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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。
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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。
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公开(公告)号：US20120053175A1
公开(公告)日：2012-03-01
申请号：US13131193
申请日：2009-11-25
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。
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公开(公告)号：US20150105401A1
公开(公告)日：2015-04-16
申请号：US14508566
申请日：2014-10-07
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。
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![Substituted pyrrolo[2,3-B]pyridines as MLK inhibitors](/abs-image/US/2014/11/04/US08877772B2/abs.jpg.150x150.jpg)
公开(公告)号：US08877772B2
公开(公告)日：2014-11-04
申请号：US13131193
申请日：2009-11-25
IPC分类号： A61K31/437 , C07D471/04 , C07D487/04 , A61K45/06
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, having a structural Formula, 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： 提供具有结构式的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。
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公开(公告)号：US6004933A
公开(公告)日：1999-12-21
申请号：US065258
申请日：1998-04-23
申请人： Lyle W. Spruce , Albert C. Gyorkos , John C. Cheronis , Val S. Goodfellow , Axel H. Leimer , John M. Young , James Ivan Gerrity
发明人： Lyle W. Spruce , Albert C. Gyorkos , John C. Cheronis , Val S. Goodfellow , Axel H. Leimer , John M. Young , James Ivan Gerrity
IPC分类号： A61K38/00 , C07K5/06 , C07K5/062 , C07K5/087 , C07K5/093 , A61K38/03 , C07D215/02 , C07D237/30 , C07D239/70 , C07D241/36 , C07D253/10
CPC分类号： C07K5/06078 , C07K5/06043 , C07K5/06052 , C07K5/0812 , C07K5/0819 , A61K38/00
摘要： The present invention relates to cysteine protease inhibitors of the general formula (I): ##STR1## wherein Z is a cysteine protease binding moiety; X and Y are S, O or optionally substituted N; and R.sub.1 is optionally substituted alkyl or aryl.
摘要翻译： 本发明涉及通式（I）的半胱氨酸蛋白酶抑制剂：其中Z是半胱氨酸蛋白酶结合部分; X和Y是S，O或任选取代的N; 并且R 1是任选取代的烷基或芳基。
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公开(公告)号：US5750506A
公开(公告)日：1998-05-12
申请号：US647281
申请日：1996-05-13
申请人： Val S. Goodfellow , Heather B. Kroona , Eric T. Whalley , Francine E. Wincott , Dana A. Zummach
发明人： Val S. Goodfellow , Heather B. Kroona , Eric T. Whalley , Francine E. Wincott , Dana A. Zummach
摘要： Bradykinin antagonists, particularly Cys.sup.6 analogs, which have an extended hydrophobic side chain.
摘要翻译： 缓激肽拮抗剂，特别是具有延长的疏水侧链的Cys6类似物。
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8.发明授权Method for preparing and identifying N-substitued 1,4-piperazines and N-substituted 1,4-piperazinediones 失效制备和鉴定N-取代的1,4-哌嗪和N-取代的1,4-哌嗪二酮的方法
公开(公告)号：US5811241A
公开(公告)日：1998-09-22
申请号：US527407
申请日：1995-09-13
申请人： Val S. Goodfellow , Donald A. McLeod , James Ivan Gerrity , Christopher P. Laudeman , Michael R. Burkard
发明人： Val S. Goodfellow , Donald A. McLeod , James Ivan Gerrity , Christopher P. Laudeman , Michael R. Burkard
IPC分类号： C07D241/08 , C07D295/02 , G01N33/53 , G01N33/543 , G01N33/566
CPC分类号： C07D295/02 , C07D241/08
摘要： The invention provides a method of synthesizing N-substituted 1,4-piperazines and N-substituted 1,4-piperazinediones. The invention also provides a method for synthesing combinatorial libraries of piperazine derivatives which can be assayed for biological activity in pre-specified ligand binding or enzymatic activity screens.
摘要翻译： 本发明提供合成N-取代的1,4-哌嗪和N-取代的1,4-哌嗪二酮的方法。 本发明还提供了合成哌嗪衍生物的组合文库的方法，其可以在预先指定的配体结合或酶活性筛选中测定生物活性。
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9.发明授权
公开(公告)号：US5610140A
公开(公告)日：1997-03-11
申请号：US284068
申请日：1994-08-01
CPC分类号： C07K7/18 , A61K38/00 , Y10S530/807 , Y10S530/815 , Y10S530/816
摘要： The present invention provides a heterodimeric compound possessing bradykinin and neurokinin receptor antagonist activities useful in the treatment of asthma and other inflammatory diseases especially those involving the airway or pulmonary system. The present invention is also useful in the treatment of pain and inflammation.
摘要翻译： 本发明提供了具有缓激肽和神经激肽受体拮抗剂活性的异二聚体化合物，其用于治疗哮喘和其它炎性疾病，特别是涉及气道或肺系统的炎性疾病。 本发明也可用于治疗疼痛和炎症。
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公开(公告)号：US5700779A
公开(公告)日：1997-12-23
申请号：US668100
申请日：1996-06-20
申请人： Val S. Goodfellow , Manoj V. Marathe , Eric T. Whalley , Timothy D. Fitzpatrick , Karen G. Kuhlman
发明人： Val S. Goodfellow , Manoj V. Marathe , Eric T. Whalley , Timothy D. Fitzpatrick , Karen G. Kuhlman
IPC分类号： A61K38/55 , A61K38/00 , A61P3/00 , A61P9/00 , A61P11/00 , A61P25/04 , A61P29/00 , A61P31/04 , A61P35/00 , A61P43/00 , C07K7/06 , C07K7/18
摘要： The present invention provides bradykinin type peptides containing N-substituted glycines, particularly bradykinin antagonist peptides useful for the treatment of conditions mediated by bradykinin including pain and inflammation.
摘要翻译： 本发明提供了含有N-取代甘氨酸的缓激肽型肽，特别是可用于治疗由缓激肽介导的病症（包括疼痛和炎症）的缓激肽拮抗剂肽。
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