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    1.
    发明专利
    未知

    公开(公告)号：DE19720803A1

    公开(公告)日：1998-11-19

    申请号：DE19720803

    申请日：1997-05-16

    Applicant: BASF AG

    Inventor： VIERGUTZ WOLFGANG DR ,  KOSER STEFAN DR

    IPC: C07D209/48 ,  C07D221/14

    Abstract: The invention relates to a method for producing bisimides of formula (I), wherein R , R , R and R have the meanings cited in the description. According to the inventive method, the corresponding dicarboxylic acid anhydride of formulas (II): R -CO-O-CO-R and (III): R -CO-O-CO-R are reacted with an amine of formula H2N-R-NH2 in the presence of a tertiary amine.

    7.
    发明专利
    未知

    公开(公告)号：DE19706337A1

    公开(公告)日：1998-08-20

    申请号：DE19706337

    申请日：1997-02-19

    Applicant: BASF AG

    Inventor： BALKENHOHL FRIEDHELM DR ,  KOSER STEFAN DR ,  HOLMAN NICHOLAS JOHN DR

    IPC: C07D487/04 ,  C12P17/18 ,  C12P41/00 ,  C07B53/00 ,  C07B41/12

    Abstract: The invention relates to a method for producing enantiomer-free esters of formula (I) (Ia or Ib), where the substituents represent the following: R is a hydrogen or a substituted or unsubstituted C1-C6-alkyl-, C1-C6-alkoxy-, or C1-C6-alkanoyl; R and R independently of each other are hydrogen or a substituted or unsubstituted C1-C6-alkyl-, C1-C6-alkoxy-, or C1-C6-alkanoyl-, C1-C6-alkylthio-, C1-C6-alkyl sulfinyl or C1-C6-alkyl sulfonyl-; R is not equal to R and independently of each other they are either hydrogen or an substituted or unsubstituted C1-C6-alkyl-, or together with the hydrogen atoms, to which they are bound, form a substituted or unsubstituted C3-C6-cyclo alkylidene; and R is a substituted or unsubstituted aryl-, C1-C20-alkyl-, C3-C20-alkenyl-, C3-C20-alkynyl-, C1-C20-alkoxy-C1-C20-alkyl. The method is characterized in that racemic compounds of the formula (II), in which the substituents R to R have the meanings given above, are reacted with a lipase or esterase in the presence of vinyl esters of formula (III), where R has the meaning given above and R represents hydrogen or methyl, to form compounds of formula (I).

    New orally active thrombin inhibiting peptide cpds.
    9.
    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).

    10.
    发明专利
    未知

    公开(公告)号：DE19706336A1

    公开(公告)日：1998-08-20

    申请号：DE19706336

    申请日：1997-02-19

    Applicant: BASF AG

    Inventor： BALKENHOHL FRIEDHELM DR ,  KOSER STEFAN DR ,  HOLMANN NICHOLAS JOHN DR

    IPC: C07D487/04 ,  C12N9/20 ,  C12P17/18 ,  C12P41/00

    Abstract: The invention relates to a method for producing enantiomer-free alcohols of formula (I), where the substituents represent the following: R is a hydrogen or a substituted or unsubstituted C1-C6-alkyl-, C1-C6-alkoxy-, or C1-C6-alkanoyl-; R and R independently of each other represent hydrogen or a substituted or unsubstituted C1-C6-alkyl-, C1-C6-alkoxy-, C1-C6-alkanoyl, C1-C6-alkylthio-, C1-C6-alkyl sulfinyl or C1-C6-alkyl sulfonyl-; and R is not equal R and independently of each other they represent either hydrogen or a substituted or unsubstituted C1-C6-alkyl-, or together with the hydrogen atoms to which they are bound form a substituted or unsubstituted C3-C6-cyclo alkylidene. The method is characterized in that racemic compounds of the formula (II), in which the substituents R to R have the meanings given above and R is a substituted or unsubstituted aryl-, C1-C20-alkyl-, C3-C20-alkenyl-, C3-C20-alkynyl-, are reacted with a lipase or esterase in the presence of an alcohol of the formula R OH (III), where R is a substituted or unsubstituted C1-C10-alkyl-.

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