JPWO2021086833A5 - - Google Patents
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- JPWO2021086833A5 JPWO2021086833A5 JP2022524665A JP2022524665A JPWO2021086833A5 JP WO2021086833 A5 JPWO2021086833 A5 JP WO2021086833A5 JP 2022524665 A JP2022524665 A JP 2022524665A JP 2022524665 A JP2022524665 A JP 2022524665A JP WO2021086833 A5 JPWO2021086833 A5 JP WO2021086833A5
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- Prior art keywords
- pharmaceutically acceptable
- compound
- enoyl
- piperazin
- prop
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Claims (22)
(5aSa,17aRa)-20-クロロ-2-[(2S,5R)-2,5-ジメチル-4-(プロプ-2-エノイル)ピペラジン-1-イル]-14,17-ジフルオロ-6-(プロパン-2-イル)-11,12-ジヒドロ-4H-1,18-(エタンジイリデン)ピリド[4,3-e]ピリミド[1,6-g][1,4,7,9]ベンゾジオキサジアザシクロドデシン-4-オン;
(5aSa,17aRa)-20-クロロ-2-[(2S,5R)-2,5-ジメチル-4-(プロプ-2-エノイル)ピペラジン-1-イル]-14,17-ジフルオロ-6-(プロパン-2-イル)-11,12-ジ[(2H)ヒドロ](11,12-2H2)-4H-1,18-(エタンジイリデン)ピリド[4,3-e]ピリミド[1,6-g][1,4,7,9]ベンゾジオキサジアザシクロドデシン-4-オン;
(5aRa,18aRa)-2-[(2S,5R)-2,5-ジメチル-4-(プロプ-2-エノイル)ピペラジン-1-イル]-12,12,18,21-テトラフルオロ-6-(プロパン-2-イル)-10,11,12,13-テトラヒドロ-4H-1,19-(エタンジイリデン)ピリド[4,3-f]ピリミド[1,6-h][1,8,10]ベンゾオキサジアザシクロトリデシン-4-オン;
(5aRa,18aRa)-2-[(2S,5R)-2,5-ジメチル-4-(プロプ-2-エノイル)ピペラジン-1-イル]-12,12,17,18,21-ペンタフルオロ-6-(プロパン-2-イル)-10,11,12,13-テトラヒドロ-4H-1,19-(エタンジイリデン)ピリド[4,3-f]ピリミド[1,6-h][1,8,10]ベンゾオキサジアザシクロトリデシン-4-オン;
(5aRa,18aRa)-2-[(2S,5R)-2,5-ジメチル-4-(プロプ-2-エノイル)ピペラジン-1-イル]-12,12,15,18,21-ペンタフルオロ-6-(プロパン-2-イル)-10,11,12,13-テトラヒドロ-4H-1,19-(エタンジイリデン)ピリド[4,3-f]ピリミド[1,6-h][1,8,10]ベンゾオキサジアザシクロトリデシン-4-オン;
(5aRa,18aRa)-2-[(2S,5R)-2,5-ジメチル-4-(プロプ-2-エノイル)ピペラジン-1-イル]-12,12,16,18,21-ペンタフルオロ-6-(プロパン-2-イル)-10,11,12,13-テトラヒドロ-4H-1,19-(エタンジイリデン)ピリド[4,3-f]ピリミド[1,6-h][1,8,10]ベンゾオキサジアザシクロトリデシン-4-オン;
(5aSa,17aRa)-20-クロロ-2-[(2S,5R)-2,5-ジメチル-4-(プロプ-2-エノイル)ピペラジン-1-イル]-16,17-ジフルオロ-6-(プロパン-2-イル)-11,12-ジ[(2H)ヒドロ](11,12-2H2)-4H-1,18-(エタンジイリデン)ピリド[4,3-e]ピリミド[1,6-g][1,4,7,9]ベンゾジオキサジアザシクロドデシン-4-オン;
2-[(2S,5R)-2,5-ジメチル-4-(プロプ-2-エノイル)ピペラジン-1-イル]-12,12,17,18,21-ペンタフルオロ-6-(プロパン-2-イル)-10,11,12,13-テトラヒドロ-4H-1,19-(エタンジイリデン)ジピリミド[4,5-f:1’,6’-h][1,8,10]ベンゾオキサジアザシクロトリデシン-4-オン;
21-クロロ-2-[(2S,5R)-2,5-ジメチル-4-(プロプ-2-エノイル)ピペラジン-1-イル]-12,12,18-トリフルオロ-6-(プロパン-2-イル)-12,13-ジヒドロ-4H,11H-1,19-(エタンジイリデン)ピリド[4,3-f]ピリミド[1,6-h][1,5,8,10]ベンゾジオキサジアザシクロトリデシン-4-オン;
20-クロロ-2-[(2S,5R)-2,5-ジメチル-4-(プロプ-2-エノイル)ピペラジン-1-イル]-17-フルオロ-6-(プロパン-2-イル)-11,12-ジヒドロ-4H,10H-1,18-(エタンジイリデン)ピリド[4,3-e]ピリミド[1,6-g][1,7,9]ベンゾオキサジアザシクロドデシン-4-オン;
からなる群から選択される化合物またはその薬学的に許容される塩。 2-[(2S,5R)-2,5-dimethyl-4-(prop-2-enoyl)piperazin-1-yl]-18,21-difluoro-6-(propan-2-yl)-10,11 , 12,13-tetrahydro-4H-1,19-ethenopyrido[4,3-f]pyrimido[1,6-h][1,8,10]benzoxadiazacyclotridecin-4-one;
(5aS a ,17aR a )-20-chloro-2-[(2S,5R)-2,5-dimethyl-4-(prop-2-enoyl)piperazin-1-yl]-14,17-difluoro-6 -(Propan-2-yl)-11,12-dihydro-4H-1,18-(ethanediylidene)pyrido[4,3-e]pyrimido[1,6-g][1,4,7,9]benzo dioxadiazacyclododecyn-4-one;
(5aS a ,17aR a )-20-chloro-2-[(2S,5R)-2,5-dimethyl-4-(prop-2-enoyl)piperazin-1-yl]-14,17-difluoro-6 -(propan-2-yl)-11,12-di[( 2 H)hydro](11,12- 2 H 2 )-4H-1,18-(ethanediylidene)pyrido[4,3-e]pyrimido[ 1,6-g][1,4,7,9]benzodioxadiazacyclododecyn-4-one;
(5aR a , 18aR a )-2-[(2S,5R)-2,5-dimethyl-4-(prop-2-enoyl)piperazin-1-yl]-12,12,18,21-tetrafluoro- 6-(propan-2-yl)-10,11,12,13-tetrahydro-4H-1,19-(ethanediylidene)pyrido[4,3-f]pyrimido[1,6-h][1,8, 10] benzoxadiazacyclotridecin-4-one;
(5aR a ,18aR a )-2-[(2S,5R)-2,5-dimethyl-4-(prop-2-enoyl)piperazin-1-yl]-12,12,17,18,21-penta fluoro-6-(propan-2-yl)-10,11,12,13-tetrahydro-4H-1,19-(ethanediylidene)pyrido[4,3-f]pyrimido[1,6-h][1, 8,10]benzoxadiazacyclotridecin-4-one;
(5aR a ,18aR a )-2-[(2S,5R)-2,5-dimethyl-4-(prop-2-enoyl)piperazin-1-yl]-12,12,15,18,21-penta fluoro-6-(propan-2-yl)-10,11,12,13-tetrahydro-4H-1,19-(ethanediylidene)pyrido[4,3-f]pyrimido[1,6-h][1, 8,10]benzoxadiazacyclotridecin-4-one;
(5aR a ,18aR a )-2-[(2S,5R)-2,5-dimethyl-4-(prop-2-enoyl)piperazin-1-yl]-12,12,16,18,21-penta fluoro-6-(propan-2-yl)-10,11,12,13-tetrahydro-4H-1,19-(ethanediylidene)pyrido[4,3-f]pyrimido[1,6-h][1, 8,10]benzoxadiazacyclotridecin-4-one;
(5aS a ,17aR a )-20-chloro-2-[(2S,5R)-2,5-dimethyl-4-(prop-2-enoyl)piperazin-1-yl]-16,17-difluoro-6 -(propan-2-yl)-11,12-di[( 2 H)hydro](11,12- 2 H 2 )-4H-1,18-(ethanediylidene)pyrido[4,3-e]pyrimido[ 1,6-g][1,4,7,9]benzodioxadiazacyclododecyn-4-one;
2-[(2S,5R)-2,5-dimethyl-4-(prop-2-enoyl)piperazin-1-yl]-12,12,17,18,21-pentafluoro-6-(propane-2 -yl)-10,11,12,13-tetrahydro-4H-1,19-(ethanediylidene)dipyrimido[4,5-f:1′,6′-h][1,8,10]benzoxadiaza Cyclotridecyn-4-one;
21-chloro-2-[(2S,5R)-2,5-dimethyl-4-(prop-2-enoyl)piperazin-1-yl]-12,12,18-trifluoro-6-(propane-2 -yl)-12,13-dihydro-4H,11H-1,19-(ethanediylidene)pyrido[4,3-f]pyrimido[1,6-h][1,5,8,10]benzodioxadia zacyclotridecin-4-one;
20-chloro-2-[(2S,5R)-2,5-dimethyl-4-(prop-2-enoyl)piperazin-1-yl]-17-fluoro-6-(propan-2-yl)-11 ,12-dihydro-4H,10H-1,18-(ethanediylidene)pyrido[4,3-e]pyrimido[1,6-g][1,7,9]benzoxadiazacyclododecyn-4-one ;
A compound selected from the group consisting of or a pharmaceutically acceptable salt thereof.
Priority Applications (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
JP2023137630A JP2023159395A (en) | 2019-10-28 | 2023-08-25 | Small molecule inhibitors of kras g12c mutant |
Applications Claiming Priority (5)
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US201962926879P | 2019-10-28 | 2019-10-28 | |
US62/926,879 | 2019-10-28 | ||
US202063030014P | 2020-05-26 | 2020-05-26 | |
US63/030,014 | 2020-05-26 | ||
PCT/US2020/057496 WO2021086833A1 (en) | 2019-10-28 | 2020-10-27 | Small molecule inhibitors of kras g12c mutant |
Related Child Applications (1)
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JP2023137630A Division JP2023159395A (en) | 2019-10-28 | 2023-08-25 | Small molecule inhibitors of kras g12c mutant |
Publications (3)
Publication Number | Publication Date |
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JP2022553994A JP2022553994A (en) | 2022-12-27 |
JPWO2021086833A5 true JPWO2021086833A5 (en) | 2023-07-19 |
JP7340100B2 JP7340100B2 (en) | 2023-09-06 |
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Family Applications (2)
Application Number | Title | Priority Date | Filing Date |
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JP2022524665A Active JP7340100B2 (en) | 2019-10-28 | 2020-10-27 | Small Molecule Inhibitor of KRAS G12C Mutant |
JP2023137630A Pending JP2023159395A (en) | 2019-10-28 | 2023-08-25 | Small molecule inhibitors of kras g12c mutant |
Family Applications After (1)
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JP2023137630A Pending JP2023159395A (en) | 2019-10-28 | 2023-08-25 | Small molecule inhibitors of kras g12c mutant |
Country Status (19)
Country | Link |
---|---|
US (3) | US11697657B2 (en) |
EP (1) | EP4051678A1 (en) |
JP (2) | JP7340100B2 (en) |
KR (1) | KR20220106980A (en) |
CN (1) | CN114867726B (en) |
AU (1) | AU2020372881A1 (en) |
BR (1) | BR112022007783A8 (en) |
CA (1) | CA3158793A1 (en) |
CO (1) | CO2022006858A2 (en) |
CR (1) | CR20220230A (en) |
DO (1) | DOP2022000090A (en) |
EC (1) | ECSP22033597A (en) |
IL (1) | IL292438A (en) |
JO (1) | JOP20220101A1 (en) |
MX (1) | MX2022005053A (en) |
PE (1) | PE20221253A1 (en) |
TW (1) | TW202130645A (en) |
WO (1) | WO2021086833A1 (en) |
ZA (1) | ZA202205938B (en) |
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