CN115279769A - N-(4-(1-(2,6-二氟苄基)-5-((二甲基氨基)甲基)-3-(6-甲氧基-3-哒嗪基)-2,4-二氧代-1,2,3,4-四氢噻吩并[2,3-d]嘧啶-6-基)苯基)-n’-甲氧基脲的结晶形式 - Google Patents
N-(4-(1-(2,6-二氟苄基)-5-((二甲基氨基)甲基)-3-(6-甲氧基-3-哒嗪基)-2,4-二氧代-1,2,3,4-四氢噻吩并[2,3-d]嘧啶-6-基)苯基)-n’-甲氧基脲的结晶形式 Download PDFInfo
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- CN115279769A CN115279769A CN202080084633.9A CN202080084633A CN115279769A CN 115279769 A CN115279769 A CN 115279769A CN 202080084633 A CN202080084633 A CN 202080084633A CN 115279769 A CN115279769 A CN 115279769A
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- 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
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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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- 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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- Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
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Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201962913560P | 2019-10-10 | 2019-10-10 | |
| US62/913560 | 2019-10-10 | ||
| PCT/EP2020/078493 WO2021069711A1 (en) | 2019-10-10 | 2020-10-09 | Crystalline 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 (1)
| Publication Number | Publication Date |
|---|---|
| CN115279769A true CN115279769A (zh) | 2022-11-01 |
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| Application Number | Title | Priority Date | Filing Date |
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| CN202080084633.9A Pending CN115279769A (zh) | 2019-10-10 | 2020-10-09 | N-(4-(1-(2,6-二氟苄基)-5-((二甲基氨基)甲基)-3-(6-甲氧基-3-哒嗪基)-2,4-二氧代-1,2,3,4-四氢噻吩并[2,3-d]嘧啶-6-基)苯基)-n’-甲氧基脲的结晶形式 |
Country Status (5)
| Country | Link |
|---|---|
| US (2) | US12338249B2 (https=) |
| EP (1) | EP4041739A1 (https=) |
| JP (1) | JP2022551316A (https=) |
| CN (1) | CN115279769A (https=) |
| WO (1) | WO2021069711A1 (https=) |
Cited By (1)
| 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 (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2912929T5 (en) | 2016-09-30 | 2025-05-09 | Sumitomo Pharma Switzerland 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 |
| CA3185151A1 (en) | 2020-05-29 | 2021-12-02 | Myovant Sciences Gmbh | Combination solid oral dosage forms of gonadotropin-releasing hormone antagonists |
| WO2022101303A1 (en) | 2020-11-11 | 2022-05-19 | Myovant Sciences Gmbh | Methods of administering relugolix |
| WO2022214645A1 (en) | 2021-04-09 | 2022-10-13 | Farmhispania Group, S.L. | Processes and intermediates for the preparation of relugolix |
| JP2024540922A (ja) | 2021-10-18 | 2024-11-06 | スミトモ ファーマ スウィッツァーランド 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’-メトキシ尿素のエタノール溶媒和物の結晶形 |
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| US20060160829A1 (en) * | 2003-01-29 | 2006-07-20 | Nobuo Cho | Thienopyrimidine compounds and use thereof |
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| CA3010509A1 (en) * | 2016-01-11 | 2017-07-20 | Janssen Pharmaceutica Nv | Substituted thiohydantoin derivatives as androgen receptor antagonists |
| US20190224196A1 (en) * | 2016-09-30 | 2019-07-25 | Myovant Sciences Gmbh | Treatment of prostate cancer |
| US20190262346A1 (en) * | 2016-09-30 | 2019-08-29 | Myovant Sciences Gmbh | Methods of treating uterine fibroids and endometriosis |
| WO2019178304A1 (en) * | 2018-03-14 | 2019-09-19 | Teva Pharmaceuticals International Gmbh | Solid state forms of relugolix |
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| CN114174302A (zh) * | 2019-08-02 | 2022-03-11 | 庄信万丰股份有限公司 | 瑞卢戈利的固态形式 |
| CN112390812A (zh) * | 2019-08-14 | 2021-02-23 | 苏州鹏旭医药科技有限公司 | 瑞卢戈利化合物的晶型和无定型固体及其制备方法 |
| 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 |
| 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 |
| CN111423452B (zh) * | 2020-03-26 | 2023-08-22 | 江西青峰药业有限公司 | 瑞卢戈利的中间体及其制备方法和应用 |
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| CA3185151A1 (en) | 2020-05-29 | 2021-12-02 | Myovant Sciences Gmbh | Combination solid oral dosage forms of gonadotropin-releasing hormone antagonists |
| US11655256B1 (en) | 2020-11-06 | 2023-05-23 | Macfarlan Smith Limited | Processes for making a solid-state form of relugolix |
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| 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 |
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| JP2024540922A (ja) | 2021-10-18 | 2024-11-06 | スミトモ ファーマ スウィッツァーランド 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’-メトキシ尿素のエタノール溶媒和物の結晶形 |
| WO2023119333A1 (en) | 2021-12-25 | 2023-06-29 | Dr. Reddy’S Laboratories Limited | Process for preparation of relugolix and its intermediates |
| IN202221021078A (https=) | 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 JP JP2022521569A patent/JP2022551316A/ja active Pending
- 2020-10-09 EP EP20790256.0A patent/EP4041739A1/en active Pending
- 2020-10-09 CN CN202080084633.9A patent/CN115279769A/zh active Pending
- 2020-10-09 WO PCT/EP2020/078493 patent/WO2021069711A1/en not_active Ceased
-
2022
- 2022-04-08 US US17/716,963 patent/US12338249B2/en active Active
-
2025
- 2025-05-19 US US19/212,513 patent/US20260042775A1/en active Pending
Patent Citations (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20060160829A1 (en) * | 2003-01-29 | 2006-07-20 | Nobuo Cho | Thienopyrimidine compounds and use thereof |
| US20150266891A1 (en) * | 2012-09-28 | 2015-09-24 | Takeda Pharmaceutical Company Limited | Production method of thienopyrimidine derivative |
| CA3010509A1 (en) * | 2016-01-11 | 2017-07-20 | Janssen Pharmaceutica Nv | Substituted thiohydantoin derivatives as androgen receptor antagonists |
| US20190224196A1 (en) * | 2016-09-30 | 2019-07-25 | Myovant Sciences Gmbh | Treatment of prostate cancer |
| US20190262346A1 (en) * | 2016-09-30 | 2019-08-29 | Myovant Sciences Gmbh | Methods of treating uterine fibroids and endometriosis |
| WO2019178304A1 (en) * | 2018-03-14 | 2019-09-19 | Teva Pharmaceuticals International Gmbh | Solid state forms of relugolix |
Non-Patent Citations (1)
| Title |
|---|
| 丁志新;门靖;曹卫凯;贾庆仪;: "公斤级SKI2496关键中间体的合成工艺改进", 中国药学杂志, no. 20, 22 October 2018 (2018-10-22), pages 15 - 18 * |
Cited By (1)
| 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 |
|---|---|
| JP2022551316A (ja) | 2022-12-08 |
| EP4041739A1 (en) | 2022-08-17 |
| WO2021069711A1 (en) | 2021-04-15 |
| US20260042775A1 (en) | 2026-02-12 |
| US20220396582A1 (en) | 2022-12-15 |
| US12338249B2 (en) | 2025-06-24 |
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Country or region after: Switzerland Address after: Basel, SUI Applicant after: Sumitomo Pharmaceutical Switzerland Ltd. Country or region after: Japan Applicant after: TAKEDA PHARMACEUTICAL Co.,Ltd. Address before: Basel, SUI Applicant before: MYOVANT SCIENCES GmbH Country or region before: Switzerland Applicant before: TAKEDA PHARMACEUTICAL Co.,Ltd. Country or region before: Japan |
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