JP2014528433A5 - - Google Patents
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- Publication number
- JP2014528433A5 JP2014528433A5 JP2014533881A JP2014533881A JP2014528433A5 JP 2014528433 A5 JP2014528433 A5 JP 2014528433A5 JP 2014533881 A JP2014533881 A JP 2014533881A JP 2014533881 A JP2014533881 A JP 2014533881A JP 2014528433 A5 JP2014528433 A5 JP 2014528433A5
- Authority
- JP
- Japan
- Prior art keywords
- tetrahydropyrrolo
- pyrazin
- acetamide
- oxo
- formula
- 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
Links
- DLFVBJFMPXGRIB-UHFFFAOYSA-N Acetamide Chemical compound CC(N)=O DLFVBJFMPXGRIB-UHFFFAOYSA-N 0.000 claims 44
- 150000001875 compounds Chemical class 0.000 claims 29
- 125000000623 heterocyclic group Chemical group 0.000 claims 22
- 125000004195 4-methylpiperazin-1-yl group Chemical group [H]C([H])([H])N1C([H])([H])C([H])([H])N(*)C([H])([H])C1([H])[H] 0.000 claims 17
- -1 3,4-difluorophenyl Chemical group 0.000 claims 16
- 125000004415 heterocyclylalkyl group Chemical group 0.000 claims 16
- 125000003710 aryl alkyl group Chemical group 0.000 claims 15
- 125000000753 cycloalkyl group Chemical group 0.000 claims 14
- 125000004179 3-chlorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C(Cl)=C1[H] 0.000 claims 13
- 125000003118 aryl group Chemical group 0.000 claims 13
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 13
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 claims 12
- 229910052739 hydrogen Inorganic materials 0.000 claims 12
- 239000001257 hydrogen Substances 0.000 claims 12
- 125000002147 dimethylamino group Chemical group [H]C([H])([H])N(*)C([H])([H])[H] 0.000 claims 9
- 150000003839 salts Chemical class 0.000 claims 9
- 125000004180 3-fluorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C(F)=C1[H] 0.000 claims 8
- 229910052736 halogen Inorganic materials 0.000 claims 7
- 150000002431 hydrogen Chemical group 0.000 claims 7
- 238000000034 method Methods 0.000 claims 7
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 6
- KDLHZDBZIXYQEI-UHFFFAOYSA-N Palladium Chemical compound [Pd] KDLHZDBZIXYQEI-UHFFFAOYSA-N 0.000 claims 6
- SNOOUWRIMMFWNE-UHFFFAOYSA-M sodium;6-[(3,4,5-trimethoxybenzoyl)amino]hexanoate Chemical compound [Na+].COC1=CC(C(=O)NCCCCCC([O-])=O)=CC(OC)=C1OC SNOOUWRIMMFWNE-UHFFFAOYSA-M 0.000 claims 6
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 5
- 125000000217 alkyl group Chemical group 0.000 claims 5
- 238000006243 chemical reaction Methods 0.000 claims 4
- 125000005843 halogen group Chemical group 0.000 claims 4
- 125000005842 heteroatom Chemical group 0.000 claims 4
- 229910052757 nitrogen Inorganic materials 0.000 claims 4
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 4
- 229910052760 oxygen Inorganic materials 0.000 claims 4
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 4
- 229910052717 sulfur Inorganic materials 0.000 claims 4
- 230000009466 transformation Effects 0.000 claims 4
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 4
- 125000004093 cyano group Chemical group *C#N 0.000 claims 3
- 239000003814 drug Substances 0.000 claims 3
- 150000002367 halogens Chemical group 0.000 claims 3
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 3
- 229910052763 palladium Inorganic materials 0.000 claims 3
- 101100297652 Coturnix japonica PIM3 gene Proteins 0.000 claims 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 2
- 101100297651 Mus musculus Pim2 gene Proteins 0.000 claims 2
- 101001001642 Xenopus laevis Serine/threonine-protein kinase pim-3 Proteins 0.000 claims 2
- 150000001345 alkine derivatives Chemical group 0.000 claims 2
- 239000002246 antineoplastic agent Substances 0.000 claims 2
- 238000006664 bond formation reaction Methods 0.000 claims 2
- 229910052799 carbon Inorganic materials 0.000 claims 2
- 229940127089 cytotoxic agent Drugs 0.000 claims 2
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 2
- 230000001404 mediated effect Effects 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 125000002914 sec-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 2
- 125000004208 3-hydroxyphenyl group Chemical group [H]OC1=C([H])C([H])=C([H])C(*)=C1[H] 0.000 claims 1
- 230000001093 anti-cancer Effects 0.000 claims 1
- 238000011319 anticancer therapy Methods 0.000 claims 1
- 150000001502 aryl halides Chemical class 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 238000007333 cyanation reaction Methods 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 230000002140 halogenating effect Effects 0.000 claims 1
- 238000000338 in vitro Methods 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 1
- 125000006239 protecting group Chemical group 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP11184337 | 2011-10-07 | ||
| EP11184337.1 | 2011-10-07 | ||
| PCT/EP2012/069586 WO2013050446A1 (en) | 2011-10-07 | 2012-10-04 | SUBSTITUTED 3,4-DIHYDROPYRROLO[1,2-a]PYRAZIN-1(2H)-ONE DERIVATIVES AS KINASES INHIBITORS |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2014528433A JP2014528433A (ja) | 2014-10-27 |
| JP2014528433A5 true JP2014528433A5 (enExample) | 2015-11-19 |
| JP5998223B2 JP5998223B2 (ja) | 2016-09-28 |
Family
ID=46970303
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014533881A Expired - Fee Related JP5998223B2 (ja) | 2011-10-07 | 2012-10-04 | キナーゼ阻害剤としての置換３，４−ジヒドロピロロ［１，２−ａ］ピラジン−１（２Ｈ）−オン誘導体 |
Country Status (5)
| Country | Link |
|---|---|
| US (1) | US9145418B2 (enExample) |
| EP (1) | EP2788351B1 (enExample) |
| JP (1) | JP5998223B2 (enExample) |
| ES (1) | ES2639064T3 (enExample) |
| WO (1) | WO2013050446A1 (enExample) |
Families Citing this family (42)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AR077468A1 (es) | 2009-07-09 | 2011-08-31 | Array Biopharma Inc | Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa |
| EP2751177B1 (en) * | 2011-08-31 | 2016-11-09 | Dow Global Technologies LLC | Method for preparing flexible polyurethane foam with hydrolysable silane compounds |
| ES2649156T3 (es) | 2013-01-14 | 2018-01-10 | Incyte Holdings Corporation | Compuestos bicíclicos de carboxamida aromática útiles como inhibidores de quinasas Pim |
| ES2941292T3 (es) | 2013-01-15 | 2023-05-19 | Incyte Holdings Corp | Tiazolecarboxamidas y compuestos de piridinecarboxamida útiles como inhibidores de PIM quinasa |
| AR097431A1 (es) | 2013-08-23 | 2016-03-16 | Incyte Corp | Compuestos de carboxamida de furo y tienopiridina útiles como inhibidores de quinasas pim |
| US9580418B2 (en) | 2014-07-14 | 2017-02-28 | Incyte Corporation | Bicyclic aromatic carboxamide compounds useful as Pim kinase inhibitors |
| US9822124B2 (en) | 2014-07-14 | 2017-11-21 | Incyte Corporation | Bicyclic heteroaromatic carboxamide compounds useful as Pim kinase inhibitors |
| WO2016100166A1 (en) | 2014-12-15 | 2016-06-23 | Bristol-Myers Squibb Company | SUBSTITUTED DIHYDRO-1H-PYRROLO[3,2-c]PYRIDIN-4(5H)-ONES AS RIPK3 INHIBITORS |
| WO2016196244A1 (en) | 2015-05-29 | 2016-12-08 | Incyte Corporation | Pyridineamine compounds useful as pim kinase inhibitors |
| WO2017011776A1 (en) | 2015-07-16 | 2017-01-19 | Array Biopharma, Inc. | Substituted pyrazolo[1,5-a]pyridine compounds as ret kinase inhibitors |
| AR105967A1 (es) | 2015-09-09 | 2017-11-29 | Incyte Corp | Sales de un inhibidor de pim quinasa |
| US9920032B2 (en) | 2015-10-02 | 2018-03-20 | Incyte Corporation | Heterocyclic compounds useful as pim kinase inhibitors |
| CA3003153A1 (en) | 2015-10-26 | 2017-05-04 | Loxo Oncology, Inc. | Point mutations in trk inhibitor-resistant cancer and methods relating to the same |
| MA44612B1 (fr) | 2016-04-04 | 2024-09-30 | Loxo Oncology, Inc. | Méthodes de traitement de cancers pédiatriques |
| US10045991B2 (en) | 2016-04-04 | 2018-08-14 | Loxo Oncology, Inc. | Methods of treating pediatric cancers |
| DK3439662T3 (da) | 2016-04-04 | 2024-09-02 | Loxo Oncology Inc | Væskeformige formuleringer af (s)-n-(5-((r)-2-(2,5-difluorphenyl)-pyrrolidin-1-yl)-pyrazol[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidin-1-carboxamid |
| EP3458456B1 (en) | 2016-05-18 | 2020-11-25 | Loxo Oncology Inc. | Preparation of (s)-n-(5-((r)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide |
| JOP20190077A1 (ar) | 2016-10-10 | 2019-04-09 | Array Biopharma Inc | مركبات بيرازولو [1، 5-a]بيريدين بها استبدال كمثبطات كيناز ret |
| TWI704148B (zh) | 2016-10-10 | 2020-09-11 | 美商亞雷生物製藥股份有限公司 | 作為ｒｅｔ激酶抑制劑之經取代吡唑并[1,5-a]吡啶化合物 |
| JOP20190092A1 (ar) | 2016-10-26 | 2019-04-25 | Array Biopharma Inc | عملية لتحضير مركبات بيرازولو[1، 5-a]بيريميدين وأملاح منها |
| JP6888101B2 (ja) | 2017-01-18 | 2021-06-16 | アレイ バイオファーマ インコーポレイテッド | ＲＥＴキナーゼ阻害剤としての置換ピラゾロ［１，５−ａ］ピラジン化合物 |
| WO2018136663A1 (en) | 2017-01-18 | 2018-07-26 | Array Biopharma, Inc. | Ret inhibitors |
| JOP20190213A1 (ar) | 2017-03-16 | 2019-09-16 | Array Biopharma Inc | مركبات حلقية ضخمة كمثبطات لكيناز ros1 |
| TWI791053B (zh) | 2017-10-10 | 2023-02-01 | 美商亞雷生物製藥股份有限公司 | 6-(2-羥基-2-甲基丙氧基)-4-(6-(6-((6-甲氧基吡啶-3-基)甲基)-3,6-二氮雜雙環[3.1.1]庚-3-基)吡啶-3-基)吡唑并[1,5-a]吡啶-3-甲腈之結晶形式及其醫藥組合物 |
| TWI876442B (zh) | 2017-10-10 | 2025-03-11 | 美商絡速藥業公司 | 6-(2-羥基-2-甲基丙氧基)-4-(6-(6-((6-甲氧基吡啶-3-基)甲基)-3,6-二氮雜雙環[3.1.1]庚-3-基)吡啶-3-基)吡唑并[1,5-a]吡啶-3-甲腈之調配物 |
| WO2019113487A1 (en) | 2017-12-08 | 2019-06-13 | Incyte Corporation | Low dose combination therapy for treatment of myeloproliferative neoplasms |
| US11524963B2 (en) | 2018-01-18 | 2022-12-13 | Array Biopharma Inc. | Substituted pyrazolo[3,4-d]pyrimidines as RET kinase inhibitors |
| US11472802B2 (en) | 2018-01-18 | 2022-10-18 | Array Biopharma Inc. | Substituted pyrazolyl[4,3-c]pyridine compounds as RET kinase inhibitors |
| EP3740491A1 (en) | 2018-01-18 | 2020-11-25 | Array Biopharma, Inc. | Substituted pyrrolo[2,3-d]pyrimidines compounds as ret kinase inhibitors |
| CN112165944B (zh) | 2018-03-29 | 2024-04-09 | 德州大学系统董事会 | 转录激活蛋白的咪唑并哌嗪抑制剂 |
| WO2019195846A1 (en) * | 2018-04-06 | 2019-10-10 | Board Of Regents, The University Of Texas System | Imidazopiperazinone inhibitors of transcription activating proteins |
| CN113194928A (zh) | 2018-07-31 | 2021-07-30 | 罗索肿瘤学公司 | (s)-5-氨基-3-(4-((5-氟-2-甲氧基苯甲酰胺基)甲基)苯基)-1-(1,1,1-三氟丙-2-基)-1h-吡唑-4-甲酰胺的喷雾干燥的分散体和制剂 |
| EP3849986B1 (en) | 2018-09-10 | 2022-06-08 | Array Biopharma, Inc. | Fused heterocyclic compounds as ret kinase inhibitors |
| JP2022515197A (ja) | 2018-12-19 | 2022-02-17 | アレイ バイオファーマ インコーポレイテッド | がんを治療するためのｆｇｆｒ阻害剤としての７－（（３，５－ジメトキシフェニル）アミノ）キノキサリン誘導体 |
| WO2020131627A1 (en) | 2018-12-19 | 2020-06-25 | Array Biopharma Inc. | Substituted pyrazolo[1,5-a]pyridine compounds as inhibitors of fgfr tyrosine kinases |
| CN113825757B (zh) * | 2019-05-24 | 2023-10-20 | 江苏恒瑞医药股份有限公司 | 取代的稠合双环类衍生物、其制备方法及其在医药上的应用 |
| EP4069369A4 (en) | 2019-12-06 | 2024-02-14 | Schrödinger, Inc. | CYCLIC COMPOUNDS AND METHODS OF USE THEREOF |
| MX2022007171A (es) | 2019-12-27 | 2022-08-22 | Schroedinger Inc | Compuestos cíclicos y métodos de uso de estos. |
| US20230365584A1 (en) | 2020-09-10 | 2023-11-16 | Schrödinger, Inc. | Heterocyclic pericondensed cdc7 kinase inhibitors for the treatment of cancer |
| US20240148732A1 (en) | 2021-01-26 | 2024-05-09 | Schrödinger, Inc. | Tricyclic compounds useful in the treatment of cancer, autoimmune and inflammatory disorders |
| TW202300150A (zh) | 2021-03-18 | 2023-01-01 | 美商薛定諤公司 | 環狀化合物及其使用方法 |
| WO2025059027A1 (en) | 2023-09-11 | 2025-03-20 | Schrödinger, Inc. | Cyclopenta[e]pyrazolo[1,5-a]pyrimidine derivatives as malt1 inhibitors |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB0520958D0 (en) * | 2005-10-14 | 2005-11-23 | Cyclacel Ltd | Compound |
| US8207165B2 (en) * | 2008-03-28 | 2012-06-26 | Nerviano Medical Sciences S.R.L. | 3,4-dihydro-2H-pyrazino[1,2-A]indol-1-one derivatives active as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them |
| EP2376492B1 (en) | 2008-09-19 | 2015-04-08 | Nerviano Medical Sciences S.r.l. | 3,4 DIHYDRO-2H-PYRROLO[1,2-a]PYRAZIN-1-ONE DERIVATIVES |
| WO2011092120A1 (en) * | 2010-01-29 | 2011-08-04 | Nerviano Medical Sciences S.R.L. | 6,7- dihydroimidazo [1,5-a] pyrazin-8 (5h) - one derivatives as protein kinase modulators |
-
2012
- 2012-10-04 EP EP12768820.8A patent/EP2788351B1/en active Active
- 2012-10-04 JP JP2014533881A patent/JP5998223B2/ja not_active Expired - Fee Related
- 2012-10-04 ES ES12768820.8T patent/ES2639064T3/es active Active
- 2012-10-04 WO PCT/EP2012/069586 patent/WO2013050446A1/en not_active Ceased
- 2012-10-04 US US14/349,516 patent/US9145418B2/en active Active
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