JP2019529435A5 - - Google Patents
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- JP2019529435A5 JP2019529435A5 JP2019515307A JP2019515307A JP2019529435A5 JP 2019529435 A5 JP2019529435 A5 JP 2019529435A5 JP 2019515307 A JP2019515307 A JP 2019515307A JP 2019515307 A JP2019515307 A JP 2019515307A JP 2019529435 A5 JP2019529435 A5 JP 2019529435A5
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- JP
- Japan
- Prior art keywords
- group
- cancer
- compound
- compound according
- halogenated
- 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.)
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- 150000001875 compounds Chemical class 0.000 claims 11
- 150000001335 aliphatic alkanes Chemical class 0.000 claims 5
- 125000000753 cycloalkyl group Chemical group 0.000 claims 5
- 229910052736 halogen Inorganic materials 0.000 claims 5
- 150000002367 halogens Chemical class 0.000 claims 5
- 229910052739 hydrogen Inorganic materials 0.000 claims 5
- 150000002431 hydrogen Chemical class 0.000 claims 5
- 239000001257 hydrogen Substances 0.000 claims 5
- 125000003545 alkoxy group Chemical group 0.000 claims 4
- 125000000000 cycloalkoxy group Chemical group 0.000 claims 4
- 238000004519 manufacturing process Methods 0.000 claims 4
- 206010028980 Neoplasm Diseases 0.000 claims 3
- 150000001336 alkenes Chemical group 0.000 claims 3
- 125000002355 alkine group Chemical group 0.000 claims 3
- 201000011510 cancer Diseases 0.000 claims 3
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- 102000004022 Protein-Tyrosine Kinases Human genes 0.000 claims 2
- 108090000412 Protein-Tyrosine Kinases Proteins 0.000 claims 2
- 102100033177 Vascular endothelial growth factor receptor 2 Human genes 0.000 claims 2
- 125000002009 alkene group Chemical group 0.000 claims 2
- 125000004414 alkyl thio group Chemical group 0.000 claims 2
- 239000002260 anti-inflammatory agent Substances 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 150000002576 ketones Chemical class 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- 229940124597 therapeutic agent Drugs 0.000 claims 2
- 125000003396 thiol group Chemical group [H]S* 0.000 claims 2
- 208000036764 Adenocarcinoma of the esophagus Diseases 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 206010018338 Glioma Diseases 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 102100021435 Macrophage-stimulating protein receptor Human genes 0.000 claims 1
- 206010030137 Oesophageal adenocarcinoma 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
- 208000005718 Stomach Neoplasms Diseases 0.000 claims 1
- 108091008605 VEGF receptors Proteins 0.000 claims 1
- 229940121363 anti-inflammatory agent Drugs 0.000 claims 1
- 229940124599 anti-inflammatory drug Drugs 0.000 claims 1
- 208000029742 colonic neoplasm Diseases 0.000 claims 1
- 125000000392 cycloalkenyl group Chemical group 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 208000028653 esophageal adenocarcinoma Diseases 0.000 claims 1
- 206010017758 gastric cancer Diseases 0.000 claims 1
- 208000029824 high grade glioma Diseases 0.000 claims 1
- 239000003112 inhibitor Substances 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 201000011614 malignant glioma Diseases 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- JRZJOMJEPLMPRA-UHFFFAOYSA-N olefin Natural products CCCCCCCC=C JRZJOMJEPLMPRA-UHFFFAOYSA-N 0.000 claims 1
- 229910052760 oxygen Inorganic materials 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 102000009076 src-Family Kinases Human genes 0.000 claims 1
- 108010087686 src-Family Kinases Proteins 0.000 claims 1
- 201000011549 stomach cancer Diseases 0.000 claims 1
- 239000000126 substance Substances 0.000 claims 1
- 229910052717 sulfur Inorganic materials 0.000 claims 1
- 229940121358 tyrosine kinase inhibitor Drugs 0.000 claims 1
- 239000005483 tyrosine kinase inhibitor Substances 0.000 claims 1
- 150000004917 tyrosine kinase inhibitor derivatives Chemical class 0.000 claims 1
- NMILGIZTAZXMTM-UHFFFAOYSA-N CCCN1CCOCC1 Chemical compound CCCN1CCOCC1 NMILGIZTAZXMTM-UHFFFAOYSA-N 0.000 description 1
- BNYAUACYQJVWNX-UHFFFAOYSA-N COc(c(N(C1)CC1N1CCOCC1)cc1ncc2)cc1c2Oc(ccc(NC(CCCCC(Nc(cc1)ccc1F)=O)=O)c1)c1F Chemical compound COc(c(N(C1)CC1N1CCOCC1)cc1ncc2)cc1c2Oc(ccc(NC(CCCCC(Nc(cc1)ccc1F)=O)=O)c1)c1F BNYAUACYQJVWNX-UHFFFAOYSA-N 0.000 description 1
- HZQKNWJBZJKRAT-UHFFFAOYSA-N COc(c(OC(C1)CC1N1CCOCC1)cc1ncc2)cc1c2Oc(c(F)c1)ccc1NC(C1(CC1)C(Nc(cc1)ccc1F)=O)=O Chemical compound COc(c(OC(C1)CC1N1CCOCC1)cc1ncc2)cc1c2Oc(c(F)c1)ccc1NC(C1(CC1)C(Nc(cc1)ccc1F)=O)=O HZQKNWJBZJKRAT-UHFFFAOYSA-N 0.000 description 1
- ZBSAZWSQJRSAHS-UHFFFAOYSA-N COc(c(OC(C1)CC1N1CCOCC1)cc1ncc2)cc1c2Oc(ccc(NC(C1(CCC1)C(Nc(cc1)ccc1[F]COc(c(OC1CC(CN2CCOCC2)C1)c1)cc2c1nccc2Oc(ccc(NC(C1(CCC1)C(Nc(cc1)ccc1F)=O)=O)c1)c1F)=O)=O)c1)c1F Chemical compound COc(c(OC(C1)CC1N1CCOCC1)cc1ncc2)cc1c2Oc(ccc(NC(C1(CCC1)C(Nc(cc1)ccc1[F]COc(c(OC1CC(CN2CCOCC2)C1)c1)cc2c1nccc2Oc(ccc(NC(C1(CCC1)C(Nc(cc1)ccc1F)=O)=O)c1)c1F)=O)=O)c1)c1F ZBSAZWSQJRSAHS-UHFFFAOYSA-N 0.000 description 1
- BPSGMWZDJGOAEG-UHFFFAOYSA-N COc(c(OC1C(CN2CCOCC2)C1)cc1ncc2)cc1c2Oc(ccc(NC(C1(CC1)C(Nc(cc1)ccc1F)=O)=O)c1)c1F Chemical compound COc(c(OC1C(CN2CCOCC2)C1)cc1ncc2)cc1c2Oc(ccc(NC(C1(CC1)C(Nc(cc1)ccc1F)=O)=O)c1)c1F BPSGMWZDJGOAEG-UHFFFAOYSA-N 0.000 description 1
- SUVGWHULDOHEIU-UHFFFAOYSA-N COc(c(OC1C(CN2CCOCC2)CC1)cc1ncc2)cc1c2Oc(ccc(NC(C1(CC1)C(Nc(cc1)ccc1F)=O)=O)c1)c1F Chemical compound COc(c(OC1C(CN2CCOCC2)CC1)cc1ncc2)cc1c2Oc(ccc(NC(C1(CC1)C(Nc(cc1)ccc1F)=O)=O)c1)c1F SUVGWHULDOHEIU-UHFFFAOYSA-N 0.000 description 1
- GNSKZQUCNAHICS-UHFFFAOYSA-N COc(c(OC1CC(CN2CCOCC2)C1)cc1ncc2)cc1c2Oc(ccc(NC(C1(CC1)C(Nc(cc1)ccc1F)=O)=O)c1)c1F Chemical compound COc(c(OC1CC(CN2CCOCC2)C1)cc1ncc2)cc1c2Oc(ccc(NC(C1(CC1)C(Nc(cc1)ccc1F)=O)=O)c1)c1F GNSKZQUCNAHICS-UHFFFAOYSA-N 0.000 description 1
- MPVXOIXRPUPSAK-UHFFFAOYSA-N COc(c(OCC(C1)CC1N1CCOCC1)cc1ncc2)cc1c2Oc(ccc(NC(C1(CC1)C(Nc(cc1)ccc1F)=O)=O)c1)c1F Chemical compound COc(c(OCC(C1)CC1N1CCOCC1)cc1ncc2)cc1c2Oc(ccc(NC(C1(CC1)C(Nc(cc1)ccc1F)=O)=O)c1)c1F MPVXOIXRPUPSAK-UHFFFAOYSA-N 0.000 description 1
- BKBMOGBZYSPFQT-UHFFFAOYSA-N COc(c(OCC(CN1CCOCC1)(F)F)cc1ncc2)cc1c2Oc(ccc(NC(C1(CC1)C(Nc(cc1)ccc1F)=O)=O)c1)c1F Chemical compound COc(c(OCC(CN1CCOCC1)(F)F)cc1ncc2)cc1c2Oc(ccc(NC(C1(CC1)C(Nc(cc1)ccc1F)=O)=O)c1)c1F BKBMOGBZYSPFQT-UHFFFAOYSA-N 0.000 description 1
- ZDSJZAOXTHSXBG-UHFFFAOYSA-N COc(c(OCC(CN1CCOCC1)F)cc1ncc2)cc1c2Oc(ccc(NC(C1(CC1)C(Nc(cc1)ccc1[F][O](C)c(c(OCC1=C(CN2CCOCC2)C1)cc1ncc2)cc1c2Oc(ccc(NC(C1(CC1)C(Nc(cc1)ccc1F)=O)=O)c1)c1F)=O)=O)c1)c1F Chemical compound COc(c(OCC(CN1CCOCC1)F)cc1ncc2)cc1c2Oc(ccc(NC(C1(CC1)C(Nc(cc1)ccc1[F][O](C)c(c(OCC1=C(CN2CCOCC2)C1)cc1ncc2)cc1c2Oc(ccc(NC(C1(CC1)C(Nc(cc1)ccc1F)=O)=O)c1)c1F)=O)=O)c1)c1F ZDSJZAOXTHSXBG-UHFFFAOYSA-N 0.000 description 1
- AMOSSRUJEBKHLD-UHFFFAOYSA-N COc(c(OCC(CN1CCOCC1)F)cc1ncc2)cc1c2Oc(ccc(NC(CCCCCC(Nc(cc1)ccc1F)=O)=O)c1)c1F Chemical compound COc(c(OCC(CN1CCOCC1)F)cc1ncc2)cc1c2Oc(ccc(NC(CCCCCC(Nc(cc1)ccc1F)=O)=O)c1)c1F AMOSSRUJEBKHLD-UHFFFAOYSA-N 0.000 description 1
- HHFNVSBWTZCYIF-UHFFFAOYSA-N COc(c(OCCCNN(CCOC1)C1=O)cc1ncc2)cc1c2Oc(ccc(NC(C1(CC1)C(Nc(cc1)ccc1F)=O)=O)c1)c1F Chemical compound COc(c(OCCCNN(CCOC1)C1=O)cc1ncc2)cc1c2Oc(ccc(NC(C1(CC1)C(Nc(cc1)ccc1F)=O)=O)c1)c1F HHFNVSBWTZCYIF-UHFFFAOYSA-N 0.000 description 1
- JAQGJERMCQKCNG-UHFFFAOYSA-N COc(c(OCCCNN(CCOC1)C1=O)cc1ncc2)cc1c2Oc(ccc(NC(CCCCCC(Nc(cc1)ccc1F)=O)=O)c1)c1F Chemical compound COc(c(OCCCNN(CCOC1)C1=O)cc1ncc2)cc1c2Oc(ccc(NC(CCCCCC(Nc(cc1)ccc1F)=O)=O)c1)c1F JAQGJERMCQKCNG-UHFFFAOYSA-N 0.000 description 1
- AACOYZJNSRJDLQ-UHFFFAOYSA-N COc(c(OCCCNN1CCOCC1)cc1ncc2)cc1c2Oc(ccc(NC(C1(CC1)C(Nc(cc1)ccc1F)=O)=O)c1)c1F Chemical compound COc(c(OCCCNN1CCOCC1)cc1ncc2)cc1c2Oc(ccc(NC(C1(CC1)C(Nc(cc1)ccc1F)=O)=O)c1)c1F AACOYZJNSRJDLQ-UHFFFAOYSA-N 0.000 description 1
- QCTMUDAWXZXIPI-UHFFFAOYSA-N COc(c(OCCCNN1CCOCC1)cc1ncc2)cc1c2Oc(ccc(NC(C1(CCC1)C(Nc(cc1)ccc1F)=O)=O)c1)c1F Chemical compound COc(c(OCCCNN1CCOCC1)cc1ncc2)cc1c2Oc(ccc(NC(C1(CCC1)C(Nc(cc1)ccc1F)=O)=O)c1)c1F QCTMUDAWXZXIPI-UHFFFAOYSA-N 0.000 description 1
- AEOFOUQQBXCVLI-UHFFFAOYSA-N COc(c(OCCN(C1)CC1N(CCOC1)C1=O)cc1ncc2)cc1c2Oc(ccc(NC(C1(CCC1)C(Nc(cc1)ccc1F)=O)=O)c1)c1F Chemical compound COc(c(OCCN(C1)CC1N(CCOC1)C1=O)cc1ncc2)cc1c2Oc(ccc(NC(C1(CCC1)C(Nc(cc1)ccc1F)=O)=O)c1)c1F AEOFOUQQBXCVLI-UHFFFAOYSA-N 0.000 description 1
- DUUFUKIIRDHEAQ-UHFFFAOYSA-N COc(c(OCCN(C1)CC1N1CCOCC1)cc1ncc2)cc1c2Oc(ccc(NC(C1(CC1)C(Nc(cc1)ccc1F)=O)=O)c1)c1F Chemical compound COc(c(OCCN(C1)CC1N1CCOCC1)cc1ncc2)cc1c2Oc(ccc(NC(C1(CC1)C(Nc(cc1)ccc1F)=O)=O)c1)c1F DUUFUKIIRDHEAQ-UHFFFAOYSA-N 0.000 description 1
- URAYJYRGEYMDCS-UHFFFAOYSA-N COc(c(OCCN(C1)CC1N1CCOCC1)cc1ncc2)cc1c2Oc(ccc(NC(CCCCCC(Nc(cc1)ccc1F)=O)=O)c1)c1F Chemical compound COc(c(OCCN(C1)CC1N1CCOCC1)cc1ncc2)cc1c2Oc(ccc(NC(CCCCCC(Nc(cc1)ccc1F)=O)=O)c1)c1F URAYJYRGEYMDCS-UHFFFAOYSA-N 0.000 description 1
- CRHOFDAFXYALKY-UHFFFAOYSA-N COc(c(OCCNN(CCOC1)C1=O)cc1ncc2)cc1c2Oc(ccc(NC(C1(CC1)C(Nc(cc1)ccc1F)=O)=O)c1)c1F Chemical compound COc(c(OCCNN(CCOC1)C1=O)cc1ncc2)cc1c2Oc(ccc(NC(C1(CC1)C(Nc(cc1)ccc1F)=O)=O)c1)c1F CRHOFDAFXYALKY-UHFFFAOYSA-N 0.000 description 1
- USUJIKHBDHJAPD-UHFFFAOYSA-N COc(c(OCCNN1CCOCC1)cc1ncc2)cc1c2Oc(ccc(NC(C1(CC1)C(Nc(cc1)ccc1F)=O)=O)c1)c1F Chemical compound COc(c(OCCNN1CCOCC1)cc1ncc2)cc1c2Oc(ccc(NC(C1(CC1)C(Nc(cc1)ccc1F)=O)=O)c1)c1F USUJIKHBDHJAPD-UHFFFAOYSA-N 0.000 description 1
- RGJADZLKUAQNSK-UHFFFAOYSA-N COc(ccc1c2nccc1Oc(cc1)ccc1NC(C1(CC1)C(Nc1ccccc1)=O)=O)c2N1CC(CN2CCOCC2)C1 Chemical compound COc(ccc1c2nccc1Oc(cc1)ccc1NC(C1(CC1)C(Nc1ccccc1)=O)=O)c2N1CC(CN2CCOCC2)C1 RGJADZLKUAQNSK-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610822529.0 | 2016-09-13 | ||
| CN201610822529.0A CN107235896B (zh) | 2016-09-13 | 2016-09-13 | 酪氨酸激酶抑制剂及其应用 |
| PCT/CN2017/089501 WO2018049861A1 (zh) | 2016-09-13 | 2017-06-22 | 酪氨酸激酶抑制剂及其应用 |
Publications (4)
| Publication Number | Publication Date |
|---|---|
| JP2019529435A JP2019529435A (ja) | 2019-10-17 |
| JP2019529435A5 true JP2019529435A5 (enExample) | 2020-11-12 |
| JPWO2018049861A5 JPWO2018049861A5 (enExample) | 2024-03-06 |
| JP7487921B2 JP7487921B2 (ja) | 2024-05-21 |
Family
ID=59982910
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019515307A Active JP7487921B2 (ja) | 2016-09-13 | 2017-06-22 | チロシンキナーゼ阻害剤及びその応用 |
Country Status (8)
| Country | Link |
|---|---|
| US (1) | US10882853B2 (enExample) |
| EP (1) | EP3511327B1 (enExample) |
| JP (1) | JP7487921B2 (enExample) |
| KR (2) | KR102382039B1 (enExample) |
| CN (2) | CN107235896B (enExample) |
| AU (1) | AU2017325641B2 (enExample) |
| ES (1) | ES2902549T3 (enExample) |
| WO (1) | WO2018049861A1 (enExample) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US11427578B1 (en) | 2017-07-18 | 2022-08-30 | Bayer Pharma Aktiengesellschaft | Substituted pyrrolopyridine-derivatives |
| CR20250117A (es) | 2018-01-26 | 2025-05-09 | Exelixis Inc | COMPUESTOS PARA EL TRATAMIENTO DE TRASTORNOS DEPENDIENTES DE CINASAS (Divisional 2020-0355) |
| CN117624045A (zh) * | 2018-01-26 | 2024-03-01 | 埃克塞里艾克西斯公司 | 用于治疗激酶依赖性病症的化合物 |
| WO2019148043A1 (en) | 2018-01-26 | 2019-08-01 | Exelixis, Inc. | Compounds for the treatment of kinase-dependent disorders |
| AR119069A1 (es) * | 2019-06-04 | 2021-11-24 | Exelixis Inc | Compuestos para el tratamiento de trastornos dependientes de quinasas |
| CN112358469A (zh) * | 2020-03-18 | 2021-02-12 | 北京康辰药业股份有限公司 | 血管生成抑制剂、其制备方法及其应用 |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2744997A1 (en) * | 2003-09-26 | 2005-04-07 | Exelixis, Inc. | C-met modulators and method of use |
| UY31800A (es) * | 2008-05-05 | 2009-11-10 | Smithkline Beckman Corp | Metodo de tratamiento de cancer usando un inhibidor de cmet y axl y un inhibidor de erbb |
| WO2010045095A1 (en) * | 2008-10-14 | 2010-04-22 | Ning Xi | Compounds and methods of use |
| WO2010111063A1 (en) * | 2009-03-21 | 2010-09-30 | Ning Xi | Amino ester derivatives, salts thereof and methods of use |
| US8664244B2 (en) | 2010-09-12 | 2014-03-04 | Advenchen Pharmaceuticals, LLC | Compounds as c-Met kinase inhibitors |
| CN105884695B (zh) * | 2015-02-13 | 2019-02-26 | 山东轩竹医药科技有限公司 | 杂环衍生物类酪氨酸激酶抑制剂 |
| CN104817497B (zh) * | 2015-03-20 | 2017-03-08 | 南京众睿缘生物科技有限公司 | 一种炔代喹啉衍生物及其制备方法和用途 |
| CN105001168A (zh) * | 2015-08-25 | 2015-10-28 | 佛山市赛维斯医药科技有限公司 | 三烷氧基取代的苯并喹唑啉类酪氨酸激酶抑制剂及其用途 |
| CN105218445B (zh) * | 2015-08-25 | 2018-05-22 | 江苏中邦制药有限公司 | 一种酪氨酸激酶抑制剂Foretinib的制备方法 |
| CN105085416A (zh) * | 2015-08-25 | 2015-11-25 | 佛山市赛维斯医药科技有限公司 | 一类硝基取代的双烷氧苯并喹唑啉类酪氨酸激酶抑制剂及用途 |
| CN105017163A (zh) * | 2015-08-25 | 2015-11-04 | 佛山市赛维斯医药科技有限公司 | 双乙氧基苯并喹唑啉类酪氨酸激酶抑制剂、制备方法及其用途 |
-
2016
- 2016-09-13 CN CN201610822529.0A patent/CN107235896B/zh active Active
- 2016-09-13 CN CN201910822704.XA patent/CN110437145A/zh active Pending
-
2017
- 2017-06-22 AU AU2017325641A patent/AU2017325641B2/en active Active
- 2017-06-22 ES ES17850066T patent/ES2902549T3/es active Active
- 2017-06-22 EP EP17850066.6A patent/EP3511327B1/en active Active
- 2017-06-22 WO PCT/CN2017/089501 patent/WO2018049861A1/zh not_active Ceased
- 2017-06-22 KR KR1020217037589A patent/KR102382039B1/ko active Active
- 2017-06-22 JP JP2019515307A patent/JP7487921B2/ja active Active
- 2017-06-22 US US16/333,050 patent/US10882853B2/en active Active
- 2017-06-22 KR KR1020197010451A patent/KR20190045354A/ko not_active Ceased