公开(公告)号：US08173650B2

公开(公告)日：2012-05-08

申请号：US12787613

申请日：2010-05-26

Applicant: Georgette Castanedo ,  Bryan Chan ,  David Goldstein ,  Rama Kondru ,  Matthew Lucas ,  Wylie Palmer ,  Stephen Price ,  Brian Safina ,  Pascal Pierre Alexandre Savy ,  Eileen Mary Seward ,  Daniel P. Sutherlin ,  Zachary K. Sweeney

Inventor： Georgette Castanedo ,  Bryan Chan ,  David Goldstein ,  Rama Kondru ,  Matthew Lucas ,  Wylie Palmer ,  Stephen Price ,  Brian Safina ,  Pascal Pierre Alexandre Savy ,  Eileen Mary Seward ,  Daniel P. Sutherlin ,  Zachary K. Sweeney

IPC: A61K31/535 ,  C07D413/14

CPC classification number: C07D513/04 ,  C07D487/04 ,  C07D491/04 ,  C07D495/04

Abstract: Formula I (Ia and Ib) compounds wherein (i) X1 is N and X2 is S, (ii) X1 is CR7 and X2 is S, (iii) X1 is N and X2 is NR2, or (iv) X1 is CR7 and X2 is O, including stereoisomers, 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, 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.

Abstract translation: 式（I）和（Ib）化合物，其中（i）X1为N，X 2为S，（ii）X1为CR7，X2为S，（iii）X1为N，X2为NR2，或（iv）X1为CR7， X 2为O，包括立体异构体，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：US08841462B2

公开(公告)日：2014-09-23

申请号：US12999003

申请日：2009-07-01

Applicant: Robert A. Heald ,  Philip Jackson ,  Joseph P. Lyssikatos ,  Stephen Price ,  Pascal Pierre Alexandre Savy

Inventor： Robert A. Heald ,  Philip Jackson ,  Joseph P. Lyssikatos ,  Stephen Price ,  Pascal Pierre Alexandre Savy

IPC: C07D275/04 ,  C07D231/56 ,  C07D513/04 ,  C07D471/04 ,  A61K31/437 ,  A61K31/428 ,  A61K31/416

CPC classification number: C07D231/56 ,  C07D275/04 ,  C07D403/12 ,  C07D405/12 ,  C07D471/04

Abstract: The invention relates to bicyclic heterocycles of formulae I and II with anti-cancer and/or anti-inflammatory activity and more specifically with MEK kinase inhibitory activity. The invention provides compositions and methods useful for inhibiting abnormal cell growth, 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.

Abstract translation: 本发明涉及式I和II的双环杂环，其具有抗癌和/或抗炎活性，更具体地涉及MEK激酶抑制活性。 本发明提供了可用于抑制异常细胞生长，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：US20100280063A1

公开(公告)日：2010-11-04

申请号：US12808346

申请日：2008-12-18

Applicant: Stephen Price ,  Robert Heald ,  Pascal Pierre Alexandre Savy

Inventor： Stephen Price ,  Robert Heald ,  Pascal Pierre Alexandre Savy

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

CPC classification number: C07D471/04 ,  C07D487/04

Abstract: 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.

Abstract translation: 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：US08653089B2

公开(公告)日：2014-02-18

申请号：US13369016

申请日：2012-02-08

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

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

IPC: A61K31/52 ,  C07D473/00

CPC classification number: 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

Abstract: 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.

Abstract translation: 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：US08394796B2

公开(公告)日：2013-03-12

申请号：US13427081

申请日：2012-03-22

Applicant: Georgette Castanedo ,  Bryan Chan ,  David Goldstein ,  Rama Kondru ,  Matthew Lucas ,  Wylie Palmer ,  Stephen Price ,  Brian Safina ,  Pascal Pierre Alexandre Savy ,  Eileen Mary Seward ,  Daniel P. Sutherlin ,  Zachary K. Sweeney

Inventor： Georgette Castanedo ,  Bryan Chan ,  David Goldstein ,  Rama Kondru ,  Matthew Lucas ,  Wylie Palmer ,  Stephen Price ,  Brian Safina ,  Pascal Pierre Alexandre Savy ,  Eileen Mary Seward ,  Daniel P. Sutherlin ,  Zachary K. Sweeney

IPC: A61K31/535

CPC classification number: C07D513/04 ,  C07D487/04 ,  C07D491/04 ,  C07D495/04

Abstract: Formula I (Ia and Ib) compounds wherein (i) X1 is N and X2 is S, (ii) X1 is CR7 and X2 is S, (iii) X1 is N and X2 is NR2, or (iv) X1 is CR7 and X2 is O, including stereoisomers, 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, 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.

Abstract translation: 式（I）和（Ib）化合物，其中（i）X1为N，X 2为S，（ii）X1为CR7，X2为S，（iii）X1为N，X2为NR2，或（iv）X1为CR7， X 2为O，包括立体异构体，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：US08293763B2

公开(公告)日：2012-10-23

申请号：US12808346

申请日：2008-12-18

Applicant: Stephen Price ,  Robert Heald ,  Pascal Pierre Alexandre Savy

Inventor： Stephen Price ,  Robert Heald ,  Pascal Pierre Alexandre Savy

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

CPC classification number: C07D471/04 ,  C07D487/04

Abstract: 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)

Abstract translation: 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：US08158625B2

公开(公告)日：2012-04-17

申请号：US12787608

申请日：2010-05-26

Applicant: Georgette Castanedo ,  David Goldstein ,  Rama Kondru ,  Matthew Lucas ,  Wylie Palmer ,  Stephen Price ,  Brian Safina ,  Pascal Pierre Alexandre Savy ,  Eileen Mary Seward ,  Daniel P. Sutherlin ,  Zachary K. Sweeney

Inventor： Georgette Castanedo ,  David Goldstein ,  Rama Kondru ,  Matthew Lucas ,  Wylie Palmer ,  Stephen Price ,  Brian Safina ,  Pascal Pierre Alexandre Savy ,  Eileen Mary Seward ,  Daniel P. Sutherlin ,  Zachary K. Sweeney

IPC: A61K31/535 ,  C07D413/14

CPC classification number: C07D495/04 ,  C07D487/04 ,  C07D513/04

Abstract: Formula I (Ia and Ib) compounds wherein (i) X1 is N and X2 is S, (ii) X1 is CR7 and X2 is S, (iii) X1 is N and X2 is NR2, (iv) X1 is CR7 and X2 is O, or (v) X1 is CR7 and X2 is NR2, including stereoisomers, 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, 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.

Abstract translation: 式（I）和（Ib）化合物，其中（i）X1为N，X2为S，（ii）X1为CR7，X2为S，（iii）X1为N，X2为NR2，（iv）X1为CR7和X2 是O，或（v）X1是CR7，X2是NR2，包括立体异构体，互变异构体，代谢物和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介导的疾病，例如炎症，免疫学 ，和癌症。 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。

公开(公告)号：US20110190257A1

公开(公告)日：2011-08-04

申请号：US12999003

申请日：2009-07-01

Applicant: Robert Andrew Heald ,  Philip Jackson ,  Joseph P. Lyssikatos ,  Stephen Price ,  Pascal Pierre Alexandre Savy

Inventor： Robert Andrew Heald ,  Philip Jackson ,  Joseph P. Lyssikatos ,  Stephen Price ,  Pascal Pierre Alexandre Savy

IPC: A61K31/397 ,  C07D471/02 ,  C07D231/56 ,  C07D277/62 ,  C07D275/06 ,  A61K31/437 ,  A61K31/416 ,  A61K31/428 ,  A61P35/00

CPC classification number: C07D231/56 ,  C07D275/04 ,  C07D403/12 ,  C07D405/12 ,  C07D471/04

Abstract: The invention relates to bicyclic heterocycles of formulae I and II with anti-cancer and/or anti-inflammatory activity and more specifically with MEK kinase inhibitory activity. The invention provides compositions and methods useful for inhibiting abnormal cell growth, 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.

Abstract translation: 本发明涉及式I和II的双环杂环，其具有抗癌和/或抗炎活性，更具体地涉及MEK激酶抑制活性。 本发明提供了可用于抑制异常细胞生长，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：US20100305096A1

公开(公告)日：2010-12-02

申请号：US12787613

申请日：2010-05-26

Applicant: Georgette Castanedo ,  Bryan Chan ,  David Goldstein ,  Rama Kondru ,  Matthew Lucas ,  Wylie Palmer ,  Stephen Price ,  Brian Safina ,  Pascal Pierre Alexandre Savy ,  Eileen Mary Seward ,  Daniel P. Sutherlin ,  Zachary K. Sweeney

Inventor： Georgette Castanedo ,  Bryan Chan ,  David Goldstein ,  Rama Kondru ,  Matthew Lucas ,  Wylie Palmer ,  Stephen Price ,  Brian Safina ,  Pascal Pierre Alexandre Savy ,  Eileen Mary Seward ,  Daniel P. Sutherlin ,  Zachary K. Sweeney

IPC: A61K31/5377 ,  C07D495/04 ,  C07D471/04 ,  C07D473/16 ,  A61K31/541 ,  A61K31/55 ,  A61K31/551 ,  A61K31/553 ,  A61P35/00 ,  A61P37/00 ,  A61P9/00 ,  A61P31/12 ,  A61P29/00 ,  A61P3/00 ,  A61P5/00 ,  A61P25/00

CPC classification number: C07D513/04 ,  C07D487/04 ,  C07D491/04 ,  C07D495/04

Abstract: Formula I (Ia and Ib) compounds wherein (i) X1 is N and X2 is S, (ii) X1 is CR7 and X2 is S, (iii) X1 is N and X2 is NR2, or (iv) X1 is CR7 and X2 is O, including stereoisomers, 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, 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.

Abstract translation: 式（I）和（Ib）化合物，其中（i）X1为N，X 2为S，（ii）X1为CR7，X2为S，（iii）X1为N，X2为NR2，或（iv）X1为CR7， X 2为O，包括立体异构体，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：US20100305084A1

公开(公告)日：2010-12-02

申请号：US12787608

申请日：2010-05-26

Applicant: Georgette Castanedo ,  David Goldstein ,  Rama Kondru ,  Matthew Lucas ,  Wylie Palmer ,  Stephen Price ,  Brian Safina ,  Pascal Pierre Alexandre Savy ,  Eileen Mary Seward ,  Daniel P. Sutherlin ,  Zachary K. Sweeney

Inventor： Georgette Castanedo ,  David Goldstein ,  Rama Kondru ,  Matthew Lucas ,  Wylie Palmer ,  Stephen Price ,  Brian Safina ,  Pascal Pierre Alexandre Savy ,  Eileen Mary Seward ,  Daniel P. Sutherlin ,  Zachary K. Sweeney

IPC: A61K31/5377 ,  C07D513/04 ,  C07D498/10 ,  A61K31/5386 ,  A61K31/555 ,  A61P37/00 ,  A61P35/00 ,  A61P9/00 ,  A61P31/12 ,  A61P29/00 ,  A61P3/00 ,  A61P5/00 ,  A61P25/00

CPC classification number: C07D495/04 ,  C07D487/04 ,  C07D513/04

Abstract: Formula I (Ia and Ib) compounds wherein (i) X1 is N and X2 is S, (ii) X1 is CR7 and X2 is S, (iii) X1 is N and X2 is NR2, (iv) X1 is CR7 and X2 is O, or (v) X1 is CR7 and X2 is NR2, including stereoisomers, 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, 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.

Abstract translation: 式（I）和（Ib）化合物，其中（i）X1为N，X2为S，（ii）X1为CR7，X2为S，（iii）X1为N，X2为NR2，（iv）X1为CR7和X2 是O，或（v）X1是CR7，X2是NR2，包括立体异构体，互变异构体，代谢物和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介导的疾病，例如炎症，免疫学 ，和癌症。 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。