JP2019504830A5 - - Google Patents
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- Publication number
- JP2019504830A5 JP2019504830A5 JP2018535293A JP2018535293A JP2019504830A5 JP 2019504830 A5 JP2019504830 A5 JP 2019504830A5 JP 2018535293 A JP2018535293 A JP 2018535293A JP 2018535293 A JP2018535293 A JP 2018535293A JP 2019504830 A5 JP2019504830 A5 JP 2019504830A5
- Authority
- JP
- Japan
- Prior art keywords
- enamide
- quinazolin
- difluoromethoxy
- ethoxy
- chloro
- 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.)
- Withdrawn
Links
- 150000001875 compounds Chemical class 0.000 claims 11
- -1 3,4-dichloro-2-fluoro-anilino Chemical group 0.000 claims 7
- 125000004786 difluoromethoxy group Chemical group [H]C(F)(F)O* 0.000 claims 6
- 125000001301 ethoxy group Chemical group [H]C([H])([H])C([H])([H])O* 0.000 claims 5
- 150000003839 salts Chemical class 0.000 claims 5
- 239000012453 solvate Substances 0.000 claims 4
- 206010028980 Neoplasm Diseases 0.000 claims 3
- 201000011510 cancer Diseases 0.000 claims 3
- 125000004547 quinazolin-6-yl group Chemical group N1=CN=CC2=CC(=CC=C12)* 0.000 claims 3
- 239000000126 substance Substances 0.000 claims 2
- RFCGQJYRNUPTAE-OWOJBTEDSA-N (E)-N-[4-(3,4-dichloro-2-fluoroanilino)-7-[2-(difluoromethoxy)ethoxy]quinazolin-6-yl]-4-morpholin-4-ylbut-2-enamide Chemical compound ClC=1C(=C(NC2=NC=NC3=CC(=C(C=C23)NC(\C=C\CN2CCOCC2)=O)OCCOC(F)F)C=CC=1Cl)F RFCGQJYRNUPTAE-OWOJBTEDSA-N 0.000 claims 1
- MYWRPXUKZOLUKT-OWOJBTEDSA-N (E)-N-[4-(3-chloro-2,4-difluoroanilino)-7-[2-(difluoromethoxy)ethoxy]quinazolin-6-yl]-4-morpholin-4-ylbut-2-enamide Chemical compound ClC=1C(=C(NC2=NC=NC3=CC(=C(C=C23)NC(\C=C\CN2CCOCC2)=O)OCCOC(F)F)C=CC=1F)F MYWRPXUKZOLUKT-OWOJBTEDSA-N 0.000 claims 1
- RPPREQFUNVYPGV-QPJJXVBHSA-N (E)-N-[4-(3-chloro-2-fluoroanilino)-7-[2-(difluoromethoxy)ethoxy]quinazolin-6-yl]-4-(dimethylamino)but-2-enamide Chemical compound ClC=1C(=C(NC2=NC=NC3=CC(=C(C=C23)NC(\C=C\CN(C)C)=O)OCCOC(F)F)C=CC=1)F RPPREQFUNVYPGV-QPJJXVBHSA-N 0.000 claims 1
- CYCKFMRTMXLGCG-GORDUTHDSA-N (E)-N-[4-(3-chloro-2-fluoroanilino)-7-[2-(difluoromethoxy)ethoxy]quinazolin-6-yl]-4-morpholin-4-ylbut-2-enamide Chemical compound ClC=1C(=C(NC2=NC=NC3=CC(=C(C=C23)NC(\C=C\CN2CCOCC2)=O)OCCOC(F)F)C=CC=1)F CYCKFMRTMXLGCG-GORDUTHDSA-N 0.000 claims 1
- ISLGYGZBXJDBJW-QPJJXVBHSA-N (E)-N-[4-(3-chloro-2-fluorophenoxy)-7-[2-(difluoromethoxy)ethoxy]quinazolin-6-yl]-4-(dimethylamino)but-2-enamide Chemical compound ClC=1C(=C(OC2=NC=NC3=CC(=C(C=C23)NC(\C=C\CN(C)C)=O)OCCOC(F)F)C=CC=1)F ISLGYGZBXJDBJW-QPJJXVBHSA-N 0.000 claims 1
- XNODREJNPSVHTJ-GORDUTHDSA-N (E)-N-[4-(3-chloro-2-fluorophenoxy)-7-[2-(difluoromethoxy)ethoxy]quinazolin-6-yl]-4-morpholin-4-ylbut-2-enamide Chemical compound ClC=1C(=C(OC2=NC=NC3=CC(=C(C=C23)NC(\C=C\CN2CCOCC2)=O)OCCOC(F)F)C=CC=1)F XNODREJNPSVHTJ-GORDUTHDSA-N 0.000 claims 1
- UCNRKLQQVFEGOV-ONEGZZNKSA-N (E)-N-[4-(3-chloro-4-fluoroanilino)-7-[2-(difluoromethoxy)ethoxy]quinazolin-6-yl]-4-(dimethylamino)but-2-enamide Chemical compound ClC=1C=C(NC2=NC=NC3=CC(=C(C=C23)NC(\C=C\CN(C)C)=O)OCCOC(F)F)C=CC=1F UCNRKLQQVFEGOV-ONEGZZNKSA-N 0.000 claims 1
- RRNISLLSHMITLK-OWOJBTEDSA-N (E)-N-[4-(3-chloro-4-fluoroanilino)-7-[2-(difluoromethoxy)ethoxy]quinazolin-6-yl]-4-morpholin-4-ylbut-2-enamide Chemical compound ClC=1C=C(NC2=NC=NC3=CC(=C(C=C23)NC(\C=C\CN2CCOCC2)=O)OCCOC(F)F)C=CC=1F RRNISLLSHMITLK-OWOJBTEDSA-N 0.000 claims 1
- BWQWWVYMWPULAV-ONEGZZNKSA-N (E)-N-[4-(3-chloro-4-fluorophenoxy)-7-[2-(difluoromethoxy)ethoxy]quinazolin-6-yl]-4-(dimethylamino)but-2-enamide Chemical compound ClC=1C=C(OC2=NC=NC3=CC(=C(C=C23)NC(\C=C\CN(C)C)=O)OCCOC(F)F)C=CC=1F BWQWWVYMWPULAV-ONEGZZNKSA-N 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
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 208000008839 Kidney Neoplasms Diseases 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 206010033128 Ovarian cancer Diseases 0.000 claims 1
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- 206010038389 Renal cancer Diseases 0.000 claims 1
- 208000000453 Skin Neoplasms Diseases 0.000 claims 1
- 208000029742 colonic neoplasm Diseases 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 201000010982 kidney cancer Diseases 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 229940002612 prodrug Drugs 0.000 claims 1
- 239000000651 prodrug Substances 0.000 claims 1
- 201000000849 skin cancer Diseases 0.000 claims 1
- 0 CC=CC(Nc1cc2c(**)ncnc2cc1OCCOC(F)F)=O Chemical compound CC=CC(Nc1cc2c(**)ncnc2cc1OCCOC(F)F)=O 0.000 description 4
- YNAVUWVOSKDBBP-UHFFFAOYSA-N C1NCCOC1 Chemical compound C1NCCOC1 YNAVUWVOSKDBBP-UHFFFAOYSA-N 0.000 description 1
- ZTEVWDIUSGCDHE-UHFFFAOYSA-N CCc(ccc(Cl)c1Cl)c1F Chemical compound CCc(ccc(Cl)c1Cl)c1F ZTEVWDIUSGCDHE-UHFFFAOYSA-N 0.000 description 1
- IKNQPNLSEBWZKX-UHFFFAOYSA-N Cc(cc1Cl)ccc1F Chemical compound Cc(cc1Cl)ccc1F IKNQPNLSEBWZKX-UHFFFAOYSA-N 0.000 description 1
- UTMXAQHUJBHEGB-UHFFFAOYSA-N Cc(ccc(F)c1Cl)c1F Chemical compound Cc(ccc(F)c1Cl)c1F UTMXAQHUJBHEGB-UHFFFAOYSA-N 0.000 description 1
- LHPJOUKIBAEPMW-UHFFFAOYSA-N Cc1cccc(Cl)c1F Chemical compound Cc1cccc(Cl)c1F LHPJOUKIBAEPMW-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662275376P | 2016-01-06 | 2016-01-06 | |
| US62/275,376 | 2016-01-06 | ||
| PCT/CA2017/050015 WO2017117680A1 (en) | 2016-01-06 | 2017-01-06 | Novel fluorinated quinazoline derivatives as egfr inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2019504830A JP2019504830A (ja) | 2019-02-21 |
| JP2019504830A5 true JP2019504830A5 (https=) | 2020-02-20 |
Family
ID=59273095
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018535293A Withdrawn JP2019504830A (ja) | 2016-01-06 | 2017-01-06 | Ｅｇｆｒ阻害剤としての新規フッ素化キナゾリン誘導体 |
Country Status (7)
| Country | Link |
|---|---|
| US (1) | US20190016689A1 (https=) |
| EP (1) | EP3400216A4 (https=) |
| JP (1) | JP2019504830A (https=) |
| CN (1) | CN108779079A (https=) |
| AU (1) | AU2017204973A1 (https=) |
| CA (1) | CA3008312A1 (https=) |
| WO (1) | WO2017117680A1 (https=) |
Families Citing this family (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN111868039A (zh) * | 2017-09-26 | 2020-10-30 | 加利福尼亚大学董事会 | 用于治疗癌症的组合物和方法 |
| KR102809395B1 (ko) | 2019-03-15 | 2025-05-16 | 더 리전트 오브 더 유니버시티 오브 캘리포니아 | 암을 치료하기 위한 조성물 및 방법 |
| EA202192575A1 (ru) | 2019-03-21 | 2022-01-14 | Онксео | Соединения dbait в сочетании с ингибиторами киназ для лечения рака |
| WO2020245208A1 (en) | 2019-06-04 | 2020-12-10 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Use of cd9 as a biomarker and as a biotarget in glomerulonephritis or glomerulosclerosis |
| TWI817018B (zh) | 2019-06-28 | 2023-10-01 | 美商艾瑞生藥股份有限公司 | 用於治療ｂｒａｆ相關的疾病和失調症之化合物 |
| CN114761006A (zh) | 2019-11-08 | 2022-07-15 | Inserm(法国国家健康医学研究院) | 对激酶抑制剂产生耐药性的癌症的治疗方法 |
| JP7832891B2 (ja) * | 2019-12-04 | 2026-03-18 | インサイト・コーポレイション | Ｆｇｆｒ阻害剤の誘導体 |
| WO2021148581A1 (en) | 2020-01-22 | 2021-07-29 | Onxeo | Novel dbait molecule and its use |
| CN111548314B (zh) * | 2020-05-22 | 2021-09-03 | 上海万巷制药有限公司 | 一种n-(3-氯-4-氟苯基)-7-氟-6-硝基-4-喹唑啉胺的生产方法 |
| TW202426436A (zh) | 2020-06-09 | 2024-07-01 | 美商艾瑞生藥股份有限公司 | 用於治療ｂｒａｆ相關的疾病和病症之化合物 |
| CN113264888A (zh) * | 2021-03-04 | 2021-08-17 | 江苏康可得生物技术股份有限公司 | 酪氨酸激酶抑制剂及其药物应用 |
| TWI825637B (zh) | 2021-03-31 | 2023-12-11 | 美商輝瑞股份有限公司 | 啶－１，６（２ｈ，７ｈ）－二酮 |
| EP4405360A4 (en) | 2021-09-23 | 2025-08-20 | Erasca Inc | POLYMORPHIC FORMS OF EGFR INHIBITOR |
| WO2023128350A1 (ko) * | 2021-12-30 | 2023-07-06 | 주식회사 비투에스바이오 | 헤테로아릴 유도체 및 이를 유효성분으로 포함하는 암의 예방 또는 치료용 약학적 조성물 |
| WO2024218632A1 (en) | 2023-04-17 | 2024-10-24 | Array Biopharma Inc. | Erk protein kinase inhibitors |
| CN119241448A (zh) * | 2024-08-16 | 2025-01-03 | 安润医药科技（苏州）有限公司 | 一种酪氨酸激酶抑制剂的可药用盐、晶体、制备方法及其用途 |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR20080095915A (ko) * | 2004-05-06 | 2008-10-29 | 워너-램버트 캄파니 엘엘씨 | 4-페닐아미노-퀴나졸린-6-일-아미드 |
| CN102731485B (zh) * | 2011-04-02 | 2016-06-15 | 齐鲁制药有限公司 | 4-(取代苯氨基)喹唑啉衍生物及其制备方法、药物组合物和用途 |
| CN102838590B (zh) * | 2011-06-21 | 2014-07-09 | 苏州迈泰生物技术有限公司 | 氨基喹唑啉衍生物及其在制备抗恶性肿瘤药物中的用途 |
| CN103874696B (zh) * | 2011-10-12 | 2015-06-03 | 苏州韬略生物科技有限公司 | 作为激酶抑制剂的喹唑啉衍生物及其使用方法 |
| WO2013166952A1 (en) * | 2012-05-07 | 2013-11-14 | Teligene Ltd | Substituted aminoquinazolines useful as kinases inhibitors |
| CN104910140A (zh) * | 2014-03-14 | 2015-09-16 | 齐鲁制药有限公司 | 喹唑啉类化合物、其制备方法及应用 |
| EP3181553B1 (en) * | 2014-08-15 | 2019-12-11 | Arromax Pharmatech Co., Ltd. | Quinazoline derivative, preparation method therefor, and pharmaceutical composition and application thereof |
-
2017
- 2017-01-06 AU AU2017204973A patent/AU2017204973A1/en not_active Abandoned
- 2017-01-06 CA CA3008312A patent/CA3008312A1/en not_active Abandoned
- 2017-01-06 JP JP2018535293A patent/JP2019504830A/ja not_active Withdrawn
- 2017-01-06 EP EP17735790.2A patent/EP3400216A4/en not_active Withdrawn
- 2017-01-06 US US16/066,574 patent/US20190016689A1/en not_active Abandoned
- 2017-01-06 WO PCT/CA2017/050015 patent/WO2017117680A1/en not_active Ceased
- 2017-01-06 CN CN201780015324.4A patent/CN108779079A/zh active Pending
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