SODIUM COMPOSITIONS AND RELATED METHODS
JP2021532160A (ja) * 2018-08-01 2021-11-25 アッヴィ・インコーポレイテッド エラゴリックスに関する投与計画
EP3572406A1 (en) 2018-10-17 2019-11-27 Sandoz Ag Acid addition salt of elagolix and related compounds
CA3117092A1 (en) 2018-10-29 2020-05-07 ObsEva S.A. Compositions and methods for the treatment of adenomyosis and rectovaginal endometriosis
SG11202104053TA (en) 2018-11-07 2021-05-28 ObsEva SA Compositions and methods for the treatment of estrogen-dependent disorders
CN109293634A (zh) * 2018-12-04 2019-02-01 中国药科大学 恶拉戈利杂质的制备方法
CN109651171A (zh) * 2019-01-13 2019-04-19 苏州鹏旭医药科技有限公司 依拉戈利及其钠盐的中间体及其盐的制备方法和应用
PH12021551685A1 (en) 2019-01-15 2022-05-16 Lupin Inc Deuterated elagolix-like compositions and methods
CN109651265A (zh) * 2019-02-16 2019-04-19 安徽诺全药业有限公司 一种Elagolix的制备方法
CN109761913A (zh) * 2019-02-16 2019-05-17 安徽华胜医药科技有限公司 一种有机金属钯催化合成elagolix中间体的方法
CN109810065B (zh) * 2019-02-16 2022-07-15 安徽华胜医药科技有限公司 一种恶拉戈利的合成方法
CN110041232A (zh) * 2019-04-10 2019-07-23 丽珠集团新北江制药股份有限公司 一种制备GnRHR药物关键中间体化合物的方法
CN109956906B (zh) * 2019-04-19 2021-01-29 奥锐特药业股份有限公司 一种噁拉戈利关键中间体的制备方法
WO2020240375A1 (en) * 2019-05-24 2020-12-03 Dr. Reddy’S Laboratories Limited Improved process for the preparation of elagolix and its intermediates
CN110204498B (zh) * 2019-06-14 2020-11-27 奥锐特药业股份有限公司 一种高效合成噁拉戈利中间体的方法
CN110372608A (zh) * 2019-07-09 2019-10-25 丽珠集团新北江制药股份有限公司 一种促性腺激素释放激素拮抗剂的制备方法
ES2802815B2 (es) * 2019-07-12 2022-03-14 Moehs Iberica Sl Sal clorhidrato de 3-[2(r)-amino-2-feniletil]-5-(2-fluoro-3-metoxifenil)-1-[2-fluoro-6-(trifluorometil)bencil]-6-metil-1h-pirimidin-2,4(1h,3h)-diona (i) en forma solida, procedimiento para su preparacion y uso de la misma en la sintesis de elagolix
CN110372609B (zh) * 2019-07-25 2021-04-09 奥锐特药业股份有限公司 一种噁拉戈利钠盐的纯化方法
CN112672998B (zh) 2019-07-31 2022-06-21 深圳仁泰医药科技有限公司 恶拉戈利与乙胺嘧啶的共晶型a及其制备方法和用途
CN114466665A (zh) 2019-08-08 2022-05-10 奥布赛瓦股份公司 用于治疗雌激素依赖性病症的组合物和方法
AU2020325721A1 (en) 2019-08-08 2022-03-03 ObsEva S.A. GnRH antagonists for the treatment of estrogen-dependent disorders
CA3149898A1 (en) 2019-09-03 2021-03-11 Ernest Loumaye Oxytocin antagonist dosing regimens for promoting embryo implantation and preventing miscarriage
IT202000001390A1 (it) * 2020-01-24 2021-07-24 Ind Chimica Srl Processo per la preparazione del sale sodico dell’acido 4-[[(1r)-2-[5-(2-fluoro-3-metossifenil)-3-[[2-fluoro-6-(trifluorometil)fenil]metil]-3,6-diidro-4-metil-2,6-diosso-1(2h)-pirimidinil]-1-feniletil]ammino]-butanoico (elagolix sale sodico) e intermedi di detto processo
US11840519B2 (en) 2019-09-03 2023-12-12 Industriale Chimica S.R.L. Process for the synthesis of the sodium salt of 4-[[(1R)-2-[5-(2-fluoro-3-methoxyphenyl)-3-[[2-fluoro-6-(trifluoromethyl)-phenyl]methyl]-3,6-dihydro-4-methyl-2.6-dioxo-1(2H)-pyrimidinyl]-1-phenylethyl]amino]-butanoic acid (elagolix sodium salt) and intermediates of said process
IT201900015458A1 (it) * 2019-09-03 2021-03-03 Ind Chimica Srl Processo per la preparazione del sale sodico dell’acido 4-[[(1r)-2-[5-(2-fluoro-3-metossifenil)-3-[[2-fluoro-6-(trifluorometil)fenil]metil]-3,6-diidro-4-metil-2,6-diosso-1(2h)-pirimidinil]-1-feniletil]ammino]-butanoico (elagolix sale sodico) e intermedi di detto processo
TWI755055B (zh) * 2019-09-18 2022-02-11 台灣神隆股份有限公司 用於製備惡拉戈利鈉及其中間體的方法
WO2021064561A1 (en) * 2019-10-03 2021-04-08 Neuland Laboratories Limited An improved process for the preparation of elagolix sodium
CN112694445B (zh) * 2019-10-22 2023-07-28 成都倍特药业股份有限公司 一种噁拉戈利钠中间体的纯化方法
ES2822398B2 (es) * 2019-10-30 2022-03-02 Moehs Iberica Sl 3-((R)-2-(Amino-2-feniletil)-1-(2-fluoro-6-trifluorometilbencil)-5-yodo-6-metil-1H-pirimidin-2,4-diona o una sal de la misma, procedimiento para su preparación y su uso en la síntesis de elagolix
US20230072265A1 (en) * 2019-12-27 2023-03-09 Msn Laboratories Private Limited, R&D Center An improved process for the preparation of 4-({(1 r)-2-[5-(2-fluoro-3methoxyphenyl)-3-{[2-fluoro-6-(trifluoro methyl) phenyl]methyl}-4-methyl-2,6-dioxo-3,6dihydropyrimidin-1(2 h)-yl]-1-phenylethyl}amino)butanoic acid or its pharmaceutically acceptable salts
CN113125575B (zh) * 2019-12-31 2023-04-18 济南尚博生物科技有限公司 一种1-(2-氟-6-(三氟甲基)苄基)-6-甲基嘧啶-二酮的定量分析方法
CN111116490A (zh) * 2020-01-15 2020-05-08 奥锐特药业股份有限公司 一种噁拉戈利中间体水杨酸盐的制备与纯化方法
WO2021160597A1 (en) 2020-02-10 2021-08-19 ObsEva S.A. Biomarkers for oxytocin receptor antagonist therapy
CN115515592A (zh) * 2020-03-05 2022-12-23 艾伯维公司 施用恶拉戈利的方法
WO2021180862A1 (en) 2020-03-12 2021-09-16 Synthon B.V. Pharmaceutical compositions comprising elagolix sodium
CN111333548B (zh) * 2020-04-10 2022-04-26 江苏海悦康医药科技有限公司 1-(2-氟-6-(三氟甲基)苄基)脲的制备方法
CN113527213B (zh) * 2020-04-20 2023-01-03 上海英诺富成生物科技有限公司 促性激素释放激素受体拮抗剂及其用途
CN113683572A (zh) * 2020-05-18 2021-11-23 陈晓雯 噁拉戈利的中间体及其制备方法和应用
CA3185151A1 (en) 2020-05-29 2021-12-02 Myovant Sciences Gmbh Combination solid oral dosage forms of gonadotropin-releasing hormone antagonists
CN113880773A (zh) * 2020-07-02 2022-01-04 南京药石科技股份有限公司 一种噁拉戈利中间体的制备方法
CN112457258A (zh) * 2020-11-26 2021-03-09 诚达药业股份有限公司 一种噁拉戈利钠及其中间体的制备方法
EP4284374A1 (en) 2021-01-29 2023-12-06 Abbvie Inc. Methods of administrating elagolix
KR102656087B1 (ko) 2024-01-12 2024-04-09 주식회사 씨엠지 Led 소자의 에폭시 수지 코팅층 형성 방법
WO2026018221A1 (en) 2024-07-18 2026-01-22 ReproNovo SA Crystalline compositions for improving embryo implantation and methods of using the same

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR19990072101A (ko) * 1995-12-14 1999-09-27 폴락 돈나 엘. 고나도트로핀 분비 호르몬의 길항제

Family Cites Families (24)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU5844896A (en) 1995-06-01 1996-12-18 Takeda Chemical Industries Ltd. Tricyclic diazepines useful as gnrh receptor antagonists
EP0862573A1 (en) 1995-10-19 1998-09-09 Takeda Chemical Industries, Ltd. Thienopyridine derivatives as gonadotropin releasing hormone antagonists
CA2229201A1 (en) 1995-10-19 1997-04-24 Satoshi Sasaki Quinoline derivatives, their production and use
SK77498A3 (en) 1995-12-14 1999-01-11 Merck & Co Inc Nonpeptide derivatives, pharmaceutical composition containing them and their use
CA2240115A1 (en) 1995-12-14 1997-06-19 Wallace T. Ashton Antagonists of gonadotropin releasing hormone
CA2240048A1 (en) 1995-12-14 1997-06-19 Mark Goulet Antagonists of gonadotropin releasing hormone
WO1998055470A1 (en) 1997-06-05 1998-12-10 Merck & Co., Inc. Antagonists of gonadotropin releasing hormone
AU7806998A (en) 1997-06-05 1998-12-21 Merck & Co., Inc. Antagonists of gonadotropin releasing hormone
CA2292881A1 (en) 1997-06-05 1998-12-10 Merck & Co., Inc. Antagonists of gonadotropin releasing hormone
AU729663B2 (en) 1997-06-05 2001-02-08 Merck & Co., Inc. Antagonists of gonadotropin releasing hormone
US6313301B1 (en) 1997-08-13 2001-11-06 Takeda Chemical Industries, Ltd. Thienopyridine derivatives, their intermediates and production thereof
CA2372044A1 (en) 1999-05-14 2000-11-23 Neurocrine Biosciences, Inc. Imidazo- and pyrrolo[1,2-a]pyrimid-4-ones as gonadotropin-releasing hormone receptor antagonists
US20020065309A1 (en) 1999-08-04 2002-05-30 Ge Peng Novel Bicyclic and tricyclic pyrrolidine derivatives as GnRH antagonists
DE60022769T2 (de) 1999-10-15 2006-07-06 Neurocrine Biosciences, Inc., San Diego Gonadotropin freisetzenden hormon rezeptor antagonisten und ihre verwandten verwendungen
PT1255738E (pt) * 2000-01-25 2012-06-19 Neurocrine Biosciences Inc Antagonistas do receptor da hormona de libertação da gonadotrofina e métodos relacionados com os mesmos
SE0100566D0 (sv) 2001-02-20 2001-02-20 Astrazeneca Ab Compounds
AU2002324586B2 (en) 2001-08-02 2008-04-24 Neurocrine Biosciences, Inc. 1,3,5-triazine-2,4,6-triones, preparation and use as gonadotropin-releasing hormone receptor antagonists
JP2005500352A (ja) 2001-08-02 2005-01-06 ニューロクライン バイオサイエンシーズ， インコーポレイテッド ゴナドトロピン放出ホルモンレセプター（ＧｎＲＨ）アンタゴニストとしての１，２，４−トリアジン−３，５−ジオン
JP2005500356A (ja) 2001-08-02 2005-01-06 ニューロクライン バイオサイエンシーズ， インコーポレイテッド ゴナドトロピン放出ホルモンレセプターアンタゴニスト
WO2003011293A2 (en) 2001-08-02 2003-02-13 Neurocrine Biosciences, Inc. Pyridinone and pyridazinone derivatives as gonadotropin-releasing hormone receptor antagonists
JP2005505525A (ja) 2001-08-02 2005-02-24 ニューロクライン バイオサイエンシーズ， インコーポレイテッド 性腺刺激ホルモン放出ホルモンレセプターアンタゴニストおよびそれに関連する方法
US7015226B2 (en) * 2003-07-07 2006-03-21 Neurocrine Biosciences, Inc. Gonadotropin-releasing hormone receptor antagonists and methods relating thereto
CN100424078C (zh) * 2003-07-07 2008-10-08 纽罗克里生物科学有限公司 作为促性激素释放激素受体拮抗剂的嘧啶-2,4-二酮衍生物
ATE428427T1 (de) * 2003-07-07 2009-05-15 Neurocrine Biosciences Inc Pyrimidin-2,4-dion-derivate als gonadotropin freisetzende hormon-rezeptor-antagonisten

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR19990072101A (ko) * 1995-12-14 1999-09-27 폴락 돈나 엘. 고나도트로핀 분비 호르몬의 길항제

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