CN114174302A - 瑞卢戈利的固态形式 - Google Patents

瑞卢戈利的固态形式 Download PDF

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Publication number
CN114174302A
CN114174302A CN202080054641.9A CN202080054641A CN114174302A CN 114174302 A CN114174302 A CN 114174302A CN 202080054641 A CN202080054641 A CN 202080054641A CN 114174302 A CN114174302 A CN 114174302A
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CN
China
Prior art keywords
anhydrous
rilogeli
dmf
dcm
solution
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Pending
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CN202080054641.9A
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English (en)
Chinese (zh)
Inventor
N·帕斯卡利德斯
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Johnson Matthey PLC
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Johnson Matthey PLC
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Filing date
Publication date
Application filed by Johnson Matthey PLC filed Critical Johnson Matthey PLC
Publication of CN114174302A publication Critical patent/CN114174302A/zh
Pending legal-status Critical Current

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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)
CN202080054641.9A 2019-08-02 2020-07-31 瑞卢戈利的固态形式 Pending CN114174302A (zh)

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 (1)

Publication Number Publication Date
CN114174302A true CN114174302A (zh) 2022-03-11

Family

ID=72145496

Family Applications (1)

Application Number Title Priority Date Filing Date
CN202080054641.9A Pending CN114174302A (zh) 2019-08-02 2020-07-31 瑞卢戈利的固态形式

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=)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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

Families Citing this family (5)

* 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
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 (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101153042A (zh) * 2003-01-29 2008-04-02 武田药品工业株式会社 噻吩并嘧啶化合物及其用途
CN104703992A (zh) * 2012-09-28 2015-06-10 武田药品工业株式会社 噻吩并吡啶衍生物的制备方法

Family Cites Families (4)

* 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
US11306104B2 (en) * 2018-03-14 2022-04-19 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

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101153042A (zh) * 2003-01-29 2008-04-02 武田药品工业株式会社 噻吩并嘧啶化合物及其用途
CN104703992A (zh) * 2012-09-28 2015-06-10 武田药品工业株式会社 噻吩并吡啶衍生物的制备方法
US20150266891A1 (en) * 2012-09-28 2015-09-24 Takeda Pharmaceutical Company Limited Production method of thienopyrimidine derivative
EP3415517A1 (en) * 2012-09-28 2018-12-19 Takeda Pharmaceutical Company Limited Crystalline form of 1-(4-1-(2,6-difluorobenzyl)-5-dimethylaminomethyl-3-(6-methoxypyridazin-3-yl)-2,4-dioxo-1,2,3,4-tetrahydrothieno(2,3-d)-pyrimidin-6yl)phenyl)-3-methoxyurea

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
KAZUHIRO MIWA等: ""Discovery of 1-{4-[1-(2,6-Difluorobenzyl)-5-[(dimethylamino)methyl]-3-(6-methoxypyridazin-3-yl)-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl]phenyl}-3-methoxyurea (TAK-385) as a Potent, OrallyActive,Non-PeptideAntagonistoftheHumanGonadotropin-Releasing Hormone Receptor"" *

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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

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
JP2022542159A (ja) 2022-09-29

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