Patent ID: 6372778
Filing Date: 2002-04-16
Classification: A61K,A61P,C07C,C07D,C07K

Abstract:
A compound of formula I: wherein:A is selected from the group consisting of Ht; â€”R1â€”Ht; â€”R1â€”C1-C6 alkyl substituted with Ht or â€”Oâ€”Ht and optionally substituted with one additional substituent selected from the group consisting of hydroxy, C1-C4 alkoxy, Ht, â€”Oâ€”Ht, â€”NR2â€”COâ€”N(R2) (R2) and â€”COâ€”N(R2) (R2); and â€”R1â€”C2-C6 alkenyl substituted with Ht or â€”Oâ€”Ht and optionally substituted with one additional substituent selected from the group consisting of hydroxy, C1-C4 alkoxy, Ht, â€”Oâ€”Ht, â€”NR2â€”COâ€”N(R2) (R2) and â€”COâ€”N(R2) (R2); each R1 is independently selected from the group consisting of â€”C(O)â€”, â€”S(O)2â€”, â€”C(O)â€”C(O)â€”, â€”Oâ€”C(O)â€”, â€”Oâ€”S(O)2, â€”NR2â€”S(O)2â€”, â€”NR2â€”C(O)â€” and â€”NR2â€”C(O)â€”C(O)â€”; each Ht is a 5-membered nitrogen-containing saturated or unsaturated heterocycle, optionally containing one additional heteroatom selected from N or O, wherein said heterocycle is optionally benzofused; and wherein any member of said Ht is optionally substituted with one to two substituents independently selected from the group consisting of oxo, â€”OR2, â€”R2, â€”N(R2) (R2), â€”R2â€”OH, â€”CN, â€”CO2R2, â€”C(O)â€”N(R2) (R2), â€”S(O)2â€”N(R2) (R2), â€”N(R2)â€”C(O)â€”R2, â€”C(O)â€”R2, â€”S(O)nâ€”R2, â€”OCF3, â€”S(O)nâ€”R7, methylenedioxy, â€”N(R2)â€”S(O)2(R2), halo, â€”CF3, â€”NO2, R7 and â€”Oâ€”R7; each R2 is independently selected from the group consisting of H and C1-C3 alkyl optionally substituted with R7; with the proviso that when R2 is C1-C3 alkyl substituted with R7, said R7 may not be substituted with an R7-containing moiety; B, when present, is â€”N(R2)â€”C(R3) (R3)â€”C(O)â€”; x is 0 or 1; each R3 is independently selected from the group consisting of H, Ht, C1-C6 alkyl, C2-C6 alkenyl, C3-C7 cycloalkyl, C5-C7 cycloalkenyl and C6-C10 aryl, wherein any member of said R3, except H, is optionally substituted with one to two substituents independently selected from the group consisting of â€”OR2, â€”C(O)â€”NHâ€”R2, â€”S(O)â€”N(R2) (R2), Ht, â€”CN, â€”SR2, â€”CO2R2, and NR2â€”C(O)â€”R2; each n is independently 1 or 2; D and Dâ€² are independently selected from the group consisting of R7; C1-C4 alkyl substituted with C3-C6 cycloalkyl, â€”Oâ€”R7 or R7, and optionally substituted with one additional substituent selected from C3-C6 cycloalkyl, â€”Oâ€”R7â€”, R7, OR2 or â€”R3; C2-C4 alkenyl substituted with C3-C6 cycloalkyl, â€”Oâ€”R7 or R7, and optionally substituted with one additional substituent selected from C3-C6 cycloalkyl, â€”Oâ€”R7â€”, R7, OR2 or â€”R3; C3-C6 cycloalkyl, which is optionally substituted with or fused with R7; and C5-C6 cycloalkenyl, which is optionally substituted with or fused with R7; each R7 is independently selected from the group consisting of phenyl and a 3-6 membered carbocyclic ring, wherein said carbocyclic ring may be saturated or unsaturated and wherein R7 is optionally substituted with one to two groups independently selected from the group consisting of oxo, â€”OR2, â€”R2, â€”N(R2) (R2), â€”N(R2)â€”C(O)â€”R2, C1-C3alkyl substituted with â€”OH and optionally substituted with R7, â€”CN, â€”CO2R2, â€”C(O)â€”N(R2) (R2), halo and â€”CF3; E is selected from the group consisting of HtE; Oâ€”HtE; HtEâ€”HtE; â€”Oâ€”R3 substituted with HtE, â€”NR2R3 substituted with HtE, C1-C6 alkyl substituted with HtE, and C2-C6 alkenyl substituted with HtE, wherein the substituted â€”Oâ€”R3, â€”NR2R3 or C1-C6 alkyl is optionally substituted with one additional substituent selected from the group consisting of R4 and HtE; C3-C6 saturated carbocycle, which is optionally substituted with one to two groups independently selected from the group consisting of R4 and HtE; and C5-C6 unsaturated carbocycle, which is optionally substituted with one to two groups independently selected from the group consisting of R4 and HtE; wherein each HtE is independently selected from the group consisting of C3-C7 cycloalkyl; C5-C7 cycloalkenyl; or C6â€”C10 aryl; wherein HtE is optionally substituted with one or two substituents independently selected from the group consisting of oxo, â€”OR2, â€”R2, â€”N(R2) (R2), â€”R2â€”OH, â€”CN, â€”CO2R2, â€”C(O)â€”N(R2) (R2), â€”S(O)2â€”N(R2) (R2), â€”N(R2)â€”C(O)â€”R2, â€”C(O)â€”R2, â€”S(O)nâ€”R2, â€”OCF3, â€”S(O)nâ€”R7, methylenedioxy, â€”N(R2)â€”S(O)2(R2), halo, â€”CF3, â€”NO2, R7 and â€”Oâ€”R7; and each R4 is independently selected from the group consisting of â€”OR2, â€”C(O)â€”NHR2, â€”S(O)2â€”NHR2, halo, â€”NR2â€”C(O)â€”R2 and â€”CN.