CN105873932B - (6S,9aS)‑N‑苄基‑6‑[(4‑羟基苯基)甲基]‑4,7‑二氧‑8‑({6‑[3‑(哌嗪‑1‑基)氮杂环丁烷‑1‑基]吡啶‑2‑基}甲基)‑2‑(丙‑2‑烯‑1‑基)‑八氢‑1H‑吡嗪并[2,1‑c][1,2,4]三嗪‑1‑甲酰胺化合物 - Google Patents
(6S,9aS)‑N‑苄基‑6‑[(4‑羟基苯基)甲基]‑4,7‑二氧‑8‑({6‑[3‑(哌嗪‑1‑基)氮杂环丁烷‑1‑基]吡啶‑2‑基}甲基)‑2‑(丙‑2‑烯‑1‑基)‑八氢‑1H‑吡嗪并[2,1‑c][1,2,4]三嗪‑1‑甲酰胺化合物 Download PDFInfo
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- CN105873932B CN105873932B CN201480067017.7A CN201480067017A CN105873932B CN 105873932 B CN105873932 B CN 105873932B CN 201480067017 A CN201480067017 A CN 201480067017A CN 105873932 B CN105873932 B CN 105873932B
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- Prior art keywords
- bases
- methyl
- octahydro
- triazine
- pyridine
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- 0 CC[C@@](C)[C@](CC)CC(C=CC1)=C(C)C=C1[C@]1CC(CCC(CC(C)C(C)(*C)*=C)=C2*CC2)CC1 Chemical compound CC[C@@](C)[C@](CC)CC(C=CC1)=C(C)C=C1[C@]1CC(CCC(CC(C)C(C)(*C)*=C)=C2*CC2)CC1 0.000 description 7
- CRLJCIHYGPHTDI-IBGZPJMESA-N CCN(CC1)[C@@H](C)CN1C(C1)CN1C(c1ccccc1)c1ccccc1 Chemical compound CCN(CC1)[C@@H](C)CN1C(C1)CN1C(c1ccccc1)c1ccccc1 CRLJCIHYGPHTDI-IBGZPJMESA-N 0.000 description 1
- HIQVWLMURZJTMI-KTPUSDJZSA-N CCN(CC1)[C@@H](C)CN1C(C1)CN1c1nc(CN(C[C@@H](C(CC2)[C@H]3Cc(ccc(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](C(CC2)[C@H]3Cc(ccc(O)c4)c4F)N(C(NCc4ccccc4)=O)N(CC=C)CC2=O)C3=O)ccc1 HIQVWLMURZJTMI-KTPUSDJZSA-N 0.000 description 1
- UBUGKJPFVFUWMO-BHVANESWSA-N CCOC(CN(Cc1cccc(F)n1)C([C@H](Cc(c(F)cc(OCc1ccccc1)c1)c1F)NC(CN(CC=C)NC(NCc1ccccc1)=O)=O)=O)OCC Chemical compound CCOC(CN(Cc1cccc(F)n1)C([C@H](Cc(c(F)cc(OCc1ccccc1)c1)c1F)NC(CN(CC=C)NC(NCc1ccccc1)=O)=O)=O)OCC UBUGKJPFVFUWMO-BHVANESWSA-N 0.000 description 1
- IIABFQCUZITFET-UHFFFAOYSA-N CN(C)C(CC1)CCN1C1CNC1 Chemical compound CN(C)C(CC1)CCN1C1CNC1 IIABFQCUZITFET-UHFFFAOYSA-N 0.000 description 1
- DZWQQLBLLDVRQM-UHFFFAOYSA-N CN(CCN1CCCCCC1)C(C1)CN1c1cccc(C=O)n1 Chemical compound CN(CCN1CCCCCC1)C(C1)CN1c1cccc(C=O)n1 DZWQQLBLLDVRQM-UHFFFAOYSA-N 0.000 description 1
- KUVDGCAHTKVSLX-CYBMUJFWSA-N C[C@H](C1)N(C)CCN1C(C1)CN1c1nc(C=S(C)C)ccc1F Chemical compound C[C@H](C1)N(C)CCN1C(C1)CN1c1nc(C=S(C)C)ccc1F KUVDGCAHTKVSLX-CYBMUJFWSA-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)
- 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 | ||
| 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 |
|---|---|
| CN105873932A CN105873932A (zh) | 2016-08-17 |
| CN105873932B true CN105873932B (zh) | 2017-11-24 |
Family
ID=53399298
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201480067017.7A Active CN105873932B (zh) | 2013-12-25 | 2014-12-22 | (6S,9aS)‑N‑苄基‑6‑[(4‑羟基苯基)甲基]‑4,7‑二氧‑8‑({6‑[3‑(哌嗪‑1‑基)氮杂环丁烷‑1‑基]吡啶‑2‑基}甲基)‑2‑(丙‑2‑烯‑1‑基)‑八氢‑1H‑吡嗪并[2,1‑c][1,2,4]三嗪‑1‑甲酰胺化合物 |
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=) |
Families Citing this family (23)
| 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 |
Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1585770A (zh) * | 2001-10-12 | 2005-02-23 | 中外药品株式会社 | 回折模拟物及其相关的方法 |
| CN101827849A (zh) * | 2007-10-15 | 2010-09-08 | (株)中外制药 | 新型回折模拟物化合物及其用途(1) |
| CN102046628A (zh) * | 2008-06-06 | 2011-05-04 | 株式会社棱镜生物实验室 | α螺旋拟似物和与其有关的方法 |
| CN103209982A (zh) * | 2010-10-14 | 2013-07-17 | Jw制药公司 | 新颖反转模拟物的化合物、其制造方法及其用途 |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| 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 |
| US20140051706A1 (en) * | 2011-02-25 | 2014-02-20 | Prism Pharma Co., Ltd. | Alpha helix mimetics and methods relating thereto |
-
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 HU HUE14873998 patent/HUE044541T2/hu unknown
- 2014-12-22 EP EP14873998.0A patent/EP3088401B1/en active Active
- 2014-12-22 WO PCT/JP2014/083932 patent/WO2015098853A1/ja not_active Ceased
- 2014-12-22 RU RU2016122867A patent/RU2669805C2/ru active
- 2014-12-22 BR BR112016013572-5A patent/BR112016013572B1/pt active IP Right Grant
- 2014-12-22 SI SI201431226T patent/SI3088401T1/sl unknown
- 2014-12-22 UA UAA201606261A patent/UA116923C2/uk unknown
- 2014-12-22 HR HRP20190908TT patent/HRP20190908T1/hr unknown
- 2014-12-22 ME MEP-2019-158A patent/ME03391B/me unknown
- 2014-12-22 MY MYPI2016702025A patent/MY173946A/en unknown
- 2014-12-22 AR ARP140104850A patent/AR098908A1/es active IP Right Grant
- 2014-12-22 PT PT14873998T patent/PT3088401T/pt unknown
- 2014-12-22 ES ES14873998T patent/ES2728353T3/es active Active
- 2014-12-22 DK DK14873998.0T patent/DK3088401T3/da active
- 2014-12-22 AU AU2014371148A patent/AU2014371148B2/en active Active
- 2014-12-22 JP JP2015554886A patent/JP6085040B2/ja active Active
- 2014-12-22 TR TR2019/08392T patent/TR201908392T4/tr unknown
- 2014-12-22 TW TW103144928A patent/TWI681961B/zh active
- 2014-12-22 CA CA2932435A patent/CA2932435C/en active Active
- 2014-12-22 KR KR1020167015608A patent/KR102307053B1/ko active Active
- 2014-12-22 LT LTEP14873998.0T patent/LT3088401T/lt unknown
- 2014-12-22 MX MX2016007705A patent/MX365376B/es active IP Right Grant
- 2014-12-22 SG SG11201604496YA patent/SG11201604496YA/en unknown
- 2014-12-22 PE PE2016000711A patent/PE20160932A1/es unknown
- 2014-12-22 SM SM20190306T patent/SMT201900306T1/it unknown
- 2014-12-22 PL PL14873998T patent/PL3088401T3/pl unknown
- 2014-12-22 RS RS20190665A patent/RS58955B1/sr unknown
- 2014-12-22 CN CN201480067017.7A patent/CN105873932B/zh active Active
-
2016
- 2016-06-01 IL IL245961A patent/IL245961A0/en active IP Right Grant
- 2016-06-07 PH PH12016501079A patent/PH12016501079A1/en unknown
- 2016-06-09 CL CL2016001419A patent/CL2016001419A1/es unknown
-
2019
- 2019-05-31 CY CY20191100578T patent/CY1122521T1/el unknown
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1585770A (zh) * | 2001-10-12 | 2005-02-23 | 中外药品株式会社 | 回折模拟物及其相关的方法 |
| CN101827849A (zh) * | 2007-10-15 | 2010-09-08 | (株)中外制药 | 新型回折模拟物化合物及其用途(1) |
| CN102046628A (zh) * | 2008-06-06 | 2011-05-04 | 株式会社棱镜生物实验室 | α螺旋拟似物和与其有关的方法 |
| CN103209982A (zh) * | 2010-10-14 | 2013-07-17 | Jw制药公司 | 新颖反转模拟物的化合物、其制造方法及其用途 |
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