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    1.
    发明专利
    未知

    公开(公告)号：DE59605782D1

    公开(公告)日：2000-09-28

    申请号：DE59605782

    申请日：1996-05-13

    Applicant: HOECHST AG

    Inventor： KLEEMANN DR ,  BRENDEL DR ,  SCHWARK DR ,  WEICHERT DR ,  LANG DR ,  ALBUS DR ,  SCHOLZ 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: 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.

    3.
    发明专利
    未知

    公开(公告)号：DE59608533D1

    公开(公告)日：2002-02-07

    申请号：DE59608533

    申请日：1996-07-15

    Applicant: HOECHST AG

    Inventor： WEICHERT DR ,  BRENDEL DR ,  KLEEMANN DR ,  LANG DR ,  SCHWARK DR ,  SCHOLZ DR ,  ALBUS DR

    IPC: A61K49/00 ,  A01N1/02 ,  A61K31/155 ,  A61K31/165 ,  A61K31/18 ,  A61P9/00 ,  A61P9/06 ,  A61P9/08 ,  A61P9/10 ,  A61P41/00 ,  C07C303/40 ,  C07C311/16 ,  C07C315/04 ,  C07C317/44

    Abstract: Benzoyl-guanidine derivs. of formula (I) and their salts are new: R1 = R4-SOm, R5R6N-SO2-, -Op-(CH2)q-(CF2)r-CF3, -SR10, -OR10 or -CR10R11R12; m = 1-2; R4, R5 = 1-8C alkyl, 3-6C alkenyl, CF3 or -CnH2n-R7; n = 0-4; R6 = H or 1-4C alkyl; R7 = 3-8C cycloalkyl or Ph (opt. substd. with 1-3 substits. from F, Cl, CF3, Me, OMe and NR8R9; R8, R9 = H or 1-4C alkyl; R5 = H; or R5 + R6 = 4-5C methylene group (with opt. replacement of a CH2 by O, S, NH, NMe or N-benzyl; ; p = 0-1; q = 0-2; r = 0-3;R10, R11, R12 = H, 1-8C alkyl, CsH2s-(3-8C cycloalkyl) or an aromatic gp. chosen from pyridyl, pyrrolyl, quinolyl, isoquinolyl, imidazolyl or Ph (in which the aromatic system may be opt. 1-3 times substd. by F, Cl, CF3, Me, OMe, OH, NH2, NHMe or N(Me)2; s = 0-2; R2 = -(CH2)u-(CF2)t-CF3; t = 0-3; u = 0-1; R3 = H or as for R1.

    5.
    发明专利
    未知

    公开(公告)号：DE59705019D1

    公开(公告)日：2001-11-29

    申请号：DE59705019

    申请日：1997-02-19

    Applicant: HOECHST AG

    Inventor： ALBUS DR ,  BRENDEL DR ,  KLEEMANN DR ,  LANG DR ,  SCHOLZ DR ,  SCHWARK DR ,  WEICHERT 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.

    6.
    发明专利
    未知

    公开(公告)号：DE59604165D1

    公开(公告)日：2000-02-17

    申请号：DE59604165

    申请日：1996-10-22

    Applicant: HOECHST AG

    Inventor： KLEEMANN DR ,  BRENDEL DR ,  SCHWARK DR ,  WEICHERT DR ,  LANG DR ,  ALBUS DR ,  SCHOLZ DR

    IPC: A61K31/165 ,  A61K31/18 ,  A61P1/16 ,  A61P3/08 ,  A61P9/04 ,  A61P9/08 ,  A61P9/10 ,  A61P11/00 ,  A61P13/02 ,  A61P15/00 ,  A61P35/00 ,  A61P41/00 ,  A61P43/00 ,  C07C279/18 ,  C07C313/02 ,  C07C313/06 ,  C07C381/10

    Abstract: Sulphonimidamides of formula R1N=S(O)(R2)N(R4)(R3) (I) and their salts are new: at least one of R1-R3 = a benzoylguanidine group of formula (a) optionally substituted in the phenyl ring by 1-4 of 1-8C alkyl, 2-8C alkenyl, (CH2)mR14, halo, CN, CF3, R22SO2, R23R24NCO, R25CO, R26R27NSO2, OR35, SR35 or NR35R36; m = 0-2; R14 = 3-8C cycloalkyl, phenyl optionally substituted by 1-3 of F, Cl, CF3, Me, OMe or NR15R16; R15, R16 = H or Me; R22, R23, R25, R26 = 1-8C alkyl, 2-8C alkenyl, (CH2)nR29 or CF3; or R23+R24, R26+R27 = 5-6 methylene groups with optionally one CH2 replaced by O, S, NH, NMe or N-benzyl; or R23, R25, R26 = H; n = 0-4; R29 = 3-7C cycloalkyl, phenyl optionally substituted by 1-3 of F, Cl, CF3, Me, OMe or NR30R31; R30, R31 = H or 1-4C alkyl; R24, R27 = H or 1-4C alkyl; R35, R36 = H or 1-6C alkyl; or R35+R36 = 4-7 methylene groups with optionally one CH2 replaced by O, S, NH, NMe or N-benzyl; or R35 = phenyl optionally substituted by 1-3 of F, Cl, CF3, Me, OMe, SO2R5, SO2NR6R7 or NR32R33; R5 = 1-6C alkyl; R6, R7 = H or 1-4C alkyl; R32, R33 = H or 1-4C alkyl; or R35 = 1-9C heteroaryl optionally substituted by 1-3 of F, Cl, CF3, CH3, OMe, OH, NH2, NHMe or N(Me)2; the remaining R1-R3 = 1-8C alkyl or (CH2)pR10; or the remaining R1, R2 = H; p = 0-4; R10 = phenyl optionally substituted by 1-3 of F, Cl, CF3, Me, OMe, SO2NR17R8 or SO2R9; R17, R8 = H or 1-4C alkyl; R9 = 1-4C alkyl; and R4 = H or 1-4C alkyl.

    7.
    发明专利
    未知

    公开(公告)号：DE59703851D1

    公开(公告)日：2001-07-26

    申请号：DE59703851

    申请日：1997-08-18

    Applicant: HOECHST AG

    Inventor： SCHWARK DR ,  BRENDEL DR ,  KLEEMANN HEINZ-WERNER ,  LANG DR ,  WEICHERT DR ,  JANSEN DR ,  SCHOLZ 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.

    8.
    发明专利
    未知

    公开(公告)号：DE59703746D1

    公开(公告)日：2001-07-19

    申请号：DE59703746

    申请日：1997-02-03

    Applicant: HOECHST AG

    Inventor： SCHWARK DR ,  BRENDEL DR ,  KLEEMANN DR ,  LANG DR ,  WEICHERT DR ,  ALBUS DR ,  SCHOLZ 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

    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.

    10.
    发明专利
    未知

    公开(公告)号：DE59703220D1

    公开(公告)日：2001-05-03

    申请号：DE59703220

    申请日：1997-05-16

    Applicant: HOECHST AG

    Inventor： BRENDEL DR ,  KLEEMANN DR ,  ENGLERT DR ,  LANG DR ,  ALBUS DR ,  LAL DR ,  GHATE VASANTRAO ANIL

    IPC: C07D295/14 ,  A01N1/02 ,  A01N47/44 ,  A61K31/155 ,  A61K31/165 ,  A61K31/445 ,  A61P3/06 ,  A61P9/00 ,  A61P9/06 ,  A61P9/10 ,  C07C271/22 ,  C07C279/20 ,  C07C279/22 ,  C07C303/40 ,  C07C311/19 ,  C07C315/04 ,  C07C317/50 ,  C07C319/20 ,  C07C323/62

    Abstract: 1-Naphthoyl-guanidines (I) and their salts are new: R2-R8 = H; F; Cl; Br; I; CN; NO2; CF3; C2F5; or XaYbZ; X = O; S; or NR10, CR11R12, CO, CONR10, COO, SO; SO2, SO2NR10, OCO, NR10CO or NR10SO2 attached to the ring via the left hand atom; R10-R12 = H; 1-6C alkyl; 1-4C perfluoroalkyl; or 3-7C cycloalkyl; Y = 1-8C alkylene with 1 CH2 optionally replaced by O, S, NR13 or o-, m- or p-phenylene; R13 = H; 1-6C alkyl; 1-4C perfluoroalkyl; or 3-6C cycloalkyl; Z = H; 1-7C alkyl; 3-7C cycloalkyl; COR15; SO2R15; NR16R17; or is Ph or a C- or N-linked N-containing 1-9C heterocycle (each optionally mono-, di- or trisubstituted by F, Cl, Br, CF3, Me, OMe or NR21R22); a, b = 0 or 1; R15 = N=C(NH2)2; NR18R19; N(CH2)cNR18R19; or OR20; c = 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 NQ; Q = H; Me; benzyl; or p-Cl-Ph; R20 = H; 1-6C alkyl; 1-4C perfluoroalkyl; or 3-7C cycloalkyl; R21, R22 = H; 1-4C alkyl; or 1-4C perfluoroalkyl; provided that when R4 = alkoxy, at least one of R2, R3 and R5-R8 is not H.

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