公开(公告)号：US07598383B2

公开(公告)日：2009-10-06

申请号：US10992612

申请日：2004-11-18

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

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

IPC: C07D487/04 ,  A61K31/44

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, R7, R8 and R9, W, X and Y are as defined in the specifications. 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，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：US20090215834A1

公开(公告)日：2009-08-27

申请号：US12186273

申请日：2008-08-05

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

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

IPC: A61K31/4412 ,  C07D213/78 ,  A61P29/00 ,  A61P35/04

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 V and pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, R7, R8 and R9, and W are as defined in the specification. Such compounds are MEK inhibitors and 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 diseases and inflammatory conditions in mammals and pharmaceutical compositions containing such compounds.

Abstract translation: 公开了式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以及W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，如癌症和炎症以及炎性病症。 还公开了使用这些化合物治疗哺乳动物的过度增殖性疾病和炎性病症的方法以及含有这些化合物的药物组合物。

公开(公告)号：US20090209554A1

公开(公告)日：2009-08-20

申请号：US10593910

申请日：2005-03-23

Applicant: Steven A. Boyd ,  Kevin R. Condroski ,  Jason De Meese ,  Stephen S. Gonzales ,  Indrani W. Gunawardana ,  Tomas Kaplan ,  Yvan Le Huerou ,  Joseph Lyssikatos ,  Todd T. Romoff ,  Francis X. Sullivan ,  Allen Thomas

Inventor： Steven A. Boyd ,  Kevin R. Condroski ,  Jason De Meese ,  Stephen S. Gonzales ,  Indrani W. Gunawardana ,  Tomas Kaplan ,  Yvan Le Huerou ,  Joseph Lyssikatos ,  Todd T. Romoff ,  Francis X. Sullivan ,  Allen Thomas

IPC: A61K31/497 ,  C12N9/99 ,  C12N5/06 ,  A61K31/4439 ,  A61P35/00 ,  C07D417/06

CPC classification number: C07D417/06 ,  C07D417/14

Abstract: The present invention provides N-3′-pyridyl-methyl or N-2′-pyrazinylmethyl thiazolium derivatives of formula (I) which are useful as transketolase inhibitors wherein R1, R2, R3, Y, R5-R9, Ra-Rd, n and X− are as defined herein. The present invention also provides pharmaceutical compositions comprising the compounds of formula (I). The invention provides methods for inhibiting transketolase activity, reducing cellular ribose-5-phosphate levels, inhibiting nucleic acid synthesis, inhibiting cell proliferation and tumor cell growth in vitro and in vivo, stimulating apoptosis in tumor cells and treating cancer by administering a compound of formula (I) or a pharmaceutical composition thereof.

Abstract translation: 本发明提供了可用作转酮酶抑制剂的式（I）的N-3'-吡啶基 - 甲基或N-2'-吡嗪基甲基噻唑鎓衍生物，其中R1，R2，R3，Y，R5-R9，Ra-Rd，n 和X-如本文所定义。 本发明还提供包含式（I）化合物的药物组合物。 本发明提供了抑制转酮醇酶活性，减少细胞核糖-5-磷酸水平，抑制核酸合成，抑制体外和体内细胞增殖和肿瘤细胞生长，刺激肿瘤细胞凋亡和通过给予式 （I）化合物或其药物组合物。

公开(公告)号：US07538120B2

公开(公告)日：2009-05-26

申请号：US11208442

申请日：2005-08-19

Applicant: Kevin Koch ,  T. Brian Hurley ,  Hong Woon Yang ,  Joseph Lyssikatos ,  James F. Blake ,  Allison L. Marlow ,  Eli M. Wallace

Inventor： Kevin Koch ,  T. Brian Hurley ,  Hong Woon Yang ,  Joseph Lyssikatos ,  James F. Blake ,  Allison L. Marlow ,  Eli M. Wallace

IPC: A61K31/44

CPC classification number: C07D261/20 ,  A61K31/42 ,  C07D417/06 ,  C07D471/04

Abstract: Disclosed are methods of treating inflammatory diseases and disorders, such as arthritis and inflammatory bowel disease, in mammals.

Abstract translation: 公开了在哺乳动物中治疗炎性疾病和病症如关节炎和炎症性肠病的方法。

公开(公告)号：US07511058B2

公开(公告)日：2009-03-31

申请号：US11410336

申请日：2006-04-24

Applicant: T. Brian Hurley ,  Eli M. Wallace ,  Joseph P. Lyssikatos ,  James Blake

Inventor： T. Brian Hurley ,  Eli M. Wallace ,  Joseph P. Lyssikatos ,  James Blake

IPC: A61K31/437 ,  C07D471/02

CPC classification number: C07D471/04 ,  C07D261/20

Abstract: Disclosed are compounds of the Formula III and pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, R7, R8, R9 R10, and W 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 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III的化合物及其药学上可接受的盐和前药，其中R 1，R 2，R 7，R 8，R 9 R 10和W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和含有这些化合物的药物组合物。

公开(公告)号：US07501427B2

公开(公告)日：2009-03-10

申请号：US10642440

申请日：2003-08-14

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

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

IPC: A01N43/54 ,  A61K31/517 ,  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.

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：US20070293501A1

公开(公告)日：2007-12-20

申请号：US10593911

申请日：2005-03-23

Applicant: Steven Boyd ,  Kevin Condroski ,  Allen Thomas ,  Stephen Gonzales ,  Indrani Gunawardana ,  Yvan Huerou ,  Todd Romoff ,  Francis Sullivan

Inventor： Steven Boyd ,  Kevin Condroski ,  Allen Thomas ,  Stephen Gonzales ,  Indrani Gunawardana ,  Yvan Huerou ,  Todd Romoff ,  Francis Sullivan

IPC: A61K31/44 ,  A61K31/444 ,  A61K31/4965 ,  A61K31/497 ,  A61P35/00 ,  C07D213/70 ,  C07D401/12 ,  C07D403/12

CPC classification number: C07D213/73 ,  C07D405/12 ,  C07D411/12

Abstract: The present invention provides thioalkeneamides of formula (I) which are useful as transketolase inhibitors: wherein R1, R2, R3, R4, R5, R6, Ra-Rd, n and ring A are as defined herein. The present invention also provides pharmaceutical compositions comprising the compounds of formula (I). The invention provides methods for inhibiting transketolase activity, reducing cellular ribose-5-phosphate levels, inhibiting nucleic acid synthesis, inhibiting cell proliferation and tumor cell growth in vitro and in vivo, stimulating apoptosis in tumor cells and treating cancer by administering a compound of formula (I) or a pharmaceutical composition thereof.

Abstract translation: 本发明提供了可用作转酮酶抑制剂的式（I）的硫代链烯酰胺：其中R 1，R 2，R 3，R 3， R 4，R 5，R 6，R 9，R 11， 环A如本文所定义。 本发明还提供包含式（I）化合物的药物组合物。 本发明提供了抑制转酮醇酶活性，减少细胞核糖-5-磷酸水平，抑制核酸合成，抑制体外和体内细胞增殖和肿瘤细胞生长，刺激肿瘤细胞凋亡和通过给予式 （I）化合物或其药物组合物。

公开(公告)号：US07271178B2

公开(公告)日：2007-09-18

申请号：US11410343

申请日：2006-04-24

Applicant: Eli M. Wallace ,  James Blake

Inventor： Eli M. Wallace ,  James Blake

IPC: C07D471/04 ,  A61K31/437

CPC classification number: C07D471/04 ,  C07D261/20

Abstract: Disclosed are compounds of the Formula V and pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, R7, R8, R9, R10, R11 and W 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 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V的化合物及其药学上可接受的盐和前药，其中R 1，R 2，R 7，R 4， 8，R 9，R 10，R 11和W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和含有这些化合物的药物组合物。

公开(公告)号：US07230099B2

公开(公告)日：2007-06-12

申请号：US10929295

申请日：2004-08-30

Applicant: Eli Wallace ,  Brian Hurley ,  Hong Woon Yang ,  Joseph Lyssikatos ,  Jim Blake ,  Alison Marlow

Inventor： Eli Wallace ,  Brian Hurley ,  Hong Woon Yang ,  Joseph Lyssikatos ,  Jim Blake ,  Alison Marlow

IPC: C07D413/04 ,  C07D401/04 ,  C07D471/06

CPC classification number: C07D471/04 ,  C07D261/20

Abstract: Disclosed are compounds of the Formula and pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, R7, R8, R9 and R10, W 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. Also disclosed are methods of using such compounds in the treatment of hyperproliferative diseases in mammals and pharmaceutical compositions containing such compounds.

Abstract translation: 公开了式及其药学上可接受的盐和前药的化合物，其中R 1，R 2，R 7，R 8， R 9，R 9和R 10，W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和含有这些化合物的药物组合物。

公开(公告)号：US07226906B2

公开(公告)日：2007-06-05

申请号：US11201478

申请日：2005-08-11

Applicant: Kevin W. Hunt ,  Laurence E. Burgess

Inventor： Kevin W. Hunt ,  Laurence E. Burgess

IPC: A61K38/13 ,  C07K5/12 ,  C07K7/64

CPC classification number: A61K38/13 ,  A61K47/54 ,  A61K47/545 ,  C07K7/645

Abstract: Provided are novel cyclosporin analogs, methods for their production, and their use for treating immunoregulatory and respiratory diseases, disorders, and conditions.

Abstract translation: 提供新的环孢菌素类似物，其生产方法及其用于治疗免疫调节和呼吸系统疾病，病症和病症的用途。