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1. 发明申请

US20100216767A1 QUINAZOLINES FOR PDK1 INHIBITION 审中-公开
标题翻译：用于PDK1抑制剂的喹唑啉
公开(公告)号：US20100216767A1
公开(公告)日：2010-08-26
申请号：US12448390
申请日：2007-12-20
申请人： Mina Aikawa , Payman Amiri , Steven Bashman , Jeffrey Dove , Rama Jain , Xiaodong Lin , Jeremy Murray , Savithri Ramurthy , Alice Rico , Wei Shu , Sharadha Subramanian , Xiaojing Michael Wang , Robert L. Warne , Yasheen Zhou
发明人： Mina Aikawa , Payman Amiri , Steven Bashman , Jeffrey Dove , Rama Jain , Xiaodong Lin , Jeremy Murray , Savithri Ramurthy , Alice Rico , Wei Shu , Sharadha Subramanian , Xiaojing Michael Wang , Robert L. Warne , Yasheen Zhou
IPC分类号： A61K31/337 , C07D239/84 , A61K31/517 , C07D401/12 , A61K31/496 , C07D403/10 , C07D413/10 , A61K31/5377 , C07D413/14 , C07D403/12 , A61P35/00
CPC分类号： C07D239/84 , C07D401/08 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/12 , C07D411/04 , C07D413/12 , C07D413/14 , C07D417/04 , C07D417/14
摘要： The invention provides novel compounds that are inhibitors of PDK1. Also provided are pharmaceutical compositions including the compounds, and methods of treating proliferative diseases, such as cancers, with the compounds or compositions.
摘要翻译：本发明提供了作为PDK1抑制剂的新型化合物。还提供了包含该化合物的药物组合物，以及用化合物或组合物治疗增殖性疾病如癌症的方法。

2. 发明授权

US07932262B2 Quinazolines for PDK1 inhibition 失效
标题翻译：喹唑啉用于PDK1抑制
公开(公告)号：US07932262B2
公开(公告)日：2011-04-26
申请号：US12295967
申请日：2007-04-05
申请人： Savithri Ramurthy , Xiaodong Lin , Sharadha Subramanian , Alice Rico , Xiaojong M. Wang , Rama Jain , Jeremy M. Murray , Stephen E. Basham , Robert L. Warne , Wei Shu , Yasheen Zhou , Jeffrey Dove , Mina Aikawa , Payman Amiri , Weibo Wang , Johanna M. Jansen , Allan S. Wagman , Keith B. Pfister , Simon Ng
发明人： Savithri Ramurthy , Xiaodong Lin , Sharadha Subramanian , Alice Rico , Xiaojong M. Wang , Rama Jain , Jeremy M. Murray , Stephen E. Basham , Robert L. Warne , Wei Shu , Yasheen Zhou , Jeffrey Dove , Mina Aikawa , Payman Amiri , Weibo Wang , Johanna M. Jansen , Allan S. Wagman , Keith B. Pfister , Simon Ng
IPC分类号： A61K31/517
CPC分类号： C07D239/94 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/10 , C07D403/12 , C07D403/14 , C07D405/04 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/04 , C07D417/06 , C07D417/14 , C07D451/06 , C07D453/02
摘要： The invention provides quinazoline compounds that are inhibitors of PDK1. Also provided are pharmaceutical compositions including the compounds, and methods of treating proliferative diseases, such as cancers, with the compounds or compositions.
摘要翻译：本发明提供作为PDK1抑制剂的喹唑啉化合物。还提供了包含该化合物的药物组合物，以及用化合物或组合物治疗增殖性疾病如癌症的方法。

3. 发明申请

US20100048561A1 QUINAZOLINES FOR PDK1 INHIBITION 失效
标题翻译：用于PDK1抑制剂的喹唑啉
公开(公告)号：US20100048561A1
公开(公告)日：2010-02-25
申请号：US12295967
申请日：2007-04-05
申请人： Savithri Ramurthy , Xiaodong Lin , Sharadha Subramanian , Alice C. Rico , Xiaojing M. Wang , Rama Jain , Jeremy M. Murray , Steven E. Basham , Robert L. Warne , Wei Shu , Yasheen Zhou , Jeffrey Dove , Mina Aikawa , Payman Amiri , Weibo Wang , Johanna M. Jansen , Allan S. Wagman , Keith B. Pfister , Simon Ng
发明人： Savithri Ramurthy , Xiaodong Lin , Sharadha Subramanian , Alice C. Rico , Xiaojing M. Wang , Rama Jain , Jeremy M. Murray , Steven E. Basham , Robert L. Warne , Wei Shu , Yasheen Zhou , Jeffrey Dove , Mina Aikawa , Payman Amiri , Weibo Wang , Johanna M. Jansen , Allan S. Wagman , Keith B. Pfister , Simon Ng
IPC分类号： A61K31/517 , C07D401/12 , C07D401/14 , C07D239/84 , C07D413/14 , A61K31/5377 , A61P35/00
CPC分类号： C07D239/94 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/10 , C07D403/12 , C07D403/14 , C07D405/04 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/04 , C07D417/06 , C07D417/14 , C07D451/06 , C07D453/02
摘要： The invention provides quinazoline compounds that are inhibitors of PDK1. Also provided are pharmaceutical compositions including the compounds, and methods of treating proliferative diseases, such as cancers, with the compounds or compositions.
摘要翻译：本发明提供作为PDK1抑制剂的喹唑啉化合物。还提供了包含该化合物的药物组合物，以及用化合物或组合物治疗增殖性疾病如癌症的方法。

4. 发明授权

US5605932A Opiate receptor ligands 失效
标题翻译：鸦片剂受体配体
公开(公告)号：US5605932A
公开(公告)日：1997-02-25
申请号：US582156
申请日：1996-01-02
申请人： Simon Ng , Robert L. Warne , Ronald N. Zuckermann , Eric J. Martin , Reyna J. Simon
发明人： Simon Ng , Robert L. Warne , Ronald N. Zuckermann , Eric J. Martin , Reyna J. Simon
IPC分类号： C07C271/24 , C07C323/32 , A61K31/185
CPC分类号： C07C271/24 , C07C323/32 , C07C2102/42
摘要： Compounds of Formula 1 bind opioid receptors: which binds to the opioid receptor: ##STR1##
摘要翻译：式1的化合物结合阿片受体：其结合阿片受体：

5. 发明授权

US5567602A Recombinant production of chymase 失效
标题翻译：重组生产糜酶
公开(公告)号：US5567602A
公开(公告)日：1996-10-22
申请号：US929198
申请日：1992-08-12
申请人： James M. Clark , Kevin R. Shoemaker , Robert L. Warne
发明人： James M. Clark , Kevin R. Shoemaker , Robert L. Warne
IPC分类号： C12N9/64 , C12N15/57 , C12N15/62 , C12N15/09 , C12N15/10
CPC分类号： C12N9/6483 , C12N15/62 , C12Y304/23004 , C07K2319/00 , C07K2319/02 , C07K2319/23 , C07K2319/43 , C07K2319/50
摘要： The instant invention is directed to recombinant production of functionally active chymase. "Functionally active" as used herein refers to the ability to exhibit one or more functional activities of a full-length wild-type chymase protein. In a preferred aspect, a proteolytically inactive chymase fusion protein comprising a functionally active portion of a non-chymase protein joined to the amino-terminus of the chymase protein is produced, which, upon cleavage away of the non-chymase fusion protein portion, becomes proteolytically active. A refolding procedure for increasing yields of proteolytically active recombinant chymase is provided. The invention is further directed to use of the recombinant chymase thus produced for preparing chymase-specific antibodies.
摘要翻译：本发明涉及功能活性胃促胰酶的重组生产。本文所用的“功能活性”是指展示全长野生型胃促胰酶抑制蛋白的一种或多种功能活性的能力。在优选的方面，产生包含与食糜酶蛋白的氨基末端连接的非食糜酶蛋白质的功能活性部分的蛋白水解无活性的糜酶融合蛋白，其在非食糜酶融合蛋白部分切除时变为蛋白水解活性。提供了提高蛋白水解活性重组糜酶产量的重折叠方法。本发明还涉及使用由此产生的用于制备胃促胰酶特异性抗体的重组胃促胰酶。

6. 发明授权

US06924122B2 Protease regulator screening assay 有权
标题翻译：蛋白酶调节剂筛选试验
公开(公告)号：US06924122B2
公开(公告)日：2005-08-02
申请号：US10225390
申请日：2002-08-20
申请人： David Y. Chien , Mark J. Selby , Kevin Shoemaker , Robert L. Warne
发明人： David Y. Chien , Mark J. Selby , Kevin Shoemaker , Robert L. Warne
IPC分类号： C07K14/18 , C12Q1/02 , C12Q1/37 , A61K38/24 , C07K1/00 , C12N15/00 , C12P21/06
CPC分类号： C07K14/005 , C12N2770/24222 , C12Q1/025 , C12Q1/37 , G01N2333/18 , G01N2500/00
摘要： A polypeptide containing an anchor region, a protease recognition site, and a detectable signal region can be produced recombinantly and directly attached to a solid support. The polypeptide is useful for screening protease regulators, especially protease inhibitors.
摘要翻译：包含锚定区，蛋白酶识别位点和可检测信号区的多肽可以重组并直接连接到固体支持物上。该多肽可用于筛选蛋白酶调节剂，特别是蛋白酶抑制剂。

7. 发明授权

US07439040B2 Protease regulator screening assay 有权
标题翻译：蛋白酶调节剂筛选试验
公开(公告)号：US07439040B2
公开(公告)日：2008-10-21
申请号：US11193615
申请日：2005-08-01
申请人： David Y. Chien , Mark J. Selby , Kevin Shoemaker , Robert L. Warne
发明人： David Y. Chien , Mark J. Selby , Kevin Shoemaker , Robert L. Warne
IPC分类号： C07K1/00 , C07K14/00 , A61K39/24
CPC分类号： C07K14/005 , C12N2770/24222 , C12Q1/025 , C12Q1/37 , G01N2333/18 , G01N2500/00
摘要： A polypeptide containing an anchor region, a protease recognition site, and a detectable signal region can be produced recombinantly and directly attached to a solid support. The polypeptide is useful for screening protease regulators, especially protease inhibitors.
摘要翻译：包含锚定区，蛋白酶识别位点和可检测信号区的多肽可以重组并直接连接到固体支持物上。该多肽可用于筛选蛋白酶调节剂，特别是蛋白酶抑制剂。

8. 发明授权

US5481020A Opiate receptor ligands 失效
标题翻译：鸦片剂受体配体
公开(公告)号：US5481020A
公开(公告)日：1996-01-02
申请号：US366830
申请日：1994-12-30
申请人： Simon Ng , Robert L. Warne , Ronald N. Zuckermann , Eric J. Martin , Reyna J. Simon
发明人： Simon Ng , Robert L. Warne , Ronald N. Zuckermann , Eric J. Martin , Reyna J. Simon
IPC分类号： C07C271/24 , C07C323/32 , C07C271/10
CPC分类号： C07C271/24 , C07C323/32 , C07C2102/42
摘要： Compounds of Formula 1 bind opioid receptors: which binds to the opioid receptor: ##STR1##
摘要翻译：式1的化合物结合阿片受体：其结合阿片受体：

9. 发明授权

US06436666B1 Protease regulator screening assay 失效
标题翻译：蛋白酶调节剂筛选试验
公开(公告)号：US06436666B1
公开(公告)日：2002-08-20
申请号：US08997055
申请日：1997-10-17
申请人： David Y. Chien , Mark J. Selby , Kevin Shoemaker , Robert L. Warne
发明人： David Y. Chien , Mark J. Selby , Kevin Shoemaker , Robert L. Warne
IPC分类号： C12P2106
CPC分类号： C07K14/005 , C12N2770/24222 , C12Q1/025 , C12Q1/37 , G01N2333/18 , G01N2500/00
摘要： A polypeptide containing an anchor region, a protease recognition site, and a detectable signal region can be produced recombinantly and directly attached to a solid support. The polypeptide is useful for screening protease regulators, especially protease inhibitors.
摘要翻译：包含锚定区，蛋白酶识别位点和可检测信号区的多肽可以重组并直接连接到固体支持物上。该多肽可用于筛选蛋白酶调节剂，特别是蛋白酶抑制剂。

10. 发明授权

US5536868A Opiate receptor ligands 失效
标题翻译：鸦片剂受体配体
公开(公告)号：US5536868A
公开(公告)日：1996-07-16
申请号：US391132
申请日：1995-02-21
申请人： Simon Ng , Robert L. Warne , Ronald N. Zuckermann , Eric J. Martin , Reyna J. Simon
发明人： Simon Ng , Robert L. Warne , Ronald N. Zuckermann , Eric J. Martin , Reyna J. Simon
IPC分类号： C07C271/24 , C07C323/32 , C07C205/05 , C07C229/04 , C07C271/10
CPC分类号： C07C271/24 , C07C323/32 , C07C2102/42
摘要： Compounds of Formula 1 bind to the opioid receptors: ##STR1## wherein R.sub.1 is a group of the formula ##STR2## where W is --(CH.sub.2).sub.a -- (where a is 0, 1, or 2), --O--, --NH--, --S--, --SO--, or --SO.sub.2 --, and Ar is phenyl, phenyl-alkyl, phenyl substituted with 1-3 halo, nitro, lower alkyl, hydroxy, amino, alkylamino, dialkylamino, and/or hydroxy-lower alkyl groups, and n is 0, 1, 2, 3, or 4;R.sub.2 and R.sub.3 are each independently H, lower alkyl, or ##STR3## where X is H, OH, lower alkyl, or lower alkoxy, and p is 0, 1, 2, or 3; R.sub.4 is ##STR4## where m is 0, 1, 2, or 3, and R is 1-3 halo, nitro, lower alkyl, hydroxy, amino, alkylamino, dialkylamino, and/or hydroxy-lower alkyl groups;R.sub.5 is cycloalkyl, bicycloalkyl, or tricycloalkyl; andR.sub.6, R.sub.7, R.sub.8, and R.sub.9 are each independently H or lower alkyl.
摘要翻译：式1的化合物与阿片受体结合：其中R 1是下式的基团：其中W是 - （CH 2）a - （其中a是0,1或2），-O-， - NH - ， - S - ， - SO-或-SO 2 - ，Ar是苯基，苯基 - 烷基，被1-3个卤素，硝基，低级烷基，羟基，氨基，烷基氨基，二烷基氨基和/或羟基 - 低级烷基，n为0,1,2,3或4; R 2和R 3各自独立地为H，低级烷基或者其中X为H，OH，低级烷基或低级烷氧基，p为0,1,2或3; R4是，其中m是0,1,2或3，R是1-3个卤素，硝基，低级烷基，羟基，氨基，烷基氨基，二烷基氨基和/或羟基 - 低级烷基; R5是环烷基，双环烷基或三环烷基; 并且R 6，R 7，R 8和R 9各自独立地为H或低级烷基。

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