BR112016013572B1 - Composto (6s,9as)-n-benzil-6-[(4-hidroxifenil)metil]-4,7-dioxo-8-({6-[3- (piperazina-1-il)azetidina-1-il]piridina-2-il}metil)-2-(prop-2-en-1-il)-octaidro-1hpirazino[2,1-c][1,2,4]triazina-1-carboxamida - Google Patents

Composto (6s,9as)-n-benzil-6-[(4-hidroxifenil)metil]-4,7-dioxo-8-({6-[3- (piperazina-1-il)azetidina-1-il]piridina-2-il}metil)-2-(prop-2-en-1-il)-octaidro-1hpirazino[2,1-c][1,2,4]triazina-1-carboxamida Download PDF

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BR112016013572B1
BR112016013572B1 BR112016013572-5A BR112016013572A BR112016013572B1 BR 112016013572 B1 BR112016013572 B1 BR 112016013572B1 BR 112016013572 A BR112016013572 A BR 112016013572A BR 112016013572 B1 BR112016013572 B1 BR 112016013572B1
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BR
Brazil
Prior art keywords
methyl
compound
production example
azetidin
mmol
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BR112016013572-5A
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English (en)
Portuguese (pt)
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BR112016013572A2 (https=
Inventor
Satoshi Inoue
Yuji Yamamoto
Kentaro Iso
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Eisai R&D Management Co. Ltd
PRISM Pharma Co., Ltd
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Publication of BR112016013572A2 publication Critical patent/BR112016013572A2/pt
Publication of BR112016013572B1 publication Critical patent/BR112016013572B1/pt

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    • 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
    • A61K31/53—Heterocyclic 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
    • 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
    • A61K31/66—Phosphorus compounds
    • A61K31/661—Phosphorus acids or esters thereof not having P—C bonds, e.g. fosfosal, dichlorvos, malathion or mevinphos
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • 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
    • C07D401/00—Heterocyclic 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
    • C07D401/14—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic 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
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/06—Phosphorus compounds without P—C bonds
    • C07F9/08—Esters of oxyacids of phosphorus
    • C07F9/09—Esters of phosphoric acids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6561—Heterocyclic 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)
BR112016013572-5A 2013-12-25 2014-12-22 Composto (6s,9as)-n-benzil-6-[(4-hidroxifenil)metil]-4,7-dioxo-8-({6-[3- (piperazina-1-il)azetidina-1-il]piridina-2-il}metil)-2-(prop-2-en-1-il)-octaidro-1hpirazino[2,1-c][1,2,4]triazina-1-carboxamida BR112016013572B1 (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
JP2013267687 2013-12-25
JP2013-267687 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 (2)

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BR112016013572A2 BR112016013572A2 (https=) 2017-10-03
BR112016013572B1 true BR112016013572B1 (pt) 2023-03-21

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AU (1) AU2014371148B2 (https=)
BR (1) BR112016013572B1 (https=)
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CL (1) CL2016001419A1 (https=)
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DK (1) DK3088401T3 (https=)
ES (1) ES2728353T3 (https=)
HR (1) HRP20190908T1 (https=)
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IL (1) IL245961A0 (https=)
JO (1) JO3809B1 (https=)
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Families Citing this family (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1444235B1 (en) * 2001-10-12 2008-06-11 Choongwae Pharma Corporation Reverse-turn mimetics and method relating thereto
US8080657B2 (en) 2001-10-12 2011-12-20 Choongwae Pharma Corporation Compounds of reverse turn mimetics and the use thereof
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
WO2009148192A1 (en) 2008-06-06 2009-12-10 Prism Biolab Corporation Alpha helix mimetics and methods relating thereto
CN102459271B (zh) * 2009-04-15 2014-07-02 Jw制药公司 回折模拟物的新化合物及其制备方法和用途
CN103209982B (zh) * 2010-10-14 2016-03-16 Jw制药公司 反转模拟物的化合物、其制造方法及其用途
US20140051706A1 (en) * 2011-02-25 2014-02-20 Prism Pharma Co., Ltd. Alpha helix mimetics and methods relating thereto

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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
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
SG11201604496YA (en) 2016-07-28

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