SG11201604496YA - (6S,9aS)-N-BENZYL-6-[(4-HYDROXYPHENYL)METHYL]-4,7-DIOXO-8-({6-[3-(PIPERAZINE-1-YL)AZETIDINE-1-YL]PYRIDINE-2-YL}METHYL)-2-(PROP-2-EN-1-YL)-OCTAHYDRO-1H-PYRAZINO[2,1-c][1,2,4]TRIAZINE-1-CARBOXAMIDE COMPOUND - Google Patents

(6S,9aS)-N-BENZYL-6-[(4-HYDROXYPHENYL)METHYL]-4,7-DIOXO-8-({6-[3-(PIPERAZINE-1-YL)AZETIDINE-1-YL]PYRIDINE-2-YL}METHYL)-2-(PROP-2-EN-1-YL)-OCTAHYDRO-1H-PYRAZINO[2,1-c][1,2,4]TRIAZINE-1-CARBOXAMIDE COMPOUND

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Publication number
SG11201604496YA
SG11201604496YA SG11201604496YA SG11201604496YA SG11201604496YA SG 11201604496Y A SG11201604496Y A SG 11201604496YA SG 11201604496Y A SG11201604496Y A SG 11201604496YA SG 11201604496Y A SG11201604496Y A SG 11201604496YA SG 11201604496Y A SG11201604496Y A SG 11201604496YA
Authority
SG
Singapore
Prior art keywords
methyl
pyrazino
octahydro
azetidine
dioxo
Prior art date
Application number
SG11201604496YA
Other languages
English (en)
Inventor
Satoshi Inoue
Yuji Yamamoto
Kentaro ISO
Original Assignee
Eisai R&D Man Co Ltd
Prism Pharma Co Ltd
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 Eisai R&D Man Co Ltd, Prism Pharma Co Ltd filed Critical Eisai R&D Man Co Ltd
Publication of SG11201604496YA publication Critical patent/SG11201604496YA/en

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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)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (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)
SG11201604496YA 2013-12-25 2014-12-22 (6S,9aS)-N-BENZYL-6-[(4-HYDROXYPHENYL)METHYL]-4,7-DIOXO-8-({6-[3-(PIPERAZINE-1-YL)AZETIDINE-1-YL]PYRIDINE-2-YL}METHYL)-2-(PROP-2-EN-1-YL)-OCTAHYDRO-1H-PYRAZINO[2,1-c][1,2,4]TRIAZINE-1-CARBOXAMIDE COMPOUND SG11201604496YA (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
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

Publications (1)

Publication Number Publication Date
SG11201604496YA true SG11201604496YA (en) 2016-07-28

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SG11201604496YA SG11201604496YA (en) 2013-12-25 2014-12-22 (6S,9aS)-N-BENZYL-6-[(4-HYDROXYPHENYL)METHYL]-4,7-DIOXO-8-({6-[3-(PIPERAZINE-1-YL)AZETIDINE-1-YL]PYRIDINE-2-YL}METHYL)-2-(PROP-2-EN-1-YL)-OCTAHYDRO-1H-PYRAZINO[2,1-c][1,2,4]TRIAZINE-1-CARBOXAMIDE COMPOUND

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RU (1) RU2669805C2 (https=)
SG (1) SG11201604496YA (https=)
SI (1) SI3088401T1 (https=)
SM (1) SMT201900306T1 (https=)
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DK2468281T3 (en) 2009-08-19 2016-03-21 Eisai R&D Man Co Ltd Quinolinderivatholdig pharmaceutical composition
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
AU2016224583B2 (en) 2015-02-25 2021-06-03 Eisai R&D Management Co., Ltd. Method for suppressing bitterness of quinoline derivative
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
BR112017027227B1 (pt) * 2015-06-16 2023-12-12 Eisai R&D Management Co., Ltd Agente anti-câncer
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
JP6553726B2 (ja) 2015-08-20 2019-07-31 エーザイ・アール・アンド・ディー・マネジメント株式会社 腫瘍治療剤
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
JP6581320B2 (ja) 2017-02-08 2019-09-25 エーザイ・アール・アンド・ディー・マネジメント株式会社 腫瘍治療用医薬組成物
EP3624800A4 (en) 2017-05-16 2021-02-17 Eisai R&D Management Co., Ltd. TREATMENT OF HEPATOCELLULAR CARCINOMA
MX2022005056A (es) 2019-10-29 2022-05-18 Eisai R&D Man Co Ltd Combinacion de un antagonista de pd-1, un inhibidor tirosina cinasa de vegfr/fgfr/ret y un inhibidor de cbp/beta-catenina para el tratamiento del cancer.
AR121544A1 (es) 2020-03-12 2022-06-15 3 2 Pharma Inhibidores de la vía de señalización por cbp / catenina y sus usos
WO2021183791A1 (en) 2020-03-12 2021-09-16 City Of Hope Wnt/cbp/catenin signaling pathway inhibitors and uses thereof
US20230390296A1 (en) 2020-10-30 2023-12-07 Keio University Novel treatment and prevention of sarcopenia-related diseases
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
US20250177406A1 (en) 2022-03-31 2025-06-05 Eisai R&D Management Co., Ltd. Pharmaceutical composition for treating 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
JPWO2024209717A1 (https=) 2023-04-06 2024-10-10
WO2025174646A1 (en) * 2024-02-12 2025-08-21 Albert Einstein College Of Medicine Inhibitors of beta-catenin c-terminal domain and methods of use

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Publication number Publication date
PT3088401T (pt) 2019-06-12
AR098908A1 (es) 2016-06-22
LT3088401T (lt) 2019-07-25
EP3088401A4 (en) 2017-06-28
PE20160932A1 (es) 2016-09-10
IL245961A0 (en) 2016-08-02
SI3088401T1 (sl) 2019-08-30
US20150175615A1 (en) 2015-06-25
SMT201900306T1 (it) 2019-07-11
PH12016501079A1 (en) 2016-07-11
UA116923C2 (uk) 2018-05-25
BR112016013572B1 (pt) 2023-03-21
RU2016122867A (ru) 2018-02-01
EP3088401B1 (en) 2019-03-06
ES2728353T3 (es) 2019-10-23
RS58955B1 (sr) 2019-08-30
BR112016013572A2 (https=) 2017-10-03
RU2669805C2 (ru) 2018-10-16
WO2015098853A1 (ja) 2015-07-02
EP3088401A1 (en) 2016-11-02
PL3088401T3 (pl) 2019-09-30
NZ720718A (en) 2020-10-30
HUE044541T2 (hu) 2019-10-28
MY173946A (en) 2020-02-28
CA2932435A1 (en) 2015-07-02
RU2016122867A3 (https=) 2018-06-18
AU2014371148B2 (en) 2018-08-09
DK3088401T3 (da) 2019-06-03
AU2014371148A1 (en) 2016-06-23
ME03391B (me) 2020-01-20
TR201908392T4 (tr) 2019-07-22
JPWO2015098853A1 (ja) 2017-03-23
KR20160094980A (ko) 2016-08-10
CN105873932B (zh) 2017-11-24
US9174998B2 (en) 2015-11-03
CL2016001419A1 (es) 2017-01-20
CA2932435C (en) 2021-08-17
TW201609736A (zh) 2016-03-16
CN105873932A (zh) 2016-08-17
HK1222656A1 (zh) 2017-07-07
KR102307053B1 (ko) 2021-10-01
HRP20190908T1 (hr) 2019-08-09
JO3809B1 (ar) 2021-01-31
CY1122521T1 (el) 2021-01-27
JP6085040B2 (ja) 2017-02-22
TWI681961B (zh) 2020-01-11
MX2016007705A (es) 2017-01-11
MX365376B (es) 2019-05-31

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