JP2011088902A5 - - Google Patents

Download PDF

Info

Publication number
JP2011088902A5
JP2011088902A5 JP2010265830A JP2010265830A JP2011088902A5 JP 2011088902 A5 JP2011088902 A5 JP 2011088902A5 JP 2010265830 A JP2010265830 A JP 2010265830A JP 2010265830 A JP2010265830 A JP 2010265830A JP 2011088902 A5 JP2011088902 A5 JP 2011088902A5
Authority
JP
Japan
Prior art keywords
alkyl
hydrogen
composition
hormone
stereoisomer
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Granted
Application number
JP2010265830A
Other languages
English (en)
Japanese (ja)
Other versions
JP5226760B2 (ja
JP2011088902A (ja
Filing date
Publication date
Application filed filed Critical
Publication of JP2011088902A publication Critical patent/JP2011088902A/ja
Publication of JP2011088902A5 publication Critical patent/JP2011088902A5/ja
Application granted granted Critical
Publication of JP5226760B2 publication Critical patent/JP5226760B2/ja
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

Links

JP2010265830A 2003-07-07 2010-11-29 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としてのピリミジン−2,4−ジオン誘導体 Expired - Lifetime JP5226760B2 (ja)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US48543403P 2003-07-07 2003-07-07
US60/485,434 2003-07-07

Related Parent Applications (1)

Application Number Title Priority Date Filing Date
JP2006518842A Division JP4722844B2 (ja) 2003-07-07 2004-07-06 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としてのピリミジン−2,4−ジオン誘導体

Publications (3)

Publication Number Publication Date
JP2011088902A JP2011088902A (ja) 2011-05-06
JP2011088902A5 true JP2011088902A5 (enExample) 2012-01-19
JP5226760B2 JP5226760B2 (ja) 2013-07-03

Family

ID=34079121

Family Applications (2)

Application Number Title Priority Date Filing Date
JP2006518842A Expired - Lifetime JP4722844B2 (ja) 2003-07-07 2004-07-06 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としてのピリミジン−2,4−ジオン誘導体
JP2010265830A Expired - Lifetime JP5226760B2 (ja) 2003-07-07 2010-11-29 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としてのピリミジン−2,4−ジオン誘導体

Family Applications Before (1)

Application Number Title Priority Date Filing Date
JP2006518842A Expired - Lifetime JP4722844B2 (ja) 2003-07-07 2004-07-06 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としてのピリミジン−2,4−ジオン誘導体

Country Status (24)

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

Families Citing this family (79)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ATE548357T1 (de) * 2000-01-25 2012-03-15 Neurocrine Biosciences Inc Gonadotropin freisetzende hormon rezeptor antagonisten und ihre verwandten verfahren
ATE407679T1 (de) * 2003-07-07 2008-09-15 Neurocrine Biosciences Inc Pyrimidin-2,4-dion-derivate als gonadotropin freisetzende hormon-rezeptor-antagonisten
AU2004257636B2 (en) 2003-07-07 2011-01-06 Neurocrine Biosciences, Inc. Pyrimidine-2,4-dione derivatives as gonadotropin-releasing hormone receptor antagonists
JP4673847B2 (ja) * 2003-07-07 2011-04-20 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
CN102134230B (zh) * 2004-03-15 2019-06-28 武田药品工业株式会社 二肽基肽酶抑制剂
AR065947A1 (es) 2007-04-06 2009-07-15 Neurocrine Biosciences Inc Antagonistas de los receptores de la hormona liberadora de gonadodropina (gnrh)
KR101506750B1 (ko) 2007-04-06 2015-03-27 뉴로크린 바이오사이언시즈 인코퍼레이티드 고나도트로핀-방출 호르몬 수용체 길항제 및 그와 관련된 방법
JP2010540534A (ja) 2007-09-28 2010-12-24 イントレキソン コーポレーション 生体治療分子の発現のための治療遺伝子スイッチ構築物およびバイオリアクター、ならびにその使用
US8765948B2 (en) 2007-11-07 2014-07-01 Neurocrine Biosciences, Inc. Processes for the preparation of uracil derivatives
ES2549502T3 (es) 2009-11-20 2015-10-28 Sk Chemicals Co., Ltd. Antagonistas de receptores de gonadoliberina, método de fabricación de los mismos, y composición farmacéutica que los contienen
EP3384930A1 (en) 2013-03-15 2018-10-10 AbbVie Inc. Compositions for use in treating heavy menstrual bleeding
EP2881391A1 (en) 2013-12-05 2015-06-10 Bayer Pharma Aktiengesellschaft Spiroindoline carbocycle derivatives and pharmaceutical compositions thereof
US10821152B2 (en) 2014-08-26 2020-11-03 Betanien Hospital Methods, agents and compositions for treatment of inflammatory conditions
US20190321363A1 (en) * 2016-06-20 2019-10-24 Dr. Reddy's Laboratories Limited Process for the preparation of elagolix sodium and its polymorph
WO2018015497A2 (en) 2016-07-21 2018-01-25 ObsEva S.A. Oxytocin antagonist dosing regimens for promoting embryo implantation and preventing miscarriage
US12043558B2 (en) 2016-08-23 2024-07-23 Swan Analytishce Instrumente AG Device and method for the electrodeionization of a liquid
EP3518952A1 (en) 2016-09-30 2019-08-07 Myovant Sciences GmbH Methods of treating female infertility
FI3518932T3 (fi) 2016-09-30 2025-02-03 Sumitomo Pharma Switzerland Gmbh Eturauhassyövän hoito
DK3518933T4 (da) 2016-09-30 2025-04-22 Takeda Pharmaceuticals Co Fremgangsmåder til behandling af uterusfibromer og endometriose
ES2983735T3 (es) 2016-12-14 2024-10-24 Purdue Research Foundation Conjugados del receptor de la hormona liberadora de hormona luteinizante (LHRH-R) y usos de los mismos
EP3388421B1 (en) 2017-04-13 2019-12-04 Sandoz AG Acid addition salts of an orally available gonadotropin-releasing hormone receptor antagonist
AU2018251951B2 (en) 2017-04-12 2020-09-03 Sandoz Ag Acid addition salts of an orally available gonadotropin-releasing hormone receptor antagonist
PT3388422T (pt) 2017-04-13 2020-02-18 Sandoz Ag Dispersão sólida amorfa de um antagonista dos recetores de hormonas libertadoras de gonadotrofina disponível por via oral
WO2018198086A1 (en) * 2017-04-28 2018-11-01 Lupin Limited Process for the preparation of elagolix and pharmaceutically acceptable salts thereof
KR20250117836A (ko) 2017-06-05 2025-08-05 깃세이 야쿠힌 고교 가부시키가이샤 자궁내막증의 치료를 위한 고나도트로핀 방출 호르몬 길항제 투약 요법
WO2018224063A2 (en) * 2017-06-08 2018-12-13 Zentiva, K.S. Solid forms of elagolix
WO2019036713A1 (en) 2017-08-18 2019-02-21 Abbvie Inc. SOLID PHARMACEUTICAL FORMULATIONS FOR THE TREATMENT OF ENDOMETRIOSIS, UTERINE FIBROIDS, POLYKYSTIC OVARY SYNDROME AND ADENOMYOSIS
WO2019036712A1 (en) 2017-08-18 2019-02-21 Abbvie Inc. PHARMACEUTICAL FORMULATIONS FOR THE TREATMENT OF ENDOMETRIOSIS, UTERINE FIBROIDS, POLYKYSTIC OVARY SYNDROME OR ADENOMYOSIS
CN111698992A (zh) * 2017-08-18 2020-09-22 艾伯维公司 用于治疗子宫内膜异位症、子宫肌瘤、多囊卵巢综合症或子宫腺肌症的药物配制物
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
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
WO2019112968A1 (en) 2017-12-05 2019-06-13 Peng Wang Processes to produce elagolix
EP3724167A1 (en) 2017-12-11 2020-10-21 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
IL278082B2 (en) 2018-04-19 2025-03-01 Abbvie Inc Methods of treating heavy menstrual bleeding
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
WO2020023459A1 (en) 2018-07-23 2020-01-30 Abbvie Inc. Elagolix sodium compositions and processes
CA3107597A1 (en) * 2018-08-01 2020-02-06 Abbvie Inc. Dosing regimens for elagolix
EP3572406A1 (en) 2018-10-17 2019-11-27 Sandoz Ag Acid addition salt of elagolix and related compounds
EP3873465B1 (en) 2018-10-29 2025-01-15 Kissei Pharmaceutical Co., Ltd. Compositions and methods for the treatment of adenomyosis and rectovaginal endometriosis
EP3876943A2 (en) 2018-11-07 2021-09-15 ObsEva S.A. 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
MX2021008457A (es) 2019-01-15 2021-10-01 Lupin Inc Composiciones de tipo elagolix deuterado y métodos.
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
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
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
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
US20220242831A1 (en) * 2019-05-24 2022-08-04 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
US20220305017A1 (en) 2019-08-08 2022-09-29 ObsEva S.A. Compositions and methods for the treatment of estrogen-dependent disorders
CN114364384A (zh) 2019-08-08 2022-04-15 奥布赛瓦股份公司 用于治疗雌激素依赖性病症的GnRH拮抗剂
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
WO2021044230A1 (en) * 2019-09-03 2021-03-11 Industriale Chimica S.R.L. Process for the synthesis of the sodium salt of 4-[[(lr)-2-[5-(2-fluoro-3-methoxyphenyl)-3-[[2-fluoro-6-(trifluoromethyl)-phenyl]methyl]-3,6-dihydro-4-methyl-2,6-dioxo-l(2h)-pyrimidinyl]-l- phenylethyl]amino]-butanoic acid (elagolix sodium salt) and intermediates of said process
CN114667141A (zh) 2019-09-03 2022-06-24 奥布赛瓦股份公司 用于促进胚胎移植和预防流产的催产素拮抗剂给药方案
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
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
US20220257597A1 (en) 2021-01-29 2022-08-18 Abbvie Inc. Methods of Administering Elagolix
KR102656087B1 (ko) 2024-01-12 2024-04-09 주식회사 씨엠지 Led 소자의 에폭시 수지 코팅층 형성 방법

Family Cites Families (25)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5866567A (en) 1995-06-01 1999-02-02 Takeda Chemical Industries, Ltd. Diazepinones, their production and use
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
IL124613A0 (en) 1995-12-14 1998-12-06 Merck & Co Inc Antagonists of gonadotropin releasing hormone
JP3230818B2 (ja) * 1995-12-14 2001-11-19 メルク エンド カンパニー インコーポレーテッド ゴナドトロピン放出ホルモン拮抗剤
AU704937B2 (en) 1995-12-14 1999-05-06 Merck & Co., Inc. Antagonists of gonadotropin releasing hormone
PL327397A1 (en) 1995-12-14 1998-12-07 Merck & Co Inc Antagonists of a gonadothropin liberating hormone
CA2291829A1 (en) 1997-06-05 1998-12-10 Merck & Co., Inc. Antagonists of gonadotropin releasing hormone
AU729752B2 (en) 1997-06-05 2001-02-08 Merck & Co., Inc. Antagonists of gonadotropin releasing hormone
EP0986557A4 (en) 1997-06-05 2001-03-14 Merck & Co Inc GONADOTROPIN RELEASING HORMON ANTAGONISTS
WO1998055116A1 (en) 1997-06-05 1998-12-10 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
WO2000069859A1 (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
KR20020045609A (ko) 1999-10-15 2002-06-19 추후기재 고나도트로핀-분비 호르몬 수용체 길항제 및 이와 관련된방법
ATE548357T1 (de) * 2000-01-25 2012-03-15 Neurocrine Biosciences Inc Gonadotropin freisetzende hormon rezeptor antagonisten und ihre verwandten verfahren
SE0100566D0 (sv) 2001-02-20 2001-02-20 Astrazeneca Ab Compounds
US6740656B2 (en) 2001-08-02 2004-05-25 Neurocrine Biosciences, Inc. Gonadotropin-releasing hormone receptor antagonists and methods relating thereto
WO2003011293A2 (en) 2001-08-02 2003-02-13 Neurocrine Biosciences, Inc. Pyridinone and pyridazinone derivatives as gonadotropin-releasing hormone receptor antagonists
EP1411945A1 (en) 2001-08-02 2004-04-28 Neurocrine Biosciences, Inc. Substituted pyridin-4-ones and their use as gonadotropin-releasing hormone receptor antagonists
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
WO2003011841A1 (en) 2001-08-02 2003-02-13 Neurocrine Biosciences, Inc. 1,2,4-triazin-3,5-diones as gonadotropin-releasing hormone receptor (gnrh) antagonists
AU2004257636B2 (en) * 2003-07-07 2011-01-06 Neurocrine Biosciences, Inc. Pyrimidine-2,4-dione derivatives as gonadotropin-releasing hormone receptor antagonists
JP4673847B2 (ja) * 2003-07-07 2011-04-20 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
ATE407679T1 (de) * 2003-07-07 2008-09-15 Neurocrine Biosciences Inc Pyrimidin-2,4-dion-derivate als gonadotropin freisetzende hormon-rezeptor-antagonisten

Similar Documents

Publication Publication Date Title
JP2011088902A5 (enExample)
JP2010536766A5 (enExample)
JP2009523760A5 (enExample)
JP2012092103A5 (enExample)
JP2011137006A5 (enExample)
JP2008044952A5 (enExample)
EP2344497A4 (en) AZAINDOL DERIVATIVES AS CRTH2 RECEPTOR ANTAGONISTS
JP2007269812A5 (enExample)
JP2009149903A5 (enExample)
EP2346865A4 (en) INDOIND DERIVATIVES AS CRTH2 RECEPTOR ANTAGONISTS
EP2620432A3 (en) Diarylhydantoin compounds
JP2013542261A5 (enExample)
JP2011207901A5 (enExample)
JP2014500861A5 (enExample)
HRP20090235A2 (hr) Karbonilirani (aza) cikloheksani kao ligandi dopaminskog receptora d<sub>3</sub>
UA92670C2 (ru) Пиразолиновые соединения и их фармацевтическое применение, композиция на их основе
JP2011227454A5 (enExample)
JP2012533546A5 (enExample)
JP2013508417A5 (enExample)
JP2008540554A5 (enExample)
JP2012510957A5 (enExample)
JP2011088926A5 (enExample)
JP2010508310A5 (enExample)
CA2745699A1 (en) Substituted benzyl and phenylsulfonyl triazolones, and use thereof
JP2012528813A5 (enExample)