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公开(公告)号:US20090069288A1
公开(公告)日:2009-03-12
申请号:US12218364
申请日:2008-07-15
申请人: Eric C. Breinlinger , Kevin P. Cusack , Adrian D. Hobson , Bin Li , Thomas D. Gordon , Robert H. Stoffel , Grier A. Wallace , Pintipa Grongsaard , Lu Wang , Lu Wang
发明人: Eric C. Breinlinger , Kevin P. Cusack , Adrian D. Hobson , Bin Li , Thomas D. Gordon , Robert H. Stoffel , Grier A. Wallace , Pintipa Grongsaard , Lu Wang , Lu Wang
IPC分类号: A61K31/4196 , C07D249/10 , C07D403/12 , C07D261/14 , A61K31/42 , A61K31/415 , C07D231/14 , A61P35/00
CPC分类号: C07D249/10 , C07D231/14 , C07D249/06 , C07D261/14 , C07D261/18 , C07D273/02 , C07D333/36 , C07D333/38 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/04 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/04 , C07D413/10 , C07D413/12 , C07D413/14 , C07D417/12
摘要: Disclosed herein are novel compounds of Formula (I), wherein the variables are defined as herein. The compounds of Formula (I) are useful as kinase inhibitors and as such would be useful in treating certain conditions and diseases, especially inflammatory conditions and diseases as well as proliferative disorders such as cancer.
摘要翻译: 本文公开了式(I)的新化合物,其中变量如本文所定义。 式(I)的化合物可用作激酶抑制剂,因此可用于治疗某些病症和疾病,特别是炎性疾病和疾病以及增殖性疾病如癌症。
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2.
公开(公告)号:US08217027B2
公开(公告)日:2012-07-10
申请号:US12075378
申请日:2008-03-11
申请人: Grier A. Wallace , Eric C. Breinlinger , Kevin P. Cusack , Shannon R. Fix-Stenzel , Thomas D. Gordon , Adrian D. Hobson , Martin E. Hayes , Graham K. Ansell , Pintipa Grongsaard
发明人: Grier A. Wallace , Eric C. Breinlinger , Kevin P. Cusack , Shannon R. Fix-Stenzel , Thomas D. Gordon , Adrian D. Hobson , Martin E. Hayes , Graham K. Ansell , Pintipa Grongsaard
IPC分类号: C07D205/02 , A61K31/397
CPC分类号: C07F9/3808 , C07C59/72 , C07C215/42 , C07C229/48 , C07C2601/08 , C07D207/16 , C07D213/30 , C07D235/12 , C07D263/32 , C07D307/24 , C07D333/16 , C07F9/091 , C07F9/3826 , C07F9/4006 , C07F9/58 , C07F9/6527 , C07F9/65515 , C07F9/655345
摘要: The present invention is directed to novel, potent, and selective agents, which are agonists or antagonists of the one or more of the individual receptors of the S1P receptor family. The compounds of the invention are useful as therapeutics for treating medical conditions associated with agonism or antagonism of the individual receptors of the S1P receptor family.
摘要翻译: 本发明涉及作为S1P受体家族的一种或多种单独受体的激动剂或拮抗剂的新颖的,有效的和选择性的药剂。 本发明的化合物可用作治疗与S1P受体家族的各个受体的激动作用或拮抗作用相关的医学病症的治疗剂。
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3.
公开(公告)号:US20090029947A1
公开(公告)日:2009-01-29
申请号:US12075378
申请日:2008-03-11
申请人: Grier A. Wallace , Eric C. Breinlinger , Kevin P. Cusack , Shannon R. Fix-Stenzel , Thomas D. Gordon , Adrian D. Hobson , Martin E. Hayes , Graham K. Ansell , Pintipa Grongsaard
发明人: Grier A. Wallace , Eric C. Breinlinger , Kevin P. Cusack , Shannon R. Fix-Stenzel , Thomas D. Gordon , Adrian D. Hobson , Martin E. Hayes , Graham K. Ansell , Pintipa Grongsaard
IPC分类号: A61K31/661 , A61K31/196 , C07C229/48 , A61K31/138 , A61K31/40 , A61K31/192 , A61K31/4192 , A61K31/397 , A61K31/343 , C07D263/52 , A61P25/00 , A61P37/02 , A61P3/10 , C07D307/81 , C07D205/04 , C07D249/06 , C07C59/72 , C07D207/08 , C07C215/42 , C07C215/38 , C07F9/06
CPC分类号: C07F9/3808 , C07C59/72 , C07C215/42 , C07C229/48 , C07C2601/08 , C07D207/16 , C07D213/30 , C07D235/12 , C07D263/32 , C07D307/24 , C07D333/16 , C07F9/091 , C07F9/3826 , C07F9/4006 , C07F9/58 , C07F9/6527 , C07F9/65515 , C07F9/655345
摘要: The present invention is directed to novel, potent, and selective agents, which are agonists or antagonists of the one or more of the individual receptors of the S1P receptor family. The compounds of the invention are useful as therapeutics for treating medical conditions associated with agonism or antagonism of the individual receptors of the S1P receptor family.
摘要翻译: 本发明涉及作为S1P受体家族的一种或多种单独受体的激动剂或拮抗剂的新颖的,有效的和选择性的药剂。 本发明的化合物可用作治疗与S1P受体家族的各个受体的激动作用或拮抗作用相关的医学病症的治疗剂。
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公开(公告)号:US20110207704A1
公开(公告)日:2011-08-25
申请号:US12861931
申请日:2010-08-24
申请人: Kevin P. Cusack , Eric C. Breinlinger , Shannon R. Fix-Stenzel , Robert H. Stoffel , Kevin R. Woller , Adrian D. Hobson , Pintipa Grongsaard
发明人: Kevin P. Cusack , Eric C. Breinlinger , Shannon R. Fix-Stenzel , Robert H. Stoffel , Kevin R. Woller , Adrian D. Hobson , Pintipa Grongsaard
IPC分类号: A61K31/675 , C07D271/06 , A61K31/4245 , C07D413/12 , C07D413/10 , C07D413/04 , A61K31/4439 , C07D401/14 , A61K31/439 , C07F9/40 , A61K31/4709 , A61K31/454 , A61K31/5377 , A61K31/397 , C07D487/04 , A61K31/4985 , A61P11/00 , A61P31/14 , A61P25/28 , A61P17/06 , A61P19/02 , A61P1/04
CPC分类号: C07D271/06 , C07D271/07 , C07D413/04 , C07D413/06 , C07D413/10 , C07D413/12 , C07D413/14 , C07D417/04 , C07D471/04 , C07D487/04
摘要: Novel oxadiazole compounds, pharmaceutical compositions containing such compounds and the use of those compounds or compositions as agonists or antagonists of the S1P family of G protein-coupled receptors for treating diseases associated with modulation of S1P family receptor activity, in particular by affording a beneficial immunosuppressive effect are disclosed.
摘要翻译: 新型恶二唑化合物,含有这些化合物的药物组合物以及这些化合物或组合物作为G蛋白偶联受体的S1P家族的激动剂或拮抗剂用于治疗与调节S1P家族受体活性有关的疾病的用途,特别是通过提供有益的免疫抑制 效果被公开。
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公开(公告)号:US07834039B2
公开(公告)日:2010-11-16
申请号:US12002196
申请日:2007-12-14
申请人: Adrian D. Hobson , Shannon R. Fix-Stenzel , Kevin P. Cusack , Eric C. Breinlinger , Graham K. Ansell , Robert H. Stoffel , Kevin R. Woller , Pintipa Grongsaard
发明人: Adrian D. Hobson , Shannon R. Fix-Stenzel , Kevin P. Cusack , Eric C. Breinlinger , Graham K. Ansell , Robert H. Stoffel , Kevin R. Woller , Pintipa Grongsaard
IPC分类号: A61K31/4245 , C07D271/06
CPC分类号: C07D271/07 , C07D271/06 , C07D413/04 , C07D413/06 , C07D413/10 , C07D413/12 , C07D413/14 , C07D417/04 , C07D471/04 , C07D487/04
摘要: Novel oxadiazole compounds, pharmaceutical compositions containing such compounds and the use of those compounds or compositions as agonists or antagonists of the S1P family of G protein-coupled receptors for treating diseases associated with modulation of S1P family receptor activity, in particular by affording a beneficial immunosuppressive effect are disclosed.
摘要翻译: 新型恶二唑化合物,含有这些化合物的药物组合物以及这些化合物或组合物作为G蛋白偶联受体的S1P家族的激动剂或拮抗剂用于治疗与调节S1P家族受体活性有关的疾病的用途,特别是通过提供有益的免疫抑制 效果被公开。
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公开(公告)号:US20120238549A1
公开(公告)日:2012-09-20
申请号:US13420957
申请日:2012-03-15
申请人: Kevin P. Cusack , Thomas D. Gordon , David C. Ihle , Martin E. Hayes , Eric C. Breinlinger , Anna M. Ericsson , Bin Li , Lei Wang , Gloria Y. Martinez , Andrew Burchat , Adrian D. Hobson , Kelly D. Mullen , Michael Friedman , Michael J. Morytko
发明人: Kevin P. Cusack , Thomas D. Gordon , David C. Ihle , Martin E. Hayes , Eric C. Breinlinger , Anna M. Ericsson , Bin Li , Lei Wang , Gloria Y. Martinez , Andrew Burchat , Adrian D. Hobson , Kelly D. Mullen , Michael Friedman , Michael J. Morytko
IPC分类号: A61K31/122 , C07D213/74 , A61K31/44 , C07D401/12 , A61K31/55 , C07C45/61 , C07C45/62 , C07D453/04 , A61P5/00 , A61P25/30 , A61P37/08 , A61P25/28 , A61P7/10 , A61P25/22 , A61P11/06 , A61P37/00 , A61P31/14 , A61P9/00 , A61P13/12 , A61P27/02 , A61P1/16 , A61P1/00 , A61P25/24 , A61P3/10 , A61P27/06 , A61P29/00 , A61P31/18 , A61P9/12 , A61P35/00 , A61P37/02 , A61P5/48 , A61P35/02 , A61P19/04 , A61P25/00 , A61P3/04 , A61P37/06 , A61P19/10 , A61P19/02 , A61P25/16 , A61P17/06 , A61P25/18 , A61P3/00 , A61P1/04 , A61P17/02 , C07C49/755
CPC分类号: C07D213/75 , C07B2200/07 , C07C45/62 , C07C45/72 , C07C45/74 , C07C49/755 , C07D231/54 , C07D235/18 , C07D241/20 , C07D401/04 , C07D401/12 , C07D405/12 , C07D453/04 , C07D487/06 , C07D491/20 , C07C49/67
摘要: The invention provides a compound of Formula (I) pharmaceutically acceptable salts, pro-drugs, biologically active metabolites, stereoisomers and isomers thereof wherein the variable are defined herein. The compounds of the invention are useful for treating immunological and oncological conditions.
摘要翻译: 本发明提供式(I)化合物的药学上可接受的盐,前药,生物活性代谢物,立体异构体和异构体,其中变量在本文中定义。 本发明的化合物可用于治疗免疫学和肿瘤学病症。
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公开(公告)号:US20080280876A1
公开(公告)日:2008-11-13
申请号:US12002196
申请日:2007-12-14
申请人: Adrian D. Hobson , Shannon R. Fix-Stenzel , Kevin P. Cusack , Eric C. Breinlinger , Graham K. Ansell , Robert H. Stoffel
发明人: Adrian D. Hobson , Shannon R. Fix-Stenzel , Kevin P. Cusack , Eric C. Breinlinger , Graham K. Ansell , Robert H. Stoffel
IPC分类号: A61K31/4245 , C07D271/06 , A61K31/4439 , A61K31/5377 , A61P37/00 , C07D413/14 , A61K31/4985 , C07D487/04 , A61K31/4725 , A61P25/00 , C07D491/052 , A61K31/454 , C07D413/02
CPC分类号: C07D271/07 , C07D271/06 , C07D413/04 , C07D413/06 , C07D413/10 , C07D413/12 , C07D413/14 , C07D417/04 , C07D471/04 , C07D487/04
摘要: Novel oxadiazole compounds, pharmaceutical compositions containing such compounds and the use of those compounds or compositions as agonists or antagonists of the S1P family of G protein-coupled receptors for treating diseases associated with modulation of S1P family receptor activity, in particular by affording a beneficial immunosuppressive effect are disclosed.
摘要翻译: 新型恶二唑化合物,含有这些化合物的药物组合物以及这些化合物或组合物作为G蛋白偶联受体的S1P家族的激动剂或拮抗剂用于治疗与调节S1P家族受体活性有关的疾病的用途,特别是通过提供有益的免疫抑制 效果被公开。
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公开(公告)号:US20110152243A1
公开(公告)日:2011-06-23
申请号:US12974311
申请日:2010-12-21
申请人: Neil Wishart , Theresa Dunstan , Jeremy J. Edmunds , Anna M. Ericsson , Catherine R. Ferenz , Adrian D. Hobson , David C. Ihle , Kent D. Stewart , Lei Wang , Lu Wang
发明人: Neil Wishart , Theresa Dunstan , Jeremy J. Edmunds , Anna M. Ericsson , Catherine R. Ferenz , Adrian D. Hobson , David C. Ihle , Kent D. Stewart , Lei Wang , Lu Wang
IPC分类号: A61K31/397 , C07D401/14 , A61K31/517 , A61K31/496 , A61K31/454 , C07D487/04 , A61K31/53 , A61K31/437 , C07D403/14 , A61K31/416 , C07D471/04 , C07D413/14 , A61K31/5377 , A61P3/10 , A61P17/06 , A61P1/04 , A61P19/02 , A61P35/00
CPC分类号: C07D487/04 , C07D487/08 , C07D495/04 , C07D498/04
摘要: The invention provides a compound of Formula (I) pharmaceutically acceptable salts, pro-drugs, biologically active metabolites, stereoisomers and isomers thereof wherein the variable are defined herein. The compounds of the invention are useful for treating immunological and oncological conditions.
摘要翻译: 本发明提供式(I)化合物的药学上可接受的盐,前药,生物活性代谢物,立体异构体和异构体,其中变量在本文中定义。 本发明的化合物可用于治疗免疫学和肿瘤学病症。
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公开(公告)号:US20080176883A1
公开(公告)日:2008-07-24
申请号:US11985724
申请日:2007-11-16
申请人: Dawn M. George , Richard W. Dixon , Michael Friedman , Adrian D. Hobson , Biqin Li , Lu Wang , Xiaoyun Wu , Neil Wishart
发明人: Dawn M. George , Richard W. Dixon , Michael Friedman , Adrian D. Hobson , Biqin Li , Lu Wang , Xiaoyun Wu , Neil Wishart
IPC分类号: A61K31/438 , C07D471/04 , A61K31/4375 , C07D401/04 , A61K31/454
CPC分类号: A61K31/454 , A61K31/437 , A61K31/438 , A61K31/4545 , A61K31/4709 , A61K31/4747 , A61K31/506 , A61K31/517 , A61K31/5377 , A61K31/55 , A61K31/553 , C07D207/14 , C07D401/04 , C07D401/14 , C07D403/12 , C07D405/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D471/10 , C07D487/04 , C07D487/10 , C07D487/14
摘要: The present invention is directed to novel aminopyrrolidines of formula I pharmaceutically acceptable salts thereof, metabolites thereof, isomers thereof, stereoisomers thereof or pro-drugs thereof, wherein the variables are as defined herein. The compounds of formula (I) are useful as chemokine receptor antagonists and as such would be useful in treating certain conditions and diseases, especially inflammatory conditions and diseases and proliferative disorders and conditions, for example, cancers.
摘要翻译: 本发明涉及式I的药学上可接受的盐的新型氨基吡咯烷,其代谢物,其异构体,其立体异构体或其前体药物,其中变量如本文所定义。 式(I)化合物可用作趋化因子受体拮抗剂,因此可用于治疗某些病症和疾病,特别是炎性病症和疾病以及增殖性疾病和病症,例如癌症。
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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。
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