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    47.
    发明专利
    未知

    公开(公告)号：DE3684636D1

    公开(公告)日：1992-05-07

    申请号：DE3684636

    申请日：1986-05-14

    Applicant: HOECHST AG

    Inventor： URBACH HANSJOERG DR ,  HENNING RAINER DR ,  BECKER REINHARD DR

    IPC: C07D521/00 ,  A61K38/00 ,  A61K38/55 ,  A61P9/12 ,  A61P43/00 ,  C07D209/52 ,  C07K1/02 ,  C07K1/06 ,  C07K1/113 ,  C07K5/02 ,  C07K5/06 ,  C07K5/062 ,  C07K5/068 ,  C07K14/81 ,  A61K37/02

    Abstract: Bicyclic amino acid peptide derivs. of formula (I) and their physiologically innocuous salts are new. n is 0, 1 or 2; R is H, 1-6C alkyl or 7-9C aralkyl; R1 is H, 1-6C alkyl opt. substd. by amino, 1-4C acylamino or benzamido, 2-6C alkenyl, 5-9C cycloalkyl, 5-9C cycloalkenyl, (5-7C cycloalkyl)-(1-4C alkyl), aryl or partially hydrogenated aryl opt. substd. by 1-4C alkyl, 1-2C alkoxy or halogen, aryl-(1-4C alkyl) or aroyl-(1C alkyl) opt. substd. in the aryl residue by 1-4C alkyl, 1-2C alkoxy or halogen, a mono- or bicyclic heterocyclic residue with 5-7 or 8-10 ring atoms of which 1-2 are S or O and/or of which 1-4 are N, or a side-chain of a naturally occurring amino acid; R2 is H, 1-6C alkyl, 2-6C alkenyl or aryl-(1-4C alkyl); x is 1-6C alkyl, 2-6C alkenyl, 5-9C cycloalkyl, aryl opt. mono-, di- or trisubstd. by 1-4C alkyl, 1-4C alkoxy, OH, halogen, NO2, NH2, 1-4C alkylamino or di-(1-4C alkyl) amino (excluding OH, NH2 or mono-alkylamino adjacent to an olefinic C-C double bond) or 3-indolyl.

    48.
    发明专利
    未知

    公开(公告)号：DE3482385D1

    公开(公告)日：1990-07-05

    申请号：DE3482385

    申请日：1984-06-30

    Applicant: HOECHST AG

    Inventor： URBACH HANSJOERG DR ,  HENNING RAINER DR ,  BECKER REINHARD DR

    IPC: A61K31/40 ,  A61K31/403 ,  A61K31/405 ,  A61K38/00 ,  A61K38/55 ,  A61P9/12 ,  A61P43/00 ,  C07D209/52 ,  C07D221/04 ,  C07K1/113 ,  C07K5/02 ,  C07K5/06 ,  C07K5/08 ,  C07K14/81

    Abstract: The invention relates to compounds of the formula I (I) in which n denotes 0 or 1, R denotes hydrogen, alkyl, alkenyl or aralkyl, R1 denotes hydrogen or alkyl, which can optionally be substituted by amino, acylamino or benzoylamino, alkenyl, cycloalkyl, cycloalkenyl, cycloalkylalkyl, aryl or partially hydrogenated aryl, each of which can be substituted by alkyl, alkoxy or halogen, aralkyl or aroylalkyl, both of which can be substituted in the aryl radical as defined previously, a monocyclic or bicyclic S- or O- and/or N-heterocyclic radical or a side chain of an aminoacid, R2 denotes hydrogen, alkyl, alkenyl or aralkyl, Y denotes hydrogen or hydroxyl, Z denotes hydrogen, or Y and Z together denote oxygen, X denotes alkyl, alkenyl, cycloalkyl, aryl, which can be monosubstituted, disubstituted or trisubstituted by alkyl, alkoxy, hydroxyl, halogen, nitro, amino, acylamino, alkylamino, dialkylamino and/or methylenedioxy, or 3-indolyl, and to a process for their preparation, agents containing them and and their use, and to 2-azabicyclo[3.1.0]hexane derivatives as intermediates, and a process for their preparation.

    50.
    发明专利
    未知

    公开(公告)号：DE3704661A1

    公开(公告)日：1988-08-25

    申请号：DE3704661

    申请日：1987-02-14

    Applicant: HOECHST AG

    Inventor： URBACH HANSJOERG DR ,  HENNING RAINER DR ,  SCHOELKENS BERNWARD DR ,  BECKER REINHARD DR

    IPC: C07D223/32 ,  A61K31/395 ,  A61K31/445 ,  A61K31/55 ,  A61K38/00 ,  A61P9/00 ,  A61P9/12 ,  A61P27/02 ,  A61P27/06 ,  A61P43/00 ,  C07D225/04 ,  C07D401/12 ,  C07D403/06 ,  C07D403/12 ,  C07D405/12 ,  C07K5/02 ,  C07K5/06

    Abstract: Cyclopenta-azocine and -azepine derivs. of formula (I) and their salts are new. In (I) m = 1 or 2; n = 0-2; R1 and R2 = H; 1-6C alkyl (opt. substd. once by OH, SH, 1-2C alkoxy, 1-2C alkylthio, COOH, 1-2C alkoxycarbonyl, 3-indolyl, imidazolyl, CONH2, amino or guanidino); 2-6C alkenyl; 3-9C cycloalkyl or cycloalkenyl; 3-7C cycloalkyl (1-4C) alkyl; 6-12C aryl (opt. partially hydrogenated) or 6-12C aryl (1-4C) alkyl (opt. OH substd. in aryl); R3 and R4 = H, 1-6C alkyl, 2-6C alkenyl or 6-12C aryl (1-4C) alkyl, opt. substd. in aryl by one MeO or NO2; Y = H or OH; Z = H; or Y and Z are together oxo; X = 1-6C alkyl (opt. substd. by NH2, acylamino, 1-6C alkylamino and/or di(1-4C)alkylamino); 2-6C alkenyl; 5-9C cycloalkyl, 1-R1-piperidin-4-yl, 6-12C aryl (opt. substd. by 1-3 of 1-4C alkyl or alkoxy, OH, halo, NO2, NH2 (itself opt. substd. by 1 or 2 1-4C alkyl) and/or methylenedioxy) or 3-indolyl; any free OH, SH, COOH, amino or guanidino can be protected conventionally.

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