Patent ID: 6787554
Filing Date: 2004-09-07
Classification: A61P,C07D

Abstract:
A compound of formula I: or a pharmaceutically acceptable salt thereof, wherein:X is hydrogen, hydroxy, halo, nitro, mercapto, cyano, carboxy, (C1-C6)alkyl, (C1-C6) alkoxy, (C1-C6)alkylthio, C1-C6)alkylsulfonyl, (C1-C6)alkylsulfinyl, â€”NR3R4, â€”(Nâ€”A)nâ€”C(O)â€”Q1â€”Q2â€”Q3 or a 3 to 10 membered azacycloalkyl; said alkyl, alkoxy, alkylthio, alkylsulfinyl and alkylsulfonyl in the definition of X being optionally substituted independently with up to three halo atoms; said azacycloalkyl in the definition of X further optionally being bridged by (C1-C6)alkylenyl; said azacycloalkyl in the definition of X being optionally gem-dialkylated or independently substituted with up to three hydroxy, oxo, (C1-C6)alkyl, (C1-C6)alkoxy or â€”C(O)â€”Q1â€”Q2â€”Q3; R is (C1-C6)alkyl; (C1-C6)alkenyl; 2-pyridyl(C1-C6)alkyl; 3-pyridyl(C1-C6)alkyl; 4-pyridyl(C1-C6)alkyl, said pyridyls being optionally substituted independently by up to three (C1-C6)alkyl, (C1-C6)alkoxy, hydroxy, halo or amino; or a radical of the formula R1 and R2 are taken separately, are different, and are (C1-C6)alkyl, aralkyl, (C3-C10) cycloalkyl or (C3-C10)cycloalkyl-(C1-C6)alkyl; or R1 and R2 are taken separa ely, are identical and are (C1-C6)alkyl; or R1 and R2 are taken together, with the nitrogen atom to which they are attached, to form a 3 to 7 membered azacycloalkyl; said azacycloalkyl in the definition of R1 and R2 being optionally bridged by (C1-C6)alkylenyl and optionally gem-dialkylated or substituted with up to three hydroxy, oxo, (C1-C6)alkyl, (C1-C6) alkoxy, phenyl-(C1-C6)alkyl or â€”C(O)â€”Q1â€”Q2â€”Q3R3 and R4 are independently hydrogen; (C1-C6)alkyl optionally substituted with up to three halo, hydroxy, cyano or (C1-C6)alkoxy; R5-carbonyl; or (C3-C10) cycloalkyl-(C0-C4) alkylenyl optionally substituted with a hydroxy, (C1-C6)alkoxy, mercapto, (C1-C6) alkylthio, amino, Nâ€”(C1-C6)alkylamino, di- Nâ€”(C1-C6)alkylamino or (C1-C4)alkyl; R5 is hydrogen or (C1-C6)alkyl optionally substituted with hydroxy, (C1-C6)alkoxy, mercapto or (C1-C6)alkylthio; n is 0 or 1; A is independently hydrogen or â€”C(O)â€”Q1â€”Q2â€”Q3; Q1 is independently â€”Oâ€”, â€”NHâ€”, â€”N(Q2â€”Q3)â€” or Q2 is independently (C0-C4)alkylenyl or â€”(CH2CH2â€”O)r; Q3 is independently hydrogen, hydroxy, methoxy, â€”Oâ€”C(O)â€”X1, â€”NHX2 or â€”N(X1)X2; p and pâ€² are independently , 0, 1, 2 or 3; Z is independently â€”CHâ€” or â€”Nâ€”; r is independently 2, 3 or 4; X1 and X2 are taken separately and are independently (C1-C6)alkyl; or X1 and X2 are taken together with the nitrogen atom to which they are attached to form a 3- to 10-membered azacycloalkyl s is 1, 2, 3 or 4; Ar is a 5- or 6-membered aryl; Y1, Y2 and Y3 are independently hydrogen, hydroxy, mercapto, amino, nitro, halo, (C1-C6)alkyl, (C1-C6)alkoxy, (C1-C6)alkylthio, (C1-C6)alkylsulfinyl, (C1-C6)alkylsulfonyl, â€”C(O)R6, â€”C(O)OR6, â€”C(O)NR6R7,â€”NR6R7, â€”(CH2)1CN or â€”(CH2)1â€”C(O)â€”Q1â€”Q2â€”Q3; said (C1-C6)alkyl, (C1-C6)alkoxy, (C1-C6)alkylthio, (C1-C6)alkylsulfinyl and (C1-C6)alkylsulfonyl being optionally substituted independently with up to three halo atoms; t is independently 0, 1 or 2; and R6 and R7 are taken separately and are independently hydrogen or (C1-C6)alkyl; or R6 and R7 are taken together with the nitrogen atom to which they are attached to form a 4- to 7-membered azacycoalkyl.