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

Замещенные пиримидинилпирролы, активные в качестве ингибиторов киназы Download PDF

Info

Publication number
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
Authority
RU
Russia
Prior art keywords
formula
compound
pyrrole
carboxamide
aminopyrimidin
Prior art date
Application number
RU2013151174A
Other languages
English (en)
Russian (ru)
Other versions
RU2013151174A (ru
Inventor
Мария Габриелла Браска
Тициано Бандьера
Джей Аарон Бертран
Паола НЬОККИ
Данило МИРИЦЦИ
Марчелла Нези
Акилле Панцери
Original Assignee
НЕРВИАНО МЕДИКАЛ САЙЕНСИЗ С.р.л.
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 НЕРВИАНО МЕДИКАЛ САЙЕНСИЗ С.р.л. filed Critical НЕРВИАНО МЕДИКАЛ САЙЕНСИЗ С.р.л.
Publication of RU2013151174A publication Critical patent/RU2013151174A/ru
Application granted granted Critical
Publication of RU2621732C2 publication Critical patent/RU2621732C2/ru

Links

Images

Classifications

    • 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

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)
  • 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
EP11162960.6 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

Publications (2)

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

Family

ID=45928917

Family Applications (1)

Application Number Title Priority Date Filing Date
RU2013151174A RU2621732C2 (ru) 2011-04-19 2012-04-05 Замещенные пиримидинилпирролы, активные в качестве ингибиторов киназы

Country Status (8)

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

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
MX354136B (es) 2012-03-30 2018-02-14 Dow Agrosciences Llc Metodos para preparar 3-sustituido. 6-trifluorometil piridinas y metodos para la utilizacion de 6-triclorometil piridinas halogenadas.
EP3049110A2 (en) * 2013-09-23 2016-08-03 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods and compositions for targeting tumor microenvironment and for preventing metastasis
DK3322706T3 (da) 2015-07-16 2021-02-01 Array Biopharma Inc Substituerede pyrazolo[1,5-a]pyridin-forbindelser som ret-kinaseinhibitorer
JP2018534296A (ja) 2015-10-26 2018-11-22 ロクソ オンコロジー, インコーポレイテッドLoxo Oncology, Inc. Trk阻害薬耐性がんにおける点変異およびそれに関連する方法
US10045991B2 (en) 2016-04-04 2018-08-14 Loxo Oncology, Inc. Methods of treating pediatric cancers
MX386416B (es) 2016-04-04 2025-03-18 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.
RS65988B1 (sr) 2016-04-04 2024-10-31 Loxo Oncology Inc Postupak lečenja pedijatrijskih karcinoma
HUE063877T2 (hu) 2016-05-18 2024-02-28 Loxo Oncology Inc (S)-N-(5-((R)-2-(2,5-dlfluorofenil)pirolidin-1-il)plrazolo[1,5-A]pirimidin-3-il) -3-hidroxipirolidin-1-karboxamid elõállítása
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
CA3049136C (en) 2017-01-18 2022-06-14 Array Biopharma Inc. Substituted pyrazolo[1,5-a]pyrazine compounds as ret kinase inhibitors
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
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
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
WO2019143994A1 (en) 2018-01-18 2019-07-25 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
KR102545594B1 (ko) 2018-07-31 2023-06-21 록쏘 온콜로지, 인코포레이티드 (s)-5-아미노-3-(4-((5-플루오로-2-메톡시벤즈아미도)메틸)페닐)-1-(1,1,1-트리플루오로프로판-2-일)-1h-피라졸-4-카르복스아미드의 분무-건조된 분산물 및 제제
CN112996794A (zh) 2018-09-10 2021-06-18 阿雷生物药品公司 作为ret激酶抑制剂的稠合杂环化合物
EP3898626A1 (en) 2018-12-19 2021-10-27 Array Biopharma, Inc. Substituted pyrazolo[1,5-a]pyridine compounds as inhibitors of fgfr tyrosine kinases
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
KR20220088699A (ko) 2019-09-27 2022-06-28 디스크 메디슨, 인크. 골수섬유증 및 관련 상태의 치료 방법
WO2021113492A1 (en) 2019-12-06 2021-06-10 Schrödinger, Inc. Cyclic compounds and methods of using same
WO2021134004A1 (en) 2019-12-27 2021-07-01 Schrodinger, Inc. Cyclic compounds and methods of using same
KR20230012539A (ko) 2020-05-13 2023-01-26 디스크 메디슨, 인크. 골수섬유증을 치료하기 위한 항-헤모주벨린 (hjv) 항체
JP2023541047A (ja) 2020-09-10 2023-09-27 シュレーディンガー, インコーポレイテッド がんの治療のための複素環式ペリ縮環cdc7キナーゼ阻害剤
EP4217354A1 (en) * 2020-09-23 2023-08-02 Nerviano Medical Sciences S.r.l. Pyrazolyl-pyrimidine derivatives as kinase inhibitors
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
US8772280B2 (en) * 2009-03-27 2014-07-08 Nerviano Medical Sciences S.R.L. N-aryl-2-(2-arylaminopyrimidin-4-yl)pyrrol-4-carboxamide derivatives as MPS1 kinase inhibitors
US8592583B2 (en) * 2009-11-04 2013-11-26 Nerviano Medical Sciences Process for the preparation of 5-(2-amino-pyrimidin-4-yl)-2-aryl-1H-pyrrole-3-carboxamides
US8658662B2 (en) * 2009-11-11 2014-02-25 Nerviano Medical Sciences S.R.L. Crystalline CDC7 inhibitor salts
JP6016915B2 (ja) * 2011-07-28 2016-10-26 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アルキニル置換ピリミジニルピロール

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). *

Also Published As

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

Similar Documents

Publication Publication Date Title
RU2621732C2 (ru) Замещенные пиримидинилпирролы, активные в качестве ингибиторов киназы
RU2666538C2 (ru) Замещенные пирролы, активные в качестве ингибиторов киназ
JP6016915B2 (ja) キナーゼ阻害剤として活性なアルキニル置換ピリミジニルピロール
JP5976778B2 (ja) キナーゼ阻害剤としてのピラゾリル−ピリミジン誘導体
TW201925187A (zh) 經碸吡啶烷基醯胺取代之雜芳基化合物
CN104884454A (zh) 用作IL-12、IL-23和/或IFNα应答调节剂的酰胺取代的杂环化合物
HK1187905B (en) Substituted pyrimidinyl-pyrroles active as kinase inhibitors
HK1208459B (en) Substituted pyrroles active as kinases inhibitors
HK1235064A1 (en) Indole carboxamides compounds useful as kinase inhibitors