JP2022542159A - 固体形態レルゴリクス（Ｒｅｌｕｇｏｌｉｘ） - Google Patents

固体形態レルゴリクス（Ｒｅｌｕｇｏｌｉｘ） Download PDF

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Publication number
JP2022542159A
JP2022542159A JP2022505338A JP2022505338A JP2022542159A JP 2022542159 A JP2022542159 A JP 2022542159A JP 2022505338 A JP2022505338 A JP 2022505338A JP 2022505338 A JP2022505338 A JP 2022505338A JP 2022542159 A JP2022542159 A JP 2022542159A
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Prior art keywords
relugolix
anhydrous
dmf
theta
dcm
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Japanese (ja)
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JPWO2021026011A5 (https=
JP2022542159A5 (https=
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パスカリデス、ニコラス
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Johnson Matthey PLC
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Johnson Matthey PLC
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Publication of JP2022542159A publication Critical patent/JP2022542159A/ja
Publication of JPWO2021026011A5 publication Critical patent/JPWO2021026011A5/ja
Publication of JP2022542159A5 publication Critical patent/JP2022542159A5/ja
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems
    • 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
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C231/00—Preparation of carboxylic acid amides
    • C07C231/12—Preparation of carboxylic acid amides by reactions not involving the formation of carboxamide groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00—Carboxylic acid amides
    • C07C233/01—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C233/02—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having nitrogen atoms of carboxamide groups bound to hydrogen atoms or to carbon atoms of unsubstituted hydrocarbon radicals
    • C07C233/03—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having nitrogen atoms of carboxamide groups bound to hydrogen atoms or to carbon atoms of unsubstituted hydrocarbon radicals with carbon atoms of carboxamide groups bound to hydrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
JP2022505338A 2019-08-02 2020-07-31 固体形態レルゴリクス（Ｒｅｌｕｇｏｌｉｘ） Pending JP2022542159A (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201962882297P 2019-08-02 2019-08-02
US62/882,297 2019-08-02
PCT/US2020/044553 WO2021026011A1 (en) 2019-08-02 2020-07-31 Solid-state forms of relugolix

Publications (3)

Publication Number Publication Date
JP2022542159A true JP2022542159A (ja) 2022-09-29
JPWO2021026011A5 JPWO2021026011A5 (https=) 2023-08-01
JP2022542159A5 JP2022542159A5 (https=) 2023-08-01

Family

ID=72145496

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2022505338A Pending JP2022542159A (ja) 2019-08-02 2020-07-31 固体形態レルゴリクス（Ｒｅｌｕｇｏｌｉｘ）

Country Status (8)

Country Link
US (1) US20230374030A1 (https=)
EP (1) EP4007760A1 (https=)
JP (1) JP2022542159A (https=)
KR (1) KR20220047972A (https=)
CN (1) CN114174302A (https=)
BR (1) BR112022001002A2 (https=)
CA (1) CA3145993A1 (https=)
WO (1) WO2021026011A1 (https=)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US12441738B2 (en) 2018-03-14 2025-10-14 Assia Chemical Industries Ltd. Solid state forms of Relugolix
WO2021031148A1 (zh) * 2019-08-21 2021-02-25 深圳仁泰医药科技有限公司 促性腺素释放激素拮抗剂的晶型及其制备方法和用途
JP2022551316A (ja) 2019-10-10 2022-12-08 ミオバント サイエンシズ ゲーエムベーハー Ｎ－（４－（１－（２，６－ジフルオロベンジル）－５－（（ジメチルアミノ）メチル）－３－（６－メトキシ－３－ピリダジニル）－２，４－ジオキソ－１，２，３，４－テトラヒドロチエノ［２，３－ｄ］ピリミジン－６－イル）フェニル）－Ｎ’－メトキシ尿素の結晶形
CN113620972A (zh) * 2021-02-02 2021-11-09 奥锐特药业(天津)有限公司 瑞卢戈利新晶型及其制备方法
CN114031626A (zh) * 2021-12-09 2022-02-11 成都科圣原医药科技有限公司 一种瑞卢戈利的合成方法
WO2025037218A1 (en) * 2023-08-11 2025-02-20 Glenmark Life Sciences Limited Crystalline solvate of relugolix and a process for its preparation

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004067535A1 (ja) * 2003-01-29 2004-08-12 Takeda Pharmaceutical Company Limited チエノピリミジン化合物およびその用途
JP2015532262A (ja) * 2012-09-28 2015-11-09 武田薬品工業株式会社 チエノピリミジン誘導体の製造方法
WO2019178304A1 (en) * 2018-03-14 2019-09-19 Teva Pharmaceuticals International Gmbh Solid state forms of relugolix
EP3666776A1 (en) * 2018-12-11 2020-06-17 Sandoz AG Hydrate of a gonadotropin-releasing hormone receptor antagonist

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2010026993A1 (ja) 2008-09-03 2010-03-11 武田薬品工業株式会社 製剤における吸収性改善方法および吸収性が改善された製剤
TWI744224B (zh) 2015-02-26 2021-11-01 日商武田藥品工業股份有限公司 固形製劑

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004067535A1 (ja) * 2003-01-29 2004-08-12 Takeda Pharmaceutical Company Limited チエノピリミジン化合物およびその用途
JP2015532262A (ja) * 2012-09-28 2015-11-09 武田薬品工業株式会社 チエノピリミジン誘導体の製造方法
WO2019178304A1 (en) * 2018-03-14 2019-09-19 Teva Pharmaceuticals International Gmbh Solid state forms of relugolix
EP3666776A1 (en) * 2018-12-11 2020-06-17 Sandoz AG Hydrate of a gonadotropin-releasing hormone receptor antagonist

Non-Patent Citations (7)

* Cited by examiner, † Cited by third party
Title
JOURNAL OF MEDICINAL CHEMISTRY, vol. 54(14), JPN6024021227, 2011, pages 4998 - 5012, ISSN: 0005557634 *
塩路雄作, 固形製剤の製造技術, vol. 普及版, JPN6011023134, 27 January 2003 (2003-01-27), pages 9 - 12, ISSN: 0005557637 *
平山令明編, 有機化合物結晶作製ハンドブック −原理とノウハウ−, JPN6011053065, 25 July 2008 (2008-07-25), pages 57 - 84, ISSN: 0005557635 *
浅原 照三, 溶剤ハンドブック, JPN6011026738, 1985, ISSN: 0005557638 *
社団法人日本化学会, 化学便覧応用化学編第６版, vol. 第4章化学合成技術, JPN6009048258, 30 January 2003 (2003-01-30), pages 178, ISSN: 0005557636 *
芦澤 一英: "塩・結晶形の最適化と結晶化技術", PHARM TECH JAPAN, vol. 18, no. 10, JPN6013060608, 2002, pages 81 - 96, ISSN: 0005557639 *
芦澤一英, 医薬品の多形現象と晶析の化学, JPN6015027444, 2002, pages 273 - 278, ISSN: 0005557640 *

Also Published As

Publication number Publication date
KR20220047972A (ko) 2022-04-19
BR112022001002A2 (pt) 2022-04-12
EP4007760A1 (en) 2022-06-08
CA3145993A1 (en) 2021-02-11
WO2021026011A1 (en) 2021-02-11
US20230374030A1 (en) 2023-11-23
CN114174302A (zh) 2022-03-11

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