×

Medicinal arylethanolamine compounds

  • US 20060205790A1
  • Filed: 10/20/2003
  • Published: 09/14/2006
  • Est. Priority Date: 10/22/2002
  • Status: Abandoned Application
0
Associated Cases
0
Associated Defendants
0
Product Citations
0
Petitions
8
Forward Citations
1
Assignment
First Claim
Patent Images

1. A compound of formula (I):

  • embedded image or a salt, solvate, or physiologically functional derivative thereof, wherein;

    Ar1 is a group selected from embedded imagewherein R4 represents hydrogen, halogen, —

    (CH2)qOR7, —

    NR7C(O)R8, —

    NR7SO2R8, —

    SO2NR7R8, —

    NR7R8, —

    OC(O)R9 or OC(O)NR7R8, and R3 represents hydrogen, halogen or C1-4 alkyl;

    or R4 represents —

    NHR10 and R3 and —

    NHR10 together form a 5- or 6-membered heterocyclic ring;

    R5 represents hydrogen, halogen, —

    OR7 or —

    NR7R8;

    R6 represents hydrogen, halogen, haloC1-4alkyl, —

    OR7, —

    NR7R8, —

    OC(O)R9 or OC(O)NR7R8;

    R7 and R8 each independently represents hydrogen or C1-4 alkyl, or in the groups —

    NR7R8, —

    SO2NR7R8 and —

    OC(O)NR7R8, R7 and R8 independently represent hydrogen or C1-4 alkyl or together with the nitrogen atom to which they are attached form a 5-, 6- or 7-membered nitrogen-containing ring, R9 represents an aryl group which may be unsubstituted or substituted by one or more substituents selected from halogen, C1-4 alkyl, hydroxyl, C1-4 alkoxy or halo C1-4 alkyl; and

    q is zero or an integer from 1 to 4;

    Ar2 is a group;

    embedded image 

    wherein R11 is selected from hydrogen, C1-6alkyl, hydroxy, C1-6alkoxy, cyano, nitro, halo, C1-6haloalkyl, XCO2R16, —

    XC(O)NR15R16, —

    XNR14C(O)R15, —

    XNR14C(O)NR15R16, —

    XNR14C(O)NC(O)NR15R16, —

    XNR14SO2R15, —

    XSO2NR17R18, XSR14, XSOR14, XSO2R14, —

    XNR15R16, —

    XNR14C(O)OR15, or XNR14SO2NR15R16, or R11 is selected from —

    X-aryl, —

    X-hetaryl, or —

    X-(aryloxy), each optionally substituted by 1 or 2 groups independently selected from hydroxy, C1-6alkoxy, halo, C1-6alkyl, C1-6haloalkyl, cyano, nitro, CONR15R16, —

    NR14C(O)R15, SR14, SOR14, —

    SO2R14, —

    SO2NR17R18, —

    CO2R16, —

    NR15R16, or hetaryl optionally substituted by 1 or 2 groups independently selected from hydroxy, C1-6alkoxy, halo, C1-6alkyl, or C1-6haloalkyl;

    X is —

    (CH2)r—

    or C2-6 alkenylene;

    r is an integer from 0 to 6;

    R14 and R15 are independently selected from hydrogen, C1-6alkyl, C3-7cycloalkyl, aryl, hetaryl, hetaryl(C1-6alkyl)- and aryl(C1-6alkyl)- and R14 and R15 are each independently optionally substituted by 1 or 2 groups independently selected from halo, C1-6alkyl, C3-7 cycloalkyl, C1-6 alkoxy, C1-6haloalkyl, —

    NHC(O)(C1-6alkyl), —

    SO2(C1-6alkyl), —

    SO2(aryl), —

    CO2H, and —

    CO2(C1-4alkyl), —

    NH2, —

    NH(C1-6alkyl), aryl(C1-6alkyl)-, aryl(C2-6alkenyl)-, aryl(C2-6alkynyl)-, hetaryl(C1-6alkyl)-, —

    NHSO2aryl, —

    NH(hetarylC1-6alkyl), —

    NHSO2hetaryl, —

    NHSO2(C1-6alkyl), —

    NHC(O)aryl, or —

    NHC(O)hetaryl;

    or R14 and R15, together with the nitrogen atom to which they are bonded, form a 5-, 6- or 7-membered nitrogen—

    containing ring;

    or where R11 is —

    XNR14C(O)NR15R16, R14 and R15 may, together with the —

    NC(O)N—

    portion of the group R1 to which they are bonded, form a saturated or unsaturated ring or where R11 is —

    XNR14C(O)OR15, R14 and R15 may, together with the —

    NC(O)O—

    portion of the group R11 to which they are bonded, form a saturated or unsaturated ring;

    R16 is selected from hydrogen, C1-6alkyl and C3-7 cycloalkyl;

    or where R11 is —

    XC(O)NR15R16 or —

    XNR14C(O)NR15R16, R15 and R16 may, together with the nitrogen to which they are bonded, form a 5-, 6-, or 7-membered nitrogen containing ring;

    R17 and R18 are independently selected from hydrogen, C1-6alkyl, C3-7cycloalkyl, aryl, hetaryl, hetaryl(C1-6alkyl)- and aryl(C1-6alkyl)-, or R17 and R18,together with the nitrogen to which they are bonded, form a 5-, 6-, or 7-membered nitrogen containing ring;

    and R17 and R18 are each optionally substituted by one or two groups independently selected from halo, C1-6alkyl, and C3-7cycloalkyl, C1-6haloalkyl;

    R12 is selected from hydrogen, pyridine, C1-6alkyl, C1-6alkoxy, halo, aryl, aryl(C1-6alkyl)-, C1-6haloalkoxy, and C1-6haloalkyl;

    R13 is selected from hydrogen, hydroxy, C1-6alkyl, C1-6alkoxy, halo, aryl, aryl(C1-6alkyl)-, C1-6haloalkoxy, and C1-6haloalkyl;

    R1 and R2 are independently selected from hydrogen and C1-4 alkyl with the proviso that the total number of carbon atoms in R1 and R2 is not more than 4;

    one of R1a and R2a is selected from hydrogen and C1-4alkyl, and the other of R1a and R2a represents hydrogen or C1-4alkyl;

    m is an integer of from 1 to 3;

    n is an integer of from 1 to 4; and

    p is zero or an integer of from 1 to 3;

    and custom character represents a single or double bond.

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