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：US20080015191A1

公开(公告)日：2008-01-17

申请号：US11722612

申请日：2005-12-22

申请人： Caroline Springer ,  Ion Niculescu-Duvaz ,  Esteban Vela ,  Adrian Gill ,  Richard Taylor ,  Richard Marais

发明人： Caroline Springer ,  Ion Niculescu-Duvaz ,  Esteban Vela ,  Adrian Gill ,  Richard Taylor ,  Richard Marais

IPC分类号： A61K31/4965 ,  A61K31/497 ,  A61K31/5377 ,  A61P35/00 ,  C07D241/16 ,  C07D241/18 ,  C07D241/20 ,  C07D413/12

CPC分类号： C07D213/74 ,  C07D241/20 ,  C07D317/46 ,  C07D319/18 ,  C07D321/10 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04 ,  C07D403/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12

摘要： The present invention pertains to certain pyrazines and pyridines, and derivatives thereof, which, inter alia, inhibit RAF (e.g., B RAF) activity, inhibit cell proliferation, treat cancer, etc., and more particularly to compounds of the formulae: (I) wherein: Q is independently —N═ or —CH═; one of RP2 and RP3 is independently a group of the formula -J1-L1-Z; wherein: if Q is —N═, then -J1-L1-Z is independently: —NH-Z; —O-Z; or S-Z; if Q is —CH═, then -J1-L1-Z is independently: —NH—(CH2)n-Z, wherein n is independently 0 or 1; —O-Z; or —S-Z; Z is independently: C6-14 carboaryl, C5-14 heteroaryl, C3-12carbocyclic, C3-12 heterocyclic; and is independently unsubstituted or substituted; the other of RP2 and RP3 is independently —H, —NHRN1, or —NHC(═O)RN2; wherein: RN1, if present, is independently —H or aliphatic saturated C1-4alkyl; RN2, if present, is independently —H or aliphatic saturated C1-4alkyl; one of RP5 and RP6 is independently a group of the formula —W—Y; wherein: W is independently: a covalent bond; —NRN4—, —O—, —S—, —C(═O)—, —CH2—; —NRN4—CH2—, —O—CH2—, —S—CH2—, —C(═O)—CH2—, —(CH2)2—; —CH2—NRN4—, —CH2—O—, —CH2—S—, or —CH2—C(═O)—; wherein RN4, if present, is independently —H or aliphatic saturated C1-4alkyl; Y is independently: C6-14carboaryl, C5-14heteroaryl, C3-12carbocyclic, C3-12heterocyclic; and is independently unsubstituted or substituted; the other of RP5 and RP6 is independently —H; and pharmaceutically acceptable salts, solvates, amides, esters, ethers, N-oxides, chemically protected forms, and prodrugs thereof. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, e.g., both in vitro and in vivo, to inhibit RAF (e.g., B-RAF) activity, to inhibit receptor tyrosine kinase (RTK) activity, to inhibit cell proliferation, and in the treatment of diseases and conditions that are ameliorated by the inhibition of RAF, RTK, etc., proliferative conditions such as cancer (e.g., colorectal cancer, melanoma), etc.

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。