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1. 发明申请

US20150099736A1 Indolyl-Pyridone Derivatives Having Checkpoint Kinase 1 Inhibitory Activity 有权
标题翻译：具有检测点激酶1抑制活性的吲哚基 - 吡啶酮衍生物
公开(公告)号：US20150099736A1
公开(公告)日：2015-04-09
申请号：US14536764
申请日：2014-11-10
申请人： Vernalis (R&D) Ltd.
发明人： Stephen Stokes , Nicolas Foloppe , Andrea Fiumana , Martin Drysdale , Simon Bedford , Paul Webb
IPC分类号： C07D413/14 , C07D401/14
CPC分类号： C07D401/14 , A61K31/4439 , A61K31/4545 , A61K31/496 , A61K31/5377 , C07D413/14
摘要： Compounds of formula (I) have checkpoint kinase 1 (CHK1) inhibitory activity: wherein R1, R2, R5 and R6 are independently selected from hydrogen, hydroxy, methyl, trifluoromethyl, hydroxymethyl, methoxy, trifluoromethoxy, methylamino and dimethylamino; R3, and R4 are independently selected from hydrogen, hydroxy, C1-C3 alkyl, fluoro-(C1-C3)-alkyl, hydroxy-(C1-C3)-alkyl, C1-C3 alkoxy, fluoro-(C1-C3)-alkoxy, hydroxy-(C1-C3)-alkoxy, —N(R11)—R12, -Alk-N(R11)—R12, —O-Alk-N(R11)—R12, —C(═O)OH, carboxy-(C1-C3)-alkyl, or —C(═O)—NH—R13; Alk is a straight or branched chain divalent C1-C6 alkylene radical; R7 and R8 are independently selected from hydrogen, hydroxy, or C1-C3 alkoxy; X is a straight chain divalent C1-C3 alkylene radical, optionally substituted on one or more carbons by R9 and/or R10; W is selected from —C(═O)—N(—R16)— or —N(—R17)—C(═O)—; Y is hydrogen, C1-C3 alkyl, C1-C3 alkoxy, or halo; and Q is selected from optionally substituted phenyl, optionally substituted cyclohexyl, or an optionally substituted 6-membered monocyclic heteroaryl ring.
摘要翻译：式（I）化合物具有检测点激酶1（CHK1）抑制活性：其中R1，R2，R5和R6独立地选自氢，羟基，甲基，三氟甲基，羟甲基，甲氧基，三氟甲氧基，甲基氨基和二甲基氨基; R 3和R 4独立地选自氢，羟基，C 1 -C 3烷基，氟 - （C 1 -C 3） - 烷基，羟基 - （C 1 -C 3） - 烷基，C 1 -C 3烷氧基，氟 - （C 1 -C 3）烷氧基，羟基 - （C1-C3） - 烷氧基，-N（R11）-R12，-Alk-N（R11）-R12，-O-Alk-N（R11）-R12，-C（= 羧基 - （C 1 -C 3） - 烷基或-C（= O）-NH-R 13; Alk是直链或支链二价C1-C6亚烷基; R 7和R 8独立地选自氢，羟基或C 1 -C 3烷氧基; X是直链的二价C1-C3亚烷基，任选地被一个或多个碳上被R9和/或R10取代; W选自-C（= O）-N（-R 16） - 或-N（-R 17）-C（= O） - ; Y是氢，C 1 -C 3烷基，C 1 -C 3烷氧基或卤素; 并且Q选自任选取代的苯基，任选取代的环己基或任选取代的6元单环杂芳基环。

2. 发明申请

US20180244652A1 Indolyl-Pyridone Derivatives Having Checkpoint Kinase 1 Inhibitory Activity 审中-公开
公开(公告)号：US20180244652A1
公开(公告)日：2018-08-30
申请号：US15962306
申请日：2018-04-25
申请人： Vernalis (R&D) Ltd.
发明人： Stephen Stokes , Nicolas Foloppe , Andrea Fiumana , Martin Drysdale , Simon Bedford , Paul Webb
IPC分类号： C07D401/14 , C07D413/14 , A61K31/5377 , A61K31/496 , A61K31/4439 , A61K31/4545
摘要： A method of treating a mammal suffering from a cancer responsive to inhibition of protein kinase activity, by administering to the mammal an amount of a compound of formula (I), or a pharmaceutically acceptable salt thereof, effective to inhibit protein kinase activity, wherein the compound of formula (I) is:

3. 发明申请

US20170298043A1 Indolyl-Pyridone Derivatives Having Checkpoint Kinase 1 Inhibitory Activity 审中-公开
公开(公告)号：US20170298043A1
公开(公告)日：2017-10-19
申请号：US15427457
申请日：2017-02-08
申请人： Vernalis (R&D) Ltd.
发明人： Stephen Stokes , Nicolas Foloppe , Andrea Fiumana , Martin Drysdale , Simon Bedford , Paul Webb
IPC分类号： C07D401/14 , A61K31/496 , A61K31/4439 , A61K31/4545 , C07D413/14 , A61K31/5377
CPC分类号： C07D401/14 , A61K31/4439 , A61K31/4545 , A61K31/496 , A61K31/5377 , C07D413/14
摘要： Compounds of formula (I) have checkpoint kinase 1 (CHK1) inhibitory activity: wherein R1, R2, R5 and R6 are independently selected from hydrogen, hydroxy, methyl, trifluoromethyl, hydroxymethyl, methoxy, trifluoromethoxy, methylamino and dimethylamino; R3, and R4 are independently selected from hydrogen, hydroxy, C1-C3 alkyl, fluoro-(C1-C3)-alkyl, hydroxy-(C1-C3)-alkyl, C1-C3 alkoxy, fluoro-(C1-C3)-alkoxy, hydroxy-(C1-C3)-alkoxy, —N(R11)—R12, -Alk-N(R11)—R12, —O-Alk-N(R11)—R12, —C(═O)OH, carboxy-(C1-C3)-alkyl, or —C(═O)—NH—R13; Alk is a straight or branched chain divalent C1-C6 alkylene radical; R7 and R8 are independently selected from hydrogen, hydroxy, or C1-C3 alkoxy; X is a straight chain divalent C1-C3 alkylene radical, optionally substituted on one or more carbons by R9 and/or R10; W is selected from —C(═O)—N(—R16)— or —N(—R17)—C(═O)—; Y is hydrogen, C1-C3 alkyl, C1-C3 alkoxy, or halo; and Q is selected from optionally substituted phenyl, optionally substituted cyclohexyl, or an optionally substituted 6-membered monocyclic heteroaryl ring.

4. 发明授权

US10696652B2 Indolyl-pyridone derivatives having checkpoint kinase 1 inhibitory activity 有权
公开(公告)号：US10696652B2
公开(公告)日：2020-06-30
申请号：US15962306
申请日：2018-04-25
申请人： Vernalis (R&D) Ltd.
发明人： Stephen Stokes , Nicolas Foloppe , Andrea Fiumana , Martin Drysdale , Simon Bedford , Paul Webb
IPC分类号： C07D401/14 , C07D413/14 , A61K31/4439 , A61K31/4545 , A61K31/496 , A61K31/5377
摘要： A method of treating a mammal suffering from a cancer responsive to inhibition of protein kinase activity, by administering to the mammal an amount of a compound of formula (I), or a pharmaceutically acceptable salt thereof, effective to inhibit protein kinase activity, wherein the compound of formula (I) is:

5. 发明授权

US09604975B2 Indolyl-pyridone derivatives having checkpoint kinase 1 inhibitory activity 有权
公开(公告)号：US09604975B2
公开(公告)日：2017-03-28
申请号：US14536764
申请日：2014-11-10
申请人： Vernalis (R&D) Ltd.
发明人： Stephen Stokes , Nicolas Foloppe , Andrea Fiumana , Martin Drysdale , Simon Bedford , Paul Webb
IPC分类号： A61K31/4439 , C07D413/14 , C07D401/14
CPC分类号： C07D401/14 , A61K31/4439 , A61K31/4545 , A61K31/496 , A61K31/5377 , C07D413/14
摘要： Compounds of formula (I) have checkpoint kinase 1 (CHK1) inhibitory activity: wherein R1, R2, R5 and R6 are independently selected from hydrogen, hydroxy, methyl, trifluoromethyl, hydroxymethyl, methoxy, trifluoromethoxy, methylamino and dimethylamino; R3, and R4 are independently selected from hydrogen, hydroxy, C1-C3 alkyl, fluoro-(C1-C3)-alkyl, hydroxy-(C1-C3)-alkyl, C1-C3 alkoxy, fluoro-(C1-C3)-alkoxy, hydroxy-(C1-C3)-alkoxy, —N(R11)—R12, -Alk-N(R11)—R12, —O-Alk-N(R11)—R12, —C(═O)OH, carboxy-(C1-C3)-alkyl, or —C(═O)—NH—R13; Alk is a straight or branched chain divalent C1-C6 alkylene radical; R7 and R8 are independently selected from hydrogen, hydroxy, or C1-C3 alkoxy; X is a straight chain divalent C1-C3 alkylene radical, optionally substituted on one or more carbons by R9 and/or R10; W is selected from —C(═O)—N(—R16)— or —N(—R17)—C(═O)—; Y is hydrogen, C1-C3 alkyl, C1-C3 alkoxy, or halo; and Q is selected from optionally substituted phenyl, optionally substituted cyclohexyl, or an optionally substituted 6-membered monocyclic heteroaryl ring.

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