首页> 外国专利> DERIVATIVES OF 1,2-DIAZEPAN AS INHIBITORS OF THE CONVERTER ENZYME OF INTERLEUQUINA-1 BETA.

DERIVATIVES OF 1,2-DIAZEPAN AS INHIBITORS OF THE CONVERTER ENZYME OF INTERLEUQUINA-1 BETA.

机译:1,2-二氮杂卓衍生物作为间白质-1间转化酶的抑制剂。

摘要

A compound represented by the ** formula ** in which m is 0 or 1; W is -CH2-, -C (O) -, S (O) 2 or -S (O) -; X is -C (H) -, -C (R8) -, or Z is -CH2-, -O-, -S-, or -N (R1) -, provided that if Z is - N (R1 ) -, then W is -C (O) -, -S (O) 2- or -S (O) -; each R1 is, separately, -H, -S (O) 2-CH3, R2 is -C (O) R8, -C (O) C (O) R8, -S (O) 2R8, -S (O ) R8, -C (O) OR8, - C (O) N (H) R8, -S (O) 2N (H) -R8, -S (O) N (H) -R8, -C (O) C (O) N (H) R8, - C (O) CH = CHR8, -C (O) CH2OR8, -C (O) CH2N (H) R8, -C (O) N (R8) 2, - S (O) 2N (R8) 2, -S (O) N (R8) 2, -C (O) C (O) N (R8) 2, -C (O) CH2N (R8) 2, -CH2-R8 , -CH2-alkenyl-R8 or -CH2-alkynyl-R8; R8 is -H, an amino acid side chain, each R4 is independently -OH, -F, -CI, -Br, -I, -NO2, -CN, -NH2, -CO2H, -C (O) NH2, - N (H) C (O) H, -N (H) C (O) NH2, - alkyl, -cycloalkyl, -perfluoroalkyl, -O-alkyl, - N (H) alkyl, -N (alkyl) 2, - C (O) N (H) alkyl, - C (O) N (alkyl) 2, -N (H) C (O) alkyl, -N (H) C (O) N (H) alkyl, - N ( H) C (O) N (alkyl) 2, -S-alkyl, -S (O) 2alkyl, -S (O) alkyl, -C (O) alkyl, -CH2NH2, -CH2N (H) alkyl, - CH2N (alkyl) 2 oN (H) C (O) Oalkyl; R5 is -OH, -OR8, -N (H) OH or -N (H) SO2R8; R6 is -H, -CH2OR9, -CH2SR10, -CH2N (H) R9, -CH2N (R9) R11, - C (H) N2, -CH2F, -CH2CI, -CH2Br, -CH2I, -C (O) N (R11) 2, -R13 or -R14.
机译:由**式**表示的化合物,其中m为0或1; W为-CH 2-,-C(O)-,S(O)2或-S(O)-; X是-C(H)-,-C(R8)-或Z是-CH2-,-O-,-S-或-N(R1)-,前提是Z是-N(R1)- ,则W为-C(O)-,-S(O)2-或-S(O)-;每个R1分别是-H,-S(O)2-CH3,R2是-C(O)R8,-C(O)C(O)R8,-S(O)2R8,-S(O) R8,-C(O)OR8,-C(O)N(H)R8,-S(O)2N(H)-R8,-S(O)N(H)-R8,-C(O)C (O)N(H)R8,-C(O)CH = CHR8,-C(O)CH2OR8,-C(O)CH2N(H)R8,-C(O)N(R8)2,-S( O)2N(R8)2,-S(O)N(R8)2,-C(O)C(O)N(R8)2,-C(O)CH2N(R8)2,-CH2-R8, -CH 2-烯基-R 8或-CH 2-炔基-R 8; R8是-H,氨基酸侧链,每个R4独立地是-OH,-F,-Cl,-Br,-I,-NO2,-CN,-NH2,-CO2H,-C(O)NH2,- N(H)C(O)H,-N(H)C(O)NH2,-烷基,-环烷基,-全氟烷基,-O-烷基,-N(H)烷基,-N(烷基)2,- C(O)N(H)烷基,-C(O)N(烷基)2,-N(H)C(O)烷基,-N(H)C(O)N(H)烷基,-N( H)C(O)N(烷基)2,-S-烷基,-S(O)2烷基,-S(O)烷基,-C(O)烷基,-CH2NH2,-CH2N(H)烷基,-CH2N (烷基)2 oN(H)C(O)O烷基; R5是-OH,-OR8,-N(H)OH或-N(H)SO2R8; R6为-H,-CH2OR9,-CH2SR10,-CH2N(H)R9,-CH2N(R9)R11,-C(H)N2,-CH2F,-CH2Cl,-CH2Br,-CH2I,-C(O)N (R11)2,-R13或-R14。

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