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1. 发明授权

US07199149B2 Monocyclic and bicyclic lactams as factor Xa inhibitors 有权
标题翻译：单环和双环内酰胺作为因子Xa抑制剂
公开(公告)号：US07199149B2
公开(公告)日：2007-04-03
申请号：US10952397
申请日：2004-09-28
申请人： Wei Han , Jennifer X. Qiao , Zilun Hu
发明人： Wei Han , Jennifer X. Qiao , Zilun Hu
IPC分类号： A61K31/4025 , C07D207/24 , C07D409/12
CPC分类号： C07D409/12 , C07D487/04
摘要： The present application describes monocyclic and bicyclic lactams and derivatives thereof of Formulae Ia–e: wherein one of one of T1 and T2 is carbonyl, thiocarbonyl, or sulfonyl or pharmaceutically acceptable salt forms thereof. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.
摘要翻译：本申请描述了式Ia-e的单环和双环内酰胺及其衍生物：

2. 发明授权

US07157470B2 Sulfonylaminovalerolactams and derivatives thereof as factor Xa inhibitors 有权
标题翻译：磺酰基氨基戊内酰胺及其衍生物作为因子Xa抑制剂
公开(公告)号：US07157470B2
公开(公告)日：2007-01-02
申请号：US10429461
申请日：2003-05-05
申请人： Joanne M. Smallheer , Donald J. Pinto , Shuaige Wang , Jennifer X. Qiao , Wei Han , Zilun Hu
发明人： Joanne M. Smallheer , Donald J. Pinto , Shuaige Wang , Jennifer X. Qiao , Wei Han , Zilun Hu
IPC分类号： A61K31/45 , A61K31/433 , A61K31/4196 , A61K31/405 , A61K31/381 , C07D211/76 , C07D285/12 , C07D249/12 , C07D209/04 , C07D409/00
CPC分类号： C07D409/14 , C07D211/76 , C07D401/10 , C07D401/14 , C07D417/14 , C07D495/04
摘要： The present application describes sulfonylaminovalerolactams and derivatives thereof of Formula I: or pharmaceutically acceptable salt forms thereof, wherein ring G is a mono- or bicyclic carbocycle or heterocycle. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.
摘要翻译：本申请描述了式I的磺酰氨基戊内酰胺及其衍生物：或其药学上可接受的盐形式，其中环G是单环或双环碳环或杂环。本发明的化合物可用作胰蛋白酶样丝氨酸蛋白酶的抑制剂，特别是因子Xa。

3. 发明授权

US07524863B2 Sulfonylaminovalerolactams and derivatives thereof as factor Xa inhibitors 有权
标题翻译：磺酰基氨基戊内酰胺及其衍生物作为因子Xa抑制剂
公开(公告)号：US07524863B2
公开(公告)日：2009-04-28
申请号：US11472825
申请日：2006-06-21
申请人： Joanne M. Smallheer , Donald J. Pinto , Shuaige Wang , Jennifer X. Qiao , Wei Han , Zilun Hu
发明人： Joanne M. Smallheer , Donald J. Pinto , Shuaige Wang , Jennifer X. Qiao , Wei Han , Zilun Hu
IPC分类号： A61K31/45 , A61K31/433 , A61K31/4196 , A61K31/405 , A61K31/381 , C07D211/76 , C07D285/12 , C07D249/12 , C07D209/04 , C07D409/00
CPC分类号： C07D409/14 , C07D211/76 , C07D401/10 , C07D401/14 , C07D417/14 , C07D495/04
摘要： The present application describes sulfonylaminovalerolactams and derivatives thereof of Formula I: or pharmaceutically acceptable salt forms thereof, wherein ring G is a mono- or bicyclic carbocycle or heterocycle. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.
摘要翻译：本申请描述了式I的磺酰氨基戊内酰胺及其衍生物：或其药学上可接受的盐形式，其中环G是单环或双环碳环或杂环。本发明的化合物可用作胰蛋白酶样丝氨酸蛋白酶的抑制剂，特别是因子Xa。

4. 发明申请

US20060247243A1 Sulfonylaminovalerolactams and derivatives thereof as factor Xa inhibitors 有权
公开(公告)号：US20060247243A1
公开(公告)日：2006-11-02
申请号：US11472825
申请日：2006-06-21
申请人： Joanne Smallheer , Donald Pinto , Shuaige Wang , Jennifer Qiao , Wei Han , Zilun Hu
发明人： Joanne Smallheer , Donald Pinto , Shuaige Wang , Jennifer Qiao , Wei Han , Zilun Hu
IPC分类号： A61K31/517 , A61K31/502 , A61K31/498 , A61K31/4709 , A61K31/4015 , C07D403/02
CPC分类号： C07D409/14 , C07D211/76 , C07D401/10 , C07D401/14 , C07D417/14 , C07D495/04
摘要： The present application describes sulfonylaminovalerolactams and derivatives thereof of Formula I: or pharmaceutically acceptable salt forms thereof, wherein ring G is a mono- or bicyclic carbocycle or heterocycle. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.

5. 发明授权

US07169795B2 Sulfonylaminovalerolactams and derivatives thereof as factor Xa inhibitors 有权
标题翻译：磺酰基氨基戊内酰胺及其衍生物作为因子Xa抑制剂
公开(公告)号：US07169795B2
公开(公告)日：2007-01-30
申请号：US10952396
申请日：2004-09-28
申请人： Wei Han , Zilun Hu , Timur Gungor
发明人： Wei Han , Zilun Hu , Timur Gungor
IPC分类号： C07D487/12 , C07D401/04 , C07D403/14 , A61K31/445 , A61P7/02
CPC分类号： C07D401/04 , C07D207/38 , C07D401/10 , C07D401/14 , C07D403/04 , C07D403/10 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D495/04
摘要： The present application describes sulfonylaminovalerolactams and derivatives thereof of Formula Ia–If: or pharmaceutically acceptable salt forms thereof, wherein ring G is a mono- or bicyclic carbocycle or heterocycle. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.
摘要翻译：本申请描述了式Ia-If的磺酰基氨基戊内酰胺及其衍生物：或其药学上可接受的盐形式，其中环G是单环或双环碳环或杂环。本发明的化合物可用作胰蛋白酶样丝氨酸蛋白酶的抑制剂，特别是因子Xa。

6. 发明申请

US20050107361A1 Monocyclic and bicyclic lactams as factor Xa inhibitors 有权
标题翻译：单环和双环内酰胺作为因子Xa抑制剂
公开(公告)号：US20050107361A1
公开(公告)日：2005-05-19
申请号：US10952397
申请日：2004-09-28
申请人： Wei Han , Jennifer Qiao , Zilun Hu
发明人： Wei Han , Jennifer Qiao , Zilun Hu
IPC分类号： A61K20060101 , A61K31/4709 , A61K31/498 , A61K31/502 , A61K31/538 , A61K31/55 , C07D43/02
CPC分类号： C07D409/12 , C07D487/04
摘要： The present application describes monocyclic and bicyclic lactams and derivatives thereof of Formulae Ia-e: wherein one of one of T1 and T2 is carbonyl, thiocarbonyl, or sulfonyl or pharmaceutically acceptable salt forms thereof. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.
摘要翻译：本申请描述了式Ia-e的单环和双环内酰胺及其衍生物：其中T 1和T 2之一的一个是羰基，硫代羰基或磺酰基或药学上其可接受的盐形式。本发明的化合物可用作胰蛋白酶样丝氨酸蛋白酶的抑制剂，特别是因子Xa。

7. 发明授权

US07312218B2 Sulfonylaminovalerolactams and derivatives thereof as factor Xa inhibitors 有权
公开(公告)号：US07312218B2
公开(公告)日：2007-12-25
申请号：US11611195
申请日：2006-12-15
申请人： Wei Han , Zilun Hu , Timur Gungor
发明人： Wei Han , Zilun Hu , Timur Gungor
IPC分类号： C07D241/36 , C07D471/02 , C07D217/06 , C07D401/00 , C07D207/00
CPC分类号： C07D401/04 , C07D207/38 , C07D401/10 , C07D401/14 , C07D403/04 , C07D403/10 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D495/04
摘要： The present application describes sulfonylaminovalerolactams and derivatives thereof of Formula Ia-If: or pharmaceutically acceptable salt forms thereof, wherein ring G is a mono- or bicyclic carbocycle or heterocycle. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.

8. 发明申请

US20070099922A1 SULFONYLAMINOVALEROLACTAMS AND DERIVATIVES THEREOF AS FACTOR XA INHIBITORS 有权
标题翻译：作为因子XA抑制剂的磺酰氨基戊酸酯衍生物及其衍生物
公开(公告)号：US20070099922A1
公开(公告)日：2007-05-03
申请号：US11611195
申请日：2006-12-15
申请人： Wei Han , Zilun Hu , Timur Gungor
发明人： Wei Han , Zilun Hu , Timur Gungor
IPC分类号： A61K31/517 , A61K31/502 , A61K31/498 , A61K31/4709 , A61K31/4015 , C07D403/02
CPC分类号： C07D401/04 , C07D207/38 , C07D401/10 , C07D401/14 , C07D403/04 , C07D403/10 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D495/04
摘要： The present application describes sulfonylaminovalerolactams and derivatives thereof of Formula Ia-If: or pharmaceutically acceptable salt forms thereof, wherein ring G is a mono- or bicyclic carbocycle or heterocycle. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.
摘要翻译：本申请描述了式Ia-If的磺酰氨基戊内酰胺及其衍生物：或其药学上可接受的盐形式，其中环G是单环或双环碳环或杂环。本发明的化合物可用作胰蛋白酶样丝氨酸蛋白酶的抑制剂，特别是因子Xa。

9. 发明申请

US20050096309A1 Sulfonylaminovalerolactams and derivatives thereof as factor Xa inhibitors 有权
标题翻译：磺酰基氨基戊内酰胺及其衍生物作为因子Xa抑制剂
公开(公告)号：US20050096309A1
公开(公告)日：2005-05-05
申请号：US10952396
申请日：2004-09-28
申请人： Wei Han , Zilun Hu , Timur Gungor
发明人： Wei Han , Zilun Hu , Timur Gungor
IPC分类号： A61K20060101 , A61K31/4178 , A61K31/513 , A61K31/55 , A61K31/551 , C07D207/14 , C07D207/38 , C07D215/12 , C07D401/04 , C07D401/10 , C07D401/14 , C07D403/04 , C07D403/10 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D495/04 , C07D43/02
CPC分类号： C07D401/04 , C07D207/38 , C07D401/10 , C07D401/14 , C07D403/04 , C07D403/10 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D495/04
摘要： The present application describes sulfonylaminovalerolactams and derivatives thereof of Formula Ia-If: or pharmaceutically acceptable salt forms thereof, wherein ring G is a mono- or bicyclic carbocycle or heterocycle. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.
摘要翻译：本申请描述了式Ia-If的磺酰基氨基戊内酰胺及其衍生物：或其药学上可接受的盐形式，其中环G是单环或双环碳环或杂环。本发明的化合物可用作胰蛋白酶样丝氨酸蛋白酶的抑制剂，特别是因子Xa。

10. 发明授权

US07507730B2 Substituted pyrazolo[1,5-a]pyrimidines as potassium channel activators 有权
标题翻译：取代的吡唑并[1,5-a]嘧啶作为钾通道激活剂
公开(公告)号：US07507730B2
公开(公告)日：2009-03-24
申请号：US11511154
申请日：2006-08-28
申请人： Wei Han , Zilun Hu
发明人： Wei Han , Zilun Hu
IPC分类号： C07D487/04 , C07D291/06 , A61K31/519 , A61K31/541 , C07D413/12 , A61K31/5355 , A61P25/06 , A61P9/06 , A61P25/08 , A61P1/04 , A61P11/08
CPC分类号： C07D487/04
摘要： Novel heterocyclic dihydropyrimidine compounds useful as inhibitors of potassium channel function (especially inhibitors of the Kv1 subfamily of voltage gated K+ channels, especially inhibitors Kv1.5 which has been linked to the ultra-rapidly activating delayed rectifier, which have the structure stereoisomers including enantiomers thereof and diastereomers thereof, or a pharmaceutically acceptable salt thereof, wherein Q is alkyl, substituted alkyl, cycloalkyl, substituted cycloalkyl, cycloheteroalkyl, substituted cycloheteroalkyl or which is aryl, substituted aryl, heteroaryl or substituted heteroaryl; R3 is wherein R1, R2, R4, R5, R6, R7, R8, R9 and R10 are defined herein. Methods of using such compounds in the prevention and treatment of arrhythmia and IKur-associated conditions, and pharmaceutical compositions containing such compounds are also provided.
摘要翻译：可用作钾通道功能抑制剂的新型杂环二氢嘧啶化合物（特别是电压门控K +通道的Kv1亚家族的抑制剂，特别是与超快速活化延迟整流剂连接的抑制剂Kv1.5，其具有包括其对映异构体的结构立体异构体其中Q是烷基，取代的烷基，环烷基，取代的环烷基，环杂烷基，取代的环杂烷基或芳基，取代的芳基，杂芳基或取代的杂芳基; R3是其中R1，R2，R4， R5，R6，R7，R8，R9和R10如本文所定义。还提供了使用这些化合物预防和治疗心律失常和IKur相关病症的方法，以及含有这些化合物的药物组合物。

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