CA3145993A1 - Solid-state forms of relugolix - Google Patents

Solid-state forms of relugolix Download PDF

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Publication number
CA3145993A1
CA3145993A1 CA3145993A CA3145993A CA3145993A1 CA 3145993 A1 CA3145993 A1 CA 3145993A1 CA 3145993 A CA3145993 A CA 3145993A CA 3145993 A CA3145993 A CA 3145993A CA 3145993 A1 CA3145993 A1 CA 3145993A1
Authority
CA
Canada
Prior art keywords
relugolix
anhydrous
solvent
dmf
dcm
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.)
Pending
Application number
CA3145993A
Other languages
English (en)
French (fr)
Inventor
Nicholas PASCHALIDES
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Macfarlan Smith Ltd
Original Assignee
Johnson Matthey PLC
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Johnson Matthey PLC filed Critical Johnson Matthey PLC
Publication of CA3145993A1 publication Critical patent/CA3145993A1/en
Pending legal-status Critical Current

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02Heterocyclic 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
    • C07D495/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C231/00Preparation of carboxylic acid amides
    • C07C231/12Preparation of carboxylic acid amides by reactions not involving the formation of carboxamide groups
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00Carboxylic acid amides
    • C07C233/01Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C233/02Carboxylic 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
    • C07C233/03Carboxylic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs

Landscapes

  • 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)
CA3145993A 2019-08-02 2020-07-31 Solid-state forms of relugolix Pending CA3145993A1 (en)

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
CA3145993A1 true CA3145993A1 (en) 2021-02-11

Family

ID=72145496

Family Applications (1)

Application Number Title Priority Date Filing Date
CA3145993A Pending CA3145993A1 (en) 2019-08-02 2020-07-31 Solid-state forms of 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

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7300935B2 (en) * 2003-01-29 2007-11-27 Takeda Pharmaceutical Company Thienopyrimidine compounds and use thereof
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
AR092707A1 (es) * 2012-09-28 2015-04-29 Takeda Pharmaceuticals Co Metodo de produccion de derivado de tienopirimidina
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

Also Published As

Publication number Publication date
KR20220047972A (ko) 2022-04-19
BR112022001002A2 (pt) 2022-04-12
EP4007760A1 (en) 2022-06-08
WO2021026011A1 (en) 2021-02-11
US20230374030A1 (en) 2023-11-23
JP2022542159A (ja) 2022-09-29
CN114174302A (zh) 2022-03-11

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Effective date: 20260116