[EN] TRIAZOLE FUSED HETEROARYL COMPOUNDS AS P38 KINASE INHIBITORS<br/>[FR] COMPOSÉS HÉTÉROARYLIQUES FUSIONNÉS DE TRIAZOLE EN TANT QU'INHIBITEURS DE KINASE P38
申请人:AMGEN INC
公开号:WO2009038784A1
公开(公告)日:2009-03-26
The present invention comprises a new class of compounds useful for modulating the activity of p38 MAP kinase. The compounds have a general Formula (I) wherein A1, A2, A3, A4, A5, A6, R1 and R5 are defined herein. The invention further provides pharmaceutical compositions including one or more compounds of Formula (I), use of such compounds and compositions for treatment of p38 MAP kinase mediated diseases including rheumatoid arthritis, psoriasis and other inflammatory disorders, as well as intermediates and processes useful for the preparation of compounds of Formula (I).
The present invention is directed to ether benzotriazole derivatives which are potentiators of metabotropic glutamate receptors, particularly the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.
TRIAZOLE FUSED HETEROARYL COMPOUNDS AND METHODS OF USE THEREOF
申请人:Pettus Liping H.
公开号:US20100292234A1
公开(公告)日:2010-11-18
The present invention comprises a new class of compounds useful for modulating the activity of p38 MAP kinase. The compounds have a general Formula I
wherein A
1
, A
2
, A
3
, A
4
, A
5
, A
6
, R
1
and R
5
are defined herein. The invention further provides pharmaceutical compositions including one or more compounds of Formula I, use of such compounds and compositions for treatment of p38 MAP kinase mediated diseases including rheumatoid arthritis, psoriasis and other inflammatory disorders, as well as intermediates and processes useful for the preparation of compounds of Formula I.
Process for the preparation of beta-lactam compounds
申请人:BEECHAM GROUP PLC
公开号:EP0112049A1
公开(公告)日:1984-06-27
The present invention provides a process for the substitution of an acylamino β-lactam compound at the carbon atom carrying the acylamino group, which process comprises reacting the β-lactam compound with an halogenating agent and a nucleophilic reagent; characterised in that the acylamino group has an acidic group on the carbon atom adjacent the carbonyl group.
In particular the process of this invention comprises reacting a β-lactam of partial structure (I):
where X represents an acidic group; with an halogenating agent and a nucleophilic reagent.
本发明提供了一种在携带酰氨基的碳原子上取代酰氨基β-内酰胺化合物的工艺,该工艺包括使β-内酰胺化合物与卤化剂和亲核试剂反应;其特征在于酰氨基在邻近羰基的碳原子上具有酸性基团。
本发明的工艺尤其包括使部分结构为(I)的β-内酰胺反应:
其中 X 代表酸性基团;与卤化剂和亲核试剂反应。
Silver halide photographic material
申请人:FUJI PHOTO FILM CO., LTD.
公开号:EP0335319A2
公开(公告)日:1989-10-04
A silver halide photographic material composed of a support having thereon at least one silver halide photosensitive emulsion layer, at least one layer of the material containing a blocked photographic reagent precursor represented by formula (I):
wherein X1 represents a divalent linking group containing a hetero atom bonded to the carbon atom, provided that X1 is linked to the carbon atom by a group other than
PUG represents a photographically useful group containing a hetero atom bonded to X1; W represents = N- or
represents hydrogen or a group capaable of being substituted; Z represents an atomic group necessary for forming a heterocyclic ring, provided that when W represents a
group, the group adjacent to W in the heterocyclic ring is a group other than
wherein R1, R2, R3, R4 and R5 each represents hydrogen or or group capable of being substituted; and m is 0 or 1, with proviso that when m is 0, the photographically useful group represented by PUG is bonded to a carbon atom via heteroatom of PUG. The photographic materials have superior stability during storage, and are capable of releasing a photographic reagent with specifically required timing during processing, and in a wide pH range.
一种卤化银感光材料,由至少有一层卤化银感光乳剂层的支撑体组成,该材料的至少一层含有由式 (I) 表示的封端感光试剂前体:
其中 X1 代表含有与碳原子键合的杂原子的二价连接基团,但 X1 与碳原子之间的连接基团必须不是
PUG 代表含有与 X1 键合的杂原子的摄影有用基团; W 代表=N-或
代表氢或可被取代的基团;Z 代表形成杂环所需的原子团,但当 W 代表
当 W 代表一个基团时,杂环中与 W 相邻的基团是一个基团,而不是
其中 R1、R2、R3、R4 和 R5 分别代表氢或可被取代的基团;以及 m 为 0 或 1,但当 m 为 0 时,PUG 所代表的对照片有用的基团通过 PUG 的杂原子与碳原子结合。这种感光材料在贮存过程中具有优异的稳定性,在加工过程中能够按照特定要求的时间释放感光试剂,并且适用于较宽的 pH 值范围。