JP2019529444A5 - - Google Patents
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- Publication number
- JP2019529444A5 JP2019529444A5 JP2019515464A JP2019515464A JP2019529444A5 JP 2019529444 A5 JP2019529444 A5 JP 2019529444A5 JP 2019515464 A JP2019515464 A JP 2019515464A JP 2019515464 A JP2019515464 A JP 2019515464A JP 2019529444 A5 JP2019529444 A5 JP 2019529444A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- cancer
- compound
- bond
- cycloalkyl
- 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
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- 125000000217 alkyl group Chemical group 0.000 claims description 64
- 125000000623 heterocyclic group Chemical group 0.000 claims description 37
- 150000001875 compounds Chemical class 0.000 claims description 29
- 229910052736 halogen Inorganic materials 0.000 claims description 23
- 150000002367 halogens Chemical class 0.000 claims description 23
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 20
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 13
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims description 12
- 229910052799 carbon Inorganic materials 0.000 claims description 12
- 150000003839 salts Chemical class 0.000 claims description 8
- 239000008194 pharmaceutical composition Substances 0.000 claims description 7
- 108091008794 FGF receptors Proteins 0.000 claims description 5
- 201000010099 disease Diseases 0.000 claims description 5
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 5
- 102000052178 fibroblast growth factor receptor activity proteins Human genes 0.000 claims description 5
- 206010006187 Breast cancer Diseases 0.000 claims description 4
- 208000026310 Breast neoplasm Diseases 0.000 claims description 4
- 208000005718 Stomach Neoplasms Diseases 0.000 claims description 4
- 125000002993 cycloalkylene group Chemical group 0.000 claims description 4
- 206010017758 gastric cancer Diseases 0.000 claims description 4
- 201000007270 liver cancer Diseases 0.000 claims description 4
- 208000014018 liver neoplasm Diseases 0.000 claims description 4
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims description 4
- 201000011549 stomach cancer Diseases 0.000 claims description 4
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims description 4
- 125000003161 (C1-C6) alkylene group Chemical group 0.000 claims description 3
- 206010005003 Bladder cancer Diseases 0.000 claims description 3
- 206010028980 Neoplasm Diseases 0.000 claims description 3
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims description 3
- 201000005112 urinary bladder cancer Diseases 0.000 claims description 3
- 206010009944 Colon cancer Diseases 0.000 claims description 2
- 206010014733 Endometrial cancer Diseases 0.000 claims description 2
- 206010014759 Endometrial neoplasm Diseases 0.000 claims description 2
- 208000000461 Esophageal Neoplasms Diseases 0.000 claims description 2
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims description 2
- 208000034578 Multiple myelomas Diseases 0.000 claims description 2
- 206010030155 Oesophageal carcinoma Diseases 0.000 claims description 2
- 206010033128 Ovarian cancer Diseases 0.000 claims description 2
- 206010061535 Ovarian neoplasm Diseases 0.000 claims description 2
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims description 2
- 206010035226 Plasma cell myeloma Diseases 0.000 claims description 2
- 206010060862 Prostate cancer Diseases 0.000 claims description 2
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims description 2
- 208000006265 Renal cell carcinoma Diseases 0.000 claims description 2
- 208000033749 Small cell carcinoma of the bladder Diseases 0.000 claims description 2
- 201000011510 cancer Diseases 0.000 claims description 2
- 208000029742 colonic neoplasm Diseases 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 201000004101 esophageal cancer Diseases 0.000 claims description 2
- 201000005202 lung cancer Diseases 0.000 claims description 2
- 208000020816 lung neoplasm Diseases 0.000 claims description 2
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims description 2
- 201000001441 melanoma Diseases 0.000 claims description 2
- 201000002528 pancreatic cancer Diseases 0.000 claims description 2
- 208000008443 pancreatic carcinoma Diseases 0.000 claims description 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 2
- 201000009410 rhabdomyosarcoma Diseases 0.000 claims description 2
- 201000007710 urinary bladder small cell neuroendocrine carcinoma Diseases 0.000 claims description 2
- 206010008342 Cervix carcinoma Diseases 0.000 claims 1
- WTKZEGDFNFYCGP-UHFFFAOYSA-N Pyrazole Chemical compound C=1C=NNC=1 WTKZEGDFNFYCGP-UHFFFAOYSA-N 0.000 claims 1
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims 1
- 201000010881 cervical cancer Diseases 0.000 claims 1
- 208000015347 renal cell adenocarcinoma Diseases 0.000 claims 1
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 description 7
- 239000000203 mixture Substances 0.000 description 6
- 229940002612 prodrug Drugs 0.000 description 6
- 239000000651 prodrug Substances 0.000 description 6
- 125000001424 substituent group Chemical group 0.000 description 5
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 description 4
- 125000003118 aryl group Chemical group 0.000 description 2
- 125000000732 arylene group Chemical group 0.000 description 2
- 125000001072 heteroaryl group Chemical group 0.000 description 2
- 125000005549 heteroarylene group Chemical group 0.000 description 2
- 238000000034 method Methods 0.000 description 2
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 description 1
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 description 1
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 description 1
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 description 1
- XFXPMWWXUTWYJX-UHFFFAOYSA-N Cyanide Chemical compound N#[C-] XFXPMWWXUTWYJX-UHFFFAOYSA-N 0.000 description 1
- 125000003342 alkenyl group Chemical group 0.000 description 1
- 125000000304 alkynyl group Chemical group 0.000 description 1
- 125000004432 carbon atom Chemical group C* 0.000 description 1
- 230000004663 cell proliferation Effects 0.000 description 1
- 210000003679 cervix uteri Anatomy 0.000 description 1
- -1 cyano, hydroxy Chemical group 0.000 description 1
- 229940079593 drug Drugs 0.000 description 1
- 239000003814 drug Substances 0.000 description 1
- 125000005842 heteroatom Chemical group 0.000 description 1
- 230000002401 inhibitory effect Effects 0.000 description 1
- 125000002950 monocyclic group Chemical group 0.000 description 1
- 230000002265 prevention Effects 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610833890.3 | 2016-09-19 | ||
| CN201610833890.3A CN107840842A (zh) | 2016-09-19 | 2016-09-19 | 炔代杂环化合物、其制备方法及其在医药学上的应用 |
| PCT/CN2017/072570 WO2018049781A1 (zh) | 2016-09-19 | 2017-01-25 | 炔代杂环化合物、其制备方法及其在医药学上的应用 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2019529444A JP2019529444A (ja) | 2019-10-17 |
| JP2019529444A5 true JP2019529444A5 (enExample) | 2020-03-05 |
| JP6906811B2 JP6906811B2 (ja) | 2021-07-21 |
Family
ID=61618562
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019515464A Active JP6906811B2 (ja) | 2016-09-19 | 2017-01-25 | アルキル置換複素環化合物、そのための調製方法およびその医学的用途 |
Country Status (12)
| Country | Link |
|---|---|
| US (3) | US10710981B2 (enExample) |
| EP (1) | EP3517535B1 (enExample) |
| JP (1) | JP6906811B2 (enExample) |
| KR (1) | KR102783517B1 (enExample) |
| CN (2) | CN107840842A (enExample) |
| AU (1) | AU2017327954B2 (enExample) |
| CA (1) | CA3036594C (enExample) |
| ES (1) | ES2925212T3 (enExample) |
| MX (1) | MX390747B (enExample) |
| RU (1) | RU2729069C1 (enExample) |
| SG (1) | SG10202102822RA (enExample) |
| WO (1) | WO2018049781A1 (enExample) |
Families Citing this family (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN113227077B (zh) * | 2018-12-13 | 2024-10-29 | 英特维特国际股份有限公司 | 一种制备1-[(3r,4s)-4-氰基四氢吡喃-3-基]-3-[(2-氟-6-甲氧基-4-吡啶基)氨基]吡唑-4-甲酰胺的方法 |
| US12351571B2 (en) | 2018-12-19 | 2025-07-08 | Array Biopharma Inc. | Substituted quinoxaline compounds as inhibitors of FGFR tyrosine kinases |
| CA3129665A1 (en) | 2019-03-21 | 2020-09-24 | Onxeo | A dbait molecule in combination with kinase inhibitor for the treatment of cancer |
| KR20220098759A (ko) | 2019-11-08 | 2022-07-12 | 인쎄름 (엥스띠뛰 나씨오날 드 라 쌍떼 에 드 라 흐쉐르슈 메디깔) | 키나제 억제제에 대해 내성을 획득한 암의 치료 방법 |
| JP2023509399A (ja) | 2019-12-26 | 2023-03-08 | ベイジン・イノケア・ファーマ・テク・カンパニー・リミテッド | （ｓ）－１－（１－アクリロイルピロリジン－３－イル）－３－（（３，５－ジメトキシフェニル）エチニル）－５－（メチルアミノ）－１ｈ－ピラゾール－４－カルボキサミドの結晶形 |
| WO2021148581A1 (en) | 2020-01-22 | 2021-07-29 | Onxeo | Novel dbait molecule and its use |
| EP4161657A1 (en) * | 2020-06-05 | 2023-04-12 | Kinnate Biopharma Inc. | Inhibitors of fibroblast growth factor receptor kinases |
| CN116057045B (zh) * | 2020-06-05 | 2026-06-09 | 金耐特生物制药公司 | 成纤维细胞生长因子受体激酶抑制剂 |
| WO2022042613A1 (zh) * | 2020-08-27 | 2022-03-03 | 上海和誉生物医药科技有限公司 | 一种1h-吡唑-4-酰胺衍生物，其制备方法和应用 |
| MX2023008186A (es) * | 2021-01-12 | 2023-07-18 | Beijing Innocare Pharma Tech Co Ltd | Proceso para preparar (s)-1-(1-acriloilpirrolidin-3-il)-3-((3,5-di metoxifenil)etinil)-5-(metilamino)-1h-pirazol-4-carboxamida. |
| CN114853739B (zh) * | 2021-02-03 | 2023-09-22 | 药雅科技(上海)有限公司 | 一种炔代吡嗪类fgfr抑制剂及其制备方法和用途 |
| CN115433190B (zh) * | 2021-06-02 | 2024-09-20 | 药雅科技(上海)有限公司 | 不可逆杂环化合物fgfr抑制剂的制备方法和用途 |
| CN115043832B (zh) * | 2021-03-08 | 2023-08-22 | 药雅科技(上海)有限公司 | 一种fgfr抑制剂炔代杂环类化合物及其制备方法和用途 |
| CA3235435A1 (en) * | 2021-11-03 | 2023-05-11 | Xiangyang Chen | Amorphous solid dispersion comprising (s)-1-(1-acryloylpyrrolidin-3-yl)-3-((3,5-dimethoxyphenyl) ethynyl)-5-(methylamino)-1h-pyrazole-4-carboxamide |
| CN118354772A (zh) * | 2021-11-16 | 2024-07-16 | 北京诺诚健华医药科技有限公司 | 治疗头颈癌的方法 |
| EP4444302A4 (en) * | 2021-12-08 | 2025-09-03 | Kinnate Biopharma Inc | SOLID STATE FORMS OF AN FGFR INHIBITOR |
| AU2022407439A1 (en) * | 2021-12-08 | 2024-06-27 | Kinnate Biopharma Inc. | Treatment of cancer with an fgfr kinase inhibitor |
| WO2023107870A1 (en) * | 2021-12-08 | 2023-06-15 | Kinnate Biopharma Inc. | Inhibitors of fibroblast growth factor receptor kinases |
| US20250332105A1 (en) * | 2024-04-25 | 2025-10-30 | Beijing Innocare Pharma Tech Co., Ltd. | Amorphous solid dispersion comprising (s)-1-(1-acryloylpyrrolidin-3-yl)-3-((3,5-dimethoxyphenyl)ethynyl)-5-(methylamino)-1h-pyrazole-4-carboxamide |
Family Cites Families (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR2833948B1 (fr) * | 2001-12-21 | 2004-02-06 | Sod Conseils Rech Applic | Nouveaux derives de benzimidazole et leur utilisation en tant que medicament |
| KR101124245B1 (ko) | 2002-06-27 | 2012-07-02 | 노보 노르디스크 에이/에스 | 치료제로서 아릴 카르보닐 유도체 |
| CN1508130A (zh) | 2002-12-18 | 2004-06-30 | 中国科学院大连化学物理研究所 | N-苯基-n’-嘧啶基取代脲类衍生物的合成方法 |
| US7150894B2 (en) * | 2003-05-01 | 2006-12-19 | Kraft Foods Holdings, Inc. | Acid whey texture system |
| SI1761520T1 (sl) | 2004-06-23 | 2008-10-31 | Lilly Co Eli | Inhibitorji kinaze |
| FR2889526B1 (fr) | 2005-08-04 | 2012-02-17 | Aventis Pharma Sa | 7-aza-indazoles substitues, compositions les contenant, procede de fabrication et utilisation |
| JP2009515998A (ja) | 2005-11-16 | 2009-04-16 | エスジーエックス ファーマシューティカルズ、インコーポレイテッド | ピラゾロチアゾールタンパク質キナーゼモジュレータ |
| FR2908409B1 (fr) | 2006-11-10 | 2009-01-09 | Sanofi Aventis Sa | Pyrazoles substituees,compositions les contenant,procede de fabrication et utilisation |
| CN101611014B (zh) * | 2006-12-21 | 2012-05-30 | 阿斯利康(瑞典)有限公司 | 用作fgfr抑制剂的酰氨基吡唑类化合物 |
| US7737149B2 (en) * | 2006-12-21 | 2010-06-15 | Astrazeneca Ab | N-[5-[2-(3,5-dimethoxyphenyl)ethyl]-2H-pyrazol-3-yl]-4-(3,5-dimethylpiperazin-1-yl)benzamide and salts thereof |
| UA105005C2 (uk) | 2008-06-16 | 2014-04-10 | Юніверсіті Оф Теннессі Рісерч Фаундейшн | Сполуки для лікування раку |
| FR2947546B1 (fr) | 2009-07-03 | 2011-07-01 | Sanofi Aventis | Derives de pyrazoles, leur preparation et leur application en therapeutique |
| GB2474748B (en) * | 2009-10-01 | 2011-10-12 | Amira Pharmaceuticals Inc | Polycyclic compounds as lysophosphatidic acid receptor antagonists |
| CA2791738C (en) | 2010-03-01 | 2020-06-09 | Gtx, Inc. | Aryl imidazolyl compounds for the treatment of cancer |
| EP2736514B1 (en) * | 2011-07-28 | 2017-10-18 | Nerviano Medical Sciences S.r.l. | Alkynyl substituted pyrimidinyl-pyrroles active as kinases inhibitors |
| WO2013024427A1 (en) | 2011-08-16 | 2013-02-21 | Glenmark Pharmaceuticals S.A. | Novel urea derivatives as tec kinase inhibitors and uses thereof |
| CN103848810A (zh) * | 2012-11-30 | 2014-06-11 | 北京赛林泰医药技术有限公司 | 鲁顿酪氨酸激酶抑制剂 |
| DK3023100T3 (da) * | 2013-07-18 | 2019-05-27 | Taiho Pharmaceutical Co Ltd | Antitumorlægemiddel til intermitterende administration af fgfr-hæmmer |
| JP6084292B2 (ja) | 2013-07-18 | 2017-02-22 | 大鵬薬品工業株式会社 | Ｆｇｆｒ阻害剤耐性癌の治療薬 |
| CN105683188B (zh) | 2013-10-25 | 2018-02-09 | 诺华股份有限公司 | 作为fgfr4抑制剂的稠环二环吡啶基衍生物 |
| EP3274344B1 (en) | 2015-03-25 | 2019-04-24 | Novartis Ag | Formylated n-heterocyclic derivatives as fgfr4 inhibitors |
-
2016
- 2016-09-19 CN CN201610833890.3A patent/CN107840842A/zh not_active Withdrawn
-
2017
- 2017-01-25 MX MX2019003143A patent/MX390747B/es unknown
- 2017-01-25 KR KR1020197011454A patent/KR102783517B1/ko active Active
- 2017-01-25 WO PCT/CN2017/072570 patent/WO2018049781A1/zh not_active Ceased
- 2017-01-25 ES ES17849992T patent/ES2925212T3/es active Active
- 2017-01-25 SG SG10202102822RA patent/SG10202102822RA/en unknown
- 2017-01-25 CA CA3036594A patent/CA3036594C/en active Active
- 2017-01-25 AU AU2017327954A patent/AU2017327954B2/en active Active
- 2017-01-25 CN CN201780057036.5A patent/CN109843873B/zh active Active
- 2017-01-25 RU RU2019112046A patent/RU2729069C1/ru active
- 2017-01-25 EP EP17849992.7A patent/EP3517535B1/en active Active
- 2017-01-25 JP JP2019515464A patent/JP6906811B2/ja active Active
-
2019
- 2019-03-14 US US16/353,806 patent/US10710981B2/en active Active
-
2020
- 2020-07-10 US US16/925,738 patent/US11059805B2/en active Active
-
2021
- 2021-07-07 US US17/369,850 patent/US11572353B2/en active Active
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