JP7713934B2 - 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溶媒和形 - Google Patents
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溶媒和形Info
- Publication number
- JP7713934B2 JP7713934B2 JP2022521570A JP2022521570A JP7713934B2 JP 7713934 B2 JP7713934 B2 JP 7713934B2 JP 2022521570 A JP2022521570 A JP 2022521570A JP 2022521570 A JP2022521570 A JP 2022521570A JP 7713934 B2 JP7713934 B2 JP 7713934B2
- Authority
- JP
- Japan
- Prior art keywords
- compound
- methoxyurea
- tetrahydrothieno
- difluorobenzyl
- dioxo
- 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.)
- Active
Links
Classifications
-
- 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
- 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
-
- 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
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0014—Skin, i.e. galenical aspects of topical compositions
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0034—Urogenital system, e.g. vagina, uterus, cervix, penis, scrotum, urethra, bladder; Personal lubricants
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Endocrinology (AREA)
- Reproductive Health (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201962913606P | 2019-10-10 | 2019-10-10 | |
| US62/913,606 | 2019-10-10 | ||
| PCT/EP2020/078475 WO2021069700A1 (en) | 2019-10-10 | 2020-10-09 | Crystalline solvated forms of n-(4-(1-(2,6-difluorobenzyl)-5- ((dimethylamino)methyl)-3-(6-methoxy-3-pyridazinyl)-2,4-dioxo-1,2,3,4- tetrahydrothieno[2,3-d]pyrimidin-6-yl)phenyl)-n'-methoxyurea |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2022551525A JP2022551525A (ja) | 2022-12-09 |
| JP2022551525A5 JP2022551525A5 (enExample) | 2023-10-17 |
| JP7713934B2 true JP7713934B2 (ja) | 2025-07-28 |
Family
ID=72852647
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2022521570A Active JP7713934B2 (ja) | 2019-10-10 | 2020-10-09 | 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溶媒和形 |
Country Status (5)
| Country | Link |
|---|---|
| US (1) | US12655154B2 (enExample) |
| EP (1) | EP4041738A1 (enExample) |
| JP (1) | JP7713934B2 (enExample) |
| CN (1) | CN115175912B (enExample) |
| WO (1) | WO2021069700A1 (enExample) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2018060501A2 (en) | 2016-09-30 | 2018-04-05 | Myovant Sciences Gmbh | Methods of treating uterine fibroids and endometriosis |
| US12441738B2 (en) | 2018-03-14 | 2025-10-14 | Assia Chemical Industries Ltd. | Solid state forms of Relugolix |
| 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 |
| WO2021069700A1 (en) | 2019-10-10 | 2021-04-15 | Myovant Sciences Gmbh | Crystalline solvated forms of n-(4-(1-(2,6-difluorobenzyl)-5- ((dimethylamino)methyl)-3-(6-methoxy-3-pyridazinyl)-2,4-dioxo-1,2,3,4- tetrahydrothieno[2,3-d]pyrimidin-6-yl)phenyl)-n'-methoxyurea |
| BR112022023937A2 (pt) | 2020-05-29 | 2022-12-27 | Myovant Sciences Gmbh | Formas de dosagem oral sólidas de combinação de antagonistas do hormônio liberador de gonadotropina |
| WO2022101303A1 (en) | 2020-11-11 | 2022-05-19 | Myovant Sciences Gmbh | Methods of administering relugolix |
| 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 |
| WO2022214645A1 (en) | 2021-04-09 | 2022-10-13 | Farmhispania Group, S.L. | Processes and intermediates for the preparation of relugolix |
| WO2023066941A1 (en) | 2021-10-18 | 2023-04-27 | Myovant Sciences Gmbh | Crystalline form of an ethanol solvate of n-(4-(1-(2,6-difluorobenzyl)-5-((dimethylamino)methyl)-3-(6-methoxy-3-pyridazinyl)-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl)phenyl)-n'-methoxyurea |
Citations (3)
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| 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 |
| WO2018060463A2 (en) | 2016-09-30 | 2018-04-05 | Myovant Sciences Gmbh | Treatment of prostate cancer |
| WO2019178304A1 (en) | 2018-03-14 | 2019-09-19 | Teva Pharmaceuticals International Gmbh | Solid state forms of relugolix |
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| WO2021069700A1 (en) | 2019-10-10 | 2021-04-15 | Myovant Sciences Gmbh | Crystalline solvated forms of n-(4-(1-(2,6-difluorobenzyl)-5- ((dimethylamino)methyl)-3-(6-methoxy-3-pyridazinyl)-2,4-dioxo-1,2,3,4- tetrahydrothieno[2,3-d]pyrimidin-6-yl)phenyl)-n'-methoxyurea |
| 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 |
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| BR112022023937A2 (pt) | 2020-05-29 | 2022-12-27 | Myovant Sciences Gmbh | Formas de dosagem oral sólidas de combinação de antagonistas do hormônio liberador de gonadotropina |
| US11655256B1 (en) | 2020-11-06 | 2023-05-23 | Macfarlan Smith Limited | Processes for making a solid-state form of relugolix |
| WO2022101303A1 (en) | 2020-11-11 | 2022-05-19 | Myovant Sciences Gmbh | Methods of administering relugolix |
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| CN115947734A (zh) * | 2021-10-09 | 2023-04-11 | 江苏希迪制药有限公司 | 瑞卢戈利溶剂化物的晶型及其制备方法 |
| WO2023066941A1 (en) | 2021-10-18 | 2023-04-27 | Myovant Sciences Gmbh | Crystalline form of an ethanol solvate of n-(4-(1-(2,6-difluorobenzyl)-5-((dimethylamino)methyl)-3-(6-methoxy-3-pyridazinyl)-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl)phenyl)-n'-methoxyurea |
| WO2023119333A1 (en) | 2021-12-25 | 2023-06-29 | Dr. Reddy’S Laboratories Limited | Process for preparation of relugolix and its intermediates |
| IN202221021078A (enExample) | 2022-04-08 | 2023-10-13 | ||
| CN115417883B (zh) | 2022-09-16 | 2024-08-27 | 浙江科聚生物医药有限公司 | 一种瑞卢戈利的晶型及其制备方法 |
-
2020
- 2020-10-09 WO PCT/EP2020/078475 patent/WO2021069700A1/en not_active Ceased
- 2020-10-09 EP EP20790251.1A patent/EP4041738A1/en active Pending
- 2020-10-09 CN CN202080082800.6A patent/CN115175912B/zh active Active
- 2020-10-09 JP JP2022521570A patent/JP7713934B2/ja active Active
-
2022
- 2022-04-08 US US17/716,965 patent/US12655154B2/en active Active
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| WO2018060463A2 (en) | 2016-09-30 | 2018-04-05 | Myovant Sciences Gmbh | Treatment of prostate cancer |
| WO2019178304A1 (en) | 2018-03-14 | 2019-09-19 | Teva Pharmaceuticals International Gmbh | Solid state forms of relugolix |
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Also Published As
| Publication number | Publication date |
|---|---|
| CN115175912A (zh) | 2022-10-11 |
| CN115175912B (zh) | 2025-04-11 |
| JP2022551525A (ja) | 2022-12-09 |
| US12655154B2 (en) | 2026-06-16 |
| US20220372044A1 (en) | 2022-11-24 |
| WO2021069700A1 (en) | 2021-04-15 |
| EP4041738A1 (en) | 2022-08-17 |
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