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USE OF ARYL-SUBSTITUTED POLYCYCLIC AMINES AS MEDICAMENTS

  • US 20090258872A1
  • Filed: 06/23/2009
  • Published: 10/15/2009
  • Est. Priority Date: 08/16/2004
  • Status: Active Grant
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First Claim
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1. A method for the treatment of obesity which comprises administering to a patient in need of said treatment an effective amount of a compound of formula I:

  • wherein A, B, D, and G are,independently of one another, N or C(R3);

    R3 is H, F, Cl, Br, I, OH, CF3, NO2, CN, OCF3, O—

    (C1-C6)-alkyl, O—

    (C1-C4)-alkoxy-(C1-C4)-alkyl, S—

    (C1-C6)-alkyl, (C1-C6)-alkyl, (C2-C6)-alkenyl, (C3-C8)-cycloalkyl, O—

    (C3-C8)-cycloalkyl, (C3-C8)-cycloalkenyl, (C2-C6)-alkynyl, (C0-C8)-alkylene-aryl, O—

    (C0-C8)-alkylene-aryl, S-aryl, N(R4)(R5), SO2—

    CH3, COOH, COO—

    (C1-C6)-alkyl, CON(R6)(R7), N(R8)CO(R9), N(R10)SO2(R11), CO(R12), or (CR13R14)x—

    O(R15);

    R4, R5, R6, R7, R8, R10 are, independently of one another, H or (C1-C8)-alkyl;

    or, alternatively, R4 and R5, R6 and R7form, independently of one another, optionally together with the nitrogen atom to which they are bonded, a 5-6 membered ring which, apart from the nitrogen atom, may also include 1 further heteroatom-containing element selected from the group consisting of NH, N—

    (C1-C6)-alkyl, oxygen and sulfur;

    R9, R11, and R12 are, independently of one another, H, (C1-C8)-alkyl or aryl;

    R13 and R14 are, independently of one another, H or (C1-C8)-alkyl;

    R15 is H, (C1-C6)-alkyl or aryl;

    x is 0, 1, 2, 3, 4, 5 or 6;

    R1 is H, (C1-C8)-alkyl, (C3-C6)-alkenyl, or (C3-C6)-alkynyl;

    X is N(R16), O, a bond, (R17)C═

    C(R18), C≡

    C, or a group of the formula (CR19R20)y, in which one or two (CR19R20) groups may be replaced by Y;

    Y is O, S, N(R21), or C═

    O;

    R16, R17, and R18 are, independently of one another, H or (C1-C8)-alkyl;

    R19 and R20 are, independently of one another, H or (C1-C4)-alkyl;

    y is 1, 2, 3, 4, 5 or 6;

    R21 is H or (C1-C8)-alkyl;

    E is a 3-14 membered bivalent carbo- or heterocyclic ring structure having 0-4 heteroatoms selected from the group consisting of N, O and S, which ring structure may optionally have substituents selected from the group consisting of H, F, Cl, Br, l, OH, CF3, CN, OCF3, oxo, O—

    (C1-C6)-alkyl, O—

    (C1-C4)-alkoxy-(C1-C4)-alkyl, S—

    (C1-C6)-alkyl, (C1-C6)-alkyl, (C2-C6)-alkenyl, (C3-C8)-cycloalkyl, O—

    (C3-C8)-cycloalkyl, (C3-C8)-cycloalkenyl, O—

    (C3-C8)-cycloalkenyl, (C2-C6)-alkynyl, (C0-C8)-alkylene-aryl, O—

    (C0-C8)-alkylene-aryl, S-aryl, N(R22)(R23), SO2—

    CH3, CON(R24)(R25), N(R26)CO(R27), N(R28)SO2(R29), and CO(R30) and may be mono- or bicyclic, wherein E is not a tetrazol-5-yl group;

    R22, R23, R24, R25, R26, and R28 are, independently of one another, H, (C1-C8)-alkyl or aryl;

    or, alternatively, R22 and R23, R24 and R25 form, independently of one another, optionally together with the nitrogen atom to which they are bonded, a 5-6 membered ring which, apart from the nitrogen atom, may also include 1 further heteroatom-containing radical selected from the group consisting of NH, N—

    (C1-C6)-alkyl, oxygen and sulfur;

    R27, R29 and R30 are, independently of one another, H, (C1-C8)-alkyl or aryl;

    K is a bond, C≡

    C, (R31)C═

    C(R32), or a group of the formula (CR33R34), in which one or more (CR33R34) groups may be replaced by Z;

    R31, R32, R35, R36, R37, R38, and R39 are, independently of one another, H or (C1-C8)-alkyl;

    Z is O, S, N(R40), CO, SO, or SO2;

    R33 and R34 are, independently of one another, H, (C1-C8)-alkyl, hydroxy-(C1-C4)-alkyl, hydroxy, or (C1-C4)-alkoxy-(C1-C4)-alkyl;

    z is 1, 2, 3, 4, 5 or 6;

    R40 is H or (C1-C8)-alkyl;

    R2 is H, (C1-C8)-alkyl, (C1-C8)-alkoxy-(C1-C4)-alkyl, (C3-C8)-alkenyl, (C3-C8)-alkynyl, or a 3 to 10-membered mono-, bi-, tri- or spirocyclic ring which may include 0 to 4 heteroatoms selected from the group consisting of oxygen, nitrogen and sulfur, wherein the ring system may additionally be substituted with one or more of the following substituents;

    F, Cl, Br, CF3, NO2, CN, (C1-C6)-alkyl, O—

    (C1-C8)-alkyl, (C1-C4)-alkoxy-(C1-C4)-alkyl, (C0-C8)-alkylene-aryl, oxo, CO(R41), CON(R42)(R43), hydroxy, COO(R44), N(R45)CO(C1-C6)-alkyl, N(R46)(R47), SO2CH3, SCF3 and S—

    (C1-C6)-alkyl, and wherein R2 is not a tetrazol-5-yl group;

    R41, R42, R43, R44, R45, R46, and R47 are, independently of one another, H or (C1-C8)-alkyl;

    or, alternatively, R42 and R43, R46 and R47 form, independently of one another, optionally together with the nitrogen atom to which they are bonded, a 5-6 membered ring which, apart from the nitrogen atom, may also include 1 further heteroatom-containing radical selected from the group consisting of NH, N—

    (C1-C6)-alkyl, oxygen and sulfur;

    E, K and R2 together form a tricyclic system wherein the rings may be, independently of one another, saturated, partially saturated or unsaturated and, in each case, comprise 3-8 ring atoms;

    L is a (CR48R49)m group in which one or more (CR48R49) groups may be replaced by M;

    M is O;

    m is 1, 2, 3, 4, 5, or 6, R48, and R49, are, independently of one another, H, (C1-C6)-alkyl, or aryl; and

    Q is selected from the following structures;

    or an N-oxide thereof or a physiologically tolerated salt thereof.

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