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    CONDESED N-HETEROCYCLIC COMPOUNDS SUBSTITUTED WITH BENZYLOXY-GROUP, PROCESS FOR PRODUCING THEM, AND THEIR USE AS BRADIQUININ-RECEPTOR-ANTAGONISTS
    2.
    发明专利
    CONDESED N-HETEROCYCLIC COMPOUNDS SUBSTITUTED WITH BENZYLOXY-GROUP, PROCESS FOR PRODUCING THEM, AND THEIR USE AS BRADIQUININ-RECEPTOR-ANTAGONISTS 未知

    公开(公告)号：HU9800649A2

    公开(公告)日：1998-12-28

    申请号：HU9800649

    申请日：1998-03-25

    Applicant: HOECHST AG

    Inventor： HEITSCH HOLGER ,  SCHOELKENS BERNWARD ,  WAGNER ADALBERT ,  WIRTH KLAUS

    IPC: A61K31/395 ,  A61K31/47 ,  A61K31/495 ,  A61P1/16 ,  A61P43/00 ,  C07D215/26 ,  C07D241/36 ,  C07D401/12 ,  C07D405/12 ,  C07D215/24 ,  C07D239/72 ,  C07D241/40 ,  C07D237/28 ,  C07D253/08 ,  C07D257/10 ,  A61K31/53 ,  A61K31/50

    Abstract: 8-Benzyloxy-(iso)quinoline derivatives (including poly-aza analogues) of formula (I) and their salts are new: D = aza-heterocyclic residue of formula (i) or (ii); X1 = N or CR6; X2 = N or CR7; X3 = N or CR8; B = benzyl variably substituted on the ring by R3-R5; R1, R2 = H, halo or 1-3C alkyl; R3, R4 = H, halo, CN, 1-3C alkyl (optionally substituted by halo), 1-3C alkoxy (optionally substituted by halo), 1-3C alkylthio (optionally substituted by halo), OH, tetrazolyl, CONHR9 or CO2R9; R5 = NO2, NH2, -NR9AYER10 or SO2NR9R10; R6, R8, R'" = H, halo, 1-4C alkyl, 1-4C alkoxy, NH2, NH-(1-4C alkyl), OH, Ar, Ar-(1-4C)-alkanediyl or CO2R9; R7, R', R" = H or 1-4C alkyl; R9 = H, 1-4C alkyl, 2-5C alkenyl or Ar-(1-3C)-alkanediyl; A = divalent residue of an aminocarboxylic acid such as methionine, alanine, phenylalanine, tyrosine, O-methyltyrosine, beta -(2-thienyl)-alanine, glycine, cyclohexylalanine, leucine, isoleucine, valine, norleucine, phenylglycine, serine, cysteine, aminopropionic acid or aminobutyric acid; Y = C=O, C=S or SO2; E = 2-5C alkene-diyl, 1-7C alkanediyl, 3-10C cycloalkanediyl or -(CH2)m-To-(CH2)n (all optionally substituted by one or more groups such as OR12, NO2, CN, CO2R9, NR13R14, SO3R12, SO2NR13R14 or CONR13R14); T = O, S or NR15; m, n = 0-6; o = 0 or 1; p = 1-3; R10 = H or 1-5C alkyl, Ar', Ar'-(1-3C)-alkanediyl or 5-10C heteroaryl (all optionally substituted by one or more groups such as halo, NO2, 1-5C alkylthio, NR13R14, NR13COR16, CO2R9, SO3R12, SO2NR13R14, OR12 or 1-6C alkyl, or Ar', 2-5C alkenyl or OA5 (themselves optionally partially or completely substituted by halo)); R11 = 1-5C alkyl or 1-5C alkoxy (both optionally partially or completely substituted by F or Cl); R12, R13 = H, 1-5C alkyl, 2-5C alkenyl, Ar, Ar-(1-5C)-alkanediyl, 3-10C cycloalkyl, (3-10C)-cycloalkyl-(1-2C)-alkanediyl, CO2-(1-5C alkyl) or CONH-(1-5C alkyl); R14 = H, CO2-(1-3C alkyl) or CO2-(1-3C)-alkanediyl-Ar'; R15 = H, CO2-(1-3C alkyl) or 1-3C alkyl; R16 = 1-3C alkyl, Ar or 5-10C heteroaryl (all optionally substituted by one or more groups such as halo, CN, NO2, NR13R14 or CO2R9); Ar, Ar' = aryl with 6-12C or 6-10C respectively; provided that if D = (ii), then R3 and R4 are not both halo, 1-3C and/or 1-3C alkoxy or H in combination with halo, 1-3C alkyl or 1-3C alkoxy, excluded from this proviso being compounds in which: (a) R5 = -N(R9)-A-Y-E-R10 and R10 = (R11)p-substituted phenyl, provided that if R10 = (R11)p-substituted phenyl then R3 and R4 are not same or different H and halo; and (b) R5 = -SO2NR9R10, provided that R3 and R4 are not both halo.

    NOVEL HETEROCYCLIC COMPOUNDS, METHOD OF OBTAINING THEM AND PHARMACEUTIC AGENT
    3.
    发明专利
    NOVEL HETEROCYCLIC COMPOUNDS, METHOD OF OBTAINING THEM AND PHARMACEUTIC AGENT 未知

    公开(公告)号：PL325597A1

    公开(公告)日：1998-09-28

    申请号：PL32559798

    申请日：1998-03-27

    Applicant: HOECHST AG

    Inventor： HEITSCH HOLGER ,  WAGNER ADALBERT ,  WIRTH KLAUS ,  SCHOELKENS BERNWARD

    IPC: A61K31/395 ,  A61K31/47 ,  A61K31/495 ,  A61P1/16 ,  C07D215/24 ,  A61P43/00 ,  C07D215/26 ,  C07D241/36 ,  C07D401/12 ,  C07D405/12 ,  C07D215/00 ,  C07D405/02 ,  C07D401/02

    Abstract: 8-Benzyloxy-(iso)quinoline derivatives (including poly-aza analogues) of formula (I) and their salts are new: D = aza-heterocyclic residue of formula (i) or (ii); X1 = N or CR6; X2 = N or CR7; X3 = N or CR8; B = benzyl variably substituted on the ring by R3-R5; R1, R2 = H, halo or 1-3C alkyl; R3, R4 = H, halo, CN, 1-3C alkyl (optionally substituted by halo), 1-3C alkoxy (optionally substituted by halo), 1-3C alkylthio (optionally substituted by halo), OH, tetrazolyl, CONHR9 or CO2R9; R5 = NO2, NH2, -NR9AYER10 or SO2NR9R10; R6, R8, R'" = H, halo, 1-4C alkyl, 1-4C alkoxy, NH2, NH-(1-4C alkyl), OH, Ar, Ar-(1-4C)-alkanediyl or CO2R9; R7, R', R" = H or 1-4C alkyl; R9 = H, 1-4C alkyl, 2-5C alkenyl or Ar-(1-3C)-alkanediyl; A = divalent residue of an aminocarboxylic acid such as methionine, alanine, phenylalanine, tyrosine, O-methyltyrosine, beta -(2-thienyl)-alanine, glycine, cyclohexylalanine, leucine, isoleucine, valine, norleucine, phenylglycine, serine, cysteine, aminopropionic acid or aminobutyric acid; Y = C=O, C=S or SO2; E = 2-5C alkene-diyl, 1-7C alkanediyl, 3-10C cycloalkanediyl or -(CH2)m-To-(CH2)n (all optionally substituted by one or more groups such as OR12, NO2, CN, CO2R9, NR13R14, SO3R12, SO2NR13R14 or CONR13R14); T = O, S or NR15; m, n = 0-6; o = 0 or 1; p = 1-3; R10 = H or 1-5C alkyl, Ar', Ar'-(1-3C)-alkanediyl or 5-10C heteroaryl (all optionally substituted by one or more groups such as halo, NO2, 1-5C alkylthio, NR13R14, NR13COR16, CO2R9, SO3R12, SO2NR13R14, OR12 or 1-6C alkyl, or Ar', 2-5C alkenyl or OA5 (themselves optionally partially or completely substituted by halo)); R11 = 1-5C alkyl or 1-5C alkoxy (both optionally partially or completely substituted by F or Cl); R12, R13 = H, 1-5C alkyl, 2-5C alkenyl, Ar, Ar-(1-5C)-alkanediyl, 3-10C cycloalkyl, (3-10C)-cycloalkyl-(1-2C)-alkanediyl, CO2-(1-5C alkyl) or CONH-(1-5C alkyl); R14 = H, CO2-(1-3C alkyl) or CO2-(1-3C)-alkanediyl-Ar'; R15 = H, CO2-(1-3C alkyl) or 1-3C alkyl; R16 = 1-3C alkyl, Ar or 5-10C heteroaryl (all optionally substituted by one or more groups such as halo, CN, NO2, NR13R14 or CO2R9); Ar, Ar' = aryl with 6-12C or 6-10C respectively; provided that if D = (ii), then R3 and R4 are not both halo, 1-3C and/or 1-3C alkoxy or H in combination with halo, 1-3C alkyl or 1-3C alkoxy, excluded from this proviso being compounds in which: (a) R5 = -N(R9)-A-Y-E-R10 and R10 = (R11)p-substituted phenyl, provided that if R10 = (R11)p-substituted phenyl then R3 and R4 are not same or different H and halo; and (b) R5 = -SO2NR9R10, provided that R3 and R4 are not both halo.

    ANELLATED N-HETEROCYCLIC RINGS SUBSTITUTED WITH BENZYLOXY-GROUP, PROCESS FOR PRODUCING THEM, AND THEIR USE AS BRADIQUININ-RECEPTOR-ANTAGONISTS
    8.
    发明专利
    ANELLATED N-HETEROCYCLIC RINGS SUBSTITUTED WITH BENZYLOXY-GROUP, PROCESS FOR PRODUCING THEM, AND THEIR USE AS BRADIQUININ-RECEPTOR-ANTAGONISTS 未知

    公开(公告)号：HU9800649D0

    公开(公告)日：1998-05-28

    申请号：HU9800649

    申请日：1998-03-25

    Applicant: HOECHST AG

    Inventor： HEITSCH HOLGER ,  SCHOELKENS BERNWARD ,  WAGNER ADALBERT ,  WIRTH KLAUS

    IPC: C07D215/24 ,  A61K31/395 ,  A61K31/47 ,  A61K31/495 ,  A61P1/16 ,  A61P43/00 ,  C07D215/26 ,  C07D241/36 ,  C07D401/12 ,  C07D405/12

    Abstract: 8-Benzyloxy-(iso)quinoline derivatives (including poly-aza analogues) of formula (I) and their salts are new: D = aza-heterocyclic residue of formula (i) or (ii); X1 = N or CR6; X2 = N or CR7; X3 = N or CR8; B = benzyl variably substituted on the ring by R3-R5; R1, R2 = H, halo or 1-3C alkyl; R3, R4 = H, halo, CN, 1-3C alkyl (optionally substituted by halo), 1-3C alkoxy (optionally substituted by halo), 1-3C alkylthio (optionally substituted by halo), OH, tetrazolyl, CONHR9 or CO2R9; R5 = NO2, NH2, -NR9AYER10 or SO2NR9R10; R6, R8, R'" = H, halo, 1-4C alkyl, 1-4C alkoxy, NH2, NH-(1-4C alkyl), OH, Ar, Ar-(1-4C)-alkanediyl or CO2R9; R7, R', R" = H or 1-4C alkyl; R9 = H, 1-4C alkyl, 2-5C alkenyl or Ar-(1-3C)-alkanediyl; A = divalent residue of an aminocarboxylic acid such as methionine, alanine, phenylalanine, tyrosine, O-methyltyrosine, beta -(2-thienyl)-alanine, glycine, cyclohexylalanine, leucine, isoleucine, valine, norleucine, phenylglycine, serine, cysteine, aminopropionic acid or aminobutyric acid; Y = C=O, C=S or SO2; E = 2-5C alkene-diyl, 1-7C alkanediyl, 3-10C cycloalkanediyl or -(CH2)m-To-(CH2)n (all optionally substituted by one or more groups such as OR12, NO2, CN, CO2R9, NR13R14, SO3R12, SO2NR13R14 or CONR13R14); T = O, S or NR15; m, n = 0-6; o = 0 or 1; p = 1-3; R10 = H or 1-5C alkyl, Ar', Ar'-(1-3C)-alkanediyl or 5-10C heteroaryl (all optionally substituted by one or more groups such as halo, NO2, 1-5C alkylthio, NR13R14, NR13COR16, CO2R9, SO3R12, SO2NR13R14, OR12 or 1-6C alkyl, or Ar', 2-5C alkenyl or OA5 (themselves optionally partially or completely substituted by halo)); R11 = 1-5C alkyl or 1-5C alkoxy (both optionally partially or completely substituted by F or Cl); R12, R13 = H, 1-5C alkyl, 2-5C alkenyl, Ar, Ar-(1-5C)-alkanediyl, 3-10C cycloalkyl, (3-10C)-cycloalkyl-(1-2C)-alkanediyl, CO2-(1-5C alkyl) or CONH-(1-5C alkyl); R14 = H, CO2-(1-3C alkyl) or CO2-(1-3C)-alkanediyl-Ar'; R15 = H, CO2-(1-3C alkyl) or 1-3C alkyl; R16 = 1-3C alkyl, Ar or 5-10C heteroaryl (all optionally substituted by one or more groups such as halo, CN, NO2, NR13R14 or CO2R9); Ar, Ar' = aryl with 6-12C or 6-10C respectively; provided that if D = (ii), then R3 and R4 are not both halo, 1-3C and/or 1-3C alkoxy or H in combination with halo, 1-3C alkyl or 1-3C alkoxy, excluded from this proviso being compounds in which: (a) R5 = -N(R9)-A-Y-E-R10 and R10 = (R11)p-substituted phenyl, provided that if R10 = (R11)p-substituted phenyl then R3 and R4 are not same or different H and halo; and (b) R5 = -SO2NR9R10, provided that R3 and R4 are not both halo.

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