ES2966512T3 - Formas cristalinas de (S)-1-(4-fluorofenil)-1-(2-(4-(6-(1-metil-1H-pirazol-4-il)pirrolo[2,1-f][1,2,4]triazin-4-il)piperazinil)-pirimidin-5-il)etan-1-amina y métodos de elaboración - Google Patents
Formas cristalinas de (S)-1-(4-fluorofenil)-1-(2-(4-(6-(1-metil-1H-pirazol-4-il)pirrolo[2,1-f][1,2,4]triazin-4-il)piperazinil)-pirimidin-5-il)etan-1-amina y métodos de elaboración Download PDFInfo
- Publication number
- ES2966512T3 ES2966512T3 ES20722936T ES20722936T ES2966512T3 ES 2966512 T3 ES2966512 T3 ES 2966512T3 ES 20722936 T ES20722936 T ES 20722936T ES 20722936 T ES20722936 T ES 20722936T ES 2966512 T3 ES2966512 T3 ES 2966512T3
- Authority
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- Prior art keywords
- compound
- crystalline
- crystalline form
- patients
- ray powder
- 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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Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- 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
- A61K31/13—Amines
- A61K31/155—Amidines (), e.g. guanidine (H2N—C(=NH)—NH2), isourea (N=C(OH)—NH2), isothiourea (—N=C(SH)—NH2)
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- 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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- 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
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Dermatology (AREA)
- Oncology (AREA)
- Hematology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201962833527P | 2019-04-12 | 2019-04-12 | |
| US201962844575P | 2019-05-07 | 2019-05-07 | |
| US202062990269P | 2020-03-16 | 2020-03-16 | |
| PCT/US2020/027724 WO2020210669A1 (en) | 2019-04-12 | 2020-04-10 | Crystalline forms of (s)-1-(4-fluorophenyl)-1-(2-(4-(6-(1-methyl-1h-pyrazol-4-yl)pyrrolo[2,1-f][1,2,4]triazin-4-yl)piperazinyl)-pyrimidin-5-yl)ethan-1-amine and methods of making |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ES2966512T3 true ES2966512T3 (es) | 2024-04-22 |
Family
ID=70476546
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES20722936T Active ES2966512T3 (es) | 2019-04-12 | 2020-04-10 | Formas cristalinas de (S)-1-(4-fluorofenil)-1-(2-(4-(6-(1-metil-1H-pirazol-4-il)pirrolo[2,1-f][1,2,4]triazin-4-il)piperazinil)-pirimidin-5-il)etan-1-amina y métodos de elaboración |
Country Status (20)
| Country | Link |
|---|---|
| US (5) | US12060354B2 (enExample) |
| EP (2) | EP4302761A3 (enExample) |
| JP (1) | JP7728178B2 (enExample) |
| CN (1) | CN113966334B (enExample) |
| CA (2) | CA3296895A1 (enExample) |
| DK (1) | DK3856341T3 (enExample) |
| ES (1) | ES2966512T3 (enExample) |
| FI (1) | FI3856341T3 (enExample) |
| HR (1) | HRP20231533T1 (enExample) |
| HU (1) | HUE064283T2 (enExample) |
| IL (2) | IL287148A (enExample) |
| LT (1) | LT3856341T (enExample) |
| MA (1) | MA53759A (enExample) |
| PL (1) | PL3856341T3 (enExample) |
| PT (1) | PT3856341T (enExample) |
| RS (1) | RS64881B1 (enExample) |
| SI (1) | SI3856341T1 (enExample) |
| SM (1) | SMT202300447T1 (enExample) |
| TW (1) | TWI845657B (enExample) |
| WO (1) | WO2020210669A1 (enExample) |
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MX365614B (es) | 2013-10-17 | 2019-06-07 | Blueprint Medicines Corp | Composiciones utiles para tratar trastornos relacionados con kit. |
| HUE064283T2 (hu) | 2019-04-12 | 2024-02-28 | Blueprint Medicines Corp | Az (S)-1-(4-fluorofenil)-1-(2-(4-(6-(1-metil-1H-pirazol-4-il)pirrolo[2,1-f][1,2,4]triazin-4-il) piperazinil)-pirimidin-5-il)etán-1-amin kristályos formái és elõállítási eljárásai |
| US12590095B2 (en) * | 2019-07-09 | 2026-03-31 | Sandoz Ag | Crystalline forms of an orally available, selective kit and PDGFR kinase inhibitor |
| GB201915447D0 (en) * | 2019-10-24 | 2019-12-11 | Johnson Matthey Plc | Polymorphs of avapritinib and methods of preparing the polymorphs |
| WO2021183709A1 (en) | 2020-03-11 | 2021-09-16 | Teva Czech Industries S.R.O | Solid state forms of avapritinib and process for preparation thereof |
| US20230279009A1 (en) | 2020-06-17 | 2023-09-07 | Teva Czech Industries S.R.O | Solid state forms of avapritinib salts |
| HU231413B1 (hu) * | 2021-02-26 | 2023-08-28 | Egis Gyógyszergyár Zrt. | Eljárás avapritinib és intermedierek előállítására |
| JP7763848B2 (ja) | 2021-03-03 | 2025-11-04 | ブループリント メディシンズ コーポレイション | Ｋｉｔ－およびｐｄｇｆｒａ－媒介性疾患を治療するための化合物を製造するための合成方法および中間生成物 |
| HU231755B1 (hu) * | 2022-08-11 | 2026-02-28 | Egis Gyógyszergyár Zrt. | Új avapritinib sók és előállítási eljárásaik |
| US20240382493A1 (en) * | 2023-05-18 | 2024-11-21 | Blueprint Medicines Corporation | Methods for treating systemic mastocytosis and gastrointestinal stromal tumors |
| WO2025170989A1 (en) | 2024-02-05 | 2025-08-14 | Blueprint Medicines Corporation | High-risk disease features of indolent systemic mastocytosis and methods for treating |
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| JPS61238784A (ja) | 1985-04-17 | 1986-10-24 | Sumitomo Seiyaku Kk | コハク酸イミド誘導体及びその酸付加塩 |
| US6982265B1 (en) | 1999-05-21 | 2006-01-03 | Bristol Myers Squibb Company | Pyrrolotriazine inhibitors of kinases |
| IL144977A0 (en) | 1999-05-21 | 2002-06-30 | Bristol Myers Squibb Co | Pyrrolotriazine derivatives and pharmaceutical compositions containing the same |
| MXPA02003436A (es) | 1999-10-07 | 2002-08-20 | Amgen Inc | Inhibidores de triazina cinasa. |
| IL150524A0 (en) | 2000-01-07 | 2003-02-12 | Transform Pharmaceuticals Inc | High-throughput formation, identification, and analysis of diverse solid-forms |
| WO2001074821A1 (en) | 2000-03-30 | 2001-10-11 | Shionogi & Co., Ltd. | Novel process for producing fused imidazopyridine derivative and novel crystal form |
| SE0102616D0 (sv) | 2001-07-25 | 2001-07-25 | Astrazeneca Ab | Novel compounds |
| PL219736B1 (pl) | 2002-04-23 | 2015-07-31 | Bristol Myers Squibb Co | Pochodna pirolotriazynoaniliny, kompozycja farmaceutyczna i jej zastosowanie |
| TW200508224A (en) | 2003-02-12 | 2005-03-01 | Bristol Myers Squibb Co | Cyclic derivatives as modulators of chemokine receptor activity |
| UA81453C2 (en) | 2003-02-27 | 2008-01-10 | Pyrazolopyridine derivates | |
| WO2005117909A2 (en) | 2004-04-23 | 2005-12-15 | Exelixis, Inc. | Kinase modulators and methods of use |
| EP1755607A2 (en) | 2004-04-29 | 2007-02-28 | Pharmix Corporation | Compositions and treatments for inhibiting kinase and/or hmg-coa reductase |
| US7439246B2 (en) | 2004-06-28 | 2008-10-21 | Bristol-Myers Squibb Company | Fused heterocyclic kinase inhibitors |
| US20050288290A1 (en) | 2004-06-28 | 2005-12-29 | Borzilleri Robert M | Fused heterocyclic kinase inhibitors |
| EP1945222B1 (en) | 2005-11-02 | 2012-12-26 | Bayer Pharma Aktiengesellschaft | Pyrrolo[2,1-f] [1,2,4]-triazin-4-ylamines as igf-1r kinase inhibitors for the treatment of cancer and other hyperproliferative diseases |
| US7348325B2 (en) | 2005-11-30 | 2008-03-25 | Bristol-Myers Squibb Company | Pyrrolotriazine kinase inhibitors |
| PL1973910T3 (pl) | 2006-01-27 | 2013-11-29 | Shanghai hengrui pharmaceutical co ltd | Pirolo[3,2-c]pirydyn-4-onowo-2-indolinonowe inhibitory kinazy białkowej |
| SI2041138T1 (sl) | 2006-07-07 | 2014-08-29 | Bristol-Myers Squibb Company | Pirolotriazin kinazni inhibitorji |
| US8415340B2 (en) | 2007-07-25 | 2013-04-09 | Bristol-Myers Squibb Company | Triazine kinase inhibitors |
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| KR20100003912A (ko) | 2008-07-02 | 2010-01-12 | 삼성전자주식회사 | 동일 포맷의 미디어 파일 간에 미디어 정보 호환이 가능한미디어 파일을 생성하는 방법 및 장치와 미디어 파일을실행하는 방법 및 장치 |
| WO2010022055A2 (en) | 2008-08-20 | 2010-02-25 | Amgen Inc. | Inhibitors of voltage-gated sodium channels |
| CA2764818A1 (en) | 2009-06-08 | 2010-12-16 | California Capital Equity, Llc | Triazine derivatives and their therapeutical applications |
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| WO2012027495A1 (en) | 2010-08-27 | 2012-03-01 | University Of The Pacific | Piperazinylpyrimidine analogues as protein kinase inhibitors |
| CN102040494A (zh) | 2010-11-12 | 2011-05-04 | 西北师范大学 | 对氟苯甲醛的制备方法 |
| NZ703495A (en) | 2012-07-11 | 2018-02-23 | Blueprint Medicines Corp | Inhibitors of the fibroblast growth factor receptor |
| JP6318156B2 (ja) | 2012-09-06 | 2018-04-25 | プレキシコン インコーポレーテッドＰｌｅｘｘｉｋｏｎ Ｉｎｃ． | キナーゼをモジュレートするための化合物および方法、ならびにその指標 |
| ME03000B (me) | 2012-12-21 | 2018-10-20 | Plexxikon Inc | Jedinjenja i metode modulacije kinaze i povezane indikacije |
| TWI629266B (zh) | 2012-12-28 | 2018-07-11 | 藍印藥品公司 | 纖維母細胞生長因子受體之抑制劑 |
| WO2014160521A1 (en) | 2013-03-15 | 2014-10-02 | Blueprint Medicines Corporation | Piperazine derivatives and their use as kit modulators |
| US9334263B2 (en) | 2013-10-17 | 2016-05-10 | Blueprint Medicines Corporation | Compositions useful for treating disorders related to kit |
| MX365614B (es) | 2013-10-17 | 2019-06-07 | Blueprint Medicines Corp | Composiciones utiles para tratar trastornos relacionados con kit. |
| PT3395814T (pt) | 2013-10-25 | 2022-07-27 | Blueprint Medicines Corp | Inibidores do recetor do fator de crescimento de fibroblastos |
| WO2015108992A1 (en) | 2014-01-15 | 2015-07-23 | Blueprint Medicines Corporation | Heterobicyclic compounds and their use as fgfr4 receptor inhibitors |
| AR099789A1 (es) | 2014-03-24 | 2016-08-17 | Actelion Pharmaceuticals Ltd | Derivados de 8-(piperazin-1-il)-1,2,3,4-tetrahidro-isoquinolina |
| US9688680B2 (en) | 2014-08-04 | 2017-06-27 | Blueprint Medicines Corporation | Compositions useful for treating disorders related to kit |
| US10202365B2 (en) | 2015-02-06 | 2019-02-12 | Blueprint Medicines Corporation | 2-(pyridin-3-yl)-pyrimidine derivatives as RET inhibitors |
| BR112018001190A2 (pt) | 2015-07-24 | 2018-09-11 | Blueprint Medicines Corp | composições úteis para tratar distúrbios relacionados a kit e pdfgr |
| WO2017035354A1 (en) | 2015-08-26 | 2017-03-02 | Blueprint Medicines Corporation | Compounds and compositions useful for treating disorders related to ntrk |
| US20170119760A1 (en) | 2015-10-28 | 2017-05-04 | Ab Science | Use of masitinib for the treatment of progressive supranuclear palsy |
| RS65069B1 (sr) | 2015-11-02 | 2024-02-29 | Blueprint Medicines Corp | Inhibitori ret-a |
| SG10201912607SA (en) | 2015-11-19 | 2020-02-27 | Blueprint Medicines Corp | Compounds and compositions useful for treating disorders related to ntrk |
| AR107912A1 (es) | 2016-03-17 | 2018-06-28 | Blueprint Medicines Corp | Inhibidores de ret |
| FI3442977T3 (fi) | 2016-04-15 | 2023-09-26 | Blueprint Medicines Corp | Aktiviinireseptorin kaltaisen kinaasin estäjät |
| JP7042812B2 (ja) | 2016-06-20 | 2022-03-28 | ノバルティス アーゲー | トリアゾロピリミジン化合物の結晶形態 |
| WO2018017983A1 (en) | 2016-07-22 | 2018-01-25 | Blueprint Medicines Corporation | Compounds useful for treating disorders related to ret |
| US10035789B2 (en) | 2016-07-27 | 2018-07-31 | Blueprint Medicines Corporation | Compounds useful for treating disorders related to RET |
| CN110022900A (zh) | 2016-09-08 | 2019-07-16 | 蓝图药品公司 | 成纤维细胞生长因子受体4抑制剂与细胞周期蛋白依赖性激酶抑制剂的组合 |
| WO2018183712A1 (en) | 2017-03-31 | 2018-10-04 | Blueprint Medicines Corporation | Pyrrolo[1,2-b]pyridazine compounds and compositions useful for treating disorders related to kit and pdgfr |
| CN109400610A (zh) | 2017-08-18 | 2019-03-01 | 浙江海正药业股份有限公司 | 吡咯并三嗪类衍生物、其制备方法及其在医药上的用途 |
| CN108191874B (zh) | 2018-01-16 | 2019-11-29 | 成都施贝康生物医药科技有限公司 | 一种C-Kit抑制剂及其应用 |
| CN118903436A (zh) * | 2018-01-31 | 2024-11-08 | 德西费拉制药有限责任公司 | 治疗肥大细胞增多症的组合疗法 |
| WO2020102095A1 (en) | 2018-11-12 | 2020-05-22 | Blueprint Medicines Corporation | Avapritinib resistance of kit mutants |
| HUE064283T2 (hu) | 2019-04-12 | 2024-02-28 | Blueprint Medicines Corp | Az (S)-1-(4-fluorofenil)-1-(2-(4-(6-(1-metil-1H-pirazol-4-il)pirrolo[2,1-f][1,2,4]triazin-4-il) piperazinil)-pirimidin-5-il)etán-1-amin kristályos formái és elõállítási eljárásai |
| US12590095B2 (en) | 2019-07-09 | 2026-03-31 | Sandoz Ag | Crystalline forms of an orally available, selective kit and PDGFR kinase inhibitor |
| GB201915447D0 (en) | 2019-10-24 | 2019-12-11 | Johnson Matthey Plc | Polymorphs of avapritinib and methods of preparing the polymorphs |
| US20220370465A1 (en) | 2019-11-04 | 2022-11-24 | Blueprint Medicines Corporation | Treatment of mast cell diseases and eosinophilic disorders |
| CN110938077B (zh) | 2019-12-25 | 2021-04-27 | 武汉九州钰民医药科技有限公司 | 合成Avapritinib的方法 |
| CN110950872A (zh) | 2019-12-25 | 2020-04-03 | 武汉九州钰民医药科技有限公司 | 制备靶向抗癌药avapritinib的方法 |
-
2020
- 2020-04-10 HU HUE20722936A patent/HUE064283T2/hu unknown
- 2020-04-10 FI FIEP20722936.0T patent/FI3856341T3/fi active
- 2020-04-10 WO PCT/US2020/027724 patent/WO2020210669A1/en not_active Ceased
- 2020-04-10 LT LTEPPCT/US2020/027724T patent/LT3856341T/lt unknown
- 2020-04-10 DK DK20722936.0T patent/DK3856341T3/da active
- 2020-04-10 JP JP2021560265A patent/JP7728178B2/ja active Active
- 2020-04-10 ES ES20722936T patent/ES2966512T3/es active Active
- 2020-04-10 HR HRP20231533TT patent/HRP20231533T1/hr unknown
- 2020-04-10 EP EP23195076.7A patent/EP4302761A3/en active Pending
- 2020-04-10 SM SM20230447T patent/SMT202300447T1/it unknown
- 2020-04-10 CA CA3296895A patent/CA3296895A1/en active Pending
- 2020-04-10 RS RS20231131A patent/RS64881B1/sr unknown
- 2020-04-10 EP EP20722936.0A patent/EP3856341B1/en active Active
- 2020-04-10 PL PL20722936.0T patent/PL3856341T3/pl unknown
- 2020-04-10 CN CN202080042782.9A patent/CN113966334B/zh active Active
- 2020-04-10 MA MA053759A patent/MA53759A/fr unknown
- 2020-04-10 SI SI202030328T patent/SI3856341T1/sl unknown
- 2020-04-10 PT PT207229360T patent/PT3856341T/pt unknown
- 2020-04-10 CA CA3136707A patent/CA3136707A1/en active Pending
- 2020-04-10 TW TW109112270A patent/TWI845657B/zh active
-
2021
- 2021-01-20 US US17/153,727 patent/US12060354B2/en active Active
- 2021-10-10 IL IL287148A patent/IL287148A/en unknown
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2022
- 2022-12-08 US US18/077,466 patent/US11964980B2/en active Active
- 2022-12-08 US US18/077,431 patent/US12252494B2/en active Active
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2023
- 2023-12-18 US US18/543,793 patent/US11999744B2/en active Active
-
2024
- 2024-08-12 US US18/800,215 patent/US20260116883A1/en active Pending
-
2025
- 2025-10-28 IL IL324301A patent/IL324301A/en unknown
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