PL3333166T3 - Proces otrzymywania n-[5-(3,5-difluorobenzylo)-1h-indazol-3-ilo]- 4-(4-metylopiperazyn-1-ylo)-2-(tetrahydropiran- 4-yloamino)benzamidu - Google Patents
Proces otrzymywania n-[5-(3,5-difluorobenzylo)-1h-indazol-3-ilo]- 4-(4-metylopiperazyn-1-ylo)-2-(tetrahydropiran- 4-yloamino)benzamiduInfo
- Publication number
- PL3333166T3 PL3333166T3 PL17195806T PL17195806T PL3333166T3 PL 3333166 T3 PL3333166 T3 PL 3333166T3 PL 17195806 T PL17195806 T PL 17195806T PL 17195806 T PL17195806 T PL 17195806T PL 3333166 T3 PL3333166 T3 PL 3333166T3
- Authority
- PL
- Poland
- Prior art keywords
- indazol
- ylamino
- piperazin
- benzamide
- pyran
- Prior art date
Links
- HAYYBYPASCDWEQ-UHFFFAOYSA-N n-[5-[(3,5-difluorophenyl)methyl]-1h-indazol-3-yl]-4-(4-methylpiperazin-1-yl)-2-(oxan-4-ylamino)benzamide Chemical compound C1CN(C)CCN1C(C=C1NC2CCOCC2)=CC=C1C(=O)NC(C1=C2)=NNC1=CC=C2CC1=CC(F)=CC(F)=C1 HAYYBYPASCDWEQ-UHFFFAOYSA-N 0.000 title 1
Classifications
-
- 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
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
- A61K31/4965—Non-condensed pyrazines
- A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
-
- 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)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP12169139 | 2012-05-23 | ||
| EP13724270.7A EP2855460B1 (en) | 2012-05-23 | 2013-05-22 | Process for the preparation of n-[5-(3,5-difluoro-benzyl)-1h-indazol-3-yl]-4-(4-methyl-piperazin-1-yl)-2-(tetrahydro-pyran-4-ylamino)-benzamide |
| EP17195806.9A EP3333166B1 (en) | 2012-05-23 | 2013-05-22 | Process for the preparation of n-[5-(3,5-difluoro-benzyl)-1h-indazol-3-yl]-4-(4-methyl-piperazin-1-yl)-2-(tetrahydro-pyran-4-ylamino)-benzamide |
| PCT/EP2013/060534 WO2013174876A1 (en) | 2012-05-23 | 2013-05-22 | Process for the preparation of n-[5-(3,5-difluoro-benzyl)-1h-indazol-3-yl]-4-(4-methyl-piperazin-1-yl)-2-(tetrahydro-pyran-4-ylamino)-benzamide |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PL3333166T3 true PL3333166T3 (pl) | 2020-09-07 |
Family
ID=48470987
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PL17195806T PL3333166T3 (pl) | 2012-05-23 | 2013-05-22 | Proces otrzymywania n-[5-(3,5-difluorobenzylo)-1h-indazol-3-ilo]- 4-(4-metylopiperazyn-1-ylo)-2-(tetrahydropiran- 4-yloamino)benzamidu |
| PL17192138T PL3290414T3 (pl) | 2012-05-23 | 2013-05-22 | Sposób otrzymywania n-[5-(3,5-difluorobenzylo)-1h-indazol-3-ilo]-4-(4-metylopiperazyn-1-ylo)-2-(tetrahydropiran-4-yloamino)benzamidu |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PL17192138T PL3290414T3 (pl) | 2012-05-23 | 2013-05-22 | Sposób otrzymywania n-[5-(3,5-difluorobenzylo)-1h-indazol-3-ilo]-4-(4-metylopiperazyn-1-ylo)-2-(tetrahydropiran-4-yloamino)benzamidu |
Country Status (17)
| Country | Link |
|---|---|
| US (3) | US9085565B2 (pl) |
| EP (4) | EP3290414B1 (pl) |
| JP (1) | JP6231556B2 (pl) |
| KR (1) | KR102151963B1 (pl) |
| CN (2) | CN104395308B (pl) |
| AR (1) | AR091138A1 (pl) |
| AU (2) | AU2013265288B2 (pl) |
| BR (1) | BR112014028841B1 (pl) |
| CA (1) | CA2873979C (pl) |
| ES (2) | ES2771100T3 (pl) |
| IL (2) | IL235761B (pl) |
| MX (1) | MX355409B (pl) |
| NZ (2) | NZ716487A (pl) |
| PL (2) | PL3333166T3 (pl) |
| RU (1) | RU2602071C2 (pl) |
| TW (1) | TWI579280B (pl) |
| WO (1) | WO2013174876A1 (pl) |
Families Citing this family (48)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8299057B2 (en) * | 2007-07-20 | 2012-10-30 | Nerviano Medical Sciences S.R.L. | Substituted indazole derivatives active as kinase inhibitors |
| RS53350B (sr) | 2008-09-22 | 2014-10-31 | Array Biopharma, Inc. | Supstituisana jedinjenja imidazo[1,2-b]piridazina kao inhibitori trk kinaze |
| HRP20140309T1 (hr) | 2008-10-22 | 2014-05-09 | Array Biopharma, Inc. | SUPSTITUIRANI SPOJEVI PIRAZOLO[1,5-a]PIRIMIDINA KAO INHIBITORI TRK KINAZE |
| AR077468A1 (es) | 2009-07-09 | 2011-08-31 | Array Biopharma Inc | Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa |
| KR102015402B1 (ko) | 2010-05-20 | 2019-08-28 | 어레이 바이오파마 인크. | Trk 키나제 저해제로서의 매크로시클릭 화합물 |
| KR102151963B1 (ko) * | 2012-05-23 | 2020-09-07 | 네르비아노 메디칼 사이언시스 에스.알.엘. | Ｎ-[5-(3,5-디플루오로-벤질)-1ｈ-인다졸-3-일]-4-(4-메틸-피페라진-1-일)-2-(테트라하이드로-피란-4-일아미노)-벤즈아미드의 제조 방법 |
| WO2015017533A1 (en) | 2013-07-30 | 2015-02-05 | Blueprint Medicines Corporation | Ntrk2 fusions |
| TWI672141B (zh) * | 2014-02-20 | 2019-09-21 | 美商醫科泰生技 | 投予ｒｏｓ１突變癌細胞之分子 |
| JP6914834B2 (ja) | 2014-11-16 | 2021-08-04 | アレイ バイオファーマ インコーポレイテッド | （Ｓ）−Ｎ−（５−（（Ｒ）−２−（２，５−ジフルオロフェニル）−ピロリジン−１−イル）−ピラゾロ［１，５−ａ］ピリミジン−３−イル）−３−ヒドロキシピロリジン−１−カルボキサミド硫酸水素塩の結晶形 |
| KR102595599B1 (ko) | 2014-12-02 | 2023-11-02 | 이그니타, 인코포레이티드 | 신경모세포종의 치료를 위한 병용 |
| WO2016089853A1 (en) * | 2014-12-03 | 2016-06-09 | Ignyta, Inc. | Multiplexed immunohistochemistry assays for diagnosis and treatment of cancer |
| KR20180021745A (ko) | 2015-06-01 | 2018-03-05 | 록쏘 온콜로지, 인코포레이티드 | 암을 진단하고 치료하는 방법 |
| RU2018103913A (ru) * | 2015-07-02 | 2019-08-02 | Асерта Фарма Б.В. | Твердые формы и композиции (s)-4-(8-амино-3-(1-(бут-2- иноил)пирролидин-2-ил)имидазо[1,5-a]пиразин-1-ил)-n-(пиридин-2-ил)бензамида |
| HUE053067T2 (hu) | 2015-07-16 | 2021-06-28 | Array Biopharma Inc | Helyettesített pirazolo[1,5-A]piridin vegyületek, mint RET kináz inhibitorok |
| TN2018000138A1 (en) | 2015-10-26 | 2019-10-04 | Array Biopharma Inc | Point mutations in trk inhibitor-resistant cancer and methods relating to the same |
| CN108697661A (zh) | 2015-12-18 | 2018-10-23 | 亚尼塔公司 | 用于治疗癌症的组合 |
| AU2017246554B2 (en) | 2016-04-04 | 2022-08-18 | Loxo Oncology, Inc. | Liquid formulations of (S)-N-(5-((R)-2-(2,5-difluorophenyl)-pyrrolidin-1-yl)-pyrazolo(1,5-a)pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide |
| ES2987501T3 (es) | 2016-04-04 | 2024-11-15 | Loxo Oncology Inc | Métodos de tratamiento de cánceres pediátricos |
| US10045991B2 (en) | 2016-04-04 | 2018-08-14 | Loxo Oncology, Inc. | Methods of treating pediatric cancers |
| KR102566858B1 (ko) | 2016-05-18 | 2023-08-11 | 어레이 바이오파마 인크. | (s)-n-(5-((r)-2-(2,5-디플루오로페닐)피롤리딘-1-일)-피라졸로[1,5-a]피리미딘-3-일)-3-히드록시피롤리딘-1-카르복사미드의 제조 방법 |
| MX379558B (es) * | 2016-05-24 | 2025-03-11 | Nerviano Medical Sciences Srl | Nueva forma cristalina de n-[5-(3,5-difluoro-bencilo)-1h-indazol-3-il]-4-(4-metilo-piperazina-1-il)-2-(tetrahidro-pirano-4-ilamino)-benzamida. |
| TWI704148B (zh) | 2016-10-10 | 2020-09-11 | 美商亞雷生物製藥股份有限公司 | 作為ｒｅｔ激酶抑制劑之經取代吡唑并[1,5-a]吡啶化合物 |
| TWI752098B (zh) | 2016-10-10 | 2022-01-11 | 美商亞雷生物製藥股份有限公司 | 作為ret激酶抑制劑之經取代吡唑并[1,5-a]吡啶化合物 |
| JOP20190092A1 (ar) | 2016-10-26 | 2019-04-25 | Array Biopharma Inc | عملية لتحضير مركبات بيرازولو[1، 5-a]بيريميدين وأملاح منها |
| EP3568204B1 (en) | 2017-01-10 | 2023-08-30 | Novartis AG | Pharmaceutical combination comprising an alk inhibitor and an shp2 inhibitor |
| WO2018136663A1 (en) | 2017-01-18 | 2018-07-26 | Array Biopharma, Inc. | Ret inhibitors |
| US11168090B2 (en) | 2017-01-18 | 2021-11-09 | Array Biopharma Inc. | Substituted pyrazolo[1,5-a]pyrazines as RET kinase inhibitors |
| JOP20190213A1 (ar) | 2017-03-16 | 2019-09-16 | Array Biopharma Inc | مركبات حلقية ضخمة كمثبطات لكيناز ros1 |
| EP3654952A1 (en) | 2017-07-19 | 2020-05-27 | Ignyta, Inc. | Pharmaceutical compositions comprising entrectinib |
| TWI812649B (zh) | 2017-10-10 | 2023-08-21 | 美商絡速藥業公司 | 6-(2-羥基-2-甲基丙氧基)-4-(6-(6-((6-甲氧基吡啶-3-基)甲基)-3,6-二氮雜雙環[3.1.1]庚-3-基)吡啶-3-基)吡唑并[1,5-a]吡啶-3-甲腈之調配物 |
| TWI791053B (zh) | 2017-10-10 | 2023-02-01 | 美商亞雷生物製藥股份有限公司 | 6-(2-羥基-2-甲基丙氧基)-4-(6-(6-((6-甲氧基吡啶-3-基)甲基)-3,6-二氮雜雙環[3.1.1]庚-3-基)吡啶-3-基)吡唑并[1,5-a]吡啶-3-甲腈之結晶形式及其醫藥組合物 |
| JP7311498B2 (ja) | 2017-10-17 | 2023-07-19 | イグナイタ インコーポレイテッド | 薬学的組成物および剤形 |
| WO2019084285A1 (en) | 2017-10-26 | 2019-05-02 | Qian Zhao | FORMULATIONS OF A MACROCYCLIC TRK KINASE INHIBITOR |
| EP3740490A1 (en) | 2018-01-18 | 2020-11-25 | Array Biopharma, Inc. | Substituted pyrazolo[3,4-d]pyrimidine compounds as ret kinase inhibitors |
| CA3087972C (en) | 2018-01-18 | 2023-01-10 | Array Biopharma Inc. | Substituted pyrazolyl[4,3-c]pyridinecompounds as ret kinase inhibitors |
| EP3740491A1 (en) | 2018-01-18 | 2020-11-25 | Array Biopharma, Inc. | Substituted pyrrolo[2,3-d]pyrimidines compounds as ret kinase inhibitors |
| CA3095366A1 (en) | 2018-03-29 | 2019-10-03 | Loxo Oncology, Inc. | Treatment of trk-associated cancers |
| CA3224985C (en) | 2018-07-31 | 2025-11-18 | Loxo Oncology, Inc. | SPRAY-DRIED DISPERSIONS, FORMULATIONS AND POLYMORPHIES OF (S)-5-AMINO-3-(4-((5-FLUORO-2-METHOXYBENZAMIDO)METHYL)PHENYL)(1,1,1-TRIFLUOROPROPANE-2-YL)-1H-PYRAZOLE-4-CARBOXAMIDE |
| JP2022500383A (ja) | 2018-09-10 | 2022-01-04 | アレイ バイオファーマ インコーポレイテッド | Ｒｅｔキナーゼ阻害剤としての縮合複素環式化合物 |
| CN113474337A (zh) | 2018-12-19 | 2021-10-01 | 奥瑞生物药品公司 | 作为fgfr抑制剂用于治疗癌症的7-((3，5-二甲氧基苯基)氨基)喹喔啉衍生物 |
| EP3898626A1 (en) | 2018-12-19 | 2021-10-27 | Array Biopharma, Inc. | Substituted pyrazolo[1,5-a]pyridine compounds as inhibitors of fgfr tyrosine kinases |
| CA3144840A1 (en) * | 2019-07-31 | 2021-02-04 | Leonie Flurina Claude Wagner-Hattler | New pharmaceutical formulation |
| US20220372024A1 (en) * | 2019-11-01 | 2022-11-24 | Johnson Matthey Public Limited Company | Crystalline forms of entrectinib |
| CN113024521B (zh) * | 2019-12-09 | 2023-01-17 | 武汉九州钰民医药科技有限公司 | 一种制备恩曲替尼的方法 |
| CN111171009B (zh) * | 2020-01-10 | 2022-07-12 | 安礼特（上海）医药科技有限公司 | 恩曲替尼晶型及其制备方法 |
| CN113354626B (zh) * | 2020-03-04 | 2025-06-03 | 罗欣药业(上海)有限公司 | 恩曲替尼的晶型及其制备方法 |
| CN113801062B (zh) * | 2020-06-15 | 2023-05-26 | 沈阳药科大学 | 3-氨基-5-(3,5-二氟苄基)-1h-吲唑的制备方法 |
| US20240308990A1 (en) * | 2021-02-03 | 2024-09-19 | Qilu Pharmaceutical Co., Ltd. | Crystal form of entrectinib and preparation method therefor |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FI58125C (fi) * | 1976-12-15 | 1985-01-02 | Orion Yhtymae Oy | Foerfarande foer framstaellning av 6,7-dimetoxi-4-amino-2-(4-(2-furoyl)-1-piperazinyl)kinazolin med blodtryckssaenkande vekan |
| DE19730989A1 (de) * | 1997-07-18 | 1999-01-21 | Merck Patent Gmbh | Piperazin-Derivate |
| EP2120932B1 (en) * | 2006-12-20 | 2014-07-09 | Nerviano Medical Sciences S.r.l. | Indazole derivatives as kinase inhibitors for the treatment of cancer |
| US8299057B2 (en) * | 2007-07-20 | 2012-10-30 | Nerviano Medical Sciences S.R.L. | Substituted indazole derivatives active as kinase inhibitors |
| ES2630026T3 (es) * | 2008-12-18 | 2017-08-17 | Nerviano Medical Sciences S.R.L. | Derivados indazólicos sustituidos activos como inhibidores de cinasa |
| KR102151963B1 (ko) | 2012-05-23 | 2020-09-07 | 네르비아노 메디칼 사이언시스 에스.알.엘. | Ｎ-[5-(3,5-디플루오로-벤질)-1ｈ-인다졸-3-일]-4-(4-메틸-피페라진-1-일)-2-(테트라하이드로-피란-4-일아미노)-벤즈아미드의 제조 방법 |
-
2013
- 2013-05-22 KR KR1020147036163A patent/KR102151963B1/ko active Active
- 2013-05-22 TW TW102118026A patent/TWI579280B/zh active
- 2013-05-22 EP EP17192138.0A patent/EP3290414B1/en active Active
- 2013-05-22 ES ES17195806T patent/ES2771100T3/es active Active
- 2013-05-22 CA CA2873979A patent/CA2873979C/en active Active
- 2013-05-22 RU RU2014151565/04A patent/RU2602071C2/ru active
- 2013-05-22 NZ NZ716487A patent/NZ716487A/en unknown
- 2013-05-22 NZ NZ703124A patent/NZ703124A/en unknown
- 2013-05-22 BR BR112014028841-0A patent/BR112014028841B1/pt active IP Right Grant
- 2013-05-22 CN CN201380026532.6A patent/CN104395308B/zh active Active
- 2013-05-22 CN CN201610455414.2A patent/CN106167485A/zh active Pending
- 2013-05-22 JP JP2015513159A patent/JP6231556B2/ja active Active
- 2013-05-22 ES ES17192138T patent/ES2751944T3/es active Active
- 2013-05-22 EP EP13724270.7A patent/EP2855460B1/en not_active Withdrawn - After Issue
- 2013-05-22 PL PL17195806T patent/PL3333166T3/pl unknown
- 2013-05-22 PL PL17192138T patent/PL3290414T3/pl unknown
- 2013-05-22 MX MX2014013924A patent/MX355409B/es active IP Right Grant
- 2013-05-22 EP EP17195806.9A patent/EP3333166B1/en active Active
- 2013-05-22 AU AU2013265288A patent/AU2013265288B2/en active Active
- 2013-05-22 WO PCT/EP2013/060534 patent/WO2013174876A1/en not_active Ceased
- 2013-05-22 EP EP19188774.4A patent/EP3581571A1/en not_active Withdrawn
- 2013-05-23 AR ARP130101795 patent/AR091138A1/es unknown
-
2014
- 2014-10-30 US US14/528,475 patent/US9085565B2/en active Active
- 2014-11-18 IL IL235761A patent/IL235761B/en active IP Right Grant
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2015
- 2015-05-20 US US14/716,986 patent/US9382235B2/en active Active
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2016
- 2016-06-03 US US15/172,478 patent/US9649306B2/en active Active
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2018
- 2018-02-13 AU AU2018201037A patent/AU2018201037B2/en active Active
- 2018-06-27 IL IL260297A patent/IL260297A/en unknown
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