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    2.
    发明专利
    未知

    公开(公告)号：DE19630082A1

    公开(公告)日：1998-01-29

    申请号：DE19630082

    申请日：1996-07-26

    Applicant: BASF AG

    Inventor： MACK HELMUT DR ,  PFEIFFER THOMAS DR ,  SEITZ WERNER DR ,  ZIERKE THOMAS DR ,  BALKENHOHL FRIEDHELM DR ,  LANGE UDO DR

    IPC: C12P17/04 ,  C07D207/22 ,  C07D401/12 ,  C07D401/04 ,  C07B57/00

    Abstract: A process is disclosed for preparing 3-pyrroline-2-carboxylic acid derivatives of formula (I), in which R stands for H, C1-C6-alkyl, benzyl, benzyl substituted at the phenyl radical, allyloxycarbonyl, C1-C6-alkyloxycarbonyl, benzyloxycarbonyl, in which the benzyl radical can be substituted by OCH3 radicals, or for C1-C4-alkylcarbonyl; or R stands for an amino acid radical which can be alkylated or acylated at the nitrogen and is linked by the C-terminal; and R stands for OH, C1-C4-alkyloxy, benzyloxy or an N R group, in which R and R represent independently from each other H, C1-C4-alkyl, benzyl, phenyl or pyridyl, in which the aromatic compounds in R and R can be substituted by up to three identical or different substituents selected from the group composed of methyl, methoxy, hydroxy, cyano or halogen. According to this process, the sulphonic acid radical is eliminated by means of a base from a compound having the formula (II), in which R and R have the above meanings and R stands for C1-C6-alkyl, benzyl, trifluoromethyl, naphthyl or phenyl optionally substituted by radicals from the group composed of methyl, nitro and halogen.

    New orally active thrombin inhibiting peptide cpds.
    8.
    发明专利
    New orally active thrombin inhibiting peptide cpds. 未知

    公开(公告)号：DE19504504A1

    公开(公告)日：1996-08-14

    申请号：DE19504504

    申请日：1995-02-10

    Applicant: BASF AG

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

    IPC: A61K38/00 ,  C07K5/06 ,  C07K5/065 ,  C07K5/072 ,  C07K5/087 ,  A61K38/57 ,  C12N9/74 ,  C12N9/99

    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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