公开(公告)号：US20100331283A1

公开(公告)日：2010-12-30

申请号：US12822066

申请日：2010-06-23

Applicant: Jeremy Hans ,  Eli M. Wallace ,  Qian Zhao ,  Shelley Allen ,  Ellen Laird ,  Joseph P. Lyssikatos ,  John E. Robisnson ,  Christopher P. Corrette ,  Robert Kirk DeLisle ,  Walter C. Voegtti

Inventor： Jeremy Hans ,  Eli M. Wallace ,  Qian Zhao ,  Shelley Allen ,  Ellen Laird ,  Joseph P. Lyssikatos ,  John E. Robisnson ,  Christopher P. Corrette ,  Robert Kirk DeLisle ,  Walter C. Voegtti

IPC: A61K31/675 ,  C07D417/04 ,  C07D513/04 ,  C07D419/04 ,  C07D471/04 ,  C07D487/04 ,  C07D495/04 ,  C07F9/06 ,  C07D417/14 ,  A61K31/433 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/5355 ,  A61K31/542 ,  A61K31/4985 ,  A61K31/5025 ,  A61K31/519 ,  A61K31/454 ,  A61P35/00 ,  A61P31/10 ,  A61P37/00 ,  A61P29/00 ,  A61P9/00

CPC classification number: C07D513/04 ,  C07D285/12 ,  C07D417/04 ,  C07D417/14 ,  C07D419/04 ,  C07D471/04 ,  C07D487/04 ,  C07D495/04 ,  C07D497/04 ,  C07F9/65395

Abstract: This invention relates to inhibitors of mitotic kinesins, particularly KSP, and methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing the inhibitors and pharmaceutical compositions in the treatment and prevention of various disorders.

公开(公告)号：US20100280043A1

公开(公告)日：2010-11-04

申请号：US12812448

申请日：2009-01-08

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

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

IPC: A61K31/496 ,  C07D471/04 ,  A61P35/00

CPC classification number: C07D471/04

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：US20100267793A1

公开(公告)日：2010-10-21

申请号：US12824521

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: A61K31/4184 ,  A61P35/04 ,  A61P17/00

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 methods of treating a hyperproliferative disorder or a disease related to vasculogenesis or angiogenesis in a mammal, comprising administering to said mammal an effective amount of a compound of the formula or a pharmaceutically accepted salt thereof, wherein A, R1, R2, R7, R8, and R9 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.

Abstract translation: 公开了治疗哺乳动物中过度增殖性疾病或与血管发生或血管发生相关的疾病的方法，包括向所述哺乳动物施用有效量的下式化合物或其药学上可接受的盐，其中A，R 1，R 2，R 7， R8和R9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中的过度增生性疾病，例如癌症和炎症。

公开(公告)号：US20100267710A1

公开(公告)日：2010-10-21

申请号：US12824497

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: A61K31/4184 ,  C07D235/06 ,  C07D405/12 ,  C07D405/06 ,  C07D417/06 ,  A61K31/427 ,  C07D413/12 ,  A61K31/5377 ,  C07D401/12 ,  A61K31/454 ,  C07D403/12 ,  C07D403/06 ,  A61K31/496 ,  C07D401/06 ,  A61K31/4439 ,  A61K31/541 ,  C07D413/06 ,  A61K31/422 ,  A61K31/4245 ,  A61P35/00

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：US07772234B2

公开(公告)日：2010-08-10

申请号：US10992605

申请日：2004-11-18

Applicant: Eli Wallace ,  Hong Woon Yang ,  James Blake

Inventor： Eli Wallace ,  Hong Woon Yang ,  James Blake

IPC: A01N43/60 ,  A61K31/495 ,  C07D237/26 ,  C07D487/00

CPC classification number: 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 Formula I and pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, R8, R9 and R10, W, X, and Z 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化合物及其药学上可接受的盐和前药，其中R1，R2，R8，R9和R10，W，X和Z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：US20100029633A1

公开(公告)日：2010-02-04

申请号：US12593879

申请日：2008-03-27

Applicant: Shelley Allen ,  Julie Marie Greschuk ,  Nicholas C. Kallan ,  Fredrik P. Marmsãter ,  Mark C. Munson ,  James P. Rizzi ,  John E. Robinson ,  Stephen T. Schlachter ,  George T. Topalov ,  Qian Zhao ,  Joseph P. Lyssikatos

Inventor： Shelley Allen ,  Julie Marie Greschuk ,  Nicholas C. Kallan ,  Fredrik P. Marmsãter ,  Mark C. Munson ,  James P. Rizzi ,  John E. Robinson ,  Stephen T. Schlachter ,  George T. Topalov ,  Qian Zhao ,  Joseph P. Lyssikatos

IPC: A61K31/5386 ,  C07D471/02 ,  A61K31/437 ,  A61P35/04 ,  C07D401/14 ,  A61K31/506 ,  C07D498/08

CPC classification number: C07D471/04

Abstract: Compounds of Formula I: in which A, B, R1, R1a, R2, R3, R4, R5 R6, R7 and R8 have the meanings given in the specification, are receptor tyrosine inhibitors useful in the treatment of diseases mediated by class 3 and class 5 receptor tyrosine kinases. Particular compounds of this invention have also been found to be inhibitors of Pim-1.

Abstract translation: 式I化合物：其中A，B，R 1，R 1a，R 2，R 3，R 4，R 5，R 6，R 7和R 8具有说明书中给出的含义，是受体酪氨酸抑制剂，其可用于治疗由3类和 5类受体酪氨酸激酶。 本发明的具体化合物也被发现是Pim-1的抑制剂。

公开(公告)号：US20090209542A1

公开(公告)日：2009-08-20

申请号：US12186202

申请日：2008-08-05

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

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

IPC: A61K31/50 ,  C07D237/06

CPC classification number: C07D213/80 ,  A61K31/437 ,  A61K31/4412 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/497 ,  A61K31/50 ,  A61K31/501 ,  A61K31/5025 ,  A61K31/5377 ,  A61K45/06 ,  C07D209/46 ,  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 ,  A61K2300/00

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

Abstract translation: 公开了式I化合物及其药学上可接受的盐和前药，其中R1，R2，R7，R8，R9和W如说明书中所定义。 这些化合物是MEK抑制剂，并且可用于治疗过度增殖性疾病，例如癌症和炎症，以及哺乳动物中的炎性病症。 还公开了使用这些化合物治疗哺乳动物中过度增生和炎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：US20090149459A1

公开(公告)日：2009-06-11

申请号：US12364310

申请日：2009-02-02

Applicant: Mark Munson ,  David A. Mareska ,  Youngboo Kim ,  Robert D. Groneberg ,  James Rizzi ,  Martha Rodriguez ,  Ganghyeok Kim ,  Guy Vigers ,  Chang Rao ,  Devan Balachari ,  Darren Harvey

Inventor： Mark Munson ,  David A. Mareska ,  Youngboo Kim ,  Robert D. Groneberg ,  James Rizzi ,  Martha Rodriguez ,  Ganghyeok Kim ,  Guy Vigers ,  Chang Rao ,  Devan Balachari ,  Darren Harvey

IPC: A61K31/416 ,  C07D471/04 ,  C07D413/02 ,  C07D231/56 ,  A61P37/00 ,  A61P31/00 ,  A61P25/28 ,  A61P19/08 ,  A61P29/00 ,  A61K31/437 ,  A61K31/5377

CPC classification number: C07D401/14 ,  C07D231/56 ,  C07D261/20 ,  C07D403/04 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12 ,  C07D471/04

Abstract: This invention relates to inhibitors of p38 and methods of utilizing the inhibitors and pharmaceutical compositions thereof in the treatment and prevention of various disorders mediated by p38.

公开(公告)号：US20090048279A1

公开(公告)日：2009-02-19

申请号：US12249421

申请日：2008-10-10

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

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

IPC: A61K31/517 ,  C07D239/94 ,  A61P35/00 ,  C07D401/12

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

Abstract: This invention provides quinazoline analogs of Formula I: where A 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 two independent R3 groups. The invention also includes methods of using compounds of Formula I as type I receptor tyrosine kinase inhibitors and for the treatment of hyperproliferative diseases such as cancer.

Abstract translation: 本发明提供式I的喹唑啉类似物：其中A与双环的5,6,7或8位上的至少一个碳键合，并且该环被至多两个独立的R 3基团取代。 本发明还包括使用式I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：US07425637B2

公开(公告)日：2008-09-16

申请号：US11061336

申请日：2005-02-18

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: C07D235/06 ,  A61K31/4184

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.

Abstract translation: 公开了式I化合物及其药学上可接受的盐和前药，其中W，R 1，R 2，R 7，R 7， SUP> 8，R 9和R 10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中的过度增生性疾病，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，以及含有这些化合物的药物组合物。