Patent ID: 6683101
Filing Date: 2004-01-27
Classification: A61P,C07D

Abstract:
Heterocycle-substituted cyclohexylamines of Formula I and their pharmaceutically acceptable salts thereof: wherein:Ar is substituted 1 to 3 times or unsubstituted aryl or substituted 1 to 3 times or unsubstituted hereroaryl, which heteroaryl is from 5 to 14 atoms having from 1 to 2 heteroatoms selected from N, O, and S wherein the substituents are selected from the groups F, Cl, Br, I, OH, NH2, SH, CN, NO2, OCH3, OC(O)CH3, CF3, OCH2CH2OH, NHC(O)CH3, NHCH3, or N(CH3)2; â€”Eâ€”Yâ€” is selected from the group consisting of â€”CH&boxH;CHâ€”N(H)â€”, â€”(CH2)2â€”N(H)â€”, â€”CH&boxH;Nâ€”N(H)â€”, â€”C(O)â€”CH2â€”N(H)â€”, â€”CH2â€”C(O)N(H)â€”, â€”CH2â€”S(O)â€”N(H)â€”, â€”CH2â€”S(O)2â€”N(H)â€”, â€”CH&boxH;CHâ€”CH(OH)â€”, â€”(CH2â€”CH(OH)â€”, â€”C(O)CH2â€”C(O)â€”, â€”C(O)â€”NHâ€”C(O)â€”, â€”N&boxH;CHâ€”N(H)â€”, â€”N(H)â€”C(O)â€”N(H)â€”, â€”Oâ€”C(O)â€”NHâ€”, â€”Sâ€”C(O)NHâ€”, â€”Oâ€”N&boxH;CH(OH)â€”, â€”Sâ€”N&boxH;CH(OH)â€”â€”N&boxH;Nâ€”N(H)â€”, â€”CH&boxH;CHâ€”CH&boxH;C(OH)â€”â€”(CH2)3â€”CH(OH)â€”, â€”(CH2)2â€”S(O)N(H), â€”(CH2)2â€”S(O)2â€”N(H)â€”, â€”CH&boxH;CHâ€”C(O)â€”N(H)â€”, â€”C(O)â€”NHâ€”N&boxH;C(OH)â€”, â€”CH&boxH;Nâ€”NHâ€”C(O), â€”CH&boxH;N(O)â€”N&boxH;C(OH)â€”, â€”N(H)â€”C(O)â€”N(H)C(O)â€”, â€”N&boxH;CHâ€”C(O)NHâ€”, â€”Oâ€”CH2â€”C(O)â€”NHâ€”, â€”Sâ€”CH2â€”C(O)â€”NHâ€”, and â€”N(H)â€”C(O)C(O)â€”N(H)â€”; d is an integer from 0 to 2; n is an integer from 1 to 6; q is an integer from 0 to 6; R1 and R2 are independently selected from the group consisting of hydrogen, alkyl, OH, hydroxyalkyl, aminoalkyl, aralkyl, or N(R4)(R5) wherein R4 and R5 are independently selected from hydrogen, alkyl, aralkyl, heteroaryl, heteroaralkyl, aminoalkyl, hydroxyalkyl, and thioalkyl; R is hydrogen, alkyl, C(O)R6, C(O)OR6, C(O)NHR6, -alkylâ€”C(O)NH2, aralkyl, (C3-C7 cyclo-alkyl)-alkyl, hydroxyalkyl, aminoalkyl, amino(hydroxy)alkyl, carboxyalkyl, heteroaraayl, alkenylalkyl, or OH wherein R6 is alkyl or aralkyl; X is independently selected from hydrogen or an electron withdrawing group; and * denotes cis or trans or a mixture thereof.