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公开(公告)号:ID18066A
公开(公告)日:1998-02-26
申请号:ID972923
申请日:1997-08-21
Applicant: HOECHST AG
Inventor: SCHWARK JAN ROBERT DR , BRENDEL JOACHIM DR , LANG HEINZ WERNER JOCHEN DR , WEICHERT ANDREAS DR , JANSEN HANS WLLI DR , SCHOLZ WOLFGANG DR
IPC: C07D213/65 , A01N1/00 , A61K31/155 , A61K31/165 , A61K31/44 , A61K31/4406 , A61P3/06 , A61P9/00 , A61P9/06 , A61P9/10 , A61P13/02 , A61P15/00 , A61P25/00 , A61P43/00 , C07C277/08 , C07C279/20 , C07C279/22 , C07C279/00
Abstract: Phenyl-substituted alkenyl-carboxylic acid guanidide compounds of formula (I) are new. T = a group (i); Ra = H, F, Cl, Br, I , CN, OH, OR6, 1-4C alkyl, Or-(CH2)aCbF2b+1, 3-8C cycloalkyl or NR7R8; r = 0 or 1; a = 0 - 4; b = 1 - 4; R6 = 1-4C alkyl, 1-4C perfluoroalkyl, 3-6C alkenyl, 3-8C cycloalkyl, phenyl or benzyl; where the phenyl nucleus is optionally substituted by 1 - 3 F, Cl, CF3, CH3, OCH3 or NR9R10 groups; R9, R10 = H, 1-4C alkyl or 1-4C perfluoroalkyl; R7, R8 = as for R6; or R7+R8 = (CH2)4 or (CH2)5, where one of the CH2 groups may be replaced by O, S, NH, N-CH3 or N-benzyl; Rb, Rc, Rd = as for Ra; x, y = 0 - 2; Rf = H, F, Cl, Br, I, CN, OR12, 1-8C alkyl, Op-(CH2)f-CgF2g+1, 3-8C cycloalkyl or 1-9C heteroaryl; p = 0 or 1; f = 0 - 4; g = 1 - 8; R12 = 1-8C alkyl, 1-4C perfluoroalkyl, 3-8C alkenyl, 3-8C cycloalkyl, phenyl or benzyl; where the phenyl nucleus may be substituted by 1 - 3 F, Cl, CF3, CH3, OCH3 or NR13R14 groups; R13, R14 = H, 1-4C alkyl or 1-4C perfluoroalkyl; Re = as for Rf; R1 = as for T, or is H, Ok-CmH2m+1, On-(CH2)p-CqF2q+1, F, Cl, Br, I, CN, CO-N=C(NH2)2, SOr1R17, SOr2-NR31R32, Ou-(CH2)v-C6H5, Ou2-(1-9C heteroaryl) (sic) or Su2-(1-9C heteroaryl) (sic); k, n = 0 or 1; m = 0-8; q = 1 - 8; p = 0-4; r1, r2 = 0 - 2; R31, R32 = H, 1-8C alkyl or 1-8C perfluoroalkyl, or R31+R32 = (CH2)4 or (CH2)5, where one of the CH2 groups may be replaced by O, S, NH, N-CH3 or N-benzyl; R17 = 1-8C alkyl; u, u2 = 0 or 1; v = 0- 4. The phenyl nucleus may be substituted by 1-3 F, Cl, CF3, CH3, OCH3, (CH2)w-NR21R22, NR18R19 or 1-9C heteroaryl groups ÄsicÜ. R18, R19, R21, R22 = 1-4C alkyl or 1-4C perfluoroalkyl; w = 1 - 4; The heterocycle of the 1-9C heteroaryl may be substituted by 1 - 3 F, Cl, CF3, CH3 or OCH3 groups. R2, R3, R4 and R5 = as for R1; or R1+R2 or R2+R3 = CH-CH=CH-CH, which is optionally substituted by 1 - 3 F, Cl, CF3, CH3, OCH3, (CH2)w2-NR24R25 or NR26R27; R24, R25, R26, R27 = H, 1-4C alkyl or 1-4C perfluoroalkyl; w2 = 1 - 4; provided that T is present 2-3 times in the molecule.
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公开(公告)号:DE19624178A1
公开(公告)日:1998-01-08
申请号:DE19624178
申请日:1996-06-18
Applicant: HOECHST AG
Inventor: WEICHERT ANDREAS DR , BRENDEL JOACHIM DR , KLEEMANN HEINZ-WERNER DR , LANG HANS JOCHEN DR , SCHWARK JAN-ROBERT DR , ALBUS UDO DR , SCHOLZ WOLFGANG DR
IPC: A61K31/165 , A01N1/02 , A01N47/44 , A61K31/10 , A61K31/155 , A61K31/18 , A61P3/06 , A61P3/10 , A61P9/00 , A61P9/06 , A61P9/08 , A61P9/10 , A61P35/00 , A61P43/00 , C07C279/10 , C07C279/20 , C07C279/22 , C07C303/40 , C07C311/19 , C07C311/47 , C07C317/42 , C07C317/50 , C07C317/46 , C07C303/30 , C07C311/15 , G01N33/50
Abstract: Benzoylguanidine compounds of formula (I) and their salts are new. R1 = R13-SOm or R14R15N-SO2; m = 1 or 2; R13 = 1-8C alkyl or perfluoroalkyl, 3-8C alkenyl or CnH2n-R16; n = 0-4; R16 = 3-8C cycloalkyl or phenyl, biphenyl or naphthyl (each optionally substituted by 1-3 F, Cl, CF3, CH3, OCH3 or NR25R26); R25, R26 = H or 1-4C alkyl or perfluoroalkyl; R14 = H, 1-8C alkyl or perfluoroalkyl, 3-8C alkenyl or CnH2n-R27; R27 = 3-8C cycloalkyl or phenyl, biphenyl or naphthyl (each optionally substituted by 1-3 F, Cl, CF3, CH3, OCH3 or NR28R29); R28, R29, R15 = H, or 1-4C alkyl or perfluoroalkyl; or R14+R15 = (CH2)a where one CH2 group may be replaced by O, S, NH, N-CH3 or N-benzyl; a = 4-5; one of R2, R3 = H and the other = CHR30R31 or C(OH)R33R34; R30 = (CH2)g-(CHOH)h-(CH2)i-(CHOH)k-R32 or (CH2)g-O-(CH2-CH2O)h-R24; R24, R32 = H or Me; g, h, i = 0-4; k = 1-4; R31, R33, R34 = H or 1-4C alkyl; or R33+R34 = 3-6C cycloalkyl; or R33 = CH2OH; R4 = 1-4C alkyl or alkoxy or F, Cl, Br, I, CN, (CH2)n'-(CF2)o-CF3; n' = 0-1; and o = 0-2.
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公开(公告)号:DE19622370A1
公开(公告)日:1997-12-11
申请号:DE19622370
申请日:1996-06-04
Applicant: HOECHST AG
Inventor: ALBUS UDO DR , BRENDEL JOACHIM DR , KLEEMANN HEINZ-WERNER DR , LANG HANS JOCHEN DR , SCHOLZ WOLFGANG DR , SCHWARK JAN-ROBERT DR , WEICHERT ANDREAS DR
IPC: A61K31/165 , A01N1/02 , A01N47/44 , A61K31/155 , A61P3/00 , A61P3/06 , A61P7/04 , A61P9/00 , A61P9/06 , A61P9/08 , A61P9/10 , A61P35/00 , C07C279/22 , C07C319/20 , C07C323/62 , C07C277/08 , C07D215/12 , C07D217/12 , C07D213/24 , C07D227/04
Abstract: Ortho-substituted benzoyl-guanidines of formula (I) and their salts are new: R = H; F; Cl; Br; I; CN; NO2; 1-8 C alkyl; 1-8 C alkoxy; 3-8 C cycloalkyl; 3-8 C cycloalkoxy; Xa-(CH2)b-(CF2)c-CF3; SR ; OR ; CR R R ; Ph, etc.;R or R = OCOR and the other = R ;R , R = H; 1-4C alkyl; 1-4C alkoxy; etc.;X = e.g. O; a = 0 or 1;b = 0-2;c = 0-3;R = -CfH2f-Q;Q = e.g. 3-8 C cycloalkyl;f = 0-2; R , R = H; 1-4 C alkyl; or R ; R = e.g. 1-8C alkyl.
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公开(公告)号:ID16989A
公开(公告)日:1997-11-27
申请号:ID971814
申请日:1997-05-28
Applicant: HOECHST AG
Inventor: BRENDEL JOACHIM DR , KLEEMANN HEINZ-WERNER DR , ENGLERT HEINRICH CHRISTIAN DR , LANG HANS JOCHEN DR , SCHWARK JAN ROBERT DR , WEICHERT ANDREAS DR , LAL BANSI DR
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 , C07C279/00
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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公开(公告)号:ID16988A
公开(公告)日:1997-11-27
申请号:ID971812
申请日:1997-05-28
Applicant: HOECHST AG
Inventor: ALBUS UDO DR , BRENDEL JOACHIM DR , KLEEMANN HEINZ WERNER DR , LANG HANS JOCHEN DR , SCHOLZ WOLFGANG DR , SCHWARK JAN ROBERT DR , WEICHERT ANDREAS DR
IPC: A61K31/165 , A61K31/155 , A61P3/06 , A61P9/00 , A61P9/10 , C07C277/06 , C07C279/22 , C07C311/15 , C07C317/44 , C07C323/62 , C07C279/00
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公开(公告)号:ID16108A
公开(公告)日:1997-09-04
申请号:ID970651
申请日:1997-03-03
Applicant: HOECHST AG
Inventor: ALBUS UDO DR , BRENDEL JOACHIM DR , KLEEMANN HEINZ-WERNER DR , LANG HANS JOCHEN DR , SCHOLZ WOLFGANG DR , SCHWARK JAN ROBERT DR , WEICHERT ANDREAS DR
IPC: A61K31/155
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公开(公告)号:DE19605610A1
公开(公告)日:1997-08-21
申请号:DE19605610
申请日:1996-02-15
Applicant: HOECHST AG
Inventor: SCHWARK JAN-ROBERT DR , BRENDEL JOACHIM DR , KLEEMANN HEINZ-WERNER DR , LANG HANS JOCHEN DR , WEICHERT ANDREAS DR , ALBUS UDO DR , SCHOLZ WOLFGANG DR
IPC: C07D333/24 , A61K31/38 , A61K31/381 , A61P9/00 , A61P9/06 , A61P9/08 , A61P9/10 , A61P35/00 , A61P43/00 , C07C279/22 , C07D333/02 , C07D333/34 , C07D409/04 , C07D417/04 , A01N1/02
Abstract: Thiophenylalkenylcarboxylic acid guanidide derivatives of formula (I) and their salts are new. at least one of R1-R3 = Op(CH2)sCqF2q+1, R40CO or R31SOk; and the others = H, F, Cl, Br, I, CN, OnaCmaH2ma+1 or OgaCraH2raR10; p = 0 or 1; s = 0-4; q = 1-8; k = 0-2; R40, R31 = 1-8C alkyl, 1-8C perfluoroalkyl, 3-8C cycloalkyl or Ph (optionally substituted by 1-3 F, Cl, CF3, Me or OMe) or NR41R42; R41,R42 = H, 1-4C alkyl or 1-4C perfluoroalkyl; or R41+R42 = (CH2)x in which a CH2 group may be replaced by O, S, NH, NMe or N-benzyl; x = 4 or 5; na = 0 or 1; ma = 0-8; ga = 0 or 1; ra = 0-4; R10 = 3-8C cycloalkyl or Ph (optionally substituted by 1-3 F, Cl, CF3, Me or OMe); R4, R5 = H, F, Cl, Br, I, CN, 1-8C alkyl, 1-8C perfluoroalkyl, 3-8C cycloalkyl or Ph (optionally substituted by 1-3 F, Cl, CF3, Me, OMe or NR14R15); R14, R15 = H, 1-4C alkyl or 1-4C perfluoroalkyl.
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公开(公告)号:CZ9602808A3
公开(公告)日:1997-06-11
申请号:CZ280896
申请日:1996-09-25
Applicant: HOECHST AG
Inventor: WEICHERT ANDREAS DR , BRENDEL JOACHIM DR , KLEEMANN HEINZ WERNER DR , LANG HANS JOCHEN , SCHWARK JAN ROBERT DR , ALBUS UDO DR , SCHOLZ WOLFGANG DR
IPC: A61K49/00 , A61K31/155 , A61K31/165 , A61P1/16 , A61P3/08 , A61P9/00 , A61P9/06 , A61P9/08 , A61P9/10 , A61P11/00 , A61P13/02 , A61P15/00 , A61P35/00 , A61P43/00 , C07C277/00 , C07C279/22
CPC classification number: C07C279/22
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公开(公告)号:DE19543194A1
公开(公告)日:1997-05-22
申请号:DE19543194
申请日:1995-11-20
Applicant: HOECHST AG
Inventor: KLEEMANN HEINZ-WERNER DR , BRENDEL JOACHIM DR , SCHWARK JAN-ROBERT DR , WEICHERT ANDREAS DR , LANG HANS-JOCHEN DR , ALBUS UDO DR , SCHOLZ WOLFGANG DR
IPC: C07C279/22 , A01N1/02 , A61K31/155 , A61K49/00 , C07C277/08 , C07D207/33 , C07D227/04
Abstract: Benzenedicarboxylic acid diguanidides of formula (I) are new: one of R1, R2, R3 and R5 = -CO-N=C(NH2)2 and the others are as follows: R1 and R5 = H, 1-4C alkyl, F, etc.;R2 = H, halo, OH, CN, CF3, CO-N=C(NH2)2, 1-8C alkyl, 2-8C alkenyl, (CH2)mR14, SO2R22, CONR23R24, COR28, SO2NR29R30, OR35 or NR35R36; and R3 = H, SR25, OR25, NR25R26 or CR25R26R27; while R4 = e.g. CF3; m = 0-2; R14 = e.g. 3-8C cycloalkyl; R22, R28 = e.g. Me; R23, R24, R29, R30 = e.g. H; R35, R36 = H or 1-6C alkyl; or R35+R36 = e.g. 4-7 CH2 gps.; R25 = H, 1-8C alkyl, etc.; R26, R27 = H, 1-8C alkyl or groups as defined for R25.
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公开(公告)号:DE19542306A1
公开(公告)日:1997-05-15
申请号:DE19542306
申请日:1995-11-14
Applicant: HOECHST AG
Inventor: KLEEMANN HEINZ-WERNER DR , BRENDEL JOACHIM DR , SCHWARK JAN-ROBERT DR , WEICHERT ANDREAS DR , LANG HANS-JOCHEN DR , ALBUS UDO DR , SCHOLZ WOLFGANG DR
IPC: C07D213/65 , A61K31/18 , A61K31/44 , A61P1/16 , A61P3/08 , A61P9/08 , A61P9/10 , A61P11/00 , A61P13/02 , A61P15/00 , A61P35/00 , A61P43/00 , C07C303/34 , C07C303/40 , C07C307/10 , C07C311/08 , C07D213/62 , C07C311/00 , C07C323/63 , A01N1/02
Abstract: 3-Sulphonylamino-benzoylguanidine derivatives of formula (I) and their salts are new. R1 = 1-8C alkyl or NR7R8; R7, R8 = H or 1-8C alkyl; R2 = H, 1-8C alkyl or SO2R9; R9 = as R1; R3 = H, 1-8C alkyl, SR25, OR25, NR25R26 or CR25R26R27; R25 = H, 1-8C alkyl, phenyl (optionally substituted by 1-3 of F, Cl, CF3, Me, OMe, OH, NH2, NHMe and NMe2) or 1-9C heteroaryl (optionally substituted as for phenyl); R26, R27 = H, 1-8C alkyl or as for R25; R4 = H, halo, OH, CN, CF3, 1-8C alkyl, 2-8C alkenyl or -(CH2)mR14; m = 0-2; R14 = 3-8C cycloalkyl or phenyl (optionally substituted by 1-3 of F, Cl, CF3, Me, OMe or NR15R16); R15, R15 = H or Me; R5, R6 = H, 1-4C alkyl, F, Cl, OR32, NR32R34 or CF3; R32-R34 = H or 1-4C alkyl.
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