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    DERIVATI AMINODIOLA
    2.
    发明专利
    DERIVATI AMINODIOLA 未知

    公开(公告)号：YU184191A

    公开(公告)日：1994-05-10

    申请号：YU184191

    申请日：1991-11-25

    Applicant: HOECHST AG

    Inventor： WAGNER A ,  HENNING R ,  NICKEL W N

    Abstract: DERIVATI AMINODIOLA, izum se nanaša na spojine s formulo kjer W stoji za -CO-, -O-CO-, -SO2- ali -NH-CO-, Ra, R2, R4, R5, R6 in R7 stoje za vodik ali organski ostanek in R3 pomeni alkil, cikloalkil ali cikloalkilalkil, postopek za njihovo pripravo, intermediati kot tudi njihova uporaba pri pripravi inhibitor-jev renina in HIV-proteaze.

    3-(4-(1-CARBOXYALK-3-YL)-ALPHA-AMINOALKANOYL)-3-AZATRICYCLO-(5.2.1.0 2-6 ) DECAN-4-YLCARBOXYLIC ACIDS
    4.
    发明专利
    3-(4-(1-CARBOXYALK-3-YL)-ALPHA-AMINOALKANOYL)-3-AZATRICYCLO-(5.2.1.0 2-6 ) DECAN-4-YLCARBOXYLIC ACIDS 未知

    公开(公告)号：NZ206236A

    公开(公告)日：1988-03-30

    申请号：NZ20623683

    申请日：1983-11-11

    Applicant: HOECHST AG

    Inventor： URBACH H ,  HENNING R ,  BECKER R

    IPC: C07D209/70 ,  A61K31/40 ,  A61K31/403 ,  A61K38/00 ,  A61K38/55 ,  A61P9/12 ,  A61P43/00 ,  C07D209/58 ,  C07D221/22 ,  C07K1/02 ,  C07K1/113 ,  C07K5/02 ,  C07K5/06 ,  C07K14/81 ,  C07K5/04

    Abstract: The invention relates to new derivatives of tricyclic aminoacids, of the formula I (I) in which n denotes 0 or 1, A denotes -CH=CH- or -CH2-CH2-, R denotes hydrogen, alkyl or aralkyl, R1 denotes hydrogen, or alkyl, which can optionally be substituted by amino, acylamino or benzoylamino, or alkenyl, cycloalkyl, cycloalkenyl, cycloalkylalkyl, aryl or partially hydrogenated aryl, each of which can be substituted by alkyl, alkoxy or halogen, or aralkyl or aroylalkyl, both of which can be substituted as defined above, or a monocyclic or bicyclic S-, O- and/or N-heterocyclene radical, or a side chain of a naturally occurring 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, cycloalkyl, aryl, which can be mono-, di- or tri-substituted by alkyl, alkoxy, hydroxyl, halogen, nitro, amino, alkylamino, dialkylamino and/or methylenedioxy, or 3-indolyl, and physiologically acceptable salts thereof, processes for their preparation, agents containing these compounds and their use, and new bicyclic aminoacids as intermediates and processes for their preparation.

    1-- PE PYRROL-2-YL-CARBOXYLIC ACID DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS
    5.
    发明专利
    1-- PE PYRROL-2-YL-CARBOXYLIC ACID DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS 未知

    公开(公告)号：NZ202903A

    公开(公告)日：1988-01-08

    申请号：NZ20290382

    申请日：1982-12-23

    Applicant: HOECHST AG

    Inventor： URBACH H ,  HENNING R ,  TEETZ V ,  GEIGER R ,  BECKER R ,  GAUL H

    IPC: A61K38/55 ,  A61K31/40 ,  A61K31/403 ,  A61K31/404 ,  A61K38/00 ,  A61P7/10 ,  A61P9/08 ,  A61P9/12 ,  C07D209/02 ,  C07D209/08 ,  C07D209/32 ,  C07D209/34 ,  C07D209/42 ,  C07D209/52 ,  C07D215/22 ,  C07D215/227 ,  C07K1/02 ,  C07K1/113 ,  C07K5/02 ,  C07K5/06 ,  A61K31/405

    Abstract: 1. Claims for the Contracting states ; BE, CH, DE, FR, GB, IT, Li, Lu, NL, SE A compound of the formula I see diagramm : EP0084164,P21,F7 in which the hydrogen atoms on the bridgehead C atoms 3a and (6+n)a have the trans configuration relative to one another and wherein n denotes 0, 1 or 2, R1 denotes methyl, R2 denotes hydrogen, (C1 -C4 )-alkyl or benzyl, Y denotes hydrogen or hydroxyl, Z denotes hydrogen or Y and Z together denote oxygen and X denotes phenyl, and its physiologically acceptable salts. 1. Claims for the Contracting state : Austria A process for the preparation of the compounds of the formula I see diagramm : EP0084164,P24,F4 in which the hydrogen atoms on the bridgehead C atoms 3a and (6+n)a have the trans configuration relative to one another and wherein n denotes 0, 1 or 2, R1 denotes methyl, R2 denotes hydrogen, (C1 -C4 )-alkyl or benzyl, Y denotes hydrogen or hydroxyl, Z denotes hydrogen or Y and Z together denote oxygen and X denotes phenyl, and its physiologically acceptable salts, which a) comprises reacting a compound of the formula II see diagramm : EP0084164,P24,F6 wherein R1 , R2 , X, Y and Z have the meanings as in formula I, with a compound of the formula III see diagramm : EP0084164,P25,F1 in which the H atoms on the C atoms 3a and (6+n)a have the trans configuration relative to one another and wherein n denotes 0, 1 or 2 and W denotes a radical which can be cleaved off by hydrogenolysis or by acid, and subsequently splitting off the radical W and, if appropriate, the radical R2 to form the free carboxyl groups, or b) for the preparation of compounds of the formula I, in which Y and Z together denote oxygen, comprises b1 ) reacting a compound of the formula IV see diagramm : EP0084164,P25,F3 in which the H atoms on the C atoms 3a and (6+n)a have the trans configuration relative to one another and wherein n and R1 have the meanings as in formula I and W has the meaning as in formula III, with a compound of the formula V, R2 O2 C-CH = CH-CO-X wherein R2 and X have the meanings as in formula I, and subsequently splitting off the radical W and, if appropriate, also the radical R2 to form the free carboxyl groups, or, b2 ) reacting a compound of the formula IV mentioned under b1 ) with a compound of the general formula VI, wherein R2 has the meaning as in formula I, and with a compound of the general formula VII OHC-CO2 R2 X-CO-CH3 wherein X has the meaning as in formula I, subsequently splitting off the radical W and, if appropriate, the radical R2 to form the free carboxyl group, or c) for the preparation of compounds of the formula I, in which Y and Z each denote hydrogen, comprises c1 ) reacting a compound of the formula IV mentioned under b1 ) with a compound of the formula VIII see diagramm : EP0084164,P25,F2 wherein R2 and X have the meanings as in formula I, reducing the Schiff's bases obtained and subsequently splitting off the radical W and, if appropriate, the radical R2 to form the free carboxyl groups, or c2 ) catalytically reducing a compound of the formula I in which Y and Z together denote oxygen, with hydrogen, or d) for the preparation of compounds of the formula I, in which Y denotes hydroxyl and Z denotes hydrogen, comprises reducing a compound of the formula I, in which Y and Z together denote oxygen, catalytically with hydrogen or with a reducing agent, such as sodium borohydride, and, if appropriate, converting the compounds obtained according to (a)-(d) into their physiologically acceptable salts.

    A PROCESS USING ALKANEPHOSPHONIC ANHYDRIDES TO FORM PEPTIDE BONDS IN THE PRODUCTION OF ANTI-ANGIOTENSIN CONVERTING DIPEPTIDES
    10.
    发明专利
    A PROCESS USING ALKANEPHOSPHONIC ANHYDRIDES TO FORM PEPTIDE BONDS IN THE PRODUCTION OF ANTI-ANGIOTENSIN CONVERTING DIPEPTIDES 未知

    公开(公告)号：NZ209544A

    公开(公告)日：1989-04-26

    申请号：NZ20954484

    申请日：1984-09-14

    Applicant: HOECHST AG

    Inventor： URBACH H ,  TEETZ V ,  HENNING R ,  WISSMAN H

    IPC: C07K14/81 ,  A61K38/00 ,  A61P43/00 ,  C07K1/08 ,  C07K1/10 ,  C07K1/113 ,  C07K5/02 ,  C07K5/06 ,  C07K5/078 ,  C07C102/06

    Abstract: 1. A process for the preparation of a compound of the formula I see diagramm : EP0135181,P11,F1 in which n is 1 or 2, R denotes hydrogen, an optionally substituted aliphatic radical having 1 to 8 carbon atoms an optionally substituted alicyclic radical having 3-9 carbon atoms, an optionally substituted aromatic radical having 6-12 carbon atoms, an optionally substituted araliphatic radical having 7-14 carbon atoms, an optionally substituted alicyclic-aliphatic radical having 7-14 carbon atoms, or a radical OR**a or SR**a , in which R**a represents an optionally substituted aliphatic radical having 1-4 carbon atoms, an optionally substituted aromatic radical having 6-12 carbon atoms or an optionally substituted heteroaromatic radical having 5-12 ring atoms, R**1 denotes hydrogen, an optionally substituted aliphatic radical having 1 to 6 carbon atoms, an optionally substituted alicyclic radical having 3-9 carbon atoms, an optionally substituted alicyclic-aliphatic radical having 4-13 carbon atoms, an optionally substituted aromatic radical having 6-12 carbon atoms, an optionally substituted araliphatic radical having 7-16 carbon atoms, an optionally substituted heteroaromatic radical having 5-12 ring atoms, or the side chain, protected when necessary, of a naturally occurring alpha-amino acid, R**2 and R**3 are identical or different and denote hydrogen, an optionally substituted aliphatic radical having 1-6 carbon atoms, an optionally substituted alicyclic radical having 3-9 carbon atoms, an optionally substituted aromatic radical having 6-12 carbon atoms, or an optionally substituted araliphatic radical having 7-16 carbon atoms, and R**4 and R**5 , together with the atoms bearing them, form a heterocyclic, monocyclic, bicyclic or tricyclic ring system having 5 to 15 carbon atoms, which process comprises reacting a compound of the formula II see diagramm : EP0135181,P12,F4 in which n, R, R**1 and R**2 have the meanings defined above, in the presence of alkanephosphonic anhydrides, with a compound of the formula III see diagramm : EP0135181,P12,F5 in which R**3 , R**4 and R**5 have the meanings defined above, where appropriate eliminating radicals which have been introduced to protect other functional groups and, where appropriate, esterifying free carboxyl groups in a manner known per se.

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