公开(公告)号：US20120202785A1

公开(公告)日：2012-08-09

申请号：US13369016

申请日：2012-02-08

申请人： Robert Heald ,  Stephen Price ,  Brian Safina ,  Pascal Pierre Alexandre Savy ,  Eileen Mary Seward ,  Daniel P. Sutherlin ,  Bohdan Waszkowycz

发明人： Robert Heald ,  Stephen Price ,  Brian Safina ,  Pascal Pierre Alexandre Savy ,  Eileen Mary Seward ,  Daniel P. Sutherlin ,  Bohdan Waszkowycz

IPC分类号： A61K31/52 ,  C07D519/00 ,  C07D487/04 ,  C07D495/04 ,  C07D403/12 ,  C07D498/06 ,  A61K31/519 ,  A61K31/5377 ,  A61P35/00 ,  A61P37/00 ,  A61P9/00 ,  A61P31/12 ,  A61P29/00 ,  A61P3/00 ,  A61P5/00 ,  A61P25/00 ,  A61P19/02 ,  A61P37/08 ,  A61P1/04 ,  A61P11/06 ,  A61P17/06 ,  A61P35/02 ,  C07D473/34

CPC分类号： C07D473/34 ,  A61K31/519 ,  A61K31/52 ,  A61K31/5377 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  C07D471/04 ,  C07D473/16 ,  C07D473/32 ,  C07D473/40 ,  C07D487/04 ,  C07D495/04 ,  C07D498/06 ,  C07D513/04 ,  C07D519/00

摘要： Formula I compounds, including stereoisomers, geometric isomers, tautomers, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting the delta isoform of PI3K, and for treating disorders mediated by lipid kinases such as inflammation, immunological disorders, and cancer. 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化合物，包括立体异构体，几何异构体，互变异构体，代谢物及其药学上可接受的盐，可用于抑制PI3K的δ同种型，以及用于治疗由脂质激酶如炎症，免疫学障碍和癌症介导的病症。 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。

公开(公告)号：US08653089B2

公开(公告)日：2014-02-18

申请号：US13369016

申请日：2012-02-08

申请人： Robert Heald ,  Stephen Price ,  Brian Safina ,  Pascal Pierre Alexandre Savy ,  Eileen Mary Seward ,  Daniel P. Sutherlin ,  Bohdan Waszkowycz

发明人： Robert Heald ,  Stephen Price ,  Brian Safina ,  Pascal Pierre Alexandre Savy ,  Eileen Mary Seward ,  Daniel P. Sutherlin ,  Bohdan Waszkowycz

IPC分类号： A61K31/52 ,  C07D473/00

CPC分类号： C07D473/34 ,  A61K31/519 ,  A61K31/52 ,  A61K31/5377 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  C07D471/04 ,  C07D473/16 ,  C07D473/32 ,  C07D473/40 ,  C07D487/04 ,  C07D495/04 ,  C07D498/06 ,  C07D513/04 ,  C07D519/00

摘要： Formula I compounds, including stereoisomers, geometric isomers, tautomers, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting the delta isoform of PI3K, and for treating disorders mediated by lipid kinases such as inflammation, immunological disorders, and cancer. 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化合物，包括立体异构体，几何异构体，互变异构体，代谢物及其药学上可接受的盐，可用于抑制PI3K的δ同种型，以及用于治疗由脂质激酶如炎症，免疫学障碍和癌症介导的病症。 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。

公开(公告)号：US09090628B2

公开(公告)日：2015-07-28

申请号：US13424500

申请日：2012-03-20

申请人： Timothy Heffron ,  Brian Safina ,  Steven Staben ,  Daniel P. Sutherlin ,  BinQing Wei ,  Richard Elliott ,  Robert Heald ,  Eileen M. Seward ,  Emanuela Gancia ,  Bohdan Waszkowycz

发明人： Timothy Heffron ,  Brian Safina ,  Steven Staben ,  Daniel P. Sutherlin ,  BinQing Wei ,  Richard Elliott ,  Robert Heald ,  Eileen M. Seward ,  Emanuela Gancia ,  Bohdan Waszkowycz

IPC分类号： A61K31/553 ,  C07D498/04 ,  C07D498/14 ,  C07D519/00

CPC分类号： C07D498/14 ,  C07D498/04 ,  C07D519/00

摘要： Benzoxazepin Formula I compounds, including stereoisomers, geometric isomers, tautomers, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting the delta isoform of PI3K, and for treating disorders mediated by lipid kinases such as inflammation, immunological disorders, and cancer. 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： 苯并西泮配方I化合物，包括立体异构体，几何异构体，互变异构体，代谢物及其药学上可接受的盐，可用于抑制PI3K的δ同种型，以及用于治疗脂质激酶如炎症，免疫学障碍和癌症介导的病症。 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。

公开(公告)号：US20100280063A1

公开(公告)日：2010-11-04

申请号：US12808346

申请日：2008-12-18

申请人： Stephen Price ,  Robert Heald ,  Pascal Pierre Alexandre Savy

发明人： Stephen Price ,  Robert Heald ,  Pascal Pierre Alexandre Savy

IPC分类号： A61K31/437 ,  C07D471/04 ,  A61P35/00

CPC分类号： C07D471/04 ,  C07D487/04

摘要： The invention relates to imidazopyridines of formula I with anti-cancer and/or anti-inflammatory activity and more specifically to imidazopyridines which inhibit MEK kinase activity. The invention provides compositions and methods useful for inhibiting abnormal cell growth or treating a hyperproliferative disorder, or treating an inflammatory disease in a mammal. The invention also relates to methods of using the compounds for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.

摘要翻译： 本发明涉及式I的咪唑并吡啶与抗癌和/或抗炎活性，更具体地涉及抑制MEK激酶活性的咪唑并吡啶类。 本发明提供了可用于抑制异常细胞生长或治疗过度增殖性疾病或治疗哺乳动物炎性疾病的组合物和方法。 本发明还涉及将化合物用于体外，原位和体内诊断或治疗哺乳动物细胞或相关病理状况的方法。

公开(公告)号：US08293763B2

公开(公告)日：2012-10-23

申请号：US12808346

申请日：2008-12-18

申请人： Stephen Price ,  Robert Heald ,  Pascal Pierre Alexandre Savy

发明人： Stephen Price ,  Robert Heald ,  Pascal Pierre Alexandre Savy

IPC分类号： A61K31/437 ,  C07D471/04 ,  A61P35/00

CPC分类号： C07D471/04 ,  C07D487/04

摘要： The invention relates to imidazopyridines of formula I with anti-cancer and/or anti-inflammatory activity and more specifically to imidazopyridines which inhibit MEK kinase activity. The invention provides compositions and methods useful for inhibiting abnormal cell growth or treating a hyperproliferative disorder, or treating an inflammatory disease in a mammal. The invention also relates to methods of using the compounds for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.(Formula I)

摘要翻译： 本发明涉及式I的咪唑并吡啶与抗癌和/或抗炎活性，更具体地涉及抑制MEK激酶活性的咪唑并吡啶类。 本发明提供了可用于抑制异常细胞生长或治疗过度增殖性疾病或治疗哺乳动物炎性疾病的组合物和方法。 本发明还涉及将化合物用于体外，原位和体内诊断或治疗哺乳动物细胞或相关病理状况的方法（式I）

公开(公告)号：US20120245144A1

公开(公告)日：2012-09-27

申请号：US13424500

申请日：2012-03-20

申请人： Timothy Heffron ,  Brian Safina ,  Steven Staben ,  Daniel P. Sutherlin ,  BinQing Wei ,  Richard Elliott ,  Robert Heald ,  Eileen M. Seward ,  Emanuela Gancia ,  Bohdan Waskowycz

发明人： Timothy Heffron ,  Brian Safina ,  Steven Staben ,  Daniel P. Sutherlin ,  BinQing Wei ,  Richard Elliott ,  Robert Heald ,  Eileen M. Seward ,  Emanuela Gancia ,  Bohdan Waskowycz

IPC分类号： A61K31/553 ,  C07D498/04 ,  A61P35/00 ,  A61P37/00 ,  A61P9/00 ,  A61P31/12 ,  A61P29/00 ,  A61P3/00 ,  A61P5/00 ,  A61P25/00 ,  A61P19/02 ,  A61P37/06 ,  A61P37/08 ,  A61P1/04 ,  A61P1/00 ,  A61P17/00 ,  A61P11/06 ,  A61P43/00 ,  A61P7/00 ,  A61P11/00 ,  A61P17/06 ,  A61P35/02 ,  C07D498/14

CPC分类号： C07D498/14 ,  C07D498/04 ,  C07D519/00

摘要： Benzoxazepin Formula I compounds, including stereoisomers, geometric isomers, tautomers, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting the delta isoform of PI3K, and for treating disorders mediated by lipid kinases such as inflammation, immunological disorders, and cancer. 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： 苯并西泮配方I化合物，包括立体异构体，几何异构体，互变异构体，代谢物及其药学上可接受的盐，可用于抑制PI3K的δ同种型，以及用于治疗脂质激酶如炎症，免疫学障碍和癌症介导的病症。 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。

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。

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。

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.

公开(公告)号：US07923456B2

公开(公告)日：2011-04-12

申请号：US12432529

申请日：2009-04-29

申请人： Stephen Price ,  Robert Heald ,  Wendy Lee ,  Mark E. Zak ,  Joanne Frances Mary Hewitt

发明人： Stephen Price ,  Robert Heald ,  Wendy Lee ,  Mark E. Zak ,  Joanne Frances Mary Hewitt

IPC分类号： A61K31/44

CPC分类号： C07D471/04 ,  C07D235/00 ,  C07D401/04 ,  C07D487/04

摘要： The invention relates to imidazopyridines of formula I with anti-cancer and/or anti-inflammatory activity and more specifically to imidazopyridines which inhibit MEK kinase activity. The invention provides compositions and methods useful for inhibiting abnormal cell growth or treating a hyperproliferative disorder, or treating an inflammatory disease in a mammal. The invention also relates to methods of using the compounds for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.

摘要翻译： 本发明涉及式I的咪唑并吡啶与抗癌和/或抗炎活性，更具体地涉及抑制MEK激酶活性的咪唑并吡啶类。 本发明提供了可用于抑制异常细胞生长或治疗过度增殖性疾病或治疗哺乳动物炎性疾病的组合物和方法。 本发明还涉及将化合物用于体外，原位和体内诊断或治疗哺乳动物细胞或相关病理状况的方法。