CN106132963B - (5,6-二氢)嘧啶并[4,5-e]吲嗪 - Google Patents

(5,6-二氢)嘧啶并[4,5-e]吲嗪 Download PDF

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Publication number
CN106132963B
CN106132963B CN201580017365.8A CN201580017365A CN106132963B CN 106132963 B CN106132963 B CN 106132963B CN 201580017365 A CN201580017365 A CN 201580017365A CN 106132963 B CN106132963 B CN 106132963B
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China
Prior art keywords
indolizine
carboxamide
anilino
dihydropyrimido
methoxy
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English (en)
Chinese (zh)
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CN106132963A (zh
Inventor
A·P·A·德曼
R·C·比杰斯曼
J·G·斯特恩伯格
J·C·M·乌特德哈格
J·J·P·德维特
G·J·R·扎曼
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SILLAJEN Inc
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Netherlands Translational Research Center BV
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/12Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains three hetero rings
    • C07D471/14Ortho-condensed systems
    • 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
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/22Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed systems contains four or more hetero rings

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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)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CN201580017365.8A 2014-04-07 2015-03-30 (5,6-二氢)嘧啶并[4,5-e]吲嗪 Active CN106132963B (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
EP14163734 2014-04-07
EP14163734.8 2014-04-07
EP15153207 2015-01-30
EP15153207.4 2015-01-30
PCT/EP2015/056839 WO2015155042A1 (en) 2014-04-07 2015-03-30 (5,6-dihydro)pyrimido[4,5-e]indolizines

Publications (2)

Publication Number Publication Date
CN106132963A CN106132963A (zh) 2016-11-16
CN106132963B true CN106132963B (zh) 2019-08-06

Family

ID=52774240

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201580017365.8A Active CN106132963B (zh) 2014-04-07 2015-03-30 (5,6-二氢)嘧啶并[4,5-e]吲嗪

Country Status (16)

Country Link
US (3) USRE48974E1 (enExample)
EP (1) EP3129374B1 (enExample)
JP (1) JP6518690B2 (enExample)
KR (1) KR102432420B1 (enExample)
CN (1) CN106132963B (enExample)
AU (1) AU2015243694B2 (enExample)
BR (1) BR112016022342B1 (enExample)
CA (1) CA2944610C (enExample)
DK (1) DK3129374T3 (enExample)
ES (1) ES2716165T3 (enExample)
HU (1) HUE043108T2 (enExample)
MX (1) MX368767B (enExample)
PL (1) PL3129374T3 (enExample)
PT (1) PT3129374T (enExample)
RU (1) RU2692479C2 (enExample)
WO (1) WO2015155042A1 (enExample)

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MX368767B (es) * 2014-04-07 2019-10-15 Netherlands Translational Res Center B V (5,6-dihidro)pirimido[4,5-e]indolizinas.
JP6993233B2 (ja) * 2015-04-17 2022-01-13 ネザーランズ トランスレーショナル リサーチ センター ビー.ブイ. Ttk阻害剤化学療法の為の予後バイオマーカー
PL3416964T3 (pl) * 2016-02-19 2021-10-18 Phoenix Molecular Designs Pochodne 6-okso-n-(1-(benzylo)-1h-pirazol-4-ilo)-6,7,8,9-tetrahydropirydo[3’,2’:4,5]pirolo[1,2-a]pirazyno-2-karboksyamidu jako inhibitory kinazy rybosomalnej s6 p90 (rsk) do leczenia nowotworu złośliwego
HUE057838T2 (hu) 2016-06-07 2022-06-28 Jacobio Pharmaceuticals Co Ltd SHP2 inhibitorokként hasznos új heterociklusos származékok
CN106551938B (zh) * 2016-11-26 2017-11-24 广东安诺药业股份有限公司 一种治疗非酒精性脂肪肝的药物及其应用
TWI664175B (zh) 2017-03-23 2019-07-01 大陸商北京加科思新藥研發有限公司 用於作為shp2抑制劑之新穎雜環衍生物
CN112839935A (zh) 2018-09-26 2021-05-25 北京加科思新药研发有限公司 可用作shp2抑制剂的新型杂环衍生物
US12378245B2 (en) 2019-02-11 2025-08-05 Phoenix Molecular Designs Crystalline forms of an RSK inhibitor
US20250049926A1 (en) * 2021-12-15 2025-02-13 Sillajen, Inc. Pharmaceutical compositions comprising modified betacyclodextrins
KR20240107189A (ko) * 2021-12-15 2024-07-08 신라젠(주) 신생물성 질환 치료에 사용하기 위한 약제학적 병용물
KR20240107329A (ko) * 2021-12-15 2024-07-09 신라젠(주) 신생물성 질환을 치료하는 방법
KR20240144991A (ko) * 2022-03-04 2024-10-04 신라젠(주) 신생물성 질환 치료에 사용하기 위한 약제학적 병용물

Citations (2)

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Publication number Priority date Publication date Assignee Title
WO2009156315A1 (en) * 2008-06-26 2009-12-30 Nerviano Medical Sciences S.R.L. Pyrazolo-quinazolines
WO2012101032A1 (en) * 2011-01-26 2012-08-02 Nerviano Medical Sciences S.R.L. Tricyclic pyrrolo derivatives, process for their preparation and their use as kinase inhibitors

Family Cites Families (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2002337142B2 (en) * 2001-09-19 2007-10-11 Aventis Pharma S.A. Indolizines as kinase protein inhibitors
KR101084871B1 (ko) 2003-05-22 2011-11-21 네르비아노 메디칼 사이언시스 에스.알.엘. 피라졸로-퀴나졸린 유도체, 그의 제조 방법 및 상기유도체의 키나제 저해제로서의 용도
US8207180B2 (en) 2006-11-28 2012-06-26 Nerviano Medical Sciences S.R.L. Tricyclic indoles and (4,5-dihydro) indoles
WO2010111406A2 (en) 2009-03-24 2010-09-30 Myriad Pharmaceuticals, Inc. Compounds and therapeutic uses thereof
ES2660146T3 (es) 2009-04-29 2018-03-21 Nerviano Medical Sciences S.R.L. Sales del inhibidor de cdk
ES2553114T3 (es) 2009-07-29 2015-12-04 Nerviano Medical Sciences S.R.L. Sales de inhibidor de plk
TW201107329A (en) 2009-07-30 2011-03-01 Oncotherapy Science Inc Fused imidazole derivative having ttk inhibitory action
EP2343297A1 (en) 2009-11-30 2011-07-13 Bayer Schering Pharma AG Triazolopyridines
WO2012080229A1 (en) 2010-12-17 2012-06-21 Bayer Pharma Aktiengesellschaft Imidazopyrazines for use as mps-1 and tkk inhibitors in the treatment hyperproliferative disorders
ES2657979T3 (es) 2013-06-24 2018-03-07 Merck Patent Gmbh Compuestos de imidazol como moduladores de FSHR y sus usos
MX368767B (es) * 2014-04-07 2019-10-15 Netherlands Translational Res Center B V (5,6-dihidro)pirimido[4,5-e]indolizinas.

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2009156315A1 (en) * 2008-06-26 2009-12-30 Nerviano Medical Sciences S.R.L. Pyrazolo-quinazolines
WO2012101032A1 (en) * 2011-01-26 2012-08-02 Nerviano Medical Sciences S.R.L. Tricyclic pyrrolo derivatives, process for their preparation and their use as kinase inhibitors

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
"Target Residence Time-Guided Optimization on TTK Kinase Results in Inhibitors with Potent Anti-Proliferative Activity";Joost C.M. Uitdehaag et al.;《Journal of Molecular Biology》;20170521;第429卷;第2211-2230页 *

Also Published As

Publication number Publication date
JP6518690B2 (ja) 2019-05-22
USRE50082E1 (en) 2024-08-20
JP2017510595A (ja) 2017-04-13
EP3129374A1 (en) 2017-02-15
US9856258B2 (en) 2018-01-02
BR112016022342A8 (pt) 2021-07-20
USRE48974E1 (en) 2022-03-15
CA2944610C (en) 2024-01-09
KR20170013866A (ko) 2017-02-07
US20170096432A1 (en) 2017-04-06
WO2015155042A1 (en) 2015-10-15
AU2015243694B2 (en) 2019-01-17
EP3129374B1 (en) 2018-12-19
RU2016141405A3 (enExample) 2018-10-02
CN106132963A (zh) 2016-11-16
ES2716165T3 (es) 2019-06-10
BR112016022342B1 (pt) 2022-10-04
MX2016012997A (es) 2016-12-07
RU2016141405A (ru) 2018-05-07
MX368767B (es) 2019-10-15
CA2944610A1 (en) 2015-10-15
KR102432420B1 (ko) 2022-08-17
DK3129374T3 (en) 2019-04-08
AU2015243694A1 (en) 2016-11-03
PL3129374T3 (pl) 2019-07-31
PT3129374T (pt) 2019-03-25
BR112016022342A2 (pt) 2017-08-15
HUE043108T2 (hu) 2019-07-29
RU2692479C2 (ru) 2019-06-25

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