JP2019501865A5 - - Google Patents
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- JP2019501865A5 JP2019501865A5 JP2018517576A JP2018517576A JP2019501865A5 JP 2019501865 A5 JP2019501865 A5 JP 2019501865A5 JP 2018517576 A JP2018517576 A JP 2018517576A JP 2018517576 A JP2018517576 A JP 2018517576A JP 2019501865 A5 JP2019501865 A5 JP 2019501865A5
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- JP
- Japan
- Prior art keywords
- crystalline hemihydrate
- crystalline
- diffraction pattern
- ray powder
- powder diffraction
- 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.)
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- 0 CCC(CN(*)C1)C1C(O)=O Chemical compound CCC(CN(*)C1)C1C(O)=O 0.000 description 15
- JQCFYUAAZPLOAT-ZJUUUORDSA-N CC[C@H](CNC1)[C@H]1c1cnc2[n]1c(cc[nH]1)c1nc2 Chemical compound CC[C@H](CNC1)[C@H]1c1cnc2[n]1c(cc[nH]1)c1nc2 JQCFYUAAZPLOAT-ZJUUUORDSA-N 0.000 description 2
- SVEHWKCSSNSKAG-UHFFFAOYSA-N CCC(CNC1)C1C(OCC)=O Chemical compound CCC(CNC1)C1C(OCC)=O SVEHWKCSSNSKAG-UHFFFAOYSA-N 0.000 description 1
- JQCFYUAAZPLOAT-UHFFFAOYSA-N CCC(CNC1)C1c1cnc2[n]1c(cc[nH]1)c1nc2 Chemical compound CCC(CNC1)C1c1cnc2[n]1c(cc[nH]1)c1nc2 JQCFYUAAZPLOAT-UHFFFAOYSA-N 0.000 description 1
- JKEVTOBMCFQXFF-YPMHNXCESA-N CC[C@H](CN(C1)OC(c2ccccc2)=O)[C@H]1C(CBr)=O Chemical compound CC[C@H](CN(C1)OC(c2ccccc2)=O)[C@H]1C(CBr)=O JKEVTOBMCFQXFF-YPMHNXCESA-N 0.000 description 1
- KAFJDPPXJADBSX-ZBFHGGJFSA-N CC[C@H](CN(C1)OC(c2ccccc2)=O)[C@H]1c1cnc2[n]1c(cc[nH]1)c1nc2 Chemical compound CC[C@H](CN(C1)OC(c2ccccc2)=O)[C@H]1c1cnc2[n]1c(cc[nH]1)c1nc2 KAFJDPPXJADBSX-ZBFHGGJFSA-N 0.000 description 1
- JQCFYUAAZPLOAT-YHMJZVADSA-N CC[C@H](CNC1)C1c1cnc2[n]1c(cc[nH]1)c1nc2 Chemical compound CC[C@H](CNC1)C1c1cnc2[n]1c(cc[nH]1)c1nc2 JQCFYUAAZPLOAT-YHMJZVADSA-N 0.000 description 1
- RTCUCQWIICFPOD-SECBINFHSA-N C[C@H](c1cccc2ccccc12)N Chemical compound C[C@H](c1cccc2ccccc12)N RTCUCQWIICFPOD-SECBINFHSA-N 0.000 description 1
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Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2020159855A JP7358317B2 (ja) | 2015-10-16 | 2020-09-24 | (3S,4R)-3-エチル-4-(3H-イミダゾ[1,2-a]ピロロ[2,3-e]-ピラジン-8-イル)-N-(2,2,2-トリフルオロエチル)ピロリジン-1-カルボキサミドおよびそれの固体型の製造方法 |
Applications Claiming Priority (9)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562242797P | 2015-10-16 | 2015-10-16 | |
| US62/242,797 | 2015-10-16 | ||
| US201562267672P | 2015-12-15 | 2015-12-15 | |
| US62/267,672 | 2015-12-15 | ||
| US201662301537P | 2016-02-29 | 2016-02-29 | |
| US62/301,537 | 2016-02-29 | ||
| US201662352380P | 2016-06-20 | 2016-06-20 | |
| US62/352,380 | 2016-06-20 | ||
| PCT/US2016/057372 WO2017066775A1 (en) | 2015-10-16 | 2016-10-17 | PROCESSES FOR THE PREPARATION OF (3S,4R)-3-ETHYL-4-(3H-IMIDAZO[1,2-a]PYRROLO[2,3-e]-PYRAZIN-8-YL)-N-(2,2,2-TRIFLUOROETHYL)PYRROLIDINE-1-CARBOXAMIDE AND SOLID STATE FORMS THEREOF |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020159855A Division JP7358317B2 (ja) | 2015-10-16 | 2020-09-24 | (3S,4R)-3-エチル-4-(3H-イミダゾ[1,2-a]ピロロ[2,3-e]-ピラジン-8-イル)-N-(2,2,2-トリフルオロエチル)ピロリジン-1-カルボキサミドおよびそれの固体型の製造方法 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2019501865A JP2019501865A (ja) | 2019-01-24 |
| JP2019501865A5 true JP2019501865A5 (enExample) | 2019-12-05 |
| JP6770775B2 JP6770775B2 (ja) | 2020-10-21 |
Family
ID=57209916
Family Applications (8)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018517576A Active JP6770775B2 (ja) | 2015-10-16 | 2016-10-17 | (3S,4R)−3−エチル−4−(3H−イミダゾ[1,2−a]ピロロ[2,3−e]−ピラジン−8−イル)−N−(2,2,2−トリフルオロエチル)ピロリジン−1−カルボキサミドおよびそれの固体型の製造方法 |
| JP2020159855A Active JP7358317B2 (ja) | 2015-10-16 | 2020-09-24 | (3S,4R)-3-エチル-4-(3H-イミダゾ[1,2-a]ピロロ[2,3-e]-ピラジン-8-イル)-N-(2,2,2-トリフルオロエチル)ピロリジン-1-カルボキサミドおよびそれの固体型の製造方法 |
| JP2022079226A Pending JP2022107001A (ja) | 2015-10-16 | 2022-05-13 | (3S,4R)-3-エチル-4-(3H-イミダゾ[1,2-a]ピロロ[2,3-e]-ピラジン-8-イル)-N-(2,2,2-トリフルオロエチル)ピロリジン-1-カルボキサミドおよびそれの固体型の製造方法 |
| JP2023096042A Pending JP2023113917A (ja) | 2015-10-16 | 2023-06-12 | (3S,4R)-3-エチル-4-(3H-イミダゾ[1,2-a]ピロロ[2,3-e]-ピラジン-8-イル)-N-(2,2,2-トリフルオロエチル)ピロリジン-1-カルボキサミドおよびそれの固体型の製造方法 |
| JP2024041977A Pending JP2024073591A (ja) | 2015-10-16 | 2024-03-18 | (3S,4R)-3-エチル-4-(3H-イミダゾ[1,2-a]ピロロ[2,3-e]-ピラジン-8-イル)-N-(2,2,2-トリフルオロエチル)ピロリジン-1-カルボキサミドおよびそれの固体型の製造方法 |
| JP2025133177A Pending JP2025166113A (ja) | 2015-10-16 | 2025-08-08 | (3S,4R)-3-エチル-4-(3H-イミダゾ[1,2-a]ピロロ[2,3-e]-ピラジン-8-イル)-N-(2,2,2-トリフルオロエチル)ピロリジン-1-カルボキサミドおよびそれの固体型の製造方法 |
| JP2025133176A Pending JP2025166112A (ja) | 2015-10-16 | 2025-08-08 | (3S,4R)-3-エチル-4-(3H-イミダゾ[1,2-a]ピロロ[2,3-e]-ピラジン-8-イル)-N-(2,2,2-トリフルオロエチル)ピロリジン-1-カルボキサミドおよびそれの固体型の製造方法 |
| JP2025165233A Pending JP2026004431A (ja) | 2015-10-16 | 2025-10-01 | (3S,4R)-3-エチル-4-(3H-イミダゾ[1,2-a]ピロロ[2,3-e]-ピラジン-8-イル)-N-(2,2,2-トリフルオロエチル)ピロリジン-1-カルボキサミドおよびそれの固体型の製造方法 |
Family Applications After (7)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020159855A Active JP7358317B2 (ja) | 2015-10-16 | 2020-09-24 | (3S,4R)-3-エチル-4-(3H-イミダゾ[1,2-a]ピロロ[2,3-e]-ピラジン-8-イル)-N-(2,2,2-トリフルオロエチル)ピロリジン-1-カルボキサミドおよびそれの固体型の製造方法 |
| JP2022079226A Pending JP2022107001A (ja) | 2015-10-16 | 2022-05-13 | (3S,4R)-3-エチル-4-(3H-イミダゾ[1,2-a]ピロロ[2,3-e]-ピラジン-8-イル)-N-(2,2,2-トリフルオロエチル)ピロリジン-1-カルボキサミドおよびそれの固体型の製造方法 |
| JP2023096042A Pending JP2023113917A (ja) | 2015-10-16 | 2023-06-12 | (3S,4R)-3-エチル-4-(3H-イミダゾ[1,2-a]ピロロ[2,3-e]-ピラジン-8-イル)-N-(2,2,2-トリフルオロエチル)ピロリジン-1-カルボキサミドおよびそれの固体型の製造方法 |
| JP2024041977A Pending JP2024073591A (ja) | 2015-10-16 | 2024-03-18 | (3S,4R)-3-エチル-4-(3H-イミダゾ[1,2-a]ピロロ[2,3-e]-ピラジン-8-イル)-N-(2,2,2-トリフルオロエチル)ピロリジン-1-カルボキサミドおよびそれの固体型の製造方法 |
| JP2025133177A Pending JP2025166113A (ja) | 2015-10-16 | 2025-08-08 | (3S,4R)-3-エチル-4-(3H-イミダゾ[1,2-a]ピロロ[2,3-e]-ピラジン-8-イル)-N-(2,2,2-トリフルオロエチル)ピロリジン-1-カルボキサミドおよびそれの固体型の製造方法 |
| JP2025133176A Pending JP2025166112A (ja) | 2015-10-16 | 2025-08-08 | (3S,4R)-3-エチル-4-(3H-イミダゾ[1,2-a]ピロロ[2,3-e]-ピラジン-8-イル)-N-(2,2,2-トリフルオロエチル)ピロリジン-1-カルボキサミドおよびそれの固体型の製造方法 |
| JP2025165233A Pending JP2026004431A (ja) | 2015-10-16 | 2025-10-01 | (3S,4R)-3-エチル-4-(3H-イミダゾ[1,2-a]ピロロ[2,3-e]-ピラジン-8-イル)-N-(2,2,2-トリフルオロエチル)ピロリジン-1-カルボキサミドおよびそれの固体型の製造方法 |
Country Status (13)
| Country | Link |
|---|---|
| US (39) | US20170129902A1 (enExample) |
| EP (5) | EP4706768A2 (enExample) |
| JP (8) | JP6770775B2 (enExample) |
| KR (2) | KR102753815B1 (enExample) |
| CN (8) | CN120289468A (enExample) |
| AU (5) | AU2016340167B2 (enExample) |
| BR (1) | BR122022024925B1 (enExample) |
| CA (9) | CA3251507C (enExample) |
| IL (3) | IL314468A (enExample) |
| MX (2) | MX387822B (enExample) |
| RU (1) | RU2018117889A (enExample) |
| SG (8) | SG10201913990RA (enExample) |
| WO (1) | WO2017066775A1 (enExample) |
Families Citing this family (59)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE2836833A1 (de) | 1978-08-23 | 1980-04-10 | Volkswagenwerk Ag | Brennkraftmaschine mit in zwei reihen angeordneten zylindern |
| RU2711869C3 (ru) | 2009-12-01 | 2022-02-02 | Эббви Инк. | Имидазопирролопиразиновые производные, полезные для лечения заболеваний, вызванных аномальной активностью протеинкиназ Jak1, Jak3 или Syk |
| US12365689B2 (en) | 2015-10-16 | 2025-07-22 | Abbvie Inc. | Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]-pyrazin-8-yl)-n-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof |
| US11524964B2 (en) | 2015-10-16 | 2022-12-13 | Abbvie Inc. | Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]-pyrazin-8-yl)-n-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof |
| SG10201913990RA (en) * | 2015-10-16 | 2020-03-30 | Abbvie Inc | PROCESSES FOR THE PREPARATION OF (3S,4R)-3-ETHYL-4-(3H-IMIDAZO[1,2-a]PYRROLO[2,3-e]-PYRAZIN-8-YL)-N-(2,2,2-TRIFLUOROETHYL)PYRROLIDINE-1-CARBOXAMIDE AND SOLID STATE FORMS THEREOF |
| US12570664B2 (en) | 2015-10-16 | 2026-03-10 | Abbvie Inc. | Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-α]pyrrolo[2,3-e]-pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof |
| US11512092B2 (en) * | 2015-10-16 | 2022-11-29 | Abbvie Inc. | Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]-pyrazin-8-yl)-n-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof |
| US20210228575A1 (en) * | 2019-09-30 | 2021-07-29 | Abbvie Inc. | Treating spondyloarthritic and psoriatic conditions with upadacitinib |
| US11365198B2 (en) | 2015-10-16 | 2022-06-21 | Abbvie Inc. | Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]-pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof |
| US20240316042A1 (en) | 2023-03-22 | 2024-09-26 | Abbvie Inc. | Methods of treating pediatric patients with upadacitinib |
| US10550126B2 (en) | 2015-10-16 | 2020-02-04 | Abbvie Inc. | Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-A]pyrrolo[2,3-e]-pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof |
| US11773106B2 (en) | 2015-10-16 | 2023-10-03 | Abbvie Inc. | Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]-pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof |
| AU2018230500B2 (en) | 2017-03-09 | 2024-03-07 | Abbvie Inc. | Methods of treating Crohn's disease and ulcerative colitis |
| US11564922B2 (en) | 2017-03-09 | 2023-01-31 | Abbvie Inc. | Methods of treating crohn's disease and ulcerative colitis |
| WO2019016745A1 (en) * | 2017-07-19 | 2019-01-24 | Dr. Reddy's Laboratories Limited | ALTERNATIVE METHODS FOR THE PREPARATION OF PYRROLIDINE DERIVATIVES |
| SMT202400306T1 (it) | 2018-03-30 | 2024-09-16 | Incyte Corp | Trattamento dell'idrosadenite suppurativa utilizzando inibitori di jak. |
| CN110872250B (zh) * | 2018-08-31 | 2023-01-10 | 苏州鹏旭医药科技有限公司 | 两种化合物及其制备方法和在合成乌西替尼中的用途 |
| US11926633B2 (en) | 2018-08-31 | 2024-03-12 | Suzhou Pengxu Pharmatech Co., Ltd | Synthesis methods for upadacitinib and intermediate thereof |
| CN112770756A (zh) * | 2018-09-29 | 2021-05-07 | 苏州科睿思制药有限公司 | 一种Upadacitinib的晶型及其制备方法和用途 |
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| WO2020115212A1 (en) | 2018-12-05 | 2020-06-11 | Lek Pharmaceuticals D.D. | Crystalline phosphate salt of selective jak1 inhibitor upadacitinib |
| CN109369659B (zh) * | 2018-12-06 | 2020-10-27 | 浙江师范大学 | 一种jak抑制剂的合成方法 |
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| CN109705011B (zh) * | 2019-01-18 | 2021-02-19 | 浙江师范大学 | 一种乌帕替尼中间体的合成方法及中间体 |
| US20210380596A1 (en) * | 2019-03-01 | 2021-12-09 | Crystal Pharmaceutical (Suzhou) Co., Ltd. | Upadacitinib crystal form and preparation method therefor and use thereof |
| WO2020202183A1 (en) | 2019-03-29 | 2020-10-08 | Mylan Laboratories Limited | The process for the preparation of upadacitinib and its intermediates |
| CN111909160B (zh) * | 2019-05-09 | 2024-05-28 | 苏州鹏旭医药科技有限公司 | 一种乌帕替尼盐类化合物及其制备方法 |
| CN110229160A (zh) * | 2019-06-11 | 2019-09-13 | 南京新酶合医药科技有限公司 | (5-甲苯磺酰基-5H-吡咯并[2,3-b]吡嗪-2-基)氨基甲酸乙酯的制备方法 |
| CN110117245B (zh) * | 2019-06-21 | 2021-03-02 | 浙江师范大学 | 一种jak抑制剂中间体的合成方法 |
| WO2021005484A1 (en) * | 2019-07-11 | 2021-01-14 | Mankind Pharma Ltd. | Pyrrolidine compounds, its salt and use in the preparation of upadacitinib thereof |
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| EP4077276A1 (en) * | 2019-12-19 | 2022-10-26 | Curia Spain S.A.U. | Process and intermediates for the preparation of upadacitinib |
| WO2021176473A1 (en) * | 2020-03-05 | 2021-09-10 | Mylan Laboratories Limited | A process for the preparation of upadacitinib and its intermediates |
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| EP4460503A4 (en) * | 2022-01-06 | 2025-12-03 | Msn Laboratories Private Ltd R&D Center | IMPROVED PROCESS FOR THE PREPARATION OF UPADACITINIB |
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| CN117285535B (zh) * | 2023-11-27 | 2024-02-02 | 中节能万润股份有限公司 | 一种乌帕替尼中间体及成盐中间体的制备方法 |
| CN117285536B (zh) * | 2023-11-27 | 2024-02-20 | 中节能万润股份有限公司 | 一种乌帕替尼中间体的制备方法 |
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| US11773106B2 (en) | 2015-10-16 | 2023-10-03 | Abbvie Inc. | Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]-pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof |
| US10550126B2 (en) | 2015-10-16 | 2020-02-04 | Abbvie Inc. | Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-A]pyrrolo[2,3-e]-pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof |
| US11512092B2 (en) | 2015-10-16 | 2022-11-29 | Abbvie Inc. | Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]-pyrazin-8-yl)-n-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof |
| SG10201913990RA (en) * | 2015-10-16 | 2020-03-30 | Abbvie Inc | PROCESSES FOR THE PREPARATION OF (3S,4R)-3-ETHYL-4-(3H-IMIDAZO[1,2-a]PYRROLO[2,3-e]-PYRAZIN-8-YL)-N-(2,2,2-TRIFLUOROETHYL)PYRROLIDINE-1-CARBOXAMIDE AND SOLID STATE FORMS THEREOF |
| SG10202112628UA (en) | 2015-11-30 | 2021-12-30 | Anacor Pharmaceuticals Inc | Topical pharmaceutical formulations for treating inflammatory-related conditions |
| WO2017126488A1 (ja) | 2016-01-18 | 2017-07-27 | 持田製薬株式会社 | 乾癬治療用組成物および治療方法 |
| US10973913B2 (en) | 2016-02-16 | 2021-04-13 | Washington University | JAK inhibitors and uses thereof |
| SG11201811760VA (en) | 2016-07-06 | 2019-01-30 | Durect Corp | Oral dosage form with drug composition, barrier layer and drug layer |
| AU2018230500B2 (en) | 2017-03-09 | 2024-03-07 | Abbvie Inc. | Methods of treating Crohn's disease and ulcerative colitis |
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| KR20240148324A (ko) | 2022-01-13 | 2024-10-11 | 애브비 인코포레이티드 | 유해 약물 상호작용 및 효과를 피하기 위한 우파다시티닙의 투여 방법 |
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