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

    • 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 or sparfloxacin
    • 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

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 (18)

Country Link
US (3) US9085565B2 (es)
EP (4) EP3581571A1 (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) ES2771100T3 (es)
HK (1) HK1207077A1 (es)
IL (2) IL235761B (es)
MX (1) MX355409B (es)
NZ (2) NZ716487A (es)
PL (2) PL3290414T3 (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
BRPI0814628B1 (pt) * 2007-07-20 2022-04-05 Nerviano Medical Sciences S.R.L. Derivados ativos de indazol substituídos como inibidores da quinase
US8450322B2 (en) 2008-09-22 2013-05-28 Array Biopharma Inc. Substituted imidazo[1,2b]pyridazine compounds as Trk kinase inhibitors
AR074052A1 (es) 2008-10-22 2010-12-22 Array Biopharma Inc Compuestos pirazolo{1,5-a}pirimidina sustituida como inhibidores de trk cinasa
AR077468A1 (es) 2009-07-09 2011-08-31 Array Biopharma Inc Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa
CR20170098A (es) 2010-05-20 2017-07-17 Array Biopharma Inc Compuestos macrociclicos como inhibidores de quinasa trk
AU2013265288B2 (en) * 2012-05-23 2017-12-21 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
EP3628749A1 (en) 2013-07-30 2020-04-01 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
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
AU2016286548B2 (en) * 2015-07-02 2020-12-10 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
CA2992586A1 (en) 2015-07-16 2017-01-19 Array Biopharma, Inc. Substituted pyrazolo[1,5-a]pyridine compounds as ret kinase inhibitors
AU2016344058A1 (en) 2015-10-26 2018-05-17 Array Biopharma Inc. Point mutations in Trk inhibitor-resistant cancer and methods relating to the same
WO2017106492A1 (en) 2015-12-18 2017-06-22 Ignyta, Inc. Combinations for the treatment of cancer
LT3439663T (lt) 2016-04-04 2024-10-10 Loxo Oncology, Inc. Vaikų vėžio gydymo būdai
US10045991B2 (en) 2016-04-04 2018-08-14 Loxo Oncology, Inc. Methods of treating pediatric cancers
RU2751767C2 (ru) 2016-04-04 2021-07-16 Локсо Онколоджи, Инк. Жидкие составы (s)-n-(5-((r)-2-(2,5-дифторфенил)пирролидин-1-ил)пиразоло[1,5-a]пиримидин-3-ил)-3-гидроксипирролидин-1-карбоксамида
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
JP7094228B2 (ja) 2016-05-24 2022-07-01 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 N-[5-(3,5-ジフルオロ-ベンジル)-1h-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドの新規結晶形
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
WO2018130928A1 (en) 2017-01-10 2018-07-19 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
CA3049136C (en) 2017-01-18 2022-06-14 Array Biopharma Inc. Substituted pyrazolo[1,5-a]pyrazine compounds as ret kinase inhibitors
JOP20190213A1 (ar) 2017-03-16 2019-09-16 Array Biopharma Inc مركبات حلقية ضخمة كمثبطات لكيناز ros1
US10398693B2 (en) 2017-07-19 2019-09-03 Ignyta, Inc. Pharmaceutical compositions and dosage forms
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
TW202410896A (zh) 2017-10-10 2024-03-16 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
CN111225662B (zh) 2017-10-17 2022-11-22 伊尼塔公司 药物组合物和剂型
EP3700576A1 (en) 2017-10-26 2020-09-02 Array Biopharma Inc. Formulations of a macrocyclic trk kinase inhibitor
CN111630054B (zh) 2018-01-18 2023-05-09 奥瑞生物药品公司 作为RET激酶抑制剂的取代的吡唑并[3,4-d]嘧啶化合物
US11472802B2 (en) 2018-01-18 2022-10-18 Array Biopharma Inc. Substituted pyrazolyl[4,3-c]pyridine compounds as RET kinase inhibitors
CN111971286B (zh) 2018-01-18 2023-04-14 阿雷生物药品公司 作为RET激酶抑制剂的取代的吡咯并[2,3-d]嘧啶化合物
MA52218A (fr) 2018-03-29 2021-02-17 Loxo Oncology Inc Traitement de cancers associés à trk
CN113194928A (zh) 2018-07-31 2021-07-30 罗索肿瘤学公司 (s)-5-氨基-3-(4-((5-氟-2-甲氧基苯甲酰胺基)甲基)苯基)-1-(1,1,1-三氟丙-2-基)-1h-吡唑-4-甲酰胺的喷雾干燥的分散体和制剂
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
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
JP7523521B2 (ja) * 2019-07-31 2024-07-26 エフ・ホフマン-ラ・ロシュ・アクチェンゲゼルシャフト 新規医薬製剤
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
CN113354626A (zh) * 2020-03-04 2021-09-07 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
CN116669735A (zh) * 2021-02-03 2023-08-29 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
JP5302896B2 (ja) * 2006-12-20 2013-10-02 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 癌治療のためのキナーゼ阻害剤としてのインダゾール誘導体
BRPI0814628B1 (pt) * 2007-07-20 2022-04-05 Nerviano Medical Sciences S.R.L. Derivados ativos de indazol substituídos como inibidores da quinase
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
AU2013265288B2 (en) 2012-05-23 2017-12-21 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

Also Published As

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

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.
MX2018014298A (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
EA201491824A1 (ru) Производные бензамида для ингибирования активности abl1, abl2 и bcr-abl1
SA515360007B1 (ar) مركبات عطرية غير متجانسة كمثبطات بروتونز تيروسين كيناز ( btk)
EA201690752A1 (ru) Ингибиторы g12c kras
MX2014004858A (es) Compuestos de 3,4-diamino-3-ciclobuten-1,2-diona disustituidos utiles en el tratamiento de patologias mediadas por quimiocinas.
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.
NZ631112A (en) Crystalline bromodomain inhibitors
EA201492005A1 (ru) Бензамидные производные для ингибирования активности abl1, abl2 и bcr-abl1
MX2013008296A (es) Diarilacetileno hidracido que contiene inhibidores de tirosina quinasa.
EA026385B9 (ru) Конденсированные гетероциклические соединения в качестве модуляторов ионных каналов
UA112317C2 (uk) Похідні 2-(1,2,3-триазол-2-іл)бензаміду та 3-(1,2,3-триазол-2-іл)піколінаміду як антагоністи рецептора орексину
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.
PH12015500746A1 (en) Benzamides
UA110128C2 (uk) Індолкарбоксаміди та бензімідазолкарбоксаміди як інсектициди та акарициди
MX337721B (es) Compuestos de heteroarilo como ligandos del receptor 5-ht4.
EA201790253A1 (ru) Ингибиторы альдостеронсинтазы
MX2015008733A (es) Derivados de 1,2,3-triazol-4-amina para el tratamiento de enfermedades y transtornos relacionados con receptores sigma.
MX366829B (es) Composiciones y formas de dosificacion de itraconazol y metodos de uso de las mismas.
MX2015003732A (es) Tratamiento de enfermedad de alzheimer leve y moderada.
EA201300389A1 (ru) Оксадиазольные ингибиторы продуцирования лейкотриена
EA201791321A1 (ru) Составы ингибитора lfa-1
MX2014003455A (es) Derivados de metanosulfonamida sustituidos con arilo o n-heteroarilo como ligandos de receptor vanilloide.
MX2014003584A (es) Derivados de metanosulfonamida sustituidos como ligandos de receptores vaniloides.

Legal Events

Date Code Title Description
FG Grant or registration