- INDAZOLE GUANIDINE F1F0-ATPASE INHIBITORS AND THERAPEUTIC USES THEREOF
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The invention provides indazole guanidine compounds that inhibit F1F0-ATPase, and methods of using indazole guanidine compounds as therapeutic agents to treat medical disorders, such as an immune disorder, inflammatory condition, or cancer.
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Paragraph 00224
(2014/01/08)
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- 3-[(Imidazolidin-2-yl)imino]indazole ligands with selectivity for the α2-adrenoceptor compared to the imidazoline I1 receptor
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A series of 3-[(4,5-dihydroimidazolidin-2-yl)imino]indazoles has been synthesized as positional analogues of marsanidine, a highly selective α2-adrenoceptor ligand. Parent compound 4a and its 4-chloro (4c) and 4-methyl (4d) derivatives display α2-adrenoceptor affinity at nanomolar concentrations (Ki = 39.4, 15.9 and 22.6 nM, respectively) and relatively high α2/I1 selectivity ratios of 82, 115 and 690, respectively. Evidence was obtained that these compounds act as partial agonists at α2A-adrenoceptors. Compound 4d with intrinsic activity comparable with that of marsanidine, but lower than that of clonidine, elicited pronounced cardiovascular effects in anesthetized rats at doses as low as 0.01 mg/kg iv.
- Sczewski, Franciszek,Kornicka, Anita,Hudson, Alan L.,Laird, Shayna,Scheinin, Mika,Laurila, Jonne M.,Rybczyńska, Apolonia,Boblewski, Konrad,Lehmann, Artur,Gdaniec, Maria
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scheme or table
p. 321 - 329
(2011/02/26)
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- Rational design of potent GSK3β inhibitors with selectivity for Cdk1 and Cdk2
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From an HTS hit, a series of potent and selective inhibitors of GSK3β have been designed based on a Cdk2-homology model and with the help of several crystal structures of the compounds within Cdk2.
- Lesuisse, Dominique,Dutruc-Rosset, Gilles,Tiraboschi, Gilles,Dreyer, Matthias K.,Maignan, Sébastien,Chevalier, Alain,Halley, Frank,Bertrand, Philippe,Burgevin, Marie-Claude,Quarteronet, Dominique,Rooney, Thomas
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scheme or table
p. 1985 - 1989
(2010/08/06)
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- Simplified Synthesis of the Precursor for the Azo Dye Chlorindazone DS
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Recently, Chlorindazone DS 1 has become an important analytical reagent for the detection of gunshot residues from newly introduced ammunition. A simplified synthesis of the precursor of the azo dye 1, 3-amino-6-chloroindazole (2), from commercially available 2,4-dichlorobenzonitrile (3a) has been described. The physical and spectroscopical properties of the known compounds 1 and 2 have been completed. 2-Chloro-4-hydrazinobenzonitrile (4a), 2-bromo-4-hydrazinobenzonitrile (4b) and a new azo dye, 1-(3′-chloro-4′-cyanobenzene-1′-ylazo)-2-hydroxynaphthalene-3, 6-disulfonic acid, disodium salt (5), have been investigated.
- Voss,Eichner
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p. 201 - 204
(2007/10/03)
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- 3-Aminoindazole derivatives
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.Iadd.Pharmaceutical compositions having muscle relaxant and analgesic activity containing 3-aminoindazoles..Iaddend.
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