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    3-(2-azetidinyl-methoxy)-pyridine derivatives useful as analgesics and azetidinyl intermediates
    49.
    发明专利
    3-(2-azetidinyl-methoxy)-pyridine derivatives useful as analgesics and azetidinyl intermediates 未知

    公开(公告)号：NZ335810A

    公开(公告)日：2001-03-30

    申请号：NZ33581097

    申请日：1997-12-10

    Applicant: ABBOTT LAB

    Inventor： HOLLADAY MARK W ,  ARNERIC STEPHEN P ,  BAI HAO ,  DART MICHAEL J ,  LIN NAN-HORNG ,  LYNCH JOHN K ,  OR YAT SUN ,  RYTHER KEITH B ,  SULLIVAN JAMES P ,  WASICAK JAMES T ,  ERHLICH PAUL P

    IPC: A61P25/04 ,  A61K31/4427 ,  A61K31/443 ,  A61K31/4439 ,  A61K31/485 ,  A61P25/28 ,  A61P29/00 ,  C07D205/04 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14

    Abstract: An 3-(2-azetidinyl-methoxy)-pyridine derivative or a pharmaceutically acceptable salt thereof has the compound of formula I wherein: Z, Y, X and the 2-azetidine stereochemistry are, respectively, selected from: a) H, H, Me (R); b) H, H, CN (S); c) H, H, Cl (S); d) H, H, Cl (R); e) H, H, Br (R); f) H, H, F (S); g) H, H, F (R); h) H, H, CHF2 (S); i) H, H, OMe (R); j) H, Me, Cl (S); k) H, Me, Cl (R); l) H, Et, F (S); m) H, ethenyl, Cl (S); n) H, ethenyl, Cl (R); o) H, ethenyl, F (S); p) H, ethenyl, F (R); q) H, ethynyl, Cl (S); r) H, ethynyl, Cl (R); s) H, Cl, Cl (S); t) H, Cl, Cl (R); u) H, Cl, F (S); v) H, Br, Me (S); w) H, Br, Me (R); x) H, Br, Cl (S); y) H, Br, Cl (R); z) H, Br, F (S); aa) H, Br, F (R); bb) H, n-Pr, H (S); cc) H, ethenyl, H (S); dd) H, ethenyl, H (R); ee) H, Cl, H (R); ff) H, F, H (S); gg) H, NO2, H (S); hh) H, OEt, H (S); ii) Cl, H, H (S); jj) Cl, H, H (R); kk) F, H, H (S); ll) F, H, F (S); mm) F, H, Me (S) or nn) F, H, Me (R) and R is H or a prodrug such as methyl, ethyl, isopropyl, n-propyl, isobutyl, t-butyl, t-pentyl, n-pentyl, n-butyl, cyclohexylmethyl, 3-methyl-1-butyn-3 -yl, optionally N-protected-Ala, optionally N-protected-Phe, phthaloyl methyl ester, 4-diethylaminobenzoyl, 2-hydroxymethylbenzoyl, acetyl, t-butyloxycarbonyl, ethoxycarbonyl, phenoxycarbonyl, 4-nitrophenoxycarbonyl, 4-methoxyphenoxycarbonyl, 4-carbomethoxyphenoxycarbonyl, 4-methylphenoxycarbonyl, 4-fluorophenoxycarbonyl, 4-chlorophenoxycarbonyl, 2,6-dimethylphenoxycarbonyl, 1 -acetoxy-1-methyl-ethoxycarbonyl, benzyloxycarbonyl, pyrrolidin-1-ylcarbonyl, N-succinimidylmethyl or N-phthalimidylmethyl or a group of formula 1, 2 (where R' is H or Me), 3, 4 or 5 (where two azetidines are attached). A pharmaceutical composition thereof is useful in controlling pain in mammals. An intermediate compound of formula II is disclosed wherein: L is an anionic leaving group which may be displaced by a nucleophile and P is a nitrogen protecting group.

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