17-09-2009 дата публикации
Номер: DE102008014077A1
Borrelidin derivatives (I) and their stereoisomers, tautomers and salts are new. Borrelidin derivatives of formula (I) and their stereoisomers, tautomers and salts are new. Either A : =O, =N-X-R1, =N-R1, H,OR3, H,N-R1, HO,R2, H,F or F,F; and B1 : =N-OH, =N-O-R1, H,R1, OH,R2, =CR4R4 or halo; or AB1 : 5 or 6 membered saturated or partially unsaturated or aromatic heterocycle with 2 or 3 heteroatom comprising N, O or S (optionally substituted with R19); D : COOH, CH 2OH, CONH 2, CSNH 2, CONHOH, COOR16, CH 2OR16, CONHR16, CONR16R17, CONHOR16 or CONHNHR16; X : O, NH(CO), NH(CO)NH or NR14; E : CN, CONH 2, CSNH 2, COOH, COOR18, CHO, CH=NOR18 or 5- or 6-membered aromatic heterocycle with 1-4 heteroatom (optionally substituted with R20); R1 : H, 1-14C alkyl, 2-14C alkenyl, 1-4C alkyl-aryl, heteroaryl, 1-4C alkyl-heteroaryl, cycloalkyl, 1-4C alkyl-cycloalkyl, heterocycloalkyl, 1-4C alkyl-heterocycloalkyl, cycloalkyl-aryl, 1-4C alkyl-cycloalkyl-aryl, heterocycloalkyl-aryl, 1-4C alkyl-heterocycloalkyl-aryl, cycloalkyl-heteroaryl, 1-4C alkyl-cycloalkyl-heteroaryl, heterocycloalkyl-heteroaryl, 1-4C alkyl-heterocycloalkyl-heteroaryl, C mH 2 m + o - pY1 p, 1-10C alkanoyl, 1-10C alkanoyl-aryl, 1-10C alkanoyl-heteroaryl, (hetero)aryloyl or T; T : (CH 2) rCH 2NHCOR11, (CH 2) rCH 2OCOR11, (CH 2) rCH 2NHCSR11, (CH 2) rCH 2S(O) nR11, (CH 2) rCH 2SCOR11, (CH 2) rCH 2OSO 2-R11, (CH 2) rCHO, (CH 2) rCH=NOH, (CH 2) rCH(OH)R11, (CH 2) rCH=NOR11, (CH 2) rCH=NOCOR11, (CH 2) rCH=NOCH 2CONR11R12, (CH 2) rCH=NOCH(CH 3)CONR11R12, (CH 2) rCH=NOC(CH 3) 2CONR11R12, (CH 2) rCH=N-NHCO-R13, (CH 2) rCH=N-NHC(O)NH-R13, (CH 2) rCH=N-NHC(S)NH-R13, (CH 2) rCH=N-NHC(NH)NH-R13, (CH 2) rCH=N-NHC(NH)-R13, (CH 2) rCH=N-NH-CO-CH 2NHCOR11, (CH 2) rCH=N-O-CH 2NHCOR11, (CH 2) rCH=N-NHCS-R13, (CH 2) rCH=CR15R16 (trans or cis), (CH 2) rCOOH, (CH 2) rCOOR11, (CH 2) rCONR11R12, (CH 2) rCH=NR11, (CH 2) rCH=N-NR11R12, (CH 2) rCH=N-NHSO 2-aryl or (CH 2) rCH=N-NHSO 2-heteroaryl; n : 0-2; r : 1-5; R2 : 1-14C alkyl, 1-14C ...
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