Patent ID: 6689909
Filing Date: 2004-02-10
Classification: A61P,C07C,C07D

Abstract:
A compound of formula (I): wherein:n is 1 or 2; R1 is chloro, fluoro, bromo, methyl or methoxy; R2 is selected from one of the following three groups: i) halo, nitro, hydroxy, amino or cyano; ii) â€”X1â€”R5 wherein X1 is a direct bond, â€”Oâ€”, â€”Sâ€”, â€”SOâ€”, â€”SO2â€”, NR6, â€”CO, â€”CONR6â€”, â€”NR6COâ€”, â€”NR6SO2â€” or NR6CONR7â€”; wherein R6 and R7 are independently hydrogen or C1-4alkyl optionally substituted with one or more A; and R5 is selected from C1-6alkyl optionally substituted with one or more A, C3-7cycloalkyl optionally substituted with one or more A, C3-7cycloalkylC1-6alkyl optionally substituted with one or more A, C2-6alkenyl optionally substituted with one or more A, C2-6alkynyl optionally substituted with one or more A, phenyl optionally substituted with one or more D, phenylC1-6allyl optionally substituted with one or more D, heteroaryl ring optionally substituted on a ring carbon by one or more D or (heteroaryl ring)C1-6alkyl optionally substituted on a ring carbon with one or more D; wherein said heteroaryl ring is a carbon linked 6-membered ring containing 1-2 nitrogen atoms or a carbon linked 5-membered ring containing 1-3 heteroatoms selected independently from O, N and S; and wherein if said 5-membered heteroaryl ring contains an â€”NHâ€” moiety that nitrogen may be optionally substituted with a group selected from G; iii) a nitrogen-linked 4-8 membered heterocyclic group optionally substituted on a ring carbon by one or more D and wherein if said heterocyclic group contains an â€”NHâ€” moiety that nitrogen may be optionally substituted with a group selected from G; R3 is C1-6alkyl optionally substituted with one or more A, C3-7cycloalkyl optionally substituted with one or more A, phenyl optionally substituted with one or more D, a carbon-linked 6-membered heteroaryl ring containing 1-2 nitrogen atoms optionally substituted on a ring carbon by one or more D, or a carbon linked 5-membered heteroaryl ring containing 1-3 heteroatoms selected independently from O, N and S optionally substituted on a ring carbon by one or more D and wherein if said 5-membered heteroaryl ring contains an â€”NHâ€” moiety that nitrogen may be optionally substituted with a group selected from G; A is selected from hydroxy, amino, halo, carboxy, Nâ€”(C1-4alkyl)amino, N,N-di-(C1-4alkyl)amino, carbamoyl and C1-6alkoxy; D is selected from: i) â€”Xaâ€”Rc wherein Xa is a direct bond, â€”Oâ€”, â€”Sâ€”, â€”SOâ€”, â€”SO2â€”, â€”COâ€”, â€”NRdSO2â€”, â€”NRdCOâ€”, NRdCONReâ€”, â€”NRdâ€” or â€”CONRdâ€”; wherein Rd and Re are independently hydrogen or C1-4alkyl optionally substituted with one or more hydroxy or C1-4alkoxy; and Rc is selected from hydrogen or C1-6alkyl optionally substituted with one or more hydroxy or C1-4alkoxy; ii) a 4-8 membered Het which is optionally substituted on a ring carbon with one or more groups selected from hydroxy, halo, C1-4alkoxy, C1-4alkyl or cyano and wherein if said 4-8 membered Het contains an â€”NHâ€” moiety that nitrogen may be optionally substituted with a group selected from G; iii) â€”Xaâ€”C1-6alkyl-Xbâ€”Rc wherein Xa and Rc are as defined hereinbefore and Xb is â€”Sâ€”, â€”SOâ€” or â€”SO2â€”; iv) cyano or halo; and v) â€”Xcâ€”Rf wherein Xc is â€”C(O)â€” or â€”SO2â€” and Rf is a nitrogen-linked 4-8 membered heterocyclic group optionally substituted on a ring carbon by one or more groups selected from hydroxy, halo, C1-4alkoxy, C1-4alkyl or cyano and wherein if said heterocyclic group contains an â€”NHâ€” moiety that nitrogen may be optionally substituted with a group selected from G; G is selected from C1-6alkyl optionally substituted with one or more A, C1-6alkanoyl optionally substituted with one or more A, C1-6alkylsulphonyl optionally substituted with one or more A, C1-6alkoxycarbonyl optionally substituted with one or more A, carbamoyl, Nâ€”(C1-6alkyl)carbamoyl optionally substituted with one or more A, Nâ€”(C1-6alkyl)2carbamoyl optionally substituted with one or more A and benzoyl optionally substituted with one or more A; and R4 is hydrogen or fluoro; or a pharmaceutically acceptable salt or an in vivo hydrolysable ester thereof.