JO3809B1 - مركب (6S، 9aS)-N- بنزيل -6-[(4- هيدروكسي فينيل) ميثيل]-4، 7- داي أوكسو -8-({6-[3-(بيبرازين -1- يل) أزيتيدين -1- يل] بيريدين -2- يل} ميثيل)-2-(بروب-2-إين- 1- يل)- أوكتا هيدرو -1H- بيرازينو [2، 1-c][1، 2، 4] ترايازين -1- كربوكساميد - Google Patents
مركب (6S، 9aS)-N- بنزيل -6-[(4- هيدروكسي فينيل) ميثيل]-4، 7- داي أوكسو -8-({6-[3-(بيبرازين -1- يل) أزيتيدين -1- يل] بيريدين -2- يل} ميثيل)-2-(بروب-2-إين- 1- يل)- أوكتا هيدرو -1H- بيرازينو [2، 1-c][1، 2، 4] ترايازين -1- كربوكساميدInfo
- Publication number
- JO3809B1 JO3809B1 JOP/2014/0373A JOP20140373A JO3809B1 JO 3809 B1 JO3809 B1 JO 3809B1 JO P20140373 A JOP20140373 A JO P20140373A JO 3809 B1 JO3809 B1 JO 3809B1
- Authority
- JO
- Jordan
- Prior art keywords
- span
- strong
- dir
- rtl
- methyl
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 2
- 125000004203 4-hydroxyphenyl group Chemical group [H]OC1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 title 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 title 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 4
- 125000000217 alkyl group Chemical group 0.000 abstract 2
- 125000005843 halogen group Chemical group 0.000 abstract 1
- 230000037361 pathway Effects 0.000 abstract 1
- 230000001105 regulatory effect Effects 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Molecular Biology (AREA)
- Biochemistry (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (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)
Abstract
يتعلق الاختراع الحالي بمركب ممثل بالصيغة (1) أو ملح مقبول صيدلانيا منه: <strong><span dir="LTR"><img src="file:///C:/Users/Darwish.Q/AppData/Local/Temp/msohtmlclip1/01/clip_image002.jpg" /></span></strong> <span dir="RTL">حيث </span><strong>R1</strong><span dir="RTL"> هي مجموعة </span><strong>C1-6</strong><span dir="RTL"> ألكيل، </span><strong>R2</strong><span dir="RTL"> و </span><strong>R3</strong><span dir="RTL"> تكون متشابهة أو مختلفة عن بعضها البعض وكل منها عبارة عن ذرة هيدروجين أو مجموعة </span><strong>C1-6</strong><span dir="RTL"> ألكيل، </span><strong>X2</strong><span dir="RTL">، </span><strong>X3 </strong><span dir="RTL"> و </span><strong>X4</strong><span dir="RTL"> تكون متشابهة او مختلفة عن بعضها البعض وكل منها عبارة عن ذرة هيدروجين أو ذرة هالوجين، و </span><strong>X5</strong><span dir="RTL"> هي ذرة هيدروجين أو </span><strong>-P(=O)(OH)2</strong><span dir="RTL"> لها نشاط تنظيم مسارة </span><strong>Wnt</strong><span dir="RTL">. </span>
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2013267687 | 2013-12-25 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| JO3809B1 true JO3809B1 (ar) | 2021-01-31 |
Family
ID=53399298
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JOP/2014/0373A JO3809B1 (ar) | 2013-12-25 | 2014-12-21 | مركب (6S، 9aS)-N- بنزيل -6-[(4- هيدروكسي فينيل) ميثيل]-4، 7- داي أوكسو -8-({6-[3-(بيبرازين -1- يل) أزيتيدين -1- يل] بيريدين -2- يل} ميثيل)-2-(بروب-2-إين- 1- يل)- أوكتا هيدرو -1H- بيرازينو [2، 1-c][1، 2، 4] ترايازين -1- كربوكساميد |
Country Status (34)
| Country | Link |
|---|---|
| US (1) | US9174998B2 (ar) |
| EP (1) | EP3088401B1 (ar) |
| JP (1) | JP6085040B2 (ar) |
| KR (1) | KR102307053B1 (ar) |
| CN (1) | CN105873932B (ar) |
| AR (1) | AR098908A1 (ar) |
| AU (1) | AU2014371148B2 (ar) |
| BR (1) | BR112016013572B1 (ar) |
| CA (1) | CA2932435C (ar) |
| CL (1) | CL2016001419A1 (ar) |
| CY (1) | CY1122521T1 (ar) |
| DK (1) | DK3088401T3 (ar) |
| ES (1) | ES2728353T3 (ar) |
| HR (1) | HRP20190908T1 (ar) |
| HU (1) | HUE044541T2 (ar) |
| IL (1) | IL245961A0 (ar) |
| JO (1) | JO3809B1 (ar) |
| LT (1) | LT3088401T (ar) |
| ME (1) | ME03391B (ar) |
| MX (1) | MX365376B (ar) |
| MY (1) | MY173946A (ar) |
| PE (1) | PE20160932A1 (ar) |
| PH (1) | PH12016501079A1 (ar) |
| PL (1) | PL3088401T3 (ar) |
| PT (1) | PT3088401T (ar) |
| RS (1) | RS58955B1 (ar) |
| RU (1) | RU2669805C2 (ar) |
| SG (1) | SG11201604496YA (ar) |
| SI (1) | SI3088401T1 (ar) |
| SM (1) | SMT201900306T1 (ar) |
| TR (1) | TR201908392T4 (ar) |
| TW (1) | TWI681961B (ar) |
| UA (1) | UA116923C2 (ar) |
| WO (1) | WO2015098853A1 (ar) |
Families Citing this family (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BR112012003592B8 (pt) | 2009-08-19 | 2021-05-25 | Eisai R&D Man Co Ltd | composição farmacêutica contendo derivado de quinolina |
| WO2012166899A2 (en) | 2011-06-03 | 2012-12-06 | Eisai R&D Management Co., Ltd. | Biomarkers for predicting and assessing responsiveness of thyroid and kidney cancer subjects to lenvatinib compounds |
| CA2957005C (en) | 2014-08-28 | 2021-10-12 | Eisai R&D Management Co., Ltd. | High-purity quinoline derivative and method for manufacturing same |
| SG11201706630UA (en) | 2015-02-25 | 2017-09-28 | Eisai R&D Man Co Ltd | Method for suppressing bitterness of quinoline derivative |
| 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 |
| BR112017027227B1 (pt) * | 2015-06-16 | 2023-12-12 | Eisai R&D Management Co., Ltd | Agente anti-câncer |
| MX2017015257A (es) * | 2015-06-23 | 2018-02-19 | Eisai R&D Man Co Ltd | Cristal de (6s, 9as)-n-bencil-8-({6-[3-(4-etilpiperazin-1-il)azeti din-1-il]piridin-2-il}metil)-6-(2-(fluoruro-4-hidroxibencil)-4,7- dioxo-2-prop-2-en-1-il)hexahidro-2h-pirazino[2,1-c] [1,2,4]triazon-1-(6h)-carboxamida. |
| 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 |
| US12303505B2 (en) | 2017-02-08 | 2025-05-20 | Eisai R&D Management Co., Ltd. | Tumor-treating pharmaceutical composition |
| BR112019023064A2 (pt) | 2017-05-16 | 2020-06-09 | Eisai R&D Man Co Ltd | tratamento de carcinoma hepatocelular |
| US20220409724A1 (en) | 2019-10-29 | 2022-12-29 | 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 |
| KR20220151178A (ko) * | 2020-03-12 | 2022-11-14 | 3＋2 파마, 엘엘씨 | Cbp/카테닌 신호전달 경로 억제제 및 그것의 용도 |
| 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 |
| WO2022092294A1 (ja) | 2020-10-30 | 2022-05-05 | 学校法人慶應義塾 | サルコペニア関連疾患等の新規治療および予防 |
| WO2023027888A1 (en) * | 2021-08-26 | 2023-03-02 | 3+2 Pharma, Llc | Pyrazole-containing cbp/catenin antagonists and uses thereof |
| CA3227813A1 (en) * | 2021-09-08 | 2023-03-16 | Eisai R&D Management Co., Ltd. | Pharmaceutical composition for treating solid tumors |
| 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 |
| CN120813358A (zh) | 2023-04-06 | 2025-10-17 | 卫材R&D管理有限公司 | 用于治疗肿瘤的药物组合物 |
| 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)
| 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 |
| 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 |
| JP2009184924A (ja) | 2006-05-31 | 2009-08-20 | Eisai R & D Management Co Ltd | 生物学的試薬用化合物 |
| BRPI0911383B1 (pt) * | 2008-06-06 | 2021-08-31 | Prism Biolab Corporation | Composto, composição farmacêutica, uso do referido composto, agentes para tratar ou prevenir câncer, fibrose, restenose associada com angioplastia, doença renal policística, doença de angiogênese aberrante, complexo de esclerose tuberosa (tsc) tumor associado com kshv, perda de cabelo, e doença de alzheimer, e processo para preparar o referido composto |
| 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 |
| ES2552462T3 (es) * | 2010-10-14 | 2015-11-30 | Jw Pharmaceutical Corporation | Nuevo compuesto de un mimético de giro inverso y un procedimiento de producción y uso del mismo |
| WO2012115286A1 (en) * | 2011-02-25 | 2012-08-30 | Prism Biolab Corporation | 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 KR KR1020167015608A patent/KR102307053B1/ko active Active
- 2014-12-22 PT PT14873998T patent/PT3088401T/pt unknown
- 2014-12-22 PL PL14873998T patent/PL3088401T3/pl unknown
- 2014-12-22 TR TR2019/08392T patent/TR201908392T4/tr unknown
- 2014-12-22 BR BR112016013572-5A patent/BR112016013572B1/pt active IP Right Grant
- 2014-12-22 WO PCT/JP2014/083932 patent/WO2015098853A1/ja not_active Ceased
- 2014-12-22 MX MX2016007705A patent/MX365376B/es active IP Right Grant
- 2014-12-22 LT LTEP14873998.0T patent/LT3088401T/lt unknown
- 2014-12-22 RS RS20190665A patent/RS58955B1/sr unknown
- 2014-12-22 AU AU2014371148A patent/AU2014371148B2/en active Active
- 2014-12-22 UA UAA201606261A patent/UA116923C2/uk unknown
- 2014-12-22 ME MEP-2019-158A patent/ME03391B/me unknown
- 2014-12-22 CA CA2932435A patent/CA2932435C/en active Active
- 2014-12-22 PE PE2016000711A patent/PE20160932A1/es unknown
- 2014-12-22 SM SM20190306T patent/SMT201900306T1/it unknown
- 2014-12-22 DK DK14873998.0T patent/DK3088401T3/da active
- 2014-12-22 SG SG11201604496YA patent/SG11201604496YA/en unknown
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- 2014-12-22 AR ARP140104850A patent/AR098908A1/es active IP Right Grant
- 2014-12-22 JP JP2015554886A patent/JP6085040B2/ja active Active
- 2014-12-22 RU RU2016122867A patent/RU2669805C2/ru active
- 2014-12-22 EP EP14873998.0A patent/EP3088401B1/en active Active
- 2014-12-22 ES ES14873998T patent/ES2728353T3/es active Active
- 2014-12-22 CN CN201480067017.7A patent/CN105873932B/zh active Active
- 2014-12-22 SI SI201431226T patent/SI3088401T1/sl unknown
- 2014-12-22 HR HRP20190908TT patent/HRP20190908T1/hr unknown
- 2014-12-22 TW TW103144928A patent/TWI681961B/zh active
- 2014-12-22 MY MYPI2016702025A patent/MY173946A/en unknown
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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
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2019
- 2019-05-31 CY CY20191100578T patent/CY1122521T1/el unknown
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