×

BORONATE ESTER COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS THEREOF

  • US 20090325903A1
  • Filed: 06/16/2009
  • Published: 12/31/2009
  • Est. Priority Date: 06/17/2008
  • Status: Abandoned Application
First Claim
Patent Images

1. A compound of formula (I):

  • or a pharmaceutically acceptable salt thereof, wherein;

    A is 0, 1, or 2;

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

    Ra 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(R4)—

    OR5b, or —

    (CH2)m

    CH(R5)—

    SR5;

    Ra1 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(R5a)—

    OR5b, or —

    (CH2)m

    CH(R5)—

    SR5;

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

    (CH2)m

    CH2

    R3, —

    (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(R5a)—

    OR5b, or —

    (CH2)m

    CH(R5)—

    SR5;

    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 R5a independently is hydrogen or a substituted or unsubstituted aliphatic, aryl, heteroaryl, or heterocyclyl group;

    each R5b 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;

    Y is hydrogen, —

    CN, or —

    NO2;

    m is 0, 1, or 2; and

    Z1 and Z2 together form a moiety derived from an alpha-hydroxy carboxylic acid, wherein the atom attached to boron in each case is an oxygen atom;

    or Z1 and Z2 together form a moiety derived from a beta-hydroxy carboxylic acid, wherein the atom attached to boron in each case is an oxygen atom.

View all claims
  • 2 Assignments
Timeline View
Assignment View
    ×
    ×