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.

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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

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Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/02Heterocyclic 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
    • C07D405/12Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/4965Non-condensed pyrazines
    • A61K31/497Non-condensed pyrazines containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs

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  • 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)

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 (18)

Country Link
US (3) US9085565B2 (es)
EP (4) EP3581571A1 (es)
JP (1) JP6231556B2 (es)
KR (1) KR102151963B1 (es)
CN (2) CN104395308B (es)
AR (1) AR091138A1 (es)
AU (2) AU2013265288B2 (es)
BR (1) BR112014028841B1 (es)
CA (1) CA2873979C (es)
ES (2) ES2751944T3 (es)
HK (1) HK1207077A1 (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 (46)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SI2176231T1 (sl) * 2007-07-20 2017-01-31 Nerviano Medical Sciences S.R.L. Substituirani indazolni derivati, aktivni kot kinazni inhibitorji
CA2738026C (en) 2008-09-22 2017-01-24 Array Biopharma Inc. Substituted imidazo[1,2b]pyridazine compounds as trk kinase inhibitors
DK3106463T6 (da) 2008-10-22 2020-02-24 Array Biopharma Inc Pyrazolo[1,5-]pyrimidinforbindelse som trk-kinasehæmmer
AR077468A1 (es) 2009-07-09 2011-08-31 Array Biopharma Inc Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa
HUE035337T2 (en) 2010-05-20 2018-05-02 Array Biopharma Inc Macrocyclic compounds as TRK kinase inhibitors
BR112014028841B1 (pt) 2012-05-23 2021-01-12 Nerviano Medical Sciences S.R.L. Formas cristalinas 1 e 2, composição farmacêutica, uso da forma cristalina 1 para o tratamento de um estado de doença tratável pela inibição de alk e processo para a preparação de n-[5-(3,5-difluoro-benzil)-1h-indazol-3-il]-4-(4-metilpiperazin-1-il)-2-(tetra-hidro-piran-4-ilamino)- benzamida
EP3027655B1 (en) 2013-07-30 2019-08-21 Blueprint Medicines Corporation Ntrk2 fusions
US10231965B2 (en) 2014-02-20 2019-03-19 Ignyta, Inc. Molecules for administration to ROS1 mutant cancer cells
DK3699181T3 (da) 2014-11-16 2023-03-20 Array Biopharma Inc Krystallinsk form af (s)-n-(5-((r)-2-(2,5-difluorphenyl)-pyrrolidin-1-yl)-pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidin-1-carboxamidhydrogensulfat
CA2969540C (en) * 2014-12-02 2023-03-21 Ignyta, Inc. Combinations for the treatment of neuroblastoma
EP3227686A4 (en) * 2014-12-03 2018-08-29 Ignyta, Inc. Multiplexed immunohistochemistry assays for diagnosis and treatment of cancer
EA201792679A1 (ru) 2015-06-01 2018-06-29 Локсо Онколоджи, Инк. Способы диагностики и лечения злокачественной опухоли
EP3322706B1 (en) 2015-07-16 2020-11-11 Array Biopharma, Inc. Substituted pyrazolo[1,5-a]pyridine compounds as ret kinase inhibitors
TN2018000138A1 (en) 2015-10-26 2019-10-04 Array Biopharma Inc 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
PE20181888A1 (es) 2016-04-04 2018-12-11 Loxo Oncology Inc Formulaciones liquidas de (s)-n-(5-((r)-2-(2,5-difluorofenil)-pirrolidin-1-il)-pirazolo[1,5-a]pirimidin-3-il)-3-hidroxipirrolidina-1-carboxamida
US10045991B2 (en) 2016-04-04 2018-08-14 Loxo Oncology, Inc. Methods of treating pediatric cancers
MA44612A (fr) 2016-04-04 2019-02-13 Loxo Oncology Inc Méthodes de traitement de cancers pédiatriques
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
PL3464276T3 (pl) * 2016-05-24 2022-04-04 Nerviano Medical Sciences S.R.L. Nowa postać krystaliczna n-[5-(3,5-difluoro-benzylo)-1h-indazol-3-ilo)-4-(4-metylopiperazyn-1-ylo)-2-tetrahydropiran-4-yloamino)-benzamidu
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
AU2018207464B2 (en) * 2017-01-10 2020-05-14 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
WO2018136663A1 (en) 2017-01-18 2018-07-26 Array Biopharma, Inc. Ret inhibitors
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 preparations that include anthraxtinib
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
WO2019077506A1 (en) 2017-10-17 2019-04-25 Ignyta, Inc. PHARMACEUTICAL COMPOSITIONS AND SOLID GALENIC FORMS
WO2019084285A1 (en) 2017-10-26 2019-05-02 Qian Zhao FORMULATIONS OF A MACROCYCLIC TRK KINASE INHIBITOR
CA3087972C (en) 2018-01-18 2023-01-10 Array Biopharma Inc. Substituted pyrazolyl[4,3-c]pyridinecompounds as ret kinase inhibitors
WO2019143991A1 (en) 2018-01-18 2019-07-25 Array Biopharma Inc. SUBSTITUTED PYRAZOLO[3,4-d]PYRIMIDINE COMPOUNDS 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
WO2019191659A1 (en) 2018-03-29 2019-10-03 Loxo Oncology, Inc. Treatment of trk-associated cancers
CA3108065A1 (en) 2018-07-31 2020-02-06 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
US11964988B2 (en) 2018-09-10 2024-04-23 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
CN113490666A (zh) 2018-12-19 2021-10-08 奥瑞生物药品公司 作为fgfr酪氨酸激酶的抑制剂的取代的吡唑并[1,5-a]吡啶化合物
EP4003309A1 (en) 2019-07-31 2022-06-01 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
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
WO2022166647A1 (zh) * 2021-02-03 2022-08-11 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
MX2009006401A (es) * 2006-12-20 2009-06-23 Nerviano Medical Sciences Srl Derivados de indazol como inhibidores de cinasa para el tratamiento del cancer.
SI2176231T1 (sl) * 2007-07-20 2017-01-31 Nerviano Medical Sciences S.R.L. Substituirani indazolni derivati, aktivni kot kinazni inhibitorji
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
BR112014028841B1 (pt) 2012-05-23 2021-01-12 Nerviano Medical Sciences S.R.L. Formas cristalinas 1 e 2, composição farmacêutica, uso da forma cristalina 1 para o tratamento de um estado de doença tratável pela inibição de alk e processo para a preparação de n-[5-(3,5-difluoro-benzil)-1h-indazol-3-il]-4-(4-metilpiperazin-1-il)-2-(tetra-hidro-piran-4-ilamino)- benzamida

Also Published As

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

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