PL3290414T3 - Sposób otrzymywania n-[5-(3,5-difluorobenzylo)-1h-indazol-3-ilo]-4-(4-metylopiperazyn-1-ylo)-2-(tetrahydropiran-4-yloamino)benzamidu - Google Patents
Sposób otrzymywania n-[5-(3,5-difluorobenzylo)-1h-indazol-3-ilo]-4-(4-metylopiperazyn-1-ylo)-2-(tetrahydropiran-4-yloamino)benzamiduInfo
- Publication number
- PL3290414T3 PL3290414T3 PL17192138T PL17192138T PL3290414T3 PL 3290414 T3 PL3290414 T3 PL 3290414T3 PL 17192138 T PL17192138 T PL 17192138T PL 17192138 T PL17192138 T PL 17192138T PL 3290414 T3 PL3290414 T3 PL 3290414T3
- 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
-
- 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
- C07D405/02—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
-
- 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)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Public Health (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 | ||
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 |
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 |
EP17192138.0A EP3290414B1 (en) | 2012-05-23 | 2013-05-22 | Crystalline form 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 |
---|---|
PL3290414T3 true PL3290414T3 (pl) | 2020-01-31 |
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 After (1)
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 |
Country Status (17)
Country | Link |
---|---|
US (3) | US9085565B2 (pl) |
EP (4) | EP2855460B1 (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) | ES2751944T3 (pl) |
IL (2) | IL235761B (pl) |
MX (1) | MX355409B (pl) |
NZ (2) | NZ703124A (pl) |
PL (2) | PL3290414T3 (pl) |
RU (1) | RU2602071C2 (pl) |
TW (1) | TWI579280B (pl) |
WO (1) | WO2013174876A1 (pl) |
Families Citing this family (48)
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NZ583450A (en) * | 2007-07-20 | 2012-05-25 | Nerviano Medical Sciences Srl | Substituted indazole derivatives active as kinase inhibitors |
CN102224153B (zh) | 2008-09-22 | 2014-04-30 | 阵列生物制药公司 | 作为trk激酶抑制剂的取代的咪唑并[1,2-b]哒嗪化合物 |
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 |
BR112012029405B1 (pt) | 2010-05-20 | 2021-01-05 | Array Biopharma Inc. | compostos macrocíclicos como inibidores de trk quinase, composição farmacêutica, uso de um composto de fórmula i ou um sal farmaceuticamente aceitável do mesmo, processo para a preparação de um composto |
EP2855460B1 (en) * | 2012-05-23 | 2017-11-08 | Nerviano Medical Sciences S.r.l. | 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 |
US10407509B2 (en) | 2013-07-30 | 2019-09-10 | Blueprint Medicines Corporation | NTRK2 fusions |
US10231965B2 (en) * | 2014-02-20 | 2019-03-19 | Ignyta, Inc. | Molecules for administration to ROS1 mutant cancer cells |
MX376478B (es) | 2014-11-16 | 2025-03-07 | Array Biopharma Inc | Forma cristalina de sulfato acido de (s)-n-(5-((r)-2-(2,5-difluorofenil)-pirrolidin-1-il)-pirazolo[1,5-a]-pirimidin-3-il)-3-hidroxipirrolidina-1-carboxamida. |
EP3227276B1 (en) * | 2014-12-02 | 2021-09-01 | Ignyta, Inc. | Combinations for the treatment of neuroblastoma |
WO2016089853A1 (en) * | 2014-12-03 | 2016-06-09 | Ignyta, Inc. | Multiplexed immunohistochemistry assays for diagnosis and treatment of cancer |
US20180140604A1 (en) | 2015-06-01 | 2018-05-24 | Loxo Oncology, Inc. | Methods of diagnosing and treating cancer |
ES2797987T3 (es) * | 2015-07-02 | 2020-12-04 | Acerta Pharma Bv | Formas sólidas y formulaciones de (S)-4-(8-amino-3-(1-(but-2-inoil)pirrolidin-2-il)imidazo[1,5-a]pirazin-1-il)-N-(piridin-2-il)benzamida |
DK3322706T3 (da) | 2015-07-16 | 2021-02-01 | Array Biopharma Inc | Substituerede pyrazolo[1,5-a]pyridin-forbindelser som ret-kinaseinhibitorer |
RU2744852C2 (ru) | 2015-10-26 | 2021-03-16 | Локсо Онколоджи, Инк. | Точечные мутации в устойчивых к ингибитору trk злокачественных опухолях и связанные с ними способы |
CA3008663A1 (en) | 2015-12-18 | 2017-06-22 | Ignyta, Inc. | Combinations of a selective tyrosine kinase inhibitor (tki) with a mek or erk inhibitor for the treatment of cancer |
HRP20241295T1 (hr) | 2016-04-04 | 2024-12-06 | Loxo Oncology, Inc. | Postupci za liječenje pedijatrijskih karcinoma |
SI3439662T1 (sl) | 2016-04-04 | 2024-11-29 | Loxo Oncology, Inc. | Tekoče formulacije (s)-n-(5-((r)-2-(2,5-difluorofenil)-pirolidin -1-il)-pirazološ1,5-aćpirimidin-3-il)-3-hidroksipirolidin-1-karboksamida |
US10045991B2 (en) | 2016-04-04 | 2018-08-14 | Loxo Oncology, Inc. | Methods of treating pediatric cancers |
DK3800189T3 (da) | 2016-05-18 | 2023-07-31 | Loxo Oncology Inc | Fremstilling af (s)-n-(5-((r)-2-(2,5-difluorphenyl)pyrrolidin-1-yl)pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidin-1-carboxamid |
AU2017271458B2 (en) | 2016-05-24 | 2020-11-26 | Nerviano Medical Sciences S.R.L. | New crystalline form of N-[5-(3,5-difluoro-benzyl)-1H-indazol-3-yl]-4-(4-methyl-piperazin-1-yl)-2-(tetrahydro-pyran-4-ylamino)-benzamide |
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 |
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US20190343836A1 (en) | 2017-01-10 | 2019-11-14 | Novartis Ag | Pharmaceutical combination comprising an alk inhibitor and a shp2 inhibitor |
JP6888101B2 (ja) | 2017-01-18 | 2021-06-16 | 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置換ピラゾロ[1,5−a]ピラジン化合物 |
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JOP20190213A1 (ar) | 2017-03-16 | 2019-09-16 | Array Biopharma Inc | مركبات حلقية ضخمة كمثبطات لكيناز ros1 |
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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 |
TW201932464A (zh) | 2018-01-18 | 2019-08-16 | 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基[4,3-c]吡啶化合物 |
US11603374B2 (en) | 2018-01-18 | 2023-03-14 | Array Biopharma Inc. | Substituted pyrrolo[2,3-d]pyrimidines compounds 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 |
EP3773725A1 (en) | 2018-03-29 | 2021-02-17 | Loxo Oncology Inc. | Treatment of trk-associated cancers |
US12109193B2 (en) | 2018-07-31 | 2024-10-08 | Loxo Oncology Inc. | Spray-dried dispersions, formulations, and polymorphs of (s)-5-amino-3-(4-((5-fluoro-2-methoxybenzamido)methyl)phenyl)-1-(1,1,1-trifluoropropan-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 |
JP2022515198A (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 | FGFRチロシンキナーゼの阻害剤としての置換ピラゾロ[1,5-a]ピリジン化合物 |
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 |
CN119909073A (zh) * | 2019-07-31 | 2025-05-02 | 豪夫迈·罗氏有限公司 | 新型药物制剂 |
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 |
BRPI0720589A2 (pt) * | 2006-12-20 | 2014-02-25 | Nerviano Medical Sciences Srl | Derivados de indazol como inibidores da quinase para tratamento do câncer, derivados de indazol como inibidores da quinase para tratamento do câncer |
NZ583450A (en) * | 2007-07-20 | 2012-05-25 | Nerviano Medical Sciences Srl | 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 |
EP2855460B1 (en) | 2012-05-23 | 2017-11-08 | Nerviano Medical Sciences S.r.l. | 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 |
-
2013
- 2013-05-22 EP EP13724270.7A patent/EP2855460B1/en not_active Withdrawn - After Issue
- 2013-05-22 NZ NZ703124A patent/NZ703124A/en unknown
- 2013-05-22 CN CN201380026532.6A patent/CN104395308B/zh active Active
- 2013-05-22 ES ES17192138T patent/ES2751944T3/es active Active
- 2013-05-22 PL PL17192138T patent/PL3290414T3/pl unknown
- 2013-05-22 MX MX2014013924A patent/MX355409B/es active IP Right Grant
- 2013-05-22 AU AU2013265288A patent/AU2013265288B2/en active Active
- 2013-05-22 WO PCT/EP2013/060534 patent/WO2013174876A1/en active Application Filing
- 2013-05-22 BR BR112014028841-0A patent/BR112014028841B1/pt active IP Right Grant
- 2013-05-22 NZ NZ716487A patent/NZ716487A/en unknown
- 2013-05-22 EP EP17195806.9A patent/EP3333166B1/en active Active
- 2013-05-22 ES ES17195806T patent/ES2771100T3/es active Active
- 2013-05-22 JP JP2015513159A patent/JP6231556B2/ja active Active
- 2013-05-22 RU RU2014151565/04A patent/RU2602071C2/ru active
- 2013-05-22 CA CA2873979A patent/CA2873979C/en active Active
- 2013-05-22 CN CN201610455414.2A patent/CN106167485A/zh active Pending
- 2013-05-22 TW TW102118026A patent/TWI579280B/zh active
- 2013-05-22 EP EP19188774.4A patent/EP3581571A1/en not_active Withdrawn
- 2013-05-22 PL PL17195806T patent/PL3333166T3/pl unknown
- 2013-05-22 EP EP17192138.0A patent/EP3290414B1/en active Active
- 2013-05-22 KR KR1020147036163A patent/KR102151963B1/ko active Active
- 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
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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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