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5-Pyrrolidinylsulfonyl Isatin Derivatives

  • US 20090041664A1
  • Filed: 12/22/2005
  • Published: 02/12/2009
  • Est. Priority Date: 01/17/2005
  • Status: Active Grant
First Claim
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1. 5-Pyrrolidinylsulfonyl isatin derivatives of the formula 1, wherein, X is —

  • O—

    , —

    S—

    or —

    NH— and

    Y is —

    CH2

    or —

    C(O)—

    ;

    R1 is an alkyl, substituted alkyl, aryl, heteroarylalkyl group, and optionally additionally comprises a spacer or linker selected from PEG1-200, an oligopeptide, polyamide, polysaccharide, —

    NHC(O)—

    ((CH2)n

    NH—

    C(O))m

    , —

    O—

    ((CH2)n-0)m

    , succinyl and 1,4-disubstituted 1,2,3-triazole units, wherein n=0-6 and m=1-200;

    R2 is an optionally substituted alkyl, heteroalkyl, aralkyl, heteroarylalkyl, carboxymethyl or methyloxycarbonylmethyl group, wherein the substituents are selected from F, I, Br, OH, NH2, methylamino, methoxy, fluoroethyloxy, fluoropropyloxy, trimethylamino, nitro, tosylate, triflate, mesylate, diazonium N2+, 3-fluorobenzoyl, 4-fluorobenzoyl, 4-fluorophenyl, tributylstannyl, trimethylstannyl, trimethylsilyl, 2-hydrazino-pyridin-5-carbonyl;

    or a metal-chelator or a metal-chelator bound to an aralkyl, aminoalkyl, hydroxyalkyl or piperazin-1-carbonylmethyl group;

    and optionally additionally comprises a spacer, linker or molecular transporter selected from Annexin V, PEG1-200, an oligopeptide, polyamide, polysaccharide, —

    NHC(O)—

    ((CH2)n

    NH—

    C(O))m

    , —

    O—

    ((CH2)n

    O)m

    , succinyl and 1,4-disubstituted 1,2,3-triazole units, wherein n=0-6 and m=1-200 and wherein R2 can also contain an amino acid selected from histidine, lysine, tyrosine, cysteine, arginine and aspartic acid.

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