×

BICYCLIC-NITROGEN COMPOUNDS AS MODULATORS OF GHRELIN RECEPTOR AND USES THEREOF

  • US 20070213359A1
  • Filed: 12/29/2006
  • Published: 09/13/2007
  • Est. Priority Date: 12/30/2005
  • Status: Abandoned Application
First Claim
Patent Images

1. A compound of Formula (I):

  • embedded image or a solvate, a polymorph, a metabolite, or a pharmaceutically acceptable salt or prodrug thereof, wherein;

    A is selected from the group consisting of hydrogen, halogen, cyano, mono-substituted, poly-substituted or unsubstituted variants of the following residues;

    alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, cycloalkynyl, aryl, heteroaryl, heteroalicyclyl, aralkyl, heteroaralkyl, (heteroalicyclyl)alkyl, sulfinyl, sulfonyl, haloalkyl, haloalkoxy, —

    C(=Z)R1, —

    C(=Z)OR1, —

    C(=Z)NR1aR1b, —

    C(R1)═

    NR1a, —

    NR1aR1b, —

    N═

    CR1aR1b, —

    N(R1)—

    C(=Z)R1, —

    N(R1)—

    C(=Z)NR1aR1b, —

    S(O)NR1aR1b, —

    S(O)2NR1aR1b, —

    N(R1)—

    S(═

    O)R1, —

    N(R1)—

    S(═

    O)2R1, —

    OR1, —

    SR1, and —

    OC(═

    O)R1;

    B is selected from the group consisting of hydrogen;

    mono-substituted, poly-substituted or unsubstituted variants of the following residues;

    alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, cycloalkynyl, aryl, heteroaryl, heteroalicyclyl, aralkyl, heteroaralkyl, (heteroalicyclyl)alkyl, —

    C(=Z)R1, —

    C(=Z)OR1, —

    C(=Z)NR1aR1b, —

    C(=Z)N(OR1a)R1b, —

    C(=Z)N(R1)NR1aR1b, —

    C(R1)═

    NR1a, —

    C≡

    N;



    NR1aR1b, —

    N═

    CR1aR1b, —

    N(R1)—

    C(=Z)R1, —

    N(R1)—

    C(=Z)NR1aR1b, —

    S(O)NR1aR1b, —

    S(O)2NR1aR1b, —

    N(R1)—

    S(═

    O)R1, —

    N(R1)—

    S(═

    O)2R1, —

    S(O)R1, —

    S(O)2R1, —

    OR1, —

    SR1, and —

    OC(═

    O)R1;

    A and B can be taken together to form an unsubstituted or substituted cycloalkyl, or unsubstituted or substituted heteroalicyclyl;

    R1, R1a and R1b are each independently selected from the group consisting of hydrogen, mono-substituted, poly-substituted or unsubstituted variants of the following residues;

    alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, cycloalkynyl, aryl, heteroaryl, heteroalicyclyl, aralkyl, heteroaralkyl, (heteroalicyclyl)alkyl and haloalkyl;

    R2 and R2a are each independently selected from the group consisting of hydrogen, cyano, mono-substituted, poly-substituted or unsubstituted variants of the following residues;

    alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, cycloalkynyl, aryl, heteroaryl, heteroalicyclyl, aralkyl, heteroaralkyl, (heteroalicyclyl)alkyl, sulfinyl, sulfonyl, haloalkyl, —

    C(=Z)R1, —

    C(=Z)OR1, —

    C(=Z)NR1aR1b, —

    C(R1)═

    NR1a, —

    (C1-4alkyl)-Z-aryl, —

    (C1-4alkyl)C(═

    O) R1, —

    NR1aR1b, —

    N═

    CR1aR1b, —

    N(R1)—

    C(=Z)R1, —

    N(R1)—

    C(=Z)NR1aR1b, —

    S(O)NR1aR1b, —

    S(O)2NR1aR1b, —

    N(R1)—

    S(═

    O)R1, —

    N(R1)—

    S(═

    O)2R1, —

    OR1, —

    SR1, and —

    OC(=Z)R1;

    or R2 and R2a can be taken together, along with the nitrogen atom to which they are attached, to form an unsubstituted or substituted heteroalicyclyl;

    R3, R3a, R3b, and R3c are each independently selected from the group consisting of hydrogen, halogen, cyano, nitro, mono-substituted, poly-substituted or unsubstituted variants of the following residues;

    alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl cycloalkynyl, aryl, heteroaryl, heteroalicyclyl, aralkyl, heteroaralkyl, (heteroalicyclyl)alkyl, sulfinyl, sulfonyl, haloalkyl, haloalkoxy, —

    C(=Z)R1, —

    C(Z)OR1, —

    C(=Z)NR1aR1b, —

    C(R1)═

    NR1a, —

    NR1aR1b, —

    N═

    CR1aR1b, —

    N(R1)—

    C(=Z)R1, —

    N(R1)—

    C(=Z)NR1aR1b, —

    S(O)NR1aR1b, —

    S(O)2NR1aR1b, —

    N(R1)—

    S(═

    O)R1, —

    N(R1)—

    S(═

    O)2R1, —

    OR1, —

    SR1, and —

    OC(=Z)R1;

    R3, R3a, R3b, and R3c can be taken together with one or more adjacent members of the group consisting of R3, R3a, R3b, and R3c to form a cycloalkyl, cycloalkenyl, cycloalkynyl, or heteroalicyclyl ring;

    R3c can be taken together with B to form a cycloalkyl, cycloalkenyl, cycloalkynyl, or heteroalicyclyl ring;

    L can be a unsubstituted or substituted lower alkylene group, wherein when L is substituted, it is substituted with one or more group(s) individually and independently selected from the group consisting of alkyl, alkenyl, halogen, haloalkyl, alkoxy, haloalkoxy, hydroxyl, and —

    CN;

    L can be taken together with R3 to form a cycloalkyl, cycloalkenyl, cycloalkynyl, or heteroalicyclyl ring;

    Y is C—

    R3 or N; and

    Z is O or S.

View all claims
  • 1 Assignment
Timeline View
Assignment View
    ×
    ×