MD3658552T2 - Procedeu de obținere a N-(5-((4-(4-((dimetilamino)metil)-3-fenil-1H-pirazol-1-il)pirimidin-2-il)amino)-4-metoxi-2-morfolinofenil)acrilamidei prin prin reacţia aminei corespunzătoare cu clorură de 3-halo-propionil - Google Patents
Procedeu de obținere a N-(5-((4-(4-((dimetilamino)metil)-3-fenil-1H-pirazol-1-il)pirimidin-2-il)amino)-4-metoxi-2-morfolinofenil)acrilamidei prin prin reacţia aminei corespunzătoare cu clorură de 3-halo-propionilInfo
- Publication number
- MD3658552T2 MD3658552T2 MDE20200593T MDE20200593T MD3658552T2 MD 3658552 T2 MD3658552 T2 MD 3658552T2 MD E20200593 T MDE20200593 T MD E20200593T MD E20200593 T MDE20200593 T MD E20200593T MD 3658552 T2 MD3658552 T2 MD 3658552T2
- Authority
- MD
- Moldova
- Prior art keywords
- morpholinophenyl
- pyrazol
- pyrimidin
- acrylamide
- dimethylamino
- Prior art date
Links
- RRMJMHOQSALEJJ-UHFFFAOYSA-N N-[5-[[4-[4-[(dimethylamino)methyl]-3-phenylpyrazol-1-yl]pyrimidin-2-yl]amino]-4-methoxy-2-morpholin-4-ylphenyl]prop-2-enamide Chemical compound CN(C)CC=1C(=NN(C=1)C1=NC(=NC=C1)NC=1C(=CC(=C(C=1)NC(C=C)=O)N1CCOCC1)OC)C1=CC=CC=C1 RRMJMHOQSALEJJ-UHFFFAOYSA-N 0.000 title 1
- 150000001412 amines Chemical class 0.000 title 1
- 238000004519 manufacturing process Methods 0.000 title 1
- 238000000034 method Methods 0.000 abstract 3
- 102000001301 EGF receptor Human genes 0.000 abstract 1
- 108060006698 EGF receptor Proteins 0.000 abstract 1
- 102000001253 Protein Kinase Human genes 0.000 abstract 1
- 150000005005 aminopyrimidines Chemical class 0.000 abstract 1
- 230000002401 inhibitory effect Effects 0.000 abstract 1
- 239000000543 intermediate Substances 0.000 abstract 1
- 108060006633 protein kinase Proteins 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
-
- 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
- C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic System
- C07F7/22—Tin compounds
- C07F7/2284—Compounds with one or more Sn-N linkages
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
-
- 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
- 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
- C07D403/02—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 two hetero rings
- C07D403/04—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 two hetero rings directly linked by a ring-member-to-ring-member bond
Abstract
Prezenta invenţie furnizează un procedeu îmbunătăţit pentru prepararea derivaţilor de aminopirimidină sau a sărurilor acceptabile farmaceutic ale acestora care au o activitate inhibitorie selectivă asupra kinazelor, în special asupra kinazelor proteice pentru receptorii factorului de creştere epidermal. Şi de asemenea, prezenta invenţie furnizează noi intermediari, utili pentru respectivul procedeu, şi procedee pentru preparea acestora.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
KR20170096212 | 2017-07-28 | ||
PCT/KR2018/008379 WO2019022485A1 (en) | 2017-07-28 | 2018-07-25 | IMPROVED PROCESS FOR THE PREPARATION OF AMINOPYRIMIDINE DERIVATIVES |
Publications (1)
Publication Number | Publication Date |
---|---|
MD3658552T2 true MD3658552T2 (ro) | 2024-02-29 |
Family
ID=65040211
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
MDE20200593T MD3658552T2 (ro) | 2017-07-28 | 2018-07-25 | Procedeu de obținere a N-(5-((4-(4-((dimetilamino)metil)-3-fenil-1H-pirazol-1-il)pirimidin-2-il)amino)-4-metoxi-2-morfolinofenil)acrilamidei prin prin reacţia aminei corespunzătoare cu clorură de 3-halo-propionil |
Country Status (31)
Country | Link |
---|---|
US (4) | US10889578B2 (ro) |
EP (1) | EP3658552B1 (ro) |
JP (2) | JP7228562B2 (ro) |
KR (1) | KR20190013553A (ro) |
CN (2) | CN111315742B (ro) |
AU (2) | AU2018308038B2 (ro) |
BR (1) | BR112020001278A2 (ro) |
CA (1) | CA3070069C (ro) |
CO (1) | CO2020000374A2 (ro) |
DK (1) | DK3658552T3 (ro) |
EA (1) | EA202090383A1 (ro) |
ES (1) | ES2962961T3 (ro) |
FI (1) | FI3658552T3 (ro) |
HR (1) | HRP20231191T1 (ro) |
HU (1) | HUE063533T2 (ro) |
IL (2) | IL271973B (ro) |
LT (1) | LT3658552T (ro) |
MA (1) | MA49700B1 (ro) |
MD (1) | MD3658552T2 (ro) |
MX (1) | MX2022008743A (ro) |
NZ (1) | NZ761156A (ro) |
PH (1) | PH12020500059A1 (ro) |
PL (1) | PL3658552T3 (ro) |
PT (1) | PT3658552T (ro) |
RS (1) | RS64654B1 (ro) |
SA (1) | SA520411112B1 (ro) |
SG (1) | SG11201913517UA (ro) |
SI (1) | SI3658552T1 (ro) |
UA (1) | UA125317C2 (ro) |
WO (1) | WO2019022485A1 (ro) |
ZA (1) | ZA202001250B (ro) |
Families Citing this family (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
IL271973B (en) * | 2017-07-28 | 2022-08-01 | Yuhan Corp | An improved process for the preparation of aminopyrimidine derivatives |
JOP20210304A1 (ar) | 2019-05-14 | 2023-01-30 | Janssen Biotech Inc | علاجات مركبة باستخدام الأجسام المضادة ثنائية النوعية المضادة لمستقبل عامل نمو البشرة (EGFR)/ مستقبل عامل نمو خلايا الكبد (c-Met) ومثبطات كيناز التيروسين الخاصة بمستقبل عامل نمو البشرة (EGFR) من الجيل الثالث |
US11850248B2 (en) * | 2019-05-14 | 2023-12-26 | Yuhan Corporation | Therapies with 3rd generation EGFR tyrosine kinase inhibitors |
US11780824B2 (en) * | 2020-12-16 | 2023-10-10 | Scinopharm Taiwan, Ltd. | Process for preparing osimertinib or a salt thereof |
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US5721237A (en) | 1991-05-10 | 1998-02-24 | Rhone-Poulenc Rorer Pharmaceuticals Inc. | Protein tyrosine kinase aryl and heteroaryl quinazoline compounds having selective inhibition of HER-2 autophosphorylation properties |
NZ533118A (en) | 2001-11-27 | 2006-07-28 | Wyeth Corp | 3-cyanoquinolines as inhibitors of EGF-R and HER2 kinases |
GB0305929D0 (en) | 2003-03-14 | 2003-04-23 | Novartis Ag | Organic compounds |
JP2008520612A (ja) | 2004-11-24 | 2008-06-19 | ノバルティス アクチエンゲゼルシャフト | JAK阻害剤およびBcr−Abl、Flt−3、FAKまたはRAFキナーゼ阻害剤のうち少なくとも1個の組合せ |
US20060270600A1 (en) | 2005-05-26 | 2006-11-30 | Eisuke Mekada | Anti-cancer agents |
TW200736232A (en) | 2006-01-26 | 2007-10-01 | Astrazeneca Ab | Pyrimidine derivatives |
ES2633318T3 (es) | 2006-10-23 | 2017-09-20 | Cephalon, Inc. | Derivados bicíclicos fusionados de 2,4-diaminopirimidina como inhibidores de ALK y c-Met |
TW200840581A (en) | 2007-02-28 | 2008-10-16 | Astrazeneca Ab | Novel pyrimidine derivatives |
WO2008124085A2 (en) | 2007-04-03 | 2008-10-16 | Exelixis, Inc. | Methods of using combinations of mek and jak-2 inhibitors |
KR101892989B1 (ko) * | 2008-06-27 | 2018-08-30 | 셀젠 카르 엘엘씨 | 헤테로아릴 화합물 및 이의 용도 |
WO2011046970A1 (en) | 2009-10-12 | 2011-04-21 | Myrexis, Inc. | Amino - pyrimidine compounds as inhibitors of tbkl and/or ikk epsilon |
EA024729B1 (ru) * | 2009-11-13 | 2016-10-31 | Джиноско | Киназные ингибиторы |
CN102762208A (zh) | 2009-12-04 | 2012-10-31 | 赛林药物股份有限公司 | 作为ck2抑制剂的吡唑嘧啶和相关杂环 |
US20130196990A1 (en) | 2010-10-06 | 2013-08-01 | Junya Qu | Benzimidazole Derivatives As PI3 Kinase Inhibitors |
JP5956999B2 (ja) | 2010-11-01 | 2016-07-27 | セルジーン アヴィロミクス リサーチ, インコーポレイテッド | ヘテロアリール化合物およびその使用 |
EP2651939B1 (en) | 2010-12-13 | 2015-04-08 | Array Biopharma, Inc. | SUBSTITUTED N-(1H-INDAZOL-4-YL)IMIDAZO[1,2-a]PYRIDINE-3-CARBOXAMIDE COMPOUNDS AS TYPE III RECEPTOR TYROSINE KINASE INHIBITORS |
CN105254616B (zh) | 2011-07-27 | 2017-10-17 | 阿斯利康(瑞典)有限公司 | 取代的n‑(2‑甲氧基‑5‑硝基苯基)嘧啶‑2‑胺化合物及其盐 |
US20130165464A1 (en) | 2011-12-23 | 2013-06-27 | Millennium Pharmaceuticals, Inc. | Heteroaryls and uses thereof |
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CN106687457B (zh) | 2014-05-13 | 2020-01-10 | 阿里亚德医药股份有限公司 | 用于激酶抑制的杂芳基化合物 |
WO2015188777A1 (en) | 2014-06-12 | 2015-12-17 | Shanghai Fochon Pharmaceutical Co Ltd | Certain protein kinase inhibitors |
AU2015331166B2 (en) * | 2014-10-13 | 2018-04-26 | Yuhan Corporation | Compounds and compositions for modulating EGFR mutant kinase activities |
CN104788427B (zh) * | 2015-02-05 | 2017-05-31 | 上海泓博智源医药股份有限公司 | 3‑(2‑嘧啶氨基)苯基丙烯酰胺类化合物及其应用 |
AR102263A1 (es) | 2015-10-14 | 2017-02-15 | Yuhan Corp | Compuestos y composiciones para la modulación de las actividades quinasa del receptor de egf mutante |
DE102017212159A1 (de) | 2017-07-14 | 2019-01-17 | Krones Aktiengesellschaft | Verfahren und Vorrichtung zur Handhabung von Stückgütern, Artikeln und/oder Gebinden |
IL271973B (en) * | 2017-07-28 | 2022-08-01 | Yuhan Corp | An improved process for the preparation of aminopyrimidine derivatives |
RS64545B1 (sr) | 2017-07-28 | 2023-09-29 | Yuhan Corp | Postupak za pripremu n-(5-(4-(4-formil-3-fenil-1h-pirazol-1-il)pirimidin-2-ilamino)-4-metoksi-2-morfolinofenil)akrilamida |
CN108826170A (zh) | 2018-06-26 | 2018-11-16 | 深圳市远润欣电子有限公司 | 局部全般照明的模式、控制方法及台灯 |
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2018
- 2018-07-25 IL IL271973A patent/IL271973B/en unknown
- 2018-07-25 MD MDE20200593T patent/MD3658552T2/ro unknown
- 2018-07-25 UA UAA202001303A patent/UA125317C2/uk unknown
- 2018-07-25 SG SG11201913517UA patent/SG11201913517UA/en unknown
- 2018-07-25 EA EA202090383A patent/EA202090383A1/ru unknown
- 2018-07-25 LT LTEPPCT/KR2018/008379T patent/LT3658552T/lt unknown
- 2018-07-25 SI SI201830998T patent/SI3658552T1/sl unknown
- 2018-07-25 WO PCT/KR2018/008379 patent/WO2019022485A1/en active Application Filing
- 2018-07-25 HU HUE18837360A patent/HUE063533T2/hu unknown
- 2018-07-25 AU AU2018308038A patent/AU2018308038B2/en active Active
- 2018-07-25 HR HRP20231191TT patent/HRP20231191T1/hr unknown
- 2018-07-25 CA CA3070069A patent/CA3070069C/en active Active
- 2018-07-25 JP JP2020504203A patent/JP7228562B2/ja active Active
- 2018-07-25 PT PT188373609T patent/PT3658552T/pt unknown
- 2018-07-25 BR BR112020001278-5A patent/BR112020001278A2/pt unknown
- 2018-07-25 NZ NZ761156A patent/NZ761156A/en unknown
- 2018-07-25 KR KR1020180086376A patent/KR20190013553A/ko not_active Application Discontinuation
- 2018-07-25 MA MA49700A patent/MA49700B1/fr unknown
- 2018-07-25 PL PL18837360.9T patent/PL3658552T3/pl unknown
- 2018-07-25 CN CN201880048638.9A patent/CN111315742B/zh active Active
- 2018-07-25 FI FIEP18837360.9T patent/FI3658552T3/fi active
- 2018-07-25 US US16/633,684 patent/US10889578B2/en active Active
- 2018-07-25 RS RS20230834A patent/RS64654B1/sr unknown
- 2018-07-25 DK DK18837360.9T patent/DK3658552T3/da active
- 2018-07-25 MX MX2022008743A patent/MX2022008743A/es unknown
- 2018-07-25 EP EP18837360.9A patent/EP3658552B1/en active Active
- 2018-07-25 ES ES18837360T patent/ES2962961T3/es active Active
- 2018-07-25 CN CN202310702453.8A patent/CN116987112A/zh active Pending
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2020
- 2020-01-07 PH PH12020500059A patent/PH12020500059A1/en unknown
- 2020-01-15 CO CONC2020/0000374A patent/CO2020000374A2/es unknown
- 2020-01-21 SA SA520411112A patent/SA520411112B1/ar unknown
- 2020-02-27 ZA ZA2020/01250A patent/ZA202001250B/en unknown
- 2020-12-08 US US17/115,037 patent/US11286253B2/en active Active
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2022
- 2022-03-25 US US17/704,718 patent/US11708362B2/en active Active
- 2022-04-24 IL IL292429A patent/IL292429B2/en unknown
- 2022-05-03 AU AU2022202936A patent/AU2022202936B2/en active Active
- 2022-11-18 JP JP2022184867A patent/JP2023027091A/ja active Pending
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2023
- 2023-06-02 US US18/328,267 patent/US20230312545A1/en active Pending
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