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公开(公告)号：US08481550B2
公开(公告)日：2013-07-09
申请号：US13216352
申请日：2011-08-24
申请人： Christopher F. Claiborne , Stephen Critchley , Courtney A. Cullis , Steven P. Langston , Hirotake Mizutani , Edward J. Olhava , Stephane Peluso , Irache Visiers , Stepan Vyskocil , Gabriel S. Weatherhead
发明人： Christopher F. Claiborne , Stephen Critchley , Courtney A. Cullis , Steven P. Langston , Hirotake Mizutani , Edward J. Olhava , Stephane Peluso , Irache Visiers , Stepan Vyskocil , Gabriel S. Weatherhead
IPC分类号： A61K31/505 , C07D239/48
CPC分类号： C07D239/42 , A61K31/53 , C07D213/56 , C07D213/69 , C07D213/74 , C07D213/81 , C07D213/82 , C07D239/36 , C07D239/48 , C07D251/18 , C07D251/48 , C07D401/04 , C07D401/06 , C07D403/04 , C07D471/04 , C07D471/08 , C07D473/30 , C07D473/34 , C07D487/04
摘要： This invention relates to compounds that inhibit E1 activating enzymes, pharmaceutical compositions comprising the compounds, and methods of using the compounds. The compounds are useful for treating disorders, particularly cell proliferation disorders, including cancers, inflammatory and neurodegenerative disorders; and inflammation associated with infection and cachexia.
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公开(公告)号：US07935694B2
公开(公告)日：2011-05-03
申请号：US12231661
申请日：2008-09-04
申请人： Christopher Blackburn , Christopher F. Claiborne , Courtney A. Cullis , Natalie A. Dales , Michael Patane , Matthew Stirling , Omar Stradella , Gabriel S. Weatherhead
发明人： Christopher Blackburn , Christopher F. Claiborne , Courtney A. Cullis , Natalie A. Dales , Michael Patane , Matthew Stirling , Omar Stradella , Gabriel S. Weatherhead
IPC分类号： A61P35/00
CPC分类号： C07D491/14 , C07D471/14 , C07D487/04 , C07D495/14
摘要： The present invention provides novel compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases.
摘要翻译： 本发明提供了可用作蛋白激酶抑制剂的新化合物。 本发明还提供包含本发明化合物的药物组合物和使用该组合物治疗各种疾病的方法。
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公开(公告)号：US20090105213A1
公开(公告)日：2009-04-23
申请号：US12231661
申请日：2008-09-04
申请人： Christopher Blackburn , Christopher F. Claiborne , Courtney A. Cullis , Natalie A. Dales , Michael Patane , Matthew Stirling , Omar Stradella , Gabriel S. Weatherhead
发明人： Christopher Blackburn , Christopher F. Claiborne , Courtney A. Cullis , Natalie A. Dales , Michael Patane , Matthew Stirling , Omar Stradella , Gabriel S. Weatherhead
IPC分类号： A61K31/55 , A61K31/397 , A61P35/00
CPC分类号： C07D491/14 , C07D471/14 , C07D487/04 , C07D495/14
摘要： The present invention provides novel compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases.
摘要翻译： 本发明提供了可用作蛋白激酶抑制剂的新化合物。 本发明还提供包含本发明化合物的药物组合物和使用该组合物治疗各种疾病的方法。
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公开(公告)号：US20120178739A1
公开(公告)日：2012-07-12
申请号：US13419663
申请日：2012-03-14
申请人： Christopher Blackburn , Christopher F. Claiborne , Courtney A. Cullis , Natalie A. Dales , Michael Patane , Matthew Stirling , Omar Stradella , Gabriel S. Weatherhead
发明人： Christopher Blackburn , Christopher F. Claiborne , Courtney A. Cullis , Natalie A. Dales , Michael Patane , Matthew Stirling , Omar Stradella , Gabriel S. Weatherhead
CPC分类号： C07D491/14 , C07D471/14 , C07D487/04 , C07D495/14
摘要： The present invention provides novel compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases.
摘要翻译： 本发明提供了可用作蛋白激酶抑制剂的新化合物。 本发明还提供包含本发明化合物的药物组合物和使用该组合物治疗各种疾病的方法。
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公开(公告)号：US20110039820A1
公开(公告)日：2011-02-17
申请号：US12903370
申请日：2010-10-13
申请人： Christopher Blackburn , Christopher F. Claiborne , Courtney A. Cullis , Natalie A. Dales , Michael Patane , Matthew Stirling , Omar Stradella , Gabriel S. Weatherhead
发明人： Christopher Blackburn , Christopher F. Claiborne , Courtney A. Cullis , Natalie A. Dales , Michael Patane , Matthew Stirling , Omar Stradella , Gabriel S. Weatherhead
CPC分类号： C07D491/14 , C07D471/14 , C07D487/04 , C07D495/14
摘要： The present invention provides novel compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases.
摘要翻译： 本发明提供了可用作蛋白激酶抑制剂的新化合物。 本发明还提供包含本发明化合物的药物组合物和使用该组合物治疗各种疾病的方法。
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公开(公告)号：US07459448B2
公开(公告)日：2008-12-02
申请号：US11242413
申请日：2005-10-03
申请人： Christopher Blackburn , Christopher F. Claiborne , Courtney A. Cullis , Natalie A. Dales , Michael Patane , Matthew Stirling , Omar Stradella , Gabriel S. Weatherhead
发明人： Christopher Blackburn , Christopher F. Claiborne , Courtney A. Cullis , Natalie A. Dales , Michael Patane , Matthew Stirling , Omar Stradella , Gabriel S. Weatherhead
IPC分类号： C07D487/04 , A61K31/55
CPC分类号： C07D491/14 , C07D471/14 , C07D487/04 , C07D495/14
摘要： The present invention provides novel compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases.
摘要翻译： 本发明提供了可用作蛋白激酶抑制剂的新化合物。 本发明还提供包含本发明化合物的药物组合物和使用该组合物治疗各种疾病的方法。
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公开(公告)号：US06921821B2
公开(公告)日：2005-07-26
申请号：US10459682
申请日：2003-06-11
申请人： Christopher Blackburn , Su-Jen Lai , Jennifer L. Che , Martin P. Maguire , Michael A. Patane , Matthew J. LaMarche , Courtney A. Cullis , James Brown , Anil Vasudevan , Jennifer C. Freeman , Mathew M. Mulhern , John K. Lynch , Ju Gao , Dariusz Wodka , Andrew J. Souers , Rajesh Iyengar , Mary Katherin Verzal , Philip R. Kym
发明人： Christopher Blackburn , Su-Jen Lai , Jennifer L. Che , Martin P. Maguire , Michael A. Patane , Matthew J. LaMarche , Courtney A. Cullis , James Brown , Anil Vasudevan , Jennifer C. Freeman , Mathew M. Mulhern , John K. Lynch , Ju Gao , Dariusz Wodka , Andrew J. Souers , Rajesh Iyengar , Mary Katherin Verzal , Philip R. Kym
IPC分类号： C07D403/14 , A61K31/453 , A61K31/4535 , A61K31/454 , A61K31/4709 , A61K31/496 , A61K31/517 , A61P3/04 , A61P3/06 , A61P3/10 , A61P5/00 , A61P15/00 , A61P25/08 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P43/00 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D451/04 , C07D205/08 , C07D239/02 , C07D401/00
CPC分类号： C07D405/14 , C07D401/14 , C07D405/12 , C07D409/14 , C07D413/14
摘要： This invention provides compounds that are antagonists of melanin concentrating hormone receptor-1 (MCH-R1). The compounds are represented by formula I: where m is zero or one, n is zero to two, Y is oxygen or —N(R9)—, R1, R2, R3, R4, R5, R9 and Ring A are defined in the specification. Coumarin and quinolone compounds where R1 and R2 together form a fused benzo ring are preferred. The invention also provides compounds of formula VI where the coumarin moiety is replaced by a quinazolinone ring. The compounds are useful for treating MCH-R1-related disorders, particularly overweight conditions including obesity.
摘要翻译： 本发明提供了作为黑色素浓缩激素受体-1（MCH-R1）的拮抗剂的化合物。 化合物由式I表示：其中m为0或1，n为0至2，Y为氧或-N（R 9） - ，R 1， R 2，R 3，R 4，R 5，R 9和R 9，和 环A在规范中定义。 其中R 1和R 2一起形成稠合苯并环的香豆素和喹诺酮化合物是优选的。 本发明还提供式VI的化合物，其中香豆素部分被喹唑啉酮环代替。 该化合物可用于治疗MCH-R1相关疾病，特别是超重状况，包括肥胖症。
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公开(公告)号：US20120142732A1
公开(公告)日：2012-06-07
申请号：US13206671
申请日：2011-08-10
申请人： Courtney A. Cullis , Krista E. Granger , Jianping Guo , Masaaki Hirose , Gang Li , Miho Mizutani , Tricia J. Vos
发明人： Courtney A. Cullis , Krista E. Granger , Jianping Guo , Masaaki Hirose , Gang Li , Miho Mizutani , Tricia J. Vos
IPC分类号： A61K31/443 , C07D413/14 , A61K31/4439 , C07D413/04 , A61K31/422 , A61K31/444 , C07D405/14 , A61K31/4545 , C07D409/14 , A61P35/00 , A61P29/00 , A61P9/00 , A61P37/08 , A61P7/02 , A61P9/12 , A61P9/04 , C07D405/04
CPC分类号： A61K31/422 , C07D405/04 , C07D405/14 , C07D409/14 , C07D413/04 , C07D413/14 , C07D417/14 , C07D471/04
摘要： This invention provides compounds of formula IA or IB: wherein HY, R1, R2, and G1, are as described in the specification. The compounds are inhibitors of VPS34 and/or PI3K and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.
摘要翻译： 本发明提供式IA或IB的化合物：其中HY，R1，R2和G1如说明书中所述。 这些化合物是VPS34和/或PI3K的抑制剂，因此可用于治疗增殖性，炎性或心血管疾病。
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公开(公告)号：US08859768B2
公开(公告)日：2014-10-14
申请号：US13206671
申请日：2011-08-10
申请人： Courtney A. Cullis , Krista E. Granger , Jianping Guo , Masaaki Hirose , Gang Li , Miho Mizutani , Tricia J. Vos
发明人： Courtney A. Cullis , Krista E. Granger , Jianping Guo , Masaaki Hirose , Gang Li , Miho Mizutani , Tricia J. Vos
IPC分类号： C07D239/02 , C07D241/02 , C07D213/22 , C07D413/00 , C07D401/00 , A61K31/505 , A61K31/44 , A61K31/42 , A61K31/422 , C07D413/14 , C07D417/14 , C07D413/04
CPC分类号： A61K31/422 , C07D405/04 , C07D405/14 , C07D409/14 , C07D413/04 , C07D413/14 , C07D417/14 , C07D471/04
摘要： This invention provides compounds of formula IA or IB: wherein HY, R1, R2, and G1, are as described in the specification. The compounds are inhibitors of VPS34 and/or PI3K and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.
摘要翻译： 本发明提供式IA或IB的化合物：其中HY，R1，R2和G1如说明书中所述。 这些化合物是VPS34和/或PI3K的抑制剂，因此可用于治疗增殖性，炎性或心血管疾病。
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