中科微点-全球专利检索

  1. Login
  2. Sign Up

Search Results

13 records (took 0.02 seconds)

    New orally active thrombin inhibiting peptide cpds.
    11.
    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).

Patent Agency Ranking