CYCLOMETALATED TRANSITION METAL COMPLEXES FOR MULTIPLEX ANALYTE DETECTION
申请人:Berkelman Thomas R.
公开号:US20100144046A1
公开(公告)日:2010-06-10
A complex containing a transition metal ion and a plurality of donor ligands each of which is fully coordinated to the transition metal ion and is either a nitrogen donor ligand or a cyclometalated donor ligand, such that at least one of the donor ligands is a cyclometalated donor ligand bears one or more reactive groups connected to at least one of the donor ligands through a linker that includes a chain of four or more atoms. The linker offers advantages that make the complex particularly effective in labeling biomolecules and in multiplex analyses.
[EN] 2,4,5-TRISUBSTITUTED THIAZOLYL DERIVATIVES AND THEIR ANTIINFLAMMATORY ACTIVITY<br/>[FR] DERIVES DE THIAZOLYL 2,4,5-TRISUBSTITUE ET ACTIVITE ANTI-INFLAMMATOIRE ASSOCIEE
申请人:JANSSEN PHARMACEUTICA NV
公开号:WO2003015776A1
公开(公告)日:2003-02-27
This invention concerns the use of a compound of formula (I), a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine and a stereochemically isomeric form thereof, wherein Z is halo; C1-6alkyl; C1-6alkyl substituted with hydroxy, carboxyl, cyano, amino, mono -or di(C1-6alkyl)amino, aminocarbonyl, mono -or di(C1-6alkyl)aminocarbonyl, C1-6alkyloxycarbonyl or C1-6alkyloxy; polyhaloC1-4alkyl; C1-4alkyloxy; cyano; amino; aminocarbonyl; mono -or di(C1-6alkyl)aminocarbonyl; C1-6alkyloxycarbonyl; C1-6alkylcarbonyloxy; H2N-S(=O)2-; mono -or di(C1-6alkyl)amino-S(=O)2; -C(=N-Rx)NRyRz; Q is an optionally substituted carbocycle or an optionally substituted heterocycle; L is substituted phenyl or an optionally substituted monocyclic 5 or 6-membered partially saturated or aromatic heterocycle or a bicyclic partially saturated or aromatic heterocycle; aryl is optionally substituted phenyl; for the manufacture of a medicament for the prevention or the treatment of diseases mediated through TNF-α and/or IL-12.
2,4,5-trisubstituded thiazolyl derivatives and their antiinflammatory activity
申请人:——
公开号:US20040254192A1
公开(公告)日:2004-12-16
This invention concerns the use of a compound of formula (I)
1
a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine and a stereochemically isomeric form thereof, wherein Z is halo; C
1-6
alkyl; C
1-6
alkyl substituted with hydroxy, carboxyl, cyano, amino, mono- or di(C
1-6
alkyl)amino, aminocarbonyl, mono- or di(C
1-6
alkyl)aminocarbonyl, C
1-6
alkyloxycarbonyl or C
1-6
alkyloxy; polyhaloC
1-4
alkyl; C
1-4
alkyloxy; cyano; amino; aminocarbonyl; mono- or di(C
1-6
alkyl)aminocarbonyl; C
1-6
alkyloxycarbonyl; C
1-6
alkylcarbonyloxy; H
2
N—S(═O)
2
—; mono- or di(C
1-6
alkyl)amino-S(═O)
2
; —C(═N—R
x
)NR
y
R
z
; Q is an optionally substituted carbocycle or an optionally substituted heterocycle; L is substituted phenyl or an optionally substituted monocyclic 5 or 6-membered partially saturated or aromatic heterocycle or a bicyclic partially saturated or aromatic heterocycle; aryl is optionally substituted phenyl; for the manufacture of a medicament for the prevention or the treatment of diseases mediated through TNF-&agr; and/or IL-12.
本发明涉及式(I)化合物的用途
1
一种 N-氧化物、一种药学上可接受的加成盐、一种季胺及其立体异构体形式,其中 Z 为卤代物;C
1-6
烷基
1-6
烷基;被羟基、羧基、氰基、氨基、单-或二(C 1-6)
1-6
烷基)氨基、氨基羰基、一或二(C 1-6
1-6
烷基)氨基羰基、C
1-6
烷氧羰基或 C
1-6
烷氧基;多卤代C
1-4
烷基
1-4
烷氧基;氰基;氨基;氨基羰基;单-或二(C 1-6)
1-6
烷基)氨基羰基;C
1-6
烷氧基羰基
1-6
烷基羰氧基
2
N-S(═O)
2
-;单或双(C
1-6
烷基)氨基-S(═O)
2
;-C(═N-R
x
) NR
y
R
z
Q 是任选取代的碳环或任选取代的杂环;L 是取代的苯基或任选取代的单环 5 或 6 元部分饱和或芳香杂环或双环部分饱和或芳香杂环;芳基是任选取代的苯基;用于制造预防或治疗通过 TNF-&agr 和/或 IL-12 介导的疾病的药物。
DONDONI, A.;DALLOCCO, T.;GALLIANI, G.;MASTELLARI, A.;MEDICI, A., TETRAHEDRON LETT., 1984, 25, N 33, 3637-3640
作者:DONDONI, A.、DALLOCCO, T.、GALLIANI, G.、MASTELLARI, A.、MEDICI, A.
DOI:——
日期:——
2,4,5-TRISUBSTITUTED THIAZOLYL DERIVATIVES AND THEIR ANTIINFLAMMATORY ACTIVITY