KR102307053B1 - (6S,9aS)-N-벤질-6-[(4-하이드록시페닐)메틸]-4,7-디옥소-8-(｛6-[3-(피페라진-1-일)아제티딘-1-일]피리딘-2-일｝메틸)-2-(프로프-2-엔-1-일)-옥타하이드로-1H-피라지노[2,1-c][1,2,4]트리아진-1-카복사미드 화합물 - Google Patents
(6S,9aS)-N-벤질-6-[(4-하이드록시페닐)메틸]-4,7-디옥소-8-(｛6-[3-(피페라진-1-일)아제티딘-1-일]피리딘-2-일｝메틸)-2-(프로프-2-엔-1-일)-옥타하이드로-1H-피라지노[2,1-c][1,2,4]트리아진-1-카복사미드 화합물 Download PDFInfo
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- KR102307053B1 KR102307053B1 KR1020167015608A KR20167015608A KR102307053B1 KR 102307053 B1 KR102307053 B1 KR 102307053B1 KR 1020167015608 A KR1020167015608 A KR 1020167015608A KR 20167015608 A KR20167015608 A KR 20167015608A KR 102307053 B1 KR102307053 B1 KR 102307053B1
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- 0 *C=C1CNCC1 Chemical compound *C=C1CNCC1 0.000 description 4
- BDTSNXIHMAWYIC-SFCXHYMASA-N C=CCN(CC(N([C@H]1Cc(cc2)ccc2O)C2CN(Cc3c(N(CC4)CCC4N4CCCC4)nccc3)C1=O)=O)N2C(NCc1ccccc1)=O Chemical compound C=CCN(CC(N([C@H]1Cc(cc2)ccc2O)C2CN(Cc3c(N(CC4)CCC4N4CCCC4)nccc3)C1=O)=O)N2C(NCc1ccccc1)=O BDTSNXIHMAWYIC-SFCXHYMASA-N 0.000 description 1
- LFBUGXTXEUHFMA-UHFFFAOYSA-N CC(C)(C)OC(N(CCN1C(C2)CN2C(c2ccccc2)c2ccccc2)CC1=C)=O Chemical compound CC(C)(C)OC(N(CCN1C(C2)CN2C(c2ccccc2)c2ccccc2)CC1=C)=O LFBUGXTXEUHFMA-UHFFFAOYSA-N 0.000 description 1
- UWELDYUFTTWGAI-PXLJZGITSA-N CCN(CC1)CCN1C(C1)CN1c1nc(CN(C[C@@H](N2[C@H]3Cc(cc4)ccc4O)N(C(NCc4ccccc4)=O)N(CC=C)CC2=O)C3=O)ccc1F Chemical compound CCN(CC1)CCN1C(C1)CN1c1nc(CN(C[C@@H](N2[C@H]3Cc(cc4)ccc4O)N(C(NCc4ccccc4)=O)N(CC=C)CC2=O)C3=O)ccc1F UWELDYUFTTWGAI-PXLJZGITSA-N 0.000 description 1
- NAGXROCYYJYVML-YIBRVOAPSA-N CCN(CC1)[C@H](C)CN1C(C1)CN1c1nc(CN(C[C@@H](N2[C@H]3Cc(c(F)cc(O)c4)c4F)N(C(NCc4ccccc4)=O)N(CC=C)CC2=O)C3=O)ccc1 Chemical compound CCN(CC1)[C@H](C)CN1C(C1)CN1c1nc(CN(C[C@@H](N2[C@H]3Cc(c(F)cc(O)c4)c4F)N(C(NCc4ccccc4)=O)N(CC=C)CC2=O)C3=O)ccc1 NAGXROCYYJYVML-YIBRVOAPSA-N 0.000 description 1
- QRVKREFDXUNYNJ-WBCKFURZSA-N CCOC(CN(Cc(nc1N(C2)CC2N(CC2)CCC2N(C)C)ccc1F)C([C@H](Cc(cc1)ccc1OC(C)(C)C)NC(CN(CC=C)NC(NCc1ccccc1)=O)=O)=O)OCC Chemical compound CCOC(CN(Cc(nc1N(C2)CC2N(CC2)CCC2N(C)C)ccc1F)C([C@H](Cc(cc1)ccc1OC(C)(C)C)NC(CN(CC=C)NC(NCc1ccccc1)=O)=O)=O)OCC QRVKREFDXUNYNJ-WBCKFURZSA-N 0.000 description 1
- YLGPPZXIZHFGMG-UHFFFAOYSA-N CCOC(CNCc(cc1)nc(Cl)c1F)OCC Chemical compound CCOC(CNCc(cc1)nc(Cl)c1F)OCC YLGPPZXIZHFGMG-UHFFFAOYSA-N 0.000 description 1
- UETAQXGOLCRTSI-UHFFFAOYSA-N CCOC(CNCc(nc1N(C2)CC2N2CCN(C)CC2)ccc1F)OCC Chemical compound CCOC(CNCc(nc1N(C2)CC2N2CCN(C)CC2)ccc1F)OCC UETAQXGOLCRTSI-UHFFFAOYSA-N 0.000 description 1
- PDRZMSITZCEJDD-UHFFFAOYSA-N CCOC(c(cc1)nc(N(C2)CC2O)c1F)OCC Chemical compound CCOC(c(cc1)nc(N(C2)CC2O)c1F)OCC PDRZMSITZCEJDD-UHFFFAOYSA-N 0.000 description 1
- HKFSYNDLFKVZBD-LRHLLKFHSA-N CN(CC1)CCN1C(C1)CN1c1cccc(CN(C[C@@H](N2[C@H]3Cc(cc4)ccc4O)N(C(NCc4ccccc4)=O)N(CC=C)CC2=O)C3=O)n1 Chemical compound CN(CC1)CCN1C(C1)CN1c1cccc(CN(C[C@@H](N2[C@H]3Cc(cc4)ccc4O)N(C(NCc4ccccc4)=O)N(CC=C)CC2=O)C3=O)n1 HKFSYNDLFKVZBD-LRHLLKFHSA-N 0.000 description 1
- HTBNUMUVUBLDBQ-PMERELPUSA-N COC([C@H](Cc(c(F)c1)ccc1OCc1ccccc1)NC(OCC1c2ccccc2-c2c1cccc2)=O)=O Chemical compound COC([C@H](Cc(c(F)c1)ccc1OCc1ccccc1)NC(OCC1c2ccccc2-c2c1cccc2)=O)=O HTBNUMUVUBLDBQ-PMERELPUSA-N 0.000 description 1
- XUKOXHXPNZXEDQ-FOPBOCKXSA-N C[C@@H](C1)N(C)CCN1C(C1)CN1c1nc(CN(C=C(N2[C@H]3Cc(ccc(O)c4)c4F)N(C(NCc4ccccc4)=O)N(CC=C)CC2=O)C3=O)ccc1 Chemical compound C[C@@H](C1)N(C)CCN1C(C1)CN1c1nc(CN(C=C(N2[C@H]3Cc(ccc(O)c4)c4F)N(C(NCc4ccccc4)=O)N(CC=C)CC2=O)C3=O)ccc1 XUKOXHXPNZXEDQ-FOPBOCKXSA-N 0.000 description 1
- DJPZUNMMOFLWDE-QMMMGPOBSA-N C[C@@H](C1)N(C)CCN1C1CNC1 Chemical compound C[C@@H](C1)N(C)CCN1C1CNC1 DJPZUNMMOFLWDE-QMMMGPOBSA-N 0.000 description 1
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Classifications
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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)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2013267687 | 2013-12-25 | ||
| JPJP-P-2013-267687 | 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 |
|---|---|
| KR20160094980A KR20160094980A (ko) | 2016-08-10 |
| KR102307053B1 true KR102307053B1 (ko) | 2021-10-01 |
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| KR1020167015608A Active KR102307053B1 (ko) | 2013-12-25 | 2014-12-22 | (6S,9aS)-N-벤질-6-[(4-하이드록시페닐)메틸]-4,7-디옥소-8-(｛6-[3-(피페라진-1-일)아제티딘-1-일]피리딘-2-일｝메틸)-2-(프로프-2-엔-1-일)-옥타하이드로-1H-피라지노[2,1-c][1,2,4]트리아진-1-카복사미드 화합물 |
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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 |
| JO3783B1 (ar) | 2014-08-28 | 2021-01-31 | Eisai R&D Man Co Ltd | مشتق كوينولين عالي النقاء وطريقة لإنتاجه |
| BR112017017428A2 (pt) | 2015-02-25 | 2018-04-03 | Eisai R&D Management Co., Ltd. | ?método para supressão do amargor de derivado de quinolina? |
| WO2016140717A1 (en) | 2015-03-04 | 2016-09-09 | Merck Sharp & Dohme Corp. | Combination of a pd-1 antagonist and a vegfr/fgfr/ret tyrosine kinase inhibitor for treating cancer |
| KR102705821B1 (ko) * | 2015-06-16 | 2024-09-12 | 가부시키가이샤 프리즘 바이오랩 | 항암제 |
| ES2870013T3 (es) * | 2015-06-23 | 2021-10-26 | Eisai R&D Man Co Ltd | Cristal de (6S,9aS)-N-bencil-8-({6-[3-(4-etilpiperazin-1-il)azetidin-1-il]piridin-2-il}metil)-6-(2-fluoro-4-hidroxibencil)-4,7-dioxo-2-(prop-2-en-1-il)hexahidro-2H-pirazino[2,1-c][1,2,4]triazin-1(6H)-carboxamida |
| SG11201801083UA (en) | 2015-08-20 | 2018-03-28 | Eisai R&D Man 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 |
| BR112019014127A2 (pt) * | 2017-02-08 | 2020-02-11 | Eisai R&D Management Co., Ltd. | Composição farmacêutica para tratamento de tumores |
| WO2018212202A1 (en) | 2017-05-16 | 2018-11-22 | Eisai R&D Management Co., Ltd. | Treatment of hepatocellular carcinoma |
| JP7691418B2 (ja) | 2019-10-29 | 2025-06-11 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | 癌を治療するためのＰＤ－１アンタゴニスト、ＶＥＧＦＲ／ＦＧＦＲ／ＲＥＴチロシンキナーゼ阻害剤、及びＣＢＰ／β－カテニン阻害剤の組合せ |
| AU2021236240B2 (en) * | 2020-03-12 | 2024-07-25 | 3+2 Pharma LLC | CBP/catenin signaling pathway inhibitors and uses thereof |
| EP4238567A4 (en) | 2020-10-30 | 2024-09-04 | Keio University | NEW TREATMENT AND PREVENTION OF DISEASES RELATED TO SARCOPENIA |
| WO2023027888A1 (en) * | 2021-08-26 | 2023-03-02 | 3+2 Pharma, Llc | Pyrazole-containing cbp/catenin antagonists and uses thereof |
| TW202327613A (zh) | 2021-09-08 | 2023-07-16 | 日商衛材R&D企管股份有限公司 | 實性瘤治療用醫藥組成物 |
| 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 |
| WO2023190748A1 (ja) | 2022-03-31 | 2023-10-05 | 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 |
| 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 |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2011500666A (ja) | 2007-10-15 | 2011-01-06 | チュンウェ ファーマ コーポレーション | リバースターン類似体の新規化合物およびその用途（３） |
| JP2011522037A (ja) | 2008-06-06 | 2011-07-28 | ＰＲＩＳＭ ＢｉｏＬａｂ株式会社 | アルファへリックスミメティック及び関連の方法 |
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| JP4387793B2 (ja) * | 2001-10-12 | 2009-12-24 | チョンウェ ファーマ コーポレーション | 逆向ターンミメティックおよびそれに関連した方法 |
| 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 |
| KR101692921B1 (ko) * | 2009-04-15 | 2017-01-05 | 제이더블유중외제약 주식회사 | 리버스턴 유사체의 신규한 화합물 및 그 제조방법과 용도 |
| WO2012050393A2 (ko) | 2010-10-14 | 2012-04-19 | 제이더블유중외제약 주식회사 | 리버스-턴 유사체의 신규한 화합물 및 그 제조방법과 용도 |
| CN103517904A (zh) * | 2011-02-25 | 2014-01-15 | 株式会社棱镜制药 | α-螺旋模拟物和与其相关的方法 |
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Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2011500666A (ja) | 2007-10-15 | 2011-01-06 | チュンウェ ファーマ コーポレーション | リバースターン類似体の新規化合物およびその用途（３） |
| JP2011522037A (ja) | 2008-06-06 | 2011-07-28 | ＰＲＩＳＭ ＢｉｏＬａｂ株式会社 | アルファへリックスミメティック及び関連の方法 |
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