公开(公告)号：US20050080258A1

公开(公告)日：2005-04-14

申请号：US10495885

申请日：2002-11-20

申请人： Jeremy Davis ,  Barry Langham ,  Manisha Naik ,  Daniel Brookings ,  Rachel Cubbon ,  Richard Franklin

发明人： Jeremy Davis ,  Barry Langham ,  Manisha Naik ,  Daniel Brookings ,  Rachel Cubbon ,  Richard Franklin

IPC分类号： A61P29/00 ,  C07D401/04 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/02 ,  C07D41/04 ,  C07D43/04

CPC分类号： C07D401/04 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/04 ,  C07D413/14

摘要： Compounds of formula (1) are described in which Ra and Rb is each independently a hydrogen atom or a group Rc, or Ra and Rb together form an oxo (═O) or thio (═S) group; X is a N atom or an optionally substituted CH group: Y is a —O— or —S— atom or —SO— or —SO2— group or an optionally substituted —CH2— or —NH— group with the proviso that when Ra and Rb together form an oxo (═O) or thio (═S) group Y is an optionally substituted —CH2— or —NH-group; L1 is a covalent bond or a linker atom or group; p is zero or the integer 1; Alk1 is an optionally substituted C1-10aliphatic or C1-10heteroaliphatic chain; n is zero the integer 1, 2 or 3 with the proviso that when n is zero Y is an optionally substituted —CH2— group: Ar is an optionally substituted C6-12aromatic or C1-9heteroaromatic group; m is zero or the integer 1, 2 or 3; q is zero or the integer 1 or 2; R1, Rc and Rd are hydrogen atoms or the substituents described in the patent specification; and the salts, solvates, hydrates and N-oxides thereof. The compounds are potent and selective inhibitors of p38 kinase and are useful in the treatment of immune or inflammatory disorders.

摘要翻译： 描述式（1）的化合物，其中R 5'和R b各自独立地为氢原子或基团R c，或者R 5'和R b一起形成氧代（= O ）或硫代（= S）基团; X是N原子或任选取代的CH基团：Y是-O-或-S-原子或-SO-或-SO 2 - 基团或任选取代的-CH 2 - 或-NH-基团，条件是当R （= O）或硫代（= S）基团Y是任选取代的-CH 2 - 或-NH-基团; L 1是共价键或连接原子或基团; p为零或整数1; Alk 1是任选取代的C 1-10脂族或C 1-10脂族链; n为整数1,2或3，条件是当n为零时Y为任选取代的-CH 2 - 基团：Ar为任选取代的C 6-12芳族或C 1-10杂芳族基团; m为零或整数1,2或3; q为零或整数1或2; R 1，R c和R d是氢原子或专利说明书中描述的取代基; 及其盐，溶剂合物，水合物和N-氧化物。 这些化合物是p38激酶的有效和选择性抑制剂，可用于治疗免疫或炎症性疾病。

公开(公告)号：US07323464B2

公开(公告)日：2008-01-29

申请号：US10495885

申请日：2002-11-20

申请人： Jeremy Martin Davis ,  Barry John Langham ,  Manisha Naik ,  Daniel Christopher Brookings ,  Rachel Jane Cubbon ,  Richard Jeremy Franklin

发明人： Jeremy Martin Davis ,  Barry John Langham ,  Manisha Naik ,  Daniel Christopher Brookings ,  Rachel Jane Cubbon ,  Richard Jeremy Franklin

IPC分类号： C07D403/04 ,  A61K31/506

CPC分类号： C07D401/04 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/04 ,  C07D413/14

摘要： Compounds of formula (1) are described in which Ra and Rb is each independently a hydrogen atom or a group Rc, or Ra and Rb together form an oxo (═O) or thio (═S) group; X is a N atom or an optionally substituted CH group: Y is a —O— or —S— atom or —SO— or —SO2— group or an optionally substituted —CH2— or —NH— group with the proviso that when Ra and Rb together form an oxo (═O) or thio (═S) group Y is an optionally substituted —CH2— or —NH-group; L1 is a covalent bond or a linker atom or group; p is zero or the integer 1; Alk1 is an optionally substituted C1-10aliphatic or C1-10heteroaliphatic chain; n is zero the integer 1, 2 or 3 with the proviso that when n is zero Y is an optionally substituted —CH2— group; Ar is an optionally substituted C6-12aromatic or C1-9heteroaromatic group; m is zero or the integer 1, 2 or 3; q is zero or the integer 1 or 2; R1, Rc and Rd are hydrogen atoms or the substituents described in the patent specification; and the salts, solvates, hydrates and N-oxides thereof. The compounds are potent and selective inhibitors of p38 kinase and are useful in the treatment of immune or inflammatory disorders.

摘要翻译： 描述式（1）的化合物，其中R a和R b各自独立地为氢原子或基团R c，或R （-O）或硫代（-S）基团一起形成一个或多个， X是N原子或任选取代的CH基团：Y是-O-或-S-原子或-SO-或-SO 2 - 基团或任选取代的-CH 2 或-NH-基团，条件是当R a a和R b一起形成氧代（-O）或硫代（-S）基团Y 是任选取代的-CH 2 - 或-NH-基团; L 1是共价键或连接子原子或基团; p为零或整数1; Alk 1是任选取代的C 1-10 1-10脂族或C 1-10 1-10杂脂肪族链; n为整数1,2或3，条件是当n为零时，Y为任选取代的-CH 2 - 基团; Ar是任选取代的C 6-12芳族或C 1-19杂芳族基团; m为零或整数1,2或3; q为零或整数1或2; R 1，R 2和R d是氢原子或专利说明书中所述的取代基; 及其盐，溶剂合物，水合物和N-氧化物。 这些化合物是p38激酶的有效和选择性抑制剂，可用于治疗免疫或炎症性疾病。