Pharmaceutical pyrazole compositions useful as inhibitors of pro

Details Pharmaceutical pyrazole compositions useful as inhibitors of pro Pharmaceutical pyrazole compositions useful as inhibitors of pro

1995-11-09

1999-06-29

Weber, Jon P.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

435184, 435194, A61K 31415, C12N 999, C12N 912

Patent

active

059169087

ABSTRACT:
A method for selectively inhibiting a kinase is disclosed, which comprises contacting a composition containing a kinase with a compound of the formula: ##STR1## wherein: R.sub.1 is lower alkyl, lower hydrocarbyl, aryl lower alkyl, heteroaryl lower alkyl, 5- or 6-membered heterocyclic aromatic, polyaromatic, polyaromatic carbonyl, polyheteroaromatic or polyheteroaromatic carbonyl; R.sub.2 is lower alkyl, lower hydrocarbyl, aryl lower alkyl, heteroaryl lower alkyl, 5- or 6-membered heterocyclic aromatic, lower hydrocarboyl, 5- or 6-membered heterocyclic aromatic carbonyl, polyaromatic or polyheteroaromatic; R.sub.3 is H or lower alkyl; R.sub.5 is H, lower alkyl, lower hydrocarbyl, aryl lower alkyl, heteroaryl lower alkyl, 5- or 6-membered heterocyclic aromatic, halogen, or cyano; and R.sub.6 is H or lower hydrocarboyl.

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L. Cecchi et al., "Synthesis and Reactivity of 1-Methyl-3-phenyl-4-diazo-5-benzoylamido-pyrazole. A Potential Antitumor Agent", J. Heterocyclic Chem., vol. 21, pp. 957-959 (1984).
L. Cecchi et al., "Carbon-13 NMR Study of 1-Methyl-3-phenyl-4-diazo-5-benzoylamido-pyrazole and Other Model Pyrazole Compounds", J. Heterocyclic Chem., vol. 22, pp. 951-952 (1985).
N. Velasco et al., "Calculations of Molecular Orbitals in Prototypes Derived From 5-Aminopyrazole", An. R. Acad. Farm., vol. 50(4), pp. 617-623 (1984)--Abstract Only.

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