JO3158B1 - عملية تحضير 4- {4 - [({[4-كلورو-3- (ترايفلوروميثيل) -فينيل] أمينو} الكربونيل)أمينو]-3-فلوروفينوكسي}- } -n-ميثلبريدين-2-كربوكساميد، وملح ومونوهيدرات منه - Google Patents
عملية تحضير 4- {4 - [({[4-كلورو-3- (ترايفلوروميثيل) -فينيل] أمينو} الكربونيل)أمينو]-3-فلوروفينوكسي}- } -n-ميثلبريدين-2-كربوكساميد، وملح ومونوهيدرات منهInfo
- Publication number
- JO3158B1 JO3158B1 JOP/2011/0125A JOP20110125A JO3158B1 JO 3158 B1 JO3158 B1 JO 3158B1 JO P20110125 A JOP20110125 A JO P20110125A JO 3158 B1 JO3158 B1 JO 3158B1
- Authority
- JO
- Jordan
- Prior art keywords
- amino
- fluorophenoxy
- methylpyridine
- carboxamide
- monohydrate
- Prior art date
Links
- 150000004682 monohydrates Chemical class 0.000 title abstract 2
- 150000003839 salts Chemical class 0.000 title abstract 2
- FNHKPVJBJVTLMP-UHFFFAOYSA-N regorafenib Chemical compound C1=NC(C(=O)NC)=CC(OC=2C=C(F)C(NC(=O)NC=3C=C(C(Cl)=CC=3)C(F)(F)F)=CC=2)=C1 FNHKPVJBJVTLMP-UHFFFAOYSA-N 0.000 title 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 1
Classifications
-
- 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
-
- 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
Landscapes
- 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)
- Containers And Plastic Fillers For Packaging (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
Abstract
يتعلق الاختراع الحالي بعملية (process) لتحضير: 4-{4-[({[4-chloro-3-(trifluoromethyl)¬phenyl]amino}carbonyl)amino]-3-fluorophenoxy}-N-methylpyridine-2-carboxamide, أملاحه وmonohydrate منه.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP10004022 | 2010-04-15 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| JO3158B1 true JO3158B1 (ar) | 2017-09-20 |
Family
ID=44070712
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JOP/2011/0125A JO3158B1 (ar) | 2010-04-15 | 2011-04-13 | عملية تحضير 4- {4 - [({[4-كلورو-3- (ترايفلوروميثيل) -فينيل] أمينو} الكربونيل)أمينو]-3-فلوروفينوكسي}- } -n-ميثلبريدين-2-كربوكساميد، وملح ومونوهيدرات منه |
Country Status (40)
| Country | Link |
|---|---|
| US (5) | US8748622B2 (ar) |
| EP (1) | EP2558448B1 (ar) |
| JP (1) | JP5934182B2 (ar) |
| KR (2) | KR20170129276A (ar) |
| CN (2) | CN103980191A (ar) |
| AR (2) | AR081060A1 (ar) |
| AU (1) | AU2011240113B2 (ar) |
| BR (1) | BR112012026117B1 (ar) |
| CA (1) | CA2796238C (ar) |
| CL (1) | CL2012002840A1 (ar) |
| CO (1) | CO6630136A2 (ar) |
| CR (1) | CR20120526A (ar) |
| CU (2) | CU24123B1 (ar) |
| DK (1) | DK2558448T3 (ar) |
| DO (2) | DOP2012000268A (ar) |
| EC (1) | ECSP12012234A (ar) |
| ES (1) | ES2542610T3 (ar) |
| GT (1) | GT201200280A (ar) |
| HK (1) | HK1200831A1 (ar) |
| HR (1) | HRP20150885T1 (ar) |
| HU (1) | HUE026821T2 (ar) |
| IL (2) | IL222348B (ar) |
| JO (1) | JO3158B1 (ar) |
| MA (1) | MA34156B1 (ar) |
| MX (1) | MX2012011734A (ar) |
| MY (2) | MY177066A (ar) |
| NZ (1) | NZ602997A (ar) |
| PE (2) | PE20130181A1 (ar) |
| PH (1) | PH12012502060A1 (ar) |
| PL (1) | PL2558448T3 (ar) |
| PT (1) | PT2558448E (ar) |
| RS (1) | RS54219B1 (ar) |
| RU (1) | RU2581585C2 (ar) |
| SG (2) | SG184172A1 (ar) |
| SI (1) | SI2558448T1 (ar) |
| TN (1) | TN2012000492A1 (ar) |
| TW (2) | TWI475992B (ar) |
| UA (1) | UA110613C2 (ar) |
| UY (2) | UY33290A (ar) |
| WO (1) | WO2011128261A1 (ar) |
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| KR101381454B1 (ko) * | 2004-09-29 | 2014-04-04 | 바이엘 인텔렉쳐 프로퍼티 게엠베하 | 열역학적으로 안정한 형태의 bay 43-9006 토실레이트 |
| KR101335932B1 (ko) | 2005-03-07 | 2013-12-04 | 바이엘 헬스케어 엘엘씨 | 암의 치료를 위한 오메가-카르복시아릴 치환된 디페닐우레아를 포함하는 제약 조성물 |
| 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 |
| AR092439A1 (es) | 2012-09-06 | 2015-04-22 | Bayer Healthcare Llc | Composicion farmaceutica recubierta que contiene regorafenib |
| MY183969A (en) | 2012-09-25 | 2021-03-17 | 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 |
| WO2015049698A2 (en) * | 2013-10-04 | 2015-04-09 | 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 |
| US9790185B2 (en) | 2014-07-09 | 2017-10-17 | 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 |
| SG11201806116SA (en) * | 2016-01-18 | 2018-08-30 | 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 |
| CA3244313A1 (en) | 2017-06-02 | 2025-06-13 | Bayer Healthcare Llc | Combination of regorafenib and pd-1/pd-l1(2) inhibitors for treating cancer |
| 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 |
| 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 |
| 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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| RU2319693C9 (ru) | 1999-01-13 | 2008-08-20 | Байер Копэрейшн | Производные мочевины (варианты), фармацевтическая композиция (варианты) и способ лечения заболевания, связанного с ростом раковых клеток (варианты) |
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| KR101381454B1 (ko) | 2004-09-29 | 2014-04-04 | 바이엘 인텔렉쳐 프로퍼티 게엠베하 | 열역학적으로 안정한 형태의 bay 43-9006 토실레이트 |
| KR101335932B1 (ko) | 2005-03-07 | 2013-12-04 | 바이엘 헬스케어 엘엘씨 | 암의 치료를 위한 오메가-카르복시아릴 치환된 디페닐우레아를 포함하는 제약 조성물 |
| WO2007053573A2 (en) | 2005-10-31 | 2007-05-10 | Bayer Pharmaceuticals Corporation | Treatment of cancer with sorafenib |
| WO2007059154A2 (en) | 2005-11-14 | 2007-05-24 | Bayer Healthcare Llc | Treatment of cancers with acquired resistance to kit inhibitors |
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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 PL PL11712881T patent/PL2558448T3/pl unknown
- 2011-04-08 KR KR1020177032906A patent/KR20170129276A/ko not_active Ceased
- 2011-04-08 SG SG2012069852A patent/SG184172A1/en unknown
- 2011-04-08 BR BR112012026117-7A patent/BR112012026117B1/pt active IP Right Grant
- 2011-04-08 RS RS20150528A patent/RS54219B1/sr unknown
- 2011-04-08 SI SI201130559T patent/SI2558448T1/sl unknown
- 2011-04-08 EP EP20110712881 patent/EP2558448B1/en active Active
- 2011-04-08 WO PCT/EP2011/055508 patent/WO2011128261A1/en not_active Ceased
- 2011-04-08 PH PH1/2012/502060A patent/PH12012502060A1/en unknown
- 2011-04-08 CA CA2796238A patent/CA2796238C/en active Active
- 2011-04-08 MX MX2012011734A patent/MX2012011734A/es active IP Right Grant
- 2011-04-08 CN CN201410248545.4A patent/CN103980191A/zh active Pending
- 2011-04-08 KR KR1020127026728A patent/KR101800041B1/ko active Active
- 2011-04-08 US US13/640,959 patent/US8748622B2/en active Active
- 2011-04-08 CN CN201180019150.1A patent/CN102947271B/zh active Active
- 2011-04-08 MY MYPI2016001879A patent/MY177066A/en unknown
- 2011-04-08 SG SG10201501221UA patent/SG10201501221UA/en unknown
- 2011-04-08 ES ES11712881.9T patent/ES2542610T3/es active Active
- 2011-04-08 MY MYPI2012004548A patent/MY162359A/en unknown
- 2011-04-08 RU RU2012148386/04A patent/RU2581585C2/ru active
- 2011-04-08 PT PT117128819T patent/PT2558448E/pt unknown
- 2011-04-08 PE PE2012002008A patent/PE20130181A1/es active IP Right Grant
- 2011-04-08 PE PE2016000780A patent/PE20160838A1/es unknown
- 2011-04-08 HR HRP20150885TT patent/HRP20150885T1/hr unknown
- 2011-04-08 JP JP2013504206A patent/JP5934182B2/ja active Active
- 2011-04-08 CU CU20120147A patent/CU24123B1/es active IP Right Grant
- 2011-04-08 MA MA35304A patent/MA34156B1/fr unknown
- 2011-04-08 HU HUE11712881A patent/HUE026821T2/en unknown
- 2011-04-08 DK DK11712881.9T patent/DK2558448T3/en active
- 2011-04-08 NZ NZ602997A patent/NZ602997A/en unknown
- 2011-04-08 AU AU2011240113A patent/AU2011240113B2/en active Active
- 2011-04-13 JO JOP/2011/0125A patent/JO3158B1/ar active
- 2011-04-14 TW TW100112905A patent/TWI475992B/zh active
- 2011-04-14 TW TW103141317A patent/TWI539951B/zh active
- 2011-08-04 UA UAA201212983A patent/UA110613C2/uk unknown
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2012
- 2012-10-08 EC ECSP12012234 patent/ECSP12012234A/es unknown
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- 2012-10-11 IL IL222348A patent/IL222348B/en active IP Right Grant
- 2012-10-12 TN TNP2012000492A patent/TN2012000492A1/en unknown
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- 2012-10-12 CO CO12180992A patent/CO6630136A2/es not_active Application Discontinuation
- 2012-10-16 CR CR20120526A patent/CR20120526A/es unknown
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2014
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2015
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2016
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2017
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2019
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2021
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