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1. 发明申请

US20090203690A1 5-SUBSTITUTED INDAZOLES AS KINASE INHIBITORS 有权
标题翻译：作为激素抑制剂的5-取代的吲哚美辛
公开(公告)号：US20090203690A1
公开(公告)日：2009-08-13
申请号：US12327991
申请日：2008-12-04
申请人： Irini Akritopoulou-Zanze , Brian D. Wakefield , Helmut Mack , Sean C. Turner , Alan F. Gasiecki , Vijaya J. Gracias , Kathy A. Sarris , Douglas M. Kalvin , Melissa J. Michmerhuizen , Qi Shuai , Jyoti R. Patel , Margaretha H.M. Bakker , Nicole Teusch , Eric F. Johnson , Peter J. Kovar , Stevan W. Djuric , Andrew J. Long , Anil Vasudevan , Dawn George , Lu Wang , Biqin Li , N. St. John Moore , Adrian D. Hobson , Keith W. Woods , Julie M. Miyashiro , Steven L. Swann, JR. , Thomas D. Penning
发明人： Irini Akritopoulou-Zanze , Brian D. Wakefield , Helmut Mack , Sean C. Turner , Alan F. Gasiecki , Vijaya J. Gracias , Kathy A. Sarris , Douglas M. Kalvin , Melissa J. Michmerhuizen , Qi Shuai , Jyoti R. Patel , Margaretha H.M. Bakker , Nicole Teusch , Eric F. Johnson , Peter J. Kovar , Stevan W. Djuric , Andrew J. Long , Anil Vasudevan , Dawn George , Lu Wang , Biqin Li , N. St. John Moore , Adrian D. Hobson , Keith W. Woods , Julie M. Miyashiro , Steven L. Swann, JR. , Thomas D. Penning
IPC分类号： A61K31/5377 , C07D403/04 , A61K31/4192 , C07D413/14 , C12N9/99 , A61P25/28 , A61P35/00
CPC分类号： C07D413/04 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/04 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/04 , C07D417/14 , C07D471/04 , C07D487/04 , C07D513/04
摘要： The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein A, R1, R2, R3 and m, are defined in the description. The present invention relates also to methods of making said compounds, and compositions containing said compounds which are useful for inhibiting kinases such as Glycogen Synthase kinase 3 (GSK-3), Rho kinase (ROCK), Janus Kinases (JAK), Cdc7, AKT, PAK4, PLK, CK2, KDR, MK2, JNK1, aurora, pim 1 and nek 2.
摘要翻译：本发明涉及式（I）化合物或其药学上可接受的盐，其中A，R 1，R 2，R 3和m在说明书中定义。本发明还涉及制备所述化合物的方法和含有所述化合物的组合物，其可用于抑制激酶例如糖原合成酶激酶3（GSK-3），Rho激酶（ROCK），Janus激酶（JAK），Cdc7，AKT ，PAK4，PLK，CK2，KDR，MK2，JNK1，极光，pim1和nek2。

2. 发明授权

US08648069B2 5-substituted indazoles as kinase inhibitors 有权
标题翻译： 5-取代的吲唑作为激酶抑制剂
公开(公告)号：US08648069B2
公开(公告)日：2014-02-11
申请号：US12327991
申请日：2008-12-04
申请人： Irini Akritopoulou-Zanze , Brian D. Wakefield , Helmut Mack , Sean C. Turner , Alan F. Gasiecki , Vijaya J. Gracias , Kathy A. Sarris , Douglas M. Kalvin , Melissa J. Michmerhuizen , Qi Shuai , Jyoti R. Patel , Margaretha Bakker , Nicole Teusch , Eric F. Johnson , Peter J. Kovar , Stevan W. Djuric , Andrew J. Long , Anil Vasudevan , Dawn George , Lu Wang , Biqin Li , N. St. John Moore , Adrian D. Hobson , Keith W. Woods , Julie M. Miyashiro , Steven L. Swann, Jr. , Thomas D. Penning
发明人： Irini Akritopoulou-Zanze , Brian D. Wakefield , Helmut Mack , Sean C. Turner , Alan F. Gasiecki , Vijaya J. Gracias , Kathy A. Sarris , Douglas M. Kalvin , Melissa J. Michmerhuizen , Qi Shuai , Jyoti R. Patel , Margaretha Bakker , Nicole Teusch , Eric F. Johnson , Peter J. Kovar , Stevan W. Djuric , Andrew J. Long , Anil Vasudevan , Dawn George , Lu Wang , Biqin Li , N. St. John Moore , Adrian D. Hobson , Keith W. Woods , Julie M. Miyashiro , Steven L. Swann, Jr. , Thomas D. Penning
IPC分类号： A61K31/541 , A61K31/5377 , A61K31/496 , A61K31/454 , A61K31/4192 , C07D417/14 , C07D405/14 , C07D401/14 , C07D403/04 , C07D403/14
CPC分类号： C07D413/04 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/04 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/04 , C07D417/14 , C07D471/04 , C07D487/04 , C07D513/04
摘要： The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein A, R1, R2, R3 and m, are defined in the description. The present invention relates also to methods of making said compounds, and compositions containing said compounds which are useful for inhibiting kinases such as Glycogen Synthase kinase 3 (GSK-3), Rho kinase (ROCK), Janus Kinases (JAK), Cdc7, AKT, PAK4, PLK, CK2, KDR, MK2, JNK1, aurora, pim 1 and nek 2.
摘要翻译：本发明涉及式（I）化合物或其药学上可接受的盐，其中A，R 1，R 2，R 3和m在说明书中定义。本发明还涉及制备所述化合物的方法和含有所述化合物的组合物，其可用于抑制激酶例如糖原合成酶激酶3（GSK-3），Rho激酶（ROCK），Janus激酶（JAK），Cdc7，AKT ，PAK4，PLK，CK2，KDR，MK2，JNK1，极光，pim1和nek2。

3. 发明申请

US20090022732A1 Crystal of a cytochrome-ligand complex and methods of use 失效
标题翻译：细胞色素 - 配体复合物的晶体和使用方法
公开(公告)号：US20090022732A1
公开(公告)日：2009-01-22
申请号：US11445018
申请日：2006-06-01
申请人： Eric F. Johnson , Jason K. Yano
发明人： Eric F. Johnson , Jason K. Yano
IPC分类号： A61K39/395 , C12N9/99 , A61K31/4436 , C12N9/02 , G06T15/00 , G06G7/58 , A61P25/34 , A61K31/444
CPC分类号： C12N9/0077 , C07K2299/00 , Y02A90/26
摘要： The teachings relates to the three-dimensional structure of a crystal of a cytochrome protein complexed with a ligand. The three-dimensional structure of four cytochrome P450 2A6-ligand complexes are disclosed. Cytochrome P450 2A6-ligand crystal structures, wherein the ligand is an inhibitor molecule, are useful for providing structural information that may be integrated into drug screening and drug design processes. Thus, the teachings also relate to methods for utilizing a crystal structure of a cytochrome P450 2A6-ligand complex for identifying, designing, selecting, or testing inhibitors of the cytochrome protein. Such inhibitors are useful as therapeutics for the treatment or modulation of i) diseases; ii) disease symptoms; or iii) the effect of other physiological events mediated by the cytochrome.
摘要翻译：该教导涉及与配体络合的细胞色素蛋白的晶体的三维结构。公开了四种细胞色素P450 2A6-配体复合物的三维结构。细胞色素P450 2A6-配体晶体结构，其中配体是抑制剂分子，可用于提供可被整合到药物筛选和药物设计过程中的结构信息。因此，该教导还涉及利用细胞色素P450 2A6-配体复合物的晶体结构鉴定，设计，选择或测试细胞色素蛋白抑制剂的方法。这种抑制剂可用作治疗或调节i）疾病的治疗剂; ii）疾病症状; 或iii）由细胞色素介导的其他生理事件的影响。

4. 发明申请

US20100160444A1 METHOD TO INHIBIT ISCHEMIA AND REPERFUSION INJURY 有权
标题翻译：抑制ISHEMIA和REPERFUSION INJURY伤害的方法
公开(公告)号：US20100160444A1
公开(公告)日：2010-06-24
申请号：US12612350
申请日：2009-11-04
申请人： Roberta Gottlieb , Paul Wentworth , Eric F. Johnson , Mark J. Yeager , David Granville
发明人： Roberta Gottlieb , Paul Wentworth , Eric F. Johnson , Mark J. Yeager , David Granville
IPC分类号： A61K31/165 , A61P9/00 , A61P9/10
CPC分类号： A61K31/405 , A61K31/415 , A61K31/4164 , A61K31/4174 , A61K31/42 , A61K31/444 , A61K31/455 , A61K31/496 , A61K31/505 , A61K31/538 , A61K31/5415 , A61K31/5513 , A61K31/554 , A61K31/60 , A61K45/06
摘要： Methods of treating or inhibiting ischemia and reperfusion injury are provided.
摘要翻译：提供治疗或抑制缺血和再灌注损伤的方法。

5. 发明授权

US07953557B2 Crystal of a cytochrome-ligand complex and methods of use 失效
标题翻译：细胞色素 - 配体复合物的晶体和使用方法
公开(公告)号：US07953557B2
公开(公告)日：2011-05-31
申请号：US11445018
申请日：2006-06-01
申请人： Eric F. Johnson , Jason K. Yano
发明人： Eric F. Johnson , Jason K. Yano
IPC分类号： G01N33/48 , G01N31/00 , G06G7/58 , G01N33/53
CPC分类号： C12N9/0077 , C07K2299/00 , Y02A90/26
摘要： The teachings relates to the three-dimensional structure of a crystal of a cytochrome protein complexed with a ligand. The three-dimensional structure of four cytochrome P450 2A6-ligand complexes are disclosed. Cytochrome P450 2A6-ligand crystal structures, wherein the ligand is an inhibitor molecule, are useful for providing structural information that may be integrated into drug screening and drug design processes. Thus, the teachings also relate to methods for utilizing a crystal structure of a cytochrome P450 2A6-ligand complex for identifying, designing, selecting, or testing inhibitors of the cytochrome protein. Such inhibitors are useful as therapeutics for the treatment or modulation of i) diseases; ii) disease symptoms; or iii) the effect of other physiological events mediated by the cytochrome.
摘要翻译：该教导涉及与配体络合的细胞色素蛋白的晶体的三维结构。公开了四种细胞色素P450 2A6-配体复合物的三维结构。细胞色素P450 2A6-配体晶体结构，其中配体是抑制剂分子，可用于提供可被整合到药物筛选和药物设计过程中的结构信息。因此，该教导还涉及用于鉴定，设计，选择或测试细胞色素蛋白抑制剂的细胞色素P450 2A6-配体复合物的晶体结构的方法。这种抑制剂可用作治疗或调节i）疾病的治疗剂; ii）疾病症状; 或iii）由细胞色素介导的其他生理事件的影响。

6. 发明授权

US08759402B2 Method to inhibit ischemia and reperfusion injury 有权
标题翻译：抑制缺血和再灌注损伤的方法
公开(公告)号：US08759402B2
公开(公告)日：2014-06-24
申请号：US12612350
申请日：2009-11-04
申请人： Roberta Gottlieb , Paul Wentworth , Eric F. Johnson , Mark J Yeager , David Granville
发明人： Roberta Gottlieb , Paul Wentworth , Eric F. Johnson , Mark J Yeager , David Granville
IPC分类号： A01N37/18 , A61K31/16 , A01N43/62 , A61K31/55
CPC分类号： A61K31/405 , A61K31/415 , A61K31/4164 , A61K31/4174 , A61K31/42 , A61K31/444 , A61K31/455 , A61K31/496 , A61K31/505 , A61K31/538 , A61K31/5415 , A61K31/5513 , A61K31/554 , A61K31/60 , A61K45/06
摘要： Methods of treating or inhibiting ischemia and reperfusion injury are provided.
摘要翻译：提供治疗或抑制缺血和再灌注损伤的方法。

7. 发明授权

US08076457B2 Crystal of a cytochrome-ligand complex and methods of use 失效
公开(公告)号：US08076457B2
公开(公告)日：2011-12-13
申请号：US13117470
申请日：2011-05-27
申请人： Eric F. Johnson , Jason K. Yano
发明人： Eric F. Johnson , Jason K. Yano
IPC分类号： G01N33/48 , G01N31/00 , G06G7/58 , G01N33/53 , C07K1/00
CPC分类号： C12N9/0077 , C07K2299/00 , Y02A90/26
摘要： The teachings relates to the three-dimensional structure of a crystal of a cytochrome protein complexed with a ligand. The three-dimensional structure of four cytochrome P450 2A6-ligand complexes are disclosed. Cytochrome P450 2A6-ligand crystal structures, wherein the ligand is an inhibitor molecule, are useful for providing structural information that may be integrated into drug screening and drug design processes. Thus, the teachings also relate to methods for utilizing a crystal structure of a cytochrome P450 2A6-ligand complex for identifying, designing, selecting, or testing inhibitors of the cytochrome protein. Such inhibitors are useful as therapeutics for the treatment or modulation of i) diseases; ii) disease symptoms; or iii) the effect of other physiological events mediated by the cytochrome.

8. 发明授权

US07615548B2 Method to inhibit ischemia and reperfusion injury 失效
标题翻译：抑制缺血和再灌注损伤的方法
公开(公告)号：US07615548B2
公开(公告)日：2009-11-10
申请号：US11030717
申请日：2005-01-06
申请人： Roberta Gottlieb , Paul Wentworth , Eric F. Johnson , Mark J. Yeager , David Granville
发明人： Roberta Gottlieb , Paul Wentworth , Eric F. Johnson , Mark J. Yeager , David Granville
IPC分类号： C11D7/26 , C11D3/00
CPC分类号： A61K31/405 , A61K31/415 , A61K31/4164 , A61K31/4174 , A61K31/42 , A61K31/444 , A61K31/455 , A61K31/496 , A61K31/505 , A61K31/538 , A61K31/5415 , A61K31/5513 , A61K31/554 , A61K31/60 , A61K45/06
摘要： Methods of treating or inhibiting ischemia and reperfusion injury are provided.
摘要翻译：提供治疗或抑制缺血和再灌注损伤的方法。

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