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    53.
    发明专利
    未知

    公开(公告)号：DE4135265A1

    公开(公告)日：1993-04-29

    申请号：DE4135265

    申请日：1991-10-25

    Applicant: BASF AG

    Inventor： KAST JUERGEN DR ,  ZIERKE THOMAS DR ,  BRATZ MATTHIAS DR ,  MISSLITZ ULF DR ,  MEYER NORBERT DR ,  LANDES ANDREAS DR ,  RADEMACHER WILHELM DR ,  WESTPHALEN KARL-OTTO DR ,  WALTER HELMUT DR

    IPC: A01N37/42 ,  A01N37/48 ,  A01N37/50 ,  A01N39/00 ,  C07C67/313 ,  C07C69/757 ,  C07C249/02 ,  C07C249/08 ,  C07C251/18 ,  C07C251/42 ,  C07C251/52 ,  C07C251/54 ,  C07C255/56 ,  C07C255/61 ,  C07C255/62 ,  C07C317/28 ,  C07D295/18 ,  C07D521/00

    Abstract: Cyclohexenone derivates have the formula (I), in which R stands for alkyl, alkenyl, alkinyl, cycloalkyl, aloxyalkyl, alkylthioalkyl, possibly substituted phenyl, possibly substituted benzyl, possibly substituted 5-/6-membered heteroaryl; W stands for 0, =N-OR or =N-R ; R stands for possibly substituted alkyl, alkenyl or alkinyl residue, possibly substituted 3- to 6-membered alkyl chain or 4- to 6-membered alkenyl or alkinyl chain, a chain link in each of the chains being substituted by -0-, -S-, -S0-, -S02- or -N(R )-; R stands for H, alkyl, alkenyl, alkinyl, alkylcarbonyl, benzoyl; R stands for H, alkyl hydroxyakyl, alkoxyalkyl or alkylthioalkyl, possibly substituted phenyl, possibly substituted benzyl; X, Y stand for -OR or -NR R ; R stands for H, alkyl, akenyl, alkinyl, alkoxyalkyl, alkylthioalkyl; R stands for H, alkyl, alkenyl, alkinyl, hydroxyalkyl, alkoxyalkyl, alkylthioalkyl and R stands for H, alkyl, alkenyl, alkinyl, hydroxyalkyl, alkoxyalkyl, alkylthioalkyl, alkylcarbonyl, possibly substituted benzoyl or R -R form together with the shared N atom a 5-/6-membered heterocycle that may contain -O-, -S- or -N(R )- as ring element; R stands for H, alkyl, alkenyl, alkinyl, alkylcarbonyl, benzoyl. Also disclosed are the agriculturally useful salts and esters of C1-C10-carboxylic acids and anorganic acids of the compounds having the formula (I). These cyclohexenone derivates (I) are useful as herbicides and plant growth regulators.

    59.
    发明专利
    未知

    公开(公告)号：DE19527574A1

    公开(公告)日：1997-01-30

    申请号：DE19527574

    申请日：1995-07-28

    Applicant: BASF AG

    Inventor： BUSCHMANN ERNST DR ,  ZIERKE THOMAS DR

    IPC: C07C231/02 ,  C07C237/02 ,  C07K1/06 ,  C07K1/08 ,  C07K7/06

    Abstract: The description relates to a process for producing alpha -(N,N dialkyl)-amino carboxylic acid amides of formula (I) in which the constituents have the meanings given, in which the corresponding free acids are reacted with primary or secondary amines in the presence of anhydrides of an alkane phosphonic acid.

    New orally active thrombin inhibiting peptide cpds.
    60.
    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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