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    IMIDAZOLE DERIVATIVES
    5.
    发明专利
    IMIDAZOLE DERIVATIVES 未知

    公开(公告)号：AU613349B2

    公开(公告)日：1991-08-01

    申请号：AU1353288

    申请日：1988-03-21

    Applicant: HOFFMANN LA ROCHE

    Inventor： KLOTZER WILHELM ,  MONTAVON MARC ,  MUSSNER RENATE ,  SINGEWALD NICOLAS

    IPC: C07D233/56 ,  A61K31/415 ,  A61K31/4164 ,  A61K31/417 ,  A61P3/00 ,  A61P29/00 ,  C07D233/61 ,  C07D233/64 ,  C07D233/80 ,  C07D233/84 ,  C07D233/88 ,  C07D521/00

    Abstract: Imidazole derivatives of the formula I wherein R1 and R2 each is lower alkyl, X is a residue of the formula R3 is hydrogen and R4 is hydrogen or lower alkyl or R3 and R4 taken together are an additional carbon-nitrogen bond; R5 is hydrogen or lower alkyl; R6 is hydrogen, lower alkyl, lower alkylthio or a residue of the formula -NR7R8; and R7 and R8 each is lower alkyl or taken together with the nitrogen atom are a 5- or 6-membered saturated heterocycle; and pharmaceutically acceptable acid addition salts thereof are described. The compounds of formula I possess valuable pharmacodynamic properties, especially inflammation-inhibiting and edema-inhibiting properties, so that they can be used for the control or prevention of illnesses, especially for the control or prevention of inflammations and edemas.

    6.
    发明专利
    未知

    公开(公告)号：FI79847B

    公开(公告)日：1989-11-30

    申请号：FI834321

    申请日：1983-11-24

    Applicant: HOFFMANN LA ROCHE

    Inventor： BROMBACHER URS ,  LINK HELMUT ,  MONTAVON MARC

    IPC: A61K31/00 ,  A61K31/435 ,  A61P33/10 ,  C07D219/06 ,  C07D219/10 ,  C07D417/12 ,  C07D417/14

    Abstract: For the Contracting States BE CH DE FR GB IT LI LU NL SE 1. Acridanone derivatives of the general formula see diagramm : EP0110298,P20,F1 wherein the dotted line signifies an optional bond, R**1 signifies hydrogen, halogen or nitro, R**2 signifies hydrogen or lower alkyl, one of the symbols R**3 and R**4 signifies hydrogen or lower alkyl and the other together with R signifies an additional bond, A signifies lower alkylene, R**5 signifies a 5-membered, nitrogen-containig, optionally lower alkyl-substituted aromatic heterocycle, amino or a group see diagramm : EP0110298,P20,F2 or see diagramm : EP0110298,P20,F3 the symbol see diagramm : EP0110298,P20,F4 signifies a 5- or 6-membered, optionally lower-alkyl substituted saturated heterocycle which can contain as a ring member an oxygen or sulphur atom or the group >NH ou >N(B)n -A**1-R**6, B signifies the group -CO-, -COO- or -SO2 -, n signifies the number 0 or 1, A**1 signifies lower alkylene, R**6 signifies hydrogen, amino, lower alkylamino or di(lower alkyl)amino and R**7 signifies hydrogen or lower alkyl, and the residues denoted as lower contain 1 to 7 carbon atoms, and pharmaceutically acceptable acid addition salts thereof. For the Contracting State AT 1. A process for the manufacture of acridanone derivatives of the general formula see diagramm : EP0110298,P22,F1 wherein the dotted line signifies an optional bond, R**1 signifies hydrogen, halogen or nitro, R**2 signifies hydrogen or lower alkyl, one of the symbols R**3 and R**4 signifies hydrogen or lower alkyl and the other together with R signifies an additional bond, A signifies lower alkylene, R**5 signifies a 5-membered, nitrogen-containing, optionally lower alkyl-substituted aromatic heterocycle, amino or a group see diagramm : EP0110298,P23,F2 or see diagramm : EP0110298,P23,F3 the symbol see diagramm : EP0110298,P23,F4 signifies a 5- or 6-membered, optionally lower-alkyl substituted saturated heterocycle which can contain as a ring member an oxygen or sulphur atom or the group >NH ou >N(B)n -A**1-R**6, B signifies the group -CO-, -COO- or -SO2 -, n signifies the number 0 or 1, A**1 signifies lower alkylene, R**6 signifies hydrogen, amino, lower alkylamino or di(lower alkyl)amino and R**7 signifies hydrogen or lower alkyl, and the residues denoted as lower contains 1 to 7 carbon atoms, and pharmaceutically acceptable acid addition salts thereof, characterized by a) cyclizing a compound of the general formula see diagramm : EP0110298,P23,F5 wherein one of the symbols R**31 and R**41 signifies hydrogen or lower alkyl and the other signifies hydrogen, R**42 signifies hydrogen or lower alkyl, R**51 signifies a residue R**5, but does not contain a primary or secondary basic amino group, and X' signifies a leaving group, and R**1, R**2 and R**5 have the above significance, b) reacting a compound of the general formula see diagramm : EP0110298,P23,F6 wherein A, R**1, R**42 and R**51 have the above significance, with a compound of the general formula see diagramm : EP0110298,P23,F7 wherein X" signifies a leaving group and the dotted line and R**2 have the above significance, or c) reacting a compound of the general formula see diagramm : EP0110298,P23,F8 wherein Y(anion) signifies an anion and X signifies a leaving group, and A, R**1 and R**51 have the above significance, with a compound of the general formula see diagramm : EP0110298,P23,F9 wherein the dotted line, R, R**2, R**3 and R**4 have the above significance, or d) cleaving off the N-protecting group in a compound of the general formula see diagramm : EP0110298,P24,F10 wherein R**8 signifies a residue R**5 which contains a primary or secondary basic amino group blocked by a N-protecting group and the dotted line, R, R**1, R**2, R**3 and R**4 have the above significance, and e) if desired, converting a compound of formula I obtained into a pharmaceutically acceptable acid addition salt.

    ACRIDANONE DERIVATIVES
    7.
    发明专利
    ACRIDANONE DERIVATIVES 未知

    公开(公告)号：CA1258854A

    公开(公告)日：1989-08-29

    申请号：CA440203

    申请日：1983-11-01

    Applicant: HOFFMANN LA ROCHE

    Inventor： BROMBACHER URS ,  LINK HELMUT ,  MONTAVON MARC

    IPC: A61K31/00 ,  A61K31/435 ,  A61P33/10 ,  C07D219/06 ,  C07D219/10 ,  C07D417/12 ,  C07D417/14 ,  A61K31/47

    Abstract: The present invention is concerned with acridanone derivatives of the general formula I wherein the dotted line signifies an optional bond, R1 signifies hydrogen, halogen or nitro, R2 signifies hydrogen or lower alkyl, one of the substituents R3 and R4 signifies hydrogen or lower alkyl and the other together with R signifies an additional bond, A signifies lower alkylene, R5 signifies a 5-membered nitrogen-containing, optionally lower alkyl-substituted aromatic heterocycle, amino or the group the symbol ? signifies a 5- or 6-membered, optionally lower alkyl-substituted saturated - ii heterocycle which can contain as a ring member an oxygen or sulphur atom or the group ?NH or ?N(B)n-A1-R6, B signifies the group -CO-, -COO-or -SO2-, n signifies the number 0 or 1, A1 signifies lower alkylene, R6 signifies hydrogen, amino, lower alkylamino or di(lower alkyl)amino and R7 signifies hydrogen or lower alkyl, and pharmaceutically acceptable acid addition salts thereof, their manufacture and pharmaceutical preparations based thereon. These novel substances possess valuable pharmacological properties and can be used in the control or prevention of illnesses. In particular, they display valuable schistosomicidal activities and can accordingly be used in the control or prevention of schistosomiasis.

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