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公开(公告)号：US20100004231A1
公开(公告)日：2010-01-07
申请号：US12459595
申请日：2009-07-01
IPC分类号： A61K31/5415 , A61K31/5377 , A61K31/502 , A61K31/497 , C07D417/08 , C07D413/14 , C07D403/10 , C07D403/14 , C07D401/08 , A61P35/00
CPC分类号： C07D403/10 , C07D401/14 , C07D403/14 , C07D413/14 , C07D417/14
摘要： This application discloses 5-phenyl-1H-pyrazin-2-one derivatives according to generic Formulae I-V: wherein, variables Q, R, Y1, Y2, Y2′, Y3, Y4, n and m are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation such as rheumatoid arthritis. Also disclosed are compositions comprising compounds of Formulae I-V and at least one carrier, diluent or excipient.
摘要翻译： 本申请公开了根据通式IV的5-苯基-1H-吡嗪-2-酮衍生物：其中，变量Q，R，Y1，Y2，Y2'，Y3，Y4，n和m如本文所述定义，其抑制 Btk。 本文公开的化合物可用于调节Btk的活性并治疗与过量Btk活性相关的疾病。 该化合物还可用于治疗与异常B细胞增殖相关的炎症和自身免疫疾病，例如类风湿性关节炎。 还公开了包含式I-V化合物和至少一种载体，稀释剂或赋形剂的组合物。
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公开(公告)号：US08536166B2
公开(公告)日：2013-09-17
申请号：US12459595
申请日：2009-07-01
IPC分类号： A61K31/496 , A61K31/497 , A61K31/517 , A61K31/5377 , A61K31/541 , C07D401/10 , C07D401/14 , C07D407/14 , C07D413/14 , C07D417/14 , A61K31/502
CPC分类号： C07D403/10 , C07D401/14 , C07D403/14 , C07D413/14 , C07D417/14
摘要： This application discloses 5-phenyl-1H-pyrazin-2-one derivatives according to generic Formulae I-V: wherein, variables Q, R, Y1, Y2, Y2′, Y3, Y4, n and m are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation such as rheumatoid arthritis. Also disclosed are compositions comprising compounds of Formulae I-V and at least one carrier, diluent or excipient.
摘要翻译： 本申请公开了根据通式IV的5-苯基-1H-吡嗪-2-酮衍生物：其中，变量Q，R，Y1，Y2，Y2'，Y3，Y4，n和m如本文所述定义，其抑制 Btk。 本文公开的化合物可用于调节Btk的活性并治疗与过量Btk活性相关的疾病。 该化合物还可用于治疗与异常B细胞增殖相关的炎症和自身免疫疾病，例如类风湿性关节炎。 还公开了包含式I-V化合物和至少一种载体，稀释剂或赋形剂的组合物。
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公开(公告)号：US08324211B2
公开(公告)日：2012-12-04
申请号：US12460226
申请日：2009-07-15
申请人： Nolan James Dewdney , Yan Lou , Eric Brian Sjogren , Michael Soth
发明人： Nolan James Dewdney , Yan Lou , Eric Brian Sjogren , Michael Soth
IPC分类号： A61K31/50 , C07D237/00
CPC分类号： C07D487/04 , C07D471/04
摘要： This application discloses 6-Phenyl-imidazo[1,2-a]pyridine and 6-Phenyl-imidazo[1,2-b]pyridazine derivatives according to generic Formulae I-V: wherein, variables Q, R, X, Y1, Y2, Y3, Y4, n, and m are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation such as rheumatoid arthritis. Also disclosed are compositions comprising compounds of Formulae I-V and at least one carrier, diluent or excipient.
摘要翻译： 本申请公开了根据通式IV的6-苯基 - 咪唑并[1,2-a]吡啶和6-苯基 - 咪唑并[1,2-b]哒嗪衍生物：其中，变量Q，R，X，Y 1， Y3，Y4，n和m如本文所述限定Btk。 本文公开的化合物可用于调节Btk的活性并治疗与过量Btk活性相关的疾病。 该化合物还可用于治疗与异常B细胞增殖相关的炎症和自身免疫疾病，例如类风湿性关节炎。 还公开了包含式I-V化合物和至少一种载体，稀释剂或赋形剂的组合物。
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公开(公告)号：US20100016301A1
公开(公告)日：2010-01-21
申请号：US12460226
申请日：2009-07-15
申请人： Nolan James Dewdney , Yan Lou , Eric Brian Sjogren , Michael Soth
发明人： Nolan James Dewdney , Yan Lou , Eric Brian Sjogren , Michael Soth
IPC分类号： A61K31/5377 , C07D487/04 , A61K31/437 , C07D471/04
CPC分类号： C07D487/04 , C07D471/04
摘要： This application discloses 6-Phenyl-imidazo[1,2-a]pyridine and 6-Phenyl-imidazo[1,2-b]pyridazine derivatives according to generic Formulae I-V: wherein, variables Q, R, X, Y1, Y2, Y3, Y4, n, and m are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation such as rheumatoid arthritis. Also disclosed are compositions comprising compounds of Formulae I-V and at least one carrier, diluent or excipient.
摘要翻译： 本申请公开了根据通式IV的6-苯基 - 咪唑并[1,2-a]吡啶和6-苯基 - 咪唑并[1,2-b]哒嗪衍生物：其中，变量Q，R，X，Y 1， Y3，Y4，n和m如本文所述限定Btk。 本文公开的化合物可用于调节Btk的活性并治疗与过量Btk活性相关的疾病。 该化合物还可用于治疗与异常B细胞增殖相关的炎症和自身免疫疾病，例如类风湿性关节炎。 还公开了包含式I-V化合物和至少一种载体，稀释剂或赋形剂的组合物。
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公开(公告)号：US08426409B2
公开(公告)日：2013-04-23
申请号：US12460387
申请日：2009-07-17
申请人： Rama K. Kondru , Yan Lou , Eric Brian Sjogren , Michael Soth
发明人： Rama K. Kondru , Yan Lou , Eric Brian Sjogren , Michael Soth
IPC分类号： A01N43/58 , A01N43/60 , A61K31/50 , A61K31/495 , C07D401/00 , C07D403/00 , C07D413/00 , C07D417/00 , C07D419/00
CPC分类号： C07D487/04
摘要： This application discloses 6-Phenyl-imidazo[1,2-a]pyrazine derivatives according to generic Formulae I-V: wherein, variables Q, R, Y1, Y2, Y3, Y4, n, and m are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation such as rheumatoid arthritis. Also disclosed are compositions comprising compounds of Formulae I-V and at least one carrier, diluent or excipient.
摘要翻译： 本申请公开了根据通式IV的6-苯基 - 咪唑并[1,2-a]吡嗪衍生物：其中变量Q，R，Y 1，Y 2，Y 3，Y 4，n和m如本文所述定义，其抑制 Btk。 本文公开的化合物可用于调节Btk的活性并治疗与过量Btk活性相关的疾病。 该化合物还可用于治疗与异常B细胞增殖相关的炎症和自身免疫疾病，例如类风湿性关节炎。 还公开了包含式I-V化合物和至少一种载体，稀释剂或赋形剂的组合物。
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公开(公告)号：US20100016302A1
公开(公告)日：2010-01-21
申请号：US12460387
申请日：2009-07-17
申请人： Rama K. Kondru , Yan Lou , Eric Brian Sjogren , Michael Soth
发明人： Rama K. Kondru , Yan Lou , Eric Brian Sjogren , Michael Soth
IPC分类号： A61K31/5377 , A61K31/502 , A61K31/4985 , C07D487/04 , A61P37/02
CPC分类号： C07D487/04
摘要： This application discloses 6-Phenyl-imidazo[1,2-a]pyrazine derivatives according to generic Formulae I-V: wherein, variables Q, R, Y1, Y2, Y3, Y4, n, and m are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation such as rheumatoid arthritis. Also disclosed are compositions comprising compounds of Formulae I-V and at least one carrier, diluent or excipient.
摘要翻译： 本申请公开了根据通式IV的6-苯基 - 咪唑并[1,2-a]吡嗪衍生物：其中变量Q，R，Y 1，Y 2，Y 3，Y 4，n和m如本文所述定义，其抑制 Btk。 本文公开的化合物可用于调节Btk的活性并治疗与过量Btk活性相关的疾病。 该化合物还可用于治疗与异常B细胞增殖相关的炎症和自身免疫疾病，例如类风湿性关节炎。 还公开了包含式I-V化合物和至少一种载体，稀释剂或赋形剂的组合物。
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公开(公告)号：US07189718B2
公开(公告)日：2007-03-13
申请号：US10807993
申请日：2004-03-23
申请人： James Patrick Dunn , Brian William Dymock , Taraneh Mirzadegan , Eric Brian Sjogren , Steven Swallow , Zachary Kevin Sweeney
发明人： James Patrick Dunn , Brian William Dymock , Taraneh Mirzadegan , Eric Brian Sjogren , Steven Swallow , Zachary Kevin Sweeney
IPC分类号： C07D237/14 , C07D237/22 , A61K31/501
CPC分类号： C07D401/12 , C07D237/14 , C07D237/22 , C07D405/06 , C07D409/06
摘要： This invention relates to novel pyridazinone derivatives of formula I wherein R1–R4, R7, R8 and X1 are as defined in the summary and pharmaceutically acceptable salts and solvates thereof, methods to inhibit or modulate Human Immunodeficiency Virus (HIV) reverse transcriptase with compounds of formula I, pharmaceutical compositions containing of formula I admixed with at least one solvent, carrier or excipient and processes to prepare compounds of formula I. The compounds are useful for treating disorders in which HIV and genetically related viruses are implicated
摘要翻译： 本发明涉及式I的新的哒嗪酮衍生物，其中R 1，R 2，R 4，R 7，R 8， 和其中X 1如本发明概述及其药学上可接受的盐和溶剂合物中所定义，用式I化合物抑制或调节人类免疫缺陷病毒（HIV）逆转录酶的方法，含有式I的药物组合物 与至少一种溶剂，载体或赋形剂反应，并制备式I化合物。该化合物可用于治疗涉及HIV和遗传相关病毒的疾病
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公开(公告)号：US08618103B2
公开(公告)日：2013-12-31
申请号：US12878048
申请日：2010-09-09
申请人： Javier de Vicente Fidalgo , Johannes Cornelius Hermann , Remy Lemoine , Hongju Li , Allen John Lovey , Eric Brian Sjogren , Michael Soth
发明人： Javier de Vicente Fidalgo , Johannes Cornelius Hermann , Remy Lemoine , Hongju Li , Allen John Lovey , Eric Brian Sjogren , Michael Soth
IPC分类号： C07D487/04 , A61K31/4985 , C07D239/04 , A61K31/506 , A61P29/00 , A61P35/00
CPC分类号： C07D487/04 , C07D513/04
摘要： The present invention relates to the use of novel compounds of Formula I, wherein the variables m, n, p, q, Q, r, R, R′, X, X′, Y, Z1, Z2, and Z3 are defined as described herein, which inhibit JAK and are useful for the treatment of auto-immune and inflammatory diseases.
摘要翻译： 本发明涉及式I的新化合物的用途，其中变量m，n，p，q，Q，r，R，R'，X，X'，Y，Z 1，Z 2和Z 3定义为 其抑制JAK并且可用于治疗自身免疫和炎性疾病。
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公开(公告)号：US20110059118A1
公开(公告)日：2011-03-10
申请号：US12878048
申请日：2010-09-09
申请人： Javier de Vicente Fidalgo , Johannes Cornelius Hermann , Remy Lemoine , Hongju Li , Allen John Lovey , Eric Brian Sjogren , Michael Soth
发明人： Javier de Vicente Fidalgo , Johannes Cornelius Hermann , Remy Lemoine , Hongju Li , Allen John Lovey , Eric Brian Sjogren , Michael Soth
IPC分类号： A61K31/4985 , C07D487/04 , A61K31/55 , A61K31/5377 , A61K31/541 , A61K31/506 , A61K39/00 , A61P29/00 , A61P37/00 , A61P19/02 , A61P17/06 , A61P25/00 , A61P3/10 , A61P11/06 , A61P35/00 , A61P1/04 , A61P25/28 , A61P35/02
CPC分类号： C07D487/04 , C07D513/04
摘要： The present invention relates to the use of novel compounds of Formula I, wherein the variables m, n, p, q, Q, r, R, R′, X, X′, Y, Z1, Z2, and Z3 are defined as described herein, which inhibit JAK and are useful for the treatment of auto-immune and inflammatory diseases.
摘要翻译： 本发明涉及式I的新化合物的用途，其中变量m，n，p，q，Q，r，R，R'，X，X'，Y，Z 1，Z 2和Z 3定义为 其抑制JAK并且可用于治疗自身免疫和炎性疾病。
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公开(公告)号：US08268840B2
公开(公告)日：2012-09-18
申请号：US12387181
申请日：2009-04-29
申请人： Frederick Brookfield , Florence Eustache , Michael Patrick Dillon , David Michael Goldstein , Leyi Gong , Xiaochun Han , Joan Heather Hogg , Jaehyeon Park , Deborah Carol Reuter , Eric Brian Sjogren
发明人： Frederick Brookfield , Florence Eustache , Michael Patrick Dillon , David Michael Goldstein , Leyi Gong , Xiaochun Han , Joan Heather Hogg , Jaehyeon Park , Deborah Carol Reuter , Eric Brian Sjogren
IPC分类号： A01N43/90 , A61K31/519 , C07D471/00
CPC分类号： C07D471/04
摘要： This application discloses novel pyrimidinyl pyridone derivatives according to formula I, wherein A, R1, R2, R3, and m are defined as described herein, which inhibit JNK. The compounds disclosed herein are useful to modulate the activity of JNK and treat diseases associated with excessive JNK activity. The compounds are useful to treat autoimmune, inflammatory, metabolic, and neurological diseases as well as cancer. Also disclosed are compositions comprising the compound of formula I and methods of treatment comprising administering a therapeutically effective amount of the compound of formula I to a subject in need thereof.
摘要翻译： 本申请公开了根据式I的新型嘧啶基吡啶酮衍生物，其中A，R1，R2，R3和m如本文所述限定，其抑制JNK。 本文公开的化合物可用于调节JNK的活性并治疗与过量JNK活性相关的疾病。 这些化合物可用于治疗自身免疫性，炎性，代谢和神经疾病以及癌症。 还公开了包含式I化合物和治疗方法的组合物，其包括向有需要的受试者施用治疗有效量的式I化合物。
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