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)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (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 |
| 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 |
| 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 |
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 |
|---|---|---|---|
| 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 |
| 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 |
Family Applications Before (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) | EP3333166B1 (pl) |
| JP (1) | JP6231556B2 (pl) |
| KR (1) | KR102151963B1 (pl) |
| CN (2) | CN106167485A (pl) |
| AR (1) | AR091138A1 (pl) |
| AU (2) | AU2013265288B2 (pl) |
| BR (1) | BR112014028841B1 (pl) |
| CA (1) | CA2873979C (pl) |
| ES (2) | ES2751944T3 (pl) |
| IL (2) | IL235761B (pl) |
| MX (1) | MX355409B (pl) |
| NZ (2) | NZ716487A (pl) |
| PL (2) | PL3290414T3 (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 |
| PT2725028T (pt) | 2008-10-22 | 2016-08-31 | Array Biopharma Inc | Compostos de pirazolo[1,5-]pirimidina substituídos como intermediários na síntese de inibidores de cinase trk |
| AR077468A1 (es) | 2009-07-09 | 2011-08-31 | Array Biopharma Inc | Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa |
| HUE044025T2 (hu) | 2010-05-20 | 2019-09-30 | Array Biopharma Inc | Makrociklusos vegyületek mint TRK-kináz inhibitorok |
| NZ716487A (en) * | 2012-05-23 | 2017-01-27 | Nerviano Medical Sciences Srl | 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 |
| EP3027655B1 (en) | 2013-07-30 | 2019-08-21 | 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 |
| FI3699181T3 (fi) | 2014-11-16 | 2023-03-28 | Array Biopharma Inc | Kiteinen muoto (s)-n-(5-((r)-2-(2,5-diluorifenyyli)-pyrrolidin-1-yyli)-pyratsolo[1,5-a]pyrimidin-3-yyli)-3-hydroksipyrrolidiini-1-karboksamidivetyysulfaatista |
| KR102595599B1 (ko) * | 2014-12-02 | 2023-11-02 | 이그니타, 인코포레이티드 | 신경모세포종의 치료를 위한 병용 |
| US20170356918A1 (en) * | 2014-12-03 | 2017-12-14 | Ignyta, Inc. | Multiplexed immunohistochemistry assays for diagnosis and treatment of cancer |
| MX2017015461A (es) | 2015-06-01 | 2018-08-15 | Loxo Oncology Inc | Métodos para diagnosticar y tratar el cáncer. |
| WO2017002095A1 (en) * | 2015-07-02 | 2017-01-05 | Acerta Pharma B.V. | Solid forms and formulations of (s)-4-(8-amino-3-(1 -(but-2-ynoyl)pyrrolidin-2-yl)imidazo[1,5-a]pyrazin-1-yl)-n-(pyridin-2-yl)benzamide |
| PL3322706T3 (pl) | 2015-07-16 | 2021-07-19 | Array Biopharma, Inc. | Podstawione związki pirazolo[1,5-a]pirydynowe jako inhibitory kinazy ret |
| EP3368039A1 (en) | 2015-10-26 | 2018-09-05 | The Regents of The University of Colorado, A Body Corporate | Point mutations in trk inhibitor-resistant cancer and methods relating to the same |
| EP3389645A4 (en) | 2015-12-18 | 2019-12-18 | Ignyta, Inc. | COMBINATIONS FOR TREATING CANCER |
| US10045991B2 (en) | 2016-04-04 | 2018-08-14 | Loxo Oncology, Inc. | Methods of treating pediatric cancers |
| CA3019661A1 (en) | 2016-04-04 | 2017-10-12 | Loxo Oncology, Inc. | Methods of treating pediatric cancers |
| RS65987B1 (sr) | 2016-04-04 | 2024-10-31 | Loxo Oncology Inc | Tečne formulacije (s)-n-(5-((r)-2-(2,5-difluorofenil)-pirolidin-1-il)-pirazolo[1,5-]pirimidin-3-il)-3-hidroksipirolidin-1-karboksamida |
| EP3800189B1 (en) | 2016-05-18 | 2023-06-28 | Loxo Oncology, Inc. | Preparation of (s)-n-(5-((r)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide |
| CN109153669B (zh) * | 2016-05-24 | 2021-12-24 | 内尔维阿诺医学科学有限公司 | 苯甲酰胺类化合物的新晶型 |
| JOP20190077A1 (ar) | 2016-10-10 | 2019-04-09 | Array Biopharma Inc | مركبات بيرازولو [1، 5-a]بيريدين بها استبدال كمثبطات كيناز ret |
| 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 |
| JOP20190092A1 (ar) | 2016-10-26 | 2019-04-25 | Array Biopharma Inc | عملية لتحضير مركبات بيرازولو[1، 5-a]بيريميدين وأملاح منها |
| ES2964956T3 (es) * | 2017-01-10 | 2024-04-10 | Novartis Ag | Combinación farmacéutica que comprende un inhibidor de ALK y un inhibidor de SHP2 |
| 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 |
| WO2019018570A1 (en) | 2017-07-19 | 2019-01-24 | Ignyta, Inc. | PHARMACEUTICAL COMPOSITIONS CONTAINING ENTRECTINIB |
| 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 |
| TWI876442B (zh) | 2017-10-10 | 2025-03-11 | 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 |
| 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 |
| US20190247398A1 (en) | 2017-10-26 | 2019-08-15 | Array Biopharma Inc. | Formulations of a macrocyclic trk kinase inhibitor |
| EP3740491A1 (en) | 2018-01-18 | 2020-11-25 | Array Biopharma, Inc. | Substituted pyrrolo[2,3-d]pyrimidines compounds as ret kinase inhibitors |
| EP3740486A1 (en) | 2018-01-18 | 2020-11-25 | Array Biopharma, Inc. | Substituted pyrazolyl[4,3-c]pyridinecompounds as ret kinase inhibitors |
| CA3087578C (en) | 2018-01-18 | 2023-08-08 | Array Biopharma Inc. | Substituted pyrazolo[3,4-d]pyrimidine compounds as ret kinase inhibitors |
| WO2019191659A1 (en) | 2018-03-29 | 2019-10-03 | Loxo Oncology, Inc. | Treatment of trk-associated cancers |
| CN117281803A (zh) | 2018-07-31 | 2023-12-26 | 罗索肿瘤学公司 | 喷雾干燥的分散体和制剂 |
| WO2020055672A1 (en) | 2018-09-10 | 2020-03-19 | Array Biopharma Inc. | Fused heterocyclic compounds as ret kinase inhibitors |
| JP2022515197A (ja) | 2018-12-19 | 2022-02-17 | アレイ バイオファーマ インコーポレイテッド | がんを治療するためのｆｇｆｒ阻害剤としての７－（（３，５－ジメトキシフェニル）アミノ）キノキサリン誘導体 |
| EP3898626A1 (en) | 2018-12-19 | 2021-10-27 | Array Biopharma, Inc. | Substituted pyrazolo[1,5-a]pyridine compounds as inhibitors of fgfr tyrosine kinases |
| EP4003309A1 (en) | 2019-07-31 | 2022-06-01 | F. Hoffmann-La Roche AG | New pharmaceutical formulation |
| WO2021084260A1 (en) * | 2019-11-01 | 2021-05-06 | Johnson Matthey Public Limited Company | Crystalline entrectinib anhydrate and monohydrate forms; crystalline entrectinib thf, nitromethane, isopropyl acetate and methanol solvate forms; processes for preparing a crystalline entrectinib anhydrate form |
| 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 |
| EA017852B1 (ru) * | 2006-12-20 | 2013-03-29 | НЕРВИАНО МЕДИКАЛ САЙЕНСИЗ С.р.л. | Производные замещенных индазолов, активные в качестве ингибиторов киназ |
| US8299057B2 (en) * | 2007-07-20 | 2012-10-30 | Nerviano Medical Sciences S.R.L. | Substituted indazole derivatives active as kinase inhibitors |
| JP5580332B2 (ja) * | 2008-12-18 | 2014-08-27 | ネルビアーノ・メデイカル・サイエンシーズ・エツセ・エルレ・エルレ | キナーゼ阻害剤として活性な置換インダゾール誘導体 |
| NZ716487A (en) | 2012-05-23 | 2017-01-27 | Nerviano Medical Sciences Srl | 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 |
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2013
- 2013-05-22 NZ NZ716487A patent/NZ716487A/en unknown
- 2013-05-22 CA CA2873979A patent/CA2873979C/en active Active
- 2013-05-22 PL PL17192138T patent/PL3290414T3/pl unknown
- 2013-05-22 AU AU2013265288A patent/AU2013265288B2/en active Active
- 2013-05-22 CN CN201610455414.2A patent/CN106167485A/zh active Pending
- 2013-05-22 EP EP17195806.9A patent/EP3333166B1/en active Active
- 2013-05-22 EP EP17192138.0A patent/EP3290414B1/en active Active
- 2013-05-22 KR KR1020147036163A patent/KR102151963B1/ko active Active
- 2013-05-22 CN CN201380026532.6A patent/CN104395308B/zh active Active
- 2013-05-22 JP JP2015513159A patent/JP6231556B2/ja active Active
- 2013-05-22 BR BR112014028841-0A patent/BR112014028841B1/pt active IP Right Grant
- 2013-05-22 ES ES17192138T patent/ES2751944T3/es active Active
- 2013-05-22 NZ NZ703124A patent/NZ703124A/en unknown
- 2013-05-22 RU RU2014151565/04A patent/RU2602071C2/ru active
- 2013-05-22 WO PCT/EP2013/060534 patent/WO2013174876A1/en not_active Ceased
- 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 EP EP19188774.4A patent/EP3581571A1/en not_active Withdrawn
- 2013-05-22 ES ES17195806T patent/ES2771100T3/es active Active
- 2013-05-22 TW TW102118026A patent/TWI579280B/zh active
- 2013-05-22 MX MX2014013924A patent/MX355409B/es active IP Right Grant
- 2013-05-23 AR ARP130101795 patent/AR091138A1/es unknown
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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
-
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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