MX355409B - Proceso para la preparacion de n- [5- (3,5-difluoro-bencil) -1h-indazol-3-il] -4- (4-metil-piperazin-1-il) -2- (tetrahidro-piran-4-ilamino) -benzamida. - Google Patents

Proceso para la preparacion de n- [5- (3,5-difluoro-bencil) -1h-indazol-3-il] -4- (4-metil-piperazin-1-il) -2- (tetrahidro-piran-4-ilamino) -benzamida.

Info

Publication number
MX355409B
MX355409B MX2014013924A MX2014013924A MX355409B MX 355409 B MX355409 B MX 355409B MX 2014013924 A MX2014013924 A MX 2014013924A MX 2014013924 A MX2014013924 A MX 2014013924A MX 355409 B MX355409 B MX 355409B
Authority
MX
Mexico
Prior art keywords
piperazin
benzamide
pyran
difluoro
tetrahydro
Prior art date
Application number
MX2014013924A
Other languages
English (en)
Other versions
MX2014013924A (es
Inventor
Alvaro Barbugian Natale
Forino Romualdo
Fumagalli Tiziano
Orsini Paolo
Original Assignee
Nerviano Medical Sciences Srl
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Nerviano Medical Sciences Srl filed Critical Nerviano Medical Sciences Srl
Publication of MX2014013924A publication Critical patent/MX2014013924A/es
Publication of MX355409B publication Critical patent/MX355409B/es

Links

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)

Abstract

La presente invención se refiere a un proceso para la preparación de N-[5-(3,5-difluoro-bencil)-1H-indazol-3-il]-4-(4-metil-piperazi n-1-il)-2-(tetrahidro-piran-4-ilamino) -benzamida. Las nuevas formas sólidas de este compuesto, su utilidad en el tratamiento de enfermedades provocadas por la mala regulación de la actividad de proteína quinasa y composiciones farmacéuticas que las contienen son también el objeto de la presente invención.
MX2014013924A 2012-05-23 2013-05-22 Proceso para la preparacion de n- [5- (3,5-difluoro-bencil) -1h-indazol-3-il] -4- (4-metil-piperazin-1-il) -2- (tetrahidro-piran-4-ilamino) -benzamida. MX355409B (es)

Applications Claiming Priority (2)

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

Publications (2)

Publication Number Publication Date
MX2014013924A MX2014013924A (es) 2015-02-17
MX355409B true MX355409B (es) 2018-04-18

Family

ID=48470987

Family Applications (1)

Application Number Title Priority Date Filing Date
MX2014013924A MX355409B (es) 2012-05-23 2013-05-22 Proceso para la preparacion de n- [5- (3,5-difluoro-bencil) -1h-indazol-3-il] -4- (4-metil-piperazin-1-il) -2- (tetrahidro-piran-4-ilamino) -benzamida.

Country Status (17)

Country Link
US (3) US9085565B2 (es)
EP (4) EP3290414B1 (es)
JP (1) JP6231556B2 (es)
KR (1) KR102151963B1 (es)
CN (2) CN106167485A (es)
AR (1) AR091138A1 (es)
AU (2) AU2013265288B2 (es)
BR (1) BR112014028841B1 (es)
CA (1) CA2873979C (es)
ES (2) ES2751944T3 (es)
IL (2) IL235761B (es)
MX (1) MX355409B (es)
NZ (2) NZ703124A (es)
PL (2) PL3333166T3 (es)
RU (1) RU2602071C2 (es)
TW (1) TWI579280B (es)
WO (1) WO2013174876A1 (es)

Families Citing this family (48)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
HUE030929T2 (en) * 2007-07-20 2017-06-28 Nerviano Medical Sciences Srl Substituted indazole derivatives active as kinase inhibitors
CA2952692C (en) 2008-09-22 2020-04-28 Array Biopharma Inc. Substituted imidazo[1,2b]pyridazine compounds
SG10201900514RA (en) 2008-10-22 2019-02-27 Array Biopharma Inc Substituted pyrazolo[1,5-a]pyrimidine compounds as trk kinase inhibitors
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
EP3290414B1 (en) 2012-05-23 2019-07-24 Nerviano Medical Sciences S.R.L. 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
US10407509B2 (en) 2013-07-30 2019-09-10 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
IL290905B2 (en) 2014-11-16 2023-09-01 Array Biopharma Inc Crystal form of (s)–n-(5–)–2–(r))5,2-difluorophenyl)-pyrrolidine-1-yl)-pyrazolo[5,1-a]pyrimidine-3-yl)-3 -Hydroxypyrrolidine-1-carboxamide hydrogen sulfate
EP3227276B1 (en) 2014-12-02 2021-09-01 Ignyta, Inc. Combinations for the treatment of neuroblastoma
US20170356918A1 (en) * 2014-12-03 2017-12-14 Ignyta, Inc. Multiplexed immunohistochemistry assays for diagnosis and treatment of cancer
HK1253093A1 (zh) 2015-06-01 2019-06-06 Loxo Oncology Inc. 诊断和治疗癌症的方法
KR20240115937A (ko) * 2015-07-02 2024-07-26 아세르타 파마. 비.브이. (S)-4-(8-아미노-3-(1-(부트-2-이노일)피롤리딘-2-일)이미다조[1,5-a]피라진-1-일)-N-(피리딘-2-일)벤즈아마이드의고체 형태 및 제제
EP3322706B1 (en) 2015-07-16 2020-11-11 Array Biopharma, Inc. Substituted pyrazolo[1,5-a]pyridine compounds as ret kinase inhibitors
WO2017075107A1 (en) 2015-10-26 2017-05-04 Nanda Nisha 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
TN2019000332A1 (en) 2016-04-04 2021-05-07 Loxo Oncology Inc Methods of treating pediatric cancers
EP3439662B1 (en) 2016-04-04 2024-07-24 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
US10045991B2 (en) 2016-04-04 2018-08-14 Loxo Oncology, Inc. Methods of treating pediatric cancers
LT3800189T (lt) 2016-05-18 2023-10-10 Loxo Oncology, Inc. (s)-n-(5-((r)-2-(2,5-difluorfenil)pirolidin-1-il)pirazolo[1,5-a]pirimidin-3- il)-3-hidroksipirolidin-1-karboksamido gavimas
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
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
JOP20190077A1 (ar) 2016-10-10 2019-04-09 Array Biopharma Inc مركبات بيرازولو [1، 5-a]بيريدين بها استبدال كمثبطات كيناز ret
JOP20190092A1 (ar) 2016-10-26 2019-04-25 Array Biopharma Inc عملية لتحضير مركبات بيرازولو[1، 5-a]بيريميدين وأملاح منها
AU2018207464B2 (en) 2017-01-10 2020-05-14 Novartis Ag Pharmaceutical combination comprising an ALK inhibitor and a SHP2 inhibitor
WO2018136663A1 (en) 2017-01-18 2018-07-26 Array Biopharma, Inc. Ret inhibitors
CN110267960B (zh) 2017-01-18 2022-04-26 阿雷生物药品公司 作为RET激酶抑制剂的取代的吡唑并[1,5-a]吡嗪化合物
JOP20190213A1 (ar) 2017-03-16 2019-09-16 Array Biopharma Inc مركبات حلقية ضخمة كمثبطات لكيناز ros1
IL271759B2 (en) 2017-07-19 2024-01-01 Ignyta Inc Pharmaceutical compositions comprising 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
EP3697390A1 (en) 2017-10-17 2020-08-26 Ignyta, Inc. Pharmaceutical compositions and dosage forms
MA50456A (fr) 2017-10-26 2020-09-02 Array Biopharma Inc Formulations d'un inhibiteur de kinase trk macrocyclique
CA3087972C (en) 2018-01-18 2023-01-10 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
CA3087354C (en) 2018-01-18 2023-01-03 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
KR102653681B1 (ko) 2018-07-31 2024-04-03 록쏘 온콜로지, 인코포레이티드 (s)-5-아미노-3-(4-((5-플루오로-2-메톡시벤즈아미도)메틸)페닐)-1-(1,1,1-트리플루오로프로판-2-일)-1h-피라졸-4-카르복스아미드의분무-건조된 분산물 및 제제
ES2922314T3 (es) 2018-09-10 2022-09-13 Array Biopharma Inc Compuestos heterocíclicos condensados como inhibidores de cinasa RET
EP3898615A1 (en) 2018-12-19 2021-10-27 Array Biopharma, Inc. 7-((3,5-dimethoxyphenyl)amino)quinoxaline derivatives as fgfr inhibitors for treating cancer
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
AU2020319662B2 (en) 2019-07-31 2024-02-29 F. Hoffmann-La Roche Ag 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
CN116669735B (zh) * 2021-02-03 2026-02-06 齐鲁制药有限公司 恩曲替尼晶型及其制备方法

Family Cites Families (6)

* Cited by examiner, † Cited by third party
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
HUE030929T2 (en) * 2007-07-20 2017-06-28 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
EP3290414B1 (en) 2012-05-23 2019-07-24 Nerviano Medical Sciences S.R.L. 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

Also Published As

Publication number Publication date
US20160279125A1 (en) 2016-09-29
NZ716487A (en) 2017-01-27
MX2014013924A (es) 2015-02-17
US9649306B2 (en) 2017-05-16
BR112014028841B1 (pt) 2021-01-12
TW201400479A (zh) 2014-01-01
TWI579280B (zh) 2017-04-21
IL235761B (en) 2018-07-31
AR091138A1 (es) 2015-01-14
US9382235B2 (en) 2016-07-05
EP3333166B1 (en) 2019-11-06
EP3581571A1 (en) 2019-12-18
RU2014151565A (ru) 2016-07-20
US9085565B2 (en) 2015-07-21
JP6231556B2 (ja) 2017-11-15
EP2855460B1 (en) 2017-11-08
PL3333166T3 (pl) 2020-09-07
JP2015517551A (ja) 2015-06-22
US20150051222A1 (en) 2015-02-19
ES2771100T3 (es) 2020-07-06
CN104395308A (zh) 2015-03-04
ES2751944T3 (es) 2020-04-02
US20150274707A1 (en) 2015-10-01
HK1207077A1 (en) 2016-01-22
IL260297A (en) 2018-08-30
EP2855460A1 (en) 2015-04-08
AU2013265288A2 (en) 2015-01-29
NZ703124A (en) 2016-07-29
KR102151963B1 (ko) 2020-09-07
CA2873979C (en) 2019-11-12
AU2013265288A1 (en) 2015-01-22
EP3290414A1 (en) 2018-03-07
AU2013265288B2 (en) 2017-12-21
RU2602071C2 (ru) 2016-11-10
AU2018201037B2 (en) 2019-07-04
PL3290414T3 (pl) 2020-01-31
CA2873979A1 (en) 2013-11-28
AU2018201037A1 (en) 2018-03-01
KR20150016352A (ko) 2015-02-11
CN104395308B (zh) 2016-08-24
CN106167485A (zh) 2016-11-30
EP3333166A1 (en) 2018-06-13
WO2013174876A1 (en) 2013-11-28
EP3290414B1 (en) 2019-07-24
IL235761A0 (en) 2015-02-01
BR112014028841A2 (pt) 2017-06-27

Similar Documents

Publication Publication Date Title
MX355409B (es) Proceso para la preparacion de n- [5- (3,5-difluoro-bencil) -1h-indazol-3-il] -4- (4-metil-piperazin-1-il) -2- (tetrahidro-piran-4-ilamino) -benzamida.
MX379558B (es) 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.
EA201492092A1 (ru) Соединения и композиции для ингибирования активности abl1, abl2 и bcr-abl1
MX342924B (es) Nuevos compuestos disustituidos de 3,4-diamino-3-ciclobuteno-1,2-d iona para uso en el tratamiento de patologias mediadas por quimiocinas.
MX2014004858A (es) Compuestos de 3,4-diamino-3-ciclobuten-1,2-diona disustituidos utiles en el tratamiento de patologias mediadas por quimiocinas.
SA515360007B1 (ar) مركبات عطرية غير متجانسة كمثبطات بروتونز تيروسين كيناز ( btk)
MY198246A (en) Novel Ferroportin Inhibitors
NZ631112A (en) Crystalline bromodomain inhibitors
MX336051B (es) Diarilacetileno hidracido que contiene inhibidores de tirosina quinasa.
EA201492005A1 (ru) Бензамидные производные для ингибирования активности abl1, abl2 и bcr-abl1
EA026385B9 (ru) Конденсированные гетероциклические соединения в качестве модуляторов ионных каналов
MY167791A (en) 2-(1,2,3-triazol-2-yl)benzamide and 3-(1,2,3-triazol-2-yl)picolinamide derivatives as orexin receptor antagonists
MX2013012652A (es) Derivados de n-[(1h-pirazol-1-il)aril]-1h-indol o 1h-indazol-3-carboxamida, su preparacion y su uso como antagonistas p2y12.
PH12013500301A1 (en) Oxadiazole inhibitors of leukotriene production
PH12014502586A1 (en) Novel ring-substituted n-pyridinyl amides as kinase inhibitors
PH12015500746A1 (en) Benzamides
EA201791321A1 (ru) Составы ингибитора lfa-1
EA201790253A1 (ru) Ингибиторы альдостеронсинтазы
MX2013014577A (es) Compuestos de heteroarilo como ligandos del receptor 5-ht4.
MX2015000179A (es) Composiciones y formas de dosificacion de itraconazol y metodos de uso de las mismas.
EA201300389A1 (ru) Оксадиазольные ингибиторы продуцирования лейкотриена
MX2015008733A (es) Derivados de 1,2,3-triazol-4-amina para el tratamiento de enfermedades y transtornos relacionados con receptores sigma.
MD20140122A2 (ro) Procedee de producere a clorhidratului de anamorelin cu un conţinut controlat de clorură
MX2013006670A (es) Derivado de 2-carboxamida-4-piperazinil-benzofurano.
MX2014003455A (es) Derivados de metanosulfonamida sustituidos con arilo o n-heteroarilo como ligandos de receptor vanilloide.

Legal Events

Date Code Title Description
FG Grant or registration