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Derivatives of 1-amino-2-cyclobutylethylboronic acid

  • US 20100081633A1
  • Filed: 09/25/2009
  • Published: 04/01/2010
  • Est. Priority Date: 09/29/2008
  • Status: Active Grant
First Claim
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1. A compound of formula (I):

  • or a pharmaceutically acceptable salt or boronic acid anhydride thereof, wherein;

    A is 0, 1, or 2;

    P is hydrogen or an amino-group-blocking moiety;

    Ra1 is C1-6 aliphatic, C1-6 fluoroaliphatic, —

    (CH2)m

    CH2

    RB, —

    (CH2)m

    CH2

    NHC(═

    NR4)NH—

    Y, —

    (CH2)m

    CH2

    CON(R4)2, —

    (CH2)m

    CH2

    N(R4)CON(R4)2, —

    (CH2)m

    CH(R6)N(R4)2, —

    (CH2)m

    CH(R5)—

    OR5, or —

    (CH2)m

    CH(R5)—

    SR5;

    each Ra2 independently is hydrogen, C1-6 aliphatic, C1-6 fluoroaliphatic, —

    (CH2)m

    CH2

    RB, —

    (CH2)m

    CH2

    NHC(═

    NR4)NH—

    Y, —

    (CH2)m

    CH2

    CON(R4)2, —

    (CH2)m

    CH2

    N(R4)CON(R4)2, —

    (CH2)m

    CH(R6)N(R4)2, —

    (CH2)m

    CH(R5)—

    OR5, or —

    (CH2)m

    CH(R5)—

    SR5;

    each Y independently is hydrogen, —

    CN, —

    NO2, or —

    S(O)2

    R10 each RB independently is a substituted or unsubstituted mono- or bicyclic ring system;

    each R4 independently is hydrogen or a substituted or unsubstituted aliphatic, aryl, heteroaryl, or heterocyclyl group;

    or two R4 on the same nitrogen atom, taken together with the nitrogen atom, form a substituted or unsubstituted 4- to 8-membered heterocyclyl ring having, in addition to the nitrogen atom, 0-2 ring heteroatoms independently selected from N, O, and S;

    each R5 independently is hydrogen or a substituted or unsubstituted aliphatic, aryl, heteroaryl, or heterocyclyl group;

    each R6 independently is a substituted or unsubstituted aliphatic, aryl, or heteroaryl group;

    each R10 independently is C1-6 aliphatic, C6-10 aryl, or —

    N(R4)2;

    m is 0, 1, or 2;

    Z1 and Z2 are each independently hydroxy, alkoxy, aryloxy, or aralkoxy;

    or Z1 and Z2 together form a moiety derived from a boronic acid complexing agent.

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