Patent ID: 6525025
Filing Date: 2003-02-25
Classification: A61P,C07C,C07D

Abstract:
A compound represented by Formula I: or a pharmaceutically acceptable salt, ester or hydrate thereof, wherein:W is a bond, â€”CH2â€”, â€”C(O)â€” or â€”C(O)CH2â€”; Z is selected from the group consisting of: (1) H, (2) C1-11alkyl, (3) C3-11cycloalkyl or a benzofused analog thereof, (4) phenyl or naphthyl, and (5) HET1, wherein HET1 represents a 5- to 10-membered mono- or bicyclic, aromatic or non-aromatic ring, or a benzofused analog thereof, containing 1-3 heteroatoms selected from O, S and N, groups (2), (3) and (5) above are optionally substituted with 1-2 oxo groups, groups (2)-(5) above are further optionally substituted with 1-3 substituents independently selected from the group consisting of: (a) halo (b) nitro, (c) hydroxy, (d) C1-4alkyl, (e) C1-4alkoxy, (f) C1-4alkylthio, (g) C3-6cycloalkyl, (h) phenyl or naphthyl, (i) phenoxy, (j) benzyl, (k) benzyloxy, and (l) a 5 or 6-membered aromatic or non-aromatic ring containing from 1-3 heteroatoms selected from O, S and N, groups (d)-(g) above are optionally substituted with oxo and 1-3 substituents independently selected from halo and C1-4alkoxy, groups (h)-(l) above are optionally substituted with 1-3 substituents independently selected from halo and C1-4alkyl, and group (4) is further optionally substituted up to its maximum with halo groups; R1 and R2 are independently selected from the group consisting of: (1) H, (2) halo, (3) hydroxy, (4) nitro, (5) cyano, (6) C1-10alkyl, C3-10cycloalkyl, C1-10alkoxy, â€”S(O)0-2C1-10alkyl or â€”NHC1-10alkyl, each optionally substituted with 1-2 oxo or carboxy groups and further optionally substituted with 1-3 substituents independently selected from the group consisting of: (a) halo, (b) hydroxy (c) cyano, (d) C1-4alkoxy, (e) â€”NHR7, wherein R7 is H or C1-5alkyl, said C1-5alkyl optionally substituted with â€”NHR8, wherein R8 is C1-5alkyl optionally substituted with oxo and further optionally substituted with a 5- to 10-membered mono- or bicyclic, aromatic or non-aromatic ring, or a benzofused analog thereof, containing 1-3 heteroatoms selected from O, S and N, and optionally substituted with oxo, (f) â€”S(O)0-2C1-4alkyl, and (g) HET2, wherein HET2 represents a 5- to 7-membered aromatic or non-aromatic ring containing 1-4 heteroatoms selected from O, S and NR7, wherein R7 is H or C1-5alkyl, said HET2 being optionally substituted with oxo and further optionally substituted with 1-2 substituents independently selected from halo and C1-4alkyl, said C1-4alkyl being optionally substituted with 1-3 halo groups, (7) phenoxy or â€”S(O)0-2phenyl, (8) benzyloxy or â€”S(O)0-2benzyl, (9) benzoyl, (10) phenyl or naphthyl, (11) â€”O-HET2 or â€”S-HET2, said HET2 being optionally substituted with oxo and further optionally substituted as defined below, and (12) HET3, wherein HET3 is a 5- or 6-membered aromatic or non-aromatic ring, or a benzofused analog thereof, containing from 1 to 4 heteroatoms selected from O, S and N, said HET3 being optionally substituted with oxo and further optionally substituted as defined below, groups (7)-(12) above are each optionally substituted with 1-2 substituents independently selected from the group consisting of: halo, cyano, C1-4alkyl and C1-4alkoxy, said C1-4alkyl and C1-4alkoxy being optionally substituted with 1-3 halo groups; or R1 and R2 may be taken in combination and represent a fused ring as shown below: â€ƒwherein Y and X are independently selected from the group consisting of â€”C(R10)2â€”, â€”C(R10)2C(R10)2â€”, â€”NR11â€”, â€”Oâ€” and â€”Sâ€”, R3 is as defined below, each R9 is independently selected from H and C1-4alkyl, each R10 is independently selected from H and C1-4alkyl, and R11 is H or C1-4alkyl, or one R9 may be joined with either one R10 or R11 on an adjacent atom to form a double bond; R3 is C1-10alkyl, optionally substituted with 1-2 oxo or carboxy groups and further optionally substituted with 1-3 substituents independently selected from the group consisting of: (a) halo, (b) hydroxy (c) cyano, (d) C1-4alkoxy, (e) â€”NHR7, wherein R7 is H or C1-5alkyl, said C1-5alkyl optionally substituted with â€”NHR8, wherein R8 is C1-5alkyl optionally substituted with oxo and further optionally substituted with a 5- to 10-membered mono- or bicyclic, aromatic or non-aromatic ring, or a benzofused analog thereof, containing 1-3 heteroatoms selected from O, S and N, and optionally substituted with oxo, (f) â€”S(O)0-2C1-4alkyl, and (g) HET2, wherein HET2 represents a 5- to 7-membered aromatic or non-aromatic ring containing 1-4 heteroatoms selected from O, S and NR7, wherein R7 is H or C1-5alkyl, said HET2 being optionally substituted with oxo and further optionally substituted with 1-2 substituents independently selected from halo or C1-4alkyl, said C1-4alkyl being optionally substituted with 1-3 halo groups, each R4 is independently selected from the group consisting of: H, halo, hydroxy, C1-6alkyl and C1-4alkoxy, said C1-6alkyl and C1-4alkoxy being optionally substituted with oxo and further optionally substituted with 1-3 halo groups; and R5 is selected from the group consisting of: H, phenyl, naphthyl, C1-6alkyl optionally substituted with OR12 and 1-3 halo groups, and C5-7cycloalkyl optionally containing one heteroatom selected from O, S and NR13, wherein R12 is selected from the group consisting of: H, C1-5alkyl optionally substituted with 1-3 halo groups, and benzyl optionally substituted with 1-3 substituents independently selected from halo, C1-4alkyl and C1-4alkoxy, and R13 is H or C1-4alkyl optionally substituted with 1-3 halo groups; and R6 represents H; or in the alternative, R5 and R6 are taken in combination and represent a ring of 4-7 members, said ring optionally containing one heteroatom selected from O, S and NR13.