ES2728353T3 - Compuesto de (6S,9aS)-N-bencil-6-[(4-hidroxifenil)metil]-4,7-dioxo-8-({6-[3-(piperazin-1-il)azetidin-1-il]piridin-2-il}metil)-2-(prop-2-en-1-il)-octahidro-1H-pirazino[2,1-c][1,2,4]triazin-1-carboxamida - Google Patents

Compuesto de (6S,9aS)-N-bencil-6-[(4-hidroxifenil)metil]-4,7-dioxo-8-({6-[3-(piperazin-1-il)azetidin-1-il]piridin-2-il}metil)-2-(prop-2-en-1-il)-octahidro-1H-pirazino[2,1-c][1,2,4]triazin-1-carboxamida Download PDF

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Publication number
ES2728353T3
ES2728353T3 ES14873998T ES14873998T ES2728353T3 ES 2728353 T3 ES2728353 T3 ES 2728353T3 ES 14873998 T ES14873998 T ES 14873998T ES 14873998 T ES14873998 T ES 14873998T ES 2728353 T3 ES2728353 T3 ES 2728353T3
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ES
Spain
Prior art keywords
methyl
azetidin
prop
octahydro
triazin
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Active
Application number
ES14873998T
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English (en)
Spanish (es)
Inventor
Satoshi Inoue
Yuji Yamamoto
Kentaro ISO
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Eisai R&D Management Co Ltd
Prism Pharma Co Ltd
Original Assignee
Eisai R&D Management 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.)
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Publication date
Application filed by Eisai R&D Management Co Ltd, Prism Pharma Co Ltd filed Critical Eisai R&D Management Co Ltd
Application granted granted Critical
Publication of ES2728353T3 publication Critical patent/ES2728353T3/es
Active legal-status Critical Current
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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)
ES14873998T 2013-12-25 2014-12-22 Compuesto de (6S,9aS)-N-bencil-6-[(4-hidroxifenil)metil]-4,7-dioxo-8-({6-[3-(piperazin-1-il)azetidin-1-il]piridin-2-il}metil)-2-(prop-2-en-1-il)-octahidro-1H-pirazino[2,1-c][1,2,4]triazin-1-carboxamida Active ES2728353T3 (es)

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
ES2728353T3 true ES2728353T3 (es) 2019-10-23

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ES14873998T Active ES2728353T3 (es) 2013-12-25 2014-12-22 Compuesto de (6S,9aS)-N-bencil-6-[(4-hidroxifenil)metil]-4,7-dioxo-8-({6-[3-(piperazin-1-il)azetidin-1-il]piridin-2-il}metil)-2-(prop-2-en-1-il)-octahidro-1H-pirazino[2,1-c][1,2,4]triazin-1-carboxamida

Country Status (34)

Country Link
US (1) US9174998B2 (https=)
EP (1) EP3088401B1 (https=)
JP (1) JP6085040B2 (https=)
KR (1) KR102307053B1 (https=)
CN (1) CN105873932B (https=)
AR (1) AR098908A1 (https=)
AU (1) AU2014371148B2 (https=)
BR (1) BR112016013572B1 (https=)
CA (1) CA2932435C (https=)
CL (1) CL2016001419A1 (https=)
CY (1) CY1122521T1 (https=)
DK (1) DK3088401T3 (https=)
ES (1) ES2728353T3 (https=)
HR (1) HRP20190908T1 (https=)
HU (1) HUE044541T2 (https=)
IL (1) IL245961A0 (https=)
JO (1) JO3809B1 (https=)
LT (1) LT3088401T (https=)
ME (1) ME03391B (https=)
MX (1) MX365376B (https=)
MY (1) MY173946A (https=)
PE (1) PE20160932A1 (https=)
PH (1) PH12016501079A1 (https=)
PL (1) PL3088401T3 (https=)
PT (1) PT3088401T (https=)
RS (1) RS58955B1 (https=)
RU (1) RU2669805C2 (https=)
SG (1) SG11201604496YA (https=)
SI (1) SI3088401T1 (https=)
SM (1) SMT201900306T1 (https=)
TR (1) TR201908392T4 (https=)
TW (1) TWI681961B (https=)
UA (1) UA116923C2 (https=)
WO (1) WO2015098853A1 (https=)

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MY162940A (en) 2009-08-19 2017-07-31 Eisai R&D Man Co Ltd Quinoline derivative-containing 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
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
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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US8080657B2 (en) 2001-10-12 2011-12-20 Choongwae Pharma Corporation Compounds of reverse turn mimetics and the use thereof
EP1444235B1 (en) * 2001-10-12 2008-06-11 Choongwae Pharma Corporation Reverse-turn mimetics and method relating thereto
US7671054B1 (en) * 2001-10-12 2010-03-02 Choongwae Pharma Corporation Reverse-turn mimetics and method relating thereto
JP2009184924A (ja) 2006-05-31 2009-08-20 Eisai R & D Management Co Ltd 生物学的試薬用化合物
JP5530427B2 (ja) * 2008-06-06 2014-06-25 株式会社PRISM Pharma アルファへリックスミメティック及び関連の方法
CA2758904C (en) * 2009-04-15 2017-04-04 Jw Pharmaceutical Corporation Novel compounds of reverse-turn mimetics, method for manufacturing the same and use thereof
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WO2012115286A1 (en) * 2011-02-25 2012-08-30 Prism Biolab Corporation Alpha helix mimetics and methods relating thereto

Also Published As

Publication number Publication date
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
CN105873932B (zh) 2017-11-24
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
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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