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
anilino
carboxamide
methoxy
dihydropyrimido
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CN201580017365.8A
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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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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic 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
    • C07D471/12—Heterocyclic 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
    • C07D471/14—Ortho-condensed systems
    • 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
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • C07D471/00—Heterocyclic 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
    • C07D471/22—Heterocyclic 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)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (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
EP14163734.8 2014-04-07
EP14163734 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) US9856258B2 (https=)
EP (1) EP3129374B1 (https=)
JP (1) JP6518690B2 (https=)
KR (1) KR102432420B1 (https=)
CN (1) CN106132963B (https=)
AU (1) AU2015243694B2 (https=)
BR (1) BR112016022342B1 (https=)
CA (1) CA2944610C (https=)
DK (1) DK3129374T3 (https=)
ES (1) ES2716165T3 (https=)
HU (1) HUE043108T2 (https=)
MX (1) MX368767B (https=)
PL (1) PL3129374T3 (https=)
PT (1) PT3129374T (https=)
RU (1) RU2692479C2 (https=)
WO (1) WO2015155042A1 (https=)

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9856258B2 (en) * 2014-04-07 2018-01-02 Netherlands Translational Research Center B.V. (5,6-dihydro)pyrimido[4,5-E]indolizines
FI3283642T3 (fi) 2015-04-17 2024-01-11 Crossfire Oncology Holding B V Prognostisia biomarkkereita ttk-inhibiittorikemoterapiaan
DK3416964T3 (da) * 2016-02-19 2021-02-22 Phoenix Molecular Designs 6-Oxo-N-(1-(benzyl)-1H-pyrazol-4-YL)-6,7,8,9-tetrahydropyrido[3',2':4,5]pyrrolo[1,2-A]pyrazin-2-carboxamid-derivater som P90 ribosomal S6 kinase- (RSK-) hæmmere til behandling af cancer
EA202092441A1 (ru) 2016-06-07 2021-05-21 Джакобио Фармасьютикалс Ко., Лтд. Новые гетероциклические производные, применимые в качестве ингибиторов shp2
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
KR20240026521A (ko) 2017-03-23 2024-02-28 자코바이오 파마슈티칼스 컴퍼니 리미티드 Shp2 억제제로서 유용한 신규한 헤테로환형 유도체
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
AU2022408915A1 (en) * 2021-12-15 2024-06-27 Sillajen, Inc. Methods of treating neoplastic diseases
KR20240107189A (ko) * 2021-12-15 2024-07-08 신라젠(주) 신생물성 질환 치료에 사용하기 위한 약제학적 병용물
MX2024007452A (es) * 2021-12-15 2024-07-09 Sillajen Inc Composiciones farmaceuticas que comprenden beta-ciclodextrinas modificadas.
WO2023167549A1 (en) * 2022-03-04 2023-09-07 Sillajen, Inc. Pharmaceutical combinations for use in the treatment of neoplastic diseases

Citations (2)

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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

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IL160915A0 (en) * 2001-09-19 2004-08-31 Aventis Pharma Sa Indolizines inhibiting kinase proteins
PT1636236E (pt) 2003-05-22 2013-12-16 Nerviano Medical Sciences Srl Derivados de pirazol-quinazolina, processo para sua preparação e sua utilização como inibidores de cinase
EP2118102B1 (en) 2006-11-28 2013-06-12 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
EP2424868B1 (en) 2009-04-29 2018-01-10 Nerviano Medical Sciences S.r.l. Cdk inhibitor salts
JP5851990B2 (ja) 2009-07-29 2016-02-03 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 Ｐｌｋ阻害剤の塩
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
CN103415518A (zh) * 2010-12-17 2013-11-27 拜耳知识产权有限责任公司 在过度增殖性病症的治疗中用作mps-1和tkk抑制剂的咪唑并吡嗪
JP6523267B2 (ja) 2013-06-24 2019-05-29 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツングＭｅｒｃｋ Ｐａｔｅｎｔ Ｇｅｓｅｌｌｓｃｈａｆｔ ｍｉｔ ｂｅｓｃｈｒａｅｎｋｔｅｒ Ｈａｆｔｕｎｇ Ｆｓｈｒの調節剤としてのイミダゾール化合物及びその使用
US9856258B2 (en) * 2014-04-07 2018-01-02 Netherlands Translational Research Center B.V. (5,6-dihydro)pyrimido[4,5-E]indolizines

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

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