JP2018504441A5 - - Google Patents
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- Publication number
- JP2018504441A5 JP2018504441A5 JP2017541694A JP2017541694A JP2018504441A5 JP 2018504441 A5 JP2018504441 A5 JP 2018504441A5 JP 2017541694 A JP2017541694 A JP 2017541694A JP 2017541694 A JP2017541694 A JP 2017541694A JP 2018504441 A5 JP2018504441 A5 JP 2018504441A5
- Authority
- JP
- Japan
- Prior art keywords
- alkylene
- alkyl
- alkynylene
- substituted
- halo
- 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.)
- Pending
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- 125000000217 alkyl group Chemical group 0.000 claims description 80
- 125000003161 (C1-C6) alkylene group Chemical group 0.000 claims description 76
- 125000006591 (C2-C6) alkynylene group Chemical group 0.000 claims description 49
- 150000001875 compounds Chemical class 0.000 claims description 26
- 125000003118 aryl group Chemical group 0.000 claims description 17
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims description 16
- 125000005843 halogen group Chemical group 0.000 claims description 15
- 125000001072 heteroaryl group Chemical group 0.000 claims description 13
- 125000001424 substituent group Chemical group 0.000 claims description 13
- 229910052731 fluorine Inorganic materials 0.000 claims description 11
- 125000001153 fluoro group Chemical group F* 0.000 claims description 11
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims description 8
- 229910052799 carbon Inorganic materials 0.000 claims description 8
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 8
- 125000006376 (C3-C10) cycloalkyl group Chemical group 0.000 claims description 7
- 125000003107 substituted aryl group Chemical group 0.000 claims description 7
- 125000006651 (C3-C20) cycloalkyl group Chemical group 0.000 claims description 6
- 201000010099 disease Diseases 0.000 claims description 5
- 229910052739 hydrogen Inorganic materials 0.000 claims description 5
- 150000003839 salts Chemical class 0.000 claims description 5
- 239000012453 solvate Substances 0.000 claims description 5
- 229910052717 sulfur Inorganic materials 0.000 claims description 5
- 229910052736 halogen Inorganic materials 0.000 claims description 4
- 150000002367 halogens Chemical class 0.000 claims description 4
- 229910052760 oxygen Inorganic materials 0.000 claims description 4
- 208000035475 disorder Diseases 0.000 claims description 3
- 125000002947 alkylene group Chemical group 0.000 claims description 2
- 125000005218 alkyleneheteroaryl group Chemical group 0.000 claims description 2
- 239000003085 diluting agent Substances 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 102000052116 epidermal growth factor receptor activity proteins Human genes 0.000 claims description 2
- 108700015053 epidermal growth factor receptor activity proteins Proteins 0.000 claims description 2
- 230000001404 mediated effect Effects 0.000 claims description 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 description 2
- 239000008194 pharmaceutical composition Substances 0.000 claims description 2
- 239000000651 prodrug Substances 0.000 claims description 2
- 229940002612 prodrug Drugs 0.000 claims description 2
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 description 6
- 239000000126 substance Substances 0.000 description 6
- 229910052801 chlorine Inorganic materials 0.000 description 5
- 238000000034 method Methods 0.000 description 4
- 206010028980 Neoplasm Diseases 0.000 description 2
- 201000011510 cancer Diseases 0.000 description 2
- 230000001613 neoplastic effect Effects 0.000 description 2
- 125000006713 (C5-C10) cycloalkyl group Chemical group 0.000 description 1
- 208000003174 Brain Neoplasms Diseases 0.000 description 1
- 206010006187 Breast cancer Diseases 0.000 description 1
- 208000026310 Breast neoplasm Diseases 0.000 description 1
- 125000000041 C6-C10 aryl group Chemical group 0.000 description 1
- 206010009944 Colon cancer Diseases 0.000 description 1
- 208000008839 Kidney Neoplasms Diseases 0.000 description 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 description 1
- 206010033128 Ovarian cancer Diseases 0.000 description 1
- 206010061535 Ovarian neoplasm Diseases 0.000 description 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 description 1
- 206010060862 Prostate cancer Diseases 0.000 description 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 description 1
- 206010038389 Renal cancer Diseases 0.000 description 1
- 208000000453 Skin Neoplasms Diseases 0.000 description 1
- 125000004419 alkynylene group Chemical group 0.000 description 1
- 208000029742 colonic neoplasm Diseases 0.000 description 1
- 238000010276 construction Methods 0.000 description 1
- 239000003814 drug Substances 0.000 description 1
- 201000010982 kidney cancer Diseases 0.000 description 1
- 201000005202 lung cancer Diseases 0.000 description 1
- 208000020816 lung neoplasm Diseases 0.000 description 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 description 1
- 125000001624 naphthyl group Chemical group 0.000 description 1
- 201000002528 pancreatic cancer Diseases 0.000 description 1
- 208000008443 pancreatic carcinoma Diseases 0.000 description 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 description 1
- 201000000849 skin cancer Diseases 0.000 description 1
- 229940124597 therapeutic agent Drugs 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562111240P | 2015-02-03 | 2015-02-03 | |
| US62/111,240 | 2015-02-03 | ||
| PCT/CA2016/050094 WO2016123706A1 (en) | 2015-02-03 | 2016-02-03 | Novel fluorinated derivatives as egfr inhibitors useful for treating cancers |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2018504441A JP2018504441A (ja) | 2018-02-15 |
| JP2018504441A5 true JP2018504441A5 (enExample) | 2019-03-14 |
Family
ID=56563262
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017541694A Pending JP2018504441A (ja) | 2015-02-03 | 2016-02-03 | 癌の治療に有用なｅｇｆｒ阻害剤としての新規フッ素化誘導体 |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US20180050993A1 (enExample) |
| EP (1) | EP3253739A4 (enExample) |
| JP (1) | JP2018504441A (enExample) |
| AU (1) | AU2016214923A1 (enExample) |
| CA (1) | CA2974442A1 (enExample) |
| WO (1) | WO2016123706A1 (enExample) |
Families Citing this family (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN108069913B (zh) * | 2016-11-18 | 2022-03-01 | 陕西师范大学 | 双(吗啉基烷氧基)喹唑啉衍生物及其在抗肿瘤方面的用途 |
| US20200290978A1 (en) * | 2017-09-26 | 2020-09-17 | The Regents Of The University Of California | Compositions and methods for treating cancer |
| WO2019071351A1 (en) * | 2017-10-12 | 2019-04-18 | Trillium Therapeutics Inc. | NOVEL 4-ARYLOXYQUINAZOLINE FLUORIN DERIVATIVES AS EGFR INHIBITORS USEFUL FOR THE TREATMENT OF CANCERS |
| CN108329276A (zh) * | 2018-04-23 | 2018-07-27 | 江苏兢业制药有限公司 | 杂环衍生物及其制备和用途 |
| KR102871791B1 (ko) | 2018-09-10 | 2025-10-15 | 미라티 테라퓨틱스, 인크. | 병용 요법 |
| EP3670501A1 (en) | 2018-12-17 | 2020-06-24 | Basf Se | Substituted [1,2,4]triazole compounds as fungicides |
| BR112021018295A2 (pt) * | 2019-03-15 | 2021-11-23 | Univ California | Composições e métodos para tratamento de câncer |
| EP3942045A1 (en) | 2019-03-21 | 2022-01-26 | Onxeo | A dbait molecule in combination with kinase inhibitor for the treatment of cancer |
| US12523663B2 (en) | 2019-06-04 | 2026-01-13 | Inserm (Institut National De La Santé Et De La Rescherche Médicale) | Use of CD9 as a biomarker and as a biotarget in glomerulonephritis or glomerulosclerosis |
| KR20220042293A (ko) | 2019-08-05 | 2022-04-05 | 베이징 즈지엔진루이 셩우이야오 커지 요우시엔공스 | 질소 함유 다환 축합 고리계 화합물, 이의 약학 조성물, 제조 방법 및 용도 |
| TWI883039B (zh) * | 2019-09-13 | 2025-05-11 | 日商明治股份有限公司 | 固形食品及固形乳 |
| EP4054579A1 (en) | 2019-11-08 | 2022-09-14 | Institut National de la Santé et de la Recherche Médicale (INSERM) | Methods for the treatment of cancers that have acquired resistance to kinase inhibitors |
| WO2021148581A1 (en) | 2020-01-22 | 2021-07-29 | Onxeo | Novel dbait molecule and its use |
| CN112125890B (zh) * | 2020-09-25 | 2022-12-06 | 华东理工大学 | 一种含异吲哚酮基喹唑啉基羧酸酯类衍生物及其应用 |
| EP4405360A4 (en) | 2021-09-23 | 2025-08-20 | Erasca Inc | POLYMORPHIC FORMS OF EGFR INHIBITOR |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5747498A (en) * | 1996-05-28 | 1998-05-05 | Pfizer Inc. | Alkynyl and azido-substituted 4-anilinoquinazolines |
| US6251912B1 (en) * | 1997-08-01 | 2001-06-26 | American Cyanamid Company | Substituted quinazoline derivatives |
| RS49779B (sr) * | 1998-01-12 | 2008-06-05 | Glaxo Group Limited, | Biciklična heteroaromatična jedinjenja kao inhibitori protein tirozin kinaze |
| ES2400339T3 (es) * | 2002-07-15 | 2013-04-09 | Symphony Evolution, Inc. | Compuestos, composiciones farmacéuticas de los mismos y su uso en el tratamiento del cáncer |
| KR20050122199A (ko) * | 2003-01-23 | 2005-12-28 | 티.케이. 시그널 리미티드 | 표피성장인자 수용체 티로신 키나제의 비가역성 억제제 및 그의 용도 |
| WO2006071079A1 (en) * | 2004-12-29 | 2006-07-06 | Hanmi Pharm. Co., Ltd. | Quinazoline derivatives for inhibiting cancer cell growth and method for the preparation thereof |
| KR20070107151A (ko) * | 2005-02-26 | 2007-11-06 | 아스트라제네카 아베 | 티로신 키나제 억제제로서의 퀴나졸린 유도체 |
| WO2007029251A2 (en) * | 2005-09-06 | 2007-03-15 | T.K. Signal Ltd. | Polyalkylene glycol derivatives of 4- (phenylamino)quinazolines useful as irreversible inhibitors of epidermal gr0wth fact0r receptor tyrosine kinase |
| EP2346507A1 (en) * | 2008-09-03 | 2011-07-27 | Boehringer Ingelheim International GmbH | Use of quinazoline derivatives for the treatment of viral diseases |
| TWI577671B (zh) * | 2011-11-14 | 2017-04-11 | Sunshine Lake Pharma Co Ltd | Aminoquinazoline derivatives and salts thereof and methods of use thereof |
| CN104119351A (zh) * | 2013-04-27 | 2014-10-29 | 复旦大学 | 4-(3-氯-4-氟苯基氨基)-7-甲氧基-喹唑啉化合物及其制备方法和用途 |
-
2016
- 2016-02-03 EP EP16746032.8A patent/EP3253739A4/en not_active Withdrawn
- 2016-02-03 WO PCT/CA2016/050094 patent/WO2016123706A1/en not_active Ceased
- 2016-02-03 US US15/546,309 patent/US20180050993A1/en not_active Abandoned
- 2016-02-03 CA CA2974442A patent/CA2974442A1/en not_active Abandoned
- 2016-02-03 JP JP2017541694A patent/JP2018504441A/ja active Pending
- 2016-02-03 AU AU2016214923A patent/AU2016214923A1/en not_active Abandoned