HUE026821T2 - Eljárás 4-{4-[({[4-klór-3-(trifluormetil)-fenil]-amino}-karbonil)-amino]-3-fluor-fenoxi}-n-metilpiridin-2-karboxamid, sói és monohidrátja elõállítására - Google Patents
Eljárás 4-{4-[({[4-klór-3-(trifluormetil)-fenil]-amino}-karbonil)-amino]-3-fluor-fenoxi}-n-metilpiridin-2-karboxamid, sói és monohidrátja elõállítására Download PDFInfo
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- HUE026821T2 HUE026821T2 HUE11712881A HUE11712881A HUE026821T2 HU E026821 T2 HUE026821 T2 HU E026821T2 HU E11712881 A HUE11712881 A HU E11712881A HU E11712881 A HUE11712881 A HU E11712881A HU E026821 T2 HUE026821 T2 HU E026821T2
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D213/81—Amides; Imides
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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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4412—Non condensed pyridines; Hydrogenated derivatives thereof having oxo groups directly attached to the heterocyclic ring
-
- 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
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Oncology (AREA)
- Hematology (AREA)
- Pyridine Compounds (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Containers And Plastic Fillers For Packaging (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
Claims (4)
- Szabadalmi igénypontok I. Bljáfás: az (tjképleii vegyít letmmoMdráíja <$56iHtíeái^ifa£ a (í¥|í képlstü vegyületet (V) képíetü vegyületseikezeljük egy íenltoiósiegyheo, ezután az oldott 0) képletü vegyöleíet egy savval kezeljük és Így az 0} képied! vegyület ep sept kapjak* amely az oldott flj képíetü vegyüteiet tartalmazó oldatból kicsapódik,. és «asft«|| képiétü vegyület sáp ep vizes bMkm oldattal kezeljük az fi) képleté vegynlet Kíonohiclratjának kksapüása céljából 2i M 1 igénypont szerinti eljárás, ahol m ftj képiéin vegyölei nrnnohidrápt 35^C és 45°C közötti hő-mérsékleten csajratjuk ki.
- 3. Az 1, vagy %> igénypont szerinti eljárás, aboi járaíékosan a feSpzödótt tnonohicMtoi csakkeíkert nyo« óráson szárítínk addig, m ig az (Π képletü vegyület képződik. 4 Az 1 - 3. igénypontok bánnsíyike szerinti eljárás, ahol s savat az fi) képlet« vegyült képződés« után PÄI renkeióeiegyben képezzük a reakcíóelegyhez egy proiikus anyagot és egy sav-pr«k«rzint adagolva, 5. A 4 igénypont szerion eljárás, ahol a savát az (1 i képtetft vegyüld: képződése tÄ ín síi® a reakció-elégyteeii képezzük a reakciodegyhez egy alköliöit és egy savklorkiot adagolva;
- 6. Az 5. igénypont szerinti eljárás, ahol az alkohol etanol és a savkiorid acetiiklortd.
- 7. Az I - ő, igénypontok bármelyike szerinti eijdés, ahol a d V) képlsAi vegydletet a (11) képletö: vegyüld- ahoi « képletben R* és JéfeÉÉése feggeílenöl a hidrogén, *ϊί, etil, »-projak izöpröpík n-fcetíl, izebutil, szek-butll, lercrbníll., ixpeotti, 2:-|>e8Íi, 3-péîSïl, 8eopéntiiÿ. <*·&$& 3*hexi1 and 3'4oxíl alkotta cs»porí> bol van megvätessfva, vagy Rs és R2 együtt 4-- 7-íagti cikloalkiígyünít alkotnak azzal a szénatommal, amelyhez kapcsolódnak --és a (!í) képleté vegyük'·egy bázis jelenl&éi^éi%zet!t reagítatá% mgjd .egy gay adagolfeapján fSlfjaik elő, a {W) képlett! vegyüietet kapva, S. A 7, igénypont szerinti eppis, ahol a (Ül) képiéi!! vegyíiktet egy alkalmas szerves nipszspel kp^il Oldat formájában használjuk, ilteívs A^amíso^-iasrÉnsk a:|¥í| képiéül vegyíllettei- ahol a képletben R * és R:2 jelentése egymástól füjggetlenüí a hidrogén, mét%, etil, n-pmpít, ízopropil, n-botít, szobiíÉ, szek-hotik töré-látli, tt-pernil, 3>fsnill, 3-pnhlí «iíspéntib o%xit, 2-hexil api í-höxíl alkotta csoportból van megválasztva, vagy R1 és # ό|ρ0ο 4 ~ 7-tagd cikloalkilgyüris alkotnak azzal a szénatommal, »melyhez kapcsolódnák ™ maglhatva álltunk elé. 9, A1* vagy 8, igénypont szerinti eljárás, ahol a t 10 képlett! vegyüleíet egy alkalmas szerves oldószerrel: készült oldat termáléban használjuk, mely oldatot a üí) képletét vegyidet hhiroklorídsójánafc egy bázissal végzett semlegesítése útján állítjuk elő. 10, A 7 ~ 9. igénypontok bármelyike szerinti eljárás, ahöl a (11) képletű vegyöleíot egy alkalmas szerves oldószerben {«löldjok, m oldatot egy protikos anyag és egy sav-preprzor tagolásával in sím előállított Sávval kezejpfe, ä (II) képiéin vegyület: sójaként fciesapa|P :P egy Mais vizes oldatával seinjégesípk· 1L A iö, igénypont szerinti eljárás, afeoí a prolik®; anyag egy alkohol: és a sáv-prefeurzor egy aeiilklorld.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP10004022 | 2010-04-15 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HUE026821T2 true HUE026821T2 (hu) | 2016-07-28 |
Family
ID=44070712
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HUE11712881A HUE026821T2 (hu) | 2010-04-15 | 2011-04-08 | Eljárás 4-{4-[({[4-klór-3-(trifluormetil)-fenil]-amino}-karbonil)-amino]-3-fluor-fenoxi}-n-metilpiridin-2-karboxamid, sói és monohidrátja elõállítására |
Country Status (39)
| Country | Link |
|---|---|
| US (5) | US8748622B2 (hu) |
| EP (1) | EP2558448B1 (hu) |
| JP (1) | JP5934182B2 (hu) |
| KR (2) | KR20170129276A (hu) |
| CN (2) | CN102947271B (hu) |
| AR (2) | AR081060A1 (hu) |
| AU (1) | AU2011240113B2 (hu) |
| BR (1) | BR112012026117B1 (hu) |
| CA (1) | CA2796238C (hu) |
| CL (1) | CL2012002840A1 (hu) |
| CO (1) | CO6630136A2 (hu) |
| CR (1) | CR20120526A (hu) |
| CU (2) | CU24123B1 (hu) |
| DK (1) | DK2558448T3 (hu) |
| DO (2) | DOP2012000268A (hu) |
| EC (1) | ECSP12012234A (hu) |
| ES (1) | ES2542610T3 (hu) |
| GT (1) | GT201200280A (hu) |
| HK (1) | HK1200831A1 (hu) |
| HR (1) | HRP20150885T1 (hu) |
| HU (1) | HUE026821T2 (hu) |
| IL (2) | IL222348B (hu) |
| JO (1) | JO3158B1 (hu) |
| MA (1) | MA34156B1 (hu) |
| MX (1) | MX2012011734A (hu) |
| MY (2) | MY162359A (hu) |
| NZ (1) | NZ602997A (hu) |
| PE (2) | PE20160838A1 (hu) |
| PL (1) | PL2558448T3 (hu) |
| PT (1) | PT2558448E (hu) |
| RS (1) | RS54219B1 (hu) |
| RU (1) | RU2581585C2 (hu) |
| SG (2) | SG10201501221UA (hu) |
| SI (1) | SI2558448T1 (hu) |
| TN (1) | TN2012000492A1 (hu) |
| TW (2) | TWI475992B (hu) |
| UA (1) | UA110613C2 (hu) |
| UY (2) | UY33290A (hu) |
| WO (1) | WO2011128261A1 (hu) |
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|---|---|---|---|---|
| UA91520C2 (en) * | 2004-09-29 | 2010-08-10 | Баер Шеринг Фарма Акциенгезельшафт | Thermodynamically stable form of tosylate |
| UA93673C2 (ru) | 2005-03-07 | 2011-03-10 | Баер Шеринг Фарма Акциенгезельшафт | Фармацевтическая композиция, которая содержит омега-карбоксиарилзамещенную дифенилмочевину, для лечения paka |
| AR081060A1 (es) | 2010-04-15 | 2012-06-06 | Bayer Schering Pharma Ag | Procedimiento para preparar 4-{4-[({[4-cloro-3-(trifluorometil)fenil]amino}carbonil)amino]-3-fluorofenoxi}-n-metilpiridin-2-carboxamida |
| JO3479B1 (ar) | 2012-09-06 | 2020-07-05 | Bayer Healthcare Llc | تركيبة دوائية مغلفة تحتوي على ريجورافنيب |
| SG11201501963RA (en) | 2012-09-25 | 2015-04-29 | Bayer Pharma AG | Combination of regorafenib and acetylsalicylic acid for treating cancer |
| CN104250227A (zh) * | 2013-06-29 | 2014-12-31 | 广东东阳光药业有限公司 | 瑞戈非尼新晶型及其制备方法 |
| US9518020B2 (en) | 2013-10-04 | 2016-12-13 | Hetero Research Foundation | Process for Regorafenib |
| CN105218439B (zh) * | 2014-06-06 | 2018-11-20 | 连云港润众制药有限公司 | 一种瑞格非尼的晶体及其制备方法 |
| WO2016005874A1 (en) * | 2014-07-09 | 2016-01-14 | Shilpa Medicare Limited | Process for the preparation of regorafenib and its crystalline forms |
| CN104557689B (zh) * | 2015-01-26 | 2016-06-29 | 重庆两江药物研发中心有限公司 | 制备4-[4-({[4-氯-3-(三氟甲基)苯基]氨基甲酰}氨基)-3-氟苯氧基]-n-甲基吡啶-2-甲酰胺及其一水合物的方法 |
| CN104592105B (zh) * | 2015-02-10 | 2017-01-18 | 杭州朱养心药业有限公司 | 瑞戈非尼及其制法 |
| CN105330600B (zh) * | 2015-11-30 | 2018-05-22 | 山东罗欣药业集团股份有限公司 | 一种瑞戈菲尼的制备方法 |
| CA3011662A1 (en) * | 2016-01-18 | 2017-07-27 | Natco Pharma Ltd | An improved process for the preparation of regorafenib |
| CN107118153A (zh) * | 2016-02-25 | 2017-09-01 | 石药集团中奇制药技术（石家庄）有限公司 | 一种瑞戈非尼一水合物晶型及其制备方法 |
| CN105879049B (zh) * | 2016-05-13 | 2019-03-26 | 浙江大学 | 一种瑞戈非尼与β-环糊精的包合物及其制备方法 |
| PT3630112T (pt) | 2017-06-02 | 2024-04-23 | Bayer Healthcare Llc | Combinação de regorafenib e nivolumab para tratamento de cancro |
| CN109438336B (zh) * | 2018-11-27 | 2019-11-22 | 广东安诺药业股份有限公司 | 一种瑞戈非尼水合物的制备方法 |
| CN109438337B (zh) * | 2018-11-27 | 2019-08-09 | 广东安诺药业股份有限公司 | 一种瑞戈非尼中间体的制备工艺 |
| EP3861989A1 (en) | 2020-02-07 | 2021-08-11 | Bayer Aktiengesellschaft | Pharmaceutical composition containing regorafenib and a stabilizing agent |
| WO2021160708A1 (en) | 2020-02-14 | 2021-08-19 | Bayer Aktiengesellschaft | Combination of regorafenib and msln-ttc for treating cancer |
| CN114315710B (zh) * | 2022-01-07 | 2024-04-26 | 江苏豪森药业集团有限公司 | 一种制备或纯化瑞戈非尼的方法 |
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-
2011
- 2011-03-23 AR ARP110100982A patent/AR081060A1/es not_active Application Discontinuation
- 2011-03-24 UY UY0001033290A patent/UY33290A/es active IP Right Grant
- 2011-04-08 EP EP20110712881 patent/EP2558448B1/en active Active
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