AU2014371148B2 - (6S,9aS)-N-Benzyl-6-[(4-hydroxyphenyl)methyl]-4,7-dioxo-8-({6-[3-(piperazin-1-yl)azetidin-1-yl]pyridin-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-(piperazin-1-yl)azetidin-1-yl]pyridin-2-yl}methyl)-2-(prop-2-en-1-yl)-octahydro-1H-pyrazino[2,1-c][1,2,4]triazine-1-carboxamide compound Download PDFInfo
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- AU2014371148B2 AU2014371148B2 AU2014371148A AU2014371148A AU2014371148B2 AU 2014371148 B2 AU2014371148 B2 AU 2014371148B2 AU 2014371148 A AU2014371148 A AU 2014371148A AU 2014371148 A AU2014371148 A AU 2014371148A AU 2014371148 B2 AU2014371148 B2 AU 2014371148B2
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- Prior art keywords
- methyl
- azetidin
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- dioxo
- pyridin
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- Legal status (The legal status 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 status listed.)
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- YJBYVWPJFFLDEA-UHFFFAOYSA-N C(C(C1)N2CCNCC2)N1C(c1ccccc1)c1ccccc1 Chemical compound C(C(C1)N2CCNCC2)N1C(c1ccccc1)c1ccccc1 YJBYVWPJFFLDEA-UHFFFAOYSA-N 0.000 description 1
- ACHKODBKPIYEAA-TXEYEHERSA-N C=CCN(CC(N([C@H]1Cc(ccc(O)c2)c2F)C2CN(Cc3cccc(N(C4)CC4N4CCNCC4)n3)C1=O)=O)N2C(NCc1ccccc1)=O Chemical compound C=CCN(CC(N([C@H]1Cc(ccc(O)c2)c2F)C2CN(Cc3cccc(N(C4)CC4N4CCNCC4)n3)C1=O)=O)N2C(NCc1ccccc1)=O ACHKODBKPIYEAA-TXEYEHERSA-N 0.000 description 1
- QPCLXPASPOEQDQ-YTTGMZPUSA-N C=CCN(CC(N1[C@H]2Cc(cc3)ccc3O)=O)N(C(NCc3ccccc3)=O)C1=CN(Cc1cccc(N(C3)CC3N3CCNCC3)n1)C2=O Chemical compound C=CCN(CC(N1[C@H]2Cc(cc3)ccc3O)=O)N(C(NCc3ccccc3)=O)C1=CN(Cc1cccc(N(C3)CC3N3CCNCC3)n1)C2=O QPCLXPASPOEQDQ-YTTGMZPUSA-N 0.000 description 1
- HUMCBGQMGBSZTM-UHFFFAOYSA-N CC(C)(C)OC(N(CCN(C1)C(C2)CN2C(OCc2ccccc2)=O)C1=C)=O Chemical compound CC(C)(C)OC(N(CCN(C1)C(C2)CN2C(OCc2ccccc2)=O)C1=C)=O HUMCBGQMGBSZTM-UHFFFAOYSA-N 0.000 description 1
- CGGIGQCERSOURU-UHFFFAOYSA-N CC(C)(C)OC(N(CCN(C1)C(C2)CN2C(c2ccccc2)c2ccccc2)C1=C)=O Chemical compound CC(C)(C)OC(N(CCN(C1)C(C2)CN2C(c2ccccc2)c2ccccc2)C1=C)=O CGGIGQCERSOURU-UHFFFAOYSA-N 0.000 description 1
- CLLCWJTWEREZFG-JEFWXSHNSA-N CCCN(C)C(C1)CN1c(nc(CN(CC(N1[C@H]2Cc(ccc(O)c3)c3F)N(C(NCc3ccccc3)=O)N(CC=C)CC1=O)C2=O)cc1)c1F Chemical compound CCCN(C)C(C1)CN1c(nc(CN(CC(N1[C@H]2Cc(ccc(O)c3)c3F)N(C(NCc3ccccc3)=O)N(CC=C)CC1=O)C2=O)cc1)c1F CLLCWJTWEREZFG-JEFWXSHNSA-N 0.000 description 1
- IPXIRECOYFNZDT-UHFFFAOYSA-N CCOC(c(cc1)nc(Cl)c1F)OCC Chemical compound CCOC(c(cc1)nc(Cl)c1F)OCC IPXIRECOYFNZDT-UHFFFAOYSA-N 0.000 description 1
- VHPCUJXVFCOGMO-UHFFFAOYSA-N CN(CC1)CCN1C(C1)CN1C(c1ccccc1)c1ccccc1 Chemical compound CN(CC1)CCN1C(C1)CN1C(c1ccccc1)c1ccccc1 VHPCUJXVFCOGMO-UHFFFAOYSA-N 0.000 description 1
- 0 CN[C@@](Cc(c(*)c1)c(*)cc1O*)C(O)=O Chemical compound CN[C@@](Cc(c(*)c1)c(*)cc1O*)C(O)=O 0.000 description 1
- QQQVLIVWQMWACQ-KRWDZBQOSA-N COC([C@H](CO)NC(OCC1c2ccccc2-c2c1cccc2)=O)=O Chemical compound COC([C@H](CO)NC(OCC1c2ccccc2-c2c1cccc2)=O)=O QQQVLIVWQMWACQ-KRWDZBQOSA-N 0.000 description 1
- DZLNJPOZHMZNFI-LJAQVGFWSA-N OC([C@H](Cc(c(F)cc(OCc1ccccc1)c1)c1F)NC(OCC1c2ccccc2-c2c1cccc2)=O)=O Chemical compound OC([C@H](Cc(c(F)cc(OCc1ccccc1)c1)c1F)NC(OCC1c2ccccc2-c2c1cccc2)=O)=O DZLNJPOZHMZNFI-LJAQVGFWSA-N 0.000 description 1
Classifications
-
- 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
-
- 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
- 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
Landscapes
- 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)
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)
| Publication Number | Publication Date |
|---|---|
| AU2014371148A1 AU2014371148A1 (en) | 2016-06-23 |
| AU2014371148B2 true AU2014371148B2 (en) | 2018-08-09 |
Family
ID=53399298
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AU2014371148A Active AU2014371148B2 (en) | 2013-12-25 | 2014-12-22 | (6S,9aS)-N-Benzyl-6-[(4-hydroxyphenyl)methyl]-4,7-dioxo-8-({6-[3-(piperazin-1-yl)azetidin-1-yl]pyridin-2-yl}methyl)-2-(prop-2-en-1-yl)-octahydro-1H-pyrazino[2,1-c][1,2,4]triazine-1-carboxamide compound |
Country Status (34)
Families Citing this family (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| SG11201700855XA (en) | 2014-08-28 | 2017-03-30 | Eisai R&D Man Co Ltd | High-purity quinoline derivative and method for manufacturing same |
| BR112017017428A2 (pt) | 2015-02-25 | 2018-04-03 | Eisai R&D Management Co., Ltd. | ?método para supressão do amargor de derivado de quinolina? |
| KR20250020678A (ko) | 2015-03-04 | 2025-02-11 | 머크 샤프 앤드 돔 엘엘씨 | 암을 치료하기 위한 pd-1 길항제 및 vegfr/fgfr/ret 티로신 키나제 억제제의 조합 |
| US11369623B2 (en) * | 2015-06-16 | 2022-06-28 | Prism Pharma Co., Ltd. | Anticancer combination of a CBP/catenin inhibitor and an immune checkpoint inhibitor |
| RU2723551C2 (ru) | 2015-06-23 | 2020-06-16 | Эйсай Ар Энд Ди Менеджмент Ко., Лтд. | Кристалл (6S,9aS)-N-бензил-8-({ 6-[3-(4-этилпиперазин-1-ил)азетидин-1-ил]пиридин-2-ил} метил)-6-(2-фтор-4-гидроксибензил)-4,7-диоксо-2-(проп-2-ен-1-ил)гексагидро-2H-пиразино[2,1-c][1,2,4]триазин-1(6H)-карбоксамида |
| RU2718048C2 (ru) | 2015-08-20 | 2020-03-30 | Эйсай Ар Энд Ди Менеджмент Ко., Лтд. | Противоопухолевое терапевтическое средство |
| 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 |
| AU2018219637B2 (en) | 2017-02-08 | 2023-07-13 | Eisai R&D Management Co., Ltd. | Tumor-treating pharmaceutical composition |
| US20200197384A1 (en) | 2017-05-16 | 2020-06-25 | Eisai R&D Management Co., Ltd. | Treatment of hepatocellular carcinoma |
| CA3155672A1 (en) | 2019-10-29 | 2021-05-06 | Yoichi Ozawa | Combination of a pd-1 antagonist, a vegfr/fgfr/ret tyrosine kinase inhibitor and a cbp/beta-catenin inhibitor for treating cancer |
| AR121544A1 (es) * | 2020-03-12 | 2022-06-15 | 3 2 Pharma | Inhibidores de la vía de señalización por cbp / catenina y sus usos |
| EP4238567A4 (en) | 2020-10-30 | 2024-09-04 | Keio University | NEW TREATMENT AND PREVENTION OF DISEASES RELATED TO SARCOPENIA |
| US20240352020A1 (en) * | 2021-08-26 | 2024-10-24 | 3+2 Pharma, Llc | Pyrazole-containing cbp/catenin antagonists and uses thereof |
| CN117794544A (zh) * | 2021-09-08 | 2024-03-29 | 卫材R&D管理有限公司 | 实体瘤治疗用医药组合物 |
| 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 |
| KR20240167633A (ko) | 2022-03-31 | 2024-11-27 | 에자이 알앤드디 매니지먼트 가부시키가이샤 | 종양 치료용 약학 조성물 |
| 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 |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2310215T3 (es) * | 2001-10-12 | 2009-01-01 | Choongwae Pharma Corporation | Estructuras mimeticas de giro inverso y metodo relacionado. |
| US7671054B1 (en) | 2001-10-12 | 2010-03-02 | 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 |
| JP2009184924A (ja) | 2006-05-31 | 2009-08-20 | Eisai R & D Management Co Ltd | 生物学的試薬用化合物 |
| ES2552239T3 (es) | 2008-06-06 | 2015-11-26 | Prism Pharma Co., Ltd. | Miméticos de hélice alfa y métodos relacionados con los mismos |
| SG175045A1 (en) * | 2009-04-15 | 2011-11-28 | Jw Pharmaceutical Corp | Novel compounds of reverse-turn mimetics, method for manufacturing the same and use thereof |
| KR101892575B1 (ko) * | 2010-10-14 | 2018-08-31 | 제이더블유중외제약 주식회사 | 리버스-턴 유사체의 신규한 화합물 및 그 제조방법과 용도 |
| WO2012115286A1 (en) * | 2011-02-25 | 2012-08-30 | Prism Biolab Corporation | Alpha helix mimetics and methods relating thereto |
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2014
- 2014-12-19 US US14/577,660 patent/US9174998B2/en active Active
- 2014-12-21 JO JOP/2014/0373A patent/JO3809B1/ar active
- 2014-12-22 BR BR112016013572-5A patent/BR112016013572B1/pt active IP Right Grant
- 2014-12-22 DK DK14873998.0T patent/DK3088401T3/da active
- 2014-12-22 UA UAA201606261A patent/UA116923C2/uk unknown
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- 2014-12-22 RU RU2016122867A patent/RU2669805C2/ru active
- 2014-12-22 TW TW103144928A patent/TWI681961B/zh active
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| Date | Code | Title | Description |
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| DA3 | Amendments made section 104 |
Free format text: THE NATURE OF THE AMENDMENT IS: AMEND THE INVENTION TITLE TO READ (6S,9AS)-N-BENZYL-6-((4-HYDROXYPHENYL)METHYL)-4,7-DIOXO-8-((6- (3-(PIPERAZIN-1-YL)AZETIDIN-1-YL)PYRIDIN-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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