公开(公告)号：US20100260868A1

公开(公告)日：2010-10-14

申请号：US12757954

申请日：2010-04-09

Applicant: Michael J. Humphries ,  Shannon L. Winski

Inventor： Michael J. Humphries ,  Shannon L. Winski

IPC: A61K31/4545 ,  A61K31/7076 ,  A61K31/519 ,  A61K31/704 ,  A61K31/664 ,  A61K31/513 ,  A61K31/7068 ,  A61K31/4745 ,  A61K33/24 ,  A61P35/00

CPC classification number: A61K31/437 ,  A61K31/4375 ,  A61K31/4545 ,  A61K31/4745 ,  A61K31/513 ,  A61K31/519 ,  A61K31/664 ,  A61K31/704 ,  A61K31/7068 ,  A61K31/7076 ,  A61K33/24 ,  A61K45/06 ,  A61K2300/00

Abstract: Methods of treating cancer by administering a DNA damaging agent and a CHK1 Inhibitor on a dosing regimen are provided.

Abstract translation: 提供了通过在给药方案上施用DNA损伤剂和CHK1抑制剂来治疗癌症的方法。

公开(公告)号：US20100204240A1

公开(公告)日：2010-08-12

申请号：US12678995

申请日：2008-09-15

Applicant: Thomas Daniel Aicher ,  Steven Armen Boyd ,  Mark Joseph Chicarelli ,  Kevin Ronald Condroski ,  Jay Bradford Fell ,  John P. Fischer ,  Indrani W. Gunawardana ,  Ronald Jay Hinklin ,  Ajay Singh ,  Timothy M. Tumer ,  Eli M. Wallce

Inventor： Thomas Daniel Aicher ,  Steven Armen Boyd ,  Mark Joseph Chicarelli ,  Kevin Ronald Condroski ,  Jay Bradford Fell ,  John P. Fischer ,  Indrani W. Gunawardana ,  Ronald Jay Hinklin ,  Ajay Singh ,  Timothy M. Tumer ,  Eli M. Wallce

IPC: A61K31/501 ,  C07D417/14 ,  A61K31/444 ,  C07D417/12 ,  A61K31/4439 ,  A61K31/4709 ,  C07D471/04 ,  A61K31/437 ,  A61K31/517 ,  C07D491/052 ,  A61K31/436 ,  A61P3/10

CPC classification number: C07D401/14 ,  C07D213/75 ,  C07D401/12 ,  C07D417/12 ,  C07D417/14

Abstract: Provided are compounds of Formula (I): wherein R2, R3, R13, L and D2 are as defined in the specification, which 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）的化合物：其中R2，R3，R13，L和D2如说明书中所定义，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，或可以 通过激活葡糖激酶，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））以及其它疾病和病症如本文讨论的疾病和病症。

公开(公告)号：US20100173955A1

公开(公告)日：2010-07-08

申请号：US12438112

申请日：2007-08-21

Applicant: George Doherty ,  Adam Cook

Inventor： George Doherty ,  Adam Cook

IPC: A61K31/44 ,  C07C229/28 ,  A61K31/195 ,  C07D213/56 ,  C07C255/50 ,  A61K31/277 ,  C07D333/22 ,  A61K31/381 ,  C07D233/54 ,  A61K31/4164 ,  A61P37/00 ,  A61P29/00 ,  A61P35/00 ,  A61P17/00 ,  A61P11/00 ,  A61P3/10 ,  A61P1/00

CPC classification number: C07C311/19 ,  C07C233/75 ,  C07C233/87 ,  C07C235/46 ,  C07C255/57 ,  C07C271/22 ,  C07C307/06 ,  C07C311/06 ,  C07C317/46 ,  C07C2601/02 ,  C07C2601/14 ,  C07C2602/10 ,  C07D213/71 ,  C07D213/81 ,  C07D213/82 ,  C07D233/42 ,  C07D333/16 ,  Y02P20/55

Abstract: Compounds of Formula (I): in which R1, R2, R7, R8, R9, R10 and A have the meanings given in the specification, are DP2 receptor modulators useful in the treatment of immunologic diseases.

Abstract translation: 其中R1，R2，R7，R8，R9，R10和A具有本说明书中给出的含义的式（I）化合物是可用于治疗免疫疾病的DP2受体调节剂。

公开(公告)号：US20100145065A1

公开(公告)日：2010-06-10

申请号：US11993745

申请日：2006-06-21

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: C07D235/04 ,  C07C229/60 ,  C07C205/58

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 Ia-1 and their synthetic intermediates: wherein Z, X1, X2, X5, R2 and R10 are as defined herein. Compounds of Formula Ia-1 and their synthetic intermediates 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Ia-1的苯并咪唑羧酸核心结构及其合成中间体：其中Z，X1，X2，X5，R2和R10如本文所定义。 式Ia-1及其合成中间体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：US07732616B2

公开(公告)日：2010-06-08

申请号：US11435562

申请日：2006-05-17

Applicant: Allison L. Marlow ,  Eli M. Wallace ,  Jeongbeob Seo ,  Joseph P. Lyssikatos ,  Hong Woon Yang ,  James Blake

Inventor： Allison L. Marlow ,  Eli M. Wallace ,  Jeongbeob Seo ,  Joseph P. Lyssikatos ,  Hong Woon Yang ,  James Blake

IPC: C07D213/00

CPC classification number: C07D213/78 ,  C07D209/46 ,  C07D213/80 ,  C07D213/82 ,  C07D215/48 ,  C07D231/56 ,  C07D237/24 ,  C07D237/28 ,  C07D237/32 ,  C07D239/74 ,  C07D401/04 ,  C07D401/06 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04 ,  C07D471/04

Abstract: Disclosed are compounds of the Formulas I and V and pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, R7, R8 and R9, W, X and Y 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, and inflammatory conditions. Also disclosed are methods of using such compounds in the treatment of hyperproliferative diseases in mammals and pharmaceutical compositions containing such compounds.

Abstract translation: 公开了式I和V的化合物及其药学上可接受的盐和前药，其中R1，R2，R7，R8和R9，W，X和Y如说明书中所定义。 这些化合物是MEK抑制剂，可用于治疗哺乳动物和炎性病症中的过度增殖性疾病，例如癌症和炎症。 还公开了使用这些化合物治疗哺乳动物中过度增殖性疾病的方法和含有这些化合物的药物组合物。

公开(公告)号：US20100130748A1

公开(公告)日：2010-05-27

申请号：US11917998

申请日：2006-06-21

Applicant: John Demattei ,  Sagar Shakya ,  Paul J. Nichols ,  Bradley R. Barnett ,  Bruno P. Hache ,  Matthew Charles Evans ,  James Gair Ford ,  John Leonard

Inventor： John Demattei ,  Sagar Shakya ,  Paul J. Nichols ,  Bradley R. Barnett ,  Bruno P. Hache ,  Matthew Charles Evans ,  James Gair Ford ,  John Leonard

IPC: C07D235/04

CPC classification number: C07D235/08 ,  C07D235/06

Abstract: Provided are methods for the synthesis of heterocyclic compounds such as benzimidazole carboxylic acid core structures having Formula Ia-2 and their synthetic intermediates: wherein X1, X2, X5, R1, R2 and R4 are as defined herein. Compounds of Formula Ia-2 and their synthetic intermediates 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Ia-2的苯并咪唑羧酸核心结构及其合成中间体：其中X 1，X 2，X 5，R 1，R 2和R 4如本文所定义。 式Ia-2及其合成中间体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：US20100063066A1

公开(公告)日：2010-03-11

申请号：US12438967

申请日：2007-08-31

Applicant: Alexandre J. Buckmelter ,  Joseph P. Lyssikatos ,  Greg Miknia ,  Li Ren ,  Steven Mark Wenglowsky ,  Bryson Rast

Inventor： Alexandre J. Buckmelter ,  Joseph P. Lyssikatos ,  Greg Miknia ,  Li Ren ,  Steven Mark Wenglowsky ,  Bryson Rast

IPC: A61K31/497 ,  C07D401/14 ,  C07D471/04 ,  A61K31/4439 ,  A61P35/00

CPC classification number: C07D491/04

Abstract: Compounds of Formulas (I), (IIA) and (IIIA) are useful for inhibiting Raf kinase and for treating disorders mediated thereby. Methods of using compounds of Formulas (I), (IIA) and (IIIA) 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），（IIA）和（IIIA）的化合物可用于抑制Raf激酶和用于治疗由此介导的病症。 使用式（I），（IIA）和（IIIA）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中的这种病症或相关病理学的方法 条件被公开。

公开(公告)号：US20090270621A1

公开(公告)日：2009-10-29

申请号：US12496973

申请日：2009-07-02

Applicant: Eli Wallace ,  George Topalov ,  Joseph Lyssikatos ,  Alexandre Buckmelter ,  Qian Zhao

Inventor： Eli Wallace ,  George Topalov ,  Joseph Lyssikatos ,  Alexandre Buckmelter ,  Qian Zhao

IPC: C07D413/12 ,  C07D239/72 ,  C07D403/12

CPC classification number: C07D498/10 ,  C04B35/632 ,  C07D239/94 ,  C07D401/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/14 ,  C07D498/04

Abstract: This invention concerns quinazoline analogs of Formula I: where an A group is bonded to at least one of the carbons at the 5, 6, 7 or 8 position of the bicyclic ring, and the ring is substituted by up to three independent R3 groups. The invention also includes methods of using these compounds as type I receptor tyrosine kinase inhibitors and for the treatment of hyperproliferative diseases such as cancer.

Abstract translation: 本发明涉及式I的喹唑啉类似物：其中A基团与双环的5,6,7或8位上的至少一个碳键合，并且该环被多达三个独立的R 3基团取代。 本发明还包括使用这些化合物作为I型受体酪氨酸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：US07585975B2

公开(公告)日：2009-09-08

申请号：US12081725

申请日：2008-04-21

Applicant: Eli Wallace ,  George Topalov ,  Joseph Lyssikatos ,  Alexandre Buckmelter ,  Qian Zhao

Inventor： Eli Wallace ,  George Topalov ,  Joseph Lyssikatos ,  Alexandre Buckmelter ,  Qian Zhao

IPC: C07D239/00 ,  C07D239/70 ,  C07D471/00 ,  C07D487/00

CPC classification number: C07D498/10 ,  C04B35/632 ,  C07D239/94 ,  C07D401/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/14 ,  C07D498/04

Abstract: This invention concerns quinazoline analogs of Formula I: where an A group is bonded to at least one of the carbons at the 5, 6, 7 or 8 position of the bicyclic ring, and the ring is substituted by up to three independent R3 groups. The invention also includes methods of using these compounds as type I receptor tyrosine kinase inhibitors and for the treatment of hyperproliferative diseases such as cancer.

公开(公告)号：US20090156603A1

公开(公告)日：2009-06-18

申请号：US12282600

申请日：2007-03-23

Applicant: Thomas D. Aicher ,  Steven Armen Boyd ,  Mark Joseph Chicarelli ,  Kevin Ronald Condroski ,  Ronald Jay Hinklin ,  Ajay Singh

Inventor： Thomas D. Aicher ,  Steven Armen Boyd ,  Mark Joseph Chicarelli ,  Kevin Ronald Condroski ,  Ronald Jay Hinklin ,  Ajay Singh

IPC: A61K31/5377 ,  C07D417/12 ,  A61K31/4439 ,  A61K31/444 ,  C07D417/14 ,  A61K31/519 ,  C07D471/04

CPC classification number: C07D417/12 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D491/04 ,  C07D495/04 ,  C07D513/04

Abstract: Provided are compounds of formula I that are useful in the treatment and/or prevention of diseases mediated by deficient levels of glucokinase activity, such as diabetes meilitus. 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: 提供式I化合物，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。