JP2017537114A5 - - Google Patents
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- Publication number
- JP2017537114A5 JP2017537114A5 JP2017530208A JP2017530208A JP2017537114A5 JP 2017537114 A5 JP2017537114 A5 JP 2017537114A5 JP 2017530208 A JP2017530208 A JP 2017530208A JP 2017530208 A JP2017530208 A JP 2017530208A JP 2017537114 A5 JP2017537114 A5 JP 2017537114A5
- Authority
- JP
- Japan
- Prior art keywords
- cancer
- pharmaceutically acceptable
- acceptable salt
- prodrug
- solvate
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
- -1 1H-indole-3-yl Chemical group 0.000 claims 17
- 150000003839 salts Chemical class 0.000 claims 12
- 239000000651 prodrug Substances 0.000 claims 11
- 229940002612 prodrug Drugs 0.000 claims 11
- 239000012453 solvate Substances 0.000 claims 11
- 150000001875 compounds Chemical class 0.000 claims 10
- 229910052739 hydrogen Inorganic materials 0.000 claims 10
- 239000001257 hydrogen Substances 0.000 claims 10
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 5
- 125000000217 alkyl group Chemical group 0.000 claims 5
- 150000002431 hydrogen Chemical class 0.000 claims 5
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 4
- 229910052736 halogen Inorganic materials 0.000 claims 4
- 150000002367 halogens Chemical class 0.000 claims 4
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 3
- 229910052760 oxygen Inorganic materials 0.000 claims 3
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 208000035475 disorder Diseases 0.000 claims 2
- 102000052116 epidermal growth factor receptor activity proteins Human genes 0.000 claims 2
- 108700015053 epidermal growth factor receptor activity proteins Proteins 0.000 claims 2
- 239000000203 mixture Substances 0.000 claims 2
- YOHYSYJDKVYCJI-UHFFFAOYSA-N n-[3-[[6-[3-(trifluoromethyl)anilino]pyrimidin-4-yl]amino]phenyl]cyclopropanecarboxamide Chemical compound FC(F)(F)C1=CC=CC(NC=2N=CN=C(NC=3C=C(NC(=O)C4CC4)C=CC=3)C=2)=C1 YOHYSYJDKVYCJI-UHFFFAOYSA-N 0.000 claims 2
- 239000001301 oxygen Substances 0.000 claims 2
- 229910052717 sulfur Inorganic materials 0.000 claims 2
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 2
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 1
- CSUGQXMRKOKBFI-UHFFFAOYSA-N 1-methylindazole Chemical compound C1=CC=C2N(C)N=CC2=C1 CSUGQXMRKOKBFI-UHFFFAOYSA-N 0.000 claims 1
- 125000004484 1-methylpiperidin-4-yl group Chemical group CN1CCC(CC1)* 0.000 claims 1
- 125000003006 2-dimethylaminoethyl group Chemical group [H]C([H])([H])N(C([H])([H])[H])C([H])([H])C([H])([H])* 0.000 claims 1
- 206010005003 Bladder cancer Diseases 0.000 claims 1
- 206010005949 Bone cancer Diseases 0.000 claims 1
- 208000018084 Bone neoplasm Diseases 0.000 claims 1
- 208000003174 Brain Neoplasms Diseases 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 206010008342 Cervix carcinoma Diseases 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 102000001301 EGF receptor Human genes 0.000 claims 1
- 108060006698 EGF receptor Proteins 0.000 claims 1
- 208000000461 Esophageal Neoplasms Diseases 0.000 claims 1
- 208000008839 Kidney Neoplasms Diseases 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 206010025323 Lymphomas Diseases 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 206010030155 Oesophageal carcinoma Diseases 0.000 claims 1
- 206010033128 Ovarian cancer Diseases 0.000 claims 1
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 1
- 208000015634 Rectal Neoplasms Diseases 0.000 claims 1
- 206010038389 Renal cancer Diseases 0.000 claims 1
- 208000000453 Skin Neoplasms Diseases 0.000 claims 1
- 208000005718 Stomach Neoplasms Diseases 0.000 claims 1
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 1
- 208000024770 Thyroid neoplasm Diseases 0.000 claims 1
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims 1
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims 1
- 230000003213 activating effect Effects 0.000 claims 1
- 239000002671 adjuvant Substances 0.000 claims 1
- 201000005188 adrenal gland cancer Diseases 0.000 claims 1
- 208000024447 adrenal gland neoplasm Diseases 0.000 claims 1
- 125000003545 alkoxy group Chemical group 0.000 claims 1
- 125000002393 azetidinyl group Chemical group 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 201000010881 cervical cancer Diseases 0.000 claims 1
- 208000029742 colonic neoplasm Diseases 0.000 claims 1
- 125000004093 cyano group Chemical group *C#N 0.000 claims 1
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 claims 1
- 230000037430 deletion Effects 0.000 claims 1
- 238000012217 deletion Methods 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 201000004101 esophageal cancer Diseases 0.000 claims 1
- 206010017758 gastric cancer Diseases 0.000 claims 1
- 201000010536 head and neck cancer Diseases 0.000 claims 1
- 208000014829 head and neck neoplasm Diseases 0.000 claims 1
- 125000000623 heterocyclic group Chemical group 0.000 claims 1
- 125000000814 indol-3-yl group Chemical group [H]C1=C([H])C([H])=C2N([H])C([H])=C([*])C2=C1[H] 0.000 claims 1
- 201000010982 kidney cancer Diseases 0.000 claims 1
- 201000007270 liver cancer Diseases 0.000 claims 1
- 208000014018 liver neoplasm Diseases 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 201000001441 melanoma Diseases 0.000 claims 1
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 claims 1
- 230000035772 mutation Effects 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 125000003386 piperidinyl group Chemical group 0.000 claims 1
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 1
- 206010038038 rectal cancer Diseases 0.000 claims 1
- 201000001275 rectum cancer Diseases 0.000 claims 1
- 201000000849 skin cancer Diseases 0.000 claims 1
- 201000011549 stomach cancer Diseases 0.000 claims 1
- 239000011593 sulfur Chemical group 0.000 claims 1
- 208000013076 thyroid tumor Diseases 0.000 claims 1
- 201000005112 urinary bladder cancer Diseases 0.000 claims 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201462090869P | 2014-12-11 | 2014-12-11 | |
| US62/090,869 | 2014-12-11 | ||
| US201562166883P | 2015-05-27 | 2015-05-27 | |
| US62/166,883 | 2015-05-27 | ||
| PCT/US2015/065286 WO2016094821A2 (en) | 2014-12-11 | 2015-12-11 | Substituted 2-anilinopyrimidine derivatives as egfr modulators |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020090467A Division JP7181558B2 (ja) | 2014-12-11 | 2020-05-25 | Ｅｇｆｒモジュレーターとしての置換２－アミノピリミジン誘導体 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2017537114A JP2017537114A (ja) | 2017-12-14 |
| JP2017537114A5 true JP2017537114A5 (enExample) | 2019-01-17 |
| JP6709786B2 JP6709786B2 (ja) | 2020-06-17 |
Family
ID=56108380
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017530208A Active JP6709786B2 (ja) | 2014-12-11 | 2015-12-11 | Ｅｇｆｒモジュレーターとしての置換２−アミノピリミジン誘導体 |
| JP2020090467A Active JP7181558B2 (ja) | 2014-12-11 | 2020-05-25 | Ｅｇｆｒモジュレーターとしての置換２－アミノピリミジン誘導体 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020090467A Active JP7181558B2 (ja) | 2014-12-11 | 2020-05-25 | Ｅｇｆｒモジュレーターとしての置換２－アミノピリミジン誘導体 |
Country Status (17)
| Country | Link |
|---|---|
| US (2) | US10590111B2 (enExample) |
| EP (1) | EP3229798A4 (enExample) |
| JP (2) | JP6709786B2 (enExample) |
| KR (1) | KR20170098865A (enExample) |
| CN (3) | CN112375067B (enExample) |
| AU (1) | AU2015360360B2 (enExample) |
| BR (1) | BR112017012272A2 (enExample) |
| CA (1) | CA2970185C (enExample) |
| CO (1) | CO2017006962A2 (enExample) |
| EA (1) | EA036453B1 (enExample) |
| HK (1) | HK1245634A1 (enExample) |
| IL (1) | IL252554A0 (enExample) |
| MX (1) | MX382869B (enExample) |
| PH (1) | PH12017501057A1 (enExample) |
| SG (2) | SG11201704685TA (enExample) |
| TW (1) | TWI618704B (enExample) |
| WO (1) | WO2016094821A2 (enExample) |
Families Citing this family (26)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN111170998B (zh) | 2014-11-05 | 2023-04-11 | 益方生物科技(上海)股份有限公司 | 嘧啶或吡啶类化合物、其制备方法和医药用途 |
| US10590111B2 (en) * | 2014-12-11 | 2020-03-17 | Beta Pharma, Inc. | Substituted 2-anilinopyrimidine derivatives as EGFR modulators |
| US11052086B2 (en) * | 2016-05-11 | 2021-07-06 | Beta Pharma, Inc. | 2-anilinopyrimidine derivatives as therapeutic agents for treatment of brain cancers |
| CN109311858B (zh) | 2016-05-26 | 2021-12-03 | 里科瑞尔姆Ip控股有限责任公司 | Egfr抑制剂化合物 |
| EP3471730B1 (en) | 2016-06-17 | 2021-10-20 | Beta Pharma, Inc. | Pharmaceutical salts of n-(2-(2-(dimethylamino)ethoxy)-4-methoxy-5-((4-(1-methyl-1h-indol-3-yl)pyrimidin-2-yl)amino)phenyl)acrylamide and crystalline forms thereof |
| CN106243044A (zh) * | 2016-06-30 | 2016-12-21 | 浙江大学 | 含卤代丙烯酰胺侧链的嘧啶类衍生物及制备和应用 |
| CN108602802B (zh) * | 2016-07-26 | 2020-01-21 | 深圳市塔吉瑞生物医药有限公司 | 用于抑制蛋白酪氨酸激酶活性的氨基嘧啶类化合物 |
| MX2019015177A (es) * | 2017-06-16 | 2020-02-07 | Beta Pharma Inc | Formulaciones farmaceuticas de n-(2-(2-(dimetilamino)etoxi)-4-meto xi-5((4-(1-metil-1h-indol-3-il)pirimidin-2-il)amino)fenil)acrilam ida y las sales de ellas. |
| CN109503573A (zh) * | 2017-09-14 | 2019-03-22 | 昆明圣加南生物科技有限公司 | 2-取代苯胺基嘧啶衍生物及其用途 |
| CN107935995A (zh) * | 2017-11-28 | 2018-04-20 | 中山大学 | 一种新型2‑苯胺基嘧啶衍生物及其在制备抗肿瘤药物中的应用 |
| CN108017633A (zh) * | 2018-01-30 | 2018-05-11 | 天津大学 | N-[5-(嘧啶-2-氨基)-2,4-二取代苯基]-2-氟代丙烯酰胺衍生物及应用 |
| PT3806898T (pt) * | 2018-06-18 | 2025-12-02 | UCB Biopharma SRL | Antagonista de gremlin-1 para utilização no tratamento do cancro |
| IL281344B2 (en) | 2018-09-10 | 2025-09-01 | Mirati Therapeutics Inc | Combination of adagrasib and cetuximab for cancer treatment |
| US12390464B2 (en) | 2019-09-23 | 2025-08-19 | Beta Pharma, Inc. | Treatment of EGFR mutant-related cancers using a combination of EGFR and CDK4/6 inhibitors |
| WO2021094379A1 (en) | 2019-11-12 | 2021-05-20 | Astrazeneca Ab | Epidermal growth factor receptor tyrosine kinase inhibitors for the treatment of cancer |
| CA3166980A1 (en) | 2020-01-20 | 2021-07-29 | Astrazeneca Ab | Epidermal growth factor receptor tyrosine kinase inhibitors for the treatment of cancer |
| US20210369709A1 (en) | 2020-05-27 | 2021-12-02 | Astrazeneca Ab | EGFR TKIs FOR USE IN THE TREATMENT OF NON-SMALL CELL LUNG CANCER |
| US20250136576A1 (en) * | 2021-07-13 | 2025-05-01 | ACEA Therapeutics, Inc. | Heterocyclic Compounds and Uses Thereof |
| CN119278041A (zh) | 2022-03-31 | 2025-01-07 | 阿斯利康(瑞典)有限公司 | 用于治疗癌症的与akt抑制剂组合的表皮生长因子受体（egfr）酪氨酸激酶抑制剂 |
| WO2023209090A1 (en) | 2022-04-28 | 2023-11-02 | Astrazeneca Ab | Bicyclic heteroaromatic compounds and their application in the treatment of cancer |
| WO2023209088A1 (en) | 2022-04-28 | 2023-11-02 | Astrazeneca Ab | Bicyclic heteroaromatic compounds and their use in the treatment of cancer |
| US20240116926A1 (en) | 2022-04-28 | 2024-04-11 | Astrazeneca Ab | Heteroaromatic compounds |
| AU2023262556A1 (en) | 2022-04-28 | 2024-12-05 | Astrazeneca Ab | Condensed bicyclic heteroaromatic compounds and their use in the treatment of cancer |
| MA71241A (fr) | 2022-06-27 | 2025-04-30 | Astrazeneca Ab | Combinaisons impliquant des inhibiteurs de tyrosine kinase du récepteur du facteur de croissance épidermique pour traiter le cancer |
| JP2025522965A (ja) | 2022-07-08 | 2025-07-17 | アストラゼネカ・アクチエボラーグ | 癌の治療のためのｈｇｆ受容体阻害剤と組み合わせた上皮成長因子受容体チロシンキナーゼ阻害剤 |
| WO2025238661A1 (en) * | 2024-05-17 | 2025-11-20 | Bdr Lifesciences Private Limited | An improved process for the preparation of osimertinib |
Family Cites Families (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2001047922A2 (en) * | 1999-12-24 | 2001-07-05 | Aventis Pharma Limited | Azaindoles |
| GB0115109D0 (en) | 2001-06-21 | 2001-08-15 | Aventis Pharma Ltd | Chemical compounds |
| JP5179509B2 (ja) * | 2006-12-08 | 2013-04-10 | エフ．ホフマン−ラ ロシュ アーゲー | 置換ピリミジン類及びｊｎｋモジュレーターとしてのこれらの使用 |
| WO2010059711A1 (en) * | 2008-11-18 | 2010-05-27 | Wisconsin Alumni Research Foundation | Sigma-1 receptor ligands and methods of use |
| JP5918693B2 (ja) | 2009-05-05 | 2016-05-18 | ダナ ファーバー キャンサー インスティテュート インコーポレイテッド | Ｅｇｆｒ阻害剤及び疾患の治療方法 |
| BR112013027734A2 (pt) * | 2011-05-04 | 2017-08-08 | Ariad Pharma Inc | compostos para a inibição de proliferação celular em cânceres impulsionados pelo egfr, método e composição farmacêutica |
| EP2736895B1 (en) * | 2011-07-27 | 2016-01-06 | Astrazeneca AB | 2-(2,4,5-substituted-anilino) pyrimidine derivatives as egfr modulators useful for treating cancer |
| AU2013204563B2 (en) * | 2012-05-05 | 2016-05-19 | Takeda Pharmaceutical Company Limited | Compounds for inhibiting cell proliferation in EGFR-driven cancers |
| CN104860941B (zh) | 2014-02-25 | 2017-03-22 | 上海海雁医药科技有限公司 | 2,4‑二取代苯‑1,5‑二胺衍生物及其应用以及由其制备的药物组合物和药用组合物 |
| PE20170268A1 (es) | 2014-06-19 | 2017-04-21 | Ariad Pharma Inc | Compuestos de heteroarilo para la inhibicion de cinasa |
| CN106458969A (zh) * | 2014-08-25 | 2017-02-22 | 四川海思科制药有限公司 | 一种(取代的苯基)(取代的嘧啶)胺基衍生物及其制备方法和药物用途 |
| CN105461695B (zh) * | 2014-09-29 | 2018-03-27 | 齐鲁制药有限公司 | 嘧啶或三嗪衍生物及其制备方法和用途 |
| CN111170998B (zh) | 2014-11-05 | 2023-04-11 | 益方生物科技(上海)股份有限公司 | 嘧啶或吡啶类化合物、其制备方法和医药用途 |
| US10590111B2 (en) * | 2014-12-11 | 2020-03-17 | Beta Pharma, Inc. | Substituted 2-anilinopyrimidine derivatives as EGFR modulators |
-
2015
- 2015-12-11 US US15/534,838 patent/US10590111B2/en active Active
- 2015-12-11 CN CN202011112988.2A patent/CN112375067B/zh active Active
- 2015-12-11 JP JP2017530208A patent/JP6709786B2/ja active Active
- 2015-12-11 MX MX2017007664A patent/MX382869B/es unknown
- 2015-12-11 TW TW104141810A patent/TWI618704B/zh not_active IP Right Cessation
- 2015-12-11 SG SG11201704685TA patent/SG11201704685TA/en unknown
- 2015-12-11 CN CN201580067776.8A patent/CN108024993B/zh active Active
- 2015-12-11 EA EA201790921A patent/EA036453B1/ru unknown
- 2015-12-11 KR KR1020177019147A patent/KR20170098865A/ko not_active Ceased
- 2015-12-11 CA CA2970185A patent/CA2970185C/en active Active
- 2015-12-11 HK HK18104991.1A patent/HK1245634A1/zh unknown
- 2015-12-11 BR BR112017012272-3A patent/BR112017012272A2/pt not_active IP Right Cessation
- 2015-12-11 EP EP15867768.2A patent/EP3229798A4/en not_active Ceased
- 2015-12-11 AU AU2015360360A patent/AU2015360360B2/en active Active
- 2015-12-11 WO PCT/US2015/065286 patent/WO2016094821A2/en not_active Ceased
- 2015-12-11 CN CN202011112986.3A patent/CN112457298B/zh active Active
- 2015-12-11 SG SG10201909060S patent/SG10201909060SA/en unknown
-
2017
- 2017-05-28 IL IL252554A patent/IL252554A0/en active IP Right Grant
- 2017-06-07 PH PH12017501057A patent/PH12017501057A1/en unknown
- 2017-07-11 CO CONC2017/0006962A patent/CO2017006962A2/es unknown
-
2020
- 2020-03-16 US US16/819,539 patent/US11414401B2/en active Active
- 2020-05-25 JP JP2020090467A patent/JP7181558B2/ja active Active
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