JP2016525075A5 - - Google Patents
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- Publication number
- JP2016525075A5 JP2016525075A5 JP2016520440A JP2016520440A JP2016525075A5 JP 2016525075 A5 JP2016525075 A5 JP 2016525075A5 JP 2016520440 A JP2016520440 A JP 2016520440A JP 2016520440 A JP2016520440 A JP 2016520440A JP 2016525075 A5 JP2016525075 A5 JP 2016525075A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- hydrogen
- methyl
- cyano
- halogen
- 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 28
- 239000001257 hydrogen Substances 0.000 claims 28
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 20
- 125000004093 cyano group Chemical group *C#N 0.000 claims 18
- 150000001875 compounds Chemical class 0.000 claims 14
- 229910052736 halogen Inorganic materials 0.000 claims 14
- 150000002367 halogens Chemical class 0.000 claims 14
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 10
- 150000003839 salts Chemical class 0.000 claims 10
- 125000001072 heteroaryl group Chemical group 0.000 claims 8
- 150000002431 hydrogen Chemical class 0.000 claims 8
- 150000001204 N-oxides Chemical class 0.000 claims 7
- 201000010099 disease Diseases 0.000 claims 7
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 7
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 5
- -1 compound N-oxides Chemical class 0.000 claims 4
- 125000003545 alkoxy group Chemical group 0.000 claims 3
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 3
- 230000003463 hyperproliferative effect Effects 0.000 claims 3
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 3
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 claims 2
- 206010027476 Metastases Diseases 0.000 claims 2
- 206010028980 Neoplasm Diseases 0.000 claims 2
- DFPAKSUCGFBDDF-UHFFFAOYSA-N Nicotinamide Chemical compound NC(=O)C1=CC=CN=C1 DFPAKSUCGFBDDF-UHFFFAOYSA-N 0.000 claims 2
- 239000004480 active ingredient Substances 0.000 claims 2
- 239000002246 antineoplastic agent Substances 0.000 claims 2
- 230000030833 cell death Effects 0.000 claims 2
- 230000006698 induction Effects 0.000 claims 2
- JLSFEGFHCJIKFV-UHFFFAOYSA-N 4-[[2-[5-cyclopropyl-1-[(3,5-dimethyl-1,2-oxazol-4-yl)methyl]-4-methylpyrazol-3-yl]-5-methoxypyrimidin-4-yl]amino]pyridine-3-carboxylic acid Chemical compound COC1=CN=C(C=2C(=C(C3CC3)N(CC3=C(ON=C3C)C)N=2)C)N=C1NC1=CC=NC=C1C(O)=O JLSFEGFHCJIKFV-UHFFFAOYSA-N 0.000 claims 1
- LTDGTLBKPUPVFW-UHFFFAOYSA-N 4-[[2-[5-cyclopropyl-4-methyl-1-[(5-methyl-1,3,4-oxadiazol-2-yl)methyl]pyrazol-3-yl]-5-methoxypyrimidin-4-yl]amino]pyridine-3-carboxamide Chemical compound COC1=CN=C(C=2C(=C(C3CC3)N(CC=3OC(C)=NN=3)N=2)C)N=C1NC1=CC=NC=C1C(N)=O LTDGTLBKPUPVFW-UHFFFAOYSA-N 0.000 claims 1
- 206010008342 Cervix carcinoma Diseases 0.000 claims 1
- UKJOGGGOUJANNH-UHFFFAOYSA-N ClC=1C=NN(C=1CN1N=C(C(=C1C1CC1)C)C1=NC=C(C(=N1)NC1=CC=NC=C1)OC)C Chemical compound ClC=1C=NN(C=1CN1N=C(C(=C1C1CC1)C)C1=NC=C(C(=N1)NC1=CC=NC=C1)OC)C UKJOGGGOUJANNH-UHFFFAOYSA-N 0.000 claims 1
- PVNIIMVLHYAWGP-UHFFFAOYSA-N Niacin Chemical compound OC(=O)C1=CC=CN=C1 PVNIIMVLHYAWGP-UHFFFAOYSA-N 0.000 claims 1
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims 1
- 239000002671 adjuvant Substances 0.000 claims 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 1
- 201000010881 cervical cancer Diseases 0.000 claims 1
- 230000000973 chemotherapeutic effect Effects 0.000 claims 1
- 125000001309 chloro group Chemical group Cl* 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 201000005787 hematologic cancer Diseases 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
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 235000005152 nicotinamide Nutrition 0.000 claims 1
- 239000011570 nicotinamide Substances 0.000 claims 1
- 229960003966 nicotinamide Drugs 0.000 claims 1
- PVNIIMVLHYAWGP-UHFFFAOYSA-M nicotinate Chemical compound [O-]C(=O)C1=CC=CN=C1 PVNIIMVLHYAWGP-UHFFFAOYSA-M 0.000 claims 1
- 235000001968 nicotinic acid Nutrition 0.000 claims 1
- 239000011664 nicotinic acid Substances 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 125000001424 substituent group Chemical group 0.000 claims 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 1
- 0 CC(*C1(C)C=N*=*C(N(*)c2nc(-c3n[n](C*)c(**)c3*)nc(*)c2*)=C1)N Chemical compound CC(*C1(C)C=N*=*C(N(*)c2nc(-c3n[n](C*)c(**)c3*)nc(*)c2*)=C1)N 0.000 description 1
- HOBJEFOCIRXQKH-UHFFFAOYSA-O [OH2+]CC(CC1)NC1=O Chemical compound [OH2+]CC(CC1)NC1=O HOBJEFOCIRXQKH-UHFFFAOYSA-O 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP13173298.4 | 2013-06-21 | ||
| EP13173298 | 2013-06-21 | ||
| PCT/EP2014/062689 WO2014202584A1 (en) | 2013-06-21 | 2014-06-17 | Heteroaryl substituted pyrazoles |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2016525075A JP2016525075A (ja) | 2016-08-22 |
| JP2016525075A5 true JP2016525075A5 (enExample) | 2017-07-20 |
Family
ID=48651939
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016520440A Pending JP2016525075A (ja) | 2013-06-21 | 2014-06-17 | ヘテロアリール置換ピラゾール類 |
Country Status (8)
| Country | Link |
|---|---|
| US (1) | US9745285B2 (enExample) |
| EP (1) | EP3010901B1 (enExample) |
| JP (1) | JP2016525075A (enExample) |
| CN (1) | CN105452237A (enExample) |
| CA (1) | CA2916194A1 (enExample) |
| ES (1) | ES2652305T3 (enExample) |
| HK (1) | HK1223098A1 (enExample) |
| WO (1) | WO2014202584A1 (enExample) |
Families Citing this family (27)
| 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 |
| CN104125957B (zh) | 2011-12-21 | 2016-05-25 | 拜耳知识产权有限责任公司 | 取代的苄基吡唑 |
| US20160046604A1 (en) * | 2013-03-21 | 2016-02-18 | Bayer Pharma Aktiengesellschaft | Heteroaryl substituted indazoles |
| EP3010911A1 (en) * | 2013-06-21 | 2016-04-27 | Bayer Pharma Aktiengesellschaft | Heteroaryl substituted pyrazoles |
| WO2014202590A1 (en) | 2013-06-21 | 2014-12-24 | Bayer Pharma Aktiengesellschaft | Substituted benzylpyrazoles |
| CN105764893A (zh) | 2013-10-30 | 2016-07-13 | 拜耳制药股份公司 | 杂芳基取代的吡唑 |
| TW201613886A (en) | 2014-06-17 | 2016-04-16 | Bayer Pharma AG | 3-amino-1,5,6,7-tetrahydro-4h-indol-4-ones |
| WO2016042084A1 (en) | 2014-09-19 | 2016-03-24 | Bayer Pharma Aktiengesellschaft | Benzyl substituted indazoles as bub1 inhibitors |
| CN107406417B (zh) | 2015-01-28 | 2020-06-09 | 拜耳制药股份公司 | 4H-吡咯并[3,2-c]吡啶-4-酮衍生物 |
| 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 |
| 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 |
| MX2023003362A (es) | 2020-09-23 | 2023-05-30 | Scorpion Therapeutics Inc | Derivados de pirrolo[3,2-c]piridin-4-ona utiles en el tratamiento del cancer. |
| TW202229282A (zh) | 2020-09-30 | 2022-08-01 | 美商史考皮恩治療有限公司 | 治療癌症之方法 |
| WO2022072645A2 (en) | 2020-09-30 | 2022-04-07 | Scorpion Therapeutics, Inc. | Methods for treating cancer |
| BR112023006531A2 (pt) | 2020-10-09 | 2023-10-03 | Scorpion Therapeutics Inc | Inibidores heterocílicos de egfr e/ou her2, para uso no tratamento de câncer |
| 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 |
| 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 |
| EP4724150A1 (en) | 2023-06-08 | 2026-04-15 | Antares Therapeutics, Inc. | A 1,5-dihydro-4h-pyrrolo[3,2-c] pyridin-4-one for use in the treatment of cancer |
Family Cites Families (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7863282B2 (en) * | 2003-03-14 | 2011-01-04 | Vertex Pharmaceuticals Incorporated | Compositions useful as inhibitors of protein kinases |
| CN102666537A (zh) | 2009-10-20 | 2012-09-12 | 艾格尔生物制药股份有限公司 | 治疗黄病毒科病毒感染的氮杂吲唑 |
| US20130178475A1 (en) | 2010-03-17 | 2013-07-11 | Ironwood Pharmaceuticals, Inc. | sGC STIMULATORS |
| SG10201502484SA (en) | 2010-03-30 | 2015-05-28 | Verseon Corp | Multisubstituted aromatic compounds as inhibitors of thrombin |
| TWI532737B (zh) * | 2010-06-30 | 2016-05-11 | 艾諾屋製藥公司 | 可溶性鳥苷酸環化酶（ｓＧＣ）刺激物 |
| UA111754C2 (uk) | 2011-10-06 | 2016-06-10 | Байєр Фарма Акцієнгезелльшафт | Заміщені бензиліндазоли для застосування як інгібіторів bub1-кінази для лікування гіперпроліферативних захворювань |
| CN104125957B (zh) | 2011-12-21 | 2016-05-25 | 拜耳知识产权有限责任公司 | 取代的苄基吡唑 |
| CA2861804C (en) | 2011-12-27 | 2021-10-26 | Ironwood Pharmaceuticals, Inc. | 2-benzyl,3(pyrimidin-2-yl)substituted pyrazoles useful as sgc stimulators |
| EP2847180B1 (en) | 2012-05-11 | 2017-01-04 | Bayer Pharma Aktiengesellschaft | Substituted cycloalkenopyrazoles as bub1 inhibitors for the treatment of cancer |
| WO2014047111A1 (en) | 2012-09-18 | 2014-03-27 | Ironwood Pharmaceuticals, Inc. | Sgc stimulators |
| EP2897953B8 (en) | 2012-09-19 | 2019-06-26 | Cyclerion Therapeutics, Inc. | Sgc stimulators |
| CA2907730A1 (en) | 2013-03-21 | 2014-09-25 | Bayer Pharma Aktiengesellschaft | Diaminoheteroaryl substituted indazoles |
| US20160046604A1 (en) | 2013-03-21 | 2016-02-18 | Bayer Pharma Aktiengesellschaft | Heteroaryl substituted indazoles |
| EP2976336A1 (en) | 2013-03-21 | 2016-01-27 | Bayer Pharma Aktiengesellschaft | 3-heteroaryl substituted indazoles |
| JP2016522231A (ja) | 2013-06-21 | 2016-07-28 | バイエル ファーマ アクチエンゲゼルシャフト | ジアミノヘテロアリール置換ピラゾール類 |
| WO2014202583A1 (en) | 2013-06-21 | 2014-12-24 | Bayer Pharma Aktiengesellschaft | Substituted benzylpyrazoles |
| WO2014202590A1 (en) | 2013-06-21 | 2014-12-24 | Bayer Pharma Aktiengesellschaft | Substituted benzylpyrazoles |
| EP3010911A1 (en) | 2013-06-21 | 2016-04-27 | Bayer Pharma Aktiengesellschaft | Heteroaryl substituted pyrazoles |
| CN105764893A (zh) | 2013-10-30 | 2016-07-13 | 拜耳制药股份公司 | 杂芳基取代的吡唑 |
| CA2961578A1 (en) | 2014-09-19 | 2016-03-24 | Bayer Pharma Aktiengesellschaft | Benzyl substituted indazoles as bub1 kinase inhibitors |
| WO2016042081A1 (en) | 2014-09-19 | 2016-03-24 | Bayer Pharma Aktiengesellschaft | Benzyl substituted indazoles as bub1 kinase inhibitors |
| CA2961570A1 (en) | 2014-09-19 | 2016-03-24 | Lars Barfacker | Benzyl substituted indazoles |
| WO2016042084A1 (en) | 2014-09-19 | 2016-03-24 | Bayer Pharma Aktiengesellschaft | Benzyl substituted indazoles as bub1 inhibitors |
-
2014
- 2014-06-17 US US14/900,548 patent/US9745285B2/en not_active Expired - Fee Related
- 2014-06-17 CN CN201480045754.7A patent/CN105452237A/zh active Pending
- 2014-06-17 CA CA2916194A patent/CA2916194A1/en not_active Abandoned
- 2014-06-17 ES ES14730544.5T patent/ES2652305T3/es active Active
- 2014-06-17 EP EP14730544.5A patent/EP3010901B1/en not_active Not-in-force
- 2014-06-17 JP JP2016520440A patent/JP2016525075A/ja active Pending
- 2014-06-17 WO PCT/EP2014/062689 patent/WO2014202584A1/en not_active Ceased
- 2014-06-17 HK HK16111252.2A patent/HK1223098A1/zh unknown
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