公开(公告)号：US20080139535A1

公开(公告)日：2008-06-12

申请号：US12019356

申请日：2008-01-24

申请人： Sampath K. Anandan ,  Xiao-Yi Xiao ,  Dinesh V. Patel ,  John S. Ward

发明人： Sampath K. Anandan ,  Xiao-Yi Xiao ,  Dinesh V. Patel ,  John S. Ward

IPC分类号： A61K31/5513 ,  C07D417/02 ,  C07D243/14 ,  A61K31/445 ,  A61P35/00 ,  C07D401/02 ,  A61K31/497

CPC分类号： C07D277/56 ,  C07D277/42 ,  C07D417/04

摘要： Disclosed are compounds which inhibit histone deacetylase (HDAC) enzymatic activity. Also disclosed are pharmaceutical compositions comprising such compounds as well as methods to treat conditions, particularly proliferative conditions, mediated at least in part by HDAC.

摘要翻译： 公开了抑制组蛋白脱乙酰酶（HDAC）酶活性的化合物。 还公开了包含这些化合物的药物组合物以及至少部分由HDAC介导的治疗条件，特别是增殖病症的方法。

公开(公告)号：US07772245B2

公开(公告)日：2010-08-10

申请号：US11354594

申请日：2006-02-14

申请人： Sampath K. Anandan ,  Xiao-Yi Xiao ,  John S. Ward ,  Dinesh V. Patel

发明人： Sampath K. Anandan ,  Xiao-Yi Xiao ,  John S. Ward ,  Dinesh V. Patel

IPC分类号： A61K31/506 ,  C07D471/02

CPC分类号： C07D471/04 ,  C07D401/04 ,  C07D487/04 ,  C07D491/04 ,  C07D495/04

摘要： Disclosed are compounds of formula I that inhibit histone deacetylase (HDAC) enzymatic activity, pharmaceutical compositions comprising such compounds, as well as methods to treat conditions, particularly proliferative conditions, mediated at least in part by HDAC, wherein A, W, W1, W2, Ar2, and G are described herein.

摘要翻译： 公开了抑制组蛋白脱乙酰酶（HDAC）酶活性的式I化合物，包含这些化合物的药物组合物以及至少部分由HDAC介导的条件，特别是增殖性病症的方法，其中A，W，W1，W2 ，Ar2和G。

公开(公告)号：US07345043B2

公开(公告)日：2008-03-18

申请号：US11096550

申请日：2005-04-01

申请人： Sampath K. Anandan ,  Xiao-Yi Xiao ,  Dinesh V. Patel ,  John Ward

发明人： Sampath K. Anandan ,  Xiao-Yi Xiao ,  Dinesh V. Patel ,  John Ward

IPC分类号： A61K31/497 ,  A61K31/427 ,  A61K31/4535 ,  A61K31/454 ,  C07D417/04 ,  C07D277/28

CPC分类号： C07D277/56 ,  C07D277/42 ,  C07D417/04

摘要： Disclosed are compounds which inhibit histone deacetylase (HDAC) enzymatic activity. Also disclosed are pharmaceutical compositions comprising such compounds as well as methods to treat conditions, particularly proliferative conditions, mediated at least in part by HDAC.

摘要翻译： 公开了抑制组蛋白脱乙酰酶（HDAC）酶活性的化合物。 还公开了包含这些化合物的药物组合物以及至少部分由HDAC介导的治疗条件，特别是增殖病症的方法。

公开(公告)号：US07164011B2

公开(公告)日：2007-01-16

申请号：US10642807

申请日：2003-08-15

申请人： Jason Lewis ,  Dinesh V. Patel ,  Sampath K. Anandan ,  Mikhail F. Gordeev

发明人： Jason Lewis ,  Dinesh V. Patel ,  Sampath K. Anandan ,  Mikhail F. Gordeev

IPC分类号： C07H15/26

CPC分类号： C07H17/00 ,  C07H15/16

摘要： Novel lincomycin derivatives are disclosed. These lincomycin derivatives exhibit antibacterial activity. As the compounds of the subject invention exhibit potent activities against bacteria, including gram positive organisms, they are useful antimicrobial agents. Methods of synthesis and of use of the compounds are also disclosed.

摘要翻译： 公开了新的林可霉素衍生物。 这些林可霉素衍生物具有抗菌活性。 由于本发明的化合物表现出对细菌（包括革兰氏阳性生物）的有效活性，因此它们是有用的抗微生物剂。 还公开了化合物的合成和使用方法。

公开(公告)号：US5929278A

公开(公告)日：1999-07-27

申请号：US81466

申请日：1998-05-19

申请人： David A. Campbell ,  Dinesh V. Patel ,  Xiao-Yi Xiao

发明人： David A. Campbell ,  Dinesh V. Patel ,  Xiao-Yi Xiao

IPC分类号： C07C323/60 ,  C07K5/06 ,  C07K5/072 ,  C07C321/00

CPC分类号： C07C323/60 ,  C07K5/06043 ,  C07K5/06095 ,  C07C2101/14

摘要： Disclosed are novel inhibitors of metalloproteases, in particular matrix metalloproteases. The disclosed inhibitors are mercaptoketone and mercaptoalcohol compounds which are useful in pharmaceutical compositions and methods for treating or controlling disease states or conditions which involve tissue breakdown, for example, arthropathy, dermatological conditions, bone resorption, inflammatory diseases, and tumor invasion and in the promotion of wound healing.

摘要翻译： 公开了金属蛋白酶，特别是基质金属蛋白酶的新型抑制剂。 所公开的抑制剂是巯基酮和巯基醇化合物，其可用于治疗或控制涉及组织分解的疾病状态或病症的方法，例如关节病，皮肤病学条件，骨吸收，炎性疾病和肿瘤侵袭以及促进 的伤口愈合。

公开(公告)号：US5840698A

公开(公告)日：1998-11-24

申请号：US549346

申请日：1995-10-27

申请人： David A. Campbell ,  Dinesh V. Patel ,  Xiao-Yi Xiao

发明人： David A. Campbell ,  Dinesh V. Patel ,  Xiao-Yi Xiao

IPC分类号： A61K38/00 ,  C07C323/60 ,  C07D209/48 ,  C07K5/06 ,  A61K38/06

CPC分类号： C07D209/48 ,  C07C323/60 ,  C07K5/06043 ,  A61K38/00

摘要： Disclosed are novel inhibitors of collagenase-1 and stromelysin-I metalloproteases. The disclosed inhibitors are mercaptoketone and mercaptoalcohol compounds which are useful in pharmaceutical compositions and methods for treating or controlling disease states or conditions which involve tissue breakdown, for example, arthropathy, dermatological conditions, bone resorption, inflammatory diseases, and tumor invasion and in the promotion of wound healing.

摘要翻译： 公开了胶原酶-1和基质溶蛋白-I金属蛋白酶的新型抑制剂。 所公开的抑制剂是巯基酮和巯基醇化合物，其可用于治疗或控制涉及组织分解的疾病状态或病症的方法，例如关节病，皮肤病学条件，骨吸收，炎性疾病和肿瘤侵袭以及促进 的伤口愈合。

公开(公告)号：US5831004A

公开(公告)日：1998-11-03

申请号：US549345

申请日：1995-10-27

申请人： David A. Campbell ,  Dinesh V. Patel ,  Xiao-Yi Xiao

发明人： David A. Campbell ,  Dinesh V. Patel ,  Xiao-Yi Xiao

IPC分类号： C07C323/60 ,  C07K5/06 ,  C07K5/072 ,  C07K5/00

CPC分类号： C07C323/60 ,  C07K5/06043 ,  C07K5/06095 ,  C07C2101/14

摘要： Disclosed are novel inhibitors of metalloproteases, in particular matrix metalloproteases. The disclosed inhibitors are mercaptoketone and mercaptoalcohol compounds which are useful in pharmaceutical compositions and methods for treating or controlling disease states or conditions which involve tissue breakdown, for example, arthropathy, dermatological conditions, bone resorption, inflammatory diseases, and tumor invasion and in the promotion of wound healing.

公开(公告)号：US08153630B2

公开(公告)日：2012-04-10

申请号：US11667205

申请日：2005-11-17

申请人： Xiao-Yi Xiao ,  Dinesh V. Patel

发明人： Xiao-Yi Xiao ,  Dinesh V. Patel

IPC分类号： C07D403/12 ,  C07D239/553 ,  A61K31/4155

CPC分类号： C07D487/12 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14

摘要： Disclosed are protein kinase inhibitors of Formula Ia and Ib, compositions comprising such inhibitors, and methods of use, thereof. More particularly, these compounds and compositions are inhibitors of Aurora-A (Aurora-2) and Aurora-B (Aurora-1) protein kinase. Also disclosed are methods of using these compounds and compositions to prevent and treat diseases associated with protein kinases, especially diseases associated with Aurora-A or Aurora-B, such as cancer.

摘要翻译： 公开了式Ia和Ib的蛋白激酶抑制剂，包含这种抑制剂的组合物及其使用方法。 更具体地说，这些化合物和组合物是Aurora-A（Aurora-2）和Aurora-B（Aurora-1）蛋白激酶的抑制剂。 还公开了使用这些化合物和组合物来预防和治疗与蛋白激酶相关疾病，特别是与Aurora-A或Aurora-B相关的疾病如癌症的方法。

公开(公告)号：US07371875B2

公开(公告)日：2008-05-13

申请号：US11077887

申请日：2005-03-11

申请人： Xiao-Yi Xiao ,  Dinesh V. Patel

发明人： Xiao-Yi Xiao ,  Dinesh V. Patel

IPC分类号： A01N43/02 ,  C07D493/00 ,  C07D498/00

CPC分类号： C07D491/048

摘要： Disclosed are compounds that inhibit proteasomic activity in cells. Also disclosed are pharmaceutical compositions comprising such compounds as well as methods to treat conditions, particularly cell proliferative conditions, such as cancer and inflammatory conditions.

公开(公告)号：US20080200485A1

公开(公告)日：2008-08-21

申请号：US11667205

申请日：2005-11-17

申请人： Xiao-Yi Xiao ,  Dinesh V. Patel

发明人： Xiao-Yi Xiao ,  Dinesh V. Patel

IPC分类号： A61K31/506 ,  C07D403/12 ,  A61P35/00

CPC分类号： C07D487/12 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14

摘要： Disclosed are protein kinase inhibitors, compositions comprising such inhibitors, and methods of use, thereof. More particularly, disclosed are inhibitors of Aurora-2 (Aurora-A) protein kinase. Also disclosed are methods of treating diseases associated with protein kinases, especially diseases associated with Aurora-2, such as cancer.

摘要翻译： 公开了蛋白激酶抑制剂，包含这种抑制剂的组合物及其使用方法。 更具体地，公开了Aurora-2（Aurora-A）蛋白激酶的抑制剂。 还公开了治疗与蛋白激酶相关疾病的方法，特别是与Aurora-2相关的疾病，例如癌症。