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    Aminoquinoline derivatives
    5.
    发明专利
    Aminoquinoline derivatives 未知

    公开(公告)号：SG47958A1

    公开(公告)日：1998-04-17

    申请号：SG1996005663

    申请日：1994-10-15

    Applicant: HOFFMANN LA ROCHE

    Inventor： JAOUET CATHERINE ,  JOLIDON SYNESE ,  HOFHEINZ WERNER

    IPC: A61K31/00 ,  A61K31/47 ,  A61K31/4706 ,  C07D215/46 ,  A61P31/00 ,  A61P33/02 ,  C07D215/42 ,  C07D401/12

    Abstract: The invention relates to aminoquinoline derivatives of the general formula in which the symbols R to R are hydrogen or one or two thereof are alkyl and the others are hydrogen, R and R are alkyl, alkenyl, aralkyl or, together with N, pyrrolidine or piperidine, also substituted by alkyl, octahydroindole or 3-azabicyclo[3.2.2]nonane and n = 0 or 1 or in which the symbols R and R are tri- or tetramethylene, all the other substituents up to R are hydrogen, n = 0 and R and R have the above meanings, or in which the symbols R and R are methylene or dimethylene and n = 1, R and R are di- or trimethylene and n = 0, R and R are di- or trimethylene and n = 1, R and R are tri- or tetramethylene and n = 0, R and R are tri- or tetramethylene and n = 1, R and R are di- or trimethylene and n = 1, all the other substituents are hydrogen apart from R , which is alkyl, alkenyl or aralkyl, or in which the symbols R and R are tri- or tetramethylene and n = 1, all the other substituents up to R are hydrogen and R and R are alkyl, alkenyl, aralkyl or, together with N, pyrrolidine or piperidine, also substituted by alkyl, R is hydrogen or halogen and R is halogen or trifluoromethyl, and pharmaceutically acceptable salts of basic compounds of the general formula I for producing pharmaceuticals for controlling both chloroquine-resistant and chloroquine-sensitive malaria pathogens.

    Diamines
    7.
    发明专利
    Diamines 未知

    公开(公告)号：ZA954795B

    公开(公告)日：1996-01-03

    申请号：ZA954795

    申请日：1995-06-09

    Applicant: HOFFMANN LA ROCHE

    Inventor： HOFHEINZ WERNER ,  MASCIADRI RAFFAELLO

    IPC: C07D215/46 ,  C07D ,  A61K

    Abstract: Disclosed are (S,S)-N,N'-bis(quinolin-4-yl)-1,2-diamine derivatives of general formula (I) wherein R1 signifies hydrogen or halogen, R2 signifies halogen or trifluoromethyl and n signifies 1 to 5, as well as their pharmaceutically acceptable salts. These products are useful as agents for the prevention and treatment of malaria especially where the pathogens are resistant to chloroquine.

    Aminoquinoline derivatives
    9.
    发明专利
    Aminoquinoline derivatives 未知

    公开(公告)号：AU7741994A

    公开(公告)日：1995-05-18

    申请号：AU7741994

    申请日：1994-10-24

    Applicant: HOFFMANN LA ROCHE

    Inventor： HOFHEINZ WERNER ,  JAQUET CATHERINE ,  JOLIDON SYNESE

    IPC: C07D215/46 ,  A61K31/00 ,  A61K31/47 ,  A61K31/4706 ,  A61P31/00 ,  A61P33/02 ,  C07D215/42 ,  C07D401/12 ,  C07D401/06

    Abstract: The invention relates to aminoquinoline derivatives of the general formula in which the symbols R to R are hydrogen or one or two thereof are alkyl and the others are hydrogen, R and R are alkyl, alkenyl, aralkyl or, together with N, pyrrolidine or piperidine, also substituted by alkyl, octahydroindole or 3-azabicyclo[3.2.2]nonane and n = 0 or 1 or in which the symbols R and R are tri- or tetramethylene, all the other substituents up to R are hydrogen, n = 0 and R and R have the above meanings, or in which the symbols R and R are methylene or dimethylene and n = 1, R and R are di- or trimethylene and n = 0, R and R are di- or trimethylene and n = 1, R and R are tri- or tetramethylene and n = 0, R and R are tri- or tetramethylene and n = 1, R and R are di- or trimethylene and n = 1, all the other substituents are hydrogen apart from R , which is alkyl, alkenyl or aralkyl, or in which the symbols R and R are tri- or tetramethylene and n = 1, all the other substituents up to R are hydrogen and R and R are alkyl, alkenyl, aralkyl or, together with N, pyrrolidine or piperidine, also substituted by alkyl, R is hydrogen or halogen and R is halogen or trifluoromethyl, and pharmaceutically acceptable salts of basic compounds of the general formula I for producing pharmaceuticals for controlling both chloroquine-resistant and chloroquine-sensitive malaria pathogens.

    PROCESS FOR PRODUCING CEFALOSPORIN DERIVATIVES
    10.
    发明专利
    PROCESS FOR PRODUCING CEFALOSPORIN DERIVATIVES 未知

    公开(公告)号：HUT62903A

    公开(公告)日：1993-06-28

    申请号：HU9203665

    申请日：1992-11-23

    Applicant: HOFFMANN LA ROCHE

    Inventor： ANGEHRN PETER ,  FURLENMEIER ANDRE ,  HEBEISEN PAUL ,  HOFHEINZ WERNER ,  LINK HELMUT

    IPC: A61K31/545 ,  A61K20060101 ,  A61K31/546 ,  A61P31/04 ,  C07D20060101 ,  C07D501/00 ,  C07D501/18 ,  C07D501/20 ,  C07D501/34 ,  C07D501/36 ,  C07D519/00 ,  C07D519/06 ,  C07D501/46

    Abstract: Cephalosporin derivatives of the general formula in which Z and Z each individually denotes a 6-membered aromatic ring substituted by two vicinal groups -OR (in which R represents hydrogen or lower alkanoyl), which additionally contain 1 or 2 O or N atoms and/or can be substituted by halogen, carboxyl or carboxy-lower alkyl, or -X-Z and -(Q)p-Z each individually denotes a group -X -CONR OH or -(Q )p-CONR OH, in which R represents hydrogen, lower alkyl or phenyl; and in which additionally A represents a nitrogen atom or a methine group (-CH=), X represents lower alkylenephenylene, phenylene or lower alkylene which is optionally substituted by carboxyl and optionally linked to one of the groups -S-, -SO-, -SO2-, -CO-, -OCO-, -NHCO-, -NHSO2- and -CONHNHCO-, X represents lower alkylene, phenylene or lower alkylenephenylene, Y represents one of the groups -O-, -OCO-, -OCH2-, -S-, -SCO-, -SO- and -SO2-, P represents a 5- or 6- membered N-monoheterocycle which is optionally substituted by lower alkyl, phenyl, hydroxyl or oxo, or an 8- to 10-membered N-biheterocycle which is optionally substituted by lower alkyl, carboxyl, lower alkoxycarbonyl, carbamoyl, hydroxymethyl or lower alkanoyloxymethyl, Q represents lower alkylenephenylene, phenylene or lower alkylene which is optionally linked to one of the groups -CO-, -OCO-, -SO2-, -NHCO- and -NHSO2-, or one of the groups -S-, -SO-, -SO2-, -CO-, -OCO-, -NHCO-, -NHSO2- and -CONHNHCO-, Q represents lower alkylene, phenylene or lower alkylenephenylene and m, n and p in each case represent the number 0 or 1; and also easily hydrolysable esters and pharmaceutically tolerable salts of these compounds and hydrates of compounds of the formula I or of their esters and salts as well as a process for their preparation and pharmaceutical preparations which contain these compounds, and also intermediates for the preparation of these compounds, and further the use of the compounds in the control of diseases and in the production of the preparations mentioned.

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