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公开(公告)号：US20120244149A1
公开(公告)日：2012-09-27
申请号：US13477587
申请日：2012-05-22
申请人： Nicole Blaquiere , Steven Do , Danette Dudley , Adrian Folkes , Robert Heald , Timothy Heffron , Mark Jones , Aleksandr Kolesnikov , Chudi Ndubaku , Alan G. Olivero , Stephen Price , Steven Staben , Lan Wang
发明人： Nicole Blaquiere , Steven Do , Danette Dudley , Adrian Folkes , Robert Heald , Timothy Heffron , Mark Jones , Aleksandr Kolesnikov , Chudi Ndubaku , Alan G. Olivero , Stephen Price , Steven Staben , Lan Wang
IPC分类号： A61K31/553 , A61K31/565 , A61P35/00 , A61P29/00 , A61P37/02 , A61P37/04 , A61P9/00 , A61P31/12 , A61P7/00 , A61P3/10 , A61P1/16 , A61K39/395 , A61P25/00
CPC分类号： C07D498/04 , A61K31/553 , A61K45/06 , C07D491/044 , C07D498/14 , C07D519/00
摘要： Benzoxazepin compounds of Formula I, including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, wherein: Z1 is CR1 or N; Z2 is CR2 or N; Z3 is CR3 or N; Z4 is CR4 or N; and B is a pyrazolyl, imidazolyl, or triazolyl ring fused to the benzoxepin ring, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
摘要翻译： 式I的苯并氧氮杂化合物，包括立体异构体，几何异构体，互变异构体，溶剂合物，代谢物及其药学上可接受的盐，其中：Z1是CR1或N; Z2为CR2或N; Z3为CR3或N; Z4是CR4或N; B是与苯并氧杂环环稠合的吡唑基，咪唑基或三唑基环，可用于抑制脂质激酶，包括p110α和PI3K的其他同种型，并用于治疗由脂质激酶介导的癌症等疾病。 公开了使用式I化合物在体外，原位和体内诊断，预防或治疗哺乳动物细胞或相关病理状况中的这种病症的方法。
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公开(公告)号：US08263633B2
公开(公告)日：2012-09-11
申请号：US12890810
申请日：2010-09-27
申请人： Nicole Blaquiere , Steven Do , Danette Dudley , Adrian Folkes , Richard Goldsmith , Robert Heald , Timothy Heffron , Aleksandr Kolesnikov , Chudi Ndubaku , Alan G. Olivero , Stephen Price , Steven Staben , BinQing Wei
发明人： Nicole Blaquiere , Steven Do , Danette Dudley , Adrian Folkes , Richard Goldsmith , Robert Heald , Timothy Heffron , Aleksandr Kolesnikov , Chudi Ndubaku , Alan G. Olivero , Stephen Price , Steven Staben , BinQing Wei
IPC分类号： A61K31/41 , C07D249/14
CPC分类号： C07D495/04 , A61K31/381 , A61K31/41 , A61K31/4196 , A61K31/4245 , A61K31/429 , A61K31/4365 , A61K31/4439 , A61K31/454 , A61K31/4545 , A61K31/496 , A61K31/4985 , A61K31/506 , A61K31/5377 , A61K31/541 , A61K31/551 , A61K45/06 , C07D249/14 , C07D495/14 , C07D513/04 , C07D513/14
摘要： Benzoxepin compounds of Formula I, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, wherein: Z1 is CR1 or N; Z2 is CR2 or N; Z3 is CR3 or N; Z4 is CR4 or N; and where (i) X1 is N and X2 is S, (ii) X1 is S and X2 is N, (iii) X1 is CR7 and X2 is S, (iv) X1 is S and X2 is CR7; (v) X1 is NR8 and X2 is N, (vi) X1 is N and X2 is NR8, (vii) X1 is CR7 and X2 is O, (viii) X1 is O and X2 is CR7, (ix) X1 is CR7 and X2 is C(R7)2, (x) X1 is C(R7)2 and X2 is CR7; (xi) X1 is N and X2 is O, or (xii) X1 is O and X2 is N, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
摘要翻译： 式I的苯并氧杂环己烯化合物，包括立体异构体，几何异构体，互变异构体，溶剂合物，代谢物及其药学上可接受的盐，其中：Z1是CR1或N; Z2为CR2或N; Z3为CR3或N; Z4是CR4或N; 并且其中（i）X1为N且X2为S，（ii）X1为S且X2为N，（iii）X1为CR7，X2为S，（iv）X1为S且X2为CR7; （ⅴ）X1为NR8，X2为N，（vi）X1为N，X2为NR8，i X1为CR7，X2为O，（ii）X1为O，X2为CR7，ix为CR7 X2为C（R7）2，（x）X1为C（R7）2，X2为CR7; （xi）X1是N，X2是O，或（xii）X1是O，X2是N，可用于抑制脂质激酶，包括p110α和PI3K的其他同种型，并用于治疗由脂质激酶介导的癌症等疾病。 公开了使用式I化合物在体外，原位和体内诊断，预防或治疗哺乳动物细胞或相关病理状况中的这种病症的方法。
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公开(公告)号：US08343955B2
公开(公告)日：2013-01-01
申请号：US13477587
申请日：2012-05-22
申请人： Nicole Blaquiere , Steven Do , Danette Dudley , Adrian Folkes , Robert Heald , Timothy Heffron , Mark Jones , Aleksandr Kolesnikov , Chudi Ndubaku , Alan G. Olivero , Stephen Price , Steven Staben , Lan Wang
发明人： Nicole Blaquiere , Steven Do , Danette Dudley , Adrian Folkes , Robert Heald , Timothy Heffron , Mark Jones , Aleksandr Kolesnikov , Chudi Ndubaku , Alan G. Olivero , Stephen Price , Steven Staben , Lan Wang
IPC分类号： A61K31/553
CPC分类号： C07D498/04 , A61K31/553 , A61K45/06 , C07D491/044 , C07D498/14 , C07D519/00
摘要： Benzoxazepin compounds of Formula I, including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, wherein: Z1 is CR1 or N; Z2 is CR2 or N; Z3 is CR3 or N; Z4 is CR4 or N; and B is a pyrazolyl, imidazolyl, or triazolyl ring fused to the benzoxepin ring, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
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公开(公告)号：US20110076292A1
公开(公告)日：2011-03-31
申请号：US12890812
申请日：2010-09-27
申请人： Nicole Blaquiere , Steven Do , Danette Dudley , Adrian Folkes , Robert Heald , Timothy Heffron , Mark Jones , Aleksandr Kolesnikov , Chudi Ndubaku , Alan G. Olivero , Stephen Price , Steven Staben , Lan Wang
发明人： Nicole Blaquiere , Steven Do , Danette Dudley , Adrian Folkes , Robert Heald , Timothy Heffron , Mark Jones , Aleksandr Kolesnikov , Chudi Ndubaku , Alan G. Olivero , Stephen Price , Steven Staben , Lan Wang
IPC分类号： A61K31/553 , C07D498/04 , C07D491/044 , C07D498/14 , A61K31/4196 , A61K31/496 , A61K31/454 , A61K39/00 , A61P35/00 , A61P35/02 , A61P29/00 , A61P9/00 , A61P1/16 , A61P31/12 , A61P7/00 , A61P3/10
CPC分类号： C07D498/04 , A61K31/553 , A61K45/06 , C07D491/044 , C07D498/14 , C07D519/00
摘要： Benzoxazepin compounds of Formula I, including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, wherein: Z1 is CR1 or N; Z2 is CR2 or N; Z3 is CR3 or N; Z4 is CR4 or N; and B is a pyrazolyl, imidazolyl, or triazolyl ring fused to the benzoxepin ring, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
摘要翻译： 式I的苯并氧氮杂化合物，包括立体异构体，几何异构体，互变异构体，溶剂合物，代谢物及其药学上可接受的盐，其中：Z1是CR1或N; Z2为CR2或N; Z3为CR3或N; Z4是CR4或N; B是与苯并氧杂环环稠合的吡唑基，咪唑基或三唑基环，可用于抑制脂质激酶，包括p110α和PI3K的其他同种型，并用于治疗由脂质激酶介导的癌症等疾病。 公开了使用式I化合物在体外，原位和体内诊断，预防或治疗哺乳动物细胞或相关病理状况中的这种病症的方法。
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公开(公告)号：US08242104B2
公开(公告)日：2012-08-14
申请号：US12890812
申请日：2010-09-27
申请人： Nicole Blaquiere , Steven Do , Danette Dudley , Adrian Folkes , Robert Heald , Timothy Heffron , Mark Jones , Aleksandr Kolesnikov , Chudi Ndubaku , Alan G. Olivero , Stephen Price , Steven Staben , Lan Wang
发明人： Nicole Blaquiere , Steven Do , Danette Dudley , Adrian Folkes , Robert Heald , Timothy Heffron , Mark Jones , Aleksandr Kolesnikov , Chudi Ndubaku , Alan G. Olivero , Stephen Price , Steven Staben , Lan Wang
IPC分类号： A61K31/553 , C07D498/04 , C07D498/14
CPC分类号： C07D498/04 , A61K31/553 , A61K45/06 , C07D491/044 , C07D498/14 , C07D519/00
摘要： Benzoxazepin compounds of Formula I, including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, wherein: Z1 is CR1 or N; Z2 is CR2 or N; Z3 is CR3 or N; Z4 is CR4 or N; and B is a pyrazolyl, imidazolyl, or triazolyl ring fused to the benzoxepin ring, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
摘要翻译： 式I的苯并氧氮杂化合物，包括立体异构体，几何异构体，互变异构体，溶剂合物，代谢物及其药学上可接受的盐，其中：Z1是CR1或N; Z2为CR2或N; Z3为CR3或N; Z4是CR4或N; B是与苯并氧杂环环稠合的吡唑基，咪唑基或三唑基环，可用于抑制脂质激酶，包括p110α和PI3K的其他同种型，并用于治疗由脂质激酶介导的癌症等疾病。 公开了使用式I化合物在体外，原位和体内诊断，预防或治疗哺乳动物细胞或相关病理状况中的这种病症的方法。
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公开(公告)号：US08673952B2
公开(公告)日：2014-03-18
申请号：US13568707
申请日：2012-08-07
申请人： Nicole Blaquiere , Steven Do , Danette Dudley , Adrian Folkes , Richard Goldsmith , Robert Heald , Timothy Heffron , Aleksandr Kolesnikov , Chudi Ndubaku , Alan G. Olivero , Stephen Price , Steven Staben , BinQing Wei
发明人： Nicole Blaquiere , Steven Do , Danette Dudley , Adrian Folkes , Richard Goldsmith , Robert Heald , Timothy Heffron , Aleksandr Kolesnikov , Chudi Ndubaku , Alan G. Olivero , Stephen Price , Steven Staben , BinQing Wei
IPC分类号： A61K31/41 , C07D249/14
CPC分类号： C07D495/04 , A61K31/381 , A61K31/41 , A61K31/4196 , A61K31/4245 , A61K31/429 , A61K31/4365 , A61K31/4439 , A61K31/454 , A61K31/4545 , A61K31/496 , A61K31/4985 , A61K31/506 , A61K31/5377 , A61K31/541 , A61K31/551 , A61K45/06 , C07D249/14 , C07D495/14 , C07D513/04 , C07D513/14
摘要： Benzoxepin compounds of Formula I, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
摘要翻译： 式I的苯并氧杂多磷化合物，包括立体异构体，几何异构体，互变异构体，溶剂合物，代谢产物及其药学上可接受的盐可用于抑制脂质激酶，包括p110α和PI3K的其他同种型，并用于治疗诸如由脂质激酶介导的癌症 。 公开了使用式I化合物在体外，原位和体内诊断，预防或治疗哺乳动物细胞或相关病理状况中的这种病症的方法。
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公开(公告)号：US20130012488A1
公开(公告)日：2013-01-10
申请号：US13568707
申请日：2012-08-07
申请人： Nicole Blaquiere , Steven Do , Danette Dudley , Adrian Folkes , Richard Goldsmith , Robert Heald , Timothy Heffron , Aleksandr Kolesnikov , Chudi Ndubaku , Alan G. Olivero , Stephen Price , Steven Staben , BinQing Wei
发明人： Nicole Blaquiere , Steven Do , Danette Dudley , Adrian Folkes , Richard Goldsmith , Robert Heald , Timothy Heffron , Aleksandr Kolesnikov , Chudi Ndubaku , Alan G. Olivero , Stephen Price , Steven Staben , BinQing Wei
IPC分类号： A61K31/429 , C07D495/04 , A61P35/00 , C07D495/14 , A61K31/4365 , A61K31/5377 , C07D513/04 , A61K31/381
CPC分类号： C07D495/04 , A61K31/381 , A61K31/41 , A61K31/4196 , A61K31/4245 , A61K31/429 , A61K31/4365 , A61K31/4439 , A61K31/454 , A61K31/4545 , A61K31/496 , A61K31/4985 , A61K31/506 , A61K31/5377 , A61K31/541 , A61K31/551 , A61K45/06 , C07D249/14 , C07D495/14 , C07D513/04 , C07D513/14
摘要： Benzoxepin compounds of Formula I, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
摘要翻译： 式I的苯并氧杂多磷化合物，包括立体异构体，几何异构体，互变异构体，溶剂合物，代谢产物及其药学上可接受的盐可用于抑制脂质激酶，包括p110α和PI3K的其他同种型，并用于治疗诸如由脂质激酶介导的癌症 。 公开了使用式I化合物在体外，原位和体内诊断，预防或治疗哺乳动物细胞或相关病理状况中的这种病症的方法。
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公开(公告)号：US20110076291A1
公开(公告)日：2011-03-31
申请号：US12890810
申请日：2010-09-27
申请人： Nicole Blaquiere , Steven Do , Danette Dudley , Adrian Folkes , Richard Goldsmith , Robert Heald , Timothy Heffron , Aleksandr Kolesnikov , Chudi Ndubaku , Alan G. Olivero , Stephen Price , Steven Staben , BinQing Wei
发明人： Nicole Blaquiere , Steven Do , Danette Dudley , Adrian Folkes , Richard Goldsmith , Robert Heald , Timothy Heffron , Aleksandr Kolesnikov , Chudi Ndubaku , Alan G. Olivero , Stephen Price , Steven Staben , BinQing Wei
IPC分类号： A61K31/429 , C07D513/04 , C07D495/04 , C07D495/14 , A61K31/381 , A61K31/4365 , A61K31/4245 , A61K31/454 , A61K31/4439 , A61K31/5377 , A61K31/496 , A61K39/00 , A61P35/00 , A61P35/02 , A61P29/00 , A61P9/00 , A61P3/10 , A61P31/12 , A61P7/00 , A61P1/16
CPC分类号： C07D495/04 , A61K31/381 , A61K31/41 , A61K31/4196 , A61K31/4245 , A61K31/429 , A61K31/4365 , A61K31/4439 , A61K31/454 , A61K31/4545 , A61K31/496 , A61K31/4985 , A61K31/506 , A61K31/5377 , A61K31/541 , A61K31/551 , A61K45/06 , C07D249/14 , C07D495/14 , C07D513/04 , C07D513/14
摘要： Benzoxepin compounds of Formula I, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, wherein: Z1 is CR1 or N; Z2 is CR2 or N; Z3 is CR3 or N; Z4 is CR4 or N; and where (i) X1 is N and X2 is S, (ii) X1 is S and X2 is N, (iii) X1 is CR7 and X2 is S, (iv) X1 is S and X2 is CR7; (v) X1 is NR8 and X2 is N, (vi) X1 is N and X2 is NR8, (vii) X1 is CR7 and X2 is O, (viii) X1 is O and X2 is CR7, (ix) X1 is CR7 and X2 is C(R7)2, (x) X1 is C(R7)2 and X2 is CR7; (xi) X1 is N and X2 is O, or (xii) X1 is O and X2 is N, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
摘要翻译： 式I的苯并氧杂环己烯化合物，包括立体异构体，几何异构体，互变异构体，溶剂合物，代谢物及其药学上可接受的盐，其中：Z1是CR1或N; Z2为CR2或N; Z3为CR3或N; Z4是CR4或N; 并且其中（i）X1为N且X2为S，（ii）X1为S且X2为N，（iii）X1为CR7，X2为S，（iv）X1为S且X2为CR7; （ⅴ）X1为NR8，X2为N，（vi）X1为N，X2为NR8，i X1为CR7，X2为O，（ii）X1为O，X2为CR7，ix为CR7 X2为C（R7）2，（x）X1为C（R7）2，X2为CR7; （xi）X1是N，X2是O，或（xii）X1是O，X2是N，可用于抑制脂质激酶包括p110α和PI3K的其他同种型，并用于治疗由脂质激酶介导的癌症等疾病。 公开了使用式I化合物在体外，原位和体内诊断，预防或治疗哺乳动物细胞或相关病理状况中的这种病症的方法。
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