发明名称 2-(ARYL- OR HETEROARYL-)PHENYL (AZA)BENZOFURAN COMPOUNDS FOR THE TREATMENT OF HEPATITIS C
摘要 ;Compounds of Formula I, including their salts, as well as compositions and methods of using the compounds are set forth. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV: formula (I).
申请公布号 US2017101416(A1) 申请公布日期 2017.04.13
申请号 US201515312022 申请日期 2015.05.19
申请人 BRISTOL-MYERS SQUIBB COMPANY 发明人 WANG Tao;Zhang Zhongxing;Kadow John F.
分类号 C07D491/048;C07D405/10 主分类号 C07D491/048
代理机构 代理人
主权项 1. A compound of Formula I, including pharmaceutically acceptable salts thereof: wherein m is 0 or 1; X is N or C—R10; R1 is methyl; R2 is Ar1; Ar1 is phenyl, 5-membered heteroaryl or 6-membered heteroaryl, and is substituted with 0-3 substituents selected from the group of cyano, halo, alkyl, cycloalkyl, haloalkyl, OH, OR101, haloalkoxy, NH2, NR102R103, COOR101, CONR102R103, S(O)2R101, S(O)2NR102R103, and NR101CONR102R103; R101 is hydrogen, alkyl or cycloalkyl with 0-3 substituents selected from halo, hydroxyl, alkoxy, and haloalkoxy; R102, R103 are each independently hydrogen, alkyl or cycloalkyl with 0-3 substituents selected from halo, hydroxyl, alkoxy, and haloalkoxy; or R102 and R103 can form a ring by joining two atoms, one from each of R102 and R103; R3 is hydrogen, halo, or alkyl; R4, R5, R6, R7, R8 are each independently selected from the group of hydrogen, halo, alkyl, cycloalkyl, haloalkyl, halocycloalkyl, hydroxyalkyl, hydroxycycloalkyl, alkoxyalkyl, alkoxycycloalkyl, alkoxy, hydroxyalkyloxy, alkoxyalkyloxy, COOR201 and CON(R202)(R203); R201 is hydrogen, alkyl or cycloalkyl with 0-3 substituents selected from halo, hydroxyl, alkoxy, and haloalkoxy; R202, R203 are each independently selected from the group of hydrogen, alkyl, cycloalkyl, alkenyl, cycloalkyl alkynyl, cyclic ether, cyclic amine, lactame, fused bicyclic alkyl, bridged bicyclic alkyl, spiro bicyclic alkyl, fused bicyclic ether, bridged bicyclic ether, spiro bicyclic ether, fused bicyclic amine, bridged bicyclic amine, and spiro bicyclic amine, with 0-3 substituents selected from the group of halo, OH, OR104, NH2, NR105R106, COOR104. CONR105R106, S(O)2R104, S(O)2NR105R106, NR104CONR105R 106, OR104CONR105R106, C(═NR107)NR105R106, NR108C(═NR107)NR105R106, haloalkoxy, Ar2, O—Ar2, and NR105—Ar2; or R202 and R203 can form a ring by joining two atoms, one from each of R202 and R203; R202 and R203 can also form bicyclic or tricyclic rings by joining multiple atoms from each of R202 and R203; R104 is hydrogen, alkyl or cycloalkyl with 0-3 substituents selected from halo, hydroxyl, alkoxy, and haloalkoxy; R105, R106 are each independently hydrogen, alkyl or cycloalkyl with 0-3 substituents selected from halo, hydroxyl, alkoxy, and haloalkoxy; or R105 and R106 can form a ring by joining two atoms, one from each of R105 and R106; R107, R108 are each independently hydrogen, alkyl or cycloalkyl with 0-3 substituents selected from halo, hydroxyl, alkoxy, and haloalkoxy; or R107 and R108 can form a ring by joining two atoms, one from each of R107 and R108; Ar2 is phenyl, 5-membered heteroaryl or 6-membered heteroaryl, and is substituted with 0-3 substituents selected from the group of cyano, halo, alkyl, cycloalkyl, haloalkyl, OH, OR204, haloalkoxy, NH2, NR205R206,COOR204, CONR205R206, S(O)2R204, S(O)2NR205R206, and NR204CONR205R206; R204 is hydrogen, alkyl or cycloalkyl with 0-3 substituents selected from halo, hydroxyl, alkoxy, and haloalkoxy; R205, R206 are each independently hydrogen, alkyl or cycloalkyl with 0-3 substituents selected from halo, hydroxyl, alkoxy, and haloalkoxy; or R205 and R206 can form a ring by joining two atoms, one from each of R205 and R206; R9 is selected from the group of hydrogen, halo, alkyl, cycloalkyl, alkoxy, Ar3 and NR301R302; R301 is selected from the group of hydrogen, alkyl, cycloalkyl, (cycloalkyl)alkyl, benzyl, alkylcarbonyl, haloalkyl carbonyl, phenyl carbonyl, (alkoxyphenyl)carbonyl, alkylsulfonyl, phenylsulfonyl, (alkoxyphenyl)sulfonyl, and (haloalkoxyphenyl)sulfonyl; R302 is hydrogen, alkyl, hydroxyalkyl, or alkoxyalkyl; or R301 and R302 taken together with the nitrogen to which they are attached is oxazolidinonyl or dioxothiazinyl; Ar3 is phenyl, 5-membered heteroaryl or 6-membered heteroaryl, and is substituted with 0-3 substituents selected from the group of cyano, halo, alkyl, cycloalkyl, haloalkyl, OH, OR303, haloalkoxy, NH2, NR304R305, COOR303, CONR304R305, S(O)2R303, S(O)2NR304R305, and NR303CONR304R305; R303 is hydrogen, alkyl or cycloalkyl with 0-3 substituents selected from halo, hydroxyl, alkoxy, and haloalkoxy; R304, R305 are each independently hydrogen, alkyl or cycloalkyl with 0-3 substituents selected from halo, hydroxyl, alkoxy, and haloalkoxy; or R304 and R305 can form a ring by joining two atoms, one from each of R304 and R305; R10 is hydrogen, alkyl, halo, N(R401)(R402), or alkylsulfonyl; R401 and R402 are each independently selected from the group of hydrogen, alkyl, hydroxyalkyl, alkoxyalkyl, alkylsulfonyl, or alkylsulfonylalkyl; or N(R401)(R402) taken together is azetidinyl, pyrrolidinyl, piperidinyl, or piperazinyl, and is substituted with 0-2 substituents selected from alkyl, hydroxyalkyl, and hydroxy.
地址 Princeton NJ US