公开(公告)号：DE3324263A1

公开(公告)日：1985-01-17

申请号：DE3324263

申请日：1983-07-06

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 ,  C07D209/02 ,  C07D403/06 ,  C07D401/06 ,  C07D401/12 ,  C07D405/06 ,  C07D413/06 ,  C07D417/06

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.

公开(公告)号：GR78901B

公开(公告)日：1984-10-02

申请号：GR830171956

申请日：1983-07-18

Applicant: HOECHST AG

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

IPC: A61K31/435 ,  A61K38/00 ,  A61P9/12 ,  C07D453/06 ,  C07K5/02

Abstract: The novel derivatives have the formula I in which n denotes 0 or 2, R denotes hydrogen, alkyl or aralkyl, R denotes hydrogen or unsubstituted or amino-, acylamino- or benzoylamino-substituted alkyl, 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, as defined above, can be substituted in the aryl radical, an S- or O- and/or N-heterocyclic radical or a side chain of an amino acid, R denotes hydrogen, alkyl, alkenyl or aralkyl, Y denotes hydrogen or hydroxyl, Z denotes hydrogen or Y and Z together denote oxygen and X denotes alkyl, alkenyl, cycloalkyl, aryl, which can be mono-, di- or trisubstituted by alkyl, alkoxy, hydroxyl, halogen, nitro, amino, alkylamino, dialkylamino and/or methylenedioxy or denotes 3-indolyl.

公开(公告)号：GR78519B

公开(公告)日：1984-09-27

申请号：GR830170831

申请日：1983-03-18

Applicant: HOECHST AG

Inventor： URBACH HANSJORG DR ,  HENNING RAINER DR ,  TEETZ VOLKER DR ,  WISSMANN HANS DR ,  BECKER REINHARD DR

IPC: A61K31/40 ,  A61K31/403 ,  A61K31/404 ,  A61K31/405 ,  A61K38/00 ,  A61K38/55 ,  A61P9/12 ,  C07D209/42 ,  C07K1/02 ,  C07K1/113 ,  C07K5/02 ,  C07K5/06 ,  C07K14/81

Abstract: The invention relates to compounds of the formula I (I) in which n denotes 0 or 1, R denotes hydrogen, alkyl or aralky, R1 denotes hydrogen or alkyl, which can optionally be substituted by amino, acylamino or benzoylamino, alkenyl, cycloalkyl, cycloalkenyl, cycloalkylalkyl, aryl or partially hydrogenated aryl, which each can be substituted by alkyl, alkoxy or halogen, arylalkyl or aroylalkyl, both of which can be substituted in the aryl radical as defined in the aforegoing, a monocyclic or bicyclic sulfur or oxygen and/or nitrogen heterocyclic radical, or a side chain of a naturally occurring aminoacid, R2 denotes hydrogen, alkyl, alkenyl or arylalkyl, Y denotes hydrogen or hydroxyl, Z denotes hydrogen or Y and Z together denote oxygen and X denotes alkyl, alkenyl, cycloalkyl, aryl, which is monosubstituted, disubstituted or trisubstituted by alkyl, alkoxy, hydroxyl, halogen, nitro, amino, alkylamino, dialkylamino or methylenedioxy or 3-indolyl, and their physiologically acceptable salts, processes for their preparation, agents containing these and their use as medicaments and also bicyclic amino acids as their intermediates and processes for their preparation.

公开(公告)号：GR77381B

公开(公告)日：1984-09-11

申请号：GR820169702

申请日：1982-11-03

Applicant: HOECHST AG

Inventor： TEETZ YOLKER DR ,  GEIGER ROLF PROF DR ,  URBACH HANSIORG DR ,  BECKER REINHARD DR ,  SCHOLKERS BERNWARD DR

IPC: C07C227/08 ,  A61K31/40 ,  A61K31/403 ,  A61K38/00 ,  A61P9/12 ,  C07C227/10 ,  C07C227/16 ,  C07C229/28 ,  C07C229/36 ,  C07C237/06 ,  C07D209/52 ,  C07D451/04 ,  C07K5/02 ,  C07K5/06

Abstract: Compounds of the formula I (I) in which the carboxyl group on carbon atom 3 is orientated in the endo-position relative to the bicyclic ring system of cis-configuration, and in which R1 denotes hydrogen, allyl, vinyl or a side-chain of a naturally occurring alpha -aminoacid, which may be protected, R2 denotes hydrogen, alkyl, alkenyl or aralkyl, Y denotes hydrogen or hydroxyl and Z denotes hydrogen, or Y and Z together denote oxygen, and X denotes alkyl, alkenyl or cycloalkyl, or aryl which is optionally mono-, di- or tri-substituted by alkyl, alkoxy, hydroxyl, halogen, nitro, amino, alkylamino, dialkylamino or methylenedioxy, or denotes indol-3-yl, a process for their preparation, agents containing these compounds and their use.

公开(公告)号：DE3246757A1

公开(公告)日：1984-06-20

申请号：DE3246757

申请日：1982-12-17

Applicant: HOECHST AG

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

IPC: A61K31/403 ,  A61K31/405 ,  A61K38/00 ,  A61P9/12 ,  A61P43/00 ,  C07D209/52 ,  C07K5/02 ,  C07D487/08 ,  A61K31/435

Abstract: Derivatives of 2-azabicyclo[2.2.1]heptane of the formula I in which n = 0 or 1, R denotes hydrogen, alkyl or aralkyl, R 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, or aralkyl or aroylalkyl which can both be substituted in the aryl radical as defined above, a mono- or bicyclic S- or O- and/or N-heterocycle radical or a side chain of an alpha -amino acid, R denotes hydrogen, alkenyl or aralkyl, Y denotes hydrogen or hydroxyl, Z denotes hydrogen or Y and Z together denote oxygen and X denotes alkyl, alkenyl, cycloalkyl, aryl which can be mono-, di- or trisubstituted by alkyl, alkoxy, hydroxyl, halogen, nitro, amino, alkylamino, dialkylamino and/or methylenedioxy, or 3-indolyl, process for their preparation, agents containing them and their use, and 2-azabicyclo[2.2.1]heptane derivatives as intermediates, and process for their preparation.