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    New orally active thrombin inhibiting peptide cpds.
    18.
    发明专利
    New orally active thrombin inhibiting peptide cpds. 未知

    公开(公告)号：DE19506610A1

    公开(公告)日：1996-08-29

    申请号：DE19506610

    申请日：1995-02-24

    Applicant: BASF AG

    Inventor： BOEHM HANS-JOACHIM DR ,  KOSER STEFAN DR ,  MACK HELMUT DR ,  PFEIFFER THOMAS DR ,  SEITZ WERNER DR ,  HOEFFKEN HANS WOLFGANG DR ,  HORNBERGER WILFRIED DR ,  ZIERKE THOMAS DR

    IPC: A61K38/00 ,  C07K5/065 ,  C07K5/06 ,  A61K38/05

    Abstract: Novel thrombin inhibitors consist of N-terminal sulphonylated peptidic p-amidino-benzamide cpds. of formula (I): R1-SO2-A-B-NH-D-C(=NH)(NH2) (I) and their stereoisomers and acid addn. salts. The amidino function may be in mono- or bis-protected form. R1 = OH, 1-20C alkyl, 1-3C fluoroalkyl, 3-8C cycloalkyl, aryl(1-10C) alkyl, aryl, heteroaryl, R2OOC-(CH2)n- or R2R3N; R2, R3 = H, 1-10C alkyl, aryl or aryl-(1-10C)alkyl or together form 2-7C alkylene which opt. includes a fused aryl or heteroaryl residual or O, S, NH or substd. N as heteroatom; n = 1-4; A = -NH-CR4R5-CO-, R4 = H, 1-8C alkyl, 3-7C cycloalkyl, aryl or aryl-(1-3C)alkyl; R = H, 1-8C alkyl, 3-7C cycloalkyl or (3-7C)cycloalkyl-CH2 (where one CH2 is opt. replaced by O, S or NR6), bicycloalkyl, bicyclo-alkylmethyl, adamantyl, adamantylmethyl, trimethylsilyl-(1-4C)alkyl, aryl, aryl-(1-3C)alkyl, heteroaryl, heteroaryl-(1-3C)alkyl or (if R4 = H) 1-8C alkyl monosubstd. by SR6, OR6 or CONR7R8; or R4+R5 = 2-6C alkylene (opt. fused with aryl); R6 = H, 1-8C alkyl or aryl-(1-3C) alkyl; R7, R8 = H, 1-4C alkyl or 3-7C cycloalkyl or together form 3-6C alkylene; B = cyclic alpha -aminoacid residue of formula (a); m = 2-4; one H in the ring of (a) is opt. replaced by OH or 1-3C alkyl if m = 3 or 4, one ring CH2 in (a) is opt. replaced by O, S, NH or N-(1-4C alkyl) and/or two vicinal H are replaced by a double bond, a fused aromatic ring or a 4-6C methylene chain; D = benzyl or heterocyclic analogue residue of formula (D1)-(D3), R9 = F, Cl, Br, NO2, R15O, R15OOC-, R15OCH2, R15NHCO, R15NH, R15CONH or R15OOCCH2O2; R15 = H, 1-6C alkyl, benzyl or phenyl; R10, R11 = H, 1-4C alkyl or OR15; or R9 + R10 or R11 = fused benzene ring or 3-5C alkylene (with 1 or 2 C opt. replaced by O); R12 = H or 1-4C alkyl; R13 = 1-4C alkyl, phenyl-(1-4C)alkyl, R15CO, CF2CO, C2F5CO, R15OCH2, R15OOC, R15OCH2CO, R15OOCCO or R15NHCOCO; R14 = H, 1-4C alkyl, F, Cl, Br, NO2, R15O, R15OOC, R15OCH2, R15CO, R15CONH, R15NHCO or R15OOCOCH2O; W, X, Y, Z = CH or N, provided that \- 1 is N, the ring in (D3) is opt. substd. by 1 or 2 of 1-4C alkyl, OH, 1-4C alkoxy, CF3, F, Cl, Br, 1-4C alkylthio and O(CH2)mCOOR6, m = 1-4. Also claimed are: (1) intermediates of formulae (VII)-(X) (where in (VII) the amidine function is opt. in mono- or bis-protected form), H2N-D-CN (VII), H2N-D-C(=NH)(NH2) (VIII), R1SO2-A-B-NH-D-CN (IX) and R1SO2-A-B-NH-D-C(=NH)(NHOH) (X), and (2) cpds. contg. the structural fragment of formula (XI): -C(=O)-NH-D-C(NH2)(=NH) (XI).

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