JPWO2021069711A5 - - Google Patents
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- JPWO2021069711A5 JPWO2021069711A5 JP2022521569A JP2022521569A JPWO2021069711A5 JP WO2021069711 A5 JPWO2021069711 A5 JP WO2021069711A5 JP 2022521569 A JP2022521569 A JP 2022521569A JP 2022521569 A JP2022521569 A JP 2022521569A JP WO2021069711 A5 JPWO2021069711 A5 JP WO2021069711A5
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- Prior art keywords
- crystalline form
- theta
- powder
- ray diffraction
- peaks
- Prior art date
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- 238000000634 powder X-ray diffraction Methods 0.000 claims 6
- KFZMGEQAYNKOFK-UHFFFAOYSA-N Isopropanol Chemical compound CC(C)O KFZMGEQAYNKOFK-UHFFFAOYSA-N 0.000 claims 3
- ZMXDDKWLCZADIW-UHFFFAOYSA-N N,N-Dimethylformamide Chemical compound CN(C)C=O ZMXDDKWLCZADIW-UHFFFAOYSA-N 0.000 claims 3
- 239000013078 crystal Substances 0.000 claims 3
- 238000001938 differential scanning calorimetry curve Methods 0.000 claims 3
- 239000012453 solvate Substances 0.000 claims 3
- 238000001757 thermogravimetry curve Methods 0.000 claims 3
- AOMXMOCNKJTRQP-UHFFFAOYSA-N 1-[4-[1-[(2,6-difluorophenyl)methyl]-5-[(dimethylamino)methyl]-3-(6-methoxypyridazin-3-yl)-2,4-dioxothieno[2,3-d]pyrimidin-6-yl]phenyl]-3-methoxyurea Chemical compound C1=CC(NC(=O)NOC)=CC=C1C1=C(CN(C)C)C(C(=O)N(C=2N=NC(OC)=CC=2)C(=O)N2CC=3C(=CC=CC=3F)F)=C2S1 AOMXMOCNKJTRQP-UHFFFAOYSA-N 0.000 claims 2
- CSCPPACGZOOCGX-UHFFFAOYSA-N Acetone Chemical compound CC(C)=O CSCPPACGZOOCGX-UHFFFAOYSA-N 0.000 claims 2
- -1 2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl Chemical group 0.000 claims 1
- 238000000113 differential scanning calorimetry Methods 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201962913560P | 2019-10-10 | 2019-10-10 | |
| US62/913,560 | 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 (3)
| Publication Number | Publication Date |
|---|---|
| JP2022551316A JP2022551316A (ja) | 2022-12-08 |
| JP2022551316A5 JP2022551316A5 (https=) | 2023-10-17 |
| JPWO2021069711A5 true JPWO2021069711A5 (https=) | 2023-10-17 |
Family
ID=72852650
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2022521569A Pending JP2022551316A (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形 |
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=) |
Families Citing this family (8)
| 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 |
| 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 |
| 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 |
Family Cites Families (52)
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| JPS5116436B1 (https=) | 1971-05-31 | 1976-05-24 | ||
| EP0237289A3 (en) | 1986-03-14 | 1988-07-27 | Takeda Chemical Industries, Ltd. | Pyrazolo [3,4-d] pyrimidine derivatives, their production and use |
| JP2859791B2 (ja) | 1992-01-31 | 1999-02-24 | 吉富製薬株式会社 | ４−ブロモメチルビフェニル化合物の製造法 |
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| JPH10298156A (ja) | 1997-04-28 | 1998-11-10 | Nippon Nohyaku Co Ltd | 置換ハロメチルフェニルカルバミド酸エステル類の製造方法 |
| US6297379B1 (en) | 1999-03-24 | 2001-10-02 | Takeda Chemical Industries, Ltd. | Thienopyrimidine compounds, their production and use |
| TWI225863B (en) | 1999-03-24 | 2005-01-01 | Takeda Chemical Industries Ltd | Thienopyrimidine compounds, their production and use |
| JP2001316391A (ja) | 2000-02-29 | 2001-11-13 | Takeda Chem Ind Ltd | チエノピリミジン誘導体の製造法 |
| US6849738B2 (en) | 2000-02-29 | 2005-02-01 | Takeda Chemical Industries, Ltd. | Processes for the production of thienopyrimidine derivatives |
| GB2361917A (en) | 2000-05-04 | 2001-11-07 | Astrazeneca Ab | Novel thieno[2,3-d]pyrimidinediones |
| JP2002088044A (ja) | 2000-09-14 | 2002-03-27 | Sumitomo Seika Chem Co Ltd | ４’−ブロモメチル−２−シアノビフェニルの製造方法 |
| HUP0401443A3 (en) | 2001-09-04 | 2008-05-28 | Organon Nv | Glycine-substituted thieno[2,3-d]pyrimidines with lh and fsh agonistic activity, use of the compounds and pharmaceutical compositions containing same |
| WO2003064429A1 (en) | 2002-01-30 | 2003-08-07 | Takeda Chemical Industries, Ltd. | Thienopyrimidines, process for preparing the same and use thereof |
| ES2217956B1 (es) | 2003-01-23 | 2006-04-01 | Almirall Prodesfarma, S.A. | Nuevos derivados de 4-aminotieno(2,3-d)pirimidin-6-carbonitrilo. |
| US7300935B2 (en) | 2003-01-29 | 2007-11-27 | Takeda Pharmaceutical Company | Thienopyrimidine compounds and use thereof |
| WO2006014647A2 (en) | 2004-07-21 | 2006-02-09 | Athersys, Inc. | Cyclic n-hydroxy imides as inhibitors of flap endonuclease and uses thereof |
| WO2006046485A1 (ja) | 2004-10-25 | 2006-05-04 | Nihon Nohyaku Co., Ltd. | 畑作用除草剤組成物及び防除方法 |
| ES2494842T3 (es) | 2005-07-22 | 2014-09-16 | Takeda Pharmaceutical Company Limited | Agente que previene la ovulación precoz |
| 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 |
| JP2010229098A (ja) * | 2009-03-27 | 2010-10-14 | Central Glass Co Ltd | イソインドリン誘導体のａ型の結晶形の製造方法及びイソインドリン誘導体のａ型の結晶形 |
| TWI508962B (zh) | 2009-04-22 | 2015-11-21 | Du Pont | 氮雜環醯胺之固體形態 |
| AR092707A1 (es) | 2012-09-28 | 2015-04-29 | Takeda Pharmaceuticals Co | Metodo de produccion de derivado de tienopirimidina |
| NZ719185A (en) * | 2013-11-01 | 2017-11-24 | Kala Pharmaceuticals Inc | Crystalline forms of therapeutic compounds and uses thereof |
| 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 |
| JP2017088564A (ja) * | 2015-11-13 | 2017-05-25 | 株式会社トクヤマ | ミルタザピンの製造方法 |
| US10689359B2 (en) | 2015-12-25 | 2020-06-23 | Xuanzhu Pharma Co., Ltd. | Crystals of quinazoline derivative and preparation method therefor |
| TWI726969B (zh) * | 2016-01-11 | 2021-05-11 | 比利時商健生藥品公司 | 用作雄性激素受體拮抗劑之經取代之硫尿囊素衍生物 |
| US20170275330A1 (en) | 2016-03-28 | 2017-09-28 | Warsaw Orthopedic, Inc. | Polymorphic forms of an oxysterol and methods of making them |
| MA46361A (fr) | 2016-09-30 | 2021-03-31 | Myovant Sciences Gmbh | Traitement du cancer de la prostate |
| ES2912929T5 (en) | 2016-09-30 | 2025-05-09 | Sumitomo Pharma Switzerland Gmbh | Methods of treating uterine fibroids and endometriosis |
| US11306104B2 (en) * | 2018-03-14 | 2022-04-19 | Teva Pharmaceuticals International Gmbh | Solid state forms of Relugolix |
| US12441738B2 (en) | 2018-03-14 | 2025-10-14 | Assia Chemical Industries Ltd. | Solid state forms of Relugolix |
| EP3666776A1 (en) * | 2018-12-11 | 2020-06-17 | Sandoz AG | Hydrate of a gonadotropin-releasing hormone receptor antagonist |
| US20220220123A1 (en) * | 2019-05-15 | 2022-07-14 | Dr. Reddy's Laboratories Limited | Amorphous and crystalline forms of relugolix |
| 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 |
| CN111333633B (zh) * | 2020-04-01 | 2023-10-20 | 江西科睿药业有限公司 | 一种瑞卢戈利的中间体化合物及其制备方法和用途 |
| 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 |
| WO2022101303A1 (en) | 2020-11-11 | 2022-05-19 | Myovant Sciences Gmbh | Methods of administering relugolix |
| CN112552312B (zh) | 2020-12-07 | 2022-08-05 | 杭州科巢生物科技有限公司 | 一种瑞卢戈利或其盐的合成方法 |
| 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 |
| US20240287090A1 (en) | 2021-09-15 | 2024-08-29 | Cipla Limited | Solid state forms of relugolix |
| 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 |
| 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
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