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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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic 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
    • C07D403/04—Heterocyclic 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F5/00—Compounds containing elements of Groups 3 or 13 of the Periodic Table
    • C07F5/02—Boron compounds
    • C07F5/025—Boronic and borinic acid compounds
    • 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F5/00—Compounds containing elements of Groups 3 or 13 of the Periodic Table
    • C07F5/02—Boron compounds

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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)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (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 2011-04-19
EP11162960.6 2011-04-19
PCT/EP2012/056266 WO2012143248A1 (en) 2011-04-19 2012-04-05 Substituted pyrimidinyl-pyrroles active as kinase inhibitors

Publications (2)

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

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RU2013151174A RU2621732C2 (ru) 2011-04-19 2012-04-05 Замещенные пиримидинилпирролы, активные в качестве ингибиторов киназы

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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 (36)

* 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
US8785650B2 (en) 2012-03-30 2014-07-22 Dow Agrosciences, Llc. Methods for preparing 3-substituted-6-trifluoromethyl pyridines and methods for using 6-trichloromethyl halogenated pyridines
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
CA2992586A1 (en) 2015-07-16 2017-01-19 Array Biopharma, Inc. Substituted pyrazolo[1,5-a]pyridine compounds as ret kinase inhibitors
EP3368039A1 (en) 2015-10-26 2018-09-05 The Regents of The University of Colorado, A Body Corporate Point mutations in trk inhibitor-resistant cancer and methods relating to the same
UA125026C2 (uk) 2016-04-04 2021-12-29 Локсо Онколоджі, Інк. РІДКІ КОМПОЗИЦІЇ (S)-N-(5-((R)-2-(2,5-ДИФТОРФЕНІЛ)ПІРОЛІДИН-1-ІЛ)ПІРАЗОЛО[1,5-a]ПІРИМІДИН-3-ІЛ)-3-ГІДРОКСИПІРОЛІДИН-1-КАРБОКСАМІДУ
UA125025C2 (uk) 2016-04-04 2021-12-29 Локсо Онколоджі, Інк. Способи лікування дитячих ракових захворювань
MX392604B (es) 2016-05-18 2025-03-24 Array Biopharma Inc Procesos para la preparacion de (s)-n-(5-((r)-2-(2,5-difluorofenil)pirrolidin-1-il)-pirazolo[1,5-a]pirimidin-3-il)-3-hidroxipirrolidin-1-carboxamida y sales del mismo.
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
TWI752098B (zh) 2016-10-10 2022-01-11 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
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
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
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
EP3740491A1 (en) 2018-01-18 2020-11-25 Array Biopharma, Inc. Substituted pyrrolo[2,3-d]pyrimidines compounds as ret kinase inhibitors
EP3740486A1 (en) 2018-01-18 2020-11-25 Array Biopharma, Inc. Substituted pyrazolyl[4,3-c]pyridinecompounds as ret kinase inhibitors
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
CA3108065C (en) 2018-07-31 2025-10-07 Loxo Oncology, Inc. SPRAY-DRIED DISPERSIONS, FORMULATIONS AND POLYMORPHIES OF (S)-5-AMINO-3-(4-((5-FLUORO-2-METHOXYBENZAMIDO)METHYL)PHENYL)(1,1,1-TRIFLUOROPROPANE-2-YL)-1H-PYRAZOLE-4-CARBOXAMIDE
ES2922314T3 (es) 2018-09-10 2022-09-13 Array Biopharma Inc Compuestos heterocíclicos condensados como inhibidores de cinasa RET
US12351571B2 (en) 2018-12-19 2025-07-08 Array Biopharma Inc. Substituted quinoxaline compounds as inhibitors of FGFR tyrosine kinases
WO2020131627A1 (en) 2018-12-19 2020-06-25 Array Biopharma Inc. Substituted pyrazolo[1,5-a]pyridine compounds as inhibitors of fgfr tyrosine kinases
CA3156007A1 (en) 2019-09-27 2021-04-01 Disc Medicine, Inc. METHODS OF TREATING MYELOFIBROSE AND ASSOCIATED CONDITIONS
US20230101747A1 (en) 2019-12-06 2023-03-30 Schrödinger, Inc. Cyclic compounds and methods of using same
IL294214B2 (en) 2019-12-27 2026-04-01 Schrodinger Inc Cyclic compounds and methods of using same
ES3075793T3 (en) 2020-05-13 2026-08-07 Disc Medicine Inc Anti-hemojuvelin (hjv) antibodies for treating myelofibrosis
AU2021273014A1 (en) 2020-05-13 2022-11-17 AbbVie Deutschland GmbH & Co. KG Anti-hemojuvelin (HJV) antibodies for treating anemia of chronic disease
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
US20240285621A1 (en) * 2020-09-23 2024-08-29 Nerviano Medical Sciences S.R.L. Pyrazolyl-pyrimidine derivatives as kinase inhibitors
GB202015187D0 (en) 2020-09-25 2020-11-11 Sentinel Oncology Ltd A pharmaceutical salt
EP4284804A1 (en) 2021-01-26 2023-12-06 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
CN122003418A (zh) 2023-09-11 2026-05-08 薛定谔公司 作为malt1抑制剂的环戊并[e]吡唑并[1,5-a]嘧啶衍生物

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
ES2593630T3 (es) * 2009-11-04 2016-12-12 Nerviano Medical Sciences S.R.L. Proceso para la preparación de 5-(2-amino-pirimidin-4-il)-2-aril-1h-pirrol-3-carboxamidas
EP2499128B1 (en) * 2009-11-11 2015-06-03 Nerviano Medical Sciences S.r.l. Crystalline cdc7 inhibitor salts
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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CN103502241A (zh) 2014-01-08
BR112013026137B1 (pt) 2020-12-01
CN103502241B (zh) 2016-03-23
BR112013026137A8 (pt) 2018-01-30
RU2013151174A (ru) 2015-05-27
WO2012143248A1 (en) 2012-10-26
HK1187905A1 (zh) 2014-04-17
BR112013026137A2 (pt) 2017-10-24
US9283224B2 (en) 2016-03-15
ES2616458T3 (es) 2017-06-13
EP2699564A1 (en) 2014-02-26
EP2699564B1 (en) 2016-12-14
JP2014516360A (ja) 2014-07-10
JP5970537B2 (ja) 2016-08-17
US20140155421A1 (en) 2014-06-05

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