- Five-membered heterocyclic compounds as inhibitors of SRC family protein kinase.
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The present invention refers to novel substituted aromatic heteroaryl derivatives of formula (I). with the definitions of A, L1, L2, G, J, X and Y according to claim 1. These novel compounds are useful for the inhibition of protein kinases, particularly of the inhibition of Src family protein kinases. Methods for inhibiting kinases by contacting kinases with these novel compounds are disclosed. In another embodiment the present invention refers to pharmaceutical compositions containing these novel compounds and their use for the preparation of medicaments for treating diseases or disorders associated with unphysiological activity of kinases in the body, particularly for the treatment of cancer, immunosuppression, and osteoporosis.
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Page/Page column 14
(2008/06/13)
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- A convenient method for the preparation of primary and symmetrical N,N'-disubstituted thioureas
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A convenient process for the preparation of both primary thioureas 2 and symmetrical N,N'-disubstituted thioureas 6 based on the condensation of amine hydrohalides 5 with potassium thiocyanate has been developed. This approach tolerates sterically bulky primary amine substrates (both chiral and achiral), and the products can usually be isolated by a simple filtration of the reaction mixture. This method is an especially attractive alternative for the synthesis of thioureas when the corresponding isothiocyanates are unavailable, or difficult to prepare. It is also worth noting that a wide variety of amine hydrohalides, which are used in this procedure, are commercially available.
- Herr,Kuhler,Meckler,Opalka
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p. 1569 - 1574
(2007/10/03)
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