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    PHENYL-SUBSTITUTED ALKENOYLGUANIDIDES, PROCESS FOR THEIR PREPARATION, THEIR USE AS DRUGS OR DIAGNOSTIC AGENTS AND DRUGS CONTAINING THEM
    16.
    发明专利
    PHENYL-SUBSTITUTED ALKENOYLGUANIDIDES, PROCESS FOR THEIR PREPARATION, THEIR USE AS DRUGS OR DIAGNOSTIC AGENTS AND DRUGS CONTAINING THEM 未知

    公开(公告)号：HRP970450B1

    公开(公告)日：2003-02-28

    申请号：HRP970450

    申请日：1997-08-21

    Applicant: HOECHST AG

    Inventor： SCHWARK JAN-ROBERT ,  BRENDEL JOACHIM ,  KLEEMANN HEINZ-WERNER ,  LANG HANS-JOCHEN ,  WEICHERT ANDREAS ,  JANSEN HANS-WILLI ,  SCHOLZ WOLFGANG

    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.

    SUBSTITUTED BENZYLOXYCARBONYL GUANIDINES,PROCESSES FOR THEIR PREPARATION, THEIR USE AS MEDICINAL OR DIAGNOSTIC AGENTS AS WELL AS MEDICAMENTS CONTAINING THEM
    18.
    发明专利
    SUBSTITUTED BENZYLOXYCARBONYL GUANIDINES,PROCESSES FOR THEIR PREPARATION, THEIR USE AS MEDICINAL OR DIAGNOSTIC AGENTS AS WELL AS MEDICAMENTS CONTAINING THEM 未知

    公开(公告)号：HRP960221B1

    公开(公告)日：2002-02-28

    申请号：HRP960221

    申请日：1996-05-15

    Applicant: HOECHST AG

    Inventor： KLEEMANN HEINZ-WERNER ,  BRENDEL JOACHIM ,  SCHWARK JAN-ROBERT ,  WEICHERT ANDREAS ,  LANG HANS-JOCHEN ,  ALBUS UDO ,  SCHOLZ WOLFGANG

    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: Phenylalkyl (oxy or amino) carbonylguanidine cpds. of formula (I) are new. R1-R3 = Y-Phe, Py, Q-Phe', Het, SR25, OR25, NR25R26, CR25R26R27, En-CvH2v-G-A-R51, H, F, Cl, Br, I, CN, T(CH2)h(ClF2l+1), SOlR31, CONR32R33, COR34, SO2NR45R46, CF2R64, CFR65R66, CFÄ(CF2)qCF3ÜR65, CÄ(CF2)pCF3Ü=CR65R66, OR67, NR67R68, 1-8C alkyl, 2-8C alkenyl or (CH2)mR14; Phe = phenyl, (substd. by one R8 gp. and opt. substd. by 1 or 2 of R'); R' = F, Cl, CF3, Me, OH, OMe or NR15R16; Het = 1-9 heteroaryl, bonded by C or N (opt. substd. by 1-3 or R'); R15, R16, R56 = H or Me; Y = bond, CH2, O, S or NR9; R8 = SOa(NR98)bNR99R10 or SOa(NR98)bNR95-C(=NR94)NR92R93; a = 1 or 2; b = 0 or 1; a+b = 2; R10, R98, R99 = H, Me, benzyl, 2-8C alkyl (opt. substd. by NR11R12 or NR13-A'-NR37R38) or 0-8 alkyl (substd. by CR39R40-CR41R42A"NR43R44); or R99+R10 = 4-6C n-alkylene (opt. with one CH2 replace by O, S, NH, NMe or N-benzyl); A' = 2-8C alkylene; A" = 0-8C alkylene; R11-R13, R23, R24 R37, R38, R43, R44 = H, 1-8C alkyl or benzyl; R39-R42 = H, 4-8C alkyl, phenyl, 1-3C alkyl (opt. substd. by phenyl) (where the phenyl gps. are opt. substd. by F, Cl, CF3, Me or OMe); Py = pyrrol-(1,2 or 3)-yl (opt. substd. by 1-4 of F, Cl, Br, I, CN, 2-8C alkanoyl, 2-8C alkoxycarbonyl, CHO, COOH, CF3, Me or OMe); m, h, l, d, r, p, q = 0-2; s is not defined; R14 = 3-8C cycloalkyl or phenyl(opt. substd. by 1-3 of F, Cl, CF3, Me, OMe and NR15R16); Q = bond, O, S or NR18; Phe' = phenyl (substd. by (CH2)kCHR17COR20 and opt. substd. by one or 2 R'); R17 = OR21 or NR21R22; R20 = OR23 or NR23R24; R22 = H, 1-8C alkyl, 1-8C alkanoyl, 1-8C alkoxycarbonyl, benzyl or benzoyloxycarbonyl; R21 = as R22 or trityl; k, z = 1-4; R25 = 0-2C alkyl substd. by Het or its N-oxide; R26, R27 = H as for R25, H or 1-4C alkyl; T = as Q but not butylimino; i = 2-6; R31 = 1-8C alkyl, 3-6C alkenyl, (CH2)nR48 or CF3; R32,R34,R45 = H or as for R31; n, v = 0-4; R47 R69-R71 = H or 1-3C alkyl; R48 = 3-7C cycloalkyl or phenyl (opt. substd. by 1-3 or F, Cl, CF3, Me, OMe and NR49R50); R33, R46 = H or 1-4C alkyl; or R32+R33, R45+R46 = (CH2)5 or (CH2)6 (both opt. with one CH2 replaced by O, S, NH, NMe or N-benzyl); R51 = basic, protonisable residue ( i.e. NR52R53, C(=NR54)NR52R51 or NR55-C(=NR54)NR52R53) or a basic 1-9C heteroaryl ring; R52-R55 = H or 1-4C alkyl or R52+R53 = C4H8 or A1; or R53+R54, R54+R55 or R52+R55 = C2H4 or A2; A1 =C5H10, C6H12 or C7H14 (all with one C atom opt. replaced by O, SOd or NR56); A2 = C3H6, C4H8 or C5H10 (all with one C opt. replaced by O, SOd or NR56); A = CeH2e (opt. with one C replaced by O, CO, CH(OR57), SOr, NR57,CON(R57), SO2N(R57), NH-CO-NR57 or SO2NHCONR57); e = 0-10; G = phenylene (opt. substd. by one or two of Me, OMe, F, Cl, Br, I, CF3, SOsMe or SOsNR61R62; w = 0 or 1; E = O, CO, CH(OR63), S, SO, SO2, NH, or NMe; R64 = 1-4C alkyl or 3-7C cycloalkyl; R67, R68 = H or 1-6C alkyl; or R67+R68 = (CH2)4-7, opt. with one CH2 replaced by O, S, SO2, NH, NMe or N-benzyl; R4, R5 = H, 1-4C alkyl, F, Cl, OR69, NR70R71 or CzF2z+1; X = O or NR72; R6, R7, R9, R18, R49, R50, R61, R62, R65, R66, R72, R92-R95 = H or 1-4C alkyl; provided that R1-R7 and R72 are not all H.

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