RU2621732C2 - Замещенные пиримидинилпирролы, активные в качестве ингибиторов киназы - Google Patents

Замещенные пиримидинилпирролы, активные в качестве ингибиторов киназы Download PDF

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RU2621732C2
RU2621732C2 RU2013151174A RU2013151174A RU2621732C2 RU 2621732 C2 RU2621732 C2 RU 2621732C2 RU 2013151174 A RU2013151174 A RU 2013151174A RU 2013151174 A RU2013151174 A RU 2013151174A RU 2621732 C2 RU2621732 C2 RU 2621732C2
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formula
compound
pyrrole
carboxamide
aminopyrimidin
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RU2013151174A
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Russian (ru)
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RU2013151174A (ru
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Мария Габриелла Браска
Тициано Бандьера
Джей Аарон Бертран
Паола НЬОККИ
Данило МИРИЦЦИ
Марчелла Нези
Акилле Панцери
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НЕРВИАНО МЕДИКАЛ САЙЕНСИЗ С.р.л.
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F5/00Compounds containing elements of Groups 3 or 13 of the Periodic Table
    • C07F5/02Boron compounds
    • C07F5/025Boronic and borinic acid compounds
    • 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F5/00Compounds containing elements of Groups 3 or 13 of the Periodic Table
    • C07F5/02Boron compounds

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
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  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
RU2013151174A 2011-04-19 2012-04-05 Замещенные пиримидинилпирролы, активные в качестве ингибиторов киназы RU2621732C2 (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP11162960.6 2011-04-19
EP11162960 2011-04-19
PCT/EP2012/056266 WO2012143248A1 (en) 2011-04-19 2012-04-05 Substituted pyrimidinyl-pyrroles active as kinase inhibitors

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RU2013151174A RU2013151174A (ru) 2015-05-27
RU2621732C2 true RU2621732C2 (ru) 2017-06-07

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US (1) US9283224B2 (enExample)
EP (1) EP2699564B1 (enExample)
JP (1) JP5970537B2 (enExample)
CN (1) CN103502241B (enExample)
BR (1) BR112013026137B1 (enExample)
ES (1) ES2616458T3 (enExample)
RU (1) RU2621732C2 (enExample)
WO (1) WO2012143248A1 (enExample)

Families Citing this family (35)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AR077468A1 (es) 2009-07-09 2011-08-31 Array Biopharma Inc Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa
JP6219922B2 (ja) * 2012-03-30 2017-10-25 ダウ アグロサイエンシィズ エルエルシー 3−置換−6−トリフルオロメチルピリジンを調製する方法およびハロゲン化6−トリクロロメチルピリジンを使用する方法
US20160237158A1 (en) * 2013-09-23 2016-08-18 Institut National De La Santé Et Da La Recherche Médicale (Inserm) Methods and Compositions for Targeting Tumor Microenvironment and for preventing Metastasis
PT3322706T (pt) 2015-07-16 2021-03-08 Array Biopharma Inc Compostos de pirazolo[1,5-a]piridina substituídos como inibidores da quinase do ret
TN2019000271A1 (en) 2015-10-26 2021-01-07 Univ Colorado Regents Point mutations in trk inhibitor-resistant cancer and methods relating to the same
US10045991B2 (en) 2016-04-04 2018-08-14 Loxo Oncology, Inc. Methods of treating pediatric cancers
IL304018A (en) 2016-04-04 2023-08-01 Loxo Oncology Inc Liquid formulations of (S)-N-(5-((R)-2-(5,2-difluorophenyl)-pyrrolidine-1-yl)-pyrazolo[5,1-A]pyrimidin-3-yl)-3 -hydroxypyrrolidine-1-carboxamide
TN2019000332A1 (en) 2016-04-04 2021-05-07 Loxo Oncology Inc Methods of treating pediatric cancers
ES2952056T3 (es) 2016-05-18 2023-10-26 Loxo Oncology Inc Preparación de (s)-n-(5-((r)-2-(2,5-difluorofenil)pirrolidin-1-il)pirazolo[1,5-a]pirimidin-3-il)-3-hidroxipirrolidina-1-carboxamida
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
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
GB201706806D0 (en) 2017-04-28 2017-06-14 Sentinel Oncology Ltd Pharmaceutical compounds
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
CN107970438B (zh) * 2017-11-28 2021-08-13 镇江市中西医结合医院(镇江市第二人民医院) 一种神经再生凝胶及其制备方法和应用
WO2019143977A1 (en) 2018-01-18 2019-07-25 Array Biopharma Inc. Substituted pyrrolo[2,3-d]pyrimidines compounds 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
JP6997876B2 (ja) 2018-01-18 2022-02-04 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置換ピラゾリル[4,3-c]ピリジン化合物
JP7286755B2 (ja) 2018-07-31 2023-06-05 ロクソ オンコロジー, インコーポレイテッド (s)-5-アミノ-3-(4-((5-フルオロ-2-メトキシベンズアミド)メチル)フェニル)-1-(1,1,1-トリフルオロプロパン-2-イル)-1h-ピラゾール-4-カルボキサミドの噴霧乾燥分散体および製剤
CA3111984A1 (en) 2018-09-10 2020-03-19 Array Biopharma Inc. Fused heterocyclic compounds as ret kinase inhibitors
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
US20220372135A1 (en) 2019-09-27 2022-11-24 Disc Medicine, Inc. Methods for treating myelofibrosis and related conditions
WO2021113492A1 (en) 2019-12-06 2021-06-10 Schrödinger, Inc. Cyclic compounds and methods of using same
MX2022007171A (es) 2019-12-27 2022-08-22 Schroedinger Inc Compuestos cíclicos y métodos de uso de estos.
CA3177830A1 (en) 2020-05-13 2021-11-18 Maria BECONI Anti-hemojuvelin (hjv) antibodies for treating myelofibrosis
CN116490507A (zh) 2020-09-10 2023-07-25 薛定谔公司 用于治疗癌症的杂环包缩合cdc7激酶抑制剂
CN116323595B (zh) * 2020-09-23 2025-08-19 内尔维亚诺医疗科学公司 作为激酶抑制剂的吡唑基-嘧啶衍生物
US20240148732A1 (en) 2021-01-26 2024-05-09 Schrödinger, Inc. Tricyclic compounds useful in the treatment of cancer, autoimmune and inflammatory disorders
TW202300150A (zh) 2021-03-18 2023-01-01 美商薛定諤公司 環狀化合物及其使用方法
WO2025059027A1 (en) 2023-09-11 2025-03-20 Schrödinger, Inc. Cyclopenta[e]pyrazolo[1,5-a]pyrimidine derivatives as malt1 inhibitors

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20040204386A1 (en) * 2002-10-17 2004-10-14 Cell Therapeutics, Inc. Pyrimidines and uses thereof
WO2007110344A1 (en) * 2006-03-27 2007-10-04 Nerviano Medical Sciences S.R.L. Pyridyl- and pyrimidinyl-substituted pyrrole-, thiophene- and furane-derivatives as kinase inhibitors
RU2006112046A (ru) * 2003-09-13 2007-11-10 Астразенека Аб (Se) Производные пиррола с антибактериальным действием
WO2009133170A1 (en) * 2008-04-30 2009-11-05 Nerviano Medical Sciences S.R.L. Process for the preparation of 5-(2-amino-pyrimidin-4-yl)-2-aryl-1h-pyrrole-3-carboxamides

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101421250A (zh) * 2006-01-30 2009-04-29 埃克塞里艾克西斯公司 作为jak-2调节剂的4-芳基-2-氨基-嘧啶或4-芳基-2-氨基烷基-嘧啶及包含它们的药物组合物
WO2009046416A1 (en) * 2007-10-05 2009-04-09 Targegen Inc. Anilinopyrimidines as jak kinase inhibitors
EP2417125B1 (en) * 2009-03-27 2015-09-09 Nerviano Medical Sciences S.r.l. N-aryl-2-(2-arylaminopyrimidin-4-yl)pyrrol-4-carboxamide derivatives as mps1 kinase inhibitors
CA2779785C (en) * 2009-11-04 2017-09-12 Nerviano Medical Sciences S.R.L. Process for the preparation of 5-(2-amino-pyrimidin-4-yl)-2-aryl-1h-pyrrole-3-carboxamides
CN102666528B (zh) * 2009-11-11 2014-04-16 内尔维阿诺医学科学有限公司 晶体cdc7 抑制剂盐
EP2736514B1 (en) * 2011-07-28 2017-10-18 Nerviano Medical Sciences S.r.l. Alkynyl substituted pyrimidinyl-pyrroles active as kinases inhibitors

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20040204386A1 (en) * 2002-10-17 2004-10-14 Cell Therapeutics, Inc. Pyrimidines and uses thereof
RU2006112046A (ru) * 2003-09-13 2007-11-10 Астразенека Аб (Se) Производные пиррола с антибактериальным действием
WO2007110344A1 (en) * 2006-03-27 2007-10-04 Nerviano Medical Sciences S.R.L. Pyridyl- and pyrimidinyl-substituted pyrrole-, thiophene- and furane-derivatives as kinase inhibitors
EA015126B1 (ru) * 2006-03-27 2011-06-30 НЕРВИАНО МЕДИКАЛ САЙЕНСИЗ С.р.л. Пиридил- и пиримидинилзамещённые производные пиррола, тиофена и фурана в качестве ингибиторов киназ
WO2009133170A1 (en) * 2008-04-30 2009-11-05 Nerviano Medical Sciences S.R.L. Process for the preparation of 5-(2-amino-pyrimidin-4-yl)-2-aryl-1h-pyrrole-3-carboxamides
EA019036B1 (ru) * 2008-04-30 2013-12-30 НЕРВИАНО МЕДИКАЛ САЙЕНСИЗ С.р.л. Способ получения 5-(2-аминопиримидин-4-ил)-2-арил-1н-пиррол-3-карбоксамидов

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
DATABASE REGISTRY, CHEMICAL ABSTRACTS SERVICE, COLUMBIO OHIO, US: abstracts REGISTRY: (Entered STN: 04 Nov 2004, RN 774608-41-2 CA)- STN: 13 Jul 2009, RN 1162257-08-0 CA); (Entered STN: 12 Nov 2012, RN 1403679-84-4 (CA INDEX NAME). *

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HK1187905A1 (zh) 2014-04-17
RU2013151174A (ru) 2015-05-27
CN103502241B (zh) 2016-03-23
CN103502241A (zh) 2014-01-08
EP2699564B1 (en) 2016-12-14
BR112013026137A8 (pt) 2018-01-30
US9283224B2 (en) 2016-03-15
EP2699564A1 (en) 2014-02-26
JP5970537B2 (ja) 2016-08-17
ES2616458T3 (es) 2017-06-13
BR112013026137B1 (pt) 2020-12-01
WO2012143248A1 (en) 2012-10-26
JP2014516360A (ja) 2014-07-10
BR112013026137A2 (pt) 2017-10-24
US20140155421A1 (en) 2014-06-05

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