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公开(公告)号：US08318719B2
公开(公告)日：2012-11-27
申请号：US12765904
申请日：2010-04-23
IPC分类号： C07D403/14 , C07D413/04 , A61K31/5513 , A61K31/553 , A61P29/00
CPC分类号： C07D413/14 , C07D403/14
摘要： This application discloses 5-phenyl-1H-pyridin-2-one, 6-phenyl-2H-pyridazin-3-one, and 5-phenyl-1H-pyrazin-2-one derivatives according to generic Formulae I-II: wherein, variables Q1, Q2, R, X, Y1, Y2, Y2′, Y3, Y4, Y5, m, and p 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 containing compounds of Formulae I-II and at least one carrier, diluent or excipient.
摘要翻译： 本申请公开了根据通式I-II的5-苯基-1H-吡啶-2-酮，6-苯基-2H-哒嗪-3-酮和5-苯基-1H-吡嗪-2-酮衍生物：其中， 变量Q1，Q2，R，X，Y1，Y2，Y2'，Y3，Y4，Y5，m和p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。 还公开了含有式I-II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：US20100273768A1
公开(公告)日：2010-10-28
申请号：US12765904
申请日：2010-04-23
IPC分类号： A61K31/553 , C07D413/14 , A61P29/00 , A61P37/00 , A61K31/5513 , A61P11/06 , A61P19/02
CPC分类号： C07D413/14 , C07D403/14
摘要： This application discloses 5-phenyl-1H-pyridin-2-one, 6-phenyl-2H-pyridazin-3-one, and 5-phenyl-1H-pyrazin-2-one derivatives according to generic Formulae I-II: wherein, variables Q1, Q2, R, X, Y1, Y2, Y2′, Y3, Y4, Y5, m, and p 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 containing compounds of Formulae I-II and at least one carrier, diluent or excipient.
摘要翻译： 本申请公开了根据通式I-II的5-苯基-1H-吡啶-2-酮，6-苯基-2H-哒嗪-3-酮和5-苯基-1H-吡嗪-2-酮衍生物：其中， 变量Q1，Q2，R，X，Y1，Y2，Y2'，Y3，Y4，Y5，m和p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。 还公开了含有式I-II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：US20110288097A1
公开(公告)日：2011-11-24
申请号：US13110053
申请日：2011-05-18
申请人： Robert Than Hendricks , Johannes Hermann , Rama Kondru , Yan Lou , Stephen Lynch , Timothy D. Owens , Michael Soth , Calvin Yee
发明人： Robert Than Hendricks , Johannes Hermann , Rama Kondru , Yan Lou , Stephen Lynch , Timothy D. Owens , Michael Soth , Calvin Yee
IPC分类号： A61K31/4985 , A61P37/02 , A61P3/10 , A61P17/02 , A61P17/06 , A61P25/28 , A61P35/02 , A61P11/06 , A61P35/00 , C07D471/04 , A61P1/00
CPC分类号： C07D487/04
摘要： The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula I, wherein the variables Q and R1 and R2 are defined as described herein, which inhibit JAK and SYK and are useful for the treatment of auto-immune and inflammatory diseases.
摘要翻译： 本发明涉及式I的新型吡咯并吡嗪衍生物的用途，其中变量Q和R 1和R 2如本文所述定义，其抑制JAK和SYK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：US20110230414A1
公开(公告)日：2011-09-22
申请号：US13039433
申请日：2011-03-03
申请人： Robert Than Hendricks , Johannes Hermann , Rama Kondru , Yan Lou , Stephen M. Lynch , Timothy D. Owens , Michael Soth
发明人： Robert Than Hendricks , Johannes Hermann , Rama Kondru , Yan Lou , Stephen M. Lynch , Timothy D. Owens , Michael Soth
IPC分类号： A61K38/00 , C07D487/04 , A61K31/4985 , A61P29/00 , A61P35/00 , A61P9/00 , A61P3/10 , A61P19/02 , A61P37/06 , A61P11/06 , A61P1/04 , A61P5/02 , A61P25/28
CPC分类号： C07D487/04
摘要： The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula I, wherein the variables Q, R2, R3, and Y are defined as described herein, which inhibit JAK and SYK and are useful for the treatment of auto-immune and inflammatory diseases.
摘要翻译： 本发明涉及式I的新型吡咯并吡嗪衍生物的用途，其中变量Q，R2，R3和Y如本文所述定义，其抑制JAK和SYK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：US20110288067A1
公开(公告)日：2011-11-24
申请号：US13110062
申请日：2011-05-18
申请人： Robert Than Hendricks , Johannes Hermann , Saul Jaime-Figueroa , Rama Kondru , Yan Lou , Stephen Lynch , Timothy D. Owens , Michael Soth , Calvin Yee
发明人： Robert Than Hendricks , Johannes Hermann , Saul Jaime-Figueroa , Rama Kondru , Yan Lou , Stephen Lynch , Timothy D. Owens , Michael Soth , Calvin Yee
IPC分类号： A61K31/4985 , C07D295/155 , C07D491/107 , A61K31/541 , A61P29/00 , A61P37/00 , A61P35/00 , A61P25/00 , A61P9/00 , A61P3/10 , A61P37/04 , A61P11/06 , A61P19/04 , A61P17/06 , A61P37/06 , A61P17/00 , A61P5/14 , A61P1/04 , A61P1/00 , A61P25/28 , A61P35/02 , C07D487/04
CPC分类号： C07D487/04 , C07D519/00
摘要： The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula I, wherein the variables Q and R, R2, and R3 are defined as described herein, which inhibit JAK and SYK and are useful for the treatment of auto-immune and inflammatory diseases.
摘要翻译： 本发明涉及式I的新型吡咯并吡嗪衍生物的用途，其中变量Q和R，R2和R3如本文所述定义，其抑制JAK和SYK，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：US08329699B2
公开(公告)日：2012-12-11
申请号：US13110053
申请日：2011-05-18
申请人： Robert Than Hendricks , Johannes Hermann , Rama Kondru , Yan Lou , Stephen Lynch , Timothy D. Owens , Michael Soth , Calvin Yee
发明人： Robert Than Hendricks , Johannes Hermann , Rama Kondru , Yan Lou , Stephen Lynch , Timothy D. Owens , Michael Soth , Calvin Yee
IPC分类号： A61K31/495
CPC分类号： C07D487/04
摘要： The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula I, wherein the variables Q and R1 and R2 are defined as described herein, which inhibit JAK and SYK and are useful for the treatment of auto-immune and inflammatory diseases.
摘要翻译： 本发明涉及式I的新型吡咯并吡嗪衍生物的用途，其中变量Q和R 1和R 2如本文所述定义，其抑制JAK和SYK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：US08518945B2
公开(公告)日：2013-08-27
申请号：US13040310
申请日：2011-03-04
申请人： Robert Than Hendricks , Johannes Hermann , Rama Kondru , Yan Lou , Stephen M. Lynch , Timothy D. Owens , Michael Soth
发明人： Robert Than Hendricks , Johannes Hermann , Rama Kondru , Yan Lou , Stephen M. Lynch , Timothy D. Owens , Michael Soth
IPC分类号： A61K31/495
CPC分类号： C07D487/04 , C07D519/00
摘要： The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula I, wherein the variables n, p, q, Q, X, X′ and Y are defined as described herein, which inhibit JAK and SYK and are useful for the treatment of auto-immune and inflammatory diseases.
摘要翻译： 本发明涉及式I的新型吡咯并吡嗪衍生物的用途，其中变量n，p，q，Q，X，X'和Y如本文所述定义，其抑制JAK和SYK，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：US20110230462A1
公开(公告)日：2011-09-22
申请号：US13040310
申请日：2011-03-04
申请人： Robert Than Hendricks , Johannes Hermann , Rama Kondru , Yan Lou , Stephen M. Lynch , Timothy D. Owens , Michael Soth
发明人： Robert Than Hendricks , Johannes Hermann , Rama Kondru , Yan Lou , Stephen M. Lynch , Timothy D. Owens , Michael Soth
IPC分类号： A61K31/4985 , C07D487/04 , A61P29/00 , A61P35/00 , A61P37/00 , A61P9/00 , A61P3/10 , A61P11/06 , A61P17/06 , A61P25/28 , A61K31/5377 , A61K31/541
CPC分类号： C07D487/04 , C07D519/00
摘要： The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula I, wherein the variables n, p, q, Q, X, X′ and Y are defined as described herein, which inhibit JAK and SYK and are useful for the treatment of auto-immune and inflammatory diseases.
摘要翻译： 本发明涉及式I的新型吡咯并吡嗪衍生物的用途，其中变量n，p，q，Q，X，X'和Y如本文所述定义，其抑制JAK和SYK，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：US08481541B2
公开(公告)日：2013-07-09
申请号：US13039433
申请日：2011-03-03
申请人： Robert Than Hendricks , Johannes Hermann , Rama Kondru , Yan Lou , Stephen M. Lynch , Timothy D. Owens , Michael Soth
发明人： Robert Than Hendricks , Johannes Hermann , Rama Kondru , Yan Lou , Stephen M. Lynch , Timothy D. Owens , Michael Soth
IPC分类号： A61K31/495
CPC分类号： C07D487/04
摘要： The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula I, wherein the variables Q, R2, R3, and Y are defined as described herein, which inhibit JAK and SYK and are useful for the treatment of auto-immune and inflammatory diseases.
摘要翻译： 本发明涉及式I的新型吡咯并吡嗪衍生物的用途，其中变量Q，R2，R3和Y如本文所述定义，其抑制JAK和SYK并且可用于治疗自身免疫和炎性疾病 。
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10.发明授权Bicyclic pyrimidine PI3K inhibitor compounds selective for P110 delta, and methods of use 有权双环嘧啶PI3K抑制剂化合物选择性为P110δ，以及使用方法公开(公告)号：US08173650B2
公开(公告)日：2012-05-08
申请号：US12787613
申请日：2010-05-26
申请人： Georgette Castanedo , Bryan Chan , David Goldstein , Rama Kondru , Matthew Lucas , Wylie Palmer , Stephen Price , Brian Safina , Pascal Pierre Alexandre Savy , Eileen Mary Seward , Daniel P. Sutherlin , Zachary K. Sweeney
发明人： Georgette Castanedo , Bryan Chan , David Goldstein , Rama Kondru , Matthew Lucas , Wylie Palmer , Stephen Price , Brian Safina , Pascal Pierre Alexandre Savy , Eileen Mary Seward , Daniel P. Sutherlin , Zachary K. Sweeney
IPC分类号： A61K31/535 , C07D413/14
CPC分类号： C07D513/04 , C07D487/04 , C07D491/04 , C07D495/04
摘要： Formula I (Ia and Ib) compounds wherein (i) X1 is N and X2 is S, (ii) X1 is CR7 and X2 is S, (iii) X1 is N and X2 is NR2, or (iv) X1 is CR7 and X2 is O, including stereoisomers, tautomers, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting the delta isoform of PI3K, and for treating disorders mediated by lipid kinases such as inflammation, immunological, and cancer. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
摘要翻译： 式（I）和（Ib）化合物，其中（i）X1为N，X 2为S，（ii）X1为CR7，X2为S，（iii）X1为N，X2为NR2，或（iv）X1为CR7， X 2为O，包括立体异构体，互变异构体，代谢物及其药学上可接受的盐，可用于抑制PI3K的δ同种型，以及用于治疗由脂质激酶如炎症，免疫学和癌症介导的病症。 公开了使用式I化合物在体外，原位和体内诊断，预防或治疗哺乳动物细胞或相关病理状况中的这种病症的方法。
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