公开(公告)号：US08324221B2

公开(公告)日：2012-12-04

申请号：US12812384

申请日：2009-01-09

Applicant: Anna L. Banka ,  James F. Blake ,  Josef R. Bencsik ,  Kin Chiu Fong ,  Martin F. Hentemann ,  Douglas M. Sammond ,  Ian S. Mitchell ,  Rui Xu ,  Eli M. Wallace ,  Tony Tang

Inventor： Anna L. Banka ,  James F. Blake ,  Josef R. Bencsik ,  Kin Chiu Fong ,  Martin F. Hentemann ,  Douglas M. Sammond ,  Ian S. Mitchell ,  Rui Xu ,  Eli M. Wallace ,  Tony Tang

IPC: A01N43/54 ,  A01N43/90 ,  A61K31/517 ,  A61K31/519 ,  C07D239/70

CPC classification number: C07D471/10 ,  C07D487/10

Abstract: The present invention provides compounds of Formula (I) including tautomers, resolved enantiomers, resolved diastereomers, solvates, metabolites, salts and pharmaceutically acceptable prodrugs thereof. Also provided are methods of using the compounds of this invention as Akt protein kinase inhibitors and for the treatment of Akt-mediated diseases, for example, hyperproliferative diseases such as cancer.

Abstract translation: 本发明提供式（I）化合物，其包括互变异构体，拆分的对映异构体，拆分的非对映体，溶剂合物，代谢物，盐和药学上可接受的前药。 还提供了使用本发明化合物作为Akt蛋白激酶抑制剂和治疗Akt介导的疾病例如过度增殖性疾病如癌症的方法。

公开(公告)号：US20120178715A1

公开(公告)日：2012-07-12

申请号：US13393767

申请日：2010-09-03

Applicant: Steven W. Andrews ,  Kevin Ronald Condroski ,  Lisa A. De Meese ,  Jay Bradford Fell ,  John P. Fischer ,  John A. Josey ,  Kevin Koch ,  Yvan Le Huerou ,  Gregory F. Miknis ,  Martha E. Rodriguez ,  George T. Topalov ,  Eli M. Wallace ,  Rui Xu

Inventor： Steven W. Andrews ,  Kevin Ronald Condroski ,  Lisa A. De Meese ,  Jay Bradford Fell ,  John P. Fischer ,  John A. Josey ,  Kevin Koch ,  Yvan Le Huerou ,  Gregory F. Miknis ,  Martha E. Rodriguez ,  George T. Topalov ,  Eli M. Wallace ,  Rui Xu

IPC: A61K31/519 ,  A61K31/5377 ,  A61P35/00 ,  A61K31/5386 ,  A61K31/675 ,  C07D487/04 ,  C07D498/08

CPC classification number: C07D487/04

Abstract: Compounds of Formula I: and salts thereof in which R1, R2, R2a, R3, n, X and ring B have the meanings given in the specification, are inhibitors of mTOR and are useful in the treatment of diseases which are sensitive to inhibition of mTOR, such as cancers.

Abstract translation: 式I化合物及其盐，其中R 1，R 2，R 2a，R 3，n，X和环B具有本说明书中给出的含义，是mTOR的抑制剂，可用于治疗对抑制作用敏感的疾病 mTOR，如癌症。

公开(公告)号：US20120157453A1

公开(公告)日：2012-06-21

申请号：US13393111

申请日：2010-08-27

Applicant: Ignacio Aliagas ,  Stefan Gradl ,  Janet Gunzner ,  Simon Mathieu ,  Joachim Rudolph ,  Zhaoyang Wen ,  Steven Mark Wenglowsky

Inventor： Ignacio Aliagas ,  Stefan Gradl ,  Janet Gunzner ,  Simon Mathieu ,  Joachim Rudolph ,  Zhaoyang Wen ,  Steven Mark Wenglowsky

IPC: A61K31/519 ,  A61K31/52 ,  C07D487/04 ,  C07D495/04 ,  C07D491/048 ,  A61P13/12 ,  A61P35/00 ,  A61P25/28 ,  A61P9/00 ,  A61P29/00 ,  A61P25/06 ,  A61P25/00 ,  C07D473/34 ,  A61K31/5377

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

Abstract: Compounds of Formula II are useful for inhibition of Raf kinases. Methods of using compounds of Formula II and stereoisomers, tautomers, prodrugs and pharmaceutically acceptable salts thereof, 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II的化合物可用于抑制Raf激酶。 公开了使用式II化合物和其立体异构体，互变异构体，前药和其药学上可接受的盐在体外，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：US08202899B2

公开(公告)日：2012-06-19

申请号：US12668005

申请日：2008-07-18

Applicant: Mark C. Munson ,  Brian C. Baer

Inventor： Mark C. Munson ,  Brian C. Baer

IPC: A61K31/415 ,  C07D231/56

CPC classification number: C07D231/56

Abstract: Compounds of Formula (I) where R1 and R2 are as defined herein, and pharmaceutically acceptable salts thereof, are useful in the treatment and prevention of various disorders mediated by kinases.

Abstract translation: 其中R1和R2如本文所定义的式（I）化合物及其药学上可接受的盐可用于治疗和预防由激酶介导的各种疾病。

公开(公告)号：US20110319631A1

公开(公告)日：2011-12-29

申请号：US13229459

申请日：2011-09-09

Applicant: John Demattei ,  Sagar Shakya ,  Anthony D. Piscopio ,  Bruno P. Hache ,  Matthew Charles Evans ,  James Gair Ford ,  Simon Mark Pointon ,  Koen Peeters ,  Timothy John Lilley ,  John Leonard

Inventor： John Demattei ,  Sagar Shakya ,  Anthony D. Piscopio ,  Bruno P. Hache ,  Matthew Charles Evans ,  James Gair Ford ,  Simon Mark Pointon ,  Koen Peeters ,  Timothy John Lilley ,  John Leonard

IPC: C07D235/06

CPC classification number: C07D235/06 ,  C07C201/08 ,  C07C205/58 ,  C07C227/04 ,  C07C227/08 ,  C07C227/18 ,  C07C229/60

Abstract: Provided are methods for the synthesis of heterocyclic compounds such as benzimidazole carboxylic acid core structures having Formula Ib-1: wherein Z, X1, X2, X5, R2b and R10 are as defined herein. Compounds of Formula Ib-1 can be used to prepare heterocyclic derivatives such as benzimidazole derivatives.

Abstract translation: 提供了用于合成杂环化合物的方法，例如具有式Ib-1的苯并咪唑羧酸核心结构：其中Z，X1，X2，X5，R2b和R10如本文所定义。 式Ib-1的化合物可用于制备杂环衍生物如苯并咪唑衍生物。

公开(公告)号：US20110245230A1

公开(公告)日：2011-10-06

申请号：US13160351

申请日：2011-06-14

Applicant: Ian S. Mitchell ,  James F. Blake ,  Rui Xu ,  Nicholas C. Kallan ,  Dengming Xiao ,  Keith Lee Spencer ,  Josef R. Bencsik ,  Eli M. Wallace ,  Stephen T. Schlachter ,  Anna L. Banka ,  Jun Liang ,  Brian Safina ,  Jun Li ,  Christine Chabot

Inventor： Ian S. Mitchell ,  James F. Blake ,  Rui Xu ,  Nicholas C. Kallan ,  Dengming Xiao ,  Keith Lee Spencer ,  Josef R. Bencsik ,  Eli M. Wallace ,  Stephen T. Schlachter ,  Anna L. Banka ,  Jun Liang ,  Brian Safina ,  Jun Li ,  Christine Chabot

IPC: A61K31/397 ,  A61K31/497 ,  A61K31/5377 ,  A61P29/00 ,  A61P35/00 ,  A61P19/02 ,  A61P25/00 ,  A61P1/00 ,  A61P3/04 ,  A61P25/28 ,  A61P11/00 ,  A61P31/00 ,  A61P25/16 ,  A61P37/06

CPC classification number: C07D409/14 ,  A61K31/517 ,  A61K31/5377 ,  A61K45/06 ,  C07D239/70 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D409/12

Abstract: The present invention provides compounds of Formula I, including tautomers, resolved enantiomers, diastereomers, solvates, metabolites, salts and pharmaceutically acceptable prodrugs thereof. Also provided are methods of using the compounds of this invention as AKT protein kinase inhibitors and for the treatment of hyperproliferative diseases such as cancer.

公开(公告)号：US08022222B2

公开(公告)日：2011-09-20

申请号：US12161366

申请日：2007-01-24

Applicant: Thomas D. Aicher ,  Steven Armen Boyd ,  Mark Joseph Chicarelli ,  Kevin Ronald Condroski ,  Rustam Ferdinand Garrey ,  Ronald Jay Hinklin ,  Ajay Singh ,  Timothy M. Turner

Inventor： Thomas D. Aicher ,  Steven Armen Boyd ,  Mark Joseph Chicarelli ,  Kevin Ronald Condroski ,  Rustam Ferdinand Garrey ,  Ronald Jay Hinklin ,  Ajay Singh ,  Timothy M. Turner

IPC: C07D417/00 ,  A61K31/44

CPC classification number: C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D495/04 ,  C07D513/04

Abstract: Provided are compounds of formula I wherein R2, L, Z, Y, G and R1 are as defined herein, that are useful in the treatment and/or prevention of diseases or disorders mediated by deficient levels of glucokinase activity or which can be treated by activating glucokinase including, but not limited to, diabetes mellitus, impaired glucose tolerance, IFG (impaired fasting glucose) and IFG (impaired fasting glycemia), as well as other diseases and disorders such as those discussed herein.

Abstract translation: 提供式I化合物，其中R 2，L，Z，Y，G和R 1如本文所定义，其可用于治疗和/或预防由缺乏葡萄糖激酶水平的活性介导的疾病或病症，或可由 激活葡萄糖激酶，包括但不限于糖尿病，葡萄糖耐量降低，IFG（空腹血糖受损）和IFG（空腹血糖受损）），以及其他疾病和病症如本文讨论的疾病和病症。

公开(公告)号：US08003805B2

公开(公告)日：2011-08-23

申请号：US12824477

申请日：2010-06-28

Applicant: Eli M. Wallace ,  Joseph P. Lyssikatos ,  Allison L. Marlow ,  T. Brian Hurley

Inventor： Eli M. Wallace ,  Joseph P. Lyssikatos ,  Allison L. Marlow ,  T. Brian Hurley

IPC: A61K31/422 ,  A61K31/4245 ,  A61K31/4184 ,  C07D403/04 ,  C07D413/04

CPC classification number: C07D235/06 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/06 ,  C07D403/12 ,  C07D405/06 ,  C07D413/04 ,  C07D413/06 ,  C07D417/06 ,  C07D417/12

Abstract: Disclosed are compounds of the Formula I and pharmaceutically acceptable salts and prodrugs thereof, wherein W, R1, R2, R7, R8, R9 and R10 are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals. Also disclosed is a method of using such compounds in the treatment of hyperproliferative diseases in mammals, and pharmaceutical compositions containing such compounds.

公开(公告)号：US08003651B2

公开(公告)日：2011-08-23

申请号：US11773946

申请日：2007-07-05

Applicant: Ian S. Mitchell ,  James F. Blake ,  Rui Xu ,  Nicholas C. Kallan ,  Dengming Xiao ,  Keith Lee Spencer ,  Josef R. Bencsik ,  Eli M. Wallace ,  Stephen T. Schlachter ,  Anna L. Banka ,  Jun Liang ,  Brian Safina ,  Jun Li ,  Christine Chabot

Inventor： Ian S. Mitchell ,  James F. Blake ,  Rui Xu ,  Nicholas C. Kallan ,  Dengming Xiao ,  Keith Lee Spencer ,  Josef R. Bencsik ,  Eli M. Wallace ,  Stephen T. Schlachter ,  Anna L. Banka ,  Jun Liang ,  Brian Safina ,  Jun Li ,  Christine Chabot

IPC: C07D239/70 ,  A61K31/497 ,  A61P35/00 ,  A61P29/00 ,  A61P25/28 ,  A61P9/00

CPC classification number: C07D409/14 ,  A61K31/517 ,  A61K31/5377 ,  A61K45/06 ,  C07D239/70 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D409/12

Abstract: The present invention provides compounds of Formula I, including tautomers, resolved enantiomers, diastereomers, solvates, metabolites, salts and pharmaceutically acceptable prodrugs thereof. Also provided are methods of using the compounds of this invention as AKT protein kinase inhibitors and for the treatment of hyperproliferative diseases such as cancer.

Abstract translation: 本发明提供了式I化合物，包括互变异构体，拆分的对映异构体，非对映异构体，溶剂合物，代谢物，盐和药学上可接受的前药。 还提供了使用本发明化合物作为AKT蛋白激酶抑制剂和治疗过度增殖性疾病如癌症的方法。

公开(公告)号：US07932277B2

公开(公告)日：2011-04-26

申请号：US12118624

申请日：2008-05-09

Applicant: Scott Seiwert ,  Steven W. Andrews ,  Leonid Beigelman ,  Lawrence M. Blatt ,  Brad Buckman ,  Kevin R. Condroski ,  Yutong Jiang ,  Robert J. Kaus ,  April L. Kennedy ,  Timothy S. Kercher ,  Michael A. Lyon ,  Bin Wang

Inventor： Scott Seiwert ,  Steven W. Andrews ,  Leonid Beigelman ,  Lawrence M. Blatt ,  Brad Buckman ,  Kevin R. Condroski ,  Yutong Jiang ,  Robert J. Kaus ,  April L. Kennedy ,  Timothy S. Kercher ,  Michael A. Lyon ,  Bin Wang

IPC: A61K31/4035 ,  A61K31/428 ,  A61K31/4025 ,  A61K31/401 ,  C07D207/09 ,  C07D403/12 ,  C07D417/12

CPC classification number: C07D217/26 ,  C07D401/12 ,  C07D417/14

Abstract: The embodiments provide compounds of the general Formula I, as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments provide compounds of the general Formula II, as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments further provide treatment methods, including methods of treating a hepatitis C virus infection and methods of treating liver fibrosis, the methods generally involving administering to an individual in need thereof an effective amount of a subject compound or composition.

Abstract translation: 实施方案提供了通式I的化合物，以及包含主题化合物的组合物，包括药物组合物。 实施方案提供了通式II的化合物，以及包含主题化合物的组合物，包括药物组合物。 实施方案还提供治疗方法，包括治疗丙型肝炎病毒感染的方法和治疗肝纤维化的方法，所述方法通常涉及向有需要的个体施用有效量的主题化合物或组合物。