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    41.
    发明专利
    未知

    公开(公告)号：TR199800301A2

    公开(公告)日：1998-09-21

    申请号：TR9800301

    申请日：1998-02-24

    Applicant: HOECHST AG

    Inventor： BRENDEL JOACHIM ,  LANG HANS JOCHEN ,  GERLACH UWE

    IPC: C07D239/24 ,  A61K31/18 ,  A61K31/335 ,  A61K31/38 ,  A61K31/39 ,  A61K31/495 ,  A61P1/00 ,  A61P9/00 ,  C07C311/07 ,  C07D239/70 ,  C07D313/08 ,  C07D321/02 ,  C07D321/06 ,  C07D

    Abstract: Benzoxepine and benzocycloheptane derivatives of formula (I), their stereoisomers and salts are new. X1 = O, S, SO, SO2, CR1R2, NR6, CO or CR1R7; R1, R2 = H, CF3, C2F5, C3F7, 1-6C alkyl or phenyl (optionally substituted by 1 or 2 of halo, CF3, NO2, CN, NH2, OH, Me, Et, OMe, NMe2, SO2NH2, SO2Me and NHSO2Me; or R1+R2 = 2-10C alkylene; R6 = H or CnH2nR8 (with one CH2 group optionally replaced by O, CH=CH, C IDENTICAL C, CO, COO, OCO, S, SO, SO2, NR9 or CONR9; R9 = H or 1-4C alkyl; n = 0-8; R8 = H, CF3, C2F5, C3F7, 3-8C cycloalkyl, NMe2, NEt2, piperidino, pyrrolidino, morpholino, 4-methyl-1-piperazinyl or pyridyl, thienyl, imidazolyl or phenyl (all optionally substituted by 1 or 2 halo, CF3, NO2, CN, NH2, OH, Me, Et, OMe, NMe2, SO2NH2, SO2Me and NHSO2Me); X2 = CR1R2 or CR2R10; or X2 = O, S, SO, SO2 or NR6 if X3 and X1 are CR1R2; R10+R7 = bond; X3 = CR1R2; or X3 = O, S, SO, SO2 or NR6 if X2 and X4 are CR1R2; X4 = CR1R2, NR6, NR11, CH(OR30) or CR2R11; R30 = H, 1-3C alkyl or 1-4C acyl; R11+R5 = bond; Y1-Y4 = CR12 or N with no more than two being N; R12 = H, halo, 1-5C alkyl, 3-8C cycloalkyl, CN, CF3, C2F5, C3F7, N3, NO2, ZCmH2mR13 or phenyl (optionally substituted by 1 or 2 halo, CF3, NO2, CN, NH2, OH, Me, Et, OMe, NMe2, SO2NH2, SO2Me and NHSO2Me); Z = O, CO, COO, OCO, S, SO, SO2, SO2NR14, NR14 or CONR14; R14 = H or 1-3C alkyl; m = 0-6; R13 = H, CF3, C2F5, C3F7, 3-8C cycloalkyl, NR15R16, CONR15R16, OR30a or phenyl, thienyl or 1-9C N-containing heterocyclyl (all optionally substituted by 1 or 2 halo, CF3, NO2, CN, NH2, OH, Me, Et, OMe, NMe2, SO2NH2, SO2Me and NHSO2Me); R15, R16 = H or 1-3C alkyl; or R15+R16 = 4-5C methylene (with one carbon optionally replaced by O, S, NH, NMe or N(benzyl)); R30a = H, 1-3C alkyl or 1-4C acyl; or Y1+Y2 = S and Y3, Y4 = CR12; R3 = NR18CxH2xR17 or CxH2xR17 (with one CH2 group optionally replaced by O, CO, S, SO, SO2 or NR19); R19 = H, Me or Et; R17 = H, Me, 3-8C cycloalkyl, CF3, C2F5 or C3F7; x = 0-10; R18 = H or 1-8C alkyl; or R18+R17 = bond if x = 3-10; or R3 = phenyl (optionally substituted by 1 or 2 halo, CF3, NO2, CN, NH2, OH, Me, Et, OMe, NMe2, SO2NH2, SO2Me and NHSO2Me); or R3+R4 = 3-8C alkylene (with one CH2 optionally replaced by O, CO, S, SO or SO2); R4 = CrH2rR20 (with one CH2 group optionally replaced by O, CH=CH, C IDENTICAL C, CO, COO, OCO, S, SO, SO2, NR21 or CONR21); R21 = H or 1-3C alkyl; r = 0-20; R20 = H, CF3, C2F5, C3F7, 3-8C cycloalkyl, NR22R23 or phenyl, thienyl or 1-9C N-containing heterocyclyl (all optionally substituted by 1 or 2 halo, CF3, NO2, CN, NH2, OH, Me, Et, OMe, NMe2, SO2NH2, SO2Me and NHSO2Me); R22, R23 = H or 1-3C alkyl; or R22+R23 = 4-5C methylene (with one carbon optionally replaced by O, S, NH, NMe or N(benzyl)); and R5 = H; or R5+R11 = bond.

    Sulfonamide-substituted fused 7-membered ring compounds, their use as a medicament, and pharmaceutical comprising them
    42.
    发明专利
    Sulfonamide-substituted fused 7-membered ring compounds, their use as a medicament, and pharmaceutical comprising them 未知

    公开(公告)号：AU5633398A

    公开(公告)日：1998-09-03

    申请号：AU5633398

    申请日：1998-02-25

    Applicant: HOECHST AG

    Inventor： BRENDEL JOACHIM ,  LANG HANS JOCHEN ,  GERLACH UWE

    IPC: C07D239/24 ,  A61K31/18 ,  A61K31/335 ,  A61K31/38 ,  A61K31/39 ,  A61K31/495 ,  A61P1/00 ,  A61P9/00 ,  C07C311/07 ,  C07D239/70 ,  C07D313/08 ,  C07D321/02 ,  C07D321/06

    Abstract: Benzoxepine and benzocycloheptane derivatives of formula (I), their stereoisomers and salts are new. X1 = O, S, SO, SO2, CR1R2, NR6, CO or CR1R7; R1, R2 = H, CF3, C2F5, C3F7, 1-6C alkyl or phenyl (optionally substituted by 1 or 2 of halo, CF3, NO2, CN, NH2, OH, Me, Et, OMe, NMe2, SO2NH2, SO2Me and NHSO2Me; or R1+R2 = 2-10C alkylene; R6 = H or CnH2nR8 (with one CH2 group optionally replaced by O, CH=CH, C IDENTICAL C, CO, COO, OCO, S, SO, SO2, NR9 or CONR9; R9 = H or 1-4C alkyl; n = 0-8; R8 = H, CF3, C2F5, C3F7, 3-8C cycloalkyl, NMe2, NEt2, piperidino, pyrrolidino, morpholino, 4-methyl-1-piperazinyl or pyridyl, thienyl, imidazolyl or phenyl (all optionally substituted by 1 or 2 halo, CF3, NO2, CN, NH2, OH, Me, Et, OMe, NMe2, SO2NH2, SO2Me and NHSO2Me); X2 = CR1R2 or CR2R10; or X2 = O, S, SO, SO2 or NR6 if X3 and X1 are CR1R2; R10+R7 = bond; X3 = CR1R2; or X3 = O, S, SO, SO2 or NR6 if X2 and X4 are CR1R2; X4 = CR1R2, NR6, NR11, CH(OR30) or CR2R11; R30 = H, 1-3C alkyl or 1-4C acyl; R11+R5 = bond; Y1-Y4 = CR12 or N with no more than two being N; R12 = H, halo, 1-5C alkyl, 3-8C cycloalkyl, CN, CF3, C2F5, C3F7, N3, NO2, ZCmH2mR13 or phenyl (optionally substituted by 1 or 2 halo, CF3, NO2, CN, NH2, OH, Me, Et, OMe, NMe2, SO2NH2, SO2Me and NHSO2Me); Z = O, CO, COO, OCO, S, SO, SO2, SO2NR14, NR14 or CONR14; R14 = H or 1-3C alkyl; m = 0-6; R13 = H, CF3, C2F5, C3F7, 3-8C cycloalkyl, NR15R16, CONR15R16, OR30a or phenyl, thienyl or 1-9C N-containing heterocyclyl (all optionally substituted by 1 or 2 halo, CF3, NO2, CN, NH2, OH, Me, Et, OMe, NMe2, SO2NH2, SO2Me and NHSO2Me); R15, R16 = H or 1-3C alkyl; or R15+R16 = 4-5C methylene (with one carbon optionally replaced by O, S, NH, NMe or N(benzyl)); R30a = H, 1-3C alkyl or 1-4C acyl; or Y1+Y2 = S and Y3, Y4 = CR12; R3 = NR18CxH2xR17 or CxH2xR17 (with one CH2 group optionally replaced by O, CO, S, SO, SO2 or NR19); R19 = H, Me or Et; R17 = H, Me, 3-8C cycloalkyl, CF3, C2F5 or C3F7; x = 0-10; R18 = H or 1-8C alkyl; or R18+R17 = bond if x = 3-10; or R3 = phenyl (optionally substituted by 1 or 2 halo, CF3, NO2, CN, NH2, OH, Me, Et, OMe, NMe2, SO2NH2, SO2Me and NHSO2Me); or R3+R4 = 3-8C alkylene (with one CH2 optionally replaced by O, CO, S, SO or SO2); R4 = CrH2rR20 (with one CH2 group optionally replaced by O, CH=CH, C IDENTICAL C, CO, COO, OCO, S, SO, SO2, NR21 or CONR21); R21 = H or 1-3C alkyl; r = 0-20; R20 = H, CF3, C2F5, C3F7, 3-8C cycloalkyl, NR22R23 or phenyl, thienyl or 1-9C N-containing heterocyclyl (all optionally substituted by 1 or 2 halo, CF3, NO2, CN, NH2, OH, Me, Et, OMe, NMe2, SO2NH2, SO2Me and NHSO2Me); R22, R23 = H or 1-3C alkyl; or R22+R23 = 4-5C methylene (with one carbon optionally replaced by O, S, NH, NMe or N(benzyl)); and R5 = H; or R5+R11 = bond.

    46.
    发明专利
    未知

    公开(公告)号：BR9703338A

    公开(公告)日：1998-08-18

    申请号：BR9703338

    申请日：1997-05-30

    Applicant: HOECHST AG

    Inventor： LAL BANSI ,  ENGLERT HEINRICK CHRISTIAN ,  LANG HANS JOCHEN ,  BRENDEL JOACHIM ,  SCHWARK JAN-ROBERT ,  KLEEMANN HEINZ WERNER ,  WEICHERT ANDREAS

    IPC: C07D295/14 ,  A01N1/02 ,  A01N47/44 ,  A61K31/155 ,  A61K31/165 ,  A61K31/27 ,  A61K31/44 ,  A61K31/495 ,  A61K31/535 ,  A61K31/5375 ,  A61P3/06 ,  A61P9/00 ,  A61P9/06 ,  A61P9/10 ,  A61P35/00 ,  A61P43/00 ,  C07C271/22 ,  C07C277/08 ,  C07C279/20 ,  C07C279/22 ,  C07C311/19 ,  C07C317/50 ,  C07C323/62 ,  C07D213/40 ,  C07D213/75 ,  C07D295/08 ,  C07D295/088

    Abstract: 2-Naphthoyl-guanidines (I) and their salts are new: R1 and R3-R8 = H; F; Cl; Br; I; CN; NO2; CF3; C2F5; VpQqU; XYaWZ; or X'YaWZ' (at least 1 is XYaWZ or X'YaWZ'); V = O; S; SO; SO2; NR60; OCO; CO; CONR60; COO; or CR66R67; Q = 1-8C alkylene with 1 CH2 optionally replaced by O, S, NR13 or o-, m- or p-phenylene; U = H; 1-7C alkyl; 3-7C cycloalkyl; COR65; SO2R65; NR61R62; or Ph or a N- or C-linked N-containing 1-9C heterocycle optionally mono-, di- or trisubstituted by F, Cl, Br, CF3, Me, OMe or NR63R64; p, q = 0 or 1; X = O; S; NR10; or CR11R12; Y = 1-8C alkylene with 1 CH2 optionally replaced by O, S, NR13 or o-, m- or p-phenylene; W = CH2; SO2; S(O)(NH); or (when W is not attached directly to a hetero atom of XYa) O or NR14; Z = COR15; SO2R15; or (when W is not O or NR14) NR16R17; a = 0 or 1; X' = CO, CONR30, COO, SO, SO2, SO2NR30, OCO, NR30CO or NR30SO2 linked with the ring via the left hand atom; Z' = COR15; SO2R15; a N- or C-linked N-containing 1-9C heterocycle optionally mono-, di- or trisubstituted by F, Cl, Br, CF3, Me, OMe or NR21R22; or (when W is not O or NR14) Z' is NR16R17; R10-R12 = H; 1-6C alkyl; 1-4C perfluoroalkyl; or 3-7C cycloalkyl; R13, R14, R68 = H; 1-6C alkyl; 1-4C perfluoroalkyl; or 3-6C cycloalkyl; R15 = N=C(NH2)2; NR18R19; N(CH2)bNR18R19; or OR20; b = 2 or 3; R16 - R19 = H; 1-8C alkyl; or 1-4C perfluoroalkyl; or R16+R17 or R18+R19 = tetra- or pentamethylene with 1 CH2 optionally replaced by O, S or NA; A = H; Me; benzyl; or p-Cl-Ph; R20, R30; R60; R66; R67 = H; 1-6C alkyl; 1-4C perfluoroalkyl; or 3-7C cycloalkyl; R21, R22; R63, R64 = H; 1-4C alkyl; or 1-4C perfluoroalkyl; R65 = N=C(NH2)2; NR61R62; or OR60; R61, R62 = H; 1-8C alkyl; or 1-4C perfluoroalkyl; or R61+R62 = tetra- or pentamethylene with 1 CH2 optionally replaced by O, S or NA; provided that at least one of R5-R8 is not H.

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