CN105873932B - (6S,9aS)‑N‑苄基‑6‑[(4‑羟基苯基)甲基]‑4,7‑二氧‑8‑({6‑[3‑(哌嗪‑1‑基)氮杂环丁烷‑1‑基]吡啶‑2‑基}甲基)‑2‑(丙‑2‑烯‑1‑基)‑八氢‑1H‑吡嗪并[2,1‑c][1,2,4]三嗪‑1‑甲酰胺化合物 - Google Patents

(6S,9aS)‑N‑苄基‑6‑[(4‑羟基苯基)甲基]‑4,7‑二氧‑8‑({6‑[3‑(哌嗪‑1‑基)氮杂环丁烷‑1‑基]吡啶‑2‑基}甲基)‑2‑(丙‑2‑烯‑1‑基)‑八氢‑1H‑吡嗪并[2,1‑c][1,2,4]三嗪‑1‑甲酰胺化合物 Download PDF

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CN105873932B
CN105873932B CN201480067017.7A CN201480067017A CN105873932B CN 105873932 B CN105873932 B CN 105873932B CN 201480067017 A CN201480067017 A CN 201480067017A CN 105873932 B CN105873932 B CN 105873932B
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methyl
octahydro
triazine
pyridine
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CN105873932A (zh
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井上谕
山本祐二
矶健太郎
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Sanitary Material R&d Management Co ltd
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-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
    • A61K31/53Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/66Phosphorus compounds
    • A61K31/661Phosphorus acids or esters thereof not having P—C bonds, e.g. fosfosal, dichlorvos, malathion or mevinphos
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • 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
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • 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
    • C07D403/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 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
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/06Phosphorus compounds without P—C bonds
    • C07F9/08Esters of oxyacids of phosphorus
    • C07F9/09Esters of phosphoric acids
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6561Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed 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)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (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)
  • Pulmonology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
CN201480067017.7A 2013-12-25 2014-12-22 (6S,9aS)‑N‑苄基‑6‑[(4‑羟基苯基)甲基]‑4,7‑二氧‑8‑({6‑[3‑(哌嗪‑1‑基)氮杂环丁烷‑1‑基]吡啶‑2‑基}甲基)‑2‑(丙‑2‑烯‑1‑基)‑八氢‑1H‑吡嗪并[2,1‑c][1,2,4]三嗪‑1‑甲酰胺化合物 Active CN105873932B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
JP2013-267687 2013-12-25
JP2013267687 2013-12-25
PCT/JP2014/083932 WO2015098853A1 (ja) 2013-12-25 2014-12-22 (6S,9aS)-N-ベンジル-6-[(4-ヒドロキシフェニル)メチル]-4,7-ジオキソ-8-({6-[3-(ピペラジン-1-イル)アゼチジン-1-イル]ピリジン-2-イル}メチル)-2-(プロプ-2-エン-1-イル)-オクタヒドロ-1H-ピラジノ[2,1-c][1,2,4]トリアジン-1-カルボキサミド化合物

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CN105873932A CN105873932A (zh) 2016-08-17
CN105873932B true CN105873932B (zh) 2017-11-24

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JP6038128B2 (ja) 2011-06-03 2016-12-07 エーザイ・アール・アンド・ディー・マネジメント株式会社 レンバチニブ化合物に対する甲状腺癌対象及び腎臓癌対象の反応性を予測及び評価するためのバイオマーカー
PT3524595T (pt) 2014-08-28 2022-09-19 Eisai R&D Man Co Ltd Derivado de quinolina altamente puro e método para produção do mesmo
LT3263106T (lt) 2015-02-25 2024-01-10 Eisai R&D Management Co., Ltd. Chinolino darinių kartumo sumažinimo būdas
KR102662228B1 (ko) 2015-03-04 2024-05-02 머크 샤프 앤드 돔 코포레이션 암을 치료하기 위한 pd-1 길항제 및 vegfr/fgfr/ret 티로신 키나제 억제제의 조합
MX373231B (es) * 2015-06-16 2020-05-08 Eisai R&D Man Co Ltd Agente anticancerigeno.
CA2986999C (en) * 2015-06-23 2023-08-08 Eisai R&D Management Co., Ltd. Crystal of (6s,9as)-n-benzyl-8-({6-[3-(4-ethylpiperazin-1-yl)azetidin-1-yl]pyridin-2-yl}methyl)-6-(2-fluoro-4-hydroxybenzyl)-4,7-dioxo-2-(prop-2-en-1-yl)hexahydro-2h-pyrazino[2,1-c][1,2,4]triazine-1(6h)-carboxamide
US12220398B2 (en) 2015-08-20 2025-02-11 Eisai R&D Management Co., Ltd. Tumor therapeutic agent
CN108084067B (zh) * 2016-11-22 2019-08-30 重庆圣华曦药业股份有限公司 一种立他司特中间体的制备方法
US12303505B2 (en) 2017-02-08 2025-05-20 Eisai R&D Management Co., Ltd. Tumor-treating pharmaceutical composition
RU2019134940A (ru) 2017-05-16 2021-06-16 Эйсай Ар Энд Ди Менеджмент Ко., Лтд. Лечение гепатоцеллюлярной карциномы
EP4051278B1 (en) 2019-10-29 2025-12-17 Eisai R&D Management Co., Ltd. Combination of a pd-1 antagonist, a vegfr/fgfr/ret tyrosine kinase inhibitor and a cbp/beta-catenin inhibitor for treating cancer
US12486275B2 (en) 2020-03-12 2025-12-02 City Of Hope Substituted pyrazino[2,1-c][1,2,4]triazines as Wnt/CBP/catenin signaling pathway inhibitors
AR121544A1 (es) 2020-03-12 2022-06-15 3 2 Pharma Inhibidores de la vía de señalización por cbp / catenina y sus usos
CN117083065A (zh) 2020-10-30 2023-11-17 庆应义塾 肌肉减少症相关疾病等的新颖治疗和预防
US20240352020A1 (en) * 2021-08-26 2024-10-24 3+2 Pharma, Llc Pyrazole-containing cbp/catenin antagonists and uses thereof
MX2024002060A (es) * 2021-09-08 2024-03-01 Eisai R&D Man Co Ltd Composicion farmaceutica para tratar tumores solidos.
CN116262120A (zh) * 2021-12-13 2023-06-16 上海中医药大学 特异性结合TRAF2的试剂在制备Wnt通路抑制剂中的应用
WO2023140369A1 (en) * 2022-01-18 2023-07-27 Prism BioLab Co., Ltd. Phosphoric acid derivatives
EP4473970A4 (en) 2022-03-31 2026-01-21 Eisai R&D Man Co Ltd PHARMACEUTICAL COMPOSITION FOR THE TREATMENT OF TUMORS
CN115784934A (zh) * 2022-11-22 2023-03-14 上海吉奉生物科技有限公司 一种酪氨酸衍生物的合成方法
AU2023439518A1 (en) 2023-04-06 2025-08-28 Eisai R&D Management Co., Ltd. Pharmaceutical composition for treating tumors
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LT3088401T (lt) 2019-07-25
EP3088401A4 (en) 2017-06-28
AU2014371148B2 (en) 2018-08-09
IL245961A0 (en) 2016-08-02
JPWO2015098853A1 (ja) 2017-03-23
SMT201900306T1 (it) 2019-07-11
AR098908A1 (es) 2016-06-22
WO2015098853A1 (ja) 2015-07-02
US20150175615A1 (en) 2015-06-25
SG11201604496YA (en) 2016-07-28
BR112016013572B1 (pt) 2023-03-21
RU2016122867A (ru) 2018-02-01
CN105873932A (zh) 2016-08-17
TWI681961B (zh) 2020-01-11
DK3088401T3 (da) 2019-06-03
KR102307053B1 (ko) 2021-10-01
CA2932435C (en) 2021-08-17
PT3088401T (pt) 2019-06-12
MX2016007705A (es) 2017-01-11
MX365376B (es) 2019-05-31
JP6085040B2 (ja) 2017-02-22
PE20160932A1 (es) 2016-09-10
UA116923C2 (uk) 2018-05-25
CA2932435A1 (en) 2015-07-02
EP3088401B1 (en) 2019-03-06
JO3809B1 (ar) 2021-01-31
MY173946A (en) 2020-02-28
TR201908392T4 (tr) 2019-07-22
CL2016001419A1 (es) 2017-01-20
EP3088401A1 (en) 2016-11-02
ES2728353T3 (es) 2019-10-23
HRP20190908T1 (hr) 2019-08-09
AU2014371148A1 (en) 2016-06-23
SI3088401T1 (sl) 2019-08-30
CY1122521T1 (el) 2021-01-27
NZ720718A (en) 2020-10-30
RU2016122867A3 (https=) 2018-06-18
HUE044541T2 (hu) 2019-10-28
PL3088401T3 (pl) 2019-09-30
US9174998B2 (en) 2015-11-03
RU2669805C2 (ru) 2018-10-16
RS58955B1 (sr) 2019-08-30
BR112016013572A2 (https=) 2017-10-03
PH12016501079A1 (en) 2016-07-11
KR20160094980A (ko) 2016-08-10
ME03391B (me) 2020-01-20
HK1222656A1 (zh) 2017-07-07
TW201609736A (zh) 2016-03-16

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