AU2004257639B2 - Pyrimidine-2, 4-dione derivatives as gonadotropin-releasing hormone receptor antagonists - Google Patents
Pyrimidine-2, 4-dione derivatives as gonadotropin-releasing hormone receptor antagonists Download PDFInfo
- Publication number
- AU2004257639B2 AU2004257639B2 AU2004257639A AU2004257639A AU2004257639B2 AU 2004257639 B2 AU2004257639 B2 AU 2004257639B2 AU 2004257639 A AU2004257639 A AU 2004257639A AU 2004257639 A AU2004257639 A AU 2004257639A AU 2004257639 B2 AU2004257639 B2 AU 2004257639B2
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- Prior art keywords
- compound
- fluoro
- dione
- pyrimidine
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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)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Endocrinology (AREA)
- Diabetes (AREA)
- Reproductive Health (AREA)
- Immunology (AREA)
- Biomedical Technology (AREA)
- Dermatology (AREA)
- Urology & Nephrology (AREA)
- Anesthesiology (AREA)
- Epidemiology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Gynecology & Obstetrics (AREA)
- Pregnancy & Childbirth (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)
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 |
|---|---|
| AU2004257639A1 AU2004257639A1 (en) | 2005-01-27 |
| AU2004257639B2 true AU2004257639B2 (en) | 2011-01-06 |
Family
ID=34079121
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AU2004257639A Expired AU2004257639B2 (en) | 2003-07-07 | 2004-07-06 | Pyrimidine-2, 4-dione derivatives as gonadotropin-releasing hormone receptor antagonists |
Country Status (24)
Families Citing this family (79)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MXPA02006848A (es) * | 2000-01-25 | 2002-12-13 | Neurocrine Bioscience Inc | Antagonistas del receptor de la hormona liberadora de gonadotropina. |
| WO2005007633A1 (en) * | 2003-07-07 | 2005-01-27 | Neurocrine Biosciences, Inc. | Gonadotropin-releasing hormone receptor antagonists and methods relating thereto |
| DE602004016516D1 (de) * | 2003-07-07 | 2008-10-23 | Neurocrine Biosciences Inc | Pyrimidin-2,4-dion-derivate als gonadotropin freisetzende hormon-rezeptor-antagonisten |
| ATE428427T1 (de) * | 2003-07-07 | 2009-05-15 | Neurocrine Biosciences Inc | Pyrimidin-2,4-dion-derivate als gonadotropin freisetzende hormon-rezeptor-antagonisten |
| CN102140090A (zh) * | 2004-03-15 | 2011-08-03 | 武田药品工业株式会社 | 二肽基肽酶抑制剂 |
| MX2009010828A (es) | 2007-04-06 | 2009-10-29 | Neurocrine Biosciences Inc | Antagonistas del receptor de la hormona liberadora de gonadotropina y metodos relacionados con los mismos. |
| PA8775701A1 (es) | 2007-04-06 | 2009-04-23 | Neurocrine Biosciences Inc | Antagonista de los receptores de la hormona liberadora de gonadotropina y procedimientos relacionados con ellos |
| MX2010003371A (es) | 2007-09-28 | 2010-05-05 | Intrexon Corp | Constructos interruptores genicos terapeuticos y biorreactores para la expresion de moleculas bioterapeuticas y usos de los mismos. |
| US8765948B2 (en) | 2007-11-07 | 2014-07-01 | Neurocrine Biosciences, Inc. | Processes for the preparation of uracil derivatives |
| WO2011062437A2 (ko) | 2009-11-20 | 2011-05-26 | 에스케이케미칼주식회사 | 고나도트로핀 방출 호르몬 수용체 길항제, 이의 제조방법 및 이를 함유하는 약제학적 조성물 |
| WO2014143669A1 (en) | 2013-03-15 | 2014-09-18 | AbbVie Inc . | Compositions for use in treating heavy menstrual bleeding and uterine fibroids |
| 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 |
| AU2017300026B2 (en) | 2016-07-21 | 2023-07-13 | 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 |
| PT3518932T (pt) | 2016-09-30 | 2025-01-16 | Takeda Pharmaceuticals Co | Tratamento do cancro da próstata |
| SMT202200254T1 (it) | 2016-09-30 | 2022-07-21 | Takeda Pharmaceuticals Co | Metodi di trattamento di fibromi uterini ed endometriosi |
| WO2018060438A1 (en) | 2016-09-30 | 2018-04-05 | Myovant Sciences Gmbh | Methods of treating female infertility |
| 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 |
| WO2018189212A1 (en) | 2017-04-12 | 2018-10-18 | Sandoz Ag | Acid addition salts of an orally available gonadotropin-releasing hormone receptor antagonist |
| 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 |
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| US11980621B2 (en) | 2017-06-05 | 2024-05-14 | Kissei Pharmaceutical Co., Ltd. | Gonadotropin-releasing hormone antagonist dosing regimens for the treatment of endometriosis |
| 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 |
| EP3668515A4 (en) * | 2017-08-18 | 2021-05-12 | Abbvie Inc. | PHARMACEUTICAL FORMULATIONS FOR THE TREATMENT OF ENDOMETRIOSIS, UTERINE FIBROMAS, 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 |
| 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 |
| US11377426B2 (en) | 2017-12-05 | 2022-07-05 | Suzhou Pengxu Pharmatech Co., Ltd. | Processes to produce elagolix |
| 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 |
| 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 |
| EP3781167A4 (en) | 2018-04-19 | 2022-02-23 | Abbvie Inc. | METHODS OF TREATMENT OF HEAVY PERIODS |
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| EP3572406A1 (en) | 2018-10-17 | 2019-11-27 | Sandoz Ag | Acid addition salt of elagolix and related compounds |
| US12280052B2 (en) | 2018-10-29 | 2025-04-22 | Kissei Pharmaceutical Co., Ltd. | 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 |
| WO2020150170A1 (en) | 2019-01-15 | 2020-07-23 | Lupin Inc. | Deuterated elagolix-like compositions and methods |
| 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 |
| 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 |
| 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 |
| 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 |
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| 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 |
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| 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 |
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