公开(公告)号：US08431713B2

公开(公告)日：2013-04-30

申请号：US12524327

申请日：2008-01-16

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

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

IPC: A61K31/44 ,  C07D213/55

CPC classification number: C07D495/04 ,  C07D417/14

Abstract: Provided are compounds having the Formula I or salts thereof, wherein R2, L, R3, R11, D2 and R13 are as defined herein, that are useful in the treatment and/or prevention of diseases mediated by deficient levels of glucokinase activity, such as diabetes mellitus. Also provided are methods of treating or preventing diseases and disorders characterized by underactivity of glucokinase or which can be treated by activating glucokinase.

Abstract translation: 提供具有式I的化合物或其盐，其中R2，L，R3，R11，D2和R13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，例如 糖尿病 还提供了治疗或预防以葡萄糖激酶不足活性为特征的疾病和病症的方法，或者可以通过激活葡糖激酶治疗。

公开(公告)号：US20130045286A1

公开(公告)日：2013-02-21

申请号：US13425186

申请日：2012-03-20

Applicant: Yvan Le Huerou ,  James F. Blake ,  Indrani W. Gunwardana ,  Pete Mohr ,  Eli M. Wallace ,  Bin Wang ,  Mark Joseph Chicarelli ,  Michael Lyon

Inventor： Yvan Le Huerou ,  James F. Blake ,  Indrani W. Gunwardana ,  Pete Mohr ,  Eli M. Wallace ,  Bin Wang ,  Mark Joseph Chicarelli ,  Michael Lyon

IPC: A61K31/4545 ,  A61K31/437 ,  A61K31/497 ,  A61K31/506 ,  A61P35/00 ,  A61K31/498 ,  A61K31/7068 ,  A61K31/4745 ,  A61K33/24 ,  A61K31/513 ,  A61K31/444 ,  A61K31/501

CPC classification number: C07D471/04 ,  C07D401/06 ,  C07D519/00

Abstract: Compounds of Formula I are useful for inhibition of CHK1 and/or CHK2. Methods of using compounds of Formula I and stereoisomers 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.

公开(公告)号：US20130018033A1

公开(公告)日：2013-01-17

申请号：US13393116

申请日：2010-08-27

Applicant: Ignacio Aliagas ,  Stefan Gradl ,  Janet Gunzner ,  Wendy Lee ,  Simon Mathieu ,  Joachim Rudolph ,  Zhaoyang Wen ,  Guiling Zhao ,  Alexandre J. Buckmelter ,  Jonas Grina ,  Joshua D. Hansen ,  Ellen Laird ,  David Moreno ,  Li Ren ,  Steven Mark Wenglowsky

Inventor： Ignacio Aliagas ,  Stefan Gradl ,  Janet Gunzner ,  Wendy Lee ,  Simon Mathieu ,  Joachim Rudolph ,  Zhaoyang Wen ,  Guiling Zhao ,  Alexandre J. Buckmelter ,  Jonas Grina ,  Joshua D. Hansen ,  Ellen Laird ,  David Moreno ,  Li Ren ,  Steven Mark Wenglowsky

IPC: A61K31/517 ,  C07D471/04 ,  A61K31/519 ,  C07D405/12 ,  A61P35/02 ,  C07D401/12 ,  C07D413/12 ,  A61K31/5377 ,  C07D239/72 ,  A61P35/00 ,  C07D239/94 ,  C07D403/12

CPC classification number: C07D239/94 ,  C07D403/12 ,  C07D405/12 ,  C07D471/04

Abstract: Compounds of Formula I are useful for inhibition of Raf kinases. Methods of using compounds of Formula I 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I化合物可用于抑制Raf激酶。 公开了使用式I化合物和立体异构体，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：US08329709B2

公开(公告)日：2012-12-11

申请号：US12812377

申请日：2009-01-09

Applicant: Anna L. Banka ,  Josef R. Bencsik ,  James Blake ,  Martin Hentemann ,  Nicholas C. Kallan ,  Jun Liang ,  Ian S. Mitchell ,  Stephen T. Schlachter ,  Eli M. Wallace ,  Rui Xu ,  Tony P. Tang

Inventor： Anna L. Banka ,  Josef R. Bencsik ,  James Blake ,  Martin Hentemann ,  Nicholas C. Kallan ,  Jun Liang ,  Ian S. Mitchell ,  Stephen T. Schlachter ,  Eli M. Wallace ,  Rui Xu ,  Tony P. Tang

IPC: A61K31/517 ,  C07D239/70

CPC classification number: C07D401/10 ,  C07D211/08 ,  C07D211/46 ,  C07D239/70 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04 ,  C07D403/10 ,  C07D409/04 ,  C07D417/04 ,  C07D417/10 ,  C07D487/04

Abstract: Compounds of Formula I are useful for inhibiting AKT protein kinases. Methods using compounds of Formula I and stereoisomers 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. Formula (I).

Abstract translation: 式I化合物可用于抑制AKT蛋白激酶。 公开了使用式I化合物及其立体异构体及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。 式（I）。

公开(公告)号：US08329701B2

公开(公告)日：2012-12-11

申请号：US12307537

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

Inventor： Ian S. Mitchell ,  James F. Blake ,  Rui Xu ,  Nicholas C. Kallan ,  Dengming Xiao ,  Keith Lee Spencer ,  Josef R. Bencsik

IPC: A61K31/519 ,  A61P29/00 ,  A61P17/00 ,  A61P9/00 ,  A61P25/28 ,  A61P15/00 ,  A61P35/00 ,  C07D491/048

CPC classification number: C07D493/04

Abstract: The present invention provides compounds, including resolved enantiomers, diastereomers, solvates and pharmaceutically acceptable salts thereof, comprising the Formula (I): 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: 本发明提供包含式（I）的分解的对映体，非对映异构体，溶剂化物和药学上可接受的盐的化合物：还提供了使用本发明化合物作为AKT蛋白激酶抑制剂和用于治疗过度增殖性疾病 作为癌症。

公开(公告)号：US08314090B2

公开(公告)日：2012-11-20

申请号：US12614048

申请日：2009-11-06

Applicant: J. Jeffry Howbert ,  Venkat Reddy Kusukuntla ,  Alexander Tretyakov ,  Nathan Nielsen ,  Pavel Krasik ,  Ji-Long Jiang ,  Hong Woon Yang

Inventor： J. Jeffry Howbert ,  Venkat Reddy Kusukuntla ,  Alexander Tretyakov ,  Nathan Nielsen ,  Pavel Krasik ,  Ji-Long Jiang ,  Hong Woon Yang

IPC: A61P31/00 ,  A61K31/55 ,  C07D223/16

CPC classification number: C07D403/10 ,  C07D223/16

Abstract: The disclosure describes method of synthesis of substituted benzazepine derivatives. Preferred methods according to the disclosure allow for large-scale preparation of benzazepine compounds having low levels of metal impurities. In some embodiments, preferred methods according to the disclosure also allow for the preparation of benzazepine derivatives without the use of chromatographic purification methods and in better yield than previously used methods for preparing such compounds. The methods disclosed herein find utility in synthetic organic chemistry as well as medicinal chemistry.

Abstract translation: 本公开描述了取代的苯并氮杂衍生物的合成方法。 根据本公开的优选方法允许大规模制备具有低水平金属杂质的苯并氮杂化合物。 在一些实施方案中，根据本公开的优选方法还允许制备苯并氮杂衍生物，而不使用色谱纯化方法，并且比以前使用的制备此类化合物的方法更好的产率。 本文公开的方法可用于合成有机化学以及药物化学。

公开(公告)号：US08304407B2

公开(公告)日：2012-11-06

申请号：US13414579

申请日：2012-03-07

Applicant: George A. Doherty ,  Charles Todd Eary ,  Robert D. Groneberg ,  Zachary Jones

Inventor： George A. Doherty ,  Charles Todd Eary ,  Robert D. Groneberg ,  Zachary Jones

IPC: A61P37/00 ,  A61K31/55 ,  C07D223/16 ,  C07D403/10

CPC classification number: C07D223/16

Abstract: Provided are compositions and methods useful for modulation of signaling through the Toll-like receptors TLR7 and/or TLR8. The compositions and methods have use in the treatment of autoimmunity, inflammation allergy, asthma, graft rejection, graft versus host disease, infection, sepsis, cancer and immunodeficiency.

Abstract translation: 提供了可用于通过Toll样受体TLR7和/或TLR8调节信号传导的组合物和方法。 组合物和方法用于治疗自身免疫，炎症过敏，哮喘，移植物排斥，移植物抗宿主病，感染，败血症，癌症和免疫缺陷。

公开(公告)号：US20120165317A1

公开(公告)日：2012-06-28

申请号：US13414579

申请日：2012-03-07

Applicant: George A. Doherty ,  C. Todd Eary ,  Robert D. Groneberg ,  Zachary Jones

Inventor： George A. Doherty ,  C. Todd Eary ,  Robert D. Groneberg ,  Zachary Jones

IPC: A61K31/55 ,  A61P37/08 ,  A61P35/00

CPC classification number: C07D223/16

Abstract: Provided are compositions and methods useful for modulation of signaling through the Toll-like receptors TLR7 and/or TLR8. The compositions and methods have use in the treatment of autoimmunity, inflammation allergy, asthma, graft rejection, graft versus host disease, infection, sepsis, cancer and immunodeficiency.

Abstract translation: 提供了可用于通过Toll样受体TLR7和/或TLR8调节信号传导的组合物和方法。 组合物和方法用于治疗自身免疫，炎症过敏，哮喘，移植物排斥，移植物抗宿主病，感染，败血症，癌症和免疫缺陷。

公开(公告)号：US08178131B2

公开(公告)日：2012-05-15

申请号：US12992468

申请日：2009-05-13

Applicant: Yvan Le Huerou ,  James F. Blake ,  Indrani W. Gunawardana ,  Peter J. Mohr ,  Eli M. Wallace ,  Bin Wang ,  Mark Joseph Chicarelli ,  Michael Lyon

Inventor： Yvan Le Huerou ,  James F. Blake ,  Indrani W. Gunawardana ,  Peter J. Mohr ,  Eli M. Wallace ,  Bin Wang ,  Mark Joseph Chicarelli ,  Michael Lyon

IPC: A61K33/24 ,  A61K31/437 ,  A61K31/7068 ,  A61K31/4745 ,  A61K31/513 ,  A61K31/497 ,  A61K31/506 ,  A61K31/501 ,  A61K31/498 ,  A61K31/5377 ,  A61K31/55 ,  A61P35/00 ,  C07D471/04

CPC classification number: C07D471/04 ,  C07D401/06 ,  C07D519/00

Abstract: Compounds of Formula (I) are useful for inhibition of CHK1 and/or CHK2. Methods of using compounds of Formula (I) and stereoisomers 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（I）的化合物可用于抑制CHK1和/或CHK2。 公开了使用式（I）化合物及其立体异构体及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：US20120101103A1

公开(公告)日：2012-04-26

申请号：US13141675

申请日：2009-12-18

Applicant: Adam Cook ,  Kevin W. Hunt ,  Robert Kirk Delisle ,  Todd Romoff ,  Christopher T. Clark ,  Ganghyeok Kim ,  Christopher P. Corrette ,  George A. Doherty ,  Laurence E. Burgess

Inventor： Adam Cook ,  Kevin W. Hunt ,  Robert Kirk Delisle ,  Todd Romoff ,  Christopher T. Clark ,  Ganghyeok Kim ,  Christopher P. Corrette ,  George A. Doherty ,  Laurence E. Burgess

IPC: A61K31/498 ,  A61K31/497 ,  A61K31/506 ,  A61K31/4709 ,  A61K31/453 ,  A61K31/444 ,  A61K31/4433 ,  A61K31/433 ,  A61K31/427 ,  A61K31/428 ,  A61K31/423 ,  A61K31/4155 ,  A61K31/4025 ,  C07D405/14 ,  C07D405/12 ,  C07D417/12 ,  A61K31/501

CPC classification number: C07D405/12 ,  C07D405/14 ,  C07D413/12 ,  C07D417/12

Abstract: Compounds of Formula I: (I) in which A, A1, R1, R7a, R7b, R8 and R10 have the meanings given in the specification, are DP2 receptor inhibitors useful in the treatment of useful in the treatment and prevention of immunologic diseases, allergic diseases such as asthma, allergic rhinitis and atopic dermatitis, and other inflammatory diseases mediated by prostaglandin D2 (PGD2). The compounds of Formula I may also be useful in treating diseases or medical conditions involving the Th2 T cell via production of IL-4, IL-5 and/or IL-13.

Abstract translation: 其中A，A1，R1，R7a，R7b，R8和R10具有本说明书中给出的含义的式I化合物：（I）是可用于治疗和预防免疫疾病的DP2受体抑制剂， 过敏性疾病如哮喘，过敏性鼻炎和特应性皮炎，以及由前列腺素D2（PGD2）介导的其他炎性疾病。 式I化合物还可用于通过产生IL-4，IL-5和/或IL-13来治疗涉及Th2T细胞的疾病或医学病症。