发明名称 Nicotinamide derivates useful as p38 inhibitors
摘要 Described is a compound of formula (I) and its use in the manufacture of a medicament to treat a disease state mediated by p38 kinase activity. R1 is selected from hydrogen, C1-6 alkyl optionally substituted, C2-6 alkenyl, C3-7 cycloalkyl and heteroaryl optionally substituted; R2 is selected from hydrogen, C1-6 alkyl and -(CH2)q-C3-7 cycloalkyl optionally substituted, or (CH2)mR1 and R2, together with the nitrogen atom to which they are bound, form a four- to six-membered heterocyclic ring optionally substituted; R3 is chloro or methyl; R4 is the group -NH-CO-R7 or CO-NH-(CH2)q-R8; X and Y are each independently selected from hydrogen, methyl and halogen; Z is halogen; m is selected from 0, 1, 2, 3 and 4; and n is selected from 0, 1 and 2. Also disclosed are the following processes for the preparation of the compound: (a) reacting a compound of formula (II) with a compound of formula (III); or (b) reacting a compound of formula (VIII) with a compound of formula (II) and then reacting the acid formed with an amine of formula (V); or (c) reacting a compound of formula (II) with a compound of formula (IX) in the presence of a catalyst.
申请公布号 NZ533865(A) 申请公布日期 2006.02.24
申请号 NZ20030533865 申请日期 2003.02.10
申请人 SMITHKLINE BEECHAM CORPORATION 发明人 BAMBOROUGH, PAUL;ASTON, NICOLA MARY;WALKER, ANN LOUISE
分类号 A61K;A61K31/443;A61K31/4436;A61K31/4439;A61K31/444;A61K31/496;A61P;A61P3/10;A61P7/02;A61P9/10;A61P11/00;A61P11/02;A61P11/04;A61P11/06;A61P11/08;A61P13/12;A61P17/02;A61P17/04;A61P17/06;A61P19/00;A61P19/02;A61P19/04;A61P19/06;A61P19/08;A61P19/10;A61P21/00;A61P25/00;A61P25/04;A61P25/08;A61P25/14;A61P25/16;A61P25/28;A61P27/14;A61P29/00;A61P31/00;A61P31/04;A61P31/06;A61P31/18;A61P33/02;A61P33/06;A61P35/00;A61P37/06;A61P37/08;A61P39/02;A61P43/00;C07D;C07D213/82;C07D401/12;C07D401/14;C07D405/12;C07D409/12;C07D417/12;(IPC1-7):C07D213/82;A61K31/441;A61K31/442 主分类号 A61K
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