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1. 发明申请

US20120053175A1 MLK INHIBITORS AND METHODS OF USE 有权
标题翻译： MLK抑制剂和使用方法
公开(公告)号：US20120053175A1
公开(公告)日：2012-03-01
申请号：US13131193
申请日：2009-11-25
申请人： Harris A. Gelbard , Stephen Dewhurst , Val S. Goodfellow , Colin J. Loweth , Torsten Wiemann
发明人： Harris A. Gelbard , Stephen Dewhurst , Val S. Goodfellow , Colin J. Loweth , Torsten Wiemann
IPC分类号： A61K31/5377 , C07D487/04 , A61K31/437 , A61K31/496 , A61P25/24 , A61K31/4985 , A61P25/28 , A61P25/16 , A61P25/00 , A61P27/16 , C07D471/04 , A61K31/506
CPC分类号： A61K31/437 , A61K31/438 , A61K31/444 , A61K31/496 , A61K31/4985 , A61K31/506 , A61K31/5377 , A61K31/553 , A61K45/06 , C07D471/04 , C07D471/10 , C07D487/04 , A61K2300/00
摘要： Provided are compounds having an inhibitory effect on Mixed Lineage Kinases. Also provided are pharmaceutical compositions, methods of preparing the compounds, synthetic intermediates, and methods of using the compounds, independently or in combination with other therapeutic agents, for treating diseases and conditions which are affected by Mixed Lineage Kinase inhibition. Also provided are methods of treatment of neuropsychiatric disorders which comprise the inhibition of Mixed Lineage Kinases.
摘要翻译：提供对混合谱系激酶具有抑制作用的化合物。还提供了药物组合物，制备化合物的方法，合成中间体，以及独立地或与其它治疗剂组合使用化合物的方法，用于治疗受混合谱系激酶抑制影响的疾病和病症。还提供了治疗包含抑制混合谱系激酶的神经精神障碍的方法。

2. 发明授权

US08846909B2 Bicyclic heteroaryl kinase inhibitors and methods of use 有权
标题翻译：双环杂芳基激酶抑制剂和使用方法
公开(公告)号：US08846909B2
公开(公告)日：2014-09-30
申请号：US13698829
申请日：2011-05-24
申请人： Harris A. Gelbard , Stephen Dewhurst , Val S. Goodfellow , Torsten Wiemann , Satheesh Babu Ravula , Colin J. Loweth
发明人： Harris A. Gelbard , Stephen Dewhurst , Val S. Goodfellow , Torsten Wiemann , Satheesh Babu Ravula , Colin J. Loweth
IPC分类号： C07D413/00 , A61K31/44
CPC分类号： A61K31/437 , A61K31/444 , A61K31/496 , A61K31/4985 , A61K31/506 , A61K31/5377 , A61K45/06 , C07D471/04 , C07D487/04 , C07D519/00
摘要： Provided are compounds having an inhibitory effect on kinases including Mixed Lineage Kinases. Also provided are pharmaceutical compositions, methods of preparing the compounds, synthetic intermediates, and methods of using the compounds, independently or in combination with other therapeutic agents, for treating diseases and conditions that are affected by Mixed Lineage Kinase inhibition. Also provided are methods of treatment of neuropsychiatric disorders that comprise the inhibition of Mixed Lineage Kinases.
摘要翻译：提供对对包括混合谱系激酶在内的激酶具有抑制作用的化合物。还提供了药物组合物，制备化合物的方法，合成中间体以及独立地或与其它治疗剂组合使用该化合物的方法，用于治疗受混合谱系激酶抑制影响的疾病和病症。还提供了治疗包含抑制混合谱系激酶的神经精神障碍的方法。

3. 发明申请

US20080200371A1 THIAZOLE AND THIADIAZOLE INHIBITORS OF TYROSINE PHOSPHATASES 审中-公开
标题翻译：酪氨酸磷酸酯的噻唑和噻唑唑抑制剂
公开(公告)号：US20080200371A1
公开(公告)日：2008-08-21
申请号：US12057609
申请日：2008-03-28
申请人： Zacharia S. CHERUVALLATH , Colin J. Loweth , Ruth F. Nutt , Darryl Rideout , Joseph E. Semple , Jing Wang , Feiyue Wu , Shankari Mylvaganam , Hengyi Zhu , Jianzhong Sun
发明人： Zacharia S. CHERUVALLATH , Colin J. Loweth , Ruth F. Nutt , Darryl Rideout , Joseph E. Semple , Jing Wang , Feiyue Wu , Shankari Mylvaganam , Hengyi Zhu , Jianzhong Sun
IPC分类号： A61K31/675 , A61K38/28 , A61P3/04 , A61K31/426 , C07D277/38 , A61K31/433 , C07D285/135 , C07F9/28 , A61P7/12 , A61P9/12
CPC分类号： C07D277/38 , C07D277/42 , C07D285/135 , C07D417/12 , C07D417/14 , C07F9/6539 , C07F9/65395
摘要： Compounds and compositions are provided for modulating the activity of protein tyrosine phosphatases. In one embodiment, the compounds and compositions are thiazoles and thiadiazoles that inhibit the activity of protein tyrosine phosphatase 1B.
摘要翻译：提供化合物和组合物用于调节蛋白酪氨酸磷酸酶的活性。在一个实施方案中，化合物和组合物是抑制蛋白酪氨酸磷酸酶1B活性的噻唑和噻二唑。

4. 发明授权

US07381736B2 Thiazole and thiadiazole inhibitors of tyrosine phosphatases 失效
标题翻译：噻唑和噻二唑抑制剂酪氨酸磷酸酶
公开(公告)号：US07381736B2
公开(公告)日：2008-06-03
申请号：US11219402
申请日：2005-09-02
申请人： Zacharia S. Cheruvallath , Colin J. Loweth , Ruth F. Nutt , Darryl Rideout , Joseph E. Semple , Jing Wang , Feiyue Wu , Shankari Mylvaganam , Hengyi Zhu , Jianzhong Sun
发明人： Zacharia S. Cheruvallath , Colin J. Loweth , Ruth F. Nutt , Darryl Rideout , Joseph E. Semple , Jing Wang , Feiyue Wu , Shankari Mylvaganam , Hengyi Zhu , Jianzhong Sun
IPC分类号： A61K31/427 , C07D277/18
CPC分类号： C07D277/38 , C07D277/42 , C07D285/135 , C07D417/12 , C07D417/14 , C07F9/6539 , C07F9/65395
摘要： Compounds and compositions are provided for modulating the activity of protein tyrosine phosphatases. In one embodiment, the compounds and compositions are thiazoles and thiadiazoles that inhibit the activity of protein tyrosine phosphatase 1B.
摘要翻译：提供化合物和组合物用于调节蛋白酪氨酸磷酸酶的活性。在一个实施方案中，化合物和组合物是抑制蛋白酪氨酸磷酸酶1B活性的噻唑和噻二唑。

5. 发明申请

US20150105401A1 MLK INHIBITORS AND METHODS OF USE 有权
标题翻译： MLK抑制剂和使用方法
公开(公告)号：US20150105401A1
公开(公告)日：2015-04-16
申请号：US14508566
申请日：2014-10-07
申请人： Harris A. Gelbard , Stephen Dewhurst , Val S. Goodfellow , Colin J. Loweth , Torsten Wiemann
发明人： Harris A. Gelbard , Stephen Dewhurst , Val S. Goodfellow , Colin J. Loweth , Torsten Wiemann
IPC分类号： C07D471/04
CPC分类号： A61K31/437 , A61K31/438 , A61K31/444 , A61K31/496 , A61K31/4985 , A61K31/506 , A61K31/5377 , A61K31/553 , A61K45/06 , C07D471/04 , C07D471/10 , C07D487/04 , A61K2300/00
摘要： Provided are compounds having an inhibitory effect on Mixed Lineage Kinases. Also provided are pharmaceutical compositions, methods of preparing the compounds, synthetic intermediates, and methods of using the compounds, independently or in combination with other therapeutic agents, for treating diseases and conditions which are affected by Mixed Lineage Kinase inhibition. Also provided are methods of treatment of neuropsychiatric disorders which comprise the inhibition of Mixed Lineage Kinases.
摘要翻译：提供对混合谱系激酶具有抑制作用的化合物。还提供了药物组合物，制备化合物的方法，合成中间体，以及独立地或与其它治疗剂组合使用化合物的方法，用于治疗受混合谱系激酶抑制影响的疾病和病症。还提供了治疗包含抑制混合谱系激酶的神经精神障碍的方法。

6. 发明申请

US20130203755A1 BICYCLIC HETEROARYL KINASE INHIBITORS AND METHODS OF USE 有权
标题翻译：双相异氟醚激酶抑制剂及其使用方法
公开(公告)号：US20130203755A1
公开(公告)日：2013-08-08
申请号：US13698829
申请日：2011-05-24
申请人： Harris A. Gelbard , Stephen Dewhurst , Val S. Goodfellow , Torsten Wiemann , Satheesh Babu Ravula , Colin J. Loweth
发明人： Harris A. Gelbard , Stephen Dewhurst , Val S. Goodfellow , Torsten Wiemann , Satheesh Babu Ravula , Colin J. Loweth
IPC分类号： A61K31/437 , A61K31/444 , A61K31/496 , A61K45/06 , C07D487/04 , A61K31/4985 , A61K31/5377 , C07D471/04 , A61K31/506
CPC分类号： A61K31/437 , A61K31/444 , A61K31/496 , A61K31/4985 , A61K31/506 , A61K31/5377 , A61K45/06 , C07D471/04 , C07D487/04 , C07D519/00
摘要： Provided are compounds having an inhibitory effect on kinases including Mixed Lineage Kinases. Also provided are pharmaceutical compositions, methods of preparing the compounds, synthetic intermediates, and methods of using the compounds, independently or in combination with other therapeutic agents, for treating diseases and conditions that are affected by Mixed Lineage Kinase inhibition. Also provided are methods of treatment of neuropsychiatric disorders that comprise the inhibition of Mixed Lineage Kinases.
摘要翻译：提供对对包括混合谱系激酶在内的激酶具有抑制作用的化合物。还提供了药物组合物，制备化合物的方法，合成中间体以及独立地或与其它治疗剂组合使用该化合物的方法，用于治疗受混合谱系激酶抑制影响的疾病和病症。还提供了治疗包含抑制混合谱系激酶的神经精神障碍的方法。

7. 发明申请

US20090156509A1 Tri-peptide Inhibitors of Serine Elastases 审中-公开
标题翻译：丝氨酸弹性蛋白酶的三肽抑制剂
公开(公告)号：US20090156509A1
公开(公告)日：2009-06-18
申请号：US12326612
申请日：2008-12-02
申请人： John C. Cheronis , Val Goodfellow , Colin J. Loweth , Shamsi Raeissi
发明人： John C. Cheronis , Val Goodfellow , Colin J. Loweth , Shamsi Raeissi
IPC分类号： A61K38/06 , C07K5/097
CPC分类号： C07K5/06052 , A61K38/00 , C07K5/021
摘要： The present invention provides compounds of formula (I): where X is R1—(CR3R4)nOC(O)—; R1—(CR3R4)nC(O)—; R1—C(O)NH(CR3R4)nOC(O)—; R1—C(O)NH(CR3R4)nC(O)—; R1—C(O)(CR3R4)nOC(O)—; or R1—C(O)(CR3R4)nC(O)—; where R1 is optionally substituted C5-10 aryl or heteroaryl; OH or NH2; where R3 and R4 are independently H or methyl; and n is 0 to 6; and Y is —CF3 or one of: where R2 is C1-8 alkyl optionally substituted with halo or —OH; —(CR6R7)p—C5-6 aryl optionally substituted with halo, —OH, C1-8 alkyl, C1-8 haloalkyl, —(CH2)mC(O)NH2 or —(CH2)mOCH3; where R6 and R7 are independently H or methyl; m is 0 to 4, and p is 0 or 1 or a pharmaceutically acceptable salt, ester, metabolite or prodrug thereof
摘要翻译：本发明提供式（I）化合物：其中X为R1-（CR3R4）nOC（O） - ; R1-（CR3R4）nC（O） - ; R1-C（O）NH（CR3R4）nOC（O） - ; R1-C（O）NH（CR3R4）nC（O） - ; R1-C（O）（CR3R4）nOC（O） - ; 或R 1 -C（O）（CR 3 R 4）n C（O） - ; 其中R 1是任选取代的C 5-10芳基或杂芳基; OH或NH2; 其中R3和R4独立地是H或甲基; n为0〜6; 并且Y是-CF 3或其中R 2是任选被卤素或-OH取代的C 1-8烷基之一; -OH，C 1-8烷基，C 1-8卤代烷基， - （CH 2）m C（O）NH 2或 - （CH 2）m OCH 3） - （CR 6 R 7）其中R 6和R 7独立地为H或甲基; m为0至4，p为0或1或其药学上可接受的盐，酯，代谢物或前药

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