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US 2001/0034348 A1Published application
6-phenylpyridyl-2-amine derivatives
AssigneePfizer Inc.
InventorsJohn A. Lowe III, Peter J. Whittle
Life of this patent
Estimating the term…
Abstract
The present invention relates to certain 6-phenyi-pyridin-2-ylamine derivatives 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 disorders.
Claims12
A compound of the formula
- 10
- and the pharmaceutically acceptable salts thereof, wherein
- R1 and R2 are selected, independently, from (C1-C6) alkyl, tetrahydronaphthalene and aralkyl, wherein the aryl moiety of said aralkyl is phenyl or naphthyl and wherein said (C1-C6) alkyl or said tetrahydronaphthalene group or the aryl ring of said aralkyl group may optionally be substituted with from one to three substituents, that are selected, independently, from halo, 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, piperidine and pyrrolidine rings may optionally be substituted with one or more substituents, preferably with from zero to two substituent that are selected, independently, from (C1-C6) alkyl, amino, (C1-C6) alkylamino, [di-(C1-C6) alkyll 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 that are selected, independently, from halo, (C1-C3)alkyl, (C1-C3)alkoxy, nitro, amino, cyano, CF3 and OCF3;
- n is 0,1 or 2;
- m is 0, 1 , or 2;
- each R8 and each R9 is selected, independantly, from (C1-C4)alkyl wherein said aryl is selcected from phenyl and naphthyl;
- alikyl and phenallyl;
- X and Y are selected, independently, from methyl, methony hydroxy and hydrogon;
- and
- R10 is (C1-C5) alkyl;
- with the proviso that R1 is absent when N is zero and R9 is absent when M is zero.
- or a pharmaceutically acceptable salt of such compound.
11 more elements
Dependencies are inferred from the claim text.