SUBSTITUTED BENZAMIDES, THEIR PRODUCTION AND THEIR USE AS CYSTEINE PROTEASE INHIBITORS

    公开(公告)号:SK14122000A3

    公开(公告)日:2001-05-10

    申请号:SK14122000

    申请日:1999-04-19

    Applicant: BASF AG

    Abstract: Benzamides of the formula Iand its tautomeric forms, possible enantiomeric and diastereomeric forms, E and Z forms, and possible physiologically tolerated salts, in which the variables have the following meanings:R1-C1-C6-alkyl, branched or unbranched, where one of the C atoms in this chain may be substituted by a phenyl ring, cyclohexyl ring, indolyl ring and an SCH3 group, and the phenyl ring in turn is substituted by by [sic] a maximum of two R4 radicals, where R4 [lacuna] hydrogen, C1-C4-alkyl, branched or unbranched, -O-C1-C4-alkyl, OH, Cl, F, Br, I, CF3, NO2, NH2, CN, COOH, COO-C1-C4-alkyl, NHCO-C1-C4-alkyl, andR2 can be NR5CO-R6 and NHR5SO2-R6, andR3 is chlorine, bromine, fluorine, C1-C6-alkyl, NHCO-C1-C4-alkyl, NHSO2-C1-C4-alkyl, NO2, -O-C1-C4-alkyl, CN, COOH, CONH2, COO-C1-C4-alkyl, SO2-C1-C4-alkyl, -SO2Ph, SO2NH-C1-C4-alkyl, iodine, SO2NH2 and NH2, andA can be aromatic rings and heteroaromatic rings such as naphthyl, quinolyl, quinoxyl, benzimidazolyl, benzothienyl, quinazolyl, phenyl, thienyl, imidazolyl, pyridyl, pyrimidyl and pyridazyl, it also being possible for the rings to be substituted by by [sic] R9 and up to 2 R8 radicals, andB a bond, -(CH2)m-, -(CH2)m-O-(CH2)o-, -(CH2)o-S-(CH2)m-, -(CH2)o-SO-(CH2)m-, -(CH2)o-SO2-(CH2)m-, -CH=CH-, -C=C-, -CO-CH=CH-, -(CH2)o-CO-(CH2)m-, -(CH2)m-NHCO-(CH2)o-, -(CH2)m-CONH-(CH2)o-, -(CH2)m-NHSO2-(CH2)o-, -NH-CO-CH=CH-, -(CH2)m-SO2NH-(CH2)o-,A-B together alsoR5 hydrogen and C1-C4-alkyl andR6 is hydrogen, phenyl, naphthyl, C1-C6-alkyl, linear or branched, it being possible for a C atom in the chain to be substituted by a phenyl ring which itself may also be substituted by one or two R4 radicals, andR8 can be hydrogen, C1-C4-alkyl, branched or unbranched, -O-C1-C4-alkyl, OH, Cl, F, Br, I, CF3, NO2, NH2, CN, COOH, COO-C1-C4-alkyl, -NHCO-C1-C4-alkyl, phenyl, NHCO-phenyl, -NHSO2-C1-C4-alkyl, -NHSO2-phenyl, -SO2-C1-C4-alkyl, pyridine [sic] and SO2-phenyl,R9 hydrogen, -CHR14-(CH2)p-R12 where R12 pyrrolidine [sic], morpholine [sic], piperidine [sic], hexahydroazepine [sic], homopiperazine [sic], and R10 [lacuna] C1-C6-alkyl, branched or unbranched, and which may also carry a phenyl ring which is in turn substituted by by [sic] a maximum of two R11 radicals, where R11 is hydrogen, C1-C4-alkyl, branched or unbranched, -O-C1-C4-alkyl, OH, Cl, F, Br, I, CF3, NO2, NH2, CN, COOH, COO-C1-C4-alkyl, NHCO-C1-C4-alkyl, -NHSO2-C1-C4-alkyl and -SO2-C1-C4-alkyl; andR13 is hydrogen and C1-C6-alkyl, branched or unbranched, andn,p is [sic], independently of one another, a number 0, 1 or 2, andm,o is [sic], independently of one another, a number 0, 1, 2, 3 or 4.

    NUEVAS BENZAMIDAS HETEROCICLICAS SUSTITUIDAS

    公开(公告)号:CO4910161A1

    公开(公告)日:2000-04-24

    申请号:CO97071820

    申请日:1997-12-09

    Applicant: BASF AG

    Abstract: Benzamida heterocíclica sustituida de la fórmula Y y sus formas tautómeras a isómeras así con en caso necesario sus sales fisiológicamente aptas, CARACTERIZADO PORQUE las variables tienen el siguiente significado, R1 hidrógeno, C1 -C6 -alquilo, O- C1 -C6 -alquilo. OH, Cl, F, Br, J, CF3 , NO2 NH2 , CN, COOH, COO.C1 -C6 -alquilo, -NHCO- C1 -C4 -alquilo, NHCO-fenilo, CONHR9 , NHSO3 - C1 -C6 -alquilo, NHSO2 -fenilo, -SO2 - C1 -C6 -alquilo o -SO2 -fenilo; R2 hidrógeno, C1 -C6 -alquilo, O- C1 -C6 -alquilo, OH, Cl, F, Br, J, CF3 , NO2 , NH2 , CN, COOH, COO-C1 -C6 - alquilo, -NHCO-C1 -C4 -alquilo, NHCO-fenilo, CONHR6 , NHSO2 -C1 -C6 -alquilo, NHSO2 -fenilo, -SO2 - C1 -C6 - alquilo o -SO2 -fenilo; o R1 y R2 juntos son una cadena de CH-CH-CH-CH que puede llevar uno o dos sustituyentes R6 ; R3 es hidrógeno cloro, bromo. fluoro, C1 -C6 -alquilo, fenilo, NHCO-C1 -C4 -alquilo, NO2 o NH2 , R4 C1 -C6 -alquilo que puede llevar otro anillo fenilociclopropil-, ciclobutil-, ciclopentil-, ciclohexil-cicloheptil-indolil-, piridil- o naftil, el que a su vez está sustituido por uno o dos residuos R7 , siendo R7 hidrógeno, C1 -C6 -alquilo, O-C1 -C6 -alquilo, OH, Cl, F, Br, J, CF3 , NO2 , NH2 , CN, COOH, COO-C1 -C4 -alquilo, -CONHR6 , -NHCO-C1 -C4 .alquilo, NHCO-fenilo, NHSO2 ,- C1 -C6 - alquilo, NHSO-fenilo, SO2 - C1 -C4 -alquilo o -SO2 -fenilo; R5 es hidrógeno, -CO-OR8 , -CO-NR9 R10 R6 es hidrógeno, C1 -C6 - alquilo, O- C1 -C6 -alquilo, OH, Cl, F, Br J, CF3 , NO2 , NH2 , CN, COOH, COO-C1 -C6 -alquilo R8 es hidrógeno o C1 -C6 -alquilo ...

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