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US 2003/0149017 A1Published application
2-Aminopyridines containing fused ring substituents
AssigneePfizer Inc.
InventorJohn Adams Lowe III
Life of this patent
Estimating the term…
Abstract
The present invention relates to 2-aminopyridine derivatives of the formula 1 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.
Claims9
A compound of the formula
- 8
- wherein ring A is a fused 5-7 membered saturated or unsaturated ring wherein from zero to two of the ring members are heteroatoms selected, independently, from nitrogen, oxygen and sulfur, with the proviso that no two adjecent ring menbers can both be heteroatoms;
- X is oxygen or a bond;
- n is an interger from two to six;
- and
- R1 and R2 are selected, independently, from (C1-C6) alkyl, aryl, tetrahydronaphthalene and aralkyl, wherein said aryl and the aryl moiety of said aralkyl is phenyl or naphthyl and the alkyl moiety is straight or branched and contains from 1 to 6 carbon atoms, and wherein said (C1-C6) alkyl, said aryl, said tetrahydronaphthalene and the aryl moiety of said aralkyl may optionally be substituted with from one to three substituents, preferably from zero to two substituents, that are selected, independently, from halo (eg., chloro, fluoro, bromo, iodo), nitro, hydroxy, cyano, amino, (C1-C4) alkoxy, and (C1-C4) alkylamino;
- or R1 and R2 form, together with the nitrogen to which they are attached, a piperazine, piperidine or pyrrolidine ring or an azabicyclic ring containing from 6 to 14 ring members, from 1 to 3 of which are nitrogen and the rest of which are carbon;
- and wherein said piperazine, azetidine, piperidine and pyrrolidine rings may optionally be substituted with one or more substituents, preferably with from zero to two substituents that are selected, independently, from (C1-C6)alkyl, amino, (C1-C6) alkylamino, [di-(C1-C6)alkyl]amino, phenyl substituted 5 to 6 membered heterocyclic rings containing from 1 to 4 rings nitrogen atoms, benzoyl, benzoylmethyl, benzylcarbonyl, phenylaminocarbonyl, phenylethyl and phenoxycarbonyl, and wherein the phenyl moieties of any of the foregoing substituents may optionally be substituted with one or more substituents, preferably with from zero to two substituents, that are selected, independently, from halo, (C1-C3)alkyl, (C1-C3)alkoxy, nitro, amino, cyano, CF3 and OCF3;
- also R1 or R2 may be connected onto the (CH2)n group to form a ring of from 4 to 7 members;
- and the pharmaceutically acceptable salt of such compounds.
7 more elements
Dependencies are inferred from the claim text.