Pharmaceutically active sulfonyl hydrazide derivatives
1 2 1 2 123 161 12 3 16 The present invention is related to sulfonyl hydrazide derivatives for use as pharmaceutically active compounds, as well as to pharmaceutical formulations containing such sulfonyl hydrazide derivatives. Said sulfonyl hydrazide derivatives are efficient modulators of the JNK p...
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07.10.2008
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Abstract | 1 2 1 2 123 161 12 3 16 The present invention is related to sulfonyl hydrazide derivatives for use as pharmaceutically active compounds, as well as to pharmaceutical formulations containing such sulfonyl hydrazide derivatives. Said sulfonyl hydrazide derivatives are efficient modulators of the JNK pathway, they are in particular efficient inhibitors of JNK 2 and 3. The present invention is furthermore related to novel sulfonyl hydrazide derivatives as well as to methods of their preparation. In Formula (I) Arand Arare independently from each other an unsubstituted or substituted aryl or beteroaryl group, Xand Xare independently from each other O or S; R, R, Rare independently from each other hydrogen or a C-C-alkyl substituent or Rforms a substituted or unsubstituted 5-6-membered saturated or unsaturated ring with Ar; or Rand Rform a substituted or unsubstituted 5-6-membered saturated or unsaturated ring; n is an integer from 0 to 5; G is selected from a group comprising or consisting of an unsubstituted or substituted 4-8 membered heterocycle containing at least one heteroatom, or G is a substituted or unstibstituted C-C-alkyl group. |
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AbstractList | 1 2 1 2 123 161 12 3 16 The present invention is related to sulfonyl hydrazide derivatives for use as pharmaceutically active compounds, as well as to pharmaceutical formulations containing such sulfonyl hydrazide derivatives. Said sulfonyl hydrazide derivatives are efficient modulators of the JNK pathway, they are in particular efficient inhibitors of JNK 2 and 3. The present invention is furthermore related to novel sulfonyl hydrazide derivatives as well as to methods of their preparation. In Formula (I) Arand Arare independently from each other an unsubstituted or substituted aryl or beteroaryl group, Xand Xare independently from each other O or S; R, R, Rare independently from each other hydrogen or a C-C-alkyl substituent or Rforms a substituted or unsubstituted 5-6-membered saturated or unsaturated ring with Ar; or Rand Rform a substituted or unsubstituted 5-6-membered saturated or unsaturated ring; n is an integer from 0 to 5; G is selected from a group comprising or consisting of an unsubstituted or substituted 4-8 membered heterocycle containing at least one heteroatom, or G is a substituted or unstibstituted C-C-alkyl group. |
Author | Arkinstall, Stephen Rueckle, Thomas Camps, Montserrat Biamonte, Marco Gotteland, Jean-Pierre Church, Dennis Halazy, Serge |
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References | Derek D. Yang et al.: "Absence of excitotoxicity-induced apoptosis in the hippocampus of mice lacking the Jnk3 gene" Nature, 389 (6653), pp. 865-870, 1997. Yoshihiro Kumage et al.: "Human c-Jun N-terminal kinase expression and activation in the nervous system" Brain Res. Mol. Brain Res., 67 (1), pp. 10-17, 1999. Kanaga Sabapathy et al.: "JNK2 is required for efficient T-cell activation and apoptosis but not for normal lymphocyte development" Current Biology, 3, pp. 116-125, 1999. R. Raja Reddy et al.: "New hypoglycemic agents-Part XVI: synthesis and evaluation of N3-aryl-N1-′4-′(3, 4-dihydro-3-oxo-2H-1, 4-benzoxazin-2-yl) acetic acid hydrazidosulfonyllphenyll ureas/thioureas" Indian Journal of Heterocyclic Chemistry, vol. 7, No. 3, pp. 185-188. (98 49188) 19981100 Xie Xiaoling et al.: "Crystal structure of JNK3: a kinase implicated in neuronal apoptosis" Structure, 6 (8), pp. 983-991, 1998. (0 330 065) 19890800 Derek D. Yang et al.: "Differentiation of CD4+ T cells to Th1 cells requires MAP kinase JNK2" Immunity, 9, pp. 575-585, 1998. (WO 01/23378) 20010400 |
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Snippet | 1 2 1 2 123 161 12 3 16 The present invention is related to sulfonyl hydrazide derivatives for use as pharmaceutically active compounds, as well as to... |
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