公开(公告)号：US20060135589A1

公开(公告)日：2006-06-22

申请号：US10524784

申请日：2003-08-08

申请人： Valerio Berdino ,  Alessandro Padova ,  Paul Wyatt ,  Gordon Saxty ,  Alison Woolford

发明人： Valerio Berdino ,  Alessandro Padova ,  Paul Wyatt ,  Gordon Saxty ,  Alison Woolford

IPC分类号： A61K31/416

CPC分类号： C07D231/56 ,  C07D401/12 ,  C07D403/12 ,  C07D405/04 ,  C07D405/12 ,  C07D409/04 ,  C07D413/04 ,  C07D413/12 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14

摘要： The invention provides a compound of the formula (I) for use in the prophylaxis or treatment of a disease state or condition mediated by a cyclin dependent kinase: wherein A is a group R2 or CH2—R2 where R2 is a carbocyclic or heterocyclic group having from 3 to 12 ring members; B is a bond or an acyclic linker group having a linking chain length of up to 3 atoms selected from C, N, S and O; R1 is hydrogen or a group selected from SO2Rb, SO2NR7R8, CONR7R8, NR7R9 and carbocyclic and heterocyclic groups having from 3 to 7 ring members; R3, R4, R5 and R6 are the same or different and are each selected from hydrogen, halogen, hydroxy, trifluoromethyl, cyano, nitro, carboxy, amino, carbocyclic and heterocyclic groups having from 3 to 12 ring members; a group Ra—Rb wherein Ra is a bond, O, CO, X1C(X2), C(X2)X1, X1C(X2)X1, S, SO, SO2, NRc, SO2NRc or NRcSO2; and Rb is selected from hydrogen, carbocyclic and heterocyclic groups having from 3 to 12 ring members, and a C1-8 hydrocarbyl group optionally substituted by one or more substituents selected from hydroxy, oxo, halogen, cyano, nitro, amino, mono- or di-C1-4 hydrocarbylamino, carbocyclic and heterocyclic groups having from 3 to 12 ring members and wherein one or more carbon atoms of the C1-8 hydrocarbyl group may optionally be replaced by O, S, SO, SO2, NRc, X1C(X2), C(X2)X1 or X1C(X2)X1; Rc is hydrogen or C1-4 hydrocarbyl; X1 is O, S or NRc and X2 is ═O, ═S or ═NRc; R7 is selected from hydrogen and a C1-8 hydrocarbyl group optionally substituted by one or more substituents selected from hydroxy, oxo, halogen, cyano, nitro, amino, mono- or di-C1-4 hydrocarbylamino, carbocyclic and heterocyclic groups having from 3 to 12 ring members and wherein one or more carbon atoms of the C1-8 hydrocarbyl group may optionally be replaced by O, S, SO, SO2, NRc, X1C(X2), C(X2)X1 or X1C(X2)X1; R8 is selected from R7 and carbocyclic and heterocyclic groups having from 3 to 12 ring members; R9 is selected from R8, COR8 and SO2R8; or NR7R8 or NR7R9 may each form a heterocyclic group having from 5 to 12 ring members; but excluding the compounds N-[(morpholin-4-yl)phenyl-1H-indazole-3-carboxamide and N-[4-(acetylaminosulphonyl)phenyl-1H-indazole-3-carboxamide.

公开(公告)号：US20050124620A1

公开(公告)日：2005-06-09

申请号：US10962085

申请日：2004-10-08

申请人： Martyn Frederickson ,  Adrian Gill ,  Alessandro Padova ,  Miles Congreve

发明人： Martyn Frederickson ,  Adrian Gill ,  Alessandro Padova ,  Miles Congreve

IPC分类号： A61K31/404 ,  C07D209/08 ,  C07D401/06 ,  C07D401/14 ,  C07D403/04 ,  C07D403/06 ,  C07D403/12 ,  C07D471/02 ,  C07D487/02 ,  A61K31/53 ,  A61K31/519

CPC分类号： C07D401/06 ,  A61K31/404 ,  C07D209/08 ,  C07D401/14 ,  C07D403/06 ,  C07D403/12 ,  Y02A50/411

摘要： Compounds are disclosed of the formula (I): in which U, T, V and W are each a nitrogen atom or carbon atom. When U, T, V or W is a carbon atom, it may be substituted. The compounds are inhibitors of p38 MAP kinase and are useful for treating inflammatory diseases such as arthritis. An example of such a compound is:

摘要翻译： 公开了式（I）的化合物：其中U，T，V和W各自为氮原子或碳原子。 当U，T，V或W为碳原子时，它可以被取代。 这些化合物是p38 MAP激酶的抑制剂，可用于治疗炎性疾病如关节炎。 这种化合物的一个例子是：

公开(公告)号：US20060063782A1

公开(公告)日：2006-03-23

申请号：US10519922

申请日：2003-07-03

申请人： Christopher Murray ,  Michael Hartshorn ,  Martyn Frederickson ,  Miles Congreve ,  Alessandro Padova ,  Steven Woodhead ,  Adrian Gill ,  Andrew Woodhead

发明人： Christopher Murray ,  Michael Hartshorn ,  Martyn Frederickson ,  Miles Congreve ,  Alessandro Padova ,  Steven Woodhead ,  Adrian Gill ,  Andrew Woodhead

IPC分类号： A61K31/4965 ,  C07D213/63 ,  A61K31/44

CPC分类号： C07D213/73 ,  C07D213/65 ,  C07D213/74 ,  C07D213/81 ,  C07D241/18 ,  C07D241/20 ,  C07D241/24 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D417/12 ,  C07D417/14 ,  C07D513/04

摘要： Compounds of the formula (I), wherein: —X═Y— is selected from —CR =CR — and —CR ═N—; R is selected from H, halo, NRR′, NHC(═O)R, NHC(═O)NRR′, NH2SO2R, and C(═O)NRR′; R and R (where present) are independently selected from H, optionally substituted C1-7 alkyl, optionally substituted C5-20 aryl, optionally substituted C3-20 heterocyclyl, halo, amino, amido, hydroxy, ether, thio, thioether, acylamido, ureido and sulfonamino; R is an optionally substituted C5-20 aryl or C5-20 heteroaryl group; and R is selected from R , halo, NHR , C(═O)NHR , OR , SR , NHC(═O)R , NHC(═O)NHR , NHS(═O)R , wherein R is H or C1-3 alkyl (optionally substituted by halo, NH2, OH, SH) are disclosed for use in therapy and for treating diseases ameliorated by inhibiting p38 MAP kinase.

摘要翻译： 式（I）的化合物，其中：-X-Y-选自-CR 2 = CR 3 - 和-CR 2 -N-; R 1选自H，卤素，NRR'，NHC（-O）R，NHC（-O）NRR'，NH 2 SO 2 R和C（-O）NRR'; R 2和R 3（如果存在）独立地选自H，任选取代的C 1-7烷基，任选取代的C 5-20芳基，任选取代的C 3-20杂环基，卤素，氨基，酰胺基，羟基，醚， 硫代，硫醚，酰氨基，脲基和磺氨基; R 4是任选取代的C 5-20芳基或C 5-20杂芳基; R 5选自R 5，卤素，NHR 5，C（O）NHR 5，OR 5，SR 5，NHC（-O） R 5，NHC（-O）NHR 5，NHS（-O）R 5，其中R 5'是H或C 1-3烷基（任选地被卤素，NH 2，OH ，SH）被公开用于治疗和治疗通过抑制p38 MAP激酶而改善的疾病。