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    RESOLVING RACEMIC MIXTURES OF BICYCLIC IMINO-ALPHA-CARBOXYLIC ESTERS
    11.
    发明专利
    RESOLVING RACEMIC MIXTURES OF BICYCLIC IMINO-ALPHA-CARBOXYLIC ESTERS 未知

    公开(公告)号：NZ206980A

    公开(公告)日：1988-05-30

    申请号：NZ20698084

    申请日：1984-01-30

    Applicant: HOECHST AG

    Inventor： GEIGER R ,  TEETZ V ,  LANGNER D ,  URBACH H ,  HENNING R

    IPC: C07D207/16 ,  C07B57/00 ,  C07D209/42 ,  C07D209/44 ,  C07D209/52 ,  C07D209/54 ,  C07K5/02 ,  C07K5/06 ,  C07K14/81

    Abstract: For the Contracting States BE CH DE FR GB IT LI LU NL SE 1. A process for resolving racemic mixtures of bicyclic imino-alpha-carboxylic esters into the components of the formula Ia and Ib see diagramm : EP0115345,P15,F1 in which R represents an aliphatic radical having 1 to 6 carbon atoms, an alicyclic radical having 4 to 10 carbon atoms, an aromatic radical having 6 to 12 carbon atoms or an araliphatic radical having 7 to 15 carbon atoms, a) A and B**1 denote hydrogen, and B**2 and C together form a chain of the formula -[CH2 ]n -, with n being 3, 4, 5 or 6, or a chain of the formula -[CH2 ]p -CH=CH-[CH2 ]q -, with (p+q) being 1, 2, 3 or 4, b) C and B**2 denote hydrogen, and A and B**1 together form a chain of the formula -[CH2 ]n -, with n bein 3, 4, 5 or 6, or a chain of the formula -[CH2 ]p -CH=CH-[CH2 ]q -, with (p+q) being 1, 2, 3 or 4, or c) A and C denote hydrogen, and B**1 and B**2 together form a chain of the formula -[CH2 ]m -, with m being 4, 5, 6 or 7, by crystallization of diastereomeric salts, which process comprises preparing the salts of the racemic esters with optically active N-acylated R- or S-aminocarboxylic acids which contain a phenyl nucleus, from the series phenylalanine, phenylglycine, beta-phenyl-alpha-aminobutyric acid, 3,4-dihydroxyphenylalalin, beta-phenylserine and tyrosine, recrystallizing them form an aprotic organic solvent or an alcohol having up to 6 carbon atoms, decomposing the precipitated, optically homogenous diastereomeric salts in a manner known per se, and isolating the enantiomers of the formula Ia or Ib, respectively, and where appropriate, converting the latter into the free acids by saponification or hydrogenolysis in a manner known per se. For the Contracting State AT 1. A process for resolving racemic mixtures of bicyclic imino-alpha-carboxylic esters into the components of the formula Ia and Ib see diagramm : EP0115345,P17,F1 in which R represents an aliphatic radical having 1 to 6 carbon atoms, an alicyclic radical having 4 to 10 carbon atoms, an aromatic radical having 6 to 12 carbon atoms or an araliphatic radical having 7 to 15 carbon atoms, a) A and B**1 denote hydrogen, and B**2 and C together form a chain of the formula -[CH2 ]n -, with n being 3, 4, 5 or 6, or a chain of the formula -[CH2 ]p -CH=CH-[CH2 ]q -, with (p+q) being 1, 2, 3 or 4, b) C and B**2 denote hydrogen, and A and B**1 together form a chain of the formula -[CH2 ]n -, with n being 3, 4, 5 or 6, or a chain of the formula -[CH2 ]p -CH=CH-[CH2 ]q -, with (p+q) being 1, 2, 3 or 4, or c) A and C denote hydrogen, and B**1 and B**2 together form a chain of the formula -[CH2 ]m -, with m being 4, 5, 6 or 7, by crystallization of diastereomeric salts, which process comprises preparing the salts of the racemic esters with optically active N-acylated R- or S-aminocarboxylic acids which contain a phenyl nucleus, from the series phenylalanine, phenylglycine, beta-phenyl-alpha-aminobutyric acid, 3,4-dihydroxyphenylalanin, beta-phenylserine and tyrosine, recrystallizing them form an aprotic organic solvent or an alcohol having up to 6 carbon atoms, decomposing the precipitated, optically homogenous diastereomeric salts in a manner known per se, and isolating the enantiomers of the formulae Ia or Ib, respectively, and, where appropriate, converting the latter into the free acids by saponification or hydrogenolysis in a manner known per se.

    1-(N-(1-CARBOXYALKYL)-ALPHA-ALKANOYL)-CIS-2,3,3A,4,5,7A- HEXAHYDRO-1H-INDOLE-2-EXOCARBOXYLIC ACIDS
    13.
    发明专利
    1-(N-(1-CARBOXYALKYL)-ALPHA-ALKANOYL)-CIS-2,3,3A,4,5,7A- HEXAHYDRO-1H-INDOLE-2-EXOCARBOXYLIC ACIDS 未知

    公开(公告)号：NZ203638A

    公开(公告)日：1987-05-29

    申请号：NZ20363883

    申请日：1983-03-21

    Applicant: HOECHST AG

    Inventor： URBACH H ,  HENNING R ,  TEETZ V ,  WISSMANN H ,  BECKER R

    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 ,  C07D209/00

    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.

    BENZOTHIAZINE DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS
    19.
    发明专利
    BENZOTHIAZINE DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS 未知

    公开(公告)号：NZ210685A

    公开(公告)日：1988-02-29

    申请号：NZ21068584

    申请日：1984-12-21

    Applicant: HOECHST AG

    Inventor： HENNING R ,  LERCH U ,  KAISER J

    IPC: A61K31/54 ,  A61K31/5415 ,  A61P3/00 ,  A61P9/00 ,  C07D279/16 ,  C07D317/00 ,  C07D417/04 ,  C07D417/12

    Abstract: Benzothiazine derivatives of the formula I (I) with (R(1), R(1)', R(1)'', R(4) and R(4)' equal to hydrogen, alkyl, alkoxy, halogen, nitro, hydroxyl, acetamido or amino; R(2) equal to hydrogen, alkyl, alkenyl, phenyl; R(3) equal to hydrogen, alkyl, alkenyl, phenyl; R(5) equal to hydrogen or (C1-C3)-alkyl; R(6) equal to one of the following groups, with R(7) and R(8) equal to hydrogen, alkyl, cycloalkyl, phenyl; R(9) equal to hydrogen, alkyl, phenyl, pyridyl, pyrimidinyl or benzoyl; R(10) equal to hydrogen, alkyl, phenyl; R(11) equal to hydrogen, hydroxyl, alkoxy or, together with R(12), a bond; and R(12) equal to hydrogen or, together with R(11), a bond; m equal to 1, 2, 3 or 4; n equal to 0 or 1; p equal to 0, 1, 2, 3 or 4, and X equal to oxygen or two hydrogen atoms, and salts of the compounds of the formula I with physiologically tolerated acids and a process for the preparation of compounds I, likewise a method of treatment of disturbances of the calcium balance of a human body are described.

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