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Compounds useful to treat retroviral infections

  • US 6,169,181 B1
  • Filed: 11/09/1998
  • Issued: 01/02/2001
  • Est. Priority Date: 05/06/1994
  • Status: Expired due to Term
First Claim
Patent Images

1. A compound of the formula I wherein R1 is H—

  • ;

    wherein R2 isa) C3-C5 alkyl, b) phenyl-(CH2)2

    , c) het-SO2NH—

    (CH2)2

    , d) cyclopropyl-(CH2)2

    , e) F-phenyl-(CH2)2

    , f) het-SO2NH-phenyl-, or g) F3C—

    (CH2)2

    ;

    or wherein R1 and R2 taken together are a double bond;

    wherein R3 is the moiety of formula X wherein R4 isa) phenyl, b) het, c) cyclopropyl, d) H3C—

    [O(CH2)2]2

    , e) het-SO2NH—

    , f) Br—

    , g) N3

    , or h) HO3S(CH2)2

    N(CH3)—

    C(O)—

    (CH2)6

    C(O)—

    NH—

    ;

    wherein R5 is —

    H;

    wherein R6 isa) R4

    (CH2)n

    CH(R8)—

    , b) H3C—

    [O(CH2)2]2

    CH2

    , c) C3-C5 alkyl, d) phenyl-(CH2)2

    , e) het-SO2NH—

    (CH2)2

    , f) (HOCH2)3C—

    NH—

    C(O)—

    NH—

    (CH2)3

    , g) (HO2C)(H2N)CH—

    (CH2)2

    C(O)—

    NH—

    (CH2)3

    , h) piperazin-1-yl-C(O)—

    NH—

    (CH2)3, i) HO3S(CH2)2

    N(CH3)—

    C(O)—

    (CH2)6

    C(O)—

    NH—

    (CH2)3

    , j) cyclopropyl-(CH2)2

    , k) F-phenyl-(CH2)2

    , l) het-SO2NH-phenyl, or m) F3C—

    (CH2)2

    ;

    wherein n is zero (0), one (1) or two (2);

    wherein R7 isa) cyclopropyl, b) CH3

    CH2

    , or c) t-butyl;

    wherein R8 isa) —

    CH2

    CH3, or b) —

    CH2-cyclopropyl;

    wherein R9 isa) —

    NR12SO2-het, b) —

    NR12SO2-phenyl substituted by zero (0) or one (1) R11, c) —

    CH2

    SO2-phenyl substituted by zero (0) or one (1) R1 1, or d) —

    CH2

    SO2-het;

    wherein het is pyridinyl, imidazolyl, benzimidazolyl, quinolinyl, pyrimidinyl, pyrazinyl, pyrazolyl, thiazolyl, purinyl, tetrahydropyranyl or quinazolinyl;

    substituted by zero (0) or one (1) R10;

    wherein R10 isa) —

    CH3, b) —

    CN, c) —

    OH, d) —

    C(O)OC2H5, e) —

    CF3, f) —

    NH2, or g) —

    C(O)—

    NH2;

    wherein R11 isa) —

    CN, b) —

    F, c) —

    OH, or d) —

    NO2;

    wherein R12 isa) —

    H, or b) —

    CH3;

    or a pharmaceutically acceptable salt thereof.

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