JP2016514718A5 - - Google Patents
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- Publication number
- JP2016514718A5 JP2016514718A5 JP2016503668A JP2016503668A JP2016514718A5 JP 2016514718 A5 JP2016514718 A5 JP 2016514718A5 JP 2016503668 A JP2016503668 A JP 2016503668A JP 2016503668 A JP2016503668 A JP 2016503668A JP 2016514718 A5 JP2016514718 A5 JP 2016514718A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- hydrogen
- hydroxy
- independently
- alkylene
- 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
Links
- 229910052739 hydrogen Inorganic materials 0.000 claims 47
- 239000001257 hydrogen Substances 0.000 claims 47
- -1 cyano, hydroxy Chemical group 0.000 claims 33
- 150000002431 hydrogen Chemical class 0.000 claims 24
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 23
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 23
- 229910052736 halogen Inorganic materials 0.000 claims 19
- 125000004093 cyano group Chemical group *C#N 0.000 claims 17
- 150000002367 halogens Chemical class 0.000 claims 17
- 125000001072 heteroaryl group Chemical group 0.000 claims 17
- 150000001204 N-oxides Chemical class 0.000 claims 14
- 150000001875 compounds Chemical class 0.000 claims 14
- 150000003839 salts Chemical class 0.000 claims 14
- 125000006163 5-membered heteroaryl group Chemical group 0.000 claims 12
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 12
- 229910052757 nitrogen Inorganic materials 0.000 claims 9
- 125000000623 heterocyclic group Chemical group 0.000 claims 8
- 125000004317 1,3,5-triazin-2-yl group Chemical group [H]C1=NC(*)=NC([H])=N1 0.000 claims 6
- 125000003349 3-pyridyl group Chemical group N1=C([H])C([*])=C([H])C([H])=C1[H] 0.000 claims 6
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 6
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 6
- 229910052731 fluorine Inorganic materials 0.000 claims 6
- 239000011737 fluorine Substances 0.000 claims 6
- 125000004043 oxo group Chemical group O=* 0.000 claims 6
- 125000004307 pyrazin-2-yl group Chemical group [H]C1=C([H])N=C(*)C([H])=N1 0.000 claims 6
- 125000004940 pyridazin-4-yl group Chemical group N1=NC=C(C=C1)* 0.000 claims 6
- 125000004527 pyrimidin-4-yl group Chemical group N1=CN=C(C=C1)* 0.000 claims 6
- 125000004105 2-pyridyl group Chemical group N1=C([*])C([H])=C([H])C([H])=C1[H] 0.000 claims 5
- 125000005842 heteroatom Chemical group 0.000 claims 5
- 125000002206 pyridazin-3-yl group Chemical group [H]C1=C([H])C([H])=C(*)N=N1 0.000 claims 5
- 125000000246 pyrimidin-2-yl group Chemical group [H]C1=NC(*)=NC([H])=C1[H] 0.000 claims 5
- 125000004528 pyrimidin-5-yl group Chemical group N1=CN=CC(=C1)* 0.000 claims 5
- 125000000217 alkyl group Chemical group 0.000 claims 4
- 201000010099 disease Diseases 0.000 claims 4
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 4
- 229910052717 sulfur Inorganic materials 0.000 claims 4
- 206010027476 Metastases Diseases 0.000 claims 3
- 206010028980 Neoplasm Diseases 0.000 claims 3
- 239000004480 active ingredient Substances 0.000 claims 3
- 229910052760 oxygen Inorganic materials 0.000 claims 3
- 239000002246 antineoplastic agent Substances 0.000 claims 2
- 230000030833 cell death Effects 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 125000001153 fluoro group Chemical group F* 0.000 claims 2
- 230000003463 hyperproliferative effect Effects 0.000 claims 2
- 230000006698 induction Effects 0.000 claims 2
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 2
- 125000004432 carbon atom Chemical group C* 0.000 claims 1
- 230000000973 chemotherapeutic effect Effects 0.000 claims 1
- 125000001301 ethoxy group Chemical group [H]C([H])([H])C([H])([H])O* 0.000 claims 1
- 125000005745 ethoxymethyl group Chemical group [H]C([H])([H])C([H])([H])OC([H])([H])* 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 208000019691 hematopoietic and lymphoid cell neoplasm Diseases 0.000 claims 1
- 208000024200 hematopoietic and lymphoid system neoplasm Diseases 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 230000009401 metastasis Effects 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
- 208000024719 uterine cervix neoplasm Diseases 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP13160520.6 | 2013-03-21 | ||
| EP13160520 | 2013-03-21 | ||
| PCT/EP2014/055657 WO2014147203A1 (en) | 2013-03-21 | 2014-03-20 | 3-heteroaryl substituted indazoles |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2016514718A JP2016514718A (ja) | 2016-05-23 |
| JP2016514718A5 true JP2016514718A5 (enExample) | 2017-04-20 |
Family
ID=47901890
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016503668A Pending JP2016514718A (ja) | 2013-03-21 | 2014-03-20 | ３−ヘテロアリール置換インダゾール類 |
Country Status (10)
| Country | Link |
|---|---|
| US (1) | US20160046610A1 (enExample) |
| EP (1) | EP2976336A1 (enExample) |
| JP (1) | JP2016514718A (enExample) |
| CN (1) | CN105209455A (enExample) |
| AR (1) | AR095706A1 (enExample) |
| CA (1) | CA2907592A1 (enExample) |
| HK (1) | HK1218750A1 (enExample) |
| TW (1) | TW201514166A (enExample) |
| UY (1) | UY35500A (enExample) |
| WO (1) | WO2014147203A1 (enExample) |
Families Citing this family (33)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| UA111754C2 (uk) | 2011-10-06 | 2016-06-10 | Байєр Фарма Акцієнгезелльшафт | Заміщені бензиліндазоли для застосування як інгібіторів bub1-кінази для лікування гіперпроліферативних захворювань |
| EP2794596B1 (en) | 2011-12-21 | 2017-05-31 | Bayer Intellectual Property GmbH | Substituted benzylpyrazoles |
| WO2014147204A1 (en) * | 2013-03-21 | 2014-09-25 | Bayer Pharma Aktiengesellschaft | Heteroaryl substituted indazoles |
| HK1217324A1 (zh) * | 2013-03-21 | 2017-01-06 | Bayer Pharma Aktiengesellschaft | 二氨基杂芳基取代的吲唑 |
| CA2916194A1 (en) | 2013-06-21 | 2014-12-24 | Bayer Pharma Aktiengesellschaft | Heteroaryl substituted pyrazoles |
| CN105408324A (zh) | 2013-06-21 | 2016-03-16 | 拜耳制药股份公司 | 取代的苄基吡唑 |
| US9682974B2 (en) | 2013-10-30 | 2017-06-20 | Bayer Pharma Aktiengesellschaft | Heteroaryl substituted pyrazoles |
| CA2935392C (en) | 2014-01-01 | 2022-07-26 | Medivation Technologies, Inc. | Amino pyridine derivatives for the treatment of conditions associated with excessive tgf.beta activity |
| JP6545199B2 (ja) | 2014-06-17 | 2019-07-17 | バイエル ファーマ アクチエンゲゼルシャフト | ３−アミノ−１，５，６，７−テトラヒドロ−４ｈ−インドール−４−オン類 |
| CN107148420A (zh) * | 2014-09-19 | 2017-09-08 | 拜耳制药股份公司 | 苄基取代的吲唑类化合物 |
| WO2016042084A1 (en) | 2014-09-19 | 2016-03-24 | Bayer Pharma Aktiengesellschaft | Benzyl substituted indazoles as bub1 inhibitors |
| SG11201705908VA (en) | 2015-01-28 | 2017-08-30 | Bayer Pharma AG | 4h-pyrrolo[3,2-c]pyridin-4-one derivatives |
| CN107922389A (zh) | 2015-06-17 | 2018-04-17 | 拜耳制药股份公司 | 3‑氨基‑1,5,6,7‑四氢‑4h‑吲哚‑4‑酮 |
| WO2017102649A1 (en) * | 2015-12-16 | 2017-06-22 | Bayer Pharma Aktiengesellschaft | Hetero-1,5,6,7-tetrahydro-4h-indol-4-ones |
| WO2017148995A1 (en) | 2016-03-04 | 2017-09-08 | Bayer Pharma Aktiengesellschaft | 1-(pyrimidin-2-yl)-1h-indazoles having bub1 kinase inhibiting activity |
| WO2017157991A1 (en) | 2016-03-18 | 2017-09-21 | Bayer Pharma Aktiengesellschaft | 1-alkyl-pyrazoles and -indazoles as bub1 inhibitors for the treatment of hyperproliferative diseases |
| WO2017157992A1 (en) | 2016-03-18 | 2017-09-21 | Bayer Pharma Aktiengesellschaft | Annulated pyrazoles as bub1 kinase inhibitors for treating proliferative disorders |
| WO2018122168A1 (en) | 2016-12-29 | 2018-07-05 | Bayer Pharma Aktiengesellschaft | Combinations of bub1 kinase and parp inhibitors |
| WO2018158175A1 (en) | 2017-02-28 | 2018-09-07 | Bayer Pharma Aktiengesellschaft | Combination of bub1 inhibitors |
| WO2018206547A1 (en) | 2017-05-12 | 2018-11-15 | Bayer Pharma Aktiengesellschaft | Combination of bub1 and atr inhibitors |
| WO2018215282A1 (en) | 2017-05-26 | 2018-11-29 | Bayer Pharma Aktiengesellschaft | Combination of bub1 and pi3k inhibitors |
| EP4217070A1 (en) | 2020-09-23 | 2023-08-02 | Scorpion Therapeutics, Inc. | Pyrrolo[3,2-c]pyridin-4-one derivatives useful in the treatment of cancer |
| WO2022072634A1 (en) | 2020-09-30 | 2022-04-07 | Scorpion Therapeutics, Inc. | Bicyclic compounds for use in the treatment cancer |
| WO2022072645A2 (en) | 2020-09-30 | 2022-04-07 | Scorpion Therapeutics, Inc. | Methods for treating cancer |
| KR20230107419A (ko) | 2020-10-09 | 2023-07-14 | 스코르피온 테라퓨틱스, 인코퍼레이티드 | 암 치료 방법 |
| WO2022094271A1 (en) | 2020-10-30 | 2022-05-05 | Scorpion Therapeutics, Inc. | Methods for treating cancer |
| WO2022098992A1 (en) | 2020-11-05 | 2022-05-12 | Scorpion Therapeutics, Inc. | Use of macrocyclic compounds in methods of treating cancer |
| WO2022197913A1 (en) | 2021-03-18 | 2022-09-22 | Scorpion Therapeutics, Inc. | Bicyclic derivatives which can be used to treat cancer |
| WO2023173083A1 (en) | 2022-03-11 | 2023-09-14 | Scorpion Therapeutics, Inc. | Tetrahydroindole derivatives as egfr and/or her2 inhibtors useful for the treatment of cancer |
| EP4293019A1 (en) * | 2022-06-13 | 2023-12-20 | Netherlands Translational Research Center Holding B.V. | 4-substituted (1h-benzo[d]imidazol-2-yl)-1h-pyrazoles as bub1 inhibitors useful for treating cancers |
| CN118772140A (zh) * | 2023-04-07 | 2024-10-15 | 四川大学 | 一类化合物及其在治疗hDHODH介导的疾病中的用途 |
| WO2024254266A1 (en) | 2023-06-08 | 2024-12-12 | Scorpion Therapeutics, Inc. | A 1,5-dihydro-4h-pyrrolo[3,2-c] pyridin-4-one for use in the treatment of cancer |
| WO2024254298A1 (en) | 2023-06-08 | 2024-12-12 | Scorpion Therapeutics, Inc. | A 1,5-dihydro-4h-pyrrolo[3,2-c] pyridin-4-one for use in the treatment of cancer |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5011472A (en) | 1988-09-06 | 1991-04-30 | Brown University Research Foundation | Implantable delivery system for biological factors |
| US6837294B2 (en) * | 2003-02-10 | 2005-01-04 | Zipshade Industrial (B.V.I.) Corp. | Pull down, push up, shade assembly |
| AU2006276088A1 (en) * | 2005-07-26 | 2007-02-08 | Vertex Pharmaceuticals Incorporated | Benzimidazoles useful as inhibitors of protein kinases |
| JP2010111624A (ja) * | 2008-11-06 | 2010-05-20 | Shionogi & Co Ltd | Ｔｔｋ阻害作用を有するインダゾール誘導体 |
| WO2011115804A1 (en) * | 2010-03-17 | 2011-09-22 | Ironwood Pharmaceuticals, Inc. | Sgc stimulators |
| EP2702055A1 (en) * | 2011-04-11 | 2014-03-05 | Nerviano Medical Sciences S.r.l. | Pyrazolyl-pyrimidine derivatives as kinase inhibitors |
| UA111754C2 (uk) * | 2011-10-06 | 2016-06-10 | Байєр Фарма Акцієнгезелльшафт | Заміщені бензиліндазоли для застосування як інгібіторів bub1-кінази для лікування гіперпроліферативних захворювань |
| EP2794596B1 (en) | 2011-12-21 | 2017-05-31 | Bayer Intellectual Property GmbH | Substituted benzylpyrazoles |
| DE102012200352A1 (de) * | 2012-01-11 | 2013-07-11 | Bayer Intellectual Property Gmbh | Substituierte, annellierte Imidazole und Pyrazole und ihre Verwendung |
| WO2013167698A1 (en) | 2012-05-11 | 2013-11-14 | Bayer Pharma Aktiengesellschaft | Substituted cycloalkenopyrazoles as bub1 inhibitors for the treatment of cancer |
| WO2014147204A1 (en) * | 2013-03-21 | 2014-09-25 | Bayer Pharma Aktiengesellschaft | Heteroaryl substituted indazoles |
| HK1217324A1 (zh) * | 2013-03-21 | 2017-01-06 | Bayer Pharma Aktiengesellschaft | 二氨基杂芳基取代的吲唑 |
-
2014
- 2014-03-20 EP EP14714196.4A patent/EP2976336A1/en not_active Withdrawn
- 2014-03-20 CN CN201480029308.7A patent/CN105209455A/zh active Pending
- 2014-03-20 CA CA2907592A patent/CA2907592A1/en not_active Abandoned
- 2014-03-20 JP JP2016503668A patent/JP2016514718A/ja active Pending
- 2014-03-20 WO PCT/EP2014/055657 patent/WO2014147203A1/en not_active Ceased
- 2014-03-20 US US14/778,975 patent/US20160046610A1/en not_active Abandoned
- 2014-03-20 HK HK16106728.8A patent/HK1218750A1/zh unknown
- 2014-03-21 TW TW103110770A patent/TW201514166A/zh unknown
- 2014-03-21 AR ARP140101319A patent/AR095706A1/es unknown
- 2014-03-24 UY UY0001035500A patent/UY35500A/es not_active Application Discontinuation
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