专利内容由知识产权出版社提供
专利名称：Benzene derivatives and pharmaceutical
composition
发明人：Mikiro Yanaka,Fuyuhiko Nishijima,Hiroyuki
Enari,Toshikazu Dewa,ToruYamazaki,Michihito Ise
申请号：US08/702116申请日：19960823公开号：US05731310A公开日：19980324
摘要：A benzene derivative of the formula (I): ##STR1## wherein R. sup.1 is hydrogen,C.sub.1-6 -alkyl, C.sub.1-6 -haloalkyl, --NH.sub.2, -- NHR.sup. 21 ; R.sup.2 is hydroxyl, --OR.sup.22, three- to seven-membered saturated cycloaliphatic amino optionallyinterrupted by one or more nitrogen, oxygen or sulfur atoms, --NHR.sup.23, --N(R.sup.24).sub.2, --NH. sub.2 ; R. sup.4 is hydrogen, C.sub.1-6 -alkyl, or --C(═O)R.sup.25 ;R.sup.7 is - -CO--, --SO.sub.2 --; R.sup.8 is --CO--, single bond; R.sup. 12 is --R.sup. 11 --R.sup.5 ; R.sup.11 is --N(R.sup.5)--, --NH--, --O--, - -N(R.sup.26)--, --N(C(═O)R.sup.27)--, --N(C(═O)NH.sub.2)--, -- N(C(═O)NHR.sup. 28)--; R.sup.13 is hydrogen, C.sub.1-6 -alkyl, C.sub.1-6 -haloalkyl, -- NHC(═O) (CH.sub.2).sub.m C.sub.6 H.sub.5, -- NHC(═O) R.sup.29, --NHC(═O)CH(C.sub.6 H.sub.5).sub.2, --NH.sub. 2, --NHR.sup.30, --(CH.sub. 2).sub.n C.sub.6H.sub.5 ; Z is C, CH, N; A is CH, N; R.sup.5 is hydrogen, --CH.sub.2 C.sub.6 H.sub.4 COOH, --CH.sub. 2 C.sub.6 H.sub.4 COOR.sup.31, --CH.sub.2 C.sub.6 H.sub.4 OH, --CH.sub.2 C.sub.6H.sub.4 OR.sup.32, --CH. sub.2 C.sub.6 H.sub.4 NH.sub.2, --CH.sub. 2 C.sub.6 H.sub.4N(R.sup.33). sub.2, --CH.sub.2 C.sub.6 H.sub.4 -azole, - -CH.sub.2 C.sub.6 H.sub.4 NHR.
sup.34, --CH.sub.2 C.sub.6 H.sub.4 C.sub.6 H.sub.4 R.sup.14 ; R.sup.14 is azole, --COOH;R.sup.21 to R.sup.34 are independently C.sub.1-6 -alkyl or C.sub.1-6 -haloalkyl; m is 0 to 6;n is 0 to 6; t is 0 or 1, with the proviso that when Z is N, R.sup.5 is hydrogen, --CH.sub.2C.sub.6 H.sub.4 COOH, --CH.sub.2 C.sub.6 H.sub.4 COOR.sup.31, --CH.sub.2 C.sub.6 H.sub.4OH, --CH.sub.2 C.sub.6 H.sub.4 OR. sup.32, --CH.sub.2 C.sub.6 H.sub.4 NH. sub.2, --CH.sub.2C.sub.6 H.sub.4 N(R.sup.33).sub.2, --CH.sub.2 C.sub.6 H. sub.4 -azole, or --CH.sub.2 C. sub.6H.sub.4 NHR.sup.34, or a salt thereof, and a pharmaceutical composition comprising saidbenzene derivative or a pharmaceutically acceptable salt thereof, and a pharmaceuticallyacceptable carrier are disclosed.
申请人：KUREHA CHEMICAL INDUSTRY CO., LTD.
代理机构：Sughrue, Mion, Zinn, Macpeak & Seas, PLLC
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