Patent ID: 6528531
Filing Date: 2003-03-04
Classification: C07D

Abstract:
A compound having the formula I: or a physiologically acceptable salt thereof,whereinn is 0 or 1; m is 0, 1 or 2; p is 1, 2 or 3; X is (1) a bond, (2) (CRaRa)p, (3) C3-7 cycloalkylene, or (4) C3-7 cycloalkylidene; R is halogen; R1 is (1) hydrogen or (2) C1-6 alkyl; R2 and R3 are independently selected from (1) hydrogen, (2) C1-6alkyl optionally substituted with ORb, (3) C2-6alkenyl, (4) C2-6alkynyl, (5) phenyl optionally substitued with ORb, (6) benzyl optionally substitued with ORb, (7) CO2Rb; or R2+R3 represent &boxH;O; or when X is a bond or (CRaRa)p, R2 and R4 together complete a 4- to 7-membered non-aromatic ring containing 1 or 2 heteroatoms independently selected from O and S(O)m, and said ring being optionally substituted with 1 to 5 groups independently selected from oxo, ORb, CH2ORb, CH2OC(O)Rb and C1-6alkyl; or when X is a bond or (CRaRa)p, R2 and R5 together complete a 4- to 7-membered non-aromatic ring containing 0 to 2 heteroatoms independently selected from O and S(O)m, said ring being optionally substituted with 1 to 5 groups independently selected from oxo, ORb, CH2ORb, CH2OC(O)Rb and C1-6alkyl; R4 is (1) ORb, (2) OC(O)Rb, (3) OC(O)ORb, (4) OC(O)(CH2)mNRbRb, (5) OSO2Rb, (6) S(O)mRb (7) OP(O)(ORb)2, or (8) CO2Rb; or R4+R6 represent &boxH;O; or R4, R5 and the carbon atoms to which they are attached form a 3- to 7-membered non-aromatic ring containing 1 or 2 heteroatoms independently selected from O or S(O)m, said ring being optionally substituted with 1 to 5 groups independently selected from oxo, ORb, CH2ORb, CH2OC(O)Rb and C1-6alkyl; or R5 and R6 are independently selected from (1) hydrogen, (2) C1-12alkyl, (3) C2-12alkenyl, (4) C2-12alkynyl, (5) C3-7cycloalkyl-(C1-6alkyl)n, (6) mono-, bi- or tricyclic heterocyclyl-(C1-6alkyl)n, wherein said heterocyclyl contains 3 to 12 ring atoms 1 to 4 of which are independently selected from O and S(O)m, (7) aryl-(C1-6alkyl)n, (8) heteroaryl-(C1-6alkyl)n, (9) CO2Rb, or (10) ORb, wherein alkyl, alkenyl and alkynyl are optionally substituted with 1 to 5 groups independently selected from Rc, cycloalkyl and heterocyclyl are optionally substituted with 1 to 5 groups independently selected from Rc, alkyl, and spirofused C3-6 cycloalkylidene, and aryl and heteroaryl are optionally substituted with 1 to 3 groups independently selected from Rd, or R5, R6 and the carbon atoms to which they are attached form a 3- to 7-membered non-aromatic ring containing 0 to 2 heteroatoms independently selected from O and S(O)m, optionally substituted with 1 to 5 groups independently selected from oxo, ORb, CH2ORb, CH2OC(O)Rb and C1-6alkyl; or when X is (CRaRa)p, R5 and any one of the Ra may together complete a 3- to 7-membered non-aromatic carbocyclic ring; R7 is (1) O or (2) methyl; Ra is (1) hydrogen, or (2) C1-6alkyl, or Rb is (1) hydrogen, (2) C1-12alkyl (3) C2-12alkenyl, (4) C2-12alkynyl, (5) C3-7cycloalkyl-(C1-6alkyl)n, (6) heterocyclyl-(C1-6alkyl)n, (7) aryl-(C1-6alkyl)n, or (8) heteroaryl-(C1-6alkyl)n, wherein alkyl, cycloalkyl, heterocyclyl, alkenyl and alkynyl are optionally substituted with up to 5 groups independently selected from Rc, and aryl and heteroaryl are optionally substituted with up to 3 groups independently selected from Rd, or two Rb groups attached to the same nitrogen atom together complete a 4- to 7-membered ring optionally containing an additional heteroatom selected from O, S and Nâ€”Rf; Rc is (1) halogen, (2) S(O)mRe, (3) ORe, (4) OC(O)NReRe, (5) OC(O)ORe, (6) OC(O)Re, (7) OSO2Re (8) OCF3, (9) CF3, (10) C(O)ORe (11) C(O)Re (12) oxo, (13) N3, (14) CN, (15) NO2, or (16) P(O)(ORe)2; Rd is (1) a group selected from Rc, (2) C1-6alkyl optionally substituted with 1 to 6 groups selected from Rc, (3) aryl optionally substituted with 1 to 3 groups selected from Rc, (4) heteroaryl optionally substituted with 1 to 3 groups selected from Rc, (5) NReRe, (6) NRfSO2Re, (7) NRfC(O)ORe, (8) NRfC(O) Re, (9) NRfC(O)NReRe; Re is (1) hydrogen, (2) C1-12alkyl optionally substituted with 1 to 5 groups selected from halogen, CN, OH and C1-10alkoxy optionally substituted with oxiranyl, hydroxy or C1-6 alkyl, (3) C2-12alkenyl, (4) C2-12alkynyl, (5) C3-7cycloalkyl-(C1-6alkyl)n, (6) aryl(C1-6alkyl)n optionally substituted with NO2, C1-6alkyl, C1-6alkoxy, or halogen, (7) heteroaryl(C1-6alkyl)n, or two Re groups together with the nitrogen atom to which they are attached form a 3- to 7-membered ring optionally containing an additional heteroatom selected from O, S and Nâ€”Rf; Rf is (1) hydrogen or (2) C1-6alkyl.