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公开(公告)号:GR3036123T3
公开(公告)日:2001-09-28
申请号:GR20010400976
申请日:2001-06-27
Applicant: HOECHST AG
Inventor: SCHWARK JAN-ROBERT DR , BRENDEL JOACHIM DR , KLEEMANN HEINZ-WERNER , LANG HANS JOCHEN DR , WEICHERT ANDREAS DR , JANSEN HANS-WILLI 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
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:CZ288332B6
公开(公告)日:2001-05-16
申请号:CZ141596
申请日:1996-05-15
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: C07D215/20 , A61K9/06 , A61K9/10 , A61K31/155 , A61K31/17 , A61K31/175 , A61K31/18 , A61K31/27 , A61K31/275 , A61K31/44 , A61K31/4406 , A61K31/4418 , A61K31/47 , A61K31/475 , A61K35/00 , A61P1/16 , A61P3/08 , A61P9/00 , A61P9/06 , A61P9/08 , A61P9/10 , A61P13/02 , A61P15/00 , A61P35/00 , A61P43/00 , C07C279/10 , C07C279/24 , C07C317/22 , C07C317/32 , C07C317/46 , C07D213/30 , C07D215/14 , G01N33/574 , G01N33/94
Abstract: In the present invention there are disclosed substituted benzyloxycarbonyl guanidines and benzylaminocarbonyl guanidines of the general formula I, in which X represents oxygen atom or NR, R represents alkyl containing 1 to 6 carbon atoms, Re1 represents hydrogen, trifluoromethyl, alkylsulfonyl containing 1 to 3 carbon atoms in the alkyl moiety, a halogen or alkyl containing 1 to 6 carbon atoms, Re2 represents hydrogen, pyridyl, alkyl containing 1 to 3 carbon atoms, a quinolyloxy group being optionally substituted with alkyl containing 1 to 3 carbon atoms, alkyl containing 1 to 6 carbon atoms, dialkylamino group containing 1 to 6 carbon atoms in the alkyl moiety, a halogen, a phenoxy group, alkoxy group containing 1 to 6 carbon atoms in the alkoxy moiety or pyridyloxy group, Re3 represents hydrogen, alkylamino group containing 1 to 3 carbon atoms in the alkyl moiety, a halogen, a phenoxy group, alkoxy group containing 1 to 6 carbon atoms in the alkoxy moiety or pyridyloxy group, Re4 represents hydrogen, a halogen or trifluoromethyl, Re5 represents hydrogen, a halogen or trifluoromethyl, Re6 represents hydrogen or alkyl containing 1 to 4 carbon atoms and Re7 represents hydrogen or alkyl containing 1 to 4 carbon atoms, as well as pharmaceutically acceptable salts thereof, further process for preparing these compounds and medicaments containing them. These compounds are efficient inhibitors of cell-exchanging system Nae+/He+ and are therefore very suitable for treating diseases connected with increased exchange of Nae+/He+.
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公开(公告)号:GR3033299T3
公开(公告)日:2000-09-29
申请号:GR20000400981
申请日:2000-04-21
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
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:GR3032293T3
公开(公告)日:2000-04-27
申请号:GR990403381
申请日:1999-12-30
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 , A61P1/16 , A61P9/00 , A61P9/06 , A61P9/08 , A61P9/10 , A61P13/02 , A61P15/00 , A61P35/00 , A61P43/00 , C07C279/10 , C07C279/20 , C07C279/22
Abstract: Ortho-substituted benzoylguanidines of formula (I) and their salts are new: R2, R3 = H, Cl, Br, I, 1-8C alkyl, 3-8C cycloalkyl or OR5; provided that one, but not both of R2 or R3 = H; R5 = 1-8C alkyl, or CdH2d-(3-8C cycloalkyl); and d = 0-2.
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公开(公告)号:DK0791577T3
公开(公告)日:2000-04-25
申请号:DK97100777
申请日:1997-01-20
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 , A61P1/16 , A61P9/00 , A61P9/06 , A61P9/08 , A61P9/10 , A61P13/02 , A61P15/00 , A61P35/00 , A61P43/00 , C07C279/10 , C07C279/20 , C07C279/22
Abstract: Ortho-substituted benzoylguanidines of formula (I) and their salts are new: R2, R3 = H, Cl, Br, I, 1-8C alkyl, 3-8C cycloalkyl or OR5; provided that one, but not both of R2 or R3 = H; R5 = 1-8C alkyl, or CdH2d-(3-8C cycloalkyl); and d = 0-2.
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公开(公告)号:CZ9800539A3
公开(公告)日:1998-09-16
申请号:CZ53998
申请日:1998-02-24
Applicant: HOECHST AG
Inventor: BRENDEL JOACHIM DR , LANG HANS JOCHEN DR , GERLACH UWE DR
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
CPC classification number: C07C311/07 , C07C2602/12 , C07D313/08
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公开(公告)号:CZ53998A3
公开(公告)日:1998-09-16
申请号:CZ53998
申请日:1998-02-24
Applicant: HOECHST AG
Inventor: BRENDEL JOACHIM DR , LANG HANS JOCHEN DR , GERLACH UWE DR
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.
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公开(公告)号:CZ9603383A3
公开(公告)日:1998-05-13
申请号:CZ338396
申请日:1996-11-18
Applicant: HOECHST AG
Inventor: KLEEMANN HEINZ-WERNER DR , BRENDEL JOACHIM DR , SCHWARK JAN-ROBERT DR , WEICHERT ANDREAS DR , LANG HANS JOCHEM DR , ALBUS UDO DR , SCHOLZ WOLFGANG DR
IPC: A61K31/165 , A61P1/16 , A61P3/08 , A61P9/08 , A61P9/10 , A61P11/00 , A61P13/02 , A61P15/00 , A61P35/00 , A61P43/00 , C07C279/20 , C07C279/22
CPC classification number: C07C279/22
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公开(公告)号:CZ65497A3
公开(公告)日:1998-05-13
申请号:CZ65497
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: A61K31/165 , A01N1/02 , A61K31/155 , A61P3/10 , A61P9/00 , A61P9/06 , A61P9/08 , A61P9/10 , A61P9/12 , A61P13/08 , A61P25/00 , A61P35/00 , A61P43/00 , C07C279/10 , C07C279/20 , C07C279/22
Abstract: Ortho-substituted benzoyl-guanidines of formula (I) and their salts are new: where R1 = H, F, Cl, Br, I, CN, NO2, 1-8C alkyl, 1-8C alkoxy, 3-8C cycloalkyl, 3-8C cycloalkoxy, Xa-(CH2)b-(CF2)c-CF3, SR10, OR10, CR10R11R12; or phenyl, naphthyl, biphenylyl, or 1-9C (sic) heteroaryl bonded via C or N and all optionally mono- to tri-substituted with F, Cl, CF3, CH3, methoxy, OH, NH2, NHCH3, NH(CH3)2; or SR13, OR13, NHR13, NR13R14, CHR13R15, CR15R16-OH, C IDENTICAL CR18, CR19=CHR18, ÄCR20R21Ük-CO, ÄCR22R23Ül-R24; one of R2, R3 = hydroxy the other as R1; R4 = 1-4C alkyl, 1-4C alkoxy, F, Cl, Br, I or (CH2)n-(CF2)o-CF3; X = O, S, NR5; a = 0-1; b = 0-2; c = 0-3; R5 = H, 1-4C alkyl, CdH2d-R6; d = 0-4; R6 = 3-8C cycloalkyl; or phenyl, biphenylyl or naphthyl (each optionally mono- to tri-substituted with F, Cl, CF3, methyl, methoxy, or NR7R8); R7, R8 = H or 1-4C alkyl; R10 = CfH2f-3-8C cycloalkyl; or phenyl optionally mono- to tri-substituted with F, Cl, CF3, CH3, methoxy, OH, NH2, NHCH3, NH(CH3)2; f = 0-2; R11, R12 = as R10, H or 1-4C alkyl; k = 0-4; l = 0-4; R13, R14 = (CH2)g-(CHOH)h-(CH2)i-(CHOH)j-R17, or (CH2)g-O-(CH2CH2O)h-R24; R17 = H, CH3; g, h, i = 0-4; j = 1-4; R15, R16 = H or 1-6C alkyl; or CR15R16 = 3-8C cycloalkyl; R18 = phenyl optionally mono- to tri-substituted with F, Cl, CF3, CH3, OCH3 or NR25R26; or 3-8C cycloalkyl; or 1-9C (sic) heteroaryl optionally substituted as for phenyl; or 1-6C alkyl optionally substituted by 1-3 OH; R25, R26 = H or 1-4C alkyl; R19-R23 = H or CH3; R24 = H, 1-6C alkyl, 3-8C cycloalkyl, CmH2m-R18; m = 1-4; n = 0-1; and o = 0-1.
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公开(公告)号:CZ265997A3
公开(公告)日:1998-03-18
申请号:CZ265997
申请日:1997-08-20
Applicant: HOECHST AG
Inventor: SCHWARK JAN-ROBERT DR , BRENDEL JOACHIM DR , KLEEMANN HEINZ-WERNER DR , LANG HANS JOCHEN DR , WEICHERT ANDREAS DR , JANSEN HANS-WILLI 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
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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