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公开(公告)号:US20050288299A1
公开(公告)日:2005-12-29
申请号:US11107027
申请日:2005-04-15
申请人: Babu Mavunkel , John Perumattam , Qing Lu , Sundeep Dugar , Bindu Goyal , Dan Wang , Sarvajit Chakravarty , Gregory Luedtke , Imad Nashashibi , Richland Tester , Xuefei Tan
发明人: Babu Mavunkel , John Perumattam , Qing Lu , Sundeep Dugar , Bindu Goyal , Dan Wang , Sarvajit Chakravarty , Gregory Luedtke , Imad Nashashibi , Richland Tester , Xuefei Tan
IPC分类号: A61K31/496 , A61K31/56 , A61K39/395 , A61K45/06 , C07D471/04 , A61K31/454 , C07D487/02 , C07D43/02
CPC分类号: C07D471/04 , A61K31/496 , A61K31/56 , A61K39/395 , A61K45/06 , Y02A50/412 , A61K2300/00
摘要: The invention is directed to methods to inhibit p38 kinase, preferably p38-α using compounds which are azaindoles wherein the azaindoles are coupled through a piperidine or piperazine type linker to another cyclic moiety.
摘要翻译: 本发明涉及使用氮杂吲哚化合物抑制p38激酶,优选p38-α的方法,其中所述氮杂吲哚通过哌啶或哌嗪型连接体偶联至另一个环状部分。
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公开(公告)号:US20070232617A1
公开(公告)日:2007-10-04
申请号:US11752255
申请日:2007-05-22
申请人: Sarvajit Chakravarty , Sundeep Dugar , Qing Lu , Gregory Luedtke , Babu Mavunkel , John Perumattam , Richard Tester
发明人: Sarvajit Chakravarty , Sundeep Dugar , Qing Lu , Gregory Luedtke , Babu Mavunkel , John Perumattam , Richard Tester
IPC分类号: A61K31/497 , A61K31/445 , C07D401/02 , C07D403/02
CPC分类号: C07D401/06 , C07D209/18 , C07D209/42 , C07D401/14 , C07D403/06 , C07D409/12 , C07D409/14
摘要: The invention is directed to methods to inhibit p38-α kinase using compounds comprising a phenyl or thienyl coupled through a piperidine or piperazine nucleus to an indole residue wherein the indole residue mandatorily has a substituent on the ring nitrogen which is an amino or substituted amino group.
摘要翻译: 本发明涉及使用包含通过哌啶或哌嗪核连接的苯基或噻吩基的化合物与吲哚残基一起抑制p38-α激酶的方法,其中吲哚残基在作为氨基或取代的氨基的环氮上强制取代基 。
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公开(公告)号:US20070161649A1
公开(公告)日:2007-07-12
申请号:US11689418
申请日:2007-03-21
申请人: Babu Mavunkel , Sarvajit Chakravarty , John Perumattam , Sundeep Dugar , Qing Lu , Xi Liang
发明人: Babu Mavunkel , Sarvajit Chakravarty , John Perumattam , Sundeep Dugar , Qing Lu , Xi Liang
IPC分类号: A61K31/496 , A61K31/454 , C07D403/02
CPC分类号: C07D209/24 , C07D401/06 , C07D401/14 , C07D403/06 , C07D403/14 , C07D405/14 , C07D413/14 , C07D417/14
摘要: The invention is directed to methods to inhibit p38-α kinase using compounds of the formula and the pharmaceutically acceptable salts thereof, or a pharmaceutical composition thereof, wherein represents a single or double bond; one Z2 is CA or CR8A and the other is CR1, CR12, NR6 or N wherein each R1, R6 and R8 is independently hydrogen or noninterfering substituent; A is —Wi—COXjY wherein Y is COR2 or an isostere thereof and R2 is hydrogen or a noninterfering substituent, each of W and X is a spacer of 2-6 Å, and each of i and j is independently 0 or 1; Z3 is NR7 or O; each R3 is independently a noninterfering substituent; n is 0-3; each of L1 and L2 is a linker; each R4 is independently a noninterfering substituent; m is 0-4; Z1 is CR5 or N wherein R5 is hydrogen or a noninterfering substituent; each of 1 and k is an integer from 0-2 wherein the sum of 1 and k is 0-3; Ar is an aryl group substituted with 0-5 noninterfering substituents, wherein two noninterfering substituents can form a fused ring; and the distance between the atom of Ar linked to L2 and the center of the α ring is 4.5-24 Å.
摘要翻译: 本发明涉及使用下式的化合物及其药学上可接受的盐或其药物组合物抑制p38-α激酶的方法,其中表示单键或双键; 一个Z 2是CA或CR 8 A,另一个是CR 1,CR 1,2, 其中每个R 1,R 6和R 8独立为氢,NR 6,N 6, 或非干扰取代基; A是其中Y是COR 2或其等同体和R 2的-Wi-i-X 氢或非干扰取代基,W和X各自为2-6的间隔基,i和j各自独立地为0或1; Z 3是NR 7或O; 每个R 3独立地是非干扰取代基; n为0-3; L 1和L 2各自为连接体; 每个R 4独立地是非干扰取代基; m为0-4; Z 1是CR 5或N,其中R 5是氢或非干扰取代基; 1和k中的每一个是0-2的整数,其中1和k之和为0-3; Ar是被0-5个非直链取代基取代的芳基,其中两个非干扰取代基可以形成稠环; 并且与L 2连接的Ar原子和α环的中心之间的距离为4.5-24埃。
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公开(公告)号:US20050065344A1
公开(公告)日:2005-03-24
申请号:US10618573
申请日:2003-07-11
申请人: Babu Mavunkel , John Perumattam , Richland Tester , Sundeep Dugar
发明人: Babu Mavunkel , John Perumattam , Richland Tester , Sundeep Dugar
IPC分类号: C07C239/20 , C07D215/12
CPC分类号: C07C239/20
摘要: Improved reagents and methods of amination are provided. The reagents are phenyl hydroxylamines containing one nitro and at least one CF3 substituent on the phenyl moiety.
摘要翻译: 提供改进的试剂和胺化方法。 试剂是苯基部分上含有一个硝基和至少一个CF 3取代基的苯基羟胺。
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公开(公告)号:US20070185112A1
公开(公告)日:2007-08-09
申请号:US11688234
申请日:2007-03-19
申请人: Babu Mavunkel , Sundeep Dugar , Gregory Luedtke , Glenn McEnroe , Xuefei Tan
发明人: Babu Mavunkel , Sundeep Dugar , Gregory Luedtke , Glenn McEnroe , Xuefei Tan
IPC分类号: A61K31/53 , A61K31/519 , A61K31/506 , A61K31/497 , A61K31/496 , C07D403/02 , C07D487/02
CPC分类号: C07D207/416 , C07D211/18 , C07D401/06 , C07D471/04 , C07D513/04
摘要: Piperazine compounds and methods for treating conditions mediated by p38-α kinase are disclosed.
摘要翻译: 公开了哌嗪化合物和治疗由p38-α激酶介导的病症的方法。
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公开(公告)号:US06696443B2
公开(公告)日:2004-02-24
申请号:US09990184
申请日:2001-11-20
申请人: Babu Mavunkel , Sundeep Dugar , Gregory Luedtke , Xuefei Tan , Glenn McEnroe
发明人: Babu Mavunkel , Sundeep Dugar , Gregory Luedtke , Xuefei Tan , Glenn McEnroe
IPC分类号: C07D40106
CPC分类号: C07D207/416 , C07D211/18 , C07D401/06 , C07D471/04 , C07D513/04
摘要: Certain compounds which contain a piperidine moiety flanked by aryl groups are inhibitors of p38-&agr; kinase and thus useful in the treatment of a variety of conditions characterized by inappropriate p38-&agr; kinase activity.
摘要翻译: 含有侧翼为芳基的哌啶部分的某些化合物是p38-α激酶的抑制剂,因此可用于治疗以不适当的p38-α激酶活性为特征的多种病症。
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