89682-89-3Relevant academic research and scientific papers
MODULATORS OF MITOTIC KINASES
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Page/Page column 52, (2008/12/07)
The invention relates to compounds of Formula (I), a prodrug, a polymorph, a tautomer, an enantiomer, a stereoisomer, a solvate, an N-oxide, or a pharmaceutically acceptable salt thereof: (formula should be inserted here) which have inhibitory effect on one or more protein kinases that are involved in cell mitosis.
Structure-Activity Relationships of Potent, Selective Inhibitors of Neuronal Nitric Oxide Synthase Based on the 6-Phenyl-2-aminopyridine Structure
Lowe III, John A.,Qian, Weimin,Drozda, Susan E.,Volkmann, Robert A.,Nason, Deane,Nelson, Robert B.,Nolan, Charles,Liston, Dane,Ward, Karen,Faraci, Steve,Verdries, Kim,Seymour, Pat,Majchrzak, Michael,Villalobos, Anabella,White, W. Frost
, p. 1575 - 1586 (2007/10/03)
The synthesis and structure-activity relationships of a series of 6-phenyl-2-aminopyridines that potently and selectively inhibit the neuronal isoform of nitric oxide synthase (nNOS) are described. Compound 14bi from this series exhibits potent in vivo activity in harmaline-induced cGMP formation in rat cerebellum, a functional model of nNOS inhibition, and in the PCP-induced hypermotility model in the rat. These results suggest that 14bi may be a useful reagent for evaluating potential therapeutic applications of nNOS inhibitors in the central nervous system.
2-aminopyridines containing fused ring substituents
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, (2008/06/13)
The present invention relates to 2-aminopyridine derivatives of the formula I: or pharmaceutically acceptable salts thereof, whereinA and B are each independently H, or together, A and B form a ring fused to the phenyl ring, said ring being saturated or unsaturated and containing from 5 to 7 ring member atoms, where said ring member atoms may optionally comprise from 1 to 2 heteroatoms selected independently from the group consisting of N, O or S, provided that no two adjacent ring members are heteroatoms;X is oxygen or a single bond;Y is (C1-C6)alkyl;R1 is hydrogen, (C1-C6)alkyl or a (C1-C6 alkyl) group substituted with —NR2R3 wherein R2 and R3 are either selected independently from the group consisting of H, alkyl, aryl, aralkyl or tetrahydronaphthalene, wherein said aryl group or said aryl moiety of said aralkyl group is phenyl or naphthyl, said alkyl group or said alkyl moiety of said aralkyl group contains from one to six carbon atoms and is straight-chained or branched, and said aryl group, said tetrahydronaphthalene or said aryl moiety of said aralkyl group is optionally substituted with from one to three of halogen, nitro, cyano, amino, (C1-C4)alkoxy and (C1-C4)alkylamino moieties, or R2 and R3 form, together with the nitrogen to which they are attached, a heterocyclic ring, or a cyclic or bicyclic ring which is saturated or unsaturated. The compounds of the invention have the ability to inhibit the activity of nitric oxide synthases (NOS), and hence, are useful in the treatment of diseases, conditions and disorders of the central nervous system, among others.
2-aminopyridines containing fused ring substituents
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, (2008/06/13)
The present invention relates to 2-aminopyridine derivatives of the formula wherein G, R1 and R2 are defined as in the specification, that exhibit activity as nitric oxide synthase (NOS) inhibitors, to pharmaceutical compositions containing them and to their use in the treatment and prevention of central nervous system and other disorders.
Amidine derivatives
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, (2008/06/13)
Compounds of formula (I) STR1 and acid addition salts thereof, wherein R1 is hydrogen, hydroxy, alkoxy, aryloxy, aralkoxy, heteroaryloxy or heteroaralkoxy; and one of R2, R3 and R4 is hydrogen and the others are the same or different and each is hydrogen, alkyl, aryl, aralkyl, heteroaryl or heteroaralkyl; or R2 is hydrogen and STR2 is mono- or bi-cyclic amino, inhibit enterotoxin-induced secretion into the small intestine and are, therefore, useful in treating enterotoxin induced diarrhoea in humans and scours in animals.
